CL2011002839A1 - 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. - Google Patents

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.

Info

Publication number
CL2011002839A1
CL2011002839A1 CL2011002839A CL2011002839A CL2011002839A1 CL 2011002839 A1 CL2011002839 A1 CL 2011002839A1 CL 2011002839 A CL2011002839 A CL 2011002839A CL 2011002839 A CL2011002839 A CL 2011002839A CL 2011002839 A1 CL2011002839 A1 CL 2011002839A1
Authority
CL
Chile
Prior art keywords
prevention
treatment
triazolo
pyridine
compounds
Prior art date
Application number
CL2011002839A
Other languages
English (en)
Inventor
Gregor James Macdonald
José Maria Cid-Núnez
Lucas Olivares Ana Isabel De
Andrés Avelino Trabanco-Suarez
Original Assignee
Janssen Pharmaceuticasl Inc
Addex Pharmaceuticals Sa
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 Janssen Pharmaceuticasl Inc, Addex Pharmaceuticals Sa filed Critical Janssen Pharmaceuticasl Inc
Publication of CL2011002839A1 publication Critical patent/CL2011002839A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • A61P25/10Antiepileptics; Anticonvulsants for petit-mal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • A61P25/12Antiepileptics; Anticonvulsants for grand-mal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Addiction (AREA)
  • Nutrition Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Anesthesiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)

Abstract

LA PRESENTE INVENCIÓN SE REFIERE A COMPUESTOS DERIVADOS DE TRIAZOLO[4,3-A]PIRIDINA DE FÓRMULA (1) DONDE TODOS LOS RADICALES SON SEGÚN LO DEFINIDO EN LAS REIVINDICACIONES. LOS COMPUESTOS DE ACUERDO CON LA INVENCIÓN SON MODULADORES ALOSTÉRICOS POSITIVOS DEL SUBTIPO 2 RECEPTOR DE GLUTAMATO METABOTRÓPICO ("MGLUR2"). LOS CUALES SON ÚTILES PARA EL TRATAMIENTO O PREVENCIÓN DE TRASTORNOS NEUROLÓGICOS Y PSIQUIÁTRICOS CON LA DISFUNCIÓN DE GLUTAMATO Y ENFERMEDADES EN LAS CUALES EL SUBTIPO MGLUR2 DE RECEPTORES<br /> METABOTRÓPICOS ESTA INVOLUCRADO. LA INVENCIÓN SE REFIERE ADEMÁS A COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN ESE TIPO DE COMPUESTOS. A PROCESOS PARA PREPARAR DICHOS COMPUESTOS Y COMPOSICIONES. Y AL USO DE ESE TIPO DE COMPUESTOS PARA LA PREVENCIÓN O TRATAMIENTO DE TRASTORNOS NEUROLÓGICOS Y PSIQUIÁTRICOS Y ENFERMEDADES EN LAS CUALES MGLUR2 ESTA INVOLUCRADO.
CL2011002839A 2009-05-12 2011-11-11 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. CL2011002839A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09160064 2009-05-12

Publications (1)

Publication Number Publication Date
CL2011002839A1 true CL2011002839A1 (es) 2012-04-09

Family

ID=40901945

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2011002839A CL2011002839A1 (es) 2009-05-12 2011-11-11 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.

Country Status (20)

