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Imlunestrant

October 1, 2025 2:39 am / Leave a comment

Imlunestrant

CAS 2408840-26-4

as tosylate: 2408840-41-3

(5R)-5-[4-[2-[3-(fluoromethyl)azetidin-1-yl]ethoxy]phenyl]-8-(trifluoromethyl)-5H-chromeno[4,3-c]quinolin-2-ol

(5r)-5-(4-(2-(3-(fluoromethyl)azetidin-1-yl)ethoxy)phenyl)-8-(trifluoromethyl)-5h-(1)benzopyrano(4,3-c)quinolin-2-ol
5h-(1)benzopyrano(4,3-c)quinolin-2-ol, 5-(4-(2-(3-(fluoromethyl)-1-azetidinyl)ethoxy)phenyl)-8-(trifluoromethyl)-, (5r)-

MF C₂₉H₂₄F₄N₂O₃ MW 524.516

FDA 9/25/2025, Inluriyo, LY3484356, LY-3484356, To treat estrogen receptor-positive, human epidermal growth factor receptor 2-negative, estrogen receptor-1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy

Imlunestrant, sold under the brand name Inluriyo, is an anti-cancer medication used for the treatment of breast cancer.^[1] It is an is an estrogen receptor antagonist.^[1] It is used as the salt, imlunestrant tosylate.^[2] It is taken by mouth.^[1] It was developed by Eli Lilly and Company.^[2]

The most common adverse events and laboratory abnormalities include decreased hemoglobin, musculoskeletal pain, decreased calcium, decreased neutrophils, increased AST, fatigue, diarrhea, increased ALT, increased triglycerides, nausea, decreased platelets, constipation, increased cholesterol, and abdominal pain.^[2]

Imlunestrant was approved for medical use in the United States in September 2025.^[2]

SYN

Imlunestrant with or without Abemaciclib in Advanced Breast CancerPublication Name: The New England journal of medicinePublication Date: 2025-03-27PMID: 39660834DOI: 10.1056/nejmoa2410858
Targeting the Estrogen Receptor for the Treatment of Breast Cancer: Recent Advances and ChallengesPublication Name: Journal of Medicinal ChemistryPublication Date: 2023-06-28PMID: 37377342DOI: 10.1021/acs.jmedchem.3c00136
Novel endocrine therapies: What is next in estrogen receptor positive, HER2 negative breast cancer?Publication Name: Cancer Treatment ReviewsPublication Date: 2023-06PMID: 37146385DOI: 10.1016/j.ctrv.2023.102569
Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical PerspectivePublication Name: International Journal of Molecular SciencesPublication Date: 2021-07-22PMCID: PMC8345926PMID: 34360578DOI: 10.3390/ijms22157812

PAT

US10654866,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US281655517&_cid=P12-MG7DCV-14904-1

Example 1A

5-(4-{2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol, Isomer 1Separate the two enantiomers of 5-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol by chiral SFC with the following conditions: Column: LUX® Cellulose-1, 5×25 cm; eluting with a mobile phase of 30% iPrOH (with 0.5% DMEA) in CO ₂; column temperature: 40° C.; flow rate: 300 g/minute; UV detection wavelength: 270 nm to give Example 1A as the first eluting enantiomer (Isomer 1). ES/MS (m/z): 525.2 (M+H). Confirm enantiomeric enrichment of Isomer 1 by chiral analytical SFC, >99% ee, t _(R): 1.30 minutes; column: CHIRALCEL® OD-H, 4.6×150 mm; eluting with a mobile phase of 30% MeOH (0.2% IPA) in CO ₂; column temperature: 40° C.; flow rate: 5 mL/minute; UV detection wavelength: 225 nm. Isolate the title compound of Example 1B to give the second eluting enantiomer (Isomer 2). ES/MS (m/z): 525.2 (M+H). Confirm enantiomeric enrichment of Isomer 2 by chiral analytical SFC, 98% ee, t _(R): 2.03 minutes; column: CHIRALCEL® OD-H, 4.6×150 mm; eluting with a mobile phase of 30% MeOH (0.2% IPA) in CO ₂; column temperature: 40° C.; flow rate: 5 mL/minute; UV detection wavelength: 225 nm.

Alternate Preparation Example 1B

Crystalline 5-(4-{2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol, Isomer 2

Stir 5-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol, 4-methylbenzenesulfonic acid, Isomer 2 (23.8 g, 0.034 mol) in water (250 mL) at 1000 rpm. Add NaOH (76 μL) and stir the solution for 2 hours. Add DCM (600 mL). Separate the mixture, dry the DCM extract with magnesium sulfate, filter the material through a syringe filter (0.45 μm), and concentrate to dryness. Allow the material to sit under a N ₂stream over a weekend. Add 1:1 EtOH/water (80 mL) and stir the mixture with sonication. Collect a tan solid by filtration on a nylon membrane to give the title compound (10.47 g, 0.02 mol, 59%).

PAT

WO2020014435

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020014435&_cid=P12-MG7DHN-18354-1

EXAMPLE 1

Racemic 5-(4-{2-[3-(Fluoromethyl)azetidin-l-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H- [ 1 ]benzopyrano[4,3 -c]quinolin-2-ol

Cool a solution of (4-{2-[3-(fluoromethyl)azetidin-l-yl]ethoxy}phenyl){3-[2-fluoro-4-(trifluoromethyl)phenyl]-7-hydroxyquinolin-4-yl}methanone (5.27 g, 9.71 mmol) in 1,4-dioxane (100 mL) to 5 °C. Add lithium triethylborohydride (1 M in THF, 30.0 mL, 30.0 mmol). Remove the cooling bath and stir for 1.5 hours at room temperature. Quench the mixture with water. Add saturated NH₄Cl solution and EtOAc. Separate the layers and extract the aqueous layer with EtOAc. Combine the organic extracts, dry over anhydrous MgS0₄, filter, and concentrate the filtrate. Dissolve the crude residue in THF (100 mL).

Add sodium hydride (60% in mineral oil, 1.94 g, 48.5 mmol). Reflux the solution for 1.5 hours. Add additional sodium hydride (60% in mineral oil, 1.94 g, 48.5 mmol), then reflux for an additional 30 minutes. Cool the solution to room temperature and quench with water. Add EtOAc and saturated NH₄Cl solution. Separate the layers and extract the aqueous layer with EtOAc. Combine the organic extract, dry over anhydrous MgS0₄, filter, and concentrate the filtrate. Purify the residue by silica gel column chromatography eluting with a gradient of 5-7% MeOH in DCM to give the title compound (3.70 g, 72%) as a light yellow foam. ES/MS (m/z): 525.2 (M+H).

Prepare the following compounds in a manner essentially analogous to the method of Example 1, with the following variations in procedure. For the reduction, use 3 to 5 equivalents of lithium triethylborohydride with reaction times from 30 minutes to one hour and drying of the organic layers over magnesium sulfate or sodium sulfate. ETse the crude residue directly or purify by silica gel column chromatography eluting with a gradient of 0-5-7.5-10% MeOH in DCM before cyclization. Complete the cyclization by refluxing in THF for up to 16 hours, or in DMF, from 2 hours at room temperature for Ex 2, to 2 hours at 85 °C for Ex 8. Extract with DCM or EtOAc and dry organic layers over magnesium sulfate or sodium sulfate. Purify by silica gel column chromatography using up to 10% (MeOH or 7 M ammoniated MeOH) in DCM (Ex 2: gradient 0-10% MeOH in DCM; Ex 5: gradient 4-10% 7 M ammoniated MeOH in DCM; Ex 8: gradient 5-7.5% 7 M ammoniated MeOH in DCM) or by high pH reversed phase HPLC as noted.

EXAMPLE 1A

-(4-{2-[3-(Fluoromethyl)azetidin-l-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H- [l]benzopyrano[4,3-c]quinolin-2-ol, Isomer 1

and

EXAMPLE 1B

5-(4-{2-[3-(Fluoromethyl)azetidin-l-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H- [l]benzopyrano[4,3-c]quinolin-2-ol, Isomer 2

Separate the two enantiomers of 5-(4-{2-[3-(fluoromethyl)azetidin-l-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H-[l]benzopyrano[4,3-c]quinolin-2-ol by chiral SFC with the following conditions: Column: LUX® Cellulose-l, 5 x 25 cm; eluting with a mobile phase of 30% iPrOH (with 0.5% DMEA) in C0₂; column temperature: 40 °C; flow rate: 300 g/minute; UV detection wavelength: 270 nm to give Example 1 A as the first eluting enantiomer (Isomer 1). ES/MS (m/z): 525.2 (M+H). Confirm enantiomeric enrichment of Isomer 1 by chiral analytical SFC, >99% ee, /(R>: 1.30 minutes; column: CHFRALCEL® OD-H, 4.6 x 150 mm; eluting with a mobile phase of 30% MeOH (0.2% IP A) in C0₂; column temperature: 40 °C; flow rate: 5 mL/minute; UV detection wavelength: 225 nm. Isolate the title compound of Example 1B to give the second eluting enantiomer (Isomer 2). ES/MS (m/z): 525.2 (M+H). Confirm enantiomeric enrichment of Isomer 2 by chiral analytical SFC, 98% ee, /_(R>: 2.03 minutes; column: CHIRALCEL® OD-H, 4.6 x 150 mm; eluting with a mobile phase of 30% MeOH (0.2% IP A) in C0₂; column temperature: 40 °C; flow rate: 5 mL/minute; UV detection wavelength: 225 nm.

Alternate Preparation EXAMPLE 1B

Crystalline 5-(4-{2-[3-(Fluoromethyl)azetidin-l-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H- [l]benzopyrano[4,3-c]quinolin-2-ol, Isomer 2

Stir 5-(4-{2-[3-(fluoromethyl)azetidin-l-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H-[l]benzopyrano[4,3-c]quinolin-2-ol, 4-methylbenzenesulfonic acid, Isomer 2 (23.8 g, 0.034 mol) in water (250 mL) at 1000 rpm. Add NaOH (76 pL) and stir the solution for 2 hours. Add DCM (600 mL). Separate the mixture, dry the DCM extract with magnesium sulfate, filter the material through a syringe filter (0.45 pm), and concentrate to dryness. Allow the material to sit under a N₂ stream over a weekend. Add 1 : 1 EtOH/water (80 mL) and stir the mixture with sonication. Collect a tan solid by filtration on a nylon membrane to give the title compound (10.47 g, 0.02 mol, 59%).

PAT

Selective estrogen receptor degradersPublication Number: US-2023234960-A1Priority Date: 2018-07-12
Selective estrogen receptor degraderPublication Number: CN-112424205-BPriority Date: 2018-07-12Grant Date: 2023-10-31
selective estrogen receptor degraderPublication Number: CN-117379428-APriority Date: 2018-07-12
Selective estrogen receptor degradersPublication Number: US-11993608-B2Priority Date: 2018-07-12Grant Date: 2024-05-28
Selective estrogen receptor degradersPublication Number: US-12128040-B2Priority Date: 2018-07-12Grant Date: 2024-10-29

PAT

https://patents.google.com/patent/US11926634B2/en

Selective estrogen receptor degraders (SERDs) bind to the estrogen receptor (ER) and downregulate ER-mediated transcriptional activity. The degradation and downregulation caused by SERDs can be useful in the treatment of various proliferative immune mediated disorders, cell proliferation disorders, including cancers such as breast cancer, ovarian cancer, endometrial cancer, prostate cancer, uterine cancer, gastric cancer, and lung cancer as well as mutations due to emerging resistance. Some small molecule examples of SERDs have been disclosed in the literature (see, e.g., WO2005073204, WO2014205136, and WO2016097071). Nonetheless, there is a need for new SERDs to treat ER-positive cancers, such as breast cancer, gastric cancer, and/or lung cancer.

As described in U.S. Pat. No. 10,654,866 (the ‘866 patent) a series of SERDs of the following formula have been discovered, along with pharmaceutically acceptable salts thereof:

wherein one of R₁and R₂are independently Cl, F, —CF₃, or —CH₃, and the other is H.

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Clinical data

Trade names	Inluriyo
Other names	LY3484356, LY-3484356
AHFS/Drugs.com	Inluriyo
License data	US DailyMed: Imlunestrant
Routes of administration	By mouth
Drug class	Estrogen receptor antagonist
ATC code	None
Legal status
Legal status	US: ℞-only^[1]
Identifiers
IUPAC name
CAS Number	2408840-26-4as tosylate: 2408840-41-3
PubChem CID	146603228
DrugBank	DB19043
ChemSpider	115010421
UNII	9CXQ3PF69Uas tosylate: F7UDT90EW5
KEGG	D12216as tosylate: D12217
ChEMBL	ChEMBL5095183
Chemical and physical data
Formula	C₂₉H₂₄F₄N₂O₃
Molar mass	524.516 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

References

https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/218881s000lbl.pdf
“FDA approves imlunestrant for ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer”. U.S. Food and Drug Administration (FDA). 25 September 2025. Retrieved 27 September 2025. This article incorporates text from this source, which is in the public domain.
“U.S. FDA approves Inluriyo (imlunestrant) for adults with ER+, HER2-, ESR1-mutated advanced or metastatic breast cancer” (Press release). Eli Lilly. 25 September 2025. Retrieved 27 September 2025 – via PR Newswire.
World Health Organization (2022). “International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 88”. WHO Drug Information. 36 (3). hdl:10665/363551.

External links

Clinical trial number NCT04975308 for “A Study of Imlunestrant, Investigator’s Choice of Endocrine Therapy, and Imlunestrant Plus Abemaciclib in Participants With ER+, HER2- Advanced Breast Cancer (EMBER-3)” at ClinicalTrials.gov

/////////Imlunestrant, FDA 2025, APPROVALS 2025, Inluriyo, CANCER, LY3484356, LY 3484356, 9CXQ3PF69U

Dapolsertib

September 30, 2025 2:51 am / Leave a comment

Dapolsertib

CAS 1616359-00-2

MF C15H18Br2N4O MW 446.14 g/mol

5,6-dibromo-4-nitro-2-piperidin-4-yl-1-propan-2-ylbenzimidazole

5,6-dibromo-4-nitro-2-(piperidin-4-yl)-1-(propan-2-yl)-1H-1,3-benzimidazole
serine/ threonine kinase inhibitor, antineoplastic

Ryvu Therapeutics SA, MEN1703, SEL24-B489

SEL24-B489
SEL-24 free base
9M7X64VTLI
SEL-24

Dapolsertib is an investigational new drug that is being evaluated for the treatment of cancer. It is dual inhibitor of PIM family of serine/threonine protein kinases and mutant forms of FMS-related tyrosine kinase 3 (FLT3) that is being developed by Ryvu Therapeutics SA.^[1]

Dapolsertib is an orally available inhibitor of PIM family serine/threonine protein kinases and mutant forms of FMS-related tyrosine kinase 3 (FLT3; STK1) with potential antineoplastic activity. Upon oral administration, dapolsertib binds to and inhibits the kinase activities of PIM-1, -2 and -3, and mutant forms of FLT3, which may result in the interruption of the G1/S phase cell cycle transition, an inhibition of cell proliferation, and an induction of apoptosis in tumor cells that overexpress PIMs or express mutant forms of FLT3. FLT3, a tyrosine kinase receptor that is overexpressed or mutated in various cancers, plays a role in signaling pathways that regulate hematopoietic progenitor cell proliferation, and in leukemic cell proliferation and survival. PIM kinases, downstream effectors of many cytokine and growth factor signaling pathways, including the FLT3 signaling pathway, play key roles in cell cycle progression and apoptosis inhibition and may be overexpressed in various malignancies.

MEN1703 (SEL24) in Participants With Acute Myeloid LeukemiaCTID: NCT03008187Phase: Phase 1/Phase 2Status: CompletedDate: 2025-04-29
MEN1703 (SEL24) to Treat Relapsed or Refractory Aggressive B-cell Non-Hodgkin Lymphoma (JASPIS-01)CTID: NCT06534437Phase: Phase 2Status: RecruitingDate: 2025-04-11

PAT

WO2014096388

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014096388&_cid=P12-MG5YKY-59978-1

3.9. Compounds of Example 26:

5,6-dibromo-4-nitro-2-(piperidin-4-yl)-1-(propan-2-yl)-1H-1,3-benzodiazole (Example 26A):

4,5-dibromo-1-N-(propan-2-yl)benzene-1,2-diamine (2,8g, 9,lmmol) and

isonipeconic acid (1,17g, 9,lmmol) were taken up in phosphoric acid (17,82g, 0,18mol). The resulting mixture was stirred at 180°C for 3,5 hours. The mixture was allowed to cool to RT and diluted with water to 200ml. The solution was basified to pH 14.0 using solid NaOH. The resulting precipitate was then filtered off and washed repeatedly with MeOH. The filtrate was concentrated in-vacuo. The product was purified on Al₂O₃ (basic) using DCM/MeOH/NH₃ sat. in MEOH (25: 15: 1). The obtained product (8,7mmol, 3,9g) was dissolved in cone. H₂SO₄ (30ml). Next KNO₃ (8,7mmol, 0,89g) was added in one portion at 0° C. The resulting mixture was stirred at 0°C for 3h and at RT overnight. Then the mixture was poured onto ice. The product was filtered and washed with water.The product was purified on on Al₂O₃ (basic) using DCM/MeOH/NH₃ sat. in MEOH (25: 15: 1) to afford 5,6-dibromo-4- nitro-2-(piperidin-4-yl)-1-(propan-2-yl)-1H-1,3-benzodiazole (1,9g). 1H NMR (600 MHz, DMSO) δ 8.74 (bs, 1H), 8.48 (s, 1H), 8.35 (bs, 1H), 4.94 (hept, J = 6.8 Hz, 1H), 3.52 – 3.46 (m, 1H), 3.42 – 3.37 (m, 2H), 3.08 (bs, 2H), 2.07 – 1.96 (m, 4H), 1.60 (d, J = 6.9 Hz, 6H). m/z 446,8; rt 2,7min.

5,6-dibromo-4-nitro-2-(piperidin-4-yl)-1-(propan-2-yl)-1H-1,3-benzodiazole (Example 26A):

4,5-dibromo-1-N-(propan-2-yl)benzene-1,2-diamine (2,8g, 9,lmmol) and

PAT

Novel benzimidazole derivatives as kinase inhibitors

Publication Number: WO-2014096388-A2

Priority Date: 2012-12-21

Novel benzimidazole derivatives as kinase inhibitorsPublication Number: KR-20150095908-APriority Date: 2012-12-21
Benzimidazole derivatives as kinase inhibitorsPublication Number: US-10174013-B2Priority Date: 2012-12-21Grant Date: 2019-01-08
Novel Benzimidazole Derivatives as Kinase InhibitorsPublication Number: US-2015336967-A1Priority Date: 2012-12-21
Novel benzimidazole derivatives as kinase inhibitorsPublication Number: US-2017152249-A1Priority Date: 2012-12-21
Benzimidazole derivatives as Kinase InhibitorsPublication Number: US-9388192-B2Priority Date: 2012-12-21Grant Date: 2016-07-12
Novel benzimidazole derivatives as kinase inhibitorsPublication Number: EP-2935244-B1Priority Date: 2012-12-21Grant Date: 2018-06-27
Novel benzimidazole derivatives as kinase inhibitorsPublication Number: ES-2688395-T3Priority Date: 2012-12-21Grant Date: 2018-11-02
Novel benzimidazole derivatives as kinase inhibitorsPublication Number: JP-2016503779-APriority Date: 2012-12-21
Novel benzimidazole derivatives as kinase inhibitorsPublication Number: JP-6169185-B2Priority Date: 2012-12-21Grant Date: 2017-07-26
Novel benzimidazole derivatives as kinase inhibitorsPublication Number: KR-101779272-B1Priority Date: 2012-12-21Grant Date: 2017-09-18

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Clinical data

Other names	MEN1703, SEL24-B489
Identifiers
IUPAC name
CAS Number	1616359-00-2
PubChem CID	76286825
IUPHAR/BPS	13204
ChemSpider	81367232
UNII	9M7X64VTLI
ChEMBL	ChEMBL4467168
Chemical and physical data
Formula	C₁₅H₁₈Br₂N₄O₂
Molar mass	446.143 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

References

Wu M, Li C, Zhu X (December 2018). “FLT3 inhibitors in acute myeloid leukemia”. Journal of Hematology & Oncology. 11 (1) 133. doi:10.1186/s13045-018-0675-4. PMC 6280371. PMID 30514344.

//////////Dapolsertib, antineoplastic, MEN1703, SEL24-B489, MEN 1703, SEL24 B489, Ryvu Therapeutics SA

Crelosidenib

September 29, 2025 8:08 am / Leave a comment

Crelosidenib

CAS 2230263-60-0

7-{[(1S)-1-(4-{(1S)-1-[4-(prop-2-enoyl)piperazin-1-yl]-2-cyclopropylethyl}phenyl)ethyl]amino}-1-ethyl-1,4-dihydro-2Hpyrimido[4,5-d][1,3]oxazin-2-one
isocitrate dehydrogenase 1 (IDH1) inhibitor, antineoplastic

MF C28H36N6O3 MW 504.6 g/mol

LY3410738
7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-(4-prop-2-enoylpiperazin-1-yl)ethyl]phenyl]ethyl]amino]-1-ethyl-4H-pyrimido[4,5-d][1,3]oxazin-2-one
7-(((1S)-1-(4-((1S)-2-cyclopropyl-1-(4-prop-2-enoylpiperazin-1-yl)ethyl)phenyl)ethyl)amino)-1-ethyl-4H-pyrimido(4,5-d)(1,3)oxazin-2-one

Crelosidenib is an investigational new drug that is being evaluated for the treatment of cancer. It acts as a selective inhibitor of isocitrate dehydrogenase 1 (IDH1), an enzyme that plays a crucial role in cellular metabolism and is frequently mutated in various cancers, including cholangiocarcinoma.^[1][2]

Crelosidenib is an orally available inhibitor of mutant form of the isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble), including the substitution mutation at arginine (R) in position 132, IDH1(R132), with potential antineoplastic activity. Upon oral administration, crelosidenib specifically and covalently binds to and modifies a single cysteine (Cys269) in the allosteric binding pocket of mutant forms of IDH1, thereby inactivating IDH1. This inhibits the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This depletes 2-HG levels, prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing mutant forms of IDH1. In addition, crelosidenib has the ability to cross the blood-brain barrier (BBB). IDH1 mutations, including IDH1(R132) mutations, are highly expressed in certain malignancies, including gliomas; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.

Syn

example 2 [US11001596B2]

https://patentscope.wipo.int/search/en/detail.jsf?docId=US289829390&_cid=P12-MG4UBU-88518-1

PAT

7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitorsPublication Number: US-2021206780-A1Priority Date: 2016-12-16
7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitorsPublication Number: US-2021230185-A1Priority Date: 2016-12-16
7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitorsPublication Number: CA-3045303-CPriority Date: 2016-12-16Grant Date: 2022-05-17
7-phenylethylamino-4H-pyrimido [4,5-D ] [1,3] oxazin-2-one compounds as inhibitors of mutant IDH1 and IDH2Publication Number: CN-110072867-BPriority Date: 2016-12-16Grant Date: 2022-07-08
Mutant IDH1 and IDH2 inhibitorsPublication Number: CN-115109075-APriority Date: 2016-12-16

Pyrido[4,3-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitorsPublication Number: EP-3763717-B1Priority Date: 2016-12-16Grant Date: 2023-03-08
7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitorsPublication Number: US-11629156-B2Priority Date: 2016-12-16Grant Date: 2023-04-18
7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitorsPublication Number: US-11649247-B2Priority Date: 2016-12-16Grant Date: 2023-05-16

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Clinical data

Other names	LY3410738
Identifiers
IUPAC name
CAS Number	2230263-60-0
PubChem CID	135125140
IUPHAR/BPS	12340
ChemSpider	115009279
UNII	A4DU555RMD
KEGG	D12708
Chemical and physical data
Formula	C₂₈H₃₆N₆O₃
Molar mass	504.635 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

References

Zarei M, Hue JJ, Hajihassani O, Graor HJ, Katayama ES, Loftus AW, et al. (February 2022). “Clinical development of IDH1 inhibitors for cancer therapy”. Cancer Treatment Reviews. 103 102334. doi:10.1016/j.ctrv.2021.102334. PMID 34974243.
Demir T, Moloney C, Mahalingam D (July 2024). “Emerging targeted therapies and strategies to overcome resistance in biliary tract cancers”. Critical Reviews in Oncology/Hematology. 199 104388. doi:10.1016/j.critrevonc.2024.104388. PMID 38754771.

.///////////Crelosidenib, Antineoplastic, cholangiocarcinoma, LY3410738, LY 3410738

Copper (64Cu) adarulatide tetraxetan

September 29, 2025 2:50 am / Leave a comment

Copper (64Cu) adarulatide tetraxetan

Adarulatide tetraxetan copper Cu-64

CAS 2841388-40-5

MF C76H10764CuN17O22, MF1,674.7

Cuprate(3-)-⁶⁴Cu, [N-[2-[4,10-bis[(carboxy-κO)methyl]-7-(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl-κN¹,κN⁴,κN⁷,κN¹⁰ ]acetyl]-L-α-aspartyl-3-cyclohexyl-L-alanyl-L-phenylalanyl-D-seryl-D-arginyl-L-tyrosyl-L-leucyl-L-tryptophanyl-L-serinato(5-)]-, hydrogen (1:3)

N-({4,10-bis[(carboxylato-κO)methyl]-7- (carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-ylκ4 N1 ,N4 ,N7 ,N10}acetyl)-L-α-aspartyl-3-cyclohexyl-Lalanyl-L-phenylalanyl-D-seryl-D-arginyl-L-tyrosyl-L-leucylL-tryptophyl-L-serinecopper

2-[4-[2-[[(2S)-3-carboxy-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]-7-(carboxylatomethyl)-10-(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate;copper-64(2+)
diagnostic imaging agent, QM8HMM6RJP

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///////////Copper (64Cu) adarulatide tetraxetan. diagnostic imaging agent, QM8HMM6RJP

Claziprotamide

September 28, 2025 2:28 am / Leave a comment

Claziprotamide

CAS 2361124-03-8, BBP 671

MF C19H20ClFN4O MW374.8 g/mol

1-[4-(6-chloropyridazin-3-yl)piperazin-1-yl]-2-(4-cyclopropyl-3-fluorophenyl)ethan-1-one

1-[4-(6-chloropyridazin-3-yl)piperazin-1-yl]-2-(4-cyclopropyl-3-fluorophenyl)ethan-1-one
pantothenate kinases 1 and 3 (PanK1 and PanK3) positive allosteric modulator

Claziprotamide is an investigational new drug that is being evaluated for the treatment of rare metabolic disorders such as pantothenate kinase-associated neurodegeneration (PKAN) and neurodegeneration with brain iron accumulation (NBIA). It acts as a positive allosteric modulator (PAM) of pantothenate kinases 1 and 3 (PANK1 and PANK2) which are critical for coenzyme A biosynthesis and cellular metabolism.^[1][2]

PAT

US11891378,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US319558593&_cid=P22-MG32VL-67777-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019133635&_cid=P22-MG32PO-63930-1

SCHEME 4B.

[00184] In one aspect, compounds of type 4.8, and similar compounds, can be prepared according to reaction Scheme 4B above. Thus, compounds of type 4.6 can be prepared by a urea bond formation reaction between an appropriate amine, e.g., 4.2 as shown above, and an appropriate isocyanate, e.g., 4.5 as shown above. Appropriate amines and appropriate isocyanates are commercially available or prepared by methods known to one skilled in the art. The nucleophilic substitution is carried out in the presence of an appropriate solvent, e.g., diethyl ether, for an appropriate period of time, e.g., 3 hours. The nucleophilic substitution is followed by a deprotection reaction. The deprotection reaction is carried out in the presence of an appropriate deprotecting agent, e.g., trifluoroacetic acid, in an appropriate solvent, e.g., dichloromethane, for an appropriate period of time, e.g., 1 hour. Compounds of type 4.8 can be prepared by an arylation reaction of appropriate amine, e.g., 4.6 as shown above, and an appropriate aryl halide, e.g., 4.7 as shown above. Appropriate aryl halides are commercially available or prepared by methods known to one skilled in the art. The arylation reaction is carried out in the presence of an appropriate base, e.g., triethylamine, in an appropriate solvent, e.g., acetonitrile, at an appropriate temperature, e.g, 160 °C, for an appropriate period of time, e.g., 30 minutes using microwave irradiations. As can be appreciated by one skilled in the art, the above reaction provides an example of a generalized approach wherein compounds similar in structure to the specific reactants above (compounds similar to compounds of type 3.6, 4.1, 4.2, and 4.3), can be substituted in the reaction to provide 4-aryl-N-phenylpiperazine-l -carboxamide derivatives similar to Formula 4.4.

PAT

Methods of treating disorders associated with castorPublication Number: US-2023321092-A1Priority Date: 2017-12-27
Small molecule modulators of pantothenate kinasesPublication Number: US-11891378-B2Priority Date: 2017-12-27Grant Date: 2024-02-06
Small molecule modulators of pantothenate kinasesPublication Number: US-2024287039-A1Priority Date: 2017-12-27
Small molecule modulator of pantothenate kinasePublication Number: KR-102728619-B1Priority Date: 2017-12-27Grant Date: 2024-11-08
Small molecule modulators of pantothenate kinasesPublication Number: US-2021061788-A1Priority Date: 2017-12-27
Methods of treating disorders associated with castorPublication Number: US-11547709-B2Priority Date: 2017-12-27Grant Date: 2023-01-10
Small molecule modulators of pantothenate kinasesPublication Number: AU-2018395222-B2Priority Date: 2017-12-27Grant Date: 2023-06-08
Small molecule modulators of pantothenate kinasePublication Number: CN-111818922-BPriority Date: 2017-12-27Grant Date: 2023-06-13
Small molecule modulators of pantothenate kinasePublication Number: JP-7352565-B2Priority Date: 2017-12-27Grant Date: 2023-09-28
Small molecule modulators of pantothenate kinasesPublication Number: EP-3731844-A1Priority Date: 2017-12-27
Small molecule modulators of pantothenate kinasePublication Number: KR-20200130242-APriority Date: 2017-12-27
MODULATORS OF SMALL MOLECULES OF PANTOTENATE KINASESPublication Number: BR-112020012875-A2Priority Date: 2017-12-27
Small molecule modulator of pantothenate kinasePublication Number: JP-2021508739-APriority Date: 2017-12-27
Methods of treating disorders associated with castorPublication Number: US-2021023081-A1Priority Date: 2017-12-27
Treatment of organic acidemias or pantothenate kinase associated neurodegeneration with modulators of pantothenate kinasesPublication Number: WO-2023230560-A1Priority Date: 2022-05-26
Methods of treating disorders associated with castorPublication Number: WO-2022133034-A1Priority Date: 2020-12-16
Small molecule modulators of pantothenate kinasesPublication Number: WO-2019133635-A1Priority Date: 2017-12-27
Small molecule modulators of pantothenate kinasesPublication Number: AU-2018395222-A1Priority Date: 2017-12-27
Small molecule modulators of pantothenate kinasePublication Number: CN-111818922-APriority Date: 2017-12-27

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Clinical data

Other names	BBP-671
Identifiers
IUPAC name
CAS Number	2361124-03-8
PubChem CID	142616838
ChemSpider	129431674
UNII	74N47PKZ3K
PDB ligand	Y92 (PDBe, RCSB PDB)
Chemical and physical data
Formula	C₁₉H₂₀ClFN₄O
Molar mass	374.84 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

References

Tangallapally R, Subramanian C, Yun MK, Edwards A, Sharma LK, Yang L, et al. (August 2024). “Development of Brain Penetrant Pyridazine Pantothenate Kinase Activators”. Journal of Medicinal Chemistry. 67 (16): 14432–14442. doi:10.1021/acs.jmedchem.4c01211. PMC 11345825. PMID 39136313.
“Claziprotamide”. PatSnap.

/////////Claziprotamide, BBP 671, ORPHAN DRUG

Camibirstat

September 27, 2025 5:24 am / Leave a comment

Camibirstat

CAS 2671128-05-3

N-{(2S)-1-[(4-{6-[(2R,6S)-2,6-dimethylmorpholin-4-yl]pyridin-2-yl}-1,3-thiazol-2-yl)amino]-3-methoxy-1-oxopropan-2-yl}-1-(methanesulfonyl)-1H-pyrrole-3-carboxamide
ATPase inhibitor, antineoplastic

MW C24H30N6O6S2 MF 562.7 g/mol

1H-Pyrrole-3-carboxamide, N-((1S)-2-((4-(6-((2R,6S)-2,6-dimethyl-4-morpholinyl)-2-pyridinyl)-2-thiazolyl)amino)-1-(methoxymethyl)-2-oxoethyl)-1-(methylsulfonyl)-
N-[(2S)-1-[[4-[6-[(2S,6R)-2,6-dimethylmorpholin-4-yl]pyridin-2-yl]-1,3-thiazol-2-yl]amino]-3-methoxy-1-oxopropan-2-yl]-1-methylsulfonylpyrrole-3-carboxamide
FHD 286

Camibirstat is an investigational new drug that is being evaluated for the treatment of cancer. It is a small molecule that acts as a selective inhibitor of SMARCA2 and SMARCA4, which are key components of the SWI/SNF chromatin remodeling complex.^[1]

It is being developed by Foghorn Therapeutics.^[2]

Camibirstat is an orally bioavailable, allosteric, small molecule inhibitor of transcription activator BRG1 (SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 4; SMARCA4) and BRM (SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2; SMARCA2), with potential antineoplastic activity. Upon oral administration, camibirstat targets, binds to, and inhibits the activity of BRG1 and/or BRM, the primary ATPase components and mutually exclusive subunits of the BRG1/BRM-associated factor (BAF) complexes. This may lead to the inhibition of the SWI/SNF chromatin remodeling complex, disrupt chromatin remodeling and gene expression, and result in the downregulation of oncogenic pathways and the inhibition of tumor cell proliferation. BAF is an important regulator of transcriptional programs and gene expression. Mutations in BAF or its transcription factor partners are found in certain diseases including cancers.

PAT

Compounds and uses thereofPublication Number: US-2024101550-A1Priority Date: 2020-01-29
Compounds and their usesPublication Number: JP-7561195-B2Priority Date: 2020-01-29Grant Date: 2024-10-03
Compounds and uses thereofPublication Number: TW-I859406-BPriority Date: 2020-01-29Grant Date: 2024-10-21
Compounds and uses thereofPublication Number: IL-295100-APriority Date: 2020-01-29
Compounds and uses thereofPublication Number: KR-20220133258-APriority Date: 2020-01-29
Compounds and uses thereofPublication Number: US-11485732-B2Priority Date: 2020-01-29Grant Date: 2022-11-01
Compounds and uses thereofPublication Number: JP-2023512039-APriority Date: 2020-01-29
Compounds and uses thereofPublication Number: US-2023129003-A1Priority Date: 2020-01-29
Compounds and uses thereofPublication Number: WO-2021155262-A1Priority Date: 2020-01-29
Compounds and uses thereofPublication Number: TW-202136252-APriority Date: 2020-01-29
Compounds and uses thereofPublication Number: AU-2021213811-A1Priority Date: 2020-01-29
Compound and use thereofPublication Number: CN-115023226-APriority Date: 2020-01-29
Compounds and uses thereofPublication Number: EP-4096664-A1Priority Date: 2020-01-29
Methods of treating cancersPublication Number: WO-2021236080-A1Priority Date: 2020-05-20
Methods of treating cancersPublication Number: EP-4153176-A1Priority Date: 2020-05-20
ways to treat cancerPublication Number: CN-115867314-APriority Date: 2020-05-20
how to treat cancerPublication Number: JP-2023535124-APriority Date: 2020-05-20
Compounds and uses thereofPublication Number: US-2021230154-A1Priority Date: 2020-01-29
Treatment options with inhibitors of BRG1 and BRM enzyme activityPublication Number: CN-117337179-APriority Date: 2021-03-19
Therapeutic regimens of an inhibitor of the enzymatic activity of brg1 and brmPublication Number: EP-4308124-A1Priority Date: 2021-03-19
Treatment regimens for inhibitors of BRG1 and BRM enzymatic activityPublication Number: JP-2024511383-APriority Date: 2021-03-19
Therapeutic regimens of an inhibitor of the enzymatic activity of brg1 and brmPublication Number: US-2024189318-A1Priority Date: 2021-03-19
Methods of treating cancersPublication Number: US-2022079940-A1Priority Date: 2020-05-20

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US331910582&_cid=P11-MG1TKU-39131-1

Example 1. Preparation of N—((S)-1-((4-(6-(cis-2,6-dimethylmorpholino)pyridin-2-yl)thiazol-2-yl)amino)-3-methoxy-1-oxopropan-2-yl)-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide

N—((S)-1-((4-(6-(cis-2,6-dimethylmorpholino)pyridin-2-yl)thiazol-2-yl)amino)-3-methoxy-1-oxopropan-2-yl)-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide was synthesized as shown in Scheme 1 below.

Step 7: Preparation of N—((S)-1-((4-(6-(cis-2,6-dimethylmorpholino)pyridin-2-yl)thiazol-2-yl)amino)-3-methoxy-1-oxopropan-2-O-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide

To a solution of 1-methylsulfonylpyrrole-3-carboxylic acid (Intermediate K) (2.43 g, 12.9 mmol), EDCI (2.69 g, 14.0 mmol), HOBt (1.89 g, 14.0 mmol), and DIPEA (10.2 mL, 58.4 mmol) in dichloromethane (50 mL) was added Intermediate J (5.00 g, 11.7 mmol). After stirring at room temperature for 4 h, the reaction mixture was concentrated under reduced pressure. The residue was diluted with water and extracted three times with ethyl acetate. The combined organic layers were washed three times with saturated aqueous NH ₄Cl, once with brine, dried over Na ₂SO ₄, filtered, and concentrated under reduced pressure to give a residue. The residue was purified by silica gel column chromatography (petroleum ether:ethyl acetate=1:1 to 1:2). The residue was triturated with methyl tert-butyl ether. After 0.5 h, the suspension was filtered, the filter cake was washed with methyl tert-butyl ether, and dried in vacuo. The solid was dissolved in dimethyl sulfoxide (12 mL) and added dropwise to water (800 mL). The suspension was filtered to give wet filter cake. The filter cake was suspended in water and stirred at room temperature. After 1 hour, the solid was collected by filtration, washed three times with water and dried in vacuo to give N—((S)-1-((4-(6-(cis-2,6-dimethylmorpholino)pyridin-2-yl)thiazol-2-yl)amino)-3-methoxy-1-oxopropan-2-yl)-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide (3.9 g, 6.93 mmol, 59.3% yield) as a white solid.

LCMS (ESI) m/z: [M+H] ⁺=563.1.

¹H NMR (400 MHz, DMSO-d6) δ 12.49 (br s, 1H), 8.51 (d, J=7.2 Hz, 1H), 7.98-7.97 (m, 1H), 7.78 (s, 1H), 7.67-7.57 (m, 1H), 7.29-7.27 (m, 1H), 7.26 (d, J=7.2 Hz, 1H), 6.88-6.74 (m, 2H), 4.94-4.91 (m, 1H), 4.25 (d, J=11.6 Hz, 2H), 3.77-3.67 (m, 2H), 3.63-3.62 (m, 2H), 3.57 (s, 3H), 3.31 (s, 3H), 2.44-2.38 (m, 2H), 1.18 (d, J=6.0 Hz, 6H).

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Clinical data

Other names	FHD286
Identifiers
IUPAC name
CAS Number	2671128-05-3
PubChem CID	156818030
ChemSpider	115010237
UNII	QHA5XLA4SA
ChEMBL	ChEMBL5095181
Chemical and physical data
Formula	C₂₄H₃₀N₆O₆S₂
Molar mass	562.66 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

References

Yu L, Wu D (July 2024). “SMARCA2 and SMARCA4 Participate in DNA Damage Repair”. Frontiers in Bioscience (Landmark Edition). 29 (7): 262. doi:10.31083/j.fbl2907262. PMID 39082357.
“Camibirstat”. PatSnap.

/////////////Camibirstat, ATPase inhibitor, antineoplastic, Foghorn Therapeutics, FHD 286

Pharma Eurasia 2026, supported by Ministry of Health, Republic of Uzbekistan!

September 27, 2025 3:14 am / Leave a comment

Uzbekistan calling…

Excited to announce Pharma Eurasia 2026, supported by the Pharmaceutical Industry Development Agency and the Ministry of Health, Republic of Uzbekistan! Join 400+ exhibitors and 7000+ industry visitors from across the globe from 20–22 May 2026 at the Tashkent Pharma Park, Uzbekistan – your gateway to pharma opportunities in the CIS & Eurasia region.

Contact: +91-9526974225 (M. Harikrishnan)

Visit: www.pharmedxworld.com

About Pharma Eurasia

Pharma Eurasia is more than just an exhibition — it’s your gateway to the most dynamic pharmaceutical markets in Central Asia, CIS, and Eurasia. Taking place on 20–22 May 2026 in Tashkent, Uzbekistan, the event unites global manufacturers, exporters, regional distributors, and investors — bringing the entire pharma ecosystem under one roof.

