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公开(公告)号：US4102890A
公开(公告)日：1978-07-25
申请号：US713381
申请日：1976-08-11
IPC分类号： C07C275/18 , C07D233/48 , C07D263/28 , C07D265/06 , C07D277/18
CPC分类号： C07D265/06 , C07C275/18 , C07D233/48 , C07D263/28 , C07D277/18 , C07C2101/02
摘要： Cyclopropylmethylamines which are substituted on the 2-position of nitrogen heterocycles so as to provide new compounds of the formula ##STR1## wherein A is oxygen, sulfur, or nitrogen; the other "R" variables in general are hydrogen, lower-alkyl, cyclopropyl, or lower-alkyl substituted cyclopropyl; and the n's are the numbers 0 to 3, inclusive, and acid addition salts thereof, are disclosed. The compounds are cardiovascular agents, which are depressive of the central nervous system. Their effects include hypnosis, analgesia, and neuro-modulation. They can be used as anti-hypertensive agents.
摘要翻译： 在氮杂环的2位上被取代的环丙基甲基胺，以提供新的式I化合物，其中A是氧，硫或氮; 另一个“R”变量通常是氢，低级烷基，环丙基或低级烷基取代的环丙基; 并且n是数字0至3，包括它们的酸加成盐。 这些化合物是抑制中枢神经系统的心血管药物。 它们的作用包括催眠，镇痛和神经调节。 它们可以用作抗高血压药。
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公开(公告)号：US3988464A
公开(公告)日：1976-10-26
申请号：US427999
申请日：1973-12-26
IPC分类号： C07D243/04 , A61K31/13 , A61K31/33 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5377 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P27/02 , C07C209/08 , C07C209/60 , C07C211/17 , C07C275/18 , C07C335/08 , C07D233/48 , C07D239/14 , C07D247/02 , C07D263/16 , C07D263/28 , C07D265/06 , C07D265/08 , C07D267/06 , C07D277/18 , C07D279/06 , C07D281/02 , A01N9/22 , A01N9/28
CPC分类号： C07C335/08 , C07C275/18 , C07D233/48 , C07D263/28 , C07D265/06 , C07D277/18 , C07C2101/02
摘要： The present invention relates to cyclopropylmethyl amines substituted by a heterocyclic radical.More particularly the heterocyclic radical is a nitrogen containing ring with 5, 6 or 7 links interrupted by another hetero atom selected from the group consisting of oxygen, sulphur and imino--NH--The invention also relates to the acid addition salts thereof with physiologically compatible mineral or organic acids.The invention extends to the processes for making them and the intermediates produced hereto.The invention also includes the pharmaceutical compositions incorporating as active ingredient at least one compound of the invention with an inert carrier.The compounds have therapeutic utility namely on the cardio-vascular diseases and on the neuro-psychological disturbances.
摘要翻译： 本发明涉及被杂环基取代的环丙基甲胺。
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3.发明授权Bicyclo (4.2.0) 1,3,5-octatriene compounds and use as .alpha.-adrenergics 失效双环（4.2.0）1,3,5-辛二烯化合物，用作α-肾上腺素能药物
公开(公告)号：US4567181A
公开(公告)日：1986-01-28
申请号：US596932
申请日：1984-04-05
IPC分类号： A61K31/415 , A61K31/505 , A61P9/00 , A61P9/12 , A61P25/02 , A61P27/16 , C07D233/06 , C07D233/20 , C07D233/22 , C07D239/06 , C07D405/04 , C07D493/04 , C07D233/04 , C07D239/02
CPC分类号： C07D405/04 , C07D233/06 , C07D493/04
摘要： Compounds of the formula: ##STR1## in which: R.sub.1 and R.sub.2 each represent, independently of one another, hydrogen, halogen, alkyl or alkoxy having from 1 to 4 carbon atoms, sulphonamide possibly substituted by an alkyl radical having from 1 to 4 carbon atoms; or together methylenedioxy, n is 0 or 1,in racemic form or in the form of optical isomers, and also their salts of addition with pharmaceutically acceptable acids. Useful in the treatment of ailments and/or conditions which are adrenoreceptor-related, such relationship being well known in the art.
