- Organic compound and organic electroluminescent device containing same
-
The invention relates to an organic compound, which is characterized by having a structure as shown in (1), wherein L1 and L2 are respectively and independently selected from a single bond, a substituted or unsubstituted C6-C30 arylene group or a substituted or unsubstituted C3-C30 heteroarylene group; Arl and Ar2 are respectively and independently selected from a substituted or unsubstituted C6-C30 aryl group or a substituted or unsubstituted C3-C30 heteroaryl group; R is halogen, a cyano group, an alkyl group, a substituted or unsubstituted C6-C30 aryl group or a substituted or unsubstituted C3-C30 heteroaryl group; and n represents an integer of 0-3.
- -
-
Paragraph 0102-0105
(2021/05/05)
-
- COMPOUNDS FOR TREATING HUNTINGTON'S DISEASE
-
The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted bicyclic heteroaryl compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
- -
-
Page/Page column 124
(2019/01/06)
-
- Application of Suzuki–Miyaura and Buchwald–Hartwig Cross-coupling Reactions to the Preparation of Substituted 1,2,4-Benzotriazine 1-Oxides Related to the Antitumor Agent Tirapazamine
-
Many 1,2,4-benzotriazine 1,4-dioxides display the ability to selectively kill the oxygen-poor cells found in solid tumors. As a result, there is a desire for synthetic routes that afford access to substituted 1,2,4-benzotriazine 1-oxides that can be used as direct precursors in the synthesis of 1,2,4-benzotriazine 1,4-dioxides. Here we describe the use of Suzuki–Miyaura and Buchwald–Hartwig cross-coupling reactions for the construction of various 1,2,4-benzotriazine 1-oxide analogs bearing substituents at the 3-position, 6-position, and 7-position.
- Sarkar, Ujjal,Hillebrand, Roman,Johnson, Kevin M.,Cummings, Andrea H.,Phung, Ngoc Linh,Rajapakse, Anuruddha,Zhou, Haiying,Willis, Jordan R.,Barnes, Charles L.,Gates, Kent S.
-
p. 155 - 160
(2017/02/05)
-
- SUBSTITUTED QUINOXALINES AND BENZOTRIAZINE P70S6 KINASE INHIBITORS
-
The invention provides compounds that inhibit or modulate the activity of p70S6 kinase, the compounds being of the formula (0), or a salt, tautomer or N-oxide thereof; wherein: X1 is N or N+(0-); X2 is N or CH; Q1 is an optionally substituted C1-8 alkylene; Q2 is a bond or an optionally substituted C1-8 alkylene group; R1 is selected from hydrogen and a group Cy1; Cy1 is an optionally substituted 4 to 7 membered monocyclic non-aromatic carbocyclic or heterocyclic group containing 0, 1 or 2 heteroatom ring members selected from O and S and oxidised forms of S; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine, C1-2 alkyl and C1-2 alkoxy, wherein each C1-2 alkyl and C1-2 alkoxy is optionally substituted with two or more fluorine atoms; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring Ar2 is an optionally substituted bicyclic 8 to 1 1 -membered heteroaryl group containing 1, 2, 3 or 4 heteroatom ring members selected from O, N and S. The compounds are useful in medicine, for example in the treatment of a disease or condition selected from cancers (e.g. triple negative breast cancer, brain tumours and brain metastases arising from non-brain cancers), neurodevelopmental diseases (e.g. Fragile X syndrome) and neurodegenerative diseases.
- -
-
Page/Page column 104
(2016/11/14)
-
- Discovery and optimization of benzotriazine Di-N-oxides targeting replicating and nonreplicating mycobacterium tuberculosis
-
Compounds bactericidal against both replicating and nonreplicating Mtb may shorten the length of TB treatment regimens by eliminating infections more rapidly. Screening of a panel of antimicrobial and anticancer drug classes that are bioreduced into cytotoxic species revealed that 1,2,4-benzotriazine di-N-oxides (BTOs) are potently bactericidal against replicating and nonreplicating Mtb. Medicinal chemistry optimization, guided by semiempirical molecular orbital calculations, identified a new lead compound (20q) from this series with an MIC of 0.31 μg/mL against H37Rv and a cytotoxicity (CC 50) against Vero cells of 25 μg/mL. 20q also had equivalent potency against a panel of single-drug resistant strains of Mtb and remarkably selective activity for Mtb over a panel of other pathogenic bacterial strains. 20q was also negative in a L5178Y MOLY assay, indicating low potential for genetic toxicity. These data along with measurements of the physiochemical properties and pharmacokinetic profile demonstrate that BTOs have the potential to be developed into a new class of antitubercular drugs.
