公开(公告)号：JP2010270135A

公开(公告)日：2010-12-02

申请号：JP2010164769

申请日：2010-07-22

Applicant: Abbott Lab ,  アボット・ラボラトリーズAbbott Laboratories

Inventor： BAUER JOHN F ,  SALEKI-GERHARDT AZITA ,  NARAYANAN BIKSHANDARKOIL A ,  CHEMBURKAR SANJAY R ,  PATEL KETAN ,  SPIWEK HARRY O ,  BAUER PHILIP E ,  ALLEN KIMBERLY A

IPC: C07D277/28 ,  A61K31/426 ,  A61K31/427 ,  A61P31/18 ,  A61P37/04 ,  C07D277/24 ,  C07D277/30 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D417/12

CPC classification number: C07D277/28

Abstract: PROBLEM TO BE SOLVED: To provide a novel crystalline polymorphous form of ritonavir and a process for producing the same.
SOLUTION: There is provided a substantially pure crystalline polymorphous form of (2S, 3S, 5S)-5-(N-(N-((N-methyl-N-((2-isopropyl-4-thiazoyl)methyl)amino)carbonyl)-L-valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl-3-hydroxyhexane which gives peaks of 2θ angle at 8.67°±0.1°, 9.88°±0.1°, 16.11°±0.1°, 16.70°±0.1°, 17.36°±0.1°, 17.78°±0.1°, 18.40°±0.1°, 18.93°±0.1°, 20.07°±0.1°, 20.65°±0.1°, 21.71°±0.1° and 25.38°±0.1° in a powder X-ray diffraction pattern. There is also provided a process for producing the crystalline polymorph form, which includes inoculating seed crystals in a solution of ritonavir, and then adding an anti-solvent.
COPYRIGHT: (C)2011,JPO&INPIT

Abstract translation: 待解决的问题：提供新型的晶体多晶形式的利托那韦及其制备方法。 提供了（2S，3S，5S）-5-（N-（N - （（N-甲基-N - （（2-异丙基-4-噻唑基）甲基） ）氨基）羰基）-L-缬氨酰基）氨基）-2-（N - （（5-噻唑基）甲氧基羰基）氨基）-1,6-二苯基-3-羟基己烷，其在8.67°±0.1°处产生2θ角的峰 ，9.88°±0.1°，16.11°±0.1°，16.70°±0.1°，17.36°±0.1°，17.78°±0.1°，18.40°±0.1°，18.93°±0.1°，20.07°±0.1°，20.65° 在粉末X射线衍射图中为±0.1°，21.71°±0.1°和25.38°±0.1°。 还提供了一种制备结晶多晶型形式的方法，其包括将晶种接种在利托那韦的溶液中，然后加入抗溶剂。 版权所有（C）2011，JPO＆INPIT

公开(公告)号：WO0004016A3

公开(公告)日：2000-03-30

申请号：PCT/US9916334

申请日：1999-07-19

Applicant: ABBOTT LAB

Inventor： BAUER JOHN F ,  SALEKI-GERHARDT AZITA ,  NARAYANAN BIKSHANDARKOIL A ,  CHEMBURKAR SANJAY R ,  PATEL KETAN ,  SPIWEK HARRY O ,  BAUER PHILIP E ,  ALLEN KIMBERLY A

IPC: A61K31/426 ,  A61K31/427 ,  A61P31/18 ,  A61P37/04 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D417/12 ,  A61K31/425

CPC classification number: C07D277/28

Abstract: A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.

Abstract translation: 公开了利托那韦的新结晶多晶型物及其使用和制备方法。

公开(公告)号：SK287381B6

公开(公告)日：2010-08-09

申请号：SK50292008

申请日：1999-07-19

Applicant: ABBOTT LAB

Inventor： BAUER JOHN F ,  SALEKI-GERHARDT AZITA ,  NARAYANAN BIKSHANDARKOIL A ,  CHEMBURKAR SANJAY R ,  PATEL KETAN ,  SPIWEK HARRY O ,  BAUER PHILIP E ,  ALLEN KIMBERLY A

IPC: A61K31/00 ,  A61K31/426 ,  A61K31/427 ,  A61P31/18 ,  A61P37/04 ,  C07D277/00 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D417/12

Abstract: Amorphous ritonavir containing no more than 10 % of any other form of ritonavir characterised by the DSC thermogram recorded at a heating rate of 5 °C/min. and a glass transition temperature from about 45 °C to about 49 °C. Described is also a method for the preparation of amorphous ritonavir and its use.

