18354-73-9Relevant articles and documents
IDO/TDO Inhibitor
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Paragraph 0334-0336; 0415; 0416, (2020/08/19)
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R1 and R2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R1 and R2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R4 represents, for example, —C(═NH)—HN2, and R6 represents, for example, a substituted or unsubstituted aryl group].
Synthesis and evaluation of 2,5-furan, 2,5-thiophene and 3,4-thiophene-based derivatives as CXCR4 inhibitors
Gaines, Theresa,Garcia, Francisco,Virani, Saniya,Liang, Zhongxing,Yoon, Younghyoun,Oum, Yoon Hyeun,Shim, Hyunsuk,Mooring, Suazette Reid
, (2019/08/06)
The interaction between G-Protein coupled receptor CXCR4 and its natural ligand CXCL12 has been linked to inflammation experienced by patients with Irritable Bowel Disease (IBD). Blocking this interaction could potentially reduce inflammatory symptoms in
Cycloadditions of siloxy alkynes with 1,2-diazines: From reaction discovery to identification of an antiglycolytic chemotype
Montavon, Timothy J.,Tuerkmen, Yunus E.,Shamsi, Noumaan A.,Miller, Christopher,Sumaria, Chintan S.,Rawal, Viresh H.,Kozmin, Sergey A.
supporting information, p. 13576 - 13579 (2014/01/06)
Cycloaddition uncovered: The title reaction produces novel polycyclic compounds with high efficiency and excellent diastereoselectivity under mild reaction conditions. A small-molecule library, synthesized using this reaction, yielded a novel chemotype which inhibited glycolytic ATP production by blocking glucose uptake in CHO-K1 cells. DMF=N,N-dimethylformamide, Tf= trifluoromethanesulfonyl, TIPS=triisopropylsilyl. Copyright
A facile synthesis of 5,6-dihydro-4H-pyrrolo[3,4-d]thiazole and other pyrrolidine-fused aromatic ring systems via one-step cyclization from diols
Yoshikawa, Kenji,Nagata, Tsutomu,Yoshino, Toshiharu,Nakamoto, Yumi,Haginoya, Noriyasu,Muto, Ryo,Mochizuki, Akiyoshi,Kanno, Hideyuki,Ohta, Toshiharu
experimental part, p. 1711 - 1720 (2012/09/07)
A facile synthetic method of 5,6-dihydro-4H-pyrrolo[3,4-d]thiazole, which is a subunit of a potent factor Xa (fXa) inhibitor was developed. This new approach employs one-step cyclization from a diol and can be applied to the syntheses of other pyrrolidine-fused aromatic ring sytems.
Functionalized isothianaphthene monomers that promote quinoidal character in donor-acceptor copolymers for organic photovoltaics
Douglas, Jessica D.,Griffini, Gianmarco,Holcombe, Thomas W.,Young, Eric P.,Lee, Olivia P.,Chen, Mark S.,Frechet, Jean M. J.
scheme or table, p. 4069 - 4074 (2012/08/07)
A series of low band gap isothianaphthene-based (ITN) polymers with various electron-withdrawing substituents and intrinsic quinoidal character were synthesized, characterized, and tested in organic photovoltaic (OPV) devices. The three investigated ITN cores contained either ester, imide, or nitrile functionalities and were each synthesized in only four linear steps. The relative electron-withdrawing strength of the three substituents on the ITN moiety was evaluated and correlated to the optical and electronic properties of ITN-based copolymers. The ester- and imide-containing p-type polymers reached device efficiencies as high as 3% in bulk heterojunction blends with phenyl C61-butyric acid methyl ester (PC61BM), while the significantly electron-deficient nitrile-functionalized polymer behaved as an n-type material with an efficiency of 0.3% in bilayer devices with poly(3-(4-n-octyl)phenylthiophene) (POPT).
Benzodithiophene and imide-based copolymers for photovoltaic applications
Braunecker, Wade A.,Owczarczyk, Zbyslaw R.,Garcia, Andres,Kopidakis, Nikos,Larsen, Ross E.,Hammond, Scott R.,Ginley, David S.,Olson, Dana C.
, p. 1346 - 1356 (2012/08/28)
Conjugated alternating copolymers were designed with low optical band gaps for organic photovoltaic (OPV) applications by considering quinoid resonance stabilization. Copolymers of thienoisoindoledione (TID) and benzodithiophene (BDT) had appreciably lower band gaps (by ~0.4 eV) than copolymers of thienopyrroledione (TPD) and BDT. In addition to intramolecular charge transfer stabilization (i.e., the "push-pull" effect), the former copolymer's quinoid resonance structure is stabilized by a gain in aromatic resonance energy in the isoindole unit. Additionally, the HOMO levels of the copolymers could be tuned with chemical modifications to the BDT monomer, resulting in open circuit voltages of greater than 1 V in photovoltaic devices. Despite the optimized band gap, TID containing polymers displayed lower photoconductance, as determined by time-resolved microwave conductivity, and decreased device efficiency (2.1% vs 4.8%) as compared with TPD analogues. These results were partially attributed to morphology, as computational modeling suggests TID copolymers have a twisted backbone, and X-ray diffraction data indicate the polymer films do not form ordered domains, whereas TPD copolymers are considerably more planar and are shown to form partially ordered domains.
Indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase
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, (2008/06/13)
The present invention relates to certain novel indane-2-mercaptoacetylamide disulfide derivatives of the formula STR1 useful as inhibitors of enkephalinase.
2-SUBSTITUTED INDANE-2-CARBOXYALKYL DERIVATIVES USEFUL AS INHIBITORS OF ENKEPHALINASE AND ACE
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, (2008/06/13)
The present invention relates to novel 2-substituted indane-2-carboxyalkyl derivatives useful as inhibitors of enkephalinase and ACE.
2-substituted indane-2-mercaptoacetylamide tricyclic derivatives useful as inhibitors of enkephalinase
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, (2008/06/13)
The present invention relates to novel 2-substitited indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.