24334-19-8Relevant academic research and scientific papers
ROCK INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF
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, (2022/01/24)
The invention relates to a ROCK inhibitor represented by formula (I), its preparation method and its use. The ROCK inhibitor has excellent ROCK inhibition activity, in particular good selective inhibition on ROCK2 kinase, has good safety and metabolic stability, and has high bioavailability. The process of preparing the ROCK inhibitor is simple, and the ROCK inhibitor is easy to purify, and therefore offers good prospects for application.
THIENO[3,2-B] PYRROLE[3,2-D]PYRIDAZINONE DERIVATIVES AND THEIR USE AS PKM2 DERIVATIVES FOR THE TREATMENT OF CANCER, OBESITY AND DIABETES RELATED DISORDERS
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Page/Page column 120, (2020/08/28)
Described herein are compounds that regulate pyruvate kinase activity, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I) wherein R2, L1-L2, U1-U7, m, ring A, and Q are as defined herein.
AMPK INHIBITORS
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Page/Page column 30, (2019/06/17)
The 5'-AMP-activated protein kinase AMPK functions as a master switch to maintain cellular and whole-body energy homeostasis and abnormal activity profiles of AMPK may cause pathological disorders. The present invention relates to a series of compounds (I
Asymmetric Hydrogenation of Azaindoles: Chemo- and Enantioselective Reduction of Fused Aromatic Ring Systems Consisting of Two Heteroarenes
Makida, Yusuke,Saita, Masahiro,Kuramoto, Takahiro,Ishizuka, Kentaro,Kuwano, Ryoichi
supporting information, p. 11859 - 11862 (2016/11/16)
High enantioselectivity was achieved for the hydrogenation of azaindoles by using the chiral catalyst, which was prepared from [Ru(η3-methallyl)2(cod)] and a trans-chelating bis(phosphine) ligand (PhTRAP). The dearomative reaction exclusively occurred on the five-membered ring, thus giving the corresponding azaindolines with up to 97:3 enantiomer ratio.
Synthesis of the new ring system bispyrido[4',3':4,5]pyrrolo [1,2-a:1',2'-d]pyrazine and its deaza analogue
Parrino, Barbara,Span, Virginia,Carbone, Anna,Barraja, Paola,Diana, Patrizia,Cirrincione, Girolamo,Montalbano, Alessandra
, p. 13342 - 13357 (2015/02/19)
Derivatives of the new ring systems bispyrido[4',3':4,5]pyrrolo[1,2-a:1',2'-d] pyrazine-6,13-dione and its deaza analogue pyrido[4",3":4',5']pyrrolo-[1',2':4,5]pyrazino [1,2-a]indole-6,13-dione were conveniently synthesized through a four-step sequence. Symmetrical derivatives of the former ring system were obtained through self condensation. On the other hand, condensation of 6-azaindole carboxylic acid with indole 2-carboxylic acid afforded the deaza analogue ring system. Derivatives of the title ring system were tested by the National Cancer Institute (Bethesda, MD, USA) and four of them exhibited modest activity against MCF7 (a breast cancer cell line) and/or UO-31 (a renal cancer cell line).
Detailed structure-activity relationship of indolecarboxamides as H 4 receptor ligands
Engelhardt, Harald,De Esch, Iwan J.P.,Kuhn, Daniel,Smits, Rogier A.,Zuiderveld, Obbe P.,Dobler, Julia,Mayer, Moriz,Lips, Sebastian,Arnhof, Heribert,Scharn, Dirk,Haaksma, Eric E.J.,Leurs, Rob
experimental part, p. 660 - 668 (2012/09/07)
A series of 76 derivatives of the indolecarboxamide 1 were synthesized, which allows a detailed SAR investigation of this well known scaffold. The data enable the definition of a predictive QSAR model which identifies several compounds with an activity comparable to 1. A selection of these new H 4R antagonists was synthesized and a comparison of predicted and measured values demonstrates the robustness of the model (47-55). In addition to the H4-receptor activity general CMC and DMPK properties were investigated. Some of the new analogs are not only excellently soluble, but display a significantly increased half-life in mouse liver microsomes as well. These properties qualify these compounds as a possible new standard for future in vivo studies (e.g 51, 52 and 55). Moreover, the current studies also provide valuable information on the potential receptor ligand interactions between the indolcarboxamides and the H4R protein.
N-SUBSTITUTED AZAINDOLES AND METHODS OF USE
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Page/Page column 16-17, (2010/09/05)
The invention relates to N-substituted azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to N-substituted azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
N-(ARYLALKYL)-1H-PYRROLOPYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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Page/Page column 8, (2008/12/05)
The invention concerns compounds of general formula (I), wherein n, the pyrrolopyridine ring, X, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.
Substituted Pyrrolopyridines, Compositions Containing Them, Manufacturing Process Therefor and Use Thereof
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Page/Page column 5; 7-8, (2008/12/06)
The invention relates to compounds of formula (I): wherein Ra, R1, Ar, L, A, W, Y, and Z are as defined in the disclosure; to compositions containing them; and to the preparation and use thereof, in particular as anticancer agents.
Rapid and efficient microwave-assisted synthesis of 4-, 5-, 6- and 7-azaindoles
Lachance, Nicolas,April, Myriam,Joly, Marc-Andre
, p. 2571 - 2577 (2007/10/03)
Under microwave irradiation conditions, the imines/enamines formed between aminopyridines and ketones are converted in moderate to good yields to the corresponding 4-, 5-, 6- or 7-azaindoles via the Hegedus-Mori-Heck reaction (intramolecular Heck reaction
