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11. 发明申请

WO2006128659A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2006128659A2
公开(公告)日：2006-12-07
申请号：PCT/EP2006/005107
申请日：2006-05-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , NIHONYANAGI, Atsuko , TOYAO, Atsushi , IWAKI, Yuki , MASUYA, Keiichi
发明人： NIHONYANAGI, Atsuko , TOYAO, Atsushi , IWAKI, Yuki , MASUYA, Keiichi
CPC分类号： C07D417/14 , C07D403/12
摘要： The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula (I), wherein R1 , R2, R11 , C, E and D are as defined in the specification.
摘要翻译：本发明涉及取代的3,4-或更高级取代的哌嗪化合物，其用于制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 药物制剂或包含所述化合物的产品，和/或包括施用所述化合物的方法，所述化合物的制备方法，以及新型中间体，起始材料和/或其合成的部分步骤。化合物特别是式（I），其中R 1，R 2，R 11，C，E和D如说明书中所定义。

12. 发明申请

WO2006094763A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2006094763A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002083
申请日：2006-03-07
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , MASUYA, Keiichi , YOKOKAWA, Fumiaki , IRIE, Osamu , NIHONYANAGI, Atsuko , TOYAO, Atsushi , EHARA, Takeru , KONISHI, Kazuhide , KANAZAWA, Takanori , SUZUKI, Masaki
发明人： MASUYA, Keiichi , YOKOKAWA, Fumiaki , IRIE, Osamu , NIHONYANAGI, Atsuko , TOYAO, Atsushi , EHARA, Takeru , KONISHI, Kazuhide , KANAZAWA, Takanori , SUZUKI, Masaki
IPC分类号： C07D211/60 , C07D401/12 , C07D413/12 , A61K31/4545 , A61P9/00
CPC分类号： C07D401/12 , C07D211/60 , C07D413/12
摘要： 3,4,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The compounds are of the formula (I), wherein the substitutents are as defined in the specification.
摘要翻译： 3,4,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包含3,4,5-取代的哌啶化合物的药物制剂和/或治疗方法，包括给予3,4,5-取代的哌啶化合物，制备3,4,5-取代哌啶化合物的方法，以及其合成的新型中间体和部分步骤。化合物是式（I），其中取代基如说明书中所定义。

13. 发明申请

WO2005070431A1 PYRAZOLO[1,5-A]PYRIMIDIN-7-YL-AMINE DERIVATIVES FOR USE IN 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吡咯并[1,5-A]吡啶基-7-YL-氨衍生物
公开(公告)号：WO2005070431A1
公开(公告)日：2005-08-04
申请号：PCT/EP2005/000602
申请日：2005-01-21
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , FLOERSHEIMER, Andreas , FURET, Pascal , IMBACH, Patricia , MASUYA, Keiichi , SCHOEPFER, Joseph , MARTINY-BARON, Georg
发明人： BOLD, Guido , FLOERSHEIMER, Andreas , FURET, Pascal , IMBACH, Patricia , MASUYA, Keiichi , SCHOEPFER, Joseph , MARTINY-BARON, Georg
IPC分类号： A61K31/505
CPC分类号： C07D487/04 , A61K31/505
摘要： The invention relates to the use of pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof in the treatment of kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds, and a process for the preparation of the novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds.
摘要翻译：本发明涉及吡唑并[1,5a]嘧啶-7-基胺化合物及其盐在治疗激酶依赖性疾病中的用途以及用于制备用于治疗所述疾病的药物制剂，新颖的吡唑并[1,5a ]嘧啶-7-基胺化合物，以及制备新的吡唑并[1,5a]嘧啶-7-基胺化合物的方法。

14. 发明申请

WO2004069256A1 2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF 审中-公开
标题翻译： 2-氰基吡咯并嘧啶及其药物用途
公开(公告)号：WO2004069256A1
公开(公告)日：2004-08-19
申请号：PCT/EP2004/001081
申请日：2004-02-05
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BUXTON, Francis, Paul , EHARA, Takeru , GANJU, Pamposh , HALLETT, Allan , IRIE, Ozamu , IWASAKI, Atsuko , KANAZAWA, Takanori , MASUYA, Keiichi , NONOMURA, Kazuhiko , SAKAKI, Junichi , SNELL, Christopher, Robert , SONG, Chuanheng , TANABE, Keiko , TENO, Naoki , UMEMURA, Ichiro , YOKOKAWA, Fumiaki
发明人： BUXTON, Francis, Paul , EHARA, Takeru , GANJU, Pamposh , HALLETT, Allan , IRIE, Ozamu , IWASAKI, Atsuko , KANAZAWA, Takanori , MASUYA, Keiichi , NONOMURA, Kazuhiko , SAKAKI, Junichi , SNELL, Christopher, Robert , SONG, Chuanheng , TANABE, Keiko , TENO, Naoki , UMEMURA, Ichiro , YOKOKAWA, Fumiaki
IPC分类号： A61K31/519
CPC分类号： C07D487/04
摘要： The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH 2 ) t -O- or -(CH 2 ) r -S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH 2 ) j - or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH 2 ) f -, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
摘要翻译：本发明涉及式（I）的吡咯并嘧啶，其中Y表示 - （CH 2）t-O - 或 - （CH 2是或2，r是1,2或3，t是1,2或3，或者Y是 - （CH 3）2， - 或-CH = CH-，j为1或2; p是1或2，或Y是 - （CH 2）f -f-，f是1或2，p是1，并且其他基团和符号具有含义如本文所定义; 它们的制备，它们作为药物的用途，含有它们的药物组合物，这种化合物在制备用于治疗神经性疼痛的药物制剂中的用途，以及在动物特别是人类中治疗这种疾病的方法。

15. 发明申请

WO2012176123A1 3 - IMIDAZOLYL- INDOLES FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译： 3 - 用于治疗增殖性疾病的咪唑啉
公开(公告)号：WO2012176123A1
公开(公告)日：2012-12-27
申请号：PCT/IB2012/053095
申请日：2012-06-19
申请人： NOVARTIS AG , FURET, Pascal , KALLEN, Joerg , LORBER, Julien , MASUYA, Keiichi
发明人： FURET, Pascal , KALLEN, Joerg , LORBER, Julien , MASUYA, Keiichi
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D417/04 , C07D471/10 , A61K31/4178 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10
摘要： The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula (I), in which: R 1 , R 2 , R 3 and R 4 are as defined in the Summary of the Invention. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.
摘要翻译：本发明涉及能够分别抑制p53或其变体和MDM2和/或MDM4或其变体之间的相互作用的3-杂环基吲哚基化合物，所述具有式（I）的化合物，其中：R1，R2， R3和R4如发明概述中所定义。由于它们的活性，所述化合物可用于治疗由MDM2和/或MDM4或其变体如炎性或增殖性疾病或保护细胞的活性介导的各种疾病和疾病。

16. 发明申请

WO2007006534A3 PIPERIDINE DERIVATIVES USEFUL IN THE DIAGNOSTIC AND THERAPEUTIC TREATMENT OF DISEASES DEPENDING ON RENIN ACTIVITY 审中-公开
标题翻译：依托仁活性诊断和治疗疾病治疗有效的哌啶衍生物
公开(公告)号：WO2007006534A3
公开(公告)日：2007-04-19
申请号：PCT/EP2006006733
申请日：2006-07-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BREITENSTEIN WERNER , EHRHARDT CLAUS , MAIBAUM JUERGEN KLAUS , OSTERMANN NILS , ZIMMERMANN JUERG , MASUYA KEIICHI , KONISHI KAZUHIDE , YOKOKAWA FUMIAKI , KANAZAWA TAKANORI , JACOBY EDGAR , MARZINZIK ANDREAS , GROSCHE PHILIPP , KAWAKAMI SHIMPEI
发明人： BREITENSTEIN WERNER , EHRHARDT CLAUS , MAIBAUM JUERGEN KLAUS , OSTERMANN NILS , ZIMMERMANN JUERG , MASUYA KEIICHI , KONISHI KAZUHIDE , YOKOKAWA FUMIAKI , KANAZAWA TAKANORI , JACOBY EDGAR , MARZINZIK ANDREAS , GROSCHE PHILIPP , KAWAKAMI SHIMPEI
IPC分类号： C07D211/56 , A61K31/55 , A61P9/00 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D403/14 , C07D211/56 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3, 5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula I wherein R1 , R2, T, R3 and R4 are as defined in the specification.
摘要翻译：本发明涉及3,5-取代的哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包括3,5-取代的哌啶化合物的药物制剂和/或治疗方法，包括给予3,5-取代的哌啶化合物，制备3,5-取代的哌啶化合物的方法和新的中间体和部分其合成步骤。优选的化合物（其也可以盐形式存在）具有式I，其中R 1，R 2，T，R 3和R 4如说明书中所定义。

17. 发明申请

WO2006074924A8 3,4,(5)-SUBSTITUTED TETRAHVDROPYRIDINES 审中-公开
标题翻译： 3,4，（5）-SUBSTITUTED TETRAHVDRRYRIDINES
公开(公告)号：WO2006074924A8
公开(公告)日：2007-04-19
申请号：PCT/EP2006000216
申请日：2006-01-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , MASUYA KEIICHI , IRIE OSAMU , NIHONYANAGI ATSUKO , TOYAO ATSUSHI , KANAZAWA TAKANORI
发明人： MASUYA KEIICHI , IRIE OSAMU , NIHONYANAGI ATSUKO , TOYAO ATSUSHI , KANAZAWA TAKANORI
IPC分类号： C07D211/78 , A61K31/4545 , A61P9/00 , C07D401/10 , C07D401/12 , C07D409/12
CPC分类号： C07D401/12 , C07D211/78 , C07D401/10 , C07D409/12
摘要： Organic Compounds 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)- substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)- substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. The 3,4(,5)- substituted tetrahydropyridine compounds have the formula I wherein the substituents and symbols are as described in the specification.
摘要翻译：有机化合物3,4（，5） - 取代的四氢吡啶化合物，用于诊断和治疗温血动物的化合物，特别是用于治疗依赖于肾素活性的疾病; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包含3,4（，5） - 取代的四氢吡啶化合物的药物制剂和/或包括施用3,4（，5） - 取代的四氢吡啶化合物的方法，以及制备3,4（， 5） - 取代的四氢吡啶化合物，以及其合成的新型中间体和部分步骤。 3,4（，5） - 取代的四氢吡啶化合物具有式I，其中取代基和符号如说明书中所述。

18. 发明申请

WO2006074924A1 3,4,(5)-SUBSTITUTED TETRAHVDROPYRIDINES 审中-公开
标题翻译： 3,4，（5）-SUBSTITUTED TETRAHVDRRYRIDINES
公开(公告)号：WO2006074924A1
公开(公告)日：2006-07-20
申请号：PCT/EP2006/000216
申请日：2006-01-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , MASUYA, Keiichi , IRIE, Osamu , NIHONYANAGI, Atsuko , TOYAO, Atsushi , KANAZAWA, Takanori
发明人： IRIE, Osamu , NIHONYANAGI, Atsuko , TOYAO, Atsushi , KANAZAWA, Takanori
IPC分类号： C07D211/78 , C07D401/12 , C07D401/10 , C07D409/12 , A61K31/4545 , A61P9/00
CPC分类号： C07D401/12 , C07D211/78 , C07D401/10 , C07D409/12
摘要： Organic Compounds 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)- substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)- substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. The 3,4(,5)- substituted tetrahydropyridine compounds have the formula I wherein the substituents and symbols are as described in the specification.
摘要翻译：有机化合物3,4（，5） - 取代的四氢吡啶化合物，用于诊断和治疗温血动物的化合物，特别是用于治疗依赖于肾素活性的疾病; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包含3,4（，5） - 取代的四氢吡啶化合物的药物制剂和/或包括施用3,4（，5） - 取代的四氢吡啶化合物的方法，以及制备3,4（， 5） - 取代的四氢吡啶化合物，以及其合成的新型中间体和部分步骤。 3,4（，5） - 取代的四氢吡啶化合物具有式I，其中取代基和符号如说明书中所述。

19. 发明申请

WO2006018284A1 COMPOUNDS AND COMPOSITIONS USEFUL AS CATHEPSIN S INHIBITORS 审中-公开
标题翻译：化合物和组合物有效用作吸收抑制剂
公开(公告)号：WO2006018284A1
公开(公告)日：2006-02-23
申请号：PCT/EP2005/008896
申请日：2005-08-16
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HART, Terance, William , HALLETT, Allan , YOKOKAWA, Fumiaki , HIRAO, Hajime , EHARA, Takeru , IWASAKI, Atsuko , SAKAKI, Junichi , MASUYA, Keiichi , KISHIDA, Masashi , IRIE, Osamu
发明人： HART, Terance, William , HALLETT, Allan , YOKOKAWA, Fumiaki , HIRAO, Hajime , EHARA, Takeru , IWASAKI, Atsuko , SAKAKI, Junichi , MASUYA, Keiichi , KISHIDA, Masashi , IRIE, Osamu
IPC分类号： C07D239/42
CPC分类号： C07D239/36 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D471/04 , C07D491/10
摘要： The present invention relates to the use of a 2-cyanopyrimidine compound of the formula (I), wherein R 1 , R 2 , R 3 and X are as defined in the specification and in the claims, in free form or in salt form, and , where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S.
摘要翻译：本发明涉及式（I）的2-氰基嘧啶化合物的用途，其中R

20. 发明申请

WO2005051366A3 DIARYL UREA DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES 审中-公开
公开(公告)号：WO2005051366A3
公开(公告)日：2005-06-09
申请号：PCT/EP2004/013459
申请日：2004-11-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , CARAVATTI, Giorgio , FLOERSHEIMER, Andreas , GUAGNANO, Vito , IMBACH, Patricia , MASUYA, Keiichi , ROESEL, Johannes , VAUPEL, Andrea , GARCIA-ECHEVERRIA, Carlos
发明人： BOLD, Guido , CARAVATTI, Giorgio , FLOERSHEIMER, Andreas , GUAGNANO, Vito , IMBACH, Patricia , MASUYA, Keiichi , ROESEL, Johannes , VAUPEL, Andrea , GARCIA-ECHEVERRIA, Carlos
IPC分类号： C07D239/34 , C07D239/46 , C07D403/12 , C07D401/12
摘要： The invention relates to the use of diaryl urea derivatives for the manufacture of pharmaceutical compositions for the treatment of RET dependent disorders, especially RET dependent tumor diseases. The invention further relates to novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives and their use in the treatment of the animal or human body, especially in the treatment of a protein kinase dependent disease, to pharmaceutical compositions comprising such novel N-[4-pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives and to the use of such novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as tumour diseases.

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