Muthukumar R Ramaswamy

US Patent:

7030084, Apr 18, 2006

Filed:

Feb 10, 2004

Appl. No.:

10/774903

Inventors:

Nnochiri N. Ekwuribe - Cary NC, US
Muthukumar Ramaswamy - Cary NC, US
Jayanthi Rajagopalan - Cary NC, US

Assignee:

Nobex Corporation - Durham NC

International Classification:

A61K 38/28
C07K 14/62
A61K 38/02
C07K 2/00

US Classification:

514 3, 514 2, 514 21, 530303, 530345, 530410

Abstract:

The present invention relates generally to hydrolyzable drug-oligomer conjugates, pharmaceutical compositions comprising such conjugates, and to methods for making and using such conjugates and pharmaceutical compositions. For example, a conjugate of insulin, PEG, and oleic acid can be orally administered.

US Patent:

7169889, Jan 30, 2007

Filed:

Jun 19, 2000

Appl. No.:

10/018879

Inventors:

Nnochiri N. Ekwuribe - Cary NC, US
Muthukumar Ramaswamy - Cary NC, US
Jayanthi Rajagopalan - Cary NC, US

Assignee:

Biocon Limited - Bangalore

International Classification:

A61K 38/28
C07K 14/62

US Classification:

530303, 514 3

Abstract:

The present invention relates generally to hydrolyzable drug-oligomer conjugates, pharmaceutical compositions comprising such conjugates, and to methods for making and using such conjugates and pharmaceutical compositions. For example, a conjugate of insulin, PEG, and oleic acid can be orally administered.

US Patent:

61911054, Feb 20, 2001

Filed:

Oct 27, 1997

Appl. No.:

8/958383

Inventors:

Nnochiri Nkem Ekwuribe - Cary NC
Muthukumar Ramaswamy - Cary NC
Balasingam Radhakrishnan - Chapel Hill NC
HameedSulthan S. Allaudeen - Durham NC

Assignee:

Protein Delivery, Inc. - Durham NC

International Classification:

A61K 3838
C07K 1462

US Classification:

514 3

Abstract:

A therapeutic formulation comprising a microemulsion of a therapeutic agent in free and/or conjugatively coupled form, wherein the microemulsion comprises a water-in-oil (w/o) microemulsion including a lipophilic phase and a hydrophilic phase, and has a hydrophilic and lipophilic balance (HLB) value between 3 and 7, wherein the therapeutic agent may for example be selected from the group consisting of insulin, calcitonin, ACTH, glucagon, somatostatin, somatotropin, somatomedin, parathyroid hormone, erythropoietin, hypothalamic releasing factors, prolactin, thyroid stimulating hormones, endorphins, enkephalins, vasopressin, non-naturally occurring opioids, superoxide dismutase, interferon, asparaginase, arginase, arginine deaminease, adenosine deaminase, ribonuclease, trypsin, chymotrypsin, papain, Ara-A (Arabinofuranosyladenine), Acylguanosine, Nordeoxyguanosine, Azidothymidine, Dideoxyadenosine, Dideoxycytidine, Dideoxyinosine Floxuridine, 6-Mercaptopurine, Doxorubicin, Daunorubicin, or I-darubicin, Erythromycin, Vancomycin, oleandomycin, Ampicillin; Quinidine and Heparin. In a particular aspect, the invention comprises an insulin composition suitable for parenteral as well as non-parenteral administration, preferably oral or parenteral administration, comprising insulin covalently coupled with a polymer including (i) a linear polyalkylene glycol moiety and (ii) a lipophilic moiety, wherein the insulin, the linear polyalkylene glycol moiety and the lipophilic moiety are conformationally arranged in relation to one another such that the insulin in the composition has an enhanced in vivo resistance to enzymatic degradation, relative to insulin alone. The microemulsion compositions of the invention are usefully employed in therapeutic as well as non-therapeutic, e. g.

US Patent:

63096331, Oct 30, 2001

Filed:

Jun 19, 1999

Appl. No.:

9/336548

Inventors:

Nnochiri Ekwuribe - Cary NC
Muthukumar Ramaswamy - Cary NC
Jayanthi Sethuraman Rajagopalan - Cary NC

Assignee:

Nobex Corporation - Research Triangle Park NC

International Classification:

A61K 9107
A61K 3817
A61K 3828
A61K 39385
C07K 1113

US Classification:

424 851

Abstract:

The invention provides a drug-oligomer conjugate having the following general formula: ##STR1## wherein D is a therapeutic drug moiety; H and H' are each a hydrophilic moiety, independently selected from the group consisting of straight or branched PEG polymers having from 2 to 130 PEG subunits, and sugars; L is a lipophilic moiety selected from the group consisting of alkyl groups having 2-26 carbon atoms, cholesterol, adamantane and fatty acids; o is a number from 1 to the maximum number of covalent bonding sites on H; m+n+p together have a value of at least one and not exceeding the total number of covalent bonding sites on D for the --H', --L and --H--L substituents; the H--L bond(s) are hydrolyzable and the D--L' bond(s), when present, are hydrolyzable; the conjugate being further characterized by one of the following: (i) m is 0 and p is at least 1; (ii) n is 0 and p is at least 1; (iii) m and n are each 0 and p is at least 1; (iv) p is 0 and m and n are each at least 1. The therapeutic drug moiety is preferably a therapeutic protein or peptide, preferably insulin or a functional equivalent thereof.