The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionizing radiation.

The present invention provides 4,6-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.

The present application is directed to solid forms of compounds of formula I: and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.

The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.

The invention relates to oxazolopyrimidine compounds of formula I, where A, R1 and R2 are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.

The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

This invention relates to novel 5-[(hydroxymethyl)aryl]-substituted pyrrolo[2,1-f][1,2,4]triazin-4-amines of formula (I), to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating angiogenesis-related disorders, in particular angiogenesis-related ocular disorders.

The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like ; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O—(alkylene)—Y, —O—Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.

The presently-disclosed subject matter relates to compounds of the formula: and methods for use thereof. The presently-disclosed subject matter relates methods of selectively differentiating a stem cell, and methods of screening for compounds useful for enhancing terminal differentiation of committed cardiac progenitor cells.

The present invention relates to a novel acid addition salt of risperidone, wherein acid counterion is selected from the group consisting of pamoic acid, caproic acid, cypionic acid, decanoic acid, camphor sulfonic acid, enanthic acid, palmitic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, levulinic acid and valeric acid, a process for the preparation and pharmaceutical composition comprising the same. Further, the invention relates to the use of said pharmaceutical composition comprising the acid addition salt of risperidone in the treatment of patient suffering from psychotic disorders.

The present invention is related to methods for the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S,6E)-dihydroxy-hept-6-enoic acid, intermediates thereof and methods for producing said intermediates.

4,6-dichloro-2-methyl-5-(1-acyl-2-imidazolin-2-yl)-aminopyrimidine is reacted with methanol in the presence of a non-ionic organic base, and moxonidine is obtained directly from the reaction mixture.

Disclosed is a method for preparing optically pure (+)-ambrisentan and (+)-darusentan, comprising: firstly catalyzing the asymmetric epoxidation of a β-unsaturated alkene using a chiral ketone derived from fructose or a hydrate thereof as a catalyst, and then subjecting the product to an epoxy compound ring-opening reaction and substitution reaction successively to obtain optically pure (+)-ambrisentan and (+)-darusentan.

A process of making a polymeric phenazonium compound having the general formula: wherein R1, R2, R4, R5, R6, R8, and R9 are the same or different, and represent hydrogen, a low alkyl or a substituted aryl, R3 starts with NH2 and is diazotized followed by a polymerization, R5 and R8 may alternatively represent monomeric or polymeric phenazonium radicals, R7 is a carbon in the aromatic ring, Rx and Ry represent any combination of CH3, C2H5, and hydrogen, except that Rx and Ry cannot both be hydrogen, A is an acid radical, and n is an integer from 2 to 100, preferably from 2 to 20 is described. The polymeric phenazonium compound is usable as an additive in a metal plating bath comprising copper. The method includes the steps of a) dissolving an effective amount of an amino compound in a formic acid solution; b) adding a nitrite salt to diazotize the amino compound; and c) adding sulfamic acid to neutralize any excess nitrous acid that may be formed in step b), whereby a polymeric phenazonium compound is produced with a smaller quantity of unreacted monomer remaining in the end product than those produced using methods of the prior art.

Derivatives of 2,5-piperazinedione of formula (I) are apoptotic peptidase activating factor 1 (Apaf-1) inhibitors, therefore they are useful as active pharmaceutical ingredients for the prophylaxis and/or treatment of a pathological and/or physiological condition associated with an increase of apoptosis.

Formaldehyde-free binder compositions are described that include an aldehyde or ketone, a nitrogen-containing salt of an inorganic acid, and an acidic compound. The acidic compound may be an organic acid, such as maleic acid or citric acid among others. The acidic compound is supplied in quantities that lower the pH of the binder composition to about 5 or less. The binder compositions may be used in methods of binding fiberglass and the resulting fiberglass products have an improved tensile strength due to the addition of the acidic compound.

A composite sheet of the present invention comprises an oxetane-epoxy-based compound, represented by chemical formula 1, as a binder.

Disclosed are oil-extended olefin block copolymer compositions with precipitated silica. The precipitated silica reduces oil-bleed while maintaining composition softness.

The object of the present invention is to provide an intermediate film for laminated glass which prevents reductions of transparency and appearance property caused by permeation of moisture and water. The above object is attained by the present invention, i.e., a composition for forming an intermediate film for a laminated glass which comprises ethylene-vinyl acetate copolymer and a compound having alkyleneoxy group. The composition of the present invention enables the formation of an intermediate film for a laminated glass that restrains white spots from occurring by the permeation of moisture and water.

Polyamide molding materials for transparent molding parts. The materials comprise transparent copolyamides that contain: (A) 40 to 100 wt % of at least one transparent copolyamide with a glass transition temperature (Tg) of at least 80° C. and not more than 150° C., composed of at least two diamines that are different from each other, wherein the at least two diamines are a mixture of (a) 50 to 90 mol % bis-(4-amino-3-methylcyclohexyl)methane (MACM) and/or bis-(4-amino-3-ethylcyclohexyl)methane (EACM) and/or bis-(4-amino-3,5-dimethylcyclohexyl)methane (TMACM) and b) 10 to 50 mol % aliphatic diamine having 9 to 14 carbon atoms, in particular decandiamine, particularly preferably at least 20 mol % decandiamine, each relative to the total amount of diamines, and of one or more aliphatic dicarboxylic acids, having 6 to 36 carbon atoms, (B) 0 to 60 wt % of at least one further polymer, (C) 0 to 10 wt % of additives, the sum of the components (A), (B) and (C) totaling 100% by weight.

Composite material that contain epoxy resin which is toughened and strengthened with thermoplastic materials and a blend of insoluble particles. The uncured matrix resins include an epoxy resin component, a soluble thermoplastic component, a curing agent and an insoluble particulate component composed of elastic particles and rigid particles. The uncured resin matrix is combined with a fibrous reinforcement and cured/molded to form composite materials that may be used for structural applications, such as primary structures in aircraft.

The invention relates to a polymer product obtained by polymerization of i) at least one monomer selected from N-vinylformamide and vinyl acetate, andii) maleic anhydrideto give a copolymer comprising N-vinylformamide and/or vinyl acetate and maleic anhydride followed by hydrolyzing formamide groups originating from N-vinylformamide to amino groups and/or acetate groups originating from vinyl acetate to hydroxyl groups and acid anhydride to dicarboxylic acid groups to give a water-soluble copolymer comprising amine and/or hydroxyl and carboxyl groups, wherein the molar ratio of the N-vinylformamide and/or vinyl acetate monomer to the maleic anhydride monomer is from 70:30 to 30:70. The polymer product can be used as a dispersing agent or as a scale inhibiting agent.

A composition comprising particulate solid (typically a pigment or filler), an organic medium (typically the organic medium may be a plastics material or an organic liquid) and a polyacrylic copolymer.

Formulations comprising an isosorbide-modified unsaturated polyester comprising maleic acid, fumaric acid, itaconic acid or maleic anhydride and isosorbide and one or more low profile additives. The formulations exhibit better shrink control in molding compound formulations with standard low profile additives than their non-isosorbide-modified analogues. These isosorbide-modified unsaturated polyester resins may be applied in molding compounds like sheet molding compounds or bulk molding compounds and may be components of fiber reinforced composites or other composite materials.

An ion-conductive thermoplastic compositions contains a partially acetalated polyvinyl alcohol, at least one support electrolyte and at least one plasticizer. The partially acetalated polyvinyl alcohol contains two different acetal units. Electrochromic laminated glass systems produced using the ion-conductive compositions and a method for producing the systems are also provided.

The invention relates to radiation curable coating systems on the basis of aqueous polyurethane dispersions, to a method for the production thereof, to the use of the coating systems as paints and/or adhesives, and to objects and substrates provided with said paints and/or adhesives.

