HRP20151077T1 - Derivati pirazola - Google Patents

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HRP20151077T1
HRP20151077T1 HRP20151077TT HRP20151077T HRP20151077T1 HR P20151077 T1 HRP20151077 T1 HR P20151077T1 HR P20151077T T HRP20151077T T HR P20151077TT HR P20151077 T HRP20151077 T HR P20151077T HR P20151077 T1 HRP20151077 T1 HR P20151077T1
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phenyl
pyrazole
carboxamide
morpholin
disorders
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Guido Galley
Cédric GHELLAMALLAH
Roger Norcross
Philippe Pflieger
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F. Hoffmann - La Roche Ag
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Claims (16)

1. Spoj, naznačen time, da ima sljedeću formulu: [image] u kojoj R1 je vodik ili fenil, opcijski supstituiran sa sljedećima: halogen, CN ili C1-7-alkoksi, ili C1-7-alkoksi supstituiran s halogenom; R2 je vodik ili C1-7-alkil; R3 je vodik ili C1-7-alkil, ili je fenil opcijski supstituiran s jednim ili više supstituenata, odabranih od sljedećih: halogen, cijano ili C1-7-alkoksi supstituiran s halogenom, ili je piridinil, opcijski supstituiran s halogenom ili C1-7-alkilom supstituiranim s halogenom, ili je pirimidinil, opcijski supstituiran s C1-7-alkilom supstituiranim s halogenom, ili je pirazinil, opcijski supstituiran sa sljedećima: halogen, cijano ili C1-7-alkil supstituiran s halogenom; R4 je vodik, C1-7-alkil ili fenil; Z je veza, -CH2- ili -O-; ili njegova farmaceutski prikladna kiselinska adicijska sol.
2. Spoj, naznačen time, da ima formulu IA-1 prema zahtjevu 1: [image] u kojoj R je vodik, halogen, CN ili C1-7-alkoksi ili C1-7-alkoksi supstituiran s halogenom; R2 je vodik ili C1-7-alkil; R3 je vodik ili C1-7-alkil; Z je veza, -CH2- ili -O-; n je 1 ili 2; ako n = 2, tada svaki R može biti određen neovisno jedan od drugoga; ili njegova farmaceutski prikladna kiselinska adicijska sol.
3. Spoj formule IA-1 prema bilo kojem od zahtjeva 1 ili 2, naznačen time, da su spojevi sljedeći: (S)-N-(4-(morfolin-2-il)fenil)-5-fenil-1H-pirazol-3-karboksamid; (S)-1-metil-N-(4-(morfolin-2-il)fenil)-5-fenil-1H-pirazol-3-karboksamid; (S)-5-(3-cijanofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-5-(3-cijanofenil)-4-metil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-5-(5-cijano-2-fluorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-5-(3-cijano-4-fluorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; ili (S)-5-(3-(difluorometoksi)fenil)-1-etil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid.
4. Spoj, naznačen time, da ima formulu IB-1 prema zahtjevu 1: [image] u kojoj R je vodik, halogen, CN ili C1-7-alkoksi ili C1-7-alkoksi supstituiran s halogenom; R2 je vodik ili C1-7-alkil; R4 je vodik ili C1-7-alkil; Z je veza, -CH2- ili -O-; n je 1 ili 2; ako n = 2, tada svaki R može biti određen neovisno jedan od drugoga; ili njegova farmaceutski prikladna kiselinska adicijska sol.
5. Spoj formule IB-1 prema bilo kojem od zahtjeva 1 ili 4, naznačen time, da su spojevi sljedeći: (S)-3-(3-klorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(4-fluorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-metoksifenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-1-metil-N-(4-(morfolin-2-il)fenil)-3-fenil-1H-pirazol-5-karboksamid; (S)-4-metil-N-(4-(morfolin-2-il)fenil)-3-fenil-1H-pirazol-5-karboksamid; (S)-3-(4-metoksifenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(2-fluorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(2-metoksifenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(2-klorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3,4-dimetoksifenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (R)-3-(4-klorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (R)-3-(2-klorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(4-klorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (R)-3-(3-klorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (R)-3-(3-metoksifenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-klorofenil)-1-metil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (R)-1-metil-N-(4-(morfolin-2-il)fenil)-3-fenil-1H-pirazol-5-karboksamid; (S)-3-(4-cijanofenil)-1-metil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(4-fluorofenil)-1-metil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-metoksifenil)-1-metil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-cijanofenil)-1-metil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-cijanofenil)-1-etil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(4-cijanofenil)-1-etil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-cijanofenil)-N-(4-(piperidin-3-il)fenil)-1H-pirazol-5-karboksamid; (R)-3-(3-cijanofenil)-N-(4-(piperidin-3-il)fenil)-1H-pirazol-5-karboksamid (rac)-3-(3-cijanofenil)-N-(4-(pirolidin-3-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-(difluorometoksi)fenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-(difluorometoksi)fenil)-1-etil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; (S)-3-(3-cijano-2-fluorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid; ili (S)-3-(3-(difluorometoksi)fenil)-1-metil-N-(4-(morfolin-2-il)fenil)-1H-pirazol-5-karboksamid.
6. Spoj, naznačen time, da ima formulu IA-2 prema zahtjevu 1: [image] u kojoj R1 je vodik; R2 je vodik ili C1-7-alkil; R3 je fenil opcijski supstituiran s jednim ili više supstituenata, odabranih od sljedećih: halogen, cijano ili C1-7-alkoksi supstituiran s halogenom, ili je piridinil, opcijski supstituiran s halogenom ili C1-7-alkilom supstituiranim s halogenom, ili je pirimidinil, opcijski supstituiran s C1-7-alkilom supstituiranim s halogenom, ili je pirazinil, opcijski supstituiran sa sljedećima: halogen, cijano ili C1-7-alkil supstituiran s halogenom; Z je veza, -CH2- ili -O-; ili njegova farmaceutski prikladna kiselinska adicijska sol.
7. Spoj formule IA-2 prema bilo kojem od zahtjeva 1 ili 6, naznačen time, da su spojevi sljedeći: (S)-1-(4-fluorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (R)-1-(4-fluorofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-1-(5-kloropiridin-2-il)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-N-(4-(morfolin-2-il)fenil)-1-(5-(trifluorometil)piridin-2-il)-1H-pirazol-3-karboksamid; (S)-1-(4-cijanofenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (R)-N-(4-(morfolin-2-il)fenil)-1-(5-(trifluorometil)piridin-2-il)-1H-pirazol-3-karboksamid; (S)-1-(4-(difluorometoksi)fenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (R)-1-(4-(difluorometoksi)fenil)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-N-(4-(morfolin-2-il)fenil)-1-(5-(trifluorometil)pirimidin-2-il)-1H-pirazol-3-karboksamid; (S)-1-(6-kloropirazin-2-il)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-1-(3-kloropirazin-2-il)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-1-(5-kloropirazin-2-il)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; (S)-N-(4-(morfolin-2-il)fenil)-1-(6-(trifluorometil)pirimidin-4-il)-1H-pirazol-3-karboksamid; (S)-N-(4-(morfolin-2-il)fenil)-1-(6-(trifluorometil)pirazin-2-il)-1H-pirazol-3-karboksamid; (S)-1-(5-cijanopirazin-2-il)-N-(4-(morfolin-2-il)fenil)-1H-pirazol-3-karboksamid; ili (S)-N-(4-(morfolin-2-il)fenil)-1-(2-(trifluorometil)pirimidin-4-il)-1H-pirazol-3-karboksamid.
8. Spoj, naznačen time, da ima formulu IB-2 prema zahtjevu 1: [image] u kojoj R1 je vodik; R2 je vodik ili C1-7-alkil; R4 je vodik, C1-7-alkil ili fenil; Z je veza, -CH2- ili -O-; ili njegova farmaceutski prikladna kiselinska adicijska sol.
9. Spoj prema bilo kojem od zahtjeva 1 ili 8, naznačen time, da spoj je sljedeći: (S)-N-(4-(morfolin-2-il)fenil)-1-fenil-1H-pirazol-5-karboksamid.
10. Postupak za proizvodnju spoja formule IA ili IB, kako je određeno prema bilo kojem od zahtjeva 1 do 9, naznačen time, da postupak obuhvaća sljedeće: a) rascjepljivanje N-zaštitne skupine od spojeva sljedećih formula: [image] na spoj sljedećih formula: [image] pri čemu PG je N-zaštitna skupina odabrana od -C(O)O-tert-butila, a ostale definicije su prema opisu u zahtjevu 1, te ako je potrebno, pretvaranje dobivenih spojeva u farmaceutski prikladne kiselinske adicijske soli.
11. Spoj prema bilo kojem od zahtjeva 1 do 9, naznačen time, da se proizvodi postupkom prema zahtjevu 10.
12. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 9, i farmaceutski prikladan nosač i/ili pomoćno sredstvo.
13. Farmaceutski sastav koji obuhvaća spoj prema bilo kojem od zahtjeva 1 do 9, te farmaceutski prikladan nosač i/ili pomoćno sredstvo, naznačen time, da se upotrebljava u liječenju depresije, anksioznih poremećaja, bipolarnog poremećaja, poremećaja s pomanjkanjem pažnje i hiperaktivnosti (ADHD), poremećaja povezanih sa stresom, psihotičkih poremećaja, shizofrenije, neuroloških bolesti, Parkinsonove bolesti, neurodegenerativnih poremećaja, Alzheimerove bolesti, epilepsije, migrene, hipertenzije, zlouporabe droga, metaboličkih poremećaja, poremećaja hranjenja, dijabetesa, dijabetskih komplikacija, pretilosti, dislipidemije, poremećaja potrošnje i izjednačavanja energije, poremećaja i zastoja homeostaze tjelesne temperature, poremećaja spavanja i cirkadijanog ritma, te kardiovaskularnih poremećaja.
14. Spojevi prema bilo kojem od zahtjeva 1 do 9, naznačeni time, da se upotrebljavaju kao terapeutski djelotvorne tvari.
15. Spojevi prema bilo kojem od zahtjeva 1 do 9, naznačeni time, da se upotrebljavaju kao terapeutski djelotvorne tvari za liječenje depresije, anksioznih poremećaja, bipolarnog poremećaja, poremećaja s pomanjkanjem pažnje i hiperaktivnosti (ADHD), poremećaja povezanih sa stresom, psihotičkih poremećaja, shizofrenije, neuroloških bolesti, Parkinsonove bolesti, neurodegenerativnih poremećaja, Alzheimerove bolesti, epilepsije, migrene, hipertenzije, zlouporabe droga, metaboličkih poremećaja, poremećaja hranjenja, dijabetesa, dijabetskih komplikacija, pretilosti, dislipidemije, poremećaja potrošnje i izjednačavanja energije, poremećaja i zastoja homeostaze tjelesne temperature, poremećaja spavanja i cirkadijanog ritma, te kardiovaskularnih poremećaja.
16. Uporaba spoja prema bilo kojem od zahtjeva 1 do 9, naznačena time, da je za proizvodnju lijekova za terapeutsko i/ili profilaktičko liječenje depresije, anksioznih poremećaja, bipolarnog poremećaja, poremećaja s pomanjkanjem pažnje i hiperaktivnosti (ADHD), poremećaja povezanih sa stresom, psihotičkih poremećaja, shizofrenije, neuroloških bolesti, Parkinsonove bolesti, neurodegenerativnih poremećaja, Alzheimerove bolesti, epilepsije, migrene, hipertenzije, zlouporabe droga, metaboličkih poremećaja, poremećaja hranjenja, dijabetesa, dijabetskih komplikacija, pretilosti, dislipidemije, poremećaja potrošnje i izjednačavanja energije, poremećaja i zastoja homeostaze tjelesne temperature, poremećaja spavanja i cirkadijanog ritma, te kardiovaskularnih poremećaja.
HRP20151077TT 2011-06-09 2015-10-12 Derivati pirazola HRP20151077T1 (hr)

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CY1116778T1 (el) 2017-03-15
CN103596567A (zh) 2014-02-19
US9073911B2 (en) 2015-07-07
NZ617350A (en) 2016-01-29
HK1191862A1 (zh) 2014-08-08
TW201302727A (zh) 2013-01-16
EP2717873B1 (en) 2015-07-15
IL229549B (en) 2019-06-30
JP2014516066A (ja) 2014-07-07
RS54183B1 (en) 2015-12-31
IL229549A0 (en) 2014-01-30
BR112013031324B1 (pt) 2021-11-03
KR101574905B1 (ko) 2015-12-04
AR088741A1 (es) 2014-07-02
KR20140029517A (ko) 2014-03-10
DK2717873T3 (en) 2015-07-27
CN103596567B (zh) 2016-03-16
CL2013003484A1 (es) 2014-08-08
WO2012168260A1 (en) 2012-12-13
JP5914642B2 (ja) 2016-05-11
ZA201308939B (en) 2014-08-27
TWI440636B (zh) 2014-06-11
PL2717873T3 (pl) 2015-12-31
PE20140934A1 (es) 2014-08-06
ES2546438T3 (es) 2015-09-23
MX2013013853A (es) 2014-01-20
BR112013031324A2 (pt) 2016-11-29
EA024648B1 (ru) 2016-10-31
SG195156A1 (en) 2013-12-30
MY162160A (en) 2017-05-31
CA2837255A1 (en) 2012-12-13
US20120316172A1 (en) 2012-12-13
AU2012266457A1 (en) 2013-11-14
SI2717873T1 (sl) 2015-09-30
MA35192B1 (fr) 2014-06-02
PT2717873E (pt) 2015-09-18
EA201391787A1 (ru) 2014-04-30
UA110525C2 (ru) 2016-01-12
CO6801764A2 (es) 2013-11-29
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