- Investigation of biaryl heterocycles as inhibitors of Wee1 kinase
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In continuation of our previous research towards the discovery of potent, selective and drug-like Wee1 inhibitors, 2 novel series of biaryl heterocycles were designed, synthesized and evaluated. The new biaryl cores were designed to enable structure?activ
- Mastracchio, Anthony,Lai, Chunqiu,Torrent, Maricel,Bromberg, Kenneth,Buchanan, Fritz G.,Ferguson, Debra,Bontcheva, Velitchka,Johnson, Eric F.,Lasko, Loren,Maag, David,Soni, Nirupama,Shoemaker, Alexander R.,Penning, Thomas D.
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supporting information
p. 1481 - 1486
(2019/04/25)
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- TAM KINASE INHIBITORS
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Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat diseases, such as cancer.
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Paragraph 0160
(2019/02/02)
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- PYRIDOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Compounds of the formula (I) in which R, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and / or systemic lupus
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Page/Page column 73; 74; 75
(2014/03/21)
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- Efficient aerobic oxidative dehydrogenation of dihydropyrimidinones and dihydropyrimidines
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4-Substituted dihydropyrimidinones and dihydropyrimidines were first efficient aerobic oxidized to the corresponding pyrimidinones and pyrimidines, respectively, in high yields by molecular oxygen in the presence of catalytic amount of N-hydroxyphthalimid
- Han, Bing,Han, Run-Feng,Ren, Yu-Wei,Duan, Xiao-Yong,Xu, Yi-Chuan,Zhang, Wei
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supporting information; experimental part
p. 5615 - 5620
(2011/08/09)
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- BENZAZEPINE DERIVATIVES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS
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A compound having the formula (1) wherein: Ra represents C1-6 alkyl, cyclobutyl or cyclopentyl; R1 represents H or C1-6 alkyl; R2 represents H or R1 and R2 together represent =0; X1 represents CR3 or N; X2 represents CR4 or N; X3 represents CR5 or N; X4 represents CR6 or N; wherein one or two of X1, X2, X3 and X4 represents N; R3, R4, R5 and R6 each independently represent H, C1-6 alkoxy or -NR7R8; R7 and R8 independently represent H or C1-6 alkyl; or R7 and R8 and the N atom to which they are attached are joined to form a N-containing heterocyclyl ring optionally substituted with one or more substituents independently selected from halogen, C1-6 alkyl and C1-6 alkoxy; or a pharmaceutically acceptable salt thereof, is provided. Compounds of the invention have been found to modulate the histamine H3 receptor.
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Page/Page column 53
(2011/08/03)
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- Mild and efficient oxidative aromatization of 4-substituted-1,4- dihydropyrimidines using (diacetoxyiodo)benzene
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(Chemical Equation Presented) 4-Alkyl or aryl-1,4-dihydropyrimidines were readily oxidized by (diacetoxyiodo)benzene under mild reaction conditions to the corresponding pyrimidine derivatives in good to excellent yields.
- Karade, Nandkishor N.,Gampawar V, Sumit,Tale, Nilesh P.,Kedar, Sanjay B.
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experimental part
p. 740 - 744
(2010/08/22)
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- 2, 5-DIAMINO-SUBSTITUTED PYRIDO [4, 3-D] PYRIMIDINES AS AUTOTAXIN INHIBITORS AGAINST CANCER
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The present invention relates to pyridopyrimidine derivatives according to formula (I), as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
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Page/Page column 88-89
(2010/06/20)
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- DIFLUOROALKENE DERIVATIVE, PEST CONTROL AGENT CONTAINING THE SAME, AND INTERMEDIATE THEREFOR
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A difluoroalkene derivative which is sufficiently effective in controlling various pests even when used in a small dose and is highly safe for crops, natural enemies to the pests, and animals; and an intermediate for the derivative. The difluoroalkene derivative is represented by the general formula: [I] wherein L1 and L2 are the same or different and each represents oxygen or sulfur; n is an integer of 2 to 8; and Q represents a 5- to 12-membered heterocyclic group having any desired heteroatom selected among nitrogen, oxygen, and sulfur.
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- Synthesis, antiviral (HSV-1) and antimycotic activities of ethyl or methyl 2,4-disubstituted 5-pyrimidinecarboxylates, 2,4-disubstituted 5-pyrimidinecarboxylic acids and 2,4-disubstituted pyrimidines
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The synthesis of ethyl or methyl 4-substituted or unsubstituted 2-methylthio-5-pyrimidinecarboxylates 3 a-i and 8 o mainly by reaction of ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates with 2-methylisothiourea is described. Also some ethyl 2-sub
- Sansebastiano,Mosti,Menozzi,Schenone,Muratore,Petta,Debbia,Pesce Schito,Schito
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p. 335 - 355
(2007/10/02)
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