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Class 546/283.4 - The additional hetero ring is five-membered


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein five ring atoms are present in the additional
No. of patents: 472
Last issue date: 07/08/2008


1                      
NumberTitleIssue Date
7396936Modulators of calcitonin and amylin receptor activity
In various aspects, the present invention relates to non-peptidic compounds, which modulate calcitonin and amylin receptor activity; to processes for the preparation of some such compounds; and to pharmaceutical compositions including such compounds. Compounds of th...
07/08/2008
7375105Pyridine substituted furan derivatives as Raf kinase inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R
05/20/2008
7345059Diphenylpyridine derivatives, preparation and therapeutic application thereof
The invention relates to 5,6-diphenylpyridine-3-carboxamide derivatives of general formula (I): where: R1 represents hydrogen or a (C1-C4)alkyl; ...
03/18/2008
7332608Anthranilamides and methods of their use
The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and p...
02/19/2008
7297694Pyridylfurans and pyrroles as Raf kinase inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. ...
11/20/2007
7235690Anthranilamides and methods of their use
The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations con...
06/26/2007
7214678Arylsulfanyl and heteroarylsulfanyl derivatives for treating pain
According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.
05/08/2007
7205305Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
04/17/2007
7196089EPreceptor antagonists
Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O...
03/27/2007
7169798Inhibitors of c-Jun N terminal kinases (JNK) and other protein kinases
The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described be...
01/30/2007
7109220Amino substituted pyridinyl methanone compounds useful in treating kinase disorders
The present invention provides amino substituted pyridinyl methanone compounds; pharmaceutical compositions comprising the compounds and methods of synthesis thereof. The compounds, which are cyclin dependent kinase (CDK) inhibitors, can be used to treat or ameliora...
09/19/2006
7087625Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formulas I–III: wherein A, B, D, R1, R
08/08/2006
7067540Substituted pyridinones
Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for ...
06/27/2006
7041702Pharmaceutically active compounds and methods of use
The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly usefu...
05/09/2006
7015320Process for the manufacture of optically active 3-substituted lactams by asymmetric hydrogenation of 3-alkylidenelactams
The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) process, comprising: contacting a compound of formula (II): ...
03/21/2006
6995179Dihydropyridine derivative
Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type...
02/07/2006
6989397Iron chelators and uses thereof
The present invention provides 2-pyridylcarboxaldehyde isonicotinoyl hydrazone (PCIH) analogues suitable for use as an in vivo iron chelators, the PCIH analogue having Formula 1: wherein R1 is an aromatic or heterocycli...
01/24/2006
6939867β3 agonists and uses thereof
Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with β-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and ...
09/06/2005
6927225Fungicidal 2-pyridyl alkyl amides and their compositions, methods of use and preparation
The present invention relates to compounds of Formula I: wherein: represents a 6-membered heterocyclic aromatic ring in which X1 is N, and X2, X
08/09/2005
6906089Triarylimidazole derivatives as cytokine inhibitors
Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2 and R3 are various substituent groups; and one of X...
06/14/2005
6903132Non-peptide GnRH agents, pharmaceutical compositions and methods for their use
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and ster...
06/07/2005
6900210Pyridinyl, pyrimidinyl and pyrazinyl amides as potassium channel openers
The present invention provides novel heterocyclic amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A, B and Z...
05/31/2005
6875768Phthalamide derivatives, intermediates in the production thereof, and agricultural/horticultural insecticides and method for using the same
Heterocyclic amine derivatives represented by general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Q represents an optio...
04/05/2005
6828332Piperidine derivatives as reuptake inhibitors
The present invention provides compounds of formula (I) and a method of inhibiting the reuptake of serotonin and antagonizing the serotonin receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula (I)...
12/07/2004
6797712Substituted amino-furan-2-yl-acetic acid and amino-thien-2-yl-acetic acid derivatives and their use in the treatment of migraine and pain
Compounds of formula I, or a pharmaceutically acceptable salt thereof, The compounds of the present invention are suitable for the treatment of pain and migraine. Also disclosed are method for preparing the compounds, an...
09/28/2004
67841376-aryl-4-aminopicolinates and their use as herbicides
4-Aminopicolinic acids having aryl or heteroaryl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control. ...
08/31/2004
6716987Derivatives of benzofuran or benzodioxazole compounds
An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1
04/06/2004
6680329N-(heterocyclyl)benzene or pyridinesulphonamides as antithrombotic agents and anticoagulants
Compounds of formula [I] ##STR1## in which: W may represent a --(CH2)2 --, --(CH2)3 --, --CH2 --C.ident.C-- or --CH2 --CH.dbd.CH-- group, R2 may in particular represent a pipe...
01/20/2004
6653302Quinoline and quinazoline compounds useful in therapy
Compounds of formula I, ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atom...
11/25/2003
6649633Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the form...
11/18/2003
6605625Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations comprising them
Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythm...
08/12/2003
6596863Medical composition containing nitroetheneamine Derivative or salt there of as active constituent
Process for producing a nitroetheneamine derivative ##STR1## or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula ##STR2## with a compound of the formula R6 --CH2 NO2 to obtain ...
07/22/2003
6518433Process for the preparation of nitroguanidine derivatives
A process for the production of a compound of formula (I) ##STR1## wherein R1 is hydrogen or C1 -C4 -alkyl; R2 is hydrogen, C1 -C6 -alkyl, C2 -C6 -alkenyl, C2 -C...
02/11/2003
6514996Derivatives of benzofuran or benzodioxole
An oxygen-containing heterocyclic compound represented by following Formula (I): ##STR1## wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, --(CH2)n --E1 --CO--G1 (whe...
02/04/2003
6498172Prostaglandin agonists and their use to treat bone disorders
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for t...
12/24/2002
6495576Aminal diones as potassium channel openers
Compounds of formula (I) ##STR1## may be useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal...
12/17/2002
6495550Pyridine-substituted benzanilides as potassium ion channel openers
The present invention provides a genus of pyridine-substituted benzanilides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods....
12/17/2002
6495571Pyridine compounds, use and preparation thereof
New pyridine compounds are provided along with their method of preparation. The compounds are useful as intermediates in preparing new anticancer agents. A few of the pyridine compounds are also useful for treating cancer....
12/17/2002
6492374Benzofuran derivatives, their preparation and use
The present invention relates to benzofuran derivatives having general Formula (I) ##STR1## wherein A is selected from (1), (2), (3), (4) ##STR2## wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6 -alkyl, C
12/10/2002
6489344Inhibitors of glycogen synthase kinase 3
New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the in...
12/03/2002
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