摘要:
The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represent, a group (V), wherein R′a and R″a are as defined in the description, or R forms with A a cyclic structure as defined in the description; R′ represents a (CH2)t—R2 group wherein q, t, and R2 are as defined in the description. The invention is useful for preparing medicines.
摘要:
The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
摘要翻译:本发明涉及用于治疗例如性功能障碍的式(I)化合物,其中R 1是任选取代的C 1-6烷基,任选取代的碳环基,任选取代的杂环基,氢,C 1-6烷氧基,-NR 2 R 3或-NR 4 SO 2 R 5; X是键 - (CH 2)n - 或 - (CH 2)Q-O-(其中Y连接至氧); 其中连接X中的一个或多个氢原子可以被C 1-4烷氧基独立地取代; 羟基; 羟基(C 1-3烷基); C 3-7环烷基; 碳环基 杂环基 或被任选被一个或多个氟或苯基取代的C 1-4烷基; n为3,4,5,6或7; q为2,3,4,5或6; Y为苯基或吡啶基,各自可以被取代; 或相邻碳原子上的两个R 8基团与互连碳原子一起可以形成稠合的任选取代的5或6元碳环或杂环基。
摘要:
A photoactivatable reagent useful as a chain transfer reagent for providing a semitelechelic polymer having one or more terminal photoactivatable groups. The reagent provides one or more photoactivatable groups and one or more sulfhydryl (or other chain transfer) groups, the photoactivatable and chain transfer groups optionally being joined together by a spacer group. The reagent can be used to prepare a polymer by serving to initiate the polymerization of ethylenically unsaturated monomers. The reagent itself becomes an integral part of the resultant polymer, thereby providing the polymer with a terminal photoactivatable nature. The method provides a number of benefits, including the ability to provide homogeneous photoactivatable polymer compositions, e.g., in terms of the uniform location of the photogroup(s) on the terminal portion of each polymer molecule and the ability to build a desired nonpolar quality, and in turn improved surfactancy, into otherwise polar polymers.
摘要:
Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
摘要翻译:公开了由式(I)表示的三环化合物:其中R 1,R 2,R 3和R 4各自独立地表示氢,C 1-6烷基,C 1-6烷氧基,C 1-6烷硫基,氨基, C 1-6烷基氨基,卤代C 1-6烷基,卤代C 1-6烷氧基,卤素,硝基,氰基,羧基,C 1-6烷氧基羰基,羟甲基,CR 9 R 10 CO 2 R 11(其中R 9,R 10和R 11各自独立地表示氢或C 1-6烷基 )或CONR 12 R 13(其中R 12和R 13各自独立地表示氢或C 1-6 - 烷基); R5表示氢或C1-6烷基; R 6,R 7和R 8各自独立地表示氢,C 1-6烷基,羟基,C 1-6烷氧基,C 1-6烷酰氧基,C 1-6烷硫基,氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O,CH2-S(O)n,(其中n表示0,1或2),CH2CH2,CH = CH或CON(R14)(其中R14表示氢或C1-6烷基) Z表示氧或硫,或其药学上可接受的盐。 该化合物具有酰基辅酶A:胆固醇酰基转移酶抑制活性,因此预期对高脂血症和动脉硬化具有预防和治疗作用。
摘要:
Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
摘要:
A substituted cycloalkyl- or heterocyclyl-carboxanilide of the formula (I) ##STR1## in which X stands for an unsubstituted or an alkyl-substituted cycloalkyl or an unsubstituted or an alkyl-substituted heterocyclic,Hal stands for halogen andY.sup.1, Y.sup.2 and Y.sup.3 independently of one another stand for hydrogen, halogen, an unsubstituted or a halogen-substituted alkyl, an unsubstituted or a halogen-substituted alkoxy or an unsubstituted or a halogen-substituted alkylthio. Such substituted cycloalkyl- or heterocyclyl-carboxanilides are useful as fungicides.
摘要:
The present invention involves compounds having the structure: ##STR1## wherein: (a) --A.sup.1 is selected from the group consisting of --OH, --H, and --O.sub.2 CR;(b) --A.sup.2 is selected from the group consisting of unsubstituted or substituted, saturated or unsaturated, straight, branched and cyclic alkyl having from 1 to about 10 carbon atoms;(c)--A.sup.3 is selected from --C(CH.sub.3).sub.3, --Si(CH.sub.3).sub.3, and --CF.sub.3 ; and(d) --Y is selected from certain low molecular weight alkyl chains which terminate in specific unsaturated functional groups: ##STR2## and aldehydes in the form of their acetals; pharmaceutical compositions comprising such compounds; and methods for treating inflammation by administering such compounds.
摘要:
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
摘要:
The present invention provides a process for preparation of Vortioxetine hydrobromide (I). The present invention also relates to the novel intermediate and its use in preparation of vortioxetine hydrobromide (I).
摘要:
Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus. The compounds have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein W1, W2, X, R1, R2, R3, R4, m and n are defined herein.
摘要翻译:用于改变胰岛素分泌的化合物,组合物和方法,特别是在治疗具有或怀疑患有糖尿病风险的受试者的情况下。 该化合物具有以下结构(I):包括其立体异构体,前药和药学上可接受的盐,其中W 1,W 2,X,R 1, R 2,R 2,R 3,R 4,m和n在本文中定义。