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1. 发明授权

US6140332A Pyrrolopyrimidines and processes for the preparation thereof 失效
标题翻译：吡咯并嘧啶及其制备方法
公开(公告)号：US6140332A
公开(公告)日：2000-10-31
申请号：US981877
申请日：1998-01-26
申请人： Peter Traxler , Guido Bold , Wolfgang Karl-Diether Brill , Jorg Frei
发明人： Peter Traxler , Guido Bold , Wolfgang Karl-Diether Brill , Jorg Frei
IPC分类号： A61K31/505 , A61P35/00 , A61P43/00 , C07D207/34 , C07D471/04 , C07D471/14 , C07D487/04 , A61K31/519
CPC分类号： C07D471/14 , C07D207/34 , C07D487/04
摘要： Described are 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I ##STR1## wherein the symbols are as defined in claim 1. Those compounds inhibit tyrosine protein kinase and can be used in the treatment of hyperproliferative diseases, for example tumour diseases.
摘要翻译： PCT No.PCT / EP96 / 02728 Sec。 371日期1998年1月26日 102（e）日期1998年1月26日PCT Filed 1996年6月24日PCT公布。出版物WO97 / 02266 日期1997年1月23日描述了式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号如权利要求1所定义。这些化合物抑制酪氨酸蛋白激酶，可用于治疗过度增殖性疾病，例如肿瘤疾病。

2. 发明授权

US6140317A Pyrrolopyrimidines and processes for their preparation 失效
标题翻译：吡咯并嘧啶及其制备方法
公开(公告)号：US6140317A
公开(公告)日：2000-10-31
申请号：US117056
申请日：1998-07-22
申请人： Peter Traxler , Jorg Frei , Guido Bold
发明人： Peter Traxler , Jorg Frei , Guido Bold
IPC分类号： A61K31/00 , A61K31/505 , A61K31/519 , A61K31/529 , A61P17/00 , A61P17/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D487/04 , A01N43/00 , A61K31/50 , C07D239/00 , C07D491/00 , C07F5/02
CPC分类号： C07D487/04
摘要： There are described compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the description, Q is heterocyclyl boned via a ring nitrogen atom and having the formula IA ##STR2## wherein R.sub.3 and R.sub.4 and m and n are as defined in the description, the ring marked A is a heterocyclyl having 5 to 9 ring atoms and having at least one saturated bond, it being possible for a further ring hetero atom selected from O and S to be present in addition to the bonding nitrogen atom, the ring system marked B is a free or benzo-, thieno-, furo-, pyrrolo- or dihydropyrrolo-fused carbocyclic ring having from 5 to 9 carbon atoms that is fused to the ring A and may be unsaturated, partially saturated or fully saturated, and the bond marked by a parallel dotted line between the ring systems marked A and B is either a single bond or a double bond, and a salt thereof where at least one salt-forming group is present. The compounds are inhibitors of protein kinases and have, for example, antitumour activity.
摘要翻译： PCT No.PCT / EP97 / 00127 Sec。 371日期：1998年7月22日 102（e）日期1998年7月22日PCT 1997年1月13日PCT PCT。公开号WO97 / 27199 日期：1997年7月31日描述式I化合物，其中R 1和R 2如说明书中所定义，Q是经由环氮原子并具有式IA的杂环基，其中R 3和R 4以及m和n如描述中，标记为A的环是具有5至9个环原子并且具有至少一个饱和键的杂环基，除了键合氮原子之外，还可以存在另外选自O和S的环杂原子，所述环标记为B的系统是具有5至9个碳原子的游离或苯并，噻吩并 - 二氢吡咯并 - 稠合的碳环，其与环A稠合并且可以是不饱和的，部分饱和的或完全饱和的，以及标记为A和B的环状体系之间的平行虚线标记的键是单键或双键，以及其中存在至少一个成盐基团的盐。这些化合物是蛋白激酶的抑制剂，并且具有例如抗肿瘤活性。

3. 发明授权

US5981533A Pyrazole derivatives and processes for the preparation thereof 失效
标题翻译：吡唑衍生物及其制备方法
公开(公告)号：US5981533A
公开(公告)日：1999-11-09
申请号：US930904
申请日：1997-10-03
申请人： Peter Traxler , Pascal Furet , Guido Bold , Jorg Frei , Marc Lang
发明人： Peter Traxler , Pascal Furet , Guido Bold , Jorg Frei , Marc Lang
IPC分类号： C07D231/38 , A61K31/505 , A61P35/00 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I ##STR1## wherein the symbols are as defined in claim 1, and intermediates for their manufacture are described.The compounds of formula I inhibit especially the tyrosine kinase activity of the receptor for epidermal growth factor and can be used, for example, in the case of epidermal hyperproliferation (psoriasis) and as anti-tumor agents.
摘要翻译： PCT No.PCT / EP96 / 01263。 371日期1997年10月3日第 102（e）日期1997年10月3日PCT 1996年3月22日PCT公布。公开号WO96 / 31510PC。日期：19964年10月10日 - 描述了式I的氨基-1H-吡唑并[3,4-d]嘧啶衍生物，其中符号如权利要求1中所定义，其中描述其制备方法。式I的化合物特别地抑制表皮生长因子受体的酪氨酸激酶活性，并且可以用于例如表皮过度增生（牛皮癣）和作为抗肿瘤剂的情况。

4. 发明申请

US20060217388A1 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：US20060217388A1
公开(公告)日：2006-09-28
申请号：US11441961
申请日：2006-05-26
申请人： Guido Bold , Janet King , Jorg Frei , Richard Heng , Paul Manley , Bernhard Wietfeld , Jeanette Wood
发明人： Guido Bold , Janet King , Jorg Frei , Richard Heng , Paul Manley , Bernhard Wietfeld , Jeanette Wood
IPC分类号： A61K31/501 , C07D403/02
CPC分类号： C07D401/06 , A61K31/501 , A61K31/502 , C07D401/14
摘要： The invention relates to the treatment of leukemias 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：本发明涉及用式I的VEGF受体酪氨酸激酶的活性抑制剂治疗白血病，所述取代基在说明书中定义; 以及新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的方法中的应用; 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。

5. 发明授权

US06180636B2 Substituted pyrrolopyrimidines and processes for their preparation 失效
标题翻译：取代的吡咯并嘧啶及其制备方法
公开(公告)号：US06180636B2
公开(公告)日：2001-01-30
申请号：US09242592
申请日：1999-02-19
申请人： Peter Traxler , Guido Bold , Marc Lang , Jörg Frei
发明人： Peter Traxler , Guido Bold , Marc Lang , Jörg Frei
IPC分类号： A61K31519
CPC分类号： C07D487/04
摘要： There are described 7H-pyrrolo[2,3-d]pyrimidine derivatives of the formula I in which the substituents are as defined in claim 1. These compounds inhibit the tyrosine kinase activity of the receptor for the epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumor agents.
摘要翻译：描述了式Iin的7H-吡咯并[2,3-d]嘧啶衍生物，其取代基如权利要求1中所定义。这些化合物抑制表皮生长因子（EGF）受体的酪氨酸激酶活性和c- erbB2激酶，可用作抗肿瘤剂。

6. 发明授权

US07323469B2 7H-pyrrolo[2,3-d]pyrimidine derivatives 失效
标题翻译： 7H-吡咯并[2,3-d]嘧啶衍生物
公开(公告)号：US07323469B2
公开(公告)日：2008-01-29
申请号：US10783000
申请日：2004-02-20
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
IPC分类号： A61K31/519 , A61K31/497 , C07D487/04 , A61P35/04
CPC分类号： C07D487/04
摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.
摘要翻译：本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物及其用途衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。

7. 发明申请

US20060270665A1 Combination comprising an agent decreasing VEGF activity and an agent decreasing EGF activity 审中-公开
标题翻译：包含降低VEGF活性的试剂和降低EGF活性的试剂的组合
公开(公告)号：US20060270665A1
公开(公告)日：2006-11-30
申请号：US11498027
申请日：2006-08-02
申请人： Jeanette Wood , Ralf Brandt , Guido Bold , Peter Traxler
发明人： Jeanette Wood , Ralf Brandt , Guido Bold , Peter Traxler
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/519 , A61K31/517 , A61K31/501
CPC分类号： A61K45/06 , A61K31/505 , A61K31/70 , A61K31/50 , A61K31/335 , A61K2300/00
摘要： The invention relates to a combination which comprises a first active ingredient which is a vasculostatic compound and a second active ingredient which decreases the activity of the epidermal growth factor (EGF), in particular, for the delay of progression or treatment of a disease associated with deregulated angiogenesis, especially a proliferative disease; a pharmaceutical composition comprising such a combination; a commercial package comprising such a combination as a combined preparation; and to a method of treatment of a warm-blooded animal, especially a human.
摘要翻译：本发明涉及一种组合，其包含第一种活性成分，其为血管平滑化合物和降低表皮生长因子（EGF）活性的第二活性成分，特别是延迟进展或治疗与放松血管生成，特别是增殖性疾病; 包含这种组合的药物组合物; 包括作为组合制剂的这种组合的商业包装; 以及治疗温血动物，特别是人的方法。

8. 发明授权

US07244729B2 4-amino-6-phenyl-pyrrolo[2,3-d]pyrimidine derivatives 失效
标题翻译： 4-氨基-6-苯基 - 吡咯并[2,3-d]嘧啶衍生物
公开(公告)号：US07244729B2
公开(公告)日：2007-07-17
申请号：US10485747
申请日：2002-08-06
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
IPC分类号： C07D413/10 , C07D487/04 , A61K31/519 , A61K31/5355 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives-alone or in combination with one or more other pharmaceutically active compounds-for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour
摘要翻译：本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物及其用途衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物

9. 发明申请

US20070161632A1 4-AMINO-6-PHENYL-PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES 失效
标题翻译： 4-氨基-6-苯基 - 吡咯并[2,3-D]吡啶衍生物
公开(公告)号：US20070161632A1
公开(公告)日：2007-07-12
申请号：US11686023
申请日：2007-03-14
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
IPC分类号： A61K31/5377 , A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.
摘要翻译：本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物及其用途衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。

10. 发明授权

US06514974B2 Pyrido-, pyrimido-, pyridazo- and pyrazo- pyridazines having angiogenesis inhibiting activity 失效
标题翻译：具有血管生成抑制活性的吡啶 - ，嘧啶并 - 哒嗪 - 和吡唑并 - 哒嗪
公开(公告)号：US06514974B2
公开(公告)日：2003-02-04
申请号：US09859858
申请日：2001-05-17
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： A61K3150
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, 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.
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。

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