Patents Examined by Alicia L Otton
  • Heterocycle and carbocycle derivatives having TRKA inhibitory activity
    Patent number: 10532985
    Abstract: The present invention relates to a compound represented by Formula (I): wherein -L- is —C(?X)—, or the like, —Z— is —NR5—, or the like, —ZA— is —NR5A—, or the like, —W— is —C(R8R9)n-, —WA— is —C(R3R4)m-, B is substituted or unsubstituted aromatic carbocyclyl, or the like, Y is a bond, or the like, the ring C is a substituted or unsubstituted aromatic heterocycle, or the like, R2 is a hydrogen atom, or the like, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: January 14, 2020
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Yukimasa, Tohru Horiguchi, Kazuya Kano
  • Boron-containing small molecules
    Patent number: 10533021
    Abstract: This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: January 14, 2020
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Stephen J. Baker, Vincent S. Hernandez, Rashmi Sharma, James A. Nieman, Tsutomu Akama, Yong-Kang Zhang, Jacob J. Plattner, Michael Richard Kevin Alley, Rajeshwar Singh, Fernando Rock
  • Fluoroalkyl-substituted aryltriazole derivatives and uses thereof
    Patent number: 10525041
    Abstract: The present invention relates to novel 5-(fluoroalkyl)-1-aryl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: January 7, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Thomas Neubauer, Marie-Pierre Collin-Kröpelin, Peter Kolkhof, Elisabeth Pook, Matthias Beat Wittwer, Klemens Lustig, Carsten Schmeck, Pierre Wasnaire, Heiko Schirmer
  • Pharmaceutical compounds
    Patent number: 10526357
    Abstract: Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.
    Type: Grant
    Filed: December 7, 2018
    Date of Patent: January 7, 2020
    Assignee: Rafael Pharmaceuticals, Inc.
    Inventors: Robert Shorr, Robert Rodriguez, Paul Bingham, Lakmal Boteju, Thomas Kwok, James Marecek
  • Methods and compositions of inhibiting DCN1-UBC12 interaction
    Patent number: 10525048
    Abstract: In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: January 7, 2020
    Assignees: Memorial Sloan Kettering Cancer Center, St. Jude Children's Research Hospital
    Inventors: Jaeki Min, Daniel C. Scott, Deepak Bhasin, Brenda A. Schulman, Bhuvanesh Singh, Jared T. Hammill, R. Kiplin Guy
  • Compounds as GPR119 agonists
    Patent number: 10526345
    Abstract: The present invention relates to novel compounds of formula (I) as GPR119 agonist, composition compositions containing such compounds and method of preparation thereof.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: January 7, 2020
    Assignee: MANKIND PHARMA LTD.
    Inventors: Rakesh Ishwar Patil, Jeevan Verma, Dharmesh Shah, Sazid Ali, Srinivasa Reddy Bapuram, Santosh Kumar Rai, Anil Kumar
  • Process for preparing AG-10, its intermediates, and salts thereof
    Patent number: 10513497
    Abstract: Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.
    Type: Grant
    Filed: February 16, 2018
    Date of Patent: December 24, 2019
    Assignee: EIDOS THERAPEUTICS, INC.
    Inventors: Pooran Chand, Yogesh Kumar Gupta, Rakesh Kumar Kumawat, Mamoun Alhamadsheh, Robert Zamboni
  • Anti-tumor compound and the medical use thereof
    Patent number: 10512627
    Abstract: The invention disclose a compound of formula (I), wherein, R1 is selected from —H or C1-C6 hydrocarbon group, —NH2, —OH, —O(CH2)nCH3 (n=0, 1 or 2), —N(CH3)2, or —CH2N(CH3)2, R2 is selected from an amino acid or an hydroxy acid or —OH (R1, R2 are not —CH3 and —OH at the same time), wherein X, Y are —H, —CH3, —CH2OH, —CH(OH)CH3, —CH2SH, —CH(CH3)2, —CH2CH(CH3)2, —CH(CH3)CH2CH3, —CH2CH2SCH3, —CH2COOH, —CH2CONH2, —CH2CH2COOH, —CH2CH2CH2CH2NH2, or —CH2CH2CONH2, R3-R5 are H or C1-C6 hydrocarbon group. The compound has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro, and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: December 24, 2019
    Assignee: Tianjin Medical University Cancer Institute and Hospital
    Inventors: Ning Zhang, Yinsong Wang, Ping Zhou, Hua Guo, Yi Luo, Xishan Hao, Hua Geng
  • TYK2 inhibitors and uses thereof
    Patent number: 10508120
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: April 12, 2019
    Date of Patent: December 17, 2019
    Assignee: Nimbus Lakshimi, Inc.
    Inventors: Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal, Scott D. Cowen, Thomas H. McLean
  • Substituted nitrogen containing compounds
    Patent number: 10501449
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is: each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
    Type: Grant
    Filed: May 31, 2018
    Date of Patent: December 10, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Navnath Dnyanoba Yadav, Rajeev S. Bhide, Rajesh Onkardas Bora, Prashantha Gunaga, Manoranjan Panda, Eldon Scott Priestley, Jeremy Richter
  • Branched hetero polyethylene glycol and intermediate
    Patent number: 10494340
    Abstract: A branched hetero polyethylene glycol according to the present invention is represented by the formula [1]: wherein X and Y represent each an atomic group containing at least a functional group which reacts with a functional group present in a bio-functional molecule to form a covalent bond and the functional group contained in the atomic group X and the functional group contained in the atomic group Y are different from each other; s is an integer of 2 to 8, which represents the number of polyethylene glycol chains; n is the number of average added moles for the polyethylene glycol chain and 20?n?2000; and E is a branching linker moiety having s-valent bonding valency for the polyethylene glycol chains and having monovalent bonding valency for the functional group Y.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: December 3, 2019
    Assignee: NOF CORPORATION
    Inventors: Yuji Yamamoto, Hiroki Yoshioka, Fumiaki Manabe
  • Compositions and methods for targeting receptors expressed in the gut
    Patent number: 10485789
    Abstract: The invention relates to novel compounds and pharmaceutical preparations thereof, as well as methods of making an using these compounds. The invention further relates to methods of treating or preventing disease using the novel compounds of the invention.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: November 26, 2019
    Assignee: Sensor Pharmaceuticals, Inc.
    Inventor: James R. Hauske
  • Preparation method for 1-substituted-1H-1,2,3-triazole 4-carboxylic acid
    Patent number: 10487063
    Abstract: Provided is a preparation method for 1-substituted-1H-1, 2, 3-triazole-4-carboxylic acid. 1-Substituted-4, 5-dibromo-1H-1,2,3-triazole is added to an isopropylmagnesium chloride to obtain 1-substituted-4-bromo-1H-1,2,3-triazole by a reaction; then an isopropylmagnesium chloride-lithium chloride composite is added directly to obtain a mixture of 1-substituted-1H-1,2,3-triazole-4-carboxylic acid and 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylic acid; secondly, to the mixture, a base and iodomethane are added to obtain 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylic acid methyl ester by a reaction; the aqueous layer is adjusted with hydrochloric acid to pH=1-5, extracted with an organic solvent and dried; then 1-substituted-1H-1,2,3-triazole-4-carboxylic acid is obtained by concentration and crystallization. The method is suitable for industrialized production and has a greater application value.
    Type: Grant
    Filed: September 16, 2015
    Date of Patent: November 26, 2019
    Assignee: ABA CHEMICALS (SHANGHAI) LIMITED
    Inventors: Yueheng Jiang, Limin Que, Jun Xu, Dongguang Qin, Tong Cai
  • Therapeutic targeting of casein kinase 1? in breast cancer
    Patent number: 10485804
    Abstract: The invention provides a method of inhibiting casein kinase 1? (CK1?), comprising contacting the CK1? with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1? can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1? and ?-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: November 26, 2019
    Assignee: The Scripps Research Institute
    Inventors: William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg
  • Crystalline forms of selective S1P1 receptor modulator and preparation method thereof
    Patent number: 10487064
    Abstract: The present disclosure relates to crystalline Form 1, Form 2, Form 3 of Ponesimod, a selective S1P1 receptor modulator, and preparation methods thereof. The X-ray powder diffraction pattern of Form 1 shows characteristic peaks at 2theta values of 18.1°±0.2°, 14.6°±0.2°, 11.3°±0.2°; the X-ray powder diffraction pattern of Form 2 shows characteristic peaks at 2theta values of 3.8°±0.2°, 10.8°±0.2°, 6.1°±0.2°; the X-ray powder diffraction pattern of Form 3 shows characteristic peaks at 2theta values of 12.2°±0.2°, 6.2°±0.2°, 5.6°±0.2°. The crystalline forms in present disclosure not only have better stability but also have higher solubility compared with the prior art forms, they are more suitable for the formulation development of Ponesimod.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: November 26, 2019
    Assignee: Crystal Pharmatech Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Jiaoyang Li, Xiaoyu Zhang
  • Process for the preparation of enantiomerically enriched 3-aminopiperidine
    Patent number: 10464898
    Abstract: The present invention relates to a process for the preparation of enantiomerically enriched 3-aminopiperidine, and in particular of its R-enantiomer (R)-3-aminopiperidine. The invention also relates to an enantiomerically enriched intermediate of said process and to specific acid-addition salts of 3-aminopiperidine (hereinafter also APIP) that are useful for obtaining a single enantiomer of APIP, and to crystalline (R)-3-aminopiperidine-dihydrochloride-monohydrate and crystalline (S)-3-aminopiperidine-di-hydrochloride-monohydrate.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: November 5, 2019
    Assignee: Reuter Chemische Apparatebau KG
    Inventors: Karl Reuter, Tobias Wedel, Viktor Meier, Mark Kantor, Vasyl Andrushko, Florian Stolz
  • Polymorphs of a mPGES-1 inhibiting triazolone compound
    Patent number: 10457649
    Abstract: The present application relates to solid state forms of a triazolone compound which exhibit mPGES-1 enzyme inhibition activity, specifically N-(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-1,2,4-triazol-3-yl)benzyl)pivalamide (Compound of formula II), and process for preparation thereof.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: October 29, 2019
    Assignee: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Nagarajan Muthukaman, Laxmikant A. Gharat, Suresh M. Kadam, Sachin Gavhane, Sandeep B. Khandagale, Sunil P. Nirgude
  • Biodegradable amino-ester nanomaterials for nucleic acid delivery
    Patent number: 10457631
    Abstract: The present disclosure relates to a series of biodegradable amino-ester lipid-like nanoparticles. In some embodiments, the biodegradable amino-ester lipid-like nanoparticles are used in methods for the delivery of nucleic acids.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: October 29, 2019
    Assignee: Ohio State Innovation Foundation
    Inventors: Yizhou Dong, Xinfu Zhang, Xiao Luo
  • Pharmaceutical compounds
    Patent number: 10450337
    Abstract: Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.
    Type: Grant
    Filed: April 14, 2017
    Date of Patent: October 22, 2019
    Assignee: Rafael Pharmaceuticals, Inc.
    Inventors: Robert Shorr, Robert Rodriguez, Paul Bingham, Lakmal Boteju, Thomas Kwok, James Marecek
  • Biocompatible N, N-disubstituted sulfonamide-containing fluorescent dye labels
    Patent number: 10442930
    Abstract: This invention relates to new fluorescent chemical entities, especially fluorescent molecules that comprise biocompatible N, N-disubstituted sulfonamide fluorochromes. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.
    Type: Grant
    Filed: February 15, 2017
    Date of Patent: October 15, 2019
    Assignee: VisEn Medical, Inc.
    Inventors: Narasimhachari Narayanan, Kevin Groves, Jeffrey D. Peterson, Milind Rajopadhye