Abstract: The present invention addresses substituted cyanothiophene derivatives of the formula I: as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.

Abstract: Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

Abstract: The invention relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5, R6, A, m, n and p are defined as in claim 1. These compounds can be used as pharmaceutical compositions for the treatment of, for example, diabetes.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I:

Abstract: Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.

Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, m, and n are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.

Abstract: The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: R1-Het-D-E??[1] wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.

Abstract: The present invention relates to phthalimide carboxylic acid derivatives of formula (I), methods for their preparation, pharmaceutical compositions containing them and their use in medicine, specifically in the treatment of cancer. (I), wherein X is O or S; R1 is a phthalimide carboxylic acid group of formula (II).

Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said novel 3-heterocyclic benzylamides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides sulfonamides, and compositions and methods utilizing sulfonamides that are useful in the treatment of diseases by blocking potassium channels associated with the onset or recurrence of the indicated conditions. Exemplary diseases treatable with the compounds, compositions and methods of the invention include sickle cell disease and glaucoma.

Abstract: The present invention relates to compounds of formula (I) wherein R1 to R8 and n are as defined in the description and claims, and pharmaceutically acceptable salts and esters thereof. The compounds are useful for the treatment of diseases such as diabetes.

Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract: A process for producing heterocyclic compounds which are useful as pesticides, drugs, fungicidal materials or intermediates thereof. TosMIC is reacted with an aldehyde or an imino compound: 1) in a solvent mixture of an aprotic solvent with a protic solvent in the presence of a base, 2) in the presence of a phase-transfer catalyst and an inorganic base, or 3) in the presence of an inorganic base. Thus, a desired product can be efficiently obtained using a solution without isolating TosMIC which is irritating and unstable, has a low decomposition point and shows explosivity.

Abstract: The present invention provides compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4, A and n have the significance given in the specification. The compounds or their salts may be administered to a patient for treating non-insulin dependent diabetes mellitus.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein X is O or S X1 is O or S; X is S or O; R1 and R2 are independently H, methyl, or halogen; R4 and R5 are independently H or C1-3 alkyl or R4 and R5 may, together with the carbon atom to which they are bonded, form a 3–5 membered cycloalkyl ring; R6 and R7 are independently H, C1-3 alkyl, or allyl; each R3 is independently halogen, C1-6 straight or branched alkyl, or CF3; and y is 0, 1, 2, 3, 4 or 5 act as hPPAR alpha agonists.

Abstract: The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5?-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

Abstract: The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5?-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.

Abstract: Compounds having the formula (I), are effective as inhibitors of IMPDH enzyme, wherein R3 is alkyl, substituted alkyl, alkoxy, haloalkoxy, or halogen, preferably methoxy, ethoxy, or trifluoromethoxy; and R1, R2, R4, and R5 are as defined in the specification.

Abstract: Objects of the present invention are the compounds of formula (I) formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.

Abstract: This invention provides a heterocyclic compound having potent tyrosine kinase-inhibiting activity represented by the formula: wherein m is an integer of 1 to 3; n is an integer of 1 or 2; R1 is a halogen atom or an optionally halogenated C1-2 alkyl group; each of R2 and R3 is, same or different, a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; R4 is a group represented by the formula: wherein p is an integer of 2 to 5; R5 is a C1-4 alkyl group substituted by alkoxycarbonyl group, carbamoyl group, carbamoyloxy group, alkylsulfonyl group, alkylsulfinyl group, sulfamoyl group, carbamoylamino group, alkylsulfonylamino group, acylamino group, and the like; or a salt thereof and a pharmaceutical composition comprising thereof.

Abstract: The invention relates to new formulations for improving the local tolerance of intravenously administered 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of the pharmacologically acceptable acid addition salts thereof.

Abstract: The present invention relates generally to novel hydantoin derivative compounds, pharmaceutical compositions containing such compounds, and methods for their use in preventing and/or treating neurological disorders, including physically damaged nerves and neurodegenerative diseases; for treating alopecia and promoting hair growth; for treating vision disorders and/or improving vision; for treating memory impairment and/or enhancing memory performance; and for treating sensorineural hearing loss by administering such compounds.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: The present invention relates to compounds of formula (I) wherein wherein R1, R2, R3, R4, R5, R6 and n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.

Abstract: There is disclosed the use of a compound of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy.

Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4.

Abstract: aP2 inhibiting compounds are provided having the formula wherein R1, R2, R3, R4, X—Z and are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.

Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(-2-oxyazolylalkylthio)-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, CONR9, R10, 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: Disclosed are compounds of the general formula which are oxamide derivatives and inhibitors of the enzyme inosine monophosphate dehydrogenase (IMPDH).

Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.

Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.

Abstract: Methods and materials for preparing N2-alkylated triazoles, such as 3-{4-[3-(5-methyl-2-phenyl-oxazol-4-yl)-propyl]-phenyl}-2-[1,2,3]triazol-2-yl-propionic acid, are disclosed. Such compounds are PPAR agonists that are useful for treating non-insulin dependent diabetes.

Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia and hypercholesteremia in a mammal. The present invention also discloses method for making the disclosed compounds.

Abstract: Compounds of formula (I) 1

Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1

Abstract: The present invention is directed to a compound of Formula I: 1

Abstract: The present invention relates to bicyclic derivatives, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG/S1P receptor mediated signal transduction.

Abstract: This invention relates to compounds of the formula 1

Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

Abstract: This invention provides a heterocyclic compound having potent tyrosine kinase-inhibiting activity represented by the formula: 1

Abstract: Compounds of formula (I): and their salts, solvates, hydrates and prodrugs are useful PCP inhibitors, processes for making the same, compositions comprising the same, and methods of treating a PCP-mediated condition or disease using the same.

Abstract: The present invention is directed to a compound of Formula I: wherein A, R1, and R2 are defined herein. The present invention is also directed to compositions comprising compounds of Formula I, methods of using compounds of Formula I, and methods of making compounds of Formula I.

Abstract: The present invention 1 includes compounds of formula (I), 1

Abstract: Substituted 3-pyridyl oxazoles which inhibit C17, 20 Lyase, pharmaceutical preparations containing them, and methods of using them in treatment of cancer arc provided.

Abstract: An organometallic luminescent material comprising the compound of formula (I) of the present invention can emit pure blue light and have high thermal stability: wherein, M1 is a monovalent or tetravalent metal selected from the group consisting of Li, Na, K, Zr, Si, Ti, Sn, Cs, Fr, Rb, Hf, Pr, Pa, Ge, Pb, Tm and Md; R is hydrogen or C1-10 alkyl; B is O, S, Se or Te; D is O or S; and n is an integer ranging from 1 to 4.

Abstract: This invention relates to novel {overscore (&ohgr;)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.