Abstract: Rapamycin derivatives; pharmaceutical compositions comprising such rapamycin derivatives and pharmaceutically acceptable carriers or diluents; and methods of using such derivatives to inhibit pathogenic fungi growth inhibition, inhibit immunosuppression or treat carcinogenic tumors are disclosed.

Abstract: A compound of formula (I) is obtainable by the cultivation of a genus Streptomyces, such as Streptomyces NCIMB 40515. in the presence of rapamycin, and recovery thereof from the culture medium. The compound, and pharmaceutical compositions containing it, is useful as an immunomodulatory agent as an anticancer agent, or in the treatment of microbial infections in animals including humans.

Abstract: The present invention provides a process for the asymmetric synthesis of camptothecin analogues as well as novel chemical intermediates of Formula I, II, and III. In general, the present process comprises conversion of a cis dioxolanone, having the same desired absolute configuration as the desired camptothecin analogue, to a compound of Formula I, II, or III, which compound is then converted to the desired camptothecin analogue.

Abstract: A method of treating ovarian cancer in a human afflicted therewith which comprises administering to such human an effective amount of a compound of the water soluble camptothecin analog class.

Abstract: The present invention provides water soluble camptothecin analogs of Formula I: ##STR1## which are particularly useful as antineoplastic agents; pharmaceutical compositions thereof; and a method of treating cancer in an animal in need thereof, including human beings, comprising inhibition of the growth of tumor cells in said animal by administration of an effective amount of a compound of Formula I.

Abstract: The present invention provides a water soluble camptothecin analog of Formula I: ##STR1## which is particularly useful as an antineoplastic agent; pharmaceutical compositions thereof; and a method of treating cancer in an animal in need thereof, including human beings, comprising inhibition of the growth of tumor cells in said animal by administration of an effective amount of a compound of Formula I.

Abstract: Rapamycin derivatives of formula ##STR1## pharmaceutical compositions comprising such rapamycin derivatives and pharmaceutically acceptable carriers or diluents; and methods of using such derivatives to inhibit pathogenic fungal growth, cause therapeutically desirable immunosuppression, or treat carcinogenic tumors are disclosed.

Abstract: Rapamycin derivatives; pharmaceutical compositions comprising such rapamycin derivatives and pharmaceutically acceptable carriers or diluents; and methods of using such derivatives to inhibit pathogenic fungi growth, inhibit immunosuppression or treat carcinogenic tumors are disclosed.

Abstract: A pharmaceutical composition comprising a compound of the camptothecin analog class and a platinum coordination compound and a pharmaceutically acceptable carrier or diluent; a method of inhibiting the growth of tumor cells in a human afflicted therewith which comprises administering to such human an effective tumor cell growth inhibiting amount of such pharmaceutical composition; and a method of inhibiting the growth of tumor cells in a human afflicated therewith which comprises administering to such human an effective tumor cell growth inhibiting amount of the combination of a compound of the camptothecin analog class and a platinum coordination compound.

Abstract: The present invention provides a process for the asymmetric synthesis of camptothecin analogues as well as novel chemical intermediates of Formula I, II, and III. In general, the present process comprises conversion of a cis dioxolanone, having the same desired absolute configuration as the desired camptothecin analogue, to a compound of Formula I, II, or III, which compound is then converted to the desired camptothecin analogue.

Abstract: A new use of, and method of treatment of atherosclerosis using, a compound selected from the group consisting essentially of compounds of Formula I: ##STR1## wherein: R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl;R.sub.2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl;R.sub.3 is hydrogen or lower alkyl of up to 6 carbon atoms;R.sub.4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2, oxygen or sulfur;Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH.sub.

Abstract: This invention relates to a new antioxidant use of, and method of treatment using certain hydroxycarbazole compounds or a pharmaceutically acceptable salt thereof. More specifically, the compounds are useful for the prevention of oxidative tissue damage to organs, particularly the central nervous system including the brain, in mammals afflicted with disease-induced ischemic trauma, particularly stroke.

Abstract: The present invention provides a process for the asymmetric synthesis of camptothecin analogues as well as novel chemical intermediates of Formula I, II, and III. In general, the present process comprises conversion of a cis dioxolanone, having the same desired absolute configuration as the desired camptothecin analogue, to a compound of Formula I, II, or III, which compound is then converted to the desired camptothecin analogue.

Abstract: The present invention provides a new medical use of the hydroxycarbazole compounds of Formula (I), preferably the hydroxylated metabolites of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol)(carve dilol), for inhibiting the migration and proliferation of smooth muscle cells. In particular, the present invention provides a new use for the hydroxycarbazole compounds of Formula (I) for prevention of restenosis following percutaneous transluminal coronary angioplasty (PTCA), suppression of the progression of vascular hypertrophy associated with hypertension, and prevention of development of atherosclerosis. ##STR1## wherein: R.sub.1 -R.sub.9 are independently --H or --OH, with the proviso that a at least one of R.sub.1 -R.sub.9 is OH.

Abstract: Rapamycin derivatives; pharmaceutical compositions comprising such rapamycin derivatives and pharmaceutically acceptable carriers or excipients; and methods of using such derivatives to inhibit pathogenic fungi growth inhibition, inhibit immunosuppression or treat carcinogenic tumors are disclosed.

Abstract: The present invention provides antiviral compounds of Formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein X is --CH.sub.2 O or --CH.sub.2 ;R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl, wherein the acyl group of said acyloxymethyl is selected from the group consisting of C.sub.1-7 alkanoyl and benzoyl optionally substituted in the phenyl ring by one, two or three substituents selected from the group consisting of fluoro, chloro, bromo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, wherein the alkyl moiety of said C.sub.1-4 alkyl and C.sub.1-4 alkoxy substituents is selected from the group consisting of methyl, ethyl, n- and iso-propyl, n-, sec-, iso- and tert-butyl,R.sub.4 is a group of formula: ##STR2## wherein R.sub.5 and R.sub.6 are independent selected from hydrogen, C.sub.1-6 alkyl and phenyl optionally substituted by one, two or three substituents selected from the group consisting of fluoro, chloro, bromo, C.sub.

Abstract: A compound of formula (I) ##STR1## or a salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, acyl or phosphate, provided that when one of R.sub.1 or R.sub.2 is phosphate, the other is hydrogen; or R.sub.1 and R.sub.2 are joined together to form a cyclic acetal group, a cyclic carbonate group or a cyclic phosphate group.Processes for preparing these compounds and their use in therapy is also described.

Abstract: The present invention provides antiviral compounds of Formula (I): ##STR1## pharmaceutical compositions prepared therefrom, and methods of treatment of viral infections therewith.

Abstract: A process for the preparation of 2,5-diamino-4,6-dichloropyrimidine, which process comprises the chlorination of 2,5-diamino-4,6-dihydroxypyrimidine with phosphorus oxychloride and a quaternary ammonium chloride or a weak tertiary amine base hydrochloride.

Abstract: A method for making 8-methyl-7-(1-oxopropyl)indolizino[1,2-b]quinolin-9(11H)-ones from 4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-3,14(4H,12 H)-diones, said method being graphically illustrated as follows: ##STR1##