|8609882||Process for deacetalisation of α aminoacetals|
The invention relates to a process for the preparation of N-protected α-aminoaldehydes by deacetalization of the acetal functional group of corresponding N-protected α-aminoacetals using formic acid. ...
A compound of formula (I), wherein A1, A2, A3, A4, R1, R2, R3, G1, G2, G3 and Q are as defined in claim 1; or a salt or N-oxide thereof. Furthermore,...
|7534908||Method for the production of optically active 3-alkylcarboxylic acids and the intermediate products thereof|
An enantioselective method for producing optically active 3-alkyl carboxylic acids comprises transforming an optically active secondary alcohol into an optically active, activated compound by introducing a leaving group; reacting the activated compound with a maloni...
|7414145||Method of enantioselective nucleophilic addition reaction of enamide to carbonyl group and synthesis method of optically active α-hydroxy-γ-keto acid ester and hydroxydiketone|
A method of an enantioselective nucleophilic addition reaction to carbonyl, which enables an asymmetric synthesis of an optically active α-hydroxy-γ-keto acid ester, an optically active α-hydroxy-γ-amino acid ester, hydroxydiketone compounds, etc. being useful a...
|7368566||Process and intermediates for preparing benzazepines|
Disclosed is a new process and intermediates for preparing benzazepines of Formula (I): wherein R1 and R2 are as defined herein. ...
|7365085||Compounds and methods|
Disclosed is a compound having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined...
|7361782||Process for preparing fluorochemical monoisocyanates|
A process for preparing fluorochemical monoisocyanates comprises reacting at least one fluorochemical alcohol represented by the formula CnF2n+1SO2NCH3(CH2)mOH, wherein n=2 to 5, and m=2 to 4, with 4,...
|7354895||Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors|
The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the preventio...
|7320983||α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors|
α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. ...
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, RN, and Rc are defined herein. These compounds i...
|7312345||Process for the preparation of dronedarone|
The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone  and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-pheneti...
This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is...
|7208510||Fungicidal combinations of active substances|
The present invention relates to fungicidally active compound combinations of a fluorobenzothiazole derivative of the formula (I) and at least one of the compounds listed in the disclosure. ...
|7115593||Fungicidal combinations of active substances|
The present invention relates to active compound combinations of a fluorobenzo-thiazole of the formula (I) and at least one of the compounds listed herein. The active compound combinations of the present inventio...
|7115777||Amide derivatives as inhibitors of the enzymatic activity of renin|
The present inventions relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, the use and manufacture of a compound of formula (I) or a pharmaceutical composition comprising a c...
|7105569||Fungicidal active compound combinations|
New active compound combinations of valinamide derivatives of the formula (I) in which R1 and R2 has the meaning given in the description, with k...
|7045660||Compounds as PDE IV and TNF-inhibitors|
This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment...
|7038044||Method for preparing 2-(2-arylmorpholin-2-yl)ethanol derivatives and intermediates|
The invention relates to a process for the preparation of substituted 2-(2-arylmorpholin-2-yl)ethanol derivatives. ...
|7022872||Method for making fluorine labeled L-Dopa|
The invention relates to a method for preparing F-Dopa and 18F-Dopa and intermediates that are useful in the method. The invention is a method that synthesizes F-Dopa and 18F-Dopa in good yield with high enantiopurity without the need for furth...
|6972292||Certain substituted polyketides, pharmaceutical compositions containing them and their use in treating tumors|
The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds ...
|6953850||Protecting groups for carbohydrate synthesis|
The invention provides collections of orthogonally-protected monosaccharides as universal building blocks for the synthesis of glycoconjugates of non-carbohydrate molecules, neo-glycoconjugates and oligosaccharides. This orthogonal protection strategy allows for the...
|RE38796||Process for producing 3-amino-2-oxo-1-halogenopropane derivatives|
Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoaceta...
|6939986||Process for preparing 1,2-diamino compounds|
The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides. ...
|6852887||Preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-P-nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines|
The present invention provides a new process for the preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of t...
|6849626||Aza-amino acid derivatives (factor Xa inhibitors 15)|
The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formul...
|6831102||Phenyl naphthol ligands for thyroid hormone receptor|
New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or...
The invention relates to a highly active, highly specific urokinase inhibitor which is suitable for therapeutic applications and can be synthesized in an extremely simple manner. Surprisingly, it was found that amidino benzylamine derivatives, especially 4-amidino-b...
|6759511||Compound used as an amino-protecting group, process for preparing the same, and synthetic method of a peptide using the same|
The present invention relates to a carbonic acid ester compound of the following formula (1): in which X, Y, and Ar are defined in the specification, which can be easily combined with the amino group of an amino acid or ...
Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.
|6696487||Fungicidal phenyl(thio)urea and phenyl(thio)carbamate derivatives|
The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: ##STR1## in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing t...
|6686470||Compounds of the saframycin-ecteinascidin series, uses, and synthesis thereof|
Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: ##STR1## wherein R1 and R4 is H, a C1 to C4 alkyl group, ...
|6683200||N-substituted-N'-substituted urea derivatives and pharmaceutical compositions containing the derivatives|
N-Substituted-N'-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF- production inhibitory activity. ##STR1##...
|6667413||Uracil compounds and use thereof|
The present invention relates to an uracil compound of the formula [I]: ##STR1## wherein W represents oxygen, sulfur, imino or C1 to C3 alkylimino; Y represents oxygen, sulfur, imino or C1 to C3 alkylimino; R
|6653501||Chiral resolution method for producing compounds useful in the synthesis of taxanes|
A method is provided for processing a solution having optical isomers to obtain a (2R,3S) target isomer: ##STR1## wherein P1 is H or a hydroxyl protecting group, R1 is H, an alkyl group, an olefinic group or an aromatic group, and R
|6649639||Antipicornaviral compounds, compositions containing them, and methods for their use|
Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treatin...
|6646150||Processes for producing (aminomethyl)trifluorocarbinol derivatives|
The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives, in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc....
|6620961||Biarylalkylenecarbamic acid derivatives and bacteriocides for agricultural and horticultural use|
Biarylalkylenecarbamic acid derivative represented by general formula (I): ##STR1## [wherein Q is a phenyl group which may be substituted or the like, X is a halogen atom, a (C1 -C6) alkyl group or the like, n is 0 or an integer of f...
|6610715||Cathecol hydrazone derivatives, process for preparing the same and pharmaceutical composition containing the same|
The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5
|6573399||Synthesis of -amino-', '-dihaloketones and process for the preparation of ଲ-amino acid derivatives by the use of the same|
The present invention provides a commercially profitable process for producing a ଲ-amino acid ester derivative which comprises reacting an -amino acid ester derivative with a base and a dihalomethane, reacting the same with a lithium amide and an ...
|6570034||Blocked phenylenediamine developers for a color photographic element|
The present invention relates to a novel blocked phenylenediamine developer useful, in reactive association, for enabling, on development, a non-magenta color, for example a cyan color, from a dye-forming coupler. In one embodiment, the developer has the ...