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公开(公告)号：US20170217986A1
公开(公告)日：2017-08-03
申请号：US15123111
申请日：2015-03-02
申请人： John A. MCCAULEY , David Johathan BENNETT , Christopher J. BUNGARD , Thomas J. GRESHOCK , M. Katharine HOLLOWAY , Peter D. WILLIAMS , Christian BEAULIEU , Sheldon CRANE , Stephanie LESSARD , Daniel MCKAY , Carmela MOLINARO , Oscar Miguel MORADEI , Vijayasaradhi SIVALENKA , Vouy Linh TRUONG , Satyanarayana TUMMANAPALLI , Merck Canada Inc.
发明人： John A. McCauley , David Jonathan Bennett , Christopher J. Bungard , Thomas J. Greshock , M. Katharine Holloway , Peter D. Williams , Christian Beaulieu , Sheldon Crane , Stephanie Lessard , Daniel Mckay , Carmela Molinaro , Oscar Miguel Moradei , Vijayasaradhi Sivalenka , Vouy Linh Truong , Satyanarayana Tummanapalli
IPC分类号： C07D498/10 , A61K31/5375 , C07D413/12 , A61K31/5377 , C07D417/14 , A61K45/06 , C07D487/04 , C07D471/04 , C07D413/06 , C07D265/36 , A61K31/5386 , C07D265/30 , C07D413/14
CPC分类号： C07D498/10 , A61K31/5375 , A61K31/5377 , A61K31/5386 , A61K45/06 , C07D265/30 , C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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公开(公告)号：US09315475B2
公开(公告)日：2016-04-19
申请号：US14021930
申请日：2013-09-09
申请人： Christian Beaulieu , David J. Bennett , Christopher J. Bungard , Ronald K. Chang , Sheldon Crane , Thomas J. Greshock , Li Hao , Kate Holloway , Jesse J. Manikowski , John A. McCauley , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Philippe G. Nantermet , Christian Nadeau , Satyanarayana Tummanapalli , William Shipe , Sanjay Kumar Singh , Vouy Linh Truong , Sivalenka Vijayasaradhi , Peter D. Williams , Catherine M. Wiscount
发明人： Christian Beaulieu , David J. Bennett , Christopher J. Bungard , Ronald K. Chang , Sheldon Crane , Thomas J. Greshock , Li Hao , Kate Holloway , Jesse J. Manikowski , John A. McCauley , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Philippe G. Nantermet , Christian Nadeau , Satyanarayana Tummanapalli , William Shipe , Sanjay Kumar Singh , Vouy Linh Truong , Sivalenka Vijayasaradhi , Peter D. Williams , Catherine M. Wiscount
IPC分类号： C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D265/30 , C07D487/04 , C07D493/04 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07F7/08
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D493/04 , C07F7/0814
摘要： The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. 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所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 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：US09133157B2
公开(公告)日：2015-09-15
申请号：US14353865
申请日：2012-10-26
IPC分类号： A61K31/381 , C07D333/10 , C07D333/20 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D277/28 , C07B59/00
CPC分类号： C07D333/20 , C07B59/002 , C07D277/28 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要： Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. 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： 公开了式I化合物：其中A，R1，R2，R3，R4A，R4B，R5，R6和R7如本文所定义。 式I所包括的化合物包括作为HIV蛋白酶抑制剂的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 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：US07405229B2
公开(公告)日：2008-07-29
申请号：US10560672
申请日：2004-06-28
申请人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel J. McKay , Renata Oballa , Joel Robichaud
发明人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel J. McKay , Renata Oballa , Joel Robichaud
IPC分类号： A61K31/44 , A61K31/445 , A61K31/417 , A61K31/4184 , C07D211/80 , C07D233/54 , C07D235/04
CPC分类号： C07D213/83 , C07C255/29 , C07C311/06 , C07C323/25 , C07C323/49 , C07C323/60 , C07C323/61 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D211/20 , C07D213/32 , C07D231/12 , C07D233/64 , C07D235/06 , C07D257/04
摘要： This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类具有通式（I）的化合物，它是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中抑制骨的疾病 表示吸收，如骨质疏松症。
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公开(公告)号：US20140200197A1
公开(公告)日：2014-07-17
申请号：US14021930
申请日：2013-09-09
申请人： JOHN A. MCCAULEY , CHRISTIAN BEAULIEU , DAVID J. BENNETT , CHRISTOPHER J. BUNGARD , RONALD K. CHANG , SHELDON CRANE , THOMAS J. GRESHOCK , LI HAO , KATE HOLLOWAY , JESSE J. MANIKOWSKI , DANIEL MCKAY , CARMELA MOLINARO , OSCAR MIGUEL MORADEI , PHILIPPE G. NANTERMET , CHRISTIAN NADEAU , TUMMANAPALLI SATYANARAYANA , WILLIAM SHIPE , SANJAY KUMAR SINGH , VOUY LINH TRUONG , SIVALENKA VIJAYARADHI , PETER D. WILLIAMS , CATHERINE M. WISCOUNT
发明人： JOHN A. MCCAULEY , CHRISTIAN BEAULIEU , DAVID J. BENNETT , CHRISTOPHER J. BUNGARD , RONALD K. CHANG , SHELDON CRANE , THOMAS J. GRESHOCK , LI HAO , KATE HOLLOWAY , JESSE J. MANIKOWSKI , DANIEL MCKAY , CARMELA MOLINARO , OSCAR MIGUEL MORADEI , PHILIPPE G. NANTERMET , CHRISTIAN NADEAU , TUMMANAPALLI SATYANARAYANA , WILLIAM SHIPE , SANJAY KUMAR SINGH , VOUY LINH TRUONG , SIVALENKA VIJAYARADHI , PETER D. WILLIAMS , CATHERINE M. WISCOUNT
IPC分类号： C07D265/30 , A61K45/06 , C07D413/12 , A61K31/695 , C07D413/06 , C07D417/12 , C07D487/04 , C07F7/08 , A61K31/5375 , A61K31/5377
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D493/04 , C07F7/0814
摘要： The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. 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所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 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：US09187415B2
公开(公告)日：2015-11-17
申请号：US13882329
申请日：2011-10-27
IPC分类号： C07C311/41 , C07C311/42 , C07D231/12 , C07D261/08 , C07D277/64 , C07D239/26 , C07D417/12 , C07D417/14 , A61K31/428 , A61K31/42 , A61K31/415 , A61K31/4439 , A61K31/4412 , A61K31/506 , A61K31/18 , C07C311/18 , C07C311/29 , C07C317/40 , C07C323/49 , C07D213/75 , A61K31/63 , A61K31/635 , A61K45/06 , C07D277/62
CPC分类号： C07C311/18 , A61K31/428 , A61K31/4439 , A61K31/506 , A61K31/63 , A61K31/635 , A61K45/06 , C07C311/29 , C07C311/41 , C07C317/40 , C07C323/49 , C07C2601/02 , C07D213/75 , C07D231/12 , C07D239/26 , C07D261/08 , C07D277/62 , C07D277/64 , C07D417/12 , C07D417/14
摘要： Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. 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： 公开了式I的化合物：其中L，A，R1，R2，R3A，R3B，R4A，R4B，R5，R6和R7如本文所定义。 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 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：US20140018326A1
公开(公告)日：2014-01-16
申请号：US13882329
申请日：2011-10-27
IPC分类号： C07C311/18 , A61K45/06 , C07D261/08 , A61K31/635 , C07D239/26 , C07D213/75 , C07D277/62 , A61K31/428 , C07D417/12 , C07D417/14 , A61K31/4439 , A61K31/506 , A61K31/63 , C07D231/12
CPC分类号： C07C311/18 , A61K31/428 , A61K31/4439 , A61K31/506 , A61K31/63 , A61K31/635 , A61K45/06 , C07C311/29 , C07C311/41 , C07C317/40 , C07C323/49 , C07C2601/02 , C07D213/75 , C07D231/12 , C07D239/26 , C07D261/08 , C07D277/62 , C07D277/64 , C07D417/12 , C07D417/14
摘要： Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. 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： 公开了式I的化合物：其中L，A，R1，R2，R3A，R3B，R4A，R4B，R5，R6和R7如本文所定义。 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 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：US20090093444A1
公开(公告)日：2009-04-09
申请号：US11988346
申请日：2006-07-05
申请人： Cameron Black , Sheldon Crane , Renata Oballa , Joel Robichaud
发明人： Cameron Black , Sheldon Crane , Renata Oballa , Joel Robichaud
IPC分类号： A61K31/663 , C07D231/12 , A61K31/59 , A61P19/00 , A61P35/00 , A61P11/00 , A61P3/00 , A61P19/10 , A61K31/415
CPC分类号： C07D231/12
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症
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公开(公告)号：US07928091B2
公开(公告)日：2011-04-19
申请号：US11988346
申请日：2006-07-05
申请人： Cameron Black , Sheldon Crane , Renata Oballa , Joel Robichaud
发明人： Cameron Black , Sheldon Crane , Renata Oballa , Joel Robichaud
IPC分类号： A61K31/663 , C07D231/12
CPC分类号： C07D231/12
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
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公开(公告)号：US20070167635A1
公开(公告)日：2007-07-19
申请号：US10560672
申请日：2004-06-28
申请人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel McKay , Renata Oballa , Joel Robichaud
发明人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel McKay , Renata Oballa , Joel Robichaud
IPC分类号： G01N33/48 , C07D233/14 , C07D233/22
CPC分类号： C07D213/83 , C07C255/29 , C07C311/06 , C07C323/25 , C07C323/49 , C07C323/60 , C07C323/61 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D211/20 , C07D213/32 , C07D231/12 , C07D233/64 , C07D235/06 , C07D257/04
摘要： This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类具有通式（I）的化合物，它是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中抑制骨的疾病 表示吸收，如骨质疏松症。
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