JP3171850B2 - アミジノ誘導体およびその一酸化窒素シンターゼ阻害剤としての使用 - Google Patents

アミジノ誘導体およびその一酸化窒素シンターゼ阻害剤としての使用

Info

Publication number
JP3171850B2
JP3171850B2 JP51127393A JP51127393A JP3171850B2 JP 3171850 B2 JP3171850 B2 JP 3171850B2 JP 51127393 A JP51127393 A JP 51127393A JP 51127393 A JP51127393 A JP 51127393A JP 3171850 B2 JP3171850 B2 JP 3171850B2
Authority
JP
Japan
Prior art keywords
acid
formula
group
pharmaceutically acceptable
compound
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 - Fee Related
Application number
JP51127393A
Other languages
English (en)
Japanese (ja)
Other versions
JPH07502512A (ja
Inventor
ビームズ、リチャード・マンスフィールド
ハドソン、ハロルド・フランシス
パーマー、リチャード・マイケル・ジョン
Original Assignee
ザ・ウエルカム・ファウンデーション・リミテッド
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 ザ・ウエルカム・ファウンデーション・リミテッド filed Critical ザ・ウエルカム・ファウンデーション・リミテッド
Publication of JPH07502512A publication Critical patent/JPH07502512A/ja
Application granted granted Critical
Publication of JP3171850B2 publication Critical patent/JP3171850B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/57Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C323/58Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/14Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Steroid Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
  • Cephalosporin Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicinal Preparation (AREA)
JP51127393A 1991-12-24 1992-12-23 アミジノ誘導体およびその一酸化窒素シンターゼ阻害剤としての使用 Expired - Fee Related JP3171850B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB919127376A GB9127376D0 (en) 1991-12-24 1991-12-24 Amidino derivatives
GB9127376.3 1991-12-24
PCT/GB1992/002387 WO1993013055A1 (en) 1991-12-24 1992-12-23 Amidino derivatives and their use as nitric oxide synthase inhibitors

Publications (2)

Publication Number Publication Date
JPH07502512A JPH07502512A (ja) 1995-03-16
JP3171850B2 true JP3171850B2 (ja) 2001-06-04

Family

ID=10706815

Family Applications (1)

Application Number Title Priority Date Filing Date
JP51127393A Expired - Fee Related JP3171850B2 (ja) 1991-12-24 1992-12-23 アミジノ誘導体およびその一酸化窒素シンターゼ阻害剤としての使用

Country Status (20)

Country Link
US (1) US5863931A (Direct)
EP (1) EP0618898B1 (Direct)
JP (1) JP3171850B2 (Direct)
AT (1) ATE178588T1 (Direct)
AU (1) AU669345B2 (Direct)
CA (1) CA2126327C (Direct)
CY (1) CY2197B1 (Direct)
DE (1) DE69228879T2 (Direct)
DK (1) DK0618898T3 (Direct)
ES (1) ES2130247T3 (Direct)
GB (1) GB9127376D0 (Direct)
GR (1) GR3030492T3 (Direct)
HU (1) HU217618B (Direct)
IL (1) IL104212A (Direct)
MY (1) MY109421A (Direct)
NZ (1) NZ246202A (Direct)
RU (1) RU2130014C1 (Direct)
TW (1) TW255881B (Direct)
WO (1) WO1993013055A1 (Direct)
ZA (1) ZA9210018B (Direct)

Families Citing this family (121)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9312761D0 (en) * 1993-06-21 1993-08-04 Wellcome Found Amino acid derivatives
US5424447A (en) * 1993-07-07 1995-06-13 The Medical College Of Wisconsin Research Foundation, Inc. Heme binding compounds and use thereof
IL110643A (en) * 1993-08-12 1998-07-15 Astra Ab Amidine derivatives their preparation and pharmaceutical compositions containing them
CN1071746C (zh) * 1993-08-12 2001-09-26 阿斯特拉公司 具有氧化氮合成酶活性的脒衍生物
US6225305B1 (en) 1993-10-04 2001-05-01 Glaxo Wellcome Inc. Substituted urea and isothiorea derivatives as no synthase inhibitors
US6297276B1 (en) 1993-10-04 2001-10-02 Glaxosmithkline Substituted urea and isothiourea derivatives as no synthase inhibitors
ATE177078T1 (de) 1993-10-21 1999-03-15 Searle & Co Amidino-derivate als no-synthetase inhibitoren
ATE222100T1 (de) * 1993-10-21 2002-08-15 Searle & Co Amidino-derivate nützlich als no synthase-hemmer
DE4337906A1 (de) * 1993-11-08 1995-05-11 Cassella Ag Verwendung von Cumarinderivaten
CA2176747A1 (en) * 1993-11-17 1995-05-26 J. Brice Weinberg Use of nitric oxide synthase inhibitors in the treatment of autoimmune diseases
GB9326136D0 (en) * 1993-12-22 1994-02-23 Erba Carlo Spa Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents
GB9404400D0 (en) * 1994-03-07 1994-04-20 Wood Pauline J Potentiation of bioreductive agents
ATE195933T1 (de) * 1994-03-10 2000-09-15 Searle & Co L-n6-(1-iminoethyl)lysin - derivate und ihre verwendung als no-synthase - inhibitoren
EP0751930B1 (en) * 1994-03-24 2000-01-05 G.D. SEARLE & CO. Amidino derivatives useful as nitric oxide synthase inhibitors
AU682768B2 (en) * 1994-05-07 1997-10-16 Astra Aktiebolag Bicyclic amidine derivatives as inhibitors of nitric oxide synthetase
PT957087E (pt) * 1994-06-15 2003-04-30 Wellcome Found Intermediarios uteis na preparacao de inibidores de enzimas
US6066333A (en) * 1994-09-22 2000-05-23 William Harvey Research Limited Pharmaceutical control of inflammation
AU723677B2 (en) * 1994-09-22 2000-08-31 William Harvey Research Limited Pharmaceutical control of inflammation
CA2132690A1 (en) * 1994-09-22 1996-03-23 Dean Willis Control and modulation of inflammatory response in humans in need of such control and modulation
US5684008A (en) * 1994-11-09 1997-11-04 G. D. Searle & Co. Aminotetrazole derivatives useful as nitric oxide synthase inhibitors
FR2727111B1 (fr) * 1994-11-21 1997-01-17 Hoechst Lab Nouveaux analogues soufres d'aminoacides, leur procede de preparation et leurs applications comme medicaments
JPH08333258A (ja) 1994-12-14 1996-12-17 Japan Tobacco Inc チアジン又はチアゼピン誘導体及びそれら化合物を含有してなる一酸化窒素合成酵素阻害剤
GB9425701D0 (en) * 1994-12-20 1995-02-22 Wellcome Found Enzyme inhibitors
WO1996021445A1 (en) * 1995-01-13 1996-07-18 The General Hospital Corporation Methods of inhibiting neurodegenerative diseases
KR100442561B1 (ko) * 1995-04-20 2004-10-14 지.디. 썰 엘엘씨 5산화2질소신타아제의억제제로유용한환상아미디노제
US5830917A (en) * 1995-09-11 1998-11-03 G. D. Searle & Co. L-N6 -(1-iminoethyl) lysine derivatives useful as nitric oxide synthase inhibitors
US5908842A (en) * 1995-12-08 1999-06-01 Merck & Co., Inc. Substituted 2-acylamino-pyridines as inhibitors of nitric oxide synthase
US5945408A (en) * 1996-03-06 1999-08-31 G.D. Searle & Co. Hydroxyanidino derivatives useful as nitric oxide synthase inhibitors
US5981511A (en) * 1996-03-06 1999-11-09 G.D. Searle & Co. Hydroxyamidino derivatives useful as nitric oxide synthase inhibitors
US6566330B1 (en) 1996-10-22 2003-05-20 Medical University Of South Carolina Foundation Research Development Positively charged non-natural amino acids, methods of making and using thereof in peptides
US6043218A (en) * 1996-10-22 2000-03-28 Medical University Of South Carolina Positively charged non-natural amino acids, methods of making thereof, and use thereof in peptides
US6090839A (en) * 1996-12-23 2000-07-18 Merck & Co., Inc. Antidiabetic agents
US6160000A (en) * 1996-12-23 2000-12-12 Merck & Co., Inc. Antidiabetic agents based on aryl and heteroarylacetic acids
US6369272B1 (en) 1997-01-13 2002-04-09 Glaxosmithkline Nitric oxide synthase inhibitors
US6620848B2 (en) 1997-01-13 2003-09-16 Smithkline Beecham Corporation Nitric oxide synthase inhibitors
MY117948A (en) * 1997-01-13 2004-08-30 Glaxo Group Ltd Nitride oxide synthase inhibitors.
FR2764889B1 (fr) * 1997-06-20 2000-09-01 Sod Conseils Rech Applic Nouveaux derives du 2-(iminomethyl)amino-phenyle, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
AU726861B2 (en) 1997-07-03 2000-11-23 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The Novel nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates, compositions and uses thereof and method of making same
US5981556A (en) * 1997-07-22 1999-11-09 G.D. Searle & Co. 1,3-diazolino and 1,3-diazolidino heterocycles as useful nitric oxide synthase inhibitors
CN1171861C (zh) * 1998-03-11 2004-10-20 G·D·西尔公司 用作一氧化氮合酶抑制剂的卤代脒基氨基酸衍生物
EP1067926A2 (en) * 1998-04-06 2001-01-17 Fujisawa Pharmaceutical Co., Ltd. Immunosuppressive imidazole derivatives and their combination preparations with tacrolimus or cyclosporins
GB9811599D0 (en) * 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
AU4821799A (en) 1998-06-10 1999-12-30 G.D. Searle & Co. Heterobicyclic and tricyclic nitric oxide synthase inhibitors
US6552052B2 (en) 1998-06-10 2003-04-22 Monsanto/G.D. Searle Pyrrolo[2,1-c][1,2,4] thiadiazoles and Pyrollo[2,1-c][1,12,4]oxadiazoles useful as nitric oxide synthase inhibitors
AU1704100A (en) 1998-09-08 2000-03-27 Monsanto Company Methods of treating osteoarthritis with inducible nitric oxide synthase inhibitors
AU2847200A (en) * 1999-01-27 2000-08-18 G.D. Searle & Co. Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors
ATE295832T1 (de) 2000-03-24 2005-06-15 Pharmacia Corp Amidino-verbindung sowie salze davon verwendbar als hemmstoffe der stickstoffmonoxid-synthase
US6956131B2 (en) 2000-04-13 2005-10-18 Pharmacia Corporation 2-amino-3, 4 heptenoic compounds useful as nitric oxide synthase inhibitors
US6787668B2 (en) 2000-04-13 2004-09-07 Pharmacia Corporation 2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
AR034120A1 (es) * 2000-04-13 2004-02-04 Pharmacia Corp Compuesto derivado halogenado del acido 2-amino-4,5 heptenoico, composicion farmaceutica que lo comprende y el uso de dicho compuesto y dicha composicion en la fabricacion de un medicamento para inhibir o modular la sintesis de acido nitrico
