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1. (WO2010083725) CEPHALOSPORIN DERIVATIVES CONTAINING SUBSTITUTED NITROGEN-CONTAINING FUSED HETEROCYCLIC RING
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/083725 International Application No.: PCT/CN2010/000086
Publication Date: 29.07.2010 International Filing Date: 20.01.2010
IPC:
C07D 501/57 (2006.01) ,A61K 31/546 (2006.01) ,A61P 31/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
501
Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
14
Compounds having a nitrogen atom directly attached in position 7
16
with a double bond between positions 2 and 3
20
7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
57
with a further substituent in position 7, e.g. cephamycines
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
542
ortho- or peri-condensed with heterocyclic ring systems
545
Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
546
containing further heterocyclic rings, e.g. cephalothin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Applicants:
山东轩竹医药科技有限公司 KBP BIOSCIENCES CO., LTD. [CN/CN]; 中国山东省济南市高新技术开发区天辰大街2518号, Shandong 250101 2518, Tianchen Street High-Tech Development Zone Jinan, Shandong 250101, CN (AllExceptUS)
黄振华 HUANG, Zhenhua [CN/CN]; CN (UsOnly)
宋运涛 SONG, Yuntao [CN/CN]; CN (UsOnly)
Inventors:
黄振华 HUANG, Zhenhua; CN
宋运涛 SONG, Yuntao; CN
Agent:
中国专利代理(香港)有限公司 CHINA PATENT AGENT (H.K.) LTD.; 中国香港特别行政区湾仔港湾道23号鹰君中心22号楼 22/F, Great Eagle Centre 23 Harbour Road Wanchai Hong Kong, CN
Priority Data:
200910014009.720.01.2009CN
200910140527.301.05.2009CN
200910145670.117.05.2009CN
200910146131.X09.06.2009CN
Title (EN) CEPHALOSPORIN DERIVATIVES CONTAINING SUBSTITUTED NITROGEN-CONTAINING FUSED HETEROCYCLIC RING
(FR) DÉRIVÉS DE CÉPHALOSPORINE CONTENANT UN HÉTÉROCYCLE FUSIONNÉ SUBSTITUÉ CONTENANT UN AZOTE
(ZH) 含有取代的含氮稠杂环的头孢菌素衍生物
Abstract:
(EN) Compounds of formula I, pharmaceutically acceptable salts, esters, isomers or solvates thereof, wherein R1 and R2 are independently hydrogen, C1-6 alkyl or amino- protecting group; X is N and the like; R3 is H and the like;ring B is a ring with 3 to 8 members; R4 is H,C1-6 alkyl and the like;R5,R6 and R7 are independently hydrogen, C1-6 alkyl and the like or R6,R7 and the atom which they connect form a ring; n is an integer from 1 to 3;and the dotted line represents single bond or double bond. The compounds have good antimicrobial activities and can be effective ingredients of agents for preventing and/or treating infection of respiratory system, otolaryngological department, bone and arthrosis infection caused by bacterial pathogen.
(FR) La présente invention concerne des composés de formule I, des sels pharmaceutiquement acceptables, des esters, des isomères ou des solvates de ceux-ci, dans laquelle R1 et R2 représentent indépendamment un hydrogène, un alkyle en C1 à C6 ou un groupe protecteur de la fonction amine; X représente N et équivalent; R3 représente H et équivalent; le cycle B est un cycle ayant de 3 à 8 chaînons; R4 représente H, un alkyle en C1 à C6 et équivalents; R5, R6 et R7 représentent indépendamment un hydrogène, un alkyle en C1 à C6 et équivalents ou R6, R7 et l'atome auquel ils sont connectés forment un cycle; n est un entier allant de 1 à 3; et la ligne en pointillés représente une liaison simple ou une double liaison. Les composés ont de bonnes activités antimicrobiennes et peuvent représenter des ingrédients efficaces d'agents de prévention et/ou de traitement d'infections du système respiratoire, des affections otorhinolaryngologiques, des os et de l'arthrose causée par un pathogène bactérien.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)
Also published as:
CN102548999