IN2012DN03824A - - Google Patents

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Publication number
IN2012DN03824A
IN2012DN03824A IN3824DEN2012A IN2012DN03824A IN 2012DN03824 A IN2012DN03824 A IN 2012DN03824A IN 3824DEN2012 A IN3824DEN2012 A IN 3824DEN2012A IN 2012DN03824 A IN2012DN03824 A IN 2012DN03824A
Authority
IN
India
Prior art keywords
antagonists
pcsk9
disclosed
methods
present
Prior art date
Application number
Inventor
Peter Peizhi Luo
Yan Ni
Kevin Caili Wang
Mark Hsieh
Xinwei Wang
Feng Dong
Andrei Golosov
Weirong Wang
Yan Li
Pingyu Zhong
Laurence B Peterson
Rose Cubbon
Sujata Sharma
Jon Condra
Jun Lu
Gopalakrishnan Parthasarathy
Stephen Soisson
Noel Byrne
Original Assignee
Merck Sharp & Dohme
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of IN2012DN03824A publication Critical patent/IN2012DN03824A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/40—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/21—Immunoglobulins specific features characterized by taxonomic origin from primates, e.g. man
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/55—Fab or Fab'
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/94—Stability, e.g. half-life, pH, temperature or enzyme-resistance
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide

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.
IN3824DEN2012 2009-10-30 2010-10-29 IN2012DN03824A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25673209P 2009-10-30 2009-10-30
US32314810P 2010-04-12 2010-04-12
PCT/US2010/054714 WO2011053783A2 (en) 2009-10-30 2010-10-29 Ax213 and ax132 pcsk9 antagonists and variants

Publications (1)

Publication Number Publication Date
IN2012DN03824A true IN2012DN03824A (en) 2015-08-28

Family

ID=43922999

Family Applications (1)

Application Number Title Priority Date Filing Date
IN3824DEN2012 IN2012DN03824A (en) 2009-10-30 2010-10-29

Country Status (8)

Country Link
US (1) US8877900B2 (en)
EP (1) EP2493507A4 (en)
JP (1) JP2013509194A (en)
CN (1) CN102639150A (en)
AU (1) AU2010313324A1 (en)
CA (1) CA2777542A1 (en)
IN (1) IN2012DN03824A (en)
WO (1) WO2011053783A2 (en)

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* Cited by examiner, † Cited by third party
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Also Published As

Publication number Publication date
EP2493507A4 (en) 2013-11-20
US20120213794A1 (en) 2012-08-23
US8877900B2 (en) 2014-11-04
AU2010313324A1 (en) 2012-04-12
JP2013509194A (en) 2013-03-14
CA2777542A1 (en) 2011-05-05
WO2011053783A2 (en) 2011-05-05
EP2493507A2 (en) 2012-09-05
WO2011053783A3 (en) 2011-07-28
CN102639150A (en) 2012-08-15

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