Additional Chalcogen Double Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 540/518)
  • Patent number: 9212187
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: December 15, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kunio Oshima, Shuuji Matsumura, Hokuto Yamabe
  • Patent number: 8940889
    Abstract: A process for producing a compound represented by formula (1), wherein each of R1, R2, R3 and R4, which may be the same or different, represents a hydrogen atom or a lower alkyl group, the process includes deprotecting a protective group (R5) of a compound represented by formula (2), wherein R1, R2, R3 and R4 are as defined above, and R5 represents a protective group of a hydroxy group. The process is an industrially advantageous, simple, and efficient process for producing a key intermediate of a benzo[b][1,4]diazepine-2,4-dione compound, which is a therapeutic medicine for arrhythmia.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: January 27, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hisayuki Tsujimori, Shinichi Taira, Hirotaka Yukawa, Kaoru Abe
  • Publication number: 20140357858
    Abstract: The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R1 and R2 represent hydrogen atom and the like, or R1 and R2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R3 and R4 represent hydrogen atom and the like, R5 represents hydrogen atom and the like, R6 and R7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(?O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(?O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(?O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.
    Type: Application
    Filed: January 10, 2013
    Publication date: December 4, 2014
    Inventors: Masatoshi Ushioda, Kunio Kobayashi, Daisuke Saito, Shogo Sakuma, Toshiyasu Imai, Kazuhide Inoue
  • Publication number: 20140343278
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Application
    Filed: June 25, 2014
    Publication date: November 20, 2014
    Inventors: Kunio OSHIMA, Shuuji MATSUMURA, Hokuto YAMABE
  • Patent number: 8822453
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: September 2, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Takashi Oshiyama, Tsuyoshi Nagase, Masataka Ueda, Kuninori Tai
  • Patent number: 8796447
    Abstract: A process for producing a compound represented by formula (1), wherein each of R1, R2, R3 and R4, which may be the same or different, represents a hydrogen atom or a lower alkyl group, the process includes deprotecting a protective group (R5) of a compound represented by formula (2), wherein R1, R2, R3 and R4 are as defined above, and R5 represents a protective group of a hydroxy group. The process is an industrially advantageous, simple, and efficient process for producing a key intermediate of a benzo[b][1,4]diazepine-2,4-dione compound, which is a therapeutic medicine for arrhythmia.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: August 5, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hisayuki Tsujimori, Shinichi Taira, Hirotaka Yukawa, Kaoru Abe
  • Publication number: 20140194621
    Abstract: A process for producing a compound represented by formula (1), wherein each of R1, R2, R3 and R4, which may be the same or different, represents a hydrogen atom or a lower alkyl group, the process includes deprotecting a protective group (R5) of a compound represented by formula (2), wherein R1, R2, R3 and R4 are as defined above, and R5 represents a protective group of a hydroxy group. The process is an industrially advantageous, simple, and efficient process for producing a key intermediate of a benzo[b][1,4]diazepine-2,4-dione compound, which is a therapeutic medicine for arrhythmia.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 10, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hisayuki TSUJIMORI, Shinichi TAIRA, Hirotaka YUKAWA, Kaoru ABE
  • Patent number: 8664217
    Abstract: The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; Al is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.
    Type: Grant
    Filed: August 22, 2012
    Date of Patent: March 4, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Kunio Oshima, Takashi Oshiyama, Shinichi Taira, Yasuhiro Menjo, Hokuto Yamabe, Shuuji Matsumura, Masataka Ueda, Yasuo Koga, Kuninori Tai, Sunao Nakayama, Toshiyuki Onogawa, Kenji Tsujimae
  • Publication number: 20140031334
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
  • Publication number: 20130150350
    Abstract: Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: February 9, 2011
    Publication date: June 13, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Bruno Simoneau, Patrick Deroy, Lee Fader, Anne-Marie Faucher, Alexander Gagnon, Chantal Grand-Maitre, Stephen Kawai, Serge Landry, Jean-Francois Mercier, Jean Rancourt
  • Publication number: 20130040941
    Abstract: The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.
    Type: Application
    Filed: August 22, 2012
    Publication date: February 14, 2013
    Inventors: Kunio Oshima, Takashi Oshiyama, Shinichi Taira, Yasuhiro Menjo, Hokuto Yamabe, Shuuji Matsumura, Masataka Ueda, Yasuo Koga, Kuninori Tai, Sunao Nakayama, Toshiyuki Onogawa, Kenji Tsujimae
  • Patent number: 8338406
    Abstract: The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: December 25, 2012
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Kunio Oshima, Takashi Oshiyama, Shinichi Taira, Yasuhiro Menjo, Hokuto Yamabe, Shuuji Matsumura, Masataka Ueda, Yasuo Koga, Kuninori Tai, Sunao Nakayama, Toshiyuki Onogawa, Kenji Tsujimae
  • Publication number: 20120149899
    Abstract: The present invention provides an industrially advantageous, simple, and efficient process for producing a key intermediate of a benzo[b][1,4]diazepine-2,4-dione compound, which is a therapeutic medicine for arrhythmia. The present invention relates to a process for producing a compound represented by formula (1), wherein each of R1, R2, R3 and R4, which may be the same or different, represents a hydrogen atom or a lower alkyl group, the process including deprotecting a protective group (R5) of a compound represented by formula (2), wherein R1, R2, R3 and R4 are as defined above, and R5 represents a protective group of a hydroxy group.
    Type: Application
    Filed: August 20, 2010
    Publication date: June 14, 2012
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hisayuki Tsujimori, Shinichi Taira, Hirotaka Yukawa, Kaoru Abe
  • Publication number: 20120108575
    Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.
    Type: Application
    Filed: January 12, 2012
    Publication date: May 3, 2012
    Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.
    Inventors: Kevin C. Brown, R, Richard Goehring, Yoshiyasu BABA, Naoki Tsuno
  • Patent number: 8119631
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: February 21, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
  • Publication number: 20110178070
    Abstract: The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: June 23, 2009
    Publication date: July 21, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Xianchang Gong, Bohan Jin, Massaki Hirose, Feng Zhou, Qing Dong
  • Publication number: 20110105477
    Abstract: The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.
    Type: Application
    Filed: September 12, 2008
    Publication date: May 5, 2011
    Applicant: The Regents of the University of Michigan
    Inventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
  • Publication number: 20100331317
    Abstract: The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.
    Type: Application
    Filed: February 20, 2009
    Publication date: December 30, 2010
    Inventors: Kunio Oshima, Takashi Oshiyama, Shinichi Taira, Yasuhiro Menjo, Hokuto Yamabe, Shuuji Matsumura, Masataka Ueda, Yasuo Koga, Kuninori Tai, Sunao Nakayama, Toshiyuki Onogawa, Kenji Tsujimae
  • Patent number: 7655647
    Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: February 2, 2010
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20100022519
    Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.
    Type: Application
    Filed: July 15, 2009
    Publication date: January 28, 2010
    Inventors: Kevin C. Brown, R. Richard Goehring, Yoshiyasu Baba, Naoki Tsuno
  • Patent number: 7456172
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: November 25, 2008
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Patent number: 7390801
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: June 24, 2008
    Assignees: Athena Neurosciences, Inc., Eli Lilly and Company
    Inventors: Eugene D. Thorsett, Michael A. Pleiss, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Bruce A. Dressman, James J. Droste, Steven S. Henry, Russell D. Stucky, Warren J. Porter
  • Patent number: 7342008
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: September 18, 2006
    Date of Patent: March 11, 2008
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Hong Liu, Lorin Andrew Thompson
  • Patent number: 7169773
    Abstract: The present invention provides a compound of formula I comprising: a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof.
    Type: Grant
    Filed: June 30, 2005
    Date of Patent: January 30, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerzy Ryszard Szewczyk, Kelly H. Donaldson
  • Patent number: 7053084
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: February 17, 2000
    Date of Patent: May 30, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventor: Richard E. Olson
  • Patent number: 6838455
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: January 4, 2005
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
  • Patent number: 6774125
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: August 10, 2004
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
  • Patent number: 6696438
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: December 12, 2002
    Date of Patent: February 24, 2004
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Bruce A. Dressman, Qing Shi
  • Patent number: 6683075
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: January 27, 2004
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Patent number: 6673921
    Abstract: A process for the preparation of the compound (I) or an acid addition salt thereof which comprises reacting a compound of formula (II), wherein R is an optionally substituted benzyl group under concomitant reduction and hydrogenolysis conditions, followed, if required, by isolation of the compound as an acid addition salt thereof.
    Type: Grant
    Filed: February 19, 2003
    Date of Patent: January 6, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: David Colclough, Anne Hodgson
  • Patent number: 6653303
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: November 25, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Publication number: 20030149027
    Abstract: A compound represented by the formula (I) 1
    Type: Application
    Filed: June 28, 2001
    Publication date: August 7, 2003
    Inventors: Satoru Oi, Nobuhiro Suzuki, Takahiro Matsumoto
  • Patent number: 6569851
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: May 27, 2003
    Assignees: Elan Pharmaceutials, Inc., Eli Lilly & Company
    Inventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. VanMeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Patent number: 6303625
    Abstract: The invention is directed to novel triazolopyridine derivatives which are useful as antagonists of GPIIb/IIIa. Pharmaceutical compositions comprising the triazolopyridine derivatives of the present invention, methods of treating conditions mediated by GPIIb/IIIa (e.g., methods for treating platelet-mediated thrombotic disorders) along with processes for making the compounds and novel intermediates are also disclosed.
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: October 16, 2001
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: William J. Hoekstra, Edward C. Lawson, Bruce E. Maryanoff
  • Patent number: 6255479
    Abstract: A method for preparing an &agr;-oxolactam comprising, reacting a corresponding &agr;-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding &agr;-oxolactam.
    Type: Grant
    Filed: December 29, 1998
    Date of Patent: July 3, 2001
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Akireddy Srinivasa Rao
  • Patent number: 6171578
    Abstract: The invention provides compounds comprising glycoprotein IIb/IIIa receptor-binding benzodiazepine derivatives covalently linked to metal ion chelators. The compounds of the invention may be labeled with a radionuclide such as 99mTc and used to image thrombi.
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: January 9, 2001
    Assignees: Diatide, Inc., Genentech, Inc.
    Inventors: Richard T. Dean, John Lister-James, Michael C. Venuti, Todd C. Somers
  • Patent number: 6130234
    Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, glaucoma, CMV retinitis, chronic pain, opioid tolerance or withdrawals, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: October 10, 2000
    Assignees: Warner-Lambert Company, Cocensys, Incorporated
    Inventors: Christopher F. Bigge, Jonathan Wright, Sui Xiong Cai, Eckard Weber, Richard Woodward, Nancy C. Lan, Zhang-Lin Zhou, John F. W. Keana
  • Patent number: 5910495
    Abstract: A method of controlling gastric emptying in patients having an early non-insulin-dependent diabetic condition and exhibiting rapid gastric emptying comprising the administration of an effective gastric emptying controlling amount of a compound of Formula (I) ##STR1## or a physiologically acceptable salt or solvate thereof.
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: June 8, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventor: Rochelle Marie Hanley
  • Patent number: 5859007
    Abstract: Benzo?b!?1,4!diazepine compounds of formula (I), where R.sup.1 is selected from C.sub.1 C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, or substituted phenyl; R.sup.2 is selected from C.sub.3 -C.sub.6 alkyl, C.sub.3 C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 alkenyl, benzyl, phenylC.sub.1 -C.sub.3 alkyl of substituted phenyl; or NR.sup.1 R.sup.2 together form 1,2,3,4-tetrahydroquinoline or benzazepine, mono-, di-, or trisubstituted independently with C.sub.1-6 alkyl C.sub.1-6 alkoxy or halogen substituents; p is an integer 0 or 1; q is an integer 0 or 1; r is an integer 0 or 1; t is an integer 0 or 1, provided that when r is 0 then t is 0; R.sup.3, R.sup.5, and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl; R.sup.4 is C.sub.1-6 alkyl or C.sub.1-6 alkenyl; R.sup.7 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.1-6 cycloalkyl, C.sub.1-6 alkenyl, phenyl, substituted phenyl, napthyl, heteroaryl, substituted heteroaryl, bicycloheteroaryl or substituted bicycloheteroaryl; or NR.sup.
