EA201890547A1 - Способ получения ингибитора parp, кристаллические формы и их применения - Google Patents

Способ получения ингибитора parp, кристаллические формы и их применения

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Publication number
EA201890547A1
EA201890547A1 EA201890547A EA201890547A EA201890547A1 EA 201890547 A1 EA201890547 A1 EA 201890547A1 EA 201890547 A EA201890547 A EA 201890547A EA 201890547 A EA201890547 A EA 201890547A EA 201890547 A1 EA201890547 A1 EA 201890547A1
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EA
Eurasian Patent Office
Prior art keywords
crystalline forms
application
obtaining
compound
parp inhibitor
Prior art date
Application number
EA201890547A
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English (en)
Other versions
EA037366B1 (ru
Inventor
Хэсянь Ван
Чаню Чжоу
Бо Рэн
Сяньчжао Куан
Original Assignee
Бейджин, Лтд.
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Application filed by Бейджин, Лтд. filed Critical Бейджин, Лтд.
Publication of EA201890547A1 publication Critical patent/EA201890547A1/ru
Publication of EA037366B1 publication Critical patent/EA037366B1/ru

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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)
  • 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)

Abstract

Настоящее изобретение относится к способу получения ингибитора Parp 1/2 (poly (ADP-ribose)polymerase - поли(аденозиндифосфатрибоза)полимераза), т.е. (R)-2-фтор-10a-метил-7,8,9,10,10a,11-гексагидро-5,6,7a,11-тетраазациклогепта[def]циклопента[а]флуорен-4(5H)-ону (далее называемому соединением A), кристаллическим формам (полиморфам) соединения A или его гидрата или сольвата, особенно кристаллической форме C сесквигидрата соединения A, способам получения кристаллических форм и их применению.
EA201890547A 2015-08-25 2016-08-22 Способ получения ингибитора parp, кристаллические формы и их применения EA037366B1 (ru)

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 true EA201890547A1 (ru) 2018-07-31
EA037366B1 EA037366B1 (ru) 2021-03-18

Family

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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 (ru)
EP (1) EP3341375B1 (ru)
JP (1) JP6940039B2 (ru)
KR (1) KR20180041748A (ru)
CN (2) CN112521390A (ru)
AU (1) AU2016312011B2 (ru)
BR (1) BR112018003634B1 (ru)
CA (1) CA2994895A1 (ru)
EA (1) EA037366B1 (ru)
IL (2) IL296835A (ru)
MX (1) MX2018002322A (ru)
NZ (1) NZ739876A (ru)
TW (1) TWI736550B (ru)
WO (1) WO2017032289A1 (ru)
ZA (1) ZA201800765B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2797921T3 (en) 2011-12-31 2017-10-02 Beigene Ltd FUSED TETRA- OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARB INHIBITORS
US10457680B2 (en) 2015-08-25 2019-10-29 Beigene, Ltd. Process for preparing a PARP inhibitor, crystalline forms, and uses thereof
EP3519051B1 (en) * 2016-09-27 2021-09-22 Beigene, Ltd. Treatment of cancers using 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
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.
US20210205323A1 (en) * 2018-06-01 2021-07-08 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
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
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
MX2021014339A (es) 2019-05-31 2022-01-06 Beigene Ltd Preparacion de granulo inhibidor de parp y proceso de preparacion del mismo.
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
WO2021046014A1 (en) 2019-09-03 2021-03-11 Teva Czech Industries S.R.O Solid state forms of pamiparib and process for preparation thereof

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1140936E (pt) 1999-01-11 2004-06-30 Agouron Pharma Inibidores triciclicos de poli(adp-ribose) polimerases
AU3652102A (en) * 2000-12-01 2002-06-11 Guilford Pharm Inc Compounds and their uses
EA009337B1 (ru) * 2003-01-09 2007-12-28 Пфайзер Инк. Трициклические соединения, представляющие собой ингибиторы протеинкиназ, для увеличения эффективности противоопухолевых агентов и лучевой терапии
CN102171214B (zh) 2008-08-06 2015-06-24 生物马林药物股份有限公司 聚(adp-核糖)聚合酶(parp)的二氢吡啶并酞嗪酮抑制剂
DK2797921T3 (en) * 2011-12-31 2017-10-02 Beigene Ltd FUSED TETRA- OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARB INHIBITORS
CN112457403B (zh) 2013-09-13 2022-11-29 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
KR102130600B1 (ko) 2014-07-03 2020-07-08 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
US10457680B2 (en) 2015-08-25 2019-10-29 Beigene, Ltd. Process for preparing a PARP inhibitor, crystalline forms, and uses thereof
EP3519051B1 (en) * 2016-09-27 2021-09-22 Beigene, Ltd. Treatment of cancers using 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
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

Also Published As

Publication number Publication date
EA037366B1 (ru) 2021-03-18
IL296835A (en) 2022-11-01
BR112018003634A2 (pt) 2018-11-21
CN112521390A (zh) 2021-03-19
AU2016312011A1 (en) 2018-03-08
IL257442B2 (en) 2023-03-01
KR20180041748A (ko) 2018-04-24
US20190177325A1 (en) 2019-06-13
EP3341375B1 (en) 2022-04-13
MX2018002322A (es) 2018-04-11
IL257442A (en) 2018-04-30
US10457680B2 (en) 2019-10-29
IL257442B (en) 2022-11-01
CA2994895A1 (en) 2017-03-02
BR112018003634B1 (pt) 2023-11-21
WO2017032289A1 (en) 2017-03-02
EP3341375A4 (en) 2019-01-16
BR112018003634A8 (pt) 2023-01-17
JP2018528199A (ja) 2018-09-27
EP3341375A1 (en) 2018-07-04
TW201718586A (zh) 2017-06-01
JP6940039B2 (ja) 2021-09-22
CN107922425A (zh) 2018-04-17
CN107922425B (zh) 2021-06-01
NZ739876A (en) 2022-09-30
ZA201800765B (en) 2019-10-30
TWI736550B (zh) 2021-08-21
AU2016312011B2 (en) 2021-02-04

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