Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: Compounds of the formula: useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating disorders, obesity, addictive disorders caused by ethanol or cocaine abuse and related illnesses.

Abstract: This invention relates to a series of substituted imidazoles of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention inhibit the production of a number of inflammatory cytokines, and are useful in the treatment of diseases associated with overproduction of inflammatory cytokines.

Abstract: Amlodipine fumarate salt compounds are useful as calcium channel blockers and in treating or preventing angina or hypertension. The fumarate salts avoid the formation of certain potential impurities that have been found to be associated with amlodipine maleate.

Abstract: A pyridine derivative represented by formula (1) wherein all the variables have been defined in the specification. The compounds are used for inhibiting collagen production and are useful for preventing or treating fibrosis.

Abstract: The present invention relates to a novel form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole, known under the generic name omeprazole. More specifically, it relates to a novel crystalline form of the potassium salt of the (S)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole. The present invention also relates to processes for preparing such a form of the potassium salt of (S)-omeprazole and pharmaceutical compositions containing it.

Abstract: The synthesis of memory enhancing, analgetic, and antidepressant N-alkyl-N-pyridinyl-1H-indol-1-armines is described.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, R4, R5, R6, X and Y are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock.

Abstract: A novel 3-hydroxypyridin-4-one compound of formula I is provided wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, R3 is selected from hydrogen and C1-6 alkyl; and R4 is selected from hydrogen, C1-6 alkyl and a group as described for R2; characterised in that R2 is selected from groups (i) —CONH—R5 (ii) —CH2NHCO—R5 (iii) —SO2NH—R5 (iv) —CH2NHSO2—R5 (v) —CR6R6OR7 (viii) —CONHCOR5  wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-3 alkyl, aryl and C7-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl, and R7 is selected from hydrogen, C1-13 alkyl, aryl and C7

Abstract: 2-phenylindoles are described, as well as a process for making them, pharmaceutical preparations that contain them, methods of using them as pharmaceutical agents.

Abstract: Compounds of the formula wherein R1, R2, R3, R4, X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.

Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.

Abstract: There is provided a solid pharmaceutical composition in a dosage form that is not enteric-coated, having active ingredients including a non-enteric coated proton pump inhibitor and at least one buffering agent. The proton pump inhibitor is omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, or an enantiomer, isomer, derivative, free base, or salt thereof, in an amount of approximately 5 mg to approximately 300 mg; and the buffering agent is in an amount of approximately 0.1 mEq to approximately 2.5 mEq per mg of proton pump inhibitor. The dosage form includes a suspension tablet, a chewable tablet, an effervescent powder, or an effervescent tablet. Also provided is a method for treating an acid-related gastrointestinal disorder in a subject in need thereof by administering to the subject a solid pharmaceutical composition.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprises of amino and piperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where X is CH or N As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.

Abstract: This invention provides compounds, and pharmaceutically acceptable salts thereof, having the structure shown below, as well as related pharmaceutical compositions, and methods of treatment and synthesis.

Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2, 2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.

Abstract: The present invention relates to a novel class of N,N′-di substituted hydantoin hydroxamates capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.

Abstract: Compounds of formula I wherein: R1 is pyridyl optionally substituted with halogen, C1-4 alkyl, C1-4 alkenyl, CN, Me2N, CO2Me, OMe, aryl, heterocyclyl, or R4; R2 is CF3; halogen; CN; branched or unbranched C1-8 alkyl; branched or unbranched C1-8 alkenyl; C3-8 cycloalkyl optionally substituted with OH, CN, or methoxy; C1-8 alkoxy; C1-4 alkyloxyalkyl; C1-8 alkylthio; C1-4 alkylthioalkyl; C1-8 dialkylamino; C1-4 dialkylaminoalkyl; CO2R4; or aryl connected to the triazole in any position that makes a stable bond and wherein the aryl thereof is optionally substituted with halogen, C1-4 alkyl, C1-4 alkenyl, CN, Me2N, CO2Me, OMe, aryl, heterocyclyl, or R4; L is —NHC(O)—; —NHC(O)O—; —NHC(O)C(O)—; —NHC(S)—; —NH—; —NHC(O)NH—; —NHC(S)NH—; —NHCH2—; —NHCH(R5)—, wherein R5 is H, CN, C1-6 alkyl, C1-6 alkyloxyalkyl, C1-6 alkylthioalkyl, C1-6 alkylsulfinylalkyl, C1-6 alkylsulfonylalkyl, C3-6 cycloalk

Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors: