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    • 2. 发明授权
    • Pyrrolotriazolopyrimidine derivatives and process for the preparation
thereof
    • 吡咯并三唑并嘧啶衍生物及其制备方法
    • US4007189A
    • 1977-02-08
    • US683055
    • 1976-05-04
    • Yasunobu SatoHiromu TakagiYasuo ShimojiSeiji Kumakura
    • Yasunobu SatoHiromu TakagiYasuo ShimojiSeiji Kumakura
    • A61K31/505A61P9/08A61P9/12A61P29/00C07D487/14
    • C07D487/14Y10S514/929
    • Pyrrolotriazolopyrimidine derivatives having the formula ##STR1## wherein R.sup.1 represents hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and R.sup.2 represents an alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group having from 5 to 8 carbon atoms, a phenyl group optionally substituted with one or more halogen atoms or a phenylalkyl group having the formula ##STR2## IN WHICH R.sup.3 represents hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, R.sup.4 represents halogen atom, an alkyl group having from 1 to 4 carbon atoms or an alkoxy group having from 1 to 4 carbon atoms, m represents an integer from 0 to 2 and n represents an integer from 0 to 3, and pharmacologically acceptable salts thereof. The compounds are useful as vasodilating or hypotensive agents and may be prepared by reacting triazolopyrimidine derivatives having the formula ##STR3## wherein X.sup.1 and X.sup.2 may be the same or different and each represents a halogen atom and R.sup.1 has the same meaning as defined above with an amine having the formulaR.sup.2 - NH.sub.2wherein R.sup.2 has the same meaning as defined above.
    • 具有式的吡咯并三唑并嘧啶衍生物,其中R 1表示氢原子或具有1至4个碳原子的烷基,R 2表示具有1至4个碳原子的烷基,具有5至8个碳原子的环烷基, 任选被一个或多个卤素原子取代的苯基或具有下式的苯基烷基:其中R 3表示氢原子或具有1至4个碳原子的烷基,R 4表示卤素原子,具有1至 4个碳原子或1〜4个碳原子的烷氧基,m表示0〜2的整数,n表示0〜3的整数,以及其药理学上可接受的盐。 这些化合物可用作血管扩张剂或降血压剂,并且可以通过使具有式(I)的三唑并嘧啶衍生物反应来制备,其中X 1和X 2可以相同或不同,并且各自表示卤素原子,并且R 1具有与上述相同的含义, 具有式R2-NH2的胺,其中R2具有与上述相同的含义。
    • 6. 发明授权
    • Angiotensin II antagosist 1-biphenylmethylimidazole compounds and their
therapeutic use
    • 血管紧张素II拮抗剂1-联苯甲基咪唑化合物及其治疗用途
    • US5616599A
    • 1997-04-01
    • US378650
    • 1995-01-26
    • Hiroaki YanagisawaKoichi FujimotoYoshiya AmemiyaYasuo ShimojiTakuro KanazakiHiroyuki KoikeToshio Sada
    • Hiroaki YanagisawaKoichi FujimotoYoshiya AmemiyaYasuo ShimojiTakuro KanazakiHiroyuki KoikeToshio Sada
    • C07D233/90C07D403/10C07D405/12C07D405/14C07F7/18C07D257/04A61K31/41A61K31/415
    • C07D403/10C07D233/90C07D405/12C07D405/14C07F7/1856
    • Compounds of the following formula (I) or the formula (I).sub.p : ##STR1## wherein R.sup.1 is alkyl or alkenyl; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R.sup.4 is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula --SiR.sup.a R.sup.b R.sup.c, in which R.sup.a, R.sup.b and R.sup.c are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R.sup.5 is carboxy or --CONR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 hydrogens or alkyl, or R.sup.8 and R.sup.9 together form alkylene; R.sup.6 is hydrogen, alkyl, alkoxy or halogen; R.sup.7 is carboxy or tetrazol-5-yl; R.sub.p.sup.1 is hydrogen, alkyl, cycloalkyl or alkanoyl; R.sub.p.sup.2 is a single bond, alkylene or alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are each hydrogen or alkyl; R.sub.p.sup.6 is carboxy or tetrazol-5-yl; and X.sub.p is oxygen or sulfur; and pharmaceutically acceptable salts and esters thereof. The compounds are AII receptor antagonists and thus have hypotensive activity and can be used for the treatment and prophylaxis of hypertension. The compounds may be prepared by reacting a biphenylmethyl compound with an imidazole compound.
    • 下式(I)或式(I)的化合物p:其中R 1是烷基或链烯基; R2和R3是与环烷基稠合的氢,烷基,烯基,环烷基,芳烷基,芳基或芳基; R4是氢,烷基,烷酰基,烯酰基,芳基羰基,烷氧基羰基,四氢吡喃基,四氢噻喃基,四氢噻吩基,四氢呋喃基,式-SiRaRbRc的基团,其中R a,R b和R c是烷基或芳基,烷氧基甲基,(烷氧基烷氧基)甲基,卤代烷氧基甲基, 芳烷基,芳基或烷酰氧基甲氧基羰基; R5是羧基或-CONR8R9,其中R8和R9的氢或烷基,或R8和R9一起形成亚烷基; R6是氢,烷基,烷氧基或卤素; R7是羧基或四唑-5-基; Rp1为氢,烷基,环烷基或烷酰基; Rp2是单键,亚烷基或亚烷基; Rp3和Rp4各自为氢或烷基; Rp6是羧基或四唑-5-基; Xp为氧或硫; 及其药学上可接受的盐和酯。 化合物是AII受体拮抗剂,因此具有低血压活性,可用于治疗和预防高血压。 该化合物可以通过使联苯甲基化合物与咪唑化合物反应来制备。