Ring Nitrogen Shared By Two Of The Cyclos Patents (Class 514/233.2)
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Patent number: 10849901Abstract: Disclosed herein are compounds and methods for inhibiting Arf6. Pharmaceutical compositions and methods for treating a subject with an inhibitor of Arf6 are also disclosed herein.Type: GrantFiled: May 27, 2015Date of Patent: December 1, 2020Assignees: Navigen, Inc., The University of Utah Research FoundationInventors: Kirill Ostanin, Mark Shenderovich, Ashok Bajji, Christopher L. Cioffi, Neil Moss, Hariprasad Vankayalapati, Dean Li
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Patent number: 10821103Abstract: The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.Type: GrantFiled: November 3, 2017Date of Patent: November 3, 2020Assignee: Arbutus Biopharma CorporationInventors: Laurèn Danielle Bailey, Yingzhi Bi, Shuai Chen, Bruce D. Dorsey, Dimitar B. Gotchev, Richard James Holland, Ramesh Kakarla, Duyan Nguyen, Mark Christopher Wood
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Patent number: 10822352Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.Type: GrantFiled: March 12, 2019Date of Patent: November 3, 2020Assignee: Achillion Pharmaceuticals, Inc.Inventors: Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang
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Patent number: 10765687Abstract: A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.Type: GrantFiled: March 22, 2019Date of Patent: September 8, 2020Assignees: Northwestern University, THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORKInventors: Jonathan Leis, Carol Carter
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Patent number: 10759794Abstract: The present application relates to novel 2-phenyl-3-(piperazinomethyl)imidazo[1,2-a]pyridine derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of respiratory disorders including, sleep-related respiratory disorders such as obstructive sleep apnoeas and central sleep apnoeas and snoring.Type: GrantFiled: December 7, 2016Date of Patent: September 1, 2020Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Martina Delbeck, Michael Hahn, Thomas Müller, Heinrich Meier, Klemens Lustig, Johanna Mosig, Luisella Toschi, Udo Albus, Doris Gehring, Björn Rosenstein
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Patent number: 10752622Abstract: The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.Type: GrantFiled: December 24, 2018Date of Patent: August 25, 2020Assignee: MANKIND PHARMA LTD.Inventors: Rakesh Ishwar Patil, Jeevan Verma, Puneet Kumar, Amol Pandurang Gunjal, Himanshu Rai, Santosh Kumar Rai, Anil Kumar
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Patent number: 10738056Abstract: The present invention relates to pyrazolopyrimidinone compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating autoimmune, inflammatory, and neurodegenerative diseases by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: September 14, 2018Date of Patent: August 11, 2020Assignee: Aduro BioTech Inc.Inventors: Chudi Obioma Ndubaku, George Edwin Katibah, Tucker Curran Roberts, Leonard Sung, Stephane Ciblat, Franck Raeppel, Vu Linh Ly, Yeeman K. Ramtohul, Taras Rybak, Mariam Zaky, Laura Gillard, Hossein Ismaili
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Patent number: 10653695Abstract: Disclosed are oral pharmaceutical compositions of neflamapimod that exhibit suitable exposure for administration in humans and/or that maintain a desirable dissolution profile under standard storage conditions.Type: GrantFiled: March 12, 2019Date of Patent: May 19, 2020Assignee: EIP Pharma, LLCInventors: John Jahangir Alam, Jeffrey Douglas Wilson
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Patent number: 10568879Abstract: A compound according to Formula I: wherein R1, LA, CyA, RA, R2, R3, and R4 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions, pain, neuroinflammatory conditions, neurodegenerative conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, cardiovascular diseases, leukemia, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.Type: GrantFiled: April 19, 2016Date of Patent: February 25, 2020Assignee: GALAPAGOS NVInventors: Christel Jeanne Marie Menet, Julien Georges Pierre-Olivier Doyon, Pieter Isabelle Roger Claes, Brigitte Allart, Maxim Maria Paul De Wachter, Giovanni Alessandro Tricarico
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Patent number: 10556869Abstract: The present invention relates to a process for providing the compound of formula I, comprising the step of reacting a compound of formula VII with a base in the presence of an alkaline- or alkaline earth metal salt (MX), wherein LG is a leaving group. The presence of an alkaline- or alkaline earth metal salt was surprisingly found to render said reaction highly reliable in terms of the yield and purity of the compound of formula I obtained. In a further aspect, the present invention relates to the compound of formula I, having less than an amount of 1.50% or less than an amount of 1.25% or less than an amount of 1.00% or less than an amount of 0.75% or less than an amount of 0.50% or less than an amount of 0.25% or less than an amount of 0.10% of the compound of formula VIII.Type: GrantFiled: January 28, 2016Date of Patent: February 11, 2020Assignee: Novartis AGInventors: Andreas Bertogg, Hanspeter Schilling
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Patent number: 10457683Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.Type: GrantFiled: April 12, 2018Date of Patent: October 29, 2019Assignee: Magenta Therapeutics Inc.Inventor: Arthur Glenn Romero
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Patent number: 10399995Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, useful as a BACE1 inhibitor.Type: GrantFiled: August 18, 2017Date of Patent: September 3, 2019Assignee: Eli Lilly and CompanyInventors: Steven James Green, Erik James Hembre, II, Dustin James Mergott
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Patent number: 10364245Abstract: Compounds of formula (I) defined herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: GrantFiled: May 23, 2018Date of Patent: July 30, 2019Assignee: CHIESI FARMACEUTICI S.p.A.Inventors: Carmelida Capaldi, Elisabetta Armani, Christopher Hurley, Barbara Giuseppina Avitabile-Woo, Roberta Lanaro, Neil Stuart Jennings
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Patent number: 10351572Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.Type: GrantFiled: February 8, 2019Date of Patent: July 16, 2019Assignee: Magenta Therapeutics Inc.Inventor: Arthur Glenn Romero
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Patent number: 10342795Abstract: The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives of formula (I) and also compounds of formula (I?) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS1 inhibitors. The invention further relates to processes for preparing novel compounds of the present invention, pharmaceutical compositions comprising compounds of the present invention as an active ingredient as well as the use of compounds of the present invention as a medicament.Type: GrantFiled: March 26, 2015Date of Patent: July 9, 2019Assignee: Janssen Pharmaceutica NVInventors: Laurence Anne Mevellec, Matthieu Ludovic Jeanty, Thierry Francois Alain Jean Jousseaume
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Patent number: 10335411Abstract: Disclosed are methods for the treatment of cancer in patients in need of such treatment. The methods comprise administering to such a patient an ubiquitin-activating enzyme (UAE) inhibitor such as ((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(3-(trifluoromethylthio) phenyl)pyrazolo[1,5-a]pyrimidin-7-ylamino)cyclopentyl)methyl sulfamate (Compound 1) or a pharmaceutically acceptable salt in combination with radiation. Also disclosed are medicaments for use in the treatment of cancer.Type: GrantFiled: October 23, 2015Date of Patent: July 2, 2019Assignee: Millennium Pharmaceuticals, Inc.Inventors: Neil Bence, Marc Hyer, Michael Milhollen, Vivek Samnotra, Sergio Luis Santillana Soto, Darshan Sappal
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Patent number: 10328066Abstract: The present disclosure pertains to a pharmaceutical combination comprising (a) an alpha-isoform specific PI3K inhibitor, (b) a cyclin dependent kinase 4/6 (CDK4/6) inhibitor, and (c) an antimetabolite antineoplastic agent; combined preparations and pharmaceutical compositions thereof; the uses of such a combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.Type: GrantFiled: August 24, 2016Date of Patent: June 25, 2019Assignee: Novartis AGInventors: Giordano Caponigro, Thomas Horn-Spirohn, Joseph Lehar
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Patent number: 10258615Abstract: The present invention provides a method of treating or ameliorating a neurodegenerative disease in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a neurodegenerative disease drug, wherein the drug is a substrate of an ABC transporter inhibitor, wherein the mammal is further administered a therapeutically effective amount of an ABC transporter inhibitor, whereby the neurodegenerative disease is treated in the mammal. In certain embodiments, the neurodegenerative disease comprises at least one selected from the group consisting of spinal cord injury, Alzheimer's disease, Parkinson's disease, Huntington's disease, prion disease, amyotrophic lateral sclerosis, a tauopathy, and chronic traumatic encephalopathy.Type: GrantFiled: December 9, 2014Date of Patent: April 16, 2019Assignee: Thomas Jefferson UniversityInventors: Davide Trotti, Piera Pasinelli, Michael R. Jablonski
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Patent number: 10253043Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.Type: GrantFiled: June 21, 2013Date of Patent: April 9, 2019Assignee: SANOFIInventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
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Patent number: 10208030Abstract: The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.Type: GrantFiled: April 4, 2017Date of Patent: February 19, 2019Assignee: Mankind Pharma Ltd.Inventors: Rakesh Ishwar Patil, Jeevan Verma, Puneet Kumar, Amol Pandurang Gunjal, Himanshu Rai, Santosh Kumar Rai, Anil Kumar
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Patent number: 10189840Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: (i) —(CR3R3)1-4—; (ii) —(CR3R3)x—Y—(CR3R3)y—; Or (iii) —Y—(CR3R3)2—Y—; and Y, R1, R2, R3, R5, R6, R8, x, and y are defined herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.Type: GrantFiled: March 17, 2016Date of Patent: January 29, 2019Assignee: Bristol-Myers Squibb CompanyInventors: Hai-Yun Xiao, Murali T. G. Dhar, Jingwu Duan, Bin Jiang, Andrew J. Tebben
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Patent number: 10160991Abstract: Disclosed herein are methods determining susceptibility of bacteria in a sample from a subject suspected of having an infection to a plurality of antibiotics simultaneously, wherein the sample is tested without first isolating the bacteria from the sample.Type: GrantFiled: April 19, 2018Date of Patent: December 25, 2018Assignee: CAP DIAGNOSTICS, LLCInventors: David A. Baunoch, Miguel F. R. Penaranda, Michael L. Opel, Maher Badir
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Patent number: 10131673Abstract: The invention concerns novel substituted tricyclic pyrazolo pyrimidine compounds of formula (I-a) or (I-b) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.Type: GrantFiled: December 7, 2015Date of Patent: November 20, 2018Assignee: Janssen Sciences Ireland UCInventors: Abdellah Tahari, Sandrine Marie Helene Vendeville, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Samuël Dominique Demin, Lili Hu
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Patent number: 10125123Abstract: Described herein are IRE1? inhibitors, compositions containing such inhibitors, and methods of treatment that include administration of such compounds. Exemplary compounds are provided throughout the application.Type: GrantFiled: March 3, 2017Date of Patent: November 13, 2018Assignee: CORNELL UNIVERSITYInventors: Laurie H. Glimcher, Sarah Elizabeth Bettigole, Juan Rodrigo Cubillos Ruiz, Joseph P. Vacca
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Patent number: 10112944Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CR6 or N; W is: (i) —(CR3R3)1-4— or (ii) —(CR3R3)x-Y—(CR3R3)y-; and Y, R1, R2, R3, R5, R6, R7, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.Type: GrantFiled: March 17, 2016Date of Patent: October 30, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Lawrence R. Marcin, Stephen T. Wrobleski, T.G. Murali Dhar
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Patent number: 10100059Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.Type: GrantFiled: December 9, 2016Date of Patent: October 16, 2018Assignee: Research Triangle InstituteInventors: Scott P. Runyon, Rangan Maitra, Sanju Narayanan, James Barnwell Thomas, Kenneth S. Rehder, Srinivas Olepu
