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1. 发明授权

US07488726B2 Rifamycin analogs and uses thereof 失效
标题翻译：利妥霉素类似物及其用途
公开(公告)号：US07488726B2
公开(公告)日：2009-02-10
申请号：US11591971
申请日：2006-11-02
申请人： John H. Van Duzer , James M. Siedlecki , Xiang Y. Yu
发明人： John H. Van Duzer , James M. Siedlecki , Xiang Y. Yu
IPC分类号： C07D498/14 , C07D491/14 , A61K31/542 , A61K31/5383 , A61P31/04 , A61P31/10
CPC分类号： C07D498/18
摘要： The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 5′-halo and/or alkoxy analogs, and various 4′- and/or 6′-substituents that incorporate a cyclic amine moiety.
摘要翻译：本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。在一种形式中，类似物在25位被乙酰化，就像利福霉素一样。在另一种形式中，类似物在25位脱乙酰化。在其他形式中，苯并恶嗪利霉素，苯并噻嗪可的霉素和苯并二氮霉素类似物在苯环的不同位置衍生化，包括3'-羟基类似物，5'-卤素和/或烷氧基类似物，以及各种4'-和/或6'- 引入环胺部分的取代基。

2. 发明申请

US20100305149A1 Polyal Drug Conjugates Comprising Variable Rate-Releasing Linkers 有权
标题翻译：包括可变速率释放连接器的多重药物缀合物
公开(公告)号：US20100305149A1
公开(公告)日：2010-12-02
申请号：US12789047
申请日：2010-05-27
申请人： Aleksandr Yurkovetskiy , Mao Yin , Gui Liu , Laura C. Akullian , John J. Kane , Cheri A. Stevenson , Charles E. Hammond , Russell C. Petter , John H. Van Duzer , Timothy B. Lowinger
发明人： Aleksandr Yurkovetskiy , Mao Yin , Gui Liu , Laura C. Akullian , John J. Kane , Cheri A. Stevenson , Charles E. Hammond , Russell C. Petter , John H. Van Duzer , Timothy B. Lowinger
IPC分类号： A61K31/439 , A61P35/00 , A61P35/04 , C07D487/18 , C07D491/22 , G01N33/50
CPC分类号： C07D519/04 , A61K47/59 , C07D491/22 , G01N2500/00 , Y10T436/145555
摘要： Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.
摘要翻译：描述包含可变速率释放连接体的多价 - 药物共轭物以及制备这种缀合物的方法。也描述了这种多种药物共轭物的用途。

3. 发明授权

US5260316A Isoquinolyl substituted hydroxylamine derivatives 失效
标题翻译：异喹啉基取代的羟胺衍生物
公开(公告)号：US5260316A
公开(公告)日：1993-11-09
申请号：US893142
申请日：1992-06-03
申请人： John H. Van Duzer , Dennis M. Roland
发明人： John H. Van Duzer , Dennis M. Roland
IPC分类号： C07D209/46 , C07D217/24 , C07D223/16 , C07D279/02 , C07D401/06 , C07D401/12 , C07D409/06 , A61K31/47 , C07D217/06 , C07D217/16
CPC分类号： C07D223/16 , C07D209/46 , C07D217/24 , C07D279/02 , C07D401/06 , C07D401/12 , C07D409/06
摘要： The compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl; C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl; Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl; Y represents SO.sub.2 or CO; A represents O, S, or a direct bond; B represents lower alkylene; or B represents lower alkenylene provided that A represents a direct bond; X represents oxygen or sulfur; R.sub.1 represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocyclic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylaminocarbonyl, C.sub.3 -C.sub.7 -cycloalkylaminocarbonyl or C.sub.3 -C.sub.7 -cycloalkyl-lower alkylaminocarbonyl; R.sub.2 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, amino, mono- or di-lower alkylamino, lower alkenylamino, lower alkynylamino, carbocyclic or heterocyclic aryl-lower alkylamino, carbocyclic or heterocyclic arylamino, C.sub.3 -C.sub.7 -cycloalkylamino, C.sub.3 -C.sub.7 -cycloalkyl-lower alkylamino or lower alkoxycarbonyl-lower alkylamino; R.sub.3 and R.sub.4 independently represent hydrogen or lower alkyl; R.sub.a represents hydrogen, lower alkyl, halo, trifluoromethyl or lower alkoxy; and pharmaceutically acceptable salts thereof; their preparation and use as lipoxygenase inhibitors are described.
摘要翻译：下式的化合物其中R表示氢，低级烷基，芳基，联芳基，C 3 -C 7 - 环烷基，芳基 - 低级烷基，芳基 - 低级烯基，芳基 - 低级炔基，芳氧基 - 低级烷基，芳硫基低级烷基 C 3 -C 7 - 环烷基 - 低级烷基，联芳基 - 低级烷基，芳基-C 3 -C 7 - 环烷基，芳基-C 3 -C 7 - 环烷基 - 低级烷基或芳氧基 - 芳基 - 低级烷基; 芳基表示碳环或杂环芳基; Z表示C1-C3-亚烷基或亚乙烯基，各自未被取代或被低级烷基取代; Y表示SO2或CO; A代表O，S或直接键; B表示低级亚烷基; 或B表示低级亚烯基，条件是A表示直接键; X表示氧或硫; R 1表示氢，酰基，低级烷氧基羰基，氨基羰基，一或二低级烷基氨基羰基，低级链烯基氨基羰基，低级炔基氨基羰基，碳环或杂环芳基 - 低级烷基氨基羰基，碳环或杂环芳基氨基羰基，C3-C7-环烷基氨基羰基或C3-C7-环烷基 - 低级烷基氨基羰基; R 2表示低级烷基，低级烷氧基羰基 - 低级烷基，C 3 -C 7 - 环烷基，碳环或杂环芳基，碳环或杂环芳基 - 低级烷基，C 3 -C 7 - 环烷基 - 低级烷基，氨基，一或二 - 低级烷基氨基，低级碳环或杂环芳基 - 低级烷基氨基，碳环或杂环芳基氨基，C 3 -C 7 - 环烷基氨基，C 3 -C 7 - 环烷基 - 低级烷基氨基或低级烷氧基羰基 - 低级烷基氨基; R3和R4独立地表示氢或低级烷基; R a表示氢，低级烷基，卤素，三氟甲基或低级烷氧基; 及其药学上可接受的盐; 描述了它们作为脂氧合酶抑制剂的制备和用途。

4. 发明授权

US08609678B2 Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof 有权
标题翻译：作为蛋白质脱乙酰酶抑制剂的反酰胺化合物及其使用方法
公开(公告)号：US08609678B2
公开(公告)日：2013-12-17
申请号：US13437672
申请日：2012-04-02
申请人： John H. Van Duzer , Ralph Mazitschek , Walter Ogier , James E. Bradner , Guoxiang Huang , Dejian Xie , Nan Yu
发明人： John H. Van Duzer , Ralph Mazitschek , Walter Ogier , James E. Bradner , Guoxiang Huang , Dejian Xie , Nan Yu
IPC分类号： A01N43/54 , A61K31/505 , C07D239/42 , C07D401/04 , C07D239/02
CPC分类号： A61K31/505 , A61K31/164 , A61K31/337 , A61K45/06 , C07C237/36 , C07C259/06 , C07D209/46 , C07D209/48 , C07D213/30 , C07D213/74 , C07D213/81 , C07D235/30 , C07D239/42 , C07D241/20 , C07D263/58 , C07D277/24 , C07D277/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D413/04 , C07D417/06
摘要： The present invention relates to “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
摘要翻译：本发明涉及包含锌螯合剂基团的“逆酰胺”化合物，以及这些化合物在抑制HDAC6中的用途以及治疗与HDAC6有关的各种疾病，病症或病症。

