摘要:
This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.
摘要:
The present invention relates to N-1-Benzyl-2-hydroxy-3-(hetero)arylamino-propyl)-isophthalamides of formula I having BACE2 inhibitory activity and their use as therapeutically active substances, their manufacture and pharmaceutical compositions. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. type 2 diabetes.
摘要:
The present invention provides a compound comprising the structure shown in Formula I for use in delivering a therapeutic nucleic acid, one or more drug agents, or a biologically active agent to a cell,
R 3 -(C=O)-Xaa-Z-R 4 Formula I
wherein Xaa is histidine, 1-methylhistidine, pyridylalanine, lysine, arginine, homoarginine, nor-norarginine, ornithine, homolysine, asparagine, N ethylasparagine, glutamine, 4-aminophenylalanine, and nor-arginine, or an N-methylated version thereof; R 3 is independently a lipophilic tail derived from a naturally-occurring or synthetic lipid, phospholipid, glycolipid, triacylglycerol, glycerophospholipid, sphingolipid, ceramide, sphingomyelin, cerebroside, or ganglioside, wherein the tail may contain a steroid; or a substituted or unsubstituted C(3-22)alkyl, C(6-12)cycloalkyl, C(6-12)cycloalkyl-C(3-22)alkyl, C(3-22)alkenyl, C(3-22)alkynyl, C(3-22)alkoxy, or C(6-12)alkoxy-C(3-22)alkyl; R 4 is independently a lipophilic tail derived from a naturally-occurring or synthetic lipid, phospholipid, glycolipid, triacylglycerol, glycerophospholipid, sphingolipid, ceramide, sphingomyelin, cerebroside, or ganglioside, wherein the tail may contain a steroid; or a substituted or unsubstituted C(3-22)alkyl, C(6-12)cycloalkyl, C(6-12)cycloalkyl-C(3-22)alkyl, C(3-22)alkenyl, C(3-22)alkynyl, C(3-22)alkoxy, or C(6-12)alkoxy-C(3-22)alkyl; wherein both R 3 and R 4 are lipophilic tails; and Z is NH, O, S, -CH 2 S-, -CH 2 S(O)-, or an organic linker consisting of 1-40 atoms selected from hydrogen, carbon, oxygen, nitrogen, and sulfur atoms; and salts thereof.
摘要:
There are presented compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein Y1,Y2, X1 ,X2, X3 and R are as described in this application. These compounds are believed to inhibit MDM2-p53 interaction and as such the compounds will have anti-hyperproliferative cellular activity.
摘要:
Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要:
The present invention relates to novel N -cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N -oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要:
Amide derivatives represented by general formula (I) or salts thereof wherein each symbol has the following meaning: ring B: an optionally substituted heteroaryl optionally fused with a benzene ring; X: a bond, lower alkylene or lower alkenylene optionally substituted by hydroxy or lower alkyl, carbonyl, or a group represented by -NH- (when X is lower alkylene optionally substituted by lower alkyl which may be bonded to the hydrogen atom bonded to a constituent carbon atom of ring B to form lower alkylene to thereby form a ring); A: a lower alkylene or a group represented by -(lower alkylene)-O-; R?1a and R1b¿: the same or different and each hydrogen or lower alkyl; R2: hydrogen or halogeno; and Z: nitrogen or a group represented by =CH-. The compounds are useful as a diabetes remedy which not only functions to both accelerate the secretion of insulin and enhance insulin sensitivity but has an antiobestic action and an antihyperlipemic action based on its selective stimulative action on a β¿3? receptor.
摘要翻译:由通式(I)表示的酰胺衍生物或其盐,其中每个符号具有以下含义:环B:任选地与苯环稠合的任选取代的杂芳基; X:一个键,任选被羟基或低级烷基取代的低级亚烷基或低级亚烯基,羰基或由-NH-表示的基团(当X是任选被低级烷基取代的低级烷基时,可以键合到与 环B的构成碳原子形成低级亚烷基,从而形成环); A:低级亚烷基或由 - (低级亚烷基)-O-表示的基团。 R 1a和R 1b相同或不同,各个氢或低级烷基; R 2:氢或卤素; 和Z:氮或由= CH-表示的基团。 该化合物可用作糖尿病药物,其不仅可以加速胰岛素的分泌并增强胰岛素敏感性,而且具有抗胆碱作用和基于其对β3受体的选择性刺激作用的抗高脂血症作用。