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1. 发明授权

US08772305B2 Substituted pyridinyl-pyrimidines and their use as medicaments 有权
标题翻译：取代的吡啶基嘧啶及其作为药物的用途
公开(公告)号：US08772305B2
公开(公告)日：2014-07-08
申请号：US13357734
申请日：2012-01-25
申请人： Georg Dahmann , Dennis Fiegen , Martin Fleck , Matthias Hoffmann , Jasna Klicic , Stephen Peter East , Spencer Charles R. Napier , John Scott
发明人： Georg Dahmann , Dennis Fiegen , Martin Fleck , Matthias Hoffmann , Jasna Klicic , Stephen Peter East , Spencer Charles R. Napier , John Scott
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
摘要翻译：本发明涉及式1的新的取代的吡啶基 - 嘧啶，其中环A是五元饱和或不饱和碳环，任选地包含一个，两个或三个彼此独立地选自N，S和O的杂原子，其中 R 1，R 2，R 4，R 3，R 5和R 6如权利要求1中所定义，并且其中环A进一步任选被一个或两个其它取代基取代，并且上述化合物的药学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物和溶剂合物。

2. 发明申请

US20130023502A1 SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS 有权
标题翻译：取代的吡啶并吡啶并作为药物使用
公开(公告)号：US20130023502A1
公开(公告)日：2013-01-24
申请号：US13357734
申请日：2012-01-25
申请人： Georg Dahmann , Dennis Fiegen , Martin Fleck , Matthias Hoffmann , Jasna Klicic , Stephen Peter East , Spencer Charles R. Napier , John Scott
发明人： Georg Dahmann , Dennis Fiegen , Martin Fleck , Matthias Hoffmann , Jasna Klicic , Stephen Peter East , Spencer Charles R. Napier , John Scott
IPC分类号： A61K31/506 , C07D409/14 , C07D401/14 , C07D413/14 , A61K31/5377 , A61K31/551 , C07D498/10 , A61K31/5386 , C07D401/04 , C07D471/04 , A61K31/553 , C07D417/14 , A61K31/541 , C07D487/04 , A61K31/56 , A61P11/02 , A61P37/08 , A61P11/06 , A61P11/00 , A61P17/00 , A61P29/00 , A61P7/06 , A61P1/04 , A61P1/16 , A61P37/00 , A61P19/02 , A61P25/00 , A61P21/04 , A61P19/10 , A61P17/06 , C07D405/14
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
摘要翻译：本发明涉及式1的新的取代的吡啶基 - 嘧啶，其中环A是五元饱和或不饱和碳环，任选地包含一个，两个或三个彼此独立地选自N，S和O的杂原子，其中 R 1，R 2，R 4，R 3，R 5和R 6如权利要求1中所定义，并且其中环A进一步任选被一个或两个其它取代基取代，并且上述化合物的药学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物和溶剂合物。

3. 发明授权

US08969568B2 Substituted naphthyridines and their use as medicaments 有权
标题翻译：取代的萘啶并用作药物
公开(公告)号：US08969568B2
公开(公告)日：2015-03-03
申请号：US13013973
申请日：2011-01-26
申请人： Matthias Hoffmann , Georg Dahmann , Dennis Fiegen , Sandra Handschuh , Jasna Klicic , Guenter Linz , Gerhard Schaenzle , Andreas Schnapp , Stephen Peter East , Michael Philip Mazanetz , Robert John Scott , Edward Walker
发明人： Matthias Hoffmann , Georg Dahmann , Dennis Fiegen , Sandra Handschuh , Jasna Klicic , Guenter Linz , Gerhard Schaenzle , Andreas Schnapp , Stephen Peter East , Michael Philip Mazanetz , Robert John Scott , Edward Walker
IPC分类号： C07D471/02 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D498/04 , C07D519/00
摘要： The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as pharmaceutical compositions containing these compounds.
摘要翻译：本发明涉及式1的新取代的萘啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂合物，其中R 1选自-O-R 3或-NR 3 R 4，R 3是C 1-6 - 烷基其被R5和R6取代，R5选自氢，支链或直链C 1-6 - 烷基，C 2-6 - 烯基，-C 1-6 - 亚烷基-O-C 1-3 - 烷基，C 1-3 - 卤代烷基， R6是环X，其中n是0或1，并且是单键或双键，并且其中A，B，D和E各自独立地选自CH 2，CH，C，N，NH，O 或S，并且其中环X通过位置A，B，D或E连接到分子，其中所述环X可任选地被一个，两个或三个残基进一步取代，每个残基各自独立地选自氧基，羟基，-C 1-3 - 烷基，-C 1-3 - 卤代烷基，-O-C 1-3 - 烷基，-C 1-3 - 链烷醇和卤素，其中R4，R2，R7，R8，R9，R10，R11和Q 可能具有的含义权利要求1中给出，以及含有这些化合物的药物组合物。

4. 发明申请

US20120028939A1 SUBSTITUTED NAPHTHYRIDINES AND THEIR USE AS MEDICAMENTS 有权
标题翻译：取代的萘啶酮及其作为药物使用
公开(公告)号：US20120028939A1
公开(公告)日：2012-02-02
申请号：US13013973
申请日：2011-01-26
申请人： Matthias Hoffmann , Georg Hoffmann , Dennis Fiegen , Sandra Handschuh , Jasna Klicic , Guenter Linz , Gerhard Schaenzle , Andreas Schnapp , Stephen Peter East , Michael Philip Mazanetz , Robert John Scott , Edward Walker
发明人： Matthias Hoffmann , Georg Hoffmann , Dennis Fiegen , Sandra Handschuh , Jasna Klicic , Guenter Linz , Gerhard Schaenzle , Andreas Schnapp , Stephen Peter East , Michael Philip Mazanetz , Robert John Scott , Edward Walker
IPC分类号： A61K31/4375 , C07D498/04 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/56 , A61P11/02 , A61P11/06 , A61P11/00 , A61P11/08 , A61P29/00 , A61P3/00 , A61P1/00 , A61P13/12 , A61P1/16 , A61P43/00 , A61P9/00 , A61P7/06 , A61P27/02 , A61P35/00 , A61P25/00 , A61P17/06 , A61P19/10 , A61P19/08 , A61P37/06 , C07D471/04
CPC分类号： C07D471/04 , C07D498/04 , C07D519/00
摘要： The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as pharmaceutical compositions containing these compounds.
摘要翻译：本发明涉及式1的新取代的萘啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂合物，其中R 1选自-O-R 3或-NR 3 R 4，R 3是C 1-6 - 烷基其被R5和R6取代，R5选自氢，支链或直链C 1-6 - 烷基，C 2-6 - 烯基，-C 1-6 - 亚烷基-O-C 1-3 - 烷基，C 1-3 - 卤代烷基， R6是环X，其中n是0或1，并且是单键或双键，并且其中A，B，D和E各自独立地选自CH 2，CH，C，N，NH，O 或S，并且其中环X通过位置A，B，D或E连接到分子，其中所述环X可以任选地被一个，两个或三个残基进一步取代，每个残基各自独立地选自氧基，羟基，-C 1-3 - 烷基，-C 1-3 - 卤代烷基，-O-C 1-3 - 烷基，-C 1-3 - 链烷醇和卤素，其中R4，R2，R7，R8，R9，R10，R11和Q 可能具有的含义权利要求1中给出，以及含有这些化合物的药物组合物。

5. 发明授权

US09096579B2 Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments 有权
标题翻译：氨基 - 吲哚基取代的咪唑基 - 嘧啶及其作为药物的用途
公开(公告)号：US09096579B2
公开(公告)日：2015-08-04
申请号：US13864394
申请日：2013-04-17
申请人： Georg Dahmann , Horst Dollinger , Christian Gnamm , Dennis Fiegen , Matthias Hoffmann , Jasna Klicic , David James Lamb , Andreas Schnapp
发明人： Georg Dahmann , Horst Dollinger , Christian Gnamm , Dennis Fiegen , Matthias Hoffmann , Jasna Klicic , David James Lamb , Andreas Schnapp
IPC分类号： A61K31/506 , A61K31/551 , A61K31/553 , A61K31/5386 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D498/10 , C07D209/42 , C07D403/06 , C07D487/04 , C07D409/14 , C07D403/14 , C07D405/14 , C07D401/14 , C07D413/14 , A61K45/06 , C07D417/14 , C07D471/04 , C07D487/10 , C07D498/04 , C07D513/04
CPC分类号： C07D403/14 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/55 , A61K31/551 , A61K31/553 , A61K45/06 , C07D209/42 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/10 , C07D498/04 , C07D498/10 , C07D513/04
摘要： The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.
摘要翻译：本发明涉及式1的新的氨基 - 吲哚取代的咪唑基 - 嘧啶，其中R 1，R 2，R 3，R 4和R 5如权利要求1所定义，及其药学上可接受的盐，以及这些化合物用于制备治疗选自哮喘，COPD，类风湿性关节炎，特异性淋巴瘤和神经系统的特定疾病的疾病。

