CN112521390A - 制备parp抑制剂、结晶形式的方法及其用途 - Google Patents

制备parp抑制剂、结晶形式的方法及其用途 Download PDF

Info

Publication number
CN112521390A
CN112521390A CN202011223061.6A CN202011223061A CN112521390A CN 112521390 A CN112521390 A CN 112521390A CN 202011223061 A CN202011223061 A CN 202011223061A CN 112521390 A CN112521390 A CN 112521390A
Authority
CN
China
Prior art keywords
compound
crystalline form
solvent
def
hexahydro
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN202011223061.6A
Other languages
English (en)
Chinese (zh)
Inventor
王鹤翔
周昌友
任博
匡先照
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Baiji Shenzhou Suzhou Biotechnology Co ltd
Original Assignee
Beigene Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=58099633&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN112521390(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Beigene Ltd filed Critical Beigene Ltd
Publication of CN112521390A publication Critical patent/CN112521390A/zh
Pending legal-status Critical Current

Links

Images

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)
  • 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)
CN202011223061.6A 2015-08-25 2016-08-22 制备parp抑制剂、结晶形式的方法及其用途 Pending CN112521390A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2015/088003 2015-08-25
CN2015088003 2015-08-25
CN201680048637.5A CN107922425B (zh) 2015-08-25 2016-08-22 制备parp抑制剂、结晶形式的方法及其用途

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201680048637.5A Division CN107922425B (zh) 2015-08-25 2016-08-22 制备parp抑制剂、结晶形式的方法及其用途

Publications (1)

Publication Number Publication Date
CN112521390A true CN112521390A (zh) 2021-03-19

Family

ID=58099633

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202011223061.6A Pending CN112521390A (zh) 2015-08-25 2016-08-22 制备parp抑制剂、结晶形式的方法及其用途
CN201680048637.5A Active CN107922425B (zh) 2015-08-25 2016-08-22 制备parp抑制剂、结晶形式的方法及其用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201680048637.5A Active CN107922425B (zh) 2015-08-25 2016-08-22 制备parp抑制剂、结晶形式的方法及其用途

Country Status (15)

Country Link
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)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
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).
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

Citations (7)

* Cited by examiner, † Cited by third party
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
CN110087730A (zh) * 2016-09-27 2019-08-02 百济神州有限公司 使用包含parp抑制剂的组合产品治疗癌症
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
CN111171031A (zh) * 2019-05-10 2020-05-19 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
CN110392687B (zh) * 2017-02-28 2022-08-02 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及其用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL210415B1 (pl) 1999-01-11 2012-01-31 Agouron Pharma Pochodne indolu, środek farmaceutyczny i zastosowanie pochodnych indolu
EP2326650B9 (en) 2008-08-06 2014-09-10 BioMarin Pharmaceutical Inc. Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp)
ES2792183T3 (es) 2013-09-13 2020-11-10 Beigene Switzerland Gmbh Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico
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
KR20180041748A (ko) 2015-08-25 2018-04-24 베이진 엘티디 Parp 억제제, 결정형의 제조방법 및 이의 용도

Patent Citations (7)

* Cited by examiner, † Cited by third party
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
CN110087730A (zh) * 2016-09-27 2019-08-02 百济神州有限公司 使用包含parp抑制剂的组合产品治疗癌症
CN110392687B (zh) * 2017-02-28 2022-08-02 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及其用途
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
CN111171031A (zh) * 2019-05-10 2020-05-19 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
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
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
TWI736550B (zh) 2021-08-21
EP3341375A4 (en) 2019-01-16
CN107922425A (zh) 2018-04-17
ZA201800765B (en) 2019-10-30
IL257442A (en) 2018-04-30

Similar Documents

Publication Publication Date Title
CN107922425B (zh) 制备parp抑制剂、结晶形式的方法及其用途
EP2850082B1 (en) 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido(2,3-d)pyrimidin-6-yl)phenyl)urea as Raf kinase inhibitor for the treatment of cancer
WO2021190467A1 (zh) 含螺环的喹唑啉化合物
WO2021129820A1 (zh) 含螺环的喹唑啉化合物
WO2022017533A1 (zh) 用作cdk7激酶抑制剂的化合物及其应用
CN113454081A (zh) 咪唑并吡啶基化合物及其用于治疗增生性疾病的用途
JP2019526605A (ja) 置換２−ｈ−ピラゾール誘導体の結晶形、塩型及びその製造方法
CN106749261A (zh) 一类取代三唑并哌嗪类parp抑制剂及其制备方法和用途
JP2025538371A (ja) 含窒素複素環系化合物の薬用可能な塩、結晶型及び調製方法
HK40040143A (en) Process for preparing parp inhibitor, crystalline forms, and uses thereof
CN103373971B (zh) 作为蛋白激酶抑制剂的脲类化合物
EP4596553A1 (en) Salt of dioxane quinoline compound, crystal form thereof, preparation methods therefor and uses thereof
EP3677581A1 (en) Deuterated indoleamine 2,3-dioxygenase inhibitor and application thereof
KR100874209B1 (ko) 3,10-다이하이드로-1Ｈ-[1,4]다이아제피노[5,6-ｂ]인돌-2-온 유도체 및 약학적으로 허용 가능한 염, 그의 제조방법및 그의 용도
WO2025231053A1 (en) Solid forms of 6-chloro-3-[(1r)-1-[3,6-dimethyl-2-(2-methylindazol-5-yl)-4-oxo-chromen-8-yl]ethoxy]pyridine-2-carboxamide
HK40061853B (zh) 用作cdk7激酶抑制剂的化合物及其应用
TW202519531A (zh) 含丙烯酮類生物抑制劑的晶型及其製備方法和應用
WO2021092892A1 (zh) 喹啉或喹唑啉类化合物在制备抗肿瘤药物中的应用
HK40058867A (en) Imidazopyridinyl compounds and use thereof for treatment of proliferative disorders

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
TA01 Transfer of patent application right
TA01 Transfer of patent application right

Effective date of registration: 20210604

Address after: Nine Biological Industrial Parks 218 Sangtian Street, Suzhou Industrial Park, Suzhou City, Jiangsu Province

Applicant after: Baiji Shenzhou (Suzhou) Biotechnology Co.,Ltd.

Address before: 94 sonaris Avenue, kamana Bay, grand caiman, British Isles

Applicant before: BEIGENE, Ltd.

REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40040143

Country of ref document: HK

RJ01 Rejection of invention patent application after publication
RJ01 Rejection of invention patent application after publication

Application publication date: 20210319