CA2683695C - 3-amido-pyrrolo[3,4-c]pyrazole-5(1h,4h,6h) carbaldehyde derivatives - Google Patents

3-amido-pyrrolo[3,4-c]pyrazole-5(1h,4h,6h) carbaldehyde derivatives Download PDF

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Publication number
CA2683695C
CA2683695C CA2683695A CA2683695A CA2683695C CA 2683695 C CA2683695 C CA 2683695C CA 2683695 A CA2683695 A CA 2683695A CA 2683695 A CA2683695 A CA 2683695A CA 2683695 C CA2683695 C CA 2683695C
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Prior art keywords
pyrazol
tetrahydropyrrolo
pharmaceutically acceptable
compound
acceptable salt
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CA2683695A
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English (en)
French (fr)
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CA2683695A1 (en
Inventor
Iriny Botrous
Yufeng Hong
Hui Li
Kevin Kun-Chin Liu
Seiji Nukui
Min Teng
Eileen Valenzuela Tompkins
Chunfeng Yin
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Pfizer Inc
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Pfizer 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2683695A 2007-04-12 2008-04-10 3-amido-pyrrolo[3,4-c]pyrazole-5(1h,4h,6h) carbaldehyde derivatives Active CA2683695C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US91146207P 2007-04-12 2007-04-12
US60/911,462 2007-04-12
US3551908P 2008-03-11 2008-03-11
US61/035,519 2008-03-11
US4011508P 2008-03-27 2008-03-27
US61/040,115 2008-03-27
PCT/IB2008/000862 WO2008125945A2 (en) 2007-04-12 2008-04-10 3-amido-pyrrolo [3, 4-c] pyrazole-5 (1h, 4h, 6h) carbaldehyde derivatives as inhibitors of protein kinase c

Publications (2)

Publication Number Publication Date
CA2683695A1 CA2683695A1 (en) 2008-10-23
CA2683695C true CA2683695C (en) 2013-06-18

Family

ID=39764996

Family Applications (1)

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CA2683695A Active CA2683695C (en) 2007-04-12 2008-04-10 3-amido-pyrrolo[3,4-c]pyrazole-5(1h,4h,6h) carbaldehyde derivatives

Country Status (11)

Country Link
US (2) US8114871B2 (https=)
EP (1) EP2195321B1 (https=)
JP (1) JP5404601B2 (https=)
KR (1) KR101113387B1 (https=)
CN (3) CN104356136A (https=)
AU (1) AU2008237660B2 (https=)
CA (1) CA2683695C (https=)
HK (1) HK1207067A1 (https=)
IL (1) IL201104A (https=)
MX (1) MX2009010951A (https=)
WO (1) WO2008125945A2 (https=)

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JP5435592B2 (ja) 2008-05-28 2014-03-05 ファイザー・インク ピラゾロスピロケトンアセチルCoAカルボキシラーゼ阻害剤
WO2011044264A2 (en) * 2009-10-06 2011-04-14 Afraxis, Inc. Pyrrolopyrazoles for treating cns disorders
EP2947082A1 (en) 2009-11-10 2015-11-25 Pfizer Inc N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
HRP20161178T1 (hr) 2010-09-30 2016-11-04 Pfizer Inc. N1-PIRAZOLOSPIROKETONSKI INHIBITORI ACETIL-CoA-KARBOKSILAZE
ES2546465T3 (es) 2010-10-29 2015-09-23 Pfizer Inc Inhibidores de N1/N2-lactama acetil-CoA carboxilasa
US8841463B2 (en) 2011-02-11 2014-09-23 Glaxosmithkline Intellectual Property Development Limited Cathepsin C inhibitors
AU2012245996B2 (en) 2011-04-22 2016-09-01 Pfizer Inc. Pyrazolospiroketone derivatives for use as acetyl-CoA carboxylase inhibitors
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US8846712B2 (en) 2011-09-12 2014-09-30 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
ES2882807T3 (es) * 2011-09-16 2021-12-02 Novartis Ag Heterociclil carboxamidas N-sustituidas
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
WO2013167403A1 (en) 2012-05-09 2013-11-14 Sanofi Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US20140206667A1 (en) 2012-11-14 2014-07-24 Michela Gallagher Methods and compositions for treating schizophrenia
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3145931B1 (en) 2014-05-23 2021-03-31 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
CA2966164C (en) 2014-10-31 2023-10-17 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole compound
NZ730759A (en) * 2014-11-21 2018-10-26 Lilly Co Eli 1,2-benzothiazole compounds for the treatment of kidney disorders
JP6854762B2 (ja) * 2014-12-23 2021-04-07 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の阻害剤
USRE50776E1 (en) 2015-03-27 2026-02-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
MX394157B (es) 2015-06-15 2025-03-24 Ube Corp Derivado de dihidropirrolopirazol sustituido.
AU2016319125B2 (en) 2015-09-09 2021-04-08 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2016355303B2 (en) 2015-11-20 2021-10-07 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
AU2017295858A1 (en) 2016-07-14 2019-01-24 Mingsight Pharmaceuticals, Inc. Treatment of cancer
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EP3885347B1 (en) 2018-11-14 2023-11-22 UBE Corporation Dihydropyrrolopyrazole derivative
US12281126B2 (en) 2018-12-28 2025-04-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
CN119684220A (zh) * 2024-12-13 2025-03-25 江苏宝众宝达药业股份有限公司 一种(2r,5r)-1,2,5-三甲基哌嗪的制备方法

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Also Published As

Publication number Publication date
MX2009010951A (es) 2009-10-29
CN104370914A (zh) 2015-02-25
KR20090130039A (ko) 2009-12-17
EP2195321B1 (en) 2016-10-19
AU2008237660A1 (en) 2008-10-23
US8114871B2 (en) 2012-02-14
IL201104A0 (en) 2010-05-17
US20100249128A1 (en) 2010-09-30
KR101113387B1 (ko) 2012-04-23
WO2008125945A2 (en) 2008-10-23
CN104356136A (zh) 2015-02-18
CA2683695A1 (en) 2008-10-23
CN101675052A (zh) 2010-03-17
WO2008125945A3 (en) 2009-03-12
HK1207067A1 (en) 2016-01-22
AU2008237660B2 (en) 2011-12-22
JP2010523643A (ja) 2010-07-15
US20120108588A1 (en) 2012-05-03
IL201104A (en) 2017-09-28
US8999981B2 (en) 2015-04-07
CN104370914B (zh) 2018-09-07
HK1207068A1 (en) 2016-01-22
EP2195321A2 (en) 2010-06-16
JP5404601B2 (ja) 2014-02-05

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