Patent(s) and the Corresponding Patented Drug(s) |
Top |
World Intellectual Property Organization (WIPO) |
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 = 21000 nM |
[1] |
Patent ID |
WO2012151319 |
Title |
Cathepsin Inhibitors for The Treatment of Bone Cancer and Bone Cancer Pain. |
Abstract |
The present invention is directed to methods of using compounds that are inhibitors of cysteine proteases, in particular, of both cathepsins S and K and optionally further cathepsins B and/or L in treating bone cancer. The present invention is directed to pharmaceutical compositions comprising these compounds for treating bone cancer and bone cancer pain, especially the pain associated with metastasis. A single compound can be used to ameliorate the pain, the injury to bone, while also reducing tumor growth, the risk of metastasis and/or invasiveness of the cancer. |
Applicant(s) |
Virobay, Inc. Booth, Robert |
Representative Drug(s) |
D06XCD |
Drug Info
|
IC50 = 0.009 nM |
[2] |
Patent ID |
WO2010121918 |
Title |
Proline Derivatives As Cathepsin Inhibitors. |
Abstract |
The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament. |
Applicant(s) |
F. Hoffmann-La Roche Ag |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Patent ID |
WO2009136997 |
Title |
Inhibitors of Human Cathepsin L, Cathepsin B, and Cathepsin S. |
Abstract |
The present invention is directed to novel protease inhibitors that are specific for cathepsin L, cathepsin B, and cathepsin S. Accordingly, the present invention encompasses compositions and methods for treating and preventing diseases and disorders associated with cathepsin L, cathepsin B, or cathepsin S function or activity. |
Applicant(s) |
The Trustes of the University of Pennsylvania |
Representative Drug(s) |
D06XTA |
Drug Info
|
IC50 = 56 nM |
[2] |
Patent ID |
WO2009112839 |
Title |
Compounds. |
Abstract |
A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain. |
Applicant(s) |
Amura Therapeutics Limited |
Representative Drug(s) |
D0QM0D |
Drug Info
|
Ki = 38 nM |
[2] |
Patent ID |
WO2010056877 |
Title |
Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S. |
Representative Drug(s) |
D05OIU |
Drug Info
|
Ki < 100 nM |
[2] |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US8680152 |
Title |
Cathepsin Inhibitors for The Treatment of Bone Cancer and Bone Cancer Pain. |
Representative Drug(s) |
D06XCD |
Drug Info
|
IC50 = 0.009 nM |
[2] |
Patent ID |
US8163793 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Patent ID |
US20150307507 |
Title |
3-Oxo-Tetrahydro-Furo[3,2-B]Pyrrol-4(5H)-Yl Derivatives I As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0MR9V |
Drug Info
|
Ki = 12 nM |
[2] |
Patent ID |
US20150307472 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
US20120282267 |
Title |
Cathepsin Inhibitors for The Treatment of Bone Cancer and Bone Cancer Pain. |
Representative Drug(s) |
D06XCD |
Drug Info
|
IC50 = 0.009 nM |
[2] |
Patent ID |
US20110207726 |
Title |
Inhibitors of Human Cathepsin L, Cathepsin B and Cathepsin S and Therapeutic Uses Thereof. |
Representative Drug(s) |
D06XTA |
Drug Info
|
IC50 = 56 nM |
[2] |
Patent ID |
US20100267722 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
European Patent Office (EPO) |
Patent ID |
EP2888244 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
EP2421826 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Patent ID |
EP2361243 |
Title |
Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S. |
Representative Drug(s) |
D05OIU |
Drug Info
|
Ki < 100 nM |
[2] |
Japan Patent Office (JPO) |
Patent ID |
JP5540004 |
Title |
Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S. |
Representative Drug(s) |
D05OIU |
Drug Info
|
Ki < 100 nM |
[2] |
Patent ID |
JP5518997 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Patent ID |
JP201553099 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
JP2012524116 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Patent ID |
JP2012508758 |
Title |
Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S. |
Representative Drug(s) |
D05OIU |
Drug Info
|
Ki < 100 nM |
[2] |
China National Intellectual Property Administration (CNIPA) |
Patent ID |
CN104583198 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
CN102731344 |
Title |
Preparation of Hydrazine Nitrile Compounds As Cathepsin Inhibitors. |
Representative Drug(s) |
D04VGR |
Drug Info
|
Ki = 0.0031 nM |
[2] |
Patent ID |
CN102405211 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Patent ID |
CN102264695 |
Title |
Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S. |
Representative Drug(s) |
D05OIU |
Drug Info
|
Ki < 100 nM |
[2] |
Russian Federal Service for Intellectual Property (Rospatent) |
Patent ID |
RU2535479 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Portuguese Institute of Industrial Property (PINPI) |
Patent ID |
PT2421826 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Intellectual Property Office of New Zealand (IPONZ) |
Patent ID |
NZ595073 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Mexican Institute of Industrial Property (IMPI) |
Patent ID |
MX2015002026 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Korean Intellectual Property Office (KIPO) |
Patent ID |
KR2015044947 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
KR2011140136 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Patent ID |
KR1320790 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Intellectual Property Office in India (IP India) |
Patent ID |
IN2015DN00962 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
IN2011KN02004 |
Title |
Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S. |
Representative Drug(s) |
D05OIU |
Drug Info
|
Ki < 100 nM |
[2] |
Israel Patent Office (ILPO) |
Patent ID |
IL237128 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
IL215065 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Spanish Patent and Trademark Office (SPTO) |
Patent ID |
ES2436550 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Trademark and Patent Offices of Costa Rica (CRTPO) |
Patent ID |
CR20150073 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Canadian Intellectual Property Office (CIPO) |
Patent ID |
CA2879796 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
CA2758210 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Patent ID |
CA2743749 |
Title |
Preparation of Fluoroalkyl Amino Acid Amides As Inhibitors of Cathepsin B, K, L, F, or S. |
Representative Drug(s) |
D05OIU |
Drug Info
|
Ki < 100 nM |
[2] |
Intellectual Property Office of Australia (IP Australia) |
Patent ID |
AU2013305102 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |
Patent ID |
AU2010241084 |
Title |
Preparation of Proline Dipetidyl Nitrile Derivatives As Cathepsin Particularly Cathepsin S and L Inhibitor. |
Representative Drug(s) |
D0X1AF |
Drug Info
|
IC50 = 0.29 nM |
[2] |
Argentinean National Institute of Industrial Property (AINPI) |
Patent ID |
AR92172 |
Title |
Novel Pyridine Derivatives As Cathepsin Inhibitors and Their Preparation. |
Representative Drug(s) |
D0JD5W |
Drug Info
|
IC50 = 0.6 nM |
[2] |