HRP20161010T1 - C5ar antagonisti - Google Patents

C5ar antagonisti Download PDF

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Publication number
HRP20161010T1
HRP20161010T1 HRP20161010TT HRP20161010T HRP20161010T1 HR P20161010 T1 HRP20161010 T1 HR P20161010T1 HR P20161010T T HRP20161010T T HR P20161010TT HR P20161010 T HRP20161010 T HR P20161010T HR P20161010 T1 HRP20161010 T1 HR P20161010T1
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HR
Croatia
Prior art keywords
group
alkyl
heteroaryl
independently selected
aryl
Prior art date
Application number
HRP20161010TT
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English (en)
Inventor
Pingchen Fan
Kevin Lloyd Greenman
Manmohan Reddy Leleti
Yandong Li
Jay Powers
Hiroko Tanaka
Ju Yang
Yibin Zeng
Original Assignee
Chemocentryx, Inc.
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Application filed by Chemocentryx, Inc. filed Critical Chemocentryx, Inc.
Publication of HRP20161010T1 publication Critical patent/HRP20161010T1/hr

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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Claims (27)

1. Spoj formule [image] ili njegova farmaceutski prihvatljiva sol, hidrat ili rotomer; naznačen time, da C1 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R1; C2 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenata R2; C3 je odabran iz skupine koja se sastoji od C1-8 alkila, C3-8 cikloalkila, C3-8 cikloalkil-C1-4 alkila, arila, aril-C1-4 alkila, heteroarila, heteroaril-C1-4 alkila, heterocikloalkila ili heterocikloalkil-C1-4 alkila, pri čemu heterocikloalkilna skupina ili dio skupine sadržava od 1 do 3 heteroatoma odabrana iz skupine koja se sastoji od N, O i S, te pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S, a svaki C3 prema potrebi je supstituiran s 1 do 3 supstituenta R3; svaki R1 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rc, -CO2Ra, -CONRaRb, -C(O)Ra, OC(O)NRaRb, -NRbC(O)Ra, -NRbC(O)2Rc, -NRa- C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa, -S(O)2NRaRb; pri čemu je svaki Ra i Rb neovisno odabran između vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika, mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena odabrane među N, O ili S; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, a pri čemu su alifatski i ciklički dijelovi Ra, Rb i Rc prema potrebi dodatno supstituirani sa jednim do tri halogena, hidroksi, metil, amino, alkilamino i dialkilamino skupinama; i po želji, kada se dva R1 supstituenta na susjednim atomima kombiniraju tako da tvore kondenzirani peteročlani ili šesteročlani karbociklični prsten; svaki R2 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rf, -CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, - NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, i -S(O)2NRdRe; pri čemu je svaki od Rd i Re neovisno odabran iz skupine koju čine vodik, C1-8 alkil i C1-8 haloalkil, ili kada je spojen na isti atom dušika, može se kombinirati s dušikovim atomom tako da tvori peteročlani ili šesteročlani prsten sa 0 do 2 dodatna heteroatoma kao članova prstena, odabranih iz niza N, O ili S; svaki Rf neovisno je odabran iz skupine koju čine C1-8 alkil, C1-8 haloalkil, C3-6 cikloalkil, heterocikloalkil, aril i heteroaril, pri čemu su alifatski i ciklički dijelovi Rd, Re i Rf prema potrebi dodatno supstituirani s jednim do tri halogena, hidroksi, metil, amino, alkilamino i dialkilamino skupinom; svaki R3 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Ri, -CO2Rg, -CONRgRh, - C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, -NRgC(O)NRgRh, -NRgRh, - ORg, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh , -X4-CONRgRh, -X4-NRhC(O)Rg, -NHRj i - NHCH2Rj, pri čemu je X4 C1-4 alkilen; svaki Rg i Rh neovisno je odabran iz skupine koju čine vodik, C1-8 alkil, C3-6 cikloalkil i C1-8 haloalkil, ili kada su spojeni na isti atom dušika, mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena, koji su odabrani među N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki R1 neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; a svaki Rj odabran je iz skupine koju čine C3-6cikloalkil, pirolinil, piperidinil, moRfolinil, tetrahidrofuranil i tetrahidropiranil i pri čemu su alifatski i ciklički dijelovi Rg, Rh, Ri i Rj prema potrebi dodatno supstituirani s jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino i dialkilamino; i X je vodik ili CH3.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da:X je vodik.
3. Spoj u skladu s patentnim zahtjevom 1 naznačen time, da spoj ima formulu: [image] ili spoj ima formulu: [image]
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da spoj ima formulu: [image] ili [image] pri čemu X1 je odabran iz skupine koja sadržava N, CH i CR1; indeks n je cijeli broj od 0 do 2; X2 je odabran iz skupine koja sadržava N, CH i CR2; a indeks m je cijeli broj od 0 do 2,
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da spoj ima formulu: [image] pri čemu je indeks p cijeli broj od 0 do 3.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da spoj ima formulu: [image] pri čemu je R3 odabran iz skupine koju čine -NRgRh, -NHRj -NHCH2Rj, -X4-NRgRh, -X4- Rj i -X4-NRhCORg.
7. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C1 odabran iz skupine koju čine fenil, piridil, indolil i tiazolil, od kojih je svaki prema potrebi supstituiran s od 1 do 3 supstituenta R1; i pri čemu je svaki R1 neovisno odabran iz skupine koja se sastoji od halogena, -CN, - Rc, -NRaRb i -ORa, i pri čemu je svaki Ra i Rb neovisno odabran iz skupine koju čine vodik, C1-8 alkil i C1-8 haloalkil, ili kada su vezani na isti atom dušika, mogu se kombinirati s dušikovim atomom i tvoriti pirolidinski prsten; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila i C3-6 cikloalkila, i pri čemu su alifatski i ciklički dijelovi Ra, Rb i Rc prema potrebi dodatno supstituirani s jednom do tri hidroksi, metil amino, alkilamino i dialkilamino skupine; i po želji, kada su dva supstituenta R1 na susjednim atomima, kombiniraju se tako da tvore peteročlani ili šesteročlani kaRbociklički prsten.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C2 odabran iz skupine koja sadržava fenil, naftil, piridil i indolil, od kojih je svaki prema potrebi supstituiran sa 1 do 3 R2 supstituenta; i pri čemu je svaki R2 neovisno odabran iz skupine koja se sastoji od halogena, Rf i - ORd; pri čemu je svaki Rd neovisno odabran od vodika, C1-8 alkila i C1-8 haloalkila; svaki Rf neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Rd i Rf prema potrebi dodatno supstituirani s jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino.
9. Spoj u skladu s patentnim zahtjevom 7, naznačen time, da je C1 odabran iz skupine koju čine [image]
10. Spoj u skladu s patentnim zahtjevom 8, naznačen time, da je C2 odabran iz skupine koju čine: [image]
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C3 odabran iz skupine koju čine C3-6 alkil, C3-6 cikloalkil, C3-6 cikloalkilC1-2alkil, fenil, piridinil, pirazolil, piperidinil, pirolidinil, piperidinilmetil i pirolidinilmetil, od kojih je svaki prema potrebi supstituiran sa 1 do 3 supstituenta R3, pri čemu je svaki R3 neovisno odabran iz skupine koja se sastoji od halogena, -Ri -CO2Rg, -CONRgRh, -NRhC(O)Rg, - NRhC(O)2Ri, -NRgRh , -ORg, -X4-Rj -X4-NRgRh, -X4-CONRgRh, -X4-NRhC(O)Rg,, -NHRj i - NHCH2Rj, pri čemu je X4 C1-3 alkilen; svaki od Rg i Rh neovisno je odabran iz skupine koju čine vodik, C1-8 alkil, C3-6 cikloalkil i C1-8 haloalkil, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji sadržava od 0 do 1 dodatnog heteroatoma kao članove prstena odabrane iz skupine koju čine N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki Ri neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; i svaki Rj odabran je iz skupine koju čine C3-6cikloalkil, pirolinil, piperidinil, moRfolinil, tetrahidrofuranil i tetrahidropiranil, i pri čemu su alifatski i ciklički dijelovi Rg, Rh, Ri i RJ prema potrebi dodatno supstituirani s jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino i dialkilamino.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C3 odabran iz skupine koju čine: [image]
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C3 odabran iz skupine koju čine: [image]
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj odabran iz skupine koju čine: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i
15. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je navedeni spoj [image] ili njegova farmaceutski prihvatljiva sol.
16. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je navedeni spoj [image] ili njegova farmaceutski prihvatljiva sol.
17. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je navedeni spoj [image] ili njegova farmaceutski prihvatljiva sol.
18. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 17, naznačen time, da se rabi u terapijskom liječenju ljudskog ili životinjskog tijela.
19. Farmaceutski pripravak, naznačen time, da sadržava farmaceutski prihvatljivi nosač i spoj formule [image] ili njegova farmaceutski prihvatljiva sol, hidrat ili rotomer; pri čemu C1 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R1; C2 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R2; C3 je odabran iz skupine koja se sastoji od C1-8 alkila, C3-8 cikloalkila, C3-8 cikloalkil-C1-4 alkila, arila, aril-C1-4 alkila, heteroarila, heteroaril-C1-4 alkila, heterocikloalkila ili heterocikloalkil-C1-4 alkila, pri čemu je heterocikloalkil skupina ili njezin dio sadržava od 1 do 3 heteroatoma odabrana iz skupine koja se sastoji od N, O i S, te pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S, a svaki C3 prema potrebi je supstituiran s 1 do 3 supstituenta R3; svaki R1 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rc, -CO2Ra, -CONRaRb, -C(O)Ra, -OC(O)NRaRb, -NRbC(O)Ra, -NRbC(O)2Rc, -NRa- C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa i -S(O)2NRaRb; pri čemu je svaki Ra i Rb neovisno odabran između vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao člana prstena iz niza N, O ili S; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Ra, Rb i RC prema potrebi dodatno supstituirani s jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; i po želji, kada su dva supstituenta R1 na susjednim atomima, kombiniraju se tako da tvore peteročlani ili šesteročlani karbociklični prsten; svaki R2 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rf, -CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, - NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, i -S(O)2NRdRe; pri čemu je svaki Rd i Re neovisno odabran iz skupine koja se sastoji od vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima 0 do 2 dodatna heteroatoma kao članove prstena odabrane od N, O ili S; svaki Rf neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Rd, Re i Rf prema potrebi dodatno supstituirani s jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; svaki R3 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Ri, -CO2R9, -CONRgRh, -C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, - NRgC(O)NRgRh, -NRgRh, -ORg, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh, -X4-CONRg Rh, - X4-NRhC(O)Rg, -NHRj i -NHCH2Rj, pri čemu je X4 C1-4 alkilen; svaki Rg i Rh neovisno je odabran iz skupine koja se sastoji od vodika, C1-8 alkila, C3-6 cikloalkila i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena odabrane između N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki Ri neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; i svaki Rj je odabran iz skupine koju čine C3-6 cikloalkil, pirolinil, piperidinil, moRfolinil, tetrahidrofuranil i tetrahidropiranil, i pri čemu su alifatski i ciklički dijelovi RG, Rh, R1 i RJ prema potrebi dodatno supstituirani s jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino i dialkilamino; i X je vodik ili CH3.
20. Spoj za uporabu u postupku liječenja sisavca koji pati od ili je sklon bolestima ili poRemećajima koji uključuju patološku aktivaciju C5a receptora, naznačen time, da je bolest ili poRemećaj upalna bolest ili poRemećaj; kardiovaskularni ili cerebrovaskularni poRemećaj; autoimuni poRemećaj; ili patološka posljedica povezane sa skupinom koju čine dijabetes ovisan o inzulinu, mellitus, lupus nefropatija, Heymann nefritis, membranski nefritis, glomerulonefritis, Reakcija na osjetljivost na kontakt i upala koje su posljedica kontakta krvi s umjetnim površinama; navedeni postupak uključuje primjenu djelotvorne količine spoja na sisavcu, pri čemu navedeni spoj ima formulu: [image] ili je njegova farmaceutski prihvatljiva sol, hidrat ili rotomer; pri čemu C1 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R1; C2 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 R2 supstituenta; C3 je odabran iz skupine koja se sastoji od C1-8 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-4 alkil, aril, aril-C1-4 alkil, heteroaril, heteroaril-C1-4 alkil, heterocikloalkil ili heterocikloalkil-C1-4 alkil, pri čemu heterocikloalkil skupina ili njezin dio sadržava od 1 do 3 heteroatoma odabrana iz skupine koja se sastoji od N, O i S, te pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S, i svaki C3 prema potrebi je supstituiran s 1 do 3 R3 supstituenta; svaki R1 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rc, -CO2Ra, -CONRaRb, -C(O)Ra, -OC(O)NRaRb, -NRbC(O)Ra, -NRbC(O)2Rc, -NRa- C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa, -S(O)2NRaRb; pri čemu je svaki Ra i Rb neovisno odabran između vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma, kao članove prstena iz niza N, O ili S; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Ra, Rb i RC prema potrebi dodatno supstituirani sa jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; i po želji, kada se dva supstituenta R1 na susjednim atomima kombiniraju tako da tvore petero ili šesteročlani karbociklični prsten; svaki R2 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rf, -CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, - NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, i -S(O)2NRdRe; pri čemu je svaki Rd i Re neovisno odabran od vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena, odabranih od N, O ili S; svaki Rf neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Rd, Re i Rf prema potrebi dodatno supstituirani s jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; svaki R3 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Ri, -CO2R9, -CONRgRh, - C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, -NRgC(O)NRgRh, -NRgRh, - ORg, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh, -X4-CONR9 Rh, -X4-NRhC(O)Rg, -NHRj i - NHCH2Rj, pri čemu je X4 C1-4 alkilen; svaki Rg i Rh neovisno je odabran iz skupine koja se sastoji od vodika, C1-8 alkila, C3-6 cikloalkila i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena odabrane između N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki Ri neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; i svaki Rj odabran je iz skupine koju čine C3-6cikloalkil, pirolinil, piperidinil, moRfolinil, tetrahidrofuranil i tetrahidropiranil i pri čemu su alifatski i ciklički dijelovi Rg, Rh, Ri i Rj prema potrebi dodatno supstituiran s jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino i dialkilamino ; i X je vodik ili CH3.
21. Spoj za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da je upalna bolest ili poRemećaj odabran iz skupine koju čine neutropenija, sepsa, septički šok, Alzheimerova bolest, multipla skleroza, moždani udar, upalne bolesti crijeva, kronična opstruktivna plućna bolest, upala povezana s opeklinama, oštećenja pluća, osteoartritis, atopični dermatitis, kronična urtikarija, ishemijsko-RepeRfuzijske ozljede, sindrom akutnog Respiratornog distResa, sindrom sistemskog upalnog odgovora, sindrom višestruke disfunkcije oRgana, odbacivanje transplantata tkiva i hiperakutno odbacivanja transplantiranih oRgana; kaRdiovaskularni ili ceRebrovaskularni poRemećaj bira se iz skupine koju čine infarkt miokaRda, koronarna tromboza, vaskularna okluzija, postoperativna vaskularna Reokluzija, ateroskleroza, traumatska ozljeda sRedišnjeg živčanog sustava i ishemijske srčane bolesti; i autoimuni poRemećaj odabran je iz skupine koju čine Reumatoidni artritis, sistemski eritematozni lupus, Guillain-BarRe sindrom, pankReatitis, lupus nefritis, lupus glomerulonefritis, psorijaza, Crohnova bolest, vaskulitis, sindrom iritabilnog crijeva, dermatomiozitis, multipla skleroza, bronhijalna astma, pemfigus, pemfigoid, skleroderma, mijastenija gravis, autoimuna hemolitička i trombocitopenična stanja, GoodpastuReov sindrom, immunovasculitis, odbacivanje tkivnih transplantata i hiperakutno odbacivanja transplantiranih oRgana.
22. Spoj za uporabu u skladu s patentnim zahtjevom 20 ili 21, naznačen time, da je bolest ili poRemećaj upalna bolest ili poRemećaj.
23. Spoj za uporabu u skladu s patentnim zahtjevom 20 ili 21, naznačen time, da je bolest ili poRemećaj kaRdiovaskularni ili ceRebrovaskularni poRemećaj.
24. Spoj za uporabu u skladu s patentnim zahtjevom 20 ili 21, naznačen time, da je bolest ili poRemećaj autoimuni poRemećaj.
25. Spoj za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da je bolest ili poRemećaj patološka posljedica povezana sa skupinom koju čine dijabetes uvjetovan inzulinom, šećerna bolest, lupus nefropatija, Heymann nefritis, membranski nefritis, glomerulonefritis, Reakcija osjetljivosti na kontakt te upala uslijed kontakta krvi s umjetnim površinama.
26. Spoj za uporabu u metodi inhibiranja stanične kemotaksije posRedovane Receptorom C5a u liječenju stanja koje je autoimuni poRemećaj, upalni poRemećaj, patološka posljedica povezana s diabetes mellitusom ovisnomo inzulinu (uključujući dijabetičku Retinopatiju), lupus nefropatija, Heymann nefritis, membranski nefritis ili drugi oblik glomerulonefritisa, Reakcije osjetljivosti na kontakt, odnosno upala uslijed kontakta krvi s umjetnim površinama koje mogu izazvati aktivaciju komplementa; bolesti povezane s ishemijskim / RepeRfuzijskim ozljedama; makularna degeneracija; kaRdiovaskularne ili ceRebrovaskularne bolesti; bolest vaskulitisa; infekcija HIV-om ili AIDS; neurodegenerativni poRemećaj; naznačen time, da podrazumijeva dovođenje u kontakt bijelih krvnih stanica sisavaca s količinom spoja koja ima modulacijski učinak na Receptor C5a, a spoj ima formulu [image] ili je njegova farmaceutski prihvatljiva sol, hidrat ili rotomer istih; pri čemu C1 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, 0 i S i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R1; C2 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, 0 i S i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R2; C3 je odabran iz skupine koja se sastoji od C1-8 alkila, C3-8 cikloalkila, C3-8 cikloalkil- C1-4 alkila, arila, aril-C1-4 alkila, heteroarila, heteroaril-C1-4 alkila, heterocikloalkila ili heterocikloalkil C1-4 alkila, pri čemu heterocikloalkil skupina ili dio sadržava od 1 do 3 heteroatoma odabrana iz skupine koja se sastoji od N, O i S, te pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S, i svaki C3 prema potrebi je supstituiran s 1 do 3 supstituenta R3; svaki R1 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rc, - CO2Ra, -CONRaRb, -C(O)Ra, -OC(O)NRaRb, -NRbC(O)Ra, -NRbC(O)2Rc, -NRa- C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa, -S(O)2NRaRb; pri čemu je svaki Ra i Rb neovisno odabran između vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s atomom dušika kako bi tvorili petero ili šestero člani prsten koji ima od 0 do 2 dodatna heteroatoma kao članova prstena odabrana iz skupine koja se sastoji od N, O ili S; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Ra, Rb i Rc prema potrebi dodatno supstituirani sa jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; i po želji, kada se dva supstituenta R1 na susjednim atomima kombiniraju tako da tvore kondenzirani peteročlani ili šesteročlani karbociklični prsten; svaki R2 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rf, - CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, -NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, i -S(O)2NRdRe; pri čemu je svaki od Rd i Re neovisno odabran od vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena, odabranih od N, O ili S; svaki Rf neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Rd, Re i Rf prema potrebi dodatno supstituirani s od jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; svaki R3 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Ri, - CO2R9, -CONRgRh, -C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, -NRgC(O)NRgRh, -NRgRh, -OR9, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh, -X4-CONR9 Rh, -X4-NRhC(O)Rg, -NHRj i -NHCH2Rj, pri čemu je X4 C1-4 alkilen; svaki Rg i Rh neovisno je odabran iz skupine koja se sastoji od vodika, C1-8 alkila, C3-6 cikloalkila i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena odabrane između N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki Ri neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; i svaki Rj je odabran iz skupine koju čine C3-6 cikloalkil, pirolinil, piperidinil, morfolinil, tetrahidrofuranil i tetrahidropiranil, i pri čemu su alifatski i ciklički dijelovi Rg, Rh, Ri i RJ prema potrebi dodatno supstituirani sa jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino, i dialkilamino; i X je vodik ili CH3.
27. Spoj za uporabu u skladu s patentnim zahtjevom 26 za liječenje bolesti, naznačen time, da je bolest odabrana iz skupine koju čine sepsa kronične opstruktivne plućne bolesti (KOPB), Reumatski artritis, lupus nefritis i multipla skleroza.
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