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 related to fused pyrimidine derivatives, which are useful as Transient Receptor Potential Vanilloid 3 (TRPV3) receptors, methods of treating deseases, 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 discloses 1H-pyrido[1,2-a]pyrimidin-4(9aH)-one derivatives or 1H-pyrimido[1,2-a]pyrimidin-4(9aH)-one derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, cancer, diabetes, obesity, metabolic syndrome and the like.

Abstract: Process for the purification of paliperidone by formation of a salt thereof, such as the hydrochloride.

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: 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 compounds of the formula where A1, A2, A3, A4, L, Q, R1, R2, R3, R4, Rx, Ry, Rz, X, Y1, Y2, Y4 and Z are as described herein, and compositions thereof that are useful in the treatment of inflammatory and immune conditions and diseases. In particular, the invention provides aryl nitrile compounds which modulate the expression and/or function of a chemokine receptor.

Abstract: The present application describes deuterium-enriched risperidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.

Abstract: Methods for determining invertebrate- and insect-specific, such as mosquito-specific, residues of acetylcholinesterases are provided herein. The methods can be used to design pesticides and insecticides that are specific for the invertebrate or insect (e.g., mosquito) enzymes, resulting in reduced toxicity concerns for mammals. Compositions for inhibiting invertebrate and insect (e.g., mosquito) acetylcholinesterases and methods for preparing the same are also provided.

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: A compound having activity to inhibit production and/or secretion of ?-amyloid protein, and is useful for prevention and/or treatment of various diseases associated with abnormal production and/or secretion of ?-amyloid protein, the compound represented by the general formula (I): [wherein, R1 represents a C1-C6 alkyl group which may have 1 to 6 halogen atoms as substituent groups, a C2-C6 alkenyl group which may have 1 to 6 halogen atoms as substituent groups, or a C3-C7 cycloalkyl group which may have 1 to 6 halogen atoms as substituent groups; R2 represents a 6-membered nitrogen-containing monocyclic aromatic heterocyclic group having 1 to 3 substituent groups, or a 9- or 10-membered nitrogen-containing bicyclic heterocyclic group having 1 to 4 substituent groups; Z1, Z2 and Z3 each independently represent a hydrogen atom, a halogen atom or a cyano group; and n represents 0, 1 or 2], salts thereof, or solvates thereof.

Abstract: The present invention relates to new pyrido[1,2-a]pyrimidin-4-one inhibitors of mast cell degranulation, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new benzisoxazole modulators of D2 receptors and/or 5-HT2A receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions.

Abstract: The present invention relates to compounds of the formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

Abstract: The invention provides a more handy and environment friendly process for preparing risperidone, which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride with 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one in a basic aqueous solution or suspension. The concentration of alkaline metal carbonates in the basic aqueous solution or suspension is ranged from 15% to 40%. The reaction is carried out at a temperature range of 101-140° C. and the reaction is completed within 10 minutes to 2 hours.

Abstract: The present invention concerns a process for preparing crystalline 3-(2-chloro-ethyl)-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one substantially free of 2-acetylbutyrolactone.

Abstract: The present invention relates to new benzisoxazole modulators of D2 receptors and/or 5-HT2A receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to a compound of formula (I), an optical isomer or a pharmaceutically acceptable salt thereof, its preparation and uses, wherein R is defined as herein. Such compounds can be presented as an optical isomer or a racemic mixture. The compounds can be metabolized in vivo to form a pharmacologically active substance as antagonist of neurotransmitters, and can be used for the treatment of the related mental disorders such as schizophrenia.

Abstract: Compounds of the Formula (I), (II) and (III) wherein Ar is for example phenylene, biphenylene or naphthylene, all of which are unsubstituted or substituted by C1-C4-alkyl, C2-C4-alkenyl, CN, OR11, SR11, CH2OR11, COOR12, CONR12R13 or halogen; R1, R2, R7 and R8 independently of one another other are hydrogen or C1-C6-alkyl; R3 and R5 together and R4 and R6 together form a C2-C6-alkylene bridge which is unsubstituted or substituted by one or more C1-C4-alkyl; R11 is hydrogen or C1-C6-alkyl; R12 and R13 independently of one another for example are hydrogen, phenyl, C1-C18-alkyl, C1-C18-alkyl which is interrupted by one or more O; n is 1-10; X is O, S or NR10; A and A1 are suitable linking groups; are suitable as photolatent bases.

Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein J is and R1, R2, R3, R4, R5, R6, R7, R8a, R8b, R8c, G1, G2, G3, G4, G5, G6, Q1, Q2, Q3, Q4, W1, W2, Y1, Y2, Y3, m and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.

Abstract: A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof.

Abstract: The present invention relates to a process for preparing aryl-substituted fused pyrimidines of the general formula (I) in which L1 to L5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy etc.; Y1 to Y3 are C—RY or N; RY is H or optionally substituted C1-C4-alkyl or two adjacent RY together form a ring; X is OH, Cl or Br; which comprises (i) the reaction of a 2-phenylmalonate with a compound (III) or a tautomer thereof, in the presence of a suitable base, where the alcohol, released during the reaction, of the formula R—OH is continuously removed from the reaction mixture under reduced pressure; giving a compound of the formula (I) or a salt thereof in which X is OH, and, if X in the compounds of the general formula (I) is chlorine or bromine, (ii) the reaction of the compounds of the formula (I) obtained in step (i) or the salts with a halogenating agent.

Abstract: The present invention relates generally to therapeutic agents, formulations comprising them and their use in the treatment, amelioration and/or prophylaxis of glioma brain tumours and related conditions. The therapeutic agent comprises two fused 6-membered rings with at least a nitrogen at position 1 and a hydroxyl at position 8.

Abstract: A compound of formula (7.2) or an acid addition salt thereof. The compound can be used as a reference standard for monitoring the presence thereof in a paliperidone sample, including monitoring the completion of a paliperidone reaction. Reduction in the amount of the compound in paliperidone can be achieved by crystallization in the presence of a hydride reductant.

Abstract: A compound of formula (6) or an acid addition salt thereof in which G is (i) a leaving group A selected from a halo group and a sulfonyloxy group, or (ii) a group of the formula (20) is useful in processes of making paliperidone and related compounds.

Abstract: Described herein is an improved, commercially viable and industrially advantageous process for the preparation of paliperidone intermediate 9-hydroxy-3-(2-chloroethyl)-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one and its hydrochloride salt. The process provides the paliperidone intermediate in higher yield and reduced reaction time compared to the previously disclosed processes, thereby providing for production of paliperidone and its pharmaceutically acceptable acid addition salts in high purity and in high yield.

Abstract: The present invention provides compounds are disclosed herein having the formula: Wherein n is 1 or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl; R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, —O—(C1-6 alkyl), —NH—(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O—(C1-6 alkyl), aryl, heteroaryl, —C(?O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X?O, NH, —C(?O)— or —N?CH—; and Each L is independently alkylene and carbonyl. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

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: A new compound of formula (IV) R represents a protecting group which is removable by hydrogenation, and use thereof as an intermediate for preparing paliperidone.

Abstract: The present invention is related to processes for the preparation of paliperidone crystalline Form II. The invention also provides a paliperidone crystalline Form II containing isopropyl alcohol, and processes for preparing the same.

Abstract: The present invention concerns novel azolidine compounds of Formula (I) wherein X denotes S, NH, CH2 or O, Y and W denotes each independently S or O, Q denotes CH or N, n and m are an integer from 0 to 2, and R1 and R2 denote independently from each other hydrogen, optionally substituted aryl, optionally substituted heterocyclyl, or an optionally substituted (C1-10) aliphatic group, R3 denotes hydrogen, lower alkyl, halogen, lower alkoxy, nitro, and R4 and R5 denote independently from each other hydrogen, halogen or alkyl, with the proviso that if one of R1 and R2 is hydrogen then the respective other one of R1 and R2 does not denote substituted or unsubstituted 2-furyland their salts, that are useful as pharmaceutical agents, e.g. as antibacterial agents, and to pharmaceutical compositions comprising such compounds.

Abstract: Provided herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity, 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, a process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity.

Abstract: Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.

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 relates to compounds that are useful for treating cellular proliferative diseases, for treating disorders mediated, at least in part, by KSP, and for inhibiting KSP. The invention also related to pharmaceutical compositions comprising such compounds, methods of treating cancer by the administration of such compositions, and processes for the preparation of the compounds.

Abstract: A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtain the compound (1). R represents hydrogen or a C1-C20 acyl group. The process is useful in the synthesis of paliperidone and derivatives.

Abstract: Compounds of the formula I R7?N—R6 RS—C,N—R4 H C, R?/I R, 3 R 2 (I) in which R, is an aromatic or heteroaromatic radical which is capable of absorbing light in the wave-length range from 200 nm to 650 nm and which is unsubstituted or substituted one or more times by C,—C,8alkyl, C2-C,ealkenyl, C2-C,8alkynyl, C,—C,ehaloalkyl, NO2, NR,OR, CN, OR,2, SR,2, C(O)R,3, C(O)OR,4, halogen or a radical of the formula II R˜—N? R6 1 R5-C,N.

Abstract: The present application describes deuterium-enriched peliperidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present application describes deuterium-enriched risperidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present invention relates to compounds that are useful for treating cellular proliferative diseases, for treating disorders mediated, at least in part, by KSP, and for inhibiting KSP. The invention also related to pharmaceutical compositions comprising such compounds, methods of treating cancer by the administration of such compositions, and processes for the preparation of the compounds.

Abstract: The present invention relates to pyrimidinones and pyridones and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ? cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs.

Abstract: Described herein are novel polymorphic forms of paliperidone, processes for preparing the novel forms and use thereof. Also provided are processes for the preparation of novel polymorphic forms of paliperidone and the use thereof in the preparation of pharmaceutical compositions.

Abstract: An improved method of making a substituted pyrazolopyrimidine. The method comprises reacting a aminopyrazole compound or a salt thereof with a substituted 1-oxo-2-propenyl-arene(-heterocycle) or a salt thereof under acidic conditions in a reaction medium including a two-phase mixture of an aqueous solution and a water-immiscible organic liquid. Specific substituted pyrazolopyrimidines include N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide and N-methyl-N-(3-{3-[2-thienyl-carbonyl]-pyrazolo[1,5-a]-pyrimidin-7-yl}phenyl)acetamide.

Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.

Abstract: Processes for preparing paliperidone.

Abstract: A compound of formula (1) is useful as a pharmaceutical and as an intermediate in making paliperidone. wherein Y is an acid-sensitive group of the formula: in which X represents an oxygen atom, a sulfur atom, or an —NH— group; Z represents a C2-C7 alkylene bridge; and R represents hydrogen or a C1-C4 alkyl group.

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.