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Class 564/237 - Benzene ring containing


Subclass of Class 564 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a guanidine contains a benzene ring.
No. of patents: 108
Last issue date: 12/07/2010


1      
NumberTitleIssue Date
7847124Alanine racemase chiral binaphthol derivative with powerful hydrogen bond donor, and optical resolution and optical transformation methods using the same
Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcoh...
12/07/2010
7351743Therapeutic guanidines
The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines. ...
04/01/2008
7285682Terphenyl guanidines as β-secretase inhibitors
The present invention provides terphenyl guanidine compounds of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibril...
10/23/2007
7153881Compounds acting as melanocortin receptor ligands
The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH2
12/26/2006
7109329Neurologically active compounds and compounds with multiple activities
This invention provides pharmacologically active compounds having neurological and other bio-active capability. These active compounds comprise the derivatives of guanidino, aminoguanidino, 2-imadazolino, 2-hydrazinoimidazolino or 2-guanidinobenzimidazolino groups.
09/19/2006
7078566Salts of guanidine derivatives and pharmaceutical preparations consisting thereof
This invention relates to salts of guanidine derivatives of formula R—X—C(═NH)NH3+Z−, wherein X represents a valence bond, —CH2—NH—, —CH2—NH—NH— or —CH═N—NH—; R represents a linear ...
07/18/2006
6906076Compounds and methods of use to treat infectious diseases
The present invention concerns alkyl aryl carbonyl compounds that possess anti-infective activity. The compounds of the invention can be used to target specific nuclear localization signal, thereby blocking importation of specific proteins or molecular complex into ...
06/14/2005
6849733Neuropeptide-Y ligands
There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of...
02/01/2005
6787569Therapeutic guanidines
The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines. ...
09/07/2004
6774263Pharmaceutically active compound and methods of use
This invention relates to racemic and optically active N-(2-chloro-5-methylthiophenyl)-N′-(3-methylsulfinylphenyl)-N′-methylguanidine, N-(2-chloro-5-methylsulfinylphenyl)-1-(7-trifluoromethyl- 1,2,3,4-tetrahydroquinolinyl)carboximidamide, and N-(3-methylsulfinyl...
08/10/2004
6768024Triamine derivative melanocortin receptor ligands and methods of using same
The invention provides triamine derivative melanocortin receptor ligands of the formula: wherein R1 to R8 and n have the meanings provided herein. The invention further provides methods of using the...
07/27/2004
6706765Aminoguanidines and alkoxyguanidines as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra
03/16/2004
6680408Processes for the preparation of ଱-substituted benzylnitroguanidines
Processes for preparing ଱-substituted benzylnitroguanidines include the steps of providing a reaction mixture comprising water, alcohol, an S-alkyl nitroisothiourea, and an ଱-substituted benzylamine; heating the reaction mixture; steam distill...
01/20/2004
6673968Method of producing n-(4,5-bis-methanesulfonyl-2-methyl-benzoyl)-guanidine, the hydrochloride thereof
The present invention relates to an NHE-1 selective Na+/H+ antiporter inhibitor N-(4,5-bismethanesulfonyl-2-methylbenzoyl)guanidine, hydrochloride, to its hydrochloride hydrate, and to a process for the preparation....
01/06/2004
6632840Monoacyl-substituted guanidines, a process for their preparation, their use as a medicament or diagnostic aid, and pharmaceutical compositions containing them
Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: ##STR1## in which X(2) is ##STR2##...
10/14/2003
6573404Method for producing ortho-alkylated benzoic acid derivatives
The invention relates to a process for the preparation of ortho-alkylated benzoic acid derivatives of the formula I ##STR1## characterized in that an aryl bromide of the formula II ##STR2## is reacted with a secondary or tertiary organolithium compound an...
06/03/2003
6570038Aqueous hexasubstituted guanidinium chlorides and methods for their preparation and use
Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful a...
05/27/2003
6436999Diacyl-substituted guanidines, a process for their preparation, their use as medicine or diagnostic aid, and medicine containing them
Diacyl-substituted guanidines of the formula I ##STR1## are described where X(1) and X(2) are ##STR2## as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis...
08/20/2002
6420556Acyl isothiocyanate resins and their use in solid-supported synthesis of guanidines
##STR1## The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed ...
07/16/2002
6369110Substituted guanidine derivatives and process for producing the same
A compound represented by the general formula (1): ##STR1## wherein each of R1, R2, R3, R4 and R5 is a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a c...
04/09/2002
6346527Guanidine derivatives
A compound of the formula: ##STR1## wherein R1 is hydrogen or halogen, R2 is hydroxy, acyl(lower)alkoxy, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkylthio(lower)alkyl, mono(or di or tri)halo(lower)alkyl, (ethoxycarbonyl)...
02/12/2002
6288123Therapeutic guanidines
The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines....
09/11/2001
6251948Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists
Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induce...
06/26/2001
6235934Aqueous hexasubstituted guanidinium chlorides and methods for their preparation and use
Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful a...
05/22/2001
6218426Non-peptide GnRH agents
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and are defined variables: ##STR1## Such compounds and their pharmaceutically acceptabl...
04/17/2001
6204384Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)
The present invention provides peptide aldehydes having an 3-amino-2-hydro yenyl acetamide group as part of the peptide backbone d an arginine group or analog at P1. These compounds e potent and specific or inhibitors of thrombin. Ther pharmaceutically ac...
03/20/2001
6187955Guanidine derivatives and process for their production
A guanidine derivative represented by formula (1), (2), (3) or its acid addition salt and a production process thereof ##STR1## wherein each of A and B is a C2 -C8 alkylene, D is a single bond, --CO-- or a C1 -C6
02/13/2001
6174924Therapeutic guanidines
The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines....
01/16/2001
6166239Oligonucleotide protecting groups
Compounds of the invention having general formula ##STR1## are useful reagents for protecting amine, guanidine, amidine or hydroxyl groups during organic synthesis. In particular, compounds are useful during oligonucleotide synthesis to protect nucle...
12/26/2000
6166088Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants
This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and...
12/26/2000
61568004-fluoroalkyl-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them
There are described benzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SOm, R(5)R(6)N--SO2 --; Op --(CH2)q --(CF2)r --CF3 ; --SR(10), --OR(10) or --C...
12/05/2000
6143932Selectively N-alkylated peptidomimetic combinatorial libraries and compounds therein
The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial ris...
11/07/2000
6121489Selectively N-alkylated peptidomimetic combinatorial libraries and compounds therein
The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial ris...
09/19/2000
6118007Preparation process of nitroguanidine derivatives
A process, as a substitute for hydrolysis, for preparing a nitroguanidine derivative represented by the following formula (2): ##STR1## wherein A represents a substituted or unsubstituted aromatic or non-aromatic hydrocarbon ring, a substituted or un...
09/12/2000
6114392Agmatine, and polyaminoguanidine-bound heterocyclic compounds for neurotrauma and neurodegenerative diseases
The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia). The invention further provides novel compounds of general formula I...
09/05/2000
6075054Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them
Benzoylguanidines of formula I ##STR1## with R(1) to R(4) as defined in the specification, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment as well as for the treatment o...
06/13/2000
6013675Therapeutic substituted guanidines
The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines....
01/11/2000
6011059Acyl guanidine sodium/proton exchange inhibitors and method
Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; an...
01/04/2000
5998481Fluoroalkyl/alkenyl-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them
There are described benzoylguanidines of the formula I ##STR1## having the definitions of R(1) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II ##STR2## with guanidine...
12/07/1999
5955507Therapeutic substituted guanidines
The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines....
09/21/1999
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