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Class 562/430 - Nitrogen


Subclass of Class 562 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the acid also contains nitrogen.
No. of patents: 492
Last issue date: 09/30/2008


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NumberTitleIssue Date
7429677Small molecule entry inhibitors
The present invention concerns a compound having the formula (I) a N-oxide form, a stereochemical isomer, racemic mixture, salt, prodrug, ester or metabolite thereof. It further relates to processes for their preparation as...
09/30/2008
7417164Fluorescent dyes for use in glucose sensing
A novel class of compounds that includes HPTS-Cys-MA, and methods of making them are disclosed herein. The class of compounds including HPTS-Cys-MA are useful as fluorescent dyes for analyte detection. ...
08/26/2008
7388008Lysine 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
7375248Inhibitors of matrix metalloproteinase
Compounds of formula (I): wherein R1 represents optionally substituted C4-12 alkyl, optionally substituted C2-6alkylaryl, or optionally substituted 5- or 6-membered aryl or hete...
05/20/2008
7371888α-(Trifluoromethyl-substituted aryloxy, arylamino, arylthio or arylmethyl)-trifluoromethyl-substituted phenylacetic acids and derivatives as antidiabetic agents
Compounds having a formula: or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders. ...
05/13/2008
7351825Cyclopropane 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
7342127Substituted anilide ligands for the thyroid receptor
Novel thyroid receptor ligands are provided having the general formula I wherein X, R1, R2, R3, R4, R5, R6, R7,...
03/11/2008
73389653,4-disubstituted, 3,5-disubstituted and 3,4,5-substituted piperidines
The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precu...
03/04/2008
7321001Asthma and allergic inflammation modulators
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins inv...
01/22/2008
7297817Thio-substituted arylmethanesulfinyl derivatives
The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein ...
11/20/2007
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
7262317Freeze-dried preparation of n[o-(p-pivaloyloxybenzenasulfonylamino) benzoyl] glycine monosodium salt tetrahydrate and process for producing same
A method for the preparation of a freeze-dried product of N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate dissolved in a mixed solvent of water and ethanol, and the freeze-dried product obtained by the method. According t...
08/28/2007
7250439Matrix metalloproteinase inhibitors
Compounds of formula (I): wherein: Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, NR5 or CR...
07/31/2007
72178325-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation
The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group;
05/15/2007
7199158Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7′, R8, R30–R34, X′, Y, Y′, t,...
04/03/2007
7199265Thyroid receptor ligands, pharmaceutical compositions comprising them and their use in the treatment of disorders influenced by thyroid hormones
This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor β, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of m...
04/03/2007
7193108Phenylpropionic acid derivatives
Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to α 4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α 4 integrin, such as inflammatory diseases in which α 4 integ...
03/20/2007
7157454Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same
The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal pr...
01/02/2007
7153869Substituted 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
7071358Arylsulfonamidobenzylic compounds
Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases. ...
07/04/2006
7064229Succinic acid derivatives
The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseases ...
06/20/2006
7056903Carboxylic acid derivatives as IP antagonists
This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 ...
06/06/2006
7041691Compounds for the modulation of PPARγ activity
Modulators of PPARγ activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity. ...
05/09/2006
7022851PNA monomer and precursor
This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers:
04/04/2006
6974828Propanoic acid derivatives as intergrin receptor antagonists
Novel propanoic acid derivatives are integrin receptor antagonists or inhibitors, in particular of the avb3 integrin receptor. The compounds of the invention are for instance useful for the treatment of solid tumors by inhibition of angiogenic growth of tumor vessel...
12/13/2005
6951886Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors and in particular as inhibitors o...
10/04/2005
6919375Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same
Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof. ...
07/19/2005
6919369Serine protease inhibitors
Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
07/19/2005
6890942Acyl sulfonamides as inhibitors of HIV integrase
The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integr...
05/10/2005
6887903N-(2-aryl-propionyl)-sulfonamides and pharmaceutical preparations containing them
The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN ...
05/03/2005
6887877Compounds and methods for the treatment or prevention of Flavivirus infections
The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection. ...
05/03/2005
6884907Hydroxamic acids and acyl hydroxamines as naaladase inhibitors
This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neurona...
04/26/2005
6884821Carboxylic acid derivatives and drugs containing the same
Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydro...
04/26/2005
6881727Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same
Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof. ...
04/19/2005
6875765Arylsulfonamide ethers, and methods of use thereof
The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1β converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized s...
04/05/2005
6875764Urea and thiourea compounds useful for treatment of coccidiosis
The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coc...
04/05/2005
6875760Glucagon antagonists/inverse agonists
A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated co...
04/05/2005
6838483Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same
Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof. ...
01/04/2005
6806365N-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
6806291Analgesic compounds, their synthesis and pharmaceutical compositions containing them
New analgesic compounds, which are prepared by the hydrolysis of N-acylated 4-hydroxyphenylamine derivatives, their synthesis and pharmaceutical compositions containing them are disclosed. These compounds surprisingly possess high analgesic activity with little hepa...
10/19/2004
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