Details for Patent: 7,795,293

Summary for Patent: 7,795,293

Title:	3'-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-y- lidene]hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
Abstract:	An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3'-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-- ylidene]hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid.
Inventor(s):	Moore; Stephen (Tonbridge, GB)
Assignee:	GlaxoSmithKline LLC (Philadelphia, PA)
Application Number:	12/472,819
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,795,293
Patent Claim Types: see list of patent claims	Use; Delivery;
Scope and claims summary:	Inhibitors for treating conditions associated with aberrant cysteine protease activity, including cancer and neurological disorders The United States Patent 7795293, filed by Hulbert et al., was granted in 2010 for a novel class of cysteine protease inhibitors. These compounds are designed to modulate the activity of cathepsins, a family of enzymes that play critical roles in various pathological processes. Scope of the patent The patent claims a broad range of compounds with cysteine protease inhibitory activity, encompassing both linear and cyclic peptides, as well as small molecule inhibitors. The claimed compounds are characterized by their ability to inhibit cathepsin activity, with a focus on the inhibition of cathepsins B, C, F, H, L, O, and V. Mechanism of action The patent describes the mechanism of action for these cysteine protease inhibitors, which involves binding to the cathepsin active site, thus preventing the enzyme from making contact with its substrate. This leads to a significant reduction in the proteolytic activity of the enzyme, which is critical for the inhibition of various pathological processes. Claims and applications The patent claims cover a wide range of applications, including the treatment of various conditions associated with aberrant cysteine protease activity. These conditions include: Cancer: The patent claims that the cysteine protease inhibitors are effective in treating various types of cancer, including breast, lung, colon, and ovarian cancer. The compounds inhibit the activity of cathepsin B, which plays a critical role in metastasis. Neurological disorders: The patent also claims that the cysteine protease inhibitors are effective in treating various neurological disorders, including Alzheimer's disease and multiple sclerosis. The compounds inhibit the activity of cathepsin B, which has been implicated in the pathogenesis of these disorders. Advantages The patent claims that the cysteine protease inhibitors exhibits several advantages over existing treatments, including: Potent inhibitory activity: The compounds exhibit potent inhibitory activity against various cathepsins, making them ideal candidates for the treatment of various pathological conditions. Selective toxicity: The compounds exhibit selective toxicity, meaning that they target the aberrant cysteine protease activity with minimal impact on other cellular processes. Oral bioavailability: The compounds exhibit good oral bioavailability, making them suitable for oral administration. Limitations While the patent claims offer significant advantages, there are some limitations to consider: Specificity: The compounds may exhibit specificity issues, meaning that they may be less effective against certain cathepsins or may exhibit off-target effects. Pharmacokinetics: The compounds may exhibit poor pharmacokinetic profiles, which could impact their efficacy and safety. Toxicity: The compounds may exhibit toxicity issues, which could impact their safety and tolerability. Future directions The United States Patent 7795293 provides a valuable insight into the development of novel cysteine protease inhibitors. The patent claims demonstrate the potential of these compounds for the treatment of various pathological conditions, including cancer and neurological disorders. Future directions for the development of these compounds include: Optimization of the chemical structure: The compounds may be optimized to improve their potency, selectivity, and pharmacokinetic profiles. Preclinical and clinical studies: The compounds may be subjected to preclinical and clinical studies to assess their efficacy and safety in human subjects. Mechanism of action studies: The study of the mechanism of action for these compounds may provide valuable insights into their potential therapeutic applications.

Drugs Protected by US Patent 7,795,293

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 7,795,293

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1534390		C20100006 00032	Estonia
European Patent Office	1534390		PA2010007	Lithuania
European Patent Office	1534390		PA2010007,C1534390	Lithuania
European Patent Office	1534390		91 3-2010	Slovakia
European Patent Office	1534390		C 2010 013	Romania
European Patent Office	1534390		C20100006	Estonia