Abstract: A method is provided for producing optically active alcohols from ketones by reducing a ketone in the presence of an iridium(III) complex having a chiral prolinamide compound as a ligand.

Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

Abstract: The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R1 and R2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R1 and R2 are as defined for the compound of formula I; and (a-ii) reductively cyclising the compound of formula III to give the compound of formula I.

Abstract: The present invention provides compounds represented by general formula (I): wherein, R1, R2, R3, L and T are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, and prodrugs thereof. The invention also relates to processes for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful in the treatment of a condition or disorder mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-?) and interleukins such as IL-1, IL-6, and IL-8. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (I) or its pharmaceutical composition, to a mammal in need thereof.

Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, each (Z)-pentadecenyl, (Z)-hexadecenyl or (Z)-heptadecenyl, etc, a and b are, the same or different, each 0 to 3, m is 1, the dotted line is a single bond or absent, X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, X4 is absent or is alkylene, etc X3 is absent or is alkyl, etc, Y is absent or anion, L3 is a single bond, —CO—O— or —O—CO— R3 is hydrogen atoms, alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—) and the like.

Abstract: The present invention includes a method of preparing a composition comprising (+)-doxapram or a salt thereof, wherein the composition is essentially free of (?)-doxapram or a salt thereof.

Abstract: Disclosed is a selective ester production process of an alcoholic hydroxyl group, which proceeds under chemically mild conditions, while having adequate environmental suitability, operability and economical efficiency. Specifically disclosed is a process for producing an ester compound, which is characterized in that an alcohol and a carboxylic acid ester compound are reacted in the presence of a compound containing zinc element, thereby selectively acylating a hydroxyl group of the alcohol.

Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

Abstract: Ester derivatives of 2-amino-2-phenyl-alkanol of general formula (I) in which: R1 forms with R3 and the nitrogen and carbon atoms to which they are respectively attached, a heterocycle with 4 to 7 members, optionally substituted in the ? position of the nitrogen atom by one or two Ra and Rb radicals being able to be independently of one another hydrogen or linear or branched alkyl (1 to 4C), and R2 is H or a —CO—O—CHR4—OCOR5 radical for which R4 is H or linear or branched alkyl (1 to 4C), and R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by the remainder of an amino acid, or represents a heterocycle, or R2 is linear or branched alkyl (1 to 4C), alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, NH2, alkylamino, dialkylamino optionally forming with the nitrogen atom to which they are attached, a heterocycle with 5 or 6 members, it being understood that the substituted alkyl radical is linear or branched and comprises at least 2C between >N—R2 and the substituent, unless speci

Abstract: Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof

Abstract: The present invention related to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to novel salts thereof, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).

Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.

Abstract: The invention provides direct processes and related catalysts for the syntheses of trisubstituted chiral pyrrolidines, piperidines, tetrahydrothiophenes, and thianes by highly enantio- and diastereoselective cascade Michael-Michael reaction of ?, ?-unsaturated aldehydes with trans-?-protected amino ?, ?-unsaturated esters.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

Abstract: Disclosed is a selective ester production process of an alcoholic hydroxyl group, which proceeds under chemically mild conditions, while having adequate environmental suitability, operability and economical efficiency. Specifically disclosed is a process for producing an ester compound, which is characterized in that an alcohol and a carboxylic acid ester compound are reacted in the presence of a compound containing zinc element, thereby selectively acylating a hydroxyl group of the alcohol.

Abstract: One aspect of the present invention relates to compounds for delivering chemotherapeutic agents to cancerous cells to reduce discomfort and deleterious side effects associated with systemic administration of such agents. Another aspect of the invention relates to methods of treating a subject with cancer by administering a therapeutically effective amount of a chemotherapeutic agent that predominately targets cancerous cells over healthy cells. Additionally, one aspect of the present invention relates to methods of inhibiting the life-cycle of a cancerous cell, as well preparing a chemotherapeutic prodrug.

Abstract: Disclosed herein is a compound comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, X, R and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.

Abstract: Disclosed are novel fusion proteins containing antibody binding regions and certain other regions. Said fusion proteins can form complexes with antibodies, which can thus be modified and be arranged three-dimensionally. Furthermore, the effect thereof can be boosted.

Abstract: Disclosed are materials and methods for preparing optically active ?-amino acids, which bind to the alpha-2-delta subunit of a calcium channel and are useful for treating pain, fibromyalgia, and a variety of psychiatric and sleep disorders. The method includes reacting a chiral allyl amine with a 2-alkynoate in the presence of a Lewis acid and a base to give a chiral tertiary enamine, which after reaction with ammonia, is hydrogenated to give optically active ?-amino acids.

Abstract: Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.

Abstract: The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae I and II wherein R21, R22, R23 and R24 are as defined in the description and claims.

Abstract: The invention relates to novel heterocycle substituted diphenyl leukotriene B4 (LTB4) antagonists, to compositions containing such compounds, and to methods of using such compounds for treatment of inflammatory diseases.

Abstract: The invention concerns compounds of formula (I) wherein in particular G presents the —N(CH3)2—, —N(C2H5)2-group or N-pyrrolidine: n is an integer equal to 1 or 2: R1, R2 and R3 independently of one another, represent a hydrogen atom or a methyl group, the successive unsaturated units capable of being moreover identical or different, provided that at least one of the substituents R1, R2 and R3 is different from H: and Y1 and Y2 represent each a —COOCH3 group or a —COOC2H5 group.

Abstract: Novel anti-tumor compounds of formula, are disclosed. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), the use of compounds of formula (I) for the treatment of cancer, and processes for the preparation of compounds (I).

Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I, Formula (I) wherein R1 is (C1-3)alkyloxy, (C1-3)alkyloxy(C1-3)alkyl, (C1-3)alkylthio, (C1-3)alkylthio(C1-3)alkyl, (C1-3)alkylsulfinyl, (C1-3)alkylsulfinyl(C1-3)alkyl, (C1-3)alkylsulfonyl, (C1-3)alkylsulfonyl(C1-3)alkyl, (C1-3)alkyloxycarbonyl, (CH2)n—CO—NR8R9? or (CH2)n—NR8R9?; n is 0, 1 or 2; R2 is hydrogen or (C1-3?)alkyl; R3 is (C1-3)alkyl or (C1-3)alkyloxy(C1-3?)alkyl; R4 is (C1-3)alkyloxy(C1-3)alkyl; or R3 and R4 form together with the nitrogen atom to which they are bound a 5-, 6-, or 7-membered ring, optionally containing a further heteroatom selected from O and S, and which ring may optionally contain a double bond and be optionally substituted with (C1-3)alkyl or (C1-3)alkyloxy; R5 and R6 are independently (C1-3)alkyl; R7 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R8 and R9 are independently (C1-3)alkyl; or R8 and R9 form together with

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, a trihalomethylcarbonyl group, such as a trifluoromethylcarbonyl group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.

Abstract: Pyrrole derivatives represented by the following formula: 1

Abstract: The present invention relates to a novel antifungal molecule 2-(3,4-dimethyl-2,5-dihydro-1H-pyrrol-2-yl)-1-methylethyl pentanoate of formula (I) from a plant Datura metel a process for isolation and characterization of the molecule and a pharmaceutical composition essentially comprising the molecule as an antifungal agent.

Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): 1

Abstract: Compounds of formula (1) containing sterically hindered groups, polymers thereof and the use of these polymers in papermaking processes and dewatering processes.

Abstract: The invention relates to novel bicyclic aromatic compounds which have the general formula (I): 1

Abstract: A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.

Abstract: A process for preparing compounds of the formula I in which R is hydrogen, C1-C6-alkoxy, —NHC1-C6-alkyl, —N(C1-C6-alkyl)2, OH, NH2 R1 is hydrogen, C1-C6-alkyl, Me3Si, C1-C6-alkyl-S R2 is Boc, C1-C6-acyl, mesyl, benzenesulfonyl, tosyl, trifluoroacetyl, A1-A3-peptide n is 1, 2 R4 is H, C1-C6-alkyl, is described.

Abstract: The invention provides compounds of formula (I) 1

Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

Abstract: This invention relates to compounds of Formula V H—Y—G—R   V and Formula VI (wherein f, X, Y, G and R have the values defined in the description) which are useful as intermediates for the preparation of compounds, or pharmaceutically acceptable salts thereof, which are useful as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.

Abstract: There is disclosed a process for producing an optically active hemiester of formula (1): 1

Abstract: This invention is directed to methods of synthesizing densely functionalized pyrrolidine compounds through the use of intramolecular Diels Alder reactions.

Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.

Abstract: A series of 3-pyrrolidinyloxy-3′-pyridyl ether compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions including these compounds. Preferred compounds are 3-pyrrolidinylmethoxy-3′-(5′-and/or 6′-substituted) pyridyl ethers.

Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives.

Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: The present invention provides pharmaceutically active compounds formula I wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl), or halo; R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; and n is 2 or 3; and or a pharmaceutically acceptable salt thereof. Also provided are compounds of formula II wherein R1a is —H or —OR5 in which R5 is a hydroxy protecting group. R2a is —H, halo, or —OR6 in which R6 is a hydroxy protecting group; and R4 is —OH or —CHO; or a pharmaceutically acceptable salt thereof.