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1.发明授权Cyanoamido-containing heterocyclic compounds useful as reversible inhibitors of cysteine proteases 有权可用作半胱氨酸蛋白酶的可逆抑制剂的含氰酰氨基的杂环化合物公开(公告)号：US06936606B2
公开(公告)日：2005-08-30
申请号：US10256512
申请日：2002-09-27
申请人： Younes Bekkali , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young , Eugene R. Hickey , Weimin Liu , Usha R. Patel
发明人： Younes Bekkali , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young , Eugene R. Hickey , Weimin Liu , Usha R. Patel
IPC分类号： C07D295/12 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/428 , A61K31/517 , A61K31/536 , A61K31/5375 , A61K31/5377 , A61P1/04 , A61P3/10 , A61P5/14 , A61P9/10 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07C257/20 , C07C269/06 , C07C271/20 , C07C271/64 , C07C319/20 , C07C323/41 , C07C323/60 , C07D211/22 , C07D213/30 , C07D213/57 , C07D239/80 , C07D263/32 , C07D265/24 , C07D275/06 , C07D277/30 , C07D295/14 , C07D295/215 , C07D307/12 , C07D307/54 , C07D309/08 , C07D309/12 , C07D333/24 , C07D401/04 , C07D401/06 , C07D239/95 , C07D401/12
CPC分类号： C07D295/215 , C07C271/64 , C07C323/60 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07D213/57 , C07D263/32 , C07D277/30 , C07D307/54 , C07D333/24
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds
摘要翻译： 公开了式（Ia）和（Ib）的新型组织蛋白酶S，K，F，L和B可逆抑制性化合物，其中R 1，R 2，R 2 R 3，R 4，R 5，R 6，R 8，R SUB， > 9＆gt;和X在本文中定义。 该化合物可用于治疗自身免疫性疾病和其他疾病。 还公开了制备这些新化合物的方法
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公开(公告)号：US06858623B2
公开(公告)日：2005-02-22
申请号：US10448698
申请日：2003-05-29
申请人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
发明人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
IPC分类号： A61K31/40 , A61K31/4468 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/5365 , A61K31/5377 , A61K31/538 , A61K31/541 , A61K31/55 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P19/10 , A61P21/04 , A61P25/28 , A61P29/00 , A61P31/00 , A61P37/00 , A61P37/06 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D401/12 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08 , A61K31/445 , A61K31/404 , A61K31/428 , A61K31/4523 , A61K31/536 , C07D223/06 , C07D239/80 , C07D263/54 , C07D265/28 , C07D277/62 , C07D451/02
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
摘要翻译： 公开了式（Ia）和（Ib）的新型组织蛋白酶S，K，F，L和B可逆抑制性化合物，其中R 2，R 3，R 4，R 5，R 6，R 7，R 8，Het和X如本文所定义 。 该化合物可用于治疗自身免疫性疾病和其他疾病。 还公开了制备这些新化合物的方法。
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公开(公告)号：US06787540B2
公开(公告)日：2004-09-07
申请号：US10261994
申请日：2002-10-01
申请人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
发明人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
IPC分类号： A61K31535
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
摘要翻译： 公开了式（Ia）和（Ib）的新型组织蛋白酶S，K，F，L和B可逆抑制性化合物，其中R2，R3，R4，R5，R6，R7，R8，Het和X如本文所定义。 该化合物可用于治疗自身免疫性疾病和其他疾病。 还公开了制备这些新化合物的方法。
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公开(公告)号：US06525052B2
公开(公告)日：2003-02-25
申请号：US09808439
申请日：2001-03-14
申请人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
发明人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
IPC分类号： A61K31335
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
摘要翻译： 公开了式（Ia）和（Ib）的新型组织蛋白酶S，K，F，L和B可逆抑制性化合物，其中R2，R3，R4，R5，R6，R7，R8，Het和X如本文所定义。 该化合物可用于治疗自身免疫性疾病和其他疾病。 还公开了制备这些新化合物的方法。
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5.发明授权公开(公告)号：US06313117B1
公开(公告)日：2001-11-06
申请号：US09627869
申请日：2000-07-28
申请人： Younes Bekkali , Rajashehar Betageri , Michel Jose Emmanuel , Eugene Richard Hickey , Weimin Liu , Usha R. Patel , Denice Mary Spero , David S. Thomson , Yancey David Ward , Erick Richard Roush Young , Sanxing Sun
发明人： Younes Bekkali , Rajashehar Betageri , Michel Jose Emmanuel , Eugene Richard Hickey , Weimin Liu , Usha R. Patel , Denice Mary Spero , David S. Thomson , Yancey David Ward , Erick Richard Roush Young , Sanxing Sun
IPC分类号： A61K315355
CPC分类号： C07D295/185 , C07B2200/07 , C07C255/31 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2602/20 , C07D207/16 , C07D211/66 , C07D403/06 , C07D405/04 , C07D409/06
摘要： Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
摘要翻译： 公开了式（I）/（Ia）的新型琥珀酸酯衍生物化合物：其中R1，R2，R3，R4，R5，R6，R7，X和A如本文所定义。 该化合物可用作半胱氨酸蛋白酶的抑制剂。 还公开了使用方法和制备这些化合物的方法。
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公开(公告)号：US06982263B2
公开(公告)日：2006-01-03
申请号：US10163015
申请日：2002-06-04
申请人： Eugene R. Hickey , Younes Bekkali , Usha R. Patel , Denice Mary Spero , David S. Thomson , Erick Richard Roush Young
发明人： Eugene R. Hickey , Younes Bekkali , Usha R. Patel , Denice Mary Spero , David S. Thomson , Erick Richard Roush Young
IPC分类号： C07D207/16 , C07D211/66 , C07D217/56 , C07D223/12 , C07D413/12
CPC分类号： C07D213/84 , C07B2200/07 , C07C255/29 , C07C271/12 , C07C271/28 , C07C271/30 , C07C271/34 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/28 , C07C2602/50 , C07D207/16 , C07D295/185 , C07D295/205 , C07D295/215
摘要： Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.
摘要翻译： 公开了本文进一步定义的式（I）的新型腈化合物，该化合物可用作半胱氨酸蛋白酶如组织蛋白酶K，S，F，L和B的可逆抑制剂。这些化合物可用于治疗由这些化合物加重的疾病和病理状况 蛋白酶，例如但不限于骨质疏松症，类风湿性关节炎，多发性硬化症，哮喘和其它自身免疫性疾病，阿尔茨海默氏病，动脉粥样硬化。 还公开了制备这些新化合物的方法。
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公开(公告)号：US07056915B2
公开(公告)日：2006-06-06
申请号：US10422471
申请日：2003-04-24
申请人： Michel Jose Emmanuel , Eugene R. Hickey , Weimin Liu , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey David Ward , Erick Richard Roush Young
发明人： Michel Jose Emmanuel , Eugene R. Hickey , Weimin Liu , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey David Ward , Erick Richard Roush Young
IPC分类号： A61K31/535 , C07D265/12
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds
摘要翻译： 公开了本文进一步定义的新颖的组织蛋白酶S，K，F，L和B可逆抑制化合物（I），（II），（Ia）和（Ib）。 该化合物可用于治疗自身免疫性疾病。 还公开了制备这些新化合物的方法
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公开(公告)号：US06420364B1
公开(公告)日：2002-07-16
申请号：US09655351
申请日：2000-09-08
申请人： Michel Jose Emmanuel , Leah L. Frye , Eugene R. Hickey , Weimin Liu , Tina Marie Morwick , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey David Ward , Erick Richard Roush Young
发明人： Michel Jose Emmanuel , Leah L. Frye , Eugene R. Hickey , Weimin Liu , Tina Marie Morwick , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey David Ward , Erick Richard Roush Young
IPC分类号： A61K31535
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
摘要翻译： 公开了本文进一步定义的新颖的组织蛋白酶S，K，F，L和B可逆抑制化合物（I），（II），（Ia）和（Ib）。 该化合物可用于治疗自身免疫性疾病。 还公开了制备这些新化合物的方法。
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公开(公告)号：US07279472B2
公开(公告)日：2007-10-09
申请号：US10937636
申请日：2004-09-09
申请人： Michel Jose Emmanuel , Leah L. Frye , Eugene R. Hickey , Weimin Liu , Tina Marie Morwick , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey David Ward , Erick Richard Roush Young
发明人： Michel Jose Emmanuel , Leah L. Frye , Eugene R. Hickey , Weimin Liu , Tina Marie Morwick , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey David Ward , Erick Richard Roush Young
IPC分类号： A61K31/535 , A61K31/497 , A61K31/40 , C07D413/02 , C07D401/12
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds
摘要翻译： 公开了本文进一步定义的新颖的组织蛋白酶S，K，F，L和B可逆抑制化合物（I），（II），（Ia）和（Ib）。 该化合物可用于治疗自身免疫性疾病。 还公开了制备这些新化合物的方法
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公开(公告)号：US06982272B2
公开(公告)日：2006-01-03
申请号：US10422473
申请日：2003-04-24
申请人： Michel Jose Emmanuel , Eugene R. Hickey , Weimin Liu , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey David Ward , Erick Richard Roush Young
发明人： Michel Jose Emmanuel , Eugene R. Hickey , Weimin Liu , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey David Ward , Erick Richard Roush Young
IPC分类号： A61K31/445 , C07D213/02 , C07D409/12
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
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