Laura Lawrence Blumberg

US Patent:

8592427, Nov 26, 2013

Filed:

Jun 24, 2011

Appl. No.:

13/168497

Inventors:

Laura Cook Blumberg - Lincoln MA, US
Julius F. Remenar - Framingham MA, US
Tarek A. Zeidan - Watertown MA, US

Assignee:

Alkermes Pharma Ireland Limited - Dublin

International Classification:

A61K 31/497
C07D 401/00

US Classification:

51425307, 544363

Abstract:

The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

US Patent:

20110003828, Jan 6, 2011

Filed:

Jun 24, 2010

Appl. No.:

12/823102

Inventors:

Laura Cook Blumberg - Lincoln MA, US
Julius F. Remenar - Framingham MA, US
Tarek A. Zeidan - Watertown MA, US

International Classification:

A61K 31/497
A61K 31/4439
A61K 31/427
C07D 471/04
C07D 401/12
C07D 417/14
C07D 417/12
A61P 3/10

US Classification:

51425304, 51425404, 514338, 514369, 544362, 544363, 544368, 5462701, 548183

Abstract:

The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

US Patent:

20110166156, Jul 7, 2011

Filed:

Dec 23, 2010

Appl. No.:

12/978274

Inventors:

Laura Cook Blumberg - Lincoln MA, US

Assignee:

Alkermes, Inc. - Waltham MA

International Classification:

A61K 31/496
C07D 239/70
A61K 31/519
C07D 417/14
C07D 413/04
A61K 31/454
A61P 25/18

US Classification:

51425404, 544282, 51425941, 544368, 546198, 514321

Abstract:

Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed.

US Patent:

20110166194, Jul 7, 2011

Filed:

Dec 23, 2010

Appl. No.:

12/978298

Inventors:

Laura Cook Blumberg - Lincoln MA, US

Assignee:

Alkermes, Inc. - Waltham MA

International Classification:

A61K 31/407
C07D 491/04
A61P 25/18

US Classification:

514410, 548421

Abstract:

Compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed:wherein R-R, G, N and A are as defined in the written description.

US Patent:

20120015866, Jan 19, 2012

Filed:

Dec 23, 2010

Appl. No.:

12/978273

Inventors:

Laura Cook Blumberg - Lincoln MA, US

Assignee:

Alkermes, Inc. - Waltham MA

International Classification:

A61K 38/06
A61P 37/08
A61K 31/519
C07D 471/04
C07K 5/097

US Classification:

514 13, 544282, 530331, 51425941

Abstract:

The present invention relates to prodrugs of parent drug compounds containing heteroaromatic NH groups.

US Patent:

20120202823, Aug 9, 2012

Filed:

Dec 22, 2011

Appl. No.:

13/335405

Inventors:

Tarek A. Zeidan - Watertown MA, US
Laura Cook Blumberg - Lincoln MA, US

International Classification:

A61K 31/496
C07D 401/14

US Classification:

51425211, 544357

Abstract:

The present invention accomplishes this by having multiple molecules of parent drugs attached to carrier moieties and by extending the period during which the parent drug is released and absorbed after administration to the patient and providing a longer duration of action per dose than the parent drug itself. Prodrug conjugates are suitable for sustained delivery of heteroaryl, lactam- amide-, imide-, sulfonamide-, carbamate-, urea-, benzamide-, acylaniline-, cyclic amide- and tertiary amine-containing parent drugs that are substituted at the amide nitrogen or oxygen atom with labile aldehyde-linked prodrug moieties. The carrier groups of the prodrugs can be hydrophobic to reduce the polarity and solubility of the parent drug under physiological conditions.

US Patent:

20130005755, Jan 3, 2013

Filed:

Jun 29, 2012

Appl. No.:

13/537544

Inventors:

Laura Cook Blumberg - Lincoln MA, US
Derrick Arnelle - Arlington MA, US

International Classification:

A61K 31/485
A61K 31/513
C07D 489/08
A61P 11/00
A61P 1/08
A61P 25/06
A61P 25/30
A61P 3/04
A61P 1/00
C07D 401/12
A61P 25/04

US Classification:

514274, 544311, 546 74, 514289

Abstract:

The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof:

US Patent:

20130096089, Apr 18, 2013

Filed:

Sep 7, 2012

Appl. No.:

13/607066

Inventors:

Julius F. Remenar - Farmingham MA, US
Laura Cook Blumberg - Lincoln MA, US
Tarek A. Zeidan - Watertown MA, US

International Classification:

C07D 401/14
C07F 9/6558
C07D 471/04
C07D 417/14
C07D 413/10
C07D 401/12
C07D 413/14

US Classification:

514 82, 544363, 51425307, 544357, 51425211, 544337, 544121, 5142352, 544368, 51425404, 51425402, 544362, 51425304

Abstract:

Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.