Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.

Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.

Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.

Abstract: The invention relates to aminoquinazoline compounds or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein A1, A2, A3, A4, R1, R2, R3, R4, R5a, R5b, R5c, R5d and p are defined as in the description.

Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R43 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.

Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRaRb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.

Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, Ra, R2a, R2b, R1, and X have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.

Abstract: The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof, as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to CNS) and/or associated with the peripheral nervous system (abbreviated to PNS).

Abstract: Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.

Abstract: This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HER1 tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds.

Abstract: Disclosed are: a substance which has an activity of inhibiting the intracellular signaling from a plant-derived cytokinin receptor and which can control the growth or differentiation of a plant. Also, disclose is a method for searching for a chemical substance capable of promoting the growth of a root of a plant, which comprises measuring the level of intracellular signaling from the receptor in a system where a cell having the receptor is contacted with a chemical substance having an agonistic activity on the receptor and a substance to be tested, comparing the level of intracellular signaling measured in the preceding step with a level of intracellular signaling measured in the absence of the chemical substance, and determining the chemical substance as being a chemical substance capable of promoting the growth of a root of a plant based on the difference obtained by the comparison; and others.

Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.

Abstract: The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: The present invention relates to a compound of the general formula (I) useful in the determining the presence, amount or activity of an enzyme in living cells, a method of preparing said compounds and a kit thereof.

Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.

Abstract: Provided are a novel compound for an organic electronic material and an organic electroluminescent device using the same. The compound for an organic electronic material according to the present invention has high electron transport efficiency, thereby preventing crystallization at the time manufacturing of a device, and allows a layer to be easily formed, thereby improving current characteristics of the device, and thus an OLED device having a lowered driving voltage and improved power efficiency as well as superior luminous efficiency and lifespan characteristics as compared with the existing material can be manufactured.

Abstract: This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR?R? and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene; n is 0, 1 or 2; and R6 is selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-?/-oxide, a solvate or a pro-drug thereof.

Abstract: Provided are novel compounds in accordance with Formula I for an organic electronic material and an organic electroluminescent device using same. The compound for an organic electronic material disclosed herein exhibits high electron transport efficiency and thus prevents crystallization upon manufacturing a device, and also facilitates the formation of a layer, thus improving current properties of the device. Thereby, OLED devices having improved power efficiency as well as reduced operating voltage can be manufactured.

Abstract: The present invention provides combinations of active agents, such combinations comprising one or more antifolate compounds. The particularly can include methotrexate and one or more further antifolate compounds. In specific embodiments, the combinations are useful for treating certain conditions, such as rheumatoid arthritis. The invention also provides articles useful to provide the combinations in desirable dosage forms and combinations. The combinations further may be useful in the treatment of further conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.

Abstract: Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided.

Abstract: The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

Abstract: A biscarbazole derivative of the invention is represented by a formula (1) below. In the formula (1): A1 represents a substituted or unsubstituted nitrogen-containing heterocyclic group having 1 to 30 ring carbon atoms; A2 represents a substituted or unsubstituted aromatic hydrocarbon group having 6 to 30 ring carbon atoms, or substituted or unsubstituted nitrogen-containing heterocyclic group having 1 to 30 ring carbon atoms; X1 and X2 each are a linking group; Y1 to Y4 each represent a substituent; p and q represent an integer of 1 to 4; and r and s represent an integer of 1 to 3.

Abstract: This invention provides compounds of Formula I wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.

Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract: A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.

Abstract: Provided herein are hydrobromide salts of a pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating a proliferative disease.

Abstract: A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.

Abstract: Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

Abstract: The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2-heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical compositions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently selected from —CH group or a nitrogen atom (—N), W is independently selected from an aryl group, an heteroaryl group, or a benzocondensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzothiophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [1,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). R1 is independently selected from hydrogen (—H), C1-C4 alkyl, hydroxymethyl (—CH2OH), aminomethyl (—CH2NH2), alkylaminomethyl [CH2NH(R2)], or di-alkylaminomethyl [CH2N(R2)2], trifluoromethyl (—CF3).

Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.

Abstract: This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N(C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.

Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.

Abstract: The invention provides novel compounds based on piperazinylpyrimidine derivatives to be used as protein kinase inhibitors. The compounds may be useful in treating or preventing different cellular proliferation disorders, such as cancer. The present invention also provides methods of preparing these compounds, and methods of using the same.

Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction

Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.

Abstract: The invention provides a compound having a heterocyclic skeleton of formula (I): wherein the indicated moieties are as described in the specification, as well as a tautomer thereof or a salt thereof. The compound is useful as a catalyst for an asymmetric synthesis.

Abstract: A compound of formula (I) wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

Abstract: The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: A method for preparing a halofuginone derivative, in particular a method for preparing an inhibitor medicament expressed by specific I-type procollagen in the invention a condensate of formula (II) reacts for 12-35 hours in a catalytic hydrogenation solvent with the existence of Ni—B amorphous alloy catalyst, at the hydrogen pressure of 0.1-10 Mpa and at the temperature of 10-60° C., and then the catalyst is filtered, the filtrate is decompressed to recover the solvent, the pH value is regulated to obtain a crude product of formula (I), and the crude product of the formula (I) is refined to obtain a refined product of formula (I).

Abstract: The present invention provides a process for making lapatinib and its pharmaceutically acceptable salt by use of new intermediates. A new process for obtaining a pharmaceutical form of lapatinib ditosylate monohydrate is also provided.

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 following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Abstract: The present invention relates to novel quinoxaline, quinazoline and phthalazine derivatives as well as multimeric derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds for the treatment and prevention of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in treating and preventing neurodegenerative diseases.