Abstract: 15-keto latanoprost and other 15-keto prostaglandin analogs are used as ocularly applied intraocular pressure reducing agents.

Abstract: A pharmaceutical composition is disclosed which is comprised of an E-type prostaglandin ligand and a COX-2 selective inhibiting compound, in combination with a pharmaceutically acceptable carrier.

Abstract: Therapeutic formulations and methods for treating erectile dysfunction with a misoprostol compound in a subject are provided, a method comprising: obtaining a therapeutic formulation having an effective dose of a misoprostol compound in an excipient carrier; and applying the therapeutic formulation topically to the subject.

Abstract: The present invention relates to a composition of topical preparation containing alprostadil alkyl ester, and more particularly, comprising an alprostadil alkyl ester, an oily vehicle, a skin permeation enhancer and an anti-irritant agent.

Abstract: Tannate compositions consisting of carbetapentane tannate and pyrilamine tannate, which are effective when administered orally for the symptomatic relief of coryza associated with the common cold, sinusitis, allergic rhinitis, unproductive cough and upper respiratory tract conditions, are disclosed.

Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.

Abstract: A &ohgr;-substituted phenyl-prostaglandin of formula (I), a process for the preparation thereof, a mediciament comprising it as active ingredient (all symbols have the same meaning as described in the specification). The compounds of the formula (I) bind strongly in PGE2 receptor (especially subtype EP4) and therefore are useful for the prophylaxis and/or treatment of immune diseases (autoimmune diseases (amyotrophic lateral sclerosis (ALS) etc.), post-transplantation graft rejection, etc.), asthma, abnormal bone formation, neurocyte death, pulmopathy, hepatopathy, etc. They are also related to sleeping disorders and platelet coagulations, and therefore they are also applicable to these diseases.

Abstract: Compositions and methods for the treatment of dry eye and related diseases utilizing 6-keto-PGF1&agr; and its analogs are disclosed.

Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein.

Abstract: Fulvic acid salts, esters or derivatives thereof in pharmaceutical preparations are effective for treating inflammation, acne, exzema or bacterial or fungal or viral infections. These pharmaceutical preparations may be given either orally or topically in the form of a solution, paste, ointment, powder to humans or animals.

Abstract: Cyclic amino acids, such as gabapentin and pregabalin, are used for treating physiological conditions associated with the use, or sequelae of use, of cocaine or other psychomotor stimulants and other addictive drugs/substances. Physiological conditions include stimulant-induced toxicities.

Abstract: Tannate compositions consisting essentially of carbetapentane tannate and chlorpheniramine tannate which are effective when administered orally for the symptomatic relief of coryza associated with the common cold, sinusitis, allergic rhinitis, unproductive cough and upper respiratory tract conditions are disclosed.

Abstract: Disclosed is a method for treatment of external secretion disorders, which comprises administering a fatty acid derivative to a subject in need of said treatment. The method of the present invention is useful for treatment of at least one condition selected from hypolacrimation including disorder of basal tear secretion, dry-eye syndrome, hyposalivation and dry-mouth syndrome.

Abstract: A selective EP2 or EP4 prostanoid receptor agonist can be used to treat female sexual dysfunction. Salts and esters of the agonists can also be used. Formulations comprising such agonists, salts, or esters can be in the form of a cream, gel, ointment, or solid, useful for topical administration.

Abstract: Methods and compositions for the antagonism of FP receptor-mediated biological responses are disclosed.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Remedies or preventives for diseases with a need for immunoregulation, diseases with a need for inhibition of inflammation, diseases with a need for regulation of tumor necrosis factor production, diseases with a need for regulation of fungal growth, diseases with a need for regulation of cell adhesion or disease with a deed for induction of heat-shock protein, which contain as the active ingredient at least one compound selected from among cyclopentenone derivatives represented by general formula [I], optically active isomers and salts thereof, wherein R1 and R2 are the same or different and each represents hydrogen, an aliphatic group, an aromatic group or an aromatic aliphatic group.

Abstract: This application relates to compositions and methods for the treatment of glaucoma and/or ocular hypertension in mammals utilizing prostaglandin E receptor agonists.

Abstract: The invention relates to agents which combat the hepatitus A virus, containing only minimal amounts of chlorine-containing and/or chlorine cleaving active ingredients, or none of said substances. The inventions also relates to the use of these agents and to a method for their production.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; where in A, B, D, X, Y, Z, R1, R3 and R4 are as defined in the specification.

Abstract: Compounds represented by the general formula (1):   (where R1 is SR6 or NR7R8, where R6 is typically an alkyl group having 1-6 carbon atoms, R7 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2 and R3 are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3 and Y4 which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are CH2; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR2, CO2R and OR.

Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: Glucokinase activating compounds of the formula wherein R1 and R2 are independently hydrogen, halo, amino, nitro, cyano, sulfonamido, lower alkyl, perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, or perfluoro-lower alkyl sulfonyl; R3 is cycloalkyl having from 3 to 7 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R4 is hydrogen, lower alkyl, lower alkenyl, hydroxy lower alkyl, halo lower alkyl, R5 and R6 are hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof

Abstract: Disclosed are compounds of the formula: which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.

Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: The present invention provides a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents, and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating disease

Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives.

Abstract: Methods and compositions for the antagonism of FP receptor-mediated biological responses are disclosed.

Abstract: A pharmaceutical composition useful for the treatment of cancer in mammals, comprising as the active ingredient a therapeutically effective amount of a jasmonate of the formula: 1

Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: Disclosed is a method for promoting bile secretion, which comprises administering an effective amount of a certain 15-keto-prostaglandin compound to a subject having a disease or condition associated with bile secretion deficient. Also disclosed is a method for treatment of a liver to be transplanted in a liver transplantation process, which comprises contacting the liver with a liquid composition comprising the 15-keto-prostaglandin compound as above.

Abstract: A pharmaceutical composition useful for the treatment of cancer in mamnmals, comprising as the active ingredient a therapeutically effective amount of a jasmonate of the formula: wherein: n is 0,1, or 2; R1 is OH, alkoxy, O-glucosyl, or imino; R2 is OH, O, alkoxy or O-glucosyl; R3, R4 and R5 are H, OH, alkoxy or O-glucosyl; and/or wherein R1 and R2, or R1 and R4 together form a lactone; and further wherein the bonds between C3:C7, C4:C5, and C9:C10 may be double or single bonds; or a derivative of said formula; the derivative having at least one of the following: a lower acyl side chain at C3 (free acid, ester or conjugate); a keto or hydroxy (free hydroxy or ester) moiety at the C6 carbon; or an n-pentenyl or n-pentyl side chain at C7. These jasmonates are useful in treating a wide variety of malignancies.

Abstract: 15-fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: The present invention relates to 5-thia-&ohgr;-substituted phenylprostaglandin E derivatives of the formula (I) (wherein, all the symbols are as defined in the specification), process for producing them and pharmaceutical compositions comprising them as active ingredient. The compounds of the formula (I) can bind to PGE2 receptors (especially, subtype EP4) strongly, so they are expected to be useful for prevention and/or treatment of immunological diseases (autoimmune diseases such as amyotrophic lateral sclerosis (ALS), multiple sclerosis, Sjoegren's syndrome, chronic rheumarthrosis and systemic lupus erythematosus etc., and rejection after organ transplantation etc.

Abstract: The present invention relates to use of prostaglandin E receptor agonists and partial agonists to stimulate mucin secretion to treat dry eye, keratoconjunctivitis, Sjogren's syndrome and related ocular surface diseases.

Abstract: The use of HETE derivatives in intraocular surgery (e.g., cataract surgery) is disclosed. The HETE derivatives protect and maintain the corneal endothelium.

Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.

Abstract: Disclosed is treatment of ocular hypertension and glaucoma by long-term therapy with a prostaglandin related compound for eliminating or reducing potential iridic pigmentation. Composition useful for the treatment, and use of the prostaglandin related compound for producing the composition are also disclosed.

Abstract: The invention relates to compositions and methods for the treatment of dry eye and related diseases utilizing 6-keto-PGF1&agr; and its analogs, according to formula (I); wherein A,B,D,Q9, Q11, R1, X and Y have the meanings given in the description. Some of these compounds are novel.

Abstract: The invention pertains to a process for preparing carbetapentane tannate. The process involves the steps of heating carbetapentane to a temperature of about 80 to about 120° C. and slowly adding tannic acid to the carbetapentane while agitating the reaction mixture. Preferably, no water or any other solvent or diluent is utilized in the process.

Abstract: To provide a prostaglandin derivative represented by the formula: wherein A is an ethylene group, a vinylene group, an ethynylene group, O(CH2)q or S(O)r(CH2)q, R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C1-10 alkyl group, a C1-10 alkyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s), a C2-10 alkenyl group, a C2-10 alkenyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s), a C2-10 alkynyl group, a C2-10 alkynyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s) or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 1 to 5, n is an integer of 1 to 4, p is 0, 1 or 2, q is an integer of 1 to 5 and r is 0, 1 or 2; a pharmaceutically acceptable salt thereof or a hydrate thereof exhibit excellent action in inhibiting the growth of vascular smooth muscle and is useful as a drug for inhibition of restenosis after per

Abstract: Compounds having a structure according to the following formula: are effective in treating disorders such as bone disorders and glaucoma in a subject in need thereof.

Abstract: A method for reducing the average number of insemination administrations per herd comprising the step of administering to the herd native or extended semen with a simultaneous or sequential administration of prostaglandin is provided. Also provided is a novel composition of matter which includes either native semen, extended semen or a semen extender, one or more prostaglandins and one or more antibioitics.

Abstract: Administration of a pharmaceutical composition in the form of a suppository comprising:

Abstract: The invention relates to a process for preparing a soft tablet capable of being chewed or disintegrated in the oral cavity. The tablet is prepared by forming a tablet having a friability of less than about 2% from a mixture comprising a pharmaceutically active ingredient, an excipient in the form of a hydrate, and a water-swellable excipient, and then applying sufficient energy, preferably in the form of heat, to the tablet for a sufficient time to decrease the hardness of the tablet by at least about 20%.

Abstract: The invention relates to a tablet capable of being chewed or disintegrated in the oral cavity, which comprises a pharmaceutically active ingredient, and a matrix comprising directly compressible dextrose monohydrate and sucralose, said tablet being substantially fat free and said matrix being substantially free of non-saccharide, water soluble polymeric binders.

Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.

Abstract: Methods and compositions for treating various disorders by administering a therapeutically effective amount of a retinoic acid receptor antagonist alone or in combination or in conjunction with other therapeutic agents to promote angiogenesis are provided. Also provided are methods for obtaining additional retinoic acid receptor antagonists for use as therapeutic agents to promote angiogenesis.

Abstract: Methods and compositions for the antagonism of FP receptor-mediated biological responses are disclosed.