Title of Invention

PHARMACEUTICAL DERMAL COMPOSITION USEFUL IN TREATMENT OF DIABETIC COMPLICATIONS

Abstract The present invention provides methods of treating diabetic complications, the methods comprising administering to a patient having or at risk of having diabetic complications, a therapeutically effective amount of a Beta adrenergic receptor antagonist or Beta-blockers. This invention is directed to methods, pharmaceutical composition and kits comprising a Beta adrenergic receptor antagonist, prodrug thereof or a pharmaceutically acceptable salt of the said Beta adrenergic receptor antagonists. This invention further relates to pharmaceutical compositions of beta adrenergic antagonists for the treatment of diabetic complications such as diabetic cataract, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy and diabetic cardiomyopathy, diabetic corneal keraopathy, diabetic dermopathy, diabetic microangiopathy and diabetic wounds.
Full Text FORM 2
THE PATENTS ACT. 1970
(39 of 1970)
And
The Patents Rules, 2003
Provisional / Complete Specification (See section 10 and Rule 13)
1. Title of the invention : Pharmaceutical composition useful in treatment of
diabetic complications
2. Applicant(s)
(a) Name : VLife Sciences Technologies Pvt. Ltd.
(b) Nationality: Indian
(c) Address : 1 Akshay Residency, 50 Anand Park, Aundh, Pune 411007, India



3. Preamble to the description: Inhibitors of aldose reductase are reported which would be highly useful in several diseases including diabetes and diabetic complications.
^ Provisional
/ The following specification
describes the invention
Complete The following specification particularly describes the invention and the manner in which to be performed

4. Description (Descriptional shall start from next page)
5. Claims (Not applicable for provisional specification. Claims should start with the
preamble 'I/We claim' on separate page)
6. Date & signature (To be given at the end of last page of specification)
7. Abstract of the invention (To be given along with complete specification on separate page)

Title: PHARMACEUTICAL COMPOSITION USEFUL IN THE TREATMENT OF DIABETIC COMPLICATIONS
Name of Inventors: Sudhir A. Kulkarni, Reena Gollapudy, Supreet K. Deshpande (VLife Sciences Technologies Pvt. Ltd., Pride Purple Coronet, S.No. 287, Baner Road, Pune-411045, India)
Assignee: VLife Sciences Technologies Pvt. Ltd., 1 Akshay Residency, 50 Anand Park, Aundh, Pune-411007, India
Abstract
In spite of the significant development in the antidiabetic therapy, the complications like neuropathy, retinopathy, nephropathy, various angiopathies and cataract continue to be the major causes of morbidity and mortality in diabetic patients. Patients with all forms of diabetes are vulnerable to these complications especially when high blood sugar levels are not adequately controlled. Complications like retinopathy are so characteristic of diabetes that its presence has been incorporated into the nosologic definition of NIDDM ( non insulin dependent diabetes mellitus). Only hyperglycemia of sufficient magnitude to be associated with retinopathy is classified as NIDDM, while lower levels of hyperglycemia that are not accompanied by retinopathy are classified as mere 'impaired glucose tolerance'. There seem to be different pathogenic mechanisms responsible for the diabetic complications. However excessive formation and accumulation of sorbitol in various tissues is believed to play a major role in the development of debilitating diabetic complications. The enzyme aldose reductase converts excess glucose in to sorbitol using NADPH as a co-factor. Hence much effort has been directed towards the synthesis of aldose reductase inhibitors. Aldose reductase inhibitors hold promise for reducing metabolic nerve injury.

A large number of aldose reductase inhibitors have been assessed for diabetic complications, but the lack of consistent efficacy and adverse effects have prevented their widespread use. The search for efficacious, safe and specific inhibitors of aldose reductase enzyme remains a major pharmaceutical challenge.
The present invention describes the beta adrenergic antagonist drugs (beta blockers) as having potent aldose reductase inhibitory activity. Beta adrenergic antagonists with aldose reductase inhibition activity are therefore useful in the prevention and treatment of various diabetic complications including retinopathy. They are also useful in the treatment of wounds and ocular conditions. Atenolol, Nadolol, Timolol, Metipranolol, Propranolol, Metoprolol, Carteolol, Bisoprolol, Sotalol, Celiprolol, Betaxolol, Levobunolol, Carvedilol, Nebivolol, Arotinolol, Labetalol, and Acebutolol are some of the examples of beta adrenergic antagonist drugs. Therapeutically effective amounts of these drugs could be administered by multiple routes-oral, parenteral, intraocular, subconjunctival and topical with appropriate vehicles.
Present disclosure is premised on the reasoning and the fact that the inhibition of aldose reductase by beta blockers helps in prevention and treatment of diabetic complications, the use of the current compounds based on their aldose reductase inhibiting property is not restricted to the diabetic syndrome.







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Documents:

1960-MUM-2005-CORRESPONDENCE(10-5-2011).pdf

1960-mum-2006-abstract(8-2-2007).pdf

1960-MUM-2006-ABSTRACT(AMENDED)-(18-5-2007).pdf

1960-MUM-2006-ABSTRACT(GRANTED)-(10-11-2011).pdf

1960-MUM-2006-CANCELLED PAGES(2-6-2011).pdf

1960-mum-2006-claims(8-2-2007).pdf

1960-MUM-2006-CLAIMS(AMENDED)-(2-6-2011).pdf

1960-MUM-2006-CLAIMS(AMENDED)-(21-1-2011).pdf

1960-MUM-2006-CLAIMS(GRANTED)-(10-11-2011).pdf

1960-MUM-2006-COPY OF PRESENTATION MADE DURING HEARING(2-6-2011).pdf

1960-mum-2006-correspondence(2-7-2009).pdf

1960-MUM-2006-CORRESPONDENCE(4-5-2011).pdf

1960-MUM-2006-CORRESPONDENCE(IPO)-(14-11-2011).pdf

1960-mum-2006-correspondence(ipo)-(3-9-2009).pdf

1960-mum-2006-description (provisional).pdf

1960-mum-2006-description(complete)-(8-2-2007).pdf

1960-MUM-2006-DESCRIPTION(GRANTED)-(10-11-2011).pdf

1960-mum-2006-form 13(18-5-2007).pdf

1960-mum-2006-form 18(18-5-2007).pdf

1960-mum-2006-form 2(8-2-2007).pdf

1960-MUM-2006-FORM 2(COMPLETE)-(8-2-2007).pdf

1960-MUM-2006-FORM 2(GRANTED)-(10-11-2011).pdf

1960-mum-2006-form 2(title page)-(8-2-2007).pdf

1960-MUM-2006-FORM 2(TITLE PAGE)-(COMPLETE)-(8-2-2007).pdf

1960-MUM-2006-FORM 2(TITLE PAGE)-(GRANTED)-(10-11-2011).pdf

1960-MUM-2006-FORM 2(TITLE PAGE)-(PROVISIONAL)-(29-11-2006).pdf

1960-MUM-2006-FORM 26(30-5-2011).pdf

1960-MUM-2006-FORM 3(29-11-2006).pdf

1960-MUM-2006-FORM 3(3-11-2009).pdf

1960-MUM-2006-FORM 3(8-1-2010).pdf

1960-mum-2006-form-1.pdf

1960-mum-2006-form-2.doc

1960-mum-2006-form-2.pdf

1960-mum-2006-form-3.pdf

1960-mum-2006-form-5.pdf

1960-MUM-2006-OTHER DOCUMENT(18-5-2007).pdf

1960-MUM-2006-REPLY TO EXAMINATION REPORT(21-1-2011).pdf

1960-MUM-2006-REPLY TO HEARING(2-6-2011).pdf

1960-MUM-2006-SPECIFICATION(AMENDED)-(18-5-2007).pdf


Patent Number 249777
Indian Patent Application Number 1960/MUM/2006
PG Journal Number 45/2011
Publication Date 11-Nov-2011
Grant Date 10-Nov-2011
Date of Filing 29-Jan-2007
Name of Patentee VLIFE SCIENCES TECHNOLOGIES PVT. LTD.
Applicant Address 1 AKSHAY RESIDENCY, 50 ANANDPARK, AUNDH, PUNE 411007,
Inventors:
# Inventor's Name Inventor's Address
1 SUDHIR A. KULKARNI VLife Sciences Technologies Pvt. Ltd. Pride Purple Coronet, S. No. 287, Baner Road, Pune 411 045
2 REENA GOLLAPUDY VLife Sciences Technologies Pvt. Ltd. Pride Purple Coronet, S. No. 287, Baner Road, Pune 411 045
3 SUPREET K. DESHPANDE VLife Sciences Technologies Pvt. Ltd. Pride Purple Coronet, S. No. 287, Baner Road, Pune 411 045
PCT International Classification Number A61K31/00
PCT International Application Number N/A
PCT International Filing date
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 NA