5. 发明授权

US5350761A Indolyl substituted hydroxylamine derivatives 失效
标题翻译：吲哚基取代的羟胺衍生物
公开(公告)号：US5350761A
公开(公告)日：1994-09-27
申请号：US99873
申请日：1993-07-30
申请人： John H. Van Duzer , Dennis M. Roland
发明人： John H. Van Duzer , Dennis M. Roland
IPC分类号： C07D209/46 , C07D217/24 , C07D223/16 , C07D279/02 , C07D401/06 , C07D401/12 , C07D409/06 , A61K31/405 , C07D209/12 , C07D209/34
CPC分类号： C07D209/46 , C07D217/24 , C07D223/16 , C07D279/02 , C07D401/06 , C07D401/12 , C07D409/06
摘要： Disclosed are the compound of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl;Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl;Y represents SO.sub.2 (sulfonyl) or CO (carbonyl);A represents O (oxygen), S (sulfur), or a direct bond;B represents lower alkylene; or B represents lower alkenylene provided that A represents a direct bond;X represents oxygen or sulfur,R.sub.1 represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocyclic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylaminocarbonyl, C.sub.3 -C.sub.7 -cycloalkylaminocarbonyl or C.sub.3 -C.sub.7 -cycloalkyl-lower alkylaminocarbonyl;R.sub.2 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, amino, mono- or di-lower alkylamino, lower alkenylamino, lower alkynylamino, carbocyclic or heterocyclic aryl-lower alkylamino, carbocyclic or heterocyclic arylamino, C.sub.3 -C.sub.7 -cycloalkylamino, C.sub.3 -C.sub.7 -cycloalkyl-lower alkylamino or lower alkoxycarbonyl-lower alkylamino;R.sub.3 and R.sub.4 independently represent hydrogen or lower alkyl;R.sub.a represents hydrogen, lower alkyl, halo, trifluoromethyl or lower alkoxy; and pharmaceutically acceptable salts thereof; which are useful as lipoxygenase inhibitors.
摘要翻译：公开了式（I）的化合物，其中R表示氢，低级烷基，芳基，联芳基，C 3 -C 7 - 环烷基，芳基 - 低级烷基，芳基 - 低级烯基，芳基 - 低级炔基，芳氧基 - 低级烷基，芳硫基 - 低级烷基，C 3 -C 7 - 环烷基 - 低级烷基，联芳基 - 低级烷基，芳基-C 3 -C 7 - 环烷基，芳基-C 3 -C 7 - 环烷基 - 低级烷基或芳氧基 - 芳基 - 低级烷基; 芳基表示碳环或杂环芳基; Z表示C1-C3-亚烷基或亚乙烯基，各自未被取代或被低级烷基取代; Y表示SO 2（磺酰基）或CO（羰基）; A表示O（氧），S（硫）或直接键; B表示低级亚烷基; 或B表示低级亚烯基，条件是A表示直接键; X代表氧或硫，R1代表氢，酰基，低级烷氧基羰基，氨基羰基，一或二低级烷基氨基羰基，低级烯基氨基羰基，低级炔基氨基羰基，碳环或杂环芳基 - 低级烷基氨基羰基，碳环或杂环芳基氨基羰基，C3-C7-环烷基氨基羰基或 C 3 -C 7 - 环烷基 - 低级烷基氨基羰基; R 2表示低级烷基，低级烷氧基羰基 - 低级烷基，C 3 -C 7 - 环烷基，碳环或杂环芳基，碳环或杂环芳基 - 低级烷基，C 3 -C 7 - 环烷基 - 低级烷基，氨基，一或二 - 低级烷基氨基，低级碳环或杂环芳基 - 低级烷基氨基，碳环或杂环芳基氨基，C 3 -C 7 - 环烷基氨基，C 3 -C 7 - 环烷基 - 低级烷基氨基或低级烷氧基羰基 - 低级烷基氨基; R3和R4独立地表示氢或低级烷基; R a表示氢，低级烷基，卤素，三氟甲基或低级烷氧基; 及其药学上可接受的盐; 它们可用作脂氧合酶抑制剂。

6. 发明授权

US08524214B2 Polyal drug conjugates comprising variable rate-releasing linkers 有权
标题翻译：包含可变速率释放接头的多价药物共轭物
公开(公告)号：US08524214B2
公开(公告)日：2013-09-03
申请号：US12789047
申请日：2010-05-27
申请人： Aleksandr Yurkovetskiy , Mao Yin , Gui Liu , Laura C. Akullian , John J. Kane , Cheri A. Stevenson , Charles E. Hammond , Russell C. Petter , John H. Van Duzer , Timothy B. Lowinger
发明人： Aleksandr Yurkovetskiy , Mao Yin , Gui Liu , Laura C. Akullian , John J. Kane , Cheri A. Stevenson , Charles E. Hammond , Russell C. Petter , John H. Van Duzer , Timothy B. Lowinger
IPC分类号： A61K31/045 , A61K31/04 , A61K31/13 , A61K31/21 , A61K31/33 , A61K31/695 , A61K31/765
CPC分类号： C07D519/04 , A61K47/59 , C07D491/22 , G01N2500/00 , Y10T436/145555
摘要： Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.
摘要翻译：描述包含可变速率释放连接体的多价 - 药物共轭物以及制备这种缀合物的方法。也描述了这种多种药物共轭物的用途。

