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: 8-Hydroxyquinoline is useful in the topical treatment of inflammatory proliferative skin diseases, especially psoriasis. It should be applied from an essentially anhydrous vehicle.

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: 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: 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: 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: Antigestagens inhibit prostaglandin synthesis by the uterus and thus can be used to treat symptoms of dysmennhorea.

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: Disclosed are steroid nitrite/nitrate ester derivatives of formula I: ##STR1## wherein, the substituents are as defined in the specification and their use in the treatment of inflammatory diseases.

Abstract: This invention relates to aerosol formulations of use for the administration of medicaments by inhalation, in particular a pharmaceutical aerosol formulation which comprises: (a) beclomethasone dipropionate monohydrate, the particle size of substantially all the monohydrate being less than 20 microns; (b) at least 0.015% by weight of the formulation of water in addition to the water of crystallization associated with the monohydrate; and (c) a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.

Abstract: A progesterone compound represented by the following formula (1): ##STR1## ?wherein R.sup.1 represents a C1-C23 hydrocarbon group!, and a neovascularization inhibitor containing the same as the active ingredient.The compound (1) has a potent neovascularization inhibitory effect and is hence useful in the treatment of malignant tumors, diabetic retinitis, rheumatism, etc.

Abstract: This invention relates to aerosol formulations of use for the administration of medicaments by inhalation, in particular a pharmaceutical aerosol formulation which comprises: (a) beclomethasone dipropionate monohydrate, the particle size of substantially all the monohydrate being less than 20 microns; (b) at least 0.015% by weight of the formulation of water in addition to the water of crystallization associated with the monohydrate; and (c) a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.

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

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

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.

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: Methods for treating angiogenesis, tumors, and ocular hypertension with steroids are disclosed herein. The steroids have angiostatic activity with reduced glucocorticoid activity.

Abstract: Invented is a Method of Treating Prostatic Adenocarcinoma by employing asteroid 5-.alpha.-reductase inhibiting compound or a combination of steroid 5-.alpha.-reductase inhibiting compounds.

Abstract: A percutaneous absorptive anesthetic is provided, wherein said anesthetic is formed by mixing a base agent of said anesthetic with one or two type of mixtures which has/have been selected from the groups, for example made of glycyrrhizin, glycyrrhetic acid, glycyrrhetic acid derivatives glycyrrhetic acid 3.beta.-monohemisuccinate, glycyrrhetic acid 3.beta.-monohemisuccinate, 18.beta.-olean-12-ene-3.beta., 30-dihemiphthalate, 18.beta.-olean-9, (11)12-diene-3.beta., 30-diol-dihemiphthalate, olean-11,13(18)-diene-3.beta., 30-diol-dihemiphthalate or their pharmaceutically allowable salt.

Abstract: Compositions and methods are provided for enhanced transdermal electrotransport of 17-hydroxy sterol compounds, including testosterone. The parent sterols are modified at the 17-hydroxy position by covalent attachment of a charged chemical modifier. The chemical modifier provides the parent sterol with enhanced transport properties and is hydrolyzed under physiological conditions to release the active parent compound.The composition comprises a 17-hydroxy sterol/chemical modifier complex, more generally represented by the formula (sterol--O--)C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+. The portion of the complex derived from the chemical modifier is indicated by "C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ ", where N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ represents a quaternary ammonium group and R.sup.1, R.sup.2, and R.sup.3 are independently selected from the group consisting of lower alkyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroalkyl, and heteroarylalkyl; or R.sup.1 and R.sup.

Abstract: Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.

Abstract: The invention is drawn to a method for suppressing an immunoresponse in animals by administering an estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R.sup.1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R.sup.2 is acyl, dansyl, or alkyl; R.sup.3, R.sup.4, and R.sup.5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; and n is an integer of 0 to 3; provided that when n is 0, all of R.sup.3, R.sup.4, and R.sup.5 are not H at the same time, and at least one of R.sup.3, R.sup.4, and R.sup.5 is a group other than H and OH; and further, when n is 2 or 3, the groups R.sup.1 are the same or different.

Abstract: An estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R.sup.1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R.sup.2 is acyl, dansyl, or alkyl; R.sup.3, R.sup.4, and R.sup.5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; and n is an integer of 0 to 3; provided that when n is 0, all of R.sup.3, R.sup.4, and R.sup.5 are not H at the same time, and at least one of R.sup.3, R.sup.4, and R.sup.5 is a group other than H and OH; and further, when n is 2 or 3, the groups R.sup.1 are the same or different; a process for preparing the same, and a pharmaceutical composition containing the conjugate are described.

Abstract: Methods for preventing and treating corneal haze resulting from exposure of the eye to laser irradiation are disclosed. The methods include administration of compositions of wound healing modulators to the eye. Compositions for use in preventing and treating the corneal haze are also disclosed.

Abstract: The application discloses methods of treating mammalian diseases characterized by undesirable angiogenesis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

Abstract: Invented is a Method of Treating Prostatic Adenocarcinoma by employing asteroid 5-.alpha.-reductase inhibiting compound or a combination of steroid 5-.alpha.-reductase inhibiting compounds.

Abstract: This invention is directed to 4-amino-17.beta.-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17.beta.-(cyclopropylylamino)androst-4-en-3-one and related compounds, a process for their synthesis, a pharmaceutical composition having C.sub.17-20 lyase and 5.alpha.-reductase inhibitory activity, the use of the present compounds as C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and also to a method for using such compounds in the treatment of androgen and/or estrogen dependent disorders, including bengin prostatic hyperplasia, breast cancer and prostatic cancer. The 4-amino compounds are prepared by the reaction of the appropriate 4,5-epoxide with sodium azide in an inert solvent in the presence of a catalytic amount of strong acid under appropriate reaction conditions. Alternatively, the 4-amino compounds are prepared by first nitration and then reduction of the appropriate steroid under appropriate reaction conditions.

Abstract: A process for the production of semisolid preparations containing micronized active ingredients is described which is characterized in that a mixture of one or two nonionic surfactants with an HLB of 9 to 18 with 2.3 to 100 times the amount by weight of a fatty acid ester of general formulaR.sub.1 --COO--R.sub.2in which R.sub.1 and R.sub.2 each represent alkyl groups or alkenyl groups with 12 to 32 carbon atoms, or a mixture of these fatty acid esters is heated until it melts, the melt with stirring is put into 10 to 200 times the amount by weight of a semisolid preparation, which is heated approximately to the same temperature, the mixture is allowed to cool with stirring and mixed with the micronized active ingredient or active ingredient mixture as well as optionally with scents.

Abstract: Pharmaceutical compositions useful in the treatment of ophthalmic inflammation and methods of treating ophthalmic inflammation with those compositions are disclosed. The compositions contain a combination of a glucocorticoid and an angiostatic steroid. The angiostatic steroid substantially prevents any significant increases in intraocular pressure which might otherwise be experienced by the patient as a side effect of the glucocorticoid component of the compositions. The therapeutic interaction of the two components therefore allows the potent anti-inflammatory properties of the glucocorticoids to be utilized without fear of elevating intraocular pressure.

Abstract: Methods for preventing and treating corneal haze resulting from exposure of the eye to laser irradiation are disclosed. The methods include administration of compositions of wound healing modulators to the eye. Compositions for use in preventing and treating the corneal haze are also disclosed.

Abstract: Polyvinyl butyrals (PVBs) with improved thermal stability and improved light resistance contain as stabilizers polynuclear phenols which phenolic radicals have a quaternary carbon atom in the para-position to the phenolic hydroxyl group and if desired in combination with synergistically acting, nitrogen-containing, sulfur-containing or phosphorus-containing co-stabilizers of the types a) to d). The use of the resulting films of low yellowness as interlayer films having substantially reduced yellowing for the production of laminated glasses and glass composites of silicate glass sheets is described.

Abstract: Pharmaceutical compositions are provided for lowering the activity of HMG-CoA reductase and/or lowering serum cholesterol, comprising an amount effective to lower the activity of HMG-CoA reductase and/or lower serum cholesterol of a side chain derivatized 15-oxygenated sterol having the formula (I): ##STR1## the basic ring structure being saturated or unsaturated, wherein R.sub.1 is --OH, .dbd.O, --OR.sub.7, ##STR2## a sulfate group, a sugar moiety, or a Mg, Na, or K salt of a sulfate group;R.sub.2 is --H, --OH, .dbd.O, mono- or di-halogen, or a C.sub.1 to C.sub.6 alkyl group, which may be unsaturated or substituted with halogen;R.sub.3 is --H, --OH, halogen, or a C.sub.1 to C.sub.6 alkyl group, which may be unsaturated or substituted with halogen;R.sub.4 is nonexistent when there is a double bond between the 8 and 14 carbons or .alpha.H, .beta.H, or an .alpha.C.sub.1 to C.sub.6 alkyl group;R.sub.5 is --OH, .dbd.O, .dbd.NOH, or ##STR3## R.sub.6 is --CH.sub.2 CH(CH.sub.3).sub.2 or CH.sub.2 N(CH.sub.3).sub.

Abstract: Angiostatic steroids for use in controlling ocular hypertension are disclosed. Pharmaceutical compositions of the angiostatic steroids and methods for their use in treating ocular hypertension, including controlling the ocular hypertension associated with primary open angle glaucoma, are disclosed. In addition, the combination of the compounds with glucocorticoids for the prevention of elevated IOP during the treatment of inflammation is disclosed.

Abstract: The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.

Abstract: An estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R.sup.1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R.sup.2 is acyl, dansyl, or alkyl; R.sup.3, R.sup.4, and R.sup.5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; and n is an integer of 0 to 3; provided that when n is 0, all of R.sup.3, R.sup.4, and R.sup.5 are not H at the same time, and at least one of R.sup.3, R.sup.4, and R.sup.5 is a group other than H and OH; and further, when n is 2 or 3, the groups R.sup.1 are the same or different; a process for preparing the same, and a pharmaceutical composition containing the conjugate are described.

Abstract: Following completion of an operative procedure, the topical application of a cortisone preparation into the area of a postoperative wound is useful in ameliorating or eliminating postoperative pain. The postoperative wound can be treated with a local anesthetic agent prior to or during application of the cortisone preparation. The raw surgical surfaces of the wound are doused once with the cortisone preparation, for example, by direct spray with an atomizer or by irrigation with a syringe and needle. The cortisone is not irrigated out with saline following its application. Normal healing takes place.

Abstract: Methods and compositions for preventing or treating ophthalmic diseases or disorders wherein an ophthalmically effective amount of the C.sub.20 through C.sub.26 aminosteroids of formula XI and their pharmaceutical, acceptable salts, hydrates or solvates is administered in an inert vehicle to arrest oxidation processes damaging to the eye.

Abstract: Methods and compositions for preventing or treating ophthalmic diseases or disorders wherein an ophthalmically effective amount of the C.sub.20 through C.sub.26 aminosteroids of formula XI and their pharmaceutical, acceptable salts, hydrates or solvates is administered in an inert vehicle to arrest oxidation processes damaging to the eye.

Abstract: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.

Abstract: New substituted pyridyltriazines of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 have the meanings given in the description, and their use for combating pests.The compounds can be prepared by analogous processes, for example by reacting pyridylamidine hydrochloride with suitable methyl imidates or with suitable benzene-isothiocyanates, or by desulphurising mercapto-substituted pyridyltriazines or by reacting them with alcohols. The mercapto-substituted compounds are also new and can be prepared by analogous processes.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.

Abstract: A self-propelling aerosol formulation which may be free from CFC's which comprises a medicament, 1,1,1,2-tetrafluoroethane, a surface active agent and at least one compound having a higher polarity than 1,1,1,2-tetrafluoroethane.

Abstract: Anti-inflammatory compounds, a method of treating inflamed ocular tissue and compositions of these compounds are described. The compounds are derivatives and analogues of known steroid compounds (e.g., dexamethasone) and are advantageously characterized in that they do not cause any significant increase in intraocular pressure during chronic use.

Abstract: A method for treating glaucoma consisting of exposing the eye to a corticosteroid and an alpha or a beta adrenergic agent to the eye which acts to decrease ocular pressure. Useful adrenergic agents include beta agonist antagonists, including, for example, epinephrine, dipivalyl epinephrine, betaxolol, levobunolol, timolol, and an alpha adrenergic agonist, including apraclonidine hydrochloride. Useful steroids, which are preferably applied topically, include dexamethasone, prednisolone, cortisone, and triamcinolone. The beta adrenergic agent is administered at a concentration between 10% and 20% of the concentration that the agent is administered in its normal use. The corticosteroid is administered at a concentration between 5% and 10% of the concentration that the corticosteroid is administration in its normal use.

Abstract: Methods and compositions for preventing or treating ophthalmic diseases or disorders wherein an ophthalmically effective amount of the C.sub.20 through C.sub.26 aminosteroids of formula XI and their pharmaceutical, acceptable salts, hydrates or solvates is administered in an inert vehicle to arrest oxidation processes damaging to the eye.

Abstract: The invention provides novel pregnane derivatives having the formula: ##STR1## wherein X=F, Cl or Br; R.sub.1 =F or Cl; R.sub.2 =H(.beta.OH) or O; R.sub.3 =alkyl(1-4 C); R.sub.4 =alkyl(1-4 C); and the dotted line indicates the optional presence of a double bond.The novel compounds have been found to possess immunomodulating properties.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.