6. 发明申请

US20110201608A1 SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES 审中-公开
标题翻译：取代的萘啶酮及其作为药物的用途
公开(公告)号：US20110201608A1
公开(公告)日：2011-08-18
申请号：US13057288
申请日：2009-07-23
申请人： Matthias Hoffmann , Thierry Bouyssou , Georg Dahamnn , Harald Engelhardt , Dennis Fiegen , Sandra Handschum , Silke Hobbie , Takeshi Kono , Ulrich Reiser , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
发明人： Matthias Hoffmann , Thierry Bouyssou , Georg Dahamnn , Harald Engelhardt , Dennis Fiegen , Sandra Handschum , Silke Hobbie , Takeshi Kono , Ulrich Reiser , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/496 , A61P11/06 , A61P19/02 , A61P1/04 , A61P17/06 , A61P35/00 , A61P17/00 , A61P11/00
CPC分类号： C07D471/04 , C07D487/04 , C07D487/10 , C07D513/04
摘要： The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 denotes a group A selected from among —O—R3, —NR3R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3 and SO2—R3 or R1 denotes a group B selected from among C6-10-aryl, five- to ten-membered, mono- or bicyclic heteroaryl with 1-3 heteroatoms selected independently of one another from among N, O and S; while this heteroaryl is linked to the structure according to formula 1 via either a C atom or an N atom, three- to ten-membered, mono- or bicyclic, saturated or partially saturated heterocyclic group with 1-3 heteroatoms selected independently of one another from among N, O and S, while this heterocyclic group is linked to the structure according to formula 1 via either a C atom or an N atom, and 5- to 11-membered spiro group which may optionally contain 1, 2 or 3 heteroatoms selected independently of one another from among N, O and S, while this spiro group is linked to the structure according to formula 1 via either a C atom or an N atom, while this group B may optionally be substituted as described in claim 1 and wherein R2 is and R3, R4, R5, R6, R6′, R7, R8, R9, R10, V, n and m may have the meanings given in claim 1, as well as pharmaceutical compositions containing these compounds.
摘要翻译：本发明涉及式1的新取代的萘啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂化物，其中R1表示选自-O-R3，-NR3R4，-CR3R4R5，（乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3或R 1表示选自C 6-10 - 芳基，5至10元，单 - 或双环杂芳基和1-3 从N，O和S中彼此独立地选择的杂原子; 而该杂芳基通过C原子或N原子连接到根据式1的结构，具有1-3个互相独立选择的杂原子的三至十元，单环或二环，饱和或部分饱和的杂环基 N，O和S中的至少一个，而该杂环基通过C原子或N原子与根据式1的结构连接，并且可以任选地含有1,2或3个杂原子的5至11元螺环 N，O和S彼此独立地选择，而该螺环通过C原子或N原子连接到根据式1的结构，而该基团B可以任选地被如权利要求1和其中R2是和R3，R4，R5，R6，R6'，R7，R8，R9，R10，V，n和m可以具有权利要求1中给出的含义，以及含有这些化合物的药物组合物。

