Abstract: A compound of the having the general formula (I) or general formula (II): wherein Z, A, B, C, R1, R2, Q, W, and n are as described herein.

Abstract: The present invention is concerned with solid oral dosage forms of comprising a) an active agent selected from valsartan and optionally HCTZ, and b) Pharmaceutically acceptable additives suitable for the preparation of solid oral dosage forms by compression methods.

Abstract: A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: The present invention provides a compound of the formula: 1

Abstract: Compounds having the formula 1

Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.

Abstract: The invention provides compound of the Formula: 1

Abstract: Compounds having the formula 1

Abstract: The present application describes lactam-containing diaminoalkyl, &bgr;-aminoacids, &agr;-aminoacids and derivatives thereof of Formula I:

Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula 1

Abstract: Use of an MPO inhibitor for the treatment of COPD.

Abstract: The invention relates to mercaptomethyl-substituted thiazolo[2,3-b]quinazolines, oxazolo[2,3-b]quinazolines and imidazolo[2,1-b]quinazolines.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animal, such as stroke.

Abstract: The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors: In formula (I), W is carbon or nitrogen, wherein at least one W is a carbon; and Y is nitrogen, oxygen, or sulfur. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.

Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.

Abstract: A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6 alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6 alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.

Abstract: Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.

Abstract: The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.

Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.

Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.

Abstract: Compound of formula (I): wherein: R1 represents hydroxy, RCO—O— or RCO—NRa—, R2 represents hydrogen, halogen, or hydroxy, R′CO—O or R′CO—NR′a—, R and R′, which may be identical or different, represent linear or branched (C1-C6)alkyl optionally substituted by aryl, linear or branched (C2-C6)alkenyl optionally substituted by aryl, linear or branched (C1-C6)perhaloalkyl, (C3-C7)cycloalkyl, adamantyl, aryl or heteroaryl, Ra and R′a, which may be identical or different, represent hydrogen or linear or branched (C1-C6)alkyl, linear or branched (C1-C6)perhaloalkyl, linear or branched (C1-C6)acyl, aryl or heteroaryl, its isomer and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as AMPA modulators.

Abstract: Certain derivatives of acridones and benzothiadiazines have been found to have anti-cancer properties by virtue of their specific inhibition of the cyclin D dependant kinase CDK4. These molecules inhibit CDK4 activity more than they inhibit the activity of other such kinases (e.g. CDC2 and CDK2). This specificity results in an improved therapeutic index when used as drugs to treat susceptible cancers.

Abstract: A compound of Formula I 1

Abstract: Nitrosylation of proteins and amino acid groups enables selective regulation of protein function, and also endows the proteins and amino acids with additional smooth muscle relaxant and platelet inhibitory capabilities. Thus, the invention relates to novel compounds achieved by nitrosylation of protein thiols. Such compounds include: S-nitroso-t-PA, S-nitroso-cathepsin; S-nitroso-lipoprotein; and S-nitroso-immunoglobulin. The invention also relates to therapeutic use of S-nitroso-protein compounds for regulating protein function, cellular metabolism and effecting vasodilation, platelet inhibition, relaxation of non-vascular smooth muscle, and increasing blood oxygen transport by hemoglobin and myoglobin. The compounds are also used to deliver nitric oxide in its most bioactive form in order to achieve the effects described above, or for in vitro nitrosylation of molecules present in the body.

Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.

Abstract: The present invention relates to a method of inhibiting or preventing infection and blood coagulation in or near a medical prosthetic device after the device has been inserted in a patient by administering to the device a pharmaceutically effective amount of a composition having: (A) at least one taurinamide derivative, and (B) at least one compound selected from the group consisting of biologically acceptable acids and biologically acceptable salts thereof, whereby there are no systemic anti-clotting and no systemic biocidal effects.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein X is nitrogen or CR3; A is O, S, or NR4, and R, R1, R2are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

Abstract: 1

Abstract: A compound of the having the general formula (I) or general formula (II): 1

Abstract: The present invention relates to the use of potassium channel agonists for the treatment of insulitis associated with various forms of diabetes such as IDDM, NIDDM, SPIDDM (LADA) and gestational diabetes.

Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen.

Abstract: The present invention is concerned with solid oral dosage forms of comprising a) an active agent selected from valsartan and optionally HCTZ , and b) Pharmaceutically acceptable additives suitable for the preparation of solid oral dosage forms by compression methods.

Abstract: The present invention relates to a novel processes for preparing pharmaceutically active fused 1,2,4-thiadiazine derivatives of general formula (I) as defined in the description and intermediates therefore.

Abstract: The present invention involves certain 8-ureido and 8-thioureido, 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the chemokine, Interleukin-8.

Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.

Abstract: The present invention relates to 4H-thieno[3,2-e]-1,2,4-thiadiazine derivatives of the general formula: 1

Abstract: This invention is directed to compounds of the formula 1

Abstract: Compounds of the formula 1

Abstract: Compound of formula (I): 1

Abstract: The present invention relates to the use of potassium channel agonists for the treatment of insulitis associated with various forms of diabetes such as IDDM, NIDDM, SPIDDM (LADA) and gestational diabetes.

Abstract: The present invention relates to 4H-thieno[3,2-e]-1,2,4-thiadiazine derivatives of the general formula: wherein X, Y, R1, R2 and R3 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: A pharmaceutical compound of the formula in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is —SR6, —SOR6, —SO2R6, —COR6, —CH2OH or —CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not —COR6 or —CONHR7; and salts thereof.

Abstract: Methods and compositions for treating ocular conditions which find their etiology in compromised ocular blood flow with brinzolamide and brimonidine are disclosed.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas 1

Abstract: The present invention is concerned with solid dosage forms comprising a) valsartan and optionally HCTZ, and b) pharmaceutically acceptable additives suitable for the preparation of solid oral dosage forms by compression methods.

Abstract: Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.

Abstract: The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer composition to a mammal, such as a human, whereby bile acids are sequestered. The polymers of the invention comprise spirobicyclic ammonium moieties and optionally, further comprise a hydrophobic substituent, a quaternary ammonium-containing substituent or a combination thereof.

Abstract: Methods and compositions for treating ocular conditions which find their etiology in compromised ocular blood flow with brinzolamide and brimonidine are disclosed.

Abstract: Methods for preventing or slowing visual field loss are disclosed.