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COMPUESTOS DE 2-AMINO-4-ARILTIAZOL COMO ANTAGONISTAS DE TRPA1
专利权人:
GLENMARK PHAMACEUTICALS S.A.
发明人:
KUMAR, SUKEERTHI,THOMAS, ABRAHAM,CHAUDHARI, SACHIN SUNDARLAL,KANSAGRA, BIPIN PARSOTTAM,YEMIREDDY, VENKATA RAMANA,KHAIRATKAR-JOSHI, NEELIMA,MUKHOPADHYAY, INDRANIL,GUDI, GIRISH
申请号:
PE0014542013
公开号:
PE02342014A1
申请日:
2011.12.15
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Refers to compounds of 2 - amino - 4 - ariltiazol of formula (i) wherein Het is a compound of formula (a), (b), among others, where ra, RB and Rd are each H or alkyl (c1-c4) r1 is h p is (i) (ii), among others, where r is alkyl (C8 - C1) or a Heterocyclic Ring 3 to 15 members R8 is H, alkyl (c1-c4), among others R2 is Halogen,Haloalquilo (C1 C8) or haloalcoxi (C1 C8) M is 0 to 5.Preferred compounds are: dihydrogen phosphate [2 - [(- 2.4 - 1.3 - dimethyl - 1,2,3,4 - cyclohexanecarboxylic tetrahidrotieno [2,3-d] pyrimidin-5-yl) acetyl] imino] - 4 - [3-fluoro-4 - (trifluoromethyl) phenyl] - 3 - 3 (2H) - thiazole il] methyl dihydrogen phosphate [4 - [2,4-difluoro-3 - (trifluoromethyl) phenyl] - 2 - {[(- 2.4 - 1.3 - dimethyl - [1,2,3 Tetrahidrotieno, 4 - [2,3-d] pyrimidin-5-yl) acetyl] imino] - 1.3 - thiazole - 3 (2H) - yl) methyl among others.It also relates to a preparation method and a Pharmaceutical composition. These compounds are antagonists of the Transient Receptor Potential of anquirina Type 1 (TRPA1) being useful in the treatment of chronic pain, neuropathic pain, Pain osteoartriticoSE REFIERE A COMPUESTOS DERIVADOS DE 2-AMINO-4-ARILTIAZOL DE FORMULA (I) DONDE Het ES UN COMPUESTO DE FORMULA (a), (b), ENTRE OTROS, EN DONDE Ra, Rb Y Rd SON CADA UNO H O ALQUILO(C1-C4) R1 ES H P ES (i), (ii), ENTRE OTROS, EN DONDE R3 ES ALQUILO(C1-C8) O UN ANILLO HETEROCICLICO DE 3 A 15 MIEMBROS R8 ES H, ALQUILO(C1-C4), ENTRE OTROS R2 ES HALOGENO, HALOALQUILO(C1-C8) O HALOALCOXI(C1-C8) m ES DE 0 A 5. SON COMPUESTOS PREFERIDOS: DIHIDROGENO FOSFATO DE [2-{[(1,3-DIMETIL-2,4-DIOXO-1,2,3,4-TETRAHIDROTIENO[2,3-d]PIRIMIDIN-5-IL)ACETIL]IMINO}-4-[3-FLUORO-4-(TRIFLUOROMETIL)FENIL]-1,3-TIAZOL-3(2H)-IL]METILO DIHIDROGENO FOSFATO DE [4-[2,4-DIFLUORO-3-(TRIFLUOROMETIL)FENIL]-2-{[(1,3-DIMETIL-2,4-DIOXO-1,2,3,4-TETRAHIDROTIENO[2,3-d]PIRIMIDIN-5-IL)ACETIL]IMINO}-1,3-TIAZOL-3(2H)-IL]METILO ENTRE OTROS. TAMBIEN SE REFIERE UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPU
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