CN100360499C - 抑制整联蛋白与其受体结合的丙酸衍生物 - Google Patents

抑制整联蛋白与其受体结合的丙酸衍生物 Download PDF

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Publication number
CN100360499C
CN100360499C CNB00809957XA CN00809957A CN100360499C CN 100360499 C CN100360499 C CN 100360499C CN B00809957X A CNB00809957X A CN B00809957XA CN 00809957 A CN00809957 A CN 00809957A CN 100360499 C CN100360499 C CN 100360499C
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alkyl
amino
group
aryl
compound
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Chinese (zh)
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CN1370143A (zh
Inventor
R·J·比迪格
G·W·霍兰德
J·M·卡斯尔
W·李
R·V·马克特
I·L·斯科特
C·吴
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Texas Biotechnology Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CNB00809957XA 1999-05-07 2000-05-05 抑制整联蛋白与其受体结合的丙酸衍生物 Expired - Fee Related CN100360499C (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US13296799P 1999-05-07 1999-05-07
US60/132967 1999-05-07
US17044199P 1999-12-10 1999-12-10
US60/170441 1999-12-10
PCT/US2000/012464 WO2000068188A1 (en) 1999-05-07 2000-05-05 Propanoic acid derivatives that inhibit the binding of integrins to their receptors

Publications (2)

Publication Number Publication Date
CN1370143A CN1370143A (zh) 2002-09-18
CN100360499C true CN100360499C (zh) 2008-01-09

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CNB00809957XA Expired - Fee Related CN100360499C (zh) 1999-05-07 2000-05-05 抑制整联蛋白与其受体结合的丙酸衍生物

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EP (1) EP1189881B2 (enExample)
JP (2) JP4841729B2 (enExample)
KR (1) KR100767199B1 (enExample)
CN (1) CN100360499C (enExample)
AT (1) ATE277923T1 (enExample)
AU (1) AU4826900A (enExample)
BR (1) BR0010349B1 (enExample)
CA (1) CA2373180C (enExample)
CZ (1) CZ304225B6 (enExample)
DE (1) DE60014369T3 (enExample)
ES (1) ES2228527T5 (enExample)
HK (1) HK1044533A1 (enExample)
HU (1) HU229155B1 (enExample)
IL (2) IL146312A0 (enExample)
MX (1) MXPA01011341A (enExample)
NO (1) NO329899B1 (enExample)
NZ (1) NZ515249A (enExample)
RO (1) RO121640B1 (enExample)
RU (1) RU2255933C9 (enExample)
SI (1) SI20876B (enExample)
SK (1) SK288186B6 (enExample)
TR (1) TR200103427T2 (enExample)
WO (1) WO2000068188A1 (enExample)

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US6972296B2 (en) 1999-05-07 2005-12-06 Encysive Pharmaceuticals Inc. Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
US6723711B2 (en) * 1999-05-07 2004-04-20 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
AR026748A1 (es) 1999-12-08 2003-02-26 Vertex Pharma Un compuesto inhibidor de caspasas, una composicion farmaceutica que lo comprende, un metodo para la sintesis del mismo y un compuesto intermediario paradicha sintesis
PE20020420A1 (es) * 2000-10-02 2002-06-27 Novartis Ag Derivados de diazacicloalcanodiona como antagonistas del antigeno asociado a la funcion del linfocito-1 (lfa-1)
FR2834212B1 (fr) * 2001-12-27 2004-07-09 Besins Int Belgique Utilisation d'une poudre a liberation immediate dans des compositions pharmaceutiques et nutraceutiques
RU2005102094A (ru) 2002-06-28 2006-02-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы каспазы и их применение
PL374971A1 (en) 2002-08-09 2005-11-14 Transtech Pharma, Inc. Aryl and heteroaryl compounds and methods to modulate coagulation
CA2511235A1 (en) 2002-12-20 2004-07-15 Vertex Pharmaceuticals Incorporated 4-oxo-3-(1-oxo-1h-isoquinolin-2-ylacetylamino)-pentanoic acid ester and amide derivatives and their use as caspase inhibitors
PE20050159A1 (es) 2003-05-27 2005-04-19 Vertex Pharma Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
JP2007501844A (ja) 2003-08-08 2007-02-01 トランス　テック　ファーマ，インコーポレイテッド アリール及びヘテロアリール化合物、組成物並びに使用方法
WO2005014532A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
EP1828144A2 (en) * 2004-11-12 2007-09-05 OSI Pharmaceuticals, Inc. Integrin antagonists useful as anticancer agents
US7728013B2 (en) 2005-05-10 2010-06-01 Intermune, Inc. Method of modulating stress-activated protein kinase system
US7553873B2 (en) 2005-07-11 2009-06-30 Wyeth Glutamate aggrecanase inhibitors
AU2006299918A1 (en) 2005-10-13 2007-04-19 Wyeth Methods for preparing glutamic acid derivatives
US8304413B2 (en) 2008-06-03 2012-11-06 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
WO2015153683A1 (en) 2014-04-02 2015-10-08 Intermune, Inc. Anti-fibrotic pyridinones
US10875875B2 (en) * 2017-04-26 2020-12-29 Aviara Pharmaceuticals, Inc. Propionic acid derivatives and methods of use thereof
TWI856956B (zh) 2018-04-12 2024-10-01 美商莫菲克醫療股份有限公司 人類整合素α４β７拮抗劑
CN115087444B (zh) * 2019-10-16 2024-09-17 莫菲克医疗股份有限公司 抑制人整联蛋白α4β7
WO2023134698A1 (zh) * 2022-01-11 2023-07-20 深圳信立泰药业股份有限公司 一种哒嗪-1(6h)-6-氧代类化合物及其制备方法与应用
CN121127462A (zh) * 2023-05-17 2025-12-12 西藏海思科制药有限公司 一种羧基衍生物及其在医药上的应用

