摘要:
The present invention relates to an androgen receptor alkylating compound, wherein the compound may include, inter alia, an active functional group, which permits the alkylation of the androgen receptor.
摘要:
There is disclosed a novel class of sulphonamido-substituted bridged bicycloalkyl derivatives comprising a substitute on the bridgehead position. The compounds modulate the production of the null-amyloid precursor protein, and hence are useful in the treatment of Alzheimer's Disease.
摘要:
The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. 1 Wherein Z represents a bivalent organic group and the like of from 2 to 3 carbon atom(s) which may have a substituent; and R3 represents a carboxyl group and the like.
摘要翻译:本发明提供一种新兴化合物,其表现出对由游离基引起的细胞损伤的抑制作用和由兴奋性转运剂如谷氨酸诱导的神经毒性。 具体地,它提供由下式表示的化合物,其盐或它们的水合物。 其中Z表示可以具有取代基的2〜3个碳原子的二价有机基团等; R 3表示羧基等。
摘要:
Compounds of Formula (I) 1 wherein R1, R2, R3, R4, R5, R6, and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要:
Application of topical synergistic microbicide composition(s) of high practical utility both as a treatment and/or prevention against HSV Type 1 and/or Type 2 and related diseases and secondary opportunist disease causing agents, while reducing the inflammation, prolonged healing times and reduce scaring.
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:
The present invention relates to therapeutic protocols and pharmaceutical compositions designed to target HBx mediated activation of Src kinase, members of the Src tyrosine kinase family and components of the Src kinase family signal transduction pathways for the treatment of HBV infection and related disorders and diseases, such as HCC. The invention further relates to pharmaceutical compositions for the treatment of HBV infection targeted to HBx and its essential activities required to sustain HBV replication. The invention is based, in part, on the Applicants' discovery that activation of Src kinase signaling cascades play a fundamental role in mammalian hepadnavirus replication. Applicants have demonstrated that HBx mediates activation of the Src family of kinases and that this activation is a critical function provided by HBx for mammalian hepadnavirus replication.
摘要:
Use of cathepsin S inhibitors for the treatment of an allergic condition, in particular an atopic allergic condition, more specifically for the treatment of hay fever, asthma, atopic dermatitis or a food allergy.
摘要:
The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a 1 in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endothelial dysfunction, and organ hypertrophies and hyperplasias. They are inhibitors of the cellular sodium/proton antiporter. They have an influence on serum lipoproteins and can therefore be used for the prophylaxis and regression of atherosclerotic changes.
摘要:
This invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase disphoric disorder (premenstrual syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula: 1 in which A is a moiety of the formula 2 where the dotted line represents optional unsaturation; R1 is hydrogen or alkyl; R2 is alkyl; R4 is hydrogen, alkyl, formyl, or alkanol; R5 and R6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy; R7 is hydrogen or alkyl; and n is 0, 1, 2, 3, or 4; or a pharmaceutically acceptable salt thereof.
摘要翻译:本发明提供一种治疗肥胖症,广泛性焦虑症,创伤后应激障碍,晚黄体期无症状(经前期综合征),注意缺陷障碍,伴有和不伴有多动症的方法,Gilles de la Tourette综合征,神经性贪食症或Shy Drager综合征 在哺乳动物中通过向哺乳动物施用有效量的以下结构式的羟基环烷基苯乙胺:其中A是下式的部分,其中虚线表示任选的不饱和度; R1是氢或烷基; R2是烷基; R4是氢,烷基,甲酰基或烷醇; R 5和R 6独立地是氢,羟基,烷基,烷氧基,烷酰氧基,氰基,硝基,烷基巯基,氨基,烷基氨基,二烷基氨基,烷酰氨基,卤素,三氟甲基或一起,亚甲基二氧基; R7是氢或烷基; 且n为0,1,2,3或4; 或其药学上可接受的盐。