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    PREPARATION OF [2-METHYL-5-PHENYL-3-(PIPERAZIN-1-YLMETHYL)] PYRROLE DERIVATIVES
    1.
    发明申请
    PREPARATION OF [2-METHYL-5-PHENYL-3-(PIPERAZIN-1-YLMETHYL)] PYRROLE DERIVATIVES 审中-公开

    公开(公告)号：US20090118509A1

    公开(公告)日：2009-05-07

    申请号：US11911272

    申请日：2006-04-05

    申请人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Om Dutt Tyagi ,  Vasanth Nalam ,  Yogendra Kumar Chauhan

    发明人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Om Dutt Tyagi ,  Vasanth Nalam ,  Yogendra Kumar Chauhan

    IPC分类号： C07D401/14

    CPC分类号： C07D207/50 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12

    摘要： A process for the preparation of compounds of Formula I and their pharmaceutically acceptable acid addition salt wherein, R1 is phenyl or substituted phenyl R2 is selected from a group consisting of phenyl which is unsubstituted or substituted with 1 or 2 substituents, each independently selected from Cl, F, or pyridine, or naphthalene, or NHCOR4 wherein R4 is aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heterocyclyl. R3 is selected from a group of formula wherein R5 is phenyl which is unsubstituted or substituted with 1 or 2 substituents each independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, nitro, amino, haloalkyl, haloalkoxy etc.; unsubstituted or substituted benzyl; unsubstituted or substituted heteroaryl; unsubstituted or substituted heteroaroyl; unsubstituted or substituted diphenylmethyl, n=0-2 and X═—NCH3, CH2, S, SO, or SO2 Such that when R2 is phenyl, which is unsubstituted or substituted with 1 or 2 substituents, each independently selected from Cl, F; R5 is not C1-C4 alkyl, or X is not —NCH3, CH2, S, SO, or SO2, when n=1, or X is not —CH2 when n=0; comprising the steps of (a) reacting compound of Formula II with a chlorinating agent in the presence or absence of catalytic amount of N,N-dimethylformamide to yield the compound of Formula III, (b) reacting the compound of Formula III with a compound of Formula R1H (R1 is as defined above), in presence of a Lewis acid to obtain the compound of Formula IV, (c) reacting the compound of Formula IV with a compound of Formula R2NH2 (R2 is as defined above) in presence of catalytic amounts of an aryl or alkyl sulphonic acid in an organic solvent to obtain the compound of Formula V, (d) reacting the compound of Formula V with various secondary amines of the Formula R3H (R3 is as defined above) in the presence of formaldehyde and acetic acid in acetonitrile followed by crystallization yield the compound of Formula I, (e) purifying the compound of Formula I by crystallization, (f) converting the purified compound of Formula I to a pharmaceutically acceptable acid addition salt.

    Purified Arabinogalactan-Protein (AGP) composition useful in the treatment psoriasis and other disorders
    7.
    发明授权
    Purified Arabinogalactan-Protein (AGP) composition useful in the treatment psoriasis and other disorders 失效
    纯化的阿拉伯半乳聚糖蛋白（AGP）组合物可用于治疗牛皮癣和其他疾病

    公开(公告)号：US07601368B2

    公开(公告)日：2009-10-13

    申请号：US10931814

    申请日：2004-09-01

    申请人： Sudershan Kumar Arora ,  Vandita Srivastava ,  Sameer Shankar Walunj

    发明人： Sudershan Kumar Arora ,  Vandita Srivastava ,  Sameer Shankar Walunj

    IPC分类号： A61K36/00

    CPC分类号： A61K36/66 ,  Y02A50/39

    摘要： A purified Arabinogalactan-Protein (AGP) composition isolated through a selective method from the leaves and/or stems of Argemone mexicana plant is described. Also described is a purified Arabinogalactan-Protein (AGP) composition isolated from the leaves and/or stems of Argemone mexicana plant, which has one or more of the following effects: immunosuppression, lymphoproliferation inhibition, cytokine modulation such as IL-2 inhibition, IFN-γ inhibition, or IL-10 induction; keratinocyte proliferation inhibition, keratolytic activity and inhibitory activity in Mouse Ear Swelling test (MEST).

    摘要翻译： 描述了通过选择性方法从Argemone mexicana植物的叶和/或茎分离的纯化的阿拉伯半乳聚糖蛋白（AGP）组合物。 还描述了从茄科植物的叶子和/或茎分离的纯化的阿拉伯半乳聚糖蛋白（AGP）组合物，其具有以下一种或多种作用：免疫抑制，淋巴增殖抑制，细胞因子调节如IL-2抑制，IFN γ抑制或IL-10诱导; 角质形成细胞增殖抑制，角质溶解活性和小鼠耳肿胀试验（MEST）中的抑制活性。