PANKNIN, OLAF,BAURLE, STEFAN,RING, SVEN,SCHWEDE, WOLFGANG,BONE, WILHELM,NOWAK-REPPEL, KATRIN,BENDER, ECKHARD,NUBBEMEYER, REINHARD,GNOTH, MARK JEAN
申请号：
PE0011142014
公开号：
PE16992014A1
申请日:
2013.01.15
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Espiroindolina refers to compounds of formula (i) where W is o u s (o) x, where X is 0 to 2 r1 is H, alkyl, cycloalkyl (C1 - C6) (C3 - C10), aryl, among others R2 is aryl or heteroaryl optionally replaced with R4, where r is Halogen, Hydroxy, C (o) NH2, among others R3 is C (o) n (r5a) (r5b), N (H) C (o) R6, among others, where r5a, r5b and R6 are each h, alkyl (C1 - C6)Alquenilo (C2 - C6), among others.Preferred compounds are: N - (3 - [2 - cloropiridin - yl) methyl] - 1 - [(4-fluorophenyl) sulfonyl] - methyl - (2 , 3, 5 , 6 - hexahidroespiro [3,4 - piran indole carboxamide] - 5 - (N - 2 - clorobencil) - 1 - [(4-fluorophenyl) sulfonyl] - methyl - (2, 3 , 5, 6 - hexahidroespiro [3,4 - piran] indole - 5 - carboxamide 1 - [(4-fluorophenyl) Sul Fonil] - 2 - methyl - N - [3 - (trifluoromethyl) pyridin-2-yl] methyl} - (, 3, 5 , 6 - hexahidroespiro [indole - 34 - piran] - 5 - carboxamide among others. It also relates to a Pharmaceutical composition. These compounds are antagonists of the receptor, gonadotropin-releasing hormone (GnRH) being useful in the treatment of fibroids in the uterus, endometriosis, polycystic ovarySE REFIERE A COMPUESTOS DERIVADOS DE ESPIROINDOLINA DE FORMULA (I) DONDE W ES O U S(O)x, DONDE x ES DE 0 A 2 R1 ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C10), ARILO, ENTRE OTROS R2 ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON R4, EN DONDE R4 ES HALOGENO, HIDROXI, C(O)NH2, ENTRE OTROS R3 ES C(O)N(R5a)(R5b), N(H)C(O)R6, ENTRE OTROS, EN DONDE R5a, R5b Y R6 SON CADA UNO H, ALQUILO(C1-C6), ALQUENILO(C2-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-[(3-CLOROPIRIDIN-2-IL)METIL]-1-[(4-FLUOROFENIL)SULFONIL]-2-METIL-1,2,2,3,5,6-HEXAHIDROESPIRO[INDOL-3,4-PIRAN]-5-CARBOXAMIDA N-(2-CLOROBENCIL)-1-[(4-FLUOROFENIL)SULFONIL]-2-METIL-1,2,2,3,5,6-HEXAHIDROESPIRO[INDOL-3,4-PIRAN]-5-CARBOXAMIDA 1-[(4-FLUOROFENIL)SULFONIL]-2-METIL-N-{[3-(TRIFLUOROMETIL)PIRIDIN-2-IL]METIL}-1,2,2,3,5,6-HEXAHIDROESPIRO[INDOL-3,4-PIRAN]-5-CARBOXAMIDA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COM