- Chopra, Sidharth,Koolpe, Gary A.,Tambo-Ong, Arlyn A.,Matsuyama, Karen N.,Ryan, Kenneth J.,Tran, Tran B.,Doppalapudi, Rupa S.,Riccio, Edward S.,Iyer, Lalitha V.,Green, Carol E.,Wan, Baojie,Franzblau, Scott G.,Madrid, Peter B.
-
p. 6047 - 6060
(2012/09/05)
-
- SUBSTITUTED BENZOTRIAZINES AND QUINOXALINES AS INHIBITORS OF P7OS6 KINASE
-
The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X1 is N or N+(O ); X2 is N or CH; Q is a C1-3 alkylene group; R1 is selected from hydrogen, C1-4 hydrocarbyl and hydroxy-C2-4 hydrocarbyl; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.
- -
-
Page/Page column 60; 61
(2010/12/26)
-
- PHARMACEUTICAL COMPOUNDS
-
The invention provides compounds of the formulae (1), (2) and (3): (1, 2, 3), or salts, solvates or tautomers thereof; wherein G, A,v, m, Xa, Xb, Xc, Xd, Xe, R2, R3, R4, Ar1, Ar2, R6, R10, R11, R12 and R13 are as defined in the claims. The compounds have activity against various kinases or, in the case of N-oxides, are reduced in hypoxic tissues to give compounds having kinase inhibiting activity.
- -
-
Page/Page column 92
(2008/12/05)
-
- Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine-a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays
-
We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines
- Noronha, Glenn,Barrett, Kathy,Boccia, Antonio,Brodhag, Tessa,Cao, Jianguo,Chow, Chun P.,Dneprovskaia, Elena,Doukas, John,Fine, Richard,Gong, Xianchang,Gritzen, Colleen,Gu, Hong,Hanna, Ehab,Hood, John D.,Hu, Steven,Kang, Xinshan,Key, Jann,Klebansky, Boris,Kousba, Ahmed,Li, Ge,Lohse, Dan,Mak, Chi Ching,McPherson, Andrew,Palanki, Moorthy S.S.,Pathak, Ved P.,Renick, Joel,Shi, Feng,Soll, Richard,Splittgerber, Ute,Stoughton, Silva,Tang, Suhan,Yee, Shiyin,Zeng, Binqi,Zhao, Ningning,Zhu, Hong
-
p. 602 - 608
(2007/10/03)
-
- HETEROCYCLIC TRIAZINES AS HYPOXIC SELECTIVE PROTEIN KINASE INHIBITORS
-
The invention relates to novel heterocyclic triazines which are useful as hypoxic selective cytotoxic agents that mediate and/or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation by administering effective amounts of such compounds.
- -
-
Page/Page column 44-45
(2010/11/25)
-
- Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors
-
We report the discovery and preliminary SAR studies of a series of structurally novel benzotriazine core based small molecules as inhibitors of Src kinase. To the best of our knowledge, benzotriazine template based compounds have not been reported as kina
- Noronha, Glenn,Barrett, Kathy,Cao, Jianguo,Dneprovskaia, Elena,Fine, Richard,Gong, Xianchang,Gritzen, Colleen,Hood, John,Kang, Xinshan,Klebansky, Boris,Li,Liao,Lohse, Dan,Mak, Chi Ching,McPherson, Andrew,Palanki, Moorthy S.S.,Pathak, Ved P.,Renick, Joel,Soll, Richard,Splittgerber, Ute,Wrasidlo, Wolfgang,Zeng, Binqi,Zhao, Ningning,Zhou
-
p. 5546 - 5550
(2007/10/03)
-
- Benzotriazine inhibitors of kinases
-
The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
- -
-
Page/Page column 27, 46
(2008/06/13)
-
- A convenient synthesis of 3-amino-1,2,4-benzotriazine 1,4-dioxide (SR 4233) and related compounds via nucleophilic aromatic substitution between nitroarenes and guanidine base
-
Reaction of 1-fluoro-2-nitrobenzene or 1,2-dinitrobenzene with guanidine in hot THF followed by treatment with potassium tert-butoxide gave 3-amino-1,2,4-benzotriazine 1-oxide in good yield, which was further oxidized by peracetic acid to afford the title compound.
- Suzuki, Hitomi,Kawakami, Takehiko
-
p. 855 - 857
(2007/10/03)
-