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1. 发明授权

US06573259B2 Inhibitors of interleukin-1&bgr; converting enzyme 失效
标题翻译：白细胞介素-1β转换酶抑制剂
公开(公告)号：US06573259B2
公开(公告)日：2003-06-03
申请号：US10035850
申请日：2001-10-23
申请人： Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
发明人： Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
IPC分类号： A61K3155
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). 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 interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-&ggr; production and methods for treating interleukin-1, apoptosis- and interferon-&ggr;-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶（“ICE”）抑制剂的新型化合物。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗白细胞介素-1-（“IL-1”），细胞凋亡，干扰素-γ诱导因子（IGIF）干扰素-γ-（“IFN-γ”）介导的疾病，过度饮食酒精摄入疾病或病毒性疾病，包括炎性疾病，自身免疫疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白细胞介素-1，凋亡和干扰素-γ介导的疾病的方法。本发明还涉及制备本发明化合物的方法。

2. 发明授权

US06974809B2 Inhibitors of interleukin 1-β converting enzyme 失效
标题翻译：白介素1-β转换酶抑制剂
公开(公告)号：US06974809B2
公开(公告)日：2005-12-13
申请号：US10424576
申请日：2003-04-25
申请人： Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
发明人： Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
IPC分类号： A61K38/00 , A61K38/55 , A61P1/00 , A61P1/18 , A61P7/00 , A61P9/10 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/14 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07K5/02 , C07K5/023 , C07K5/097 , C07D491/00 , C07D495/00 , A61K31/55
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme (“ICE”). 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 interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), interferon-γ-(“IFN-γ”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-γ production and methods for treating interleukin-1, apoptosis- and interferon-γ-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶（“ICE”）抑制剂的新型化合物。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗白细胞介素-1-（“IL-1”），细胞凋亡，干扰素-γ诱导因子（IGIF）干扰素-γ-（“IFN-γ”）介导的疾病，过度饮食酒精摄入疾病或病毒性疾病，包括炎性疾病，自身免疫疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白细胞介素-1，凋亡和干扰素-γ介导的疾病的方法。本发明还涉及制备本发明化合物的方法。

3. 发明授权

US06329365B1 Inhibitors of interleukin-1&bgr; converting enzyme 失效
标题翻译：白细胞介素-1β转换酶抑制剂
公开(公告)号：US06329365B1
公开(公告)日：2001-12-11
申请号：US09326495
申请日：1999-06-04
申请人： Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
发明人： Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
IPC分类号： A61K3155
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). 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 interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-&ggr; production and methods for treating interleukin-1, apoptosis- and interferon-&ggr;-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶（“ICE”）抑制剂的新型化合物。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗白细胞介素-1-（“IL-1”），细胞凋亡，干扰素-γ诱导因子（IGIF）干扰素-γ-（“IFN-γ”）介导的疾病，过度饮食酒精摄入疾病或病毒性疾病，包括炎性疾病，自身免疫疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白细胞介素-1，凋亡和干扰素-γ介导的疾病的方法。本发明还涉及制备本发明化合物的方法。

4. 发明授权

US06350741B1 Inhibitors of interleukin-1&bgr; converting enzyme 失效
标题翻译：白细胞介素-1β转换酶抑制剂
公开(公告)号：US06350741B1
公开(公告)日：2002-02-26
申请号：US09326494
申请日：1999-06-04
申请人： Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
发明人： Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
IPC分类号： A61K3155
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). 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 interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-&ggr; production and methods for treating interleukin-1, apoptosis- and interferon-&ggr;-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶（“ICE”）抑制剂的新型化合物。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗白细胞介素-1-（“IL-1”），细胞凋亡，干扰素-γ诱导因子（IGIF）或“干扰素-γ”（“IFN-γ”）介导的疾病，包括炎性疾病，自身免疫性疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白细胞介素-1，凋亡和干扰素-γ介导的疾病的方法。本发明还涉及制备本发明化合物的方法。

5. 发明授权

US07790713B2 Inhibitors of interleukin-1β converting enzyme 失效
标题翻译：白细胞介素-1抑制剂转化酶
公开(公告)号：US07790713B2
公开(公告)日：2010-09-07
申请号：US11655938
申请日：2007-01-18
申请人： 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
发明人： 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
IPC分类号： C07D243/12 , A61K31/55 , A61P29/00
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β 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-γ-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-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing-N-acylamino compounds.
摘要翻译：本发明涉及作为白介素-1和bgr的抑制剂的新型化合物。转化酶。本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗IL-1，细胞凋亡，IGIF和IFN-γ介导的疾病，炎性疾病，自身免疫性疾病破坏性骨病，增殖性疾病，感染性疾病，退行性疾病和坏死性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性，用于治疗白细胞介素-1，细胞凋亡，IGIF和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。本发明还涉及N-酰基氨基化合物的制备方法。

6. 发明授权

US06423840B1 Inhibitors of interleukin-1&bgr; converting enzyme 失效
标题翻译：白细胞介素-1β转换酶抑制剂
公开(公告)号：US06423840B1
公开(公告)日：2002-07-23
申请号：US09773477
申请日：2001-01-31
申请人： 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
发明人： 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
IPC分类号： C07D47104
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; 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-&ggr;-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-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶抑制剂的新型化合物。本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗IL-1，细胞凋亡，IGIF和IFN-γ介导的疾病，炎性疾病，自身免疫性疾病破坏性骨病，增殖性疾病，感染性疾病，退行性疾病和坏死性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性，治疗白细胞介素-1，细胞凋亡，IGIF-和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。本发明还涉及制备N-酰基氨基化合物的方法。

7. 发明授权

US06204261B1 Inhibitors of interleukin-1&bgr; Converting enzyme inhibitors 失效
标题翻译：白细胞介素-1β抑制剂转化酶抑制剂
公开(公告)号：US06204261B1
公开(公告)日：2001-03-20
申请号：US08761483
申请日：1996-12-06
申请人： 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
发明人： 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
IPC分类号： A61K3155
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: which compounds are inhibitors of interleukin-1beta converting enzyme.
摘要翻译：本发明涉及下式的吡嗪并[1,2-a] [1,2]二氮杂-1-甲酰胺化合物：该化合物是白细胞介素-1β转换酶的抑制剂。

8. 发明授权

US08119631B2 Inhibitors of interleukin-1β converting enzyme 失效
标题翻译：白细胞介素-1抑制剂转化酶
公开(公告)号：US08119631B2
公开(公告)日：2012-02-21
申请号：US12786221
申请日：2010-05-24
申请人： 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
发明人： 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
IPC分类号： C07D243/12 , C07D255/04 , C07D257/10 , C07D259/00 , A61K31/55 , A61P29/00
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β 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-γ-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-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.
摘要翻译：本发明涉及作为白介素-1和bgr的抑制剂的新型化合物。转化酶。本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗IL-1，细胞凋亡，IGIF和IFN-γ介导的疾病，炎性疾病，自身免疫性疾病破坏性骨病，增殖性疾病，感染性疾病，退行性疾病和坏死性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性，用于治疗白细胞介素-1，细胞凋亡，IGIF和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。本发明还涉及制备N-酰基氨基化合物的方法。

9. 发明授权

US06258948B1 Inhibitors of Interleukin-1&bgr; converting enzyme 失效
标题翻译：白细胞介素-1β转换酶抑制剂
公开(公告)号：US06258948B1
公开(公告)日：2001-07-10
申请号：US09400639
申请日：1999-09-21
申请人： 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
发明人： 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
IPC分类号： C07D26702
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-IB 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-&ggr;-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-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.
摘要翻译：本发明涉及作为白介素-IB转化酶抑制剂的新型化合物。本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗IL-1，细胞凋亡，IGIF和IFN-γ介导的疾病，炎性疾病，自身免疫性疾病破坏性骨病，增殖性疾病，感染性疾病，退行性疾病和坏死性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性，治疗白细胞介素-1，细胞凋亡，IGIF-和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。本发明还涉及制备N-酰基氨基化合物的方法。

10. 发明授权

US06632942B2 Asymmetric synthesis of piperazic acid and derivatives thereof 失效
标题翻译：哌嗪酸及其衍生物的不对称合成
公开(公告)号：US06632942B2
公开(公告)日：2003-10-14
申请号：US10168463
申请日：2002-06-14
申请人： Andrea L. C. Robidoux , Siro Serafini , Petra Dieterich , Stefania Leonardi , John Stibbard
发明人： Andrea L. C. Robidoux , Siro Serafini , Petra Dieterich , Stefania Leonardi , John Stibbard
IPC分类号： C07D23704
CPC分类号： C07D487/04 , C07D237/04
摘要： This invention provides a concise, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an (R)-2,5-dihydroxyvalerate ester intermediate. After the hydroxy groups are converted to suitable leaving groups, such as mesylates, the ester is treated with a bis-protected hydrazine to provide the desired (3S)-piperazic acid derivative. The (3R) enantiomer of piperazic acid may be similarly obtained starting with L-glutamic acid. The method may also be used to obtain piperazic acid derivatives that have moderate optical purity or are racemic. By this method, piperazic acid derivatives may be obtained that are useful as intermediates for pharmacologically active compounds. For example, certain intermediates of this invention are useful for preparing caspase inhibitors, particularly inhibitors of ICE, through additional steps known in the art.
摘要翻译：本发明提供哌嗪酸及其衍生物的简明，不对称合成，由此可以以高光学纯度获得（3S） - 或（3R） - 对映体形式。（3S） - 哌嗪酸通过（R）-2,5-二羟基戊酸酯中间体衍生自D-谷氨酸。将羟基转化为合适的离去基团（如甲磺酸酯）后，用双 - 保护的肼处理酯，得到所需的（3S） - 哌嗪酸衍生物。哌嗪酸的（3R）对映异构体可以从L-谷氨酸开始类似地获得。该方法也可用于获得具有中等光学纯度或外消旋的哌嗪酸衍生物。通过该方法，可以得到可用作药理活性化合物的中间体的哌嗪酸衍生物。例如，通过本领域已知的附加步骤，本发明的某些中间体可用于制备胱天蛋白酶抑制剂，特别是ICE的抑制剂。

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