Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.

Abstract: There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R25, R26 and R27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Abstract: Substituted pyrazoles of general formula methods of manufacturing them, compositions containing them, and methods of using them to, for example, treat autoimmune diseases mediated by cathepsin S, and inhibit cathepsin S activity, are described.

Abstract: This invention provides compounds which are represented by a general formula [I] [in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower alkyl; D stands for a 3–10 membered aliphatic nitrogen-containing heterocyclic group; R3, R4 and R5 may be same or different, and each stands for hydrogen, lower alkyl optionally having substituent group(s) and the like; and a is 0 or 1]. These compounds exhibit high affinity to nociceptin receptors and whereby inhibit actions of nociceptin, and are useful as an analgesic, antiobestic, agent for ameliorating brain function, treating agents for Alzheimer's disease and dementia, and therapeutic agents for schizophrenia, neurodegenerative diseases, depression, diabetes insipidus, polyuria, hypotension and the like.

Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.

Abstract: The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.

Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.

Abstract: The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.

Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor

Abstract: This invention relates to novel tetrazolyl-propionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby resulting in prevention and treatment of the neuropathology associated with production of A?-peptide. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease.

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.

Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recit

Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.

Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems re

Abstract: This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R?, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.

Abstract: Compounds according to formula (I) wherein n is 0-3, R′ is optionally substituted C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from hydrogen and optionally substituted C1-6 alkyl, or R5 and R8 are an alkylene chain, are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.

Abstract: The invention provides compounds having the imidazole, oxazole, or thiazole skeleton and uses thereof. The compounds described herein bind to phosphodiesterase 6D. The compounds disclosed herein can be used to modulate the activity of phosphodiesterase 6. The invention provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects. Kits comprising the compounds of the invention are also provided.

Abstract: The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives.

Abstract: The present invention relates to a compound of the formula I 1

Abstract: Compounds of the present invention modulate PN3 in mammals and are useful in treating pain in mammals.

Abstract: This invention relates to substituted imidazoles of Formula I 1

Abstract: The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: The present invention provides medicinal compositions characterized by comprising as the active ingredient either a compound represented by a formula [I] or a pharmaceutically acceptable composite thereof; 1

Abstract: Benzotriazoles of formula I 1

Abstract: This invention relates to novel tetrazolylpropionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I): 1

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: This invention relates to extended dosing regimens for the selective estrogen receptor modulator bazedoxefine (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1 H-indol-5-ol).

Abstract: This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

Abstract: The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.

Abstract: Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cy

Abstract: Compounds having the formula 1

Abstract: Aryl substituted 1,4-diazepanes are provided such as derivatives of 6-(1,4-diazepan-1-yl)benzo[cd]indol-2(1H)-one, 6-(1,4-diazepan-1-yl)acenaphthylen-1(2H)-one and 5-(1,4-diazepan-1-yl)-2H-naphtho[1,8-cd]isothiazole-1,1-dioxide. Also provided are pharmaceutical compositions containing one or more of the aryl substituted 1,4-diazepanes. The aryl substituted 1,4-diazepanes are useful for treating disorders or deficiencies associated with the 5-HT2C receptor.

Abstract: Disclosed are compounds of the formula: 1

Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: 1

Abstract: This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.

Abstract: Compounds according to formula (I) wherein n is 1-4, R1 is optionally substituted C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7 and R8 are each independently selected from hydrogen and optionally substituted C1-6 alkyl are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.

Abstract: Compounds of formula (I) wherein Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered hereroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R5 represents an optionally s

Abstract: This invention relates to novel N-heterocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.

Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.

Abstract: The present invention relates to compounds of formula: 1

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: The invention concerns benzimidazole derivatives of the general formula (I) 1

Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

Abstract: This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof.