AR053153A1 - Derivados de pirazina -2- carboxamida como antagonistas de mglur5 - Google Patents

Derivados de pirazina -2- carboxamida como antagonistas de mglur5

Info

Publication number
AR053153A1
AR053153A1 ARP060100779A ARP060100779A AR053153A1 AR 053153 A1 AR053153 A1 AR 053153A1 AR P060100779 A ARP060100779 A AR P060100779A AR P060100779 A ARP060100779 A AR P060100779A AR 053153 A1 AR053153 A1 AR 053153A1
Authority
AR
Argentina
Prior art keywords
alkyl
chf2
cycloalkyl
alkenyl
optionally substituted
Prior art date
Application number
ARP060100779A
Other languages
English (en)
Inventor
Georg Jaeschke
Sabine Kolczewski
Richard Hugh Philip Porter
Eric Vieira
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR053153A1 publication Critical patent/AR053153A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Usos y medicamentos utiles como antagonistas del recetor metabotropico del glutamato. Reivindicacion 1: Compuestos de formula general (1) en donde R1 es un anillo de 5 o 6- miembros respectivamente de formula (2) o (3); r2 es H, alquilo c1-7, cicloalquilo C3-6 o -(CH2)m-Ra; R3 es H, arilo o heteroarilo que está opcionalmente sustituido por: CN, Cl, F, Br, CF3, CHF2, o -O-C1-7 alquilo, -(CO)-Rb, -(CH2)m-Rc, -NH-(CO)-C1-7 alquilo; -O-CH2F, -O-CHF2, -O-CF3, -S(O)2-Rd o heteroarilo que está opcionalmente sustituido por alquilo C1-7;R4 es H, -O, Cl, F, Br, CN, -CHF2, CF3, C1-7 alquilo, -O-(CO)-C1-7 alquilo o -(CH2)m-Re; R5 es alquilo C1-7-alquilo o alquil C1-7-alquil-C3-6 cicloalquilo; -(CH2)n-O-Rf, C3-8 alquenil-O-Rf, -(CH2)n-NRgRh, - C2-6 alquenil-NRgRh o -(CH2)n-Re; Ra es -O-C1-7 alquilo o -OH; Rb es C1-7 alquilo, NH2, o -O-C1-7 alquilo; Rc es -OH, NH2, o NH-(CO)-O-C1-7 alquilo; Rd es C1-7 alquilo, -NH2, -NH-C1-7 alquilo o -N-di(C1-7 alquilo); Re es -OH, -CH2F, -CHF2, -CF3 o -O- (CO)-C1-7 alquilo; Rf es C1-7 alquilo, C3-8 alquenilo, C3-6 cicloalquilo, fenil, bencilo o -(CO)-R'; Rg, Rh son independientemente H, C1-7 alquilo, C3-6 cicloalquilo, C3-8 alquenilo, fenilo, bencilo, o-(CO)-R' o Rg y Rh también pueden formar, junto con el átomo de N al que están unidos, un anillo heterocíclico o de heteroarilo de 5 a 7 miembros opcionalmente sustituido con 1 o 2 OH; R' es NH2, -NH-C1-7 alquilo, C1-7 alquilo, o C1-7 alcoxilo; m es 1 a 4; n es 2 a 6; así como las sales farmacéuticamente aceptables de los mismos.
ARP060100779A 2005-03-04 2006-03-02 Derivados de pirazina -2- carboxamida como antagonistas de mglur5 AR053153A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05101704 2005-03-04

Publications (1)

Publication Number Publication Date
AR053153A1 true AR053153A1 (es) 2007-04-25

Family

ID=36518434

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060100779A AR053153A1 (es) 2005-03-04 2006-03-02 Derivados de pirazina -2- carboxamida como antagonistas de mglur5

Country Status (16)

Country Link
US (2) US20060199828A1 (es)
EP (1) EP1858862B1 (es)
JP (1) JP4774410B2 (es)
KR (1) KR100929941B1 (es)
CN (1) CN101208311B (es)
AR (1) AR053153A1 (es)
AU (1) AU2006222252B2 (es)
BR (1) BRPI0609256A2 (es)
CA (1) CA2600169C (es)
IL (1) IL185327A0 (es)
MX (1) MX2007010563A (es)
NO (1) NO20074287L (es)
RU (1) RU2407739C2 (es)
TW (1) TWI310378B (es)
WO (1) WO2006094691A1 (es)
ZA (1) ZA200707139B (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU769853B2 (en) * 1999-06-11 2004-02-05 Atossa Genetics, Inc. Gel composition for filing a breast milk duct prior to surgical excision of the duct or other breast tissue
EP2157090A4 (en) * 2007-06-21 2011-09-07 Taisho Pharmaceutical Co Ltd PYRAZINAMIDVERBINDUNG
GB0713686D0 (en) * 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
CL2008003651A1 (es) 2007-12-10 2009-06-19 Novartis Ag Compuestos derivados de 3,5-diamino-6-cloropirazinamida sustituida; composicion farmaceutica; combinacion farmaceutica; y uso en el tratamiento de una condición inflamatoria o alergica, en particular una enfermedad inflamatoria u obstructiva de las vias respiratorias.
WO2009078432A1 (ja) * 2007-12-18 2009-06-25 Taisho Pharmaceutical Co., Ltd. １-アルキル-４-アミノ-１ｈ-ピラゾール-３-カルボキサミド化合物
US8501757B2 (en) 2009-09-17 2013-08-06 Vanderbilt University Substituted phenylamine carboxamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same
US8470820B2 (en) 2010-01-22 2013-06-25 Hoffman-La Roche Inc. Nitrogen-containing heteroaryl derivatives
US8703768B2 (en) 2010-06-09 2014-04-22 Hoffmann-La Roche Inc. Nitrogen containing heteroaryl compounds
AU2012223720A1 (en) 2011-03-03 2013-09-26 Vanderbilt University 6-alkyl-n-(pyridin-2-yl)-4-aryloxypicolinamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same
US9403808B2 (en) * 2011-10-28 2016-08-02 Hoffmann-La Roche Inc. Pyrazine derivatives
AU2014353150A1 (en) 2013-11-19 2016-07-07 Vanderbilt University Substituted imidazopyridine and triazolopyridine compounds as negative allosteric modulators of mGluR5
MA39337B1 (fr) * 2014-02-14 2019-11-29 Takeda Pharmaceuticals Co Modulateurs de pyrazines de gpr6
US9533982B2 (en) 2014-03-20 2017-01-03 Vanderbilt University Substituted bicyclic heteroaryl carboxamide analogs as mGluR5 negative allosteric modulators
US9550778B2 (en) 2014-10-03 2017-01-24 Vanderbilt University Substituted 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analogs as negative allosteric modulators of mGluR5
US10472347B2 (en) * 2014-11-18 2019-11-12 Merck Sharp & Dohme Corp. Aminopyrazine compounds with A2A antagonist properties
WO2016144792A1 (en) * 2015-03-06 2016-09-15 Alpharmagen, Llc Alpha 7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
CN106317027A (zh) * 2015-06-15 2017-01-11 山东轩竹医药科技有限公司 杂芳基酰胺类衍生物及其作为tgr5激动剂的应用
BR112022017093A2 (pt) * 2020-02-27 2023-02-14 Syngenta Crop Protection Ag Compostos de diazina-bisamida ativos em termos pesticidas

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0321115B1 (en) 1987-12-14 1991-08-14 Sawai Pharmaceutical Co., Ltd. Carboxamide derivatives having tetrazole and thiazole rings and their use
AU2005215379A1 (en) 2004-02-12 2005-09-01 Merck & Co., Inc. Bipyridyl amides as modulators of metabotropic glutamate receptor-5
BRPI0607583A2 (pt) 2005-03-04 2009-09-15 Hoffmann La Roche derivados de piridin-2-carboxamida como antagonistas mglur5, método para sua preparação, medicamento contendo os mesmos, bem como uso relacionado aos referidos compostos

