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AR006310A1 - Un inhibidor de la serina proteasa, una composicion farmaceutica que comprende dicho inhibidor y usos de dicho inhibidor - Google Patents

Un inhibidor de la serina proteasa, una composicion farmaceutica que comprende dicho inhibidor y usos de dicho inhibidor

Info

Publication number
AR006310A1
AR006310A1 ARP970100833A ARP970100833A AR006310A1 AR 006310 A1 AR006310 A1 AR 006310A1 AR P970100833 A ARP970100833 A AR P970100833A AR P970100833 A ARP970100833 A AR P970100833A AR 006310 A1 AR006310 A1 AR 006310A1
Authority
AR
Argentina
Prior art keywords
chr2
amino acid
inhibitor
r2ooc
optionally substituted
Prior art date
Application number
ARP970100833A
Other languages
English (en)
Original Assignee
Akzo Nobel Nv
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 Akzo Nobel Nv filed Critical Akzo Nobel Nv
Publication of AR006310A1 publication Critical patent/AR006310A1/es

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    • 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
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • C07K5/0222Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
    • 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
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • C07K5/06113Asp- or Asn-amino acid
    • 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
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un inhibidor de la serina proteasa que tiene la fórmula (I), que comprende: A es H, D, L alfa-hidroxiacetilo opcionalmente substituido, R1, R1-O-C(O)-.R1-C(O)-, R1-SO2-, R2OOC-(CHR2)m-SO2-, R2OOC-(CHR2)m-,H2NCO-(CHR2)m-, o un grupo N-protector,en donde R1 es seleccionado entre (1-12C), (2-12C)alquenilo, (2-12C)-alquinilo y (3-8C)cicloalquilo, grupos que pueden ser opcionalmente substituidos con (3-8C)cicloalquilo, (1-6C)-alcoxi, oxo, OH,COOH, CF3 o halógeno, y de (6-14C)arilo,(7-15 C)aralquilo y (8-1)aralquilo y (8-16)aralquenilo, cuyos grupos arilo pueden ser opcionalmentesubstituidos con (1-6C)alquilo, (3-8C)-cicloalquilo, (1-6C)alcoxi, OH, COOH, CF3 o halógeno; cada grupo R2 es independientemente H o tiene elmismosi gnificado que R1; m es 1, 2 o 3; B es un enlace, un aminoácido de la fórmula -NH-CH[(CH2)pC(O)OH]-C(O)- o un derivado éster del mismo y siendo pigual a 0, 1, 2 o 3, -N((1-12C)alquilo-CH2-CO-, -N((2-12C)-alquenilo-CH2-CO-,-N((2-12C)alquini lo)-CH2-CO-, -N(bencilo)-CH2-CO-, D-1-Tiq, D-3Tiq,D-Atc,Aic, D-1-Piq, D-3-Piq o un L- o D-aminoácido que tiene una cadena lateral hidrófoba, básica o neutra, aminoácido que puede estar opcionalmentesubstituido conN-(1-6C)alquilo; o A y B junto s son el residuo R3R4N-CHR5-C(O)- en donde R3 y R4 independientemente son R1, R-O-C(O)-, R1-C(O)-, R1-SO2-,R2OOC-(CHR2)m-SO2-, R2OOC-(CHR2)m-, H2NCO-(CHR2)m-, o un grupo N-protector, o uno de R3 y R4 estáconectado con R5 para formar un anillo d e 5 o 6miembros junto con N-C al cual están unidos, anillo que puede ser fusionado con un anillo de 6 miembros alifático o aromático; y R5 es unacadena lateral hidrófoba, básica o neutra; X es unL-aminoácido con una cadena lateral hidrófo ba, serina, treonina, un aminoácido cíclico que contiene
ARP970100833A 1996-03-01 1997-03-03 Un inhibidor de la serina proteasa, una composicion farmaceutica que comprende dicho inhibidor y usos de dicho inhibidor AR006310A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP96200543 1996-03-01

Publications (1)

Publication Number Publication Date
AR006310A1 true AR006310A1 (es) 1999-08-25

Family

ID=8223736

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP970100833A AR006310A1 (es) 1996-03-01 1997-03-03 Un inhibidor de la serina proteasa, una composicion farmaceutica que comprende dicho inhibidor y usos de dicho inhibidor

Country Status (25)

