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 present invention relates to acylguanidine derivatives of formula (I) in which R1, R2, R4, R5, R6, A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extend of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.

Abstract: A process for the preparation of alkylene diamine triacetic acid (derivatives) which comprises the conversion of an alkylene diamine (derivative) to a metal salt of an alkylene diamine triacetic acid (derivative). The reaction is carried out in the presence of a polyvalent metal ion Ma+ and the entire reaction is carried out under hydrolyzing conditions if any of the reactants contain or form nitrile or amide groups.

Abstract: Compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases.

Abstract: Novel triazolo derivatives represented by the following formula and pharmaceutically acceptable salts thereof, as well as chemokine inhibitors containing the same as an effective component. These are useful as therapeutic agents for allergic diseases such as bronchial asthma and atopic dermatitis; therapeutic agents for inflammatory diseases such as chronic rheumatoid arthritis; therapeutic agents for autoimmune diseases such as ulcerative colitis and nephritis; and as anti-AIDS drugs.

Abstract: The current invention relates to compounds of Formula I pharmaceutical compositions and methods of use as nitric oxide synthase inhibitors, wherein the substituents are defined in the application.

Abstract: The invention relates to novel inhibitors of human tryptase which are used in the pharmaceutical industry for the production of medicaments.

Abstract: The 6-(spirocyclopropyl)-penicillanic acid 4,4-dioxides of the general Formula (I): as defined herein above which exhibit beta-lactamase inhibiting activity, use of such compounds in combination with beta-lactam antibiotics for inhibiting beta-lactamases, pharmaceutical compositions and processes for preparing such compounds.

Abstract: The invention concerns a method for recuperating and purifying a lactic acid solution obtained initially from a fermentation medium or any other source, consisting in a pre-treatment to eliminate the ion loads capable of catalysing the lactic acid condensation and based on the principle of ion exchange or any other related principle, followed by at least a step of concentration at low temperature and brief retention time and at least a step of distilling the lactic acid using a thin layer process.

Abstract: The present invention relates to novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 inhibitors.

Abstract: The invention relates to novel N-(substituted phenyl)-N′-[&ohgr;-(5-substituted-7-oxo-7H-thieno[3,2-b]pyran-3-carbonylamino)alkyl]piperazines their N-oxides and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neutogenic lower urinary tract dysfunction (NLUTD), and other conditions. The compounds may be administered alone or in combination with an anticholinergic compound.

Abstract: A compound of formula (I), or a pharmaceutically-acceptable salt thereof, wherein A is an optionally substituted 5- or 6-membered monocyclic aromatic ring containing 1, 2 or 3 ring heteroatoms; B is optionally substituted phenylene or a 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen heteroatoms; R and R1 are hydrogen or (1-4C)alkyl; n is 1 or 2; R2 and R3 are hydrogen, (1-6C)alkyl, (4-7C)cycloalkyl, or (2-6C)alkenyl, or R2 and R3 may form along with the nitrogen to which they are attached a 5-, 6- or 7-membered heterocyclic ring, wherein each R2 or R3 group or any heterocyclic ring formed from R2 and R3 may be optionally substituted with various substituent groups, and wherein Q may be optionally substituted by various substituent groups, which posseses antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals.

Abstract: The present invention relates to novel 3-heteroarylidene-2-indolinone compounds and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

Abstract: The present invention involves a process for preparing a stable final formulation product of a compound of formula I, or its pharmaceutically acceptable salt, hydrate or solvate by incorporating a suitable carbon dioxide source to an unstable monosodium adduct of carbapenem antibiotic compound.

Abstract: The present invention is based on a series of acrylic cross-linking agents containing two or more dehydroalanine moieties (H2C═C(NHCOR′)COOR) per monomer. Monomers of the general structure H2C═C(NHCOCH3)COO(CH2)iOO(CH3CONH) C═CH2 with i=4, 5, and 8 can be polymerized or copolymerized under UV-curing conditions or by simple heating above melting point, leading to cross-linked polymeric materials. When polymerized on metallic surfaces, exceptional adhesion is obtained with no need for additional adhesion enhancers.

Abstract: Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, and also possible physiologically tolerated salts, in which the variables have the meanings indicated in the description.

Abstract: This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached may

Abstract: Substituted (4-bromopyrazol-3-yl)benzazoles I and their salts where R1=H, C1-C4-alkyl, C1-C4-haloalkyl; R2=CN, Cl-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-haloalkylthio, C1-C4-alkylsulfinyl, C1-C4-haloalkylsulfinyl, C1-C4-alkylsulfonyl, C1-C4-haloalkylsulfonyl; R4=H, halogen; R5=H, CN, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; Z=—N═C(XR6)—O— or —N═C(XR6)—S—, attached to &agr; via the nitrogen, oxygen or sulfur; X=a chemical bond, oxygen, sulfur, —S(O)—, —SO2—, —NH— or —N(R7)—; R6, R7=Cl-C6-alkyl, Cl-C6-haloalkyl, cyano-Cl-C4-alkyl, hydroxy-C1-C4-alkyl, C3-C6-alkenyl, cyano-C3-C6-alkenyl, C3-C6-haloalkenyl, C3-C6-alkynyl, cyano-C3-C6-alkynyl, C3-C6-haloalkynyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-haloalkoxy-C1-C4-alkyl, C3-C4-alkenyloxy-C1-C4-alkyl, C3-C4-alkynyloxy-C1-C4-alkyl,

Abstract: The present invention provides novel compounds exemplified by pyrrolic nitrogens used as anion and neutral species recognition elements with an aromatic core as a signal group. Described are methods for the synthesis of various pyrrole aryl compounds as well as various applications for these compounds. Methods of use include the binding and detection of specific analytes in a mixture and, in some examples, the separation of the analyte from the mixture. Additional methods of use include the transport of therapeutic agents and the sensing of components, degradants, and impurities in foodstuffs.

Abstract: The present invention relates to a plurality of novel processes and novel intermediates for preparing 3-(1-hydroxyphenyl-1-alkoximinomethyl)dioxazines, which are known as intermediates for preparing compounds having fungicidal properties (WO 95-04728).