BR112018003634B1 - Forma cristalina de sesqui-hidrato de um inibidor parp, método de preparação da dita forma cristalina e composição farmacêutica compreendendo a dita forma - Google Patents
Forma cristalina de sesqui-hidrato de um inibidor parp, método de preparação da dita forma cristalina e composição farmacêutica compreendendo a dita forma Download PDFInfo
- Publication number
- BR112018003634B1 BR112018003634B1 BR112018003634-0A BR112018003634A BR112018003634B1 BR 112018003634 B1 BR112018003634 B1 BR 112018003634B1 BR 112018003634 A BR112018003634 A BR 112018003634A BR 112018003634 B1 BR112018003634 B1 BR 112018003634B1
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- crystalline form
- solvent
- crystalline
- hydrate
- 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 (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2015/088003 | 2015-08-25 | ||
| CNCN2015/088003 | 2015-08-25 | ||
| 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 (3)
| Publication Number | Publication Date |
|---|---|
| BR112018003634A2 BR112018003634A2 (en) | 2018-11-21 |
| BR112018003634A8 BR112018003634A8 (pt) | 2023-01-17 |
| BR112018003634B1 true BR112018003634B1 (pt) | 2023-11-21 |
Family
ID=58099633
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112018003634-0A BR112018003634B1 (pt) | 2015-08-25 | 2016-08-22 | Forma cristalina de sesqui-hidrato de um inibidor parp, método de preparação da dita forma cristalina e composição farmacêutica compreendendo a dita forma |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10457680B2 (https=) |
| EP (1) | EP3341375B1 (https=) |
| JP (1) | JP6940039B2 (https=) |
| KR (1) | KR20180041748A (https=) |
| CN (2) | CN112521390A (https=) |
| AU (1) | AU2016312011B2 (https=) |
| BR (1) | BR112018003634B1 (https=) |
| CA (1) | CA2994895A1 (https=) |
| EA (1) | EA037366B1 (https=) |
| IL (2) | IL257442B2 (https=) |
| MX (1) | MX385450B (https=) |
| NZ (1) | NZ739876A (https=) |
| TW (1) | TWI736550B (https=) |
| WO (1) | WO2017032289A1 (https=) |
| ZA (1) | ZA201800765B (https=) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX353578B (es) | 2011-12-31 | 2018-01-19 | Beigene Ltd | Dihidrodiazpinocarbazolonas tetra o penta-ciclicas fusionadas como inhibidores de poli (adp-ribosa) polimerasa (parp). |
| EA037366B1 (ru) | 2015-08-25 | 2021-03-18 | Бейджин, Лтд. | Способ получения ингибитора parp, кристаллические формы и их применения |
| CN110087730B (zh) * | 2016-09-27 | 2023-03-28 | 百济神州(苏州)生物科技有限公司 | 使用包含parp抑制剂的组合产品治疗癌症 |
| CN115433187B (zh) | 2017-02-28 | 2023-10-27 | 百济神州(苏州)生物科技有限公司 | 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式组合物及其用途 |
| 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 |
| 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 |
| WO2019015561A1 (en) * | 2017-07-17 | 2019-01-24 | Beigene, Ltd. | TREATMENT OF CANCERS USING A COMBINATION COMPRISING INHIBITORS OF PARP, TEMOZOLOMIDE AND / OR RADIOTHERAPY |
| JP7407740B2 (ja) | 2018-05-18 | 2024-01-04 | ノバルティス アーゲー | Ｔｌｒ７／ｔｌｒ８阻害剤の結晶形態 |
| 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 |
| CN111171002B (zh) * | 2019-05-16 | 2021-04-06 | 百济神州(苏州)生物科技有限公司 | 一种parp抑制剂中间体的制备方法 |
| 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 |
| 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 |
| CN113438944A (zh) * | 2019-05-31 | 2021-09-24 | 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 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| 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 |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6495541B1 (en) | 1999-01-11 | 2002-12-17 | Agouron Pharmaceuticals, Inc. | Tricyclic inhibitors of poly(ADP-ribose) polymerases |
| JP4323802B2 (ja) * | 2000-12-01 | 2009-09-02 | エムジーアイ・ジーピー・インコーポレーテッド | 化合物およびその使用 |
| JP3990718B2 (ja) * | 2003-01-09 | 2007-10-17 | ファイザー・インク | キナーゼ阻害剤としてのジアゼピノインドール誘導体 |
| CN104478875B (zh) | 2008-08-06 | 2017-04-12 | 麦迪韦逊科技有限公司 | 聚(adp‑核糖)聚合酶(parp)的二氢吡啶并酞嗪酮抑制剂 |
| MX353578B (es) | 2011-12-31 | 2018-01-19 | Beigene Ltd | Dihidrodiazpinocarbazolonas tetra o penta-ciclicas fusionadas como inhibidores de poli (adp-ribosa) polimerasa (parp). |
| CN112552401B (zh) | 2013-09-13 | 2023-08-25 | 广州百济神州生物制药有限公司 | 抗pd1抗体及其作为治疗剂与诊断剂的用途 |
| CN106604742B (zh) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
| EA037366B1 (ru) | 2015-08-25 | 2021-03-18 | Бейджин, Лтд. | Способ получения ингибитора parp, кристаллические формы и их применения |
| CN110087730B (zh) * | 2016-09-27 | 2023-03-28 | 百济神州(苏州)生物科技有限公司 | 使用包含parp抑制剂的组合产品治疗癌症 |
| CN115433187B (zh) * | 2017-02-28 | 2023-10-27 | 百济神州(苏州)生物科技有限公司 | 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式组合物及其用途 |
| 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 EA EA201890547A patent/EA037366B1/ru not_active IP Right Cessation
- 2016-08-22 CN CN202011223061.6A patent/CN112521390A/zh active Pending
- 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 US US15/753,993 patent/US10457680B2/en active Active
- 2016-08-22 KR KR1020187008548A patent/KR20180041748A/ko not_active Ceased
- 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 WO PCT/CN2016/096200 patent/WO2017032289A1/en not_active Ceased
- 2016-08-22 CA CA2994895A patent/CA2994895A1/en active Pending
- 2016-08-22 IL IL257442A patent/IL257442B2/en unknown
- 2016-08-22 EP EP16838548.2A patent/EP3341375B1/en not_active Not-in-force
- 2016-08-22 BR BR112018003634-0A patent/BR112018003634B1/pt not_active IP Right Cessation
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| CN107922425B (zh) | 2021-06-01 |
| CA2994895A1 (en) | 2017-03-02 |
| MX2018002322A (es) | 2018-04-11 |
| EA037366B1 (ru) | 2021-03-18 |
| IL257442B2 (en) | 2023-03-01 |
| TW201718586A (zh) | 2017-06-01 |
| EP3341375A1 (en) | 2018-07-04 |
| CN112521390A (zh) | 2021-03-19 |
| BR112018003634A8 (pt) | 2023-01-17 |
| JP6940039B2 (ja) | 2021-09-22 |
| EA201890547A1 (ru) | 2018-07-31 |
| EP3341375B1 (en) | 2022-04-13 |
| KR20180041748A (ko) | 2018-04-24 |
| CN107922425A (zh) | 2018-04-17 |
| MX385450B (es) | 2025-03-18 |
| WO2017032289A1 (en) | 2017-03-02 |
| ZA201800765B (en) | 2019-10-30 |
| TWI736550B (zh) | 2021-08-21 |
| IL257442A (en) | 2018-04-30 |
| JP2018528199A (ja) | 2018-09-27 |
| NZ739876A (en) | 2022-09-30 |
| AU2016312011A1 (en) | 2018-03-08 |
| AU2016312011B2 (en) | 2021-02-04 |
| US20190177325A1 (en) | 2019-06-13 |
| IL257442B (en) | 2022-11-01 |
| US10457680B2 (en) | 2019-10-29 |
| BR112018003634A2 (en) | 2018-11-21 |
| IL296835A (en) | 2022-11-01 |
| EP3341375A4 (en) | 2019-01-16 |
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Legal Events
| Date | Code | Title | Description |
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