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94 条记录 (耗时 0.046 秒)

    Phthalazine Derivatives with Angiogenesis Inhibiting Activity
    81.
    发明申请
    Phthalazine Derivatives with Angiogenesis Inhibiting Activity 审中-公开
    具有血管发生抑制活性的酞嗪衍生物

    公开(公告)号：US20090076003A1

    公开(公告)日：2009-03-19

    申请号：US12141179

    申请日：2008-06-18

    申请人： Guido Bold ,  Paul William Manley

    发明人： Guido Bold ,  Paul William Manley

    IPC分类号： A61K31/5377 ,  C07D237/30 ,  A61K31/498 ,  A61P29/00 ,  A61P35/00 ,  C07D413/14

    CPC分类号： C07D401/06 ,  C07D405/12 ,  C07D409/12

    摘要： The invention relates to new phthalazine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment of a disease, especially of a disease that responds to the inhibition of tyrosine kinases, more especially the inhibition of the vascular endothelial growth factor (VEGF) receptor kinase, preferably the treatment of a proliferative disease, such as a tumour disease.

    摘要翻译： 本发明涉及新的酞嗪衍生物，其制备方法，其在治疗人或动物体的方法中的应用，其单独使用或与一种或多种其它药物活性化合物组合用于治疗 疾病，特别是对酪氨酸激酶的抑制作出反应的疾病，更特别地抑制血管内皮生长因子（VEGF）受体激酶，优选治疗增殖性疾病如肿瘤疾病。

    Heterobicyclic Carboxamides as Inhibitors for Kinases
    82.
    发明申请
    Heterobicyclic Carboxamides as Inhibitors for Kinases 失效
    异双环酰胺作为激酶抑制剂

    公开(公告)号：US20090030009A1

    公开(公告)日：2009-01-29

    申请号：US12281715

    申请日：2007-03-09

    申请人： Guido Bold ,  Andrea Vaupel ,  Marc Lang

    发明人： Guido Bold ,  Andrea Vaupel ,  Marc Lang

    IPC分类号： A61K31/496 ,  C07D239/24 ,  A61P35/00 ,  A61K31/505

    CPC分类号： C07D413/12 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    摘要： The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.

    摘要翻译： 本发明涉及式（I）的新型有机化合物及其在治疗动物或人体中的用途，包括式（I）化合物的药物组合物和式（I）化合物用于 制备用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，特别是肿瘤疾病的药物组合物。

    Phthalazine derivatives for treating inflammatory diseases
    85.
    发明申请
    Phthalazine derivatives for treating inflammatory diseases 审中-公开

    公开(公告)号：US20050176711A1

    公开(公告)日：2005-08-11

    申请号：US11099292

    申请日：2005-04-05

    申请人： Guido Bold ,  Janet King ,  Joerg Frei ,  Richard Heng ,  Paul Manley ,  Bernhard Wietfeld ,  Jeanette Wood

    发明人： Guido Bold ,  Janet King ,  Joerg Frei ,  Richard Heng ,  Paul Manley ,  Bernhard Wietfeld ,  Jeanette Wood

    IPC分类号： A61K31/502 ,  A61K31/506 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P25/04 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  A61K31/53 ,  A61K31/501 ,  C07D43/02

    CPC分类号： C07D401/06 ,  A61K31/501 ,  A61K31/502 ,  C07D401/14

    摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, wherein r is 0 to 2, n is 0 to 3 R1 and R2 a) are independently in each case a lower alkyl; b) together form a bridge of subformula I*, wherein the bond is achieved via the two terminal C atoms and m is 0 to 4, or c) together form a bridge of subformula I**, wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen, and the others are in each case CH, and the bond is achieved via atoms T1 and T4; G is —C(═O)—, —CHF—, —CF2—, lower alkylene, C2-C6alkenylene, lower alkylene or C3-C6alkenylene substituted by acyloxy or hydroxy, —CH2—O—, —CH2S—, —CH2—NH—, —CH2—O—CH2—, —CH2—S—CH2—, —CH2—NH—CH2—, oxa (—O—), thia (—S—), imino (—NH—), —CH2—O—CH2—, —CH2S—CH2— or —CH2—NH—CH2—; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; Q is lower alkyl, lower alkoxy or halogen; Ra and Ra′ are each independently H or lower alkyl; X is imino, oxa, or thia; Y is hydrogen, aryl, heteroaryl, or unsubstituted or substituted cycloalkyl; and Z is mono- or disubstituted 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, alkylphenylsulfonyl, or (alternatively or, in a broader aspect of the invention, in addition) selected from the group consisting of ureido, halo-lower alkylthio, halo-lower alkansulfonyl, pyrazolyl, lower-alkyl pyrazolyl and C2-C7alkenyl; wherein—if more than 1 radical Z (m≧2) is present—the substituents Z are selected independently from each other; and wherein the bonds characterized in subformula I* by a wavy line are either single or double bonds; or an N-oxide of said compound, wherein 1 or more N atoms carry an oxygen atom; or a pharmaceutically acceptable salt thereof; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularisation, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

    Phthalazines with angiogenesis inhibiting activity
    87.
    发明授权
    Phthalazines with angiogenesis inhibiting activity 失效
    具有血管生成抑制活性的酞嗪类

    公开(公告)号：US06710047B2

    公开(公告)日：2004-03-23

    申请号：US10338062

    申请日：2003-01-07

    申请人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

    发明人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

    IPC分类号： A61K31495

    CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

    摘要： 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.

    摘要翻译： 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。

    Isoquinoline derivatives with angiogenesis inhibiting activity
    88.
    发明授权
    Isoquinoline derivatives with angiogenesis inhibiting activity 失效
    具有血管生成抑制活性的异喹啉衍生物

    公开(公告)号：US06608071B2

    公开(公告)日：2003-08-19

    申请号：US09781036

    申请日：2001-02-09

    申请人： Karl-Heinz Altmann ,  Guido Bold ,  Paul William Manley

    发明人： Karl-Heinz Altmann ,  Guido Bold ,  Paul William Manley

    IPC分类号： A61K31505

    CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

    摘要： 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.

    摘要翻译： 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。

    Antivirally active heterocyclic azahexane derivatives
    90.
    发明授权
    Antivirally active heterocyclic azahexane derivatives 有权
    抗病毒活性杂环氮杂己烷衍生物

    公开(公告)号：US06300519B1

    公开(公告)日：2001-10-09

    申请号：US09448328

    申请日：1999-11-23

    申请人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    发明人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    IPC分类号： C07C20904

    CPC分类号： C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

    摘要： There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

    摘要翻译： 描述式I *的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基，R 4 是通过环碳原子键合的不饱和杂环基在4-位上被取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，脯氨酰基的杂原子（ -SO-）和磺酰基（-SO 2 - ），并且是未取代的或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中提及的含义之一，R 6独立地为R 1，为低级烷氧基羰基 或其盐，条件是存在至少一种成盐基团。化合物是天冬氨酸逆转录病毒蛋白酶的抑制剂，并且可以用于例如AIDS的治疗。 它们具有出色的药效学性质。