- Iridium-catalyzed enantioselective hydrogenation of unsaturated heterocyclic acids
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Spiral binding: A highly enantioselective hydrogenation of unsaturated heterocyclic acids has been developed by using chiral iridium/spirophosphino oxazoline catalysts (see scheme; BArF-=tetrakis[3,5- bis(trifluoromethyl)phenyl]borate, Boc=tert-butoxycarbonyl). This reaction provided an efficient method for the preparation of optically active heterocyclic acids with excellent enantioselectivities. Copyright
- Song, Song,Zhu, Shou-Fei,Pu, Liu-Yang,Zhou, Qi-Lin
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p. 6072 - 6075
(2013/07/05)
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- Crystalline and amorphous forms of tiagabine
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The present invention provides 24 new forms of tiagabine, including 22 new crystalline forms of tiagabine and its salts, an amorphous form of tiagabine free base, and a cocrystal form of tiagabine hydrochloride with 2-furancarboxylic acid. The present invention further provides a process for preparing each of the new tiagabine forms. The present invention further provides a pharmaceutical composition containing at least one of the new tiagabine forms, and a process for the preparation thereof. The present invention further provides a method of treating a disease related to GABA uptake in a mammal, comprising the step of administering to the mammal a therapeutically effective amount of at least one of the new tiagabine forms.
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Page/Page column 13
(2008/06/13)
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- Modified form of the R(-)-N-(4,4-di(3-methylthien-2-yl)but-3-enyl)-nipecotic acid hydrochloride
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The present invention provides R(-)-N-(4,4-di(3-methylthien-2-yl)but-3-enyl)-nipecotic acid hydrochloride in its pure and stable anhydrous form.
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- The Synthesis of Novel GABA Uptake Inhibitors. 1. Elucidation of the Structure-Activity Studies Leading to the Choice of (R)-1--3-piperidinecarboxylic Acid (Tiagabine) as an Anticonvulsant Drug Candidate
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A series of different synthetic approaches to novel GABA uptake inhibitors are described, leading to examples which are derivatives of nipecotic acid and guvacine, substituted at nitrogen by 4,4-diaryl-3-butenyl or 2-(diphenylmethoxy)ethyl moieties.The in vitro value for inhibition of 3H>-GABA uptake in rat synaptosomes was determined for each compound.It was found that the most potent examples are those having a substituent in an "ortho" position in one or both aromatic/heteroatomic groups.The majority of the compounds described are structurally related to tiagabine, (R)-1--3-piperidinecarboxylic acid hydrochloride (NNC 05-0328) and some of the reasoning behind the selection of this compound as a drug candidate is summarized.
- Andersen, Knud Erik,Braestrup, Claus,Groenwald, Frederik C.,Joergensen, Anker S.,Nielsen, Erik B.,et al.
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p. 1716 - 1725
(2007/10/02)
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