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...that in 1800 ether was first used by partyers as a fun diversion? Sniffing the gas led to hilarious and raucous laughter as people watched each other become more and more intoxicated and silly. Several doctors independently realized the value ether would have to anesthetize surgery patients. Of those who claimed rights to the "discovery," none had a happy ending. One had a seizure and died defending his rights. Another spent his life in an asylum because he had been denied acclaim. A third became addicted to chloroform and, in a New York City jail, he soaked a cloth in the drug, severed an artery and bled to death.

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Class 514/332 - Plural six-membered hetero rings consisting of one nitrogen and five carbon atoms


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter which contains at least two of the six-membered
No. of applications: 394
Last issue date: 05/24/2012


1                    
Application No.Application TitleIssue Date
20120130144TREATMENT OF LUNG CANCER WITH A NITROBENZAMIDE COMPOUND IN COMBINATION WITH A GROWTH FACTOR INHIBITOR
In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of trea...
05/24/2012
20120083489BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISTS
The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and d...
04/05/2012
20120083443Control of ATP Release by Red Blood Cells and Therapeutic Applications Thereof
The invention is based upon the discovery that red blood cells contain phosphodiesterase 3B (PDE3B), and that inhibition of that phosphodiesterase allows for an enhanced accumulation of cAMP and subsequent release of ATP. It was further discovered that RBCS treated with...
04/05/2012
20120071539COMPOUNDS AND METHODS FOR MODULATING THE SILENCING OF A POLYNUCLEOTIDE OF INTEREST
Methods and compositions comprising chemical compounds that modulate the silencing of a polynucleotide of interest in a cell are provided. Such chemical compounds when used in combination with an appropriate silencing element can be used to modulate (increase or decreas...
03/22/2012
20120070510WOUND AND MUCOUS MEMBRANE DISINFECTANT
Aqueous wound and mucous membrane disinfectant containing a) octenidine dihydrochloride, and b) one or more active ingredients selected from the group ethanol, 1-propanol, 2-propanol, undecylene amidopropyl trimonium methosulfate, 3-(4-chlorophenoxy)-1,2-propanediol and...
03/22/2012
20120053170NICOTINAMIDE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF AS ANTICANCER DRUGS
The present invention relates to nicotinamide derivatives of formula (I), to compositions containing same, and to the therapeutic use thereof, in particular as anticancer drugs. The invention also relates to the method for preparing said compounds, as well as to some of...
03/01/2012
20120053209ANTICANCER COMPOUNDS, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
The invention relates to nicotinamide derivatives that can be used as anticancer drugs....
03/01/2012
20120039805Therapeutics And Methods For Treating Neoplastic Diseases Comprising Determining The Level Of Caveolin-1 And/Or Caveolin-2 In A Stromal Cell Sample
The invention provides diagnostic and therapeutic methods for neoplastic disease patients with neoplasms of for example, the breast, skin, kidney, lung, pancreas, rectum and colon, prostate, bladder, epithelial, non-epithelial; lymphomas, sarcomas, melanomas, and the li...
02/16/2012
20120015961ISOTHIOUREA DERIVATIVES OR ISOUREA DERIVATIVES HAVING BACE1 INHIBITORY ACTIVITY
The present invention provides, for example, a compound of the following formula (I):

  • wherein R1 is substituted amino and the like,
  • 01/19/2012
20120004593ANTISEPTIC BASED ON BISPYRIDINIUM ALKANES
An antimicrobially effective composition includes a) at least 0.15% by weight of bispyridinium alkane, b) at least 3.5% by weight of humectant and c) water. Upon dilution with water, the composition produces a solution with an osmolality of from 230 to 350 mOsmol/kg and...
01/05/2012
20110312875PEPTIDIC COMPOUNDS
The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and...
12/22/2011
20110312974HETEROARYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS
Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone...
12/22/2011
20110313000CCR9 INHIBITORS AND METHODS OF USE THEREOF
The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds re...
12/22/2011
20110305729Scriptaid Isosteres and Their Use in Therapy
Compounds of the invention are of the formula (I); wherein: custom-character is a double bond and X is C; or 12/15/2011
20110306597Nicotinamide Derivatives
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allerg...
12/15/2011
20110300234Methods of Treating Tumor Cells Using RHCC Protein, Fragment or Variant
Methods of treating tumor cells in an individual comprise administering to the individual a drug having anti-tumor effect, wherein the drug is delivered into the tumor cells via Right-Handed Coiled-Coil (RHCC) protein or a fragment or variant thereof. The drug may, for ...
12/08/2011
20110294793HYDROXYPHENYL SULFONAMIDES AS ANTIAPOPTOTIC BCL INHIBITORS
The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compou...
12/01/2011
20110288129AMIDE DERIVATIVES AS TRPV1 ANTAGONISTS
The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof,

wherein R1, R2, and R3, ...

11/24/2011
20110275674Small Molecules Modulator of Epigenetic Regulation and Their Therapeutic Applications
Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not...
11/10/2011
20110275615NOVEL SUBSTITUTED AMIDES, THEIR PREPARATION AND USE
An amide of the formula I

and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meani...

11/10/2011
20110275675Antimicrobial Dental Materials
Dental material which contains an antimicrobial active ingredient according to general formula (I),

in which R1=H, C1 to C3 alkylene residue; R2=a linear or branche...

11/10/2011
20110263564PYRIDINE, BICYCLIC PYRIDINE AND RELATED ANALOGS AS SIRTUIN MODULATORS
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, disease...
10/27/2011
20110257199NOVEL TERARYL COMPOUNDS AS ANTIPARASITIC AGENTS
Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues....
10/20/2011
20110251158FULLERENE THERAPIES FOR INFLAMMATION AND INHIBITION OF BUILD-UP OF ARTERIAL PLAQUE
Described herein are methods for treating inflammatory disorders or for inhibiting the build-up of arterial plaque. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene....
10/13/2011
20110237626COMPOSITIONS FOR HYGIENIC HAND DISINFECTION AND DISINFECTANT HANDWASHING
The invention relates to a disinfectant composition which includes a) one or more 1- or 2-(C1- to C24-alkyl)glycerol ethers, b) one or more bispyridiniumalkanes and c) one or more amine oxides, and to the use of the composition for hygienic hand di...
09/29/2011
20110237573N- (HETERO)ARYL, 2- (HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.

...

09/29/2011
201102375762-AMINOPYRIMIDIN-4-ONE AND 2-AMINOPYRIDINE DERIVATIVES BOTH HAVING BACE1-INHIBITING ACTIVITY
The present invention provides a compound which has an effect of inhibiting amyloid-β production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-β proteins. The present invention relates to a compound rep...
09/29/2011
20110237578AMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF
Compounds are provided according to formula (I), where A, B, W, X′, L, R1, R3, R4b, and m′ are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of ...
09/29/2011
201102304674,6-DIAMINONICOTINAMIDE COMPOUND
[Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal t...
09/22/2011
201102241923-Arylamino Pyridine Derivatives
The invention provides novel, substituted 3-arylamino pyridine compounds

pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as define...

09/15/2011
20110224179MEDICAMENT AND METHOD OF DIAGNOSIS
We disclose a diagnostic test to determine suitable therapeutic intervention of subjects suffering from subclinical Cushing's syndrome [SCS] and also agents that antagonise the action of cortisol or inhibit excess cortisol production in the treatment of conditions such ...
09/15/2011
20110224225Inhibitors of protein kinases
Compounds of general Formula (I):

wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dep...

09/15/2011
20110217301METHODS FOR TREATING OR SCREENING FOR COMPOUNDS FOR THE TREATMENT OF SEPSIS
The present invention relates to a method for treating and screening for compounds for the treatment of sepsis. More specifically, the treatment and screening methods are based on the discovery that granzyme B containing platelets (GzmB-platelet) causes apoptosis by dir...
09/08/2011
20110217360OCTENIDINE COMPOSITION
The invention relates to octenidine or a pharmaceutical salt thereof, in particular octenidine dihydrochloride, which is intended for mutual therapeutic administration of the octenidine in solution with a polyalcohol of formula 1: (H—C—OH)a(HO—C—OH)
09/08/2011
20110206783P2X3, RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN
The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 rec...
08/25/2011
20110206638COMPOSITIONS AND METHODS FOR REDUCING THE MUTATION RATE OF VIRUSES
The disclosure provides compositions and methods for reducing the mutation rate of a virus, such as an RNA virus or a DNA virus, in a cell infected with the virus by, in one aspect, contacting the cell with an effective amount of an iron chelator or an antioxidant. Also...
08/25/2011
20110201576Small molecule inhibitors of stat3 with anti-tumor activity
The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or i...
08/18/2011
20110201591ISONICOTINAMIDE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is ...
08/18/2011
20110195125Nanoparticles For Drug Delivery To The Central Nervous System
The present disclosure relates to compositions and methods for producing nanoparticles to provide relatively more rapid delivery of such particles across the blood-brain barrier. The nanoparticles may be formed from bis-quaternary pyridinium-aldoxime salts that may also...
08/11/2011
20110184023THE SALTS OF N-[4-(1-CYANOCYCLOPENTYL)PHENYL]-2-(4-PYRIDYLMETHYL)AMINO-3-PYRIDINECARBOXAMIDE
The present invention relates to the salts of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl) amino-3-pyridine carboxamide, especially hydrochloride and mesylate thereof, and the use of said salts in the preparation of an antineoplastic medicament....
07/28/2011
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