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    • 8. 发明授权
    • Anti-spasmdoic agents having an acetylenic bond
    • 具有炔属键的抗痉挛剂
    • US4957941A
    • 1990-09-18
    • US463892
    • 1990-01-09
    • William M. Davis
    • William M. Davis
    • C07D295/084
    • C07D295/084
    • A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## where Y is H or OH;j is an integer from 0 to 4;k is an integer from 0 to 4, and whereinm is an integer from 1 to 4;n is an integer from 1 to 4;p is an integer from 1 to 4; andX may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof, but when X is nonexistent the terminal group in which both the n-chain and the p-chain is a methyl group. ##STR2## The reaction was performed under reflux condensation. Following the reaction, which was usually complete within a few hours, the acid chlorides were vacuum distilled and reacted with a thiol compound as described above.The compounds of this invention are anti-muscarinic agents (cholinergic-muscarinic receptor antagonists) which inhibit the actions of acetylcholine on autonomic effectors innervated by postganglionic cholinergic nerves as well as on smooth muscle that lacks cholinergic innervation. Since a major component of parasympathetic control of smooth muscle occurs via muscarinic receptors, these compounds are effective as modifiers of smooth muscle activity.Thiphenamil hydrochloride has been shown to decrease spasm of the gastrointestinal tract, biliary tract, ureter and uterus without producing characteristic atropinic side effects on salivary and sweat glands, GI glands, the eye or the cardiovascular system. This invention results in compounds which are as efficacious as thiphenamil hydrochloride, or more so, in relaxing various smooth muscle systems while at the same time demonstrating thiphenamil hydrochloride's lack of associated side-effects.
    • 提供了一类新的具有两条支链的抗痉挛化合物。 该化合物具有通式:其中Y是H或OH; j为0〜4的整数, k为0〜4的整数,m为1〜4的整数, n是1至4的整数; p是1至4的整数; 并且X可以不存在,或者可以是O,S,NH或CH 2或其盐,但是当X不存在其中n链和p链都是甲基的末端基团时。 反应在回流冷凝下进行。 反应通常在几小时内完成,如上所述,将酰氯真空蒸馏并与硫醇化合物反应。 本发明的化合物是抑制乙酰胆碱对由神经节后胆碱能神经支配的自主神经作用者以及缺乏胆碱能神经支配的平滑肌的作用的抗毒蕈碱药(胆碱能 - 毒蕈碱受体拮抗剂)。 由于平滑肌副交感神经控制的主要成分是通过毒蕈碱受体发生的,所以这些化合物作为平滑肌活性的调节剂是有效的。 已经证明,盐酸泰而米米可以减少胃肠道,胆道,输尿管和子宫的痉挛,而不会对唾液腺和汗腺,胃腺,眼睛或心血管系统产生特征性的阿托品副作用。 本发明产生的化合物与盐酸泰维必利素一样有效,或更倾向于在放松各种平滑肌系统的同时,同时显示出盐酸泰尼泊尔缺乏相关的副作用。
    • 9. 发明授权
    • Method of treating smooth muscle spasm
    • 治疗平滑肌痉挛的方法
    • US4725593A
    • 1988-02-16
    • US853378
    • 1986-04-15
    • William M. Davis
    • William M. Davis
    • A61K31/265A61K31/54
    • A61K31/265
    • A new method of treating a patient suffering smooth muscle spasm comprises administering to the patient an effective amount of anti-spasmodic compound having the general formula: ##STR1## where R is selected from the group consisting of: ##STR2## wherein W is CH.sub.2, NH, O or S, ##STR3## wherein Y is an alicyclic ring ring having 3-12 carbon atoms, and ##STR4## the total number of carbon atoms in R is equal to or less than 20. Furthermore, m is an integer from 1 to 4, n is an integer from 1 to 4, p is an integer from 1 to 4 and q is an integer from 1 to 4. X may be nonexistent or may be 0, S, NH or CH.sub.2 or salts thereof. However, when X is nonexistent the terminal group in both the n-chain and the p-chain is a methyl group provided that a is zero or 1 and when a is 1, X is selected from the group consisting of 0, S, and CH.sub.2 and n and p are integers from 1 to 4; and when a is 0 then X is nonexistent and n and p are integers from 1 to 4 and the terminal group in both the n-chain and the p-chain is methyl; and pharmaceutically acceptable salts thereof.
    • 治疗患有平滑肌痉挛的患者的新方法包括向患者施用有效量的具有以下通式的抗痉挛化合物:其中R选自:其中W是CH 2, NH,O或S,其中Y是具有3-12个碳原子的脂环族环,并且R中的总碳原子数等于或小于20.此外,m是 1至4,n为1至4的整数,p为1至4的整数,q为1至4的整数.X可以不存在或可以为0,S,NH或CH 2或其盐。 然而,当X不存在时,n链和p链中的末端基团是甲基,条件是a为0或1,当a为1时,X选自0,S和 CH2和n和p是1至4的整数; 当a为0时,X不存在,n和p为1〜4的整数,n链和p链中的末端基为甲基; 及其药学上可接受的盐。