SI2797921T1 - Condensed tetra- or pentacyclic dihydrodiazepinocarbazolones as PARP inhibitors - Google Patents

Condensed tetra- or pentacyclic dihydrodiazepinocarbazolones as PARP inhibitors Download PDF

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Publication number
SI2797921T1
SI2797921T1 SI201131351T SI201131351T SI2797921T1 SI 2797921 T1 SI2797921 T1 SI 2797921T1 SI 201131351 T SI201131351 T SI 201131351T SI 201131351 T SI201131351 T SI 201131351T SI 2797921 T1 SI2797921 T1 SI 2797921T1
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Slovenia
Prior art keywords
heteroaryl
alkyl
heterocyclyl
cycloalkyl
aryl
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SI201131351T
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English (en)
Slovenian (sl)
Inventor
Changyou Zhou
Bo Ren
Hexiang Wang
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Beigene, Ltd.
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Publication date
Application filed by Beigene, Ltd. filed Critical Beigene, Ltd.
Publication of SI2797921T1 publication Critical patent/SI2797921T1/en

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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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (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)
SI201131351T 2011-12-31 2011-12-31 Condensed tetra- or pentacyclic dihydrodiazepinocarbazolones as PARP inhibitors SI2797921T1 (en)

Applications Claiming Priority (2)

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
EP11878508.8A EP2797921B1 (en) 2011-12-31 2011-12-31 Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors

Publications (1)

Publication Number Publication Date
SI2797921T1 true SI2797921T1 (en) 2018-01-31

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SI201131351T SI2797921T1 (en) 2011-12-31 2011-12-31 Condensed tetra- or pentacyclic dihydrodiazepinocarbazolones as PARP inhibitors

Country Status (29)

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US (4) US9260440B2 (enExample)
EP (2) EP2797921B1 (enExample)
JP (1) JP6034877B2 (enExample)
KR (1) KR101716012B1 (enExample)
CN (2) CN103703004B (enExample)
AU (1) AU2011384858B2 (enExample)
BR (1) BR112014012628B8 (enExample)
CA (1) CA2856309C (enExample)
CY (1) CY1119804T1 (enExample)
DK (1) DK2797921T3 (enExample)
EA (1) EA027533B1 (enExample)
ES (1) ES2645814T3 (enExample)
HR (1) HRP20171883T1 (enExample)
HU (1) HUE035153T2 (enExample)
IL (1) IL233365A (enExample)
IN (1) IN2014DN06169A (enExample)
LT (1) LT2797921T (enExample)
ME (1) ME02855B (enExample)
MX (1) MX353578B (enExample)
NO (1) NO2797921T3 (enExample)
NZ (1) NZ624063A (enExample)
PL (1) PL2797921T3 (enExample)
PT (1) PT2797921T (enExample)
RS (1) RS56616B1 (enExample)
SG (1) SG11201401726VA (enExample)
SI (1) SI2797921T1 (enExample)
SM (1) SMT201700543T1 (enExample)
WO (1) WO2013097225A1 (enExample)
ZA (1) ZA201405560B (enExample)

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RS56616B1 (sr) 2011-12-31 2018-02-28 Beigene Ltd Kondenzovani tetra ili penta-ciklični dihidrodiazepinokarbazoloni kao parp inhibitori
EP2822656B1 (en) 2012-03-07 2016-10-19 Institute of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
US9611223B2 (en) 2013-09-11 2017-04-04 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
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
CA3017388C (en) * 2016-04-01 2024-03-12 Zeno Royalties & Milestones, LLC Estrogen receptor modulators
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
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
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
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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
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WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
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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

Also Published As

Publication number Publication date
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
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
CN103703004B (zh) 2016-06-29
PL2797921T3 (pl) 2018-02-28
EP2797921B1 (en) 2017-09-06

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