TWI736550B - 製備ｐａｒｐ抑制劑、結晶形式的方法及其用途 - Google Patents

製備ｐａｒｐ抑制劑、結晶形式的方法及其用途 Download PDF

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TWI736550B
TWI736550B TW105127160A TW105127160A TWI736550B TW I736550 B TWI736550 B TW I736550B TW 105127160 A TW105127160 A TW 105127160A TW 105127160 A TW105127160 A TW 105127160A TW I736550 B TWI736550 B TW I736550B
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compound
crystalline form
cancer
solvent
sesquihydrate
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TW105127160A
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English (en)
Chinese (zh)
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TW201718586A (zh
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王鶴翔
昌友 周
任博
匡先照
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開曼群島商百濟神州有限公司
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
TW105127160A 2015-08-25 2016-08-24 製備ｐａｒｐ抑制劑、結晶形式的方法及其用途 TWI736550B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CNPCT/CN2015/088003 2015-08-25
CN2015088003 2015-08-25

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TW201718586A TW201718586A (zh) 2017-06-01
TWI736550B true TWI736550B (zh) 2021-08-21

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US (1) US10457680B2 (enExample)
EP (1) EP3341375B1 (enExample)
JP (1) JP6940039B2 (enExample)
KR (1) KR20180041748A (enExample)
CN (2) CN112521390A (enExample)
AU (1) AU2016312011B2 (enExample)
BR (1) BR112018003634B1 (enExample)
CA (1) CA2994895A1 (enExample)
EA (1) EA037366B1 (enExample)
IL (2) IL296835A (enExample)
MX (1) MX385450B (enExample)
NZ (1) NZ739876A (enExample)
TW (1) TWI736550B (enExample)
WO (1) WO2017032289A1 (enExample)
ZA (1) ZA201800765B (enExample)

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MX353578B (es) 2011-12-31 2018-01-19 Beigene Ltd Dihidrodiazpinocarbazolonas tetra o penta-ciclicas fusionadas como inhibidores de poli (adp-ribosa) polimerasa (parp).
KR20180041748A (ko) 2015-08-25 2018-04-24 베이진 엘티디 Parp 억제제, 결정형의 제조방법 및 이의 용도
EP3519051B1 (en) * 2016-09-27 2021-09-22 Beigene, Ltd. Treatment of cancers using combination comprising parp inhibitors
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
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
MX2020012259A (es) * 2018-05-18 2021-01-29 Novartis Ag Formas cristalinas de un inhibidor de tlr7/tlr8.
CN112292133A (zh) * 2018-06-01 2021-01-29 百济神州有限公司 在胃癌治疗中的parp抑制剂维持疗法
USD926356S1 (en) * 2019-03-14 2021-07-27 Tuanfang Liu Battery for electronic cigarette
CN113004279B (zh) * 2019-05-10 2023-01-06 百济神州(苏州)生物科技有限公司 一种控制含parp抑制剂倍半水合物产物的含水量的方法
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
KR20220016028A (ko) * 2019-05-31 2022-02-08 베이진 엘티디 Parp 억제제 펠릿 제조 및 이의 제조방법
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
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. 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
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

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WO2013097225A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors

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PL210415B1 (pl) 1999-01-11 2012-01-31 Agouron Pharma Pochodne indolu, środek farmaceutyczny i zastosowanie pochodnych indolu
ATE478664T1 (de) * 2000-12-01 2010-09-15 Eisai Inc Azaphenanthridone-derivate und deren verwendung als parp-inhibitoren
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ES2792183T3 (es) 2013-09-13 2020-11-10 Beigene Switzerland Gmbh Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico
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KR20180041748A (ko) 2015-08-25 2018-04-24 베이진 엘티디 Parp 억제제, 결정형의 제조방법 및 이의 용도
EP3519051B1 (en) * 2016-09-27 2021-09-22 Beigene, Ltd. Treatment of cancers using combination comprising parp inhibitors
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
CN113004279B (zh) * 2019-05-10 2023-01-06 百济神州(苏州)生物科技有限公司 一种控制含parp抑制剂倍半水合物产物的含水量的方法

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CN107922425B (zh) 2021-06-01
IL296835A (en) 2022-11-01
TW201718586A (zh) 2017-06-01
AU2016312011A1 (en) 2018-03-08
US20190177325A1 (en) 2019-06-13
EA201890547A1 (ru) 2018-07-31
MX385450B (es) 2025-03-18
NZ739876A (en) 2022-09-30
KR20180041748A (ko) 2018-04-24
CN112521390A (zh) 2021-03-19
US10457680B2 (en) 2019-10-29
WO2017032289A1 (en) 2017-03-02
BR112018003634A8 (pt) 2023-01-17
BR112018003634B1 (pt) 2023-11-21
IL257442B (en) 2022-11-01
MX2018002322A (es) 2018-04-11
EP3341375A1 (en) 2018-07-04
BR112018003634A2 (en) 2018-11-21
IL257442B2 (en) 2023-03-01
EP3341375B1 (en) 2022-04-13
JP6940039B2 (ja) 2021-09-22
CA2994895A1 (en) 2017-03-02
AU2016312011B2 (en) 2021-02-04
JP2018528199A (ja) 2018-09-27
EA037366B1 (ru) 2021-03-18
EP3341375A4 (en) 2019-01-16
CN107922425A (zh) 2018-04-17
ZA201800765B (en) 2019-10-30
IL257442A (en) 2018-04-30

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