Chalcogen Bonded Directly To Ring Carbon Of The Additional Six-membered Nitrogen Containing Hetero Ring Patents (Class 514/253.12)
  • Patent number: 10350205
    Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds useful as modulators of MAGL and/or FAAH. The subject compounds and compositions are useful for the treatment of pain and neurological disorders.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: July 16, 2019
    Assignee: Abide Therapeutics, Inc.
    Inventors: Cheryl A. Grice, Justin S. Cisar, Katharine K. Duncan, Yu Feng, John J. M. Wiener, Olivia D. Weber
  • Patent number: 10294236
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: May 21, 2019
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Mui Cheung, Michael P. Demartino, Hilary Schenck Eidam, Huiping Amy Guan, Donghui Qin, Chengde Wu, Zhen Gong, Haiying Yang, Haiyu Yu, Zhiliu Zhang
  • Patent number: 10292975
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: May 21, 2019
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Michael P. Demartino, Huiping Amy Guan
  • Patent number: 10111866
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: October 30, 2018
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Michael P. Demartino, Huiping Amy Guan
  • Patent number: 9656978
    Abstract: The present invention relates to novel compounds of Formula I capable of inhibiting tissue transglutaminase, and uses of the same in medicine. In particular, the invention provides compounds for use in the treatment of prevention of disease and conditions such as fibrosis (e.g. cystic fibrosis), scarring, neurodegenerative diseases (e.g. Alzheimer's disease, Huntington's disease and Parkinson's disease), autoimmune diseases (e.g. multiple sclerosis and coeliac disease), thrombosis, proliferative disorders (e.g. cancers), AIDS, psoriasis and inflammation (e.g. chronic inflammatory diseases).
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 23, 2017
    Assignee: ASTON UNIVERSITY
    Inventors: Martin Griffin, Daniel Rathbone, Leonas Eduard Badarau
  • Patent number: 9439434
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: September 13, 2016
    Assignee: Inscent, Inc.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Patent number: 9079891
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: July 14, 2015
    Assignee: CALCIMEDICA, INC.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 9056859
    Abstract: This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: June 16, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Reynalda K. deJesus, Yuping Zhu, Lihu Yang, Shawn Walsh, Haifeng Tang, Dooseop Kim, Barbara Pio, Aurash Shahripour, Kevin Belyk
  • Patent number: 9045495
    Abstract: Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1?), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: June 2, 2015
    Assignee: AERPIO THERAPEUTICS INC.
    Inventors: Joseph H. Gardner, Robert Shalwitz
  • Patent number: 9045390
    Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: June 2, 2015
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Gorgens, Jan Dittgen, Dieter Feucht, Isolde Hauser-Hahn, Christopher Hugh Rosinger, Alfred Angermann
  • Patent number: 9034874
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: May 19, 2015
    Assignee: NOVARTIS AG
    Inventors: Yves Auberson, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Patent number: 9029381
    Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: May 12, 2015
    Assignee: Astrazeneca AB
    Inventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
  • 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: 20150099762
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Inventors: Hilary Schenck EIDAM, Kaushik RAHA, Zhen GONG, Huiping Amy GUAN, Chengde WU, Haiying YANG, Haiyu YU, Zhiliu ZHANG, Mui CHEUNG
  • Patent number: 8999971
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: April 7, 2015
    Assignee: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Publication number: 20150087635
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: December 4, 2014
    Publication date: March 26, 2015
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Publication number: 20150087639
    Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
    Type: Application
    Filed: July 18, 2013
    Publication date: March 26, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
  • Patent number: 8980890
    Abstract: The invention relates to compounds and methods for treating cell proliferation disorders.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: March 17, 2015
    Assignee: Kinex Pharmaceuticals, LLC
    Inventor: David G. Hangauer, Jr.
  • Publication number: 20150050237
    Abstract: The present invention relates to the field of anti-mycobacterial therapeutics, in particular the treatment of tuberculosis, especially including pulmonary multidrug-resistant tuberculosis (MDR-TB), with applications in extensively drug-resistant tuberculosis (XDR-TB) and extremely drug-resistant tuberculosis (XXDR-TB), preferably in combination therapy.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 19, 2015
    Inventors: Vasu Nair, Maurice O. Okello, Machhindra G. Gund, Byung I. Seo, Pankajkumar R. Singh, Naveen K. Mangu
  • Patent number: 8937071
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 20, 2015
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck Eidam, Kaushik Raha, Zhen Gong, Huiping Amy Guan, Chengde Wu, Haiying Yang, Haiyu Yu, Zhiliu Zhang, Mui Cheung
  • 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: 20150005315
    Abstract: Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
    Type: Application
    Filed: December 10, 2012
    Publication date: January 1, 2015
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, James B. Thomas, Hernan A. Navarro, S. Wayne Mascarella, Scott P. Runyon, Chunyang Jin, Chad M. Kormos
  • Publication number: 20140378471
    Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
  • Publication number: 20140364419
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Patent number: 8901116
    Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.
    Type: Grant
    Filed: September 16, 2013
    Date of Patent: December 2, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Byong Sung Kwak, Hong Sik Moon, Han-Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
  • Patent number: 8895562
    Abstract: The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: July 29, 2009
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Michiel Luc Maria Van Gool
  • Publication number: 20140343059
    Abstract: Disclosed are novel piperazine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
    Type: Application
    Filed: July 29, 2014
    Publication date: November 20, 2014
    Inventors: Roger B. CLARK, Daniel ELBAUM
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Publication number: 20140336165
    Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.
    Type: Application
    Filed: November 14, 2012
    Publication date: November 13, 2014
    Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
  • Patent number: 8883776
    Abstract: Certain cycloalkyloxy- and heterocycloalkyloxypyridine compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Grant
    Filed: November 17, 2008
    Date of Patent: November 11, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael A. Letavic, Emily M. Stocking
  • Patent number: 8883774
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: November 11, 2014
    Assignee: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Publication number: 20140315884
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 23, 2014
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20140315903
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: HASSAN JULIEN IMOGAI, JOSE MARIA CID-NUNEZ, JOSE IGNACIO ANDRES-GIL, ANDRES AVELINO TRABANCO-SUAREZ, JULEN OYARZABAL SANTAMARINA, FRANK MATTHIAS DAUTZENBERG, GREGOR JAMES MACDONALD, SHRILEY ELIZABETH PULLAN, ROBERT JOHANNES LUTJENS, GUILLAUME ALBERT JACQUES DUVEY, VANTHEA NHEM, TERRY PATRICK FINN, GAGIK MELIKYAN
  • Publication number: 20140309192
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complication(s) resulting from elevated blood pressure and/or reduced tissue perfusion.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: Thuy-Anh Tran, Anthony C. Blackburn, Bryan A. Kramer, Maiko Nagura, Carleton R. Sage, Young-Jun Shin, Ning Zou
  • Publication number: 20140296253
    Abstract: The present invention provides: a novel compound which has a useful pharmacological action for treating heart failure or shock without increasing heart rate; and a pharmaceutical composition using the same. The present invention relates to a diphenylmethyl piperazine derivative represented by general formula (I) (In the formula, R1 is a hydrogen atom or a hydroxy group. R2 is a hydrogen atom, a halogen atom, a hydroxy group, an alkyl group having one to five carbon atoms, or an alkoxyl group having one to five carbon atoms, excluding the case where R1 is a hydroxy group and R2 is a chlorine atom.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 2, 2014
    Applicant: AETAS PHARMA CO., LTD.
    Inventor: Noboru Kaneko
  • Publication number: 20140288045
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Publication number: 20140288086
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Applicants: PFIZER INC., AGOURON PHARMACEUTICALS, INC.
    Inventors: Jingrong Jean CUI, Lee Andrew FUNK, Lei JIA, Pei-Pei KUNG, Jerry Jialun MENG, Mitchell David NAMBU, Mason Alan PAIRISH, Hong SHEN, Michelle TRAN-DUBE
  • Publication number: 20140275111
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck EIDAM, Kaushik Raha, Zhen Gong, Huiping Guan, Chengde Wu, Haiying Yang, Haiyu Yu, Zhiliu Zhang, Mui CHEUNG
  • Publication number: 20140275016
    Abstract: Described are compounds of Formula 1 which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Thiwanka Samarakoon, Lakshminarayana Vogeti, Michael D. Kaufman, William C. Patt, YuMi Ahn
  • Patent number: 8829003
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilizing or immobilizable derivative thereof; wherein: any one or two of X.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: September 9, 2014
    Assignee: Changzhou Le Sun Pharmaceuticals Limited
    Inventors: Shudong Wang, Osama Chahrour, Tiangong Lu, Anran Hu
  • Patent number: 8815869
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: August 26, 2014
    Assignee: AbbVie Inc.
    Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
  • Publication number: 20140235609
    Abstract: The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for treating diseases connected to tehinhibition of H3 receptor.
    Type: Application
    Filed: October 8, 2012
    Publication date: August 21, 2014
    Inventors: Tie-Lin Wang, Xuechun Zhang
  • Publication number: 20140221392
    Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.
    Type: Application
    Filed: December 27, 2013
    Publication date: August 7, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
  • Publication number: 20140221391
    Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.
    Type: Application
    Filed: December 27, 2013
    Publication date: August 7, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
  • Publication number: 20140213580
    Abstract: Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.
    Type: Application
    Filed: June 18, 2012
    Publication date: July 31, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
  • Patent number: 8785632
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: July 22, 2014
    Assignees: Agouron Pharmaceuticals, Inc., Pfizer Inc.
    Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
  • Patent number: 8765739
    Abstract: Compounds of formula [I]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salts or solvates thereof.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: July 1, 2014
    Assignee: Japan Tobacco Inc.
    Inventors: Kazutaka Ikegashira, Taku Ikenogami, Naoki Ogawa, Tatsuya Matsumoto, Takahiro Oka, Takuya Matsuo, Takayuki Yamasaki
  • Publication number: 20140163017
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 19, 2013
    Publication date: June 12, 2014
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140163036
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: July 17, 2013
    Publication date: June 12, 2014
    Inventors: Yves AUBERSON, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang