公开(公告)号：WO2011053665A1

公开(公告)日：2011-05-05

申请号：PCT/US2010/054376

申请日：2010-10-28

Applicant: MERCK SHARP & DOHME CORP. ,  NI, Yan, G. ,  PANDIT, Shilpa

Inventor： NI, Yan, G. ,  PANDIT, Shilpa

IPC: G01N33/53 ,  C12P21/08

CPC classification number: G01N33/573 ,  G01N33/6893 ,  G01N2333/96433 ,  G01N2800/32

Abstract: Methods of using PCSK9 antagonists. More specifically, methods for measuring circulating PCSK9 levels in a biological sample by means of an immunoassay.

Abstract translation: 使用PCSK9拮抗剂的方法。 更具体地，通过免疫测定来测量生物样品中的循环PCSK9水平的方法。

公开(公告)号：WO2009100318A1

公开(公告)日：2009-08-13

申请号：PCT/US2009/033369

申请日：2009-02-06

Applicant: MERCK & CO., INC. ,  CONDRA, Jon, H. ,  CUBBON, Rose, M. ,  HAMMOND, Holly, A. ,  MCCABE, Timothy ,  PANDIT, Shilpa ,  PETERSON, Laurence, B. ,  SANTORO, Joseph, C. ,  SITLANI, Ayesha ,  WOOD, Dana, D. ,  MACH, Henryk ,  YODER, Heidi ,  GREGORY, Sonia, M. ,  BLUE, Jeffrey, T. ,  WANG, Kevin ,  LUO, Peter ,  NAWROCKI, Denise, K. ,  ZHONG, Pingyu ,  DONG, Feng ,  LI, Yan

Inventor： CONDRA, Jon, H. ,  CUBBON, Rose, M. ,  HAMMOND, Holly, A. ,  MCCABE, Timothy ,  PANDIT, Shilpa ,  PETERSON, Laurence, B. ,  SANTORO, Joseph, C. ,  SITLANI, Ayesha ,  WOOD, Dana, D. ,  MACH, Henryk ,  YODER, Heidi ,  GREGORY, Sonia, M. ,  BLUE, Jeffrey, T. ,  WANG, Kevin ,  LUO, Peter ,  NAWROCKI, Denise, K. ,  ZHONG, Pingyu ,  DONG, Feng ,  LI, Yan

IPC: C07K16/40 ,  C12N9/64 ,  A61K39/395 ,  C12N15/13 ,  A61P3/06

CPC classification number: C07K16/40 ,  A61K2039/505 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/76 ,  C07K2317/77 ,  C07K2317/92 ,  C12N9/6424

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 ('PCSK9') are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

Abstract translation: 公开了人前体蛋白转化酶枯草杆菌蛋白酶-Kexin 9型（'PCSK9'）的拮抗剂。 所公开的拮抗剂在抑制PCSK9功能方面是有效的，因此，呈现用于治疗与PCSK9活性相关的病症的所需拮抗剂。 本发明还公开了编码所述拮抗剂，载体，宿主细胞和包含拮抗剂的组合物的核酸。 还公开了制备PCSK9特异性拮抗剂的方法以及使用拮抗剂抑制或拮抗PCSK9功能的方法，并且形成了本公开的重要的附加方面。

公开(公告)号：WO2008063382A3

公开(公告)日：2008-12-04

申请号：PCT/US2007023223

申请日：2007-11-02

Applicant: MERCK & CO INC ,  SITLANI AYESHA ,  SPARROW CARL P ,  PANDIT SHILPA ,  CONDRA JON H ,  HAMMOND HOLLY A

Inventor： SITLANI AYESHA ,  SPARROW CARL P ,  PANDIT SHILPA ,  CONDRA JON H ,  HAMMOND HOLLY A

IPC: A61K39/395 ,  C07K16/40

CPC classification number: C07K16/40 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/76 ,  C07K2317/92

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 ("PCSK9") are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

Abstract translation: 公开了人前体蛋白转化酶枯草杆菌蛋白酶-Kexin 9型（“PCSK9”）的拮抗剂。 所公开的拮抗剂在抑制PCSK9功能方面是有效的，因此，在治疗与PCSK9活性相关的病症中使用期望的拮抗剂是有用的。 本发明还公开了编码所述拮抗剂，载体，宿主细胞和包含拮抗剂的组合物的核酸。 还公开了制备PCSK9特异性拮抗剂的方法以及使用拮抗剂抑制或拮抗PCSK9功能的方法，并且形成了本公开的重要的附加方面。

公开(公告)号：WO2008057457A2

公开(公告)日：2008-05-15

申请号：PCT/US2007/023212

申请日：2007-11-02

Applicant: MERCK & CO., INC. ,  SPARROW, Carl, P. ,  SITLANI, Ayesha ,  PANDIT, Shilpa ,  CONDRA, Jon, H. ,  HAMMOND, Holly, A.

Inventor： SPARROW, Carl, P. ,  SITLANI, Ayesha ,  PANDIT, Shilpa ,  CONDRA, Jon, H. ,  HAMMOND, Holly, A.

