HRP20120187T1 - Derivati 2-oksoalkil-1-piperazin-2-ona, njihovo dobivanje i njihova upotreba u terapiji - Google Patents
Derivati 2-oksoalkil-1-piperazin-2-ona, njihovo dobivanje i njihova upotreba u terapiji Download PDFInfo
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- HRP20120187T1 HRP20120187T1 HR20120187T HRP20120187T HRP20120187T1 HR P20120187 T1 HRP20120187 T1 HR P20120187T1 HR 20120187 T HR20120187 T HR 20120187T HR P20120187 T HRP20120187 T HR P20120187T HR P20120187 T1 HRP20120187 T1 HR P20120187T1
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Abstract
Spoj formule (I): naznačen time što:- m je 0 ili 1;- A je: a B je atom vodikailiA je atom vodika, a B je: ;- R1 i R2, koji mogu biti isti ili različiti, su neovisno atom vodika ili halogena, C1-C4 alkilna, C1-C4 fluoralkilna, C1-C2 perfluoralkilna ili C1-C4 alkoksi skupina ili trifluormetoksi skupina;- n je 1 ili 2;- R3 je skupina formule: gdje se R4 i R5, koji mogu biti isti ili različiti, nalaze na bilo kojem od dostupnih položaja i neovisno su atom vodika ili halogena, hidroksilna, C1-C4 alkilna, C1-C4 fluoralkilna, C1-C2 perfluoralkilna, C1-C4 alkoksi skupina, trifluormetoksi skupina, cijano skupina, COOH, COOalkilna, CONH2, CONR6R7 ili NHCOR skupina,- R, R6 i R7 su C1-C6 alkil; u obliku baza ili adicijskih soli s kiselinama. Patent sadrži još 14 patentnih zahtjeva.
Claims (15)
1. Spoj formule (I):
[image]
naznačen time što:
– m je 0 ili 1;
– A je:
[image]
a B je atom vodika
ili
A je atom vodika, a B je:
[image]
;
– R1 i R2, koji mogu biti isti ili različiti, su neovisno atom vodika ili halogena, C1-C4 alkilna, C1-C4 fluoralkilna, C1-C2 perfluoralkilna ili C1-C4 alkoksi skupina ili trifluormetoksi skupina;
– n je 1 ili 2;
– R3 je skupina formule:
[image]
gdje se R4 i R5, koji mogu biti isti ili različiti, nalaze na bilo kojem od dostupnih položaja i neovisno su atom vodika ili halogena, hidroksilna, C1-C4 alkilna, C1-C4 fluoralkilna, C1-C2 perfluoralkilna, C1-C4 alkoksi skupina, trifluormetoksi skupina, cijano skupina, COOH, COOalkilna, CONH2, CONR6R7 ili NHCOR skupina,
– R, R6 i R7 su C1-C6 alkil;
u obliku baza ili adicijskih soli s kiselinama.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što se R4 i R5, koji mogu biti isti ili različiti, nalaze na bilo kojem od dostupnih položaja i neovisno su CONH2, CONR6R7 ili NHCOR; u obliku baza ili adicijskih soli s kiselinama.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što:
– m je 1;
– A je:
[image]
a B je atom vodika;
– R1 i R2, koji mogu biti isti ili različiti, su neovisno atom vodika ili halogena, C1-C4 alkilna, C1-C4 fluoralkilna, C1-C2 perfluoralkilna ili C1-C4 alkoksi skupina ili trifluormetoksi skupina;
– n je 1 ili 2;
– R3 je skupina formule:
[image]
gdje se R4 i R5, koji mogu biti isti ili različiti, nalaze na bilo kojem od dostupnih položaja i neovisno su atom vodika ili halogena, hidroksilna, C1-C4 alkilna, C1-C4 fluoralkilna, C1-C2 perfluoralkilna ili C1-C4 alkoksi skupina, trifluormetoksi skupina, cijano skupina, ili COOH ili COOalkilna skupina;
u obliku baza ili adicijskih soli s kiselinama.
4. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što R1 nije H; u obliku baza ili adicijskih soli s kiselinama.
5. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je R1 na položaju -2-, -3- ili -4- i atom je klora ili radikal CF3, a R2 je vodik ili 3- ili 4-Cl; u obliku baza ili adicijskih soli s kiselinama.
6. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što R3 je 2-piridinil ili 2-pirimidinil, od kojih je svaki supstituiran s R4 i R5, kao što je definirano u patentnom zahtjevu 1; u obliku baza ili adicijskih soli s kiselinama.
7. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što n = 1; u obliku baza ili adicijskih soli s kiselinama.
8. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva 1 i 3 do 7, naznačen time što
R1 je 3-CF3;
R2 je 4-klor;
R3 je 2-piridilni ostatak, supstituiran na položaju 5 s CF3; i
n = 1;
u obliku baze ili adicijskih soli s kiselinama.
9. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što ga se bira između:
Spoja br. 1: 4-{2-[4-(4-klor-3-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 2: 4-{2-[4-(4-klor-3-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-metilpiridin-2-il)piperazin-2-ona;
Spoja br. 3: 4-{2-[4-(4-klorfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 4: 4-{2-okso-2-[4-(3-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]etil}-1-piridin-2-ilpiperazin-2-ona;
Spoja br. 5: 4-{2-[4-(4-klor-3-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-piridin-2-ilpiperazin-2-ona;
Spoja br. 6: 4-{2-[4-(4-klorfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-piridin-2-ilpiperazin-2-ona;
Spoja br. 7: 4-{2-[4-(2,3-diklorfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 8: 4-{2-[4-(4-klorfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(6-klorpiridin-2-il)piperazin-2-ona;
Spoja br. 9: 4-{2-[4-(3-klorfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 10: 4-{2-[4-(4-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 11: 4-{2-[4-(3-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 12: 4-{2-[4-(4-klor-3-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-piridin-3-ilpiperazin-2-ona;
Spoja br. 13: 1-(6-klorpiridin-3-il)-4-{2-[4-(4-klor-3-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}piperazin-2-ona;
Spoja br. 14: 4-{2-okso-2-[5-(3-trifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]etil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 15: 4-{2-okso-2-[4-(3-trifluormetoksilfenil)-3,6-dihidro-2H-piridin-1-il]etil}-1-piridin-2-ilpiperazin-2-ona;
Spoja br. 16: 4-{2-[4-(4-klor-3-trifluormetilfenil)-2,5-dihidropirol-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 17: 4-{2-[4-(3,5-bistrifluormetilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 18: 4-{2-[4-(3-metilfenil)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 19: 4-{2-[4-fenil-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluormetilpiridin-2-il) piperazin-2-ona;
Spoja br. 20: 4-{2-okso-2-[5-(2,3-diklorfenil)-3,6-dihidro-2H-piridin-1-il]etil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
Spoja br. 21: 4-{2-okso-2-[5-(3-metoksifenil)-3,6-dihidro-2H-piridin-1-il]etil}-1-(5-trifluormetilpiridin-2-il)piperazin-2-ona;
u obliku baza ili adicijskih soli s kiselinama.
10. Postupak dobivanja spoja formule (I), u skladu s bilo kojim od prethodnih patentnih zahtjeva, gdje su A, B, m, n, R3 definirani kao gore, naznačen time što uključuje korak reakcije spoja formule (IV)
[image]
gdje su A, B, m i n definirani kao u općoj formuli (I), a Hal je atom halogena, sa spojem opće formule (V):
[image]
gdje je R3 definiran kao u općoj formuli (I), u prisutnosti baze.
11. Spoj formule (IV)
[image]
naznačen time što su A, B, m i n definirani u skladu s bilo kojim od patentnih zahtjeva 1 do 9, a Hal je atom halogena;
s izuzetkom 2-klor-1-[4-(2-metoksifenil)-3,6-dihidro-2H-piridin-1-il]etanon i 2-klor-1-[4-(4-bromfenil)-3,6-dihidro-2H-piridin-1-il]etanona;
u obliku baze ili adicijskih soli s kiselinama.
12. Medikament, naznačen time što sadrži spoj formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 9, ili adicijsku sol tog spoja s farmaceutski prihvatljivom kiselinom.
13. Farmaceutski pripravak, naznačen time što sadrži spoj formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 9, ili njegovu farmaceutski prihvatljivu sol, a također i najmanje jednu farmaceutski prihvatljivu pomoćnu tvar.
14. Spoj opće formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što je namijenjen pripravi medikamenta namijenjenog upotrebi u sprječavanju ili liječenju neurodegenerativnih bolesti središnjeg i perifernog živčanog sustava, staračke demencije, epilepsije, Alzheimerove bolesti, Parkinsonove bolesti, Huntingtonove koreje, Downovog sindroma, prionskih bolesti, amnezije, shizofrenije, depresije, bipolarnog poremećaja, amiotrofne lateralne skleroze, multiple skleroze, kardiovaskularnih stanja, postishemijske oštećenja srca, kardiomiopatija, infarkta miokarda, insuficijencije srca, ishemije srca, cerebralnog infarkta; perifernih neuropatija, oštećenja vidnog živca i mrežnice, pigmentne degeneracije mrežnice, glaukoma, ishemije mrežnice, degeneracije makule, ozljeda leđne moždine, ozljeda lubanje, ateroskleroze, stenoza, poremećaja ožiljavanja, alopecije, raka, tumoura, metastaza, leukemija, poremećaja dišnog sustava, plućne upale, alergije, astme, kronične opstruktivne plućne bolesti, kutane, somatske, visceralne i neurološke boli, kronične neuropatske i upalne boli, autoimunih bolesti, reumatoidnog artritisa, ankilozantnog spondiloartritisa, psorijatičnog artritisa, pločaste psorijaze, lomova kostiju, bolesti kostiju i osteoporoze.
