Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.

Abstract: The invention relates to a novel process for preparing enantiomerically enriched or pure tetrahydroquinoline derivatives by reacting a chiral dihydropyran-methylamine C with a aldehyde B and an aniline A in a multicomponent one pot synthesis in the presence of a protonic acid or Lewis acid with a suitable solvent. A, B, C have the meaning as described in the specification.

Abstract: The present invention relates to compounds of formula (I) wherein c, X, Y, R2, R3, R4 and R6 are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection.

Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.

Abstract: The present invention provides Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and discloses methods for the treatment of inflammatory and immune disorders comprising administering to a patient in need thereof an effective amount of Compound (I) or a pharmaceutically acceptable salt thereof.

Abstract: An improved chemical synthesis for compounds having useful biological activity is disclosed, where the use of TMEDA or N,N,N?,N?-tetramethyl-ethane-1,2-diamine gives improved yield.

Abstract: [Problems] To provide a compound which is useful as an NMDA receptor antagonist. [Means for Solution] The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.

Abstract: The invention provides compounds having the formula: wherein R1 is halogen. The invention also provides compositions comprising the compounds, and methods of treating diseases or disorders that comprise administering one or more of the compounds to a subject in need thereof. The disclosed compounds have CCR1 antagonist activity.

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.

Abstract: Compounds having the formula A-R wherein A is a hetereoaryl and R is Ia, Ib or Ic and wherein A, R, R1, R2a, R2b, R2c, R3a, R3b, R4, R5, R6, Ra, Rb, Rc, Rd, X, X1, X2 and n are as are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.

Abstract: Provided are non-steroidal tricyclic compounds that are modulators of androgen receptors and methods for making and using such compounds.

Abstract: The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction.

Abstract: A new class of compounds containing aza-dibenzothiophene or aza-dibenzofuran are provided. The compounds may be used in organic light emitting devices giving improved stability, improved efficiency, long lifetime and low operational voltage. In particular, the compounds may be used as the host material of an emissive layer having a host and an emissive dopant, or as a material in an enhancement layer.

Abstract: The present invention relates to novel processes for preparing 6-(difluoromethoxy)[1] benzofuro[3,2-c]pyridine-9-carbaldehyde, which is a novel and useful intermediate for preparing compounds with PDE4 inhibitory activity, such as 3,5-dichloro-4-(6-difluoromethoxybenzo[4,5]furo[3,2-c]pyridin-9-ylcarboxamido)-1-pyridiniumolate.

Abstract: Ketimines, enamines and oxazolidines are moisture labile functional groups that in the presence of water undergo hydrolysis to yield free amines. Within the art such latent amines have found utility in curable compositions where it is desirable to initiate cure in the presence moisture. A number of novel polyketimines, polyenamines, polymeric oxazolidines and oxazolidines are disclosed. In particular, polymeric compounds of the above classes derived from C6 cyclic diketones and polyamines are reported. Suitable C6 cyclic diketones include cyclohexanediones and quinones. The invention further relates to the applications of the materials, such as in moisture cure adhesives.

Abstract: The invention provides compounds having the formula: wherein R1 is halogen. The invention also provides compositions comprising the compounds, and methods of treating diseases or disorders that comprise administering one or more of the compounds to a subject in need thereof. The disclosed compounds have CCR1 antagonist activity.

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds.

Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.

Abstract: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.

Abstract: Compounds of the formula (I), in which E, R3, R4, R5, X, Y, W, Q1, Q2, Z, s and m have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.

Abstract: The invention relates to a method for producing ammonium hexafluorophosphates of general formula (1) wherein R1, R2, R3 and R4 are defined as in the claims and in the description, said novel ammonium hexafluorophosphates and to the use thereof for producing pharmaceutically active compounds.

Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa to Xe are each a carbon atom or a nitrogen atom, m is 0 to 2, and ring A to ring C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.

Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, X, Y, W, Q1, Q2, Z, s and m have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 inc

Abstract: The present invention relates to substituted thienyl- and furanyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders.

Abstract: The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, a diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome.

Abstract: 4-substituted 1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR2, O, S, SO, SO2; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, which are optionally substituted; R2 is aryl substituted with —COOR4; or R2 is: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b (b-5); -a1=a2-a3=a4- is —CH?CH—CH?CH—; —N?CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein hydrogen atoms in (c-1)-(c-5) may be replaced by certain radicals; R3 is optionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R21 is halo, hydroxy, amino, carboxyl, C1-6alkyl, C3-7cycloalkyl, arylC1-6alkyl, formyl, C1-6alkylcarbonyl, C1

Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.

Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: This invention relates to novel processes for the preparation of compounds of the formula [1], wherein R1, R2, R3 and R4 are as defined in the claims and description as well as pharmaceutically acceptable salts thereof. The compounds of the formula [1] are hexacyclic compounds having potent anti-tumor activity.

Abstract: The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula I wherein R1, R2, R3, R6, R7 and Q are defined as in claim 1 as well as their crystalline forms for the treatment of proliferative diseases such as cancer.

Abstract: This invention relates to cleaning compositions comprising organic catalysts having enhanced enzyme compatibility and processes for making and using such cleaning compositions.

Abstract: Carbazole-containing compounds are provided. In particular, the compounds are oligocarbazole-containing compounds having an unsymmetrical structure. The compounds may be useful in organic light emitting devices, in particular as hosts in the emissive layer of such devices.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.

Abstract: Carbazole-containing compounds are provided. In particular, the compounds are oligocarbazole-containing compounds having an unsymmetrical structure. The compounds may be useful in organic light emitting devices, in particular as hosts in the emissive layer of such devices.

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including inflammatory and immune diseases, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted

Abstract: This invention concerns the synthesis of polycyclic structural components of pharmacological compounds, including the synthesis of fused benzofuro-heterocycles, through selective palladium-catalyzed cross-coupling and intramolecular cyclization.

Abstract: This invention relates to cleaning compositions comprising organic catalysts having enhanced enzyme compatibility and processes for making and using such cleaning compositions.

Abstract: The invention describes novel organic nitric oxide enhancing salts of nonsteroidal antiinflammatory drugs (NSAIDs) and novel compositions comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent.

Abstract: The invention relates to a new process for preparing tiotropium salts of general formula 1 wherein X? may have the meanings given in the claims and in the specification.

Abstract: The use of azaxanthones for treating diseases associated with tumor cells which express one or more protein of S100 family, and in treating patients that have malignancies consisting of tumors of an epithelial or mesenchymal nature, where these compounds are effective in retarding the progression and/or metastasis of these tumors.

Abstract: The invention relates to compounds of the formula (I), in which R1, R2, R3, R4, Y and A have the meanings indicated, and to processes for the preparation thereof and to the use thereof for the preparation of medicaments.

Abstract: The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with at least one radical that is attached to the phenyl radical by a carbon-carbon bond as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherin all variables are defined in claim 1.

Abstract: This invention relates to a compound of Formula (I) wherein Y is CH or N; Ar1 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each selected independently from (C1-C3)alkoxy halo, OH, CF3, CN, NO2 and (C1-C3)alkyl, said alkyl being optionally substituted with CF3; Ar2 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each independently selected from halo, OH, CN, NO2, CF3, (C1-C6)alkoxy, NR1R1, S(O)2R2, C(O)R3, and (C1-C6)alkyl optionally substituted with R4, and its use in treating hyper-proliferative disorders.

Abstract: Nucleophosmin inhibitors are disclosed which inhibit the multimerization of nucleophosmin and the biological activity of nucleophosmin, such as the ability of nucleophosmin to inhibit apoptosis and inhibit cellular differentiation. These small molecule inhibitors are useful for treating diseases and disorders, such as cancer associated with dysregulated nucleophosmin expression. Methods for identifying small molecule inhibitors of nucleophosmin involving multimerization sites for nucleophosmin are also disclosed.