Carbocyclic Ring Containing Patents (Class 546/194)
  • Patent number: 11939295
    Abstract: A 6-(3-hydroxyphenyl)-2-methoxy-4-(3-methylphenyl)nicotinonitrile as an antimicrobial compound, its synthesis, and its use as an antimicrobial agent.
    Type: Grant
    Filed: November 14, 2023
    Date of Patent: March 26, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed
  • Patent number: 11834462
    Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
    Type: Grant
    Filed: April 6, 2022
    Date of Patent: December 5, 2023
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Sun Hee Kim, Yunfei Zhu
  • Patent number: 11827618
    Abstract: The embodiments of present invention provide processes and an intermediate for the large-scale preparation of 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl]benzamide hemisuccinate, and formulations and product forms, such as tablets, made by these processes. Additionally, embodiments of the present invention provide tablets including 25 mg, 50 mg, 100 mg, or 200 mg free base equivalent of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide hemisuccinate.
    Type: Grant
    Filed: April 14, 2023
    Date of Patent: November 28, 2023
    Inventors: Aktham Aburub, David Andrew Coates, Scott Alan Frank, Mark Steven Kerr, Roger Ryan Rothhaar, Radhe Krishan Vaid
  • Patent number: 11440885
    Abstract: The present invention provides using a substituted 1-arylalkyl-4-acylaminopiperidine compound of Formula I: to treat various clinical conditions including, but not limited to, hemorrhagic shock, nicotine withdrawal symptoms, gastrointestinal side effects of opioids, cancer therapy, epithelial wounds, herpes zoster infection, or opioid-induced pruritus. In compound of Formula I, R1 is C1-10 alkyl, C1-10 haloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; R2 is C1-6 alkylene; Y is optionally substituted aryl, optionally substituted heteroaryl, or a moiety of the formula —C(?O)—X1, wherein X1 is —OR3 or —NR4R5, where each of R3, R4 and R5 is H or C1-10 alkyl.
    Type: Grant
    Filed: March 25, 2020
    Date of Patent: September 13, 2022
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERISTY OF ARIZONA
    Inventors: Ruben S. Vardanyan, Victor J. Hruby
  • Patent number: 11414428
    Abstract: Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR1, N or N-oxide; X is CR2, N or N-oxide; Y is CR3, N or N-oxide; Z is CR4, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and R9 and R10 are as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer.
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: August 16, 2022
    Assignee: Auckland UniServices Limited
    Inventors: Brian Desmond Palmer, Lai-Ming Ching
  • Patent number: 11186590
    Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
    Type: Grant
    Filed: May 19, 2020
    Date of Patent: November 30, 2021
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Sun Hee Kim, Yunfei Zhu
  • Patent number: 11178872
    Abstract: A compound represented by a formula (I), or a salt thereof: wherein Ar1 is a substituted or unsubstituted C6-10 aryl group, or the like; the number of X1 groups that can be substituted on Ar1 is 5 or less; X1 is a halogeno group, a substituted or unsubstituted C1-6 alkyl group, or the like; Z is a single bond, a sulfur atom, or an oxygen atom; A is a nitrogen atom or a carbon atom; X2 is a halogeno group, a substituted or unsubstituted C1-6 alkyl group, or the like; m is an integer of 0 to 2 when A is a nitrogen atom and is an integer of 0 to 3 when A is a carbon atom; R1 to R4 and R6 to R9 each independently represent a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, or the like; R5 is a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, or the like; k represents the number of CR6R7 moieties in a parenthesis and is 0 or 1; h represents the number of CR3R4 moieties in a parenthesis and is 0 or 1; and Ar is a substituted or unsubstituted C6-10 aryl group, or the like.
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: November 23, 2021
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Jun Iwata, Fumiya Nishio, Takao Iwasa, Satoshi Makino, Koichi Hirata
  • Patent number: 11174228
    Abstract: Disclosed are small molecule antagonists of ?4?7 integrin, and methods of using them to treat a number of specific diseases or conditions.
    Type: Grant
    Filed: July 27, 2020
    Date of Patent: November 16, 2021
    Assignee: Morphic Therapeutic, Inc.
    Inventors: Matthew G. Bursavich, Dawn M. Troast, Bryce A. Harrison, Blaise S. Lippa, Bruce N. Rogers, Kyle D. Konze, Aleksey I. Gerasyuto, Tyler Day, Fu-Yang Lin, Kristopher N. Hahn, Mats A. Svensson, Byungchan Kim, Cheng Zhong, Alexey A. Lugovskoy, Brian Sosa
  • Patent number: 11168079
    Abstract: The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of famesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: November 9, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joseph E. Carpenter, Matthias Broekema, Jianxin Feng, Chunjian Liu, Wei Wang, Ying Wang
  • Patent number: 11053214
    Abstract: The present invention provides new pseudo-polymorphs of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide which are useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine headache.
    Type: Grant
    Filed: December 5, 2017
    Date of Patent: July 6, 2021
    Assignee: CoLucid Pharmaceuticals, Inc.
    Inventors: Brigida Allieri, Paul Fagan, Emma Sharp, Raymond D. Skwierczynski
  • Patent number: 11014905
    Abstract: The present invention relates to a pyridine derivative of formula (1) wherein R1 is optionally-substituted C1-6 alkyl, optionally-substituted C3-10 cycloalkyl, or optionally-substituted 5- to 10-membered saturated or partially-unsaturated heterocyclyl; R2 is halogen atom, cyano, C1-6 alkyl which may be optionally substituted with 1 to 3 the same or different halogen atoms, C1-6 alkoxy which may be optionally substituted with 1 to 3 the same or different halogen atoms, or amino which may be optionally substituted with 1 to 2 the same or different C1-6 alkyl; and the bind with broken line is single or double bond, or a pharmaceutically acceptable salt thereof, which is useful as a medicament for treating symptoms in anxiety-related disorder.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: May 25, 2021
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Hidefumi Yoshinaga, Hiro Uemachi, Tomomi Ohno, Jeremy Besnard
  • Patent number: 10934272
    Abstract: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: March 2, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 2) LIMITED
    Inventors: Stephen John Atkinson, Emmanuel Hubert Demont, Lee Andrew Harrison, Etienne Levernier, Alexander G. Preston, Jonathan Thomas Seal, Ian David Wall, Robert J. Watson, James Michael Woolven
  • Patent number: 10919852
    Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R1a, R1b, R1c, R1d, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: February 16, 2021
    Assignee: ChemoCentryx, Inc.
    Inventors: Christopher Lange, Viengkham Malathong, Venkat Reddy Mali, Jeffrey McMahon, Darren J. McMurtrie, Sreenivas Punna, Howard S. Roth, Rajinder Singh, Yu Wang, Ju Yang, Penglie Zhang
  • Patent number: 10793543
    Abstract: The present invention provides a compound represented by formula (I), or a pharmaceutically acceptable salt, a solvate, an ester, an acid, a metabolite or a prodrug thereof. The compound itself in the present invention or in combination with at least one therapeutic agent can be used for preventing or treating diseases, disorders or symptoms caused by the adjustment of the activity of tyrosine kinase C-KIT, or affected by the activity of the tyrosine kinase C-KIT or involving in the activity of the tyrosine kinase C-KIT, especially cancers or other cell proliferation diseases.
    Type: Grant
    Filed: March 28, 2017
    Date of Patent: October 6, 2020
    Assignees: PRECEDO PHARMACEUTICALS CO., LTD, HEFEI GRACEVO BIO-MEDICINE CO., LTD
    Inventors: Qingsong Liu, Jing Liu, Qiang Wang, Beilei Wang, Feiyang Liu, Shuang Qi, Ziping Qi, Fengming Zou, Cheng Chen, Wenchao Wang, Chen Hu, Xiaochuan Liu, Wei Wang, Aoli Wang, Li Wang, Zhenquan Hu, Tao Ren
  • Patent number: 10696689
    Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
    Type: Grant
    Filed: September 17, 2019
    Date of Patent: June 30, 2020
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Sun Hee Kim, Yunfei Zhu
  • Patent number: 10550102
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; 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: December 11, 2018
    Date of Patent: February 4, 2020
    Assignee: NOVARTIS AG
    Inventors: Christopher M. Adams, Doug Bevan, Michael Paul Capparelli, Takeru Ehara, Luciana Ferrara, Nan Ji, Erik Meredith, Muneto Mogi, James J. Powers, Ganesh Prasanna, Nello Mainolfi, Mitsunori Kato
  • Patent number: 10208018
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; 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: July 2, 2015
    Date of Patent: February 19, 2019
    Assignee: NOVARTIS AG
    Inventors: Christopher M. Adams, Doug Bevan, Michael Paul Capparelli, Takeru Ehara, Luciana Ferrara, Nan Ji, Mitsunori Kato, Nello Mainolfi, Erik Meredith, Muneto Mogi, James J. Powers, Ganesh Prasanna
  • Patent number: 10092556
    Abstract: A novel compound which has an excellent aurora A-selective inhibitory action and is useful as an orally administrable anticancer agent is provided. Also, a novel agent for potentiation of anti-tumor effect of microtubule agonists, which include a taxane anticancer agent, and a combination therapy are provided.
    Type: Grant
    Filed: April 18, 2016
    Date of Patent: October 9, 2018
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Tetsuya Sugimoto, Hidekazu Takahashi, Morihiro Mitsuya, Norio Masuko, Hiroshi Sootome
  • Patent number: 9771357
    Abstract: The present invention provides a compound having ALXR agonist activity. Specifically, the invention provides a compound having ALXR agonist activity represented by general formula (I) wherein all the symbols are as defined in the specification, a salt thereof, a solvate thereof, or a prodrug thereof as well as an agent containing the same as an active ingredient for preventing and/or treating an ALXR-associated disease, such as an inflammatory bowel disease, an autoimmune disease, a chronic inflammatory disease, asthma, pulmonary fibrosis, atopic dermatitis, ischemia-reperfusion injury, myocardial infarction, or Alzheimer's disease.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: September 26, 2017
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Masahiko Terakado, Masaya Hirobe, Maki Iwahashi, Kousuke Tani, Tetsuya Sugiyama
  • Patent number: 9758511
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: September 12, 2017
    Assignee: AbbVie Inc.
    Inventors: Michael L. Curtin, Kenton Longenecker, Todd M. Hansen, Richard F. Clark, Bryan Sorensen, Howard R. Heyman, Zhiqin Ji
  • Patent number: 9637474
    Abstract: The present invention provides an aminopyridine compound, or a pharmaceutically acceptable salt thereof, that inhibits Aurora A and, therefore may be useful in treating cancer.
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: May 2, 2017
    Assignee: Eli Lilly and Company
    Inventor: James Robert Henry
  • Patent number: 9453037
    Abstract: The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: September 27, 2016
    Assignee: KEMPHARM, INC
    Inventors: Sven Guenther, Guochen Chi, Bindu Bera, Travis Mickle, Sanjib Bera
  • Patent number: 9346787
    Abstract: A novel compound which has an excellent aurora A-selective inhibitory action and is useful as an orally administrable anticancer agent is provided. Also, a novel agent for potentiation of anti-tumor effect of microtubule agonists, which include a taxane anticancer agent, and a combination therapy are provided.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: May 24, 2016
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Tetsuya Sugimoto, Hidekazu Takahashi, Morihiro Mitsuya, Norio Masuko, Hiroshi Sootome
  • Patent number: 9198902
    Abstract: The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R1, R2, R3, R4, R5, R6, R7, R8, m, n1, n2, p and q are the same as those defined in the description.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: December 1, 2015
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Hui Zhang, Mingwei Fan, Liang Sun
  • Patent number: 9114138
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: August 25, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Terry Patrick Finn
  • Patent number: 9079928
    Abstract: The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: July 14, 2015
    Assignee: KemPharm, Inc.
    Inventors: Sven Guenther, Guochen Chi, Bindu Bera, Travis Mickle, Sanjib Bera
  • Publication number: 20150141399
    Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: February 5, 2015
    Publication date: May 21, 2015
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Publication number: 20150141397
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: May 21, 2015
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20150141425
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Application
    Filed: November 3, 2014
    Publication date: May 21, 2015
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Patent number: 9034874
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: May 19, 2015
    Assignee: NOVARTIS AG
    Inventors: Yves Auberson, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang
  • Publication number: 20150133473
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 20, 2013
    Publication date: May 14, 2015
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Joseph E. Drumm III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Publication number: 20150133497
    Abstract: Disclosed are a glycine reuptake inhibitor and the use thereof. The glycine reuptake inhibitor is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is one or more groups selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy; R2 is selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, and C1-6 haloalkoxy; and each of R3 and R4 is independently selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy.
    Type: Application
    Filed: November 21, 2012
    Publication date: May 14, 2015
    Applicant: Beijing Medisan Technology Co., Ltd.
    Inventors: Jinai Liu, Mingxin Wang, Fan Yang, Ailing Wang, Yan Zhu, Jin Cui, Lei Ji
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150126522
    Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
    Type: Application
    Filed: May 15, 2013
    Publication date: May 7, 2015
    Applicant: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Celine Duquenne, Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
  • Publication number: 20150126486
    Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Atsushi NAGANAWA, Kensuke KUSUMI, Kazuhiro OTSUKI, Tetsuya SEKIGUCHI, Akito KAKUUCHI, Koji SHINOZAKI, Hiroshi YAMAMOTO, Shigeyuki NONAKA
  • Publication number: 20150126364
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z1, Z2, J1, J2, M, R1a, R1b, R2a, R2b, R2c, R2d, R14 and R14a are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Applicant: E I Du Pont de Nemours and Company
    Inventors: Thomas Francis Pahutski, JR., Matthew James Campbell, Dominic Ming-Tak Chan, Jeffrey Keith Long, Thomas Martin Stevenson
  • Publication number: 20150126516
    Abstract: A piperidine compound represented by the following Formula (1): wherein ring A, ring B, and ring C are the same or different and each represent a benzene ring or a nitrogen-containing heteroaromatic ring; W represents a C1-C4 alkylene or alkenylene group; X, Y, and Z are the same or different and each represent a halogen atom, a C1-C6 alkyl group, a halo C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo C1-C6 alkoxy group; m, n, and p are the same or different and each represent an integer of 0 to 5; when m is greater than or equal to 2, the Xs are the same or different; when n is greater than or equal to 2, the Ys are the same or different; and when p is greater than or equal to 2, the Zs are the same or different has an excellent controlling efficacy against pests.
    Type: Application
    Filed: April 12, 2013
    Publication date: May 7, 2015
    Inventor: Sadayuki Arimori
  • Publication number: 20150126490
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
  • Publication number: 20150119412
    Abstract: A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent the prophylaxis or treatment of diabetes mellitus are provided.
    Type: Application
    Filed: October 28, 2014
    Publication date: April 30, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo Kasai, Takashi Nakahata, Asato Kina, Hideki Hirose, Takeshi Yamasaki, Tohru Yamashita, Yoichi Nishikawa
  • 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
  • Patent number: 9018200
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Patent number: 9018224
    Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
  • Publication number: 20150105386
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: October 24, 2014
    Publication date: April 16, 2015
    Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Muller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steven L. Swann, Jr., Dominique Bonafoux, Ryan Keddy, Adrian Donald Hobson, Anil Vasudevan
  • Publication number: 20150105354
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20150105391
    Abstract: Certain embodiments of the present invention provide selected compounds having a molecular structure according to Formula 1: In Formula 1, Z is —CO—, —SO—, or —SO2—; Ar is phenyl, heteroaryl, or heterocycloalkyl; Het is heteroaryl; R is R?, X, or NR1R2; R? is R3, or OR3; R? is R4, or OR4; R1 and R2 are each independently H, alkyl, or acyl; R3 is H, heteroaryl, or alkyl; R4 is H, heteroaryl, or CnH2n+1 (n>2); and X is F, Br, I, CN, or NO2. In some embodiments, compounds having a molecular structure according to Formula 1 have the property of inhibiting a growth of a cell line selected from HeLa and MB468 with a sub-micromolar IC50.
    Type: Application
    Filed: July 19, 2014
    Publication date: April 16, 2015
    Inventors: Wen-Hwa Lee, Jiewen Zhu, Chun-Mei Hu
  • Publication number: 20150105371
    Abstract: This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Markus FRANK, Hans HAEBERLE, Manuel HENRY, Thorsten PACHUR, Marco SANTAGOSTINO, Uwe STERTZ, Thomas TREBING, Ulrike WERTHMANN
  • Patent number: 9006242
    Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: April 14, 2015
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki
  • Publication number: 20150099783
    Abstract: The present invention relates to CCR3 inhibitors of formula 1, wherein R1 is H, C1-6-alkyl, C0-4-alkyl-C3-6-cycloalkyl, C1-6-haloalkyl; R2 is H, C1-6-alkyl; X is an anion selected from the group consisting of chloride or ½ dibenzoyltartrate j is 1 or 2. for use as a medicament for the treatment of diseases selected from dry age-related macular degeneration (dAMD), wet age-related macular degeneration (wAMD), retinopathy of prematurity (ROP), central retinal vein occlusion (CRVO), nasal polyposis, eosinophilic esophagitis, eosinophillic gastroenteritis (e.g. eosinophilic gastritis and eosinophilic ententeritis), hypereosinophilic syndrome and Churg Strauss syndrome.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Michael Chadham NIVENS, Thierry BOUYSSOU, Peter SEITHER, Rolf GOEGGEL
  • Publication number: 20150099736
    Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substitu
    Type: Application
    Filed: November 10, 2014
    Publication date: April 9, 2015
    Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
  • Publication number: 20150099746
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 9, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone