MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS
    4.
    发明公开
    MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 有权
    趋化因子受体活性调节剂,结晶形式和过程

    公开(公告)号:EP2046779A2

    公开(公告)日:2009-04-15

    申请号:EP07813363.4

    申请日:2007-07-26

    CPC classification number: C07D403/12 C07D207/273 C07D317/72

    Abstract: The present invention provides a novel antagonist or partial agonists/antagonist of MCP-I receptor activity: N-((lR,2S,5R)-5-(tert-butylamino)-2- ((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l- yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((lR,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6- (trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and 'HET' are as described herein. Compounds that are useful intermediates of the process are also provided herein.

    Abstract translation: N - ((1R,2S,5R)-5-(叔丁基氨基)-2 - ((S)-2-氧代-3 - (6-(三氟甲基)喹唑啉-4-基氨基)吡咯烷-1-基)环己基)乙酰胺,或其药学上可接受的盐,溶剂化物或前药,其具有理想药理学特性的意想不到的组合。 还提供了本发明的晶体形式。 含有其的药物组合物及其作为治疗炎性疾病,变应性疾病,自身免疫疾病,代谢疾病,癌症和/或心血管疾病的药物的方法也是本发明的目的。 本发明还提供了制备式(I)化合物的方法,其包括N - ((1R,2S,5R)-5-(叔丁基氨基)-2 - ((S)-2-氧代-3- (三氟甲基)喹唑啉-4-基氨基)吡咯烷-1-基)环己基)乙酰胺:其中R 1,R 8,R 9,R 10和'HET'如本文所述。 本文还提供了作为该方法的有用中间体的化合物。

    PYRIDIL-SUBSTITUTED SPIRO-HYDANTOIN COMPOUNDS AND USE THEREOF
    5.
    发明公开
    PYRIDIL-SUBSTITUTED SPIRO-HYDANTOIN COMPOUNDS AND USE THEREOF 审中-公开
    吡啶取代的螺型 - 海南霉素化合物及其用途

    公开(公告)号:EP1828193A1

    公开(公告)日:2007-09-05

    申请号:EP05854057.6

    申请日:2005-12-14

    CPC classification number: C07D487/10

    Abstract: A class of substituted spiro-hydantoin compounds (II) having the formula: (II) its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group, as defined herein, is provided. Pharmaceutical compositions and methods of treating anti-inflammatory and/or immune diseases with the pyridyl-substituted spiro-hydantoin compounds are also objectives of this invention.

    Abstract translation: 提供了一类具有下式的取代螺海因化合物(II):(II)其药学上可接受的盐,对映异构体,溶剂合物或前药,其中R16是如本文所定义的取代的吡啶基。 用吡啶基取代的螺海因化合物治疗抗炎和/或免疫疾病的药物组合物和方法也是本发明的目的。

Patent Agency Ranking