KR920004416A - 트롬빈 저해활성을 가지고 있는 화합물 - Google Patents

트롬빈 저해활성을 가지고 있는 화합물 Download PDF

Info

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
Other languages
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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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 (OSRAM)
JP (1) JP2539965B2 (OSRAM)
KR (1) KR920004416A (OSRAM)
AU (1) AU643312B2 (OSRAM)
CA (1) CA2048953A1 (OSRAM)
CS (1) CS248491A3 (OSRAM)
FI (1) FI913788L (OSRAM)
GB (1) GB9017694D0 (OSRAM)
HU (1) HUT59161A (OSRAM)
IE (1) IE912841A1 (OSRAM)
IL (1) IL99163A (OSRAM)
MX (1) MX9100628A (OSRAM)
MY (1) MY106529A (OSRAM)
NZ (1) NZ239359A (OSRAM)
PT (1) PT98638B (OSRAM)
RU (1) RU2075481C1 (OSRAM)
TW (1) TW275634B (OSRAM)
ZA (1) ZA916393B (OSRAM)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5574014A (en) * 1988-04-28 1996-11-12 Thrombosis Research Institute Inhibitors of trypsin-like enzymes
US6313096B1 (en) 1988-04-28 2001-11-06 Trigen Limited 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.
CA2133657A1 (en) * 1992-04-16 1993-10-28 Peter R. Bernstein Substituted derivatives
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.
AU677297B2 (en) * 1993-03-03 1997-04-17 Novartis Ag Peptide boronic acid derivatives 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
US5780631A (en) * 1993-06-03 1998-07-14 Astra Aktiebolag Starting materials in the synthesis of thrombin and kininogenase inhibitors
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
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
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
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
WO1995009859A1 (en) * 1993-10-07 1995-04-13 The Du Pont Merck Pharmaceutical Company Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring
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
PL321759A1 (en) * 1995-02-17 1997-12-22 Basf Ag Novel thrombosin inhibitors
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
ATE226192T1 (de) 1995-07-26 2002-11-15 Mitsubishi Chem Corp Penizillaminamid-derivate
GB9515489D0 (en) * 1995-07-28 1995-09-27 Sandoz Ltd Organic compounds
TWI238827B (en) 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
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
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
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
CA2268381A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Selective factor xa inhibitors
US6063794A (en) * 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
CA2268270A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Heterocyclic derivatives as 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
US6133256A (en) * 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
NZ500354A (en) 1997-04-14 2001-11-30 Cor Therapeutics Inc Cyclic diaza compounds as selective factor Xa inhibitors for treating thrombotic related disorders
CA2285685A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
CA2285659A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
US6100234A (en) * 1997-05-07 2000-08-08 Tufts University Treatment of HIV
US6040145A (en) 1997-05-07 2000-03-21 Tufts University Potentiation of the immune response
HUP0003906A2 (hu) 1997-06-19 2001-05-28 Du Pont Pharmaceuticals Co. Xa faktort gátló hatású heterociklusos vegyületek és ezeket tartalmazó gyógyszerkészítmények
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
CN1163594C (zh) 1997-09-29 2004-08-25 尖端医疗有限公司 体外造血细胞的刺激
AU751111B2 (en) 1998-01-26 2002-08-08 Basf Aktiengesellschaft Thrombin inhibitors
JP2003504301A (ja) 1998-04-01 2003-02-04 ブリストル−マイヤーズ スクイブ ファーマ カンパニー インテグリンアンタゴニスト
AU770319C (en) 1998-05-04 2004-11-25 Point Therapeutics, Inc. Hematopoietic stimulation
JP2002517401A (ja) 1998-06-05 2002-06-18 ポイント セラピューティクス， インコーポレイテッド 環状ボロプロリン化合物
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
WO2000038683A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
WO2002048157A2 (en) * 2000-12-13 2002-06-20 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
CA2431588A1 (en) 2000-12-18 2002-06-27 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
CA2436176A1 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
ATE317850T1 (de) 2001-05-30 2006-03-15 Novartis Pharma Gmbh 2-((n-(2-amino-3-(heteroaryl- oder - aryl)propionyl)aminoacyl)amino)- alkylboronsäurederivate
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
US7371729B2 (en) 2002-09-09 2008-05-13 Trigen Limited Boronic acid salts useful in parenteral formulations
AU2003263333A1 (en) * 2002-09-09 2004-03-29 Trigen Limited Multivalent metal salts of boronic acids for treating thrombosis
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC CARBOCYCLIC PROLINAMIDE DERIVATIVES
ES2971784T3 (es) 2016-06-21 2024-06-07 Orion Ophthalmology LLC Derivados heterocíclicos de prolinamida

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

Similar Documents

Publication Publication Date Title
KR920004416A (ko) 트롬빈 저해활성을 가지고 있는 화합물
US5288707A (en) Borolysine peptidomimetics
US5187157A (en) Peptide boronic acid inhibitors of trypsin-like proteases
AU743735B2 (en) Selective factor Xa inhibitors
US5250720A (en) Intermediates for preparing peptide boronic acid inhibitors of trypsin-like proteases
AU677297B2 (en) Peptide boronic acid derivatives having protease inhibiting activity
HU913037D0 (en) Tripeptide dericatives having anti-thrombotic effect and method for producing same
IL113505A (en) Factor xa inhibitors and pharmaceutical compositions containing same
TW360632B (en) Octacyclodepsipeptides having an endoparasiticidal action
KR930007972A (ko) 환상 혈관활성 펩티드
CA2431487A1 (en) Oligo or polyalkylene glycol-coupled thrombin inhibitors
AU735722B2 (en) Peptidomimetics containing 6-peptidylamino-1-naphthalenesulfonamide moieties
CA2051115A1 (en) 4h-3,1-benzoxazin-4-one compounds and their pharmaceutical compositions for inhibiting elastase
KR970700664A (ko) 신규 인체 백혈구 엘라스타제의 억제제 및 관련 약제학적 조성물 및 사용방법(novel human leukocyte elastase (hle) inhibitors, and related pharmaceutical compositions and methods of use)
JPS6490164A (en) Novel spergualin-related compound and production thereof
CA1333208C (en) Peptide boronic acid inhibitors of trypsin-like proteases
JPH053880B2 (OSRAM)
RO107661B1 (ro) Derivați peptidici, inhibitori ai serinproteazei și procedeu pentru prepararea acestora
HUP0003500A2 (hu) Adhézió inhibitor ciklopeptidszármazékok, azokat tartalmazó gyógyszerkészítmények, eljárás előállításukra, és alkalmazásuk

Legal Events

Date Code Title Description
PA0109 Patent application

Patent event code: PA01091R01D

Comment text: Patent Application

Patent event date: 19910812

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 19960809

Comment text: Request for Examination of Application

Patent event code: PA02011R01I

Patent event date: 19910812

Comment text: Patent Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 19981104

Patent event code: PE09021S01D

E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 19990226

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 19981104

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I