HRP20220913T1 - Inhibitori rho kinaze - Google Patents
Inhibitori rho kinaze Download PDFInfo
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- HRP20220913T1 HRP20220913T1 HRP20220913TT HRP20220913T HRP20220913T1 HR P20220913 T1 HRP20220913 T1 HR P20220913T1 HR P20220913T T HRP20220913T T HR P20220913TT HR P20220913 T HRP20220913 T HR P20220913T HR P20220913 T1 HRP20220913 T1 HR P20220913T1
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- alkyl
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- independently selected
- halo
- alkenyl
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- 239000003590 rho kinase inhibitor Substances 0.000 title 1
- -1 hydroxy, amino Chemical group 0.000 claims 20
- 125000005843 halogen group Chemical group 0.000 claims 19
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 15
- 125000004093 cyano group Chemical group *C#N 0.000 claims 15
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 15
- 125000001424 substituent group Chemical group 0.000 claims 15
- 125000005842 heteroatom Chemical group 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 6
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 6
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 6
- 125000004043 oxo group Chemical group O=* 0.000 claims 6
- 101000669921 Homo sapiens Rho-associated protein kinase 2 Proteins 0.000 claims 4
- 102100039314 Rho-associated protein kinase 2 Human genes 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
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Claims (4)
1. Spoj koji inhibira ROCK 2 za upotrebu u liječenju autoimunog poremećaja kod subjekta, pri čemu je autoimuni poremećaj psorijaza, atopijski dermatitis, ekcem ili bolest transplantata protiv domaćina (GVHD), te pri čemu je spoj koji inhibira ROCK2 spoj s formulom (XXXII):
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu:
R1 je odabran iz skupine koja sadrži -O-(CH2)y-CO2R12, -O-(CH2)y-C(=O)NR13R14, -O-(CH2)y-heteroaril, -O-(CH2)y-cikloalkil, -O-C(=O)-(CH2)y-NR13R14, -O-(CH2)z-NR13R14, -NH-C(=O)-(CH2)y-NR13R14, -NH-C(=O)-X-R15, -NH-(CH2)y-NR13R14;
R12 je odabran iz skupine koja sadrži C1-C6 alkil, -(C1-C6 alkil)-O-(C1-C6 alkil), -(C1-C6 alkil)-NR16R17, -(C1-C6 alkil)-C(=O)NR16R17, -(C1-C6 alkil)-O-(C1-C6 alkil)-O-(C1-C6 alkil), aril, aralkil, heteroaril, C3-C7 cikloalkil, tro- do dvanaesteročlani heterociklički prsten koji sadrži do 3 heteroatoma, od kojih svaki može biti izborno supstituiran na jednom ili više atoma ugljika s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
R13 i R14 su neovisno odabrani iz skupine koju čine H, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, -(C1-C6 alkil)-O-(C1-C6 alkil), -(C1-C6 alkil)-NR16R17, -(C1-C6 alkil)-C(=O)NR16R17 , aril, aralkil, heteroaril, C3-C7 cikloalkil, tro- do dvanaesteročlani heterociklički prsten koji sadrži do 3 heteroatoma, od kojih svaki može biti po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C3-C7 cikloalkil, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
ili R13 i R14 mogu se uzeti zajedno da tvore tro- do dvanaesteročlani heterociklički prsten koji ima do 3 heteroatoma koji je po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, C3-C7 cikloalkil, okso, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
X je odabran od kovalentne veze, O, NH, i C1-C6 alkil;
R15 je odabran iz skupine koja sadrži heteroaril, C3-C7 cikloalkil, tro- do dvanaesteročlani heterociklički prsten koji sadrži do 3 heteroatoma, od kojih svaki može biti po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoro alkil,
ili R15 je odabran od -(C1-C6 alkil)-O-(C1-C6 alkil), -(C1-C6 alkil)-NR16R17, -CO2R18, -O-(CH2)x-CO2R18, i -C(=O)NR16R17;
R16 i R17 su neovisno odabrani iz skupine koju čine H, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, -(C1-C6 alkil)-O-(C1-C6 alkil), aril, aralkil, heteroaril, C3-C7 cikloalkil, tro- do dvanaesteročlani heterociklički prsten koji sadrži do 3 heteroatoma, od kojih svaki može biti po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
ili R16 i R17 mogu se uzeti zajedno da tvore tro- do dvanaesteročlani heterociklički prsten koji ima do 3 heteroatoma koji je po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, okso, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
R18 je odabran iz skupine koja sadrži H, aril, aralkil, heteroaril, C1-C6 alkil, -(C1-C6 alkil)-O-(C1-C6 alkil), -(C1-C6 alkil)-NR16R17, -(C1-C6 alkil)-O-(C1-C6 alkil)-O-(C1-C6 alkil), od kojih svaki može biti po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoroalkil;
x je odabran od 0 do 6;
y je odabran od 0 do 6;
z je odabran od 2 do 6;
svaki R2 je neovisno odabran iz skupine koja sadrži niži alkil, CN, halo, hidroksi, niži alkoksi, amino, i perfluoro niži alkil;
svaki R3 je neovisno odabran iz skupine koja sadrži niži alkil, CN, halo, hidroksi, niži alkoksi, amino, i perfluoro niži alkil;
n je odabran od 0 do 4; i
m je odabran od 0 do 3.
