Plural 1,4-diazine Rings Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/252.11)
  • Patent number: 10301630
    Abstract: The present invention provides methods and compositions for inducing expression of Ube3a in a cell by contacting the cell with a topoisomerase inhibitor. Particular embodiments include a method of treating a genomic imprinting disorder, such as Angelman syndrome, in a subject by administering to the subject an effective amount of a topoisomerase inhibitor.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: May 28, 2019
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Benjamin David Philpot, Mark John Zylka, Bryan Leo Roth, John Arthur Allen, Hsien-Sung Huang
  • Patent number: 10150761
    Abstract: The invention concerns novel substituted pyridine-piperazinyl analogs of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: December 11, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Delphine Yvonne Raymonde Lardeau, Xavier Marc Bourdrez, Wendy Mia Albert Balemans, Dirk André Emmy Roymans
  • Patent number: 10124001
    Abstract: Disclosed are methods and compositions for modulating cancer stem cells. More particularly, the present invention discloses the use of protein kinase C theta inhibitors (PKC-?) for inhibiting the growth of PKC-?-overexpressing cells including cancer stem cells, for enhancing the biological effects of chemotherapeutic drugs or irradiation on cancer cells, for treating cancer, including metastatic cancer and/or for preventing cancer recurrence.
    Type: Grant
    Filed: September 18, 2014
    Date of Patent: November 13, 2018
    Assignee: University of Canberra
    Inventors: Sudha Rao, Anjum Zafar
  • Patent number: 10123949
    Abstract: The group of inventions relates to the field of aesthetic, plastic and reconstructive cosmetology/medicine, and more particularly to meso threads used for remedying aesthetic and age-related changes to the skin, and to methods for producing such threads. Proposed is a multicomponent meso thread consisting of a core and a shell. The core is realized in the form of a fibroin thread, and the shell contains hyaluronic acid or a salt thereof or a polyelectrolyte complex of hyaluronic acid or a salt thereof and chitosan or a salt thereof. Also proposed are a variant of the thread having a plastifying agent in the shell, and methods for producing the proposed meso threads.
    Type: Grant
    Filed: April 11, 2016
    Date of Patent: November 13, 2018
    Assignee: MARTIN'EX International Research and Development Centre
    Inventors: Natal'ya Pavlovna Mihajlova, Mihail Anatol'evich Selyanin, Sergej Alekseevich Uspenskij
  • Patent number: 10085981
    Abstract: Embodiments of the present disclosure include compositions and pharmaceutical compositions that include protein acyl transferases (PAT) inhibitors, methods of treating a condition or disease, methods of treating autopalmitoylation activity, and the like.
    Type: Grant
    Filed: July 13, 2016
    Date of Patent: October 2, 2018
    Assignees: University of South Florida, Torrey Pines Institute for Molecular Studies
    Inventors: Robert Joseph Deschenes, Marcello Angelo Giulianotti, Richard Allen Houghten, David Allen Mitchell, Laura Dawn Hamel
  • Patent number: 10052322
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
    Type: Grant
    Filed: October 23, 2017
    Date of Patent: August 21, 2018
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Anil Menon, Darshan K. Parikh, Dora Visky, Nathan Boersen, Thomas Lee, Xiaozhang Liang
  • Patent number: 9920035
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: March 20, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Sara Frattini, Dieter Hamprecht, Joerg Kley
  • Patent number: 9827243
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: November 28, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Matthew Michael Kreilein, Thomas Lee, Ying Li, Jean Xu, William Wei-Hwa Leong, Benjamin Cohen
  • Patent number: 9783526
    Abstract: The present invention relates to oligooxopiperazines that mimic helix ?B of the C-terminal transactivation domain of HIF-1?. Also disclosed are pharmaceutical compositions containing these oligooxopiperazines and methods of using these oligooxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF-1? with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).
    Type: Grant
    Filed: February 8, 2016
    Date of Patent: October 10, 2017
    Assignee: New York University
    Inventors: Paramjit S. Arora, Brooke Bullock Lao
  • Patent number: 9782427
    Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor having the following formula (I): and an effective amount of a cytidine analog, such as 5-azacytidine, to a patient having a cancer.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: October 10, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventor: Heather Raymon
  • Patent number: 9745284
    Abstract: The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: August 29, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 9669038
    Abstract: Disclosed herein are novel heterocyclic compounds, their salts, pharmaceutical compositions comprising such compounds and salts, and their uses in modulating protein-protein interactions and for treating diseases resulting from aberrant protein-protein interactions.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: June 6, 2017
    Assignee: GLOBAVIR BIOSCIENCES, INC.
    Inventors: Chenera Balan, Usha Nagavarapu
  • Patent number: 9656975
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Grant
    Filed: November 4, 2014
    Date of Patent: May 23, 2017
    Assignee: H. Lundbeck A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Patent number: 9624203
    Abstract: The present invention relates to oligooxopiperazines and their use. Methods for preparing oligooxopiperazines are also disclosed.
    Type: Grant
    Filed: April 11, 2016
    Date of Patent: April 18, 2017
    Assignee: New York University
    Inventors: Paramjit S. Arora, Petra To{hacek over (s)}ovská, Danielle Guarracino, Brooke Bullock Lao
  • Patent number: 9624197
    Abstract: The present invention is directed to 2-pyridylamino-4-nitrile-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridylamino-4-nitrile-piperidinyl compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: April 18, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 9611277
    Abstract: The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: April 4, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Christine F. Gelin, Terry P. Lebold, Brock T. Shireman, Jeannie M. Ziff
  • Patent number: 9555033
    Abstract: Provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by a LKB1 and/or AMPK gene or protein loss or mutation.
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: January 31, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Rajesh Chopra, Yuhong Ning, Sabita Sankar, Shuichan Xu, Weiming Xu
  • Patent number: 9505764
    Abstract: Provided herein are methods for treating or preventing chronic lymphocytic leukemia, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound to a patient having chronic lymphocytic leukemia.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: November 29, 2016
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Heather Raymon, Shuichan Xu, Antonia Lopez-Girona, Toshiya Tsuji, Kristen Mae Hege
  • Patent number: 9499471
    Abstract: The present invention relates to a compound of formula (I) as defined herein.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: November 22, 2016
    Assignee: Medizinische Hochschule Hannover
    Inventors: Dietmar Manstein, Matthias Preller, Marcus Furch, Markus Kalesse, Nina Diaz-Gomez
  • Patent number: 9493440
    Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: November 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Wei Li, Andrew Stamford, Marc Poirer, Paul Tempest
  • Patent number: 9429568
    Abstract: Silaanthracene compounds and methods of producing silaanthracene compounds, in particular silaanthracene fluorophores for use as red or near infrared sensors, probes, dyes, and tags are provided.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: August 30, 2016
    Assignee: Board of Trustees of Southern Illinois University on Behalf of Southern Illinois University Carbondale
    Inventors: Daniel Dyer, Denise DeAnne Dyer, Colleen Scott, Matthew McCarroll, Lichang Wang, Narsimha Sattenapally, Quinn Best
  • Patent number: 9416134
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to the Compound for formula 1: having the name 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4 -dihydropyrazino[2,3-b]pyrazin-2(1H)-one and tautomers thereof.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: August 16, 2016
    Assignee: Signal Pharmaceuticals, LLC
    Inventor: Jeffrey Eckert
  • Patent number: 9359364
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: June 7, 2016
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Anil Menon, Darshan K. Parikh, Dora Visky, Matthew Michael Kreilein, Nathan Boersen, Thomas Lee, Ying Li, Jean Xu, Xiaozhang Liang, William Wei-Hwa Leong, Benjamin Cohen
  • Patent number: 9358232
    Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor and an effective amount of N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide to a patient having a cancer.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: June 7, 2016
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Kristen Mae Hege, Rajesh Chopra
  • Patent number: 9309230
    Abstract: The present invention relates to oligooxopiperazines and their use. Methods for preparing oligooxopiperazines are also disclosed.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: April 12, 2016
    Assignee: New York University
    Inventors: Paramjit S. Arora, Petra To{hacek over (s)}ovská, Danielle Guarracino, Brooke Bullock Lao
  • Patent number: 9310364
    Abstract: The present invention provides novel methods and assays for high-throughput screening of combinatorial libraries to identify FPR1 and/or FPR2 ligands (e.g., agonists and/or antagonists), preferably FPR1 agonists and/or FPR2 antagonists, by positional scanning deconvolution. The invention also provides novel FPR1 and FPR2 ligands (e.g, agonists and antagonists), related pharmaceutical compositions and methods of treating FPR1 and FPR2-related disorders.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: April 12, 2016
    Assignees: STC.UNM, TORREY PINES INSTITUTE FOR MOLECULAR STUDIES
    Inventors: Bruce S. Edwards, Larry A. Sklar, Clemencia Pinilla, Richard A. Houghten, Jon R. Appel, Marc A. Giulianotti, Jose Medina-Franco
  • Patent number: 9255086
    Abstract: The present invention relates to oligooxopiperazines that mimic helix ?B of the C-terminal transactivation domain of HIF-1?. Also disclosed are pharmaceutical compositions containing these oligooxopiperazines and methods of using these oligooxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF-1? with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: February 9, 2016
    Assignees: New York University, University of Southern California
    Inventors: Paramjit S. Arora, Bogdan Olenyuk, Brooke Bullock Lau, Ivan Grishagin
  • Patent number: 9212165
    Abstract: The present invention provides compounds of formula (I): where R1, R2, X, Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: December 15, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Dario Doller, Guiying Li
  • Patent number: 9199962
    Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: June 11, 2012
    Date of Patent: December 1, 2015
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Nadia Brugger, Kristopher Josephson
  • Patent number: 9187440
    Abstract: The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2—or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a ster
    Type: Grant
    Filed: August 17, 2012
    Date of Patent: November 17, 2015
    Assignee: REMYND NV
    Inventors: Gerard Griffioen, Giuseppe Cecere, Matthias Nettekoven, Katrien Princen, Hasane Ratni, Mark Rogers-Evans, Walter Vifian
  • Patent number: 9187496
    Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Grant
    Filed: November 13, 2012
    Date of Patent: November 17, 2015
    Assignee: Idenix Pharmaceuticals LLC
    Inventors: Cyril B. Dousson, David Dukhan, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
  • Patent number: 9181199
    Abstract: Disclosed are uracil derivatives of the formula (I): wherein R1, R2, R3, and X are as defined herein, and use thereof as therapeutic agents. The uracil derivatives are used in particular together with a cytostatic agent for suppressing or reducing resistance building up on cytostatic treatment.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: November 10, 2015
    Assignee: RESprotect GmbH
    Inventors: Rudolf Fahrig, Kurt Eger, Martin Fuhrer, Nicole Heinze, Matthias Klemm, Jorg-Christian Heinrich
  • Patent number: 9156819
    Abstract: The present invention is directed to 2-pyridyloxy-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyl-oxy-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: October 13, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 9155736
    Abstract: Provided herein are methods for treating a cancer treatable by inhibition of phosphorylation of PRAS40, GSK3? or p70S6K1, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a cancer treatable by inhibition of phosphorylation of PRAS40, GSK3? or p70S6K1.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: October 13, 2015
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Weiming Xu, Deborah Mortensen, Shuichan Xu, Kimberly Elizabeth Fultz
  • Patent number: 9084779
    Abstract: Novel compounds which are derivatives of tetra-O-methyl nordihydroguaiaretic acid (NDGA), as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof are provided. These NDGA derivatives have a nitroimidazole moiety and these derivatives show preferential toxicity to hypoxic cells as hypoxic cytotoxins. Their cytotoxicity toward hypoxic cells is a result of abstraction of hydrogen from target molecules by free radicals formed in the reduction of the nitro group. This makes the disclosed compounds an effective anti cancer drug because hypoxic cells are generally considered to be more resistant to anti cancer drugs than normal cells. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including hepatocellular carcinoma, breast cancer and prostate cancer, are also provided.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: July 21, 2015
    Assignee: The Johns Hopkins University
    Inventors: Ru Chih C. Huang, David Edward Mold, Jih Ru Hwu, Ming Hua Hsu, Szu Chun Wu
  • Patent number: 9067932
    Abstract: The present invention relates to compounds of pyrazolopyridine derivatives useful as inhibitors of protein kinase. In one embodiment the compounds of the present invention are represented by the following structural formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: June 30, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Boyall, Guy Brenchley, Chris Davis, Damien Fraysse, Julian Golec, Juan-Miguel Jimenez, Andrew Miller, Luca Settimo, Heather Twin, Stephen Young
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Publication number: 20150141417
    Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: May 14, 2012
    Publication date: May 21, 2015
    Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Publication number: 20150126484
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: May 7, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth Celeste Deselm, Yufang Xiao, Hui Qiu, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Publication number: 20150126499
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 9023852
    Abstract: The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: May 5, 2015
    Assignee: Remynd NV
    Inventors: Gerard Griffioen, Matthias Nettekoven, Katrien Princen, Hasane Ratni, Walter Vifian
  • Publication number: 20150119395
    Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.
    Type: Application
    Filed: April 4, 2013
    Publication date: April 30, 2015
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Patent number: 9018214
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: April 28, 2015
    Assignee: Astex Therapeutics Limited
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • Publication number: 20150111851
    Abstract: This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Timothy Boebel, Kristy Bryan, Peter Lee Johnson, Beth Lorsbach, Kevin G. Meyer, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
  • Publication number: 20150105397
    Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
  • Publication number: 20150099751
    Abstract: The in situ gel loaded with phosphodiesterase Type V (PDE5) inhibitors nanoemulsion was prepared using an innovative approach to reformulate the PDE5 inhibitors in a nanoemulsion, and then loading the nanoemulsion into an in situ gel base. These preparations are administered by intramuscular injection in order to give a depot effect for a period of time that exceeds 15 days. The in situ gel composition gives slow, controlled release of the PDE5 inhibitor. The in situ gel composition is useful for prophylaxis and treatment of some important chronic diseases, such as diabetic complications, benign prostatic hyperplasia, erectile dysfunction, and diseases associated with endothelial dysfunction.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 9, 2015
    Applicant: KING ABDULAZIZ UNIVERSITY
    Inventors: HISHAM AHMED MOHAMMED MOSLI, SALAH ABDELMONEIM GHAREIB ATTEIAH, KHALED MOHAMED HOSNY OMAR, HANY MOHAMED ABD EL-MALIK EL-BASSOSSY, MOHAMED HANY ABDULWAHAB MOSILHY HELAL
  • Patent number: 8999981
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: April 7, 2015
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
  • Publication number: 20150094294
    Abstract: The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a Plasmodium species, comprising administering to said mammal or contacting said Plasmodium species with, an effective amount of a pyrimidin-4,6-dicarboxylic acid amide derivative.
    Type: Application
    Filed: February 28, 2013
    Publication date: April 2, 2015
    Inventors: Richard W. Scott, Robert W. Kavash, Wenxi Pan, Katie Freeman, Michael J. Costanzo, Doron Greenbaum, Yongjiang Xu, Trevor Young