    Type: Grant
    Filed: November 14, 1996
    Date of Patent: January 12, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: Christopher Joseph Aquino, Marcus Brackeen, Milana Dezube, Brad Richard Henke, Gavin Charles Hirst, Peter Walter Jeffs, Tanya Momtahen, Elizabeth Ellen Sugg, Edward Martin Suh, Timothy Mark Willson
  • Patent number: 5834463
    Abstract: Compounds represented by the formula: ##STR1## wherein ring A is benzene; Ar is aromatic group; R.sup.1, R.sup.2 and R.sup.3 each stands for H, acyl, hydrocarbon or heterocyclic, or R.sup.2 and R.sup.3, taken together, may form non-aromatic cyclic hydrocarbon; X is methylene or carbonyl; ......... is single bond or double bond; when ......... is single bond, Y is --NR.sup.4 -- (R.sup.4 is H, acyl, hydrocarbon or heterocyclic), when ......... is double bond, Y is N; n is 1-3, provided that, X is carbonyl and, at the same time, R.sup.2 and R.sup.3, taken together, form non-aromatic cyclic hydrocarbon, ......... is double bond or R.sup.4 is a heterocyclic or --Z(CH.sub.2).sub.m --W (Z is methylene or carbonyl, W is optionally substituted amino, and m denotes 0-5), or salts thereof have an excellent GnRH receptor antagonistic action and/or an action of improving sleep disturbances.
    Type: Grant
    Filed: June 26, 1995
    Date of Patent: November 10, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Nobuhiro Fujii, Koichi Kato, Masaomi Miyamoto
  • Patent number: 5776929
    Abstract: A benzodiazepine derivative of the formula (I): ##STR1## wherein R.sub.1 is a bond, --CH.sub.2 --, --CH.sub.2 O--, --SCH.sub.2 -- or a group of the formula: ##STR2## R.sub.2 is a lower alkyl, --COOR.sub.5, --CONH(CH.sub.2).sub.n COOR.sub.5, --CONHSO.sub.2 R.sub.5, --SO.sub.2 NHCOR.sub.5, or an optionally substituted heterocyclic group (R.sub.5 is a hydrogen atom, lower alkyl or benzyl and n is an integer of 1 to 5); R.sub.3 is a bond, --CO-- or --CONH--; and R.sub.4 is an optionally substituted heterocyclic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: July 7, 1998
    Assignee: Shionogi & Co., Ltd.
    Inventors: Sanji Hagishita, Susumu Kamata, Kaoru Seno, Nobuhiro Haga, Yasunobu Ishihara
  • Patent number: 5739129
    Abstract: Compounds of general formula (I) and physiologically salts thereof, processes for their preparation and their use as modulators of the effects of gastrin and CCK.
    Type: Grant
    Filed: October 11, 1996
    Date of Patent: April 14, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Christopher Joseph Aquino, Elizabeth Ellen Sugg, Jerzy Ryszard Szewczyk
  • Patent number: 5733867
    Abstract: Compounds of general formula (I) ##STR1## wherein R.sup.1 represents a phenyl, C.sub.3-7 cycloalkyl, C.sub.7-11 bridgedcycloalkyl or C.sub.1-6 alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C.sub.1-6 alkoxycarbonyl, C.sub.3-7 cycloalkyl, or C.sub.3-7 bridgedcycloalkyl group;R.sup.2 represents phenyl substituted by a group (CH.sub.2).sub.n NR.sup.4 R.sup.5, O(CH.sub.2).sub.p R.sup.6, or (CH.sub.2).sub.n CO.sub.2 R.sup.11 ;R.sup.3 represents phenyl optionally substituted by one or 2 halogen atoms;R.sup.4 represents hydrogen or C.sub.1-4 alkyl;R.sup.5 represents acyl, or C.sub.2-4 alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C.sub.1-4 alkyl or hydroxy groups.R.sup.6 represents hydroxy, C.sub.1-4 alkoxy, CO.sub.2 R.sup.7 or NR.
    Type: Grant
    Filed: November 4, 1996
    Date of Patent: March 31, 1998
    Assignee: Glaxo Wellcome SpA
    Inventors: Giovanni Curotto, Mario Pellegatti, Stefano Polinelli
  • Patent number: 5716953
    Abstract: Compounds of formula (I) ##STR1## wherein the substituents are defined in the specification are antagonists of gastrin and CCK.
    Type: Grant
    Filed: March 22, 1996
    Date of Patent: February 10, 1998
    Assignee: Glaxo Wellcome S.p.A.
    Inventors: Daniele Donati, Antonella Ursini, Mauro Corsi
  • Patent number: 5700797
    Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 23, 1997
    Assignee: Merck & Co, Inc.
    Inventors: David A. Claremon, Nigel Liverton, Harold G. Selnick
  • Patent number: 5686449
    Abstract: The invention relates to compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof having gastrin and/or CCK-B antagonist activity.
    Type: Grant
    Filed: October 23, 1995
    Date of Patent: November 11, 1997
    Assignee: Glaxo Wellcome S.p.A.
    Inventors: Maria Elvira Tranquillini, Gabriella Finizia, Antonella Ursini
  • Patent number: 5646140
    Abstract: This invention pertains to novel benzodiazepine compounds of formula (I) ##STR1## which exhibit agonistic activity for CCK-A receptors, enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals for use in medicine as anorectic agents in the regulation of appetite, the treatment of obesity and the maintenance of weight loss.
    Type: Grant
    Filed: October 13, 1995
    Date of Patent: July 8, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: Elizabeth Ellen Sugg, Christopher Joseph Aquino, Jerzy Ryszard Szewczyk, Harry Finch, Robin Arthur Ellis Carr
  • Patent number: 5641775
    Abstract: The invention relates to 3-phenylureido-1,5-benzodiazepine-diones of formula (I) ##STR1## and pharmaceutically acceptable salts and solvates thereof, and to their use as gastrin/CCK-B antagonists.
    Type: Grant
    Filed: October 23, 1995
    Date of Patent: June 24, 1997
    Assignee: Glaxo SpA
    Inventors: Harry Finch, David Gordon Trist, Aldo Feriani, Giorgio Tarzia, Pritom Shah
  • Patent number: 5637697
    Abstract: This invention relates to compounds of formula (IV) which are useful as intermediates in the preparation of 1,5-benzodiazepine compounds.
    Type: Grant
    Filed: July 1, 1996
    Date of Patent: June 10, 1997
    Assignee: Glaxo SpA
    Inventors: Harry Finch, David G. Trist, Giorgio Tarzia
  • Patent number: 5585376
    Abstract: The present invention relates to compounds of general formula (I) ##STR1## and physiologically acceptable salts thereof wherein the group NR.sub.1 R.sub.2 represents a 5-7 membered saturated heterocyclic ring which may be substituted by one or two methyl groups; R.sub.3 is C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or phenyl optionally substituted by 1 or 2 halogen atoms; R.sub.4 is phenyl or phenyl substituted by one or two groups selected from the group consisting of halogen, C.sub.1-4 alkyl, trifluoromethyl, trifluoromethoxy or (CH.sub.2).sub.n R.sub.5 wherein n is zero or 1 and R.sub.5 represents C.sub.1-4 alkoxy, hydroxy, nitro, cyano, CO.sub.2 R.sub.6, S(O).sub.p CH.sub.3, NR.sub.7 R.sub.8, CONR.sub.7 R.sub.8, SO.sub.2 NR.sub.7 CO(C.sub.1-4)alkyl, tetrazolyl, carboxamidotetrazolyl, or a 3-trifluoromethyl 1,2,4-triazolyl; R.sub.6 is hydrogen, C.sub.1-4 alkyl or benzyl; R.sub.7 is hydrogen or C.sub.1-4 alkyl, R.sub.8 is hydrogen, C.sub.1-4 alkyl, SO.sub.2 CH.sub.3 or SO.sub.2 CF.sub.3, X represent hydrogen, C.
    Type: Grant
    Filed: October 30, 1995
    Date of Patent: December 17, 1996
    Assignee: Glaxo Wellcome Inc.
    Inventors: Harry Finch, Pritom Shah, Robin A. E. Carr