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HRP20100284T1 - Derivati piperazinila korisni u liječenju bolesti posredovanih receptorom gpr38 - Google Patents

Derivati piperazinila korisni u liječenju bolesti posredovanih receptorom gpr38 Download PDF

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HRP20100284T1
HRP20100284T1 HR20100284T HRP20100284T HRP20100284T1 HR P20100284 T1 HRP20100284 T1 HR P20100284T1 HR 20100284 T HR20100284 T HR 20100284T HR P20100284 T HRP20100284 T HR P20100284T HR P20100284 T1 HRP20100284 T1 HR P20100284T1
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methyl
phenyl
piperazinyl
pyridinecarboxamide
fluorophenyl
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HR20100284T
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Jason Mitchell Darren
Thomas Seal Jonathan
Thompson Mervyn
Marie Westaway Susan
Louisa Brown Samantha
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Glaxo Group Limited
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38476358&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20100284(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0612844A external-priority patent/GB0612844D0/en
Priority claimed from GB0711525A external-priority patent/GB0711525D0/en
Application filed by Glaxo Group Limited filed Critical Glaxo Group Limited
Publication of HRP20100284T1 publication Critical patent/HRP20100284T1/hr

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Abstract

Spoj formule (I) ili njegova sol: naznačen time štoA je fenil ili 6-člani heteroarilni prsten, po potrebi supstituiran s jednim supstituentom odabranim od halogena, C(1-4)alkil i C(1-4)alkoksi; R1 i R2 su nezavisno H ili C(1-4)alkil; R3 je po potrebi supstituirani fenil, 5 ili 6 člani heteroarilni prsten, ili 5 ili 6 člani heterociklički prsten; B je po potrebi supstituirani fenil, 6-člani heteroarilni prsten ili 6-člani heterociklički prsten povezan s amidnim ugljikom preko ugljikovog atoma; Y je veza, NH, N-C(1-4)alkil, O, C=O, ili CH2;R4 je vodik, C(1-4)alkil ili C(1-4)alkoksialkil; ikad su R3 ili B supstituirani, to mogu biti 1, 2 ili 3 supstituenta, svaki nezavisno odabran od halogena, C(1-4)alkil, C(1-4)alkoksi, C(3-7)cikloalkil, hidroksi, trifluormetoksi, trifluormetil, nitro, cijano, fenil, NH2, NHR5, NR5R6, NHCOR5, NHSO2R5, C(O)CF3, C(O)C(1-4)alkil, C(O)C(3-7)cikloalkil, C(O)OC(1-4)alkil, C(O)OC(3-7)cikloalkil, OC(O)C(1-4)alkil, OC(O)C(3-7)cikloalkil, CONH2, CONHR5, CONR5R6, SOR6, SO2CF3, SO2R6, OSO2R6, OSO2CF3, SO2NH2, SO2NHR5, SO2NR5R6, pritom R5 i R6 mogu biti jednaki ili različiti i predstavljaju C(1-4) alkil, fenil po potrebi supstituiran s halogenom ili 5 ili 6 člani heteroaril po potrebi supstituiran s halogenom. Patent sadrži još 15 patentnih zahtjeva.

Claims (16)

1. Spoj formule (I) ili njegova sol: [image] naznačen time što A je fenil ili 6-člani heteroarilni prsten, po potrebi supstituiran s jednim supstituentom odabranim od halogena, C(1-4)alkil i C(1-4)alkoksi; R1 i R2 su nezavisno H ili C(1-4)alkil; R3 je po potrebi supstituirani fenil, 5 ili 6 člani heteroarilni prsten, ili 5 ili 6 člani heterociklički prsten; B je po potrebi supstituirani fenil, 6-člani heteroarilni prsten ili 6-člani heterociklički prsten povezan s amidnim ugljikom preko ugljikovog atoma; Y je veza, NH, N-C(1-4)alkil, O, C=O, ili CH2; R4 je vodik, C(1-4)alkil ili C(1-4)alkoksialkil; i kad su R3 ili B supstituirani, to mogu biti 1, 2 ili 3 supstituenta, svaki nezavisno odabran od halogena, C(1-4)alkil, C(1-4)alkoksi, C(3-7)cikloalkil, hidroksi, trifluormetoksi, trifluormetil, nitro, cijano, fenil, NH2, NHR5, NR5R6, NHCOR5, NHSO2R5, C(O)CF3, C(O)C(1-4)alkil, C(O)C(3-7)cikloalkil, C(O)OC(1-4)alkil, C(O)OC(3-7)cikloalkil, OC(O)C(1-4)alkil, OC(O)C(3-7)cikloalkil, CONH2, CONHR5, CONR5R6, SOR6, SO2CF3, SO2R6, OSO2R6, OSO2CF3, SO2NH2, SO2NHR5, SO2NR5R6, pritom R5 i R6 mogu biti jednaki ili različiti i predstavljaju C(1-4) alkil, fenil po potrebi supstituiran s halogenom ili 5 ili 6 člani heteroaril po potrebi supstituiran s halogenom.
2. Spoj prema zahtjevu 1 ili njegova sol, naznačen time što: A je po potrebi supstituirani fenil ili piridil; i/ili R1 je vodik ili metil; i/ili R2 je vodik ili metil; i/ili R3 je po potrebi supstituirani fenil, morfolinil ili piperidinil, oksadiazolil, piridil, pirimidinil, imidazolil, pirolil; i/ili B je po potrebi supstituirani fenil, piperidinil, pirimidinil ili piridil; i/ili Y je NH, O, CH2, C=O ili veza; i/ili R4 je vodik, metil, etil, metoksietil ili izopropil; kad je R3 supstituiran, može biti supstituiran s fluorom, klorom, cijano, CONH2, metilom, metoksi ili trifluormetoksi; i kad je B supstituiran, može biti supstituiran s metilom.
3. Spoj prema bilo kojem od zahtjeva 1 do 2, naznačen time što R1 i R2 su različiti od vodika i piperazinski C* ugljici imaju 3R,5S-konfiguraciju.
4. Spoj prema zahtjevu 1, naznačen time što je: 6-(3-fluorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-[(4-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 1-(4-fluorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-piperidinkarboksamid 6-(4-fluorfenil)-N,2-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(4-fluorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-(4-morfolinil)-3-piridinkarboksamid 4’-fluor-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-bifenilkarboksamid 6-(4-fluorfenil)-2-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 1-[(3-fluorfenil)karbonil]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-piperidinkarboksamid 1-[(3-fluorfenil)metil]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-piperidinkarboksamid 1-(4-klorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-piperidinkarboksamid N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-(1-piperidinil)-3-piridinkarboksamid 6-(2-fluorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(2,4-difluorfenil)-N,2-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3,4-difluorfenil)-N,2-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3-fluorfenil)-N,2-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 4-[(3-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)benzamid 6-(3-cijanofenil)-N,2-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(4-cijanofenil)-N,2-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 4-[(4-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)benzamid N-(4-{[(3R,5S)-3,5-dimetil-1-piperazinil]metil}fenil)-6-(4-fluorfenil)-N,2-dimetil-3-piridinkarboksamid 2-[(4-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)benzamid N-(4-{[(3R,5S)-3,5-dimetil-1-piperazinil]metil}fenil)-6-(4-fluorfenil)-N-metil-3-piridinkarboksamid 2-[(2-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)benzamid 3-[(4-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)benzamid 3-[(3-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)benzamid 6-[(4-fluorfenil)amino]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 2-(4-fluorfenil)-N,4-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-5-pirimidinkarboksamid 2-(4-fluorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-5-pirimidinkarboksamid 6-(4-fluorfenil)-N,2-dimetil-N-(4-{[(3R)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(4-fluorfenil)-N-metil-N-(4-{[(3R)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 4’-fluor-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-bifenilkarboksamid 4’-fluor-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-bifenilkarboksamid 6-(2-cijanofenil)-N,2-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3-fluorfenil)-N-metil-N-[4-(1-piperazinilmetil)fenil]-3-piridinkarboksamid 6-[(3-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-[(2-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3-fluorfenil)-N,2-dimetil-N-[4-(1-piperazinilmetil)fenil]-3-piridinkarboksamid 6-[2-(aminokarbonil)fenil]-N,2-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3-fluorfenil)-N-metil-N-(3-metil-4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3-cijanofenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(2-cijanofenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-[(3-cijanofenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid N-(2-fluor-4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-(3-fluorfenil)-N-metil-3-piridinkarboksamid 