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61. 发明申请

WO02020463A2 FXR MODULATORS 审中-公开
标题翻译： FXR调制器
公开(公告)号：WO02020463A2
公开(公告)日：2002-03-14
申请号：PCT/US2001/027239
申请日：2001-08-31
IPC分类号： A61P35/00 , C07C233/75 , C07C237/22 , C07C311/19 , C07C311/29 , C07D209/48 , C07D241/44 , C07D279/02 , A61K31/16 , C07C311/17 , C07K14/705
CPC分类号： C07D209/48 , C07C233/75 , C07C237/22 , C07C311/19 , C07C311/29 , C07C2601/14 , C07D241/44 , C07D279/02
摘要： The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7 alpha -hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR gamma and PPAR alpha . Thus, compounds described herein are useful in treating other biological activities such as obesity, diabetes, lipid associated disorders, cancer, inflammatory disorders, disorders involving a disrupted or dysfunctional epidermal barrier, and various other metabolic disorders.
摘要翻译：本发明提供了可用于调节法呢酯X受体（FXR）的化合物，药物组合物和方法。由于FXR涉及负面控制胆固醇7α-羟化酶（cyp7a）的表达水平，参与胆固醇胆固醇氧化代谢的限速酶可用于治疗与异常高相关的疾病或低胆固醇水平在某些方面，本文所述的FXR调节剂（例如拮抗剂）阻断某些胆酸（FXR的内源性配体）产生的cyp7a表达的负反馈下调。此外，由于FXR在一些细胞类型中与类视黄醇X受体（RXR）形成异源二聚体，因此细胞中FXR活性水平的调节对由RXR或其他RXR相互作用介导的各种生物过程具有广泛的影响蛋白质如PPARγ和PPARα。因此，本文所述的化合物可用于治疗其它生物活性，例如肥胖症，糖尿病，脂质相关疾病，癌症，炎症性疾病，涉及破坏性或功能失调的表皮屏障的疾病以及各种其他代谢紊乱。

62. 发明申请

WO0142219A3 NOVEL SUBSTITUTED PHENANTHRIDINONES AND METHODS OF USE THEREOF 审中-公开
标题翻译：新的取代的苯并芘酮及其使用方法
公开(公告)号：WO0142219A3
公开(公告)日：2001-12-13
申请号：PCT/US0042656
申请日：2000-12-07
申请人： INOTEK CORP , SZABO CSABA , JAGTAP PRAKASH , SOUTHAN GARRY , SALZMAN ANDREW L
发明人： SZABO CSABA , JAGTAP PRAKASH , SOUTHAN GARRY , SALZMAN ANDREW L
IPC分类号： C07D221/12 , C07D279/02 , A61K31/473 , A61P9/00 , A61P25/00
CPC分类号： C07D279/02 , C07D221/12
摘要： This invention provides a novel class of substituted 6(5H) phenanthridinone compounds. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described.
摘要翻译：本发明提供了一类新的取代的6（5H）菲啶酮化合物。还描述了药物组合物，制备和使用该化合物或其药学上可接受的盐，水合物，前药或其混合物的方法。

63. 发明申请

WO0140208A3 PROCESS FOR SYNTHESIS OF 4-HYDROXY-2H-1,2-BENZOTHIAZINE-3-CARBOXAMIDES 审中-公开
标题翻译：合成4-羟基-2H- 1,2-BENZOTHIAZ-3-CARBOXAMID的方法
公开(公告)号：WO0140208A3
公开(公告)日：2001-11-29
申请号：PCT/YU0000009
申请日：2000-04-06
申请人： AD ZDRAVLJE , STANKOVIC SLOBODAN , STOJANOVIC NEBOJSA , MILOSEVIC SNEZANA , NIKOLIC DEJAN
发明人： STANKOVIC SLOBODAN , STOJANOVIC NEBOJSA , MILOSEVIC SNEZANA , NIKOLIC DEJAN
IPC分类号： C07D279/02 , C07D417/12
CPC分类号： C07D417/12 , C07D279/02
摘要： Suggested invention is related to the field of organic chemistry technology, specifically to the process for preparation of the compound 4-hydroxy - 2 - methyl - 2 H - 1 , 2 - benzothiazine - 3 - carboxamide - 1 , 1 -dioxide, of general formula (I), wherein R denotes one of the following radicals: alkyl group (C2-C6), cycloalkyl, benzyl, phenyl, pyridyl, methyl-pyridyl, pyrimidyl, thiazole, isothiazole. Concerning clinical practice, the special interest, as non-steroidal antirheumatics characterized by anti-inflammatory and analgesic properties, belongs to: piroxicam (4-hydroxy-2-methyl-N-(2-pyridinyl-2H-1,2-benzothiazine-3-carboxamid-1,1-dioxide)), isoxicam (4-hydroxy-2-methyl-N-(5-methyl-3-isoxazolyl-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide)) and sudoxicam (4-hydroxy-2-methyl-N-2-thiazolyl-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide). Individual characteristics of the present invention are: the use of ethylester and dimethyl formamide with sodium ethoxide for opening of the cycle and for work at low temperatures in the mentioned phase; afterwards, methylation and final condensation with an amine of general formula NH2-Retard tablete, wherein R denotes: 2-pyridyl, alkyl substituted 2-pyridyl, 2-thiazole, 2-thiazole substituted with one or two alkyl groups, while each alkyl has from 1 to 4 carbon atoms or 5-methyl-3- isoxazolyl, using specific catalysts and adsorbents in an inert solvent and inert atmosphere.
摘要翻译：建议的发明涉及有机化学技术领域，具体涉及制备化合物4-羟基-2-甲基-2H-1,2-苯并噻嗪-3-甲酰胺-1,1-二氧化物的方法式（I）其中R表示以下基团之一：烷基（C 2 -C 6），环烷基，苄基，苯基，吡啶基，甲基 - 吡啶基，嘧啶基，噻唑，异噻唑。关于临床实践，作为以抗炎和止痛性质为特征的非类固醇抗风湿剂的特殊兴趣属于：炎酷茜（4-羟基-2-甲基-N-（2-吡啶基-2H-1,2-苯并噻嗪-2-基） 3-甲酰胺-1,1-二氧化物）），异山梨醇（4-羟基-2-甲基-N-（5-甲基-3-异恶唑基-2H-1,2-苯并噻嗪-3-甲酰胺-1,1-二氧化物））和苏氨昔康（4-羟基-2-甲基-N-2-噻唑基-2H-1,2-苯并噻嗪-3-甲酰胺-1,1-二氧化物）。本发明的个体特征是：使用乙酯和二甲基甲酰胺与乙醇钠打开循环并在上述阶段在低温下工作; 然后与通式为NH 2的胺进行甲基化和最终缩合，其中R表示：2-吡啶基，烷基取代的2-吡啶基，2-噻唑，被一个或两个烷基取代的2-噻唑，而每个烷基具有 1至4个碳原子或5-甲基-3-异恶唑基，在惰性溶剂和惰性气氛中使用特定的催化剂和吸附剂。

64. 发明申请

WO0054759A3 LXR MODULATORS 审中-公开
标题翻译： LXR调制器
公开(公告)号：WO0054759A3
公开(公告)日：2001-02-15
申请号：PCT/US0006611
申请日：2000-03-15
申请人： TULARIK INC
发明人： LI LEPING , MEDINA JULIO C , HASEGAWA HIROHIKO , CUTLER SERENA T , LIU JIWEN , ZHU LIUSHENG , SHAN BEI , LUSTIG KEVIN
IPC分类号： C07D295/10 , A61K31/136 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/196 , A61K31/235 , A61K31/24 , A61K31/27 , A61K31/277 , A61K31/351 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/4164 , A61K31/4188 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/429 , A61K31/433 , A61K31/4406 , A61K31/4436 , A61K31/47 , A61K31/472 , A61K31/5375 , A61K31/538 , A61K31/5415 , A61K31/55 , A61P3/02 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P19/10 , A61P25/30 , C07C233/60 , C07C233/75 , C07C235/42 , C07C271/28 , C07C271/58 , C07C275/32 , C07C307/10 , C07C311/08 , C07C311/21 , C07C311/29 , C07C311/44 , C07C317/14 , C07D209/04 , C07D209/08 , C07D213/71 , C07D215/36 , C07D215/58 , C07D223/16 , C07D261/10 , C07D265/36 , C07D271/08 , C07D271/12 , C07D277/20 , C07D277/54 , C07D279/02 , C07D285/14 , C07D295/185 , C07D295/20 , C07D295/215 , C07D309/14 , C07D333/34 , C07D333/40 , C07D333/42 , C07D409/04 , C07D409/12 , C07D413/12 , C07D513/04
CPC分类号： C07D285/14 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/196 , A61K31/24 , A61K31/27 , A61K31/277 , A61K31/381 , A61K31/4164 , A61K31/4188 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/429 , A61K31/433 , A61K31/4406 , A61K31/4436 , A61K31/47 , C07C233/60 , C07C233/75 , C07C235/42 , C07C271/28 , C07C271/58 , C07C275/32 , C07C307/10 , C07C311/08 , C07C311/21 , C07C311/29 , C07C311/44 , C07C317/14 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D209/04 , C07D271/12 , C07D295/185 , C07D295/215 , C07D333/34 , C07D409/12
摘要： The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.
摘要翻译：本发明提供用于调节细胞中LXR的作用的化合物，组合物和方法。化合物和组合物既可用作LXR功能的诊断指标，也可用作药理活性剂。化合物和组合物特别用于治疗与胆固醇代谢相关的疾病状态，特别是动脉粥样硬化和高胆固醇血症。

65. 发明申请

WO00054759A2 LXR MODULATORS 审中-公开
标题翻译： LXR调制器
公开(公告)号：WO00054759A2
公开(公告)日：2000-09-21
申请号：PCT/US2000/006611
申请日：2000-03-15
IPC分类号： C07D295/10 , A61K31/136 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/196 , A61K31/235 , A61K31/24 , A61K31/27 , A61K31/277 , A61K31/351 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/4164 , A61K31/4188 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/429 , A61K31/433 , A61K31/4406 , A61K31/4436 , A61K31/47 , A61K31/472 , A61K31/5375 , A61K31/538 , A61K31/5415 , A61K31/55 , A61P3/02 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P19/10 , A61P25/30 , C07C233/60 , C07C233/75 , C07C235/42 , C07C271/28 , C07C271/58 , C07C275/32 , C07C307/10 , C07C311/08 , C07C311/21 , C07C311/29 , C07C311/44 , C07C317/14 , C07D209/04 , C07D209/08 , C07D213/71 , C07D215/36 , C07D215/58 , C07D223/16 , C07D261/10 , C07D265/36 , C07D271/08 , C07D271/12 , C07D277/20 , C07D277/54 , C07D279/02 , C07D285/14 , C07D295/185 , C07D295/20 , C07D295/215 , C07D309/14 , C07D333/34 , C07D333/40 , C07D333/42 , C07D409/04 , C07D409/12 , C07D413/12 , C07D513/04 , A61K31/00
CPC分类号： C07D285/14 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/196 , A61K31/24 , A61K31/27 , A61K31/277 , A61K31/381 , A61K31/4164 , A61K31/4188 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/429 , A61K31/433 , A61K31/4406 , A61K31/4436 , A61K31/47 , C07C233/60 , C07C233/75 , C07C235/42 , C07C271/28 , C07C271/58 , C07C275/32 , C07C307/10 , C07C311/08 , C07C311/21 , C07C311/29 , C07C311/44 , C07C317/14 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D209/04 , C07D271/12 , C07D295/185 , C07D295/215 , C07D333/34 , C07D409/12 , Y02A50/411
摘要： The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.
摘要翻译：本发明提供用于调节细胞中LXR的作用的化合物，组合物和方法。化合物和组合物既可用作LXR功能的诊断指标，也可用作药理活性剂。化合物和组合物特别用于治疗与胆固醇代谢相关的疾病状态，特别是动脉粥样硬化和高胆固醇血症。

66. 发明申请

WO99041230A1 PROCESSES AND INTERMEDIATES USEFUL TO MAKE ANTIFOLATES 审中-公开
标题翻译：使用过程和中间体有助于制备抗体
公开(公告)号：WO99041230A1
公开(公告)日：1999-08-19
申请号：PCT/US1999/001689
申请日：1999-01-27
IPC分类号： C07D333/40 , A61K31/519 , A61P35/00 , C07D275/02 , C07D307/68 , C07D333/38 , C07D471/04 , C07C255/00 , C07D207/02 , C07D211/04 , C07D213/02 , C07D231/02 , C07D231/04 , C07D231/06 , C07D231/10 , C07D233/02 , C07D233/04 , C07D233/54 , C07D237/02 , C07D237/04 , C07D237/06 , C07D239/02 , C07D239/04 , C07D239/06 , C07D239/20 , C07D239/24 , C07D241/02 , C07D241/06 , C07D241/10 , C07D261/02 , C07D263/02 , C07D265/02 , C07D265/04 , C07D265/28 , C07D277/02 , C07D279/02 , C07D279/04 , C07D279/10 , C07D307/02 , C07D333/02 , C07D405/14 , C07D409/14 , C07D413/02 , C07D417/02 , C07D471/02
CPC分类号： C07D471/04 , C07D333/38 , Y02P20/55
摘要： The present invention concerns intermediates, and processes directed to and from those intermediates, to a series of pyrimidine derivatives of formula (V), which are intermediates to useful antifolate compounds or are themselves useful antifolate compounds.
摘要翻译：本发明涉及涉及中间体和从这些中间体引入的一系列式（Ⅴ）嘧啶衍生物的方法，它们是有用的抗叶酸化合物的中间体，或本身是有用的抗叶酸化合物。

67. 发明申请

WO98033496A1 SULPHONAMIDE DERIVATIVES 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：WO98033496A1
公开(公告)日：1998-08-06
申请号：PCT/US1998/001881
申请日：1998-01-30
IPC分类号： C07D295/12 , A61K31/18 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4439 , A61K31/4465 , A61K31/451 , A61K31/455 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K31/54 , A61K31/695 , C07C307/06 , C07C307/08 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C311/08 , C07C311/09 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/16 , C07C311/18 , C07C311/24 , C07C311/29 , C07C311/39 , C07C311/53 , C07D207/16 , C07D207/26 , C07D207/277 , C07D211/18 , C07D211/26 , C07D211/28 , C07D213/42 , C07D213/76 , C07D213/81 , C07D213/82 , C07D239/26 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D271/06 , C07D277/10 , C07D277/20 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/56 , C07D277/66 , C07D279/02 , C07D295/20 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/71 , C07D333/16 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/34 , C07D333/38 , C07D333/40 , C07D333/58 , C07D333/68 , C07D409/04
CPC分类号： A61K31/18 , A61K31/381 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/4418 , A61K31/451 , A61K31/455 , C07C307/08 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C311/09 , C07C311/14 , C07C311/16 , C07C311/24 , C07C311/29 , C07C311/39 , C07C311/53 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D207/277 , C07D211/18 , C07D211/28 , C07D213/42 , C07D213/81 , C07D213/82 , C07D239/26 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D271/06 , C07D277/24 , C07D277/28 , C07D277/56 , C07D277/66 , C07D279/02 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/71 , C07D333/16 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/34 , C07D333/38 , C07D333/58 , C07D333/68 , C07D409/04
摘要： Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula (I): R -L-NHSO2R , in which R represents an unsubstituted or substituted aromatic or heteroaromatic group; R represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R R N in which R and R each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring; and pharmaceutically acceptable salts thereof. Also disclosed are novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them.
摘要翻译：可以使用有效量的式（I）化合物：R 1 -L-NHSO 2 R 2来加强哺乳动物中的谷氨酸受体功能，其中R 1表示未取代或取代的芳族或杂芳族基团; （1-6C）烷基，（3-6C）环烷基，（1-6C）氟代烷基，（1-6C）氯烷基，（2-6C）烯基，（1-4C）烷氧基（1-4C ）烷基，未被取代或被卤素取代的苯基，（1-4C）烷基或（1-4C）烷氧基或式R 3 R 4的基团，其中R 3和R 4，吡啶基，哌啶基，吗啉代，哌嗪基，六氢氮杂或八氢az嗪基;（Ⅳ）代表（1-4C）烷基，或与它们所连接的氮原子一起形成氮杂环丁烷基，吡咯烷基，哌啶基，（1-6C）烷基，（2-6C）烷基，（2-6C）烯基，芳基（2-甲基苯基）丙烯基， 6C）烯基和芳基，或两个与它们所连接的碳原子或碳原子一起形成（3-8C）碳环的取代基; 及其药学上可接受的盐。还公开了式（I）的新化合物，其制备方法和含有它们的药物组合物。

68. 发明申请

WO1996026195A1 BENZOTHIAZINE DIOXIDES AS ENDOTHELIN ANTAGONISTS 审中-公开
标题翻译：苯扎他定二氧化物作为内皮素拮抗剂
公开(公告)号：WO1996026195A1
公开(公告)日：1996-08-29
申请号：PCT/US1996001093
申请日：1996-01-26
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BERRYMAN, Kent, Alan , BUNKER, Amy, Mae , DOHERTY, Annette, Marian , EDMUNDS, Jeremy, John
IPC分类号： C07D279/02
CPC分类号： C07D275/06 , C07D279/02 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： Novel benzothiazine dioxides which are antagonists of endothelin are described, as well as novel intermediates used in their preparation, methods for the preparation, and pharmaceutical compositions of the same, which are useful in treating elevated levels of endohelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
摘要翻译：描述了作为内皮素拮抗剂的新型苯并噻嗪二氧化物，以及其制备中使用的新型中间体，其制备方法及其药物组合物，其可用于治疗高水平的内皮素，重要的血管性恶性和肺动脉高压，脑梗塞，脑缺血，充血性心力衰竭和蛛网膜下腔出血。

69. 发明申请

WO1995018117A1 BENZOTHIAZINE DERIVATIVE 审中-公开
标题翻译：苯并噻嗪衍生物
公开(公告)号：WO1995018117A1
公开(公告)日：1995-07-06
申请号：PCT/JP1994002194
申请日：1994-12-22
申请人： SUNTORY LIMITED , MIZUNO, Akira , SHIBATA, Makoto , IWAMORI, Tomoe , INOMATA, Norio
发明人： SUNTORY LIMITED
IPC分类号： C07D279/02
CPC分类号： C07D417/06 , C07D279/02 , C07D513/10
摘要： A benzothiazine derivative represented by general formula (I) or a salt thereof, wherein the broken line indicates the presence or absence of a bond; Z represents any of the groups (a), (b), (c), (d), (e), (f), (g) and (h); (wherein R1 represents alkyl, aralkyl, etc.; R2 represents alkyl, aralkyl, etc.; R3 represents H, alkyl, etc.; R4 represents H, aralkyl, etc.; X1, X2 and X3 represent each O or S; and G represents optionally substituted ethylene, trimethylene, etc.); A represents alkylene, alkenylene, etc.; Y represents CH, C= or N, provided when Y is CH, then m represents O or 1, n represents 1 or 2, and B represents O, S, carbonyl, etc., when Y is C=, then m represents 1, n represents 1 or 2, and B represents (i) (wherein the double bond is bound to Y, and R6 represents optionally substituted aryl, etc.), and when Y is N, then m represents O or 1, n represents 2 or 3, and B represents carbonyl, sulbonyl, etc.; E1 and E2 represent each H or lower alkyl; and D represents an aromatic hydrocarbon group, aromatic heterocyclic group, etc. The benzothiazine derivatives and salts thereof have a potent serotonin 2 blocker activity and an excellent alpha 1 blocker activity selectivity and are highly safe, thus providing drugs utilizing a serotonin 2 receptor antagonism, for example, remedies for circulatory diseases such as ischemic heart diseases, cerebrovascular diseases and peripheral circulation disorder.
摘要翻译：由通式（I）表示的苯并噻嗪衍生物或其盐，其中虚线表示存在或不存在键; Z代表（a），（b），（c），（d），（e），（f），（g）和（h）（其中R1表示烷基，芳烷基等; R2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分别表示O或S; G表示任选取代的亚乙基，三亚甲基等）; A代表亚烷基，亚烯基等; Y表示CH，C =或N，当Y为CH时，m表示0或1，n表示1或2，B表示O，S，羰基等，Y为C = m时，m表示1 ，n表示1或2，B表示（i）（其中双键与Y结合，R6表示任选取代的芳基等），当Y为N时，m表示0或1，n表示2 或3，B表示羰基，磺基等; E1和E2表示每个H或低级烷基; 苯并噻嗪衍生物及其盐具有有效的5-羟色胺2阻断剂活性和优异的α1阻断剂活性选择性，并且是高度安全的，因此提供利用5-羟色胺2受体拮抗作用的药物，例如，循环系统疾病如缺血性心脏病，脑血管疾病和外周循环障碍的补救措施。

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