Abstract: The present invention provides freebase and salt forms of (R)-N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine, which act as inhibitors of AHR, and compositions and methods thereof, useful for treating various conditions in which the aryl hydrocarbon receptor (AHR) is implicated.

Abstract: The present invention relates to pyrazolo [1,5-a][1,3,5]triazine and pyrazolo [1,5-a]pyrimidine derivatives having Formula I: and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides solid forms of (R)—N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine maleate (Compound 2) represented by the formula:

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof a compound described herein.

Abstract: Provided are crystalline forms of 2-Methyl-1-[(4-[6-(trifluoromethyl) pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol mesylate useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof said compound.

Abstract: Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein.

Abstract: In some aspects, the present invention provides compounds of the formula (IV), wherein the variables are as defined herein, which may be used as inhibitors of histone demethylase or spermine oxidase. Also provided herein are pharmaceutical compositions of the compounds and methods using the compounds in the treatment of diseases such as cancer and cardiovascular disease.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The present invention relates to a therapeutic drug or a preventive drug for hypertension or high-normal blood pressure, comprising (a) and (b) as active ingredients: (a) a 2-phenylthiazole compound represented by formula (I) or a pharmaceutically acceptable salt thereof; (b) at least one compound or a pharmaceutically acceptable salt thereof selected from the group consisting of calcium antagonists, renin-angiotensin system inhibitors, diuretics, sympatholytic agents, vasodilators, and medicinally acceptable salts of these. The present invention also relates to a therapeutic method or a preventive method for hypertension or high-normal blood pressure, comprising administering the above (a) and (b) in amounts effective for treating or preventing hypertension or high-normal blood pressure.

Abstract: A kit for protecting keratin materials against UV radiation above 280 nm, including at least two different compositions, at least one compound (X), at least one compound (Y), and at least one hydrophobic screening system including (i) at least one hydrophobic organic sunscreen agent (A) absorbing UV radiation of 320-400 nm and at least one hydrophobic organic sunscreen agent (B) absorbing UV radiation of 280-320 nm, and optionally an inorganic sunscreen (D); (ii) at least one hydrophobic organic sunscreen (C) absorbing UV radiation of 280-400 nm, and optionally an inorganic sunscreen (D); or (iii) at least one hydrophobic organic sunscreen (A) absorbing UV radiation of 320-400 nm and either at least one hydrophobic organic sunscreen (C) absorbing UV radiation of 280-400 nm, or at least one inorganic sunscreen (D); at least one of compounds (X) and (Y) being a silicone compound.

Abstract: The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid.

Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.

Abstract: Provided are biocidal compositions comprising glutaraldehyde and a compound selected from the group consisting of 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; tris(hydroxymethyl)-nitromethane; and a hexahydrotriazine compound. The compositions are useful for controlling microorganisms in aqueous or water-containing systems.

Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.

Abstract: The present intervention generally relates to compositions comprising a PDE11 inhibitor for increasing cortisol levels in a subject, or for increasing the production of cortisol from adenocortical cells in a subject. Aspects of the invention relate to the use of a PDE11 inhibitor in a method of treatment of low cortisol levels and/or adrenal insufficiency in a subject, or a method of treating a disease or disorders associated with adrenal insufficiency. Aspects of the invention relate to PDE11 inhibitors belonging to compounds of formula (I)-(VI), and their use alone or in combination with long-term corticosteroid treatment to elevate cortisol levels in a subject, and/or to treat adrenal insufficiency.

Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

Abstract: Methods of treating bleeding disorders, such as bleeding diseases such as hemophilia, by administering adenosine 2a receptor and/or adenosine 2b receptor antagonists to subjects in need thereof are disclosed. In some embodiments, the methods further include administration of the antagonist with one or more of Factor VIII, Factor IX and Factor XI to treat the bleeding disorder.

Abstract: The present invention relates to combinations of triazine derivatives and of insulin sensitizers.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, where R1 is a (C1-C6)alkyl or (C3-C6)cycloalkyl group; R2 is a (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkenyl, (C1-C6)fluoroalkyl, (C1-C3)fluoroalkoxy, or (C1-C6)alkoxy(C1-C6)alkyl group, substituted: (i) with one to three hydroxyl groups, or (ii) with an NRaRb group, where Ra and Rb are independently a hydrogen atom or a (C1-C3)alkyl group; or a pyrrolidinylmethyl group substituted with one to three hydroxyl groups; R9 is the same as R2 or hydrogen; the R2 and R9 groups independently being substitutable with an —OCOR3 group, where R3 is a natural or unnatural amino acid derivative or a piperidyl group; alternatively, R2 and R9 together form a heterocyclic compound; X and Y are independently a substitutable phenyl or heteroaryl group, the heteroaryl group being a thienyl, pyridyl, pyrimidinyl, thiazolyl, pyrrolyl, or furanyl group; and R6 is a hydrogen or a (C1-C3)alkyl group.

Abstract: This invention relates with anti-tumor activities of new compounds containing an adamantyl group or analogs thereof.

Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.

Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: A method of treatment for epilepsy and other disease states is described, which comprises delivery of gabapentin in a gastric retained dosage form.

Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.

Abstract: For the separation, removal, isolation, purification, characterization, identification or quantification of fibrinogen or a protein that is a fibrinogen analogue, an affinity adsorbent is used that is a compound of formula II wherein one X is N and the other is N, C—Cl or C—CN; Y is O, S or NR2; 0 Z is O, S or NR3; R2 and R3 are each H, alkyl, hydroxyalkyl, benzyl or &bgr; -phenylethyl; n is 0 to 6; A is a support matrix, optionally linked to the triazine ring by a spacer; R7 is a group bearing a positive charge at neutral pH; W is an optional linker; V is an aromatic group; and R8 and R9 are each H, OH, alkyl, alkoxy, amino, NH2, acyloxy, acylamino, CO2H, sulphonic acid, carbamoyl, sulphamoyl, alkylsulphonyl or halogen or a cyclic structure such as a morpholino group, or R8 and R9 are linked to form such a cyclic structure.

Abstract: The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.

Abstract: The present invention relates to methods of preserving or increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof. The present invention also relates to methods of increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.

Abstract: The present invention includes methods, articles, compositions and colorant dyes and pigments that include biocidal N-halamine dye composition having two or more heterocyclic ring structures attached to one or more N-halamine groups, wherein one or more halogens associate with the one or more one or more N-halamine groups to affect biocidal activity.

Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

Abstract: An oil-in-water emulsified sunscreen cosmetic which contains: (A) Containing the following three types of surfactants (A-1)-(A-3); (A-1) A POE stearic ester having a POE mole number of 20-120; (A-2) sorbitan tristearate; and (A-3) glyceryl stearate having a HLB of 5-8; (B) bis-ethylhexyloxyphenolmethoxyphenyltriazine and/or tert-butylmethoxybenzoylmethane, oil soluble ultraviolet absorbents, solid at room temperatures; (C) ethylhexyl methoxycinnamate and/or octocrylene, oil soluble ultraviolet absorbents, liquid at room temperature; (D) phenylbenzimidazolesulfonic acid, a water soluble ultraviolet absorbent; and (E) a higher alcohol having 14-24 carbon atoms.

Abstract: The present disclosure relates to a method of treating hyperuricemia in a patient that also suffers from a second disease state requiring treatment with theophylline, wherein the patient receives concomitant treatment with a xanthine oxidoreductase inhibitor and theophylline without resulting in theophylline toxicity to the patient and without substantial adjustments to the manufacturer's recommended dosage of theophylline.

Abstract: Compositions and methods of treating endothelial disorders, including: asthma, erectile dysfunction, pulmonary hypertension, cardiovascular disorders, and other disorders, using a synergistic combination of at least one arginase inhibitor and at least one phosphodiesterase (PDE1), (PDE2) and/or (PDE5) inhibitor are described.

Abstract: The invention provides ?-helix mimetic structures and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.

Abstract: Antitumor combinations comprising a taxane and at least one epidophllotoxin for treating neoplastic diseases are described.

Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond, —C(O)—, or —C(R3?)(R4?)—; X is —N(R1)— or —C(R6)(R7)—; Y is —S(O)2—, —C(?O)—, —PO(OR9) or —C(R6?R7?)—; is a single or double bond and R, R1, R2, R3, R4, R3?, R4?, R5, R6, R6?, R7 and R7? are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

Abstract: Antitumor combinations comprising a taxane and at least one antimetabolite for treating neoplastic diseases are described.

Abstract: For the separation, removal, isolation, purification, characterization, identification or quantification of plasminogen or a protein that is a plasminogen analogue, an affinity adsorbent is used that is a compound of formula (II) wherein one X is N and the other is N, C—Cl or C—CN; A is a support matrix, optionally linked to the triazine ring by a spacer; Z is O, S or N—R and R is H, C1-6 alkyl, C1-6 hydroxyalkyl, benzyl or &bgr;-phenylethyl; B is an optionally substituted hydrocarbon linkage containing from 1 to 10 carbon atoms; D is H, OH or a primary amino, secondary amino, tertiary amino, quaternary ammonium, imidazole, guanidino or amidino group; or B-D is —CHCOOH—(CH2)3-4—NH2; and q is 2 to 6.

Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, Formula (1): wherein A1, A2, A3, A4, A5 and A6 are independently, selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3; A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2. and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfo?yl, C1-C6 alkylamino, C2-G6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

Abstract: Provided are biocidal compositions comprising 2,2-dibromo-3-nitrilopropionamide and a compound selected from the group consisting of 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; tris(hydroxymethyl)-nitromethane; and a hexahydrotriazine compound. The compositions are useful for controlling microorganisms in aqueous or water containing systems.

Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The present invention relates to the use of specific derivatives of triazinetriones for controlling coccidioses in livestock, especially pigs.

Abstract: Methods for identifying prodrug antibiotic compounds and direct inhibitory antibiotic compounds utilizing various screens are provided. Also provided are methods for treating infections using these compounds.

Abstract: Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.

Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Abstract: The present invention relates to methods for reducing the progression of at least one of cardiac hypertrophy, cardiac remodeling or left ventricular dysfunction following a cardiac insult in a subject in need of treatment thereof. Moreover, the present invention also relates to methods of delaying the onset of heart failure symptoms or reducing the incidence of cardiovascular events following a cardiac insult in a subject in need of treatment thereof.

Abstract: The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson's disease. In one embodiment, the invention features a compound of formula (I).