Abstract: The present invention relates to use of (thio)-carbamoyl-cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of acute mania. Furthermore, the present invention relates to the treatment of acute mania through the administration of (thio)-carbamoyl cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to use of (thio)-carbamoyl-cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of schizophrenia. Furthermore, the present invention relates to the treatment of schizophrenia through the administration of (thio)-carbamoyl cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof.

Abstract: 4-((1R,3S)-6-Chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine hydrogen succinate, pharmaceutical compositions containing the salt and the medical use thereof, including for the treatment of schizophrenia and other psychotic disorders. Also described are methods for the preparation of 4-((1R,3S)-6-Chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine and medical uses thereof.

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.

Abstract: The invention relates to a DGAT inhibitor of formula (I) including any stereochemically isomeric form thereof, wherein A represents CH or N; X represents O or NRx; the dotted line represents an optional bond in case A represents a carbon atom; Y represents a direct bond; —NRx—C(?O)—; —C(?O)—NRx—; —NRx—C(?O)—Z—; —NRx—C(?O)—Z—NRy—; —NRx—C(?O)—Z—NRy—C(?O)—; —NRx—C(?O)—Z—NRy—C(?O)—O—; —NRx—C(?O)—Z—O—; —NRx—C(?O)—Z—O—C(?O)—; —NRx—C(?O)—Z—C(?O)—; —NRx—C(?O)—Z—C(?O)—O—; —NRx—C(?O)—O—Z—C(?O)—; —NRx—C(?O)—O—Z—C(?O)—O—; —NRx—C(?O)—O—Z—O—C(?O)—; —NRx—C(?O)—Z—C(?O)—NRy—; —NRx—C(?O)—Z—NRy—C(?O)—NRy—; —C(?O)—Z—; —C(?O)—Z—O—; —C(?O)—NRx—Z—; —C(?O)—NRx—Z—O—; —C(?O)—NRx—Z—C(?O)—O—; —C(?O)—NRx—Z—O—C(?O)—; —C(?O)—NRx—O—Z—; —C(?O)—NRx—Z—NRy—; —C(?O)—NRx—Z—NRy—C(?O)—; —C(?O)—NRx—Z—NRy—C(?O)—O—; R1 represents optionally substituted C1-12alkyl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRx—C(?O)—Z—; —NRx—C(?O)—Z—NRy; —NRx—C(?O)—Z—C(?O)—NRy—; —C(?O)—Z—;

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

Abstract: The present invention relates to new pyrrolidinone inhibitors of PDE-4 activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention relates to 5-HT6 receptor modulators. Compositions comprising arylamine compounds and acetylcholinesterase inhibitors and use of these compositions are disclosed. Such uses include e.g., the treatment, modulation and/or prevention of Alzheimer's disease and memory disorders, and psychological disorders such as schizophrenia, are disclosed.

Abstract: The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.

Abstract: The present invention relates to metabolites of (thio)carbamoyl cyclohexane derivatives, particularly, metabolites of trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimemylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing the same and to their use in the treatment and/or prevention of a conditions which requires modulation of dopamine receptors.

Abstract: The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

Abstract: The invention provides a novel class of cyclic oximes of Formula I: wherein A, X, Y, Z, W, R1, R2, R3 and n are as described in the summary of the invention; useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

Abstract: The present invention relates to an active substance combination comprising at least one compound with 5-HT6 receptor affinity, and at least one cholinesterase inhibitor, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament.

Abstract: Crystalline base of compound trans-1-(1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, processes for the preparation of purified free base or salts of this compound, pharmaceutical compositions comprising the base and medical use thereof, including for treatment of schizophrenia and other psychotic disorders.

Abstract: The present invention relates to new dopamine D3 and D2 and serotonin 5-HT1A receptor subtype preferring ligands of formula (I); wherein A represents alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or a group of formula —NR1R2, wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, alkenyl, aryl, heteroaryl or cycloalkyl or R1 and R2 form with the adjacent nitrogen atom and optionally with further heteroatom(s) a heterocyclic ring; m is an integer of 0 to 1; n is an integer of 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmacological compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine and/or 5-HT1A receptors.

Abstract: A compound represented by the general formula (I): wherein R1 is wherein R26 and R28 are each independently lower alkyloxy and the like; n1 is an integer of 0 to 3; Z is a optionally substituted C1-C5 alkynylene which may be interrupted with a substituent selected from Substituent group a and the like; A is a group represented by the formula: wherein R6 and R7 are each independently lower alkyl and the like; m and n are each independently 0, 1, or 2; R2 is a hydrogen atom and the like; R3 is optionally substituted lower alkyl and the like; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxyl and the like, or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof.

Abstract: Provided herein are methods of treating gastrointestinal motility disorders by targeting the dopamine 3 receptor (D3R). A D3R agonist is administered to a subject to decrease gastrointestinal motility to treat the disorder. A D3R antagonist is administered to a subject to decrease gastrointestinal motility to treat the disorder.

Abstract: The present invention provides a pharmaceutical composition comprising a combination of an Hsp 90 family protein inhibitor and at least one compound, the said pharmaceutical composition wherein the Hsp 90 family protein inhibitor is a benozoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl, or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like], or a prodrug thereof; or a pharmaceutically acceptable salt thereof, and the like.

Abstract: Amphiphilic monomeric compounds and corresponding homopolymers and copolymers capable of assembly and invertible configuration in introduction to and change in fluid medium.

Abstract: A catecholamine or related compound of formula (I) having (S)-configuration at ?-carbon and having a lipophilicity greater than (S)-noradrenalme, a physiologically tolerated salt thereof, a prodrug thereof, a physiologically functional derivative thereof or any mixture thereof is useful as an anti-angiogemc agent A catecholamine or related compound of formula (II) in which a ?-hydroxy group has been modified is also anti-angiogemc

Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.

Abstract: A family of structurally rigid dopamine D3 receptor selective ligands is described. The family of structurally rigid dopamine D3 receptor selective ligands has the formula wherein A is cis or trans —CH?CH—, —C?C—, or cyclohexyl. B is cis or trans —CH?CH— or absent. R1 represents an optionally substituted phenyl group, wherein said substituents are selected from the group consisting of: hydrogen, halogen, amino, nitro, hydroxyl, alkoxy, alkyl, acyl and pyridyl, and said substitution may occur at any of the ortho, meta, or para positions, or R1 represents a heteroaromatic ring. A preferred heteroaromatic ring is indole, quinoxoline, pyridyl, pyrimidyl, or imidazole. R2 and R3 may be independently hydrogen or a halogen, or R2 alone may be C1, C2, or C3 alkoxy, and m is 1 or 2, and n is 0, 1, or 2.

Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.

Abstract: Disclosed herein are a new phenylacetate derivative represented by Chemical Formula 1 or pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for prevention or treatment of diseases induced by the activation of T-type calcium ion channels containing the same. The composition containing the phenylacetate derivative according to the present invention effectively inhibits the activation of T-type calcium ion channels and may be useful in the prevention or treatment of diseases such as hypertension, cancer, epilepsy, and neurogenic pains induced by the activation of T-type calcium ion channels. wherein, X, R1, and R3 are as defined herein.

Abstract: Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R1, R2, R3 and R4 represent hydrogen atom, a halogen atom, cyano group, nitro group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R5 represents a halogen atom, cyano group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R6 represents a C5-7 cycloalkyl group, a substituted C5-7 cycloalkyl group, a 5 to 7-membered completely saturated heterocyclic group or a substituted 5 to 7-membered completely saturated heterocyclic group, X represents a single bond, oxygen atom, sulfur atom, NR7, —O—CH2— or —N(R8)—CH2—, R7 represents hydrogen atom or a C1-4 alkyl group, or R7 may combine with a substituent of R6 to represent a single bond, methylene group or ethylene group, R8 represents hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group, which is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of diseases caused by an activation of

Abstract: The application discloses compounds that inhibit ubiquitin ligase activity. The application further discloses antiviral compounds, anticancer compounds, and compounds useful for the treatment of neurological disorders.

Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.

Abstract: The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.

Abstract: Crystalline base of compound trans-1-((1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, processes for the preparation of purified free base or salts of this compound, pharmaceutical compositions comprising the base and medical use thereof, including for treatment of schizophrenia and other psychotic disorders.

Abstract: The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein the symbols have meaning as defined, which are antagonists of CCR-1 and which find use pharmaceutically for treatment of diseases and conditions in which CCR-1 is implicated, e.g. inflammatory diseases.

Abstract: The present invention provides a novel salt form or solvate of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid. The present invention provides 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid hydrochloride, calcium 5-methyl-2-(piperazin-1-yl)benzenesulfonate and 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid 2,2,2-tetrafluoroethanolate.

Abstract: It is provided a liquid preparation stably including (2S)-1-(4-amino-2,3,5-trimethylphenoxy)-3-{4-[4-(4-fluorobenzyl)phenyl]-1-piperazinyl}-2-propanol or its pharmaceutically acceptable salt as an active ingredient. The present invention relates to a liquid preparation including the above compound or its pharmaceutically acceptable salt as an active ingredient, the liquid preparation including: (a) at least one selected from the group consisting of sulfite, bisulfite, pyrosulfite, ?-thioglycerol and cysteine, (b) a ?-cyclodextrin derivative, and (c) a pH buffer, wherein the pH value thereof is adjusted within a range of from 3 to 5.

Abstract: A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.

Abstract: The invention provides compounds formulae I-III, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.

Abstract: Methods of treating or preventing a disease or disorder in a subject are provided by the present invention which include administering a composition including a therapeutically effective amount of a protein kinase C (PKC) zeta inhibitor. A disease or disorder treated or prevented by administration of a PKC zeta inhibitor is characterized by abnormal vascular permeability. Diseases or disorders treated or prevented by administration of a composition including a therapeutically effective amount of a PKC zeta inhibitor include cancer, an ischemic condition and microvascular complications of a systemic or local condition in the subject, such as diabetes and/or diabetic macular edema. Additionally, methods of inhibiting PKC zeta are provided which include incubating PKC zeta in vivo, in vitro and/or in silico with a PKC zeta inhibitor.

Abstract: This invention relates to inhibiting 11?HSD1.

Abstract: The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal.

Abstract: The present invention relates to a novel piperazine derivative or pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition for treating central nervous system diseases comprising an effective amount of the piperazine compound and a method of treating central nervous system (CNS) disorder such as psychosis in a mammal.

Abstract: The invention relates to methods for the treatment of a sleep disorder in a mammal comprising administering to said mammal an effective amount of a compound of formula (I): wherein all variables are as defined herein.

Abstract: The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.

Abstract: Novel immune potentiators, novel vaccine adjuvants, novel compounds and pharmaceutical compositions, as well as novel methods for treating viral infections, including HCV, by administering the compounds and compositions, and novel methods for modulating the immune response by administering the compounds and/or compositions.

Abstract: Methods of treating cancer using compounds according to Formula (I) are disclosed herein, wherein X, X1, X2, Ra, R1, R2, R3, R4, R5, R6, R7, g, M, y, a, b, d, e, V, W, Z and Q are as defined herein.

Abstract: A method for treating a neurodegenerative disorder. The method includes administering to a subject in need thereof an effective amount of one or more thiourea compounds of formula (I) or (II): Each variable in formula (I) or (II) is defined herein. Also disclosed is use of these thiourea compounds to reduce microglia-mediated neuro-inflammation or enhancing microglial phagocytosis of A?.

Abstract: The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists.

Abstract: This invention relates to the use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases.