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Class 514/401 - 2-imidazolines


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the 1,3-diazole ring contains one
No. of patents: 257
Last issue date: 02/08/2011


1              
NumberTitleIssue Date
7884122Extended release formulation and method of treating adrenergic dysregulation
A composition and method of treating adrenergic dysregulation by administering the composition is disclosed, wherein the composition comprises a a2-adrenergic receptor agonist; a pharmaceutically acceptable hydrophilic matrix and a release-retardant of a metal alkyl...
02/08/2011
7812049Method and therapeutic/cosmetic topical compositions for the treatment of rosacea and skin erythema using α-adrenoceptor agonists
The present invention is directed to the treatment of skin erythema as exhibited in rosacea and other conditions characterized by increased erythema (redness) of the skin. These conditions exhibit dilation of blood vessels due to a cutaneous vascular hyper-reactivit...
10/12/2010
7799816Imidazolinylmethyl aryl sulfonamide
This invention relates to an alpha-1 A receptor partial agonist, which is represented by Formula I: and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions con...
09/21/2010
7728028Substituted imidazoline compounds
Substituted imidazoline derivatives corresponding to Formula I: a method for producing them from substituted aldehyde compounds of Formula B: and the use of such imidazoline deriv...
06/01/2010
7652056Multi-substituted imidazolines and method of use thereof
A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The ...
01/26/2010
7528161NF-kappaB inhibitors and uses thereof
A new class of imidazolines as 4-position esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combinati...
05/05/2009
7439241Compounds, formulations, and methods for treating or preventing rosacea
In methods, compounds, and topical formulations for treatment of rosacea incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, ...
10/21/2008
7407980Imidazolinylmethyl aralkylsulfonamides
Compounds of the Formula: where R1-R6 are those defined herein and methods for producing the same. Also provided are pharmaceutical compositions comprising a Compound of Formula I and methods for their...
08/05/2008
7375125Melanocortin-4 receptor binding compounds and methods of use thereof
Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, ...
05/20/2008
7345078NF-κB inhibitors and uses thereof
A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The ...
03/18/2008
7312199Process for the production of (−)-epigallocatechin gallate
A process is provided for making (−)-epigallocatechin gallate (EGCG) by subjecting a green tea extract to chromatography on a macroporous polar resin, eluting EGCG from the resin with a polar elution solvent, optionally concentrating the eluate, optionally regener...
12/25/2007
7309706Method for the treatment of diseases requiring inhibition or a reduction in the activity of pH value-regulating bicarbonate transporter proteins
The use of selective imidazoline receptor agonists, such as moxonidine, rilmenidine, LNP-509, S-23515, PMS-812, PMS-847 and BU-98008, and their physiologically compatible acid addition salts in pharmaceutical preparations for the treatment and/or inhibition of funct...
12/18/2007
7304037Cytostatic conjugates with integrin ligands
The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to αvβ3 integrin antagonists via preferred linking units which can be selectively cleaved by elastase, i.e. by an enzyme which can especial...
12/04/2007
7291642Bradykinin-B1 antagonists, process for their preparation and their use as medicaments
The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and ...
11/06/2007
7262223Amidine derivatives for treating amyloidosis
The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a t...
08/28/2007
7252934Synergistic activation of regulatory elements by Rel proteins and a steroid receptor
Interaction of Rel proteins and steroid receptors is known to result in repression of target genes. Here we describe the discovery of a new mechanism in which Rel proteins and steroid receptors act synergistically to activate a regulatory element. This mechanism is ...
08/07/2007
7226947Use of creatine as a fat substitute
The invention relates to the use of creatine or creatine salts as a fat substitute to be given to breeding animals and feeder animals. The creatine or creatine salts are used as a substitute for flesh meal, fish meal and/or antimicrobial performance enhancers, growt...
06/05/2007
7125990Imidazolyl derivatives as corticotropin releasing factor inhibitors
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) usefu...
10/24/2006
7082330Implantable medical device employing sonomicrometer output signals for detection and measurement of cardiac mechanical function
Implantable medical devices (IMDs) for detection and measurement of cardiac mechanical and electrical function employ a system and method for determining mechanical heart function and measuring mechanical heart performance of upper and lower and left and right heart...
07/25/2006
7029706Composition for the treatment of cutaneous mycosis
The inventions relates to the use of silica in the formulation of antifungal composition for the treatment of cutaneous mycoses, and method to manufacture an antifungal powder with boric acid and silica. ...
04/18/2006
6995186Olopatadine formulations for topical administration
Topical formulations of olopatadine for treatment of allergic or inflammatory disorders of the eye and nose are disclosed. The aqueous formulations contain approximately 0.17-0.62% (w/v) of olopatadine and an amount of polyvinylpyrrolidone or polystyrene sulfonic ac...
02/07/2006
6953798β-alanine derivates
Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra′)R  (1) Ar1 is an optionally substituted aromatic or...
10/11/2005
6911451Phenylalanine derivatives
Phenylalanine derivatives of formula (1) are described: wherein L1 is a linker atom or group; X1 is a group selected from —N(R3)CO—, —N(R3)SO
06/28/2005
6878735Multi-substituted imidazolines and method of use thereof
A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The ...
04/12/2005
6858594Compounds and methods for treating urinary incontinence
The present invention relates to the use of α1L-agonists for treating urinary incontinence. ...
02/22/2005
6838475Imidazolidinones as NS3-serine protease inhibitors of hepatitis C virus
The present invention discloses novel imidazolidinones which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazolidinones as well as...
01/04/2005
6784183Diphenylurea compounds
Compounds of formula (I): and medicinal products containing the same which are useful as dual α2/5-HT2c antagonists. ...
08/31/2004
6777426Imidazole and imidazoline derivatives and uses thereof
This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human α2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulatio...
08/17/2004
6756395Imidazolinyimethyl aralklsulfonamides
Compounds of the Formula: where R1-R6 are those defined herein and methods for producing the same. Also provided are pharmaceutical compositions comprising a Compound of Formula I and methods for th...
06/29/2004
6750238Aralkyl ester soft drugs
The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is administered. The parent drug comp...
06/15/2004
6677341(R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and m...
01/13/2004
6649637Inhibition of intracellular replication by pyridinylimidazoles
Substituted pyridinylimidazoles SB203580 and SB202190 strongly inhibit replication and cause stage conversion from active tachyzoites to relatively dormant bradyzoites of the medically important, obligate intracellular parasite Toxoplasma gondii. The pyri...
11/18/2003
6608095Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
This invention provides a compound of the formula: ##STR1## or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, w...
08/19/2003
6596752Inhibitors of 댔댡 mediated cell adhesion
The present invention relates to small molecules according to the formula [I]: ##STR1## which are potent inhibitors of 댔ଲ.sub.1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing ଱
07/22/2003
6589972ଲ-phenylalanine derivatives as integrin antagonists
The present invention relates to compounds of the general formula (1) ##STR1## wherein R4 is --SO2 R4', --COOR4", --COR4', --CONR4'2 or --CSNR4'2 ; R4...
07/08/2003
6586478Methods and compositions for improving sleep
Methods and compositions for improving sleep in individuals with sleep disorders or other conditions which interfere with normal sleep via administration of a NO-mimetic are provided....
07/01/2003
6569862Methods for treatment of disorders of cardiac contractility
The present invention relates to methods for modulating calcium sensitivity of cardiac muscle. In preferred aspects, the invention provides methods for enhancing myocardial contractility and cardiac performance, and methods for treatment of heart failure ...
05/27/2003
6566387IL-8 receptor antagonists
The invention relates to the use of guanidine compounds in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8)....
05/20/2003
6552061Amino acid derivatives and anti-inflammatory agents
Provided are an anti-inflammatory agent containing, as an active ingredient, at least one selected from amino acid derivatives represented by formula (I) ##STR1## wherein Ar represents an optionally substituted 2-hydroxyaryl group, n is 0 or 1, R
04/22/2003
6541478Smoking cessation treatments using naltrexone and related compounds
Nicotine dependency is treated by administration of an opioid antagonist. In some embodiments, rapid or ultra rapid detoxification techniques include using a combination of an effective amount of an opioid antagonist such as nalmefene, naloxone or naltrex...
04/01/2003
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