AU2011384858B2 - Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors - Google Patents

Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors Download PDF

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Publication number
AU2011384858B2
AU2011384858B2 AU2011384858A AU2011384858A AU2011384858B2 AU 2011384858 B2 AU2011384858 B2 AU 2011384858B2 AU 2011384858 A AU2011384858 A AU 2011384858A AU 2011384858 A AU2011384858 A AU 2011384858A AU 2011384858 B2 AU2011384858 B2 AU 2011384858B2
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alkyl
aryl
cycloalkyl
heterocyclyl
heteroaryl
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AU2011384858A1 (en
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Bo REN
Hexiang Wang
Changyou Zhou
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BeOne Medicines 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)
AU2011384858A 2011-12-31 2011-12-31 Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors Ceased AU2011384858B2 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2011/085148 WO2013097225A1 (en) 2011-12-31 2011-12-31 Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors

Publications (2)

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AU2011384858A1 AU2011384858A1 (en) 2014-05-29
AU2011384858B2 true AU2011384858B2 (en) 2016-05-05

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AU2011384858A Ceased AU2011384858B2 (en) 2011-12-31 2011-12-31 Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors

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US (4) US9260440B2 (enEXAMPLES)
EP (2) EP3315500B1 (enEXAMPLES)
JP (1) JP6034877B2 (enEXAMPLES)
KR (1) KR101716012B1 (enEXAMPLES)
CN (2) CN106220635B (enEXAMPLES)
AU (1) AU2011384858B2 (enEXAMPLES)
BR (1) BR112014012628B8 (enEXAMPLES)
CA (1) CA2856309C (enEXAMPLES)
CY (1) CY1119804T1 (enEXAMPLES)
DK (1) DK2797921T3 (enEXAMPLES)
EA (1) EA027533B1 (enEXAMPLES)
ES (1) ES2645814T3 (enEXAMPLES)
HR (1) HRP20171883T1 (enEXAMPLES)
HU (1) HUE035153T2 (enEXAMPLES)
IL (1) IL233365A (enEXAMPLES)
IN (1) IN2014DN06169A (enEXAMPLES)
LT (1) LT2797921T (enEXAMPLES)
ME (1) ME02855B (enEXAMPLES)
MX (1) MX353578B (enEXAMPLES)
NO (1) NO2797921T3 (enEXAMPLES)
NZ (1) NZ624063A (enEXAMPLES)
PL (1) PL2797921T3 (enEXAMPLES)
PT (1) PT2797921T (enEXAMPLES)
RS (1) RS56616B1 (enEXAMPLES)
SG (1) SG11201401726VA (enEXAMPLES)
SI (1) SI2797921T1 (enEXAMPLES)
SM (1) SMT201700543T1 (enEXAMPLES)
WO (1) WO2013097225A1 (enEXAMPLES)
ZA (1) ZA201405560B (enEXAMPLES)

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AU2011384858B2 (en) 2011-12-31 2016-05-05 Beigene, Ltd. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors
DK2822656T3 (en) 2012-03-07 2017-01-30 Inst Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
CA2922469A1 (en) 2013-09-11 2015-03-19 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
IL296835A (en) * 2015-08-25 2022-11-01 Beigene Ltd Process for preparing parp inhibitor, crystalline forms, and uses thereof
AU2017242027B2 (en) 2016-04-01 2020-10-08 Recurium Ip Holdings, Llc Estrogen receptor modulators
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
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
US20200155567A1 (en) * 2017-07-17 2020-05-21 Beigene, Ltd. Treatment of cancers using a combination comprising parp inhibitors, temozolomide and/or radiation therapy
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
MX2021014339A (es) * 2019-05-31 2022-01-06 Beigene Ltd Preparacion de granulo inhibidor de parp y proceso de preparacion del mismo.
KR20220044528A (ko) 2019-08-06 2022-04-08 리커리엄 아이피 홀딩스, 엘엘씨 돌연변이체를 치료하기 위한 에스트로겐 수용체 조절제
WO2021046014A1 (en) 2019-09-03 2021-03-11 Teva Czech Industries S.R.O Solid state forms of pamiparib and process for preparation thereof
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
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of 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

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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
WO2004063198A1 (en) * 2003-01-09 2004-07-29 Pfizer Inc. Diazepinoindole derivatives as kinase inhibitors
WO2010017055A2 (en) * 2008-08-06 2010-02-11 Lead Therapeutics, Inc. Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp)

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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
US20200155567A1 (en) 2017-07-17 2020-05-21 Beigene, Ltd. Treatment of cancers using a combination comprising parp inhibitors, temozolomide and/or radiation therapy

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Publication number Priority date Publication date Assignee Title
WO2002044183A2 (en) * 2000-12-01 2002-06-06 Guilford Pharmaceuticals Inc. Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors
WO2004063198A1 (en) * 2003-01-09 2004-07-29 Pfizer Inc. Diazepinoindole derivatives as kinase inhibitors
WO2010017055A2 (en) * 2008-08-06 2010-02-11 Lead Therapeutics, Inc. Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp)

Also Published As

Publication number Publication date
HK1192233A1 (zh) 2014-08-15
EP2797921A1 (en) 2014-11-05
CN103703004B (zh) 2016-06-29
US20170305921A1 (en) 2017-10-26
CN103703004A (zh) 2014-04-02
CN106220635A (zh) 2016-12-14
US20190016731A1 (en) 2019-01-17
PL2797921T3 (pl) 2018-02-28
BR112014012628B1 (pt) 2021-02-09
EP2797921A4 (en) 2015-10-21
EA201491303A1 (ru) 2014-10-30
MX353578B (es) 2018-01-19
CA2856309C (en) 2016-06-07
RS56616B1 (sr) 2018-02-28
EP2797921B1 (en) 2017-09-06
NO2797921T3 (enEXAMPLES) 2018-02-03
PT2797921T (pt) 2017-11-14
EA027533B1 (ru) 2017-08-31
US20150175617A1 (en) 2015-06-25
BR112014012628B8 (pt) 2023-01-17
SG11201401726VA (en) 2014-10-30
JP6034877B2 (ja) 2016-11-30
US9617273B2 (en) 2017-04-11
US10112952B2 (en) 2018-10-30
HUE035153T2 (en) 2018-05-02
EP3315500B1 (en) 2020-03-18
SI2797921T1 (en) 2018-01-31
HRP20171883T1 (hr) 2018-01-12
WO2013097225A1 (en) 2013-07-04
JP2015503526A (ja) 2015-02-02
ME02855B (me) 2018-04-20
MX2014007840A (es) 2014-08-21
US20160159811A1 (en) 2016-06-09
BR112014012628A2 (pt) 2017-06-13
KR101716012B1 (ko) 2017-03-13
CN106220635B (zh) 2019-03-08
US10501467B2 (en) 2019-12-10
SMT201700543T1 (it) 2018-01-11
CY1119804T1 (el) 2018-06-27
CA2856309A1 (en) 2013-07-04
AU2011384858A1 (en) 2014-05-29
IN2014DN06169A (enEXAMPLES) 2015-08-21
DK2797921T3 (en) 2017-10-02
NZ624063A (en) 2016-09-30
EP3315500A1 (en) 2018-05-02
LT2797921T (lt) 2017-11-27
IL233365A0 (en) 2014-08-31
KR20140107353A (ko) 2014-09-04
ES2645814T3 (es) 2017-12-07
IL233365A (en) 2016-08-31
US9260440B2 (en) 2016-02-16
ZA201405560B (en) 2017-02-22

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