Additional Hetero Ring Attached Directly Or Indirectly To The Seven-membered Hetero Ring By Nonionic Bonding Patents (Class 514/217.03)
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Patent number: 10987351Abstract: The present invention provides novel compounds of formula (Ia) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, metabolic diseases, fibrotic diseases, or cholestatic diseases.Type: GrantFiled: January 29, 2018Date of Patent: April 27, 2021Assignee: GenfitInventors: Jean-Francois Delhomel, Enrico Perspicace, Zouher Majd, Peggy Parroche, Robert Walczak, Pascal Bonnet, Jade Fogha
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Patent number: 10953017Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.Type: GrantFiled: July 8, 2019Date of Patent: March 23, 2021Assignee: SOUTHERN RESEARCH INSTITUTEInventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
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Patent number: 10654866Abstract: Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, and the other is hydrogen, and methods for their use are provided.Type: GrantFiled: July 11, 2019Date of Patent: May 19, 2020Assignee: Eli Lilly and CompanyInventors: Jolie Anne Bastian, Jeffrey Daniel Cohen, Almudena Rubio, Daniel Jon Sall
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Patent number: 10562925Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R1, R2 or R3 is —P(?O)(OH)2, and the other two of R1, R2 and R3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.Type: GrantFiled: February 19, 2019Date of Patent: February 18, 2020Assignee: TOLERO PHARMACEUTICALS, INC.Inventors: Adam Siddiqui-Jain, David J. Bearss
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Patent number: 10550139Abstract: Embodiments of the present disclosure relate generally to novel achiral and chiral sulfur-, nitrogen- and phosphorus-containing ligands, designated as NNS-type, P(O)NS-type, PNS-type, SNNS-type, SNNP(O)-type, or SNNP-type polydentate ligands and transition metal complexes of these ligands, including iridium complexes having PNS-type and NNS-type ligands. The catalysts derived from these ligands and transition metal complexes may be used in a wide range of catalytic reactions, including hydrogenation and transfer hydrogenation of unsaturated organic compounds, dehydrogenation of alcohols and boranes, various dehydrogenative couplings, chemoselective hydrogenation of ?,?-unsaturated alcohols, and other catalytic transformations.Type: GrantFiled: December 9, 2016Date of Patent: February 4, 2020Assignee: Triad National Security, LLCInventors: Pavel A. Dub, John Cameron Gordon
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Patent number: 10358415Abstract: Disclosed is a process for preparing unsaturated malonates and/or their isomers. The process includes the step of reacting an aldehyde and a dialkyl malonate in the presence of a Lewis acid and a carboxylic acid thereby forming an unsaturated malonate.Type: GrantFiled: March 11, 2016Date of Patent: July 23, 2019Assignee: International Flavors & Fragrances Inc.Inventors: Michael Cheskis, Yigal Becker
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Patent number: 10259835Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R1, R2 or R3 is —P(?O)(OH)2, and the other two of R1, R2 and R3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.Type: GrantFiled: August 9, 2017Date of Patent: April 16, 2019Assignee: Tolero Pharmaceuticals, Inc.Inventors: Adam Siddiqui-Jain, David J. Bearss
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Patent number: 10045939Abstract: Methods of treating atrial arrhythmia include administering an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof, such that the at least one antiarrhythmic pharmaceutical agent first enters the heart through the pulmonary vein to the left atrium. Other methods of treating atrial arrhythmia include administering by inhalation an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof. An amount of the at least one antiarrhythmic pharmaceutical agent may peak in the coronary sinus of the heart at a time ranging from 10 seconds to 30 minutes from initiation of the administering. Unit doses, aerosols, and kits are also contemplated.Type: GrantFiled: February 26, 2015Date of Patent: August 14, 2018Assignee: InCarda Therapeutics, Inc.Inventors: Carlos A. Schuler, Rangachari Narasimhan
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Patent number: 9932327Abstract: The present invention relates to the rohitukine (5,7-dihydroxy-8-(3-hydroxy-1-methyl-piperidin-4-yl)-4H-chromen-4-ones) analogs of formula A and pharmaceutically acceptable salts thereof. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various proliferative disorders such as melanoma, leukemia, breast cancer and prostate cancer etc. [insert Formula A here] wherein, n=0 or 1, when n=1, the dotted line indicates the double bond.Type: GrantFiled: April 16, 2014Date of Patent: April 3, 2018Assignee: The Council of Scientific & Industrial ResearchInventors: Ram A. Vishwakarma, Sandip B. Bharate, Shashi Bhushan, Dilip M. Mondhe, Shreyans K. Jain, Samdarshi Meena, Santosh K. Guru, Anup S. Pathania, Suresh Kumar, Akanksha Behl, Mubashir J. Mintoo, Sonali S. Bharate, Prashant Joshi
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Patent number: 9701608Abstract: Process for the industrial synthesis of the compound of formula (I):Type: GrantFiled: December 4, 2014Date of Patent: July 11, 2017Assignee: LES LABORATORIES SERVIERInventors: Jean-Françoís Briere, Raphaël Lebeuf, Vincent Levacher, Christophe Hardouin, Jean-Pierre Lecouve
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Patent number: 9662371Abstract: Methods of treating certain behavioral characteristics associated with autism are provided. Additionally, methods of treating disorders associated with repetitive behaviors, social deficits and/or cognitive deficits are also provided. A therapeutic amount of oxytocin or oxytocin analogs, either alone or in combination, are administered to individuals demonstrating behavioral characteristics associated with autism or other disorders to reduce the severity of the debilitating behavior. In various aspects, characteristics such as deficit in social awareness or cognitive skills and repetitive behaviors are treated. Co-administration of oxytocin and/or oxytocin analogs with known psychopharmacologic agents is also provided. Advantageously, oxytocin and oxytocin analogs do not have deleterious effects with other drugs such that administration results in few side effects.Type: GrantFiled: October 3, 2003Date of Patent: May 30, 2017Assignee: Neuropharmacology Services, LLCInventor: Eric Hollander
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Patent number: 9634260Abstract: The disclosure provides a conjugated compound having phenoxathiinl, method for preparing the same and OLED. The conjugated compound has one of the following formulas: Different kinds of electron-rich conjugated aromatic units are reacted with intermediate having phenoxathiinl by Suzuki coupling, Buchwald-Hartwig coupling, or Cu-catalyzed amination of halogenated aromatic hydrocarbons for forming the conjugated compound having phenoxathiin. The prepared novel compound is fluorescent, so that it can be used as the material of light emitting layer of OLED devices.Type: GrantFiled: May 22, 2015Date of Patent: April 25, 2017Assignee: SHENZHEN CHINA STAR OPTOELECTRONICS TECHNOLOGY CO., LTD.Inventors: Xianjie Li, Yuanchun Wu, Shijian Su, Ming Liu, Kunkun Liu
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Patent number: 9573932Abstract: The present disclosure provides a method for preparing a compound of formula XVII, comprising: (1) contacting a compound of formula XIV with a compound of formula 3 to obtain a compound of formula 2; and (2) contacting the compound of formula 2 with a compound of formula 4 to obtain a compound of formula XVII. The method is low toxicity, cheap, easy to get, environmentally and friendly, and is economical and industrially applicable.Type: GrantFiled: March 2, 2015Date of Patent: February 21, 2017Inventor: Yong Xu
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Patent number: 9440922Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: GrantFiled: February 11, 2015Date of Patent: September 13, 2016Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yasuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Patent number: 9062034Abstract: 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: GrantFiled: March 5, 2013Date of Patent: June 23, 2015Assignee: 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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Publication number: 20150051194Abstract: 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: October 31, 2014Publication date: February 19, 2015Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. WENTLAND
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Patent number: 8946203Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: GrantFiled: March 5, 2013Date of Patent: February 3, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Steven Richard Brunette, Michael J. Burke, Suresh R. Kapadia, Thomas Martin Kirrane, Matthew Russell Netherton, Hossein Razavi, Sonia Rodriguez, Anjan Saha, Robert Sibley, Lana Louise Smith-Keenan, Hidenori Takahashi, Michael Robert Turner, Jiang-Ping Wu, Erick Richard Roush Young, Qiang Zhang, Qing Zhang, Renee M. Zindell
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Publication number: 20150018341Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 15, 2015Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
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Publication number: 20140343045Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: May 23, 2014Publication date: November 20, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Publication number: 20140329802Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: ApplicationFiled: March 28, 2014Publication date: November 6, 2014Applicant: Astellas Pharma Inc.Inventors: Shunichiro HACHIYA, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
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Publication number: 20140309185Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
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Publication number: 20140256712Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: March 12, 2014Publication date: September 11, 2014Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
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Patent number: 8729068Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: GrantFiled: October 26, 2012Date of Patent: May 20, 2014Assignee: Astellas Pharma Inc.Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
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Publication number: 20140107095Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: SERAGON PHARMACEUTICALS, INC.Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
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Publication number: 20140088077Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.Type: ApplicationFiled: December 3, 2013Publication date: March 27, 2014Applicant: SANOFIInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
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Publication number: 20130267501Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: January 22, 2013Publication date: October 10, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventor: The Board of Trustees of the Leland Stanford Junior University
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Publication number: 20130244996Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael J. BURKE, Suresh R. KAPADIA, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Hossein RAZAVI, Sonia RODRIGUEZ, Anjan SAHA, Robert SIBLEY, Lana Louise SMITH-KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, Jiang-Ping WU, Erick Richard Roush YOUNG, Qiang ZHANG, Qing ZHANG, Renee M. ZINDELL
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Publication number: 20130196973Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 13, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
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Publication number: 20130123242Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
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Publication number: 20130116232Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: June 8, 2011Publication date: May 9, 2013Applicant: ARAGON PHARMACEUTICALS, INC.Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
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Publication number: 20130109677Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: December 3, 2010Publication date: May 2, 2013Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming Shao, John Emmerson Campbell, Michael Charles Hewitt, Una Campbell, Taleen G. Hanania
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Publication number: 20130053369Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: ApplicationFiled: October 26, 2012Publication date: February 28, 2013Applicant: Astellas Pharma Inc.Inventor: Astellas Pharma Inc.
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Publication number: 20130029973Abstract: A compound has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating hyperphosphatemia, preventing hyperphosphatemia, or both. The compound is a tetrahydrobenzothiophene compound. A pharmaceutical composition for treating hyperphosphatemia includes the compound or salt thereof. A method of treating hyperphosphatemia includes administering to a subject an effective amount of the compound or salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: January 31, 2013Applicant: ASTELLAS PHARMA INC.Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
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Patent number: 8362008Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: GrantFiled: December 11, 2008Date of Patent: January 29, 2013Assignee: The University Of EdinburghInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Patent number: 8314247Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: GrantFiled: January 9, 2008Date of Patent: November 20, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20120270847Abstract: Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid pro-drug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.Type: ApplicationFiled: July 16, 2010Publication date: October 25, 2012Applicant: SHIRE LLCInventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
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Patent number: 8232270Abstract: The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (?)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (?)-meptazinol compounds were synthesized, from the starting material (?)-meptazinol, successively by N-demethylation forming (?)-nor-meptazinol and then by acylation with ?,?-alkanediacyl dihalides or alkylation with ?,?-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced A? aggregation test demonstrated that the bivalent (?)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both AChE and A? aggregation. The most potent compound inhibited both AChE and BChE at nM level, which was 10000 and 1500 times more potent than (?)-MEP hydrochloride, respectively.Type: GrantFiled: July 24, 2007Date of Patent: July 31, 2012Inventors: Zhuibai Qiu, Qiong Xie, Hongzhuan Chen, Hao Wang, Zheng Xia, Meiyan Lu, Xinghai Wang
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Patent number: 8217032Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.Type: GrantFiled: June 23, 2011Date of Patent: July 10, 2012Assignee: Eli Lilly and CompanyInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
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Publication number: 20120172351Abstract: A compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof have a GPR40 receptor activation action and is useful as an insulin secretagogue or a prophylactic or therapeutic drug for diabetes and the like.Type: ApplicationFiled: June 8, 2010Publication date: July 5, 2012Inventors: Nobuyuki Negoro, Yoshito Terao, Satoshi Mikami, Tomoya Yukawa
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Publication number: 20120129837Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: ApplicationFiled: January 30, 2012Publication date: May 24, 2012Inventors: Wieslaw M. Cholody, Yi Zang, Norman E. Ohler, Sheela Chellappan, Janak Padia, Karina Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel
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Patent number: 8183235Abstract: Disclosed is a compound represented by the formula (I) below as a dihydronaphthalene compound having a chemical structure which is excellent in production efficiency when compared with lasofoxifene and nafoxidine. This compound is useful as a proteasome inhibitor and/or an antitumor agent.Type: GrantFiled: September 11, 2008Date of Patent: May 22, 2012Assignee: Tokyo University of Science Educational Foundation Administrative OrganizationInventor: Isamu Shiina
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Publication number: 20120094973Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
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Patent number: 8153624Abstract: Compounds of formula (I): formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.Type: GrantFiled: July 11, 2008Date of Patent: April 10, 2012Assignee: Eli Lilly and CompanyInventors: Michael James Genin, Francisco Javier Agejas-Chicharro, Ana Belen Bueno Melendo, Peter Rudolph Manninen, Alan M. Warshawsky
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120077775Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.Type: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicants: LE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURGInventors: Nicolas WINSSINGER, Sofia BARLUENGA, Martin KARPLUS
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Patent number: 8138172Abstract: The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.Type: GrantFiled: July 3, 2007Date of Patent: March 20, 2012Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co Ltd.Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
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Publication number: 20120015925Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.Type: ApplicationFiled: May 16, 2011Publication date: January 19, 2012Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Takehiko SASAHARA, Mitsunobu MOHRI, Ken-ichi KASAHARA
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Patent number: 8084466Abstract: Bicyclic heteroaryl-substituted imidazole compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: December 16, 2008Date of Patent: December 27, 2011Assignee: Janssen Pharmaceutica NVInventors: David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20110306601Abstract: Antagonists of group 1 metabotropic glutamate receptors (mGluR) potentiate the effect of positive AMPA receptor modulators on neurotrophin expression, such as brain-derived neurotrophic factor (BDNF). The findings described herein suggest a combinatorial approach for drug therapies, using both positive AMPA receptor modulators and mGluR antagonists, to enhance brain neurotrophism.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicant: The Regents of the University of CaliforniaInventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
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Publication number: 20110281847Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.Type: ApplicationFiled: June 23, 2011Publication date: November 17, 2011Applicant: ELI LILLY AND COMPANYInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace