(12) Translation of european patent specification

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1 (12) Translation of european patent specification (11) NO/EP B1 (19) NO NORWAY (1) Int Cl. A61K 31/4196 (06.01) A61K 31/424 (06.01) A61P 21/00 (06.01) A61P 2/04 (06.01) C07D 249/08 (06.01) C07D 413/12 (06.01) Norwegian Industrial Property Office (21) Translation Published (80) Date of The European Patent Office Publication of the Granted Patent (86) European Application Nr (86) European Filing Date (87) The European Application s Publication Date (30) Priority.09.07, JP, 030 (84) Designated Contracting States: Designated Extension States: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR BA ME (73) Proprietor Astellas Pharma Inc., 3-11, Nihonbashi-Honcho 2-chome Chuo-ku, Tokyo , JP-Japan (72) Inventor KISO, Tetsuo, c/o Astellas Pharma Inc.3-11 Nihonbashi-Honcho 2-chomeChuo-ku, Tokyo , JP-Japan TSUKAMOTO, Mina, c/o Astellas Pharma Inc.3-11 Nihonbashi-Honcho 2- chomechuo-ku, Tokyo , JP-Japan (74) Agent or Attorney Tandbergs Patentkontor AS, Postboks 70 Vika, 0118 OSLO, Norge (4) Title TRIAZOLE DERIVATIVE FOR USE IN THE TREATMENT OF NEUROPATHIC PAIN AND FIBROMYALGIA (6) References Cited: WO-A1-03/0401 WO-A1-0/ WO-A1-06/03080 WO-A1-06/ WO-A1-07/ WO-A1-/ JP-A Captain David Williams: "Vicious Circle Theory of Chronic Fatigue Syndrome and Fibromyalgia",, July 1999 ( ), XP , Retrieved from the Internet: URL:http://www.newtreatments.org/fromweb/l icoriceprotocol.txt [retrieved on ] STAAB C.A. ET AL.: '11beta-Hydroxysteroid dehydrogenase type 1 is an important regulator at the interface of obesity and inflammation' JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY vol. 119, no. 1-2, February, pages 6-72, XP

2 Enclosed is a translation of the patent claims in Norwegian. Please note that as per the Norwegian Patents Acts, section 66i the patent will receive protection in Norway only as far as there is agreement between the translation and the language of the application/patent granted at the EPO. In matters concerning the validity of the patent, language of the application/patent granted at the EPO will be used as the basis for the decision. The patent documents published by the EPO are available through Espacenet (http://worldwide.espacenet.com) or via the search engine on our website here: https://search.patentstyret.no/ NO/EP

3 1 Patentkrav EP Forbindelse representert ved den følgende formel (I-b) eller et farmasøytisk akseptabelt salt derav for anvendelse ved behandling av smerte valgt fra nevropatisk smerte og fibromyalgi: karakterisert ved at: R 1b er aryl som kan være substituert; R 2b er C 1-6 alkyl; R 3b er C 1-6 alkyl; R 4b er C 1-6 alkyl eller cykloalkyl; og ring A b er aryl eller heteroaryl, som hver kan være substituert. 2. Forbindelse eller et salt derav for anvendelse i henhold til krav 1, som er en forbindelse representert ved følgende formel (Ic) eller et farmasøytisk akseptabelt salt derav: 2 hvori: R 1c er fenyl substituert med halogen; R 4c er metyl, etyl, isopropyl eller cyklopropyl; og ring A c er fenyl substituert med halogen, eller -C(O)NH Forbindelse eller et salt derav for anvendelse i henhold til krav 2, hvori ring A c er fenyl som er substituert med -C(O)NH 2 i 4-stillingen, og kan være ytterligere substituert med halogen.

4 2 4. Forbindelse eller et salt derav for anvendelse i henhold til krav 2, hvori ring A c er fenyl substituert med halogen.. Forbindelse eller et salt derav for anvendelse i henhold til krav 1, som er valgt fra følgende forbindelser og farmasøytisk akseptable salter derav: (2-brom-4-fluorfenyl)-4-metyl--[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]-4H- 1,2,4-3-(2-klor-4-fluorfenyl)-4-metyl--[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]-4H- 1,2,4-3-(2-klorfenyl)-4-metyl--[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]-4H-1,2,4-3-[1-(4-klor-2,6-difluorfenoksy)-1-metyletyl]--(2-klorfenyl)-4-metyl-4H-1,2,4-3-[1-(4-klor-2,6-difluorfenoksy)-1-metyletyl]--(2-klor-4-fluorfenyl)-4-metyl- 4H-1,2,4-3-(2-fluorfenyl)-4-metyl--[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]-4H-1,2,4-4-metyl-3-[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]--[3-(trifluormetyl)-1Hpyrazol-4-yl]-4H-1,2,4-4-{-1-(4-klor-2,6-difluorfenoksy)-1-metyletyl]-4-etyl-4H-1,2,4-triazol-3-4-{4-isopropyl--[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]-4H-1,2,4-triazol-3-4-{-[1-(4-klor-2,6-difluorfenoksy)-1-metyletyl]-4-metyl-4H-1,2,4-triazol-3-yl}- 3-fluorbenzamid, 4-{4-cyklopropyl--[1-(2,4-difluorfenoksy)-1-metyletyl]-4H-1,2,4-triazol-3-yl}- 3-fluorbenzamid, 3-fluor-4-{4-metyl--[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]-4H-1,2,4-triazol-3-4-{-[1-(4-klor-2,6-difluorfenoksy)-1-metyletyl]-4-isopropyl-4H-1,2,4-triazol-3-3-klor-4-{4-cyklopropyl--[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]-4H-1,2,4- triazol-3-yl}-benzamid, og 3-fluor-4-{4-isopropyl--[1-metyl-1-(2,4,6-trifluorfenoksy)etyl]-4H-1,2,4- triazol-3-yl}benzamid.

5 3 6. Forbindelse eller et salt derav for anvendelse i henhold til krav 1, som er 3-[1-(4- klor-2,6-difluorfenoksy)-1-metyletyl]--(2-klorfenyl)-4-metyl-4h-1,2,4-triazol eller et farmasøytisk akseptabelt salt derav. 7. Forbindelse eller et salt derav for anvendelse i henhold til krav 1, som er 4-{-[1-(4- klor-2,6-difluorfenoksy)-1-metyletyl]-4-metyl-4h-1,2,4-triazol-3-yl}-3-fluorbenzamid eller et farmasøytisk akseptabelt salt derav. 8. Forbindelse eller et salt derav for anvendelse i henhold til krav 1, som er 4-{4- cyklopropyl--[1-(2,4-difluorfenoksy)-1-metyletyl]-4h-1,2,4-triazol-3--yl}-3- fluorbenzamid, eller et farmasøytisk akseptabelt salt derav. 9. Forbindelse eller et salt derav for anvendelse i henhold til hvilket som helst av de foregående krav, hvori smerten er nevropatisk smerte.. Forbindelse eller et salt derav for anvendelse i henhold til hvilket som helst av kravene 1-8, hvori smerten er fibromyalgi. 11. Anvendelse av en forbindelse representert ved formel (Ib) ifølge krav 1, eller et farmasøytisk akseptabelt salt derav for fremstilling av et terapeutisk middel for behandling av smerte valgt fra nevropatisk smerte og fibromyalgi.

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