182748-72-7Relevant academic research and scientific papers
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
Khan, Sajid,Zhang, Xuan,Lv, Dongwen,Zhang, Qi,He, Yonghan,Zhang, Peiyi,Liu, Xingui,Thummuri, Dinesh,Yuan, Yaxia,Wiegand, Janet S.,Pei, Jing,Zhang, Weizhou,Sharma, Abhisheak,McCurdy, Christopher R.,Kuruvilla, Vinitha M.,Baran, Natalia,Ferrando, Adolfo A.,Kim, Yong-mi,Rogojina, Anna,Houghton, Peter J.,Huang, Guangcun,Hromas, Robert,Konopleva, Marina,Zheng, Guangrong,Zhou, Daohong
, p. 1938 - 1947 (2019)
B-cell lymphoma extra large (BCL-XL) is a well-validated cancer target. However, the on-target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as ABT263, as safe and effective anticancer agents. To reduce
IMPROVED APELIN RECEPTOR (APJ) AGONISTS AND USES THEREOF
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Paragraph 00222, (2017/07/05)
This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.
ACYLSULFONAMIDE DERIVATIVES FOR TREATING SENESCENCE-ASSOCIATED DISEASES AND DISORDERS
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Paragraph 0319; 0320, (2017/07/14)
Compounds represented by Formula (I) and (II) and salts thereof are described herein. The compounds or salts of Formula (I) and (II) may be used to treat senescence-associated diseases and disorders.
Novel heteroaryl butanoic acid derivatives
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Page/Page column 29-31, (2017/08/02)
The present invention describes novel heteroaryl butanoic acid derivatives that are good drug candidates especially with regard to leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel he
HETEROARYL BUTANOIC ACID DERIVATIVES AS LTA4H INHIBITORS
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Page/Page column -32, (2015/07/07)
The present invention describes novel heteroaryl butanoic acid derivatives that are good drug candidates especially with regard to leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel he
Stereoselective synthesis of both enantiomers of trans-2- (diphenylmethylideneamino)cyclopropanecarboxylic acid using a chiral pool approach and their incorporation in dipeptides
Meiresonne, Tamara,Mangelinckx, Sven,De Kimpe, Norbert
, p. 9566 - 9571,6 (2020/08/20)
The stereoselective synthesis of (1R,2R)- and (1S,2S)-trans-2- (diphenylmethylideneamino)cyclopropanecarboxylic acid has been accomplished in six steps starting from (2S)- and (2R)-β-benzyl N-(tert-butoxycarbonyl) aspartate, respectively. The key-step in
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors
Yoshikawa, Kenji,Yoshino, Toshiharu,Yokomizo, Yoshihiro,Uoto, Kouichi,Naito, Hiroyuki,Kawakami, Katsuhiro,Mochizuki, Akiyoshi,Nagata, Tsutomu,Suzuki, Makoto,Kanno, Hideyuki,Takemura, Makoto,Ohta, Toshiharu
scheme or table, p. 2133 - 2140 (2011/04/24)
We previously reported on a series of cyclohexanediamine derivatives as highly potent factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an alternative scaffold. Ethylenediamine derivatives possessing a substituent at the C1 position in S configuration and phenylenediamine derivatives possessing a substituent at the C5 position demonstrated moderate to strong anti-fXa activity. Further SAR studies led to the identification of compound 30h which showed both good in vitro activity (fXa IC50 = 2.2 nM, PTCT2 = 3.9 μM) and in vivo antithrombotic efficacy.
Preparative synthesis of β-amino alcohols from α-amino dicarboxylic acid derivatives
Kirillova, Yu. G.,Baranov,Prokhorov,Esipova,Shvets
experimental part, p. 1315 - 1317 (2010/01/11)
A low-expensive preparative procedure has been developed for the synthesis of protected β-amino alcohols from α-amino dicarboxylic acid derivatives.
The synthesis of Fmoc-O-allyl β-serine
Bergman, Ylva,Ciampini, Marisa,Jalal, Sania,Lagiakos, Helen Rachel,Aguilar, Marie-Isabel,Perlmutter, Patrick
experimental part, p. 2861 - 2863 (2009/06/28)
Two concise routes for the synthesis of the title amino acid have been developed. The first route employs Seebach's general approach [Seebach, D.; Lelais, G.; Micuch, P.; Josien-Lefebvre, D.; Rossi, F. Helv. Chim. Acta 2004, 87, 3131] with Arndt Eistert h
Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids
Sagi, Kazuyuki,Nakagawa, Tadakiyo,Yamanashi, Masahiro,Makino, Shingo,Takahashi, Mitsuo,Takayanagi, Masaru,Takenaka, Kaoru,Suzuki, Nobuyasu,Oono, Seiji,Kataoka, Noriyasu,Ishikawa, Kohki,Shima, Sayaka,Fukuda, Yumiko,Kayahara, Takashi,Takehana, Shunji,Shima, Yoichiro,Tashiro, Kazumi,Yamamoto, Hiroshi,Yoshimoto, Ryota,Iwata, Seinosuke,Tsuji, Takashi,Sakurai, Kuniya,Shoji, Masataka
, p. 1845 - 1857 (2007/10/03)
An inhibitor of factor Xa (fXa), the m-substituted benzamidine AXC1578 (1a), was structurally modified with the aim of increasing its potency. In particular, pyruvic acid and propionic acid substituents were incorporated into the P1 benzamidine moiety to
