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199 条记录 (耗时 0.027 秒)

    Thyromimetic organic compounds
    141.
    发明申请
    Thyromimetic organic compounds 失效
    甲状腺素有机化合物

    公开(公告)号：US20020107390A1

    公开(公告)日：2002-08-08

    申请号：US09931683

    申请日：2001-08-16

    发明人： Paivi J. Kukkola

    IPC分类号： C07D281/02 ,  C07D277/02 ,  C07D279/12 ,  C07D269/02 ,  C07D265/30 ,  C07D263/04 ,  C07D243/08 ,  C07D239/04 ,  C07D233/02

    CPC分类号： C07C235/62 ,  C07C311/29 ,  C07C317/22 ,  C07C323/67 ,  C07C2601/14 ,  C07D213/64 ,  C07D213/75 ,  C07D295/192 ,  C07D295/26

    摘要： Compounds of the formula 1 in which W is O, S, S(O) or S(O)2; X is nullSR4, nullS(O)R4, or nullS(O)2R4, nullS(O)2NR5R6; or X is nullC(O)NR5R6 provided that nullC(O)NR5R6 is located at the 3null, 4null or 5null position; Y is O or H2; Z is hydrogen, halogen, hydroxy, optionally substituted alkoxy, aralkoxy, acyloxy or alkoxycarbonyloxy; R is hydrogen, halogen, trifluoromethyl, lower alkyl or cycloalkyl; R1 is hydroxy, optionally substituted alkoxy, aryloxy, heteroaryloxy, aralkyloxy, cycloalkoxy, heteroaralkoxy or -NR5R6; R2 is hydrogen, halogen or alkyl; R3 is halogen or alkyl; R4 is optionally substituted alkyl, aryl, aralkyl, heteroaralkyl or heteroaryl; R5, R6 and R7 are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or R5 and R6 combined are alkylene optionally interrupted by O, S, S(O), S(O)2 or NR7 which together with the nitrogen atom to which they are attached form a 5- to 7-membered ring; n represents zero or an integer from 1 to 4; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; a method to prevent and treat diseases associated with an imbalance of thyroid hormones, such as hypo- and hyperthyroidism, obesity, osteoporosis and depression; and, a method of lowering LDL cholesterol and Lp(a) levels in mammals using such compounds.

    摘要翻译： W为O，S，S（O）或S（O）2的式的化合物; X是-SR 4，-S（O）R 4或-S（O）2 R 4，-S（O）2 NR 5 R 6; 或者X是-C（O）NR 5 R 6，条件是-C（O）NR 5 R 6位于3'，4'或5'位; Y为O或H2; Z是氢，卤素，羟基，任选取代的烷氧基，芳烷氧基，酰氧基或烷氧基羰基氧基; R是氢，卤素，三氟甲基，低级烷基或环烷基; R1是羟基，任选取代的烷氧基，芳氧基，杂芳氧基，芳烷氧基，环烷氧基，杂芳烷氧基或-NR5R6; R2是氢，卤素或烷基; R3是卤素或烷基; R 4是任选取代的烷基，芳基，芳烷基，杂芳烷基或杂芳基; R5，R6和R7独立地是氢，任选取代的烷基，环烷基，芳基，芳烷基，杂芳基或杂芳烷基; 或R 5和R 6组合的是任选被O，S，S（O），S（O）2或NR 7中断的亚烷基，它们与它们所连接的氮原子一起形成5-至7-元环; n表示0或1至4的整数; 其药学上可接受的盐; 包含所述化合物的药物组合物; 一种预防和治疗与甲状腺激素失衡相关的疾病的方法，如甲状腺功能低下和甲状腺功能亢进，肥胖，骨质疏松症和抑郁症; 以及使用这种化合物降低哺乳动物的LDL胆固醇和Lp（a）水平的方法。

    Process for preparing optically active benzothiazepine compound and intermediate therefor
    143.
    发明授权
    Process for preparing optically active benzothiazepine compound and intermediate therefor 失效
    光学活性苯并硫氮杂化合物及其中间体的制备方法

    公开(公告)号：US5945533A

    公开(公告)日：1999-08-31

    申请号：US909077

    申请日：1997-08-14

    申请人： Tadashi Kometani ,  Hiroaki Matsumae ,  Takeji Shibatani

    发明人： Tadashi Kometani ,  Hiroaki Matsumae ,  Takeji Shibatani

    IPC分类号： C07D281/10 ,  C12P17/14 ,  C07D281/02

    CPC分类号： C07D281/10 ,  C12P17/14

    摘要： Powdery aggregate of 2-phenyl-1,5-benzothiazepin-3,4(2H,5H)-dione compound: ##STR1## wherein Ring A and Ring B are benzene ring having optionally substituent selected from lower alkyl, lower alkoxy and halogen, which is prepared by admixing solution of the compound (II) in polar organic solvent with solvent which does not substantially dissolve the compound (II) but is miscible with said polar organic solvent, and separating and collecting the resultant particles of the compound (II). Said aggregate of the compound (II) can be converted into optically active 3-hydroxy-2-phenyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one compounds (I) on industrial scale, which are useful as intermediate for various medicaments.

    摘要翻译： 2-苯基-1,5-苯并硫氮杂-3,4（2H，5H） - 二酮化合物的粉状骨料：其中环A和环B为任选具有选自低级烷基，低级烷氧基和卤素的取代基的苯环，其被制备 通过将化合物（II）在极性有机溶剂中的溶液与基本上不溶解化合物（II）但与所述极性有机溶剂混溶的溶剂混合，并分离和收集所得化合物（II）的颗粒。 所述化合物（II）的聚集体可以工业规模转化为光学活性的3-羟基-2-苯基-2,3-二氢-1,5-苯并硫氮杂-4（5H） - 酮化合物（I） 用作各种药物的中间体。

    Heterogeneous synthesis of azepinones from esters
    147.
    发明授权
    Heterogeneous synthesis of azepinones from esters 失效
    来自酯的氮杂异构体的非均相合成

    公开(公告)号：US5250680A

    公开(公告)日：1993-10-05

    申请号：US939536

    申请日：1992-09-02

    申请人： Daniel E. Martin

    发明人： Daniel E. Martin

    IPC分类号： C07D281/10 ,  C07D281/02

    CPC分类号： C07D281/10

    摘要： An amino-acid ester compound can be cyclized into a cyclic amido-carbonyl compound by contacting the amino-acid ester compound in a liquid medium with a heterogeneous acidic ion-exchange substance. For example, 2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)propionic acid, methyl ester, threo form, can be cyclized in an aqueous mixture into cis-2-(4-methoxyphenyl)-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one by employing a sulfonated polystyrene-divinylbenzene ion-exchange resin in its acid form, e.g., Dowex.RTM. 50X4-400. at yields exceeding 85 percent of theory, and the product can be used to make diltiazem hydrochloride.

    摘要翻译： 氨基酸酯化合物可通过使液体介质中的氨基酸酯化合物与异质酸性离子交换物质接触而环化成环状酰氨基 - 羰基化合物。 例如，2-羟基-3-（2-氨基苯硫基）-3-（4-甲氧基苯基）丙酸甲酯可以在水性混合物中环化成顺式-2-（4-甲氧基苯基）-3 - 羟基-2,3-二氢-1,5-苯并硫氮杂-4（5H） - 酮，其采用其酸形式的磺化聚苯乙烯 - 二乙烯基苯离子交换树脂，例如Dowex TM 50X4-400。 产量超过理论值的85％，该产品可用于制备盐酸地尔硫卓。

    Sulfimidoperoxycarboxylic acids
    148.
    发明授权
    Sulfimidoperoxycarboxylic acids 失效
    磺酰氧基羧基酸

    公开(公告)号：US5153189A

    公开(公告)日：1992-10-06

    申请号：US793803

    申请日：1991-11-18

    申请人： Walter Rupp ,  Hanspeter Gethoffer ,  Gerd Reinhardt ,  Frank Jaekel

    发明人： Walter Rupp ,  Hanspeter Gethoffer ,  Gerd Reinhardt ,  Frank Jaekel

    IPC分类号： A01N43/80 ,  C07D275/02 ,  C07D275/03 ,  C07D275/06 ,  C07D279/02 ,  C07D281/02 ,  C11D3/39 ,  C11D7/54

    CPC分类号： C07D275/02 ,  C07D275/03 ,  C07D275/06 ,  C11D3/3945

    摘要： Sulfimidoperoxycarboxylic acids of the formula ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.20 - alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl or C.sub.1 -C.sub.10 -alkylaryl,R.sup.2 is hydrogen, fluorine, chlorine, bromine or a group of the formula SO.sub.3 M, CO.sub.2 M or OSO.sub.3 M,M is hydrogen, an alkali metal or ammonium ion or the stoichiometric amount of an alkaline earth metal ion andX is C.sub.1 -C.sub.19 -alkylene or ortho-, meta- or para-arylene.These sulfimidoperoxycarboxylic acids are suitable as bleaches, oxidants or disinfectants.

    摘要翻译： 式中，A为式（1）的基团的亚磺酰基过氧羧酸为数字0,1或2，R 1为氢，氟，氯，溴，C 1 -C 20烷基，C 2 C 20 - 烯基，芳基或C 1 -C 10烷基芳基，R 2是氢，氟，氯，溴或式SO 3 M，CO 2 M或OSO 3 M的基团，M是氢，碱金属或铵离子或化学计量的 碱土金属离子和X是C 1 -C 19 - 亚烷基或邻 - 间 - 或对 - 亚芳基。 这些亚磺酰过氧羧酸适合作为漂白剂，氧化剂或消毒剂。