Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
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Patent number: 11304981Abstract: The invention concerns a pharmaceutical composition comprising a platelet lysate and its use to treat a wound, an anal fissure, vaginal atrophy or a wrinkle.Type: GrantFiled: October 19, 2018Date of Patent: April 19, 2022Assignee: Cell Therapy LimitedInventors: Thomas Averell Houze, Martin John Evans, Ajan Trevor Reginald, Ina Laura Pieper
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Patent number: 11285158Abstract: The present disclosure provides methods of increasing skin pigmentation in a subject in need thereof using salt-inducible kinase (SIK) inhibitors, such as macrocyclic compounds of Formula (I), bicyclic urea compounds of Formula (II), (III), and (IV), and compounds of Formula (V), (VI), (VI-A), or (VII). Also provided are pharmaceutical compositions, methods, and uses that include or involve a compound described herein.Type: GrantFiled: February 28, 2018Date of Patent: March 29, 2022Assignees: The General Hospital Corporation, Dana-Farber Cancer Institute, Inc.Inventors: David E. Fisher, Nisma Mujahid, Ryo Murakami, Nathanael S. Gray, Yanke Liang, Hwan Geun Choi
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Patent number: 11274108Abstract: Compounds of the formulas which are useful as colony stimulating factor-1 receptor inhibitors (“CSF-1R inhibitors”).Type: GrantFiled: July 19, 2016Date of Patent: March 15, 2022Assignee: GENZYME CORPORATIONInventors: John L. Kane, Jr., Claude Barberis, Mark Czekaj, Paul Erdman, Barret Giese, Michael Kothe, Tieu-Binh Le, Jinyu Liu, Liang Ma, Markus Metz, Vinod Patel, Andrew Scholte, Patrick Wai-Kwok Shum, Linli Wei
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Patent number: 11236105Abstract: The present invention provides compounds that modulate protein function, specifically phosphodiesterase 4 (PDE4). The invention provides methods of treating, ameliorating, and/or preventing diseases, disorders, and conditions associated with PDE4. Compositions, including in combination with other inflammatory mediators, are also provided.Type: GrantFiled: February 11, 2020Date of Patent: February 1, 2022Assignee: BioTheryX, Inc.Inventors: Robert Sullivan, Paul E. Erdman, Eduardo Torres, Leah Fung, Kyle W. H. Chan, Frank Mercurio
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Patent number: 11166943Abstract: Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect. An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).Type: GrantFiled: May 19, 2020Date of Patent: November 9, 2021Assignee: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Hiromi Muraoka, Akira Kanoh
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Patent number: 11155544Abstract: The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase (“BTK”) inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: July 26, 2019Date of Patent: October 26, 2021Assignee: Principia Biopharma Inc.Inventors: David M. Goldstein, Timothy D. Owens
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Patent number: 11110096Abstract: Provided herein are pharmaceutical compositions comprising a phosphatidylinositol 3-kinase inhibitor or a pharmaceutically acceptable form thereof, and a Bcl-2 inhibitor or a pharmaceutically acceptable form thereof. Also provided herein are methods for treating cancer comprising administration the compositions, and uses of the compositions, e.g., for the treatment of cancer.Type: GrantFiled: May 4, 2017Date of Patent: September 7, 2021Assignee: Infinity Pharmaceuticals, Inc.Inventors: Jeffery L. Kutok, Howard M. Stern
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Patent number: 11098017Abstract: The present application provides compounds useful for treating disorders associated with abnormal steroidogenesis. Methods of treating disorders associated with abnormal steroidogenesis, methods of inhibiting 11?-hydroxylase activity, and pharmaceutical compositions comprising the compounds are also provided.Type: GrantFiled: May 17, 2018Date of Patent: August 24, 2021Assignee: The General Hospital CorporationInventor: Douglas Raines
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Patent number: 11091477Abstract: Novel compounds and pharmaceutically acceptable salts capable of modulating the activity of kinases, including Akt, ERK and MEK. Such modulation affects biological functions, for example, by inhibiting cell proliferation and/or inducing apoptosis. Also provided are pharmaceutical compositions and medicaments, comprising the compounds or salts of the invention, alone or in combination with other therapeutic agents or palliative agents.Type: GrantFiled: August 14, 2017Date of Patent: August 17, 2021Assignee: Madera Therapeutics, LLCInventor: Edwin J. Iwanowicz
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Patent number: 11059817Abstract: The present technology provides compounds according to Formulas (I), (II), or (III) useful in inhibiting an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus in a cell and/or treating subjects suffering from an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus.Type: GrantFiled: September 22, 2016Date of Patent: July 13, 2021Assignee: The Regents of the University of CaliforniaInventors: Paul Krogstad, Michael E. Jung, Jun Zuo, Yanpeng Xing
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Patent number: 11046699Abstract: Disclosed herein are pyrozolo-pyrimidin-amino-cycloalkyl compounds, analogs thereof, pharmaceutical compositions comprising thereof and therapeutic uses therefor.Type: GrantFiled: June 4, 2019Date of Patent: June 29, 2021Assignee: RAPT THERAPEUTICS, INC.Inventors: Minna H. T. Bui, Adrian O. Dukes, Xinping Han, Dennis X. Hu, Jeffrey J. Jackson, Yoo Min Ko, Paul R. Leger, Anqi Ma, Jack Maung, Andrew A. Ng, Akinori Okano, Omar Robles, Grant Shibuya, Hunter P. Shunatona, Jacob B. Schwarz, Anton A. Shakhmin, David J. Wustrow, Mikhail Zibinsky
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Patent number: 11040947Abstract: A compound of Formula I: wherein: Y is —C(O)NHR1 or —NHC(O)R1; R1 is aryl; ?is ?optionally substituted with one or more substituents selected from the group consisting of oxo, F, Cl, Br, I, alkyl, NH2, NHR4, NHC(O)R4, NHC(O)OR4, NR5R6, OH, OR4, SR4, cycloalkyl and aryl; or ?is ?optionally substituted with one or more substituents selected from the group consisting of F, Cl, Br, I, CN, NO2, alkyl, C(O)R4, C(O)NHR4, C(O)NR5R6, C(O)OH, C(O)OR4, NH2, NHR4, NHC(O)OR4, NR5R6, OH, OR4, SR4, cycloalkyl and aryl; each R4 is independently alkyl, cycloalkyl, or aryl; each R5 is independently alkyl, cycloalkyl, or aryl; each R6 is independently alkyl, cycloalkyl, or aryl; or each R5 and R6, together with the nitrogen atom to which they are attached, independently form an unsubstituted heterocyclic alkyl or unsubstituted heterocyclic aryl; and X is —S— or —O—; and n is 2, 3, or 4.Type: GrantFiled: March 22, 2018Date of Patent: June 22, 2021Assignee: The Research Foundation for The State University of New YorkInventors: Iwao Ojima, Vincent Alford, Anushree Kamath, Jian Cao, Xiadong Ren, Nicole Sampson, Monaf Awwa
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Patent number: 11000527Abstract: The invention provides compositions and methods that are effective to improve NO production in vivo and/or to increase NO levels in blood. Such compositions and methods may be useful to improve the effects of PDE5 inhibitors, for example, on erectile dysfunction or pulmonary hypertension.Type: GrantFiled: September 24, 2019Date of Patent: May 11, 2021Assignee: INNOVUS PHARMACEUTICALS, INC.Inventor: Bassam Damaj
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Patent number: 10961216Abstract: Provided herein are compounds useful for modulating the activity of an androgen receptor, or a variant thereof, and related compositions and methods. Compounds of the invention are useful for antagonizing the androgen receptor splice variant AR-v7, and for the treatment of castration-resistant prostate cancer.Type: GrantFiled: November 21, 2018Date of Patent: March 30, 2021Assignee: Massachusetts Institute of TechnologyInventors: David Freeman, Nicholas B. Struntz, Shelby K. Doyle, Andre Richters, Angela N. Koehler
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Patent number: 10919914Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: GrantFiled: June 7, 2017Date of Patent: February 16, 2021Assignee: Infinity Pharmaceuticals, Inc.Inventors: Catherine A. Evans, Martin R. Tremblay
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Patent number: 10906899Abstract: Disclosed herein are compounds and compositions for treating or inhibiting RSV and related members of the pneumovirus and paramyxovirus families such as human metapneumovirus, mumps virus, human parainfluenzaviruses, and Nipah and hendra virus, and methods of treatment or prevention thereof.Type: GrantFiled: May 10, 2017Date of Patent: February 2, 2021Assignee: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.Inventors: Richard K. Plemper, Eddy Lee, John Vernachio, Elyse Bourque
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Patent number: 10849886Abstract: Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect. An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).Type: GrantFiled: April 21, 2017Date of Patent: December 1, 2020Assignee: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Hiromi Muraoka, Akira Kanoh
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Patent number: 10842793Abstract: The present invention relates to compounds that have the capability of inhibiting the secretion of fibroblast growth factor 2 (FGF2) by tumor cells, as well as uses of said compound in medicine, in particular in the prevention and/or treatment of cancerous or inflammatory diseases.Type: GrantFiled: February 7, 2017Date of Patent: November 24, 2020Assignees: Universitat Heidelberg, European Molecular Biology LaboratoryInventors: Walter Nickel, Joe Lewis
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Patent number: 10792283Abstract: The present disclosure provides selective phosphoinositide 3-kinase inhibitors of formula (A), or pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of conditions mediated by one or more P13K isoforms, such as PI3K delta (PI3K?). The present disclosure further provides methods of inhibiting phosphoinositide 3-kinase inhibitors using these compounds for treatment of disorders related to phosphatidylinositol 3-kinase activity.Type: GrantFiled: February 28, 2017Date of Patent: October 6, 2020Assignee: HANGZHOU ZHENGXIANG PHARMACEUTICALS CO., LTD.Inventor: Xiaolin Hao
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Patent number: 10696688Abstract: The present invention relates to fused pyrimidines of formulae I and II wherein, R1, R2 are as herein described. The present invention particularly relates to isoform selective PI3K? inhibition and their medicinal use as anticancer agents.Type: GrantFiled: November 21, 2016Date of Patent: June 30, 2020Assignee: Council of Scientific & Industrial ResearchInventors: Sandip Bibishan Bharate, Shashi Bhushan, Shabber Mohammed, Santosh Kumar Guru, Sonali Sandip Bharate, Vikas Kumar, Girish Mahajan, Mubashir Javed Mintoo, Dilip Manikrao Mondhe, Ram Vishwakarma
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Patent number: 10640502Abstract: Disclosed are methods for treating cancers associated with rearrangements in the mixed lineage leukemia gene (MLL-r), including MLL-r leukemia. The methods typically include administering a therapeutic amount of one or more therapeutic agents that inhibit the biological activity of one or more members of the interleukin-1 signaling pathway such inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4).Type: GrantFiled: July 9, 2018Date of Patent: May 5, 2020Assignee: Northwestern UniversityInventors: Ali Shilatifard, Kaiwei Liang, Edwin Richard Smith, Gary E. Schiltz
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Patent number: 10633382Abstract: The present invention provides compounds according to formula (I) below that are PDE1 enzyme inhibitors and their use as medicaments, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.Type: GrantFiled: October 17, 2017Date of Patent: April 28, 2020Assignee: H. Lundbeck A/SInventors: Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård, Mikkel Jessing, Paulo Jorge Vieira Vital, Karsten Juhl
