EA037366B1 - Способ получения ингибитора parp, кристаллические формы и их применения - Google Patents
Способ получения ингибитора parp, кристаллические формы и их применения Download PDFInfo
- Publication number
- EA037366B1 EA037366B1 EA201890547A EA201890547A EA037366B1 EA 037366 B1 EA037366 B1 EA 037366B1 EA 201890547 A EA201890547 A EA 201890547A EA 201890547 A EA201890547 A EA 201890547A EA 037366 B1 EA037366 B1 EA 037366B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- crystalline form
- compound
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- degrees
- ray powder
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2015088003 | 2015-08-25 | ||
| PCT/CN2016/096200 WO2017032289A1 (en) | 2015-08-25 | 2016-08-22 | Process for preparing parp inhibitor, crystalline forms, and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201890547A1 EA201890547A1 (ru) | 2018-07-31 |
| EA037366B1 true EA037366B1 (ru) | 2021-03-18 |
Family
ID=58099633
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201890547A EA037366B1 (ru) | 2015-08-25 | 2016-08-22 | Способ получения ингибитора parp, кристаллические формы и их применения |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10457680B2 (enExample) |
| EP (1) | EP3341375B1 (enExample) |
| JP (1) | JP6940039B2 (enExample) |
| KR (1) | KR20180041748A (enExample) |
| CN (2) | CN107922425B (enExample) |
| AU (1) | AU2016312011B2 (enExample) |
| BR (1) | BR112018003634B1 (enExample) |
| CA (1) | CA2994895A1 (enExample) |
| EA (1) | EA037366B1 (enExample) |
| IL (2) | IL257442B2 (enExample) |
| MX (1) | MX385450B (enExample) |
| NZ (1) | NZ739876A (enExample) |
| TW (1) | TWI736550B (enExample) |
| WO (1) | WO2017032289A1 (enExample) |
| ZA (1) | ZA201800765B (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS56616B1 (sr) | 2011-12-31 | 2018-02-28 | Beigene Ltd | Kondenzovani tetra ili penta-ciklični dihidrodiazepinokarbazoloni kao parp inhibitori |
| CN107922425B (zh) | 2015-08-25 | 2021-06-01 | 百济神州有限公司 | 制备parp抑制剂、结晶形式的方法及其用途 |
| US11202782B2 (en) * | 2016-09-27 | 2021-12-21 | Beigene, Ltd. | Treatment cancers using a combination comprising PARP inhibitors |
| US10899763B2 (en) | 2017-02-28 | 2021-01-26 | Beigene, Ltd. | Crystalline forms of salts of fused penta-cyclic dihydrodiazepinocarbazolones, and uses thereof |
| WO2018165615A1 (en) | 2017-03-09 | 2018-09-13 | The Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Parp-1 and methods of use thereof |
| US12121518B2 (en) | 2017-03-09 | 2024-10-22 | The Board Of Supervisors Of Louisiana State Universi And Agricultural And Mechanical College | PARP-1 and methods of use thereof |
| WO2019015561A1 (en) * | 2017-07-17 | 2019-01-24 | Beigene, Ltd. | TREATMENT OF CANCERS USING A COMBINATION COMPRISING INHIBITORS OF PARP, TEMOZOLOMIDE AND / OR RADIOTHERAPY |
| AU2019268583B2 (en) | 2018-05-18 | 2022-01-27 | Novartis Ag | Crystalline forms of a TLR7/TLR8 inhibitor |
| AU2019275722A1 (en) * | 2018-06-01 | 2020-11-12 | Beigene, Ltd. | Maintenance therapy of a PARP inhibitor in treating gastric cancer |
| USD926356S1 (en) * | 2019-03-14 | 2021-07-27 | Tuanfang Liu | Battery for electronic cigarette |
| CN111171031B (zh) * | 2019-05-10 | 2021-04-09 | 百济神州(苏州)生物科技有限公司 | 一种含parp抑制剂倍半水合物产物的制备方法 |
| CN111171001B (zh) * | 2019-05-16 | 2022-04-29 | 百济神州(苏州)生物科技有限公司 | 一种parp抑制剂中间体的结晶方法 |
| CN113402502B (zh) * | 2019-05-16 | 2022-10-14 | 百济神州(苏州)生物科技有限公司 | 一种parp抑制剂中间体制备的物料组合体系 |
| CN112007011B (zh) * | 2019-05-31 | 2024-07-23 | 百济神州(苏州)生物科技有限公司 | 一种parp抑制剂微丸胶囊及其制备工艺 |
| WO2020239097A1 (zh) * | 2019-05-31 | 2020-12-03 | 百济神州有限公司 | 一种parp抑制剂微丸制剂及其制备工艺 |
| WO2021046014A1 (en) | 2019-09-03 | 2021-03-11 | Teva Czech Industries S.R.O | Solid state forms of pamiparib and process for preparation thereof |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025217307A1 (en) | 2024-04-09 | 2025-10-16 | Revolution Medicines, Inc. | Methods for predicting response to a ras(on) inhibitor and combination therapies |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002044183A2 (en) * | 2000-12-01 | 2002-06-06 | Guilford Pharmaceuticals Inc. | Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors |
| WO2004063198A1 (en) * | 2003-01-09 | 2004-07-29 | Pfizer Inc. | Diazepinoindole derivatives as kinase inhibitors |
| WO2013097225A1 (en) * | 2011-12-31 | 2013-07-04 | Beigene, Ltd. | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20010573B1 (en) | 1999-01-11 | 2006-04-30 | Agouron Pharmaceuticals | Tricyclic inhibitors of poly(adp-ribose) polymerases |
| EP2767537B1 (en) | 2008-08-06 | 2017-04-12 | Medivation Technologies, Inc. | Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP) |
| JP6623353B2 (ja) | 2013-09-13 | 2019-12-25 | ベイジーン スウィッツァーランド ゲーエムベーハー | 抗ｐｄ−１抗体並びにその治療及び診断のための使用 |
| KR102003754B1 (ko) | 2014-07-03 | 2019-07-25 | 베이진 엘티디 | Pd-l1 항체와 이를 이용한 치료 및 진단 |
| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
| CN107922425B (zh) | 2015-08-25 | 2021-06-01 | 百济神州有限公司 | 制备parp抑制剂、结晶形式的方法及其用途 |
| US11202782B2 (en) * | 2016-09-27 | 2021-12-21 | Beigene, Ltd. | Treatment cancers using a combination comprising PARP inhibitors |
| US10899763B2 (en) * | 2017-02-28 | 2021-01-26 | Beigene, Ltd. | Crystalline forms of salts of fused penta-cyclic dihydrodiazepinocarbazolones, and uses thereof |
| WO2019015561A1 (en) | 2017-07-17 | 2019-01-24 | Beigene, Ltd. | TREATMENT OF CANCERS USING A COMBINATION COMPRISING INHIBITORS OF PARP, TEMOZOLOMIDE AND / OR RADIOTHERAPY |
| CN111171031B (zh) * | 2019-05-10 | 2021-04-09 | 百济神州(苏州)生物科技有限公司 | 一种含parp抑制剂倍半水合物产物的制备方法 |
-
2016
- 2016-08-22 CN CN201680048637.5A patent/CN107922425B/zh active Active
- 2016-08-22 NZ NZ739876A patent/NZ739876A/en not_active IP Right Cessation
- 2016-08-22 US US15/753,993 patent/US10457680B2/en active Active
- 2016-08-22 CN CN202011223061.6A patent/CN112521390A/zh active Pending
- 2016-08-22 WO PCT/CN2016/096200 patent/WO2017032289A1/en not_active Ceased
- 2016-08-22 CA CA2994895A patent/CA2994895A1/en active Pending
- 2016-08-22 KR KR1020187008548A patent/KR20180041748A/ko not_active Ceased
- 2016-08-22 EP EP16838548.2A patent/EP3341375B1/en not_active Not-in-force
- 2016-08-22 EA EA201890547A patent/EA037366B1/ru not_active IP Right Cessation
- 2016-08-22 BR BR112018003634-0A patent/BR112018003634B1/pt not_active IP Right Cessation
- 2016-08-22 IL IL257442A patent/IL257442B2/en unknown
- 2016-08-22 AU AU2016312011A patent/AU2016312011B2/en not_active Ceased
- 2016-08-22 JP JP2018510352A patent/JP6940039B2/ja not_active Expired - Fee Related
- 2016-08-22 MX MX2018002322A patent/MX385450B/es unknown
- 2016-08-22 IL IL296835A patent/IL296835A/en unknown
- 2016-08-24 TW TW105127160A patent/TWI736550B/zh not_active IP Right Cessation
-
2018
- 2018-02-06 ZA ZA201800765A patent/ZA201800765B/en unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002044183A2 (en) * | 2000-12-01 | 2002-06-06 | Guilford Pharmaceuticals Inc. | Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors |
| WO2004063198A1 (en) * | 2003-01-09 | 2004-07-29 | Pfizer Inc. | Diazepinoindole derivatives as kinase inhibitors |
| WO2013097225A1 (en) * | 2011-12-31 | 2013-07-04 | Beigene, Ltd. | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors |
Non-Patent Citations (1)
| Title |
|---|
| "RN: 1858211-28-5" STN Registry, 02 February 2016 (2016-02-02) * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN107922425A (zh) | 2018-04-17 |
| ZA201800765B (en) | 2019-10-30 |
| MX385450B (es) | 2025-03-18 |
| CN112521390A (zh) | 2021-03-19 |
| US20190177325A1 (en) | 2019-06-13 |
| IL296835A (en) | 2022-11-01 |
| CN107922425B (zh) | 2021-06-01 |
| EP3341375B1 (en) | 2022-04-13 |
| BR112018003634A8 (pt) | 2023-01-17 |
| JP6940039B2 (ja) | 2021-09-22 |
| KR20180041748A (ko) | 2018-04-24 |
| IL257442A (en) | 2018-04-30 |
| CA2994895A1 (en) | 2017-03-02 |
| BR112018003634A2 (en) | 2018-11-21 |
| EP3341375A4 (en) | 2019-01-16 |
| IL257442B2 (en) | 2023-03-01 |
| AU2016312011A1 (en) | 2018-03-08 |
| WO2017032289A1 (en) | 2017-03-02 |
| BR112018003634B1 (pt) | 2023-11-21 |
| JP2018528199A (ja) | 2018-09-27 |
| EP3341375A1 (en) | 2018-07-04 |
| AU2016312011B2 (en) | 2021-02-04 |
| IL257442B (en) | 2022-11-01 |
| TW201718586A (zh) | 2017-06-01 |
| MX2018002322A (es) | 2018-04-11 |
| TWI736550B (zh) | 2021-08-21 |
| US10457680B2 (en) | 2019-10-29 |
| EA201890547A1 (ru) | 2018-07-31 |
| NZ739876A (en) | 2022-09-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM |