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。

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。

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。

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。

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。

公开(公告)号：US20110178069A1

公开(公告)日：2011-07-21

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： A61K31/5513 ,  C07D243/14 ,  C07D401/12 ,  A61P19/02 ,  A61P1/18 ,  A61P1/00 ,  A61P17/06

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。

公开(公告)号：US20120165319A1

公开(公告)日：2012-06-28

申请号：US13293592

申请日：2011-11-10

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： A61K31/551 ,  A61K31/55 ,  A61P19/02 ,  A61P1/18 ,  A61P29/00 ,  A61P35/02 ,  A61P1/04 ,  A61P37/00 ,  A61P1/16 ,  A61P25/00 ,  A61P17/06 ,  A61P37/06 ,  C07D487/04 ,  A61P1/00

CPC分类号： C07D243/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  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。

公开(公告)号：US6008217A

公开(公告)日：1999-12-28

申请号：US575641

申请日：1995-12-20

申请人： Mark James Batchelor ,  David Bebbington ,  Guy W. Bemis ,  Wolf Herman Fridman ,  Roger John Gillespie ,  Julian M. C. Golec ,  David J. Lauffer ,  David J. Livingston ,  Saroop Singh Matharu ,  Michael D. Mullican ,  Mark A. Murcko ,  Robert Murdoch ,  Robert E. Zelle

发明人： Mark James Batchelor ,  David Bebbington ,  Guy W. Bemis ,  Wolf Herman Fridman ,  Roger John Gillespie ,  Julian M. C. Golec ,  David J. Lauffer ,  David J. Livingston ,  Saroop Singh Matharu ,  Michael D. Mullican ,  Mark A. Murcko ,  Robert Murdoch ,  Robert E. Zelle

IPC分类号： A61K38/00 ,  C07K5/02 ,  C07D217/22 ,  A61K31/47 ,  C07D217/16

CPC分类号： C07K5/0202 ,  A61K38/00

摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. 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 an IL-1 mediated disease, an apoptosis mediated disease, AML, CML, melanoma, myeloma, Kaposi's sarcoma, graft vs host disease, rheumatoid arthritis, inflammatory bowel disorder, psoriasis, osteoarthritis, myeloma, apoptosis, sepsis, rheumatoid arthritis, asthma, Alzheimer's disease, Parkinson's disease, and ischemic heart disease diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

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合于抑制ICE活性，因此可有利地用作抗IL-1介导的疾病，细胞凋亡介导的疾病，AML，CML，黑素瘤，骨髓瘤，卡波西氏肉瘤，移植物 与宿主疾病，类风湿性关节炎，炎性肠病，牛皮癣，骨关节炎，骨髓瘤，凋亡，败血症，类风湿性关节炎，哮喘，阿尔茨海默病，帕金森病和缺血性心脏病疾病相关。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性的方法和用于治疗白细胞介素-1介导的疾病的方法。

公开(公告)号：US5874424A

公开(公告)日：1999-02-23

申请号：US598332

申请日：1996-02-08

申请人： Mark James Batchelor ,  David Bebbington ,  Guy W. Bemis ,  Wolf Herman Fridman ,  Roger John Gillespie ,  Julian M. C. Golec ,  David J. Lauffer ,  David J. Livingston ,  Saroop Singh Matharu ,  Michael D. Mullican ,  Mark A. Murcko ,  Robert Murdoch ,  Robert E. Zelle

发明人： Mark James Batchelor ,  David Bebbington ,  Guy W. Bemis ,  Wolf Herman Fridman ,  Roger John Gillespie ,  Julian M. C. Golec ,  David J. Lauffer ,  David J. Livingston ,  Saroop Singh Matharu ,  Michael D. Mullican ,  Mark A. Murcko ,  Robert Murdoch ,  Robert E. Zelle

IPC分类号： A61K38/00 ,  C07K5/02 ,  A61K31/55 ,  C07D243/02

CPC分类号： C07K5/0202 ,  A61K38/00

摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. 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 an IL-1 mediated disease, an apoptosis mediated disease, AML, CML, melanoma, myeloma, Kaposi's sarcoma, graft vs host disease, rheumatoid arthritis, inflammatory bowel disorder, psoriasis, osteoarthritis, myeloma, apoptosis, sepsis, rheumatoid arthritis, asthma, Alzheimer's disease, Parkinson's disease, and ischemic heart disease diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

公开(公告)号：US6162790A

公开(公告)日：2000-12-19

申请号：US24537

申请日：1998-02-17

申请人： Guy W. Bemis ,  John P. Duffy ,  Wolf Herman Fridman ,  Julian M. C. Golec ,  David J. Livingston ,  Michael D. Mullican ,  Mark A. Murcko ,  Robert E. Zelle

发明人： Guy W. Bemis ,  John P. Duffy ,  Wolf Herman Fridman ,  Julian M. C. Golec ,  David J. Livingston ,  Michael D. Mullican ,  Mark A. Murcko ,  Robert E. Zelle

IPC分类号： A61K38/00 ,  A61K38/55 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P5/14 ,  A61P7/00 ,  A61P7/06 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P43/00 ,  C07K5/00 ,  C07K5/02 ,  C07K5/08 ,  C07K5/083

CPC分类号： C07K5/0205 ,  A61K38/00 ,  C07K5/0202 ,  Y02A50/475

摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1 .beta. converting enzyme. 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 and apoptosis-mediated diseases, including inflammatory diseases, autoimmune diseases, proliferative, infectious, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

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介素-1和细胞凋亡介导的疾病（包括炎性疾病，自身免疫性疾病，增殖性，感染性和退行性疾病）的药物。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性的方法和用于治疗白细胞介素-1介导的疾病的方法。