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Patent number: 10632114Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: GrantFiled: April 27, 2018Date of Patent: April 28, 2020Assignee: Agios Pharmaceuticals, Inc.Inventors: Shin-San Michael Su, Lenny Dang
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Patent number: 10604524Abstract: The present invention relates to compounds of formulae I, or pharmaceutically acceptable salts or esters thereof, wherein: R1 is selected from H and CO—NR8R9, wherein R8 and R9 are each independently selected from H, alkyl, cycloalkyl and mono or bicyclic heterocycloalkyl, wherein said alkyl group is optionally substituted by one or more R12 groups, and said heterocycloalkyl is optionally substituted by R10 or R12; or R8 and R9 are linked, together with the nitrogen to which they are attached, to form a heterocycloalkyl group optionally containing one or more additional heteroatoms, and optionally substituted by one or more groups select from R10 and (CH2)mR12; R2 is selected from H and alkyl, wherein said alkyl group is optionally substituted by one or more R12 groups; R3 is selected from alkyl, cycloalkyl and heterocycloalkyl, each of which may be optionally substituted by halo, OH or alkoxy; Z1, Z2, Z3 and Z4 are all C; R4, R5, R6 and R7 are each independently selected from H, alkyl, CN, NO2, OH, alkoxy, NType: GrantFiled: November 16, 2016Date of Patent: March 31, 2020Assignee: LIFE ARCInventors: Jon James Winter-Holt, Edward Giles Mciver, Stephen Lewis, Joanne Osborne
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Patent number: 10577382Abstract: Provided is a compound represented by the following formula, or a salt thereof: [wherein each symbol is as defined herein].Type: GrantFiled: April 27, 2017Date of Patent: March 3, 2020Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Youichi Kawakita, Takuto Kojima, Noriyuki Nii, Yoshiteru Ito, Nobuki Sakauchi, Hiroshi Banno, Xin Liu, Koji Ono, Keisuke Imamura, Shinichi Imamura
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Patent number: 10564168Abstract: Certain embodiments include methods of assessing male fertility.Type: GrantFiled: May 2, 2017Date of Patent: February 18, 2020Inventors: Amina El Jamali, Veronique Barnes
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Patent number: 10526327Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: GrantFiled: May 4, 2018Date of Patent: January 7, 2020Assignee: Celgene Quanticel Research, Inc.Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
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Patent number: 10472360Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.Type: GrantFiled: August 3, 2017Date of Patent: November 12, 2019Assignee: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventors: Soo Yei Ho, Stephanie Eliane Blanchard, Athisayamani Jeyaraj Duraiswamy, Jenefer Alam, Vikrant Arun Adsool
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Patent number: 10442815Abstract: The invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof and/or stereoisomers thereof. The compounds of the invention are useful in therapy.Type: GrantFiled: August 19, 2016Date of Patent: October 15, 2019Assignee: Karus Therapeutics LimitedInventors: Stephen J. Shuttleworth, Franck A. Silva, Alexander R. L. Cecil, Rikki P. Alexander, Alice E. Gatland, Daniel J. Finnemore
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Patent number: 10435375Abstract: Provided herein are small molecule modulators of CXCR4 activity (e.g., agonists, antagonists, inverse agonists, partial agonists), and methods of use thereof (e.g., for the treatment of disease).Type: GrantFiled: May 5, 2016Date of Patent: October 8, 2019Assignee: Northwestern UniversityInventors: Gary E. Schiltz, Richard J. Miller, Rama K. Mishra
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Patent number: 10406140Abstract: Provided is a compound which is useful as an AMPK activator, represented by formula: wherein the symbols are defined in the specification.Type: GrantFiled: May 19, 2017Date of Patent: September 10, 2019Assignee: SHIONOGI & CO., LTD.Inventors: Yuusuke Tamura, Toshihiro Wada
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Patent number: 10342814Abstract: This disclosure demonstrates that inhibition of Sirt5 can suppress malignant transformation of cells. Therefore, methods of treating cancer based on inhibition of Sirt5 are disclosed.Type: GrantFiled: September 7, 2012Date of Patent: July 9, 2019Assignee: CORNELL UNIVERSITYInventors: Hening Lin, Richard Cerione
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Patent number: 10336770Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: GrantFiled: June 29, 2017Date of Patent: July 2, 2019Assignee: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Chenggeng Qian
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Patent number: 10328069Abstract: Methods are provided for treating a lymphoproliferative malignancy to a patient in need of such treatment, comprising administering to the patient an effective amount of compound A as described herein.Type: GrantFiled: May 19, 2017Date of Patent: June 25, 2019Assignee: EXELIXIS, INC.Inventors: Arthur DeCillis, Joanne Lager
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Patent number: 10266535Abstract: Provided in the present invention is a novel inhibitor of FLT3 kinase, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite or prodrug thereof. Also provided in the present invention are a pharmaceutical composition comprising a compound of formula (I) and a use and method for preventing or treating cell proliferative conditions and/or FLT3-related conditions, in particular for conditions responding to the inhibition of FLT3 kinase (especially FLT3/ITD mutant kinases).Type: GrantFiled: August 7, 2015Date of Patent: April 23, 2019Assignees: HEFEI INSTITUTES OF PHYSICAL SCIENCE, CHINESE ACADEMY OF SCIENCES, HEFEI COSOURCE PHARMACEUTICAL CO., LTD.Inventors: Jing Liu, Qingsong Liu, Xixiang Li, Aoli Wang, Hong Wu, Cheng Chen, Wenchao Wang, Chen Hu, Zheng Zhao, Jiaxin Wu, Juan Liu, Kailin Yu, Wei Wang, Li Wang, Beilei Wang
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Patent number: 10253028Abstract: The compound 3,3,3-trifluoro-N-((1,4-trans)-4-((3-((S)-2-methylmorpholino)-IH-pyrazolo[3,4-d]pyrimidin-6-yl)amino)cyclohexyl)propane-1-sulfonamide having the Formula (I) or a salt thereof, its opposite enantiomer, compositions comprising the compound and its use in the treatment or prevention of leishmaniasis, particularly visceral leishmaniasis.Type: GrantFiled: January 21, 2016Date of Patent: April 9, 2019Assignees: GlaxoSmithKline Intellectual Property Development Limited, University of DundeeInventors: Timothy James Miles, Michael George Thomas
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Patent number: 10239863Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.Type: GrantFiled: October 20, 2017Date of Patent: March 26, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Ning Shao, Scott D. Edmondson, Santhosh Neelamkavil, Zhuyan Guo, Eric Mertz, Yi Zang, Jiafang He
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Patent number: 10189856Abstract: The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs.Type: GrantFiled: May 24, 2011Date of Patent: January 29, 2019Assignee: Adverio Pharma GMBHInventors: Claudia Hirth-Dietrich, Peter Sandner, Johannes-Peter Stasch, Andreas Knorr, Georges Von Degenfeld, Michael Hahn, Markus Follmann
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Patent number: 10167313Abstract: The present invention relates to compounds of Formula I, IA, II, IIA, III, or IIIA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).Type: GrantFiled: January 6, 2017Date of Patent: January 1, 2019Assignee: Genesis Technologies LimitedInventors: Jan-Eric Ahlfors, Khalid Mekouar
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Patent number: 10160762Abstract: The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypo-function or basal ganglia dysfunction.Type: GrantFiled: May 24, 2016Date of Patent: December 25, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Dong-Ming Shen, Michael P. Dwyer, Christopher J. Sinz, Deping Wang, Shawn J. Stachel, Daniel V. Paone, Ashley Forster, Richard Berger, Yili Chen, Yimin Qian, Shimin Xu, Chunmei Hu, William D. Shipe, Jianmin Fu, Zhigang Guo, Haitang Li, Yingjian Bo
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Patent number: 10155767Abstract: The present invention provides a therapeutic agent of acute myeloid leukemia containing a 1,3,7-trisubstituted 3,4-dihydropyrimido[4,5-d]pyrimidine-2(1H)-one compound as an active ingredient, which has proliferation inhibitory activity for a human acute myeloid leukemia cell line OCI-AML3 having a NRAS mutant gene while having low inhibitory activity for wild type NRAS and has activity of inhibiting GCK and ACK1 protein kinases at the same time.Type: GrantFiled: August 9, 2017Date of Patent: December 18, 2018Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Tae Bo Sim, Han Na Cho, Eun Hye Ju, Woo Young Hur, Ho Jong Yoon, Chi Man Song
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Patent number: 10118904Abstract: The invention relates to triazole compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.Type: GrantFiled: June 3, 2016Date of Patent: November 6, 2018Assignee: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Robert J. Davies, Jingrong Cao, Meghan Elise Cockerill, Philip Noel Collier, Elisabeth Doyle, James Daniel Frantz, Huai Gao, Brian Anthony Goldman, Ronald Lee Grey, Jr., Anne-Laure Grillot, Wenxin Gu, James A. Henderson, Raul Eduardo Krauss Irarrazaval, Adrianne Lynn Kolpak, Yusheng Liao, Sanjay Shivayogi Magavi, David Messersmith, Albert Charles Pierce, Emanuele Perola, Elizabeth Jin-Sun Ryu, Joshua Syken, Jian Wang, Michael Paul DeNinno, Francois Maltais
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Patent number: 10111864Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: GrantFiled: April 25, 2017Date of Patent: October 30, 2018Assignee: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Chenggeng Qian
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Patent number: 10106536Abstract: Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related to seizures, pain, neurotransmitter release, etc.Type: GrantFiled: May 10, 2017Date of Patent: October 23, 2018Assignee: Knopp Biosciences LLCInventors: Lynn Resnick, George T. Topalov, Charles A. Flentge, James S. Hale, David A. Mareska
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Patent number: 10064868Abstract: Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.Type: GrantFiled: June 3, 2015Date of Patent: September 4, 2018Assignee: MEI PHARMA, INC.Inventors: S. David Brown, David J. Matthews
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Patent number: 10053465Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.Type: GrantFiled: August 25, 2016Date of Patent: August 21, 2018Assignee: Incyte CorporationInventors: Yun-Long Li, David M. Burns, Hao Feng, Joseph Glenn, Chunhong He, Taisheng Huang, Song Mei, Jun Pan, Xiaozhao Wang, Yingda Ye
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Patent number: 10039846Abstract: Bradykinin B1 receptor (B1R) targeting peptides and compounds are radiolabelled with radioisotopes that are suitable for imaging and/or radiotherapy. The radiolabelled peptides and compounds have utility in imaging tissues expressing or overexpressing B1R and/or treating diseases or conditions in which B1R is expressed or overexpressed, including cancer.Type: GrantFiled: September 13, 2013Date of Patent: August 7, 2018Assignee: BRITISH COLUMBIA CANCER AGENCY BRANCHInventors: Kuo-shyan Lin, Francois Benard, Jinhe Pan, Felix Mesak, Zhengxing Zhang
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Patent number: 10022461Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.Type: GrantFiled: October 4, 2017Date of Patent: July 17, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Abbas M. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
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Patent number: 9994562Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: GrantFiled: March 12, 2014Date of Patent: June 12, 2018Assignee: Celgene Quanticel Research, Inc.Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
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Patent number: 9980961Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: GrantFiled: May 1, 2017Date of Patent: May 29, 2018Assignee: AGIOS PHARMACEUTICALS, INC.Inventors: Shin-San Michael Su, Lenny Dang