- 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF LIVER CANCER
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The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, for (use in) the treatment and/or prophylaxis of liver cancer.
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Paragraph 0861
(2020/09/09)
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- 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF LIVER CANCER
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The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, for (use in) the treatment and/or prophylaxis of liver cancer.
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Page/Page column 87
(2019/09/18)
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- 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF VIRUS INFECTION
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The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds as TLR7 agonists for the treatment of viral infections.
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Page/Page column 39
(2018/03/25)
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- Design, synthesis, and optimization of balanced dual NK1/NK 3 receptor antagonists
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In connection with a program directed at potent and balanced dual NK 1/NK3 receptor ligands, a focused exploration of an original class of peptidomimetic derivatives was performed. The rational design and molecular hybridization of a novel phenylalanine core series was achieved to maximize the in vitro affinity and antagonism at both human NK1 and NK3 receptors. This study led to the identification of a new potent dual NK1/NK3 antagonist with pKi values of 8.6 and 8.1, respectively.
- Hanessian, Stephen,Jennequin, Thomas,Boyer, Nicolas,Babonneau, Vincent,Soma, Udaykumar,Mannoury La Cour, Clotilde,Millan, Mark J.,De Nanteuil, Guillaume
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p. 550 - 555
(2014/06/09)
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- Synthesis of o -me ulongamide b and o -me ulongamide c, natural modified cyclodepsipeptides
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Synthesis of O-Me ulongamide B and O-Me ulongamide C, modified natural cyclodepsipeptides, was achieved by a convergent route. The respective dipeptides and tridepsipeptides were coupled, obtaining linear depsipentapeptides, which were then deprotected and cyclized. These compounds were tested against three different types of human carcinoma cells and showed only moderate activity.
- Alvarado, Cuauhtémoc,Hernández, Gerardo,Díaz, Eduardo,Soano, José D.,Vilchis-Reyes, Miguel A.,Martínez-Urbina, Miguel A.,Guzmán, Angel
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p. 993 - 1006
(2013/03/13)
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- Synthesis and biological evaluation of analogues of the marine cyclic depsipeptide obyanamide
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On the basis of the total synthesis of obyanamide, 20 analogues of this marine cyclic depsipeptide have been synthesized by (i) preparation of the tripeptide fragments in the western hemisphere using Z/OtBu protocol; (ii) preparation of the dipeptide fragments in the eastern hemisphere using Boc/OMe protocol; and (iii) fragments coupling, removal of protecting groups (Boc and OtBu, in one pot), and macrocyclizaion in the last step. The cytotoxic test showed that three synthetic compounds exhibited moderate activities against HL-60, KB, LOVO, and A549 cell lines. According to the results, the β-amino acid residue was found to play a critical role in the biological activities. Additionally, the ester bond along with the Ala(Thz) moiety was also essential for biological activities. However, it seems too early to draw a conclusion that the N-methylation of Val/Phe can lead to higher or lower cytotoxic activities.
- Zhang, Wei,Ding, Ning,Li, Yingxia
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experimental part
p. 533 - 539
(2012/05/04)
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- Total synthesis and reassignment of stereochemistry of obyanamide
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The total synthesis of a marine cytotoxic cyclic depsipeptide obyanamide is reported. The synthesis has led to a reassignment of the C-3 configuration in β-amino acid residue. And this revision is also supported by biological test.
- Zhang, Wei,Ma, Zhen-Hua,Mei, Duo,Li, Chun-Xia,Zhang, Xiu-Li,Li, Ying-Xia
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p. 9966 - 9972
(2007/10/03)
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- The total synthesis and reassignment of stereochemistry of dragonamide
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The first total synthesis of dragonamide is reported. The synthesis has led to a reassignment of the configuration at the stereogenic centre on the alkyne-bearing fragment of the molecule.
- Chen, Hongliang,Feng, Yaqing,Xu, Zhengshuang,Ye, Tao
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p. 11132 - 11140
(2007/10/03)
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- The total synthesis and stereochemical revision of yanucamide A
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(Matrix presented) The first total synthesis of yanucamide A is reported via amide and ester couplings of the key components. This synthesis has established the configuration at the previously ambiguous 3-position, and also revised the stereochemistry at the 22-position, to give 3S,12S,17S,22S for the natural product.
- Xu, Zhengshuang,Peng, Yungui,Ye, Tao
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p. 2821 - 2824
(2007/10/03)
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- New kelatorphan-related inhibitors of enkephalin metabolism: Improved antinociceptive properties
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In order to improve the in vivo protection of enkephalins from enzymatic degradation, a new series of inhibitors derived from kelatorphan [HONHCOCH2CH(CH2Ph)CONHCH(CH3)COOH], the first-described complete inhibitor of enkephalin metabolism, were designed by modification of the C-terminal amino acid. The progressive lengthening of the chain of this residue shows that a β-alanine seems to be the best basic model for the conception of such types of compounds. On the other hand, the methylation of the amide bond, which is well accepted by aminopeptidase N (EC 3.4.11.2) and dipeptidylaminopeptidase, induced a significant loss of affinity for neutral endopeptidase -24.11. Starting from these data, compounds containing a variously substituted β-alanine residue and corresponding to the general formula HONHCOCH2CH(CH2Ph)CONHCH(R1)CH(R2)COOH were synthesized. All these molecules inhibit neutral endopeptidase -24.11 and dipeptidylaminopeptidase in the nanomolar range, and those containing an aromatic chain (compound 7A, R1 = CH2Ph,R2 = H, and compound 8A, R1 = Ph, R2 = H) inhibit the biologically relevant aminopeptidase N, with IC50's around 10-8 M. Intracerebroventricular injection in mice of these multienzyme inhibitors produced an efficient and naloxone-reversible analgesic response (hot plate test): compounds 7A and 8A were shown to be more potent than kelatorpohan in increasing the jump latency time, in agreement with their in vitro properties, and these new compounds were found to increase the forepaw lick latency, a reflex considered as a typical morphine response.
- Xie,Soleilhac,Schmidt,Peyroux,Roques,Fournie-Zaluski
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p. 1497 - 1503
(2007/10/02)
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