- Immunoregulator
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The invention discloses an immune regulator, in particular to a compound for inhibiting IL - 17A and application of the compound as an immunomodulator in preparation of medicines. The invention discloses a compound shown in formula I. The application of t
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Paragraph 0119; 0139-0141
(2021/11/26)
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- Asymmetric Multicomponent Sulfa-Michael/Mannich Cascade Reaction: Synthetic Access to 1,2-Diamino-3-Organosulfur Compounds and 2-Nitro Allylic Amines
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A novel catalytic asymmetric three-component intermolecular sulfa-Michael/Mannich cascade reaction has been developed using a chiral multifunctional catalyst. This reaction provides facile access to 1-amino-2-nitro-3-organosulfur compounds bearing three c
- Hou, Wenduan,Wei, Qi,Liu, Guisheng,Chen, Jing,Guo, Jing,Peng, Yungui
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supporting information
p. 4870 - 4873
(2015/10/12)
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- Novel potent inhibitors of hepatitis C virus (HCV) NS3 protease with cyclic sulfonyl P3 cappings
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Extensive SAR studies of the P3 capping group led to the discovery of a series of potent inhibitors with sultam and cyclic sulfonyl urea moieties as the P3 capping. The bicyclic thiophene-sultam or phenyl-sultam cappings were selected for further SAR development. Modification at the P3 side chain determined that the tert-butyl group was the best choice at that position. Optimization of P1 residue significantly improved potency and selectivity. The combination of optimal moieties at all positions led to the discovery of compound 33. This compound had the best overall profile in potency and PK profile: excellent Ki* of 5.3 nM and activity in replicon (EC90) of 80 nM, extremely high selectivity of 6100, and a good rat PO AUC of 1.43 μM h.
- Chen, Kevin X.,Vibulbhan, Bancha,Yang, Weiying,Nair, Latha G.,Tong, Xiao,Cheng, Kuo-Chi,Njoroge, F. George
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body text
p. 1105 - 1109
(2009/08/07)
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- Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.
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The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM.
- Catalano, John G,Deaton, David N,Furfine, Eric S,Hassell, Annie M,McFadyen, Robert B,Miller, Aaron B,Miller, Larry R,Shewchuk, Lisa M,Willard Jr., Derril H,Wright, Lois L
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p. 275 - 278
(2007/10/03)
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- Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents
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This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.
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Page column 111
(2010/02/05)
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- A Versatile Method for the Synthesis of (S)- or (R)-Cycloalkylglycines, (S)- or (R)-N-Heterocyclic and α,β-Unsaturated N-Heterocyclic α-Amino Acids
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Two different types of cyclic α-amino acids, cycloalkylglycines and N-heterocyclic α-amino acids, were prepared in optically pure form from the same chiral synthon 1-(R) (or 1-(S)) simply by altering the quantity or type of base required for anion formation.Elaboration of the heterocyclic intermediate 3 provided α,β-unsaturated N-heterocyclic α-amino acids.
- Pauly, Regine,Sasaki, N. Andre,Potier, Pierre
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p. 237 - 240
(2007/10/02)
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- A Synthesis of Protected Aminoalkyl Epoxides from α-Amino Acids
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The synthesis of alkylamino epoxides C is presented.Key steps include the synthesis of amino aldehyde 5 by reduction (DIBAH) of ester 3 or by oxidation of N-protected amino alcohol 4, both edducts of which are derived from amino acids.A study of the olefination of aldehyde 5 with unstabilized ylides is presented, and protected allylic amino 6, obtained in good to excellent optical purity, is oxidized (MCPBA) to epoxide C.Threo selectivity is observed in the epoxidation reaction.
- Luly, Jay R.,Dellaria, Joseph F.,Plattner, Jacob J.,Soderquist, Jeffrey L.,Yi, Nwe
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p. 1487 - 1492
(2007/10/02)
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