Additional Hetero Ring Containing Patents (Class 546/256)
  • Patent number: 10815208
    Abstract: Provided is a method for preparing 2-hydroxy-4-(2, 3-disubstituted benzyloxy)-5-substituted benzaldehyde derivative represented by formula (I). The method comprises the following steps: (1) preparing 3-aryl-2-substituted toluene derivative 2 by using 3-iodo-2-substituted toluene derivative 1 and aryl boronic acid 5 or aryl boronate as starting materials; (2) preparing a benzyl halide derivative 3 by using 3-aryl-2-substituted toluene derivative 2 as starting materials; and (3) preparing 4-(2, 3-disubstituted benzyloxy)-2-hydroxy-5-substituted benzaldehyde derivative (I) by using benzyl halide derivative 3 and 2,4-dihydroxy-5-substituted benzaldehyde 6.
    Type: Grant
    Filed: May 23, 2017
    Date of Patent: October 27, 2020
    Assignees: Institute of Materia Medica, Chinese Academy of Medical Sciences, Tianjin Chase Sun Pharmaceutical Co., LTD
    Inventors: Zhiqiang Feng, Xiaoguang Chen, Yang Yang, Fangfang Lai
  • Patent number: 10730830
    Abstract: A compound of general formula (I-1): wherein the symbols are defined in the specification, has a selective S1P5 receptor binding activity and modulates the function of an S1P5 receptor, and can therefore be a therapeutic agent for a S1P5-mediated disease, for example, neurodegenerative diseases such as schizophrenia, Binswanger's disease and the like.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: August 4, 2020
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Toshihide Watanabe, Kensuke Kusumi, Yuichi Inagaki
  • Patent number: 10710982
    Abstract: A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
    Type: Grant
    Filed: February 12, 2020
    Date of Patent: July 14, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, Jiansheng Wan
  • Patent number: 10577348
    Abstract: A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: March 3, 2020
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Pranav Gupta, Jason Wan, Scott T. Trzaska
  • Patent number: 10577367
    Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: March 3, 2020
    Assignee: BIOGEN MA INC.
    Inventors: Timothy Chan, Kevin Guckian, Tracy Jenkins, Jermaine Thomas, Jeffery Vessels, Gnanasambandam Kumaravel, Robert Meissner, Joseph Lyssikatos, Brian Lucas, Irina Leaf, Jeremy Duffield
  • Patent number: 10562850
    Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: February 18, 2020
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, V. Satish Kumar, Weihe Zhang, Lakshminarayana Vogeti
  • Patent number: 10544133
    Abstract: Compounds having the following formula: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.
    Type: Grant
    Filed: June 15, 2018
    Date of Patent: January 28, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rajeev S. Bhide, John V. Duncia, John Hynes, Satheesh Kesavan Nair, William J. Pitts, Sreekantha Ratna Kumar, Daniel S. Gardner, Natesan Murugesan, Venkatram Reddy Paidi, Joseph B. Santella, Ramesh Kumar Sistla, Hong Wu
  • Patent number: 10468256
    Abstract: A method of forming a material layer includes providing a substrate into a reaction chamber, providing a source material onto a substrate, the source material being a precursor of a metal or semimetal having a ligand, providing an ether-based modifier on the substrate, purging an inside of the reaction chamber, and reacting a reaction material with the source material to form the material layer.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: November 5, 2019
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Sun-min Moon, Youn-soo Kim, Han-jin Lim, Yong-jae Lee, Se-hoon Oh, Hyun-jun Kim, Jin-sun Lee
  • Patent number: 10414740
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: June 4, 2018
    Date of Patent: September 17, 2019
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
  • Patent number: 10208023
    Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotrophic lateral sclerosis, glaucoma, ischemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: February 19, 2019
    Inventor: Mark G. DeGiacomo
  • Patent number: 10183929
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: January 22, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar K C, John Hood
  • Patent number: 10047225
    Abstract: Disclosed are styryl dyes of formula wherein R1, R2, R3, R?1, R?2 and R?3 independently of each other are hydrogen; —NH(CO)—C1-C5alkyl; —N(C1-C5alkyl)(C1-C5alkyl-CN); C1-C6alkoxy; a heterocyclic radical; or R1 and R2 or R?1 and R?2 together form a 5- to 10-membered, monocyclic, carbocyclic or heterocyclic ring; wherein at least one of R1, R2, R3, R?1, R?2 and R?3 is different from hydrogen; Q and Q? independently from each other are the direct bond; *—C(O)—*; *—C(O)O—*; *—OCO—*; *—N(R4)—*; ?*—C(O)N(R6)—*; or *—(R6)NC(O)—*; and R4, R5 and R6 independently from each other are hydrogen; C1-C14alkyl; C2-C14alkenyl; C6-C12aryl; C6-C12aryl-C1-C10alkyl; or C1-C10alkyl(C5-C12aryl); X and X? are *—(CH2)m—*; Y1 and Y2 independently from each other are C1-C10alkylene; C5-C10cycloalkylene; C5-C12arylene; or C5-C12arylene-(C1-C10alkylene); An? is an anion; m is a number from 1 to 8; n is 0, or 1; and p is 0, or 1.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: August 14, 2018
    Assignee: BASF SE
    Inventors: Frank Bachmann, Christian Cremer, Markus Knobloch, Beate Fröhling, Werner Specker
  • Patent number: 10035787
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: July 31, 2018
    Assignee: ELI LILLY AND COMPANY
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
  • Patent number: 9988385
    Abstract: This invention provides 1,4-dihydropyrrolo[3,2-b]pyrrole derivatives which can be used as strongly fluorescent compounds and a one-stage method for their synthesis from simple substrates.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: June 5, 2018
    Assignee: INSTYTUT CHEMII ORGANICZNEJ POLSKIEJ AKADEMII NAUK
    Inventors: Anita Janiga, Maciej Krzeszewski, Daniel Gryko
  • Patent number: 9962386
    Abstract: Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, Ra, Ra?, Rb, Rc, X1, X2, X3, Rd, Z1, and Z2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.
    Type: Grant
    Filed: April 17, 2017
    Date of Patent: May 8, 2018
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Matthew O. Duffey, Dylan England, Brian Scott Freeze, Zhigen Hu, Steven Langston, Charles McIntyre, Hirotake Mizutani, Koji Ono, He Xu
  • Patent number: 9758507
    Abstract: A chiral synthesis of pyrrolidine compounds en route to selective neuronal nitric oxide synthase inhibitors, and representative inhibitor compounds heretofore unattainable.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: September 12, 2017
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Fengtian Xue
  • Patent number: 9708291
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: July 18, 2017
    Assignee: Vanda Pharmaceuticals Inc.
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
  • Patent number: 9650340
    Abstract: The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine 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: November 12, 2013
    Date of Patent: May 16, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Lücking, Niels Böhnke, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Dirk Kosemund, Rolf Bohlmann, Ludwig Zorn
  • Patent number: 9617243
    Abstract: The present invention relates to novel aminopyridyloxypyrazole compounds that inhibit the activity of transforming growth factor beta receptor 1 (TGF?R1), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, preferably colon cancer, melanoma, hepatocellular carcinoma, renal cancer, glioblastoma, pancreatic cancer, myelodysplastic syndrome, lung cancer, and gastric cancer, and/or fibrosis, preferably liver fibrosis and chronic kidney disease.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: April 11, 2017
    Assignee: Eli Lilly and Company
    Inventors: William T. McMillen, Sajan Joseph, Huaxing Pei, Jason Scott Sawyer, Gaiying Zhao, David A. Coates, Craig D. Wolfangel
  • Patent number: 9598405
    Abstract: The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: March 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Kaleen Konrad Childers, Maria Emilia Di Francesco, John Michael Ellis, Andrew M. Haidle, Yuan Liu, Alan B. Northrup, Brendan O'Boyle, Ryan D. Otte, Michael H. Reutershan, Dilrukshi Vitharana, Hyun Chong Woo
  • Patent number: 9518041
    Abstract: Provided is (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione or a salt thereof. Also provided is a drug containing as the active ingredient (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione or a salt thereof.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: December 13, 2016
    Assignee: KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Noriyuki Kamei, Daigo Kamimura, Yoshitake Sumikawa, Shota Tokuoka
  • Patent number: 9499528
    Abstract: Methods for preparing 2,5-Bis(benzoxazol-2?-yl)benzene-1,4-diol derivatives (Zinhbo derivatives) are provided. Zinhbo derivatives are used to detect zinc ions and have particular application in vivo and in vitro. Zinhbo derivatives upon excitation give a florescence response emission that can be used to determine the presence of zinc cation in solution. Zinhbo derivatives complexed with zinc cations upon excitation can produce a florescence response emission in the visible and near infrared range. Zinhbo derivatives complexed with zinc cations exhibit a large stoke shift between the excitation and emission wavelengths.
    Type: Grant
    Filed: April 8, 2014
    Date of Patent: November 22, 2016
    Assignee: The University of Akron
    Inventors: Yi Pang, Junfeng Wang
  • Patent number: 9493488
    Abstract: The present invention is to provide highly solid state emissive fluorophores of the formula 1 and 2 useful for the solid state lighting. The formula 1 and 2 have good solid state emission in blue and green region respectively. The zinc complexes of formula 1A and 2A have yellow and red emission respectively in solid state. The present invention also provide high solid state emissive assay of formula 1 and 2 to convert UV light into visible light by coating the color tunable materials on the 365-nm emitting solid state LED. The present invention further provides carbazole end-capped bipyridine for screening of metal salts with different counterions in solutions. The discrimination of the various metal salts can be monitored by noting the fluorescence change in solution. The zinc salts with different counterions have different emission color in solution. The present invention also develop a new two photon active fluorescent Zn2+ specific probe for detecting Zn2+ in cellular environments.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: November 15, 2016
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ajayaghosh Ayyappanpillai, Divya Kizhumuri, Srinivasan Sampath
  • Patent number: 9428488
    Abstract: To provide an industrially useful method for producing pharmaceutically useful 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, and an intermediate for producing the compound. The method for producing compound represented by formula (1) is represented by the following reaction scheme, and the intermediate is represented by the following formula (4).
    Type: Grant
    Filed: July 24, 2013
    Date of Patent: August 30, 2016
    Assignee: FUJIYAKUHIN CO., LTD.
    Inventors: Yoshiyuki Iwabuchi, Sachiho Miyata, Junichiro Uda, Osamu Nagata
  • Patent number: 9353110
    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: July 17, 2015
    Date of Patent: May 31, 2016
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masaki Takahashi, Takamasa Tanabe, Mai Ito, Yoshihiko Nokura
  • Patent number: 9198420
    Abstract: The present invention relates to norbormide analogs having rodenticidal activity; rodenticidal compositions comprising the analogs; uses of the analogs as rodenticides; uses of the analogs in the manufacture of rodenticidal compositions; and methods for controlling rodents using the compositions.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: December 1, 2015
    Assignee: Landcare Research New Zealand Limited
    Inventors: Brian Hopkins, Margaret Anne Brimble, David Rennison, Sergio Bova, Maurizio Cavalli, Olivia Laita
  • Patent number: 9187426
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: November 17, 2015
    Assignees: Novartis AG, Xenon Pharmaceuticals
    Inventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
  • Patent number: 9172051
    Abstract: Polyphenylene compounds such as compounds represented by Formulas 1-28 may be used in electronic devices such as organic light-emitting devices. For example, the compounds may be used as host material in an emissive layer.
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: October 27, 2015
    Assignee: Nitto Denko Corporation
    Inventors: Shijun Zheng, David T. Sisk, Liping Ma
  • Patent number: 9131694
    Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. Novel pyridine compounds for use in controlling pests are disclosed.
    Type: Grant
    Filed: November 1, 2013
    Date of Patent: September 15, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Noormohamed M. Niyaz, Francis E. Tisdell, Gerald B. Watson, James M. Renga, William C. Lo, Maurice C. H. Yap
  • Patent number: 9051284
    Abstract: Compounds useful in porous films for light extraction and/or light scattering in electronic devices, such as light-emitting devices, are described herein. These compounds may be represented by Formula 1, as described herein.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: June 9, 2015
    Assignee: NITTO DENKO CORPORATION
    Inventors: Shijun Zheng, Jensen Cayas, David T. Sisk
  • Patent number: 9040563
    Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: May 26, 2015
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
    Inventors: Said M. Sebti, Andrew Hamilton
  • Patent number: 9040572
    Abstract: This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method of preparing a benzoimidazole derivative at high purity and high yield, wherein the benzoimidazole derivative is synthesized using a novel intermediate, namely, benzaldehyde, and thereby the preparation process is simple so that it can be applied to production.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: May 26, 2015
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: In Woo Kim, Ji Duck Kim, Hong Chul Yoon, Hee Kyoon Yoon, Byung Goo Lee, Joon Hwan Lee, Young Mook Lim, Soo Jin Choi
  • Publication number: 20150137084
    Abstract: Triptycene derivatives having symmetric or asymmetric substituents are provided. The triptycene derivatives of the present invention may be applied in phosphorescent lighting devices ranging from deep blue to red and may be applied as a host material, an electron transporting material or a hole transporting material. An OLED device is also herein disclosed.
    Type: Application
    Filed: May 19, 2014
    Publication date: May 21, 2015
    Applicant: National Tsing Hua University
    Inventors: Chien-Hong CHENG, Ho-Hsiu CHOU, Cheng-Chang LAI
  • Patent number: 9035096
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 19, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20150133473
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 20, 2013
    Publication date: May 14, 2015
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Joseph E. Drumm III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Patent number: 9029531
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: May 12, 2015
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
  • Publication number: 20150123089
    Abstract: The present application provides a new nitrogen-containing heterocyclic compound and an organic electronic device using the same.
    Type: Application
    Filed: April 12, 2013
    Publication date: May 7, 2015
    Inventors: Dong Hoon Lee, Tae Yoon Park, Sung Kil Hong, Boonjae Jang, Minseung Chun, Dong Sik Kim, Minyoung Kang
  • 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
  • Publication number: 20150126558
    Abstract: To provide crystal polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, which is a useful pharmaceutical, and a production method therefor. Through purification of a corresponding salt, recrystallization, or storage under humidified conditions, three different crystal forms; i.e., crystalline polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile are produced.
    Type: Application
    Filed: July 24, 2013
    Publication date: May 7, 2015
    Applicant: FUJIYAKUHIN CO., LTD.
    Inventors: Yoshiyuki Iwabuchi, Sachiho Miyata, Takahiro Sato, Junichiro Uda, Takamitsu Kandou, Tadashi Inoue, Hiroyuki Nakano
  • Patent number: 9024033
    Abstract: The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical foimulation for the inhibition of malaria parasite proliferation.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: May 5, 2015
    Assignee: MMV Medicines for Malaria Venture
    Inventors: Michael John Witty, David Hardick
  • Publication number: 20150115232
    Abstract: A chrysene-based compound and an organic light-emitting device including the same, the chrysene-based compound being represented by Formula 1, below:
    Type: Application
    Filed: April 17, 2014
    Publication date: April 30, 2015
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Kwang-Hyun KIM, Young-Kook KIM, Eun-Young LEE
  • Publication number: 20150119377
    Abstract: This invention recites substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in animals. The substituents A, B, R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Inventors: Susan M. K. Sheehan, Valerie A. Vaillancourt
  • Publication number: 20150119384
    Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.
    Type: Application
    Filed: January 6, 2015
    Publication date: April 30, 2015
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • 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: 9018382
    Abstract: Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: April 28, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Celine Duquenne, Neil Johnson, Steven D. Knight, Louis LaFrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
  • Publication number: 20150111735
    Abstract: A pesticidal composition comprises a pyridine triazole compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, Z, and x 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: Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse
  • Publication number: 20150111734
    Abstract: A pesticidal composition comprises at least one compounds selected from a compound of formula, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, Q, Z, L, La, and x 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: Yu Zhang, Asako Kubota, Noormohamed M. Niyaz, Thomas Barton, Tony K. Trullinger, Christian T. Lowe, Paul R. LePlae, Ann M. Buysse, Martin J. Walsh, Negar Garizi, Ricky Hunter, Daniel Knueppel
  • Publication number: 20150111866
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.
    Type: Application
    Filed: April 26, 2013
    Publication date: April 23, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
  • Publication number: 20150111018
    Abstract: In some embodiments, the present disclosure pertains to methods of capturing a gas from an environment by associating the environment with a porous carbon material that includes, without limitation, protein-derived porous carbon materials, carbohydrate-derived porous carbon materials, cotton-derived porous carbon materials, fat-derived porous carbon materials, waste-derived porous carbon materials, asphalt-derived porous carbon materials, coal-derived porous carbon materials, coke-derived porous carbon materials, asphaltene-derived porous carbon materials, oil product-derived porous carbon materials, bitumen-derived porous carbon materials, tar-derived porous carbon materials, pitch-derived porous carbon materials, anthracite-derived porous carbon materials, melamine-derived porous carbon materials, and combinations thereof. In some embodiments, the associating results in sorption of gas components (e.g., CO2, H2S, and combinations thereof) to the porous carbon material.
    Type: Application
    Filed: August 13, 2014
    Publication date: April 23, 2015
    Applicant: William Marsh Rice University
    Inventors: James M. Tour, Desmond E. Schipper, Chih-Chau Hwang, Josiah Tour, Almaz S. Jalilov, Gedeng Ruan