191097-27-5Relevant academic research and scientific papers
Benzofuran derivatives, preparation method thereof and application of the derivatives in medicine
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, (2019/10/01)
The invention relates to benzofuran derivatives, a preparation method thereof and application of the derivatives in medicine, particularly novel benzofuran derivatives shown as a general formula (I),a preparation method thereof, pharmaceutical compositions comprising the derivatives and application thereof as therapeutic agent, especially as PAR-4 antagonists, with substitutes in the general formula (I) being defined in the description.
Novel leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry
Cao, Jiangying,Ma, Chunhua,Zang, Jie,Gao, Shuai,Gao, Qianwen,Kong, Xiujie,Yan, Yugang,Liang, Xuewu,Ding, Qin'ge,Zhao, Chunlong,Wang, Binghe,Xu, Wenfang,Zhang, Yingjie
, p. 3145 - 3157 (2018/06/01)
The over-expression of aminopeptidase N on diverse malignant cells is associated with the tumor angiogenesis and metastasis. In this report, one new series of leucine ureido derivatives containing the triazole moiety was designed, synthesized and evaluated as APN inhibitors. Among them, compound 13v showed the best APN inhibition with an IC50 value of 0.089 ± 0.007 μM, which was two orders of magnitude lower than that of bestatin (IC50 = 9.4 ± 0.5 μM). Compound 13v also showed dose-dependent anti-angiogenesis activities. Even at the lower concentration (10 μM), compound 13v presented similar anti-angiogenesis activity compared with bestatin at 100 μM in both the human umbilical vein endothelial cells (HUVECs) capillary tube formation assay and the rat thoracic aorta rings test. Moreover, compared with bestatin, 13v exhibited comparable, if not better in vivo anti-metastasis activity in a mouse H22 pulmonary metastasis model.
NOVEL SUBSTITUTED PHENYL-OXATHIAZINE DERIVATIVES, METHOD FOR PRODUCING THEM, DRUGS CONTAINING SAID COMPOUNDS AND THE USE THEREOF
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Paragraph 0385; 0386, (2014/02/15)
The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
CYCLOHEXANE DERIVATIVE COMPOUND
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Paragraph 0458-0465, (2013/08/15)
To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, -O-, -NH-, -N(C1-C3 alkyl)-, -C(=O)-, -S-, -S(O)-, -S(O2)- or a single bond.
Structure-activity relationship studies of 4-benzyl-1H-pyrazol-3-yl β-d-glucopyranoside derivatives as potent and selective sodium glucose co-transporter 1 (SGLT1) inhibitors with therapeutic activity on postprandial hyperglycemia
Fushimi, Nobuhiko,Fujikura, Hideki,Shiohara, Hiroaki,Teranishi, Hirotaka,Shimizu, Kazuo,Yonekubo, Shigeru,Ohno, Kohsuke,Miyagi, Takashi,Itoh, Fumiaki,Shibazaki, Toshihide,Tomae, Masaki,Ishikawa-Takemura, Yukiko,Nakabayashi, Takeshi,Kamada, Noboru,Ozawa, Tomonaga,Isaji, Masayuki,Kobayashi, Susumu
, p. 6598 - 6612,15 (2012/12/12)
Sodium glucose co-transporter 1 (SGLT1) plays a dominant role in the absorption of glucose in the gut and is considered a promising target in the development of treatments for postprandial hyperglycemia. A series of 4-benzyl-1H-pyrazol-3-yl β-d-glucopyran
Tandem Ugi MCR/mitsunobu cyclization as a short, protecting-group-free route to benzoxazinones with four diversity points
Banfi, Luca,Basso, Andrea,Giardini, Lorenzo,Riva, Renata,Rocca, Valeria,Guanti, Giuseppe
, p. 100 - 109 (2011/03/21)
A tandem Ugi/Mitsunobu protocol, starting from o-aminophenols, α-hydroxy acids, amines and aldehydes gives benzo[b][1,4]oxazin-3-ones of general formula 1 in two high-yielding steps, with the introduction of up to four diversity inputs. The mildness of the methodology allows the stereospecific synthesis of enantiomerically pure products as well as the introduction of additional functional groups. The overall procedure can also be carried out in a one-pot manner. A tandem Ugi/Mitsunobu protocol, starting from o-aminophenols and α-hydroxy acids, gives benzo[b][1,4]oxazin-3-ones, with the introduction of up to four diversity inputs, in two high-yielding steps. The procedure may be carried out in a one-pot fashion and has a very broad scope, also allowing the synthesis of enantiomerically pure products.
