299954-60-2Relevant academic research and scientific papers
Amide compound and derivative thereof, preparation method, pharmaceutical composition and application thereof
-
Paragraph 0096-0099, (2021/07/09)
The invention discloses an amide compound and derivative thereof, a preparation method, a pharmaceutical composition and application thereof. The structure of the amide compound is shown as a formula (I). The derivatives of theamide compound relate to a stereoisomer, a tautomer, a metabolite, a metabolic precursor, a prodrug, a solvate, a salt of the solvate, a crystal, a pharmaceutically acceptable salt or a mixture of the above of theamide compound. The amide compound and the derivative thereof have an efficient inhibition effect on indoleamine 2, 3-dioxygenase 1, and can be used for preparing medicines for treating indoleamine 2, 3-dioxygenase 1 mediated immunosuppression related diseases, the prepared medicine can exert the medicine effect at the molecular level and is wide in application, and the synthesis method of the compound is simple, convenient and easy to operate.
Glutamate receptor photomodulators
-
Paragraph 0103-0106; 0109-0110, (2015/04/15)
The present invention relates to the discovery of particular aromatic compounds of formula (1), possessing activity as modulators of metabotropic glutamate receptors (mGIuR) whose modulatory activity on the receptor may be controlled by irradiation with suitable light resulting in the optical control of receptor biological function, to the use of said compounds as a medicament, and to pharmaceutical compositions comprising said compounds of formula (1).
SAR analysis of a series of acylthiourea derivatives possessing broad-spectrum antiviral activity
Burgeson, James R.,Moore, Amy L.,Boutilier, Jordan K.,Cerruti, Natasha R.,Gharaibeh, Dima N.,Lovejoy, Candace E.,Amberg, Sean M.,Hruby, Dennis E.,Tyavanagimatt, Shanthakumar R.,Allen III, Robert D.,Dai, Dongcheng
scheme or table, p. 4263 - 4272 (2012/07/17)
A series of acylthiourea derivatives were designed, synthesized, and evaluated for broad-spectrum antiviral activity with selected viruses from Poxviridae (vaccinia virus) and two different genera of the family Bunyaviridae (Rift Valley fever and La Cross
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu4) with CNS exposure in rats
Engers, Darren W.,Field, Julie R.,Le, Uyen,Zhou, Ya,Bolinger, Julie D.,Zamorano, Rocio,Blobaum, Anna L.,Jones, Carrie K.,Jadhav, Satyawan,Weaver, C. David,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
supporting information; experimental part, p. 1106 - 1110 (2011/04/26)
Herein we report the discovery, synthesis, and evaluation of a series of N-(4-acetamido)-phenylpicolinamides as positive allosteric modulators of mGlu4. Compounds from the series show submicromolar potency at both human and rat mGlu4. In addition, pharmacokinetic studies utilizing subcutaneous dosing demonstrated good brain exposure in rats.