Also Published As

Publication number Publication date
NO20074287L (no) 2007-12-03
AU2006222252B2 (en) 2012-02-16
CN101208311B (zh) 2013-06-12
EP1858862B1 (en) 2016-04-20
US7947685B2 (en) 2011-05-24
CA2600169C (en) 2013-11-05
US20090233944A1 (en) 2009-09-17
ZA200707139B (en) 2008-10-29
EP1858862A1 (en) 2007-11-28
WO2006094691A1 (en) 2006-09-14
AU2006222252A1 (en) 2006-09-14
BRPI0609256A2 (pt) 2010-03-09
JP4774410B2 (ja) 2011-09-14
TW200700396A (en) 2007-01-01
IL185327A0 (en) 2008-02-09
KR100929941B1 (ko) 2009-12-04
RU2407739C2 (ru) 2010-12-27
CA2600169A1 (en) 2006-09-14
CN101208311A (zh) 2008-06-25
RU2007132656A (ru) 2009-04-10
MX2007010563A (es) 2007-10-04
US20060199828A1 (en) 2006-09-07
KR20070107101A (ko) 2007-11-06
TWI310378B (en) 2009-06-01
JP2008531630A (ja) 2008-08-14

Similar Documents

Publication Publication Date Title
AR053153A1 (es) Derivados de pirazina -2- carboxamida como antagonistas de mglur5
AR054232A1 (es) Derivados de piridina -2- carboxamida como antagonistas de mglur5
AR059512A1 (es) Derivados de piridina -2- carboxamida
AR052558A1 (es) Derivados de tiazol-4-carboxamida como antagonistas de mglur5
AR051995A1 (es) Derivados de tieno-piridina como intensificadores alostericos de gaba -b
CO5680434A2 (es) 2,4-pirimidinadiaminas utiles en el tratamiento de enfermedades neoplasticas, desordenes del sistema inmune e inflamatorios
AR077935A1 (es) Derivados de 3-amino-5 fenil-5,6-dihidro-2h-(1,4)oxazina
CO6190626A2 (es) Compuestos y composiciones como inhibidores de proteasa activadora de canal
AR083849A1 (es) Antagonistas de mdm2 de espiro-oxindol
CO6321166A2 (es) Compuestos de pirrol
AR054024A1 (es) Derivados de piridina -3- carboxamida como agonistas inversos de cb1
UY30897A1 (es) Derivados de pentafluorotiobenzamidoacetonitrilo, composiciones conteniéndolos y aplicaciones
AR062677A1 (es) Derivados de biaril-sulfonamida, procesos de produccion y composiciones farmaceuticas que los comprenden
AR079327A1 (es) Derivados de 2-amino-5,5-difluor -5,6-dihidro-4h-(1,3) oxazin-4-il) fenil)-amida
PE20070528A1 (es) Compuestos heterociclicos como ligandos del receptor vaniloide del subtipo 1
AR085960A1 (es) 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2
AR069849A1 (es) Derivados de heteroarilo como antagonistas de receptor de orexina
AR071385A1 (es) Compuestos de 2-imino-3-metil pirrolopirimidinona sustituida con tiofenilo,composiciones farmaceuticas que los contienen,y uso de los mismos para el tratamiento de patologias asociadas con la proteina beta amiloide,tales como alzheimer y otros formas de demencia.
AR058701A1 (es) Derivados de piracinil-s-espiro-oxacinoquinolin-pirimidin-triona como agentes antibacterianos
PE20071152A1 (es) Compuestos derivados de azabiciclo[3.1.0]hex como moduladores de receptores de dopamina d3
AR052568A1 (es) Derivados de pirazolo -pirimidina como antagonstas de mglur2
AR064547A1 (es) Derivados de azaspiro como antagonistas del receptor v1a
AR069796A1 (es) Derivados de bencimidazol, sustituido por carboxilo o por hidroxilo, proceso para prepararlos y composiciones farmaceuticas que los contienen
AR060604A1 (es) Nuevos arilamino n- heteroarilos como inhibidores de mek
AR067058A1 (es) Oxazolidinonas sustituidas y su uso para preparar medicamentos

Legal Events

Date Code Title Description
FA Abandonment or withdrawal