Ring Nitrogen Is Shared By Two Of The Cyclos (e.g., Ergot, Alkaloids, Etc.) Patents (Class 544/346)
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Patent number: 11897897Abstract: The present invention relates to crystalline forms of cabotegravir sodium and to methods for their preparation. Furthermore, the invention relates to a pharmaceutical composition comprising one of said crystalline forms of cabotegravir sodium, preferably in a predetermined and/or effective amount, and at last one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prophylaxis of viral infections such as HIV infections.Type: GrantFiled: May 19, 2021Date of Patent: February 13, 2024Assignee: VIIV HEALTHCARE UK (NO.3) LIMITEDInventors: Verena Adamer, Andrea Thaler
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Patent number: 11891393Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: November 3, 2021Date of Patent: February 6, 2024Assignee: Enanta Pharmaceuticals, Inc.Inventors: Joseph Panarese, Dexter Davis, Samuel Bartlett, Katherine Chong, Nathaniel Kenton, Yat Sun Or
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Patent number: 11234977Abstract: The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions and pharmaceutical combinations containing such compounds, as well as methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus (HBV), and for reducing the occurrence of serious conditions associated with HBV.Type: GrantFiled: December 19, 2018Date of Patent: February 1, 2022Assignee: Novartis AGInventors: Jiping Fu, Wooseok Han, Xianming Jin, Keith Bruce Pfister, Joseph Michael Young
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Patent number: 11198693Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: November 20, 2019Date of Patent: December 14, 2021Assignee: Enanta Pharmaceuticals, Inc.Inventors: Joseph Panarese, Dexter Davis, Samuel Bartlett, Katherine Chong, Nathaniel Kenton, Yat Sun Or
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Patent number: 11180503Abstract: The present invention provides a compound of Formula (I), wherein X is H or C1-C3 alkyl optionally substituted with hydroxyl; Y is H, hydroxy, or methyl; R is ethyl, n-propyl, cyclopropyl, or Formula (II); and A is methyl, cyclopropyl or trifluoromethyl; or a pharmaceutically acceptable salt thereof; with the proviso that when X and Y are both H and R is n-propyl, then A is other than methyl; for use as a human PDE1 inhibitor.Type: GrantFiled: July 26, 2018Date of Patent: November 23, 2021Assignee: ELI LILLY AND COMPANYInventors: Michael James Genin, William Glen Holloway, Richard Duane Johnston, John Richard Morphy, Qing Shi
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Patent number: 11040986Abstract: The present invention relates to crystalline forms of cabotegravir sodium and to methods for their preparation. Furthermore, the invention relates to a pharmaceutical composition comprising one of said crystalline forms of cabotegravir sodium, preferably in a predetermined and/or effective amount, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prophylaxis of viral infections such as HIV infections.Type: GrantFiled: January 25, 2018Date of Patent: June 22, 2021Assignee: Sandoz AGInventors: Verena Adamer, Andrea Thaler
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Patent number: 11028090Abstract: Provided are a novel [1,2,4]triazolo[4,3-a]quinoxaline derivative, a method for preparing the same, and a pharmaceutical composition for preventing or treating bromodomain extra-terminal (BET) protein-related diseases including cancer and autoimmune diseases, containing the same as an active ingredient.Type: GrantFiled: January 25, 2018Date of Patent: June 8, 2021Assignees: Dong Wha Pharm. Co., Ltd., Korea Research Institute of Chemical TechnologyInventors: Kwangho Lee, Gildon Choi, Imran Ali, Joo Yun Lee, Jin Soo Lee, Whui Jung Park, Yong Tae Kim, Seung Hwan Kim, Jung Hwan Kim, Jae-Kyung Lim
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Patent number: 10975096Abstract: Methods of making compounds of Formula I are disclosed:Type: GrantFiled: November 18, 2019Date of Patent: April 13, 2021Assignee: Gilead Sciences, Inc.Inventors: Anna Chiu, John Enquist, Jr., Nolan Griggs, Christopher Hale, Norihiro Ikemoto, Katie Ann Keaton, Matt Kraft, Scott E. Lazerwith, Michel Leeman, Zhihui Peng, Kate Schrier, Jonathan Trinidad, Jochem Van Herpt, Andrew W. Waltman
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Patent number: 10689384Abstract: The invention relates to imidazo[1,2-a]quinoxaline compounds of formula (I) for the treatment of cancer, the pharmaceutical compositions comprising said chemical compounds, and the therapeutic uses thereof.Type: GrantFiled: December 30, 2015Date of Patent: June 23, 2020Assignees: Universite de Montpellier, Centre National de la Recherche Scientifique (CNRS), Axlr, Satt du Languedoc RoussillonInventors: Carine Deleuze-Masquefa, Pierre-Antoine Bonnet, Pierre Cuq, Cindy Patinote
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Patent number: 10654871Abstract: The present invention relates to the preparation of a compound of formula VIII:Type: GrantFiled: December 3, 2018Date of Patent: May 19, 2020Assignee: ViiV Healthcare CompanyInventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
