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1. 发明申请

WO2011057382A1 SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS 审中-公开
标题翻译：作为RININ抑制剂有用的螺环哌啶衍生物
公开(公告)号：WO2011057382A1
公开(公告)日：2011-05-19
申请号：PCT/CA2010/001632
申请日：2010-10-12
申请人： MERCK FROSST CANADA LTD. , CHEN, Austin , ASPIOTIS, Renee , MCKAY, Daniel , HAN, Yongxin , FOURNIER, Pierre-André
发明人： CHEN, Austin , ASPIOTIS, Renee , MCKAY, Daniel , HAN, Yongxin , FOURNIER, Pierre-André
IPC分类号： C07D491/107 , A61P25/22 , A61P27/02 , A61P5/42 , A61P9/00 , C07D491/20 , A61K31/438 , A61P13/12
CPC分类号： C07D491/107 , C07D491/20
摘要： Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is -(C=O)-, -CH 2 - or =CH-; U is a bond or -CH2-, or, when V iS =CH-, U is-CH=; X is =CH-, =CF-, =C(OR 3 )-, or -(C=O)-; and Y is =CH-, =CF-, =N-, or, for the case when X is -(C=O)-, Y is -N(R 3 )-.
摘要翻译：作为式（I）的螺环哌啶衍生物的肾素抑制剂及其用于治疗心血管疾病和肾功能不全的药物组合物。或其立体异构体，或其药学上可接受的盐或其立体异构体的药学上可接受的盐，其中：对于其发生的每一种情况，n独立地为0,1或2; W是五或六元饱和或不饱和的杂环或碳环单环，A是（i）五或六元饱和或不饱和的杂环或碳环单环或（ii）第一个五元或六元饱和或不饱和的杂环或碳环与第二个五元或六元饱和或不饱和的杂环或碳环稠合，V是 - （C = O） - ， - CH 2 - 或= CH-; U是键或-CH 2 - ，或当V iS = CH-时，U是-CH =; X = CH-，= CF-，= C（OR 3） - 或 - （C = O） - ; 并且Y是= CH-，= CF-，= N-，或者对于X是 - （C = O） - 的情况，Y是-N（R 3） - 。

2. 发明申请

WO2010114978A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：WO2010114978A1
公开(公告)日：2010-10-07
申请号：PCT/US2010/029588
申请日：2010-04-01
申请人： MERCK SHARP & DOHME CORP. , MERCK FROSST CANADA LTD. , MCKAY, Daniel, J. , ARBOUR, Melissa , ASPIOTIS, Renee , CHEN, Austin , DOLMAN, Sarah Jennifer , FOURNIER, Pierre-Andre , GALLANT, Michel , HAN, Yongxin , HUGHES, Greg , JANEY, Jacob , JUTEAU, Helene , LACOMBE, Patrick , LALIBERTE, Sebastien , LAUZON, Sophie , MACDONALD, Dwight , MACKAY, Bruce , MELLON, Christophe , MOLINARO, Carmela , MORLEY, Krista, L. , O'SHEA, Paul , RAMTOHUL, Yeeman, K. , SIMARD, Daniel , TSUI, Chit
发明人： MCKAY, Daniel, J. , ARBOUR, Melissa , ASPIOTIS, Renee , CHEN, Austin , DOLMAN, Sarah Jennifer , FOURNIER, Pierre-Andre , GALLANT, Michel , HAN, Yongxin , HUGHES, Greg , JANEY, Jacob , JUTEAU, Helene , LACOMBE, Patrick , LALIBERTE, Sebastien , LAUZON, Sophie , MACDONALD, Dwight , MACKAY, Bruce , MELLON, Christophe , MOLINARO, Carmela , MORLEY, Krista, L. , O'SHEA, Paul , RAMTOHUL, Yeeman, K. , SIMARD, Daniel , TSUI, Chit
IPC分类号： A61K31/535
CPC分类号： C07D211/26 , C07D211/22 , C07D211/28 , C07D211/52 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14
摘要： The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
摘要翻译：本发明涉及联芳基哌啶基肾素抑制剂化合物及其在治疗心血管事件和肾功能不全中的用途。

3. 发明申请

WO2009023964A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：WO2009023964A1
公开(公告)日：2009-02-26
申请号：PCT/CA2008/001482
申请日：2008-08-18
申请人： MERCK FROSST CANADA LTD. , JUTEAU, Helene , GALLANT, Michel , DUBE, Daniel , ROY, Patrick , ASPIOTIS, Renee , FORTIN, Rejean , LACOMBE, Patrick , MCKAY, Daniel , WU, Tom, Yao-Hsiang
发明人： JUTEAU, Helene , GALLANT, Michel , DUBE, Daniel , ROY, Patrick , ASPIOTIS, Renee , FORTIN, Rejean , LACOMBE, Patrick , MCKAY, Daniel , WU, Tom, Yao-Hsiang
IPC分类号： C07C217/54 , A61K31/137 , A61K31/16 , A61K31/21 , A61K31/277 , A61K31/44 , C07C233/00 , C07C237/00 , C07C255/00 , C07C271/00 , C07D213/04
CPC分类号： C07C217/62 , C07C217/48 , C07C229/38 , C07C237/10 , C07C237/20 , C07C255/43 , C07C271/12 , C07C323/32 , C07D213/38 , C07D213/64 , C07D213/89 , C07D317/60
摘要： The present invention relates to biphenyl compounds of formula (I). These compounds are renin inhibitors of a non- peptidic nature and of low molecular weight. The invention further relates to a pharmaceutical composition containing said compounds, as well as their use and method of treatment of cardiovascular events and renal insufficiency.
摘要翻译：本发明涉及式（I）的联苯化合物。这些化合物是非肽性和低分子量的肾素抑制剂。本发明进一步涉及含有所述化合物的药物组合物及其治疗心血管事件和肾功能不全的用途和方法。

4. 发明申请

WO2008141462A1 NOVEL CASE OF RENIN INHIBITORS 审中-公开
标题翻译：瑞恩抑制剂新案例
公开(公告)号：WO2008141462A1
公开(公告)日：2008-11-27
申请号：PCT/CA2008001005
申请日：2008-05-23
申请人： MERCK FROSST CANADA LTD , WU TOM YAO-HSIANG , JUTEAU HELENE , GALLANT MICHEL , DUBE DANIEL , ROY PATRICK , ASPIOTIS RENEE , GRIMM ERICH L , LALIBERTE SEBASTIEN , CHEN AUSTIN
发明人： WU TOM YAO-HSIANG , JUTEAU HELENE , GALLANT MICHEL , DUBE DANIEL , ROY PATRICK , ASPIOTIS RENEE , GRIMM ERICH L , LALIBERTE SEBASTIEN , CHEN AUSTIN
IPC分类号： C07D211/60 , A61K31/451 , A61K31/4523 , A61K31/5377 , A61P9/00 , A61P13/10 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
CPC分类号： C07D211/60 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D417/12
摘要： The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups. The disclosed low molecular weight, orally active renin inhibitors are of non-peptide nature and have long duration of action. The compounds can be used in the treatment of cardiovascular events and renal insufficiency.
摘要翻译：本发明涉及具有羧酸酯或羧酸端基的基于哌啶的肾素抑制剂化合物。所公开的低分子量口服活性肾素抑制剂具有非肽性质并且具有长的作用持续时间。该化合物可用于治疗心血管事件和肾功能不全。

5. 发明申请

WO2010094126A8 HETEROCYCLIC DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开
标题翻译：作为硬脂酸苄酯A DELTA-9去饱和酶的抑制剂的杂环衍生物
公开(公告)号：WO2010094126A8
公开(公告)日：2012-03-08
申请号：PCT/CA2010000228
申请日：2010-02-18
申请人： MERCK CANADA INC , ISABEL ELISE , LACHANCE NICOLAS , LECLERC JEAN-PHILIPPE , LEGER SERGE , OBALLA RENATA M , POWELL DAVID , RAMTOHUL YEEMAN K , ROY PATRICK , TRANMER GEOFFREY K , ASPIOTIS RENEE , LI LIANHAI , MARTINS EVELYN
发明人： ISABEL ELISE , LACHANCE NICOLAS , LECLERC JEAN-PHILIPPE , LEGER SERGE , OBALLA RENATA M , POWELL DAVID , RAMTOHUL YEEMAN K , ROY PATRICK , TRANMER GEOFFREY K , ASPIOTIS RENEE , LI LIANHAI , MARTINS EVELYN
IPC分类号： C07D417/04 , A61K31/454 , A61K31/496 , A61K31/4995 , A61K31/551 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/14 , C07D487/08
CPC分类号： C07D413/14 , A61K31/454 , A61K31/496 , A61K31/4995 , A61K31/551 , C07D403/04 , C07D403/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D487/08
摘要： Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1-substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N-CR5R6, C=CR5 or CR13-CR5R6, Y is a bond or -C(O)-, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.
摘要翻译：结构式（I）的杂环化合物或其药学上可接受的盐，其中W是R 1取代的杂芳基，R 1是被含有酯或羧酸的基团取代的杂芳基环，XT是N-CR 5 R 6，C = CR 5或 CR13-CR5R6，Y是键或-C（O） - ，a和b表示选自1至4的整数，Ar是任选取代的苯基或萘基，是硬脂酰辅酶A-9去饱和酶的抑制剂 SCD）杂环化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，动脉粥样硬化，肥胖，糖尿病，神经系统疾病，代谢综合征，胰岛素抵抗，癌症，肝脂肪变性和非酒精性脂肪性肝炎。

6. 发明申请

WO2008141462A9 NOVEL CASE OF RENIN INHIBITORS 审中-公开
公开(公告)号：WO2008141462A9
公开(公告)日：2008-11-27
申请号：PCT/CA2008/001005
申请日：2008-05-23
申请人： MERCK FROSST CANADA LTD. , WU, Tom, Yao-Hsiang , JUTEAU, Helene , GALLANT, Michel , DUBE, Daniel , ROY, Patrick , ASPIOTIS, Renee , GRIMM, Erich, L. , LALIBERTE, Sebastien , CHEN, Austin
发明人： WU, Tom, Yao-Hsiang , JUTEAU, Helene , GALLANT, Michel , DUBE, Daniel , ROY, Patrick , ASPIOTIS, Renee , GRIMM, Erich, L. , LALIBERTE, Sebastien , CHEN, Austin
IPC分类号： C07D211/60 , A61K31/451 , A61K31/4523 , A61K31/5377 , A61P13/10 , A61P9/00 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups. The disclosed low molecular weight, orally active renin inhibitors are of non-peptide nature and have long duration of action. The compounds can be used in the treatment of cardiovascular events and renal insufficiency.

7. 发明申请

WO0220465A2 GAMMA-KETOACID DIPEPTIDES AS INHIBITORS OF CASPASE-3 审中-公开
标题翻译：作为CASPASE-3的抑制剂的GAMMA-KETOACID DIPEPTIDES
公开(公告)号：WO0220465A2
公开(公告)日：2002-03-14
申请号：PCT/CA0101272
申请日：2001-09-06
申请人： MERCK FROSST CANADA INC , HAN YONGXIN , GIROUX ANDRE , GRIMM ERICH L , ASPIOTIS RENEE , BLACK CAMERON
发明人： HAN YONGXIN , GIROUX ANDRE , GRIMM ERICH L , ASPIOTIS RENEE , BLACK CAMERON
IPC分类号： C12N9/99 , A61K38/55 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/14 , A61P21/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P31/04 , A61P31/18 , A61P37/04 , A61P43/00 , C07C237/22 , C07D213/63 , C07D215/22 , C07D215/233 , C07D217/24 , C07D239/34 , C07D241/44 , C07D271/06 , C07D307/86 , C07D413/12 , C07D495/04 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/078 , A61K31/16
CPC分类号： C07D215/233 , C07C237/22 , C07D213/63 , C07D217/24 , C07D239/34 , C07D241/44 , C07D271/06 , C07D307/86 , C07D413/12 , C07D495/04
摘要： This invention encompasses the novel compounds of Formula (I), which are useful in the treatment of caspase-3 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula (I) as well as methods for treatment of caspase-3 mediated diseases.
摘要翻译：本发明包括式（I）的新化合物，其可用于治疗半胱天冬酶-3介导的疾病。本发明还包括含有式（I）化合物的某些药物组合物以及治疗半胱天冬酶-3介导的疾病的方法。

8. 发明申请

WO2010094126A1 HETEROCYCLIC DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开
标题翻译：作为硬脂酸苄酯A DELTA-9去饱和酶的抑制剂的杂环衍生物
公开(公告)号：WO2010094126A1
公开(公告)日：2010-08-26
申请号：PCT/CA2010/000228
申请日：2010-02-18
申请人： MERCK FROSST CANADA LTD. , ISABEL, Elise , LACHANCE, Nicolas , LECLERC, Jean-Philippe , LEGER, Serge , OBALLA, Renata, M. , POWELL, David , RAMTOHUL, Yeeman, K. , ROY, Patrick , TRANMER, Geoffrey, K. , ASPIOTIS, Renee , LI, Lianhai , MARTINS, Evelyn
发明人： ISABEL, Elise , LACHANCE, Nicolas , LECLERC, Jean-Philippe , LEGER, Serge , OBALLA, Renata, M. , POWELL, David , RAMTOHUL, Yeeman, K. , ROY, Patrick , TRANMER, Geoffrey, K. , ASPIOTIS, Renee , LI, Lianhai , MARTINS, Evelyn
IPC分类号： C07D417/04 , A61K31/454 , A61K31/496 , A61K31/4995 , A61K31/551 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/14 , C07D487/08
CPC分类号： C07D413/14 , A61K31/454 , A61K31/496 , A61K31/4995 , A61K31/551 , C07D403/04 , C07D403/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D487/08
摘要： Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R 1 -substituted heteroaryl, R 1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N-CR 5 R 6 , C=CR 5 or CR 13 -CR 5 R 6 , Y is a bond or -C(O)-, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.
摘要翻译：结构式（I）的杂环化合物或其药学上可接受的盐，其中W是R 1取代的杂芳基，R 1是被含有酯或羧酸的基团取代的杂芳基环，XT是N-CR 5 R 6，C = CR 5或 CR13-CR5R6，Y是键或-C（O） - ，a和b表示选自1至4的整数，Ar是任选取代的苯基或萘基，是硬脂酰辅酶A-9去饱和酶的抑制剂 SCD）杂环化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，动脉粥样硬化，肥胖，糖尿病，神经系统疾病，代谢综合征，胰岛素抵抗，癌症，肝脂肪变性和非酒精性脂肪性肝炎。

9. 发明申请

WO2005070883A1 NITRIC OXIDE RELEASING PRODRUGS OF DIARYL-2-(5H)-FURANONES AS CYCLOOXYGENASE-2 INHIBITORS 审中-公开
标题翻译：二氧化氮（5H） - 芳族化合物的氧化氮释放物作为CYCLOOXYGENASE-2抑制剂
公开(公告)号：WO2005070883A1
公开(公告)日：2005-08-04
申请号：PCT/CA2005/000083
申请日：2005-01-25
申请人： MERCK FROSST CANADA & CO. , DUFRESNE, Claude , BERTHELETTE, Carl , LI, Lianhai , GUAY, Daniel , GALLANT, Michel , LACOMBE, Patrick , ASPIOTIS, Renee , WANG, Zhaoyin , STURINO, Claudio, F.
发明人： DUFRESNE, Claude , BERTHELETTE, Carl , LI, Lianhai , GUAY, Daniel , GALLANT, Michel , LACOMBE, Patrick , ASPIOTIS, Renee , WANG, Zhaoyin , STURINO, Claudio, F.
IPC分类号： C07C317/46
CPC分类号： C07C311/29 , A61K31/04 , C07C317/46
摘要： The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. Formula (I). The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula 1. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while also reducing the risk of thrombotic cardiovascular events.
摘要翻译：本发明包括式I的新化合物，其是可用于治疗环加氧酶-2介导的疾病的二芳基-2-（5H） - 呋喃酮的一氧化氮释放前药。式（I）。本发明还包括用于治疗环加氧酶-2介导的疾病的某些药物组合物和方法，其包括使用式1化合物。上述化合物可用作与低剂量阿司匹林联合治疗以治疗慢性环氧合酶-2介导的疾病或病症同时也降低血栓性心血管事件的风险。

10. 发明申请

WO2005070868A1 COMBINATION THERAPY FOR TREATING CYCLOOXYGENASE-2 MEDIATED DISEASES OR CONDITIONS IN PATIENTS AT RISK OF THROMBOTIC CARDIOVASCULAR EVENTS 审中-公开
标题翻译：用于治疗患有血栓性心脏病事件的患者的CYCLOOXYGENASE-2介导的疾病或病症的组合治疗
公开(公告)号：WO2005070868A1
公开(公告)日：2005-08-04
申请号：PCT/CA2005/000082
申请日：2005-01-25
申请人： MERCK FROSST CANADA & CO. , DUFRESNE, Claude , BERTHELETTE, Carl , LI, Lianhai , GUAY, Daniel , GALLANT, Michel , LACOMBE, Patrick , ASPIOTIS, Renee , WANG, Zhaoyin , STURINO, Claudio, F.
发明人： DUFRESNE, Claude , BERTHELETTE, Carl , LI, Lianhai , GUAY, Daniel , GALLANT, Michel , LACOMBE, Patrick , ASPIOTIS, Renee , WANG, Zhaoyin , STURINO, Claudio, F.
IPC分类号： C07C203/04
CPC分类号： C07C203/04 , A61K31/04 , A61K31/045 , A61K31/22 , A61K31/24 , A61K31/616 , A61K45/06 , A61K2300/00
摘要： The invention is directed to a method for treating a cyclooxygenase-2 mediated disease or condition in a mammalian patient at risk of a thrombotic cardiovascular event, wherein the patient is on aspirin therapy to reduce the risk of the thrombotic cardiovascular event, comprising orally concomitantly or sequentially administering to the patient a cyclooxygenase-2 selective inhibitor in an amount effective to treat the cyclooxygenase-2 mediate disease or condition, and a nitric oxide donating compound in accordance with Formula (I) or a pharmaceutically acceptable salt thereof, wherein the nitric oxide donating compound is administered in an amount effective to reduce the gastrointestinal toxicity caused by the combination of the cyclooxygenase-2 selective inhibitor and aspirin. Pharmaceutical compositions are also encompassed.
摘要翻译：本发明涉及一种用于治疗患有血栓性心血管事件风险的哺乳动物患者中环氧合酶-2介导的疾病或病症的方法，其中所述患者服用阿司匹林治疗以降低血栓性心血管事件的风险，包括口服伴随地或以有效治疗所述环加氧酶-2介导疾病或病症的量向所述患者依次施用环氧合酶-2选择性抑制剂和根据式（I）的一氧化氮供体化合物或其药学上可接受的盐，其中所述一氧化氮以有效减少由环氧合酶-2选择性抑制剂和阿司匹林的组合引起的胃肠道毒性的量施用给药化合物。还包括药物组合物。

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