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1. 发明申请

WO0233596A3 METHOD OF OPERATING A COMPUTER SYSTEM TO PERFORM A DISCRETE SUBSTRUCTURAL ANALYSIS 审中-公开
标题翻译：操作计算机系统以执行离散分析分析的方法
公开(公告)号：WO0233596A3
公开(公告)日：2003-10-02
申请号：PCT/EP0111955
申请日：2001-10-16
申请人： APPLIED RESEARCH SYSTEMS , CHURCH DENNIS , COLINGE JACQUES
发明人： CHURCH DENNIS , COLINGE JACQUES
IPC分类号： C07B61/00 , C07C39/40 , C07C233/44 , C07C323/32 , C07C335/16 , G01N33/48 , G01N33/50 , G06F20060101 , G06F17/18 , G06F17/30 , G06F17/50 , G06F19/16 , G06F19/00
CPC分类号： G06F19/16
摘要： The invention provides a method of operating a computer system, and a corresponding computer system, for performing a discrete substructural analysis. First, a database of molecular structures is accessed. The database is searchable by molecular structure information and biological and/or chemical properties. In said database, a set of molecules is identified that have a given biological and/or chemical property. Fragments of the molecules in said subset are then determined, and a score value is calculated for each fragment, indicating the contribution of the respective fragment to said given biological and/or chemical property. Finally, a reiteration process is performed by analyzing the determined fragments and calculated scores values, whereby first at least one fragment is selected that has a score value indicating high contribution to said biological and/or chemical property, and then the steps of accessing, identifying, determining and calculating are repeated. Fragments may be any structural subunit of the molecules. The biological and/or chemical properties include biochemical, pharmacological, toxicological, pesticidal, herbicidal and catalytic properties. The invention is preferably used for DNA backsequencing or drug discovery. Preferred embodiments include an reiteration process that increases the fragment size in each iteration, the use of generiy substructures, and an annealing process that glues fragments together.
摘要翻译：本发明提供了一种操作计算机系统的方法和用于执行离散子结构分析的对应的计算机系统。首先，访问分子结构的数据库。数据库可以通过分子结构信息和生物和/或化学性质进行搜索。在所述数据库中，鉴定出一组具有给定生物和/或化学性质的分子。然后确定所述子集中的分子的片段，并计算每个片段的得分值，指示相应片段对所述给定生物和/或化学性质的贡献。最后，通过分析确定的片段和计算的分数值来进行重复过程，由此首先选择具有指示对所述生物和/或化学性质的高贡献的分数值的至少一个片段，然后访问，识别，重复确定和计算。片段可以是分子的任何结构亚基。生物和/或化学性质包括生物化学，药理学，毒理学，杀虫剂，除草和催化性质。本发明优选用于DNA逆序测序或药物发现。优选的实施方案包括在每次迭代中增加片段大小，使用通用亚结构以及将片段粘合在一起的退火过程的重复过程。

2. 发明申请

WO02102359A3 ALKYLIDENE PYRAZOLIDINEDIONE DERIVATIVES AND USE FOR TREATING DIABETES AND OBESITY 审中-公开
标题翻译：亚苄基吡唑啉酮衍生物和用于治疗糖尿病和肥胖的用途
公开(公告)号：WO02102359A3
公开(公告)日：2003-08-28
申请号：PCT/EP0206627
申请日：2002-06-14
申请人： APPLIED RESEARCH SYSTEMS , BOMBRUN AGNES , RUECKLE THOMAS , SWINNEN DOMINIQUE , GONZALEZ JEROME , CHURCH DENNIS
发明人： BOMBRUN AGNES , RUECKLE THOMAS , SWINNEN DOMINIQUE , GONZALEZ JEROME , CHURCH DENNIS
IPC分类号： A61K31/00 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61P3/04 , A61P3/10 , A61P15/00 , A61P15/08 , A61P43/00 , C07D231/32 , C07D401/06 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06
CPC分类号： C07D401/06 , A61K31/00 , A61K31/4155 , A61K31/4192 , C07D231/32 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06
摘要： The present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula I for the treatment and/or prevention of diabetes type I and/or II, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity and polycystic ovary syndrome PCOS. In particular, the present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula I to modulate, notably to inhibit the activity of PTPs, in particular PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel alkylidene pyrazolidinedione derivatives. I R1 and R2 represent independently from each other an unsubstituted or substituted aryl or heteroaryl.
摘要翻译：本发明涉及式I的亚烷基吡唑烷二酮衍生物用于治疗和/或预防I型和/或II型糖尿病，葡萄糖耐量降低，胰岛素抵抗，高血糖症，肥胖症和多囊卵巢综合征PCOS的用途。特别地，本发明涉及使用式I的亚烷基吡唑烷二酮衍生物调节，特别是抑制PTP的活性，特别是PTP1B，TC-PTP，SHP和GLEPP-1的活性。本发明还涉及新的亚烷基吡唑烷二酮衍生物。 R1和R2彼此独立地表示未取代或取代的芳基或杂芳基。

3. 发明申请

WO0226733A3 sHARMACEUTICALLY ACTIVE SULFONAMIDE DERIVATIVES BEARING BOTH LIPOPHILIC AND IONISABLE MOIETIES AS INHIBITORS OF PROTEIN JUNKINASES 审中-公开
标题翻译：作为蛋白胨的抑制剂的两亲性和可溶性动物的主动磺酰胺衍生物
公开(公告)号：WO0226733A3
公开(公告)日：2002-08-01
申请号：PCT/IB0101772
申请日：2001-09-27
申请人： APPLIED RESEARCH SYSTEMS , HALAZY SERGE , CHURCH DENNIS , CAMPS MONTSERRAT , GOTTELAND JEAN-PIERRE , RUECKLE THOMAS , BIAMONTE MARCO , ARKINSTALL STEPHEN
发明人： HALAZY SERGE , CHURCH DENNIS , CAMPS MONTSERRAT , GOTTELAND JEAN-PIERRE , RUECKLE THOMAS , BIAMONTE MARCO , ARKINSTALL STEPHEN
IPC分类号： A61K31/4025 , A61K31/4535 , A61K31/4545 , A61K31/5377 , A61K31/55 , A61P1/04 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/12 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07D333/34 , C07D409/12 , C07D409/14 , C07D413/14
CPC分类号： C07D409/12 , C07D333/34 , C07D409/14 , C07D413/14
摘要： The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related 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 which is substituted with at least one ionisable moiety to which a lipophilic chain is attached and which is containing at least 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：本发明涉及具有亲油部分并且基本上可溶的磺酰胺衍生物。所述化合物特别用作药物活性化合物。本发明还涉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，它们特别是JNK 2和3的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。根据本发明的作为合适的药剂的式（I）化合物是其中Ar 1和Ar 2彼此独立地为取代或未取代的芳基或杂芳基，X为O或S，优选O; R 1为氢或C 1 C 1-6 - 烷基或R 1与Ar 1形成取代或未取代的5-6元饱和或不饱和环; n为0至5，优选1-3至最优选1的整数;式（I）中的Y 是未被取代的或取代的4-12元饱和的环状或双环烷基，其被至少一个亲电链连接的可离子化部分取代，并且含有至少一个氮原子，其中所述环内的一个氮原子是与式（I）的磺酰基形成键，从而提供磺酰胺。

4. 发明专利

CA2394809C BENZAZOLE DERIVATIVES AND THEIR USE AS JNK MODULATORS 未知
公开(公告)号：CA2394809C
公开(公告)日：2011-03-15
申请号：CA2394809
申请日：2000-12-20
申请人： APPLIED RESEARCH SYSTEMS
发明人： HALAZY SERGE , CHURCH DENNIS , CAMPS MONTSERRAT , GAILLARD PASCALE , GOTTELAND JEAN-PIERRE
IPC分类号： C07D417/06 , A61K31/506 , A61K31/517 , A61K31/5377 , A61P1/04 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/06 , C07D277/64 , C07D403/06 , C07D413/06 , C07D417/14 , C07D521/00
摘要： The present invention is related to benzazole derivatives accord-ing to formula (I) wherein X is O, S, or NR O with R0 being H or an unsubstituted or substituted C1-C6alkyl, and G is an unsubstituted or substituted pyrimidinyl group, notably for use as pharmaceutically active compounds, as well as to phar-maceutical formulations containing such benzazoles derivatives. Said benzazoles derivatives are efficient modulators of the JNK pathway, they are in particular ef-ficient and selective inhibitors of JNK2 and/or 3.

5. 发明专利

CA2420568C PHARMACEUTICALLY ACTIVE BENZSULFONAMIDE DERIVATIVES AS INHIBITORS OF PROTEIN JUNKINASES 未知
公开(公告)号：CA2420568C
公开(公告)日：2010-09-21
申请号：CA2420568
申请日：2001-09-27
申请人： APPLIED RESEARCH SYSTEMS
发明人： HALAZY SERGE , CHURCH DENNIS , CAMPS MONTSERRAT , GOTTELAND JEAN-PIERRE , RUECKLE THOMAS , BIAMONTE MARCO , ARKINSTALL STEPHEN
IPC分类号： C07D211/96 , A61K31/401 , A61K31/4468 , A61P9/10 , A61P11/06 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/00 , C07D207/48
摘要： The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group.X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, -COOR3, -CONR3R3', OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.

6. 发明专利

BG65797B1 PHARMACEUTICALLY ACTIVE SULPONAMIDE DERIVATIVES 未知
公开(公告)号：BG65797B1
公开(公告)日：2009-12-31
申请号：BG10652702
申请日：2002-03-18
申请人： APPLIED RESEARCH SYSTEMS
发明人： ARKINSTALL STEPHEN , HALAZY SERGE , CHURCH DENNIS , CAMPS MONTSERRAT , RUECKLE THOMAS , GOTTELAND JEAN-PIERRE , BIAMONTE MARCO
IPC分类号： A61K31/4525 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/519 , A61K31/52 , A61K31/5377 , A61K31/551 , A61K31/553 , A61P1/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D209/14 , C07D333/34 , C07D333/36 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D473/32 , C07D487/08 , C07D495/04
摘要： The present invention is related to sulfonamide derivatives of formula I 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 Ar and Ar are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R is hydrogen or a C1-C6-alkyl group, preferably H, or R forms a substituted or unsubstituted 5-6-membered saturated or non-saturated ring with Ar ; 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 within said ring is forming a bond with the sulfonyl group of formula I thus providing the sulfonamide.

7. 发明专利

HRP20020496A2 BENZAZOLE DERIVATIVES AND THEIR USE AS JNK MODULATORS 未知
公开(公告)号：HRP20020496A2
公开(公告)日：2006-03-31
申请号：HRP20020496
申请日：2002-06-06
申请人： APPLIED RESEARCH SYSTEMS
发明人： GOTTELAND JEAN PIERRE , GAILLARD PASCALE , CAMPS MONTSERRAT , CHURCH DENNIS , HALAZY SERGE
IPC分类号： C07D417/06 , A61K31/506 , A61K31/517 , A61K31/5377 , A61P1/04 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/06 , C07D277/64 , C07D403/06 , C07D413/06 , C07D417/14 , C07D521/00
摘要： The present invention is related to benzazole derivatives according to formula I wherein X is O, S or NR , G is selected from the group comprising or consisting of unsubstituted or substituted aryl or heteroaryl substituents, unsubstituted or substituted 3-8-membered saturated or unsaturated ring systems containing at least one heteroatom selected from N, O or S; said 3-8-membered ring system may be fused with a substituted or unsubstituted aryl or heteroaryl system thus providing a bicyclic system; notably for use as pharmaceutically active compounds. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to certain novel benzazole derivatives of formula I.

8. 发明专利

NO20060573L 未知
公开(公告)号：NO20060573L
公开(公告)日：2006-02-03
申请号：NO20060573
申请日：2006-02-03
申请人： APPLIED RESEARCH SYSTEMS
发明人： CHURCH DENNIS , RUECKLE THOMAS , SHAW JEFFREY , COVINI DAVID
IPC分类号： A61K31/427 , C07D413/06 , A61P29/00 , A61P37/00 , C07D417/06 , C07D417/14
摘要： The present invention is related to 2-imino-azolinone-vinyl fused-benzene derivatives of Formula (1) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

10. 发明专利

DE60024115D1 未知
公开(公告)号：DE60024115D1
公开(公告)日：2005-12-22
申请号：DE60024115
申请日：2000-09-28
申请人： APPLIED RESEARCH SYSTEMS
发明人： ARKINSTALL STEPHEN , HALAZY SERGE , CHURCH DENNIS , CAMPS MONTSERRAT , RUECKLE THOMAS , GOTTELAND JEAN-PIERRE , BIAMONTE MARCO
IPC分类号： A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/519 , A61K31/52 , A61K31/5377 , A61K31/551 , A61K31/553 , A61P1/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D333/34 , C07D333/36 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D473/32 , C07D487/08 , C07D495/04
摘要： The present invention is related to sulfonamide derivatives of formula I 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 Ar and Ar are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R is hydrogen or a C1-C6-alkyl group, preferably H, or R forms a substituted or unsubstituted 5-6-membered saturated or non-saturated ring with Ar ; 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 within said ring is forming a bond with the sulfonyl group of formula I thus providing the sulfonamide.

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