Abstract: The present invention relates to pyridine methylene azolidinone compounds of Formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, allergy, asthma, pancreatitis, multi-organ failure, kidney diseases, platelet aggregation, cancer, sperm motility, graft rejection or lung injuries. Specifically, the present invention is related to pyridine methylene azolidinone derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide-3-kinases, PI3Ks.

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: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

Abstract: Compositions, methods, and combination therapies for the treatment of cancers, including lymphomas, leukemias, melanomas, lung cancer, and metastatic disease, are provided. Specifically, compositions comprising ligands to Pgrmc1 are disclosed for use in treating and inhibiting tumor growth and progression and inhibition of metastases. The compositions and methods using these ligands can be used alone or in combination with other reagents and cancer treatment modalities.

Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.

Abstract: A method for treating or preventing a host mammal that exhibits aversive signs and symptoms present during protracted abstinence or extended discontinuation syndromes as seen after cessation of compulsive activity, behaviors, or substance use is disclosed. That method comprises administering to a host mammal in need a pharmaceutical composition containing an aversive sign and symptom lessening amount a compound of Formula I or a pharmaceutically acceptable salt thereof dissolved or dispersed in a physiologically acceptable diluent, and repeating the administration as needed, wherein W, X, Y and Z, R1 and Ar are defined within. Data are provided in rats as host mammals using behavioral models dependent on the CRF1 system: defensive burying, alcohol dependence, cocaine dependence and nicotine dependence. A contemplated method also is useful for inhibiting relapse of such a behavior.

Abstract: The present application describes macrocyclic compounds of formula (I) with NS3 protease inhibitory activity for treating hepatitis C virus infection.

Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.

Abstract: The invention is directed to Compounds of Formula (I). The invention provides compounds that inhibit, regulate, and/or modulate P13K that are useful in the treatment of hyperproliferative diseases, such as cancer.

Abstract: The invention provides compounds of the general Formula (I) where R1, R2, and A are defined herein, as well as the preparation, compositions and uses thereof.

Abstract: The invention provides compounds of Formula (Ia) or pharmaceutically acceptable salts thereof, as well as the preparation, compositions and uses thereof, where R1, R2, R3, and m are defined as described above.

Abstract: The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of G protein-coupled receptor 119 (“GPR119”) in a patient.

Abstract: This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.

Abstract: Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in treating p38 mediated disorders in a patient.

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract: The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.

Abstract: Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract: The invention is directed to a Compound of Formula I, II, or III. The invention provides compounds that inhibit, regulate, and/or modulate PI3K that are useful in the treatment of hyperproliferatives diseases, such as cancer.

Abstract: Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors.

Abstract: The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-K?).

Abstract: Compounds of formula (I): A-B—C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an

Abstract: The present invention relates to novel compounds of formula I and therapeutically acceptable salts thereof, their pharmaceutical compositions, processes for making them and their use as therapeutic methods for treatment and/or prevention of various diseases.

Abstract: Compounds of the following formula are provided for use with MEK (I): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract: The present invention relates to methods and compositions for modulating levels of amyloid-? peptide (A?) exhibited by non-neuronal (i.e., peripheral) cells, fluids, or tissues. The invention also relates to modulation of A? levels via selective modulation (e.g., inhibition) of ?-secretase activity. The invention also relates to methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an A?-related disorder, by administering a compound that result in the modulation of ?-secretase in a non-neuronal tissue, either directly or indirectly to prevent, treat or ameliorate the symptoms of a brain A? disorder, such as Alzheimer's disease.

Abstract: The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.

Abstract: The present invention relates to uses, methods and compositions for treating immune-mediated glomerulonephritis, such as crescentic glomerulonephritis. More specifically, the invention relates to the use of an EFGR antagonist or of an inhibitor of EGFR or HB-EGF expression for the treatment of said diseases.

Abstract: This application discloses novel pyrimidinyl pyridone derivatives according to Formula I, wherein R1, R2, and R3 are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.

Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.

Abstract: The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-K?).

Abstract: The invention is directed to Compounds of Formula I: optionally as a single stereoisomer or mixture of stereoisomers thereof, and additionally optionally as a pharmaceutically acceptable salt thereof; as well as methods of making and using the compounds.

Abstract: The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.

Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds, and 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(M)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.

Abstract: Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors.

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer s disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia.

Abstract: The present invention is directed to compounds of formula (I), (Ia),(Ic) and (Id), compositions, and uses thereof as an inhibitor of the p38 kinase, and wherein, inter alia R1 is C(Z)N(R10?)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10?)C(Z)(CR10R20)vRb; N(R10?)C(Z)N(R10?)(CR10R20)vRb; or N(R10?)OC(Z)(CR10R20)vRb; R3 is C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroarylC1-10 alkyl, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted; X is R2, OR2?, S(O)mR2?, (CH2)n?N(R10?)S(O)mR2?, (CH2)n?N(R10?)C(O)R2?, (CH2)n?NR4R14, (CH2)n?N(R2 ?)(R2?), or N(R10?)—Rh—NH—C(?N—CN)NRqRq?; and R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted; or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I), wherein: R1 is amino, R4 is hydrogen, and R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.

Abstract: Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain.

Abstract: Substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-2-yl and 5,6,7,8-tetrahydro-quinazolin-2-yl compounds, corresponding to formula I processes for the production thereof, pharmaceutical preparations containing these compounds the use thereof for the production of pharmaceutical preparations and related method of treating or inhibiting certain disorders or conditions, including pain.

Abstract: Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.

Abstract: Disclosed are compounds and derivatives thereof their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.

Abstract: Compounds of formula I: wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds, pharmaceutical compositions, methods of using the compounds for treatment of p38 MAP kinase-mediated diseases, and methods of using the compounds for treatment of Raf kinase-mediated diseases.

Abstract: Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.

Abstract: Provided herein are pharmaceutical compositions comprising one or more phosphodiesterase inhibitors of type IV (“PDE-IV”), and at least one other active ingredient such as muscarinic receptor antagonists (MRA), ?2-agonists, p38 MAP Kinase inhibitors, or corticosteroids and optionally one or more pharmaceutically acceptable excipients. In addition, methods of treating autoimmune, inflammatory or allergic diseases or disorders are provided.

Abstract: 2-amino-pyrido(3,2-d)pyrimidine derivatives with a specific substitution pattern on positions 4 and 6 of the core structure are useful in the treatment or prevention of an infection due to a virus from the Flaviviridae family, especially HCV, when administered to a patient in a therapeutically effective amount.

Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein, abl kinase protein, bcr-abl kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein comprises the step of contacting said kinase protein with the novel compounds.

Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract: The disclosure relates to methods of treating leukaemia, in particular myeloid leukaemia, comprising administering the compound N-[2-(2,1,3-benzothiadiazol-5-ylamino)-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-N?-(1,1-dimethylethyl)-urea or a hydrate, a pharmaceutically acceptable salt or a solvate thereof.

Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: This invention relates to compounds of Formula (I), and to pharmaceutically acceptable salts and solvates thereof, wherein Z, W, X, Y, V, R1, R2, and R3 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula (I) and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula (I). The invention also relates to methods of preparing the compounds of Formula (I).