- Structure-based drug design of tricyclic 8H-indeno[1,2-d][1,3]thiazoles as potent FBPase inhibitors
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With the goal of improving metabolic stability and further enhancing FBPase inhibitory activity, a series of tricyclic 8H-indeno[1,2-d][1,3]thiazoles was designed and synthesized with the aid of structure-based drug design. Extensive SAR studies led to th
- Tsukada, Tomoharu,Takahashi, Mizuki,Takemoto, Toshiyasu,Kanno, Osamu,Yamane, Takahiro,Kawamura, Sayako,Nishi, Takahide
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- 6-OXO-1,6-DIHYDROPYRIDAZINE DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
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A 6-oxo-1,6-dihydropyridazine derivative, a preparation method therefor and medical use thereof, in particular, a 6-oxo-1,6-dihydropyridazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutical composition containing the derivative, and use thereof as a NaV inhibitor and use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases. Each substituent in general formula (I) is the same as defined in the description.
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Paragraph 0145-0146; 0152; 0289-0290
(2021/11/14)
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- Compound and application of compound in preparation of medicines
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The invention discloses a compound and its application in a medicine. the invention specifically provides a compound as shown in the formula (I) or a stereisomer, a geometrical isomer, a tautomer, a racemate, nitric oxide, hydrate, a solvate, a metabolite, pharmaceutically acceptable salts or a prodrug of the compound as shown in the formula (I). The invention also discloses an application of the compound in preparation of a medicine. The medicine is used in treating cancers.
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Paragraph 0158; 0159
(2016/10/08)
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- Bicyclic amino-substituted compounds
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A compound of formula (I), wherein X is O, CH 2, S, SO or SO 2 ; R is F or Cl; R 1 is H, C 1 -C 6 alkyl or C 2 -C 6 alkenyl; R 2 is H, C 1 -C 6 alkyl or C 2 -C 6 alkenyl; R 3 is H, C 1 -C 6, alkyl, a pharmaceutically acceptable salt thereof, an enantiomer thereof, and a pharmaceutically acceptable salt of said enantiomer for use in therapy. A pharmaceutical preparation containing as active ingredient any one of said compounds. A process for the preparation of a compound of formula (I).
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