- Bisheterocycle substituted oxa-spiro derivative, and preparation method and medical application thereof
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The invention relates to a bisheterocyclic substituted oxa-spiro derivative, and a preparation method and medical application thereof. Specifically, the invention discloses compounds of formula (I) and formula (II) or pharmaceutically acceptable salts, stereoisomers or solvates thereof, and a preparation method and application thereof. Each group in the formulas is as defined in the specificationand claims in detail.
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Paragraph 0276-0277; 0279
(2020/09/23)
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- Synthesis and characterization of potential impurities of Vigabatrin-An anti epileptic drug
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The present work describes the synthesis and characterization of four potential impurities of Vigabatrin (1) namely 2-(2-aminobut-3-enyl)malonic acid (2) (Vigabatrin USP impurity-E), 2-(2-oxo-5-vinylpyrrolidin-1-yl)acetic acid (3) (USP Tablets impurity), 4-aminohexanoic acid (4) and 2,2′-oxo-5,5′-bispyrrolidinyl ether (5). Compound 4 is a possible process related impurity of 1 where as compound 5 is a process related impurity of 5-ethoxy-2-pyrrolinone (16). All these impurities have a significant impact on the quality of the drug product. This work is extremely useful for generic pharmaceutical industry.
- Karumanchi, Kishore,Natarajan, Senthil Kumar,Gadde, Sunil,Chavakula, Ramadas,Korupolu, Raghu Babu,Bonige, Kishore Babu
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p. 359 - 366
(2019/01/30)
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- Thiazoline derivatives
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Object: To provide compounds useful as inhibitors of blood platelet aggregation for intravenous administration. Constitution: A thiazoline derivative represented by the formula: STR1 ?wherein R1 is a hydroxyl group, an alkoxy group, a cycloalkoxy group or a group represented by the formula: R4 NH-- (wherein R4 is a cycloalkyl group), R2 is an alkyl group, a cycloalkyl group or a phenylalkyl group, R3 is a hydrogen atom or an alkyl group, and n is an integer of 2 to 9! or a salt thereof.
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