Unsaturated Ring Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/144)
  • Patent number: 11505549
    Abstract: A novel process for preparation of Deutetrabenazine ((RR, SS)-1,3,4,6,7-11b-Hexahydro-9,10-di(methoxy-d6)-3-(2-methylpropyl)-2H-benzo [a] quinolizin-2-one) of formula I comprises of methylation of N-(2-(3,4-dihydroxy-phenyl)-ethyl)-formamide compound of formula III with deuteriated methanol (CD3OD or CD3OH) to obtain d6-N-(2-(3,4-dimethoxy-phenyl)-ethyl)-formamide compound of formula IV; cyclization of d6-N-(2-(3,4-dimethoxy-phenyl)-ethyl)-formamide in presences of dehydrating agent to obtain d6-6,7-Dimethoxy-3,4-dihydroisoquinoline compound of formula V; reacting d6-6,7-Dimethoxy-3,4-dihydroisoquinoline compound of formula V with 2-acetyl-N,N,N,4-tetramethyl-1-pentanaminium iodide compound of formula VI.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: November 22, 2022
    Inventor: Lakshmi Prasad Alaparthi
  • Patent number: 11064697
    Abstract: The present invention relates to compounds I wherein the variables are defined as given in the description and claims. The invention further relates to uses, processes and intermediates for compounds I.
    Type: Grant
    Filed: July 18, 2016
    Date of Patent: July 20, 2021
    Assignee: BASF SE
    Inventors: Wassilios Grammenos, Christian Winter, Bernd Mueller, Antje Wolf, Ana Escribano Cuesta, Erica Cambeis, Jan Klaas Lohmann, Thomas Grote, Manuel Kretschmer, Nadine Riediger, Ian Robert Craig, Christine Wiebe, Violeta Terterya-Seiser, Andreas Koch, Marcus Fehr
  • Patent number: 10906897
    Abstract: Compounds of the formula (I) wherein Q1, Q2, Y—X, R1, R2, R3, R4, Rb, Rc, Rd, R5, R6, R7, Ra, m and n 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: August 8, 2016
    Date of Patent: February 2, 2021
    Assignee: Syngenta Participations AG
    Inventors: Laura Quaranta, Stephan Trah, Matthias Weiss, Farhan Bou Hamdan
  • Patent number: 10087191
    Abstract: The present invention relates to a piperidine derivative and the preparation method and a pharmaceutical use thereof. In particular, the present invention relates to the piperidine derivative as shown by general formula (I) and the preparation method thereof and a pharmaceutical composition containing the same, and the use thereof as an estrogen receptor modulator in the treatment of estrogen receptor mediated or dependent diseases or conditions, the diseases preferably being breast cancer. In the abstract, the definition of each substituent of the general formula (I) is the same as that in the description.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: October 2, 2018
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Shanghai Yu, Fanglong Yang, Lei Chen, Jingjing Yan, Xiqian Zhang, Zhichao Xie, Lingxiang Chen, Mingxun He
  • Patent number: 9150538
    Abstract: Provided is a simple and efficient method for the large-scale production of a 4,4-difluoro-3,4-dihydroisoquinoline derivative. In the method for producing a 4,4-difluoro-3,4-dihydroisoquinoline derivative represented by general formula (1): a compound represented by general formula (2): is reacted with hydrogen fluoride.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: October 6, 2015
    Assignee: MITSUI CHEMICALS AGRO, INC.
    Inventors: Hideki Umetani, Nobuhiro Kondo, Fumie Kajino
  • Publication number: 20150126517
    Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: January 9, 2015
    Publication date: May 7, 2015
    Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
  • Publication number: 20150126529
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 7, 2015
    Inventors: Upender Velaparthi, Peiying Liu
  • Patent number: 9012443
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Amgen Inc.
    Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
  • Patent number: 8993593
    Abstract: This invention provides a compound of formula A The compound provided herein can affect the opening of, or otherwise modulate, voltage-gated potassium channels. The compound provided herein is useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
    Type: Grant
    Filed: February 1, 2010
    Date of Patent: March 31, 2015
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jean-Michel Vernier, Martha Alicia De La Rosa, Huanming Chen, Jim Zhen Wu, Gary Lee Larson, Ian Wayne Cheney
  • Publication number: 20150072978
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Application
    Filed: November 17, 2014
    Publication date: March 12, 2015
    Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew J. Souers
  • Patent number: 8975411
    Abstract: An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: March 10, 2015
    Assignees: Neugen Pharma Inc., Wakunaga Pharmaceutical Co., Ltd.
    Inventors: Joh-E Ikeda, Noriaki Hirayama, Satoshi Inoue, Kazunori Tanaka, Takuya Kanno
  • Patent number: 8975263
    Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C1-C3 alkyl group, each substituent R2 may be the same or different and may each represent a C1-C3 alkyl group, R3 represents an optionally substituted pyridyl group or the like, R4 and R5, which are the same or different, each represent a C1-C3 alkyl group, R6 and R7, which are the same or different, each represent a C1-C3 alkyl group, and n represents 0 to 3.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: March 10, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shigeo Yamanoi, Katsuji Kagechika, Tsuyoshi Soneda, Yuichi Ochiai, Hidenori Namiki, Fuminao Doi, Madoka Hoshino, Shoko Yoshida
  • Patent number: 8969377
    Abstract: The present disclosure is directed to compounds of the structure (X): wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(?O)—, —NHC(?O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: March 3, 2015
    Assignee: Ardelyx, Inc.
    Inventors: Noah Bell, Christopher Carreras, Dominique Charmot, Jeffrey W Jacobs, Michael Robert Leadbetter, Marc Navre
  • Publication number: 20150057218
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 26, 2015
    Inventors: Min ZHONG, Leping LI
  • Patent number: 8957062
    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: April 5, 2012
    Date of Patent: February 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
  • Publication number: 20150034938
    Abstract: A compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode are disclosed and the compound for an organic optoelectronic device represented by the following Chemical Formula 1 or 2 provides an organic light emitting diode having life-span characteristics due to excellent electrochemical and thermal stability, and high luminous efficiency at a low driving voltage.
    Type: Application
    Filed: September 12, 2014
    Publication date: February 5, 2015
    Inventors: Dong-Min KANG, Hyun-Jung KIM, Chang-Ju SHIN, Jong-Woo WON, Nam-Heon LEE, Soo-Young JEONG, Ho-Kuk JUNG, Mi-Young CHAE
  • Patent number: 8933096
    Abstract: The invention provides a compound of formula (I): or a salt or prodrug thereof, wherein R1, R4-R8, R10, R2?-R6?, W, and A have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as antibacterial agents.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: January 13, 2015
    Assignees: Rugers, The State University of New Jersey, University of Medicine and Dentistry of New Jersey
    Inventors: Edmond J. Lavoie, Ajit Parhi, Daniel S. Pilch
  • Publication number: 20150005287
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: January 1, 2015
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Patent number: 8901345
    Abstract: The problem to be solved is to produce, at high yields with high purity, anhydrous crystals of a compound represented by formula (1) that is an important intermediate for preparation of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof. The solution thereto is an industrial preparation process that provides, with high purity, anhydrous crystals of a compound represented by the following formula (1), which is an intermediate for the production of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof, wherein Boc represents a tert-butoxycarbonyl group.
    Type: Grant
    Filed: January 2, 2013
    Date of Patent: December 2, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Koutarou Kawanami, Hideaki Ishikawa, Masahiro Shoji
  • Patent number: 8889675
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: November 18, 2014
    Assignee: AbbVie Inc.
    Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
  • Publication number: 20140336186
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Application
    Filed: July 9, 2014
    Publication date: November 13, 2014
    Inventors: Thomas BRETSCHNEIDER, Eva-Maria FRANKEN, Ulrich GÖRGENS, Martin FÜSSLEIN, Achim HENSE, Joachim KLUTH, Hans-Georg SCHWARZ, Adeline KÖHLER, Olga MALSAM, Arnd VOERSTE, Angela BECKER
  • Patent number: 8883784
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: November 11, 2014
    Assignee: AbbVie Inc.
    Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
  • Patent number: 8883763
    Abstract: The use of isoquinolones for preparing drugs, including novel isoquinolones as well as their synthesis method. In particular, isoquinolone derivatives used in the treatment of pathological angiogenesis, and more particularly of cancer.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: November 11, 2014
    Assignees: Universite Joseph Fourier, Centre National de la Recherche Scientifique, Institut Curie
    Inventors: Andrei Popov, Aurélie Juhem, Jean-Claude Florent, Chi-Hung N'Guyen
  • Publication number: 20140323518
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.
    Type: Application
    Filed: August 2, 2012
    Publication date: October 30, 2014
    Inventors: Aiping Cheng, Neeraj Garg, Lars Krüger, Joakim Löfstedt, Eva Koch, Konrad Koehler, Lars Hagberg, Daniel Nöteberg
  • Patent number: 8871738
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Publication number: 20140315939
    Abstract: The invention provides a compound of formula I: or a salt or prodrug thereof, wherein Y, W, Z, Z1, Z2, Z3, Z4, and R1-R12 have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.
    Type: Application
    Filed: February 21, 2014
    Publication date: October 23, 2014
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Daniel S. Pilch, Ajit Parhi, Malvika Kaul
  • 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
  • Patent number: 8859200
    Abstract: The present invention provides a reagent for analysis of immature leukocytes comprising: a surfactant which can damage cell membranes of erythrocytes and mature leukocytes, a solubilizing agent which can shrink the damaged blood cells and at least one dye for staining nucleic acid selected from the dyes of the formulae (I) and (II), wherein X? is an anion.
    Type: Grant
    Filed: June 25, 2008
    Date of Patent: October 14, 2014
    Assignee: Sysmex Corporation
    Inventors: Yukiko Kataoka, Tomohiro Tsuji, Shinichiro Oguni, Ayumu Yoshida, Masaki Abe
  • Patent number: 8853242
    Abstract: [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided. [Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: October 7, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Takuya Washio, Wataru Hamaguchi
  • Publication number: 20140296232
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicants: Massachusetts General Hospital, The Broad Institute, Inc.
    Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu
  • Patent number: 8841320
    Abstract: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: September 23, 2014
    Inventors: Darryl J. Bornhop, H. Charles Manning, Mingfeng Bai, Shelby Wyatt Sinha
  • Publication number: 20140249130
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
    Type: Application
    Filed: May 4, 2012
    Publication date: September 4, 2014
    Inventors: Denis Deschenes, Michael D. Altman, John Michael Ellis, Christian Fischer, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Adam J. Schell, Graham F. Smith, Brandon M. Taoka, Corey Bienstock, Maria Emilia Di Francesco, Anthony Donofrio, Scott Peterson, Kerrie B. Spencer, James Patrick Jewell, Amjad Ali, David Jonathan Bennett, Qun Dang, John Wai
  • Publication number: 20140243524
    Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle opti
    Type: Application
    Filed: May 2, 2014
    Publication date: August 28, 2014
    Applicants: Albany Molecular Research, Inc., Bristol-Myers Squibb Company
    Inventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck
  • Publication number: 20140235647
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
  • Publication number: 20140235862
    Abstract: Provided is a simple and efficient method for the large-scale production of a 4,4-difluoro-3,4-dihydroisoquinoline derivative. In the method for producing a 4,4-difluoro-3,4-dihydroisoquinoline derivative represented by general formula (1): a compound represented by general formula (2): is reacted with hydrogen fluoride.
    Type: Application
    Filed: September 28, 2012
    Publication date: August 21, 2014
    Applicant: MITSUI CHEMICALS AGRO, INC.
    Inventors: Hideki Umetani, Nobuhiro Kondo, Fumie Kajino
  • Publication number: 20140228576
    Abstract: Provided are an efficient method for producing 3,4-dihydroisoquinoline derivatives and useful production intermediates thereof. Provided is a method for producing 3,4-dihydroisoquinoline derivatives represented by general formula (1), comprising converting a compound represented by general formula (3) in the presence of acid after reacting with an aniline derivative, or converting a compound represented by general formula (3) by reacting with an aniline derivative in the presence of an acid.
    Type: Application
    Filed: September 28, 2012
    Publication date: August 14, 2014
    Applicant: MITSUI CHEMICALS AGRO, INC.
    Inventors: Hideki Umetani, Nobuhiro Kondo, Fumie Kajino, Munetsugu Morimoto
  • Publication number: 20140212359
    Abstract: AIE (aggregation-induced emission)-active TPE derivatives, TPE-TPP, TPE-MitoR and TPE-IQ are contemplated. These specific TPE derivatives are useful as fluorescent agents for mitochondrial imaging and as apoptosis inducers. Possessing high specificity to mitochondria, superior photostability and appreciable tolerance to microenvironment change, TPE derivatives are well-suited imaging agents for mitochondrial targeting and morphological change tracking. Because of their synthetic flexibility, TPE derivatives can be further modified as dual-functional probes for an array of applications such as sensing of ROS, metal ions, or pH change in mitochondria.
    Type: Application
    Filed: January 27, 2014
    Publication date: July 31, 2014
    Applicant: The Hong Kong University of Science and Technology
    Inventors: Benzhong TANG, Yuning HONG, Sijie CHEN, Wai Tung LEUNG, Engui ZHAO, Haiqin DENG
  • Patent number: 8791263
    Abstract: A compound represented by the general formula (M): (wherein R1 represents a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR3, N(R3)2, C(?O)OR3 or C(?O)N(R3)2, R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, R4 represents a hydrogen atom, an oxygen atom or OR5, and R5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: July 29, 2014
    Assignee: Osaka University
    Inventors: Motomasa Kobayashi, Naoyuki Kotoku, Masayoshi Arai, Satoru Tamura
  • Patent number: 8785473
    Abstract: The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: July 22, 2014
    Assignee: Renascience Co., Ltd.
    Inventors: Toshio Miyata, Kenji Murano, Nagahisa Yamaoka, Akihisa Maeda
  • Publication number: 20140194376
    Abstract: The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).
    Type: Application
    Filed: August 24, 2012
    Publication date: July 10, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140187543
    Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivaties can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
    Type: Application
    Filed: September 25, 2013
    Publication date: July 3, 2014
    Inventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten K. Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste
  • Publication number: 20140179675
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140171439
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 19, 2014
    Applicant: Janssen Pharmaceutica, N.V.
    Inventors: Kristof VAN EMELEN, Marc Gustaaf Celine VERDONCK, Sven Franciscus Anna VAN BRANDT, Patrick Rene ANGIBAUD, Lieven MEERPOEL, Alexey Borisovich DYATKIN
  • Publication number: 20140155381
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 5, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140151670
    Abstract: An exemplary embodiment of the present application provides a new compound and an organic electronic device using the same. The organic electronic device according to an exemplary embodiment of the present application shows excellent characteristics in terms of efficiency, driving voltage, and service life.
    Type: Application
    Filed: July 19, 2013
    Publication date: June 5, 2014
    Applicant: LG CHEM, LTD.
    Inventors: Dong Hoon Lee, Minyoung Kang, Jungi Jang, Boonjae Jang, Minseung Chun, Kidong Koo
  • Publication number: 20140142082
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 22, 2014
    Applicant: PHENEX PHARMACEUTICALS AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20140128427
    Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 8, 2014
    Applicant: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
  • Patent number: 8716312
    Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: May 6, 2014
    Assignee: Merck Sharp & Dohme Corporation
    Inventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Patent number: 8680293
    Abstract: This invention relates to novel agents that are analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
    Type: Grant
    Filed: August 1, 2007
    Date of Patent: March 25, 2014
    Assignee: Syntarga B.V.
    Inventors: Patrick Henry Beusker, Henri Johannes Spijker, Johannes Albertus Frederikus Joosten, Tijl Huijbregts, Franciscus Marinus Hendrikus de Groot