Abstract: Isoindolin-1-one-substituted propionamide glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: The invention provides improved and simplified methods of synthesizing ligands containing a heteroatom-bearing bridge using a novel intermediate compound. The ligands may be used to form metal complexes that are useful in diagnostic and therapeutic applications.

Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1): and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.

Abstract: Compounds of the formula where W is n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is —O—, —S—, —NH, or —CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or —Q—R4; R2 and R3 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, —COR3, —CO2R8, —CONR9R10, —OR3, —SO2NR9R10, or —S(O)4R9; R9 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three- to seven-membered alkyl ring or a three- to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 to C3 alkyl; R11 is hydrogen, —OR12, or —NHCOR12; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alk

Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.

Abstract: The invention provides improved and simplified methods of synthesizing ligands containing a heteroatom-bearing bridge using a novel intermediate compound. The ligands may be used to form metal complexes that are useful in diagnostic and therapeutic applications.

Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.

Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.

Abstract: Compounds of the formula where W is are particularly useful in treating migraine and other disorders, such as depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, pain and chronic paroxysmal hemicrania and headache associated with vascular disorders. The compounds can also be used as centrally acting antihypertensives and vasodilators.

Abstract: This invention involves compounds having the following structure: wherein: a) R1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R2 and R3 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo; c) R4, R5 and R6 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino; halo; and 2-imidazolinylamino; and wherein one and only one of R4, R5 and R6 is 2-imidazolinylamino; d) R7 is selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo;

Abstract: An imidazole derivative of formula (I) or a pharmaceutically acceptable salt or derivative thereof. The compounds of formula I exhibit affinity for alpha2 adrenoceptors.

Abstract: Compounds of the formula where W is n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is —O—, —S—, —NH, or —CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 ; alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or —Q—R4; R2 and R3 are each independently hydrogen, Cl1 to C8 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, —COR8, —CO2R9, —CONR9R10, —OR8, —SO2NR8R10, or —S(O)4R9; R9 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three- to seven-membered alkyl ring or a three- to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 to C3 alkyl; R11 is hydrogen, —OR12, or —NHCOR12; R12 is hydrogen, C1 to C4 alkyl, aryl, or C1 to C3

Abstract: A description is given of diphenyl compounds of formula wherein R is a camphor or hydantoin derivative; and R1 is hydrogen; or C1-C5alkyl. These compounds are suitable as light stabilizers in cosmetic, pharmaceutical and veterinary formulations.

Abstract: Novel compounds of formula I: 1

Abstract: This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: Novel 5-benzyl-octahydroindoles and 6-benzyl-decahydroquinolines substituted in the 1-position are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

Abstract: The present invention relates to novel imidazoly 2-indolinones and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

Abstract: Compounds of formula I, 1

Abstract: The present invention relates to compounds of formula (I) wherein: Ar1 or Ar2 is an optionally substituted indole, and the other group is an optionally substituted aromatic or heteroaromatic group, preferably an optionally substituted indole, X is O or S, and R2 is H, hydroxy, amino, C1-6alkyl, hydroxyC1-6alkyl or aminoC1-6alkyl, and salts and solvates thereof and solvates of such salts, and the use of such compounds in medical therapies.

Abstract: Phenylazole compounds represented by general formula (1) or pharmaceutically acceptable salts thereof and drugs for hyperlipemia which contain these compounds as the active ingredient, wherein A represents imidazolyl, pyrazolyl, etc.; B represents (1a) or (1b) (wherein R2 and R3 represent each hydrogen, C1-6 alkyl, etc; and k is 0 or an integer of 1 to 15); Y represents O, S, a bond, etc.; and Z represents an optionally substituted and saturated or unsaturated heterocycle containing 1 to 4 N, O or S atoms. Among all, compounds wherein Z is substituted chroman-2-yl, 2,3-dihydrobenzofuran-2-yl, etc. have an effect of inhibiting the formation of lipid peroxides too.

Abstract: The present invention relates to compounds of formula (I): wherein: Ar is an optionally substituted aromatic or heteroaromatic group, R1 is H, C1-6alkyl, CF3, phenyl, benzyl, carboC1-6alkoxy, carbamoyl, or methyl(N—C1-6alkylcarbamoyl) R2 is H, C1-6alkyl, aminoC1-6alkyl, hydroxyC1-6alkyl, (mono- or di- C1-6alkyl)aminoC1-6alkyl, (aminoC1-3alkylphenyl)C1-3alkyl, amidinothio C1-6alkyl, R3 is H or C1-6alkoxy, R4 is H or together with R2, forms an annulated ring which may be substituted by hydroxyC1-3alkyl or amidinothio C1-3alkyl, or aminoC1-3alkyl; and pharmaceutically acceptable salts thereof; and the use of such compounds in medical therapies.

Abstract: An imidazole derivative of formula (I) 1

Abstract: A compound of the formula: wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralklyl, or the like, R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, or the like, X is hydroxy or optionally substituted amino, Y is COOR R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl, has integrase inhibition activity, and is useful as an anti-HIV drug.

Abstract: A method for the prophylaxis or treatment of conditions for which 5-HT1-like agonists are indicated comprising the administration of therapeutically-effective amount of compounds of formula (I) 1

Abstract: 3-Substituted indole carbohydrazides having the formula are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.

Abstract: Compounds of formula (I), wherein A and A are independently the same or different group of formula (II) wherein: R′ is H, CH3, C(CH3)2,—ORa, —N(Ra)2, —N(Ra)ORa or -DP; R is H or CH3; Ra is H, C1-C3 alkyl; D is a bond, alkylene, —C(═O)—, —S(O)— or S(O)2—; P is an optionally substituted, mono or bicyclic carbo- or hetereocycle; R″ is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or —C(═O)N(R′″)-; Q is absent, a bond, —CH(OH)— or CH2—; or R″ together with Q, M and R define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R is —ORa, -, N(Ra)2, —N(Ra)ORa or -DP, if M is a bond and Q is absent; X is H, OH, OCH3, Y is H, OH, OCH3, but X and Y are not both H; Z′ and Z″ are independently —(

Abstract: The present invention relates to novel imidazoly 2-indolinones and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

Abstract: Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.

Abstract: Disclosed are 4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. The compounds of the invention 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 the foregoing compounds, methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis using these compounds, as well as intermediates useful in the preparation of compounds of the invention.

Abstract: Urocanic acid derivatives useful as antiallergic agents represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R2 denotes hydrogen or lower alkyl, R3 denotes nitro, amino, cyano or COOR2, wherein R2 in said COOR2 is as defined above, and Q denotes carbon or nitrogen.

Abstract: Disclosed are 4-aryloxindoles that 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 the foregoing compounds, as well as methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis, using said compounds.

Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: The subject invention pertains to compounds which are useful as antiinflammatory agents and to compositions containing such compounds as active ingredients. The novel uses of the compounds relate to the anti-neurogenic inflammatory properties of the disclosed bis-heterocyclic compounds. Specifically exemplified herein are dragmacidin f, topsentin d, and topsentin e, and their salts, analogs, and derivatives.

Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof, or prodrug esters thereof, A is where Z is N or CH, or where Z is  or CH2 when is a single bond; and wherein L1, R, R1, R3, R3′, R3a, R3b, R4, R4′, R5, R5a, X,  are as defined herein.

Abstract: Disclosed are substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds.

Abstract: This invention relates to herbicidal compounds of formula (I), methods of making such herbicidal compounds and methods of using such herbicidal compounds. It has been found that compounds of formula (I) are useful as pre-emergent and post-emergent herbicides. Formula (I) is as follows: where Q, X, Y, n, and R are as described herein. This invention is also directed to intermediates used in the preparation of such herbicidal compounds.

Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.

Abstract: Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula and the pharmaceutically acceptable salts thereof. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.

Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic delivery of such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: The present invention relates to small peptides that cause penile erections in male animals when injected into the paraventricular nucleus of the hypothalamus or when given systemically (intravenously or subcutaneously) to such animals. These peptides are useful in the treatment of erectile dysfunction.

Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

Abstract: This invention provides a series of substituted 2-imidazolines which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these compounds.