Abstract: The present invention relates generally to cyclic carbamates and isoxazolidines or Formula (I) or their pharmaceutically acceptable salts thereof, which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: A process for the preparation of a racemic or optically active compound of the formula where the group R1 is an unsubstituted or a halogen substituted C1-4-alkyl, a C1-4-alkoxy, an aryl, an arylalkyl, an aryloxy, or arylalkylloxy.

Abstract: Compounds of the formulae (IA) and (IB): wherein R1 is C1 to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from C1 to C4 alkoxy; halo; CN; CF3; OCF3 or C1 to C4 alkyl wherein said C1 to C4 alkyl group is optionally substituted by C1 to C4 haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2 is C1 to C6 alkyl and R13 is OR3 or NR5R6, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.

Abstract: Infrared radiation-sensitive heterocyclic oxonol compounds have been found that are represented by Structure DYE as follows: wherein R is a secondary or tertiary amine, R1 and R2 are independently heterocyclic or carbocyclic aromatic groups, and M+ is a monovalent cation, provided that at least one of R, R1 and R2 contains at least one heterocyclic group. These compounds have a &lgr;max above 700 nm and are can be used in a number of photosensitive or heat-sensitive imaging materials.

Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl Z represents carbon or nitrogen provided that where Z is carbon, R11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R11 represents an electron pair; R5 is hydrogen or lower alkyl, L and m represent integers; n is 0, or an integer; R12 and R13 independently represent lower alkyl; or together may together form an optionally substituted 5-11 membered ring with the nitrogen atoms to which they are bonded;CR′R″ represents a methylene group optionally substituted with lower alkyl;and k is an integer of from 1

Abstract: The present invention relates to pyrazolo-pyrimidinyl compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

Abstract: New substituted phenyl uracils are described which have general formula (I), in which R1 is halogen, or optionally substituted alkyl, R2 is optionally substituted alkyl, R3 is an amino group or optionally substituted alkyl, alkenyl or alkynyl, R4 is a cyano group or halogen, R5 is a cyano group or thiocarbamoyl, R6 group (2) or group (3) in which Q1 and Q2 are oxygen or sulphur, R7 is hydrogen or optionally substituted alkyl, R8 is hydrogen or optionally substituted alkyl, alkoxy, alkylamino, dialkylamino, alkylcarbonylamino, alkylsulfonylamino, alkenyl, alkenyloxy, alkynyl, cycloalkyl, cycloalkyloxy, cycloalkylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, aryl, aryloxy, arylamino, arylcarbonylamino, arylsulfonylamino, arylalkyl, arylalkoxy or arylalkylamino group, R9 and R10 are alkyl. A method for production of said compounds and their use as herbicides are described.

Abstract: The compounds of formula (I) wherein R1, R2 and X have the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.

Abstract: Novel imidazoquinoxalines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.

Abstract: 3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases.

Abstract: The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula wherein G, R1 and R2 are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system and other disorders.

Abstract: 1,2,4-Thiadiazine and 1,4-thiazine derivates represented by formula (I): wherein A, B, D, R1, R2, R3 and R4 are defined in the description, compositions thereof and methods for preparing the compounds are described. 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: Disclosed are novel 4,5-pyrazinoxindoles having the formula These compounds inhibit or modulate protein kinases, in particular JNK protein kinases. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing such compounds, and methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis, using these compounds.

Abstract: Remedies/preventives (therapeutic or preventive agents) against frequent urination (pollakiuria)/urinary incontinence which contain as an active ingredient compound having a tropone structure or pharmacologically acceptable salt thereof and a novel compound having the tropone structure. The compounds having a tropone structure and having the above pharmacological effects are those represented by, for example, general (1): wherein R1 and R2 represent each a hydrogen atom, lower alkyl group, etc., R3 represents —OR or —NR2; R4, R5 and R12 represents each a hydrogen atom or a lower alkyl group, X represents a nitrogen atom or CH, Z represents —CHAr2, an unsubstituted or substituted phenyl, etc. m is 1 or 2. These compounds are novel ones excluding those wherein Z is —CHAr2.

Abstract: Process for preparing intermediates of formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

Abstract: Intermediates of Formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

Abstract: This invention encompasses compounds of the formula wherein Ar represents a mono- , di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists or human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: Aryl- or heteroaryluracils of formula I wherein R1 signifies methyl or ethyl; R2 signifies —CF3, —CClF2, —CCl2F, or —C2F5; and Q is an aryl or heteroaryl group; are produced whereby a compound of formula II O═C═N—Q  (II) is reacted at a temperature of −5° C. to +40° C. with an enamine of formula III wherein R19 signifies C1-C6-alkyl, in the presence of a solvent and of 0.1 to 0.4 equivalents of a base with respect to the employed enamine of formula III. The compounds of formula I are useful as herbicides. An example of the compounds of formula I is 2-chloro-5-(3,6-dihydro-2,6-dioxo-3-methyl-4-trifluoromethyl-1-(2H)pyrimidinyl)-benzoic acid 1-aalyloxycarbonyl-1-methyl-ethyl-ester.

Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g.