James J Zapf

US Patent:

7196108, Mar 27, 2007

Filed:

Mar 6, 2003

Appl. No.:

10/384391

Inventors:

Magnus Pfahl - Solana Beach CA, US
Catherine Tachdjian - San Diego CA, US
Hussien A. Al-Shamma - Encinitas CA, US
Andrea Fanjul Giachino - San Diego CA, US
Karine Jakubowicz-Jaillardon - Villebon sur Yvette, FR
Jianhua Guo - San Diego CA, US
Richard M. Fine - Ridgewood NJ, US
Lyle W. Spruce - Chula Vista CA, US
James W. Zapf - San Diego CA, US

Assignee:

Incyte San Diego Inc. - Wilmington DE
Ortho McNeil Pharmaceutical Inc. - Rariton NJ

International Classification:

A61K 31/343
A61K 31/381
A61K 31/382
A61K 31/403
A61K 31/4166
A61K 31/427
A61K 31/4353
A61K 31/538
A61K 31/5415
C07D 277/34
C07D 265/36
C07D 243/10
C07D 241/36
C07D 233/72
C07D 223/14
C07D 221/02
C07D 209/04
C07D 335/04
C07D 333/50
C07D 319/14
C07D 311/04
C07D 307/77

US Classification:

514366, 540544, 540553, 540582, 544 2, 544 63, 544 89, 546112, 546113, 548200, 5483111, 548452, 549 32, 549377, 549396, 549462, 51421105, 51421207, 5142305, 5142521, 514300, 514387, 514412, 514453

Abstract:

The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.

US Patent:

20030105333, Jun 5, 2003

Filed:

Mar 8, 2002

Appl. No.:

10/098184

Inventors:

Magnus Pfahl - Solana Beach CA, US
Catherine Tachdjian - San Diego CA, US
Hussien Al-Shamma - Encinitas CA, US
Andrea Fanjul - San Diego CA, US
David Pleynet - San Diego CA, US
Lyle Spruce - Chula Vista CA, US
Richard Fine - Ridgewood NJ, US
James Zapf - San Diego CA, US
Jianhua Guo - San Diego CA, US

International Classification:

C07K014/705
C07D271/06
C07D277/62
C07D271/10

US Classification:

548/131000, 548/143000, 548/252000, 530/350000

Abstract:

Disclosed are molecules that activate an RXR receptor, wherein the molecule comprises an RXR binding portion which binds the RXR receptor and comprises a side pocket contacting residue which contacts a side-pocket 1 of an RXR receptor.

US Patent:

20030216432, Nov 20, 2003

Filed:

Mar 6, 2003

Appl. No.:

10/384352

Inventors:

Magnus Pfahl - Solana Beach CA, US
Catherine Tachdjian - San Diego CA, US
Hussien Al-Shamma - Encinitas CA, US
Andrea Giachino - San Diego CA, US
Karine Jakubowicz-Jaillardon - Villebon sur Yvette, FR
Jianhua Guo - San Diego CA, US
James Zapf - San Diego CA, US

International Classification:

A61K031/4709
A61K031/427
C07D417/02

US Classification:

514/314000, 514/365000, 546/165000, 548/181000

Abstract:

The present invention relates to certain substituted heterocycles of Formula (200), wherein B, H, I, J and K together with the Arform a ring containing at least one amide residue, and W, X, Y and Z together form a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases such as type 2 diabetes, and related disorders of lipid and carbohydrate metabolism, including atherosclerosis. The compounds are also useful for treating diseases of uncontrolled proliferation, such as cancers in general, including breast cancer.

US Patent:

20040097566, May 20, 2004

Filed:

Dec 6, 2002

Appl. No.:

10/313341

Inventors:

Magnus Pfahl - Solana Beach CA, US
Hussien Al-Shamma - Encinitas CA, US
Andrea Giachino - San Diego CA, US
David Pleynet - San Diego CA, US
Haifeng Bao - San Diego CA, US
Lyle Spruce - Chula Vista CA, US
Christopher Cow - San Diego CA, US
Catherine Tachdjian - San Diego CA, US
James Zapf - San Diego CA, US
Torsten Wiemann - Encinitas CA, US

International Classification:

A61K031/426
A61K031/421
C07D277/32
C07D263/18
C07D413/02
C07D417/02

US Classification:

514/369000, 514/376000, 548/182000, 548/225000

Abstract:

The present invention relates to certain substituted heterocycles, including 2-substituted thiazolidinone and 2-substituted oxazolidinone compounds. These compounds are useful in the treatment of diseases related to uncontrolled cellular proliferation, such as cancer or precancerous conditions. The compounds are also useful for modulating lipid and/or carbohydrate metabolism, and treating Type II diabetes, hyperglycemia or obesity, and for treating inflammatory diseases such as arthritis. Some disclosed embodiments of the invention relate to compounds having the structures indicated below, or a pharmaceutically acceptable salt thereof.

US Patent:

20050014767, Jan 20, 2005

Filed:

Jan 29, 2004

Appl. No.:

10/769725

Inventors:

Magnus Pfahl - Solana Beach CA, US
Catherine Tachdjian - San Diego CA, US
Torsten Wiemann - Encinitas CA, US
Christopher Cow - San Diego CA, US
Lyle Spruce - Chula Vista CA, US
Andrea Giachino - San Diego CA, US
Allan Kaspar - San Diego CA, US
James Zapf - San Diego CA, US

International Classification:

A61K031/497
A61K031/4439
A61K031/423
A61K031/4184

US Classification:

514255050, 514337000, 514338000, 514375000, 514394000, 544405000, 546272700, 548215000, 548304700

Abstract:

The invention relates to certain compounds whose structures are shown below, and their pharmaceutically acceptable salts and prodrugs, and pharmaceutical compositions thereof, which are useful for treating treating diseases of uncontrolled cellular proliferation, including cancer. wherein:

US Patent:

20050038098, Feb 17, 2005

Filed:

Apr 19, 2004

Appl. No.:

10/827111

Inventors:

Catherine Tachdjian - San Diego CA, US
Jianhua Guo - San Diego CA, US
Mohamed Boudjelal - San Diego CA, US
Hussien Al-Shamma - Encinitas CA, US
Andrea Giachino - San Diego CA, US
Karine Jakubowicz-Jaillardon - Villebon sur Yvette, FR
Qing Chen - San Diego CA, US
James Zapf - San Diego CA, US
Magnus Pfahl - Solana Beach CA, US

International Classification:

C07D049/02
C07D045/02
A61K031/416
A61K031/4025
A61K031/381
A61K031/353

US Classification:

514406000, 514422000, 514444000, 514456000, 548364400, 548525000, 549060000, 549403000

Abstract:

The invention relates to novel heterocyclic compounds having the structure illustrated by Formula (I) wherein the Arradicals are substituted dihydronapthalene or isochroman radicals, the Arradicals are aryl or heteroaryl radicals; and HAr is a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one radical. The compounds of Formula (I) can have biological activity for advantageously regulating carbohydrate metabolism, including serum glucose level, and lipid metabolism, and can be useful for the treatment of hyperlipidemia and/or hypercholesterolemia, and Type II diabetes. The compounds of Formula (I) can also have utility in the treatment of diseases of uncontrolled proliferation, including cancer.

US Patent:

20050209286, Sep 22, 2005

Filed:

Mar 1, 2005

Appl. No.:

11/069930

Inventors:

Magnus Pfahl - Solana Beach CA, US
Catherine Tachdjian - San Diego CA, US
Hussien Al-Shamma - Encinitas CA, US
Andrea Fanjul - San Diego CA, US
David Pleynet - San Diego CA, US
Lyle Spruce - Chula Vista CA, US
Richard Fine - Ridgewood NJ, US
James Zapf - San Diego CA, US
Jianhua Guo - San Diego CA, US

International Classification:

A61K031/4439
A61K031/4245
G06F019/00
G01N033/48
G01N033/50
C07D285/14

US Classification:

514341000, 514364000, 546269100, 548134000, 702019000

Abstract:

Disclosed are molecules that activate an RXR receptor, wherein the molecule comprises an RXR binding portion which binds the RXR receptor and comprises a side pocket contacting residue which contacts a side-pocket 1 of an RXR receptor.

US Patent:

20050222186, Oct 6, 2005

Filed:

Jun 7, 2003

Appl. No.:

10/517594

Inventors:

Monika Baudler - Konstanz, DE
Shripad Bhagwat - San Diego CA, US
Paul Erdman - San Diego CA, US
Florian Gantner - Osaka, JP
Moorthy Palanki - Encinitas CA, US
Christian Schudt - Konstanz, DE
Josef Stadlwieser - Konstanz, DE
James Zapf - San Diego CA, US

Assignee:

Altana Pharma AG - Konstanz

International Classification:

A61K031/506
C07D043/14
C07D413/14
C07D417/14

US Classification:

514275000, 544296000, 544324000

Abstract:

The invention relates to substituted diaminopyrimidine compounds, which are effective therapeutic compounds for treating diseases and disorders associated with those commonly treated by Protein Kinase C theta (PKCθ) inhibitors.