Additional Hetero Ring Attached Directly Or Indirectly To The Quinazoline Ring System By Nonionic Bonding Patents (Class 514/266.2)
  • Patent number: 11008306
    Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: May 18, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, John Lloyd, Heather Finlay, James Neels, Naveen Kumar Dhondi, Prashantha Gunaga, Abhisek Banerjee, Ashokkumar Adisechan
  • Patent number: 10968202
    Abstract: The present invention relates compounds of Formula (A) as H3R antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of Histamine 3 Receptor (H3R) functions. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to H3R functions in humans.
    Type: Grant
    Filed: June 23, 2020
    Date of Patent: April 6, 2021
    Assignee: XW LABORATORIES INC.
    Inventors: Jia-Ning Xiang, Xuesong Xu, Yi Feng, Wai-Si Eng
  • Patent number: 10882851
    Abstract: This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR?R?, C1-7 alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7 alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7 alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7 alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R? and R? are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: January 5, 2021
    Assignee: Gilead Sciences, Inc.
    Inventors: Ling-Jie Gao, Piet André Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
  • Patent number: 10865218
    Abstract: Methylene blue (MB) derivatives selectively detect F? by desilylation reaction to act as a fluorescent probe.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: December 15, 2020
    Assignee: The Procter & Gamble Company
    Inventors: Yunming Shi, Ross Strand, Tao Yi, Peng Wei, FengFeng Xue
  • Patent number: 10858340
    Abstract: Disclosed are a crystal of a maleate of a compound of formula (I), a preparation method for the crystal, a crystallization composition of same, a pharmaceutical composition of same, and uses thereof in preventing and treating a tumor.
    Type: Grant
    Filed: August 24, 2017
    Date of Patent: December 8, 2020
    Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO. LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD., CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Song Tang, Yizhong Zhu, Fei Liu, Jie Zhou, Zhilin Chen, Hongjiang Xu, Xin Tian
  • Patent number: 10842669
    Abstract: A method of treatment is disclosed herein. The method includes administering to a patient in need thereof a polymer implant device containing a biocompatible drug, or a plurality of nanoparticles or microparticles conjugated with the biocompatible drug, the biocompatible drug comprising one or more Rock inhibitors, one or more Wnt inhibitors, one or more integrin inhibitors, and/or one or more glycogen synthase kinase 3 (GSK-3) inhibitors, the patient having a medical condition selected from the group consisting of dry eye, glaucoma, retinal detachment, retinal degeneration, age-related macular degeneration, a cataract, uveitis, a corneal genetic disease, postoperative inflammation, immune-related inflammatory processes, diabetic retinopathy, a side effect occurring after cataract surgery, a side effect occurring after refractive surgery, and combinations thereof.
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: November 24, 2020
    Inventor: Gholam A. Peyman
  • Patent number: 10752640
    Abstract: Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: August 25, 2020
    Assignee: NUEVOLUTION A/S
    Inventors: Jimmi Gerner Seitzberg, Tine Titilola Akinlemnu Kronborg, Visnja Poljak, Gitte Friberg, Lene Teuber
  • Patent number: 10709708
    Abstract: The invention provides combinations comprising a MERTK inhibitor, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor and methods of use thereof, including methods of treating disorders such as cancer.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: July 14, 2020
    Assignees: The University of North Carolina at Chapel Hill, Emory University
    Inventors: Dan Yan, H. Shelton Earp, III, Deborah Ann DeRyckere, Douglas Kim Graham, Jing Wan
  • Patent number: 10689366
    Abstract: Provided herein are bifunctional compounds that inhibit MALT1 and/or promote targeted ubiquitination for the degradation of MALT1. In particular, provided are compounds that can bind MALT1, a protein whose activity is responsible for constitutive NF-KB signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)), and can assist in its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon, VHL), which can ubiquitinate MALT1, marking it for proteasome degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating cancer with the bifunctional compounds, methods of promoting the degradation of MALT1, and methods of binding E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: June 23, 2020
    Assignees: Cornell University, Dana-Farber Cancer Institute, Inc.
