The Additional Hetero Ring Is A Five-membered Nitrogen Hetero Ring Patents (Class 514/252.05)
  • Patent number: 10370406
    Abstract: SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: August 6, 2019
    Assignee: SCYNEXIS, INC.
    Inventor: Yi Zhang
  • Patent number: 10239846
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: March 26, 2019
    Assignee: CELGENE INTERNATIONAL II SÀRL
    Inventors: Esther Martinborough, Marcus F. Boehm, Adam Richard Yeager, Junko Tamiya, Liming Huang, Enugurthi Brahmachary, Manisha Moorjani, Gregg Alan Timony, Jennifer L. Brooks, Robert Peach, Fiona Lorraine Scott, Michael Allen Hanson
  • Patent number: 10231929
    Abstract: A solid dispersion for achieving improved solubility and absorbability of a pharmaceutically active ingredient, which contains (1) an amorphous pharmaceutically active ingredient, (2) one or more substances selected from among methyl cellulose and organic acids and (3) an enteric base material. In cases where methyl cellulose is contained therein, the solid dispersion does not contain any water-soluble polymer other than methyl cellulose.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: March 19, 2019
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yukihiro Nomura, Yuki Tsushima, Yutaka Ebisawa
  • Patent number: 10226449
    Abstract: Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: March 12, 2019
    Assignee: 3-V Biosciences, Inc.
    Inventors: Timothy Sean Heuer, Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu, Gregory Duke, Yamini Ohol-Gupta, Marie O'Farrell
  • Patent number: 10195197
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
    Type: Grant
    Filed: August 24, 2017
    Date of Patent: February 5, 2019
    Assignee: Calithera Biosciences, Inc.
    Inventors: Mark K. Bennett, Matthew I. Gross, Susan D. Bromley, Keith Orford
  • Patent number: 10174074
    Abstract: SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.
    Type: Grant
    Filed: January 14, 2016
    Date of Patent: January 8, 2019
    Assignee: SCYNEXIS, INC.
    Inventor: Yi Zhang
  • Patent number: 10077254
    Abstract: A tetrazolinone compound represented by formula (1) wherein E represents the following group E16; Y represents —O—CH2—; Q represents the following group Q46; R8 represents a C1-C6 alkyl group; R3, R30 and R31 are the same or different and represent a hydrogen atom; A represents a C6-C16 aryl group optionally having one or more atoms or groups selected from Group P1; R5 represents a C1-C3 alkyl group; and X represents an oxygen atom or a sulfur atom, has excellent control activity against pests.
    Type: Grant
    Filed: October 15, 2014
    Date of Patent: September 18, 2018
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Shuhei Azuma, Teruki Takahashi
  • Patent number: 10065934
    Abstract: Provided herein are novel substituted urea derivatives, and pharmaceutical compositions thereof. Also provided herein are uses of the compounds or pharmaceutical compositions thereof for preventing, managing, treating or lessening a proliferative disease, and modulating the activity of protein kinase.
    Type: Grant
    Filed: July 16, 2015
    Date of Patent: September 4, 2018
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Changchung Cheng, Yingjun Zhang, Bing Liu, Bohua Long, Yu Chen, Zhixin Cheng
  • Patent number: 9975863
    Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphingosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: May 22, 2018
    Assignee: The Scripps Research Institute
    Inventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
  • Patent number: 9944664
    Abstract: The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: April 17, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Michael R. Loso, Gary D. Gustafson, Asako Kubota, Maurice C. Yap, Zachary A. Buchan, Kimberly M. Steward, Michael T. Sullenberger, William J. Hoekstra, Christopher M. Yates
  • Patent number: 9867372
    Abstract: A tetrazolinone compound of formula (1): wherein R1 and R2 each independently represents a hydrogen atom, etc.; R3 represents a C1-C6 alkyl group, etc.; R4, R5, and R6 each independently represents a hydrogen atom, etc.; A represents a C6-C16 aryl group optionally having one or more atoms or groups selected from Group P, etc.; Q represents the following group Q1, etc.; and X represents an oxygen atom or a sulfur atom, has excellent control activity against pests.
    Type: Grant
    Filed: April 23, 2014
    Date of Patent: January 16, 2018
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yuya Yoshimoto, Sadayuki Arimori, Zengye Hou
  • Patent number: 9801879
    Abstract: This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: October 31, 2017
    Assignee: AGENEBIO, INC.
    Inventor: John A. Lowe, III
  • Patent number: 9550756
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: January 24, 2017
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
  • Patent number: 9357779
    Abstract: Ketoheteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols A, L1, G, X, Y, T and R1 have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 7, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Thomas Seitz, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Patent number: 9220266
    Abstract: Ketoheteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols A, L1, G, X, Y, T and R1 have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: December 29, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Thomas Seitz, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Patent number: 9212130
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: December 15, 2015
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Tohru Horiguchi
  • Patent number: 9198422
    Abstract: The present invention relates to novel pyrazoles of formula I wherein the variables are as defined in the description, a method for controlling invertebrate pests, a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, and to an agricultural composition.
    Type: Grant
    Filed: April 16, 2012
    Date of Patent: December 1, 2015
    Assignee: BASF SE
    Inventors: Christian Defieber, Sebastian Soergel, Daniel Saelinger, Ronan Le Vezouet, Karsten Koerber, Steffen Gross, Deborah L. Culbertson, Koshi Gunjima
  • Patent number: 9095596
    Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: August 4, 2015
    Assignee: Southern Research Institute
    Inventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
  • Patent number: 9090599
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: July 28, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffman Jensen
  • Patent number: 9079866
    Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3?, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: July 14, 2015
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Genesis M. Bacani, Wendy Eccles, Anne E. Fitzgerald, Steven D. Goldberg, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Alice Lee-Dutra, Jing Liu, Kelly J. McClure, Steven P. Meduna, Daniel J. Pippel, Mark D. Rosen, Zachary S. Sales
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Patent number: 9029531
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: May 12, 2015
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
  • Patent number: 9029639
    Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein A is a substituted or unsubstituted oxazole or thiazole or imidazole radical; V is C(Rv) or N; W is C(Rw) or N; with the proviso that either V or W is N; Rt, Ru, Rv, Rw are H, halogen, C1-C4-alkyl and the like; X1 is S, O or NR1a, wherein R1a is selected H, C1-C10-alkyl and the like; X2 is OR2a, NR2bR2c, S(O)mR2d, wherein m is 0, 1 or 2, R2a is C1-C4-alkyl, C1-C4-haloalkyl and the like, R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl and the like, or R2b and R2c together with the nitrogen atom to which they are bound form a heterocycle, and R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl and the like; and R1 is H, CN, C1-C10-alkyl and the like.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: May 12, 2015
    Assignee: BASF SE
    Inventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Deborah L. Culbertson, Douglas D. Anspaugh
  • Publication number: 20150119384
    Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.
    Type: Application
    Filed: January 6, 2015
    Publication date: April 30, 2015
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Publication number: 20150105398
    Abstract: A substituted alkenylbenzene compound of formula (4): wherein X1 is selected from the group consisting of a halogen atom, —SF5, C1-C6haloalkyl, hydroxy C1-C6haloalkyl, C1-C6alkoxy C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6 haloalkoxy C1-C3haloalkoxy C1-C3haloalkoxy, C1-C6haloalkylthio, C1-C6haloalkylsulfinyl and C1-C6haloalkylsulfonyl; X3 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy and C1-C6 alkylthio; X4 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, C1-C4alkyl, C1-C4alkoxy and C1-C4haloalkoxy; R3 is —C(R3a)(R3b)R3c, where R3a and R3b independently of each other are a halogen atom, or R3a and R3b together form 3- to 6-membered ring together with the carbon atom bonding them by forming a C2-C5haloalkylene chain, and R3c is selected from the group consisting of a hydrogen atom, halogen atom, C1-C5alkyl, C1-C5haloalkyl, C1-C4haloalkoxy and C1-C4haloalkylthio, with a proviso that in case here X1
    Type: Application
    Filed: December 12, 2014
    Publication date: April 16, 2015
    Inventors: Takeshi MITA, Takamasa KIKUCHI, Takashi MIZUKOSHI, Manabu YAOSAKA, Mitsuaki KOMODA
  • Publication number: 20150099757
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 9, 2015
    Inventors: Takahiko TANIGUCHI, Akira KAWADA, Mitsuyo KONDO, John F. QUINN, Jun KUNITOMO, Masato YOSHIKAWA, Makoto FUSHIMI
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8987273
    Abstract: The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacture and their use for the treatment of benign and malignant neoplasia.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
  • Publication number: 20150080380
    Abstract: This invention relates to novel therapeutic uses for compounds which are inverse agonists of the H3 receptor. In particular this invention relates to therapeutic use of these compounds in the treatment of Multiple Sclerosis.
    Type: Application
    Filed: January 15, 2013
    Publication date: March 19, 2015
    Inventors: Hongtao Lu, Rong Wang
  • Publication number: 20150072959
    Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: November 13, 2014
    Publication date: March 12, 2015
    Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
  • Publication number: 20150065507
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 5, 2015
    Applicant: Glaxo Group Limited
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8962608
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: February 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
  • Publication number: 20150031686
    Abstract: Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 29, 2015
    Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
  • Patent number: 8940774
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: January 27, 2015
    Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
  • Patent number: 8940735
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: January 27, 2015
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
  • Patent number: 8937177
    Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein the substituents are as defined in the description, a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.
    Type: Grant
    Filed: March 22, 2011
    Date of Patent: January 20, 2015
    Assignee: BASF SE
    Inventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson
  • Patent number: 8916566
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: December 23, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
  • Publication number: 20140371231
    Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
  • Patent number: 8912183
    Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: December 16, 2014
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
  • Publication number: 20140364436
    Abstract: The present invention relates to compounds of Formula VIII with absolute configuration R or S: as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula VIII, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Applicant: ASTAR BIOTECH LLC
    Inventors: Chunrong YU, Haihong HUANG, Dongfeng ZHANG, Peng LI
  • Publication number: 20140357614
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xioahu Zhang
  • Patent number: 8901119
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: December 2, 2014
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • 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: 20140350026
    Abstract: The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R? and R? are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.
    Type: Application
    Filed: November 9, 2012
    Publication date: November 27, 2014
    Inventors: Xianjin Luo, Weidong Ye
  • Publication number: 20140343070
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug the
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Publication number: 20140329797
    Abstract: The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: October 16, 2012
    Publication date: November 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Unterschemmann
  • Publication number: 20140329825
    Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.
    Type: Application
    Filed: November 26, 2012
    Publication date: November 6, 2014
    Applicant: NOVARTIS AG
    Inventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
  • Patent number: 8871767
    Abstract: Disclosed are compounds of formula (I): where X, Y, X, A, R1, R2, and R3 are defined herein. Also disclosed are pharmaceutically acceptable salts of the compounds, compositions containing the compounds, and methods of using the compounds to treat, e.g., cancer.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: October 28, 2014
    Assignee: Hengrui (USA) Ltd.
    Inventors: Robert N. Atkinson, Andy J. Ommen, James M. Veal, Kenneth H. Huang, Emilie D. Smith
  • Patent number: 8865718
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Grant
    Filed: October 10, 2013
    Date of Patent: October 21, 2014
    Assignee: Calithera Biosciences Inc.
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Patent number: 8865709
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: October 21, 2014
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina