JP2539965B2 - 有機化学における改良 - Google Patents

有機化学における改良

Info

Publication number
JP2539965B2
JP2539965B2 JP3201750A JP20175091A JP2539965B2 JP 2539965 B2 JP2539965 B2 JP 2539965B2 JP 3201750 A JP3201750 A JP 3201750A JP 20175091 A JP20175091 A JP 20175091A JP 2539965 B2 JP2539965 B2 JP 2539965B2
Authority
JP
Japan
Prior art keywords
formula
mmol
compound
boc
alkyl
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.)
Expired - Lifetime
Application number
JP3201750A
Other languages
English (en)
Japanese (ja)
Other versions
JPH04330094A (ja
Inventor
ライナー・メッテルニッヒ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sandoz AG
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 JPH04330094A publication Critical patent/JPH04330094A/ja
Application granted granted Critical
Publication of JP2539965B2 publication Critical patent/JP2539965B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime 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)
JP3201750A 1990-08-13 1991-08-12 有機化学における改良 Expired - Lifetime JP2539965B2 (ja)

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 (2)

Publication Number Publication Date
JPH04330094A JPH04330094A (ja) 1992-11-18
JP2539965B2 true JP2539965B2 (ja) 1996-10-02

Family

ID=10680563

Family Applications (1)

Application Number Title Priority Date Filing Date
JP3201750A Expired - Lifetime JP2539965B2 (ja) 1990-08-13 1991-08-12 有機化学における改良

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
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.
WO1993021214A1 (en) * 1992-04-16 1993-10-28 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.
MY131622A (en) * 1993-03-03 2007-08-30 Novartis Ag Organic compounds
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
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
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
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
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
AU7922794A (en) * 1993-10-07 1995-05-01 Du Pont Merck Pharmaceutical Company, The 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
BR9607582A (pt) * 1995-02-17 1998-07-07 Basf Ag Composto e peptídeo ou substância peptidomimética
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
EA000966B1 (ru) 1995-07-26 2000-08-28 Мицубиси Кемикал Корпорейшн Производные пеницилламинамида
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
WO1998016547A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
CA2268264A1 (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
WO1998016524A1 (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
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 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
EP0975625A1 (en) 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
US6204268B1 (en) 1997-04-14 2001-03-20 Cor Therapeutics, Inc Selective factor Xa inhibitors
WO1998046627A1 (en) 1997-04-14 1998-10-22 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
AU8150398A (en) 1997-06-19 1999-01-04 Du Pont Pharmaceuticals Company Inhibitors of factor xa with a neutral p1 specificity group
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
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
ES2285785T3 (es) 1997-09-29 2007-11-16 Point Therapeutics, Inc. Estimulacion de celulas hematopoyeticas in vitro.
HUP0100082A3 (en) 1998-01-26 2001-12-28 Abbott Gmbh & Co Kg Thrombin inhibitor, peptide derivatives, pharmaceutical compositions comprising thereof and their use
CA2333927A1 (en) 1998-04-01 1999-10-07 Dupont Pharmaceuticals Company Pyrimidines and triazines as integrin antagonists
US6300314B1 (en) 1998-05-04 2001-10-09 Point Therapeutics, Inc. Hematopoietic stimulation
AU765370B2 (en) 1998-06-05 2003-09-18 Point Therapeutics, Inc. Cyclic boroproline compounds
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
CA2348740A1 (en) 1998-12-23 2000-07-06 Ruth R. Wexler Thrombin or factor xa 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
CA2431588A1 (en) 2000-12-18 2002-06-27 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. 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
EP1399468B1 (en) 2001-05-30 2006-02-15 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
JP2006511593A (ja) 2002-09-09 2006-04-06 トライジェン・リミテッド ボロン酸塩および血栓症の治療におけるその使用
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
DK3472149T3 (da) 2016-06-21 2023-11-27 Orion Ophthalmology LLC Heterocykliske prolinamidderivater
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC CARBOCYCLIC PROLINAMIDE DERIVATIVES

Citations (2)

* 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

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Patent Citations (2)

* 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

Non-Patent Citations (10)

* Cited by examiner, † Cited by third party
Title
ＢＩＯＣＨＩＭ．ＢＩＯＰＨＹＳ．ＡＣＴＡ１４８〜２！（１９６７）Ｐ．４１４−４２２
ＣＨＥＭ．ＢＥＲ．１０８〜９！（１９７５）Ｐ．３０７９−３０９０
ＨＥＬＶ．ＣＨＩＭ．ＡＣＴＡ６２〜４！（１９７９）Ｐ．９５６−９６４
ＨＥＬＶ．ＣＨＩＭ．ＡＣＴＡ６４〜７！（１９８１）Ｐ．２０８４−２０８９
ＩＮＴ．Ｊ．ＰＥＰＴ．ＰＲＯＴＥＩＮＲＥＳ．３０〜１！（１９８７）Ｐ．１３−２１
Ｊ．ＣＨＥＭ．ＳＯＣ．，ＤＡＬＴＯＮＴＲＡＮＳ．（１９８５）〜１！Ｐ．１７−２６
Ｊ．ＭＥＤ．ＣＨＥＭ．１１〜２！（１９６８）Ｐ．４０２−４０３
ＬＡＮＧＭＵＩＲ６〜１！（１９９０）Ｐ．１７７−１８２
ＰＥＰＴ．，ＰＲＯＣ．ＥＵＲ．ＰＥＰＴ．ＳＹＭＰ．，１７ＴＨ（１９８３）Ｐ．３３３−３３６
ＴＥＴＲＡＨＥＤＲＯＮ４４〜１７！（１９８８）Ｐ．５２７７−５２９２

Also Published As

Publication number Publication date
PT98638A (pt) 1992-06-30
IL99163A0 (en) 1992-07-15
CS248491A3 (en) 1992-02-19
HUT59161A (en) 1992-04-28
RU2075481C1 (ru) 1997-03-20
JPH04330094A (ja) 1992-11-18
FI913788L (fi) 1992-02-14
ZA916393B (en) 1993-04-28
KR920004416A (ko) 1992-03-27
IE912841A1 (en) 1992-02-26
EP0471651A3 (en) 1993-02-10
HU912541D0 (en) 1992-01-28
FI913788A7 (fi) 1992-02-14
IL99163A (en) 1996-01-19
AU643312B2 (en) 1993-11-11
MX9100628A (es) 1994-02-28
NZ239359A (en) 1993-09-27
PT98638B (pt) 1999-01-29
GB9017694D0 (en) 1990-09-26
CA2048953A1 (en) 1992-02-14
FI913788A0 (fi) 1991-08-09
MY106529A (en) 1995-06-30
TW275634B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 1996-05-11
AU8179291A (en) 1992-02-20
EP0471651A2 (en) 1992-02-19

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