Abstract: Compounds of formula I: modulate the activity of ?-secretase, and hence find use in treatment or prevention of Alzheimer's disease and related conditions.

Abstract: The invention encompasses the novel compounds of Formula (I) and Formula (II), which are prodrugs that convert in vivo to diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. These prodrugs are far more soluble in aqueous media than the active agents into which they convert, in vivo. As such compounds of Formula (I) and (II) are advantageous for, among other things intravenous administration. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula (I) and Formula (II).

Abstract: The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders—such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to ?2?-1 subunit of Ca channels.

Abstract: Phenyl compounds substituted with a fused-heterobicyclo moiety, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

Abstract: Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

Abstract: 6H-pyrrolo[3,4-d]pyridazine compounds and methods of their use of as ligands of voltage gated calcium channels (VGCC), useful in the treatment of neuropathic pain, and psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other.

Abstract: The present invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a derivative thereof, X is —CO2H, 1H-tetrazol-5-yl or 2H-tetrazol-5-yl and R1 and R2 are each independently selected from the group consisting of: C1-6alkyl and C3-6cycloalkyl, as well as pharmaceutical composition comprising said compounds and methods of using said compounds. The compounds of the present invention lower the level of A?42 and are therefore useful for preventing, delaying or reversing the progression of Alzheimer s Disease.

Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.

Abstract: Phenyl compounds substituted with a fused-heterobicyclo moiety, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

Abstract: Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at 2 the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

Abstract: The present invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, wherein each R1 may be substituted at any substitutable position on A and each R1 is independently selected from the group consisting of: halo, cyano, C1-4alkoxy, C1-4alkylthio and C1-4alkyl, each of said C1-4alkoxy, C1-4alkylthio and C1-4alkyl optionally substituted with 1 to 3 halo groups, R2 is selected from the group consisting of: C1-6alkyl and C3-6cycloalkyl, R3 is selected from the group consisting of: hydrogen, C1-6alkyl and C3-6cycloalkyl and R4 is a nitric oxide releasing moiety. Pharmaceutical composition comprising said compounds and methods of using said compounds are also encompassed. The compounds of the present invention lower the level of A?42 and are therefore useful for treating or preventing Alzheimer's Disease. The compounds of the invention also release nitric oxide in vivo and have a reduced potency for cyclooxygenase activity.

Abstract: Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.

Abstract: Amino acid di- and tri-peptide analogs having C-terminal vinylic groups, pharmaceutical compositions containing the analogs and methods of treating diseases using cysteinyl protease inhibitors; particularly neurodegenerative, autoimmune, cognitive disorders, stroke and traumatic injury.

Abstract: Recombinant cells expressing fluorescence resonance energy transfer reporter polypeptides and cell-based assays for apoptosis; screening assays for identifying and selecting candidate compounds modulating apoptosis.

Abstract: Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.

Abstract: Methods of use of compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds provided for use in the methods are those of the formula: ##STR1## in which R.sub.1 is preferably 2-methylpropenyl, 2-butenyl, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each preferably independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is preferably H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; and X is preferably an aldehyde, .alpha.-ketoester or .alpha.-ketoamide.

Abstract: Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is an alcohol, particularly a secondary alcohol.

Abstract: Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided Among the compounds are those of formulae I and II: ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; --R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is preferably an .alpha.-ketoester or .alpha.-ketoamide or aldehyde.

Abstract: Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is an alcohol, particularly a secondary alcohol.

Abstract: Methods of use of compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds provided for use in the methods are those of the formula: ##STR1## in which R.sub.1 is preferably 2-methylpropenyl, 2-butenyl, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each preferably independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; Q is preferably --C(O)--; R.sub.B is preferably iso-butyl; R.sub.A is --(T).sub.m --(D).sub.m --R.sub.1, in which T is preferably oxygen or NH, m is 0 or 1, and D is preferably C.sub.1-4 alkyl or C.sub.2-4 alkenyl; and X is preferably an aldehyde, .alpha.-ketoester or .alpha.-ketoamide.