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51.发明授权2′-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases 有权2'-叠氮基取代的核苷衍生物及其用于治疗病毒性疾病的方法公开(公告)号：US09156872B2
公开(公告)日：2015-10-13
申请号：US14111685
申请日：2012-04-11
申请人： Vinay Girijavallabhan , F. George Njoroge , Stephane Bogen , Frank Bennett , Vishal Verma , Ashok Arasappan , Kevin Chen , Ying Huang , Angela Kerekes , Latha Nair , Dmitri Pissarnitski , Qun Dang , Ian Davies , David B. Olsen , Andrew Stamford , Joseph P. Vacca
发明人： Vinay Girijavallabhan , F. George Njoroge , Stephane Bogen , Frank Bennett , Vishal Verma , Ashok Arasappan , Kevin Chen , Ying Huang , Angela Kerekes , Latha Nair , Dmitri Pissarnitski , Qun Dang , Ian Davies , David B. Olsen , Andrew Stamford , Joseph P. Vacca
IPC分类号： C07H19/06 , C07H19/10 , C07H19/12 , C07H19/16 , C07H19/04 , C07H19/20 , C07H19/207 , C07H19/11 , C07H19/213 , A61K31/7056 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/708 , A61K45/06
CPC分类号： C07H19/06 , A61K31/7056 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/708 , A61K45/06 , A61P31/14 , C07H19/10 , C07H19/11 , C07H19/12 , C07H19/16 , C07H19/20 , C07H19/207 , C07H19/213
摘要： The present invention relates to 2′-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Azido Substituted Nucleoside Derivative, and methods of using the 2′-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
摘要翻译： 本发明涉及式（I）的2'-叠氮基取代的核苷衍生物及其药学上可接受的盐，其中B，X，R 1，R 2和R 3如本文所定义。 本发明还涉及包含至少一种2'-叠氮基取代的核苷衍生物的组合物，以及使用2'-叠氮基取代的核苷衍生物治疗或预防患者HCV感染的方法。
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公开(公告)号：US20130178468A1
公开(公告)日：2013-07-11
申请号：US13606929
申请日：2012-09-07
申请人： Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C. A. Isaccs , Wei Han , Melissa Egbertson , Richard Pracitto
发明人： Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C. A. Isaccs , Wei Han , Melissa Egbertson , Richard Pracitto
IPC分类号： C07D471/14 , C07D498/14
CPC分类号： C07D471/14 , A61K31/4353 , A61K31/4375 , C07D498/14
摘要： Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 式I的三环化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中键A，环A，R 1，R 2和R 3在本文中定义。 该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防，治疗或延迟。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US08461185B2
公开(公告)日：2013-06-11
申请号：US12740098
申请日：2008-10-29
申请人： Christopher S. Burgey , Diem N. Nguyen , Daniel V. Paone , Craig M. Potteiger , Joseph P. Vacca
发明人： Christopher S. Burgey , Diem N. Nguyen , Daniel V. Paone , Craig M. Potteiger , Joseph P. Vacca
IPC分类号： A61K31/4439 , C07D413/14
CPC分类号： C07D413/14 , C07D261/04 , C07D261/08 , C07D261/20 , C07D263/32 , C07D413/04 , C07D413/12 , C07D417/14 , C07D487/04
摘要： The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
摘要翻译： 本发明涉及在治疗与疼痛有关的疾病状态，特别是外周疼痛，炎症性疼痛或可用P2X3受体亚基调节剂治疗的组织损伤疼痛中发挥关键作用的新型P2X3受体拮抗剂。
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公开(公告)号：US08377873B2
公开(公告)日：2013-02-19
申请号：US12446296
申请日：2007-10-19
申请人： Nigel J. Liverton , Vincenzo Summa , Joseph P. Vacca , Maria Emilia Di Francesco , Marco Pompei
发明人： Nigel J. Liverton , Vincenzo Summa , Joseph P. Vacca , Maria Emilia Di Francesco , Marco Pompei
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/0808
摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use treating or preventing HCV infections.
摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。
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公开(公告)号：US08247401B2
公开(公告)日：2012-08-21
申请号：US12740105
申请日：2008-10-29
申请人： Christopher S. Burgey , Diem Nguyen , Zhengwu Deng , Daniel V. Paone , Craig M. Potteiger , Joseph P. Vacca
发明人： Christopher S. Burgey , Diem Nguyen , Zhengwu Deng , Daniel V. Paone , Craig M. Potteiger , Joseph P. Vacca
IPC分类号： A61K31/397 , A61K31/5377 , A61K31/538 , A61K31/506 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/42 , A61K31/4245 , A61K31/4155 , A61K31/4192 , A61K31/4196 , C07D265/28 , C07D413/00 , C07D401/00 , C07D471/00 , C07D491/00
CPC分类号： C07C233/66 , C07C233/65 , C07C233/83 , C07C233/87 , C07D213/56 , C07D213/61 , C07D213/89 , C07D239/26 , C07D249/08 , C07D271/06 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
摘要翻译： 本发明涉及在治疗与疼痛有关的疾病状态，特别是外周疼痛，炎症性疼痛或可用P2X3受体亚基调节剂治疗的组织损伤疼痛中发挥关键作用的新型P2X3受体拮抗剂。
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56.发明授权2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease 有权用作治疗阿尔茨海默病的β-分泌酶抑制剂的2,4,6-取代的吡啶基衍生物化合物公开(公告)号：US07968571B2
公开(公告)日：2011-06-28
申请号：US11547994
申请日：2005-04-20
申请人： James C. Barrow , Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer , Joseph P. Vacca , Shawn J. Stachel , Craig A. Coburn , Matthew G. Stanton
发明人： James C. Barrow , Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer , Joseph P. Vacca , Shawn J. Stachel , Craig A. Coburn , Matthew G. Stanton
IPC分类号： A61K31/443 , C07D413/04
CPC分类号： C07D413/04 , C07D401/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention is directed to 2,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的2,4,6-取代的吡啶衍生物化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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公开(公告)号：US20100093779A1
公开(公告)日：2010-04-15
申请号：US12446763
申请日：2007-10-22
IPC分类号： A61K31/4745 , C07D498/14 , A61P31/12
CPC分类号： C07D498/18
摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。
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公开(公告)号：US07696192B2
公开(公告)日：2010-04-13
申请号：US11662246
申请日：2005-09-06
申请人： Ian M. Bell , Steven N. Gallicchio , Craig A. Stump , Cory R. Theberge , Joseph P. Vacca , C. Blair Zartman , Xufang Zhang
发明人： Ian M. Bell , Steven N. Gallicchio , Craig A. Stump , Cory R. Theberge , Joseph P. Vacca , C. Blair Zartman , Xufang Zhang
IPC分类号： A61K31/554
CPC分类号： C07D519/00 , C07D209/96 , C07D471/06 , C07D471/16 , C07D487/06
摘要： The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are 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.
摘要翻译： 本发明涉及式I化合物：其中A1，A2，B1，B2，B3，B4，D1，D2，J，K，T，U，V，W，X，Y，Z， R5a，R5b，R5c，m和n在本文中定义），其可用作CGRP受体的拮抗剂，并且可用于治疗或预防涉及CGRP的疾病，例如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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59.发明申请Cyclic Ketal Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease 有权用于治疗阿尔茨海默病的循环型β-分泌酶抑制剂公开(公告)号：US20090176836A1
公开(公告)日：2009-07-09
申请号：US11989990
申请日：2006-07-28
IPC分类号： A61K31/443 , C07D307/20 , A61K31/341 , C07D405/10 , A61K31/4025 , C07D405/12 , A61P25/28 , A61P43/00
CPC分类号： C07D307/22 , C07D405/12
摘要： The present invention is directed to cyclic ketal compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及式（I）的环状缩酮化合物，其是β-分泌酶的抑制剂并且可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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60.发明授权N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease 有权用于治疗阿尔茨海默氏病的N-烷基苯基卡巴酰胺β-分泌酶抑制剂公开(公告)号：US07291620B2
公开(公告)日：2007-11-06
申请号：US10563538
申请日：2004-06-25
IPC分类号： A61K31/4965 , A61K31/445 , A61K31/40 , A61K31/279 , A61K31/16
CPC分类号： C07C237/10 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D207/10 , C07D207/14 , C07D211/38 , C07D295/084 , C07D295/185
摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗或预防涉及β-分泌酶的疾病如阿尔茨海默氏病的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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