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: Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein.

Abstract: Crystalline monohydrate of (1?,2?,4?,5?,7?)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.

Abstract: The invention relates to a new process for producing powdered preparations for inhalation wherein a substance having a smaller particle size distribution is metered continuously through a suitable feed device onto a moving bed of a powdered substance having a larger particle size distribution.

Abstract: Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

Abstract: The present invention relates to the preparation of universal inactivated vaccines and their use in preparing compositions for the prophylaxis and therapy of dermatomycosis. Vaccines according to the present invention have the advantage of conferring immunity against all important causes of dermatomycosis in animals and are characterized by stable immunogenic properties, easy preparation, high content of microconidia and lack of side reactions in animals.

Abstract: The invention relates in its first aspect to a rapidly decomposing tablet for pain therapy containing meloxicam [4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide] in the form of a salt with an inorganic or organic base providing rapid absorption of the active substance, the process of its preparation by direct tabletting, and furthermore relates in a second aspect to the crystalline meloxicam meglumin salt mono- and dihydrate and the preparation thereof.

Abstract: The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) wherein: R1 denotes a group selected from among methyl, ethyl, propyl, cyclopentyl, cyclohexyl, phenyl, benzyl and —C(Me2)phenyl, each of which is optionally mono-, di- or trisubstituted by hydroxy; and, R2 denotes a group selected from among methyl, ethyl, propyl and benzyl.

Abstract: The present invention relates to indolinones substituted in the 6-position of general formula wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: The present invention relates to the use of ?1L-agonists for treating urinary incontinence.

Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, Y, and n are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.

Abstract: A compound of formula 1 wherein: A is a group selected from X? is an anion with a single negative charge; R1 and R2 are each independently a C1-C4-alkyl optionally substituted with hydroxy or halogen; and R3, R4, R5, R6, R7, and R8 are each independently hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, CF3, CN, NO2, or halogen, with the proviso that at least one of the groups R3, R4, R5, R6, R7, and R8 is not hydrogen, processes for preparing these compounds, pharmaceutical compositions containing these compounds, and their use as pharmaceutical compositions.

Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.

Abstract: The present invention relates generally to a method for identifying molecules that bind the R7.1 epitope of LFA-1 or bind LFA-1 such that the R7.1 epitope is modified. The present invention further relates to a method for determining occupancy of the LFA-1 receptor by molecules that bind to the R7.1 epitope or bind LFA-1 such that the R7.1 epitope is modified after administration to a subject. The present invention further relates to molecules useful in the methods of the invention.

Abstract: Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.

Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein R1 is selected from: H, haloalkyl, (C1-6)alkyl, (C2-6)alkenyl, (C3-7)cycloalkyl, (C2-6)alkynyl, (C5-7)cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C6-10)bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR5, wherein R5 is H, halogen, haloalkyl, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; X is N or CR5; D is N or CR5; each of Y1 and Y2 is independently O or S; Z is O, N, or NRZ wherein RZ is H, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; R3 and R4 are each independently H, (C1-6)alkyl, first (C3-7)cycloalkyl or 6- or 10-membered aryl, Het (C1-6)alkyl-6- or 10-membered aryl, (C1-6)alkyl-Het; or each R3 and R4 are independently covalently bonded together to form second (C3-7)cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R3 or R4

Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.

Abstract: Carboxylic acid amides of general formula having an antithrombotic activity and a factor Xa-inhibiting activity. Exemplary are: (a) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-4-(2,5-dihydro-pyrrol-1-yl-carbonyl)-3-methyl-benzamide, (b) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, (c) N-[1-(5-amidino-2-hydroxy-phenyl)-2-phenyl-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, and (d) N-[1-(5-amidino-2-hydroxy-phenyl)-2-(pyridin-3-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide.