Abstract: The present invention provides 2-aryl or heteroaryl indole derivatives which are ASIC channel modulators, maceutical compositions containing such compounds, and methods of using them as therapeutic agents.

Abstract: A hydrophobic binding pocket on ubiquitin-protein ligase E3 is described, and used in designing the inhibitors disrupting ubiquitin conjugating enzyme E2 and E3 interaction. Four types of inhibitors designed by using the binding pocket are provided, which can be used for cancer treatment.

Abstract: The invention relates to 4-substituted 1-aminocyclohexane corresponding to formula (I) to a method for the production thereof, to pharmaceutical formulations containing these compounds and to the utilization of 4-substituted 1-aminocyclohexane compounds for the production of pharmaceutical formulations and related methods of treatment.

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: Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.

Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.

Abstract: The indolium compounds of the present invention are represented by general formula (I) below and exhibit thermal decomposition behavior further suitable for optical recording materials used in an optical recording layer of an optical recording medium for high-speed recording.

Abstract: There are described Compounds of formula (I) in which R3 to R8 are independently selected from hydrogen, halogen, trihaloalkyl, alkyl having 1, 2, 3, 4 or 5 carbon atoms, electron donor groups selected from alkoxy having 1, 2, 3, 4 or 5 carbon atoms, trihaloalkoxy, hydroxy or amino, electron acceptor groups selected from cyano, sulphonic, nitro, or amide; R1 is an optionally substituted phenyl, benzyl or cyclohexyl group; R2 is selected from amino, substituted amino or guanidino groups, Z is a saturated or unsaturated C1-5 hydrocarbon chain, and salts thereof. A process for their preparation and compositions containing them are also described. The Compounds are either agonists or antagonists of a specific adenosine receptor or a number of adenosine receptors and have usefulness for the treatment of inflammation, arthritic conditions, rheumatoid arthritis, Osteoarthritis, mental disorders, or for inducing central nerve regeneration.

Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: Multi-ligand capture agents comprising two or more ligands are described, and related compositions, methods and systems.

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: The invention provides novel indane compounds which are useful in the treatment of affective disorders, pain disorders, attention deficit hyperactivity disorder (ADHD), cognitive disorders, substance abuse, smoking cessation and stress urinary incontinence.

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: A process for making the compound of formula (I) wherein Ac represents acetate; X represents O or CH2; Y represents C1-C6alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF3, OCF3, OH, C1-C6alkyl, C1-C6alkoxy, C1-C6thioalkyl, NH2, N(C1-C6alkyl)2, NH(C1-C6alkyl), NC(O)—(C1C6alkyl), and NO2. In his process, a compound of formula (II) is reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).

Abstract: Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.

Abstract: Compounds of formula I their manufacture, pharmaceutical compositions containing them and their use as medicaments.

Abstract: Polymorphic forms of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide free base and salts thereof are prepared by various processes.

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

Abstract: A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like. A compound of the formula (I): wherein a group represented by the formula: is a group represented by the formula: and the like, R1 is carboxy and the like, R3 is —(CH2)n-N(—Y)—SO2—Ar and the like, the other symbols are as defined in claim 1.

Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.

Abstract: 4-alkyl/4-alkenyl/4-alkynyl methyl/-1-arylcyclohexylamine compounds corresponding to the formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them to treat or inhibit pain or other specified conditions associated with the ORL1 receptor.

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

Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.

Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.

Abstract: The present invention provides novel biocompatible macromonomers, hydrogels, methods of synthesis and methods of use thereof. The biocompatible hydrogels of the present invention are prepared using native chemical ligation (NCL), in which a thioester readily reacts with a N-terminal thiol (cysteine) through transesterification and rearrangement to form an amide bond through a five-member ring intermediate.

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 relates to single and dual reporter luminescence assays utilizing reagents to quench an optical, e.g., an enzyme-mediated luminescence, reaction. In one embodiment of the invention, a reagent is added to an assay which selectively quenches a first enzyme-mediated luminescence reaction without affecting a subsequent distinct enzyme-mediated luminescent reaction(s). An assay kit containing one or more selective quench reagents, and compositions comprising the quench reagent(s), are also provided.

Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.

Abstract: The invention relates to a combination which comprises (a) a cyclooxygenase-2 inhibitor (“COX-2 inhibitor”) and (b) a histone deacetylase inhibitor (“HDAI”) for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of pre-malignant colon lesions or a colon cancer or other malignancies in a mammal, particularly a human. The invention also relates to pharmaceutical compositions comprising such a combination and to a method of treating pre-malignant colon lesions (e.g. polyps) and colon cancer, as well as other malignancies, in a mammal, particularly a human, with such a combination. The present invention further also relates to a commercial package or product comprising such a combination.

Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.

Abstract: The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxyl

Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.

Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.

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

Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.

Abstract: The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: useful as inhibitors of PHEX. These derivatives are useful for promoting generation of bone mass and treating or preventing diseases or conditions associated with a phosphate metabolism defect. Methods for preparation and intermediates are also disclosed.

Abstract: This invention is in the area of phenylindoles that are useful for the treatment of HIV infection, and, in particular, phenylindoles that exhibit significant activity against resistant strains of HIV. The phenylindoles have at least two substituents other than hydrogen on the benzo ring of the indole function, preferably at the 4? and 5?, 5? and 6? or the 5? and 7? positions, optionally in combination with disubstitution at positions 3? and 5? on the phenyl ring of the compound, and carboxamide containing moieties at position-2 on the indole group of the compound. Methyl is a preferred group for substitution on the phenyl ring. Preferred substituents for the benzo ring of the indole function include but are not limited to chlorine, fluorine, bromine, iodine, CF3, methoxy, CN, and NO2.

Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where A, B, and R1-R3 are defined herein.

Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

Abstract: Compounds of formula I their manufacture, pharmaceutical compositions containing them and their use as medicaments.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R1, R2 and R3 are each independently selected from OH, C1-6alkyl, OC1-6alkyl, OC(O)C1-6alkyl, C(O)OC1-6alkyl, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), C(O)NHC1-6alkyl, C(O)N(C1-6alkyl)(C1-6alkyl), SH, SC1-6alkyl, NO2, CF3, OCF3 and halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1–4 substituents independently selected from OH, C1-6alkyl, C1-6alkoxy, C1-3alkylenedioxy, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6)(C1-6alkyl), SH, S—C1-6alkyl, NO2, CF3, OCF3 and halogen. The compounds of Formula I are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.

Abstract: The invention relates to derivatives of indole-3-carboxamide having general formula (I): wherein: R1 represents a C3–C10 alkyl, a C5–C10 carbocyclic radical that is unsubstituted or substituted one or more times with a methyl group; R2 represents a hydrogen atom or a (C1–C4)alkyl group; R3 represents a halogen atom or a (C1–C4)alkyl group; R4 represents a hydrogen or halogen atom or a (C1–C4)alkyl group; R5 represents a (C1–C4)alkyl group or a trifluoromethyl; X represents a sulfur atom, an —NHSO2— group or an —SO2— group; and n is equal to 2 or 3. The invention also relates to a method of preparing the aforementioned derivatives and to the application of same in therapeutics.

Abstract: The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with 5-HT6 receptors, including schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders selected from the group consisting of age-related cognitive decline, mild cognitive impairment, and dementia, comprising: administering to a patient in need thereof an effective amount of a compound of formula I.

Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: The present invention provides a method for making substituted indole compounds of general formula III comprising the step of: (a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I) (I) wherein: X, R and R1 are defined herein with a substituted acetylene of formula (II) wherein R2 and R3 are defined herein in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III);

Abstract: Compounds useful as inhibitors of cyclooxygenase-2 activity have the formulae I or Ia: wherein: Q1, Q2, n, m, X, Y and R are as defined herein.

Abstract: Methods for identifying MarR family inhibiting compounds are described. The methods include the use of computer aided rational based drug design programs and three dimensional structures of MarR family polypeptides.