80074-34-6Relevant articles and documents
MODIFIED PROTEINS AND PROTEIN DEGRADERS
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Paragraph 001656-001658, (2021/12/08)
Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
Discovery of novel high potent and cellular active ADC type PTP1B inhibitors with selectivity over TC-PTP via modification interacting with C site
Du, Yongli,Zhang, Yanhui,Ling, Hao,Li, Qunyi,Shen, Jingkang
, p. 692 - 700 (2018/01/01)
PTP1B serving as a key negative regulator of insulin signaling is a novel target for type 2 diabetes and obesity. Modification at ring B of N-{4-[(3-Phenyl-ureido)-methyl]-phenyl}-methane-sulfonamide template to interact with residues Arg47 and Lys41 in t
Novel substituted sulfamide compound, preparation method and application thereof as PTP1B inhibitor
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Paragraph 0019; 0023, (2017/06/28)
The invention relates to a novel substituted sulfamide compound of a structure of a formula I as shown in the description, a pharmaceutically acceptable salt of the novel substituted sulfamide compound, a preparation method, and relates to a medicinal composition comprising the compound of the formula I or a pharmaceutically acceptable salt of the compound. The compound of the formula I or the pharmaceutically acceptable salt of the compound has activity of inhibiting protein tyrosine phosphatase 1B (PTP1B), so that the compound or the pharmaceutically acceptable salt of the compound has an application of preparing a medicine for preventing/treating symptoms or diseases such as hyperglycemia and type-2 diabetes.
Novel urea protein tyrosine phosphatase 1B inhibitor, and preparation method, pharmaceutical composition and application thereof
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Paragraph 0027-0028, (2017/01/09)
The invention relates to novel urea compounds with a structure as shown in a general formula I in the specification or pharmaceutically acceptable salts thereof, wherein the urea compounds and the pharmaceutically acceptable salts thereof can be used as a novel inhibitor of protein tyrosine phosphatase (PTP) 1B. The invention also relates to a pharmaceutical composition containing the compounds as shown in the general formula I or the pharmaceutically acceptable salts of the compounds. The compounds as shown in the general formula I or the pharmaceutically acceptable salts thereof have the effect of inhibiting the activity of the protein tyrosine phosphatase 1B (PTP1B), and can be applied in preparation of drugs capable of preventing and/or treating symptoms or diseases like hyperglycemia and type 2 diabetes.
5-[3-(2,5-diethoxy-4-methylsulfonyl-benzyl)-ureido]-2-ethoxylmethyl benzoate new compound and preparation method and application thereof
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Paragraph 0010, (2017/05/02)
The invention provides a new compound. The name of the compound is 5-[3-(2,5-diethoxy-4-methylsulfonyl-benzyl)-ureido]-2-ethoxylmethyl benzoate; molecular weight of the compound is 509.5; and structure of the compound is as shown in the structural formula (compound 1). Meanwhile, the invention provides a preparation method of the compound 1. The compound provided by the invention has good drug-likeness and can be used in the research field of new drugs, especially in the research field of type-II diabetes innovative drugs.
COMPOUNDS AND THEIR SALTS SPECIFIC TO THE PPAR RECEPTORS AND THE EGF RECEPTORS AND THEIR USE IN THE MEDICAL FIELD
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Paragraph 0040, (2013/03/26)
Therefore the present invention relates specifically to the compounds of general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising H, —CnH2n-1, a linear or branched alkyl group having from 1 to 6
Syntheses and studies of hydantoin derivatives as potential anti-tuberculosis inhibitors
Liu, Yan,Zhong, Wu,Li, Song
experimental part, p. 133 - 136 (2012/06/18)
A short and efficient synthesis of (Z)-2-substituted-5-(4-((2-substitued-5- oxoimidazolidin-4-ylidene)methyl)benzamido)benzoic acid derivatives (8a-g) as potential type of FabH inhibitors is described. Their structures were confirmed by MS, NOE and 1H NMR.
Design and Synthesis of Novel Cyclooxygenase-1 Inhibitors as Analgesics: 5-Amino-2-ethoxy-N-(substituted-phenyl)benzamides
Fukai, Ryosuke,Zheng, Xiaoxia,Motoshima, Kazunori,Tai, Akihiro,Yazama, Futoshi,Kakuta, Hiroki
experimental part, p. 550 - 560 (2011/12/22)
We previously found that N-(4-aminophenyl)-4-trifluoromethylbenzamide (TFAP), a COX-1 inhibitor, exhibits an analgesic effect without causing gastric damage. Unfortunately, TFAP causes reddish purple coloration of urine, and its analgesic effect is less potent than that of indomethacin. Herein we describe our study focusing on the development of 4- and 5-amino-2-alkoxy-N-phenylbenzamide scaffolds, designed on the basis of the structures of TFAP and parsalmide, another known COX-1 inhibitory analgesic agent. 5-Amino-2-ethoxy-N-(2- or 3-substituted phenyl)benzamide derivatives exhibited analgesic activity in a murine acetic acid induced writhing test. Among these compounds, 5-amino-2-ethoxy-N-(2-methoxyphenyl)benzamide (9v) possesses potent COX-1 inhibitory and analgesic activities, similar to those of indomethacin. In addition, 5-amino-2-ethoxy-N-(3-trifluoromethylphenyl)benzamide (9g) showed a more potent analgesic effect than indomethacin or 9v without causing apparent gastric damage or coloration of urine, although its COX-1 inhibitory activity was weaker than that of indomethacin or 9v. Thus, 9g and 9v appear to be promising candidates for analgesic agents and are attractive lead compounds for further development of COX-1 inhibitors.
Compounds and their salts specific to the PPAR receptors and the EGF receptors and their use in the medical field
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Page/Page column 8, (2009/05/28)
Therefore the present invention relates specifically to the compounds of general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising H, —CnH2n-1, a linear
