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: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the structure (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Z, L2 and w are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

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

Abstract: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.

Abstract: The compounds of formula I in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.

Abstract: The invention relates to substituted sulfonamido-macrocycles according to the general formula (I): in which R1, R2, R4, R5, A, B, C, L, X, Y, Z, n, and m are as defined in the claims, and salts, N-oxides, or solvates thereof, to pharmaceutical compositions comprising said substituted sulfonamido-macrocycles, to methods of preparing said substituted sulfonamido-macrocycles as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.

Abstract: The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.

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: Compounds of formula (I): wherein A represents a 5, 6 or 7-membered (hetero)aromatic or non-aromatic ring, n and n? represent 0, 1 or 2 X represents an alkylene chain as defined in the description, R3 represents an aryl or heteroaryl group, one of the groups R1 and R2 represents a hydrogen atom and the other represents a group of formula (II) as defined in the description. Medicinal products containing the same which are useful in treating conditions involving a defect in apoptosis.

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: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly hyperproliferative diseases such as cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly hyperproliferative diseases such as cancer.

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 provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.

Abstract: The invention provides compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each independently of one another represent a hydrogen atom or a (C1-C4)alkyl group, or else R2 and R3, together with the nitrogen atom bearing them, form a pyrrolidinyl, piperidinyl, morpholinyl or 4-(C1-C4)alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type which may carry one or more halogen atoms and/or one or more (C1-C4)alkyl and/or (C1-C4)alkoxy groups; in the form of bases, addition salts with acids, solvates or hydrates; the pharmaceutical compositions comprising them, processes for preparing them, and synthesis intermediates.

Abstract: The invention relates to a pyridazine derivative of formula (I), wherein the variables are as defined herein, pharmaceutical composition thereof, process for its preparation, and its pharmaceutical use.

Abstract: The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of m, R1, Z, n and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal

Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

Abstract: The present invention relates to hexacyclic compound of the formula [1], wherein Z, R3 and R4 are as identified therein, and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of cell proliferative disorders.

Abstract: The invention concerns compounds of general formula (I), wherein: X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1–C4)alkyl group; R2 and R3, represent each, independently of each other, a hydrogen atom or a (C1–C4)alkyl group, or R2 and R3 form, with the atom which bears them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl, pyridazinyl type, the heteroaromatic group may represent one or several halogen atoms and/or one or several (C1–C4)alkyl, (C1–C4)alkoxyl groups; in the form of bases, addition salts to acids, solvates or hydrates.

Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2–3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formul

Abstract: New compounds having a tricyclic pyrazolotriazolopyrimidine ring structure are provided and methods of using those compounds for a variety of therapeutic indications.

Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl.

Abstract: 8-phenyl-6,9-dihydro-[1,2,4]triazolo[3,4-i]purin-5-one derivatives of formula (I): or a pharmaceutically acceptable salt thereof processes for their preparation, pharmaceutical compositions containing them and their use as PDE 5 inhibitors.

Abstract: A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R1N—C?O or N?C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, V1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, V2 represents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when V1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X—Y-Z represents R1aN—C?O and R2 represents a substituted lower

Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.

Abstract: The invention provides compounds of formula (I) wherein R is as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals, for use in the treatment of any state associated with high levels of activeted PARP.

Abstract: A class of substituted imadazolo[2,1-a]phthalazine derivatives as ligands for GABAA receptors of formula I: which are partial or full inverse agonists of an ?5 receptor subunit while being relatively free of activity at ?1 and/or ?2 and/or ?3 receptor subunit binding sites are described herein; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.

Abstract: Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, are useful as anti-inflammatory agents, in which R1, R2, and R3 are hydrogen, halogen, alkyl, or perfluoroalkyl; R4 is an optionally substituted alkyl or cycloalkyl group; X is a linker; A is an aryl, heteroaryl, heterocycle, cycloalkyl, or is absent; and R7 is a substituent on A as defined in the specification.

Abstract: Disclosed herein are compounds having the structural formula A including pharmaceutically acceptable salts or solvates of said compound, wherein X, Y, Q and R are as defined in the specification; pharmaceutical compositions thereof; methods of treating central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment, and processes for preparing the compound of this invention.

Abstract: The present invention relates to hexacyclic compound of the formula [1], wherein Z, R3 and R4 are as identified therein, and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of cell proliferative disorders.

Abstract: The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.

Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and the pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a compound of formula I 1

Abstract: The invention provides compounds of formula I: 1

Abstract: The invention provides compounds of formula I: wherein R1-R8 and A-G have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.

Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.

Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Abstract: Tri-heterocyclic compound of formula (I) 1

Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5-or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.

Abstract: The present invention provides compounds that act to suppress p53 activity in mammalian cells, and a method to effectively suppress p53 activity in the cells of a mammal subject to a stress or pathology that is ameliorated by such suppression.

Abstract: Compounds of formula (I′), wherein A, R1 to R3 and t are as defined in the disclosure, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.

Abstract: The present invention provides a compound of formula I 1

Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein R1 and R2 are as defined in the specification. The compounds are useful for the treatment of viral infections.

Abstract: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

Abstract: A compound of the formula 1

Abstract: The invention provides compounds of formula (I) wherein R is as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals, for use in the treatment of any state associated with high levels of activeted PARP.

Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted  m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—,  phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinso

Abstract: The invention relates to triazolo[4,3-a]pyrido[2,3-d]pyrimidine-5-one derivatives, their regioisomers, their salts and their solvates if they exist, their preparation, compositions containing them and their use. These derivatives possess properties inhibiting PDE4 and/or the release of TNF&agr;, and may therefore be used for the treatment or prevention of numerous conditions by virtue of the inhibition of the PDE4 enzyme and the resulting increase in the cAMP level.

Abstract: This invention concerns amide derivatives of Formula (I) wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.