CAS: 141388-76-3; (R)-7-(3-Aminoazepan-1-yl)-8-Chloro-1-Cyclopropyl-6-Fluoro-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

📜盐酸贝西沙星置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应 2.5H,以87%的收率获得贝西沙星
参考文献: Acid Salts Of Fluoroquinolone Carboxylic Acid Based Compositions And Methods Of Making And Using The Same[fr] Sels D'Acide De Compositions à Base D'Acide Fluoroquinolone Carboxylique Et Procédés De Fabrication Et D'Utilisation Associés
标题: Acid Salts Of Fluoroquinolone Carboxylic Acid Based Compositions And Methods Of Making And Using The Same[fr] Sels D'Acide De Compositions à Base D'Acide Fluoroquinolone Carboxylique Et Procédés De Fabrication Et D'Utilisation Associés
摘要:本公开涉及制药和化学科学领域.本公开通常涉及治疗剂的合成,制备该类剂的过程,包含该类治疗剂的组合物以及它们的用途.具体而言,该公开涉及药用重要的氟喹诺酮羧酸盐基化学分子[式(i)的化合物],制备这些分子的方法,其组合物,以及将这类分子用作治疗剂的用途.所述的氟喹诺酮羧酸盐基化学分子的酸盐在治疗感染方面具有用途,如耳部感染,中耳炎,包括急性中耳炎,复发性中耳炎,伴有渗出物的中耳炎,慢性中耳炎,慢性化脓性中耳炎,外耳炎(包括急性外耳炎,慢性外耳炎),内耳炎以及其组合.

专利信息

专利号:US-7632944-B2
优先权日:2007-01-24
标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
发明人：HARMS ARTHUR E
权利人:BAUSCH & LOMB
摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.

专利号:US-8227597-B2
优先权日:2006-10-06
标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
发明人：HARMS ARTHUR E
权利人:HARMS ARTHUR E; BAUSCH & LOMB
摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.

专利号:US-8252783-B2
优先权日:2007-01-24
标 题:Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
发明人：HARMS ARTHUR E; ARUL RAMAKRISHNAN; SONI ANIL K
权利人:HARMS ARTHUR E; ARUL RAMAKRISHNAN; SONI ANIL K; BAUSCH & LOMB
摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, Ib, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.

专利号:US-9295731-B2
优先权日:2013-04-01
标题 :Cleavable drug conjugates, compositions thereof and methods of use
发明人：NGUYEN MARK QUANG
权利人:NGUYEN MARK QUANG
摘要:Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.