HRP20131183T1 - Fenilalkilpiperazini s aktivnošä†u modulatora tnf - Google Patents

Fenilalkilpiperazini s aktivnošä†u modulatora tnf Download PDF

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HRP20131183T1
HRP20131183T1 HRP20131183AT HRP20131183T HRP20131183T1 HR P20131183 T1 HRP20131183 T1 HR P20131183T1 HR P20131183A T HRP20131183A T HR P20131183AT HR P20131183 T HRP20131183 T HR P20131183T HR P20131183 T1 HRP20131183 T1 HR P20131183T1
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Croatia
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compound
ethyl
pentylphenyl
methyl
piperazine
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HRP20131183AT
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Marco Baroni
Olaf Ritzeler
Marco Zanchet
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Sanofi
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Priority claimed from FR0803337A external-priority patent/FR2932480B1/fr
Priority claimed from FR0807361A external-priority patent/FR2940288B1/fr
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Publication of HRP20131183T1 publication Critical patent/HRP20131183T1/hr

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Claims (15)

1. Spoj formule (I): [image] , naznačen time što: – R1 i R2, međusobno neovisno, predstavljaju atom vodika, atom halogena, (C1-C5) alkilnu skupinu, (C1-C5) halogenalkilnu skupinu, (C1-C2)perfluoralkilnu skupinu, (C1-C5) alkoksi skupinu ili (C1-C2)perfluoralkoksi skupinu; – R3 predstavlja (C1-C5) alkilnu skupini; – A predstavlja =CH- ili =N-; u obliku baze ili adicijske soli s kiselinom.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što – R1 predstavlja (C1-C5) halogenalkilnu skupinu ili (C1-C2) perfluoralkilnu skupinu; u obliku baze ili adicijske soli s kiselinom.
3. Spoj u skladu s patentnim zahtjevom 2, naznačen time što – R1 predstavlja (C1-C5) fluoralkilnu skupinu; u obliku baze ili adicijske soli s kiselinom.
4. Spoj u skladu s patentnim zahtjevom 1, 2 ili 3, naznačena time što: – R2 predstavlja atom vodika ili (C1-C5) alkilnu skupinu; u obliku baze ili adicijske soli s kiselinom.
5. Spoj u skladu s patentnim zahtjevom 1, 2, 3 ili 4, naznačen time što je piperazin vezan preko etilne skupine na položaju 3 u fenilnoj skupini: [image] , u obliku baze ili adicijske soli s kiselinom.
6. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što – R1 predstavlja (C1-C2) perfluoralkilnu skupinu; u obliku baze ili adicijske soli s kiselinom.
7. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što – R2 predstavlja atom vodika ili (C1-C3) alkilnu skupinu; u obliku baze ili adicijske soli s kiselinom.
8. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je: 1-[2-(4-metil-3-pentilfenil)etil]-4-(3-trifluormetilfenil)piperazin; u obliku baze ili adicijske soli s kiselinom.
9. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što ga se bira između: – spoja 1: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hemipamoat; – spoja 1 bis: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hemipamoat, u obliku smjese s 0,5 mol slobodne pamoinske kiseline; – spoja 2: 1-(3-trifluormetilfenil)-4-[2-(4-metoksi-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 3: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-propilfenil)etil]piperazin-hidroklorid; – spoja 4: 1-(3-fluorfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 5: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-heptilfenil)etil]piperazin-hidroklorid; – spoja 6: 1-(6-trifluormetilpirid-2-il)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 7: 1-(3-fluorfenil)-4-[2-(4-metoksi-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 8: 1-(3-difluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 9: 1-(fenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 10: 1-(3-metoksifenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 11: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-(2-metilbutil)fenil)etil]piperazin-hidroklorid; – spoja 12: 1-(3-difluormetilfenil)-4-[2-(4-metoksi-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 13: 1-(3-trifluormetilfenil)-4-[2-(4-metoksi-3-heptilfenil)etil]piperazin-hidroklorid; – spoja 14: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-heksilfenil)etil]piperazin-hidroklorid; – spoja 15: 1-(3-trifluormetilfenil)-4-[2-(4-metoksi-3-propilfenil)etil]piperazin-hidroklorid; – spoja 16: 1-(fenil)-4-[2-(4-metoksi-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 17: 1-(4-klorfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 18: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 19: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-benzensulfonat; – spoja 20: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-2-naftalensulfonat; – spoja 21: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-p-tolilsulfonat; – spoja 22: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hemi-2,5-naftalendisulfonat; – spoja 23: 1-(4-fluorfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-dihidroklorid; – spoja 24: 1-(4-metoksifenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin (baza); – spoja 25: 1-(5-brompirid-2-il)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-dihidroklorid; – spoja 26: 1-[2-(4-metil-3-pentilfenil)etil]-4-(5-trifluormetilpirid-2-il)piperazin-dihidroklorid; – spoja 27: 1-(4-tert-butilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 28: 1-(4-etoksifenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-dihidroklorid; – spoja 29: 1-[2-(4-metil-3-pentilfenil)etil]-4-m-tolilpiperazin-dihidroklorid; – spoja 30: 1-[2-(4-metil-3-pentilfenil)etil]-4-pirid-2-ilpiperazin-dihidroklorid; – spoja 31: 1-(6-brompirid-2-il)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 32: 1-(2-klorfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 33: 1-(2-metilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 34: 1-(3-trifluormetoksilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 35: 1-(5-klorpirid-2-il)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-hidroklorid; – spoja 36: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-oksalat; – spoja 37: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-fumarat; – spoja 38: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-sukcinat; – spoja 39: 1-(3-trifluormetilfenil)-4-[2-(4-metil-3-pentilfenil)etil]piperazin-dihipurat.
10. Postupak dobivanja spoja u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što se sastoji u koraku kondenziranja spoja formule (II): [image] , gdje su R1 i A definirani kao u patentnom zahtjevu 1, sa spojem formule (III): [image] , gdje su R2 i R3 definirani kao u patentnom zahtjevu 1, a Q predstavlja izlaznu skupinu, uz izborno njegovo prevođenje u njegovu sol.
11. Farmaceutski pripravak, naznačen time što kao djelatnu tvar sadrži spoj formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 9, ili njegovu farmaceutski prihvatljivu sol.
12. Medikament, naznačen time što kao djelatnu tvar sadrži spoj formule (I) u skladu s patentnim zahtjevima 1 do 9, ili njegovu farmaceutski prihvatljivu sol.
13. Upotreba spoja formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 9, ili njegove farmaceutski prihvatljive soli, naznačena time što je spoj namijenjen pripravi medikamenta za liječenje ili sprječavanje boli i/ili bolesti povezanih s imunosnim i upalnim poremećajima.
14. Upotreba spoja formule (I), ili njegove farmaceutski prihvatljive soli, u skladu s patentnim zahtjevom 13, naznačena time što je spoj namijenjen pripravi medikamenta za liječenje boli ili upala u zglobovima.
15. Upotreba spoja formule (I), ili njegove farmaceutski prihvatljive soli, u skladu s patentnim zahtjevom 14, naznačena time što se medikament injicira u zglobove.
HRP20131183AT 2008-06-16 2013-12-12 Fenilalkilpiperazini s aktivnošä†u modulatora tnf HRP20131183T1 (hr)

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