The present invention relates to a process for preparing a compound of formula wherein: R2 is cycloalkyl or alkyl, each of which may be optionally substituted; Y is —CONR3R4, —CN or CO2R5; R3, R4 and R5 are each independently H or alkyl; n is 1 to 6; wherein said process comprising the steps of: (i) treating a compound of formula (IV), where R1 is alkyl, with a compound of formula (V) and forming a compound of formula (IIIb); (ii) treating said compound of formula (IIIb) with a compound of formula (I1) to form a compound of formula (I).

The invention relates to ceramide dimers which are constructed from two ceramide molecules which are crosslinked to each other via their lipophilic end. The ceramide molecules thereby have at least one hydrophilic group at their hydrophilic end for increasing the hydration shell of the dimer. The ceramide dimers according to the invention can be used as pharmaceutical preparation or as cosmetic preparation.

The present invention provides compounds of the formula: which are useful as inhibitors of PHD and pharmaceutical compositions thereof.

[Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of Solving the Problem]A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups),a salt of the compound, or a solvate of the salt or the compound.

Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.

The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1 is halogen, vinylene-aryl, substituted aryl, heteroaryl or a benzo[1,3]dioxolil group,W is a group of formula —NH—SO2—R2 or heteroaryl group or NHR3 group where R3 is hydrogen or heteroaryl; and n is 1, 2, 3 or 4. Furthermore, the present invention is directed to pharmaceutical composition containing at least one compound of general formula (I) and/or pharmaceutically acceptable salts or solvates thereof and for the use of them for the preparation of pharmaceutical compositions for the prophylaxis and/or the treatment of protein kinase related, especially CDK9-related diseases e.g. cell proliferative disease, infectious disease, pain, cardiovascular disease and inflammation.

Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

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 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.

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.

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.

Structured films containing multi-walled carbon nanotubes (“MWCNTs”) have enhanced mechanical performance in terms of strength, fracture resistance, and creep recovery of polyimide (“PI”) films. Preferably, the loadings of MWCNTs can be in the range of 0.1 wt % to 0.5 wt %. The strength of the new PI films dried at 60° C. increased by 55% and 72% for 0.1 wt % MWCNT and 0.5 wt % MWCNT loadings, respectively, while the fracture resistance increased by 23% for the 0.1 wt % MWCNTs and then decreases at a loading of 0.5 wt % MWCNTs. The films can be advantageously be created by managing a corresponding shift in the annealing temperature at which the maximum strength occurs as the MWCNT loadings increase.

There may be provided a process for producing a polyimide siloxane solution composition having a further improved long-term viscosity stability; and a polyimide siloxane solution composition. In the process for producing the polyimide siloxane solution composition by polymerizing/imidizing a tetracarboxylic acid component and a diamine component consisting of (a) a diaminopolysiloxane, (b) a diamine having a polar group and (c) a diamine other than (a) and (b) in a solvent, the tetracarboxylic acid component and the diamine component excluding (b) the diamine having a polar group are polymerized/imidized to provide a reaction mixture solution, and then (b) the diamine having a polar group is added to the reaction mixture solution last, and the mixture is polymerized/imidized.

The invention is drawn to fluid concentrate formulations of fatty acid monoethanolamides comprising (a) about 71-76% by weight of one or more C8-C22 fatty acid monoethanolamides, (b) about 15-17% by weight of water, and (c) about 10-12% by weight of one or more hydrotropes, based on the fluid formulation, wherein the fluid formulation is homogeneous, pumpable and color stable at a temperature of less than 55° C. A preferred embodiment is drawn to fluid concentrate formulations of cocamide monoethanolamide (CMEA) consisting of (a) about 71-76% by weight of CMEA, (b) about 15-17% by weight of water, and (c) about 10-12% by weight of glycerol, based on the fluid formulation. Methods of preparing the fluid concentrate formulations mulations are also disclosed. The fluid concentrate formulations of fatty acid monoethanolamides are useful in the preparation of cosmetic and pharmaceutical compositions.

An individual alkamide and/or a mixture having two or more different alkamides, is disclosed for changing, masking or reducing the unpleasant flavor impression of an unpleasant-tasting substance or mixture of substances. The alkamide can be trans-pellitorine; cis-pellitorine; 2Z,4Z- or 2Z,4E-decadienoic acid-N-isobutylamide; 2E,4E-decadienoic acid-N-([2S]-2-methylbutyl)amide; 2E,4E-decadienoic acid-N-([2R]-2-methylbutylamide); 2E,4Z-decadienoic acid-N-(2-methylbutyl)amide; achilleamide; sarmentine; 2E- or 3E-decenoic acid-N-isobutylamide; 3E-nonenoic acid-N-isobutylamide; spilanthol; homospilanthol; 2E,6Z,8E-decatrienoic acid-N-([2R]-2-methylbutyl)amide; 2E- or 2Z-decen-4-oic acid-N-isobutylamide; α-sanshool; α-hydroxysanshool; γ-hydroxysanshool; γ-hydroxysanshool; γ-hydroxyisosanshool; γ-dehydrosanshool; γ-sanshool; bungeanool; isobungeanool; dihydrobungeanool; or tetrahydrobungeanool, or combinations thereof.

The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers of 0 or 1, with the proviso that when m is 0, n is 1 and when m is 1, n is 0; andwherein the dashed circle represents either single or double bonds.

A rinse-off composition, such as a shampoo, hair conditioner or shower gel, comprising a rinse-off composition base, lactoyl ethanolamine and at least one compound selected from the group consisting of N-(4-cyanomethylphenyl) p-menthanecarboxamide and N-(2-pyridin-2-ylethyl) p-menthanecarboxamide. The compositions provide a pleasant, long-lasting cooling sensation.

A novel substituted N-acetyl-L-cysteine (NAC) derivative and methods of using this compound for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

There is provided a method for producing an aqueous acrylamide solution by reacting a composition including acrylonitrile with water to produce acrylamide, in which the composition including acrylonitrile includes 3 to 15 mg of propionitrile per 1 kg of the total weight of the composition including acrylonitrile. According to the present invention, a production method with which it is possible to suppress acrylamide polymerization without lowering quality and thereby obtain a stable aqueous acrylamide solution can be provided.

Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. This disclosure deals with the use of halo active aromatic sulfonamide organic compounds as odor control and/or biocidal agents in a cleaning solution for use with bovines and other dairy animals.

There is provided a method for producing an aqueous acrylamide solution by reacting a composition including acrylonitrile with water to produce acrylamide, in which the composition including acrylonitrile includes 3 to 15 mg of propionitrile per 1 kg of the total weight of the composition including acrylonitrile. According to the present invention, a production method with which it is possible to suppress acrylamide polymerization without lowering quality and thereby obtain a stable aqueous acrylamide solution can be provided.

The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.

The subject of the present invention are novel esters of (acyloxymethyl)acrylamide, a pharmaceutical composition containing them and their use in the production of drugs for the prophylaxis or treatment of oncogenic diseases and diseases connected with increased cell proliferation.

A method for inhibiting the crystal growth rate of an amide compound present in a molten polyolefin-based resin and a method for producing a polyolefin-based resin molded article are provided. A phenol compound is incorporated into an amide compound-containing polyolefin-based resin such that a weight ratio, amide compound:phenol compound, is 60:40 to 10:90.

A polyimide demonstrates low coefficient of hygroscopic expansion and low water absorption coefficient when used as an insulation film. The polyimide is derived from a tetracarboxylic acid dianhydride containing ester group expressed by the general formula below, and a polyester imide precursor: wherein R is independent and represents a straight or branched-chain alkyl group with 1 to 6 carbon atoms or straight or branched-chain alkoxyl group with 1 to 6 carbon atoms, n is an integer of 0 to 4, and m is an integer of 2 to 4, but wherein, if m =2, n is an integer of 1 to 4.

The present invention relates to a process of making a compound of formula (I): Wherein, R1, R2, R4 and X are as defined herein.

This disclosure relates to a method for preparing alkyl lactate with high yield and high selectivity, comprising the step of reacting glycerol with water or alcohol in the presence of a catalyst. In addition, the present invention provides a method for efficiently preparing lactamide using the alkyl lactate.

Phosphoranimide-metal catalysts are disclosed. The catalysts comprise first row transition metals such as nickel, cobalt or iron. The hydrocarbon-soluble catalysts have a metal to anionic phosphoranimide ratio of 1:1, and have no inactive bulk phase and no dative ancillary ligands. The electronic state of the clusters can be adjusted to optimize catalytic activity for a range of commercially important reductive transformations, including hydrodesulfurization. A method of synthesis of these catalysts by anionic metathesis of a halide substituted precursor followed by oxidation is also disclosed.

A modified polysiloxane compound is represented by following Formula (1), in which R1 to R9 represent hydrocarbon groups selected from linear alkyl groups having 1 to 20 carbon atoms, branched chain alkyl groups having 3 to 6 carbon atoms, and cyclic alkyl groups having 3 to 6 carbon atoms; p and q represent average numbers of siloxane units indicated in parentheses, where p is a number of 1 or more and q is a number of 2 or more; and “A” represents a group selected from a group represented by following Formula (2), a group represented by following Formula (3), and hydrogen atom. The modified polysiloxane compound has at least a siloxane unit wherein “A” is the group represented by following Formula (2), and a siloxane unit wherein “A” is the group represented by following Formula (3).

Methods to make R13P═N—TiCl3 and (1-R2-Indenyl)Ti(N═PR13)Cl2, where R1 is independently selected from C1-30 hydrocarbyl radical which is unsubstituted or further substituted by one or more halogen atom, a C1-8 alkoxy radical, a C6-10 aryl radical, a C6-10 aryloxy radical, an amido radical, a silyl radical, and a germanyl radical; P is phosphorus; N is nitrogen (and bonds to the metal M); R2 is a substituted or unsubstituted alkyl group, a substituted or an unsubstituted aryl group, or a substituted or unsubstituted benzyl group, wherein substituents for the alkyl, aryl or benzyl group are selected from alkyl, aryl, alkoxy, aryloxy, alkylaryl, arylalkyl and halide substituents. The method to make R13P═N—TiCl3 combines a titanium species TiCl3(OR) where R is an alkyl or aromatic group, with a trimethylsilyl phosphinimide compound R13P═N—SiMe3 in the presence of solvent, to give the titanium complex R13P═N—TiCl3. The method to make (1-R2-Indenyl)Ti(N═PR13)Cl2 consists of deprotonating 1-R2-indene with an appropriate base, followed by reaction with R13P═N—TiCl3.

Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumors, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.

The present invention discloses novel process for the preparation of (2R)-2-acetamido-N- benzyl-3-methoxypropanamide of Formula I involving novel intermediates of Formula-XIX and Formula-XX.

The present invention is directed towards microcapsules, uses and methods of microencapsulation with improved properties regarding agglomeration, bleeding and control of the reaction. The invention is especially suitable for chemical compounds with at least one carboxamide group, preferably for microencapsulation of those compounds wherein the carbonyl group is attached to a nitrogen atom or nitrogenated heterocycle and wherein the microencapsulation reaction may be too vigorous. The microcapsules are characterized by a mixed glycoluril-polyurea polymer wall, wherein the polyurea groups come from a urea-formaldehyde resin and not from isocyanate monomers or prepolymers. The process of making such microcapsules a dispersant in the oil phase of the type of block copolymer of vinylpyrrolidone/vinylalkene and/or vinylpyrrolidone/vinyl acetate and the microencapsulation reaction may be carried out without the presence of any polyamine/polyol acting as a catalyst.

The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.

Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S;A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; andR1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.

New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.

Disclosed is a humidity indicator which contains no heavy metal and has good visibility of a color change that occurs when the humidity is increased. The humidity indicator can be produced by applying an aqueous coating comprising a leuco dye, an acidic compound which is in a solid state at ambient temperature, a deliquescent substance and an aqueous resin emulsion onto a substrate such as a resin film, a nonwoven fabric or a paper, and heating and drying the resulting product.

A system and method can support a flooding mechanism using a multicast group in a middleware machine environment. The middleware machine environment can comprise a gateway instance that includes an external port for receiving one or more data packets from an external network. The middleware machine environment also comprises one or more host servers, each of which is associated with one or more virtual machines that can process the data packets. Furthermore, said host servers can provide virtual interfaces that belong to a virtual hub associated with the gateway instance. At least one said packet is a flooded packet that is specified with an unknown destination address when it is received at the external port. The gateway instance operates to send the flooded packet to the multicast group that operates to forward the flooded packet to one or more said host servers in the multicast group.

A description is given of N-(1,2,5-oxadiazol-3-yl)pyridinecarboxamides of the general formula (I) as herbicides. R in this formula (I) stands for radicals such as hydrogen, organic radicals, and other radicals such as halogen. W stands for a substituted pyridyl radical.

The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.

Disclosed are solid forms of 8-chloro-N-[(2-chloro-5-methoxyphenyl)sulfonyl]-6-(trifluoromethyl)-imidazo[1,2-a]pyridine-2-carboxamide (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are nematocidal compositions comprising a nematocidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other nematicide, insecticide and/or fungicide are also disclosed.Also disclosed are methods for protecting a plant from nematodes comprising applying to the plant, or portion, or seed thereof, or to the growing medium of the plant, a nematocidally effective amount of Compound 1 comprising the polymorph Form A.

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.

There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.

This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method of preparing a benzoimidazole derivative at high purity and high yield, wherein the benzoimidazole derivative is synthesized using a novel intermediate, namely, benzaldehyde, and thereby the preparation process is simple so that it can be applied to production.

A composition is provided for use as a friction modifier for an automatic transmission, which comprises a condensation product of a hydroxypolycarbox-ylic acid, such as 2,3-di-hydroxybutanedioic acid or 2-hydroxybutanedioic acid, with an N,N-di(hydrocarbyl)alkylenediamine, where each hydrocarbyl group contains 1 to 22 carbon atoms, provided that the total number of carbon atoms in the two hydrocarbyl groups is at least about 9, and the alkylene group contains 2 to 4 carbon atoms.

Biomaterials that support cell attachment and growth are provided. In one aspect, biomaterials are provided comprising a first polymer matrix comprising reactive amino moieties and a second polymer matrix that interpenetrates with the first polymer matrix, where the second polymer matrix comprises a poly(alkylene oxide) comprising two or more alkylene oxide oligomers joined by gamma-thioether carbonyl linkages. In another aspect, biomaterials are provided comprising at least one biopolymer comprising amino groups, thiol groups, and bifunctional modifiers connecting at least some of the amino groups to at least some of the thiol groups; and at least one poly(alkylene oxide) cross-linked to at least two thiol groups of the biopolymer. The biomaterials may further comprise a pharmacologically active agent or cells. Methods of administering such biomaterials to a patient in need thereof are also provided.