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Class 549/72 - Nitrogen or chalcogen attached indirectly to the hetero ring by nonionic bonding


Subclass of Class 549 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen or chalcogen (i.e., oxygen, sulfur,
No. of applications: 88
Last issue date: 12/29/2011


1      
Application No.Application TitleIssue Date
20110318359METHOD FOR REDUCING BLOOD PRESSURE USING INHIBITORS OF PLASMA KALLIKREIN
The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor....
12/29/2011
20110306542NOVEL GLP-1 RECEPTOR STABILIZERS AND MODULATORS
Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the ...
12/15/2011
20110275835PROCESS FOR PREPARING (S)-(+)-N-METHYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE BY USING OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL COMPOUND AS INTERMEDIATE
The present invention provides (S)-methylhydroxylaminopropanol compound as an intermediate in preparation of (S)-(+)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-(1-naphthyloxy)-3-(2-...
11/10/2011
20110275663N-Acylthiourea and N-Acylurea Inhibitors of the Hedgehog Protein Signalling Pathway
The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivat...
11/10/2011
20110263556New Compounds
This invention relates to compounds of formula I,

their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medi...

10/27/2011
20110257196COMPOUNDS FOR TREATMENT OF CANCER
The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant ...
10/20/2011
20110257182Novel amido derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors
The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—s...
10/20/2011
20110218221NOVEL HISTONE DEACETYLASE INHIBITORS, PROCESS FOR PREPARATION AND USES THEREOF
The present invention relates to compounds represented by formula (I) or composition comprising at least one of such compounds, which are inhibitors of histone deacetylase. The detailed description of these compounds is disclosed in the Description. These compounds and ...
09/08/2011
20110213003SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
This invention provides compounds of formula (I):

    • wherein X1, X2, ...
09/01/2011
201102131565-MEMBERED HETEROCYCLIC COMPOUND
A compound represented by the following general formula (I):

[wherein R1 and R2 represent an alkyl group, X represents —S—, —O— or —NH—, Y represents C or N, R3 re...

09/01/2011
20110207945Process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols
Provided is a process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols, particularly of (S)-(−)- and (R)-(+)-3-N-methylamino-1-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of formula ...
08/25/2011
20110207739Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhi...
08/25/2011
20110178101DUAL-ACTING THIOPHENE, PYRROLE, THIAZOLE AND FURAN ANTIHYPERTENSIVE AGENTS
In one aspect, the invention relates to compounds having the formula:

wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt ...

07/21/2011
20110160207HETEROCYCLIC AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS
A compound of Formula I

and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating ...

06/30/2011
20110144189GUANYLHYDRAZONE COMPOUNDS, COMPOSITIONS, METHODS OF MAKING AND USING
The present invention relates to compounds having the formula:

    • salts thereof; compositio...
06/16/2011
20110118303NOVEL COMPOUNDS DERIVED FROM TAURINE, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE
The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity.

In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by mea...

05/19/2011
20110092496THIOPHENE COMPOUNDS AND THROMBOPOIETIN RECEPTOR ACTIVATORS
A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

04/21/2011

20110021528NOVEL HYDROXAMATES AS THERAPEUTIC AGENTS
The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase act...
01/27/2011
20110021771INHIBITORS OF HISTONE DEACETYLASE
This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof...
01/27/2011
20110009457Aminobenzamide Derivatives as Useful Agents for Controlling Animal Parasistes
The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases...
01/13/2011
20100297542SULPHONIUM SALT INITIATORS
Compounds of the formula (I), wherein X is a single bond, CRaRb O, S, NRC, NCORC, CO, SO or SO2; L, L1, L2, L3, L4, L5, L6, L7 and L8...
11/25/2010
20100280036Modulation of Pathogenicity
The present invention relates to the use of compounds of the general Formula (I):

wherein in Formula (I),

    11/04/2010
    20100273835NOVEL COMPOUNDS
    The invention provides compounds of general formula (I)

    or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are des...

    10/28/2010
    20100260778SMALL-MOLECULE BOTULINUM TOXIN INHIBITORS
    Small-molecule inhibitors of Botulinum toxin, including BoNTA, BoNTD and BoNTE are provided, as well as methods of using the inhibitors....
    10/14/2010
    20100261675FUNGICIDAL COMPOSITION CONTAINING ACID AMIDE DERIVATIVE
    Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upo...
    10/14/2010
    20100261760EP2 Receptor Agonists
    The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor....
    10/14/2010
    20100240717NOVEL THIOPHENE DERIVATIVES AS S1P1/EDG1 RECEPTOR AGONISTS
    The invention relates to thiophene derivatives of formula (I)/their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *—CO—CH═CH—, *—CO—CH2CH2
    09/23/2010
    20100240911Process for the preparation of N-monosubstituted beta-amino alcohols
    A process for the preparation of a compound of formula:

    and/or an addition salt of a proton acid, which process comprises the following steps:
    (a) reacting a mixture comprising (i) a methyl ketone of fo...

    09/23/2010
    20100216849BIPHENYLCARBOXAMIDES
    This invention relates to novel biphenylcarboxamides of the formula (I)

      • in which R, Z, X...
    08/26/2010
    20100217008PROCESS FOR THE PREPARATION OF VALSARTAN AND INTERMEDIATE PRODUCTS
    The present invention relates to a new method for the production of valsartan, a valine derivative having the chemical N name is (S)—N-(1-carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2′-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]amine, and pharmacologically acceptable salt...
    08/26/2010
    20100204487PROCESS FOR MAKING THIOPHENE CARBOXAMIDE DERIVATIVES
    The invention encompasses a process for making a thiophene carboxamide derivative, which is an EP4 antagonist useful for treating pain and inflammation....
    08/12/2010
    20100190779VIRAL POLYMERASE INHIBITORS
    Compounds of formula I:

    wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase....

    07/29/2010
    20100173981THERAPEUTIC COMPOUNDS
    Disclosed herein is a compound according to one of the formulas or a pharmaceutically acceptable salt thereof, medicaments for the treatment of glaucoma or ocular hypertension and compositions related thereto, as further elaborated herein.

    ...

    07/08/2010
    20100144785FUNGICIDE N-6-MEMBERED FUSED (HETERO) ARYL-METHYLENE-N-CYCLOALKYL CARBOXAMIDE DERIVATIVES
    The present invention relates N-(aromatic, 6-membered, fused, (hetero)aryl-methylene)-N-cycloalkyl carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl g...
    06/10/2010
    20100137347SUBSTITUTED ARYLCYCLOPENTENES AS THERAPEUTIC AGENTS
    Disclosed herein is a compound of the formula (I). Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.

    ...

    06/03/2010
    20100137417Glucagon Receptor Antagonists, Preparation and Therapeutic Uses
    The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such ...
    06/03/2010
    20100137336NOVEL AMIDO DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
    The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—s...
    06/03/2010
    20100137599PROCESS FOR PREPARING 1,4-BUTANDIOL MONITRATE
    The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds....
    06/03/2010
    20100137291NITROSATED NONSTEROIDAL ANTIINFLAMMATORY COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releas...
    06/03/2010
    20100113477Inhibitors of mycobacterium tuberculosis malate synthase, methods of making and uses thereof
    The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or th...
    05/06/2010
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