Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 546/159)
  • Patent number: 11078185
    Abstract: The invention relates to Mycobacterium tuberculosis-thioredoxin reductase inhibitors, processes for the preparation thereof, drugs containing said compounds, and the use of said compounds for manufacturing drugs.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: August 3, 2021
    Assignee: TECHNISCHE UNIVERSITAT DORTMUND
    Inventors: Oliver Koch, Luis Bering
  • Patent number: 10952436
    Abstract: Compounds of formula (I), wherein the substitutents are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
    Type: Grant
    Filed: March 13, 2018
    Date of Patent: March 23, 2021
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Laura Quaranta, Farhan Bou Hamdan, Matthias Weiss
  • Patent number: 10836748
    Abstract: The invention relates to a compound according to general formula (I), which acts as a bradykinin (BK) B2 receptor antagonist; to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament.
    Type: Grant
    Filed: April 28, 2020
    Date of Patent: November 17, 2020
    Assignee: Pharvaris Netherlands B.V.
    Inventors: Christoph Gibson, Joern Saupe, Horst-Dieter Ambrosi, Lars Ole Haustedt
  • Patent number: 10307412
    Abstract: The present application provides a quinoline derivative against non-small cell lung cancer. 1-[[[4-(4-fluoro-2-methyl)-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine or a pharmaceutically acceptable salt thereof provided by the present application can be used for the treatment of non-small cell lung cancer, and relative to placebo, can significantly improve non-small cell lung cancer patients without progression of survival. 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine or a pharmaceutically acceptable salt thereof provided by the present application can be used for the treatment of lung adenocarcinoma, and relative to placebo, can significantly improve lung adenocarcinoma patients without progression of survival.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: June 4, 2019
    Inventors: Xunqiang Wang, Yadong Miu, Min Zhou, Shanchun Wang, Ling Yang, Wei Shi
  • Patent number: 10300059
    Abstract: The present invention relates to a pharmaceutical composition and a therapeutic combination comprising a novel cholesteryl ester transfer protein (CETP) inhibitor and a HMG CoA Reductase inhibitor, which may be used in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: May 28, 2019
    Assignee: DEZIMA PHARMA B.V.
    Inventors: John Ford, Patrick Round, John Kastelein
  • Patent number: 10206915
    Abstract: Disclosed herein are pharmaceutically acceptable complex formulations comprising complexes of Ivacaftor, or a salt or derivative thereof, together with complexation agents and pharmaceutically acceptable excipients; processes for the preparation thereof; and pharmaceutical compositions containing them. The complexes possess instantaneous redispersibility, increased apparent solubility and permeability compared to KALYDECO, no observable food effect which deliver the opportunity of precise dosing and ease of administration of the reconstituted complex Ivacaftor in solution form.
    Type: Grant
    Filed: April 25, 2017
    Date of Patent: February 19, 2019
    Assignee: Druggability Technologies IP Holdco Limited
    Inventors: Richárd Balázs Kárpáti, Gergo Patyi, Orsolya Basa-Dénes, Erzsébet Réka Angi, Tamás Jordán, Tamás Solymosi, Hristos Glavinas, Genovéva Filipcsei
  • Patent number: 10039753
    Abstract: The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R1, R1a, R1b, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: August 7, 2018
    Assignee: Pfizer Inc.
    Inventors: Karen Jean Coffman, Paul Galatsis, Michelle Renee Garnsey, Jaclyn Louise Henderson, Bethany Lyn Kormos, Ravi G. Kurumbail, Martin Youngjin Pettersson, Matthew Richard Reese, Antonia Friederike Stepan, Patrick Robert Verhoest, Travis T. Wager
  • Patent number: 9980954
    Abstract: The present disclosure relates to a quinoline derivative which inhibits the activity of histone methyltransferases (ESET/SETDB1) specific for the histone molecule H3K9 or a pharmaceutically acceptable salt thereof and a use thereof.
