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Co-crystals and salts of CCR3 inhibitors
专利权人:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人:
FRANK, MARKUS,HAEBERLE, HANS,HENRY, MANUEL,PACHUR, THORSTEN,SANTAGOSTINO, MARCO,STERTZ, UWE,TREBING, THOMAS,WERTHMANN, ULRIKE
申请号:
ES11764572
公开号:
ES2535264T3
申请日:
2011.10.06
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Co-crystals of compounds of formula 1 ** Formula ** * (HX) j R2b 1 in which R 1 is C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 haloalkyl, halogen; m is 1, 2 or 3; each of R2a and R2b is independently selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C3-6 cycloalkyl, COO-C1-6 alkyl, O-C1-6 alkyl, CONR2b.1R2b. 2, halogen; R2b.1 is H, C1-6 alkyl, C0-4 alkyl-C3-6 cycloalkyl, C1-6 haloalkyl; R2b.2 is H, C1-6 alkyl; or R2b.1 and R2b.2 together are a C3-6 alkylene group that forms a heterocyclic ring with the nitrogen atom, where optionally a carbon atom or the ring is replaced by an oxygen atom; R3 is H, C1-6 alkyl; X is an anion selected from the group consisting of chloride, bromide, iodide, sulfate, phosphate, methanesulfonate, nitrate, maleate, acetate, benzoate, citrate, salicylate, fumarate, tartrate, dibenzoyltartrate, oxalate, succinate, benzoate and p-toluenesulfonate ; j is 0, 0.5, 1, 1.5 or 2; with a co-crystal forming agent selected from the group consisting of orotic acid, hippuric acid, L-pyroglutamic acid, D-pyroglutamic acid, nicotinic acid, L - (+) - ascorbic acid, saccharin, piperazine, acid 3 - hydroxy-2-naphthoic acid, mucic acid (galactaric), pamoic acid (embonic), stearic acid, colic acid, deoxycholic acid, nicotinamide, isonicotinamide, succinamide, uracil, L-lysine, L-proline, D-valine, L- arginine, glycineCo-cristales de compuestos de fórmula 1**Fórmula** * (HX)j R2b 1 en la que R1 es alquilo C1-6, haloalquilo C1-6, O-haloalquilo C1-6, halógeno; m es 1, 2 ó 3; cada uno de R2a y R2b se selecciona independientemente entre H, alquilo C1-6, alquenilo C1-6, alquinilo C1-6, cicloalquilo C3-6, COO-alquilo C1-6, O-alquilo C1-6, CONR2b.1R2b.2, halógeno; R2b.1 es H, alquilo C1-6, alquil C0-4-cicloalquilo C3-6, haloalquilo C1-6; R2b.2 es H, alquilo C1-6; o R2b.1 y R2b.2 juntos son un grupo alquileno C3-6 que forma con el átomo de nitrógeno un anillo heterocíclico, donde opcionalmente un átomo de carbono o el anillo está reemplazado por un átomo de oxígeno; R3
来源网站:
中国工程科技知识中心
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