- METHOD FOR PRODUCING NITROGEN-CONTAINING AROMATIC AMIDE, METHOD FOR PRODUCING PYRROLE-IMIDAZOLE POLYAMIDE, AND COMPOUND
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To provide a method for producing a nitrogen-containing aromatic amide that is capable of using a monomer unit obtained under milder reaction condition and uses catalytic amide bond formation, and a method for producing a pyrrole-imidazole polyamide. [1] A method for producing a nitrogen-containing aromatic amide, including reacting a compound 1 represented by the general formula (1) and a compound 2 represented by the general formula (2) in the presence of a transition metal catalyst and a base, so as to provide a compound 3 represented by the general formula (3). [2] A method for producing a pyrrole-imidazole polyamide, including using the compound 3 obtained by the production method according to the item [1]. [3] A compound represented by the general formula (2aa), the general formula (2ab), the general formula (2ac), or the general formula (2ad).
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Paragraph 0088; 0288; 0289; 0290; 0291; 0292; 0293; 0294
(2019/04/05)
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- Synthesis of pyrrole-imidazole polyamide oligomers based on a copper-catalyzed cross-coupling strategy
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Pyrrole-imidazole (Py-Im) polyamides are useful tools for chemical biology and medicinal chemistry studies due to their unique binding properties to the minor groove of DNA. We developed a novel method of synthesizing Py-Im polyamide oligomers based on a Cu-catalyzed cross-coupling strategy. All four patterns of dimer fragments could be synthesized using a Cu-catalyzed Ullmann-type cross-coupling with easily prepared monomer units. Moreover, we demonstrated that pyrrole dimer, trimer, and tetramer building blocks for Py-Im polyamide synthesis were accessible by combining site selective iodination of the pyrrole/pyrrole coupling adduct.
- Shiga, Naoki,Takayanagi, Shihori,Muramoto, Risa,Murakami, Tasuku,Qin, Rui,Suzuki, Yuta,Shinohara, Ken-ichi,Kaneda, Atsushi,Nemoto, Tetsuhiro
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supporting information
p. 2197 - 2200
(2017/04/27)
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- INDOLIN-2-ONE DERIVATIVES
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The present invention is concerned with indolin-2-one derivatives of general formula (I) wherein the substituents are defined in claim 1. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of s
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Page/Page column 53
(2017/06/15)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
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Page/Page column 32
(2012/12/13)
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- GAMMA SECRETASE MODULATORS
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The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions conta
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Page/Page column 132
(2009/07/17)
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