Additional Hetero Ring Attached Directly Or Indirectly To The Seven-membered Hetero Ring By Nonionic Bonding Patents (Class 514/217.03)
  • Patent number: 10259835
    Abstract: 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: Grant
    Filed: August 9, 2017
    Date of Patent: April 16, 2019
    Assignee: Tolero Pharmaceuticals, Inc.
    Inventors: Adam Siddiqui-Jain, David J. Bearss
  • Patent number: 10045939
    Abstract: 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: Grant
    Filed: February 26, 2015
    Date of Patent: August 14, 2018
    Assignee: InCarda Therapeutics, Inc.
    Inventors: Carlos A. Schuler, Rangachari Narasimhan
  • Patent number: 9932327
    Abstract: 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: Grant
    Filed: April 16, 2014
    Date of Patent: April 3, 2018
    Assignee: The Council of Scientific & Industrial Research
    Inventors: 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
  • Patent number: 9701608
    Abstract: Process for the industrial synthesis of the compound of formula (I):
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: July 11, 2017
    Assignee: LES LABORATORIES SERVIER
    Inventors: Jean-Françoís Briere, Raphaël Lebeuf, Vincent Levacher, Christophe Hardouin, Jean-Pierre Lecouve
  • Patent number: 9662371
    Abstract: 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: Grant
    Filed: October 3, 2003
    Date of Patent: May 30, 2017
    Assignee: Neuropharmacology Services, LLC
    Inventor: Eric Hollander
  • Patent number: 9634260
    Abstract: 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: Grant
    Filed: May 22, 2015
    Date of Patent: April 25, 2017
    Assignee: SHENZHEN CHINA STAR OPTOELECTRONICS TECHNOLOGY CO., LTD.
    Inventors: Xianjie Li, Yuanchun Wu, Shijian Su, Ming Liu, Kunkun Liu
  • Patent number: 9573932
    Abstract: 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: Grant
    Filed: March 2, 2015
    Date of Patent: February 21, 2017
    Inventor: Yong Xu
  • Patent number: 9440922
    Abstract: 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: Grant
    Filed: February 11, 2015
    Date of Patent: September 13, 2016
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: 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
  • Patent number: 9062034
    Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: June 23, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Sandra Handschuh, Herbert Nar
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8946203
    Abstract: 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: Grant
    Filed: March 5, 2013
    Date of Patent: February 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: 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
  • Publication number: 20150018341
    Abstract: 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: Application
    Filed: December 28, 2012
    Publication date: January 15, 2015
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
  • Publication number: 20140343045
    Abstract: 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: Application
    Filed: May 23, 2014
    Publication date: November 20, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Publication number: 20140329802
    Abstract: 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: Application
    Filed: March 28, 2014
    Publication date: November 6, 2014
    Applicant: Astellas Pharma Inc.
    Inventors: Shunichiro HACHIYA, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Publication number: 20140309185
    Abstract: 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: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
  • Publication number: 20140256712
    Abstract: 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: Application
    Filed: March 12, 2014
    Publication date: September 11, 2014
    Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.
    Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
  • Patent number: 8729068
    Abstract: 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: Grant
    Filed: October 26, 2012
    Date of Patent: May 20, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Publication number: 20140107095
    Abstract: 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: Application
    Filed: December 20, 2013
    Publication date: April 17, 2014
    Applicant: SERAGON PHARMACEUTICALS, INC.
    Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
  • Publication number: 20140088077
    Abstract: 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: Application
    Filed: December 3, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
  • Publication number: 20130267501
    Abstract: 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: Application
    Filed: January 22, 2013
    Publication date: October 10, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventor: The Board of Trustees of the Leland Stanford Junior University
  • Publication number: 20130244996
    Abstract: 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: Application
    Filed: March 5, 2013
    Publication date: September 19, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: 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
  • Publication number: 20130196973
    Abstract: 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: Application
    Filed: March 13, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: 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
  • Publication number: 20130123242
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Application
    Filed: October 26, 2012
    Publication date: May 16, 2013
    Applicant: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: 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
  • Publication number: 20130116232
    Abstract: 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: Application
    Filed: June 8, 2011
    Publication date: May 9, 2013
    Applicant: ARAGON PHARMACEUTICALS, INC.
    Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
  • Publication number: 20130109677
    Abstract: 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: Application
    Filed: December 3, 2010
    Publication date: May 2, 2013
    Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, John Emmerson Campbell, Michael Charles Hewitt, Una Campbell, Taleen G. Hanania
  • Publication number: 20130053369
    Abstract: 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: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Publication number: 20130029973
    Abstract: 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: Application
    Filed: April 27, 2011
    Publication date: January 31, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Patent number: 8362008
    Abstract: 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: Grant
    Filed: December 11, 2008
    Date of Patent: January 29, 2013
    Assignee: The University Of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Patent number: 8314247
    Abstract: 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: Grant
    Filed: January 9, 2008
    Date of Patent: November 20, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
  • Publication number: 20120270847
    Abstract: 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: Application
    Filed: July 16, 2010
    Publication date: October 25, 2012
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Patent number: 8232270
    Abstract: 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: Grant
    Filed: July 24, 2007
    Date of Patent: July 31, 2012
    Inventors: Zhuibai Qiu, Qiong Xie, Hongzhuan Chen, Hao Wang, Zheng Xia, Meiyan Lu, Xinghai Wang
  • Patent number: 8217032
    Abstract: 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: Grant
    Filed: June 23, 2011
    Date of Patent: July 10, 2012
    Assignee: Eli Lilly and Company
    Inventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
  • Publication number: 20120172351
    Abstract: 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: Application
    Filed: June 8, 2010
    Publication date: July 5, 2012
    Inventors: Nobuyuki Negoro, Yoshito Terao, Satoshi Mikami, Tomoya Yukawa
  • Publication number: 20120129837
    Abstract: 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: Application
    Filed: January 30, 2012
    Publication date: May 24, 2012
    Inventors: Wieslaw M. Cholody, Yi Zang, Norman E. Ohler, Sheela Chellappan, Janak Padia, Karina Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel
  • Patent number: 8183235
    Abstract: 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: Grant
    Filed: September 11, 2008
    Date of Patent: May 22, 2012
    Assignee: Tokyo University of Science Educational Foundation Administrative Organization
    Inventor: Isamu Shiina
  • Publication number: 20120094973
    Abstract: 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: Application
    Filed: December 21, 2011
    Publication date: April 19, 2012
    Applicant: NATIONAL TAIWAN UNIVERSITY
    Inventors: Yueh-Hsiung Kuo, Ming-Jai Su
  • Patent number: 8153624
    Abstract: 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: Grant
    Filed: July 11, 2008
    Date of Patent: April 10, 2012
    Assignee: Eli Lilly and Company
    Inventors: Michael James Genin, Francisco Javier Agejas-Chicharro, Ana Belen Bueno Melendo, Peter Rudolph Manninen, Alan M. Warshawsky
  • Publication number: 20120083488
    Abstract: 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: Application
    Filed: June 9, 2010
    Publication date: April 5, 2012
    Inventors: 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
  • Publication number: 20120077775
    Abstract: 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: Application
    Filed: September 23, 2011
    Publication date: March 29, 2012
    Applicants: LE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURG
    Inventors: Nicolas WINSSINGER, Sofia BARLUENGA, Martin KARPLUS
  • Patent number: 8138172
    Abstract: 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: Grant
    Filed: July 3, 2007
    Date of Patent: March 20, 2012
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co Ltd.
    Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
  • Publication number: 20120015925
    Abstract: 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: Application
    Filed: May 16, 2011
    Publication date: January 19, 2012
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Takehiko SASAHARA, Mitsunobu MOHRI, Ken-ichi KASAHARA
  • Patent number: 8084466
    Abstract: 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: Grant
    Filed: December 16, 2008
    Date of Patent: December 27, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: David E. Kindrachuk, Jennifer D. Venable
  • Publication number: 20110306601
    Abstract: 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: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicant: The Regents of the University of California
    Inventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
  • Publication number: 20110281847
    Abstract: 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: Application
    Filed: June 23, 2011
    Publication date: November 17, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
  • Publication number: 20110201589
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Application
    Filed: August 10, 2009
    Publication date: August 18, 2011
    Applicant: EVOTEC AG
    Inventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xialou Wang
  • Publication number: 20110200553
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Application
    Filed: April 7, 2011
    Publication date: August 18, 2011
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammed Arshad Siddiqui, Wuyi Wang, Constanin G. Yannopoulos
  • Publication number: 20110172208
    Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
    Type: Application
    Filed: June 26, 2009
    Publication date: July 14, 2011
    Applicant: Kissei Pharmaceutical Co., Ltd.
    Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
  • Patent number: 7973030
    Abstract: 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: Grant
    Filed: February 25, 2005
    Date of Patent: July 5, 2011
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
  • Publication number: 20110152234
    Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 23, 2010
    Publication date: June 23, 2011
    Inventors: Alan Faull, Craig Johnstone, Andrew Morley, Jeffrey Philip Poyser
  • Publication number: 20110129542
    Abstract: In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: August 12, 2008
    Publication date: June 2, 2011
    Inventors: Santhosh Neelamkavil, Craig D. Boyle, Samuel Chackalamannil