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Class 514/385 - 1,3-diazoles


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the five-membered hetero ring is
No. of patents: 342
Last issue date: 11/22/2011


1                  
NumberTitleIssue Date
8063084Heterocyclic compounds suitable for the treatment of diseases related to elevated lipid levels
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also ...
11/22/2011
8039498Imidazole compounds
Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
10/18/2011
8026265Heterocycle substituted ketone derivatives as histone deacetylase (HDAC) inhibitors
The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, inclu...
09/27/2011
8017639Imidazole compounds
Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
09/13/2011
7935718Treatment of dyskinesia
The present invention relates to the use of compounds that enhance H3-histamine receptor activity, or activation (e.g. H3-histamine receptor agonists) for the treatment of dyskinesia. The compounds are particularly useful for treating dyskinesi...
05/03/2011
7928131Imidazole compounds
Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
04/19/2011
7812046PPAR ligands that do not cause fluid retention, edema or congestive heart failure
Methods are provided for treating or prophylactically preventing metabolic disorders in humans without causing, promoting, or aggravating fluid retention, peripheral edema, pulmonary edema, or congestive heart failure, by administration of a therapeutically effectiv...
10/12/2010
7776899Methods for treatment of erectile dysfunction
Improved drug compositions and methods useful in the treatment of male erectile dysfunction. An optimized mixture of the drugs phentolamine mesylate, papaverine hydrochloride, and alprostadil in a buffer containing L-arginine and glycine is to be injected into the p...
08/17/2010
7754750Metalloproteinase inhibitors
Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12. ...
07/13/2010
7718684Methods and materials for assessing prostate cancer therapies and compounds
A modest (2-5 fold) increase in androgen receptor (AR) mRNA is the only expression change consistently associated with developing resistance to antiandrogen therapy. Increased levels of AR confer resistance to anti-androgens by amplifying signal output from low leve...
05/18/2010
7709514Therapeutic molecules and methods-1
Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) as defined herein, is provided. The invention also relates to methods of treating diseases or condition...
05/04/2010
7662844Naphthylene derivatives as cytochrome P450 inhibitors
Compounds of the formula and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G1, Q1, Z, R1, R2, R3, R4a, R
02/16/2010
7625934Metalloproteinase inhibitors
Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12. ...
12/01/2009
7622491Modulators of PPAR and methods of their preparation
The present invention is directed to certain novel compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceu...
11/24/2009
7579368Cis-imidazolines
There are presented compounds of the formula or pharmaceutically acceptable salts thereof, wherein Y1, Y2, X1, X2, X3 and R are as described in this applicati...
08/25/2009
7563814Olmesartan medoxomil with reduced levels of impurities
The present invention provides the preparation of olmesartan medoxomil containing less than about 0.1% of one or more of the impurities OLM-Me, OLM-Cl, and OLM-eliminate. ...
07/21/2009
7541375Azole derivatives and pharmaceutical compositions containing them
The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or prevent...
06/02/2009
75110673-hydroxymethyl-4-hydroxy-phenyl-derivatives for the treatment of respiratory diseases
The present invention relates to the use of the compounds of general formula 1 wherein the groups R1, X and Y may have the meanings given in the claims and in the specification, for preparing a pharmaceutical com...
03/31/2009
7507756Scalable synthesis of imidazole derivatives
Imidazole derivatives, compositions containing them, methods of preparing them, including regioselective scale-up synthetic methods, and methods of using them. ...
03/24/2009
7504425Compounds useful in the treatment of anthrax and inhibiting lethal factor
This invention relates to compounds of formula (I), and a method for treating anthrax or inhibiting lethal factor by administrating a composition containing a compound of formula (I) and a pharmaceutically acceptable carrier. This invention further relates to the us...
03/17/2009
7485657Anti-cytokine heterocyclic compounds
Disclosed are compounds of formula (I) The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as ch...
02/03/2009
74427162-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to t...
10/28/2008
7427631Metalloproteinase inhibitors
Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12. ...
09/23/2008
7419995N-substituted benzimidazoyl c-Kit inhibitors and combinatorial benzimidazole library
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors. Combinatorial libraries composed of compounds represented by Formula (I) or benzimidazol...
09/02/2008
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
7417030Indazole peptidomimetics as thrombin receptor antagonists
The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, athero...
08/26/2008
7390506Lipophilic drug compositions
The invention is directed to biologically active lipophilic compositions comprising a biologically active covalently attached to, or encapsulated within, a lipid. Preferably, a biologically active agent is both covalently attached to a lipid and encapsulated within ...
06/24/2008
7390824Method for treating diabetes employing an aP2 inhibitor and combination
A method is provided for treating diabetes and related diseases, especially Type II diabetes, employing an aP2 inhibitor or a combination of an aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin. ...
06/24/2008
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
7390908Compounds effecting glucokinase
The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or preventio...
06/24/2008
7368467Ion channel modulators
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and...
05/06/2008
7361663N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions cont...
04/22/2008
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
73450774-(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 receptors in ...
03/18/2008
7345072Phenyltetrazole compounds
Novel phenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists and the processes for the conversion thereof to biologically active molecules. ...
03/18/2008
7326696Amino-methyl substituted tetracycline compounds
Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed. ...
02/05/2008
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
7323433R-(-)-1-[2-(7-chlorobenzo[b]thiopen-3-yl-methoxy)-2-(2,4-dichlorophenyl)-ethyl]-1H-imidazole
The invention relates to R-(−)-1-[2-(7-Chloro-benzo[b]thiophen-3-yl-methoxy)-2-(2,4-dichloro-phenyl)-ethyl]-1H-imidazole and the salts thereof. The invention also relates to compositions thereof and their use either for treating fungal infections in humans and ani...
01/29/2008
7317032Imidazolyl inhibitors of 15-lipoxygenase
The present invention provides imidazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions. ...
01/08/2008
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