Patents Issued in January 29, 2019
  • Substituted N,2-diarylquinoline-4-carboxamides and the use thereof as anti-inflammatory agents
    Patent number: 10189788
    Abstract: The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.
    Type: Grant
    Filed: September 7, 2015
    Date of Patent: January 29, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Hartmut Beck, Tobias Thaler, Raimund Kast, Daniel Meibom, Mark Meininghaus, Carsten Terjung, Martina Delbeck, Klemens Lustig, Uwe Muenster, Britta Olenik
  • Process for the preparation of androgen receptor antagonists and intermediates thereof
    Patent number: 10189789
    Abstract: The present invention relates to an improved process for the preparation of carboxamide structured androgen receptor (AR) antagonists such as N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (1A) and key intermediates thereof such as 2-chloro-4-(1H-pyrazol-3-yl)benzonitrile (V). AR antagonists are useful in the treatment of cancer, particularly prostate cancer and other diseases where AR antagonism is desired.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: January 29, 2019
    Assignee: Orion Corporation
    Inventors: Ilpo Laitinen, Oskari Karjalainen
  • Imidazoline compound, mobility control system, plugging agent for gas channeling, and method for carbon dioxide flooding
    Patent number: 10189790
    Abstract: An imidazoline compound, a mobility control system, a plugging agent for gas channeling, and a method for carbon dioxide flooding. The structure of the imidazoline compound is represented by formula (1), in which R is pentadecyl, heptadecenyl, or heptadecyl. A mobility control system that contains the imidazoline compound can interact with carbon dioxide to form a plugging agent for gas channeling, and thereby attains a plugging effect for carbon dioxide channeling in a carbon dioxide flooding process.
    Type: Grant
    Filed: July 6, 2018
    Date of Patent: January 29, 2019
    Assignees: China University of Geosciences (Beijing), China University of Petroleum(East China)
    Inventors: Qing You, Caili Dai, Yan Zhang, Yifei Liu, Jichao Fang, Huan Wang
  • Pyridyl analogs of 1-(2-cyano-3,12-dioxooleana-1,9(11)dien-28-oyl) imidazole
    Patent number: 10189791
    Abstract: Pyridyl analogs of 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole and pharmaceutical compositions containing the same are provided.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: January 29, 2019
    Assignee: Trustees of Dartmouth College
    Inventors: Michael B. Sporn, Gordon W. Gribble
  • Method and apparatus for synthesizing a water-soluble hexaaryl biimidazole
    Patent number: 10189792
    Abstract: A method for forming a water-soluble hexaaryl biimidazole, comprising the steps of reacting benzil with a carboxy benzaldehyde and ammonium acetate to yield a carboxy triaryl imidazole, and dimerizing the carboxy triaryl imidazole in an alkaline aqueous solution of potassium ferricyanide to yield a water-soluble salt of a bicarboxy hexaaryl biimidazole.
    Type: Grant
    Filed: March 8, 2017
    Date of Patent: January 29, 2019
    Inventor: Stephen L Finson
  • Method for preparing azoxystrobin
    Patent number: 10189793
    Abstract: The present invention provides a process for preparing azoxystrobin, which is performed by reacting 2-cyanophenol or a salt thereof with a compound represented by formula I under the catalysis of a trimethylamine catalyst to obtain the azoxystrobin represented by formula II, which allows the yield of the product azoxystrobin to reach 98% or more, the yield of separated product to reach 95% or more and the post-processing to be simple. The trimethylamine catalyst can be recycled and reused in synthesizing the target product azoxystrobin, which not only reduces the cost but also reduces the total nitrogen and COD in wastewater. The advantages regarding of cost and environmental protection of the method according to the present invention are significant and thus the method is suitable for industrial production.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: January 29, 2019
    Assignee: CAC NANTONG CHEMICAL CO., LTD
    Inventors: Binglian Yang, Haishui Wang, Simian Xie, Xiaohong Tian, Jiwang Xu
  • Heteroaryl compounds and uses thereof
    Patent number: 10189794
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: January 29, 2019
    Assignees: Celgene CAR LLC, Sanofi
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
  • Aryl amine substituted quinoxaline used as anticancer drugs
    Patent number: 10189795
    Abstract: The present invention provides new compounds of formula I(a)-I(d) and II, The compounds can inhibit cancerous inhibitor of protein phosphate 2A (CIP2A), can be used as protein phosphate 2A (PP2A) accelerator and oncoprotein SET antagonist, and can treat cancers effectively.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: January 29, 2019
    Inventors: Kuen-Feng Chen, Chung-Wai Shiau
  • [4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or salt thereof
    Patent number: 10189796
    Abstract: The present invention relates to a novel [4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or a salt thereof. The compound or a salt thereof of the present invention has a glucocorticoid receptor agonist activity, and is useful as a medicine, in particular as a prophylactic or therapeutic agent for the glucocorticoid receptor related disease.
