BR112018003634A8 - Processo para preparar um inibidor parp, formas cristalinas e usos destes - Google Patents

Processo para preparar um inibidor parp, formas cristalinas e usos destes

Info

Publication number
BR112018003634A8
BR112018003634A8 BR112018003634A BR112018003634A BR112018003634A8 BR 112018003634 A8 BR112018003634 A8 BR 112018003634A8 BR 112018003634 A BR112018003634 A BR 112018003634A BR 112018003634 A BR112018003634 A BR 112018003634A BR 112018003634 A8 BR112018003634 A8 BR 112018003634A8
Authority
BR
Brazil
Prior art keywords
crystalline forms
preparing
parp inhibitor
compound
inhibitor
Prior art date
Application number
BR112018003634A
Other languages
English (en)
Other versions
BR112018003634B1 (pt
BR112018003634A2 (pt
Inventor
Hexiang Wang
Zhou Changyou
Ren Bo
Kuang Xianzhao
Original Assignee
Beigene Ltd
Beigene Switzerland Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Beigene Ltd, Beigene Switzerland Gmbh filed Critical Beigene Ltd
Publication of BR112018003634A2 publication Critical patent/BR112018003634A2/pt
Publication of BR112018003634A8 publication Critical patent/BR112018003634A8/pt
Publication of BR112018003634B1 publication Critical patent/BR112018003634B1/pt

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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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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

PROCESSO PARA PREPARAR UM INIBIDOR PARP, FORMAS CRISTALINAS E USOS DESTES. A presente invenção refere-se a um processo para a preparação de um inibidor Parp1 / 2, isto é, (R) -2-fluoro-10a-metil-7,8,9,10,10a, 11-hexa-hidro-5,6,7a, 11-tetraazaciclohepta [def] ciclopenta [a] fluoren-4 (5H) -ona (daqui em diante referido como Composto A), formas cristalinas (polimorfos) do Composto A ou hidratado ou solvente, especialmente a forma cristalina C do Composto A sesqui-hidrato, métodos para a preparação das formas cristalinas e a sua utilização.
BR112018003634-0A 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 BR112018003634B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2015/088003 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 (pt) 2018-11-21
BR112018003634A8 true BR112018003634A8 (pt) 2023-01-17
BR112018003634B1 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 (pt)
EP (1) EP3341375B1 (pt)
JP (1) JP6940039B2 (pt)
KR (1) KR20180041748A (pt)
CN (2) CN112521390A (pt)
AU (1) AU2016312011B2 (pt)
BR (1) BR112018003634B1 (pt)
CA (1) CA2994895A1 (pt)
EA (1) EA037366B1 (pt)
IL (2) IL296835A (pt)
MX (1) MX2018002322A (pt)
NZ (1) NZ739876A (pt)
TW (1) TWI736550B (pt)
WO (1) WO2017032289A1 (pt)
ZA (1) ZA201800765B (pt)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106220635B (zh) 2011-12-31 2019-03-08 百济神州有限公司 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮
AU2016312011B2 (en) 2015-08-25 2021-02-04 Beigene, Ltd. Process for preparing Parp inhibitor, crystalline forms, and uses thereof
WO2018059437A1 (en) 2016-09-27 2018-04-05 Beigene, Ltd. Treatment cancers using combination comprising parp inhibitors
WO2018157794A1 (en) * 2017-02-28 2018-09-07 Beigene, Ltd. Crystalline forms of salts of fused tera or penta-cyclic dihydrodiazepinocarazolones, 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
CN110891576A (zh) * 2017-07-17 2020-03-17 百济神州有限公司 使用包含parp抑制剂、替莫唑胺和/或放射疗法的组合治疗癌症
WO2019220390A1 (en) * 2018-05-18 2019-11-21 Novartis Ag Crystalline forms of a tlr7/tlr8 inhibitor
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
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
CN112007011A (zh) * 2019-05-31 2020-12-01 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
AU2020282478A1 (en) * 2019-05-31 2021-09-16 Beigene, Ltd. PARP inhibitor pellet preparation and preparation process therefor
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
JP4093448B2 (ja) 1999-01-11 2008-06-04 アグロン・ファーマシューティカルズ・インコーポレーテッド ポリ（ａｄｐ−リボース）ポリメラーゼの三環系阻害剤
US6887996B2 (en) * 2000-12-01 2005-05-03 Guilford Pharmaceuticals Inc. Compounds and their use
ATE404564T1 (de) * 2003-01-09 2008-08-15 Pfizer Diazepinoindolderivate als kinaseinhibitoren
EP2326650B9 (en) 2008-08-06 2014-09-10 BioMarin Pharmaceutical Inc. Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp)
CN106220635B (zh) * 2011-12-31 2019-03-08 百济神州有限公司 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮
SG11201601844TA (en) 2013-09-13 2016-04-28 Beigene Ltd Anti-pd1 antibodies and their use as therapeutics and diagnostics
JP6526189B2 (ja) 2014-07-03 2019-06-05 ベイジーン リミテッド 抗ｐｄ−ｌ１抗体並びにその治療及び診断のための使用
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
AU2016312011B2 (en) 2015-08-25 2021-02-04 Beigene, Ltd. Process for preparing Parp inhibitor, crystalline forms, and uses thereof
WO2018059437A1 (en) 2016-09-27 2018-04-05 Beigene, Ltd. Treatment cancers using combination comprising parp inhibitors
WO2018157794A1 (en) 2017-02-28 2018-09-07 Beigene, Ltd. Crystalline forms of salts of fused tera or penta-cyclic dihydrodiazepinocarazolones, and uses thereof
CN110891576A (zh) * 2017-07-17 2020-03-17 百济神州有限公司 使用包含parp抑制剂、替莫唑胺和/或放射疗法的组合治疗癌症
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

Also Published As

Publication number Publication date
CA2994895A1 (en) 2017-03-02
MX2018002322A (es) 2018-04-11
TWI736550B (zh) 2021-08-21
TW201718586A (zh) 2017-06-01
BR112018003634B1 (pt) 2023-11-21
JP6940039B2 (ja) 2021-09-22
CN107922425B (zh) 2021-06-01
JP2018528199A (ja) 2018-09-27
BR112018003634A2 (pt) 2018-11-21
CN107922425A (zh) 2018-04-17
EA201890547A1 (ru) 2018-07-31
IL257442B2 (en) 2023-03-01
AU2016312011A1 (en) 2018-03-08
EP3341375A1 (en) 2018-07-04
NZ739876A (en) 2022-09-30
US20190177325A1 (en) 2019-06-13
IL296835A (en) 2022-11-01
WO2017032289A1 (en) 2017-03-02
EA037366B1 (ru) 2021-03-18
KR20180041748A (ko) 2018-04-24
IL257442A (en) 2018-04-30
EP3341375B1 (en) 2022-04-13
CN112521390A (zh) 2021-03-19
ZA201800765B (en) 2019-10-30
US10457680B2 (en) 2019-10-29
AU2016312011B2 (en) 2021-02-04
EP3341375A4 (en) 2019-01-16
IL257442B (en) 2022-11-01

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B350 Update of information on the portal [chapter 15.35 patent gazette]
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Free format text: NOTIFICACAO DE DEVOLUCAO DO PEDIDO EM FUNCAO DA REVOGACAO DO ART. 229-C DA LEI NO 9.279, DE 1996, POR FORCA DA LEI NO 14.195, DE 2021

B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B25A Requested transfer of rights approved

Owner name: BEIGENE SWITZERLAND GMBH (CH)

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 22/08/2016, OBSERVADAS AS CONDICOES LEGAIS