73998-95-5Relevant academic research and scientific papers
Development of a Rapid Scale-Up Synthesis of (S)-N-(8-((2-Amino-2,4-dimethylpentyl)oxy)-5H-chromeno[3,4-c]pyridin-2-yl)acetamide, a Potent Adaptor-Associated Kinase 1 Inhibitor
Li, Jianqing,Smith, Daniel,Pawluczyk, Joseph,Krishnananthan, Subramaniam,Wang, Bei,Hou, Xiaoping,Zhao, Rulin,Kempson, James,Sun, Dawn,Yip, Shiuhang,Wu, Dauh-Rurng,Maddala, Nageswararao,Vetrichelvan, Muthalagu,Gupta, Anuradha,Macor, John E.,Dzierba, Carolyn D.,Mathur, Arvind
supporting information, p. 437 - 446 (2022/02/09)
(S)-N-(8-((2-Amino-2,4-dimethylpentyl)oxy)-5H-chromeno[3,4-c]pyridin-2-yl)acetamide (1) is a potent adaptor-associated kinase 1 inhibitor, which may have the potential to treat neuropathic pain and other neurological disorders including schizophrenia, Parkinson’s disease, bipolar disorder, and Alzheimer’s disease. For preclinical studies, a substantial amount of high-quality material was required. The original discovery route for the preparation of this compound suffered from scale-up issues that included a very low-yielding C-O coupling step and the use of expensive and toxic reagents. This paper describes a rapid scale-up synthesis accomplished in eight steps, which involves the coupling of phenol 17 with oxathiazolidine 18 as the key transformation.
TRICYCLIC KINASE INHIBITORS AND USE THEREOF
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Paragraph 0179-0181, (2021/03/13)
The present application provides novel compounds that are inhibitors of kinases, including AMPK-related kinases like NUAK1, NUAK2, SIK1, SIK2, SIK3, MARK1, MARK2, MARK3, MARK4, as well as AURKA, AURKB, AURKC, CLK1, CLK2, DCAMKL2, MAPK7, MKNK2, PIK3CD, PKN3, RET, TAOK1, TAOK2, TAOK3, ULK2 and their mutants. The application also provides compositions, including pharmaceutical compositions, kits that include compounds, and methods of making and using compounds. The compounds provided herein are useful in treating diseases, disorders, or conditions that are mediated by these kinases.
CARBOXAMIDES AS UBIQUITIN-SPECIFIC PROTEASE INHIBITORS
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Paragraph 00289, (2019/02/25)
The present disclosure relates to modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25, pharmaceutical compositions comprising the inhibitors, and methods of using the inhibitors. The modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25 can be useful in the treatment of cancers, among other ailments.
Synthesis and antibacterial evaluation of hydrazone derivatives bearing 6-chlorothieno[3,2-c]pyridine Moiety
Sree Lakshmana Rao,Basaveswara Rao, Mandava V.,Prasad
, p. 627 - 632 (2019/02/06)
The present investigation describes the overall preparation of 6-chlorothieno[3,2-c]pyridine-2-carbohydrazide-hydrazone subsidiaries (7a-r) from industrially accessible ethyl-4,6-dichloronicotinate as starting material. The synthesis of these derivatives
3,4-dihydropyrido[4,3-d]pyrimidine derivative, and preparation method and use thereof
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Paragraph 0069; 0072; 0083-0085, (2019/10/07)
The invention relates to a 3,4-dihydropyrido[4,3-d]pyrimidine derivative, and a preparation method and a use thereof. The compound is a compound represented by formula I, or a pharmaceutically acceptable salt or stereoisomer or tautomer thereof, and R to R are as defined in the description.
BICYCLIC PROLINE COMPOUNDS
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Paragraph 0284-0287, (2018/02/22)
The invention is concerned with the compounds of formula (I) and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
Fibroblast growth factor receptor selective inhibitor and application thereof
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Paragraph 0158; 0160; 0161, (2017/08/02)
The invention relates to a fibroblast growth factor receptor selective inhibitor and application thereof. The invention provides a compound of a formula (I), a three-dimensional isomer, a tautomer or a pharmaceutically acceptable salt thereof, and an appl
Fibroblast growth factor receptor selective inhibitor and applications thereof
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Paragraph 0162; 0167-0169, (2017/08/23)
The invention discloses a fibroblast growth factor receptor selective inhibitor and applications thereof. The invention provides a compound as shown in a formula (I), and a stereoisomer, a tautomer or pharmaceutically accepted salts thereof, and applicati
1-(HET)ARYLSULFONYL-(PYRROLIDINE OR PIPERIDINE)-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS
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Paragraph 0980; 0981; 0982, (2016/09/22)
The invention is concerned with the compounds of formula I and salts thereof and other compounds of formulas II-IX as disclosed herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formulas I-IX as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain or asthma.
COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS
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Page/Page column 76; 77, (2015/03/28)
The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
