Abstract: Novel bile acids according to the general formula ##STR1## wherein R.sub.1 represents a hydroxyl group, R.sub.2 and R.sub.3 both represent a hydrogen or a hydroxyl group, or R.sub.2 represents a hydroxyl group or a .beta. hydroxyl group and R.sub.3 represents a hydrogen or R.sub.3 represents a hydroxyl group and R.sub.2 represents a hydrogen, and R.sub.4 represents a (CH.sub.2).sub.n R.sub.5 wherein n is from 1 to 6, and R.sub.5 represents --0--PO(OH).sub.2, --CH(OH)COOH, a nitrogen containing saturated heterocyclic ring group, NR.sub.6 R.sub.7, wherein R.sub.6 and R.sub.7 are the same or different and each represent hydrogen or a C.sub.1 -C.sub.10 alkyl group or CO--R.sub.8 wherein R.sub.8 represents an amino acid moiety, R-phenylglycine, 12-aminododecanoic acid or 4-aminohippuric acid are synthesized from cholic, deoxycholic, chenodeoxycholic, ursodeoxycholic and lithocholic acids and iodo-derivatives thereof by known processes and/or by novel processes according to the present invention.

Abstract: The present invention relates to an oligonucleotide or analog thereof conjugated to a molecule comprising a structure, which structure (a) is of substantially fixed conformation; (b) contains, is directly attached to, or is attached to a carbon atom that is directly attached to, an first amine; and (c) contains, is directly attached to, or is attached to an atom that is directly attached to a phosphate, a second amine, or a cationic sulfur. In a preferred embodiment, the structure consists of at least a nonaromatic cyclic portion or substituted derivative thereof. In a specific embodiment, the structure is a nonaromatic cyclic compound. In another embodiment, the molecule is a steroid. In yet another particular aspect, the structure is an aromatic compound. In another embodiment, the structure can bind to a nucleic acid sequence in a nonintercalative manner.

Abstract: Novel compounds having anti-HIV activity are disclosed along with formulations and methods for treating human immunodeficiency viral infections employing these compounds.

Abstract: A compound represented by the general formula: ##STR1## wherein A-O-denotes a residue of a compound having an estrogenic activity; R.sub.1 denotes H or a C.sub.1 -C.sub.6 alkyl group; X denotes a single bond, a C.sub.1 -C.sub.10 alkylene group or a group of the formula ##STR2## wherein R.sub.2 denotes H or a C.sub.1 -C.sub.5 alkyl group; Z denotes a nitro group or a halogen; n is an integer of 3 to 12; k is an integer of 1 to 5; L is an integer of 0 to 5; and q is an integer of 1 to 3,and physiologically acceptable salts thereof are disclosed.The compounds have a high affinity to bone tissues, and the compounds per se and metabolites thereof show significant therapeutic effect on bone diseases such as osteoporosis, rheumatoid arthritis and osteoarthritis.

Abstract: Asteroid derivative of the general formula: ##STR1## wherein X--O-- represents a residue of steroid compound and --A-- represents --CO[NH(CHR.sup.1).sub.y --(Y).sub.p --CO].sub.m NH--, --CO--(R.sup.2).sub.x --(Z).sub.q --CO--NH--, or --CO--(CH.sub.2).sub.n --. A therapeutic agent to osteopathy comprising the above steroid derivative is also provided.

Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.

Abstract: Encapsulated PI compositions such as liposomes containing plant PI and th use to prevent mitogenic transformation of normal splenic lymphoid cells (including lymphocytes transformed induced by treatment of cells with lipid A) by exposing the cells thereto.

Abstract: Steroids of the formula ##STR1## wherein R.sup.1 to R.sup.4, X and n have the significance given in the description, which lower the intestinal resorption of cholesterol and plasma cholesterol and a process of making same from corresponding steroids having an alcohol residue of the formula --O--X--OH in the 3-position.

Abstract: Described are new agents for treating bone disorders associated with a reduction in bone mass and abnormalities in bone resportion or bone formation including osteoporosis. Paget's disease, bone metastases and malignant hypercalcemia. The agents are hydroxyl containing steroidal hormones, having bone resportion antagonist or bone formation stimulatory activity, covalently linked through the hydroxyl group via a bond hydrolyzable in the human body, e.g. carbamate or carbonate, which is further covalently linked to an amino, or hydroxy substituted alkylidene-1,1-bisphosphonate, through the respective amino or hydroxy group. The alkyl bisphosphonate moiety confers bone affinity. The agent acts by delivering the steroidal hormone directly to the bone target site where it is released for bone resorption antagonist or bone formation stimulatory action by hydrolysis of the hydrolyzable covalent bond.

Abstract: This invention relates to a stereoisomerically pure .DELTA..sup.2 compound of the formula (I): ##STR1## wherein: R.sup.1 is hydrogen or --(C.dbd.O)--R.sup.2, wherein:R.sup.2 is an organic substituent selected from the group consisting of alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkylalkylenes, haloalkyls, aryls, haloaryls and arylalkylenes, and their product by the process of:(a) reacting the 17.beta.-hydroxy group of 17.beta.-hydroxy-5.alpha.-estr-1-en-3-one with dihydropyran to produce the 3-keto-17.beta.-ether;(b) reducing the 3-keto-17.beta.-ether product of step (a) with lithium in ammonia;(c) reacting the product of step (b) with dialkyl chlorophosphate to produce the 3-substituted phosphate;(d) reducing the product of step (c) with lithium and ammonia to produce the .DELTA..sup.2 -protected-17.beta.-ether product;(e) hydrolysis of the produce of step (d) to product the .DELTA..sup.2 -17.beta.-hydroxy compound;(f) oxidizing the 17.beta.

Abstract: The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase.

Abstract: Diacyl phosphatides having a polyunsaturated carboxylic acid at the 2 position are found to have cytotoxic effect against tumor cells. Subject compositions may be employed in vivo or in vitro for inhibiting tumor cell growth, either by themselves or in combination with other cytotoxic drugs. The compositions may be administered as liposomes.

Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase. Also invented are intermediates used in preparing these compounds.

Abstract: 9 alpha, 11 beta and 11 beta-substituted estranes are disclosed which exhibit elevated estrogenic and postcoital contraceptive activities. A process for their manufacture and their use in pharmaceuticals is also disclosed.