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Class 546/304 - Nitrogen attached directly to the six-membered hetero ring by nonionic bonding


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached directly to the six-membered
No. of patents: 391
Last issue date: 04/24/2012


1                    
NumberTitleIssue Date
8163930Process for preparing pyridinamines and novel polymorphs thereof
The present invention relates to an improved process for the synthesis and purification of 3-chloro-N-(3-chloro-5-tri-fluoromethyl-2-pyridyl)-a,a,a-trifluoro-2,6-dinitro-p-toluidine (fluazinam) and other pyridinamines, which implements methyl isobutyl ketone (MIBK) ...
04/24/2012
8134009Process for the oxidation of secondary amines into the corresponding nitroxides
The invention relates to a process for the preparation of secondary nitroxide radicals from their corresponding secondary amines by oxidation with an organic peracid, comprising the steps a) adding to a reaction vessel a secondary amine, optionally together with an ...
03/13/2012
80396322-aminio-pyridine derivatives and their use as potassium channel modulators
This invention relates to novel 2-amino-pyridine derivative useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutic...
10/18/2011
8034949Pyrrolidine compound and a process for preparing the same
The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R1 and R2 is (A) optionally substituted aryl (or heteroa...
10/11/2011
7932395Substituted 1-dihydropyrazoles, their preparation and use
This invention provides compounds of Formula I, methods for their preparation and use for preparing compounds of Formula II wherein R1, R2, R3, R5, R...
04/26/2011
7514564Substituted amine derivatives and methods of use
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for p...
04/07/2009
7435815Sulfonylamino-acetic acid derivatives
The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmac...
10/14/2008
74140644-(3,3-dihalo-allyloxy) phenoxy alkyl derivatives
Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1-C6alkylene bridge; ...
08/19/2008
74109864-6-diphenyl pyridine derivatives as antiinflammatory agents
4-aryl pyrimidine compounds of general formula and salts thereof: wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is hydrogen or hydroxy; R3 is hydrogen, C1-6 alkyl, etc.; R4 is hydrogen, hydroxy, halogen, amino, etc.; R5 is hydroxy,...
08/12/2008
7399775β-amyloid protein production/secretion inhibitor
Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety...
07/15/2008
7388021Urea antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating disease...
06/17/2008
7388022Polysubstituted 1,1-pyridylaminocyclopropanamine compounds
A compound selected from those of formula (I): wherein: n represents an integer from 1 to 6 inclusive, R1 and R2 represent a hydrogen atom, a (C1-C6)alky...
06/17/2008
7375121Chemical compounds
The present invention concerns 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...
05/20/2008
7371753Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and sp...
05/13/2008
7368572Acetylene derivatives as inhibitors of histone deacetylase
The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparin...
05/06/2008
73421153-substituted-6-aryl pyridines
3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred...
03/11/2008
7332498Modulation of KSP kinesin activity with heterocyclic-fused pyrimidinone derivatives
A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts there...
02/19/2008
7332548Process for production of a polyester product from alkylene oxide and carboxylic acid
A process to produce polyester product from alkylene oxide and carboxylic acid. More specifically this process relates to a process to produce polyethylene terephthalate where terephthalic acid and ethylene oxide are reacted to form a partially esterified terephthal...
02/19/2008
7323474Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase
The invention relates to pyridine derivatives of formula (I) wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage in the preparation...
01/29/2008
7320989Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use. ...
01/22/2008
7320990Crystalline form of a biphenyl compound
The invention provides a crystalline naphthalene-1,5-disulfonic acid salt of biphenyl-2-ylcarbamic acid 1-{9-[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydro-quinolin-5 -yl)ethylamino]nonyl}piperidin-4-yl ester or a solvate thereof. This invention also provides pharmac...
01/22/2008
73148496-(poly-substituted aryl)-4-aminopicolinates and their use as herbicides
4-Aminopicolinic acids having tri- and tetra-substituted aryl substituents in the 6-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control. ...
01/01/2008
72946421,3-Diamino-2-hydroxypropane pro-drug derivatives
The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are ...
11/13/2007
7285565Benzamides and related inhibitors of factor Xa
Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders. ...
10/23/2007
7279578Sulfonylamino-acetic acid derivatives
The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmac...
10/09/2007
7268237Direct dianhydride synthesis
This invention is related to a method for making diether dianhydrides by the reaction of halophthalic anhydride and a metal salt of an aromatic dihydroxy compound in the presence of a solvent and a phase transfer catalyst. Typical phase transfer catalyst include gua...
09/11/2007
7268147Compounds useful for the treatment of diseases
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds accord...
09/11/2007
7268135Biaryl sulfonamides and methods for using same
The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors. ...
09/11/2007
7265122Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use. ...
09/04/2007
7265136Substituted stilbene compounds with vascular damaging activity
A compound for use in inducing necrosis in vascular tissue of a tumor in an animal. The compound contains a first moiety which is a cis-stilbene moiety and a second moiety which is an inhibitor of the formation or action of nitric acid. Also, a method for inducing n...
09/04/2007
7262209Carbonyloxy-cyanomethyl compounds as antiparasitic agents
The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances gi...
08/28/2007
7256192Aromatic diamide derivatives, chemicals for agricultural or horticultural use and usage thereof
The present invention relates to an aromatic diamide derivative represented by the general formula (I): [A1 is optionally substituted (C1-C8)alkylene grou...
08/14/2007
7226936Pyridinic sulfonamide derivatives method of production and use thereof
New pyridinic sulfonamide derivatives represented by a general formula (I), wherein R1, represents a mono- or polyhalogenated C1–12-alkyl or a mono- or poly-halogenated C3–8-cycloalkyl group. The method of production of such derivatives and their use as active t...
06/05/2007
72237785-substituted-2-arylpyridines
Novel 5-substituted-2-arylpyridine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyridine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particula...
05/29/2007
7223788Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have...
05/29/2007
7220863Process for preparing 2-aminopyridine derivatives
A method for preparing 2-aminopyridine derivatives, which comprises substituting of fluorine for hydrazine moiety and reducing with hydrogen using 3-substituted-2,5,6-trifluoropyridine as a starting material, provides 2-aminopyridine derivatives having a purity over...
05/22/2007
7214693Heterocyclic selective androgen receptor modulators and methods of use thereof
This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and a...
05/08/2007
7208507Pyridines and uses thereof
The invention relates to pyridines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor cells. ...
04/24/2007
7205411Aminopyridine derivatives as mGluR5 antagonists
The invention relates to novel aminopyridine derivatives of formula (I) wherein R1 is methyl an R4 and amino group —NR6R7 and R5 forms an arylalkynyl- or heteroarylalkynyl-group. The compounds are useful in the pr...
04/17/2007
7186834Substituted iminoazines
The invention relates to novel substituted iminoazines of the general formula (I) in which R1, R2, R3, R4, Z1, Z2 and Z
03/06/2007
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