Claims for Patent: 7,501,513

Summary for Patent: 7,501,513

Title:	Immunosuppressive effects of pteridine derivatives
Abstract:	This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro-derivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.
Inventor(s):	Waer; Mark Jozef Albert (Heverlee, BE), Herdewijn; Piet Andre Maurits Maria (Rotselaar/Wezemaal, BE), Pfleiderer; Wolfgang Eugen (Constance, DE), Marchand; Arnaud Didier Marie (Heverlee, BE), De Jonghe; Steven Cesar Alfons (Brussels, BE)
Assignee:	4 AZA Bioscience NV (Leuven, BE)
Application Number:	10/595,126
Patent Claims:	1. A pteridine derivative selected from the group consisting of: 2-amino-4-morpholino-6-(4-acetanilide)pteridine, 2-amino-4-morpholino-6-(3-acetanilide)pteridine, 2-amino-4-morpholino-6-(4-aminophenyl)pteridine, 2-amino-4-morpholino-6-(3-aminophenyl)pteridine, 2-amino-4-morpholino-6-(4-benzoylaminophenyl)pteridine, 2-amino-4-morpholino-6-(4-phenoxyacetylaminophenyl)pteridine, 2-amino-4-morpholino-6-(4-propionylaminophenyl)pteridine, 2-amino-4-morpholino-6-(4-furoylaminophenyl)pteridine, 2-amino-4-morpholino-6-(4-cyclohexanoylaminophenyl)pteridine, 2-amino-4-morpholino-6-[4-(4-chlorobenzoyl)aminophenyl]pteridine, 2-amino-4-morpholino-6-(4-benzyloxyacetylaminophenyl)pteridine, 2-amino-4-morpholino-6-(4-isonicotinoylaminophenyl)pteridine; 2-amino-4-morpholino-6-(4-naphtoylaminophenyl)pteridine; 2-amino-4-morpholino-6-(4-methylsulfonylaminophenyl)pteridine; 2-amino-4-morpholino-6-(4-ethylsuccinylaminophenyl)pteridine; 2-amino-4-morpholino-6-[4-(4-methylbenzoate)aminophenyl)pteridine; 2-amino-4-morpholino-6-(3-benzoylaminophenyl)pteridine; 2-amino-4-morpholino-6-(3-benzensulfonylaminophenyl)pteridine, 2-amino-4-morpholino-6-(3-phenoxyacetylaminophenyl)pteridine; 2-amino-4-morpholino-6-(3-isonicotinoylaminophenyl)pteridine; 2-amino-4-morpholino-6-(3-cyclohexanoylaminophenyl)pteridine; 2-amino-4-morpholino-6-[3-(4-methylbenzoate)aminophenyl]pteridine; 2-amino-4-morpholino-6-(3-ethylsuccinylaminophenyl)pteridine; 2-amino-4-morpholino-6-(3-ethylmalonylaminophenyl)pteridine; 2-amino-4-morpholino-6-(3-benzyloxyacetylaminophenyl)pteridine, 2-amino-4-morpholino-6-(3-ethylsulfonylaminophenyl)pteridine, 2-amino-4-morpholino-6-[3-Boc-(L)-phenylalanine-aminophenyl]pteridine; 2-amino-4-morpholino-6-[3-Boc-(D)-phenylalanine-aminophenyl]pteridine; 2-amino-4-morpholino-6-[3-Boc-(L)-tryptophane-aminophenyl]pteridine; 2-amino-4-morpholino-6-[3-Boc-(D)-tryptophane-aminophenyl]pteridine, 2-amino-4-morpholino-6-(4-hydroxyphenyl)pteridine, 2,4-di-(thienyl-2-methylarnino)-6-(3,4-dimethoxy-phenyl)pteridine, 2-amino-4-morpholino-6-(4-benzyloxyphenyl)pteridine, 2-amino-4-morpholino-6-(4-(phenethyloxy)-phenyl)pteridine, 2-amino-4-morpholino-6-(4-phenoxy-butyronitrile)pteridine, 2-amino-4-morpholino-6-(4-propoxy-phenyl)pteridine, 2-amino-4-morpholino-6-(4-phenoxy-butyric acid ethyl ester)pteridine, 2-amino-4-morpholino-6-(4-phenoxy-acetic acid ethyl ester)pteridine, 2-amino-4-morpholino-6-(4-(2-methoxyethoxy)-phenyl)pteridine, 2-amino-4-morpholino-6-(4-butoxy-phenyl)-pteridine, 2-amino-4-(diethanolamino)-6-[[3,4-(dimethoxyphenyl)]pteridine, 2-amino-4-(benzylamino)-6-[[3,4-(dimethoxyphenyl)]pteridine; 2-amino-4-(phenylethylamino)-6-[[3,4-(dimethoxyphenyl)]pteridine, 2-amino-4-(2-thienylmethylamino)-6-[[3,4-(dimethoxyphenyl)]pteridine, 2-amino-4-thiomorpholine-6-[[3,4-(dimethoxyphenyl)]pteridine. 2. A pharmaceutical composition comprising as an active principle at least one pteridine derivative according to claim 1. 3. A pharmaceutical composition comprising as an active principle at least one pteridine derivative according to claim 1, and further comprising one or more biologically active drugs selected from the group consisting of immuno-suppressant and/or immunomodulator drugs. 4. A pharmaceutical composition comprising as an active principle at least one pteridine derivative according to claim 1, and further comprising one or more immunosuppressant drugs selected from the group consisting of cyclosporin A; pentoxyfylline; daltroban, sirolimus, tacrolimus; rapamycin; leflunomide; mycophenolic acid and salts thereof; azathioprine, brequinar; gusperimus; 6-mercaptopurine; mizoribine; chloroquine; hydroxy-chloroquine; etanercept; infliximab; and kineret. 5. A pharmaceutical composition comprising as an active principle at least onepteridine derivative according to claim 1 and further comprising one or more immunomodulator drugs selected from the group consisting of acemannan, amiprilose, bucillamine, ditiocarb sodium, imiquimod, Inosine Pranobex, interferon-.beta., interferon-.gamma., lentinan, levamisole, pidotimod, romurtide, platonin, procodazole, propagermanium, thymomodulin, thymopentin and ubenimex. 6. A pharmaceutical composition comprising as an active principle at least one pteridine derivative according to claim 1 and further comprising one or more pharmaceutically acceptable carriers or excipients.

Details for Patent 7,501,513

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Janssen Biotech, Inc.	REMICADE	infliximab	For Injection	103772	08/24/1998		2024-04-22
Immunex Corporation	ENBREL	etanercept	For Injection	103795	11/02/1998		2024-04-22
Immunex Corporation	ENBREL	etanercept	For Injection	103795	05/27/1999		2024-04-22
Immunex Corporation	ENBREL	etanercept	Injection	103795	09/27/2004		2024-04-22
Immunex Corporation	ENBREL	etanercept	Injection	103795	02/01/2007		2024-04-22
Immunex Corporation	ENBREL MINI	etanercept	Injection	103795	09/14/2017		2024-04-22
Immunex Corporation	ENBREL	etanercept	Injection	103795			2024-04-22