Abstract: The present invention provides glucoimidazole derivatives and methods of making them. The compounds can be used to inhibit the activity of O-GlcNAcase enzymes, including both bacterial OGA (bOGA) and human OGA (hOGA) and can be selective, showing low inhibition of hexosaminidases. The compounds can be used to study the role of the O-GlcNAcase modification in human or animal cells. Furthermore the compounds can have therapeutic uses in the treatment of diseases mediated by the activity of O-GlcNAcase enzymes including type II diabetes, Alzheimers disease, and cancer.

Abstract: The present invention relates to immune response modifiers of formula (I), which act selectively through agonism, of Toll-Like Receptors (TLRs), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infection and cancer.

Abstract: The present invention relates to compounds of the general formula (I): wherein A, B, C and D each independently are a methine group or a nitrogen atom, said methine group optionally having a substituent(s) with at least one of them meaning the methine group; E means a group represented by the following formulae (E1): R1 means a lower alkyl group or an aryl group optionally having a substituent(s) or means a lower alkylene group linked to arbitrary, linkable position(s) of E, and others. The compounds of the present invention are useful as an agent for the treatment of a variety of diseases related to NPY.

Abstract: Muscarinic agonists of the formula (I) with M1 selectivity which are useful as agents for stimulating the cognitive functions of the brain.

Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.

Abstract: Compounds of formula wherein the residues R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, salts thereof; their use, methods of their use, processes for their production, pharmaceutical compositions comprising them, their combinations with second drug substances and the use thereof and the like. The compounds are protein kinase inhibitors and can be used for the treatment of diseases mediated by protein kinase inhibitors, e.g. for the treatment of various proliferative diseases.

Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein.

Abstract: Compounds are provided which may be used to inhibit DPP-IV comprising the formula: wherein the substituents are as described in the specification and claims.

Abstract: This invention relates to derivatives of 4-(benzimidazol-2-yl)fluorene and 4-(azabenzimidazol-2-yl)fluorene, to pharmaceutical compositions comprising such derivatives, and to methods of treatment of disorders related to Hsp90 protein activity, comprising administering such derivatives.

Abstract: Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, L1, V, W, T, Z, R, Y1, and p are as defined herein.

Abstract: The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound having the general formula (I): wherein R1 represents a C1-C6 alkyl group, a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; R2 represents a C1-C6 alkyl group; R3 represents a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; Q represents a group represented by the formula ?CH— or a nitrogen atom; and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, and the like, or a pharmacologically acceptable salt thereof.

Abstract: The present invention relates to compounds of formula (I). These compounds are a novel type of peptide deformylase (PDF) inhibitors, and are therefore of great interest especially as new antibiotics.

Abstract: The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening of compounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral infections.

Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.

Abstract: The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man.

Abstract: Compounds of following formula (I) are provided that have both angiotensin II receptor antagonist activity and PPARy agonist activity. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment of diseases with the compounds including type 2 diabetes, insulin resistance, hyperinsulinemia, hyperlipidemia, hypertriglyceridemia, metabolic syndrome, congestive heart failure, and hypertension.

Abstract: The present invention relates to a new process for the preparation of compounds of general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5?-methylthioadenosine phosphorylases (MTAP), 5?-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). The present invention relates to a new process for the preparation of compounds of general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5?-methylthioadenosine phosphorylases (MTAP), 5?-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH).

Abstract: The invention relates to crystalline 1H-Imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate, E6070, its method of preparation, and its therapeutic uses. Pharmaceutical compositions containing crystalline E6070 and a pharmaceutically acceptable carrier represent one embodiment of the invention. The invention also relates to methods for treating an inflammatory disorder, an autoimmune disorder, or a proliferative disorder comprising the step of administering to a patient in need thereof a therapeutically effective amount of crystalline E6070.

Abstract: The invention relates to enantiomer (?) of tentoprazole. The inventive enantiomer (?) of tenatoprazole, or (?)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]imidazol[4,5-b]pyridine exhibits improved pharmacokinetic properties which make it possible to use a once a day posology of a drug for relevant indications. The enantiomer (?) of tentoprazole can be used for treating digestive pathologies.

Abstract: The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening ofcompounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral infections.

Abstract: The present invention generally relates to methods for the preparation of compounds that contain imidazole moieties. In some embodiments, the methods include the reaction of a diamine with a dichloroimmonium compound to produce the imidazole moiety. In some embodiments, the methods are employed to prepare compounds having the Formulas II, II or III below: I II III wherein the constituent variables are as described herein.

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.

Abstract: Compounds of Formula (I) or a pharmaceutically acceptable derivative thereof: wherein R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: The present invention relates to imidazo[4,5-c]pyridine compounds and pharmaceutical compositions for the treatment or prevention of viral infections, wherein the imidazo[4,5-c]pyridine compounds have the formula:

Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc.

Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

Abstract: The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(?O)—, —C(?NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combinatio

Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.

Abstract: The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed.

Abstract: An emitting compound for an organic electroluminescent device, and an organic electroluminescent device using the same, supply an effective luminance, an efficient driving voltage, and color purity. The emitting compound has an imidazo-pyridine frame represented as in the following Formula 1: where R1 to R14, each of which is independent, refer to the functional groups recited herein.

Abstract: Methods for preparing compounds of the Formulas IV and I are disclosed. The methods include combining a compound of the Formula II: with a benzylamine of the Formula III: in the presence of an acid to provide a 1H-imidazo[4,5-c]pyridine compound of the Formula IV.

Abstract: 1H-Imidazo[4,5-c]naphthyridin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, 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 present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein X, R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: This invention relates to compounds and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein.

Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc.

Abstract: Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

Abstract: The invention relates to novel imidazopyridine derivatives and to their use in the treatment of diseases and disorders which may e.g. involve angiogenesis and/or pain, including autoimmune and inflammatory diseases.

Abstract: The present invention provides a heterocyclic compound having potent tyrosine kinase-inhibiting activity represented by formula: (wherein, R1b is a C6-10 aryl group which has substituent(s), and the like; Ta is a single bond, a C1-6 alkyl group, —CH2O—, and the like; X and Y are the same or different, and each is a nitrogen atom which may have substituent(s), and the like; the broken line is a single bond or a double bond; Za is a nitrogen atom or CH; W is a single bond, an oxygen atom, and the like; Q is a C6-10 aryl group which may have substituent(s) or an aromatic heterocyclic group which may have substituent(s)); or a salt thereof and a pharmaceutical composition comprising thereof.

Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.

Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.

Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC? inhibitors, and their methods of use are disclosed.

Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.

Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein A and R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.

Abstract: The present invention relates to compounds according to the structure (I), Where B is formula (Ia), formula (Ib) or formula (Ic); A is H, OR2 or halogen (F, Cl, Br, I, preferably F or Br, more preferably F); A? is H, OR2 or halogen (F, Cl, Br, I, preferably F or Br, more preferably F); A? is H or OR1, with the proviso that when A? is OR, A is H; and when A is OR2, A? is H; X is C—R3 or N; Y is C—R3 or N; preferably X or Y is N and X and Y are not both simultaneously N; R3 is H or C1-C3 alkyl; D is H or NHR2; E is absent or H; G is O or NHR2; J is N or C—R4; K is N or C—H; R4 is H, halogen (F, Cl, Br, I), CN, —C(?O)NH2, NH2, NO2, —C?C—H (cis or trans) or —C?C—H; Ra is H or CH3; Each R1 is independently H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate, phosphodiester group; Each R2 is independently H, an acyl group, a C1-C20 alkyl or ether group; and Pharmaceutically acceptable salts, solvates or polymorphs thereof.

Abstract: Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines) with an amino substituent at the 1-position, pharmaceutical compositions containing 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: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).

Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.