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Patent number: 10647728Abstract: The present invention relates to the preparation of a compound of formula VI:Type: GrantFiled: December 3, 2018Date of Patent: May 12, 2020Assignee: ViiV Healthcare CompanyInventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
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Patent number: 10125147Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R4d is a lower alkyl optionally substituted with substituent E, or the like; and R6d is a lower alkyl group optionally substituted with substituent group E, or the like].Type: GrantFiled: September 20, 2017Date of Patent: November 13, 2018Assignee: SHIONOGI & CO., LTD.Inventors: Yukihito Sumino, Moriyasu Masui, Daisuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
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Patent number: 10125146Abstract: A crystalline methyl (4R,12aS)-7-(benzyloxy)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1?,2?:4,5] pyrazino[2,1-b][1,3]oxazine-9-carboxylate of the formula (U2):Type: GrantFiled: September 20, 2017Date of Patent: November 13, 2018Assignee: SHIONOGI & CO., LTD.Inventors: Yukihito Sumino, Moriyasu Masui, Daisuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
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Patent number: 10081632Abstract: Described herein are carboxamide derivatives of Formula (II) that are useful as inhibitors of p90 ribosomal S6 kinase (RSK), pharmaceutical compositions comprising the derivatives, and methods of using the derivatives in treating diseases or conditions associated with RSK activity: wherein R2, R4a, R4b, R11, R12, and n are defined in the specification.Type: GrantFiled: July 31, 2017Date of Patent: September 25, 2018Assignee: PHOENIX MOLECULAR DESIGNSInventors: Sandra E. Dunn, Aarthi Jayanthan, Jaipal Reddy Nagireddy, Subhash Annedi, John H. Van Drie, Timothy S. Daynard, My-my Huynh
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Patent number: 9969750Abstract: A process for preparing a compound shown by formula (W6): wherein each Hal is independently chloro or bromo, using a novel process for preparing a pyridine derivative represented by formula (W2), wherein R6d is as defined herein.Type: GrantFiled: September 20, 2017Date of Patent: May 15, 2018Assignee: Shionogi and Co., Ltd.Inventors: Yukihito Sumino, Moriyasu Masui, Daisuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
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Patent number: 9802959Abstract: A process for preparing a compound shown by formula (W5): wherein each Hal is independently chloro or bromo, using a novel process for preparing a pyridine derivative represented by formula (W2), wherein R6d is as defined herein.Type: GrantFiled: March 28, 2017Date of Patent: October 31, 2017Assignee: Shionogi & Co., Ltd.Inventors: Yukihito Sumino, Moriyasu Masui, Diasuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
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Patent number: 9707246Abstract: The invention is directed to a method for treatment of viral infections, particularly HIV infection. The method involves administering compounds which are substituted (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-6-oxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamides of formula (I).Type: GrantFiled: August 5, 2015Date of Patent: July 18, 2017Assignees: SHIONOGI & CO., LTD., VIIV HEALTHCARE COMPANYInventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
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Patent number: 9650394Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) wherein R1d, R2d, and R4d are as defined herein.Type: GrantFiled: March 17, 2016Date of Patent: May 16, 2017Assignee: Shionogi & Co., Ltd.Inventors: Yukihito Sumino, Moriyasu Masui, Daisuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
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Patent number: 9643981Abstract: The present invention relates to the preparation of (4R,12aS)-N-(2,4-difluorobenzyl)-7-methoxy-4 -methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide of the formula VIIa:Type: GrantFiled: July 28, 2015Date of Patent: May 9, 2017Assignee: ViiV Healthcare CompanyInventors: Steven N. Goodman, Huan Wang, Douglas Mans, Matthew Kowalski
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Patent number: 9527868Abstract: Provided herein, inter alia, is the synthesis of ETP derivatives. The uses of the ETP derivatives described herein include treatment of cancer.Type: GrantFiled: April 17, 2015Date of Patent: December 27, 2016Assignees: CITY OF HOPE, THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Larry Eugene Overman, Marcus Baumann, Sangkil Nam, David Horne, Richard Jove, Jun Xie, Claudia Kowolik
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Patent number: 9321789Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) wherein R1d, R2d, and R4d are as defined herein.Type: GrantFiled: October 20, 2014Date of Patent: April 26, 2016Assignee: Shinogi & Co., Ltd.Inventors: Yukihito Sumino, Moriyasu Masui, Diasuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
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Patent number: 9187497Abstract: Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R31, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: August 1, 2014Date of Patent: November 17, 2015Assignee: Takeda Phamaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 9163029Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.Type: GrantFiled: October 23, 2013Date of Patent: October 20, 2015Assignee: BIOTA SCIENTIFIC MANAGEMENT PTY LTD.Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Helen Anderson
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Patent number: 9150593Abstract: Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.Type: GrantFiled: December 12, 2014Date of Patent: October 6, 2015Assignee: MAP Pharmaceuticals, Inc.Inventors: Robert O. Cook, Jian Zhang, Thomas A. Armer
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Patent number: 9133216Abstract: The compounds are intermediates in the preparation of therapeutic agents useful in the treatment of viral infections, particularly HIV infection. The compounds are (3S,11aR)-6-[(phenylmethyl)oxy]-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-9 and/or (3S,11aR)-6-[(phenylmethyl)oxy]-8-bromo-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-10.Type: GrantFiled: March 17, 2015Date of Patent: September 15, 2015Assignees: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
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Patent number: 9040531Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: GrantFiled: May 7, 2010Date of Patent: May 26, 2015Assignee: PRISM BioLab Co., Ltd.Inventors: Takenao Odagami, Yuji Kogami, Hiroyuki Kouji
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Publication number: 20150133456Abstract: Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.Type: ApplicationFiled: January 9, 2015Publication date: May 14, 2015Inventors: Thomas Armer, Shashidhar Kori, Libo Wu
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Publication number: 20150133428Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventors: Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Mark D. Wittman, Bradley C. Pearce, Erika M. V. Araujo, Bireshwar Dasgupta, Jalathi Surendran Nair, Sakthi Kumaran Janakiraman, Chandrasekhar Reddy Rachamreddy, Mettu Mallikarjuna Rao, Arul Mozhi Selvan Subbiah Karuppiah, Bandreddy Subba Reddy, Pulicharla Nagalakshmi, Rajesh Onkardas Bora, Shilpa Holehatti Maheshwarappa, Selvakumar Kumaravel, Dibakar Mullick, Ramesh Sistla
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Patent number: 9012650Abstract: The compounds are therapeutic agents useful in the treatment of viral infections, particularly HIV infection. The compounds are substituted (3S, 11aR)-N-[(2,4 -difluorophenyl)methyl]-6-oxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamides of formula (I).Type: GrantFiled: May 21, 2014Date of Patent: April 21, 2015Assignees: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
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Publication number: 20150065485Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20150031652Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: August 1, 2014Publication date: January 29, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20150031876Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.Type: ApplicationFiled: September 5, 2014Publication date: January 29, 2015Applicant: Shionogi & Co., Ltd.Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
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Patent number: 8933132Abstract: The invention relates to novel piperazine compounds of formula (I): to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial, i.e. in particular to treat pain.Type: GrantFiled: January 19, 2012Date of Patent: January 13, 2015Assignee: Convergence Pharmaceuticals LimitedInventors: David Norton, Daniele Andreotti, Simon E. Ward, Roberto Profeta, Simone Spada, Helen Susanne Price
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Patent number: 8916565Abstract: The invention relates to pyrrolopyrazine-spirocyclic piperidine amide compounds of formula (I) useful as inhibitors of ion channels: wherein R1, R2, R3, R4, A, m, n, and o are as defined in the description. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: February 2, 2012Date of Patent: December 23, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida Ruah, Edward Adam Kallel, Mark Thomas Miller, Vijayalaksmi Arumugam, Jason McCartney, Corey Anderson, Peter Diederik Jan Grootenhuis, Licong Jiang
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Patent number: 8901126Abstract: Substituted imidazo[1,5-a]quinoxalin-4-one compounds of formula (I) described herein exhibit PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: GrantFiled: March 7, 2013Date of Patent: December 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hirofumi Yamamoto, Kazunori Kamijo, Kazuyuki Tsuchiya, Ryushi Seo, Satoshi Yamamoto
