Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
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Patent number: 10864213Abstract: The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: May 11, 2015Date of Patent: December 15, 2020Assignee: VERONA PHARMA PLCInventors: Katharine Abbott-Banner, John Hanrahan, David Thomas
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Patent number: 10861630Abstract: An inductor includes a body having a first magnetic portion above and below a coil, and a second magnetic portion above and below the first magnetic portion. The magnetic flux density of the magnetic substance in the first magnetic portion is higher than that of the magnetic substance in the second magnetic portion.Type: GrantFiled: April 28, 2017Date of Patent: December 8, 2020Assignee: SAMSUNG ELECTRO-MECHANICS CO., LTD.Inventors: Han Wool Ryu, Jung Hyuk Jung, Hyo Chan Oh, Yoon Hee Kim, Woon Chul Choi, Jin Ho Ku, Il Jin Park
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Patent number: 10763438Abstract: There is provided a material comprising a n-doped electrically conductive polymer comprising at least one electron-deficient aromatic moiety, each electron-deficient aromatic moiety having a gas-phase electron affinity (EA) of 1-3 eV; and at least one counter-cation covalently bonded to the polymer or to a further polymer comprised in the material, the polymer being n-doped to a charge density of 0.1-1 electron per electron-deficient aromatic moiety, the polymer being capable of forming a layer having a vacuum workfunction (WF) of 2.5-4.5 eV, and wherein all the counter-cations comprised in the material are immobilised such that any electron in the polymer cannot significantly diffuse or migrate out of the polymer. There is also provided a method of preparing the material.Type: GrantFiled: July 1, 2016Date of Patent: September 1, 2020Assignee: National University of SingaporeInventors: Lay-Lay Chua, Peter Kian-Hoon Ho, Rui-Qi Png, Mervin Chun-Yi Ang, Kim-Kian Choo, Cindy Guan-Yu Tang
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Patent number: 10696675Abstract: A novel imidazopyridine derivative compound and uses thereof are disclosed.Type: GrantFiled: June 28, 2017Date of Patent: June 30, 2020Assignee: HANMI PHARMACEUTICAL CO., LTD.Inventors: Moon Sub Lee, Eun Young Byun, Ji Sook Kim, Won Jeoung Kim, Nam Du Kim, Seung Hyun Jung, Young Gil Ahn
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Patent number: 10688191Abstract: A therapeutic method and composition which includes a cannabinoid chemically linked to a chemotherapy agent. The therapeutic composition is capable of crossing the blood-brain barrier, and delivery of the composition across the blood-brain barrier provides both chemotherapy for the treatment of brain cancer and alleviation of side effects caused by the chemotherapy agent. Once across the blood-brain barrier, the chemotherapy agent will be released to attack cancer cells, and the cannabinoid will be free to bind to cannabinoid receptors in the brain to alleviate side effects of chemotherapy such as nausea/vomiting, pain and decreased appetite.Type: GrantFiled: January 19, 2018Date of Patent: June 23, 2020Assignee: HR BIOMED, LLCInventor: Heidi Rowles
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Patent number: 10676483Abstract: A method of treating a patient having cancer is provided comprising administering a therapeutically effective amount of a tricyclic compound or a pharmaceutically acceptable salt of the tricyclic compound to a patient. A method of inhibiting the mitosis of a cancerous cell is also provided.Type: GrantFiled: September 25, 2019Date of Patent: June 9, 2020Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 10654868Abstract: Provided is a dihydropyrazole azepine compound serving as an Akt inhibitor; specifically disclosed is a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 13, 2017Date of Patent: May 19, 2020Assignee: HARBIN ZHENBAO PHARMACEUTICAL CO., LTD.Inventors: Lun Lu, Zhibo Zhang, Gang Li, Lihong Hu, Charles Z. Ding, Shuhui Chen
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Patent number: 10611779Abstract: The invention relates to novel compounds of the formula (I) in which Q, Aa, Ab, Ac, Ad, R1 and n have the definitions given above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.Type: GrantFiled: September 15, 2017Date of Patent: April 7, 2020Assignees: Bayer CropScience Aktiengesellschaft, Bayer AktiengesellschaftInventors: Ruediger Fischer, Dominik Hager, Laura Hoffmeister, Nina Kausch-Busies, Marc Mosrin, David Wilcke, Matthieu Willot, Kerstin Ilg, Ulrich Goergens, Andreas Turberg
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Patent number: 10487092Abstract: The present invention relates to substituted pyrazolopyridinamine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and/or angiogenesis disorder, inflammatory disease and disease associated with inflammatory pain, as a sole agent or in combination with other active ingredients.Type: GrantFiled: December 14, 2015Date of Patent: November 26, 2019Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Anja Giese, Ulrich Klar, Keith Graham, Georg Kettschau, Detlev Sülzle, Philip Lienau, Kirstin Petersen, Julien LeFranc, Nicole Schmidt
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Patent number: 10471005Abstract: Present invention relates to a low dose pharmaceutical composition, preferably oral composition comprising therapeutically effective amount of [(2-hydroxy-4-oxo-6,7,8,9-tetrahydro-4H,5H-10-thia-1,4a-diaza-benzo[a]azulene-3-carbonyl)-amino]-acetic acid (compound A) in the range of 2.5 mg to 60 mg. Present invention also relates to a method of treating inflammatory bowel disease in a mammal by administrating said low dose pharmaceutical composition. Further, present invention relates to a use of the compound A for the preparation of low dose pharmaceutical composition for the treatment of inflammatory bowel disease in a mammal.Type: GrantFiled: February 22, 2017Date of Patent: November 12, 2019Assignee: Torrent Pharmaceuticals LimitedInventors: Chaitanya Dutt, Vijay Chauthaiwale, Ram Gupta, Shitalkumar Zambad, Shailesh Deshpande, Jignesh Kotecha, Ramesh Gupta, Sanjay Srivastava, Laxmikant Chhipa, Jaya Abraham
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Patent number: 10414769Abstract: The present invention encompasses compounds of formula (I) wherein the groups A, R and q are defined in claim 1, their use as inhibitors of IGF-1R, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.Type: GrantFiled: May 10, 2016Date of Patent: September 17, 2019Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Treu, Stephan Karl Zahn
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Patent number: 10357508Abstract: In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid prodrug (e.g., galangin prodrug).Type: GrantFiled: March 15, 2013Date of Patent: July 23, 2019Assignee: BUCK INSTITUTE FOR RESEARCH ON AGINGInventors: Varghese John, Dale E. Bredesen
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Patent number: 10253044Abstract: The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.Type: GrantFiled: February 27, 2017Date of Patent: April 9, 2019Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Yujun Zhao, Bing Zhou, Angelo Aguilar, Liu Liu, Longchuan Bai, Donna McEachern, Duxin Sun, Bo Wen, Ruijuan Luo, Ting Zhao, Arul Chinnaiyan, Irfan A. Asangani, Jeanne Stuckey, Jennifer Lynn Meagher, Xu Ran, Yang Hu
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Patent number: 10226464Abstract: The present invention provides, inter alia, compounds capable of inhibiting NF-?B. Pharmaceutical compositions containing and methods of using the compounds are also provided herein.Type: GrantFiled: December 29, 2016Date of Patent: March 12, 2019Assignee: ImmuneTarget, Inc.Inventors: Samedy Ouk, Hsiou-Chi Liou
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Patent number: 10179790Abstract: A compound of formula I, (I) or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer.Type: GrantFiled: June 4, 2015Date of Patent: January 15, 2019Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNINGInventors: Martin Scobie, Olov Wallner, Tobias Koolmeister, Karl Sven Axel Vallin, Carl Martin Henriksson, Sylvain Jacques, Evert Homan, Thomas Helleday
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Patent number: 10166271Abstract: This disclosure reveals that cyclic corticotrophin releasing factor (CRF) antagonist peptides (such as astressin B, its functional fragments, and their derivatives) induce hair growth and prevent hair loss in vivo. This important discovery enables, for instance, methods of promoting hair growth, and methods of treating hair loss (such as the hair loss that occurs normally in some individuals or that is the result of a health disorder or therapeutic treatment). Exemplary cyclic CRF antagonist peptides useful in the disclosed methods are provided throughout the disclosure.Type: GrantFiled: June 20, 2007Date of Patent: January 1, 2019Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, SALK INSTITUTE FOR BIOLOGICAL STUDIESInventors: Million Mulugeta, Lixin Wang, Yvette Taché, Jean Rivier
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Patent number: 10149852Abstract: The present disclosure describes the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogs/derivatives as well as their acceptable salts, for treating neuropathic pain resulting from chemotherapy. Methods, compositions, dose units and dose forms of tetrodotoxin related to the use are described.Type: GrantFiled: September 16, 2016Date of Patent: December 11, 2018Assignee: WEX PHARMACEUTICALS INC.Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Jose Manuel Baeyens, Susan Lu, Donald Wong, Walter Korz
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Patent number: 10085991Abstract: The present invention is directed to formulations comprising PVP polymer, a dispersion of a compound of Formula I (API), and citric acid, which formulations mitigate the effects of coadministering the compound of Formula I with a proton pump inhibitor compound.Type: GrantFiled: December 1, 2015Date of Patent: October 2, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Lei Zhu, Yvonne Cegielnik, Qun Lu
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Patent number: 10005789Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), according to Formula I, below, wherein R1, R2, R3 and R4 are as defined herein, useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.Type: GrantFiled: August 6, 2015Date of Patent: June 26, 2018Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
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Patent number: 9981921Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.Type: GrantFiled: December 16, 2016Date of Patent: May 29, 2018Assignee: ArQule, Inc.Inventors: Craig Bates, David P. Reed
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Patent number: 9968574Abstract: The present invention provides, among other things, therapeutic compositions and methods that can effectively treat, slow or prevent a neurological disease (e.g., a neurodegenerative disease, e.g., mild cognitive impairment (MCI) or Alzheimer's disease (AD)), in particular, based on therapeutically effective amount of nifedipine, oxidized or nitroso nifedipine derivatives, lactam (e.g., a compound of formula (Ic) or (Ic-i), e.g., NFD-L1), thyroxine (T4), triiodothyronine (T3) and combinations thereof.Type: GrantFiled: November 18, 2010Date of Patent: May 15, 2018Assignee: The University of Kentucky Research FoundationInventors: Mark Lovell, Bert Lynn
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Patent number: 9896455Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: GrantFiled: August 22, 2016Date of Patent: February 20, 2018Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 9802955Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: GrantFiled: October 3, 2016Date of Patent: October 31, 2017Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 9790234Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.Type: GrantFiled: September 27, 2016Date of Patent: October 17, 2017Assignee: NIMBUS IRIS, INC.Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Patent number: 9717903Abstract: Methods to restore and/or improve the libido, the sex drive, in males and females, without introducing any external unnatural drugs. The process utilizes a TENS/EMS (Transcutaneous Electrical Nerve Stimulation/Electronic Muscle Stimulation) machine to naturally generate the increased production by the human body's nerve fiber's neurotransmitters.Type: GrantFiled: March 17, 2015Date of Patent: August 1, 2017Inventor: Gary Barrett
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Patent number: 9708332Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4 and n are defined herein, are useful as inhibitors of RSV.Type: GrantFiled: October 29, 2013Date of Patent: July 18, 2017Assignee: MEDIVIR ABInventors: Claudio Sturino, Teddy Halmos, Anne Decor, Martin Duplessis, Patrick Deroy, Araz Jakalian, Louis Morency, Cyrille Kuhn, Chantal Grand-Maitre, Martin Tremblay, Christian Brochu
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Patent number: 9695135Abstract: The invention provides compounds of formula I: and salts thereof wherein R1-R4 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts, and methods for their use in therapy. The compounds have useful antiviral properties.Type: GrantFiled: May 11, 2015Date of Patent: July 4, 2017Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Eddy Arnold, Joseph D. Bauman, John E. Kerrigan, Ajit K. Parhi, Kalyan Das, Cody Kelley, Dishaben V. Patel
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Patent number: 9649302Abstract: The present disclosure relates to pharmaceutical compositions useful for (and to a method of) treating autoimmune, respiratory and/or inflammatory diseases and conditions. The method involves administering to a subject in need thereof roflumilast N-oxide by inhalation. The present disclosure particularly relates to the treatment of asthma and chronic obstructive pulmonary disease (COPD) by administering roflumilast N-oxide by inhalation.Type: GrantFiled: January 28, 2014Date of Patent: May 16, 2017Assignee: INCOZEN THERAPEUTICS PVT. LTD.Inventor: Swaroop K. Vakkalanka
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Patent number: 9636342Abstract: The invention provides a method for treating prostate cancer in a subject comprising administering to the subject an effective amount of a selective inhibitor of one or more of CDK8 and CDK19. In some embodiments the inhibitor inhibits CDK19. In some embodiments, the inhibitor inhibits CDK8 at a Kd of lower than 200 nM and/or inhibits CDK19 at a Kd of lower than 100 nM. In some embodiments, the prostate cancer is androgen independent. In some embodiments, the prostate cancer is androgen independent due to one or more of androgen receptor gene amplification, androgen receptor gene mutation, ligand-independent transactivation of androgen receptor and activation of intracellular androgen synthesis. In some embodiments, the inhibitor inhibits increased activity of NF-?B. In some embodiments, the inhibitor does not inhibit increased basal levels of NF-?B. In some embodiments, inhibition of one or more genes by AR is not inhibited.Type: GrantFiled: November 1, 2013Date of Patent: May 2, 2017Assignee: University of South CarolinaInventors: Mengqian Chen, Igor Roninson
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Patent number: 9604937Abstract: A compound of formula (I), or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1.Type: GrantFiled: November 26, 2013Date of Patent: March 28, 2017Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNINGInventors: Martin Scobie, Thomas Helleday, Tobias Koolmeister, Sylvain Jacques
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Patent number: 9585885Abstract: [Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D2 receptors. [Solution] The present invention provides a compound represented by the general formula (I): in which R1 is C1-6 alkyl or the like; R2 is hydrogen or the like; R3 and R4 are each hydrogen, C1-6 alkyl, R10R11N—C1-6 alkyl, aralkyl, or the like; R5 and R6 are hydrogen or the like; and R7 is hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine D2 receptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.Type: GrantFiled: December 6, 2013Date of Patent: March 7, 2017Assignee: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Toshihiro Nishimura, Yasunori Ueno, Kiyoshi Kasai, Masako Yoshida
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Patent number: 9556187Abstract: This disclosure relates to novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities. A tricyclic heterocyclic compound represented by the formula (Ib), wherein the rings Ab and Bb, Xb, Yb, R1b, R2b, R3b, L1b, L2b, L3b and nb are as defined in the specification.Type: GrantFiled: October 2, 2015Date of Patent: January 31, 2017Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
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Patent number: 9504688Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).Type: GrantFiled: May 2, 2013Date of Patent: November 29, 2016Assignees: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, THE CURATORS OF THE UNIVERSITY OF MISSOURIInventors: David Ginsburg, Scott D. Larsen, Bryan Yestrepsky, Hongmin Sun
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Patent number: 9505756Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: GrantFiled: February 6, 2015Date of Patent: November 29, 2016Assignee: HYDRA BIOSCIENCES, INC.Inventors: Xinyuan Wu, Spencer David Kimball, Ping Chen, Ding Zhou, Shaoping Peng
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Patent number: 9422297Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: GrantFiled: September 25, 2014Date of Patent: August 23, 2016Assignee: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Patent number: 9415005Abstract: This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.Type: GrantFiled: March 13, 2013Date of Patent: August 16, 2016Assignee: VeroScience LLCInventor: Anthony H. Cincotta
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Patent number: 9403778Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides dermatological compositions comprising a compound of formula I or mixtures of one or more compounds of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for protecting skin or DNA from photodamage or repairing photodamaged skin or DNA.Type: GrantFiled: January 11, 2013Date of Patent: August 2, 2016Assignee: Regents of the University of MinnesotaInventors: Robert Vince, Abbas Raza, Christine Dreis
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Patent number: 9402830Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.Type: GrantFiled: May 1, 2015Date of Patent: August 2, 2016Assignee: Melior Discovery, Inc.Inventors: John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
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Patent number: 9382287Abstract: Methods are provided for using methotrexate (MTX) active agents in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of an MTX active agent in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2?-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions and kits that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.Type: GrantFiled: October 6, 2014Date of Patent: July 5, 2016Assignee: Tosk, Inc.Inventors: William A. Garland, Brian D. Frenzel, Travis Karg
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Patent number: 9365575Abstract: The present invention relates to compounds of Formula I or a pharmaceutically acceptable salt thereof, wherein variables R, Ar, X, and Ar1 and n are as defined herein. The compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: May 20, 2013Date of Patent: June 14, 2016Assignee: Allergan, Inc.Inventors: Thomas C. Malone, Julie A. Wurster, Clarence Eugene Hull, III
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Patent number: 9359370Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.Type: GrantFiled: July 31, 2014Date of Patent: June 7, 2016Assignee: Beta Pharma, Inc.Inventors: Yinxiang Wang, Guojian Xie, Lieming Ding, Fenlai Tan, Yunyan Hu, Wei He, Bin Han, Wei Long, Yong Liu, Haima Ai, Charles Davis, Don Zhang
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Patent number: 9303035Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: December 17, 2013Date of Patent: April 5, 2016Assignee: Novartis AGInventors: Mahbub Ahmed, Alexander Ashall-Kelly, Graham Charles Bloomfield, Louisa Gueritz, Jeffrey McKenna, Joseph McKenna, Simon Mutton, Rakesh Parmar, Jon Sheperd, Paul Wright
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Patent number: 9301958Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.Type: GrantFiled: June 4, 2012Date of Patent: April 5, 2016Assignee: Phytotox LimitedInventor: Nestor Antonio Lagos Wilson
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Patent number: 9284318Abstract: The present invention relates to novel kinase inhibitors. Compounds of this class have been found to be effective inhibitors of protein kinases, including members of PDGFR and VEGFR families.Type: GrantFiled: April 3, 2012Date of Patent: March 15, 2016Assignee: Pharmascience, Inc.Inventors: Alain Laurent, Yannick Rose, Stephen Morris, James Jaquith
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Patent number: 9284335Abstract: Described herein are compounds and chemical entities of Formula (I), methods of their synthesis, compositions comprising them, and their use in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.Type: GrantFiled: June 18, 2013Date of Patent: March 15, 2016Assignee: Dart NeuroScience (Cayman) Ltd.Inventors: Amy Allan, Bryan Branstetter, Brian Dyck, Laurent Gomez, Tami Jo Marrone, Marco Peters, Michael I. Weinhouse
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Patent number: 9260452Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: GrantFiled: June 8, 2012Date of Patent: February 16, 2016Assignee: Sunovion Pharmaceuticals Inc.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Patent number: 9227979Abstract: Disclosed are compounds of the formula (I) which are fluorescently labeled antagonists of the A3 adenosine receptor: wherein A, R1, R2, and Y are as described herein. Also disclosed are diagnostic compositions and a method of diagnosis of a patient for a possible treatment by an antagonist of the A3 adenosine receptor, involving the use of one or more of these compounds as diagnostic agents.Type: GrantFiled: January 24, 2013Date of Patent: January 5, 2016Assignees: The United States of America, as represented by The Secretary, Department of Health and Human Services, Universita Degli Studi Di Trieste, Universita Degli Studi Di PadovaInventors: Kenneth A. Jacobson, Santhosh Kumar Thatikonda, Eszter Erika Kozma, Giampiero Spalluto, Stefano Moro, Stephanie Federico
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Patent number: 9181269Abstract: The present invention discloses novel enantiomeric antifungal compounds of Formula (1a) and Formula (1b) containing thieno-[2,3-d]Jpyrimidin-4(3H)-one moiety and pharmaceutically acceptable salts thereof, method of preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these compounds.Type: GrantFiled: May 31, 2011Date of Patent: November 10, 2015Assignees: FDC Limited, Council for Scientific & Industrial ResearchInventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmeshwer Prabhkara Sawargave, Subhash Prataprao Chavan, Mohan Anand Chandavarkar, Ramkrishnan Ramachandran Iyer, Vikas Vasant Nawathye, Gajanan Jalindar Chavan, Amit Chandrakant Tawte, Deepali Damodar Rao
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Patent number: 9173846Abstract: This invention provides novel solid pharmaceutical compositions and processes for the bulk production of said compositions. This invention also provides methods of using the pharmaceutical compositions in the treatment of cancer.Type: GrantFiled: May 14, 2010Date of Patent: November 3, 2015Assignee: MILLENNIUM PHARMACEUTICALS, INC.Inventor: Bhavishya Mittal
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Patent number: 9163022Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to rheumatoid arthritis.Type: GrantFiled: September 4, 2014Date of Patent: October 20, 2015Assignee: vTv Therapeutics LLCInventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel