Abstract: A process of forming the cis- or the trans-isomers of thiazine-indigo compounds comprising the step of reacting o-aminomercapto-carbocyclic or -heterocyclic compounds with a maleic acid or fumaric acid derivative in the presence of an aqueous system. The invention further relates to a process of converting cis-isomers of thiazine-indigo compounds into the trans-isomers being pigments. The invention also relates to the cis-isomers of thiazine-indigo compounds of formula I as defined in claim 14 which are new compounds.

Abstract: Compounds of formula (I) 1

Abstract: New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: Psychogenic impotence can be ameliorated without substantial undesirable side effects by administration of apomorphine and an antiemetic agent in an amount sufficient to substantially reduce nausea symptoms associated with the use of apomorphine.

Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.

Abstract: Compounds of the formula I 1

Abstract: A therapeutic agent for glaucoma comprises (+)-(R)-3,4-Dihydro-2-[5-methoxy-2-[3-[N-methyl-N-[2-[(3,4-methylenedioxy) phenoxy]ethyl]amino]propoxy]phenyl]-4-methyl-3-oxo-2H-1,4-benzothiazine or its salt as active ingredient and pharmaceutically acceptable excipients. The therapeutic agent lowers the intraocular pressure upon topical or systemic administration.

Abstract: A compound of the formula: in which R1 is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl, R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl, R3 is hydrogen or amidino-protective group, A is lower alkylene or carbonyl, X is Y is lower alkylene, —S— or —SO2—, Z is —S— or —O—, and the line: is a single bond or a double bond, or pharmaceutically acceptable salts thereof, which is useful as a medicament.

Abstract: A pyrrolesulfonamide derivative having the following formula (I): is provided wherein P, A, Y, l, Z1 and Z2 are as described herein, wherein the derivative has strong serotonin-2 receptor antagonistic action, low toxicity and fewer side effects, and its use as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula 1,

Abstract: The present invention relates to fused 1,4-thiazine-2-carbonitrile derivatives, compositions thereof and methods for preparing the compounds. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.

Abstract: Aromatic camptothecin ester compounds having the formula: are described as well as formulations containing the compounds. Methods of treating cancer and/or tumors are also disclosed.

Abstract: Cyanine and related dyes, such as merocyanine, styryl and oxonol dyes, are strongly light-absorbing and highly luminescent. Cyanine and related dyes having functional groups make them reactive with amine, hydroxy and sulfhydryl groups are covalently attached to proteins, nucleic acids, carbohydrates, sugars, cells and combinations thereof, and other biological and nonbiological materials, to make these materials fluorescent so that they can be detected. The labeled materials can then be used in assays employing excitation light sources and luminescence detectors. For example, fluorescent cyanine and related dyes can be attached to amine, hydroxy or sulfhydryl groups of avidin and to antibodies and to lectins. Thereupon, avidin labeled with cyanine type dyes can be used to quantify biotinvlated materials and antibodies conjugated with cyanine-type dyes can be used to detect and measure antigens and haptens. In addition, cyanine-conjugated lectins can be used to detect specific carbohydrate groups.

Abstract: Use of the proprietary drug amiloride for the treatment of cancer types that depend on an enzymatic cascade triggered by the activation of plasminogen to plasmin by the specific activating enzyme Urokinase Plasminogen Activator (uPA). Administration of amiloride inhibits the action of uPA, inhibits the ability of the cancer cell to attract new blood supply, blocks the Na+/H+ transporter, and inhibits ornithine decarboxylase necessary for DNA synthesis. Further, in combination with amiloride, a different step in the enzymatic cascade is targeted by a secondary agent, Batimistat, for example, which is a metalloprotease inhibitor. Additionally, the use of hydrochlorothiazide promotes excretion of potassium.

Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.

Abstract: A growth hormone secretagogue is useful for enhancing the return of patients to independent living status following acute deconditioning such as that which may result from immobilization, surgery, or major injury such as hip fracture.

Abstract: Compounds of Formula I wherein X and R1-6, are as defined herein, tautomeric forms thereof, and isomeric forms thereof, and salts thereof, are suitable for treating diseases that are induced by the action of nitrogen monooxide at pathological concentration. Such diseases include neurodegenerative diseases, inflammatory diseases, auto-immune diseases, and cardiovascular diseases.

Abstract: The power of citalopram, fluvoxamine and paroxetine to increase the availability of sarotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.