Title:
3-CYCLOPROPYLMETHOXY-4-DIFLUOROMETHOXY-N-(3,5-DICHLOROPYRID-4-YL)BENZAMIDE IN THE TREATMENT OF MULTIPLE SCLEROSIS
Document Type and Number:
WIPO Patent Application WO/2000/053182
Kind Code:
A2
Abstract:
The invention relates to the novel use of 3-cyclopropylmethoxy-4-difluoromethoxy-N-(3,5-dichloropyrid-4-yl)benzamide, a pharmacologically tolerable salt thereof or its N-oxide in the treatment of multiple sclerosis.
Inventors:
AMSCHLER HERMANN (DE)
HATZELMANN ARMIN (DE)
SCHUDT CHRISTIAN (DE)
KLEY HANS-PETER (DE)
SANDERS KARL (DE)
HATZELMANN ARMIN (DE)
SCHUDT CHRISTIAN (DE)
KLEY HANS-PETER (DE)
SANDERS KARL (DE)
Application Number:
PCT/EP2000/001703
Publication Date:
September 14, 2000
Filing Date:
March 01, 2000
Export Citation:
Assignee:
BYK GULDEN LOMBERG CHEM FAB (DE)
KLEY HANS PETER (DE)
SANDERS KARL (DE)
KLEY HANS PETER (DE)
SANDERS KARL (DE)
International Classes:
A61K31/44; A61K31/4412; A61P25/00; (IPC1-7): A61K31/44
Domestic Patent References:
| WO1994002465A1 | 1994-02-03 | |||
| WO1995001338A1 | 1995-01-12 | |||
| WO1995028926A1 | 1995-11-02 |
Other References:
NAVIKAS V ET AL: "The phosphodiesterase i.v. inhibitor rolipram in vitro reduces the numbers of MBP-reactive IFN-gamma and TNF-alpha mRNA expressing blood mononuclear cells in patients with multiple sclerosis." CLIN NEUROPHARMACOL, JUL-AUG 1998, 21 (4) P236-44, XP002113588 UNITED STATES
SOMMER N ET AL: "Therapeutic potential of phosphodiesterase type 4 inhibition in chronic autoimmune demyelinating disease." J NEUROIMMUNOL, OCT 1997, 79 (1) P54-61, XP002113589 NETHERLANDS
DINTER H ET AL: "Phosphodiesterase type IV inhibitors in the treatment of multiple sclerosis." J MOL MED, FEB 1997, 75 (2) P95-102, XP002113590 GERMANY
GENAIN CP ET AL: "Prevention of autoimmune demyelination in non-human primates by a cAMP-specific phosphodiesterase inhibitor." PROC NATL ACAD SCI U S A, APR 11 1995, 92 (8) P3601-5, XP002113591 UNITED STATES
SOMMER N ET AL: "Therapeutic potential of phosphodiesterase type 4 inhibition in chronic autoimmune demyelinating disease." J NEUROIMMUNOL, OCT 1997, 79 (1) P54-61, XP002113589 NETHERLANDS
DINTER H ET AL: "Phosphodiesterase type IV inhibitors in the treatment of multiple sclerosis." J MOL MED, FEB 1997, 75 (2) P95-102, XP002113590 GERMANY
GENAIN CP ET AL: "Prevention of autoimmune demyelination in non-human primates by a cAMP-specific phosphodiesterase inhibitor." PROC NATL ACAD SCI U S A, APR 11 1995, 92 (8) P3601-5, XP002113591 UNITED STATES
Attorney, Agent or Firm:
BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH (Konstanz, DE)
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Claims:
Patent claims
| 1. | The use of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloropyrid4yl) benzamide or a pharmaceutically acceptable salt thereof in the production of medicaments for the treatment of multiple sclerosis. |
| 2. | The use of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloroloxypyrid4yl) benzamide in the production of medicaments for the treatment of multiple sclerosis. |
| 3. | The use of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloropyrid4yl) benzamide or a pharmaceutically acceptable salt thereof for the treatment of multiple sclerosis. |
| 4. | The use of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloroloxypyrid4yl) benzamide for the treatment of multiple sclerosis. |
| 5. | The use of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloropyrid4yl) benzamide or a pharmaceutically acceptable salt thereof in the production of tablets, coated tablets or capsules having an active compound content of between 0.05 mg and 2 mg of 3cyclopropylmethoxy4difluoromethoxy N (3, 5dichloropyrid4yl) benzamide for the treatment of multiple sclerosis. |
