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1.
公开(公告)号:US20070185324A1
公开(公告)日:2007-08-09
申请号:US11643261
申请日:2006-12-20
申请人: Frenel De Morin , Jian Chen , Elizabeth Doherty , Stephen Hitchcock , Qi Huang , Joseph Kim , Gang Liu , Thomas Nixey , Nick Paras , Jeffrey Petkus , Daniel Retz , Adrian Smith , Andrew Tasker , Jiawang Zhu
发明人: Frenel De Morin , Jian Chen , Elizabeth Doherty , Stephen Hitchcock , Qi Huang , Joseph Kim , Gang Liu , Thomas Nixey , Nick Paras , Jeffrey Petkus , Daniel Retz , Adrian Smith , Andrew Tasker , Jiawang Zhu
IPC分类号: A61K31/541 , A61K31/5377 , C07D417/02 , C07D403/02
CPC分类号: C07D401/14 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z′, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译: 本发明包括能够调节Raf激酶的新一类化合物,因此可用于治疗Raf激酶介导的疾病,包括黑素瘤,肿瘤和其它癌症相关病症。 这些化合物具有通式I,其中R 1是和A 1,A 2,A 3,A 3, X,Z,Z',R 1,R 2,R 3,R 3, 本文定义了R 5,R 5和R 6。 本发明还包括药物组合物,用于治疗Raf激酶介导的疾病的方法,以及可用于制备本发明化合物的中间体和方法。
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2.
公开(公告)号:US20110251199A1
公开(公告)日:2011-10-13
申请号:US13163666
申请日:2011-06-17
申请人: Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel M. Retz , Adrian L. Smith , Jiawang Zhu
发明人: Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel M. Retz , Adrian L. Smith , Jiawang Zhu
IPC分类号: A61K31/502 , A61K31/517 , A61P35/00 , A61K31/506 , C07D403/10 , C07D413/14 , C07D417/10 , C07D401/14
CPC分类号: C07D401/14 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I and A1, A2, A3, A4, X, Z, Z′, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译: 本发明包括能够调节Raf激酶的新一类化合物,因此可用于治疗Raf激酶介导的疾病,包括黑素瘤,肿瘤和其它癌症相关病症。 该化合物具有通式Ⅰ和A1,A2,A3,A4,X,Z,Z',R1,R2,R3,R4,R5和R6的定义。 本发明还包括药物组合物,用于治疗Raf激酶介导的疾病的方法,以及可用于制备本发明化合物的中间体和方法。
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3.Substituted pyrimidine compounds as RAF inhibitors and methods of use 失效
标题翻译: 取代的嘧啶化合物作为RAF抑制剂和使用方法公开(公告)号:US08440674B2
公开(公告)日:2013-05-14
申请号:US13163666
申请日:2011-06-17
申请人: Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen A. Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel Martin Retz , Adrian Leonard Smith , Jiawang Zhu
发明人: Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen A. Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel Martin Retz , Adrian Leonard Smith , Jiawang Zhu
IPC分类号: A01N43/54
CPC分类号: C07D401/14 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z′, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译: 本发明包括能够调节Raf激酶的新一类化合物,因此可用于治疗Raf激酶介导的疾病,包括黑素瘤,肿瘤和其它癌症相关病症。 该化合物具有通式I,其中R1为和A1,A2,A3,A4,X,Z,Z',R1,R2,R3,R4,R5和R6如本文所定义。 本发明还包括药物组合物,用于治疗Raf激酶介导的疾病的方法,以及可用于制备本发明化合物的中间体和方法。
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公开(公告)号:US20050277631A1
公开(公告)日:2005-12-15
申请号:US11195134
申请日:2005-08-01
申请人: Elizabeth Doherty , Jiawang Zhu , Markian Stec , Mark Norman , Hui-Ling Wang , Christopher Fotsch , Ning Chen , Partha Chakrabarti , Celia Dominguez , James Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil Ognyanov , Liping Pettus , Robert Rzasa
发明人: Elizabeth Doherty , Jiawang Zhu , Markian Stec , Mark Norman , Hui-Ling Wang , Christopher Fotsch , Ning Chen , Partha Chakrabarti , Celia Dominguez , James Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil Ognyanov , Liping Pettus , Robert Rzasa
IPC分类号: A61P29/00 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/64 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/22 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/40 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12 , A61K31/549 , A61K31/501 , C07D417/02 , C07D43/02
CPC分类号: C07D231/40 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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公开(公告)号:US20050272777A1
公开(公告)日:2005-12-08
申请号:US11195159
申请日:2005-08-01
申请人: Elizabeth Doherty , Jiawang Zhu , Markian Stec , Mark Norman , Hui-Ling Wang , Christopher Fotsch , Ning Chen , Partha Chakrabarti , Celia Dominguez , James Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil Ognyanov , Liping Pettus , Robert Rzasa
发明人: Elizabeth Doherty , Jiawang Zhu , Markian Stec , Mark Norman , Hui-Ling Wang , Christopher Fotsch , Ning Chen , Partha Chakrabarti , Celia Dominguez , James Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil Ognyanov , Liping Pettus , Robert Rzasa
IPC分类号: A61P29/00 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/64 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/22 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/40 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12 , A61K31/4439 , C07D417/02
CPC分类号: C07D231/40 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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公开(公告)号:US07332511B2
公开(公告)日:2008-02-19
申请号:US11195159
申请日:2005-08-01
申请人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
发明人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
IPC分类号: C07D213/30 , C07D213/32 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/4427 , A61P19/02 , A61P35/00
CPC分类号: C07D231/40 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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公开(公告)号:US20110166132A1
公开(公告)日:2011-07-07
申请号:US12746902
申请日:2008-12-12
申请人: Stephen A. Hitchcock , Jian J. Chen , Mqhele Vellah Ncube , Thomas Nixey , Albert Amegadzie , Roxanne Kunz , Wenyan Qian , Ning Chen , Christopher M. Tegley , Frenel F. De Morin , Chester Chenguang Yuan , Qingyian Liu , Jiawang Zhu , Tanya A.N. Peterkin , Jeffrey A. Adams , Essa Hu , Frank Chavez, JR.
发明人: Stephen A. Hitchcock , Jian J. Chen , Mqhele Vellah Ncube , Thomas Nixey , Albert Amegadzie , Roxanne Kunz , Wenyan Qian , Ning Chen , Christopher M. Tegley , Frenel F. De Morin , Chester Chenguang Yuan , Qingyian Liu , Jiawang Zhu , Tanya A.N. Peterkin , Jeffrey A. Adams , Essa Hu , Frank Chavez, JR.
IPC分类号: A61K31/538 , C07D213/56 , C07D413/12 , C07D401/12 , C07D401/14 , C07D413/14 , C07D405/12 , C07D233/61 , C07D403/12 , A61K31/4418 , A61K31/4439 , A61K31/496 , A61K31/444 , A61K31/4725 , A61K31/4545 , A61K31/5377 , A61K31/4433 , A61K31/4709 , A61K31/4164 , A61K31/4178 , A61P25/28
CPC分类号: C07D213/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12
摘要: The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
摘要翻译: 本发明提供了γ-分泌酶调节剂的化合物,因此可用于治疗通过调节γ分泌酶如阿尔茨海默病可治疗的疾病。 还提供含有这些化合物的药物组合物和制备这些化合物的方法。
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公开(公告)号:US07148221B2
公开(公告)日:2006-12-12
申请号:US11195134
申请日:2005-08-01
申请人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
发明人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
IPC分类号: C07D237/14 , C07D237/18 , C07D223/16 , C07D223/18 , A61K31/501 , A61P25/06
CPC分类号: C07D231/40 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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公开(公告)号:US07144888B2
公开(公告)日:2006-12-05
申请号:US10638009
申请日:2003-08-08
申请人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
发明人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
IPC分类号: C07D239/34 , C07D239/38 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/505 , A61K31/506 , A61K31/4427 , A61P19/02 , A61P25/06
CPC分类号: C07D231/40 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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公开(公告)号:US20110118250A1
公开(公告)日:2011-05-19
申请号:US12909566
申请日:2010-10-21
申请人: Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Wenge Zhong
发明人: Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Wenge Zhong
IPC分类号: A61K31/538 , C07D405/12 , A61K31/4433 , A61K31/444 , C07D405/14 , A61K31/4439 , A61K31/506 , A61K31/497 , C07D413/12 , A61K31/5377 , A61K31/4178 , A61K31/4545 , A61K31/453 , C07D311/96 , A61K31/352 , C07D407/12 , A61K31/4709 , C07D401/12 , C07D409/12 , A61K31/422 , A61K31/4025 , C07D471/04 , A61K31/501 , A61P25/28 , A61P25/00 , A61P25/16
CPC分类号: C07D405/12 , C07D413/12
摘要: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病(包括阿尔茨海默氏病(AD))和相关病症的新一类化合物。 在一个实施方案中,化合物具有通式I,其中A,B,R 3,R 4,R 5,i和j在本文中定义。 本发明还包括药物组合物,其包括一种或多种式I化合物,这些化合物的使用方法,包括治疗AD和相关疾病,通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案,可用于制备本发明化合物的中间体和方法。
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