- Sultam compound and preparation method thereof
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The invention provides a sultam compound and a preparation method thereof. The method provided by the invention specifically comprises the following steps: putting a catalyst C, sulfamide B and an oxidant D into an organic solvent, performing a reaction,
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Paragraph 0125-0127; 0135-0138; 0151-0154
(2019/11/12)
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- Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents
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A series of novel carbazole-containing sulfonamides and sulfamides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the results of efficacy studies in diet-induced obese (DIO) mice, and the desired pharmacokinetic parameters, compound 41 was selected for further profiling.
- Humphries, Paul S.,Bersot, Ross,Kincaid, John,Mabery, Eric,McCluskie, Kerryn,Park, Timothy,Renner, Travis,Riegler, Erin,Steinfeld, Tod,Turtle, Eric D.,Wei, Zhi-Liang,Willis, Erik
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p. 757 - 760
(2016/05/24)
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- Identification of a novel RAMP-independent CGRP receptor antagonist
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Identification of an HIV integrase inhibitor with micromolar affinity for the CGRP receptor led to the discovery of a series of structurally novel CGRP receptor antagonists. Optimization of this series produced compound 16, a low-molecular weight CGRP rec
- Zartman, C. Blair,Bell, Ian M.,Gallicchio, Steven N.,Graham, Samuel L.,Kane, Stefanie A.,Mallee, John J.,Rutledge, Ruth Z.,Salvatore, Christopher A.,Vacca, Joseph P.,Williams, Theresa M.
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scheme or table
p. 6705 - 6708
(2011/12/21)
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- 3-(1,1-DIOXOTETRAHYDRO-1,2-THIAZIN-2-YL) or 3-(1,1-DOXO-ISOTHIAZOLIDIN-2YL) SUBSTITUTED BENZAMIDE COMPOUNDS AS ASP2 INHIBITORS
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The present invention relates to hydroxyethylene compounds of formula (I); having A sp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease wherein R1 represents a group of formula Zc.
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Page/Page column 15
(2010/02/09)
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- Indole nitriles
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Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5and R6are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
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- Indole nitriles
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Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
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- Practical Synthesis of Sultams via Sulfonamide Dianion Alkylation: Application to the Synthesis of Chiral Sultams
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(Equation presented) A practical synthesis of sultams was developed via intramolecular sulfonamide dianion alkylation. This method has been applied toward the synthesis of chiral sultams, which are synthetically valuable as chiral auxiliaries.
- Lee, Jaemoon,Zhong, Yong-Li,Reamer, Robert A.,Askin, David
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p. 4175 - 4177
(2007/10/03)
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- N-Nitroso Sultams: On the Direction of Approach of Nucleophiles to the Sulfonyl Group
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The N-nitroso derivatives of propanesultam, butanesultam, and pentanesultam were synthesized along with N-nitropropanesultam and N-nitro-N-methylmethanesulfonamide.The decompositions of the N-nitroso sultams, wich increase in rate with increasing ring size, yield the corresponding sultones and also varying amounts of regenerated sultams.These reactions are discussed in terms of higher energy pathway involving approach of the nucleophile in a direction between of sulfonyl oxygens (on the O, O, N face) and a lower energy pathway involving the conformer which permits approach of the nucleophile trans to and colinear with one of the coordinate covalent oxygen atoms (on R, O, N face). The mechanisms of the decomposition of the N-nitro sulfonamides and the tosyloxy diimide N-oxides are also discussed.N-nitrosopropanesultam (and the butyl analoque) are potent inhibitors of proteinase α-chymotrypsin.
- White, Emil H.,Lim, Hyung M.
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p. 2162 - 2166
(2007/10/02)
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- A General Mechanism for the Oxidative Cleavage of Amine Disulfides and Cystine in Aqueous Iodine. Isolation of Cyclic Sulfinamides
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When disulfides are cleaved by aqueous iodine, neighboring group participation facilitates the rate of reaction and the formation of cyclized products.The series of bis-disulfides 2 was prepared, X = N(CH3)2, 1, NH2, 2, N(CH3)3+, 3, as well as 2, 4.The tertiary amine, 1, is oxidized by aqueous I2 at a rate which is accelerated by as much as 106 over the rate of reaction of the quaternary ammonium iodide salt 3.The oxidation products of 1 are the sulfinic and sulfonic acids while 3 yields the sulfonic acid.Aqueous iodine reacts with the primary amines 2 and 4 at moderately accelerated rates to give the cyclic sulfinamides, isothiazolidine 1-oxide from 2 and tetrahydro-1,2-thiazine 1-oxide from 4.This oxidative cyclization reaction is the most direct route to these cyclic sulfinamides.At a given pH, the rate law for the oxidation of 1 and 2 is -d/dt = -k.At high pH, compound 4 has the same rate law.The kinetic data for 4 at low pH and for 3 resemble those reported in a classical study of the aqueous iodine oxidative cleavage of cystine.The kinetics and mechanisms of these reactions will be discussed.
- Doi, Joyce Takahashi,Musker, W. Kenneth
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