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    • 2. 发明授权
      US07135502B1 Colchinol derivatives as vascular damaging agents 失效
    • Colchinol derivatives as vascular damaging agents
    • US07135502B1
    • 2006-11-14
    • US09869925
    • 1999-12-24
    • Peter D Davis , Jean-Claude Arnould , Francis T Boyle
    • Peter D Davis , Jean-Claude Arnould , Francis T Boyle
    • A61K31/05
    • A61K31/165
    • The invention relates to the use of compounds of formula (I): wherein X is —C(O)—, —C(S)—, —C═NOH, or —CH(R7)— wherein R7 is hydrogen, hydroxy, C1-7alkoxy, —OR8 or —NR8R9 (wherein R8 is a group —Y1R10 (wherein Y1 is a direct bond, —C(O)—, —C(S)—, —S—, —C(O)O, —C(O)NR11—, —SO2— or —SO2NR12— (wherein R11 and R12, which may be the same or different, each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl) and R10 is as defined herein, and R9 includes hydrogen; R1, R2 and R3 are as defined herein and are preferably methyl; R4, R5 and R6 are as defined herein with the proviso that R5 is not hydroxy, alkoxy, substituted alkoxy, —OPO3H2, —O—C1-7alkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 4. 发明授权
      US06720323B2 Colchinol derivatives as angiogenesis inhibitors 失效
    • Colchinol derivatives as angiogenesis inhibitors
    • Colchinol衍生物作为血管生成抑制剂
    • US06720323B2
    • 2004-04-13
    • US10332271
    • 2003-01-07
    • Jean Claude Arnould
    • Jean Claude Arnould
    • A61K315375
    • C07D295/185 , A61K38/00 , C07C217/74 , C07C2603/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/088 , C07F9/091 , C07K5/06026
    • The invention related to colchinol derivatives of the formula (I): Wherein: R1, R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is 0 or an integer from 1 to 4 inclusive, (provided that when b is 0, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazolyl, phosphoryloxy, hydroxy, amino, N—(C1-4alkyl)amino, N,N-di(C1-3alkyl)amino, or of the formula —Y1(CH2)0R11 or —NHCH(R12)COOH; [wherein Y1 is a direct single bond, —O—, —C(O)—, —N(R13)C(O)— or —C(O)N(R13)— (wherein R13 is hydrogen, C1-4alkyl, C1-3alkoxyC2-3alkyl, aminoC2-3alkyl or hydroxyC2-3alkyl); e is 0 or an integer from 1 to 4 inclusive.
    • 本发明涉及式（I）的科屈醇衍生物：其中：R 1，R 2和R 3各自独立地为羟基，磷酰氧基（-OPO 3 H 2），C 1-4烷氧基或其体内可水解的酯 羟基，条件是R 1，R 2和R 3中的至少2个是C 1-4烷氧基; A是-CO - ， - C（O）O - ， - CON（R 8） - （其中R 8是氢，C 1-4烷基，C 1-3烷氧基C 1-3烷基，氨基C 1-3烷基或羟基C 1-3烷基） ; a是1到4的整数; R 5'和R b独立地选自氢，羟基和氨基; B是-O - ， - CO-，N（R 9）CO-，-CON（R 9） - ， - N（R 9）C（O） 9）CON（R 10） - ， - N（R 9）SO 2 - ， - SO 2 N（R 9） - 或直接单金（其中R 9和R 10独立地 选自氢，C 1-4烷基，C 1-3烷氧基C 1-3烷基，氨基C 1-3烷基和羟基C 1-3烷基）; b为0或1〜4的整数，（b为0时，B为单键直接键合）。 D是羧基，磺基，四唑基，咪唑基，磷酰氧基，羟基，氨基，N-（C 1-4烷基）氨基，N，N-二（C 1-3烷基）氨基或式-Y 1（CH 2） 或-NHCH（R 12）COOH; [其中Y 1是直接单键，-O - ， - C（O） - ， - N（R 13）C（O） - 或-C（O）N（R 13） （其中R 13是氢，C 1-4烷基，C 1-3烷氧基C 2-3 - 烷基，氨基C 2-3 - 烷基或羟基C 2-3 - 烷基）。 e为0或1〜4的整数。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 6. 发明授权
      US06410539B1 Imidazole derivatives and their use as farnesyl protein transferase inhibitors 失效
    • Imidazole derivatives and their use as farnesyl protein transferase inhibitors
    • 咪唑衍生物及其作为法呢基蛋白转移酶抑制剂的用途
    • US06410539B1
    • 2002-06-25
    • US09509476
    • 2000-03-24
    • Jean-Claude Arnould
    • Jean-Claude Arnould
    • A61K3150
    • C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08
    • The present invention relates to a compound of Formula (1) wherein Ar1 represent (A) or (B) or (C); R1 is hydrogen, C1-4alkyl or C1-4alkanoyl; R12 and R13 are independently hydrogen or C1-4alkyl; Ar2 is phenyl or heteroaryl; p is 0 or 1; Ar3 is of formula (I) wherein W, X, Y and Z are independently CH or N, provided that at least two of W, X, Y and Z are CH and R2 and —(CH2)nR3 are attached to ring carbon atoms; R2 is a group of Formula (II) or R2 represents a lactone of Formula (III) the group of Formula (II) or (III) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; provided that: when n is 0, Ar3 is substituted by R2 in the 4-position and —(CH2)nR3 in the 3- or 5-position; and when n is 1 or 2, Ar3 is substituted by R2 in the 3- or 5-position and —(CH2)nR3 in the 4-position; and R5-R9, m and n are as defined in the specification; or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.
