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51. 发明授权

US5219871A Muscarinic receptor antagonists 失效
标题翻译：肌肉受体拮抗剂
公开(公告)号：US5219871A
公开(公告)日：1993-06-15
申请号：US416894
申请日：1989-10-04
申请人： Peter E. Cross , Alexander R. MacKenzie
发明人： Peter E. Cross , Alexander R. MacKenzie
IPC分类号： A61K31/00 , A61K31/335 , A61K31/34 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P25/02 , C07C237/20 , C07C237/24 , C07C255/42 , C07C255/47 , C07C255/58 , C07C311/08 , C07C311/29 , C07C311/39 , C07C323/25 , C07C323/36 , C07C323/38 , C07C323/49 , C07C323/62 , C07C323/67 , C07D213/38 , C07D213/74 , C07D241/12 , C07D307/79 , C07D311/84 , C07D313/12 , C07D317/58 , C07D319/16 , C07D319/18 , C07D335/14 , C07D337/12
CPC分类号： C07D307/79 , C07C237/20 , C07C237/24 , C07C255/42 , C07C255/47 , C07C255/58 , C07C311/08 , C07D213/38 , C07D317/58 , C07D319/16 , C07C2102/08 , C07C2103/38
摘要： Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.

52. 发明授权

US5013756A Catechol derivatives, a process of preparation thereof, and therapeutical compositions containing the same 失效
标题翻译：儿茶酚衍生物，其制备方法和含有它们的治疗组合物
公开(公告)号：US5013756A
公开(公告)日：1991-05-07
申请号：US356568
申请日：1989-05-23
申请人： Michel Follet , Marc Bonato
发明人： Michel Follet , Marc Bonato
IPC分类号： C12N9/99 , A61K31/095 , A61K31/10 , A61K31/19 , A61K31/215 , A61K31/22 , A61K31/235 , A61K31/38 , A61K31/382 , A61K45/06 , A61P7/02 , A61P7/06 , A61P9/08 , A61P9/10 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C313/00 , C07C323/20 , C07C323/45 , C07C323/62 , C07D335/04 , C07D335/06 , C07D337/08 , C07D337/12 , C07D521/00
CPC分类号： C07D335/06 , A61K31/10 , C07C323/00 , C07D337/08
摘要： This invention relates to catechol derivatives having the general formula ##STR1## wherein R represents various substituents, to a process for the preparation of the same comprising reacting S-(3,4-dihydroxyphenyl)-isothiourea, which has the formula II, with a tosylate of the general formula III ##STR2## and to therapeutical compositions wherein the active ingredient is one of these compounds.

53. 发明授权

US4645758A Urinary incontinence ameliorating dibenz- b,e- -oxepin and -thiepin derivatives, compositions, and method of use therefor 失效
标题翻译：尿失禁改善二苯并b，e-氧化皮蛋白和硫蛋白衍生物，组合物及其使用方法
公开(公告)号：US4645758A
公开(公告)日：1987-02-24
申请号：US820428
申请日：1986-01-17
申请人： Nils-Erik Willman , Bengt C. H. Sjogren , Lennart G. Nordh , Gustav L. Persson , Goran H. Sjoholm
发明人： Nils-Erik Willman , Bengt C. H. Sjogren , Lennart G. Nordh , Gustav L. Persson , Goran H. Sjoholm
IPC分类号： C07D493/10 , A61K31/00 , A61K31/335 , A61K31/38 , A61P13/02 , A61P15/00 , C07D313/12 , C07D337/12 , C07D405/06 , C07D493/04 , C07D493/14 , C07D493/20 , C07D493/22 , C07D495/04 , C07D495/10 , C07D495/14 , C07D495/20 , C07D495/22 , C07D498/10 , C07D498/20 , C07D498/22 , A61K31/36
CPC分类号： C07D405/06 , C07D313/12 , C07D337/12
摘要： The invention concerns:Novel dibenz/b,e/oxepin and dibenz/b,e/thiepin compounds having the general formula: ##STR1## wherein X is O or S,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are each selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulponyl, halogen, trifluoromethyl, trifluoromethylthio, lower dialkylsulphonamido, nitro, hydroxy, cyano, carbamyl, carboxy, lower alkoxycarbonyl, amino, N-lower alkylamino, N,N-diloweralkylamino, lower acylamido, lower alkanesulfonamido and lower acyl and, when on adjacent carbon atoms at the positions 2 and 3 and/or 8 and 9, two of the substituents R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 taken together may form a methylenedioxy group;R.sup.5 and R.sup.6 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aralkyl, lower hydroxyalkyl, lower aminoalkyl, lower alkylaminoalkyl, lower dialkylaminoalkyl, lower alkoxyalkyl and together with the nitrogen atom, R.sup.5 and R.sup.6 may form a 5- or 6- membered ring, such as pyrrolidine, piperidine, morpholine, piperazine, and N-lower alkyl or N-hydroxy lower alkyl substituted rings such as N-alkylpiperazine or N-hydroxyalkyl piperazine or the like,R.sup.7 is hydrogen or lower alkyl; optionally in the form of addition salts with pharmaceutically acceptable inorganic or organic acids and optionally in the form of essentially pure enantiomers.The invention also includes compositions containing the novel compounds, processes for their preparation and a method of treatment therewith.The compounds have pharmacological effects.
摘要翻译：本发明涉及：具有以下通式的新型二苯并/ b，e /氧杂七环素和二苯并/ b，e /硫氮烯化合物：其中X为O或S，R 1，R 2，R 3和R 4的化合物相同或不同的并且各自选自氢，低级烷基，低级烯基，低级炔基，低级环烷基，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基亚磺酰基，卤素，三氟甲基，三氟甲硫基，低级二烷基磺酰胺基，硝基，羟基，氰基，氨基甲酰基，羧基，低级烷氧基羰基，氨基，N-低级烷基氨基，N，N-二低级烷基氨基，低级酰基酰氨基，低级链烷磺酰氨基和低级酰基，当在位置2和3和/或8和9相邻的碳原子上时，取代基R 1和R 2或R 3和R 4一起可以形成亚甲二氧基; R5和R6相同或不同，选自氢，低级烷基，低级烯基，低级炔基，低级环烷基，芳烷基，低级羟基烷基，低级氨基烷基，低级烷基氨基烷基，低级二烷基氨基烷基，低级烷氧基烷基，氮原子，R5和R6可以形成5-或6-元环，例如吡咯烷，哌啶，吗啉，哌嗪和N-低级烷基或N-羟基低级烷基取代的环，例如N-烷基哌嗪或N-羟基烷基哌嗪 R 7为氢或低级烷基; 任选地以与药学上可接受的无机酸或有机酸加成盐的形式，并且任选地以基本上纯的对映异构体的形式。本发明还包括含有新化合物的组合物，其制备方法及其处理方法。该化合物具有药理作用。

54. 发明授权

US4064141A Novel esters of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-alkanoic acids 失效
标题翻译：新的6,11-二氢二苯并 - {8e.e {9-硫杂-11-酮-3-链烷酸
公开(公告)号：US4064141A
公开(公告)日：1977-12-20
申请号：US706866
申请日：1976-07-19
申请人： Jack Ackrell
发明人： Jack Ackrell
IPC分类号： C07D337/12 , C07D411/12
CPC分类号： C07D337/12
摘要： Esters of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-ones of the formula: ##STR1## wherein R is hydrogen or methyl and R.sup.1 is --CH.sub.2 --CH(OH)--CH.sub.2 OH, ##STR2## where Y is either O or S, or ##STR3## where R.sup.2 and R.sup.3 are independently hydrogen, alkyl having 1 to 6 carbon atoms, phenyl or benzyl or together R.sup.2 and R.sup.3 form an alkylene bridge having 4, 5 or 6 carbon atoms, and processes for the production thereof.
摘要翻译： 6,11-二氢二苯并-β-thiepin-11-的下式：其中R是氢或甲基，R 1是-CH 2 -CH（OH）-CH 2 OH，其中 Y是O或S，或者其中R 2和R 3独立地是氢，具有1至6个碳原子的烷基，苯基或苄基，或者R 2和R 3一起形成具有4,5或6个碳原子的亚烷基桥，和用于生产。

55. 发明授权

US3752851A Anti diabetically active sulfonyl ureas and sulfonyl semicarbazides 失效
标题翻译：抗糖尿病活性硫磺和硫代半胱氨酸
公开(公告)号：US3752851A
公开(公告)日：1973-08-14
申请号：US3752851D
申请日：1971-09-21
申请人： BOEHRINGER MANNHEIM GMBH
发明人： STACH K , SCHMIDT F , WINTER W , FAULAND E , AUMUELLER W
IPC分类号： C07D209/86 , C07D295/28 , C07D311/82 , C07D313/12 , C07D335/02 , C07D337/12 , C07D337/16 , C07C127/00
CPC分类号： C07D295/32 , C07C2603/18 , C07D209/86 , C07D311/82 , C07D313/12 , C07D335/02 , C07D337/12 , C07D337/16 , Y10S514/866
摘要： NOVEL SULFONYL UREAS HAVING THE FORMULA:

X
NH-R2)-(R1-1,2-PHENYLENE)-)

WHEREIN X REPRESENTS OXYGEN, SULFUR, SATURATED, UNSATURATED, STRAIGHT OR BRANCHED CHAIN ALKYLENE CONTAINING UP TO 3 CARBON ATOMS, OXYMETHYLENE, THIAMETHYLENE, THIAETHYLENE, IMINOMETHYLENE, ALKYLATED IMINOMETHYLENE, ACYLATED IMINOMETHYLENE, CARBOXIMIDO, ALKYLATED CARBOXIMIDO, OR A VALENCY BOND, R1 IS HYDROGEN, HALOGEN, ALKYL, ALKOXY OR TRIFLUOROMETHYL, Y IS SATURATED, UNSATURATED, STRAIGHT OR BRANCHED CHAIN ALKYLENE CONTAINING UP TO 6 CARBON ATOMS OR SUCH ALKYLENE GROUP CONTAINING A NITROGEN OR OXYGEN ATOM, Z IS STRAIGHT OR BRANCHED CHAIN ALKYLENE CONTAINING UP TO 4 CARBON ATOMS AND R2 IS STRAIGHT OR BRANCHED CHAIN, SATURATED OR UNSATURATED ALKYL OR CYCLOALKYL, AND SUCH GROUPS INTERRUPTED BY OXYGEN OR SULFUR ATOMS OR CONTAINING AN ENDO-ALKYLENE GROUP AND SUBSTITUTED OR UBSUBSTITUTED ARYL OR ARALKYL. THE AFORESAID SULFONYL UREAS CONSTITUTE EXTREMELY EFFECTIVE ANTI-DIABETIC AGENTS.

56. 发明授权

US3716544A CERTAIN 6,11-DIHYDRO-11-(3-ALPHA-TROPANYLOXY)-DIBENZO[b,e]THIEPINE-5-OXIDES AND THE CORRESPONDING DIOXIDES AND DERIVATIVES THEREOF 失效
标题翻译：某些6,11-二氢-11-（3-羟基 - 戊二烯） - 二苯并[b，e]噻吩-5-氧化物及其相应的二氧化物及其衍生物
公开(公告)号：US3716544A
公开(公告)日：1973-02-13
申请号：US3716544D
申请日：1971-07-13
申请人： SANDOZ LTD
发明人： GADIENT F
IPC分类号： C07D337/12 , C07D451/06 , C07D43/06
CPC分类号： C07D451/06 , C07D337/12
摘要： WHEREIN R is alkyl of one to four carbon atoms and n is 1 or 2, or R is alkyl of two to four carbon atoms and n is 0, AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. The compounds are useful in the prophylaxis and treatment of gastric ulcers.

The invention concerns new dibenzothiepines of the formula:
摘要翻译：本发明涉及下式的新的二苯并噻吖庚因：

57. 发明授权

US3646009A Anti-diabetically active sulfonyl-semicarbazides 失效
标题翻译：抗糖尿病活性硫代半乳糖苷
公开(公告)号：US3646009A
公开(公告)日：1972-02-29
申请号：US3646009D
申请日：1968-03-11
申请人： BOEHRINGER & SOEHNE GMBH
发明人： WINTER WERNER , FAULAND ERICH , STACH KURT , SCHINIDT FELIX HELMUT , AUMULLER WALTER
IPC分类号： C07D209/86 , C07D295/28 , C07D311/82 , C07D313/12 , C07D335/02 , C07D337/12 , C07D337/16 , C07D29/12
CPC分类号： C07D295/32 , C07C2603/18 , C07D209/86 , C07D311/82 , C07D313/12 , C07D335/02 , C07D337/12 , C07D337/16 , Y10S514/866
摘要： NOVEL SULFONYL UREAS AND SULFONYL-SEMICARBAZIDES HAVING THE FORMULA:

1-((-1,2-PHENYLENE-X-(R1-1,2-PHENYLENE)-)>Y-CO-NH-Z-),

4-(R2-NH-CO-NH-SO2-)BENZENE

WHEREIN X REPRESENTS OXYGEN, SULFUR SATURATED, UNSTAURATED, STRAIGHT OR BRANCHED CHAIN ALKYLENE CONTAINING UP TO 3 CARBON ATOMS, OXYMETHYLENE, THIAMETHYLENE, THIAETHYLENE, IMINOMETHYLENE, ALKYLATED IMINOMETHYLENE, ACYLATED MINOMETHYLENE, CARBOXIMIDO, ALKYLATED CARBOXIMIDO, OR A VALENCY BOND, R1 IS HYDROGEN, HALOGEN ALKYL, ALKOXY OR TRIFLUOROMETHYL, Y IS SATURATED, UNSATURATED, STRAIGHT OR BRANCHED CHAIN ALKYLENE CONTAINING UP TO 6 CARBON ATOMS OR SUCH ALKYLENE GROUP CONTAINING A NITROGEN OR OXYGEN ATOM, Z IS STRAIGHT OR BRANCHED CHAIN ALKLYENE CONTAINING UP TO 4 CARBON ATOMS AND R2 IS STRAIGHT OR BRANCHED CHAIN, SATURATED OR UNSTAURATED ALKYL OR CYCLOALKYL, AND SUCH GROUPS INTERRUPTED BY OXYGEN OR SULFUR ATOMS OR CONTAINNG AN ENDO-ALKYLENE GROUP, SUBSTITUTED OR UNSUBSTITUTED ARYL OR ARALKYL OR SUBSTTITUTED, UNSUBSTITUTED, SATUATED OR UNSATURATED ALKYLENE-IMINO CONTAINING 3 TO 7 CARBON ATOMS OR SUCH ALKYLENE-IMINOI CONTAINING AN ENDO-ALKYLENE GROUP. THE AFORESAID SULFONYL UREAS AND SULFONYL-SEMICARAZIDES CONSTITUTE EXTREMELY EFFECTIVE ANTI-DIABETIC AGENTS.

58. 发明授权

US3639423A Tricyclic aminomethyl derivatives 失效
标题翻译：三聚氨基甲酸衍生物
公开(公告)号：US3639423A
公开(公告)日：1972-02-01
申请号：US3639423D
申请日：1967-12-11
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WINTER WERNER , THIEL MAX , STACH KURT , SCHAUMANN WOLFGANG , RIBBENTROP ANNEMARIE
IPC分类号： C07D313/12 , C07D337/12 , C07D337/16 , A61K27/00 , C07D9/00 , C07D65/16
CPC分类号： C07D337/12 , C03C2217/263 , C03C2218/15 , C07D313/12 , C07D337/16 , Y10S514/906
摘要： NOVEL COMPOUNDS POSSESSING VALUABLE PHARMACOLOGICAL PROPERTIES AND USEFUL AS MUSCLE RELAXANTS, TRANQUILIZING AGENTS, ANTI-CONVULSIVES, ETC. ARE DISCLOSED. THE COMPOUNDS ARE DEFINED BY THE FOLLOWING FORMULA:

1-R1,3,4-(-CH(-CH(-R2)-N(-R3)-R4)-(1,2-PHENYLENE)-X-)

BENZENE

WHEREIN X IS SULFUR, OXYMETHYLENE, THIAMETHYLENE, THIAETHYLENE, IMINOMETHYLENE, PROPYLENE - 1,3 OR ALKYLATED IMINOMETHYLENE; R1 IS HYDROGEN, LOWER ALKYL, HALOGEN, ALKOXY TRIFLUOROMETHYL, OR ALKYL MERCAPTO AND R2, R3 AND R4 ARE EACH HYDROGEN OR LOWER ALKYL; OR A PHYSIOLOGICALLY ACCEPTABLE ACID ADDITION SALT THEREOF. THERE ARE ALSO DISCLOSED COMPOSITIONS CONTAINING THE ABOVE COMPOUNDS AS ACTIVE INGREDIENT AND METHODS OF USING THE SAME.

59. 发明授权

US3609167A IBENZO{8 b,e{9 {0 THIEPINES 失效
标题翻译： IBENZO {8 b，e {9 {0 THIEPINES
公开(公告)号：US3609167A
公开(公告)日：1971-09-28
申请号：US3609167D
申请日：1962-04-02
申请人： SMITH KLINE FRENCH LAB
发明人： ZIRKLE CHARLES L
IPC分类号： C07C65/24 , C07D313/12 , C07D337/12 , C07D67/00
CPC分类号： C07D337/12 , C07C65/24 , C07D313/12
摘要： Disclosed are dibenzo (b,e) -oxepin and dibenzo (b,e) thiepin11-one useful as intermediates for the preparation of corresponding 11-aminoalkylated derivatives which have pharmaceutical activity.

60. 发明授权

US3594392A Dibenzo(b,e)thiepine-1,1-dioxides 失效
标题翻译： DIBENZO（B，E）THIEPINE-1,1-DIOXIDES
公开(公告)号：US3594392A
公开(公告)日：1971-07-20
申请号：US3594392D
申请日：1961-12-04
申请人： AMERICAN HOME PROD
发明人： WINTHROP STANLEY O , DAVIS MARTIN A
IPC分类号： C07D337/12 , C07D67/00
CPC分类号： C07D337/12
摘要： DIBENZO (B,E)THIEPINE - 1,1 - DIOXIDES, HAVING ANTIHISTAMINIC AND ANTICHOLINERGIC PROPERTIES, AND INTERMEDIATES THEREFOR ARE DISCLOSED.

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