CN1309633A - 作为整合素抑制剂的二酰基肼衍生物 - Google Patents

作为整合素抑制剂的二酰基肼衍生物 Download PDF

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Publication number
CN1309633A
CN1309633A CN99808610A CN99808610A CN1309633A CN 1309633 A CN1309633 A CN 1309633A CN 99808610 A CN99808610 A CN 99808610A CN 99808610 A CN99808610 A CN 99808610A CN 1309633 A CN1309633 A CN 1309633A
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CN
China
Prior art keywords
formula
compound
acid
compounds
protecting group
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
CN99808610A
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English (en)
Chinese (zh)
Inventor
G·赫尔泽曼
S·古德曼
H·克斯勒
C·吉布森
J·S·施米特
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Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CN1309633A publication Critical patent/CN1309633A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/15—Oximes (>C=N—O—); Hydrazines (>N—N<); Hydrazones (>N—N=) ; Imines (C—N=C)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C281/00—Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C281/06—Compounds containing any of the groups, e.g. semicarbazides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN99808610A 1998-07-15 1999-07-06 作为整合素抑制剂的二酰基肼衍生物 Pending CN1309633A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19831710A DE19831710A1 (de) 1998-07-15 1998-07-15 Diacylhydrazinderivate
DE19831710.7 1998-07-15

Publications (1)

Publication Number Publication Date
CN1309633A true CN1309633A (zh) 2001-08-22

Family

ID=7874107

Family Applications (1)

Application Number Title Priority Date Filing Date
CN99808610A Pending CN1309633A (zh) 1998-07-15 1999-07-06 作为整合素抑制剂的二酰基肼衍生物

Country Status (22)

Country Link
US (1) US6326403B1 (enExample)
EP (1) EP1097127B1 (enExample)
JP (1) JP2002520382A (enExample)
KR (1) KR20010079520A (enExample)
CN (1) CN1309633A (enExample)
AR (1) AR019777A1 (enExample)
AT (1) ATE234276T1 (enExample)
AU (1) AU753333B2 (enExample)
BR (1) BR9912072A (enExample)
CA (1) CA2337305A1 (enExample)
DE (2) DE19831710A1 (enExample)
DK (1) DK1097127T3 (enExample)
ES (1) ES2194486T3 (enExample)
HU (1) HUP0102602A3 (enExample)
ID (1) ID27168A (enExample)
NO (1) NO20010203L (enExample)
PL (1) PL345398A1 (enExample)
PT (1) PT1097127E (enExample)
SK (1) SK412001A3 (enExample)
TW (1) TW448145B (enExample)
WO (1) WO2000003973A1 (enExample)
ZA (1) ZA200101267B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104027805A (zh) * 2014-06-18 2014-09-10 北京大学 抑制整合素α5的物质在制备预防内皮细胞激活和/或动脉粥样硬化的产品中的新用途

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4817503B2 (ja) 1999-06-01 2011-11-16 バイオジェン・アイデック・エムエイ・インコーポレイテッド Ｖｌａ−１に対するブロッキングモノクローナル抗体および炎症性障害の処置のためのその使用
UY26664A1 (es) * 2000-04-14 2001-11-30 Abbott Lab Hidrazidas y alcoxiamidas inhibidoras de la angiogénesis.
US20020002152A1 (en) 2000-04-14 2002-01-03 Craig Richard A. Hydrazide and alkoxyamide angiogenesis inhibitors
DE10040105A1 (de) 2000-08-17 2002-02-28 Merck Patent Gmbh Peptid- und Peptidmimetika-Derivate mit Integrin-Inhibitor-Eigenschaften
DE10040103A1 (de) 2000-08-17 2002-02-28 Merck Patent Gmbh Peptid- und Peptidmimetika-Derivate mit Integrin-Inhibitor-Eigenschaften II
DZ3415A1 (fr) * 2000-08-31 2002-03-07 Chiron Corp Guanidinobenzamides comme mc4-r agonistes.
PT1385823E (pt) 2001-04-09 2007-01-31 Novartis Vaccines & Diagnostic Compostos de guanidino como agonistas do receptor de melanocortina-4 (r-mc4)
EE200300509A (et) 2001-04-13 2004-08-16 Biogen, Inc. Antikehad VLA-1 vastu
DE60333937D1 (de) 2002-05-23 2010-10-07 Novartis Vaccines & Diagnostic Substituierte quinazolinone verbindungen
US7226577B2 (en) 2003-01-13 2007-06-05 Bracco Imaging, S. P. A. Gastrin releasing peptide compounds
US7304161B2 (en) 2003-02-10 2007-12-04 Intrexon Corporation Diaclhydrazine ligands for modulating the expression of exogenous genes in mammalian systems via an ecdysone receptor complex
US7456315B2 (en) 2003-02-28 2008-11-25 Intrexon Corporation Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
JP2007501861A (ja) 2003-05-23 2007-02-01 カイロン コーポレイション Ｍｃ４−ｒアゴニストとしてのグアニジノ置換キナゾリノン化合物
DE10325049A1 (de) * 2003-06-02 2004-12-23 Merck Patent Gmbh Peptid- und Peptidmimetika-Derivate mit Integrin-Inhibitor-Eigenschaften III
US7368453B2 (en) 2003-11-19 2008-05-06 Chiron Corporation Quinazolinone compounds with reduced bioaccumulation
WO2005117954A2 (en) 2004-06-04 2005-12-15 The Scripps Research Institute Compositions and methods for treatment of neovascular diseases
JP4745175B2 (ja) * 2005-12-28 2011-08-10 本田技研工業株式会社 自動二輪車
CN105381459A (zh) * 2006-05-25 2016-03-09 比奥根Ma公司 治疗中风的方法
ES2672513T3 (es) 2007-05-29 2018-06-14 Intrexon Corporation Ligandos de diacilhidrazina quirales para modular la expresión genética exógena a través del complejo del receptor de ecdisona
US10316095B2 (en) 2012-02-16 2019-06-11 Santarus, Inc. Antibody formulations
SG11201506875YA (en) 2013-03-15 2015-09-29 Intrexon Corp Boron-containing diacylhydrazines
CA2950390C (en) 2014-05-30 2020-09-22 Pfizer Inc. Carbonitrile derivatives as selective androgen receptor modulators
MX2017003403A (es) 2014-09-17 2017-06-19 Intrexon Corp Compuestos de diacilhidrazina que contienen boro.
IL274300B2 (en) 2017-11-01 2024-09-01 Arrowhead Pharmaceuticals Inc Alpha v beta 6 integrin ligands, compositions comprising same and uses thereof
KR20230167082A (ko) 2021-04-08 2023-12-07 애로우헤드 파마슈티컬스 인코포레이티드 진행성 당화 최종 산물에 대한 수용체의 발현을 억제하기 위한 RNAi 작용제, 그의 조성물, 및 사용 방법
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5051405A (en) * 1989-10-10 1991-09-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Anti-thrombotic peptides and pseudopeptides
JPH06505978A (ja) * 1991-02-05 1994-07-07 スミスクライン・ビーチャム・コーポレイション 芳香族エステルまたはアミドを含有する抗凝集性ペプチド
US5530028A (en) * 1992-11-23 1996-06-25 Rohm And Haas Company Insecticidal N'-substituted-N,N'-diacylhydrazines
JPH08505846A (ja) * 1992-12-29 1996-06-25 スミスクライン・ビーチャム・コーポレイション 血小板凝集阻害用化合物
ATE227567T1 (de) 1994-05-27 2002-11-15 Merck & Co Inc Präparate zur hemmung der durch osteoklasten vermittelten knochenresorption
US5482962A (en) * 1994-07-22 1996-01-09 Rohm And Haas Company Insecticidal N,N'-disubstituted-N-N'-diacylhydrazines
EP0880511A4 (en) * 1996-01-16 1999-06-16 Merck & Co Inc Integrin receptor antagonists

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104027805A (zh) * 2014-06-18 2014-09-10 北京大学 抑制整合素α5的物质在制备预防内皮细胞激活和/或动脉粥样硬化的产品中的新用途

Also Published As

Publication number Publication date
NO20010203D0 (no) 2001-01-12
PT1097127E (pt) 2003-07-31
AU753333B2 (en) 2002-10-17
TW448145B (en) 2001-08-01
NO20010203L (no) 2001-01-12
JP2002520382A (ja) 2002-07-09
EP1097127A1 (de) 2001-05-09
ZA200101267B (en) 2002-10-04
ES2194486T3 (es) 2003-11-16
DE59904547D1 (de) 2003-04-17
BR9912072A (pt) 2001-09-25
DE19831710A1 (de) 2000-01-20
ATE234276T1 (de) 2003-03-15
US6326403B1 (en) 2001-12-04
KR20010079520A (ko) 2001-08-22
AR019777A1 (es) 2002-03-13
WO2000003973A1 (de) 2000-01-27
DK1097127T3 (da) 2003-06-10
CA2337305A1 (en) 2000-01-27
HUP0102602A2 (hu) 2002-01-28
PL345398A1 (en) 2001-12-17
ID27168A (id) 2001-03-08
EP1097127B1 (de) 2003-03-12
HUP0102602A3 (en) 2002-02-28
SK412001A3 (en) 2001-08-06
AU5031399A (en) 2000-02-07

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