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    • 5. 发明授权
      US06514974B2 Pyrido-, pyrimido-, pyridazo- and pyrazo- pyridazines having angiogenesis inhibiting activity 失效
    • Pyrido-, pyrimido-, pyridazo- and pyrazo- pyridazines having angiogenesis inhibiting activity
    • 具有血管生成抑制活性的吡啶 - ，嘧啶并 - 哒嗪 - 和吡唑并 - 哒嗪
    • US06514974B2
    • 2003-02-04
    • US09859858
    • 2001-05-17
    • Guido Bold , Jörg Frei , Peter Traxler , Karl-Heinz Altmann , Helmut Mett , David Raymond Stover , Jeanette Marjorie Wood
    • Guido Bold , Jörg Frei , Peter Traxler , Karl-Heinz Altmann , Helmut Mett , David Raymond Stover , Jeanette Marjorie Wood
    • A61K3150
    • C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D471/04
    • The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are as defined, then G is selected from the group comprising lower alkylene, —CH2—O—, —CH2—S—, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.
    • 本发明涉及式I化合物，其中r为0至2，n为0至2; m为0〜4; R1和R2（i）在每种情况下都是低级烷基，或（ii）一起在子式I *中形成桥，或（iii）一起形成子式I **中的桥，其中一个或两个环成员T1，T2 ，T3和T4是氮，余数分别为CH; A，B，D和E是N或CH，其中不多于2个这些基团是N; G是低级亚烷基，酰氧基或羟基 - 低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂，硫杂或亚氨基; Q是甲基; R为H或低级烷基; X是亚氨基，氧杂或硫杂; Y是芳基，吡啶基或（未）取代的环烷基; 羟基，醚化或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二取代的氨基甲酰基，脒基， 胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基。 并且其中以波浪线表征的键是单键或双键; 或所述化合物的N-氧化物，其规定如果Y是吡啶基或未取代的环烷基，则X是亚氨基，剩余的基团如所定义，则G选自低级亚烷基，-CH 2 -O-， -CH 2 -S-，氧杂和硫杂; 或其盐。 该化合物抑制血管发生。
    • 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
      US06710047B2 Phthalazines with angiogenesis inhibiting activity 失效
    • Phthalazines with angiogenesis inhibiting activity
    • 具有血管生成抑制活性的酞嗪类
    • US06710047B2
    • 2004-03-23
    • US10338062
    • 2003-01-07
    • Guido Bold , Jörg Frei , Peter Traxler , Karl-Heinz Altmann , Helmut Mett , David Raymond Stover , Jeanette Marjorie Wood
    • Guido Bold , Jörg Frei , Peter Traxler , Karl-Heinz Altmann , Helmut Mett , David Raymond Stover , Jeanette Marjorie Wood
    • A61K31495
    • C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D471/04
    • The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etheritied or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are as defined, then G is selected from the group comprising lower alkylene, —CH2—O—, —CH2—S—, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.
    • 本发明涉及式I化合物，其中r为0至2，n为0至2; m为0〜4; R1和R2（i）在每种情况下都是低级烷基，或（ii）一起在子式I *中形成桥，或（iii）一起形成子式I **中的桥，其中一个或两个环成员T1，T2 ，T3和T4是氮，余数分别为CH; A，B，D和E是N或CH，其中不多于2个这些基团是N; G是低级亚烷基，酰氧基或羟基 - 低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂，硫杂或亚氨基; Q是甲基; R是H或低级烷基; X是亚氨基，氧杂或硫杂; Y是芳基，吡啶基或（未）取代的环烷基; 羟基，醚基或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二取代的氨基甲酰基，脒基， 胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基。 并且其中以波浪线表征的键是单键或双键; 或所述化合物的N-氧化物，其规定如果Y是吡啶基或未取代的环烷基，则X是亚氨基，剩余的基团如所定义，则G选自低级亚烷基，-CH 2 -O-， -CH 2 -S-，氧杂和硫杂; 或其盐。 该化合物抑制血管发生。
    • 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
    • 7. 发明授权
      US06608071B2 Isoquinoline derivatives with angiogenesis inhibiting activity 失效
    • Isoquinoline derivatives with angiogenesis inhibiting activity
    • 具有血管生成抑制活性的异喹啉衍生物
    • US06608071B2
    • 2003-08-19
    • US09781036
    • 2001-02-09
    • Karl-Heinz Altmann , Guido Bold , Paul William Manley
    • Karl-Heinz Altmann , Guido Bold , Paul William Manley
    • A61K31505
    • C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14
    • The invention relates to compounds of formula I wherein r is from 0 to 2; n is from 0 to 2; m is from 0 to 4; A, B, D and E are each independently of the others N or CH, with the proviso that not more than two of those radicals are N; G is lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa (—O—), thia (—S—) or imino (—NH—), or is lower alkylene substituted by acyloxy or by hydroxy; Q is lower alkyl, especially methyl; R is H or lower alkyl; X is imino, oxa or thia; Y is lower alkyl or, especially, aryl, heteroaryl or unsubstituted or substituted cycloalkyl; and Z is amino, mono- or di-substituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-di-substituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenyl-sulfinyl, phenylsulfonyl, phenyl-lower alkanesulfonyl or alkylphenylsulfonyl, and where, if more than one radical Z is present (m≧2), the substituents Z are identical or different; and wherein the bonds indicated by a wavy line are either single bonds or double bonds; or an N-oxide of the mentioned compound, wherein one or more N atoms carry an oxygen atom; or a salt thereof. The compounds inhibit especially angiogenesis.
    • 本发明涉及式I的化合物，其中0至2; n为0〜2; m为0至4; A，B，D和E各自独立地为N或CH，条件是不多于两个这些基团为N; G为低级亚烷基，-CH 2 -O-， - CH2-，-CH2-NH-，氧杂（-O-），硫杂（-S-）或亚氨基（-NH-），或被酰氧基或羟基取代的低级亚烷基; Q是低级烷基， ; R为H或低级烷基; X为亚氨基，氧杂或硫杂; Y为低级烷基或特别是芳基，杂芳基或未取代或取代的环烷基; 羟基，醚化或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二 - 取代的烷基， 取代的氨基甲酰基，脒基，胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基 - 亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基，其中如果多于一个基团Z 存在（m> = 2）时，取代基Z相同或不同;其中由波浪线表示的键为单键或双键;或所述化合物的N-氧化物，其中一个或多个N原子携带 氧原子;或其盐。 该化合物特别抑制血管生成。
    • 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
    • 8. 发明授权
      US06258812B1 Phthalazines with angiogenesis inhibiting activity 有权
    • Phthalazines with angiogenesis inhibiting activity
    • 具有血管生成抑制活性的酞嗪类
    • US06258812B1
    • 2001-07-10
    • US09367273
    • 1999-10-20
    • Guido Bold , Jörg Frei , Peter Traxler , Karl-Heinz Altmann , Helmut Mett , David Raymond Stover , Jeanette Marjorie Wood
    • Guido Bold , Jörg Frei , Peter Traxler , Karl-Heinz Altmann , Helmut Mett , David Raymond Stover , Jeanette Marjorie Wood
    • A61K31498
    • C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D471/04
    • The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* (I*) or (iii) together form a bridge in subformula I** (I**), wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; c is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are a s defined, then G is selected from the group comprising lower alkylene, —CH2—O—, CH2—S—, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.
    • 本发明涉及式I化合物，其中r为0至2，n为0至2; m为0〜4; R1和R2（i）在每种情况下都是低级烷基，或（ii）一起在子式I *（I *）中形成桥，或（iii）一起形成子式I **（I **）中的桥，其中 环成员T1，T2，T3和T4中的一个或两个是氮，余下的都是CH; A，B，D和E是N或CH，其中不多于2个这些基团是N; G是低级亚烷基，酰氧基或羟基 - 低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂，硫杂或亚氨基; Q是甲基; c是H或低级烷基; X是亚氨基，氧杂或硫杂; Y是芳基，吡啶基或（未）取代的环烷基; 羟基，醚化或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二取代的氨基甲酰基，脒基， 胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基。 并且其中以波浪线表征的键是单键或双键; 或所述化合物的N-氧化物，其规定如果Y是吡啶基或未取代的环烷基，则X是亚氨基，剩余的基团如所定义，则G选自低级亚烷基，-CH 2 -O-， CH2-S-，氧杂和硫杂; 或其盐。 该化合物抑制血管发生。
    • 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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