Abstract: The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-pyrrole derivatives of formula (I) 1

Abstract: The invention relates to novel tetrahydroisoquinoline derivatives of general formula I and theirs use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and their use as anti-infectives, wherein R1, R2 and R3 are as defined in claim 1.

Abstract: Compounds of formula I are provided 1

Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The present invention aims to identify the molecule involved in mechanical allodynia, and to develop and provide a pharmaceutical composition to target this molecule such that the composition is effective in the treatment of mechanical allodynia. The present invention also aims to provide a screening method for compounds for use in such pharmaceutical compositions, a method of determining mechanical allodynia, and a treatment method of mechanical allodynia.

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.

Abstract: Provided herein are methods of using compounds of formula (IA-IF) that are aryl- and heteroaryl-substituted tetrahydroisoquinolines, for the treatment of chronic and neuropathic pain, the treatment and prevention of migraine headache, and the treatment of stress, urge and mixed urinary incontinence.

Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract: Provided herein are methods of using compounds of formula (1) that are aryl- and heteroaryl-substituted tetrahydroisoquinolines, for the treatment of chronic and neuropathic pain, the treatment and prevention of migraine headache, and the treatment of stress, urge and mixed urinary incontinence.

Abstract: The invention treats proteinase-related disorders by interfering with the binding of the metal needed by matrix metalloproteinases, such as PLA-2. The compounds used are known microbial-based chelators of known high solubility. For example, dipicolinic acid has a high affinity to calcium and is soluble in both water and glycerin, as might be expected due to its role in the formation of bacterial endospores. Thus, unlike most chelation agents, the compounds are intended to be permeable enough to cross a vertebrate's cell membrane, a prerequisite for meaningful inhibition of protein-regulated cellular functions such as the inflammatory cascade and accompanying formation of free fatty acids.

Abstract: The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists.

Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I 1

Abstract: Aminoisoquinoline derivatives of the following formulae or analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an excellent effect of inhibiting activated blood-coagulation factor X, and they are useful as anticoagulants or agents for preventing or treating thrombi or emboli.

Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.

Abstract: The present invention relates to an agent for the treatment and/or prevention of allergy which comprises, as an active ingredient, an inducible nitrogen monoxide synthase inhibitor, preferably a condensed piperidine compound represented by formula (I), or an acid addition salt thereof or a hydrate thereof: 1

Abstract: The invention provides a method for improving attentive cognition comprising administering a compound that potentiates intraneuronal carbonic anhydrase activity thereby improving establishment of a theta rhythm.

Abstract: The invention encompasses a series of tetrahydroisoquinolines of formula I which are antagonists of the human melatonin MT2 receptor and are useful as chronobiotic and sleep agents.

Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I 1

Abstract: The invention relates to compounds of formula (1) 1

Abstract: Disclosed are isoquinolino derivatives of the formula wherein Y is >C═O or —CH2—, Z is >C═O or —CH2—, and R1, R2 and m are as defined herein as well as the pharmaceutically acceptable salts thereof. These compounds are MAO-B selective inhibitors useful, inter alia, in the treatment of Alzheimer's disease and/or senile dementia.

Abstract: Disclosed is an inhibitor of CCR8 that is represented by Structural Formula (I): 1

Abstract: Active compound combinations, which have a light protection action, of 4,4′,4″-(1,3,5-triazine-2,4,6-triyltriimino)-trisbenzoic acid tris(2-ethylhexyl ester) and one or more emulsifiers chosen from the group of substances of the general structural formula wherein R1, R2 and R3 independently of one another are chosen from the group which comprises: H and branched and unbranched, saturated and unsaturated fatty acid radicals having 8 to 24 carbon atoms, in which up to three aliphatic hydrogen atoms can be replaced by hydroxyl groups, and n is a number from 2 to 8.

Abstract: The novel heterocyclic compound of the present invention is a novel heterocyclic compound having the formula (I) 1

Abstract: This invention relates to substituted isoquinoline derivatives and their use as anticonvulsants.

Abstract: The invention relatests compound of formula (I): 1

Abstract: Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K+ channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca++ activated K+ channel (IKCa1) prevents the pre-Ca++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.

Abstract: The present invention provides a novel nitrogen-containing heterocyclic compound useful as a phosphodiesterase-4 inhibitor, and a medicament comprising the same. Further, the present invention provides a nitrogen-containing heterocyclic compound represented by the following formula, its salt or hydrates thereof, and a medicament comprising the same.

Abstract: Methods and materials for preparing quinapril, its pharmaceutically acceptable salts, including quinapril hydrochloride, are disclosed. The method includes reacting (2S,4S)-2-(4-methyl-2,5-dioxo-oxazolidin-3-yl)-4-phenyl-butyric acid ethyl ester with (3S)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid tert-butyl ester to yield quinapril tert-butyl ester, which is subsequently reacted with an acid to yield quinapril or an acid addition salt of quinapril.

Abstract: The present invention provides a method of treating or preventing migraine comprising administering to a patient in need thereof an effective amount of a selective iGluR5 receptor antagonist. The present invention further provides novel compounds functional as selective iGluR5 receptor antagonists as well as compositions and formulations comprising said selective iGluR5 receptor antagonists.

Abstract: PDF inhibitors and novel methods for their use are provided.

Abstract: This invention relates to compounds useful for treating or preventing obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease, prostatic disease, and the like, and to pharmaceutical composition, methods, and kits comprising such compounds.

Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.

Abstract: The novel heterocyclic derivative of the present invention is a novel heterocyclic derivative having the formula (I′) 1

Abstract: The invention provides compounds of the formula: 1

Abstract: Condensed pyridine compounds represented by formula (I): wherein: R1 and R3 are, independently, hydrogen, halogen, lower alkyl, or lower alkoxy; R2 represents an amino substituent; ring A is a benzene ring, pyridine ring, thiophene ring, or furan ring; and B represents a substituent containing a ring structure. Also, pharmaceutically acceptable salt and hydrates thereof. These compounds are clinically useful medicaments having; serotonin antagonism, and in particular, for treating, ameliorating, or preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.

Abstract: The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: This invention is directed to the compound of formula (I) which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as in inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.

Abstract: The present invention is directed to multifluoro-substituted Chalcones and analogs thereof, represented by the general Formula I: 1

Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.

Abstract: Compounds of formula (I): and medicinal products containing the same which are useful as dual &agr;2/5-HT2c antagonists.

Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

Abstract: The invention is directed to methods of bone healing by administering a p38 MAP kinase inhibitor. The invention is directed to methods of treating bone fractures, bone diseases, bone grafting, especially enhancing bone healing following facial reconstruction, maxillary reconstruction, mandibular reconstruction or tooth extraction, enhancing long bone extension, enhancing prosthetic ingrowth, and increasing bone synostosis by administering a p38 MAP kinase inhibitor.

Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: Compounds according to the formula A-Z-W as herein described, wherein A is selected from the groups consisting of: A′-(CH2)n—, A′-(CH2)nSO2—, and A′-(CH2)nCO—, where n is 0 to 4; and A═ is selected from

Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to naphthol, quinoline and isoquinoline-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.

Abstract: The present invention relates to compounds of the formula (I) wherein X1 is wherein R1, R2 and R10 are independently hydrogen or a suitable substituent; R11 and R12 are independently hydrogen or a suitable substituent; R is unsaturated 5 to 6-membered heteromonocyclic group; A is direct bond or —NH—; X2 is monocyclic arylene, unsaturated 5 to 6-membered heteromonocyclic group or cycloalkenylene; Y is bivalent group selected from ethylene, trimethylene and vinylene, wherein CH2 is optionally replaced by NH or O, and CH is optionally replaced by N; and Z is —(CH2)n—, —CO—(CH2)m—, —CH═CH— or —CO—NH—, wherein n is 1, 2 or 3 and m is 1 or 2, or a salt thereof. The compounds of the present invention inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.

Abstract: The present invention provides methods and kits for treating osteoarthritis using an estrogen agonist/antagonist.

Abstract: Compounds of formula (I) 1