Disclosed is an adhesive for a polarizing plate that comprises a polyvinyl alcohol-based resin with an acetoacetyl group and an amine-based metal compound crosslinking agent, and a method of manufacturing the same.

Injection molded articles and process of forming the same are described herein. The processes generally include providing a polyolefin including one or more propylene heterophasic copolymers, the polyolefin having an ethylene content of at least 10 wt. % based on the total weight of the polyolefin; contacting the polyolefin with a polylactic acid and a reactive modifier to form a compatiblized polymeric blend, wherein the reactive modifier is produced by contacting a polypropylene, a multifunctional acrylate comonomer, and an initiator under conditions suitable for the formation of a glycidyl methacrylate grafted polypropylene (PP-g-GMA) having a grafting yield in a range from 1 wt. % to 15 wt. %; and injection molding the compatibilized polymeric blend into an article.

A self-priming spackling compound includes between about 35% by weight and about 65% by weight acrylic latex resin, between about 20% by weight and about 50% by weight filler material, and between about 1% by weight and about 20% by weight water. In certain aspects, the latex resin may have an average latex particle size of less than about 0.18 microns, a minimum film formation temperature of less than about 15 degrees Celsius, and/or a glass transition temperature (Tg) of less than about 25 degrees Celsius. To further enhance the self-priming performance of the spackling compound, the formulation may further comprise a colorant such as titanium dioxide.

Plasticizing system which can be used in particular for the plasticizing of a tire diene elastomer composition containing, in combination: a plasticizing hydrocarbon resin, the glass transition temperature of which is greater than 0° C.; anda tri- or pyromellitate ester corresponding to the formula (I): in which the R radicals, which are identical or different, represent a hydrocarbon radical and the R' radical represents hydrogen or COOR group. Also, a rubber composition incorporating the plasticizing system and the use of such a composition for the manufacture of a tire or tire semi-finished product made of rubber, in particular of a tire tread, exhibiting an improved wear resistance without having a detrimental affect on its wet grip.

Disclosed are oil-extended olefin block copolymer compositions with microcrystalline wax. The microcrystalline wax reduces oil-bleed while maintaining composition softness.

Water-borne cross-linking polymeric compositions and related embodiments, such as methods of making and using the compositions, as well as products formed with said compositions are described. The water-borne composition may comprise one or more polymers formulated from one or more monomers of which at least one is a monomer that yields acetaldehyde as a hydrolysis product, and incorporating cross-linking functionality such as, but not limited to, carbonyl or epoxy functionality, and a blocked cross-linking agent, for example, a hydrazone. Neither the cross-linking functionality nor the acetaldehyde reacts with the blocked cross-linking agent; however, the blocked cross-linking agent is capable of conversion to an alternative form cross-linking agent such as, but not limited to, a hydrazide, to yield a cross-linked polymer. The alternative form cross-linking agent may be formed in an equilibrium reaction including the blocked cross-linking agent.

A rubber composition for manufacturing tyres is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more 1,2,4-triazine compounds chosen from compounds of formula I and compounds of formula II: Certain specific 1,2,4-triazine derivatives are described.

A 1,3-diketoamide functional monomer represented by the following formula (1): wherein R and Y are independently selected from the group consisting of hydrogen, an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 20 carbon atoms, and an aralkyl group having from 7 to 20 carbon atoms; and wherein X and Z are independently selected from the group consisting of an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 20 carbon atoms, and an aralkyl group having from 7 to 20 carbon atoms. Also disclosed are emulsion, suspension, and solution polymers comprising residues from the 1,3-diketoamide functional monomer of formula 1 and, optionally, one or more additional ethylenically unsaturated monomers. Both latex and self-curing coating compositions described herein exhibit excellent hydrolytic stability, including increased retention of 1,3-diketo functionality.

An aqueous dispersion includes particles at least partially encapsulated in a microgel where the microgel is prepared from a hyperbranched acrylic polymer. In addition, a method for making an aqueous dispersion includes: (1) mixing in an aqueous medium: (a) particles, (b) at least one ethylenically unsaturated monomer, and (c) a water-dispersible hyperbranched acrylic polymer having ethylenic unsaturation; and (2) polymerizing the at least one ethylenically unsaturated monomer and water-dispersible hyperbranched acrylic polymer having ethylenic unsaturation to at least partially encapsulate the particles in a microgel.

A primer solution for enhanced adhesion to a rigid substrate for aviation and aerospace applications includes an aminosilane-capped polyurethane prepolymer and a first solvent. The first solvent reacts with or modifies the surface of the rigid substrate, enabling the primer solution including the aminosilane-capped polyurethane prepolymer to become a part of the surface of the rigid substrate.

The present invention has an object to provide an ink for inkjet textile printing which has excellent fastnesses and causes less bleeding on a textile and to provide a low cost method for inkjet textile printing by using said ink; and relates to an ink for inkjet textile printing wherein the ink contains at least one kind disperse dye, a dispersing agent, water and at least one kind (referred to as A compound) of the compounds represented by the following formula (1): (wherein, n is an integer number of 1 to 12) and at least one kind compound (referred to as B' compound) selected from the group consisting of alkanediols having 3 to 5 carbon atoms and polypropylene glycols, as organic solvents, the total content of A compound and B' compound is 12 to 50% by weight based on the total amount of the ink, and the ratio by weight of A compound to B' compound is in the range of 5:1 to 0.7:1.

The present invention pertains to an additive combination comprising at least two sterically hindered amines, at least one further stabilizer, a dispersing agent and a plasticizer. The present invention also pertains to a composition comprising an organic material susceptible to degradation by light, oxygen and/or heat, and the additive combination and to the use and the process for stabilizing organic material against degradation by light, oxygen and/or heat by the additive combination.

The present invention is directed at a binder for a battery electrode comprising an ethylene oxide-containing copolymer including a first monomer of ethylene oxide (EO) and at least one additional monomer selected from an alkylene-oxide that is different from the first monomer of EO, an alkyl glycidyl ether, or a combination thereof; wherein the ethylene oxide-containing copolymer has a weight average molecular weight less than about 200,000 g/mole (e.g., from about 10,000 to about 100,000), the molar fraction of the first monomer of EO (XEo) in the ethylene oxide-containing copolymer is greater than 0.80 (e.g., from about 0.80 to about 0.995), and the ethylene oxide-containing copolymer has a peak melting temperature (Tp), in ° C., for a selected XEO in the range of about 0.80 to about 0.995, which is below a maximum value of Tpmax, at the selected XEO, which is calculated using the equation Tpmax=(60−150 (1−XEO)).

A rubber composition that can be used in applications such as automotive tires and can improve the fuel efficiency performance and driving stability of automobiles and the like, a method for producing a rubber composition, and a tire using the same are provided. A rubber composition comprising: (A) a conjugated diene rubber which is obtained by polymerizing a conjugated diene compound or polymerizing a conjugated diene compound and an aromatic vinyl compound and has a group having an active hydrogen and a group capable of chemically binding to a silica, (B) a silica, (C) a silane coupling agent (I) capable of reacting with a carbon-carbon double bond of the conjugated diene in the conjugated diene rubber, and (D) a silane coupling agent (II) capable of reacting with the group having an active hydrogen; a method for producing a rubber composition, which comprises mixing the above-mentioned composition; and a tire which is obtained by crosslinking and molding the rubber composition obtained by the method for production.

Non water-soluble polymers with a comb structure and a (meth)acrylic skeleton on which are grafted side chains containing at least one hydrophobic monomer of the styrene or (meth)acrylic ester type on C1 to C4, and at least one hydroxy or methoxy polylakylene glycol monomer. The levels of monomers are such that the polymer is amphiphilic because it is both rich in hydrophobic monomer and polylakylene glycol monomer. These products, used in paper coating dispersions, enable an increase in their Brookfield™ viscosity, a reduction in their ACAV viscosity, and an improvement in their water retention, which makes them particularly well suited for dry extract and/or high deposit speed coatings.

A long-fiber-reinforced resin composition including (A) a long-fiber-reinforced thermoplastic resin pellet including a thermoplastic resin, a modified polyolefin-based resin modified with an unsaturated carboxylic acid or its derivative and reinforcing fiber and satisfying (A-1) the melt index of the thermoplastic resin is 100-250 g/10 min, (A-2) the relaxation time λ of the thermoplastic resin is 0.1 (sec) or less, (A-3) the content of the reinforcing fiber is 40-70 wt %, and (A-4) the content of the modified polyolefin-based resin is 1-5 wt %; and (B) a polyolefin-based resin satisfying (B-1) the melt index of the polyolefin-based resin is 20-70 g/10 min, and (B-2) the relaxation time λ of the polyolefin-based resin is 0.23 (sec) or less; wherein the content of reinforcing fiber contained in (A) is 20-60 wt % relative to the total amount of the fiber-reinforced resin composition.

A platinum complex having the following formula (I) is disclosed, ##STR1## wherein R1 and R2 may be the same or different and each independently represents a methyl group or an ethyl group, and the configuration of 1,2-diaminocyclohexane is either cis-, trans-l-, trans-d-, or trans-dl-.The compound possess excellent antitumor activity with a high therapeutic index and abundant water solubility, and thus are effective as an antitumor agent.

Beta-lactamase inhibiting compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition or carboxylate salt thereof; where n is zero, 1 or 2; X3 is H or Br, R1 is H, the residue of certain carboxy-protecting groups or the residue of an ester group readily hydrolyzable in vivo; one of R12 and R13 is H and the other is vinyl, certain aryl, alkylthio, alkylsulfonyl or certain heterocyclyl, aminomethyl, thiocarboxyamido or amidino groups; one of R2 and R3 is H and the other is as disclosed for the other of R12 and R13, or is Cl or CH2 OH, and R18 is H or certain acyl groups; intermediates useful in their production, methods for their preparation and use, and pharmaceutical compositions containing them.

Compounds of formula (I) ##STR1## in which R1 is hydrogen, O°, CN, NO, cyanomethyl, C1 -C12 -alkyl, C3 -C12 -alkenyl or C3 -C12 -alkynyl subject to the proviso that the carbon atom attached to the nitrogen atom is a primary carbon atom, C7 -C12 -aralkyl, C1 -C12 -acyl, 2,3-epoxypropyl, OH-monosubstituted C2 -C6 -alkyl or 2,3-dihydroxypropyl, R2 is hydrogen, C1 -C18 -alkyl, C5 -C18 -cycloalkyl, C6 -C18 -aryl or C7 -C18 -aryalkyl, R3 is C6 -C18 -aryl or a group of the formula (II) ##STR2## in which R1 is as defined above, n is an integer from 1 to 4 and R4 is an organic or inorganic radical of a valency equal to n are useful for stabilizing organic material against oxidative, thermal and/or light induced degradation.

A glycerol derivative which is effective to reduce blood pressure and has the formula: ##STR1## wherein R1 is an alkyl group having 10-22 carbon atoms, R2 is a lower acyl group or benzoyl, each of R3 and R4 independently is hydrogen or a straight or branched chain alkyl group having 1-6 carbon atoms; each of R5, R6 and R7 independently is hydrogen, a straight or branched chain alkyl group having 1-6 carbon atoms, an aryl group or an aralkyl group; and each of m and n independently is 0 or a positive integer under the condition of m+n=2-8.

The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R1, R2, R3 and R4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.