Abstract: The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR2 wherein R2 is H or C1-C6 alkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5, wherein R4 and R5 are as defined in the specification; and R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined in the specification. The invention further relates to a process for the preparation of the intermediates.

Abstract: The present invention relates to certain N-biaryl and N-arylheteroaryl 2-substituted piperazine derivatives of Formula (Ia) that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2C receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.

Abstract: A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.

Abstract: In one aspect, the present invention provides compounds having formula (1) or (100), a salt thereof or a hydrate of the foregoing, which compounds exhibit excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome; rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.

Abstract: Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided.

Abstract: Disclosed is a method for use of phenyl sulfone compounds of formula (I) in the treatment of anxiety.

Abstract: The present invention relates to compounds of formula I and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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: A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, J, K, W, V, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: The present invention relates to nitro-substituted phenyl-piperazine compounds of general formula I, a process for their preparation, medicaments comprising said nitro-substituted phenyl-piperazine compounds as well as the use of said nitro-substituted phenylpiperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.

Abstract: Disclosed herein are new methods of treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver in a subject by modulating PPAR? with sulfonyl-substituted bicyclic compounds and compositions as pharmaceuticals.

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). Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

Abstract: Described is a method for making the trans-1-((1R,3S)-6-chloro-3-phenylin-dan-1-yl)-3,3-dimethylpiperazine (formula I) and salts thereof and a similar method for making 4-((1R,3S)-6-chloro-3-phenylin-dan-1-yl)-1,2,2-trimethylpiperazine (formula IX) and salts thereof, which method comprises conversion of a compound of formula IVa to the compound of formula I or the compound of formula IX, respectively.

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 the use of at least one inhibitor of at least one ABC-transporter capable of transporting hyaluronan across a lipid bilayer, such as verapamil or valspodar, for the preparation of a pharmaceutical composition for the treatment of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, e.g. arthritis. Furthermore, the present invention relates to a method for screening a compound which is suitable for the treatment of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, e.g. arthritis. The present invention also relates to a method for screening a compound which reduces the transport of hyaluronan mediated by (an) ABC-transporter(s). Furthermore, the present invention relates to a method for identifying a subject at risk for a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, e.g.

Abstract: N,N?-disubstituted piperazine compounds, processes for the production thereof, and pharmaceutical preparations containing these compounds. The use of N,N?-disubstituted piperazine compounds for the production of pharmaceutical preparations and in related methods of treatment.

Abstract: Disclosed are bisbenzamidine and bisbenzamidoxime compounds useful for treatment of treatment of trypanosomiasis. The compounds disclosed are useful for treating mammals infected with parasitic hemoflagellates, in particular Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense.

Abstract: The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Ra, Rb, Rc, Rd, Re, Rf and Y are as defined in the specification. The compounds are partial or full agonists at the growth hormone secretagogue (GHS) receptors. Pharmaceutical compositions comprising the compounds methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.

Abstract: This invention relates to a genus of compounds, represented by the formula (I) diagrammed below, wherein the meanings of R1, R2, R3, R4, R5, R6, R7, R8, D and n are indicated therein, which are inhibitors of cathepsin K. These compounds are useful for treating or preventing atherosclerosis and atherosclerotic cardiovascular disease.

Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.

Abstract: The present invention relates to certain biarylz and arylheteroaryl piperazine derivatives of Formula (Ia) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.

Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.

Abstract: Improved taste masking of pharmaceutical compositions of unpleasant-tasting drugs and cyclodextrin is achieved by forming a mixture of drug and cyclodextrin wherein the drug's dissolution rate has been retarded, or the the cyclodextrin's dissolution rate has been enhanced, or by both.

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

Abstract: The present invention provides novel quaternary amino-functional chalcone derivatives and analogues exhibiting interesting antibacterial activity. The compounds have the general formula (Y1)m—Ar1(X1)—C(=O)VAr2(X2)?(Y2)p (I), wherein V designates —CH2—CH2—, —CH?CH— or —C?C—; Ar1 and Ar2 independently are aryl and heteroaryl; m=0, 1, 2, p=0, 1, 2, m+p>0; each Y1 and Y2 independently is -Z—N+(R1)(R2)R4 Q? (A); —NR3-Z—N+(R1)(R2)R4 Q? (B), or —O-Z—N+(R1)(R2)R4 Q? (C), R1, R2, R3, R4, X1, X2 are substituents, and Q? is an anion. The present invention also relates to the compounds for use as pharmaceutically active agents, in particular against bacterial infections (such as Gram-negative and Gram-positive bacteria, including antibiotic-sensitive or resistant strains), and in the medical treatment of bacterial infections in mammals.

Abstract: The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.

Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system

Abstract: The present invention discloses methods to reduce C-reactive protein (CRP) in patients in need thereof comprising the selective modulation of PPAR?.

Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.

Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.

Abstract: This invention relates to novel phenyl sulfone compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.

Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Abstract: The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. The compounds according to the invention are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.

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 invention relates to compounds of the general Formula (I): The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of Formula (I).

Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.

Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.

Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application.

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said novel 3-heterocyclic benzylamides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.

Abstract: The present invention provides isoeugenol derivative compounds having the moiety and having ?2-adrenergic/5-HT2A antagonist, 5-HT re-uptake inhibition, and anti-oxidant activities.

Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1–C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1–C4 alkyl, C1–C4 alkoxy, alkylthio, hydroxy, amino, mono(C1–C4)alkylamino, di(C1–C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.

Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6

Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.