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Class 546/282.1 - The additional hetero ring is six-membered


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein six ring atoms are present in the additional
No. of patents: 250
Last issue date: 01/10/2012


1              
NumberTitleIssue Date
8093394Derivatives of 5-thioxylopyranose and use of same for treatment
The invention relates to new compounds of 5-thioxilose, preferably derivatives of the 5-thioxilopyranose type, and to a method for preparing the same and their use as the active ingredient of drugs mainly intended for treating or inhibiting thrombosis or heart failu...
01/10/2012
78516345-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide derivatives as renin inhibitors for the treatment of hypertension
The application relates to novel alkanamides of the general formula (I) where X is —CH2— or >CH—OH; (A) R1 is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical whe...
12/14/2010
73751002-amino-pyridine derivatives 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 according to the ...
05/20/2008
73685756-alkylamino-2,2′-disubstituted-7,8-disubstituted-2H-1-benzopyran derivatives as 5-lipoxygenase inhibitor
When a multi-step process reaction is carried out in a solution, it generally requires several treatments and purification procedures to go through with after the reaction, however, the inventive method for preparing 2,2′-disubstituted-3,4-dihydro-7,8-disubstitute...
05/06/2008
7358359Antibacterial agents
Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacteria...
04/15/2008
73549362-phenylpyran-4-one derivatives
The present invention relates to 2-(4-sulphonylphenyl)pyran-4-one derivatives of general formula processes for their preparation, pharmaceutical compositions containing them, and their medical uses. ...
04/08/2008
7329675Substituted azabicyclic compounds
This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members...
02/12/2008
7259166Substituted-cycloalkyl and oxygenated-cycloalkyl glucokinase activators
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of...
08/21/2007
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
7186737Inhibitors 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 inhibitors of ZAP70. The invention also relates to methods for producing these...
03/06/2007
7186709Dihydropyrancarboxamides and uses thereof
The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R...
03/06/2007
7166726Aryl substituted 3,4-dihydroanthracene derivatives having retinoid antagonist or retinoid inverse agonist type biological activity
Disclosed herein are compounds of the formula wherein R1 is independently H or alkyl of 1 to 6 carbons; R2 is optional and is defined as lower alkyl of 1 to 6 carbons, F, Cl, Br...
01/23/2007
7132420Aspartic protease inhibitors
The present invention provides an aspartic proteinase-inhibiting compound of the formula: wherein a, b, c, d, and e, can be the same or different and each are R7, OR7, SR7, NR
11/07/2006
7115637Inhibitors 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...
10/03/2006
7091221Partial ester of cellulose with nitrogenous carboxylic acid and process for producing the same
According to the present invention, there are provided a novel partial ester of a nitrogenous carboxylic acid ester with cellulose, the partial ester being useful as an antibacterial agent, a flame retardant, etc., and a simple and convenient process for preparing t...
08/15/2006
7034035Fungicidal mono-, bi-, and tri-cycloheteroalkyl amides and their compositions, methods of use and preparation
The present invention relates to compounds of Formula I: wherein: a)  represents a 6-membered heterocyclic aromatic ring in w...
04/25/2006
7026476Intermediate arylamine compounds
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes...
04/11/2006
6995162Substituted alkylamine derivatives and methods of use
Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical composit...
02/07/2006
6953798β-alanine derivates
Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra′)R  (1) Ar1 is an optionally substituted aromatic or...
10/11/2005
6942980Methods of identifying compounds having nuclear receptor negative hormone and/or antagonist activities
Methods of characterizing and identifying negative hormones of nuclear receptors. Also disclosed are methods of making modulators of retinoid nuclear receptor transactivation activity, assays for agonists, antagonists, and negative hormones of the RAR receptor, and ...
09/13/2005
69193712,6-substituted chroman derivatives useful as beta-3 adrenoreceptor agonists
This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions. ...
07/19/2005
69169334-pyridinyl-n-acyl-l-phenylalanines
Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4. ...
07/12/2005
6890928Aromatic sulfone hydroxamic acids and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This inventi...
05/10/2005
6878714Substituted alkylamine 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...
04/12/2005
6833367Certain substituted polyketides, pharmaceutical compositions containing them and their use in treating tumors
The present invention relates to certain substituted polyketides of formula I, wherein A, B and C are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating ...
12/21/2004
6689889Chromatographic separation of enantiomers of lactones
The present invention relates to the use of optically active polymers of N-acryloyl-phenylalanine neomenthylamide as such, in crosslinked form and/or in carrier-bonded form as stationary phases for the chromatographic separation of enantiomers of lactones...
02/10/2004
6689794Aromatic sulfone hydroxamates and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamates (also known as "aromatic sulfone hydroxamic acids") and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as "matrix metalloprotease" or "MMP") activity and/or aggrecan...
02/10/2004
6680338Hydroxamic and carboxylic acid derivatives
Compounds having therapeutic utility are of formula (I) wherein n=0-1; X is S(O)0-2 ; Y is OR1 or NHOH; R2 and R4 are independently H or a group (optionally substituted with R10) selected from C...
01/20/2004
6632945Inhibitors 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...
10/14/2003
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
65968732-and 2,5-substituted phenylketoenols
The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) ##STR1## in which Het represents one of the groups ##STR2## in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and interme...
07/22/2003
6534445Substituted pyridine herbicides
##STR1## Compounds of formula (I), in which the substituents are as defined in claim 1 and the agrochemically tolerated salts M+ and all stereoisomers and tautomers of the compounds of formula (I) are suitable for use as herbicides....
03/18/2003
6518431Process for preparing substituted pyridines
A process for preparing a compound of the formula ##STR1## wherein n, R1, R2, R3 and X are as defined above, used as an intermediate in the synthesis of ଲ-adrenergic receptor agonists....
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
6495568Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
Compounds of formula (I): ##STR1## or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH...
12/17/2002
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
6486332Fluorescent pigments
Compounds of formula A(B)x, (I) wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which ...
11/26/2002
6465509Pyrones as inhibitors of cyclooxygenase-2
The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as m...
10/15/2002
6458950Compounds and pharmaceutical compositions containing the same
A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen,...
10/01/2002
6451792Medical composition containing nitroetheneamine derivative or salt thereof as active constituent
A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): ##STR1## wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof....
09/17/2002
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