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Publication number: 20140349970Abstract: The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, 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: June 9, 2014Publication date: November 27, 2014Applicant: ABBVIE INC.Inventors: Neil Wishart, Maria A. Argiriadi, Eric C. Breinlinger, David J. Calderwood, Anna M. Ericsson, Bryan A. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Michael Z. Hoemann, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kelly D. Mullen, Gagandeep Somal, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller
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Publication number: 20140315883Abstract: The invention provides a compound of Formula (I as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: April 18, 2014Publication date: October 23, 2014Applicant: ABBVIE INC.Inventors: Eric Breinlinger, Heather Davis, Michael Hoemann, Bin Li, Biqin Li, Gagandeep Somal, Stacy Van Epps, Lu Wang, Lu Wang
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Publication number: 20140315888Abstract: The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.Type: ApplicationFiled: September 28, 2012Publication date: October 23, 2014Applicant: C&C RESEARCH LABORATORIESInventors: Pil Su Ho, Dong Oh Yoon, Sun Young Han, Won Il Lee, Jung Sook Kim, Woul Seong Park, Sung Oh Ahn, Hye Jung Kim
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Patent number: 8841448Abstract: Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.Type: GrantFiled: October 7, 2013Date of Patent: September 23, 2014Assignee: Map Pharmaceuticals, Inc.Inventors: Robert O. Cook, Jian Zhang, Thomas A. Armer
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Publication number: 20140275056Abstract: The present invention is directed to a compound of Formula (I): The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael A. Letavic, Dale A. Rudolph
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Publication number: 20140256679Abstract: The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: May 21, 2014Publication date: September 11, 2014Applicants: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian Alvin JOHNS, Jason Gordon WEATHERHEAD, Toshikazu HAKOGI, Yasunori AOYAMA
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Publication number: 20140256937Abstract: The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.Type: ApplicationFiled: October 12, 2012Publication date: September 11, 2014Applicant: SHIONOGI & CO., LTD.Inventor: Toshiyuki Akiyama
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Patent number: 8829000Abstract: The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.Type: GrantFiled: September 14, 2012Date of Patent: September 9, 2014Assignee: ASKA Pharmaceutical Co., Ltd.Inventors: Makoto Okada, Shuichiro Sato, Kenji Kawade, Kotaro Gotanda, Atsushi Shinbo, Youichi Nakano, Hideo Kobayashi
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Publication number: 20140249143Abstract: Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: GlaxoSmithKline LLCInventors: Anna Lindsey Banka, Janos Botyanszki, Eric Gregory Burroughs, John George Catalano, Wendy Huang Chern, Hamilton D. Dickson, Margaret J. Gartland, Robert Hamatake, Hans Hofland, Jesse Daniel Keicher, Christopher Brooks Moore, John Bradford Shotwell, Matthew David Tallant, Jean-Philippe Therrien, Shihyun You
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Publication number: 20140243348Abstract: Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed.Type: ApplicationFiled: January 22, 2014Publication date: August 28, 2014Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: David M. Knipe, Kevin Bryant, David H. Dreyfus
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Publication number: 20140235645Abstract: The present invention is directed to pyridine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders.Type: ApplicationFiled: September 10, 2012Publication date: August 21, 2014Applicant: H. LUNDBECK A/SInventors: Morten Jorgensen, Anne Techau Bruun, Lars Kyhn Rasmussen
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Publication number: 20140221356Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: December 19, 2013Publication date: August 7, 2014Inventors: Haolun JIN, Scott E. LAZERWITH, Teresa Alejandra TREJO MARTIN, Elizabeth M. BACON, Jeromy J. COTTELL, Zhenhong R. CAI, Hyung-Jung PYUN, Philip Anthony MORGANELLI, Mingzhe JI, James G. TAYLOR, Xiaowu CHEN, Michael R. MISH, Manoj C. DESAI
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Publication number: 20140221355Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, Z2, or Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: December 19, 2013Publication date: August 7, 2014Inventors: Scott E. LAZERWITH, Haolun JIN, Hyung-Jung Pyun
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Publication number: 20140200209Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: March 14, 2014Publication date: July 17, 2014Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
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Publication number: 20140194434Abstract: Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and or 5-HT1B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.Type: ApplicationFiled: March 10, 2014Publication date: July 10, 2014Applicant: MAP Pharmaceuticals, Inc.Inventors: Robert O. Cook, THOMAS A. ARMER, Sergey Alexandrovich KOSAREV, Dejian Xie, Jian Zhang