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1. 发明授权

US08168645B2 Arylsulfonamide compounds 有权
标题翻译：芳基磺酰胺化合物
公开(公告)号：US08168645B2
公开(公告)日：2012-05-01
申请号：US12513835
申请日：2007-11-15
申请人： Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne J. Fairbrother , John A. Flygare , Michael F. T. Koehler
发明人： Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne J. Fairbrother , John A. Flygare , Michael F. T. Koehler
IPC分类号： A61K31/517 , C07D239/72
CPC分类号： C07D239/94
摘要： The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: wherein A1, A2, B1, B2, B3, X, Z, R1, R2, R3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.
摘要翻译：本发明一般涉及模拟某些肽和蛋白质的生物学活性的小分子，含有它们的组合物及其用途。特别地，本发明涉及模拟仅含BH3蛋白的生物学活性的通式（I）的化合物，并能够结合并中和原生存Bcl-2蛋白：其中A1，A2，B1，B2， B3，X，Z，R1，R2，R3和t如本文所述。本发明还涉及制备模仿肽和蛋白质的一部分的苯磺酰胺化合物的方法，以及这些化合物在调节细胞死亡中的用途以及治疗和/或预防与细胞死亡调节相关的疾病或病症。

2. 发明申请

US20110077265A1 INHIBITORS OF IAP 有权
标题翻译： IAP的抑制剂
公开(公告)号：US20110077265A1
公开(公告)日：2011-03-31
申请号：US12598027
申请日：2008-04-29
申请人： John A. Flygare , Frederick Cohen , Kurt Deshayes , Michael F. T. Koehler , Lewis J. Gazzard , Lan Wang , Chudi Ndubaku
发明人： John A. Flygare , Frederick Cohen , Kurt Deshayes , Michael F. T. Koehler , Lewis J. Gazzard , Lan Wang , Chudi Ndubaku
IPC分类号： A61K31/437 , C07D417/14 , C07D513/04 , C07D403/12 , C12N5/071 , C07K2/00 , A61K31/4545 , A61K31/433 , A61K31/4025 , A61K31/427 , A61P35/00
CPC分类号： C07D417/14 , C07D207/16 , C07D519/00
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3′, R4, R4′ and R5, are as described herein.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中具有通式U1-M-U2的化合物，其中M是共价连接U1的R2，R3，R4或R5的连接基团与R2，R3 ，R4或R5组的U2; U1和U2具有通式（I），G，X 1，X 2，R 2，R 3，R 3'，R 4，R 4'和R 5如本文所述。

3. 发明授权

US08907092B2 Inhibitors of IAP 有权
标题翻译： IAP抑制剂
公开(公告)号：US08907092B2
公开(公告)日：2014-12-09
申请号：US12598027
申请日：2008-04-29
申请人： John A. Flygare , Frederick Cohen , Kurt Deshayes , Michael F. T. Koehler , Lewis J. Gazzard , Lan Wang , Chudi Ndubaku
发明人： John A. Flygare , Frederick Cohen , Kurt Deshayes , Michael F. T. Koehler , Lewis J. Gazzard , Lan Wang , Chudi Ndubaku
IPC分类号： C07D277/46 , C07D513/04 , C07D417/14 , A61K31/4365 , A61K31/4436 , A61K31/427 , C07D207/16 , C07D519/00
CPC分类号： C07D417/14 , C07D207/16 , C07D519/00
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3′, R4, R4′ and R5, are as described herein.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中具有通式U1-M-U2的化合物，其中M是共价连接U1的R2，R3，R4或R5的连接基团与R2，R3 ，R4或R5组的U2; U1和U2具有通式（I），G，X 1，X 2，R 2，R 3，R 3'，R 4，R 4'和R 5如本文所述。

4. 发明授权

US08273743B2 Quinoxaline inhibitors of the hedgehog signalling 失效
标题翻译：刺猬信号的喹喔啉抑制剂
公开(公告)号：US08273743B2
公开(公告)日：2012-09-25
申请号：US11587963
申请日：2005-04-29
申请人： Michael F. T. Koehler , Richard Goldsmith , Daniel P. Sutherlin
发明人： Michael F. T. Koehler , Richard Goldsmith , Daniel P. Sutherlin
IPC分类号： A61K31/495 , A61K31/44
CPC分类号： C07D413/12 , C07D241/42 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A is a carbocycle or heterocycle; X is alkylene, NR4C(O), NR4C(S), NR4C(NH), NR4SO, NR4SO2, NR4C(O)NH, NR4C(S)NH, C(O)NR4, C(S)NR4, C(NH)NR4, NR4PO or NR4PO(OH) wherein R4 is H or alkyl; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl or a heterocycle each of which is optionally substituted with hydroxy, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R2 is halogen, hydroxy, alkyl, acyl or alkoxy each optionally substituted with hydroxy, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R3 is halogen, hydroxy, alkyl, acyl or alkoxy each optionally substituted with hydroxy, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; m is 0-3; n is 0-3; and salts and solvates thereof. The invention also provides methods of using these compounds for therapy and/or prophylaxis in a mammal of hyperproliferative diseases and angiogenesis mediated diseases due to their activity for inhibiting the hedgehog signaling pathway.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导的新型抑制剂，其中化合物具有通式I：其中A是碳环或杂环; X是亚烷基，NR4C（O），NR4C（S），NR4C（NH），NR4SO，NR4SO2，NR4C（O）NH，NR4C（S）NH，C（O）NR4，C（S）NR4，C ）NR4，NR4PO或NR4PO（OH），其中R4是H或烷基; R1选自烷基，环烷基，芳基或杂环，其各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; R2是卤素，羟基，烷基，酰基或烷氧基，各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; R3是卤素，羟基，烷基，酰基或烷氧基，各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; m为0-3; n为0-3; 及其盐和溶剂合物。本发明还提供了使用这些化合物治疗和/或预防哺乳动物由于其抑制刺猬蛋白信号通路的活性而引起的过度增殖性疾病和血管生成介导的疾病的方法。

5. 发明申请

US20120270886A1 INHIBITORS OF IAP 审中-公开
标题翻译： IAP的抑制剂
公开(公告)号：US20120270886A1
公开(公告)日：2012-10-25
申请号：US13542548
申请日：2012-07-05
申请人： Michael F. T. Koehler , Lewis Gazzard , Vickie Hsiao-Wei Tsui
发明人： Michael F. T. Koehler , Lewis Gazzard , Vickie Hsiao-Wei Tsui
IPC分类号： A61K31/519 , A61K31/428 , A61P35/00 , A61K31/437
CPC分类号： C07D403/04 , C07D417/04 , C07D417/14 , C07D513/04
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3′, R4, R4′, R5, R6, R6′, and n are as described herein.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有通式（I）：其中Q，X1，X2，Y，Z1，Z2，Z3，Z4，R1，R2，R3， R3'，R4，R4'，R5，R6，R6'和n如本文所述。

6. 发明授权

US08247557B2 IAP inhibitors 失效
标题翻译： IAP抑制剂
公开(公告)号：US08247557B2
公开(公告)日：2012-08-21
申请号：US12096590
申请日：2006-12-19
申请人： Michael F. T. Koehler , Lewis Gazzard , Vickie Hsiao-Wei Tsui
发明人： Michael F. T. Koehler , Lewis Gazzard , Vickie Hsiao-Wei Tsui
IPC分类号： C07D513/02 , A01N43/42
CPC分类号： C07D403/04 , C07D417/04 , C07D417/14 , C07D513/04
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3′, R4, R4′, R5, R6, R6′ and n are as described herein.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有通式（I）：其中Q，X1，X2，Y，Z1，Z2，Z3，Z4，R1，R2，R3， R3'，R4，R4'，R5，R6，R6'和n如本文所述。

7. 发明授权

US08063218B2 Imidazopyridine inhibitors of IAP 有权
标题翻译： IAP的咪唑并吡啶抑制剂
公开(公告)号：US08063218B2
公开(公告)日：2011-11-22
申请号：US12520205
申请日：2007-12-14
申请人： Michael F. T. Koehler
发明人： Michael F. T. Koehler
IPC分类号： C07D491/02
CPC分类号： C07D471/04
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein Q, X1, X2, Y, Z R1, R2, R3, R3′, R4, R4′, R5, R6, R6′ and n are as described herein.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有通式I：其中Q，X1，X2，Y，Z R1，R2，R3，R3'，R4，R4'，R5 ，R6，R6'和n如本文所述。

8. 发明授权

US09278961B2 Pyridyl inhibitors of hedgehog signalling 有权
公开(公告)号：US09278961B2
公开(公告)日：2016-03-08
申请号：US12960609
申请日：2010-12-06
申请人： Janet L. Gunzner , Daniel Sutherlin , Mark S. Stanley , Liang Bao , Georgette M. Castanedo , Rebecca L. Lalonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina , Michael F. T. Koehler
发明人： Janet L. Gunzner , Daniel Sutherlin , Mark S. Stanley , Liang Bao , Georgette M. Castanedo , Rebecca L. Lalonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina , Michael F. T. Koehler
IPC分类号： C07D213/38 , C07D417/12 , C07D401/14 , A61K31/44 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07F9/58
CPC分类号： C07D213/16 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/58
摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

9. 发明授权

US08163763B2 Pyrimidine compounds, compositions and methods of use 有权
标题翻译：嘧啶化合物，组合物和使用方法
公开(公告)号：US08163763B2
公开(公告)日：2012-04-24
申请号：US12533935
申请日：2009-07-31
申请人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F. T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
发明人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F. T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
IPC分类号： A61K31/519 , C07D471/04
CPC分类号： C07D471/18 , C07D471/14
摘要： Disclosed are compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
摘要翻译：公开了式I化合物，其包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，其可用于调节PIKK相关激酶信号传导，例如mTOR和用于治疗疾病（例如癌症），至少部分地由PIKK信号通路的失调（例如mTOR）介导。

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