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    Macrocyclic lactams
    1.
    发明授权
    Macrocyclic lactams 失效
    大环内酰胺

    公开(公告)号：US07112581B2

    公开(公告)日：2006-09-26

    申请号：US10673036

    申请日：2003-09-25

    Applicant: Scott C. Mitchell ,  Benjamin Nicholson

    Inventor： Scott C. Mitchell ,  Benjamin Nicholson

    IPC: A61K31/395 ,  A61K35/02 ,  A61P35/00 ,  C07D225/02

    CPC classification number: C07D225/02

    Abstract: Compounds represented by the following structure (I), acid-addition salts and pro-drugs are disclosed: wherein the ring structure includes no substitutions, one substitution, or more than one substitution; and wherein n is equal to an integer grater than 1, preferably 2, 3, or 4; m is equal to a positive integer, preferably 1, 2 or 3, and each separate Xn and X are each separately selected from a nucleophilic residue, preferably —H, —OH, —O—CO-alkyl, —O-alkyl, —NH2, a halogen and the like; and wherein the dashed line represents a C—C bond or a C—H bond, and the dashed and solid line represents either a carbon-carbon single bond or a carbon-carbon double bond.

    Abstract translation: 公开了由以下结构（I）表示的化合物，酸加成盐和前药：其中环结构不包括取代，一个取代或多于一个取代; 并且其中n等于1，优选2,3或4的整数倍; m等于正整数，优选1,2或3，并且每个单独的X n和X各自独立地选自亲核残基，优选-H，-OH，-O-CO- 烷基，-O-烷基，-NH 2，卤素等; 并且其中虚线表示C-C键或C-H键，虚线和实线表示碳 - 碳单键或碳 - 碳双键。

    Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
    3.
    发明授权
    Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 有权
    脱氢苯基乙二烯和其类似物，以及脱氢苯基黑曲霉素及其类似物的合成

    公开(公告)号：US07935704B2

    公开(公告)日：2011-05-03

    申请号：US11051268

    申请日：2005-02-04

    Applicant: Michael A. Palladino ,  George Kenneth Lloyd ,  Yoshio Hayashi ,  Benjamin Nicholson

    Inventor： Michael A. Palladino ,  George Kenneth Lloyd ,  Yoshio Hayashi ,  Benjamin Nicholson

    IPC: A61K31/497

    CPC classification number: A61K31/496

    Abstract: Compounds represented by the following structure (I) are disclosed: as 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 R1, R1′, R1″, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.

    Abstract translation: 公开了由以下结构（I）表示的化合物：制备这种化合物的方法，其中所述方法包括使二酰基二酮哌嗪与第一醛反应以产生中间体化合物; 并使所述中间体化合物与第二醛反应以产生一类具有通式结构的化合物，其中第一种醛和第二种醛选自恶唑烷羧醛，咪唑甲醛，苯甲醛，咪唑甲醛衍生物和苯甲醛衍生物， 从而形成上述化合物，其中R1，R1'，R1“，R2，R3，R4，R5和R6，X1和X2，Y，Z，Z1，Z2，Z3和Z4各自可以以一致的方式分别定义 附带说明。 还公开了治疗血管增生的组合物和方法。

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