AR072969A1 - Derivados de ciclohexilamida, composiciones farmaceuticas y usos como antagonistas del receptor del factor de liberacion de corticotropina (crf - 1) - Google Patents
Derivados de ciclohexilamida, composiciones farmaceuticas y usos como antagonistas del receptor del factor de liberacion de corticotropina (crf - 1)Info
- Publication number
- AR072969A1 AR072969A1 ARP090102998A ARP090102998A AR072969A1 AR 072969 A1 AR072969 A1 AR 072969A1 AR P090102998 A ARP090102998 A AR P090102998A AR P090102998 A ARP090102998 A AR P090102998A AR 072969 A1 AR072969 A1 AR 072969A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- alkyl
- alkoxy
- phenyl
- halo
- Prior art date
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Abstract
Reivindicacion 1: Un compuesto de la formula 1: en donde R1 es -(CH2)n(SO2)mRx; Rx es fenilo, bifenilo, naftilo o heteroarilo, cada uno de los cuales puede estar opcionalmente sustituido por uno o más sustituyentes seleccionados a partir del grupo que consiste en alquilo de 1 a 10 átomos de carbono, alcoxilo de 1 a 10 átomos de carbono, hidroxi-alquilo de 1 a 10 átomos de carbono, halogeno, halo-alquilo de 1 a 10 átomos de carbono, halo-alcoxilo de 1 a 10 átomos de carbono, nitrilo, -CO2R25, -(CH2)pNR29R30, -SO2NR31R32, alcoxilo (de 1 a 6 átomos de carbono)-alquilo (de 1 a 6 átomos de carbono)-, un heterociclo de 5 o 6 miembros, un heteroarilo de 5 o 6 miembros, fenilo, fenil-alquilo (de 1 a 6 átomos de carbono)- ariloxilo, estando cada uno del heterociclo de 5 o 6 miembros, heteroarilo de 5 o 6 miembros, fenilo, y ariloxilo, opcionalmente sustituido por uno o más sustituyentes seleccionados a partir del grupo que consiste en carboxilo, alquilo de 1 a 6 átomos de carbono, halogeno e hidroxilo; R2 es hidrogeno o alquilo de 1 a 6 átomos de carbono, o R1 y R2, junto con el átomo de nitrogeno con el que están unidos, forman un heteroarilo de 5 o 6 miembros que contiene 2, 3 o 4 heteroátomos, estando el heteroarilo opcionalmente sustituido por uno o más sustituyentes seleccionados a partir del grupo que consiste en alquilo de 1 a 10 átomos de carbono, alcoxilo de 1 a 10 átomos de carbono, halogeno, halo-alquilo de 1 a 10 átomos de carbono, halo-alcoxilo de 1 a 10 átomos de carbono, fenilo, o un heterociclo de 5 o 6 miembros, estando el heterociclo opcionalmente sustituido por carboxilo; R3, R4, R5, R6, R7, R9, R10, R17, R22, R25, R29, R30, R31 y R32, los cuales pueden ser iguales o diferentes, son cada uno hidrogeno o alquilo de 1 a 6 átomos de carbono; R30 es hidrogeno, alquilo de 1 a 6 átomos de carbono, o R33CO-; R33 es alquilo de 1 a 6 átomos de carbono; R8 es fenilo, o un heteroarilo, cada uno de los cuales puede estar opcionalmente sustituido por uno o más sustituyentes seleccionados a partir del grupo que consiste en alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, halogeno, alcoxilo de 1 a 6 átomos de carbono, nitrilo o dialquil-amino de 1 a 6 átomos de carbono, o dos sustituyentes adyacentes pueden formar juntos un anillo carbocíclico o heterocíclico saturado o insaturado; m es un entero de 0 o 1; n es un entero de 0, 1 o 2; p es un entero de 0 a 6; e isomeros del mismo; en forma libre o en forma de sal.
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JP5748777B2 (ja) * | 2010-02-02 | 2015-07-15 | ノバルティス アーゲー | Crf受容体アンタゴニストとしてのシクロヘキシルアミド誘導体 |
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US8546416B2 (en) | 2011-05-27 | 2013-10-01 | Novartis Ag | 3-spirocyclic piperidine derivatives as ghrelin receptor agonists |
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 |
AU2013255458A1 (en) | 2012-05-03 | 2014-10-09 | Novartis Ag | L-malate salt of 2, 7 - diaza - spiro [4.5 ] dec- 7 - yle derivatives and crystalline forms thereof as ghrelin receptor agonists |
US9814723B2 (en) * | 2013-02-23 | 2017-11-14 | Lixin Zhang | Compositions and methods for prophylaxis and therapy for Meniere's disease |
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