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    ANTIOXIDANTS
    2.
    发明申请
    ANTIOXIDANTS 审中-公开
    抗氧化剂

    公开(公告)号：WO01064661A1

    公开(公告)日：2001-09-07

    申请号：PCT/JP2001/001347

    申请日：2001-02-23

    IPC: A61K31/395 ,  A61K31/554 ,  A61P3/10 ,  A61P9/10 ,  A61P11/00 ,  A61P25/00 ,  A61P25/16 ,  A61P27/12 ,  A61P39/06 ,  A61P43/00 ,  C07D285/36 ,  C07D285/38 ,  C07D285/00

    CPC classification number: C07D285/38 ,  A61K31/395 ,  A61K31/554 ,  C07D285/36

    Abstract: The invention provides excellent antioxidants. Compounds of the general formula (1) or pharmacologically acceptable salts thereof are excellent in antioxidant activity and therefore useful as remedies for cataract and ischemic heart diseases due to oxidative stress, wherein R1, R2 and R3 are each independently hydrogen or lower alkyl; R4 is a carboxylic acid group or an ester or amide thereof; m is 0 or 1; and n is 1 or 2.

    Abstract translation: 本发明提供优异的抗氧化剂。 通式（1）的化合物或其药理学上可接受的盐具有优异的抗氧化活性，因此可用作由于氧化应激引起的白内障和缺血性心脏病的治疗，其中R1，R2和R3各自独立地为氢或低级烷基; R4是羧酸基团或其酯或酰胺; m为0或1; n为1或2。

    HETEROCYCLIC COMPOUNDS, COMBINATORIAL LIBRARIES THEREOF AND METHODS OF SELECTING DRUG LEADS
    4.
    发明申请
    HETEROCYCLIC COMPOUNDS, COMBINATORIAL LIBRARIES THEREOF AND METHODS OF SELECTING DRUG LEADS 审中-公开
    杂环化合物及其组合文库及选择药物引导方法

    公开(公告)号：WO2003059876A2

    公开(公告)日：2003-07-24

    申请号：PCT/IL2003/000008

    申请日：2003-01-02

    Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM ,  GILON, Chaim

    Inventor： GILON, Chaim

    IPC: C07D

    CPC classification number: C07D285/00 ,  C07D285/38 ,  C07K1/047 ,  C40B40/00

    Abstract: The present invention provides new heterocyclic compounds that have a relatively flexible backbone. These compounds may be used to produce new combinatorial libraries that will permit screening for lead compounds and selection of drug candidates for a variety of uses in human medicine, veterinary medicine and in agriculture. The members of libraries provided by the invention differ from each other (in addition to the conventional chemical and positional diversity attained by the different substituents on the ring) in two novel aspects : (a) the ring size; and (b) the chirality of the substituents on the ring. This leads to conformational diversity and flexibility that allows the selection of the most active compound, not only on the basis of the nature and proper arrangement of the substituents attained by the known chemical and positional diversity, but also based on the ability to undergo conformational complementarity attained by the conformational diversity. The present invention further provides combinatorial libraries comprising a plurality of the heterocyclic compounds of the present invention, and methods of screening the combinatorial libraries for compounds having a beneficial biological effect. The screening methods provided herein may be automated and/or computerized, for example by using a computer program to virtually screen the combinatorial libraries in order to identify compounds that are predicted to adopt bioactive conformations that will give rise to the desired biological effect.

    Abstract translation: 本发明提供了具有相对柔性主链的新杂环化合物。 这些化合物可用于生产新的组合文库，其将允许筛选铅化合物和选择用于人类医学，兽医学和农业中各种用途的候选药物。 本发明提供的文库的成员在两个新颖的方面彼此不同（除了通过环上不同取代基获得的常规化学和位置多样性）（a）环尺寸; 和（b）环上的取代基的手性。 这导致构象多样性和灵活性，其允许选择最活跃的化合物，不仅基于通过已知化学和位置多样性获得的取代基的性质和适当排列，而且还基于经历构象互补性的能力 由构象多样性所达到。 本发明还提供了包含多个本发明的杂环化合物的组合文库，以及筛选具有有益生物学作用的化合物的组合文库的方法。 本文提供的筛选方法可以是自动化和/或计算机化的，例如通过使用计算机程序来虚拟筛选组合文库，以便鉴定预测采用将产生所需生物效应的生物活性构象的化合物。

    NEOVASCULARIZATION INHIBITORS
    6.
    发明申请
    NEOVASCULARIZATION INHIBITORS 审中-公开
    新生血管抑制剂

    公开(公告)号：WO99034795A1

    公开(公告)日：1999-07-15

    申请号：PCT/JP1999/000018

    申请日：1999-01-07

    IPC: C07D285/38 ,  A61K31/395 ,  A61K31/55

    CPC classification number: C07D285/38

    Abstract: Cyclic disulfide derivatives represented by general formula (I), wherein R , R and R represent each H or alkyl; m is 0 or 1, and n is 1 or 2. Because of having effects of inhibiting neovascularization, regulating vascular permeability and preventing vascular endothelial growth factor from releasing, these compounds are expected as being useful as remedies for diseases in which neovascularization, vascular permeability or vascular endothelial growth factor participates, in particular, retinal diseases such as diabetic retinopathy, macular degeneration, retinal venous obliteration and retinal arterial obliteration, neovascularization glaucoma and tumors such as anginoma.

