-
公开(公告)号：US4595757A
公开(公告)日：1986-06-17
申请号：US681169
申请日：1984-12-13
IPC分类号： C07D275/06 , C07D295/096 , C07D317/58 , C07D513/04 , C07D405/12 , C07D417/12
CPC分类号： C07D275/06 , C07D295/096 , C07D317/58 , C07D513/04
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is ##STR2## wherein B is a moiety having the formula ##STR3## R is H, mono- or dihalo, amino, nitro, cyano, hydroxy, trifuoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, lowercycloalkyl, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, loweralkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro;X is SO.sub.2, SO, S or C.dbd.O; andR.sup.2 is phenyl or 1,3-benzodioxol-5-yl;and the pharmacologically acceptable salts thereof, which are (H.sup.+ +K.sup.+)ATPase inhibitors exhibiting a cytoprotective action, are useful in the treatment of conditions where there is hypersecretion of gastric acid, such as gastric and peptic ulceration, as well as in conditions such as stress ulceration.
摘要翻译： 其中R 1是其中B是具有式R 1的部分的式的化合物是H，单或二卤代，氨基，硝基，氰基，羟基，三氟甲基，巯基，低级烷基，低级烷氧基 ，烷酰基，低级环烷基，羧基，烷氧基羰基，一或二低级烷基取代的氨基，烷酰基氨基，低级烷基硫代，低级烷基磺酰基，氨磺酰基，低级烷基取代的氨磺酰基，苯基或被卤素，低级烷氧基，三氟甲基，羟基 ，氨基，氰基或硝基; X是SO 2，SO，S或C = O; 并且R 2是苯基或1,3-苯并间二氧杂环戊烯-5-基; 和其药理学上可接受的盐，其是表现出细胞保护作用的（H ++ K +）ATP酶抑制剂，可用于治疗胃酸过多分泌的病症，例如胃和消化性溃疡，以及在这些病症 作为应激性溃疡。
-
公开(公告)号：US4461901A
公开(公告)日：1984-07-24
申请号：US472404
申请日：1983-03-04
IPC分类号： C07D213/73 , C07D275/06 , C07D417/12
CPC分类号： C07D213/73 , C07D275/06 , C07D417/12 , Y10S514/927
摘要： Compounds of the formula: ##STR1## wherein X is SO.sub.2, SO or S; andA is an amine selected from the group: ##STR2## wherein R is hydrogen, (lower)alkyl, (lower)alkoxy or halo; n is 2-4; andthe pharmacologically acceptable salts thereof are disclosed.
摘要翻译： 下式的化合物：其中X是SO 2，SO或S; 并且A是选自以下的胺：其中R是氢，（低级）烷基，（低级）烷氧基或卤素; n为2-4; 并公开了其药理学上可接受的盐。
-
3.发明授权
公开(公告)号：US4743692A
公开(公告)日：1988-05-10
申请号：US913876
申请日：1986-09-30
IPC分类号： C07D417/12 , C07D513/04
CPC分类号： C07D417/12 , C07D513/04
摘要： A compound of the formula: ##STR1## in which A is a 3,4-; 3,2-; or 2,3-fused thieno- moiety or a benzo- moiety;X is alkylene of 2 to 5 carbon atoms;R.sup.1 is hydrogen, bromo or methyl;R.sup.2 is methoxy when R.sup.1 is hydrogen, methyl when R.sup.1 is bromo, and bromo when R.sup.1 is methyl;R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sup.3 and R.sup.4, taken together, are ethylene when X is ethylene;R.sup.5 is hydrogen when A is thieno, and when A is benzo, R.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, halo or alkoxy of 1 to 6 carbon atoms;R.sup.6 is hydrogen when A is thieno, and when A is benzo, R.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, halo, alkoxy of 1 to 6 carbon atoms, amino, nitro, sulfamoyl or pyridinyl;m is one of the integers 0 or 1;n is one of the integers 3, 4 or 5;p is one of the integers 0, 1 or 2; andthe dotted line in the thiazole ring represents unsaturation necessary to complete the 3,2- or 2,3- thieno- ring;or a pharmaceutically acceptable salt thereof are histamine H.sub.1 -antagonists useful in the treatment of various allergic reactions in the mammal.
