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1. 发明申请

WO2005051366A2 DIARYL UREA DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES 审中-公开
标题翻译：治疗蛋白激酶依赖性疾病的二尿嘧啶衍生物
公开(公告)号：WO2005051366A2
公开(公告)日：2005-06-09
申请号：PCT/EP2004013459
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 , C07D401/12 , C07D403/12 , A61K31/00
CPC分类号： C04B35/632 , C07D239/34 , C07D239/47 , C07D401/12 , C07D403/12
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.
摘要翻译：本发明涉及二芳基脲衍生物在制备用于治疗RET依赖性疾病，特别是RET依赖性肿瘤疾病的药物组合物中的用途。本发明还涉及新的N- [4-（嘧啶-4-基氧基） - 苯基] -N'-苯基 - 脲衍生物及其在治疗动物或人体中的用途，特别是在治疗蛋白激酶对于包含这样的新的N- [4-嘧啶-4-基氧基） - 苯基] -N'-苯基 - 脲衍生物的药物组合物和使用这种新的N- [4-（嘧啶-4-基氧基） - 苯基] -N'-苯基 - 脲衍生物，用于制备用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病如肿瘤疾病的药物组合物。

2. 发明申请

WO2006059234A3 BICYCLIC AMIDES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的双环酰胺
公开(公告)号：WO2006059234A3
公开(公告)日：2006-07-20
申请号：PCT/IB2005004030
申请日：2005-09-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD GUIDO , CAPRARO HANS-GEORG , CARAVATTI GIORGIO , FLOERSHEIMER ANDREAS , FURET PASCAL , MANLEY PAUL W , VAUPEL ANDREA , PISSOT SOLDERMANN CAROLE , GESSIER FRANCOIS , SCHNELL CHRISTIAN , LITTLEWOOD-EVANS AMANDA JANE , KAPA PRASAD KOTESWARA , BAJWA JOGINDER S , JIANG XINGLONG
发明人： BOLD GUIDO , CAPRARO HANS-GEORG , CARAVATTI GIORGIO , FLOERSHEIMER ANDREAS , FURET PASCAL , MANLEY PAUL W , VAUPEL ANDREA , PISSOT SOLDERMANN CAROLE , GESSIER FRANCOIS , SCHNELL CHRISTIAN , LITTLEWOOD-EVANS AMANDA JANE , KAPA PRASAD KOTESWARA , BAJWA JOGINDER S , JIANG XINGLONG
IPC分类号： C07D403/12 , A61K31/505 , C07D239/46 , C07D413/12
CPC分类号： C07D239/47 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
摘要翻译：本发明涉及式（I）化合物及其在治疗动物或人体中的用途，涉及包含式I化合物的药物组合物，以及涉及式I化合物在制备使用的药物组合物中的用途用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，例如特别是肿瘤疾病。

3. 发明申请

WO2005077951A3 7H-PYRROLOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译： 7H-吡咯烷酮衍生物
公开(公告)号：WO2005077951A3
公开(公告)日：2006-03-02
申请号：PCT/EP2005001635
申请日：2005-02-17
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CARAVATTI GIORGIO , VAUPEL ANDREA
发明人： CARAVATTI GIORGIO , VAUPEL ANDREA
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula (I), wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives - alone or in combination with one or more other pharmaceutically active compounds - for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.
摘要翻译：本发明涉及式（I）的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物和使用这样的衍生物 - 单独或与一种或多种其它药学活性化合物组合，用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。

4. 发明申请

WO2008119741A3 3-IMIDAZOLYL-INDOLES FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于治疗增殖性疾病的3-咪唑啉吲哚
公开(公告)号：WO2008119741A3
公开(公告)日：2008-12-04
申请号：PCT/EP2008053667
申请日：2008-03-27
申请人： NOVARTIS AG , BOETTCHER ANDREAS , BUSCHMANN NICOLE , FURET PASCAL , GROELL JEAN-MARC , KALLEN JOERG , HERGOVICH LISZTWAN JOANNA , MASUYA KEIICHI , MAYR LORENZ , VAUPEL ANDREA
发明人： BOETTCHER ANDREAS , BUSCHMANN NICOLE , FURET PASCAL , GROELL JEAN-MARC , KALLEN JOERG , HERGOVICH LISZTWAN JOANNA , MASUYA KEIICHI , MAYR LORENZ , VAUPEL ANDREA
IPC分类号： C07D403/04 , A61K31/4164 , A61P35/00
CPC分类号： C07D403/04
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) wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. 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，R4 ，RA，Y和Y如说明书中所定义。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。

5. 发明申请

WO2006072589A3 DISUBSTITUTED UREAS AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的消除性尿路炎
公开(公告)号：WO2006072589A3
公开(公告)日：2006-10-12
申请号：PCT/EP2006000098
申请日：2006-01-09
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FURET PASCAL , MARTINY-BARON GEORG , MCCARTHY CLIVE , RASETTI VITTORIO , VAUPEL ANDREA
发明人： FURET PASCAL , MARTINY-BARON GEORG , MCCARTHY CLIVE , RASETTI VITTORIO , VAUPEL ANDREA
IPC分类号： C07D403/12 , A61K31/496 , A61P35/00
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14
摘要： The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.
摘要翻译：本发明涉及式（I）化合物，其作为激酶抑制剂的用途，包含所述化合物的新药物制剂，用于诊断或治疗温血动物，特别是人的所述化合物，其用于治疗疾病或用于制造可用于治疗对激酶活性调节作出反应的疾病的药物制剂，包括将所述化合物施用于温血动物，特别是人的治疗方法，以及所述化合物的制备方法。

6. 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.

7. 发明专利

ES2469644T3 Derivados de tiazol y pirazol como inhibidores de cinasa Flt-3 未知
公开(公告)号：ES2469644T3
公开(公告)日：2014-06-18
申请号：ES04818403
申请日：2004-11-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： BOLD GUIDO , FLOERSHEIMER ANDREAS , FURET PASCAL , GUAGNANO VITO , MASUYA KEIICHI , VAUPEL ANDREA , SCHOEPFER JOSEPH
IPC分类号： C07D277/42 , A61K31/4155 , A61K31/427 , C07D231/38 , C07D409/04 , C07D417/04 , C07D417/10
摘要： Compuesto seleccionado del grupo que consiste en: (5-fenil-tiazol-2-il)-[4-(2-pirrolidin-1-il-etoxi)-fenil]-amina; (3-dimetilaminometil-fenil)-(5-fenil-tiazol-2-il)-amina; [5-(4-metoxi-fenil)-tiazol-2-il]-[4-(2-pirrolidin-1-il-etoxi)- fenil]-amina; (4-metoxi-fenil)-[5-(4-metoxi-fenil)-tiazol-2-il]-amina; [5-(4-metoxi-fenil)-tiazol-2-il]-[4-(4-metil-piperazin-1-il)-fenil]-amina; [4-(2-dimetilamino-etoxi)-fenil]-[5-(4-metoxi-fenil)-tiazol-2-il]-amina; 4-{2-[4-(2-pirrolidin-1-il-etoxi)-fenilamino]-tiazol-5-il}-fenol; {5-[4-(3-dimetilamino-propoxi)-fenil]-tiazol-2-il}-fenil-amina; 4-[5-(3-metoxi-fenil)-tiazol-2-ilamino]-fenol; 4-[5-(3-metoxi-fenil)-tiazol-2-il]-[4-(2-pirrolidin-1-il-etoxi)-fenil]-amina; (4-metoxi-fenil)-(5-tiofen-3-il-tiazol-2-il)-amina; 4-(5-tiofen-3-il-tiazol-2-il-amino)-fenol; [4-(2-dimetilamino-etoxi)-fenil]-(5-tiofen-3-il-tiazol-2-il)-amina; [4-(3-dimetilamino-propoxi)-fenil]-(5-tiofen-3-il-tiazol-2-il)-amina; [4-(2-pirrolidin-1-il-etoxi)-fenil]-(5-tiofen-3-il-tiazol-2-il)-amina; [4-(2-piperidin-1-il-etoxi)-fenil]-(5-tiofen-3-il-tiazol-2-il)-amina; [4-(2-di-isopropilamino-etoxi)-fenil]-(5-tiofen-3-il-tiazol-2-il)-amina; [4-(2-morfolin-4-il-etoxi)-fenil]-(5-tiofen-3-il-tiazol-2-il)-amina; (5-fenil-1H-pirazol-3-il)-[4-(2-pirrolidin-1-il-etoxi)-fenil]-amina; [4-(2-pirrolidin-1-il-etoxi)-fenil]-(5-tiofen-3-il-1H-pirazol-3-il)-amina; [4-(2-dimetilamino-etoxi)-fenil]-(5-tiofen-3-il-1H-pirazol-3-il)-amina; [4-(3-dimetilamino-propoxi)-fenil]-(5-tiofen-3-il-1H-pirazol-3-il)-amina; [4-(2-dietilamino-etoxi)-fenil]-(5-tiofen-3-il-1H-pirazol-3-il)-amina; [5-(2-cloro-fenil)-1H-pirazol-3-il]-fenil-amina; [5-(2-cloro-fenil)-1H-pirazol-3-il]-[4-(4-metil-piperazin-1-il)-fenil]-amina; y sales farmacéuticamente aceptables de estos compuestos.

8. 发明申请

WO0125210A3 SUBSTITUTED 2-THIO-3,5-DICYANO-4-ARYL-6-AMINOPYRIDINES AND THE USE THEREOF AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译：取代的2-硫代-3,5-二氰基-4-芳基-6-氨基吡啶及其作为腺苷受体配体
公开(公告)号：WO0125210A3
公开(公告)日：2001-10-11
申请号：PCT/EP0009153
申请日：2000-09-19
申请人： BAYER AG , ROSENTRETER ULRICH , HENNING ROLF , BAUSER MARCUS , KRAEMER THOMAS , VAUPEL ANDREA , HUEBSCH WALTER , DEMBOWSKY KLAUS , SALCHER SCHRAUFSTAETTER OLGA , STASCH JOHANNES PETER , KRAHN THOMAS , PERZBORN ELISABETH
发明人： ROSENTRETER ULRICH , HENNING ROLF , BAUSER MARCUS , KRAEMER THOMAS , VAUPEL ANDREA , HUEBSCH WALTER , DEMBOWSKY KLAUS , SALCHER-SCHRAUFSTAETTER OLGA , STASCH JOHANNES-PETER , KRAHN THOMAS , PERZBORN ELISABETH
IPC分类号： A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P1/16 , A61P3/10 , A61P9/10 , A61P11/00 , A61P13/00 , A61P15/00 , A61P25/00 , A61P25/04 , A61P29/00 , A61P35/00 , A61P43/00 , C07D213/85 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/4427
CPC分类号： C07D401/12 , C07D213/85 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to compounds of general formula (I), a method for the production thereof and the use thereof as pharmacologically effective substances for a broad medical indication spectrum. Furthermore, selective adenosine receptor ligands, preferably selective adenosine A1-, adenosine A2a- and/or adenosine A2b-receptor ligands are provided for the prophylaxis and/or the treatment of diseases, especially cardiovascular diseases, diseases of the urogenital region, diseases of the respiratory tract, inflammatory and neuroinflammatory diseases, diabetes, especially pancreatic diabetes, neurodegenerative diseases, pain states, cancer as well as liver fibrosis and liver cirrhosis.
摘要翻译：有通式（I）的所述化合物，它们的制备方法以及它们作为药理学活性物质为广泛医学适应症频谱使用的方法。此外，选择性腺苷受体配体，优选选择性腺苷A1-，腺苷A2a和/或腺苷A2B受体的配体提供了用于预防和/或治疗的疾病，特别是心血管疾病; 泌尿生殖区的疾病; 呼吸道疾病; 炎性和神经炎性疾病; 糖尿病，尤其是糖尿病; 神经变性疾病; 疼痛; 癌症; 和肝纤维化和肝硬化。

9. 发明专利

ES2362907T3 FENILACETAMINAS ADECUADAS COMO INHIBIDORES DE QUINASA PROTEINICA. 未知
公开(公告)号：ES2362907T3
公开(公告)日：2011-07-14
申请号：ES06724286
申请日：2006-04-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： BOLD GUIDO , FURET PASCAL , GUAGNANO VITO , MCCARTHY CLIVE , VAUPEL ANDREA
IPC分类号： A61K31/4184 , C07D471/04 , A61K31/4188 , A61P35/00 , A61P35/02 , C07D235/04 , C07D235/06 , C07D401/12 , C07D403/12 , C07D473/00
摘要： Un compuesto de la formula I, donde cada uno de R1 y R2, independientemente uno de otro, se selecciona del grupo consistente de hidrogeno, halo y C1-C7- alquilo; R3 esta ausente si Z es nitrogeno o, si Z es C (carbono), es hidrogeno, arilo no sustituido o sustituido o heterociclilo no sustituido o sustituido; X es N (nitrogeno) o CH (carbono sustituido con hidrogeno), Y es CH o N, Z es C o N, y Q es una unidad estructural de la formula (A) donde R4 es hidrogeno, halo, hidrogeno no sustituido o sustituido, arilo no sustituido o sustituido, heterociclilo no sustituido o sustituido enlazado a traves de un atomo de anillo diferente a nitrogeno, cicloalquilo no sustituido o sustituido, alquilo no sustituido o sustituido, alquenilo no sustituido o sustituido o alquinilo no sustituido o sustituido; R5 es hidrogeno, alquilo no sustituido o sustituido, hidrogeno no sustituido o sustituido, arilo no sustituido o sustituido o heterociclilo no sustituido o sustituido; y R6 es hidrogeno, cicloalquilo no sustituido o sustituido o alquilo no sustituido o (preferiblemente) sustituido; o una unidad estructural de la formula (B) donde R7 es arilo no sustituido o sustituido o heterociclilo no sustituido o sustituido y R8 es alquilo o cicloalquilo; donde el asterisco * en las formulas (A) y (B) marca el enlace a traves del cual la unidad estructural esta enlazada al NH del grupo amida en la formula I; y (a) cada uno de R9 y R10, independientemente del otro, se selecciona del grupo consistente de hidrogeno, hidroxilo y C1-C7-alquilo; o (b) R9 y R10 representan juntos oxo; o R1 y R9 forman juntos un grupo -C(O)-CH2- o -CH2-CH2-, R2 se selecciona del grupo consistente de hidrogeno, halo y C1-C7-alquilo, y R10 representa hidrogeno; o una sal farmaceuticamente aceptable de los mismos.

10. 发明专利

PT1718651E DERIVADOS 7H-PIRROLOPIRIMIDINA 未知
公开(公告)号：PT1718651E
公开(公告)日：2009-07-17
申请号：PT05715376
申请日：2005-02-17
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： CARAVATTI GIORGIO , VAUPEL ANDREA
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00

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