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1. 发明授权

US09321788B2 Tricyclic antibiotics 有权
公开(公告)号：US09321788B2
公开(公告)日：2016-04-26
申请号：US14124144
申请日：2012-06-11
申请人： Berangere Gaucher , Franck Hubert Danel , Tong Xie , Lin Xu
发明人： Berangere Gaucher , Franck Hubert Danel , Tong Xie , Lin Xu
IPC分类号： C07D498/04 , C07D491/14 , C07D491/147 , C07D491/052 , C07D495/04
CPC分类号： C07D498/04 , C07D491/052 , C07D491/14 , C07D491/147 , C07D495/04
摘要： The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.

2. 发明申请

US20140235855A1 Tricyclic Antibiotics 有权
标题翻译：三环抗生素
公开(公告)号：US20140235855A1
公开(公告)日：2014-08-21
申请号：US14124144
申请日：2012-06-11
申请人： Berangere Gaucher , Franck Hubert Danel , Tong Xie , Lin Xu
发明人： Berangere Gaucher , Franck Hubert Danel , Tong Xie , Lin Xu
IPC分类号： C07D498/04 , C07D491/052 , C07D495/04 , C07D491/147
CPC分类号： C07D498/04 , C07D491/052 , C07D491/14 , C07D491/147 , C07D495/04
摘要： Compounds of formula (I), wherein A1 represents —O—, —S— or —CH2—; A2 represents —CH2— or —O—; A3 represents C3-C8-cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, —C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; m is 0 or 1; n is 1; the —(CH2)n— group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.
摘要翻译：式（I）化合物，其中A 1表示-O - ， - S-或-CH 2 - ; A2表示-CH2-或-O-; A3表示C3-C8-亚环烷基; 饱和或不饱和的4至8元杂环基与1,2或3个选自氮或氧的杂原子，该基团A3为未取代或取代的; A4表示C1-C4亚烷基，-C（= O） - ; G表示未取代或取代的芳基或杂芳基; X1表示氮原子或CR1; R1表示氢原子或卤素原子; R1表示氢原子; m为0或1; n为1; - （CH 2）n - 基团是未取代的或取代的; p为0或1; 或其药学上可接受的盐对于用作治疗细菌感染的药物是有价值的。

3. 发明授权

US08927541B2 Tricyclic antibiotics 有权
标题翻译：三环类抗生素
公开(公告)号：US08927541B2
公开(公告)日：2015-01-06
申请号：US13511292
申请日：2010-12-17
申请人： Bérangère Gaucher , Franck Hubert Danel , XiaoHu Tang , Tong Xie , Lin Xu
发明人： Bérangère Gaucher , Franck Hubert Danel , XiaoHu Tang , Tong Xie , Lin Xu
IPC分类号： C07D491/052 , C07D498/14 , A61K31/536 , A61K31/5365
CPC分类号： C07D513/04 , C07D491/04 , C07D491/052 , C07D491/147 , C07D495/04 , C07D498/04 , C07D498/14
摘要： The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
摘要翻译：本发明涉及式I的抗菌化合物：其中所有可变取代基如本文所述定义，其可用于治疗细菌感染。

4. 发明申请

US20120245345A1 TRICYCLIC ANTIBIOTICS 有权
标题翻译： TRICYCLIC抗生素
公开(公告)号：US20120245345A1
公开(公告)日：2012-09-27
申请号：US13511292
申请日：2010-12-17
申请人： Bérangère Gaucher , Franck Hubert Danel , XiaoHu Tang , Tong Xie , Lin Xu
发明人： Bérangère Gaucher , Franck Hubert Danel , XiaoHu Tang , Tong Xie , Lin Xu
IPC分类号： C07D491/052 , C07D498/14 , C07D495/04 , C07D513/04
CPC分类号： C07D513/04 , C07D491/04 , C07D491/052 , C07D491/147 , C07D495/04 , C07D498/04 , C07D498/14
摘要： Compound of formula (I): wherein A1 represents —O—, —S— or —N—R3; A2 represents —CH2—, —O—, —N—R4, —C(═O)— or —CH(O—R4)—; A3 represents C3-C8cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, C2-C4alkenylene, >C═O or a group selected from —C2H4NH—, —C2H4O—, and —C2H4S— being linked to the adjacent NR5-group via the carbon atom; and G represents aryl or heteroaryl, which is un-substituted or substituted and R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylcarbonyloxy, C1-C6alkylsulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted; R3, R4 and R5 independently of one another, represent hydrogen or C1-C6alkyl; X1 and X2 independently of one another, represent a nitrogen atom or CR2, with the proviso that at least one of X1 and X2 represents a nitrogen atom; m is 1; and the (CH2)m moiety is optionally substituted by C1-C4alkyl; halogen, carboxy, hydroxy, C1-C4alkoxy, C1-C4-alkylcarbonyloxy, amino, mono- or di-(C1-C4alkyl)amino or acylamino n is 0, 1 or 2 or pharmaceutically acceptable salt thereof are valuable for use as a medicament for the treatment of bacterial infections.
摘要翻译：式（I）化合物：其中A1表示-O - ， - S-或-N-R 3; A 2表示-CH 2 - ， - O - ， - N-R 4，-C（= O） - 或-CH（O-R 4） - ; A3表示C3-C8亚环烷基; 饱和和不饱和的4至8元杂环基与1,2或3个选自氮，氧和硫的杂原子，该基团A3为未取代或取代的; A4表示C1-C4亚烷基，C2-C4亚烯基，> C = O或选自-C2H4NH-，-C2H4O-和-C2H4S-的基团，其通过碳原子连接到相邻的NR5-基团; 并且G表示未取代或取代的芳基或杂芳基，R 1和R 2彼此独立地表示氢或选自羟基，卤素，巯基，氰基，硝基，C 1 -C 6烷基，C 1 -C 6烷氧基， C 1 -C 6烷硫基，C 1 -C 6烷基羰基氧基，C 1 -C 6烷基磺酰氧基，C 1 -C 6杂烷基羰氧基，C 5 -C 6杂环羰基氧基，C 1 -C 6杂烷氧基，其中杂烷基，杂烷氧基或杂环基包含1,2或3个选自氮，氧和硫的杂原子，其中烷基部分是未取代的或进一步取代的; R 3，R 4和R 5彼此独立地表示氢或C 1 -C 6烷基; X 1和X 2彼此独立地表示氮原子或CR 2，条件是X 1和X 2中的至少一个表示氮原子; m为1; （CH 2）m部分任选被C 1 -C 4烷基取代; 卤素，羧基，羟基，C 1 -C 4烷氧基，C 1 -C 4烷基羰基氧基，氨基，单 - 或二 - （C 1 -C 4烷基）氨基或酰氨基n是0,1或2或其药学上可接受的盐对于用作药物是有价值的用于治疗细菌感染。

5. 发明授权

US08716280B2 Bicyclic antibiotics 有权
标题翻译：双环抗生素
公开(公告)号：US08716280B2
公开(公告)日：2014-05-06
申请号：US13145323
申请日：2010-01-21
申请人： Berangere Gaucher , Franck Hubert Danel , Patrick Roussel
发明人： Berangere Gaucher , Franck Hubert Danel , Patrick Roussel
IPC分类号： C07D498/04 , C07D413/04 , A61K31/5415 , A61K31/5383
CPC分类号： C07D513/04 , C07D215/20 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04 , C07D519/00
摘要： The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
摘要翻译：式I的抗菌化合物，其中X 1，X 3; X 4和X 6各自独立地表示氮原子或CR 2，条件是X 1，X 3; X4和X6表示氮原子; X代表C-H，C-（C 1 -C 6烷基），C-（C 1 -C 6烷氧基），C-卤素，C-COOH; X 5表示C-H或C-（C 1 -C 6烷基），C-卤素; A1，A2，A3，R1和R4表示各种取代基，G表示未取代或取代的芳基或杂芳基，哪种化合物对病原菌表现出良好的活性。

6. 发明申请

US20120040957A1 Novel Bicyclic Antibiotics 有权
公开(公告)号：US20120040957A1
公开(公告)日：2012-02-16
申请号：US13145323
申请日：2010-01-21
申请人： Berangere Gaucher , Franck Hubert Danel , Patrick Roussel
发明人： Berangere Gaucher , Franck Hubert Danel , Patrick Roussel
IPC分类号： A61K31/5415 , C07D498/04 , C07D413/14 , C07D471/04 , A61P31/04 , C07D405/12 , A61K31/5383 , A61K31/498 , A61K31/4375 , A61K31/4709 , C07D417/14 , C07D417/12
CPC分类号： C07D513/04 , C07D215/20 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D498/04 , C07D519/00
摘要： Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; R1 and R2, independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, carboxy, amino, C1-C6alkylamino, di(C1-C6alkyl)amino, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylamino-carbonyloxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkylcarbonyloxy, C1-C6alkyl-sulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclyl-carbonyloxy, C1-C6heteroalkyl, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted by halogeno, cyano, hydroxy, C1-C4alkoxy, C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, unsubstituted or substituted phenoxy or phenylcarbonyl, unsubstituted or substituted C5-C6heterocyclyl or carboxy; A1 represents a divalent group of one of the formulae —O—(CH2)m—(CH2)—, —S—(CH2)m—(CH2)— or —(C═O)O—(CH2)m—(CH2)—, wherein the (CH2)m moiety is optionally substituted by C1-C4alkyl, C2-C4alkenyl, C3-C6cycloalkyl, C3-C6cycloalkylmethyl, morpholinomethyl, halogen, carboxy, hydroxy, C1-C4alkoxy; C1-C4alkoxyC1-C4alkyl, C1-C4alkoxy(C1-C4alkylenoxy)C1-C4alkyl, benzyloxyC1-C4alkyl, amino, mono- or di-(C1-C4alkyl)amino or acylamino, in which substituents the alkyl moieties can be further substituted by 1 or more fluoro atoms m is 0, 1 or 2, provided that the nunber of atoms in the direct chain between the two terminal valencies of A1 is at least 3, which group A1 is linked to A2 via the terminal (CH2)-moiety; A2 is a group selected from C3-C8 cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A2 is unsubstituted or substituted; R4 represents hydrogen or C1-C4 alkyl; A3 represents C1-C4 alkylene, C2-C4 alkenylene, >C═O, —C(O)C1-C3 alkylene-, —C(═O)NH—, or a group selected from —C2H4NH—, —C2H4O—, and —C2H4S— being linked to the adjacent NR4-group via the carbon atom; and G represents aryl or heteroaryl, which is unsubstituted or substituted and n is 0, 1 or 2; or a pharmaceutically acceptable salts, hydrates or solvates thereof are valuable antibacterial agents.

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