TR199801704T2 - Serin proteaz inhibit�rleri. - Google Patents

Serin proteaz inhibit�rleri.

Info

Publication number
TR199801704T2
TR199801704T2 TR1998/01704T TR9801704T TR199801704T2 TR 199801704 T2 TR199801704 T2 TR 199801704T2 TR 1998/01704 T TR1998/01704 T TR 1998/01704T TR 9801704 T TR9801704 T TR 9801704T TR 199801704 T2 TR199801704 T2 TR 199801704T2
Authority
TR
Turkey
Prior art keywords
protease inhibitors
serine protease
compounds
prodrugs
formula
Prior art date
Application number
TR1998/01704T
Other languages
English (en)
Turkish (tr)
Inventor
Egbert Peter Adang Anton
Original Assignee
Akzo Nobel N.V.
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 N.V. filed Critical Akzo Nobel N.V.
Publication of TR199801704T2 publication Critical patent/TR199801704T2/xx

Links

Classifications

    • 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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (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)
TR1998/01704T 1996-03-01 1997-02-26 Serin proteaz inhibit�rleri. TR199801704T2 (xx)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
TR199801704T2 true TR199801704T2 (xx) 1998-12-21

Family

ID=8223736

Family Applications (1)

Application Number Title Priority Date Filing Date
TR1998/01704T TR199801704T2 (xx) 1996-03-01 1997-02-26 Serin proteaz inhibit�rleri.

Country Status (25)

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

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU719216B2 (en) * 1996-02-13 2000-05-04 Akzo Nobel N.V. Serine protease inhibitors
JP2001525823A (ja) 1997-05-15 2001-12-11 イーライ・リリー・アンド・カンパニー 抗血栓化合物
KR20010043004A (ko) 1998-04-30 2001-05-25 개리 이. 프라이드만 피코르나 바이러스 억제 화합물, 그의 제조 방법 및 용도
EP1105412A1 (en) * 1998-08-17 2001-06-13 Cortech, Inc. Serine protease inhibitors comprising alpha-keto heterocycles
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The 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
US6489308B1 (en) 1999-03-05 2002-12-03 Trustees Of University Of Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of nitric-oxide-induced clinical conditions
CN1372566A (zh) 1999-08-04 2002-10-02 阿格罗尼制药公司 抗细小核糖核酸病毒的化合物和组合物,它们的药物用途,及其合成原料
NZ523134A (en) 2000-06-14 2004-08-27 Agouron Pharma Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
WO2002008187A1 (en) 2000-07-21 2002-01-31 Schering Corporation Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
MXPA03000627A (es) 2000-07-21 2004-07-30 Schering Corp Nuevos peptidos como inhibidores de proteasa serina-ns3 del virus de la hepatitis c.
HUP0304058A2 (hu) 2001-01-30 2004-04-28 Bristol-Myers Squibb Company Xa faktor szulfonamid-laktám inhibitorok és alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
US7405210B2 (en) * 2003-05-21 2008-07-29 Osi Pharmaceuticals, Inc. Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
ES2353309T3 (es) 2004-03-08 2011-03-01 Prosidion Ltd. Hidrazidas del ácido pirrolopiridin-2-carboxílico como inhibidores de glucógeno fosforilasa.
ATE424821T1 (de) 2004-12-02 2009-03-15 Prosidion Ltd Pyrrolopyridin-2-karbonsäureamide
RU2509776C2 (ru) * 2008-10-15 2014-03-20 ДАНИСКО ЮЭс ИНК. МОДИФИЦИРОВАННЫЕ ВАРИАНТЫ ИНГИБИТОРОВ ПРОТЕАЗ Bowman Birk
EP4257191A3 (en) 2016-06-21 2023-11-22 Orion Ophthalmology LLC Heterocyclic prolinamide derivatives
WO2017222914A1 (en) 2016-06-21 2017-12-28 Inception 4, Inc. Carbocyclic prolinamide derivatives
WO2022013684A1 (en) 2020-07-11 2022-01-20 Pfizer Inc. Antiviral heteroaryl ketone derivatives
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
WO1994025051A1 (en) * 1993-04-30 1994-11-10 Merck & Co., Inc. Thrombin inhibitors
SE9301916D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
ZA951618B (en) 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
ZA951617B (en) 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
US5561146A (en) 1994-06-10 1996-10-01 Bristol-Myers Squibb Company Modified guanidino and amidino thrombin inhibitors
JPH10503176A (ja) * 1994-06-17 1998-03-24 コーバス インターナショナル, インコーポレイテッド 酵素インヒビターとしての3−アミノ−2−オキソ−1−ピペリジン酢酸誘導体
JPH0820597A (ja) * 1994-07-07 1996-01-23 Meiji Seika Kaisha Ltd トロンビン阻害作用を有する複素環カルボニル化合物
JPH11508535A (ja) * 1994-12-22 1999-07-27 バイオケム ファーマ インコーポレイテッド 低分子量2環式トロンビン阻害剤

Also Published As

Publication number Publication date
DE69714222D1 (de) 2002-08-29
BR9707808A (pt) 1999-07-27
PL328875A1 (en) 1999-03-01
CZ277898A3 (cs) 1999-06-16
WO1997031937A1 (en) 1997-09-04
HUP9900390A2 (hu) 1999-06-28
IL120310A (en) 2002-02-10
IL120310A0 (en) 1997-06-10
HK1021541A1 (en) 2000-06-16
ES2180933T3 (es) 2003-02-16
TW442452B (en) 2001-06-23
KR19990087415A (ko) 1999-12-27
PT886647E (pt) 2002-12-31
AU1877597A (en) 1997-09-16
AU709330B2 (en) 1999-08-26
AR006310A1 (es) 1999-08-25
DE69714222T2 (de) 2003-02-20
CA2246246A1 (en) 1997-09-04
EP0886647B1 (en) 2002-07-24
US6410684B1 (en) 2002-06-25
JP2000506837A (ja) 2000-06-06
HUP9900390A3 (en) 2000-11-28
ATE221080T1 (de) 2002-08-15
DK0886647T3 (da) 2002-11-04
CN1212704A (zh) 1999-03-31
RU2178419C2 (ru) 2002-01-20
NZ331484A (en) 2000-01-28
NO983991L (no) 1998-10-30
EP0886647A1 (en) 1998-12-30
ZA971667B (en) 1997-09-10
NO983991D0 (no) 1998-08-31

Similar Documents

Publication Publication Date Title
TR199801151T2 (xx) Trombin inhibit�r� �n ila�lar.
NZ331484A (en) Serine protease inhibitors having an alkynylamino side chain for use in treatment of thrombin related diseases
TR199801705T2 (xx) Serin proteaz inhibit�rleri.
TR199801569T2 (xx) Serin proteaz inhibit�rleri.
TR200103493T2 (tr) Metaloproteaz önleyicileri
TR200101120T2 (tr) Serin proteaz inhibitörü
EA200100675A1 (ru) Ингибиторы протеазы
MX9800146A (es) Nuevos inhibidores de trombina, su preparacion y su uso.
DE60023266D1 (de) Serinprotease-inhibitoren
EA199700186A1 (ru) Новые дипептидные амидины, используемые в качестве ингибиторов тромбина
ATE170169T1 (de) Retrovirale protease inhibitoren
SE9602646D0 (sv) Pharmaceutically-useful compounds
SE9602263D0 (sv) New amino acid derivatives
ATE260112T1 (de) Amidino proteaseinhibitoren
EE200000322A (et) Uued ühendid
IS5966A (is) Nýjar amídínóafleiður og notkun þeirra sem þrombínhemlar
SE0001803D0 (sv) New compounds i
IL154077A0 (en) New amidino derivatives and their use as thrombin inhibitors
SE0102921D0 (sv) Pharmaceutically useful compounds
DK0666755T3 (da) Inhibering af HIV-infektion
BR0211847A (pt) Composto ou um derivado farmaceuticamente aceitável do mesmo, formulação farmacêutica, uso do composto ou do derivado, métodos para tratar uma condição onde a inibição de trombina é requerida, e para tratar uma condição onde a terapia anticoagulante é indicada, e, processo para a preparação de um composto
TR200102914T2 (tr) Trombin önleyicilerinin önilaçları
DK0666841T3 (da) Succinoylamino-hydroxyethylaminosulfaminsyrederivater til anvendelse som inhibitorer af retrovirale proteaser
PT937075E (pt) Novas imidazo- e oxazolo-piridinas como inibidores da fosfodiesterese
GEP20032923B (en) Sulphonamide Derivatives as Prodrugs of Aspartyl Protease Inhibitors, Pharmaceutical compositions containing the Same and Methods for Treatment