公开(公告)号：US07001899B2

公开(公告)日：2006-02-21

申请号：US10457720

申请日：2003-06-09

申请人： John August Wos ,  Yili Wang ,  Kofi Abeka Oppong ,  Steven Victor O'Neil ,  Michael Christopher Laufersweiler ,  David Lindsey Soper ,  Biswanath De ,  Thomas Prosser Demuth, Jr.

发明人： John August Wos ,  Yili Wang ,  Kofi Abeka Oppong ,  Steven Victor O'Neil ,  Michael Christopher Laufersweiler ,  David Lindsey Soper ,  Biswanath De ,  Thomas Prosser Demuth, Jr.

IPC分类号： C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/554

CPC分类号： C07D405/12 ,  A61K38/00 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07K5/0202 ,  C07K5/06078

摘要： The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: wherein each X is independently selected from: i) —C(W)2—; ii) —C(O)—; iii) —NR2—; iv) —S—; v) —S(O)—; vi) —S(O)2—; vii) two units, one from each adjacent X unit, can be taken together to form a substituted or unsubstituted double bond having the formula —CW═CW—; wherein each W is hydrogen of a unit having the formula —(L2)j—R2, the index j is 0 or 1; R is a carbocyclic or heterocyclic aryl ring; R1 is a cysteine trap; each R2 is independently a suitable substituent; and L, L1, and L2 are linking units.

摘要翻译： 本发明涉及新化合物，包含所述化合物的组合物及其用途，所述化合物具有下式：化学式id =“CHEM-US-00001”num =“000

公开(公告)号：US07138395B2

公开(公告)日：2006-11-21

申请号：US10457188

申请日：2003-06-09

申请人： Steven Victor O'Neil ,  Michael Christopher Laufersweiler ,  Yili Wang ,  Kofi Abeka Oppong ,  David Lindsey Soper ,  John August Wos ,  Biswanath De ,  Thomas Prosser Demuth, Jr.

发明人： Steven Victor O'Neil ,  Michael Christopher Laufersweiler ,  Yili Wang ,  Kofi Abeka Oppong ,  David Lindsey Soper ,  John August Wos ,  Biswanath De ,  Thomas Prosser Demuth, Jr.

IPC分类号： C07D471/04 ,  C07D498/04 ,  A61K31/4995 ,  A61K31/537 ,  A61P29/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: X is —CH2—, —O— or —NR9—; R is a carbocyclic or heterocyclic ring; R1 is a cysteine trap; R2a, R2a′, R2b, and R2b′ are each independently hydrogen, C1–C4 alkyl, C1–C4 alkoxy, and mixtures thereof; or R2a′ and R2b′ can taken together to form a double bond; R9 is hydrogen or a unit having the formula -L2-R10; L is the same as defined herein above; R10 is hydrogen; substituted or unsubstituted C1–C6 linear; branched, or cyclic hydrocarbyl; substituted or unsubstituted aryl; substituted or unsubstituted C1–C9 heterocyclic; and substituted or unsubstituted heteroaryl.

摘要翻译： 本发明涉及新化合物，包含所述化合物的组合物及其用途，所述具有下式的化合物：X为-CH 2 - ， - O-或-NR 9 > - ; R是碳环或杂环; R 1是半胱氨酸阱; R 2a，R 2a，R 2b和R 2b'各自独立地为氢，C

公开(公告)号：US07041696B2

公开(公告)日：2006-05-09

申请号：US10457181

申请日：2003-06-09

申请人： John August Wos ,  David Lindsey Soper ,  Steven Victor O'Neil ,  Yili Wang ,  Kofi Abeka Oppong ,  Michael Christopher Laufersweiler ,  Jian Chen ,  Biswanath De ,  Thomas Prosser Demuth, Jr.

发明人： John August Wos ,  David Lindsey Soper ,  Steven Victor O'Neil ,  Yili Wang ,  Kofi Abeka Oppong ,  Michael Christopher Laufersweiler ,  Jian Chen ,  Biswanath De ,  Thomas Prosser Demuth, Jr.

IPC分类号： C07D487/04 ,  A61K31/403 ,  A61P29/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention relates to interleukin-1β converting enzyme inhibitors having the formula: R is a carbocyclic or heterocyclic ring; R1 is a cysteine trap; R2a, R2a′, R2b, and R2b′ are each independently hydrogen, C1–C4 alkyl, C1–C4 alkoxy, and mixtures thereof; or R2a′ and R2b′ can taken together to form a double bond; L and L1 are linking groups having the formula: T is selected from the group consisting of: i) —NR6—; ii) —O—; iii) —NR6S(O)2—; iv) —S(O)2NR6—; and v) mixtures thereof; R6 is hydrogen, substituted or unsubstituted C1–C20 linear, branched, or cyclic alkyl, C6–C20 aryl, C7–C20 alkylenearyl, and mixtures thereof; the indices w, w1, and w2 are each independently 0 or 1; i) hydrogen; ii) C1–C4 linear, branched, and cyclic alkyl; iii) R3a and R3b or R4a, and R4b can be taken together to form a carbonyl unit; iv) two R3a or two R3b units from adjacent carbon atoms or two R4a or two R4b units from adjacent carbon atoms can be taken together to form a double bond; and v) mixtures thereof; the index m is from 0 to 5; the index n is from 0 to 5.

摘要翻译： 本发明涉及具有下式的白细胞介素-1β转换酶抑制剂：R是碳环或杂环; R 1是半胱氨酸阱; R 2a，R 2a，R 2b和R 2b'各自独立地为氢，C