摘要:
The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.
摘要:
This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro; m is 1 or 2; X is O or NR.sub.7 ; and R.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.
摘要:
Disclosed are methods for improving various aberrant metabolic indices in mammals including humans by administration of muscarinic (particularly M1) receptor antagonists alone or in combination with prolactin inhibiting compounds. Preferably the administration takes place at a predetermined time (or, if a combination of muscarinic receptor antagonist and prolactin inhibitor is used, at different predetermined times) during a 24-hour period when the administration is effective (or its effect more pronounced). The invention has application in the treatment of lipid and glucose metabolism disorders.
摘要:
The present invention provides a compound having the structure: ##STR1## wherein X, Y, and Z are independently H, Cl, Br, F, OCH.sub.3, I, or an alkyl group having 1 to 6 carbon atoms; and R is ##STR2## wherein n is 0 to 6, X' and Y' are independently H, Cl, F, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, OCH.sub.3, OH, CF.sub.3, OCF.sub.3, NO.sub.2, NH.sub.2, N(CH.sub.3).sub.2, NHCOCH.sub.3, NCS, NHCOCH.sub.2 Br, or N.sub.3, and (CH.sub.2).sub.n, if present, may be substituted with OH, OCH.sub.3, or an alkyl or alkenyl group having 1 to 3 carbon atoms. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier. The present invention further provides a method for treating a disease characterized by a dopamine deficiency which comprises administering to a subject in need of such treatment an amount of the pharmaceutical composition above effective to treat the disease.
摘要翻译:本发明提供具有以下结构的化合物:其中X,Y和Z独立地为H,Cl,Br,F,OCH 3,I或具有1至6个碳原子的烷基; 其中n为0至6,X'和Y'独立地为H,Cl,F,CH 3,C 2 H 5,C 3 H 7,C 4 H 9,OCH 3,OH,CF 3,OCF 3,NO 2,NH 2,N(CH 3) 2,NHCOCH 3,NCS,NHCOCH 2 Br或N 3,和(CH 2)n(如果存在)可以被OH,OCH 3或具有1至3个碳原子的烷基或烯基取代。 本发明还提供包含上述化合物和药学上可接受的载体的药物组合物。 本发明进一步提供一种治疗以多巴胺缺乏为特征的疾病的方法,其包括对需要这种治疗的受试者施用有效治疗疾病的上述药物组合物的量。
摘要:
A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.
摘要:
Disclosed are cationic lipids capable of facilitating transport of biologically active agents into cells, including the transfection of cells by therapeutic polynucleotides, the delivery of antiviral drugs, and the introduction of immunogenic peptides. The cationic lipids, comprising an ammonium group, have the general structure ##STR1## Also disclosed are adducts of these compounds comprising additional cationic sites that enhance the transfective or transport activity. Structure-activity correlations provide for the selection of preferred compounds to be synthesized for this purpose. Compositions disclosed for use of these cationic lipid include formulations for in vitro transfection and pharmaceutical formulations for parenteral and topical administration of therapeutic agents.
摘要:
Novel compounds are disclosed, which are derivatives of 1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]-isoquinolines, represented by general formula (I): ##STR1## as well as pharmaceutical compositions and methods for the treatment of depression in warm-blooded animals, e.g., man. Novel intermediates are also part of the invention.
摘要:
The invention provides compounds of Formula XXIII: wherein R1 is hydrogen, alkyl, acyl, or silyl, R2 is hydrogen, alkyl, benzyl, acyl, or ester, and R3 is hydrogen, alkyl, an aromatic group, azacyclic, carbocycle, aryl, cycloalkyl, heterocycloalkyl, heterocycle, heteroaryl, heteroalkyl, acyl, or ester, as well as derivatives and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.