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11. 发明授权

US5250548A Angiotensin II receptor antagonists 失效
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：US5250548A
公开(公告)日：1993-10-05
申请号：US844351
申请日：1992-03-02
申请人： Martin Winn , Biswanath De , Thomas M. Zydowsky , Daniel J. Kerkman , John F. DeBernardis , Saul H. Rosenberg , Kazumi Shiosaki , Fatima Z. Basha , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Steven Boyd , Diane M. Yamamoto , Anthony K. L. Fung
发明人： Martin Winn , Biswanath De , Thomas M. Zydowsky , Daniel J. Kerkman , John F. DeBernardis , Saul H. Rosenberg , Kazumi Shiosaki , Fatima Z. Basha , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Steven Boyd , Diane M. Yamamoto , Anthony K. L. Fung
IPC分类号： C07D239/42 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/14 , A61K31/44
CPC分类号： C07D239/42 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/14
摘要： Compounds are disclosed having the formula: ##STR1## The compounds of the invention are angiotensin II receptor antagonists.
摘要翻译：公开了具有下式的化合物：本发明的化合物是血管紧张素II受体拮抗剂。

12. 发明授权

US06831175B2 Kinase inhibitors 有权
标题翻译：激酶抑制剂
公开(公告)号：US06831175B2
公开(公告)日：2004-12-14
申请号：US10317914
申请日：2002-12-12
申请人： Qun Li , Keith W. Woods , Gui-Dong Zhu , John P. Fischer , Jianchun Gong , Tongmei Li , Virajkumar Gandhi , Sheela A. Thomas , Garrick K. Packard , Xiaohong Song , Jason N. Abrams , Robert B. Diebold , Jürgen Dinges , Charles W. Hutchins , Vincent S. Stoll , Saul H. Rosenberg , Vincent L. Giranda
发明人： Qun Li , Keith W. Woods , Gui-Dong Zhu , John P. Fischer , Jianchun Gong , Tongmei Li , Virajkumar Gandhi , Sheela A. Thomas , Garrick K. Packard , Xiaohong Song , Jason N. Abrams , Robert B. Diebold , Jürgen Dinges , Charles W. Hutchins , Vincent S. Stoll , Saul H. Rosenberg , Vincent L. Giranda
IPC分类号： C07D21136
CPC分类号： C07D401/04 , C07D213/63 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/14 , C07D471/04 , C07D475/02
摘要： Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
摘要翻译：具有该化学式的化合物可用于抑制蛋白激酶。还公开了抑制蛋白激酶的组合物和抑制患者蛋白激酶的方法。

13. 发明授权

US5332742A Renin inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US5332742A
公开(公告)日：1994-07-26
申请号：US147208
申请日：1993-11-03
申请人： Saul H. Rosenberg
发明人： Saul H. Rosenberg
IPC分类号： A61K38/00 , C07D277/28 , C07D295/26 , C07K5/065 , A61K31/495 , A61K37/00 , C07D417/00
CPC分类号： C07D295/26 , C07D277/28 , C07K5/06078 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1## wherein R.sub.1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-l-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl;R.sub.2 is benzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;R.sub.3 is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH.sub.3 S-- or CH.sub.3 SCH.sub.2 --;R.sub.4 is isobutyl or cyclopropyl;R.sub.5 is hydrogen or loweralkyl; andX is CH.sub.2 or NH; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that when X is NH and R.sub.3 is 2-amino-4-thiazolyl, then R.sub.4 is cyclopropyl.
摘要翻译：其中R1是4-哌嗪基，1-甲基-4-哌嗪基，1-甲基-1-氧代-4-哌嗪基，2-氧代-4-哌嗪基，4-吗啉基，4-吗啉基， 4-硫代吗啉基或1-甲基-4-高哌嗪基; R2是苄基，2-苯基乙基，1-萘基甲基或2-萘基甲基; R3是4-噻唑基，2-氨基-4-噻唑基，2-噻唑基，5-噻唑基，1-吡唑基，3-吡唑基，1-咪唑基，正丙基，异丙基，CH3S-或CH3SCH2-; R4是异丁基或环丙基; R5是氢或低级烷基; X为CH 2或NH; 或其药学上可接受的盐，酯或前药; 条件是当X是NH且R3是2-氨基-4-噻唑基时，则R4是环丙基。

14. 发明授权

US5268374A Non-peptide renin inhibitors 失效
标题翻译：非肽肾素抑制剂
公开(公告)号：US5268374A
公开(公告)日：1993-12-07
申请号：US700185
申请日：1991-05-22
申请人： Anthony K. L. Fung , William R. Baker , Yoek-Lin Armiger , Saul H. Rosenberg , Biswanath De , Jacob J. Plattner , Steven A. Boyd , Dale J. Kempf , Hing L. Sham , Hollis D. Kleinert , Robert A. Mantei
发明人： Anthony K. L. Fung , William R. Baker , Yoek-Lin Armiger , Saul H. Rosenberg , Biswanath De , Jacob J. Plattner , Steven A. Boyd , Dale J. Kempf , Hing L. Sham , Hollis D. Kleinert , Robert A. Mantei
IPC分类号： C07C237/08 , C07C317/28 , C07C323/58 , C07D203/18 , C07D211/44 , C07D211/62 , C07D211/96 , C07D233/54 , C07D295/185 , C07D401/12 , C07D407/12 , C07D413/12 , A61K37/43 , C07K5/08
CPC分类号： C07D233/64 , C07C237/08 , C07C317/28 , C07C323/58 , C07D203/18 , C07D211/44 , C07D211/62 , C07D211/96 , C07D295/185 , C07D401/12 , C07D407/12 , C07D413/10 , C07C2101/14
摘要： The present invention relates to renin inhibiting compounds of the formula: ##STR1##
摘要翻译：本发明涉及下式的肾素抑制化合物：

15. 发明授权

US5258362A Renin inhibiting compounds 失效
标题翻译：肾素抑制化合物
公开(公告)号：US5258362A
公开(公告)日：1993-11-02
申请号：US880250
申请日：1992-05-13
申请人： Saul H. Rosenberg
发明人： Saul H. Rosenberg
IPC分类号： A61K38/00 , C07D205/04 , C07D263/06 , C07D277/30 , C07D303/36 , C07D305/06 , C07D405/12 , C07D407/04 , C07D417/12 , C07D417/14 , C07D487/04 , C07D521/00 , C07H15/14 , C07K5/06 , C07K5/065 , C07K5/078 , C07K9/00 , A21K37/00 , C07K5/08
CPC分类号： C07D231/12 , C07D205/04 , C07D233/56 , C07D249/08 , C07D263/06 , C07D277/30 , C07D303/36 , C07D305/06 , C07D405/12 , C07D407/04 , C07D417/12 , C07D417/14 , C07D487/04 , C07H15/14 , C07K5/06026 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K9/001 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1## wherein R.sub.0 is a mimic of the Phe-His dipeptide sequence of angiotensinogen which preceeds the renin cleavage site;R.sub.4 is loweralkyl, cycloalkylalkyl or arylalkyl;R.sub.5 is hydrogen, loweralkyl, hydroxyalkyl, loweralkenyl or formyl;R.sub.6 is --OH or --NH.sub.2 ; andD is ##STR2## wherein R.sub.7 is hydrogen or loweralkyl and R.sub.8 is hydrogen, loweralkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, cycloalkylalkyl, loweralkenyl, alkynyl, aryl, arylalkyl, heterocyclic or heterocyclicalkyl; or R.sub.7 and R.sub.8 taken together --(CH.sub.2).sub.n -- wherein n is 3-6; and R.sub.9 is loweralkyl; or a pharmaceutically acceptable salt, ester or prodrug thereof.
摘要翻译：一种下列化学式的肾素抑制化合物：其中R0是血管紧张素原的Phe-His二肽序列的模拟物，其中血管紧张素原来源于肾素切割位点; R4是低级烷基，环烷基烷基或芳基烷基; R5是氢，低级烷基，羟烷基，低级烯基或甲酰基; R6是-OH或-NH2; 并且D是其中R 7是氢或低级烷基，且R 8是氢，低级烷基，羟基烷基，烷氧基烷基，硫代烷氧基烷基，卤代烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，环烷基，环烷基烷基，低级烯基，炔基，芳基，芳基烷基，杂环或杂环烷基。或者R 7和R 8一起形成 - （CH 2）n - ，其中n是3-6; 且R 9为低级烷基; 或其药学上可接受的盐，酯或前药。

16. 发明申请

US20100028889A1 COMPANION DIAGNOSTIC ASSAYS FOR CANCER THERAPY 审中-公开
标题翻译：用于癌症治疗的组合诊断测定
公开(公告)号：US20100028889A1
公开(公告)日：2010-02-04
申请号：US12490558
申请日：2009-06-24
申请人： Mark G. Anderson , Paul E. Kroeger , Saul H. Rosenberg , Stephen K. Tahir , John A. Wass , Christin Tse , Viswanath Devanarayan
发明人： Mark G. Anderson , Paul E. Kroeger , Saul H. Rosenberg , Stephen K. Tahir , John A. Wass , Christin Tse , Viswanath Devanarayan
IPC分类号： C12Q1/68 , G06F7/00
CPC分类号： C12Q1/6886 , C12Q2600/106
摘要： Methods for identifying cancer patients eligible to receive Bcl-2 family inhibitor therapy and for monitoring patient response to Bcl-2 family inhibitor therapy comprise assessment of the expression levels of the biomarker combinations set out in TABLES 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20 in a patient tissue sample. The methods of the invention allow more effective identification of patients to receive Bcl-2 family inhibitor therapy and of determination of patient response to the therapy.
摘要翻译：鉴定符合接受Bcl-2家族抑制剂治疗和监测患者对Bcl-2家族抑制剂治疗的反应的癌症患者的方法包括评估表1，2，3，4，5， 6，7，8，9，10，11，12，13，14，15，16，17，18，19或20。本发明的方法允许更有效地鉴定患者以接受Bcl-2家族抑制剂治疗和确定患者对治疗的反应。

17. 发明授权

US5326776A Angiotensin II receptor antagonists 失效
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：US5326776A
公开(公告)日：1994-07-05
申请号：US21839
申请日：1993-02-24
申请人： Martin Winn , Biswanath De , Thomas M. Zydowsky , Daniel J. Kerkman , John F. DeBernardis , Saul H. Rosenberg , Kazumi Shiosaki , Fatima Z. Basha , Kenneth P. Spina , Thomas W. von Geldern , Steven Boyd , Diane M. Yamamoto , Anthony K. L. Fung
发明人： Martin Winn , Biswanath De , Thomas M. Zydowsky , Daniel J. Kerkman , John F. DeBernardis , Saul H. Rosenberg , Kazumi Shiosaki , Fatima Z. Basha , Kenneth P. Spina , Thomas W. von Geldern , Steven Boyd , Diane M. Yamamoto , Anthony K. L. Fung
IPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , A61K31/41 , A61K31/415 , C07D403/10
CPC分类号： C07D403/12 , C07D413/10 , C07D417/12
摘要： Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.
摘要翻译：公开了具有下式的化合物：其中取代基在本文中定义。本发明的化合物是血管紧张素II受体拮抗剂。

18. 发明授权

US5310740A Renin inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US5310740A
公开(公告)日：1994-05-10
申请号：US901368
申请日：1992-06-19
申请人： Saul H. Rosenberg , Jon F. Denissen
发明人： Saul H. Rosenberg , Jon F. Denissen
IPC分类号： A61K31/415 , A61K31/425 , A61K31/426 , A61K31/495 , A61K31/54 , A61K31/55 , A61K38/00 , A61P3/08 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P31/12 , A61P43/00 , C07D231/12 , C07D241/04 , C07D277/22 , C07D277/28 , C07D277/40 , C07D279/12 , C07D295/08 , C07D295/26 , C07D403/12 , C07D413/12 , C07D417/12 , C07K1/113 , C07K5/06 , C07K5/065 , C07K14/81 , A61K31/535 , C07D237/30 , C07D413/00
CPC分类号： C07D295/26 , C07D277/28 , C07K5/06078 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1##wherein R.sub.1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl;R.sub.2 is benzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;R.sub.3 is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH.sub.3 S-- or CH.sub.3 SCH.sub.2 --;R.sub.4 is isobutyl or cyclopropyl;R.sub.5 is hydrogen or loweralkyl; andX is CH.sub.2 or NH; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that when X is NH and R.sub.3 is 2-amino-4-thiazolyl, then R.sub.4 is cyclopropyl.
摘要翻译：其中R1是4-哌嗪基，1-甲基-4-哌嗪基，1-甲基-1-氧代-4-哌嗪基，2-氧代-4-哌嗪基，4-吗啉基，4-吗啉基， 4-硫代吗啉基或1-甲基-4-高哌嗪基; R2是苄基，2-苯基乙基，1-萘基甲基或2-萘基甲基; R3是4-噻唑基，2-氨基-4-噻唑基，2-噻唑基，5-噻唑基，1-吡唑基，3-吡唑基，1-咪唑基，正丙基，异丙基，CH3S-或CH3SCH2-; R4是异丁基或环丙基; R5是氢或低级烷基; X为CH 2或NH; 或其药学上可接受的盐，酯或前药; 条件是当X是NH且R3是2-氨基-4-噻唑基时，则R4是环丙基。

19. 发明授权

US5164388A Heterocyclic peptide renin inhibitors 失效
标题翻译：杂环肽肾素抑制剂
公开(公告)号：US5164388A
公开(公告)日：1992-11-17
申请号：US678266
申请日：1991-04-18
申请人： Biswanath De , Thomas N. Zydowsky , William R. Baker , Joseph F. Dellaria , Saul H. Rosenberg , Hwan S. Jae
发明人： Biswanath De , Thomas N. Zydowsky , William R. Baker , Joseph F. Dellaria , Saul H. Rosenberg , Hwan S. Jae
IPC分类号： A61K38/00 , C07D211/14 , C07D211/76 , C07D213/74 , C07D233/54 , C07D239/42 , C07D241/04 , C07D241/08 , C07D243/08 , C07D263/10 , C07D263/22 , C07D295/15 , C07D403/06 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/06 , C07K5/078
CPC分类号： C07D233/64 , C07D211/14 , C07D211/76 , C07D213/74 , C07D239/42 , C07D241/04 , C07D241/08 , C07D243/08 , C07D263/10 , C07D263/22 , C07D295/15 , C07D403/06 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/06 , C07K5/06139 , A61K38/00 , C07C2101/14
摘要： A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.
摘要翻译：其中X是N，O或CH的式（Ⅰ）的肾素抑制化合物; R1不存在或官能团; A和L独立地选自C = O，SO 2和CH 2; D是C = O，SO 2或CH 2; Y为N或CH; R2是氢，低级烷基或取代的烷基; Z是功能组; R3是低级烷基或取代的烷基; n为0或1; T是模拟血管紧张素原的Leu-Val切割位点; 或其药学上可接受的盐，酯或前药。

20. 发明授权

US4857507A Angiotensinogen analogs 失效
公开(公告)号：US4857507A
公开(公告)日：1989-08-15
申请号：US946883
申请日：1987-01-09
申请人： Saul H. Rosenberg , Joseph Dellaria , Anthony K, L. Fung , Dale J. Kempf , Jay R. Luly , Jacob J. Plattner
发明人： Saul H. Rosenberg , Joseph Dellaria , Anthony K, L. Fung , Dale J. Kempf , Jay R. Luly , Jacob J. Plattner
IPC分类号： A61K38/00 , C07D207/12 , C07D231/12 , C07D233/54 , C07D263/20 , C07D295/185 , C07D317/28 , C07D319/06 , C07D339/06 , C07D339/08 , C07D405/06 , C07D409/06 , C07K5/02 , C07K5/065
CPC分类号： C07D231/12 , C07D207/12 , C07D233/64 , C07D263/20 , C07D295/185 , C07D317/28 , C07D319/06 , C07D339/06 , C07D339/08 , C07D405/06 , C07D409/06 , C07K5/02 , C07K5/0227 , C07K5/06078 , A61K38/00 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.10 or SR.sub.10 wherein R.sub.10 is hydrogen, loweralkyl or aminoalkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.13 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, aminoalkyl, alkoxycarbonylalkyl, carboxyalkyl, N-protected aminoalkyl, alkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, dialkylaminoalkyl, (heterocyclic) alkyl or a substituted or unsubstituted heterocyclic; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloaklylmethyl, benzyl, .alpha.,.alpha.-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)-methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R.sub.1 is phenoxy, thiophenoxy or anilino, B is CH.sub.2 or CHOH or A is hydrogen, R.sub.3 is loweralkyl, vinylloweralkyl, benzyl or heterocyclic ring substituted methyl, R.sub.5 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.2 and R.sub.4 are independently selected from hydrogen and loweralkyl; R.sub.6 is CHOH or CO; R.sub.7 is CH.sub.2, CF.sub.2 or CF with the proviso that when R.sub.6 is CO, R.sub.7 is CF.sub.2 ; R.sub.8 is CH.sub.2, CHR.sub.14 wherein R.sub.14 is lower-alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or R.sub.7 and R.sub.8 taken together can be ##STR3## with the proviso that when R.sub.7 is CF.sub.2, R.sub.8 is CH.sub.2 ; E is O, S, SO, SO.sub.2, NR.sub.15 wherein R.sub.15 is hydrogen or loweralkyl or NR.sub.16 CO wherein R.sub.16 is hydrogen or loweralkyl; R.sub.9 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protected group, or E and R.sub.9 taken together can be N.sub.3, with the proviso that when E is NH, R.sub.9 is an N-protecting group; and pharmaceutically acceptable salts thereof.

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