Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.

Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.

Abstract: Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.

Abstract: The invention provides a novel process for the synthesis of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one, the process comprising of reacting the salicylic acid with salicylamide in the presence of p-toluenesulfonyl chloride, base and solvent. The use of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one in the preparation of Deferasirox is also disclosed in the invention.

Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.

Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.

Abstract: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.

Abstract: The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound of formula (I): wherein —X? is —CR7? or —N?, ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2 a and R2 b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, R5 is hydrogen, substituted or unsubstituted alkyl or the like, each R6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins.

Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.

Abstract: Disclosed is a crystal of 2-(hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one useful as a preventive or therapeutic agent for obesity and the like. Specifically disclosed is a crystal of 2-(hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one having a powder X-ray diffraction pattern in which characteristic peaks appear at powder X-ray diffraction interplanar spacings (d) of around 16.54±0.2, 13.26±0.2, 4.70±0.2, 4.38±0.2, and 3.67±0.2?.

Abstract: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.

Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.

Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.

Abstract: The present invention includes compounds having structural formula (I): or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.

Abstract: The present invention provides redox drug derivatives. In particular, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, (3R,4R,5S)-4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid ethyl ester, (3S)-3-(aminomethyl)-5-methylhexanoic acid, (3S)-1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-?-?-diphenyl-3-pyrrolidineacetamide, (1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4-(diaminomethylideneamino)-2-hydroxy-cyclopentane-1-carboxylic acid and (2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid redox derivatives.

Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.