摘要翻译： 下式的化合物：其中A是3,4-; 3,2; 或2,3-稠合的噻吩并 - 部分或苯并 - 部分; X是2至5个碳原子的亚烷基; R1是氢，溴或甲基; 当R 1为氢时，R 2为甲氧基，当R 1为溴时，R 2为甲基; R3是氢或1至6个碳原子的烷基; R4是氢或1至6个碳原子的烷基; 当X是亚乙基时，R 3和R 4一起是乙烯; 当A为噻吩并且当A为苯甲基时，R 5为氢，R 5为氢，1至6个碳原子的烷基，卤素或1至6个碳原子的烷氧基; 当A为噻吩并且当A为苯甲基时，R 6为氢，R 5为氢，1至6个碳原子的烷基，卤素，1至6个碳原子的烷氧基，氨基，硝基，氨磺酰基或吡啶基; m是整数0或1之一; n是整数3,4或5之一; p是整数0,1或2之一; 并且噻唑环中的虚线表示完成3,2-或2,3-噻吩环所必需的不饱和键; 或其药学上可接受的盐是用于治疗哺乳动物各种过敏反应的组胺H1拮抗剂。
-
公开(公告)号：US4788306A
公开(公告)日：1988-11-29
申请号：US88189
申请日：1987-08-21
申请人： Guy A. Schiehser , Donald P. Strike
发明人： Guy A. Schiehser , Donald P. Strike
IPC分类号： C07D303/48
CPC分类号： C07D303/48 , Y10S514/884
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, hydroxy, lower alkyl, lower alkoxy, haloloweralkyl, haloloweralkyl sulfonyl, halo or nitro;R.sup.3 is hydrogen, lower alkyl, or aryl of 7-12 carbon atoms; ##STR2## A is --CH.sub.2 --, --O-- or --S--; m is 1-8;n is 0-7, with the proviso that m+n.ltoreq.8;or a pharmacologically acceptable salt thereof, and their use as fatty acid oxidation inhibitors possessing a significantly reduced potential for impairment of normal cardiac function, and having particular utility in the treatment of glucose and fatty acid metabolism disorders, such as diabetes.
摘要翻译： 公开了式IMA的化合物，其中R 1和R 2各自独立地为氢，羟基，低级烷基，低级烷氧基，卤代低级烷基，卤代低级烷基磺酰基，卤素或硝基。 R3是7-12个碳原子的氢，低级烷基或芳基; A是-CH 2 - ， - O-或-S-; m为1-8; n为0-7，条件是m + n = 8; 或其药理学上可接受的盐，以及它们作为脂肪酸氧化抑制剂的用途，其具有显着降低正常心脏功能损害的潜力，并且在治疗葡萄糖和脂肪酸代谢障碍如糖尿病中具有特别的用途。
-
公开(公告)号：US4587345A
公开(公告)日：1986-05-06
申请号：US655978
申请日：1984-09-28
申请人： Guy A. Schiehser , Donald P. Strike
发明人： Guy A. Schiehser , Donald P. Strike
IPC分类号： C07D513/04 , C07D333/34
CPC分类号： C07D513/04
摘要： A process for preparing certain thieno-fused heterocyclic compounds having H.sub.2 -receptor antagonist and antisecretory activity, which comprises reacting a suitable thienoisothiazole derivative with an appropriate (furanylmethylthio)ethanamine derivative to yield an intermediate, which is subjected to cyclization to yield the desired final product.
摘要翻译： 一种制备具有H 2受体拮抗剂和抗分泌活性的某些噻吩并杂的杂环化合物的方法，其包括使合适的噻吩异噻唑衍生物与适当的（呋喃基甲硫基）乙胺衍生物反应，得到中间体，其经受环化以产生所需的最终产物 。
-
公开(公告)号：US4490527A
公开(公告)日：1984-12-25
申请号：US468221
申请日：1983-02-22
申请人： Guy A. Schiehser , Donald P. Strike
发明人： Guy A. Schiehser , Donald P. Strike
IPC分类号： C07D209/46 , C07D209/48 , C07D209/50 , C07D275/06 , C07D277/04 , C07D295/096 , C07D307/52 , C07D417/12 , C07D495/04 , C07D513/04 , C07D279/12
CPC分类号： C07D209/48 , C07D209/46 , C07D209/50 , C07D275/06 , C07D277/04 , C07D295/096 , C07D307/52 , C07D417/12 , C07D495/04 , C07D513/04
摘要： Compounds of the formula: ##STR1## wherein B is a moiety having the formula: ##STR2## R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, cycloalkyl of 4-7 carbon atoms, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, lower alkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro.X is SO.sub.2, SO, S or C.dbd.O; andA is amine selected from the group ##STR3## , wherein R.sup.1 is hydrogen or R.sup.2 CH.sub.2 wherein R.sup.2 is mono- or diloweralkylamino, mono- or di-N-lower alkylaminoloweralkyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl; R.sup.3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R.sup.3 is (1-piperidinyl)methyl, R.sup.1 is hydrogen; n is 1 to 4, and the pharmacologically acceptable salts thereof.
摘要翻译： 其中B是下式的部分：其中B是具有下式的部分：R 1是单 - 或二卤代，氨基，硝基，氰基，羟基，三氟甲基，巯基，低级烷基，低级烷氧基， 烷酰基，4-7个碳原子的环烷基，羧基，烷氧基羰基，一或二低级烷基取代的氨基，烷酰基氨基，低级烷基硫代，低级烷基磺酰基，氨磺酰基，低级烷基取代的氨磺酰基，苯基或被卤素取代的苯基，低级烷基， 低级烷氧基，三氟甲基，羟基，氨基，氰基或硝基。 X是SO 2，SO，S或C = O; 并且A是选自其中n = 1-4的基团
或 ，其中R1是氢或R2CH2，其中R2是单或二低级烷基氨基，单或二-N-低级烷基氨基低级烷基， （2-呋喃基）甲基氨基，苄基氨基，低级环烷基氨基，1-吡咯烷基，1-哌啶基，1-六氢氮杂基，1-八氢吖嗪基，3-噻唑烷基，4-吗啉基或4-硫代吗啉基; R 3是氢或（1-哌啶基）甲基，条件是当R 3是（1-哌啶基）甲基时，R 1是氢; n为1〜4，及其药理学上可接受的盐。 -
7.发明授权Process for preparing thieno-fused heterocyclic anti-ulcer agents and intermediates therefor 失效噻吩并稠合的杂环抗溃疡剂及其中间体的制备方法
公开(公告)号：US4622402A
公开(公告)日：1986-11-11
申请号：US767558
申请日：1985-08-20
申请人： Guy A. Schiehser , Donald P. Strike
发明人： Guy A. Schiehser , Donald P. Strike
IPC分类号： C07D513/04 , C07D519/00 , C07D275/00
CPC分类号： C07D513/04
摘要： A process for preparing certain thieno-fused heterocyclic compounds having H.sub.2 -receptor antagonist and antisecretory activity, which involves the reaction of a mercaptan, obtained by reduction of a thienoisothiazole amino alkyl disulfide, with a 5-substituted-2-furanylmethanol; and said thienoisothiazole amino alkyl disulfide intermediates.
摘要翻译： 制备具有H 2受体拮抗剂和抗分泌活性的某些噻吩并杂的杂环化合物的方法，其涉及通过还原噻吩异噻唑氨基烷基二硫化物得到的硫醇与5-取代-2-呋喃基甲醇的反应; 并称噻吩异噻唑氨基烷基二硫化物中间体。
-
公开(公告)号：US5491231A
公开(公告)日：1996-02-13
申请号：US345972
申请日：1994-11-28
IPC分类号： A61K31/435 , A61P9/00 , A61P29/00 , A61P31/04 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/395 , C07D491/06
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, ##STR2## or hydrogen; R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl , or R.sup.2 and R.sup.3 may be taken together to form a cycloalkyl ring;R.sup.4 is a heterocyclic N-oxide radical, which may be optionally substituted;R.sup.5 is alkyl or arylalkyl;R.sup.6 and R.sup.7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted;k=0-1,m=0-1;n=1-6;with the proviso that R and R.sup.1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构
的化合物，其中R和R 1各自独立地是氢或氢; R 2和R 3各自独立地为烷基，芳基烷基，或者R 2和R 3可以一起形成环烷基环; R4是杂环N-氧化物基团，其可任选被取代; R5是烷基或芳基烷基; R 6和R 7一起形成饱和的N-烷基 - 杂环N-氧化物，其可任选被取代; k = 0-1，m = 0-1; n = 1-6; 条件是R和R 1不是氢，它们可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。 -
公开(公告)号：US5362718A
公开(公告)日：1994-11-08
申请号：US229261
申请日：1994-04-18
IPC分类号： C07D487/18 , A61K31/00 , A61K31/435 , A61K31/436 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/695 , A61K31/395 , C07D498/16 , C07D7/04
