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1. 发明申请

WO2007131153A2 METHODS FOR THE PREPARATION OF PYRAZOLE-CONTAINING COMPOUNDS 审中-公开
标题翻译：制备含吡唑化合物的方法
公开(公告)号：WO2007131153A2
公开(公告)日：2007-11-15
申请号：PCT/US2007/068210
申请日：2007-05-04
申请人： JANSSEN PHARMACEUTICA N.V. , DENG, Xiaohu , LIANG, Jimmy,T. , MANI, Neelakandha
发明人： DENG, Xiaohu , LIANG, Jimmy,T. , MANI, Neelakandha
IPC分类号： C07D317/16 , C07D405/06 , C07D487/04
CPC分类号： C07D487/04 , C07D317/16 , C07D405/06
摘要： The present invention is directed to novel processes for the preparation of fused pyrazole compounds, useful for the treatment of disorders and conditions mediated by serotonin receptor activity.
摘要翻译：本发明涉及制备用于治疗5-羟色胺受体活性介导的病症和病症的稠合吡唑化合物的新方法。

2. 发明申请

WO2014152604A1 P2X7 MODULATORS 审中-公开
标题翻译： P2X7调制器
公开(公告)号：WO2014152604A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/027522
申请日：2014-03-14
申请人： JANSSEN PHARMACEUTICA NV , ALCAZAR VACA, Manuel Jesus , ALLISON, Brett, D. , ANDRES GIL, Jose Ignacio , CHROVIAN, Christa, C. , COATE, Heather, R. , DE ANGELIS, Meri , DENG, Xiaohu , DVORAK, Curt, A. , GELIN, Christine, F. , LETAVIC, Michael, A. , LIANG, Jimmy, T. , MANI, Neelakandha, S. , RECH, Jason, C. , SAVALL, Brad, M. , SOYODE-JOHNSON, Akinola , STENNE, Brice, M. , SWANSON, Devin, M. , WALL, Jessica, L.
发明人： ALCAZAR VACA, Manuel Jesus , ALLISON, Brett, D. , ANDRES GIL, Jose Ignacio , CHROVIAN, Christa, C. , COATE, Heather, R. , DE ANGELIS, Meri , DENG, Xiaohu , DVORAK, Curt, A. , GELIN, Christine, F. , LETAVIC, Michael, A. , LIANG, Jimmy, T. , MANI, Neelakandha, S. , RECH, Jason, C. , SAVALL, Brad, M. , SOYODE-JOHNSON, Akinola , STENNE, Brice, M. , SWANSON, Devin, M. , WALL, Jessica, L.
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P37/02
CPC分类号： C07D471/04 , A61K31/497 , C07B2200/07 , C07D401/14 , C07F7/0812 , Y02A50/414
摘要： The present invention is directed to compounds of Formulas (I, la, lla and IIb). The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, la, lla and IIb). Methods of making and using the compounds of Formulas (I, la, lla and IIb) are also within the scope of the invention.
摘要翻译：本发明涉及式（I，Ia，11a和IIb）的化合物。本发明还涉及包含式（I，Ia，11a和IIb）化合物的药物组合物。制备和使用式（I，Ia，11a和IIb）化合物的方法也在本发明的范围内。

3. 发明申请

WO2009126806A3 THIAZOLOPYRIDIN-2-YLOXY-PHENYL AND THIAZOLOPYRAZIN-2-YLOXY-PHENYL AMINES AS MODULATORS OF LEUKOTRIENE A4 HYDROLASE 审中-公开
公开(公告)号：WO2009126806A3
公开(公告)日：2009-10-15
申请号：PCT/US2009/040070
申请日：2009-04-09
申请人： JANSSEN PHARMACEUTICA NV , BACANI, Genesis, M. , BROGGINI, Diego , CHEUNG, Eugene, Y. , CHROVIAN, Christa, C. , DENG, Xiaohu , FOURINE, Anne, M. , GOMEZ, Laurent , GRICE, Cheryl, A. , KEARNEY, Aaron, M. , LANDRY-BAYLE, Adrienne, M. , LEE-DUTRA, Alice , LIANG, Jimmy, T. , LOCHNER, Susanne , MANI, Neelakandha, S. , SANTILLAN, Alejandro , SAPPEY, Kathleen, C. , SEPASSI, Kia , TANIS, Virginia, M. , WICKBOLDT, Alvah, T. , WIENER, John, J. M. , ZINSER, Hartmut
发明人： BACANI, Genesis, M. , BROGGINI, Diego , CHEUNG, Eugene, Y. , CHROVIAN, Christa, C. , DENG, Xiaohu , FOURINE, Anne, M. , GOMEZ, Laurent , GRICE, Cheryl, A. , KEARNEY, Aaron, M. , LANDRY-BAYLE, Adrienne, M. , LEE-DUTRA, Alice , LIANG, Jimmy, T. , LOCHNER, Susanne , MANI, Neelakandha, S. , SANTILLAN, Alejandro , SAPPEY, Kathleen, C. , SEPASSI, Kia , TANIS, Virginia, M. , WICKBOLDT, Alvah, T. , WIENER, John, J. M. , ZINSER, Hartmut
IPC分类号： C07D498/04 , A61K31/4985
摘要： Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.

4. 发明申请

WO2009102937A1 PROCESSES FOR THE PREPARATION OF CARBON-LINKED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S 审中-公开
标题翻译：制备CATHEPSIN的碳链烷基四氢吡喃 - 吡啶调节剂的方法
公开(公告)号：WO2009102937A1
公开(公告)日：2009-08-20
申请号：PCT/US2009/034031
申请日：2009-02-13
申请人： SUNESIS PHARMACEUTICALS, INC. , MANI, Neelakandha, S. , LIANG, Jimmy, T. , DENG, Xiaohu
发明人： MANI, Neelakandha, S. , LIANG, Jimmy, T. , DENG, Xiaohu
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Method of making carbon-linked tetrahydro-pyrazolo-pyridine compounds of the following Formula (I) and pharmaceutically acceptable salts thereof: comprising reacting a compound of formula (IX): with a compound of formula (X): to form a compound of Formula (I); wherein: R 1 and R 7 taken together with the nitrogen to which they are attached form a morpholine ring, unsubstituted or substituted with one or two methyl substituents; R 3 is H or OH; R 4 is -SO 2 CH 3 , -CONH 2 , or -COCONH 2 ; R 5 is H or methyl; R 6 is a benzyl group, unsubstituted or substituted with one or two substituents independently selected from the group consisting of C 1-4 alkyl, CF 3 , halo, OH, -OC 1-4 alkyl, -OCF 3 , -OCHF 2 , NR dd R ee , -CO 2 C 1-4 alkyl, -SC 1-4 alkyl, and -SO 2 C 1-4 alkyl; where R dd and R ee are each independently H or C 1-4 alkyl; R 7 is H, fluoro, or chloro; and LG 1 is iodide, bromide, or trifluoromethanesulfonate. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.
摘要翻译：制备下式（I）的碳 - 连四氢 - 吡唑并 - 吡啶化合物及其药学上可接受的盐的方法：包括使式（Ⅸ）化合物与式（Ⅹ）化合物反应：使式（一世）; 其中：R 1和R 7与它们所连接的氮一起形成吗啉环，未被取代或被一个或两个甲基取代基取代; R3是H或OH; R4是-SO2CH3，-CONH2或-COCONH2; R5是H或甲基; R6是未取代的或被一个或两个取代基取代的苄基，所述取代基独立地选自C 1-4烷基，CF 3，卤素，OH，-OC 1-4烷基，-OCF 3，-OCHF 2，NR d R e，-CO 2 C 1-4烷基， SC1-4烷基和-SO2C1-4烷基; 其中Rdd和Ree各自独立地为H或C 1-4烷基; R7是H，氟或氯; 和LG1是碘化物，溴化物或三氟甲磺酸盐。这些化合物可用于治疗由组织蛋白酶S活性介导的疾病状态，病症和病症的药物组合物和方法，例如银屑病，疼痛，多发性硬化，动脉粥样硬化和类风湿性关节炎。

5. 发明申请

WO2006039383A2 SYNTHESIS BY CHIRAL DIAMINE-MEDIATED ASYMMETRIC ALKYLATION 审中-公开
标题翻译：手性二胺介导的不对称烷基化合成
公开(公告)号：WO2006039383A2
公开(公告)日：2006-04-13
申请号：PCT/US2005034972
申请日：2005-09-28
申请人： JANSSEN PHARMACEUTICA NV , DENG XIAOHU , MANI NEELAKANDHA
发明人： DENG XIAOHU , MANI NEELAKANDHA
IPC分类号： C07D295/00
CPC分类号： C07D401/06 , C07D203/10 , C07D203/18 , C07D205/04 , C07D207/08 , C07D207/48 , C07D211/22 , C07D211/96 , C07D223/04 , C07D225/02
摘要： Chiral synthesis from an achiral starting material by chiral diaminemediated, such as sparteine-mediated, intermolecular asymmetric alkylation with a strained cyclic ether in the presence of a Lewis acid.
摘要翻译：通过手性二胺介导的非手性起始材料的手性合成，例如在路易斯酸存在下用张力环介导的分子间介导的分子间不对称烷基化。

6. 发明申请

WO2009105220A1 ARYL-HYDROXYETHYLAMINO-PYRIMIDINES AND TRIAZINES AS MODULATORS OF FATTY ACID AMIDE HYDROLASE 审中-公开
标题翻译：作为脂肪酸酰胺水解酶的调节剂的ARYL-羟基乙酰氨基吡啶和三嗪
公开(公告)号：WO2009105220A1
公开(公告)日：2009-08-27
申请号：PCT/US2009/001043
申请日：2009-02-18
申请人： JANSSEN PHARMACEUTICA N.V. , APODACA, Richard , BREITENBUCHER, J., Guy , CHAMBERS, Alison, L. , DENG, Xiaohu , HAWRYLUK, Natalie, A. , KEITH, John, M. , MANI, Neelakandha, S. , MERIT, Jeffrey, E. , PIERCE, Joan, M. , SEIERSTAD, Mark , XIAO, Wei
发明人： APODACA, Richard , BREITENBUCHER, J., Guy , CHAMBERS, Alison, L. , DENG, Xiaohu , HAWRYLUK, Natalie, A. , KEITH, John, M. , MANI, Neelakandha, S. , MERIT, Jeffrey, E. , PIERCE, Joan, M. , SEIERSTAD, Mark , XIAO, Wei
IPC分类号： A01N43/66 , A61K31/53
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D251/22 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12
摘要： Certain aryl-hydroxyethylamino-pyrimidine and triazine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.
摘要翻译：描述了某些芳基 - 羟乙基氨基 - 嘧啶和三嗪化合物，其可用作FAAH抑制剂。这些化合物可用于治疗由脂肪酰胺水解酶（FAAH）活性介导的疾病状态，病症和病症的药物组合物和方法，例如焦虑症，疼痛，炎症，睡眠障碍，进食障碍，能量代谢紊乱，和运动障碍（例如多发性硬化）。还公开了合成这些化合物的方法。

7. 发明申请

WO2007016286A1 SYNTHESIS OF 4/5-PYRIMIDINYLIMIDAZOLES VIA SEQUENTIAL FUNCTIONALIZATION OF 2,4-DICHLOROPYRIMIDINE 审中-公开
标题翻译：通过2,4-二氯吡啶的顺序功能化合成4,5-二氨基嘧啶的合成
公开(公告)号：WO2007016286A1
公开(公告)日：2007-02-08
申请号：PCT/US2006/029280
申请日：2006-07-27
申请人： JANSSEN PHARMACEUTICA N.V. , DENG, Xiaohu , MANI, Neelakandha
发明人： DENG, Xiaohu , MANI, Neelakandha
IPC分类号： C07D239/42 , C07D403/04
CPC分类号： C07D239/42 , C07D403/04 , C07D403/14
摘要： This invention relates to methods of making pyrimidinyl-substituted imidazole compounds by sequential substitution of the 4- and 2-chloro groups of 2,4-dichloropyrimidine, nucleophilic substitution to form pyrimidinylalkyne derivatives, oxidation to the corresponding 1 ,2-diketones, and cyclocondensation reactions.
摘要翻译：本发明涉及通过4-二氯嘧啶的4-和2-氯基取代嘧啶基取代的咪唑化合物的方法，亲核取代形成嘧啶基炔衍生物，氧化成相应的1,2-二酮和环缩合反应。

8. 发明申请

WO2009126806A2 THIAZOLOPYRIDIN-2-YLOXY-PHENYL AND THIAZOLOPYRAZIN-2-YLOXY-PHENYL AMINES AS MODULATORS OF LEUKOTRIENE A4 HYDROLASE 审中-公开
标题翻译：作为水杨酸A4水解酶的调节剂的噻唑吡啶-2-氧基苯基和噻唑啉-2-甲氧基苯胺
公开(公告)号：WO2009126806A2
公开(公告)日：2009-10-15
申请号：PCT/US2009040070
申请日：2009-04-09
申请人： JANSSEN PHARMACEUTICA NV , BACANI GENESIS M , BROGGINI DIEGO , CHEUNG EUGENE Y , CHROVIAN CHRISTA C , DENG XIAOHU , FOURINE ANNE M , GOMEZ LAURENT , GRICE CHERYL A , KEARNEY AARON M , LANDRY-BAYLE ADRIENNE M , LEE-DUTRA ALICE , LIANG JIMMY T , LOCHNER SUSANNE , MANI NEELAKANDHA S , SANTILLAN ALEJANDRO , SAPPEY KATHLEEN C , SEPASSI KIA , TANIS VIRGINIA M , WICKBOLDT ALVAH T , WIENER JOHN J M , ZINSER HARTMUT
发明人： BACANI GENESIS M , BROGGINI DIEGO , CHEUNG EUGENE Y , CHROVIAN CHRISTA C , DENG XIAOHU , FOURINE ANNE M , GOMEZ LAURENT , GRICE CHERYL A , KEARNEY AARON M , LANDRY-BAYLE ADRIENNE M , LEE-DUTRA ALICE , LIANG JIMMY T , LOCHNER SUSANNE , MANI NEELAKANDHA S , SANTILLAN ALEJANDRO , SAPPEY KATHLEEN C , SEPASSI KIA , TANIS VIRGINIA M , WICKBOLDT ALVAH T , WIENER JOHN J M , ZINSER HARTMUT
IPC分类号： A61K31/437 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61P29/00 , C07D453/02 , C07D513/04 , C12N9/50
CPC分类号： C07D498/04 , C07D451/02
摘要： Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
摘要翻译：描述了噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯基胺化合物，其可用作LTA4水解酶（LTA4H）调节剂。这样的化合物可以用于调节LTA4H的药物组合物和方法以及用于治疗由LTA4水解酶活性介导的疾病状态，障碍和病症。

9. 发明申请

WO2007131153A3 METHODS FOR THE PREPARATION OF PYRAZOLE-CONTAINING COMPOUNDS 审中-公开
标题翻译：制备含吡唑化合物的方法
公开(公告)号：WO2007131153A3
公开(公告)日：2008-01-10
申请号：PCT/US2007068210
申请日：2007-05-04
申请人： JANSSEN PHARMACEUTICA NV , DENG XIAOHU , LIANG JIMMY T , MANI NEELAKANDHA
发明人： DENG XIAOHU , LIANG JIMMY T , MANI NEELAKANDHA
IPC分类号： C07D317/16 , C07D405/06 , C07D487/04
CPC分类号： C07D487/04 , C07D317/16 , C07D405/06
摘要： The present invention is directed to novel processes for the preparation of fused pyrazole compounds, useful for the treatment of disorders and conditions mediated by serotonin receptor activity (I).
摘要翻译：本发明涉及用于制备用于治疗5-羟色胺受体活性介导的病症和病症的稠合吡唑化合物的新方法（I）。

10. 发明申请

WO2006004742A3 a, ß-UNSATURATED ESTERS AND ACIDS BY STEREOSELECTIVE DEHYDRATION 审中-公开
标题翻译： a，ß不饱和酯和酸通过立体选择性脱水
公开(公告)号：WO2006004742A3
公开(公告)日：2006-12-07
申请号：PCT/US2005022910
申请日：2005-06-28
申请人： JANSSEN PHARAMCEUTICA N V , DENG XIAOHU , MANI NEELAKANDHA , MAPES CHRISTOPHER M
发明人： DENG XIAOHU , MANI NEELAKANDHA , MAPES CHRISTOPHER M
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/14
摘要： There are provided by the present invention certain pyrazole based CCK-1 receptor modulators which have the general formula: wherein Ar is an aromatic or heteroaromatic group, X is a hydrocarbon linker, Y is a bond or hydrocarbon linker and R 1 , R 2 , R 3 , R 4 and R 5 are certain organic substituents, methods for making the same, and stereoselective dehydration methods for generally making a,ß-unsaturated esters, acids and their derivatives.
摘要翻译：本发明提供了具有以下通式的某些基于吡唑的CCK-1受体调节剂：其中Ar是芳族或杂芳族基团，X是烃连接基，Y是键或烃连接基，R 1， R 2，R 3，R 4，R 4和R 5是某些有机取代基，R 1，R 2，R 4，制备相同的立体选择性脱水方法，通常制备β-不饱和酯，酸及其衍生物。

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