Acyclic Nitrogen Bonded Directly To The Hetero Ring Patents (Class 540/509)
  • Patent number: 10881667
    Abstract: A method of treating a subject suffering from epilepsy includes administering an effective amount of a cholecystokinin-2 receptor antagonist or a pharmaceutical acceptable salt thereof to the subject. A pharmaceutical composition includes the cholecystokinin-2 receptor antagonist or a pharmaceutical acceptable salt thereof as active ingredient, one or more antiepileptic compounds, and a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: January 5, 2021
    Assignee: City University of Hong Kong
    Inventors: Jufang He, Xiao Li, Ailian Tan, Yujie Peng, Shenghui Xu, Yujie Yang, Xu Zhang, MD. Monir Hossain
  • Publication number: 20140357605
    Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: December 4, 2014
    Inventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim
  • Patent number: 8853204
    Abstract: A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: October 7, 2014
    Assignee: Arrow Therapeutics Limited
    Inventors: Kenneth Powell, Richard Kelsey, Malcolm Carter, Dagmar Alber, Lara Wilson, Elisa Henderson, Phil Chambers, Debra Taylor, Stan Tyms, Verity Dowdell
  • Patent number: 8822454
    Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Grant
    Filed: December 9, 2013
    Date of Patent: September 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim
  • Publication number: 20140100365
    Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Application
    Filed: December 9, 2013
    Publication date: April 10, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim, Francis Y. Lee
  • Publication number: 20140087992
    Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
    Type: Application
    Filed: September 20, 2013
    Publication date: March 27, 2014
    Inventors: Ashvinikumar V. Gavai, George V. DeLucca, Daniel O'Malley, Patrice Gill, Claude A. Quesnelle, Brian E. Fink, Yufen Zhao, Francis Y. Lee
  • Patent number: 8629136
    Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: January 14, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim, Francis Y. Lee
  • Patent number: 8324202
    Abstract: Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C?O or CH2 used as antineoplastic agent.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: December 4, 2012
    Assignees: Universita Degli Studi di Firenze, A.I.L. Firenze Sezione Autonoma di Firenze Dell'Associazione Italiana Contro le Leucemie, Linfomi E Mieloma—Onlus
    Inventors: Francesco Paoletti, Maria Novella Romanelli, Cristina Cellai, Anna Laurenzana, Luca Guandalini
  • Publication number: 20120245151
    Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Application
    Filed: March 22, 2012
    Publication date: September 27, 2012
    Inventors: ASHVINIKUMAR V. GAVAI, CLAUDE A. QUESNELLE, SOONG-HOON KIM, FRANCIS Y. LEE
  • Publication number: 20120015938
    Abstract: The present invention relates to a compound represented by a formula (I): wherein R1 represents a halogen atom or the like; R2 represents a hydrogen atom or the like; R3 and R4 each independently represents lower alkyl; R5 represents phenyl or the like; R6 represents a halogen atom or the like; m is an integer of from 0 to 2; p is an integer of from 1 to 4; and q is an integer of from 1 to 5 as an inhibitor of DGAT1 and its use for the treatment of hyperlipidemia etc.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 19, 2012
    Applicant: MSD K.K.
    Inventors: Masanori Asai, Tasuku Haketa, Seiichi Inamura, Hideki Kurihara, Teruyuki Nishimura, Tadashi Shimamura
  • Publication number: 20110319396
    Abstract: The present invention relates to a compound represented by the formula (I): wherein R1 represents a hydrogen atom or the like; R2 represents lower alkyl or the like; R3 and R4 represent lower alkyl or the like; R5 represents phenyl or the like; R6 represents a hydrogen atom or the like; m is an integer of from 0 to 2; p is an integer of from 1 to 4; and q is an integer of from 1 to 5, or a pharmaceutical acceptable salt thereof, and a DGAT 1 inhibitor comprising the compound.
    Type: Application
    Filed: January 19, 2010
    Publication date: December 29, 2011
    Applicant: MSD K.K.
    Inventors: Masanori Asai, Tasuku Haketa, Seiichi Inamura, Makoto Ishikawa, Hideki Jona, Hiroshi Kawamoto, Hideki Kurihara, Jun Shibata, Tadashi Shimamura, Takuya Suga, Hitomi Watanabe
  • Publication number: 20110294793
    Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.
    Type: Application
    Filed: June 8, 2009
    Publication date: December 1, 2011
    Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
  • Patent number: 7994161
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: August 9, 2011
    Assignee: Sanofi-Aventis
    Inventors: Jidong Zhang, Yannick Benedetti, Alain Commerçon
  • Publication number: 20110178069
    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: Application
    Filed: May 24, 2010
    Publication date: July 21, 2011
    Applicant: 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
  • Patent number: 7977330
    Abstract: The invention relates to salts of 1-(2-Fluoro-phenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-urea and crystalline forms thereof, their production and usage, and pharmaceutical preparations containing such salts and crystalline forms.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: July 12, 2011
    Assignee: Novartis AG
    Inventors: Lilli Feng, Xinglong Jiang, Piotr H. Karpinski
  • Publication number: 20110059043
    Abstract: The invention concerns benzodiazepine derivatives of Formula I: wherein W, X, L1, L2, L3, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
    Type: Application
    Filed: September 2, 2010
    Publication date: March 10, 2011
    Applicant: ARROW THERAPEUTICS LIMITED
    Inventors: Michael Christopher Stratton BARNES, Helena Jade DENNISON, Stephen Sean FLACK, James Andrew LUMLEY, Pui Shan PANG, Keith Charles SPENCER
  • Publication number: 20100331316
    Abstract: Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C?O or CH2 used as antineoplastic agent.
    Type: Application
    Filed: December 18, 2008
    Publication date: December 30, 2010
    Inventors: Francesco Paoletti, Maria Novella Romanelli, Cristina Cellai, Anna Laurenzana, Luca Guandalini
  • Patent number: 7718795
    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: April 2, 2008
    Date of Patent: May 18, 2010
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Publication number: 20100069373
    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: Application
    Filed: November 10, 2009
    Publication date: March 18, 2010
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20100056501
    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: Application
    Filed: September 22, 2009
    Publication date: March 4, 2010
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20100048541
    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: Application
    Filed: September 17, 2009
    Publication date: February 25, 2010
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Qi HAN, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20100041639
    Abstract: This invention relates to novel cyclic malonamides 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: Application
    Filed: October 21, 2009
    Publication date: February 18, 2010
    Applicant: BRISTOL-MYERS SQIBB PHARMA COMAPNY
    Inventors: Richard E. Olson, Michael G. Yang
  • Publication number: 20100015063
    Abstract: Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; -each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R?, CONR?R?, —NH—CO—R?, —S(O)R?, —S(O)2R?, —NH—S(O)2R?, —S(O)NR?R? or —S(O)2NR?R? wherein each R? and R? is the same or different and represents hydrogen or C1-6 alkyl; -n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(0)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alk
    Type: Application
    Filed: June 2, 2009
    Publication date: January 21, 2010
    Applicant: Arrow Therapeutics Limited
    Inventors: Malcolm Carter, Elisa Henderson, Richard Kelsey, Lara Wilson, Phil Chambers, Debra Taylor, Stan Tyms
  • Publication number: 20100009965
    Abstract: This invention relates to novel cyclic malonamides 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: Application
    Filed: September 2, 2009
    Publication date: January 14, 2010
    Applicant: BRISTOL-MYERS SQIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Michael G. Yang
  • Publication number: 20100009966
    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: Application
    Filed: September 15, 2009
    Publication date: January 14, 2010
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Qi HAN, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20090318427
    Abstract: Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R?, —CONR?R?, —NH—C0-R?, —S(O)R?, —S(O)2R?, —NH—S(O)2R?, —S(O)NR?R? or —S(O)2NR?R?, wherein each R? and R? is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; —R4 represents hydrogen or C1-6 alkyl; —R5 represents C1-6alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, aryl-C(O)—
    Type: Application
    Filed: September 19, 2005
    Publication date: December 24, 2009
    Inventors: Helena Dennison, Justin Warne, Keith Spencer, George Cockerill, James Lumley
  • Patent number: 7632832
    Abstract: Compounds of Formula I: (where variables R1, R2, R3, R7, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache, and 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: January 13, 2006
    Date of Patent: December 15, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Christopher S. Burgey, Theresa M. Williams, Zhengwu J. Deng, Craig A. Stump
  • Patent number: 7582624
    Abstract: Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV.
    Type: Grant
    Filed: September 22, 2003
    Date of Patent: September 1, 2009
    Assignee: Arrow Therapeutics Limited
    Inventors: Malcolm Carter, Philip Chambers, Verity Dowdell, Elisa Ann Henderson, Richard David Kelsey, Debra Taylor, Stanley Tyms, Lara Wilson
  • Publication number: 20090163478
    Abstract: The invention relates to salts of 1-(2-Fluoro-phenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-urea and crystalline forms thereof, their production and usage, and pharmaceutical preparations containing such salts and crystalline forms.
    Type: Application
    Filed: May 21, 2007
    Publication date: June 25, 2009
    Inventors: Lili Feng, Xinglong Jiang, Piotr H. Karpinski
  • Patent number: 7507815
    Abstract: This invention relates to novel lactams 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: December 4, 2007
    Date of Patent: March 24, 2009
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
  • Publication number: 20090075971
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
    Type: Application
    Filed: November 10, 2008
    Publication date: March 19, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Jidong Zhang, Yannick Benedetti, Alain Commercon
  • Publication number: 20090062256
    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: Application
    Filed: October 24, 2008
    Publication date: March 5, 2009
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventor: Richard E. Olson
  • Patent number: 7498324
    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: April 19, 2007
    Date of Patent: March 3, 2009
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
  • Patent number: 7476665
    Abstract: The present invention is directed to compounds of Formula I: I (where variables R1?, R2?, R3?, R6?, R7?, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: June 24, 2004
    Date of Patent: January 13, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Christopher S. Burgey, Craig A. Stump, Theresa M. Williams
  • Patent number: 7456278
    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: October 31, 2007
    Date of Patent: November 25, 2008
    Assignee: Bristol-Myers Squibb Pharma Corporation
    Inventor: Richard E. Olson
  • Publication number: 20080275024
    Abstract: This invention relates to novel cyclic malonamides 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: Application
    Filed: June 19, 2008
    Publication date: November 6, 2008
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Michael G. Yang
  • Patent number: 7423033
    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 1, 2008
    Date of Patent: September 9, 2008
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Hong Liu, Lorin Andrew Thompson
  • Publication number: 20080207602
    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: Application
    Filed: April 2, 2008
    Publication date: August 28, 2008
    Applicant: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Publication number: 20080171735
    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: Application
    Filed: March 10, 2008
    Publication date: July 17, 2008
    Applicant: 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
  • Publication number: 20080139536
    Abstract: Use of a compound which is (a) a benzodiazepine derivative of the formula (I) or an N-oxide thereof or (b) a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing an RSV infection wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6alkyl)amino, vitro, cyano, —CO2R?, —CONR?R?, —NH—CO—R?, —S(O)R?, —S(O)2R?, —NH—S(O)2R?, —S(O)NR?R? or —S(O)2NR?R?, wherein each R? and R? is the same or different and represents hydrogen or C1-6 alkyl; n is from O to 3; R4 represents hydrogen or C1-6 alkyl; X represents —CO—, —CO—NR?—, —S(O)— or —S(O)2—, wherein R? is hydrogen or a C1-C6 alkyl group; and R5 represents a heteroaryl or heterocyclyl group which is substituted by a C1C6 hydroxyalkyl group or a —(C1-C4 alkyl)-X1—(C1-C4 alkyl)-X2—(C1-C4 alkyl} group
    Type: Application
    Filed: March 18, 2005
    Publication date: June 12, 2008
    Applicant: Novartis Pharmaceuticals Corporation
    Inventors: Verity Dowdell, Richard Kelsey, Malcolm Carter, Dagmar Alber, Elisa Henderson
  • Publication number: 20080132482
    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: Application
    Filed: February 1, 2008
    Publication date: June 5, 2008
    Applicant: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
  • Publication number: 20080125413
    Abstract: Compounds of Formula I: (where variables R1, R2, R3, R7, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache, and 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 13, 2006
    Publication date: May 29, 2008
    Inventors: Christopher S. Burgey, Theresa M. Williams, Zhengwu J. Deng, Craig A. Stump
  • Patent number: 7375101
    Abstract: Compounds of Formula (I) wherein R1, R3, R4, R5 and X are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared.
    Type: Grant
    Filed: December 11, 2002
    Date of Patent: May 20, 2008
    Assignee: AstraZeneca AB
    Inventors: Carmen Leung, Vijayaratnam Santhakumar, Miroslaw Tomaszewski, Simon Woo
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7304055
    Abstract: This invention relates to novel lactams 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: July 25, 2006
    Date of Patent: December 4, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
  • Patent number: 7276496
    Abstract: This invention relates to novel cyclic malonamides 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 6, 2006
    Date of Patent: October 2, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Michael G. Yang
  • Patent number: 7250410
    Abstract: The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: July 31, 2007
    Assignee: Via Pharmaceuticals, Inc.
    Inventors: Jean-Jacques Bourguignon, Yan Lagouge, Claire Lugnier, Eveline Klotz, Jean-Paul Macher, Pierre Raboisson, Dominique Schultz
  • Patent number: 7205293
    Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: March 10, 2004
    Date of Patent: April 17, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Ian M. Bell, Samuel L. Graham, Theresa M. Williams, Craig A. Stump