KR920004416A - 트롬빈 저해활성을 가지고 있는 화합물 - Google Patents

트롬빈 저해활성을 가지고 있는 화합물 Download PDF

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Publication number
KR920004416A
KR920004416A KR1019910013860A KR910013860A KR920004416A KR 920004416 A KR920004416 A KR 920004416A KR 1019910013860 A KR1019910013860 A KR 1019910013860A KR 910013860 A KR910013860 A KR 910013860A KR 920004416 A KR920004416 A KR 920004416A
Authority
KR
South Korea
Prior art keywords
compound
formula
amino acid
alkyl
represented
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
KR1019910013860A
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English (en)
Korean (ko)
Inventor
레이너 메테르니히 닥터
Original Assignee
예안 크레이머, 한스 루돌프 하우스
산도즈 리미티즈
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 예안 크레이머, 한스 루돌프 하우스, 산도즈 리미티즈 filed Critical 예안 크레이머, 한스 루돌프 하우스
Publication of KR920004416A publication Critical patent/KR920004416A/ko
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1019910013860A 1990-08-13 1991-08-12 트롬빈 저해활성을 가지고 있는 화합물 Ceased KR920004416A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB909017694A GB9017694D0 (en) 1990-08-13 1990-08-13 Improvements in or relating to organic chemistry
GB9017694 1990-08-13

Publications (1)

Publication Number Publication Date
KR920004416A true KR920004416A (ko) 1992-03-27

Family

ID=10680563

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019910013860A Ceased KR920004416A (ko) 1990-08-13 1991-08-12 트롬빈 저해활성을 가지고 있는 화합물

Country Status (18)