Country Link
US (2) US8716480B2 (es)
EP (1) EP2430021B1 (es)
JP (1) JP5707391B2 (es)
KR (1) KR20120039532A (es)
CN (1) CN102439009B (es)
AR (1) AR076860A1 (es)
AU (1) AU2010246608B2 (es)
CA (1) CA2760084C (es)
CL (1) CL2011002839A1 (es)
EA (1) EA020556B1 (es)
ES (1) ES2428401T3 (es)
HK (1) HK1166784A1 (es)
IL (1) IL215911A (es)
MX (1) MX2011011963A (es)
MY (1) MY153913A (es)
NZ (1) NZ595945A (es)
SG (1) SG175931A1 (es)
TW (1) TW201100415A (es)
WO (1) WO2010130423A1 (es)
ZA (1) ZA201107833B (es)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
TWI417095B (zh) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc 1,4-二取代之3-氰基-吡啶酮衍生物及其作為mGluR2-受體之正向異位性調節劑之用途
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
JP5366269B2 (ja) 2007-09-14 2013-12-11 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. 1,3−二置換4−(アリル−x−フェニル)−1h−ピリジン−2−オン
US9114138B2 (en) 2007-09-14 2015-08-25 Janssen Pharmaceuticals, Inc. 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′] bipyridinyl-2′-ones
CN101801930B (zh) 2007-09-14 2013-01-30 奥梅-杨森制药有限公司 1,3-二取代的-4-苯基-1h-吡啶-2-酮
US8785486B2 (en) 2007-11-14 2014-07-22 Janssen Pharmaceuticals, Inc. Imidazo[1,2-A]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
WO2010025890A1 (en) 2008-09-02 2010-03-11 Ortho-Mcneil-Janssen Pharmaceuticals, Inc 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
WO2010043396A1 (en) 2008-10-16 2010-04-22 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
WO2010060589A1 (en) 2008-11-28 2010-06-03 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
SG10201402250TA (en) 2009-05-12 2014-07-30 Janssen Pharmaceuticals Inc 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
MX2011011962A (es) 2009-05-12 2012-02-28 Janssen Pharmaceuticals Inc Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostericos positivos de receptores de glutamato metabotropico (mglur2).
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
CA2815120A1 (en) 2010-11-08 2012-05-18 Jose Ignacio Andres-Gil Radiolabelled mglur2 pet ligands
WO2012062750A1 (en) 2010-11-08 2012-05-18 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
ES2552879T3 (es) 2010-11-08 2015-12-02 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
EP2643320B1 (en) 2010-11-08 2015-03-04 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
US8765767B2 (en) * 2012-03-16 2014-07-01 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
WO2015042243A1 (en) * 2013-09-19 2015-03-26 Bristol-Myers Squibb Company Triazolopyridine ether derivatives and their use in neurological and pyschiatric disorders
EA201891617A3 (ru) 2014-01-21 2019-04-30 Янссен Фармацевтика Нв Комбинации, содержащие положительные аллостерические модуляторы или ортостерические агонисты метаботропного глутаматергического рецептора 2 подтипа, и их применение
HUE053734T2 (hu) 2014-01-21 2021-07-28 Janssen Pharmaceutica Nv 2-es altípusú metabotróp glutamáterg receptor pozitív allosztérikus modulátorait tartalmazó kombinációk és alkalmazásuk
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
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
CN104876884B (zh) * 2014-11-24 2018-02-02 上海化工研究院有限公司 一种稳定同位素标记灭蝇胺及其衍生物的合成方法
CA2967153A1 (en) 2014-12-03 2016-06-09 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo[1,5-.alpha.]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors
RU2695651C2 (ru) * 2014-12-11 2019-07-25 Янссен Фармацевтика Нв 1,2,4-ТРИАЗОЛО[4,3-a]ПИРИДИНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПОЛОЖИТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ MGLUR2
CN108290856A (zh) 2015-08-11 2018-07-17 尼奥迈德研究所 芳基-取代的二氢喹诺酮、它们的制备和它们作为药物的用途
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
CA2994478C (en) 2015-08-12 2023-10-03 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
JP6929285B2 (ja) 2015-12-18 2021-09-01 ヤンセン ファーマシューティカ エヌ.ベー. 放射性標識mGluR2/3PETリガンド
EP3389727B1 (en) 2015-12-18 2020-08-12 Janssen Pharmaceutica NV Radiolabelled mglur2/3 pet ligands
WO2017127930A1 (en) * 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
CN107383002B (zh) * 2016-05-17 2021-07-13 中国科学院上海药物研究所 一类含氟三氮唑并吡啶类化合物及其制备方法、药物组合物和用途
CN111116582B (zh) * 2019-12-18 2022-07-29 大连大学 一种mGluR2拮抗剂

Family Cites Families (441)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE790440A (es) 1971-10-23 1973-04-24 Bayer Ag
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
JPS5382783U (es) 1976-12-13 1978-07-08
JPS5752334Y2 (es) 1977-03-16 1982-11-13
ZA782648B (en) 1977-05-23 1979-06-27 Ici Australia Ltd The prevention,control or eradication of infestations of 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
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
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
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
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
EP0478195B1 (en) 1990-09-21 1999-05-26 Rohm And Haas Company Dihydropyridazinones and pyridazinones as fungicides
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
AU668694B2 (en) 1991-12-19 1996-05-16 Sanofi-Synthelabo Saccharin derivative proteolytic enzyme inhibitors
US5378720A (en) 1991-12-19 1995-01-03 Sterling Winthrop Inc. 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
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
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
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
WO1994029273A1 (en) 1993-06-09 1994-12-22 Smithkline Beecham Corporation Bicyclic fibrinogen antagonists
DE4326758A1 (de) * 1993-08-10 1995-02-16 Basf Ag [1,3,4]Triazolo[1,5-a]pyridine
SK282402B6 (sk) 1993-08-19 2002-01-07 Janssen Pharmaceutica N. V. Deriváty dihydrobenzopyránu, spôsob a medziprodukty na ich výrobu, ich použitie a farmaceutický prostriedok na ich báze
CN1066718C (zh) 1993-08-19 2001-06-06 詹森药业有限公司 取代的芳氧基烷基二胺及其制备方法和用途
AU7467294A (en) 1993-08-20 1995-03-21 Banyu Pharmaceutical Co., Ltd. Tyrosine kinase inhibitor
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
US5679683A (en) 1994-01-25 1997-10-21 Warner-Lambert Company Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
CN1057522C (zh) 1994-03-10 2000-10-18 藤泽药品工业株式会社 作为前列腺素i2激动剂的萘衍生物
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
JPH10504569A (ja) 1994-08-24 1998-05-06 イーライ・リリー・アンド・カンパニー 向代謝性グルタメート受容体拮抗剤としてのピロリジニルジカルボン酸誘導体
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
US5869428A (en) 1995-03-13 1999-02-09 Ishihara Sangyo Kaisha Ltd. Pyridonesulfonylurea compounds, process for their production and herbicides containing them
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
KR100400639B1 (ko) 1995-04-27 2003-12-31 미쯔비시 웰 파마 가부시키가이샤 복소환식아미드화합물및그의의약용도
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
ATE187172T1 (de) 1995-09-15 1999-12-15 Sanofi Synthelabo Chinolin-2-on derivate als serotonin antagonisten
US6130217A (en) 1995-09-20 2000-10-10 Pfizer Inc Compounds enhancing antitumor activity of other cytotoxic agents
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
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
ATE321757T1 (de) 1995-12-08 2006-04-15 Janssen Pharmaceutica Nv (imidazol-5-yl)methyl-2-chinolinonderivate als farnesyl protein transferase inhibitoren
GB9602166D0 (en) 1996-02-02 1996-04-03 Zeneca Ltd Aminoheterocyclic derivatives
US6313127B1 (en) 1996-02-02 2001-11-06 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
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
US5741798A (en) 1996-06-03 1998-04-21 Boehringer Ingelheim Pharmaceuticals, Inc. 2-benzyl-4-sulfonyl-4H-isoquinolin-1,3-diones and their use as antiinflammatory agents
WO1998006724A1 (fr) 1996-08-09 1998-02-19 Yamanouchi Pharmaceutical Co., Ltd. Agonistes du recepteur du glutamate metabotropique
DE19632423A1 (de) 1996-08-12 1998-02-19 Merck Patent Gmbh Thienopyrimidine
ATE230399T1 (de) 1996-08-14 2003-01-15 Astrazeneca Ab Substituierte pyrimidinderivate und ihre pharmazeutische anwendung
EP0927171B1 (en) 1996-09-16 2002-02-20 Du Pont Pharmaceuticals Company Pyrazinones and triazinones and their derivatives thereof
DE19638484A1 (de) 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
DE19638486A1 (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
WO1998024780A2 (en) 1996-12-05 1998-06-11 Amgen Inc. Substituted pyrimidinone and pyridinone compounds and their use
JP4352115B2 (ja) 1997-01-24 2009-10-28 クラヴィス・ファルマ・アーエスアー ゲムシタビン誘導体
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
US6204292B1 (en) 1997-07-18 2001-03-20 Georgetown University Bicyclic metabotropic glutamate receptor ligands
ES2172840T3 (es) 1997-07-18 2002-10-01 Hoffmann La Roche Derivados de 5h-tiazolo(3,2-a)pirimidina.
WO1999006041A1 (en) 1997-07-31 1999-02-11 Celgene Corporation SUBSTITUTED ALKANOHYDROXAMIC ACIDS AND METHOD OF REDUCING TNFα LEVELS
DE69822638T2 (de) 1997-08-14 2005-02-24 F. Hoffmann-La Roche Ag Heterocyclische vinylether zur behandlung neurologischer krankheiten
US6358975B1 (en) 1997-08-15 2002-03-19 Johns Hopkins University Method of using selective parp inhibitors to prevent or treat neurotoxicity
US20020028813A1 (en) 1997-09-03 2002-03-07 Paul F. Jackson Thioalkyl compounds, methods, and compositions for inhibiting parp activity
US6121278A (en) 1997-09-03 2000-09-19 Guilford Pharmaceuticals, Inc. Di-n-heterocyclic compounds, methods, and compositions for inhibiting parp activity
US6635642B1 (en) 1997-09-03 2003-10-21 Guilford Pharmaceuticals Inc. PARP inhibitors, pharmaceutical compositions comprising same, and methods of using same
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
WO1999011622A1 (en) 1997-09-03 1999-03-11 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
