1,2-Amino Alcohols and Their Heterocyclic Derivatives as Chiral Auxiliaries in Asymmetric Synthesis

4. Biosynthesis of Leukotrienes 5869 4.1. Discovery of the Leukotriene Pathway and a Common Unstable Intermediate 5869 4.2. Conversion of Arachidonic Acid into Leukotriene A4 (LTA4) Is a Two-Step Concerted Reaction Catalyzed by a Single Lipoxygenase 5869 4.3. Structural Elucidation of Slow-Reacting Substance of Anaphylaxis, A Mixture of Leukotrienes 5870 5. Enzymes and Proteins in Leukotriene Biosynthesis 5870 5.1. Cytosolic Phospholipase A2α (cPLA2α) 5870 5.1.1. Molecular Properties and Regulation of cPLA2α 5870 5.1.2. Crystal Structure and Catalytic Mechanism of cPLA2α 5871 5.2. 5-Lipoxygenase (5-LO) 5871 5.2.1. Cellular Expression of 5-LO 5871 5.2.2. Regulation of 5-LO Gene (ALOX5) Transcription 5872 5.2.3. Naturally Occurring Mutations in the Gene Promoter of 5-LO 5872 5.2.4. Allosteric and Post-translational Regulation of 5-LO 5872 5.2.5. Structure function relationships in 5-LO 5872 5.2.6. Crystal Structure of 5-LO 5872 5.3. 5-Lipoxygenase-Activating Protein (FLAP) 5873 5.3.1. FLAP Is Critical for Cellular 5-LO Activity 5873 5.3.2. Effects of FLAP on Leukotriene Production 5873 5.3.3. FLAP Gene (ALOX5AP) and Regulation of Expression 5874 5.3.4. Crystal Structure of FLAP 5874 5.4. LTA4 Hydrolase 5874 5.4.1. LTA4 Hydrolase Is a Substrate-Selective and Suicide-Inactivated Epoxide Hydrolase 5874 5.4.2. LTA4 Hydrolase Is Bifunctional and Belongs to the M1 Family of Zinc Metallopeptidases 5874 5.4.3. LTA4 Hydrolase Cleaves the Chemotactic Pro-Gly-Pro, a Role for the Aminopeptidase Activity during Resolution of Inflammation 5875 5.4.4. Crystal Structure of LTA4 Hydrolase 5875 5.4.5. Mechanism of the Epoxide Hydrolase Reaction 5876 5.4.6. Mechanism of the Aminopeptidase Activity 5876 5.4.7. Two Catalytic Activities Exerted via Specific but Overlapping Active Sites 5877 5.5. LTC4 Synthase 5877 5.5.1. Molecular Properties of LTC4 Synthase 5877 5.5.2. LTC4 Synthase Is a Member of the MAPEG Superfamily of IntegralMembraneProteins 5877 5.5.3. Gene Structure and Regulation of LTC4 Synthase Expression 5877 5.5.4. Crystal Structure of LTC4 Synthase 5877 5.5.5. Catalytic Mechanism of LTC4 Synthase 5878 6. Intracellular Protein Trafficking and Compartmentalization of Leukotriene Biosynthesis 5878 6.1. Translocation of cPLA2α 5878 6.2. Translocation of 5-LO and Association with FLAP on the Nuclear Envelope 5879 6.2.1. 5-LO in the Nucleoplasm 5879 6.2.2. Organization of a Leukotriene Biosynthetic Complex in the Nuclear Membrane 5879 6.3. Leukotriene Biosynthesis in Lipid Bodies and Actions on Extracellular Granules 5879

Lipoxygenase and leukotriene pathways: biochemistry, biology, and roles in disease.

Applications of oxaziridines in organic synthesis

Random arrays of single molecules are provided for carrying out large scale analyses, particularly of biomolecules, such as genomic DNA, cDNAs, proteins, and the like. In one aspect, arrays of the invention comprise concatemers of DNA fragments that are randomly disposed on a regular array of discrete spaced apart regions, such that substantially all such regions contain no more than a single concatemer. Preferably, such regions have areas substantially less than 1 μm 2 and have nearest neighbor distances that permit optical resolution of on the order of 10 9 single molecules per cm 2 . Many analytical chemistries can be applied to random arrays of the invention, including sequencing by hybridization chemistries, sequencing by synthesis chemistries, SNP detection chemistries, and the like, to greatly expand the scale and potential applications of such techniques.

Single Molecule Arrays for Genetic and Chemical Analysis

The invention encompasses the novel compound of Formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).

Phenyl heterocycles as COX-2 inhibitors

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), whrein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R?2 and R3? are not both hydrido; further provided that R2 is not carboxyl or methyl when R3 is hydrido and when R4 is phenyl; further provided that R4 is not triazolyl when R2 is methyl; further provided that R4 is not aralkenyl when R2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R4 is not phenyl when R2 is methyl and R3 is carboxyl; and further provided that R4 is not unsubstituted thienyl when R2 is trifluoromethyl; or a pharmaceutically acceptable salt thereof.

Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation

Improved Procedure for the Reduction of N-Acyloxazolidinones

A class of 3,4-diaryl substitued thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I), wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R?2 and R3? are independently aryl or heteroaryl; and wherein R?2 and R3? are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.

Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents

A class of 1,3,5-substituted pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of formula (I) wherein R1 is lower alkylsulfonyl or sulfamyl; wherein R2 is aryl or heteroaryl; wherein R2 is optionally substituted at a substitutable position with one or more radicals selected from halo, lower alkoxy, lower alkyl, nitro, lower alkylthio, amino, lower haloalkyl, hydroxyl, carboxyl, N-monoalkylamino, N,N-dialkylamino, cyano, alkoxycarbonyl and acylamino; wherein R3 is selected from hydrido, lower alkyl, lower haloalkyl, cyano, carboxyl, alkoxycarbonyl, amino, acyl, acylamino, halo and alkylsulfonylamino; wherein R4 is aryl or heteroaryl; wherein R4 is optionally substituted at a substitutable postion with one or more radicals selected from halo, lower alkoxy, lower alkyl, nitro, lower alkylthio, amino, lower haloalkyl, hydroxyl, carboxyl, N-monoalkylamino, N,N-dialkylamino, cyano, alkoxycarbonyl and acylamino; provided at least one or R?2 and R4? cannot be phenyl or substituted triazole, when R1 is sulfamyl; further provided R2 cannot be 4-methoxyphenyl or 4-methylphenyl when R4 is 4-methoxyphenyl or 4-methylphenyl, and when R1 is sulfamyl; and further provided that R2 cannot be tetrazole when R4 is fluorophenyl, and when R1 is methylsulfonyl; or a pharmaceutically-acceptable salt thereof.

1,3,5 trisubstituted pyrazole compounds for treatment of inflammation

A class of substituted thiazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula (II), wherein R4 is selected from alkyl and amino, wherein R5 is selected from aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R5 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, aminosulfonyl, alkyl, alkenyl, alkynyl, cyano, carboxyl, carboxyalkyl, alkoxycarbonyl, aminocarbonyl, acyl, N-alkylaminocarbonyl, N-arylaminocarbonyl, N,N-dialkylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, haloalkoxy, amino, N-alkylamino, N,N-dialkylamino, heterocyclic and nitro; and wherein R6 is selected from halo, amino, alkoxy, nitro, hydroxyl, aminocarbonyl, acyl, alkylaminocarbonyl, arylaminocarbonyl, alkenyl, alkynyl, haloalkoxy, alkylamino, arylamino, aralkylamino, alkoxycarbonylalkyl, alkylaminoalkyl, heterocycloalkyl, aralkyl, cyanoalkyl, N-alkylsulfonylamino, heteroarylsulfonylalkyl, heteroarylsulfonylhaloalkyl, aryloxyalkyl, aralkyloxyalkyl, aryl and heterocyclo, wherein the aryl and heterocyclo radicals are optionally substituted at a substitutable position with one or more radicals selected from halo, alkyl, alkoxy, alkylthio, alkylsulfinyl, haloalkyl, haloalkoxy, carboxyalkyl, alkoxycarbonyl, aminocarbonyl, amino, acyl and alkylamino; or a pharmaceutically-acceptable salt thereof.

Substituted thiazoles for the treatment of inflammation

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