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1. 发明申请

WO2007014462A1 EP4 RECEPTOR AGONIST, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： EP4受体激动剂，其组合物及其方法
公开(公告)号：WO2007014462A1
公开(公告)日：2007-02-08
申请号：PCT/CA2006/001254
申请日：2006-07-28
申请人： MERCK FROSST CANADA LTD. , COLUCCI, John , HAN, Yongxin , FARAND, Julie, A.
发明人： COLUCCI, John , HAN, Yongxin , FARAND, Julie, A.
IPC分类号： C07D265/10 , A61P27/06 , A61K31/535
CPC分类号： C07D265/10 , C07D413/06 , C07D417/06
摘要： This invention relates to potent selective agonists of the EP 4 subtype of prostaglandin E 2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts. The compounds of the present invention are the compounds of Formula (I).
摘要翻译：本发明涉及前列腺素E 2受体的EP 4亚型的有效选择性激动剂，它们在治疗青光眼和其它病症中的用途或制剂，其相关以提高患者眼中的眼内压。本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。本发明的化合物是式（I）的化合物。

2. 发明申请

WO2007014454A1 EP4 RECEPTOR AGONIST, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： EP4受体激动剂，其组合物及其方法
公开(公告)号：WO2007014454A1
公开(公告)日：2007-02-08
申请号：PCT/CA2006/001243
申请日：2006-07-28
申请人： MERCK FROSST CANADA LTD. , COLUCCI, John , HAN, Yongxin , FARAND, Julie, A.
发明人： COLUCCI, John , HAN, Yongxin , FARAND, Julie, A.
IPC分类号： C07D413/06 , A61K31/5355 , A61P19/00 , A61P19/08 , A61P19/10 , A61P27/02
CPC分类号： C07D413/06
摘要： This invention relates to potent selective agonists of the EP 4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译：本发明涉及前列腺素E2受体的EP 4亚型的有效选择性激动剂，它们在治疗青光眼和其它病症中的用途或制剂，其与眼睛中眼内压升高有关病人。本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。

3. 发明申请

WO2005116010A1 EP4 RECEPTOR AGONIST, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： EP4受体激动剂，其组合物及其方法
公开(公告)号：WO2005116010A1
公开(公告)日：2005-12-08
申请号：PCT/CA2005/000773
申请日：2005-05-20
申请人： MERCK FROSST CANADA LTD. , BELLEY, Michel , COLUCCI, John , GIRARD, Mario , HAN, Yongxin , LACOMBE, Patrick
发明人： BELLEY, Michel , COLUCCI, John , GIRARD, Mario , HAN, Yongxin , LACOMBE, Patrick
IPC分类号： C07D401/10
CPC分类号： C07C65/21 , C07C63/331 , C07C63/66 , C07C65/24 , C07C65/28 , C07D213/61 , C07D213/64 , C07D213/65 , C07D257/04 , C07D333/40 , C07D401/10 , C07D401/12 , C07D401/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14
摘要： This invention relates to potent selective agonists of the EP 4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译：本发明涉及前列腺素E2受体的EP4亚型的有效选择性激动剂，它们在治疗青光眼和其它病症中的用途或其制剂，其与患者眼睛中的眼内压升高有关。本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。

4. 发明申请

WO2008104055A1 INDOLE AND INDOLINE CYCLOPROPYL AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为EP4受体拮抗剂的吲哚和吲哚啉环酰胺衍生物
公开(公告)号：WO2008104055A1
公开(公告)日：2008-09-04
申请号：PCT/CA2008/000351
申请日：2008-02-22
申请人： MERCK FROSST CANADA LTD. , BOYD, Michael , COLUCCI, John , HAN, Yongxin
发明人： BOYD, Michael , COLUCCI, John , HAN, Yongxin
IPC分类号： C07D209/08 , A61K31/404 , A61K31/41 , C07D403/12
CPC分类号： C07D209/08 , C07D209/42 , C07D403/12
摘要： The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及吲哚和二氢吲哚环丙酰胺衍生物作为EP4受体拮抗剂，其可用于治疗EP4介导的疾病或病症，例如急性和慢性疼痛，骨关节炎，类风湿性关节炎和癌症。还包括药物组合物和使用方法。

5. 发明申请

WO2008089581A1 FUSED AROMATIC PTP-1B INHIBITORS 审中-公开
标题翻译： FUSED AROMATIC PTP-1B抑制剂
公开(公告)号：WO2008089581A1
公开(公告)日：2008-07-31
申请号：PCT/CA2008/000172
申请日：2008-01-24
申请人： MERCK FROSST CANADA LTD. , COLUCCI, John , WILSON, Marie-Claire , HAN, Yongxin , DUFRESNE, Claude , BELLEY, Michel , LAU, Cheuk, K. , BAYLY, Christopher
发明人： COLUCCI, John , WILSON, Marie-Claire , HAN, Yongxin , DUFRESNE, Claude , BELLEY, Michel , LAU, Cheuk, K. , BAYLY, Christopher
IPC分类号： C07F9/60 , A61K31/662 , A61K31/675 , A61P3/10 , A61P35/00 , C07F9/38 , C07F9/40
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
摘要翻译：本发明包括由下式表示的新一类化合物，它们是PTP-1B酶的抑制剂。本发明还包括药物组合物，其包括上述化合物（式I）和治疗或预防PTP-1B介导的疾病包括糖尿病的方法。

6. 发明申请

WO2006122403A1 QUINOLINE DERIVATIVES AS EP4 ANTAGONISTS 审中-公开
标题翻译：喹啉衍生物作为EP4拮抗剂
公开(公告)号：WO2006122403A1
公开(公告)日：2006-11-23
申请号：PCT/CA2006/000789
申请日：2006-05-15
申请人： MERCK FROSST CANADA LTD. , BELLEY, Michel , BURCH, Jason , COLUCCI, John , FARAND, Julie , GIRARD, Mario , HAN, Yongxin
发明人： BELLEY, Michel , BURCH, Jason , COLUCCI, John , FARAND, Julie , GIRARD, Mario , HAN, Yongxin
IPC分类号： C07D471/04 , A61K31/44 , A61K31/435 , A61K31/4745 , A61K31/498 , A61K31/501 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom., a N(O) group or a C(R 5 ) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.
摘要翻译：本发明涉及可用于治疗EP4介导的疾病或病症（例如急性和慢性疼痛，骨关节炎，类风湿性关节炎和癌症）的前列腺素E型受体拮抗剂的喹啉衍生物。衍生物具有式（I）的以下结构：其中A和B表示氮原子或CH基团，条件是它们不能同时为CH，Q可以表示氮或碳原子，Y和Z 是氮原子，N（O）基或C（R 5）基团。还包括包含式（I）的衍生物的药物组合物。

7. 发明申请

WO2011020193A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：WO2011020193A1
公开(公告)日：2011-02-24
申请号：PCT/CA2010/001281
申请日：2010-08-17
申请人： MERCK FROSST CANADA LTD. , CHIH-YU CHEN, Austin , LALIBERTE, Sébastien , LAROUCHE, Guillaume , HAN, Yongxin , MCKAY, Daniel
发明人： CHIH-YU CHEN, Austin , LALIBERTE, Sébastien , LAROUCHE, Guillaume , HAN, Yongxin , MCKAY, Daniel
IPC分类号： C07D491/107 , A61K31/438 , A61P25/22 , A61P27/06 , A61P9/00 , C07D491/20
CPC分类号： A61K31/438 , C07D491/107 , C07D519/00
摘要： Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R 1 is hydrogen, C 1-6 -alkyl or C 3-6 -cycloalkyl, wherein said C 1-6 -alkyl or C 3-6 -cycloalkyl group can be independently substituted with 1-3 halogens; A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to another five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is a bond or -(C=O)-, -CH(OH)-, -CH 2 - or =CH-; U is a bond or -CH2-, or for the case 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：作为结构式（I）的螺环哌啶酰胺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。其中对于其发生的每个实例，n独立地为0,1或2; R 1是氢，C 1-6 - 烷基或C 3-6 - 环烷基，其中所述C 1-6 - 烷基或C 3-6 - 环烷基可以独立地被1-3个卤素取代; A是（i）五或六元饱和或不饱和杂环或碳环单环或（ii）五元或六元饱和或不饱和的杂环或碳环，其与另一个五元或六元饱和或不饱和杂环或碳环，V是一个键或 - （C = O） - ， - CH（OH） - ， - CH 2 - 或= CH-; U是键或-CH 2 - ，或者当V = CH-的情况下，U是-CH =; X = CH-，= CF-，= C（OR 3） - 或-C = O-; 并且Y是= CH-，= CF-，= N-，或者当X是-C = O-时，Y是-N（R3） - 的情况。

8. 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） - 。

9. 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。

10. 发明申请

WO2010034110A1 BETA-CARBOLINE SULPHONYLUREA DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为EP4受体拮抗剂的β-碳酰胺磺酰胺衍生物
公开(公告)号：WO2010034110A1
公开(公告)日：2010-04-01
申请号：PCT/CA2009/001330
申请日：2009-09-22
申请人： MERCK FROSST CANADA LTD. , BERTHELETTE, Carl , BOYD, Michael , BURCH, Jason , DUFRESNE, Claude , FARAND, Julie , HAN, Yongxin , STURINO, Claudio, F.
发明人： BERTHELETTE, Carl , BOYD, Michael , BURCH, Jason , DUFRESNE, Claude , FARAND, Julie , HAN, Yongxin , STURINO, Claudio, F.
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention is directed to ß-carboline sulphonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, inflammation, osteoarthritis, and rheumatoid arthritis. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及作为EP4受体拮抗剂的β-咔啉磺酰脲衍生物，其可用于治疗EP4介导的疾病或病症，例如急性和慢性疼痛，炎症，骨关节炎和类风湿性关节炎。还包括药物组合物和使用方法。

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