C=o Bonded Directly To The Hetero Ring (x Is Chalcogen) Patents (Class 514/448)
  • Patent number: 11027219
    Abstract: Disclosed is an oxidation process to produce a crude carboxylic acid product carboxylic acid product. The process comprises oxidizing a feed stream comprising at least one oxidizable compound to generate a crude carboxylic acid slurry comprising furan-2,5-dicarboxylic acid (FDCA) and compositions thereof. Also disclosed is a process to produce a dry purified carboxylic acid product by utilizing various purification methods on the crude carboxylic acid.
    Type: Grant
    Filed: August 27, 2019
    Date of Patent: June 8, 2021
    Assignee: Eastman Chemical Company
    Inventors: Kenny Parker, Mesfin Janka, Ashfaq Shaikh, Lee Partin
  • Patent number: 10085962
    Abstract: Compounds, methods, and compositions are provided for the treatment of cancer, neurological disorders, and fibrotic disorders. Specifically, the invention includes administering an effective amount of a compound of Formula I, II, or III, or a pharmaceutically acceptable composition, salt, isotopic analog, prodrug, or combination thereof, to a subject suffering from a cancer, neurological disorder, or fibrotic disorder.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: October 2, 2018
    Assignee: Avoscience, LLC
    Inventor: Richard Huber
  • Patent number: 9814694
    Abstract: Compounds, methods, and compositions are provided for the treatment of cancer, neurological disorders, and fibrotic disorders. Specifically, the invention includes administering an effective amount of a compound of Formula I, II, or III, or a pharmaceutically acceptable composition, salt, isotopic analog, prodrug, or combination thereof, to a subject suffering from a cancer, neurological disorder, or fibrotic disorder.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: November 14, 2017
    Assignee: Avioscience, LLC
    Inventor: Richard Huber
  • Patent number: 9770022
    Abstract: The present invention relates to fungicidal N-cycloalkyl-N-[(bicyclylphenyl)methylene]carboxamide derivatives and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: September 26, 2017
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Jurgen Benting, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Philippe Rinolfi, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann
  • Patent number: 9504994
    Abstract: Disclosed is an oxidation process to produce a crude carboxylic acid product carboxylic acid product. The process comprises oxidizing a feed stream comprising at least one oxidizable compound to generate a crude carboxylic acid slurry comprising furan-2,5-dicarboxylic acid (FDCA) and compositions thereof. Also disclosed is a process to produce a dry purified carboxylic acid product by utilizing various purification methods on the crude carboxylic acid.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: November 29, 2016
    Assignee: EASTMAN CHEMICAL COMPANY
    Inventors: Mesfin Janka, Kenny Parker, Ashfaq Shaikh, Lee Partin
  • Patent number: 9365485
    Abstract: Disclosed herein is a compound of the formula Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.
    Type: Grant
    Filed: May 8, 2014
    Date of Patent: June 14, 2016
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 9200047
    Abstract: The invention describes HLA class II binding peptides encoded by the SSX-2 tumor associated gene, as well as nucleic acids encoding such peptides and antibodies relating thereto. The peptides stimulate the activity and proliferation of CD4+ T lymphocytes. Methods and products also are provided for diagnosing and treating conditions characterized by expression of the SSX-2 gene.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: December 1, 2015
    Assignee: Ludwig Institute for Cancer Research, Ltd.
    Inventors: Danila Valmori, Maha Ayyoub
  • Patent number: 9156806
    Abstract: A process to produce a dry purified furan-2,5-dicarboxylic acid (FDCA) is described. After oxidation of 5-(hydroxymethyl)furfural (5-HMF), a crude FDCA stream is produced that is fed to a crystallization zone followed by a solid-liquid displacement zone to form a low impurity slurry stream. The solids in the low impurity slurry stream are dissolved in a dissolution zone to produce a hydrogenation feed that is hydrogenated in a hydrogenation reactor to generate a hydrogenated FDCA composition. The hydrogenated FDCA composition is routed to a crystallization zone to form a crystallized produce stream that is separated from liquid in a solid-liquid separation zone to generate a purified wet cake stream containing FDCA that can be dried in a drying zone to generate a dry purified FDCA product stream.
