60060-44-8Relevant academic research and scientific papers
TARGETED BIFUNCTIONAL DEGRADERS
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Page/Page column 174, (2021/04/17)
The present invention provides, in one aspect, bifunctional compounds that can be used to promote or enhance degradation of certain circulating proteins. In another aspect, the present invention provides bifunctional compounds that can be used to promote or enhance degradation of certain autoantibodies. In certain embodiments, treatment or management of a disease and/or disorder requires degradation, removal, or reduction in concentration of the circulating protein or the autoantibody in the subject. Thus, in certain embodiments, administration of a compound of the invention to the subject removes or reduces the circulation concentration of the circulating protein or the autoantibody, thus treating, ameliorating, or preventing the disease and/or disorder. In certain embodiments, the circulating protein is TNF.
Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation
Wang, Zhengyu,Shi, Xiaofan,Zhang, Huan,Yu, Liang,Cheng, Yanhua,Zhang, Hefeng,Zhang, Huibin,Zhou, Jinpei,Chen, Jing,Shen, Xu,Duan, Wenhu
, p. 128 - 152 (2017/08/10)
Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of hypoglycemia caused by over-activation of GK in islet cells and dyslipidemia caused by over-activation of intrahepatic GK. In the effort to mitigate risks of hypoglycemia and dyslipidemia while maintaining the promising efficacy of GK activator, we investigated a series of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific partial GK activators, which led to the identification of compound 72 that showed a good balance between in vitro potency and enzyme kinetic parameters, and protected β-cells from streptozotocin-induced apoptosis. Chronic treatment of compound 72 demonstrated its potent activity in regulation of glucose homeostasis and low risk of dyslipidemia with diabetic db/db mice in oral glucose tolerance test (OGTT). Moreover, acute treatment of compound 72 did not induce hypoglycemia in C57BL/6J mice even at 200 mg/kg via oral administration.
TRICYCLIC MODULATORS OF TNF SIGNALING
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Page/Page column 132, (2016/11/02)
The invention provides tricyclic heterocyclic compounds, pharmaceutically acceptable salts, prodrugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the invention may be useful for treating immunological and oncological conditions.
Synthesis of Impurities of Pramipexole Dihydrochloride
Hu, Tianwen,Yang, Feipu,Jiang, Tao,Chen, Weiming,Zhang, Jian,Li, Jianfeng,Jiang, Xiangrui,Shen, Jingshan
, p. 1899 - 1905 (2017/02/10)
Three impurities of pramipexole dihydrochloride were synthesized, and the possible generation mechanisms and the preparation methods of some impurities were reviewed. The desired configuration at C7 of 3 was built by a Mitsunobu reaction.
FUSED THIOPHENE AND THIAZOLE DERIVATIVES AS ROR GAMMA MODULATORS
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Page/Page column 100, (2015/07/16)
The present invention provides fused thiophene and thiazole derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which R1, R2, R3, R4, R5, R6, R7, X1, X2, L, m, n and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in disease(s) or disorder(s) where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the fused thiophene and thiazole derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
Monobromomalononitrile: An efficient regioselective mono brominating agent towards active methylene compounds and enamines under mild conditions
Pathak, Sudipta,Kundu, Ashis,Pramanik, Animesh
, p. 10180 - 10187 (2014/03/21)
The potential of monobromomalononitrile (MBM) as a convenient source of cationic bromine in organic bromination reaction has been explored. Studies reveal that MBM can be a good substitute for N-bromosuccinimide (NBS) in various respects. Enamines and act
IMINO COMPOUNDS AS PROTECTING AGENTS AGAINST ULTRAVIOLET RADIATIONS
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Page/Page column 35, (2014/01/08)
The present invention relates to compounds having the general Formula I: which absorb UV radiations and protect biological materials as well as non-biological materials from damaging exposure to UV radiations. The present invention also relates to formulations and compositions comprising such compounds for use in absorbing UV radiations and in protecting biological materials as well as non-biological materials against UV radiations.
UREA DERIVATIVE HAVING PI3K INHIBITORY ACTIVITY
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Page/Page column 119, (2012/03/26)
Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.
MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 100, (2011/06/25)
Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5- dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors
McIntyre, Neil A.,McInnes, Campbell,Griffiths, Gary,Barnett, Anna L.,Kontopidis, George,Slawin, Alexandra M. Z.,Jackson, Wayne,Thomas, Mark,Zheleva, Daniella I.,Wang, Shudong,Blake, David G.,Westwood, Nicholas J.,Fischer, Peter M.
supporting information; experimental part, p. 2136 - 2145 (2010/08/07)
Following the recent discovery and development of 2-anilino-4-(thiazol-5- yl)pyrimidine cyclin dependent kinase (CDK) inhibitors, a program was initiated to evaluate related ring-constrained analogues, specifically, 2-methyl- and 2-amino-N-aryl-4,5-dihydr
