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    Intermediates of benzoxazinone derivatives and preparation thereof
    2.
    发明授权
    Intermediates of benzoxazinone derivatives and preparation thereof 失效
    苯并恶嗪酮衍生物的中间体及其制备方法

    公开(公告)号：US06331627B1

    公开(公告)日：2001-12-18

    申请号：US09610623

    申请日：2000-07-05

    申请人： Vidya Bhushan Lohray ,  Braj Bhushan Lohray ,  Rao Bheema Paraselli ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti

    发明人： Vidya Bhushan Lohray ,  Braj Bhushan Lohray ,  Rao Bheema Paraselli ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti

    IPC分类号： C07D27916

    CPC分类号： C07C323/62 ,  C07C235/48 ,  C07C327/48 ,  C07D239/90 ,  C07D265/22 ,  C07D279/08

    摘要： The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereo-somers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their analogs, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, novel intermediates and pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及新型抗肥胖和低胆固醇血症化合物，其衍生物，其类似物，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂合物和含有它们的药学上可接受的组合物。 更具体地，本发明涉及通式（I）的新型β-芳基-α-氧代取代的烷基羧酸，其衍生物，它们的类似物，它们的互变异构形式，它们的立体异构体，它们的多晶型物，其药学上可接受的盐，它们的 药学上可接受的溶剂合物和含有它们的药学上可接受的组合物。本发明还涉及制备上述新化合物，其类似物，其衍生物，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，药学上可接受的盐 可接受的溶剂合物，新型中间体和含有它们的药物组合物。

    Benzothiazine derivative
    3.
    发明授权
    Benzothiazine derivative 失效
    苯并噻嗪衍生物

    公开(公告)号：US06664251B2

    公开(公告)日：2003-12-16

    申请号：US09955416

    申请日：2001-09-19

    申请人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Iwamori ,  Norio Inomata

    发明人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Iwamori ,  Norio Inomata

    IPC分类号： C07D27916

    CPC分类号： C07D275/06 ,  C07D279/02 ,  C07D417/06 ,  C07D513/10

    摘要： Disclosed are benzothiazine derivatives represented by the following formula (I): wherein the dashed line indicates the presence or absence of a bond; Z represents one of the following groups: in which R1 and R2 individually represent alkyl, aralkyl or the like, R3 represents H, alkyl or the like, R4 represents H, aralkyl or the like, X1, X2 and X3 individually represent O or S, and G represents substituted or unsubstituted ethylene, trimethylene or the like; Q1 and Q2 individually represent H, OH, halogen, alkoxy or the like; A represents alkylene, alkenylene or the like; Y represents CH, C═ or N; when Y is CH, m stands for 0 or 1, n stands for 1 or 2, B represents O, S, carbonyl or the like, when Y is C═, m stands for 1, n stands for 1 or 2, B represents: in which the double bond is linked to Y, R6 represents substituted or unsubstituted aryl or the like; when Y is N, m stands for 0 or 1, n stands for 2 or 3 and B represents carbonyl, sulfonyl or the like, E1 and E2 individually represent H or lower alkyl; and D represents an aromatic hydrocarbon group or an aromatic heterocyclic group; and salts thereof. The benzothiazine derivatives (I) and their salts according to the present invention have strong serotonin-2 blocking action, have excellent selectivity to this action against &agr;1 blocking action and have high safety. Accordingly, the present invention has made it possible to provide pharmaceuticals making use of antagonistic action against serotonin-2 receptors, for example, therapeutics for various circulatory diseases such as ishemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

    摘要翻译： 公开了由下式（I）表示的苯并噻嗪衍生物：其中虚线表示存在或不存在键; Z表示以下基团之一：其中R1和R2分别表示烷基，芳烷基等，R3表示H，烷基等，R4表示H，芳烷基等，X1，X2和X3各自表示O或S ，G表示取代或未取代的乙烯，三亚甲基等; Q1和Q2各自表示H，OH，卤素，烷氧基等; A表示亚烷基，亚烯基等; Y表示CH，C =或N; 当Y是CH时，m代表0或1，n代表1或2，B代表O，S，羰基等，当Y是C =，m代表1，n代表1或2，B代表 ：其中双键与Y连接，R​​6表示取代或未取代的芳基等; 当Y为N时，m代表0或1，n代表2或3，B代表羰基，磺酰基等，E1和E2分别代表H或低级烷基; D表示芳香族烃基或芳香族杂环基; 其盐。根据本发明的苯并噻嗪衍生物（I）及其盐具有强的5-羟色胺-2阻断作用，对该作用对α1阻断作用具有优异的选择性并具有高安全性。 因此，本发明使得可以提供利用针对5-羟色胺-2受体的拮抗作用的药物，例如用于各种循环系统疾病如血液性心脏病，脑血管障碍和外周循环障碍的治疗剂。

    Preparation of trans-thiazineindigo pigments
    7.
    发明授权
    Preparation of trans-thiazineindigo pigments 失效
    反噻嗪染料的制备

    公开(公告)号：US06649758B2

    公开(公告)日：2003-11-18

    申请号：US09886569

    申请日：2001-06-21

    申请人： Petra Maria Rothe ,  Leonhard Unverdorben ,  Bruno Piastra

    发明人： Petra Maria Rothe ,  Leonhard Unverdorben ,  Bruno Piastra

    IPC分类号： C07D27916

    CPC分类号： C09B7/00

    摘要： A process for preparing symmetrical or asymmetrical trans-thiazineindigo pigments of the formula (1) which comprises a) condensing, in an aqueous medium, a compound of the formula (2) with a compound of the formula (3a) or (3b) or a compound of the formula (4) with a compound of the formula (3a) and/or (3b)  by maintaining the reaction mixture at a temperature between 30 and 65° C. for at least 1 hour and then b) maintaining the reaction mixture at a temperature between 100 and 180° C. and a pressure between 2 and 50 bar for at least 1 hour in the presence of an amide.

    摘要翻译： 制备式（1）的对称或不对称的反噻嗪靛色素的方法，其包括：a）在水性介质中将式（2）的化合物与式（3a）或（3b）的化合物或 将式（4）的化合物与式（3a）和/或（3b）的化合物通过将反应混合物保持在30至65℃的温度至少1小时，然后b）将反应混合物保持在 温度为100至180℃，压力为2至50巴，在酰胺存在下至少1小时。

    Substituted 4H-1,4-benzothiazine-2-carboxamide: GABA brain receptor ligands
    8.
    发明授权
    Substituted 4H-1,4-benzothiazine-2-carboxamide: GABA brain receptor ligands 失效
    取代的4H-1,4-苯并噻嗪-2-甲酰胺：GABA脑受体配体

    公开(公告)号：US06448246B1

    公开(公告)日：2002-09-10

    申请号：US09578928

    申请日：2000-05-25

    申请人： Guolin Cai ,  Gang Liu ,  Pamela A. Albaugh

    发明人： Guolin Cai ,  Gang Liu ,  Pamela A. Albaugh

    IPC分类号： C07D27916

    CPC分类号： C07D417/12 ,  C07D279/16 ,  G01N33/948

    摘要： Disclosed are 4H-1,4-Benzothiazine-2-carboxamides. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, depression, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译： 公开了4H-1,4-苯并噻嗪-2-甲酰胺。 这些化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 这些化合物可用于诊断和治疗焦虑，抑郁，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。 还提供药物组合物，包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。