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1. 发明申请

US20080009488A1 Raf Modulators and Methods of Use 有权
标题翻译： Raf调制器和使用方法
公开(公告)号：US20080009488A1
公开(公告)日：2008-01-10
申请号：US11568789
申请日：2005-03-25
申请人： Neel Anand , Charles Blazey , Owen Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Curtis , Larisa Dubenko , Abigail Kennedy , Steven Defina , Angie Kim , Jean-Claire Manalo , Csaba Peto , Kenneth Rice , Tsze Tsang , Anagha Joshi
发明人： Neel Anand , Charles Blazey , Owen Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Curtis , Larisa Dubenko , Abigail Kennedy , Steven Defina , Angie Kim , Jean-Claire Manalo , Csaba Peto , Kenneth Rice , Tsze Tsang , Anagha Joshi
IPC分类号： A61K31/4184 , A61K31/454 , A61K31/497 , A61K31/538 , A61P35/00 , C07D211/32 , C07D235/04 , C07D265/36 , C07D403/14 , C12N5/06 , C12N5/08 , G01N33/573
CPC分类号： C07D413/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译：本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。本发明的化合物抑制，调节和/或调节激酶，特别是Raf。使用化合物及其药物组合物治疗激酶依赖性疾病和病症的方法也是本发明的一个方面。

2. 发明申请

US20070032515A1 Anaplastic lymphoma kinase modulators and methods of use 失效
标题翻译：间变性淋巴瘤激酶调节剂及其使用方法
公开(公告)号：US20070032515A1
公开(公告)日：2007-02-08
申请号：US10565657
申请日：2004-07-23
申请人： Neel Anand , Charles Blazey , Owen Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Curtis , Larisa Dubenko , Abigail Kennedy , Richard Khoury , Angie Kim , Jean-Claire Manalo , Csaba Peto , Kenneth Rice , Tsze Tsang
发明人： Neel Anand , Charles Blazey , Owen Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Curtis , Larisa Dubenko , Abigail Kennedy , Richard Khoury , Angie Kim , Jean-Claire Manalo , Csaba Peto , Kenneth Rice , Tsze Tsang
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04 , C07D491/147 , C07D519/00
摘要： The present invention comprises compounds and pharmaceutical compositions comprising the compounds that are inhibitors of ALK. The invention also comprises methods of using the compounds and compositions to treat diseases mediated by ALK, including diseases such as cancer, immunological disorders, cardiovascular diseases, and other degenerative disorders.
摘要翻译：本发明包括包含作为ALK抑制剂的化合物的化合物和药物组合物。本发明还包括使用化合物和组合物来治疗由ALK介导的疾病，包括诸如癌症，免疫学障碍，心血管疾病和其它退行性疾病的疾病的方法。

3. 发明申请

US20060069077A1 Receptor-type kinase modulators and methods of use 有权
公开(公告)号：US20060069077A1
公开(公告)日：2006-03-30
申请号：US10522004
申请日：2003-07-14
申请人： Kenneth Rice , Neel Anand , Joerg Bussenius , Simona Costanzo , Abigail Kennedy , Angie Kim , Csaba Peto , Tsze Tsang , Charles Blazey
发明人： Kenneth Rice , Neel Anand , Joerg Bussenius , Simona Costanzo , Abigail Kennedy , Angie Kim , Csaba Peto , Tsze Tsang , Charles Blazey
IPC分类号： A61K31/517 , C07D239/94 , C07D239/88
CPC分类号： C07D403/12 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K31/5513 , A61K31/553 , A61K31/7064 , C07D239/94 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/04 , C07D487/04 , C07D493/04
摘要： The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

4. 发明授权

US5849709A Saccharopeptides and derivatives thereof 失效
标题翻译：糖肽及其衍生物
公开(公告)号：US5849709A
公开(公告)日：1998-12-15
申请号：US438669
申请日：1995-05-10
申请人： Peter Fugedi , Csaba Peto
发明人： Peter Fugedi , Csaba Peto
IPC分类号： A61K31/70 , A61K31/7028 , A61P9/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07H3/06 , C07H13/04 , C07H15/04 , C07H15/18 , A61K38/04
CPC分类号： A61K31/7008 , A61K31/7016 , A61K31/702 , C07H13/04 , C07H15/04 , C07H15/18 , C07H3/06
摘要： Saccharopeptides and methods of using the novel saccharopeptides are described having the following structural formula I: W--�--Y--W--!.sub.m (I) wherein W is independently one or more saccharide(s); Y is independently --CO--NH-- or --NH--CO--; and m is an integer greater than or equal to one; or structural formula II: W--Y--�W--X--W--Y!.sub.n --W (II) wherein W is independently one or more saccharide(s); S is a difunctional or polyfunctional alkyl, aryl or aralkyl group, lipid, amino acid or peptide capable of covalently joining together said saccharides; Y is independently --CO--NH-- or --NH--CO--; and n is an integer greater than or equal to zero; or formula III: W--Y.sup.1 --X.sup.1 --Y.sup.2 --W (III) wherein W is independently one or more saccharide(s); X.sup.1 is a difunctional or polyfunctional alkyl, aryl or aralkyl group capable of covalently joining together said saccharides; Y.sup.1 is --NH--CO--; and Y.sup.2 is --CO--NH--.
摘要翻译：描述了使用这种新型糖肽的糖肽和具有以下结构式I的W - [ - Y-W-] m（I），其中W独立地为一种或多种糖类; Y独立地是-CO-NH-或-NH-CO-; m是大于或等于1的整数; 或结构式II：W-Y- [W-X-W-Y] n -W（II）其中W独立地为一种或多种糖类; S是能够将所述糖共价连接在一起的二官能或多官能的烷基，芳基或芳烷基，脂质，氨基酸或肽; Y独立地是-CO-NH-或-NH-CO-; 并且n是大于或等于零的整数; 或式III：W-Y1-X1-Y2-W（III）其中W独立地为一个或多个糖; X1是能够将所述糖共价连接在一起的二官能或多官能的烷基，芳基或芳烷基; Y1是-NH-CO-; 而Y2是-CO-NH-。

5. 发明申请

US20100216831A1 DESLORATADINE CRYSTALLINE FORMS MIXTURES HAVING A LOW LEVEL OF RESIDUAL SOLVENTS 审中-公开
标题翻译： DESLORATADINE晶体结构混合物具有低水平的残留溶剂
公开(公告)号：US20100216831A1
公开(公告)日：2010-08-26
申请号：US11917839
申请日：2006-11-17
申请人： Zoltan Toth , Piroska Kovacs , Csaba Peto , Adrienne Kovacsne Mezei
发明人： Zoltan Toth , Piroska Kovacs , Csaba Peto , Adrienne Kovacsne Mezei
IPC分类号： A61K31/4545 , C07D401/02
CPC分类号： C07D401/04
摘要： Provided are desloratadine mixtures, comprising a low level of residual solvents and processes for the preparation thereof.
摘要翻译：提供了地氯雷他定混合物，其包含低水平的残留溶剂及其制备方法。

6. 发明授权

US07608714B2 Production of dolasetron 失效
标题翻译：多拉司琼的生产
公开(公告)号：US07608714B2
公开(公告)日：2009-10-27
申请号：US11650294
申请日：2007-01-05
申请人： Janos Hajko , Tivadar Tamas , Adrienne Kovacsne-Mezei , Erika Magyar Molnarne , Csaba Peto , Csaba Szabo
发明人： Janos Hajko , Tivadar Tamas , Adrienne Kovacsne-Mezei , Erika Magyar Molnarne , Csaba Peto , Csaba Szabo
IPC分类号： C07D221/22 , C07D451/00 , C07D455/00
CPC分类号： C07D471/18 , C07D303/40 , C07D451/14 , C07F7/1804
摘要： The present invention provides an improved process for the preparation of Dolasetron salts, in particularly Dolasetron mesylate. Also provided are intermediates for the process and methods of preparing the intermediates.
摘要翻译：本发明提供了制备Dolasetron盐的改进方法，特别是甲磺酸多拉司琼。还提供了制备中间体的方法和方法的中间体。

7. 发明申请

US20070203177A1 Forms of dolasetron mesylate and processes for their preparation 审中-公开
标题翻译：甲磺酸多拉司琼的形式及其制备方法
公开(公告)号：US20070203177A1
公开(公告)日：2007-08-30
申请号：US11650352
申请日：2007-01-05
申请人： Janos Hajko , Tivadar Tamas , Adrienne Kovacsne-Mezei , Erika Molnarne , Csaba Peto , Csaba Szabo
发明人： Janos Hajko , Tivadar Tamas , Adrienne Kovacsne-Mezei , Erika Molnarne , Csaba Peto , Csaba Szabo
IPC分类号： A61K31/4745
CPC分类号： C07D471/18 , C07D303/40 , C07D451/14 , C07F7/1804
摘要： The present invention provides crystalline polymorphic forms of Dolasetron mesylate. Also provided are methods of preparing the crystalline polymorphic forms of Dolasetron mesylate. Further, the crystalline Dolasetron mesylate forms may be used in pharmaceutical compositions.
摘要翻译：本发明提供了甲磺酸多沙司琼的结晶多晶型物。还提供了制备甲磺酸多沙司琼的结晶多晶型形式的方法。此外，结晶的多沙司琼甲磺酸盐形式可以用于药物组合物。

8. 发明申请

US20060223841A1 Stable pharmaceutical compositions of desloratadine and processes for preparation of polymorphic forms of desloratadine 审中-公开
公开(公告)号：US20060223841A1
公开(公告)日：2006-10-05
申请号：US11447336
申请日：2006-06-05
申请人： Zoltan Toth , Piroska Kovacs , Csaba Peto , Adrienne Kovacsne-Mezei
发明人： Zoltan Toth , Piroska Kovacs , Csaba Peto , Adrienne Kovacsne-Mezei
IPC分类号： A61K31/473 , C07D221/02
CPC分类号： C07D401/04 , A61K31/4545
摘要： Provided are stable pharmaceutical compositions of desloratadine. Also provided are processes for preparing polymorphs of desloratadine

9. 发明申请

US20070203175A1 Productioin of dolasetron 审中-公开
标题翻译：多拉司琼的生产
公开(公告)号：US20070203175A1
公开(公告)日：2007-08-30
申请号：US11650355
申请日：2007-01-05
申请人： Janos Hajko , Tivadar Tamas , Adrienne Kovacsne-Mezei , Erika Molnarne , Csaba Peto , Csaba Szabo
发明人： Janos Hajko , Tivadar Tamas , Adrienne Kovacsne-Mezei , Erika Molnarne , Csaba Peto , Csaba Szabo
IPC分类号： A61K31/4745 , C07D471/14 , C07F7/02 , C07D453/00
CPC分类号： C07D471/18 , C07D303/40 , C07D451/14 , C07F7/1804
摘要： The present invention provides an improved process for the preparation of Dolasetron salts, in particularly Dolasetron mesylate. Also provided are intermediates for the process and methods of preparing the intermediates. Intermediates for preparing Dolasetron according to the invention include 7-alkoxycarbonyl-9-(alkoxycarbonylmethyl)-3-trialkylsilyloxy-9-azabicyclo[3.3.1]nonane compounds (SAN compounds) and endo-9-alkoxycarbonyl-5-trialkylsilyloxy-8-azatricyclo[5.3.1.03,8]undecan-10-one compounds (SQO compounds).
摘要翻译：本发明提供了制备Dolasetron盐的改进方法，特别是甲磺酸多拉司琼。还提供了制备中间体的方法和方法的中间体。用于制备根据本发明的多沙司琼的中间体包括7-烷氧基羰基-9-（烷氧基羰基甲基）-3-三烷基甲硅烷氧基-9-氮杂双环[3.3.1]壬烷化合物（SAN化合物）和内-9-烷氧基羰基-5-三烷基甲硅烷氧基-8- 氮杂三环[5.3.1.0 3,8]十一碳-10-酮化合物（SQO化合物）。

10. 发明申请

US20060135547A1 Stable pharmaceutical compositions of desloratadine and processes for preparation of polymorphic forms of desloratadine 审中-公开
标题翻译：地氯雷他定的稳定药物组合物和地氯雷他定的多晶型物的制备方法
公开(公告)号：US20060135547A1
公开(公告)日：2006-06-22
申请号：US11283276
申请日：2005-11-17
申请人： Zoltan Toth , Piroska Kovacs , Csaba Peto , Adrienne Kovacsne-Mezei
发明人： Zoltan Toth , Piroska Kovacs , Csaba Peto , Adrienne Kovacsne-Mezei
IPC分类号： A61K31/473 , C07D221/16
CPC分类号： C07D401/04 , A61K31/4545
摘要： Provided are stable pharmaceutical compositions of desloratadine. Also provided are processes for preparing polymorphs of desloratadine
摘要翻译：提供地氯雷他定的稳定药物组合物。还提供了制备地氯雷他定多晶型物的方法

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