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: May 29, 2018
    Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Hyunah Choo, Sun-Joon Min, Yun Kyung Kim, Hoon Ryu, Hyemyung Seo, Juhyeon Kim, Jihoon Jang, Sungsu Lim, Younghee Kim, Yu Jin Hwang, Yong Seo Cho
  • Patent number: 9783498
    Abstract: The present invention relates a new process to synthesize 6-(7-((1-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide (AL3810) by deprotection of substituted benzyl 1-((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)-methyl)cyc-lopropylcarbamate (Formula I) under a diluted or weak acidic condition. A stable crystalline form of 6-(7-((1-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide has also been prepared.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: October 10, 2017
    Assignee: Advenchen Pharmaceuticals, LLC
    Inventor: Guoqing Paul Chen
  • Patent number: 9527817
    Abstract: Compounds and methods for treating or preventing a neurodegenerative disease, disorder or condition associated with the overall activity of hsp90 but not with the ATPase activity of hsp90, including peripheral neuropathy, such as peripheral neuropathy caused by chemotherapy or diabetes, disorders 5 of the central nervous system, such as Alzheimer's disease and Parkinsons disease, and motor neuron diseases, such as amyotrophic lateral sclerosis (ALS), in a subject are provided.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: December 27, 2016
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Ahmet Hoke, Weiran Chen, Jing Zhu
  • Patent number: 9522889
    Abstract: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: December 20, 2016
    Assignee: BIOGEN MA INC.
    Inventors: Kevin Guckian, Gnanasambandam Kumaravel, Bin Ma, Sha Mi, Hairuo Peng, Zhaohui Shao, Lihong Sun, Arthur Taveras, Deping Wang, Zhili Xin, Lei Zhang
  • Patent number: 9512104
    Abstract: The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: December 6, 2016
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 9485987
    Abstract: The present invention provides an aqueous suspended agricultural chemical composition comprising an agricultural chemical active ingredient, an alkyl naphthalene sulfonate formalin condensate and one or two or more compounds selected from the group consisting of an alkyl sulfate, a polyoxyalkylene alkyl ether sulfate, an alkyl phosphoric acid and a salt thereof, a polyoxyalkylene alkyl ether phosphoric acid and a salt thereof, and a polyoxyalkylene alkyl ether acetic acid and a salt thereof. The aqueous suspended agricultural chemical composition suppresses the crystal growth of the agricultural chemical active ingredient, and has an excellent effect on pest control and an excellent storage stability.
    Type: Grant
    Filed: January 29, 2014
    Date of Patent: November 8, 2016
    Assignees: MEIJI SEIKA PHARMA CO., LTD., NIPPON KAYAKU CO., LTD.
    Inventors: Atsushi Sato, Mitsuyuki Yabuzaki, Shigeru Ueno, Yoshinori Muramatsu, Kazuteru Ogawa, Hidetoshi Shirakura
  • Patent number: 9486418
    Abstract: Method for the treatment or prophylaxis of dry eye disorders by the administration of alkylamino-polyhydroxyalkanes and compositions thereof.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: November 8, 2016
    Assignee: Dynamis Pharmaceuticals, Inc.
    Inventors: Alice Marcy, Annette M. Tobia
  • Patent number: 9359375
    Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
    Type: Grant
    Filed: August 12, 2014
    Date of Patent: June 7, 2016
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Patent number: 9340508
    Abstract: A process for the preparation in high yields and purity of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.
    Type: Grant
    Filed: March 18, 2015
    Date of Patent: May 17, 2016
    Assignee: CLOVIS ONCOLOGY ITALY S.R.L.
    Inventors: Silvano Spinelli, Valeria Livi
  • Patent number: 9321730
    Abstract: The present invention relates methods of preparing quinoline derivative compounds, and administering such compounds in the treatment of solid and non-solid tumors, notably on liver cancer.
    Type: Grant
    Filed: August 21, 2007
    Date of Patent: April 26, 2016
    Assignee: The Hong Kong Polytechnic University
    Inventors: Albert Sun-chi Chan, Johnny Cheuk-on Tang, Kim-hung Lam, Chung-hin Chui, Stanton Hon-lung Kok, Sau Hing Chan, Filly Cheung, Roberto Gambari, Chor Hing Cheng
  • Patent number: 9302992
    Abstract: Novel quinoline derivatives are disclosed. Also disclosed are synthesis and use thereof for treating neurodegenerative diseases.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: April 5, 2016
    Assignee: ANNJI PHARMACEUTICAL CO., LTD.
