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    Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists
    2.
    发明授权
    Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists 失效
    取代的氮杂双环己烷衍生物作为毒蕈碱受体拮抗剂

    公开(公告)号：US07517905B2

    公开(公告)日：2009-04-14

    申请号：US10552456

    申请日：2003-04-09

    申请人： Anita Mehta ,  Bruhaspathy Miriyala ,  Sudershan Kumar Arora ,  Jang Bahadur Gupta

    发明人： Anita Mehta ,  Bruhaspathy Miriyala ,  Sudershan Kumar Arora ,  Jang Bahadur Gupta

    IPC分类号： A61K31/403 ,  C07D209/52

    CPC分类号： C07D209/52

    摘要： This invention relates to the derivatives of substituted azabicyclo hexanes. The compounds of this invention can function as muscarinic receptor antagonists and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.

    摘要翻译： 本发明涉及取代的氮杂双环己烷的衍生物。 本发明的化合物可用作毒蕈碱受体拮抗剂，可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病。 本发明还涉及制备本发明化合物的方法，含有本发明化合物的药物组合物和通过毒蕈碱受体介导的疾病的治疗方法。

    SUBSTITUTED OXAZOLIDINONE DERIVATIVES
    3.
    发明申请
    SUBSTITUTED OXAZOLIDINONE DERIVATIVES 审中-公开
    取代的氧杂环丁酮衍生物

    公开(公告)号：US20090247545A1

    公开(公告)日：2009-10-01

    申请号：US11577083

    申请日：2004-12-28

    申请人： Mukund Keshao Gurjar ,  Madhusudan Nagorao Deshmukh ,  Anita Mehta ,  Sudershan Kumar Arora ,  Ashok Rattan

    发明人： Mukund Keshao Gurjar ,  Madhusudan Nagorao Deshmukh ,  Anita Mehta ,  Sudershan Kumar Arora ,  Ashok Rattan

    IPC分类号： A61K31/496 ,  C07D413/10 ,  A61P31/04

    CPC分类号： C07D263/20 ,  C07D413/10

    摘要： The present invention provides substituted oxazolidinone derivatives, which can be used as antimicrobial agents. Compounds disclosed can be used for the treatment or prevention of a condition caused by or contributed to by bacteria, such as, inter alia, multiply-resistant Staphylococci, Streptococci, Enterococci, Bacterioides spp., Clostridium spp., Mycobacterium spp. Bacillus spp., Corynebacterium spp. Heptoslreptacoccus spp. Listeria spp., Legionella spp., Haemophilus influenza, Moraxella, Eschericia faecalis, and Eschericia coli. Processes for the preparation of disclosed compounds, pharmaceutical compositions thereof, and method of treating microbial infection are provided.

    摘要翻译： 本发明提供了可用作抗微生物剂的取代的恶唑烷酮衍生物。 所公开的化合物可用于治疗或预防由细菌引起的或由细菌引起的病症，例如多重耐药葡萄球菌，链球菌，肠球菌，细菌属，梭菌属，分枝杆菌属。 芽孢杆菌属，棒状杆菌属 肝细胞线粒体 利斯特氏菌属（Listeria spp。），军团菌属（Legionella spp。），嗜血杆菌流感，流感嗜血杆菌，大肠埃希氏菌和大肠埃希氏菌。 提供了制备所公开化合物的方法，其药物组合物，以及治疗微生物感染的方法。

    Purified Arabinogalactan-Protein (AGP) composition useful in the treatment psoriasis and other disorders
    5.
    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。

    PROCESS FOR THE PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT
    9.
    发明申请
    PROCESS FOR THE PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT 审中-公开
    制备ATAZANAVIR或其BISULFATE盐的方法

    公开(公告)号：US20140343290A1

    公开(公告)日：2014-11-20

    申请号：US14235127

    申请日：2012-07-25

    申请人： Rakesh Kumar Singh ,  Nagaraju Gottumukkala ,  Mahavir Singh Khanna ,  Rajesh Kumar Thaper ,  Mohan Prasad ,  Sudershan Kumar Arora

    发明人： Rakesh Kumar Singh ,  Nagaraju Gottumukkala ,  Mahavir Singh Khanna ,  Rajesh Kumar Thaper ,  Mohan Prasad ,  Sudershan Kumar Arora

    IPC分类号： C07D213/42

    CPC分类号： C07D213/42

    摘要： The present invention relates to an improved process for the preparation of atazanavir bisulfate, an inhibitor of retroviral aspartate protease. The process of the present invention comprises conversion of 1,1-dimethylethyl[(2S,3R)-4-chloro-3-hydroxy-phenylbutan-2-yl]carbamate (Formula II) into 1-[4-(pyridine-2-yl)-phenyl]-4(S)-5 hydroxy-2-N-tert-butoxycarbonylamino-5(S)—N—(N-methoxycarbonyl-(L)-tert-leucyl)amino-6-phenyl-2-azahexane (Formula VII) without isolating intermediate compounds formed therein, followed by its subsequent conversion to atazanavir or its bisulfate salt.

    摘要翻译： 本发明涉及一种制备逆转录病毒天冬氨酸蛋白酶抑制剂阿扎那韦硫酸氢盐的改进方法。 本发明的方法包括将[（2S，3R）-4-氯-3-羟基 - 苯基丁-2-基]氨基甲酸酯（式II）的1,1-二甲基乙基酯转化为1- [4-（吡啶-2 - 基） - 苯基] -4（S）-5-羟基-2-N-叔丁氧基羰基氨基-5（S）-N-（N-甲氧基羰基 - （L） - 叔 - 亮氨酰基）氨基-6-苯基-2 （式Ⅶ），而不分离其中形成的中间体化合物，随后转化成阿扎那韦或其硫酸氢盐。

    PREPARATION OF [2-METHYL-5-PHENYL-3-(PIPERAZIN-1-YLMETHYL)] PYRROLE DERIVATIVES
    10.
    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.