Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: its pharmaceutically acceptable salt or solvate thereof, wherein X is hydrogen or the like, Y is a group of the formula: Z is —NR7— or the like, R1 is hydrogen or the like, R2 and R3 are each independently hydrogen or the like, n is 0 or 1, p is 0 to 6.

Abstract: The invention includes benzisoxazole piperazine compositions and methods of using them for modulating sleep.

Abstract: A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

Abstract: The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.

Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

Abstract: There is provided compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. Compounds include imidazothiazole derivatives that can inhibit interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity.

Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.

Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.

Abstract: The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein C1 and C2 represent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R1, R2, R3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.

Abstract: Compounds having the general formula III?, or IV? wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, S—R or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and heterocycli

Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.

Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.

Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.

Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.

Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.

Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: A compound which specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist is provided. It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein R1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is —N(R4)—C(?O)—C(?O)—, —N(R4)—(CR5R6)p—C(?O)—, —N(R4)—C(?O)—(CR7R8)q— or —C(?O)—N(R4)—(CR7R8)q—, p and q are each independently an integer of 1 to 3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or lower alkyl, A1 is benzoxazolinone or the like, and A2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.

Abstract: This invention relates to a process for the preparation of 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride, a partial dopamine-D2 receptor agonist and a full serotonin 5-HT1A receptor agonist. This invention also relates to the monohydrate of said compound, as well as to pharmaceutical compositions containing these compounds, to methods for preparing these compounds, to methods for preparing intermediates useful for their synthesis, and to methods for preparing compositions containing these compounds.

Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.

Abstract: The invention relates to processes for the preparation of substantially pure ziprasidone. The invention also relates to the preparation of acid addition salts of ziprasidone. More particularly, it relates to the preparation of substantially pure hydrochloride salt of ziprasidone. The invention also relates to pharmaceutical compositions that include the substantially pure ziprasidone or ziprasidone hydrochloride and use of said compositions for treating schizophrenia.

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.

Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.

Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.

Abstract: The present invention relates to a novel cycloalkane derivative which has an excellent psychotropic action.

Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.

Abstract: Provided is a heterocyclic compound showing strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.

Abstract: Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed.

Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.

Abstract: The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.

Abstract: The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.

Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.

Abstract: The present disclosure provides novel pharmaceutical dosage forms such as a maintenance treatment dose and methods for making the same, and methods for using said compounds and maintenance treatment doses to treat and prevent diseases and/or disorders.

Abstract: The present invention relates to a novel cycloalkane derivative which has a useful psychotropic action with less side effect.

Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.

Abstract: The present invention relates to a new and useful amorphous form of ziprasidone hydrochloride (5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride) and preparations thereof.

Abstract: The present invention provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.

Abstract: The present invention relates to bifeprunox derivatives of formula (I) wherein R1 is one substituent chosen from 3-OH, 4-OH, 3-OSO3H and 4-OSO3H; R2 is H; or an N-oxide or a pharmaceutically acceptable salt, or a solvate or hydrate of any of the foregoing. The compounds of the invention may be used in the treatment or alleviation of dopamine D2 receptor mediated diseases or conditions.

Abstract: This invention relates to a process for the preparation of 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride, a partial dopamine-D2 receptor agonist and a full serotonin 5-HT1A receptor agonist. 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride The invention also relates to polymorphic forms of said compound, as well as to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, to methods for preparing intermediates useful for their synthesis, and to methods for preparing compositions containing these compounds.

Abstract: A compound of formal (I) is described: wherein R1 and R2 are as defined in the text and wherein the compounds are intended for use in treating medical conditions characterized by an imbalance in dopamine receptor activity.

Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

Abstract: The present invention relates to a novel cycloalkane derivative which exhibits an excellent psychotropic action and has less side effect.

Abstract: The present invention relates to a process for preparing Ziprasidone of formula I, or a pharmaceutically acceptable salt or a solvate or a hydrate thereof; comprising the steps of reacting 1-(1,2-benzisothiazol-3-yl) piperazine of formula II or its salt: with 5-(2-haloethyl)-6-chloro-oxindole of formula III: wherein X is leaving groups like fluoro, chloro, bromo, iodo or sulphonyl; in the presence of a dispersing agent and a base in a solvent to form ziprasidone of formula I; and optionally converting the ziprasidone formed into a pharmaceutically acceptable acid addition salts of ziprasidone; or a solvate or a hydrate thereof.

Abstract: A transdermal composition that contains an antipsychotic is provided for the treatment of neuropsychiatric disorders. Also, provided are methods for preparing a topical antipsychotic composition. Methods for treating neuropsychiatric disorders, including schizophrenia, are further disclosed. The transdermal composition includes a therapeutically effective amount of an antipsychotic in an amount sufficient to treat neuropsychiatric disorders in a pharmaceutically acceptable carrier.

Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.

Abstract: The present invention provides compounds of the general formula (I) wherein X, n and R1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, methods for their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, useful in the treatment and/or the prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.

Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.

Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety

Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.