摘要:
The invention provides compounds which directly inhibit IRE-1α activity in vitro , prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要:
A substrate for solid phase synthesis comprising a solid phase-linker combination of formula (I) is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediate useful therein. Among the novel intermediates are compounds of formula (II) wherein R is -NO2 or -CHO; R is -OCH3, -CHO or -H; R is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n = 1 or 3-12. A substrate of solid phase synthesis of formula (III) is also disclosed.
摘要翻译:公开了用于固相合成的底物,其包含式(I)的固相 - 连接体组合。 还公开了制备其中有用的基材和化学中间体的方法。 其中新的中间体是式(II)的化合物,其中R 1是-NO 2或-CHO; R 2是-OCH 3,-CHO或-H; R 3选自羟基,具有多个氨基的固体支持物的残基和酯的残基,n = 1或3-12。 还公开了式(III)的固相合成的底物。
摘要:
The present invention relates to a compound of formula (I) R to R are hydrogen or methyl, where two R to R on adjacent carbon atoms together with a C-C single bond may stand for a C-C double bond, provided that, in the carbon chain substituted by R to R , only one of the substituents R to R is methyl and only an adjacent pair of said substituents contribute to a C-C double bond, a process for its production and its use as a medicament, especially for treating diseases produced by an HIV infection.
摘要:
本发明提供ATG类似物及其制备方法和应用,ATG类似物的具体结构如下列三个通式所示: 式(I),式(II),式(III) 其中,X/Y/Z可以分别选自C、N、S、O, R 1, R 2, R 3, R 4, R 5 各自分别选自: H,CH 3 基团,脂肪族或者芳香族碳氢化合物基团,硝基,磷酸基,硫化物基团,砜类基团,腈类基团,杂环基,硼酸酯或硼酸基团,酯类基团,胺类基团。本发明所提供的ATG类似物具有更好的水溶性和防止在一级代谢中被分解的效果。
摘要:
Provided herein are compounds and processes to prepare intermediates and precursors of pregabalin and related compositions, and processes for the preparation of pregabalin.
摘要:
Compounds according to general formulae (Ia to Ie) wherein: X = O or S; Y is O, S or CH2, CHR, CRR, where R is C1-7 alkyl; Z is O or S; R1 is H or C1-7 alkyl; R2 is H or C1-7 alkyl; R4 is H or C1-7 alkyl at any vacant position on the aromatic ring; R3 is C1-7 alkyl-L1-R5-L2- R6-COOH, C3-10 cycloalkyl-L1-R5-L2- R6-COOH or Ar-C0-7 alkyl-L1-R5-L2- R6-COOH; each of L1 and L2 is absent or a suitable linker such as an amide CONH; or an ether -O-, or a thioether -S- or a sulphone -S02-; R5 is C1-7 alkyl, C3-1O cycloalkyl or Ar-C0-7 alkyl each of which is substituted with either NR8R9, where the nitrogen atom is capable of being protonated in solution to give N HR8R9; or a quaternary nitrogen atom N R8R9R10, such that R5 contains a positive charge; each of R8, R9 and R10 is independently C1-7 alkyl, C3-10 cycloalkyl or Ar-C0-7 alkyl, or any two or more of R8, R9 and R10 together form an alicyclic or arylalicyclic ring system; R6 is C1-7 alkyl, C3-10 cycloalkyl or Ar-C0-7 alkyl; and their salts, hydrates, solvates, complexes or prodrugs are of use as linkers for conjugating an epitope to a carrier protein.
摘要翻译:根据通式(Ia至Ie)的化合物,其中:X = O或S; Y是O,S或CH 2,CHR,CRR,其中R是C 1-7烷基; Z是O或S; R1是H或C1-7烷基; R2是H或C1-7烷基; R4是芳环上任何空位的H或C 1-7烷基; R3是C1-7烷基-L1-R5-L2-R6-COOH,C3-10环烷基-L1-R5-L2-R6-COOH或Ar-C10-烷基-L1-R5-L2-R6-COOH; L1和L2各自不存在,或者合适的接头如酰胺CONH; 或醚-O-,或硫醚-S-或砜-S02-; R5是C1-7烷基,C3-1O环烷基或任选被NR8R9取代的Ar-C0-7烷基,其中氮原子能够在溶液中被质子化,得到N + HR8R9; 或季氮原子N + R 8 R 9 R 10,使得R 5含有正电荷; R 8,R 9和R 10各自独立地为C 1-7烷基,C 3-10环烷基或Ar-C 0-7烷基,或R 8,R 9和R 10中的任何两个或更多个一起形成脂环族或芳基脂环族环系; R 6是C 1-7烷基,C 3-10环烷基或Ar-C 0-7烷基; 并且它们的盐,水合物,溶剂合物,复合物或前药可用作将表位与载体蛋白缀合的接头。
摘要:
A method for the solid phase synthesis of compounds of formula (1), in which either or both of R1 or R2 are combinatorially variable by a process represented by scheme (4) and wherein: X is (a), (b), (c) or (d); Y is H or a side chain functional group protective moiety such as Fmoc; R21 is an intermediate form of R2 which is subsequently chemically transformed to give the desired R2; and n is between 2 and 12, preferably 4. The invention also provides compounds and combinatorial libraries of compounds of formula (1), as well as intermediate compounds for use in the method.
摘要:
The invention provides compounds which directly inhibit IRE-1a activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要:
Provided herein are compounds and processes to prepare intermediates and precursors of pregabalin and related compositions, and processes for the preparation of pregabalin.