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1. 发明申请

WO2009037467A1 PYRROLOPYRIMIDINE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：WO2009037467A1
公开(公告)日：2009-03-26
申请号：PCT/GB2008/003179
申请日：2008-09-19
申请人： VERNALIS (R & D) LTD. , JORDAN, Allan , BEDFORD, Simon , BURKHARD, Klenke , YULE, Ian , POULLENNEC, Karinne
发明人： JORDAN, Allan , BEDFORD, Simon , BURKHARD, Klenke , YULE, Ian , POULLENNEC, Karinne
IPC分类号： C07D487/04 , A61K31/517 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) are A 2B receptor antagonists: wherein Ri is optionally substituted aryl or an optionally substituted monocyclic heteroaryl group having 5 or 6 ring atoms; R 2 and R 3 are independently selected from hydrogen, or optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkoxy-(C 1 - C 6 )-alkyl, C 3 -C 8 cycloalkyl, aryl, heteroaryl, aryl-(C 1 -C 6 )-alkyl, or heteroaryl-(C 1 - C 6 )-alkyl; R 4 and R 5 are independently selected from hydrogen, optionally substituted C 1 -C 6 alkyl, optionally substituted aryl, aryl-(C 1 -C 6 )-alkyl optionally substituted in the ring part thereof, -NHR 7 -N(-R 8 )-R 9 , -NH-(C=O)-R 10 , -(C=O)- NH-R 11, -(C=O)-O-R 12 , or halo; R 6 is hydrogen, C 1 -C 6 alkyl, aryl-(C 1 -C 6 )-alkyl, - (C=O)-NH-R 13 , -(C=O)-R 14 , aryl, heteroaryl, hydroxy-(C 1 -C 6 )-alkyl, or C 3 -C 8 cycloalkyl-alkyl; and R 7 , R 8 , R 9, R 10 , R 11 , R 12 , R 13 and R 14 are independently selected from C 1 -C 6 alkyl, aryl, aryl-(C 1 -C 6 )-alkyl and heteroaryl.
摘要翻译：式（I）化合物是A2B受体拮抗剂：其中R 1是任选取代的芳基或具有5或6个环原子的任选取代的单环杂芳基; R 2和R 3独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C 1 -C 6） - 烷基或杂芳基 - （C 1 -C 6） - 烷基; R 4和R 5独立地选自氢，任选取代的C 1 -C 6烷基，任选取代的芳基，在其环部分任选取代的芳基 - （C 1 -C 6） - 烷基，-NHR 7 -N（-R 8）-R 9，-NH-（ C = O）-R 10， - （C = O）-NH-R 11， - （C = O）-O-R 12或卤素; R 6是氢，C 1 -C 6烷基，芳基 - （C 1 -C 6） - 烷基， - （C = O）-NH-R 13， - （C = O）-R 14，芳基，杂芳基，羟基 - （C 1 -C 6） - 烷基或C 3 -C 8环烷基 - 烷基; 并且R 7，R 8，R 9，R 10，R 11，R 12，R 13和R 14独立地选自C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基和杂芳基。

2. 发明申请

WO2009037468A1 THIENOPYRIMIDINE COMPOUNDS AND COMPOSITIONS 审中-公开
标题翻译：噻吗啉化合物和组合物
公开(公告)号：WO2009037468A1
公开(公告)日：2009-03-26
申请号：PCT/GB2008/003180
申请日：2008-09-19
申请人： VERNALIS (R & D) LTD. , JORDAN, Allan , BEDFORD, Simon , BURKHARD, Klenke , YULE, Ian , POULLENNEC, Karinne
发明人： JORDAN, Allan , BEDFORD, Simon , BURKHARD, Klenke , YULE, Ian , POULLENNEC, Karinne
IPC分类号： C07D495/04 , A61K31/33 , A61P11/00
CPC分类号： C07D495/04
摘要： Compounds of formula (I) are A 2B wherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C 1 -C 6 alkoxy-( C 1 -C 6 )-alkyl, C 3 -C 8 cycloalkyl, aryl, heteroaryl, aryl-( C 1 -C 6 )-alkyl, or heteroaryl-( C 1 -C 6 )-alkyl; or R- 1 and R 2 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R 3 and R 4 are independently selected from hydrogen, or optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkoxy-( C 1 -C 6 )-alkyl, C 3 - C 8 cycloalkyl, aryl, heteroaryl, aryl-( C 1 -C 6 )-alkyl, or heteroaryl- C 1 -C 6 )-alkyl; or R 3 and R 4 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R 5 and R 6 are independently selected from hydrogen, C 1 -C 6 alkyl, aryl, aryl-( C 1 -C 6 )-alkyl, - NHR 7 -N(-R 8 )-R 9 , -NH-(C=O)-R 10 , -(C=O)-NH-R 11 , -(C=O)-O-R 12 , or halo; and R 7 , R 8, R 9 , R 10 , R- 11 , and R 12 are independently selected from C 1 -C 6 alkyl, aryl, aryl-( C 1 -C 6 )-alkyl and heteroaryl.
摘要翻译：式（I）化合物是其中R 1和R 2独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C1- C6） - 烷基或杂芳基 - （C1-C6） - 烷基; 或R 1和R 2与它们所连接的氮原子一起形成任选取代的5或6元环; R 3和R 4独立地选自氢或任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基 - （C 1 -C 6） - 烷基，C 3 -C 8环烷基，芳基，杂芳基，芳基 - （C 1 -C 6） - 烷基或杂芳基-C 1 -C 6） - 烷基; 或者R 3和R 4与它们所连接的氮原子一起形成任选取代的5或6元环; R 5和R 6独立地选自氢，C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基，-NHR 7 -N（-R 8）-R 9，-NH-（C = O）-R 10， - （ C = O）-NH-R 11， - （C = O）-O-R 12或卤素; 并且R 7，R 8，R 9，R 10，R 11和R 12独立地选自C 1 -C 6烷基，芳基，芳基 - （C 1 -C 6） - 烷基和杂芳基。

3. 发明申请

WO2009037463A1 THIENOPYRIMIDINE COMPOUNDS 审中-公开
标题翻译：噻吗啉化合物
公开(公告)号：WO2009037463A1
公开(公告)日：2009-03-26
申请号：PCT/GB2008/003173
申请日：2008-09-19
申请人： VERNALIS (R & D) Ltd. , JORDAN, Allan , BEDFORD, Simon , BURKHARD, Klenke , YULE, Ian , POULLENNEC, Karinne
发明人： JORDAN, Allan , BEDFORD, Simon , BURKHARD, Klenke , YULE, Ian , POULLENNEC, Karinne
IPC分类号： C07D495/04 , A61K31/33 , A61P11/00
CPC分类号： C07D495/04 , A61K31/519 , C07D495/14
摘要： Compounds of formula (I) are A 2B receptor antagonists, wherein R 1 is optionally substituted aryl or an optionally substituted 5- or 6- membered heteroaryl ring; R 2 and R 3 are independently selected from hydrogen, C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkyl-(C 1 -C 6 )-alkyl, aryl- (C 1 -C 6 )-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C 1 -C 6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid- 3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R 2 and R 3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R 4 is C 1 -C 3 alkyl, C 2 -C 3 alkenyl, -N(-R 5 )- R 6 , or optionally substituted heteroarylmethylamino; and R 5 and R 6 are independently selected from hydrogen or C 1 -C 3 alkyl; or R 5 and R 6 taken together with the nitrogen atonrto which they are attached form an optionally substituted 4- to 6-membered saturated ring.
摘要翻译：式（I）化合物是A2B受体拮抗剂，其中R 1是任选取代的芳基或任选取代的5-或6-元杂芳基环; R2和R3独立地选自氢，C1-C6烷基，C3-C8环烷基，C3-C8环烷基 - （C1-C6） - 烷基，在其环部分任意取代的芳基 - （C 1 -C 6） - 烷基，任选通过C1-C6亚烷基链连接并任选在其环部分取代的5-或6-元单环杂环基，苯并咪唑-2-基 - 甲基，吡啶-3-基 - 羰基或（1-甲基 - 哌啶 -4-基） - 羰基甲基; 或者R 2和R 3与它们所连接的氮原子一起形成任选取代的5-或6-元环; R 4是C 1 -C 3烷基，C 2 -C 3烯基，-N（-R 5）-R 6或任选取代的杂芳基甲基氨基; 并且R 5和R 6独立地选自氢或C 1 -C 3烷基; 或R 5和R 6与它们所连接的氮原子一起形成任选取代的4至6元饱和环。

4. 发明申请

US20160311781A1 PROCESS FOR MAKING SUBSTITUTED QUINAZOLINE COMPOUNDS 有权
标题翻译：制备取代的喹啉腈化合物的方法
公开(公告)号：US20160311781A1
公开(公告)日：2016-10-27
申请号：US15102417
申请日：2014-12-08
申请人： Michael Luzung , Guy Humphrey , Bangping Xiang , Kevin M. Belyk , Stephen Mark Dalby , Wilfried Schwab , Burkhard Klenke , Tom Moody , Gareth Brown
发明人： Michael Luzung , Guy Humphrey , Bangping Xiang , Kevin M. Belyk , Stephen Mark Dalby , Wilfried Schwab , Burkhard Klenke , Tom Moody , Gareth Brown
IPC分类号： C07D239/84 , B01J31/02
CPC分类号： C07D239/84 , B01J31/0202 , B01J31/0232 , B01J31/0244 , B01J31/0271 , B01J2231/324 , C07D295/125
摘要： The present invention is directed to a process for making Substituted Quinazoline Compounds of formula (I): which are useful for the treatment and prophylaxis of HCMV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).

5. 发明申请

US20080255134A1 Cardiotonic Compounds With Inhibitory Activity Against Beta-Adrenergic Receptors And Phosphodiesterase 审中-公开
标题翻译：对β-肾上腺素能受体和磷酸二酯酶具有抑制活性的强心药物
公开(公告)号：US20080255134A1
公开(公告)日：2008-10-16
申请号：US11791894
申请日：2005-11-08
申请人： Malcolm George Taylor , Burkhard Klenke , Peter D. Suzdak , Reza Mazhari
发明人： Malcolm George Taylor , Burkhard Klenke , Peter D. Suzdak , Reza Mazhari
IPC分类号： A61K31/501 , C07D401/02 , C07D401/10 , A61K31/44 , C07D401/12 , A61P9/10
CPC分类号： C07D401/14 , C07D209/88 , C07D213/86 , C07D237/04 , C07D401/04 , C07D401/12 , C07D403/12 , C07D403/14
摘要： The present invention provides compounds of formula (I) possessing inhibitory activity against β adrenergic receptors and phosphodiesterase (PDE), including type 3 phosphodiesterase (PDE-3). The present invention further provides pharmaceutical compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for regulating calcium homeostasis, for treating a disease, disorder or condition in which disregulation of calcium homeostasis is implicated and for treating cardiovascular disease, stroke, epilepsy, an ophthalmic disorder or migraine.
摘要翻译：本发明提供对β-肾上腺素能受体和磷酸二酯酶（PDE）具有抑制活性的式（I）化合物，包括3型磷酸二酯酶（PDE-3）。本发明还提供包含这些化合物的药物组合物，制备这些化合物的方法，以及使用这些化合物调节钙稳态的方法，用于治疗其中涉及钙稳态失调的疾病，病症或病症，以及治疗心血管疾病，中风，癫痫，眼科障碍或偏头痛。

6. 发明授权

US09890128B2 Process for making substituted quinazoline compounds 有权
公开(公告)号：US09890128B2
公开(公告)日：2018-02-13
申请号：US15102417
申请日：2014-12-08
申请人： Michael Luzung , Guy Humphrey , Bangping Xiang , Kevin M. Belyk , Stephen Mark Dalby , Wilfried Schwab , Burkhard Klenke , Tom Moody , Gareth Brown
发明人： Michael Luzung , Guy Humphrey , Bangping Xiang , Kevin M. Belyk , Stephen Mark Dalby , Wilfried Schwab , Burkhard Klenke , Tom Moody , Gareth Brown
IPC分类号： C07D239/84 , B01J31/02 , C07D295/125
CPC分类号： C07D239/84 , B01J31/0202 , B01J31/0232 , B01J31/0244 , B01J31/0271 , B01J2231/324 , C07D295/125
摘要： The present invention is directed to a process for making Substituted Quinazoline Compounds of formula (I): which are useful for the treatment and prophylaxis of HCMV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).

7. 发明申请

US20080090827A1 Compounds With Mixed Pde-Inhibitory and Beta-Adrenergic Antagonist or Partial Agonist Activity For Treatment of Heart Failure 审中-公开
标题翻译：具有混合Pde抑制剂和β-肾上腺素能拮抗剂或部分激动剂活性的化合物用于治疗心力衰竭
公开(公告)号：US20080090827A1
公开(公告)日：2008-04-17
申请号：US11791893
申请日：2005-11-08
申请人： Malcolm Taylor , Burkhard Klenke , Peter Suzdak , Reza Mazhari
发明人： Malcolm Taylor , Burkhard Klenke , Peter Suzdak , Reza Mazhari
IPC分类号： A61K31/50 , A61K31/444 , A61P25/06 , A61P25/08 , A61P27/02 , A61P9/00 , C07D237/04 , C07D401/04
CPC分类号： C07D237/04 , C07D401/04 , C07D403/12
摘要： This invention provides compounds that possess inhibitory activity against β-adrenergic receptors and phosphodiesterase PDE, including phosphodiesterase 3 (PDE3). This invention further provides pharmaceutical compositions comprising such compounds; methods of using such compounds for treating cardiovascular disease, stroke, epilepsy, ophthalmic disorder or migraine; and methods of preparing pharmaceutical compositions and compounds that possess inhibitory activity against β-adrenergic receptors and PDE.
摘要翻译：本发明提供具有对β-肾上腺素能受体和磷酸二酯酶PDE（包括磷酸二酯酶3（PDE3））的抑制活性的化合物。本发明进一步提供包含这些化合物的药物组合物; 使用这些化合物治疗心血管疾病，中风，癫痫，眼科障碍或偏头痛的方法; 以及制备具有对β-肾上腺素能受体和PDE的抑制活性的药物组合物和化合物的方法。

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