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Class 514/273 - The nitrogen is part of a hetero ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the nitrogen is a part of a heterocyclic
No. of patents: 104
Last issue date: 03/17/2009


1      
NumberTitleIssue Date
75044112,3,6-Trisubstituted-4-pyrimidone derivatives
A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases ...
03/17/2009
7452897Use of substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives for the treatment of neurodegenerative diseases
The invention relates to therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are use...
11/18/2008
7432266Phosphodiesterase 4 inhibitors
Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs. ...
10/07/2008
7405222Methods and compositions for treatment of erectile dysfunction
Disclosed are methods and compositions for treatment of male sexual dysfunction. A method of treating male sexual dysfunction includes administering a pharmaceutical composition effective to cause said male to sustain an erection. The composition is formulated based...
07/29/2008
73784132-amino-3-(alkyl)-pyrimidone derivatives
A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; ...
05/27/2008
7211581Substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives
The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): wherein: R1 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R2 repres...
05/01/2007
7202251Bicyclic anilide spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds of the formula: that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache...
04/10/2007
7151096Cyclic compounds and compositions as protein kinase inhibitors
The invention provides a novel class of cyclic compounds, pharmaceutical compositions comprising such cyclic compounds and methods of using such compounds to treat or prevent diseases and disorders associated with cyclin-dependent kinases (CDKs) activity, particular...
12/19/2006
7135572Diaryl 1,2,4-triazole derivatives as a highly selective cyclooxygenase-2 inhibitor
The present invention relates to a novel diaryl 1,2,4-triazole derivative of the following formula 1 as a highly selective cyclooxygenase-2 inhibitor: Wherein, R1, R2, R3, R4...
11/14/2006
7115601HIV integrase inhibitors
Compounds of the present disclosure are spirocycle-substituted pyrimidinecarboxamides. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating HIV infection and AIDS. ...
10/03/2006
7091201Arylalkane-sulfonamides having endothelin-antagonist activity
The invention relates to novel aryl-alkane-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compos...
08/15/2006
7087597Pyrimidine 5-carboxamide compounds, process for producing the same and use thereof
Compounds of the formula wherein R1, R2, R3, R4, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be use...
08/08/2006
7067523Use of pyrone carboxylates for controlling pests
Pests can be controlled by applying an effective amount of a compound of formula (1): wherein R is C2–C6 alkyl, C3–C6 cycloalkyl, (C3–C6 cyc...
06/27/2006
70152284-amino-2-(2-pyridyl)pyrimidines as microbicidal active substances
Compounds of formula wherein R1 and R2 are each independently of the other hydrogen; unsubstituted or mono- or poly-halo-substituted C1–C20alkyl, C1â...
03/21/2006
6919329N-Aryl-2-oxazolidinone-5-carboxamides and their derivatives
The present invention provides antibacterial agents having the formulae I, II, and III described herein. ...
07/19/2005
6872729Pyrimidinylbenzimidazole and triazinylbenzimidazole derivatives and agricultural/horticultural fungicides
A pyrimidinylbenzimidazole or triazinylbenzimidazole derivative represented by the general formula (I): wherein A is N or CR3, and R1, R2, R3, X, Y and n are as defined in th...
03/29/2005
6852717Compounds useful as anti-inflammatory agents
Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds. ...
02/08/2005
6846829N-heterocyclic derivatives as NOS inhibitors
N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using the...
01/25/2005
68443352-amino-3-(alkyl)-pyrimidone derivatives as GSK3.β.inhibitors
A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C
01/18/2005
6818648Aryloxy- and arylthiosubstituted pyrimidines and triazines and derivatives thereof
The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl sy...
11/16/2004
67875392,4,5,-trisubstituted pyrimidine derivatives
The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)
09/07/2004
67650091,4-Disubstituted benzo-fused compounds
Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory dis...
07/20/2004
67563805-phenyl-pyrimidine derivatives
Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethy...
06/29/2004
6753332Sulfonyl heteroaryl triazoles as anti-inflammatory/analgesic agents
The present invention relates to compounds of the formula wherein R1, R3, R5 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicin...
06/22/2004
6716851Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defi...
04/06/2004
6613773Fungicides
The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: ##STR1## wherein X is CH2 O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an o...
09/02/2003
6548512Nitrogen containing heteroaromatics as factor Xa inhibitors
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(.dbd.NH)NH2, which are useful...
04/15/2003
6512000Aminocarbonyl-substituted benzimidazoles having tryptase-inhibitory activity
A method for treating diseases in which tryptase inhibitors may be of thereapeutic value, which comprises the administration of a thereapeutic amount of a compound of the formula ##STR1## The invention also comprises novel compounds of the formula (I). Exempla...
01/28/2003
6500440Topical preparation of alprostadil for the treatment of erectile dysfunction
The present invention relates to a composition of topical preparation containing alprostadil, which has excellent skin permeation rate with little skin irritation, which is prepared by dissolving alprostadil or a solid dispersion thereof prepared using po...
12/31/2002
6489347Process
##STR1## Compounds of structure (1) are obtained by reduction of compounds of the structures ##STR2## ##STR3## Compounds of structure (1), especially where Z is a hydrogen atom or a 3,4-methylenedioxyphenyl group, are important intermediates for inte...
12/03/2002
6482829Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
The invention relates to compounds of the formula ##STR1## as described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor....
11/19/2002
6432947N-heterocyclic derivatives as NOS inhibitors
N-Heterocyclic derivatives of the formula (I): ##STR1## are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors o...
08/13/2002
6432963Pyrimidine-5-carboxamide derivatives
Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof ##STR1## [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1 CO, CONR1, C.dbd.N--OR1 or a bond, Y: a l...
08/13/2002
6395736Compositions and methods for the treatment of anorectal disorders
Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O2-) scavengers, ଲ-adrenergic agonists, cAMP-dependent protein kinase activa...
05/28/2002
6395727Method of treating Bulimia Nervosa and related eating disorders by administration of atypical antipsychotic medications
The invention relates to a method of treating non-psychotic disorders by administration of atypical antipsychotic medications, in particular, risperidone. More specifically, the invention relates to a method of treating the eating disorder Bulimia Nervosa...
05/28/2002
6391879Therapeutic anti-fungal nail preparation
A therapeutic solution and application procedure for curing and preventing nail fungus and athlete's foot infections or Onychomycosis comprising a combination of an anti-fungal agent with DMSO in a anhydrous solution of Polyglycol. The DMSO acts as a solv...
05/21/2002
6372752Inha inhibitors and methods of use thereof
The invention relates to compounds which inhibit the Mycobacterial enoyl-ACP reductase required for cell wall biosynthesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of use of these compounds for t...
04/16/2002
6372751Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
This invention is directed to aryl and heterocyclyl substituted pyrimidine derivatives selected from the following formulae: ##STR1## wherein Z1, Z2, R1, R2, R3, R4, R5 and R
04/16/2002
6358942Phenyloxazolidinones having a c-c bond 4-8 membered heterocyclic rings
A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR1 ; R1 is H, C1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R1 is --(CH2)h
03/19/2002
6329379Hepatitis C inhibitor tri-peptides
Racemates, diastereoisomers and optical isomers of a compound of formula (I): ##STR1## wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alk...
12/11/2001
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