ES2754590T3 - An¿¢logos de compuestos de 4h-pirazolo[1,5-¿A]bencimidazol como inhibidores de las PARP - Google Patents

An¿¢logos de compuestos de 4h-pirazolo[1,5-¿A]bencimidazol como inhibidores de las PARP Download PDF

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Publication number
ES2754590T3
ES2754590T3 ES15777444T ES15777444T ES2754590T3 ES 2754590 T3 ES2754590 T3 ES 2754590T3 ES 15777444 T ES15777444 T ES 15777444T ES 15777444 T ES15777444 T ES 15777444T ES 2754590 T3 ES2754590 T3 ES 2754590T3
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Prior art keywords
fluoro
benzo
imidazo
carboxamide
pyrazol
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Active
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ES15777444T
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English (en)
Spanish (es)
Inventor
Zhaozhong Ding
Shuhui Chen
Gang Li
Cailin Wang
Zhibo Zhang
Ronghua Tu
Yang Yue
Hailiang Chen
Wenjie Sun
Lu Huang
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Hubei Bio Pharmaceutical Industrial Tech Institute Inc
HUMANWELL HEALTHCARE GROUP CO Ltd
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Hubei Bio Pharmaceutical Industrial Tech Institute Inc
HUMANWELL HEALTHCARE GROUP CO Ltd
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Priority claimed from CN201410144173.0A external-priority patent/CN104974161B/zh
Application filed by Hubei Bio Pharmaceutical Industrial Tech Institute Inc, HUMANWELL HEALTHCARE GROUP CO Ltd filed Critical Hubei Bio Pharmaceutical Industrial Tech Institute Inc
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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
    • C07D487/04Ortho-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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/424Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
ES15777444T 2014-04-10 2015-03-30 An¿¢logos de compuestos de 4h-pirazolo[1,5-¿A]bencimidazol como inhibidores de las PARP Active ES2754590T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201410144173.0A CN104974161B (zh) 2014-04-10 2014-04-10 作为PARP抑制剂的4H-吡唑并[1,5-α]苯并咪唑化合物的类似物
CN201510113090 2015-03-13
PCT/CN2015/075363 WO2015154630A1 (zh) 2014-04-10 2015-03-30 作为PARP抑制剂的4H-吡唑并[1,5-α]苯并咪唑化合物的类似物

Publications (1)

Publication Number Publication Date
ES2754590T3 true ES2754590T3 (es) 2020-04-20

Family

ID=54287319

Family Applications (1)

Application Number Title Priority Date Filing Date
ES15777444T Active ES2754590T3 (es) 2014-04-10 2015-03-30 An¿¢logos de compuestos de 4h-pirazolo[1,5-¿A]bencimidazol como inhibidores de las PARP

Country Status (22)

Country Link
US (1) US9856262B2 (en:Method)
EP (1) EP3130592B1 (en:Method)
JP (1) JP6359175B2 (en:Method)
KR (1) KR101921486B1 (en:Method)
CN (1) CN106459057B (en:Method)
AU (1) AU2015245786B2 (en:Method)
BR (1) BR112016023397B1 (en:Method)
CA (1) CA2944801C (en:Method)
DK (1) DK3130592T3 (en:Method)
ES (1) ES2754590T3 (en:Method)
HU (1) HUE047410T2 (en:Method)
IL (1) IL248258B (en:Method)
MX (1) MX368496B (en:Method)
NZ (1) NZ725165A (en:Method)
PL (1) PL3130592T3 (en:Method)
PT (1) PT3130592T (en:Method)
RU (1) RU2672722C2 (en:Method)
SA (1) SA516380051B1 (en:Method)
SG (1) SG11201608438YA (en:Method)
TW (1) TWI671301B (en:Method)
WO (1) WO2015154630A1 (en:Method)
ZA (1) ZA201607736B (en:Method)

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CN104974161B (zh) * 2014-04-10 2019-11-01 湖北生物医药产业技术研究院有限公司 作为PARP抑制剂的4H-吡唑并[1,5-α]苯并咪唑化合物的类似物
AU2016333293B2 (en) * 2015-09-30 2020-07-30 Hubei Bio-Pharmaceutical Industrial Technological Institute Inc. Salt type and crystal type of 4H-pyrazolo (1, 5-alpha) benzimidazole compound and preparation method and intermediate thereof
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
ES2998110T3 (en) 2017-04-27 2025-02-19 Elanco Animal Health Gmbh New bicyclic pyrazole derivatives
CN115028641B (zh) * 2022-07-19 2024-05-28 湖南大学 一种钴催化合成5,8-双官能团取代咪唑并[1,2-a]吡嗪类化合物的方法
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
WO2025056690A1 (en) 2023-09-12 2025-03-20 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Parp1- and immune-checkpoint inhibitors for the treatment of cancer patients overexpressing ubqln1 and/or ubqln4
CN116969954B (zh) * 2023-09-21 2023-11-28 广东省农业科学院农业质量标准与监测技术研究所 一类含内酰胺的三环稠合杂环化合物及其应用
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
CN117534677B (zh) * 2024-01-09 2024-03-12 广东省农业科学院农业质量标准与监测技术研究所 一类含亚胺的三环稠合杂环化合物及其应用
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

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NZ547990A (en) * 2003-12-22 2010-04-30 Smithkline Beecham Cork Ltd CRF receptor antagonists and methods relating thereto
WO2007076127A2 (en) 2005-12-22 2007-07-05 Biogen Idec Ma Inc Condensed imidazoles or pyrazoles and their use as transforming growth factor modulators
WO2007144669A1 (en) * 2006-06-15 2007-12-21 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Pyrazolo[1,5-a]quinazolin-5(4h)-ones as inhibitors of poly(adp-ribose)polymerase (parp)
EP2069351B1 (en) * 2006-06-20 2015-10-28 AbbVie Inc. Pyrazoloquinazolinones as parp inhibitors
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DK2656843T3 (en) 2012-04-26 2015-04-20 Helmut Schickaneder Esters of bendamustine and related compounds, and medical use thereof
KR20150006873A (ko) * 2012-05-04 2015-01-19 메르크 파텐트 게엠베하 피롤로트리아지논 유도체
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Also Published As

Publication number Publication date
DK3130592T3 (da) 2019-11-04
KR101921486B1 (ko) 2018-11-26
CA2944801A1 (en) 2015-10-15
TW201620913A (zh) 2016-06-16
TWI671301B (zh) 2019-09-11
WO2015154630A1 (zh) 2015-10-15
RU2016144202A (ru) 2018-05-15
CN106459057B (zh) 2019-06-07
NZ725165A (en) 2018-04-27
ZA201607736B (en) 2017-09-27
CN106459057A (zh) 2017-02-22
HUE047410T2 (hu) 2020-04-28
MX368496B (es) 2019-10-04
CA2944801C (en) 2019-02-12
SA516380051B1 (ar) 2020-05-17
US9856262B2 (en) 2018-01-02
RU2016144202A3 (en:Method) 2018-05-15
EP3130592B1 (en) 2019-08-14
BR112016023397B1 (pt) 2022-08-16
EP3130592A4 (en) 2017-09-06
JP2017510653A (ja) 2017-04-13
US20170029430A1 (en) 2017-02-02
SG11201608438YA (en) 2016-11-29
MX2016013265A (es) 2017-05-03
AU2015245786A1 (en) 2016-11-03
JP6359175B2 (ja) 2018-07-18
PL3130592T3 (pl) 2020-05-18
BR112016023397A2 (en:Method) 2017-08-15
AU2015245786B2 (en) 2018-03-15
PT3130592T (pt) 2019-11-21
RU2672722C2 (ru) 2018-11-19
IL248258B (en) 2018-11-29
KR20170005807A (ko) 2017-01-16
EP3130592A1 (en) 2017-02-15

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