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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

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    • 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
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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)

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EP05101704 2005-03-04

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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)
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Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL146801A0 (en) * 1999-06-11 2002-07-25 Pro Duct Health Inc Gel composition for filling a breast milk duct prior to surgical excision of the duct or other breast tissue
US20100190980A1 (en) * 2007-06-21 2010-07-29 Taisho Pharmaceutical Co., Ltd Pyrazinamide compound
GB0713686D0 (en) * 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
WO2009074575A2 (en) 2007-12-10 2009-06-18 Novartis Ag Organic compounds
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
EP2477631A4 (en) * 2009-09-17 2013-05-08 Univ Vanderbilt SUBSTITUTED PHENYLAMINE CARBOXAMIDE ANALOGUES AS NEGATIVE ALLOSTERIC MGLUR5 MODULATORS AND METHOD FOR THEIR PREPARATION AND USE
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
EP2680849A4 (en) * 2011-03-03 2015-02-18 Univ Vanderbilt 6-ALKYL-N- (PYRIDIN-2-YL) -4-ARYLOXYPICOLINAMIDE ANALOGUE AS MGLUR5 NEGATIVE ALLOSTERIC MODULATORS AND METHOD FOR THEIR PREPARATION AND USE
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
CR20160428A (es) 2014-02-14 2017-04-04 Takeda Pharmaceuticals Co Pizazinas moduladoras 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
JP6779204B2 (ja) * 2014-11-18 2020-11-04 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ａ２ａ拮抗薬特性を有するアミノピラジン化合物
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
EP4110766A1 (en) * 2020-02-27 2023-01-04 Syngenta Crop Protection AG Pesticidally active diazine-bisamide compounds

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
CA2555402A1 (en) 2004-02-12 2005-09-01 Celine Bonnefous Bipyridyl amides as modulators of metabotropic glutamate receptor-5
CA2599974C (en) 2005-03-04 2013-12-31 F. Hoffmann-La Roche Ag Pyridine-2-carboxamide derivatives as mglur5 antagonists

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