- [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
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The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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Page/Page column 146-147
(2021/02/19)
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- Novel indole sulfides as potent HIV-1 NNRTIs
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In a previous communication we described a series of indole based NNRTIs which were potent inhibitors of HIV replication, both for the wild type and K103N strains of the virus. However, the methyl ether functionality on these compounds, which was crucial for potency, was susceptible to acid promoted indole assisted SN1 substitution. This particular problem did not bode well for an orally bioavailable drug. Here we describe bioisosteric replacement of this problematic functional group, leading to a series of compounds which are potent inhibitors of HIV replication, and are acid stable.
- Brigg, Siobhan,Pribut, Nicole,Basson, Adriaan E.,Avgenikos, Moscos,Venter, Reinhardt,Blackie, Margaret A.,van Otterlo, Willem A.L.,Pelly, Stephen C.
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supporting information
p. 1580 - 1584
(2016/12/03)
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- Expedient one-pot synthesis of indolo[3,2-c]isoquinolines via a base-promoted N-Alkylation/tandem cyclization
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A transition metal-free, one-pot protocol has been developed for the synthesis of 11H-indolo[3,2-c]isoquinolin-5-amines via the atom economical annulation of ethyl (2-cyano-phenyl)carbamates and 2-cyanobenzyl bromides. This method proceeds via sequential
- Nguyen, Huy H.,Fettinger, James C.,Haddadin, Makhluf J.,Kurth, Mark J.
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supporting information
p. 5429 - 5433
(2015/09/15)
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- Synthesis of the new ring system pyrrolizino[2,3-b]indol-4(5H)-one
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Derivatives of the new ring system pyrrolizino[2,3-b]indol-4(5H)-one were prepared in four steps starting from substituted benzonitriles bearing a functionalized amino group in the adjacent position. The unsubstituted- and the dimethoxy-pyrrolizinoindolon
- Diana, Patrizia,Stagno, Antonina,Barraja, Paola,Montalbano, Alessandra,Carbone, Anna,Parrino, Barbara,Cirrincione, Girolamo
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body text
p. 3374 - 3379
(2011/06/11)
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- Synthesis and biological evaluation of 1-methyl-2-(3′,4′, 5′-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors
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The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compounds modified with respect to positions C-4 to C-7 with different moieties (chloro, methyl, or methoxy). Additional structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as methyl or ethyl. We have identified 1-methyl-2-(3,4,5-trimethoxybenzoyl)-3-amino-7-methoxyindole as a new highly potent antiproliferative agent that targets tubulin at the colchicine binding site and leads to apoptotic cell death.
- Romagnoli, Romeo,Baraldi, Pier Giovanni,Sarkar, Taradas,Carrion, Maria Dora,Cara, Carlota Lopez,Cruz-Lopez, Olga,Preti, Delia,Tabrizi, Mojgan Aghazadeh,Tolomeo, Manlio,Grimaudo, Stefania,Di Cristina, Antonella,Zonta, Nicola,Balzarini, Jan,Brancale, Andrea,Hsieh, Hsing-Pang,Hamel, Ernest
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p. 1464 - 1468
(2008/09/20)
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- Halogen substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
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The invention relates to halogen substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1, R2, R3, R4 and n are as defined in the specification and to pharmaceutica
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Page/Page column 15
(2008/06/13)
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- Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
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The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising administering a therapeutically effective amount of a substituted
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Page/Page column 15
(2010/10/20)
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- Triazoloquinazoline compounds, and their methods of preparation, pharmaceutical compositions, and uses
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[1,2,4]triazolo[1,5-c]quinazoline compounds of the formula STR1 wherein R1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R2 is hydrogen or lower alkyl; X is oxygen or NR3, R3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N--R3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N--R3.
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