Peter J Meltzer

US Patent:

6291512, Sep 18, 2001

Filed:

Sep 27, 2000

Appl. No.:

9/671534

Inventors:

Peter C. Meltzer - Lexington MA
Bertha K. Madras - Newton MA
Paul Blundell - Winchester MA
Zhengming Chen - Woburn MA

Assignee:

Organix, Inc. - Woburn MA
President and Fellows of Harvard College - Cambridge MA

International Classification:

A61K 3138
A61K 3135
C07D33502
C07D31100

US Classification:

514432

Abstract:

New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7- substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

US Patent:

6353105, Mar 5, 2002

Filed:

May 19, 1999

Appl. No.:

09/314441

Inventors:

Peter C. Meltzer - Lexington MA
Bertha K. Madras - Newton MA
Paul Blundell - Winchester MA
Zhengming Chen - Woburn MA

Assignee:

Organix, Inc. - Woburn MA
President and Fellows of Harvard College - Cambridge MA

International Classification:

C07D40100

US Classification:

546125, 546127

Abstract:

New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

US Patent:

6525206, Feb 25, 2003

Filed:

Oct 17, 2000

Appl. No.:

09/691396

Inventors:

Peter C. Meltzer - Lexington MA
Paul Blundell - Winchester MA
Pinglang Wang - Cambridge MA
Bertha K. Madras - Newton MA

Assignee:

President and Fellows of Harvard College - Cambridge MA
Organix, Inc. - Woburn MA

International Classification:

C07D31500

US Classification:

549427

Abstract:

Featured compounds have high monoamine transport affinity and are characterized by one of the following two general formulas set out above. The compounds bind selectively or non-selectively to monoamine transporters. The compounds are useful to treat various medical indications including attention deficit hyperactivity disorder (ADHD), Parkinsons disease, cocaine addiction, smoking cessation, weight reduction, obsessive-compulsive disorder, various forms of depression, traumatic brain injury, stroke, and narcolepsy.

US Patent:

6548041, Apr 15, 2003

Filed:

May 10, 2000

Appl. No.:

09/568106

Inventors:

Peter C. Meltzer - Lexington MA
Paul Blundell - Somerville MA
Bertha K. Madras - Newton MA
Alan J. Fischman - Boston MA
Alun G. Jones - Newton Centre MA
Ashfaq Mahmood - Brookline MA

Assignee:

Organix, Inc. - Woburn MA
President and Fellow of Harvard College - Cambridge MA
The General Hospital Corporation - Boston MA

International Classification:

A61K 5100

US Classification:

424 165, 424 111, 424 93, 546124, 546112, 534 14

Abstract:

Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.

US Patent:

6670375, Dec 30, 2003

Filed:

Jun 6, 2001

Appl. No.:

09/875523

Inventors:

Peter C. Meltzer - Lexington MA
Bertha K. Madras - Newton MA
Paul Blundell - Winchester MA
Zhengming Chen - Woburn MA

Assignee:

Organix, Inc. - Woburn MA
President and Fellows of Harvard College - Cambridge MA

International Classification:

A61K 31439

US Classification:

514304, 546132

Abstract:

New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

US Patent:

6677338, Jan 13, 2004

Filed:

Feb 28, 2002

Appl. No.:

10/085482

Inventors:

Bertha K. Madras - Newton MA
Peter C. Meltzer - Lexington MA

Assignee:

President and Fellows of Harvard College - Cambridge MA
Organix, Inc. - Woburn MA

International Classification:

A61K 31352

US Classification:

5142388, 514320, 514432, 514456, 544173, 544111, 546192, 546200, 549 23, 549283, 549285, 549397

Abstract:

The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.

US Patent:

7026516, Apr 11, 2006

Filed:

Feb 24, 2003

Appl. No.:

10/374892

Inventors:

Peter C. Meltzer - Lexington MA, US
Paul Blundell - Winchester MA, US
Pinglang Wang - Cambridge MA, US
Bertha K. Madras - Newton MA, US

Assignee:

President and Fellows of Harvard College - Cambridge MA
Organix, Inc. - Woburrn MA

International Classification:

C07C 43/02

US Classification:

568626, 558303, 544106

Abstract:

Featured compounds have high monoamine transport affinity and are characterized by one of the following two general formulas set out above. The compounds bind selectively or non-selectively to monoamine transporters. The compounds are useful to treat various medical indications including attention deficit hyperactivity disorder (ADHD), Parkinson's disease, cocaine addiction, smoking cessation, weight reduction, obsessive-compulsive disorder, various forms of depression, traumatic brain injury, stroke, and narcolepsy.

US Patent:

7081238, Jul 25, 2006

Filed:

Aug 17, 2001

Appl. No.:

09/932302

Inventors:

Bertha K. Madras - Newton MA, US
Alan J. Fischman - Boston MA, US
Peter C. Meltzer - Lexington MA, US

Assignee:

The President and Fellows of Harvard College - Cambridge MA
The General Hospital Corporation - Boston MA
Organix, Inc. - Woburn MA

International Classification:

A61K 51/00
A61K 49/00

US Classification:

424 165, 424 91

Abstract:

A method of diagnosing attention deficient-hyperactivity disorder (ADHD) in a human patient by assessing the level of dopamine transporter in at least one region of the patient's central nervous system, where an elevated level of dopamine transporter in the patient is indicative of ADHD. In embodiments of the invention, assessment of dopamine transporter levels includes assessing binding of a dopamine transporter ligand to the dopamine transporters using PET or SPECT.