Three Or More Hetero Atoms In The Tetracyclo Ring System Patents (Class 514/287)
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Patent number: 11964976Abstract: Novel pyrido[3?,4?:4,5]pyrrolo[3,2-c][1,6]naphthyridine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[3?,4?:4,5]pyrrolo[3,2-c][1,6]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.Type: GrantFiled: September 12, 2023Date of Patent: April 23, 2024Assignee: KING FAISAL UNIVERSITYInventors: Christophe Tratrat, Michelyne Haroun
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Patent number: 11932642Abstract: Novel pyrido[3?,4?:4,5]pyrrolo[3,2-b][1,6]naphthyridine compounds of the formula as shown below, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[3?,4?:4,5]pyrrolo[3,2-b][1,6]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.Type: GrantFiled: August 21, 2023Date of Patent: March 19, 2024Assignee: KING FAISAL UNIVERSITYInventors: Christophe Tratrat, Michelyne Haroun
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Patent number: 11884668Abstract: Pyrido[3?,4?:4,5]pyrrolo[2,3-c]quinolone compounds are provided. The pyrido[3?,4?:4,5]pyrrolo[2,3-c]quinolone compounds have the general formula: where R1 is H, C(O)OH4, O or OH: R2 is H, C(O)OH, C(O)OR4, or OH: and R3 is C—C6 alkyl, C1-C6 haloalkyl, C1-C6 cyanoalkyl, (CH2)2-3NR7R8, (CH2)1-2aryl, (CH2)1-2heteroaryl, C(O)—(CH2)2-3NR7R8, C(O)aryl, C(O)heteroaryl, NH(CH2)2-3NR7R8, NH(CH2)0-1aryl, NH(CH2)0-1heteroaryl, NHC(O)—(CH2)2-3NR7R sNHC(O)aryl, NHC(O)heteroaryl, NHS(o)2-(CH2)2-3NR7R8, NHS(O)2aryl, NHS(O)2heteroaryl, S(O)2—(CH2)2-3NR7R8, S(O)2aryl, S(O)2heteroaryl, C3-C6 cycloalyl, C3-C6 halocycloalyl, C3-C6 cyanoccloalyl, aryl, or 5- or 6-membered heteroaryl. The compounds are inhibitors of protein kinase CK2 activity.Type: GrantFiled: August 2, 2023Date of Patent: January 30, 2024Assignee: KING FAISAL UNIVERSITYInventors: Christophe Tratrat, Michelyne Haroun
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Patent number: 11858934Abstract: Pyrido[4?,3?:5,6]pyrimido[1,2-a]indole compounds are provided. The pyrido[4?,3?:5,6]pyrimido[1,2-a]indole compounds have the general formula: where R1 represents aryl, heteroaryl, aminoaryl, aminoheteroaryl, aminoalkyl, aminocycloalkyl, aryloxy, heteroaryloxy, or alkoxy; and R2 and R3 represent hydrogen, carboxyl, ester, amide, halogen, alkyl, aryl, hydroxyl, alkoxy, aryloxy, aminoalkyl, aminocycloalkyl, aminoaryl, or aminoheteroaryl. The compounds show inhibitory activity against CK2 enzyme, and may be used as anticancer agents.Type: GrantFiled: July 17, 2023Date of Patent: January 2, 2024Assignee: KING FAISAL UNIVERSITYInventors: Christophe Tratrat, Michelyne Haroun
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Patent number: 11845749Abstract: Pyrido[4?,3?:5,6]pyrazino[1,2-a]indole compounds are provided. The compounds exhibit inhibitory activity against CK2 enzyme and may be used as anticancer agents. The compounds have the following general formula I: where R1 represents aryl, heteroaryl, aminoaryl, aminoheteroaryl, aminoalkyl, aminocycloalkyl, aryloxy, heteroaryloxy, or alkoxy; and R2 and R3 represent hydrogen, carboxyl, ester, amide, halogen, alkyl, aryl, hydroxyl, alkoxy, aryloxy, aminoalkyl, aminocycloalkyl, aminoaryl, or aminoheteroaryl.Type: GrantFiled: July 13, 2023Date of Patent: December 19, 2023Assignee: KING FAISAL UNIVERSITYInventors: Christophe Tratrat, Michelyne Haroun
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Patent number: 11104957Abstract: The present invention relates to compositions and methods for treating of cancer. In some embodiments, the invention relates to the use of agents that can modulate a component in the CDX2-KLF4 signaling pathway to treat myelodysplastic syndromes (MDS), acute myelogenous leukemia (AML), acute lymphocytic leukemia (ALL), adult T-cell leukaemia (ATLL), lymphoma, gastric cancer, multiple myeloma, or combinations thereof, or a condition associated with abnormal activity of the CDX2-KLF4 signaling pathway.Type: GrantFiled: March 20, 2018Date of Patent: August 31, 2021Assignee: Aptose Biosciences, Inc.Inventor: William G. Rice
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Patent number: 11020488Abstract: Provided are pyrroloquinolin compounds of formula (1) or (II). In certain aspects, the pyrroloquinolin compounds are therapeutic, e.g., for treating a cell proliferative disorder. Also provided are conjugates that include the pyrroloquinolin compounds of the present disclosure. Compositions, e.g., pharmaceutical compositions, that include the pyrroloquinolin compounds and conjugates of the present disclosure are also provided. Further provided are therapeutic methods involving the administration of the pyrroloquinolin compounds, conjugates or compositions of the present disclosure. Kits that include the pyrroloquinolin compounds, conjugates or compositions are also provided.Type: GrantFiled: March 13, 2018Date of Patent: June 1, 2021Assignees: The Regents of the University of California, Henry Ford Health SystemInventors: Phillip Crews, Frederick A. Valeriote, Sheng Lin, Erin P. McCauley, Nicholas Lorig-Roach, Karen Tenney
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Patent number: 10566545Abstract: A condensed cyclic compound and an organic light-emitting device including the same are provided. The organic light-emitting device includes a first electrode, a second electrode, and an organic layer disposed between the first electrode and the second electrode. The organic layer includes the condensed cyclic compound represented by Formula 1: in Formula 1, A11 is a C1-C60 heterocyclic group, A12 is a C5-C60 carbocyclic group or a C1-C60 heterocyclic group, X11 is O or S, X12 is C, X13 is selected from N, C, and C(R13), X14 is selected from N, C, and C(R14), and X13 and X14 are linked via a single bond or a double bond.Type: GrantFiled: August 23, 2017Date of Patent: February 18, 2020Assignee: SAMSUNG DISPLAY CO., LTD.Inventors: Munki Sim, Junha Park, Hyoyoung Lee, Eunjae Jeong, Youngkook Kim, Seokhwan Hwang
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Patent number: 10464938Abstract: The present invention provides pharmaceutical compositions comprising certain optionally substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, and as further defined herein:Type: GrantFiled: June 12, 2019Date of Patent: November 5, 2019Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng, Lawrence P. Wennogle
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Patent number: 10456400Abstract: In some aspects, the present invention relates to aza-ellipticine compounds of the formula: wherein the variables are as defined herein. The application also provides novel methods of preparing aza-ellipticine compounds, methods of using the compounds, and pharmaceutical compositions thereof.Type: GrantFiled: May 15, 2015Date of Patent: October 29, 2019Assignee: MUSC Foundation for Research DevelopmentInventors: Christopher C. Lindsey, Craig C. Beeson
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Patent number: 10406151Abstract: The present invention provides a method of inducing autophagy, the method including administering to a subject an effective amount of a pyrroloquinoline quinone compound or a salt thereof.Type: GrantFiled: November 20, 2017Date of Patent: September 10, 2019Assignee: MITSUBISHI GAS CHEMICAL COMPANY, INC.Inventor: Kazuto Ikemoto
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Patent number: 10081600Abstract: The invention features 2-alkoxy-11-hydroxyaporphine derivatives that selectively bind D2high receptors. The compounds are useful for imaging D2high receptors and for the treatment of diseases, such as Parkinson's disease, sexual dysfunction, and depressive disorders.Type: GrantFiled: November 9, 2016Date of Patent: September 25, 2018Assignee: The McLean Hospital CorporationInventors: John L. Neumeyer, Yu-Gui Si, Anna Waclawa Sromek
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Patent number: 10035800Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y3, A1, A2, A3 and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: GrantFiled: March 12, 2014Date of Patent: July 31, 2018Assignee: AbbVie Inc.Inventors: Steven D. Fidanze, Dauchun Liu, Robert A. Mantei, Keith F. McDaniel, John Pratt, George S. Sheppard, Le Wang, Andrew Bogdan, James H. Holms, Justin D. Dietrich, Jasmina Marjanovic, Lisa A. Hasvold, Yujia Dai
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Patent number: 9920069Abstract: Compounds that specifically kill fluoroquinolone (FQ) resistant bacteria have been developed and are described herein. The FQs are the most commonly prescribed antibiotics to adults in the U.S. and thus are extremely important drugs. However, bacterial resistant to these drugs is now ubiquitous in some of the most common and deadly Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Indeed, FQs are no longer indicated for treatment of MRSA and VRE infections because of such resistance. The compounds have specific and potent activity versus MRSA and VRE.Type: GrantFiled: March 17, 2015Date of Patent: March 20, 2018Assignee: The Board of Trustees of the University of IllinoisInventors: Paul J. Hergenrother, Elizabeth I. Parkinson, Joseph S. Bair
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Patent number: 9567643Abstract: The present invention relates to compositions and methods for treating of cancer. In some embodiments, the invention relates to the use of agents that can modulate a component in the CDX2-KLF4 signaling pathway to treat myelodysplastic syndromes (MDS), acute myelogenous leukemia (AML), acute lymphocytic leukemia (ALL), adult T-cell leukaemia (ATLL), lymphoma, gastric cancer, multiple myeloma, or combinations thereof, or a condition associated with abnormal activity of the CDX2-KLF4 signaling pathway.Type: GrantFiled: October 3, 2014Date of Patent: February 14, 2017Assignee: Aptose Biosciences Inc.Inventor: William G. Rice
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Patent number: 9526721Abstract: Tetrahydroprotoberbine (THPB) compounds and their use in the treatment of neurological, psychiatric and neurodegenerative diseases is provided. The compounds include d-govadine, l-govadine and racemic govadine, as well as d-THPBs of general formula (I). Enantioselective processes for preparing compounds of formula (I), and d- and l-govadine are also provided.Type: GrantFiled: August 2, 2012Date of Patent: December 27, 2016Inventors: James Jackson Miller, Anthony George Phillips, Christopher Court Lapish, Glenn Martin Sammis
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Patent number: 9512123Abstract: Generally, the present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: GrantFiled: May 9, 2015Date of Patent: December 6, 2016Assignee: Pimera, Inc.Inventor: Mustapha Haddach
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Patent number: 9419229Abstract: Disclosed are a compound for an organic optoelectric device, an organic optoelectric device including the same and a display device including the organic optoelectric device, wherein the compound for an organic optoelectric device is represented by the following Chemical Formula 1, In the above Chemical Formula 1, R1 to R7, X, L1 and L2 are the same as described in the detailed description.Type: GrantFiled: November 20, 2013Date of Patent: August 16, 2016Assignee: CHEIL INDUSTRIES, INC.Inventors: Jin-Seok Hong, Dong-Min Kang, Eun-Sun Yu, Soo-Young Jeong, Ji-Hun Shin, Dong-Kyu Ryu, Han-ill Lee, Yu-Na Jang
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Patent number: 9044501Abstract: Provided are novel use of an extract of Lycoris chejuensis or a compound isolated therefrom for inhibition of ?-amyloid production and/or prevention, improvement and/or treatment of a neurodegenerative disease, more specifically a ?-amyloid production inhibitor, and/or a composition for prevention or treatment of a neurodegenerative disease containing one or more kinds selected from the group consisting of an extract of Lycoris chejuensis, and/or dihydrolycoricidine, 2-methoxypancracine, lycoricidine, and/or lycoricidinol, as an active ingredient; a method for inhibiting ?-amyloid production, and/or preventing and/or treating a neurodegenerative disease using the same; and, a method for preparing the same.Type: GrantFiled: October 28, 2009Date of Patent: June 2, 2015Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Hyun-Ok Yang, Hak-Cheol Kwon, Jin-Soo Park, Sung-Kwon Chung, Myung-Soo Kim
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Patent number: 9018227Abstract: The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists.Type: GrantFiled: March 18, 2011Date of Patent: April 28, 2015Assignees: Indiana State University, The United States of America, as Represented by the Secretary, Department of Health and Human ServicesInventors: Richard W. Fitch, Thomas F. Spande, H. Martin Garraffo, Herman J. C. Yeh, Kathryn Daly
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Patent number: 9012441Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: GrantFiled: January 9, 2014Date of Patent: April 21, 2015Assignee: Gilead Sciences, Inc.Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
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Publication number: 20150104392Abstract: The present invention relates to compositions, biomarkers, and their use in treatment of cancer. In some embodiments, the invention relates to the use of several biomarkers in methods for determining the responsiveness of a human subject to a specific compound, methods for monitoring the efficacy of the compound, or methods for treating a human subject.Type: ApplicationFiled: October 3, 2014Publication date: April 16, 2015Inventor: WILLIAM G. RICE
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Publication number: 20150099775Abstract: The present invention relates to compositions and methods for treating of cancer. In some embodiments, the invention relates to the use of agents that can modulate a component in the CDX2-KLF4 signaling pathway to treat myelodysplastic syndromes (MDS), acute myelogenous leukemia (AML), acute lymphocytic leukemia (ALL), adult T-cell leukaemia (ATLL), lymphoma, gastric cancer, multiple myeloma, or combinations thereof, or a condition associated with abnormal activity of the CDX2-KLF4 signaling pathway.Type: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Inventor: WILLIAM G. RICE
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Publication number: 20150099774Abstract: New phenanthroline derivatives as drug as well as methods for producing said compounds are provided.Type: ApplicationFiled: April 5, 2013Publication date: April 9, 2015Inventors: Bernd Clement, Christopher Meier, Dieter Heber, Lars Stenzel
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Patent number: 8993588Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: June 2, 2008Date of Patent: March 31, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Ian Bell, Harold Selnick, C. Blair Zartman
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Publication number: 20150065504Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).Type: ApplicationFiled: August 19, 2014Publication date: March 5, 2015Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
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Patent number: 8962620Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 4, 2013Date of Patent: February 24, 2015Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Patent number: 8927566Abstract: The present invention relates to a norepinephrine and selective serotonin receptor blocker and the use thereof. The norepinephrine and selective serotonin receptor blocker is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is selected from the group consisting of C1-6 alkyl, C1-6 alkoxy, C6-10 aralkyl, C6-10 arylalkoxy, C1-6 haloalkyl and C1-6 haloalkoxy; and R2 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. R3 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. The compound of the present invention is effective norepinephrine and selective serotonin receptor blocker.Type: GrantFiled: November 21, 2012Date of Patent: January 6, 2015Assignee: Beijing Medisan Technology Co., Ltd.Inventors: Mingxin Wang, Jinai Liu, Fan Yang, Ailing Wang, Jiguo Sun, Yan Wang, Jin Cui, Lei Ji
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Publication number: 20150005322Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: September 12, 2014Publication date: January 1, 2015Inventors: Rajendra Parasmal JAIN, Sarvajit Chakravarty
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Patent number: 8895726Abstract: The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen orType: GrantFiled: February 19, 2008Date of Patent: November 25, 2014Assignees: The Institut Curie, The University of Montpellier 2 Science and TechniquesInventors: Fabrice Lejeune, Jamal Tazi, David Grierson, Christian Rivalle, Florence Mahuteau-Betzer
