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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

WO03014102B1 CERTAIN SUBSTITUTED POLYKETIDES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN TREATING TUMORS 审中-公开
标题翻译：某些取代的多糖，含有它们的药物组合物及其在治疗肿瘤中的用途
公开(公告)号：WO03014102B1
公开(公告)日：2003-11-27
申请号：PCT/EP0208734
申请日：2002-08-05
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , KINDER FREDERICK RAY JR , BAIR KENNETH WALTER , RAMSEY TIMOTHY MICHAEL , SABIO MICHAEL LLOYD
发明人： KINDER FREDERICK RAY JR , BAIR KENNETH WALTER , RAMSEY TIMOTHY MICHAEL , SABIO MICHAEL LLOYD
IPC分类号： A61K31/164 , A61K31/27 , A61K31/366 , A61P35/00 , A61P35/02 , C07C269/02 , C07C269/06 , C07C271/10 , C07D309/30 , C07C271/12
CPC分类号： C07D309/30
摘要： The present invention relates to certain substituted polyketides of formula (I), wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
摘要翻译：本发明涉及某些取代的式（I）的聚酮化合物，其中A，B，C，D，E，F和m如本文所定义，含有所述化合物的药物组合物以及所述化合物在治疗肿瘤中的用途。

3. 发明申请

WO2003080567A2 INTERMEDIATES FOR THE SYNTHESIS OF DISCODERMOLIDE AND RELATED ANALOGUES AND METHODS FOR THEIR PREPARATION 审中-公开
标题翻译：氯吡格雷合成及相关模拟物的中间体及其制备方法
公开(公告)号：WO2003080567A2
公开(公告)日：2003-10-02
申请号：PCT/EP2003/003152
申请日：2003-03-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CHEN, Weichun , FRANCAVILLA, Charles , JAGOE, Christopher, Turchik , KINDER, Frederick, Ray, Jr.
发明人： CHEN, Weichun , FRANCAVILLA, Charles , JAGOE, Christopher, Turchik , KINDER, Frederick, Ray, Jr.
IPC分类号： C07C271/22
CPC分类号： C07F7/1892 , C07C29/10 , C07C33/02 , C07C45/29 , C07C47/21 , C07F7/1852 , C07F7/188
摘要： The invention relates to processes for preparing intermediates utilized in the synthesis of discodermolide and analogues thereof, to novel compounds utilized in the processes and to novel compounds prepared by the processes.
摘要翻译：本发明涉及制备用于合成除草剂及其类似物的中间体的方法，用于该方法中使用的新化合物和通过该方法制备的新型化合物。

4. 发明申请

WO2003014102A1 CERTAIN SUBSTITUTED POLYKETIDES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN TREATING TUMORS 审中-公开
标题翻译：某些取代的聚酮化合物，含有它们的药物组合物及其用于治疗肿瘤的用途
公开(公告)号：WO2003014102A1
公开(公告)日：2003-02-20
申请号：PCT/EP2002/008734
申请日：2002-08-05
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , KINDER, Frederick, Ray, Jr. , BAIR, Kenneth, Walter , RAMSEY, Timothy, Michael , SABIO, Michael, Lloyd
发明人： KINDER, Frederick, Ray, Jr. , BAIR, Kenneth, Walter , RAMSEY, Timothy, Michael , SABIO, Michael, Lloyd
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： The present invention relates to certain substituted polyketides of formula (I), wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
摘要翻译：本发明涉及式（I）的某些取代的聚酮化合物，其中A，B，C，D，E，F和m如本文所定义，含有所述化合物的药物组合物和用途所述化合物治疗肿瘤。

5. 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。

6. 发明申请

WO2003080567A3 INTERMEDIATES FOR THE SYNTHESIS OF DISCODERMOLIDE AND RELATED ANALOGUES AND METHODS FOR THEIR PREPARATION 审中-公开
公开(公告)号：WO2003080567A3
公开(公告)日：2003-10-02
申请号：PCT/EP2003/003152
申请日：2003-03-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CHEN, Weichun , FRANCAVILLA, Charles , JAGOE, Christopher, Turchik , KINDER, Frederick, Ray, Jr.
发明人： CHEN, Weichun , FRANCAVILLA, Charles , JAGOE, Christopher, Turchik , KINDER, Frederick, Ray, Jr.
IPC分类号： C07C271/22
摘要： The invention relates to processes for preparing intermediates utilized in the synthesis of discodermolide and analogues thereof, to novel compounds utilized in the processes and to novel compounds prepared by the processes.

7. 发明申请

WO02098843A3 CERTAIN SALTS OF DISCODERMOLIDE ACID, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN TREATING TUMORS 审中-公开
标题翻译：含有酪氨酸的某些盐，包含它们的药物组合物及其在治疗肿瘤中的用途
公开(公告)号：WO02098843A3
公开(公告)日：2003-05-01
申请号：PCT/EP0204218
申请日：2002-04-16
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , KINDER FREDERICK RAY JR , KAPA PRASAD KOTESWARA , LOESER ERIC M
发明人： KINDER FREDERICK RAY JR , KAPA PRASAD KOTESWARA , LOESER ERIC M
IPC分类号： C07D295/00 , A61K31/27 , A61P35/00 , A61P35/02 , C07C269/06 , C07C271/12
CPC分类号： C07C271/12 , C07B2200/07
摘要： The present invention relates to discodermolidate acid salts of formula (I) where R is as defined herein, pharmaceutical compositions containing said salts, the use of said salts alone or in combination with other therapeutic agents in treating tumors and to a process for making said salts.
摘要翻译：本发明涉及其中R如本文所定义的式（I）的discodermolidate酸盐，含有所述盐的药物组合物，单独使用所述盐或与其它治疗剂组合治疗肿瘤的用途及其制备方法。

8. 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。

9. 发明申请

WO2005014574A1 SUBSTITUTED LACTAMS AND THEIR USE AS ANTI-CANCER AGENTS 审中-公开
标题翻译：替代LACTAMS及其作为抗癌剂的用途
公开(公告)号：WO2005014574A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008284
申请日：2004-07-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BAIR, Kenneth, Walter , KINDER, Frederick, Ray, Jr. , VERSACE, Richard, William
发明人： BAIR, Kenneth, Walter , KINDER, Frederick, Ray, Jr. , VERSACE, Richard, William
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D223/12
摘要： This invention relates to certain substituted lactam compounds of the formula (I), particularly caprolactam compounds, which are useful for the treatment of cancer.
摘要翻译：本发明涉及某些取代的式（I）的内酰胺化合物，特别是可用于治疗癌症的己内酰胺化合物。

10. 发明申请

WO2002098843A2 CERTAIN SALTS OF DISCODERMOLIDE ACID, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN TREATING TUMORS 审中-公开
标题翻译：含有酪氨酸的某些盐，包含它们的药物组合物及其在治疗肿瘤中的用途
公开(公告)号：WO2002098843A2
公开(公告)日：2002-12-12
申请号：PCT/EP2002/004218
申请日：2002-04-16
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , KINDER, Frederick, Ray, Jr. , KAPA, Prasad, Koteswara , LOESER, Eric, M.
发明人： KINDER, Frederick, Ray, Jr. , KAPA, Prasad, Koteswara , LOESER, Eric, M.
IPC分类号： C07C271/12
CPC分类号： C07C271/12 , C07B2200/07
摘要： The present invention relates to discodermolidate acid salts of formula (I) where R is as defined herein, pharmaceutical compositions containing said salts, the use of said salts alone or in combination with other therapeutic agents in treating tumors and to a process for making said salts.
摘要翻译：本发明涉及其中R如本文所定义的式（I）的discodermolidate酸盐，含有所述盐的药物组合物，单独使用所述盐或与其它治疗剂组合治疗肿瘤的用途及其制备方法。

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