Abstract: A compound which can be attached to a solid support and used as a reagent for methods of solid phase synthesis has the following structure: (I) where Ri is selected from hydrogen and C1-C6 alkyl; R2 is selected from hydrogen, hydroxy, and C1-C6 alkoxy, or together R1 and R2 form a single bond; R3, R4, R5 and R6 are the same or different from each other and each represents hydrogen, C1-C6 alkyl, and halogen, or together R3 and R4 with R5 and R6 form an aromatic ring, further wherein the aromatic ring is substituted with one or more X; X is selected from halogen, nitro, amino, and aminocarbonyl; s is 0, 1, 2, or 3, t is 0, 1, 2, or 3, wherein s+t?1; R7 and R8 are the same or different from each other and each represents hydroxy, halogen, hydrogen, C1-C6 alkoxy, oxyacyl, or together R7 and R8 form a carbonyl; Y is selected from a methylene or substituted methylene, nucleoside, nucleotide, protected nucleoside, protected nucleotide, C1-C6 aryl, arylalkyl, heteroalkyl, heterocycle, and heteroaryl; n is 1, 2, 3, 4,

Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: New bicyclic derivatives of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.

Abstract: A crystalline form of N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzenesulfonamide having a diffraction peak at a diffraction angle (2?±0.2°) of 19.1° in a powder X-ray diffraction.

Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbylamino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.

Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.

Abstract: The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.

Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I), a method for the production of these compounds, pharmaceutical compositions containing them, and methods of using them for the prevention and/or treatment of various diseases.

Abstract: Imidoalkancarboxylic acids of formula (I) are described, wherein A, X and M are as defined in the application, said acids being in a crystalline form which in contact with water gives rise to crystals having sizes lower than 30 micron.

Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C?O, C?S, S?O, SO2, S, O, (CR6R7)n, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.

Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.

Abstract: This invention generally relates to muscarinic receptor antagonists of formula (I) which are useful, among other uses for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.

Abstract: The invention relates to the use of carboxyamine compounds and salts thereof in the treatment of HDAC dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.

Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4, X5, R4, and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.

Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).

Abstract: The present invention relates to multifunctional ?-agonist compounds comprising a reactive oxygen species scavenger group and a nitric oxide donor, and their use for the treatment of respiratory diseases involving airway obstruction, such as asthma and chronic bronchitis. The invention further relates to methods and devices for administering the compounds.

Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.

Abstract: The present invention relates to spirobenzofuran lactam derivatives of the formula I which are formed during fermentation by the microorganism Stachybotris atra ST002348, DSM 14952, processes for their preparation, their use as pharmaceuticals, and the microorganism Stachybotris atra ST002348, DSM 14952.

Abstract: Prodrugs of glycogen phosphorylase inhibiting compounds are provided which are useful in treating diabetes, having the formula I G(—O2CR?)m(—OH)n(—O2C(CH2)pCH3)qI wherein G is a C3 to C5 branched or straight carbon chain and (—O2CR?), (—OH) and (—O2C(CH2)pCH3) are attached to any available carbon atom along G; —O2CR? is a fragment of a compound of formula Ib where W is a bicyclic heteroaryl; m, n, p, q, X, Y, Z, R1 and R2 are as defined herein, as exemplified by Further provided are pharmaceutical compositions and methods for treating diabetes and related diseases employing the above compounds above, either alone or in combination with another therapeutic agent.

Abstract: Disclosed is a compound represented by Structural Formula (I): R1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstituted aryl group. Z1 is ?O, ?S, ?NOR11. R is represented by a Structural Formula selected from (II)–(VII): The variables in Structural Formulas (II)–(VII) are described herein.

Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors.

Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

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: Novel 4-Biarylbutyric and 5-Biarylpentanoic Acid Derivatives, use of substituted 4-Biarylbutyric and 5-Biarylpentanoic Acid Derivatives as Matrix Metalloprotease Inhibitors for the Treatment of Respiratory Diseases, pharmaceutical compositions containing them, and a process for using them. The compounds of the invention have the generalized formula (I) (T)xA—B—D—E—CO2H wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group, x is 0, 1, or 2; the group D represents (a), (b), (c), or (d); the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.

Abstract: 2,3-Dihydro-isoindol-1-one derivatives, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them, for the prevention and treatment of diseases which are mediated by monoamine oxidase B.

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

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Novel 3-(2-aminopropyl)-H-indol-5-ols useful for lowering and controlling IOP and treating glaucoma are disclosed.

Abstract: A compound of formula [I]:

Abstract: There is provided a series of novel &agr;-(N-sulfonamido)acetamide compounds of the Formula (I) 1

Abstract: Disclosed is a compound represented by Structural Formula (I): R1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstituted aryl group. Z1 is ═O, ═S, ═NOR11, or ═NR11. R is represented by a Structural Formula selected from (II)-(VII): The variables in Structural Formulas (II)-(VII) are described below.

Abstract: Compounds of Formula (I) 1

Abstract: The present application describes aryl sulfonyls of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein D, E, and M are defined below, are effective factor Xa inhibitors.

Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.

Abstract: The present invention relates to novel aromatic amines of general formula (I) and to the use of these amines for the treatment of obesity, anorexia, inflammation, mental disorders an other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.

Abstract: A novel calcium receptor active compound having the formula is provided:

Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.

Abstract: An amine ether of formula (A) wherein a is 1 or 2; and when a is 1, E is E′; when a is 2, E is L; E′ is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cycloalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or bricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E′ is a radical of formula (VII) as explained in claim 1; T′ is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)—R22; or T′ is C5-C12cycloalkyl; C5-C12cacloalkyl which is interrupted by at least one O or —NR18—; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or —NR18—; or T′ is —C(G1)(G2)—T″; or C1-C18alkyl or C5-C12cycloalkyl substituted by F(I)T″ is hydrogen, halogen, NO2, cyano,

Abstract: Anionic polymerization initiators useful in the preparation of polymers having a protected amine functional group. The amine functionality includes a first protecting group, which can be aralkyl, methyl, allyl or tertiary alkyl group. The other of the amine protecting groups can be the same as the first protecting group. Alternatively, the second protecting group can be different from the first protecting group, in which case it is selected to have differential stability to agents used to remove the aralkyl, methyl, allyl or tertiary alkyl protecting group.

Abstract: Oompounds of formula (I), wherein R2 represents a hydrogen atom or a C1-4 alkyl group; q is 1 or 2; A represents a group of formula (a), (b), (c) or (d), wherein Ar represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; or an optionally substituted bicyclic ring system; Ar1 and Ar2 each independently represent an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; and Y represents a bond, —NHCO—, —CONH—, —CH2—, or —(CH2)mY1(CH2)n—, wherein Y1 represents O, S, SO2 or CO and m and n each represent zero or (I) such that the sum of m+n is zero or 1; providing that when A represents a group of formula (a), any substituent present in Ar ortho to the carboxamide moiety is necessarily a hydrogen or methoxy group; r and s independently represent an integer from zero to 3 such that the sum of r and s is equal to an integer from 1 to 4; V repres

Abstract: Anionic polymerization initiators useful in the preparation of polymers having a protected amine functional group. The amine functionality includes a first protecting group, which can be aralkyl, methyl, allyl or tertiary alkyl group. The other of the amine protecting groups can be the same as the first protecting group. Alternatively, the second protecting group can be different from the first protecting group, in which case it is selected to have differential stability to agents used to remove the aralkyl, methyl, allyl or tertiary alkyl protecting group.

Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Orohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.

Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.