Abstract: The present invention relates to novel 2-heteroaryl substituted indole derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted indole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer?s disease therapeutic agents.

Abstract: The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R4, X, Y, Z and m are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

Abstract: 2-Substituted indole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract: The present invention relates to indolone-acetamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as for the treatment of epilepsy, epileptogenesis, seizure disorders and convulsion.

Abstract: Use of a compound corresponding to formula (I) in which R represents hydrogen or a group chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene, cycloalkylidyne and —CONH2 groups, and the —COR? and —COOR? groups, in which R? is chosen from alkyl, alkylene, alkylidyne, cycloalkyl, cycloalkylene and cycloalkylidyne groups, it being possible for said groups R and/or R? to be substituted and/or interrupted with -0-, —COO—, —OCO—, —NHCO— or —CONH— functions, or a pharmaceutically acceptable salt of said compound, for obtaining a medicament for use in the treatment of faecal incontinence.

Abstract: Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(?O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C?O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)-substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)-substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. The 3,4(,5)-substituted tetrahydropyridine compounds have the formula I wherein the substituents and symbols are as described in the specification.

Abstract: The present invention relates to extended benzamide derivatives of the general formula I, to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the EP2 receptor.

Abstract: Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.

Abstract: The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof; wherein X, R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: The invention relates to compounds of formula (I): Wherein X1, X2, X3, X4, Y and W are as described herein. The invention also relates to a preparation method and to a therapeutic application.

Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.

Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.

Abstract: The invention is concerned with vinylogous acids derivatives of formula (I) wherein A and R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.

Abstract: The invention relates to novel amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.

Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.

Abstract: This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Abstract: Compounds of formula (I): wherein: A represents a divalent radical: wherein: Z represents an oxygen atom or a sulphur atom, R6 represents a hydrogen atom, an alkyl, alkenyl, arylalkyl or polyhaloalkyl group or a substituted, linear or branched alkyl chain, represents a single bond or a double bond, R1, R2, R3 and R4 represent a hydrogen or halogen atom, an alkyl, alkoxy, hydroxy, cyano, nitro, polyhaloalkyl or optionally substituted amino group, or a linear or branched alkyl chain substituted by one or more groups, R5 represents a hydrogen atom or an alkyl, aminoalkyl or hydroxyalkyl group, X and Y represent a hydrogen atom or an alkyl group, Ra, Rb, Rc and Rd represent a hydrogen or halogen atom, an alkyl, hydroxy, alkoxy, cyano, nitro, polyhaloalkyl, optionally substituted amino group, or a substituted, linear or branched alkyl chain, Re represents a hydrogen atom or an alkyl, arylalkyl or alkenyl group or a substituted, linear or branched alkyl chain, their enantiomers, diastereoisomers

Abstract: The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.

Abstract: The invention relates biaryl substituted diazabicycloalkanes, and more particularly bicycloheteroaryl substituted fused diazabicycloalkane derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions.

Abstract: The invention features methods of treating visceral pain or a condition in a mammal caused by the action of nitric oxide synthase (NOS) or by the action of serotonin 5HT1D/1B receptors, by administering to a patient in need thereof a therapeutically effective amount of an indole compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof. The methods of the invention may further comprise the administration of additional therapeutic agent. The invention also features new compounds of Formula (I), pharmaceutical compositions thereof, and methods of resolving enantiomeric mixtures.

Abstract: Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, and —O(CH2)p—O—(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.

Abstract: A 2-arylindole compound substituted in position 5, of formula (I): in which X, Y, Z, W, A, R and R? have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.

Abstract: Compounds of formula (I): wherein: R1 and R2, which may be the same or different, represent a hydrogen atom or a linear or branched (C1-C6)alkyl group, R3 represents a hydrogen or halogen atom, a linear or branched (C1-C6)alkyl group, or a linear or branched (C1-C6)alkoxy group, Het represents a pyridyl, pyrimidinyl or piperidyl group, which are optionally substituted by one or more groups selected from halogen, linear or branched (C1-C6)alkyl and linear or branched (C1-C6)alkoxy, —represents a single bond or a double bond, their enantiomers and diastereoisomers, and also addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of depression, anxiety, disorders of memory in the course of aging and/or neurodegenerative diseases, and in the palliative treatment of Parkinson's disease, and for adaptation to stress.

Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

Abstract: An object of the present invention is to provide a medicament as a thyroid hormone receptor ligand which is sufficient in drug efficacy and safety, and has the excellent action as a drug. The present invention provides a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: [wherein [Chemical Formula 2] is a single bond or a double bond; A is —CH2— or —CO—; X, Y, and Z are each independently a nitrogen atom or a carbon atom; R1 is a hydrogen atom or an aralkyl group; R2 is an alkyl group or an aralkyl group, etc.; R3 is a hydrogen atom or an alkyl group, etc.; R4 is a hydrogen atom or an alkyl group; R5 is a hydrogen atom, an alkyl group or a halo lower alkyl group, etc.; R6 is a hydrogen atom or an alkyl group; R7 is a hydrogen atom, etc.; R8 is a hydrogen atom, or an alkyl group, etc.; and E is —NHCO-G-COR12, etc. (wherein G is a single bond or an alkylene group, and R12 is a hydroxy group or an alkoxy group)].

Abstract: Compounds of formula (1) are described: in which X is an —O— or —S— atom or —N(R2)— group and R1 is a group Ar1L2Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an optionally substituted bicyclic heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH?C(R)—, OR—CH(CH2R)— in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof. The compounds are selective inhibitors of alpha 4 integrins such as ?4?1 and are of use in modulating cell adhesion for the prophylaxis or treatment of inflammatory diseases or disorders, such as rheumatoid arthritis, in which the extravasculation of leukocytes plays a role.

Abstract: The invention provides compounds, pharmaceutical compositions and methods for the therapeutic treatment and prevention of neurodegenerative disorder and other A?42-related diseases and disorders.

Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, A and Z have defined meanings.

Abstract: The present invention relates to 5-substituted indole derivatives of formula (I): having inhibitory potential of dipeptidyl peptidase IV (DPP IV) enzyme where x and R1 are defined as defined in the specification

Abstract: The present invention relates to pyridinyloxy- and pyrimidinyloxyindole derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.

Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.

Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.

Abstract: Indole derivatives that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives. The compounds are substituted at least at the 3 position of the indole.

Abstract: The present invention relates to novel benzoheterocyclylethylcarboxamide derivatives of formula (I) in which the substituents are in the description, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions, methods for the control of phytopathogenic fungi of plants using these compounds or their compositions:

Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.

Abstract: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur.

Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, al

Abstract: The present invention relates to ?-alkyl substituted N-acyltryptophanols of the formula I in which R1, R2, R3, R4, R5, R6, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.

Abstract: The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or —NH—, R1 represents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which R2 and R3 are both hydrogen atoms), and an antifungal agent containing the above compound.

Abstract: Aromatic compounds exemplified by exhibit antimicrobial activity.

Abstract: Crystal form of besipirdine chlorhydrate (Form I) corresponding to the Formula (A) below: the aforementioned form being characterized at least by one of the following physico-chemical properties: a) In FTIR, it displays at least the following absorption bands of the infrared spectrum: 778, 1198, 1121, but not the following absorption bands of the infrared spectrum: 3395, 1583, 732, the aforementioned bands being expressed in cm?1 at ±5 cm?1; b) In PXRD, it shows at least the following reflections, which are the most intense ones but whose intensity hereafter is given for information only: Formula (II) c) In DSC, it displays at least an endothermic peak at 187.3±2.0° C. using 5° C./min scanning conditions, and a fusion enthalpy ?H of 130.4±2.0 J/g. The invention also relates to the processes used for the preparation of form I as well as its applications in urology.

Abstract: The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C1-C4 alkyl, C1-C4 alkoxy group, or the neighboring V and Z groups in given case together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are substituted carbon atom or one of them is nitrogen atom, and the salts thereof.

Abstract: The invention describes novel organic nitric oxide enhancing salts of nonsteroidal antiinflammatory drugs (NSAIDs) and novel compositions comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent.