AU669345B2 - Amidino derivatives and their use as nitric oxide synthase inhibitors - Google Patents

Amidino derivatives and their use as nitric oxide synthase inhibitors Download PDF

Info

Publication number
AU669345B2
AU669345B2 AU31692/93A AU3169293A AU669345B2 AU 669345 B2 AU669345 B2 AU 669345B2 AU 31692/93 A AU31692/93 A AU 31692/93A AU 3169293 A AU3169293 A AU 3169293A AU 669345 B2 AU669345 B2 AU 669345B2
Authority
AU
Australia
Prior art keywords
formula
group
date
international
pct
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.)
Ceased
Application number
AU31692/93A
Other languages
English (en)
Other versions
AU3169293A (en
Inventor
Richard Mansfield Beams
Harold Francis Hodson
Richard Michael John Palmer
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.)
Wellcome Foundation Ltd
Original Assignee
Wellcome Foundation Ltd
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 Wellcome Foundation Ltd filed Critical Wellcome Foundation Ltd
Publication of AU3169293A publication Critical patent/AU3169293A/en
Application granted granted Critical
Publication of AU669345B2 publication Critical patent/AU669345B2/en
Anticipated expiration legal-status Critical
Ceased 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)
AU31692/93A 1991-12-24 1992-12-23 Amidino derivatives and their use as nitric oxide synthase inhibitors Ceased AU669345B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB919127376A GB9127376D0 (en) 1991-12-24 1991-12-24 Amidino derivatives
GB9127376 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
AU3169293A AU3169293A (en) 1993-07-28
AU669345B2 true AU669345B2 (en) 1996-06-06

Family

ID=10706815

Family Applications (1)

Application Number Title Priority Date Filing Date
AU31692/93A Ceased AU669345B2 (en) 1991-12-24 1992-12-23 Amidino derivatives and their use as nitric oxide synthase inhibitors

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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2240041A (en) * 1989-12-22 1991-07-24 Scras Agents for blocking endothelin derived relaxing factor

Family Cites Families (3)

* 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
CA2036770C (en) * 1990-02-26 2003-09-09 Jeffrey P. Whitten Inhibitors of nitric oxide biosynthesis

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2240041A (en) * 1989-12-22 1991-07-24 Scras Agents for blocking endothelin derived relaxing factor

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
JP3171850B2 (ja) 2001-06-04
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
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
AU669345B2 (en) Amidino derivatives and their use as nitric oxide synthase inhibitors
DE69516141T2 (de) Enzymhemmer
US5281627A (en) Substituted arginines and substituted homoarginines and use thereof
EP0705257B1 (en) Aminoacid derivatives as no synthase inhibitors
SK281697B6 (sk) Soľ organickej bázy a n,n'-diacetylcystínu, spôsob jej výroby, jej použitie a farmaceutický prostriedok s jej obsahom
EP0751930B1 (en) Amidino derivatives useful as nitric oxide synthase inhibitors
US5216023A (en) Polyunsaturated fatty acid derivatives, pharmaceutical compositions containing the same, method for the preparation thereof, and their use as medicament
BRPI0614805A2 (pt) poliaminas úteis como produtos terapêuticos antiparasìticos e anticáncer e como inibidores de demetilase lisina-especìficos
PL129383B1 (en) Method of manufacture of novel xanthogenates
WO1995013804A1 (en) S-alkyl-isothioureido-amino acids and use thereof
US5268500A (en) Compound, composition and method for the reduction of lipids the modification of the affinity of hemoblogin for oxygen and the prevention of platelet aggregation
EP4072537A1 (en) Cystine diamide analogs for cystinuria
US3300510A (en) Hydantoins
WO1996000061A1 (en) Glutathione n-hydroxycarbamoyl thioesters and method of inhibiting neoplastic growth
WO1988010113A1 (en) Compound, composition and method for the reduction of lipids the modification of the affinity of hemoglobin for oxygen and the prevention of platelet aggregation
WO2023168240A1 (en) Small molecule inhibitors of enpp1
US6956131B2 (en) 2-amino-3, 4 heptenoic compounds useful as nitric oxide synthase inhibitors
PT96297A (pt) Processo para a preparacao de compostos de arilo ortossubstituido com fenilaceto nitrilalquilaminoalquilo uteis como imunossupressores
CZ297276B6 (cs) Derivát triazepinonu, zpusob jeho prípravy a farmaceutický prostredek, který ho obsahuje