Abstract: The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, wherein Y1, m, n, R1; X1; X2; R2; X3; X4; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are kinase inhibitors useful for the treatment of disease states mediated by kinase, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.

Abstract: The present invention relates to compounds useful as inhibitors of Tec family protein kinases. These compounds have the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, G, Cy1, and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.

Abstract: Compounds having formula 1: are produced by contacting a compound having formula (6A) with a compound having formula (7), or tautomers thereof, in the presence of a non-nucleophilic base, wherein V, A, Z, L, L1, W, X, B?, R and n are as defined herein.

Abstract: The present invention comprises pyridopyrimidinediamine compounds of the general formula I: The compounds of the present invention are potent inhibitors of PTP1B. Accordingly, the invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.

Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.

Abstract: Compounds having formula 1 are produced by contacting a compound having formula(6A) with a compound having formula (7), or tautomers thereof, in the presence of a non-nucleophilic base, wherein V, A, Z, L, L1,W, X, B?, R and N are as defined herein.

Abstract: The present invention is directed to methods for screening for metallohydrolase inhibitors using metal binding moieties in combination with targeting moieties.

Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

Abstract: Thiopheneprymidinone compounds useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.

Abstract: The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.

Abstract: Use of a precursor of an n-dopant for doping an organic semiconductive material, as a blocking layer, as a charge injection layer, as an electrode material, as a storage material or as a semiconductor material itself in electronic or optoelectronic components, the precursor being selected from the following formulae 1-3c:

Abstract: The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed.

Abstract: Thiopheneprymidinone compounds useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.

Abstract: Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.

Abstract: Compounds of formula: are disclosed. In these compounds is a heterocyclic ring. The compounds are useful as analgesics, anti-pruritics, anti-diarrheal agents, anticonvulsants, antitussives, anorexics/antiobesity agents and as treatments for hyperalgesia, drug addiction, respiratory depression, dyskinesia, pain (including neuropathic pain), irritable bowel syndrome and gastrointestinal motility disorders.

Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

Abstract: The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment and/or prophylaxis of narcolepsy.

Abstract: [Problems] To provide an efficient process for producing an optically active epoxy compound. [Means For Solving Problems] The process for producing an optically active epoxy compound comprises asymmetrically epoxidizing an unsaturated compound with an oxidizing agent in the presence of an optically active titanium-salen complex, an optically active titanium-salalen complex or an optically active titanium-salan complex, with addition of a buffering agent or a buffer solution. The process can inhibit catalyst degradation, reduce the amount of the catalyst used in the reaction, and inhibit a by-product, compared with the prior art, and can provide an optically active epoxy compound in high chemical yield and optical yield and with high quality, and therefore is an industrially useful process.

Abstract: Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R14, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

Abstract: The present invention provides tetracyclic imidazole analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing these compounds, and methods of using the same.

Abstract: The present invention relates to a 6,7-dihydrobenzimidazo[1,2-c]quinazolin-6-one carboxylic acid and its esters of the general structural formula (I), and provides a method for their synthesis (I) where R and each R? are selected independently from the list comprising —H—CH3, —C2H5, —C3H7, -iso-C3H7, —CH2CH2CH2CH3, —CH(CH3)CH2CH3, —CH2CH(CH3)CH3 and —C(CH3)3; n is 1, 2, 3 or 4; Y is a substituent selected from the list comprising —CH3, —C2H5, —NO2, —Cl, —Br, —F, —CF3, —CN, —OH, —OCH3, —OC2H5, —OCOCH3, —OCN, —SCN, —NH2, —NHCOCH3; and z is 0, 1, 2, 3 or 4.

Abstract: The present invention is related to 6,7-dihydrobenzimidazo[1,2-c]quinazolin-6-one derivatives of the general structural formula (I), the anisotropic optical film based on these derivatives with phase-retarding properties for displays, and method of producing thereof (I) where X is a carboxylic group COOH, m is 0, 1, 2 or 3; Y is a sulfonic group SO3H, n is 0, 1, 2 or 3; Z is an add amide group L-NH2; p is 0, 1, 2 or 3; K is a counterion selected from the list comprising H, NH4+, Na+, K+, Li+, Mg2+, Ca2+, Zn2+, and Al3+; s is the number of counterions providing neutral state of the molecule; R is a substituent selected from the list comprising CH3, C2H5, NO2, Cl, Br, F, CF3, CN, OH, OCH3, OC2H5, OCOCH3, OCN, SCN, NH2, and NHCOCH3; w is 0, 1, 2, 3 or 4; and R1 is a substituent selected from the list comprising H, CH3, C2H5, C3H7, i-C3H7, CH2CH2CH2CH3, CH(CH3)CH2CH3, CH2CH(CH3)CH3 and C(CH3)3 and L is a linking group.

Abstract: Disclosed are compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof or wherein R1, R2, R3, R4, R6, R7, R14, W, V, X, Y, A and b are as described above in the specification. Also disclosed is a method of inhibiting aspartyl protease, methods of treating cardiovascular diseases, cognitive diseases, neurodegenerative diseases, and other biological processes and indications. Combination treatments and compositions are also disclosed.

Abstract: Provided are compounds of the formula: wherein RN1 is a substituent of formula G1—NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.

Abstract: The present application describes substituted pyrimidine compounds of formula (I) wherein X, A1, R1, R2, R3, R4, R5, R6, R7, R8, R9, p, q, r, v, and w are defined in the specification, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions.

Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.

Abstract: The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed.

Abstract: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHCOR?, NHSO2R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.

Abstract: The invention relates to novel pyrimidothienoindazoles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.

Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-C6alkyl, polyhaloC1-C6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, p

Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

Abstract: The invention relates to novel pyrimidothienoindazoles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.

Abstract: The present invention relates to the preparation of compounds which are capable of inducing cell death such as apoptotic cell death (apoptosis), and/or for reducing a cell proliferative disorder.

Abstract: 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.

Abstract: A pyridothienopyrimidine derivative of formula (I), or the pharmaceutically acceptable salts or N-oxides thereof are disclosed, as well as pharmaceutical compositions comprising said compounds and methods of treatment or prevention of a pathological condition or disease susceptible to amelioration by inhibition of phosphodiesterase 4 using said compounds are disclosed.

Abstract: Inhibitors of Pim kinases, ways to make them and methods of treating patients using them are disclosed.

Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.

Abstract: The present disclosure relates to a pyridofuropyrimidine derivative of formula (I): wherein G1 is a group chosen from —CR6R7— and —O— wherein R6 and R7 are independently chosen from hydrogen atoms and C1-4 alkyl groups; R1 and R2 are independently chosen from hydrogen atoms and C1-4 alkyl groups; R3 is chosen from C1-4 alkyl, C1-4 alkoxy, amino, hydroxy, mono-C1-4alkylamino, di-C1-4alkylamino, C3-8cycloalkylamino, aryl, heteroaryl and saturated N-containing heterocyclyl groups which are bound to the pyridine ring through their nitrogen atom, all of them being optionally substituted by one or more substituents chosen from halogen atoms and hydroxy, C1-4 alkyl, C1-4alkoxy-C1-4alkyl, aryl-C1-4alkyl, —O(CO)OR8, C1-4 alkoxy, —(CO)NR8R9, —CN, —CF3, —NR8R9, —SR8 and —SO2NH2 groups wherein R8 and R9 are each independently chosen from a hydrogen atom or a C1-4 alkyl group; R4 and R5 are independently chosen from hydrogen atoms, C1-4alkyl groups, hydroxyl-C1-4alkyl groups and groups of formula (II): wherein p a

Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-?]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2/f]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-g allcyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.

Abstract: The invention relates to compounds of general formula (I); 1a, 1 b, 1 c and 1 d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNF?-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.

Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.

Abstract: The present invention discloses novel steroid mimics wherein a tri- or tetravalent phosphorous atom is isosterically substituted at any one of the seventeen positions occupied by the carbon atom in the steroidal skeleton, and wherein each adjacent position to the phosphorous is either unsubstituted or optionally substituted by nitrogen or an oxygen atom to satisfy the valency of said phosphorous atom. The invention is illustrated schematically below using both aromatic and non-aromatic steroids. Although the isosteric substitution phosphorous atom in the above structures 3–7 is indicated at 13, 14, and 17 positions, it is to be noted that the phosphorous can be substituted at any one of the seventeen positions in non-aromatic or eleven positions in aromatic steroids. The phosphorous atom may be trivalent or tetravalent, and may be radioactive or non-radioactive. The adjacent atoms, X, Y, or Z may be carbon, oxygen, or nitrogen.

Abstract: The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 2,8,9-substituted purines and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.

Abstract: The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P. vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other amide and imide derivatives and their 1-hydroxy analogs. The derivatives of the present invention are also soluble in common organic solvents to facilitate the purification in a large scale synthesis of the composition.

Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.

Abstract: The present invention provides methods to manipulate differentiation of a neuroblastoma cell line (IMR-32) such that predominant Nav expression is either Nav1.3 in IMR-32 cells exposed to retinoic acid or Nav1.7 in cells grown under non-differentiating conditions. The cells of the present invention are useful for the discovery of new compounds that modulate the function of either Nav1.3 and/or Nav1.7.

Abstract: This invention is directed to compound of the following formula (I): wherein R1, R2, R3 and R4 are as described herein. These compounds and pharmaceutical compositions containing the compounds are useful in treating inflammatory disorders in mammals.

Abstract: A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.