Additional Hetero Ring Containing Patents (Class 514/336)
  • Patent number: 10300154
    Abstract: The invention provides cardiovascular imaging agents comprising an anticoagulant (e.g., dabigatran derivatives) with a label (e.g., radiolabeled, fluorinated or radiofluorinated). Methods for using the cardiovascular imaging agents and kits containing the cardiovascular imaging agents or components suitable for production of the cardiovascular imaging agents are also provided.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: May 28, 2019
    Inventor: David R Elmaleh
  • Patent number: 10233175
    Abstract: The present invention relates to novel pyridinium compounds, their isomers, steroisomers, atropisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses process for preparing novel compounds and pharmaceutical composition of said compounds. The invention further relates to the use of the above mentioned compounds for the preparation of medicament for use as pharmaceuticals.
    Type: Grant
    Filed: April 5, 2016
    Date of Patent: March 19, 2019
    Assignee: Torrent Pharmaceuticals Limited
    Inventors: Chaitanya Dutt, Rameshchandra Gupta, Manish Patel, Jaya Abraham, Vivek Mishra, Amit Kesarwani, Shailesh Deshpande, Shital Kumar Zambad, Anoop Mathur, Jignesh Kotecha, Sachin Latad, Anita Chaudhari
  • Patent number: 10214510
    Abstract: The present invention relates to fungicidal N-cycloalkyl-N-(biheterocyclylethylene)carboxamide derivatives and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Grant
    Filed: April 12, 2016
    Date of Patent: February 26, 2019
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Philippe Desbordes, Philippe Rinolfi
  • Patent number: 10214490
    Abstract: This disclosure relates to picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: February 26, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: Zachary A. Buchan, Yu Lu, David M. Jones, Kevin G. Meyer, Chenglin Yao, Brannon Sam, Jeremy Wilmot
  • Patent number: 10173982
    Abstract: This disclosure relates to picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: January 8, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: Zachary A. Buchan, Yu Lu, David M. Jones, Kevin G. Meyer, Chenglin Yao, Brannon Sam, Jeremy Wilmot
  • Patent number: 10172905
    Abstract: The invention relates to methods of treating protein degradation disorders, such cellular proliferative disorders (e.g., cancer) and protein deposition disorders (e.g., neurodegenerative disorders). The invention provides methods and pharmaceutical compositions for treating these diseases using aggresome inhibitors or combinations of aggresome inhibitors and proteasome inhibitors. The invention further relates to methods and pharmaceutical compositions for treating multiple myeloma. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: January 8, 2019
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: Kenneth C. Anderson, James E. Bradner, Edward Franklin Greenberg, Teru Hideshima, Nicholas Paul Kwiatkowski, Ralph Mazitschek, Stuart L. Schreiber, Jared Shaw, Stephen J. Haggarty
  • Patent number: 10150762
    Abstract: The present invention comprises methods of making 5-(2,3-dichloro-4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2-hydroxy-2-methylpropyl)-4-(R1-1-carbonyl)thiazole-2-carboxamide, wherein R1 is defined in the specification.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: December 11, 2018
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven Goldberg, Hariharan Venkatesan, Olaf Kinzel, Christian Gege, Christoph Steeneck, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 10100041
    Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: October 16, 2018
    Assignee: GRÜNENTHAL GMBH
    Inventors: Stefan Schunk, Melanie Reich, René Michael Koenigs
  • Patent number: 10071995
    Abstract: The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
    Type: Grant
    Filed: September 22, 2015
    Date of Patent: September 11, 2018
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Susanne Röhrig, Eloisa Jimenez Núnez, Karl-Heinz Schlemmer, Adrian Tersteegen, Henrik Teller, Alexander Hillisch, Stefan Heitmeier, Martina Victoria Schmidt, Jan Stampfuß
  • Patent number: 10058541
    Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.
    Type: Grant
    Filed: May 25, 2017
    Date of Patent: August 28, 2018
    Assignee: VERSEON CORPORATION
    Inventors: Kevin Michael Short, Son Minh Pham, David Charles Williams, David Ben Kita
  • Patent number: 9981938
    Abstract: Disclosed herein are compounds according to Formulas 1-12, compositions comprising these compounds, and methods of lowering intraocular pressure (IOP) or causing hair growth, and methods of using the same.
    Type: Grant
    Filed: May 12, 2015
    Date of Patent: May 29, 2018
    Assignee: ALLERGAN, INC.
