CL2011002838A1 - Compuestos derivados de 1,2,4-triazolo[4,3-a]piridina, moduladores alostéricos de receptores mglur2; composición farmacéutica; proceso para prepararla; y su uso en el tratamiento o la prevención de un trastorno del sistema nervioso central seleccionado de ansiedad y esquizofrenia, entre otros. - Google Patents

Compuestos derivados de 1,2,4-triazolo[4,3-a]piridina, moduladores alostéricos de receptores mglur2; composición farmacéutica; proceso para prepararla; y su uso en el tratamiento o la prevención de un trastorno del sistema nervioso central seleccionado de ansiedad y esquizofrenia, entre otros.

Info

Publication number
CL2011002838A1
CL2011002838A1 CL2011002838A CL2011002838A CL2011002838A1 CL 2011002838 A1 CL2011002838 A1 CL 2011002838A1 CL 2011002838 A CL2011002838 A CL 2011002838A CL 2011002838 A CL2011002838 A CL 2011002838A CL 2011002838 A1 CL2011002838 A1 CL 2011002838A1
Authority
CL
Chile
Prior art keywords
prevention
treatment
triazolo
schizophrenia
anxiety
Prior art date
Application number
CL2011002838A
Other languages
English (en)
Inventor
Daniel Oehlrich
Gregor James Macdonald
Nuñez Jose Maria Cid
Andres Avelino Trabanco-Suarez
Gary John Tresadern
Ramiro Juan Antonio Vega
Original Assignee
Addex Pharmaceuticals Sa
Janssen Pharmaceuticals Inc
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 Addex Pharmaceuticals Sa, Janssen Pharmaceuticals Inc filed Critical Addex Pharmaceuticals Sa
Publication of CL2011002838A1 publication Critical patent/CL2011002838A1/es

Links

Classifications

    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)

Abstract

SE DESCRIBEN COMPUESTO DERIVADOS DE TRIAZOLO (4, 3-A) PIRIDINA DE FORMULA (I) EN DONDE TODOS LOS RADICALES SON COMO SE DEFINE EN LAS REIVINDICACIONES. LOS COMPUESTOS DE ACUERDO CON LA INVENCIÓN SON MODULADORES ALOSTÉRICOS POSITIVOS DEL RECEPTOR DE GLUTAMATO METABOLRÓPICO SUBTIPO 2 ('MGLUR2'). UTILES PARA EL TRATAMIENTO O LA PREVENCIÓN DE TRASTORNOS NEUROLÓGICOS Y PSIQUIÁTRICOS ASOCIADOS<br /> CON UNA DISFUNCIÓN DEL GLUTAMATO Y ENFERMEDADES EN LAS CUALES ESTÁ INVOLUCRADO EL SUBTIPO MGLUR2 DE RECEPTORES METABOTRÓPICOS. UNA COMPOSICIÓN FARMACÉUTICAS QUE COMPRENDEN DICHOS COMPUESTOS. A PROCESOS PARA PREPARAR DICHOS COMPUESTOS Y COMPOSICIONES. Y AL USO DE DICHOS COMPUESTOS PARA LA<br /> PREVENCIÓN O EL TRATAMIENTO DE TRASTORNOS NEUROLÓGICOS Y PSIQUIÁTRICOS Y ENFERMEDADES EN LAS CUALES ESTÁ INVOLUCRADO MGLUR2. TAL COMO ANSIEDAD. ESQUIZOFRENIA. MIGRAÑA Y EPILEPSIA.  
CL2011002838A 2009-05-12 2011-11-11 Compuestos derivados de 1,2,4-triazolo[4,3-a]piridina, moduladores alostéricos de receptores mglur2; composición farmacéutica; proceso para prepararla; y su uso en el tratamiento o la prevención de un trastorno del sistema nervioso central seleccionado de ansiedad y esquizofrenia, entre otros. CL2011002838A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09160059 2009-05-12

Publications (1)

Publication Number Publication Date
CL2011002838A1 true CL2011002838A1 (es) 2012-04-09

Family

ID=41429238

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2011002838A CL2011002838A1 (es) 2009-05-12 2011-11-11 Compuestos derivados de 1,2,4-triazolo[4,3-a]piridina, moduladores alostéricos de receptores mglur2; composición farmacéutica; proceso para prepararla; y su uso en el tratamiento o la prevención de un trastorno del sistema nervioso central seleccionado de ansiedad y esquizofrenia, entre otros.

Country Status (32)

Country Link
US (4) US8937060B2 (es)
EP (1) EP2430022B1 (es)
JP (1) JP5634506B2 (es)
KR (1) KR101753826B1 (es)
CN (1) CN102439008B (es)
AR (1) AR076861A1 (es)
AU (1) AU2010246609B2 (es)
BR (1) BRPI1012870B8 (es)
CA (1) CA2760741C (es)
CL (1) CL2011002838A1 (es)
CY (1) CY1114718T1 (es)
DK (1) DK2430022T3 (es)
EA (1) EA020672B1 (es)
ES (1) ES2440001T3 (es)
HK (1) HK1169405A1 (es)
HR (1) HRP20131122T1 (es)
IL (1) IL215912A (es)
JO (1) JO2907B1 (es)
ME (1) ME01573B (es)
MX (1) MX2011011964A (es)
MY (1) MY161325A (es)
NZ (1) NZ596078A (es)
PL (1) PL2430022T3 (es)
PT (1) PT2430022E (es)
RS (1) RS53075B (es)
SG (2) SG10201402250TA (es)
SI (1) SI2430022T1 (es)
SM (1) SMT201400003B (es)
TW (1) TWI468406B (es)
UA (1) UA108070C2 (es)
WO (1) WO2010130424A1 (es)
ZA (1) ZA201107834B (es)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
NZ584152A (en) 2007-09-14 2011-11-25 Ortho Mcneil Janssen Pharm 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones
KR101520086B1 (ko) 2007-09-14 2015-05-14 얀센 파마슈티칼스 인코포레이티드 １´,３´-이치환된-４-페닐-３,４,５,６-테트라히드로-２ｈ,１´ｈ-[１,４´]비피리디닐-２´-온
KR20100080597A (ko) 2007-09-14 2010-07-09 오르토-맥닐-얀센 파마슈티칼스 인코포레이티드 １,３-이치환된-４-페닐-1ｈ-피리딘-2-온
JP5433582B2 (ja) * 2007-11-14 2014-03-05 ジャンセン ファーマシューティカルズ， インコーポレイテッド． イミダゾ［１，２−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体の正のアロステリック調節因子としてのその使用
CA2735764C (en) 2008-09-02 2016-06-14 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
US8697689B2 (en) 2008-10-16 2014-04-15 Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
US8691813B2 (en) 2008-11-28 2014-04-08 Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
EA020671B1 (ru) 2009-05-12 2014-12-30 Янссен Фармасьютикалз, Инк. ПРОИЗВОДНЫЕ 1,2,4-ТРИАЗОЛО[4,3-a]ПИРИДИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПОЛОЖИТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2
BRPI1012870B8 (pt) 2009-05-12 2021-05-25 Addex Pharmaceuticals Sa derivados de 1,2,4-triazolo[4,3-a]piridina e seu uso como moduladores alostericos positivos de receptores de mglur2 e composição farmacêutica
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
US9018227B2 (en) 2010-03-19 2015-04-28 Indiana State University Nicotinic acetylcholine receptor agonists
PE20130576A1 (es) 2010-05-13 2013-05-19 Amgen Inc Compuestos heterociclicos de nitrogeno utiles como inhibidores de pde10
US20130230459A1 (en) * 2010-11-08 2013-09-05 Janssen Pharmaceuticals, Inc. RADIOLABELLED mGluR2 PET LIGANDS
PT2649069E (pt) 2010-11-08 2015-11-20 Janssen Pharmaceuticals Inc Derivados de 1,2,4-triazolo[4,3-a]piridina e sua utilização como moduladores alostéricos positivos de recetores mglur2
US9012448B2 (en) 2010-11-08 2015-04-21 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors
AU2011328203B2 (en) * 2010-11-08 2015-03-19 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
WO2013038362A1 (en) 2011-09-15 2013-03-21 Novartis Ag 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase
US8765767B2 (en) 2012-03-16 2014-07-01 Bristol-Myers Squibb Company Positive allosteric modulators of mGluR2
US9682980B2 (en) 2012-06-21 2017-06-20 Bristol-Myers Squibb Company Positive allosteric modulators of mGluR2
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) * 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
KR102502485B1 (ko) * 2014-01-21 2023-02-21 얀센 파마슈티카 엔.브이. 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도
ME03518B (me) 2014-01-21 2020-04-20 Janssen Pharmaceutica Nv Kombinacije koje obuhvataju pozitivne alosterične modulatore ili ortosterične agoniste metabotropnog glutamatergičnog receptora podtipa 2 i njihova primjena
WO2016016382A1 (en) 2014-08-01 2016-02-04 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors
JO3601B1 (ar) 2014-08-01 2020-07-05 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
JOP20150177B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
CN107001373B (zh) 2014-08-01 2020-01-07 詹森药业有限公司 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途
JOP20150179B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
CA2967542C (en) 2014-12-03 2022-11-29 Janssen Pharmaceutica Nv Radiolabelled mglur2 pet ligands
EP3227295B1 (en) 2014-12-03 2019-02-20 Janssen Pharmaceutica NV 6,7-dihydropyrazolo[1,5- ]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors
WO2016092002A1 (en) 2014-12-11 2016-06-16 Janssen Pharmaceutica Nv 1,2,4-triazolo[4,3-a]pyridine compounds and their use as positive allosteric modulators of mglur2 receptors
US11033641B2 (en) 2015-12-18 2021-06-15 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 pet ligands
ES2820823T3 (es) 2015-12-18 2021-04-22 Janssen Pharmaceutica Nv Ligandos PET mGluR2/3 radiomarcados
DK3519416T3 (da) * 2016-09-27 2021-05-25 Merck Sharp & Dohme Chroman, isochroman og dihydroisobenzofuranderivater som mglur2-negative allosteriske modulatorer, sammensætninger og anvendelse deraf
CA3045121A1 (en) 2016-11-28 2018-05-31 Praxis Precision Medicines, Inc. Compounds and their methods of use
WO2018098491A1 (en) 2016-11-28 2018-05-31 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11492345B2 (en) 2017-02-13 2022-11-08 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11731966B2 (en) 2017-04-04 2023-08-22 Praxis Precision Medicines, Inc. Compounds and their methods of use
WO2019002548A1 (en) 2017-06-29 2019-01-03 INSERM (Institut National de la Santé et de la Recherche Médicale) TREATMENT OF MIGRAINE WITH TREK1, TREK2 AGONIZATION OR HETEROMERS COMPRISING SAME
US11278535B2 (en) 2017-08-15 2022-03-22 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11866439B2 (en) 2018-05-30 2024-01-09 Praxis Precision Medicines, Inc. Ion channel modulators
WO2020231849A1 (en) * 2019-05-10 2020-11-19 The Broad Institute, Inc. Methods for treating disorders associated with sleep spindle deficits
US11773099B2 (en) 2019-05-28 2023-10-03 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11279700B2 (en) 2019-05-31 2022-03-22 Praxis Precision Medicines, Inc. Ion channel modulators
US11505554B2 (en) 2019-05-31 2022-11-22 Praxis Precision Medicines, Inc. Substituted pyridines as ion channel modulators
WO2021081357A1 (en) * 2019-10-23 2021-04-29 Neurocycle Therapeutics, Inc. Treatment of epileptic conditions with gabaa receptor modulators
US11767325B2 (en) 2019-11-26 2023-09-26 Praxis Precision Medicines, Inc. Substituted [1,2,4]triazolo[4,3-a]pyrazines as ion channel modulators
US20210246140A1 (en) * 2020-01-31 2021-08-12 The General Hospital Corporation Modulators of metabotropic glutamate receptor 2
US20240208983A1 (en) * 2021-04-02 2024-06-27 Vanderbilt University 1,2,4-triazolo[4,3-a]pyridine derivatives as negative allosteric modulators of metabotropic glutamate receptor 2
CN116217571A (zh) * 2023-03-28 2023-06-06 上海锐谱医药科技有限公司 一种制备药物砌块1,2,4-三唑并[4,3-a]吡啶-3-胺的方法

Family Cites Families (475)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2976146A (en) 1958-11-28 1961-03-21 Eastman Kodak Co Novel cyan-forming couplers
BE790440A (es) 1971-10-23 1973-04-24 Bayer Ag
JPS5752334B2 (es) 1974-02-05 1982-11-06
JPS538707B2 (es) 1974-02-05 1978-03-31
JPS50106981U (es) 1974-02-08 1975-09-02
US3906953A (en) 1974-05-23 1975-09-23 American Optical Corp Endoscopic surgical laser system
SU509578A1 (ru) 1974-09-19 1976-04-05 Стерлитамакский Химический Завод Способ получени пропилендиаминов
IE43079B1 (en) 1975-03-20 1980-12-17 Ici Ltd Quinolone derivatives
GB1502312A (en) 1975-03-20 1978-03-01 Ici Ltd Quinolone derivatives
FR2311776A1 (fr) 1975-05-23 1976-12-17 Sogeras Diamino-2,4 bromo-5 chloro-6 pyrimidines et procede pour leur preparation
GB1570494A (en) 1975-11-28 1980-07-02 Ici Ltd Thienopyrimidine derivatives and their use as pesticides
DE2614831A1 (de) 1976-04-06 1977-10-20 Bayer Ag 1,3,4-thiadiazolylderivate, verfahren zu ihrer herstellung sowie ihre verwendung als herbizide
JPS5382783U (es) 1976-12-13 1978-07-08
JPS5382783A (en) 1976-12-29 1978-07-21 Yamanouchi Pharmaceut Co Ltd Novel pyridone derivs and process for their preparation
JPS5752334Y2 (es) 1977-03-16 1982-11-13
US4196207A (en) 1977-05-23 1980-04-01 Ici Australia Limited Process for controlling eradicating or preventing infestations of animals by Ixodid ticks
DE2750288A1 (de) 1977-11-10 1979-05-17 Thomae Gmbh Dr K Neue 9-(omega-heteroarylamino- alkylamino)-erythromycine, ihre salze, verfahren zu ihrer herstellung und diese enthaltende arzneimittel
US4432979A (en) 1981-10-26 1984-02-21 William H. Rorer, Inc. Pyridone compounds
FI824314L (fi) 1981-12-16 1983-06-17 Sankyo Co Thienopyrimidin-derivater, deras framstaellning och deras medicinska anvaendning
US4358453A (en) 1982-01-08 1982-11-09 Schering Corporation 1,2,4-Triazolo[4,3-a]pyridines
US4520025A (en) 1982-07-21 1985-05-28 William H. Rorer, Inc. Bicyclic nitrogen heterocyclic ethers and thioethers, and their pharmaceutical uses
JPS59210083A (ja) 1983-05-13 1984-11-28 Otsuka Chem Co Ltd １，３，４−チアジアゾ−ル−５−オン誘導体、その製造法及び該誘導体を有効成分とする除草剤
JPS6092285A (ja) 1983-10-26 1985-05-23 Shionogi & Co Ltd イソオキサゾ−ル系環状尿素類
DE3406329A1 (de) 1984-02-22 1985-08-22 Merck Patent Gmbh, 6100 Darmstadt Pyridone
US4550166A (en) 1984-05-21 1985-10-29 American Cyanamid Company (Pyridinyl)-1,2,4-triazolo[4,3-a]pyridines
DE3717561A1 (de) 1987-05-25 1988-12-08 Thomae Gmbh Dr K Indol-, isochinolin- und benzazepinderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
US5175157A (en) 1985-11-27 1992-12-29 Boehringer Ingelheim Gmbh Cyclic amine derivatives, pharmaceutical compositions containing these compounds and methods for preparing them
US4866074A (en) 1987-05-08 1989-09-12 Rorer Pharmaceutical Corporation Naphtheridinone- and pyridooxazinone-pyridone compounds, cardiotonic compositions including same, and their uses
JPS649978A (en) 1987-07-02 1989-01-13 Shionogi & Co Perfluoroalkylisoxazole derivative
EP0308020A3 (en) 1987-09-18 1990-12-05 Merck & Co. Inc. 5-(aryl and heteroaryl)-6-(aryl and heteroaryl)-1,2-dihydro-2-oxo 3-pyridinecarboxylic acids and derivatives thereof
US5260293A (en) 1988-01-30 1993-11-09 Merck Sharp & Dohme Limited Pyrazines, pyrimidines and pyridazines useful in the treatment of senile dementia
GB8804448D0 (en) 1988-02-25 1988-03-23 Smithkline Beckman Intercredit Compounds
JP2614081B2 (ja) 1988-05-27 1997-05-28 大塚化学株式会社 光学活性β−ラクタム誘導体の製造法
JPH02124871A (ja) 1988-07-27 1990-05-14 Dainippon Pharmaceut Co Ltd １位が置換された複素環式カルボン酸アミド誘導体
DE68923527D1 (de) 1988-10-20 1995-08-24 Sandoz Ag Faserreaktive Azofarbstoffe.
US5032602A (en) 1988-12-14 1991-07-16 Bayer Aktiengesellschaft Inhibiting HMG-CoA reductase with novel substituted 2-pyridones and pyrid-2-thiones
HU206337B (en) 1988-12-29 1992-10-28 Mitsui Petrochemical Ind Process for producing pyrimidine derivatives and pharmaceutical compositions
JPH02277044A (ja) 1989-04-19 1990-11-13 Fuji Photo Film Co Ltd ハロゲン化銀写真感光材料
US5236917A (en) 1989-05-04 1993-08-17 Sterling Winthrop Inc. Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof
US5280026A (en) 1989-05-30 1994-01-18 Smithkline Beecham Intercredit B.V. Thienopyrimidines
AU622330B2 (en) 1989-06-23 1992-04-02 Takeda Chemical Industries Ltd. Condensed heterocyclic compounds having a nitrogen atom in the bridgehead for use as fungicides
US4978663A (en) 1989-08-16 1990-12-18 Hoechst-Roussel Pharmaceuticals Inc. 5-(1-aminocyclohexyl)-2(1H)-pyridinone compounds which have pharmaceutical utility
GB8926560D0 (en) 1989-11-24 1990-01-17 Zambeletti Spa L Pharmaceuticals
IL96432A0 (en) 1989-11-30 1991-08-16 Schering Ag Pesticidal compositions containing pyridine derivatives and novel pyridine derivatives
DE3940480A1 (de) 1989-12-07 1991-06-13 Bayer Ag Chromogene enaminverbindungen, ihre herstellung und verwendung als farbbildner
WO1991009848A1 (en) 1989-12-22 1991-07-11 The Upjohn Company Pyridinones useful as antiatherosclerotic agents
FR2657610A1 (fr) 1990-01-29 1991-08-02 Rhone Poulenc Agrochimie Triazolopyridines herbicides.
GB9104238D0 (en) 1990-03-16 1991-04-17 Ici Pharma 3-tetrazolylthiomethyl cephalosporin antibiotics
DE4008726A1 (de) 1990-03-19 1991-09-26 Basf Ag Thieno(2,3-d)pyrimidinderivate
AU651337B2 (en) 1990-03-30 1994-07-21 Dowelanco Thienopyrimidine derivatives
RU1796625C (ru) 1990-06-27 1993-02-23 Киевский Государственный Университет Им.Т.Г.Шевченко 3-Амино-7-нитро-4(2,3,4-триметоксифенил)-2-фенил-1(2Н)изохинолон, обладающий аналептическим действием
ES2131506T3 (es) 1990-09-21 1999-08-01 Rohm & Haas Dihidropiridacinonas y piridacinonas como fungicidas.
KR920008026A (ko) 1990-10-24 1992-05-27 오노 화아마슈티칼 캄파니 리미팃드 이소퀴놀리논 유도체 또는 이의 무독성 산부가염 또는 이의 수화물, 이의 제조방법 및 이를 포함하는 약제 조성물
AU1532492A (en) 1991-04-18 1992-11-17 Dr. Lo Zambeletti S.P.A. Use of heterocyclic compounds for the treatment of inflammatory pain
DE4122240A1 (de) 1991-07-05 1993-01-07 Boehringer Mannheim Gmbh Dibenz(b,e)azepinderivate und diese enthaltende arzneimittel
US5332750A (en) 1991-09-04 1994-07-26 Merck Patent Gesellschaft Mit Beschrankter Haftung 1,2-dihydro-2-oxopyridines
DE4129340A1 (de) 1991-09-04 1993-03-11 Merck Patent Gmbh 1,2-dihydro-2-oxopyridine
DE4131924A1 (de) 1991-09-25 1993-07-08 Hoechst Ag Substituierte 4-alkoxypyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel
US5204198A (en) 1991-10-28 1993-04-20 Eastman Kodak Company Photoelectrographic elements utilizing nonionic sulfonic acid photogenerators
US5416099A (en) 1991-10-29 1995-05-16 Merck & Co., Inc. Fibrinogen receptor antagonists
DE4221583A1 (de) 1991-11-12 1993-05-13 Bayer Ag Substituierte biphenylpyridone
JP2878531B2 (ja) 1991-12-16 1999-04-05 富士写真フイルム株式会社 ハロゲン化銀写真感光材料
US5378720A (en) 1991-12-19 1995-01-03 Sterling Winthrop Inc. Saccharin derivative proteolytic enzyme inhibitors
AU668694B2 (en) 1991-12-19 1996-05-16 Sanofi-Synthelabo Saccharin derivative proteolytic enzyme inhibitors
TW219935B (es) 1991-12-25 1994-02-01 Mitsubishi Chemicals Co Ltd
GB9200293D0 (en) 1992-01-08 1992-02-26 Wyeth John & Brother Ltd Piperazine derivatives
GB9201694D0 (en) 1992-01-27 1992-03-11 Smithkline Beecham Intercredit Compounds
JPH05204071A (ja) 1992-01-29 1993-08-13 Konica Corp ハロゲン化銀写真感光材料
JP3042156B2 (ja) 1992-02-20 2000-05-15 田辺製薬株式会社 ナフタレン誘導体、その製法及びその合成中間体
DE4206045A1 (de) 1992-02-27 1993-09-02 Bayer Ag Sulfonylbenzyl substituierte pyridone
JPH06110557A (ja) 1992-09-28 1994-04-22 Stec Kk マスフローコントローラ
US5922773A (en) 1992-12-04 1999-07-13 The Children's Medical Center Corp. Glaucoma treatment
AU660132B2 (en) 1992-12-21 1995-06-08 Bayer Aktiengesellschaft Substituted 4-phenyl-pyridones and 4-phenyl-2-alkoxypyridine
JPH06211797A (ja) 1993-01-19 1994-08-02 Tosoh Corp テトラヒドロイソキノリン誘導体、その製法及び抗真菌剤
JPH06211798A (ja) 1993-01-19 1994-08-02 Tosoh Corp テトラヒドロイソキノリノン誘導体及びその製造方法
SE9300657D0 (sv) 1993-02-26 1993-02-26 Astra Ab New compounds
US5814645A (en) 1993-03-24 1998-09-29 Bayer Aktiengesellschaft Arylor hetaryl substituted nitrogen heterocycles and their use as pesticides
DE4316077A1 (de) 1993-05-13 1994-11-17 Bayer Ag Substituierte Mono- und Bihydridylmethylpyridone
EP0702671A4 (en) 1993-06-09 1996-06-19 Smithkline Beecham Corp BICYCLIC FIBRINOGEN ANTAGONISTS
JPH07101861A (ja) 1993-08-10 1995-04-18 Tanabe Seiyaku Co Ltd 抗喘息薬
DE4326758A1 (de) 1993-08-10 1995-02-16 Basf Ag [1,3,4]Triazolo[1,5-a]pyridine
US5824682A (en) 1993-08-18 1998-10-20 Janssen Pharmaceutica, N.V. Vasoconstrictive dihydrobenzopyran derivatives
PL179008B1 (pl) 1993-08-19 2000-07-31 Janssen Pharmaceutica Nv Nowy zwiazek, podstawiona aryloksyalkilodwuamina o dzialaniu naczyniozwezajacym, kompozycja farmaceutycznai sposób wytwarzania podstawionej aryloksyalkilodwuaminy. PL PL
WO1995006032A1 (en) 1993-08-20 1995-03-02 Banyu Pharmaceutical Co., Ltd. Tyrosine kinase inhibitor
JP3701984B2 (ja) 1993-08-31 2005-10-05 サントリー株式会社 ラベル化シクロプロパン誘導体およびその製造方法
US5424435A (en) 1993-10-18 1995-06-13 Olin Corporation 1-hydroxy-6-substituted-2-pyridones
US5500420A (en) 1993-12-20 1996-03-19 Cornell Research Foundation, Inc. Metabotropic glutamate receptor agonists in the treatment of cerebral ischemia
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
EP0749424B1 (en) 1994-03-10 2001-09-12 Fujisawa Pharmaceutical Co., Ltd. Naphthalene derivatives as prostaglandin i2 agonists
ES2079323B1 (es) 1994-06-21 1996-10-16 Vita Invest Sa Derivados de indol utiles para el tratamiento de la migraña, composicion y uso correspondientes.
GB9416554D0 (en) 1994-08-19 1994-10-12 Ciba Geigy Ag Glutamate receptor
WO1996005828A1 (en) 1994-08-24 1996-02-29 Eli Lilly And Company Pyrrolidinyl di-carboxylic acid derivatives as metabotropic glutamate receptor antagonists
US5473077A (en) 1994-11-14 1995-12-05 Eli Lilly And Company Pyrrolidinyl di-carboxylic acid derivatives as metabotropic glutamate receptor agonists
US6017697A (en) 1994-11-14 2000-01-25 Eli Lilly And Company Excitatory amino acid receptor protein and related nucleic acid compounds
US5512576A (en) 1994-12-02 1996-04-30 Sterling Winthrop Inc. 2-substituted 1,2,5,-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
US5789426A (en) 1995-01-20 1998-08-04 Cornell Research Foundation, Inc. Method for the treatment of fibroproliferative disorders by application of inhibitors of protein hydroxylation
US5869486A (en) 1995-02-24 1999-02-09 Ono Pharmaceutical Co., Ltd. Fused pyrimidines and pyriazines as pharmaceutical compounds
DE19507522C2 (de) 1995-03-03 2003-05-28 Basf Ag Verfahren zur Herstellung von 3,4-Dihydroisochinolinverbindungen und 3,4-Dihydroisochinolinium-Salzen
TW324008B (en) 1995-03-13 1998-01-01 Ishihara Sangyo Kaisha Pyridone sulfonylurea compound, its production process and weed killer containing such compound
DE19510965A1 (de) 1995-03-24 1996-09-26 Asta Medica Ag Neue Pyrido/3,2-e/pyrazinone mit antiasthmatischer Wirksamkeit und Verfahren zu deren Herstellung
EP0826671B1 (en) 1995-04-27 2004-12-29 Mitsubishi Pharma Corporation Heterocyclic amide compounds and medicinal use of the same
JPH08325248A (ja) 1995-05-26 1996-12-10 Chugoku Kayaku Kk テトラゾール類の新規な合成試薬及びそれを用いたテトラゾール類の製造方法
US5849587A (en) 1995-06-09 1998-12-15 Cornell Research Foundation, Inc. Method of inhibiting viral replication in eukaryotic cells and of inducing apoptosis of virally-infected cells
US5659033A (en) 1995-09-13 1997-08-19 Neurogen Corporation N-aminoalkylfluorenecarboxamides; a new class of dopamine receptor subtype specific ligands
US5958924A (en) 1995-09-15 1999-09-28 Synthelabo Quinolein-2 (1H)-one derivatives as serotonin antagonists
JPH1045750A (ja) 1995-09-20 1998-02-17 Takeda Chem Ind Ltd アゾール化合物、その製造方法及び用途
US6130217A (en) 1995-09-20 2000-10-10 Pfizer Inc Compounds enhancing antitumor activity of other cytotoxic agents
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
DE19540027A1 (de) 1995-10-27 1997-04-30 Gruenenthal Gmbh Substituierte Imidazolidin-2,4-dion-Verbindungen als pharmazeutische Wirkstoffe
US5554607A (en) 1995-11-28 1996-09-10 American Home Products Corporation Use of 2-thioxo-imidazolin-4-one derivatives in the treatment of atherosclerosis
TW418195B (en) 1995-11-28 2001-01-11 American Home Prod 2-thioxo-imidazolidin-4-one derivatives
WO1997021701A1 (en) 1995-12-08 1997-06-19 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivatives
EP0880501A1 (en) 1996-02-02 1998-12-02 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
GB9602166D0 (en) 1996-02-02 1996-04-03 Zeneca Ltd Aminoheterocyclic derivatives
GB9602294D0 (en) 1996-02-05 1996-04-03 Zeneca Ltd Heterocyclic compounds
US6084084A (en) 1996-02-21 2000-07-04 Nps Pharmaceuticals, Inc. Human metabotropic glutamate receptor
US5710274A (en) 1996-02-28 1998-01-20 Neurogen Corporation N-aminoalkyldibenzofurancarboxamides; new dopamine receptor subtype specific ligands
US5756518A (en) 1996-04-02 1998-05-26 Kowa Co., Ltd. Phenylene derivatives
JPH1029979A (ja) 1996-04-12 1998-02-03 Ajinomoto Co Inc 新規ピリジン誘導体
WO1997046532A1 (en) 1996-06-03 1997-12-11 Boehringer Ingelheim Pharmaceuticals, Inc. 2-benzyl-4-sulfonyl-4h-isoquinolin-1,3-diones and their use as anti-inflammatory agents
AU3783497A (en) 1996-08-09 1998-03-06 Yamanouchi Pharmaceutical Co., Ltd. Metabotropic glutamate receptor agonists
DE19632423A1 (de) 1996-08-12 1998-02-19 Merck Patent Gmbh Thienopyrimidine
AU3701797A (en) 1996-08-14 1998-03-06 Zeneca Limited Substituted pyrimidine derivatives and their pharmaceutical use
AU4270297A (en) 1996-09-16 1998-04-02 Du Pont Pharmaceuticals Company Pyrazinones and triazinones and their derivatives thereof
DE19638486A1 (de) 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
DE19638484A1 (de) 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
DE19644228A1 (de) 1996-10-24 1998-04-30 Merck Patent Gmbh Thienopyrimidine
US6284794B1 (en) 1996-11-05 2001-09-04 Head Explorer Aps Method for treating tension-type headache with inhibitors of nitric oxide and nitric oxide synthase
AU735901C (en) 1996-12-05 2004-02-12 Amgen, Inc. Substituted pyrimidinone and pyridone compounds and methods of use
DK0986570T3 (da) 1997-01-24 2003-07-28 Conpharma As Gemcitabinderivat
US5855654A (en) 1997-01-30 1999-01-05 Rohm And Haas Company Pyridazinones as marine antifouling agents
FR2759366B1 (fr) 1997-02-11 1999-04-16 Centre Nat Rech Scient Composes constituant notamment des effecteurs de recepteurs du systeme nerveux central sensibles aux amino acides neuroexcitateurs, leur preparation et leurs applications biologiques
US6262068B1 (en) 1997-02-21 2001-07-17 Bristol-Myers Squibb Company Lactam derivatives as antiarrhythmic agents
WO1998038168A1 (en) 1997-02-27 1998-09-03 Tanabe Seiyaku Co., Ltd. Isoquinolinone derivatives, process for preparing the same, and their use as phosphodiesterase inhibitors
ES2131463B1 (es) 1997-04-08 2000-03-01 Lilly Sa Derivados de ciclopropilglicina con propiedades farmaceuticas.
GB9708945D0 (en) 1997-05-01 1997-06-25 Merck Sharp & Dohme Therapeutic agents
DE19728996A1 (de) 1997-07-07 1999-01-14 Basf Ag Triazolverbindungen und deren Verwendung
AU743899B2 (en) 1997-07-18 2002-02-07 Georgetown University Bicyclic metabotropic glutamate receptor ligands
DK0891978T3 (da) 1997-07-18 2002-07-01 Hoffmann La Roche 5H-Thiazol(3,2-a)pyrimidinderivativer
CN1265590A (zh) 1997-07-31 2000-09-06 赛尔金有限公司 取代的链烷异羟肟酸及降低肿瘤坏死因子α水平的方法
IL134168A0 (en) 1997-08-14 2001-04-30 Hoffmann La Roche Heterocyclic vinylethers against neurological disorders
US6358975B1 (en) 1997-08-15 2002-03-19 Johns Hopkins University Method of using selective parp inhibitors to prevent or treat neurotoxicity
US6635642B1 (en) 1997-09-03 2003-10-21 Guilford Pharmaceuticals Inc. PARP inhibitors, pharmaceutical compositions comprising same, and methods of using same
US6121278A (en) 1997-09-03 2000-09-19 Guilford Pharmaceuticals, Inc. Di-n-heterocyclic compounds, methods, and compositions for inhibiting parp activity
US20020022636A1 (en) 1997-09-03 2002-02-21 Jia-He Li Oxo-substituted compounds, process of making, and compositions and methods for inhibiting parp activity
US6197785B1 (en) 1997-09-03 2001-03-06 Guilford Pharmaceuticals Inc. Alkoxy-substituted compounds, methods, and compositions for inhibiting PARP activity
US20020028813A1 (en) 1997-09-03 2002-03-07 Paul F. Jackson Thioalkyl compounds, methods, and compositions for inhibiting parp activity
AU9298098A (en) 1997-09-03 1999-03-22 Guilford Pharmaceuticals Inc. Amino-substituted compounds, methods, and compositions for inhibiting parp activity
AU9740998A (en) 1997-09-08 1999-03-29 F. Hoffmann-La Roche Ag Piperidine derivatives against malaria
EP0903343B1 (en) 1997-09-19 2003-05-28 SSP Co., Ltd. Alpha-Substituted phenylpropionic acid derivative and medicine containing the same
EP1017682A4 (en) 1997-09-26 2000-11-08 Merck & Co Inc NEW ANGIOGENESIS INHIBITORS
US6465484B1 (en) 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
US6162804A (en) 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
WO1999018096A1 (en) 1997-10-02 1999-04-15 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
JP3329337B2 (ja) 1997-10-14 2002-09-30 三菱ウェルファーマ株式会社 ピペラジン化合物およびその医薬としての用途
WO1999021992A2 (en) 1997-10-23 1999-05-06 Ganimed Pharmaceuticals Gmbh Nucleic acid molecules encoding a glutamate receptor
JP4321737B2 (ja) 1997-12-17 2009-08-26 塩野義製薬株式会社 新規ピリジン化合物
EP1045836B1 (en) 1997-12-18 2008-03-05 Boehringer Ingelheim Pharmaceuticals Inc. Pyridones as src family sh2 domain inhibitors
US6013672A (en) 1997-12-18 2000-01-11 Uab Research Foundation Agonists of metabotropic glutamate receptors and uses thereof
ATE389636T1 (de) 1997-12-19 2008-04-15 Amgen Inc Substituierte pyridin- und pyridazinderivate und ihre pharmazeutische verwendung
FR2772763B1 (fr) 1997-12-24 2004-01-23 Sod Conseils Rech Applic Nouveaux analogues tetracycliques de camptothecines, leurs procedes de preparation, leur application comme medicaments et les compositions pharmaceutiques les contenant
IT1298155B1 (it) 1998-01-19 1999-12-20 Moreno Paolini Composti pirimidin 3-ossido per il trattamento delle patologie muscolo-scheletriche, in particolare per il trattamento della
US6664250B2 (en) 1998-01-20 2003-12-16 Bristol-Myers Squibb Co. Lactam derivatives as antiarrhythmic agents
US6316498B1 (en) 1998-01-28 2001-11-13 Taisho Pharmaceutical Co., Ltd. Fluorine-containing amino acid derivatives
ATE245641T1 (de) 1998-02-17 2003-08-15 Tularik Inc Antivirale pyrimidinderivate
JP3665567B2 (ja) 1998-03-17 2005-06-29 ファイザー・プロダクツ・インク ビシクロ［２．２．１］ヘプタンおよび関連化合物
CN1295570A (zh) 1998-04-08 2001-05-16 诺瓦提斯公司 N－吡啶酮基除草剂
AU3170099A (en) 1998-04-16 1999-11-08 Yamanouchi Pharmaceutical Co., Ltd. Remedies for obesity
EP0955301A3 (en) 1998-04-27 2001-04-18 Pfizer Products Inc. 7-aza-bicyclo[2.2.1]-heptane derivatives, their preparation and use according to their affinity for neuronal nicotinic acetylcholine receptors
DE19822198C2 (de) 1998-05-16 2003-02-13 Wella Ag Oxonolfarbstoffe enthaltende Mittel und Verfahren zur Erzeugung von semipermanenten Färbungen auf Haaren
PL345906A1 (en) 1998-06-04 2002-01-14 Abbott Lab Cell adhesion-inhibiting antinflammatory compounds
DE19826671A1 (de) 1998-06-16 1999-12-23 Hoechst Schering Agrevo Gmbh 1,3-Oxazolin- und 1,3-Thiazolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel
FR2781218B1 (fr) 1998-07-15 2001-09-07 Lafon Labor Compositions pharmaceutiques comprenant des 2-quinolones
JP2000072751A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd イソキノリノン誘導体
ATE269293T1 (de) 1998-08-31 2004-07-15 Taisho Pharmaceutical Co Ltd 6-fluoro(3.1.0)hexan-derivate
AU760020B2 (en) 1998-08-31 2003-05-08 Merck & Co., Inc. Novel angiogenesis inhibitors
JP2000072731A (ja) 1998-08-31 2000-03-07 Taisho Pharmaceut Co Ltd ４−置換−２−アミノビシクロ［３．１．０］ヘキサン−２，６−ジカルボン酸誘導体及び製薬用組成物
CH694053A5 (de) 1998-09-03 2004-06-30 Hoffmann La Roche Verfahren zur Herstellung von 2-Amino-bicyclo[3.1.0]hexan-2,6-dicarbonsäure-Derivaten.
US6284759B1 (en) 1998-09-30 2001-09-04 Neurogen Corporation 2-piperazinoalkylaminobenzo-azole derivatives: dopamine receptor subtype specific ligands
SE9803518D0 (sv) 1998-10-15 1998-10-15 Astra Pharma Prod Novel compounds
AU1308400A (en) 1998-10-30 2000-05-22 G.D. Searle & Co. Novel amino acid heterocyclic amide derivatives useful as nitric oxide synthase inhibitors
PE20001236A1 (es) 1998-11-13 2000-11-10 Lilly Co Eli Moduladores del receptor de aminoacidos excitadores
US6133271A (en) 1998-11-19 2000-10-17 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure thienopyrimidine derivatives
US5948911A (en) 1998-11-20 1999-09-07 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure to thienopyrimidine derivatives
EP1006112A1 (en) 1998-12-01 2000-06-07 Cerebrus Pharmaceuticals Limited 3-Hydroxy-2(1H)-pyridinone or 3-hydroxy-4(1H)-pyridinone derivatives useful as reactive oxygen species (ROS) scavengers
EP1133474B1 (en) 1998-12-04 2007-02-21 Bristol-Myers Squibb Company 3-substituted-4-arylquinolin-2-one derivatives as potassium channel modulators
AU2847200A (en) 1999-01-27 2000-08-18 G.D. Searle & Co. Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors
US6245759B1 (en) 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
TW564247B (en) 1999-04-08 2003-12-01 Akzo Nobel Nv Bicyclic heteraromatic compound
GB9908175D0 (en) 1999-04-09 1999-06-02 Lilly Co Eli Method of treating neurological disorders
US6972296B2 (en) 1999-05-07 2005-12-06 Encysive Pharmaceuticals Inc. Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
US6723711B2 (en) 1999-05-07 2004-04-20 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
EP1183238A1 (en) 1999-05-17 2002-03-06 Eli Lilly And Company Metabotropic glutamate receptor antagonists
NZ515894A (en) 1999-06-02 2003-09-26 Nps Pharma Inc Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases
US6498180B1 (en) 1999-06-03 2002-12-24 Eli Lilly And Company Excitatory amino acid receptor modulators
JP2004509059A (ja) 1999-06-03 2004-03-25 アボット・ラボラトリーズ 細胞接着抑制性抗炎症化合物
JP4783967B2 (ja) 1999-07-21 2011-09-28 大正製薬株式会社 含フッ素アミノ酸誘導体を有効成分とする医薬
US6350763B1 (en) 1999-07-21 2002-02-26 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammation disease
AU6420700A (en) 1999-08-05 2001-03-05 Prescient Neuropharma Inc. Novel 1,4-benzodiazepine compounds and derivatives thereof
US6660753B2 (en) 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
US7040838B2 (en) 1999-08-27 2006-05-09 Kristar Enterprises, Inc. High capacity catch basin filtration system with adjustable deflector ring
CN2390948Y (zh) 1999-09-17 2000-08-09 徐平武 混凝土屋顶、楼面施工金属组合专用模具
SI1224174T1 (en) 1999-10-15 2003-12-31 F. Hoffmann-La Roche Ag Benzodiazepine derivatives as metabotropic glutamate receptor antagonists
HUP0203294A3 (en) 1999-10-15 2003-03-28 Hoffmann La Roche Benzodiazepine derivatives, process for their preparation, pharmaceutical compositions containing them and their use
CA2387351C (en) 1999-10-19 2009-09-08 Merck & Co., Inc. Indole derivatives as tyrosine kinase inhibitors
SV2002000205A (es) 1999-11-01 2002-06-07 Lilly Co Eli Compuestos farmaceuticos ref. x-01095
GB2355982A (en) 1999-11-03 2001-05-09 Lilly Co Eli Heterocyclic amino acids
AU2220801A (en) 1999-12-22 2001-07-03 Kyorin Pharmaceutical Co. Ltd. Tricyclic compounds and addition salts thereof
EP1254904B1 (en) 2000-01-20 2006-05-24 Eisai Co., Ltd. Novel piperidine compounds and drugs containing the same
GB0002100D0 (en) 2000-01-28 2000-03-22 Novartis Ag Organic compounds
US6800651B2 (en) 2000-02-03 2004-10-05 Eli Lilly And Company Potentiators of glutamate receptors
KR100521735B1 (ko) 2000-02-25 2005-10-17 에프. 호프만-라 로슈 아게 아데노신 수용체 조절인자
DE10012373A1 (de) 2000-03-14 2001-09-20 Dresden Arzneimittel Verwendung von Pyrido[3,2-e]-pyrazinonen als Inhibitoren der Phosphodiesterase 5 zur Therapie von erektiler Dysfunktion
GB0007108D0 (en) 2000-03-23 2000-05-17 Novartis Ag Organic compounds
US6469026B2 (en) 2000-03-24 2002-10-22 Millennium Pharmaceuticals, Inc. Isoquinolone inhibitors of factor Xa
GB0007193D0 (en) 2000-03-25 2000-05-17 Univ Manchester Treatment of movrmrnt disorders
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
WO2001083481A1 (fr) 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Derives d'imidazopyridine
EP1288199A4 (en) 2000-04-28 2005-10-12 Shionogi & Co INHIBITORS OF MMP-12
EP1277726B1 (en) 2000-04-28 2007-01-03 Nihon Nohyaku Co., Ltd. Process for the preparation of 2-halobenzoic acids
US20020009713A1 (en) 2000-05-11 2002-01-24 Miller Freda D. Methods for identifying modulators of neuronal growth
JP2004507457A (ja) 2000-05-11 2004-03-11 協和醗酵工業株式会社 ２−ピペリドン化合物
US20040077599A1 (en) 2000-05-11 2004-04-22 Kenneth Curry Novel spiro[2.4]heptane amino carboxy compounds and derivatives thereof
MXPA02011858A (es) 2000-05-31 2004-07-30 Tanabe Seiyaku Co Inhibidores de adhesion de celula mediada por alfabeta2.
US7081481B2 (en) 2000-05-31 2006-07-25 Eli Lilly And Company Excitatory amino acid receptor modulators
DE60137426D1 (de) 2000-06-12 2009-03-05 Eisai R&D Man Co Ltd 1,2-dihydropyridinverbindungen, verfahren zu deren herstellung und deren verwendung
JP2002003401A (ja) 2000-06-27 2002-01-09 Japan Science & Technology Corp 脳由来神経栄養因子誘導剤
CA2413747A1 (en) 2000-06-27 2002-01-03 Centre National De La Recherche Scientifique Mammal 2p domain mechano-sensitive k+ channel, cloning and applications thereof
JP2002012533A (ja) 2000-06-27 2002-01-15 Kao Corp 染毛剤組成物
CN1216038C (zh) 2000-06-28 2005-08-24 大正制药株式会社 新型二羧酸衍生物
DE10031390A1 (de) 2000-07-03 2002-01-17 Knoll Ag Pyrimidinderivate und ihre Verwendung zur Prophylaxe und Therapie der zerebralen Ischämie
US20020041880A1 (en) 2000-07-05 2002-04-11 Defeo-Jones Deborah Method of treating cancer
US6861530B2 (en) 2000-07-07 2005-03-01 Kyowa Hakko Kogyo Co., Ltd. Piperidine derivatives
JP2002040252A (ja) 2000-07-27 2002-02-06 Shiseido Co Ltd コレステリック液晶層を含む光学シート、それを用いた情報記録体、情報記録方法並びに情報判別方法
DE10038019A1 (de) 2000-08-04 2002-02-14 Bayer Ag Substituierte Triazolopyrid(az)ine
KR100804111B1 (ko) 2000-08-11 2008-02-18 에자이 알앤드디 매니지먼트 가부시키가이샤 2-아미노피리딘 화합물 및 그의 의약 용도
BRPI0113757B1 (pt) 2000-09-11 2017-05-23 Chiron Corp derivados de quinolinona como inibibores de tirosina quinase
AU2002213422A1 (en) 2000-09-13 2002-03-26 Georgetown University Synthesis of 2-hydroxymethylglutamic acid and congeners thereof
JP2002105085A (ja) 2000-09-28 2002-04-10 Yamanouchi Pharmaceut Co Ltd 新規イミダゾチアゾール誘導体
AU2001293847B2 (en) 2000-10-02 2007-05-24 Janssen Pharmaceutica N.V. Metabotropic glutamate receptor antagonists
DE10058663A1 (de) 2000-11-25 2002-05-29 Merck Patent Gmbh Verwendung von Thienopyrimidinen
WO2002051849A1 (fr) 2000-12-26 2002-07-04 Daiichi Pharmaceutical Co., Ltd. Inhibiteurs cdk4
US6977266B2 (en) 2000-12-28 2005-12-20 Shionogi & Co., Ltd. Pyridone derivatives having affinity for cannabinoid 2-type receptor
JP2002308882A (ja) 2001-02-08 2002-10-23 Yamanouchi Pharmaceut Co Ltd チエノピリミジン誘導体
AU2002258400A1 (en) 2001-02-16 2002-08-28 Tularik Inc. Methods of using pyrimidine-based antiviral agents
JP4343534B2 (ja) 2001-03-02 2009-10-14 ゲーペーツェー バイオテック アクチェンゲゼルシャフト ３ハイブリッド・アッセイ・システム
DE10291003D2 (de) 2001-03-08 2004-04-15 Ilfa Industrieelektronik Und L Mehrschichtige Leiterplatte
US6596731B2 (en) 2001-03-27 2003-07-22 Hoffmann-La Roche Inc. Substituted imidazo[1,2-A] pyridine derivatives
EP1385983A4 (en) 2001-04-02 2005-11-16 Merck & Co Inc IN VIVO METHODS FOR DETERMINING THE ACTIVITY OF RECEPTOR-TYPE KINASE INHIBITORS
FR2823209B1 (fr) 2001-04-04 2003-12-12 Fournier Lab Sa Nouvelles thiohydantoines et leur utilisation en therapeutique
IL157873A0 (en) 2001-04-12 2004-03-28 Hoffmann La Roche DIHYDRO-BENZO [b] [1,4] DIAZEPIN-2-ONE DERIVATIVES AS MGLUR2 ANTAGONISTS II
CZ20033002A3 (cs) 2001-04-12 2004-03-17 F. Hoffmann-La Roche Ag Deriváty dihydrobenzo [b] [1,4]diazepin-2-onu jako antagonisty mGluR2
SE0101579D0 (sv) 2001-05-04 2001-05-04 Astrazeneca Ab New compounds
SK13752003A3 (en) 2001-05-14 2004-11-03 Bristol Myers Squibb Pharma Co Substituted pyrazinones, pyridines and pyrimidines as ligands of factor releasing corticotropine
US7144903B2 (en) 2001-05-23 2006-12-05 Amgen Inc. CCR4 antagonists
JP2004536807A (ja) 2001-05-30 2004-12-09 アルテオン インコーポレイテッド 緑内障ｖの治療方法
CA2448306A1 (en) 2001-05-30 2002-12-05 Alteon Inc. Method for treating fibrotic diseases or other indications
JP4424983B2 (ja) 2001-06-05 2010-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド １，４−ジ置換ベンゾ−縮合シクロアルキルウレア化合物
WO2002102807A1 (fr) 2001-06-14 2002-12-27 Banyu Pharmaceutical Co., Ltd. Nouveaux derives d'isoxazolopyridone et leur utilisation
EP1397142A4 (en) 2001-06-19 2004-11-03 Bristol Myers Squibb Co PYRIMIDINE PHOSPHODIESTERASE (PDE) INHIBITORS 7
JP2003012653A (ja) 2001-06-28 2003-01-15 Yamanouchi Pharmaceut Co Ltd キナゾリン誘導体
US6750350B2 (en) 2001-08-02 2004-06-15 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
WO2003022852A2 (en) 2001-09-11 2003-03-20 Smithkline Beecham Corporation Furo-and thienopyrimidine derivatives as angiogenesis inhibitors
JP4459619B2 (ja) 2001-10-02 2010-04-28 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 化合物
WO2003032994A2 (de) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren
TWI330183B (es) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
TW200406466A (en) 2001-11-13 2004-05-01 Ciba Sc Holding Ag Compositions comprising at least one oxonol dye and at least one metal complex
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
GB0129260D0 (en) 2001-12-06 2002-01-23 Eisai London Res Lab Ltd Pharmaceutical compositions and their uses
MXPA04005790A (es) 2001-12-14 2004-09-13 Novo Nordisk As Compuestos y usos de los mismos para reducir la actividad de la lipasa sensible a la hormona.
EP1465869B1 (en) 2001-12-21 2013-05-15 Exelixis Patent Company LLC Modulators of lxr
CA2471642C (en) 2001-12-27 2011-05-24 Taisho Pharmaceutical Co., Ltd. 6-fluorobicyclo[3.1.0]hexane derivatives
DE10164139A1 (de) 2001-12-27 2003-07-10 Bayer Ag 2-Heteroarylcarbonsäureamide
JP2005170790A (ja) 2002-01-09 2005-06-30 Ajinomoto Co Inc Ｎ−アルキルスルフォニル置換アミド誘導体
JP2005515254A (ja) 2002-01-17 2005-05-26 スミスクライン ビーチャム コーポレーション カテプシンｋ阻害剤として有用なシクロアルキルケトアミド誘導体
US20050113283A1 (en) 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
JP2005519915A (ja) 2002-01-18 2005-07-07 セレテック・リミテッド・ライアビリティ・カンパニー Ｅｄｇ受容体に関連する症状の処置方法
WO2003064428A1 (en) 2002-01-29 2003-08-07 H. Lundbeck A/S Furano- and thienopyrimidines as neurokinase inhibitors
US6949542B2 (en) 2002-02-06 2005-09-27 Hoffman-La Roche Inc. Dihydro-benzo[b][1,4]diazepin-2-one derivatives
US20030220280A1 (en) 2002-02-07 2003-11-27 Bunge Mary Bartlett Schwann cell bridge implants and phosphodiesterase inhibitors to stimulate CNS nerve regeneration
US20040116489A1 (en) 2002-02-12 2004-06-17 Massey Steven Marc Synthetic excitatory amino acids
AU2003211931A1 (en) 2002-02-13 2003-09-04 Takeda Chemical Industries, Ltd. Jnk inhibitor
CA2476012C (en) 2002-02-14 2011-04-19 Pharmacia Corporation Substituted pyridinones as modulators of p38 map kinase
AU2003205558A1 (en) 2002-02-19 2003-09-09 H. Lundbeck A/S Thioibotenic acid and derivatives thereof
US6833380B2 (en) 2002-03-07 2004-12-21 Warner-Lambert Company, Llc Compounds that modulate PPAR activity and methods of preparation
PL372427A1 (en) 2002-03-14 2005-07-25 Bayer Healthcare Ag Monocyclic aroylpyridinones as antiinflammatory agents
CA2479744A1 (en) 2002-03-28 2003-10-09 Paul E. Finke Substituted 2,3-diphenyl pyridines
EA009334B1 (ru) 2002-03-29 2007-12-28 Янссен Фармацевтика Н.В. Меченные радиоактивными изотопами производные хинолина и их применение в качестве лигандов метаботропного глутаматного рецептора
WO2003084610A1 (en) 2002-04-03 2003-10-16 Eli Lilly And Company Therapy for psychoses combining an atypical antipsychotic and an mglu2/3 receptor agonist
US6864261B2 (en) 2002-05-02 2005-03-08 Euro-Celtique S.A. Therapeutic agents useful for treating pain
WO2003092595A2 (en) 2002-05-02 2003-11-13 Merck & Co., Inc Tyrosine kinase inhibitors
TW200407324A (en) 2002-05-17 2004-05-16 Bristol Myers Squibb Co Bicyclic modulators of androgen receptor function
WO2003099808A1 (en) 2002-05-21 2003-12-04 Amgen Inc. Substituted heterocyclic compounds and methods of use
AU2003232146B2 (en) 2002-06-11 2009-06-18 Eli Lilly And Company Prodrugs of excitatory amino acids
PL374191A1 (en) 2002-06-13 2005-10-03 Vertex Pharmaceuticals Incorporated 2-ureido-6-heteroaryl-3h-benzoimidazole-4-carboxylic acid derivatives and related compounds as gyrase and/or topoisomerase iv inhibitors for the treatment of bacterial infections
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
GB0214268D0 (en) 2002-06-20 2002-07-31 Celltech R&D Ltd Chemical compounds
AU2003246927A1 (en) 2002-07-03 2004-01-23 Astex Technology Limited 3-`(hetero) arylmethoxy ! pyridines and their analogues as p38 map kinase inhibitors
US7262194B2 (en) 2002-07-26 2007-08-28 Euro-Celtique S.A. Therapeutic agents useful for treating pain
US20040138238A1 (en) 2002-08-08 2004-07-15 Dhanoa Dale S. Substituted aminopyrimidine compounds as neurokinin antagonists
GB0218630D0 (en) 2002-08-10 2002-09-18 Tanabe Seiyaku Co Novel compounds
GB0218800D0 (en) 2002-08-13 2002-09-18 Celltech R&D Ltd Chemical compounds
WO2004017950A2 (en) 2002-08-22 2004-03-04 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
AU2003262805A1 (en) 2002-08-26 2004-03-11 Merck & Co., Inc. Acetophenone potentiators of metabotropic glutamate receptors
US20060110358A1 (en) 2002-08-28 2006-05-25 Hsu Henry H Combination therapy for treatment of fibrotic disorders
MY139563A (en) 2002-09-04 2009-10-30 Bristol Myers Squibb Co Heterocyclic aromatic compounds useful as growth hormone secretagogues
AU2002951247A0 (en) 2002-09-06 2002-09-19 Alchemia Limited Compounds that interact with kinases
CA2498022C (en) 2002-09-10 2012-10-23 Novartis Ag Combination of mglur antagonists for the treatment of addictive disorders
US20060147923A1 (en) 2002-09-11 2006-07-06 Daggett Lorrie P Nucleic acid sequences encoding novel point mutations on mglur2 and mglur3
JP2006505532A (ja) 2002-09-19 2006-02-16 ベーリンガー インゲルハイム （カナダ） リミテッド 非ヌクレオシド逆転写酵素インヒビター
ATE331716T1 (de) 2002-09-19 2006-07-15 Boehringer Ingelheim Ca Ltd Nicht-nukleosidische inhibitoren der reverse transkriptase
TW200410975A (en) 2002-09-26 2004-07-01 Nihon Nohyaku Co Ltd New pesticide and method for using it, new substituted thienopyrimidine derivative, its intermediate, and method for producing it
US7067658B2 (en) 2002-09-30 2006-06-27 Bristol-Myers Squibb Company Pyridino and pyrimidino pyrazinones
US7998163B2 (en) 2002-10-03 2011-08-16 Boston Scientific Scimed, Inc. Expandable retrieval device
US7393549B2 (en) 2002-10-23 2008-07-01 Daiichi Pure Chemicals Co., Ltd. Defructosylation method
US20040138204A1 (en) 2002-10-30 2004-07-15 Harrington James Frederick Compositions and methods for pain reduction
MXPA05004670A (es) 2002-11-01 2005-08-18 Abbott Lab Agentes anti-infecciones.
US7902203B2 (en) 2002-11-01 2011-03-08 Abbott Laboratories, Inc. Anti-infective agents
US6930117B2 (en) 2002-11-09 2005-08-16 The Procter & Gamble Company N-alkyl-4-methyleneamino-3-hydroxy-2-pyridones
CA2507100C (en) 2002-11-21 2012-10-09 Chiron Corporation 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer
WO2004054979A1 (ja) 2002-12-18 2004-07-01 Takeda Pharmaceutical Company Limited Ｊｎｋ阻害剤
JP5269281B2 (ja) 2002-12-30 2013-08-21 セルジーン コーポレイション フルオロアルコキシ置換１，３−ジヒドロイソインドリル化合物およびそれらの医薬としての使用
EP1599468B1 (en) 2003-01-14 2007-10-03 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
ITMI20030151A1 (it) 2003-01-30 2004-07-31 Recordati Ind Chimica E Farma Ceutica S P A Uso di antagonisti selettivi del recettore mglu5 per il trattamento di disfunzioni neuromuscolari del tratto urinario inferiore.
EP1592684B1 (en) 2003-02-04 2008-07-30 F. Hoffmann-La Roche Ag Malonamide derivatives as gamma-secretase inhibitors
DE10306250A1 (de) 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CN1751038A (zh) 2003-02-24 2006-03-22 艾尼纳制药公司 作为葡萄糖代谢调节剂的经取代芳基和杂芳基衍生物及葡萄糖代谢失调的预防和治疗
DE602004010791T2 (de) 2003-03-03 2008-12-04 F. Hoffmann-La Roche Ag 2,5-substituiertetetrahydroisochinoline zur verwendung als 5-ht6 modulatoren
ITFI20030058A1 (it) 2003-03-06 2004-09-07 Univ Firenze Formulazioni farmaceutiche contenenti tiazolidinedioni
DE10311065A1 (de) 2003-03-13 2004-09-23 Abbott Gmbh & Co. Kg Pyrimidin-2-on-Verbindungen und ihre therapeutische Verwendung
WO2004092123A2 (en) 2003-04-10 2004-10-28 Microbia, Inc. Inhibitors of fungal invasion
JP2006523707A (ja) 2003-04-15 2006-10-19 アストラゼネカ アクツィエボラーグ 治療化合物
JP2004339080A (ja) 2003-05-13 2004-12-02 Tokyo Institute Of Technology ピラゾ−ル誘導体を含有する高血圧治療剤
WO2004110350A2 (en) 2003-05-14 2004-12-23 Torreypines Therapeutics, Inc. Compouds and uses thereof in modulating amyloid beta
EP1624900A4 (en) 2003-05-20 2007-05-02 Univ California METHOD OF BINDING AGENTS AT BETA AMYLOID PLAQUE
GB0315950D0 (en) 2003-06-11 2003-08-13 Xention Discovery Ltd Compounds
EP1636205A1 (en) 2003-06-12 2006-03-22 Novo Nordisk A/S Pyridinyl carbamates as hormone-sensitive lipase inhibitors
CA2572324A1 (en) 2003-07-02 2005-01-13 Warner-Lambert Company Llc Combination of an allosteric inhibitor of matrix metalloproteinase-13 and a ligand to an alpha-2-delta receptor
MXPA06000514A (es) 2003-07-14 2006-06-20 Decode Genetics Ehf Metodos de diagnostico y tratamiento del asma y otras enfermedades respiratorias basandose en la asociacion de haplotipos.
GB0320300D0 (en) 2003-08-29 2003-10-01 Cancer Rec Tech Ltd Pyrimidothiophene compounds
BRPI0413861A (pt) 2003-08-29 2006-10-24 Vernalis Cambridge Ltd compostos de pirimidotiofeno
GB0322016D0 (en) 2003-09-19 2003-10-22 Merck Sharp & Dohme New compounds
PE20050444A1 (es) 2003-10-31 2005-08-09 Takeda Pharmaceutical Compuestos de piridina como inhibidores de la peptidasa
BRPI0507498A (pt) 2004-02-18 2007-07-10 Astrazeneca Ab composto, composição farmacêutica, uso do composto, e, métodos para tratar distúrbios mediados por mglur 5 e para inibir ativação de receptores de mglur 5
DE102004009039A1 (de) 2004-02-23 2005-09-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und Verwendung als Arzneimittel
WO2005089752A2 (en) 2004-03-15 2005-09-29 Ptc Therapeutics, Inc. Tetra-cyclic carboline derivatives for inhibiting angiogenesis
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
EP1764367A1 (en) 2004-04-12 2007-03-21 Sankyo Company, Limited Thienopyridine derivatives
US7459562B2 (en) 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
GB0413605D0 (en) 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
US8063004B2 (en) 2004-07-22 2011-11-22 Malcera, L.L.C. Chemical composition of matter for the liquefaction and dissolution of asphaltene and paraffin sludges into petroleum crude oils and refined products at ambient temperatures and method of use
EP1621539A1 (en) 2004-07-27 2006-02-01 Aventis Pharma S.A. Heterocycle -substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
CN1993326A (zh) 2004-07-30 2007-07-04 默克公司 代谢型谷氨酸受体的杂环苯乙酮增效剂
WO2006015158A1 (en) 2004-07-30 2006-02-09 Merck & Co., Inc. Indanone potentiators of metabotropic glutamate receptors
EP1778685B1 (de) 2004-08-02 2008-03-26 Schwarz Pharma Ag Carboxamide des indolizins und seiner aza- und diazaderivate
WO2006024970A1 (en) 2004-08-11 2006-03-09 Koninklijke Philips Electronics, N.V. Ultrasonic diagnosis of ischemic cardiodisease
TW200613272A (en) 2004-08-13 2006-05-01 Astrazeneca Ab Isoindolone compounds and their use as metabotropic glutamate receptor potentiators
MX2007001612A (es) 2004-08-18 2007-04-10 Upjohn Co Compuestos novedosos de triazolopiridina para el tratamiento de la inflamacion.
DE102004044884A1 (de) 2004-09-14 2006-05-24 Grünenthal GmbH Substituierte bizyklische Imidazo-3-yl-amin-Verbindungen
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
US20080096935A1 (en) 2004-10-25 2008-04-24 Pinkerton Anthony B Heterocyclic Indanone Potentiators of Metabotropic Glutamate Receptors
US7858646B2 (en) 2004-11-22 2010-12-28 Eli Lilly And Company Potentiators of glutamate receptors
US7434262B2 (en) 2004-12-08 2008-10-07 At&T Intellectual Property I, L.P. Methods and systems that selectively resurrect blocked communications between devices
DE102004061288A1 (de) 2004-12-14 2006-06-29 Schering Ag 3-Amino-Pyrazolo[3,4b]pyridine als Inhibitoren von Proteintyrosinkinasen, deren Herstellung und Verwendung als Arzneimittel
US20090069340A1 (en) 2004-12-27 2009-03-12 Astrazeneca Ab Pyrazolone Compounds As Metabotropic Glutamate Receptor Agonists For The Treatment Of Neurological And Psychiatric Disorders
US7456289B2 (en) 2004-12-31 2008-11-25 National Health Research Institutes Anti-tumor compounds
WO2006091496A2 (en) 2005-02-24 2006-08-31 Merck & Co., Inc. Benzazole potentiators of metabotropic glutamate receptors
KR100968989B1 (ko) 2005-03-23 2010-07-09 에프. 호프만-라 로슈 아게 ｍＧｌｕＲ2 길항제로서 아세틸렌일-피라졸로-피리미딘 유도체
AU2006234627C1 (en) 2005-04-08 2009-11-26 Eisai R & D Management Co., Ltd. Therapeutic agent for dyskinesia
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
US7579360B2 (en) 2005-06-09 2009-08-25 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
WO2006137350A1 (ja) 2005-06-22 2006-12-28 Kissei Pharmaceutical Co., Ltd. 新規なフロピリジン誘導体、それを含有する医薬組成物およびそれらの用途
DE202005011415U1 (de) 2005-07-13 2005-10-06 Arnold & Richter Cine Technik Gmbh & Co Betriebs Kg Vorrichtung zur elektrischen Kontaktierung von Leuchtmitteln in Scheinwerfern
CA2616020A1 (en) 2005-08-05 2007-02-15 Astrazeneca Ab Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators
WO2007021309A1 (en) 2005-08-12 2007-02-22 Astrazeneca Ab Substituted isoindolones and their use as metabotropic glutamate receptor potentiators
WO2007027669A1 (en) 2005-08-29 2007-03-08 Cps Biofuels, Inc. Improved biodiesel fuel, additives, and lubbricants
EP1764099A3 (en) 2005-09-17 2007-05-09 Speedel Experimenta AG Diaminoalcohol derivatives for the treatment of Alzheimer, malaria, HIV
JP2009507900A (ja) 2005-09-17 2009-02-26 シュペーデル・エクスペリメンタ・アーゲー 高血圧の処置のためのレニン阻害剤としての５−アミノ−４−ヒドロキシ−７−（イミダゾ［１，２−ａ］ピリジン−６−イルメチル）−８−メチル−ノナミド誘導体および関連化合物
WO2008051197A2 (en) 2005-09-20 2008-05-02 Mayo Foundation For Medical Education And Research Small-molecule botulinum toxin inhibitors
ES2340321T3 (es) 2005-09-27 2010-06-01 F.Hoffmann-La Roche Ag Oxadiazolilpirazolo-pirimidinas, como antagonistas de mglur2.
GB0521373D0 (en) 2005-10-20 2005-11-30 Kudos Pharm Ltd Pthalazinone derivatives
PT1971601E (pt) 2005-11-15 2010-01-26 Array Biopharma Inc Derivados de n4-fenil-quinazolina-4-amina e compostos relacionados como inibidores de tirosina quinases receptoras do tipo i erbb para o tratamento de doenças hiperproliferativas
AR057218A1 (es) 2005-12-15 2007-11-21 Astra Ab Compuestos de oxazolidinona y su uso como pontenciadores del receptor metabotropico de glutamato
TW200804281A (en) 2006-02-16 2008-01-16 Astrazeneca Ab New metabotropic glutamate receptor-potentiating isoindolones
WO2007103760A2 (en) 2006-03-02 2007-09-13 Smithkline Beecham Corporation Thiazolones for use as pi3 kinase inhibitors
AR059898A1 (es) * 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
GB0606774D0 (en) 2006-04-03 2006-05-10 Novartis Ag Organic compounds
GB0608263D0 (en) 2006-04-26 2006-06-07 Glaxo Group Ltd Compounds
WO2007135529A2 (en) 2006-05-23 2007-11-29 Pfizer Products Inc. Azabenzimidazolyl compounds as mglur2 potentiators
WO2007135527A2 (en) 2006-05-23 2007-11-29 Pfizer Products Inc. Benzimidazolyl compounds
JP5228911B2 (ja) 2006-06-19 2013-07-03 東レ株式会社 多発性硬化症の治療又は予防剤
AU2007272009A1 (en) 2006-07-12 2008-01-17 Syngenta Limited Triazolopyridine derivatives as herbicides
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
WO2008012622A2 (en) 2006-07-25 2008-01-31 Pfizer Products Inc. Azabenzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
WO2008012623A1 (en) 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
CN101511802A (zh) 2006-09-13 2009-08-19 阿斯利康(瑞典)有限公司 螺唑烷酮化合物及其作为代谢型谷氨酸受体增效剂的用途
AU2007307031B2 (en) 2006-10-11 2011-11-24 Amgen Inc. Imidazo- and triazolo-pyridine compounds and methods of use therof
EP2089389A2 (en) 2006-11-01 2009-08-19 Bristol-Myers Squibb Company Heterocyclic compounds as modulators of glucocorticoid receptor, ap-1, and/or nf-kappa-b activity
TW200831085A (en) 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
JP5442449B2 (ja) 2006-12-22 2014-03-12 アステックス、セラピューティックス、リミテッド 新規化合物
CA2672172C (en) 2006-12-22 2016-05-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
WO2008100715A1 (en) 2007-02-09 2008-08-21 Astrazeneca Ab Aza-isoindolones and their use as metabotropic glutamate receptor potentiators - 613
ES2320955B1 (es) 2007-03-02 2010-03-16 Laboratorios Almirall S.A. Nuevos derivados de 3-((1,2,4)triazolo(4,3-a)piridin-7-il)benzamida.
EP2129668A1 (en) 2007-03-07 2009-12-09 Janssen Pharmaceutica N.V. Substituted phenoxy thiazolidinediones as estrogen related receptor-alpha modulators
TW200900391A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-phenyl-piperidin-1-yl)-pyridin-2-one derivatives
EA200970838A1 (ru) 2007-03-07 2010-02-26 Янссен Фармацевтика Н.В. ЗАМЕЩЕННЫЕ ФЕНОКСИПРОИЗВОДНЫЕ N-АЛКИЛИРОВАННЫЕ ТИАЗОЛИДИНДИОНЫ В КАЧЕСТВЕ МОДУЛЯТОРОВ ЭСТРОГЕН-РОДСТВЕННЫХ РЕЦЕПТОРОВ α
EP2134698A1 (en) 2007-03-07 2009-12-23 Janssen Pharmaceutica, N.V. Substituted phenoxy aminothiazolones as estrogen related receptor-alpha modulators
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
GB0704407D0 (en) 2007-03-07 2007-04-18 Glaxo Group Ltd Compounds
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
AU2008226649B2 (en) 2007-03-09 2013-08-01 Sanofi Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof
WO2008124085A2 (en) 2007-04-03 2008-10-16 Exelixis, Inc. Methods of using combinations of mek and jak-2 inhibitors
WO2008130853A1 (en) 2007-04-17 2008-10-30 Astrazeneca Ab Hydrazides and their use as metabotropic glutamate receptor potentiators - 681
WO2008145616A1 (en) 2007-05-25 2008-12-04 Abbott Gmbh & Co. Kg Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (mglu2 receptor)
TWI417100B (zh) 2007-06-07 2013-12-01 Astrazeneca Ab 二唑衍生物及其作為代謝型麩胺酸受體增效劑-８４２之用途
TW200911255A (en) 2007-06-07 2009-03-16 Astrazeneca Ab Metabotropic glutamate receptor oxadiazole ligands and their use as potentiators-841
WO2009004430A1 (en) 2007-06-29 2009-01-08 Pfizer Inc. N-benzyl oxazolidinones and related heterocycleic compounds as potentiators of glutamate receptors
KR20100080597A (ko) 2007-09-14 2010-07-09 오르토-맥닐-얀센 파마슈티칼스 인코포레이티드 １,３-이치환된-４-페닐-1ｈ-피리딘-2-온
KR101520086B1 (ko) 2007-09-14 2015-05-14 얀센 파마슈티칼스 인코포레이티드 １´,３´-이치환된-４-페닐-３,４,５,６-테트라히드로-２ｈ,１´ｈ-[１,４´]비피리디닐-２´-온
NZ584152A (en) 2007-09-14 2011-11-25 Ortho Mcneil Janssen Pharm 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones
WO2009041567A1 (ja) 2007-09-27 2009-04-02 Banyu Pharmaceutical Co., Ltd. メラニン凝集ホルモン受容体拮抗作用を有するジアリールケチミン誘導体
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
JP5433582B2 (ja) 2007-11-14 2014-03-05 ジャンセン ファーマシューティカルズ， インコーポレイテッド． イミダゾ［１，２−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体の正のアロステリック調節因子としてのその使用
CA2711123A1 (en) 2008-01-24 2009-07-30 Merck Sharp & Dohme Corp. 3,5-disubstituted-1,3-oxazolidin-2-one derivatives
JP5309162B2 (ja) 2008-03-06 2013-10-09 サノフイ 置換されたジヒドロ、トリヒドロ及びテトラヒドロシクロアルキルオキサゾロピリミジノン、その製造及び使用
DE102008001056A1 (de) 2008-04-08 2009-10-15 Robert Bosch Gmbh Umlenkeinrichtung für einen Strahl einer elektromagnetischen Welle
CA2723729A1 (en) 2008-05-15 2009-11-19 Merck Sharp & Dohme Corp. Oxazolobenzimidazole derivatives
US20110124661A1 (en) 2008-05-15 2011-05-26 Merck Sharp & Dohme Corp. Oxazolobenzimidazole derivatives
US7790760B2 (en) 2008-06-06 2010-09-07 Astrazeneca Ab Metabotropic glutamate receptor isoxazole ligands and their use as potentiators 286
TW201006801A (en) 2008-07-18 2010-02-16 Lilly Co Eli Imidazole carboxamides
UY32049A (es) 2008-08-14 2010-03-26 Takeda Pharmaceutical Inhibidores de cmet
WO2010022081A1 (en) 2008-08-19 2010-02-25 Array Biopharma Inc. Triazolopyridine compounds as pim kinase inhibitors
TWI496779B (zh) 2008-08-19 2015-08-21 Array Biopharma Inc 作為ｐｉｍ激酶抑制劑之三唑吡啶化合物
CA2735764C (en) 2008-09-02 2016-06-14 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
US8697689B2 (en) 2008-10-16 2014-04-15 Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
US8691813B2 (en) 2008-11-28 2014-04-08 Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
AT507619B1 (de) 2008-12-05 2011-11-15 Oesterreichisches Forschungs Und Pruefzentrum Arsenal Ges M B H Verfahren zur approximation des zeitlichen verlaufs von verkehrsdaten
CA2744946A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
WO2010114726A1 (en) 2009-03-31 2010-10-07 Merck Sharp & Dohme Corp. Aminobenzotriazole derivatives
EP2417135A1 (en) 2009-04-07 2012-02-15 Schering Corporation Substituted triazolopyridines and analogs thereof
EA020671B1 (ru) 2009-05-12 2014-12-30 Янссен Фармасьютикалз, Инк. ПРОИЗВОДНЫЕ 1,2,4-ТРИАЗОЛО[4,3-a]ПИРИДИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПОЛОЖИТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2
BRPI1012870B8 (pt) 2009-05-12 2021-05-25 Addex Pharmaceuticals Sa derivados de 1,2,4-triazolo[4,3-a]piridina e seu uso como moduladores alostericos positivos de receptores de mglur2 e composição farmacêutica
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
WO2010141360A1 (en) 2009-06-05 2010-12-09 Merck Sharp & Dohme Corp. Biaryl benzotriazole derivatives
EP2470527A4 (en) 2009-08-20 2013-02-27 Merck Sharp & Dohme BENZOTRIAZOLE D ETHER DERIVATIVES
CN102002040A (zh) 2009-09-01 2011-04-06 上海药明康德新药开发有限公司 一种三唑并吡啶环化合物的合成方法
AR078172A1 (es) 2009-09-15 2011-10-19 Sanofi Aventis Fenoximetil dihidro oxazolopirimidinonas sustituidas y uso de las mismas como moduladores de receptores metabotropicos de mglur
WO2011034741A1 (en) 2009-09-15 2011-03-24 Merck Sharp & Dohme Corp. Imidazopyridin-2-one derivatives
AR078173A1 (es) 2009-09-15 2011-10-19 Sanofi Aventis Bifeniloximetil dihidro oxazolopirimidinonas sustituidas, su preparacion y su uso
AR078171A1 (es) 2009-09-15 2011-10-19 Sanofi Aventis Dihidrobenzocicloalquiloximetil-oxazolopirimidinonas sustituidas, preparacion y uso de las mismas
JP5204071B2 (ja) 2009-09-25 2013-06-05 パナソニック株式会社 電気かみそり
US8507521B2 (en) 2009-11-02 2013-08-13 Merck Sharp + Dohme B.V. Heterocyclic derivatives
AU2011223898A1 (en) 2010-03-04 2012-09-13 Merck Sharp & Dohme Corp. Positive allosteric modulators of mGluR2
US8748632B2 (en) 2010-03-19 2014-06-10 Sanford-Burnham Medical Research Institute Positive allosteric modulators of group II mGluRs
US8314120B2 (en) 2010-03-30 2012-11-20 Abbott Gmbh & Co. Kg Small molecule potentiators of metabotropic glutamate receptors
US8664214B2 (en) 2010-03-30 2014-03-04 AbbVie Deutschland GmbH & Co. KG Small molecule potentiators of metabotropic glutamate receptors I
WO2011137046A1 (en) 2010-04-29 2011-11-03 Merck Sharp & Dohme Corp. Substituted 1,3-benzothiazol-2(3h)-ones and [1,3]thiazolo[5,4-b]pyridin-2(1h)-ones as positive allosteric modulators of mglur2
CA2795218A1 (en) 2010-04-30 2011-11-03 Helen Blade Polymorphs of a metabotropic glutamate receptor positive allosteric modulator
EP2579717A4 (en) 2010-06-09 2013-12-11 Merck Sharp & Dohme POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
CN101893589B (zh) 2010-06-29 2012-10-17 中国人民解放军第三0二医院 一种无菌检查方法及其使用的全封闭集菌安瓿培养器
EP2603079B1 (en) 2010-08-12 2018-09-19 Merck Sharp & Dohme Corp. Positive allosteric modulators of mglur2
US8785481B2 (en) 2010-09-29 2014-07-22 Merck Sharp & Dohme Corp. Ether benzotriazole derivatives
US9012448B2 (en) * 2010-11-08 2015-04-21 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors
PT2649069E (pt) 2010-11-08 2015-11-20 Janssen Pharmaceuticals Inc Derivados de 1,2,4-triazolo[4,3-a]piridina e sua utilização como moduladores alostéricos positivos de recetores mglur2
AU2011328203B2 (en) 2010-11-08 2015-03-19 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
US20130230459A1 (en) 2010-11-08 2013-09-05 Janssen Pharmaceuticals, Inc. RADIOLABELLED mGluR2 PET LIGANDS
EP2705025A4 (en) 2011-05-03 2015-01-21 Merck Sharp & Dohme Hydroxymethyl-biaryl BENZOTRIAZOL DERIVATIVES
WO2012151136A1 (en) 2011-05-03 2012-11-08 Merck Sharp & Dohme Corp. Aminomethyl biaryl benzotriazole derivatives
WO2012151139A1 (en) 2011-05-03 2012-11-08 Merck Sharp & Dohme Corp. Alkyne benzotriazole derivatives
JP6211797B2 (ja) 2012-05-14 2017-10-11 パナソニック株式会社 除臭剤を備えた除臭装置、および除臭装置を備えた冷蔵庫
US9191739B2 (en) 2013-03-25 2015-11-17 Bose Corporation Active reduction of harmonic noise from multiple rotating devices
JP6211798B2 (ja) 2013-05-17 2017-10-11 富士機械製造株式会社 基板上の異物検査方法および異物検査装置

Also Published As

Publication number Publication date
EA020672B1 (ru) 2014-12-30
BRPI1012870A2 (pt) 2016-04-05
WO2010130424A9 (en) 2011-01-27
JO2907B1 (en) 2015-09-15
DK2430022T3 (da) 2013-12-02
EA201190303A1 (ru) 2012-06-29
JP2012526737A (ja) 2012-11-01
ME01573B (me) 2014-09-20
SG10201402250TA (en) 2014-07-30
CA2760741A1 (en) 2010-11-18
US9737533B2 (en) 2017-08-22
HK1169405A1 (en) 2013-01-25
AR076861A1 (es) 2011-07-13
EP2430022B1 (en) 2013-11-20
KR20120059453A (ko) 2012-06-08
US9226930B2 (en) 2016-01-05
TWI468406B (zh) 2015-01-11
UA108070C2 (uk) 2015-03-25
TW201100416A (en) 2011-01-01
US10071095B2 (en) 2018-09-11
HRP20131122T1 (hr) 2013-12-20
US20170333426A1 (en) 2017-11-23
CN102439008B (zh) 2015-04-29
ZA201107834B (en) 2012-12-27
AU2010246609A1 (en) 2011-11-17
MY161325A (en) 2017-04-14
AU2010246609B2 (en) 2013-09-05
JP5634506B2 (ja) 2014-12-03
RS53075B (en) 2014-04-30
IL215912A (en) 2015-02-26
CA2760741C (en) 2018-05-01
CY1114718T1 (el) 2016-10-05
IL215912A0 (en) 2012-01-31
PT2430022E (pt) 2013-12-26
SG176021A1 (en) 2011-12-29
US20120184525A1 (en) 2012-07-19
SMT201400003B (it) 2014-03-07
BRPI1012870B8 (pt) 2021-05-25
PL2430022T3 (pl) 2014-02-28
US20160067245A1 (en) 2016-03-10
BRPI1012870B1 (pt) 2020-10-13
US20150141403A1 (en) 2015-05-21
US8937060B2 (en) 2015-01-20
ES2440001T3 (es) 2014-01-27
SI2430022T1 (sl) 2014-04-30
KR101753826B1 (ko) 2017-07-04
CN102439008A (zh) 2012-05-02
WO2010130424A1 (en) 2010-11-18
NZ596078A (en) 2013-06-28
MX2011011964A (es) 2012-02-23
EP2430022A1 (en) 2012-03-21

Similar Documents

Publication Publication Date Title
CL2011002838A1 (es) Compuestos derivados de 1,2,4-triazolo[4,3-a]piridina, moduladores alostéricos de receptores mglur2; composición farmacéutica; proceso para prepararla; y su uso en el tratamiento o la prevención de un trastorno del sistema nervioso central seleccionado de ansiedad y esquizofrenia, entre otros.
CL2011002837A1 (es) Compuestos derivados de 1,2,4-triazolo[4,3-a]piridina, moduladores alostericos positivos de receptores mglur2; composicion farmaceutica; proceso para prepararla; y su uso en el tratamiento o la prevencion de un trastorno del sistema nervioso central tal como la ansiedad, esquizofrenia y migraña, entre otros.
CL2011002839A1 (es) Compuestos derivados de 1,2,4-triazolo[4,3-a]piridina, moduladores alostéricos positivos de receptores mglur2; composición farmacéutica y su proceso de preparacion; combinación farmaceutica; y su uso en el tratamiento o prevencion de un trastorno del sistema nervioso central tal como ansiedad y esquizofrenia, entre otros.
CL2008002745A1 (es) Compuestos derivados de 1`, 3`-disustituidos-4-fenil-3,4,5,6-tetrahidro-2h- 1`h[1,4`]bipiridinil-2`-ona, modulares alostericos positivos del receptor glutamatergico mglur2; composicion farmaceutica; y uso de los compuestos en el tratamiento del sistema nervioso central mediado por mglur2.
EA200801934A1 (ru) 1,4-двузамещённые 3-циано-пиридоновые производные и их применение в качестве позитивных модуляторов рецепторов mglur2
EA201000332A1 (ru) 1,3-двузамещенные 4-фенил-1н-пиридин-2-оны
MX2010005110A (es) Derivados de imidazo[1,2-a]piridina y su uso como moduladores alostericos positivos de los receptores de glutamato metabotropico 2.
AR065622A1 (es) Derivados de 3-ciano -4- (4-fenil- piperidin -1- il) piridin -2- ona
MX2011003691A (es) Derivados de indol y benzomorfolina como moduladores de los receptores de glutamato metabotropico.
CR20140085A (es) Inhibidores de pde10 de pirimidina
ECSP088128A (es) Benzimidazoles tricíclicos y su uso como moduladores de receptores metabotrópicos de glutamato
GT200800265A (es) Pirido (3,2-e)piracinas, su uso como inhibidores de fosfadiesterasa 10, y procesos para prepararlas.
EA200901162A1 (ru) Производные 1,4-дизамещённого 3-цианопиридона и их применение в качестве положительных модуляторов рецептора mglur2
EA201000331A1 (ru) 1&#39;,3-двузамещенные 4-(арил-х-фенил)-1h-пиридин-2-оны
AR065654A1 (es) 3-ciano-4-(4-tetrahidropiran-fenil)-piridin-2-ona derivados,composiciones farmaceuticas que los contienen,metodo de preparacion de los mismos,y usos para prevenir o tratar trastornos neurologicos y psiquiatricos.
UA98098C2 (ru) ПРОИЗВОДНЫЕ ПИРИДИНОНА И ИХ ПРИМЕНЕНИЕ КАК ПОЛОЖИТЕЛЬНЫХ АЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2
UY32888A (es) Dihidrobenzocicloalquiloximetil-oxazolopirimidinonas sustituidas, preparación y uso de las mismas
CO6321241A2 (es) Derivados de 1,3,4- tiadiazol espiro condensados para la inhibicion de la actividad de quinesina (ksp)
CL2011003302A1 (es) Compuestos derivados de amida del acido alquil-sulfonico; composicion farmaceutica; uso de los compuestos como moduladores de la disfuncion de glutamato para prevenir o tratar trastornos neurologicos y psiquiatricos como esquizofrenia, enfermedad de alzheimer, trastornos de deficit de atencion/hiperactividad, perdida de audicion, entre otros.
BR112017019685A2 (pt) composto, composição farmacêutica, uso de um composto ou um sal ou um solvato farmaceuticamente aceitável do mesmo, e, método para tratamento de uma doença ou condição
CO6541592A2 (es) Tiazoles biciclicos como moduladores alostericos de receptores de mglur5
ECSP14013268A (es) Inhibidores de pde10 de pirimidina