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

Abstract: In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.

Abstract: The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.

Abstract: The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and R4 and R6, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.

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: N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.

Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.

Abstract: The present invention relates to new benzoic acid inhibitors of ATP-sensitive potassium channel activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

Abstract: The present invention provides crystalline forms of fentanyl alkaloid and methods for preparing crystalline forms of fentanyl alkaloid.

Abstract: A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3.

Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Abstract: Compounds of formula (I) and salts and solvates are provided: wherein R2 is selected from phenyl substituted with n R1 groups, and pyridyl substituted with n R1 groups; n=0, 1 or 2; each R1 is independently selected from the group consisting of halo, C1-4alkyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy and cyano; R3 is selected from hydrogen and C1-2 alkyl; R4 is selected from the group consisting of ethyl, n-propyl, i-propyl, n-butyl, i-butyl and t-butyl; or R3 and R4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring optionally substituted with one or more groups X; each X is independently selected from the group consisting of C1-4alkyl, and haloC1-4alkyl; R12 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl and methylthio; R13 is selected from hydrogen, chloro and trifluoromethyl; R14 is selected from hydrogen, trifluoromethyl and chloro; R15 is selected from hydrogen, chloro and trifluoromethyl; R16 is selected

Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.

Abstract: The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.

Abstract: The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.

Abstract: The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and R4 and R6, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.

Abstract: The present application describes deuterium-enriched alvimopan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present application describes deuterium-enriched saredutant, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: N-Benzoyl arylsulfonamides having the formula are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).

Abstract: The present invention is directed to compounds of formula I compositions comprising them and their use.

Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.

Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compounds of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject.

Abstract: The present invention relates to salts of aryl compounds as discussed below and to methods of manufacture thereof, as well as other subject matter. More particularly, the invention relates to salts useful as intermediates for the synthesis of the cinnamanilide of formula (Y): where Ra is selected from H, OH, C1, C2, C3 or C4 alkyl; and R1 is C1, C2, C3 or C4 alkyl.

Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [ao] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and s stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q? stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.

Abstract: The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. Said compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use.

Abstract: The invention concerns benzamide compounds of formula (I), wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).

Abstract: Compounds of Formula: wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

Abstract: Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of thrombotic disorders.

Abstract: Described herein is an improved, commercially viable and industrially advantageous process for the preparation of Repaglinide intermediate, ethyl (S)-2-ethoxy-4-[N-(1-(2-piperidino-phenyl)-3-methyl-1-butyl)-aminocarbonylmethyl]-benzoate. The process provides the Repaglinide intermediate in higher yield and purity compared to the previously disclosed processes, thereby providing for production of Repaglinide and its pharmaceutically acceptable salts in high purity and in high yield.

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: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

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: The present invention discloses and claims a compound of general formula (I) wherein A, X and R2 are as described herein. Also disclosed and claimed is application of this compound in a variety of therapeutic applications.

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: This invention relates to organic compounds of formula I, in which Ar1 is unsubstituted phenyl substituted by one or more halogen atoms; Ar2 is unsubstituted phenyl or phenyl substituted by one or more substituents selected from the group consisting of halogen, cyano and C1-C8-alkoxy; R1 is hydrogen or methyl optionally substituted by hydroxy; R10 is hydrogen or hydroxy; and pharmaceutically acceptable salts thereof. Compositions containing them, methods for their preparation and their use as pharmaceuticals are also described.

Abstract: Novel antagonists of ?4?1 integrin and/or ?4?7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.

Abstract: This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.