JP2010520198A5 - - Google Patents
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- Publication number
- JP2010520198A5 JP2010520198A5 JP2009551709A JP2009551709A JP2010520198A5 JP 2010520198 A5 JP2010520198 A5 JP 2010520198A5 JP 2009551709 A JP2009551709 A JP 2009551709A JP 2009551709 A JP2009551709 A JP 2009551709A JP 2010520198 A5 JP2010520198 A5 JP 2010520198A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline
- salt form
- sulfate
- crystalline salt
- cyclohexylmethyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 239000000203 mixture Substances 0.000 claims description 89
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- 239000011541 reaction mixture Substances 0.000 claims description 78
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 67
- -1 8- {2- [cyclohexylmethyl-((S) -2,3-dihydroxy-propionyl) amino] ethyl} -8-aza-bicyclo [3.2.1] oct-3-yl Chemical group 0.000 claims description 66
- 238000000034 method Methods 0.000 claims description 66
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 38
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 33
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| TWI415850B (zh) * | 2007-07-20 | 2013-11-21 | Theravance Inc | 製備ｍｕ類鴉片受體拮抗劑之中間物的方法 |
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| TWI423801B (zh) | 2007-08-27 | 2014-01-21 | Theravance Inc | 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物 |
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| PT3277278T (pt) * | 2015-04-02 | 2020-04-16 | Theravance Biopharma R&D Ip Llc | Forma farmacêutica de combinação de um antagonista do recetor opioide mu e um agente opioide |
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| US6900228B1 (en) * | 1998-03-10 | 2005-05-31 | Research Triangle Institute | Opiate compounds, methods of making and methods of use |
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| US20020025948A1 (en) * | 2000-06-23 | 2002-02-28 | Banks Bernard Joseph | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| GEP20084300B (en) * | 2001-10-22 | 2008-02-11 | Pfizer Prod Inc | 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists |
| US7381721B2 (en) * | 2003-03-17 | 2008-06-03 | Adolor Corporation | Substituted piperidine compounds |
| US20040204453A1 (en) * | 2003-04-14 | 2004-10-14 | Pfizer Inc | 4-Phenyl-piperidine compounds and their use as modulators of opioid receptors |
| US7056930B2 (en) | 2003-04-14 | 2006-06-06 | Pfizer Inc. | 2-Azabicyclo[3.3.1]nonane derivatives |
| JP3984281B2 (ja) * | 2003-04-14 | 2007-10-03 | ファイザー・プロダクツ・インク | ３−アザビシクロ〔３，２，１〕オクタン誘導体 |
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| US6992090B2 (en) * | 2003-06-16 | 2006-01-31 | Adolor Corporation | Substituted piperidine compounds and methods of their use |
| EP1737853A1 (en) | 2004-02-03 | 2007-01-03 | Janssen Pharmaceutica N.V. | 3-(diheteroarylmethylene)-8-azabicyclo¬3.2.1|octane and 3-((aryl)(heteroaryl)methylene)-8-azabicyclo¬3.2.1|octane derivatives |
| US7087749B2 (en) * | 2004-03-11 | 2006-08-08 | Adolor Corporation | Substituted piperidine compounds and methods of their use |
| MY145633A (en) | 2006-03-01 | 2012-03-15 | Theravance Inc | 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| MX2009004965A (es) | 2006-11-07 | 2009-06-05 | Nektar Therapeutics Al Corp | Formas de dosificacion y co-administracion de un agonista de opioides y un antagonista de opioides. |
| TWI409067B (zh) * | 2007-02-28 | 2013-09-21 | Theravance Inc | ８-氮雜雙環〔３．２．１〕辛烷化合物之結晶型 |
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