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Class 546/74 - Two of the cyclos share at least three ring members (e.g., morphinans, etc.)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein at least three ring members of one cyclo
No. of applications: 52
Last issue date: 05/24/2012


1    
Application No.Application TitleIssue Date
20120129879Compounds and Compositions for Use in Phototherapy and in Treatment of Ocular Neovascular Disease and Cancers
The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, th...
05/24/2012
20120029007MORPHINAN COMPOUNDS
This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are ...
02/02/2012
20110306603LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF
8-Substituted-2,6-methano-3-benzazocines of general structure

are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications....

12/15/2011
20110257214MORPHINAN COMPOUNDS
This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are ...
10/20/2011
20110243889OPIOID AND OPIOID-LIKE COMPOUNDS AND USES THEREOF
The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock and oth...
10/06/2011
20110230511CARBOXAMIDE BIOISOSTERES OF OPIATES
A compound of formula I is disclosed.

Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications....

09/22/2011
20110212173Controlled Release Treatment of Depression
There is described a pharmaceutical composition for controlled release of an active compound wherein the active compound is selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, tri...
09/01/2011
20110206780MORPHINAN MODULATORS OF NMDA RECEPTORS, SIGMA1 RECEPTORS, SIGMA2 RECEPTORS, AND/OR A3B4 NICOTINIC RECEPTORS
The present invention relates to new morphinan modulators of NMDA receptors, σ1 receptors, σ2 receptors, and/or α3β4 nicotinic receptors, pharmaceutical compositions thereof, and methods of use thereof.

...

08/25/2011
20110190267PRODRUGS OF OPIOIDS AND USES THEREOF
The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are provid...
08/04/2011
20110112130Opioid-Nornicotine Codrugs Combinations for Pain Management
The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and nornicotine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic a...
05/12/2011
20110112131Opioid-Ketamine and Norketamine Codrug Combinations for Pain Management
The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and ketamine or norketamine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a s...
05/12/2011
20110071296Preparation of 10-Keto Morphinans by Benzylic Oxidation
The present invention provides processes for the preparation of 10-keto and/or 10-hydroxy morphinans. In particular, the invention provides to processes for preparing a 10-keto morphinan by chromium-catalyzed benzylic oxidation of a morphinan with a periodic acid....
03/24/2011
20110065743KAPPA OPIOID RECEPTOR LIGANDS
Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such a...
03/17/2011
20110015219(+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof
The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as a method for identifying (+)-morphinans that may be therapeutically effective by determining whether the (+)-morphinan inhibits the activation of TLR9. A...
01/20/2011
20100317858METAL COORDINATION COMPOUND AND LIGHT-EMITTING MATERIAL CONTAINING THE SAME
To provide a light-emitting device that is capable of red-light-emitting with high luminance and high efficiency and that is excellent in endurance; and a metal coordination compound metal coordination compound having a partial structure represented by formula (1) that ...
12/16/2010
20100317861Remove Amination of 6-Keto Normorphinans by Catalytic Hydrogen Transfer
The present invention provides processes for the stereoselective synthesis of 6-alpha-amino morphinans. In particular, the invention provides processes for the reductive amination of 6-keto normorphinans by catalytic transfer hydrogenation....
12/16/2010
20100210843Process for the Reductive Alkylation of Normorphinans
The invention provides a process for the N-alkylation of normorphinan compounds to produce N-alkylated morphinan compounds. In particular, the process relates to the alkylation of a normorphinan compound by a carboxaldehyde in the presence of a reducing agent to form an...
08/19/2010
20100190817LARGE SUBSTITUENT, NON-PHENOLIC AMINE OPIOIDS
8-Substituted-2,6-methano-3-benzazocines of general structure

are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications....

07/29/2010
20100120813PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF
The present invention provides a compound of formula I:

wherein X, R1, and R2 are as defined herein, and compositions thereof....

05/13/2010
20100113500ORALLY BIOAVAILABLE PRODUCTS OF (+)-3-HYDROXYMORPHINAN FOR PARKINSON'S DISEASE PREVENTION OR TREATMENT
The present invention is directed to a novel prodrug of (+)-3-hydroxymorphinan compound of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the same, and its use for preventing or treating Parkinson's disease....
05/06/2010
20100099699PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF
The present invention provides a compound of formula I:

wherein X, R1, and R2 are as defined herein, and compositions thereof, useful as a peripheral mu opioid receptor ant...

04/22/2010
20100081819Processes for the synthesis of tertiary amines
The invention provides processes for the preparation of morphinans having a tertiary amine. In particular, the present invention provides processes for the formation of tertiary amine alkaloids by direct N-alkylation of secondary amine alkaloids, the processes co-mediat...
04/01/2010
20100081817Processes for the selective amination of ketomorphinans
The present invention is generally directed to a process for the preparation of a ketomorphinan comprising maintaining a ketone group as unprotected and performing reductive amination using a hydrogen source and a catalyst....
04/01/2010
20100069639Processes for the Synthesis of Five and Six Membered Heterocyclic Rings
The present invention provides processes for the synthesis of five and six membered rings. In particular, the present invention provides processes for the synthesis of five and six membered rings in alkaloids....
03/18/2010
20100068786METHODS AND COMPOSITIONS FOR REVERSING P-GLYCOPROTEIN MEDICATED DRUG RESISTANCE
A method for inhibiting therapeutic drug resistance within a cell over-expressing a membrane protein is provided. The method comprises synthesizing a dimeric prodrug inhibitor of a monomeric therapeutic agent; administering the dimeric prodrug inhibitor to the membrane ...
03/18/2010
20100048906Preparation of Substituted Morphinan-6-Ones and Salts and Intermediates Thereof
The present invention is directed to processes for the synthesis of morphinan-6-ones and salts, intermediates, and analogs thereof....
02/25/2010
20100035826CONTROLLED RELEASE OF PHENOLIC OPIOIDS
A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate....
02/11/2010
20100009927Anti-Inflammatory and Anti-Allergy Extracts from Nettle
The present invention relates in part to nettle extracts that are useful for treating or preventing seasonal allergies, allergic rhinitis, and other inflammatory conditions....
01/14/2010
20090270624PROCESS FOR PURIFYING NOROXYMORPHONE COMPOUNDS
A process for purifying plant extracts which consist essentially of noroxymorphone compounds and which comprise, as impurities, α,β-unsaturated noroxymorphone compounds, by (a) converting the plant extract or the product of a subsequent stage in the synthesis of a sel...
10/29/2009
20090197905QUATERNARY OPIOID CARBOXAMIDES
Compounds of formulas:

are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates....

08/06/2009
20090176818Antitussive Agent
An antitussive, which can be used for therapy or prophylaxis of coughing, is disclosed. The antitussive comprises as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic substituent or a pharmaceutically acceptable acid addition salt thereo...
07/09/2009
20090156816Sinomenine derivatives and processes for their synthesis
The invention generally provides processes and intermediate compounds useful for the production of sinomenine derivatives. In particular, the process may encompass synthetic routes for the production of (+)-sinomenine derivatives and their intermediates....
06/18/2009
20090143417METHODS OF TREATING PAIN
The present invention is directed to methods and compositions for inducing, promoting or otherwise facilitating pain relief. More particularly the present invention discloses the combination of a nitric oxide donor and an opioid analgesic in the therapeutic management o...
06/04/2009
20090048447METHOD FOR DECREASING OPIOID METABOLISM
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2OH, —CH2NH2, —NHSO2CH3,

Q is O or S and Y is O, S or NOH are usef...

02/19/2009
20090005563CONVERSION OF THEBAINE TO MORPHINE DERIVATIVES
The present invention provides methods for the conversion of thebaine to a morphine derivative, such as hydrocodone. Novel ketal intermediates of the conversion are provided. A one-pot procedure for the conversion comprises treating thebaine with an acid in the presence...
01/01/2009
20080318966Sinomenine Derivatives and Preparation and Uses Thereof
The present invention relates to the preparation and pharmacological use of sinomenine derivatives of formula I. The approach disclosed herein is the modification of D ring by-substituting for R. Additional substitutions in the other rings are also provided herein. Seve...
12/25/2008
20080292585Azonafide Derivatives, Methods for Their Production and Pharmaceutical Compositions Therefrom
Azonafide derivatives are obtained by reacting azonafide with aldehydes, acyl halides, thioacyl halides, monoisocyanates, isothiocyanates, sulfonyl halides, monohalogenoalkanes, monohalogenoalkenes or monohalogenoalkynes, and are useful as active ingredients of pharmace...
11/27/2008
20080280936Morphinan Compounds
This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods...
11/13/2008
20080262231Processes for Preparing Morphinans and Intermediates Thereof
The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a β,γ-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture ...
10/23/2008
20080233606USE OF RAMAN SPECTROSCOPY IN ENZYME ACTIVITY ASSAYS
Provided herein are assays for detecting enzyme activity using Raman Spectroscopy....
09/25/2008
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