Patent(s) and the Corresponding Patented Drug(s) |
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World Intellectual Property Organization (WIPO) |
Patent ID |
WO2013116663 |
Title |
Novel Cysteine Protease Inhibitors and Uses Thereof. |
Abstract |
The invention provides for novel cysteine protease inh ibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors. |
Applicant(s) |
The Trustes of Columbia University In the City of New York |
Representative Drug(s) |
D05LZV |
Drug Info
|
Ki = 50 nM |
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[1] |
2
|
D0HZ1Z
|
Drug Info
|
Ki = 50 nM
|
[1] |
3
|
D0OI2F
|
Drug Info
|
Ki = 100 nM
|
[1] |
4
|
D0WS4U
|
Drug Info
|
Ki > 1000 nM
|
[1] |
5
|
D03ZOR
|
Drug Info
|
N.A.
|
[1] |
6
|
D08CGI
|
Drug Info
|
N.A.
|
[1] |
7
|
D0FG4C
|
Drug Info
|
N.A.
|
[1] |
8
|
D0IO8Y
|
Drug Info
|
N.A.
|
[1] |
9
|
D0KA3L
|
Drug Info
|
N.A.
|
[1] |
10
|
D0L3RN
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2013163567 |
Title |
Novel Alpha-Helical Peptidomimetic Inhibitors and Methods Using Same. |
Abstract |
The present invention includes a novel class of highly specific protease inhibitors. In one embodiment, the inhibitors of the invention are a-helical in structure. In another embodiment, the present invention represents the first demonstration of a highly specific cysteine protease inhibitor. The invention includes a composition comprising a peptide, or a salt thereof, having at least one a-helix, wherein the peptide inhibits a protease. In one embodiment, the peptide comprises at least two cysteine residues, wherein the at least two cysteine residues occupy i,i+4 positions in the peptide and are covalently connected through a linker. In another embodiment, the linker comprises alpha, alpha' -meta-xylylene. |
Applicant(s) |
The Trustes of the University of Pennsylvania |
Representative Drug(s) |
D06LLT |
Drug Info
|
Ki = 11000 nM |
[1] |
Patent ID |
WO2013014314 |
Title |
Derivatives of 5-Azolone As Calpain Inhibitors. |
Abstract |
The invention relates to compounds derived from 4-arylmethylene-1,3-azol-5-one, with or without amino substitutes in the R1 position, with activity as calpain inhibitors. Said compounds have the general formula (I), where R1, R2, X, Y and W have the meaning mentioned in the description and in the claims, the tautomers and the possible salts thereof. In particular, said compounds have the general formulae (l-A.), (I-B.) y (l-C), where R1, R2, R3, R4, R5 X, Y and Z have the meaning mentioned in the description and the claims, the tautomers and the possible salts thereof. Compounds (I) can be used in preventive or therapeutic treatment of disorders related to elevated levels of calpain activity. |
Applicant(s) |
Univ Alcala Henares |
Representative Drug(s) |
D0U2JU |
Drug Info
|
Inhibitory activity = 99.4 % |
[1] |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US20128283363 |
Title |
Carboxamide Compounds and Their Use As Calpain Inhibitors. |
Representative Drug(s) |
D0H0LO |
Drug Info
|
N.A. |
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[1] |
2
|
D0XC2D
|
Drug Info
|
N.A.
|
[1] |