公开(公告)号：AU2007202943A1

公开(公告)日：2007-07-19

申请号：AU2007202943

申请日：2007-06-26

Applicant: ABBOTT LAB

Inventor： BAUER PHILIP E ,  ALLEN KIMBERLY A ,  NARAYANAN BIKSHANDARKOIL A ,  CHEMBURKAR SANJAY R ,  SALEKI-GERHARDT AZITA ,  SPIWEK HARRY O ,  BAUER JOHN F ,  PATEL KETAN

IPC: C07D417/00

公开(公告)号：PT946537E

公开(公告)日：2005-08-31

申请号：PT97951641

申请日：1997-12-12

Applicant: ABBOTT LAB

Inventor： NARAYANAN BIKSHANDARKOIL A ,  OLIVER-SHAFFER PATRICIA A ,  RESEK JAMES E ,  SINGAM PULLA R

IPC: C07D317/60 ,  C07D405/04

公开(公告)号：DK0946537T3

公开(公告)日：2005-08-15

申请号：DK97951641

申请日：1997-12-12

Applicant: ABBOTT LAB

Inventor： NARAYANAN BIKSHANDARKOIL A ,  SINGAM PULLA R ,  RESEK JAMES E ,  OLIVER-SHAFFER PATRICIA A

IPC: C07D317/60 ,  C07D405/04

Abstract: The present invention relates to an asymmetric Michael Addition reaction to produce nitro ketone diasteroisomers with enhanced stereoselectivity.

公开(公告)号：PT1097148E

公开(公告)日：2004-05-31

申请号：PT99934143

申请日：1999-07-19

Applicant: ABBOTT LAB

Inventor： BAUER JOHN F ,  CHEMBURKAR SANJAY R ,  SALEKI-GERHARD AZITA ,  NARAYANAN BIKSHANDARKOIL A ,  PATEL KETAN ,  SPIWEK HARRY O ,  BAUER PHILIP E ,  ALLEN KIMBERLY A

IPC: A61K31/426 ,  A61K31/427 ,  A61P31/18 ,  A61P37/04 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D417/12 ,  A61K31/425

Abstract: This Application concerns the use of Form II crystalline ritonavir as a pharmaceutical agent, as well as methods of preparing pharmaceutical compositions, which methods employ Form II crystalline ritonavir. The Application further concerns methods for obtaining Form I crystalline ritonavir, which methods employ Form II crystalline ritonavir.

公开(公告)号：TR200100171T2

公开(公告)日：2001-05-21

申请号：TR200100171

申请日：1999-07-19

Applicant: ABBOTT LAB

Inventor： BAUER JOHN F ,  SALEKI-GERHARDT AZITA ,  NARAYANAN BIKSHANDARKOIL A ,  CHEMBURKAR SANJAY R ,  PATEL KETAN ,  SPIWEK HARRY O ,  BAUER PHILIP E ,  ALLEN KIMBERLY A

IPC: A61K31/426 ,  A61K31/427 ,  A61P31/18 ,  A61P37/04 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D417/12 ,  A61K31/425

Abstract: This Application concerns the use of Form II crystalline ritonavir as a pharmaceutical agent, as well as methods of preparing pharmaceutical compositions, which methods employ Form II crystalline ritonavir. The Application further concerns methods for obtaining Form I crystalline ritonavir, which methods employ Form II crystalline ritonavir.

公开(公告)号：SK287586B6

公开(公告)日：2011-03-04

申请号：SK50282008

申请日：1999-07-19

Applicant: ABBOTT LAB

Inventor： BAUER JOHN F ,  SALEKI-GERHARDT AZITA ,  NARAYANAN BIKSHANDARKOIL A ,  CHEMBURKAR SANJAY R ,  PATEL KETAN ,  SPIWEK HARRY O ,  BAUER PHILIP E ,  ALLEN KIMBERLY A

IPC: A61K31/00 ,  A61K31/426 ,  A61K31/427 ,  A61P31/18 ,  A61P37/04 ,  C07D277/00 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D417/00 ,  C07D417/12

Abstract: Described is a method for the preparation of pharmaceutical composition containing ritonavir, in which form II crystalline ritonavir is dissolved in a receptacle, which is a mixing tank.

公开(公告)号：CZ298188B6

公开(公告)日：2007-07-18

申请号：CZ2001203

申请日：1999-07-19

Applicant: ABBOTT LAB

Inventor： BAUER JOHN F ,  SALEKI-GERHARDT AZITA ,  NARAYANAN BIKSHANDARKOIL A ,  CHEMBURKAR SANJAY R ,  PATEL KETAN ,  SPIWEK HARRY O ,  BAUER PHILIP E ,  ALLEN KIMBERLEY A

IPC: C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  A61P31/18 ,  A61P37/04 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42

Abstract: Popisuje se krystalický polymorf ritonaviru, neboli (2S, 3S, 5S)-5-(N-(N-((N-methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)karbonyl)-L-valinyl)amino)-2-(N-((5-thiazolyl)methoxykarbonyl)amino)-1,6-difenyl-3-hydroxyhexanu, a zpusoby jeho prípravy.