Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.

Abstract: This invention relates to novel compounds of formula (I). Formula (I) in which the variable groups are as defined in the specification and claims, to pharmaceutical compositions containing them, and to a method of treatment using them for treatment of cancer.

Abstract: Provided herein are pyrrolotriazine compounds for treatment of JAK kinase, including JAK2 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

Abstract: The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer.

Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.

Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation, wherein R1, R2, R3, R4, Q, A and B are as defined herein.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.

Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

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

Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.

Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof.

Abstract: Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic framework are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and pro-drugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to a use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.

Abstract: The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.

Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract: A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed.

Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.

Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

Abstract: The invention relates to triazine derivatives of formula (I): which are inhibitors of phosphodiesterase 2 or 10, useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.

Abstract: The invention relates to imidazo[5,1-c][1,2,4]benzotriazine derivatives of formula I: which are inhibitors of phosphodiesterase 2 or 10 useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.

Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I) are useful as kinase modulators, including Btk modulation, wherein R1, R2, R4, Q, Y, A and D are as defined herein.

Abstract: Preparing dyes suitable for cosmetic use that start with known dyes and link them, for example, with 1,3,5 triazine to bulky organic groups that control solubility.

Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or pharmaceutically acceptable salt, stereoisomer, or hydrate thereof, wherein R1 is lower alkyl, R2 and R3 are independently selected from lower alkyl, and lower alkenyl and lower alkynyl, wherein the lower alkyl, lower alkenyl, and lower alkynyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio, A is N or C—H, B is N, C—H, C—(SO2—R4), or C—CO—R4, D is N, C—H, C—(SO2—R4) or C—CO—R4, E is N or C—H, wherein only one of A, B or E may be N, and one of B or D is C—(SO2—R4) or C—CO—R4, R4 is a group having the formula: in which each R5, R6, R7 and R8 are independently selected from H and lower alkyl, wherein the lower alkyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio; and additionally or alternatively R6 and R5

Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

Abstract: This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.

Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.

Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract: This invention relates to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.

Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.

Abstract: The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.

Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.

Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.

Abstract: A compound of formula (I): wherein the substituents are as defined in the specification as inhibitor of C-Jun N terminal Kinases (JNK) and P-38 Kinases.

Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.

Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or pharmaceutically acceptable salt, stereoisomer, or hydrate thereof, wherein R1 is lower alkyl, R2 and R3 are independently selected from lower alkyl, and lower alkenyl and lower alkynyl, wherein the lower alkyl, lower alkenyl, and lower alkynyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio, A is N or C—H, B is N, C—H, C—(SO2—R4), or C—CO—R4, D is N, C—H, C—(SO2—R4) or C—CO—R4, E is N or C—H, wherein only one of A, B or E may be N, and one of B or D is C—(SO2—R4) or C—CO—R4, R4 is a group having the formula: in which each R5, R6, R7 and R8 are independently selected from H and lower alkyl, wherein the lower alkyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio; and additionally or alternatively R6 and R5

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases.

Abstract: The invention relates to novel uses of imidazo[1,2,4]triazinones for producing a medicament for the treatment and/or prophylaxis of coronary cardiopathy, heart failure, pulmonary hypertension, bladder complaints, prostatic hyperplasia, nitrate-induced tolerance, or diseases of the eye, such as glaucoma, for the treatment or prophylaxis of central, retinal or posterior ciliary artery occlusion, central retinal vein occlusion, optical neuropathy, such as anterior ischaemic optical neuropathy and glaucomatous optical neuropathy, in addition to macular degeneration, diabetes, in particular diabetic gastroparesis, for the treatment of dysperistalsis of the stomach and oesophagus, female infertility, premature contractions, pre-eclampsia, alopecia, psoriasis associated with renal syndrome, cystic fibrosis, cancer and for improving cognition, powers of concentration, learning skills or hypermnesia, in particular if the disorder is a symptom of dementia.

Abstract: Compounds of the formula (I): or a pharmaceutically-acceptable salt or pro-drug thereof: wherein R1 is selected for example from hydrogen, halogen, optionally substituted methyl; R2 and R3 are independently selected from hydrogen, fluoro, chloro and trifluoromethyl; R4 and R5 are independently selected, for example, from hydrogen, methyl, optionally substituted (2-4C)alkyl, C(O)R6 or R4 and R5 together with the nitrogen to which they are attached form an optionally substituted 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring or an optionally substituted imidazole ring. Methods for making the compounds of formula (I), compositions containing them and their use as antibacterial agents are also described.

Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.

Abstract: The present invention relates to heterocyclic compounds represented by the formula I or pharmaceutically acceptable salts thereof and antitumor agents containing the heterocyclic compounds as effective components: wherein X represents nitrogen atom or CH; R1 represents CHnF3-n (wherein n is 1 or 2), hydroxy C1-C6 alkyl, NHR6 [wherein R6 represents hydrogen atom or COR (wherein R represents hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy)]; R2 represents morpholino (which may be substituted with one to four C1-C6 alkyl), thiomorpholino, piperidino, pyrrolidinyl (which may be substituted with hydroxy C1-C6 alkyl), oxazolidinyl (which may be substituted with one or two C1-C6 alkyl) or tetrahydro-1,4-thiazin-1-oxo-4-yl; R3 and R4 each represent hydrogen atom or C1-C6 alkyl; and R5 represents hydrogen atom, amino or hydroxyl.

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: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.

Abstract: The present invention relates to heterocyclic compounds represented by the formula I wherein X represents nitrogen atom or CH; R1 represents halogen atom or hydroxyl; R2 represents hydrogen atom, hydroxyl or amino; R3 represents morpholino (which may be substituted with one or two C1–C6 alkyl), pyrrolidinyl (which may be substituted with hydroxy C1–C6 alkyl) or NR6R7 [R6 represents C1–C6 alkyl and R7 represents piperidinyl (which may be substituted with C1–C6 alkyl)]; R4 and R5 each represents hydrogen atom or C1–C6 alkyl, with the proviso that R2 is hydrogen atom and R3 is pyrrolidinyl (which may be substituted with hydroxy C1–C6 alkyl) when R1 is hydroxyl

Abstract: The present invention relates to heterocyclic compounds represented by the formula I or pharmaceutically acceptable salts thereof and antitumor agents containing the heterocyclic compounds as effective components: wherein X represents nitrogen atom or CH; R1 represents CHnF3-n (wherein n is 1 or 2), hydroxy C1–C6 alkyl, NHR6 [wherein R6 represents hydrogen atom or COR (wherein R represents hydrogen atom, C1–C6 alkyl or C1–C6 alkoxy)]; R2 represents morpholino (which may be substituted with one to four C1–C6 alkyl), thiomorpholino, piperidino, pyrrolidinyl (which may be substituted with hydroxy C1–C6 alkyl), oxazolidinyl (which may be substituted with one or two C1–C6 alkyl) or tetrahydro-1,4-thiazin-1-oxo-4-yl; R3 and R4 each represent hydrogen atom or C1–C6 alkyl; and R5 represents hydrogen atom, amino or hydroxyl.