专利号:US-7935704-B2 优先权日:2003-08-01 标 题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 发明人:PALLADINO MICHAEL A; LLOYD GEORGE KENNETH; HAYASHI YOSHIO; NICHOLSON BENJAMIN 权利人:NEREUS PHARMACEUTICALS INC 摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ″, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.
专利号:US-7956058-B2 优先权日:2002-08-02 标 题:Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 发明人:HAYASHI YOSHIO; PALLADINO JR MICHAEL A; GRODBERG JENNIFER 权利人:NEREUS PHARMACEUTICALS INC 摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ′, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.
专利号:EP-2054420-B1 优先权日:2006-08-02 标题:Benzimidazo[1,2-c][1,2,3]thiadiazol-7-sulfonamides as inhibitors of carbonic anhydrase and the intermediates for production thereof 发明人:MATULIS DAUMANTAS; DUDUTIENE VIRGINIJA; MATULIENE JURGITA; MISTINAITE LINA 权利人:BIOTECHNOLOGIJOS INST 摘要:The invention is related to novel compounds - benzimidazo[1,2-c][1,2,3]thiadiazole sulfonamides, corresponding to the general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression such as glaucome. The compounds of formula (I) inhibits enzymes such as carbonic anhydrases and metallo proteinases. This invention is also related to new intermediate compounds which are used for the synthesis of sulfonamides of formula (I).
专利号:US-2023266302-A1 优先权日:2020-07-24 标 题:Synthesis and use of n-benzyl sulfonamides 发明人:LAMAR ANGUS A; SHEAFF ROBERT J 权利人:THE UNIV OF TULSA 摘要:Disclosed is a method for preparing N-benzyl sulfonamides. Also disclosed is a composition for treating cancer. The composition includes a N-benzyl sulfonamide and a metabolic inhibitor. Also disclosed is a method for determining the impact on cell ATP levels of a composition containing a N-benzyl sulfonamide with or without a metabolic inhibitor.
专利号:US-9290529-B2 优先权日:2011-10-24 标题:Carbonic anhydrase inhibitors and method of their production 发明人:BRYNDA JIRI; CIGLER PETR; GRUNER BOHUMIR; MALOY REZACOVA PAVLINA; MADER PAVEL; SICHA VACLAV; BAKARDJIEV MARIO; HOLUB JOSEF; DZUBAK PETR; HAJDUCH MARIAN 权利人:USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CESKE REPUBLIKY V V I; USTAV MOLEKULARNI GENETIKY AKADEMIE VED CESKE REPUBLIKY V V I; USTAV ANORGANICKE CHEMIE AKADEMIE VED CESKE REPUBLIKY V V I; UNIV PALACKEHO 摘要:Derivatives of boron cluster compounds of general formula I and their pharmaceutically acceptable salts and solvates, and their specific inhibition effect on the enzyme carbonic anhydrase IX, a protein overexpressed in cancer tissues. Methods of synthesis and the use of the novel derivatives. These inhibitors of human carbonic anhydrase IX can be used as active compounds of pharmaceuticals for diagnostics and/or therapy of cancer diseases.
专利号:US-7674903-B2 优先权日:2002-08-02 标题:Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
1: Pogacar Z, Johnson JL, Krenning L, De Conti G, Jochems F, Lieftink C, Velds A, Wardak L, Groot K, Schepers A, Wang L, Song JY, van de Ven M, van Tellingen O, Medema RH, Beijersbergen RL, Bernards R, Leite de Oliveira R. Indisulam synergizes with palbociclib to induce senescence through inhibition of CDK2 kinase activity. PLoS One. 2022 Sep 6;17(9):e0273182. doi: 10.1371/journal.pone.0273182. 2: Hopkins MD, Witt RC, Flusche AME, Philo JE, Ozmer GL, Purser GH, Sheaff RJ, Lamar AA. Synthesis and biological evaluation of N-alkyl sulfonamides derived from polycyclic hydrocarbon scaffolds using a nitrogen-centered radical approach. Org Biomol Chem. 2022 Aug 24;20(33):6680-6693. doi: 10.1039/d2ob01291j. 127:106017. doi: 10.1016/j.bioorg.2022.106017. Epub 2022 Jul 9. 5(9):e202101348. doi: 10.26508/lsa.202101348.
合成参考文献
参考文献:10.1021/jm901855h 摘要:Joseph P, Turtaut F, Ouahrani-Bettache S, Montero JL, Nishimori I, Minakuchi T, Vullo D, Scozzafava A, Köhler S, Winum JY, Supuran CT. Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis. J Med Chem. 2010 Mar 11;53(5):2277–85. doi: 10.1021/jm901855h. 参考文献:10.1016/j.bmc.2011.06.038 摘要:Nishimori I, Minakuchi T, Vullo D, Scozzafava A, Supuran CT. Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. Bioorg Med Chem. 2011 Aug 15;19(16):5023–30. doi: 10.1016/j.bmc.2011.06.038.