Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.

Abstract: A process for preparing doxazosin mesylate in modification A which comprises dissolving doxazosin with methanesulfonic acid in methanol or a mixture of an aprotic, polar organic solvent and methanol, removing any turbidity from the resulting solution, and stirring the resulting clear solution until no further precipitate separates out, removing, washing with methanol, heating the precipitate in the moist state in ethanol and, after cooling, isolating the resulting product is described.

Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.

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, prodrugs and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, A, X, Y and Z are 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: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: A method of producing alkylene glycol esters of unbranched aliphatic dicarboxylic acids with limited homolog distribution, and the use of the esters produced as monomer structural units for producing polymers are disclosed.

Abstract: Compounds containing tetrahydrobenzindole which bind to serotonin receptor and are useful in treatment or prevention of disease induced by abnormality of central peripheral serotonin controlling functions.

Abstract: The present invention discloses compounds of formula (I), and tautomeric forms, pharmaceutically acceptable salts, or solvates thereof. Preferably, the compounds of the invention are dual activators of hPPAR&ggr; and hPPAR{acute over (&agr;)}.

Abstract: This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 2,4-diaminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula I: and Formula II: where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R8 and R9 include hydrogen and alkyl, and Z is carboxy. This invention also provides pharmaceutical formulations comprising a compound of Formula I or II together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.

Abstract: The present invention relates to novel thio-aminotetralin compounds of the formula (I) wherein Z, X, R1, R2, R3, R4, R5, and R6 are defined herein. The compounds are useful in pain management.

Abstract: The present invention relates to novel amidino compounds of formula (I), or a salt, solvate, or physiologically functional derivative thereof; wherein R1 is selected from C1-4 alkyl, C3-4 cycloalkyl, C1-4 hydroxyalkyl, and C1-4 haloalkyl; to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.

Abstract: Thienopyrimidines of the formula I and their physiologically acceptable salts, in which R1, R2 and X have the meanings given in claim 1, inhibit phosphodiesterase V and can be employed for the treatment of illnesses of the cardiovascular system and for the treatment and/or therapy of impaired potency.

Abstract: The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.

Abstract: This invention encompasses a process for making a compound of Formula A These compounds are intermediates useful in the preparation of certain non-steroidal anti-inflammnatory agents.

Abstract: New imidazotriazolopyrimidine derivatives of the formula Preferred are those compounds wherein: R1 denotes methyl, which is optionally substituted by phenyloxy or pyrrole; or R1 denotes benzyl which is optionally substituted by hydroxy, methoxy, dimethylaminoethoxy or fluorine; or R1 denotes cyclopentyl, furan or phenylethyl; R2 or R3 denote ethyl, n-propyl, allyl or propargyl; R4 or R6 denote hydrogen; and, R5 denotes methyl, n-propyl, tert.butyl, cyclopentyl or norbornenyl. These are adenosine antagonists are are useful for, inter alia, the treatment of senile dementia of the Alzheimer's type.

Abstract: Processes are disclosed for the oxidation of alkanes such as, for example, propane, to form unsaturated carboxylic aldehydes and acids such as, for example, acrolein and acrylic acid. The processes utilize oxygen and recycle alkanes, e.g. propane, to the aldehyde reactor. The presence of the alkane-to-aldehyde reaction can enhance the efficiency of the processes.

Abstract: The present invention relates to novel &bgr;-carboline derivatives of the general formula wherein all the variables are as described within the specification, useful as phosphodiesterase inhibitors. The present invention further relates to use of the described derivatives for the treatment of diseases and conditions related to PDE, for example male erectile dysfunction.

Abstract: This invention relates to compounds of formula (I), wherein A, B, D, E, K, G, Z, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. Compounds (I) are corticotropin releasing factor (hormone) CRF (CRH) antagonists.

Abstract: The invention relates to compounds of the formulas 1 and 2 and to pharmaceutically acceptable salts and hydrates thereof, wherein X1, R1, R2 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1 and 2 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formulas 1 and 2.

Abstract: A carboxylic acid tertiary alkyl ester (Chemical formula 1) of high purity is obtained at a high yield ratio, by continually adding an esterification agent possessing a monovalent acid group, which agent is ester-interchangeable with a tertiary alcohol, to a mixed fluid of a carboxylic acid and a tertiary alcohol: R1(COOR2)n.