459836-89-6Relevant academic research and scientific papers
1,3,4-OXADIAZOLE HOMOPHTHALIMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 231, (2020/12/11)
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.
1,3,4-OXADIAZOLE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 211-212, (2020/12/11)
The present invention relates to 1,3,4-oxadiazole derivative compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, a use thereof in preparation of a medicament, a pharmaceutical composition comprising the same, a therapeutic method using the composition, and a method for preparing the same, and the 1,3,4-oxadiazole derivative compounds are represented by a following chemical formula (I).
PIPERAZINYL AND PIPERIDINYL QUINAZOLIN-4(3H)-ONE DERIVATIVES HAVING ACTIVITY AGAINST PAIN
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Page/Page column 206, (2020/05/28)
The present invention relates to piperazinyl and piperidinyl quinazolin-4(3H)-one derivatives having pharmacological activity towards the (formula (I)) subunit, in particular the (formula (2)) subunit, of the voltage-gated calcium channel, in particular having dual pharmacological activity towards both the (formula (I)) subunit, in particular the (formula (2)) subunit, of the voltage-gated calcium channel and the μ-opioid receptor. The present invention also relates to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
Synthesis, Evaluation and Proposed Binding Pose of Substituted Spiro-Oxindole Dihydroquinazolinones as IRAP Inhibitors
?qvist, Johan,Agalo, Faith,Engen, Karin,Gutiérrez-de-Terán, Hugo,Hallberg, Mathias,Jensen, Annika Jenmalm,Konda, Vivek,Larhed, Mats,Lundb?ck, Thomas,Rosenstr?m, Ulrika,Vanga, Sudarsana Reddy
, p. 325 - 337 (2020/04/07)
Insulin-regulated aminopeptidase (IRAP) is a new potential macromolecular target for drugs aimed for treatment of cognitive disorders. Inhibition of IRAP by angiotensin IV (Ang IV) improves the memory and learning in rats. The majority of the known IRAP inhibitors are peptidic in character and suffer from poor pharmacokinetic properties. Herein, we present a series of small non-peptide IRAP inhibitors derived from a spiro-oxindole dihydroquinazolinone screening hit (pIC50 5.8). The compounds were synthesized either by a simple microwave (MW)-promoted three-component reaction, or by a two-step one-pot procedure. For decoration of the oxindole ring system, rapid MW-assisted Suzuki-Miyaura cross-couplings (1 min) were performed. A small improvement of potency (pIC50 6.6 for the most potent compound) and an increased solubility could be achieved. As deduced from computational modelling and MD simulations it is proposed that the S-configuration of the spiro-oxindole dihydroquinazolinones accounts for the inhibition of IRAP.
OXAZINE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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Paragraph 0094; 0095; 0097, (2016/10/07)
PROBLEM TO BE SOLVED: To provide a compound that specifically inhibits the signal transmission of an IL-23 receptor uncompetitively with IL-23 without inhibiting phosphoenzyme activity of janus kinases. SOLUTION: The present invention provides an oxazine derivative represented by the following formula or a pharmacologically acceptable salt thereof. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
INVERSE AGONISTS AND NEUTRAL ANTAGONISTS FOR THE TSH RECEPTOR
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Page/Page column 51, (2011/10/31)
TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.
BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ANTIVARAL AGENTS
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Page/Page column 83, (2010/10/03)
The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together
