Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
  • Patent number: 11173157
    Abstract: The present disclosure relates to a class of pyrimidine derivatives having immunomodulating properties that act via TLR7 which are useful in the treatment of viral infections and cancers.
    Type: Grant
    Filed: July 15, 2020
    Date of Patent: November 16, 2021
    Assignee: APROS THERAPEUTICS, INC.
    Inventor: Tom Yao-Hsiang Wu
  • Patent number: 11136310
    Abstract: A series of 2-imino-6-methyltetrahydropyrimidin-4(1H)-one derivatives, substituted in the 6-position by a phenyl moiety which in turn is meta-substituted by an optionally substituted unsaturated fused bicyclic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.
    Type: Grant
    Filed: November 24, 2016
    Date of Patent: October 5, 2021
    Assignee: UCB Biopharma SRL
    Inventors: Rebecca Louise Charlton, Teresa De Haro Garcia, Martin Alexander Lowe, Malcolm Maccoss, Trevor Morgan, Richard David Taylor, Zhaoning Zhu
  • Patent number: 11098044
    Abstract: The present disclosure provides a compound of Formula (I) or pharmaceutically acceptable salt, stereoisomers thereof, a pharmaceutical composition comprising the compound, and a method to treat or prevent neurodegenerative diseases using the compound.
    Type: Grant
    Filed: February 21, 2020
    Date of Patent: August 24, 2021
    Assignee: 1ST Biotherapeutics, Inc.
    Inventors: Jinhwa Lee, Suyeon Jo, Keonseung Lim, A Yeong Park, Jae Eun Kim, Misoon Kim, Seung Mook Lim
  • Patent number: 11033457
    Abstract: A particulate plug for removing a preservative from a solution, suspension, or emulsion comprising a drug is presented. The plug comprises microparticles of a homopolymer comprising a hydrophilic repeating unit or of a copolymer comprising at least one hydrophilic repeating unit and at least one hydrophobic repeating unit. The microparticles are irregular-shaped rigid aggregates and are sized and packed to yield a hydraulic permeability greater than 0.01 Da. The homopolymers have absorbed portions of a preservative to be removed and/or a drug for delivery in solution, as can the copolymer.
    Type: Grant
    Filed: April 18, 2019
    Date of Patent: June 15, 2021
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Anuj Chauhan, Phillip J. Dixon, Poorvajan Sekar
  • Patent number: 11020391
    Abstract: The present invention provides compounds that can modulate the amount of Nav1.7 protein, a key protein in pain signaling, that is present in the cellular surface and methods for using such compounds. In particular, compounds of the invention modulate the amount of Nav1.7 protein on the cellular surface by modulating SUMOylation of CRMP2. Thus, compounds of the invention can be used to treat various clinical conditions associated with the presence and/or activation of Nav1.7 protein on the cellular surface and/or SUMOylation of CRMP2.
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: June 1, 2021
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: May Khanna, Rajesh Khanna, Vijay Gokhale, Reena Chawla
  • Patent number: 11013741
    Abstract: Tartrate salts of the compound of structure (I), crystalline forms thereof, and therapeutic applications thereof for treating solid tumors (e.g., advanced solid tumor) or hematopoietic cancers. Also provided herein are methods for synthesizing the tartrate salts and the crystalline forms thereof.
    Type: Grant
    Filed: April 5, 2019
    Date of Patent: May 25, 2021
    Assignee: Sumitomo Dainippon Pharma Oncology, Inc.
    Inventors: Adam Siddiqui-Jain, Paul Flynn, Akihito Nonoyama, Akihito Kiguchiya
  • Patent number: 10981893
    Abstract: Provided herein are heterocyclic derivative compounds of Formula (I) and pharmaceutical compositions comprising said compounds. The compounds of Formula (I) are useful for inhibiting plasma kallikrein. Furthermore, the disclosed compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: April 20, 2021
    Assignee: ATTUNE PHARMACEUTICALS, INC.
    Inventors: Andrew McDonald, Shawn Qian
  • Patent number: 10906878
    Abstract: The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.
    Type: Grant
    Filed: May 6, 2019
    Date of Patent: February 2, 2021
    Assignee: DANA FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Hwan G. Choi, Li Tan
  • Patent number: 10888562
    Abstract: Tartrate salts of the compound of structure (I), crystalline forms thereof, and therapeutic applications thereof for treating solid tumors (e.g., advanced solid tumor) or hematopoietic cancers. Also provided herein are methods for synthesizing the tartrate salts and the crystalline forms thereof.
    Type: Grant
    Filed: April 5, 2019
    Date of Patent: January 12, 2021
    Assignee: Sumitomo Dainippon Pharma Oncology, Inc.
    Inventors: Adam Siddiqui-Jain, Paul Flynn, Akihito Nonoyama, Akihito Kiguchiya
  • Patent number: 10851082
    Abstract: Disclosed are substituted aromatic N-heterocyclic compounds. The disclosed compounds typically exhibit kinase inhibition activity, for example, and inhibit Mnk1 kinase and/or Mnk2 kinase. The disclosed compounds may be used in pharmaceutical compositions and methods for treating diseases or disorders associated with Mnk1 kinase activity and/or Mnk2 kinase activity, such as cancers, diabetes, autism, and fragile X syndrome.
    Type: Grant
    Filed: May 3, 2018
    Date of Patent: December 1, 2020
    Assignee: Northwestern University
    Inventors: Gary E. Schiltz, Javier Izquierdo-Ferrer, Purav Vagadia, Matthew R. Clutter, Rama K. Mishra, Leonidas C. Platanias
  • Patent number: 10836784
    Abstract: A phosphoramidochloridate morpholino monomer of the following formula is provided:
    Type: Grant
    Filed: September 17, 2019
    Date of Patent: November 17, 2020
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Atsushi Endo, Robert T. Yu, Francis Fang, Hyeong Wook Choi, Mingde Shan
  • Patent number: 10822327
    Abstract: A 2-substituted aromatic ring-pyrimidine derivative as shown in a general formula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chk1 kinase inhibitory activity and are promising Chk1 inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: November 3, 2020
    Assignees: ZHEJIANG UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Tao Liu, Jia Li, Yongzhou Hu, Yubo Zhou, Xiaowu Dong, Anhui Gao, Pinrao Song, Peipei Wang, Lexian Tong, Xiaobei Hu, Mingbo Su
  • Patent number: 10787446
    Abstract: The invention provides a compound of formula: or a salt thereof, wherein the variables RAA, n, ring A, ring B, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, and R9 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: September 29, 2020
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Philippe Bergeron, Kristen Burford, Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Abid Hasan, Kwong Wah Lai, Zhiguo Liu, Steven McKerrall, Teresa Phuongtram Nguyen, Brian Safina, Daniel Sutherlin, Tao Wang
  • Patent number: 10774033
    Abstract: Provided herein are methods and intermediates for making (1R,2R,5R)-5-amino-2-methylcyclohexanol hydrochloride, which are useful for the preparation of compounds useful for the treatment of a disease, disorder, or condition associated with the JNK pathway.
    Type: Grant
    Filed: January 28, 2019
    Date of Patent: September 15, 2020
    Assignee: Celgene Corporation
    Inventors: Terrence Joseph Connolly, Hon-Wah Man, Periyandi Nagarajan, Chinnapillai Rajendiran, Jasti Venkateswarlu
  • Patent number: 10717728
    Abstract: Provided are compounds of the formula: and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels.
    Type: Grant
    Filed: June 4, 2019
    Date of Patent: July 21, 2020
    Assignee: Cadent Therapeutics, Inc.
    Inventors: Dipak Vasantrao Amrutkar, Kelly Foster, Thomas Amos Jacobsen, Martin R. Jefson, Gregg F. Keaney, Janus Schreiber Larsen, Karin Sandager Nielsen
  • Patent number: 10689705
    Abstract: The FGFR-encoding gene was studied extensively with regard to its expression, hyperamplification, mutation, translocation, or such in various cancer cells. As a result, novel fusion polypeptides in which the FGFR3 polypeptide is fused with a different polypeptide were identified and isolated from several types of bladder cancer-derived cells and lung cancer cells. The use of a fusion polypeptide of the present invention as a biomarker in FGFR inhibitor-based cancer therapy enables one to avoid side effects in cancer therapy and control the therapeutic condition to produce the best therapeutic effect, thereby enabling individualized medicine.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: June 23, 2020
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Yoshito Nakanishi, Nukinori Akiyama, Yukari Nishito
  • Patent number: 10689351
    Abstract: Provided herein are isotopologues of Compound A, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.
    Type: Grant
    Filed: June 26, 2019
    Date of Patent: June 23, 2020
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Hon-Wah Man, Mohit Atul Kothare
  • Patent number: 10683297
    Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
    Type: Grant
    Filed: November 10, 2018
    Date of Patent: June 16, 2020
    Assignees: CALITOR SCIENCES, LLC, NORTH & SOUTH BROTHER PHARMACY INVESTMENT COMPANY LIMITED
    Inventors: Ning Xi, Minxiong Li, Ju Peng, Xiaobo Li, Tao Zhang, Haiyang Hu, Wuhong Chen, Changlin Bai, Donghua Ke, Peng Chen
  • Patent number: 10647685
    Abstract: The present invention relates to a 6-phenoxypyrimidine derivative, a method for preparing the compound and a pharmaceutical composition containing the compound as an active ingredient. Because the 6-phenoxypyrimidine compound represented by Chemical Formula 1 according to the present invention has an activity of inhibiting the production of nitric oxide (NO) as an inflammation-related factor, it is useful in treating and preventing inflammatory diseases including immunological diseases.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: May 12, 2020
    Assignee: Korea Institute of Science and Technology
    Inventors: Eun Joo Roh, Karam Mohamed Hasan Fara Ahmed, So Ra Paik, Woo Young Hur, Elkamhawy Ahmed
  • Patent number: 10577374
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 7, 2017
    Date of Patent: March 3, 2020
    Assignees: Sunesis Pharmaceuticals, Inc., Biogen MA Inc.
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Patent number: 10562861
    Abstract: The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: February 18, 2020
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Seiji Hori, Futoshi Hasegawa, Daisuke Urabe, Hirotaka Kurebayashi
  • Patent number: 10562888
    Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.
    Type: Grant
    Filed: April 13, 2016
    Date of Patent: February 18, 2020
    Assignee: Eisai R&D Management Co., LTD.
    Inventors: George Moniz, Kristen Sanders, Arani Chanda, Kenshi Yoshida
  • Patent number: 10556871
    Abstract: A method for preparing 5-(4-bromophenyl)-4,6-dichloropyrimidine is provided. The method comprises the steps of: preparing methyl p-bromophenylacetate (Intermediate I) by catalytic esterification of p-bromophenylacetic acid, and then reacting with dimethyl carbonate to synthesize 2-(4-bromophenyl)-malonic acid-1,3-dimethyl ester (Intermediate 2), cyclizing with formamidine hydrochloride to obtain 5-(4-bromophenyl)-4,6-dihydroxypyrimidine (Intermediate 3), and then chlorinating to give the product 5-(4-bromophenyl)-4,6-dichloropyrimidine. In the process of preparing Intermediate 1 in the present invention, a solid acid is used as a catalyst. Moreover, in the process of preparing Intermediate 2, sodium methoxide is used as a base in place of sodium hydride or sodium amide used in the prior art. Furthermore, Intermediate 3 is prepared by a one-pot process.
    Type: Grant
    Filed: January 9, 2019
    Date of Patent: February 11, 2020
    Assignee: ZHEJIANG XIANFENG TECHNOLOGIES CO., LTD.
    Inventors: Feifei Gao, Junlong Gao, Minliang Zhu, Wei Lu, Yi Liu
  • Patent number: 10548897
    Abstract: This invention relates to antagonists of Kinase Suppressor of Ras (KSR). Pharmaceutical compositions comprising KSR inhibitors and methods of treating cancer are also provided.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: February 4, 2020
    Assignee: Icahn School of Medicine at Mount Sinai
    Inventors: Arvin Dar, Neil Dhawan, Alex P. Scopton
  • Patent number: 10501537
    Abstract: The present invention provides methods of treating cancer, particularly cancers that had developed resistance to PD-1 and PDL-1 blockade. Also included are methods of identifying therapeutic targets for the treatment of cancer.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: December 10, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventor: Kwok-Kin Wong
  • Patent number: 10456399
    Abstract: A method for treating cancer in patients with creatinine clearance of 15 mL/min or more and less than 30 mL/min, including dividing a combination drug containing ?,?,?-trifluorothymidine (FTD) and 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride in a molar ratio of 1:0.5, in a dose of 30 to 50 mg/m2/day as FTD-equivalent, into two to four times a day, and orally administering it to the patient.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: October 29, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Kenichiro Yoshida
  • Patent number: 10457666
    Abstract: Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2?±0.2°).
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: October 29, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hideki Kazuno, Tomonobu Mutsumi
  • Patent number: 10441586
    Abstract: The present invention provides compounds that can modulate the amount of Nav 1.7 protein, a key protein in pain signaling, that is present in the cellular surface and methods for using such compounds. In particular, compounds of the invention modulate the amount of Nav 1.7 protein on the cellular surface by modulating SUMOylation of CRMP2. Thus, compounds of the invention can be used to treat various clinical conditions associated with the presence and/or activation of Nav 1.7 protein on the cellular surface and/or SUMOylation of CRMP2.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: October 15, 2019
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: May Khanna, Rajesh Khanna, Vijay Gokhale, Reena Chawla
  • Patent number: 10442788
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y—Z-L-R1??(I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: April 1, 2016
    Date of Patent: October 15, 2019
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Hui Cao, Wei Li, Jorden Kass, Xuri Gao, Xiaowen Peng, Meizhong Jin, Yat Sun Or
  • Patent number: 10428051
    Abstract: The present invention relates to substituted amide derivatives having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opioid 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: July 28, 2016
    Date of Patent: October 1, 2019
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Monica Garcia-Lopez, Carmen Almansa-Rosales, Ana Virginia Llorente-Fernandez, Lourdes Garriga-Sanahuja, Ute Christmann
  • Patent number: 10316002
    Abstract: The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: June 11, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael Gray, Hwan Geun Choi, Li Tan
  • Patent number: 10196357
    Abstract: The invention relates to compounds of formula IB and methods for modulating one or more components of a kinase cascade using these compounds.
    Type: Grant
    Filed: April 14, 2008
    Date of Patent: February 5, 2019
    Assignee: Athenex, Inc.
    Inventor: David G. Hangauer, Jr.
  • Patent number: 10138223
    Abstract: An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2?±0.1°) in powder X-ray diffraction.
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: November 27, 2018
    Assignee: TAIHO PHARMACEUTICALS CO., LTD.
    Inventors: Hideki Kazuno, Tomonobu Mutsumi
  • Patent number: 10130631
    Abstract: The present invention relates to a therapeutic agent for chronic myelogenous leukemia with reduced drug-resistance and side-effects containing a 1,6-disubstituted indole compound.
    Type: Grant
    Filed: August 15, 2017
    Date of Patent: November 20, 2018
    Assignee: Korea Institute of Science and Technology
    Inventors: Tae Bo Sim, Ho Jong Yoon, Woo Young Hur, Yun Ju Nam, Hwan Geun Choi
  • Patent number: 10117853
    Abstract: A compound exerts a strong analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. A cyclic amine derivative represented by general formula or a pharmacologically acceptable salt thereof: A method of treating neuropathic pain includes administering a therapeutically effective amount of the cyclic amine derivative to a mammal. A method of treating fibromyalgia syndrome includes administering a therapeutically effective amount of the cyclic amine derivative to a mammal.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: November 6, 2018
    Assignee: Toray Industries, Inc.
    Inventors: Shuji Udagawa, Yasuhiro Morita, Naoki Izumimoto, Katsuhiko Iseki, Shunsuke Iwano, Tomoya Miyoshi, Yuji Osada, Tetsuro Koreeda, Masanori Murakami, Motohiro Shiraki, Kei Takahashi, Keiyu Oshida, Eriko Higashi
  • Patent number: 10059675
    Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: August 28, 2018
    Assignee: Purdue Pharma L.P.
    Inventors: Chiyou Ni, Laykea Tafesse, Jiangchao Yao, Mark A. Youngman, Minnie Park, Bin Shao
  • Patent number: 10053429
    Abstract: The present invention provides compounds of the Formula below: [Formula should be inserted here] Where A, X, R. and R2-R3 are as described herein; methods of treating patients for hypertriglyceridemia and cardiovascular disease including dyslipidemia and atherosclerosis, and processes for preparing the compounds.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: August 21, 2018
    Assignee: Eli Lilly and Company
    Inventors: Ana Maria Escribano, Maria Rosario Gonzalez, Celia Lafuente Blanco, Maria Dolores Martin-Ortega Finger, Michael R Wiley
  • Patent number: 10047056
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: July 20, 2017
    Date of Patent: August 14, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Makonen Belema, Van N. Nguyen
  • Patent number: 9890140
    Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: February 13, 2018
    Assignee: ASTRAZENECA AB
    Inventor: James McCabe
  • Patent number: 9856232
    Abstract: A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: wherein Z is selected from CH2O, O, and N; X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof. The present subject matter also relates to a method of making a dihydropyrimidinone derivative, a method of treating a gastrointestinal disease, a method of treating an ulcer, a pharmaceutical composition, and a method of making a pharmaceutical composition.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: January 2, 2018
    Assignee: KING SAUD UNIVERSITY
    Inventors: Mashooq Ahmad Bhat, Mohamed Abdulrahman Al-Omar
  • Patent number: 9809559
    Abstract: The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: November 7, 2017
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Brandon H. Brown, Ernest A. Carra, Jeffrey N. Hemenway, Henry Morrison, Troy Reynolds, Bing Shi, Dimitrios Stefanidis, Fang Wang, Matthew Robert Warr, James Andrew Whitney, Yan Xin
  • Patent number: 9809568
    Abstract: The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: November 7, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Duane DeMong, Michael Miller, Hong Liu, Xing Dai, Thomas Greshock, Andrew Stamford, Ravi Nargund
  • Patent number: 9802903
    Abstract: This invention is directed to: (a) processes for preparing a compound and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compound and salts; (c) pharmaceutical compositions comprising the compound or salts; and (d) methods of use of such compositions.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: October 31, 2017
    Assignee: AbbVie Inc.
    Inventors: Jean-Christophe Califano, James J. Napier, Calvin L. Becker, Su Yu
  • Patent number: 9795596
    Abstract: The present invention relates to selective cancer treatment regimes based on assaying for the presence or absence of a glutamine or a nucleic acid that encodes glutamine at position 859 of the catalytic p110? subunit of PI3K; methods for producing a transmittable form of information for predicting the responsiveness of patient to (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), or a pharmaceutically acceptable salt thereof; and a kit thereof.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: October 24, 2017
    Assignee: Novartis AG
    Inventors: Pascal Furet, Christine Fritsch, Sauveur-Michel Maira
  • Patent number: 9790229
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: January 25, 2016
    Date of Patent: October 17, 2017
    Assignees: Sunesis Pharmaceuticals, Inc., Biogen MA Inc.
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Patent number: 9789111
    Abstract: The invention relates to pharmaceutical compositions having casein kinase 1 delta (CK1?) inhibitors and to the use of the inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.
    Type: Grant
    Filed: April 2, 2015
    Date of Patent: October 17, 2017
    Assignee: ELECTROPHORETICS LIMITED
    Inventors: Joseph M. Sheridan, Jonathan R. Heal, William D. O. Hamilton, Ian H. Pike
  • Patent number: 9776992
    Abstract: 1-Oxo-1,2-dihydroisoquinolin-7-yl-(5-substituted-thiophen-2-yl)-sulfonamide compounds, formulations containing those compounds, and their use as AICARFT inhibitors.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: October 3, 2017
    Assignee: Eli Lilly and Company
    Inventors: Harold Burns Brooks, Robert Dean Dally, Timothy Barrett Durham, Kevin Robert Fales, Kwame Frimpong, Jefferson Ray McCowan, Frank George Njoroge, Timothy Alan Shepherd, Chong Si, Kenneth Jeff Thrasher, James Lee Toth, Zhipei Wu
  • Patent number: 9771347
    Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
    Type: Grant
    Filed: April 13, 2015
    Date of Patent: September 26, 2017
    Assignee: Exelixis, Inc.
    Inventors: Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava
  • Patent number: RE46757
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: March 20, 2018
    Assignee: Novartis AG
    Inventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
  • Patent number: RE48285
    Abstract: The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: October 27, 2020
    Assignee: Sierra Oncology, Inc.
    Inventors: Brandon H. Brown, Ernest A. Carra, Jeffrey N. Hemenway, Henry Morrison, Troy Reynolds, Bing Shi, Dimitrios Stefanidis, Fang Wang, Matthew Robert Warr, James Andrew Whitney, Yan Xin