    Inventors: Robert M. Burk, David W. Old, Wha Bin Im, Richard S. Graham, Mu-Lan Lee
  • Patent number: 9974307
    Abstract: The present invention provides a composition for controlling pests having an excellent control efficacy on pests. A composition for controlling pests comprising a compound represented by the formula (1): wherein each of symbols are the same as defined in the Description, or N-oxide thereof; and one or more compounds selected from the group consisting of a group of azole-type compound, a group of strobilurin-type compound, a group of phenylamido-type compound, a group of a compound for controlling rice blast, a group of a compound for controlling sheath blight of rice, and a group of fungicidal compound selected from fludioxonil, ethaboxam, tolclofos-methyl, and captan; shows an excellent controlling efficacy on pests.
    Type: Grant
    Filed: January 30, 2014
    Date of Patent: May 22, 2018
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Chie Shimizu, Masashi Kamezaki, Yoshihiko Nokura
  • Patent number: 9974304
    Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: May 22, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Kyle A. DeKorver, Johnathan E. DeLorbe, Kevin G. Meyer, Chenglin Yao, Ronald J. Heemstra, William H. Dent, III
  • Patent number: 9932335
    Abstract: The present invention relates to compounds of formula wherein R1, Y1, Y2, X, R and n are as defined herein.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: April 3, 2018
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Theresa Maria Ballard, Emmanuel Pinard, Herve Schaffhauser, Katrin Groebke Zbinden, Thomas Ryckmans, Alexander Flohr
  • Patent number: 9889122
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: February 13, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Jorgen Eskildsen, Anette Graven Sams, Ask Puschl
  • Patent number: 9890120
    Abstract: A process for preparing N-[(6-chloropyridin-3-yl)methyl]-2,2-difluoroethan-1-amine of formula (III) wherein 2,2-difluoroethylamine of formula (I) is reacted with a halide of formula (II) in the presence of a hydroxide of an alkali metal or alkaline earth metal.
    Type: Grant
    Filed: March 18, 2015
    Date of Patent: February 13, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Wahed Ahmed Moradi, Guenter Schlegel, Albert Schnatterer
  • Patent number: 9889139
    Abstract: Provided is a method of treating inflammatory bowel disease comprising administering a pharmaceutical composition comprising a 6-aminopyridin-3-ol compound or a pharmaceutically acceptable salt thereof as an active ingredient to a subject, which inhibits colitis in a model of inflammatory bowel disease, and accordingly, they may be suitable for use as a drug for the prevention or treatment of inflammatory bowel disease.
    Type: Grant
    Filed: August 16, 2016
    Date of Patent: February 13, 2018
    Assignee: Research Cooperation Foundation of Yeungnam University
    Inventors: Byeong Seon Jeong, Jung Ae Kim, Dong Guk Kim, You Ra Kang, Tae Gyu Nam
  • Patent number: 9850236
    Abstract: The present invention comprises compounds of Formula I. wherein: X, A1, A2, A3, A4, R1, R2, and R3 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: December 26, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Steven Goldberg, Hariharan Venkatesan, Virginia Tanis, Olaf Kinzel, Christian Gege, Christoph Steeneck, Gerald Kleymann, Thomas Hoffmann, Anne M. Fourie, Xiaohua Xue
  • Patent number: 9795551
    Abstract: A tetrapeptide having antioxidant activity is provided. The tetrapeptide has a structure comprising, in amino acid sequence from N-terminus to C-terminus: tryptophan-X-tyrosine-X; wherein X is arginine, lysine, histidine or any positively-charged amino acid derivative such as 5-hydroxylysine, ornithine, 2,4-diamino-butyrate and 2,3-diamino-propionate. Each amino acid of the sequence or its Homo-amino acid derivative is independently of the D configuration (D-stereoisomer) or of the L configuration (L-stereoisomer), and the C-terminal comprises one selected from the group consisting of carboxyl (—COOH), and carboxamide (—CONH2). A composition stabilized to oxidation or having antioxidant activity and a method for attenuating effects of free radicals on a keratinous material are also provided.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: October 24, 2017
    Assignee: L'OREAL
    Inventors: Jean-Marc Sabatier, Zhi Pan
  • Patent number: 9765093
    Abstract: The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: September 19, 2017
    Assignee: Padlock Therapeutics, Inc.
