Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1

Abstract: Compounds of the formula where the variables have the meaning defined in the specification, are specific or selective agonists of RXR retinoid receptors.

Abstract: An optical information recording medium has a recording layer composed essentially of an oxonol compound of the following formula: 1

Abstract: A compound of the formula: and its pharmaceutically effective salts, wherein R1 and R2 are independently selected from the following: (a) hydrogen, halo, R5—, C2-6 alkenyl, C2-6 alkynyl, hydroxy-R5—, R5—O—R5—, or the like; (b) Ar—, Ar—R5—, Ar—C2-6 alkenyl, Ar—C2-6 alkynyl, Ar—O—, Ar—O—R5— or the like; (c) R5—C(O)—, —NO2, cyano, NH2—C(O)—, R5—NH—C(O)—, (R5)2—N—C(O)—, Ar—C(O)— or the like; and (d) R5—C(O)—NH—, Ar—C(O)—NH— or the like; wherein Ar is optionally substituted aryl or heteroaryl such as phenyl and pyridyl; and wherein R5 is optionally halo-substituted C1-6 alkyl; R3 is selected from the following: (e) cyano, formyl, tetrazolyl, triazolyl, imidazolyl, oxazolyl, thiazolyl, R5—C(O)—, C2-6 alkenyl-C(O)—, C2-6 alkynyl-C(O)—, R5—C(O)—R5—, or the

Abstract: The present invention relates to compounds of formula (I): in which R1 represents a hydrogen or halogen atom, or a group CF3; R2 and R3 represent, independently, a hydrogen atom or a methyl group; n and n′ each represent, independently, 0 or 1; * represents the positions of attachment; A represents N or CH; X represents a sulfur or oxygen atom; R4 and R5 represent, independently, a hydrogen atom or a (C1-C6) alkyl group; and also their salts or solvates, to a method for the preparation thereof and to the pharmaceutical compositions containing them.

Abstract: A compound represented in general formula (X) and (XI):

Abstract: The present invention relates to novel bicyclic thiophene derivative compounds of the following formula: 1

Abstract: The present invention provides compounds of formula I and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula I.

Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1

Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydrobenzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.

Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1

Abstract: The instant invention provides novel benzothiophene compounds for use in treating skeletal diseases.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

Abstract: A compound of the formula 1

Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.

Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.

Abstract: 3-(amino- or aminoalkyl) pyridinone derivatives having the formula (1) 1

Abstract: Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable arylsulfonyl or heteroarylsulfonyl group attached to the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs. The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion.

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates to compounds of formula (I): 1

Abstract: Described are polymeric matrix compatibilized naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one substituent containing terminal and/or pendant groups selected from hydroxyl, carboxyl, sulfo, sulfono, (meth)acryloxy, 2-(methacryloxy)ethylcarbamyl, epoxy or a mixture thereof. Specific substituents are also present on the naphtho, indeno and/or pyrano portions of the compounds. These compounds may be represented by the following graphic formulae: Also described are various substrates that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, are also described.

Abstract: This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof; in which preferably R3, R4 and R6 are each hydrogen; X is C═O or CH2; and R7 and R8 are each independently selected from the group consisting of hydrogen, (C1-C12)alkyl, (C3-C8)cycloalkyl and (C1-C12)alkyl (C6-C14)aryl; or R7 and R8 when taken together form a (C2-C7)alkylene group; or —NR7R8 together forms a (C2-C14)heterocyclic or substituted (C2-C14)heterocyclic. Such compounds modulate the activity of serine hydrolases and can be used in pharmaceutical compositions for the treatment of Alzheimer's disease.

Abstract: The present invention provides compounds having the Formula I 1

Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.

Abstract: A compound of formula (I): 1

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R5 is hydrogen or C1-C6 alkyl; and R represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.

Abstract: Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments are disclosed.

Abstract: The present invention provides bis-aminomethylcarbonyl compounds that are inhibitors of cysteine and serine proteases. The compounds are particularly useful for treating diseases in which excess cysteine protease activity has been implicated, including osteoporosis, periodontitis and arthritis.

Abstract: Compounds of the formula Where the variables are defined as in the specification, are selective agonists of RXR retinoid receptors.

Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo [c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.

Abstract: Disclosed are new organometallic complex molecules having light-emitting and electron-transporting characteristics. Also disclosed is organic EL (electroluminescent) devices using these organometallic complex molecules as electron-transporting materials. The organometallic complex molecules are used to form a light-emitting layer with or without doping of another light-emitting material. The organometallic complex molecules can also be used in an electron-transporting layer of the organic EL device. The organic EL devices incorporating the organometallic complex molecules have high thermal stability.

Abstract: This invention is directed to compounds of formula (III): wherein B, C, D, E, R1, R2 and R3 are disclosed herein. These components are disclosed as being useful as anti-coagulants.

Abstract: 1,3-Disubstituted Indolin-2-Ones compounds are useful in the treatment of neoplasia.

Abstract: Heterocyclic-substituted compounds of the formula 1

Abstract: This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R2)W, —C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, —CH(R4)CH2CO2R3, —COR3, or —PO3(R3)2; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or —CH2(3-pyridyl); W is —CO R3, —CONH2, —CONHOH, —CN, CONH(CH2)2CN, 5-tetrazole, or —PO3(R3)2; R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: The present invention relates to the compounds of formula (I) in which X, R1, R2 and R3 are as defined in claim 1. These compounds are cholesteryl acyl transferase (ACAT) inhibitors.

Abstract: A compound selected from those of formula (I): wherein: X represents oxygen, sulphur, or NR3 wherein R3 is as defined in the description, Y represents oxygen, sulphur, NR3, or may represent single bond in certain cases, T represents nitrogen, carbon, or CH, A represents single bond, alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, or —SO2—R4— wherein R4 is as defined in the description, W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycloalkyloxy or heteroaryloxy, or hydroxyamino, U1 represents hetero, or alkylene wherein one or more of carbon may optionally be replaced by one or more hetero atoms, V1 represents arylene, heteroarylene,or heterocycloalkylene, U2 represents single bond, hetero or alkylene wherein one or more carbon may optionally be replaced by one or more hetero atoms, V2 represents aryl, heteroaryl, or heterocycloalkyl, Ra, Rb, Rc, which may be identical or different, each independently of the others r

Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.

Abstract: The present invention relates to 2-aminopyridine derivatives of the formula I: 1

Abstract: The present invention relates to pyridone derivatives and herbicidal compositions containing the pyridone derivatives as active ingredients.

Abstract: A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.

Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.

Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.

Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g.

Abstract: The invention is directed to improved methods for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.