专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

61. 发明申请

WO1996016051A1 HYPOLIPIDEMIC BENZOTHIAZEPINES 审中-公开
标题翻译：高血压BENZOTHIAZEPINES
公开(公告)号：WO1996016051A1
公开(公告)日：1996-05-30
申请号：PCT/GB1995002700
申请日：1995-11-16
申请人： THE WELLCOME FOUNDATION LIMITED , BRIEADDY, Lawrence, Edward , HANDLON, Anthony, Louis , HODGSON, Gordon, Lewis, Jr.
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D281/10
CPC分类号： C07F9/6536 , C07D281/10
摘要： The invention is concerned with novel hypolipidemic compounds of formula (I), with processes and novel intermediates for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, and associated diseases such as atherosclerosis.
摘要翻译：本发明涉及式（I）的新型降血脂化合物，其制备方法和新中间体，含有它们的药物组合物及其在医药中的用途，特别是用于预防和治疗高脂血症和相关疾病如动脉粥样硬化。

62. 发明申请

WO1994018183A1 HYPOLIPIDAEMIC CONDENSED 1,4-THIAZEPINES 审中-公开
标题翻译：高分子浓缩的1,4-二氧杂环己烷
公开(公告)号：WO1994018183A1
公开(公告)日：1994-08-18
申请号：PCT/GB1994000299
申请日：1994-02-15
申请人： THE WELLCOME FOUNDATION LIMITED , BRIEADDY, Lawrence, Edward , HODGSON, Gordon, Lewis, Jr.
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D281/10
CPC分类号： C07D417/04 , C07D281/08 , C07D281/10 , C07D513/04
摘要： The invention provides a compound of formula (I), wherein n is an integer of from 0 to 2; R is an optional substituent; R is hydrogen or C1-6alkyl; R is an atom or group selected from hydrogen, C1-6alkyl (including cycloalkyl and cycloalkylalkyl), C1-4alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R is hydrogen, OH, C1-6alkyl, C1-6alkoxy or -OC1-6acyl; R is a group independently selected from C1-6alkyl (including cycloalkyl and cycloalkylalkyl), C2-6alkenyl, and C2-6alkynyl which groups are optionally substituted; R is a group independently selected from C2-6alkyl (including cycloalkyl and cycloalkylalkyl), C2-6alkenyl and C2-6alkynyl, which groups are optionally substituted; or R and R , together with the carbon atom to which they are attached, form a C3-7spiro cycloalkyl group which is optionally substituted; R and R are independently selected from hydrogen and C1-6alkyl; and X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein optionally one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; or X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; and salts, solvates and physiologically functional derivatives thereof, pharmaceutical formulations comprising such compounds, processes for their preparation and their use in reducing bile acid uptake and hence as hypolipidaemic compounds.
摘要翻译：本发明提供式（I）化合物，其中n为0-2的整数; R是任选的取代基; R 1是氢或C 1-6烷基; R 2是选自氢，C 1-6烷基（包括环烷基和环烷基烷基），C 1-4烷氧基，吡咯基，噻吩基，吡啶基，1,3-苯并二氧杂环戊烯，苯基和萘基的原子或基团，这些基团任选被取代; R 3是氢，OH，C 1-6烷基，C 1-6烷氧基或-OC 1-6苯基; R 4是独立地选自C 1-6烷基（包括环烷基和环烷基烷基），C 2-6烯基和任选被取代的C 2-6炔基的基团; R 5是独立地选自C 2-6烷基（包括环烷基和环烷基烷基），C 2-6烯基和C 2-6炔基的基团，该基团任选被取代; 或R 4和R 5与它们所连接的碳原子一起形成任选取代的C 3-7螺环烷基; R 6和R 7独立地选自氢和C 1-6烷基; 并且X是具有5至10个碳原子（包括形成硫杂环的一部分的两个碳原子）的芳族或非芳族单环或双环体系，其中任选地一个或多个碳原子被杂原子代替（ s）独立地选自氮，氧和硫; 或X是具有5至10个碳原子（包括形成硫杂环的一部分的两个碳原子）的芳族或非芳族单环或双环体系，其中一个或多个碳原子被杂原子）独立地选自氮，氧和硫; 及其盐，溶剂化物和生理功能衍生物，包含这些化合物的药物制剂，其制备方法及其在减少胆汁酸摄取中的用途，因此作为降血脂化合物。

63. 发明申请

WO1994001421A1 BENZOTHIAZEPINE AND BENZOXAZEPINE DERIVATIVES AS CHOLECYSTOKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯并吖嗪和苯并吖庚因衍生物作为选择素受体拮抗剂
公开(公告)号：WO1994001421A1
公开(公告)日：1994-01-20
申请号：PCT/US1993003389
申请日：1993-04-14
申请人： PFIZER INC. , NAGEL, Arthur, A.
发明人： PFIZER INC.
IPC分类号： C07D267/14
CPC分类号： C07D281/10 , C07D267/14
摘要： The present invention relates to novel substituted benzothiazepines and benzoxazepines of formula (I), wherein R1, R2, R7, R8, R9 and X are as defined below, and to novel intermediates used in the synthesis of such compounds. Such compounds are useful in the treatment and prevention of gastrointestinal disorders, pain and anxiety disorders.
摘要翻译：本发明涉及式（I）的新的取代的苯并硫氮杂和苯并氧氮杂，其中R 1，R 2，R 7，R 8，R 9和X如下所定义，以及用于合成这些化合物的新中间体。这些化合物可用于治疗和预防胃肠疾病，疼痛和焦虑症。

64. 发明申请

WO1992021668A1 BENZOTHIAZEPINONES AND THEIR USE AS ANTICONVULSANTS 审中-公开
标题翻译：苯并噻唑类及其作为抗生素使用
公开(公告)号：WO1992021668A1
公开(公告)日：1992-12-10
申请号：PCT/EP1992001221
申请日：1992-05-25
申请人： THE BOOTS COMPANY PLC , BUCKETT, William, Roger , HARRIS, Paul, John , HOUSLEY, John, Rosindale , JEFFERY, James, Edward , NICHOL, Kenneth, John , FERNANDEZ NAVARRO, Enriqueta
发明人： THE BOOTS COMPANY PLC
IPC分类号： C07D281/10
CPC分类号： C07D281/10
摘要： Compounds of formula (I) in which n = 0, 1 or 2; R1 independently represents halo, alkyl of 1 to 4 carbon atoms or alkoxy, haloalkyl of 1 to 4 carbon atoms, nitro, cyano, carboxy, alkanoyl of 1 to 4 carbon atoms, optionally alkylated carbamoyl or optionally alkylated sulphamoyl; R2, R3, R4, R5 and R6 independently represent hydrogen or alkyl of 1 to 4 carbon atoms; and m = 0 or an integer from 1 to 4 have utility as anticonvulsants in the treatment of neurological disorders such as epilepsy.
摘要翻译：其中n = 0,1或2的式（I）化合物; R1独立地表示卤素，1至4个碳原子的烷基或烷氧基，1至4个碳原子的卤代烷基，硝基，氰基，羧基，1至4个碳原子的烷酰基，任选烷基化的氨基甲酰基或任选烷基化的氨磺酰基; R2，R3，R4，R5和R6独立地表示氢或1-4个碳原子的烷基; 并且m = 0或1至4的整数在治疗诸如癫痫的神经障碍中具有用作抗惊厥药。

65. 发明申请

WO1991017153A1 1,5-BENZOTHIAZEPINONE DERIVATIVES, THEIR PREPARATIONS AND PHARMACEUTICAL USE 审中-公开
标题翻译： 1,5-BENZOTHIAZEPINONE衍生物，其制备和药物使用
公开(公告)号：WO1991017153A1
公开(公告)日：1991-11-14
申请号：PCT/EP1991000742
申请日：1991-04-18
申请人： ISTITUTO LUSO FARMACO D'ITALIA S.P.A. , SALIMBENI, Aldo , CALIARI, Saturnino , FICI, Francesco , MANGHISI, Elso
发明人： ISTITUTO LUSO FARMACO D'ITALIA S.P.A.
IPC分类号： C07D281/10
CPC分类号： C07D281/10
摘要： The invention relates to compounds of general formula (I) and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and pharmaceutical compositions containing them. The new compounds, characterized by the presence on the basic nitrogen of at least a branched or cyclic alkyl group and/or by a substitution in the alkyl chain, are endowed with good calcium antagonistic properties and with a longer duration of action in comparison with diltiazem. Said compounds can be usefully utilized in several vascular pathologies such as hypertension and ischemic cardiopathy.
摘要翻译：本发明涉及通式（I）的化合物及其药学上可接受的盐，其制备方法和含有它们的药物组合物。特征在于在碱性氮上存在至少一个支链或环状烷基和/或通过在烷基链中取代的新化合物具有良好的钙拮抗性质，与地尔硫卓相比具有更长的作用持续时间。所述化合物可用于几种血管病变如高血压和缺血性心脏病。

66. 发明申请

WO1991005549A1 BENZOHETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：苯甲酮化合物
公开(公告)号：WO1991005549A1
公开(公告)日：1991-05-02
申请号：PCT/JP1990001340
申请日：1990-10-18
申请人： OTSUKA PHARMACEUTICAL COMPANY, LIMITED , OGAWA, Hidenori , MIYAMOTO, Hisashi , KONDO, Kazumi , YAMASHITA, Hiroshi , NAKAYA, Kenji , KOMATSU, Hajime , TANAKA, Michinori , KORA, Shinya , TOMINAGA, Michiaki , YABUUCHI, Yoichi
发明人： OTSUKA PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： A61K31/00
CPC分类号： C07D215/233 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D215/42 , C07D215/54 , C07D223/16 , C07D225/06 , C07D241/42 , C07D243/12 , C07D243/14 , C07D265/36 , C07D267/14 , C07D279/16 , C07D281/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/10
摘要： Novel benzoheterocyclic compounds of formula (I), wherein R is H, halogen, alkyl, optionally substituted amino, alkoxy; R is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R is a group: -NR R or -CO-NR R ; R is H, optionally substituted benzoyl, alkyl; R is a group alpha [R is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: -O-A-NR R ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenyl-alkanoyl, etc.; R is H or alkyl; R is cycloalkyl or optionally substituted phenyl; and W is a group: -(CH2)p (p is 3 to 5) or -CH=CH-(CH2)q (q is 1 to 3), the carbon atom of these groups being optionally replaced by 0, S, SO, SO2 or a group: -N(R )- and further these groups having optionally 1 to 3 substituents of alkyl, alkoxycarbonyl, carboxy, OH, O, alkanoyloxy, etc., which have excellent vasopressin antagonistic activies and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
摘要翻译：式（I）的新型苯并杂环化合物，其中R 1是H，卤素，烷基，任选取代的氨基，烷氧基; R 2是H，卤素，烷氧基，苯基烷氧基，OH，烷基，任选取代的氨基，氨基甲酰基 - 烷氧基，任选取代的氨基 - 烷氧基，任选取代的苯甲酰氧基; R 3是基团-NR 4 R 5或-CO-NR 11 R 12; R 4是H，任选取代的苯甲酰基，烷基; R 5是α基团[R 16是卤素，任选取代的烷基，OH，烷氧基，烷酰氧基，烷硫基，烷酰基，羧基，烷氧基羰基，CN，NO 2，任选取代的氨基，苯基，环烷基等，或一个基团：-OA-NR 6 R 7; m为0〜3]，苯基 - 烷氧基羰基，烷酰基，苯基 - 烷酰基等; R 11是H或烷基; R 12是环烷基或任选取代的苯基; 并且W是： - （CH 2）p（p为3至5）或-CH = CH-（CH 2）q（q为1至3），这些基团的碳原子任选被0，S， SO，SO 2或基团-N（R 13） - 并且这些基团具有任选1至3个烷基，烷氧基羰基，羧基，OH，O，烷酰氧基等的取代基，其具有优异的加压素拮抗活性，可用作血管扩张剂，降血压剂，水利尿剂，血小板凝集抑制剂和含有该化合物作为活性成分的血管加压素拮抗剂组合物。

67. 发明申请

WO2016064082A2 NOVEL AMINOALKYL BENZOTHIAZEPINE DERIVATIVE AND USE THEREOF 审中-公开
标题翻译：新型氨基烷基苯并噻嗪衍生物及其用途
公开(公告)号：WO2016064082A2
公开(公告)日：2016-04-28
申请号：PCT/KR2015009044
申请日：2015-08-28
申请人： CJ HEALTHCARE CORP
发明人： JUNG WON HYUK , KIM SEUNG IN , JI SEUNG HEE , KO DONG HYUN , SONG SEOG BEOM , LEE KEUN HO , JUN HYUNG JIN , KIM DONG KYU , KIM DONG HYUN
IPC分类号： C07D281/10 , A61K31/554 , A61P1/00 , C07D281/08
CPC分类号： A61K31/554 , C07D281/08 , C07D281/10
摘要： The present invention relates to a novel aminoalkyl benzothiazepine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition, containing the same as an active ingredient, for preventing or treating constipation.
摘要翻译：本发明涉及一种新的氨基烷基苯并硫氮杂衍生物或其药学上可接受的盐以及含有该化合物作为活性成分用于预防或治疗便秘的药物组合物。

68. 发明申请

WO2014144650A9 BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF PRIMARY SCLEROSING CHOLANGITIS AND INFLAMMATORY BOWEL DISEASE 审中-公开
标题翻译：胆汁酸循环抑制剂治疗原发性硬化性胆管炎和炎性肠病
公开(公告)号：WO2014144650A9
公开(公告)日：2014-11-27
申请号：PCT/US2014029151
申请日：2014-03-14
申请人： LUMENA PHARMACEUTICALS INC
发明人： GEDULIN BRONISLAVA , GREY MICHAEL , O'DONNELL NIALL , KELLER BRADLEY T
CPC分类号： C07D487/08 , A61K9/0019 , A61K9/0056 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K31/155 , A61K31/38 , A61K31/46 , A61K31/554 , A61K31/7042 , C07C279/12 , C07D207/09 , C07D249/14 , C07D281/10 , C07D295/15 , C07D337/08 , C07D409/10
摘要： Provided herein are methods of treating or ameliorating primary sclerosing cholangitis and inflammatory bowel disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating primary sclerosing cholangitis comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
摘要翻译：本文提供了通过向有需要的个体施用治疗有效量的根尖钠依赖性胆汁酸转运蛋白抑制剂（ASBTI）或其药学上可接受的盐来治疗或改善原发性硬化性胆管炎和炎性肠病的方法。还提供了用于治疗或改善原发性硬化性胆管炎的方法，其包括向有需要的个体施用治疗有效量的ASBTI或其药学上可接受的盐。

69. 发明申请

WO2009032286A2 OLIGOMER-CALCIUM CHANNEL BLOCKER CONJUGATES 审中-公开
标题翻译： OLIGOMER-CALCIUM通道阻塞器
公开(公告)号：WO2009032286A2
公开(公告)日：2009-03-12
申请号：PCT/US2008010385
申请日：2008-09-03
申请人： NEKTAR THERAPEUTICS AL CORP , REN ZHONGXU , DENG BO-LIANG , RIGGS-SAUTHIER JENNIFER , HARVEY MICAH
发明人： REN ZHONGXU , DENG BO-LIANG , RIGGS-SAUTHIER JENNIFER , HARVEY MICAH
CPC分类号： A61K31/4422 , A61K31/4418 , A61K47/48215 , A61K47/60 , C07C255/43 , C07D211/90 , C07D281/10 , C07D413/04 , C07D417/04
摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
摘要翻译：本发明提供通过共价连接水溶性低聚物进行化学修饰的小分子药物。本发明的缀合物当通过多种施用途径中的任一种施用时，显示出与未附着于水溶性低聚物的小分子药物的特征不同的特征。

70. 发明申请

WO2009026444A1 RYANODINE CHANNEL BINDERS AND USES THEREOF 审中-公开
标题翻译： RYANODINE CHANNEL BINDERS及其用途
公开(公告)号：WO2009026444A1
公开(公告)日：2009-02-26
申请号：PCT/US2008/073871
申请日：2008-08-21
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , COREY, Elias, James
发明人： COREY, Elias, James
IPC分类号： A61K31/00
CPC分类号： C07D417/06 , C07D281/10 , C07D337/08 , C07D409/06 , C07D413/06
摘要： Increasing the affinity of calstabin-2 for the cardiac calcium channel RyR2 and thereby stabilizing the channel in the closed state has recently been identified as as novel mechanism for treating heart failure, particularly ventricular arrhythmias. JTV-519, a 1,4- benzothiazepine derivative, has been shown to stabilize the calstabin2/RyR2 complex. Novel derivatives of JTV-519 that may be useful in treatment or prevention of heart failure, atrial fibrillation, or exericse-induced cardiac arrhythmias are provided. Synthetic methodology and intermediates in the synthesis of the inventive JTV-519 derivatives are also described.
摘要翻译：最近已经将钙调蛋白-2的心肌钙通道RyR2的亲和力提高到闭合状态，从而使通道稳定化，作为治疗心力衰竭，特别是室性心律失常的新型机制。已证明JTV-519是1,4-苯并硫氮杂衍生物，稳定了calstabin2 / RyR2复合物。提供了可用于治疗或预防心力衰竭，心房颤动或心律失常心律失常的JTV-519的新型衍生物。还描述了合成方法和合成本发明JTV-519衍生物的中间体。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式