    Type: Grant
    Filed: April 23, 2014
    Date of Patent: October 13, 2015
    Assignee: Eastman Chemical Company
    Inventors: Ashfaq Schahanawaz Shaikh, Kenny Randolph Parker, Mesfin Ejerssa Janka, Lee Reynolds Partin
  • Publication number: 20150140081
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140080
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140077
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140076
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140078
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150141427
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150140079
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140075
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150126559
    Abstract: The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 7, 2015
    Applicant: UNIVERSITA DEGLI STUDI DI FERRARA
    Inventors: Jan Balzarini, Wim Dehaen, Joice Thomas, Sandra Liekens, Romeo Romagnoli, Pier Giovanni Baraldi
  • Patent number: 9024042
    Abstract: Compositions and methods for treating glaucoma are provided. In particular hydrophilic ester prodrugs and their use to reduce central corneal thickening is provided.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: May 5, 2015
    Assignee: Allergan, Inc.
    Inventors: Wha-Bin Im, Robert M. Burk
  • Patent number: 9023885
    Abstract: The invention relates to pharmaceutical compositions and methods of treating inflammatory-related diseases associated with pro-inflammatory cytokine expression and/or reduced expression of anti-inflammatory cytokines. The method typically comprises administration of one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA. Preferably the pharmaceutical composition comprises one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, an anti-inflammatory agent, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: May 5, 2015
    Assignee: Natrogen Therapeutics International, Inc.
    Inventors: Longgui Wang, Xiao Mei Liu, Lian Mo, Simon K. Mencher, James P. McCarron, Jr.
  • Publication number: 20150119454
    Abstract: Described herein are well-defined cyclopentanols useful for treating glaucoma and ocular hypertension.
    Type: Application
    Filed: October 29, 2014
    Publication date: April 30, 2015
    Inventors: Robert M. Burk, Todd S. Gac
  • 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: 9006283
    Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: April 14, 2015
    Assignee: Acumen Pharmaceuticals, Inc.
    Inventors: Grant A. Krafft, Todd Pray, William F. Goure
  • Patent number: 9006249
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 9006464
    Abstract: Disclosed herein are compounds having a formula: Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Grant
    Filed: November 5, 2008
    Date of Patent: April 14, 2015
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen, Robert M. Burk
  • Publication number: 20150099636
    Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 9, 2015
    Inventors: Robert Eugene HORMANN, Bing Li
  • 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
  • Patent number: 9000032
    Abstract: Disclosed herein are compounds having a formula: or a pharmaceutically acceptable salt thereof, as well as therapeutic methods, medicaments, and compositions related thereto.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: April 7, 2015
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 8969404
    Abstract: A process for purifying a crude furan 2,5-dicarboxylic acid composition (cFDCA) by hydrogenation of a FDCA composition dissolved in a hydrogenation solvent such as water, and hydrogenating under mild conditions, such as at a temperature within a range of 130° C. to 225° C. by contacting the solvated FDCA composition with hydrogen in the presence of a hydrogenation catalyst under a hydrogen partial pressure within a range of 10 psi to 900 psi. A product FDCA composition is produced having a low amount of tetrahydrofuran dicarboxylic acid, a low b*, and a low amount of 5-formyl furan-2-carboxylic acid (FFCA).
    Type: Grant
    Filed: February 4, 2013
    Date of Patent: March 3, 2015
    Assignee: Eastman Chemical Company
    Inventors: Mesfin Ejerssa Janka, Charles Edwan Sumner, Jr., Shane Kipley Kirk, Ashfaq Shahanawaz Shaikh, Kenny Randolph Parker
  • 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
  • Patent number: 8952031
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: February 10, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Patent number: 8946451
    Abstract: The invention relates to lipoic acid acylated salicylate derivatives; compositions comprising an effective amount of a lipoic acid acylated salicylate derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a lipoic acid acylated salicylate derivative.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: February 3, 2015
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Publication number: 20150023868
    Abstract: The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders.
    Type: Application
    Filed: February 21, 2014
    Publication date: January 22, 2015
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Othon Iliopoulos, Michael Zimmer
  • Publication number: 20150005320
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 1, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
  • Publication number: 20140378459
    Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: December 25, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Jiro Fujiyasu, Kazuhiko Ohne, Susumu Yamaki, Tomoyoshi Imaizumi, Takeshi Hondo, Keisuke Matsuura, Tomohki Satou, Satoshi Sasamura
  • Publication number: 20140357705
    Abstract: Disclosed herein are compounds having a formula: or a pharmaceutically acceptable salt thereof, as well as therapeutic methods, medicaments, and compositions related thereto.
    Type: Application
    Filed: May 30, 2014
    Publication date: December 4, 2014
    Applicant: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20140348850
    Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.
    Type: Application
    Filed: August 15, 2014
    Publication date: November 27, 2014
    Inventors: Edward P. Feener, Allen Clermont
  • Patent number: 8895552
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: November 25, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Publication number: 20140343108
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel amidated derivatives of oleanolic acid according to formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Inventors: Frank Rong, Rongzhen Xu, Fuwen Xie, Hongxi Lai
  • Patent number: 8889732
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: November 18, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • 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: 20140323558
    Abstract: The invention provides well-defined compounds that are either EP2 agonists, EP4 agonists, or mixed EP2/EP4 agonist. The compounds are useful for treating a variety of pathological conditions associated with activity of the EP2 and/or EP4 receptors.
    Type: Application
    Filed: April 29, 2014
    Publication date: October 30, 2014
    Applicant: Allergan, Inc.
    Inventor: David W. Old
  • Publication number: 20140309264
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, 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: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK
  • Publication number: 20140302069
    Abstract: Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 9, 2014
    Inventors: David Fairlie, Robert C. Reid
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Publication number: 20140235681
    Abstract: Disclosed herein is method of treating glaucoma or ocular hypertension comprising administering a prostaglandin agonist and a second therapeutically active agent to a mammal in need thereof, wherein said second therapeutically active agent is selected from: ?-Blockers, Adrenergic Agonists, non-selective adrenergic agonists, ?2-selective adrenergic agonists, Carbonic Anhydrase Inhibitors, Cholinergic Agonists, direct acting cholinergic agonists, chlolinesterase inhibitors, Glutamate Antagonists, Ca2+ channel blockers, Prostamides, Prostaglandins, Cannabinoids, and combinations thereof. Compositions and medicaments containing a combination of these two active agents are also disclosed.
    Type: Application
    Filed: December 6, 2013
    Publication date: August 21, 2014
    Applicant: ALLERGAN, INC.
    Inventors: SCOTT M. WHITCUP, ROBERT M. BURK, DAVID W. OLD, YARIV DONDE, WHA-BIN IM, MARK A. HOLOBOSKI
  • Publication number: 20140228416
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: September 12, 2013
    Publication date: August 14, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20140213552
    Abstract: The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 31, 2014
    Applicant: Endo Pharmaceuticals Inc.
    Inventors: Scott Kevin Thompson, Roger Astbury Smith, Sandeep Gupta, Tony Priestley, Nicholas James Laping, Ashis K. Saha, Sonali Rudra
  • Publication number: 20140213611
    Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.
    Type: Application
    Filed: July 6, 2012
    Publication date: July 31, 2014
    Applicant: KalVista Pharmaceuticals Limited
    Inventors: David Michael Evans, Rebecca Louise Davie, Hannah Joy Edwards, David Philip Rooker
  • Patent number: RE48150
    Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 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. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
    Type: Grant
    Filed: January 3, 2017
    Date of Patent: August 11, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Gregory Notte, Jeff Zablocki