Abstract: The invention relates to compounds of general formula (I), a method for the production thereof and the use thereof as pharmacologically effective substances for a broad medical indication spectrum. Furthermore, selective adenosine receptor ligands, preferably selective adenosine A1-, adenosine A2a- and/or adenosine A2b-receptor ligands are provided for the prophylaxis and/or the treatment of diseases, especially cardiovascular diseases, diseases of the urogenital region, diseases of the respiratory tract, inflammatory and neuroinflammatory diseases, diabetes, especially pancreatic diabetes, neurodegenerative diseases, pain states, cancer as well as liver fibrosis and liver cirrhosis.

Abstract: The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, Rc, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract: Monoclinic 2-chloro-N-(4?-chlorobiphenyl-2-yl)nicotinamide melting at 147-148° C. and of the formula I and a process for the preparation thereof.

Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I) or (II), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction.

Abstract: The present invention relates to phosphinic acid derivatives as GABAB antagonists, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.

Abstract: Disclosed are processes for the synthesis and purification of prostaglandins and analogues thereof, especially analogues of PGF2?.

Abstract: Indenoisoquinolines and dihydroindenoisoquinolines are described. In particular, such compounds possessing one or more electron withdrawing substituents are described. The in vitro anticancer activities of these molecules tested in the National Cancer Institute's screen of 55 cell lines is described. The compounds tested for topoisomerase I (top1) inhibition is described.

Abstract: The present invention provides an anti-coronavirus agent including as an active ingredient as exemplified by nelfinavir and salts thereof, an anti-SARS agent including the anti-coronavirus agent, and a method of treating SARS using the anti-SARS agent.

Abstract: The present invention provides certain substituted 1,4-dihydropyridine compounds, including pure enantiomeric forms and pharmaceutical formulations thereof. These compounds provide for elevation of ?-MyHC protein levels and ?-MyHC mRNA levels, and most frequently these same compounds provide simultaneous lowering of ?-MyHC protein levels and ?-MyHC mRNA levels. Thus, these compounds may be used alone or in conjunction with other drugs to treat heart failure.

Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.

Abstract: A novel crystalline form of quinapril hydrochloride of formula (I) An amorphous form of quinapril hydrochloride substantially free of impurities, specially diketopiperazine compound, and conforming to pharmacopoeial specifications formed from the said novel crystalline form of quinapril hydrochloride of formula (I). The crystalline quinapril hydrochloride is in the form nitroalkane solvate in which the nitroalkane is nitromethane, nitroethane and nitropropanae. Each such nitroalkane solvate having particular characteristic X-ray diffraction patterns. A process for preparation of amorphous form of quinapril hydrochloride, substantially free of impurities, specially diketopiperazine compound, and conforming to pharmacopoeial specifications, using the novel crystalline quinapril hydrochloride as an intermediate. The process involves obtaining free base compound of formula (V) by adjusting the pH of a solution of the benzyl ester maleate salt of quinapril of formula (V) between 7.5-8.

Abstract: The present disclosure provides compositions for inhibiting proteases, methods for synthesizing the compositions, and methods of using the disclosed protease inhibitors. Aspects of the disclosure include a peptidyl propenoyl hydrazide compositions that inhibit proteases, for example cysteine proteases, either in vivo or in vitro.

Abstract: The present invention relates to glycinamide derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.

Abstract: Compounds which bind to opioid receptors are provided. In a preferred embodiment of the invention, the compounds are opioid receptor antagonists. The present invention also provides methods of treating conditions which are mediated by an opioid receptor.

Abstract: A process for forming a facial tris-cyclometallated iridium or rhodium complex isomer comprises heating an original solid composition containing meridional isomer of the metal complex at a temperature and for a time sufficient to form a product containing the facial isomer in an increased ratio to meridional isomer compared to the original composition.

Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, i and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.

Abstract: The invention is directed to compounds having the following Formula I: and methods of using them for the treatment of proliferative diseases.

Abstract: The invention relates to novel processes for the preparation of high-purity roflumilast.

Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIV”) integrase enzyme.

Abstract: It is intended to provide novel labeling reagents characterized by having a group capable of binding to a substance to be labeled (for example, a biological substance, a physiologically active substance, etc.), easily forming a complex together with a rare earth ion, the complex being stable in an aqueous solution, and having a sufficient fluorescence intensity and a long fluorescence life time regardless of buffer types; complexes composed of the above labeling reagent with a rare earth ion; fluorescence labels containing the above complex; a fluorescence assay method using the above fluorescent label; etc. Namely, labeling reagents comprising a compound having a 2,2?:6?,2?-tripyridine skeleton or a 2,6-dipyrazolopyridine skeleton and having a group capable of binding to a substance to be labeled (for example, a biological substance, a physiologically active substance, etc.