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Publication number: 20140343089Abstract: The present invention relates to a norepinephrine and selective serotonin receptor blocker and the use thereof. The norepinephrine and selective serotonin receptor blocker is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is selected from the group consisting of C1-6 alkyl, C1-6 alkoxy, C6-10 aralkyl, C6-10 arylalkoxy, C1-6 haloalkyl and C1-6 haloalkoxy; and R2 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. R3 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. The compound of the present invention is effective norepinephrine and selective serotonin receptor blocker.Type: ApplicationFiled: November 21, 2012Publication date: November 20, 2014Inventors: Mingxin Wang, Jinai Liu, Fan Yang, Ailing Wang, Jiguo Sun, Yan Wang, Jin Cui, Lei Ji
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Patent number: 8859561Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: September 23, 2010Date of Patent: October 14, 2014Assignee: Medivation Technologies, Inc.Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Publication number: 20140303144Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: October 9, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Patent number: 8853234Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: GrantFiled: March 9, 2011Date of Patent: October 7, 2014Assignee: Senhwa Biosciences, Inc.Inventors: Johnny Yasuo Nagasawa, Fabrice Pierre, Mustapha Haddach, Michael Schwaebe, Levan Darjania, Jeffrey P. Whitten
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Patent number: 8829023Abstract: The invention relates to a process for obtaining compounds derived from tetrahydro-?-carboline, specifically tadalafil and intermediate products from the synthesis, comprising the reaction between piperonal and an alkyl ester of D-tryptophan as a salt, and in the absence of any other component, followed by haloacetylation and a final cyclization with methylamine.Type: GrantFiled: February 10, 2012Date of Patent: September 9, 2014Assignee: Interquim, S.A.Inventors: Xavier Berzosa Rodríguez, Francisco Marquillas Olondriz
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Publication number: 20140234345Abstract: The present application is directed to covalent conjugates between an isocarbostyril alkaloid and a lipophilic biomolecule, to pharmaceutical compositions comprising the conjugates and to therapeutic uses thereof, in particular for treating cancer.Type: ApplicationFiled: July 11, 2012Publication date: August 21, 2014Applicant: BIOLYSE PHARMA CORPORATIONInventors: Claude Mercure, Rajashree Sathyamurthy
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Publication number: 20140228353Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: August 14, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
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Publication number: 20140221417Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: January 9, 2014Publication date: August 7, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, Yunfeng Eric HU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140213571Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: August 20, 2012Publication date: July 31, 2014Inventors: Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
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Publication number: 20140206671Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: January 27, 2014Publication date: July 24, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Youssef Bennani, Tianseng Wang, Francesco Salituro, John P. Duffy
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Publication number: 20140162985Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: September 6, 2013Publication date: June 12, 2014Applicant: ABBVIE INC.Inventors: Andrew Burchat, Thomas D. Gordon, Kelly D. Mullen, David C. Ihle, Michael J. Morytko, Kevin P. Cusack, Gloria Y. Lo Schiavo, Lei Wang, Michael Friedman
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Patent number: 8703792Abstract: The present application relates to novel C-1 substituted analogues of pancratistatin and 7-dexoypancratistatin of Formula (I), pharmaceutical compositions thereof and the use of said compounds of Formula (I) in the treatment of cancer The application also relates to processes for the preparation of said compound of Formula (I) and intermediates thereof.Type: GrantFiled: December 17, 2009Date of Patent: April 22, 2014Assignee: Brock UniversityInventors: Tomas Hudlicky, Jonathan Collins
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Patent number: 8697064Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.Type: GrantFiled: December 26, 2012Date of Patent: April 15, 2014Assignee: Pierre Fabre MedicamentInventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
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Patent number: 8691814Abstract: The present invention provides compounds having formula (I): wherein R1, R2, R3 and n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of inflammatory or autoimmune and proliferative disorders and as inhibitors of cell adhesion molecule expression and inflammatory cytokine signal transduction generally.Type: GrantFiled: November 2, 2010Date of Patent: April 8, 2014Assignee: Eisai R&D Management Co., Ltd.Inventors: Jane Daun, Heather A. Davis, Bruce DeCosta, Fabian Gusovsky, Ieharu Hishinuma, Yimin Jiang, Toshihiko Kaneko, Kouichi Kikuchi, Seiichi Kobayashi, André Lescarbeau, Xiang-Yi Li, Kenzo Muramoto, Norihito Ohi, Marc Pesant, Boris M. Seletsky, Motohiro Soejima, Mark Spyvee, Lynda Tremblay, Ye Yao, Hiromitsu Yokohama, Yan (Janet) Zhao, Wanjun Zheng
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Publication number: 20140088086Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: ApplicationFiled: March 7, 2013Publication date: March 27, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc.
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Patent number: 8680107Abstract: The invention presents methods of identifying small molecule compounds that are activators of tumor suppressor protein p53 pathway, and its associated family members p63 and p73, function. The invention is further drawn to methods of killing tumor cells and treating cancers or other conditions requiring activation of the p53 family member pathways and DNA damage response pathways with the small molecules.Type: GrantFiled: June 19, 2008Date of Patent: March 25, 2014Assignee: The Johns Hopkins UniversityInventors: Marikki Laiho, Karita Peltonen
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Publication number: 20140031275Abstract: Disclosed herein are methods and compositions for the eradication of bacterial infections. In particular, methods and compositions are disclosed for the eradication of persister and slow growing bacterial cell populations. In particular embodiments, the methods and compositions disclosed herein are useful for eradication of biofilms.Type: ApplicationFiled: October 1, 2013Publication date: January 30, 2014Applicant: NORTHEASTERN UNIVERSITYInventors: Kim LEWIS, Brian CONLON, Mark L. NELSON, Michael P. POLLASTRI, Thomas A. DAHL
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Publication number: 20140031362Abstract: The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.Type: ApplicationFiled: April 12, 2012Publication date: January 30, 2014Applicant: PIERRE FABRE MEDICAMENTInventors: Rémi Rabot, Karim Bedjeguelal, El Bachir Kaloun, Philippe Schmitt, Nicolas Rahier, Patrice Mayer, Emmanuel Fournier
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Patent number: 8630703Abstract: Hydrophobic weak base compounds such as hydrophobic weak base chemotherapeutic agents (which are not an anthracycline) for use in the treatment of medical conditions such as proliferative disease or disorder in a subject, in combination with illumination of a region in a body of the subject which is characterized by the presence of proliferating cells, are disclosed. The hydrophobic weak base compound and a wavelength of illumination are selected such that the hydrophobic weak base compound acts as a therapeutically effective photosensitizer when exposed to the illumination.Type: GrantFiled: March 8, 2012Date of Patent: January 14, 2014Assignee: Technion Research & Development Foundation LimitedInventors: Yehuda G. Assaraf, Yamit Adar Turgeman, Andrzej M. Skladanowski, Arjan W. Griffioen, Henk Verheul, Kristy Gotink, Hubert Van Den Bergh, Patrycja Nowak-Sliwinska
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Patent number: 8598167Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: July 9, 2013Date of Patent: December 3, 2013Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan