摘要:
##STR1## The present invention is directed to a class of novel carbocyclic derivatives having formulas (I) and (II) and their use as anti-viral and anti-neoplastic agents, wherein X 1 and X 2 are each independently hydrogen, fluorine, or chlorine, R is hydrogen or hydroxymethyl, J is a radical of formulas (a), (b) and (c). Y 1 is a CH group, a CCl group, a CBr group or a CNH 2 group, Y 2 and Y 3 are each independently nitrogen or a CH group, Y 1 is a CH group, a CCl group, a CBr group or a CNH 2 group, Y 2 and Y 3 are each independently nitrogen or a CH group, Y 4 is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy or halogen, Y 5 is NH 2 or C 1 -C 4 alkoxy, Q is NH 2 , NHOH, NHCH 3 , OH, or hydrogen, and V is hydrogen, halogen or NH 2 ; or a pharmaceutically acceptable salt thereof.
摘要:
Aryloxyalkanol derivatives having the formulaAr--O(CH.sub.2).sub.n OHwherein n is an integer from 3 to 8 and Ar is (1) 1- or 2-naphthylenyl, (2) phenyl optionally substituted by from 1 to 3 C.sub.1-4 lower alkyl groups, or (3) a diphenyl moiety of structure ##STR1## wherein Y is a bond, CH.sub.2 or CH.sub.2 O, and esters thereof have antiretrovirus activity and are effective in a method for treating a retrovirus infection.
摘要:
This invention relates to pyridinyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.
摘要:
Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used to control the growth of tumor tissue and can be used as antigout agents.
摘要:
Certain Castanospermine ester derivatives of the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are each independently hydrogen, C.sub.1-14 alkanoyl, C.sub.1-14 alkenoyl, cyclohexanecarbonyl, C.sub.1-8 alkoxyacetyl, ##STR2## naphthalenecarbonyl optionally substituted by methyl or halogen; phenyl (C.sub.2-6 alkanoyl) wherein the phenyl is optionally substituted by methyl or halogen; cinnamoyl; pyridinecarbonyl optionally substituted by methyl or halogen; dihydropyridine carbonyl optionally substituted by C.sub.1 -C.sub.10 alkyl; thiophenecarbonyl optionally substituted by methyl or halogen; or furancarbonyl optionally substituted by methyl or halogen; Y is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylmercapto, cyano or dimethylamino; Y' is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or it is combined with Y to give 3,4-methylenedioxy; Y" is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen; with R, R.sub.1 and R.sub.2 being selected in such a way that at least one of them, but not more than two of them, is hydrogen; are disclosed to be effective in treating diseases caused by Herpes Simplex Virus (HSV) Types 1 and 2.
摘要:
This invention relates to quinolyloxazole-2-ones which are useful in the treatment of multi-drug resistant tumors. The quinoloyloxazole-2-ones act to prevent drug resistance and thus allow conventional chemotherapeutic agents to kill tumor cells as if drug resistance were not present.
摘要:
This invention relates to quinolyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.
摘要:
Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used as antigout agents. The chalcone derivatives are also reported to inhibit the destruction of the myelin sheath in the central nervous system of multiple sclerosis patients and are thus useful in controlling the progressive nature of the disease.
摘要:
Diarylalkyl piperidines of formula (1) ##STR1## reverse drug resistance in multi-drug resistant tumors. These compounds apparently function by inhibiting a p-glycoprotein pump which becomes activated in late stage tumor development and which is inherently present in tumors from certain origins.