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1. 发明申请

WO2010084050A3 QUINAZOLINONE DERIVATIVES USEFUL AS VANILLOID ANTAGONISTS 审中-公开
标题翻译：喹诺酮类衍生物有助于VANILLOID ANTAGONISTS
公开(公告)号：WO2010084050A3
公开(公告)日：2011-01-27
申请号：PCT/EP2010050243
申请日：2010-01-12
申请人： NOVARTIS AG , CHEN WEICHUN , KIM HONG-YONG , LIANG JESSICA , MUTZ MICHAEL , PRASHAD MAHAVIR , TOWLER CHRISTOPHER , WU RUOQIU
发明人： CHEN WEICHUN , KIM HONG-YONG , LIANG JESSICA , MUTZ MICHAEL , PRASHAD MAHAVIR , TOWLER CHRISTOPHER , WU RUOQIU
IPC分类号： A61P11/06 , A61K31/505 , C07D239/88
CPC分类号： C07D239/91 , A61K31/517
摘要： There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin- 3-yl)-benzonitrile having structural formula I(B) and to a method of preparing it. There is further a process or method for the manufacture of a pharmaceutically active quinazolinone compounds of the formula (I), wherein the symbols have the meanings given in the description, said process comprising reacting a compound of the formula (II), wherein R4* is R1*-C(=O)- wherein R1* is independently selected from the group of meanings of R1 as defined for a compound of the formula (I) so that R1* and R1 are identical to or different from each other, or R4*is especially H, and R1 and R3, R5 and R6 are as defined for a compound of the formula (I), or a salt thereof, under simultaneous or sequential condensation and cyclisation conditions with an aniline compound of the formula (III), wherein R2 and m are as defined for a compound of the formula (I). Further reactions and related embodiments are also claimed and disclosed.
摘要翻译：描述了具有结构式I（B）的4-（7-羟基-2-异丙基-4-氧代-4H-喹唑啉-3-基） - 苄腈的新的多晶型物及其制备方法。还有一种制备式（I）的药学活性喹唑啉酮化合物的方法或方法，其中符号具有在说明书中给出的含义，所述方法包括使式（II）化合物（其中R4 * 是R 1 * -C（= O） - 其中R 1 *独立地选自如式（I）化合物所定义的R 1的含义，使得R 1 *和R 1彼此相同或不同，或 R4 *特别是H，并且R 1和R 3，R 5和R 6如式（I）化合物或其盐在与式（III）的苯胺化合物同时或顺序缩合和环化条件下所定义，其中R 2和m如式（I）化合物所定义。还要求和公开其他反应和相关实施方案。

2. 发明申请

WO2010084050A2 QUINAZOLINONE DERIVATIVES USEFUL AS VANILLOID ANTAGONISTS 审中-公开
标题翻译：喹诺酮类衍生物有助于VANILLOID ANTAGONISTS
公开(公告)号：WO2010084050A2
公开(公告)日：2010-07-29
申请号：PCT/EP2010/050243
申请日：2010-01-12
申请人： NOVARTIS AG , CHEN, Weichun , KIM, Hong-Yong , LIANG, Jessica , MUTZ, Michael , PRASHAD, Mahavir , TOWLER, Christopher , WU, Ruoqiu
发明人： CHEN, Weichun , KIM, Hong-Yong , LIANG, Jessica , MUTZ, Michael , PRASHAD, Mahavir , TOWLER, Christopher , WU, Ruoqiu
IPC分类号： A61P11/06 , C07D239/88 , A61K31/505
CPC分类号： C07D239/91 , A61K31/517
摘要： There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin- 3-yl)-benzonitrile having structural formula I(B) and to a method of preparing it. There is further a process or method for the manufacture of a pharmaceutically active quinazolinone compounds of the formula (I), wherein the symbols have the meanings given in the description, said process comprising reacting a compound of the formula (II), wherein R 4 * is R 1 *-C(=O)- wherein R 1 * is independently selected from the group of meanings of R 1 as defined for a compound of the formula (I) so that R 1 * and R 1 are identical to or different from each other, or R 4 *is especially H, and R 1 and R 3 , R 5 and R 6 are as defined for a compound of the formula (I), or a salt thereof, under simultaneous or sequential condensation and cyclisation conditions with an aniline compound of the formula (III), wherein R 2 and m are as defined for a compound of the formula (I). Further reactions and related embodiments are also claimed and disclosed.
摘要翻译：描述了具有结构式I（B）的4-（7-羟基-2-异丙基-4-氧代-4H-喹唑啉-3-基） - 苄腈的新的多晶型物及其制备方法。还有一种用于制备式（I）的药学活性喹唑啉酮化合物的方法或方法，其中符号具有在说明书中给出的含义，所述方法包括使式（II）化合物（其中R4 * 是R 1 * -C（= O） - 其中R 1 *独立地选自如式（I）化合物所定义的R 1的含义，使得R 1 *和R 1彼此相同或不同，或 R4 *特别是H，并且R 1和R 3，R 5和R 6如式（I）化合物或其盐在与式（III）的苯胺化合物同时或顺序缩合和环化条件下所定义，其中R 2和m如式（I）化合物所定义。还要求和公开其他反应和相关实施方案。

3. 发明申请

WO2002076946A2 PYRIDINE DERIVATIVES 审中-公开
标题翻译：吡啶衍生物
公开(公告)号：WO2002076946A2
公开(公告)日：2002-10-03
申请号：PCT/EP2002/003332
申请日：2002-03-25
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , CULSHAW, Andrew, James , GULL, Peter , HALLETT, Allan , KIM, Hong-Yong , SEILER, Max, Peter , ZIMMERMANN, Kaspar , LIU, Yugang , PRASHAD, Mahavir
发明人： CULSHAW, Andrew, James , GULL, Peter , HALLETT, Allan , KIM, Hong-Yong , SEILER, Max, Peter , ZIMMERMANN, Kaspar , LIU, Yugang , PRASHAD, Mahavir
IPC分类号： C07D211/00
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula I (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义，及其制备。式I化合物是人类香草素受体1（hVR1）的功能阻断剂，可用作药物; 特别是用于治疗疼痛。

4. 发明申请

WO02076946A3 FUSED PYRIDINE DERIVATIVES FOR USE AS VANILLOID RECEPTOR ANTAGONISTS FOR TREATING PAIN. 审中-公开
标题翻译：用于治疗疼痛的VANILLOID受体拮抗剂的氟化吡啶衍生物。
公开(公告)号：WO02076946A3
公开(公告)日：2002-12-27
申请号：PCT/EP0203332
申请日：2002-03-25
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , CULSHAW ANDREW JAMES , GULL PETER , HALLETT ALLAN , KIM HONG-YONG , SEILER MAX PETER , ZIMMERMANN KASPAR , LIU YUGANG , PRASHAD MAHAVIR
发明人： CULSHAW ANDREW JAMES , GULL PETER , HALLETT ALLAN , KIM HONG-YONG , SEILER MAX PETER , ZIMMERMANN KASPAR , LIU YUGANG , PRASHAD MAHAVIR
IPC分类号： A61K31/519 , A61K31/522 , A61K45/00 , A61P1/04 , A61P1/18 , A61P7/00 , A61P7/10 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/14 , A61P13/10 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P25/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P35/00 , A61P37/08 , C07D471/04 , C07D495/14
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula (I) wherein R , R , R , R and R are as defined in the description, and the preparation thereof. The compounds of formula I are functional blockers of the human vanilloid receptor 1 (hVR1) and are useful as pharmaceuticals; in particular for treating pain.
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义，及其制备。式I化合物是人类香草素受体1（hVR1）的功能阻断剂，可用作药物; 特别是用于治疗疼痛。

5. 发明申请

WO1997042970A1 DEPIGMENTATING AGENT IN THE TREATMENT OF MELASMA 审中-公开
标题翻译： MELASMA治疗代谢试剂
公开(公告)号：WO1997042970A1
公开(公告)日：1997-11-20
申请号：PCT/KR1997000081
申请日：1997-05-10
申请人： KIM, Dae-Ghon , YOU, Kyung-Ran , KIM, Eun-Sil , KIM, Hong-Yong
IPC分类号： A61K38/22
CPC分类号： A61K31/70 , A61K31/57 , A61K2300/00
摘要： This invention relates to a depigmenting agent, particularly a depigmenting compound containing a combination of corticosteroid and lincosamide. The corticosteroid of this invention may be selected from cortisol, cortisone, cortisterone, deoxycortisterone, aldosterone, prednisolone, triamcinolone, paramethasone, or betamethasone, dexamethasone; it is preferred to select betamethasone or dexamethasone, and its contents are in the range of 0.01 to 10 %, preferably in the range of 0.04 to 1 %. The lincosamide of this invention may be selected from lincomycin or clindamycin and its contents are in the range of 0.1 to 50 %, preferably in the range of 0.1 to 5 %. According to this invention, the formulation of a depigmenting agent may include a skin cream containing ointment base, additionally, lotion, solution, suspension, ointment, aerosol (spray), foam, paste, gel, or patch preparation. The depigmenting agent of this invention has a remarkable depigmenting effect with less side effects.
摘要翻译：本发明涉及一种脱色剂，特别是含有皮质类固醇和氯胺素组合的脱色素。本发明的皮质类固醇可以选自皮质醇，可的松，皮质酮，脱氧皮质醇，醛固酮，泼尼松龙，曲安奈德，地塞米松或倍他米松，地塞米松; 优选选择倍他米松或地塞米松，其含量为0.01〜10％，优选为0.04〜1％。本发明的林可酰胺可以选自林可霉素或克林霉素，其含量范围为0.1〜50％，优选为0.1〜5％。根据本发明，脱色剂的制剂可以包括含有软膏基质的护肤霜，另外还包括洗剂，溶液，悬浮液，软膏剂，气雾剂（喷雾剂），泡沫剂，糊剂，凝胶剂或贴片制剂。本发明的脱色剂具有显着的色素沉着效应，副作用较小。

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