Abstract: A supported gold catalyst is used for selective oxidation. In particular, an alcohol or ketone is oxidized to produce the corresponding carboxylic acid, an alcohol is oxidized to produce the corresponding ketone, and xylene is oxidized to produce the corresponding mono-alcohol or di-alcohol.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The invention relates to a process for the preparation of an ?-benzyl ester of an amino diacid, characterized in that the amino diacid is reacted with a benzyl alcohol derivative of formula (I) in which the R1 substituent or substituents, which are identical or different, represent a hydrogen atom, a C1 to C4 alkyl group, a C1 to C4 alkoxy group or a halogen atom and n is equal to 1, 2 or 3, in the presence of at least one mol per mole of the amino diacid of an alkanesulphonic acid, optionally in the presence of a solvent. The intermediate alkanesulphonates of the ?-benzyl esters of amino diacids and the ?-benzyl esters of amino diacids are obtained with a good yield and an excellent purity by virtue of this process.

Abstract: Compounds of the general formula (I) wherein R1 represents halogen, R2 and R3 represent H or halogen, and R4 represents C3-8-cycloalkyl or optionally substituted phenyl, pharamceutical compositions containing such materials, and methods of using such materials in the treatment of various diseases are disclosed and claimed.

Abstract: The invention relates to NEP inhibitors for treating cardiovascular disorders. Preferred NEP inhibitors are compounds of formula (I) wherein R1 is C1–C6alkyl, C1–C6alkoxyC1–C3alkyl or C1–C6alkoxyC1–C6alkoxyC1–C3alkyl; R2 is hydrogen or C1–C6alkyl; L is a three atom linkage selected from —CH2—X—CH2— and —CH2—CH2—X— where the right hand side of the linkage is attached to R3 and where X is oxygen, sulfur or methylene; R3 is phenyl or aromatic heterocyclyl, either of which may be independently substituted by one or more groups selected from: C1–C6alkyl, halo, haloC1–C6alkyl, C1–C6alkoxy, haloC1–C6alkoxy, C1–C6alkylthio, haloC1–C6alkylthio and nitrile; and R4 and R5 are either both hydrogen, or one of R4 and R5 is hydrogen and the other is a biolabile ester-forming group that in the body of a patient is replaced by hydrogen.

Abstract: The present invention relates to a production method of (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid which comprises optical resolution of racemic 3-hydroxy-3-(2-phenylethyl)hexanoic acid with an optically active amine of the formula (VIII) wherein R2 is 3,4-dimethoxyphenyl or 2-chlorophenyl. According to the present invention, (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid useful as a starting material of a pharmaceutical agent can be efficiently produced with a high optical purity and a relatively high total yield.

Abstract: A synthetic reaction to produce [2-(2-aminoethoxy)ethoxy] acetic acid (AEEA) derivatives. This synthetic reaction does not require isolation and purification of intermediates. The AEEA derivatives can be used to synthesize high load polystyrene-polyethylene glycol-like resins having excellent swelling characteristics.

Abstract: Compounds having the formula are useful for treating conditions which arise from or are exacerbated by angiogenesis. Also disclosed are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

Abstract: A novel antibiotic thiobutacin, obtainable from Lechevalieria aerocolonigenes strain VK-A9, and antifungal and antioomycete compositions comprising thiobutacin as an active ingredient for control of plant diseases, e.g., those attributable to pathogens such as Phytophthora capsici and Botrytis cinerea.

Abstract: The present invention relates to a process for the highly regioselective aromatic nitration of alkyl 4-alkanoylamino-3-alkyl-benzoates in the 5-position in a mixture containing nitric acid and the use of the resulting products for preparing, in particular, pharmaceutically active benzimidazole derivatives.

Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac arrhythmias, thyrotoxicosis and subclinical hyperthyrodism.

Abstract: (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid is crystallized as an anhydrous, stoichiometric 1.5 HCl salt and a scaleable crystallization method is disclosed. The salt form was characterized and the absolute configuration of the chiral center was confirmed as “S”. (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid was high melting and appears acceptably non-hygroscopic for use in a pharmaceutical composition.

Abstract: Novel compounds of formula (I) are described wherein: R1=(CH2)mCH3 where m is 0 or an integer in the range from 1 to 16, or an alkenyl, alkynyl, alkoxy, alkylthio, or alkyl sulfinyl group having from 2 to 17 carbon atoms; R2=H, CH3 or CH2CH3; R3=H or CH3; R4H or CH3; R5=lower alkyl having from 1 to 5 carbon atoms; n is an integer in the range from 1 to 3, and X is carboxyl (COOH) or carbalkoxy (COOR5), cyano (C?N), phosphonic acid (PO3H2), phosphonate ester (PO3[R5]2) or 5-tetrazole, and pharmaceutically acceptable salts thereof. Preferably, the compounds are optically pure enantiomers of the R— or S—configuration in which R3=R4=R5=H, R2=CH3 and R1 is a saturated aliphatic chain of one to five carbon atoms.

Abstract: The invention provides a process for producing a fluorine-containing compound from an inexpensive material. Namely, Compound I such as RACH2OH is reacted with Compound II such as XCORB to form Compound III such as RACH2OCORB, followed by fluorination in a liquid phase to form Compound IV such as RAFCF2OCORBF, which is converted to Compound V such as RAFCOF and/or Compound VI such as RBFCOF. RA is an alkyl group or the like, RB is a perhalogenoalkyl group or the like, RAF and RBF are fluorinated RA and RB, and X is halogen.

Abstract: Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.

Abstract: Compounds of the general formula (I) wherein R1 represents halogen, R2 represent H or halogen, and R3 represents C3-8-cycloalkyl, C3-8-cycloalkenyl, or optionally substituted phenyl, pharmaceutical compositions containing such material, and methods of using such materials in the treatment of various diseases are disclosed and claimed.

Abstract: The invention relates to compounds of the general formula (I) wherein R1 represents H, halogen, or OCF3; R2 and R3 each represents H or halogen; R4 represents C1-6-alkyl, C3-8-cycloalkyl, CF3, OCF3, F, Cl, OMe, or optionally substituted phenyl; V represents O, CH2O, OCF2, or O—C1-6-alkyl-O; and W represents CH2 or CH2CH2. A process for making such compounds, pharmaceutical compositions containing them, and methods of treatment of various conditions using them are also disclosed and claimed.

Abstract: A process for producing a hydrogenated ester by hydrogenating an unsaturated group-containing ester having a specific structure by using a hydrogenating catalyst so as to obtain a hydrogenated ester with a high selectivity. It is preferred that the unsaturated group-containing ester as the raw material is diluted with an inert solvent and/or the concentration of carboxylic acid contained in the raw material is made 1 wt. % or less so as to effect a hydrogenation reaction. The hydrogenating catalyst to be used for the above hydrogenation may preferably be one comprising at least one metal selected from Group 8 elements, Group 9 elements, and Group 10 elements in the periodic table according to Nomenclature of Inorganic Chemistry, Revised Edition, 1989, International Union of Pure and Applied Chemistry, and preferably has an acidity of 1.0×10?1 mmol/g or less.

Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds having the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): and Ar2, X1, R1, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined in the specification.

Abstract: The compound O-(2-[18F]fluoroethyl)-L-tyrosine has proven to be particularly suitable for positron emission tomography and has already been tested in clinical practice. Until now, the compound has been prepared according to a relatively laborious method (Wester H. J. et al., J. Nucl. Med. 1999; 40: 205-212). The invention relates to L-tyrosine derivatives of the formula (1) whereby R1 represents a suitable protective group for the carboxy group, R2 a suitable protective group for the amino group and R3 a suitable leaving group, R1 represents a methylthiomethyl group, a tetrahydrofuranyl group, a diphenylmethyl group, a para-methoxybenzyl group, a piperonyl group or a tert-butyl group, R2 an alkyl- or an arylalkyl group and R3 a p-tosyloxy, methanesulfonyloxy, trifluoromethanesulfonyloxy or bromine. The invention also relates to a method for preparing O-(2-[18F]-fluoroethyl)-L-tyrosine from the initial compounds of formula (1) and method for the preparation of these initial compounds.