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1.发明申请BIARYL PDE4 INHIBITORS FOR TREATING INFLAMMATORY, CARDIOVASCULAR AND CNS DISORDERS 审中-公开用于治疗炎症，心血管和中枢神经疾病的BIARYL PDE4抑制剂公开(公告)号：US20090324569A1
公开(公告)日：2009-12-31
申请号：US12275163
申请日：2008-11-20
申请人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Adalie Motta , Gary Schiltz , Georgeta Hategan , Timothy Hagen
发明人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Adalie Motta , Gary Schiltz , Georgeta Hategan , Timothy Hagen
IPC分类号： A61K31/44 , C07D401/04 , C07D231/12 , C07D237/14 , C07D277/38 , C07D285/135 , C07D213/72 , C07D403/10 , C07D413/06 , C07D401/06 , A61K31/4427 , A61K31/5377 , A61K31/4439 , A61K31/4412 , A61K31/4164 , A61K31/4245 , A61K31/445 , A61K31/437 , A61K31/415 , A61K31/506 , A61K31/54 , A61K31/122 , A61K31/435 , A61P9/00 , A61P35/00 , A61P11/00
CPC分类号： C07C217/84 , A61K31/136 , A61K31/397 , A61K31/41 , A61K31/426 , A61K31/437 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/5377 , A61K45/06 , C07B2200/05 , C07C65/40 , C07C69/94 , C07C275/32 , C07C275/62 , C07C305/24 , C07C307/10 , C07D205/04 , C07D207/16 , C07D213/38 , C07D213/40 , C07D213/64 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/79 , C07D213/81 , C07D213/84 , C07D213/89 , C07D231/12 , C07D233/90 , C07D239/42 , C07D257/04 , C07D275/06 , C07D277/42 , C07D285/12 , C07D285/135 , C07D401/04 , C07D401/06 , C07D403/04 , C07D471/04 , C07D473/18 , C07D473/40
摘要： The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders. The compounds have general formula I: A particular embodiment is
摘要翻译： 本发明涉及含有至少一个其它环的联芳基化合物属。 该化合物是可用于治疗和预防中风，心肌梗塞和心血管炎性疾病和病症的PDE4抑制剂。 该化合物具有通式I：具体实施方案是
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2.发明申请BIARYL PDE4 INHIBITORS FOR TREATING INFLAMMATORY, CARDIOVASCULAR AND CNS DISORDERS 有权用于治疗炎症，心脏病和中枢神经疾病的BIARYL PDE4抑制剂公开(公告)号：US20120183522A1
公开(公告)日：2012-07-19
申请号：US13430164
申请日：2012-03-26
申请人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Adalie Motta , Gary Schiltz , Georgeta Hategan , Timothy Hagen
发明人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Adalie Motta , Gary Schiltz , Georgeta Hategan , Timothy Hagen
IPC分类号： A61K31/4418 , C07D471/04 , A61K31/437 , C07D401/04 , A61K31/4427 , C07D237/14 , A61K31/50 , C07D413/12 , A61K31/501 , C07D413/06 , A61K31/5377 , C07D279/02 , A61K31/54 , A61K31/473 , A61K31/439 , A61K31/445 , A61K31/44 , A61K31/355 , A61K31/122 , A61K38/43 , A61P25/00 , A61P9/10 , A61P9/00 , A61P35/00 , A61P11/06 , A61P11/00 , A61P25/28 , A61P25/14 , A61P19/00 , A61P25/24 , A61P25/22 , A61P13/10 , C07D213/65
CPC分类号： C07C217/84 , A61K31/136 , A61K31/397 , A61K31/41 , A61K31/426 , A61K31/437 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/5377 , A61K45/06 , C07B2200/05 , C07C65/40 , C07C69/94 , C07C275/32 , C07C275/62 , C07C305/24 , C07C307/10 , C07D205/04 , C07D207/16 , C07D213/38 , C07D213/40 , C07D213/64 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/79 , C07D213/81 , C07D213/84 , C07D213/89 , C07D231/12 , C07D233/90 , C07D239/42 , C07D257/04 , C07D275/06 , C07D277/42 , C07D285/12 , C07D285/135 , C07D401/04 , C07D401/06 , C07D403/04 , C07D471/04 , C07D473/18 , C07D473/40
摘要： The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders. The compounds have general formula I: A particular embodiment is
摘要翻译： 本发明涉及含有至少一个其它环的联芳基化合物属。 该化合物是可用于治疗和预防中风，心肌梗塞和心血管炎性疾病和病症的PDE4抑制剂。 该化合物具有通式I：具体实施方案是
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3.发明授权Biaryl PDE4 inhibitors for treating inflammatory, cardiovascular and CNS disorders 有权用于治疗炎症，心血管和CNS疾病的二芳基PDE4抑制剂公开(公告)号：US08791267B2
公开(公告)日：2014-07-29
申请号：US13430164
申请日：2012-03-26
申请人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Adalie Motta , Gary Schiltz , Georgeta Hategan , Timothy Hagen
发明人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Adalie Motta , Gary Schiltz , Georgeta Hategan , Timothy Hagen
IPC分类号： C07D213/72 , A61K31/435
CPC分类号： C07C217/84 , A61K31/136 , A61K31/397 , A61K31/41 , A61K31/426 , A61K31/437 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/5377 , A61K45/06 , C07B2200/05 , C07C65/40 , C07C69/94 , C07C275/32 , C07C275/62 , C07C305/24 , C07C307/10 , C07D205/04 , C07D207/16 , C07D213/38 , C07D213/40 , C07D213/64 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/79 , C07D213/81 , C07D213/84 , C07D213/89 , C07D231/12 , C07D233/90 , C07D239/42 , C07D257/04 , C07D275/06 , C07D277/42 , C07D285/12 , C07D285/135 , C07D401/04 , C07D401/06 , C07D403/04 , C07D471/04 , C07D473/18 , C07D473/40
摘要： The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders. The compounds have general formula I: A particular embodiment is
摘要翻译： 本发明涉及含有至少一个其它环的联芳基化合物属。 该化合物是可用于治疗和预防中风，心肌梗塞和心血管炎性疾病和病症的PDE4抑制剂。 该化合物具有通式I：具体实施方案是
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公开(公告)号：US20090131530A1
公开(公告)日：2009-05-21
申请号：US12275168
申请日：2008-11-20
IPC分类号： A61K31/165 , C07C233/02 , A61P29/00
CPC分类号： C07D213/73 , C07C43/29 , C07C43/295 , C07C45/71 , C07C205/38 , C07C275/32 , C07C311/08 , C07D213/81 , C07D213/83 , C07C47/575
摘要： Compounds of the formula: are disclosed. The compounds act as phosphodiesterase-4 modulators, and useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions. Other embodiments are also disclosed.
摘要翻译： 公开了下式的化合物。 该化合物作为磷酸二酯酶-4调节剂，可用于治疗中风，心肌梗死和心血管炎症状况。 还公开了其他实施例。
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5.发明授权Substituted benzoazole PDE4 inhibitors for treating inflammatory, cardiovascular and CNS disorders 有权用于治疗炎症，心血管和CNS疾病的取代的苯扎唑PDE4抑制剂公开(公告)号：US08883833B2
公开(公告)日：2014-11-11
申请号：US12275165
申请日：2008-11-20
申请人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Munagala Rao
发明人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Munagala Rao
IPC分类号： C07D513/04 , C07D498/04 , C07D417/04 , C07D417/06 , C07D417/14 , C07D277/64 , C07D277/82 , C07D263/56 , C07D263/58 , A61K31/519 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/428 , A61K31/423
CPC分类号： C07D417/14 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/519 , C07D263/56 , C07D263/58 , C07D277/64 , C07D277/82 , C07D417/04 , C07D417/06 , C07D498/04 , C07D513/04
摘要： The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles. A particular embodiment is
摘要翻译： 本发明涉及用于治疗中风，心肌梗塞和心血管炎症状况的可用于治疗中风，心肌梗死和心血管炎症状况的苯环的吡啶和嘧啶环的取代苯并唑和其对应物与包含这些化合物的药物组合物的方法， 治疗哺乳动物的中风，心肌梗死和心血管炎症状况。 化合物具有通式I：其中A和B是碳环或杂环。 一个特定的实施例是
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公开(公告)号：US08877816B2
公开(公告)日：2014-11-04
申请号：US12275168
申请日：2008-11-20
IPC分类号： A61K31/165 , C07C233/02 , A61P29/00 , C07C311/08 , C07C275/32 , C07C43/295 , C07D213/73 , C07C45/71 , C07C43/29 , C07C205/38 , C07D213/81 , C07D213/83
CPC分类号： C07D213/73 , C07C43/29 , C07C43/295 , C07C45/71 , C07C205/38 , C07C275/32 , C07C311/08 , C07D213/81 , C07D213/83 , C07C47/575
摘要： Compounds of the formula: are disclosed. The compounds act as phosphodiesterase-4 modulators, and useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions. Other embodiments are also disclosed.
摘要翻译： 公开了下式的化合物。 该化合物作为磷酸二酯酶-4调节剂，可用于治疗中风，心肌梗死和心血管炎症状况。 还公开了其他实施例。
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7.发明申请SUBSTITUTED BENZOAZOLE PDE4 INHIBITORS FOR TREATING INFLAMMATORY, CARDIOVASCULAR AND CNS DISORDERS 有权替代苯扎唑PDE4抑制剂治疗炎症，心血管疾病和中枢神经系统疾病公开(公告)号：US20090130077A1
公开(公告)日：2009-05-21
申请号：US12275165
申请日：2008-11-20
申请人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Munagala Rao
发明人： Jasbir Singh , Mark E. Gurney , Alex Burgin , Vincent Sandanayaka , Alexander Kiselyov , Munagala Rao
IPC分类号： A61K31/428 , C07D277/82 , C07D417/10 , C07D417/14 , C07D513/04 , C07D401/10 , A61K31/435 , A61K31/122 , A61P35/00 , A61P1/00 , A61P11/00 , A61K31/4353 , A61K31/496 , A61P9/00 , A61K31/454 , A61K31/4245 , A61K31/4439
CPC分类号： C07D417/14 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/519 , C07D263/56 , C07D263/58 , C07D277/64 , C07D277/82 , C07D417/04 , C07D417/06 , C07D498/04 , C07D513/04
摘要： The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles. A particular embodiment is
摘要翻译： 本发明涉及用于治疗中风，心肌梗塞和心血管炎症状况的可用于治疗中风，心肌梗死和心血管炎症状况的苯环的吡啶和嘧啶环的取代苯并唑和其对应物与包含这些化合物的药物组合物的方法， 治疗哺乳动物的中风，心肌梗死和心血管炎症状况。 化合物具有通式I：其中A和B是碳环或杂环。 一个特定的实施例是
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8.发明授权公开(公告)号：US07750012B2
公开(公告)日：2010-07-06
申请号：US11462278
申请日：2006-08-03
IPC分类号： A61K31/495 , A61K31/496 , C07D295/15 , C07D333/16 , A61K31/5375 , A61K31/5377 , A61K31/451 , A61K31/4523 , C07D211/34 , C07D211/58 , C07D413/12
CPC分类号： C07D295/033 , C07D211/58 , C07D295/096 , C07D295/15 , C07D333/16 , C07D333/28
摘要： The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
摘要翻译： 本发明涉及作为LTA4H（白三烯A4水解酶）抑制剂的联芳基氮连接杂环化学属。 这些化合物具有通式，它们可用于治疗和预防和预防炎性疾病和病症。
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9.发明申请BIARYL SUBSTITUTED NITROGEN CONTAINING HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION 审中-公开含有LTA4H用于治疗感染的含二氮杂环己烷的含氮杂环化合物公开(公告)号：US20090233969A1
公开(公告)日：2009-09-17
申请号：US12472958
申请日：2009-05-27
IPC分类号： A61K31/445 , C07D207/12 , A61K31/40 , C07D211/46 , A61P29/00 , C12N9/99
CPC分类号： C07D207/12 , C07D211/46
摘要： The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
摘要翻译： 本发明涉及作为LTA4H（白三烯A4水解酶）抑制剂的联芳基取代的氮连接杂环的化学属。 这些化合物具有以下通式：它们可用于治疗和预防和预防炎性疾病和病症。
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10.发明申请PYRAZOLYLPHENYL AND PYRROLYLPHENYL INHIBITORS OF LTA4H FOR TREATING INFLAMMATION 失效LTA4H用于治疗炎症的吡咯并噻吩和吡咯烷酮抑制剂公开(公告)号：US20080033013A1
公开(公告)日：2008-02-07
申请号：US11833313
申请日：2007-08-03
申请人： Vincent Sandanayaka , Jasbir Singh , Lei Zhao , Peng Yu , Mark E. Gurney
发明人： Vincent Sandanayaka , Jasbir Singh , Lei Zhao , Peng Yu , Mark E. Gurney
IPC分类号： A61K31/4523 , A61K31/4025 , A61P1/00 , A61P11/00 , A61P19/02 , A61P29/00 , A61P9/00 , C07D207/00 , C07D221/00 , C12N9/99
CPC分类号： C07D231/12 , C07D207/325 , C07D207/333 , C07D207/34 , C07D231/14 , C07D231/16
摘要： Two chemical genera of pyrazolylphenyl and pyrrolylphenyl derivatives are disclosed. They have the general formula: In these compounds ring (a) is a pyrazole or pyrrole; Q is selected from the group consisting of a direct bond, O, S, SO, SO2, NR1, CH2, CF2, and C(O); HET is a 4-7-membered saturated nitrogenous heterocycle; and taken together ZW is H or Z is (CH2)1-10 in which one or two (CH2) may optionally be replaced by —O—, —NR1—, —SO—, —S(O)2—, —C(═O)— or —C═O(NH)—; and W is hydrogen, acyl, hydroxyl, carboxyl, amino, carboxamido, aminoacyl, —COOalkyl, —CHO, heterocyclyl, substituted aryl or substituted heterocyclyl. The compounds are inhibitors of LTA4H (leukotriene A4 hydrolase). They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
摘要翻译： 公开了吡唑基苯基和吡咯基苯基衍生物的两种化学属。 它们具有以下通式：在这些化合物中，环（a）是吡唑或吡咯; Q选自直接键O，S，SO，SO 2，NR 1，CH 2，CF 3， SUB 2和C（O）; HET是4-7元饱和含氮杂环; 并且合并在一起ZW是H或Z是（CH 2）2 - ，其中一个或两个（CH 2/2）可以任选地被替换 ，-O - ， - SO - ， - S（O）2 - ， - C（ - ） - 或-CO（NH） - ; W是氢，酰基，羟基，羧基，氨基，甲酰胺基，氨基酰基，-COO烷基，-CHO，杂环基，取代的芳基或取代的杂环基。 这些化合物是LTA4H（白三烯A4水解酶）的抑制剂。 它们可用于治疗和预防和预防炎性疾病和病症。
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