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1. 发明申请

WO2008008480A3 NITROHETEROARYL-CONTAINING RIFAMYCIN DERIVATIVES 审中-公开
标题翻译：含有硝基的含有RIFAMYCIN衍生物
公开(公告)号：WO2008008480A3
公开(公告)日：2008-03-13
申请号：PCT/US2007015970
申请日：2007-07-12
申请人： CUMBRE PHARMACEUTICALS INC , DING CHARLES Z , KIM IN HO , WANG JIANCHENG , MA ZHENKUN , JIN YAFEI , COMBRINK KEITH D , LU GENLIANG , LYNCH A SIMON
发明人： DING CHARLES Z , KIM IN HO , WANG JIANCHENG , MA ZHENKUN , JIN YAFEI , COMBRINK KEITH D , LU GENLIANG , LYNCH A SIMON
IPC分类号： C07D498/08 , A61K31/395 , C07D498/18 , C07D498/22 , C07D519/00
CPC分类号： C07D498/18 , C07D498/08 , C07D498/22 , C07D519/00
摘要： Substituted rifamycin derivatives of formula I uses thereof and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.or their pharmaceutically acceptable salt thereof, wherein R 1 is a hydrogen or acetyl group, G is a structure of formula (II, III, IV or V): wherein, in formula (II, III, IV or V), Q is N- or CR 2 . which is bonded to a linkage, group "L", which in turn is bonded to a structure A-NO 2 ,and R 2 is a group selected from hydrogen, substituted or unsubstituted (C 1 -C 6 )alkyl, aryl, heteroaryl, or heterocycloalkyl group; The structure A-NO 2 is a structural formula (VI1 VII, VIII or IX): wherein Y is a bond which is bonded to linkage group "L", defined as above; and Z is a carbon (-CR 7 R 8 -), carbonyl (-C(O)-), amide (-C(O)N-), sulfonamide (-S(O 2 )N-), or a heteroatom selected from N, O, S, SO or SO 2 ; wherein R 5 , R 6 , R 7 , and R 8 are independently a group selected from hydrogen, substituted or unsubstituted (C 1 -C 6 )alkyl, aryl. heteroaryl. or heterocycloalkyl group; R 5 and R 6 R 7 and R 8 can join together to form a five to seven-member ring system optionally containing one to three heteroatoms.
摘要翻译：公开了其取代的利福霉素衍生物的用途，并且公开了含有利福霉素衍生物的药物组合物。还公开了合成这些取代的利福霉素衍生物的方法。利福霉素衍生物具有抗细菌活性，并且在治疗细菌性疾病中对许多人和兽医病原体有效。或其药学上可接受的盐，其中R 1是氢或乙酰基，G 是式（II，III，IV或V）的结构：其中，在式（II，III，IV或V）中，Q是N-或CR 2。其键合到键，组“L”，其又结合于结构A-NO 2，并且R 2是选自氢，取代的基团或未取代的（C 1 -C 6 -C 6）烷基，芳基，杂芳基或杂环烷基; 结构A-NO 2结构式（VI1 VII，VIII或IX）：其中Y是与上述定义的连接基团“L”键合的键; （C（O） - ），酰胺（-C（O）N-），磺酰胺（C（O）（-S（O）2 - ）N-）或选自N，O，S，SO或SO 2的杂原子; 其中R 5，R 6，R 7和R 8独立地是选自氢，取代的或未取代的（C 1 -C 6 -C 6）烷基，芳基。杂。或杂环烷基; R 5和R 6 R 7和R 8可以连接在一起以形成五至七元环系统任选地含有一至三个杂原子。

2. 发明申请

WO2009064792A1 QUINOLONE CARBOXYLIC ACID-SUBSTITUTED RIFAMYCIN DERIVATIVES 审中-公开
标题翻译：喹诺酮羧酸取代的赖氨明衍生物
公开(公告)号：WO2009064792A1
公开(公告)日：2009-05-22
申请号：PCT/US2008/083246
申请日：2008-11-12
申请人： CUMBRE PHARMACEUTICALS INC. , DING, Charles, Z. , JIN, Yafei , COMBRINK, Keith , KIM, In, Ho
发明人： DING, Charles, Z. , JIN, Yafei , COMBRINK, Keith , KIM, In, Ho
IPC分类号： C07D491/20 , C07D498/16 , A61K31/498 , A61K31/5383
CPC分类号： C07D491/20 , C07D498/16
摘要： The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.
摘要翻译：化合物包括取代的利福霉素衍生物，其中喹诺酮羧酸药效团与苯并恶嗪利福霉素或螺哌啶利多霉素共价键合。利福霉素衍生物可用作抗微生物剂，并且对许多人和兽医革兰氏阳性和革兰氏阴性病原体有效。本发明化合物的优点在于利福霉素和喹诺酮类抗菌药代动力剂与匹配的药代动力学共同输送到感兴趣的靶向病原体。同时向目标病原体递送多种抗菌药代动力，最大限度地实现协同作用，并最大限度地减少给予抗生素的耐药性。

3. 发明申请

WO2008008480A2 NITROHETEROARYL-CONTAINING RIFAMYCIN DERIVATIVES 审中-公开
标题翻译：含有硝基的含有RIFAMYCIN衍生物
公开(公告)号：WO2008008480A2
公开(公告)日：2008-01-17
申请号：PCT/US2007/015970
申请日：2007-07-12
申请人： CUMBRE PHARMACEUTICALS INC. , DING, Charles, Z. , KIM, In, Ho , WANG, Jiancheng , MA, Zhenkun , JIN, Yafei , COMBRINK, Keith, D. , LU, Genliang , LYNCH, A., Simon
发明人： DING, Charles, Z. , KIM, In, Ho , WANG, Jiancheng , MA, Zhenkun , JIN, Yafei , COMBRINK, Keith, D. , LU, Genliang , LYNCH, A., Simon
IPC分类号： C07D498/08 , C07D498/18 , C07D498/22 , C07D519/00 , A61K31/395
CPC分类号： C07D498/18 , C07D498/08 , C07D498/22 , C07D519/00
摘要： Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.
摘要翻译：公开了其中硝基咪唑，硝基噻唑或硝基呋喃药效团与利福霉素共价结合的取代的利福霉素衍生物，使用利福霉素衍生物的方法和含有利福霉素衍生物的药物组合物。还公开了合成这些取代的利福霉素衍生物的方法。利福霉素衍生物具有抗菌活性，并且在治疗细菌性疾病中对许多人和兽医病原体有效。

4. 发明专利

CA2574301A1 (R/S) RIFAMYCIN DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS 未知
公开(公告)号：CA2574301A1
公开(公告)日：2006-02-02
申请号：CA2574301
申请日：2005-07-21
申请人： CUMBRE PHARMACEUTICALS INC
发明人： MINOR KEITH P , HARRAN SUSAN , KIM IN HO , HE YONG , LONGGOOD JAMIE CAROL , MA ZHENKUN , COMBRINK KEITH D , DING CHARLES Z , JIN YAFEI , LI JING
IPC分类号： C07D498/08 , A61K31/4709 , A61P31/04

5. 发明专利

AT427311T 未知
公开(公告)号：AT427311T
公开(公告)日：2009-04-15
申请号：AT05791212
申请日：2005-07-21
申请人： CUMBRE PHARMACEUTICALS INC
发明人： DING CHARLES , MA ZHENKUN , LI JING , HARRAN SUSAN , HE YONG , MINOR KEITH , KIM IN , LONGGOOD JAMIE , JIN YAFEI , COMBRINK KEITH
IPC分类号： C07D498/08 , A61K31/4709 , A61P31/04

6. 发明专利

CA2574301C (R/S) RIFAMYCIN DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS 未知
公开(公告)号：CA2574301C
公开(公告)日：2013-09-10
申请号：CA2574301
申请日：2005-07-21
申请人： CUMBRE PHARMACEUTICALS INC
发明人： DING CHARLES Z , MA ZHENKUN , LI JING , HARRAN SUSAN , HE YONG , MINOR KEITH P , KIM IN HO , LONGGOOD JAMIE CAROL , JIN YAFEI , COMBRINK KEITH D
IPC分类号： C07D498/08 , A61K31/4709 , A61P31/04
摘要： Rifamycin derivatives having the following structure of general formula (I) (both hydroquinone and corresponding quinone (C1-C4) forms): or its salts, hydrates or prodrugs thereof; wherein a preferred R1 comprises hydrogen or acetyl and a prefered R2 comprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.

7. 发明专利

CA2574307A1 RIFAMYCIN DERIVATIVES FOR TREATING MICROBIAL INFECTIONS 未知
公开(公告)号：CA2574307A1
公开(公告)日：2006-02-02
申请号：CA2574307
申请日：2005-07-21
申请人： CUMBRE PHARMACEUTICALS INC
发明人： LI JING , MA ZHENKUN , MINOR KEITH P , KIM IN HO , DING CHARLES Z , HARRAN SUSAN , HE YONG , LONGGOOD JAMIE CAROL , JIM YAFEI , COMBRINK KEITH D
IPC分类号： C07D498/08 , A61K31/4709 , A61P31/04

8. 发明专利

AU2005267054A1 (R/S) rifamycin derivatives, their preparation and pharmaceutical compositions 未知
公开(公告)号：AU2005267054A1
公开(公告)日：2006-02-02
申请号：AU2005267054
申请日：2005-07-21
申请人： CUMBRE PHARMACEUTICALS INC
发明人： HARRAN SUSAN , DING CHARLES Z , LI JING , KIM IN HO , JIN YAFEI , HE YONG , MA ZHENKUN , MINOR KEITH P , COMBRINK KEITH D , LONGGOOD JAMIE CAROL
IPC分类号： C07D498/08 , A61K31/4709 , A61P31/04

9. 发明专利

DE602005013671D1 未知
公开(公告)号：DE602005013671D1
公开(公告)日：2009-05-14
申请号：DE602005013671
申请日：2005-07-21
申请人： CUMBRE PHARMACEUTICALS INC
发明人： DING CHARLES Z , MA ZHENKUN , LI JING , HARRAN SUSAN , HE YONG , MINOR KEITH P , KIM IN HO , LONGGOOD JAMIE CAROL , JIN YAFEI , COMBRINK KEITH D
IPC分类号： C07D498/08 , A61K31/4709 , A61P31/04

10. 发明授权

US07238694B2 Rifamycin imino derivatives effective against drug-resistant microbes 有权
标题翻译：对抗耐药性微生物有效的利福霉素亚氨基衍生物
公开(公告)号：US07238694B2
公开(公告)日：2007-07-03
申请号：US11034279
申请日：2005-01-12
申请人： Charles Z. Ding , Yafei Jin , Jamie C. Longgood , Zhenkun Ma , Jing Li , In Ho Kim , Keith P. Minor , Susan Harran
发明人： Charles Z. Ding , Yafei Jin , Jamie C. Longgood , Zhenkun Ma , Jing Li , In Ho Kim , Keith P. Minor , Susan Harran
IPC分类号： C07D498/08 , C07D519/00 , A61K31/4709 , A61K31/496 , A61P31/04
CPC分类号： C07D498/08 , C07D519/00
摘要： The present invention relates to rifamycin 3-iminomethylenyl (—CH═N—) derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. The claimed rifamycin derivative has a rifamycin moiety covalently linked to a linker through an iminomethylenyl (—CH═N—) group at the C-3 carbon of the rifamycin moiety and the linker is, in turn, covalently linked to a quinolone structure or its pharmacophore within the DNA gyrase and topoisomerase IV inhibitor family. The inventive rifamycins are novel and exhibit activity against both rifampin and ciprofloxacin-resistant microorganisms.
摘要翻译：本发明涉及具有抗菌活性的利福霉素3-亚氨基亚甲基（-CH-N-）衍生物，其包括抗药性微生物的活性。所要求的利福霉素衍生物具有通过利莫霉素部分的C-3碳上的亚氨基亚甲基（-CH-N-）基团与连接体共价连接的利福霉素部分，并且连接体又与喹诺酮结构共价连接或其 DNA促旋酶和拓扑异构酶IV抑制剂家族内的药效团。本发明的利福霉素是新颖的，并且表现出抵抗利福平和环丙沙星抗性微生物的活性。

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