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CO(CR.sup.3 R.sup.4).sub.b (CR.sup.5 R.sup.6).sub.d CR.sup.7 R.sup.8 R.sup.9 ;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or --F;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11, or R.sup.5 and R.sup.6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3 R.sup.4).sub.f 0R.sup.10 ;R.sup.7 is hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11 ;R.sup.8 and R.sup.9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11, or R.sup.8 and R.sup.9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3 R.sup.4).sub.f OR.sup.10 ;R.sup.10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl;R.sup.11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl;X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl;b=0-6;d=0-6; andf=0-6with the proviso that R.sup.1 and R.sup.2 are both not hydrogen and further provided that either R.sup.1 or R.sup.2 contains at least one --(CR.sup.3 R.sup.4).sub.f OR.sup.10, X, or --(CR.sup.3 R.sup.4).sub.f OR.sup.10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 其中R 1和R 2各自独立地是氢或-CO（CR 3 R 4）b（CR 5 R 6）d CR 7 R 8 R 9的结构化合物
R 3和R 4各自独立地为氢，烷基，烯基，炔基，三氟甲基或-F; R 5和R 6各自独立地为氢，烷基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11，或者R 5和R 6可以一起形成X或环烷基环， 用 - （CR 3 R 4）f O R 10单取代，二取代或三取代; R 7是氢，烷基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11; R 8和R 9各自独立地为氢，烷基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11，或者R 8和R 9可以一起形成X或环烷基环， 用 - （CR 3 R 4）fOR 10单取代，二取代或三取代; R 10是氢，烷基，烯基，炔基，三（烷基）甲硅烷基，三（烷基）甲硅烷基乙基，三苯甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基，氯乙基或四氢吡喃基; R11是氢，烷基，烯基，炔基或苯基烷基; X是5-（2,2-二烷基）[1,3]二烷基，5-（2,2-二环烷基）[1,3]二氧杂环己基，4-（2,2-二烷基）[1,3] 4-（2,2-二环烷基）[1,3]二烷基，4-（2,2-二烷基）[1,3]二氧戊环基或4-（2,2-二环烷基）[1,3]二氧戊环基; b = 0-6; d = 0-6; 并且f = 0-6，条件是R 1和R 2都不是氢，并且进一步规定R1或R2含有至少一个 - （CR 3 R 4）fOR 10，X或 - （CR 3 R 4）fOR 10取代的环烷基，或药学上 其可接受的盐可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。 -
公开(公告)号：US4933365A
公开(公告)日：1990-06-12
申请号：US301937
申请日：1989-01-25
IPC分类号： A61K31/335
CPC分类号： A61K31/335
摘要： There is disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals which comprises administering to a mammal so afflicated an effective amount of a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, hydroxy, lower alkyl, lower alkoxy, haloloweralkyl, haloloweralkyl sulfonyl, halo or nitro;R.sup.3 is hydrogen, lower alkyl, or aryl of 7-12 carbon atoms;X is ##STR2## A is --CH.sub.2 --, --O-- or --S--; m is 0-8;n is 0-7, with the proviso that m+n.ltoreq.8;or a pharmacologically acceptable salt thereof.
摘要翻译： 公开了一种用于治疗哺乳动物的免疫炎症状况，如过敏，过敏反应，哮喘和炎症的方法，其包括向受影响的哺乳动物施用有效量的具有下式的化合物：其中R1和R2各自为 独立地是氢，羟基，低级烷基，低级烷氧基，卤代低级烷基，卤代烷基磺酰基，卤素或硝基; R3是7-12个碳原子的氢，低级烷基或芳基; X是-CH 2 - ， - O-或-S-; m为0-8; n为0-7，条件是m + n = 8; 或其药理学上可接受的盐。
-
-
-
-
-
-
-
-
-
搜索结果
35 条记录 (耗时 0.022 秒)
