摘要:
N-Arylphenylacetamide derivatives represented by the following formula [I]: (wherein R1 is C1-6 alkoxy, etc.; R2 is hydrogen, —(CH2)m—N(R6)(R7) (m is an integer of from 1 to 4; R6 is hydrogen, C1-4 alkyl, etc., R7 is hydrogen, etc.), etc.; R3 is hydrogen, halogen, etc.; R4 is C6-10 alkyl, —Y—R8 (Y is a single bond, C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc., R8 is aryl, C3-8 cycloalkyl, C6-15 polycycloalkyl, etc.), etc.; R5 is hydrogen, etc.; and X1 is hydrogen), or pharmaceutically acceptable salts thereof or hydrates or solvates of the same, and a pharmaceutical composition containing the same. These compounds are useful as preventives and/or remedies giving no pain at the early stage of administration, which are efficacious in oral administration and have potent analgesic and antiinflammatory effects.
摘要翻译:由下式[I]表示的N-芳基苯基乙酰胺衍生物:其中R 1是C 1-6烷氧基等; R 2, 是(CH 2)n -N(R 6)(R 7)(m)是(CH 2) 1〜4的整数; R 6为氢,C 1-4烷基等,R 7为氢等。 )等; R 3是氢,卤素等; R 4是C 6-10烷基,-YR“ 8(Y为单键,C 1-6亚烷基,C 2-6亚烯基,C 2-6亚炔基 等等,R 8是芳基,C 3-8环烷基,C 6-15-15多环烷基等)等; R 和其中X 1是氢)或其药学上可接受的盐或其水合物或溶剂合物,以及含有它们的药物组合物。 这些化合物可用作在给药早期不给予疼痛的预防剂和/或补救剂,其在口服给药中是有效的并且具有有效的镇痛和抗炎作用。
摘要:
The invention provides the following compound (I): wherein R1 is methoxy group, hydroxyl group or hydrogen atom; R2 is hydrogen atom, C1-4 alkyl group, C1-4 alkylcarbonyl group or arylcarbonyl group; D is a group of the following formula (A), (B), or (C). The compound is useful as a medicament for treating neuropathic pain or pain caused by various diseases such as rheumatoid arthritis and osteoarthritis, and inflammation.
摘要:
The invention provides the following compound (I): wherein R1 is methoxy group, hydroxyl group or hydrogen atom; R2 is hydrogen atom, C1-4 alkyl group, C1-4 alkylcarbonyl group or arylcarbonyl group; D is a group of the following formula (A), (B), or (C). The compound is useful as a medicament for treating neuropathic pain or pain caused by various diseases such as rheumatoid arthritis and osteoarthritis, and inflammation.
摘要:
1-�.omega.-(3,4-Dihydro-2-naphthalenyl)alkyl!cyclic amine derivative of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are H, halogen, OH, alkyl, alkoxy, hydroxymethyl, etc., or R.sup.1 and R.sup.2 combine to form methylenedioxy, trimethylene, etc., R.sup.3 is H, etc., R.sup.4 is H, OH, alkyl, etc., R.sup.5 is H, alkyl, etc., p is integer of from 2 to 6, and q is integer of from 3 to 7, provided that when p is 2, and q is 5, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are not simultaneously H, or salts thereof, or N-oxide derivatives thereof, or a process for preparing the same, or pharmaceutical composition containing the same. The compounds of the present invention show potent inhibitory effect on the micturition reflex, and are useful as agents for treatment of frequent urination and urinary incontinence.
摘要:
Compounds of the formula: ##STR1## wherein R.sub.1 represents fluorine atom at the para position, chlorine atom at the para position, methyl group at the para position or trifluoromethyl group at the para or meta position; and R.sub.2 represents hydrogen atom, methyl group, ethyl group, 2-hydroxyethyl group or 3-hydroxypropyl group, provided that R.sub.2 represents ethyl group, 2-hydroxyethyl group or 3-hydroxypropyl group when R.sub.1 represents fluorine atom at the para position, methyl group at the para position or trifluoromethyl group at the para position, and a pharmaceutically acceptable salt therof, process for the preparation thereof, and pharmaceutical composition containing the same. The compounds and pharmaceutically acceptable salts thereof show excellent cytoprotective effect and useful for prophylaxis and treatment of peptic ulcer and inflammatory gastrointestinal diseases.
摘要:
Use of a compound of the formula: ##STR1## wherein R is hydrogen atom or ethyl group, or a pharmaceutically acceptable salt thereof for prophylaxis and/or treatment of peptic ulcer, and a method for prophylaxis and/or treatment of peptic ulcer disease which comprises administering an effective amount of the above-mentioned compound to warm blooded aninal, especially human. Said active compounds have excellent pharmacological activities such as inhibition of ulceration and inhibition of gastric secretion, and hence, are useful as an anti-peptic ulcer agent.
摘要:
Novel 2-cyclic amino-2-(1,2-benzisoxazol-3-yl)acetic acid derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 is a lower alkyl group, Am is a 5- to 9-membered saturated cyclic amino group which may be substituted by a lower alkyl group, and the group: ##STR2## binds to the piperidine moiety at 3- or 4-position of the latter, and their pharmaceutically acceptable acid addition salts and quaternary ammonium salts, process for their preparation, and pharmaceutical compositions containing these compounds. They have potent anticholinergic antispasmodic activity, while they are weak in side effects such as mydriasis, inhibition of salivary secretion and tachycardia.