Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo [1,2-&agr;]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.

Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-a]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.

Abstract: Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-&agr;]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.

Abstract: The invention relates to new compounds of general formula I or the pharmaceutically acceptable salts thereof, wherein X=N-R3 or CH-R4, Y=CH2 or (CH2)2, Z=O or H2; and R1, R2, R3, R4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: The present invention relates to new pharmaceutical formulations for aerosols with at least two or more active substances for administration by inhalation or by nasal route. Specifically, the invention relates to pharmaceutical preparations for propellant-driven metered dose aerosols using a fluorohydrocarbon (HFC) as propellant, which contain a combination of active substance of two or more active substances, wherein at least one active substance is present in dissolved form together with at least one other active substance in the form of suspended particles.

Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl o

Abstract: Provided are compounds of the general formula I: wherein R2 is selected from the group consisting of H, F, Cl, (C1-4) alkyl, (C3-4) cycloalkyl and CF3; R4 is H or Me; R5 is H, Me or Et, with the proviso that R4 and R5 are not both Me, and if R4 is Me then R5 cannot be Et; R11 is Et, cyclopropyl, propyl, isopropyl, or isobutyl; and Q is selected from the group consisting of: and pharmaceutically acceptable salts thereof, as inhibitors of HIV reverse transcriptase, wild-type and several mutant strains.

Abstract: Pharmaceutical preparations for producing powder aerosols using propellant gases which use TG 227, and possibly also TG 11, TG 12, TGH 114, propane, butane, pentane or DME.

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.

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 invention relates to the use of tricyclic nitrogen heterocycles of general formula I as pharmaceutical compositions with an inhibitory effect on PDE IV, wherein the groups R1, R2 and R3 have the meanings given in the specification and claims.

Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl- 1-H-imidazo[ 1 ,2-a]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment of prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.

Abstract: New advantageous propellent gas mixtures contain two or more components, at least one of which is a partially fluorinated lower alkane, and may be used in pharmaceutical preparations.

Abstract: Novel compounds of the formula I: which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-1,3-dihydroindol-2-one; 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydro-indol-2-one; 3-benzyl-1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydroindol-2-one; 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-4-hydroxy-3-methyl-1,3-dihydroindol-2-one; and, 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-5-fluoro-1,3-dihydroindol-2-one.

Abstract: Bezimidazole derivatives of general formula (I) having tryptase-inhibitory activity. Exemplary are: N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5-yl}-N-diethylaminoethyl-(4-ethoxycarbonyl-benzenesulphonamide)-hydrochloride, N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5-yl}-N-diethylaminoethyl-(dansylamide)-dihydrochloride, and N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5-yl}-N-diethylaminoethyl-(3-bromo-benzenesulphonamide)-hydrochloride.

Abstract: The invention relates to polymorphs of 4′-[2-n-propyl-4-methyl-6-(l-methylbenzimid azol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: telmisartan), particularly polymorphic form B, mixtures of the polymorphs, processes for preparing telmisartan containing form B and the use thereof for preparing a pharmaceutical composition.

Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl o

Abstract: Disclosed is a process of making substituted pyrazoles from substituted benzophenone hydrazones with a variety of 1,3-bifunctional substrates under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds.

Abstract: The invention relates to carboxamide-substituted benzimidazole derivatives of general formula (I) wherein the groups R1, R2, R3 and R4 may have the meanings given in the claims and in the specification, processes for preparing them and the use of carboxamide-substituted benzimidazole derivatives as pharmaceutical compositions, particularly as pharmaceutical compositions with a tryptase-inhibiting effect.