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: January 29, 2019
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Kenji Kawashima, Yusuke Yamazaki, Shinji Takaoka, Daisuke Shii, Tomoko Oda, Takahiro Matsuyama
  • Chemical modulators of immune checkpoints and therapeutic use
    Patent number: 10189797
    Abstract: Compounds and pharmaceutical compositions that down-regulate immune checkpoints such as PD-1, PD-L1 and CTLA-4 are provided. Also provided are methods of treating a disease by down-regulating immune checkpoints such as PD-1, PD-L1 and CTLA-4. The methods are useful for treating cancer and viral infection in a subject.
    Type: Grant
    Filed: December 30, 2016
    Date of Patent: January 29, 2019
    Assignee: Duke University
    Inventors: Wei Chen, Herbert Kim Lyerly, Xiu-rong Ren, Jiangbo Wang, Hongtao Guo, Amy Hobeika, Robert A. Mook
  • Antimicrobial compounds, methods of making the same and articles comprising them
    Patent number: 10189798
    Abstract: The present disclosure pertains to antimicrobial compounds that include silver (Ag) and an s-triazine ring with substitutions at nitrogen or carbon atoms of the s-triazine ring. In one example, the antimicrobial silver s-triazine may be readily incorporated in a variety of compositions and devices in both medical and non-medical settings. In another example, the said compounds may possess broad spectrum antimicrobial activity against bacteria, viruses, fungi and other microbes.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: January 29, 2019
    Assignee: MEDICAL TECHNOLOGY RESEARCH INC
    Inventor: Bhalchandra M. Karandikar
  • Process for preparing substituted phenylisoxazoline derivatives
    Patent number: 10189799
    Abstract: The present invention relates to a process for preparing substituted phenylisoxazoline derivatives.
    Type: Grant
    Filed: February 29, 2016
    Date of Patent: January 29, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Christian Funke, Jens Dietmar Heinrich, Sergii Pazenok, Norbert Lui
  • Method for preparing N-(1,3,4-oxadiazol-2-yl)arylcarboxamides
    Patent number: 10189800
    Abstract: A method for preparing N-(1,3,4-oxadiazol-2-yl)arylcarboxamides of formula (I) is described. The substituents therein are radicals such as hydrogen, alkyl, haloalkyl or aryl.
    Type: Grant
    Filed: September 23, 2016
    Date of Patent: January 29, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Christian Funke, Arnd Neeff, Sergii Pazenok, Norbert Lui
  • Method for synthesizing tetrahydroisoquinoline thiazolidine
    Patent number: 10189801
    Abstract: The present invention relates to a method for synthesizing tetrahydroisoquinoline thiazolidine, which can be conducted under a relatively mild reaction condition and can rapidly synthesize tetrahydroisoquinoline thiazolidine.
    Type: Grant
    Filed: February 20, 2018
    Date of Patent: January 29, 2019
    Assignee: NATIONAL CHI NAN UNIVERSITY
    Inventors: Te-Fang Yang, Sheng-Han Huang, Yan-Liang Lin, Yu-Wei Shih, Yi-Pang Chiu
  • Aminoalcohol lipidoids and uses thereof
    Patent number: 10189802
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: January 29, 2019
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions
    Patent number: 10189803
    Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
    Type: Grant
    Filed: September 20, 2016
    Date of Patent: January 29, 2019
    Assignee: ILLINOIS INSTITUTE OF TECHNOLOGY
    Inventor: Hyun-Soon Chong
  • Method for producing dicarboxylic acid compound
    Patent number: 10189804
    Abstract: It is an object of the present invention to provide an excellent method for producing an excellent therapeutic agent. The solution of the present invention is as shown in the following scheme: wherein R1 represents a C1-C6 alkyl group, R2 represents a C1-C6 alkyl group, and R3 represents a C1-C6 alkyl group.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: January 29, 2019
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Masayuki Murakami, Yuichi Aki, Daisuke Fukatsu, Kenichi Kimura, Makoto Michida, Koji Hamaoka
  • Metabolism probes for therapy and diagnosis
    Patent number: 10189805
    Abstract: Novel 2-substituted glutamylanides useful as modulators of ASCT2 inhibitors. Compounds of the present invention can be used to treat patients suffering from diseases caused or influenced by abnormal ASCT2 transporter dysfunction.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: January 29, 2019
    Assignee: Vanderbilt University
    Inventors: H. Charles Manning, Michael Schulte
  • Fiber conduit apparatus for conducting chemical reactions and chemical extractions
    Patent number: 10189806
    Abstract: A fiber reaction process whereby reactive components contained in immiscible streams are brought into contact to effect chemical reactions and separations. The conduit reactor utilized contains wettable fibers onto which one stream is substantially constrained and a second stream is flowed over to continuously create a new interface there between to efficiently bring about contact of the reactive species and thus promote reactions thereof or extractions thereby. Co-solvents and phase transfer catalysts may be employed to facilitate the process.
    Type: Grant
    Filed: October 7, 2015
    Date of Patent: January 29, 2019
    Assignee: Chemtor, LP.
    Inventor: John Lee Massingill
  • Tetrahydrothiophene-based GABA aminotransferase inactivators
    Patent number: 10189807
    Abstract: Tetrahydrothiophene and related heterocyclic analogs and related methods for GABA aminotransferase inactivation.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: January 29, 2019
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Hoang V. Le, Dustin D. Hawker
  • Solid forms of 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide, and their pharmaceutical compositions and uses
    Patent number: 10189808
    Abstract: Solid forms comprising 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: January 29, 2019
    Assignee: Celgene Corporation
    Inventors: Paul F. Fernandez, Antonio C. Ferretti, Mohit A. Kothare, Ying Li, Hon-Wah Man, Weihong Zhang
  • SGC stimulators
    Patent number: 10189809
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: January 29, 2019
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R. Iyengar, Ara Mermerian, Angelika Fretzen
  • Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
    Patent number: 10189810
    Abstract: There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. 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 serine proteases, including thrombin and various kallikreins.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: January 29, 2019
    Assignee: VERSEON CORPORATION
    Inventors: Kevin Michael Short, David Ben Kita, Maria de los Angeles Estiarte-Martinez, Son Minh Pham
  • Method for preparing the anhydrous crystalline form of isoniazid-derived hydrazone, thus produced cristalline polymorph of the anhydrous form, use thereof for the treatment of Alzheimer's disease, parkinsonism and other neurodegenerative disorders, and pharmaceutical composition
    Patent number: 10189811
    Abstract: The present invention relates to the method for preparing the anhydrous crystalline form of isoniazid-derived hydrazone (8-hydroxyquinoline-2-carboxaldehyde isonicotinoyl hydrazone), to the thus produced polymorph and to the use thereof for the treatment of Alzheimer's disease and parkinsonism, inter alia, and to a pharmaceutical composition.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: January 29, 2019
    Assignee: FACULDADES CATÓLICAS, Associação sem fins Lucrativos
    Inventors: Nicolás Adrián Rey, Leonardo Viana de Freitas
  • Bi-benzyl isoquinoline derivative, preparation method and use thereof in hepatopathy treatment and prevention
    Patent number: 10189812
    Abstract: The invention disclosed a compound of general formula (I), a single stereoisomer thereof, a mixture of stereoisomers thereof, and a prodrug, pharmaceutically acceptable salt and metabolite thereof, X1, X2, X3, X4, R1, R2, x, y and z being as defined in the present invention.
    Type: Grant
    Filed: June 29, 2015
    Date of Patent: January 29, 2019
    Assignees: THE KEY LABORATORY OF CHEMISTRY FOR NATURAL PRODUC, VERSITECH LIMITED
    Inventors: Weidong Pan, Yibin Feng, Yazhou Liu, Ning Wang, Lan Huang, Guangyi Liang, Maosheng Zhang, Tianlei Li, Huayong Lou, Zhanxing Hu, Sheng Liu, Peixue Cao, Jinghua Ruan, Junjie Lan, Chao Chen
  • Formylated N-heterocyclic derivatives as FGFR4 inhibitors
    Patent number: 10189813
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: January 29, 2019
    Assignee: NOVARTIS AG
    Inventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knoepfel, Catherine Leblanc, Robert Mah
  • Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
    Patent number: 10189814
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: January 29, 2019
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, Roger Shen-Chu Chen, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Weihong Zhang
  • 2-(3-pyridinyl)-1H-benzimidazole derivative compound and medicine containing same
    Patent number: 10189815
    Abstract: Provided is a compound represented by general formula (1) or a salt thereof as well as a medicine containing the compound or the salt. In the formula, R1, R2, R3, R4, R5, X1, X2, and X3 are defined.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: January 29, 2019
    Assignees: NIHON MEDI-PHYSICS CO., LTD., KYOTO UNIVERSITY, NATIONAL HOSPITAL ORGANIZATION
    Inventors: Akihiro Izawa, Kei Akama, Yuki Okumura, Yurie Fukui, Nobuya Kobashi, Tsutomu Abe, Yoshihiro Doi, Miho Ikenaga, Hideo Saji, Hiroyuki Kimura, Mitsuhide Naruse
  • Substituted pyridines as inhibitors of human immunodeficiency virus replication
    Patent number: 10189816
    Abstract: Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: January 29, 2019
    Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITED
    Inventors: Kyle J. Eastman, John F. Kadow, Kyle E. Parcella, B. Narasimhulu Naidu, Tao Wang, Zhiwei Yin, Zhongxing Zhang
  • Inhibitors of Bruton's tyrosine kinase
    Patent number: 10189817
    Abstract: The present invention provides a compound, solid forms, and compositions thereof, which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same. The present invention also provides methods of making provided compound and solid forms.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: January 29, 2019
    Assignee: BIOGEN MA INC.
    Inventors: Brian T. Hopkins, Xiongwei Cai, Timothy R. Chan, Patrick Conlon, Michael Humora, Tracy J. Jenkins, J. Michael Macphee, Xianglin Shi, Ross A. Miller, Andrew Thompson
  • 5-(5-(2-(3-aminopropdoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitfile (S)-lactate monohydrate
    Patent number: 10189818
    Abstract: The disclosure herein includes 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile (S)-lactate monohydrate that inhibits Chk1/2 and is useful in the treatment of cancer.
    Type: Grant
    Filed: December 1, 2016
    Date of Patent: January 29, 2019
    Assignee: Eli Lilly and Company
    Inventor: Alessandra B. Ennett-Shepard
  • Factor IXa inhibitors
    Patent number: 10189819
    Abstract: The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: January 29, 2019
    Assignees: Merck Sharp & Dohme, Corp., Mochida Paraceuticals Co., Ltd.
    Inventors: Ting Zhang, Yi-Heng Chen, Liangqin Guo, Alan Hruza, Tianying Jian, Bing Li, Dongfang Meng, Dann L. Parker, Edward C. Sherer, Harold B. Wood, Isao Sakurada
  • Heterocyclic amides useful as protein modulators
    Patent number: 10189820
    Abstract: Disclosed are compounds having the formula: wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: January 29, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: John F. Mehlmann, Joseph J. Romano
  • Fused 1,4-dihydrodioxin derivatives as inhibitors of heat shock transcription factor I
    Patent number: 10189821
    Abstract: The present invention relates to compounds of formula I as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: October 24, 2016
    Date of Patent: January 29, 2019
    Assignee: Cancer Research Technology Limited
    Inventors: Keith Jones, Carl Rye, Nicola Chessum, Matthew Cheeseman, Adele E. Pasqua, Kurt G. Pike, Paul F. Faulder
  • Heterocyclic modulators of lipid synthesis
    Patent number: 10189822
    Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: January 29, 2019
    Assignee: 3-V Biosciences, Inc.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu, Gregory Duke, Yamini Ohol-Gupta, Timothy Sean Heuer, Marie O'Farrell
  • Neprilysin inhibitors
    Patent number: 10189823
    Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: January 29, 2019
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Adam D. Hughes
  • Pyrimidine-diamine dual HSP90/TRAP1 inhibitors
    Patent number: 10189824
    Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical composition thereof, which are useful as dual Hsp90/TRAP1 inhibitors. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and their use in treating one or more cancers.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: January 29, 2019
    Assignee: Calasia Pharmaceuticals, Inc.
    Inventors: Srinivasa Reddy Natala, Sridhar G. Prasad
  • Heteroaryl compounds and methods of use thereof
    Patent number: 10189825
    Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: January 29, 2019
    Assignees: SUNOVION PHARMACEUTICALS INC., PGI DRUG DISCOVERY LLC
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Heterocyclic compounds and methods of use
    Patent number: 10189826
    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: Grant
    Filed: March 4, 2016
    Date of Patent: January 29, 2019
    Assignee: Medivation Technologies LLC
    Inventors: Brahmam Pujala, Ramniwas Jangir, Rambabu Guguloth, Bharat Uttam Shinde, Roopa Rai, Son Minh Pham, Sebastian Bernales, Jeffrey Lindquist, Mausumee Guha, Satyanarayana Kallem, Bhawana Bhatt, Vikas Ramdas Bhagwat
  • Retinoic acid receptor antagonists as chaperone-mediated autophagy modulators and uses thereof
    Patent number: 10189827
    Abstract: Compounds, compositions and methods are provided for selectively activating chaperone-mediated autophagy (CMA), protecting cells from oxidative stress, proteotoxicity and lipotoxicity, and/or antagonizing activity of retinoic acid receptor alpha (RAR?) in subjects in need thereof.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: January 29, 2019
    Assignee: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Ana Maria Cuervo, Evripidis Gavathiotis, Qisheng Xin, Bhaskar C. Das
  • 1-methylpyrazole-piperazine compounds having multimodal activity against pain
    Patent number: 10189828
    Abstract: The present invention relates to 1-methylpyrazole-piperazine compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: January 29, 2019
    Assignee: LABORATORIOS DEL DR. ESTEVE S.A.
    Inventors: Carmen Almansa-Rosales, Monica Garcia-Lopez, Lourdes Garriga-Sanahuja, Ana Virginia Llorente-Fernandez
  • Inhibiting agents for Bruton's tyrosine kinase
    Patent number: 10189829
    Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.
    Type: Grant
    Filed: August 27, 2018
    Date of Patent: January 29, 2019
    Assignee: BIOGEN MA INC.
    Inventors: Brian T. Hopkins, Bin Ma, Robin Prince, Isaac Marx, Joseph P. Lyssikatos, Fengmei Zheng, Matthew Peterson, Daniel B. Patience
  • Alkyl-heteroaryl substituted quinone derivatives for treatment of oxidative stress disorders
    Patent number: 10189830
    Abstract: Disclosed herein are alkyl-heteroaryl substituted quinone derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 29, 2019
    Assignee: BIOELECTRON TECHNOLOGY CORPORATION
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Christopher R. Cornell
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 10189831
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: January 29, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Yongxin Han, Yaozong Li, Yunfu Luo, Mehul Patel
  • Crystalline solid forms of a BET inhibitor
    Patent number: 10189832
    Abstract: The present application relates to crystalline solid forms of an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: January 29, 2019
    Assignee: Incyte Corporation
    Inventors: Shili Chen, Zhongjiang Jia, Pingli Liu, Lei Qiao, Yongzhong Wu, Jiacheng Zhou
  • Solid forms of a compound modulating kinases
    Patent number: 10189833
    Abstract: Solid forms of the compound, [5-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(6-trifluoromethyl-pyridin-3-ylmethyl)-amine HCl salt (Compound I) and its free base, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3, were prepared and characterized: Also provided are methods of using the solid forms.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: January 29, 2019
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Gary Conard Visor
  • Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer
    Patent number: 10189834
    Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: January 29, 2019
    Assignee: AstraZeneca AB
    Inventors: Bernard Christophe Barlaam, Kurt Gordon Pike
  • Derivatives and methods of treating hepatitis B infections
    Patent number: 10189835
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: January 29, 2019
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventors: George D. Hartman, Scott Kuduk
  • Therapeutic compounds, compositions and methods of use thereof
    Patent number: 10189836
    Abstract: Compounds of Formula (I) and methods of use as Janus kinase inhibitors are described herein.
    Type: Grant
    Filed: June 15, 2018
    Date of Patent: January 29, 2019
    Assignee: Genentech, Inc.
    Inventors: Yun-Xing Cheng, Rongbao Hua, Terry Kellar, Wei Li, Paul Gibbons, Mark Edward Zak
  • Crystalline (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt
    Patent number: 10189837
    Abstract: Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer.
    Type: Grant
    Filed: July 17, 2017
    Date of Patent: January 29, 2019
    Assignee: Medivation Technologies LLC
    Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Shichun Peng