Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: Provided are manassantin compounds and methods of using the compounds. Provided are methods of treating a disease, the method comprising administering a compound according to Formula I. Further provided are pharmaceutical compositions comprising compounds according to Formula I. Also provided are methods of inhibiting HIF-1 in a cell, the methods comprising administering to the cell a compound according to Formula I.

Abstract: The present invention provides an organocatalyst of formula (I), wherein R1 is —H, —OH, —O—Si(R4)(R5)(R6) or C1-6alkoxy, in which R4, R5 and R6 are identical or different and independently selected from the group consisting of C1-6alkyl, phenyl and phenyl substituted with C1-6alkyl; R2 is —OH or ?O; X1 is one selected from the group consisting of —NH—, —S— and X2 is one selected from the group consisting of —C(?O)—, —CH2— and and X1 is different from X2. The high yield and enantioselectivity of an addition reaction are obtained by using the organocatalyst of the present invention.

Abstract: Compounds of Formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

Abstract: The present invention relates to an enantioselective synthesis of (+)-trans enantiomer of pyrrolidines substituted with flavones, represented by Formula 1 or salts thereof, which are inhibitors of cyclin dependant kinases and can be used for treatment of proliferative disorders such as cancer wherein Ar has the meaning as indicated in the claims.

Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor.

Abstract: The present invention provides an organocatalyst of formula (I), wherein R1 is —H, —OH, —O—Si(R4)(R5)(R6) or C1-6alkoxy, in which R4, R5 and R6 are identical or different and independently selected from the group consisting of C1-6alkyl, phenyl and phenyl substituted with C1-6alkyl; R2 is —OH or ?O; X1 is one selected from the group consisting of —NH—, —S— and X2 is one selected from the group consisting of —C(?O)—, —CH2— and and X1 is different from X2. The high yield and enantioselectivity of an addition reaction are obtained by using the organocatalyst of the present invention.

Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: A quaternary ammonium salt of the formula (1), electrolytic solution and electrochemical device using the salt wherein R1 is straight-chain or branched alkyl having 1 to 4 carbon atoms, R2 is methyl or ethyl, and X? is a fluorine-containing anion.

Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Allskiren. Inter alia, the invention provides a process for the manufacture of a compound of the formula III, wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof. The manufacture comprises (preferably consists of) reacting a compound of the formula I, with a reagent able to transform hydroxy into X where X is for example a leaving group.

Abstract: Provided herein are compounds of formulae I to II that bind to androgen receptors and/or modulate activity of androgen receptors; and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.

Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Compounds of the formula I: wherein m, n, Ar, R1 and R2 are as defined herein. Methods of making the compounds and using the compounds are disclosed.

Abstract: The present invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention provides a process for the manufacture of a compound of the formula III, wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof. The manufacture comprises (preferably consists of) reacting a compound of the formula I, with a reagent able to transform hydroxy into X where X is for example a leaving group.

Abstract: The invention relates to an ophthalmologic composition including a dye of the general formula I in which R1=substituted or unsubstituted hydrocarbon radical, R2=substituted or unsubstituted hydrocarbon radical with at least one polymerizable double bond, R3?H or substituted or unsubstituted hydrocarbon radical, R4?H, electron-withdrawing substituent or substituted or unsubstituted hydrocarbon radical and X?O, S, NH or NR5, wherein R5 is a substituted and/or unsubstituted hydrocarbon radical. Moreover, the invention relates to another ophthalmologic composition and an ophthalmologic lens.

Abstract: A compound represented by the formula (I) wherein ring A is a 5- to 8-membered ring optionally having further substituent(s) other than R6, R7 and R8, R1 is an electron-withdrawing group, R2, R3, R4 and R5 are each independently a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, R6 is a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, R7 is a cyano group, a nitro group, an acyl group optionally having substituent(s), an optionally esterified or amidated carboxyl group or a hydrocarbon group optionally having substituent(s), or R6 and R7 optionally form, together with the carbon atom bonded thereto, a ring optionally having substituent(s), and R8 is a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxyg

Abstract: A chemical genus of biphenyl heterocycle derivative inhibitors of LTA4H (leukotriene A4 hydrolase) of the formula: is disclosed. In these compounds Q and Z are (CH2)1-10; in which one or two (CH2) may optionally be replaced by —O—, —NR1—, —SO—, —S(O)2—, —C(?O)— or —C?O(NH)—; Het is a 5-7 membered non-aromatic nitrogen heterocycle; and W is acyl, hydroxyl, carboxyl, amino, carboxamido, aminoacyl, —COOalkyl, —CHO, heterocyclyl, substituted aryl, or substituted heterocyclyl, or taken together ZW can be H or —COOalkyl. The compounds are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and Alzheimer's disease with a derivative of ginger oil are also provided. Also provided is a method of conditioning biological extracts, such as a medicinal plant extract, by a reductive amination process to give nitrogen-containing derivatives.

Abstract: The present invention relates to an enantioselective synthesis of (+)-trans enantiomer of pyrrolidines substituted with flavones, represented by Formula 1 or salts thereof, which are inhibitors of cyclin dependant kinases and can be used for treatment of proliferative disorders such as cancer. wherein Ar has the meaning as indicated in the claims.

Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

Abstract: Provided are novel compositions which uniquely inhibit sphingosine kinase Type 1 (SphK1) and which are useful in a number of applications including killing or damaging cancer cells, inducing apoptosis, inhibiting growth, metastasis and development of chemoresistance in cancer cells, leukemia, increasing the effectiveness of anti-cancer agents, attenuating immune reactivity, inhibiting survival signaling in cancer cells, and reducing symptoms of multiple sclerosis.

Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: The invention provides for a pharmaceutical composition capable of modulating the androgen receptor comprising a compound of formula I wherein R1, R2, R3, X, Y, Z and G are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.

Abstract: Disclosed herein are substituted benzhydrylethers of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of their use thereof.

Abstract: The present invention relates to the compounds of the general formula (I), a composition for and a method of treating breast cancer or other proliferative disorders in a subject using a compound of general formula [I], wherein the substituents are as defined in the specification.

Abstract: The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.

Abstract: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.

Abstract: This invention relates to nitroproline derivative compounds and procedures for their preparation and the preparation of pharmaceutical compositions containing the compounds. The invention also relates to the administration of compounds of the invention as agents for the treatment of mammalian diseases whose pathogenic and pathophysiological mechanisms depend on or are significantly contributed by undesirable cellular and molecular activities or responses induced by integrin-dependent molecular interactions.

Abstract: New compounds that bind to monoamine transporters are described. The compounds of the present invention can be racemic or pure R— or S-enantiomers. Certain preferred compounds of the present invention have a high selectively dopamine transporter versus the serotonin transporter. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and Alzheimer's disease with a derivative of ginger oil are also provided. Also provided is a method of conditioning biological extracts, such as a medicinal plant extract, by a reductive amination process to give nitrogen-containing derivatives.

Abstract: A method for removing impurities from racemic cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol and purified cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol useful as an estrogen agonist/antagonist.

Abstract: Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: The present invention discloses an aminothiol compound having a general formula I wherein R1-R5 are substitutable ligands. Such compound can perform as a superior catalyst in an asymmetric addition reaction of organic metal compounds and aldehyde. According to the present invention, the aminothiol compound is needed only less than 0.02% based on main reactants to obtain enantioselectivity higher than 98% enantiomeric excess, whereby the asymmetric reactions can become very economic.

Abstract: The invention relates to a process for the reduction of compounds comprising a carbon-carbon (C?C), carbon-oxygen (C?O), or carbon-nitrogen (C?N) double bond, to a corresponding hydrogenated alkane, alcohol or amine, comprising contacting a compound comprising the C?C, C?O or C?N double bond with a hydrogen donor solvent and a catalyst comprising a metal complex having a tridentate aminodiphosphine ligand under transfer hydrogenation conditions.

Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.

Abstract: The invention relates to a process for preparing 2-methylpyrrolidine and, more particularly, specific enantiomers of 2-methylpyrrolidine. Novel intermediates also are described.

Abstract: The invention is a method for producing ?-aminopentadienoate derivatives of formula (1), the method comprising reacting a streptocyanine derivative of formula (2) with an ester derivative of formula (3) in the presence of an organic base.

Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.

Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

Abstract: Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.

Abstract: Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.