70886-35-0Relevant academic research and scientific papers
Heterocyclic Derivatives of 2-Amino-4-nitrophenol
Foeldenyi,Szalontai,Szebenyi,Kvintovics,Bartik
, p. 305 - 311 (1996)
A new pathway for the synthesis of cyclic derivatives of 2-amino-4-nitrophenol by application of dibromoalkanes is described. This general method was used for the preparation of several heterocycles (partially saturated 1,4-benzoxazines, 1,5-benzoxazepine
Metal-free N-formylation of 2-aminophenols using dimethylformamide and CSA
Yang, Yuanyong,Li, Yingxian,Zhang, Zhenhua,Zhao, Yonglong,Feng, Wei
supporting information, p. 1040 - 1046 (2019/03/29)
DMF has been proved to be an efficient formylation reagent for 2-aminophenols in the presence of (±) camphorsulfonic acid (CSA) in this work. CSA works as an acid catalyst and a neutralizer of dimethyl amine which is kicked off from DMF. Both electron-wit
GLUCURONIDE PRODRUGS OF TOFACITINIB
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Page/Page column 44, (2018/09/28)
The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula (I): (Formula (I)) where A1 and R1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
GLUCURONIDE PRODRUGS OF JANUS KINASE INHIBITORS
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Paragraph 0299; 0300, (2018/12/11)
The invention relates to glucuronide prodrug compounds of Janus kinase (JAK) inhibitors having formula I: where W1, R1 and A1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
ORGANIC COMPOUNDS
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Page/Page column 108, (2010/11/27)
Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer (such as prostate or breast cancer), osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
Synthesis of new tetracycle fused acridine analogues bearing oxazole ring
Robin, Maxime,Faure, Robert,Perichaud, Alain,Galy, Jean-Pierre
, p. 981 - 988 (2007/10/03)
New acridine derivatives have been prepared via Ullman condensation involving benzoxazole (5) and 2-bromo-benzoic acid. Linear products were obtained. The structure of oxazolo[4,5-b]acridine was determined by NMR spectroscopy.
The vicarious nucleophilic substitution of hydrogen and related reactions in nitrobenzoxazoles
Makosza, Mieczyslaw,Stalewski, Jacek
, p. 7277 - 7286 (2007/10/02)
5- and 6-nitrobenzoxazoles 3 and 4 react with nucleophiles exclusively at C-2, giving ring opening products. If position 2- is blocked with phenyl substituent the reaction takes place in the carbocyclic ring affording the VNS products. 2-Methylthio-5-nitrobenzoxazole 7 and its 6-nitro isomer 8 give products which result from addition of a nucleophile to the carbocyclic ring (VNS) as well as to the heterocyclic ring (S(N)Ar and ring cleavage). 2-Methylthiobenzoxazoles can be readily converted to the corresponding benzoxazolones via oxidative hydrolysis.
