CN1284783C - 作为p38蛋白激酶抑制剂的取代的含氮杂环 - Google Patents

作为p38蛋白激酶抑制剂的取代的含氮杂环 Download PDF

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Publication number
CN1284783C
CN1284783C CNB031587968A CN03158796A CN1284783C CN 1284783 C CN1284783 C CN 1284783C CN B031587968 A CNB031587968 A CN B031587968A CN 03158796 A CN03158796 A CN 03158796A CN 1284783 C CN1284783 C CN 1284783C
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China
Prior art keywords
compound
disease
phenyl
medicine
inhibitor
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Expired - Fee Related
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CNB031587968A
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English (en)
Chinese (zh)
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CN1519240A (zh
Inventor
G·W·比密斯
F·G·萨利图罗
J·P·杜非
J·E·科克兰
E·M·哈伦格汤
M·A·穆科
K·P·威尔森
M·苏
V·P·加鲁劳
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Priority claimed from US08/822,373 external-priority patent/US5945418A/en
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of CN1519240A publication Critical patent/CN1519240A/zh
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Publication of CN1284783C publication Critical patent/CN1284783C/zh
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    • C07ORGANIC CHEMISTRY
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    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/70Sulfur atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P23/00Anaesthetics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • 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
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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D241/12Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D471/02Heterocyclic 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 two hetero rings
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Animal Behavior & Ethology (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
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  • Virology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNB031587968A 1996-12-18 1997-12-17 作为p38蛋白激酶抑制剂的取代的含氮杂环 Expired - Fee Related CN1284783C (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US3428896P 1996-12-18 1996-12-18
US60/034,288 1996-12-18
US08/822,373 1997-03-20
US08/822,373 US5945418A (en) 1996-12-18 1997-03-20 Inhibitors of p38
US08/862,925 1997-06-10
US08/862,925 US6147080A (en) 1996-12-18 1997-06-10 Inhibitors of p38

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CNB971813825A Division CN1153770C (zh) 1996-12-18 1997-12-17 作为p38蛋白激酶抑制剂的取代的含氮杂环

Publications (2)

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CN1519240A CN1519240A (zh) 2004-08-11
CN1284783C true CN1284783C (zh) 2006-11-15

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CNB031587968A Expired - Fee Related CN1284783C (zh) 1996-12-18 1997-12-17 作为p38蛋白激酶抑制剂的取代的含氮杂环
CNB971813825A Expired - Fee Related CN1153770C (zh) 1996-12-18 1997-12-17 作为p38蛋白激酶抑制剂的取代的含氮杂环

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CNB971813825A Expired - Fee Related CN1153770C (zh) 1996-12-18 1997-12-17 作为p38蛋白激酶抑制剂的取代的含氮杂环

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US (1) US6147080A (https=)
EP (1) EP0951467B1 (https=)
JP (1) JP4171072B2 (https=)
CN (2) CN1284783C (https=)
AP (1) AP1136A (https=)
AT (1) ATE236165T1 (https=)
AU (1) AU738000B2 (https=)
BG (1) BG64533B1 (https=)
BR (1) BR9714415A (https=)
CA (1) CA2274825C (https=)
CZ (1) CZ299600B6 (https=)
DE (1) DE69720522T2 (https=)
DK (1) DK0951467T3 (https=)
EA (1) EA002855B1 (https=)
EE (1) EE04191B1 (https=)
ES (1) ES2202658T3 (https=)
HU (1) HUP0001125A3 (https=)
ID (1) ID21919A (https=)
IL (1) IL130349A0 (https=)
IS (1) IS5069A (https=)
NO (1) NO315047B1 (https=)
NZ (1) NZ336146A (https=)
PL (1) PL202464B1 (https=)
PT (1) PT951467E (https=)
SK (1) SK284578B6 (https=)
TR (1) TR199902194T2 (https=)
TW (1) TW521071B (https=)
WO (1) WO1998027098A1 (https=)

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US7091181B2 (en) 1994-12-12 2006-08-15 Omeros Corporation Method of inhibition of pain and inflammation during surgery comprising administration of soluble TNF receptors
US6608060B1 (en) 1996-12-18 2003-08-19 Vertex Pharmaceuticals Incorporated Inhibitors of p38
WO1999019471A1 (en) 1997-10-16 1999-04-22 Board Of Regents, The University Of Texas System Models and treatments for cardiac hypertrophy in relation with nf-at3 function
WO1999032121A1 (en) 1997-12-19 1999-07-01 Smithkline Beecham Corporation Compounds of heteroaryl substituted imidazole, their pharmaceutical compositions and uses
MY132496A (en) * 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
WO1999061039A2 (en) * 1998-05-22 1999-12-02 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Novel composition for modulating ischemic cell death
US6858617B2 (en) 1998-05-26 2005-02-22 Smithkline Beecham Corporation Substituted imidazole compounds
EP1277740A1 (en) * 1998-06-12 2003-01-22 Vertex Pharmaceuticals Incorporated Inhibitors of p38
JP2002517486A (ja) 1998-06-12 2002-06-18 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 p38のインヒビター
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
WO2000017175A1 (en) * 1998-09-18 2000-03-30 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
AR023659A1 (es) 1998-09-18 2002-09-04 Vertex Pharma Un compuesto inhibidor de p38, una composicion farmaceutica que lo comprende y el uso de dicha composicion en el tratamiento y prevencion de estados patologicos
AU1127700A (en) * 1998-10-20 2000-05-08 Omeros Medical Systems, Inc. Irrigation solution containing mapk inhibitors and their use for treating pain and inflammation
WO2000025791A1 (en) 1998-11-04 2000-05-11 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
UA73492C2 (en) * 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
MXPA01008440A (es) 1999-02-22 2002-04-24 Boehringer Ingelheim Pharma Derivados heterociclicos policiclos como agentes anti-inflamatorios..
NZ528846A (en) 1999-03-12 2005-05-27 Boehringer Ingelheim Pharma Compounds useful as anti-inflammatory agents
WO2000055152A1 (en) 1999-03-12 2000-09-21 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
JP2000281588A (ja) * 1999-03-30 2000-10-10 Sankyo Co Ltd ガンの予防又は治療薬及びそのスクリーニング方法
WO2001001986A1 (en) * 1999-07-02 2001-01-11 Lipton Stuart A Method of reducing neuronal injury or apoptosis
ATE312823T1 (de) 1999-07-09 2005-12-15 Boehringer Ingelheim Pharma Verfahren zur herstellung heteroarylsubstituierter ureaverbindungen
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