Lendon Norwood Pridgen

US Patent:

6355813, Mar 12, 2002

Filed:

Jun 29, 2000

Appl. No.:

09/607173

Inventors:

William Morrow Clark - Philadelphia PA
Ivan Lantos - Wayne PA
Robert John Mills - Norristown PA
Lendon Norwood Pridgen - Collegeville PA
Ann Marie Tickner - Norristown PA

Assignee:

SmithKline Beecham Corporation - Philadelphia PA

International Classification:

C07D31770

US Classification:

549432, 568630, 568648, 568649, 568656

Abstract:

Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentanopyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S, 2R, 3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

US Patent:

6441173, Aug 27, 2002

Filed:

Jul 27, 2000

Appl. No.:

09/626999

Inventors:

Jeffery L. Wood - Blue Bell PA
Michael Anthony McGuire - West Norriton PA
Robert John Mills - Norristown PA
Lendon Norwood Pridgen - Collegeville PA
Marvin Sungwhan Yu - Audubon PA
Qiaogong Su - Norristown PA

Assignee:

SmithKline Beecham Corporation - Philadelphia PA

International Classification:

C07D22122

US Classification:

546 26, 546183, 5462837

Abstract:

This invention relates to an improved process for preparing (+) (1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof, preferably the ethylene diamine 2:1 salt. This invention relates to novel intermediates useful in preparing (+) (1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid. This invention relates to an improved process for preparing (+) (1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof, preferably the disodium salt. This invention relates to novel intermediates useful in preparing (+) (1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid.

US Patent:

50083902, Apr 16, 1991

Filed:

Nov 3, 1988

Appl. No.:

7/266728

Inventors:

Paul E. Bender - Cherry Hill NJ
Ivan Lantos - Blackwood NJ
Michael A. McGuire - Norristown PA
Lendon N. Pridgen - Audubon PA
Herbert B. Winicov - Blue Bell PA

Assignee:

SmithKline Beckman Corporation - Philadelphia PA

International Classification:

C07D51304

US Classification:

546199

Abstract:

6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.

US Patent:

61145491, Sep 5, 2000

Filed:

May 8, 1998

Appl. No.:

8/776803

Inventors:

Jeffery L. Wood - Blue Bell PA
Michael Anthnoy McGuire - West Norriton PA
Robert John Mills - Norristown PA
Lendon Norwood Pridgen - Collegeville PA
Marvin Sungwhan Yu - Audubon PA
Qiaogong Su - Norristown PA

Assignee:

SmithKline Beecham Corporation - Philadelphia PA

International Classification:

C07D31770

US Classification:

549432

Abstract:

Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentano[b]pyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)4-methoxyphenyl]-1-(3,4-methylenedioxypheny l)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S, 2R, 3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(p rop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

US Patent:

6143907, Nov 7, 2000

Filed:

Feb 4, 1997

Appl. No.:

8/776804

Inventors:

William Morrow Clark - Philadelphia PA
Ivan Lantos - Wayne PA
Robert John Mills - Norristown PA
Lendon Norwood Pridgen - Collegeville PA
Ann Marie Tickner - Norristown PA

Assignee:

SmithKline Beecham Corporation - Philadelphia PA

International Classification:

C07D31744
C07D22102

US Classification:

549445

Abstract:

Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentanopyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylen edioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyph eyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

US Patent:

44776632, Oct 16, 1984

Filed:

Apr 7, 1982

Appl. No.:

6/366443

Inventors:

Bing L. Lam - King of Prussia PA
Lendon N. Pridgen - Audubon PA

Assignee:

SmithKline Beckman Corporation - Philadelphia PA

International Classification:

C07D40106

US Classification:

544310

Abstract:

A series of chemical reactions starting from the condensation of uracil with an acid stable heterocyclic aldehyde in an acid medium produces biologically active end products which are 2-heterocyclylmethylthioethylamino-5-heterocyclylmethyl-4-pyrimidinones. The new reactions and intermediates of this invention are particularly useful for preparing 2[2-(5-dimethylaminomethyl-2-furylmethylthio)-ethylamino]-5-(6-methyl-3-py ridylmethyl)-4-pyrimidinone and its salts. This compound is a potent H. sub. 2 -antagonist with a long duration of activity.

US Patent:

48032794, Feb 7, 1989

Filed:

Apr 28, 1986

Appl. No.:

6/856246

Inventors:

Paul E. Bender - Cherry Hill NJ
Ivan Lantos - Blackwood NJ
Michael A. McGuire - Norristown PA
Lendon N. Pridgen - Audubon PA
Herbert B. Winicov - Blue Bell PA

Assignee:

SmithKline Beckman Corporation - Philadelphia PA

International Classification:

C07D51304

US Classification:

546271

Abstract:

6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.

US Patent:

46200010, Oct 28, 1986

Filed:

Sep 11, 1984

Appl. No.:

6/649394

Inventors:

Bing L. Lam - King of Prussia PA
Lendon N. Pridgen - Audubon PA

Assignee:

SmithKline Beckman Corporation - Philadelphia PA

International Classification:

C07D40106

US Classification:

544310

Abstract:

A series of chemical reactions starting from the condensation of uracil with an acid stable heterocyclic aldehyde in an acid medium produces biologically active end products which are 2-heterocyclylmethylthioethylamino-5-heterocyclylmethyl-4-pyrimidinones. The new reactions and intermediates of this invention are particularly useful for preparing 2[2-(5-dimethylaminomethyl-2-furylmethylthio)-ethylamino]-5-(6-methyl-3-py ridylmethyl)-4-pyrimidinone and its salts. This compound is a potent H. sub. 2 -antagonist with a long duration of activity.