AR032318A1 (es) * 2000-04-13 2003-11-05 Pharmacia Corp Compuesto derivado halogenado del acido 2-amino-5,6 heptenoico; composicion farmaceutica que lo comprende y su uso en la fabricacion de un medicamento util como inhibidor de la oxido nitrico sintetasa
US6545170B2 (en) 2000-04-13 2003-04-08 Pharmacia Corporation 2-amino-5, 6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
AR030416A1 (es) 2000-04-13 2003-08-20 Pharmacia Corp COMPUESTO DERIVADO HALOGENADO DEL ACIDO 2-AMINO-3,4 HEPTENOICO, COMPOSICION FARMACEUTICA QUE LO COMPRENDE Y SU USO EN LA FABRICACION DE UN MEDICAMENTO uTIL COMO INHIBIDOR DE LA OXIDO NITRICO SINTETASA
US6344473B1 (en) 2000-08-07 2002-02-05 G.D. Searle & Co. Imidazoles useful as nitric oxide synthase inhibitors
AR031608A1 (es) * 2000-09-15 2003-09-24 Pharmacia Corp Derivados de los acidos 2-amino-2-alquil-3-hexenoico y -hexinoico utiles como inhibidores de oxido nitrico sintetasa
AR031129A1 (es) 2000-09-15 2003-09-10 Pharmacia Corp Derivados de los acidos 2-amino-2-alquil-4-hexenoico y -hexinoico utiles como inhibidores de oxido nitrico sintetasa
MY131964A (en) 2000-09-15 2007-09-28 Pharmacia Corp 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives useful as nitric oxide synthase inhibitors
ITTO20010110A1 (it) 2001-02-08 2002-08-08 Rotta Research Lab Nuovi derivati benzamidinici dotati di attivita' anti-infiammatoria ed immunosoppressiva.
US7012098B2 (en) 2001-03-23 2006-03-14 Pharmacia Corporation Inhibitors of inducible nitric oxide synthase for chemoprevention and treatment of cancers
US6673338B1 (en) 2001-09-10 2004-01-06 The United States Of America As Represented By The Department Of Health And Human Services Nitric oxide-releasing imidate and thioimidate diazeniumdiolates, compositions, uses thereof and method of making same
US20030109522A1 (en) * 2001-09-24 2003-06-12 Manning Pamela T. Ophthalmologic treatment methods using selective iNOS inhibitors
US6949530B2 (en) 2002-07-18 2005-09-27 The United States Of America As Represented By The Department Of Health And Human Services Nitric oxide-releasing amidine diazeniumdiolates, compositions and uses thereof and method of making same
WO2004012726A2 (en) * 2002-08-02 2004-02-12 Pharmacia Corporation Methods for treatment and prevention of gastrointestinal conditions
US6998503B2 (en) 2002-08-23 2006-02-14 Pharmacia Corporation Crystalline solid form of (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
RU2250897C1 (ru) * 2003-12-15 2005-04-27 Волгоградский государственный технический университет (ВолгГТУ) Способ получения адамантилсодержащих n-имидоилированных эфиров аминокарбоновых кислот
CA2552195C (en) 2003-12-30 2012-01-24 Vasopharm Biotech Gmbh 4-amino-7,8-dihydropteridines, pharmaceutical compositions containing them and their use for the treatment of diseases which are caused by an increased nitric oxide level
AR049384A1 (es) 2004-05-24 2006-07-26 Glaxo Group Ltd Derivados de purina
TWI307630B (en) 2004-07-01 2009-03-21 Glaxo Group Ltd Immunoglobulins
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
US7579335B2 (en) 2005-01-10 2009-08-25 Glaxo Group Limited Androstane 17α-carbonate derivatives for use in the treatment of allergic and inflammatory conditions
TW200724142A (en) 2005-03-25 2007-07-01 Glaxo Group Ltd Novel compounds
TWI389690B (zh) 2005-03-25 2013-03-21 Glaxo Group Ltd 新穎化合物(一)
GB0514809D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
TW200730498A (en) 2005-12-20 2007-08-16 Glaxo Group Ltd Compounds
RU2307121C1 (ru) * 2006-04-17 2007-09-27 Государственное образовательное учреждение высшего профессионального образования Волгоградский государственный технический университет (ВолгГТУ) Способ получения адамантилсодержащих n-имидоилированных производных аминокарбоновых кислот
EA200801997A1 (ru) 2006-04-20 2009-04-28 Глаксо Груп Лимитед Новые соединения
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
PL2046787T3 (pl) 2006-08-01 2011-10-31 Glaxo Group Ltd Związki pirazolo[3,4-b]pirydynowe i ich zastosowanie jako inhibitory PDE4
AR065804A1 (es) 2007-03-23 2009-07-01 Smithkline Beecham Corp Compuesto de indol carboxamida, composicion farmaceutica que lo comprende y uso de dicho compuesto para preparar un medicamento
AU2009325091A1 (en) 2008-05-23 2010-06-17 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein inhibitor
ATE552255T1 (de) 2008-06-05 2012-04-15 Glaxo Group Ltd 4-aminoindazole
US8163743B2 (en) 2008-06-05 2012-04-24 GlaxoGroupLimited 4-carboxamide indazole derivatives useful as inhibitors of PI3-kinases
WO2010094643A1 (en) 2009-02-17 2010-08-26 Glaxo Group Limited Quinoline derivatives and their uses for rhinitis and urticaria
EP2406255B1 (en) 2009-03-09 2015-04-29 Glaxo Group Limited 4-oxadiazol-2-yl-indazoles as inhibitors of pi3 kinases
EP2406249A1 (en) 2009-03-10 2012-01-18 Glaxo Group Limited Indole derivatives as ikk2 inhibitors
US20120058984A1 (en) 2009-03-17 2012-03-08 Catherine Mary Alder Pyrimidine derivatives used as itk inhibitors
US20120035247A1 (en) 2009-03-19 2012-02-09 Merck Sharp & Dohme Corp. RNA Interference Mediated Inhibition of Signal Transducer and Activator of Transcription 6 (STAT6) Gene Expression Using Short Interfering Nucleic Acid (siNA)
WO2010107955A2 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF BTB AND CNC HOMOLOGY 1, BASIC LEUCINE ZIPPER TRANSCRIPTION FACTOR 1 (BACH 1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) SEQUENCE LISTING
WO2010107952A2 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CONNECTIVE TISSUE GROWTH FACTOR (CTGF) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US20120029054A1 (en) 2009-03-19 2012-02-02 Merck Sharp & Dohme Corp. RNA Interference Mediated Inhibition of GATA Binding Protein 3 (GATA3) Gene Expression Using Short Intefering Nucleic Acid (siNA)
US20120022142A1 (en) 2009-03-27 2012-01-26 Merck Sharp & Dohme Corp. RNA Interference Mediated Inhibition of Signal Transducer and Activator of Transcription 1 (STAT1) Gene Expression Using Short Interfering Nucleic Acid (siNA)
JP2012521762A (ja) 2009-03-27 2012-09-20 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸(siNA)を用いた神経成長因子β鎖(NGFβ)遺伝子発現のRNA干渉媒介性阻害
EP2411516A1 (en) 2009-03-27 2012-02-01 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF APOPTOSIS SIGNAL-REGULATING KINASE 1 (ASK1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
MX2011010072A (es) 2009-03-27 2011-10-06 Merck Sharp & Dohme Inhibicion mediada por interferencia de acido ribonucleico de la expresion del gen de la molecula de adhesion intercelular 1 usando acido nucleico corto de interferencia.
EP2411520A2 (en) 2009-03-27 2012-02-01 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF THE THYMIC STROMAL LYMPHOPOIETIN (TSLP) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
JP2012524754A (ja) 2009-04-24 2012-10-18 グラクソ グループ リミテッド Cracチャネル阻害剤としてのピラゾールおよびトリアゾ−ルカルボキサミド
JP2012524755A (ja) 2009-04-24 2012-10-18 グラクソ グループ リミテッド Cracチャネル阻害剤としてのn−ピラゾリルカルボキサミド
JP5570589B2 (ja) 2009-04-30 2014-08-13 グラクソ グループ リミテッド Pi3キナーゼ阻害剤としてのオキサゾール置換インダゾール
WO2011067366A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
JP2013512879A (ja) 2009-12-03 2013-04-18 グラクソ グループ リミテッド Pi3キナーゼの阻害剤としてのベンズピラゾール誘導体
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
WO2011084316A2 (en) 2009-12-16 2011-07-14 3M Innovative Properties Company Formulations and methods for controlling mdi particle size delivery
WO2011110575A1 (en) 2010-03-11 2011-09-15 Glaxo Group Limited Derivatives of 2-[2-(benzo- or pyrido-) thiazolylamino]-6-aminopyridine, useful in the treatment of respiratoric, allergic or inflammatory diseases
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
WO2012032067A1 (en) 2010-09-08 2012-03-15 Glaxo Group Limited Polymorphs and salts of n- [5- [4- (5- { [(2r,6s) -2, 6 - dimethyl - 4 -morpholinyl] methyl} - 1, 3 - oxazol - 2 - yl) - 1h- inda zol-6-yl] -2- (methyloxy) - 3 - pyridinyl] methanesulfonamide
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
WO2012035055A1 (en) 2010-09-17 2012-03-22 Glaxo Group Limited Novel compounds
EP2630126B1 (en) 2010-10-21 2015-01-07 Glaxo Group Limited Pyrazole compounds acting against allergic, immune and inflammatory conditions
JP2013544794A (ja) 2010-10-21 2013-12-19 グラクソ グループ リミテッド アレルギー性障害、炎症性障害及び免疫障害に作用するピラゾール化合物
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
EP2683716A1 (en) 2011-03-11 2014-01-15 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
JP6494633B2 (ja) 2013-09-22 2019-04-03 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーCalitor Sciences, Llc 置換されているアミノピリミジン化合物および使用方法
WO2015148869A1 (en) 2014-03-28 2015-10-01 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
EP3142694A2 (en) 2014-05-12 2017-03-22 Glaxosmithkline Intellectual Property (No. 2) Limited Pharmaceutical compositions comprising danirixin for treating infectious diseases
US9938257B2 (en) 2015-09-11 2018-04-10 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
EP3710006A4 (en) 2017-11-19 2021-09-01 Sunshine Lake Pharma Co., Ltd. SUBSTITUTED HETEROARYL COMPOUNDS AND THEIR METHODS OF USE
EP3740468B1 (en) 2018-01-20 2025-12-31 Sunshine Lake Pharma Co., Ltd. Substituted Aminopyrimidine Compounds and Methods of Use
EP4125919A1 (en) 2020-03-26 2023-02-08 GlaxoSmithKline Intellectual Property Development Limited Cathepsin inhibitors for preventing or treating viral infections

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI832053L (fi) * 1982-06-10 1983-12-11 Syntex Inc Nonapeptid- och dekapeptidanaloger av lhrh anvaendbara som lhrh-antagonister samt deras framstaellningsfoerfarande
US5028627A (en) * 1989-09-13 1991-07-02 Cornell Research Foundation, Inc. Method of using arginine derivatives to inhibit systemic hypotension associated with nitric oxide production or endothelial derived relaxing factor
GB8929076D0 (en) * 1989-12-22 1990-02-28 Scras Treatment of shock by blocking agents of edrf effect or formation
CA2036770C (en) * 1990-02-26 2003-09-09 Jeffrey P. Whitten Inhibitors of nitric oxide biosynthesis

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Br.J.Pharmacol.,Vol.101,No.3(1990)p.746−p.752

Also Published As

Publication number Publication date
MY109421A (en) 1997-01-31
TW255881B (Direct) 1995-09-01
HUT70502A (en) 1995-10-30
GB9127376D0 (en) 1992-02-19
AU3169293A (en) 1993-07-28
ZA9210018B (en) 1994-06-23
EP0618898A1 (en) 1994-10-12
IL104212A0 (en) 1993-05-13
RU94031155A (ru) 1996-04-20
ATE178588T1 (de) 1999-04-15
ES2130247T3 (es) 1999-07-01
HU217618B (hu) 2000-03-28
GR3030492T3 (en) 1999-10-29
JPH07502512A (ja) 1995-03-16
EP0618898B1 (en) 1999-04-07
AU669345B2 (en) 1996-06-06
DK0618898T3 (da) 1999-10-18
DE69228879T2 (de) 1999-08-26
US5863931A (en) 1999-01-26
DE69228879D1 (de) 1999-05-12
CY2197B1 (en) 2002-11-08
CA2126327C (en) 2005-05-17
RU2130014C1 (ru) 1999-05-10
HU9401848D0 (en) 1994-09-28
NZ246202A (en) 1996-05-28
WO1993013055A1 (en) 1993-07-08
IL104212A (en) 1998-02-22
CA2126327A1 (en) 1993-07-08

Similar Documents

Publication Publication Date Title
JP3171850B2 (ja) アミジノ誘導体およびその一酸化窒素シンターゼ阻害剤としての使用
TWI843372B (zh) 用於降解突變kras蛋白之化合物及其應用
KR100430207B1 (ko) 효소억제제
RU2089550C1 (ru) Производное 1,4-бензотиазепина
ES2653717T3 (es) Pirazolil- y pirimidinil-enonas tricíclicas como moduladores antioxidantes de la inflamación
IL49786A (en) Furo(orthieno)(3,2-c)pyridinium derivatives their preparation and pharmaceutical compositions containing them
ES2367532T3 (es) Derivados de imidazolidina, sus usos, su preparación y composicones que los contienen.
HU219453B (hu) Fruktopiranóz-diacetálok imidátszármazékai és azokat hatóanyagként tartalmazó gyógyászati készítmények, valamint eljárás a készítmények előállítására
JPH09501651A (ja) Noシンターゼ阻害剤としてのアミノ酸誘導体
JPH09504524A (ja) 酸化窒素シンターゼ阻害剤として有用なアミジノ誘導体
MX2015002807A (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble.
JPH10508847A (ja) 酸化窒素合成酵素インヒビターとして有用なアミノテトラゾール誘導体
US3639477A (en) Novel propoxyguanidine compounds and means of producing the same
JP2026016715A (ja) 狂犬病治療のための環状アミド化合物およびその方法
HU199440B (en) Process for producing morpholine derivatives and pharmaceutical compositions comprising the compounds
AU2020401565A1 (en) Cystine diamide analogs for cystinuria
BG100326A (bg) Амиди на фенилциклохексилкарбоксилната киселина, метод за получаването им и тяхната употреба като лекарствени средства
ES2473792T3 (es) Compuestos cin�micos y derivados de los mismos para la inhibición de la histona desacetilasa
US3300510A (en) Hydantoins
IE51791B1 (en) Pharmaceutical compositions effective against coronary heart disease and hypertension
KR20180020119A (ko) 새로운 5형포스포디에스테라아제 억제제 및 그 용도
JPH08269013A (ja) ピラゾリジン誘導体及びラジカルスカベンジャー、脳梗塞抑制剤、脳浮腫抑制剤
EP4486738A1 (en) Small molecule inhibitors of enpp1
CZ297276B6 (cs) Derivát triazepinonu, zpusob jeho prípravy a farmaceutický prostredek, který ho obsahuje
GB2307911A (en) Substituted saturated aza heterocycle inhibitors of nitric oxide synthase

Legal Events

Date Code Title Description
R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20080323

Year of fee payment: 7

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20090323

Year of fee payment: 8

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20090323

Year of fee payment: 8

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20100323

Year of fee payment: 9

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20100323

Year of fee payment: 9

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110323

Year of fee payment: 10

LAPS Cancellation because of no payment of annual fees