Country Link
US (1) US6410684B1 (es)
EP (1) EP0886647B1 (es)
JP (1) JP2000506837A (es)
KR (1) KR19990087415A (es)
CN (1) CN1212704A (es)
AR (1) AR006310A1 (es)
AT (1) ATE221080T1 (es)
AU (1) AU709330B2 (es)
BR (1) BR9707808A (es)
CA (1) CA2246246A1 (es)
CZ (1) CZ277898A3 (es)
DE (1) DE69714222T2 (es)
DK (1) DK0886647T3 (es)
ES (1) ES2180933T3 (es)
HU (1) HUP9900390A3 (es)
IL (1) IL120310A (es)
NO (1) NO983991L (es)
NZ (1) NZ331484A (es)
PL (1) PL328875A1 (es)
PT (1) PT886647E (es)
RU (1) RU2178419C2 (es)
TR (1) TR199801704T2 (es)
TW (1) TW442452B (es)
WO (1) WO1997031937A1 (es)
ZA (1) ZA971667B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUP9901187A3 (en) * 1996-02-13 1999-11-29 Akzo Nobel Nv Serine protease inhibitors
AU7292398A (en) 1997-05-15 1998-12-08 Eli Lilly And Company Antithrombotic compound
DK1073672T3 (da) 1998-04-30 2003-12-08 Agouron Pharma Antipicornavirale forbindelser, deres fremstilling og anvendelse
KR20010106444A (ko) * 1998-08-17 2001-11-29 존 더블류. 갈루치 2세 알파-케토 헤테로사이클을 포함하는 세린 프로테아제 억제제
AU3511500A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions
WO2000051624A2 (en) 1999-03-05 2000-09-08 The Trustees Of University Technology Corporation Methods and compositions useful in inhibiting apoptosis
US6849605B1 (en) 1999-03-05 2005-02-01 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of viral infections
CA2380647A1 (en) 1999-08-04 2001-02-15 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
BR0111727A (pt) 2000-06-14 2003-05-27 Agouron Pharma Compostos e composições antipicornavirais, seus usos farmacêuticos, e materiais para a sua sìntese
RU2003105221A (ru) * 2000-07-21 2004-09-20 Шеринг Корпорейшн (US) Новые пептиды, как ингибиторы ns3-серинпротеазы вируса гепатита с
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
CN102206247B (zh) 2000-07-21 2013-03-27 默沙东公司 一种具有HCV NS3/NS4a蛋白酶抑制活性的化合物
EP1358178A2 (en) 2001-01-30 2003-11-05 Bristol-Myers Squibb Company Sulfonamide lactam inhibitors of factor xa
US7405210B2 (en) * 2003-05-21 2008-07-29 Osi Pharmaceuticals, Inc. Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
WO2005085245A1 (en) 2004-03-08 2005-09-15 Prosidion Limited Pyrrolopyridine-2-carboxylic acid hydrazides
ATE424821T1 (de) 2004-12-02 2009-03-15 Prosidion Ltd Pyrrolopyridin-2-karbonsäureamide
EP2344531B1 (en) * 2008-10-15 2014-12-10 Danisco US Inc. Modified variant bowman birk protease inhibitors
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
MX392422B (es) 2016-06-21 2025-03-24 Orion Ophthalmology LLC Derivados de prolinamida heterociclica
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds

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US4556655A (en) * 1984-09-24 1985-12-03 Schering Corporation Antihypertensive compounds having both diuretic and angiotensin converting enzyme inhibitory activity
CA2008116C (en) * 1989-02-23 2001-11-20 Thomas Weller Glycine derivatives
ZW11290A1 (en) * 1989-07-14 1990-10-31 Smithkline Beecham Corp Hemoregulatory peptides
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US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
ZA951617B (en) * 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
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Also Published As

Publication number Publication date
ATE221080T1 (de) 2002-08-15
WO1997031937A1 (en) 1997-09-04
NO983991L (no) 1998-10-30
ES2180933T3 (es) 2003-02-16
HK1021541A1 (en) 2000-06-16
CZ277898A3 (cs) 1999-06-16
EP0886647A1 (en) 1998-12-30
TR199801704T2 (xx) 1998-12-21
JP2000506837A (ja) 2000-06-06
DK0886647T3 (da) 2002-11-04
PT886647E (pt) 2002-12-31
KR19990087415A (ko) 1999-12-27
CN1212704A (zh) 1999-03-31
IL120310A0 (en) 1997-06-10
AU1877597A (en) 1997-09-16
ZA971667B (en) 1997-09-10
IL120310A (en) 2002-02-10
NZ331484A (en) 2000-01-28
HUP9900390A3 (en) 2000-11-28
US6410684B1 (en) 2002-06-25
RU2178419C2 (ru) 2002-01-20
DE69714222T2 (de) 2003-02-20
PL328875A1 (en) 1999-03-01
DE69714222D1 (de) 2002-08-29
BR9707808A (pt) 1999-07-27
HUP9900390A2 (hu) 1999-06-28
AU709330B2 (en) 1999-08-26
NO983991D0 (no) 1998-08-31
EP0886647B1 (en) 2002-07-24
TW442452B (en) 2001-06-23
CA2246246A1 (en) 1997-09-04

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