Abstract: Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well as those using compounds that are inhibitors of only one specific NHE. Advantageous screening techniques and assays for evaluating a compound's therapeutic activity are also disclosed.

Abstract: This invention discloses compounds useful as steroid sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R is selected from the group consisting of hydrogen, a lower alkyl group, an alkoxy group, halogen, NH.sub.2, NO.sub.2, C.tbd.N and N.dbd.C.dbd.S; and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The compounds also comprise the formula (5) ##STR2## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1 -C.sub.

Abstract: Polymorph "A" a novel polymorphic form of N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid. Novel processes for preparing polymorph "A" are also disclosed.

Abstract: Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well as those using compounds that are inhibitors of only one specific NHE. Advantageous screening techniques and assays for evaluating a compound's therapeutic activity are also disclosed.

Abstract: Vitamin D.sub.3 analogues of formula ##STR1## wherein R represents a 1-hydroxyalkyl group or 1-fluoroalkyl group in a trans- configuration with a 3-hydroxyl group on the A ring and R.sup.2 represents the substituents completing a vitamin D.sub.3 analogue. These novel compounds are potent anti-proliferative substances with activities comparable to that of calcitriol but with vitamin D.sub.3 receptor binding ratings of less than 10.sup.-3 compared to that of calcitriol.

Abstract: Compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, and are as defined herein, their use as antiinflammatory, immunosuppressive, and antiallergic agents, pharmaceutical compositions comprising them, and methods for their preparation comprising irradiating compounds of formula II ##STR2## under an inert atmosphere, in the presence or absence of a compound of formula R.sub.3 --S--S(O).sub.m --R.sub.8, where R.sub.7, R.sub.8, and m are as defined herein, and methods for their preparation comprising oxidizing, reducing, halogenating, or alkylating compounds of formula I are disclosed.

Abstract: Novel 17-hydroxyiminoalkyl and 17-hydroxyiminomethylalkenyl steroids of the general formula (I) ##STR1## where A, R.sup.1 and R.sup.2 are defined in the specification are disclosed. The compounds have cardiovascular activity. Pharmaceutical compositions containing compounds of formula (I) are also disclosed for the treatment of heart failure and hypertension.

Abstract: Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to ether of the foregoing, are utilized for the treatment and/or prevention of vaginal atrophy, hyprogonadism, diminished libido, osteoporosis, urinary incontinence, ovarian cancer, uterine cancer, skin atrophy, for contraception, and, in combination with an estrogen and/or progestin, for the treatment of menopause. The precursors may be formulated for percutaneous or transmucosal administration. Gels, solutions, lotions, creams, ointments and transdermal patches for the administration of these precursors are provided, as are certain pharmaceutical compositions and kits which can be used for the prevention and treatment of a wide variety of conditions related to decreased secretion of sex steroid precursors by the adrenals.

Abstract: The invention is drawn to a process for isolating and purifying a phytosterol composition from a pulping soap by first extracting a creamy precipitate from the pulping soap using a solvent mixture of water, ketone, and hydrocarbon, and then purifying the cremy precipitate to form the phytosterol composition. The invention also includes the phytosterol composition formed by this method.

Abstract: The disclosure is of methods of treating various skin disorders, including skin cancer, with compounds of novel 1.alpha.-hydroxy vitamin D.sub.4 and novel analogues, thereof, including 1,25 dihydroxy vitamin D.sub.4 and 1,24 dihydroxy vitamin D.sub.4. Novel 1.alpha.-hydroxy vitamin D.sub.4 compounds and compounds of novel analogues suitable for use in the treatment of such disorders are also disclosed herein.

Abstract: A method of treating a viral infection includes administering an effective amount of a compound having the following structure: ##STR1## or a pharmaceutically acceptable salt thereof. This compound treats the viral infection by suppressing the growth of a viral target cell. As one specific example, this compound may be used to treat HIV infection.

Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.

Abstract: 1.alpha.-Hydroxy-24-epi-vitamin D.sub.4 and novel intermediates formed in a novel method of preparing this compound. The method includes campesterol as a starting material which is converted to 24-epi-vitamin D.sub.4 which is in turn hydroxylated to 1.alpha.-hydroxy-24-epi-vitamin D.sub.4 via tosylated and cyclic derivatives of 24-epi-vitamin D.sub.4. 1.alpha.-Hydroxy-24-epi-vitamin D.sub.4 has been found to be bioactive.

Abstract: Described is a process for the regioselective dehydration of 11-hydroxy steroids using PCl.sub.5, PCl.sub.3, POCl.sub.3 or either SO.sub.2 Cl.sub.2 and imidazole, or PPh.sub.3 and CCl.sub.4. The disclosed process selectively forms .DELTA..sup.9,11 steroids from either 11-.alpha.- or 11-.beta.-hydroxy steroids, and can also be used for the one-step conversion of 11,21 -dihydroxy steroids to 21-chloro-.DELTA..sup.9,11 steroids. Also disclosed are processes for the regioselective conversion of 11-.beta.-chloro steroids to .DELTA..sup.9,11 steroids, and for regioselectively converting an 11,17,21-trihydroxy streoid to a 21-chloro-11,17-dihydroxy steroid.

Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.

Abstract: The invention is drawn to a process for the preparation of a steroid of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and theo A, B, C, and D ring system has at least one double bond and is optionally substituted by at least one optionally protected hydroxy, optionally protected keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms, and alkenyl and alkynyl of 2 to 4 carbon atoms by reacting the corresponding 17-ketosteroid with a compound of the formula ##STR2## and then by reacting the resulting compound with an aryl sulfenyl halide. The intermediate produced then undergoes rearrangement followed by epimerization with a strong base to obtain a mixture of the corresponding sulfoxide diastereoisomers which is reacted with a thiophilic compound. The intermediate produced undergoes acid hydrolysis to provide the compound of formula I.

Abstract: A method of inhibiting angiogenesis in a patient includes administering to the patient an effective amount of squalamine or a pharmaceutically acceptable salt of squalamine. Alternatively, a compound according to the following Formula (III) (or a pharmaceutically acceptable salt thereof) can be administered: ##STR1## wherein Z.sub.5 is .alpha.-H or .beta.-H; each of the substituents Z.sub.7 is selected from the group of --H, --OH, --SH, --NH.sub.2, --F, --(C.sub.1 -C.sub.3)-alkyl, and --(C.sub.1 -C.sub.3)-alkoxy; and one of the substituents Z.sub.12 is --H and the other is --H or --OH. X' is a polyamine side chain of the formula --X.sub.1 --(CH.sub.2).sub.p --X.sub.2 --(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III), wherein one of X.sub.1 and X.sub.2 is --N(R.sup.IV) and the other is selected from the group of --N(R.sup.V), --O, --S, and --CH.sub.2. R.sup.IV and R.sup.V are each --H or --(C.sub.1 -C.sub.3)-alkyl, p and q are each an integer of from 0 to 5 (but both are not 0). R.sup.II and R.sup.

Abstract: 18-nor-vitamin D.sub.3 analogs in which the angular methyl group attached to carbon 13 of the CD-ring has been removed and replaced by a hydrogen atom. The 18-nor vitamin D compounds are characterized by relatively high cell differentiation activity, while exhibiting much lower activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone. These compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis, because of their preferential calcemic activity, and for the treatment of psoriasis due to their cell differentiation activity.

Abstract: 18,19-dinor-vitamin D.sub.3 analogs in which the angular methyl group attached to carbon 13 of the CD-ring and the exocyclic methylene group attached to carbon 10 of the A-ring have been removed and replaced by a hydrogen atom. The 18,19-dinor vitamin D compounds are characterized by relatively high cell differentiation activity, and marked intestinal calcium transport activity while exhibiting lower activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone. These compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis, because of their preferential calcemic activity, and for the treatment of psoriasis due to their cell differentiation activity.

Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.