5-[(4-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid 5-[(3-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid N-(2-fluor-4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-[(4-fluorfenil)oksi]-N-metil-3-piridinkarboksamid 5-[(3-cijanofenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid 5-[(4-fluorfenil)amino]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid 1-[(3,4-difluorfenil)metil]-N-metil-N-(4- { [(3S)-3-metil-1-piperazinil]metil}fenil)-4-piperidinkarboksamid 1-[(4-fluorfenil)metil]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-piperidinkarboksamid N-(3-fluor-4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-(3-fluorfenil)-N-metil-3-piridinkarboksamid N-(3-fluor-4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-[(4-fluorfenil)oksi]-N-metil-3-piridinkarboksamid 1-[(3-cijanofenil)metil]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-piperidinkarboksamid 1-[(4-cijanofenil)metil]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-piperidinkarboksamid 6-(3-fluorfenil)-N-(1-metiletil)-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid N-etil-6-(3-fluorfenil)-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3- fluorfenil)-N-[2-(metiloksi) etil]-N-(4- { [ (3S)- 3- metil- 1- piperazinil] metil} fenil)- 3- piridinkarboksamid 6-[(4-fluorfenil)oksi]-N-metil-N-(3-metil-4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3-fluorfenil)-N-metil-N-(5-{[(3S)-3-metil-1-piperazinil]metil}-2-piridinil)-3-piridinkarboksamid 6-[(4-fluorfenil)oksi]-N-metil-N-(5-{[(3S)-3-metil-1-piperazinil]metil}-2-piridinil)-3-piridinkarboksamid 6-[(4-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid 6-(4-fluor-4-piperidinil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-(3-fluorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid N-metil-4-(3-metil-1,2,4-oksadiazol-5-il)-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)benzamid N-etil-6-[(4-fluorfenil)oksi]-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-(3-piridiniloksi)-3-piridinkarboksamid 6-[(3-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid 6-(4,4-difluor-1-piperidinil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid 6-[(4-fluorfenil)oksi]-N-metil-N-(6-{[(3S)-3-metil-1-piperazinil]metil}-3-piridinil)-3-piridinkarboksamid 5-(4-fluorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid 5-(3-cijanofenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid N-metil-5-[3-(metiloksi)fenil]-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid N-metil-5-[4-(metiloksi)fenil]-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid 5-(3-fluorfenil)-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2-piridinkarboksamid 6-[(4-fluorfenil)oksi]-N-metil-N-(4-metil-5-{[(3S)-3-metil-1-piperazinil]metil}-2-piridinil)-3-piridinkarboksamid 6-(4-fluorfenil)-N-metil-N-(6-{[(3S)-3-metil-1-piperazinil]metil}-3-piridinil)-3-piridinkarboksamid N,2’-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3,4’-bipiridin-6-karboksamid 6-[(4-fluorfenil)oksi]-N-[2-(metiloksi)etil]-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid N-(3-klor-4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-[(4-fluorfenil)oksi]-N-metil-3-piridinkarboksamid N,2’-dimetil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-2,4’-bipiridin-5-karboksamid N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-(2-piridinil)benzamid N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-(2-pirimidinil)benzamid N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-(1H-pirazol-1-il)benzamid N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-6-(1H-pirol-1-il)-3-piridinkarboksamid N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-4-{[4-(trifluormetil)fenil]karbonil}benzamid ili njegova sol.
5. Spoj prema zahtjevu 1, naznačen time što je 6-[(4-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamid ili njegova sol.
6. Spoj prema zahtjevu 1, naznačen time što je fumaratna sol 6-[(4-fluorfenil)oksi]-N-metil-N-(4-{[(3S)-3-metil-1-piperazinil]metil}fenil)-3-piridinkarboksamida.
7. Spoj prema zahtjevu 1, naznačen time što je 6-[(4-fluorfenil)oksi]-N-metil-N-(4-metil-5-{[(3S)-3-metil-1-piperazinil]metil}-2-piridinil)-3-piridinkarboksamid ili njegova sol.
8. Spoj kao što je definirano u bilo kojem od zahtjeva 1 do 7, naznačen time što se upotrebljava kao terapijska tvar.
9. Spoj kao što je definirano u bilo kojem od zahtjeva 1 do 7, ili njegova farmaceutski prihvatljiva sol, naznačen time što se upotrebljava za liječenje stanja ili poremećaja posredovanih putem receptora GPR38.
10. Spoj kao što je definirano u bilo kojem od zahtjeva 1 do 7 ili njegova farmaceutski prihvatljiva sol, koji se upotrebljava za liječenje stanja ili poremećaja posredovanih putem receptora GPR38, naznačen time što stanje ili poremećaj su poremećaji gastroezofagealnog refluksa, funkcionalna dispepsija, sindrom iritabilnog crijeva, zatvor, intestinalna pseudo-opstrukcija, paralitički ileus nakon operacije ili druge manipulacije, povraćanje, želučana staza ili hipomotilitet uzrokovan raznim bolestima poput dijabetesa i/ili primjenom drugih lijekova, ili kod enteralno hranjenih pacijenata, Crohnova bolest, kolitis, kaheksija povezana s uznapredovalim bolestima kao što je rak i/ili njegovo liječenje, kaheksija povezana s apetitom/metabolizmom i drugi poremećaji kao što je inkontinencija.
11. Upotreba spoja prema bilo kojem od zahtjeva 1 do 7, ili njegove farmaceutski prihvatljive soli, naznačena time što se upotrebljava za proizvodnju lijeka za upotrebu u liječenju stanja ili poremećaja putem receptora GPR38.
12. Upotreba prema zahtjevu 11, naznačena time što stanje ili poremećaji su poremećaji gastroezofagealnog refluksa, funkcionalna dispepsija, sindrom iritabilnog crijeva, zatvor, intestinalna pseudo-opstrukcija, paralitički ileus nakon operacije ili druge manipulacije, povraćanje, želučana staza ili hipomotilitet uzrokovan raznim bolestima poput dijabetesa i/ ili primjenom drugih lijekova, ili kod enteralno hranjenih pacijenata, Crohnove bolesti, kolitis, kaheksija povezana s uznapredovalim bolestima kao što je rak i/ili njegovo liječenje, kaheksija povezana s apetitom/metabolizmom i drugi poremećaji kao što je inkontinencija.
13. Farmaceutski pripravak, naznačen time što sadržava spoj definiran prema bilo kojem od zahtjeva 1 do 7, ili njegova farmaceutski prihvatljiva sol.
14. Postupak, naznačen time što se upotrebljava za dobivanje farmaceutskog pripravka prema zahtjevu 13.
15. Postupak za dobivanje spoja prema zahtjevu 1 ili njegove soli, naznačen time što postupak sadržava reakciju spoja formule (II) [image] u kojem R1, R2, A i R4 su kao što je definirano iznad i Q je vodik ili odgovarajuća zaštitna skupina dušika i spoja formule R3-Y-B-C(=O)-L1 u kojem R3, B i Y su kao što je definirano iznad i L1 je odlazeća skupina, upotrebom uvjeta prikladnih za formiranje amidne veze.
16. Postupak za dobivanje spoja prema zahtjevu 1 ili njegove soli, naznačen time što postupak sadržava reakciju spoja formule (VIII) [image] u kojem R1, R2, R4, A, B i Q su kao što je definirano iznad i L3 predstavlja odlazeću skupinu, i spoja formule M1-Y-R3 u kojem R3 i Y su kao što je definirano u zahtjevu 1 i M1 predstavlja vodik ili metalni ostatak, po potrebi u prisutnosti odgovarajućeg i po potrebi upotrebom prikladnog katalizatorskog sustava s prijelaznim metalom i nakon toga po potrebi izvođenje jedne ili više od sljedećih reakcija: a. Prevođenje jednog spoja formule (I) u drugi spoj formule (I); b. Uklanjanje bilo koje zaštitne skupine; c. Formiranje prikladne farmaceutski prihvatljive soli ili solvata tako formiranog spoja.
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ATE465150T1 (de) 2010-05-15
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US8853218B2 (en) 2014-10-07
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