ES2169105T3 - Agentes antitromboticos tripeptidicos. - Google Patents

Agentes antitromboticos tripeptidicos.

Info

Publication number
ES2169105T3
ES2169105T3 ES95201960T ES95201960T ES2169105T3 ES 2169105 T3 ES2169105 T3 ES 2169105T3 ES 95201960 T ES95201960 T ES 95201960T ES 95201960 T ES95201960 T ES 95201960T ES 2169105 T3 ES2169105 T3 ES 2169105T3
Authority
ES
Spain
Prior art keywords
group
amino
substituted
tripeptidic
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
ES95201960T
Other languages
English (en)
Inventor
Paul David Gesellchen
Robert Theodore Shuman
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and 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 Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of ES2169105T3 publication Critical patent/ES2169105T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • C07K5/08—Tripeptides
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • 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
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • External Artificial Organs (AREA)
  • Inert Electrodes (AREA)

Abstract

SE PRESENTAN INHIBIDORES DE LA TROMBINA REPRESENTADOS POR LA FORMULA EN LA QUE A(C=O)- ES, ENTRE OTROS, FENILGLICILO, CICLOHEXILGLICILO, CICLOHEXENILGLICILO, TIENILGLICILO O NAFTILGLICILO, EN DONDE EL GRUPO {AL}-AMINO SE SUSTITUYE PREFERENTEMENTE POR ALQUILO, P. EJ., METILO O UN GRUPO ALCOXICARBONILO, CICLOALCOXICARBONILO O ARILOALCOXICARBONILO, P. EJ. T-BUTILOXICARBONILO. A(C=O)- TAMBIEN REPRESENTA UN GRUPO ACETILO {AL}-SUSTITUIDO TAL COMO {AL}-METOXIFENILACETILO; O UN GRUPO BICICLICO TAL COMO UN GRUPO TETRAHIDROISOQUINOLIN-1-ILO; O UN GRUPO 1-AMINO O CICLOALQUILCARBONILO (SUSTITUIDO POR AMINO) TAL COMO 1-AMINOCICLOHEXILCARBONILO. TAMBIEN SE PRESENTAN UN METODO PARA INHIBIR LA FORMACION DE COAGULOS DE SANGRE EN SERES HUMANOS Y ANIMALES MEDIANTE LA ADMINISTRACION DE UN INHIBIDOR DE LA TROMBINA DE LA FORMULA DE ARRIBA Y LAS FORMULACIONES FARMACEUTICAS UTILES PARA LLEVAR A CABO EL METODO.
ES95201960T 1990-09-28 1991-09-26 Agentes antitromboticos tripeptidicos. Expired - Lifetime ES2169105T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58955390A 1990-09-28 1990-09-28
US75609191A 1991-09-06 1991-09-06

Publications (1)

Publication Number Publication Date
ES2169105T3 true ES2169105T3 (es) 2002-07-01

Family

ID=27080589

Family Applications (2)

Application Number Title Priority Date Filing Date
ES91308785T Expired - Lifetime ES2194835T3 (es) 1990-09-28 1991-09-26 Agentes antitromboticos a base de tripeptidos.
ES95201960T Expired - Lifetime ES2169105T3 (es) 1990-09-28 1991-09-26 Agentes antitromboticos tripeptidicos.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES91308785T Expired - Lifetime ES2194835T3 (es) 1990-09-28 1991-09-26 Agentes antitromboticos a base de tripeptidos.

Country Status (22)

Country Link
EP (4) EP0684258A2 (es)
JP (1) JP3023019B2 (es)
KR (1) KR100219993B1 (es)
CN (1) CN1036399C (es)
AT (2) ATE211147T1 (es)
AU (1) AU645347B2 (es)
BR (1) BR9104181A (es)
CA (1) CA2052013C (es)
CZ (1) CZ285980B6 (es)
DE (2) DE69133217T2 (es)
DK (1) DK0685489T3 (es)
ES (2) ES2194835T3 (es)
FI (1) FI107733B (es)
HU (2) HU217441B (es)
IE (1) IE913423A1 (es)
IL (1) IL99527A (es)
MX (1) MX9101280A (es)
NO (1) NO309984B1 (es)
NZ (1) NZ239907A (es)
PT (1) PT99068B (es)
RU (1) RU2077538C1 (es)
SK (1) SK281731B6 (es)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6008217A (en) * 1995-12-20 1999-12-28 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5874424A (en) * 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
US5430023A (en) * 1990-09-28 1995-07-04 Eli Lilly And Company Tripeptide antithrombotic agents
CA2071621C (en) * 1991-06-19 1996-08-06 Ahihiko Hosoda Aldehyde derivatives
CA2075154A1 (en) * 1991-08-06 1993-02-07 Neelakantan Balasubramanian Peptide aldehydes as antithrombotic agents
SE9102462D0 (sv) * 1991-08-28 1991-08-28 Astra Ab New isosteric peptides
US5416093A (en) * 1991-11-12 1995-05-16 Eli Lilly And Company Antithrombotic agents
AU663169B2 (en) * 1992-03-04 1995-09-28 Gyogyszerkutato Intezet Kft New anticoagulant peptide derivatives and pharmaceutical compositions containing the same as well as a process for the preparation thereof
US5583146A (en) * 1992-12-02 1996-12-10 Bristol-Myers Squibb Company Heterocyclic thrombin inhibitors
US5455229A (en) * 1992-12-23 1995-10-03 Eli Lilly And Company Method for minimizing and containing ischemic and reperfusion injury
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
JPH06340619A (ja) * 1993-05-03 1994-12-13 Bristol Myers Squibb Co グアニジニルまたはアミジニル置換メチルアミノ複素環トロンビン抑制剤
US5783563A (en) * 1993-06-03 1998-07-21 Astra Aktiebolag Method for treatment or prophylaxis of venous thrombosis
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
US5439888A (en) * 1994-03-04 1995-08-08 Eli Lilly And Company Antithrombotic agents
ZA951618B (en) * 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5885967A (en) * 1994-03-04 1999-03-23 Eli Lilly And Company Antithrombotic agents
CA2143533A1 (en) * 1994-03-04 1995-09-05 Kenneth D. Kurz Antithrombotic agents
ZA951617B (en) * 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
GB2287027A (en) * 1994-03-04 1995-09-06 Lilly Co Eli Tripeptide antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5488037A (en) * 1994-03-04 1996-01-30 Eli Lilly And Company Antithrombotic agents
US5602101A (en) * 1994-03-04 1997-02-11 Eli Lilly And Company Antithrombotic agents
US5436229A (en) * 1994-03-04 1995-07-25 Eli Lilly And Company Bisulfite adducts of arginine aldehydes
US5484772A (en) * 1994-03-04 1996-01-16 Eli Lilly And Company Antithrombotic agents
EP0748333A4 (en) * 1994-03-04 2000-05-10 Lilly Co Eli ANTITHROMBOTIC SUBSTANCES
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
US5847135A (en) * 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5756466A (en) * 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5510369A (en) * 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
SE9404196D0 (sv) * 1994-12-02 1994-12-02 Astra Ab New antithrombotic formulation
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
US5721214A (en) * 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
US6022861A (en) * 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6046169A (en) * 1995-06-07 2000-04-04 Cor Therapeutics, Inc. Inhibitors of factor XA
US5843904A (en) * 1995-12-20 1998-12-01 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1βconverting enzyme
TWI238827B (en) 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
HU222199B1 (hu) * 1996-06-05 2003-05-28 Gyógyszerkutató Intézet Kft. Véralvadásgátló hatású peptid-aldehid-származékok és a vegyületeket tartalmazó gyógyszerkészítmények
US6245743B1 (en) 1996-06-05 2001-06-12 Cor Therapeutics, Inc. Inhibitors of factor Xa
HU224315B1 (hu) * 1996-06-05 2005-07-28 Gyógyszerkutató Intézet Kft. Véralvadásgátló hatású peptidil-arginin-aldehid-származékok és a vegyületeket tartalmazó gyógyszerkészítmények
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
JP2001525823A (ja) 1997-05-15 2001-12-11 イーライ・リリー・アンド・カンパニー 抗血栓化合物
EP1051431A1 (de) 1998-01-26 2000-11-15 Basf Aktiengesellschaft Thrombininhibitoren
KR100377557B1 (ko) * 1999-02-12 2003-03-26 주식회사 엘지생명과학 아실 구아니딘 작용기를 갖는 선택적 트롬빈 억제제
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
AU2002230836A1 (en) 2000-12-18 2002-07-01 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
CA2436176A1 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
US20050070480A1 (en) * 2001-08-21 2005-03-31 Sandor Bajusz Peptide arginals and methods for treating disseminated intravascular coagulation
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds

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Publication number Priority date Publication date Assignee Title
HU178398B (en) * 1979-06-12 1982-04-28 Gyogyszerkutato Intezet Process for producing new agmatine derivatives of activity against haemagglutination
HU192646B (en) * 1984-12-21 1987-06-29 Gyogyszerkutato Intezet Process for preparing new n-alkyl-peptide aldehydes
DE68923572T2 (de) * 1988-03-28 1996-01-18 British Tech Group Peptide.
DE3827415A1 (de) * 1988-08-12 1990-02-15 Behringwerke Ag Peptidderivate, verfahren zu ihrer herstellung und ihre verwendung
GB8823480D0 (en) * 1988-10-06 1988-11-16 Ciba Geigy Ag Antidote

Also Published As

Publication number Publication date
IE913423A1 (en) 1992-04-08
EP0837071A1 (en) 1998-04-22
AU8478091A (en) 1992-04-02
DE69132884D1 (de) 2002-01-31
JP3023019B2 (ja) 2000-03-21
NO309984B1 (no) 2001-04-30
EP0684258A2 (en) 1995-11-29
CS291391A3 (en) 1992-04-15
EP0479489A2 (en) 1992-04-08
NZ239907A (en) 1993-07-27
CZ285980B6 (cs) 1999-12-15
EP0684258A3 (es) 1996-01-10
EP0479489B1 (en) 2003-03-19
CN1060472A (zh) 1992-04-22
NO913773D0 (no) 1991-09-26
ATE211147T1 (de) 2002-01-15
FI107733B (fi) 2001-09-28
CA2052013C (en) 2001-01-30
BR9104181A (pt) 1992-06-02
ATE234857T1 (de) 2003-04-15
RU2077538C1 (ru) 1997-04-20
KR920006369A (ko) 1992-04-27
HU913037D0 (en) 1992-01-28
HU217441B (hu) 2000-01-28
KR100219993B1 (ko) 1999-10-01
CN1036399C (zh) 1997-11-12
DE69132884T2 (de) 2002-08-22
DK0685489T3 (da) 2002-03-11
EP0479489A3 (en) 1993-10-13
EP0685489A2 (en) 1995-12-06
CA2052013A1 (en) 1992-03-29
HU211634A9 (en) 1995-12-28
NO913773L (no) 1992-03-30
JPH04257600A (ja) 1992-09-11
DE69133217T2 (de) 2004-02-05
FI914566A (fi) 1992-03-29
AU645347B2 (en) 1994-01-13
PT99068B (pt) 1999-02-26
IL99527A (en) 1997-08-14
ES2194835T3 (es) 2003-12-01
FI914566A0 (fi) 1991-09-27
PT99068A (pt) 1992-08-31
SK281731B6 (sk) 2001-07-10
HUT59162A (en) 1992-04-28
EP0685489B1 (en) 2001-12-19
DE69133217D1 (de) 2003-04-24
MX9101280A (es) 1992-05-04
EP0685489A3 (es) 1996-01-10

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