Plural Isoquinoline Ring Systems Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/308)
-
Patent number: 11074737Abstract: A system including a non-transitory computer readable medium configured to store instructions thereon; and a processor. The processor is configured to execute the instructions for defining a virtual space associated with a first user, wherein the virtual space comprises a first region and a first avatar. The processor is configured to execute the instructions for causing the first avatar to enter the first region based on received first input; and moving the first avatar within the first region in response to a received second input. The processor is configured to execute the instructions for registering charging information the received second input; and removing the first avatar from the first region in response to a received third input. The processor is configured to execute the instructions for performing charging-related processing, in accordance with the registered charging information, in response to removing the first avatar from the first region.Type: GrantFiled: April 16, 2020Date of Patent: July 27, 2021Assignee: COLOPL, INC.Inventor: Kento Nakashima
-
Patent number: 10618885Abstract: One embodiment provides a compound of Formula I that activates autophagy, a pharmaceutical composition and use thereof:Type: GrantFiled: January 3, 2018Date of Patent: April 14, 2020Inventors: Zhi-Hong Jiang, Li-Ping Bai, Xiaobo Zhou, Kam Wai Vincent Wong, Zhiyuan Zheng, Yuen Kwan Betty Law
-
Patent number: 10376498Abstract: Method for treating a viral infection in a patient, comprising administering to the patient a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, comprising a moiety represented by figure (I), wherein R1 is a saturated or unsaturated bivalent hydrocarbon group. Viruses subject to treatment can include HIV and flaviviruses such as west nile, dengue, or hepatitis C virus. Compositions and methods of isolation and purification are also described including from the Red Sea sponge.Type: GrantFiled: October 29, 2015Date of Patent: August 13, 2019Assignee: King Abdullah University of Science and TechnologyInventors: Christian R. Voolstra, Aubrie O'Rourke, Stephan Kremb
-
Patent number: 10259798Abstract: The present invention relates to a method for preparing magnesium lithospermate B. The method is characterized in that: magnesium lithospermate B is extracted or purified from a Salvia miltiorrhiza plant material or a Salvia miltiorrhiza extract in the presence of an added magnesium salt. The present invention also relates to a high-purity magnesium lithospermate B product prepared by the method of the present invention, wherein the content of magnesium lithospermate B is more than 95% by weight.Type: GrantFiled: February 9, 2015Date of Patent: April 16, 2019Assignees: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES, SHANGHAI GREEN VALLEY PHARMACEUTICAL CO., LTD.Inventors: Lijiang Xuan, Yiping Wang, Weibin Song, Chunguang Chen, Dingxiang Li, Xiaoyu Zhou, Yunlong Gu, Liang Hu, Jing Zhao, Wenwei Xu, Shumei Wang
-
Patent number: 9675608Abstract: The present invention discloses a method of treating cancer and/or multidrug-resistant cancer, comprising administering an effective amount of hernandezine or thalidezine. A pharmaceutical composition comprising hernandezine or thalidezine admixed with a pharmaceutical carrier for treating cancers and/or multidrug-resistant cancer is also disclosed.Type: GrantFiled: October 28, 2015Date of Patent: June 13, 2017Assignee: Macau University of Science and TechnologyInventors: Kam Wai Wong, Yuen Kwan Law, Liang Liu
-
Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
Patent number: 9670181Abstract: The invention relates to compounds of the formula wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.Type: GrantFiled: June 25, 2014Date of Patent: June 6, 2017Assignees: ALLERGAN, INC., EXONHIT THERAPEUTICS SAInventors: Bertrand Leblond, Cedric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang -
Patent number: 9499518Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.Type: GrantFiled: September 13, 2010Date of Patent: November 22, 2016Assignees: University of Kentucky Research Foundation, University of UtahInventors: Joseph R. Holtman, Peter A. Crooks, Linda P. Dwoskin, J. Michael McIntosh, Elzbieta Pogonowska Wala
-
Patent number: 9345257Abstract: Enhancing the bioavailability of a drug or dietary supplement by administering it concurrently with one or more members of the d-tetrandrine family.Type: GrantFiled: March 12, 2014Date of Patent: May 24, 2016Assignee: CBA Pharma, Inc.Inventor: Daryl L. Barnett
