Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 540/521)
  • Patent number: 10358441
    Abstract: The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors.
    Type: Grant
    Filed: February 16, 2018
    Date of Patent: July 23, 2019
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: In Jong Kim, Jianming Yu, Thomas P. Blaisdell, Joseph Panarese, Brian C. Shook, Yat Sun Or
  • Publication number: 20150148334
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 28, 2015
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Patent number: 8952003
    Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: February 10, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Patent number: 8846951
    Abstract: 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: Grant
    Filed: November 19, 2010
    Date of Patent: September 30, 2014
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: 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: 20140275019
    Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHD
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
  • Publication number: 20140275033
    Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
  • Patent number: 8779154
    Abstract: 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: Grant
    Filed: September 25, 2007
    Date of Patent: July 15, 2014
    Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
  • Publication number: 20140194410
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: November 7, 2013
    Publication date: July 10, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Matthew O. Duffey, Amy M. Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
  • Publication number: 20140179676
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: ABBVIE INC.
    Inventors: Kevin P. Cusack, Thomas D. Gordon, Michael Z. Hoemann, David C. Ihle, Bin Li, Gloria Y. Lo Schiavo, Gagandeep K. Somal, Michael Friedman, Martin E. Hayes, Wouter Iwema Bakker
  • Publication number: 20140128375
    Abstract: Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Inventors: Ian M. Bell, Harold B. Selnick
  • Publication number: 20140045821
    Abstract: Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 13, 2014
    Inventors: Peter Wipf, Qiming Jan Wang
  • Patent number: 8637501
    Abstract: 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 in the present invention.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 28, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Matthew David Surman, James Francis Grabowski, Jr., Emily Elizabeth Freeman
  • Patent number: 8598158
    Abstract: The present invention relates to certain lactam ring-containing compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein D, E, X1, R1, R2, R3, R4, R9, and R10 are as herein described. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma, and chronic obstructive pulmonary disorder.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: December 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong Xiao, Anandan Palani, Robert G. Aslanian, Sylvia Degrado, Xianhai Huang, Wei Zhou, Michael Sofolarides, Xiao Chen
  • Publication number: 20130310366
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 21, 2013
    Applicant: Albany Molecular Research, Inc.
    Inventors: David D. MANNING, Christopher L. CIOFFI
  • Publication number: 20130267498
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: February 13, 2013
    Publication date: October 10, 2013
    Inventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
  • Publication number: 20130252943
    Abstract: In one aspect, the invention relates to substituted bicyclic oxazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: February 27, 2013
    Publication date: September 26, 2013
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, María Luz Martín-Martín
  • Publication number: 20130237523
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 12, 2013
    Applicant: AFFINIUM PHARMACEUTICALS, INC.
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20130210804
    Abstract: The present invention is directed to tricyclic compounds which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 20, 2011
    Publication date: August 15, 2013
    Inventors: Neville J. Anthony, Robert P. Gomez, Jing Li, Swati P. Mercer, Anthony J. Roecker, Craig A. Stump, Theresa M. Williams
  • Patent number: 8507667
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: August 13, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Matthew O. Duffey, Amy M. Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
  • Patent number: 8431566
    Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.
    Type: Grant
    Filed: September 30, 2011
    Date of Patent: April 30, 2013
    Assignee: Infinity Discovery, Inc.
    Inventors: Alfredo Castro, Michael J. Grogan, Andre Lescarbeau, Martin Tremblay
  • Publication number: 20130045962
    Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
    Type: Application
    Filed: November 6, 2008
    Publication date: February 21, 2013
    Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart
  • Publication number: 20130029972
    Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt or hydrate, and a pharmaceutical composition containing said compound, or a pharmaceutically acceptable salt or hydrate, useful as a Notch pathway signaling inhibitor for the treatment of cancer.
    Type: Application
    Filed: July 18, 2012
    Publication date: January 31, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventors: Philip Arthur HIPSKIND, Gregory Alan STEPHENSON
  • Publication number: 20120316154
    Abstract: The present invention relates to certain lactam ring-containing compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein D, E, X1, R1, R2, R3, R4, R9, and R10 are as herein described. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma, and chronic obstructive pulmonary disorder.
    Type: Application
    Filed: December 9, 2010
    Publication date: December 13, 2012
    Inventors: Dong Xiao, Anandan Palani, Robert G Aslanian, Sylvia Degrado, Xianhai Huang, Wei Zhou, Michael Sofolarides, Xiao Chen
  • Publication number: 20120309743
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 9, 2012
    Publication date: December 6, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
  • Publication number: 20120302551
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 9, 2012
    Publication date: November 29, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
  • Publication number: 20120302550
    Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
    Type: Application
    Filed: February 10, 2011
    Publication date: November 29, 2012
    Applicant: Pfizer Inc.
    Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
  • Publication number: 20120295887
    Abstract: Pharmaceutically acceptable salts of pyrrolo-nitrogenous heterocyclic derivatives, preparation method and medical use thereof are disclosed. More specifically, pharmaceutically acceptable salts of (R,Z)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-methylene)-5-(2-hydroxy-3-morpholinyl-4-yl-propyl)-3-methyl-5,6,7,8-tetrahydro-1H-pyrrolo[3,2-c]azepin-4-one presented by formula (I), the preparation method and the use thereof as therapeutic agents, especially as protein kinase inhibitors, are disclosed.
    Type: Application
    Filed: January 7, 2011
    Publication date: November 22, 2012
    Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD., JIANGSU HENGRUI MEDICINE CO., LTD.
    Inventor: Peng Cho Tang
  • Publication number: 20120258955
    Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.
    Type: Application
    Filed: December 16, 2010
    Publication date: October 11, 2012
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Gregor James MacDonald, Andrés Avelino Trabanco-Suárez, Susana Conde-Ceide, Gary John Tresadern, José Manuel Bartolomé-Nebreda, Joaquin Pastor-Fernández
  • Publication number: 20120251491
    Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: May 12, 2010
    Publication date: October 4, 2012
    Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
  • Patent number: 8268992
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: September 18, 2012
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
  • Publication number: 20120219641
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 30, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: David D. Manning, Christopher Lawrence Cioffi
  • Publication number: 20120214794
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: October 13, 2011
    Publication date: August 23, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20120202750
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 9, 2012
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Publication number: 20120184530
    Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.
    Type: Application
    Filed: March 27, 2012
    Publication date: July 19, 2012
    Applicant: TETRALOGIC PHARMACEUTICALS CORPORATION
    Inventor: Stephen M. CONDON
  • Publication number: 20120172348
    Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: July 22, 2010
    Publication date: July 5, 2012
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Patent number: 8183365
    Abstract: Methods are provided for preparing compounds of the general formula (I) wherein X1 is an aryl hydrocarbon group optionally substituted with one or more groups independently selected from —R, —NH2, —NHR, —NR2, —OH, —OR, —F, —Cl, —Br, —I, —CF3, —C(?O)OH, —C(?O)OR, —C(?O)NH2, —C(?O)NHR, and —C(?O)NR2; X2 is —H, —R, —NHR, —NR2, —OR, —F, —Cl, —Br, or —I; and R is C1 to C10 hydrocarbyl. The methods comprise a double-dehydrogenation reaction step in which a functionalized aminohydroazepinone skeleton comprising an aminoimidazole ring is reacted with 2-iodoxybenzene to form the imidazo[4,5-d]azepine ring system present in formula (I). Example methods comprising the double-dehydrogenation reaction step are provided as efficient synthetic routes to ceratamine A, ceratamine B, and the des-methyl analogs thereof.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: May 22, 2012
    Assignee: The Ohio State University
    Inventors: Robert S. Coleman, Erica L. Campbell, Daniel J. Carper
  • Patent number: 8153623
    Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: April 10, 2012
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
  • Publication number: 20120083484
    Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.
    Type: Application
    Filed: September 30, 2011
    Publication date: April 5, 2012
    Inventors: Alfredo Castro, Michael J. Grogan, Andre Lescarbeau, Martin Tremblay
  • Publication number: 20120070409
    Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Application
    Filed: February 3, 2011
    Publication date: March 22, 2012
    Applicant: Japan Tobacco Inc.
    Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
  • Publication number: 20120065190
    Abstract: Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: December 14, 2007
    Publication date: March 15, 2012
    Inventors: Ian M. Bell, Harold G. Selnick
  • Publication number: 20110257157
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 30, 2011
    Publication date: October 20, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
  • Patent number: 7998952
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: August 16, 2011
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
  • Patent number: 7968535
    Abstract: This invention relates to the use of azapaullones, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA and neurodegenerative disorders.
    Type: Grant
    Filed: May 4, 2006
    Date of Patent: June 28, 2011
    Assignees: Develogen Atkiengesellschaft, Technische Universitaet Carolo-Wilhelmina Zu Braunschweig
    Inventors: Rainer Mussmann, Conrad Peter Kunick, Hendrik Stukenbrock, Marcus Geese, Simone Kegel, Ulrike Burk
  • Patent number: 7968536
    Abstract: The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: June 28, 2011
    Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
  • Patent number: 7964590
    Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: June 21, 2011
    Assignee: Infinity Discovery, Inc.
    Inventors: Alfredo C. Castro, Michael J. Grogan, Andre Lescarbeau, Martin Tremblay
  • Publication number: 20110130382
    Abstract: 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: Application
    Filed: October 21, 2010
    Publication date: June 2, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
  • Patent number: 7951795
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, G1, G2, G3, J, m, n, p, R1, R2, R3, R4 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: May 31, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Harold G. Selnick
  • Publication number: 20110118231
    Abstract: 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: Application
    Filed: November 19, 2010
    Publication date: May 19, 2011
    Applicants: ABBOTT LABORATORIES, ABBOTT GMBH & CO. KG
    Inventors: 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: 20110086834
    Abstract: Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
    Type: Application
    Filed: June 26, 2009
    Publication date: April 14, 2011
    Applicant: AMGEN INC.
    Inventors: Guoqing Chen, Timothy D. Cushing, Paul Faulder, Benjamin Fisher, Xiao He, Kexue Li, Zhihong Li, Wen Liu, Lawrence R. Mcgee, Vatee Pattaropong, Jennifer L. Seganish, Youngshook Shin, Zhulun Wang
  • Publication number: 20110053910
    Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
    Type: Application
    Filed: July 3, 2006
    Publication date: March 3, 2011
    Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring