Abstract: Use of betulinic acid and/or its derivatives for inhibiting and/or preventing angiogenesis is described. Compositions containing betulinic acid derivatives with or without betulinic acid can be used for these purposed.

Abstract: Compounds of the androstane series are described having general formula and solvates thereof, in which R1 represents O, S or NH; R2 individually represents OC(═O)C1-6 alkyl; R3 individually represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; or R2 and R3 together represent where R6 and R7 are the same or different and each represents hydrogen or C1-6 alkyl; R4 and R5 are the same or different and each represents hydrogen or halogen and represents a single or a double bond. These compounds and their solvates have use in medicine as anti-inflammatory or anti-allergic agents.

Abstract: Apoptotic cell death in a fully differentiated, non-dividing cell such as a neuron is caused by an abortive attempt of the cell to re-enter or pass through the mitotic cycle. Therefore, agents which prevent such entry or passage are effective in preventing, or at least delaying, apoptotic cell death and are therefore useful in the treatment of neurodegenerative diseases in general, including stroke, Alzheimer's disease, Parkinson's disease and motor-neuron disease in particular.

Abstract: Androgens and their derivates and analogs, such as anabolic agents, are characterized by at least one substituent or substituent grouping with radical trapping properties.

Abstract: A pharmaceutical composition includes, as an active ingredient, a compound according to formula 1436 as shown in FIG. 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. Various pharmaceutical products may be produced including this pharmaceutical composition. Such pharmaceutical products may be used for the treatment of cancers, such as leukemia; inflammation; arthritis; and viruses, such as HSV. Methods for using the pharmaceutical compositions also are described. In these methods, various diseases are treated or other body functions are activated or inhibited by administering an effective amount of the pharmaceutical composition. For example, inflammation, arthritis, herpes simplex virus, melanoma, and leukemia may be treated by administering an effective amount of the pharmaceutical compositions. Viral replication, weight gain, and growth factor production can be inhibited by administering an effective amount of these pharmaceutical compositions.

Abstract: Methods, compositions, and compounds for modulating the GABA.sub.A receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.

Abstract: The invention relates to a method of alleviating the symptoms of PMS and anxiety. The method comprises nasally administering a steroid which is a human vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.

Abstract: A method and composition for topically treating non-metastasizing skin eruptions of warts with tazarotene in a suitable pharmaceutical composition. The compositions can include corticosteroids or fluorouracil.

Abstract: The pharmaceutical compositions including a slightly soluble drug incorporated in a water-swellable, but water-insoluble cross-linked polymer, a surface active agent, and an oil show much improved dissolution and, consequently, bioavailability in respect of the drug as is or used with a polymeric carrier of said type.

Abstract: A method for preventing tissue damage associated with graft-versus-host disease in a patient having undergone hematopoietic cell transplantation, and host-versus-graft disease in a patient having undergone organ allograft transplantation. The method includes orally administering to the patient a prophylactically effective amount of a topically active corticosteroid, such as beclomethasone dipropionate, for a period of time following hematopoietic cell or organ allograft transplantation, and prior to the presentation of symptoms associated with graft-versus-host disease or host-versus-graft disease. Representative tissues includes tissue of the intestine and liver, while representative tissue damage includes inflammation thereof.

Abstract: The present invention provides a composition for attracting termites containing a steroid derivative of formula I ##STR1## The present invention also provides a method for attracting or controlling termites with the composition.

Abstract: The present invention provides:the new use of compositions of morphine and compounds of Formula II wherein ##STR1## R.sup.1 is H or Me, preferably H; R.sup.2 is OH, preferably in alpha conformation;R.sup.3 is H;or R.sup.2 and R.sup.3, taken together, are O;R.sup.4 is H or Me, preferably Me and preferably in alpha conformation;R.sup.5 is H;R.sup.6 is H;or R.sup.5 and R.sup.6, taken together, are O;R.sup.7 is H or Me, preferably H;R.sup.8 =H,OH,OAc,SH,SAc,Cl,Br,Fincluding solvates thereof, pharmaceutically acceptable derivatives thereof, prodrugs thereof, tautomers thereof, isomers thereof, and metabolites thereof.

Abstract: The invention provides a method for the treatment and prevention of urinary incontinence in mammals, e.g., human males and females, especially nonpregnant female mammals, by administering a nitric oxide synthase substrate and/or nitric oxide donor, alone or in combination with an estrogenic agent and/or a progestational substance, with or without supplementation with an alpha-adrenergic agonist, beta-adrenergic receptor blocking agent, cholinergic-receptor blocking compound or a cholinergic-receptor-stimulating drug, as well as pharmaceutical compositions useful in practicing the methods of this invention.

Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a pregnane or cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.

Abstract: The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active compounds are alkyl 17.alpha.-dichloroacetoxy-11.beta.-hydroxyandrosta-1,4-dien-3-one-17.beta. -carboxylates and related androstenes.

Abstract: Novel angiostatic .DELTA..sup.4,9(11) -steroids (I), ##STR1## C.sub.21 -oxygenated steroids (II) and other known steroidal compounds have been found to be useful in treating angiogenesis in mammals who have a need for the same. These steroids are useful in treating diseases of neovascularization such as cancer, diabetes and arthritis.

Abstract: One or more formulations for treating psoriasis and other skin disorders characterized by redness, itching, flaking, scaling, and plaque-type growth. The formulation includes a carrier component, one or more active ingredient components, and a surfactant component. The carrier preferably includes an alcohol in substantially equal volume with isopropyl myristate. The active ingredient component preferably includes a superpotent or high-potency corticosteroid such as clobetasol propionate, an anti-flaking ingredient such as zinc pyrithione, or a combination of the two. It may also include an anti-fungal compound. The surfactant component preferably includes an alkyl sulfate such as sodium lauryl sulfate. The formulations made by applied topically either in spray form or as a direct-contact liquid.

Abstract: The invention discloses 3-ketosteroids of the following formula used to inhibit steroid C.sub.17-20 lyase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropyloxy, cyclopropylamino, acetylthioalkane, 2,2-dimethyldioxolan4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkylthiol;R.sub.1 is hydrogen, hydroxy or C.sub.1-6 alkyl;R and R.sub.1 together may indicate .dbd.O, that is an oxygen double bonded to the 17 carbon;R.sub.2, R.sub.3, and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 and R.sub.6 are each independently hydrogen or OH;R.sub.5 and R.sub.6 together may indicate .dbd.O, that is an oxygen double bonded to the 11 carbon;R.sub.7 is hydrogen or C.sub.1 -C.sub.8 alkyl;R.sub.8 is C.sub.1 -C.sub.8 alkyl; andwith the proviso that, when R is OH, then R.sub.1 is hydrogen; andwith the proviso that, when R.sub.5 is OH, then R.sub.6 is hydrogen.

Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a 19-nor pregnane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.

Abstract: The topical application to the ocular surface or adjacent regions of the eye of a preparation containing a therapeutically effective amount of an androgen or androgen analogue or a therapeutically effective amount of TGB-.beta. is disclosed as a method of relieving the chronic and acute manifestation of dry eye signs and symptoms in keratoconjunctivitis sicca (KCS), for example in Sjogren's syndrome. Measurement of the increased tear levels of TGF-.beta. is disclosed as a diagnostic test to monitor the therapeutic effect of topical treatment with androgen or androgen analogues.

Abstract: A method of improving the productivity of a ruminant animal comprising administering to said animals an effective amount of an ecdysone compound.

Abstract: A pharmaceutical composition for trans-mucosal or transdermal administration wherein a per-C.sub.2-18 acylated cyclodextrin is used as a drug reservoir or carrier. The composition can be used safely and exhibits excellent drug release behavior.

Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.

Abstract: The present invention provides an external therapeutic composition for dermatitis comprising an aqueous solution including a therapeutically effective amount of an adrenal cortical steroid, a cyclodextrin, polysaccharides, and a carrier such as water, prepared by clathrating the adrenal cortical steroid in the cyclodextrin using a homomixer to form a clathrate, and adding the clathrate to an aqueous solution of polysaccharides, while being stirred uniformly, to dissolve the clathrate in the aqueous solution, as well as a method for the treatment of dermatitis in a mammalian subject, which comprises administering to said subject a therapeupically effective amount of the external therapeutic composition for dermatitis described above. The external therapeutic composition for dermatitis according to the present invention is extremely safe and can cure dermatitis such as an atopic dermatitis or the like without side effects.

Abstract: The present invention is directed to a method of conferring protection on a population of cells associated with an ischemic focus, in subject, comprising:(a) providing an estrogen compound having insubstantial sex-related activity; and(b) administering an effective cumulative amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Also directed is a method of treating a myocardial infarct in a subject and an ischemic event with the above combination.

Abstract: The 17.alpha.-cyanomethylestra-4,9-diene derivative compounds are of formula I: ##STR1## wherein R.sub.1 is an alkyl group having from 1 to 2 carbon atoms; R.sub.2 is an alkyl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms or a trialkylsilyl group; and R.sub.3 is an oxygen atom or a R--O--N group, wherein R is a hydrogen atom, an acyl group with 1 to 10 carbon atoms, an alkyl group with 1 to 10 carbon atoms, a sulfamoyl group, an alkylsilyl group or a trialkylsilyl group. These compounds, particularly in combination with at least one suitable estrogen, are suitable for treatment of endometrioses or gestagen-dependent tumors and for hormonal contraception and climacteric hormone replacement therapy (HRT). Processes for making the new steroids are described as well as methods of making the pharmaceutical compositions containing them.

Abstract: Provided are active esters of carboxy polysaccharides and semisynthetic derivatives of carboxy polysaccharides, wherein all or part of the carboxy groups thereof are esterified with an aromatic alcohol, a substituted aromatic alcohol, an aromatic heterocyclic alcohol, a substituted aromatic heterocyclic alcohol, an N-hydroxylamine, or a combination thereof. Also provided is a process for producing such active esters. These active esters can be used for the preparation of modified carboxy polysaccharides or modified semisynthetic derivatives of such carboxy polysaccharides, in the form of esters, thioesters, or amides. Such active esters, modified polysaccharides, and modified semisynthetic derivatives of carboxy polysaccharides can be used in the biomedical and pharmaceutical fields to prepare, for example, cosmetic articles, health care articles, surgical articles, and diagnostic kits.

Abstract: Apoptotic cell death in a fully differentiated, non-dividing cell such as a neuron is caused by an abortive attempt of the cell to re-enter or pass through the mitotic cycle. Therefore, agents which prevent such entry or passage are effective in preventing, or at least delaying, apoptotic cell death and are therefore useful in the treatment of neurodegenerative diseases in general, including stroke, Alzheimer's disease, Parkinson's disease and motor-neuron disease in particular.

Abstract: The present invention relates to a pharmaceutical composition or preparation which comprises hydroxyl containing steroidal hormones and organic nitrite/nitrate or other nitric oxide donating agents.

Abstract: 17-Deoxycorticoid-21-carboxylic esters of the formula I ##STR1## are described, in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl and R(2) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(4) is OH, with an activated carboxylic acid of the formula III,R(5)-CO--X-R(1) III.The compounds I possess very strong local and topical antiinflammatory activity and exhibit a very good ratio of local to systemic antiinflammatory effect, which ratio is often clearly superior to that of structurally related corticoid 21-esters which do not carry any aryl or hetaryl group in the 21-ester residue or to that of analogous 17-deoxycorticoids having an unesterified, that is a free, 21-hydroxyl group.

Abstract: The invention relates to the preparation and struction of a kind of pharmaceutical base comprising 5% to 25% by weight of beeswax and 95% to 75% by weight of a hydrophobic solvent. The pharmaceutical base has a netted framework structure with beeswax being the frame and the hydrophobic solvent being included in the frame. Also, the present invention relates to pharmaceutical compositions, dressing and cosmetics prepared by using the base and the method for preparing the same.

Abstract: Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition is a unit dosage in the form of a tablet that comprises about 0.01% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 98% by weight of a hydrocolloid gum obtainable from higher plants; and about 2% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating lower GI disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.

Abstract: The invention describes a method and composition for treating obesity or related disorders in animals using an anorectic agent and dehydroepiandrosterone (DHEA). The composition effectively diminishes caloric intake, may alter metabolism, weight gain, or a combination thereof.

Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a 19-nor pregnane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.

Abstract: The invention provides a method for the treatment and prevention of urinary incontinence in mammals, e.g., human males and females, especially nonpregnant female mammals, by administering a nitric oxide synthase substrate and/or nitric oxide donor, alone or in combination with an estrogenic agent and/or a progestational substance, with or without supplementation with an alpha-adrenergic agonist, beta-adrenergic receptor blocking agent, cholinergic-receptor blocking compound or a cholinergic-receptor-stimulating drug, as well as pharmaceutical compositions useful in practicing the methods of this invention.

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: Methods and formulations for treating ocular neovascularization using angiostatic steroids are disclosed.

Abstract: In accordance with the present invention, it has been discovered that certain synthetic steroid compounds are capable of inhibiting the efflux pump which is believed to be responsible for multidrug resistance, while at the same time activating glucocorticoid-induced response. Thus, chemotherapy of glucocorticoid sensitive tumors can be enhanced by use of a compound having the dual ability to activate glucocorticoid-induced response and facilitate the accumulation of drug at the target site, with reduced or eliminated competition by the drug efflux system.

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: This invention provides a method of contraception which comprises administering to a female of child bearing age for 28 consecutive days,a first phase combination of a progestin at a daily dosage equivalent in progestational activity to 40-125 .mu.g levonorgestrel and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 .mu.g ethinyl estradiol for 3-8 days beginning on day 1 of the menstrual cycle, wherein the same dosage of the progestin and estrogen combination is administered in each of the 3-8 days,a second phase combination of a progestin at a daily dosage equivalent in progestational activity to 40-125 .mu.g levonorgestrel and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 .mu.

Abstract: The invention relates to the use of antiglucocorticoid steroids for the manufacture of a pharmaceutical composition for the treatment of anxiety disorders.

Abstract: A method for obtaining an extract containing the natural mixture of conjugated estrogens from mare urine by solid-phase extraction of the mixture of conjugated estrogens from the urine of pregnant mares on non-ionic semi-polar polymeric adsorber resins.

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: In this invention, the new etheno- and ethano-19,11-bridged 4-estrenes of general formula I ##STR1## are described, in whichW, R.sup.1, R.sup.2, R.sup.6a, R.sup.6b, R.sup.7, R.sup.14, R.sup.15, R.sup.16, R.sup.11, R.sup.11' and R.sup.19 have the meaning indicated in the description, as well as a process for their production.The new compounds have strong progestational activity and are suitable for the production of pharmaceutical agents.

Abstract: Methods and formulations for treating ocular neovascularization using angiostatic steroids are disclosed.

Abstract: Inter and/or intramolecular cross-linked esters of acid polysaccharides are disclosed in which a part or all of the carboxy groups are esterified with hydroxyl groups of the same molecule and/or of different molecules of the acid polysaccharide. These inner cross-linked esters of polysaccharide acids are useful in the field of biodegradable plastic materials, to manufacture sanitary and surgical articles, in the cosmetic and pharmaceutical fields, in the food industry and in many other industrial fields.

Abstract: There are disclosed novel oral prodrugs of phosphonate nucleotide analogs which are hydrolyzable under physiological conditions to yield compounds which are useful as antiviral agents, especially as agents effective against RNA and DNA viruses. They may also find use as antitumor agents.

Abstract: The present invention provides compounds and methods of inducing a variety of therapeutic responses in a subject in need of such treatment. The method includes administering a compound of Formula (I) ##STR1## wherein R.sub.1 -R.sub.7 are as defined in the specification; and wherein said compound of Formula (I) is ethylenically unsaturated at a set of locations selected from the group consisting of (a) between C.sub.4 and C.sub.5 ; (b) both between C.sub.3 and C.sub.4 and between C.sub.5 and C.sub.6 ; (c) between C.sub.5 and C.sub.6 ; (d) both between C.sub.4 and C.sub.5 and between C.sub.6 and C.sub.7 ; (e) both between C.sub.3 and C.sub.4 between C.sub.5 and C.sub.6 and between C.sub.7 and C.sub.8 ; (f) both between C.sub.4 and C.sub.5 and between C.sub.7 and C.sub.8 ; and (g) both between C.sub.5 and C.sub.6 and between C.sub.7 and C.sub.8.The compounds of Formula (I) are administered in an amount effective to induce the desired therapeutic response.

Abstract: A topical composition comprising LYCD together with known topically active useful medicinal agents such as anti-wrinkling, antibiotic, anticancer, antifungal, antiinflammatory such as anti-acne, antiviral, wound healing, and hair-growing agents. The LYCD works together with the other active agents to achieve a synergistic result more effective than can be obtained from the topical agents individually, and more effective than could be predicted from the mere addition of the known efficacies of the individual ingredients.

Abstract: Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition comprises about 0.5% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 80% by weight of a hydrocolloid gum obtainable from higher plants; and about 10% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating colon disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.