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1. 发明授权

US07122547B1 Anthranilic acid amides and the use thereof as medicaments 失效
标题翻译：邻氨基苯甲酸酰胺及其作为药物的用途
公开(公告)号：US07122547B1
公开(公告)日：2006-10-17
申请号：US09831506
申请日：1999-11-09
申请人： Andreas Huth , Dieter Seidelmann , Karl-Heinz Thierauch , Guido Bold , Paul William Manley , Pascal Furet , Jeanette Marjorie Wood , Jürgen Mestan , Jose Brüggen , Stefano Ferrari , Martin Krüger , Eckhard Ottow , Andreas Menrad , Michael Schirner
发明人： Andreas Huth , Dieter Seidelmann , Karl-Heinz Thierauch , Guido Bold , Paul William Manley , Pascal Furet , Jeanette Marjorie Wood , Jürgen Mestan , Jose Brüggen , Stefano Ferrari , Martin Krüger , Eckhard Ottow , Andreas Menrad , Michael Schirner
IPC分类号： A61K31/505 , C07D239/26
CPC分类号： C07C237/32
摘要： The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.
摘要翻译：本发明涉及邻氨基苯甲酸酰胺及其用作治疗由持续血管发生引起的疾病的药物，以及邻氨基苯甲酸酰胺生产中的中间产物。

2. 发明授权

US07002022B2 N-Aryl (thio) anthranilic acid amide derivatives, their preparation and their use as VEGF 失效
标题翻译： N-芳基（硫代）邻氨基苯甲酸酰胺衍生物，其制备及其作为VEGF的用途
公开(公告)号：US07002022B2
公开(公告)日：2006-02-21
申请号：US10828951
申请日：2004-04-21
申请人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
发明人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
IPC分类号： C07C49/76 , C07C49/786 , C07C49/82 , C07C49/825 , C07C49/884
CPC分类号： A61K31/415 , A61K31/44 , A61K31/47 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/89 , C07D215/12 , C07D233/54 , C07D405/12
摘要： Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R2 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要翻译：描述的是式（I）的化合物，其中W是O或S; X是NR 8; Y为CR 9 R 10 - （CH 2）n其中R 9和R 10为氢， / SUB>彼此独立地为氢或低级烷基，n为0〜3的整数。或Y为SO 2; R 2是芳基; R 2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二甲酰亚氨基，并且在Y = SO的情况下 2不能表示2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地是H或除氢以外的取代基; 和R 7和R 8彼此独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。式（I）化合物可用于治疗，例如，的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

3. 发明授权

US08552002B2 Compounds and compositions as protein kinase inhibitors 有权
标题翻译：化合物和组合物作为蛋白激酶抑制剂
公开(公告)号：US08552002B2
公开(公告)日：2013-10-08
申请号：US11570983
申请日：2005-06-23
申请人： Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul William Manley , Joseph Schoepfer , Carsten Spanka
发明人： Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul William Manley , Joseph Schoepfer , Carsten Spanka
IPC分类号： A01N43/54 , C07D239/02
CPC分类号： C07D239/48 , C07D251/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
摘要翻译：本发明涉及式（I）化合物，其中取代基X1，R1，R2，R3和R4具有本发明说明书中阐述和解释的含义，制备这些化合物的方法，含有它们的药物组合物，其任选与一种或多种其它药学活性化合物组合用于治疗对蛋白激酶活性的抑制作出反应的疾病的用途，以及治疗这种疾病的方法。

4. 发明授权

US07652022B2 Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases 失效
标题翻译：用于治疗蛋白激酶依赖性疾病的二芳基脲衍生物
公开(公告)号：US07652022B2
公开(公告)日：2010-01-26
申请号：US10515113
申请日：2003-05-28
申请人： Andreas Floersheimer , Pascal Furet , Paul William Manley , Guido Bold , Eugen Boss , Vito Guagnano , Andrea Vaupel
发明人： Andreas Floersheimer , Pascal Furet , Paul William Manley , Guido Bold , Eugen Boss , Vito Guagnano , Andrea Vaupel
IPC分类号： A01N43/54 , A01N43/40 , A61K31/505 , A61K31/44 , C07D239/02
CPC分类号： C07D213/40 , A61K31/33 , A61K31/395 , C07D213/38 , C07D213/64 , C07D213/68 , C07D213/69 , C07D213/81 , C07D213/84 , C07D213/89 , C07D239/34 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/52 , C07D401/04 , C07D401/12 , C07D403/12
摘要： The invention relates to the use of diaryl urea derivatives in the treatment of protein kinase dependent diseases or for the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising diaryl urea derivatives for the treatment of said diseases, diaryl urea derivatives for use in the treatment of said diseases, novel diaryl urea derivatives, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.
摘要翻译：本发明涉及二芳基脲衍生物在治疗蛋白激酶依赖性疾病或用于制备用于治疗所述疾病的药物组合物中的用途，二芳基脲衍生物在治疗所述疾病中的应用方法，药物制剂包括用于治疗所述疾病的二芳基脲衍生物，用于治疗所述疾病的二芳基脲衍生物，新型二芳基脲衍生物，包含这些新型二芳基脲衍生物的药物制剂，制备新型二芳基脲衍生物的方法，或使用上述新型二芳基脲衍生物的方法，和/或这些新型二芳基脲衍生物用于动物或人体的治疗。

5. 发明授权

US08034814B2 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：US08034814B2
公开(公告)日：2011-10-11
申请号：US12953837
申请日：2010-11-24
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, and to 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 especially of a disease that responds to the inhibition of especially the vascular endothelial growth factor receptor kinase, preferably the treatment of a proliferative disease, or the treatment of inflammatory rheumatic or rheumatoid arthritis and/or pain; and the use of such a compound alone or in combination with one or more other pharmaceutically active compounds for the manufacture of a pharmaceutical preparation for the treatment of said diseases in an animal.
摘要翻译：本发明涉及式I的新的酞嗪衍生物及其制备方法，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的组合特别是治疗特别是对特别是血管内皮生长因子受体激酶的抑制，优选治疗增殖性疾病或治疗炎性风湿性或类风湿性关节炎和/或疼痛的疾病的治疗; 以及这种化合物单独使用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动物中所述疾病的药物制剂。

6. 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。

7. 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。

8. 发明授权

US06878720B2 VEGF receptor tyrosine kinase inhibitors 失效
标题翻译： VEGF受体酪氨酸激酶抑制剂
公开(公告)号：US06878720B2
公开(公告)日：2005-04-12
申请号：US10180289
申请日：2002-06-26
申请人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
发明人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
IPC分类号： C07D233/64 , A61K20060101 , A61K31/00 , A61K31/166 , A61K31/167 , A61K31/415 , A61K31/417 , A61K31/44 , A61K31/4409 , A61K31/443 , A61K31/444 , A61K31/47 , A61K31/4745 , A61K31/497 , A61K31/505 , A61P20060101 , A61P17/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07C20060101 , C07C223/02 , C07C237/30 , C07C317/26 , C07D20060101 , C07D211/22 , C07D213/04 , C07D213/38 , C07D213/40 , C07D213/61 , C07D213/64 , C07D213/89 , C07D215/12 , C07D215/14 , C07D215/36 , C07D215/58 , C07D233/54 , C07D265/26 , C07D401/12 , C07D401/14 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D471/02
CPC分类号： A61K31/415 , A61K31/44 , A61K31/47 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/89 , C07D215/12 , C07D233/54 , C07D405/12
摘要： Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a bicyclic heteroaryl group comprising one ring nitrogen atom with the exception that R2 cannot represent 2-phthalimidyl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要翻译：描述的是式（I）的化合物，其中W是O或S; X为NR8; Y为CR 9 R 10 - （CH 2）n，其中R 9和R 10彼此独立地为氢或低级烷基，n为0〜3的整数。或Y为SO2; R1是芳基; R2是包含一个环氮原子的二环杂芳基，不同的是R 2不能代表2-邻苯二酰亚氨基; R 3，R 4，R 5和R 6中的任何一个独立地为H或氢以外的取代基; 且R 7和R 8彼此独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。式（I）化合物可用于治疗，例如，的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

9. 发明授权

US06706731B2 Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase 失效
标题翻译：抑制血管发生和/或VEGF受体酪氨酸激酶的吡啶衍生物
公开(公告)号：US06706731B2
公开(公告)日：2004-03-16
申请号：US10203579
申请日：2002-10-11
申请人： Guido Bold , Paul William Manley
发明人： Guido Bold , Paul William Manley
IPC分类号： C07D47104
CPC分类号： C07D401/06 , C07D471/04
摘要： The invention relates to pyridine derivatives of formula I: wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage in the preparation of a pharmaceutical composition for the treatment of a disease which responds to an inhibition of angiogenesis, and pharmaceutical compositions containing such compounds.
摘要翻译：本发明涉及式I的吡啶衍生物：其中取代基和符号如说明书所述定义，其制备方法，它们在制备用于治疗对抑制作用的疾病的药物组合物中的用途血管生成和含有这些化合物的药物组合物。

10. 发明授权

US06624174B2 2-amino-nicotinamide derivatives and their use as VEGF-receptor tyrosine kinase inhibitors 有权
标题翻译： 2-氨基 - 烟酰胺衍生物及其作为VEGF-受体酪氨酸激酶抑制剂的用途
公开(公告)号：US06624174B2
公开(公告)日：2003-09-23
申请号：US10181005
申请日：2002-07-11
申请人： Paul William Manley , Guido Bold
发明人： Paul William Manley , Guido Bold
IPC分类号： C07D21382
CPC分类号： C07D213/82 , A61K31/445 , C07D213/89 , C07D401/14 , C07D417/14
摘要： The invention relates to the use of 2 amino-nicotinamide derivatives of formula I wherein n is from 1 up to and including 6; W is O or S; R1 and R3 represent independently of each other hydrogen, lower alkyl or lower acyl; R2 represents a cycloalkyl group, an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; R and R′ are independently of each other hydrogen or lower alkyl; X represents an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; or a N-oxide, a possible tautomer thereof or a pharmaceutically acceptable salt of such a compound, alone or in combination with one or more other pharmaceutically active compounds for the preparation of a pharmaceutical composition for use for therapy of a disease which responds to an inhibition of the VEGF-receptor tyrosine kinase activity; and to new 2-amino-nicotinamide derivatives of formula I and processes for the preparation thereof.
摘要翻译：本发明涉及式I的2种氨基 - 烟酰胺衍生物的用途，其中n为1至6，W为O或S; R 1和R 3彼此独立地为氢，低级烷基或低级酰基; R 2表示环烷基，芳基或包含一个或多个环氮原子和0,1或2个彼此独立地选自氧和硫的杂原子的单环或双环杂芳基，这些基团在每种情况下是未取代的或单取代或多取代; R和R'彼此独立地为氢或低级烷基; X表示芳基，或单环或双环杂芳基，其包含一个或多个环氮原子和0,1或2个独立地为彼此选自氧和硫，这些基团在每种情况下都是未取代的或单取代或多取代的;或N-氧化物，其可能的互变异构体或这种化合物的药学上可接受的盐，alo ne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对VEGF-受体酪氨酸激酶活性的抑制作出反应的疾病的药物组合物;以及新的2-氨基 - 烟酰胺衍生物式I及其制备方法。

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