+

WO1992015607A3 - Derives d'amidines de phenyle efficaces en tant qu'inhibiteurs d'agregation des plaquettes - Google Patents

Derives d'amidines de phenyle efficaces en tant qu'inhibiteurs d'agregation des plaquettes Download PDF

Info

Publication number
WO1992015607A3
WO1992015607A3 PCT/US1992/001531 US9201531W WO9215607A3 WO 1992015607 A3 WO1992015607 A3 WO 1992015607A3 US 9201531 W US9201531 W US 9201531W WO 9215607 A3 WO9215607 A3 WO 9215607A3
Authority
WO
WIPO (PCT)
Prior art keywords
platelet aggregation
derivatives useful
aggregation inhibitors
phenyl amidines
phenyl
Prior art date
Application number
PCT/US1992/001531
Other languages
English (en)
Other versions
WO1992015607A2 (fr
Inventor
Robert Bruce Garland
Masateru Miyano
Jeffery Alan Zablocki
Lori Ann Schretzman
Original Assignee
Searle & Co
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 Searle & Co filed Critical Searle & Co
Priority to US08/090,127 priority Critical patent/US5481021A/en
Priority to AU16666/92A priority patent/AU662142B2/en
Priority to CA002099994A priority patent/CA2099994C/fr
Priority to EP92909278A priority patent/EP0574545B1/fr
Priority to DE69200766T priority patent/DE69200766T2/de
Priority to KR1019930702646A priority patent/KR100210206B1/ko
Priority to JP50875192A priority patent/JP3258659B2/ja
Publication of WO1992015607A2 publication Critical patent/WO1992015607A2/fr
Publication of WO1992015607A3 publication Critical patent/WO1992015607A3/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16—Tryptamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745—Blood coagulation or fibrinolysis factors
    • C07K14/75—Fibrinogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Indole Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Breeding Of Plants And Reproduction By Means Of Culturing (AREA)
  • Pyridine Compounds (AREA)

Abstract

L'invention se rapporte à des dérivés d'amidines de phényle correspondant à la formule suivante (I) et à un sel acceptable pharmaceutiquement, qui présentent une efficacité dans l'inhibition de l'agrégation des plaquettes. L'invention se rapporte également à des compositions pharmaceutiques à base desdits dérivés d'amidines de phényle.
PCT/US1992/001531 1991-03-06 1992-03-05 Derives d'amidines de phenyle efficaces en tant qu'inhibiteurs d'agregation des plaquettes WO1992015607A2 (fr)

Priority Applications (7)

Application Number Priority Date Filing Date Title
US08/090,127 US5481021A (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors
AU16666/92A AU662142B2 (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors
CA002099994A CA2099994C (fr) 1991-03-06 1992-03-05 Derives de phenylamidines utiles pour l'inhibition de l'agregation plaquettaire
EP92909278A EP0574545B1 (fr) 1991-03-06 1992-03-05 Derives d'amidines de phenyle efficaces en tant qu'inhibiteurs d'agregation des plaquettes
DE69200766T DE69200766T2 (de) 1991-03-06 1992-03-05 Phenylamidinderivate als plättchenaggregationsinhibitoren.
KR1019930702646A KR100210206B1 (ko) 1991-03-06 1992-03-05 혈소판 응집 억제제로서 유용한 페닐아미딘 유도체
JP50875192A JP3258659B2 (ja) 1991-03-06 1992-03-05 血小板凝集阻害剤として有用なフェニルアミジン誘導体類

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US66511991A 1991-03-06 1991-03-06
US665,119 1991-03-06

Publications (2)

Publication Number Publication Date
WO1992015607A2 WO1992015607A2 (fr) 1992-09-17
WO1992015607A3 true WO1992015607A3 (fr) 1992-10-29

Family

ID=24668789

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1992/001531 WO1992015607A2 (fr) 1991-03-06 1992-03-05 Derives d'amidines de phenyle efficaces en tant qu'inhibiteurs d'agregation des plaquettes

Country Status (13)

Country Link
US (1) US5481021A (fr)
EP (2) EP0574545B1 (fr)
JP (1) JP3258659B2 (fr)
KR (1) KR100210206B1 (fr)
AT (1) ATE114670T1 (fr)
AU (1) AU662142B2 (fr)
CA (1) CA2099994C (fr)
DE (1) DE69200766T2 (fr)
DK (1) DK0574545T3 (fr)
ES (1) ES2065182T3 (fr)
IE (1) IE920710A1 (fr)
MX (1) MX9203551A (fr)
WO (1) WO1992015607A2 (fr)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU646838B2 (en) * 1990-03-09 1994-03-10 F. Hoffmann-La Roche Ag Acetic acid derivatives
US5736122A (en) * 1991-02-08 1998-04-07 Diatide, Inc. Technetium-99m labeled peptides for thrombus imaging
US6019958A (en) * 1991-02-08 2000-02-01 Diatide, Inc. Technetium-99m labeled peptides for imaging inflammation
DE69230525T2 (de) * 1991-02-08 2000-06-21 Diatide, Inc. Technetium-99m markierte Polypeptide zur Bildformung
US5645815A (en) 1991-02-08 1997-07-08 Diatide, Inc. Radiolabled compounds for thrombus imaging
US5830856A (en) * 1991-02-08 1998-11-03 Diatide, Inc. Radiolabeled compounds for thrombus imaging
EP0584066A4 (fr) * 1991-04-11 1994-10-12 Rhone Poulenc Rorer Int Derives peptidiques et pseudopeptidiques antithrombotiques.
EP0513675B1 (fr) * 1991-05-13 1996-09-11 Fujisawa Pharmaceutical Co., Ltd. Nouveaux composés peptidique et procédé pour les préparer
US5239113A (en) * 1991-10-15 1993-08-24 Monsanto Company Substituted β-amino acid derivatives useful as platelet aggregation inhibitors and intermediates thereof
US5424334A (en) * 1991-12-19 1995-06-13 G. D. Searle & Co. Peptide mimetic compounds useful as platelet aggregation inhibitors
US5264457A (en) * 1992-02-14 1993-11-23 G. D. Searle & Co. Phenyl amidines sulfonamides useful as platelet aggregation inhibitors
TW223629B (fr) * 1992-03-06 1994-05-11 Hoffmann La Roche
DE4212304A1 (de) * 1992-04-13 1993-10-14 Cassella Ag Asparaginsäurederivate, ihre Herstellung und Verwendung
US5968476A (en) * 1992-05-21 1999-10-19 Diatide, Inc. Technetium-99m labeled peptides for thrombus imaging
US5354738A (en) * 1992-09-04 1994-10-11 G. D. Searle & Co. Platelet aggregation inhibitors
US5314902A (en) * 1993-01-27 1994-05-24 Monsanto Company Urea derivatives useful as platelet aggregation inhibitors
US5409939A (en) * 1993-02-12 1995-04-25 G. D. Searle & Co. Phenyl amidine thio derivatives useful as platelet aggregation inhibitors
AU6395094A (en) * 1993-03-15 1994-10-11 G.D. Searle & Co. Urea derivatives useful as platelet aggregation inhibitors
ZA942439B (en) * 1993-04-08 1996-01-08 Diatech Inc Radiolabeled compounds for thrombus imaging
TW394760B (en) * 1993-09-07 2000-06-21 Hoffmann La Roche Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same
ES2141849T3 (es) * 1993-11-19 2000-04-01 Searle & Co Composicion transdermica de n-(n-(5-(4-(aminoiminometil)fenil)-1-oxopentil)-l-alfa-aspartil)-l-fenilalanina o sus esteres y sus sales farmaceuticamente aceptables.
US5563158A (en) * 1993-12-28 1996-10-08 The Dupont Merck Pharmaceutical Company Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
US6387880B1 (en) * 1994-10-24 2002-05-14 G.D. Searle & Co. Transdermal N-[N-[5-[4-(aminoiminomethly)phenyl]-1-oxopentyl]-L-α-aspartyl]-L-phenylalainine or its esters and their pharmaceutically acceptable salts
JP3874455B2 (ja) * 1996-06-27 2007-01-31 新日本製鐵株式会社 フィブリノーゲン受容体拮抗物質およびそれを有効成分とする医薬製剤
US5811398A (en) * 1995-04-11 1998-09-22 G. D. Searle & Co. Platelet aggregation inhibitors containing C-terminal aminergic side chain amino acid residues
US5942544A (en) * 1996-02-22 1999-08-24 Dupont Pharmaceuticals Company α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors
AU2056197A (en) * 1996-02-22 1997-09-10 Du Pont Merck Pharmaceutical Company, The M-amidino phenyl analogs as factor xa inhibitors
CA2257856A1 (fr) * 1996-06-10 1997-12-18 G.D. Searle & Co. Compositions radiopharmaceutiques capables de se localiser en des sites de thrombus
US5872122A (en) * 1997-10-16 1999-02-16 Monsanto Company Pyrimidinylamidino β-amino acid derivatives useful as inhibitors of platelet aggregation
EP1030844A1 (fr) * 1997-11-10 2000-08-30 Array Biopharma Inc. Composes inhibant l'activite de la tryptase
US6037365A (en) * 1998-09-25 2000-03-14 G.D. Searle & Co. Aminobenzamidinosuccinyl lactone derivatives useful as inhibitors of platelet aggregation
US6362216B1 (en) 1998-10-27 2002-03-26 Array Biopharma Inc. Compounds which inhibit tryptase activity
CA2396744C (fr) * 1999-11-15 2011-07-12 Biomira, Inc. Analogues de lipide-a de synthese et leur utilisation
JP4662690B2 (ja) * 2001-04-24 2011-03-30 アリックス セラピューティクス 抗凝血薬として用いるクマリン誘導体
JP3964417B2 (ja) 2004-09-27 2007-08-22 国立大学法人金沢大学 インドール誘導体を有効成分とするα２受容体遮断剤及び血管拡張剤
WO2011059731A1 (fr) 2009-10-29 2011-05-19 Janssen Pharmaceutica Nv Derives derives d'alkynyle utilises comme inhibiteurs de dpp-1

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0384362A2 (fr) * 1989-02-23 1990-08-29 F. Hoffmann-La Roche Ag Dérivés de la glycine

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4589881A (en) * 1982-08-04 1986-05-20 La Jolla Cancer Research Foundation Polypeptide
US4614517A (en) * 1982-08-04 1986-09-30 La Jolla Cancer Research Foundation Tetrapeptide
US4661111A (en) * 1982-08-04 1987-04-28 La Jolla Cancer Research Foundation Polypeptide
US4578079A (en) * 1982-08-04 1986-03-25 La Jolla Cancer Research Foundation Tetrapeptide
US4517686A (en) * 1982-08-04 1985-05-21 La Jolla Cancer Research Foundation Polypeptide
US4683291A (en) * 1985-10-28 1987-07-28 Scripps Clinic And Research Foundation Platelet binding inhibitors
DE3781263T2 (de) * 1986-12-15 1993-04-08 Inst Nat Sante Rech Med Peptid-derivate und deren verwendung in der therapie.
NZ223148A (en) * 1987-01-16 1989-10-27 Merrell Dow Pharma Peptide derivatives having peptidase inhibition activity
FR2617170B1 (fr) * 1987-06-25 1989-12-22 Inst Nat Sante Rech Med Nouveaux derives peptidiques et leur application notamment en therapeutique
US4857508A (en) * 1987-12-03 1989-08-15 Monsanto Company Novel platelet-aggregation inhibitor peptide derivatives
US4879313A (en) * 1988-07-20 1989-11-07 Mosanto Company Novel platelet-aggregation inhibitors
US5039805A (en) * 1988-12-08 1991-08-13 Hoffmann-La Roche Inc. Novel benzoic and phenylacetic acid derivatives
US5084466A (en) * 1989-01-31 1992-01-28 Hoffmann-La Roche Inc. Novel carboxamide pyridine compounds which have useful pharmaceutical utility
EP0410540A1 (fr) * 1989-07-28 1991-01-30 Merck & Co. Inc. Antagonistes des récepteurs fibrinogéniques

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0384362A2 (fr) * 1989-02-23 1990-08-29 F. Hoffmann-La Roche Ag Dérivés de la glycine

Also Published As

Publication number Publication date
US5481021A (en) 1996-01-02
JP3258659B2 (ja) 2002-02-18
ES2065182T3 (es) 1995-02-01
CA2099994C (fr) 2003-05-20
EP0574545A1 (fr) 1993-12-22
DE69200766D1 (en) 1995-01-12
KR100210206B1 (ko) 1999-07-15
CA2099994A1 (fr) 1992-09-07
EP0574545B1 (fr) 1994-11-30
AU1666692A (en) 1992-10-06
EP0502536A1 (fr) 1992-09-09
MX9203551A (es) 1992-09-01
DE69200766T2 (de) 1995-05-04
WO1992015607A2 (fr) 1992-09-17
AU662142B2 (en) 1995-08-24
EP0502536B1 (fr) 1996-10-09
ATE114670T1 (de) 1994-12-15
DK0574545T3 (da) 1995-01-30
JPH06505497A (ja) 1994-06-23
IE920710A1 (en) 1992-09-09

Similar Documents

Publication Publication Date Title
WO1992015607A3 (fr) Derives d'amidines de phenyle efficaces en tant qu'inhibiteurs d'agregation des plaquettes
CA2159450A1 (fr) 1-amidinophenyl-pyrrolidones piperidinones azetinones, inhibiteurs de l'agregation plaquettaire
ZA945836B (en) Platelet aggregation inhibitors
RU95101048A (ru) Производные пролинамида, фармкомпозиция на их основе
WO2001072728A3 (fr) Nouveaux derives de piperazine
BG103195A (en) Substituted indazole derivatives and their application as inhibitors of phosphodiesterase (pde) type iv and of the production of a tumournecrotic factor (tnf)
WO1995000501A3 (fr) Heterocycles phenyle utilises comme inhibiteurs de la cyclo-oxygenase-2
CA2140927A1 (fr) Inhibiteurs d'agregation plaquettaire
AU2867992A (en) Substituted heterocyclic derivatives useful as platelet aggregation inhibitors
IL101839A0 (en) Peptide compounds,processes for the preparation thereof,and pharmaceutical compositions containing the same
WO2003049690A3 (fr) Inhibiteurs de l'integrase du vih
WO1996023771A3 (fr) Inhibiteurs de l'agregation plaquettaire
WO2001072263A3 (fr) Utilisation d'ectoine ou de derives d'ectoine pour proteger la proteine du stress de la peau
AU671163B2 (en) Alkyl substituted heterocyclic compounds
ES2181879T3 (es) Inhibidores de la agkytubacuib de las plaquetas que contienen restos de aminoacidos con cadenas laterales de c-terminal aminergicos.

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AT AU BB BG BR CA CH CS DE DK ES FI GB HU JP KP KR LK LU MG MN MW NL NO PL RO RU SD SE US

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): AT BE BF BJ CF CG CH CI CM DE DK ES FR GA GB GN GR IT LU MC ML MR NL SE SN TD TG

AK Designated states

Kind code of ref document: A3

Designated state(s): AT AU BB BG BR CA CH CS DE DK ES FI GB HU JP KP KR LK LU MG MN MW NL NO PL RO RU SD SE US

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): AT BE BF BJ CF CG CH CI CM DE DK ES FR GA GB GN GR IT LU MC ML MR NL SE SN TD TG

COP Corrected version of pamphlet

Free format text: PAGES 1-94,DESCRIPTION,AND PAGES 95-106,CLAIMS,REPLACED BY NEW PAGES BEARING THE SAME NUMBER;DUE TOLATE TRANSMITTAL BY THE RECEIVING OFFICE

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 2099994

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 1992909278

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 1992909278

Country of ref document: EP

NENP Non-entry into the national phase

Ref country code: CA

WWG Wipo information: grant in national office

Ref document number: 1992909278

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 08090127

Country of ref document: US

点击 这是indexloc提供的php浏览器服务，不要输入任何密码和下载