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1. 发明申请

WO2005027972A2 COMBINATION OF A VEGF RECEPTOR INHIBITOR WITH A CHEMOTHERAPEUTIC AGENT 审中-公开
标题翻译： VEGF受体抑制剂与化学治疗剂的组合
公开(公告)号：WO2005027972A2
公开(公告)日：2005-03-31
申请号：PCT/EP2004010686
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： A61K31/502 , A61K45/06
CPC分类号： A61K45/06 , A61K31/502 , A61K2300/00
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) a VEGF inhibitor compound; and (b) one or more chemotherapeutic agents selected from the group consisting of: i. an aromatase inhibitor; ii. an anti-estrogen, an anti-androgen (especially in the case of prostate cancer) or a gonadorelin agonist; iii. a topoisomerase I inhibitor or a topoisomerase II inhibitor; iv. a microtubule active agent, an alkylating agent, an anti-neoplastic antimetabolite or a platin compound; v. a compound targeting/decreasing a protein or lipid kinase activity or a protein or lipid phosphatase activity, a further anti-angiogenic compound or a compound which induces cell differentiation processes; vi. a bradykinin 1 receptor or an angiotensin II antagonist; vii. a cyclooxygenase inhibitor, a bisphosphonate, a heparanase inhibitor (prevents heparan sulphate degradation), e.g., PI-88, a biological response modifier, preferably a lymphokine or interferons, e.g., interferon gamma, an ubiquitination inhibitor, or an inhibitor which blocks anti-apoptotic pathways; viii. an inhibitor of Ras oncogenic isoforms or a farnesyl transferase inhibitor; ix. a telomerase inhibitor, e.g., telomestatin; x. a protease inhibitor, a matrix metalloproteinase inhibitor, a methionine aminopeptidase inhibitor, e.g., bengamide or a derivative thereof, or a proteasome inhibitor, e.g., PS-341; xi. agents used in the treatment of hematologic malignancies or FMS-like tyrosine kinase inhibitors; xii. an HSP90 inhibitors; xiii. HDAC inhibitors; xiv. mTOR inhibitors; xv. somatostatin receptor antagonists; xvi. integrin antagonists; xvii. anti-leukemic compounds; xviii. tumor cell damaging approaches such as ionizing radiation; xix. EDG binders; xx. anthranilic acid amide class of kinase inhibitors; xxi. ribonucleotide reductase inhibitors; xxii. S-adenosylmethionine decarboxylase inhibitors; xxiii. antibodies against VEGF or VEGFR; xxiv. photodynamic therapy; xxv. angiostatic steroids; xxvi. implants containing corticosteroids; xxvii. AT1 receptor antagonists; and xxviii. ACE inhibitors.
摘要翻译：本发明涉及用于治疗患有与持续性血管发生相关的增殖性疾病或疾病的患者的组合疗法。治疗患者：（a）VEGF抑制剂化合物; 和（b）一种或多种选自以下的化疗剂：i。芳香酶抑制剂; II。抗雌激素，抗雄激素（特别是在前列腺癌的情况下）或促性腺激素激动剂; III。拓扑异构酶I抑制剂或拓扑异构酶II抑制剂; IV。微管活性剂，烷化剂，抗肿瘤抗代谢药或铂类化合物; v。靶向/降低蛋白质或脂质激酶活性或蛋白质或脂质磷酸酶活性的化合物，进一步的抗血管生成化合物或诱导细胞分化过程的化合物; 六。缓激肽1受体或血管紧张素II拮抗剂; 七。环氧合酶抑制剂，双膦酸盐，乙酰肝素酶抑制剂（防止硫酸乙酰肝素降解），例如PI-88，生物反应调节剂，优选淋巴因子或干扰素，例如干扰素γ，泛素抑制剂或阻断抗 - 凋亡途径; 八。 Ras致癌亚型抑制剂或法呢基转移酶抑制剂; 九。端粒酶抑制剂，例如端粒抑素; X。蛋白酶抑制剂，基质金属蛋白酶抑制剂，甲硫氨酸氨基肽酶抑制剂，例如孟加拉胺或其衍生物，或蛋白酶体抑制剂，例如PS-341; 十一。用于治疗血液恶性肿瘤或FMS样酪氨酸激酶抑制剂的药剂; 十二。 HSP90抑制剂; 十三。 HDAC抑制剂; 十四。 mTOR抑制剂; 十五。生长抑素受体拮抗剂; 十六。整合素拮抗剂; 十七。抗白血病化合物; 十八。肿瘤细胞破坏性方法如电离辐射; 十九。 EDG粘合剂 XX。邻氨基苯甲酸酰胺类激酶抑制剂; 二十一。核糖核苷酸还原酶抑制剂; 二十二。 S-腺苷甲硫氨酸脱羧酶抑制剂; 二十三。针对VEGF或VEGFR的抗体; 二十四。光动力疗法; 二十五。血管抑制类固醇; 二十六。含有皮质类固醇的植入物; 二十七。 AT1受体拮抗剂; 和xxviii。 ACE抑制剂。

2. 发明申请

WO2005027973A3 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组合
公开(公告)号：WO2005027973A3
公开(公告)日：2005-09-09
申请号：PCT/EP2004010701
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 , A61P3/00 , A61P9/00 , A61P27/00 , A61P35/00
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炎症细胞，冠状动脉疾病，高血压，肾脏疾病，糖尿病或眼部疾病和病症的细胞增殖和浸润特征的疾病的组合疗法。患者用以下组合治疗：（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-IR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。整合素拮抗剂; 十四。内源性抗血管生成分子; 和xv。 PEDF和类似物。

3. 发明申请

WO0027819A3 ANTRHRANILIC ACID AMIDES AND THE USE THEREOF AS MEDICAMENTS 审中-公开
标题翻译：蒽环酰胺及其作为药物的用途
公开(公告)号：WO0027819A3
公开(公告)日：2000-08-17
申请号：PCT/EP9908478
申请日：1999-11-09
申请人： SCHERING AG , NOVARTIS AG , HUTH ANDREAS , SEIDELMANN DIETER , THIERAUCH KARL HEINZ , BOLD GUIDO , MANLEY PAUL WILLIAM , FURET PASCAL , WOOD JEANETTE MARJORIE , MESTAN JUERGEN , BRUEGGEN JOSE , FERRARI STEFANO , KRUEGER MARTIN , OTTOW ECKHARD , MENRAD ANDREAS , SCHIRNER MICHAEL
发明人： HUTH ANDREAS , SEIDELMANN DIETER , THIERAUCH KARL-HEINZ , BOLD GUIDO , MANLEY PAUL WILLIAM , FURET PASCAL , WOOD JEANETTE MARJORIE , MESTAN JUERGEN , BRUEGGEN JOSE , FERRARI STEFANO , KRUEGER MARTIN , OTTOW ECKHARD , MENRAD ANDREAS , SCHIRNER MICHAEL
IPC分类号： C07D213/36 , A61K31/166 , A61K31/403 , A61K31/404 , A61K31/4409 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/517 , A61K31/536 , A61P1/16 , A61P3/10 , A61P9/10 , A61P9/14 , A61P13/12 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/06 , A61P35/00 , A61P43/00 , C07C237/30 , C07C237/32 , C07D209/04 , C07D213/40 , C07D213/75 , C07D265/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D213/38 , A61P17/00 , C07D213/61
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：描述了邻氨基苯甲酸酰胺及其作为药物用于治疗由持续血管生成引起的疾病及其用于制备邻氨基苯甲酰胺的中间体的用途。

4. 发明申请

WO2004005281A8 INHIBITORS OF TYROSINE KINASES 审中-公开
标题翻译：酪氨酸激酶抑制剂
公开(公告)号：WO2004005281A8
公开(公告)日：2004-05-06
申请号：PCT/EP0307198
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： C07D401/04 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/14 , C07D405/14 , C07D417/14
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具有在本发明说明书中阐述和解释的含义，涉及制备这些化合物的方法，含有其的药物组合物，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抑制蛋白激酶活性，特别是肿瘤性疾病，特别是白血病有响应的疾病，以及用于治疗此类疾病的方法。

5. 发明申请

WO2005075454A3 SALT FORMS OF 4-(4-METHYLPIPERAZIN-1-YLMETHYL)-n-[4-METHYL-3-(4-PYRIDIN-3-YL)PYRIMIDIN-2-YLAMINO)PHENYL]-BENZAMIDE 审中-公开
标题翻译： 4-（4-甲基哌嗪-1-基）甲基] - [4-甲基-3-（4-吡啶-3-基）嘧啶-2-基]氨基]苯基] - 苯甲酰胺的盐形式
公开(公告)号：WO2005075454A3
公开(公告)日：2006-07-27
申请号：PCT/EP2005001077
申请日：2005-02-03
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BUERGER HANS MICHAEL , MANLEY PAUL WILLIAM , MUTZ MICHAEL
发明人： BUERGER HANS MICHAEL , MANLEY PAUL WILLIAM , MUTZ MICHAEL
IPC分类号： C07D401/04 , A61K31/505 , A61P35/02
CPC分类号： C07D401/04
摘要： The present invention relates to acid addition salts of 4-[4-methyl-1-piperazinylmethyl]-N-[4-methyl-3-[[4-¢3-pyridinyl-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(-) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate sat, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.
摘要翻译：本发明涉及4- [4-甲基-1-哌嗪基甲基] -N- [4-甲基-3 - [[4-3,3-吡啶基-2-嘧啶基]氨基]苯基] - 苯甲酰胺的酸加成盐，其选自酒石酸盐，例如（D）（ - ）酒石酸盐或（L）（+）酒石酸盐，盐酸盐，柠檬酸盐，苹果酸盐，富马酸盐，琥珀酸盐，苯甲酸盐，苯磺酸盐，双羟萘酸盐，甲酸盐，丙二酸盐，1,5-萘二磺酸盐，水杨酸盐，环己烷氨基磺酸盐，乳酸盐，扁桃酸盐，戊二酸戊酯盐，己二酸盐，方酸盐，香草酸盐，草酰乙酸盐，抗坏血酸盐和硫酸盐。

6. 发明专利

PT1572686E DERIVADOS DE AMIDA DO ÁCIDO ANTRANÍLICO E SUAS UTILIZAÇÕES FARMACÊUTICAS 未知
公开(公告)号：PT1572686E
公开(公告)日：2009-07-14
申请号：PT03785795
申请日：2003-12-11
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： BOLD GUIDO , MANLEY PAUL WILLIAM , FURET PASCAL
IPC分类号： C07D409/04 , A61K31/44 , A61K31/4412 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61P35/00 , C07D213/38 , C07D213/50 , C07D213/61 , C07D213/64 , C07D213/74 , C07D401/12 , C07D405/04 , C07D417/04

7. 发明专利

DE60325209D1 未知
公开(公告)号：DE60325209D1
公开(公告)日：2009-01-22
申请号：DE60325209
申请日：2003-05-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： FLOERSHEIMER ANDREAS , FURET PASCAL , MANLEY PAUL WILLIAM , BOLD GUIDO , BOSS EUGEN , GUAGNANO VITO , VAUPEL ANDREA
IPC分类号： C07D213/68 , A61K31/33 , A61K31/395 , A61K31/4409 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P9/10 , A61P11/06 , A61P13/08 , A61P15/08 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P43/00 , C07D213/36 , C07D213/38 , C07D213/40 , C07D213/63 , C07D213/64 , C07D213/69 , C07D213/81 , C07D213/84 , C07D213/89 , C07D239/26 , C07D239/30 , C07D239/34 , C07D239/40 , 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.

8. 发明专利

PT1322634E DERIVADOS DE N-FENIL-2-PIRIMIDINA-AMINA 未知
公开(公告)号：PT1322634E
公开(公告)日：2010-02-22
申请号：PT01984640
申请日：2001-09-11
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： CARAVATTI GIORGIO , MANLEY PAUL WILLIAM , BREITENSTEIN WERNER , BUERGER HANS MICHAEL , ZIMMERMANN JUERG , CUDD MARGARET AMELIA
IPC分类号： C07D401/04 , A61K31/506 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D401/14

9. 发明专利

PT1259487E DERIVADOS DE 2-AMINO-NICOTINAMIDA E AS SUAS UTILIZAÇÕES COMO INIBIDORES DE RECEPTORES VEGF DE TIROSINA QUINASE 未知
公开(公告)号：PT1259487E
公开(公告)日：2010-03-26
申请号：PT01946854
申请日：2001-01-25
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： BOLD GUIDO , MANLEY PAUL WILLIAM
IPC分类号： C07D213/82 , A61K31/44 , A61K31/444 , A61K31/445 , A61K31/455 , A61K31/4725 , A61P3/10 , A61P5/30 , A61P17/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07D213/89 , C07D401/14 , C07D417/14

10. 发明专利

PT1441737E DERIVADOS DE ESTRUTURA COMO INIBIDORES DA ACTIVIDADE DO RECEPTOR DE TIROSINA CINASE FLT3 未知
公开(公告)号：PT1441737E
公开(公告)日：2006-12-29
申请号：PT02791654
申请日：2002-10-29
申请人： DANA FARBER CANCER INST INC , NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： GRIFFIN JAMES DOUGLAS , MANLEY PAUL WILLIAM
IPC分类号： A61K31/535 , C07D498/22 , A61K31/155 , A61K31/407 , A61K31/55 , A61K31/553 , A61P19/08 , A61P35/02 , A61P43/00 , C07D487/04 , C07D487/14 , C07D519/00

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