    Inventors: Ji-Wang Chern, Chen-Wei Huang, Pei-Teh Chang, Rahul Subhash Talekar
  • Patent number: 9216173
    Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: December 22, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
  • Patent number: 9139530
    Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
    Type: Grant
    Filed: May 8, 2014
    Date of Patent: September 22, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
  • Patent number: 9126934
    Abstract: An objective of the present invention is to provide a process for producing 4-carbonyl oxyquinoline derivatives useful as agricultural and horticultural pesticides and fungicides. The objective can be attained by a process for producing 4-carbonyl oxyquinoline derivatives represented by general formula (1), the process including reacting a quinolone derivative with a halogenated compound or an acid anhydride in the presence of a phase transfer catalyst and a base.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: September 8, 2015
    Assignees: NIPPON KAYAKU CO., LTD., MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Shizuo Shimano, Akinori Morikawa, Kenichi Yamamoto, Hiroki Hotta, Kazumi Yamamoto, Nozomu Nakanishi, Nobuto Minowa
  • Patent number: 9120749
    Abstract: The present invention directs a compound represented by formula (I).
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: September 1, 2015
    Assignee: ONCOTHERAPY SCIENCE, INC.
    Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Raymond Huntley, Joel R. Walker, Helene Decornez
  • Patent number: 9090592
    Abstract: The present invention relates to novel heterocyclic compounds of formula I wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3?, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3? activity using the compounds.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: July 28, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Sean Colm Turner, Helmut Mack, Margaretha Henrica Maria Bakker, Marcel Van Gaalen, Carolin Hoft, Wilfried Hornberger
  • Patent number: 9090587
    Abstract: Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-y1}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided. In these crystals, decomposition due to influences of light is suppressed as compared to that in crystals of the compound (1) in free, and their storage stability is high. These crystals have higher solubility in water than the crystals of the compound (1) in free.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: July 28, 2015
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Ichiro Araya, Akinori Goto, Wataru Minagawa, Keiko Funada, Muneki Nagao
  • Patent number: 9051305
    Abstract: The present invention relates to a compositions for and methods of cancer treatment in which compounds of Formula I or Formula II. In some aspects, the treatment of B-cell Lymphoma or other hematopoietic cancers is encompassed. In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds of Formula I or Formula II. Combination therapy with, for example, a class of therapeutics known as 26S proteasome inhibitors, for example, Bortezomib, are also included. In another aspect the present invention relates to autoimmune treatment with compounds of Formula I or Formula II. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: June 9, 2015
    Assignee: Eutropics Pharmaceuticals, Inc.
    Inventors: Michael H. Cardone, Andrew F. Kolodziej, David Richard
  • Patent number: 9045425
    Abstract: The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: June 2, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Brian Luisi, Sneha Ghanshyam Arekar, Adriana Costache, Kirk Raymond Dinehart, Steven C. Johnston, Bobbianna J. Neubert-Langille
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Patent number: 9040560
    Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: May 26, 2015
    Assignee: Merck Patent GmbH
    Inventors: Amanda E. Sutton, Thomas E. Richardson, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Yufang Xiao, Andreas Goutopoulos, Ruoxi Lan, David Perrey, Harold George Vandeveer, Lesley Liu-Bujalski, Frank Stieber, Brian L. Hodous, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
  • Publication number: 20150141527
    Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
    Type: Application
    Filed: July 22, 2014
    Publication date: May 21, 2015
    Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy James DAVIS, Vincent DARMOHUSODO, Melissa WONG, Victor SELCHAU
  • Patent number: 9029395
    Abstract: Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: May 12, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Robert J. Watson
  • Patent number: 9029396
    Abstract: The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: May 12, 2015
    Assignee: Novartis AG
    Inventors: Nigel Graham Cooke, Rita Ramos, Karen Kammertoens, Maurice Van Eis
  • Patent number: 9018229
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: April 28, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
  • Patent number: 9012645
    Abstract: A process for the preparation in high yields and purity of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: April 21, 2015
    Assignee: Clovis Oncology Italy S.R.L.