摘要翻译： 下式的化合物：其中：R 1和R 2各自独立地表示氢，卤素，具有1至4个碳原子的烷基或烷氧基，磺酰胺可以被具有1至4个的烷基取代 碳原子 或一起亚甲二氧基，n为0或1，以外消旋形式或旋光异构体的形式，以及它们与药学上可接受的酸的加成盐。 可用于治疗与肾上腺素受体相关的疾病和/或病症，这种关系是本领域熟知的。
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公开(公告)号：US4260610A
公开(公告)日：1981-04-07
申请号：US957659
申请日：1978-11-03
IPC分类号： C07D409/12 , A61K31/495 , A61K31/505 , A61P9/08 , A61P9/12 , A61P25/00 , A61P29/00 , C07D327/00 , C07D327/04 , C07D411/12 , C07D417/12 , C07D411/14 , C07D417/14
CPC分类号： C07D327/04
摘要： Disubstituted piperazines of the formula: ##STR1## in which: n is 1 or 2,X is oxygen and Y is sulfur or sulfonyl or X and Y are both sulfur or sulfonyl, andHet is a 5- or 6-membered heterocyclic radical having from 1 to 3 hetero atoms inclusive selected from nitrogen and sulfur and optionally substituted by one or more alkyl each having from 1 to 5 carbon atoms inclusive.These compounds may be used as medicines, especially in the treatment of central nervous system disorders and Parkinson's disease.
摘要翻译： 下式的二取代哌嗪：其中：n为1或2，X为氧，Y为硫或磺酰基或X和Y均为硫或磺酰基，Het为具有5或6元杂环基， 包括选自氮和硫的1至3个杂原子，并且任选被一个或多个包含1至5个碳原子的烷基取代。 这些化合物可以用作药物，特别是用于治疗中枢神经系统障碍和帕金森病。
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公开(公告)号：US4123531A
公开(公告)日：1978-10-31
申请号：US745032
申请日：1976-11-26
IPC分类号： A61K31/16 , A61K31/165 , A61P25/08 , C07C67/00 , C07C233/35 , C07C313/00 , C07C323/62 , C07D207/06 , C07D295/13 , A61K31/495 , C07D295/08 , C07D295/10
CPC分类号： C07D295/13 , C07D207/06
摘要： This invention relates to novel acetamides, the nitrogen of which is substituted with an amino lower alkyl chain.This invention also relates to a process for producing the said N-substituted acetamides.The end compounds have therapeutical utility and find a use as anti-convulsant agents.
摘要翻译： 本发明涉及新的乙酰胺，其氮被氨基低级烷基链取代。
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公开(公告)号：US4010267A
公开(公告)日：1977-03-01
申请号：US562226
申请日：1975-03-26
IPC分类号： A61K31/495 , A61P9/08 , A61P25/26 , C07D317/46 , C07D317/72 , C07D405/12 , C07D417/12 , C07D295/08
CPC分类号： C07D317/72 , C07D317/46 , Y10S514/929
摘要： Benzodioxole compounds of the formula: vasodilator ##STR1## WHEREIN R.sub.1 is hydrogen, lower alkyl, aryl, haloaryl, lower-alkylaryl, lower-alkoxyaryl, methylenedioxyaryl, ethylenedioxyaryl, trifluoromethylaryl, nitroaryl or aminoaryl,R.sub.2 is lower-alkyl, aryl, haloaryl, lower-alkylaryl, lower-alkoxyaryl, methylenedioxyaryl, ethylenedioxyaryl, trifluoromethylaryl, nitroaryl or aminoaryl, orR.sub.1 + r.sub.2 are --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --(CH.sub.2).sub.6 -- andHet is pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, quinazolinyl, 1,3,5 triazinyl or 1,3-thiazolyl, each being optionally substituted by lower-alkyl, lower-alkoxy, hydroxyl or phenyl.These compounds are used as medicines especially as peripheral vasocilator agent and central nervous system stimulant.
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公开(公告)号：US4267178A
公开(公告)日：1981-05-12
申请号：US14876
申请日：1979-02-26
IPC分类号： C07D417/12 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/443 , A61K31/495 , A61K31/505 , A61P9/12 , C07D405/12 , C07D405/14 , A61K31/36 , A61K31/335
CPC分类号： C07D405/14
摘要： Disubstituted piperazines of the formula ##STR1## in which n is 1 or 2,m is 0 or 1, andHet is pyridyl, pyrimidinyl, pyrazinyl, thiazolyl or thiadiazolyl each optionally substituted by one or more alkyl having from 1 to 5 carbon atoms inclusive.These compounds and their physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of hypertension.
摘要翻译： 式为“IMAGE”的二取代哌嗪，其中n为1或2，m为0或1，Het为吡啶基，嘧啶基，吡嗪基，噻唑基或噻二唑基，各自任选被一个或多个含有1至5个碳原子的烷基取代 。 这些化合物及其生理上可耐受的酸加成盐可以用作药物，特别是用于治疗高血压。
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公开(公告)号：US4177272A
公开(公告)日：1979-12-04
申请号：US864204
申请日：1977-12-27
IPC分类号： C07D403/04 , A61K31/495 , A61K31/496 , A61P9/00 , A61P9/12 , A61P25/00 , C07D249/14 , C07D271/06 , C07D271/07 , C07D285/08 , C07D285/12 , C07D285/135 , C07D317/00 , C07D319/00 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , A61K31/50
CPC分类号： C07D271/07 , C07D249/14 , C07D285/08 , C07D285/135
摘要： Disubstituted piperazines of the formula: ##STR1## wherein: ##STR2## is naphthyl, benzo [b] furanyl, benzo [b] thienyl, benzodioxolyl, benzodioxanyl, benzodioxacycloheptanyl, coumaranyl, chromanyl, .DELTA..sup.3 -chromenyl, thiochromanyl or .DELTA..sup.3 -thiochromenyl,X is nitrogen and simultaneously Y is oxygen or sulfur, orX is sulfur, imino (NH) or methylimino (N CH.sub.3) and simultaneously Y is nitrogen, andR is hydrogen, lower alkyl, phenyl, halophenyl, lower-alkylphenyl or lower alkoxyphenyl.These compounds possess interesting pharmacological and therapeutic properties, and may be used as medicines, especially in the treatment of hypertension, peripheral vascular disorders and Parkinson's disease.
摘要翻译： 下式的二取代哌嗪其中：苯并[b]呋喃基，苯并[b]噻吩基，苯并二恶唑基，苯并二氧杂环戊烷基，苯并二恶环庚烷基，香豆素基，苯并二氢吡喃基，DELTA 3-苯并二氢吡喃基， ，X是氮，同时Y是氧或硫，或X是硫，亚氨基（NH）或甲基亚氨基（N CH3），同时Y是氮，R是氢，低级烷基，苯基，卤代苯基，低级烷基苯基或低级 烷氧基苯基。 这些化合物具有有趣的药理和治疗特性，可用作药物，特别是用于治疗高血压，外周血管疾病和帕金森病。
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公开(公告)号：US4100286A
公开(公告)日：1978-07-11
申请号：US741740
申请日：1976-11-15
IPC分类号： A61K31/505 , A61K31/52 , A61P9/00 , A61P21/02 , A61P25/00 , A61P25/08 , C07D239/48 , C07D473/00 , C07D473/34 , C07D473/40 , C07D487/04
CPC分类号： C07D487/04 , C07D239/48 , C07D473/00 , C07D473/34 , C07D473/40
摘要： Heterocyclic compounds of the formula: ##STR1## WHEREIN ONE OF Y and Z is CH, the other being N, A is a straight or branched saturated hydrocarbon chain from C.sub.2 to C.sub.6 inclusive, X is chlorine, hydroxy, alkoxy or alkylthio each from C.sub.1 to C.sub.5 inclusive, R is hydrogen, alkyl, hydroxyalkyl or dihydroxyalkyl each from C.sub.1 to C.sub.3 inclusive, R' is halogen, alkyl or alkoxy each from C.sub.1 to C.sub.3 inclusive and n is 0, 1 or 2.These compounds, their optical isomers and their physiologically tolerable salts are used as medicines especially in the treatment of central nervous system disorders.
摘要翻译： 下式的杂环化合物：Y和Z之一为CH，另一个为N，A为C2至C6的直链或支链饱和烃链，其中X为氯，羟基，烷氧基或烷硫基，各自为C1 为C 5，R为氢，烷基，羟基烷基或二羟基烷基，各自为C 1〜C 3，其中R 1为卤素，烷基或烷氧基，各自为C 1〜C 3，其中n为0,1或2。
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公开(公告)号：US3954765A
公开(公告)日：1976-05-04
申请号：US512461
申请日：1974-10-07
IPC分类号： C07D417/12 , A61K31/495 , A61P9/08 , A61P9/12 , A61P25/00 , A61P25/04 , B01J23/00 , C07B61/00 , C07D295/04 , C07D311/04 , C07D417/14 , C07D295/12
CPC分类号： C07D417/14
摘要： Piperazine derivatives of the formula: ##SPC1##Wherein n is 0 or 1, X is oxygen or sulfur, R and R', which are the same or different, are hydrogen or lower alkyl and: ##SPC2##Is always bonded to the benzene ring.These compounds are used as medicine especially in the treatment of peripheral vascular disorders, Parkinson's disease, hypertension and pain.
摘要翻译： 下式的哌嗪衍生物：
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