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    • 4. 发明申请
    • INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS
    • 作为CRTH2受体配体的衍生物
    • WO2010142934A1
    • 2010-12-16
    • PCT/GB2009/050671
    • 2009-06-12
    • PULMAGEN THERAPEUTICS (ASTHMA) LIMITEDHYND, GeorgeMONTANA, John GaryFINCH, HarryARIENZO, RosaAHMED, Shahadat
    • HYND, GeorgeMONTANA, John GaryFINCH, HarryARIENZO, RosaAHMED, Shahadat
    • C07D209/10C07D401/06C07D401/12C07D401/14C07D403/06A61P37/00A61K31/4439C07D409/06C07D409/14C07D413/06C07D417/06C07D417/14A61K31/4178A61K31/422A61K31/404
    • C07D417/14C07D209/10C07D401/06C07D401/12C07D401/14C07D403/06C07D409/06C07D413/06C07D417/06
    • The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: {3-[3-chloro-4-(pyridine-2-sulfonyl)isothiazol-5-ylmethyl]-5-fluoro-2- methylindol-1-yl}acetic acid, [3-(5-benzenesulfonyl-3-methyl-3H-imidazol-4-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid, [3-(5-benzenesulfonyloxazol-4-ylmethyl)-5-fluoro-2-methylindol-1-yl]acetic acid, [3-(3-benzenesulfonyl-4-met ylthiophen-2-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {5-fluoro-2-methyl-3-[2-(pyridin-2-ylsulfamoyl)benzyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[4-methyl-3-(pyridine-2-sulfonyl)thiophen-2- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[3-methyl-5-(pyridine-2-sulfonyl)-3H-imidazol-4- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-3-[2-(3-fluorophenylsulfamoyl)pyridin-3-ylmethyl]-2-methylindol-1- yl}acetic acid, [3-(4-benzenesulfonyloxazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {3-[2-(3-cyanophenylsulfamoyl)benzyl]-5-fluoro-2-methylindol-1-yl}acetic acid, [3-(4-benzenesulfonylthiazol-5-ylmethyl)-5-chloro-2-methyl-indol-1-yl]acetic acid, [3-(4-benzenesulfonyl-2-methylthiazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, and [3-(4-benzenesulfonyl-3-methylisothiazol-5-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid.
    • 以下化合物是可用于治疗呼吸系统疾病的CRTH2拮抗剂:{3- [3-氯-4-(吡啶-2-磺酰基)异噻唑-5-基甲基] -5-氟-2-甲基吲哚-1-基} 乙酸,[3-(5-苯磺酰基-3-甲基-3H-咪唑-4-基甲基)-5-氟-2-甲基吲哚-1-基]乙酸[3-(5-苯磺酰基恶唑-4-基甲基 )-5-氟-2-甲基吲哚-1-基]乙酸,[3-(3-苯磺酰基-4-甲基噻吩-2-基甲基)-5-氟-2-甲基吲哚-1-基]乙酸, {5-氟-2-甲基-3- [2-(吡啶-2-基氨磺酰基)苄基]吲哚-1-基}乙酸{5-氟-2-甲基-3- [4-甲基-3- (吡啶-2-磺酰基)噻吩-2-基甲基]吲哚-1-基}乙酸{5-氟-2-甲基-3- [3-甲基-5-(吡啶-2-磺酰基) 咪唑-4-基甲基]吲哚-1-基}乙酸,{5-氟-3- [2-(3-氟苯基氨磺酰基)吡啶-3-基甲基] -2-甲基吲哚-1-基}乙酸[3 - (4-苯磺酰氧基-5-基甲基)-5-氟-2-甲基吲哚-1-基]乙酸{3- [2-(3-氰基苯基氨磺酰基)苄基] -5-氟-2-甲基吲哚-1-基] 乙酸,[3- (4-苯磺酰基噻唑-5-基甲基)-5-氯-2-甲基 - 吲哚-1-基]乙酸[3-(4-苯磺酰基-2-甲基噻唑-5-基甲基)-5-氟-2- 甲基吲哚-1-基]乙酸和[3-(4-苯磺酰基-3-甲基异噻唑-5-基甲基)-5-氟-2-甲基吲哚-1-基]乙酸。
    • 9. 发明申请
    • ISOINDOLE DERIVATIVES AS ANTIMICROBIAL AGENTS
    • 作为抗微生物剂的ISOINDOLE衍生物
    • WO2007029076A1
    • 2007-03-15
    • PCT/IB2006/002368
    • 2006-08-30
    • RANBAXY LABORATORIES LIMITEDAHMED, ShahadatDAS, BiswajitUPADHYAY, Dilip, J.
    • AHMED, ShahadatDAS, BiswajitUPADHYAY, Dilip, J.
    • C07D209/46C07D209/48C07D403/12C07D401/12C07D417/12A61K31/4035A61K31/4192A61K31/4427A61K31/433A61P31/00
    • C07D209/46C07D209/44C07D209/48C07D401/14C07D403/12C07D417/12
    • Provided herein are substituted aromatic compound of Formula (I), which are tRNA synthetase inhibitors, and hence can be used as antimicrobial agents. Compounds disclosed herein can be used for the treatment or prevention of a condition caused by or contributed to by gram positive, gram negative, anaerobic bacteria or fungal organisms, more particularly against bacterium, for example, Staphylococci, Enterococci, Streptococci, Haemophilus, Moraxalla, Escherichia, Chlamydia, Rickettsiae, Mycoplasm, Legionella, Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae, and fungal organisms, for example, Aspergillus, Blastomyces, Candida, Coccidiodes, Cryptococcus, Epidermophyton, Hendersonula, Histoplasma, Microsporum, Paecilomyces, Paracoccidiodes, Pneumocystis, Trichophyton, or Trichosporium. Processes for the preparation of these compounds, pharmaceutical compositions thereof, and method of treating microbial infections are also provided.
    • 本文提供了取代的式(I)芳族化合物,其为tRNA合成酶抑制剂,因此可用作抗微生物剂。 本文公开的化合物可用于治疗或预防由革兰氏阳性,革兰氏阴性,厌氧细菌或真菌生物引起的或由其贡献的病症,特别是针对细菌,例如葡萄球菌,肠球菌,链球菌,嗜血杆菌,莫萨拉, 大肠杆菌,衣原体,立克次氏体,支原体,军团菌,分枝杆菌,幽门螺杆菌,梭菌属,拟杆菌属,棒状杆菌属,芽孢杆菌属或肠杆菌属,以及真菌生物体,例如曲霉属,布氏酵母属,假丝酵母​​属,椰子球菌属,隐球菌属,表皮癣菌,亨氏球菌,组织胞浆菌, ,副球孢子虫,肺孢子虫,发癣菌或三孢子虫。还提供了用于制备这些化合物的方法,其药物组合物和治疗微生物感染的方法。