Additional Chalcogen Double Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 540/518)
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Patent number: 9212187Abstract: 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: GrantFiled: June 25, 2014Date of Patent: December 15, 2015Assignee: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kunio Oshima, Shuuji Matsumura, Hokuto Yamabe
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Patent number: 8940889Abstract: 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: GrantFiled: March 10, 2014Date of Patent: January 27, 2015Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hisayuki Tsujimori, Shinichi Taira, Hirotaka Yukawa, Kaoru Abe
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Publication number: 20140357858Abstract: 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: ApplicationFiled: January 10, 2013Publication date: December 4, 2014Inventors: Masatoshi Ushioda, Kunio Kobayashi, Daisuke Saito, Shogo Sakuma, Toshiyasu Imai, Kazuhide Inoue
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Publication number: 20140343278Abstract: 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: ApplicationFiled: June 25, 2014Publication date: November 20, 2014Inventors: Kunio OSHIMA, Shuuji MATSUMURA, Hokuto YAMABE
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Patent number: 8822453Abstract: 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: GrantFiled: August 20, 2010Date of Patent: September 2, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Takashi Oshiyama, Tsuyoshi Nagase, Masataka Ueda, Kuninori Tai
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Patent number: 8796447Abstract: 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: GrantFiled: August 20, 2010Date of Patent: August 5, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hisayuki Tsujimori, Shinichi Taira, Hirotaka Yukawa, Kaoru Abe
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Publication number: 20140194621Abstract: 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: ApplicationFiled: March 10, 2014Publication date: July 10, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hisayuki TSUJIMORI, Shinichi TAIRA, Hirotaka YUKAWA, Kaoru ABE
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Patent number: 8664217Abstract: 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: GrantFiled: August 22, 2012Date of Patent: March 4, 2014Assignee: 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
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Publication number: 20140031334Abstract: 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: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
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Publication number: 20130150350Abstract: Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: February 9, 2011Publication date: June 13, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Bruno Simoneau, Patrick Deroy, Lee Fader, Anne-Marie Faucher, Alexander Gagnon, Chantal Grand-Maitre, Stephen Kawai, Serge Landry, Jean-Francois Mercier, Jean Rancourt
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Publication number: 20130040941Abstract: 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: ApplicationFiled: August 22, 2012Publication date: February 14, 2013Inventors: Kunio Oshima, Takashi Oshiyama, Shinichi Taira, Yasuhiro Menjo, Hokuto Yamabe, Shuuji Matsumura, Masataka Ueda, Yasuo Koga, Kuninori Tai, Sunao Nakayama, Toshiyuki Onogawa, Kenji Tsujimae
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Patent number: 8338406Abstract: 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: GrantFiled: February 20, 2009Date of Patent: December 25, 2012Assignee: 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
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Publication number: 20120149899Abstract: 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: ApplicationFiled: August 20, 2010Publication date: June 14, 2012Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hisayuki Tsujimori, Shinichi Taira, Hirotaka Yukawa, Kaoru Abe
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Publication number: 20120108575Abstract: 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: ApplicationFiled: January 12, 2012Publication date: May 3, 2012Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.Inventors: Kevin C. Brown, R, Richard Goehring, Yoshiyasu BABA, Naoki Tsuno
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Patent number: 8119631Abstract: 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: GrantFiled: May 24, 2010Date of Patent: February 21, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: 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
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Publication number: 20110178070Abstract: 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: ApplicationFiled: June 23, 2009Publication date: July 21, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xianchang Gong, Bohan Jin, Massaki Hirose, Feng Zhou, Qing Dong
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Publication number: 20110105477Abstract: 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: ApplicationFiled: September 12, 2008Publication date: May 5, 2011Applicant: The Regents of the University of MichiganInventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
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Publication number: 20100331317Abstract: 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: ApplicationFiled: February 20, 2009Publication date: December 30, 2010Inventors: Kunio Oshima, Takashi Oshiyama, Shinichi Taira, Yasuhiro Menjo, Hokuto Yamabe, Shuuji Matsumura, Masataka Ueda, Yasuo Koga, Kuninori Tai, Sunao Nakayama, Toshiyuki Onogawa, Kenji Tsujimae
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Patent number: 7655647Abstract: 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: GrantFiled: February 19, 2009Date of Patent: February 2, 2010Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Publication number: 20100022519Abstract: 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: ApplicationFiled: July 15, 2009Publication date: January 28, 2010Inventors: Kevin C. Brown, R. Richard Goehring, Yoshiyasu Baba, Naoki Tsuno
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Patent number: 7456172Abstract: 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: GrantFiled: January 13, 2006Date of Patent: November 25, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard E. Olson
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Patent number: 7390801Abstract: 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: GrantFiled: May 12, 2006Date of Patent: June 24, 2008Assignees: Athena Neurosciences, Inc., Eli Lilly and CompanyInventors: 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
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Patent number: 7342008Abstract: 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: GrantFiled: September 18, 2006Date of Patent: March 11, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Hong Liu, Lorin Andrew Thompson
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Patent number: 7169773Abstract: The present invention provides a compound of formula I comprising: a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof.Type: GrantFiled: June 30, 2005Date of Patent: January 30, 2007Assignee: SmithKline Beecham CorporationInventors: Jerzy Ryszard Szewczyk, Kelly H. Donaldson
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Patent number: 7053084Abstract: 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: GrantFiled: February 17, 2000Date of Patent: May 30, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Richard E. Olson
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Patent number: 6838455Abstract: 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: GrantFiled: December 23, 2002Date of Patent: January 4, 2005Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
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Patent number: 6774125Abstract: 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: GrantFiled: October 7, 2002Date of Patent: August 10, 2004Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
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Patent number: 6696438Abstract: 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: GrantFiled: December 12, 2002Date of Patent: February 24, 2004Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Bruce A. Dressman, Qing Shi
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Patent number: 6683075Abstract: 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: GrantFiled: January 6, 2003Date of Patent: January 27, 2004Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: 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
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Patent number: 6673921Abstract: 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: GrantFiled: February 19, 2003Date of Patent: January 6, 2004Assignee: SmithKline Beecham CorporationInventors: David Colclough, Anne Hodgson
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Patent number: 6653303Abstract: 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: GrantFiled: January 6, 2003Date of Patent: November 25, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: 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
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Publication number: 20030149027Abstract: A compound represented by the formula (I) 1Type: ApplicationFiled: June 28, 2001Publication date: August 7, 2003Inventors: Satoru Oi, Nobuhiro Suzuki, Takahiro Matsumoto
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Patent number: 6569851Abstract: 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: GrantFiled: June 22, 1999Date of Patent: May 27, 2003Assignees: Elan Pharmaceutials, Inc., Eli Lilly & CompanyInventors: 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
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Patent number: 6303625Abstract: 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: GrantFiled: July 15, 1999Date of Patent: October 16, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: William J. Hoekstra, Edward C. Lawson, Bruce E. Maryanoff
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Patent number: 6255479Abstract: 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: GrantFiled: December 29, 1998Date of Patent: July 3, 2001Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Akireddy Srinivasa Rao
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Patent number: 6171578Abstract: 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: GrantFiled: April 14, 1999Date of Patent: January 9, 2001Assignees: Diatide, Inc., Genentech, Inc.Inventors: Richard T. Dean, John Lister-James, Michael C. Venuti, Todd C. Somers
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Patent number: 6130234Abstract: 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: GrantFiled: December 20, 1996Date of Patent: October 10, 2000Assignees: Warner-Lambert Company, Cocensys, IncorporatedInventors: Christopher F. Bigge, Jonathan Wright, Sui Xiong Cai, Eckard Weber, Richard Woodward, Nancy C. Lan, Zhang-Lin Zhou, John F. W. Keana
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Patent number: 5910495Abstract: 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: GrantFiled: April 14, 1997Date of Patent: June 8, 1999Assignee: Glaxo Wellcome Inc.Inventor: Rochelle Marie Hanley
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Patent number: 5859007Abstract: 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: GrantFiled: November 14, 1996Date of Patent: January 12, 1999Assignee: 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
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Patent number: 5834463Abstract: 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: GrantFiled: June 26, 1995Date of Patent: November 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Nobuhiro Fujii, Koichi Kato, Masaomi Miyamoto
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Patent number: 5776929Abstract: 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: GrantFiled: June 25, 1996Date of Patent: July 7, 1998Assignee: Shionogi & Co., Ltd.Inventors: Sanji Hagishita, Susumu Kamata, Kaoru Seno, Nobuhiro Haga, Yasunobu Ishihara
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Patent number: 5739129Abstract: 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: GrantFiled: October 11, 1996Date of Patent: April 14, 1998Assignee: Glaxo Wellcome Inc.Inventors: Christopher Joseph Aquino, Elizabeth Ellen Sugg, Jerzy Ryszard Szewczyk
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Patent number: 5733867Abstract: 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: GrantFiled: November 4, 1996Date of Patent: March 31, 1998Assignee: Glaxo Wellcome SpAInventors: Giovanni Curotto, Mario Pellegatti, Stefano Polinelli
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Patent number: 5716953Abstract: Compounds of formula (I) ##STR1## wherein the substituents are defined in the specification are antagonists of gastrin and CCK.Type: GrantFiled: March 22, 1996Date of Patent: February 10, 1998Assignee: Glaxo Wellcome S.p.A.Inventors: Daniele Donati, Antonella Ursini, Mauro Corsi
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Patent number: 5700797Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.Type: GrantFiled: June 7, 1995Date of Patent: December 23, 1997Assignee: Merck & Co, Inc.Inventors: David A. Claremon, Nigel Liverton, Harold G. Selnick
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Patent number: 5686449Abstract: The invention relates to compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof having gastrin and/or CCK-B antagonist activity.Type: GrantFiled: October 23, 1995Date of Patent: November 11, 1997Assignee: Glaxo Wellcome S.p.A.Inventors: Maria Elvira Tranquillini, Gabriella Finizia, Antonella Ursini
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Patent number: 5646140Abstract: 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: GrantFiled: October 13, 1995Date of Patent: July 8, 1997Assignee: Glaxo Wellcome Inc.Inventors: Elizabeth Ellen Sugg, Christopher Joseph Aquino, Jerzy Ryszard Szewczyk, Harry Finch, Robin Arthur Ellis Carr
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Patent number: 5641775Abstract: 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: GrantFiled: October 23, 1995Date of Patent: June 24, 1997Assignee: Glaxo SpAInventors: Harry Finch, David Gordon Trist, Aldo Feriani, Giorgio Tarzia, Pritom Shah
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Patent number: 5637697Abstract: This invention relates to compounds of formula (IV) which are useful as intermediates in the preparation of 1,5-benzodiazepine compounds.Type: GrantFiled: July 1, 1996Date of Patent: June 10, 1997Assignee: Glaxo SpAInventors: Harry Finch, David G. Trist, Giorgio Tarzia
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Patent number: 5585376Abstract: 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: GrantFiled: October 30, 1995Date of Patent: December 17, 1996Assignee: Glaxo Wellcome Inc.Inventors: Harry Finch, Pritom Shah, Robin A. E. Carr