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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&INPITAbstract 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
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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。
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公开(公告)号：WO9943299A2
公开(公告)日：1999-09-02
申请号：PCT/US9903675
申请日：1999-02-19
Applicant: ABBOTT LAB
Inventor： FU LU MOU YING , BAUER JOHN F , DZIKI WALTER , TAYLOR VICTOR E , WANG ZHENG
CPC classification number: A61K9/0095
Abstract: The present invention relates to a pharmaceutical composition and concentrate suitable for oral administration comprising a hydrophilic drug solubilized in a lipophilic phase comprising a fatty acid, and water; an oral formulation comprising uniform dispersion of the pharmaceutical concentrate in an aqueous phase optionally comprising a self-emulsifying material; and to a process of making the same.
Abstract translation: 本发明涉及适于口服给药的药物组合物和浓缩物，其包含溶解在包含脂肪酸的亲脂相中的亲水性药物和水; 包含药物浓缩物均匀分散在任选包含自乳化材料的水相中的口服制剂; 并涉及制造它的过程。
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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.
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公开(公告)号：DK1418174T3
公开(公告)日：2009-05-18
申请号：DK03029709
申请日：1999-07-19
Applicant: ABBOTT LAB
Inventor： BAUER JOHN F , SALEKI-GERHARDT AZITA , PATEL KETAN , CHEMBURKAR SANJAY R , SPIWEK HARRY O
IPC: C07D277/24 , A61K31/425 , A61K31/426 , A61K31/427 , A61P31/18 , A61P37/04 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/40 , C07D277/42 , C07D417/12
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.
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Patent Agency Ranking
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
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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.
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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.
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公开(公告)号：CO4970788A1
公开(公告)日：2000-11-07
申请号：CO99011498
申请日：1999-02-24
Applicant: ABBOTT LAB
Inventor： MOU YING FU LU , BAUER JOHN F , DZIKI WALTEER , TAYLOR VICTOR E , ZHENG WANG
Abstract: Un concentrado farmacéutico para administración oral quecontiene una droga hidrofílica solubilizada en una fase lipofílica que consiste de un ácido graso y agua. 2El proceso de la Reivindicación 21, en donde el concentrado contiene además un alcohol C1 -C5 que varía entre 0% y 60% en volumen del concentrado.
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公开(公告)号：DE69510999D1
公开(公告)日：1999-09-02
申请号：DE69510999
申请日：1995-03-06
Applicant: ABBOTT LAB
Inventor： MORLEY JAMES A , BAUER JOHN F , PATEL RAMESH R , SPANTON STEPHEN G , HENRY RODGER F
IPC: A61K31/505 , A61P9/12 , C07B63/00 , C07D405/12
Abstract: The present invention provides a non-solvated crystalline polymorph of terazosin monohydrochloride designated Form III and methods for its preparation. Also disclosed is terazosin monohydrochloride methanolate and processes for its production as well as processes for its conversion to other crystalline forms of terazosin monohydrochloride.
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