Abstract: The present invention provides pharmaceutical compositions comprising an allosteric adenosine A1 receptor enhancer, such as T-62, in an oral dosage form and processes for the manufacture of such compositions and dosage forms. In another aspect, the present invention relates to a method of employing such dosage forms for the treatment of pain, including acute pain, e.g., postoperative pain, chronic pain, inflammatory pain, neuropathic pain and pain associated with migraine.

Abstract: The present invention provides a compound of Formula (I): wherein R1, R2, R3 and R4 are each independently selected from a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted C7-C14 aralkyl group and —C(?O)Rx; Rx represents an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C1-C6 alkoxy group or —NReRf; Ar1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents —(CH2)m-(L)p- or -(L)p-(CH2)m—; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents —O—, —S— or —NR5—; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical co

Abstract: The present invention relates to new compounds of formula I. (I) wherein R1 to R12, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.

Abstract: A cannabinoid receptor modulator containing a compound represented by Formula (I0) wherein, X is an oxygen atom, etc., R0 is an optionally substituted acylamino group, ring A0 is a benzene ring which may further have a substituent in addition to R0, and ring B is an optionally substituted 5-membered heterocycle, or a salt thereof or a prodrug thereof.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The present invention provides crystal forms of (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)(4-chlorophenyl)methanone of the formula processes for the production of such crystal forms; pharmaceutical compositions comprising such crystal forms; and methods of treating diseases or conditions modulated by the adenosine A1 receptor, in particular neuropathic pain, in a mammal in need thereof, by employing such crystal forms, or pharmaceutical compositions comprising such.

Abstract: The present invention provides methods of identifying compounds that protect against ototoxicity induced by one or more noxious stimuli, and methods of treating an individual with compounds identified using the present screening methods. Also provided are compounds demonstrated to have otoprotective effects.

Abstract: The present application relates to cannabinoid receptor ligands containing compounds of formula (I) wherein A, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present application refers to the use of mycobacterial protein serine/threonine kinases for developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases.

Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I: methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical formulations and related methods of treating or inhibiting certain diseases or conditions.

Abstract: The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives 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 herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections.

Abstract: The invention relates to the use of novel cyclohexyl analogues of E-type prostaglandins as EP4 agonists, in general, and, in particular as ocular hypotensives. The cyclohexyl analogues used in accordance with the invention are represented by the following formula I: wherein the wavy segments represent ? or ? bond, dashed line represents the presence or absence of a bond W, Y, Z, R, R1, R2 and R3 are as defined in the specification.

Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1-C5) alkyl group, (C2-C5) alkenyl, or a (C2-C5) alkynyl, (C1-C5) alkoxy, (C2-C5) alkenyloxy, or (C2-C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1-C5) alkyl, (C2-C5) alkenyl, or (C2-C5) alkynyl, or a cyclo

Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.

Abstract: The invention provides a glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): wherein m is an integer selected among 1-3; R1 to R4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl, a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.

Abstract: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof useful as Estrogen Receptor beta agonists for treating Estrogen Receptor beta mediated diseases such as benign prostatic hyperplasia.

Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, to their use for the treatment of dyslipidaemia, atherosclerosis and diabetes, to pharmaceutical compositions comprising them and to the processes for the preparation of these compounds.

Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.

Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.

Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: New fused thiophene compounds are provided and methods of using those compounds for a variety of therapeutic indications. Compounds of the invention are particularly useful for treatment of neuropathic pain.

Abstract: The invention provides compounds of formula (I) for use as GLP-1 receptor agonists.

Abstract: The present invention provides methods for identifying a patient at risk for developing AMD by identifying the presence of the Y402H polymorphism or other at risk variants in the complement factor H gene. The present invention further provides methods for treating persons having AMD or at risk for developing AMD as a result of having the Y402H polymorphism or other at risk variants in the complement factor H gene.

Abstract: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.

Abstract: Mammalian hair growth is reduced by applying an inhibitor of telomerase to the skin.

Abstract: The present invention relates to compounds of 2-thia-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-?(TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Abstract: Pharmaceutical formulations containing substituted 2-aryl-aminoacetic acid compounds and/or substituted 2-heteroaryl-aminoacetic acid compounds corresponding to formula I, as well as to their use in the production of drugs and in related methods of treating or inhibiting pain and neurodegenerative disease.

Abstract: A biodegradable, flexible covering for a breast implant is provided which comprises one or more biodegradable polymer layers dimensioned and shaped to cover at least a portion of the breast implant. The implant can be inserted into an opening of the covering immediately prior to surgery, but alternate configurations and times of insertion are contemplated as well as open or sheet type devices. The coverings can optionally contain one or more drugs for delivery at the surgical site, particularly for treating or preventing infection, pain, inflammation, capsular contracture, scarring or other complications associated with breast augmentation or breast reconstruction.

Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(?O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3, or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(?O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl gro

Abstract: The invention relates to the use of novel cyclohexyl analogues of E-type prostaglandins as EP4 agonists, in general, and, in particular as ocular hypotensives. The cyclohexyl analogues used in accordance with the invention are represented by the following formula I: wherein the wavy segments represent ? or ? bond, dashed line represents the presence or absence of a bond W, Y, Z, R, R1, R2 and R3 are as defined in the specification.

Abstract: The subject invention provides ginkgolide C derivatives compounds having the structure: wherein R is H or -A-Ar, where A is an alkyl group; and Ar is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, —CH2CO2R4, and —CH2CONR5R6; where R4 is an alkyl group; and R5 and R6 are each, independently, hydrogen or a branched or unbranched alkyl group; wherein R1 is H or —COR7, where R7 is alkyl, aryl or amino; wherein R2 is present or absent, and when present is H, —COR8 or —CO—Z—R8; where R8 is alkyl, aryl or amino; and Z is oxygen; wherein R3 is present or absent, and when present is —COR9; where R9 is alkyl or aryl; wherein only one of R2 or R3 is present in the compound; wherein only two of R, R1, R2 and R3 are H; and wherein each of a and b designates a single covalent bond which is present or absent, where bond a is present when R3 is absent and bond b is present when R2

Abstract: The invention relates to compounds of Formula (1) for use in modulating potassium channel activity in cells.

Abstract: Aminophosphonate and amino bisphosphonate compounds and methods for their preparation are provided. Also provided are pharmaceutical and agricultural compositions containing the compounds. The compounds and compositions are useful in methods for treatment of various diseases, including, inflammation, autoimmune disease, cardiovascular disease, bacterial infection, viral disease, abnormal cell proliferation, bone resorption disease, osteoporosis, or parasitic disease and in various agricultural methods, including, methods of eradicating weeds.

Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.

Abstract: The present invention pertains to the use of a S1P receptor agonist in the manufacture of a medicament in the treatment of an ocular disorder.

Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

Abstract: The invention relates to compounds of general Formula I, the production thereof, and the use thereof as a medicinal product.

Abstract: There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl

Abstract: The invention relates to annelated phenyl piperazine and phenyl diazepane carboxamides of general formula (I) containing oxygen. The compounds are suitable for medical use.

Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.

Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.

Abstract: Compounds of the formula (I): in which R1, R2, R3, R?3 and R4 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, the pharmaceutical compositions comprising them, and the processes for the preparation of these compounds.

Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.

Abstract: There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0,