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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Beone Pharmaceutical Suzhou 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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)

Priority Applications (1)

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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

Applications Claiming Priority (1)

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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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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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US (4) US9260440B2 (enExample)
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WO (1) WO2013097225A1 (enExample)
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CA3017388C (en) * 2016-04-01 2024-03-12 Zeno Royalties & Milestones, LLC Estrogen receptor modulators
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US10899763B2 (en) 2017-02-28 2021-01-26 Beigene, Ltd. Crystalline forms of salts of fused penta-cyclic dihydrodiazepinocarbazolones, and uses thereof
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
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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
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
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
US11278532B2 (en) 2019-08-06 2022-03-22 Recurium Ip Holdings, Llc Estrogen receptor modulators for treating mutants
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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

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

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Patentee before: BEIGENE, Ltd.

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