    Inventors: Rajesh Devraj, Gnanasambandam Kumaravel, Laura Gleave, Adrian Kotey, Thomas Krulle, Cristina Lecci, Heather Tye, Ian Wigginton
  • Patent number: 9573926
    Abstract: The invention provides ester compounds for treating ophthalmic diseases. The esters of the invention are particularly advantageous due to their stability in aqueous solutions.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: February 21, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Robert M. Burk, Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 9549555
    Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: January 24, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Jonathan E. DeLorbe, Kyle A. DeKorver, Kevin G. Meyer, Chenglin Yao, Jeremy Wilmot, Ian O'Callaghan, Ronald J. Heemstra, William H. Dent, III, Rebecca Lyn K. C. LaLonde
  • Patent number: 9474281
    Abstract: To provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the formula (I) or its salt: wherein when A is —N?, B is —CX4?; when A is —CH?, B is —N?; each of X1 and X2 which are independent of each other, is a halogen atom, an alkoxy group, a hydroxyl group, an alkyl group, a CF3 group or an alkylthio group; X3 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; X4 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; R1 is an alkyl group; R2? is an alkoxy group; p is 0, 1 or 2; and each of R2? and R2?? is an alkoxy group, and (b) at least one additional fungicide.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: October 25, 2016
    Assignee: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Munekazu Ogawa, Akihiro Nishimura
  • Patent number: 9458137
    Abstract: The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: October 4, 2016
    Assignee: NantBioScience, Inc.
    Inventors: Chunlin Tao, Qinwei Wang, David Ho, Tulay Polat, Laxman Nallan, Patrick Soon-Shiong
  • Patent number: 9388175
    Abstract: This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(?O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(?O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(?O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkyl
    Type: Grant
    Filed: February 13, 2008
    Date of Patent: July 12, 2016
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Christopher James Grantham, Theodorus Dinklo, Anne Simone Josephine Lesage
  • Patent number: 9376389
    Abstract: A method for preparing a 2,2-difluoroethylamine of the formula (III) in which 2,2-difluoroethylamine of the formula (I) is reacted with a halide of the formula (II) in the presence of a tertiary nitrogen base: where, in the formulae (II) and (III), Hal and A are defined as stated in the description.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: June 28, 2016
    Assignee: Bayer Cropscience AG
    Inventors: Christian Funke, Norbert Lui, Rafael Warsitz, Albert Schnatterer
  • Patent number: 9375000
    Abstract: Arylpyrrolidines of Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite-controlling agents.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: June 28, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jun Mihara, Mamoru Hatazawa, Daiei Yamazaki, Hidetoshi Kishikawa, Kei Domon, Hidekazu Watanabe, Norio Sasaki, Tetsuya Murata, Koichi Araki, Eiichi Shimojo, Teruyuki Ichihara, Tadashi Ishikawa, Katsuhiko Shibuya, Ulrich Görgens, Peter Bruechner, Reiner Fischer, Johannes-Rudolf Jansen, Tobias Kapferer, Simon Maechling, Michael Maue, Arnd Voerste
  • Patent number: 9333196
    Abstract: The invention relates to the use of quaternary pyridinium salts of formula (I), wherein R is NH2, CH3, or N(H)CH2OH group, and X is pharmaceutically acceptable counterion, for the preparation of vasoprotective agent for the treatment or prevention of conditions or diseases associated with dysfunction of vascular endothelium, oxidative stress, and/or insufficient production of endothelial prostacyclin PGI2, in particular but not exclusively if the above coincides with hypercholesterolemia, hypertriglyceridemia or low HDL level.
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: May 10, 2016
    Assignee: Pharmena Spólka Akcyjna (Pharmena S.A.)
    Inventors: Jerzy Gębicki, Stefan Chłopicki
  • Patent number: 9334238
    Abstract: The invention relates to pyridylidene compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted pyridylidene compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted pyridylidene compounds. The N-substituted pyridylidene compounds of the present invention are defined by the following formula I: wherein X, Het, R1, R2, R3, R4 and R6 are defined as in the description.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: May 10, 2016
    Assignee: BASF SE
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Patent number: 9278958
    Abstract: The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: March 8, 2016
    Assignees: Katholieke Universiteit Leuven K.U. Leuven R&D, Universita Degli Studi Di Ferrara
    Inventors: Jan Balzarini, Wim Dehaen, Joice Thomas, Sandra Liekens, Romeo Romagnoli, Pier Giovanni Baraldi
  • Patent number: 9271501
    Abstract: The present invention relates to the use of strobilurine type compounds of formula I and the N-oxides and the salts thereof for combating phytopathogenic fungi containing a mutation in the mitochondrial cytochrome b gene conferring resistance to Qo inhibitors, and to methods for combating such fungi. The invention also relates to novel compounds, processes for preparing these compounds, to compositions comprising at least one such compound, to plant health applications, and to seeds coated with at least one such compound.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: March 1, 2016
    Assignee: BASF SE
    Inventors: Joachim Rheinheimer, Violeta Terteryan, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Sebastian Georgios Rohrer, Wassilios Grammenos, Christian Pilger, Franz Roehl, Markus Gewehr, Gerd Stammler, Jurith Montag, Hubert Sauter
  • Patent number: 9265253
    Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: February 23, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Fangzheng Li, Kevin G. Meyer, James M. Renga, Chenglin Yao, Jeremy Wilmot, Jessica Herrick, Karla Bravo-Altamirano, Timothy Boebel
  • Patent number: 9220265
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 5, 2014
    Date of Patent: December 29, 2015
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
  • Patent number: 9156856
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: October 13, 2015
    Assignee: AbbVie Inc.
    Inventors: Aaron R. Kunzer, Steven W. Elmore, Laura A. Hexamer, Cheol-Min Park, Andrew J. Souers, Gerard M Sullivan, Gary T. Wang, Xilu Wang, Michael D. Wendt
  • Patent number: 9150542
    Abstract: The present invention relates to a process for the preparation of crystalline Form I of methanesulfonate salt of dabigatran etexilate. (Formula (I)). The present invention does not require the isolation of the dabigatran etexilate intermediate.
    Type: Grant
    Filed: September 2, 2013
    Date of Patent: October 6, 2015
    Assignee: RANBAXY LABORATORIES LIMITED
    Inventors: Sudhir Singh Sanwal, Anandam Vempali, Balaguru Murugesan, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
  • Patent number: 9089135
    Abstract: The present invention relates to novel active ingredient combinations which consist of fluopyram and further known active insecticidal ingredients, and are very suitable for controlling animal pests, such as insects and/or unwanted acarids and/or nematodes, in foliar and soil application and/or in seed treatment.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: July 28, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Wolfram Andersch, Heike Hungenberg, Heiko Rieck
  • Patent number: 9090584
    Abstract: The invention provides well-defined amides for treating glaucoma and ocular hypertension.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: July 28, 2015
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Todd Gac
  • 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: 20150133503
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating tuberculosis, comprising: (a) a pharmaceutically effective amount of a compound represented by the following chemical formula 1; and (b) a pharmaceutically acceptable carrier. Chemical formula 1 The compound contained as an active ingredient of the present invention inhibits the expression and activity of CO-DH in tubercle bacillus so as to effectively block the detoxification of carbon monoxide, which is an important survival factor of tubercle bacillus, and is safe for the human body since the compound targets CO-DH which does not exist in the human body. In addition, the compound creates a synergistic effect when combined with a conventional tuberculostatic drug, and thus can be more effective for treating tuberculosis.
    Type: Application
    Filed: February 13, 2013
    Publication date: May 14, 2015
    Inventors: Young Min Kim, Seung Jung Han, Tae Gwon Oh, Sae Woong Park, Sang Nae Cho, Mi Young Hahn, Jee Hee Suh, Kyu Yang Yi
  • Publication number: 20150126490
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
  • Publication number: 20150126559
    Abstract: The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 7, 2015
    Applicant: UNIVERSITA DEGLI STUDI DI FERRARA
    Inventors: Jan Balzarini, Wim Dehaen, Joice Thomas, Sandra Liekens, Romeo Romagnoli, Pier Giovanni Baraldi
  • Patent number: 9023870
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: May 5, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Anette Graven Sams, Jørgen Eskildsen, Ask Puschl
  • Publication number: 20150119397
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: January 8, 2015
    Publication date: April 30, 2015
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150111741
    Abstract: A pesticidal composition comprises a synergistically effective amount of a nicotinic acetylcholine receptor (nAChR) agonist compound and a pesticide selected from N-(3-chloro-1-(pyridin-3-yl)-1H-pyrazol-4-yl)-N-ethyl-3-((3,3,3-trifluoropropyl)thio)propanamide (I), N-(3-chloro-1-(pyridin-3-yl)-1H-pyrazol-4-yl)-N-ethyl-3-((3,3,3-trifluoropropyl)sulfinyl)propanamide (II), or any agriculturally acceptable salt thereof. A method of controlling pests comprises applying the pesticidal composition near a population of pests. A method of protecting a plant from infestation and attack by insects comprises contacting the plant with the synergistic pesticidal composition.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Luis E. Gomez, Mike Shaw, Tony K. Trullinger, Ricky Hunter, John Herbert, Mary E. Kubiszak
  • Patent number: 9012360
    Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: April 21, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Peter Jeschke, Robert Velten, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 9012651
    Abstract: Disclosed herein are modulators of TRPV3 of formula (I) wherein X1, X2, R1, R2, Rx, and n are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: April 21, 2015
    Assignee: AbbVie Inc.
    Inventors: Bruce Clapham, Phil B. Cox, Michael J. Dart, Arthur Gomtsyan, Tammie K. Jinkerson, Ryan G. Keddy, Michael E. Kort, Philip R. Kym, Mark Matulenko, Robert G. Schmidt, Clara I. Villamil, Eric A. Voight, Kevin R. Woller
  • Publication number: 20150105429
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 9006269
    Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: April 14, 2015
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias