247133-22-8Relevant articles and documents
Synthesis and biological evaluation of N-alkylated 8-oxybenz[c]azepine derivatives as selective PPARδ agonists
Luckhurst, Christopher A.,Ratcliffe, Marianne,Stein, Linda,Furber, Mark,Botterell, Sara,Laughton, David,Tomlinson, Wendy,Weaver, Richard,Chohan, Kamaldeep,Walding, Andrew
scheme or table, p. 531 - 536 (2011/02/27)
We describe the discovery of small molecule benzazepine derivatives as agonists of human peroxisome proliferator-activated receptor δ (PPARδ) that displayed excellent selectivity over the PPARα and PPARγ subtypes. Compound 8 displayed good PK in the rat a
NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 68, (2008/12/05)
Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein X, R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring
Ueno, Hiroshi,Yokota, Katsuyuki,Hoshi, Jun-Ichi,Yasue, Katsutaka,Hayashi, Mikio,Hase, Yasunori,Uchida, Itsuo,Aisaka, Kazuo,Katoh, Susumu,Cho, Hidetsura
, p. 3586 - 3604 (2007/10/03)
A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine
Amidine compounds
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, (2008/06/13)
A compound of the formula [I] wherein R1, R2and R3are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the presen
Synthesis of 2,3,4,5-tetrahydro-1H-2-benzazepines via Pummerer-type cyclization of N-arylmethyl-N-(3-phenylsulfinylpropyl) formamides
Horiguchi, Yoshie,Saitoh, Toshiaki,Terakado, Sachiko,Honda, Konomi,Kimura, Tomoko,Toda, Jun,Sano, Takehiro
, p. 967 - 984 (2007/10/03)
A construction of 1H-benzazepine ring system was achieved via a modified Pummerer reaction of N-arylmethyl-N-(3-phenylsulfinylpropyl)-formamides (5) using trifluoroacetic acid and borontrifluoride etherate. This method provides an effective synthesis of 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-2-benzazepine (10a), the synthetic intermediate of capsazepine (1), an antagonist of capsaicin and resinferatoxin.
NITROGENOUS FUSED HETEROCYCLE COMPOUNDS, PROCESS FOR THE PREPARATION THEREOF AND AGENTS CONTAINING THE SAME
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, (2008/06/13)
A nitrogen-containing condensed heterocyclic derivative of the present invention, which is a compound represented by the formula: wherein ring A represents benzene ring optionally having a further substituent, -L-represents -O-, -NR3a-, -S-, -SO-, -SO2-, -SO2NR3a-, -SO2NHCONR3a-, -SO2NHC(=NH)NR3a-, -C(=S)-, or -CONR3a- (wherein R3a and R3b represent independently hydrogen atom, cyano group, hydroxy group, amino group, a C1-6 alkyl group or a C1-6 alkoxy group), n represents an integer of 0 to 6, R is hydrogen atom or a hydrocarbon group optionally having a substituent, and may be different in repetition of n, R1 represents a hydrocarbon group optionally having a substituent or a group represented by the formula: (wherein R7 represents a hydrocarbon group optionally having a substituent), R2 represents hydrogen atom, an acyl group, a hydrocarbon group optionally having a substituent or a heterocyclic group optionally having a substituent, X represents a bond, O, S, SO, SO2 or NR4 (wherein R4 represents hydrogen atom, an acyl group or a hydrocarbon group optionally having a substituent), k and m represent independently an integer of 0 to 5, and 1k+m5, or a salt thereof, and the like, has an excellent thermal production promoting activity and the like, and is useful as an agent for preventing or treating obesity and obesity-based diseases.