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111. 发明授权

US4769373A Anti-arrhythmic azabicyclic compounds 失效
标题翻译：抗心律不齐的氮杂双环化合物
公开(公告)号：US4769373A
公开(公告)日：1988-09-06
申请号：US674773
申请日：1984-11-26
申请人： Karoly Nador , Gabor Kraiss , Margit Paroczay , Egon Karpati , Laszlo Szporny
发明人： Karoly Nador , Gabor Kraiss , Margit Paroczay , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/435 , A61P9/06 , A61P25/02 , C07D211/72 , C07D221/22 , C07D405/12 , C07D409/12 , A61K31/44
CPC分类号： C07D221/22 , C07D211/72 , C07D405/12 , C07D409/12
摘要： The invention relates to new anti-arrythmic azabicyclo[3.3.1]nonanes of the general formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are C.sub.1-4 alkyl groups which are the same or different, or one of them is a benzyl group and the others are C.sub.1-4 alkyl groups, andR.sup.4 is a hydroxy group, or an etherified hydroxy group of the formula --OR.sup.5, or an esterified hydroxy group of the formula --OOCR.sup.6, in which the esterifying groupR.sup.5 is a phenyl or benzyl group which optionally each can have a trihalomethyl substituent or one or more halogen or C.sub.1-4 substituents, or is a diphenyl or benzhydryl group, and the esterifying groupR.sup.6 is a C.sub.1-8 alkyl or a C.sub.3-6 cycloalkyl group, or a phenyl or benzyl group which optionally each can have a halo-substituent or one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro or phenyl substituents, or is an optionally halogenated or hydrogenated naphthyl group, or a cinnamyl group optionally substituted by a halogen atom or C.sub.1-4 alkoxy groups, or is a benzhydryl or 1,1-diphenyl-hydroxymethyl group, or is a heterocyclic substituent selected from the group consisting of thenyl, 9-xanthenyl or 3-indolyl-(C.sub.1-3 alkyl) groups,as well as the stereoisomers and pharmaceutically acceptable acid addition salts thereof.The invention also provides a process for the preparation of the new compounds of the general formula (I), in which new intermediates of the general formula (IV), ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, are utilized.
摘要翻译：本发明涉及通式（I）的新的抗焦虑氮杂二氮杂双环[3.3.1]壬烷，其中R1，R2和R3是相同或不同的C1-4烷基，或其中之一它们是苄基，其它是C 1-4烷基，R4是羟基，或式-OR5的醚化羟基或式-OOCR6的酯化羟基，其中酯化基团R5 是任选地可以具有三卤代甲基取代基或一个或多个卤素或C 1-4取代基的苯基或苄基，或者是二苯基或二苯甲基，酯化基团R6是C 1-8烷基或C 3-6环烷基基团或苯基或苄基，其任选地各自可以具有卤素取代基或一个或多个C 1-4烷基，C 1-4烷氧基，硝基或苯基取代基，或者是任选卤代或氢化的萘基或肉桂基任选被卤素原子或C 1-4烷氧基取代，或者是二苯甲基或1,1-二苯基 - 氢或者是选自草酰基，9-呫吨基或3-吲哚基 - （C 1-3烷基）基团的杂环取代基，以及它们的立体异构体和药学上可接受的酸加成盐。本发明还提供了制备通式（I）的新化合物的方法，其中通式（IV）的新中间体，其中R 1，R 2和R 3如上所定义，被利用。

112. 发明授权

US4661498A Furo 3,2-c pyridine derivatives and their use in treating depression and cerebral ischemia 失效
标题翻译： Furo 3,2-c吡啶衍生物及其在治疗抑郁症和脑缺血中的应用
公开(公告)号：US4661498A
公开(公告)日：1987-04-28
申请号：US780453
申请日：1985-09-26
申请人： Alexander Wick , Jonathan Frost , Jean Bertin
发明人： Alexander Wick , Jonathan Frost , Jean Bertin
IPC分类号： A61K31/435 , A61P25/24 , A61P25/26 , C07D211/72 , C07D211/74 , C07D491/04 , C07D491/048 , A61K31/44
CPC分类号： C07D491/04 , C07D211/72 , C07D211/74
摘要： Compounds of general formula (I) ##STR1## wherein R1 represents a phenyl, halophenyl, methylphenyl, ethylphenyl, methoxyphenyl, trifluoromethylphenyl or naphthyl group, R2 represents hydrogen or a methyl or phenyl group, and R3 represents hydrogen or a benzyl group, except compounds in which R1 is a phenyl or 4-fluorophenyl group, R2 is hydrogen and R3 is hydrogen or a benzyl group, and their pharmaceutically acceptable acid addition salts have useful anti-depressant and anti-ischaemic properties.
摘要翻译：通式（I）的化合物其中R 1表示苯基，卤代苯基，甲基苯基，乙基苯基，甲氧基苯基，三氟甲基苯基或萘基，R 2表示氢或甲基或苯基，R 3表示氢或苄基除了R1是苯基或4-氟苯基，R2是氢和R3是氢或苄基的化合物以外，其药学上可接受的酸加成盐具有有用的抗抑郁和抗缺血性质。

113. 发明授权

US4370477A Certain 2-(arylaliphatic thio)-pyridinium compounds 失效
标题翻译：某些2-（芳基脂族硫代） - 吡啶鎓化合物
公开(公告)号：US4370477A
公开(公告)日：1983-01-25
申请号：US286831
申请日：1981-07-27
申请人： Roger Crossley
发明人： Roger Crossley
IPC分类号： C07D211/72 , C07D213/70 , C07D213/02
CPC分类号： C07D213/70 , C07D211/72
摘要： The invention concerns the treatment of ulcers and hypersecretion in a mammal using compounds of the formula IAr--A--S--Y Iwhere Ar is phenyl, which may be substituted or cycloalkyl of 5 to 7 carbon atoms, A is saturated or unsaturated lower alkylene which may be substituted by lower alkyl, oxo or hydroxy, 5 is sulphur and Y is an optionally substituted pyridine, pyridinium, tetrahydropyridine or tetrahydropyridinium radical. Certain novel compounds and pharmaceutical compositions are also claimed.
摘要翻译：本发明涉及使用式I Ar-ASY I的化合物治疗哺乳动物的溃疡和过度分泌，其中Ar是可以被取代的苯基或可以是5-7个碳原子的环烷基，A是饱和或不饱和的低级亚烷基，其可以是被低级烷基，氧代或羟基取代，5是硫，Y是任选取代的吡啶，吡啶鎓，四氢吡啶或四氢吡啶鎓基团。还要求保护某些新的化合物和药物组合物。

114. 发明授权

US4324789A 1-Benzyl-5-nitro-4-(pyridyl or imidazolyl) alkylamino-1,2,3,6-tetrahydropyrimidines and blocking of histamine H.sub.2 失效
标题翻译： 1-苄基-5-硝基-4-（吡啶基或咪唑基）烷基氨基-1,2,3,6-四氢嘧啶和其组胺H 2受体的阻断
公开(公告)号：US4324789A
公开(公告)日：1982-04-13
申请号：US159525
申请日：1980-06-16
申请人： Michael L. Roantree , Rodney C. Young
发明人： Michael L. Roantree , Rodney C. Young
IPC分类号： C07D203/12 , C07D207/24 , C07D211/72 , C07D239/06 , A61K31/505
CPC分类号： C07D239/06 , C07D203/12 , C07D207/24 , C07D211/72
摘要： 2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur or oxygen. The compounds of the invention are preferably dihydropyrroles or tetrahydropyrridines or pyrimidines. The compounds of the invention are histamine H.sub.2 -receptor antagonists.
摘要翻译：具有3-硝基和2-杂环基烷基氨基的2,3-不饱和含氮杂环化合物。 2-位取代基的烷基优选被硫或氧中断。本发明的化合物优选为二氢吡咯或四氢吡啶或嘧啶。本发明的化合物是组胺H2受体拮抗剂。

115. 发明授权

US4304781A Treatment of ulcers and hypertension 失效
标题翻译：治疗溃疡和高血压
公开(公告)号：US4304781A
公开(公告)日：1981-12-08
申请号：US170366
申请日：1980-07-21
申请人： Roger Crossley
发明人： Roger Crossley
IPC分类号： C07D211/72 , C07D213/70 , A61K31/44
CPC分类号： C07D213/70 , C07D211/72
摘要： The invention concerns the treatment of ulcers and hypersecretion in a mammal using compounds of the formula IAr--A--S--Y Iwhere Ar is phenyl, which may be substituted or cycloalkyl of 5 to 7 carbon atoms, A is saturated or unsaturated lower alkylene which may be substituted by lower alkyl, oxo or hydroxy, S is sulphur and Y is an optionally substituted pyridine, pyridinium, tetrahydropyridine or tetrahydropyridinium radical. Certain novel compounds and pharmaceutical compositions are also disclosed.
摘要翻译：本发明涉及使用式I Ar-ASY I的化合物治疗哺乳动物的溃疡和过度分泌，其中Ar是可以被取代的苯基或可以是5-7个碳原子的环烷基，A是饱和或不饱和的低级亚烷基，其可以是被低级烷基，氧代或羟基取代，S是硫，Y是任选取代的吡啶，吡啶鎓，四氢吡啶或四氢吡啶鎓基团。还公开了某些新型化合物和药物组合物。

116. 发明授权

US4218455A 1-(4-Fluorophenyl)-4-[1,2,3,6-tetrahydro -4-(phenylthio)-1-pyridinyl]-butanones and related sulfoxides and sulfones 失效
标题翻译： 1-（4-氟苯基）-4- [1,2,3,6-四氢-4-（苯硫基）-1-吡啶基] - 丁酮和相关的亚砜和砜
公开(公告)号：US4218455A
公开(公告)日：1980-08-19
申请号：US922511
申请日：1978-07-10
申请人： Lawrence D. Wise , Patrick F. Flynn , Glenn C. Morrison
发明人： Lawrence D. Wise , Patrick F. Flynn , Glenn C. Morrison
IPC分类号： C07D211/72 , C07D213/70 , A61K31/44 , C07D213/04
CPC分类号： C07D213/70 , C07D211/72
摘要： Tetrahydropyridylbutyrophenones of the following formula IX: ##STR1## wherein x is hydrogen, halogen such as fluorine, chlorine, bromine or iodine, trifluoromethyl, alkoxy, nitro, cyano, amino, lower alkyl of 1 to 6 carbons, aryl or substituted aryl; y is hydrogen or halogen; and n is 0, 1 or 2; and the non-toxic, pharmaceutically acceptable acid addition salts thereof. Tetrahydropyridylbutanols having the formula X: ##STR2## wherein x and y are as defined above, as well as their non-toxic, pharmaceutically acceptable acid addition salts, are also disclosed. The compounds of the invention having the formulas IX and X are useful as antipsychotics.
摘要翻译：下式IX的四氢吡啶基丁酰苯：IX其中x是氢，卤素如氟，氯，溴或碘，三氟甲基，烷氧基，硝基，氰基，氨基，1至6个碳的低级烷基，芳基或取代的芳基; y是氢或卤素; 且n为0,1或2; 和其无毒的药学上可接受的酸加成盐。还公开了具有式X的XRD的四氢吡啶基丁醇，其中x和y如上所定义，以及它们的无毒的药学上可接受的酸加成盐。具有式IX和X的本发明化合物可用作抗精神病药。

117. 发明授权

US4196210A N-Aryl-N-(1-L-4-piperidinyl)-arylacetamides 失效
标题翻译： N-芳基-N-（1-L-4-哌啶基） - 芳基乙酰胺
公开(公告)号：US4196210A
公开(公告)日：1980-04-01
申请号：US924484
申请日：1978-07-13
申请人： Stefan Sanczuk , Hubert K. Fr. Hermans
发明人： Stefan Sanczuk , Hubert K. Fr. Hermans
IPC分类号： C07D211/58 , C07D211/66 , C07D211/72 , A61K31/445 , C07D409/12
CPC分类号： C07D211/72 , C07D211/58 , C07D211/66
摘要： Novel N-aryl-N-(1-L-4-piperidinyl)arylacetamides useful as anti-arrhythmic agents, a method of treating arrhythmia which comprises the systemic administration of such compounds to warm-blooded animals and pharmaceutical compositions to be used therefor.
摘要翻译：用作抗心律失常剂的新型N-芳基-N-（1-L-4-哌啶基）芳基乙酰胺，一种治疗心律不齐的方法，其包括向温血动物全身施用此类化合物以及为此使用的药物组合物。

118. 发明授权

US4153235A Substituted cycloalkyl lactamimides 失效
标题翻译：取代的环状内酰胺
公开(公告)号：US4153235A
公开(公告)日：1979-05-08
申请号：US877653
申请日：1978-02-14
申请人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
发明人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
IPC分类号： C07D207/22 , C07D211/72 , C07D223/10 , C07D223/12 , C07D225/02 , C07D223/04
CPC分类号： C07D207/22 , C07D211/72 , C07D223/10 , C07D223/12 , C07D225/02 , Y10S514/822 , Y10S514/866 , Y10S514/869 , Y10S514/884
摘要： Compounds possessing hypoglycemic, hypotensive, anti-inflammatory, anticoagulant and diuretic acitivity are represented by compounds of the following formula ##STR1## wherein Y is thienyl, cycloalkyl of from 5 to 7 carbon atoms, phenyl or substituted phenyl in which case the substituents on the substituted phenyl are selected from halogen, such as fluorine, chlorine, bromine or iodine, lower alkyl of from 1 to 4 carbon atoms and lower alkoxy of from 1 to 4 carbon atoms; Z is hydrogen or hydroxy; R is hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl of from 1 to 4 carbon atoms or halogen, such as chlorine, fluorine, bromine or iodine; m is from 3 to 6; and n is from 3 to 11. Pharmaceutical compositions of these compounds and their use are also disclosed.

119. 发明授权

US4144344A Antihypertensive 1-substituted-4-(2-oxo-1-imidazolidinyl) piperidines 失效
标题翻译：抗高血压1-取代-4-（2-氧代-1-咪唑烷基）哌啶
公开(公告)号：US4144344A
公开(公告)日：1979-03-13
申请号：US761510
申请日：1977-01-21
申请人： Kurt Eichenberger , Hans Kuhnis , Franz Ostermayer , Herbert Schroter
发明人： Kurt Eichenberger , Hans Kuhnis , Franz Ostermayer , Herbert Schroter
IPC分类号： A61K31/4409 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/505 , A61P9/06 , A61P9/12 , A61P25/02 , C07D211/58 , C07D211/72 , C07D211/74 , C07D213/74 , C07D401/04 , C07D401/14
CPC分类号： C07D213/74 , C07D211/58 , C07D211/72
摘要： A process known per se for the manufacture of oxygenated N-aryl-diazacyclic compounds of the formula ##STR1## wherein EACH OF R.sub.1 and R.sub.2 represents a substituted or unsubstituted aryl group and alk represents a lower alkylene group which separates both nitrogen atoms from each other by 2 or 3 carbon atoms, or salts thereof.The novel compounds can be used as antihypertensives, antitachycardiac agents and .alpha.-receptor blockers.
摘要翻译：本领域已知的用于制备式（I）的氧化N-芳基 - 二氮环化合物的方法，其中R 1和R 2各自表示取代或未取代的芳基，而alk表示分开两个氮原子的低级亚烷基彼此间有2或3个碳原子，或其盐。

120. 发明授权

US4126689A N-aryl-N-(1-alkyl-4-piperidinyl)-arylacetamides 失效
标题翻译： N-亚甲基-N-（1-烷基-4-哌啶子基） - 十六烷基胺
公开(公告)号：US4126689A
公开(公告)日：1978-11-21
申请号：US795669
申请日：1977-05-11
申请人： Stefan Sanczuk , Hubert K. F. Hermans
发明人： Stefan Sanczuk , Hubert K. F. Hermans
IPC分类号： C07D211/58 , C07D211/66 , C07D211/72 , A61K31/445
CPC分类号： C07D211/58 , C07D211/66 , C07D211/72 , Y10S514/821
摘要： Novel N-aryl-N-(1-L-4-piperidinyl)arylacetamides useful as antiarrhythmic agents, a method of treating arrhythmia which comprises the systemic administration of such compounds to warm-blooded animals and pharmaceutical compositions to be used therefor.

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