Here, industry leaders connect, collaborate, and explore opportunities to shape the future of pharmaceuticals in one of the world’s fastest-growing hubs.

Why Tashkent

Position your business at the heart of Central Asia’s trade crossroads. Tashkent offers unmatched connectivity to CIS, Eurasian, Middle Eastern, and South Asian markets — supported by government incentives, zero-duty pharma zones, and a rapidly growing demand for medicines and medical technology.

Join us in Tashkent, Uzbekistan, from 20–22 May 2026, and unlock the gateway to new partnerships, expanding networks, and a market ready for your products.

SPSR Excellence Award 2025 – SPSR Global Pharmacist Excellence Awards 2025

September 27, 2025 3:03 am / 1 Comment on SPSR Excellence Award 2025 – SPSR Global Pharmacist Excellence Awards 2025

Honoured to get SPSR Excellence Award 2025 – SPSR Global Pharmacist Excellence Awards 2025
From the Society of Pharmaceutical Sciences and Research (SPSR)!
In recognition of your excellent work and valuable contributions in the field of Pharmaceutical Sciences and allied disciplines, it gives us great pleasure to confer upon you the:
SPSR Excellence Award 2025 – SPSR Global Pharmacist Excellence Awards 2025
This prestigious award will be conferred during the:
101st SPSR International Webinar & SPSR World Pharmacists Day Excellence Awards 2025
Theme: “Think Health, Think Pharmacist”
Event Details
Date: Thursday, 25th September 2025
Time: 8:00 PM – 10:00 PM IST
Mode: Online (YouTube Live)
YouTube Link: https://youtube.com/live/BcUPHOGweIA?feature=share
The SPSR World Pharmacist Day Excellence Awards are instituted to acknowledge individuals who have demonstrated outstanding dedication, innovation, and impact in advancing pharmacy, healthcare, and allied sciences.
We extend our heartfelt congratulations and look forward to honoring your achievements on this prestigious occasion.
Warm regards,
Mrs. Monika Sabharwal
Founder and National Secretary
Society of Pharmaceutical Sciences and Research (SPSR)
Website – www.spsrpharma.org
Email – secretary@spsrpharma.org
Follow us – https://in.linkedin.com/company/spsr2010
SPSR WhatsApp Channel – https://whatsapp.com/channel/0029Va8rRBpDZ4LjgD2QQV0P

Brimarafenib

September 26, 2025 2:31 am / Leave a comment

Brimarafenib

CAS 1643326-82-2

MF C24H17F3N4O4 MW482.4 g/mol

N-{(1S,1aS,6bS)-5-[(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-4-yl)oxy]-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-1-yl}-N′-(2,4,5-trifluorophenyl)urea
rapidly accelerated fibrosarcoma (Raf) kinase inhibitor,

1-((1S,1aS,6bS)-5-((7-oxo-6,8-dihydro-5H-1,8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa(b)(1)benzofuran-1-yl)-3-(2,4,5-trifluorophenyl)urea
1-[(1S,1aS,6bS)-5-[(7-oxo-6,8-dihydro-5H-1,8-naphthyridin-4-yl)oxy]-1a,6b-dihydro-1H-cyclopropa[b][1]benzofuran-1-yl]-3-(2,4,5-trifluorophenyl)urea

Antineoplastic, MapKure, LLC, SpringWorks Therapeutics, BeiGene, BGB-3245, BGB 3245, GXS33OY2CB

Brimarafenib is an investigational new drug that is being evaluated for the treatment of cancer. It targets the proto-oncogene BRAF with activating mutations BRAF mutations (such as V600E), non-V600 BRAF mutations, and RAF fusions.^[1]^[2]

It is being developed by MapKure, LLC, a joint venture between SpringWorks Therapeutics and BeiGene.^[1]

Brimarafenib is an orally available inhibitor of both monomer and dimer forms of activating mutations of the serine/threonine-protein kinase BRAF (B-raf) protein, including V600 BRAF mutations, non-V600 BRAF mutations, and RAF fusions, with potential antineoplastic activity. Upon administration, brimarafenib targets and binds to both monomeric and dimeric forms of activating BRAF mutations and fusions. This may result in the inhibition of BRAF-mediated signaling and inhibit proliferation in tumor cells expressing BRAF mutations and fusions. BRAF belongs to the RAF family of serine/threonine protein kinases and plays a role in regulating the mitogen-activated protein kinase (MAPK)/ extracellular signal-regulated kinase (ERK) signaling pathway, which is often dysregulated in human cancers and plays a key role in tumor cell proliferation and survival. BRAF mutations and fusions have been identified in a number of solid tumors and are drivers of cancer growth.

PAT

US9670203

PAT

WO2014206343

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014206343&_cid=P22-MG0802-32937-1

PAT

Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors

Publication Number: WO-2014206343-A1

Priority Date: 2013-06-28

Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitorsPublication Number: US-2016368914-A1Priority Date: 2013-06-28
Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitorsPublication Number: US-2017233391-A1Priority Date: 2013-06-28
Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitorsPublication Number: US-2019144446-A1Priority Date: 2013-06-28
Fused tricyclic urea compounds as Raf kinase and/or Raf kinase dimer inhibitorsPublication Number: US-9670203-B2Priority Date: 2013-06-28Grant Date: 2017-06-06
Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitorsPublication Number: US-9920055-B2Priority Date: 2013-06-28Grant Date: 2018-03-20

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Clinical data

Other names	BGB-3245
Identifiers
IUPAC name
CAS Number	1643326-82-2
PubChem CID	117807031
IUPHAR/BPS	13203
ChemSpider	129144353
UNII	GXS33OY2CB
Chemical and physical data
Formula	C₂₄H₁₇F₃N₄O₄
Molar mass	482.419 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

References

“Brimarafenib”.
Tellenbach FL, Seiler LL, Johnson M, Rehrauer H, Schukla P, Martinez-Gomez J, et al. “Combination of the Novel Raf Dimer Inhibitor Brimarafenib with the Mek Inhibitor Mirdametinib is Effective Against Nras Mutant Melanoma”. SSRN: 4934723. doi:10.2139/ssrn.4934723.

///////Brimarafenib, Antineoplastic, MapKure, LLC, SpringWorks Therapeutics, BeiGene, BGB-3245, BGB 3245, GXS33OY2CB

Brezivaptan

September 25, 2025 2:53 am / Leave a comment

Brezivaptan

CAS 1370444-22-6

ANC-501, THY-1773, TS-121, 575OB1CKN0

MF C25H30ClN5O3 MW 484.0 g/mol

2-[3-(3-chlorophenyl)-1-{4-[2-(morpholin-4-yl)ethyl]phenyl}-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]-N-(propan-2-yl)acetamide

2-[3-(3-chlorophenyl)-1-[4-(2-morpholin-4-ylethyl)phenyl]-5-oxo-1,2,4-triazol-4-yl]-N-propan-2-ylacetamide
vasopressin receptor antagonist

ANC-501 in the Treatment of Adults With Major Depressive DisorderCTID: NCT05439603Phase: Phase 2Status: CompletedDate: 2024-12-31
A Study to Evaluate the Safety and Efficacy of TS-121 as an Adjunctive Treatment for Major Depressive DisorderCTID: NCT03093025Phase: Phase 2Status: TerminatedDate: 2020-07-14
Exploratory Study Using Positron Emission Tomography With TS-121 and [11C]TASP0410699 in Healthy Adult Male SubjectsCTID: NCT02448212Phase: Phase 1Status: CompletedDate: 2017-02-14

Brezivaptan^[1] (developmental code names ANC-501, THY-1773, TS-121) is an orally active, selective vasopressin V_1B receptor antagonist which is under development by Taisho Pharmaceutical for the adjunctive treatment of major depressive disorder.^[2][3][4] As of November 2022, it is in phase II clinical trials for this indication.^[2][3][5]

ANC-501 is under investigation in clinical trial NCT05439603 (ANC-501 in the Treatment of Adults With Major Depressive Disorder).

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US90328697&_cid=P11-MFYT6K-98384-1

Synthesis of Example Aa-1

2-[3-(3-Chlorophenyl)-1-{4-[2-(morpholin-4-yl)ethyl]phenyl}-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]-N-(propan-2-yl)acetamide

A mixture of the compound (100 mg) prepared in Reference Example P-I1, morpholine (0.03 mL), N,N-diisopropylethylamine (0.35 mL), and MeCN (3.00 mL) was stirred at an outside temperature of 80° C. overnight. After cooling, the solvent was distilled off under reduced pressure. The residue was purified by column chromatography (SNAP Cartridge HP-Sil: 10 g, mobile phase: CHCl ₃/MeOH=98/2 to 85/15 (v/v); and SNAP Cartridge KP-NH: 28 g, mobile phase: n-hexane/CHCl ₃=80/20 to 0/100 (v/v)) and preparative thin-layer chromatography (PTLC) (1.0 mm silica gel 60F ₂₅₄plate, mobile phase: EtOAc/MeOH=95/5 (v/v)). The resulting crude product was washed with a solvent mixture of EtOAc and n-hexane (EtOAc/n-hexane=1/4 (v/v)) with stirring to yield the title compound (70 mg, colorless solid).

MS (ESI pos.) m/z: 484 ([M+H] ⁺).

¹H-NMR (600 MHz, CDCl ₃)δ(ppm); 1.20 (6H, d, J=6.4 Hz), 2.48-2.67 (6H, m), 2.80-2.88 (2H, m), 3.76 (4H, br. s.), 4.06-4.13 (1H, m), 4.36 (2H, s), 6.37-6.45 (1H, m), 7.31 (2H, d, J=8.3 Hz), 7.46-7.50 (1H, m), 7.51-7.55 (1H, m), 7.74-7.77 (1H, m), 7.85-7.88 (1H, m), 7.94 (2H, d, J=8.7 Hz).

PAT

1,2,4-triazolone derivativePublication Number: NZ-608729-APriority Date: 2010-10-01
1, 2, 4-triazolone derivativePublication Number: US-2013197217-A1Priority Date: 2010-10-01
1, 2, 4-triazolone derivative and use thereof as an antagonist on the arginine-vasopressin 1B receptorPublication Number: US-9193695-B2Priority Date: 2010-10-01Grant Date: 2015-11-24
1,2,4-triazolone derivative, substance and pharmaceutical compositionPublication Number: BR-112013007389-B1Priority Date: 2010-10-01
1,2,4-triazolone derivativePublication Number: EP-2623499-A1Priority Date: 2010-10-01
1,2,4-triazolone derivativePublication Number: EP-2623499-B1Priority Date: 2010-10-01Grant Date: 2015-04-22
DERIVAT 1,2,4-TRIAZOLONAPublication Number: HR-P20150462-T1Priority Date: 2010-10-01
1,2,4-triazolone derivativePublication Number: HU-E025729-T2Priority Date: 2010-10-01
1,2,4-triazolone derivativePublication Number: IL-225091-APriority Date: 2010-10-01
Methods of treating depression with 1,2,4-triazolone derivativesPublication Number: WO-2023235785-A1Priority Date: 2022-06-01
1,2,4-triazolone derivativePublication Number: AU-2011308403-A1Priority Date: 2010-10-01
1,2,4-triazolone derivativePublication Number: AU-2011308403-B2Priority Date: 2010-10-01Grant Date: 2014-08-21
1,2,4-Triazolone DerivativesPublication Number: CN-103119028-APriority Date: 2010-10-01
1,2,4-Triazolone DerivativesPublication Number: CN-103119028-BPriority Date: 2010-10-01Grant Date: 2016-05-25

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References

PubChem. “Brezivaptan”. pubchem.ncbi.nlm.nih.gov. Retrieved 2024-08-15.
“TS 121 -“. AdisInsight. Springer Nature Switzerland AG.
“New Drug Pipeline – Taisho Pharmaceutical Holdings”.
Kamiya M, Sabia HD, Marella J, Fava M, Nemeroff CB, Umeuchi H, Iijima M, Chaki S, Nishino I (September 2020). “Efficacy and safety of TS-121, a novel vasopressin V1B receptor antagonist, as adjunctive treatment for patients with major depressive disorder: A randomized, double-blind, placebo-controlled study”. Journal of Psychiatric Research. 128: 43–51. doi:10.1016/j.jpsychires.2020.05.017. PMID 32521250. S2CID 219587135.
Inatani S, Mizuno-Yasuhira A, Kamiya M, Nishino I, Sabia HD, Endo H (May 2021). “Prediction of a clinically effective dose of THY1773, a novel V1B receptor antagonist, based on preclinical data”. Biopharmaceutics & Drug Disposition. 42 (5): 204–217. doi:10.1002/bdd.2273. PMC 8252455. PMID 33734452.

External links

Clinical trial number NCT03093025 for “A Study to Evaluate the Safety and Efficacy of TS-121 as an Adjunctive Treatment for Major Depressive Disorder” at ClinicalTrials.gov

Clinical data

Other names	TS-121; TS121; TS-1211; TS1211; THY1773; THY-1773; ANC-501; ANC501
Routes of administration	By mouth
Identifiers
IUPAC name
CAS Number	1370444-22-6
PubChem CID	56952080
DrugBank	DB18907
ChemSpider	129325033
UNII	575OB1CKN0
ChEMBL	ChEMBL5314910
Chemical and physical data
Formula	C₂₅H₃₀ClN₅O₃
Molar mass	484.00 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

////////////Brezivaptan, ANC-501, THY-1773, TS-121, ANC 501, THY 1773, TS 121, 575OB1CKN0

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Example 1A

Alternate Preparation Example 1B

Crystalline 5-(4-{2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol, Isomer 2

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Example 1. Preparation of N—((S)-1-((4-(6-(cis-2,6-dimethylmorpholino)pyridin-2-yl)thiazol-2-yl)amino)-3-methoxy-1-oxopropan-2-yl)-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide

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Synthesis of Example Aa-1

2-[3-(3-Chlorophenyl)-1-{4-[2-(morpholin-4-yl)ethyl]phenyl}-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]-N-(propan-2-yl)acetamide

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