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1. 发明申请

WO2003099771A3 DIARYL UREA DERIVATIVES USEFUL FOR THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES 审中-公开
公开(公告)号：WO2003099771A3
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005634
申请日：2003-05-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, William , BOLD, Guido , BOSS, Eugen , GUAGNANO, Vito , VAUPEL, Andrea
发明人： FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, William , BOLD, Guido , BOSS, Eugen , GUAGNANO, Vito , VAUPEL, Andrea
IPC分类号： C07D213/68
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.

2. 发明申请

WO2003040102A1 ANTHRANILIC ACID AMIDES AND THEIR USE AS VEGF RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：氨基酸类抗坏血酸和其作为VEGF受体酪氨酸激酶抑制剂的用途
公开(公告)号：WO2003040102A1
公开(公告)日：2003-05-15
申请号：PCT/EP2002/012444
申请日：2002-11-07
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
发明人： BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
IPC分类号： C07D213/64
CPC分类号： C07D213/64 , C07D213/70
摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein R 1 represents H or lower alkyl, R 2 represents H or lower alkyl, R 3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof 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 neoplastic disease, such as a tumor disease, of retinopathy or age - related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, 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 a neoplastic disease, of retinopathy or age-related macular degeneration.
摘要翻译：本发明涉及式（I）的邻氨基苯甲酰胺衍生物，其中R1表示H或低级烷基，R2表示H或低级烷基，R3表示全氟低级烷基，X表示O或S，或N-氧化物或互变异构体其邻氨基苯甲酸酰胺，其N-氧化物及其互变异构体的盐; 其制备方法，其用于治疗人或动物体的应用，其单独使用或与一种或多种其它药学活性化合物组合用于特别是肿瘤性疾病如肿瘤疾病的治疗，视网膜病变或年龄相关性黄斑变性; 用于治疗动物，特别是人类中的这种疾病的方法，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的用途，用于制备用于治疗肿瘤的药物制剂视网膜病变或年龄相关性黄斑变性疾病。

3. 发明申请

WO2003099771A2 DIARYL UREA DERIVATIVES USEFUL FOR THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES 审中-公开
标题翻译：用于治疗蛋白激酶依赖性疾病的二尿嘧啶衍生物
公开(公告)号：WO2003099771A2
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005634
申请日：2003-05-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, William , BOLD, Guido , BOSS, Eugen , GUAGNANO, Vito , VAUPEL, Andrea
发明人： FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, William , BOLD, Guido , BOSS, Eugen , GUAGNANO, Vito , VAUPEL, Andrea
IPC分类号： C07C275/00
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。

4. 发明申请

WO2004052884A1 ANTHRANILIC ACID AMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：氨基酸衍生物及其药物用途
公开(公告)号：WO2004052884A1
公开(公告)日：2004-06-24
申请号：PCT/EP2003/014086
申请日：2003-12-11
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
发明人： BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
IPC分类号： C07D409/04
CPC分类号： C07D405/04 , C07D213/38 , C07D213/50 , C07D213/61 , C07D213/64 , C07D213/74 , C07D401/12 , C07D409/04 , C07D417/04
摘要： The present invention relates to new anthranilic acid amide 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.
摘要翻译：本发明涉及新的邻氨基苯甲酸酰胺衍生物，其制备方法，其在人或动物体的治疗方法中的应用，其用途 - 单独使用或与一种或多种其它药学活性化合物组合。

5. 发明申请

WO2003040101A1 ANTHRANILIC ACID AMIDES AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：氨基酸和其药物用途
公开(公告)号：WO2003040101A1
公开(公告)日：2003-05-15
申请号：PCT/EP2002/012445
申请日：2002-11-07
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
发明人： BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
IPC分类号： C07D213/38
CPC分类号： C07C237/40 , C07D213/38 , C07D213/89
摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein Ar is represented by the subformula (I a ), wherein R a represents H or lower alkyl, and R 1 represents H or perfluoro lower alkyl, R 2 represents H, halogen, C 2 -C 7 alkyl, C 2 -C 7 alkenyl or lower aklynyl; or Ar is represented by the subformula (I b ) and R 1 represents perfluoro lower alkyl, and R 2 represents bromo, iodo, C 2 -C 7 alkyl, C 2 -C 7 alkenyl or lower alkynyl, or R 1 represents H, and R 2 represents fluoro, bromo, iodo, ethyl, C 5 -C 7 alkyl, C 2 -C 7 alkenyl or lower alkynyl; to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age-related macular degeneration; to a method for the treatment of such diseases in animals; and to 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 a neoplastic disease, of retinopathy or age-related macular degeneration.
摘要翻译：本发明涉及式（I）的邻氨基苯甲酰胺衍生物，其中Ar由亚式（Ia）表示，其中Ra表示H或低级烷基，R1表示H或全氟低级烷基，R2表示H，卤素，C2- C7烷基，C2-C7链烯基或低级甲酰胺基; 或Ar由亚式（Ib）表示，R 1表示全氟低级烷基，R 2表示溴，碘，C 2 -C 7烷基，C 2 -C 7链烯基或低级炔基，或R 1表示H，R 2表示氟，溴，碘，乙基 C 5 -C 7烷基，C 2 -C 7链烯基或低级炔基; 其N-氧化物和互变异构体，以及这种邻氨基苯甲酰胺，其N-氧化物和互变异构体的盐; 进行准备; 其用于治疗人或动物体的用途，其单独使用或与一种或多种其它药学活性化合物组合用于特别是治疗视网膜病变或年龄的肿瘤疾病如肿瘤疾病的治疗相关性黄斑变性; 涉及在动物中治疗这些疾病的方法; 以及使用这样的化合物 - 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肿瘤性疾病，视网膜病变或年龄相关性黄斑变性的药物制剂。

6. 发明申请

WO2004005281A1 INHIBITORS OF TYROSINE KINASES 审中-公开
标题翻译： TYROSINE KINASES的抑制剂
公开(公告)号：WO2004005281A1
公开(公告)日：2004-01-15
申请号：PCT/EP2003/007198
申请日：2003-07-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BREITENSTEIN, Werner , FURET, Pascal , JACOB, Sandra , MANLEY, Paul, William
发明人： BREITENSTEIN, Werner , FURET, Pascal , JACOB, Sandra , MANLEY, Paul, William
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D405/14
摘要： The invention relates to compounds of formula (I) Wherein the substituents R1, R2 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, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such disease.
摘要翻译：本发明涉及式（I）化合物，其中取代基R 1，R 2和R 4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，其用途任选地与一种或多种其它药物活性化合物组合，用于治疗对蛋白激酶活性，特别是肿瘤疾病，特别是白血病的抑制作出反应的疾病，以及治疗这种疾病的方法。

7. 发明申请

WO2005027973A2 COMBINATIONS OF A VEGF RECEPTOR INHIBITOR WITH OTHER THERAPEUTIC AGENTS 审中-公开
标题翻译： VEGF受体抑制剂与其他治疗药物的联合应用
公开(公告)号：WO2005027973A2
公开(公告)日：2005-03-31
申请号：PCT/EP2004/010701
申请日：2004-09-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , BOLD, Guido , BRUEGGEN, Josef, Bernhard , HUANG, Jerry, Min-Jian , KINDER, Frederick, Ray , LANE, Heidi , LATOUR, Elisabeth, Jeanne , MANLEY, Paul, William , WOOD, Jeanette, Marjorie
发明人： BOLD, Guido , BRUEGGEN, Josef, Bernhard , HUANG, Jerry, Min-Jian , KINDER, Frederick, Ray , LANE, Heidi , LATOUR, Elisabeth, Jeanne , MANLEY, Paul, William , WOOD, Jeanette, Marjorie
IPC分类号： A61K45/06
CPC分类号： A61K45/06
摘要： The invention relates to a combination therapy for treating patients suffering from diseases characterized by cell proliferation and infiltration of inflammatory cells, coronary diseases, hypertension, renal diseases, diabetes, or ocular diseases and conditions. The patient is treated with a combination of: (a) a VEGF inhibitor compound; and (b) one or more second therapeutic agents selected from the group consisting of: i. angiostatic steroids; ii. photosensitizers; iii. implants containing corticosteroids; iv. AT1 receptor antagonists; V. ACE inhibitors; vi. cyclooxygenase inhibitors; vii. IGF-IR inhibitors; viii. mTOR kinase inhibitors; ix. somatostatin receptor antagonists; X. P13K inhibitors; A. Raf kinase inhibitors; xii. PKC inhibitors; xiii. integrin antagonists; xiv. endogenous anti-anglogenic molecules; and xv. PEDF and analogs.
摘要翻译：本发明涉及用于治疗患有以细胞增殖和炎症细胞浸润，冠状动脉疾病，高血压，肾脏疾病，糖尿病或眼部疾病和病症为特征的疾病的患者的组合疗法。用以下组合治疗患者：（a）VEGF抑制剂化合物; 和（b）一种或多种选自以下的第二治疗剂：i。血管生成抑制类固醇; II。光敏剂; III。含有皮质类固醇的植入物; IV。 AT1受体拮抗剂; V. ACE抑制剂; 六。环氧合酶抑制剂; 七。 IGF-1R抑制剂; 八。 mTOR激酶抑制剂; 九。生长抑素受体拮抗剂; X.P13K抑制剂; A.Raf激酶抑制剂; 十二。 PKC抑制剂; 十三。整联蛋白拮抗剂; 十四。内源性抗血管生成分子; 和xv。 PEDF和类似物。

8. 发明申请

WO2005027972A3 COMBINATION OF A VEGF RECEPTOR INHIBITOR WITH A CHEMOTHERAPEUTIC AGENT 审中-公开
公开(公告)号：WO2005027972A3
公开(公告)日：2005-03-31
申请号：PCT/EP2004/010686
申请日：2004-09-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , BRUEGGEN, Josef, Bernhard , HUANG, Jerry, Min-Jian , KINDER, Frederick, Ray, Jr. , LANE, Heidi , LATOUR, Elisabeth, Jeanne , MANLEY, Paul, William , WOOD, Jeanette, Marjorie
发明人： BOLD, Guido , BRUEGGEN, Josef, Bernhard , HUANG, Jerry, Min-Jian , KINDER, Frederick, Ray, Jr. , LANE, Heidi , LATOUR, Elisabeth, Jeanne , MANLEY, Paul, William , WOOD, Jeanette, Marjorie
IPC分类号： A61K45/06
摘要： The present invention relates to a combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis. The patient is treated with a VEGF inhibitor compound; and one or more chemotherapeutic agents.

9. 发明申请

WO2004029038A1 NOVEL PYRIMIDINEAMIDE DERIVATIVES AND THE USE THEREOF 审中-公开
标题翻译：新型吡咯胺酰胺衍生物及其用途
公开(公告)号：WO2004029038A1
公开(公告)日：2004-04-08
申请号：PCT/EP2003/010724
申请日：2003-09-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , MANLEY, Paul, William , BREITENSTEIN, Werner , JACOB, Sandra , FURET, Pascal
发明人： MANLEY, Paul, William , BREITENSTEIN, Werner , JACOB, Sandra , FURET, Pascal
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The invention relates to novel substituted N-(3-benzoylaminophenyl)-4-pyridyl-2-pyrimidinarnine derivatives, processes for the preparation thereof, 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, especially a neoplastic disease, and a method for the treatment of such a disease.
摘要翻译：本发明涉及新的取代的N-（3-苯甲酰氨基苯基）-4-吡啶基-2-嘧啶胺衍生物，其制备方法，含有它们的药物组合物，其用途任选与一种或多种其它药物活性化合物组合用于治疗对抑制蛋白激酶活性，特别是肿瘤性疾病作出反应的疾病以及治疗这种疾病的方法。

10. 发明申请

WO2002092603A1 OXAZOLO-AND FUROPYRIMIDINES AND THEIR USE IN MEDICAMENTS AGAINST TUMORS 审中-公开
标题翻译：氧化还原酶和抗氧化剂及其在肿瘤药物中的应用
公开(公告)号：WO2002092603A1
公开(公告)日：2002-11-21
申请号：PCT/EP2002/005241
申请日：2002-05-13
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , BOLD, Guido , MANLEY, Paul, William , MARTIN-KOHLER, Andreas , SEQUIN, Urs
发明人： BOLD, Guido , MANLEY, Paul, William , MARTIN-KOHLER, Andreas , SEQUIN, Urs
IPC分类号： C07D498/04
CPC分类号： C07D491/04
摘要： The invention relates to pharmaceutically acceptable compounds of formula I, wherein the radicals have the significances given in the description. Compounds of formula I are useful against tumor diseases.
摘要翻译：本发明涉及药学上可接受的式I化合物，其中基团具有在说明书中给出的含义。式I化合物可用于治疗肿瘤疾病。

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