公开(公告)号：US06277879B1

公开(公告)日：2001-08-21

申请号：US09173143

申请日：1998-10-15

Applicant: Ze-Qi Xu ,  Michael T. Flavin ,  David Zembower

Inventor： Ze-Qi Xu ,  Michael T. Flavin ,  David Zembower

IPC: A61K3135

CPC classification number: C07D493/04 ,  A61K45/06 ,  C07D311/16 ,  C07D493/14

Abstract: Calanolide analogues that demonstrate potent antiviral activity against many viruses are provided. Also provided is a method of using calanolide analogues for treating or preventing viral infections. The calanolide analogues provided are obtained via syntheses employing chromene 4 and chromanone 7 as key intermediates.

Abstract translation: 提供了表现出针对许多病毒的有效抗病毒活性的卡立奈德类似物。 还提供了使用丙烯酰胆碱类似物治疗或预防病毒感染的方法。 提供的甘露糖苷类似物通过使用色烯4和苯并二氢吡喃酮7作为关键中间体的合成获得。

公开(公告)号：US5981770A

公开(公告)日：1999-11-09

申请号：US924840

申请日：1997-09-05

Applicant: Michael T. Flavin ,  Ze-Qi Xu ,  Albert Khilevich ,  David Zembower ,  John D. Rizzo ,  Shuyuan Liao ,  Aye Mar ,  Lin Lin ,  Vilayphone Vilaychack ,  Darko Brankovic ,  Sergey Dzekhster ,  Jinjun Liu

Inventor： Michael T. Flavin ,  Ze-Qi Xu ,  Albert Khilevich ,  David Zembower ,  John D. Rizzo ,  Shuyuan Liao ,  Aye Mar ,  Lin Lin ,  Vilayphone Vilaychack ,  Darko Brankovic ,  Sergey Dzekhster ,  Jinjun Liu

IPC: A61K45/06 ,  C07D311/16 ,  C07D493/04 ,  C07D493/14 ,  C07D493/00

CPC classification number: C07D493/04 ,  A61K45/06 ,  C07D311/16 ,  C07D493/14

Abstract: A method of preparing (+)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. According to the disclosed method, chromene 4 intermediate was subjected to a chlorotitanium-mediated aldol reaction with acetaldehyde to selectively produce (.+-.)-8a. Separation and enzyme-mediated resolution of (.+-.)-8a produced (+)-8a. Cyclization of (+)-8a under neutral Mitsunobu conditions followed by Luche reduction of (+)-7 produced (+)-calanolide A in high yield and enantiomeric purity. The method of the invention has been extended to produce potent antiviral calanolide A analogues.

Abstract translation: 提供了从色烯4制备（+） - 丙内酰脲A，1，一种有效的HIV逆转录酶抑制剂的方法。 根据所公开的方法，将色烯4中间体与乙醛进行氯代钛介导的醛醇缩合反应以选择性地产生（+/-） - 8a。 （+） - 8a的（+/-） - 8a的分离和酶介导的分辨率。 （+） - 8a在中性Mitsunobu条件下循环，然后以高产率和对映异构体纯度，（+） - 7产生（+） - 卡立拉内酯A的Luche还原。 已经扩展了本发明的方法，以产生强效的抗病毒性甘露糖苷A类似物。

公开(公告)号：US07714017B2

公开(公告)日：2010-05-11

申请号：US11247431

申请日：2005-10-11

Applicant: Jasbir Singh ,  Mark Gurney ,  Georgeta Hategan ,  Peng Yu ,  David Zembower ,  Nian Zhou ,  Alexandre Mikhaylovich Polozov ,  Wayne Edward Zeller

Inventor： Jasbir Singh ,  Mark Gurney ,  Georgeta Hategan ,  Peng Yu ,  David Zembower ,  Nian Zhou ,  Alexandre Mikhaylovich Polozov ,  Wayne Edward Zeller

IPC: A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  C07D209/02 ,  C07D209/04 ,  A61K31/19 ,  A61K31/192 ,  C07C61/12

CPC classification number: C07D263/58 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D235/06 ,  C07D487/04 ,  C07D513/04

Abstract: Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:

Abstract translation: 公开了用于治疗或预防前列腺素介导的疾病或病症的环取代的稠合双环羧酸。 化合物具有通式A的代表性实例是：

公开(公告)号：US20090291948A1

公开(公告)日：2009-11-26

申请号：US12534390

申请日：2009-08-03

Applicant: Jasbir Singh ,  Mark E. Gurney ,  Georgeta Hategan ,  Peng Yu ,  David Zembower ,  Nian Zhou

Inventor： Jasbir Singh ,  Mark E. Gurney ,  Georgeta Hategan ,  Peng Yu ,  David Zembower ,  Nian Zhou

IPC: A61K31/538 ,  C07D403/02 ,  A61K31/4162 ,  G01N33/566 ,  C07D513/04 ,  C07D487/02 ,  A61K31/429 ,  A61K31/4188 ,  A61K31/47 ,  C07D215/02 ,  C07D215/227 ,  C07D265/36 ,  C07D209/04 ,  A61K31/405 ,  A61P29/00 ,  A61P9/10

CPC classification number: C07D263/58 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:

Abstract translation: 公开了用于治疗或预防前列腺素介导的疾病或病症的酰基磺酰胺，邻位取代的稠合双环化合物。 化合物具有通式A的代表性实例是：

公开(公告)号：US07598397B2

公开(公告)日：2009-10-06

申请号：US11169161

申请日：2005-06-27

Applicant: Jasbir Singh ,  Mark E. Gurney ,  Georgeta Hategan ,  Peng Yu ,  David Zembower ,  Nian Zhou

Inventor： Jasbir Singh ,  Mark E. Gurney ,  Georgeta Hategan ,  Peng Yu ,  David Zembower ,  Nian Zhou

IPC: C07D411/00

CPC classification number: C07D263/58 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:

Abstract translation: 公开了用于治疗或预防前列腺素介导的疾病或病症的酰基磺酰胺，邻位取代的稠合双环化合物。 化合物具有通式A的代表性实例是：

公开(公告)号：US20070213319A1

公开(公告)日：2007-09-13

申请号：US11651927

申请日：2007-01-10

Applicant: David Zembower ,  Jasbir Singh ,  Rama Mishra ,  Dawoon Jung ,  Xiaokang Zhu

Inventor： David Zembower ,  Jasbir Singh ,  Rama Mishra ,  Dawoon Jung ,  Xiaokang Zhu

IPC: A61K31/55 ,  A61K31/5377 ,  A61K31/517 ,  C07D413/02 ,  C07D405/02 ,  C07D403/02

CPC classification number: C07D239/95 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04

Abstract: This invention is directed to compounds and compositions that have biological properties useful for modulating HGF/SF activity. In certain embodiments, said compounds and compositions may be used in the treatment and prophylaxis of cancer or other dysproliferative diseases, as well as inflammatory diseases such as rheumatoid arthritis.

Abstract translation: 本发明涉及具有可用于调节HGF / SF活性的生物学特性的化合物和组合物。 在某些实施方案中，所述化合物和组合物可用于治疗和预防癌症或其它增生性疾病，以及炎性疾病如类风湿性关节炎。

公开(公告)号：US20060142355A1

公开(公告)日：2006-06-29

申请号：US11247431

申请日：2005-10-11

Applicant: Jasbir Singh ,  Mark Gurney ,  Georgeta Hategan ,  Peng Yu ,  David Zembower ,  Nian Zhou ,  Alexandre Polozov ,  Wayne Zeller

Inventor： Jasbir Singh ,  Mark Gurney ,  Georgeta Hategan ,  Peng Yu ,  David Zembower ,  Nian Zhou ,  Alexandre Polozov ,  Wayne Zeller

IPC: A61K31/43 ,  A61K31/4188 ,  A61K31/4162 ,  C07D498/02 ,  C07D487/02

CPC classification number: C07D263/58 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D235/06 ,  C07D487/04 ,  C07D513/04

Abstract: Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:

Abstract translation: 公开了用于治疗或预防前列腺素介导的疾病或病症的环取代的稠合双环羧酸。 化合物具有通式A的代表性实例是：

公开(公告)号：US5977385A

公开(公告)日：1999-11-02

申请号：US115984

申请日：1998-07-15

Applicant: Michael T. Flavin ,  Ze-Qi Xu ,  Albert Khilevich ,  David Zembower ,  John D. Rizzo ,  Shuyuan Liao ,  Aye Mar ,  Lin Lin ,  Vilayphone Vilaychack ,  Darko Brankovic ,  Sergey Dzekhster ,  Jinjun Liu

Inventor： Michael T. Flavin ,  Ze-Qi Xu ,  Albert Khilevich ,  David Zembower ,  John D. Rizzo ,  Shuyuan Liao ,  Aye Mar ,  Lin Lin ,  Vilayphone Vilaychack ,  Darko Brankovic ,  Sergey Dzekhster ,  Jinjun Liu

IPC: A61K45/06 ,  C07D311/16 ,  C07D493/04 ,  C07D493/14 ,  C07D493/00

CPC classification number: C07D493/04 ,  A61K45/06 ,  C07D311/16 ,  C07D493/14

Abstract: A method of preparing (+)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. According to the disclosed method, chromene 4 intermediate was subjected to a chlorotitanium-mediated aldol reaction with acetaldehyde to selectively produce (.+-.)-8a. Separation and enzyme-mediated resolution of (.+-.)-8a produced (+)-8a. Cyclization of (+)-8a under neutral Mitsunobu conditions followed by Luche reduction of (+)-7 produced (+)-calanolide A in high yield and enantiomeric purity. The method of the invention has been extended to produce potent antiviral calanolide A analogues.

公开(公告)号：US5859050A

公开(公告)日：1999-01-12

申请号：US926307

申请日：1997-09-05

Applicant: Michael T. Flavin ,  Ze-Qi Xu ,  Albert Khilevich ,  David Zembower ,  John D. Rizzo ,  Lin Lin

Inventor： Michael T. Flavin ,  Ze-Qi Xu ,  Albert Khilevich ,  David Zembower ,  John D. Rizzo ,  Lin Lin

IPC: A61K45/06 ,  C07D311/16 ,  C07D493/04 ,  C07D493/14 ,  A61K31/35

CPC classification number: C07D493/04 ,  A61K45/06 ,  C07D311/16 ,  C07D493/14

Abstract: A method of preparing (+)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. According to the disclosed method, chromene 4 intermediate was subjected to a chlorotitanium-mediated aldol reaction with acetaldehyde to selectively produce (.+-.)-8a. Separation and enzyme-mediated resolution of (.+-.)-8a produced (+)-8a. Cyclization of (+)-8a under neutral Mitsunobu conditions followed by Luche reduction of (+)-7 produced (+)-calanolide A in high yield and enantiomeric purity. The method of the invention has been extended to produce potent antiviral calanolide A analogues.