IPC: A61K39/395

CPC classification number: C07K16/40 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/76 ,  C07K2317/92

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 ("PCSK9") are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

公开(公告)号：WO2010068526A1

公开(公告)日：2010-06-17

申请号：PCT/US2009/066303

申请日：2009-12-02

Applicant: MERCK SHARP & DOHME CORP. ,  NI, Yan ,  SITLANI, Ayesha ,  PANDIT, Shilpa ,  LEWIS, Dale ,  SHEN, Xun ,  LOBO, Sharon ,  MCCABE, Timothy ,  CONDRA, Jon ,  CUBBON, Rose

Inventor： NI, Yan ,  SITLANI, Ayesha ,  PANDIT, Shilpa ,  LEWIS, Dale ,  SHEN, Xun ,  LOBO, Sharon ,  MCCABE, Timothy ,  CONDRA, Jon ,  CUBBON, Rose

IPC: G01N33/53

CPC classification number: C07K16/40 ,  C07K2317/55 ,  G01N33/543 ,  G01N33/573 ,  G01N2333/96433

Abstract: Methods of using PCSK9 antagonists More specifically, methods for measuring circulating PCSK9 levels in a biological sample by means of an immunoassay The immunoassay used can be a solid phase immunoassay, such as a dissociation-enhanced lanthanide fluorescence immunoassay utilizing an E07 capture antibody or coating and a G08 or H23 detecting antibody.

Abstract translation: 使用PCSK9拮抗剂的方法更具体地，通过免疫测定法测量生物样品中的循环PCSK9水平的方法所用的免疫测定可以是固相免疫测定，例如利用E07捕获抗体或涂层的解离增强镧系荧光免疫测定， G08或H23检测抗体。

公开(公告)号：WO2008057457A3

公开(公告)日：2008-12-11

申请号：PCT/US2007023212

申请日：2007-11-02

Applicant: MERCK & CO INC ,  SPARROW CARL P ,  SITLANI AYESHA ,  PANDIT SHILPA ,  CONDRA JON H ,  HAMMOND HOLLY A

Inventor： SPARROW CARL P ,  SITLANI AYESHA ,  PANDIT SHILPA ,  CONDRA JON H ,  HAMMOND HOLLY A

IPC: A61K39/395 ,  C07K16/40

CPC classification number: C07K16/40 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/76 ,  C07K2317/92

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 ("PCSK9") are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

公开(公告)号：WO2008133647A3

公开(公告)日：2009-02-26

申请号：PCT/US2007023169

申请日：2007-11-02

Applicant: MERCK & CO INC ,  SITLANI AYESHA ,  SPARROW CARL P ,  PANDIT SHILPA ,  CONDRA JON H ,  WOOD DANA D ,  FISHER TIMOTHY S

Inventor： SITLANI AYESHA ,  SPARROW CARL P ,  PANDIT SHILPA ,  CONDRA JON H ,  WOOD DANA D ,  FISHER TIMOTHY S

IPC: A61K39/00

CPC classification number: C07K16/40 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/76 ,  C07K2317/92

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 ("PCSK9") are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

Abstract translation: 公开了人前体蛋白转化酶枯草杆菌蛋白酶-Kexin 9型（“PCSK9”）的拮抗剂。 所公开的拮抗剂在抑制PCSK9功能方面是有效的，因此，在治疗与PCSK9活性相关的病症中使用期望的拮抗剂是有用的。 本发明还公开了编码所述拮抗剂，载体，宿主细胞和包含拮抗剂的组合物的核酸。 还公开了制备PCSK9特异性拮抗剂的方法以及使用拮抗剂抑制或拮抗PCSK9功能的方法，并形成了本公开的重要的附加方面。

公开(公告)号：WO2008057459A3

公开(公告)日：2008-11-27

申请号：PCT/US2007023214

申请日：2007-11-02

Applicant: MERCK & CO INC ,  SPARROW CARL P ,  SITLANI AYESHA ,  PANDIT SHILPA ,  CONDRA JON H ,  HAMMOND HOLLY A

Inventor： SPARROW CARL P ,  SITLANI AYESHA ,  PANDIT SHILPA ,  CONDRA JON H ,  HAMMOND HOLLY A

IPC: A61K39/395 ,  C07K16/40

CPC classification number: C07K16/40 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/76 ,  C07K2317/92

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 ("PCSK9") are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

公开(公告)号：WO2008133647A2

公开(公告)日：2008-11-06

申请号：PCT/US2007/023169

申请日：2007-11-02

Applicant: MERCK & CO., INC. ,  SITLANI, Ayesha ,  SPARROW, Carl, P. ,  PANDIT, Shilpa ,  CONDRA, Jon, H. ,  WOOD, Dana, D. ,  FISHER, Timothy, S.

Inventor： SITLANI, Ayesha ,  SPARROW, Carl, P. ,  PANDIT, Shilpa ,  CONDRA, Jon, H. ,  WOOD, Dana, D. ,  FISHER, Timothy, S.

IPC: A61K39/395

CPC classification number: C07K16/40 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/76 ,  C07K2317/92

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 ("PCSK9") are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

Abstract translation: 披露了人类前蛋白转化酶枯草杆菌蛋白酶 - kexin 9型的拮抗剂（“PCSK9”）。 所公开的拮抗剂在抑制PCSK9功能方面是有效的，并因此提供了用于治疗与PCSK9活性相关的病症的理想拮抗剂。 本发明还公开了编码所述拮抗剂，载体，宿主细胞和包含拮抗剂的组合物的核酸。 还公开了制备PCSK9特异性拮抗剂的方法以及使用拮抗剂抑制或拮抗PCSK9功能的方法，并且形成本公开的重要的另外方面。

公开(公告)号：WO2008057458A3

公开(公告)日：2008-05-15

申请号：PCT/US2007/023213

申请日：2007-11-02

Applicant: MERCK & CO., INC. ,  SPARROW, Carl, P. ,  SITLANI, Ayesha ,  PANDIT, Shilpa ,  CONDRA, Jon, H. ,  HAMMOND, Holly, A.

Inventor： SPARROW, Carl, P. ,  SITLANI, Ayesha ,  PANDIT, Shilpa ,  CONDRA, Jon, H. ,  HAMMOND, Holly, A.

IPC: A61K39/395 ,  C07K16/40

Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 ("PCSK9") are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.