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WO1994012165A3 - Inhibiteurs enzymatiques - Google Patents

Inhibiteurs enzymatiques Download PDF

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Publication number
WO1994012165A3
WO1994012165A3 PCT/GB1993/002437 GB9302437W WO9412165A3 WO 1994012165 A3 WO1994012165 A3 WO 1994012165A3 GB 9302437 W GB9302437 W GB 9302437W WO 9412165 A3 WO9412165 A3 WO 9412165A3
Authority
WO
WIPO (PCT)
Prior art keywords
enzyme inhibitors
medicine
processes
advantage
preparation
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
PCT/GB1993/002437
Other languages
English (en)
Other versions
WO1994012165A2 (fr
Inventor
Edward Patrick Garvey
Gerald Joseph Tanoury
Jeffrey Alan Oplinger
Eric Steven Furfine
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
Priority claimed from GB929224948A external-priority patent/GB9224948D0/en
Priority claimed from GB939315159A external-priority patent/GB9315159D0/en
Priority claimed from GB939319663A external-priority patent/GB9319663D0/en
Application filed by Wellcome Foundation Ltd filed Critical Wellcome Foundation Ltd
Priority to JP6512923A priority Critical patent/JPH08503940A/ja
Priority to EP94900266A priority patent/EP0670720A1/fr
Priority to AU55330/94A priority patent/AU5533094A/en
Publication of WO1994012165A2 publication Critical patent/WO1994012165A2/fr
Publication of WO1994012165A3 publication Critical patent/WO1994012165A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/30—Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/333—Radicals substituted by oxygen or sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00—Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/30—Isothioureas
    • C07C335/32—Isothioureas having sulfur atoms of isothiourea groups bound to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/32—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D277/12—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D277/18—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/38—Nitrogen atoms
    • C07D277/40—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/18—Radicals substituted by singly bound hetero atoms other than halogen by sulfur atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Dérivés d'isothiourée; leur utilisation en médecine, notamment dans le traitement des affections où il serait avantageux d'inhiber la synthase d'oxyde nitrique; formulations pharmaceutiques les comportant; et leurs procédés de préparation.
PCT/GB1993/002437 1992-11-27 1993-11-26 Inhibiteurs enzymatiques Ceased WO1994012165A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP6512923A JPH08503940A (ja) 1992-11-27 1993-11-26 酵素阻害薬
EP94900266A EP0670720A1 (fr) 1992-11-27 1993-11-26 Inhibiteurs enzymatiques
AU55330/94A AU5533094A (en) 1992-11-27 1993-11-26 Enzyme inhibitors

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB929224948A GB9224948D0 (en) 1992-11-27 1992-11-27 Nitric oxide synthase inhibitors
GB939315159A GB9315159D0 (en) 1993-07-22 1993-07-22 Nitric oxide synthase inhibitors
GB9319663.2 1993-09-23
GB9315159.5 1993-09-23
GB939319663A GB9319663D0 (en) 1993-09-23 1993-09-23 Enzyme inhibitors
GB9224948.1 1993-09-23

Publications (2)

Publication Number Publication Date
WO1994012165A2 WO1994012165A2 (fr) 1994-06-09
WO1994012165A3 true WO1994012165A3 (fr) 1994-12-08

Family

ID=27266488

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB1993/002437 Ceased WO1994012165A2 (fr) 1992-11-27 1993-11-26 Inhibiteurs enzymatiques

Country Status (7)

Country Link
EP (1) EP0670720A1 (fr)
JP (1) JPH08503940A (fr)
CN (1) CN1095710A (fr)
AU (1) AU5533094A (fr)
IL (1) IL107771A0 (fr)
SI (1) SI9300616A (fr)
WO (1) WO1994012165A2 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8883779B2 (en) 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
US8895548B2 (en) 2007-04-24 2014-11-25 Shionogi & Co., Ltd. Pharmaceutical composition for treating alzheimer's disease
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
US9273053B2 (en) 2008-06-13 2016-03-01 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having Beta secretase inhibitory activity
US9290466B2 (en) 2009-12-11 2016-03-22 Shionogi & Co., Ltd. Oxazine derivatives
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9407515A (pt) * 1993-08-12 1997-01-07 Astra Ab Composto formulação farmaceutica uso do composto processos para o tratamento de desordens neurodegenerativas ou de enxaqueca ou para a prevenção e a reversão da tolerância aos opiatos e diazepinas ou para o tratamento do vicio das drogas e para a preparação do composto
EP0724570B1 (fr) * 1993-10-21 1999-03-03 G.D. Searle & Co. Derives amidino utiles en tant qu'inhibiteurs de la synthase de l'oxyde nitrique
MX9605366A (es) * 1994-05-07 1997-12-31 Astra Ab Derivados de amidina biciclicos como inhibidores de la oxido nitrico sintetasa.
GB9418912D0 (en) * 1994-09-20 1994-11-09 Fisons Corp Pharmaceutically active compounds
AU4149696A (en) * 1994-11-15 1996-06-06 Merck & Co., Inc. Substituted heterocycles as inhibitors of nitric oxide synthase
AU4515896A (en) * 1994-12-12 1996-07-03 Merck & Co., Inc. Substituted 2-acylamino-pyridines as inhibitors of nitric oxide synthase
DE19530870A1 (de) * 1994-12-14 1996-06-20 Japan Tobacco Inc Thiazin- oder Thiazepinderivate
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
DE4444930A1 (de) * 1994-12-16 1996-06-27 Cassella Ag 2-Amino-1,3-thiazepine und deren Verwendung als Hemmstoffe der Stickstoffmonoxid-Synthase
WO1996021445A1 (fr) * 1995-01-13 1996-07-18 The General Hospital Corporation Procedes d'inhibition de maladies neurodegeneratives
TW397812B (en) * 1995-02-11 2000-07-11 Astra Ab Bicyclic isothiourea derivatives useful in therapy
FR2730733B1 (fr) * 1995-02-17 1997-07-04 Hoechst Lab Nouveaux derives nitro-ethyleniques soufres et leurs applications en tant qu'inhibiteurs de no-synthase
US5929063A (en) * 1995-03-24 1999-07-27 Children's Hospital Medical Center Mercapto and seleno derivatives as inhibitors of nitric oxide synthase
US5674907A (en) * 1995-03-24 1997-10-07 Children's Hospital Medical Center Mercapto derivatives as inhibitors of nitric oxide synthase
GB9506188D0 (en) * 1995-03-27 1995-05-17 Fujisawa Pharmaceutical Co Amidine derivatives
EP0821674B1 (fr) * 1995-04-20 2003-08-06 G.D. SEARLE & CO. Agents amidino cycliques utiles en tant qu'inhibiteurs de synthase de l'oxyde nitrique
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
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
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
EP1067926A2 (fr) * 1998-04-06 2001-01-17 Fujisawa Pharmaceutical Co., Ltd. Nouvelle utilisation
CA2333691A1 (fr) 1998-06-10 1999-12-16 G.D. Searle & Co. Inhibiteurs heterobicycliques et tricycliques de no synthetase
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
GB9903404D0 (en) 1999-02-16 1999-04-07 Angiogene Pharm Ltd Methods of treatment and compositions useful for the treatment of diseases involving angiogenesis
CZ304346B6 (cs) * 2000-01-19 2014-03-19 Cadila Healthcare Ltd. Substituovaný pyrrolový derivát s hypolipidemickou hypocholesteremickou aktivitou, způsob jeho přípravy a farmaceutický přípravek obsahující tyto sloučeniny
NZ520813A (en) 2000-03-24 2004-05-28 Pharmacia Corp Amidino compounds useful as nitric oxide synthase inhibitors
US7087633B2 (en) 2000-03-31 2006-08-08 Universitair Medisch Centrum Method for treating perinatal asphyxia in a human or animal neonate
CA2419302C (fr) * 2000-03-31 2009-12-15 Universitair Medisch Centrum Utilisation de 2-iminobiotine pour la prevention ou le traitement de l'asphyxie perinatale chez les nouveau-nes
US6545170B2 (en) 2000-04-13 2003-04-08 Pharmacia Corporation 2-amino-5, 6 heptenoic acid derivatives 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
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
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
US6956131B2 (en) 2000-04-13 2005-10-18 Pharmacia Corporation 2-amino-3, 4 heptenoic compounds 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
FR2810036B1 (fr) * 2000-06-09 2004-04-23 Aventis Pharma Sa Derives de 4,5-dihydro-1,3-thiazol-2-ylamine, leur preparation et les compositions phamarceutiques les contenant
FR2832152A1 (fr) * 2001-11-09 2003-05-16 Aventis Pharma Sa Utilisation de derives de 2-amino-thiazoline comme inhibiteurs de no-synthase inductible
US6451821B1 (en) 2000-06-09 2002-09-17 Aventis Pharma S.A. Use of 2-aminothiazoline derivatives as inhibitors of inducible no-synthase
FR2810037B1 (fr) * 2000-06-09 2004-04-23 Aventis Pharma Sa Utilisation de derives de 2-aminothiazoline comme inhibiteurs de no-synthase inductible
US6420566B2 (en) 2000-06-09 2002-07-16 Aventis Pharma S.A. Pharmaceutical compositions containing a 4, 5-dihydro-1, 3-thiazol-2-ylamine derivative, novel derivatives and preparation thereof
US6344473B1 (en) 2000-08-07 2002-02-05 G.D. Searle & Co. Imidazoles useful as nitric oxide synthase inhibitors
US7012098B2 (en) 2001-03-23 2006-03-14 Pharmacia Corporation Inhibitors of inducible nitric oxide synthase for chemoprevention and treatment of cancers
CA2669810A1 (fr) 2001-11-09 2003-05-15 Aventis Pharma S.A. Composes intermediaires pour la preparation de derives de 2-amino-thiazoline
AU2002358874B2 (en) 2001-11-09 2007-09-06 Aventis Pharma S.A. 2-amino-4-heteroarylethyl thiazoline derivatives and their use an inhibitors of inducible no-synthase
FR2832151B1 (fr) * 2001-11-09 2004-12-17 Aventis Pharma Sa Utilisation de derives de 2-amino-4-heteroarylethyl-thiazoline comme inhibiteurs de no-synthase inductible
FR2832150B1 (fr) * 2001-11-09 2004-07-16 Aventis Pharma Sa Utilisation de derives de 2-amino-4-pyridylmethyl-thiazoline comme inhibiteurs de no-synthase inductible
CA2465877C (fr) * 2001-11-09 2009-12-29 Aventis Pharma S.A. Utilisation de derives de 2-amino-4-pyridylmethyl-thiazoline comme inhibiteurs de non-synthase inductible
US8173642B2 (en) 2005-10-25 2012-05-08 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
WO2007108004A2 (fr) * 2006-03-23 2007-09-27 Meditor Pharmaceuticals Ltd. Derives du s-alkylisothiouronium pour le traitement de maladies inflammatoires
TW200902526A (en) 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
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Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1178242A (en) * 1966-02-05 1970-01-21 Wellcome Found Novel Biologically Active Bis-Isothioureas
DE2317106A1 (de) * 1972-04-06 1973-10-11 Uniroyal Inc 2-(3-benzo eckige klammer auf b eckige klammer zu thenyl)-2-thiopseudoharnstoff und dessen pharmazeutisch vertraegliche salze sowie diese enthaltende arzneipraeparate
US3954982A (en) * 1972-04-20 1976-05-04 Smith Kline & French Laboratories Limited Pharmaceutical compositions and method of inhibiting H-1 and H-2 histamine receptors
US4126670A (en) * 1976-03-29 1978-11-21 Smith Kline & French Laboratories Limited Method of stimulating histamine H2 -receptors
US4208430A (en) * 1979-03-15 1980-06-17 Smithkline Corporation Pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase
US4262125A (en) * 1979-07-23 1981-04-14 American Home Products Corporation (1H-Imidazol-5-ylmethyl)isothioureas
EP0245669A2 (fr) * 1986-05-14 1987-11-19 Medopharm Arzneimittelwerk Dr. Zillich GmbH & Co. Préparation pharmaceutique pour empêcher les dommages aux cellules vivantes par des radicaux libres, respectivement pour augmenter l'efficacité des composés organiques du soufre et procédé pour augmenter la durée de vie d'organes isolés
EP0420396A2 (fr) * 1989-07-25 1991-04-03 Smith Kline & French Laboratories Limited Dérivés d'imidazole comme agonistes H3 de l'histamine
WO1991004037A1 (fr) * 1989-09-19 1991-04-04 Jan Kristoffer Hellstrand Preparation antitumorale comprenant de l'interleukine-2 et de l'histamine, leurs analogues ou des agonistes de recepteur de h¿2?
EP0547558A1 (fr) * 1991-12-16 1993-06-23 Washington University Utilisation d'aminoguanidine pour la fabrication d'un médicament pour inhiber la formation d'oxyde nitrique
US7759999B2 (en) * 2007-11-09 2010-07-20 Hynix Semiconductor Inc. Externally asynchronous internally clocked system

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1178242A (en) * 1966-02-05 1970-01-21 Wellcome Found Novel Biologically Active Bis-Isothioureas
DE2317106A1 (de) * 1972-04-06 1973-10-11 Uniroyal Inc 2-(3-benzo eckige klammer auf b eckige klammer zu thenyl)-2-thiopseudoharnstoff und dessen pharmazeutisch vertraegliche salze sowie diese enthaltende arzneipraeparate
US3790600A (en) * 1972-04-06 1974-02-05 Uniroyal Inc 2-(3-benzo(b)thenyl)-2-thiopseudourea and its pharmaceutically acceptable salts
US3954982A (en) * 1972-04-20 1976-05-04 Smith Kline & French Laboratories Limited Pharmaceutical compositions and method of inhibiting H-1 and H-2 histamine receptors
US4126670A (en) * 1976-03-29 1978-11-21 Smith Kline & French Laboratories Limited Method of stimulating histamine H2 -receptors
US4208430A (en) * 1979-03-15 1980-06-17 Smithkline Corporation Pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase
US4262125A (en) * 1979-07-23 1981-04-14 American Home Products Corporation (1H-Imidazol-5-ylmethyl)isothioureas
EP0245669A2 (fr) * 1986-05-14 1987-11-19 Medopharm Arzneimittelwerk Dr. Zillich GmbH & Co. Préparation pharmaceutique pour empêcher les dommages aux cellules vivantes par des radicaux libres, respectivement pour augmenter l'efficacité des composés organiques du soufre et procédé pour augmenter la durée de vie d'organes isolés
EP0420396A2 (fr) * 1989-07-25 1991-04-03 Smith Kline & French Laboratories Limited Dérivés d'imidazole comme agonistes H3 de l'histamine
WO1991004037A1 (fr) * 1989-09-19 1991-04-04 Jan Kristoffer Hellstrand Preparation antitumorale comprenant de l'interleukine-2 et de l'histamine, leurs analogues ou des agonistes de recepteur de h¿2?
EP0547558A1 (fr) * 1991-12-16 1993-06-23 Washington University Utilisation d'aminoguanidine pour la fabrication d'un médicament pour inhiber la formation d'oxyde nitrique
US7759999B2 (en) * 2007-11-09 2010-07-20 Hynix Semiconductor Inc. Externally asynchronous internally clocked system

Non-Patent Citations (22)

* Cited by examiner, † Cited by third party
Title
"accession number 04916379", DIALOG INFORMATION SERVICES, FILE 155: MEDLINE *
"accession number 05268819", DIALOG INFORMATION SERVICES, FILE 155: MEDLINE *
"accession number 05837693", DIALOG INFORMATION SERVICES, FILE 155: MEDLINE *
"accession number 08184588", DIALOG INFORMATION SERVICES, FILE 155: MEDLINE *
"The Merck Index, 11th Edition", MERCK & CO., INC., RAHWAY, N.J., U.S.A. *
B.MALINOWSKA ET AL.: "Identification of endothelial H1, vascular H2 and cardiac presynaptic H3 receptors in the pithed rat", NAUNYN-SCHMIEDEBERG'S ARCH. PHARMACOL., vol. 347, no. 1, January 1993 (1993-01-01), pages 55 - 60 *
DATABASE WPI Derwent World Patents Index; AN 92-259284 *
E.E.J.HAAKSMA ET AL.: "A theoretical study concerning the mode of interaction of the histamine H2-agonist dimaprit", J.MOL.GRAPH., vol. 10, no. 2, June 1992 (1992-06-01), pages 79 - 87 *
G.A.FECHNER ET AL.: "ANTIPROLIFERATIVE AND DEPIGMENTING EFFECTS OF THE HISTAMINE (H2) AGONIST DIMAPRIT AND ITS DERIVATIVES ON HUMAN MELANOMA CELLS", BIOCHEM. PHARMACOL., vol. 43, no. 10, 28 May 1992 (1992-05-28), pages 2083 - 2090, XP025542111, DOI: doi:10.1016/0006-2952(92)90165-F *
G.J.DURANT ET AL.: "Dimaprit, [S-[3-(N,N-dimethylamino)propyl]isothiourea], A Highly Specific Histamine H2-Receptor Agonist. Part 2. Structure-Activity Considerations", AGENTS ACTIONS, vol. 7, no. 1, March 1977 (1977-03-01), pages 39 - 43 *
G.J.STERK ET AL.: "The influence of guanidino and isothiourea groups in histaminergic compounds on H2-activity", AGENTS ACTIONS, vol. 18, no. 1-2, April 1986 (1986-04-01), pages 137 - 140 *
I.R.KATZ ET AL., INT. IMMUNOL., vol. 4, no. 2, February 1992 (1992-02-01), pages 183 - 190 *
J.L.ORTIZ ET AL.: "Histamine Receptors on Human Isolated Pulmonary Arterial Muscle Preparations: Effects of Endothelial Cell Removal and Nitric Oxide Inhibitors", J.PHARMACOL.EXP.THER., vol. 260, no. 2, February 1992 (1992-02-01), pages 762 - 767 *
K.NAGARAJAN ET AL.: "Structure Activity Relations among Cyclic & Acyclic S-(3-Indolyl)isothioureas - Development of a Potent Vasoconstrictor, Tinazole, 3-(2-Imidazolin-2-yl-thio)indole", INDIAN J. EXP. BIOL., vol. 19, no. 12, December 1981 (1981-12-01), pages 1150 - 1153, XP009064573 *
L.BEAULIEU ET AL., INT. ARCH. ALLERGY APPL. IMMUNOL., vol. 79, no. 3, 1986, pages 249 - 252 *
M.KELM ET AL.: "Mechanisms of Histamine-Induced Coronary Vasodilation: H1-Receptor-Mediated Release of Endothelium-Derived Nitric Oxide", J.VASC.RES., vol. 30, no. 3, May 1993 (1993-05-01), pages 132 - 138 *
M.R.VICKERS ET AL., AGENTS ACTIONS, vol. 12, December 1982 (1982-12-01), pages 691 - 698 *
R.GANELLIN: "Medicinal Chemistry and Dynamic Structure-Activity Analysis in the Discovery of Drugs Acting at Histamine H2 Receptors", J.MED.CHEM., vol. 24, no. 8, August 1981 (1981-08-01), pages 913 - 920 *
S.A.SELEZNEV ET AL., PATOL. FIZIOL. EKSP. TER., no. 1, January 1984 (1984-01-01), pages 41 - 45 *
S.B.FLYNN ET AL.: "THE CARDIOVASCULAR RESPONSE TO DIMAPRIT, A SELECTIVE HISTAMINE H2-RECEPTOR AGONIST", BR.J.PHARMACOL., vol. 61, no. 1, September 1977 (1977-09-01), pages 101 - 107 *
S.FRENCH ET AL.: "Modulation of in vitro Cellular Immune Response by Histamine Agonists or Antagonists in Murine Species", ARZNEIMITTELFORSCHUNG, vol. 35, no. 1A, 1985, pages 390 - 394 *
T.HIRAYAMA ET AL.: "Anti-tumor Activities of Some Heterocyclic and Nitrogen-containing Compounds", YAKUGAKU ZASSHI, vol. 100, no. 12, 1980, pages 1225 - 1234 *

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WO1994012165A2 (fr) 1994-06-09
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JPH08503940A (ja) 1996-04-30
SI9300616A (en) 1994-06-30
AU5533094A (en) 1994-06-22

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