7. 发明申请

US20110263549A1 4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS 有权
标题翻译： 4-二甲基苯胺基 - 取代的萘啶，并作为药物使用
公开(公告)号：US20110263549A1
公开(公告)日：2011-10-27
申请号：US13057330
申请日：2009-07-23
申请人： Dennis Fiegen , Sandra Handschuh , Silke Hobbie , Matthias Hoffmann , Takeshi Kono , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
发明人： Dennis Fiegen , Sandra Handschuh , Silke Hobbie , Matthias Hoffmann , Takeshi Kono , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
IPC分类号： A61K31/573 , A61K31/4375 , A61P11/00 , A61P19/10 , A61P1/04 , A61P31/14 , A61P7/06 , A61P25/00 , C07D471/04 , A61P19/02
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof. In formula 1, R1 can represent a group A selected from among the group comprising —O—R3, —NR3 R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3, and SO2—R3, or R1 represents a group B selected from among the group comprising: —C6-10-aryl;—a five-membered to ten-membered, monocyclic or bicyclic heteroaryl containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heteroaryl is linked to the structure according to formula 1 via a C atom or an N atom;—a three-membered to ten-membered, monocyclic or bicyclic, saturated or partially saturated heterocycle containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heterocycle is linked to the structure according to formula 1 via a C atom or an N atom; and—a 5-membered to 11-membered spiro group which can optionally contain 1, 2, or 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said spiro group is linked to the structure according to formula 1 via a C atom or an N atom, wherein said group B can be optionally substituted as described in claims 1, and R3,R4,R5,R6, and m can have the meanings indicated in claim 1. The invention also relates to pharmaceutical compositions containing said compounds.
摘要翻译：本发明涉及式1的新型取代萘啶以及其药理学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物或溶剂合物。在式1中，R 1可以表示选自-O-R 3，-NR 3 R 4，-CR 3 R 4 R 5， - （乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3的基团A，或R 1表示选自包括以下基团的基团：-C 6-10 - 芳基; - 含有1至3个独立地选自以下的杂原子的五元至十元单环或双环杂芳基：N，O，和S，其中所述杂芳基通过C原子或N原子连接到根据式1的结构; - 含有1至3个独立选择的杂原子的三元至十元单环或双环饱和或部分饱和的杂环包括N，O和S的基团，其中所述杂环通过C原子或N原子连接到根据式1的结构; 和可以任选地含有1,2或3个独立地选自包括N，O和S的基团的杂原子的5元至11元螺环，其中所述螺环与根据式1的结构连接通过C原子或N原子，其中所述基团B可以如权利要求1所述任选被取代，并且R 3，R 4，R 5，R 6和m可以具有权利要求1中所示的含义。本发明还涉及药物组合物含有所述化合物。

8. 发明授权

US08957088B2 4-dimethylamino-phenyl-substituted naphthyridines, and use thereof as medicaments 有权
标题翻译： 4-二甲基氨基 - 苯基取代的萘啶，及其用作药物
公开(公告)号：US08957088B2
公开(公告)日：2015-02-17
申请号：US14071016
申请日：2013-11-04
申请人： Dennis Fiegen , Sandra Handschuh , Silke Hobbie , Matthias Hoffmann , Takeshi Kono , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
发明人： Dennis Fiegen , Sandra Handschuh , Silke Hobbie , Matthias Hoffmann , Takeshi Kono , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
IPC分类号： A61K31/4375 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 and R6 may have the meanings as described in claim 1, as well as medicaments which contain these compounds. Further, the invention relates to methods of treating a disease selected from asthma, COPD, allergic rhinitis, adult respiratory distress syndrome, bronchitis, allergic dermatitis, contact dermatitis, idiopathic thrombocytopenic purpura, rheumatoid arthritis and allergic rhinoconjunctivitis by administrating an appropriate amount of a compound of formula 1 to a patient in need thereof.
摘要翻译：本发明涉及式1的新的取代的萘啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂合物，其中R 1和R 6可以具有权利要求1所述的含义，以及含有这些化合物。此外，本发明涉及通过施用适量的化合物治疗选自哮喘，COPD，变应性鼻炎，成人呼吸窘迫综合征，支气管炎，过敏性皮炎，接触性皮炎，特发性血小板减少性紫癜，类风湿性关节炎和过敏性鼻炎的疾病的方法式1给有需要的患者。

9. 发明授权

US08604049B2 4-dimethylamino-phenyl-substituted naphthyridines, and use thereof as medicaments 有权
标题翻译： 4-二甲基氨基 - 苯基取代的萘啶，及其用作药物
公开(公告)号：US08604049B2
公开(公告)日：2013-12-10
申请号：US13057330
申请日：2009-07-23
申请人： Dennis Fiegen , Sandra Handschuh , Silke Hobbie , Matthias Hoffmann , Takeshi Kono , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
发明人： Dennis Fiegen , Sandra Handschuh , Silke Hobbie , Matthias Hoffmann , Takeshi Kono , Yayoi Sato , Andreas Schnapp , Annette Schuler-Metz
IPC分类号： A61K31/573 , A61K31/4375 , A61P11/00 , A61P19/10 , A61P1/04 , A61P31/14 , A61P7/06 , A61P25/00 , A61P19/02 , C07D471/04
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof. In formula 1, R1 can represent a group A selected from among the group comprising —O—R3, —NR3R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3, and SO2—R3, or R1 represents a group B selected from among the group comprising: —C6-10-aryl; —a five-membered to ten-membered, monocyclic or bicyclic heteroaryl containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heteroaryl is linked to the structure according to formula 1 via a C atom or an N atom; —a three-membered to ten-membered, monocyclic or bicyclic, saturated or partially saturated heterocycle containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heterocycle is linked to the structure according to formula 1 via a C atom or an N atom; and —a 5-membered to 11-membered spiro group which can optionally contain 1, 2, or 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said spiro group is linked to the structure according to formula 1 via a C atom or an N atom, wherein said group B can be optionally substituted as described in claims 1, and R3, R4, R5, R6, and m can have the meanings indicated in claim 1. The invention also relates to pharmaceutical compositions containing said compounds.
摘要翻译：本发明涉及式1的新型取代萘啶以及其药理学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物或溶剂合物。在式1中，R 1可以表示选自-O-R 3，-NR 3 R 4，-CR 3 R 4 R 5， - （乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3的基团A，或 R 1表示选自以下的基团B：-C 6-10 - 芳基; 包含1至3个独立地选自N，O和S的杂原子的五元至十元单环或二环杂芳基，其中所述杂芳基通过C原子连接至根据式1的结构，或一个N原子; 包含1-3个独立地选自包括N，O和S的杂原子的3至10元，单环或双环饱和或部分饱和的杂环，其中所述杂环与根据式1的结构连接通过C原子或N原子; 和可以任选地含有1,2或3个独立地选自N，O和S的组的杂原子的5元至11元螺环，其中所述螺环与根据式1的结构连接通过C原子或N原子，其中所述基团B可以如权利要求1所述任选被取代，并且R 3，R 4，R 5，R 6和m可以具有权利要求1中所示的含义。本发明还涉及药物组合物含有所述化合物。

10. 发明授权

US08648085B2 1, 5-dihydro-pyrazolo (3, 4-D) pyrimidin-4-one derivatives and their use as PDE9A mudulators for the treatment of CNS disorders 有权
标题翻译： 1,5-二氢 - 吡唑并（3,4-D）嘧啶-4-酮衍生物及其用作治疗CNS紊乱的PDE9A混悬剂
公开(公告)号：US08648085B2
公开(公告)日：2014-02-11
申请号：US12744750
申请日：2008-11-27
申请人： Christian Eickmeier , Cornelia Dorner-Ciossek , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
发明人： Christian Eickmeier , Cornelia Dorner-Ciossek , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P3/04 , A61P3/10 , A61P25/16
CPC分类号： C07D487/04
摘要： The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterized by general Formula (I): with R1 being phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X independently of each other being selected from C2-C6-alky1 or Ci-C6-alkoxy, where C2-C6-alkyl and C1-C6-alkoxy are at least dihalogenated up to perhalogenated. preferably with 2 to 6 halogen substituents, and the halogen atoms being selected from the group of fluoro, chloro and bromo, preferably fluoro; R2 being phenyl or heteroaryl, where phenyl is substituted by 1 to 3 radicals and heteroaryl is optionally substituted by 1 to 3 radicals in each case independently of one another selected from the group of C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, amino, nitro, hydroxy, C1-C6-alkylamino, halogen, C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl. C1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl. heteroarylcarbonylamino, C1-C6-alkylsulphonyl-amino, C1-C6-alkylsulphonyl and C1-C6-alkylthio; The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving, perception, concentration, learning and/or memory in patients in need thereof.
摘要翻译：本发明涉及新的取代吡唑并嘧啶。在化学上，化合物的特征在于通式（I）：其中R 1为苯基或吡啶基，其中任何一个被1至4个，优选1至3个取代基X取代; X独立地选自C 2 -C 6 - 烷基或C 1 -C 6 - 烷氧基，其中C 2 -C 6 - 烷基和C 1 -C 6 - 烷氧基至少被二卤代化为全卤代。优选具有2至6个卤素取代基，并且卤素原子选自氟，氯和溴，优选氟; R 2是苯基或杂芳基，其中苯基被1至3个基团取代，杂芳基任选被1至3个基团取代，各自独立地选自C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，羟基羰基氰基，三氟甲基，氨基，硝基，羟基，C 1 -C 6烷基氨基，卤素，C 6 -C 10 - 芳基羰基氨基，C 1 -C 6烷基羰基氨基，C 1 -C 6烷基氨基羰基。 C 1 -C 6 - 烷氧基羰基，C 6 -C 10 - 芳基氨基羰基，杂芳基氨基羰基。杂芳基羰基氨基，C 1 -C 6烷基磺酰基 - 氨基，C 1 -C 6 - 烷基磺酰基和C 1 -C 6烷硫基; 新化合物应用于制造药物，特别是用于改善，感知，集中，学习和/或记忆有需要的患者的药物。

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