- Lactam analogues of galiellalactone
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A synthetic route to lactam analogues of the fungal STAT3 inhibitor galiellalactone is presented. The synthesis involves a one-pot tosylamide amide coupling/intramolecular Michael addition and an introduction of an α,β-unsaturation, regioselectively directed by the tosyl functionality. An iodolactonization of the octahydroindolizine 9 and a re-opening of the lactone were employed for introducing an iodo substituent, facilitating the preparation of 8-substituted analogues (e.g., 4) using a Suzuki cross-coupling.
- Nilsson, Jakob,Gidl?f, Ritha,Johansson, Martin,Sterner, Olov
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- Conjugate of cytotoxin molecule and cell binding receptor molecule
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A conjugate of a strong cytotoxin molecule and a cell binding receptor molecule has a structure shown in a molecular formula (I), wherein T, L, m, n, -----, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are defined in the text. The conjugate is used for treating cancer, immunological diseases and infectious diseases.
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Paragraph 0032; 0302-0304
(2019/10/10)
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- CONJUGATE OF CELL-BINDING RECEPTOR WITH CYTOTOXIC AGENT
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PROBLEM TO BE SOLVED: To provide a conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule for targeted treatment. SOLUTION: According to the present invention, there is provided a conjugate having a structure of formula (I) and a pharmaceutical acceptable salt and a solvate thereof. The conjugate is used for treating cancer, autoimmune disease, and infectious disease. (T is a targeting or binding ligand; L is a releasable linker; a broken line is a linkage bond that L connects to a molecule inside the bracket independently; n is an integer of 1 to 20; m is an integer of 1 to 10; and a structure in parentheses is a potent antimitotic agent/drug.) SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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Paragraph 0223; 0224
(2017/10/31)
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- CONJUGATES OF CELL BINDING MOLECULES WITH CYTOTOXIC AGENTS
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A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a formula (I), wherein T, L, m, n, Y, R1, R2, R3, R4, R5, R6, R7, R8, Rsu
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Paragraph 0204; 0205
(2017/07/15)
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- Conjugates of Cell Binding Molecules with Cytotoxic Agents
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A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a Formula (I), wherein T, L, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9
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Paragraph 0198; 0199
(2017/11/06)
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- Synthesis of 4-maleimidobutyric acid and related maleimides
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Maleimidoalkanoic acids and their activated derivatives, such as their N-hydroxysuccinimide esters, are important, though expensive, linkers for the conjugation of biomolecules. During our synthesis of UCS1025A, we have developed a chromatography-free preparation of 4-maleimidobutyric acid on a one-mole scale. Georg Thieme Verlag Stuttgart.
- De Figueiredo, Renata Marcia,Oczipka, Philipp,Froehlich, Roland,Christmann, Mathias
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p. 1316 - 1318
(2008/12/22)
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- Design and synthesis of a novel DNA-encoded chemical library using Diels-Alder cycloadditions
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DNA-encoded chemical libraries are increasingly being employed for the identification of binding molecules to protein targets of pharmaceutical relevance. Here, we describe the synthesis and characterization of a DNA-encoded chemical library, consisting of 4000 compounds generated by Diels-Alder cycloaddition reactions. The compounds were encoded with unique DNA fragments which were generated through a stepwise assembly process and serve as amplifiable bar codes for the identification and relative quantification of library members.
- Buller, Fabian,Mannocci, Luca,Zhang, Yixin,Dumelin, Christoph E.,Scheuermann, Joerg,Neri, Dario
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supporting information; experimental part
p. 5926 - 5931
(2009/05/31)
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