Class 546/323 - Acyclic nitrogen bonded directly to the carbonyl

Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which acyclic nitrogen is bonded directly to
No. of patents: 254
Last issue date: 04/06/2010

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Number	Title	Issue Date
7692020	Process for the preparation of pyridylcarboxylic amides and esters The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially...	04/06/2010
7414060	Pyridine-2-carboxyamide derivatives The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods...	08/19/2008
7388008	Lysine based compounds The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for exampl...	06/17/2008
7384945	Indole or benzimidazole derivatives as CB1 inverse agonists Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound...	06/10/2008
7378448	Diphenylether amide derivatives as opioid receptor antagonists A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3′, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mi...	05/27/2008
7351825	Cyclopropane compounds and pharmaceutical use thereof The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1):	04/01/2008
7320993	Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, ...	01/22/2008
7309800	Biphenylcarboxylic amide derivatives as p38 kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...	12/18/2007
7271289	Biphenylcarboxylic amide derivatives as p38 kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...	09/18/2007
7223774	Benzamide 2-hydroxy-3-diaminoalkanes The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the...	05/29/2007
7208629	5′-Carbamoyl-1,1-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, �...	04/24/2007
7183297	Biphenyl-derivatives as p38-kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...	02/27/2007
7166726	Aryl 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
7166590	Amino acid derivatives A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO,...	01/23/2007
7166623	2′-Methyl-5′-(1,3,4-oxadiazol-2-yl)-1,1′-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...	01/23/2007
7153869	Substituted amino acids as erythropoietin mimetics This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molec...	12/26/2006
7151118	Biphenylcarboxylic amide derivatives as p38-kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...	12/19/2006
7125898	Nicotinamide derivatives useful as p38 inhibitors. Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.	10/24/2006
7071219	Mono-acylated o-phenylendiamines derivatives Mono-acylated o-phenylendiamines derivatives of formula A wherein Ar, R1, and R2 are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of h...	07/04/2006
7071175	Pyridine mercapto carboxylic acids as carboxypeptidase U inhibitors The present invention relates to 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 prev...	07/04/2006
7015237	Pyridine matrix metalloproteinase inhibitors Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydrox...	03/21/2006
6995178	Insecticidal anthranilamides This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein A, B, J, R1, R2, R3 and R4 and n a...	02/07/2006
6992095	Stilbene compounds comprising an adamantyl group, compositions and methods thereof The invention relates to novel stilbene compounds having the general formula (I): as well as to pharmaceutical compositions for use in human or veterinary medicine, including dermatological, rheumatic, respiratory, card...	01/31/2006
6953798	β-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
6949539	Admantane derivatives The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compo...	09/27/2005
6949556	Acylated 1,2,3,4-tetrahydronaphthyl amines and their use as pharmaceutical agents The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C a...	09/27/2005
6942980	Methods 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
6936719	Biaryl compounds as serine protease inhibitors Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents. ...	08/30/2005
6933298	Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides and the use thereof for selectively inhibiting collagenases Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides of formula I. These compounds are found to possess the property of selectively inhibiting collagenase (MMP). They may therefore be useful in prophylaxis and therapy of diseases who...	08/23/2005
6894168	Carbamoyl tetrahydropyridine derivatives Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl...	05/17/2005
6806365	N-alkanoylphenylalamine derivatives Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related t...	10/19/2004
6780874	Enamine derivatives Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a ...	08/24/2004
6747041	Heterocyclic dicarboxylic acid diamide derivatives, agricultural/horticultural insecticides and method of using the same Heterocyclic dicarboxylic acid diamide derivative represented by the general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; ...	06/08/2004
6720425	Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity. ...	04/13/2004
6703379	Benzene derivatives and pharmaceutical use thereof The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammat...	03/09/2004
6642252	Acid derivatives useful as serine protease inhibitors Compounds having the formula (I), ##STR1## are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, IXa, Xa, and/or XIa, wherein ring B is phenyl or pyridyl, W is preferably C(.dbd.O)NR4 R5, L is a link...	11/04/2003
6632823	Substituted pyridine compounds useful as modulators of acetylcholine receptors In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered...	10/14/2003
6632816	Aromatic derivatives as HIV aspartyl protease inhibitors The present invention provides HIV aspartyl protease inhibitors of the formula; ##STR1## and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may b...	10/14/2003
6630493	Heterocyclically substituted amides, their preparation and use Amides of the general formula I ##STR1## and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, thei...	10/07/2003
6610700	Enamine derivatives Enamine derivatives of formula (1) are described: ##STR1## wherein R1 is a group Ar1 L2 Ar2 Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom ...	08/26/2003

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Class 546/323 - Acyclic nitrogen bonded directly to the carbonyl