Mark R Collins

US Patent:

6339098, Jan 15, 2002

Filed:

Apr 19, 2000

Appl. No.:

09/552630

Inventors:

Mark A. Collins - Norristown PA
Valerie A. Mackner - Conshohocken 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 31428

US Classification:

514373, 548207

Abstract:

This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein R , and R are each, independently, hydrogen, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, heteroarylalkyl, and alkynyl. R and R may be taken together to form a ring and together contain âCH (CH ) CH â, âCH CH CMe CH CH â, âO(CH ) CH â, O(CH ) Oâ, âCH CH OCH CH â, âCH CH NR CH CH â. R and R may be taken together to form a double bond, the double bond having two methyl groups bonded to the terminal end, having a cycloalkyl group bonded to the terminal end, having an oxygen bonded to the terminal end, or having a cycloether bonded to the terminal end; or a double bond. R is hydrogen, hydroxyl, NH , alkyl, substituted alkyl, alkenyl, alkynyl, substituted or, COR. R is hydrogen, halogen, âCN, âNH , alkyl, substituted alkyl, alkoxy, alkoxy, aminoalkyl, or substituted aminoalkyl; R is a trisubstituted phenyl ring having the structure, or is a five or six membered heteroaryl ring, containing 1, 2, or 3 heteroatoms selected from the group consisting of O, S, SO, SO and NR , or pharmaceutically acceptable salt thereof.

US Patent:

6407101, Jun 18, 2002

Filed:

Apr 19, 2000

Appl. No.:

09/552544

Inventors:

Mark A. Collins - Norristown PA
Valerie A. Mackner - Conshohocken PA
Jay E. Wrobel - Lawrenceville NJ
Lin Zhi - San Diego CA
Todd K. Jones - Solana Beach CA
James P. Edwards - San Diego CA
Christopher M. Tegley - Thousand Oaks CA

Assignee:

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

International Classification:

C07D41310

US Classification:

5142305, 544 92

Abstract:

This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein T is O, S, or absent; R , and R are each, independently, hydrogen, alkyl, substituted alkyl; or R and R are taken together form a ring and together contain âCH (CH ) CH â, âCH CH CMe CH CH â, âO(CH ) CH â, âO(CH ) Oâ, âCH CH OCH CH â, or âCH CH NR CH CH â; n=1-5; p=1-4; q=1-4; R is hydrogen, OH, NH , alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or COR ; R is hydrogen, alkyl, substituted alky, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R is hydrogen, halogen, CN, NH , alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R is hydrogen, allyl, or substituted alkyl; R is hydrogen, alkyl, substituted alkyl, or COR ; R is hydrogen, alkyl, substituted alkyl, alko, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.

US Patent:

6436929, Aug 20, 2002

Filed:

Apr 19, 2000

Appl. No.:

09/552354

Inventors:

Puwen Zhang - Audubon PA
Andrew Fensome - Wayne PA
Eugene A. Terefenko - Quakertown PA
Lin Zhi - San Diego CA
Todd K. Jones - Solana Beach CA
James P. Edwards - San Diego CA
Christopher M. Tegley - Thousand Oaks CA
Jay E. Wrobel - Lawrenceville NJ
Mark A. Collins - Norristown PA

Assignee:

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

International Classification:

A61K 31535

US Classification:

5142305, 544 70, 544 92

Abstract:

The present invention provides compounds which are agonists of the progesterone receptor and have the structures: wherein R and R are independent substituents selected from the group of H, optionally substituted C to C alkyl, alkenyl, alkynyl, or alkynyl groups C to C cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or COR or NR COR ; or R and R are fused to form an optionally substituted 3 to 8 membered Spiro cyclic alkyl or alkenyl ring or a Spiro cyclic ring containing one to three heteroatoms selected from O, S and N; R is selected from H, amino, or optionally substituted C to C alkyl, aryl, C to C alkoxy, or C to C aminoalkyl groups; R is H, C to C alkyl, or substituted C to C alkyl; R is H, OH, NH , COR , or optionally substituted C to C alkyl, C to C alkenyl, or alkynyl groups; R is selected from H or optionally substituted C to C alkyl, aryl, C to C alkoxy, or C to C aminoalkyl groups; Q is S, NR , or CR R ; R is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring with 1, 2, or 3 ring heteroatoms selected from the group of O, S, SO, SO or NR ; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds for contraception and the treatment of progesterone-related maladies.

US Patent:

6562857, May 13, 2003

Filed:

Jan 9, 2002

Appl. No.:

10/043513

Inventors:

Mark A. Collins - Norristown PA
Valerie A. Mackner - Conshohocken PA
Jay E. Wrobel - Lawrenceville NJ
Lin Zhi - San Diego CA
Todd K. Jones - Solana Beach CA
James P. Edwards - San Diego CA
Christopher M. Tegley - Thousand Oaks CA

Assignee:

Wyeth - Madison NJ

International Classification:

C07D40310

US Classification:

514414, 514409, 514278, 546 17, 548408, 548409, 548411, 548412, 548452, 548465, 548518, 548484, 548486

Abstract:

This invention provides a progesterone receptor agonist of formula 1 having the structure wherein T is O, S, or absent; R , and R are each, independently, hydrogen, alkyl, substituted alkyl; or R and R are taken together form a ring and together contain âCH (CH ) CH â, âCH CH CMe CH CH â, âO(CH ) CH â, âO(CH ) Oâ, âCH CH OCH CH â, or âCH CH NR CH CH â; n=1-5; p=1-4; q=1-4; R is hydrogen, OH, NH , alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or COR ; R is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R is hydrogen, halogen, CN, NH , alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R is hydrogen, alkyl, or substituted alkyl; R is hydrogen, alkyl, substituted alkyl, or COR , R is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.

US Patent:

6982261, Jan 3, 2006

Filed:

Jan 15, 2003

Appl. No.:

10/342719

Inventors:

Mark A. Collins - Norristown PA, US
Valerie A. Mackner - Conshohocken PA, US
Jay E. Wrobel - Lawrenceville NJ, US
Lin Zhi - San Diego CA, US
Todd K. Jones - Solana Beach CA, US
James P. Edwards - San Diego CA, US
Christopher M. Tegley - Thousand Oaks CA, US

Assignee:

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

International Classification:

A61K 31/54
A01K 31/535
C07D 279/16
C07D 498/00

US Classification:

5142242, 5142305, 544 50, 544 92

Abstract:

This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein T is O, S, or absent; R, and Rare each, independently, hydrogen, alkyl, substituted alkyl; or Rand Rare taken together form a ring and together contain —CH(CH)CH—, —CHCHCMeCHCH—, —O(CH)CH—, —O(CH)O—, —CHCHOCHCH—, or —CHCHNRCHCH—;.

US Patent:

7081457, Jul 25, 2006

Filed:

May 6, 2002

Appl. No.:

10/140034

Inventors:

Puwen Zhang - Audubon PA, US
Andrew Fensome - Wayne PA, US
Eugene A. Terefenko - Quakertown PA, US
Lin Zhi - San Diego CA, US
Todd K. Jones - Solana Beach CA, US
James P. Edwards - San Diego CA, US
Christopher M. Tegley - Thousand Oaks CA, US
Jay E. Wrobel - Lawrenceville NJ, US
Mark A. Collins - Norristown PA, US

Assignee:

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

International Classification:

A61K 31/535
C07D 295/00
C07D 265/12

US Classification:

5142305, 544 70, 544 92

Abstract:

Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure:.

US Patent:

7569564, Aug 4, 2009

Filed:

Feb 9, 2006

Appl. No.:

11/351002

Inventors:

Puwen Zhang - Audubon PA, US
Andrew Fensome - Wayne PA, US
Eugene A. Terefenko - Quakertown PA, US
Lin Zhi - San Diego CA, US
Todd K. Jones - Solana Beach CA, US
James P. Edwards - San Diego CA, US
Christopher M. Tegley - Thousand Oaks CA, US
Jay E. Wrobel - Lawrenceville NJ, US
Mark A. Collins - Norristown PA, US

Assignee:

Wyeth - Madison NJ

International Classification:

A61K 31/536
C07D 265/12

US Classification:

5142305, 544 90, 544 92

Abstract:

Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure:.

US Patent:

7846924, Dec 7, 2010

Filed:

Jul 19, 2005

Appl. No.:

11/184313

Inventors:

Mark A. Collins - Norristown PA, US
Valerie A. Mackner - Conshohocken PA, US
Jay E. Wrobel - Lawrenceville NJ, US
Lin Zhi - San Diego CA, US
Todd K. Jones - Solana Beach CA, US
Christopher M. Tegley - Thousand Oaks CA, US
James P. Edwards - San Diego CA, US

Assignee:

Wyeth LLC - Madison NJ

International Classification:

A61K 31/54

US Classification:

5142265

Abstract:

This invention provides a progesterone receptor antagonist of formula 1 having the structure.