119647-73-3Relevant articles and documents
HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
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Paragraph 0014, (2015/11/16)
Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
ALKYLATED PIPERAZINE COMPOUNDS
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Paragraph 0344, (2013/05/21)
Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
PHOTOCHEMOTHERAPEUTIC HETEROCYCLIC AGENTS HAVING ANTIPROLIFERATIVE AND ANTINEOPLASTIC ACTIVITY
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Page/Page column 4, (2012/06/01)
The present invention concerns the synthesis of new analogs of angelicins, pyrrolo [3,2-h]quinoline, for the treatment of pathologies having hyperproliferative character included those having neoplastic nature. The treatment is based on the combined actio
Synthesis of pyrrolo[3,2-h]quinolinones with good photochemotherapeutic activity and no DNA damage
Barraja, Paola,Caracausi, Libero,Diana, Patrizia,Carbone, Anna,Montalbano, Alessandra,Cirrincione, Girolamo,Brun, Paola,Palu, Giorgio,Castagliuolo, Ignazio,Dall'Acqua, Francesco,Vedaldi, Daniela,Salvador, Alessia
scheme or table, p. 4830 - 4843 (2010/08/06)
In the search for new photochemotherapeutic agents, a series of derivatives of the ring system pyrrolo[3,2-h]quinoline - bioisosters of the angular furocoumarin angelicin - were synthesized through a four-step synthetic approach, in reasonable overall yields. Eight of the synthesized derivatives showed a remarkable phototoxicity against a panel of four human tumor cell lines and a great dose UV-A dependence, reaching IC50 values at submicromolar level. The mode of cellular death photoinduced by pyrrolo[3,2-h]quinolines was evaluated through a series of flow cytometric analysis and other tests were performed to clarify their mechanism of action.
New strategy for indole synthesis from ethyl pyrrole-2-carboxylate (synthetic studies on indoles and related compounds. XXXIX)
Tani, Masanobu,Ariyasu, Takahiro,Ohtsuka, Masanori,Koga, Terumi,Ogawa, Yumi,Yokoyama, Yuusaku,Murakami, Yasuoki
, p. 55 - 61 (2007/10/03)
As a synthetic application of the previously reported C4-acylation of ethyl pyrrole-2-carboxylate (1), a new strategy for indole synthesis was developed. Ethyl pyrrole-2-carboxylate (1) was allowed to react with succinic anhydride or 3-methoxycarbonylpropionyl chloride to give, in good yield, a C4-succinyl derivative of 1, which was converted into ethyl 7-oxo-4,5,6,7- tetrahydroindole-2-carboxylate (6) as a key intermediate for indole synthesis. Starting from 6, several indoles functionalized on the benzene moiety were synthesized.
Non-peptidic Inhibitors of Human Leukocyte Elastase. 4. Design, Synthesis, and in Vitro and in Vivo Activity of a Series of β-Carbolinone-Containing Trifluoromethyl Ketones
Veale, Chris A.,Damewood, James R.,Steelman, Gary B.,Bryant, Craig,Gomes, Bruce,Williams, Joseph
, p. 86 - 97 (2007/10/02)
A novel series of human leukocyte elastase (HLE) inhibitors containing the β-carbolinone ring system are reported.The design of these trifluoromethyl ketone-based inhibitors used a combination of structural information obtained from X-ray crystallography
THE FRIEDEL-CRAFTS ACYLATION OF ETHYL PYRROLE-2-CARBOXYLATE. SCOPE, LIMITATIONS, AND APPLICATION TO SYNTHESIS OF 7-SUBSTITUTED INDOLES
Murakami, Yasuoki,Tani, Masanobu,Ariyasu, Takahiro,Nishiyama, Chika,Watanabe, Toshiko,Yokoyama, Yuusaku
, p. 1855 - 1860 (2007/10/02)
The Friedel-Crafts acylation of ethyl pyrrole-2-carboxylate (3) was studied under a variety of conditions using various Lewis acids and acyl chlorides.The acylation with some Lewis acids such as BF3*OEt2 gave a mixture of 4- and 5-acyl derivatives (5 and