    Abstract translation: 由通式（I）表示的环状二硫化物衍生物，其中R 1，R 2和R 3各自表示H或烷基; m为0或1，n为1或2.由于具有抑制新血管形成，调节血管通透性和预防血管内皮生长因子释放的作用，预期这些化合物可用作新血管形成，血管通透性 或血管内皮生长因子参与，特别是视网膜疾病如糖尿病视网膜病变，黄斑变性，视网膜静脉闭塞和视网膜动脉闭塞，新生血管性青光眼和诸如血管瘤的肿瘤。

    PEPTIDYL DERIVATIVES AS METALLOPROTEINASE INHIBITORS
    8.
    发明申请
    PEPTIDYL DERIVATIVES AS METALLOPROTEINASE INHIBITORS 审中-公开
    肽衍生物作为金属蛋白酶抑制剂

    公开(公告)号：WO1994025434A1

    公开(公告)日：1994-11-10

    申请号：PCT/GB1994000895

    申请日：1994-04-27

    Applicant: CELLTECH LIMITED ,  MORPHY, Richard, John ,  MILLICAN, Andrew, Thomas

    Inventor： CELLTECH LIMITED

    IPC: C07C323/60

    CPC classification number: C07D285/38 ,  A61K41/00 ,  C07C317/50 ,  C07C323/60 ,  C07C323/61 ,  C07C2601/02

    Abstract: Compounds of formula (1) are described where R represents a -CONHOR [where R is a hydrogen atom or an acyl group], carboxyl (-CO2H), esterified carboxyl, -SR or -P(O)(X R )- -X R group, where X and X , which may be the same or different, is each an oxygen or sulphur atom and R and R , which may be the same or different each represents a hydrogen atom or an optionally substituted alkyl, aryl, or aralkyl group; R represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group, R represents a group -Z (CH2)mZ -Ar wherein Ar is an aryl or heteroaryl group, Z and Z , which may be the same or different, is each a bond or a heteroatom, and m is zero or an integer 1 to 6 with the proviso that when m is zero, Z is a bond, and Z is a heteroatom; R represents a hydrogen atom or an alkyl group; R represents a hydrogen atom or an alkyl group; R represents a group -C(R )(R )Het-R , wherein R and R which may be the same or different is each an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R )- groups (where R is a hydrogen atom or an optionally substituted alkyl group), or an optionally substituted cycloalkyl, cycloalkenyl, aryl or heteroaryl group, or R and R together with the carbon atom to which they are attached are linked together to form an optionally substituted cycloalkyl or cycloalkenyl group, Het is -O-, -S(O)p- [where p is zero, or an integer 1 or 2] or -N(R )-, and R is a hydrogen atom or an aliphatic, cycloaliphatic, heterocycloaliphatic, aromatic, or heteroaromatic group; X is an amino (-NH2), substituted amino, hydroxyl or substituted hydroxyl group, or is linked to the atom of group Het in R to form a chain -X-Alk-R - where X is -N(R )-, Alk is an optionally substituted alkylene chain and R is -Het-C(R )(R )-; and the salts, solvates, hydrates and prodrugs thereof. The compounds are orally active metalloproteinase inhibitors and in particular have a selective gelatinase action, have a long duration of action, and may be of use in the prophylaxis or treatment of diseases or disorders in which stromelysis, collagenase or gelatinase have a role, for example in the treatment of cancer to control the development of tumor metastases.

    Abstract translation: 其中R表示-CONHOR 6 [其中R 6为氢原子或酰基]，羧基（-CO 2 H），酯化羧基，-SR 6或-P （O）（X 1 R 7）-X 2 R 8基团，其中X 1和X 2可以相同或不同，各自为氧或硫 原子和R 7和R 8可以相同或不同，各自表示氢原子或任选取代的烷基，芳基或芳烷基; R 1表示氢原子或任选取代的烷基，烯基，芳基，芳烷基，杂芳烷基或杂芳硫基烷基，R 2表示基团-Z 2（CH 2）mZ 1 -Ar，其中Ar为 芳基或杂芳基，Z 1和Z 2可以相同或不同，各自为键或杂原子，m为0或1至6的整数，条件是当m为0时， Z 2是一个键，Z 1是杂原子; R 3表示氢原子或烷基; R 4表示氢原子或烷基; R 5表示基团-C（R 9）（R 10）Het-R 11，其中R 9和R 10可以相同或不同，各自为任选取代的 任选地被一个或多个-O-或-S-原子或-N（R 12） - 基团（其中R 12是氢原子或任选取代的烷基）中间的烷基或烯基，或任选地 取代的环烷基，环烯基，芳基或杂芳基，或R 9和R 10与它们所连接的碳原子一起连接在一起形成任选取代的环烷基或环烯基，Het是-O-， - S（O）p- [其中p为0或整数1或2]或-N（R 12） - ，R 11为氢原子或脂族，脂环族，杂脂环族，芳族或 杂芳族基团 X是氨基（-NH 2），取代的氨基，羟基或取代的羟基，或连接至R 5中的Het基团的原子以形成链-X-Alk-R 5 - ，其中X为 - N（R 12） - ，Alk是任选取代的亚烷基链，R 5是-Het-C（R 9）（R 10） - ; 及其盐，溶剂合物，水合物和前药。 这些化合物是口服活性金属蛋白酶抑制剂，特别是具有选择性明胶酶作用，具有长的作用时间，并且可用于预防或治疗其中溶解，胶原酶或明胶酶具有作用的疾病或病症，例如 在治疗癌症中控制肿瘤转移的发展。

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