Abstract: Certain imidazoethyl thiophenes/thiazoles and benzothiophenes of the formula: where Z is CH or N; and X is independently selected from the group consisting of hydrogen, C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C4-1alkoxy and nitro; are &agr;2-adrenoceptor agonists/antagonists which are useful in the treatment of hypertension, glaucoma, sexual dysfunction, depression, attention deficit hyperactivity disorder, the need for anesthesia, cardiac arrythmia or the need for analgesia.

Abstract: The present invention relates to an ocular hypotensive composition and a composition for treatment of glaucoma which comprising an amount of 20-substituted-PGs or 20-substituted 15-keto-PGs effective as an ocular hypotensive agent; these compounds exhibit no or little side effect such as transient ocular hypertensive response, hyperemia of conjunctiva or of iris, dacryops, lema, closed eye and the like. The present invention relates to ocular hypotensive agents which contains 13,14-dihydro-15-keto-prostagrandins, which shows no transient ocular hypertensive response that PGs usually show.

Abstract: A compound selected from those of formula (I): wherein: denotes single bond or double bond, n is integer from 1 to 6 inclusive, R1, and R2 represent a group selected from hydrogen, linear or branched (C1-C6)-alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, X represents a group selected from —CH═CH—, oxygen, S(O)m wherein m is integer from 0 to 2 inclusive, and NR3 wherein R3 represents a group as defined in the description, Y represents CH or CH2 depending on whether denotes single bond or double bond, or may have the additional meaning of oxygen when X represents oxygen, T represents monocyclic or polycyclic (C3-C10)cycloalkyl optionally containing within the ring system oxygen, selenium, S(O)p, NR3, or SiR4R5 wherein p, R3, R4, and R5 are as defined in the description, its isomers and addition salts thereof with a pharmaceutically-accep

Abstract: The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.

Abstract: A compound is disclosed havin the formula AW—SiR1R2R3 wherein R1 and R2 are independently alkyl, cycloalkyl, alkenyl, alkynyl, aryl, aralkyl, alkaryl, or a hydrophilic group; R3 is a hydrophilic group; and AW is the covalently bonded form of a drug AWH, wherein W is O, NH, S, or an enolate group. The hydrophilic group may be either non-neutral, or may be a polyol. This compound serves as a prodrug for the drug AWH. A method for preparing these compounds is also disclosed. Also disclosed is a method of treatment or prevention of gastric ulcers by administering the prodrug compounds.

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: The present invention relates to novel oxazoline derivatives of the formula (I) in which the radicals A, B, Q and R are each as defined in the description to processes for their preparation and to their use for controlling animal pests.

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.

Abstract: The present invention comprises small molecular weight, non-peptidic inhibitors of formulae I-VII of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).

Abstract: The invention relates to substituted 8,8a-dihydro-3aH-indeno[1,2-d]thiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.

Abstract: There is disclosed a process for producing an acid salt of a (Z)-2-aminothiazole compound of the formula (I): wherein R1 and R2 independently represent an alkyl group having 1 to 5 carbon atoms, Y represents a halogen atom, —OSO3H or —OPO(OH)2, m indicates the valence number of an inorganic acid of the formula: HY wherein Y represents the same as defined above, and n indicates an integer of 1 or 2, which process is characterized by: reacting an acid salt of a 2-aminothiazole compound of the formula (II): wherein R1 and R2 independently represent an alkyl group having 1 to 5 carbon atoms, X represents a bromine atom or an iodine atom, and the wavy line means that this compound is a mixture of the E- and Z-isomers, with the inorganic acid of the formula HY.

Abstract: Compounds represented by the following formula (I),: wherein R represents a lower alkyl group which may be substituted; n represents an integer of from 1 to 10; and X represents an anion species. The compounds are useful as active ingredients of fluorescent labeling agents or medicaments for diagnosis.

Abstract: Novel phenylacetic acid heterocyclyl amides of the formula in which R1, R2, R3, R4, A, X and n are as defined in the description, a process for preparing these novel compounds and their use for controlling undesirable microorganisms and animal pests. Novel intermediates of the formula and a plurality of processes for their preparation.

Abstract: The invention relates to novel substituted thiazol(in)ylidenaminosulphonyl-amino(thio)carbonyl-triazolinones of the formula (I) in which Q represents oxygen or sulphur, R1 represents hydrogen, amino, alkylideneamino or represents an in each case optionally substituted radical from the group consisting of alkyl, alkoxy, alkylamino, dialkylamino, alkanoylamino, alkenyl, alkinyl, alkenyloxy, cycloalkyl, cycloalkylalkyl, cycloalkylamino, aryl and arylalkyl, R2 represents hydrogen, cyano, halogen or represents an in each case optionally substituted radical from the group consisting of alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino, alkenyl, alkinyl, alkenyloxy, alkenylthio, alkenylamino, cycloalkyl, cycloalkylalkyl, cycloalkyloxy, cycloalkylthio, cycloalkylamino, aryl, aryloxy, arylthio, arylamino, arylalkyl, arylalkoxy, arylalkylthio and arylalkylamino, R3 represents an in each case optionally substituted radical from the group consisting of alkyl, alkoxy,

Abstract: The esylate, mesylate, and tartrate salts of ziprasidone exhibit excellent solubilities in cyclodextrins.

Abstract: An apoptosis inhibitor which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: —CO—, —CH(OH)— or —NR3— where R3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.

Abstract: The present invention relates to a hydrazine oxoacetamide derivative or its salt which exhibits an excellent insecticidal effect even at a low concentration. The hydrazine oxoacetamide derivative has the following Formula (I): wherein R1 represents a chlorine atom or a bromine atom, Y represents an oxygen atom or a methylene group, and when Y is an oxygen atom, p is 2 and when Y is a methylene group, p is 0, R2 represents a trifluoromethyl group, R3 represents a hydrogen atom or a methyl group, R4 represents a hydrogen atom or a methyl group, and R5 represents a methyl group, an ethyl group, an n-propyl group, a cyclopropyl group, an allyl group or a propargyl group.

Abstract: Compounds of Formula 1, where the symbols are as defined in the specification, are useful as ocular hypotensive agents but do not exert their activity through the FP prostaglandin receptor. In particular the compound PGF2&agr; 1-ethanolamide, having the formula was discovered to be present in mammalian tissue as a naturally occurring substance, was synthesized in a substantially pure form and was found to be effective for lowering intraocular pressure in the mammalian eye, but not acting through the FP receptor through which many ocular hypotensive prostaglandins act.

Abstract: Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where x is 0 or 1 and y is 0 or 1 (provided that x=1 when y=0 and x=0 when y=1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.

Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.