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1. 发明申请

WO2010072599A1 DIHYDROPYRIDONE UREAS AS P2X7 MODULATORS 审中-公开
标题翻译：二氢吡啶酮作为P2X7调节剂
公开(公告)号：WO2010072599A1
公开(公告)日：2010-07-01
申请号：PCT/EP2009/067032
申请日：2009-12-14
申请人： F. HOFFMANN-LA ROCHE AG , BROTHERTON-PLEISS, Christine E. , CAROON, Joan Marie , LOPEZ-TAPIA, Francisco Javier , NITZAN, Dov , WALKER, Keith Adrian Murray
发明人： BROTHERTON-PLEISS, Christine E. , CAROON, Joan Marie , LOPEZ-TAPIA, Francisco Javier , NITZAN, Dov , WALKER, Keith Adrian Murray
IPC分类号： C07D211/86 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/4422 , A61K31/47 , A61P11/00 , A61P11/06 , A61P19/02 , A61P29/00
CPC分类号： C07D211/86 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, n, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中m，n，R 1，R 2，R 3，R 4和R 5如本文所定义。还公开了制备化合物和使用该化合物治疗与P2X7嘌呤能受体有关的疾病的方法。

2. 发明申请

WO2010072597A1 DIHYDROPYRIDONE AMIDES AS P2X7 MODULATORS 审中-公开
标题翻译：二氢吡啶酮作为P2X7调节剂
公开(公告)号：WO2010072597A1
公开(公告)日：2010-07-01
申请号：PCT/EP2009/067026
申请日：2009-12-14
申请人： F. HOFFMANN-LA ROCHE AG , BERGER, Jacob , CAROON, Joan Marie , KRAUSS, Nancy Elisabeth , LOPEZ-TAPIA, Francisco Javier , WALKER, Keith Adrian Murray , ZHAO, Shu-Hai
发明人： BERGER, Jacob , CAROON, Joan Marie , KRAUSS, Nancy Elisabeth , LOPEZ-TAPIA, Francisco Javier , WALKER, Keith Adrian Murray , ZHAO, Shu-Hai
IPC分类号： C07D401/12 , C07D413/12 , A61K31/44
CPC分类号： C07D401/12 , C07D413/12
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 and R a are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，n，R1，R2，R3，R4，R5和Ra如本文所定义。还公开了制备化合物和使用该化合物治疗与P2X7嘌呤能受体有关的疾病的方法。

3. 发明申请

WO2010003084A3 PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：WO2010003084A3
公开(公告)日：2010-03-25
申请号：PCT/US2009049558
申请日：2009-07-02
申请人： MEMORY PHARM CORP , ROCHE PALO ALTO LLC , HOPPER ALLEN T , CAROON JOAN MARIE , CHIN ELBERT , DUNN ROBERT , LABADIE SHARADA SHENVI , LI JIM , SCHUMACHER RICHARD ALLEN , TALAMAS FRANCISCO XAVIER
发明人： HOPPER ALLEN T , CAROON JOAN MARIE , CHIN ELBERT , DUNN ROBERT , LABADIE SHARADA SHENVI , LI JIM , SCHUMACHER RICHARD ALLEN , TALAMAS FRANCISCO XAVIER
IPC分类号： C07D257/08 , A61K31/395 , A61K31/41 , A61P25/28
CPC分类号： C07D277/28 , C07C217/92 , C07C229/60 , C07C255/58 , C07C2601/04 , C07C2601/08 , C07D213/36 , C07D213/64 , C07D213/74 , C07D231/12 , C07D237/08 , C07D239/26 , C07D263/32 , C07D307/20 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3, and R4 are as defined herein.
摘要翻译：通过新化合物，例如N-取代的苯胺和二苯胺类似物实现PDE4抑制。本发明的化合物具有式I：其中R 1，R 2，R 3和R 4如本文所定义。

4. 发明申请

WO1993014086A1 SUBSTITUTED 1-ISOQUINOLONE DERIVATIVES AS ANGIOTENSIN II ANTAGONISTS 审中-公开
标题翻译：取代的1-异喹啉酮衍生物作为ANGIOTENSIN II拮抗剂
公开(公告)号：WO1993014086A1
公开(公告)日：1993-07-22
申请号：PCT/US1993000188
申请日：1993-01-15
申请人： SYNTEX (U.S.A.) INC. , FISHER, Lawrence, E. , CAROON, Joan, M. , STABLER, Stephen, R. , CLARK, Robin, D.
发明人： SYNTEX (U.S.A.) INC.
IPC分类号： C07D401/10
CPC分类号： C07D221/20 , C07D217/24 , C07D401/10 , C07D409/10
摘要： 1-Isoquinolone derivatives and related compounds according to formula (I) wherein, Y is selected from the group consisting of H, OH, lower alkoxy, and halo; X is selected from the group consisting of H, lower alkyl acid, lower alkyl ester, and lower alkyl; and R is selected from the group consisting of H, alkenyl, lower alkyl, lower cycloalkyl, unsubstituted or substituted 3-spiro-1H-indane of structure (II) wherein R is H, OH, lower alkyl, lower alkoxy or halo, and 3-spiro-cycloalkyl of structure (III) wherein n is an integer from zero to six, provided that when R is spiro- X is H, or a pharmaceutically acceptable salt thereof, with the proviso that when R is spiro-, X is H, and when R is H, alkenyl, lower alkyl or lower cycloalkyl substituted at the 3-position of the isoquinolone moiety and X is H or lower alkyl, the (2"-1H--tetrazol-5-yl)biphenyl-4'-ylmethyl group cannot be at the 2(N) position, are useful as angiotensin II receptor antagonists. Also disclosed are methods of synthesis, intermediates, pharmaceutical formulations and methods of treatment.
摘要翻译： 1-异喹诺酮衍生物和根据式（I）的相关化合物，其中Y选自H，OH，低级烷氧基和卤素; X选自H，低级烷基酸，低级烷基酯和低级烷基; 和R 1选自H，烯基，低级烷基，低级环烷基，结构（II）的未取代或取代的3-螺-1H-二氢化茚，其中R 2是H，OH，低级烷基，低级烷氧基或卤素，和结构（III）的3-螺环烷基，其中n为0至6的整数，条件是当R 1为螺环X为H时，或其药学上可接受的盐，条件是当R 1为螺 - ，X为H时，当R 1为H时，在异喹啉酮部分的3位被取代的链烯基，低级烷基或低级环烷基，X为H或低级烷基，（ 2“-1H-四唑-5-基）联苯-4'-基甲基不能在2（N）位，可用作血管紧张素II受体拮抗剂。还公开了合成方法，中间体，药物制剂和方法的治疗。

5. 发明申请

WO2011012592A1 DIHYDROPYRIMIDONE AMIDES AS P2X7 MODULATORS 审中-公开
标题翻译： DIHYDROPYRIMIDONE AMIDES作为P2X7调节剂
公开(公告)号：WO2011012592A1
公开(公告)日：2011-02-03
申请号：PCT/EP2010/060830
申请日：2010-07-27
申请人： F. HOFFMANN-LA ROCHE AG , BROTHERTON-PLEISS, Christine E. , CAROON, Joan Marie , LOPEZ-TAPIA, Francisco Javier , WALKER, Keith Adrian Murray
发明人： BROTHERTON-PLEISS, Christine E. , CAROON, Joan Marie , LOPEZ-TAPIA, Francisco Javier , WALKER, Keith Adrian Murray
IPC分类号： C07D239/22 , C07D401/12 , C07D403/12 , A61K31/513 , A61P3/00 , A61P11/00
CPC分类号： C07D403/12 , C07D239/22 , C07D401/12
摘要： Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R a and R b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中m，n，R 1，R 2，R 3，R 4，R 5，R a和R b如本文所定义。还公开了制备化合物和使用该化合物治疗与P2X7嘌呤能受体有关的疾病的方法。

6. 发明申请

WO2006135828A3 TRISUBSTITUTED AMINES AS PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
标题翻译：作为磷酸二酯酶4抑制剂的三唑胺
公开(公告)号：WO2006135828A3
公开(公告)日：2007-04-26
申请号：PCT/US2006022655
申请日：2006-06-09
申请人： MEMORY PHARM CORP , HOFFMANN LA ROCHE , TALAMAS FRANCISCO XAVIER , CAROON JOAN MARIE , DUNN ROBERT , HOPPER ALLEN , KUESTER ERIC , SCHUMACHER RICHARD , TEHIM ASHOK
发明人： TALAMAS FRANCISCO XAVIER , CAROON JOAN MARIE , DUNN ROBERT , HOPPER ALLEN , KUESTER ERIC , SCHUMACHER RICHARD , TEHIM ASHOK
IPC分类号： C07D211/58 , A61K31/4427 , A61K31/4468 , A61P29/00 , C07D401/12 , C07D403/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
CPC分类号： C07D211/58 , C07D401/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： PDE4 inhibition is achieved by novel compounds,' e.g., N-substituted diarylamine analogs. The compounds of the present invention are of Formulas I-III; (I), (II) and (III) wherein A, B, D, E, G, J, K, R 1 , R 2 , R 3 , R 4 , R 11 , R 12 , R 13 , R 14 , R 21 , R 22 , R 23 and R 24 are as defined herein.
摘要翻译： PDE4抑制通过新化合物例如N-取代的二芳基胺类似物来实现。本发明的化合物是式I-III的化合物; （I），（II）和（III）其中A，B，D，E，G，J，K，R 1，R 2， 3，R 4，R 11，R 12，R 13，R 12， 14，R 21，R 22，R 23和R 24如本文所定义。

7. 发明申请

WO2010072605A1 DIHYDROPYRIDONE AMIDES AS P2X7 MODULATORS 审中-公开
标题翻译：二氢吡啶酮作为P2X7调节剂
公开(公告)号：WO2010072605A1
公开(公告)日：2010-07-01
申请号：PCT/EP2009/067054
申请日：2009-12-14
申请人： F. HOFFMANN-LA ROCHE AG , BERGER, Jacob , CAROON, Joan Marie , LOPEZ-TAPIA, Francisco Javier , NITZAN, Dov , WALKER, Keith Adrian Murray , ZHAO, Shu-Hai
发明人： BERGER, Jacob , CAROON, Joan Marie , LOPEZ-TAPIA, Francisco Javier , NITZAN, Dov , WALKER, Keith Adrian Murray , ZHAO, Shu-Hai
IPC分类号： C07D211/86 , C07D405/12 , A61K31/4412 , A61K31/4418
CPC分类号： C07D211/86 , C07D405/12
摘要： Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 and R a are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中m，n，R1，R2，R3，R4，R5和Ra如本文所定义。还公开了制备化合物和使用该化合物治疗与P2X7嘌呤能受体有关的疾病的方法。

8. 发明申请

WO2010003084A2 PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：WO2010003084A2
公开(公告)日：2010-01-07
申请号：PCT/US2009/049558
申请日：2009-07-02
申请人： MEMORY PHARMACEUTICALS CORPORATION , ROCHE PALO ALTO LLC , HOPPER, Allen, T. , CAROON, Joan, Marie , CHIN, Elbert , DUNN, Robert , LABADIE, Sharada, Shenvi , LI, Jim , SCHUMACHER, Richard, Allen , TALAMAS, Francisco, Xavier
发明人： HOPPER, Allen, T. , CAROON, Joan, Marie , CHIN, Elbert , DUNN, Robert , LABADIE, Sharada, Shenvi , LI, Jim , SCHUMACHER, Richard, Allen , TALAMAS, Francisco, Xavier
IPC分类号： C07D257/08 , A61K31/395 , A61K31/41 , A61P25/28
CPC分类号： C07D277/28 , C07C217/92 , C07C229/60 , C07C255/58 , C07C2601/04 , C07C2601/08 , C07D213/36 , C07D213/64 , C07D213/74 , C07D231/12 , C07D237/08 , C07D239/26 , C07D263/32 , C07D307/20 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R 1 , R 2 , R 3 , and R 4 are as defined herein.
摘要翻译：通过新化合物，例如N-取代的苯胺和二苯胺类似物来实现PDE4的抑制。本发明的化合物具有式I：其中R 1，R 2，R 3和R 4如本文所定义。

9. 发明申请

WO2007051735A1 ARYLSULFONYLCHROMANS AS 5-HT6 INHIBITORS INDOLYLMALEIMIDE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： ARYLSULFONYLCHROMANS作为蛋白激酶抑制剂的5-HT6抑制剂吲哚酰亚胺衍生物
公开(公告)号：WO2007051735A1
公开(公告)日：2007-05-10
申请号：PCT/EP2006/067732
申请日：2006-10-24
申请人： F. HOFFMANN-LA ROCHE AG , BERGER, Jacob , CAROON, Joan, Marie , LOPEZ-TAPIA, Francisco, Javier , LOWRIE, JR., Lee, Edwin , NITZAN, Dov , ZHAO, Shu-Hai
发明人： BERGER, Jacob , CAROON, Joan, Marie , LOPEZ-TAPIA, Francisco, Javier , LOWRIE, JR., Lee, Edwin , NITZAN, Dov , ZHAO, Shu-Hai
IPC分类号： C07D311/22 , C07D311/58 , C07D405/06 , A61K31/353
CPC分类号： C07D311/22 , C07D311/58 , C07D405/06
摘要： Compounds of the formula (I): formula (I), wherein m, n, p, X, Ar, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Methods of making the compounds and using the compounds for treatment of 5-HT6 receptor- mediated diseases are disclosed.
摘要翻译：式（I）化合物：式（I）其中m，n，p，X，Ar，R 1，R 2，R 3， R 4，R 4和R 5如本文所定义。公开了制备化合物和使用该化合物治疗5-HT6受体介导的疾病的方法。

10. 发明申请

WO2006135828A2 PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：WO2006135828A2
公开(公告)日：2006-12-21
申请号：PCT/US2006/022655
申请日：2006-06-09
申请人： MEMORY PHARMACEUTICALS CORPORATION , F. HOFFMANN-LA ROCHE AG , TALAMAS, Francisco, Xavier , CAROON, Joan, Marie , DUNN, Robert , HOPPER, Allen , KUESTER, Eric , SCHUMACHER, Richard , TEHIM, Ashok
发明人： TALAMAS, Francisco, Xavier , CAROON, Joan, Marie , DUNN, Robert , HOPPER, Allen , KUESTER, Eric , SCHUMACHER, Richard , TEHIM, Ashok
IPC分类号： C07D211/58 , C07D401/12 , C07D403/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/4427 , A61K31/4468 , A61P29/00
CPC分类号： C07D211/58 , C07D401/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： PDE4 inhibition is achieved by novel compounds,' e.g., N-substituted diarylamine analogs. The compounds of the present invention are of Formulas I-III; (I), (II) and (III) wherein A, B, D, E, G, J, K, R 1 , R 2 , R 3 , R 4 , R 11 , R 12 , R 13 , R 14 , R 21 , R 22 , R 23 and R 24 are as defined herein.
摘要翻译：新的化合物，例如N-取代的二芳基胺类似物可以实现PDE4抑制。本发明的化合物是式I-III的化合物; （I），（II）和（III）其中A，B，D，E，G，J，K，R 1，R 2， R 4，R 4，R 11，R 12，R 13，R 12， 14，R 21，R 22，R 23和R 24如本文所定义。

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