-
Patent number: 9169268Abstract: The present invention provides a method of preventing, alleviating and/or treating depression, comprising the step of administering to a subject in need thereof a therapeutically effective amount of a 7-alkoxy fangchinoline compound or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: October 6, 2014Date of Patent: October 27, 2015Assignee: Peking UniversityInventors: Yonghe Zhang, Xueqiong Zhang, Zhaofu Sheng
-
Patent number: 9133158Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.Type: GrantFiled: November 29, 2012Date of Patent: September 15, 2015Assignee: HOFFMAN-LA ROCHE INC.Inventors: Johannes Aebi, Kurt Amrein, Wenming Chen, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan, Zhanguo Wang, Mingwei Zhou
-
Patent number: 9119847Abstract: The present invention discloses a method of treating neurodegenerative disorder comprising administering an effective amount of an alkaloid which is a bisbenzylisoquinline alkaloid isolated from the traditional Chinese medicinal herb Nelumbo nucifera. The pharmaceutical composition thereof for treating Huntington's disease is also disclosed.Type: GrantFiled: December 8, 2014Date of Patent: September 1, 2015Assignee: Macau University of Science and TechnologyInventors: Yuen Kwan Law, Kam Wai Wong, Liang Liu
-
Publication number: 20150133427Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: October 15, 2014Publication date: May 14, 2015Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
-
Publication number: 20150133492Abstract: This invention is directed to the use of N-desmethyldauricine, a novel autophagy enhancer, in treating cancers or neurodegenerative conditions.Type: ApplicationFiled: October 29, 2014Publication date: May 14, 2015Inventors: Kam Wai WONG, Yuen Kwan LAW, Zhi Hong JIANG, Liang LIU, Wai Kit CHAN, Xiao Jun YAO
-
Patent number: 8940774Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.Type: GrantFiled: November 26, 2013Date of Patent: January 27, 2015Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
-
Publication number: 20150018352Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: March 7, 2013Publication date: January 15, 2015Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
-
Publication number: 20150004134Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.Type: ApplicationFiled: December 3, 2013Publication date: January 1, 2015Applicant: CALITHERA BIOSCIENCES, INC.Inventors: Mark K. Bennett, Matthew I. Gross, Susan D. Bromley, Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
-
SUBSTITUTED 6,7-DIALKOXY-3-ISOQUINOLINOL DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE 10A)
Publication number: 20140309253Abstract: The invention relates to compounds of the formula wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.Type: ApplicationFiled: June 25, 2014Publication date: October 16, 2014Inventors: Bertrand Leblond, Cedric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang -
Publication number: 20140275157Abstract: Enhancing the cellular uptake of a drug or dietary supplement by administering it concurrently with one or more members of the d-tetrandrine family.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: CBA Pharma, Inc.Inventor: Daryl L. Barnett
-
Publication number: 20140275061Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: September 18, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
-
Publication number: 20140228343Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: December 20, 2013Publication date: August 14, 2014Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
-
Publication number: 20140221345Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: December 20, 2013Publication date: August 7, 2014Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
-
Patent number: 8772316Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.Type: GrantFiled: February 17, 2012Date of Patent: July 8, 2014Assignees: Allergan, Inc., Exonhit Therapeutics SAInventors: Bertrand Leblond, John E. Donello, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, Rong Yang
-
Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
-
Tris-Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors
Publication number: 20140080866Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.Type: ApplicationFiled: November 26, 2013Publication date: March 20, 2014Applicant: University of Kentucky Research FoundationInventors: Peter Crooks, Linda DWOSKIN, Roger Papke, Guangrong ZHENG, Sangeetha SUMITHRAN -
Publication number: 20140073591Abstract: Multidrug resistance reversers of the d-tetrandrine family are used in conjunction with penicillins and other principle drugs used to treat MRSA.Type: ApplicationFiled: September 12, 2013Publication date: March 13, 2014Applicant: CBA Pharma, Inc.Inventors: Wayne Michael Putnam, Beth D. Gudeman
-
Publication number: 20140045872Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.Type: ApplicationFiled: September 14, 2011Publication date: February 13, 2014Applicant: NOVARTIS AGInventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
-
Publication number: 20140011836Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.Type: ApplicationFiled: September 6, 2013Publication date: January 9, 2014Applicant: University of Kentucky Research FoundationInventors: Joseph R. HOLTMAN, Peter Anthony CROOKS, Linda P. DWOSKIN, J. Michael MCINTOSH, Elzbieta Pogonowska WALA
-
Patent number: 8623877Abstract: The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: January 7, 2014Assignee: SanofiInventors: Zhongli Gao, Ryan Hartung
-
Patent number: 8592451Abstract: The invention provides neuromuscular blockade agents of the non-depolarizing type with few if any circulatory effects. Compounds of the invention include bis(isoquinolylalkanol) diesters of fumaric, maleic, succinic, and acetylenedicarboxylic acids; compositions suitable for parenteral administration of these compounds as a surgical adjunct to anesthesia, and methods of preparation of the compounds. Compounds of the invention can produce neuromuscular blockade of short or intermediate duration, which for various compounds can be reversed by administration of a thiol compound such as L-cysteine, D-cysteine or glutathione. For various compounds of the invention, the neuromuscular blockade effect can be reversed quickly, efficiently, and without notable side-effects.Type: GrantFiled: March 17, 2010Date of Patent: November 26, 2013Assignee: Cornell UniversityInventor: John J. Savarese
-
Publication number: 20130296333Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: July 9, 2013Publication date: November 7, 2013Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
-
Publication number: 20130289027Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).Type: ApplicationFiled: January 23, 2012Publication date: October 31, 2013Applicant: ViiV Healthcare UK LimitedInventors: Martha Alicia De La Rosa, Simon Haydar, Brian Alvin Johns, Emile Johann Velthuisen
-
Patent number: 8557812Abstract: The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.Type: GrantFiled: August 22, 2005Date of Patent: October 15, 2013Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Guoping Wang, Guozhi Tang, Renxiao Wang, Zaneta Nikolovska-Coleska, Dajun Yang, Liang Xu
-
Publication number: 20130231366Abstract: This application provides a method for the use of select quaternary ammonium antagonists to alpha-7 nAChR for the treatment of cancer and HIV and AIDS.Type: ApplicationFiled: February 20, 2013Publication date: September 5, 2013Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATIONInventors: Roger L. PAPKE, Peter A. CROOKS, Linda P. DWOSKIN, Gretchen Lopez HERNANDEZ, Zhenfa ZHANG, Jeffrey S. THINSCHMIDT, Guangrong ZHENG
-
Patent number: 8513280Abstract: The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect.Type: GrantFiled: September 9, 2010Date of Patent: August 20, 2013Assignees: Institut National de la Sante et de la Recherche Medicale, Commissariat a l'Energie Atomique, Gesellschaft fur Biotechnologische Forschung mbH (GBF)Inventors: Annie Andrieux, Didier Job, Annie Schweitzer, Gerhard Höfle
-
Patent number: 8507491Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: GrantFiled: August 24, 2009Date of Patent: August 13, 2013Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
-
Publication number: 20130203709Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
-
Publication number: 20130158068Abstract: The present invention relates to a novel dicarboximide derivative of berbamine represented by formula I, including, but not limited to, a phthalimide derivative of berbamine and an aromatic heterocyclic dicarboximide derivative of berbamine, or a pharmaceutically acceptable salt thereof, to a process for preparation of the same, to a pharmaceutical composition comprising said compound and to use thereof in manufacture of an antitumor medicament.Type: ApplicationFiled: August 25, 2011Publication date: June 20, 2013Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
-
Publication number: 20130116276Abstract: The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinson's disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol.Type: ApplicationFiled: April 13, 2010Publication date: May 9, 2013Applicant: Institute of Chinese Materia Medica, Chinese Academy of Medical SciencesInventors: Tingliang Jiang, Feng Sui, Hairu Huo, Lanfang Li, Shuying Guo
-
Publication number: 20130059838Abstract: The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.Type: ApplicationFiled: November 6, 2012Publication date: March 7, 2013Applicant: SANOFIInventor: Sanofi
-
Patent number: 8362020Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: December 21, 2010Date of Patent: January 29, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
-
Patent number: 8357805Abstract: The present invention provides an improved method for obtaining cisatracurium besylate, which preferably chromatographically separating cisatracurium besylate from a mixture of (1R,1?R)-atracurium isomers via flash chromatography.Type: GrantFiled: March 5, 2008Date of Patent: January 22, 2013Assignee: CHEMAGIS Ltd.Inventors: Oded Arad, Elena Ostrovsky
-
Patent number: 8338455Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 19, 2007Date of Patent: December 25, 2012Assignee: Amgen Inc.Inventors: Yuan Cheng, Deborah Choquette, Jean-Christophe Harmange, Andrew Tasker
-
Patent number: 8299253Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: December 22, 2006Date of Patent: October 30, 2012Assignee: University of Kentucky Research FoundationInventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha P Sumithran
-
Publication number: 20120263670Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.Type: ApplicationFiled: June 29, 2011Publication date: October 18, 2012Applicant: Ardelyx, Inc.Inventors: Dominique Charmot, Jeffrey W. Jacobs, Michael Robert Leadbetter, Marc Navre, Christopher Carreras, Noah Bell
-
Publication number: 20120258957Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders or diseases influenced by modulation of orexins, such as sleep disorders.Type: ApplicationFiled: November 22, 2010Publication date: October 11, 2012Inventors: Matilda Jane Bingham, Andrew Dunbar, Margaret Jean Laats, Grant Wishart
-
Patent number: 8263607Abstract: Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings.Type: GrantFiled: May 20, 2008Date of Patent: September 11, 2012Assignee: Astellas Pharma Inc.Inventors: Jun-ichi Shishikura, Makoto Inoue, Takashi Ogiyama, Koichi Yonezawa, Susumu Yamaki, Kazuhiro Yokoyama, Shuichirou Kakimoto, Hidetsugu Okada
-
Publication number: 20120214837Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicants: ExonHit Therapeutics SA, ALLERGAN, INC.Inventors: Bertrand Leblond, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, John E. Donello, Rong Yang
-
Publication number: 20120108629Abstract: The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinson's disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol.Type: ApplicationFiled: April 13, 2010Publication date: May 3, 2012Applicant: Institute of Chinese Materia Medica, China AcademyInventors: Tingliang Jiang, Feng Sui, Hairu Huo, Lanfang Li, Shuying Guo
-
Publication number: 20120095041Abstract: The invention provides neuromuscular blockade agents of the non-depolarizing type with few if any circulatory effects. Compounds of the invention include bis(isoquinolylalkanol) diesters of fumaric, maleic, succinic, and acetylenedicarboxylic acids; compositions suitable for parenteral administration of these compounds as a surgical adjunct to anesthesia, and methods of preparation of the compounds. Compounds of the invention can produce neuromuscular blockade of short or intermediate duration, which for various compounds can be reversed by administration of a thiol compound such as L-cysteine, D-cysteine or glutathione. For various compounds of the invention, the neuromuscular blockade effect can be reversed quickly, efficiently, and without notable side-effects.Type: ApplicationFiled: March 17, 2010Publication date: April 19, 2012Applicant: Cornell UniversityInventor: John J. Savarese
-
Patent number: 8148398Abstract: The invention provides novel neuromuscular blocking agents, methods of using the neuromuscular blocking agents as well as reagents, methods and kits for reversing the effects of the neuromuscular blocking agents.Type: GrantFiled: December 5, 2007Date of Patent: April 3, 2012Assignee: Cornell Research Foundation, Inc.Inventor: John J. Savarese