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1. 发明申请

WO2013000994A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：WO2013000994A1
公开(公告)日：2013-01-03
申请号：PCT/EP2012/062544
申请日：2012-06-28
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , BEHL, Berthold , LAPLANCHE, Loic , DINGES, Jürgen , JAKOB, Clarissa
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , BEHL, Berthold , LAPLANCHE, Loic , DINGES, Jürgen , JAKOB, Clarissa
IPC分类号： C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：本发明涉及新的羧酰胺化合物，含有它们的药物组合物及其在治疗中的用途。所述化合物具有有价值的治疗性质，并且特别适用于治疗或控制选自神经障碍和精神障碍的医学病症，用于改善与此类疾病相关的症状并降低此类疾病的风险。

2. 发明申请

WO2005095387A1 TRICYCLIC PYRAZOLE KINASE INHIBITORS 审中-公开
标题翻译： TRICYCLIC PYRAZOZKINASE INHIBITORS
公开(公告)号：WO2005095387A1
公开(公告)日：2005-10-13
申请号：PCT/US2005/009900
申请日：2005-03-24
申请人： ABBOTT LABORATORIES , MAKOTO, Aoyama , ARNOLD, Lee, D. , DINGES, Jürgen , DIXON, Richard, W. , DJURIC, Stevan, W. , ERICSSON, Anna, M. , FISCHER, Kimba , GASIECKI, Alan, F. , GRACIAS, Vijaya, J. , HOLMS, James, H. , MICHAELIDES, Michael, R. , MUCKEY, Melanie, A. , RAFFERTY, Paul , STEINMAN, Douglas, H. , WADA, Carol, K. , XIA, Zhiren , AKRITOPOULOU-ZANZE, Irini , ZHANG, Henry, Q.
发明人： MAKOTO, Aoyama , ARNOLD, Lee, D. , DINGES, Jürgen , DIXON, Richard, W. , DJURIC, Stevan, W. , ERICSSON, Anna, M. , FISCHER, Kimba , GASIECKI, Alan, F. , GRACIAS, Vijaya, J. , HOLMS, James, H. , MICHAELIDES, Michael, R. , MUCKEY, Melanie, A. , RAFFERTY, Paul , STEINMAN, Douglas, H. , WADA, Carol, K. , XIA, Zhiren , AKRITOPOULOU-ZANZE, Irini , ZHANG, Henry, Q.
IPC分类号： C07D409/04
CPC分类号： C07D471/04 , C07D231/54 , C07D409/04 , C07D409/14 , C07D413/14 , C07D495/04 , C07D495/14
摘要： Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：本发明的化合物可用于抑制蛋白酪氨酸激酶。还公开了制备化合物，含有化合物的组合物和使用该化合物的处理方法的方法。

3. 发明申请

WO2013068489A1 HETEROCYCLIC CARBOXAMIDES USEFUL AS INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：用作磷酸二酯酶类型10A的抑制剂的杂环碳酰胺
公开(公告)号：WO2013068489A1
公开(公告)日：2013-05-16
申请号：PCT/EP2012/072175
申请日：2012-11-08
申请人： ABBOTT GMBH & CO. KG , ABBVIE INC.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , DINGES, Jürgen , JAKOB, Clarissa
IPC分类号： C07D217/26 , C07D237/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , A61K31/472 , A61K31/502 , A61K31/4375 , A61P25/00
CPC分类号： C07D217/26 , A61K31/47 , C07D217/24 , C07D237/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/08 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07D471/04
摘要： Novel inhibitor compounds of phosphodiesterase type 10A The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：磷酸二酯酶10A的新型抑制剂化合物本发明涉及作为10A型磷酸二酯酶抑制剂的化合物及其用于制备药物的用途，因此其适用于治疗或控制选自神经障碍和精神障碍的医学病症，用于改善与这种障碍相关的症状并降低这种障碍的风险。

4. 发明申请

WO2013068470A1 INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：磷酸二酯酶类型10A的抑制剂
公开(公告)号：WO2013068470A1
公开(公告)日：2013-05-16
申请号：PCT/EP2012/072150
申请日：2012-11-08
申请人： ABBOTT GMBH & CO. KG , ABBVIE INC.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , TURNER, Sean , BEHL, Berthold , LAPLANCHE, Loic , DINGES, Jürgen , JAKOB, Clarissa , BLACK, Lawrence A.
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D519/00 , A61K31/519 , A61P25/00
CPC分类号： C07D519/00 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to novel compounds of the formula (I) which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Q is O or S, X 1 is N or CH, X 2 is N or C-R 7 ; X 3 is O, S, -X 4 =C(R 8 )-, where C(R 8 ) is bound to the carbon atom which carries R 2 , or -X 5 =C(R 9 )-, where X 5 is bound to the carbon atom which carries R 2 ; X 4 is N or C-R 9 ; X 5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R 1 is selected inter alia from hydrogen, halogen, OH, C 1 -C 4 -alkyl, trimethylsilyl, C 1 -C 4 -alkylsulfanyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 4 - alkoxy, C 1 -C 4 -alkoxy-C 1 -C 4 -alkoxy, the moiety Y 1 -Cyc 1 ; R 2 is selected inter alia from hydrogen, halogen, OH, C 1 -C 4 -alkyl, trimethylsilyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 1 -C 4 - alkoxy-C 1 -C 4 -alkoxy, C 2 -C 4 -alkenyloxy, etc; A represents one of the following groups A 1 , A 2 , A 3 , A 4 or A 5 : where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R 3 to R 9 , R 3e , R 3f , A', Y 1 and Cyc 1 are defined in the claims.
摘要翻译：本发明涉及作为10A型磷酸二酯酶抑制剂的式（I）化合物及其用于制备药物的用途，因此其适用于治疗或控制选自神经障碍和精神障碍的医学病症，用于改善与这种障碍相关的症状并降低这种障碍的风险。其中Q为O或S，X1为N或CH，X2为N或C-R7; X3是O，S，-X4 = C（R8） - ，其中C（R8）与携带R2的碳原子结合，或-X5 = C（R9） - ，其中X5与携带的碳原子结合 R2; X4是N或C-R9; X5是N; Het选自任选取代的苯基，单环杂芳基和稠合双环杂芳基; R1特别是选自氢，卤素，OH，C 1 -C 4烷基，三甲基甲硅烷基，C 1 -C 4烷基硫烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 4烷氧基 - C1-C4-烷氧基，Y1-Cyc1部分; R2特别是选自氢，卤素，OH，C 1 -C 4 - 烷基，三甲基甲硅烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷氧基-C 1 -C 4烷氧基， C2-C4-烯氧基等; A代表以下组A1，A2，A3，A4或A5：其中*表示分别与Het和氮原子相连的点; 并且在权利要求中定义R3至R9，R3e，R3f，A'，Y1和Cyc1。

5. 发明申请

WO2004032908A2 METHOD OF INHIBITING ANGIOGENESIS 审中-公开
标题翻译：抑制血管生成的方法
公开(公告)号：WO2004032908A2
公开(公告)日：2004-04-22
申请号：PCT/US2003/031220
申请日：2003-10-02
申请人： ABBOTT LABORATORIES
发明人： HAVIV, Fortuna , BRADLEY, Michael, F. , DINGES, Jürgen , SAUER, Daryl, R. , HENKIN, Jack
IPC分类号： A61K31/00
CPC分类号： C07D213/82 , A61K31/455 , C07D401/04 , C07D405/04 , C07D405/12 , C07D409/04
摘要： Compounds having the formula are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds.
摘要翻译：具有下式的化合物是血管生成抑制剂。还公开了含有该化合物的组合物，制备该化合物的方法以及使用该化合物的治疗方法。

6. 发明申请

WO2003086398A1 AMINOCARBONYL SUBSTITUTED PYRIDINES, PYRIDAZINES, PYRIMIDINES, PYRAZINES AND TRIAZINES HAVING ANTIANGIOGENIC ACTIVITY 审中-公开
标题翻译：氨基羰基取代的吡啶类，吡咯烷酮，吡咯烷酮，具有抗生素活性的吡啶类和三嗪类
公开(公告)号：WO2003086398A1
公开(公告)日：2003-10-23
申请号：PCT/US2003/011066
申请日：2003-04-03
申请人： ABBOTT LABORATORIES
发明人： HAVIV, Fortuna , BRADLEY, Michael, F. , HENKIN, Jack , DINGES, Jürgen , SAUER, Daryl, R. , KOLACZKOWSKI, Lawrence , VASUDEVAN, Anil , PARK, David, C.
IPC分类号： A61K31/455
CPC分类号： C07D213/81 , A61K31/4439 , A61K31/4545 , A61K31/4747 , A61K31/496 , A61K31/541 , A61K31/551 , C07D213/82 , C07D239/28 , C07D241/24 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D491/10
摘要： Compounds having the formula (I) are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds. A is selected from the group consisting of pyridine, pyridine N-oxide, pyridazine, pyrimidine. pyrazine, and triazine; R 1 and R 2 , together with the nitrogen atom to which they are attached, form a five - to eight - membered ring containing an additional zero to two heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur; wherein the ring can be optionally substituted with one, two, or three substituents independently selected from the group consisting of alkoxyalkyl, alkoxycarbonyl, alkyl, unsubstituted alkylcarbonyl, amino, aminocarbonyl, aryl, arylalkoxycarbonyl, wylalkyl, carboxy, formyl, haloalkyl, heterocycle, (heterocycle)alkyl, hydroxy, hydroxyalkoxyalkyl, hydroxyalkyl, and spiroheterocycle; R 3 at each occurance is independently selected from the group consisting 'of alkenyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, alkyl, unsubstituted alkylcarbonyl, alkylsulfanyl, amino, aminocarbonyl, aryl, arylalkyl, aryloxy, cyano, cyanoalkyl, cyanoalkyl, (cycloalkyl)alkyl, halo, haloalkyl, heterocycle, hydroxy, hydroxyalkyl, and nitro; X is selected from the group consisting of O, S, and CH 2 ; and m is 0-4.
摘要翻译：具有式（I）的化合物是血管发生抑制剂。还公开了含有化合物的组合物，制备化合物的方法和使用该化合物的治疗方法。 A选自吡啶，吡啶N-氧化物，哒嗪，嘧啶。吡嗪和三嗪; R 1和R 2与它们所连接的氮原子一起形成含有另外的0至2个选自氮，氧和硫的杂原子的五元至八元环; 其中所述环可以任选被一个，两个或三个独立地选自烷氧基烷基，烷氧基羰基，烷基，未取代的烷基羰基，氨基，氨基羰基，芳基，芳基烷氧基羰基，二烷基，羧基，甲酰基，卤代烷基，杂环，（杂环）烷基，羟基，羟基烷氧基烷基，羟烷基和螺杂环; R 3各自独立地选自：烯基，烷氧基，烷氧基烷基，烷氧基羰基，烷基，未取代的烷基羰基，烷基硫烷基，氨基，氨基羰基，芳基，芳烷基，芳氧基，氰基，氰基烷基，氰基烷基，（环烷基）烷基，卤素，卤代烷基，杂环，羟基，羟基烷基和硝基; X选自O，S和CH 2; m为0-4。

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