15. Spoj u skladu s patentnim zahtjevom 14, naznačen time što je sposoban inhibirati dimerizaciju p75NTR receptora, neovisno o njegovom ligandu.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0803298A FR2932481B1 (fr) | 2008-06-13 | 2008-06-13 | Derives de 4-{2-°4-phenyl-3,6-dihydro-2h-pyridin-1-yl!-2- oxo-alkyl}-1-piperazin-2-one, leur preparation et leur application en therapeutique. |
| PCT/FR2009/051117 WO2009150387A1 (fr) | 2008-06-13 | 2009-06-12 | Derives de 2-oxo-alkyl-1-piperazin-2-one, leur preparation et leur application en therapeutique |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120187T1 true HRP20120187T1 (hr) | 2012-03-31 |
Family
ID=40305319
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20120187T HRP20120187T1 (hr) | 2008-06-13 | 2009-06-12 | Derivati 2-oksoalkil-1-piperazin-2-ona, njihovo dobivanje i njihova upotreba u terapiji |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US8247404B2 (hr) |
| EP (1) | EP2310383B8 (hr) |
| JP (1) | JP5476372B2 (hr) |
| KR (1) | KR101601999B1 (hr) |
| CN (1) | CN102124001B (hr) |
| AR (1) | AR072102A1 (hr) |
| AT (1) | ATE535524T1 (hr) |
| AU (1) | AU2009259120B2 (hr) |
| BR (1) | BRPI0915482B8 (hr) |
| CA (1) | CA2726666C (hr) |
| CL (1) | CL2010001432A1 (hr) |
| CO (1) | CO6300943A2 (hr) |
| CY (1) | CY1112417T1 (hr) |
| DK (1) | DK2310383T3 (hr) |
| EA (1) | EA019924B1 (hr) |
| ES (1) | ES2378380T3 (hr) |
| FR (1) | FR2932481B1 (hr) |
| HR (1) | HRP20120187T1 (hr) |
| IL (1) | IL209903A (hr) |
| JO (1) | JO2773B1 (hr) |
| MX (1) | MX2010013694A (hr) |
| MY (1) | MY151228A (hr) |
| NZ (1) | NZ589842A (hr) |
| PL (1) | PL2310383T3 (hr) |
| PT (1) | PT2310383E (hr) |
| RS (1) | RS52252B (hr) |
| SI (1) | SI2310383T1 (hr) |
| TW (1) | TWI400238B (hr) |
| UY (1) | UY31894A (hr) |
| WO (1) | WO2009150387A1 (hr) |
| ZA (1) | ZA201008791B (hr) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2932481B1 (fr) | 2008-06-13 | 2010-10-08 | Sanofi Aventis | Derives de 4-{2-°4-phenyl-3,6-dihydro-2h-pyridin-1-yl!-2- oxo-alkyl}-1-piperazin-2-one, leur preparation et leur application en therapeutique. |
| FR2932482B1 (fr) * | 2008-06-13 | 2010-10-08 | Sanofi Aventis | Nouveaux derives de (phenyl-3,6-dihydro-2h-pyridinyl)- (piperazinyl ponte)-1-alcanone et leur utilisation comme inhibiteurs de p75 |
| FR2953839A1 (fr) | 2009-12-14 | 2011-06-17 | Sanofi Aventis | Nouveaux derives d'(heterocycle-piperidine condensee)-(piperazinyl)-1alcanone ou d'(heterocycle-pyrrolidine condensee)-(piperazinyl)-1alcanone et leur utilisation comme inhibiteurs de p75 |
| FR2953836B1 (fr) | 2009-12-14 | 2012-03-16 | Sanofi Aventis | Nouveaux derives (heterocycle-tetrahydro-pyridine)-(piperazinyl)-1-alcanone et (heterocycle-dihydro-pyrrolidine)-(piperazinyl)-1-alcanone et leur utilisation comme inhibiteurs de p75 |
| EP2606894A1 (en) | 2011-12-20 | 2013-06-26 | Sanofi | Novel therapeutic use of p75 receptor antagonists |
| EP2950095B1 (en) | 2014-05-28 | 2018-08-29 | Technische Universität Dresden | Cell-based assay and screening methods for modulators of p75NTR signaling |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3236243A1 (de) * | 1982-09-30 | 1984-04-05 | Merck Patent Gmbh, 6100 Darmstadt | Schwefelhaltige indolderivate |
| FR2744448B1 (fr) * | 1996-02-02 | 1998-04-24 | Pf Medicament | Nouvelles piperidines derivees d'aryl piperazine, ainsi que leur procede de preparation, les compositions pharmaceutiques et leur utilisation comme medicaments |
| JP2003514508A (ja) * | 1997-07-01 | 2003-04-15 | ノボ ノルディスク アクティーゼルスカブ | グルカゴン拮抗剤／逆作用剤 |
| US6613942B1 (en) * | 1997-07-01 | 2003-09-02 | Novo Nordisk A/S | Glucagon antagonists/inverse agonists |
| AU4198400A (en) | 1999-04-06 | 2000-10-23 | Krenitsky Pharmaceuticals Inc. | Neurotrophic thio substituted pyrimidines |
| UA77526C2 (en) * | 2002-06-07 | 2006-12-15 | Sanofi Aventis | Substituted derivatives of 1-piperazineacylpiperidine, a method for the preparation thereof and their use in therapy |
| FR2862968B1 (fr) * | 2003-12-01 | 2006-08-04 | Sanofi Synthelabo | Derives de 4-[(arylmethyl)aminomethyl]piperidine, leur preparation et leur application en therapeutique |
| FR2862967B1 (fr) * | 2003-12-01 | 2006-08-04 | Sanofi Synthelabo | Derives de (4-phenylpiperazin-1-yl)acylpiperidine, leur preparation et leur application en therapeutique |
| FR2932481B1 (fr) | 2008-06-13 | 2010-10-08 | Sanofi Aventis | Derives de 4-{2-°4-phenyl-3,6-dihydro-2h-pyridin-1-yl!-2- oxo-alkyl}-1-piperazin-2-one, leur preparation et leur application en therapeutique. |
| FR2932482B1 (fr) * | 2008-06-13 | 2010-10-08 | Sanofi Aventis | Nouveaux derives de (phenyl-3,6-dihydro-2h-pyridinyl)- (piperazinyl ponte)-1-alcanone et leur utilisation comme inhibiteurs de p75 |
-
2008
- 2008-06-13 FR FR0803298A patent/FR2932481B1/fr not_active Expired - Fee Related
-
2009
- 2009-06-01 JO JO2009197A patent/JO2773B1/en active
- 2009-06-11 TW TW098119565A patent/TWI400238B/zh active
- 2009-06-11 AR ARP090102109A patent/AR072102A1/es active IP Right Grant
- 2009-06-12 MX MX2010013694A patent/MX2010013694A/es active IP Right Grant
- 2009-06-12 NZ NZ589842A patent/NZ589842A/xx not_active IP Right Cessation
- 2009-06-12 PL PL09761938T patent/PL2310383T3/pl unknown
- 2009-06-12 BR BRPI0915482A patent/BRPI0915482B8/pt active IP Right Grant
- 2009-06-12 RS RS20120082A patent/RS52252B/en unknown
- 2009-06-12 SI SI200930179T patent/SI2310383T1/sl unknown
- 2009-06-12 AT AT09761938T patent/ATE535524T1/de active
- 2009-06-12 KR KR1020117000793A patent/KR101601999B1/ko active Active
- 2009-06-12 EA EA201170015A patent/EA019924B1/ru not_active IP Right Cessation
- 2009-06-12 JP JP2011513037A patent/JP5476372B2/ja active Active
- 2009-06-12 MY MYPI20105853 patent/MY151228A/en unknown
- 2009-06-12 EP EP09761938A patent/EP2310383B8/fr active Active
- 2009-06-12 PT PT09761938T patent/PT2310383E/pt unknown
- 2009-06-12 WO PCT/FR2009/051117 patent/WO2009150387A1/fr active Application Filing
- 2009-06-12 UY UY0001031894A patent/UY31894A/es not_active Application Discontinuation
- 2009-06-12 ES ES09761938T patent/ES2378380T3/es active Active
- 2009-06-12 HR HR20120187T patent/HRP20120187T1/hr unknown
- 2009-06-12 CA CA2726666A patent/CA2726666C/fr active Active
- 2009-06-12 DK DK09761938.1T patent/DK2310383T3/da active
- 2009-06-12 CN CN200980131553.8A patent/CN102124001B/zh active Active
- 2009-06-12 AU AU2009259120A patent/AU2009259120B2/en active Active
-
2010
- 2010-12-07 ZA ZA2010/08791A patent/ZA201008791B/en unknown
- 2010-12-09 IL IL209903A patent/IL209903A/en active IP Right Grant
- 2010-12-13 US US12/966,408 patent/US8247404B2/en active Active
- 2010-12-13 CO CO10156026A patent/CO6300943A2/es active IP Right Grant
- 2010-12-13 CL CL2010001432A patent/CL2010001432A1/es unknown
-
2012
- 2012-02-29 CY CY20121100212T patent/CY1112417T1/el unknown
- 2012-07-24 US US13/556,328 patent/US20120289518A1/en not_active Abandoned
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