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1. 发明专利

JP2012149099A Organic compound 有权
标题翻译：有机化合物
公开(公告)号：JP2012149099A
公开(公告)日：2012-08-09
申请号：JP2012109447
申请日：2012-05-11
申请人： Novartis Ag , ノバルティスアーゲー
发明人： HOEHN PASCALE , KOCH BERND , MUTZ MICHAEL
IPC分类号： C07D498/22 , A61K31/553 , A61P35/00
CPC分类号： C07D498/22
摘要： PROBLEM TO BE SOLVED: To provide a new crystalline form II of N-benzoyl-staurosporine, compositions containing the compound, processes for the preparation of the compound, and use of the crystalline form II of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, particularly humans, and to provide an amorphous form of N-benzoyl-staurosporine, compositions containing the compound, processes for the preparation of the compound, and use of the amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, particularly humans.SOLUTION: A preparation process of N-benzoyl-staurosporine is provided, comprising reacting staurosporine with a benzoic anhydride. The process optionally further includes a step of seeding the reaction solution to produce either amorphous or crystalline form II of N-benzoyl-staurosporine.
摘要翻译：待解决的问题：为了提供N-苯甲酰基星形孢菌素的新结晶形式II，含有该化合物的组合物，该化合物的制备方法以及N-苯甲酰基星形孢菌素的结晶形式II在诊断中的用途温血动物，特别是人类的方法或治疗方法，以及提供无定形形式的N-苯甲酰基星形孢菌素，含该化合物的组合物，制备该化合物的方法，以及使用无定形N-苯甲酰基星形孢菌素诊断方法或治疗温血动物，特别是人类。解决方案：提供N-苯甲酰基星孢菌素的制备方法，包括使星形孢菌素与苯甲酸酐反应。该方法还可包括将反应溶液接种以产生N-苯甲酰基星形孢菌素的无定形或结晶形式II的步骤。版权所有（C）2012，JPO＆INPIT

2. 发明专利

JP2014074067A F, g, h, i and k crystal forms of imatinib mesylate 审中-公开
标题翻译： F，G，H，I和K晶形体的晶体形式
公开(公告)号：JP2014074067A
公开(公告)日：2014-04-24
申请号：JP2014005741
申请日：2014-01-16
申请人： Novartis Ag , ノバルティスアーゲー
发明人： MUTZ MICHAEL
IPC分类号： C07D401/04 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/506 , A61K47/02 , A61K47/04 , A61K47/12 , A61K47/32 , A61K47/38 , A61K47/42 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： C07D401/04 , C07D401/14
摘要： PROBLEM TO BE SOLVED: To provide specific crystal forms of methanesulfonic acid addition salts of 4-(4-methylpiperazine-1-ylmethyl)-N-[4-methyl-3-(4-(pyridine-3-yl)pyrimidine-2-ylamino)phenyl]-benzamide.SOLUTION: There are provided the F crystal form, the G crystal form, the H crystal form, the I crystal form and the K crystal form of methanesulfonic acid addition salts of 4-(4-methylpiperazine-1-ylmethyl)-N-[4-methyl-3-(4-(pyridine-3-yl)pyrimidine-2-ylamino)phenyl]-benzamide.
摘要翻译：要解决的问题：提供4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3-（4-（吡啶-3-基）嘧啶-2 - 基氨基）苯基] - 苯甲酰胺。溶液：提供了4-（4-甲基哌嗪-1-基）苯甲酰胺的F晶型，G晶型，H晶型，I晶型和K晶型甲磺酸加成盐，嗪-1-基甲基）-N- [4-甲基-3-（4-（吡啶-3-基）嘧啶-2-基氨基）苯基] - 苯甲酰胺。

3. 发明专利

JP2014051517A Polymorphic form of deferasirox(icl670a) 审中-公开
标题翻译： DEFERASIROX的多晶型（ICL670A）
公开(公告)号：JP2014051517A
公开(公告)日：2014-03-20
申请号：JP2013228491
申请日：2013-11-01
申请人： Novartis Ag , ノバルティスアーゲー
发明人： MUTZ MICHAEL
IPC分类号： C07D249/08 , A61K31/4196 , A61P7/06 , A61P39/04
CPC分类号： C07D249/08 , A61K31/4196
摘要： PROBLEM TO BE SOLVED: To provide a crystalline form of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid, its amorphous form, a production method of the same, and a composition comprising them.SOLUTION: A production method of crystalline form B of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid comprises the following steps: (a) heating crystalline form A of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid to its melting point of about 261°C or higher, (b) cooling the melted product of the step (a) to about room temperature or below to obtain amorphous form, (c) heating the amorphous form of the step (b) to a temperature of 95°C or higher, preferably 190°C or higher to recrystallize to the crystalline form B, and (d) by cooling to the room temperature, isolating crystalline form B of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl].
摘要翻译：待解决的问题：提供4- [3,5-双（2-羟基苯基） - [1,2,4]三唑-1-基]苯甲酸的结晶形式，其无定形形式，相同的组合物和包含它们的组合物。溶液：4- [3,5-双（2-羟基苯基） - [1,2,4]三唑-1-基]苯甲酸的晶型B的制备方法包括以下步骤：（a）将结晶形式A的4- [3,5-双（2-羟基苯基） - [1,2,4]三唑-1-基]苯甲酸加热至约261℃或更高的熔点，（b）将步骤（a）的熔融产物冷却至约室温或更低温度以获得无定形形式，（c）将步骤（b）的无定形形式加热到95℃或更高的温度，优选190℃ ℃以上，再结晶成B型，（d）冷却至室温，分离4- [3,5-双（2-羟基苯基） - [1,2,4]三唑 -1-基]。

4. 发明专利

JP2013227324A Stabilized amorphous form of imatinib mesylate 审中-公开
标题翻译：稳定的非对映体形式
公开(公告)号：JP2013227324A
公开(公告)日：2013-11-07
申请号：JP2013128722
申请日：2013-06-19
申请人： Novartis Ag , ノバルティスアーゲー
发明人： GONCALVES ELISABETE , KALB OSKAR , MUTZ MICHAEL , WIRTH WOLFGANG , LAKSHMAN JAY PARTHIBAN
IPC分类号： A61K31/506 , A61K9/20 , A61K9/48 , A61K47/02 , A61K47/40 , A61K47/42 , A61P35/00 , A61P35/02 , A61P35/04
CPC分类号： A61K31/506 , A61K9/146 , A61K9/4858 , A61K9/4866 , A61K47/02 , A61K47/10 , A61K47/32 , A61K47/34 , A61K47/38 , A61K47/40
摘要： PROBLEM TO BE SOLVED: To provide a stabilized amorphous form of imatinib mesylate.SOLUTION: A pharmaceutical composition comprises a formulation principle that stabilizes an amorphous form of Imatinib mesylate and amorphous Imatinib mesylate, optionally together with a least one pharmaceutically acceptable carrier. The formulation principle is selected from solid dispersions, cyclodextrin complexes, co-milling with selected excipients. A capsule contains between an amount of stabilized amorphous Imatinib mesylate which corresponds to 50 mg and 200 mg of Imatinib mesylate, wherein the shell contains gelatine, titanium dioxide, or red iron oxide. The ratio of weight of capsule fill to capsule shell is between about 100:25 and 100:50. A tablet comprises an amount of stabilized amorphous Imatinib mesylate which corresponds to 100 mg, 400 mg or 800 mg of Imatinib mesylate.
摘要翻译：要解决的问题：提供稳定的非晶形式的伊马替尼甲磺酸盐。解决方案：药物组合物包含稳定无定形形式的甲磺酸伊马替尼和无定形伊马替尼甲磺酸盐的任选与至少一种药学上可接受的载体一起的制剂原理。制剂原理选自固体分散体，环糊精复合物，与选择的赋形剂共研磨。胶囊含有一定量的对应于50mg和200mg甲磺酸伊马替尼的稳定化的非晶形伊马替尼甲磺酸盐，其中该壳含有明胶，二氧化钛或红色氧化铁。胶囊填充物与胶囊壳的重量比在约100:25至100:50之间。片剂包含一定量的对应于100mg，400mg或800mg甲磺酸伊马替尼的稳定的非晶形伊马替尼甲磺酸盐。

5. 发明专利

JP2010099089A Method for fermentation production of cytostatic agent and crystal thereof 审中-公开
标题翻译：用于发酵细胞生长的方法及其结晶
公开(公告)号：JP2010099089A
公开(公告)日：2010-05-06
申请号：JP2010015022
申请日：2010-01-27
申请人： Novartis Ag , ノバルティスアーゲー
发明人： HOFMANN HANS , MAHNKE MARION , MEMMERT KLAUS , PETERSEN FRANK , SCHUPP THOMAS , KUESTERS ERNST , MUTZ MICHAEL
IPC分类号： C12P17/00 , A61K31/00 , A61K31/427 , A61P35/00 , A61P35/04 , A61P43/00 , B01D15/00 , B01D15/08 , C07D493/04 , C12N1/14 , C12P20060101 , C12P17/16 , C12P17/18 , C12R1/01 , C12R1/645
CPC分类号： C07D493/04 , C07D417/14 , C07K2299/00 , C12P17/167 , C12P17/181 , C12R1/01
摘要： PROBLEM TO BE SOLVED: To provide a method for producing epothilones in a large scale. SOLUTION: In order to produce epothilones in bioengineering scale, a method for concentrating epothilones, particularly epothilones A and/or B, especially epothilone B in a culture medium is disclosed. The method comprises microorganisms producing their compounds, particularly myxobacteria (as bacteria for producing natural products), thereby a complex soluble in the medium is added to the medium. New crystal of epothilone B is also disclosed. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供大规模生产埃坡霉素的方法。解决方案：为了在生物工程规模中生产埃坡霉素，公开了一种在培养基中浓缩埃坡霉素，特别是埃坡霉素A和/或B，特别是埃坡霉素B的方法。该方法包括产生其化合物的微生物，特别是产生天然产物的细菌（作为生产天然产物的细菌），从而将可溶于培养基的复合物加入到培养基中。还公开了埃坡霉素B的新晶体。版权所有（C）2010，JPO＆INPIT

6. 发明公开

KR20180054816A 모노박탐 항생제의 염 및 고체 형태 审中-公开
公开(公告)号：KR20180054816A
公开(公告)日：2018-05-24
申请号：KR20187011354
申请日：2016-09-20
申请人： NOVARTIS AG
发明人： AUBIN ERIC , CASAREZ ANTHONY , FISCH ANDREAS , LI ZAIXING , LINDVALL MIKA , MOSER HEINZ ERNST , MUTZ MICHAEL , RECK FOLKERT , RIEBESEHL BERND ULRICH , SCHOENHENTZ MARC , SETHURAMAN VIJAY , SIMMONS ROBERT LOWELL
IPC分类号： C07D417/14 , A61K31/427 , A61P31/00 , A61P31/04
CPC分类号： C07D417/14
摘要： 본발명은 1-(((Z)-(1-(2-아미노티아졸-4-일)-2-옥소-2-(((3S,4R)-2-옥소-4-((2-옥소옥사졸리딘-3-일)메틸)-1-술포아제티딘-3-일)아미노)에틸리덴)아미노)옥시)시클로프로판카르복실산 (본원에서화합물 X로지칭됨)의신규고체형태, 염및 다형체, 이들을함유하는제약조성물, 및그의제조방법및 요법에서의용도를제공한다.

7. 发明专利

JP2005068156A Fermentative preparation process and crystal form of cytostatic 审中-公开
标题翻译：发酵制备工艺和结晶形式
公开(公告)号：JP2005068156A
公开(公告)日：2005-03-17
申请号：JP2004287797
申请日：2004-09-30
申请人： Novartis Ag , ノバルティスアクチエンゲゼルシャフト
发明人： HOFMANN HANS , MAHNKE MARION , MEMMERT KLAUS , PETERSEN FRANK , SCHUPP THOMAS , KUESTERS ERNST , MUTZ MICHAEL
IPC分类号： A61K31/00 , A61K31/427 , A61P35/00 , A61P35/04 , A61P43/00 , B01D15/00 , B01D15/08 , C07D493/04 , C12N1/14 , C12P20060101 , C12P17/16 , C12P17/18 , C12R1/01 , C12R1/645
CPC分类号： C07D493/04 , C07D417/14 , C07K2299/00 , C12P17/167 , C12P17/181 , C12R1/01
摘要： PROBLEM TO BE SOLVED: To provide a method for a large scale production of epothilones. SOLUTION: The invention relates to a process for biotechnological preparation of epothilones comprising concentration of epothilones in culture media, especially concentrating epothilone A and/or epothilone B, more especially concentrating epothilone B, wherein the process comprises microorganisms which produce these compounds, especially comprising myxobacteria as producers of natural substances, whereby a complex which is soluble in the culture medium is added to the medium. And a new crystal form of the epothilone B is disclosed in the specification. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：要解决的问题：提供大规模生产埃坡霉素的方法。解决方案：本发明涉及埃博霉素的生物技术制备方法，其包括在培养基中浓缩埃坡霉素，特别是浓缩埃坡霉素A和/或埃坡霉素B，特别是浓缩埃坡霉素B，其中该方法包括产生这些化合物的微生物，特别是包含作为天然物质的生产者的粘液细菌，由此将可溶于培养基的复合物添加到培养基中。在本说明书中公开了埃坡霉素B的新结晶形式。版权所有（C）2005，JPO＆NCIPI

8. 发明申请

WO9942602A3 FERMENTATIVE PREPARATION PROCESS FOR CYTOSTATICS AND CRYSTAL FORMS THEREOF 审中-公开
标题翻译：用于细胞周期和晶体形式的发酵制备方法
公开(公告)号：WO9942602A3
公开(公告)日：1999-11-25
申请号：PCT/EP9901025
申请日：1999-02-17
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH
发明人： HOFMANN HANS , MAHNKE MARION , MEMMERT KLAUS , PETERSEN FRANK , SCHUPP THOMAS , KUESTERS ERNST , MUTZ MICHAEL
IPC分类号： A61K31/00 , A61K31/427 , A61P35/00 , A61P35/04 , A61P43/00 , B01D15/00 , B01D15/08 , C07D493/04 , C12N1/14 , C12P20060101 , C12P17/16 , C12P17/18 , C12R1/01 , C12R1/645
CPC分类号： C07D493/04 , C07D417/14 , C07K2299/00 , C12P17/167 , C12P17/181 , C12R1/01
摘要： The invention relates to a process for concentrating epothilones in culture media, a process for the production of epothilones, a process for separating epothilones A and B and a strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. Crystal forms of epothilone B are also described.
摘要翻译：本发明涉及用于将埃坡霉素浓缩在培养基中的方法，埃坡霉素的生产方法，分离埃坡霉素A和B的方法以及通过诱变获得的用于产生埃坡霉素的菌株，以及与其有关的方面。还描述了埃坡霉素B的晶体形式。

9. 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。

10. 发明申请

WO2008019820A3 CRYSTAL FORM OF EPOTHILONE B AND USE IN PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： EPOTHILONE B的晶体形态和药物组合物的使用
公开(公告)号：WO2008019820A3
公开(公告)日：2008-04-17
申请号：PCT/EP2007007173
申请日：2007-08-14
申请人： NOVARTIS AG , KUESTERS ERNST , MUTZ MICHAEL , STOWASSER FRANK
发明人： KUESTERS ERNST , MUTZ MICHAEL , STOWASSER FRANK
IPC分类号： C07D493/04 , A61K31/425 , A61K35/00
CPC分类号： C07D493/04
摘要： The invention relates to new crystal forms of epothilone B.
摘要翻译：本发明涉及埃坡霉素B的新晶型。

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