The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/361)
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Patent number: 11684625Abstract: The present invention relates to novel compounds of formula (I) that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).Type: GrantFiled: May 30, 2019Date of Patent: June 27, 2023Assignee: AC Immune SAInventors: Sreenivasachary Nampally, Emanuele Gabellieri, Jerome Molette
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Patent number: 10807958Abstract: The present invention relates to the compound having Formula (I) or pharmaceutically acceptable salts or solvates thereof, and its use in treating and/or preventing a Tauopathy.Type: GrantFiled: June 15, 2018Date of Patent: October 20, 2020Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), UNIVERSITE DE LILLE 2 DROIT ET SANTEInventors: Nicolas Sergeant, Luc Buee, Patricia Melnyk, Marion Gay, Nicolas Le Fur
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Patent number: 10017476Abstract: The present invention relates to the compound having Formula (I) or pharmaceutically acceptable salts or solvates thereof, and its use in treating and/or preventing a Tauopathy.Type: GrantFiled: March 16, 2016Date of Patent: July 10, 2018Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), CENTRE HOSPITALIER REGIONAL ET UNIVERSITAIRE DE LILLE (CHRU), UNIVERSITE DE LILLE 2 DROIT ET SANTEInventors: Nicolas Sergeant, Luc Buee, Patricia Melnyk, Marion Gay, Nicolas Le Fur
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Patent number: 9540365Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.Type: GrantFiled: March 14, 2014Date of Patent: January 10, 2017Assignee: OSTEOQC INC.Inventors: Debra Ellies, Jean-Philippe Rey, F. Scott Kimball
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Patent number: 9458170Abstract: The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.Type: GrantFiled: June 17, 2013Date of Patent: October 4, 2016Assignee: YULIANG LIInventor: Yuliang Li
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Publication number: 20150139905Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.Type: ApplicationFiled: October 9, 2014Publication date: May 21, 2015Inventors: Dinesh Chimmanamada, Weiwen Ying
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Publication number: 20150141419Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.Type: ApplicationFiled: May 9, 2013Publication date: May 21, 2015Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
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Patent number: 9034869Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are 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: March 7, 2013Date of Patent: May 19, 2015Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
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Patent number: 9029387Abstract: The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.Type: GrantFiled: February 28, 2011Date of Patent: May 12, 2015Assignee: Merck Patent GmbHInventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
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Publication number: 20150105554Abstract: The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: May 10, 2013Publication date: April 16, 2015Inventors: Carlo Gambacorti-Passerini, Luca Mologni, Leonardo Scapozza, William Bisson, Shaheen Ahmed, Peter Goekjian, Sébastien Tardy, Alexandre Orsato, David Gueyrard, Joseph Benoit
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Patent number: 9006246Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.Type: GrantFiled: July 5, 2011Date of Patent: April 14, 2015Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
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Publication number: 20150098905Abstract: The present invention relates to targeting agents and methods: of using the targeting agents to detect a fungal cell in a subject.Type: ApplicationFiled: May 8, 2013Publication date: April 9, 2015Applicant: Rutgers, The State University of New JerseyInventors: David S. Perlin, Guillermo Garcia-Effron, Arkady Mustaev
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Patent number: 8999977Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are 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: March 8, 2013Date of Patent: April 7, 2015Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
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Patent number: 8999978Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are 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: November 16, 2012Date of Patent: April 7, 2015Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
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Publication number: 20150094302Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: December 11, 2014Publication date: April 2, 2015Applicant: Genentech, Inc.Inventors: James John Crawford, Wendy B. Young
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Publication number: 20150080366Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.Type: ApplicationFiled: April 3, 2013Publication date: March 19, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Lee Fader, Pierre Louis Beaulieu, Murray Bailey, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Oliver Hucke, Marc-André Joly, Mélissa Leblanc, Olivier Lepage, Benoit Moreau, Julie Naud, Martin Poirier, Elisia Villemure
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Publication number: 20150065499Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, and Y are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.Type: ApplicationFiled: February 26, 2013Publication date: March 5, 2015Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Patent number: 8962607Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2013Date of Patent: February 24, 2015Assignee: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M McDonnell, Philip M Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20150051204Abstract: Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.Type: ApplicationFiled: March 28, 2012Publication date: February 19, 2015Applicant: SJT MOLECULAR RESEARCH, S.L.Inventors: Juan Carlos Agreda Navajas, Roberto Mikio Kassuya
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Publication number: 20150038438Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.Type: ApplicationFiled: August 29, 2012Publication date: February 5, 2015Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
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Publication number: 20150023990Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.Type: ApplicationFiled: September 30, 2014Publication date: January 22, 2015Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah J. Slania
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Publication number: 20140357647Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 7-substituted fangchinoline derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.Type: ApplicationFiled: January 21, 2013Publication date: December 4, 2014Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.Inventors: Frank Rong, Rongzhen Xu, Hongxi Lai, Fuwen Xie
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Publication number: 20140343015Abstract: A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C?O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.Type: ApplicationFiled: September 7, 2012Publication date: November 20, 2014Applicants: NIPPON CHEMIPHAR CO., LTD., THE KITASATO INSTITUTEInventors: Hiroshi Nagase, Hideaki Fujii, Eriko Nakata, Yoshikazu Watanabe, Toshihiro Takahashi
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Publication number: 20140343047Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 5-substituted tetrandrine derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.Type: ApplicationFiled: August 20, 2012Publication date: November 20, 2014Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
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Publication number: 20140336178Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.Type: ApplicationFiled: April 29, 2014Publication date: November 13, 2014Applicants: The General Hospital Corporation, Massachusetts Institute of TechnologyInventors: Aleksey G. Kazantsev, Anne B. Young, David E. Housman, Steven M. Hersch
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Publication number: 20140336188Abstract: N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.Type: ApplicationFiled: July 24, 2014Publication date: November 13, 2014Applicants: PURDUE RESEARCH FOUNDATION, THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETSRInventors: Mark S. CUSHMAN, Andrew E. MORRELL, Muthukaman NAGARAJAN, Yves G. POMMIER, Keli K. AGAMA, Smitha ANTONY
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Publication number: 20140329800Abstract: The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.Type: ApplicationFiled: December 13, 2012Publication date: November 6, 2014Inventors: Daxin Gao, Heping Yang, Yajun Yu
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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: 8865130Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.Type: GrantFiled: March 27, 2012Date of Patent: October 21, 2014Assignee: Vanderbilt UniversityInventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
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Publication number: 20140302987Abstract: Use of substituted isoquinolinones, isoquinolinediones, isoquinolinetriones and dihydroisoquinolinones of the general formula (I) or their respective salts where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.Type: ApplicationFiled: July 2, 2012Publication date: October 9, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Jens Frackenpohl, Hans-Joachim Zeiss, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döering, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills
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Patent number: 8853391Abstract: Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.Type: GrantFiled: December 3, 2009Date of Patent: October 7, 2014Assignee: Merck Patent GmbHInventors: Bayard R. Huck, Amanda E. Sutton, Benny C. Askew, Jr., Christopher Charles Victor Jones, Garry R. Smith, Nadia Brugger
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Publication number: 20140288068Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: OssiFi Inc.Inventors: Debra Ellies, Jean-Philippe Rey, F. Scott Kimball
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Patent number: 8822448Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: GrantFiled: March 7, 2013Date of Patent: September 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
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Publication number: 20140243311Abstract: The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is cyano or the like; R2 and R3 are hydrogen or the like; R4 is C1-6 alkyl or the like; R5 is C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, cycloalkyl-C1-6 alkyl, aralkyl or the like; R6 and R7 are each hydrogen, C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, C1-6 alkoxy-C1-6 alkyl, R12R13N—C1-6 alkyl or the like, which exhibit potent dopamine D2 receptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.Type: ApplicationFiled: March 12, 2012Publication date: August 28, 2014Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Toshihiro Nishimura, Hirotaka Teranshi, Masako Yoshida, Yasunori Ueno, Kiyoshi Kasai
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Publication number: 20140242121Abstract: The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.Type: ApplicationFiled: October 3, 2012Publication date: August 28, 2014Applicant: JANUS BIOTHERAPEUTICS, INC.Inventors: Grayson B. Lipford, Charles M. Zepp
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Publication number: 20140235616Abstract: The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.Type: ApplicationFiled: September 24, 2012Publication date: August 21, 2014Applicant: SANOFIInventors: Alexandre Benazet, Olivier Duclos, Nathalie Guillo, Gilbert Lassalle, Karim Macary, Valerie Vin
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Patent number: 8785639Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: GrantFiled: December 1, 2010Date of Patent: July 22, 2014Assignee: AbbVie Inc.Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
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Publication number: 20140194414Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are 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: March 8, 2013Publication date: July 10, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: MEDIVATION TECHNOLOGIES, INC.
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Publication number: 20140179671Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: September 12, 2013Publication date: June 26, 2014Applicant: Corcept Therapeutics, Inc.Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
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Publication number: 20140171407Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: February 17, 2014Publication date: June 19, 2014Applicant: Genentech, Inc.Inventors: Hazel Joan Dyke, Lewis Gazzard, Karen Williams, Huifen Chen, Samuel Kintz, Joy Drobnick, Joseph P. Lyssikatos, Simon Goodacre, Calum Macleod, Charles Ellwood
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Publication number: 20140163012Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.Type: ApplicationFiled: October 31, 2013Publication date: June 12, 2014Applicant: Albany Molecular Research, Inc.Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
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Publication number: 20140148451Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.Type: ApplicationFiled: May 9, 2012Publication date: May 29, 2014Applicants: Translational Genomics Research Institute, Van Andel Research InstituteInventors: Jeffrey Paul MacKeigan, Katie Renee Martin, Megan Lynne Goodall, Stephen Gately, Tong Wang
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Patent number: 8729072Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: November 2, 2012Date of Patent: May 20, 2014Assignee: F. Hoffman-La Roche AGInventors: James John Crawford, Wendy B. Young
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Patent number: 8716274Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: November 2, 2012Date of Patent: May 6, 2014Assignee: Genentech, Inc.Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
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Publication number: 20140121152Abstract: The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled release of an active agent. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an active agent from the prodrug so as to attenuate enzymatic cleavage of the prodrug.Type: ApplicationFiled: March 8, 2012Publication date: May 1, 2014Applicant: Signature Therapeutics, Inc.Inventors: Thomas E. Jenkins, Craig O. Husfeld
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Publication number: 20140107129Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: December 11, 2013Publication date: April 17, 2014Applicant: Galderma Research & DevelopmentInventors: Laurence CLARY, Sandrine CHAMBON, Laurent CHANTALAT, Carine ROSIGNOLI, Olivier ROYE, Jean-Claude PASCAL, Marlene SCHUPPLI-NOLLET
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Piperazinone-substituted tetrahydro-carboline MCH-1 antagonists, methods of making, and uses thereof
Patent number: 8697700Abstract: The present invention relates to piperazinone-substituted tetrahydrocarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.Type: GrantFiled: December 20, 2011Date of Patent: April 15, 2014Assignee: Albany Molecular Research, Inc.Inventors: Matthew D. Surman, Peter R. Guzzo -
Publication number: 20140093505Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.Type: ApplicationFiled: June 4, 2012Publication date: April 3, 2014Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Frank Wu, Yan Zhang
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Publication number: 20140079636Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.Type: ApplicationFiled: March 15, 2013Publication date: March 20, 2014Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Publication number: 20140073058Abstract: Methods of using dyes and associated technology are provided. A dye, such as a monomeric dye or a dimeric dye, may be used in a nucleic acid gel staining application and/or a nucleic acid detection application. Such a dye and a salt that comprises an anion that is associated with a strong acid and a cation that is associated with a strong base may be used in such an application. A dimeric dye, such as a dimeric dye capable of forming a hairpin-like structure, may be used to stain and/or detect nucleic acids via a release-on-demand mechanism. A dimeric dye having low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, may be used to stain and/or detect nucleic acids.Type: ApplicationFiled: August 8, 2013Publication date: March 13, 2014Applicant: Biotium, Inc.Inventors: Fei Mao, Wai-Yee Leung