Abstract: The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.

Abstract: The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.

Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

Abstract: The present invention relates to 2-isopropoxy-5-methyl-4-(piperidin-4-yl) aniline dihydrochloride monohydrate and a preparation method of the same. The 2-isopropoxy-5-methyl-4-(piperidin-4-yl) aniline dihydrochloride monohydrate has a very good crystal form and is well suitable for recrystallization purification; further, the effect of impurity removal effect is very good, and any single impurity can be controlled less than 0.1%.

Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

Abstract: A compound of formula (I) wherein A, p, R1, R3, R4, R5, R6, m, R7, n and R8 are as defined in claim 1. Furthermore, the present invention relates to intermediates used to prepare compounds of formula (I), to methods of using them to combat and control insect, acarine, nematode and mollusc pests and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.

Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.

Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.

Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

Abstract: An aqueous solution containing 0.1-20 wt % of a cyclic ammonium hydroxide is a useful developer for photosensitive resist materials. A resist pattern is formed by applying a chemically amplified positive resist composition onto a substrate to form a resist film, exposing the resist film to high-energy radiation, and developing the exposed resist film in a cyclic ammonium hydroxide-containing aqueous solution.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract: Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor is represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent.

Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).

Abstract: 4-Fluoro-4-phenylpiperidin-1-yl ? antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.

Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.

Abstract: Provided herein are methods of restoring vitamin D sensitivity in tumor cells that are vitamin D resistant. Also provided are methods of treating, preventing or managing cancer using an immunomodulatory compound in combination with a vitamin D agent. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.

Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X, Y and Q are each as defined in the description, and agrochemically active salts thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).

Abstract: A process is described for preparing aromatic and heteroaromatic amines of the general formula (I) Ar—NR1R2, in which an aromatic compound with the general formula (II) Ar—X is reacted in the presence of a catalyst with an amine of the general formula (III) H—NR1R2 and a base, wherein the catalyst is selected from transition metal complexes having one or more ligands with the general formula (IV).

Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.

Abstract: The present invention relates to a compound represented by formula 1 in the present specification or a pharmaceutically acceptable thereof, which inhibits an apoptosis mechanism of auditory hair cells for various ototoxicities leading to deafness, and protects the auditory organ and hearing, a method for preparation thereof, and a composition containing the same.

Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.

Abstract: There is provided a process for producing an aminopropyne or an enaminone comprising the step of reacting a metal acetylide, an amine and a carbonyl-containing compound in the presence of a transition metal catalyst. There is also provided a process for producing an aminopropyne comprising the step of reacting a metal acetylide, an amine and a halide-containing compound in the presence of a transition metal catalyst at a reaction temperature of 50° C. to 150° C. There are also provided processes to further synthesize the aminopropyne produced to obtain a butyneamine, another aminopropyne or a triazol.

Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of hypertrophic cardiomyopathy, as well as to a method of treating HCM, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said HCM. The invention further relates to a treatment programme for treating HCM, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HCM or the symptoms thereof.

Abstract: The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.

Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.

Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.

Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.

Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.

Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.

Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.

Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize aryl alcohol derivatives as cross-coupling partners. Embodiments of the invention include methods for the amination of aryl sulfamates and carbamates, which are attractive cross-coupling partners, particularly for use in multistep synthesis. Illustrative embodiments include versatile means to use simple derivatives of phenol as precursors to polysubstituted aryl amines, as exemplified by a concise synthesis of the antibacterial drug linezolid.

Abstract: The invention relates to palladium(0)-tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.

Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.

Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

Abstract: The present invention relates to compounds having therapeutic effects against disorders in the central nervous system, and in particular substituted phenylpiperidines of the formula 1: wherein R is as defined herein.

Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.

Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

Abstract: The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).

Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of HfnEF, as well as to a method of treating HfnEF, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said HFnEF. The invention further relates to a treatment program for treating HFnEF, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HFnEF or the symptoms thereof.

Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.

Abstract: The subject matter of the invention is compounds corresponding to formula (I), in which: R1 and R2, together with the nitrogen atom to which they are attached, constitute a saturated heterocyclic radical containing from 4 to 7 atoms, which is preferably substituted; one of the two substituents R3 and R6 is a group Y-A-R9; Y is an oxygen atom or an —S(O)n?—, or —OSO2 group; A is an unsubstituted (C1-C4) alkylene group; R9 is an —OR19, —CH3, —NR19R20, —CONR19R20, —NR15COR19, —S(O)nR21, or —NR13SO2R21 group; —R10 is a hydrogen atom or a (C1-C4) alkyl group. The present invention also relates to the methods of preparation and the therapeutic uses of the compounds of formula (I).

Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

Abstract: 4-Fluoro-4-phenylpiperidin-1-yl ? antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.

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

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 application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Abstract: A compound of the structure wherein R1 and R2 are each, independently, hydrogen or —CO(CR3R4)b(CR5R6)dCR7R8R9; R3 and R4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or —F; R5 and R6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4)fOR10, —CF3, —F, or —CO2R11, or R5 and R6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with —(CR3R4)fOR10; R7 is hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4-)fOR10, —CF3, —F, or CO2R11; R8 and R9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4)fOR10, —CF3, —F, or —CO2R11, or R8 and R9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with —(CR3R4-)fOR10; R10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl; R11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl; X is