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Prifetrastat
Prifetrastat
CAS 2569008-99-5
MFC19H18N4O5S MW414.4 g/mol
N-(6-((1H-Pyrazol-1-yl)methyl)-4-methoxybenzo[d]isoxazol-3-yl)-2-methoxybenzenesulfonamide
2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide
antineoplastic, PF-07248144, PF 07248144, Solid tumours, CANCER, KAT6-IN-1, GN6DU4ZE30
Prifetrastat is an inhibitor of MYST histone acetyltransferase (HAT) KAT6, with potential antineoplastic activity. Upon administration, prifetrastat targets and binds to KAT6, and inhibits the acetylation of histones and other nonhistone substrates. This may disrupt gene expression and inhibit the proliferation of tumors that overexpress KAT6. KAT6A (MOZ; MYST3) and KAT6B (MORF; MOZ2; MYST4), commonly amplified genes in solid tumors, play key roles in cell cycle regulation and in tumorigenesis.
Prifetrastat (also known as PF-07248144) is an investigational, first-in-class small molecule drug that acts as a selective inhibitor of the epigenetic modifiers KAT6A and KAT6B. It is primarily studied as an antineoplastic agent for hormone receptor-positive (ER+/HER2–) advanced or metastatic breast cancer.
Mechanism of Action
- Inhibits KAT6A and KAT6B histone acetyltransferases to block abnormal tumor cell growth.
- Suppresses lineage-specific gene expression tied to estrogen receptor signaling and drug resistance.
- Induces cell cycle arrest and tumor senescence.
Clinical Development
- Evaluated in clinical trials (such as phase 1/2 and phase 3 evaluations) for patients whose breast cancer progressed after prior endocrine therapy and CDK4/6 inhibitors.
- Commonly tested in combination regimens alongside anti-estrogen therapies like fulvestrant
Prifetrastat (also known as PF-07248144) is an investigational, first-in-class small molecule drug that acts as a selective inhibitor of the epigenetic modifiers KAT6A and KAT6B. It is primarily studied as an antineoplastic agent for hormone receptor-positive (ER+/HER2–) advanced or metastatic breast cancer.
Mechanism of Action
- Inhibits KAT6A and KAT6B histone acetyltransferases to block abnormal tumor cell growth.
- Suppresses lineage-specific gene expression tied to estrogen receptor signaling and drug resistance.
- Induces cell cycle arrest and tumor senescence.
Clinical Development
- Evaluated in clinical trials (such as phase 1/2 and phase 3 evaluations) for patients whose breast cancer progressed after prior endocrine therapy and CDK4/6 inhibitors.
- Commonly tested in combination regimens alongside anti-estrogen therapies like fulvestrant
- Phase IIIHER2 negative breast cancer
- Phase IISolid tumours
- No development reportedBreast cancer
- 07 Aug 2026Prifetrastat is still in phase II development in Solid-tumours (Combination therapy, Late-stage disease, Metastatic disease, Second-line therapy or greater) in USA, Australia, Japan, China, South Korea (PO, Tablet) (NCT04606446)
- 07 Aug 2026Prifetrastat is still in phase II development in Solid-tumours (Monotherapy, Late-stage disease, Metastatic disease, Second-line therapy or greater) in USA, Australia, Japan, China, South Korea (PO, Tablet) (NCT04606446)
- 28 Jul 2026No recent reports of development identified for phase-I development in Breast-cancer(Metastatic disease) in USA (PO)
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020254946&_cid=P12-MSO1IP-41527-1
Example 45: Preparation of 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide according to Scheme C (Route A).
To a suspension of 4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-amine (A-2) (2.5 g, 10 mmol) in pyridine (8.0 mL) was added 2-methoxybenzene-1-sulfonyl chloride (3.17 g, 15.4 mmol). The reaction was stirred at 120 °C for 1.5 h. The mixture was cooled to room temperature and diluted with MeOH. The resulting suspension was filtered. and the filter cake was washed with MeOH (30 mL). The solids were dissolved in DCM (50 mL) and MeOH (30 mL) was added. The DCM was removed under vacuum
and the precipitate was collected by filtration. The filter cake was dried by lyophilization to provide 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide (Example 45) (2.5 g, 59% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) d 10.18 (s, 1H), 7.87 (d, J= 2.0 Hz, 1H), 7.80 (dd, J=1.6, 7.9 Hz, 1H), 7.66– 7.59 (m, 1H), 7.49 (d, J=1.5 Hz, 1H), 7.19 (d, J=8.3 Hz, 1H), 7.09 (t, J=7.7 Hz, 1H), 6.83 (s, 1H), 6.74 (s, 1H), 6.30 (t, J=2.0 Hz, 1H), 5.44 (s, 2H), 3.82 (s, 3H), 3.78 (s, 3H); m/z (ESI+) 415.0 (M+H) + .
Example 45: Alternative preparation of 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide according to Scheme D.
A 100 mL reactor equipped with an overhead stirrer was charged with 4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzoxazol-3-amine (A-2) (10.00 g, 40.94 mmol), 2-methoxybenzenesulfonyl chloride (10.15 g, 49.13 mmol), and acetonitrile (100 mL). The resulting suspension was stirred at 25 °C for 55 minutes. Via pipette, dimethylsulfoxide (0.36 mL, 4.09 mmol) was added in one portion. Via syringe, 3,5-lutidine (14.8 mL, 122.82 mmol) was added dropwise over 15 minutes. The resulting light-yellow suspension was stirred at 25 °C for 18 hours to reach >98% conversion as judged by LCMS. The reaction mixture was acidified with 1 M aq. HCl (100 mL), then
concentrated to ~80 mL (rotary evaporator, 40 °C, 85 mbar). The slurry was treated with additional 1 M aq. HCl (40 mL) to rinse down the walls of the vessel, then stirred at 20 °C for 2.5 hours. The resulting precipitate was collected by suction filtration. The filter cake was washed with water (2 x 50 mL), then dried under vacuum at 35 °C for 48 hours, affording crude 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide (Example 45) (15.2 g, 90% yield, 98% purity by LCMS) as a solid. m/z 415.1 (M+H) + .
To purify the crude product, a suspension of crude 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide (Example 45) (14.00 g, 33.78 mmol) in dichloromethane (210 mL) was heated in a 40 °C bath until a clear solution was obtained (10 minutes). The mixture was filtered, and the filtrate returned to a clean reaction vessel, using additional dichloromethane (70 mL) to quantitate the transfer. Ethyl acetate (140 mL) was added to the solution over 2 minutes, then the mixture stirred for 2.5 hours. No crystallization was observed, so the solution was concentrated under reduced pressure (200 mbar) to remove dichloromethane (volume was reduced by about 70 mL). More ethyl acetate (140 mL) was added to the residue, and the mixture stirred at room temperature for 21 hours. The resulting suspension was concentrated under reduced pressure (40 °C, 200 mbar) to about 280 mL, then stirred at room temperature for 3 hours. The solids were collected by filtration, with additional ethyl acetate (70 mL) used to rinse the reaction vessel and filter cake. The filter cake was dried in a vacuum oven at 35 °C for 23 hours, affording 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide (Example 45) (12.0 g, 85% yield, 97.9% purity by UPLC, no single impurity larger than 0.5%) as a solid. m/z 415.1 (M+H) + .
To purify further, a suspension of 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide (Example 45) (2.0 g, 4.73 mmol) in acetone (80 mL) was heated to reflux (bath temperature 55 °C) with stirring for 2 hours. While the mixture was still heated, ethyl acetate (30 mL) was added slowly, so that the internal temperature remained above 45 °C. The resulting slurry was concentrated to about 30 mL under mild vacuum (bath temp 65 °C), then cooled slowly at a rate of 1 °C/min to 20 °C (~31 minutes). The resulting precipitate was collected by suction filtration. The filter cake dried under vacuum at 50 °C for 22 hours, yielding 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamide (Example 45) (1.825 g, 93% yield, 99.5% purity by UPLC) as a crystalline solid. 1 hour
NMR (400 MHz, CHLOROFORM-d) d 8.14 (dd, J=1.7, 7.8 Hz, 1H), 8.04 (s, 1H), 7.59 -7.51 (m, 2H), 7.44 (d, J=2.2 Hz, 1H), 7.14 – 7.06 (m, 1H), 6.95 (d, J=8.3 Hz, 1H), 6.78 (d, J=0.6 Hz, 1H), 6.45 (s, 1H), 6.32 (t, J=2.1 Hz, 1H), 5.38 (s, 2H), 3.97 (s, 3H), 3.91 (s, 3H).
PAT
PAT
Scheme 1
Step 2
In an inerted reactor were added 6-((1 H-pyrazol-1-yl)methyl)-4-methoxybenzo[d]isoxazol-3-amine (lnt-4, 27.5 Kg, 112.6 mol, 1 equiv.), 2-methoxybenzenesulfonyl chloride (lnt-5, 33.9 Kg, 168.9 mol, 1.5 equiv.) and THF (248 L, 9-L/Kg). A solution of sodium te/Y-butoxide in THF (2 M, 197 L, 394.1 mol, 3.5 eq.) was added to the stirred mixture at 20 °C over 4 h. At the end of the addition the line was rinsed with THF (27.5 L, 1 L/Kg) and the mixture stirred for a further 1 h. Following reaction completion water (413 L, 15 L/Kg) was added at once followed by slow addition of aq. HCI (2 M, 197 L, 394.1 mol, 3.5 equiv.). The mixture was left stirring overnight, then the slurry was filtered, washed twice with CH3OH (82.5 L, 3 L/Kg) and dried to afford the title compound as a white solid (42.32 Kg, 90.6% yield).
1H NMR (400 MHz, DMSO) 5 10.09 (s, 1 H), 7.87 (dd, J = 2.3, 0.7 Hz, 1 H), 7.81 (dd, J = 7.8, 1.7 Hz, 1 H), 7.63 (ddd, J = 8.4, 7.4, 1.7 Hz, 1 H), 7.50 (dd, J = 1.8, 0.7 Hz, 1 H), 7.10 (td, J = 7.6, 1 .0 Hz, 1 H), 6.84 (d, J = 1 .0 Hz, 1 H), 6.30 (t, J = 2.1 Hz, 1 H), 5.44 (s, 2H), 3.83 (s, 3H), 3.79 (s, 3H). 13C NMR (101 MHz, DMSO) 5 164.82, 156.92, 154.39, 151.76, 144.13, 139.80, 135.73, 131.03, 130.43, 127.66, 120.52, 113.34, 106.25, 106.17, 104.42, 101.33, 56.51, 56.42, 55.01. HRMS: Ci9Hi8N4O5S+ [M+1 ]+ calculated:
415.1072; measured: 415.1071.
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References
- Benzisoxazole sulfonamide derivativesPublication Number:HR-P20231501-T1Priority Date:2019-06-18
- Benzisoxazole sulfonamide derivativesPublication Number:US-12371425-B2Priority Date:2019-06-18Grant Date:2025-07-29
- Benzisoxazole sulfonamide derivativesPublication Number:EP-3986890-B9Priority Date:2019-06-18Grant Date:2025-04-16
- Benzisoxazole sulfonamide derivativesPublication Number:EP-4299135-B1Priority Date:2019-06-18Grant Date:2025-08-06
- Benzisoxazole sulfonamide derivativesPublication Number:AU-2020296361-A1Priority Date:2019-06-18
- Benzisoxazole sulfonamide derivativesPublication Number:EP-4299135-A2Priority Date:2019-06-18
- Benzisoxazole sulfonamide derivativesPublication Number:TW-202115048-APriority Date:2019-06-18
- Benzisoxazole sulfonamide derivativesPublication Number:CN-114364672-BPriority Date:2019-06-18Grant Date:2024-09-06
- Benzisoxazole sulfonamide derivativesPublication Number:EP-3986890-A1Priority Date:2019-06-18
- Benzisoxazole sulfonamide derivativesPublication Number:US-11492346-B2Priority Date:2019-06-18Grant Date:2022-11-08
- Benzisoxazole sulfonamide derivativesPublication Number:CA-3143666-A1Priority Date:2019-06-18
- Benzisoxazole sulfonamide derivativesPublication Number:CN-114364672-APriority Date:2019-06-18
- Benzisoxazole sulfonamide derivativesPublication Number:EP-3986890-B1Priority Date:2019-06-18Grant Date:2023-11-15
- Benzisoxazole sulfonamide derivativesPublication Number:WO-2020254946-A1Priority Date:2019-06-18
- Kat6 inhibitor and combinations for breast cancer treatmentPublication Number:EP-4181920-B1Priority Date:2020-07-15Grant Date:2025-09-10
- Benzisoxazole sulfonamide derivativesPublication Number:KR-20220024671-APriority Date:2019-06-18
- Benzisoxazole Sulfonamide DerivativesPublication Number:US-2023174522-A1Priority Date:2019-06-18
- Benzisoxazole Sulfonamide DerivativesPublication Number:US-2020399258-A1Priority Date:2019-06-18
- Benzisoxazole sulfonamide derivativesPublication Number:CA-3143666-CPriority Date:2019-06-18Grant Date:2024-06-11
- Dosing regimens comprising a kat6 inhibitor for the treatment of cancerPublication Number:WO-2024023703-A1Priority Date:2022-07-29
- Dosing regimens comprising a kat6 inhibitor for the treatment of cancerPublication Number:EP-4561571-A1Priority Date:2022-07-29
- Kat6 inhibitor methods and combinations for cancer treatmentPublication Number:EP-4181920-A1Priority Date:2020-07-15
- Kat6 inhibitor methods and combinations for cancer treatmentPublication Number:WO-2022013369-A1Priority Date:2020-07-15
- KAT6 inhibitor methods and combinations for cancer treatmentPublication Number:CN-116113407-APriority Date:2020-07-15
- Crystalline form of 2-methoxy-n-{4-methoxy-6-[(1h-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulfonamidePublication Number:WO-2025141469-A1Priority Date:2023-12-26
- Sulfonamide compound and use thereofPublication Number:WO-2025098417-A1Priority Date:2023-11-08
- MYST InhibitorsPublication Number:US-2025122182-A1Priority Date:2023-09-27
- Dosing regimens comprising a kat6 inhibitor for the treatment of cancerPublication Number:TW-202415373-APriority Date:2022-07-29
- Dosing regimen comprising KAT6 inhibitors for treating cancerPublication Number:CN-119604288-APriority Date:2022-07-29
///////////prifetrastat, anax labs, antineoplastic, PF-07248144, PF 07248144, Solid tumours, CANCER, KAT6-IN-1, GN6DU4ZE30
#prifetrastat, #anax labs, #antineoplastic, #PF-07248144, #PF 07248144, #Solid tumours, #CANCER, #KAT6-IN-1, #GN6DU4ZE30
Plodicitinib
Plodicitinib
CAS 2360992-48-7
MF C19H22FN7O2 MW399.42
1-[(3S,4R)-3-[[2-[(1-ethylpyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]-4-fluoropiperidin-1-yl]prop-2-en-1-one
1-[(3S,4R)-3-({2-[(1-ethyl-1H-pyrazol-4-yl)amino]-7Hpyrrolo[2,3-d]pyrimidin-4-yl}oxy)-4-fluoropiperidin-1-yl]prop2-en-1-one
Janus tyrosine kinase 3/TEC family kinase inhibitor, antiinflammatory, veterinary, SX5UEP3JXA
Plodicitinib is a Janus tyrosine kinase 3/TEC family kinase inhibitor with anti-inflammatory activity.
Plodicitinib is a small-molecule, dual Janus tyrosine kinase 3 (JAK3) and TEC family kinase (specifically BTK) inhibitor that exhibits strong anti-inflammatory properties.
Mechanism of Action
The compound blocks specific enzymatic pathways involved in cellular signaling:
- JAK3 Inhibition: It targets Janus kinase 3, which plays an essential role in transmitting signals for cytokines that regulate immune cell development and activation.
- TEC/BTK Inhibition: It blocks Bruton’s tyrosine kinase (BTK), a component vital for B-cell development and activation. [1, 2]
- Combined Effect: By blocking these pathways, it suppresses the overactive immune and inflammatory responses that drive autoimmune and allergic conditions.
Applications and Development Status
- Veterinary Medicine: In early 2026, Daewoong Pharmaceutical submitted an application to the Animal and Plant Quarantine Agency in South Korea for commercial approval of plodicitinib. It is being positioned as a specialized, companion animal-only treatment to manage atopic dermatitis in dogs.
- Research Use: In the scientific community, it is actively utilized as a laboratory tool compound to study kinase signaling pathways and inflammatory disease models.
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=US306969271&_cid=P22-MSL6QJ-67927-1
Example 4: Preparation of 1-(cis-3-((2-((1-ethyl-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one
19.3 mg (yield: 27.8%) of the title compound was obtained in the same manner as in Example 1, except that cis-tert-butyl-4-fluoro-3-hydroxypiperidine-1-carboxylate was used instead of trans-tert-butyl-4-fluoro-3-hydroxypiperidine-1-carboxylate in Example 1.
Example 5: Preparation of 1-((3S,4R)-3-((2-((1-ethyl-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one
| 16.2 mg (yield: 57.4%) of the title compound was obtained in the same manner as in Example 1, except that tert-butyl(3S,4R)-4-fluoro-3-hydroxypiperidine-1-carboxylate was used instead of trans-tert-butyl-4-fluoro-3-hydroxypiperidine-1-carboxylate in Example 1. |
Example 25: Preparation of 1-((3S,4S)-3-((2-((1-ethyl-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one
The compound of Example 1 was separated by CHIRALCEL OZ-H column to obtain the title compound with an analysis time of 10.1 minutes.
1H NMR (500 MHz, CD 3OD) δ 7.98-7.95 (m, 1H), 7.57-7.55 (m, 1H), 6.84-6.53 (m, 2H), 6.26-6.08 (m, 2H), 5.78-5.52 (m, 1H), 5.41-5.40 (m, 1H), 5.10-5.04 (m, 1H), 4.50-4.06 (m, 4H), 3.89-3.86 (m, 1H), 3.55-3.50 (m, 1H), 2.19-2.16 (m, 1H), 1.95-1.94 (m, 1H), 1.45-1.41 (m, 3H)
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025121903&_cid=P22-MSL6W2-73218-1
1-((3S,4R)-3-((2-((1-ethyl-1H-pyrazole-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one is represented by the following chemical formula 1:
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WEBSITE https://www.anaxlab.com/
Discovery Solutions, Supporting the chemistry needs of clients in the Medical, Analytical and Bio Sciences
Development Solutions, Developing from Lab scale to PR&D, Kilo Scale-ups and Commercial Scales
SEE MORE………Integrated Solutions, Manufacturing Solutions, Products,
Can’t Find? Let’s Connect
Phone : +91 897704 2010 / +91 9177075735, Email : info@anaxlab.com
#MedicinalChemistry, #DrugDiscovery, #OrganicSynthesis, #ChemicalLibrary, #BuildingBlocks, #SARStudies, #ChemistryInnovation, #medchem, #Drugdevelopment, #Biotech, #Biotechnology, #AnaxLaboratories, #Pharma
AS ON FEB2026 4.574 LAKHS VIEWS ON BLOG WORLDREACH AVAILABLEFOR YOUR ADVERTISEMENT
join me on Linkedin
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join me on Researchgate
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join me on Facebook
Anthony Melvin Crasto Dr. | Facebook
join me on twitter
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+919321316780 call whatsaapp
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References
- Tartrate salt of 1-((3s,4r)-3-((2-((1-ethyl-1h-pyrazol-4-yl)amino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one, crystalline form thereof, and method for preparing samePublication Number:WO-2025121903-A1Priority Date:2023-12-05
- Method for preparation of 1-((3s,4r)-3-((2-((1-ethyl-1h-pyrazol-4-yl)amino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one, and intermediate compounds thereofPublication Number:WO-2025121899-A1Priority Date:2023-12-05
- Phosphate salt of 1-((3s,4r)-3-((2-((1-ethyl-1h-pyrazol-4-yl)amino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one, crystalline form thereof, and method for preparation thereofPublication Number:WO-2025121900-A1Priority Date:2023-12-05
- Oxy-fluoropiperidine derivative as kinase inhibitorPublication Number:EP-3733673-A1Priority Date:2017-12-28
- Oxy-fluoropiperidine Derivative as Kinase InhibitorPublication Number:US-2020308177-A1Priority Date:2017-12-28
- Oxy-fluoropiperidine compounds as kinase inhibitors, pharmaceutical composition comprising the same and their use in the prevention or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases or hyperproliferative diseases and immune-mediated diseases, cancers, tumorsPublication Number:BR-112020013141-B1Priority Date:2017-12-28
- Substituted piperidines as kinase inhibitorsPublication Number:US-11339167-B2Priority Date:2017-12-28Grant Date:2022-05-24
- Oxy-haloperidine derivatives as kinase inhibitorsPublication Number:CN-111527091-APriority Date:2017-12-28
- Oxy-fluoropiperidine derivatives as kinase inhibitorPublication Number:KR-102318929-B1Priority Date:2017-12-28Grant Date:2021-10-28
- Oxy-fluoropiperidine derivative as a kinase inhibitorPublication Number:JP-6995428-B2Priority Date:2017-12-28Grant Date:2022-01-14
- Oxy-fluoropiperidine derivatives as kinase inhibitorPublication Number:CA-3084962-A1Priority Date:2017-12-28
- Oxy-fluoropiperidine derivative as a kinase inhibitorPublication Number:ES-2922633-T3Priority Date:2017-12-28Grant Date:2022-09-19
- Oxy-fluoropiperidine derivatives as kinase inhibitorPublication Number:KR-20190080803-APriority Date:2017-12-28
- Oxy-fluoropiperidine derivatives as kinase inhibitorPublication Number:CA-3084962-CPriority Date:2017-12-28Grant Date:2022-08-09
- Oxy-fluoropiperidine derivative as kinase inhibitorPublication Number:EP-3733673-B1Priority Date:2017-12-28Grant Date:2022-06-29
- Oxy-haloperidine derivatives as kinase inhibitorsPublication Number:CN-111527091-BPriority Date:2017-12-28Grant Date:2023-03-28
- Oxy-fluoropiperidine derivatives as kinase inhibitorPublication Number:KR-20210062618-APriority Date:2017-12-28
- Oxy-fluoropiperidine derivatives as kinase inhibitorPublication Number:KR-102592083-B1Priority Date:2017-12-28Grant Date:2023-10-20
- OXY-FLUOROPIPERIDINE DERIVATIVE AS A KINASE INHIBITORPublication Number:HR-P20221043-T1Priority Date:2017-12-28
- Oxy-fluoropiperidine derivative as kinase inhibitorPublication Number:IL-275207-BPriority Date:2017-12-28
/////////anax labs, plodicitinib, Janus tyrosine kinase 3/TEC family kinase inhibitor, antiinflammatory, veterinary, SX5UEP3JXA
#anax labs, #plodicitinib, #Janus tyrosine kinase 3/TEC family kinase inhibitor, #antiinflammatory, #veterinary, #SX5UEP3JXA
Peturadol
Peturadol
CAS 686301-48-4
MFC12H20N6O MW264.33 g/mol
5-{[2-(6-amino-9H-purin-9-yl)ethyl]amino}pentan-1-ol
central analgesic, NB001, NB 001, HTS 09836, J89QT81NBQ
NB-001 has been investigated for the treatment of Recurrent Herpes Labialis.
NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity
Peturadol (also known by its developmental code NB001) is a potent, selective, and orally active adenylyl cyclase 1 (AC1) inhibitor. It is primarily recognized as a specialized chemical compound used in advanced medical and pharmacological laboratory research.
Because drug names can sometimes look or sound very similar, please check the spelling carefully. If you are looking for a medication prescribed to you by a doctor, it is highly likely you mean Patradol (a combination painkiller containing tramadol and paracetamol) or Pentadol / Tapentadol (an opioid analgesic).
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01324466 | NanoBio Corporation | Recurrent Herpes Labialis | 2011-04 | PHASE3 |
| NCT05290493 | Nobias Therapeutics, Inc. | 22q11 Deletion Syndrome | 2022-02-10 | PHASE2 |
| NCT01695187 | NanoBio Corporation | Herpes Labialis | 2012-10 | PHASE3 |
| NCT01321359 | NanoBio Corporation | Recurrent Herpes Simplex Labialis | 2011-04 | PHASE3 |
| NCT00453401 | NanoBio Corporation | Herpes Labialis | 2007-02 | PHASE2 |
- NB-001 in Children and Adolescents With 22q11 Deletion SyndromeCTID:NCT05290493Phase:Phase 2Status:CompletedDate:2025-02-10
- NB-001 Treatment of Recurrent Herpes LabialisCTID:NCT01695187Phase:Phase 3Status:Unknown statusDate:2013-06-14
- A Multicenter Study of NB-001 in the Treatment of Recurrent Herpes Labialis (SHaRCS)CTID:NCT01324466Phase:Phase 3Status:CompletedDate:2013-05-23
- Safety, Pharmacokinetics, and Efficacy Study of NB-001 to Treat Recurrent Herpes LabialisCTID:NCT00453401Phase:Phase 2Status:CompletedDate:2008-05-30
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2007041863&_cid=P22-MSFGZW-54602-1
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=US210409779&_cid=P22-MSFGZW-54602-1
Synthesis and Purification of Intermediate 2
(2) Synthesis and Purification of NB001
PAT
- Method for treating neuronal and non-neuronal painPublication Number:CA-2625553-CPriority Date:2005-10-14Grant Date:2014-03-11
- Method for treating neuronal and non-neuronal painPublication Number:WO-2007041863-A1Priority Date:2005-10-14
- Methods for treating herpes virus infectionsPublication Number:CA-2721510-A1Priority Date:2008-04-18
- Method for treating neuronal and non-neuronal painPublication Number:EP-1948182-B1Priority Date:2005-10-14Grant Date:2012-12-12
- Method for Treating Neuronal and Non-Neuronal PainPublication Number:US-2009233922-A1Priority Date:2005-10-14
- Method for treating neuronal and non-neuronal painPublication Number:CA-2625553-A1Priority Date:2005-10-14
- Methods for treating neural and non-neuralgiaPublication Number:JP-5404045-B2Priority Date:2005-10-14Grant Date:2014-01-29
- Neuronal stem cell differentiationPublication Number:WO-2015055987-A1Priority Date:2013-10-14
- Phosphodiesterase Inhibitor TreatmentPublication Number:US-2024108627-A1Priority Date:2013-03-15
- Phosphodiesterase Inhibitor TreatmentPublication Number:US-2022226332-A1Priority Date:2013-03-15
- Process for preparing an enantiomerically enriched, deuterated secondary alcohol from a corresponding ketone without reducing deuterium incorporationPublication Number:US-9074233-B2Priority Date:2010-09-01Grant Date:2015-07-07
- Methods for treating herpes virus infectionsPublication Number:US-2010075914-A1Priority Date:2008-04-18
- Anti-hsv pre-exposure prophylaxisPublication Number:EP-3166680-B1Priority Date:2014-07-07Grant Date:2023-11-15
- Viral prophylaxis treatment methods and pre-exposure prophylaxis kitsPublication Number:EP-4342545-A2Priority Date:2014-07-07
- Neuronal stem cell differentiationPublication Number:EP-3058064-A1Priority Date:2013-10-14
- neuronal stem cell differentiationPublication Number:CN-105658787-APriority Date:2013-10-14
- Neuronal stem cell differentiationPublication Number:US-2016257930-A1Priority Date:2013-10-14
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References
[1]. Min Zhuo. Method for treating neuronal and non-neuronal pain. US8124599B2.
[2]. Wang H, et al., Identification of an adenylyl cyclase inhibitor for treating neuropathic and inflammatory pain. Sci Transl Med. 2011 Jan 12;3(65):65ra3. [Content Brief]
[3]. Zhou Z, et al., Inhibition of calcium-stimulated adenylyl cyclase subtype 1 (AC1) for the treatment of pain and anxiety symptoms in Parkinson’s disease mice model. Mol Pain. 2024 Jan-Dec;20:17448069241266683. [Content Brief]
////////////peturadol, anax labs, central analgesic, NB001, NB 001, HTS 09836, J89QT81NBQ
#peturadol, #anax labs, #central analgesic, #NB001, #NB 001, #HTS 09836, #J89QT81NBQ
Petadeferitrin
Petadeferitrin
CAS911714-45-9
MFC16H21NO6S MW355.4 g/mol
(4S)-2-[2-hydroxy-4-[2-(2-methoxyethoxy)ethoxy]phenyl]-4-methyl-5H-1,3-thiazole-4-carboxylic acid
- (4S)-4,5-Dihydro-2-(2-hydroxy-4-(2-(2-methoxyethoxy)ethoxy)phenyl)-4-methyl-4-thiazolecarboxylic acid
- 4-Thiazolecarboxylic acid, 4,5-dihydro-2-(2-hydroxy-4-(2-(2-methoxyethoxy)ethoxy)phenyl)-4-methyl-, (4S)-
- (4S)-4,5-dihydro-2-[2-hydroxy-4-[2-(2-methoxyethoxy)ethoxy]phenyl]-4-methyl-4-thiazolecarboxylic acid
(4S)-2-{2-hydroxy-4-[2-(2-methoxyethoxy)ethoxy]phenyl}-4-methyl4,5-dihydro-1,3-thiazole-4-carboxylic acid
iron chelating agent, SP 420, WBX54NZ436
Petadeferitrin is an orally bioavailable iron-chelating agent and derivative of desferrithiocin, with iron chelating and protective activities in diseases of iron overload. Upon oral administration, petadeferitrin targets, binds to and chelates free iron. This induces the excretion of iron, prevents iron accumulation and prevents cellular and/or tissue damage associated with iron overload.
Petadeferitrin (formerly known as SP-420) is an investigational, orally bioavailable, small-molecule iron chelator being developed by Pharmacosmos (and its subsidiary Abfero Pharmaceuticals) to treat patients with transfusion-dependent iron overload. The drug works by binding to excess free iron in the body and forming complexes that are primarily excreted through bile and feces.
Key Characteristics & Mechanisms
- Drug Class: It is a tridentate iron chelator and a derivative of desferrithiocin.
- Enhanced Efficiency: In preclinical studies, it demonstrated a higher iron clearance efficiency (ICE value of 26.7) compared to desferrithiocin.
- Brain-Penetrant: It is uniquely characterized as a brain-penetrant agent, which could expand its potential protective use in specific diseases associated with iron accumulation.
Clinical Development Status
- Investigational Status: The drug remains investigational and has not yet been approved for commercial use anywhere in the world.
- Target Diseases: Clinical evaluation focuses on individuals who suffer from iron overload due to frequent blood transfusions, such as patients with β-thalassemia and sickle cell disease.
- Ongoing Studies: Pharmacosmos is actively evaluating the drug in Phase II clinical trials (such as ClinicalTrials.gov ID NCT05693909) to assess its safety, tolerability, and dosing advantages over existing options. Early human data suggests it may offer effective clearance with less frequent dosing compared to some currently approved alternatives.
- A Trial Testing SP-420 in Subjects With Transfusion-dependent β-thalassemia or Low-risk Myelodysplastic SyndromesCTID:NCT05693909Phase:Phase 2Status:RecruitingDate:2025-09-24
- Safety of SP-420 in the Treatment of Transfusional Iron OverloadCTID:NCT04741542Phase:Phase 1Status:TerminatedDate:2024-12-27
- SP-420 in Subjects With Transfusion-dependent Beta-Thalassemia or Other Rare AnemiasCTID:NCT03801889Phase:Phase 2Status:WithdrawnDate:2020-10-05
- Safety and Pharmacokinetic Study of Escalating Doses of SP-420, an Iron Chelator, in Patients With β-ThalassemiaCTID:NCT02274233Phase:Phase 1Status:TerminatedDate:2015-09-29
An open-label, dose-escalation, dose-finding, and proof-of-concept trial of SP-420 in subjects with transfusion-dependent β-thalassemiaEudraCT:2022-002395-36
Phase:Phase 2, Status:Trial now transitioned, Date:2022-12-16
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=US42268401&_cid=P21-MSCM3W-69668-1
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2006107626&_cid=P21-MSCM3W-69668-1
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=US43268075&_cid=P21-MSCM3W-69668-1
PAT
Desferrithiocin polyether analoguesPublication Number:
US-2017217912-A1Priority Date:
2005-04-04
- Deferithiocin polyether analoguePublication Number:JP-6178816-B2Priority Date:2005-04-04Grant Date:2017-08-09
- Deferithiocin polyether analoguePublication Number:JP-2008536833-APriority Date:2005-04-04
- Desferrithiocin polyether analoguesPublication Number:EP-3190106-A1Priority Date:2005-04-04
- Desferrithiocin polyether analoguesPublication Number:US-9567309-B2Priority Date:2005-04-04Grant Date:2017-02-14
- Desferrithiocin polyether analoguesPublication Number:US-2013030028-A1Priority Date:2005-04-04
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References
- Target Class Profiling of Small-Molecule MethyltransferasesPublication Name:ACS Chemical BiologyPublication Date:2023-03-28PMCID:PMC10983791PMID:36976909DOI:10.1021/acschembio.3c00124
- Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitorsPublication Name:Proceedings of the National Academy of Sciences of the United States of AmericaPublication Date:2020-11-23PMCID:PMC7733812PMID:33229545DOI:10.1073/pnas.2005463117
- Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput ScreeningPublication Name:SLAS discovery : advancing life sciences R & DPublication Date:2020-01PMCID:PMC10791069PMID:31498718DOI:10.1177/2472555219873068
- A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoproteinPublication Name:Molecular PharmacologyPublication Date:2019-11PMCID:PMC6790066PMID:31515284DOI:10.1124/mol.119.115964
- Safety and pharmacokinetics of the oral iron chelator SP‐420 in β‐thalassemiaPublication Name:American Journal of HematologyPublication Date:2017-10-31PMID:28940308DOI:10.1002/ajh.24914
- Metabolically programmed iron chelatorsPublication Name:Bioorganic & Medicinal ChemistryPublication Date:2015-09-01PMCID:PMC4608554PMID:26231739DOI:10.1016/j.bmc.2015.06.059
- Substituent Effects on Desferrithiocin and Desferrithiocin Analogue Iron-Clearing and Toxicity ProfilesPublication Name:Journal of Medicinal ChemistryPublication Date:2012-08-13PMCID:PMC3583384PMID:22889170DOI:10.1021/jm300509y
- CCDC 757291: Experimental Crystal Structure DeterminationPublication Date:2011DOI:10.5517/cctf0rz
- The Impact of Polyether Chain Length on the Iron Clearing Efficiency and Physiochemical Properties of Desferrithiocin AnaloguesPublication Name:Journal of Medicinal ChemistryPublication Date:2010-04-08PMCID:PMC2951135PMID:20232803DOI:10.1021/jm9018146
/////////petadeferitrin, ANAX LABS, iron chelating agent, SP 420, WBX54NZ436
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Perzebertinib, Bizrolertinib
Perzebertinib, Bizrolertinib
CAS 2414056-31-6
MFC27H26F2N8O3 MW548.5 g/mol
5-[(4R)-3,3-difluoro-1-methylpiperidin-4-yl]oxy-6-methoxy-N-[3-methyl-4-([1,2,4]triazolo[1,5-c]pyrimidin-7-yloxy)phenyl]quinazolin-4-amine
- 4-Quinazolinamine, 5-[[(4R)-3,3-difluoro-1-methyl-4-piperidinyl]oxy]-6-methoxy-N-[3-methyl-4-([1,2,4]triazolo[1,5-c]pyrimidin-7-yloxy)phenyl]-
- 5-[[(4R)-3,3-Difluoro-1-methyl-4-piperidinyl]oxy]-6-methoxy-N-[3-methyl-4-([1,2,4]triazolo[1,5-c]pyrimidin-7-yloxy)phenyl]-4-quinazolinamine
5-{[(4R)-3,3-difluoro-1-methylpiperidin-4-yl]oxy}-6-methoxy-N-{3-methyl-4-[([1,2,4]triazolo[1,5-c]pyrimidin-7-yl)oxy]phenyl}quinazolin4-amine
epidermal growth factor receptor tyrosine kinase inhibitor, antineoplastic, ZN-A-1041, ZN 1041, RG 6596, Bizrolertinib, UN8TM5120C
Perzebertinib (also known as bizrolertinib or by developmental codes ZN-A-1041, ZN-1041, and RG6596) is an orally active, potent, and highly selective HER2 (ERBB2) tyrosine kinase inhibitor (TKI) designed to treat advanced solid tumors, primarily HER2-positive breast cancer.
Mechanism of Action
Perzebertinib functions as a selective, irreversible inhibitor of the HER2 tyrosine kinase. It blocks the ATP-binding site of the receptor to stop autophosphorylation. This action shuts down downstream signaling via the PI3K/AKT and MAPK pathways, successfully suppressing the growth, survival, and migration of tumor cells overexpressing HER2.
Key Clinical Advantages
- Blood-Brain Barrier (BBB) Penetration: The drug is designed to cross the blood-brain barrier effectively. This makes it highly valuable for treating brain metastases, a common and aggressive complication in advanced HER2-positive breast cancers.
- EGFR Sparing: Unlike older pan-EGFR/HER2 inhibitors, perzebertinib is engineered to spare wild-type EGFR. Sparing EGFR helps minimise common on-target side effects like severe skin rash and diarrhea.
- Efflux Resistance: It is not a substrate for P-gp or BCRP efflux pumps, allowing it to maintain high concentrations within central nervous system (CNS) tissues.
Development and Clinical Status
Initially discovered and developed by Suzhou Zanrong Pharmaceutical Technology (Zion Pharma), the asset is being co-developed in partnership with Roche and Genentech.
The drug has progressed through Phase 1 clinical studies evaluating its safety and pharmacokinetics in advanced solid tumors, moving forward into Phase 2/3 evaluations for HER2-positive advanced or locally advanced metastatic breast cancer. It is frequently evaluated as a monotherapy or in combination regimens alongside established therapies like capecitabine, trastuzumab, or pertuzumab
PAT
US11723908, Example 37, EG 77
https://patentscope.wipo.int/search/en/detail.jsf?docId=US344952565&_cid=P10-MS9QYW-06569-1
PAT
International Patent Publication No. WO 2020/057511 A1, which is incorporated herein by reference in its entirety, discloses quinazoline compounds that inhibit type I receptor tyrosine kinases, demonstrate good brain penetration in animals, and possess favorable toxicity profiles (for example a decreased activity against hERG), and thus particularly useful in the treatment of type I receptor tyrosine kinases mediated diseases or conditions, in particular ErbB2-associated disease or conditions, including cancer (e.g., metastatic cancer, such as brain metastases). A specific compound, which is identified as (R)-N-(4-([1,2,4]triazolo[1,5-c]pyrimidin-7-yloxy)-3-methylphenyl)-5-((3,3-difluoro-1-methylpiperidin-4-yl)oxy)-6-methoxyquinazolin-4-amine (also referred to as compound (I) herein),
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020057511&_cid=P10-MS9R3W-09545-1
[0681]
(S) -N- (4- ( [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yloxy) -3-methylphenyl) -5- ( (3, 3-difluoro-1-methylpiperidin-4-yl) oxy) -6-methoxyquinazolin-4-amine
Step 5: (R) -N- (4- ( [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yloxy) -3-methylphenyl) -5- ( (3, 3-difluoro-1-methylpiperidin-4-yl) oxy) -6-methoxyquinazolin-4-amine and
[0696]
(S) -N- (4- ( [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yloxy) -3-methylphenyl) -5- ( (3, 3-difluoro-1-methylpiperidin-4-yl) oxy) -6-methoxyquinazolin-4-amine
[0697]
[0698]
To a solution of 4-chloro-5- ( (3, 3-difluoro-1-methylpiperidin-4-yl) oxy) -6-methoxyquinazoline (410 mg, 1.19 mmol) in Propan-2-ol (60 mL) was added TsOH. H 2O (68 mg, 0.36 mmol) and 4- ( [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yloxy) -3-methylaniline (259 mg, 1.07 mmol) . The resulting mixture was stirred at 100℃ under Ar 2protection and concentrated. The residue was dissolved in H 2O (100 mL) , basified with aq. NaHCO 3to pH =7-8, extracted with DCM: MeOH = 20: 1 (100 mLx3) . The combined organic layers were dried over anhydrous Na 2SO 4, filtered and concentrated. The residue was purified by column chromatography (DCM/MeOH=30/1) to give product (300 mg, 46%yield) as white solid. The racemic material was subsequently separated by chiral SFC to give two isomers:
[0699]
(R) -N- (4- ( [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yloxy) -3-methylphenyl) -5- ( (3, 3-difluoro-1-methylpiperidin-4-yl) oxy) -6-methoxyquinazolin-4-amine (Peak 1, retention time 6.241 min, ee: >99%) (100 mg, 67%) as a white solid. MS (ESI) m/z: 549.2 (M+H) +. 1H NMR (400 MHz, CDCl 3) δ 10.04 (s, 1H) , 9.20 (s, 1H) , 8.61 (s, 1H) , 8.33 (s, 1H) , 7.88 (d, J = 2.0 Hz, 1H) , 7.79-7.76 (m, 1H) 7.69 (d, J = 9.2 Hz, 1H) , 7.53 (d, J = 9.2 Hz, 1H) , 7.11 (d, J = 8.8 Hz, 1H) , 6.90 (s, 1H) , 4.84-4.79 (m, 1H) , 4.03 (s, 3H) , 3.22-3.21 (m, 1H) , 2.93 (d, J = 7.2 Hz, 1H) , 2.38 (s, 3H) , 2.41-2.34 (m, 1H) , 2.34-2.27 (m, 1H) , 2.19 (s, 3H) , 2.16-2.10 (m, 2H) .
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References
- Quinazoline derivatives as antitumor agentsPublication Number:US-2023293533-A1Priority Date:2018-09-18
- Quinazoline derivatives as antitumor agentsPublication Number:ES-2971927-T3Priority Date:2018-09-18Grant Date:2024-06-10
- Quinazoline derivatives as antitumor agentsPublication Number:EP-4360713-B1Priority Date:2018-09-18Grant Date:2024-10-30
- Quinazoline derivatives as antitumor agentsPublication Number:ES-3007082-T3Priority Date:2018-09-18Grant Date:2025-03-19
- Quinazoline derivatives as antitumor agentsPublication Number:EP-4360713-A2Priority Date:2018-09-18
- Quinazoline derivatives as antitumor agentsPublication Number:EP-3853220-B1Priority Date:2018-09-18Grant Date:2024-01-03
- Quinazoline derivatives as antitumor agentsPublication Number:EP-3853220-A1Priority Date:2018-09-18
- Quinazoline derivatives as antitumor agentsPublication Number:US-2021386742-A1Priority Date:2018-09-18
- Quinazoline derivatives as antitumor agentsPublication Number:US-11723908-B2Priority Date:2018-09-18Grant Date:2023-08-15
- Crystalline forms of quinazoline derivatives, preparation, compositions and uses thereofPublication Number:CN-120623183-APriority Date:2021-10-20
- Crystalline forms of quinazoline derivatives, preparation, compositions and uses thereofPublication Number:CN-120309621-APriority Date:2021-10-20
- Quinazoline derivatives as antitumor agentsPublication Number:WO-2020057511-A1Priority Date:2018-09-18
- Quinazoline Derivatives as Antitumor AgentsPublication Number:JP-7546550-B2Priority Date:2018-09-18Grant Date:2024-09-06
- Quinazoline derivatives as antitumor agentsPublication Number:CA-3099776-A1Priority Date:2018-09-18
/////////perzebertinib, anax labs, epidermal growth factor receptor tyrosine kinase inhibitor, antineoplastic, ZN-A-1041, ZN 1041, RG 6596, Bizrolertinib, UN8TM5120C
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New Drug Approvals 
