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A relevant excerpt from the patent application:

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Statement of Beneficial Ownership (sc 13d) "Edgar (US Regulatory)" - 1/18/2017 5:22:01 PM
Ariad Pharmaceuticals, Inc. Acquisition May Not Be in the Best Interests of ARIA Shareholders "PR Newswire (US)" - 1/18/2017 10:48:00 AM
Statement of Changes in Beneficial Ownership (4) "Edgar (US Regulatory)" - 1/17/2017 5:08:32 PM
Written Communication Relating to an Issuer or Third Party (sc To-c) "Edgar (US Regulatory)" - 1/11/2017 5:24:26 PM
Statement of Changes in Beneficial Ownership (4) "Edgar (US Regulatory)" - 1/10/2017 6:18:41 PM
Written Communication Relating to an Issuer or Third Party (sc To-c) "Edgar (US Regulatory)" - 1/10/2017 5:30:12 PM
Current Report Filing (8-k) "Edgar (US Regulatory)" - 1/10/2017 3:06:07 PM
Amended Statement of Beneficial Ownership (sc 13d/a) "Edgar (US Regulatory)" - 1/10/2017 8:13:52 AM
Written Communication Relating to an Issuer or Third Party (sc To-c) "Edgar (US Regulatory)" - 1/9/2017 5:13:19 PM
Harwood Feffer LLP Announces Investigation of ARIAD Pharmaceuticals, Inc. "PR Newswire (US)" - 1/9/2017 5:05:00 PM
Written Communication by the Subject Company Relating to a Third Party Tender Offer (sc14d9c) "Edgar (US Regulatory)" - 1/9/2017 4:38:49 PM
Rigrodsky & Long, P.A. Announces Investigation Of Buyout "Business Wire" - 1/9/2017 12:46:00 PM
ARIAD Enters into Definitive Agreement to Be Acquired by Takeda for $5.2 Billion "Business Wire" - 1/9/2017 8:02:00 AM
Takeda to Acquire ARIAD Pharmaceuticals, Inc. "Business Wire" - 1/9/2017 8:00:00 AM
ARIAD to Present at the 35th Annual J.P. Morgan Healthcare Conference "Business Wire" - 1/3/2017 7:35:00 AM
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Current Report Filing (8-k) "Edgar (US Regulatory)" - 12/8/2016 8:01:52 AM
Current Report Filing (8-k) "Edgar (US Regulatory)" - 12/7/2016 4:07:44 PM
ARIAD’s Investigational Medicine Brigatinib Demonstrated 15.6 Month Systemic Median Progression-Free Survival in ALTA Study "Business Wire" - 12/7/2016 7:35:00 AM
ARIAD Announces Data Presentations at American Society of Hematology Meeting "Business Wire" - 12/6/2016 7:35:00 AM
ARIAD Presents Updated Brigatinib Data with 18.4 Months Median Intracranial Progression Free Survival (PFS) in ALK+ NSCLC Pat... "Business Wire" - 12/5/2016 7:35:00 AM
ARIAD to Host Webcast and Conference Call on Brigatinib Data Presentations at the World Conference on Lung Cancer "Business Wire" - 12/2/2016 4:05:00 PM
Current Report Filing (8-k) "Edgar (US Regulatory)" - 11/30/2016 4:06:56 PM
ARIAD Announces FDA Full Approval & Label Update for Iclusig® (ponatinib) Based on Long-Term Efficacy & Safety Data from Pha... "Business Wire" - 11/29/2016 7:35:00 AM
Current Report Filing (8-k) "Edgar (US Regulatory)" - 11/18/2016 4:07:44 PM
iandy   Friday, 07/12/13 07:16:59 AM
Re: jaybe post# 32123
Post # of 80338 
A relevant excerpt from the patent application:

>There is no cure for PD. Current therapy relies heavily on replenishing dopamine by giving patients oral doses of a dopaminergic agent like the dopamine precursor levodopa (alone or in the combination carbidopa levodopa) or a dopamine agonist. Such therapy can provide relief, although with the increasing risk of serious side effects and often with diminishing therapeutic results, requiring increasing doses as treatment continues, and more serious side effects. There is a profound need for additional therapeutics for PD.

c-Abl is a major regulator of parkin function and phosphorylates parkin on tyrosine 143. This phosphorylation inhibits parkin's E3 ubiquitin ligase activity leading to

accumulation of AIMP2 and FBP1 and loss of parkin's cytoprotective function and cell death. One Abl inhibitor, STI-571 , has been found to maintain parkin in a catalytically active and neuroprotective state by preventing phosphorylation of parkin. As such, it is believed that inhibition of c-Abl presents a viable approach for the treatment of PD. o, et al., PNAS, 107(38), 16691 -16696 (2010). One challenge of using STI-571 to treat PD is that it has poor penetration of the blood-brain barrier as demonstrated in mice and humans. Thus, there is a need for Abl inhibitors that cross the blood-brain barrier for the treatment of PD.

Applicant's own WO 2007/075869, which is hereby incorporated herein by reference for all purposes, discloses certain compounds that inhibit inter alia Abl. One notable Abl inhibitor is ponatinib, which is currently the subject of a clinical trial to determine the efficacy of ponatinib in patients with chronic myeloid leukemia (CML) in chronic phase (CP), accelerated phase (AP) or blast phase (BP) or with Ph positive (Ph+) acute lymphoblastic leukemia (ALL) who either are resistant or intolerant to either dasatinib or nilotinib, or have the T315I mutation of Bcr-Abl (clinical trials.gov identifier NCT01207440). WO 2007/075869 does not explicitly mention using such Abl inhibitors for the treatment of PD.

SUMMARY

It has been unexpectedly discovered that certain Abl inhibitors cross the blood brain barrier and are useful in the regulation of parkin and accordingly for the treatment of PD.<




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