公开(公告)号：US20070259948A1

公开(公告)日：2007-11-08

申请号：US11498805

申请日：2006-08-04

申请人： Mukund Keshav Gurjar ,  Radhika Dilip Wakharkar ,  Hanumant Bapurao Borate ,  Ramesh Ganesh Kelkar ,  Andiappan Murugan ,  Mohan Anand Chandavarkar ,  Shreerang Vidyadhar Joshi ,  Sharangi Ravindra Vaiude

发明人： Mukund Keshav Gurjar ,  Radhika Dilip Wakharkar ,  Hanumant Bapurao Borate ,  Ramesh Ganesh Kelkar ,  Andiappan Murugan ,  Mohan Anand Chandavarkar ,  Shreerang Vidyadhar Joshi ,  Sharangi Ravindra Vaiude

IPC分类号： A61K31/381 ,  A61K31/341 ,  C07D307/26 ,  C07D317/00 ,  C07D409/02

CPC分类号： C07D307/58 ,  C07D317/30 ,  C07D405/12 ,  C07D409/12

摘要： The present invention relates to compounds of formula (1), its solvates and pharmaceutically acceptable salts having antifungal activity and its pharmaceutical composition comprising an effective amount of compound of formula (1) wherein R is substituted alkyl, alkenyl, aryl, heteroaryl, 2-thienyl, 3-thienyl, halothienyl, haloalkyl, halophenyl, or pyrrolyl; and R1 and R2, each independent of the other, are hydrogen, halogen, or alkoxy. The invention also relates to a process for the preparation of said compounds by contacting the intermediate alcohol, prepared from 1,2-O-isopropylideneglyceraldehyde and substituted phenylacetates, with acid chlorides under appropriate conditions to obtain some of the preferred compounds of the invention.

摘要翻译： 本发明涉及具有抗真菌活性的式（1）化合物，其溶剂合物和药学上可接受的盐，其药物组合物包含有效量的式（1）化合物，其中R是取代的烷基，烯基，芳基，杂芳基， 噻吩基，3-噻吩基，卤代噻吩基，卤代烷基，卤代苯基或吡咯基; 和R 1和R 2各自独立地是氢，卤素或烷氧基。 本发明还涉及一种制备所述化合物的方法，该方法是在适当的条件下使由1,2-碘异丙基甘油醛和取代的苯乙酸酯制备的中间体醇与酰氯接触，以获得本发明的一些优选化合物。

公开(公告)号：US08129369B2

公开(公告)日：2012-03-06

申请号：US13121730

申请日：2009-10-16

申请人： Hanumant Bapurao Borate ,  Suleman Riyasaheb Maujan ,  Sangmeshwer Prabhakar Sawargave ,  Ramesh Ganesh Kelkar ,  Radhika Dilip Wakharkar ,  Mohan Anand Chandavarkar ,  Sharangi Ravinda Vaiude ,  Vinay Anant Joshi

发明人： Hanumant Bapurao Borate ,  Suleman Riyasaheb Maujan ,  Sangmeshwer Prabhakar Sawargave ,  Ramesh Ganesh Kelkar ,  Radhika Dilip Wakharkar ,  Mohan Anand Chandavarkar ,  Sharangi Ravinda Vaiude ,  Vinay Anant Joshi

IPC分类号： C07D413/06 ,  C07D417/06 ,  A61K31/423 ,  A61K31/536

CPC分类号： C07D417/06 ,  C07D413/06

摘要： The present invention discloses novel compounds of the Formula (1), comprising benzothiazinone, benzoxazinone or benzoxazolinone moieties having antifungal activity, method for preparing these compounds and the use of these compounds as antifungal agents in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.

摘要翻译： 本发明公开了具有抗真菌活性的苯并噻嗪酮，苯并恶嗪酮或苯并恶唑啉酮部分的新型式（1）化合物，其制备方法以及这些化合物作为抗真菌剂在预防和治疗真菌感染中的用途，以及含有 这些新化合物。