Three Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/211.1)
-
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
-
Patent number: 8846951Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: GrantFiled: November 19, 2010Date of Patent: September 30, 2014Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
-
Publication number: 20140288047Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
-
Patent number: 8835422Abstract: The present invention provides substituted imidazoheterocycles having the general structure of formula I: wherein Y is chosen from —O—, —OCRgRh—, —CRgRhO—, —CRgRh—, —(CRgRh)2—, —NRi—, —CRgRhNRi— and —NRiCRgRh—. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: December 1, 2009Date of Patent: September 16, 2014Assignee: Cara Therapeutics, Inc.Inventors: Stephen J. O'Connor, Jason S. Newcom, Janet L. Ralbovsky, Gary R. Gustafson, R. Paul Beckett, Robert Zhiyong Luo
-
Patent number: 8828989Abstract: The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes of the formula wherein R1 and R2 are as defined herein and which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments.Type: GrantFiled: August 23, 2012Date of Patent: September 9, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Cosimo Dolente, Patrick Schnider
-
Publication number: 20140248378Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: July 5, 2012Publication date: September 4, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
-
Publication number: 20140243316Abstract: A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: wherein R is a hydrogen atom, a C1-6 alkyl group or the like, R1 is a C1-6 alkyl group, a C1-6 alkoxy group or the like, R2 is a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or the like, R3 is a hydrogen atom, a C1-6 alkyl group or the like, and R4 is a C1-6 alkyl group or the like.Type: ApplicationFiled: February 26, 2014Publication date: August 28, 2014Applicant: Eisai R&D Management Co., Ltd.Inventors: Mamoru Takaishi, Nobuhiro Sato, Tomoyuki Shibuguchi, Takafumi Motoki, Yoshinori Takahashi, Takeo Sasaki, Alan Braunton
-
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
-
Publication number: 20140206618Abstract: The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.Type: ApplicationFiled: August 16, 2012Publication date: July 24, 2014Inventors: Alexander Pasternak, Timothy Blizzard, Harry Chobanian, Reynalda de Jesus, Fa-Xiang Ding, Shuzhi Dong, Candido Gude, Dooseop Kim, Haifeng Tang, Shawn Walsh, Barbara Pio, Jinlong Jiang
-
Patent number: 8779154Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 25, 2007Date of Patent: July 15, 2014Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
-
Patent number: 8772301Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: GrantFiled: December 17, 2010Date of Patent: July 8, 2014Assignee: Sunovion Pharmaceuticals, Inc.Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
-
Publication number: 20140171411Abstract: A dual H1 inverse agonist/5-HT2A receptor antagonist of the formula (I), its uses, and methods for its preparation are described.Type: ApplicationFiled: August 22, 2012Publication date: June 19, 2014Applicant: C/O ELI LILLY AND COMPANYInventor: Andrew James Ledgard
-
Publication number: 20140171410Abstract: Compounds relating to batrachotoxin are provided, in particular analogues that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier, including vehicles that modulate transdermal permeation of the compound. The subject compounds are useful in treatments, including treatments to reduce neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the batrachotoxin-related compounds.Type: ApplicationFiled: December 13, 2013Publication date: June 19, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Justin Du Bois, Abigail Sloan Devlin, Matthew M. Logan, Frederic Menard, Tatsuya Toma
-
Publication number: 20140121199Abstract: A dual H1/5-HT2A receptor antagonist of the formula:, its uses, and methods for its preparation are described.Type: ApplicationFiled: July 2, 2012Publication date: May 1, 2014Applicant: ELI LILLY AND COMPANYInventor: Andrew James Ledgard
-
Publication number: 20140080808Abstract: The present invention relates to a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof having an excellent effect of inhibiting 11?-hydroxysteroid dehydrogenase type 1: General formula (I) wherein R1 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from substituent group A or a heterocyclic group that may be substituted with 1 to 4 group(s) independently selected from substituent group A; R2 independently represents a halogen atom or a C1-C6 alkyl group; n represents an integer of 0 to 2; and substituent group A represents the group consisting of halogen atoms, C1-C6 alkyl groups, and so forth.Type: ApplicationFiled: October 18, 2013Publication date: March 20, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Makoto Mori, Kunihiko Fujii, Masaharu Inui, Takayuki Baba, Yukari Onishi, Atsushi Aoyagi
-
Publication number: 20140044706Abstract: Methods and compositions are provided for treating hyperproliferative disorders in patients with a PI3K inhibitor, GDC-0032 as a single agent or in combination with chemotherapeutic agents.Type: ApplicationFiled: June 7, 2013Publication date: February 13, 2014Inventors: Marcia Belvin, Lori Friedman, Deepak Sampath, Jeffrey Wallin
-
Patent number: 8614207Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: GrantFiled: July 9, 2012Date of Patent: December 24, 2013Assignee: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
-
Publication number: 20130338141Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.Type: ApplicationFiled: August 19, 2013Publication date: December 19, 2013Inventors: Richard C. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddes, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
-
Patent number: 8586574Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: November 20, 2012Date of Patent: November 19, 2013Assignee: Genentech, Inc.Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
-
Publication number: 20130302282Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: October 21, 2011Publication date: November 14, 2013Applicant: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
-
Patent number: 8569285Abstract: Compounds of formula (I): wherein R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphonylaminoalkyl or N-hydroxycarboximidamide group. Medicinal products containing the same which are useful as modulators of the AMPA receptor.Type: GrantFiled: September 15, 2011Date of Patent: October 29, 2013Assignee: Les Laboratoires ServierInventors: Alexis Cordi, Patrice Desos, Pierre Lestage, Laurence Danober
-
Patent number: 8557738Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof (wherein, R1 to R6 each independently represents a hydrogen atom, unsubstituted or substituted C1-20 alkyl group and the like, R1 and R2, R3 and R4, or R5 and R6 may together form an unsubstituted or substituted 5- to 8-membered ring, A-B, in which A represents a carbon atom and B represents a nitrogen atom, represents the formula: C?N and the like, Y represents an oxygen atom and the like, X and X? each independently represent an unsubstituted or substituted C1-20 alkyl group and the like, m represents an integer of 0 to 2, and n represents an integer of 0 to 4), and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof, demonstrates reliable effects and can be used safely.Type: GrantFiled: August 10, 2009Date of Patent: October 15, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Masahiro Yokoyama, Kotaro Shibayama, Motoaki Sato
-
Publication number: 20130261105Abstract: This invention relates to novel pyrazolopyrimidines and their use as metabotropic glutamate 5 receptor antagonists (mGlu5 receptor antagonists), pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of mGlu5 receptor mediated disorders.Type: ApplicationFiled: March 27, 2013Publication date: October 3, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk GOTTSCHLING, Heiner EBEL, Doris RIETHER, Bernd WELLENZOHN
-
Publication number: 20130261103Abstract: Pyridazinone compounds of Formula I 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: ApplicationFiled: August 31, 2011Publication date: October 3, 2013Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
-
Patent number: 8546377Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: GrantFiled: October 21, 2010Date of Patent: October 1, 2013Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
-
Patent number: 8536164Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: December 13, 2011Date of Patent: September 17, 2013Assignee: Pfizer Inc.Inventors: Todd W. Butler, Ramalakshmi Y. Chandrasekaran, Scot R. Mente, Chakrapani Subramanyam, Travis T. Wager
-
Patent number: 8530463Abstract: Multimodal particulate formulations of medicaments and methods for their use, e.g. by nasal or pulmonary administration for the treatment of various medical conditions, are provided.Type: GrantFiled: November 6, 2008Date of Patent: September 10, 2013Assignees: Hale Biopharma Ventures LLC, Aegis Therapeutics, LLCInventors: Steve Cartt, David Medeiros, Edward T. Maggio
-
Publication number: 20130225558Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. 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: February 18, 2011Publication date: August 29, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
-
Patent number: 8518933Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2 -a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7 -octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2 -a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: GrantFiled: April 22, 2010Date of Patent: August 27, 2013Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Bhadra Shelat, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
-
Publication number: 20130217672Abstract: A (+)-3-hydroxymorphinan-based polycycle derivative of formula (I) is effective as a neuroprotective agent for neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and ischemic stroke.Type: ApplicationFiled: May 13, 2011Publication date: August 22, 2013Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Jong Yup Kim, Jeongmin Kim, Kwang Woo Ahn
-
Publication number: 20130217666Abstract: The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: February 15, 2013Publication date: August 22, 2013Applicant: Genentech, Inc.Inventor: Genentech, Inc.
-
Publication number: 20130210803Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-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: February 18, 2011Publication date: August 15, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
-
Patent number: 8507470Abstract: The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: July 27, 2010Date of Patent: August 13, 2013Assignees: Sanofi, Mitsubishi Electric CorporationInventors: Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
-
Patent number: 8501728Abstract: The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: July 27, 2010Date of Patent: August 6, 2013Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
-
Publication number: 20130079331Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 20, 2012Publication date: March 28, 2013Applicant: GENENTECH, INC.Inventor: GENENTECH, INC.
-
Patent number: 8404674Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: March 4, 2008Date of Patent: March 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
-
Publication number: 20130039904Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.Type: ApplicationFiled: August 2, 2010Publication date: February 14, 2013Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.Inventor: Lifeng Xu
-
Publication number: 20130035326Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 18, 2010Publication date: February 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
-
Patent number: 8367655Abstract: The present invention discloses pyridoindolobenzox- and thiazepine compositions of Formula 1, wherein A is —CH(R9)—X—, —XCH(R9)—; —CO—X— or —X—CO—; X is —O—, —S—, —SO—, or —SO2—. Y is a single bond or a double bond. D and E are independently —(CH2)n—; and ‘n’ varies from 0 to 2. R1 to R9 are various electron donating, electron withdrawing, hydrophilic, or lipophilic groups selected to optimize the physicochemical and biological properties of compounds of Formula I.Type: GrantFiled: July 2, 2010Date of Patent: February 5, 2013Assignee: Daya Drug Discoveries, Inc.Inventor: Parthasarathi Rajagopalan
-
Publication number: 20130005706Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
-
Patent number: 8343955Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: May 22, 2012Date of Patent: January 1, 2013Assignee: Genentech, Inc.Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
-
Patent number: 8329687Abstract: The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action, which is represented by the formula wherein A is —OR1 or —S(O)pR2, R1 and R2 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group to optionally having substituent(s), and p is 0, 1 or 2, or a salt thereof.Type: GrantFiled: November 14, 2008Date of Patent: December 11, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Matsumoto, Tomokazu Kusumoto
-
Publication number: 20120309724Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
-
Patent number: 8324201Abstract: Provided is a compound having a serotonin 5-HT2C receptor activating action. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: July 28, 2011Date of Patent: December 4, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigekazu Sasaki, Tomokazu Kusumoto
-
Patent number: 8318722Abstract: Provided is a compound having a serotonin 5-HT2C receptor activating action. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: June 14, 2010Date of Patent: November 27, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigekazu Sasaki, Tomokazu Kusumoto
-
Patent number: 8318720Abstract: In part, the present invention is directed to antibacterial compounds.Type: GrantFiled: July 19, 2007Date of Patent: November 27, 2012Assignee: Affinium Pharmaceuticals, Inc.Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
-
Patent number: 8314088Abstract: Provided is a compound having a serotonin 5-HT2C receptor activating action. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: July 28, 2011Date of Patent: November 20, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigekazu Sasaki, Tomokazu Kusumoto
-
Publication number: 20120276051Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: July 9, 2012Publication date: November 1, 2012Applicant: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
-
Publication number: 20120251497Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: April 25, 2012Publication date: October 4, 2012Inventors: Min Zhong, Leping Li
-
Publication number: 20120252780Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 29, 2010Publication date: October 4, 2012Inventors: Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch