CN103703004B - 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 - Google Patents

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 Download PDF

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CN103703004B
CN103703004B CN201180072418.8A CN201180072418A CN103703004B CN 103703004 B CN103703004 B CN 103703004B CN 201180072418 A CN201180072418 A CN 201180072418A CN 103703004 B CN103703004 B CN 103703004B
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CN103703004A (zh
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周昌友
任博
王鹤翔
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Baiji Shenzhou Suzhou Biotechnology Co ltd
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Beigene Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06Peri-condensed 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
    • A61K31/55Heterocyclic 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • C07D471/16Peri-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
    • C07D471/22Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201180072418.8A 2011-12-31 2011-12-31 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 Active CN103703004B (zh)

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CN201610603192.4A CN106220635B (zh) 2011-12-31 2011-12-31 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

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PCT/CN2011/085148 WO2013097225A1 (en) 2011-12-31 2011-12-31 Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors

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CN103703004B true CN103703004B (zh) 2016-06-29

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CN201610603192.4A Active CN106220635B (zh) 2011-12-31 2011-12-31 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

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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
CN106883232B (zh) 2017-03-31 2019-01-22 苏州康润医药有限公司 一种氮杂非那烯-3-酮的衍生物及其制备方法与应用
WO2019015561A1 (en) * 2017-07-17 2019-01-24 Beigene, Ltd. TREATMENT OF CANCERS USING A COMBINATION COMPRISING INHIBITORS OF PARP, TEMOZOLOMIDE AND / OR RADIOTHERAPY
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
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
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
KR20220016028A (ko) * 2019-05-31 2022-02-08 베이진 엘티디 Parp 억제제 펠릿 제조 및 이의 제조방법
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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
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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
WO2019015561A1 (en) 2017-07-17 2019-01-24 Beigene, Ltd. TREATMENT OF CANCERS USING A COMBINATION COMPRISING INHIBITORS OF PARP, TEMOZOLOMIDE AND / OR RADIOTHERAPY

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WO2002044183A2 (en) * 2000-12-01 2002-06-06 Guilford Pharmaceuticals Inc. Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors
CN1759118A (zh) * 2003-01-09 2006-04-12 美国辉瑞有限公司 作为激酶抑制剂的二氮杂䓬并吲哚衍生物
WO2010017055A2 (en) * 2008-08-06 2010-02-11 Lead Therapeutics, Inc. Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp)

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CA2856309A1 (en) 2013-07-04
NO2797921T3 (enExample) 2018-02-03
US10112952B2 (en) 2018-10-30
EP2797921B1 (en) 2017-09-06
PT2797921T (pt) 2017-11-14
EA027533B1 (ru) 2017-08-31
BR112014012628B1 (pt) 2021-02-09
CA2856309C (en) 2016-06-07
PL2797921T3 (pl) 2018-02-28
ME02855B (me) 2018-04-20
CN106220635A (zh) 2016-12-14
EP3315500B1 (en) 2020-03-18
CN103703004A (zh) 2014-04-02
HK1192233A1 (zh) 2014-08-15
SI2797921T1 (en) 2018-01-31
IL233365A0 (en) 2014-08-31
EP3315500A1 (en) 2018-05-02
DK2797921T3 (en) 2017-10-02
ZA201405560B (en) 2017-02-22
SG11201401726VA (en) 2014-10-30
US10501467B2 (en) 2019-12-10
IN2014DN06169A (enExample) 2015-08-21
EA201491303A1 (ru) 2014-10-30
CN106220635B (zh) 2019-03-08
US20160159811A1 (en) 2016-06-09
LT2797921T (lt) 2017-11-27
EP2797921A4 (en) 2015-10-21
HUE035153T2 (en) 2018-05-02
ES2645814T3 (es) 2017-12-07
BR112014012628A2 (pt) 2017-06-13
US20190016731A1 (en) 2019-01-17
US9260440B2 (en) 2016-02-16
US9617273B2 (en) 2017-04-11
BR112014012628B8 (pt) 2023-01-17
CY1119804T1 (el) 2018-06-27
HRP20171883T1 (hr) 2018-01-12
SMT201700543T1 (it) 2018-01-11
MX2014007840A (es) 2014-08-21
AU2011384858B2 (en) 2016-05-05
KR101716012B1 (ko) 2017-03-13
IL233365A (en) 2016-08-31
US20150175617A1 (en) 2015-06-25
AU2011384858A1 (en) 2014-05-29
JP6034877B2 (ja) 2016-11-30
US20170305921A1 (en) 2017-10-26
KR20140107353A (ko) 2014-09-04
MX353578B (es) 2018-01-19
WO2013097225A1 (en) 2013-07-04
EP2797921A1 (en) 2014-11-05
JP2015503526A (ja) 2015-02-02
NZ624063A (en) 2016-09-30
RS56616B1 (sr) 2018-02-28

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