    • 本发明涉及式（1）的化合物，其中Ar 1表示（A）或（B）或（C）; R1是氢，C1-4烷基或C1-4烷酰基; R 12和R 13独立地是氢或C 1-4烷基; Ar 2是苯基或杂芳基; p为0或1; Ar 3具有式（I），其中W，X，Y和Z独立地是CH或N，条件是W，X，Y和Z中的至少两个是CH，R 2和 - （CH 2）n R 3连接到环碳原子上 ; R2是式（II）的基团，或R2表示在相应的游离氨基酸中在手性α碳处具有L或D构型的式（II）或（III）的基团的式（III）的内酯; n为0,1或2; R3是苯基或杂芳基; 条件是：当n为0时，Ar 3在4-位被R 2取代，在3-或5-位被 - （CH 2）n R 3取代; 当n为1或2时，Ar 3在3-或5-位被R 2取代，在4-位被 - （CH 2）n R 3取代; 和R5-R9，m和n如说明书中所定义; 或其药学上可接受的盐，前药或溶剂化物。 其制备方法，用作治疗剂和含有它们的药物组合物。 一个特别的用途是癌症治疗。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US07186745B2 Indolone derivatives having vascular damaging activity 失效
    • Indolone derivatives having vascular damaging activity
    • US07186745B2
    • 2007-03-06
    • US10469834
    • 2002-03-04
    • Jean-Claude Arnould
    • Jean-Claude Arnould
    • A61K31/40 , C07D235/24
    • C07D209/34 , A61K31/404
    • This invention relates to the use of compounds of Formula (I) as vascular damaging agents: wherein X is selected from: —O—, —S—, —S(O)—, —S(O2)—, —N(R5)—, —C(O)—, —C(O)N(R5)—, —N(R5)C(O)—, —S(O2)N(R5)—, or —N(R5)S(O2)—; R1 is independently selected from: amino, halo, hydroxy, —OPO3H2, C1-4alkyl, or C1-4alkoxy, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified; R2 is selected from: hydrogen or C1-4alkyl; R3 is selected from: hydrogen, halo, hydroxy, hydroxyC1-4alkyl, cyano, cyanoC1-4alkyl, carboxy, carboxyC1-4alkyl, C1-4alkanoyl, C1-4alkanoylC1-4alkyl, carbamoyl, carbamoylC1-4alkyl, C1-4alkoxy, C1-4alkoxycarbonyl, C1-4alkoxycarbonylC1-4alkyl, C1-4alkoxycarbonylamino, amino, N—C1-4alkylamino, NN-diC1-4alkylamino, aminoC1-4alkyl, N—C1-4alkylaminoC1-4alkyl, NN-diC1-4alkylaminoC1-4alkyl, ureido, or C1-4alkylureyleno; R4 is independently selected from: C1-4alkyl, C1-4alkoxy or halo; R5 is selected from: hydrogen or C1-4alkyl; n is 0 or 1; p is 0, 1, 2 or 3; and q is 0, 1 or 2; or a salt, pro-drug or solvate thereof. The invention also relates to novel compounds of Formula (I) and to processes for the preparation of compounds of Formula (I).
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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