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US5847135A (en) * 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme

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US5874424A (en) * 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
GR851819B (enExample) * 1984-08-17 1985-11-26 Wyeth John & Brother Ltd
HUT68769A (en) * 1991-05-07 1995-07-28 Merck & Co Inc FIBRINOGéN RECEPTOR ANTAGONIST COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AS EFFECTIVE SUBSTANCE
EP0761680A3 (en) * 1995-09-12 1999-05-06 Ono Pharmaceutical Co., Ltd. Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity
IL128221A (en) * 1996-07-25 2003-12-10 Biogen Inc Cell adhesion inhibitors
JP2002511052A (ja) * 1996-08-29 2002-04-09 メルク エンド カンパニー インコーポレーテッド インテグリンアンタゴニスト
EP0932598A1 (en) * 1996-10-11 1999-08-04 Warner-Lambert Company ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME
DE19647380A1 (de) * 1996-11-15 1998-05-20 Hoechst Ag 5-Ring-Heterocyclen als Inhibitoren der Leukozytenadhäsion und VLA-4-Antagonisten
AR016751A1 (es) * 1996-11-22 2001-08-01 Athena Neurosciences Inc Metodo para inhibir la liberacion del peptido beta-amiloide en una celula, composicion farmaceutica y compuestos utiles en dicho metodo
DE69823178T2 (de) * 1997-05-02 2005-06-23 Akzo Nobel N.V. Serine protease inhibitoren
DE19741235A1 (de) * 1997-09-18 1999-03-25 Hoechst Marion Roussel De Gmbh Neue Imidazolidinderivate, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
US6331640B1 (en) * 1998-10-13 2001-12-18 Hoffmann-La Roche Inc. Diaminopropionic acid derivatives
WO2000061631A1 (en) * 1999-04-12 2000-10-19 Astrazeneca Ab Modified pentapeptide antagonists of the atrial natriuretic peptide clearance receptor

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US5847135A (en) * 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme

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RU2255933C2 (ru) 2005-07-10
HUP0202184A2 (hu) 2002-12-28
EP1189881A1 (en) 2002-03-27
IL146312A (en) 2010-12-30
IL146312A0 (en) 2002-07-25
NO20015419D0 (no) 2001-11-06
SK16092001A3 (sk) 2002-04-04
CA2373180C (en) 2009-12-15
JP5468578B2 (ja) 2014-04-09
EP1189881B1 (en) 2004-09-29
JP2012006932A (ja) 2012-01-12
CZ20013983A3 (cs) 2002-04-17
ES2228527T3 (es) 2005-04-16
DE60014369T2 (de) 2005-11-24
HK1044533A1 (zh) 2002-10-25
WO2000068188A9 (en) 2002-08-29
ATE277923T1 (de) 2004-10-15
RU2255933C9 (ru) 2005-11-20
NO329899B1 (no) 2011-01-24
SI20876B (sl) 2009-08-31
JP2002544187A (ja) 2002-12-24
DE60014369T3 (de) 2013-06-27
HU229155B1 (en) 2013-09-30
DE60014369D1 (de) 2004-11-04
HUP0202184A3 (en) 2003-03-28
SI20876A (sl) 2002-10-31
KR20020009608A (ko) 2002-02-01
NZ515249A (en) 2004-07-30
WO2000068188A1 (en) 2000-11-16
JP4841729B2 (ja) 2011-12-21
AU4826900A (en) 2000-11-21
SK288186B6 (sk) 2014-05-06
NO20015419L (no) 2001-12-20
ES2228527T5 (es) 2013-05-23
RO121640B1 (ro) 2008-01-30
CN1370143A (zh) 2002-09-18
BR0010349B1 (pt) 2011-10-04
KR100767199B1 (ko) 2007-10-17
BR0010349C1 (pt) 2003-11-04
TR200103427T2 (tr) 2002-10-21
CZ304225B6 (cs) 2014-01-15
BR0010349A (pt) 2003-07-08
MXPA01011341A (es) 2002-06-21
PL354957A1 (en) 2004-03-22
CA2373180A1 (en) 2000-11-16
EP1189881B2 (en) 2013-01-23
EP1189881A4 (en) 2002-11-27

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