AU2016312011B2 - Process for preparing Parp inhibitor, crystalline forms, and uses thereof - Google Patents

Process for preparing Parp inhibitor, crystalline forms, and uses thereof Download PDF

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Publication number
AU2016312011B2
AU2016312011B2 AU2016312011A AU2016312011A AU2016312011B2 AU 2016312011 B2 AU2016312011 B2 AU 2016312011B2 AU 2016312011 A AU2016312011 A AU 2016312011A AU 2016312011 A AU2016312011 A AU 2016312011A AU 2016312011 B2 AU2016312011 B2 AU 2016312011B2
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AU
Australia
Prior art keywords
crystalline form
compound
solvent
hydrate
group
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Ceased
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AU2016312011A
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English (en)
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AU2016312011A1 (en
Inventor
Xianzhao Kuang
Bo REN
Hexiang Wang
Changyou Zhou
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BeOne Medicines Ltd
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Beigene Ltd
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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=AU2016312011(B2) "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 AU2016312011A1 publication Critical patent/AU2016312011A1/en
Application granted granted Critical
Publication of AU2016312011B2 publication Critical patent/AU2016312011B2/en
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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

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)
AU2016312011A 2015-08-25 2016-08-22 Process for preparing Parp inhibitor, crystalline forms, and uses thereof Ceased AU2016312011B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2015088003 2015-08-25
CNPCT/CN2015/088003 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
AU2016312011A1 AU2016312011A1 (en) 2018-03-08
AU2016312011B2 true AU2016312011B2 (en) 2021-02-04

Family

ID=58099633

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2016312011A Ceased AU2016312011B2 (en) 2015-08-25 2016-08-22 Process for preparing Parp inhibitor, crystalline forms, and uses thereof

Country Status (15)

Country Link
US (1) US10457680B2 (OSRAM)
EP (1) EP3341375B1 (OSRAM)
JP (1) JP6940039B2 (OSRAM)
KR (1) KR20180041748A (OSRAM)
CN (2) CN107922425B (OSRAM)
AU (1) AU2016312011B2 (OSRAM)
BR (1) BR112018003634B1 (OSRAM)
CA (1) CA2994895A1 (OSRAM)
EA (1) EA037366B1 (OSRAM)
IL (2) IL296835A (OSRAM)
MX (1) MX385450B (OSRAM)
NZ (1) NZ739876A (OSRAM)
TW (1) TWI736550B (OSRAM)
WO (1) WO2017032289A1 (OSRAM)
ZA (1) ZA201800765B (OSRAM)

Families Citing this family (23)

* 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
NZ739876A (en) 2015-08-25 2022-09-30 Beigene Ltd Process for preparing parp inhibitor, crystalline forms, and uses thereof
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
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
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
AR117573A1 (es) 2018-05-18 2021-08-18 Novartis Ag Formas cristalinas de un inhibidor tlr7 / tlr8
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
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
AU2020282478A1 (en) * 2019-05-31 2021-09-16 Beigene, Ltd. PARP inhibitor pellet preparation and preparation process therefor
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
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 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
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (1)

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

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AU781711B2 (en) 1999-01-11 2005-06-09 Agouron Pharmaceuticals, Inc. Tricyclic inhibitors of poly(ADP-ribose) polymerases
ES2354249T3 (es) 2000-12-01 2011-03-11 Eisai Inc. Derivados de azafenantridona y su uso como inhibidores de parp.
CA2512683C (en) * 2003-01-09 2010-03-16 Pfizer Inc. Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agents and radiation therapy
SG193842A1 (en) 2008-08-06 2013-10-30 Biomarin Pharm Inc Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp)
PT3702373T (pt) 2013-09-13 2022-09-27 Beigene Switzerland Gmbh Anticorpos anti-pd1 e a sua utilização como agentes terapêuticos e de diagnóstico
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
NZ739876A (en) 2015-08-25 2022-09-30 Beigene Ltd Process for preparing parp inhibitor, crystalline forms, and uses thereof
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
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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013097225A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors

Also Published As

Publication number Publication date
CA2994895A1 (en) 2017-03-02
KR20180041748A (ko) 2018-04-24
BR112018003634A2 (en) 2018-11-21
CN107922425A (zh) 2018-04-17
JP6940039B2 (ja) 2021-09-22
IL257442B (en) 2022-11-01
CN107922425B (zh) 2021-06-01
IL257442A (en) 2018-04-30
BR112018003634B1 (pt) 2023-11-21
US20190177325A1 (en) 2019-06-13
CN112521390A (zh) 2021-03-19
NZ739876A (en) 2022-09-30
EP3341375A1 (en) 2018-07-04
EP3341375B1 (en) 2022-04-13
JP2018528199A (ja) 2018-09-27
TW201718586A (zh) 2017-06-01
ZA201800765B (en) 2019-10-30
WO2017032289A1 (en) 2017-03-02
EA037366B1 (ru) 2021-03-18
US10457680B2 (en) 2019-10-29
AU2016312011A1 (en) 2018-03-08
MX2018002322A (es) 2018-04-11
TWI736550B (zh) 2021-08-21
EP3341375A4 (en) 2019-01-16
EA201890547A1 (ru) 2018-07-31
IL257442B2 (en) 2023-03-01
MX385450B (es) 2025-03-18
IL296835A (en) 2022-11-01
BR112018003634A8 (pt) 2023-01-17

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