KR20180041748A - Parp 억제제, 결정형의 제조방법 및 이의 용도 - Google Patents

Parp 억제제, 결정형의 제조방법 및 이의 용도 Download PDF

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KR20180041748A
KR20180041748A KR1020187008548A KR20187008548A KR20180041748A KR 20180041748 A KR20180041748 A KR 20180041748A KR 1020187008548 A KR1020187008548 A KR 1020187008548A KR 20187008548 A KR20187008548 A KR 20187008548A KR 20180041748 A KR20180041748 A KR 20180041748A
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compound
crystalline form
crystalline
group
diffraction pattern
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헤샹 왕
창유 조우
보 렌
시안자오 광
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베이진 엘티디
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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)
  • 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)
KR1020187008548A 2015-08-25 2016-08-22 Parp 억제제, 결정형의 제조방법 및 이의 용도 Ceased KR20180041748A (ko)

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

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KR20180041748A true KR20180041748A (ko) 2018-04-24

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KR1020187008548A Ceased KR20180041748A (ko) 2015-08-25 2016-08-22 Parp 억제제, 결정형의 제조방법 및 이의 용도

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US (1) US10457680B2 (enExample)
EP (1) EP3341375B1 (enExample)
JP (1) JP6940039B2 (enExample)
KR (1) KR20180041748A (enExample)
CN (2) CN107922425B (enExample)
AU (1) AU2016312011B2 (enExample)
BR (1) BR112018003634B1 (enExample)
CA (1) CA2994895A1 (enExample)
EA (1) EA037366B1 (enExample)
IL (2) IL257442B2 (enExample)
MX (1) MX385450B (enExample)
NZ (1) NZ739876A (enExample)
TW (1) TWI736550B (enExample)
WO (1) WO2017032289A1 (enExample)
ZA (1) ZA201800765B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USD926356S1 (en) * 2019-03-14 2021-07-27 Tuanfang Liu Battery for electronic cigarette

Families Citing this family (29)

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RS56616B1 (sr) 2011-12-31 2018-02-28 Beigene Ltd Kondenzovani tetra ili penta-ciklični dihidrodiazepinokarbazoloni kao parp inhibitori
CN107922425B (zh) 2015-08-25 2021-06-01 百济神州有限公司 制备parp抑制剂、结晶形式的方法及其用途
US11202782B2 (en) * 2016-09-27 2021-12-21 Beigene, Ltd. Treatment cancers using a 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
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
AU2019268583B2 (en) 2018-05-18 2022-01-27 Novartis Ag Crystalline forms of a TLR7/TLR8 inhibitor
AU2019275722A1 (en) * 2018-06-01 2020-11-12 Beigene, Ltd. Maintenance therapy of a PARP inhibitor in treating gastric cancer
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
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
WO2020239097A1 (zh) * 2019-05-31 2020-12-03 百济神州有限公司 一种parp抑制剂微丸制剂及其制备工艺
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
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
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
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors

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HRP20010573B1 (en) 1999-01-11 2006-04-30 Agouron Pharmaceuticals Tricyclic inhibitors of poly(adp-ribose) polymerases
DE60142921D1 (de) * 2000-12-01 2010-10-07 Eisai Inc Azaphenanthridone-derivate und deren verwendung als parp-inhibitoren
DK1585749T3 (da) * 2003-01-09 2008-09-22 Pfizer Diazepinoindol-derivater som kinaseinhibitorer
EP2767537B1 (en) 2008-08-06 2017-04-12 Medivation Technologies, Inc. Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP)
RS56616B1 (sr) * 2011-12-31 2018-02-28 Beigene Ltd Kondenzovani tetra ili penta-ciklični dihidrodiazepinokarbazoloni kao parp inhibitori
JP6623353B2 (ja) 2013-09-13 2019-12-25 ベイジーン スウィッツァーランド ゲーエムベーハー 抗ｐｄ−１抗体並びにその治療及び診断のための使用
KR102003754B1 (ko) 2014-07-03 2019-07-25 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
CN107922425B (zh) 2015-08-25 2021-06-01 百济神州有限公司 制备parp抑制剂、结晶形式的方法及其用途
US11202782B2 (en) * 2016-09-27 2021-12-21 Beigene, Ltd. Treatment cancers using a 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
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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USD926356S1 (en) * 2019-03-14 2021-07-27 Tuanfang Liu Battery for electronic cigarette

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Publication number Publication date
CN107922425A (zh) 2018-04-17
ZA201800765B (en) 2019-10-30
MX385450B (es) 2025-03-18
CN112521390A (zh) 2021-03-19
US20190177325A1 (en) 2019-06-13
IL296835A (en) 2022-11-01
CN107922425B (zh) 2021-06-01
EP3341375B1 (en) 2022-04-13
BR112018003634A8 (pt) 2023-01-17
JP6940039B2 (ja) 2021-09-22
IL257442A (en) 2018-04-30
CA2994895A1 (en) 2017-03-02
BR112018003634A2 (en) 2018-11-21
EP3341375A4 (en) 2019-01-16
IL257442B2 (en) 2023-03-01
AU2016312011A1 (en) 2018-03-08
WO2017032289A1 (en) 2017-03-02
BR112018003634B1 (pt) 2023-11-21
JP2018528199A (ja) 2018-09-27
EP3341375A1 (en) 2018-07-04
AU2016312011B2 (en) 2021-02-04
IL257442B (en) 2022-11-01
TW201718586A (zh) 2017-06-01
EA037366B1 (ru) 2021-03-18
MX2018002322A (es) 2018-04-11
TWI736550B (zh) 2021-08-21
US10457680B2 (en) 2019-10-29
EA201890547A1 (ru) 2018-07-31
NZ739876A (en) 2022-09-30

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