ES2194486T3 - Derivados de diacilhidrazina como inhibidores de integrina. - Google Patents

Derivados de diacilhidrazina como inhibidores de integrina.

Info

Publication number
ES2194486T3
ES2194486T3 ES99934576T ES99934576T ES2194486T3 ES 2194486 T3 ES2194486 T3 ES 2194486T3 ES 99934576 T ES99934576 T ES 99934576T ES 99934576 T ES99934576 T ES 99934576T ES 2194486 T3 ES2194486 T3 ES 2194486T3
Authority
ES
Spain
Prior art keywords
diacilhidrazine
integrine
inhibitors
derivatives
formula
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.)
Expired - Lifetime
Application number
ES99934576T
Other languages
English (en)
Inventor
Gunter Holzemann
Simon Goodman
Horst Kessler
Christoph Gibson
Jorg Simon Schmitt
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.)
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
Application granted granted Critical
Publication of ES2194486T3 publication Critical patent/ES2194486T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Compuestos de la fórmula I **(Fórmula)** donde X significa H2N-C(=NH)-NH-, Y significa **(Fórmula)** -(CH2)n-, -(CH2) CH2)o o -(CH2)n-Het2-(CH2)q-, Z significa -(CH2)r-R5, R1, R2 significa H, R3 significa H, R5 significa COOH, Het2 significa piridilo, n significa 3, 4 ó 5, m, o, p, q, r significan en cada caso, independientemente entre sí, 0, 1 ó 2, así como sus sales y solvatos.
ES99934576T 1998-07-15 1999-07-06 Derivados de diacilhidrazina como inhibidores de integrina. Expired - Lifetime ES2194486T3 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ES2194486T3 true ES2194486T3 (es) 2003-11-16

Family

ID=7874107

Family Applications (1)

Application Number Title Priority Date Filing Date
ES99934576T Expired - Lifetime ES2194486T3 (es) 1998-07-15 1999-07-06 Derivados de diacilhidrazina como inhibidores de integrina.

Country Status (22)

Country Link
US (1) US6326403B1 (es)
EP (1) EP1097127B1 (es)
JP (1) JP2002520382A (es)
KR (1) KR20010079520A (es)
CN (1) CN1309633A (es)
AR (1) AR019777A1 (es)
AT (1) ATE234276T1 (es)
AU (1) AU753333B2 (es)
BR (1) BR9912072A (es)
CA (1) CA2337305A1 (es)
DE (2) DE19831710A1 (es)
DK (1) DK1097127T3 (es)
ES (1) ES2194486T3 (es)
HU (1) HUP0102602A3 (es)
ID (1) ID27168A (es)
NO (1) NO20010203D0 (es)
PL (1) PL345398A1 (es)
PT (1) PT1097127E (es)
SK (1) SK412001A3 (es)
TW (1) TW448145B (es)
WO (1) WO2000003973A1 (es)
ZA (1) ZA200101267B (es)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1181054A1 (en) 1999-06-01 2002-02-27 Biogen, Inc. A blocking monoclonal antibody to vla-1 and its use for the treatment of inflammatory disorders
US20020002152A1 (en) 2000-04-14 2002-01-03 Craig Richard A. Hydrazide and alkoxyamide angiogenesis inhibitors
UY26664A1 (es) * 2000-04-14 2001-11-30 Abbott Lab Hidrazidas y alcoxiamidas inhibidoras de la angiogénesis.
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.
ES2278016T3 (es) 2001-04-09 2007-08-01 Novartis Vaccines And Diagnostics, Inc. Compuestos guanidino como agonistas del receptor de melanocortina 4 (mc4-r).
DE60236735D1 (de) 2001-04-13 2010-07-29 Biogen Idec Inc Antikörper gegen vla-1
PT1551834E (pt) 2002-05-23 2010-09-30 Novartis Vaccines & Diagnostic Compostos de quinazolinona substituídos
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
CA2523015A1 (en) 2003-05-23 2004-12-29 Chiron Corporation Guanidino-substituted quinazolinone compounds as mc4-r agonists
DE10325049A1 (de) * 2003-06-02 2004-12-23 Merck Patent Gmbh Peptid- und Peptidmimetika-Derivate mit Integrin-Inhibitor-Eigenschaften III
MXPA06005736A (es) 2003-11-19 2006-12-14 Chiron Corp Compuestos de quinazolinona con bioacumulacion reducida.
PT2484365E (pt) 2004-06-04 2013-12-12 Scripps Research Inst Composições e métodos para o tratamento de doenças neovasculares
JP4745175B2 (ja) * 2005-12-28 2011-08-10 本田技研工業株式会社 自動二輪車
PL2034830T3 (pl) 2006-05-25 2015-04-30 Biogen Ma Inc Przeciwciało anty-VLA-1 do leczenia udaru
CA2689137C (en) 2007-05-29 2017-05-02 Intrexon Corporation Chiral diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
JP6345123B2 (ja) 2012-02-16 2018-06-20 サンタラス， インコーポレイテッド 抗ｖｌａ１（ｃｄ４９ａ）抗体医薬組成物
US9127024B2 (en) 2013-03-15 2015-09-08 Intrexon Corporation Boron-containing diacylhydrazines
ES2864079T3 (es) 2014-05-30 2021-10-13 Pfizer Derivados de carbonitrilo como moduladores selectivos del receptor de andrógenos
CN104027805B (zh) * 2014-06-18 2017-02-15 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
AU2015317862A1 (en) 2014-09-17 2017-04-06 Intrexon Corporation Boron-containing diacylhydrazine compounds
WO2019089765A1 (en) 2017-11-01 2019-05-09 Arrowhead Pharmcaceuticals, Inc. Integrin ligands and uses thereof
JP2024516096A (ja) 2021-04-08 2024-04-12 アローヘッド ファーマシューティカルズ インコーポレイテッド 終末糖化産物受容体の発現を阻害するためのＲＮＡｉ剤、その組成物、及び使用方法
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
WO1992013552A1 (en) * 1991-02-05 1992-08-20 Smithkline Beecham Corporation Anti-aggregatory peptides containing an aromatic ester or amide
US5530028A (en) * 1992-11-23 1996-06-25 Rohm And Haas Company Insecticidal N'-substituted-N,N'-diacylhydrazines
US5726192A (en) * 1992-12-29 1998-03-10 Smithkline Beecham Corporation Platelet aggregation inhibiting compounds
JPH10501222A (ja) 1994-05-27 1998-02-03 メルク エンド カンパニー インコーポレーテッド 破骨細胞仲介骨吸収を抑制するための化合物
US5482962A (en) * 1994-07-22 1996-01-09 Rohm And Haas Company Insecticidal N,N'-disubstituted-N-N'-diacylhydrazines
AU713676B2 (en) * 1996-01-16 1999-12-09 Merck & Co., Inc. Integrin receptor antagonists

Also Published As

Publication number Publication date
KR20010079520A (ko) 2001-08-22
HUP0102602A2 (hu) 2002-01-28
PL345398A1 (en) 2001-12-17
US6326403B1 (en) 2001-12-04
PT1097127E (pt) 2003-07-31
SK412001A3 (en) 2001-08-06
DE59904547D1 (de) 2003-04-17
DE19831710A1 (de) 2000-01-20
DK1097127T3 (da) 2003-06-10
JP2002520382A (ja) 2002-07-09
AU5031399A (en) 2000-02-07
AR019777A1 (es) 2002-03-13
WO2000003973A1 (de) 2000-01-27
EP1097127B1 (de) 2003-03-12
NO20010203L (no) 2001-01-12
TW448145B (en) 2001-08-01
ATE234276T1 (de) 2003-03-15
ID27168A (id) 2001-03-08
NO20010203D0 (no) 2001-01-12
HUP0102602A3 (en) 2002-02-28
AU753333B2 (en) 2002-10-17
CN1309633A (zh) 2001-08-22
ZA200101267B (en) 2002-10-04
CA2337305A1 (en) 2000-01-27
EP1097127A1 (de) 2001-05-09
BR9912072A (pt) 2001-09-25

Similar Documents

Publication Publication Date Title
ES2194486T3 (es) Derivados de diacilhidrazina como inhibidores de integrina.
TR199801255T2 (xx) Vitronektin resept�r antagonistleri.
TR199901667T2 (xx) 3-Heterosiklil-ikame edilmi� benzoil t�revleri
DE69115280D1 (de) Indolderivate, die die leukotrienbiosynthese hemmen.
ES2170252T3 (es) Tetrahidroimidazopiridoindoldionas como inhibidores de cgmp especifico pde.
TR199801253T2 (xx) Vitronektin resept�r� antagonistleri.
PT1140944E (pt) Derivados de epotilona e sua utilizacao como agentes antitumorais
ATE427300T1 (de) Heterocyclisch substituierte amide als calpainhemmer
CO4750823A1 (es) Sales bisindolilmaleimidas con un puente n,n´ como inhibidores de proteina quinasa c
HUP0203750A2 (hu) IX Faktor/IXa faktor ellenanyagok és ellenanyag származékok
ATE133179T1 (de) Steroid-sulfatase-inhibitoren
CY1105386T1 (el) Βενζοϋλοσουλφοναμιδια και σουλφονυλβενζαμιδινες για χρηση σαν παραγοντες κατα του ογκου
NO971538L (no) Purin- og guaninforbindelser som inhibitorer for PNP
PT889886E (pt) Novas fenantridinas substituidas na posicao 6
TR200201205T2 (tr) N-ikame edilmiş karbamoiloksialkil-azolyum türevleri.
TR200003384T2 (tr) Arginin türevleri kullanılarak oksazolidinon antibakteriyel maddelerin etkisinin arttırılması
PA8485101A1 (es) Nuevos antibioticos macrolidos.
AR241082A2 (es) Nuevos derivados de pirazol utiles como agentes herbicidas, las composiciones herbicidas que los contienen y los procedimientos para producir estos derivados de pirazol&#34;.
TR199701645A2 (xx) Vitronektin resept�r antagonistleri,bunlar�n imalat� ve kullan�m�
DE60318826D1 (de) Alkoxypyridinderivate
UY25211A1 (es) Inhibidores de isoquinolinilguanidina uroquinasa
PA8508301A1 (es) Inhibidores de la proteina c del procolageno
ATE333457T1 (de) Zyklische gmp-spezifische phosphodiesteraseinhibitoren
PA8466101A1 (es) Agentes terapeuticos
AR025797A1 (es) Quinazolinonas