- NOVEL PROCESS FOR MAKING (2R)-(3-AMINO-2-FLUOROPROPYL)PHOSPHINIC ACID FORM A
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The present invention is directed to a novel process for the preparation of the crystalline form A of (2R)-(3-amino-2-fluoropropyl)phosphinic acid.
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Page/Page column 8-9
(2009/07/25)
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- NOVEL CRYSTALLINE FORM B OF (2R)-(3-AMINO-2-FLUOROPROPYL)PHOSPHINIC ACID
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The present invention relates to a novel crystalline form of (2R)-(3-amino-2- fluoropropyl)phosphinic acid, the present invention is also directed to the use of the crystalline form for the treatment of gastrointestinal disorders as well as to a pharmaceutical compositions comprising the same and a process for the preparation of the crystalline form.
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Page/Page column 14
(2009/07/25)
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- NOVEL CRYSTALLINE FORM C OF (2R)-(3-AMINO-2-FLUOROPROPYL)PHOSPHINIC ACID
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The present invention relates to a novel crystalline form of (2R)-(3-amino-2- fluoropropyl)phosphinic acid, the present invention is also directed to the use of the crystalline form for the treatment of gast rointestinal disorders as well as to a pharmaceutical composition comprising the same and a process for the preparation of the crystalline form.
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Page/Page column 13
(2009/07/25)
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- Synthesis and pharmacological evaluation of novel γ-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors
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We have previously demonstrated that the prototypical GABAB receptor agonist baclofen inhibits transient lower esophageal sphincter relaxations (TLESRs), the most important mechanism for gastroesophageal reflux. Thus, GABAB agonists could be exploited for the treatment of gastroesophageal reflux disease. However, baclofen, which is used as an antispastic agent, and other previously known GABAB agonists can produce CNS side effects such as sedation, dizziness, nausea, and vomiting at higher doses. We now report the discovery of atypical GABAB agonists devoid of classical GABAB agonist related CNS side effects at therapeutic doses and the optimization of this type of compound for inhibition of TLESRs, which has resulted in a candidate drug (R)-7 (AZD3355) that is presently being evaluated in man.
- Alstermark, Christer,Amin, Kosrat,Dinn, Sean R.,Elebring, Thomas,Fjellstr?m, Ola,Fitzpatrick, Kevin,Geiss, William B.,Gottfries, Johan,Guzzo, Peter R.,Harding, James P.,Holmén, Anders,Kothare, Mohit,Lehmann, Anders,Mattsson, Jan P.,Nilsson, Karolina,Sundén, Gunnel,Swanson, Marianne,Von Unge, Sverker,Woo, Alex M.,Wyle, Michael J.,Zheng, Xiaozhang
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experimental part
p. 4315 - 4320
(2009/05/30)
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