Ring Sulfur In The Bicyclo Ring System Patents (Class 546/114)
  • Patent number: 12077537
    Abstract: The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of a Retroviridae viral infection, including an infection caused by the HIV virus.
    Type: Grant
    Filed: February 15, 2023
    Date of Patent: September 3, 2024
    Assignee: Gilead Sciences, Inc.
    Inventors: Chienhung Chou, Scott E. Lazerwith, John O. Link, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 11958866
    Abstract: A synthetic protocol to use a thiourea or urea compound and auric chloride as starting materials to obtain thiazole and benzothiazole derivatives. The synthesis can be conducted at room temperature and the final compound can result from cyclization of the thiourea or urea compound in the presence of an Au salt from the auric chloride.
    Type: Grant
    Filed: October 17, 2023
    Date of Patent: April 16, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Awal Noor, Ezzat Khan, Umar Ali Khan
  • Patent number: 11814399
    Abstract: A synthetic protocol to use a thiourea or urea compound and auric chloride as starting materials to obtain thiazole and benzothiazole derivatives. The synthesis can be conducted at room temperature and the final compound can result from cyclization of the thiourea or urea compound in the presence of an Au salt from the auric chloride.
    Type: Grant
    Filed: April 7, 2023
    Date of Patent: November 14, 2023
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Awal Noor, Ezzat Khan, Umar Ali Khan
  • Patent number: 11680064
    Abstract: The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of a Retroviridae viral infection, including an infection caused by the HIV virus.
    Type: Grant
    Filed: June 24, 2021
    Date of Patent: June 20, 2023
    Assignee: Gilead Sciences, Inc.
    Inventors: Chienhung Chou, Darryl Kato, Scott E. Lazerwith, John O. Link, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 11306103
    Abstract: The present invention relates to a novel thieno[3,2-b]pyridine-5(4H)-one derivative compound, a preparation method thereof, and a use thereof. The novel thieno[3,2-b]pyridine-5(4H)-one derivative compound according to the present invention is synthesized via an aza-[3+3] cyclization addition reaction using BOP, wherein the compound is obtained by synthesizing a 4-arylthiophen-3-amine in which aryl groups such as 4-piperidyl-C6H4, 4-pyrrolidyl-C6H4, 4-MeOC6H4, 3,4,5-(MeO)3C6H4, C6H5, 4-C6H5C6H4, and 4-F3COC6H4 are introduced via a synthesis process by a bromination reaction, a hydrolysis reaction, a decarboxylation reaction, and a Suzuki coupling reaction of methyl 3-aminothiophene carboxylate, and by synthesizing 4-arylthiophen-3-amine and mono-methyl fumarate via a formal aza-[3+3] cyclization addition reaction using BOP and conjugation.
    Type: Grant
    Filed: December 27, 2017
    Date of Patent: April 19, 2022
    Inventors: Jong Seok Lee, Dan Bi Sung, Bo Hyun Mun, Hyi Seung Lee, Yeon Ju Lee, Ji Hoon Lee, Hee Jae Shin, Sol Park
  • Patent number: 10906898
    Abstract: Improving the solubility of an organic compound. A cocrystal of (1) 6-ethyl-N-[1-(hydroxyacetyl)piperidin-4-yl]-1-methyl-4-oxo-5-(2-oxo-2-phenylethyl)-3-(2,2,2-trifluoroethoxy)-4,5-dihydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide and (2) L-malic acid or L-tartaric acid.
    Type: Grant
    Filed: January 31, 2017
    Date of Patent: February 2, 2021
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kentaro Iwata, Yukihiro Ikeda
  • Patent number: 10829497
    Abstract: Disclosed are a crystal form II of a thienopyridine derivative bisulfate and a preparation method therefor and the use thereof. The X-ray powder diffraction pattern of the crystal form II represented by the 2? diffraction angle exhibits characteristic diffraction peaks at 12.86°, 13.58°, 15.58°, 17.64°, 18.42°, 21.56°, 22.90°, 23.70° and 24.64°. The crystal form can be used as an active ingredient for preparing a pharmaceutical composition for preventing and treating diseases caused by thrombi. Compared with the original crystal form, the crystal form II of the invention has a better stability, with denser bulk solid particles, and is less susceptible to static electricity, and has better fluidity and compressibility, and when used as an active ingredient for preparing a pharmaceutical composition, the pharmaceutical preparation prepared with the crystal form II has a stronger stability.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: November 10, 2020
    Assignee: ZHONGRONG KAITE (BEIJING) BIOTECHNOLOGY CO., LTD.
    Inventors: Jingkai Gu, Xueyu Xu, Hao Wang, Xue Zhao
  • Patent number: 10334132
    Abstract: An image reading device includes an image reading portion, a detection processing portion, a determination processing portion, and a rotation processing portion. The image reading portion is configured to read an image of a document. The detection processing portion is configured to detect a face image included in a read image read by the image reading portion. The determination processing portion is configured to determine an orientation of the face image when the face image is detected by the detection processing portion. The rotation processing portion is configured to rotate the read image so as to cause the orientation of the face image determined by the determination processing portion to coincide with a predetermined specific direction when the orientation of the face image does not coincide with the specific direction.
    Type: Grant
    Filed: October 25, 2017
    Date of Patent: June 25, 2019
    Assignee: KYOCERA Document Solutions Inc.
    Inventor: Arvin Gil Servino
  • Patent number: 10065929
    Abstract: The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: September 4, 2018
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Romain Siegrist, Bibia Heidmann, Simon Stamm, John Gatfield, Olivier Bezencon
  • Patent number: 9943507
    Abstract: Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: April 17, 2018
    Assignees: Memorial Sloan-Kettering Cancer Center, The Rockefeller University
    Inventors: Marilyn D. Resh, Joseph Fraser Glickman, Elissaveta Petrova, Ouathek Ouerfelli
  • Patent number: 9597320
    Abstract: Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: March 21, 2017
    Assignees: Memorial Sloan-Kettering Cancer Center, The Rockefeller University
    Inventors: Marilyn D. Resh, Joseph Fraser Glickman, Elissaveta Petrova, Ouathek Ouerfelli
  • Patent number: 9340555
    Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
    Type: Grant
    Filed: July 28, 2014
    Date of Patent: May 17, 2016
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu
  • Patent number: 9266874
    Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: February 23, 2016
    Assignee: LIGAND PHARMACEUTICALS INCORPORATED
    Inventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
  • Patent number: 9260450
    Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: February 16, 2016
    Assignee: THESAN PHARMACEUTICALS, INC.
    Inventors: Stephen D. Barrett, James B. Kramer, Mark L. Boys, Huifen Chen
  • Patent number: 9242994
    Abstract: Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: January 26, 2016
    Assignees: Memorial Sloan-Kettering Cancer Center, The Rockefeller University
    Inventors: Marilyn D. Resh, Joseph Fraser Glickman, Elissaveta Petrova, Ouathek Ouerfelli
  • Patent number: 9233980
    Abstract: The present invention provides a novel process for preparing a substituted aromatic compound such as an aromatic halo compound or a salt thereof through a transformation reaction of an aromatic diazonium salt from an aromatic amino compound at stable high yields utilizing a novel Sandmeyer-like reaction using a nitroxide radical compound as a reaction catalyst.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: January 12, 2016
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventor: Koutarou Kawanami
  • Patent number: 9091692
    Abstract: There is provided a fluorescent dye which can improve the fluorescent intensity at the time of labeling to thereby detect a biomolecule with higher sensitivity. The fluorescent dye of the present invention includes a nitrogen cation-containing group or a nitrogen-containing group. Its high water solubility can improve the rate of labeling for a biomolecule to thereby detect a biomolecule with high sensitivity.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: July 28, 2015
    Assignee: SHINICHIRO ISOBE
    Inventors: Shinichiro Isobe, Shuntaro Mataka
  • Patent number: 9045493
    Abstract: Compounds of the formula I are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: June 2, 2015
    Assignee: MERCK PATENT GMBH
    Inventors: Hans Michael Eggenweiler, Guenter Hoelzemann, Dieter Dorsch
  • Patent number: 9040707
    Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, Andrés Avelino Trabanco-Suárez, Susana Conde-Ceide, Gary John Tresadern, José Manuel Bartolomé-Nebreda, Joaquin Pastor-Fernández
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Patent number: 9034896
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene) Heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 21, 2014
    Date of Patent: May 19, 2015
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
  • Publication number: 20150133465
    Abstract: The invention provides compounds of formula (I): wherein R1-R3, n, and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Yongzheng Zhang, Malvika Kaul
  • 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: 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: 9018378
    Abstract: This invention relates to intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: April 28, 2015
    Assignee: Methylgene Inc.
    Inventors: Franck Raeppel, Ljubomir Isakovic, Stephen William Claridge, Michael Mannion, Lijie Zhan, Marie-Claude Granger, Arkadii Vaisburg
  • Patent number: 9018134
    Abstract: There is provided a compound having an excellent controlling effect on pests represented by the formula (1): wherein, A1 represents —NR7—, etc., A2 represents a nitrogen atom, etc., A3 represents a nitrogen atom, etc., R1 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R2, R3 and R4 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more halogen atoms, etc., R5 and R6 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R7 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group W, etc., n represents 0, 1 or 2, or an N-oxide thereof.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: April 28, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masaki Takahashi, Takamasa Tanabe, Mai Ito, Yoshihiko Nokura, Atsushi Iwata
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150105419
    Abstract: Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Marilyn D. Resh, Joseph Fraser Glickman, Elissaveta Petrova, Ouathek Ouerfelli
  • Publication number: 20150099883
    Abstract: The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: in the formula, Cy represents an unsubstituted or X-substituted phenyl group or the like, X represents a halogen atom or the like, R1 represents an ethyl group or the like, R2 represents a hydrogen atom or the like, R3 and R4 represents a methyl group or the like, X1 represents a methylthio group or the like, m1 represents an integer of 1 to 4, X2 represents a methyl group or the like, m2 is an integer of 0 to 3.
    Type: Application
    Filed: April 8, 2013
    Publication date: April 9, 2015
    Inventors: Hironori Furukawa, Daisuke Hanai, Tetsuo Tamai, Jun Kanazawa, Katsunori Tanaka, Asaho Nagagata
  • Patent number: 9000006
    Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Grant
    Filed: April 9, 2014
    Date of Patent: April 7, 2015
    Assignee: Fibrogen, Inc.
    Inventors: Eric D. Turtle, Lee A. Flippin, Michael P. Arend, Heng Cheng
  • Publication number: 20150094315
    Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
    Type: Application
    Filed: July 1, 2014
    Publication date: April 2, 2015
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
  • Publication number: 20150094329
    Abstract: A compound represented by formula (1) and an N-oxide thereof have excellent pest control effect. (In the formula, Het to which R1—S(O)n is bonded represents a five-membered aromatic heterocyclic ring represented by formula H1, H2, H3 or H4 (wherein Y1 represents an oxygen atom or the like; Y2 represents an oxygen atom or the like; G1, G2 and G3 may be the same or different and each represents a nitrogen atom or the like; R1 represents a C1-C6 alkyl group which may have one or more atoms or groups selected from the group X, or the like; and n represents 0, 1 or 2); A1 represents an oxygen atom or the like; A2 represents a nitrogen atom or the like; A3 represents a nitrogen atom or the like; and R2 and R3 may be the same or different and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from the group X, or the like.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 2, 2015
    Inventors: Yoshihiko Nokura, Mai Ito, Chie Shimizu, Hajime Mizuno
  • Publication number: 20150087829
    Abstract: The present invention relates to compounds of formula I wherein RS denotes F or CF3, Ra denotes H or C1-4-alkyl and Z denotes a leaving group or an optionally substituted or protected hydroxyl group, suitable as intermediates in the synthesis of indanyloxydihydrobenzofuranylacetic acids, which are GPR40 agonists, to a process for preparing these intermediates and to the process for preparing the GPR40 agonists making use of an asymmetric catalytic hydrogenation reaction in the presence of a transition metal catalyst and a chiral auxiliary.
    Type: Application
    Filed: September 24, 2014
    Publication date: March 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Georg DAHMANN, Holger WAGNER, Matthias ECKHARDT, Markus FRANK, Marco SANTAGOSTINO, Juergen SCHNAUBELT, Uwe STERTZ, Thorsten PACHUR
  • Publication number: 20150080377
    Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a
    Type: Application
    Filed: August 31, 2013
    Publication date: March 19, 2015
    Inventor: Daljit Singh Dhanoa
  • Publication number: 20150076418
    Abstract: The invention relates to novel conjugated polymers comprising in their backbone one or more divalent donor units, like for example benzo[1,2-b:4,5-b?]dithiophene-2,6-diyl (BDT), that are linked on both sides to an acceptor unit, to methods of preparing the polymers and educts or intermediates used in such preparation, to polymer blends, mixtures and formulations containing the polymers, to the use of the polymers, polymer blends, mixtures and formulations as semiconductors organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to OE, OPV and OPD devices comprising these polymers, polymer blends, mixtures or formulations.
    Type: Application
    Filed: February 15, 2013
    Publication date: March 19, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Nicolas Blouin, Amy Phillips, Lana Nanson, Steven Tierney, Toby Cull, Priti Tiwana, Stephane Berney, Miguel Carrasco-Orozco, Frank Egon Meyer
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Publication number: 20150072993
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Zengyun AN, Liang CHEN, Shuhui CHEN, Jean Marie DEFAUW, Scott Dale HOLMSTROM, Ping HU, Chongzhi TANG, William Hunter WHITE, Wentao WU, Yang ZHANG
  • Publication number: 20150072998
    Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
    Type: Application
    Filed: April 16, 2013
    Publication date: March 12, 2015
    Inventors: Sanford Markowitz, James K.V. Willson, Bruce A. Posner, Joseph Ready, Yongyou Zhang, Hsin-Hsiung Tai, Melissa Moss, Monika Antczak, Stanton Gerson, KiBeom Bae, Sung Yeun Yang, Amar Desai
  • Patent number: 8975407
    Abstract: The present application is related to compounds represented by Formula I, which are novel allosteric modulators of ?7nAChR.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 10, 2015
    Assignee: Anvyl LLC
    Inventor: Richard Kanner
  • Patent number: 8975235
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 10, 2015
    Assignee: InterMune, Inc.
    Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Publication number: 20150065468
    Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
  • Publication number: 20150065501
    Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Publication number: 20150057265
    Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Yun-Long Li, David M. Burns, Hao Feng, Taisheng Huang, Song Mei, Jun Pan, Oleg Vechorkin, Hai-Fen Ye, Wenyu Zhu, Maria Rafalski, Anlai Wang, Chu-Biao Xue
  • Patent number: 8962627
    Abstract: The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: February 24, 2015
    Assignee: Prestwick Chemical, Inc.
    Inventors: Stephan Schann, Stanislas Mayer, Christophe Morice, Bruno Giethlen
  • Patent number: 8962598
    Abstract: The present invention relates to compounds which are 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: February 24, 2015
    Assignee: Immunahr AB
    Inventor: Lars Pettersson
  • Patent number: 8957211
    Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: February 17, 2015
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • Publication number: 20150045217
    Abstract: Thiazolopyridinones of the general formula (I) are described as herbicides. In this formula (I), R1, R2, R3 and R4 represent radicals such as hydrogen, organic radicals such as alkyl and other radicals such as halogen, nitro and cyano.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 12, 2015
    Inventors: Christian Waldraff, Stefan Lehr, Alfred Angermann, Hansjoerg Dietrich, Jan Dittgen, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker
  • Patent number: 8952160
    Abstract: The present invention relates to novel compounds according to Formula I or II, methods, and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF). Formula (I) or (II).
    Type: Grant
    Filed: January 12, 2009
    Date of Patent: February 10, 2015
    Assignee: Fibrogen, Inc.
    Inventors: Xiaoti Zhou, Michael P. Arend, Min Wu, Lee A. Flippin
  • Patent number: 8952161
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: February 10, 2015
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
  • Publication number: 20150034161
    Abstract: Organic molecule semi-conducting chromophores containing a halogen-substituted core structure are disclosed. Such compounds can be used in organic heterojunction devices, such as organic molecule solar cells and transistors.
    Type: Application
    Filed: February 19, 2013
    Publication date: February 5, 2015
    Inventors: Arnold B. Tamayo, Corey V. Hoven, Thomas K. Wood, Braden Smith