|7910775||Synthesis of 2-Hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide|
Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I ...
|7728173||Processes for preparing venlafaxine and venlafaxine hydrochloride of form I|
A process for preparing venlafaxine in a high yield as well as processes for producing venlafaxine hydrochloride of form I having a very hight polymorphic purity are described. ...
|7482488||Aryl and heteroaryl propene amides, derivatives thereof and therapeutic uses thereof|
Compounds useful as antiproliferative agents, radioprotective agents and cytoprotective agents, including, for example, anticancer agents, are provided according to formula I: wherein ring A, ring B,,X, R1, R2, R3, a, and b are as de...
|7439356||Substituted indan derivatives|
The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR2 wherein R2 is H or C1-C
|7423154||Asymmetric process for the preparation of diarylethylpiperazines derivatives and novel asymmetric diarylmethylamines as intermediates|
An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral su...
|7385072||Methods for the preparation of Entacapone|
The invention disclosed in this application relates to an improved process for the preparation of Entacapone. In one embodiment the process involves: (i) reacting a 3-alkoxy-4-hydroxy-5-nitrobenzadehyde with N,N-diethylaminocyanoacetamide in the presence of a mild a...
Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders
|7196220||Bone targeting compounds for delivering agents to the bone for interaction therewith|
The present invention relates to compounds of the formula or pharmaceutically acceptable salts thereof, useful for delivering agents having the capacity to diagnose, treat or prevent bone injury or disease to the b...
|7196100||Opioid receptor antagonists|
A compound of the formula (I) wherein the variables X1 to X5, R1 to R7 including R3′, E, q, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer...
|6960581||Glucocorticoid mimetics, methods of making them, pharmaceutical formulations, and uses thereof|
A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical com...
|6891066||N-(4-substituted phenyl)-anthranilic acid hydroxamate esters|
The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. ...
|6803383||Inhibition of angiogenesis and tumor growth|
Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core. ...
|6774116||Prodrugs via acylation with cinnamate|
A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically donating or electronically with...
|6770778||N-(4-substituted phenyl)-anthranilic acid hydroxamate esters|
The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof. ...
|6737420||Compounds to treat Alzheimer's disease|
The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases. ...
|6706765||Aminoguanidines and alkoxyguanidines as protease inhibitors|
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra
|6660872||Method of producing methoxyimino acetic amide|
The present invention relates to novel processes for preparing methoxyimino-acetamides....
|6646162||Compounds and compositions for delivering active agents|
Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well....
|6548549||Acylaminosalicylic acid amides and their uses as pesticides|
The invention relates to known and to new acylaminosalicylamides, to a plurality of processes for their preparation and to their use as pesticides. The present application furthermore relates to new intermediates, to a plurality of processes for their pre...
|6518310||Aminoguanidines and alkoxyguanidines as protease inhibitors|
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1## wherein X is O or NR9 and R1 -R4, R6 -R9, R11, R12, Ra, Rb, R
|6509379||Phenylacetic acid derivatives, process and intermediate products for their preparation, and their use as fungicides and pesticides|
Phenylacetic acid derivatives of the formula I ##STR1## where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests....
Propanolamine derivatives represented by the following formula (I): ##STR1## These derivatives may be 댣 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria ac...
|6414031||Bisoximether derivatives, methods and intermediate products for the production thereof, and their use for combating fungicidal pests and animal pests|
There are disclosed bisoxime ether derivatives of the formula I ##STR1## in which the variables have the following meanings: R1 is halogen, C1 -C4 -alkyl, C1 -C4 -haloalkyl, C1 -C4 -a...
|6372937||Enhanced catalyzed reporter deposition|
A method for enhancing the conversion of a phenol substrate to a product by a peroxidase enzyme comprises the steps of reacting a conjugate comprising a detectably labeled phenol with a peroxidase enzyme in the presence of an enhancing reagent, the enhanc...
|6355666||Protected forms of pharmacologically active agents and uses therefor|
In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of...
|6342576||Urethanized ଲ-hydroxyalkylamide compound, a process for preparing it and its use for preparing powder coating materials|
A urethanized ଲ-hydroxyalkylamide compound, a process for its preparation, and powder coating materials containing them....
|6340691||Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase and tace inhibitors|
Compounds of the formula ##STR1## are useful in treating disease conditions mediated by TNF-, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss....
Compounds of formula ##STR1## (I), wherein either X is CH or N, Y is OR1 and Z is O, or X is N, Y is NHR8 and Z is O, S or S(.dbd.O); R1, R2 and R3 are as defined according to the specification; m is 0, 1 ...
|6303350||Physiologically active substances TKR2449, process for producing the same, and microorganism|
The present invention has for its object to provide novel biologically active substances which is of value as a therapeutic agent for fungal infections and immune disorders. This invention is related to a biologically active substance TKR2449 analog(s) wh...
|6248781||Compounds useful in the treatment of conditions mediated by peroxisome proliferator-activated receptors (PPAR)|
The present invention relates to compounds of formula (I) ##STR1## wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These ...
|6239179||N-aminoalkyl-2-anthracenecarboxamides; new dopamine receptor subtype specific ligands|
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4, R5, R6, R7, R8 and R9 a...
|6204384||Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)|
The present invention provides peptide aldehydes having an 3-amino-2-hydro yenyl acetamide group as part of the peptide backbone d an arginine group or analog at P1. These compounds e potent and specific or inhibitors of thrombin. Ther pharmaceutically ac...
|6169116||Amino-tetralines, pharmaceutical compositions containing them and their pharmaceutical uses|
Compounds of formula I ##STR1## wherein R1, R2, R3, R4 and R5 are as defined in the description, are useful as pharmaceuticals....
|6150374||Substituted cycloalkenes, process of preparing them and method of using them as pesticides|
The invention relates to novel substituted cycloalkenes of the formula (I), ##STR1## to a plurality of processes for their preparation, and to novel intermediates and a plurality of processes for their preparation....
|6147224||2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors|
Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR1 R1)n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent ar...
|6143734||Nitroso esters of ଲ-oxo-amides and aryl propionic acid derivatives of non-steroidal antiinflammatory drugs|
A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a compound comprising an enolic anilide non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO2 gr...
|6130349||Catalytic compositions and methods for asymmetric allylic alkylation|
Complexes of a selected class of chiral ligands with molybdenum, tungsten or chromium, preferably molybdenum, are effective as catalysts in highly enantioselective and regioselective alkylation of allylic substrates. Such compositions provide a versatile ...
|6117365||Phenolic acid amides of hydroxy-substituted benzylamines|
The invention relates to specific phenolic acid amides of hydroxy-substituted benzylamines of the formula I ##STR1## to a process for their preparation and to their use as antioxidants or as free-radical scavengers, in particular in the cosmetic or d...
|6084130||Aryl substituted bicyclic amines as selective dopamine D3 ligands|
Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of structural Formula I: ##STR1##...
|6054457||Benzamide derivatives and their use as vasopressin antagonists|
This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower...