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Class 548/375.1 - Nitrogen attached indirectly to the diazole ring by acyclic nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached indirectly to the
No. of patents: 370
Last issue date: 03/27/2012


1                    
NumberTitleIssue Date
8143425Heterocyclic aromatic compounds useful as growth hormone secretagogues
Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1a
03/27/2012
7910747Phosphonate and phosphinate pyrazolylamide glucokinase activators
Pyrazoloamides are provided which are phosphonate and phosphinate glucokinase activators that are useful in treating diabetes and related diseases and have the structure wherein i...
03/22/2011
7790905Pharmaceutical propylene glycol solvate compositions
The invention relates to pharmaceutical compositions comprising propylene glycol solvates of APIs. ...
09/07/2010
7531669Methods for treating neural disorders and conditions, and compounds useful therefor
In accordance with the present invention, there are provided novel compounds that protect neurons and/or promote neuroregeneration and/or promote memory formation. Such compounds are useful for treatment of a variety of neural disorders and conditions. In another as...
05/12/2009
7476744Polymorphic crystalline forms of celecoxib
Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory compound of low water solubility in a therapeutically effective amount, wherein the compound is present in the form...
01/13/2009
7442802Cyclooxygenase-2 selective inhibitors, compositions and methods of use
The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulat...
10/28/2008
7432285Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use
The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that don...
10/07/2008
7399765Substituted diazabicycloalkane derivatives
Compounds of formula (I) Z-Ar1—Ar2  (I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substitute...
07/15/2008
7361769Heterocyclyls as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders
The present invention discloses compounds of formula I wherein m, n, p, R1, R2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as metho...
04/22/2008
7358371Process for the preparation of 1,5—carboxylic acid derivatives
The present invention comprises a process for the preparation of compounds that possess an affinity for the cannabinoid receptor in the human brain. These compounds are useful as immunomodulators and psychotropic agents in the treatment of thymic disorders, vomiting...
04/15/2008
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
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
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
7297710Derivatives of N-[(1,5-diphenyl-1H-pyrazol-3-yl)methyl]sulfonamide, their preparation and their application in therapeutics
The present invention relates to compounds corresponding to the formula (I): In which R1, R2, R3, R4 and R5 are as described herein. The invention also relates to the m...
11/20/2007
7294645Derivatives of N′-(1,5-diphenyl-1H-pyrazol-3-yl) sulfonamide with CB1 receptor affinity
The invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 are as defined here...
11/13/2007
7271191Pyrazole derivatives as gamma-secretase inhibitors useful in the treatment of Alzheimer's disease
The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease. ...
09/18/2007
7253170Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5...
08/07/2007
7247628Cannabinoid receptor ligands and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment diseases, conditions and/or disorders herein. ...
07/24/2007
7247635Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors conta...
07/24/2007
7241793Phenyloxyalkanonic acid derivatives as hPPAR activators
A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein: ...
07/10/2007
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
7220867Solid-state form of celecoxib having enhanced bioavailability
The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallizatio...
05/22/2007
7211598Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use
The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor having at least one oxime group or hydrazone gr...
05/01/2007
7208528Polyamine analogues as therapeutic and diagnostic agents
Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine t...
04/24/2007
7202236Modified release pharmaceutical formulation
A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R1 represents C?1-2#191 alkyl substituted by one or more fluoro substituents; R2 represents hydrogen, hydroxy, methoxy or ethoxy;...
04/10/2007
7192906Substituted pyrazole derivatives, production process thereof, and herbicide compositions containing the derivatives
Substituted pyrazole compounds of the formula (1). The compounds are synthesized from a pyrazole derivative and a haloalkyleneoxime ester derivative, and have excellent herbicidal effects. Herbicide compositions containing the substituted pyrazole derivatives or hyd...
03/20/2007
7183306Pyrazole derivatives
A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; ...
02/27/2007
7179825Retinoic acid mimetic anilides
The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3
02/20/2007
7151113Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5...
12/19/2006
7138414Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals
The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the formula I whe...
11/21/2006
7129233Mandelic acid derivatives and their use as thrombin inhibitors
There is provided a compound of formula I wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including pro...
10/31/2006
7122547Anthranilic acid amides and the use thereof as medicaments
The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides. ...
10/17/2006
7109349Process for obtaining Cizolirtine and its enantiomers
A process is described for the preparation of a precursor alcohol of Cizolirtine, (±)-2-[phenyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethylethanamine and its enantiomers. The process involves the asymmetric addition of a metalated phenyl reagent to a pyrazolcarb...
09/19/2006
7102026Process for preparing and isolating -bicalutamide and its intermediates
The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{...
09/05/2006
7078531Process for obtaining enantiomers of thienylazolylalcoxyethanamines
A process is described for the preparation of a precursor alcohol of (±)-2-[thienyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethyletanamine and in general for thienylazolylalcoxyethanamines and their enantiomers. The process involves asymmetric addition of a metala...
07/18/2006
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
7056932Heterocyclyl substituted 1-alkoxy acetic acid amides
The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as ...
06/06/2006
7045532ACE-2 modulating compounds and methods of use thereof
ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-Λ  (I) Wherein Z is...
05/16/2006
70418333-step synthesis of pyrazolotriazole couplers and coupler intermediates
A process and intermediate useful for forming a 1H-Pyrazolo[1,5-b][1,2,4]triazole compounds comprise the step of reacting a 1,5-diaminopyrazole bearing a substituent, bonded to one and only one of the amine nitrogens by an acyl or thioacyl group, with a dehydrating ...
05/09/2006
7030239Compounds to treat Alzheimer's disease
The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases. ...
04/18/2006
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