IL99163A - Peptides comprising c-terminal boronic acid derivatives having serine protease inhibiting activity their preparation and pharmaceutical compositions containing them - Google Patents

Peptides comprising c-terminal boronic acid derivatives having serine protease inhibiting activity their preparation and pharmaceutical compositions containing them

Info

Publication number
IL99163A
IL99163A IL9916391A IL9916391A IL99163A IL 99163 A IL99163 A IL 99163A IL 9916391 A IL9916391 A IL 9916391A IL 9916391 A IL9916391 A IL 9916391A IL 99163 A IL99163 A IL 99163A
Authority
IL
Israel
Prior art keywords
formula
compound
mmol
amino acid
boc
Prior art date
Application number
IL9916391A
Other languages
English (en)
Other versions
IL99163A0 (en
Original Assignee
Sandoz Ag
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 Sandoz Ag filed Critical Sandoz Ag
Publication of IL99163A0 publication Critical patent/IL99163A0/xx
Publication of IL99163A publication Critical patent/IL99163A/en

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)
IL9916391A 1990-08-13 1991-08-12 Peptides comprising c-terminal boronic acid derivatives having serine protease inhibiting activity their preparation and pharmaceutical compositions containing them IL99163A (en)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
IL99163A0 IL99163A0 (en) 1992-07-15
IL99163A true IL99163A (en) 1996-01-19

Family

ID=10680563

Family Applications (1)

Application Number Title Priority Date Filing Date
IL9916391A IL99163A (en) 1990-08-13 1991-08-12 Peptides comprising c-terminal boronic acid derivatives having serine protease inhibiting activity their preparation and pharmaceutical compositions containing them

Country Status (18)

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

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.
JPH07505877A (ja) * 1992-04-16 1995-06-29 ゼネカ・リミテッド α−アミノボロン酸ペプチド及びエラスターゼ阻害剤としてのそれらの使用
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.
WO1994021650A1 (en) * 1993-03-24 1994-09-29 The Du Pont Merck Pharmaceutical Company 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
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide 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
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
CA2174311A1 (en) * 1993-10-07 1995-04-13 Gregory James Pacofsky 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
FI973360L (fi) * 1995-02-17 1997-08-15 Basf Ag Uusia dipeptidisiä amidiineja trombiininestäjiksi
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
WO1997005108A1 (en) 1995-07-26 1997-02-13 Mitsubishi Chemical Corporation Penicillaminamide derivatives
GB9515489D0 (en) * 1995-07-28 1995-09-27 Sandoz Ltd Organic compounds
TW541316B (en) * 1995-12-21 2003-07-11 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
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
EP0932615A1 (en) * 1996-10-11 1999-08-04 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
CA2268270A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Heterocyclic derivatives as factor xa inhibitors
AU743544B2 (en) * 1996-10-11 2002-01-31 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
EP0975659A1 (en) * 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
EP0977773A1 (en) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
JP2001523226A (ja) 1997-04-14 2001-11-20 シーオーアール セラピューティクス インコーポレイテッド 選択的Ｘａ因子阻害剤
EP0975625A1 (en) 1997-04-14 2000-02-02 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
JP2002507968A (ja) 1997-06-19 2002-03-12 デュポン ファーマシューティカルズ カンパニー 中性のＰ１特異性基を有するＸａ因子阻害剤
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
KR100458403B1 (ko) 1997-09-29 2004-11-26 포인트 써러퓨틱스, 인크. 생체외 조혈세포의 자극방법
US6740647B1 (en) 1998-01-26 2004-05-25 Abbott Gmbh & Co., Kg Thrombin inhibitors
WO1999050249A2 (en) 1998-04-01 1999-10-07 Du Pont Pharmaceuticals Company Pyrimidines and triazines as integrin antagonists
JP2002513762A (ja) 1998-05-04 2002-05-14 ポイント セラピューティクス， インコーポレイテッド 造血刺激
DK1084129T3 (da) 1998-06-05 2003-05-19 Point Therapeutics Inc Cykliske boroProlinforbindelser
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
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin 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
WO2002064559A2 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
JP4416501B2 (ja) 2001-05-30 2010-02-17 ノバルティス アクチエンゲゼルシャフト ２−｛［ｎ−（２−アミノ−３−（ヘテロアリールまたはアリール）プロピオニル）−アミノアシル］−アミノ｝−アルキルボロン酸誘導体
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
DK1396270T3 (da) * 2002-09-09 2006-08-28 Trigen Ltd Borsyresalte
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
WO2017222914A1 (en) 2016-06-21 2017-12-28 Inception 4, Inc. Carbocyclic prolinamide derivatives
EP3472149B1 (en) 2016-06-21 2023-08-30 Orion Ophthalmology LLC Heterocyclic 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

Also Published As

Publication number Publication date
HUT59161A (en) 1992-04-28
CS248491A3 (en) 1992-02-19
ZA916393B (en) 1993-04-28
GB9017694D0 (en) 1990-09-26
PT98638B (pt) 1999-01-29
IL99163A0 (en) 1992-07-15
IE912841A1 (en) 1992-02-26
FI913788A0 (fi) 1991-08-09
HU912541D0 (en) 1992-01-28
TW275634B (cs) 1996-05-11
KR920004416A (ko) 1992-03-27
CA2048953A1 (en) 1992-02-14
MY106529A (en) 1995-06-30
JPH04330094A (ja) 1992-11-18
EP0471651A2 (en) 1992-02-19
FI913788L (fi) 1992-02-14
RU2075481C1 (ru) 1997-03-20
JP2539965B2 (ja) 1996-10-02
FI913788A7 (fi) 1992-02-14
MX9100628A (es) 1994-02-28
AU8179291A (en) 1992-02-20
NZ239359A (en) 1993-09-27
PT98638A (pt) 1992-06-30
AU643312B2 (en) 1993-11-11
EP0471651A3 (en) 1993-02-10

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