| 6. | The use of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloro1oxypyrid4yl) benzamide in the production of tablets, coated tablets or capsules having an active compound content of between 0.05 mg and 2 mg of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloro1oxypyrid4yl) benz amide for the treatment of multiple sclerosis. |
| 7. | The use as claimed in claim 5 or 6, wherein the tablets, coated tablets or capsules have an ac tive compound content of between 0.1 and 1 mg. |
| 8. | The use of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloropyrid4yl) benzamide or a pharmaceutically acceptable salt thereof as claimed in one of claims 1,3 or 5, wherein the multiple sclerosis is the episodically proceeding form of multiple sclerosis. |
| 9. | The use of 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloro1oxypyrid4yl) benzamide as claimed in one of claims 2,4 or 6, wherein the multiple sclerosis is the episodically proceeding form of multiple sclerosis. |
| 10. | A commercially available product, consisting of a customary secondary pack, a primary pack containing the medicament and, if desired, a pack insert, the medicament leading to the attenuation of the symptoms of multiple sclerosis, the suitability of the medicament for the treatment of multiple scle rosis being indicated on the secondary pack and/or on the pack insert of the commercial available product, and the medicament containing 3cyclopropylmethoxy4difluoromethoxyN (3, 5dichloropyrid 4yt) benzamide, a pharmacologically tolerable salt thereof or its Noxide. |
Description:
INTERNATIONALSEARCHREPORT Inter.malApplicationNo PCT/EP00/01703 C.(Continuation) DOCUMENTSCONSIDEREDTOBERELEVANT CategoryCitationofdocument,withindication,whereappropriate,o
ftherelevantpassagesRelevanttoclaimNo. YWO9528926A(SCHERING1-10 AKTIENGESELLSCHAFT) 2November1995(1995-11-02) citedintheapplication thewholedocument YNAVIKASVETAL:"Thephosphodiesterase1-10 i.v.inhibitorrolipraminvitroreduces thenumbersofMBP-reactiveIFN-gammaand TNF-alphamRNAexpressingblood mononuclearcellsinpatientswith multiplesclerosis." CLINNEUROPHARMACOL,JUL-AUG1998,21(4) P236-44, XP002113588 UNITEDSTATES thewholedocument YSOMMERNETAL:"Therapeuticpotentialof1-10 phosphodiesterasetype4inhibitionin chronicautoimmunedemyelinatingdisease." JNEUROIMMUNOL,OCT1997,79(1)P54-61, XP002113589 NETHERLANDS thewholedocument YDINTERHETAL:"Phosphodiesterasetype1-10 IVinhibitorsinthetreatmentofmultiple sclerosis." JMOLMED,FEB1997,75(2)P95-102, XP002113590 GERMANY thewholedocument YGENAINCPETAL:"Preventionof1-10 autoimmunedemyelinationinnon-human primatesbyacAMP-specific phosphodiesteraseinhibitor." PROCNATLACADSCIUSA,APR111995,92 (8)P3601-5, XP002113591 UNITEDSTATES thewholedocument 1 INTERNATIONALSEARCHREPORT | Intel Jnal ApplicationNo InformationonpatentfamilymembersPCT/EP 00/01703 PatentdocumentPublication Patent family Publication citedinsearchreportdate member(s)date WO9402465A03-02-1994AU 4717693 A 14-02-1994 CA 2140441 A 03-02-1994 CZ 9500147 A 17-07-1996 EP 0652868 A 17-05-1995 FI 950375 A 27-01-1995 HU 72656 A 28-05-1996 HU 211979 B 29-01-1996 JP 8503925 T 30-04-1996 MX 9304571 A 31-05-1994 NO 950319 A 27-03-1995 NZ 254881 A 25-09-1996 PL 307265 A 15-05-1995 US 5935978 A 10-08-1999 US 5679696 A 21-10-1997 US 5698711 A 16-12-1997 ZA 9305448 A 19-05-1994 US 5840724 A 24-11-1998 WO9501338A12-01-1995AU 687087 B 19-02-1998 AU 7490794 A 24-01-1995 CA 2165192 A 12-01-1995 CN 1126468A,B 10-07-1996 CZ 9600001 A 12-06-1996 EP 0706513 A 17-04-1996 FI 956333 A 29-12-1995 HU 73232 A 29-07-1996 JP 8512041 T 17-12-1996 NO 955211 A 21-12-1995 NZ 271316 A 24-11-1997 PL 311820 A 18-03-1996 RU 2137754 C 20-09-1999 SK 161795 A 03-07-1996 US 5712298 A 27-01-1998 WO9528926A02-11-1995US 5672622 A 30-09-1997 AU 699085 B 19-11-1998 AU 2266295 A 16-11-1995 CA 2188269 A 02-11-1995 EP 0758233 A 19-02-1997 US 5847010 A 08-12-1998 US 6060501 A 09-05-2000