Abstract: The present invention relates to tricyclic 2-pyrimidone compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: The compounds of formula I in which R1, R2, R3, R4 and R5 have the meanings as given in the description are PDE4/7 inhibitors.

Abstract: Disclosed are sulfonylquinoxalone derivatives of the general formula: These compounds are useful as bradykinin antagonists.

Abstract: The compounds of formula I in which the given substituents have the meanings as given in the description, are novel effective PDE4 inhibitors.

Abstract: Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphercal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

Abstract: The invention relates to a process for preparing enantiomerically enriched aryl-aminopropanols and to their use and also to intermediates.

Abstract: Hydroxy-imino derivatives of formula IIb are disclosed, in which R and R1 have the meanings given in the description.

Abstract: An ultraviolet radiation absorbent for thermoplastic polymer materials such as polyethylene terephthalate or polycarbonate contains cyclic imino ester compound of a specified structure in an amount of over 99.5 weight % and less than 100 weight % and having an acid value in the range of 1×10?3–1 and/or a chlorine ion content in the range of 1×10?1–1×103 ppm.

Abstract: This invention pertains to compounds of Formula I: and the pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to Hsp90 complex modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including chronic myeloid leukemia, melanoma, breast, ovarian, brain, thyroid, colorectal, prostate, and bladder cancer, heart disease, stroke, autoimmune/inflammatory diseases, and neurodegenerative diseases.

Abstract: The present invention relates to 8-amino-aryl-substituted imidazopyrazines which modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: Methods for the preparation of pharmaceutically acceptable organic or inorganic salts of 5-methylpyrazinecarboxylic acid-4-oxide esters including tris(hydroxymethyl)aminomethanol, N,N-dimethylethanolamine, N-methyl-D-glucamine, L-Lysine, L-arginine, Na, K, Ca and Mg. The esters of 5-methylpyrazinecarboxylic acid-4-oxide are oxidized in aqueous hydrogen peroxide at a pH of 2.5 to 7 in the presence of a catalyst selected from the group consisting of sodium tungstate, tungstic acid and ammonium heptamolybdate. The salts are formed by saponification of the esters followed by alcohol precipitation, or by reaction with a metal trimethylsilanoate, or by the reaction of organic bases with the saponified acids.

Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.

Abstract: This invention pertains to a method for flavoring an ingestible composition with a flavoring agent in organoleptically purified form, unaccompanied by substances of natural origin present in mango. The flavoring agent may be used in a wide variety of ingestible vehicles such as chewing gum compositions, hard and soft confections, dairy products, beverage products including juice drinks and juice products, green vegetable and chicken products, and the like. The present invention also pertains to an ingestible composition comprising an ingestible vehicle and an organoleptically effective amount of the purified flavoring agent. The present invention further pertains to ethyl 3-mercaptobutyrate represented by the formula, CH3(SH)CHCH2COOCH2CH3, in purified form, unaccompanied by substances of natural origin present in mango.

Abstract: The present invention provides a novel a condensed polycyclic compound useful as a phosphodiesterase 4 inhibitor, which is shown by the formula [I]: or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same.

Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.

Abstract: Highly pure triethylenediamine is obtained by a process in which triethylenediamine is freed from high boilers and then the triethylenediamine is vaporized from the mixture thus obtained and is passed into a liquid solvent. The process makes it possible in particular to obtain highly pure solutions of triethylenediamine. Crystallization is generally unnecessary.

Abstract: Methods for the preparation of pharmaceutically acceptable salts of 5-methylpyrazine-carboxylic acid-4-oxide by using the oxidizing agent OXONE® for the N-oxidation of C1-4 methylpyrazinecarboxylic acid esters. The pharmaceutically acceptable salts are then formed by the saponification of the esters followed by alcohol precipitation.

Abstract: An acrylate compound of formula (4): is produced by allowing an acrylic acid compound of formula (1): to react with an unsaturated compound of formula (2) or (3): In formulae (1) through (4), R1 and R2 are H or F, R3 is H, F, or an alkyl, alkenyl, fluoroalkyl or fluoroalkenyl group, R4 and R5 are H, halogen, or an alkyl, alkenyl, halogenated alkyl or halogenated alkenyl group; and X and Y are an unsubstituted or substituted hydrocarbon group, and dashed line - - - means that X and Y may be bonded together to form a cyclic structure.

Abstract: The present invention concerns compounds of general formula (I): in which the substituents are as described herein.

Abstract: The present invention provides a method for industrially producing an optically active lysine derivative useful as a pharmaceutical intermediate. More particularly, the present invention provides a production method including protecting an amino group or an amino group and carboxyl group of optically active 2-amino-6-methyl-6-nitroheptanoic acid with a protecting group, reducing a nitro group to synthesize a 6,6-dimethyl lysine derivative and reacting the 6,6-dimethyl lysine derivative with an acetic acid derivative.