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公开(公告)号：EP4371982A3
公开(公告)日：2024-08-21
申请号：EP24161427.0
申请日：2018-02-22
发明人： SMITH, Peter Andrew , ROBERTS, Tucker Curran , HIGUCHI, Robert I. , PARASELLI, Prasuna , KOEHLER, Michael F. T. , SCHWARZ, Jacob Bradley , CRAWFORD, James John , LY, Cuong Q. , HANAN, Emily J. , HU, Huiyong , CHEN, Yongsheng , YU, Zhiyong , WINSHIP, Paul Colin Michael , McCLEOD, Calum , BLENCH, Toby
IPC分类号： A61K31/395 , A61P31/04 , C07D403/12 , C07D245/04 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D491/08
CPC分类号： C07D245/04 , A61P31/04 , C07D403/12 , C07D401/14 , C07D405/14 , C07D491/08 , C07D401/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D471/04 , Y02A50/30
摘要： Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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公开(公告)号：EP4371982A2
公开(公告)日：2024-05-22
申请号：EP24161427.0
申请日：2018-02-22
发明人： SMITH, Peter Andrew , ROBERTS, Tucker Curran , HIGUCHI, Robert I. , PARASELLI, Prasuna , KOEHLER, Michael F. T. , SCHWARZ, Jacob Bradley , CRAWFORD, James John , LY, Cuong Q. , HANAN, Emily J. , HU, Huiyong , CHEN, Yongsheng , YU, Zhiyong , WINSHIP, Paul Colin Michael , McCLEOD, Calum , BLENCH, Toby
IPC分类号： C07D401/12
CPC分类号： C07D245/04 , A61P31/04 , C07D403/12 , C07D401/14 , C07D405/14 , C07D491/08 , C07D401/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D471/04 , Y02A50/30
摘要： Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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公开(公告)号：EP3377473A1
公开(公告)日：2018-09-26
申请号：EP16840309.5
申请日：2016-11-21
发明人： CHEN, Yongsheng , SMITH, Peter Andrew , ROBERTS, Tucker Curran , HIGUCHI, Robert I. , PARASELLI, Prasuna , KOEHLER, Michael F. T. , SCHWARZ, Jacob Bradley , CRAWFORD, James John , LY, Cuong Q. , HANAN, Emily J. , HU, Huiyong , YU, Zhiyong
IPC分类号： C07D245/04 , A61K31/395 , A61P31/04
CPC分类号： C07D245/04 , A61K9/0014 , A61K31/395 , A61K31/407 , A61K31/4196 , A61K31/43 , A61K31/431 , A61K31/496 , A61K31/545 , A61K31/546 , A61K38/06 , A61K38/07 , A61K38/08 , A61K45/06 , A61K2300/00 , A61P31/04 , C07K5/0202 , C07K5/0812 , C07K5/0815 , C07K5/1008 , C07K5/1013 , C07K5/1019 , C07K5/1021 , C07K5/1024 , C07K7/06 , C07K7/08 , C07K9/008 , Y02A50/401 , Y02A50/404 , Y02A50/406 , Y02A50/47 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/483
摘要： Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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公开(公告)号：EP3377474A1
公开(公告)日：2018-09-26
申请号：EP16843251.6
申请日：2016-11-21
发明人： CHEN, Yongsheng , SMITH, Peter Andrew , ROBERTS, Tucker Curran , HIGUCHI, Robert I. , PARASELLI, Prasuna , KOEHLER, Michael F. T. , SCHWARZ, Jacob Bradley , CRAWFORD, James John , LY, Cuong Q. , HU, Huiyong , YU, Zhiyong
IPC分类号： C07D245/04 , A61K31/395 , A61P31/04
CPC分类号： C07D245/04 , A61K45/06
摘要： Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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公开(公告)号：EP1745041B1
公开(公告)日：2012-06-20
申请号：EP05856681.1
申请日：2005-04-29
申请人： Genentech, Inc. , Curis, Inc.
IPC分类号： C07D403/12 , C07D241/42 , C07D409/12 , C07D413/12 , C07D401/12 , C07D405/12 , C07D403/04 , C07D401/14 , A61K31/498 , A61P35/00
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 hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R2 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R3 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; m is 0-3; n is 0-3; and salts and solvates thereof.
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公开(公告)号：EP1745041A2
公开(公告)日：2007-01-24
申请号：EP05856681.1
申请日：2005-04-29
申请人： Genentech, Inc.
IPC分类号： C07D403/12 , C07D241/42 , C07D409/12 , C07D413/12 , C07D401/12 , C07D405/12 , C07D403/04 , C07D401/14 , A61K31/498 , A61P35/00
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 hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R2 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R3 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; m is 0-3; n is 0-3; and salts and solvates thereof.
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7.发明授权
公开(公告)号：EP1789390B1
公开(公告)日：2011-11-09
申请号：EP05795325.9
申请日：2005-09-02
申请人： Genentech, Inc. , Curis, Inc.
发明人： GUNZNER, Janet , SUTHERLIN, Daniel , STANLEY, Mark , BAO, Liang , CASTANEDO, Georgette , LALONDE, Rebecca , WANG, Shumei , REYNOLDS, Mark , SAVAGE, Scott , MALESKY, Kimberly , DINA, Michael , KOEHLER, Michael F. T.
IPC分类号： C07D213/40 , C07D213/82 , C07D409/12 , C07D413/12 , C07D401/14 , C07D417/04 , C07D417/12 , C07D213/56 , C07D213/38 , C07D213/75 , C07D401/12 , C07D405/12 , C07D213/81 , C07D213/70 , C07F9/142 , A61K31/4418 , A61K31/4427 , A61P35/00
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 , C07F9/588
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, and n are as described herein.
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公开(公告)号：EP2148858A1
公开(公告)日：2010-02-03
申请号：EP08747109.0
申请日：2008-04-29
申请人： Genentech, Inc.
发明人： FLYGARE, John A. , COHEN, Frederick , DESHAYES, Kurt , KOEHLER, Michael F. T. , GAZZARD, Lewis J. , WANG, Lan , NDUBAKU, Chudi
IPC分类号： C07D209/02 , C07D263/06 , C07D513/04
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.
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公开(公告)号：EP1973899A2
公开(公告)日：2008-10-01
申请号：EP06850324.2
申请日：2006-12-19
申请人： Genentech, Inc.
IPC分类号： C07D403/04
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.
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