Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: Compounds comprising Formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-16. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.

Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.

Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.

Abstract: Ruthenium nanoparticles supported on non-cross-linked soluble polystyrene were prepared by reacting [RuCl2(C6H5CO2Et)]2 with polystyrene in open air. They effectively catalyze intra- and intermolecular carbenoid insertion into C—H and N—H bonds, alkene cyclopropanation, and ammonium ylide/[2,3]-sigmatropic rearrangement reactions. This supported ruthenium catalyst is much more reactive than [RuCl2(p-cymene)]2 and Ru(Por)CO] for catalytic intermolecular carbenoid C—H bond insertion into saturated alkanes. By using a-diazoacetamide as a substrate for intramolecular carbenoid C—H insertion, the supported ruthenium catalyst can be to recovered and reused for ten successive iterations without significant loss of activity.

Abstract: 4-(Substituted phenyl)hexahydropyrido[2,1-c][1,4]oxazin-6-one represented by formula (I) or a salt thereof is useful as an intermediate for the production of a bicyclic cinnamide compound which is an A? production inhibitor. 4-(Substituted phenyl)hexahydropyrido[2,1-c][1,4]oxazin-6-one or the salt thereof can be produced in an industrially advantageous manner by subjecting a compound represented by formula (II) or a salt thereof to an intramolecular condensation reaction.

Abstract: The present invention relates to a use of a specific alpha-arylmethoxyacrylate derivative, or its pharmacologically acceptable salt or solvate for preventing and treating metabolic bone diseases.

Abstract: This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome proliferator-activated receptors (PPAR), in particular the PPAR? suptype.

Abstract: The present invention provides ?-hydroxy benzeneacetic acid derivatives of the formula as defined in the specification which is a precursor indispensable for synthesis of compounds having two 5-membered lactone rings fused to central cyclohexa-1,4-diene nucleus, and a process of easily preparing the same. According to the preparation process of the present invention, the ?-hydroxy benzeneacetic acid derivative can be readily prepared at high purity and yield without using toxic materials or producing toxic by-products. Some novel compounds, synthesized by using such a ?-hydroxy benzeneacetic acid derivative, have excellent fastness properties, dye fixing rate and leveling property to general synthetic fiber materials such as polyester fibers and their blends with other fibers, especially to micro fibers, and also can be used as a coloring agent for plastic resins, color tonors, color filters, etc.

Abstract: An improved process for preparing o-chloromethylphenylglyoxylic esters of the formula which comprises converting a compound of the formula by reaction with magnesium into the corresponding Grignard reagent which is then reacted with a compound of the formula to give the compound of the formula which is then cleaved by reaction with a chloroformic ester of the formula CICOOR4 or by reaction with phosgene to give the compound of the formula (I), followed by the isolation of the compound of the formula (I), and also an improved process for preparing (E)-2-(2-chloromethylphenyl)-2-alkoximinoacetic esters of the formula and intermediates for their preparation.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.

Abstract: Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

Abstract: The present invention relates to a highly pure (2R,3S)-4-benzyl-3-(4-fluorophenyl)morpholin-2-yl 3,5-bis(trifluoromethyl)benzoate of Formula II, and a process for its preparation. The present invention further provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof, using the highly pure compound of Formula II. The present invention also provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof which comprises of cyclising the compound of Formula VII at elevated temperature, in the absence of solvent.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: Therapeutic compounds are disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed. The compounds described herein are used to treat ocular conditions, bowel disease and baldness.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention relates to processes for preparing carboxylic acid derivatives, comprising the reaction of at least one carboxylic acid and/or of a carboxylic acid derivative with at least one alcohol and/or an amine in the presence of a metal-containing catalyst, wherein, after the reaction has ended, the metal-containing catalyst is contacted with water and a superabsorbent, the contacting of the catalyst with the water leading to hydrolysis of the catalyst. The present invention further relates to the use of superabsorbents for removing a metal-containing catalyst from a mixture after hydrolysis of the catalyst.

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt or stereoisomer thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

Abstract: The present invention relates to compounds having the general formula (I) with the definitions of A, X, R1-R6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of ?-secretase activity.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.

Abstract: Compounds of formula (I) have been found to be useful as inhibitors of DDAH.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.

Abstract: The present invention relates to photochromic 2H-naphtho[1,2-b]pyrans as well as their use in synthetic resins of all types, especially for ophthalmic purposes. In particular, the present invention relates to photochromic naphthopyran compounds, for which a further ring system is bonded to the f side of the naphthopyran. The inventive photochromic dyes generally have the general formula (I) wherein n, R1, R2, R3, X, B and B? are defined as in claim 1. The inventive compounds are distinguished by good darkening and decolorizing properties and a very good service life.

Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.

Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.

Abstract: This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein the variables are as defined herein.

Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.

Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.

Abstract: The invention relates to a process for preparing enantiomer-enriched 3-heteroaryl-3-hydroxypropanoic acid derivatives and 3-heteroaryl-1-aminopropan-3-ols, and to their use.

Abstract: The present invention relates to a process for effectively preparing prostaglandin derivatives and to a stereospecific alkyl halide containing 15S-alcohol group as a starting material.

Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.

Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the &agr;&ngr;&bgr;3 and/or the &agr;&ngr;&bgr;5 integrin without significantly antagonizing the IIb/IIIa integrin.

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.

Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I, Formula (I) wherein R1 is (C1-3)alkyloxy, (C1-3)alkyloxy(C1-3)alkyl, (C1-3)alkylthio, (C1-3)alkylthio(C1-3)alkyl, (C1-3)alkylsulfinyl, (C1-3)alkylsulfinyl(C1-3)alkyl, (C1-3)alkylsulfonyl, (C1-3)alkylsulfonyl(C1-3)alkyl, (C1-3)alkyloxycarbonyl, (CH2)n—CO—NR8R9? or (CH2)n—NR8R9?; n is 0, 1 or 2; R2 is hydrogen or (C1-3?)alkyl; R3 is (C1-3)alkyl or (C1-3)alkyloxy(C1-3?)alkyl; R4 is (C1-3)alkyloxy(C1-3)alkyl; or R3 and R4 form together with the nitrogen atom to which they are bound a 5-, 6-, or 7-membered ring, optionally containing a further heteroatom selected from O and S, and which ring may optionally contain a double bond and be optionally substituted with (C1-3)alkyl or (C1-3)alkyloxy; R5 and R6 are independently (C1-3)alkyl; R7 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R8 and R9 are independently (C1-3)alkyl; or R8 and R9 form together with

Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula 1

Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”) , apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.

Abstract: Disclosed herein are novel morpholinoketone derivatives of formula (I): 1

Abstract: O-medium alkyl esters of diflunisal and related compounds are disclosed having anti-platelet activity, hydroxy radical scavenging properties, enhanced hepatic clearance and low ulcerogenic potential. These compounds have general formula (I) wherein n equals 3-13.

Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: Compounds of formula (1) containing sterically hindered groups, polymers thereof and the use of these polymers in papermaking processes and dewatering processes.