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1. 发明申请

US20120282619A1 METHOD FOR SCREENING ANTI-CANCER COMPOUNDS INHIBITING FUNCTION OF TM4SF5 AND ANTI-CANCER COMPOSITION CONTAINING CHALCONE COMPOUNDS 有权
标题翻译：用于筛选抗癌化合物抑制TM4SF5功能的方法和含有化合物的抗癌组合物
公开(公告)号：US20120282619A1
公开(公告)日：2012-11-08
申请号：US13482568
申请日：2012-05-29
申请人： Ki Hun Park , Jung Weon Lee , Young Bae Ryu , Hyung Won Ryu , Sin-Ae Lee
发明人： Ki Hun Park , Jung Weon Lee , Young Bae Ryu , Hyung Won Ryu , Sin-Ae Lee
IPC分类号： C12Q1/48 , C12Q1/68 , C12Q1/02 , G01N33/566 , G01N33/573 , C12Q1/34
CPC分类号： A61K31/135 , C07C49/835 , C07C49/84 , C07C309/66 , C07C309/73 , C07C309/75 , C07C309/76 , C07C311/21 , C07C311/29 , C07C311/44 , G01N33/5011 , G01N2333/9121
摘要： The present invention relates to a method for screening an anticancer compound and an anticancer compound screened using the method, and more particularly, to a method for screening an anticancer compound, the method comprising: culturing cancer cells expressing the oncogenic protein transmembrane 4 L6 family member 5 (TM4SF5), expressed as the polypeptide of SEQ ID NO: 2, treating the cancer cells with an anticancer candidate, and determining that the anticancer candidate is an anticancer substance when the candidate exhibits antagonistic activity against tumor formation and metastasis based on several events through the molecular mechanism of TM4SF5. The present invention also relates to chalcone compounds screened to have anticancer activity using the method, and an anticancer composition comprising the compound as an effective ingredient.
摘要翻译：本发明涉及使用该方法筛选抗癌化合物和抗癌化合物的方法，更具体地，涉及一种抗癌化合物的筛选方法，所述方法包括：培养表达致癌蛋白跨膜4L6家族成员的癌细胞 5（TM4SF5），表达为SEQ ID NO：2的多肽，用抗癌候选物治疗癌细胞，并且当候选物基于若干事件显示出对肿瘤形成和转移的拮抗活性时，确定抗癌候选物是抗癌物质通过TM4SF5的分子机制。本发明还涉及使用该方法筛选具有抗癌活性的查耳酮化合物和包含该化合物作为有效成分的抗癌组合物。

2. 发明申请

US20100233610A1 POLYMER HAVING A SULFONIC GROUP OR A SULFONATE GROUP AND AN AMIDE GROUP AND METHOD OF PRODUCING SAME 有权
标题翻译：具有磺基或亚磺酸基的聚合物及其生产方法
公开(公告)号：US20100233610A1
公开(公告)日：2010-09-16
申请号：US12783975
申请日：2010-05-20
申请人： Tatsuki Fukui , Takashi Kenmoku , Ako Kusakari , Chieko Mihara , Tetsuya Yano , Norikazu Fujimoto
发明人： Tatsuki Fukui , Takashi Kenmoku , Ako Kusakari , Chieko Mihara , Tetsuya Yano , Norikazu Fujimoto
IPC分类号： G03G9/08 , C08F28/02 , G03G9/097 , G03G9/087 , G03G13/20 , G03G15/08
CPC分类号： C08F8/34 , C07C309/15 , C07C309/51 , C07C309/69 , C07C309/76 , C08F8/14 , C08F212/08 , C08F220/58 , C08F2220/585 , G03G9/08726 , G03G9/097 , C08F220/14
摘要： A polymer is provided in which a sulfonic group or a derivative thereof is introduced. The polymer includes a unit represented by the following chemical formula (1): wherein R represents -A1-SO2R1; A1 is selected from an alkylene group, a heterocyclic ring, an aromatic ring; and —SO2R1 is a sulfonic group or of a derivative of a sulfonic acid.
摘要翻译：提供其中引入了磺酸基或其衍生物的聚合物。聚合物包括由下列化学式（1）表示的单元：其中R表示-A1-SO2R1; A1选自亚烷基，杂环，芳香环，和-SO 2 R 1是磺酸基或磺酸衍生物。

3. 发明申请

US20100121023A1 POLYMER HAVING A SULFONIC GROUP OR A SULFONATE GROUP AND AN AMIDE GROUP AND METHOD OF PRODUCING SAME 审中-公开
标题翻译：具有磺基或亚磺酸基的聚合物及其生产方法
公开(公告)号：US20100121023A1
公开(公告)日：2010-05-13
申请号：US12560852
申请日：2009-09-16
申请人： Tatsuki Fukui , Takashi Kenmoku , Ako Kusakari , Chieko Mihara , Tetsuya Yano , Norikazu Fujimoto
发明人： Tatsuki Fukui , Takashi Kenmoku , Ako Kusakari , Chieko Mihara , Tetsuya Yano , Norikazu Fujimoto
IPC分类号： C08G69/26
CPC分类号： C08F8/34 , C07C309/15 , C07C309/51 , C07C309/69 , C07C309/76 , C08F8/14 , C08F212/08 , C08F220/58 , C08F2220/585 , G03G9/08726 , G03G9/097 , C08F220/14
摘要： A polymer is provided in which a sulfonic group or a derivative thereof is introduced. The polymer includes a unit represented by the following chemical formula (1): wherein R represents -A1-SO2R1; Al is selected from an alkylene group, a heterocyclic ring, an aromatic ring; and —SO2R1 is a sulfonic group or of a derivative of a sulfonic acid.
摘要翻译：提供其中引入了磺酸基或其衍生物的聚合物。聚合物包括由下列化学式（1）表示的单元：其中R表示-A1-SO2R1; Al选自亚烷基，杂环，芳香环，和-SO 2 R 1是磺酸基或磺酸衍生物。

4. 发明申请

US20100041916A1 PROCESS FOR PRODUCTION OF SULFONIC ACID ESTER 有权
标题翻译：硫酸酯生产工艺
公开(公告)号：US20100041916A1
公开(公告)日：2010-02-18
申请号：US12441004
申请日：2007-04-20
申请人： Kuniaki Okamoto , Tsutomu Watahiki , Motoshige Sumino , Takao Shibasaki
发明人： Kuniaki Okamoto , Tsutomu Watahiki , Motoshige Sumino , Takao Shibasaki
IPC分类号： C07C309/30 , C07C309/01 , C07C309/28
CPC分类号： C07C303/26 , C07D327/00 , C07C309/65 , C07C309/66 , C07C309/73 , C07C309/76 , C07C309/67
摘要： The present invention provides a method for producing a sulfonate ester efficiently and in high yield.The present invention is an invention of a method for producing a sulfonate ester compound, which comprising reacting: (a) a compound having a sulfo group (—SO3H); and (b) a compound having a group represented by the general formula [1]: —OR1 [1] [wherein, R1 represents a sulfonyl group represented by the general formula [2]: —SO2—R2 [2] (wherein, R2 represents a halogen atom, a haloalkyl group, an alkoxy group, or an optionally substituted alkyl group or an optionally substituted aryl group) or an acyl group represented by the general formula [3]: (wherein, R3 represents an optionally substituted alkyl group or an optionally substituted aryl group)]; in the presence of an organic base which is capable of forming a salt with said sulfo group.
摘要翻译：本发明提供了一种有效且高收率地生产磺酸酯的方法。本发明是一种磺酸酯化合物的制造方法的发明，其包括：（a）具有磺基（-SO 3 H）的化合物; 和（b）具有由通式[1]表示的基团的化合物：-OR1 [1] [其中，R1表示由通式[2]表示的磺酰基：-SO 2 -R 2 [2]（其中， R2表示卤素原子，卤代烷基，烷氧基或任选取代的烷基或任选取代的芳基）或由通式[3]表示的酰基：（其中，R 3表示任选取代的烷基或任选取代的芳基）]; 在能够与所述磺基形成盐的有机碱存在下进行。

5. 发明申请

US20080167347A1 Ctgf Expression Inhibitor 审中-公开
标题翻译： Ctgf表达抑制剂
公开(公告)号：US20080167347A1
公开(公告)日：2008-07-10
申请号：US11795533
申请日：2006-01-19
申请人： Kaoru Seno , Toshihiro Shinosaki , Satoshi Hata , Isamu Yamada , Hiroki Sato , Mikayo Hayashi
发明人： Kaoru Seno , Toshihiro Shinosaki , Satoshi Hata , Isamu Yamada , Hiroki Sato , Mikayo Hayashi
IPC分类号： A61K31/45 , C07C235/68 , A61K31/167 , C07D211/96
CPC分类号： A61K31/167 , A61K31/45 , C07C235/64 , C07C255/57 , C07C305/24 , C07C309/76 , C07C311/04 , C07C311/08 , C07C311/21 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/12 , C07C323/62 , C07D207/323 , C07D207/48 , C07D211/96 , C07D213/30 , C07D213/40 , C07D215/48 , C07D233/64 , C07D235/08 , C07D239/34 , C07D239/42 , C07D243/08 , C07D279/02 , C07D295/088 , C07D295/135 , C07D295/155 , C07D295/185 , C07D295/192 , C07D295/26 , C07D307/12 , C07D307/42 , C07D307/52 , C07D307/79 , C07D307/81 , C07D317/60 , C07D333/22 , C07D333/54 , C07D333/58 , C07D335/02 , C07D401/12
摘要： A CTGF expression inhibitor comprising a compound of the formula I: a pharmaceutically acceptable salt or solvate thereof as an active ingredient, (wherein Y is hydroxy or a group of the formula: —NH—SO2—Y′ (wherein Y′ is optionally substituted aryl or optionally substituted alkyl), and R1 to R9 are each independently hydrogen, halogen, optionally substituted alkyl, optionally substituted alkoxy or the like).
摘要翻译：一种CTGF表达抑制剂，其包含式I化合物：其药学上可接受的盐或溶剂化物作为活性成分（其中Y为羟基或式-NH-SO 2 -Y '（其中Y'为任选取代的芳基或任选取代的烷基），R 1至R 9各自独立地为氢，卤素，任选取代的烷基，任选取代的烷氧基或类似）。

6. 发明申请

US20070049742A1 Single Pot Process For The Preparation Of Diazonaphthoquinonesulfonyl Ester 有权
标题翻译：单罐方法制备重氮萘醌磺酰酯
公开(公告)号：US20070049742A1
公开(公告)日：2007-03-01
申请号：US11277006
申请日：2006-03-20
申请人： Vummadi Reddy , Boddu Rao , Maruthi Ram Reddy , Chiguru Srinivas , Chilukuri Ramesh , Vaidya Rao
发明人： Vummadi Reddy , Boddu Rao , Maruthi Ram Reddy , Chiguru Srinivas , Chilukuri Ramesh , Vaidya Rao
IPC分类号： C07C245/02
CPC分类号： C07C303/28 , C07C2602/10 , C07C309/71 , C07C309/76
摘要： The present invention provides a single pot process for the preparation of diazonaphthoquinonesulfonyl ester, a useful organic material for micro electronic and dye industry. This study pertains to the one pot preparation of diazonaphthoquinonesulfonyl esters using the corresponding diazonaphthoquinine sulfonic acid or its sodium salt, diphosgene or triphosgene, variety of hydroxy compounds and tertiary organic base in an organic solvent medium.
摘要翻译：本发明提供了制备用于微电子和染料工业的有用的重氮萘醌磺酰酯的单罐方法。本研究涉及在有机溶剂介质中使用相应的重氮萘醌醌磺酸或其钠盐，双光气或三光气，多种羟基化合物和叔有机碱的一氮杂萘醌磺酰酯的一锅制备。

7. 发明申请

US20050059638A1 Aryl, heteroaromatic and bicyclic aryl nitrone compounds, prodrugs and pharmaceutical compositions of the same to treat human disorders 审中-公开
标题翻译：芳基，杂芳族和双环芳基硝酮化合物，其药物组合物和药物组合物用于治疗人类疾病
公开(公告)号：US20050059638A1
公开(公告)日：2005-03-17
申请号：US10911788
申请日：2004-08-03
申请人： Michael Kelly , Satyanarayana Janagani , Ravindra Upasani
发明人： Michael Kelly , Satyanarayana Janagani , Ravindra Upasani
IPC分类号： A61K20060101 , A61K31/195 , A61K31/40 , A61K31/44 , A61K31/66
CPC分类号： C07C291/02 , C07C309/46 , C07C309/61 , C07C309/76 , C07C311/16 , C07C323/47 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/75 , C07D215/36 , C07D231/12 , C07D233/06 , C07D295/135 , C07D333/38 , C07F9/3856 , C07F9/4021
摘要： Disclosed are aryl, heteroaromatic and bicyclic aryl nitrone compounds and pharmaceutical compositions containing such derivatives. The disclosed compositions are useful for preventing and/or treating pain, neurodegenerative, autoimmune and inflammatory diseases or conditions in mammals.
摘要翻译：公开了芳基，杂芳族和双环芳基硝酮化合物和含有这些衍生物的药物组合物。所公开的组合物可用于预防和/或治疗哺乳动物中的疼痛，神经退行性，自身免疫性和炎性疾病或病症。

8. 发明授权

US06730783B2 Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：制备氨基胍和烷氧基胍作为蛋白酶抑制剂的方法
公开(公告)号：US06730783B2
公开(公告)日：2004-05-04
申请号：US10419972
申请日：2003-04-22
申请人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan
IPC分类号： A61K31255
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12，说明书中列出的R a，R b，R c，Y，Z，n和m以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐是描述。还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。

9. 发明授权

US06706765B2 Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：氨基胍和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：US06706765B2
公开(公告)日：2004-03-16
申请号：US10359078
申请日：2003-02-06
申请人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan , Thomas P. Stagnaro
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan , Thomas P. Stagnaro
IPC分类号： A61K3118
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12，说明书中列出的R a，R b，R c，Y，Z，n和m以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐是描述。还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。

10. 发明授权

US5602260A Selected O-quinonediazide sulfonic acid esters of phenolic compounds and their use in radiation-sensitive compositions 失效
标题翻译：酚类化合物的选择的O-醌二叠氮化物磺酸酯及其在辐射敏感组合物中的用途
公开(公告)号：US5602260A
公开(公告)日：1997-02-11
申请号：US451939
申请日：1995-05-26
申请人： Andrew J. Blakeney , Arturo N. Medina , Medhat A. Toukhy , Lawrence Ferreira , Sobhy Tadros
发明人： Andrew J. Blakeney , Arturo N. Medina , Medhat A. Toukhy , Lawrence Ferreira , Sobhy Tadros
IPC分类号： G03F7/039 , C07C39/15 , C07C39/17 , C07C43/23 , C07C47/575 , C07C309/76 , C07D307/80 , C07D317/54 , C07D319/18 , C08G8/00 , C08G8/10 , G03F7/022 , C07D407/10
CPC分类号： C07C43/23 , C07C309/76 , C07C47/575 , C07C2102/10
摘要： A photosensitive compound comprising at least one o-quinonediazide sulfonic acid ester of a phenolic compound, said esters selected from the group consisting of formulae (IB) and (IIB): ##STR1## wherein the variables are as defined in the description.
摘要翻译：一种光敏化合物，其包含至少一种酚类化合物的邻醌二叠氮磺酸酯，所述酯选自式（IB）和（IIB）：其中变量如说明书中所定义。

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