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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crystalline form
crystalline
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diffraction pattern
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헤샹 왕
창유 조우
보 렌
시안자오 광
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베이진 엘티디
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/22Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline 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)
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  • 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)

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

Cited By (1)

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USD926356S1 (en) * 2019-03-14 2021-07-27 Tuanfang Liu Battery for electronic cigarette

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IN2014DN06169A (https=) 2011-12-31 2015-08-21 Beigene Ltd
EP3341375B1 (en) 2015-08-25 2022-04-13 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
TW201840564A (zh) 2017-02-28 2018-11-16 英屬開曼群島商百濟神州有限公司 稠合的四環或五環二氫二氮呯幷哢唑酮的鹽的結晶形式及其用途
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
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
US20200155567A1 (en) * 2017-07-17 2020-05-21 Beigene, Ltd. Treatment of cancers using a combination comprising parp inhibitors, temozolomide and/or radiation therapy
JP7407740B2 (ja) 2018-05-18 2024-01-04 ノバルティス アーゲー Tlr7/tlr8阻害剤の結晶形態
WO2019228499A1 (en) * 2018-06-01 2019-12-05 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
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
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
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
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
US20250375445A1 (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
WO2026015796A1 (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
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
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EP3341375B1 (en) 2015-08-25 2022-04-13 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
TW201840564A (zh) 2017-02-28 2018-11-16 英屬開曼群島商百濟神州有限公司 稠合的四環或五環二氫二氮呯幷哢唑酮的鹽的結晶形式及其用途
US20200155567A1 (en) 2017-07-17 2020-05-21 Beigene, Ltd. Treatment of cancers using a combination comprising parp inhibitors, temozolomide and/or radiation therapy
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

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

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