公开(公告)号：EP2308832B1

公开(公告)日：2018-09-12

申请号：EP10182900.0

申请日：2001-06-29

申请人： Trustees of Tufts College ,  Paratek Pharmaceuticals, Inc.

发明人： Nelson, Mark L. ,  Frechette, Roger ,  Viski, Peter ,  Ismail, Mohamed Y ,  Bowser, Todd ,  Dumornay, Jimmy ,  Rennie, Glen ,  Liu, Gui ,  Koza, Darrell ,  Sheahan, Paul ,  Stapleton, Karen ,  Hawkins, Paul ,  Bhatia, Beena ,  Verma, Atul ,  McIntyre, Laura ,  Warchol, Ted

IPC分类号： C07C237/26 ,  A61K31/65 ,  A61P31/04 ,  A61P17/00

CPC分类号： A61K31/65 ,  C07C237/26 ,  C07C255/59 ,  C07C271/22 ,  C07C271/28 ,  C07C271/30 ,  C07C271/58 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C275/50 ,  C07C275/54 ,  C07C311/06 ,  C07C311/21 ,  C07C333/08 ,  C07C335/22 ,  C07C381/10 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/46 ,  C07D295/155 ,  C07F9/4006 ,  C07F9/4056 ,  Y02A50/473 ,  Y02A50/481

摘要： The present invention pertains, at least in part, to novel 9- substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

公开(公告)号：EP2308832A1

公开(公告)日：2011-04-13

申请号：EP10182900.0

申请日：2001-06-29

申请人： Trustees Of Tufts College ,  Paratek Pharmaceuticals, Inc.

发明人： Nelson, Mark L. ,  Frechette, Roger ,  Viski, Peter ,  Ismail, Mohamed Y ,  Bowser, Todd ,  Dumornay, Jimmy ,  Rennie, Glen ,  Liu, Gui ,  Koza, Darrell ,  Sheahan, Paul ,  Stapleton, Karen ,  Hawkins, Paul ,  Bhatia, Beena ,  Verma, Atul ,  McIntyre, Laura ,  Warchol, Ted

IPC分类号： C07C237/26 ,  A61K31/65

CPC分类号： A61K31/65 ,  C07C237/26 ,  C07C255/59 ,  C07C271/22 ,  C07C271/28 ,  C07C271/30 ,  C07C271/58 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C275/50 ,  C07C275/54 ,  C07C311/06 ,  C07C311/21 ,  C07C333/08 ,  C07C335/22 ,  C07C381/10 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/46 ,  C07D295/155 ,  C07F9/4006 ,  C07F9/4056 ,  Y02A50/473 ,  Y02A50/481

摘要： The present invention pertains, at least in part, to novel 9- substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

摘要翻译： 本发明至少部分涉及新的9-取代的米诺环素化合物。 这些米诺环素化合物可用于治疗许多四环素化合物应答状态，例如细菌感染和肿瘤，以及一般的米诺环素和四环素化合物的其它已知应用，例如一般阻断四环素化合物，如阻断四环素外排和 基因表达的调节。

公开(公告)号：EP1679305B1

公开(公告)日：2012-02-08

申请号：EP06007501.7

申请日：2001-06-29

申请人： TRUSTEES OF TUFTS COLLEGE ,  Paratek Pharmaceuticals, Inc.

发明人： Nelson, Mark, L. ,  Frechette, Roger ,  Viski, Peter ,  Ismail, Mohamed ,  Bowser, Todd ,  Dumornay, Jimmy ,  Rennie, Glen ,  Liu, Gui ,  Koza, Darrell ,  Sheahan, Paul ,  Stapleton, Karen ,  Hawkins, Paul ,  Bhatia, Beena ,  Verma, Atul ,  Mcintyre, Laura ,  Warchol, Tad

IPC分类号： C07C237/26 ,  A61K31/65

CPC分类号： A61K31/65 ,  C07C237/26 ,  C07C255/59 ,  C07C271/22 ,  C07C271/28 ,  C07C271/30 ,  C07C271/58 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C275/50 ,  C07C275/54 ,  C07C311/06 ,  C07C311/21 ,  C07C333/08 ,  C07C335/22 ,  C07C381/10 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/46 ,  C07D295/155 ,  C07F9/4006 ,  C07F9/4056 ,  Y02A50/473 ,  Y02A50/481

摘要： The present invention pertains, at least in part, to novel 9- substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

公开(公告)号：EP2308832B8

公开(公告)日：2019-04-24

申请号：EP10182900.0

申请日：2001-06-29

申请人： Trustees of Tufts College ,  Paratek Pharmaceuticals, Inc.

发明人： Nelson, Mark L. ,  Frechette, Roger ,  Viski, Peter ,  Ismail, Mohamed Y ,  Bowser, Todd ,  Dumornay, Jimmy ,  Rennie, Glen ,  Liu, Gui ,  Koza, Darrell ,  Sheahan, Paul ,  Stapleton, Karen ,  Hawkins, Paul ,  Bhatia, Beena ,  Verma, Atul ,  Honeyman, Laura ,  Warchol, Ted

IPC分类号： C07C237/26 ,  A61K31/65 ,  A61P31/04 ,  A61P17/00

公开(公告)号：EP2289871A1

公开(公告)日：2011-03-02

申请号：EP10183426.5

申请日：2001-06-29

申请人： Paratek Pharmaceuticals, Inc. ,  TRUSTEES OF TUFTS COLLEGE

发明人： Nelson, Mark L. ,  Frechette, Roger ,  Viski, Peter ,  Ismail, Mohamed ,  Bowser, Todd ,  Bhatia, Beena ,  Messersmith, David ,  McIntyre, Laura ,  Koza, Darrell ,  Rennie, Glen ,  Sheahan, Paul ,  Hawkins, Paul ,  Verma, Atul ,  Warchol, Tad ,  Bandarage, Upul

IPC分类号： C07C237/26 ,  C07C311/06 ,  A61K31/65

CPC分类号： C07D213/64 ,  C07C237/26 ,  C07C251/24 ,  C07C251/48 ,  C07C271/22 ,  C07C271/28 ,  C07C271/58 ,  C07C275/24 ,  C07C311/06 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2603/46 ,  C07D207/22 ,  C07D213/50 ,  C07D213/56 ,  C07D239/36 ,  C07D261/18 ,  C07D277/30 ,  C07D277/42 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D307/54 ,  C07D307/68 ,  C07D307/79 ,  C07D317/60 ,  C07D333/24 ,  C07D333/28 ,  C07D333/60 ,  C07F9/2475

摘要： The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

摘要翻译： 本发明至少部分地涉及新的7-取代四环素化合物。 这些四环素化合物可用于治疗多种四环素化合物反应状态，例如细菌感染和肿瘤，以及其它已知的米诺环素和四环素化合物的一般应用，例如阻断四环素外排和调节基因表达。

公开(公告)号：EP1679305A1

公开(公告)日：2006-07-12

申请号：EP06007501.7

申请日：2001-06-29

申请人： TRUSTEES OF TUFTS COLLEGE ,  Paratek Pharmaceuticals, Inc.

发明人： Nelson, Mark, L. ,  Frechette, Roger ,  Viski, Peter ,  Ismail, Mohamed ,  Bowser, Todd ,  Dumornay, Jimmy ,  Rennie, Glen ,  Liu, Gui ,  Koza, Darrell ,  Sheahan, Paul ,  Stapleton, Karen ,  Hawkins, Paul ,  Bhatia, Beena ,  Verma, Atul ,  Mcintyre, Laura ,  Warchol, Tad

IPC分类号： C07C237/26 ,  A61K31/65

CPC分类号： A61K31/65 ,  C07C237/26 ,  C07C255/59 ,  C07C271/22 ,  C07C271/28 ,  C07C271/30 ,  C07C271/58 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C275/50 ,  C07C275/54 ,  C07C311/06 ,  C07C311/21 ,  C07C333/08 ,  C07C335/22 ,  C07C381/10 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/46 ,  C07D295/155 ,  C07F9/4006 ,  C07F9/4056 ,  Y02A50/473 ,  Y02A50/481

摘要： The present invention pertains, at least in part, to novel 9- substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

摘要翻译： 本发明至少部分地涉及新的9-取代的米诺环素化合物。 这些米诺环素化合物可用于治疗许多四环素化合物反应状态，例如细菌感染和肿瘤，以及通常其他已知的米诺环素和四环素化合物的应用，例如通常阻断四环素化合物，例如阻断四环素外排和 调节基因表达。

公开(公告)号：EP2311451A1

公开(公告)日：2011-04-20

申请号：EP10184869.5

申请日：2003-03-10

申请人： Paratek Pharmaceuticals, Inc.

发明人： Nelson, Mark L. ,  Ohemeng, Kwasi ,  Frechette, Roger ,  Ismail, Mohamed Y ,  Honeyman, Laura ,  Bowser, Todd ,  Abato, Paul ,  Amoo, Victor ,  Assefa, Haregewein ,  Bhatia, Beena ,  Berniac, Joel ,  Chen, Jackson ,  Kim, Oak ,  Mechiche, Rachid ,  Reddy, Laxma N. ,  Verma, Atul K. ,  Viski, Peter ,  Warchol, Tadeusz ,  Yanachkov, Ivan

IPC分类号： A61K31/40 ,  A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/415 ,  A61K31/445 ,  A61K31/65 ,  C07C235/66 ,  C07D207/00 ,  C07D207/30 ,  C07D311/06 ,  A61P31/04

CPC分类号： C07D207/404 ,  C07C237/26 ,  C07C239/20 ,  C07C255/58 ,  C07C271/22 ,  C07C275/34 ,  C07C323/60 ,  C07C335/12 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/46 ,  C07D207/16 ,  C07D207/20 ,  C07D207/335 ,  C07D209/44 ,  C07D211/58 ,  C07D211/70 ,  C07D213/20 ,  C07D213/64 ,  C07D213/82 ,  C07D213/89 ,  C07D231/12 ,  C07D261/10 ,  C07D261/14 ,  C07D261/18 ,  C07D277/42 ,  C07D277/56 ,  C07D295/116 ,  C07D295/155 ,  C07D295/215 ,  C07D307/52 ,  C07D307/54 ,  C07D317/66 ,  C07D335/02

摘要： A tetracycline compound of the formula (II):

wherein:
J 1 is hydrogen, substituted or unsubstituted alkyl, aryl, sulfonyl, acyl or substituted carbonyl; J 2 is hydrogen, aryl, sulfonyl or acyl; or J 1 and J 2 are linked to form a ring; provided that at least one of J 1 or J 2 is not hydrogen; J 3 and J 4 are each alkyl, halogen or hydrogen; X is CHC(R 13 Y'Y), CR 6 'R 6 , C=CR 6 R 6 , S, NR 6 or O; R 2 , R 4 and R 4" are each independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic or heteroaromatic; R 4 is NR 4 'R 4 ", alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen or hydrogen; R 2' , R 3 , R 10 R 11 and R 12 are each hydrogen; R 5 is hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy or aryl carbonyloxy; R 6 and R 6 ' are each independently hydrogen, methylene, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; R 9 is hydrogen; R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; R 13 is hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; and Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl, or pharmaceutically acceptable salts or esters thereof.

摘要翻译： 式（II）的四环素化合物：其中：J 1是氢，取代或未取代的烷基，芳基，磺酰基，酰基或取代的羰基; J 2是氢，芳基，磺酰基或酰基; 或J 1和J 2连接形成环; 条件是J 1或J 2中的至少一个不是氢; J 3和J 4各自为烷基，卤素或氢; X是CHC（R 13 Y'Y），CR 6'R 6，C = CR 6 R 6，S，NR 6或O; R 2，R 4和R 4“各自独立地为氢，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，芳基，杂环或杂芳族; R 4为NR 4' 烯基，炔基，芳基，羟基，卤素或氢; R 2'，R 3，R 10 R 11和R 12各自为氢; 烷基，链烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，烷基羰基氧基或芳基羰基氧基; R 6和R 6'各自独立地为氢，亚甲基，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R 9是氢; R 8为氢，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R 13是氢，羟基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; 其中Y'和Y各自独立地为氢，卤素，羟基，氰基，巯基，氨基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基或其药学上可接受的盐或酯。

公开(公告)号：EP2316450A1

公开(公告)日：2011-05-04

申请号：EP10184863.8

申请日：2003-03-10

申请人： Paratek Pharmaceuticals, Inc.

发明人： Nelson, Mark L. ,  Ohemeng, Kwasi ,  Frechette, Roger ,  Ismail, Mohamed Y ,  Honeyman, Laura ,  Bowser, Todd ,  Abato, Paul ,  Amoo, Victor ,  Assefa, Haregewein ,  Berniac, Joel ,  Bhatia, Beena ,  Chen, Jackson ,  Kim, Oak ,  Mechiche, Rachid ,  Reddy, N. Laxma ,  Verma, Atul K. ,  Viski, Peter ,  Warchol, Tadeusz ,  Yanachkov, Ivan

IPC分类号： A61K31/40 ,  A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/415 ,  A61K31/445 ,  A61K31/65 ,  C07C235/66 ,  C07D207/00 ,  C07D207/30 ,  C07D311/06 ,  A61P31/04

CPC分类号： C07D207/404 ,  C07C237/26 ,  C07C239/20 ,  C07C255/58 ,  C07C271/22 ,  C07C275/34 ,  C07C323/60 ,  C07C335/12 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/46 ,  C07D207/16 ,  C07D207/20 ,  C07D207/335 ,  C07D209/44 ,  C07D211/58 ,  C07D211/70 ,  C07D213/20 ,  C07D213/64 ,  C07D213/82 ,  C07D213/89 ,  C07D231/12 ,  C07D261/10 ,  C07D261/14 ,  C07D261/18 ,  C07D277/42 ,  C07D277/56 ,  C07D295/116 ,  C07D295/155 ,  C07D295/215 ,  C07D307/52 ,  C07D307/54 ,  C07D317/66 ,  C07D335/02

摘要： A tetracycline compound having the following formula:

wherein:
J 5 and J 6 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, sulfonyl, acyl, substituted carbonyl or substituted thiocarbonyl, or linked to form a ring;
J 7 and J 8 are each alkyl, halogen, or hydrogen;
R 7 dimethylamino; and
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl, or pharmaceutically acceptable salts thereof.

摘要翻译： 具有下式的四环素化合物：其中：J 5和J 6各自独立地为氢，烷基，烯基，炔基，芳基，磺酰基，酰基，取代的羰基或取代的硫代羰基，或连接形成环; J 7和J 8各自为烷基，卤素或氢; R 7二甲基氨基; 其中R 8为氢，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基。

公开(公告)号：EP2298732A1

公开(公告)日：2011-03-23

申请号：EP10184631.9

申请日：2001-06-29

申请人： Paratek Pharmaceuticals, Inc.

发明人： Hawkins, Paul ,  Bhatia, Been ,  Warhol, Tad ,  Nelson, Mark L. ,  Frechette, Roger ,  Viski, Peter ,  Ismail, Mohammed ,  Bowser, Todd ,  McIntyre, Laura ,  Reddy, Laxma ,  Stapleton, Karen ,  Sheahan, Paul

IPC分类号： C07C237/26 ,  A61K31/65

CPC分类号： C07C237/26 ,  B32B37/0007 ,  B32B37/003 ,  B32B37/1284 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/46 ,  C07D209/48 ,  C07D213/82 ,  C07D215/14 ,  C07D307/24 ,  C07D317/60

摘要： A 7, 9-substituted tetracycline selected from:

摘要翻译： A选自7,9取代四环素：

公开(公告)号：EP2301913A1

公开(公告)日：2011-03-30

申请号：EP10184559.2

申请日：2001-06-29

申请人： Paratek Pharmaceuticals, Inc.

发明人： Hawkins, Paul ,  Bhatia, Beena ,  Warchol, Tad ,  Nelson, Mark, L. ,  Frechette, Roger ,  Viski, Peter ,  Ismail, Mohamed ,  Bowser, Todd ,  McIntyre, Laura ,  Reddy, Laxma ,  Stapleton, Karen ,  Sheahan, Paul

IPC分类号： C07C237/26 ,  A61K31/65

CPC分类号： C07C237/26 ,  B32B37/0007 ,  B32B37/003 ,  B32B37/1284 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/46 ,  C07D209/48 ,  C07D213/82 ,  C07D215/14 ,  C07D307/24 ,  C07D317/60

摘要： A 7, 9-substituted tetracycline compound of Formula I:

wherein:
X is CH 2 ;
R 4' and R 4" are each independently alkyl;
R 4 is NR 4' R 4" ;
R 2 , R 2' , R 3 , R 8 , R 10 , R 11 and R 12 are each hydrogen;
R 5 is hydrogen or hydroxyl;
R 7 is alkyl, alkenyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, arylalkyl, amino, acyl or -(CH 2 ) 0-3 NR 7c C(=W')WR 7a ;
R 9 is nitro, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, arylalkyl, amino, arylalkenyl, arylalkynyl, thionitroso, acyl or -(CH 2 ) 0-3 NR 9c C(=Z')ZR 9a ;
Z is CR 9d R 9e , S, NR 9b or O;
Z' is O, S or NR 9f ;
W is CR 7d R 7e , S, NR 7b or O;
W' is O, S or NR 7f ; and
R 7a , R 7b , R 7c , R 7d , R 7e , R 7f , R 9a , R 9b , R 9c , R 9d , R 9e and R 9f are each independently hydrogen, acyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic or heteroaromatic;
or a 7, 9-substituted tetracycline compound selected from:






and

摘要翻译： 7，9-取代的式I的四环素化合物：其中：X是CH 2; R 4'和R 4“各自独立地为烷基; R 4为NR 4'R 4”; R 2，R 2'，R 3，R 8，R 10，R 11和R 12各自为氢; R 5是氢或羟基; R 7是烷基，烯基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，芳基烷基，氨基，酰基或 - （CH 2）0-3 NR 7c C（= W'）WR 7a; R 9是硝基，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，芳烷基，氨基，芳基烯基，芳基炔基，亚硫基，酰基或 - （CH 2）0-3 NR 9c C（= Z' 9a; Z为CR 9d R 9e，S，NR 9b或O; Z'是O，S或NR 9f; W是CR 7d R 7e，S，NR 7b或O; W'是O，S或NR 7f; R 7a，R 7b，R 7c，R 7d，R 7e，R 7f，R 9a，R 9b，R 9c，R 9d，R 9e和R 9f各自独立地为氢，酰基，烷基，烯基，炔基，烷氧基 烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，芳基，杂环或杂芳族; 或选自以下的7,9取代的四环素化合物