DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Dapolsertib
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
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014096388&_cid=P12-MG5YKY-59978-1
3.9. Compounds of Example 26:
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
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.
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
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
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)
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
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
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
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
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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!
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
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
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
PAT
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
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 V1B 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 254 plate, 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). |
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
Atumelnant
Atumelnant
CAS 2392970-97-5
MF C33H42F3N5O3 MW 613.7 g/mol
CRN04894, NR57FH6U1N
CRINETICS PHARMA, Orphan Drug Status, Congenital adrenal hyperplasia
N-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-(2-ethoxyphenyl)-3-[(2R)-2-ethyl-4-[1-(trifluoromethyl)cyclobutanecarbonyl]piperazin-1-yl]pyridine-2-carboxamide
N-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-(2-ethoxyphenyl)-3-{(2R)-2-ethyl-4-[1-(trifluoromethyl) cyclobutane-1-carbonyl]piperazin-1-yl}pyridine-2-carboxamide
Adrenocorticotropic hormone receptor antagonist
- OriginatorCrinetics Pharmaceuticals
- ClassAmides; Antineoplastics; Antisecretories; Benzene derivatives; Cyclobutanes; Ethers; Fluorocarbons; Ketones; Piperazines; Pyridines; Quinuclidines; Small molecules
- Mechanism of ActionMelanocortin type 2 receptor antagonists
- Orphan Drug StatusYes – Congenital adrenal hyperplasia
- Phase IICongenital adrenal hyperplasia; Cushing syndrome
- No development reportedEctopic ACTH syndrome
- 21 Aug 2025Atumelnant receives Orphan Drug status for Congenital adrenal hyperplasia in the US
- 07 Aug 2025Crinetics pharmaceuticals plans phase II/III clinical trial for Cushing’s disease in 1H 2026
- 08 May 2025Crinetics Pharmaceuticals plans the phase III CALM-CAH trial for Congenital adrenal hyperplasia (In adults) (PO), in the second half of 2025
Atumelnant (INNTooltip International Nonproprietary Name; developmental code name CRN04894) is an investigational new drug developed by Crinetics Pharmaceuticals for the treatment of adrenocorticotropic hormone (ACTH)-dependent endocrine disorders.[1] It is a selective antagonist of the melanocortin type 2 receptor (MC2R), also known as the ACTH receptor, which is primarily expressed in the adrenal glands.[1][2] The drug is orally active.[1] Atumelnant is being evaluated to treat conditions such as congenital adrenal hyperplasia (CAH) and ACTH-dependent Cushing’s syndrome caused for example by pituitary adenomas.[3]
Atumelnant is an orally bioavailable nonpeptide antagonist of the adrenocorticotropic hormone (ACTH) receptor (ACTHR; melanocortin receptor 2; MC2R), with potential steroid hormone production inhibitory activity. Upon oral administration, atumelnant competes with ACTH for receptor binding to MC2R in the adrenal cortex and inhibits ACTH signaling. This may inhibit the synthesis and secretion of steroid hormones. MC2R, a member of the melanocortin receptor subfamily of type 1 G protein-coupled receptors, plays a key role in adrenal steroidogenesis.
PAPER
Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist
Publication Name: ACS Medicinal Chemistry Letters
Publication Date: 2024-03-19, PMCID: PMC11017392, PMID: 38628803
DOI: 10.1021/acsmedchemlett.3c00514
PATENTS
- Melanocortin subtype-2 receptor antagonists and uses thereofPublication Number: IL-279152-B2Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: US-2024300920-A1Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor antagonists and uses thereofPublication Number: IL-279152-B1Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: JP-2024009837-APriority Date: 2018-06-05
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: KR-102695210-B1Priority Date: 2018-06-05Grant Date: 2024-08-13
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: US-2024109866-A1Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: CN-112533904-BPriority Date: 2018-06-05Grant Date: 2024-10-29
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: US-10981894-B2Priority Date: 2018-06-05Grant Date: 2021-04-20
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: US-2021002254-A1Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: US-2021238164-A1Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: US-11566015-B2Priority Date: 2018-06-05Grant Date: 2023-01-31
- Melanocortin subtype-2 receptor (MC2R) antagonists and their usesPublication Number: JP-7359783-B2Priority Date: 2018-06-05Grant Date: 2023-10-11
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: US-2020216415-A1Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: US-10766877-B2Priority Date: 2018-06-05Grant Date: 2020-09-08
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: CN-112533904-APriority Date: 2018-06-05
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: EP-3802500-A1Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: KR-20210005995-APriority Date: 2018-06-05
- Melanocortin subtype-2 receptor (MC2R) antagonists for the treatment of diseasePublication Number: CN-117043146-APriority Date: 2021-03-19
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: US-10562884-B2Priority Date: 2018-06-05Grant Date: 2020-02-18
- Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereofPublication Number: US-10604507-B2Priority Date: 2018-06-05Grant Date: 2020-03-31
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: US-2019367481-A1Priority Date: 2018-06-05
- Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereofPublication Number: US-2020010452-A1Priority Date: 2018-06-05
Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of diseasePublication Number: US-2022313691-A1Priority Date: 2021-03-19 - Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of diseasePublication Number: WO-2022197798-A1Priority Date: 2021-03-19
- Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of diseasePublication Number: TW-202302108-APriority Date: 2021-03-19
- Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of diseasePublication Number: AU-2022240609-A1Priority Date: 2021-03-19
- Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of diseasePublication Number: EP-4308553-A1Priority Date: 2021-03-19
- Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of acth-dependent cushing’s syndromePublication Number: WO-2024211343-A1Priority Date: 2023-04-05
- Crystalline melanocortin subtype-2 receptor (mc2r) antagonistPublication Number: TW-202430167-APriority Date: 2022-12-16
- Crystalline melanocortin subtype-2 receptor (mc2r) antagonistPublication Number: US-2024208963-A1Priority Date: 2022-12-16
- Crystalline melanocortin subtype-2 receptor (mc2r) antagonistPublication Number: WO-2024130091-A1Priority Date: 2022-12-16
- Treatment of congenital adrenal hyperplasia and polycystic ovary syndromePublication Number: WO-2023163945-A1Priority Date: 2022-02-2
SYN
PATENT
https://patentscope.wipo.int/search/en/detail.jsf?docId=US278278493&_cid=P22-MFXDN2-76849-1
Example 31: N-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-(2-ethoxyphenyl)-3-[(2R)-2-ethyl-4-[1-(trifluoromethyl)cyclobutanecarbonyl]piperazin-1-yl]pyridine-2-carboxamide (Compound 1-410)
Step 31-1, Preparation of 6-(2-ethoxyphenyl)-3-[(2R)-2-ethyl-4-[1-(trifluoromethyl)cyclobutanecarbonyl]piperazin-1-yl]pyridine-2-carboxylic acid
Step 31-2, Preparation of N-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-(2-ethoxyphenyl)-3-[(2R)-2-ethyl-4-[1-(trifluoromethyl)cyclobutanecarbonyl]piperazin-1-yl]pyridine-2-carboxamide
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References
- “Crinetics Pharmaceuticals”. AdisInsight. 21 January 2025. Retrieved 25 February 2025.
- “Atumelnant (CRN04894)”. crinetics.com. 14 August 2020.
- Varlamov EV, Gheorghiu ML, Fleseriu M (December 2024). “Pharmacological management of pituitary adenomas – what is new on the horizon?”. Expert Opinion on Pharmacotherapy. 26 (2): 119–125. doi:10.1080/14656566.2024.2446625. PMID 39718553.
| Clinical data | |
|---|---|
| Other names | CRN04894 |
| Routes of administration | Oral[1] |
| Drug class | Melanocortin MC2 receptor antagonist[1] |
| Identifiers | |
| IUPAC name | |
| CAS Number | 2392970-97-5 |
| PubChem CID | 146361282 |
| IUPHAR/BPS | 13339 |
| ChemSpider | 129750231 |
| UNII | NR57FH6U1N |
| KEGG | D13102 |
| Chemical and physical data | |
| Formula | C33H42F3N5O3 |
| Molar mass | 613.726 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
////////Atumelnant, CRN04894, CRN 04894, NR57FH6U1N, CRINETICS PHARMA, Orphan Drug Status, Congenital adrenal hyperplasia, PHASE 3
New Drug Approvals 
