1,3-thiazole Ring Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/270.4)
  • Patent number: 10059670
    Abstract: Provided herein are processes and intermediate compounds useful for the preparation of 2-carboxamide cycloamino urea derivatives, and useful intermediates therefore.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: August 28, 2018
    Assignee: Novartis AG
    Inventors: Bernhard Erb, Isabelle Sylvie Gallou, Florian Karl Kleinbeck-Riniker
  • Patent number: 9445597
    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: Grant
    Filed: October 17, 2014
    Date of Patent: September 20, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Negar Garizi, Martin J. Walsh, Ann M. Buysse, Daniel Knueppel, Asako Kubota, Noormohamed M. Niyaz, Yu Zhang, Ricky Hunter, Tony K. Trullinger
  • Patent number: 9428487
    Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to use thereof for controlling animal pests, in particular arthropods and especially insects.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: August 30, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Bretschneider, Eva-Maria Franken, Ulrich Görgens, Martin Fusslein, Achim Hense, Joachim Kluth
  • Patent number: 9357780
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Grant
    Filed: August 8, 2014
    Date of Patent: June 7, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl DeAmicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra Lee McLeod, Ronald Ross, Jr., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
  • Patent number: 9198428
    Abstract: The invention disclosed in this document is related to the field of processes to produce certain 2-(pyridine-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazole amides.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: December 1, 2015
    Assignee: Dow AgroSciences, LLC.
    Inventors: Ronald Ross, Jr., Carl DeAmicis, Yuanming Zhu, Noormohamed M. Niyaz, Kim E. Arndt, Scott P. West, Gary Roth
  • Patent number: 9169239
    Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of Formulae (1), (3) or (4) of this process.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: October 27, 2015
    Assignee: Sandoz AG
    Inventors: Peter Kremminger, Hubert Sturm
  • Patent number: 9145404
    Abstract: The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a power X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 2; (2) an anhydrous tetomilast type A crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 4; (3) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 8; (4) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIGS. 10; and (5) a mixture consisting of the above anhydrous tetomilast type A crystal and an anhydrous tetomilast type B crystal.
    Type: Grant
    Filed: December 31, 2013
    Date of Patent: September 29, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Satoshi Aoki, Kenji Nakaya, Masahiro Sota, Masashi Ishigami
  • Patent number: 9108952
    Abstract: The invention disclosed in this document is related to the field of processes to produce certain 2-(pyridine-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazole amides.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: August 18, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Ronald Ross, Jr., Carl DeAmicis, Yuanming Zhu, Noormohamed M. Niyaz, Kim E. Arndt, Scott P. West, Gary Roth
  • Patent number: 9034871
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: May 19, 2015
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • Publication number: 20150126485
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • 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: 20150111730
    Abstract: A pesticidal composition comprises a compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R4, R5, R6, R7, Z, Q, and Y are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests, or to an area to control pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Noormohamed M. Niyaz, Ann M. Buysse, David A. Demeter, Negar Garizi, Ricky Hunter, Daniel Knueppel, Paul R. LePlae, Christian T. Lowe, Akshay Patny, Tony K. Trullinger, Martin J. Walsh, Yu Zhang
  • Patent number: 9006270
    Abstract: The present invention relates to specific solid forms of (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-(4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl)-amide, and its solvates. The present invention further relates to processes for preparing said solid forms, pharmaceutical compositions comprising said solid forms, and methods of using said solid forms and pharmaceutical compositions to treat disease.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Isabelle Sylvie Gallou, Cornelius Gauer, Frank Stowasser
  • Patent number: 9006446
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: April 14, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl Deamicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra Lee McLeod, Ronald Ross, Jr., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
  • Patent number: 8993769
    Abstract: The invention disclosed in this document is related to the field of processes to produce certain 2-(pyridine-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazole amides.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: March 31, 2015
    Assignee: Dow AgroSciences, LLC.
    Inventors: Ronald Ross, Jr., Carl DeAmicis, Yuanming Zhu
  • Patent number: 8993601
    Abstract: The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a power X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 2; (2) an anhydrous tetomilast type A crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 4; (3) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 8; (4) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. 10; and (5) a mixture consisting of the above anhydrous tetomilast type A crystal and an anhydrous tetomilast type B crystal.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: March 31, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Satoshi Aoki, Kenji Nakaya, Masahiro Sota, Masashi Ishigami
  • Publication number: 20150087639
    Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
    Type: Application
    Filed: July 18, 2013
    Publication date: March 26, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
  • Patent number: 8987312
    Abstract: The invention provides a series of -?ketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof.
    Type: Grant
    Filed: July 8, 2009
    Date of Patent: March 24, 2015
    Assignee: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Publication number: 20150073138
    Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to a intermediates of this process.
    Type: Application
    Filed: September 7, 2012
    Publication date: March 12, 2015
    Applicant: Sandoz AG
    Inventors: Peter Kremminger, Hubert Sturm
  • Publication number: 20150065519
    Abstract: This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Inventors: Sarvajit Chakravarty, Roopa Rai, Son Minh Pham, Brahmam Pujala, Ramniwas Jangir, Rambabu Guguloth, Vijay Kumar Sharma
  • Patent number: 8969573
    Abstract: Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: March 3, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Michael Chorev, Bertal Huseyin Aktas, Jose A. Halperin, Gerhard Wagner
  • Publication number: 20150051177
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Inventor: Darren Orton
  • Publication number: 20150045394
    Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Inventors: Andreas Kling, Helmut Mack, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150045353
    Abstract: In accordance with the present invention, there are provided formulations of gamma secretase modulators (GSMs) which are suitable for oral delivery and have improved transport properties relative to prior art formulations thereof. Also provided are methods for the preparation of such improved formulations and uses thereof for the delivery of GSMs to subjects in need thereof.
    Type: Application
    Filed: August 9, 2013
    Publication date: February 12, 2015
    Applicant: Neurogenetic Pharmaceuticals, Inc.
    Inventors: William T. COMER, Maria Z. KOUNNAS, Bryan M. KNOX, Nathan S. BARKSDALE
  • Publication number: 20150045218
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl DeAmicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra L. McLeod, Ronald Ross, JR., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
  • Patent number: 8940771
    Abstract: The present invention relates to compounds of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: January 27, 2015
    Assignee: Novartis AG
    Inventors: Giorgio Caravatti, Robin Alec Fairhurst, Pascal Furet, Vito Guagnano, Patricia Imbach
  • Publication number: 20140364460
    Abstract: Fatostatin, a recently described inhibitor of SREBP activation, significantly reduces the level of mutant p53 binding to the HMG-CoA reductase gene promoter. Further, fatostatin treatment had a dramatic effect on normalizing the abnormal 3D morphology of 3 strains of breast cancer cells: MDA-468 cells, MDA-231 cells, and SKBR3 cells. The results show a functional interaction with SREBPs as being critical for mutant p53-mediated upregulation of the mevalonate pathway genes. At a clinical level, inhibition of the mevalonate pathway, either alone or in combination with other therapies, offers a novel, safe and much needed therapeutic option for tumors bearing mutant p53.
    Type: Application
    Filed: January 18, 2013
    Publication date: December 11, 2014
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: William Allen Freed-Pastor, Carol Prives, Timothy Osborne
  • Publication number: 20140357670
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Application
    Filed: May 28, 2014
    Publication date: December 4, 2014
    Inventors: Saleem Ahmad, Lidet A. Negash
  • Publication number: 20140336186
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Application
    Filed: July 9, 2014
    Publication date: November 13, 2014
    Inventors: Thomas BRETSCHNEIDER, Eva-Maria FRANKEN, Ulrich GÖRGENS, Martin FÜSSLEIN, Achim HENSE, Joachim KLUTH, Hans-Georg SCHWARZ, Adeline KÖHLER, Olga MALSAM, Arnd VOERSTE, Angela BECKER
  • Patent number: 8871944
    Abstract: An object is to provide a thiazole derivative produced from easily available raw materials by a simplified production process. Provided are a process for producing a novel thiazole derivative represented by the general formula (I), which is characterized by adding a strong base to a thioamide represented by the general formula (II) and reacting the mixture with a thioformamide represented by the general formula (III), and a novel thiazole derivative.
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: October 28, 2014
    Assignee: Gifu University
    Inventor: Toshiaki Murai
  • Publication number: 20140309237
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Patent number: 8853246
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: October 7, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl Deamicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra Lee McLeod, Ronald Ross, Jr., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
  • Publication number: 20140296064
    Abstract: The present invention relates to pesticidal methods for the use and application of substituted 3-pyridyl thiazole compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to insecticidal substituted 3-pyridyl thiazole compounds or of the compositions comprising such compounds for combating invertebrate pests and uses thereof. The substituted 3-pyridyl thiazole compounds of the present invention are defined by the following general formula (I): wherein R1, R2 A and m are defined as in the description.
    Type: Application
    Filed: July 13, 2012
    Publication date: October 2, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Gemma Veitch, Arun Narine, Joachim Dickhaut, Karsten Körber, Prashant Deshmukh, Nina Gertrud Bandur
  • Publication number: 20140275033
    Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
  • Publication number: 20140275178
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
  • Publication number: 20140249154
    Abstract: Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Inventors: Andrea Cuconati, Xiaodong Xu, Timothy M. Block
  • Publication number: 20140249024
    Abstract: The present invention relates to pesticidal methods for the use and application of substituted 3-pyridyl thiazole compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to insecticidal substituted 3-pyridyl thiazole compounds or of the compositions comprising such compounds for combating invertebrate pests and uses thereof. The substituted 3-pyridyl thiazole compounds of the present invention are defined by the following general formula (I): wherein R1, R2 A and m are defined as in the description.
    Type: Application
    Filed: July 13, 2012
    Publication date: September 4, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Gemma Veitch, Arun Narine, Joachim Dickhaut, Karsten Körber, Prashant Deshmukh, Nina Gertrud Bandur
  • Publication number: 20140242099
    Abstract: The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: August 28, 2014
    Inventors: Shoujun Chen, Junyi Zhang, Jun Jiang, Teresa Kowalczyk-Przewloka, Zhiqiang Xia, Shijie Zhang
  • Publication number: 20140235852
    Abstract: The present invention relates to an improved process for preparing (2R,3aR,10Z,11aS,2aR,14aR)-cyclopenta[c]cyc-lopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxylic acid, 2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2[[7-methoxy-8-methyl-2-[4-10 (1-methylethyl)-2-thiazolyl]-4-quinolinyl]oxy]-5-methyl-4,14-dioxo-, ethyl ester. This compound is an intermediate in the overall synthesis route of the macrocyclic compound TMC 435. TMC 435 is an inhibitor of NS3/4A protease which plays an important role in the replication of the hepatitis C virus.
    Type: Application
    Filed: October 26, 2012
    Publication date: August 21, 2014
    Applicant: Janssen Pharmaceuticals, Inc.
    Inventors: Andras Horvath, Stijn Wuyts, Dominique Paul Michel Depré, Wouter Louis J. Couck, Jozef Ludo Jan Cuypers, Syuzanna Harutyunyan, Gregory Fabien Sebastian Binot
  • Publication number: 20140235637
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: InterMune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Publication number: 20140221374
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinase mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.
    Type: Application
    Filed: March 16, 2012
    Publication date: August 7, 2014
    Applicant: Ruga Corporation
    Inventors: Jean-Michel Vernier, Stephanie Hopkins, Pierre-Yves Bounaud, Patrick O'Connor, David Matthews, Steve Bender
  • Patent number: 8790855
    Abstract: The present invention provides a charge control agent containing, as an active substance(s), one or two or more thiazolidinedione derivatives represented by the following formula (1), where R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc.; R3 to R7, which may be identical to or different from each other, represent a hydrogen atom, a chlorine atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc., and may be joined to each other to form a ring; and V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and 0 to 3 of any of V, W, X, Y and Z are nitrogen atoms which do not have the substituents of R3 to R7.
    Type: Grant
    Filed: September 1, 2011
    Date of Patent: July 29, 2014
    Assignee: Hodogaya Chemical Co., Ltd
    Inventors: Ikuo Kimura, Motonori Tsuji, Masami Ito, Masaya Tojo, Kanae Hiraishi
  • Patent number: 8785468
    Abstract: Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: July 22, 2014
    Assignee: Amgen Inc.
    Inventors: Xiaohui Du, Zice Fu, Jonathan B. Houze, XianYun Jiao, Yong-Jae Kim, Leping Li, Jinqian Liu, Mike Elias Lizarzaburu, Julio C. Medina, Wang Shen, Simon Turcotte, Ming Yu
  • Patent number: 8778976
    Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: July 15, 2014
    Assignee: Baylor College of Medicine
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Qian Mao, Shinji Kamisuki, Akira Kugimiya
  • Publication number: 20140187780
    Abstract: The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
    Type: Application
    Filed: December 24, 2013
    Publication date: July 3, 2014
    Applicant: Enanta Pharmaceuticals, Inc.
    Inventors: In Jong Kim, Tongzhu Liu, Jiang Long, Guoqiang Wang, Yao-Ling Qiu, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
  • Publication number: 20140179648
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: Shuang Liu, Bryan Cordell Duffy, John Frederick Quinn, May Xiaowu Jiang, Ruifang Wang, Gregory Scott Martin, He Zhao, Bruce Francis Molino, Peter Ronald Young
  • Publication number: 20140171470
    Abstract: The present invention relates to specific solid forms of (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-(4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl)-amide, and its solvates. The present invention further relates to processes for preparing said solid forms, pharmaceutical compositions comprising said solid forms, and methods of using said solid forms and pharmaceutical compositions to treat disease.
    Type: Application
    Filed: June 19, 2012
    Publication date: June 19, 2014
    Inventors: Isabelle Slyvie Gallou, Cornelius Gauer, Frank Stowasser
  • Publication number: 20140148471
    Abstract: The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests, which include arthropods and especially insects, and to processes for preparing the novel compounds.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Reiner FISCHER, Martin FÜßLEIN, Peter JESCHKE, Adeline KÖHLER, Joachim KLUTH, Friedrich August MÜHLTHAU, Yoshitaka SATO, Arnd VOERSTE, Eiichi SHIMOJO
  • Publication number: 20140148457
    Abstract: Compounds of the formula I in which R, R1, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: April 12, 2012
    Publication date: May 29, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Srinivasa R. Karra, Wolfgang Staehle, Eike Staub, Margarita Wucherer-Plietker
  • Patent number: 8735595
    Abstract: The present invention relates to compounds of formula (I) which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: May 27, 2014
    Assignee: AbbVie Inc.
    Inventors: Yu Gui Gu, Xiangdong Xu, Moshe Weitzberg, Hing L. Sham