Acyclic Nitrogen Bonded Directly To The Hetero Ring Patents (Class 540/509)
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Patent number: 10881667Abstract: 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: GrantFiled: October 30, 2018Date of Patent: January 5, 2021Assignee: City University of Hong KongInventors: Jufang He, Xiao Li, Ailian Tan, Yujie Peng, Shenghui Xu, Yujie Yang, Xu Zhang, MD. Monir Hossain
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Publication number: 20140357605Abstract: 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: ApplicationFiled: July 28, 2014Publication date: December 4, 2014Inventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim
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Patent number: 8853204Abstract: 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: GrantFiled: March 18, 2005Date of Patent: October 7, 2014Assignee: Arrow Therapeutics LimitedInventors: Kenneth Powell, Richard Kelsey, Malcolm Carter, Dagmar Alber, Lara Wilson, Elisa Henderson, Phil Chambers, Debra Taylor, Stan Tyms, Verity Dowdell
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Patent number: 8822454Abstract: 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: GrantFiled: December 9, 2013Date of Patent: September 2, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim
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Publication number: 20140100365Abstract: 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: ApplicationFiled: December 9, 2013Publication date: April 10, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim, Francis Y. Lee
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Publication number: 20140087992Abstract: 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: ApplicationFiled: September 20, 2013Publication date: March 27, 2014Inventors: Ashvinikumar V. Gavai, George V. DeLucca, Daniel O'Malley, Patrice Gill, Claude A. Quesnelle, Brian E. Fink, Yufen Zhao, Francis Y. Lee
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Patent number: 8629136Abstract: 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: GrantFiled: March 22, 2012Date of Patent: January 14, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim, Francis Y. Lee
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Patent number: 8324202Abstract: Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C?O or CH2 used as antineoplastic agent.Type: GrantFiled: December 18, 2008Date of Patent: December 4, 2012Assignees: Universita Degli Studi di Firenze, A.I.L. Firenze Sezione Autonoma di Firenze Dell'Associazione Italiana Contro le Leucemie, Linfomi E Mieloma—OnlusInventors: Francesco Paoletti, Maria Novella Romanelli, Cristina Cellai, Anna Laurenzana, Luca Guandalini
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Publication number: 20120245151Abstract: 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: ApplicationFiled: March 22, 2012Publication date: September 27, 2012Inventors: ASHVINIKUMAR V. GAVAI, CLAUDE A. QUESNELLE, SOONG-HOON KIM, FRANCIS Y. LEE
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Publication number: 20120015938Abstract: 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: ApplicationFiled: February 12, 2010Publication date: January 19, 2012Applicant: MSD K.K.Inventors: Masanori Asai, Tasuku Haketa, Seiichi Inamura, Hideki Kurihara, Teruyuki Nishimura, Tadashi Shimamura
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Publication number: 20110319396Abstract: 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: ApplicationFiled: January 19, 2010Publication date: December 29, 2011Applicant: 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
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Publication number: 20110294793Abstract: 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: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Patent number: 7994161Abstract: 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: GrantFiled: November 10, 2008Date of Patent: August 9, 2011Assignee: Sanofi-AventisInventors: Jidong Zhang, Yannick Benedetti, Alain Commerçon
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Publication number: 20110178069Abstract: 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: ApplicationFiled: May 24, 2010Publication date: July 21, 2011Applicant: 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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Patent number: 7977330Abstract: 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: GrantFiled: May 21, 2007Date of Patent: July 12, 2011Assignee: Novartis AGInventors: Lilli Feng, Xinglong Jiang, Piotr H. Karpinski
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Publication number: 20110059043Abstract: 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: ApplicationFiled: September 2, 2010Publication date: March 10, 2011Applicant: ARROW THERAPEUTICS LIMITEDInventors: Michael Christopher Stratton BARNES, Helena Jade DENNISON, Stephen Sean FLACK, James Andrew LUMLEY, Pui Shan PANG, Keith Charles SPENCER
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Publication number: 20100331316Abstract: Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C?O or CH2 used as antineoplastic agent.Type: ApplicationFiled: December 18, 2008Publication date: December 30, 2010Inventors: Francesco Paoletti, Maria Novella Romanelli, Cristina Cellai, Anna Laurenzana, Luca Guandalini
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Patent number: 7718795Abstract: 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: April 2, 2008Date of Patent: May 18, 2010Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard E. Olson
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Publication number: 20100069373Abstract: 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: ApplicationFiled: November 10, 2009Publication date: March 18, 2010Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Publication number: 20100056501Abstract: 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: ApplicationFiled: September 22, 2009Publication date: March 4, 2010Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Publication number: 20100048541Abstract: 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: ApplicationFiled: September 17, 2009Publication date: February 25, 2010Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventors: Qi HAN, Hong Liu, Richard E. Olson, Michael G. Yang
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Publication number: 20100041639Abstract: 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: ApplicationFiled: October 21, 2009Publication date: February 18, 2010Applicant: BRISTOL-MYERS SQIBB PHARMA COMAPNYInventors: Richard E. Olson, Michael G. Yang
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Publication number: 20100015063Abstract: 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 alkType: ApplicationFiled: June 2, 2009Publication date: January 21, 2010Applicant: Arrow Therapeutics LimitedInventors: Malcolm Carter, Elisa Henderson, Richard Kelsey, Lara Wilson, Phil Chambers, Debra Taylor, Stan Tyms
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Publication number: 20100009966Abstract: 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: ApplicationFiled: September 15, 2009Publication date: January 14, 2010Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventors: Qi HAN, Hong Liu, Richard E. Olson, Michael G. Yang
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Publication number: 20100009965Abstract: 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: ApplicationFiled: September 2, 2009Publication date: January 14, 2010Applicant: BRISTOL-MYERS SQIBB PHARMA COMPANYInventors: Richard E. Olson, Michael G. Yang
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Publication number: 20090318427Abstract: 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: ApplicationFiled: September 19, 2005Publication date: December 24, 2009Inventors: Helena Dennison, Justin Warne, Keith Spencer, George Cockerill, James Lumley
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Patent number: 7632832Abstract: 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: GrantFiled: January 13, 2006Date of Patent: December 15, 2009Assignee: Merck & Co., Inc.Inventors: Christopher S. Burgey, Theresa M. Williams, Zhengwu J. Deng, Craig A. Stump
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Patent number: 7582624Abstract: Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV.Type: GrantFiled: September 22, 2003Date of Patent: September 1, 2009Assignee: Arrow Therapeutics LimitedInventors: Malcolm Carter, Philip Chambers, Verity Dowdell, Elisa Ann Henderson, Richard David Kelsey, Debra Taylor, Stanley Tyms, Lara Wilson
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Publication number: 20090163478Abstract: 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: ApplicationFiled: May 21, 2007Publication date: June 25, 2009Inventors: Lili Feng, Xinglong Jiang, Piotr H. Karpinski
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Patent number: 7507815Abstract: 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: GrantFiled: December 4, 2007Date of Patent: March 24, 2009Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
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Publication number: 20090075971Abstract: 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: ApplicationFiled: November 10, 2008Publication date: March 19, 2009Applicant: SANOFI-AVENTISInventors: Jidong Zhang, Yannick Benedetti, Alain Commercon
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Publication number: 20090062256Abstract: 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: ApplicationFiled: October 24, 2008Publication date: March 5, 2009Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventor: Richard E. Olson
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Patent number: 7498324Abstract: 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: April 19, 2007Date of Patent: March 3, 2009Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Patent number: 7476665Abstract: 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: GrantFiled: June 24, 2004Date of Patent: January 13, 2009Assignee: Merck & Co., Inc.Inventors: Christopher S. Burgey, Craig A. Stump, Theresa M. Williams
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Patent number: 7456278Abstract: 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: October 31, 2007Date of Patent: November 25, 2008Assignee: Bristol-Myers Squibb Pharma CorporationInventor: Richard E. Olson
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Publication number: 20080275024Abstract: 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: ApplicationFiled: June 19, 2008Publication date: November 6, 2008Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventors: Richard E. Olson, Michael G. Yang
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Patent number: 7423033Abstract: 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 1, 2008Date of Patent: September 9, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Hong Liu, Lorin Andrew Thompson
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Publication number: 20080207602Abstract: 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: ApplicationFiled: April 2, 2008Publication date: August 28, 2008Applicant: Bristol-Myers Squibb Pharma CompanyInventor: Richard E. Olson
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Publication number: 20080171735Abstract: 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: ApplicationFiled: March 10, 2008Publication date: July 17, 2008Applicant: 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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Publication number: 20080139536Abstract: 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} groupType: ApplicationFiled: March 18, 2005Publication date: June 12, 2008Applicant: Novartis Pharmaceuticals CorporationInventors: Verity Dowdell, Richard Kelsey, Malcolm Carter, Dagmar Alber, Elisa Henderson
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Publication number: 20080132482Abstract: 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: ApplicationFiled: February 1, 2008Publication date: June 5, 2008Applicant: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
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Publication number: 20080125413Abstract: 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: ApplicationFiled: January 13, 2006Publication date: May 29, 2008Inventors: Christopher S. Burgey, Theresa M. Williams, Zhengwu J. Deng, Craig A. Stump
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Patent number: 7375101Abstract: 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: GrantFiled: December 11, 2002Date of Patent: May 20, 2008Assignee: AstraZeneca ABInventors: Carmen Leung, Vijayaratnam Santhakumar, Miroslaw Tomaszewski, Simon Woo
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Patent number: 7365196Abstract: 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: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: 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
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Patent number: 7358239Abstract: 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 isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7304055Abstract: 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: GrantFiled: July 25, 2006Date of Patent: December 4, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
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Patent number: 7276496Abstract: 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: GrantFiled: January 6, 2006Date of Patent: October 2, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Michael G. Yang
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Patent number: 7250410Abstract: 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: GrantFiled: June 7, 2002Date of Patent: July 31, 2007Assignee: Via Pharmaceuticals, Inc.Inventors: Jean-Jacques Bourguignon, Yan Lagouge, Claire Lugnier, Eveline Klotz, Jean-Paul Macher, Pierre Raboisson, Dominique Schultz
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Patent number: 7205293Abstract: 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: GrantFiled: March 10, 2004Date of Patent: April 17, 2007Assignee: Merck & Co., Inc.Inventors: Ian M. Bell, Samuel L. Graham, Theresa M. Williams, Craig A. Stump