- 1,3,4-OXADIAZOLE HOMOPHTHALIMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention relates to novel compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, a medicinal use thereof, and a method for preparing the same. The novel compounds according to the present invention, stereoisomers thereof or pharmaceutically acceptable salts thereof have the histone deacetylase 6 (HDAC6) inhibitory activity, and are effective in preventing or treating HDAC6-related diseases, comprising infectious diseases; neoplasm; endocrinopathy; nutritional and metabolic diseases; mental and behavioral disorders; neurological diseases; eye and ocular adnexal diseases; circulatory diseases; respiratory diseases; digestive diseases; skin and subcutaneous tissue diseases; musculoskeletal system and connective tissue diseases; and teratosis or deformities, or chromosomal aberration.
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- Pyrazolopyrimidine compounds and preparation method thereof, and applications in preparation of anti-cancer drugs
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The invention provides a class of pyrazolopyrimidine compounds represented by a formula (I) or pharmaceutically acceptable salts thereof, and a preparation method thereof, and applications of the pyrazolopyrimidine compounds or the pharmaceutically accept
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Paragraph 0140-0142; 0148-0152
(2020/04/17)
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- Intramolecular photoreactions of thiohomophthalimides with an alkenyl group in their N-side chain. Regioselective synthesis of heterocycle-fused isoquinoline derivatives through [2+2] photocycloaddition
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Upon irradiation, thiohomophthalimides with an alkenyl group in their N-side chain or at the benzylic position give tricyclic isoquinoline derivatives through regioselective intramolecular [2+2] cycloaddition or Norrish type II reaction, respectively, in
- Takechi, Haruko,Takahashi, Hajime,Machida, Minoru
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p. 201 - 207
(2007/10/03)
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- Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: A new class of inhibitors of lck kinase
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An imidazo[4,5-h]isoquinolin-7,9-dione (1) was identified as an adenosine 5′-triphosphate competitive inhibitor of lck by high throughput screening. Initial structure-activity relationship studies identified the dichlorophenyl ring and the imide NH as important pharmacophores. A binding model was constructed to understand how 1 binds to a related kinase, hck. These results suggested that removing the gem-dimethyl group and flattening the ring would enhance activity. This was realized by converting 1 to the imidazo[4,5-h]isoquinolin-9-one (20), resulting in an 18-fold improvement in potency against lck and a 50-fold increase in potency in a cellular assay.
- Snow, Roger J.,Cardozo, Mario G.,Morwick, Tina M.,Busacca, Carl A.,Dong, Yong,Eckner, Robert J.,Jacober, Stephen,Jakes, Scott,Kapadia, Suresh,Lukas, Susan,Panzenbeck, Maret,Peet, Gregory W.,Peterson, Jeffrey D.,Prokopowicz III, Anthony S.,Sellati, Rosemarie,Tolbert, Robert M.,Tschantz, Matt A.,Moss, Neil
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p. 3394 - 3405
(2007/10/03)
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- Nitrogenous heterocyclic compounds and hyperlipemia remedy containing the same
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Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia. wherein A represents group —CR1R2—(CH2)i— where R1and R2each represent a hydrogen atom or alkyl, —CH═CH—, —O—CH2—, or —S(O)j—CH2—; B represents a hydrogen or halogen atom; X represents —CR3R4R5, —NR6R7, —(CH2—CH═C(CH3)—CH2)p—CH2CH═C(CH3)2, alkyl, cycloalkyl, phenyl, cinnamyl, or heteroaromatic ring; Y represents —(CH2)q—, —CH═CH—, —NR8—, an oxygen atom, or a bond; Z represents carbonyl or a bond; K represents alkylene or a bond; L represents —CH═CH— or a bond; and M represents a hydrogen atom, alkyl, cycloalkyl, phenyl, heterocyclic ring, biphenyl, or diphenylmethyl.
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- Pyrrolobenzimidazoles for treating heart or circulatory diseases
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Pyrrolobenzimidazoles, processes for the preparation thereof and pharmaceutical compositions thereof for the treatment of coronary insufficiencies, cardiac failure, blood circulatory disturbances and occlusive diseases. The new pyrrolobenzimidazoles are of the formula STR1 wherein R1 is hydrogen, alkyl, alkenyl or cycloalkyl, R2 is hydrogen, alkyl, alkenyl, cyano or a substituted carbonyl or R1 and R2 together represent cycloalkylene or form alkylidene or cycloalkylidene, X is a valency bond, C1 -C4 alkylene or vinylene, T is oxygen or sulphur and Py is pyridyl or substituted pyridyl and including the tautomers thereof and the physiologically acceptable salts thereof.
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