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Patent number: 10085992Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.Type: GrantFiled: November 3, 2016Date of Patent: October 2, 2018Assignee: G1 Therapeutics, Inc.Inventors: Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
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Patent number: 10076523Abstract: This invention is in the area of improved compounds for and methods of treating selected RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, improved treatment of select RB-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as highly selective and, in certain embodiments, short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.Type: GrantFiled: December 21, 2016Date of Patent: September 18, 2018Assignee: G1 Therapeutics, Inc.Inventors: Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
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Patent number: 10053464Abstract: A series of substituted [1,2,4]triazolo[4,3-b]pyridazine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: December 8, 2014Date of Patent: August 21, 2018Assignee: UCB BIOPHARMA SPRLInventor: Daniel Christopher Brookings
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Patent number: 9988365Abstract: Provided herein are 2-(2,4-difluorophenyl)-1,1-difluoro-1-(5-substituted-pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ols and 1-(2,4-difluorophenyl)-2,2-difluoro-2-(5-substituted-pyridin-2-yl)ethanones and processes for their preparation.Type: GrantFiled: March 19, 2015Date of Patent: June 5, 2018Assignee: VPS-3, Inc.Inventors: William J. Hoekstra, Nakyen Choy, Carl DeAmicis, Daniel Knueppel, Jim Renga, Michael T. Sullenberger, Gregory Whiteker, Yuanming Zhu, Gary D. Gustafson
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Patent number: 9980982Abstract: The invention provides compositions and methods for utilizing human epididymal secretion protein E4 (HE4) in the prevention and treatment of cancer and other human diseases.Type: GrantFiled: June 6, 2012Date of Patent: May 29, 2018Assignee: Women & Infants Hospital of Rhode IslandInventors: Richard G. Moore, Rakesh K. Singh
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Patent number: 9931345Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.Type: GrantFiled: October 7, 2016Date of Patent: April 3, 2018Assignee: Presidents and Fellows of Harvard CollegeInventors: Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
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Patent number: 9932334Abstract: A series of substituted 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine derivatives, being potent treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: December 8, 2014Date of Patent: April 3, 2018Assignee: UCB BIOPHARMA SPRLInventors: Victoria Elizabeth Jackson, Boris Kroeplien, Martin Alexander Lowe, John Robert Porter
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Patent number: 9902727Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: GrantFiled: November 25, 2014Date of Patent: February 27, 2018Assignee: Bayer Intellectual Property GmbHInventors: William Scott, Ningshu Liu, Manfred Möwes, Andrea Hägebarth, Ursula Mönning, Ulf Bömer
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Patent number: 9902723Abstract: The present invention provides a method for manufacturing a compound represented by formula (I). With this method, provided is a method for manufacturing a 4-substituted-N-(2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1H-pyrazole-5-carboxylic acid amide derivative; or an intermediate for this manufacturing method.Type: GrantFiled: July 29, 2015Date of Patent: February 27, 2018Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Tsutomu Satoh, Takashi Kudoh, Tetsuo Iwama
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Patent number: 9896459Abstract: Azaindoles having inhibitory activity on RSV replication and having the formula I compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: May 12, 2016Date of Patent: February 20, 2018Assignee: Janssen Sciences Ireland UCInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 9879009Abstract: The present invention provides a method for manufacturing a compound represented by formula (I). With this method, provided are a method for manufacturing a 4-heteroaryl-N-(2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1H-pyrazole-5-carboxylic acid amide derivative; and an intermediate for this manufacturing method.Type: GrantFiled: July 29, 2015Date of Patent: January 30, 2018Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Tsutomu Satoh, Takashi Kudoh, Tetsuo Iwama
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Patent number: 9850240Abstract: A series of substituted [1,2,4]triazolo[4,3-a]pyridine derivatives, being potent modulators of human TNF activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: December 8, 2014Date of Patent: December 26, 2017Assignee: UCB BIOPHARMA SPRLInventors: Daniel Christopher Brookings, Victoria Elizabeth Jackson
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Patent number: 9828350Abstract: The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.Type: GrantFiled: February 5, 2016Date of Patent: November 28, 2017Assignee: Janssen Pharmaceutica NVInventors: Andrés Avelino Trabanco-Suárez, Frederik Jan Rita Rombouts, Gary John Tresadern, Michiel Luc Maria Van Gool, Gregor James Macdonald, Carolina Martinez Lamenca, Henricus Jacobus Maria Gijsen
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Patent number: 9801961Abstract: The present invention relates to compounds of general formula wherein R1 is (a) phenyl, optionally substituted by one or two substituents selected from 3H, halogen, lower alkyl, di-methyl-amino, NHC(O)-lower alkyl, C(O)O-lower alkyl, lower alkoxy, OC(3H)3, O11CH3, OCH2CH218F, lower alkoxy substituted by halogen, hydroxy, lower alkyl substituted by hydroxy, S-lower alkyl, (b) heterocyclyl group, (c) benzo[d][1,3]dioxol-5-yl, (d) 2,3-dihydrobenzo[b][1,4]dioxin-6-yl, (e) indolin-2-one, or (f) heteroaryl, selected from the group consisting of thiophenyl, benzofuranyl, benzothiophenyl, pyrazinyl, and benzothiazolyl; R2 is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3 is lower alkyl, C(3H)3, 11CH3, lower alkyl substituted by halogen, —(CH2)2—O-lower alkyl substituted by halogen or cycloalkyl; or R2 and R3 form together with the N-atom to which they are attach a ring containing —CH2CH2CHRCH2CH2—, —CH2CH2CHRCH2—, —CH2CHRCH2—, —CH2CH2—NR—CH2CH2—, —CH2CH2—O—CH2CH2—, or, R is hydrogen, halogType: GrantFiled: November 19, 2015Date of Patent: October 31, 2017Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Henner Knust, Matthias Koerner, Dieter Muri
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Patent number: 9789087Abstract: Disclosed herein are methods for determining whether a PAR4 inhibitor should be administered to a human subject, the methods comprising administering a PAR4 inhibitor to a subject determined to have a “G” allele for a single-nucleotide polymorphism (SNP) at rs773902, and not administering a PAR4 inhibitor to a subject determined to have an “A” allele for the SNP at rs773902. A genotyping assay can be used to determine the SNP.Type: GrantFiled: August 2, 2016Date of Patent: October 17, 2017Assignee: THOMAS JEFFERSON UNIVERSITYInventors: Paul Bray, Michael Holinstat, Leonard Edelstein
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Patent number: 9783543Abstract: The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I), in which A, R1, R2, R3, R4 and n are as defined in the claims, 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 hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: GrantFiled: November 14, 2013Date of Patent: October 10, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ludwig Zorn, Knut Eis, Volker Schulze, Detlev Sülzle, Florian Puehler, Philip Lienau, Ulf Bömer, Kirstin Petersen, Andrea Hägebarth
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Patent number: 9745304Abstract: The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): in which A, R1, R2, R3, R4 and n are as defined in the claims, 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 hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: GrantFiled: January 28, 2014Date of Patent: August 29, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ludwig Zorn, Knut Eis, Volker Schulze, Detlev Sülzle, Florian Puehler, Philip Lienau, Ulf Bömer, Kirstin Petersen, Andrea Hägebarth
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Patent number: 9708312Abstract: A compound according to Formula (Ia), wherein Cy, L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula (I) that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis), lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.Type: GrantFiled: December 17, 2013Date of Patent: July 18, 2017Assignee: GALAPAGOS NVInventors: Frédéric Gilbert Labéguère, Gregory John Robert Newsome, Luke Jonathan Alvey, Laurent Raymond Maurice Sanière, Stephen Robert Fletcher
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Patent number: 9682992Abstract: The subject of the present invention are water-soluble derivatives of camptothecin, their synthesis and use. These compounds exhibit preferable biological properties for use in anti-neoplasm therapy.Type: GrantFiled: October 25, 2013Date of Patent: June 20, 2017Assignees: INSTYTUT CHEMII ORGANICZNEJ POLSKIEJ AKADE, NARODOWY INSTYTUT LEKÓWInventors: Lech Kozerski, Robert Kawęcki, Beata Naumczuk, Karolina Hyz, Wojciech Bocian, Jerzy Sitkowski, Elżbieta Bednarek, Katarzyna Wiktorska, Katarzyna Lubelska
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Patent number: 9675549Abstract: Provided herein is a tablet comprising, as a drug, N-(5-tert-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea or a pharmaceutically acceptable salt thereof, which is a medicament for treating acute myeloid leukemia (AML), the tablet characterized by comprising a composite of N-(5-tert-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea or a pharmaceutically acceptable salt thereof and hydroxypropyl-?-cyclodextrin in a ratio ranging from 1:8 to 1:20.Type: GrantFiled: September 30, 2013Date of Patent: June 13, 2017Assignee: Ambit Biosciences CorporationInventors: Shinsuke Oba, Hiroyasu Toyota, Satomi Ikeuchi, Takumi Hara, Emiko Murayama, Kei Motonaga
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Patent number: 9669035Abstract: The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE10). In particular, the invention relates to combinations of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051324 and in WO 2011/110545.Type: GrantFiled: June 25, 2013Date of Patent: June 6, 2017Assignee: JANSSEN PHARMACEUTICA NVInventors: Antonius Adrianus Hendrikus Petrus Megens, Xavier Jean Michel Langlois, José Ignacio Andrés-Gil
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Patent number: 9649317Abstract: The present invention is directed to triazolopyrimidine, phenylpyrimidine, pyridopyridazine, and pyridotriazine compounds which are microtubule-stabilizing compounds and their use in the treatment of neurodegenerative disorders, in particular, tauopathies, such as for example, Alzheimer's disease, frontotemporal lobar degeneration, Pick's disease, progressive supranuclear palsy (PSP), and corticobasal degeneration. In addition, the compounds of the invention may be useful for other diseases where tau pathology is a comorbidity or where microtubule function is compromised, for example, schizophrenia, Parkinson's disease (PD), PD with dementia, Lewy body disease with dementia, and amyotrophic lateral sclerosis.Type: GrantFiled: September 19, 2013Date of Patent: May 16, 2017Assignee: The Trustees of the University of PennsylvaniaInventors: Carlo Ballatore, Kurt R. Brunden, Adam T. Hoye, Virginia M. Y. Lee, Amos B. Smith, John Q. Trojanowski
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Patent number: 9550771Abstract: Compounds of the formula I or II: or pharmaceutically acceptable salts thereof, wherein R1 is a group of formula (a), (b), (c); (d) or (e): and m, n, X, Y, R1, R2, R3, R4, Rb and Rc are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: GrantFiled: September 10, 2014Date of Patent: January 24, 2017Assignee: Genentech, Inc.Inventors: Benjamin Fauber, Alberto Gobbi
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Patent number: 9518240Abstract: A method for treating liquefied hydrocarbons including acid gases to remove said acid gases while minimizing loss of amine species, he method comprising the step of contacting he liquefied hydrocarbons with an absorbent aqeuous solution of a first amine compound, the first amine compound having the structure: wherein R1 is hydrogen or propane-2,3-diol and R2 is propane-2,3-diol, or mixtures thereof.Type: GrantFiled: June 11, 2013Date of Patent: December 13, 2016Assignee: Dow Global Technologies LLCInventors: Christophe R. Laroche, James M. Hill