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1. 发明申请

US20050054706A1 Pharmaceutically active compounds and methods of use 有权
标题翻译：药物活性化合物和使用方法
公开(公告)号：US20050054706A1
公开(公告)日：2005-03-10
申请号：US10491902
申请日：2002-10-23
申请人： Stephen Arkinstall , Antonio Arulanandam , Xuliang Jiang , Sharad Magar , Roustem Nabioullin , John Zhang , Peter Blume-Jensen
发明人： Stephen Arkinstall , Antonio Arulanandam , Xuliang Jiang , Sharad Magar , Roustem Nabioullin , John Zhang , Peter Blume-Jensen
IPC分类号： A61K31/41 , A61K31/4164 , A61K31/417 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61P1/04 , A61P1/14 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/02 , A61P7/06 , A61P7/10 , A61P9/00 , A61P9/14 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/06 , A61P15/08 , A61P15/10 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/04 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D233/54 , C07D233/60 , C07D233/61 , C07D233/68 , C07D249/08 , C07D257/04 , C07D401/12 , C07D405/12 , A61K31/415 , A61K31/416
CPC分类号： C07D233/60 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4439 , C07D233/54 , C07D233/56 , C07D233/61 , C07D233/64 , C07D233/68 , C07D249/08 , C07D257/04 , C07D401/12 , C07D405/12
摘要： The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing various cancers, inflammation, septic shock, preterm labor, infertility, pain, and ischemia, and other diseases and disorders associated with MEK-1 and/or ERK-2 activation.
摘要翻译：本发明提供取代的吡唑烷酮化合物，以及使用或包含一种或多种这些化合物的治疗方法和药物组合物。本发明的化合物可用于各种疗法，包括治疗或预防各种癌症，炎症，败血性休克，早产，不孕，疼痛和缺血以及与MEK-1和/或ERK-2相关的其它疾病和病症激活。

2. 发明申请

US20070225202A1 Methods for Identifying Modulators of Active Kit Tyrosine Kinase Receptor 审中-公开
标题翻译：鉴定活性成分酪氨酸激酶受体调节剂的方法
公开(公告)号：US20070225202A1
公开(公告)日：2007-09-27
申请号：US10579286
申请日：2004-12-06
申请人： Julian Andreev , Brian Healey , Peter Blume-Jensen , Stephen Arkinstall , Rong Dong
发明人： Julian Andreev , Brian Healey , Peter Blume-Jensen , Stephen Arkinstall , Rong Dong
IPC分类号： A61K31/00 , C07K16/00 , G01N33/567
CPC分类号： G01N33/5011 , C07K16/2803 , C07K16/44 , C07K2317/34 , G01N33/566 , G01N33/574 , G01N2333/9121 , G01N2500/04
摘要： The present invention relates to cell-based assays useful for screening for modulators, such as inhibitors, of activated mutant KIT tyrosine kinase receptors, which are associated with mast cell-related disorders, such as mastocytosis and various types of cancer. The invention further provides for the treatment of mast cell-related disorders with an inhibitor identified by the screening method.
摘要翻译：本发明涉及用于筛选与肥大细胞相关病症如肥大细胞增多症和各种类型的癌症有关的活化突变型KIT酪氨酸激酶受体的调节剂如抑制剂的基于细胞的测定法。本发明还提供了通过筛选方法鉴定的抑制剂治疗肥大细胞相关病症。

3. 发明申请

US20050100989A1 FSH glycosylation mutant 失效
标题翻译： FSH糖基化突变体
公开(公告)号：US20050100989A1
公开(公告)日：2005-05-12
申请号：US10934707
申请日：2004-09-02
申请人： Louise Garone , Stephen Arkinstall , William Brondyk , Robert Campbell , Xuliang Jiang , Sean McKenna , Mark Tepper
发明人： Louise Garone , Stephen Arkinstall , William Brondyk , Robert Campbell , Xuliang Jiang , Sean McKenna , Mark Tepper
IPC分类号： A61K20060101 , C07H21/04 , C07K14/59
CPC分类号： C07K14/59
摘要： A novel FSH mutant with increased glycosylation and longer half-lifes for use in inducing folliculogenesis in human patients is described. The FSH mutant permits the use of lower cumulative doses of FSH to achieve the same or better clinical result.
摘要翻译：描述了具有增加的糖基化和更长的半衰期用于诱导人类患者卵泡发生的新型FSH突变体。 FSH突变体允许使用较低累积剂量的FSH来实现相同或更好的临床结果。

4. 发明授权

US07432286B1 Pharmaceutically active sulfonyl hydrazide derivatives 失效
标题翻译：药物活性磺酰肼衍生物
公开(公告)号：US07432286B1
公开(公告)日：2008-10-07
申请号：US10088074
申请日：2000-09-28
申请人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean-Pierre Gotteland , Marco Biamonte
发明人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean-Pierre Gotteland , Marco Biamonte
IPC分类号： C07D417/12 , C07D213/74 , A61K31/44
CPC分类号： C07D213/74 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
摘要： The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation. In Formula (I) Ar1 and Ar2 are independently from each other an unsubstituted or substituted aryl or beteroaryl group, X1 and X2 are independently from each other O or S; R1, R2, R3 are independently from each other hydrogen or a C1-C6-alkyl substituent or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; or R2 and R3 form a substituted or unsubstituted 5-6-membered saturated or unsaturated ring; n is an integer from 0 to 5; G is selected from a group comprising or consisting of an unsubstituted or substituted 4-8 membered heterocycle containing at least one heteroatom, or G is a substituted or unstibstituted C1-C6-alkyl group.
摘要翻译：本发明涉及用作药物活性化合物的磺酰肼衍生物以及含有这种磺酰肼衍生物的药物制剂。所述磺酰肼衍生物是JNK途径的有效调节剂，它们特别是JNK 2和3的有效抑制剂。本发明还涉及新型磺酰肼衍生物及其制备方法。在式（I）中，Ar 1和Ar 2彼此独立地为未取代或取代的芳基或双芳基，X 1和X 2独立地为 SUP> 2 彼此独立地为O或S; R 1，R 2，R 3，3彼此独立地为氢或C 1 -C 3 > 6个 - 烷基取代基或R 1'与Ar 1形成取代或未取代的5-6元饱和或不饱和的环; 或R 2和R 3形成取代或未取代的5-6元饱和或不饱和环; n为0〜5的整数， G选自包含至少一个杂原子的未取代或取代的4-8元杂环或由其组成，或G是取代或未取代的C 1 -C 6 烷基。

5. 发明授权

US08012995B1 Pharmaceutically active sulfonamide derivatives 失效
标题翻译：药物活性磺酰胺衍生物
公开(公告)号：US08012995B1
公开(公告)日：2011-09-06
申请号：US10070954
申请日：2000-09-28
申请人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean Pierre Gotteland , Marco Biamonte
发明人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean Pierre Gotteland , Marco Biamonte
IPC分类号： A61P25/00 , A61P9/00 , A61K31/4436 , A61K31/4439 , A61K31/44 , C07D417/14 , C07D417/12 , C07D409/14 , C07D409/12 , C07D213/74
CPC分类号： C07D409/12 , C07D333/34 , C07D409/14 , C07D413/12 , C07D471/04 , C07D471/10 , C07D487/08 , C07D495/04
摘要： The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6 membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.
摘要翻译：本发明涉及式（I0）的磺酰胺衍生物，特别用作药物活性化合物，以及含有这种磺酰胺衍生物的药物制剂。所述磺酰胺衍生物是JNK途径的有效调节剂，它们特别有效和选择性抑制剂本发明还涉及新型磺酰胺衍生物及其制备方法，本发明式（I）化合物作为合适的药剂是其中Ar 1和Ar 2独立地为每个其它取代或未取代的芳基或杂芳基，X是O或S，优选O; R 1是氢或C 1 -C 6烷基，或者R 1与Ar 1; n形成取代或未取代的5-6元饱和或不饱和环是0至5的整数，优选1-3和最优选1;式（I）中的Y是未取代的或取代的4-1 含有至少一个氮原子的2-元饱和环状或双环烷基，由此一个氮原子，由此所述环中的一个氮原子与式（I）的磺酰基形成键，从而提供磺酰胺。

6. 发明授权

US07638538B1 Pharmaceutically active sulfonyl amino acid derivatives 失效
标题翻译：药物活性磺酰氨基酸衍生物
公开(公告)号：US07638538B1
公开(公告)日：2009-12-29
申请号：US10088090
申请日：2000-09-28
申请人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean-Pierre Gotteland , Marco Biamonte
发明人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean-Pierre Gotteland , Marco Biamonte
IPC分类号： A61K31/44 , C07D409/12
CPC分类号： C07D409/12
摘要： The present invention is related to sulfonyl amino acid derivatives of formula (I), notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl amino acid derivatives. Said sulfonyl amino acid are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 33. The present invention is furthermore related to novel sulfonyl amino acid derivatives as well as to methods of their preparation.
摘要翻译：本发明涉及式（I）的磺酰基氨基酸衍生物，特别用作药物活性化合物，以及含有这种磺酰氨基酸衍生物的药物制剂。所述磺酰氨基酸是JNK途径的有效调节剂，它们特别是JNK 2和33的有效抑制剂。本发明还涉及新型磺酰氨基酸衍生物及其制备方法。

7. 发明授权

US08017628B2 Pharmaceutically active sulfonyl hydrazide derivatives 失效
标题翻译：药物活性磺酰肼衍生物
公开(公告)号：US08017628B2
公开(公告)日：2011-09-13
申请号：US12172485
申请日：2008-07-14
申请人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean-Pierre Gotteland , Marco Biamonte
发明人： Stephen Arkinstall , Serge Halazy , Dennis Church , Montserrat Camps , Thomas Rueckle , Jean-Pierre Gotteland , Marco Biamonte
IPC分类号： C07D417/12 , C07D213/74 , A61K31/44
CPC分类号： C07D213/74 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
摘要： Sulfonyl hydrazide compounds according to formula I geometrical isomers thereof, optically active enantiomers thereof, diastereomers thereof, racemates thereof, and/or pharmaceutically acceptable salts thereof are useful in method for treating a neuronal disorder, an autoimmune disease, a cardiovascular disease, or cancer in a patient in need of such treatment.
摘要翻译：根据式I的磺酰肼化合物其几何异构体，其旋光活性对映异构体，其非对映异构体，其外消旋体和/或其药学上可接受的盐可用于治疗神经元病症，自身免疫性疾病，心血管疾病或癌症的方法需要这样治疗的病人。

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