    Inventors: Ari M. Melnick, Lorena Fontan Gabas, Nathanael S. Gray, David A. Scott, John Hatcher, Guangyan Du
  • Patent number: 10682353
    Abstract: The present disclosure provides a method of treating a patient with refractory or resistant cancer by administering a therapeutically effective amount of a compound of formula (I), such as Varlitinib, or an enantiomer thereof or a pharmaceutically acceptable salt of any one of the same. Also provided is a compound of formula (I) for use in the treatment of resistant or refractory cancer and use of a compound of formula (I) for the manufacture of a medicament for the treatment of resistant or refractory cancer.
    Type: Grant
    Filed: September 5, 2016
    Date of Patent: June 16, 2020
    Assignee: ASLAN Pharmaceuticals PTE LTD
    Inventors: Bertil Lindmark, Lisa Ooi
  • Patent number: 10562891
    Abstract: The present invention relates to quinazolinones and related compounds which are inhibitors of PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: February 18, 2020
    Assignee: Ribon Therapeutics Inc.
    Inventors: Laurie B. Schenkel, Melissa Marie Vasbinder, Kevin Wayne Kuntz, Kerren Kalai Swinger
  • Patent number: 10507209
    Abstract: The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.
    Type: Grant
    Filed: August 7, 2017
    Date of Patent: December 17, 2019
    Assignee: XUANZHU PHARMA CO, LTD.
    Inventors: Yanyan Dong, Chengkon Shih
  • Patent number: 10357494
    Abstract: In one aspect the present disclosure provides a method of sensitizing a cancer patient to chemotherapy by administering a combination therapy comprising; a) a therapeutically effective amount of a compound of formula (I) an enantiomer thereof or a pharmaceutically acceptable salts of any one of the same, and b) a chemotherapeutic agent or a combination of chemotherapeutic agents.
    Type: Grant
    Filed: September 5, 2016
    Date of Patent: July 23, 2019
    Assignee: ASLAN Pharmaceuticals PTE LTD
    Inventors: Bertil Lindmark, Lisa Ooi
  • Patent number: 10239843
    Abstract: The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: March 26, 2019
    Assignee: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Alison E. McGonagle, Allan Jordan, Bohdan Waszkowycz, Colin Hutton, Ian Waddell, James R. Hitchin, Kate Mary Smith, Niall M. Hamilton
  • Patent number: 10214511
    Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: February 26, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: John Lloyd, Heather Finlay, Prashantha Gunaga, Abhisek Banerjee, Ashokkumar Adisechan
  • Patent number: 10087148
    Abstract: The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. 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: December 4, 2015
    Date of Patent: October 2, 2018
    Assignees: THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES OFFICE OF TECHNOLOGY TRANSFER, NATIONAL INSTITUTE OF HEALTH, SOUTHERN RESEARCH INSTITUTE
    Inventors: Subramaniam Ananthan, Richard B. Rothman
  • Patent number: 9861618
    Abstract: The present invention comprises compounds of Formula I wherein: R1, R2, R3, R4, R5, R7, R8, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the 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 Formula I.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: January 9, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Steven Goldberg, Christoph Steeneck, Christian Gege, Olaf Kinzel, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 9840516
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: October 10, 2014
    Date of Patent: December 12, 2017
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Tao Wu, Pingda Ren, Yi Liu, Yuan Liu, Yun Oliver Long
  • Patent number: 9770026
    Abstract: Disclosed is a substituted pyrimidine compound having a structure as represented by formula PY. See the description for the definition of each substituent in the formula. The compound of the present invention provides broad-spectrum bactericidal, pesticidal, and acaricidal activities, provides great control effects against plant diseases such as cucumber downy mildew, corn rust, wheat powdery mildew, rice blast, and cucumber gray mold, specifically provides improved control effects against cucumber downy mildew, corn rust, wheat powdery mildew, and rice blast, provides great control effects against aphid, carmine spider mite, diamondback moth, and armyworm, and acquires great effects at a minimal dosage. The compound of the present invention also provides characteristics such as a simplified preparation method.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: September 26, 2017
    Assignee: Shenyang Sinochem Agrochemicals R&D Co., Ltd.
    Inventors: Changling Liu, Lizeng Wang, Yuquan Song, Xufeng Sun, Jie Lan, Aiying Guan, Junfeng Wang, Jinbo Zhang, Cong Feng, Minna Zhu, Zhinian Li, Lanhui Ren, Xiuhui Chang, Fan Yang, Qin Sun, Wei Chen, Shaowu Liu, Yinping Zhou, Zhonggang Shan, Baoshan Chai, Bin Wang, Jizhong Zhou
  • Patent number: 9730934
    Abstract: The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: August 15, 2017
    Assignee: XUANZHU PHARMA CO., LTD.
    Inventors: Zhenhua Huang, Yanyan Dong
  • Patent number: 9717720
    Abstract: The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: August 1, 2017
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Patent number: 9649312
    Abstract: This invention generally relates to compositions and methods for cancer treatment and, in particular, to compositions able to interact (e.g., bind to) with MUC1 growth factor receptor or its ligands, and methods for treating the same. The invention also relates to assays or use of such compositions for the treatment of patients susceptible to or exhibiting symptoms characteristic of cancer or tumorigenesis. Other compositions of the present invention useful for the treatment or prevention of cancer or tumorigenesis include homologs, analogs, derivatives, enantiomers or functional equivalents. The present compositions can also be packaged in kits in some cases.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: May 16, 2017
    Assignee: Minerva Biotechnologies Corporation
    Inventor: Cynthia Bamdad
  • Patent number: 9567358
    Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
    Type: Grant
    Filed: March 18, 2015
    Date of Patent: February 14, 2017
    Assignee: AstraZeneca AB
    Inventors: Nicola Murdoch Heron, Frederic Henri Jung, Andrew Mortlock, Georges Pasquet
  • Patent number: 9556151
    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 18, 2014
    Date of Patent: January 31, 2017
    Assignee: ASTRAZENECA AB
    Inventor: James McCabe
  • Patent number: 9458114
    Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: October 4, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, John Lloyd, Heather Finlay, Ji Jiang, James Neels, Naveen Kumar Dhondi, Prashantha Gunaga, Abhisek Banerjee, Ashokkumar Adisechan
  • Patent number: 9394544
    Abstract: Disclosed herein are methods, compounds and compositions designed for ameliorating oxidative stress in cells. In particular, disclosed are viral vectors that express RNA interfering molecules for inhibiting expression or activity of Nox1 or RAC1. Depending on the location of administration, expression of inhibiting molecules can reduce oxidative stress in neurons associated with a particular neurodegenerative condition.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: July 19, 2016
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventor: Yoon-Seong Kim
  • Patent number: 9388142
    Abstract: Compounds of the formula I in which R1, R2, R3, X1, X2 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: July 12, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Hans-Peter Buchstaller
  • Patent number: 9359347
    Abstract: The subject invention concerns materials and methods for inhibiting the Akt/PKB pathway. In one embodiment, a compound of the invention inhibits kinase activity and/or phosphorylation levels of Akt proteins. The subject invention also concerns methods for inhibiting or killing a cancer cell or other cell in which expression of an Akt protein is elevated or constitutively active, comprising contacting the cell with an effective amount of a compound of formula I. The subject invention also concerns methods for treating cancer or a tumor in a person or animal comprising administering an effective amount of a compound of formula I to the person or animal.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: June 7, 2016
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Mei Sun, Said M. Sebti
  • Patent number: 9347863
    Abstract: The present invention provides labeling and capture reagents that comprise phosphorothioate oligonucleotides (PS-ODN). The PS-ODN bind to all white blood cells (leukocytes) in an indiscriminative fashion and enable the labeling, capture, or concentration of leukocytes in a manner that preserves the antigenic integrity of the cells. Methods for the use of phosphorothioate oligonucleotides are provided.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: May 24, 2016
    Assignee: Becton, Dickinson and Company
    Inventors: Majid Mehrpouyan, Marybeth Sharkey
  • Patent number: 9321762
    Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein G is a heteroaryl, heterocyclic or alkyne; X is N or CH; L1 is —N(R7)—, —O—, —C(S)—, —C(O)—, or —S—; L2 is —N(R8)— or —O—; R1 and R2 are independently hydrogen, halogen, hydroxyl, amino, cyano, nitro, carboxy, C1-C4 alkoxy, C1-C4 alkoxy C1-C4 alkoxy, N,N—(C1-C4 dialkyl)amino C1-C4 alkoxy, N—(C1-C4 alkyl)amino C1-C4 alkoxy, C1-C4 alkanoyl, C1-C4 alkanoyloxy, N—(C1-C4 alkyl)amino, N,N—(C1-C4 dialkyl)amino, C1-C4 alkanoyl amino, or heterocyclyl, wherein C1-C4 alkyl is optionally substituted with one or more substituents selected from fluorine and chlorine; R3, R4 and R5 are independently hydrogen, fluorine or chlorine; R6 is C1-C4 alkyl or aryl, which is optionally substituted with one or more substituents selected from halogen, hydroxyl, amino, cyano, nitro; or R6 and R8 form a 5-6 membered cyclyl or heterocyclyl.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: April 26, 2016
    Assignee: Development Center for Biotechnology
    Inventors: Mann-Yan Kuo, Chu-Bin Liao, Shao-Zheng Peng, Shih-Chieh Yen, Nan-Horng Lin
  • Patent number: 9321759
    Abstract: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for inhibiting cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, and methods for treating these disorders.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: April 26, 2016
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Mark I. Greene, Hongtao Zhang, Alan Berezov, Zheng Cai
  • Patent number: 9315500
    Abstract: The present invention relates to bicyclic heteroaryl cycloalkyldiamine derivatives, to processes for their production, to their use as SYK inhibitors and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: April 19, 2016
    Assignee: NOVARTIS AG
    Inventors: Peter Buehlmayer, Alexander Baxter Smith, Gebhard Thoma, Maurice Van Eis
  • Patent number: 9309228
    Abstract: The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: April 12, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Markus Ostermeier, Peter Sieger
  • Patent number: 9290475
    Abstract: The invention provides 3-deuterium-enriched 3-(6-, 7-, or 8-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: March 22, 2016
    Assignee: DeuteRx, LLC
    Inventor: Sheila DeWitt
  • Patent number: 9249121
    Abstract: Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: February 2, 2016
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man, Benjamin M. Cohen, Ying Li, Jean Xu, William W. Leong
  • Patent number: 9238666
    Abstract: A compound of structural formula (I), wherein R is H or —PO3H or a pharmaceutically acceptable salt form thereof. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: January 19, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jayakumar S. Warrier, Navnath Dnyanoba Yadav
  • Patent number: 9205087
    Abstract: A series of new 6-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones have been synthesized. The compounds are structurally related to adoprazine, a potential atypical antipsychotics bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling of suitably modified aryl bromides with tert-butyl piperazine-1-carboxylate afforded the advanced intermediate piperazinyl-3,4-dihydroquinazolin-2(1H)-one. The reductive amination of the latter with appropriately designed biarylaldehydes accomplished the synthesis of these compounds.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: December 8, 2015
    Assignees: KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS, KING ABDULAZIZ CITY FOR SCIENCE AND TECHNOLOGY
    Inventor: Nisar Ullah
  • Patent number: 9192610
    Abstract: The present invention relates to the use of a series of quinazoline-derived compounds to produce a medicament for the treatment and/or prevention of neurological and/or neurodegenerative diseases, such as Parkinson's disease or Alzheimer's disease. The present invention also relates to a method for the treatment and/prevention of neurological and/neurodegenerative diseases comprising the administration of a therapeutically effective amount of said compounds.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: November 24, 2015
    Assignee: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS
    Inventors: Ana Martínez Gil, Carmen Gil Ayuso-Gontan, Concepción Pérez Martín, Ana Pérez Castillo, José Morales García, Miriam Redondo Sancho, Marina Sanz San Cristóbal
  • Patent number: 9186399
    Abstract: The invention relates to oligonucleotides including at least one FANA substituted nucleotide analog and a pyrimidine-purine dinucleotide. The invention also relates to pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: September 29, 2008
    Date of Patent: November 17, 2015
    Assignee: AdiutTide Pharmaceuticals GmbH
    Inventors: Eugen Uhlmann, Harald Debelak, Marion Jurk, Markus Weber
  • Patent number: 9187459
    Abstract: The invention provides quinazoline-7-ether derivatives, particularly 4-anilinyl-6-butenamido-quinazoline-7-ether derivatives that are inhibitors of the receptor protein tyrosine kinases (RTK). The compounds are useful in the treatment of diseases and disorders where RTK activity is implicated such as a hyperproliferative diseases (e.g., cancer). Also provided are methods of preparation of the quinazoline derivatives and methods of use as therapeutic agents alone or in a drug combination.
    Type: Grant
    Filed: May 17, 2012
    Date of Patent: November 17, 2015
    Assignee: NewGen Therapeutics, Inc.
    Inventors: Wang Shen, Wei Xiao, Jack Maung, Aimin Zhang, Xiaoling Zheng, Zhenzhong Wang, Qingming Guo, Yingguang Li
  • Patent number: 9180114
    Abstract: This invention relates to methods for neuroprotection, promoting survival of motor neurons and the treatment of motor neuron diseases by preventing cell signaling through the classic prostaglandin D2 receptor DP1.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: November 10, 2015
    Assignee: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Kevin Eggan, Francesco Paolo DiGiorgio
  • Patent number: 9169241
    Abstract: The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: October 27, 2015
    Assignee: Max-Planck-Gesellschaft Zur Forderung der Wissenschaften E.V.
    Inventors: Axel Ullrich, Robert Torka, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
  • Patent number: 9155739
    Abstract: Histone deacetylases inhibitors (HDACIs) and methods for treating cancer in a subject in need thereof are disclosed. The HDACIs comprise a compound of Formula X. or a pharmaceutically acceptable salt thereof. In one embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is fluoro; R5 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; and R6 is hydrogen, or a salt thereof. In another embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; R5 is chloro or fluoro; and R6 is hydrogen.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: October 13, 2015
    Assignee: ANNJI PHARMACEUTICAL CO., LTD.
    Inventors: Ji-Wang Chern, Chao-Wu Yu, Pei-Teh Chang
  • Patent number: 9145376
    Abstract: Compounds of formula (I) in which R3 is chosen from hydrogen, cyano, nitro, acetyl and C(?O)NH2, and Ar is optionally substituted monocyclic or bicyclic aryl or heteroaryl, are useful as antitumor agents.
    Type: Grant
    Filed: January 18, 2012
    Date of Patent: September 29, 2015
    Assignee: The Rockefeller University
    Inventors: James K. Chen, Tarun M. Kapoor, Ari J. Firestone, Joshua S. Weinger
  • Patent number: 9145388
    Abstract: A series of new 6-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones have been synthesized. The compounds are structurally related to adoprazine, a potential atypical antipsychotics bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling of suitably modified aryl bromides with tert-butyl piperazine-1-carboxylate afforded the advanced intermediate piperazinyl-3,4-dihydroquinazolin-2(1H)-one. The reductive amination of the latter with appropriately designed biarylaldehydes accomplished the synthesis of these compounds.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: September 29, 2015
    Assignees: King Fahd University of Petroleum and Minerals, King Abdulaziz City for Science Technology
    Inventor: Nisar Ullah
  • Patent number: 9139577
    Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: September 22, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Andreas Blum, Dirk Gottschling, Armin Heckel, Joerg P. Hehn, Bernhard Schmid, Dieter Wiedenmayer
  • Patent number: 9090568
    Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: July 28, 2015
    Assignee: IMPACT Therapeutics, Inc.
    Inventors: Dong Liu, Minsheng Zhang, Kan He, Lianshan Zhang
  • Patent number: 9062028
    Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: June 23, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
  • Patent number: 9045437
    Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R7, R8, R2?, R3?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br methoxyl group, NH2 group or NMe2 group; X represents NH, O or S; R6 is selected from the group consisting of: piperidinyl group, morpholino group, methoxyl group, and dimethylamine group. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.
    Type: Grant
    Filed: July 30, 2013
    Date of Patent: June 2, 2015
    Assignee: China Medical University
    Inventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen, Yang-Chang Wu
  • Patent number: 9040548
    Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3, wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3, wherein R3 is as defined herein; 3) C2-5alkynylR3, wherein R3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: January 3, 2014
    Date of Patent: May 26, 2015
    Assignee: AstraZeneca AB
    Inventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin