| Patent(s) and the Corresponding Patented Drug(s) |
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| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2015112445 |
| Title |
6-Phenyl- or 6-(Pyridin-3-Yl)Indazole Derivatives and Methods of Use. |
| Abstract |
Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, R3, R4, R5, R6, and X are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions. |
| Applicant(s) |
Abbvie Inc |
| Representative Drug(s) |
D0J9ZG |
Drug Info
|
IC50 = 1 nM |
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[1] |
|
2
|
D0T2OX
|
Drug Info
|
IC50 = 1.7 nM
|
[1] |
|
3
|
D0V5AG
|
Drug Info
|
IC50 = 2.6 nM
|
[1] |
| Patent ID |
WO2016061228 |
| Title |
Inhibition of Trk Kinase Mediated Tumor Growth and Disease Progression. |
| Abstract |
It has been shown that Compound 1 unexpectedly and potently inhibits TRK kinases, including all three forms of TRK: NTRKl, NTRK2, and NTRK3. Additionally it has been shown that Compound 1 potently inhibits oncogenic mutated forms of TRK kinases, including fusion proteins. By way of exemplification, Compound 1 potently inhibits the NTRKl oncogenic fusion protein TPM3/NTRK1 in cellular assays. Compound 1 inhibits TRK kinase mediated tumor growth in vivo in a TPM3/NTRK1 xenograft model. |
| Applicant(s) |
Deciphera Pharmaceuticals, Llc |
| Representative Drug(s) |
D0FA6S |
Drug Info
|
IC50 = 0.44 nM |
[1] |
| Patent ID |
WO2015089139 |
| Title |
Tropomyosin-Related Kinase (Trk) Inhibitors. |
| Abstract |
Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)). |
| Applicant(s) |
Genzyme Corporation |
| Representative Drug(s) |
D07RLB |
Drug Info
|
IC50 = 0.5 nM |
[1] |
| Patent ID |
WO2014177510 |
| Title |
Polymer Conjugates of Indolocarbazole Compounds In The Treatment of Pruritus. |
| Abstract |
The present invention is directed to the novel use of polymer conjugates of a class of indolocarbazole compounds for the prevention, alleviation or/and treatment of pruritus, particularly of pruritus associated with or caused by dermatological diseases. |
| Applicant(s) |
Creabilis Sa |
| Patent ID |
WO2014105958 |
| Title |
Fused Pyrimidine Compounds and Use Thereof. |
| Abstract |
Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. Fused pyrimidine compounds that are inhibitors of Trk receptors (e.g., Trk A, Trk B and Trk C) are provided also. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer. |
| Applicant(s) |
Medivation Technologies, Inc |
| Representative Drug(s) |
D0NS6S |
Drug Info
|
IC50 = 3 nM |
[1] |
| Patent ID |
WO2014016434 |
| Title |
Derivatives of Azaindazole or Diazaindazole Type for Treating A Cancer Overexpressing Trk. |
| Abstract |
The present invention relates to a compound of following formula (I) or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein. |
| Applicant(s) |
Pierre Fabre Medicament |
| Representative Drug(s) |
D0Y1NH |
Drug Info
|
IC50 = 64 nM |
[2] |
| Patent ID |
WO2010106028 |
| Title |
Use of A Kinase Inhibitor for The Treatment of Thymoma. |
| Abstract |
The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents. |
| Applicant(s) |
Nerviano Medical Sciences S.R.L |
| Representative Drug(s) |
D0AU4G |
Drug Info
|
IC50 = 5 nM |
[2] |
| Patent ID |
WO2007022999 |
| Title |
Polymer Conjugates of K-252A and Derivatives Thereof. |
| Abstract |
The present invention relates to novel polymer conjugates of K-252a and derivatives thereof and to their use for the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of kinase-associated pathologies. In particular, the present invention relates to the prevention, alleviation and treatment of HMGB1-associated pathologies. In a particular aspect, the invention relates to the use of the novel polymer conjugates of K-252a and derivatives thereof in the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of neurological disorders, neuropathies and neurodegenerative disorders of the central and peripheral nervous system. In a further preferred aspect, the invention relates to the use of the polymer conjugates in the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of dermal pathologies, in particular dermal pathologies associated with an excessive keratinocyte proliferation, in particular psoriasis. In a still further aspect, the invention relates to the use of the polymer conjugates in the prevention, alleviation and treatment of NGF-related pain. More specifically, the present invention relates to a polymer conjugate of K-252a and derivatives thereof, wherein the polymer is polyethylene glycol or methoxy-polyethylene glycol formula (I). |
| Applicant(s) |
Creabilis Therapeutics Spa Traversa, et al |
