1,3-thiazoles (including Hydrogenated) Patents (Class 546/269.7)
  • Patent number: 10426762
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: October 1, 2019
    Assignee: COCRYSTAL PHARMA, INC.
    Inventors: Sam S. Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Patent number: 10414767
    Abstract: Deuterated quinazolinone compounds and pharmaceutical compositions containing such compounds are provided. In particular, deuterated quinazolinone compounds of formula (I) are provided, as well as pharmaceutical compositions containing such compounds or crystal form, pharmaceutically acceptable salts, hydrates or solvates thereof. The deuterated quinazolinone compounds of formula (I) can be used for treating and/or preventing PI3K kinase-associated diseases, such as cancer, cell proliferative diseases and the like.
    Type: Grant
    Filed: January 30, 2015
    Date of Patent: September 17, 2019
    Assignee: Suzhou Zelgen Biopharmaceuticals Co., Ltd.
    Inventors: Binhua Lv, Chengwei Li
  • Patent number: 10265305
    Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: April 23, 2019
    Assignee: Poxel SA
    Inventors: Sheila DeWitt, Vincent Jacques, Leonardus van der Ploeg
  • Patent number: 9943521
    Abstract: The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: April 17, 2018
    Assignee: Gilead Sciences, Inc.
    Inventor: Gregory Notte
  • Patent number: 9896423
    Abstract: The present disclosure provides a deuterium substituted 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine compound with a structure represented by formula (I) or a derivative thereof, a pharmaceutical composition containing the compound or the derivative thereof, and an application of the compound or the derivative thereof in preparing drugs. The compound can reduce oxidative metabolism thereof, increase the drug concentration in blood and the effective bioavailability, so as to lower the dosage and reduce the toxicity and other side effects. The deuterium 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine compound and its derivative thereof provided by the present disclosure can be used to treat related diseases such as affective disorders, depression and anxiety.
    Type: Grant
    Filed: September 28, 2014
    Date of Patent: February 20, 2018
    Assignees: Jiangsu Jibeier Pharmaceutical Co., Ltd., Zhenjiang San An Pharmaceutical Co., Ltd.
    Inventors: Zhongyi Geng, Xinghai Chen, Parker Aulma, Wei Peng
  • Patent number: 9416117
    Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: August 16, 2016
    Assignee: DeuteRx, LLC
    Inventor: Sheila DeWitt
  • Patent number: 9328113
    Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentifylline and related compounds are beneficial.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: May 3, 2016
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger D. Tung, Bhaumik Pandya, Scott L. Harbeson
  • Patent number: 9226923
    Abstract: The present invention relates to spirocyclic compounds of formula I, namely spirocyclic (1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amines having protein kinase inhibitory activity, and methods of synthesizing and using such compounds. Preferred compounds are c-Met and/or ALK inhibitors useful for the treatment of abnormal cell growth, such as cancers.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: January 5, 2016
    Assignee: Nanjing Allgen Pharma Co. Ltd.
    Inventors: Zhaoyin Wang, Lianhai Li, Zhigang Wang
  • Patent number: 9169243
    Abstract: The present application relates to compounds having the inhibitory activity to apoptosis signal-regulating kinase (ASK1), thus are thus useful in treating ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: October 27, 2015
    Assignee: Gilead Sciences, Inc.
    Inventor: Gregory Notte
  • Patent number: 9040692
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: May 26, 2015
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20150141428
    Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 21, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Publication number: 20150126522
    Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
    Type: Application
    Filed: May 15, 2013
    Publication date: May 7, 2015
    Applicant: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Celine Duquenne, Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
  • Publication number: 20150111734
    Abstract: A pesticidal composition comprises at least one compounds selected from a compound of formula, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, Q, Z, L, La, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Yu Zhang, Asako Kubota, Noormohamed M. Niyaz, Thomas Barton, Tony K. Trullinger, Christian T. Lowe, Paul R. LePlae, Ann M. Buysse, Martin J. Walsh, Negar Garizi, Ricky Hunter, Daniel Knueppel
  • Publication number: 20150105388
    Abstract: This invention relates to new carboxamide-substituted heteroaryl-pyrazoles, method for their production, their use for the treatment and/or prophylaxis of diseases, as well as their use for the production of pharmaceutical agents for the treatment and/or prophylaxis of diseases, in particular retroviral diseases, in humans and/or animals.
    Type: Application
    Filed: November 29, 2012
    Publication date: April 16, 2015
    Applicant: AICURIS GMBH & CO. KG
    Inventors: Steffen Wildum, Burkhard Klenke, Astrid Wendt
  • Publication number: 20150105550
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8987258
    Abstract: The present invention relates to novel chromenone analog sirtuin modulator compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods and combination therapies thereof for use in increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: March 24, 2015
    Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Publication number: 20150072859
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 12, 2015
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul R. LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
  • Patent number: 8969581
    Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: March 3, 2015
    Assignee: DeuteRx, LLC
    Inventor: Sheila DeWitt
  • Publication number: 20150057280
    Abstract: The invention relates to pyridylidene compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted pyridylidene compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted pyridylidene compounds. The N-substituted pyridylidene compounds of the present invention are defined by the following formula I: wherein X, Het, R1, R2, R3, R4 and R6 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Applicant: BASF SE
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Korber
  • Publication number: 20150051402
    Abstract: Disclosed are thiazole methylamino pyridine compounds represented by the general formula (I) having fungicidal, insecticidal/acaricidal, and herbicidal activity, the preparation method thereof, the fungicidal, insecticidal/acaricidal, and herbicidal compositions containing the compounds of the present invention, and the use and the method for controlling fungi, insects/acari and weeds of the compounds of the present invention.
    Type: Application
    Filed: October 11, 2012
    Publication date: February 19, 2015
    Inventors: Aiping Liu, Xiaoguang Wang, Lian He, Xiaoming Ou, Minhua Liu, Ming Chen, Xingping Liu, Ming Tang, Yeguo Ren, Haobin Chen
  • Patent number: 8957070
    Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Patent number: 8957094
    Abstract: A therapeutic agent or prophylactic agent has an analgesic effect on both nociceptive pain and neuropathic pain and is effective in treatment of fibromyalgia. The agent includes as an effective ingredient a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: February 17, 2015
    Assignee: Toray Industries, Inc.
    Inventors: Chihiro Yoshida, Kaoru Nakao
  • Publication number: 20150045396
    Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like
    Type: Application
    Filed: March 18, 2013
    Publication date: February 12, 2015
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Akihiko Takeuchi, Hiroyuki Tsuchiya
  • Patent number: 8946231
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Craig M. Potteiger
  • Patent number: 8946435
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: February 3, 2015
    Assignee: Metabolic Solutions Development Company, LLC
    Inventors: Steven P. Tanis, Timothy Parker, Robert C. Gadwood, James R. Zeller, Gerald D. Artman, III, Scott D. Larsen
  • Patent number: 8946426
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
  • Patent number: 8946233
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: February 3, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20150025046
    Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.
    Type: Application
    Filed: February 27, 2013
    Publication date: January 22, 2015
    Inventors: Mihir Mandal, Timothy A. Blizzard, Helen Chen, Harry Chobanian, Yan Guo, Barbara Pio, Zhicai Wu, Tesfaye Biftu, William J. Greenlee, Johnny Zhaoning Zhu
  • Publication number: 20150018363
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: January 11, 2013
    Publication date: January 15, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Tsuyoshi Maekawa, Keiko Kakegawa, Tsuneo Yasuma, Asato Kina, Jumpei Aida, Uttam Khamrai, Mrinalkanti Kundu
  • Patent number: 8927551
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: January 6, 2015
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20150005279
    Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Applicant: ABBVIE INC.
    Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
  • Patent number: 8921370
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: December 30, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Publication number: 20140378687
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Inventors: Steven P. Tanis, Timothy Parker, Robert C. Gadwood, James R. Zeller, Gerald D. Artman, III, Scott D. Larsen
  • Publication number: 20140378511
    Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CYP17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 25, 2014
    Inventors: Roger Astbury Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
  • Publication number: 20140371276
    Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.
    Type: Application
    Filed: December 19, 2012
    Publication date: December 18, 2014
    Inventors: Alessio Moriconi, Gianluca Bianchini, Sandro Colagioia, Laura Brandolini, Andrea Aramini, Chiara Liberati, Silvia Bovolenta
  • Patent number: 8912335
    Abstract: The present invention relates to novel salts of thiazolidinediones and other pharmaceutical agents that are useful for treating and/or preventing metabolic diseases (e.g., diabetes, or neurodegenerative diseases (e.g., Alzheimer's Disease).
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: December 16, 2014
    Assignee: Metabolic Solutions Development Company, LLC
    Inventors: Gerard R. Colca, Steven P. Tanis, Scott D. Larsen
  • Publication number: 20140357675
    Abstract: Compounds are provided having an excellent hypoglycemic effect and ? cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Shigeo Yamanoi, Hidenori Namiki, Yuichi Ochiai, Madoka Hoshino, Koji Matsumoto
  • Patent number: 8901121
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: December 2, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
  • Patent number: 8895748
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: November 25, 2014
    Assignee: Metabolic Solutions Development Company, LLC
    Inventors: Steven P. Tanis, Timothy Parker, Robert C. Gadwood, James R. Zeller, Gerald D. Artman, III, Scott D. Larsen
  • Publication number: 20140336168
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 13, 2014
    Inventor: AbbVie Inc.
  • Publication number: 20140329796
    Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
  • Publication number: 20140315913
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20140303213
    Abstract: The present invention relates to the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. Also provided are methods for the treatment and/or prevention of one or more metabolic disorders, for example, obesity or diabetes, utilizing fatostatin A and/or a derivative and/or analog thereof and/or the A-B-C tripartite compounds.
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Mizuki Watanabe
  • Publication number: 20140303157
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: August 27, 2012
    Publication date: October 9, 2014
    Inventors: William J. Hoekstra, Robert J. Schotzinger
  • Publication number: 20140296515
    Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Alexandros VAKALOPOULOS, Daniel MEIBOM, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Jörg KELDENICH, Hans-Georg LERCHEN, Peter NELL, Frank SÜßMEIER, Ursula KRENZ
  • Publication number: 20140296239
    Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicant: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
  • Publication number: 20140296295
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Walter HÜBSCH, Daniel MEIBOM, Alexandros VAKALOPOULOS, Barbara ALBRECHT-KÜPPER, Peter NELL, Katja ZIMMERMANN, Frank SÜßMEIER, Joerg KELDENICH
  • Patent number: RE48286
    Abstract: The invention relates to compounds of formula (I): wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
    Type: Grant
    Filed: June 21, 2019
    Date of Patent: October 27, 2020
    Assignee: Intercept Pharmaceuticals, Inc.
    Inventor: Roberto Pellicciari