Two Of The Cyclos Share At Least Three Ring Carbons (e.g., Benzomorphans, Etc.) Patents (Class 546/97)
  • Patent number: 10507188
    Abstract: Particles comprising an opioid receptor antagonist as well as methods of their use and methods of their preparation are provided herein. Such particles may be used for treating and preventing opioid-induced side effects in patients, and may be provided to chronic opioid users as well.
    Type: Grant
    Filed: December 7, 2017
    Date of Patent: December 17, 2019
    Assignee: The University of Chicago
    Inventor: Chun-Su Yuan
  • Patent number: 10450275
    Abstract: Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, and neuropathic pain.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: October 22, 2019
    Assignee: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Stephen F. Martin, James J. Sahn, Luisa Scott, Jonathan Thomas Pierce-Shimomura
  • Patent number: 10287249
    Abstract: A method of resolving a racemic mixture of (±)-Huperzine A to (?)-Huperzine A includes: separating the (?)-Huperzine A from the racemic mixture of (±)-Huperzine A by chiral high performance liquid chromatography (HPLC), the chiral HPLC being performed utilizing a mobile phase including a solution including an alcohol and one selected from dichloromethane, trichloromethane, and a mixture thereof, and the chiral HPLC being performed utilizing a chiral stationary phase including a polysaccharide derivative.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: May 14, 2019
    Assignee: Amphastar Pharmaceuticals, Inc.
    Inventors: Yonggang Xu, Hao Wei, Song Chen, Haoning Zhang
  • Patent number: 9975854
    Abstract: The invention provides compounds as represented by Formula I or I? and pharmaceutically acceptable salts, solvates, and diastereomers thereof: Wherein R1, R2, R2a, R3, and R4 are defined in the disclosure. The invention also provides compounds of Formulae II, III, and A-H, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. In certain embodiments, Compounds of the Invention are useful for treating pain, constipation, and other conditions as delineated in the disclosure. Without wishing to be bound by any theory, it is believed that Compounds of the Invention are effective in treating conditions that are modulated by activity of opioid and/or ORL-1 receptors.
    Type: Grant
    Filed: May 5, 2015
    Date of Patent: May 22, 2018
    Assignee: Purdue Pharma L.P.
    Inventors: Laykea Tafesse, Jiangchao Yao, Jianming Yu, R. Richard Goehring
  • Patent number: 9056836
    Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula I-ID as shown below, wherein R1, R2a, R2b, R3 and R4 are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
    Type: Grant
    Filed: January 30, 2014
    Date of Patent: June 16, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Jeffrey Lockman, Jae Hyun Park, Laykea Tafesse, Jiangchao Yao, Jianming Yu
  • Publication number: 20150141650
    Abstract: The present invention relates to certain amide derivatives that have the ability to inhibit 11-?-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.
    Type: Application
    Filed: December 21, 2012
    Publication date: May 21, 2015
    Inventors: Jagannath Madanahalli Ranganath Rao, Uppala Venkatesham, Sivanageswara Rao Doppalapudi, Bommegowda Yadaganahalli Kenchegowda, George Fernand, Jenson George, G R Madhavan, Gorle Paidapu Naidu, V. S. Naga Rajesh Kadambari, S Jagannath, R Manivannan, T Senthil Kumar, B Siva Senthil Kumar, Rayi Mallikarjuna
  • Publication number: 20150119416
    Abstract: 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.
    Type: Application
    Filed: January 5, 2015
    Publication date: April 30, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8987453
    Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: March 24, 2015
    Assignee: AbbVie Inc.
    Inventors: Michael R. Schrimpf, Diana L. Nersesian, Kevin B. Sippy, Jianguo Ji, Tao Li, Marc Scanio, Lei Shi, Chih-Hung Lee, William H. Bunnelle, Geoff G. Z. Zhang, Paul J. Brackemeyer, Shuang Chen, Rodger F. Henry
  • Patent number: 8957085
    Abstract: 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.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: February 17, 2015
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Publication number: 20150045384
    Abstract: The present application relates to analogues of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof.
    Type: Application
    Filed: May 23, 2014
    Publication date: February 12, 2015
    Applicant: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Laura Cook Blumberg, Dan Deaver, David Eyerman
  • Patent number: 8901148
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: December 2, 2014
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Patent number: 8859580
    Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
  • Publication number: 20140275545
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
    Type: Application
    Filed: December 19, 2013
    Publication date: September 18, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Publication number: 20140221419
    Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula I-ID as shown below, wherein R1, R2a, R2b, R3 and R4 are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
    Type: Application
    Filed: January 30, 2014
    Publication date: August 7, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Jeffrey Lockman, Jae Hyun Park, Laykea Tafesse, Jiangchao Yao, Jianming Yu
  • Publication number: 20140194457
    Abstract: 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.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Patent number: 8765780
    Abstract: The present invention relates to compounds defined by Formula (I), wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Grant
    Filed: May 12, 2009
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bradford S. Hamilton, Joerg Kley, Thorsten Lehmann-Lintz
  • Publication number: 20140179669
    Abstract: The present invention relates to compounds defined by formula I wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Stefan PETERS, Matthias ECKHARDT, Bradford S. HAMILTON, Frank HIMMELSBACH, Joerg KLEY
  • Publication number: 20140135351
    Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula I?, Formula IA?, Formula IB?, Formula IC?, or Formula ID? as shown below; and related Formula I?, Formula IA?, Formula IB?, Formula IC?, or Formula ID?; Formula I, Formula IA, Formula IB, Formula IC, or Formula ID; wherein R1, R2a, R2b, R3 and R4 are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: PURDUE PHARMA L.P.
    Inventors: Jeffrey LOCKMAN, Laykea TAFESSE, Jiangchao YAO, Jianming YU
  • Publication number: 20140107143
    Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 17, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Publication number: 20130345251
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: August 23, 2013
    Publication date: December 26, 2013
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Patent number: 8598204
    Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: December 3, 2013
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Ishtiyaque Ahmad, Pradeep Jayarajan, Nagaraj Vishwottam Kandikere, Anil Karbhari Shinde, Rama Sastri Kambhampati, Gopinadh Bhyrapuneni, Jyothsna Ravula, Sriramachandra Murthy Patnala, Venkateswarlu Jasti
  • Publication number: 20130317226
    Abstract: The present invention relates to the use of the Sigma-1 receptor (Sig1R) in the context of the post-transcriptional regulation of the membrane expression of ion channels. The present invention can be used in the field of the treatment of diseases involving ion channels. These are, for example, nervous system diseases, neurodegenerative diseases, heart diseases, and cancer.
    Type: Application
    Filed: January 31, 2012
    Publication date: November 28, 2013
    Applicants: UNIVERSITE NICE SOPHIA ANTIPOLIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS
    Inventors: Olivier Soriani, Mauro Franck Borgese, Sonia Martial
  • Publication number: 20130184256
    Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 18, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Henning PRIEPKE, Georg DAHMANN, Kai GERLACH, Roland PFAU, Wolfgang WIENEN, Annette SCHULER-METZ, Sandra HANDSCHUH, Herbert NAR
  • Patent number: 8466171
    Abstract: Disclosed are fused heterocyclic compounds of Formula (I): or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: June 18, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Weifang Shan, James Aaron Balog, Ashvinikumar V. Gavai, Yufen Zhao
  • Patent number: 8436175
    Abstract: 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.
    Type: Grant
    Filed: March 22, 2011
    Date of Patent: May 7, 2013
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Patent number: 8426594
    Abstract: The invention relates to Benzomorphan Compounds of Formula (I): wherein X, R1, R2, R3, R4, and R5 are as defined herein. These compounds are useful for treating constipation preferably constipation caused by mu-opioid agonist therapy.
    Type: Grant
    Filed: November 28, 2008
    Date of Patent: April 23, 2013
    Assignee: Purdue Pharma L.P.
    Inventor: Donald J. Kyle
  • Publication number: 20130096132
    Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
    Type: Application
    Filed: October 16, 2012
    Publication date: April 18, 2013
    Applicant: ABBVIE INC.
    Inventor: AbbVie Inc.
  • Publication number: 20130072682
    Abstract: Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4 ,5-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone.
    Type: Application
    Filed: October 15, 2012
    Publication date: March 21, 2013
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Actavis Group PTC EHF, Engelbert Seide
  • Publication number: 20130018051
    Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Patent number: 8314119
    Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: November 20, 2012
    Assignee: AbbVie Inc.
    Inventors: Michael R. Schrimpf, Diana L. Nersesian, Kevin B. Sippy, Jianguo Ji, Tao Li, Marc Scanio, Lei Shi, Chih-Hung Lee, William H. Bunnelle, Geoff G. Z. Zhang, Paul J. Brackemeyer, Shuang Chen, Rodger F. Henry
  • Publication number: 20120289702
    Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.
    Type: Application
    Filed: December 28, 2010
    Publication date: November 15, 2012
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
  • Publication number: 20120277216
    Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.
    Type: Application
    Filed: December 29, 2009
    Publication date: November 1, 2012
    Applicant: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Ishtiyaque Ahmad, Pradeep Jayarajan, Nagaraj Vishwottam Kandikere, Anil Karbhari Shinde, Rama Sastri Kambhampati, Gopinadh Bhyrapuneni, Jyothsna Ravula, Sriramachandra Murthy Patnala, Venkateswarlu Jasti
  • Publication number: 20120258981
    Abstract: The invention relates to a process for the synthesis of quaternized compounds of formula:
    Type: Application
    Filed: April 5, 2012
    Publication date: October 11, 2012
    Applicant: Alkermes, Inc.
    Inventor: Scott Duncan
  • Patent number: 8258300
    Abstract: The azo dyes relate to thiophene azo dyes of the general formula: where R1 is Cyano or C1-C5 alkoxy carbonyl; R2 is hydrogen, halogene, C1-C2 alkyl, phenyl, or substituted phenyl; and R3 is C1-C5 alkoxy carbonyl, C1-C4 alkanoyl, benzoyl, phenyl, alkyl substituted phenyl, or alkoxy phenyl; or R2 and R3 are fused cycloalkane with C3-C5.
    Type: Grant
    Filed: September 29, 2008
    Date of Patent: September 4, 2012
    Assignee: King Abdulaziz University
    Inventor: Abdullah Mohamed Asiri
  • Patent number: 8252929
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: August 28, 2012
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Publication number: 20120149900
    Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.
    Type: Application
    Filed: January 8, 2010
    Publication date: June 14, 2012
    Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
  • Patent number: 8163916
    Abstract: The invention relates to compounds that are substituted azaadamantane ester and carbamate derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: April 24, 2012
    Assignee: Abbott Laboratories
    Inventors: Michael R. Schrimpf, Diana L. Nersesian, Kevin B. Sippy, Jianguo Ji, Tao Li, Lei Shi
  • Patent number: 8097726
    Abstract: A huperzine A compound is provided. The huperzine A compound has following formula: wherein X comprises O or S, Y comprises —O—, —S—, —CH(R4)—, —C(R4)(R5)—, —C(R4)?C(R5)—, —C?C—, —NH— or —N(R4)—, n is 0, 1 or 2, R3 is C(?X)—(Y)n—R1 provided that R2 is H or R2 and R3 are combined to form ?CH—Ar, wherein R1, R4 and R5 independently comprise hydrogen, C1-C32 alkyl, C1-C32 alkenyl, C1-C32 alkynyl, C1-C32 aryl or C1-C32 heteroaryl, in which alkyl, alkenyl, alkynyl, aryl or heteroaryl with one or more substituents comprising halogen, hydroxyl, alkoxy, aryloxyl, amino, alkylamino, arylamino, dialkylamino, diarylamino, imino, alkylimino, arylimino, acylamido, diacylamido, acylimido, cyano, nitro, mercapto, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, thio, sulfonyl or sulfinyl, and Ar comprises aryl or heteroaryl.
    Type: Grant
    Filed: May 17, 2007
    Date of Patent: January 17, 2012
    Assignee: Industrial Technology Research Institute
    Inventors: On Lee, Jenn-Tsang Hwang, Chi-Y Hung
  • Publication number: 20110306603
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: August 23, 2011
    Publication date: December 15, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Publication number: 20110288101
    Abstract: One aspect of the present invention relates to aqueous surgical compositions comprising a sigma-1 receptor agonist. Another aspect of the present invention relates to methods of irrigating ocular tissues during an ophthalmic surgical procedure such as cataract surgery. Such methods comprise bathing the ocular tissues with a composition comprising a sigma-1 receptor agonist.
    Type: Application
    Filed: May 20, 2011
    Publication date: November 24, 2011
    Applicant: ALCON RESEARCH, LTD.
    Inventors: Lixin Wang, Marcia Danielle Ong, Chi-Chun Tsai, Michael Hartzer
  • Patent number: 8026252
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: September 27, 2011
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Publication number: 20110230511
    Abstract: 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.
    Type: Application
    Filed: March 22, 2011
    Publication date: September 22, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Publication number: 20110224437
    Abstract: Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(4,5-diamino-10-aza-tricyclo[6.3.1.02.7]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone.
    Type: Application
    Filed: August 31, 2009
    Publication date: September 15, 2011
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Girish Dixit, Krishnadatt Sharma, Kundan Singh Shekhawat, Nitin Sharadchandra Pradhan
  • Publication number: 20110207763
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
    Type: Application
    Filed: May 9, 2011
    Publication date: August 25, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Publication number: 20110190262
    Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: November 14, 2008
    Publication date: August 4, 2011
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
  • Patent number: 7897766
    Abstract: The invention relates to amine-substituted aza-adamantane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. Radiolabelled compounds useful for evaluating the binding affinity to ?7 nicotinic acetylcholine receptors also are described.
    Type: Grant
    Filed: September 7, 2006
    Date of Patent: March 1, 2011
    Assignee: Abbott Laboratories
    Inventors: Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson, William H. Bunnelle, Diana L. Nersesian
  • Patent number: 7893256
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: February 22, 2011
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Adam Hughes
  • Publication number: 20100324080
    Abstract: The invention relates to Benzomorphan Compounds of Formula (I): wherein X, R1, R2, R3, R4, and R5 are as defined herein. These compounds are useful for treating constipation preferably constipation caused by mu-opioid agonist therapy.
    Type: Application
    Filed: November 28, 2008
    Publication date: December 23, 2010
    Applicant: PURDUE PHARMA L.P.
    Inventor: Donald Kyle
  • Publication number: 20100190817
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: July 21, 2009
    Publication date: July 29, 2010
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Publication number: 20100184986
    Abstract: Organocatalysts, particularly proline sulfonamide organocatalysts, having a first general formula as follows are disclosed. Embodiments of a method for using these organocatalysts also are disclosed. The method comprises providing a disclosed organocatalyst, and performing a reaction, often an enantioselective or diastereoselective reaction, using the organocatalyst. Solely by way of example, disclosed catalysts can be used to perform aldol reactions, conjugate additions, Michael additions, Robinson annulations, Mannich reactions, ?-aminooxylations, ?-hydroxyaminations, ?-aminations and alkylation reactions. Certain of such reactions are intramolecular cyclizations used to form cyclic compounds, such as 5- or 6-membered rings, having one or more chiral centers. Disclosed organocatalysts generally are much more soluble in typical solvents used for organic synthesis than are known compounds.
    Type: Application
    Filed: March 17, 2010
    Publication date: July 22, 2010
    Inventors: Rich Garrett Carter, Hua Yang