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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

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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
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.)
Ceased
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
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.)
GD Searle LLC
Original Assignee
GD Searle LLC
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 GD Searle LLC filed Critical GD Searle LLC
Priority to CA002099994A priority Critical patent/CA2099994C/fr
Priority to DE69200766T priority patent/DE69200766T2/de
Priority to AU16666/92A priority patent/AU662142B2/en
Priority to US08/090,127 priority patent/US5481021A/en
Priority to JP50875192A priority patent/JP3258659B2/ja
Priority to EP92909278A priority patent/EP0574545B1/fr
Priority to KR1019930702646A priority patent/KR100210206B1/ko
Publication of WO1992015607A2 publication Critical patent/WO1992015607A2/fr
Publication of WO1992015607A3 publication Critical patent/WO1992015607A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Hydrogenated Pyridines (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 Ceased WO1992015607A2 (fr)

Priority Applications (7)

Application Number Priority Date Filing Date Title
CA002099994A CA2099994C (fr) 1991-03-06 1992-03-05 Derives de phenylamidines utiles pour l'inhibition de l'agregation plaquettaire
DE69200766T DE69200766T2 (de) 1991-03-06 1992-03-05 Phenylamidinderivate als plättchenaggregationsinhibitoren.
AU16666/92A AU662142B2 (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors
US08/090,127 US5481021A (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors
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
EP92909278A EP0574545B1 (fr) 1991-03-06 1992-03-05 Derives d'amidines de phenyle efficaces en tant qu'inhibiteurs d'agregation des plaquettes
KR1019930702646A KR100210206B1 (ko) 1991-03-06 1992-03-05 혈소판 응집 억제제로서 유용한 페닐아미딘 유도체

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 Ceased 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)

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AU646838B2 (en) * 1990-03-09 1994-03-10 F. Hoffmann-La Roche Ag Acetic acid derivatives
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
ES2141102T3 (es) * 1991-02-08 2000-03-16 Diatide Inc Polipeptidos marcados con tecnecio-99m para la generacion de imagenes.
US6019958A (en) * 1991-02-08 2000-02-01 Diatide, Inc. Technetium-99m labeled peptides for imaging inflammation
US5736122A (en) * 1991-02-08 1998-04-07 Diatide, Inc. Technetium-99m labeled peptides for thrombus imaging
JPH08503920A (ja) * 1991-04-11 1996-04-30 ローヌ−プーラン ローラー インターナショナル（ホウルディングス） インコーポレイテッド 抗血栓ペプチドおよび偽ペプチド誘導体
ATE142641T1 (de) * 1991-05-13 1996-09-15 Fujisawa Pharmaceutical Co Neue peptid-verbindungen und verfahren zur herstellung davon
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
ATE220926T1 (de) * 1993-04-08 2002-08-15 Diatide Inc Radiomarkierte verbindungen zur thrombus- bilderzeugung
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
PT892780E (pt) * 1996-02-22 2003-02-28 Bristol Myers Squibb Pharma Co Analogos de m-amidino fenilo como inibidores do factor xa
JP2001504801A (ja) * 1996-06-10 2001-04-10 ジー．ディー．サール アンド カンパニー 血栓サイトに局在化可能な放射性医薬組成物
UA63887C2 (en) * 1996-10-28 2004-02-16 Lg Chemical Ltd Selective thrombin inhibitors and a pharmaceutical composition based thereon
US5872122A (en) * 1997-10-16 1999-02-16 Monsanto Company Pyrimidinylamidino β-amino acid derivatives useful as inhibitors of platelet aggregation
WO1999024407A1 (fr) * 1997-11-10 1999-05-20 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
US7491707B1 (en) * 1999-11-15 2009-02-17 Biomira, Inc. Synthetic lipid-a-analogs and uses thereof
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
ES2513291T3 (es) 2009-10-29 2014-10-24 Janssen Pharmaceutica Nv Derivados alquinilo útiles como inhibidores de la 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

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US4614517A (en) * 1982-08-04 1986-09-30 La Jolla Cancer Research Foundation Tetrapeptide
US4578079A (en) * 1982-08-04 1986-03-25 La Jolla Cancer Research Foundation Tetrapeptide
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US4517686A (en) * 1982-08-04 1985-05-21 La Jolla Cancer Research Foundation Polypeptide
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EP0275748B1 (fr) * 1986-12-15 1992-08-19 Institut National De La Sante Et De La Recherche Medicale (Inserm) Nouveaux dérivés peptidiques et leur application notamment en thérapeutique
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
CA2021951A1 (fr) * 1989-07-28 1991-01-29 Ruth F. Nutt Antagonistes des recepteurs du fibrinogene

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

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