ES2200248T3 (es) 1997-09-19 2004-03-01 Ssp Co., Ltd. Derivados de acudi fenilpropionico sustituido en alfa y medicamento que los contienen.
US6465484B1 (en) 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
CA2303830A1 (en) 1997-09-26 1999-04-08 Merck & Co., Inc. Novel 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
NZ504465A (en) 1997-10-14 2001-11-30 Welfide Corp 1-Phenylacylamino substituted piperazine derivatives which are 4-substituted by a heteroaryl group
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
ATE388139T1 (de) 1997-12-18 2008-03-15 Boehringer Ingelheim Pharma Pyridone als hemmer der sh2-domäne der src- familie
US6013672A (en) 1997-12-18 2000-01-11 Uab Research Foundation Agonists of metabotropic glutamate receptors and uses thereof
CN1284945A (zh) 1997-12-19 2001-02-21 安姆根有限公司 取代的吡啶和哒嗪化合物及其药物用途
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
AU734812B2 (en) 1998-01-28 2001-06-21 Taisho Pharmaceutical Co., Ltd. Fluorine-containing amino acid derivatives
IL137922A0 (en) 1998-02-17 2001-10-31 Tularik Inc Anti-viral pyrimidine derivatives
TR200002671T2 (tr) 1998-03-17 2000-12-21 Pfizer Products Inc. Bisiklo(2.2.1)Heptanlar ve ilgili bileşikler
AU738222B2 (en) 1998-04-08 2001-09-13 Novartis Ag N-pyridonyl herbicides
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
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And 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
CA2341865C (en) 1998-08-31 2006-01-17 Taisho Pharmaceutical Co., Ltd. 6-fluorobicyclo[3.1.0]hexane derivatives
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
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
ID28959A (id) 1998-12-04 2001-07-19 Bristol Myers Squibb Co Turunan-turunan 3-tersubstitusi-4-arilkinolin-2-on sebagai modulator saluran kalium
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
CN1361768A (zh) 1999-06-02 2002-07-31 Nps药物有限公司 代谢移变的谷氨酸盐受体拮抗剂和它们治疗中枢神经系统疾病的用途
BR9916746A (pt) 1999-06-03 2005-01-11 Abbott Lab Compostos anti-inflamatórios que inibem adesão de célula
EP1189873A1 (en) 1999-06-03 2002-03-27 Lilly, S.A. Excitatory amino acid receptor modulators
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
JP2003506440A (ja) 1999-08-05 2003-02-18 プレサイエント ニューロファーマ インコーポレイテッド 中枢神経系に関連する疾患の処置のための1,4−ジアゼピン誘導体
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
US6355653B1 (en) * 1999-09-06 2002-03-12 Hoffmann-La Roche Inc. Amino-triazolopyridine derivatives
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
DE60009116T2 (de) 1999-10-15 2005-02-17 F. Hoffmann-La Roche Ag Benzodiazepinderivate und deren verwendung als metabotrope glutamatrezeptor antagonisten
PT1224174E (pt) 1999-10-15 2004-01-30 Hoffmann La Roche Derivados de benzodiazepina como antagonistas do receptor metabotropico do glutamato
EP1226136B1 (en) 1999-10-19 2004-12-29 Merck &amp; Co., Inc. 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
AU779442B2 (en) 2000-01-20 2005-01-27 Eisai Co. Ltd. Novel piperidine compounds and drugs containing the same
GB0002100D0 (en) 2000-01-28 2000-03-22 Novartis Ag Organic compounds
EP1255735A2 (en) 2000-02-03 2002-11-13 Eli Lilly And Company Pyridine derivatives as potentiators of glutamate receptors
BR0108611A (pt) 2000-02-25 2003-05-06 Hoffmann La Roche Moduladores de receptor de adenosina
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
WO2001072712A1 (en) 2000-03-24 2001-10-04 Cor Therapeutics, Inc. ISOQUINOLONE INHIBITORS OF FACTOR Xa
GB0007193D0 (en) 2000-03-25 2000-05-17 Univ Manchester Treatment of movrmrnt disorders
KR100830859B1 (ko) 2000-04-27 2008-05-21 아스텔라스세이야쿠 가부시키가이샤 이미다조피리딘 유도체 및 이를 함유하는 의약 조성물
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
US6897237B2 (en) 2000-04-28 2005-05-24 Shionogi & Co. Ltd. MMP-12 inhibitors
CN1209336C (zh) 2000-04-28 2005-07-06 日本农药株式会社 生产2-卤代苯甲酸的方法
WO2001085716A1 (en) 2000-05-11 2001-11-15 Kyowa Hakko Kogyo Co., Ltd 2-piperidone compounds for the treatment of cancer
NZ522674A (en) 2000-05-11 2004-10-29 Kenneth Curry Novel spiro[2.4]heptane amino carboxy compounds and derivatives thereof
US20020009713A1 (en) 2000-05-11 2002-01-24 Miller Freda D. Methods for identifying modulators of neuronal growth
US7081481B2 (en) 2000-05-31 2006-07-25 Eli Lilly And Company Excitatory amino acid receptor modulators
BRPI0111596B8 (pt) 2000-06-12 2022-07-26 Eisai Co Ltd Composto piridona, processo de produção do composto, composição farmacêutica, e uso do dito composto
JP2002003401A (ja) 2000-06-27 2002-01-09 Japan Science & Technology Corp 脳由来神経栄養因子誘導剤
JP2002012533A (ja) 2000-06-27 2002-01-15 Kao Corp 染毛剤組成物
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
US6770676B2 (en) 2000-06-28 2004-08-03 Taisho Pharmaceutical Co., Ltd. Dicarboxylic acid derivatives
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
JP4251868B2 (ja) 2000-08-11 2009-04-08 エーザイ・アール・アンド・ディー・マネジメント株式会社 2−アミノピリジン化合物および医薬用途
SG174632A1 (en) 2000-09-11 2011-10-28 Novartis Vaccines & Diagnostic Quinolinone derivatives
US6599940B2 (en) 2000-09-13 2003-07-29 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
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
WO2002070662A2 (en) 2001-03-02 2002-09-12 Gpc Biotech Ag Three hybrid assay system
WO2002074025A2 (de) 2001-03-08 2002-09-19 Ilfa Industrieelektronik Und Leiterplattenfertigung Aller Art Gmbh Mehrschichtige leiterplatte
US6596731B2 (en) 2001-03-27 2003-07-22 Hoffmann-La Roche Inc. Substituted imidazo[1,2-A] pyridine derivatives
WO2002079498A1 (en) 2001-04-02 2002-10-10 Merck & Co., Inc. In vivo methods of determining activity of receptor-type kinase inhibitors
CA2442557C (en) 2001-04-12 2008-12-23 F. Hoffmann-La Roche Ag Dihydro-benzo¬b|¬1,4|diazepin-2-one derivatives as mglur2 antagonists ii
DK1379522T3 (da) 2001-04-12 2005-05-30 Hoffmann La Roche Dihydro-benzo(b)(1,4)diazeping-2-on-derivater som MGLUR2-antagonister I
SE0101579D0 (sv) 2001-05-04 2001-05-04 Astrazeneca Ab New compounds
CN1527710A (zh) 2001-05-14 2004-09-08 ����˹�ж�-����˹˹����ҩƷ��˾ 作为促肾上腺皮质激素释放因子配体的取代的吡嗪酮、吡啶和嘧啶
WO2002094264A1 (en) 2001-05-23 2002-11-28 Tularik Inc. Ccr4 antagonists
CA2448317A1 (en) 2001-05-30 2002-12-05 Alteon Inc. Method for treating glaucoma v
CA2448306A1 (en) 2001-05-30 2002-12-05 Alteon Inc. Method for treating fibrotic diseases or other indications
US6720321B2 (en) 2001-06-05 2004-04-13 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-disubstituted benzo-fused cycloalkyl urea compounds
JPWO2002102807A1 (ja) 2001-06-14 2004-09-30 萬有製薬株式会社 新規イソキサゾロピリドン誘導体及びその用途
CA2450934A1 (en) 2001-06-19 2002-12-27 Marco Dodier Pyrimidine inhibitors of phosphodiesterase (pde) 7
JP2003012653A (ja) 2001-06-28 2003-01-15 Yamanouchi Pharmaceut Co Ltd キナゾリン誘導体
WO2003011293A2 (en) 2001-08-02 2003-02-13 Neurocrine Biosciences, Inc. Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists
US7427623B2 (en) 2001-09-11 2008-09-23 Smithkline Beecham Corporation 4-Amino-2,3-disubstituted thieno[2,3-d]pyrimidines and pharmacetical compositions thereof
ES2309206T3 (es) 2001-10-02 2008-12-16 Smithkline Beecham Corporation Compuestos quimicos.
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
US7067517B2 (en) 2001-12-14 2006-06-27 Nero Nordisk A/S Use of compounds for decreasing activity of hormone-sensitive lipase
JP5082033B2 (ja) 2001-12-21 2012-11-28 エグゼリクシス パテント カンパニー エルエルシー Lxrのモジュレーター
KR20090031962A (ko) 2001-12-27 2009-03-30 다이쇼 세이야꾸 가부시끼가이샤 6-플루오로비시클로[3.1.0]헥산 유도체
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
EP1513522A2 (en) 2002-01-18 2005-03-16 Sri International Methods of treating conditions associated with an edg receptor
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
EP1482916A4 (en) 2002-02-07 2007-12-12 Univ Miami THERAPY BASED ON SCHWANN CELLS AND PHOSPHODIESTERASE INHIBITORS
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
ES2334990T3 (es) 2002-02-14 2010-03-18 Pharmacia Corporation Piridinonas sustituidas como moduladores de p38 map quinasa.
WO2003070712A1 (en) 2002-02-19 2003-08-28 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
WO2003076405A1 (en) 2002-03-14 2003-09-18 Bayer Healthcare Ag Monocyclic aroylpyridinones as antiinflammatory agents
CA2479744A1 (en) 2002-03-28 2003-10-09 Paul E. Finke Substituted 2,3-diphenyl pyridines
NZ535438A (en) 2002-03-29 2006-08-31 Janssen Pharmaceutica Nv Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands
AU2003218063A1 (en) 2002-04-03 2003-10-20 Eli Lilly And Company Therapy for psychoses combining an atypical antipsychotic and an mglu2/3 receptor agonist
EP1503757B1 (en) 2002-05-02 2007-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
US6864261B2 (en) 2002-05-02 2005-03-08 Euro-Celtique S.A. Therapeutic agents useful for treating pain
JP4606161B2 (ja) 2002-05-21 2011-01-05 アムジエン・インコーポレーテツド 置換複素環式化合物および使用方法
BR0311558A (pt) 2002-06-11 2007-04-27 Lilly Co Eli composto ou sal farmaceuticamente aceitável do mesmo, processo para preparar o mesmo, métodos para afetar os receptores de glutamato metabotrópicos ligados a camp, para administrar uma quantidade eficaz de um composto e para tratar um distúrbio neurológico e psiquiátrico em um paciente, e, formulação farmacêutica
MXPA04012628A (es) 2002-06-13 2005-03-23 Patricia Olivershaffer DERIVADOS Y COMPUESTOS RELACIONADOS DEL áCIDO 2-UREIDO-6-HETEROARIL-3H-BENZOIMIDAZOL-4-CARBOXILICO COMO INHIBIDORES DE GIRASA Y/O TOPOISOMERASA IV PARA EL TRATAMIENTO DE INFECCIONES BACTERIALES.
GB0214268D0 (en) 2002-06-20 2002-07-31 Celltech R&D Ltd Chemical compounds
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
US20060063782A1 (en) 2002-07-03 2006-03-23 Murray Christopher W 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
AU2003255845A1 (en) 2002-08-22 2004-03-11 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
EP1556038A2 (en) 2002-08-26 2005-07-27 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
CN102793698A (zh) 2002-09-10 2012-11-28 诺瓦提斯公司 治疗包括成瘾与抑郁症在内的与mGLU受体相关疾病的mGLU受体拮抗剂
CA2497356A1 (en) 2002-09-11 2004-03-25 Merck & Co., Inc. Nucleic acid sequences encoding novel point mutations on mglur2 and mglur3
EP1543006A1 (en) 2002-09-19 2005-06-22 Boehringer Ingelheim (Canada) Ltd. Non-nucleoside reverse transcriptase inhibitors
CA2495721C (en) 2002-09-19 2009-08-18 Boehringer Ingelheim (Canada) Ltd. Non-nucleoside reverse transcriptase inhibitors
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
ATE423216T1 (de) 2002-10-23 2009-03-15 Daiichi Pure Chemicals Co Ltd Neue fructosylpeptidoxidase und deren nutzung
US20040138204A1 (en) 2002-10-30 2004-07-15 Harrington James Frederick Compositions and methods for pain reduction
US7902203B2 (en) 2002-11-01 2011-03-08 Abbott Laboratories, Inc. Anti-infective agents
MXPA05004670A (es) 2002-11-01 2005-08-18 Abbott Lab Agentes anti-infecciones.
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
AU2003289386A1 (en) 2002-12-18 2004-07-09 Takeda Pharmaceutical Company Limited Jnk inhibitors
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
KR20110010824A (ko) 2003-01-14 2011-02-07 아레나 파마슈티칼스, 인크. 대사 조절제로서의 1,2,3-삼치환된 아릴 및 헤테로아릴 유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된 장애의 예방 및 치료
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.
WO2004069826A1 (en) 2003-02-04 2004-08-19 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
PL378295A1 (pl) 2003-02-24 2006-03-20 Arena Pharmaceuticals, Inc. Podstawione pochodne arylowe i heteroarylowe jako modulatory metabolizmu glukozy oraz profilaktyka i leczenie zaburzeń tego metabolizmu
EP1601358B1 (en) 2003-03-03 2007-12-19 F. Hoffmann-La Roche Ag 2,5-substituted tetrahydroisoquinolines for use as 5-ht6 modulators
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
WO2004092135A2 (en) 2003-04-15 2004-10-28 Astrazeneca Substituted benzosulphonamide as potentiators of glutamate receptors
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
CN102584813B (zh) 2003-05-14 2016-07-06 Ngc药物公司 化合物及其在调节淀粉样蛋白β中的用途
WO2005040337A2 (en) 2003-05-20 2005-05-06 The Regents Of The University Of California METHODS FOR BINDING AGENTS TO β-AMYLOID PLAQUES
GB0315950D0 (en) 2003-06-11 2003-08-13 Xention Discovery Ltd Compounds
WO2005002585A1 (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
EP1646372A2 (en) 2003-07-14 2006-04-19 Decode Genetics EHF. Methods of diagnosis and treatment for asthma based on haplotype association
NZ546044A (en) 2003-08-29 2009-09-25 Vernalis Cambridge Ltd Pyrimidothiophene compounds
GB0320300D0 (en) 2003-08-29 2003-10-01 Cancer Rec Tech Ltd Pyrimidothiophene compounds
GB0322016D0 (en) 2003-09-19 2003-10-22 Merck Sharp & Dohme New compounds
SG150539A1 (en) 2004-02-18 2009-03-30 Astrazeneca Ab Tetrazole compounds and their use as metabotropic glutamate receptor antagonists
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
EP1726585A4 (en) * 2004-03-05 2009-07-15 Banyu Pharma Co Ltd HETEROCYCLIC DERIVATIVE WITH FIVE ELEMENTS SUBSTITUTED BY A DIARYLE
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
AU2005233437A1 (en) 2004-04-12 2005-10-27 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
WO2006014918A2 (en) 2004-07-30 2006-02-09 Merck & Co., Inc. Heterocyclic acetophenone potentiators of metabotropic glutamate receptors
EP1773792A1 (en) 2004-07-30 2007-04-18 Merck & Co., Inc. Indanone potentiators of metabotropic glutamate receptors
KR20070045254A (ko) 2004-08-02 2007-05-02 슈바르츠 파르마 악티엔게젤샤프트 인돌리진 카르복사미드 및 그 아자 및 디아자유도체
CN100560030C (zh) 2004-08-11 2009-11-18 皇家飞利浦电子股份有限公司 缺血性心脏病的超声诊断
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
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
AU2005299797A1 (en) 2004-10-25 2006-05-04 Merck & Co., Inc. Heterocyclic indanone potentiators of metabotropic glutamate receptors
WO2006057870A1 (en) 2004-11-22 2006-06-01 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
BRPI0517423A (pt) 2004-12-27 2008-10-07 Astrazeneca Ab composto, composição farmacêutica, método para o tratamento ou prevenção de distúrbios neurológicos e psiquiátricos associados com disfunção do glutamato em um animal, e, uso em um composto
US7456289B2 (en) 2004-12-31 2008-11-25 National Health Research Institutes Anti-tumor compounds
US7960417B2 (en) 2005-02-24 2011-06-14 Merck Sharp & Dohme Corp. Benzazole potentiators of metabotropic glutamate receptors
PL1863818T3 (pl) 2005-03-23 2010-08-31 Hoffmann La Roche Pochodne acetylenylo-pirazolo-pirymidyny jako antagoniści MGLUR2
EP1875912A4 (en) 2005-04-08 2008-06-04 Eisai R&D Man Co Ltd MEANS OF TREATING UNWILLING MOVEMENTS
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
US20070032469A1 (en) 2005-08-05 2007-02-08 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
EP1948654B1 (en) 2005-09-17 2009-06-24 Novartis Ag 5-amino-4-hydroxy-7- (imidazo [1,2-a] pyridin-6- ylmethyl)-8-methyl-nonamide derivatives and related compounds as renin inhibitors for the treatment of hypertension
US8492428B2 (en) 2005-09-20 2013-07-23 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.
CN102887891B (zh) 2005-11-15 2016-03-09 阿雷生物药品公司 N4-苯基-喹唑啉-4-胺衍生物和相关化合物
AR057218A1 (es) 2005-12-15 2007-11-21 Astra Ab Compuestos de oxazolidinona y su uso como pontenciadores del receptor metabotropico de glutamato
CN101384586A (zh) * 2006-02-14 2009-03-11 诺华公司 Pi-3激酶抑制剂及其应用方法
TW200804281A (en) 2006-02-16 2008-01-16 Astrazeneca Ab New metabotropic glutamate receptor-potentiating isoindolones
EP1993539A4 (en) 2006-03-02 2010-05-19 Glaxosmithkline Llc THIAZOLONE AS A PI3 KINASE INHIBITOR
TWI417095B (zh) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc 1,4-二取代之3-氰基-吡啶酮衍生物及其作為mGluR2-受體之正向異位性調節劑之用途
RU2008143179A (ru) * 2006-03-31 2010-05-10 Новартис АГ (CH) Органические соединения
GB0606774D0 (en) 2006-04-03 2006-05-10 Novartis Ag Organic compounds
GB0608263D0 (en) 2006-04-26 2006-06-07 Glaxo Group Ltd Compounds
WO2007135527A2 (en) 2006-05-23 2007-11-29 Pfizer Products Inc. Benzimidazolyl compounds
WO2007135529A2 (en) 2006-05-23 2007-11-29 Pfizer Products Inc. Azabenzimidazolyl compounds as mglur2 potentiators
CN101472900B (zh) 2006-06-19 2011-07-27 东丽株式会社 多发性硬化症的治疗或预防药
US20100035756A1 (en) 2006-07-12 2010-02-11 Syngenta Limited Triazolophyridine 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
WO2008032191A2 (en) 2006-09-13 2008-03-20 Astrazeneca Ab Spiro-oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators
CA2665195C (en) * 2006-10-11 2011-08-09 Amgen Inc. Imidazo- and triazolo-pyridine compounds and methods of use thereof
US7994190B2 (en) 2006-11-01 2011-08-09 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
TW200831085A (en) 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
CN101679409B (zh) 2006-12-22 2014-11-26 Astex治疗学有限公司 双环杂环衍生化合物、其医药组合物和其用途
CA2672172C (en) 2006-12-22 2016-05-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
JP2010518104A (ja) 2007-02-09 2010-05-27 アストラゼネカ・アクチエボラーグ アザ−イソインドロンおよび代謝型グルタミン酸レセプター増強剤−613としてのそれらの使用
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.
CA2679944A1 (en) 2007-03-07 2008-09-12 Janssen Pharmaceutica N.V. Substituted phenoxy thiazolidinediones 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
UA98484C2 (ru) 2007-03-07 2012-05-25 Янссен Фармацевтика Н.В. ЗАМЕЩЕННЫЕ ФЕНОКСИАМИНОТИАЗОЛОНЫ КАК МОДУЛЯТОРЫ α-РЕЦЕПТОРА ЭСТРОГЕНА
EP2132188B1 (en) 2007-03-07 2011-12-14 Janssen Pharmaceutica N.V. Substituted phenoxy n-alkylated thiazoledinedione as estrogen related receptor-alpha modulators
AR065622A1 (es) 2007-03-07 2009-06-17 Ortho Mcneil Janssen Pharm Derivados de 3-ciano -4- (4-fenil- piperidin -1- il) piridin -2- ona
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
JP5351056B2 (ja) 2007-03-09 2013-11-27 サノフイ 置換されたジヒドロ及びテトラヒドロオキサゾロピリミジノン、その製造並びに使用
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
JP5615700B2 (ja) 2007-05-25 2014-10-29 アボット ゲーエムベーハー ウント カンパニー カーゲー 代謝型グルタミン酸受容体2(mglu2受容体)の陽性調節剤としての複素環化合物
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
US9114138B2 (en) 2007-09-14 2015-08-25 Janssen Pharmaceuticals, Inc. 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′] bipyridinyl-2′-ones
JP5366269B2 (ja) 2007-09-14 2013-12-11 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. 1,3−二置換4−(アリル−x−フェニル)−1h−ピリジン−2−オン
CN101801930B (zh) 2007-09-14 2013-01-30 奥梅-杨森制药有限公司 1,3-二取代的-4-苯基-1h-吡啶-2-酮
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
US8785486B2 (en) 2007-11-14 2014-07-22 Janssen Pharmaceuticals, Inc. Imidazo[1,2-A]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
AU2009206658A1 (en) 2008-01-24 2009-07-30 Merck Sharp & Dohme Corp. 3,5-substituted-1,3-oxazolidin-2-one derivatives
WO2009110901A1 (en) 2008-03-06 2009-09-11 Sanofi-Aventis Substituted dihydro, trihydro and tetrahydro cycloalkyloxazolopyrimidinones, preparation and use thereof as allosteric modulators of mglur
DE102008001056A1 (de) 2008-04-08 2009-10-15 Robert Bosch Gmbh Umlenkeinrichtung für einen Strahl einer elektromagnetischen Welle
JP2011520892A (ja) 2008-05-15 2011-07-21 メルク・シャープ・エンド・ドーム・コーポレイション オキサゾロベンゾイミダゾール誘導体
CA2723727A1 (en) 2008-05-15 2009-11-19 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
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
WO2010022081A1 (en) 2008-08-19 2010-02-25 Array Biopharma Inc. Triazolopyridine compounds as pim kinase inhibitors
WO2010025890A1 (en) 2008-09-02 2010-03-11 Ortho-Mcneil-Janssen Pharmaceuticals, Inc 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
WO2010043396A1 (en) 2008-10-16 2010-04-22 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
WO2010060589A1 (en) 2008-11-28 2010-06-03 Ortho-Mcneil-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
EP2393807B1 (en) 2009-02-04 2013-08-14 Boehringer Ingelheim International GmbH Cyclic inhibitors of 11 -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
MX2011011962A (es) 2009-05-12 2012-02-28 Janssen Pharmaceuticals Inc Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostericos positivos de receptores de glutamato metabotropico (mglur2).
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
SG10201402250TA (en) 2009-05-12 2014-07-30 Janssen Pharmaceuticals Inc 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
WO2010141360A1 (en) 2009-06-05 2010-12-09 Merck Sharp & Dohme Corp. Biaryl benzotriazole derivatives
US8975286B2 (en) 2009-08-20 2015-03-10 Merck Sharp & Dohme Corp. Ether benzotriazole 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
AR078173A1 (es) 2009-09-15 2011-10-19 Sanofi Aventis Bifeniloximetil dihidro oxazolopirimidinonas sustituidas, su preparacion y su uso
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
AR078171A1 (es) 2009-09-15 2011-10-19 Sanofi Aventis Dihidrobenzocicloalquiloximetil-oxazolopirimidinonas sustituidas, preparacion y uso de las mismas
WO2011034741A1 (en) 2009-09-15 2011-03-24 Merck Sharp & Dohme Corp. Imidazopyridin-2-one derivatives
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
WO2011109277A1 (en) 2010-03-04 2011-09-09 Merck Sharp & Dohme Corp. Positive allosteric modulators of mglur2
WO2011116356A2 (en) 2010-03-19 2011-09-22 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
US20130035332A1 (en) 2010-04-29 2013-02-07 Layton Mark E Substituted 1,3-Benzothiazol-2(3H)-Ones and [1,3]Thiazolo[5,4-B]Pyridin-2(IH)-Ones as Positive Allosteric Modulators of MGLUR2
MX2012012447A (es) 2010-04-30 2012-11-21 Astrazeneca Ab Polimorfos de modulador alosterico positivo de receptores metabotropicos de glutamato.
WO2011156245A2 (en) 2010-06-09 2011-12-15 Merck Sharp & Dohme Corp. 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
EP2643320B1 (en) 2010-11-08 2015-03-04 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
CA2815120A1 (en) 2010-11-08 2012-05-18 Jose Ignacio Andres-Gil Radiolabelled mglur2 pet ligands
ES2552879T3 (es) 2010-11-08 2015-12-02 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
WO2012062750A1 (en) 2010-11-08 2012-05-18 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
US20140088151A1 (en) 2011-05-03 2014-03-27 Douglas C. Beshore Alhydroxymethyl biaryl benzotriazole derivatives
US8772276B2 (en) 2011-05-03 2014-07-08 Merck Sharp & Dohme Corp. Alkyne benzotriazole derivatives
EP2704573A4 (en) 2011-05-03 2014-10-15 Merck Sharp & Dohme AMINOMETHYL biaryl BENZOTRIAZOL DERIVATIVES

Also Published As

Publication number Publication date
EA020556B1 (ru) 2014-12-30
US9085577B2 (en) 2015-07-21
IL215911A0 (en) 2012-01-31
NZ595945A (en) 2013-03-28
MY153913A (en) 2015-04-15
CN102439009A (zh) 2012-05-02
EP2430021A1 (en) 2012-03-21
ES2428401T3 (es) 2013-11-07
SG175931A1 (en) 2011-12-29
AU2010246608A1 (en) 2011-11-17
CN102439009B (zh) 2014-11-12
CA2760084C (en) 2017-09-05
EA201190302A1 (ru) 2012-06-29
IL215911A (en) 2015-02-26
TW201100415A (en) 2011-01-01
JP5707391B2 (ja) 2015-04-30
US8716480B2 (en) 2014-05-06
WO2010130423A1 (en) 2010-11-18
US20140200208A1 (en) 2014-07-17
JP2012526736A (ja) 2012-11-01
EP2430021B1 (en) 2013-08-28
AR076860A1 (es) 2011-07-13
MX2011011963A (es) 2012-03-14
AU2010246608B2 (en) 2012-10-11
ZA201107833B (en) 2013-02-27
KR20120039532A (ko) 2012-04-25
CA2760084A1 (en) 2010-11-18
US20120184528A1 (en) 2012-07-19
HK1166784A1 (en) 2012-11-09

Similar Documents

Publication Publication Date Title
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.
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.
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.
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.
CR20140085A (es) Inhibidores de pde10 de pirimidina
MX2010005110A (es) Derivados de imidazo[1,2-a]piridina y su uso como moduladores alostericos positivos de los receptores de glutamato metabotropico 2.
PH12015502685A1 (en) 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
CO2018005163A2 (es) Compuesto de [1,2,4]triazolo[1,5-a]pirimidin-7-ilo
ECSP066856A (es) Compuestos novedosos como moduladores del receptor opioide
CL2009000975A1 (es) Compuestos derivados de quinuclidina, ligandos del receptor de acetilcolina a7; su composicion farmaceutica; su uso para el tratamiento de trastornos del sistema nervioso central, en especial afectivos y neurodegenerativos, enfermedades tales como esquizofrenia y alzheimer.
AR068510A1 (es) Derivados de 4-fenil-1h-piridin-2-ona - 1,3 disustituidos, composiciones farmaceuticas que los contienen y usos de los mismos para tratar o prevenir trastornos del sistema nervioso central.
BR112017001726A2 (pt) compostos de 6,7-di-hidropirazolo [1,5-a]pirazin-4(5h)-ona e seus usos como moduladores alostéricos negativos de receptores mglur2
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
NI202000074A (es) Moduladores alostéricos de espiropiperidina de receptores nicotínicos de acetilcolina
CL2008003927A1 (es) Compuestos derivados de imidazo[1,2-a]piridina-2-heterociclil-metanona, moduladores de los receptores nucleares nurr1; compuestos intermediarios; composicion farmaceutica; medicamento; y uso para el tratamiento y prevencion de enfermedades neurodegenerativas, psiquiatricas, inflamatorias, osteoporosis, cancer, entre otras.
PA8790101A1 (es) Derivados de aminoalquilazol como antagonistas de histamina-3
PA8781601A1 (es) &#34; derivados de azaciclilbenzamida como antagonistas de histamina-3
WO2014150114A8 (en) Substituted pyridizinone derivatives as pde10 inhibitors
AR125085A1 (es) Profármacos de compuestos de pde10
ECSP14013268A (es) Inhibidores de pde10 de pirimidina