公开(公告)号：US20110183968A1

公开(公告)日：2011-07-28

申请号：US13121730

申请日：2009-10-16

申请人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmeshwer Prabhaker Sawargave ,  Ramesh Ganesh Kelkar ,  Radhike Dilip Wakharkar ,  Sharangi Ravindra Vaiude ,  Vinay Anant Joshi

发明人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmeshwer Prabhaker Sawargave ,  Ramesh Ganesh Kelkar ,  Radhike Dilip Wakharkar ,  Sharangi Ravindra Vaiude ,  Vinay Anant Joshi

IPC分类号： A61K31/5415 ,  C07D417/06 ,  A61P31/10 ,  C07D413/06 ,  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。

公开(公告)号：US09512087B2

公开(公告)日：2016-12-06

申请号：US13994323

申请日：2012-04-04

申请人： Hanumant Bapurao Borate ,  Sangmeshwer Prabhakar Sawargave ,  Subhash Prataprao Chavan ,  Mohan Anand Chandavarkar ,  Ramkrishnan Ramachaandran Iyer ,  Amit Chandrakant Tawte ,  Deepali Damodar Rao

发明人： Hanumant Bapurao Borate ,  Sangmeshwer Prabhakar Sawargave ,  Subhash Prataprao Chavan ,  Mohan Anand Chandavarkar ,  Ramkrishnan Ramachaandran Iyer ,  Amit Chandrakant Tawte ,  Deepali Damodar Rao

IPC分类号： C07D249/08 ,  C07D249/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D249/08 ,  C07D249/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： Disclosed herein are novel antifungal compounds of Formula 1, containing fluconazole pharmacophore moieties coupled with other moieties including aryl enones and chalcones and pharmaceutically acceptable salts thereof, methods for preparing these compounds and pharmaceutical preparations containing these novel compounds for prevention and treatment of fungal infections.

公开(公告)号：US20140249194A1

公开(公告)日：2014-09-04

申请号：US14264574

申请日：2014-04-29

申请人： Hanumant Bapurao BORATE ,  SANGESHWER PRABHAKAR SAWARGAVE ,  SUBHASH PRATAPRAO CHAVAN ,  MOHAN ANAND CHANDAVARKAR ,  RAMAKRISHNAN RAMACAHNDRAN IYER ,  AMIT CHANDRAKANT TAWTE ,  DEEPALI DAMODAR RAO

发明人： Hanumant Bapurao BORATE ,  SANGESHWER PRABHAKAR SAWARGAVE ,  SUBHASH PRATAPRAO CHAVAN ,  MOHAN ANAND CHANDAVARKAR ,  RAMAKRISHNAN RAMACAHNDRAN IYER ,  AMIT CHANDRAKANT TAWTE ,  DEEPALI DAMODAR RAO

IPC分类号： C07D409/12

CPC分类号： C07D409/12 ,  C07B2200/07

摘要： The invention discloses optically active compounds of Formula (1a) or Formula (1b), wherein R1 and R2 are independently selected from the group consisting of hydrogen and a halogen selected from the group consisting of fluorine, chlorine, bromine, and iodine; and wherein (a) R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group having a linear or branched chain having 1 to 20 carbon atoms, or (b) R3 and R4 together form a cycloalkyl ring having 3 to 10 carbon atoms fused to the thiophene ring; and wherein R5 is CN or COOR′, where R′ is methyl or ethyl. The compounds of Formula (1a) or Formula (1b) may be used in pharmaceutical compositions for treating fungal infections.

摘要翻译： 本发明公开了式（1a）或式（1b）的光学活性化合物，其中R 1和R 2独立地选自氢和选自氟，氯，溴和碘的卤素; 并且其中（a）R 3和R 4独立地选自氢和具有1至20个碳原子的直链或支链的烷基，或（b）R 3和R 4一起形成具有3至10个 与噻吩环稠合的碳原子; 并且其中R 5是CN或COOR'，其中R'是甲基或乙基。 式（1a）或式（1b）的化合物可用于治疗真菌感染的药物组合物中。

公开(公告)号：US08324227B2

公开(公告)日：2012-12-04

申请号：US12742211

申请日：2008-09-05

申请人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmesher Prabhakar Sawargave ,  Sheerang Vidhyadhar Joshi ,  Sharangi Vaiude ,  Mohan Anand Chandavarkar

发明人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmesher Prabhakar Sawargave ,  Sheerang Vidhyadhar Joshi ,  Sharangi Vaiude ,  Mohan Anand Chandavarkar

IPC分类号： C07D495/04 ,  A61K31/519 ,  A01N43/54

摘要： The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.

摘要翻译： 本发明公开了含有噻吩并[2,3-d]嘧啶-4（3H） - 酮部分及其药学上可接受的盐的式（1）的新化合物，制备这些化合物的方法，这些化合物在 预防和治疗真菌感染，以及含有这些新化合物的药物制剂。

公开(公告)号：US09181269B2

公开(公告)日：2015-11-10

申请号：US14004869

申请日：2011-05-31

申请人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmeshwer Prabhkara Sawargave ,  Subhash Prataprao Chavan ,  Mohan Anand Chandavarkar ,  Ramkrishnan Ramachandran Iyer ,  Vikas Vasant Nawathye ,  Gajanan Jalindar Chavan ,  Amit Chandrakant Tawte ,  Deepali Damodar Rao

发明人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmeshwer Prabhkara Sawargave ,  Subhash Prataprao Chavan ,  Mohan Anand Chandavarkar ,  Ramkrishnan Ramachandran Iyer ,  Vikas Vasant Nawathye ,  Gajanan Jalindar Chavan ,  Amit Chandrakant Tawte ,  Deepali Damodar Rao

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D491/00 ,  C07D495/00 ,  C07D495/04

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The present invention discloses novel enantiomeric antifungal compounds of Formula (1a) and Formula (1b) containing thieno-[2,3-d]Jpyrimidin-4(3H)-one moiety and pharmaceutically acceptable salts thereof, method of preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these compounds.

摘要翻译： 本发明公开了含有噻吩并[2,3-d]嘧啶-4（3H） - 酮部分的式（1a）和式（1b）的新型对映体抗真菌化合物及其药学上可接受的盐，制备这些化合物的方法 这些化合物在预防和治疗真菌感染中的应用，以及含有这些化合物的药物制剂。

公开(公告)号：US08236840B2

公开(公告)日：2012-08-07

申请号：US13058358

申请日：2009-10-01

申请人： Hanumant Bapurao Borate ,  Sangmeshwer Prabhakar Sawargave ,  Suleman Riyajsaheb Maujan ,  Mohan Anand Chandavarkar ,  Sharangi Ravinda Vaiude ,  Vinay Anant Joshi

发明人： Hanumant Bapurao Borate ,  Sangmeshwer Prabhakar Sawargave ,  Suleman Riyajsaheb Maujan ,  Mohan Anand Chandavarkar ,  Sharangi Ravinda Vaiude ,  Vinay Anant Joshi

IPC分类号： A61K31/41 ,  A61K31/4196 ,  A61P31/10 ,  C07D409/12

CPC分类号： C07D409/12

摘要： The present invention discloses novel compounds of the Formula (1), containing thiophene moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.

摘要翻译： 本发明公开了含有噻吩部分及其药学上可接受的盐的式（1）的新化合物，制备这些化合物的方法，这些化合物在预防和治疗真菌感染中的用途，以及含有这些新化合物的药物制剂。

公开(公告)号：US20140011818A1

公开(公告)日：2014-01-09

申请号：US14004869

申请日：2011-05-31

申请人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmeshwer Prabhkara Sawargave ,  Subhash Prataprao Chavan ,  Mohan Anand Chandavarkar ,  Ramkrishnan Ramachandran Iyer ,  Vikas Vasanat Nawathye ,  Gajanan Jalindar Chavan ,  Amit Chandrakant Tawte ,  Deepali Damodar Rao

发明人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmeshwer Prabhkara Sawargave ,  Subhash Prataprao Chavan ,  Mohan Anand Chandavarkar ,  Ramkrishnan Ramachandran Iyer ,  Vikas Vasanat Nawathye ,  Gajanan Jalindar Chavan ,  Amit Chandrakant Tawte ,  Deepali Damodar Rao

IPC分类号： C07D495/04

CPC分类号： C07D495/04 ,  A61K31/519

摘要： The present invention discloses novel enantiomeric antifungal compounds of Formula (1a) and Formula (1b) containing thieno-[2,3-d]Jpyrimidin-4(3H)-one moiety and pharmaceutically acceptable salts thereof, method of preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these compounds.

摘要翻译： 本发明公开了含有噻吩并[2,3-d]嘧啶-4（3H） - 酮部分的式（1a）和式（1b）的新型对映体抗真菌化合物及其药学上可接受的盐，制备这些化合物的方法 这些化合物在预防和治疗真菌感染中的应用，以及含有这些化合物的药物制剂。

公开(公告)号：US20130303579A1

公开(公告)日：2013-11-14

申请号：US13994323

申请日：2012-04-04

申请人： Hanumant Bapurao Borate ,  Sangmeshwer Prabhakar Sawargave ,  Subhash Prataprao Chavan ,  Mohan Anand Chandavarkar ,  Ramkrishnan Ramachaandran Iyer ,  Amit Chandrakant Tawte ,  Deepali Damodar Rao

发明人： Hanumant Bapurao Borate ,  Sangmeshwer Prabhakar Sawargave ,  Subhash Prataprao Chavan ,  Mohan Anand Chandavarkar ,  Ramkrishnan Ramachaandran Iyer ,  Amit Chandrakant Tawte ,  Deepali Damodar Rao

IPC分类号： C07D249/08 ,  C07D403/12 ,  C07D409/12

CPC分类号： C07D249/08 ,  C07D249/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： Disclosed herein are novel antifungal compounds of Formula 1, containing fluconazole pharmacophore moieties coupled with other moieties including aryl enones and chalcones and pharmaceutically acceptable salts thereof, methods for preparing these compounds and pharmaceutical preparations containing these novel compounds for prevention and treatment of fungal infections.

摘要翻译： 本文公开了新颖的式1的抗真菌化合物，其含有与其它部分（包括芳基酮和查尔酮及其药学上可接受的盐）偶联的氟康唑药效团部分，制备这些化合物的方法和含有这些用于预防和治疗真菌感染的新化合物的药物制剂。

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。

公开(公告)号：US20100273815A1

公开(公告)日：2010-10-28

申请号：US12742211

申请日：2008-09-05

申请人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmesher Prabhakar Sawargave ,  Sheerang Vidhyadhar Joshi ,  Sharangi Vaiude ,  Mohan Anand Chandavarkar

发明人： Hanumant Bapurao Borate ,  Suleman Riyajsaheb Maujan ,  Sangmesher Prabhakar Sawargave ,  Sheerang Vidhyadhar Joshi ,  Sharangi Vaiude ,  Mohan Anand Chandavarkar

IPC分类号： A01N43/54 ,  C07D495/04 ,  A01P3/00

摘要： The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.

摘要翻译： 本发明公开了含有噻吩并[2,3-d]嘧啶-4（3H） - 酮部分及其药学上可接受的盐的式（1）的新化合物，制备这些化合物的方法，这些化合物在 预防和治疗真菌感染，以及含有这些新化合物的药物制剂。