Additional Chalcogen Containing Hetero Ring Patents (Class 514/382)
  • Patent number: 9486442
    Abstract: The invention is directed to methods of treating organ specific infections in a host organism by administering compounds that target host receptors and/or host cellular signaling molecules to prevent a pathogen from infecting the organ. For example, the administration of a compound to prevent a pathogen from crossing the blood-brain barrier to prevent a brain infection.
    Type: Grant
    Filed: February 3, 2015
    Date of Patent: November 8, 2016
    Assignee: The Johns Hopkins University
    Inventor: Kwang S. Kim
  • Patent number: 9408405
    Abstract: The present invention relates to the use of one or more compounds that are capable of increasing the serum level of insulin-like growth factor 1 (IGF-1) for the preparation of a therapeutical composition, in particular in the form of a food supplement, for the treatment of subjects suffering from serious fatigue and exhausting symptoms, burn-out and chronic fatigue syndrome. The same composition can also be used by patients suffering from depression, Alzheimer disease, irritated bowel syndrome, osteoporosis, type 2 diabetes, or for anti-aging, immune therapy and recovery after exercise. The composition also has a use in veterinary applications for increasing the growth and immunity in animals.
    Type: Grant
    Filed: October 3, 2003
    Date of Patent: August 9, 2016
    Assignee: Veijlen N.V.
    Inventors: Hubert Jean Marie François Gillessen, Christian Rebiere
  • Patent number: 9309227
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: April 12, 2016
    Assignees: The Scripps Research Institute, Ember Therapeutics, Inc.
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Amy S. Ripka, Jeffrey O. Saunders
  • Patent number: 9283218
    Abstract: The present invention relates to an amorphous solid dispersion comprising a tetrazole derivative of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The solid dispersion of the present invention comprises a water-soluble polymer or an acid so as to improve the solubility of its active ingredient, i.e., the tetrazole derivative of the formula (I), thereby improving its absorption rate, and thus can be effectively used to reduce multi-drug resistance (MDR) in cancer cells.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: March 15, 2016
    Assignee: HANMI PHARM. CO., LTD
    Inventors: Yong Il Kim, Jun Young Choi, Young Keun Choi, Jae Hyun Park, Jong Soo Woo
  • Publication number: 20150148389
    Abstract: The invention is directed to methods of treating organ specific infections in a host organism by administering compounds that target host receptors and/or host cellular signaling molecules to prevent a pathogen from infecting the organ. For example, the administration of a compound to prevent a pathogen from crossing the blood-brain barrier to prevent a brain infection.
    Type: Application
    Filed: February 3, 2015
    Publication date: May 28, 2015
    Inventor: Kwang S. Kim
  • Publication number: 20150148388
    Abstract: The present invention is directed to stable chemical compositions and dosage forms that comprise nebivolol and valsartan and which achieve therapeutically effective plasma levels of both actives in hypertensive patients following administration, as well as to methods of lowering blood pressure and treating hypertension using such compositions and dosage forms.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Inventors: Anil Chhettry, Mahendra G. Dedhiya, Kinjal Suchak, Stephan Ortiz, Chun Lin Chen
  • Patent number: 9040530
    Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 26, 2015
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
  • Patent number: 9034906
    Abstract: Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1-4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: May 19, 2015
    Assignees: Asahi Glass Company, Limited, Kaken Pharmaceutical Co., Ltd.
    Inventors: Takahiko Murata, Masahiro Amakawa, Shin Teradaira, Yasushi Matsumura, Katsuhiko Konishi
  • Publication number: 20150126371
    Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.
    Type: Application
    Filed: May 29, 2013
    Publication date: May 7, 2015
    Inventors: Matthias Witschel, Frank Stelzer, Johannes Hutzler, Tao Qu, Thomas Mietzner, Klaus Kreuz, Klaus Grossmann, Raphael Aponte, Hans Wolfgang Hoeffken, Frederick Calo, Thomas Ehrhardt, Anja Simon, Liliana Parra Rapado
  • Publication number: 20150119329
    Abstract: The present invention is directed to a composition for the treatment or prevention of cerebral malaria that comprises an angiotensin receptor type-2 agonist and an antimalaria drug. The present invention is further directed to methods for treating and preventing cerebral malaria that involve administering an angiotensin receptor type-2 agonist and/or an angiotensin receptor type-1 antagonist.
    Type: Application
    Filed: April 16, 2013
    Publication date: April 30, 2015
    Applicant: NEW YORK UNIVERSITY
    Inventors: Ana Maria Rodriguez Fernandez, Julio Gallego-Delgado
  • Publication number: 20150111889
    Abstract: The present invention relates to compounds of the formula (I), wherein the residues A, R1 to R5, Z1 and Z2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 16, 2013
    Publication date: April 23, 2015
    Applicant: SANOFI
    Inventors: Marc Nazare, Detlef Kozian, Martin Bossart, Werngard Czechtizky, Andreas Evers
  • Patent number: 9012655
    Abstract: Among other things, in general, antimicrobial and/or adjuvant compounds are provided according to Formula Ia: (Ia) in which E and R1-11 have the meanings described herein; and prodrugs and pharmaceutically acceptable salts thereof. Other formulae and methods of use are also provided.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: April 21, 2015
    Assignee: Denouamed, Inc.
    Inventors: Fan Wu, Erhu Lu, Christopher J. Barden
  • 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
  • Publication number: 20150099733
    Abstract: Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 9, 2015
    Applicant: AJINOMOTO CO., INC.
    Inventors: Takahiro KOSHIBA, Munetaka TOKUMASU, Taisuke ICHIMARU, Koji OHSUMI, Tadakiyo NAKAGAWA, Tatsuhiro YAMADA, Kayo MATSUMOTO, Tamotsu SUZUKI
  • Publication number: 20150094304
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
  • Patent number: 8987457
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: March 24, 2015
    Assignee: Novartis AG
    Inventors: Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Publication number: 20150065516
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: October 29, 2014
    Publication date: March 5, 2015
    Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Halyan Wang
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 8969394
    Abstract: The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included. (Formulas I and II).
    Type: Grant
    Filed: August 10, 2007
    Date of Patent: March 3, 2015
    Assignee: Merck Frosst Canada Ltd.
    Inventors: Marc Blouin, Jason Burch, Yongxin Han, Christophe Mellon
  • Publication number: 20150057238
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 26, 2015
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
  • Patent number: 8962671
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R11, R30, R40, R50 and R60 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: Grant
    Filed: January 24, 2012
    Date of Patent: February 24, 2015
    Assignee: Sanofi
    Inventors: Sven Ruf, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Thomas Olpp, Klaus Wirth
  • Publication number: 20150018400
    Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.
    Type: Application
    Filed: May 2, 2014
    Publication date: January 15, 2015
    Inventors: YARIV DONDE, JEREMIAH H. NGUYEN, KAREN M. KEDZIE, DANIEL W. GIL, JOHN E. DONELLO, WHA-BIN IM
  • Publication number: 20150018401
    Abstract: Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1-4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Inventors: Takahiko MURATA, Masahiro AMAKAWA, Shin TERADAIRA, Yasushi MATSUMURA, Katsuhiko KONISHI
  • Publication number: 20150018399
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: August 5, 2014
    Publication date: January 15, 2015
    Inventors: SONGNIAN LIN, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
  • Publication number: 20140378457
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
  • Patent number: 8912199
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: December 16, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Patent number: 8911765
    Abstract: A biodegradable, flexible covering for a breast implant is provided which comprises one or more biodegradable polymer layers dimensioned and shaped to cover at least a portion of the breast implant. The implant can be inserted into an opening of the covering immediately prior to surgery, but alternate configurations and times of insertion are contemplated as well as open or sheet type devices. The coverings can optionally contain one or more drugs for delivery at the surgical site, particularly for treating or preventing infection, pain, inflammation, capsular contracture, scarring or other complications associated with breast augmentation or breast reconstruction.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: December 16, 2014
    Assignee: Tyrx, Inc.
    Inventors: Arikha Moses, Satish Pulapura, Qing Ge, Sarita Nethula, Irene Shatova, Archana Rajaram
  • Publication number: 20140349973
    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: December 10, 2012
    Publication date: November 27, 2014
    Applicant: Viamet Pharmaceuticals, Inc
    Inventors: William J. Hoekstra, Christopher M. Yates
  • Publication number: 20140328917
    Abstract: An organic compound nano-powder comprising a granular organic compound with an average particle diameter of 500 nm or less and a 90%-diameter of less than 1500 nm and a carbohydrate compound comprising at least any one of a sugar and a sugar alcohol and with amount of 0.3 times or more by mass relative to amount of the organic compound, a method for producing the same, and a suspension having the organic compound dispersed in a liquid dispersion medium in which the organic compound is insoluble or poorly soluble.
    Type: Application
    Filed: May 11, 2013
    Publication date: November 6, 2014
    Inventors: Takahiro Tada, Kazuhiro Kagami, Shiro Yokota
  • Patent number: 8877787
    Abstract: Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1-4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: November 4, 2014
    Assignees: Asahi Glass Company, Limited, Kaken Pharmaceutical Co., Ltd.
    Inventors: Takahiko Murata, Masahiro Amakawa, Shin Teradaira, Yasushi Matsumura, Katsuhiko Konishi
  • Publication number: 20140323510
    Abstract: Disclosed herein is a compound of the formula Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.
    Type: Application
    Filed: May 8, 2014
    Publication date: October 30, 2014
    Applicant: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20140309265
    Abstract: The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer.
    Type: Application
    Filed: November 9, 2012
    Publication date: October 16, 2014
    Inventors: Benjamin Adam Seigal, Nicholas Terrett, Percy H. Carter, Robert M. Borzilleri, Yong Zhang, Michael M. Miller
  • Publication number: 20140308243
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—Z—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: April 16, 2014
    Publication date: October 16, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Zhigang Chen, Yat Sun Or
  • Publication number: 20140309266
    Abstract: Among other things, in general, antimicrobial and/or adjuvant compounds are provided according to Formula Ia: (Ia) in which E and R1-11 have the meanings described herein; and prodrugs and pharmaceutically acceptable salts thereof. Other formulae and methods of use are also provided.
    Type: Application
    Filed: March 2, 2012
    Publication date: October 16, 2014
    Applicant: DENOVAMED INC.
    Inventors: Fan Wu, Erhu Lu, Christopher J. Barden
  • Patent number: 8859600
    Abstract: Acetone solvate crystals of trityl olmesartan medoxomil are provided.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: October 14, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hiroshi Kiyota, Hideaki Ishikawa
  • Publication number: 20140302125
    Abstract: There is provided a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more calcium channel blocker, angiotensin II receptor blocker or angiotensin converting enzyme inhibitor along with one or more rate controlling excipient.
    Type: Application
    Filed: August 23, 2012
    Publication date: October 9, 2014
    Applicant: Wockhardt Ltd.
    Inventors: Mandar Madhukar Kodgule, Premchand Dalichandji Nakhat, Amit Gupta, Girish Kumar Jain
  • Patent number: 8846736
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: September 30, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140288042
    Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds 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: Application
    Filed: October 25, 2012
    Publication date: September 25, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
  • Publication number: 20140275185
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: May 30, 2014
    Publication date: September 18, 2014
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • Publication number: 20140275020
    Abstract: This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds 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: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
  • Patent number: 8835476
    Abstract: The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: September 16, 2014
    Inventors: Fan Wu, Donald Weaver, Chris Barden, Christopher McMaster, David Byers, Annette Henneberry, Fuqiang Ban
  • Publication number: 20140235683
    Abstract: Compositions and methods for the treatment of norovirus infection are disclosed.
    Type: Application
    Filed: July 9, 2012
    Publication date: August 21, 2014
    Applicants: Alios Biopharma Inc., Indiana University Research & Technology Corporation
    Inventors: Ch. V. Subba-Reddy, C. Cheng Kao, Dave Smith, Leo Beigelman
  • Patent number: 8802707
    Abstract: This invention is a method of killing the stealthy intra-cellular bacteria which are key to the pathogenesis Cancers. These very tiny L-form Cell-Wall-Deficient (CWD) antibiotic-resistant bacteria live within the cytoplasm of cells, including the phagocytic cells (e.g. monocytes, macrophages, lymphocytes, neutrophils and polymorphonuclear cells) of the immune system itself. The cellular proliferation in Cancer is catalysed the action of the same tiny L-form bacteria. They cause the cell nucleus to release mRNA signaling the Th1 cytokine cascade without the need for conventional signaling via, for example, CD4+T -Lymphocytes. Some of these Cytokines and Chemokines, including, without limitation, Cellular Adhesion Molecule (CAM), create the environment which allows the cellular proliferation to start, and then allows the cancerous growth to gain a foothold in the body. Killing these stealthy pathogens removes the environment needed to initiate and feed the cellular proliferation commonly called ‘Cancer’.
    Type: Grant
    Filed: July 31, 2006
    Date of Patent: August 12, 2014
    Inventor: Trevor Gordon Marshall
  • Patent number: 8791143
    Abstract: The present invention relates to novel anthranilic diamide derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: July 29, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Arnd Voerste, Ulrich Görgens
  • Patent number: 8778938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
  • Publication number: 20140194481
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140171445
    Abstract: The invention provides a method of enhancing the efficacy of antibiotic treatment of tuberculosis, trypanosomiasis, leprosy, and leishmaniasis involving co-administering to a mammal undergoing antibiotic treatment therapeutically effective amounts of a first compound that is an inhibitor of 5-lipoxygenase and optionally a second compound that is a product of the cyclooxygenase pathways. The invention also provides a pharmaceutical composition comprising an antibiotic, an inhibitor of 5-lipoxygenase, and a product of the cyclooxygenase pathways.
    Type: Application
    Filed: August 2, 2012
    Publication date: June 19, 2014
    Applicant: The USA, as represented by the Secretary, Department of Health and Human Services
    Inventors: Katrin Mayer-Barber, Bruno de Bezerril Andrade, Alan Sher, Daniel Leo Barber
  • Publication number: 20140163025
    Abstract: The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R1 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 12, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Elke LANGKOPF, Holger WAGNER
  • Publication number: 20140135322
    Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 15, 2014
    Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
  • Publication number: 20140128441
    Abstract: Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1-4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.
    Type: Application
    Filed: January 9, 2014
    Publication date: May 8, 2014
    Applicants: Kaken Pharmaceutical Co., Ltd., Asahi Glass Company, Limited
    Inventors: Takahiko MURATA, Masahiro AMAKAWA, Shin TERADAIRA, Yasushi MATSUMURA, Katsuhiko KONISHI