7. 发明授权

US5334600A Isoquinolyl substituted hydroxylamine derivatives 失效
标题翻译：异喹啉基取代的羟胺衍生物
公开(公告)号：US5334600A
公开(公告)日：1994-08-02
申请号：US12081
申请日：1993-02-01
申请人： John H. Van Duzer , Dennis M. Roland
发明人： John H. Van Duzer , Dennis M. Roland
IPC分类号： C07D209/46 , C07D217/24 , C07D223/16 , C07D279/02 , C07D401/06 , C07D401/12 , C07D409/06 , A61K31/47 , C07D217/06 , C07D217/16
CPC分类号： C07D209/46 , C07D217/24 , C07D223/16 , C07D279/02 , C07D401/06 , C07D401/12 , C07D409/06
摘要： The compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl; Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl; Y represents SO.sub.2 (sulfonyl) or CO (carbonyl); A represents .sub.0 (oxygen), S (sulfur), or a direct bond; B represents lower alkylene; or B represents lower alkenylene or lower alkynylene provided that A represents a direct bond; X represents oxygen or sulfur, R.sub.1 represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocyclic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylaminocarbonyl, C.sub.3 -C.sub.7 -cycloalkylaminocarbonyl or C.sub.3 -C.sub.7 -cycloalkyl-lower alkylaminocarbonyl; R.sub.2 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloaikyl-lower alkyl, amino, mono- or di-lower alkylamino, lower alkenylamino, lower alkynylamino, carbocyclic or heterocyclic aryl-lower alkylamino, carbocyclic or heterocyclic arylamino, C.sub.3 -C.sub.7 -cycloalkylamino, C.sub.3 -C.sub.7 -cycloalkyl-lower alkylamino or lower alkoxycarbonyl-lower alkylamino; R.sub.3 and R.sub.4 independently represent hydrogen or lower alkyl; R.sub.a represents hydrogen, lower alkyl, halo, trifluoromethyl or lower alkoxy; and pharmaceutically acceptable salts thereof; and their preparation and use as lipoxygenase inhibitors are described.
摘要翻译：下式的化合物其中R表示氢，低级烷基，芳基，联芳基，C 3 -C 7 - 环烷基，芳基 - 低级烷基，芳基 - 低级烯基，芳基 - 低级炔基，芳氧基 - 低级烷基，芳硫基低级烷基，C 3 -C 7 - 环烷基 - 低级烷基，联芳基 - 低级烷基，芳基-C 3 -C 7 - 环烷基，芳基-C 3 -C 7 - 环烷基 - 低级烷基或芳氧基 - 芳基 - 低级烷基; 芳基表示碳环或杂环芳基; Z表示C1-C3-亚烷基或亚乙烯基，各自未被取代或被低级烷基取代; Y表示SO 2（磺酰基）或CO（羰基）; A代表0（氧），S（硫）或直接键; B表示低级亚烷基; 或B表示低级亚烯基或低级亚烷基，条件是A表示直接键; X代表氧或硫，R1代表氢，酰基，低级烷氧基羰基，氨基羰基，一或二低级烷基氨基羰基，低级烯基氨基羰基，低级炔基氨基羰基，碳环或杂环芳基 - 低级烷基氨基羰基，碳环或杂环芳基氨基羰基，C3-C7-环烷基氨基羰基或 C 3 -C 7 - 环烷基 - 低级烷基氨基羰基; R 2表示低级烷基，低级烷氧基羰基 - 低级烷基，C 3 -C 7 - 环烷基，碳环或杂环芳基，碳环或杂环芳基 - 低级烷基，C 3 -C 7 - 环烷基 - 低级烷基，氨基，一或二 - 低级烷基氨基，低级碳环或杂环芳基 - 低级烷基氨基，碳环或杂环芳基氨基，C 3 -C 7 - 环烷基氨基，C 3 -C 7 - 环烷基 - 低级烷基氨基或低级烷氧基羰基 - 低级烷基氨基; R3和R4独立地表示氢或低级烷基; R a表示氢，低级烷基，卤素，三氟甲基或低级烷氧基; 及其药学上可接受的盐; 并描述其作为脂氧合酶抑制剂的制备和用途。

8. 发明授权

US4929751A Vinyl tricarbonyl compounds and methods of making the same 失效
标题翻译：乙烯基三羰基化合物及其制备方法
公开(公告)号：US4929751A
公开(公告)日：1990-05-29
申请号：US109804
申请日：1987-10-19
申请人： Harry H. Wasserman , Natesan Murugesan , John H. Van Duzer
发明人： Harry H. Wasserman , Natesan Murugesan , John H. Van Duzer
IPC分类号： C07C69/738 , C07D231/12 , C07D263/32 , C07D401/06 , C07D403/06 , C07D405/06
CPC分类号： C07D401/06 , C07C69/738 , C07D263/32 , C07D403/06 , C07D405/06
摘要： A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R.sub.1 is a hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, and cycloalkyl with 3 to 7 carbon atoms,R.sub.2 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic,R.sub.3 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic, andR.sub.4 is unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl are 3 to 7 carbon atoms. Such vinyl tricarbonyl compound is effective against tumor cells.
摘要翻译：其中R1是氢，卤素，未取代或取代的C1至C30烷基，未取代或取代的芳基，芳基烷基和具有3至7个碳原子的环烷基的式IMAMA的乙烯基三羰基化合物或其一水合物 R 2为氢，卤素，未取代或取代的C 1 -C 30烷基，未取代或取代的芳基，芳基烷基，具有3至7个碳原子的环烷基，氰基，硝基或杂环基，R 3为氢，卤素，未取代或取代的C 1至C 30 烷基，未取代或取代的芳基，芳基烷基，具有3至7个碳原子的环烷基，氰基，硝基或杂环，并且R 4是未取代或取代的C 1至C 30烷基，未取代或取代的芳基，芳烷基，环烷基具有3至7个碳原子。这种乙烯基三羰基化合物对肿瘤细胞有效。

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