DE69132884T2 - Tripeptidisches antithrombotisches Mittel - Google Patents

Tripeptidisches antithrombotisches Mittel

Info

Publication number
DE69132884T2
DE69132884T2 DE69132884T DE69132884T DE69132884T2 DE 69132884 T2 DE69132884 T2 DE 69132884T2 DE 69132884 T DE69132884 T DE 69132884T DE 69132884 T DE69132884 T DE 69132884T DE 69132884 T2 DE69132884 T2 DE 69132884T2
Authority
DE
Germany
Prior art keywords
group
amino
substituted
antithrombotic agent
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 - Fee Related
Application number
DE69132884T
Other languages
English (en)
Other versions
DE69132884D1 (de
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
Publication of DE69132884D1 publication Critical patent/DE69132884D1/de
Application granted granted Critical
Publication of DE69132884T2 publication Critical patent/DE69132884T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related 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
DE69132884T 1990-09-28 1991-09-26 Tripeptidisches antithrombotisches Mittel Expired - Fee Related DE69132884T2 (de)

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 (2)

Publication Number Publication Date
DE69132884D1 DE69132884D1 (de) 2002-01-31
DE69132884T2 true DE69132884T2 (de) 2002-08-22

Family

ID=27080589

Family Applications (2)

Application Number Title Priority Date Filing Date
DE69133217T Expired - Fee Related DE69133217T2 (de) 1990-09-28 1991-09-26 Antithrombotische Tripeptid-Wirkstoffe
DE69132884T Expired - Fee Related DE69132884T2 (de) 1990-09-28 1991-09-26 Tripeptidisches antithrombotisches Mittel

Family Applications Before (1)

Application Number Title Priority Date Filing Date
DE69133217T Expired - Fee Related DE69133217T2 (de) 1990-09-28 1991-09-26 Antithrombotische Tripeptid-Wirkstoffe

Country Status (22)

Country Link
EP (4) EP0684258A2 (de)
JP (1) JP3023019B2 (de)
KR (1) KR100219993B1 (de)
CN (1) CN1036399C (de)
AT (2) ATE234857T1 (de)
AU (1) AU645347B2 (de)
BR (1) BR9104181A (de)
CA (1) CA2052013C (de)
CZ (1) CZ285980B6 (de)
DE (2) DE69133217T2 (de)
DK (1) DK0685489T3 (de)
ES (2) ES2169105T3 (de)
FI (1) FI107733B (de)
HU (2) HU217441B (de)
IE (1) IE913423A1 (de)
IL (1) IL99527A (de)
MX (1) MX9101280A (de)
NO (1) NO309984B1 (de)
NZ (1) NZ239907A (de)
PT (1) PT99068B (de)
RU (1) RU2077538C1 (de)
SK (1) SK281731B6 (de)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US6008217A (en) * 1995-12-20 1999-12-28 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
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
JPH08501057A (ja) * 1992-03-04 1996-02-06 ヂョヂセルクタトー インテーゼット カーエフテー 新規な抗凝結因子ペプチド誘導体及びそれを含有する製薬学的組成物及びその製造方法
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
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
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
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
CA2143533A1 (en) * 1994-03-04 1995-09-05 Kenneth D. Kurz Antithrombotic agents
US5602101A (en) * 1994-03-04 1997-02-11 Eli Lilly And Company Antithrombotic agents
US5885967A (en) * 1994-03-04 1999-03-23 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
US5484772A (en) * 1994-03-04 1996-01-16 Eli Lilly And Company Antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5436229A (en) * 1994-03-04 1995-07-25 Eli Lilly And Company Bisulfite adducts of arginine aldehydes
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5488037A (en) * 1994-03-04 1996-01-30 Eli Lilly And Company Antithrombotic agents
IL112795A (en) * 1994-03-04 2001-01-28 Astrazeneca Ab Derivatives of peptides as antithrombotic drugs, their preparation, and pharmaceutical preparations containing them
JPH09509943A (ja) * 1994-03-04 1997-10-07 イーライ・リリー・アンド・カンパニー 抗血栓剤
GB2287027A (en) * 1994-03-04 1995-09-06 Lilly Co Eli Tripeptide antithrombotic agents
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
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated 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
US6046169A (en) * 1995-06-07 2000-04-04 Cor Therapeutics, Inc. Inhibitors of factor XA
US6069130A (en) * 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic 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
US5721214A (en) * 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
US5843904A (en) * 1995-12-20 1998-12-01 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1βconverting enzyme
TW541316B (en) 1995-12-21 2003-07-11 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
US6214841B1 (en) 1997-05-15 2001-04-10 Eli Lilly And Company Antithrombotic compound
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
WO2002050056A1 (en) 2000-12-18 2002-06-27 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
US7144899B2 (en) 2001-02-09 2006-12-05 Merck & Co., Inc. Thrombin inhibitors
WO2003016273A2 (en) * 2001-08-21 2003-02-27 Ivax Corporation 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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
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
GB2217331C (en) * 1988-03-28 1994-11-16 Nat Res Dev Oligopeptides and their use as analgesics
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
EP0479489A2 (de) 1992-04-08
AU645347B2 (en) 1994-01-13
ES2169105T3 (es) 2002-07-01
FI914566A (fi) 1992-03-29
ES2194835T3 (es) 2003-12-01
EP0685489A3 (de) 1996-01-10
CN1060472A (zh) 1992-04-22
CZ285980B6 (cs) 1999-12-15
PT99068A (pt) 1992-08-31
FI914566A0 (fi) 1991-09-27
HU913037D0 (en) 1992-01-28
EP0684258A3 (de) 1996-01-10
EP0684258A2 (de) 1995-11-29
CN1036399C (zh) 1997-11-12
NO309984B1 (no) 2001-04-30
HUT59162A (en) 1992-04-28
RU2077538C1 (ru) 1997-04-20
KR920006369A (ko) 1992-04-27
DE69132884D1 (de) 2002-01-31
HU217441B (hu) 2000-01-28
JPH04257600A (ja) 1992-09-11
DK0685489T3 (da) 2002-03-11
PT99068B (pt) 1999-02-26
IE913423A1 (en) 1992-04-08
ATE234857T1 (de) 2003-04-15
FI107733B (fi) 2001-09-28
NZ239907A (en) 1993-07-27
NO913773D0 (no) 1991-09-26
CA2052013A1 (en) 1992-03-29
IL99527A (en) 1997-08-14
EP0479489A3 (en) 1993-10-13
AU8478091A (en) 1992-04-02
CA2052013C (en) 2001-01-30
EP0685489A2 (de) 1995-12-06
ATE211147T1 (de) 2002-01-15
EP0685489B1 (de) 2001-12-19
KR100219993B1 (ko) 1999-10-01
JP3023019B2 (ja) 2000-03-21
EP0837071A1 (de) 1998-04-22
MX9101280A (es) 1992-05-04
SK281731B6 (sk) 2001-07-10
HU211634A9 (en) 1995-12-28
NO913773L (no) 1992-03-30
BR9104181A (pt) 1992-06-02
CS291391A3 (en) 1992-04-15
EP0479489B1 (de) 2003-03-19
DE69133217D1 (de) 2003-04-24
DE69133217T2 (de) 2004-02-05

Similar Documents

Publication Publication Date Title
DE69132884T2 (de) Tripeptidisches antithrombotisches Mittel
RU2075481C1 (ru) Производные борсодержащих пептидов и фармацевтическая композиция, обладающая ингибирующей активностью к трипсинподобным сериновым протеазам
HUP0002495A1 (hu) VLA-4 Által közvetített leukocita adhéziót gátló dipeptidszármazékok és rokon vegyületek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
MX9706069A (es) Nuevos inhibidores de la trombina.
HUP0003921A2 (hu) VLA-4 által közvetített leukocitaadhéziót gátló szulfonilezett dipeptidszármazékok, ezeket tartalmazó gyógyászati készítmények és alkalmazásuk
DK267686D0 (da) Difluorketonpeptidderivater og fremgangsmaade til fremstilling deraf samt midler indeholdende derivaterne
HUP0201088A2 (hu) Új alfa-aminosav-szulfonil-vegyületek, eljárás előállításukra és ilyen vegyületeket tartalmazó gyógyászati készítmények
EP0739886A3 (de) Selektive Thrombin-Hemmer
ES2081817T3 (es) Polipeptido con secuencias principales repetidas que se fijan en la celula.
DE69625505D1 (de) Guanidino proteiase inhibitoren
ATE99934T1 (de) Heteroaryl-3-oxo-propannitril-derivate, nuetzlich zur behandlung von rheumatoider arthritis und anderen autoimmunkrankheiten.
DK0775158T3 (da) Cyclopeptolider
MY111431A (en) Tripeptide antithrombotic agents
FR2756562B1 (fr) Nouveaux composes de n-benzenesulfonyl-l-proline, procede de preparation et utilisation en therapeutique
EA200000598A1 (ru) Новые ингибиторы металлопротеазы, способ их получения и содержащие их фармацевтические композиции
DK0868428T3 (da) Phosphonsyrederivater med metallopeptidaseinhiberende aktivitet
HUP0003500A2 (hu) Adhézió inhibitor ciklopeptidszármazékok, azokat tartalmazó gyógyszerkészítmények, eljárás előállításukra, és alkalmazásuk

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee