摘要:
O-Carbamoyl-phenylalaninol having substituent at benzene ring, represented by the general formula I, and pharmaceutically useful salts thereof, which are useful for the prophylaxis and treatment of CNS disorder including depression and anxiety, are disclosed: ##STR1## wherein R is lower alkyl containing 1 to 8 carbon atoms, halogen such as F, Cl and I, alkoxy containing 1 to 3 carbon atoms, thioalkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, or trifluorocarbon, and x is an integer of 1 to 3, with a proviso that R is the same or different when x is 2 or 3.
摘要:
The present invention relates to O-thiocarbamoyl-aminoalkanol compound represented by the following structural formula (VI), (VIII) and (IX) which are a racemic or enantiomerically enriched and pharmaceulically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein Ar is a phenyl group as described as follows: ##STR2## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br, and I, alkoxy containing 1 to 3 carbon atoms, thioalkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, or taifluorocarbon, and x is an integer from 1 to 3, with the proviso that R is the same or different when x is 2 or 3. R.sub.1 and R.sub.2 may be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, 3 to 7-membered aliphatic cyclic compounds and R.sub.1 and R.sub.2, together with the adjoining N-atom, form a 5 to 7-membered cyclic compound which optionally comprises zero to one additional nitrogen atoms substituted with a member selected from the group consisting of hydrogen, alkyl and aryl groups, or zero to one oxygen atoms directly unconnected, R.sub.3 and R.sub.4 may be same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, 3 to 7-membercd aliphatic cyclic compounds and R.sub.3 and R.sub.4, together with the adjoining N-atom, form a 5 to 7-membered cyclic compound which optidonally comprises zero to one additional nitrogen atoms substituted with a member selected from the group consisting of hydrogen, alkyl and aryl groups, or zero to one oxygen atoms directly unconnected, each of l, m and n is zero or 1, and the pharmaceutically acceptable salts thereof.
摘要:
The present invention relates to a racemic or enantiomerically enriched O-carbamoyl-phenylalaninol compound represented by the following structural formula V and pharmaceutically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein Ph is a phenyl group as described as follows: ##STR2## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms, and x is an integer from 1 to 3, with the proviso that R is the same or different when x is 2 or 3, R.sup.1 and R.sup.2 may be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cyclic propyl and 5 to 7-membered aliphatic cyclic compounds, and R.sup.1 and R.sup.2 may be joined to form a 5 to 7-membered cyclic compound which may comprise zero to one additional nitrogen atom substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, or zero to one oxygen atom directly unconnected, excluding the instance where R, R.sup.1, and R.sup.2 are all hydrogen, and the pharmaceutically acceptable salts thereof. The present invention also relates to O-carbamoyl-(D)-phenylalaninol compounds, represented by the following structural formula IX: ##STR3## wherein Ph, R.sup.1, and R.sup.2 are as described above, and the pharmaceutically acceptable salts thereof.
摘要:
The present invention relates to O-carbamoyl-(D)-phenylalaninol compound represented by the following structural formula V and pharmaceutically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein R.sup.1 and R.sup.2 may be the same with or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl containing 1 to 8 carbon atoms, and 5 to 7-membered aliphatic cyclic compounds which may comprise not more than two nitrogen or oxygen atoms directly unconnected, the total number of carbon atom of R.sup.1 and R.sup.2 ranging from 0 to 16.
摘要:
A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
摘要:
A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
摘要:
This invention is directed to a method of treating sexual dysfunction in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, CI, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and O to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the oxygen atom.
摘要翻译:本发明涉及治疗受试者的性功能障碍的方法,其包括施用治疗有效量的式(I)化合物或其药学上可接受的盐或酯的步骤,其中Rx是选自下组的成员 由氢,1至8个碳原子的低级烷基,选自F,Cl,Br和I的卤素,含有1至3个碳原子的烷氧基,硝基,羟基,三氟甲基和含有1至3个碳原子的硫代烷氧基组成; x为1〜3的整数,条件是当x为2或3时R可以相同或不同; R 1和R 2可以相同或不同,并且独立地选自氢,1至8个碳原子的低级烷基,芳基,芳基烷基,3至7个碳原子的环烷基; R1和R2可以连接形成被选自氢,烷基和芳基的成员所取代的5至7元杂环,其中环状化合物可包含1至2个氮原子和0至1个氧原子 其中氮原子彼此不直接连接或与氧原子直接连接。
摘要:
A method of vehicle modulated administration of an anticonvulsive agent to the nasal mucous membranes of humans and animals is disclosed. The vehicle system is an aqueous pharmaceutical carrier comprising an aliphatic alcohol, a glycol and a biological surfactant such as a bile salt or a lecithin. The pharmaceutical composition provides a means to control and promote the rate and extent of transmucosal permeation and absorption of the medicaments via a single and multiple administration. Nasal administration of the pharmaceutical preparation produces a high plasma concentration of the anticonvulsant nearly as fast as intravenous administration. Such compositions are particularly suitable for a prompt and timely medication of patients in the acute and/or emergency treatment of status epilepticus and other fever-induced seizures.
摘要:
Azole compounds containing carbamoyl group and pharmaceutically useful salts thereof are described. The compounds are effective anticonvulsants which are used in the treatment of disorders of the central nervous system, especially as anxiety, depression, convulsion, epilepsy, migraine, bipolar disorder, drug abuse, smoking, ADHD, obesity, sleep disorder, neuropathic pain, stroke, cognitive impairment, neurodegeneration, stroke and muscle spasm.
摘要:
There are disclosed novel sulfamate compounds containing N-substituted carbomoyl group including their racemates and (R)- and (S)-optical isomers represented by Formulas I, II and III, pharmaceutically useful for the prophylaxis and treatment of the disorders of the central nervous system, especially for nervous myalgia, epilepsy and minimal brain dysfunction: ##STR1## (III).