RU2075481C1 - Производные борсодержащих пептидов и фармацевтическая композиция, обладающая ингибирующей активностью к трипсинподобным сериновым протеазам - Google Patents

Производные борсодержащих пептидов и фармацевтическая композиция, обладающая ингибирующей активностью к трипсинподобным сериновым протеазам Download PDF

Info

Publication number
RU2075481C1
RU2075481C1 SU915001319A SU5001319A RU2075481C1 RU 2075481 C1 RU2075481 C1 RU 2075481C1 SU 915001319 A SU915001319 A SU 915001319A SU 5001319 A SU5001319 A SU 5001319A RU 2075481 C1 RU2075481 C1 RU 2075481C1
Authority
RU
Russia
Prior art keywords
pro
mmol
formula
group
tmsal
Prior art date
Application number
SU915001319A
Other languages
English (en)
Russian (ru)
Inventor
Меттерних Райнер
Original Assignee
Сандос АГ
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 Сандос АГ filed Critical Сандос АГ
Application granted granted Critical
Publication of RU2075481C1 publication Critical patent/RU2075481C1/ru

Links

Images

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)
SU915001319A 1990-08-13 1991-08-12 Производные борсодержащих пептидов и фармацевтическая композиция, обладающая ингибирующей активностью к трипсинподобным сериновым протеазам RU2075481C1 (ru)

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
RU2075481C1 true RU2075481C1 (ru) 1997-03-20

Family

ID=10680563

Family Applications (1)

Application Number Title Priority Date Filing Date
SU915001319A RU2075481C1 (ru) 1990-08-13 1991-08-12 Производные борсодержащих пептидов и фармацевтическая композиция, обладающая ингибирующей активностью к трипсинподобным сериновым протеазам

Country Status (18)

Country Link
EP (1) EP0471651A3 (enExample)
JP (1) JP2539965B2 (enExample)
KR (1) KR920004416A (enExample)
AU (1) AU643312B2 (enExample)
CA (1) CA2048953A1 (enExample)
CS (1) CS248491A3 (enExample)
FI (1) FI913788A7 (enExample)
GB (1) GB9017694D0 (enExample)
HU (1) HUT59161A (enExample)
IE (1) IE912841A1 (enExample)
IL (1) IL99163A (enExample)
MX (1) MX9100628A (enExample)
MY (1) MY106529A (enExample)
NZ (1) NZ239359A (enExample)
PT (1) PT98638B (enExample)
RU (1) RU2075481C1 (enExample)
TW (1) TW275634B (enExample)
ZA (1) ZA916393B (enExample)

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.
DE69314169T2 (de) * 1992-04-16 1998-01-15 Zeneca Ltd Peptide mit eine alphaaminoboronaire gruppe and ihre verwendung als elastasehemmer
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
US5563127A (en) * 1993-03-24 1996-10-08 The Dupont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
WO1994021650A1 (en) * 1993-03-24 1994-09-29 The Du Pont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
US5783563A (en) * 1993-06-03 1998-07-21 Astra Aktiebolag Method for treatment or prophylaxis of venous thrombosis
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
EP0722449A1 (en) * 1993-10-07 1996-07-24 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
CZ245797A3 (cs) * 1995-02-17 1998-06-17 Basf Aktiengesellschaft Derivát amidinu dipeptidu jako inhibitor thrombinu
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
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
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
CA2268270A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Heterocyclic derivatives as factor xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
CA2268381A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Selective factor xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
CA2268264A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Selective factor xa inhibitors
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
EP0975625A1 (en) 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
CA2285659A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
CA2285705A1 (en) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
EP0977772A1 (en) 1997-04-14 2000-02-09 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
IL133526A0 (en) 1997-06-19 2001-04-30 Du Pont Pharm Co Inhibitors of factor xa with a neutral p1 specificity group
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
ATE357509T1 (de) 1997-09-29 2007-04-15 Point Therapeutics Inc Stimulierung von hämatopoietischen zellen im vitro
KR100689923B1 (ko) 1998-01-26 2007-03-09 애보트 게엠베하 운트 콤파니 카게 트롬빈 억제제
CA2333927A1 (en) 1998-04-01 1999-10-07 Dupont Pharmaceuticals Company Pyrimidines and triazines as integrin antagonists
IL139247A0 (en) 1998-05-04 2001-11-25 Point Therapeutics Inc Hematopoietic stimulation
NZ508642A (en) 1998-06-05 2003-10-31 Point Therapeutics Inc Cyclic boroproline compounds
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa 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
WO2002050056A1 (en) 2000-12-18 2002-06-27 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
JP2005504003A (ja) 2001-02-09 2005-02-10 メルク　エンド　カムパニー　インコーポレーテッド トロンビン阻害剤
CN100415770C (zh) 2001-05-30 2008-09-03 诺瓦提斯公司 2－{[n－(2－氨基－3－(杂芳基或芳基)丙酰基)－氨基酰基]－氨基}－烷基硼酸衍生物
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
US20050288253A1 (en) 2002-09-09 2005-12-29 Trigen Limited Boronic acid salts
EP1396270B1 (en) 2002-09-09 2006-05-10 Trigen Limited Boronic acid salts and use thereof in the preparation of medicaments for treating thrombosis
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CN109476637B (zh) 2016-06-21 2022-02-01 奥瑞恩眼科有限责任公司 杂环脯氨酰胺衍生物
WO2017222914A1 (en) 2016-06-21 2017-12-28 Inception 4, Inc. Carbocyclic prolinamide derivatives

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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Европейский патент N 0293881, кл. C 07 K 5/00, 1988. *

Also Published As

Publication number Publication date
HUT59161A (en) 1992-04-28
KR920004416A (ko) 1992-03-27
AU8179291A (en) 1992-02-20
JPH04330094A (ja) 1992-11-18
FI913788L (fi) 1992-02-14
EP0471651A3 (en) 1993-02-10
HU912541D0 (en) 1992-01-28
GB9017694D0 (en) 1990-09-26
ZA916393B (en) 1993-04-28
CA2048953A1 (en) 1992-02-14
PT98638B (pt) 1999-01-29
MX9100628A (es) 1994-02-28
AU643312B2 (en) 1993-11-11
EP0471651A2 (en) 1992-02-19
CS248491A3 (en) 1992-02-19
IL99163A0 (en) 1992-07-15
FI913788A7 (fi) 1992-02-14
IE912841A1 (en) 1992-02-26
JP2539965B2 (ja) 1996-10-02
FI913788A0 (fi) 1991-08-09
IL99163A (en) 1996-01-19
TW275634B (enExample) 1996-05-11
NZ239359A (en) 1993-09-27
MY106529A (en) 1995-06-30
PT98638A (pt) 1992-06-30

Similar Documents

Publication Publication Date Title
RU2075481C1 (ru) Производные борсодержащих пептидов и фармацевтическая композиция, обладающая ингибирующей активностью к трипсинподобным сериновым протеазам
US5288707A (en) Borolysine peptidomimetics
US5858979A (en) Inhibitors and substrates of thrombin
AU670381B2 (en) Thrombin inhibitors
US5672582A (en) Thrombin inhibitors
EP0688336B1 (en) Peptide boronic acid derivatives having protease inhibiting activity
EP0293881A2 (en) Peptide boronic acid inhibitors of trypsin-like proteases
EP0815123B1 (en) Beta-sheet mimetics and use thereof as protease inhibitors
WO1996030396A1 (en) β-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS
US5574014A (en) Inhibitors of trypsin-like enzymes
US5686419A (en) Basic α-aminoalkylphosphonate derivatives
US6313096B1 (en) Inhibitors of trypsin-like enzymes
US5648338A (en) Inhibitors and substrates of thrombin
US6387881B1 (en) Inhibitors and substrates of thrombin
NO300504B1 (no) Forbindelse og terapeutisk preparat omfattende denne
RO107661B1 (ro) Derivați peptidici, inhibitori ai serinproteazei și procedeu pentru prepararea acestora
PL167469B1 (pl) Sposób wytwarzania nowych peptydowych pochodnych kwasu borowego
HK1025777A (en) Inhibitors and substrates of thrombin