    Inventors: Silvano Spinelli, Valeria Livi
  • Publication number: 20150105366
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
  • Publication number: 20150105404
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Publication number: 20150105372
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE, MAXWELL D. CUMMINGS
  • Patent number: 9006444
    Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: April 14, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Maria Emilia Di Francesco, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
  • Publication number: 20150099882
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Applicant: Pfizer Inc.
    Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
  • Patent number: 8993767
    Abstract: The present invention relates to multiphoton activable organic compounds responding to the following formula (I). The present invention also relates to a method of synthesizing the compounds of the invention, to an aqueous solution comprising at least one compound of the invention, and to their specific uses. The present invention also concerns a method of liberating organic ligands, said method involving the step of irradiating a compound according to the invention.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: March 31, 2015
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Peter Dalko, Morgane Petit, David Ogden, Francine Acher
  • Patent number: 8987456
    Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: March 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Publication number: 20150073017
    Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: Xi CHEN, Junfa FAN, Pingchen FAN, Antoni KRASINSKI, Lianfa LI, Rebecca M. LUI, Jeffrey P. McMAHON, Jay P. POWERS, Yibin ZENG, Penglie ZHANG
  • Patent number: 8975278
    Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Grant
    Filed: September 19, 2007
    Date of Patent: March 10, 2015
    Assignee: Prana Biotechnology Limited
    Inventors: Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Gaik Beng Kok, Guy Krippner
  • Patent number: 8975408
    Abstract: Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.
    Type: Grant
    Filed: January 20, 2014
    Date of Patent: March 10, 2015
    Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.
    Inventors: Gianni Gottardo, Pierluigi Padovan, Sergio Osti
  • Patent number: 8969577
    Abstract: The present invention relates to curable compositions comprising a thermolatent amidine base and an organic material which is polymerizable or crosslinkable with a basic or nucleophilic catalyst. In particular, the invention relates to curable coating compositions, especially powder coating compositions, and curable adhesive compositions, as well as to the use a thermolatent amidine base as a curing catalyst for thermally induced base-catalyzed polymerization or crosslinking reactions.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: March 3, 2015
    Assignee: BASF SE
    Inventors: Peter Nesvadba, Lucienne Bugnon Folger, Ralf Knischka
  • Patent number: 8969381
    Abstract: The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing CXCR4 related conditions, typically prevention or treatment of viral infections such as HIV or for managing cancer.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: March 3, 2015
    Assignee: Emory University
    Inventors: Lawrence J. Wilson, John Wiseman, Dennis C. Liotta, Michael G. Natchus
  • Publication number: 20150057288
    Abstract: A pest control method for honeybee parasitic pests has been found, which is highly safe to honeybees and demonstrates excellent pest control effects against honeybee parasitic pests by using a honeybee parasitic pest control agent containing at least one of a compound represented by Formula (I) and acid addition salts thereof.
    Type: Application
    Filed: November 10, 2014
    Publication date: February 26, 2015
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Ryo HORIKOSHI, Masaaki MITOMI
  • Patent number: 8957091
    Abstract: The present invention relates to the use of quinolinone derivatives of general formula (I), ligands of the Smo receptor or of related receptors which target a binding site of the receptor which is different from the known ligand binding sites, as research tools for identifying modulators of the Smo receptor or of related receptors, characterizing the Hedgehog signalling pathway and diagnosis; the invention also relates to kits containing said derivatives of general formula (I).
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: February 17, 2015
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Martial Ruat, Helene Faure, Tatiana Gorojankina
  • Patent number: RE46617
    Abstract: The present invention relates to the field of synthesizing anti-infective compounds. More particularly, the invention relates to synthesizing a family of quinolone compounds useful as anti-infective agents. The invention includes a process for preparing a quinolone compound wherein less than about 0.40% of dimeric impurity of the quinolone is produced.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: November 28, 2017
    Assignee: MELINTA THERAPEUTICS, INC.
    Inventors: Roger Hanselmann, Maxwell M. Reeve, Graham Johnson