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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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
GB9017694 1990-08-13
GB909017694A GB9017694D0 (en) 1990-08-13 1990-08-13 Improvements in or relating to organic chemistry

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.
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.
ES2101516T3 (es) * 1993-03-03 1997-07-01 Ciba Geigy Ag Derivados peptidos de acido boronico que tienen actividad inhibidora de proteasas.
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
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
US5780631A (en) * 1993-06-03 1998-07-14 Astra Aktiebolag Starting materials in the synthesis of thrombin and kininogenase inhibitors
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
AU7922794A (en) * 1993-10-07 1995-05-01 Du Pont Merck Pharmaceutical Company, The Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring
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
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
KR100388185B1 (ko) * 1995-02-17 2003-11-28 애보트 게엠베하 운트 콤파니 카게 트롬빈 억제제로서의 신규 디펩티드 아미딘
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
AU725483B2 (en) 1995-07-26 2000-10-12 Mitsubishi Chemical Corporation Penicillaminamide derivatives
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
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. 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
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
AU743735B2 (en) * 1996-10-11 2002-02-07 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
AU6896298A (en) 1997-04-14 1998-11-11 Cor Therapeutics, Inc. Selective factor xa inhibitors
WO1998046591A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
US6133256A (en) * 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
EP0977773A1 (en) 1997-04-14 2000-02-09 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
PT991625E (pt) 1997-06-19 2005-10-31 Bristol Myers Squibb Pharma Co Inibidores de factor xa com um grupo de especificidade p1 neutro
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
IL135068A (en) 1997-09-29 2004-03-28 Point Therapeutics Inc Stimulation of hematopoietic cells in vitro
CN1289341A (zh) 1998-01-26 2001-03-28 Basf公司 凝血酶抑制剂
AU3213799A (en) 1998-04-01 1999-10-18 Du Pont Pharmaceuticals Company Integrin antagonists
KR20010052302A (ko) 1998-05-04 2001-06-25 바바라 피. 월너 조혈 자극
WO1999062914A1 (en) 1998-06-05 1999-12-09 Point Therapeutics, Inc. Cyclic boroproline compounds
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
EP1058549A4 (en) 1998-12-23 2003-11-12 Bristol Myers Squibb Pharma Co FACTOR Xa OR THROMBIN INHIBITORS
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
AU2002230764A1 (en) * 2000-12-13 2002-06-24 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
JP2004516286A (ja) 2000-12-18 2004-06-03 メルク エンド カムパニー インコーポレーテッド ベンジルアミン誘導体およびそれのトロンビン阻害薬としての使用
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
WO2002064559A2 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
WO2002096933A1 (en) 2001-05-30 2002-12-05 Novartis Ag 2-{[n-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid derivatives
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
DE60305113T2 (de) 2002-09-09 2006-12-07 Trigen Ltd. Borsäuresalze und deren Verwendung in der Bereitstellung von Medikamente für die Thrombosebehandlung
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
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
MX392422B (es) 2016-06-21 2025-03-24 Orion Ophthalmology LLC Derivados de prolinamida heterociclica

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

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
CA1333208C (en) Peptide boronic acid inhibitors of trypsin-like proteases
PL167469B1 (pl) Sposób wytwarzania nowych peptydowych pochodnych kwasu borowego
HK1025777A (en) Inhibitors and substrates of thrombin