Abstract: Disclosed are compounds of Formula 1, wherein X is O or S; Y is O or S; and R1, R2, R3 and R4 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: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

Abstract: Disclosed is an arthropod pest control composition having an excellent controlling effect on arthropod pests, which comprises a compound represented by formula (I): wherein each symbol is as defined in the present description; and metalaxyl or metalaxyl M.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.

Abstract: Novel conjugates and immunogens derived from risperidone and antibodies generated by these immunogens are useful in immunoassays for the quantification and monitoring of risperidone and paliperidone in biological fluids.

Abstract: [Problems to be solved by the invention] A method and sensor for detecting the fluorides, chlorides or bromides of hydrocarbons such as C5F8 or C4F6 are provided, which are capable of the detection with quickness and high sensitivity at a room temperature or a temperature closer thereto, not a high temperature, without interference with hindrance gases from fluorine liquids or the like. [Means for solving the problems] A detection agent, detection method, and detection sensor based on an optical change or mass change by a direct reaction with a nitrogen compound having at least two rings at which an amidine backbone is centered, which is represented by the following general formula (I).

Abstract: Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

Abstract: Embodiments of this invention provide methods for therapeutic use of cyclic G-2-allylProline (cG-2-allylP) to treat peripheral neuropathies, including toxin-induced peripheral neuropathy and diabetic peripheral neuropathy as well as manufacture of medicaments including tablets, capsules, and other orally active compositions containing cG-2-allylP, as well as injectable solutions that are useful for treatment of such conditions.

Abstract: The present invention provides a control agent that is extremely effective in controlling bacterial diseases. The quorum sensing inhibitor and bacterial disease control agent for agricultural and horticultural use of the present invention contain a pyrimidinone compound represented by General Formula (1): wherein R1 represents a C1-5 alkyl group or a phenyl group, and R2 represents a hydrogen atom or a C1-5 alkyl group, provided that R1 cannot be a methyl group when R2 represents a hydrogen atom.

Abstract: A salt catalyst comprises an ionic complex of i) a nitrogen base comprising one or more guanidine and/or amidine functional groups, and ii) an oxoacid comprising one or more active acid groups, the active acid groups independently comprising a carbonyl group (C?O), sulfoxide group (S?O), and/or a phosphonyl group (P?O) bonded to one or more active hydroxy groups; wherein a ratio of moles of the active hydroxy groups to moles of the guanidine and/or amidine functional groups is greater than 0 and less than 2.0. The salt catalysts are capable of catalyzing ring opening polymerization of cyclic carbonyl compounds.

Abstract: Methods and formulations for the treatment of multiple sclerosis with drugs with affinity for both serotonergic 5-HT2 and dopaminergic receptors such as the D2 receptor are herein disclosed. According to one embodiment, a method includes delivering a therapeutic dosage of drugs with affinity for both serotonergic 5-HT2 and dopaminergic receptors such as the D2 receptors to a subject exhibiting symptoms of multiple sclerosis to alleviate the symptoms.

Abstract: Disclosed are compounds of Formula 1, wherein R1 is phenyl or pyridinyl, each optionally substituted with Q and up to 3 substituents independently selected from R2; each R2 is independently halogen, cyano, SF5, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio or C1-C4 haloalkylthio; and Q is phenyl or pyridinyl, each optionally substituted with up to 5 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy. 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: The present invention relates to compounds of Formula I as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and methods of treating a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogenital disorders, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof.

Abstract: The present invention relates to a novel process for the preparation of paliperidone and its intermediates and also relates to an improved process for the preparation of paliperidone compound of formula (I).

Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.

Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.

Abstract: The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent Paliperidone carrier conjugate of formula (I) wherein Z0 is defined in the description and the claims as well as pharmaceutical composition comprising said compounds. The compounds are useful as medicament, especially for diseases or disorders which can be treated by Paliperidone.

Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.

Abstract: The present invention related to fused pyrimidine derivatives, which are useful as Transient Receptor Potential Vanilloid 3 (TRPV3) receptors, methods of treating diseases, disorders, conditions modulated by TRPV3. The present invention having the formula (I) and its pharmaceutically acceptable salts thereof, and its processes thereof, wherein all variables are as described herein.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.

Abstract: The disclosure relates to methods and materials useful for depolymerizing a polymer. In one embodiment, for example, the disclosure provides a method for depolymerizing a polymer containing electrophilic linkages, wherein the method comprises contacting the polymer with a nucleophilic reagent in the presence of a guanidine-containing compound. The methods and materials of the disclosure find utility, for example, in the field of waste reclamation and recycling.

Abstract: The present invention relates to an improved process for obtaining Paliperidone, I, comprising alkylating compound VI, or a salt thereof, with compound V, or a salt thereof, using a base selected from triethylamine or diisopropylethylamine and, optionally, a solvent. Moreover, the invention relies on the preparation of intermediates used in such process.

Abstract: The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4.

Abstract: The present invention relates to pharmaceutical composition for subcutaneous injection comprising a paliperidone compound wherein the composition releases the paliperidone with an immediate onset of action and continuously for at least 3 weeks, and wherein the composition has a pharmacokinetic profile in vivo with substantially no burst release of the paliperidone. The compositions are useful as medicaments for the treatment of psychotic disorders and diseases.

Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a—R3e, R4, R5, R6, R7, R8, X1 and E 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: The present invention relates to a novel process for the preparation of paliperidone by hydrolysis of 9-O-acylated paliperidone. In a preferred embodiment of the present invention, Paliperidone Form (II) of purity of about 98% or more was obtained by basic hydrolysis of 9-O-Acetyl Paliperidone.

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula I: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula I.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Abstract: Base-polymerizable or base-crosslinkable compositions comprising select bicyclic amines with benzylic substitution undergo photochemically induced, base-catalysed reactions upon photochemical conversion of the benzylically substituted amine to an amidine derivative.

Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.

Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.

Abstract: The present invention relates to novel compounds of formula (VIII) and (X), processes for their preparation and their use in the preparation of paliperidone or a salt thereof. There is also provided by the present invention novel processes for preparing intermediates for use in the preparation of paliperidone or a salt thereof, and novel processes for preparing paliperidone or a salt thereof.

Abstract: The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): Wherein n, R1, R2, R3, R4, R5 and R6 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

Abstract: Provided herein are impurities of paliperidone, 3-[2-[4-[1-(4-fluoro-2-hydroxyphenyl)methanoyl]piperidinyl-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one (methanoyl impurity), 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (dehydroxy impurity) and 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidin-4,9-dione (9-keto impurity), and processes for preparing and isolating thereof. Provided further herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities, process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities. Provided also herein are improved and efficient processes for preparing paliperidone intermediates.

Abstract: The present invention relates to an improved process for the preparation of pure Paliperidone of formula (I). The present invention more specifically provides an improved process for the preparation of pure Paliperidone which may contain impurities in the acceptable level of pharmacopoeia requirement specifically 3-{2-[4-(5-Fluoro-benzo[d]isoxazol-3-yl]-piperidin-1-yl]-ethyl}-2-methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidine-4,9-dione of Formula (IV).

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.

Abstract: There is provided a hemihydrate form of the sodium salt of pemirolast.

Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed. Wherein m, n, o, Y, Z, R1, R2, R3, R4, R5 R6 and R7 are as described herein. Also disclosed are the salts of compounds of formula (I). The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.

Abstract: Disclosed are compounds of Formula 1, N-oxides and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, EC(?X1); a is 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, X1 and E 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: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 0, 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, R8, X1 and E 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: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

Abstract: Provided herein are solid state forms of paliperidone salts, processes for preparation, pharmaceutical compositions, and method of treating thereof. Paliperidone is represented by the following structural formula (I): More particularly, provided are solid state forms of paliperidone acid addition salts, wherein the acid counter ion is provided by an acid selected from the group consisting of L-(+)-tartaric acid, p-toluenesulfonic acid, maleic acid, oxalic acid, fumaric acid, acetic acid and malic acid. Provided also herein is a process for preparing substantially pure paliperidone free base using the solid state forms of paliperidone salts.

Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob

Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.

Abstract: The invention relates to the use of 4-phenylbutyric acid and/or salts thereof, of the formula (I) for enhancing stress tolerance in plants to abiotic stress, preferably drought stress, and to the associated enhancement in plant growth and/or increase in plant yield.

Abstract: Novel conjugates and immunogens derived from risperidone and antibodies generated by these immunogens are useful in immunoassays for the quantification and monitoring of risperidone and paliperidone in biological fluids.

Abstract: A transdermal preparation is provided that contains risperidone and/or a pharmaceutically acceptable salt thereof as a drug, and the amount of the drug is 1 to 20 parts by mass based on 100 parts by mass of the total mass of the preparation. The skin permeation rate of the preparation is 0.5 to 30 ?g/cm2/hour, and the drug diffusion coefficient of the preparation in the skin is 1.2×10?6 to 10.0×10?6 cm/hour.