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Patent No. 6125480

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Class 514/386 - Divalent chalcogen or acyclic nitrogen double bonded directly to ring carbon of the diazole ring, or tautomeric equivalent


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a ring carbon of the 1,3-diazole
No. of patents: 177
Last issue date: 05/01/2012


1          
NumberTitleIssue Date
8168666Substituted carbinol compound
There is provided a novel LXRβ agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by infl...
05/01/2012
8158666Process for the preparation of (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-YL)-1,3-dihydroimidazole-2-thione
A process for making (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione and pharmaceutically acceptable salts thereof, and for making intermediates useful in the formation of said compound. ...
04/17/2012
8129423Imidazolone and imidazoloidinone derivatives as 11b-HSD1 inhibitors
Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositio...
03/06/2012
81196744-phenylimidazole-2-thione tyrosinase inhibitors and pharmaceutical/cosmetic applications thereof
Novel 4-phenylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigm...
02/21/2012
79894834-heteroarylimidazole-2-thione tyrosinase inhibitors and pharmaceutical/cosmetic applications thereof
Novel 4-heteroarylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of ...
08/02/2011
7968580Imidazolidin-2-one derivatives as selective androgen receptor modulators (SARMS)
The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmace...
06/28/2011
7947722Imidazolidinone derivative, method of producing the same and method of producing optically active amino acid
The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino...
05/24/2011
7928132Methods for the amelioration of episodes of acute or chronic ulcerative colitis
Methods of ameliorating episodes of accute or chronic colitis are provided by using methimazole derivatives and tautomeric cyclic thiones in combination with another pharmaceutical compound. ...
04/19/2011
7902241Ureido substituted benzoic acid compounds and their use for nonsense suppression and the treatment of disease
The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions. ...
03/08/2011
78385454-(condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or s...
11/23/2010
7786157OXO-imidazolidines as modulators of chemokine receptors
The present invention provides compounds having formula (I): or pharmaceutically acceptable salts and N-oxides thereof, wherein the subscript m is an integer from 0-4; Ar is an optionally substitute...
08/31/2010
7723368Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase
The present invention provides compounds and methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles. ...
05/25/2010
7582667Dihydrospiro[dibenzo[a,d][7]annulene-5,4′-imidazol] compounds for the inhibition of beta-secretase
The present invention provides a 10,11-dihydrospiro[dibenzo[a,d][7]annulene -5,4′-imidazol]-5′(1′H)-one compound of formula I Also provided are methods and compositions for the inhibition of β-secretase (BACE) and the ...
09/01/2009
75695952-((2-thioxo-2,3-dihydro-1H-imidazol-4-yl)methyl)-3,4-dihydronaphthalen-1(2H)-one
A compound of the formula or a pharmaceutically acceptable salt thereof, is disclosed herein. Methods and compositions related thereto are also disclosed. ...
08/04/2009
7531565Imidazolidin-2-one derivatives as selective androgen receptor modulators (SARMS)
The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmace...
05/12/2009
74199944-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2- thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cyloalkenylmethyl) imidazol-2-ones and related compounds
Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in ...
09/02/2008
7417047Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for β-secretase modulation
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and ...
08/26/2008
7407963Cyclopropane CGRP antagonists, medicaments containing these compounds, and method for the production thereof
A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable p...
08/05/2008
7405233Ureido substituted benzoic acid compounds and their use for nonsense suppression and the treatment of disease
The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions. ...
07/29/2008
73968494-(Condensed cyclicmethyl)-imidazole-2-thiones acting as αadrenergic agonists
Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or s...
07/08/2008
7390829Alpha-2 adrenergic agonists
A compound is disclosed herein comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein R is OH or NH2. Methods, compositions, and medicaments related thereto...
06/24/2008
7390821Methods of reducing angiogenesis
The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associat...
06/24/2008
7390798Carboxamide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in...
06/24/2008
7358239Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is...
04/15/2008
73582692-((2-Thioxo-2,3-dihydro-1H-imidazol-4-yl)methyl)-3,4-dihydronapthalen-1(2H)-one
A compound of the formula or a pharmaceutically acceptable salt thereof, is disclosed herein. Methods and compositions related thereto are also disclosed. ...
04/15/2008
73234854-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic re...
01/29/2008
73234777-((1H-imidazol-4-yl)methyl)-5,6,7,8-tetrahydroquinoline
A compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed. ...
01/29/2008
73040832-iminoimidazole derivatives (2)
A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents h...
12/04/2007
7288559Carboxamide spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pha...
10/30/2007
7282592Resorcinol derivatives
The present invention relates to certain resorcinol derivatives and their use as skin lightening agents. ...
10/16/2007
72765224-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones, 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
The compound of the formula wherein the * indicates an asymmetric carbon, is specific to alpha2B adrenergic receptors in preference over alpha2A and alpha2C adrenergic receptors, ...
10/02/2007
7141561Substituted diaryl heterocycles, process for their preparation and their use as medicaments
This invention discloses and claims diary heterocycles of formula (I) and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of formula (I) for the t...
11/28/2006
7138421Anti-androgenic pyrrolidines with tumor-inhibiting action
This invention relates to anti-androgenic N-[ω-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounce...
11/21/2006
7125904Peripherally-selective inhibitors of dopamine-β-hydroxylase and method of their preparation
Compounds of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkyl...
10/24/2006
7115777Amide derivatives as inhibitors of the enzymatic activity of renin
The present inventions relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, the use and manufacture of a compound of formula (I) or a pharmaceutical composition comprising a c...
10/03/2006
7109227Imidazolamino compounds
The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds. ...
09/19/2006
7101875Methods for treating arthritic disorders
This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods ...
09/05/2006
70912324-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic re...
08/15/2006
7049332HIV inhibiting N-aminoimidazole derivatives
An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 ...
05/23/2006
7045534Methods of reducing angiogenesis
The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associat...
05/16/2006
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