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3-Phenyl-5-ureidoisothiazol-4-carboximide and 3-amino-5-phenylisothiazole derivatives as kinase inhibitors
专利权人:
ALLERGAN; INC.
发明人:
MALONE, Thomas C.,HULL, Clarence,BORAL, Sougato,WURSTER, Julie A.,EDELMAN, Jeffrey L.,ROBINSON, Michael R.
申请号:
ES12810524
公开号:
ES2623652T3
申请日:
2012.12.27
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula I: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: X1 is N and X2 is S; L1 is selected from the group consisting of -N (R) -, -N (R) -C (>; = O) -N (R) -, -OC (>; = O) -N (R) -, -N (R) -C (>; = O) - and -C (>; = O) -N (R) -; L2 is selected from the group consisting of a covalent bond, -N (R) -, -N (R) -C (>; = O) -, -C (>; = O) -N (R) - and -N ( R) -C (>; = O) - N (R) -; each R is independently H or C1-6 alkyl; each R1 is independently selected from the group consisting of alkyl, C1-6 haloalkyl, halogen and OR; or wherein two adjacent R1 groups taken together with the carbon atoms to which they are attached form a six membered aryl or a five or six membered heteroaryl; n is 0, 1 or 2; R2 is selected from the group consisting of: a) H; b) C1-6 alkyl unsubstituted or substituted with one or two substituents selected from the group consisting of heterocyclyl, -C (>; = O) OR, hydroxy, C1-6 alkoxy and aryl; and c) ** Formula ** and R3 is selected from the group consisting of H, hydroxy, -NO2, aryl and heteroaryl, wherein said aryl or heteroaryl is unsubstituted or substituted with one to three substituents selected from the group consisting of halo, C1-6 haloalkyl and C1-6 alkyl.Un compuesto de fórmula I:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en donde: X1 es N y X2 es S; L1 se selecciona del grupo que consiste en -N(R)-, -N(R)-C(>;=O)-N(R)-, -O-C(>;=O)-N(R)-, -N(R)-C(>;=O)- y -C(>;=O)-N(R)- ; L2 se selecciona del grupo que consiste en un enlace covalente, -N(R)-, -N(R)-C(>;=O)-, -C(>;=O)-N(R)- y -N(R)-C(>;=O)- N(R)-; cada R es independientemente H o alquilo C1-6; cada R1 se selecciona independientemente del grupo que consiste en alquilo, haloalquilo C1-6, halógeno y OR; o en donde dos grupos R1 adyacentes tomados junto con los átomos de carbono a los que están unidos forman un arilo de seis miembros o un heteroarilo de cinco o seis miembros; n es 0, 1 o 2; R2 se selecciona del
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