Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/245)
  • Patent number: 11414390
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, and/or solvates, racemic mixtures, enantiomers, diasteromers, and tautomers thereof, wherein A, R1, R2, R3, R3?, R4, R4?, R5, R6, R7, R8, m, and n are as defined in the detailed description.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: August 16, 2022
    Assignee: Hutchison Medipharma Limited
    Inventors: Wei-Guo Su, Guangxiu Dai, Kun Xiao
  • Patent number: 11206827
    Abstract: The present invention relates to a herbicidal composition comprising specific quinolinecarboxylic acids selected from quinclorac and quinmerac. The invention also relates to methods and uses for controlling undesirable vegetation, in particular in crops.
    Type: Grant
    Filed: July 6, 2016
    Date of Patent: December 28, 2021
    Assignee: BASF AGRO B.V.
    Inventors: Helmut Kraus, Bernd Sievernich, Mariano Etcheverry, Richard R. Evans, Ryan Louis Nielson, Cyrill Zagar, Rex A. Liebl
  • Patent number: 11201291
    Abstract: The invention relates to purely organic emitter molecules of a new type according to formula I and to the use thereof in optoelectronic devices, in particular in organic light-emitting diodes (OLEDs), comprising donor D: an aromatic or heteraromatic chemical group on which the HOMO is located and which optionally has at least one substitution; acceptor A: an aromatic or heteromatic chemical group on which the LUMO is located and which optionally has at least one substitution; bridge B1, bridge B2: organic groups that link the donor D and the acceptor A in a non-conjugated manner; wherein in particular the energy difference ?E(S1?T1) between the lowest excited singlet (S1) state of the organic emitter molecule and the triplet (T1) state of the organic emitter molecule lying thereunder is less than 2000 cm?1.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: December 14, 2021
    Assignee: SICHUAN KNOWLEDGE EXPRESS INSTITUTE FOR INNOVATIVE TECHNOLOGIES CO., LTD
    Inventors: Hartmut Yersin, Rafal Czerwieniec, Larisa Mataranga-Popa
  • Patent number: 11028061
    Abstract: Formulations and methods for reducing blood glucose and/or increasing insulin signaling in a subject have been developed. The formulations include SBI-477 and compounds based on SBI-477 i.e., SBI-477 analogs (collectively, SBI-477 compounds) and/or Mondo family inhibitors, in an effective amount to inhibit intracellular lipid accumulation and/or increase cellular glucose uptake when compared to levels in a control subject not administered the composition. Also disclosed are methods of reducing intracellular lipid accumulation and/or increase glucose uptake in a subject in need thereof. The method includes administering to the subject an effective amount of SBI-477 compounds and/or Mondo family inhibitor to reducing intracellular lipid accumulation and/or increase glucose uptake in the subject.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: June 8, 2021
    Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Daniel Kelly, Richard Vega, Hampton Sessions, Teresa Leone, Byungyong Ahn, Satyamaheshwar Peddibhotla
  • Patent number: 11021464
    Abstract: The invention discloses a crystal of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine compound, a mesylate salt and crystal thereof, a preparation method thereof, a composition containing thereof, and a use thereof for inhibiting activity of mutant IDH2 and treating cancer.
    Type: Grant
    Filed: January 22, 2018
    Date of Patent: June 1, 2021
    Assignees: Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Lianyungang Runzhong Pharmaceutical Co., Ltd, Centaurus Biopharma Co., Ltd
    Inventors: Ticong Huang, Huifeng Xiao, Rui Zhao, Fei Liu, Wei Wei, Hongjiang Xu, Xiaojin Wang, Jingli Wu
  • Patent number: 10961254
    Abstract: The present invention relates to 2-amino-4-arylpyrimidine and 2-amino-4-aryltriazine compounds as inhibitors of heat shock protein 90 family of chaperone proteins. The invention also features pharmaceutical compositions and kits that include the compounds and compositions of the invention. The invention further relates to the medical use of these compounds and compositions for the treatment of a disorder in a subject. For example, the disorder is a neurodegenerative disease.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: March 30, 2021
    Assignees: Yuma Therapeutics, Inc., The Brigham and Women's Hospital, Inc.
    Inventors: Gregory D. Cuny, Marcie A. Glicksman, Kevin J. Hodgetts, Steven L. Mathieu, Yukari Y. Perrella, Vincent Darmency, Hrvoje Lusic
  • Patent number: 10723722
    Abstract: The present invention relates to materials for organic electroluminescent devices, in particular carbazolyl compounds substituted by electron-deficient heteroaryl groups, for use as triplet matrix materials in organic electroluminescent devices, for example the compounds of formula (1). The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these.
    Type: Grant
    Filed: October 11, 2016
    Date of Patent: July 28, 2020
    Assignee: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Aurélie Ludemann, Dominik Joosten, Tobias Grossmann, Jonas Valentin Kroeber
  • Patent number: 10611736
    Abstract: The present invention provides a 2,4,6-trisubstituted s-triazine compound represented by general formula (I) or pharmaceutically acceptable salts, prodrugs or solvates thereof, a preparation method therefor, and use of these compounds in preparing drugs for preventing or treating diseases associated with protein kinase and vimentin dysregulation, and cell vacuolization, and in particular, drugs for treating or preventing cancer growth and metastasis, tissue fibrosis and atherosclerosis.
    Type: Grant
    Filed: May 11, 2017
    Date of Patent: April 7, 2020
    Assignee: Aluda Pharmaceuticals, Inc.
    Inventors: Qizheng Yao, Jianping Wu, Ruihuan Chen, Lei Zhang, Shining Yao, Lian Mo, Qingqing Zhang
  • Patent number: 10105369
    Abstract: Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL).
    Type: Grant
    Filed: January 8, 2018
    Date of Patent: October 23, 2018
    Assignee: Agios Pharmaceuticals, Inc.
    Inventor: Samuel V. Agresta
  • Patent number: 9986735
    Abstract: Described herein are compositions and methods for increasing the survivability of one or more beneficial microorganisms.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: June 5, 2018
    Assignee: NOVOZYMES BIOAG A/S
    Inventors: Diego Omar Demares, Florencia Olivieri, Gabriel Osvaldo Gutkind
  • Patent number: 9889137
    Abstract: Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL).
    Type: Grant
    Filed: June 2, 2017
    Date of Patent: February 13, 2018
    Assignee: Agios Pharmaceuticals, Inc.
    Inventor: Samuel V. Agresta
  • Patent number: 9856204
    Abstract: In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: January 2, 2018
    Assignees: UNIVERSITY OF IOWA RESEARCH FOUNDATION, THE UNITED STATES OF AMERICA AS REPRESENTED BY VETERANS AFFAIRS
    Inventors: Christopher M. Adams, Steven D. Kunkel, Manish Suneja, Michael Welsh
  • Patent number: 9845298
    Abstract: The invention provides novel compounds and compositions comprising a 5-HT2B antagonist of formula I: and related methods for treating a person having a disorder characterized by undesirable 5-HT2B receptor signaling, such as migraine, irritable bowel syndrome (IBS), pulmonary arterial hypertension (PAH), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (GI) tract disorders.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: December 19, 2017
    Assignee: National Institute of Biological Sciences, Beijing
    Inventors: Niu Huang, Yu Zhou, Xingyu Lin
  • Patent number: 9814464
    Abstract: A wound drainage and hemostasis promoting medical device (1) are disclosed. A balloon (15) is temporary inflated and arranged outside a sheath (10), in contact with tissue surrounding a wound cavity for hemostasis promotion. The drainage device comprises a fluid communication channel for wound exudate from wound. The balloon is deflated and retracted into said sheath for removal from said wound cavity. Thus the medical device is percutaneously retractable from said confined wound.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: November 14, 2017
    Assignee: AEEG AB
    Inventor: Anders Jönsson
  • Patent number: 9751845
    Abstract: The invention provides novel compounds and compositions comprising a 5-HT2B antagonist of formula I: and related methods for treating a person having a disorder characterized by undesirable 5-HT2B receptor signaling, such as migraine, irritable bowel syndrome (IBS), pulmonary arterial hypertension (PAH), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (GI) tract disorders.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: September 5, 2017
    Assignee: National Institute of Biological Sciences, Beijing
    Inventors: Niu Huang, Yu Zhou, Xingyu Lin
  • Patent number: 9694013
    Abstract: Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL).
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: July 4, 2017
    Assignee: Agios Pharmaceuticals, Inc.
    Inventor: Samuel V. Agresta
  • Patent number: 9598410
    Abstract: The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or arterial flutter.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: March 21, 2017
    Assignee: SANOFI
    Inventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler, Josef Pernerstorfer, Joachim Brendel
  • Patent number: 9586936
    Abstract: A heteroarylamine compound includes protein kinase inhibition activity, a pharmaceutically acceptable salt thereof and a pharmaceutical composition for preventing and treating a disease caused by abnormal cell growth, which contains the compound as an active ingredient.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: March 7, 2017
    Assignee: KOREA INSTITITUE OF SCIENCE AND TECHNOLOGY
    Inventors: Tae Bo Sim, Ho Jong Yoon, Ji Hye Yoon, Woo Young Hur, Eun Joo Roh, Yeon Ui Kwak
  • Patent number: 9409903
    Abstract: The invention provides triazine compounds and methods of their use to modulate protein kinases and to treat diseases mediated by said protein kinases.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: August 9, 2016
    Assignee: NantBioScience, Inc.
    Inventors: Chunlin Tao, Qinwei Wang, David Ho, Laxman Nallan, Tulay Polat, Xiaowen Sun, Neil Desai
  • Patent number: 9382215
    Abstract: The invention provides compounds, compositions and methods for treating myotonic dystrophy. The compounds can selectively bind to CUG repeats in RNA, or to CTG repeats in DNA, and inhibit replication of the nucleic acids.
    Type: Grant
    Filed: June 5, 2014
    Date of Patent: July 5, 2016
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Steven C. Zimmerman, Chun-Ho Wong, Paul J. Hergenrother, Jessie Peh
  • Patent number: 9376421
    Abstract: The invention provides rationally designed multi-targeting therapeutic agents for myotonic dystrophy type 1 (DM1), an incurable neuromuscular disease that originates in an abnormal expansion of CTG repeats (CTGexp) in the DMPK gene. The rationally designed small molecules target the DM1 pathobiology in three distinct ways: (1) binding the expanded trinucleotide repeat, CTGexp, and inhibiting its transcription to the toxic CUGexp RNA, (2) binding the CUGexp RNA and releasing sequestered muscleblind-like protein (MBNL1), and (3) cleaving the toxic CUGexp in an RNase-like manner. Importantly, the compounds can reduce the levels of CUGexp in DM1 model cells and reverse two separate CUGexp-induced phenotypes of DM1.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: June 28, 2016
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Steven C. Zimmerman, Long M. Luu, Lien T. T. Nguyen
  • Patent number: 9309239
    Abstract: The present application relates to novel substituted 6-fluoro-1H-pyrazolo[4,3-b]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for preparing Medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: April 12, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat
  • Patent number: 9271984
    Abstract: The present invention relates to triazine derivatives of formula (I) for their use in the treatment of type 1 diabetes mellitus, and to compositions comprising said triazine derivatives.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: March 1, 2016
    Assignee: POXEL
    Inventors: Pascale Fouqueray, Daniel Cravo, Sophie Hallakou-Bozec, Sébastien Bolze
  • Patent number: 9221768
    Abstract: For the separation, removal, isolation, purification, characterisation, identification or quantification of fibrinogen or a protein that is a fibrinogen analogue, an affinity adsorbent is used that is a compound of formula II wherein one X is N and the other is N, C—CI or C—CN; Y is O, S or NR2; Z is O, S or NR3; R2 and R3 are each H, alkyl, hydroxyalkyl, benzyl or ?-phenylethyl; n is 0 to 6; A is a support matrix, optionally linked to the triazine ring by a spacer; R7 is a group bearing a positive charge at neutral pH; W is an optional linker; V is an aromatic group; and R8 and R9 are each H, OH, alkyl, alkoxy, amino, NH2, acyloxy, acylamino, CO2H, sulphonic acid, carbamoyl, sulphamoyl, alkylsulphonyl or halogen or a cyclic structure such as a morpholino group, or R8 and R9 are linked to form such a cyclic structure.
    Type: Grant
    Filed: July 30, 2013
    Date of Patent: December 29, 2015
    Assignee: PROMETIC BIOSCIENCES INC.
    Inventors: Jason Richard Betley, James Christopher Pearson, Ben Martin Beacom, Tadeusz Antoni Podgorski, Robert William Pannell
  • Patent number: 9216198
    Abstract: The present disclosure describes compositions providing for controlled release of nitric oxide (NO) and methods for production of these compositions. In some embodiments, the compositions may include a biodegradable polymer and a nitric oxide-releasing material at least partially encapsulated by the biodegradable polymer. Nitric oxide-releasing materials may include, for example, diazeniumdiolates and nitric oxide contained within a zeolite, metal-organic framework or other porous material. In general, the compositions are spun into a porous fiber, which may be further annealed by heating in order to densify the fiber. Annealing may prolong the NO release profile. Medical devices containing the compositions described herein are also contemplated by the present disclosure. Medical devices include, for example, textiles, bandages and articles of clothing.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: December 22, 2015
    Assignee: THE BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Kenneth J. Balkus, Jr., Harvey A. Liu
  • Patent number: 9150546
    Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ?Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ?Z is ?O, etc.; and n is an integer of 0 to 4.
    Type: Grant
    Filed: February 10, 2010
    Date of Patent: October 6, 2015
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Hiroyuki Kai, Takayuki Kameyama, Tsuyoshi Hasegawa, Miho Oohara, Yukio Tada, Takeshi Endoh
  • Patent number: 9144573
    Abstract: The present invention generally relates to prostaglandin transport. More specifically, the invention is directed to compounds that inhibit prostaglandin transport and subsequent COX-2 induction, and methods relating thereto.
    Type: Grant
    Filed: July 23, 2012
    Date of Patent: September 29, 2015
    Assignees: Albert Einstein College of Medicine of Yeshiva University, New York University
    Inventors: Victor L. Schuster, Yuling Chi, Young-Tae Chang, Jaeki Min
  • Patent number: 9139586
    Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: February 21, 2014
    Date of Patent: September 22, 2015
    Assignee: Novartis AG
    Inventors: Gurdip Bhalay, Emma Budd, Graham Charles Bloomfield, Stephen Paul Collingwood, Andrew Dunstan, Lee Edwards, Peter Gedeck, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt, Paul Oakley, Nichola Smith
  • Patent number: 9133171
    Abstract: The present invention relates to disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: September 15, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulrich Lücking, Dirk Kosemund, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Rolf Bohlmann
  • Patent number: 9090609
    Abstract: The present application relates to novel benzyl-substituted carbamates, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: July 28, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Niels Lindner, Frank Wunder, Volkhart Min-Jian Li
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Publication number: 20150147376
    Abstract: Microparticles containing an ultraviolet light absorbing polymer and 3-iodo-2-propynyl butylcarbamate (“IPBC”) resist discoloration by sunlight and other ultraviolet light sources. Methods for preparing the microparticles produce polymer-shielded, formaldehyde-free IPBC formulations which resist discoloration and leaching, and are especially useful in water-based applications. The microparticles include a polymer or a poly(vinyl formal) homopolymer that absorbs light over a range of ultraviolet wavelengths associated with IPBC discoloration. The microparticles may be utilized in paints, stains, stuccoes, adhesives, and plastics, for example.
    Type: Application
    Filed: December 29, 2014
    Publication date: May 28, 2015
    Inventor: Jorg Thomas Wilken
  • Patent number: 9040530
    Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 26, 2015
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
  • Patent number: 9035048
    Abstract: The invention relates to compounds of formula (I) wherein the radicals R1 to R6 have the meaning according to claim 1, and/or physiologically acceptable salts thereof, for the prophylactic or therapeutic treatment and/or monitoring of physiological and/or pathological conditions that are associated with the activity of AMP-activated protein kinase (AMPK). Another object of the invention concerns the use of said compounds for enhancing glucose homeostasis, improving podocytopathy and/or decreasing the production of reactive oxygen species (ROS). The invention also relates to a method for in-vitro diagnosing diabetic nephropathy and a method for screening compounds that reduce podocytopathy, in each case by applying synaptopodin as biomarker.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: May 19, 2015
    Assignee: POXEL
    Inventors: Daniel Cravo, Sophie Hallakou-Bozec, Didier Mesangeau, Samer Elbawab
  • Publication number: 20150126510
    Abstract: The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.
    Type: Application
    Filed: March 18, 2013
    Publication date: May 7, 2015
    Applicants: Universiteit Antwerpen, Shakturana CV
    Inventors: Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Kevin Karel Florentina Arien, Guido Louis Emile Vanham, Paulus Lewi (deceased)
  • Publication number: 20150126512
    Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 7, 2015
    Applicant: GENZYME CORPORATION
    Inventors: Scott F. Sneddon, John L. Kane, Bradford H. Hirth, Frederic Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
  • Publication number: 20150126506
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Publication number: 20150119362
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 30, 2015
    Inventors: Mark E. Gurney, Timothy J. Hagen, Joel R. Walker, Xuesheng Mo, A. Samuel Vellekoop, Robert Campbell, Lei Zhu, Donna L. Romero
  • Patent number: 9018209
    Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: April 28, 2015
    Assignee: Yale University
    Inventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
  • Publication number: 20150111731
    Abstract: A pesticidal composition comprises one or more of the following compounds: 3-(thiazol-2-yl)pyridine 1-oxide compound of formula I or II, or N-(4-chloro-2-(pyridin-3-yl)thiazol-5-yl)-3-(methylthio)propanamide compound (C3), or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and Q, are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Negar Garizi, Martin J. Walsh, Ann M. Buysse, Daniel Knueppel, Asako Kubota, Noormohamed M. Niyaz, Yu Zhang, Ricky Hunter, Tony K. Trullinger
  • Publication number: 20150110742
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) and Toll-like receptor agonist (TLR) through a linker and a multifunctional connector group or molecule.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 23, 2015
    Applicant: Yale University
    Inventors: David Spiegel, Kelly Fitzgerald
  • Publication number: 20150111871
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 23, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Publication number: 20150111873
    Abstract: Pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 23, 2015
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch, Gerd Rühter, Carsten Schultz-Fademrecht, Peter Nussbaumer
  • Publication number: 20150111857
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
  • Publication number: 20150105377
    Abstract: The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: March 12, 2013
    Publication date: April 16, 2015
    Inventors: Joseph M. Gozgit, Victor M. Rivera, William C. Shakespeare, Xiaotian Zhu, David C. Dalgarno
  • Publication number: 20150094310
    Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventor: Florian Holsboer
  • Patent number: 8993757
    Abstract: The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
  • Patent number: 8987264
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
  • Patent number: 8987265
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
  • Publication number: 20150080393
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 19, 2015
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner