Arthur A Santilli

US Patent:

6369056, Apr 9, 2002

Filed:

Apr 19, 2000

Appl. No.:

09/552356

Inventors:

Puwen Zhang - Audubon PA
Arthur A. Santilli - Havertown PA
Andrew Fensome - Wayne PA
Eugene A. Terefenko - Quakertown PA
Andrew Q. Viet - Upper Darby PA
Jay E. Wrobel - Lawrenceville NJ
James P. Edwards - San Diego CA
Todd K. Jones - Solana Beach CA
Christopher M. Tegley - Thousands Oaks CA
Lin Zhi - San Diego CA

Assignee:

American Home Products Corporation - Madison NJ
Ligand Pharmaceuticals, Inc. - San Diego CA

International Classification:

A61K 31535

US Classification:

5142305, 544 70, 544 71, 544 92

Abstract:

This invention provides compounds of the formula: wherein: A, B and D are N or CH, with the proviso that A, B and D can not all be CH; R and R are independent substituents selected from H, COR , NR COR , or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or groups; or R and R are fused to form an optionally substituted 3 to 8 membered spirocyclic or heterocyclic ring; R is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R is H, C to C alkyl, or substituted C to C alkyl; R is H, OH, NH , or optionally substituted alkyl, or alkenyl, or COR ; R is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R is a substituted benzene ring or a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO or NR ; R is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R is H, alkyl, or substituted alkyl; R is H or alkyl; Q is O, S, NR , or CR R ; R is CN, SO CF , or optionally substituted alkyl, cycloalkyl, aryl, or heterocyclic ring; R and R are H, NO , CN CO R , or optionally substituted alkyl, cycloalkyl, aryl, or heterocyclic; R is C to C alkyl; or CR R form a six membered ring of the structure below: W is O or a chemical bond; or a pharmaceutically acceptable salt thereof, as well as their use and pharmaceutical compositions as agonists and antagonists of the progesterone receptor.

US Patent:

6380178, Apr 30, 2002

Filed:

Apr 19, 2000

Appl. No.:

09/552545

Inventors:

Gary S. Grubb - Newtown Square PA
Arthur A. Santilli - Havertown PA
Andrew Q. Viet - Upper Darby PA
Puwen Zhang - Audubon PA
Andrew Fensome - Wayne PA
Jay E. Wrobel - Lawrenceville NJ
James P. Edwards - San Diego CA
Todd K. Jones - Solana Beach CA
Christopher M. Tegley - Thousand Oaks CA
Lin Zhi - San Diego CA

Assignee:

American Home Products Corporation - Madison NJ
Ligand Pharmaceuticals, Inc. - San Diego CA

International Classification:

A61K 3156

US Classification:

514171, 5142305, 514321, 514414

Abstract:

This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: where A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C to C alkyl group; R and R are independent substituents selected from the group of H, C to C alkyl, substituted C to C alkyl, C to C alkenyl, substituted C to C alkenyl, C to C alkynyl, substituted C to C alkynyl, C to C cycloalkyl, substituted C to C cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, COR , or NR COR ; or R and R are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. These methods of treatment may be used for contraception.

US Patent:

6380185, Apr 30, 2002

Filed:

Feb 25, 2000

Appl. No.:

09/513807

Inventors:

Marci C. Koko - Wayne PA
John W. Ullrich - Schwenksville PA
Arthur A. Santilli - Havertown PA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

A61K 3155

US Classification:

51421708, 5142352, 514323, 514414, 514415, 540602, 544144, 546201, 548456, 548491

Abstract:

The present invention provides compounds of the formula: wherein R , R , R , R , X, n Y and Z, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical formulations and methods of treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.

US Patent:

6441019, Aug 27, 2002

Filed:

Jul 17, 2001

Appl. No.:

09/906875

Inventors:

Arthur A. Santilli - Havertown PA
Andrew Q. Viet - Upper Darby PA
Puwen Zhang - Audubon PA
Andrew Fensome - Wayne PA
Jay E. Wrobel - Lawrenceville NJ
James P. Edwards - San Diego CA
Todd K. Jones - Solana Beach CA
Christopher M. Tegley - Thousand Oaks CA
Lin Zhi - San Diego CA

Assignee:

Wyeth - Madison NJ
Ligand Pharmaceuticals, Inc. - San Diego CA

International Classification:

A61K 31535

US Classification:

514409, 548411, 548453, 514421

Abstract:

This invention provides compounds of the formula: wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C to C alkyl group; R and R are independent substituents selected from the group of H, C to C alkyl, substituted C to C alkyl, C to C alkenyl, substituted C to C alkenyl, C to C alkynyl, substituted C to C alkynyl, C to C cycloalkyl, substituted C to C cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, COR , or NR COR ; or R and R are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. The compounds of this invention are useful as agonists and antagonists of the progesterone receptor and in methods of inducing contraception and in the treatment or prevention of benign or malignant neoplastic diseases.

US Patent:

6787538, Sep 7, 2004

Filed:

Jul 10, 2003

Appl. No.:

10/617096

Inventors:

Chris P. Miller - Strafford PA
Michael D. Collini - Clifton Heights PA
Bach D. Tran - Baltimore MD
Arthur A. Santilli - Havertown PA

Assignee:

Wyeth - Madison NJ

International Classification:

A61P 530

US Classification:

51421707, 514323, 514414, 514415

Abstract:

The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in providing hormone replacement therapy.

US Patent:

6835729, Dec 28, 2004

Filed:

Nov 24, 2003

Appl. No.:

10/720504

Inventors:

Chris P. Miller - Strafford PA
Michael D. Collini - Clifton Heights PA
Bach D. Tran - Baltimore MD
Arthur A. Santilli - Havertown PA

Assignee:

Wyeth - Madison NJ

International Classification:

A61P 306

US Classification:

51421707, 514323, 514414, 514415

Abstract:

The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in lowering cholesterol levels.

US Patent:

6924281, Aug 2, 2005

Filed:

Aug 11, 2004

Appl. No.:

10/916118

Inventors:

Chris P. Miller - Strafford PA, US
Michael D. Collini - Clifton Heights PA, US
Bach D. Tran - Baltimore MD, US
Arthur A. Santilli - Havertown PA, US

Assignee:

Wyeth - Madison NJ

International Classification:

A61P005/24

US Classification:

51421707, 514323, 514414, 514415

Abstract:

The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating male pattern baldness.

US Patent:

6951852, Oct 4, 2005

Filed:

Oct 24, 2003

Appl. No.:

10/692777

Inventors:

Chris P. Miller - Strafford PA, US
Michael D. Collini - Clifton Heights PA, US
Bach D. Tran - Baltimore MD, US
Arthur A. Santilli - Havertown PA, US

Assignee:

Wyeth - Madison NJ

International Classification:

A61P019/00
A61P019/02

US Classification:

51421707, 514323, 514414, 514415

Abstract:

The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in the treatment or inhibition of osteoarthritis.