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41. 发明授权

US07399761B2 Phthalazine derivatives with angiogenesis inhibiting activity 失效
标题翻译：具有血管生成抑制活性的酞嗪衍生物
公开(公告)号：US07399761B2
公开(公告)日：2008-07-15
申请号：US10475419
申请日：2002-05-03
申请人： Guido Bold , Paul William Manley
发明人： Guido Bold , Paul William Manley
IPC分类号： C07D401/06 , A61K31/502
CPC分类号： C07D401/06 , C07D405/12 , C07D409/12
摘要： The invention relates to new phthalazine derivatives of formula (I), wherein 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; 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; X is imino, oxa, or thia; Y is hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or unsubstituted or substituted cycloalkyl; and wherein the bonds characterized in subformula (I*) by a wavy line are either single or double bonds; to an N-oxide of a compound of formula I; a tautomer or mixture of tautomers of a compound of formula (I) of an N-oxide thereof; and a pharmaceutically acceptable salt of a compound of formula (I), of an N-oxide or of a tautomer or mixture of tautomers thereof; processes for their preparation and pharmaceutical uses.
摘要翻译：本发明涉及式（I）的新的2,3-二氮杂萘衍生物，其中R 1和R 2：a）在各种情况下独立地为低级烷基; b）一起形成子公式（I *）的桥，其中该键通过两个C末端原子实现，m是0至4; 或c）一起形成子公式（I **）的桥，其中一个或两个环构件T 1，T 2，T 3， SUB>和T 4是氮，其余各自为CH，并且键通过原子T 1和T 4取代。 ; A，B，D，E和T独立地为N或CH，但条件是这些基团中至少一个并且不超过三个为N; X是亚氨基，氧杂或硫杂; Y是氢，取代或未取代的芳基，取代或未取代的杂芳基，或未取代或取代的环烷基; 并且其中通过波浪线表征在子公式（I *）中的键是单键或双键; 涉及式I化合物的N-氧化物; 其互变异构体或其N-氧化物的式（I）化合物的互变异构体的混合物; 和式（I）化合物的药学上可接受的盐，N-氧化物或互变异构体或其互变异构体的混合物; 其制备方法和药物用途。

42. 发明授权

US06686347B2 Phthalazine derivatives for treating inflammatory diseases 失效
标题翻译：用于治疗炎性疾病的酞嗪衍生物
公开(公告)号：US06686347B2
公开(公告)日：2004-02-03
申请号：US09964025
申请日：2001-09-26
申请人： Guido Bold , Janet Dawson King , Jörg Frei , Richard Heng , Paul William Manley , Bernhard Wietfeld , Jeanette Marjorie Wood
发明人： Guido Bold , Janet Dawson King , Jörg Frei , Richard Heng , Paul William Manley , Bernhard Wietfeld , Jeanette Marjorie Wood
IPC分类号： A61K3133
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, the substituents being defined in the specification; 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 neovascularization, 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.
摘要翻译：本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，所述取代基在本说明书中定义;以及新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的过程中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

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