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1. 发明授权

US11766433B2 Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer 有权
公开(公告)号：US11766433B2
公开(公告)日：2023-09-26
申请号：US17089519
申请日：2020-11-04
申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education
发明人： Peter Wipf , James K. Johnson , Erin M. Skoda , Joel B. Nelson , Zhou Wang , Serene Tai , Keita Takubo , John Milligan
IPC分类号： A61K31/495 , A61K31/504 , A61K31/4985 , A61K31/497 , A61K31/4439 , A61K31/401 , A61K31/407 , A61K31/122 , A61K31/47 , A61K9/00 , A61P35/00 , A61K31/167 , A61K31/4166 , A61K31/58
CPC分类号： A61K31/504 , A61K9/0053 , A61K31/122 , A61K31/167 , A61K31/401 , A61K31/407 , A61K31/4439 , A61K31/47 , A61K31/497 , A61K31/4985 , A61P35/00 , A61K31/4166 , A61K31/58 , A61K2300/00
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I:

R20—(Z)b—(Y)c—(R21)a—(X)d—R22—R23

wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.

2. 发明申请

US20210061779A1 COMPOUNDS FOR TREATING PROSTATE CANCER 有权
公开(公告)号：US20210061779A1
公开(公告)日：2021-03-04
申请号：US17095653
申请日：2020-11-11
申请人： University of Pittsburgh - of the Commonwealth System of Higher Education
发明人： Peter Wipf , Erin M. Skoda , Zhou Wang
IPC分类号： C07D295/192 , A61K31/495 , A61K31/496 , A61K31/551 , A61K31/58 , A61K31/4525 , A61K45/06 , C07D213/70 , C07D261/08 , C07D295/26 , C07D317/54 , C07D333/16 , C07D413/12
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: R20—(Z)b—(Y)c—(R21)a—X—R22—R23 wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)— or —S(═O)(═O)—; R22 is a moiety that includes at least one divalent amino radical; R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; a is 0 or 1; b is 0 or 1; and c is 0 or 1; provided that if X is —C(═O)— then Y is not S.

3. 发明授权

US10882834B2 Compounds for treating prostate cancer 有权
公开(公告)号：US10882834B2
公开(公告)日：2021-01-05
申请号：US15023349
申请日：2014-09-18
申请人： University of Pittsburgh—of the Commonwealth System of Higher Education
发明人： Peter Wipf , Erin M. Skoda , Zhou Wang
IPC分类号： A61K31/495 , C07D295/185 , C07D295/192 , A61K45/06 , C07D295/26 , C07D213/70 , C07D333/16 , C07D261/08 , C07D317/54 , C07D413/12 , A61K31/4525 , A61K31/551 , A61K31/58 , A61K31/496
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: R20—(Z)b—(Y)c—(R21)a—X—R22—R23 wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(=0)- or —S(=0)(=0)-; R22 is a moiety that includes at least one divalent amino radical; R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; a is 0 or 1; b is 0 or 1; and c is 0 or 1; provided that if X is —C(=0)- then Y is not S.

4. 发明授权

US10544110B2 Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer 有权
公开(公告)号：US10544110B2
公开(公告)日：2020-01-28
申请号：US15961475
申请日：2018-04-24
申请人： University of Pittsburgh-Of the Commonwealth System of Higher Education
发明人： Peter Wipf , James K. Johnson , Erin M. Skoda , Joel B. Nelson , Zhou Wang
IPC分类号： C07D261/08 , C07D451/00 , C07D413/12 , A61K31/454 , C07D295/185 , A61K31/495 , A61K31/496 , A61K31/42 , A61K31/46 , A61K31/4166 , A61K45/06 , A61K31/58
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: R20—(Z)b—(Y)c—(R21)a—(X)d—R22—R23 wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.

5. 发明申请

US20160264540A1 COMPOUNDS FOR TREATING PROSTATE CANCER 审中-公开
标题翻译：用于治疗前列腺癌的化合物
公开(公告)号：US20160264540A1
公开(公告)日：2016-09-15
申请号：US15023349
申请日：2014-09-18
申请人： UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
发明人： Peter Wipf , Erin M. Skoda , Zhou Wang
IPC分类号： C07D295/192 , A61K45/06 , A61K31/495 , C07D295/26 , C07D213/70 , C07D333/16 , C07D261/08 , C07D317/54 , C07D413/12 , A61K31/4525 , A61K31/551 , A61K31/58 , A61K31/496
CPC分类号： C07D295/192 , A61K31/4525 , A61K31/495 , A61K31/496 , A61K31/551 , A61K31/58 , A61K45/06 , C07D213/70 , C07D261/08 , C07D295/26 , C07D317/54 , C07D333/16 , C07D413/12 , A61K2300/00
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: R20—(Z)b—(Y)c—(R21)a—X—R22-R23 wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(=0)- or —S(=0)(=0)-; R22 is a moiety that includes at least one divalent amino radical; R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; a is 0 or 1; b is 0 or 1; and c is 0 or 1; provided that if X is —C(=0)- then Y is not S.
摘要翻译：具有式I的化合物或其药学上可接受的盐或酯：R20-（Z）b-（Y）c-（R21）a-X-R22-R23，其中R20是芳基，取代的芳基，杂芳基，取代的杂芳基，杂环烷基，取代的杂环烷基，烷氧基，芳氧基，含甲硅烷基的基团，含硼基的基团，含膦基团，氨基，含硫基团，含硒基团，卤化物或硝基包含组; Z是烷二基，取代的烷二基，环烷二基或取代的环烷二基; Y是S，O或NR10，其中R10是H或烷基; R21是烷二基，取代的烷二基，环烷二基，取代的环烷二基，链二烯基，取代的链二烯基，亚三链烯基，取代的链三烯基; X是-C（= O） - 或-S（= O）（= O） - ; R 22是包含至少一个二价氨基的部分; R 23是芳基，取代的芳基，杂芳基，取代的杂芳基，杂环烷基，取代的杂环烷基，烷氧基，芳氧基，含甲硅烷基的基团，含硼基的基团，含膦基团，氨基，含硫基团，含卤基，卤素或硝基的基团; a是0或1; b为0或1; 且c为0或1; 条件是如果X是-C（= 0） - 则Y不是S.

6. 发明申请

US20190022093A1 SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER 审中-公开
公开(公告)号：US20190022093A1
公开(公告)日：2019-01-24
申请号：US16139950
申请日：2018-09-24
申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education
发明人： Peter Wipf , James K. Johnson , Erin M. Skoda , Joel B. Nelson , Zhou Wang , Serene Tai , Keita Takubo , John Milligan
IPC分类号： A61K31/504 , A61K31/4985 , A61K31/497 , A61K31/4439 , A61K31/401 , A61K31/407 , A61K31/167 , A61K31/122 , A61K31/47 , A61K9/00 , A61P35/00
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: R20-(Z)b-(Y)c—(R21)a—(X)d—R22—R23 wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.

7. 发明申请

US20160257657A1 SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER 审中-公开
标题翻译：用于治疗耐药性前列腺癌的雄激素受体的核转录因子的小分子抑制剂
公开(公告)号：US20160257657A1
公开(公告)日：2016-09-08
申请号：US15080237
申请日：2016-03-24
申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education
发明人： Peter Wipf , James K. Johnson , Erin M. Skoda , Joel B. Nelson , Zhou Wang
IPC分类号： C07D261/08 , A61K31/4166 , A61K31/42 , A61K31/496 , A61K31/46 , A61K31/495 , C07D413/12 , A61K31/454 , C07D451/00 , A61K31/58 , C07D295/185
CPC分类号： C07D261/08 , A61K31/4166 , A61K31/42 , A61K31/454 , A61K31/46 , A61K31/495 , A61K31/496 , A61K31/58 , A61K45/06 , C07D295/185 , C07D413/12 , C07D451/00 , A61K2300/00
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: R20—(Z)b—(Y)c—(R21)a—(X)d—R22—R23 wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.
摘要翻译：根据式I的化合物或其药学上可接受的盐或酯：R 20 - （Z）b - （Y）c - （R 21）a - （X）d -R 22 -R 23，其中R 20是芳基，取代的芳基，杂芳基，取代的杂芳基，杂环烷基，取代的杂环烷基，烷氧基，芳氧基，含硫基团或含硒基团; Z是烷二基，取代的烷二基，环烷二基或取代的环烷二基; Y是S，O，S（= O），-S（= O）（= O） - 或NR 10，其中R 10是H或烷基; R21是烷二基，取代的烷二基，环烷二基，取代的环烷二基亚二烯基，取代的链二烯基，亚烷基三烯基，取代的链三烯基; X是-C（= O） - ， - S（= O）（= O） - 或-N（H）C（= O） - ; R22包括至少一个二价氨基; R 23是芳基，取代的芳基，杂芳基，取代的杂芳基，杂环烷基，取代的杂环烷基，烷氧基，芳氧基，含硫基团或含硒基团; a，b，c和d独立地为0或1。

8. 发明申请

US20210186963A1 SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER 有权
公开(公告)号：US20210186963A1
公开(公告)日：2021-06-24
申请号：US17089519
申请日：2020-11-04
申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education
发明人： Peter Wipf , James K. Johnson , Erin M. Skoda , Joel B. Nelson , Zhou Wang , Serene Tai , Keita Takubo , John Milligan
IPC分类号： A61K31/504 , A61K31/4985 , A61K31/497 , A61K31/4439 , A61K31/401 , A61K31/407 , A61K31/122 , A61K31/47 , A61K9/00 , A61P35/00 , A61K31/167
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: R20—(Z)b—(Y)c—(R21)a—(X)d—R22—R23 wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.

9. 发明授权

US10906876B2 Tetrahydroisoquinolines as selective NADPH oxidase 2 inhibitors 有权
公开(公告)号：US10906876B2
公开(公告)日：2021-02-02
申请号：US16444824
申请日：2019-06-18
申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education
发明人： Patrick Joseph Pagano , Peter Wipf , Maria Eugenia Cifuentes-Pagano , Erin M. Skoda
IPC分类号： C07D221/22 , C07D453/06 , A61K31/4748 , A61K45/06 , C07D401/06 , C07D405/10 , C07D409/06 , C07D413/06
摘要： Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof: wherein “” represents a single or double bond, R1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Ra is hydrogen, —CH2R2, R3, or —SO2R4; R2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R4 is lower aliphatic, or substituted or unsubstituted aryl; and R5 is hydrogen, halogen, or lower aliphatic.

10. 发明申请

US20180237403A1 SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER 审中-公开
公开(公告)号：US20180237403A1
公开(公告)日：2018-08-23
申请号：US15961475
申请日：2018-04-24
申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education
发明人： Peter Wipf , James K. Johnson , Erin M. Skoda , Joel B. Nelson , Zhou Wang
IPC分类号： C07D261/08 , C07D451/00 , C07D413/12 , A61K31/454 , A61K31/4166 , C07D295/185 , A61K45/06 , A61K31/495 , A61K31/496 , A61K31/42 , A61K31/58 , A61K31/46
CPC分类号： C07D261/08 , A61K31/4166 , A61K31/42 , A61K31/454 , A61K31/46 , A61K31/495 , A61K31/496 , A61K31/58 , A61K45/06 , C07D295/185 , C07D413/12 , C07D451/00 , A61K2300/00
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: R20—(Z)b—(Y)c—(R21)a—(X)d—R22—R23 wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.

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