Country Link
EP (1) EP0471651A3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (1) JP2539965B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR920004416A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU643312B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2048953A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CS (1) CS248491A3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
FI (1) FI913788A7 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
GB (1) GB9017694D0 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HU (1) HUT59161A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IE (1) IE912841A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (1) IL99163A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (1) MX9100628A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MY (1) MY106529A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NZ (1) NZ239359A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PT (1) PT98638B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
RU (1) RU2075481C1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
TW (1) TW275634B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ZA (1) ZA916393B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6313096B1 (en) 1988-04-28 2001-11-06 Trigen Limited Inhibitors of trypsin-like enzymes
US5574014A (en) * 1988-04-28 1996-11-12 Thrombosis Research Institute Inhibitors of trypsin-like enzymes
US6825169B1 (en) 1991-10-22 2004-11-30 Trustees Of Tufts College Inhibitors of dipeptidyl-aminopeptidase type IV
MX9206628A (es) * 1991-11-22 1993-05-01 Boehringer Ingelheim Pharma Ester de prolinaboronato y metodo para su preparacion.
AU3959693A (en) * 1992-04-16 1993-11-18 Zeneca Limited Alpha-aminoboronic acid peptides and their use as elastase inhibitors
FR2701951B1 (fr) * 1993-02-24 1995-06-09 Adir Nouveaux derives peptidiques de l'acide boronique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
NZ262415A (en) * 1993-03-03 1996-10-28 Sandoz Ltd Peptide boronic acid inhibitors having protease inhibiting activity
AU6448794A (en) * 1993-03-24 1994-10-11 Du Pont Merck Pharmaceutical Company, The Boronic acid and ester inhibitors of thrombin
US5563127A (en) * 1993-03-24 1996-10-08 The Dupont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
US5783563A (en) * 1993-06-03 1998-07-21 Astra Aktiebolag Method for treatment or prophylaxis of venous thrombosis
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
IL111175A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them
AU7922794A (en) * 1993-10-07 1995-05-01 Du Pont Merck Pharmaceutical Company, The Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring
IL111176A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Dipeptide boronic acid inhibitors of trypsin-like enzymes and pharmaceutical compositions containing them
US6060462A (en) * 1993-10-20 2000-05-09 Dupont Pharmaceuticals Company Electrophilic peptide analogs as inhibitors of trypsin-like enzymes
GB9401483D0 (en) * 1994-01-26 1994-03-23 Sandoz Ltd Organic compounds
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
FR2721611B1 (fr) * 1994-06-22 1996-09-27 Adir Nouveaux dérivés peptidiques de l'acide boronique, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent .
US5510369A (en) * 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
SE9404196D0 (sv) * 1994-12-02 1994-12-02 Astra Ab New antithrombotic formulation
EP0873356A1 (de) * 1995-02-17 1998-10-28 Basf Aktiengesellschaft Neue dipeptidische amidine als thrombin-inhibitoren
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
KR100445094B1 (ko) 1995-07-26 2005-06-17 미쓰비시 가가꾸 가부시키가이샤 페니실라민아미드유도체
GB9515489D0 (en) * 1995-07-28 1995-09-27 Sandoz Ltd Organic compounds
AR005245A1 (es) 1995-12-21 1999-04-28 Astrazeneca Ab Prodrogas de inhibidores de trombina, una formulación farmaceutica que las comprende, el uso de dichas prodrogas para la manufactura de un medicamento y un procedimiento para su preparacion
FR2745288B1 (fr) * 1996-02-27 1998-04-17 Adir Nouveaux derives de l'acide boronique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5965532A (en) * 1996-06-28 1999-10-12 Trustees Of Tufts College Multivalent compounds for crosslinking receptors and uses thereof
US6004955A (en) * 1996-08-15 1999-12-21 Dupont Pharmaceuticals Company Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
JP2001502674A (ja) * 1996-10-11 2001-02-27 シーオーアール・セラピューティックス・インコーポレーテッド 選択的Ｘａ因子阻害物質
WO1998016524A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. HETEROCYCLIC DERIVATIVES AS FACTOR Xa INHIBITORS
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
AU743735B2 (en) * 1996-10-11 2002-02-07 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
WO1998046591A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
EP0977773A1 (en) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
US6133256A (en) * 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
AU6896298A (en) 1997-04-14 1998-11-11 Cor Therapeutics, Inc. Selective factor xa inhibitors
US6040145A (en) 1997-05-07 2000-03-21 Tufts University Potentiation of the immune response
US6100234A (en) * 1997-05-07 2000-08-08 Tufts University Treatment of HIV
BR9810151A (pt) 1997-06-19 2000-08-08 Du Pont Pharm Co Composto, composição farmacêutica e método para tratamento ou prevenção de uma desordem tromoboembólica
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
DE69837393T2 (de) 1997-09-29 2007-12-06 Point Therapeutics, Inc., Boston Stimulierung von hämatopoietischen zellen im vitro
WO1999037668A1 (de) 1998-01-26 1999-07-29 Basf Aktiengesellschaft Thrombininhibitoren
EP1054871A2 (en) 1998-04-01 2000-11-29 Du Pont Pharmaceuticals Company Pyrimidines and triazines as integrin antagonists
TWI252107B (en) 1998-05-04 2006-04-01 Piint Therapeutics Inc Pharmaceutical compositions and kits for hematopoietic usage
EP1084129B1 (en) 1998-06-05 2003-01-22 Point Therapeutics, Inc. Cyclic boroproline compounds
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
EP1140862A4 (en) 1998-12-23 2004-07-28 Bristol Myers Squibb Pharma Co THROMBIN OR Xa FACTOR INHIBITORS
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
US6727366B2 (en) 2000-12-13 2004-04-27 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis C virus NS3 protease inhibitors
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
WO2002064559A2 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
PT1399468E (pt) 2001-05-30 2006-05-31 Novartis Ag Derivados do acido 2-{[n-(2-amino-3-(heteroaril ou aril)propionil)-aminoacil]-amino}-alquilboronico
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
PL376535A1 (pl) 2002-09-09 2006-01-09 Trigen Limited Sole kwasu boronowego i ich zastosowanie w leczeniu zakrzepicy
US7371729B2 (en) 2002-09-09 2008-05-13 Trigen Limited Boronic acid salts useful in parenteral formulations
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
PT3472149T (pt) 2016-06-21 2023-11-23 Orion Opthalmology Llc Derivados de prolinamida heterocíclicos
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3325478A (en) 1964-11-17 1967-06-13 Du Pont alpha-amino-1-adamantylmethyl penicillins
US4537907A (en) 1980-10-06 1985-08-27 University Of Illinois Foundation Hypnotic composition and method of inducing sleep
US5187157A (en) * 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
EP0315574A3 (de) * 1987-11-05 1990-08-22 Hoechst Aktiengesellschaft Renin-Inhibitoren
DE3827340A1 (de) * 1988-08-12 1990-02-15 Hoechst Ag Verwendung von (alpha)-aminoboronsaeure-derivaten zur prophylaxe und behandlung von viruserkrankungen
DE3840452A1 (de) * 1988-12-01 1990-06-07 Hoechst Ag (beta)-amino-boronsaeure-derivate

Also Published As

Publication number Publication date
PT98638A (pt) 1992-06-30
AU8179291A (en) 1992-02-20
ZA916393B (en) 1993-04-28
MX9100628A (es) 1994-02-28
FI913788L (fi) 1992-02-14
FI913788A7 (fi) 1992-02-14
IE912841A1 (en) 1992-02-26
MY106529A (en) 1995-06-30
HU912541D0 (en) 1992-01-28
GB9017694D0 (en) 1990-09-26
RU2075481C1 (ru) 1997-03-20
IL99163A0 (en) 1992-07-15
CS248491A3 (en) 1992-02-19
JPH04330094A (ja) 1992-11-18
EP0471651A3 (en) 1993-02-10
TW275634B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 1996-05-11
PT98638B (pt) 1999-01-29
NZ239359A (en) 1993-09-27
CA2048953A1 (en) 1992-02-14
EP0471651A2 (en) 1992-02-19
FI913788A0 (fi) 1991-08-09
HUT59161A (en) 1992-04-28
JP2539965B2 (ja) 1996-10-02
AU643312B2 (en) 1993-11-11
IL99163A (en) 1996-01-19

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