CN104356136A - 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物 - Google Patents

作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物 Download PDF

Info

Publication number
CN104356136A
CN104356136A CN201410533054.4A CN201410533054A CN104356136A CN 104356136 A CN104356136 A CN 104356136A CN 201410533054 A CN201410533054 A CN 201410533054A CN 104356136 A CN104356136 A CN 104356136A
Authority
CN
China
Prior art keywords
dimethyl
compound
radical
pharmaceutically acceptable
tetrahydro
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201410533054.4A
Other languages
English (en)
Chinese (zh)
Inventor
I·伯特鲁斯
洪玉峰
李辉
K·K-C·刘
贯井齐治
滕敏
E·V·汤普金斯
尹春风
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Ltd
Original Assignee
SmithKline Beecham Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by SmithKline Beecham Ltd filed Critical SmithKline Beecham Ltd
Publication of CN104356136A publication Critical patent/CN104356136A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • 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)
CN201410533054.4A 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物 Pending CN104356136A (zh)

Applications Claiming Priority (6)

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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN200880014779A Division CN101675052A (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物

Publications (1)

Publication Number Publication Date
CN104356136A true CN104356136A (zh) 2015-02-18

Family

ID=39764996

Family Applications (3)

Application Number Title Priority Date Filing Date
CN201410533054.4A Pending CN104356136A (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
CN201410533053.XA Expired - Fee Related CN104370914B (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
CN200880014779A Pending CN101675052A (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物

Family Applications After (2)

Application Number Title Priority Date Filing Date
CN201410533053.XA Expired - Fee Related CN104370914B (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
CN200880014779A Pending CN101675052A (zh) 2007-04-12 2008-04-10 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物

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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008237660B2 (en) 2007-04-12 2011-12-22 Pfizer Inc. 3-amido-pyrrolo [3, 4-C] pyrazole-5 (1H, 4H, 6H) carbaldehyde derivatives as inhibitors of protein kinase C
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
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1447810A (zh) * 2000-08-10 2003-10-08 法玛西雅意大利公司 具有激酶抑制剂活性的二环吡唑类、其制备方法和包含它们的药物组合物
WO2004080457A1 (en) * 2003-03-11 2004-09-23 Pharmacia Italia S.P.A. Bicyclo-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
CN1726217A (zh) * 2002-12-19 2006-01-25 法玛西雅意大利公司 用作激酶抑制剂的取代的吡咯并吡唑衍生物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007506787A (ja) * 2003-09-23 2007-03-22 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとしてのピラゾロピロール誘導体
AU2005323797B2 (en) 2005-01-10 2009-07-09 Pfizer Inc. Pyrrolopyrazoles, potent kinase inhibitors
AU2008237660B2 (en) 2007-04-12 2011-12-22 Pfizer Inc. 3-amido-pyrrolo [3, 4-C] pyrazole-5 (1H, 4H, 6H) carbaldehyde derivatives as inhibitors of protein kinase C

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1447810A (zh) * 2000-08-10 2003-10-08 法玛西雅意大利公司 具有激酶抑制剂活性的二环吡唑类、其制备方法和包含它们的药物组合物
CN1726217A (zh) * 2002-12-19 2006-01-25 法玛西雅意大利公司 用作激酶抑制剂的取代的吡咯并吡唑衍生物
WO2004080457A1 (en) * 2003-03-11 2004-09-23 Pharmacia Italia S.P.A. Bicyclo-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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
CA2683695C (en) 2013-06-18
US20100249128A1 (en) 2010-09-30
KR101113387B1 (ko) 2012-04-23
WO2008125945A2 (en) 2008-10-23
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

Similar Documents

Publication Publication Date Title
CN104370914B (zh) 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
US11780853B2 (en) Substituted N-pyrimidin-4-yl-3-aminopyrrolo[3,4-C]pyrazoles as protein kinase C inhibitors
CN101646673B (zh) 作为pkc抑制剂的3-氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
HK1139662A (en) 3-amido-pyrrolo [3,4-c] pyrazole-5 (1h,4h, 6h)carbaldehyde derivatives as inhibitors of protein kinase c
HK1207068B (zh) 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c] 吡唑-5(1h, 4h, 6h)甲醛衍生物
HK1139130B (en) 3-amino-pyrrolo[3,4-c]pyrazole-5(1h, 4h, 6h) carbaldehyde derivatives as pkc inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1207067

Country of ref document: HK

RJ01 Rejection of invention patent application after publication

Application publication date: 20150218

RJ01 Rejection of invention patent application after publication
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1207067

Country of ref document: HK