Abstract: The invention relates to new 2-heterocyclically substituted dihydropyrimidines, medicaments which contain these 2-heterocyclically substituted dihydropyrimidines, and a process for preparation of medicaments. The invention furthermore relates to the use of the 2-heterocyclically substituted dihydropyrimidines for the production of a medicament, in particular for the treatment of acute or chronic viral diseases, in particular for the production of a medicament for the treatment of acute or chronic hepatitis B infections.

Abstract: Disclosed is an improved process for the continuous production of aromatic carboxylic acids by the liquid-phase oxidation of an alkyl aromatic compound with an oxygen-containing gas in the presence of oxidation catalyst which results in reduced wastewater generation, reduced condensing capacity requirements, and, optionally, increased power recovery, and. The process effectively utilizes the heat of reaction in the process of removing excess water generated from the reaction and minimizes the loss of solvent used as the carrier for the reaction catalyst by removing reactor off-gas directly into a water removal column for distillation. A portion of the overhead aqueous vapors are removed from the top of the water removal column as a vapor distillate, with the remaining overhead aqueous vapors being condensed then subsequently refluxed to the fractionating zone of the water removal column.

Abstract: The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R21, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)—Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (VIII) of the formula HNR3—Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H.

Abstract: A compound of the formula wherein the substituents are as defined in the specification and solvates and salts thereof useful for treating bone and cartilage diseases.

Abstract: The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; —A—B— represents —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 is a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also be hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(&bo

Abstract: Compounds of formula I in which R1 represents a substituted or unsubstituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, phenylamino or phenylmethyl residue, and R2 represents an optionally substituted aryl or heteroaryl residue, with metallo-proteinase inhibitor activity.

Abstract: The invention relates to novel substituted cyanophenyluracils of the general formula (I) in which R1, R2, R3, R4, R5 and Q are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides and insecticides.

Abstract: The thienopyrimidines of the formula (I) and their physiologically compatible salts display a phosphodiesterase V inhibiting activity and can be used for treating diseases of the cardiovascular system and for treatment and/or therapy of erectile dysfunction.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.

Abstract: An aqueous potassium sorbate solution has a dissolved oxygen concentration of not more than 3.0 mg/l. The aqueous potassium sorbate solution can be obtained (i) by degassing an aqueous potassium sorbate solution to thereby control the dissolved oxygen concentration to 3.0 mg/l or less, or (ii) by performing a reaction in a system, in which the oxygen concentrations of the gas phase and of materials to be reacted are reduced, in the production of an aqueous potassium sorbate solution by a reaction of sorbic acid and potassium hydroxide in the presence of water. The resulting aqueous potassium sorbate solution exhibits successively stable hue.

Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract: Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract: The present invention can be used in medical practice specifically in chemical and pharmaceutical production of medicinal agents capable of modulating the immune system. This invention essentially relates to a new medicinal preparation 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt having immunomodulatory, antiinflammatory, and antioxidant properties. The preparation is obtained from 3-nitro-phthalanhydride by consecutive isolation of intermediate and end products. The intermediate products include 5-nitro-2,3-dihydrophthalazine-1,4-dione and 5-amino-2,3-dihydrophthala2ine-1,4-dione. The reaction between 5-amino-2,3-dihydrophthalazine-1,4-dione and sodium hydroxide yields the target product, 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. The method allows to produce the medicinal preparation with high pharmaceutical activity. It is provided an example of application of this preparation.

Abstract: 2,3-Benzodiazepines of formula (I), their stereoisomers and acid addition salts, wherein the variables have the meaning given in the specification, and pharmaceutical compositions containing them which are suitable for treating conditions associated with muscle spasms, epilepsy as well as acute and chronic forms of neurodegenerative diseases are disclosed.

Abstract: Thieno[2,3-d]pyrimidine compounds of general formula (1) useful as drugs having a cGMP-specific phosphodiesterase inhibiting effect and the preparation thereof wherein Q is formula: (CH2)n—N(r1)—C(r2) (r3), CH═CH—CH═CH, or (CH2)m which is bonded to a and b; R1 is hydrogen or C1-C6 alkyl; R2 is C3-C8 cycloalkyl optionally substituted with G1, phenyl optionally substituted with G2, or a saturated or unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, O and S and being optionally substituted with G3; and R3 is a saturated or unsaturated heretocyclic group having 1 to 4 heteroatoms selected from N, O and S and being optionally substituted with G3 or (CH2)kC(═O)R4 or CH═CHC(O)R4.

Abstract: Two series of 6,7,2′,3′,4′,5′-substituted 2-phenyl-4-quinazolinones and 6,2′,3′,4′,5′-substituted 2,3-dihydro-2-phenyl-4-quinazolinones are synthesized and evaluated for cytotoxicity against a panel of human tumor cell lines, such as epidermoid carcinoma of the nasopharynx (KB), lung carcinoma (A-549), ileocecal carcinoma (HCT-8), breast cancer (MCF-7), melanoma (SKMEL-2), ovarian cancer (1A9), glioblastoma (U-87-MG), bone (HOS), P-gp-expressing epidermoid carcinoma of the nasopharynx (KB-VIN), and prostate cancer (PC3) cell lines, and some of the compounds are found potent. The present invention also synthesizes 2-phenyl-4-alkoxy-quinazoline compounds, wherein some of the compounds exhibit antiplatelet activity.

Abstract: This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1-6 carbon atoms; R′ is hydrogen, alkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, trifluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, trifluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least one of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorde

Abstract: Sodium salt of 3-(4-cinnamyl-1-piperazinyl)-iminomethyl rifamycin SV was synthesized. The compound shows high activity against Gram-positive and Gram-negative microorganims, Mycobacterium tuberculosis (including atypical and rifampicin resistant) and may be used in the medical practice. The sodium salt has formula (II). The process for preparation of the sodium salt consists of reacting equimolar quantities of 3-(4-cinnamyl-1-piperazinyl)-iminomethyl rifamycin SV and sodium ascorbate with addition of 30% methanol solution of sodium methylate, followed by filtration and removement of the solvent by distillation under reduced pressure. The compound can also be obtained from the sodium salt of 3-formil rifamycin SV, which is reacting with N1-amino-N4-cinnamypiperazin in medium of inert solvent at room temperature.

Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.

Abstract: An improved method for preparing N-[3(3-cyanopyrazole[1,5-a]pyrimidine-7-yl)phenyl]-N-ethyl-acetamide having the FORMULA I: in which the product in question is obtained in “a single step” starting with N-[3-[3-(dimethylamine)-1-oxo-2-propenyl]phenyl]acetamide (II) according to the following sequence: In a first stage N-[3-[3-(dimethylamine)-oxo-2-propenyl]phenyl]acetamide (II) is added in portions to a suspension of sodium hydride in dimethylformamide in the presence of ethyl iodide. The resulting suspension of compound (III) (N-[3-[3-(dimethylamine)-1-oxo-2-propenyl]phenyl]-N-ethyl-acetamide) is diluted with water until solution A is obtained which is used as it is. Subsequently, solution A is added to solution B of 3-amino-pyrazole-4-carbonitrile IV) in aqueous DMF/hydrochloric acid.