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1.发明授权Pleuromutilin derivatives for the treatment of diseases mediated by microbes 有权Pleuromutilin-Derivate zur Behandlung von durch Mikroben vermittelten Krankheiten
公开(公告)号：EP2380874B1
公开(公告)日：2016-12-28
申请号：EP11005863.3
申请日：2008-03-19
发明人： Riedl, Rosemarie , Heilmayer, Werner , Badegruber, Rudolf , Strickmann, Dirk , Novak, Rodger , Ferencic, Matthias , Bulusu, Atchyuta Rama Chandra Murty
IPC分类号： C07C323/52 , A61K31/215 , A61P31/00
CPC分类号： A61K31/5375 , A61K31/215 , A61K31/357 , C07C323/52 , C07C323/61 , C07C2601/14 , C07C2603/99 , C07D295/096 , C07D317/72
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2.发明公开PLEUROMUTILIN DERIVATIVES FOR USE IN THE TREATMENT OF DISEASES MEDIATED BY MICROBES 有权富兰克林堡德克萨斯州立大学维克登堡
公开(公告)号：EP2614049A1
公开(公告)日：2013-07-17
申请号：EP11751528.8
申请日：2011-08-11
IPC分类号： C07C323/52 , A61K31/215 , A61P31/00
CPC分类号： C07C323/52 , A61K31/235 , A61K45/06 , C07C2601/04 , C07C2601/08 , C07C2601/18 , C07C2602/42 , C07C2602/44 , C07C2603/99
摘要： Compounds selected from the group ofN-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C 0-4 )alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C 0-4 )alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C 0-4 )alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C 0-4 )alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C 0-4 )alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C 0-4 )alkyt-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.
摘要翻译： 选自作为14-O- [（氨基（C 0-4）烷基 - 羟基 - 环烷基 - 或双环烷基硫烷基） - 乙酰基] - 木聚糖的N-取代或N-烷基化或N-酰化的14-O- （氨基（C 0-4）烷基 - 羟基 - 环丁基硫烷基） - 乙酰基] - 木兰林，14-O - [（氨基（C 0-4）烷基 - 羟基 - 环戊基硫烷基） - 乙酰基] （氨基（C 0-4）烷基 - 羟基 - 环庚基硫烷基） - 乙酰基] - 木霉素，14-O - [（氨基（C 0-4）烷基 - 羟基 - 环辛基硫烷基） - 乙酰基] 任选呈盐和/或溶剂化物形式的[（氨基（C 0-4）烷基 - 羟基 - 双环烷基硫烷基） - 乙酰基] - 木
坦林，包含这些化合物的药物组合物及其作为药物的用途，例如 用于治疗微生物感染和治疗痤疮，任选地与其它药物活性剂组合。-
3.发明公开Pleuromutilin derivatives containing a hydroxyamino- or acyloxyaminocycloalkyl group 有权含有羟基氨基 - 或酰氧基氨基环烷基的截短侧耳素衍生物
公开(公告)号：EP2298733A2
公开(公告)日：2011-03-23
申请号：EP10009685.8
申请日：2006-06-26
IPC分类号： C07C323/52 , A61K31/16 , A61P17/00
CPC分类号： C07C323/52 , C07C2601/14 , C07C2603/99
摘要： The present invention relates to compounds of general formula I
wherein
R is hydrogen and R 1 is hydroxy or acyloxy, or
R is acyl and R 1 is hydroxy or acyloxy,
X is sulphur, oxygen or NR 10 , wherein R 10 is hydrogen or (C 1-4 )alkyl;
Y is sulphur or oxygen;
R 2 is hydrogen or one or more substituents, e.g. including substituents such as conventional in organic, e.g. (pleuro)mutilin, chemistry;
R4 is hydrogen or (C 1-4 )alkyl;
R 5 is hydrogen or (C 1-4 )alkyl;
R 3 and R 3 ' are hydrogen, deuterium, or halogen;
R 6 , R 7 and R 8 are hydrogen, halogen or deuterium;
m is a number selected from 0 to 4,
n is a number selected from 0 to 10, and
p is a number selected from 0 to 10;
with the proviso that n plus p are at least 1.
These compounds are useful as pharmaceuticals, particularly as antimicrobials.摘要翻译： 本发明涉及通式I的化合物，其中R是氢并且R1是羟基或酰氧基，或者R是酰基并且R1是羟基或酰氧基，X是硫，氧或NR10，其中R10是氢或（C1-4） 烷基; Y是硫或氧; R 2是氢或一个或多个取代基，例如 包括取代基如常规的有机物， （pleuro）mutilin，化学; R4是氢或（C1-4）烷基; R5是氢或（C1-4）烷基; R3和R3'是氢，氘或卤素; R6，R7和R8是氢，卤素或氘; m是选自0至4的数字，n是选自0至10的数字，并且p是选自0至10的数字; 条件是n + p至少为1.这些化合物可用作药物，特别是作为抗菌剂。
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4.发明公开PLEUROMUTILIN DERIVATIVES HAVING ANTIBACTERIAL ACTIVITY 有权PLEUROMUTILINDERIVATE MIT ANTIBAKTERIELLER WIRKUNG
公开(公告)号：EP1305282A1
公开(公告)日：2003-05-02
申请号：EP01954024.4
申请日：2001-07-09
发明人： ASCHER, Gerd , BERNER, Heinz
IPC分类号： C07C323/52 , A61K31/10 , A61P31/04
CPC分类号： C07C323/52 , A61K31/215 , C07C2601/14 , C07C2603/99
摘要： A compound selected from 14-O-[(Cycloalkyl-sulfanyl)acetyl]mutilins; 14-O-[Cycloalkyl-alkyl-sulfanyl)acetyl] mutilins; 14-O-[(Cycloalkoxy)acetyl] mutilins; or 14-O[(Cycloalkyl-alkoxy)acetyl] mutilins and its use as a pharmaceutical.
摘要翻译： 选自14-O - [（环烷基 - 硫烷基）乙酰基] mutilins的化合物; 14-O - [（环烷基 - 烷基 - 硫烷基）乙酰基] mutilins; 14-O - [（环烷氧基）乙酰基] mutilins; 和14-O - [（环烷基 - 烷氧基）乙酰基] mutilins及其作为药物的用途。
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5.发明授权PLEUROMUTILIN DERIVATIVES CONTAINING A HYDROXYAMINO- OR ACYLOXYAMINOCYCLOALKYL GROUP 有权含有羟氨基或酰氧基氨基环酰基团的巯基咪唑衍生物
公开(公告)号：EP1896404B1
公开(公告)日：2014-09-17
申请号：EP06741055.5
申请日：2006-06-26
IPC分类号： C07C323/52 , A61K31/16 , A61P17/00
CPC分类号： C07C323/52 , C07C2601/14 , C07C2603/99
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6.发明公开Pleuromutilin derivatives containing a hydroxyamino- or acyloxyaminocycloalkyl group 有权促甲状腺激素羟基氨基酸Acyloxyaminocyclicalkylgruppe
公开(公告)号：EP2298733A3
公开(公告)日：2011-12-14
申请号：EP10009685.8
申请日：2006-06-26
IPC分类号： C07C323/52 , A61K31/16 , A61P17/00
CPC分类号： C07C323/52 , C07C2601/14 , C07C2603/99
摘要： The present invention relates to compounds of general formula I
wherein
R is hydrogen and R 1 is hydroxy or acyloxy, or
R is acyl and R 1 is hydroxy or acyloxy,
X is sulphur, oxygen or NR 10 , wherein R 10 is hydrogen or (C 1-4 )alkyl;
Y is sulphur or oxygen;
R 2 is hydrogen or one or more substituents, e.g. including substituents such as conventional in organic, e.g. (pleuro)mutilin, chemistry;
R4 is hydrogen or (C 1-4 )alkyl;
R 5 is hydrogen or (C 1-4 )alkyl;
R 3 and R 3 ' are hydrogen, deuterium, or halogen;
R 6 , R 7 and R 8 are hydrogen, halogen or deuterium;
m is a number selected from 0 to 4,
n is a number selected from 0 to 10, and
p is a number selected from 0 to 10;
with the proviso that n plus p are at least 1.
These compounds are useful as pharmaceuticals, particularly as antimicrobials.摘要翻译： 本发明涉及通式Ⅰ化合物，其中R为氢，R 1为羟基或酰氧基，或R为酰基，R 1为羟基或酰氧基，X为硫，氧或NR 10，其中R 10为氢或（ C 1-4）烷基; Y是硫或氧; R 2是氢或一个或多个取代基，例如。 包括诸如常规的有机的取代基。 （胸膜）mutilin，化学; R4是氢或（C 1-4）烷基; R 5是氢或（C 1-4）烷基; R 3和R 3'是氢，氘或卤素; R 6，R 7和R 8是氢，卤素或氘; m是选自0至4的数，n是选自0至10的数，p是选自0至10的数; 条件是n加p至少为1.这些化合物可用作药物，特别是作为抗微生物剂。
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7.发明授权PLEUROMUTILIN DERIVATIVES FOR THE TREATMENT OF DISEASES MEDIATED BY MICROBES 有权PLEUROMUTILINDERIVATE用于治疗由微生物介导的疾病
公开(公告)号：EP2137143B1
公开(公告)日：2011-09-07
申请号：EP08714294.9
申请日：2008-03-19
发明人： MANG, Rosemarie , HEILMAYER, Werner , BADEGRUBER, Rudolf , STRICKMANN, Dirk , NOVAK, Rodger , FERENCIC, Mathias , BULUSU, Atchyuta, Rama, Chandra, Murty
IPC分类号： C07C323/52 , A61K31/215 , A61P31/00
CPC分类号： A61K31/5375 , A61K31/215 , A61K31/357 , C07C323/52 , C07C323/61 , C07C2601/14 , C07C2603/99 , C07D295/096 , C07D317/72
摘要： A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m = 0 then R3 is in position 2', and if m = 1 then R3 is on position 1'); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl; R2 is hydrogen or - (C3-6)cycloalkyl, or - unsubstituted (C1-6)alkyl, or - (C1-6)alkyl substituted by one or more of - hydroxy; preferably one or two, - methoxy, - halogen, - (C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatome e. g. selected from N or O, or R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or - with the proviso that R3 is bound to 2' R3 represents -O-(CH2)P-O- with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl.
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8.发明公开PLEUROMUTILIN DERIVATIVES USEFUL AS ANTIBACTERIALS 有权ALS ANTIBAKTERIELLE MITTEL GEEIGNETE PLEUROMUTILINDERIVATE
公开(公告)号：EP1910282A1
公开(公告)日：2008-04-16
申请号：EP06760805.9
申请日：2006-07-26
发明人： MANG, Rosemarie , BERNER, Heinz
IPC分类号： C07C323/52 , A61K31/10 , A61P31/04
CPC分类号： C07C323/52 , C07C2603/99
摘要： The present invention relates to compounds selected from the group consisting of 14-0- [((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or - imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cycloalkylsulfanyl- or - cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl- cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]- mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl- oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)- alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.
摘要翻译： 本发明涉及选自14-O - [（（单或二烷基氨基） - 环烷基硫烷基 - 或 - 环烷基 - 氧基） - 乙酰基 - 硫代乙酰基或 - 亚氨氧基] - 木霉素的化合物，14-O - [（（环烷基 - 或杂环基氨基） - 环烷基硫烷基 - 或 - 环烷基 - 氧基） - 乙酰基 - - 硫代乙酰基或 - 亚氨氧基] - 木兰亭，14-O - [（（杂环-N-基 - 环烷基） 或 - 氧基） - 乙酰基 - 硫代乙酰基或 - 亚氨基氧基] - 木兰林，14-O - [（（（单或二烷基氨基） - 环烷基） - 烷基硫烷基 - 或 - 烷氧基） - 乙酰基， - 硫代乙酰基或 - 亚氨基氧基] - 木兰林，14-O - [（（（环烷基 - 或杂环基氨基） - 环烷基） - 烷基硫烷基 - 或 - 烷氧基） - 乙酰基 - 硫代乙酰基或 - 亚氨基氧基] - 木
坦酚，以及14-O- [ （（杂环-N-基 - 环烷基） - 烷基硫烷基 - 或 - 烷基 - 氧基） - 乙酰基 - 硫代乙酰基或 - 亚氨氧基] - 木兰亭，以及它们作为药物的用途。-
公开(公告)号：EP1910282B1
公开(公告)日：2014-07-02
申请号：EP06760805.9
申请日：2006-07-26
发明人： RIEDL, Rosemarie , BERNER, Heinz
IPC分类号： C07C323/52 , A61K31/10 , A61P31/04
CPC分类号： C07C323/52 , C07C2603/99
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10.发明公开Pleuromutilin derivatives for the treatment of diseases mediated by microbes 有权用于治疗疾病的截短侧耳素衍生物由微生物介导的
公开(公告)号：EP2380874A3
公开(公告)日：2011-12-07
申请号：EP11005863.3
申请日：2008-03-19
发明人： Riedl, Rosemarie , Heilmayer, Werner , Badegruber, Rudolf , Strickmann, Dirk , Novak, Rodger , Ferencic, Matthias , Bulusu, Atchyuta Rama Chandra Murty
IPC分类号： C07C323/52 , A61K31/215 , A61P31/00
CPC分类号： A61K31/5375 , A61K31/215 , A61K31/357 , C07C323/52 , C07C323/61 , C07C2601/14 , C07C2603/99 , C07D295/096 , C07D317/72
摘要： A compound of formula (I)
wherein
n is 0 to 4;
m is 0 or 1 with the proviso that the sulphur atom and R 3 are in vicinal position (if m = 0 then R 3 is in position 2', and if m = 1 then R 3 is on position 1');
R is ethyl or vinyl;
R 1 is hydrogen or (C 1-6 )alkyl,
R 2 is hydrogen or
- (C 3 - 6 )cycloalkyl, or
- unsubstituted (C 1 - 6 )alkyl, or
- (C 1 - 6 )alkyl substituted by one or more of
- hydroxy; preferably one or two,
- methoxy,
- halogen,
- (C 3 - 6 )cycloalkyl, or
R 1 and R 2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatome e. g. selected from N or O, or
R 1 is hydroxy and R 2 is formyl;
R 3 is OH, OR 4 , a halogen atom, or
- with the proviso that R 3 is bound to 2' R 3 represents -O-(CH 2 ) p -O- with p is 2 or 3;
R 4 is unsubstituted (C 1 - 6 )alkyl or (C 3 - 6 )cycloalkyl.
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