Two Of The Cyclos Share At Least Three Ring Carbons (e.g., Benzomorphans, Etc.) Patents (Class 546/97)
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Patent number: 10829455Abstract: 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: GrantFiled: March 19, 2019Date of Patent: November 10, 2020Inventors: Yonggang Xu, Hao Wei, Song Chen, Haoning Zhang
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Patent number: 10507188Abstract: 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: GrantFiled: December 7, 2017Date of Patent: December 17, 2019Assignee: The University of ChicagoInventor: Chun-Su Yuan
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Patent number: 10450275Abstract: Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, and neuropathic pain.Type: GrantFiled: December 22, 2015Date of Patent: October 22, 2019Assignee: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: Stephen F. Martin, James J. Sahn, Luisa Scott, Jonathan Thomas Pierce-Shimomura
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Patent number: 10287249Abstract: 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: GrantFiled: June 26, 2015Date of Patent: May 14, 2019Assignee: Amphastar Pharmaceuticals, Inc.Inventors: Yonggang Xu, Hao Wei, Song Chen, Haoning Zhang
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Patent number: 9975854Abstract: 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: GrantFiled: May 5, 2015Date of Patent: May 22, 2018Assignee: Purdue Pharma L.P.Inventors: Laykea Tafesse, Jiangchao Yao, Jianming Yu, R. Richard Goehring
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Patent number: 9056836Abstract: 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: GrantFiled: January 30, 2014Date of Patent: June 16, 2015Assignee: Purdue Pharma L.P.Inventors: Jeffrey Lockman, Jae Hyun Park, Laykea Tafesse, Jiangchao Yao, Jianming Yu
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Publication number: 20150141650Abstract: 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: ApplicationFiled: December 21, 2012Publication date: May 21, 2015Inventors: 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
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Publication number: 20150119416Abstract: 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: ApplicationFiled: January 5, 2015Publication date: April 30, 2015Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. WENTLAND
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Patent number: 8987453Abstract: 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: GrantFiled: October 16, 2012Date of Patent: March 24, 2015Assignee: 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
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Patent number: 8957085Abstract: 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: GrantFiled: March 12, 2014Date of Patent: February 17, 2015Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Publication number: 20150045384Abstract: 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: ApplicationFiled: May 23, 2014Publication date: February 12, 2015Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Laura Cook Blumberg, Dan Deaver, David Eyerman
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Patent number: 8901148Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: GrantFiled: August 23, 2013Date of Patent: December 2, 2014Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Patent number: 8859580Abstract: 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: GrantFiled: November 14, 2008Date of Patent: October 14, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
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Publication number: 20140275545Abstract: 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: ApplicationFiled: December 19, 2013Publication date: September 18, 2014Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Publication number: 20140221419Abstract: 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: ApplicationFiled: January 30, 2014Publication date: August 7, 2014Applicant: Purdue Pharma L.P.Inventors: Jeffrey Lockman, Jae Hyun Park, Laykea Tafesse, Jiangchao Yao, Jianming Yu
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Publication number: 20140194457Abstract: 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: ApplicationFiled: March 12, 2014Publication date: July 10, 2014Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Patent number: 8765780Abstract: 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: GrantFiled: May 12, 2009Date of Patent: July 1, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Bradford S. Hamilton, Joerg Kley, Thorsten Lehmann-Lintz
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Publication number: 20140179669Abstract: 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: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Stefan PETERS, Matthias ECKHARDT, Bradford S. HAMILTON, Frank HIMMELSBACH, Joerg KLEY
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Publication number: 20140135351Abstract: 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: ApplicationFiled: November 8, 2013Publication date: May 15, 2014Applicant: PURDUE PHARMA L.P.Inventors: Jeffrey LOCKMAN, Laykea TAFESSE, Jiangchao YAO, Jianming YU
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Publication number: 20140107143Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.Type: ApplicationFiled: September 27, 2013Publication date: April 17, 2014Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Publication number: 20130345251Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Patent number: 8598204Abstract: 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: GrantFiled: December 29, 2009Date of Patent: December 3, 2013Assignee: Suven Life Sciences LimitedInventors: 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
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Publication number: 20130317226Abstract: 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: ApplicationFiled: January 31, 2012Publication date: November 28, 2013Applicants: UNIVERSITE NICE SOPHIA ANTIPOLIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRSInventors: Olivier Soriani, Mauro Franck Borgese, Sonia Martial
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Publication number: 20130184256Abstract: 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: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Henning PRIEPKE, Georg DAHMANN, Kai GERLACH, Roland PFAU, Wolfgang WIENEN, Annette SCHULER-METZ, Sandra HANDSCHUH, Herbert NAR
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Patent number: 8466171Abstract: 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: GrantFiled: October 31, 2008Date of Patent: June 18, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Weifang Shan, James Aaron Balog, Ashvinikumar V. Gavai, Yufen Zhao
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Patent number: 8436175Abstract: 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: GrantFiled: March 22, 2011Date of Patent: May 7, 2013Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Patent number: 8426594Abstract: 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: GrantFiled: November 28, 2008Date of Patent: April 23, 2013Assignee: Purdue Pharma L.P.Inventor: Donald J. Kyle
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Publication number: 20130096132Abstract: 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: ApplicationFiled: October 16, 2012Publication date: April 18, 2013Applicant: ABBVIE INC.Inventor: AbbVie Inc.
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Publication number: 20130072682Abstract: 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: ApplicationFiled: October 15, 2012Publication date: March 21, 2013Applicant: ACTAVIS GROUP PTC EHFInventors: Actavis Group PTC EHF, Engelbert Seide
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Publication number: 20130018051Abstract: 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: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
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Patent number: 8314119Abstract: 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: GrantFiled: November 5, 2007Date of Patent: November 20, 2012Assignee: 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
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Publication number: 20120289702Abstract: 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: ApplicationFiled: December 28, 2010Publication date: November 15, 2012Applicant: Nippon Soda Co., Ltd.Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
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Publication number: 20120277216Abstract: 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: ApplicationFiled: December 29, 2009Publication date: November 1, 2012Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: 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
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Publication number: 20120258981Abstract: The invention relates to a process for the synthesis of quaternized compounds of formula:Type: ApplicationFiled: April 5, 2012Publication date: October 11, 2012Applicant: Alkermes, Inc.Inventor: Scott Duncan
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Patent number: 8258300Abstract: 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: GrantFiled: September 29, 2008Date of Patent: September 4, 2012Assignee: King Abdulaziz UniversityInventor: Abdullah Mohamed Asiri
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Patent number: 8252929Abstract: 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: GrantFiled: May 9, 2011Date of Patent: August 28, 2012Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Publication number: 20120149900Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.Type: ApplicationFiled: January 8, 2010Publication date: June 14, 2012Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
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Patent number: 8163916Abstract: 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: GrantFiled: March 20, 2008Date of Patent: April 24, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Diana L. Nersesian, Kevin B. Sippy, Jianguo Ji, Tao Li, Lei Shi
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Patent number: 8097726Abstract: 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: GrantFiled: May 17, 2007Date of Patent: January 17, 2012Assignee: Industrial Technology Research InstituteInventors: On Lee, Jenn-Tsang Hwang, Chi-Y Hung
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Publication number: 20110306603Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: August 23, 2011Publication date: December 15, 2011Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland
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Publication number: 20110288101Abstract: 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: ApplicationFiled: May 20, 2011Publication date: November 24, 2011Applicant: ALCON RESEARCH, LTD.Inventors: Lixin Wang, Marcia Danielle Ong, Chi-Chun Tsai, Michael Hartzer
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Patent number: 8026252Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: GrantFiled: June 3, 2009Date of Patent: September 27, 2011Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Publication number: 20110230511Abstract: 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: ApplicationFiled: March 22, 2011Publication date: September 22, 2011Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland
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Publication number: 20110224437Abstract: 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: ApplicationFiled: August 31, 2009Publication date: September 15, 2011Applicant: ACTAVIS GROUP PTC EHFInventors: Girish Dixit, Krishnadatt Sharma, Kundan Singh Shekhawat, Nitin Sharadchandra Pradhan
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Publication number: 20110207763Abstract: 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: ApplicationFiled: May 9, 2011Publication date: August 25, 2011Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland
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Publication number: 20110190262Abstract: 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: ApplicationFiled: November 14, 2008Publication date: August 4, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
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Patent number: 7897766Abstract: 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: GrantFiled: September 7, 2006Date of Patent: March 1, 2011Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson, William H. Bunnelle, Diana L. Nersesian
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Patent number: 7893256Abstract: 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: GrantFiled: April 8, 2010Date of Patent: February 22, 2011Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Publication number: 20100324080Abstract: 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: ApplicationFiled: November 28, 2008Publication date: December 23, 2010Applicant: PURDUE PHARMA L.P.Inventor: Donald Kyle
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Publication number: 20100190817Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: July 21, 2009Publication date: July 29, 2010Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland