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1. 发明公开

EP1255752A2 PYRROLE SUBSTITUTED 2-INDOLINONE PROTEIN KINASE INHIBITORS 有权转让
标题翻译：吡咯取代的吲哚啉-2- ON蛋白激酶抑制剂
公开(公告)号：EP1255752A2
公开(公告)日：2002-11-13
申请号：EP01914376.7
申请日：2001-02-15
申请人： Sugen, Inc. , PHARMACIA & UPJOHN COMPANY , Miller, Todd , Li, Xiaoyuan , Sun, Li , Wei, Chung Chen , Shirazian, Shahrzad , Liang, Congxin , Vojkovsky, Tomas , Nematalla, Asaad S. , Tang, Peng Cho
发明人： TANG, Peng, Cho , MILLER, Todd , LI, Xiaoyuan , SUN, Li , WEI, Chung, Chen , SHIRAZIAN, Shahrzad , LIANG, Congxin , VOJKOVSKY, Tomas , NEMATALLA, Asaad, S. , HAWLEY, Michael
IPC分类号： C07D403/06 , A61K31/404 , A61P43/00 , C07D403/14 , C07D401/14
CPC分类号： C07D233/56 , C07D207/33 , C07D209/44 , C07D231/12 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14
摘要： The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

2. 发明专利

AU3977001A Pyrrole substituted 2-indolinone protein kinase inhibitors 未知
公开(公告)号：AU3977001A
公开(公告)日：2001-08-27
申请号：AU3977001
申请日：2001-02-15
申请人： SUGEN INC , TANG PENG CHO , MILLER TODD , LI XIAOYUAN , SUN LI , WEI CHUNG CHEN , SHIRAZIAN SHAHRZAD , LIANG CONGXIN , VOJKOVSKY TOMAS , ASAAD S NEMATALLA
发明人： TANG PENG CHO , MILLER TODD , LI XIAOYUAN , SUN LI , WEI CHUNG CHEN , SHIRAZIAN SHAHRZAD , LIANG CONGXIN , VOJKOVSKY TOMAS , NEMATALLA ASAAD S , HAWLEY MICHAEL
IPC分类号： C07D401/14 , A61K31/404 , A61K31/4178 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P3/10 , A61P9/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/32 , C07D207/33 , C07D209/44 , C07D401/12 , C07D403/00 , C07D403/06 , C07D403/12 , C07D403/14 , C07D521/00
摘要： The present invention relates to pyrrole substituted-2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

3. 发明申请

WO2005016875A2 GEOMETRICALLY RESTRICTED 3-CYCLOPENTYLIDENE-1,3-DIHYDROINDOL-2-ONES AS POTENT PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：几何限制性3-环丙基-1,3-二氢吲哚-2-酮作为蛋白激酶激酶抑制剂
公开(公告)号：WO2005016875A2
公开(公告)日：2005-02-24
申请号：PCT/US2004/022310
申请日：2004-08-05
申请人： SUGEN, INC. , ZHANG, Fang-Jie , CUI, Jingrong , WEI, Chung, Chen , TANG, Peng, Cho
发明人： ZHANG, Fang-Jie , CUI, Jingrong , WEI, Chung, Chen , TANG, Peng, Cho
IPC分类号： C07D
CPC分类号： C07D209/34 , C07D209/42 , C07D403/06 , C07D403/14 , C07D471/04
摘要： The present invention relates to certain sulfonamido-substituted geometrically restricted indolinones of the formula (I): wherein R 1 - R 12 and X are variables defined herein. The sulfonamido-substituted geometrically restricted indolinones of the preferred embodiments of the present invention modulate the activity of protein kinases ("PKs"). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
摘要翻译：本发明涉及式（I）的某些亚磺酰氨基取代的几何限制的二氢吲哚酮：其中R1-R12和X是本文定义的变量。本发明优选实施方案的亚磺酰氨基取代的几何限制性二氢吲哚酮调节蛋白激酶（“PKs”）的活性。因此，本发明的化合物可用于治疗与异常PK活性相关的疾病。还公开了包含这些化合物的药物组合物，利用包含这些化合物的药物组合物治疗疾病的方法及其制备方法。

4. 发明申请

WO2004093821A2 TREATMENT OF ANTHRAX INFECTION USING INHIBITORS OF LETHAL FACTOR PROTEASE ACTIVITY 审中-公开
标题翻译：使用抑制因子的因子蛋白酶活性治疗神经传染
公开(公告)号：WO2004093821A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/013737
申请日：2004-04-22
申请人： HAWAII BIOTECH, INC. , GOLDMAN, Mark, Evan , O'MALLEY, Sean , SIMO, Ondrej , NAGATA, Melissa , JIAO, Guan-Sheng , HEMSCHEIDT, Klaus, Thomas , TANG, Peng, Cho , CREGAR, Lynne
发明人： GOLDMAN, Mark, Evan , O'MALLEY, Sean , SIMO, Ondrej , NAGATA, Melissa , JIAO, Guan-Sheng , HEMSCHEIDT, Klaus, Thomas , TANG, Peng, Cho , CREGAR, Lynne
IPC分类号： A61K
CPC分类号： A61K31/70 , C07K7/06
摘要： Compounds containing spaced N and/or O, by virtue of their ability to inhibit the protease activity of lethal factor from B. anthracis, are useful in the prevention and treatment of anthrax toxicity. Libraries of these compounds are also useful as substrates for screening methods to identify LF inhibitors.
摘要翻译：含有间隔N和/或O的化合物由于能够抑制炭疽芽孢杆菌致死因子的蛋白酶活性而被用于预防和治疗炭疽毒性。这些化合物的文库也可用作鉴定LF抑制剂的筛选方法的底物。

5. 发明申请

WO2002066463A1 3-(4-AMIDOPYRROL-2-YLMETHLIDENE)-2-INDOLINONE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的3-（4-氨基吡咯-2-基）甲氧基] -2-吲哚啉酮衍生物
公开(公告)号：WO2002066463A1
公开(公告)日：2002-08-29
申请号：PCT/US2002/004407
申请日：2002-02-15
申请人： GUAN, Huiping , LIANG, Congxin , SUN, Li , TANG, Peng, Cho , WEI, Chung, Chen , MAURAGIS, Michael, A. , VOJKOVSKY, Tomas , JIN, Qingwu , HERRINTON, Paul, Matthew
发明人： GUAN, Huiping , LIANG, Congxin , SUN, Li , TANG, Peng, Cho , WEI, Chung, Chen , MAURAGIS, Michael, A. , VOJKOVSKY, Tomas , JIN, Qingwu , HERRINTON, Paul, Matthew
IPC分类号： C07D403/06
CPC分类号： C07D403/06 , C07D403/14 , C07D471/04
摘要： The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
摘要翻译：本发明涉及吡咯取代的2-二氢吲哚酮化合物及其药学上可接受的盐，其调节蛋白激酶的活性，因此预期可用于预防和治疗与蛋白激酶相关的细胞病症例如癌症。

6. 发明申请

WO0160814A3 PYRROLE SUBSTITUTED 2-INDOLINONE PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： PYRROLE取代的2-INDOLINONE蛋白激酶抑制剂
公开(公告)号：WO0160814A3
公开(公告)日：2002-01-24
申请号：PCT/US0104813
申请日：2001-02-15
申请人： SUGEN INC , UPJOHN CO , TANG PENG CHO , MILLER TODD , LI XIAOYUAN , SUN LI , WEI CHUNG CHEN , SHIRAZIAN SHAHRZAD , LIANG CONGXIN , VOJKOVSKY TOMAS , NEMATALLA ASAAD S , HAWLEY MICHAEL
发明人： TANG PENG CHO , MILLER TODD , LI XIAOYUAN , SUN LI , WEI CHUNG CHEN , SHIRAZIAN SHAHRZAD , LIANG CONGXIN , VOJKOVSKY TOMAS , NEMATALLA ASAAD S , HAWLEY MICHAEL
IPC分类号： C07D401/14 , A61K31/404 , A61K31/4178 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P3/10 , A61P9/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/32 , C07D207/33 , C07D209/44 , C07D401/12 , C07D403/00 , C07D403/06 , C07D403/12 , C07D403/14 , C07D521/00
CPC分类号： C07D233/56 , C07D207/33 , C07D209/44 , C07D231/12 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14
摘要： The present invention relates to pyrrole substituted 2-indolinone compounds of formula (I): and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefor are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
摘要翻译：本发明涉及式（I）的吡咯取代的2-二氢吲哚酮化合物及其可调节蛋白激酶活性的药学上可接受的盐，预期可用于预防和治疗蛋白激酶相关的细胞病症例如癌症。

7. 发明申请

WO9824432A3 Use of indolinone compounds as modulators of protein kinases 审中-公开
标题翻译：使用吲哚酮化合物作为蛋白激酶的调节剂
公开(公告)号：WO9824432A3
公开(公告)日：1998-08-13
申请号：PCT/US9722210
申请日：1997-12-02
申请人： SUGEN INC , MCMAHON GERALD , TANG PENG CHO , SUN LI , TRAN NGOC MY
发明人： MCMAHON GERALD , TANG PENG CHO , SUN LI , TRAN NGOC MY
IPC分类号： A61K31/404 , A61K31/40
CPC分类号： A61K31/404
摘要： The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

8. 发明申请

WO1998024432A2 USE OF INDOLINONE COMPOUNDS AS MODULATORS OF PROTEIN KINASES 审中-公开
标题翻译：吲哚宁酮化合物作为蛋白激酶调节剂的使用
公开(公告)号：WO1998024432A2
公开(公告)日：1998-06-11
申请号：PCT/US1997022210
申请日：1997-12-02
申请人： SUGEN, INC. , McMAHON, Gerald , TANG, Peng, Cho , SUN, Li , TRAN, Ngoc, My
发明人： SUGEN, INC.
IPC分类号： A61K31/40
CPC分类号： A61K31/404
摘要： The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
摘要翻译：本发明涉及能够调节酪氨酸激酶信号转导以调节，调节和/或抑制异常细胞增殖的有机分子。

9. 发明申请

WO1998007695A1 INDOLINONE COMBINATORIAL LIBRARIES AND RELATED PRODUCTS AND METHODS FOR THE TREATMENT OF DISEASE 审中-公开
标题翻译：吲哚宁酮组合病毒及相关产品及治疗疾病的方法
公开(公告)号：WO1998007695A1
公开(公告)日：1998-02-26
申请号：PCT/US1997014736
申请日：1997-08-20
申请人： SUGEN, INC. , TANG, Peng, Cho , SUN, Li , McMAHON, Gerald , HIRTH, Klaus, Peter , SHAWVER, Laura, Kay
发明人： SUGEN, INC.
IPC分类号： C07D209/34
CPC分类号： C07D401/06 , C07D209/34 , C07D403/06 , C07D405/06 , C07D409/06 , C07D455/06 , C07D495/04
摘要： The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1' position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety. Indolinone compounds that are modified with substituents, particularly at the 5 position of the oxindole ring, can effectively activate protein kinases. This invention also features novel hydrosoluble indolinone compounds that are tyrosine kinase inhibitors and related products and methods.
摘要翻译：本发明涉及能够调节，调节和/或抑制蛋白激酶信号转导的有机分子。这些化合物可用于治疗与未调节的蛋白激酶信号转导相关的疾病，包括细胞增殖性疾病如癌症，动脉粥样硬化，关节炎和再狭窄以及诸如糖尿病的代谢疾病。本发明具有抑制蛋白激酶及相关产物和方法的吲哚啉酮化合物。可以通过向3 - [（吲哚-3-基）亚甲基] -2-二氢吲哚酮，特别是在吲哚环的1'位置添加化学取代基来获得对FLK蛋白激酶特异性的抑制剂。特异性抑制FLK和血小板衍生生长因子蛋白激酶的吲哚酮化合物可以含有四氢吲哚或环戊基-b-吡咯部分。被取代基修饰的吲哚啉酮化合物，特别是在羟吲哚环的5位，可以有效地激活蛋白激酶。本发明还具有酪氨酸激酶抑制剂和相关产物和方法的新型水溶性吲哚啉酮化合物。

10. 发明申请

WO2006119125A3 METHODS FOR SYNTHESIS OF CAROTENOIDS, INCLUDING ANALOGS, DERIVATIVES, AND SYNTHETIC AND BIOLOGICAL INTERMEDIATES 审中-公开
标题翻译：用于合成碳酸的方法，包括模拟物，衍生物，合成和生物中间体
公开(公告)号：WO2006119125A3
公开(公告)日：2007-01-11
申请号：PCT/US2006016487
申请日：2006-05-01
申请人： HAWAII BIOTECH INC , LOCKWOOD SAMUEL F , NADOLSKI GEOFF , BURDICK DAVID , TANG PENG CHO , JACKSON HENRY L , FANG ZHIQIANG , DU YISHU , YANG MIN , GEISS WILLIAM , WILLIAMS RICHARD
发明人： LOCKWOOD SAMUEL F , NADOLSKI GEOFF , BURDICK DAVID , TANG PENG CHO , JACKSON HENRY L , FANG ZHIQIANG , DU YISHU , YANG MIN , GEISS WILLIAM , WILLIAMS RICHARD
IPC分类号： C07F9/113 , C07C69/40
CPC分类号： C07C29/147 , C07C11/21 , C07C33/02 , C07C45/298 , C07C47/21 , C07C49/743 , C07C67/08 , C07C67/30 , C07C67/343 , C07C67/39 , C07C69/40 , C07C69/602 , C07C403/24 , C07C2601/16 , C07F9/113 , C07F9/65515 , C07C69/73 , C07C35/21
摘要： A method for synthesizing intermediates for use in the synthesis of carotenoid synthetic intermediates, carotenoid analogs, and/or carotenoid derivatives. The carotenoid analog, derivative, or intermediate may be administered to a subject for the inhibition and/or amelioration of any disease that involves production of reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals. In some embodiments, the invention may include methods for synthesizing chemical compounds including an analog or derivative of a carotenoid. Carotenoid analogs or derivatives may include acyclic end groups. In some embodiments, a carotenoid analog or derivative may include at least one substituent. The substituent may enhance the solubility of the carotenoid analog or derivative such that the carotenoid analog or derivative at least partially dissolves in water. Each R 3 ma be independently hydrogen or methyl. Each R 1 and R 2 may be independently:
摘要翻译：用于合成用于合成类胡萝卜素合成中间体，类胡萝卜素类似物和/或类胡萝卜素衍生物的中间体的方法。类胡萝卜素类似物，衍生物或中间体可以施用于受试者以抑制和/或改善涉及产生活性氧，活性氮物质，自由基和/或非自由基的任何疾病。在一些实施方案中，本发明可以包括合成包括类胡萝卜素类似物或衍生物的化合物的方法。类胡萝卜素类似物或衍生物可包括无环端基。在一些实施方案中，类胡萝卜素类似物或衍生物可包括至少一个取代基。取代基可以增强类胡萝卜素类似物或衍生物的溶解度，使得类胡萝卜素类似物或衍生物至少部分地溶解在水中。每个R 3独立地是氢或甲基。每个R 1和R 2可以独立地是：

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