AR068635A1 - Derivados de 1, 1, 1 - trifluor - 2 - hidroxi - 3 - fenilpropano, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades asociadas con la modulacion del receptor de glucocorticoides. - Google Patents
Derivados de 1, 1, 1 - trifluor - 2 - hidroxi - 3 - fenilpropano, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades asociadas con la modulacion del receptor de glucocorticoides.Info
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- AR068635A1 AR068635A1 ARP080104168A ARP080104168A AR068635A1 AR 068635 A1 AR068635 A1 AR 068635A1 AR P080104168 A ARP080104168 A AR P080104168A AR P080104168 A ARP080104168 A AR P080104168A AR 068635 A1 AR068635 A1 AR 068635A1
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- alkoxy
- alkyl
- halogen
- phenyl
- carbonyl
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Abstract
Los compuestos son utiles como antagonistas de receptor de glucocorticoide para el tratamiento y/o la prevencion de enfermedades tales como la diabetes, la dislipidemia, la obesidad, la hipertension, las enfermedades cardiovasculares, el desequilibrio adrenal o la depresion. Se proveen además, composiciones farmacéuticas que los contienen. Reivindicacion 1: Compuestos de la formula general (1) en la que A es C-R1b o N; R1a, R1b, R1c, R1d y R1e con independencia entre sí se eligen entre el grupo formado por hidrogeno, alquilo C1-7, (cicloalquil C3-7)-alquilo C1-7, halogeno, halogeno-alquilo C1-7, halogeno-alcoxi C1-7, halogeno-(alquil C1-7)-sulfoniloxi, hidroxi, hidroxi-alquilo C1-7, alcoxi C1-7, (alcoxi C1-7)-alcoxi C1-7, hidroxi-alcoxi C1-7, amino-alcoxi C1-7, ciano, carboxilo, carboxil-alquilo C1-7, carboxil-alcoxi C1-7, (alcoxi C1-7)-carbonilo, (alcoxi C1-7)-carbonil-alcoxi C1-7, (alcoxi C1-7)-carbonilamino-alcoxi C1-7, (alquil C1-7)-carboniloxi-alcoxi C1-7, aminocarbonil-alcoxi C1-7, di(alquil C1-7)-amino, di(alquenil C2-7)-amino, (alquil C1-7)-sulfonil-amino, fenilcarbonilamino, fenilsulfoniloxi, heteroaril-alcoxi C1-7, dicho anillo heteroarilo se elige entre el grupo formado por oxadiazolilo, isoxazolilo, tiadiazolilo y tetrazolilo y está sin sustituir o sustituido por alquilo C1-7, feniloxi y fenil-alcoxi C1-7, dicho anillo fenilo está sin sustituir o sustituido una, dos o tres veces por sustituyentes elegidos entre el grupo formado por halogeno, halogeno-alquilo C1-7, alquilo C1-7, hidroxi, ciano, (alquil C1-7)-sulfonilo, alcoxi C1-7 y halogeno-alcoxi C1-7; o R1c y R1d o R1d y R1e juntos son -CH=CH-CH=CH- para formar un anillo fenilo junto con los átomos de carbono a los que están unidos; R2 se elige entre el grupo formado por alquilo C1-7, (cicloalquil C3-7)-alquilo C1-7, carboxil-alquilo C1-7, (alcoxi C1-7)-carbonil-alquilo C1-7, triazolil-alquilo C1-7 y fenilo, dicho fenilo está sin sustituir o sustituido por uno, dos o tres grupos halogeno; R3 es hidrogeno o alquilo C1-7; o R2 y R3 junto con el átomo de carbono al que están unidos forman un anillo cicloalquilo C3-5; R4 es un anillo heteroarilo elegido entre el grupo formado por piridilo, pirazinilo, pirimidinilo, piridazinilo, 2-oxo-1,2-dihidropiridinilo, quinolinilo, isoquinolinilo, cinolinilo, pirazolilo, imidazolilo, tiazolilo, pirazolo[1,5-a]piridilo, imidazo[1,2-a]piridilo, quinoxalinilo, benzotiazolilo, benzotriazolilo, indolilo, indazolilo, 3,4-dihidro-1H-isoquinolinilo y 3,4-dihidro-2H-pirido[3,2-b] [1,4]oxazinilo, dicho anillo heteroarilo está sin sustituir o sustituido por uno, dos o tres sustituyentes elegidos entre el grupo formado por halogeno, halogeno-alquilo C1-7, ciano, alquilo C1-7, (cicloalquil C3-7)-alquilo C1-7, alcoxi C1-7, (alcoxi C1-7)-alcoxi C1-7, ciano-alcoxi C1-7, hidroxi-alcoxi C1-7, halogeno-alcoxi C1-7 carboxilo, carboxil-alquilo C1-7, carboxil-alcoxi C1-7, (alcoxi C1-7)-carbonilo, (alcoxi C1-7)-carbonil-alquilo C1-7, (alcoxi C1-7)-carbonil-alcoxi C1-7, R6R7N-carbonil-alcoxi C1-7, en el que R6 y R7 se eligen con independencia entre hidrogeno o alquilo C1-7 o R6 y R7 junto con el átomo de nitrogeno al que están unidos forman un anillo heterocíclico elegido entre pirrolidina, piperidina, morfolina y tiomorfolina, fenilo, dicho fenilo está sin sustituir o sustituido por uno, dos o tres sustituyentes elegidos entre el grupo formado por halogeno, halogeno-alquilo C1-7, alquilo C1-7, hidroxi, ciano, carboxilo, (alcoxi C1-7)-carbonilo y alcoxi C1-7; piridilo, heterociclilo elegido entre el grupo formado por pirrolidina y piperidina, dicho anillo heterociclilo está sin sustituir o sustituido por carboxilo o (alcoxi C1-7)-carbonilo, fenil-alquilo C1-7, feniloxi y fenil-alcoxi C1-7; R5 es hidrogeno o metilo; n es el numero 0 o 1; y sus sales farmacéuticamente aceptables. Reivindicacion 21: Un proceso de obtencion de los compuestos de la formula (1) segun cualquiera de las reivindicaciones de 1 a 20, dicho proceso consiste en: tratar un compuesto de formula (2) en la que A, n, de R1a a R1e, R2, R3 y R4 tienen los significados definidos anteriormente, con trifluorometiltrimetilsilano y un fluoruro adecuado para obtener un compuesto de la formula (3), en la que R5 es hidrogeno, y, si se desea, alquilar el compuesto de la formula (3) con un yoduro de metilo en presencia de una base, por ejemplo NaH, obteniéndose un compuesto de la formula (4), en al que R5 es metilo, y, si se desea, convertir el compuesto obtenido en una sal farmacéuticamente aceptable.
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EP07117360 | 2007-09-27 |
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AR068635A1 true AR068635A1 (es) | 2009-11-25 |
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ARP080104168A AR068635A1 (es) | 2007-09-27 | 2008-09-25 | Derivados de 1, 1, 1 - trifluor - 2 - hidroxi - 3 - fenilpropano, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades asociadas con la modulacion del receptor de glucocorticoides. |
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US (2) | US8143280B2 (es) |
EP (1) | EP2205562B1 (es) |
JP (1) | JP5242691B2 (es) |
KR (1) | KR101174982B1 (es) |
CN (1) | CN101808992B (es) |
AR (1) | AR068635A1 (es) |
AT (1) | ATE502012T1 (es) |
AU (1) | AU2008303600B8 (es) |
BR (1) | BRPI0817242A8 (es) |
CA (1) | CA2700277A1 (es) |
CL (1) | CL2008002863A1 (es) |
DE (1) | DE602008005634D1 (es) |
DK (1) | DK2205562T3 (es) |
ES (1) | ES2360272T3 (es) |
IL (1) | IL204052A (es) |
MX (1) | MX2010002893A (es) |
PE (1) | PE20090741A1 (es) |
PL (1) | PL2205562T3 (es) |
PT (1) | PT2205562E (es) |
RU (1) | RU2481333C2 (es) |
TW (1) | TWI426904B (es) |
WO (1) | WO2009040288A1 (es) |
ZA (1) | ZA201001797B (es) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2010049073A1 (en) * | 2008-10-30 | 2010-05-06 | Bayer Schering Pharma Aktiengesellschaft | 1,1,1-trifluoro-3-amino-3-heteroaryl-2-propanoles, a process for their production and their use as anti-inflammatory agents |
US8138189B2 (en) * | 2009-03-26 | 2012-03-20 | Hoffman-La Roche Inc. | Substituted benzene compounds as modulators of the glucocorticoid receptor |
JP5408415B2 (ja) * | 2009-06-10 | 2014-02-05 | Jsr株式会社 | 1位置換3,5−ジアミノベンゼンの製造方法 |
BR112012013195A2 (pt) * | 2009-12-04 | 2016-08-09 | Nissan Chemical Ind Ltd | compostos de 2-piridona. |
WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
CA2816088A1 (en) * | 2010-10-28 | 2012-05-03 | Viamet Pharmaceuticals, Inc. | Metalloenzyme inhibitor compounds |
EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2015024848A1 (en) * | 2013-08-23 | 2015-02-26 | Basf Se | Compounds with terminal heteroarylcyanovinylene groups and their use in organic solar cells |
JP6048533B2 (ja) * | 2014-05-12 | 2016-12-21 | 日産化学工業株式会社 | 2−ピリドン化合物を含有する医薬 |
IL274654B2 (en) * | 2017-11-16 | 2023-11-01 | Syngenta Participations Ag | A process for the preparation of amines and amides of cyclobutane rich in enantiomers and diastereomers |
US10450022B2 (en) | 2018-01-31 | 2019-10-22 | David Watson | Device for adjusting a seat position of a bicycle seat |
KR20210153056A (ko) * | 2019-03-18 | 2021-12-16 | 리네트 케이. 니만 | 인슐린 감수성 개선 방법 |
Family Cites Families (12)
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TW263495B (es) * | 1992-12-23 | 1995-11-21 | Celltech Ltd | |
CZ289317B6 (cs) * | 1994-04-11 | 2002-01-16 | Sankyo Company Limited | Heterocyklická sloučenina, farmaceutický prostředek ji obsahující a její pouľití |
SI1169312T1 (en) | 1999-03-29 | 2005-02-28 | F. Hoffmann-La Roche Ag | Glucokinase activators |
MXPA04009329A (es) * | 2002-03-26 | 2005-01-25 | Boehringer Ingelheim Pharma | Mimeticos de glucocorticoides, metodos para su preparacion, composiciones farmaceuticas y usos de los mismos. |
DE10330358A1 (de) * | 2003-07-01 | 2005-02-03 | Schering Ag | Heterozyklisch substituierte Pentanol-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
DE10346939A1 (de) | 2003-10-06 | 2005-05-19 | Schering Ag | Heterocyclisch substituierte Pentanole, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
US20050090559A1 (en) * | 2003-07-01 | 2005-04-28 | Markus Berger | Heterocyclically-substituted pentanol derivatives, process for their production and their use as anti-inflammatory agents |
UY28526A1 (es) | 2003-09-24 | 2005-04-29 | Boehringer Ingelheim Pharma | Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos |
MX2007014811A (es) | 2005-06-10 | 2008-02-14 | Boehringer Ingelheim Int | Mimeticos de glucocorticoides, metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos. |
CN101321726A (zh) | 2005-09-30 | 2008-12-10 | 大日本住友制药株式会社 | 新型稠合吡咯衍生物 |
EP1783114A1 (en) * | 2005-11-03 | 2007-05-09 | Novartis AG | N-(hetero)aryl indole derivatives as pesticides |
EA015542B1 (ru) * | 2006-01-24 | 2011-08-30 | Янссен Фармацевтика Н.В. | Новые 2-замещённые бензимидазолы в качестве селективных модуляторов рецептора андрогена (sarms) |
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- 2008-09-18 CA CA2700277A patent/CA2700277A1/en not_active Abandoned
- 2008-09-18 ES ES08804354T patent/ES2360272T3/es active Active
- 2008-09-18 AT AT08804354T patent/ATE502012T1/de active
- 2008-09-18 DE DE602008005634T patent/DE602008005634D1/de active Active
- 2008-09-18 DK DK08804354.2T patent/DK2205562T3/da active
- 2008-09-18 PL PL08804354T patent/PL2205562T3/pl unknown
- 2008-09-18 MX MX2010002893A patent/MX2010002893A/es active IP Right Grant
- 2008-09-18 CN CN2008801090597A patent/CN101808992B/zh not_active Expired - Fee Related
- 2008-09-18 PT PT08804354T patent/PT2205562E/pt unknown
- 2008-09-18 AU AU2008303600A patent/AU2008303600B8/en not_active Ceased
- 2008-09-18 WO PCT/EP2008/062412 patent/WO2009040288A1/en active Application Filing
- 2008-09-18 EP EP08804354A patent/EP2205562B1/en not_active Not-in-force
- 2008-09-18 KR KR1020107006692A patent/KR101174982B1/ko not_active IP Right Cessation
- 2008-09-18 RU RU2010116352/04A patent/RU2481333C2/ru not_active IP Right Cessation
- 2008-09-25 PE PE2008001670A patent/PE20090741A1/es not_active Application Discontinuation
- 2008-09-25 AR ARP080104168A patent/AR068635A1/es unknown
- 2008-09-26 TW TW097137403A patent/TWI426904B/zh not_active IP Right Cessation
- 2008-09-26 CL CL2008002863A patent/CL2008002863A1/es unknown
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2010
- 2010-02-18 IL IL204052A patent/IL204052A/en not_active IP Right Cessation
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