2. Spoj za upotrebu prema zahtjevu 1, naznačen time što je spoj koji inhibira ROCK2 spoj s formulom
[image]
3. Spoj za upotrebu prema zahtjevu 1, naznačen time što je spoj koji inhibira ROCK2 spoj s formulom XXXIV:
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu:
R13 i R14 su neovisno odabrani iz skupine koju čine H, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, -(C1-C6 alkil)-O-(C1-C6 alkil), -(C1-C6 alkil)-NR16R17, -(C1-C6 alkil)-C(=O)NR16R17 , aril, aralkil, heteroaril, C3-C7 cikloalkil, tro- do dvanaesteročlani heterociklički prsten koji sadrži do 3 heteroatoma, od kojih svaki može biti po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C3-C7 cikloalkil, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
ili R13 i R14 mogu se uzeti zajedno da tvore tro- do dvanaesteročlani heterociklički prsten koji ima do 3 heteroatoma koji je po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, C3-C7 cikloalkil, okso, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
R16 i R17 su neovisno odabrani iz skupine koju čine H, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, -(C1-C6 alkil)-O-(C1-C6 alkil), aril, aralkil, heteroaril, C3-C7 cikloalkil, tro- do dvanaesteročlani heterociklički prsten koji sadrži do 3 heteroatoma, od kojih svaki može biti po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
ili R16 i R17 mogu se uzeti zajedno da tvore tro- do dvanaesteročlani heterociklički prsten koji ima do 3 heteroatoma koji je po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, okso, hidroksi, amino,
cijano i C1-C3 perfluoro alkil;
svaki R2 je neovisno odabran iz skupine koja sadrži niži alkil, CN, halo, hidroksi, niži alkoksi, amino, i perfluoro niži alkil;
svaki R3 je neovisno odabran iz skupine koja sadrži niži alkil, CN, halo, hidroksi, niži alkoksi, amino, i perfluoro niži alkil;
n je odabran od 0 do 4; i
m je odabran od 0 do 3.
4. Spoj za upotrebu prema zahtjevu 1, naznačen time što je spoj koji inhibira ROCK2 spoj s formulom XXXIVa:
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu:
R13 i R14 su neovisno odabrani iz skupine koju čine H, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, -(C1-C6 alkil)-O-(C1-C6 alkil), -(C1-C6 alkil)-NR16R17, -(C1-C6 alkil)-C(=O)NR16R17 , aril, aralkil, heteroaril, C3-C7 cikloalkil, tro- do dvanaesteročlani heterociklički prsten koji sadrži do 3 heteroatoma, od kojih svaki može biti po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C3-C7 cikloalkil, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
ili R13 i R14 mogu se uzeti zajedno da tvore tro- do dvanaesteročlani heterociklički prsten koji ima do 3 heteroatoma koji je po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, okso, hidroksi, amino,
cijano i C1-C3 perfluoro alkil;
R16 i R17 su neovisno odabrani iz skupine koju čine H, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, -(C1-C6 alkil)-O-(C1-C6 alkil), aril, aralkil, heteroaril, C3-C7 cikloalkil, tro- do dvanaesteročlani heterociklički prsten koji sadrži do 3 heteroatoma, od kojih svaki može biti po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, hidroksi, amino, cijano i C1-C3 perfluoro alkil;
ili R16 i R17 mogu se uzeti zajedno da tvore tro- do dvanaesteročlani heterociklički prsten koji ima do 3 heteroatoma koji je po izboru supstituiran s od 1 do 3 supstituenta neovisno odabrana iz niza koji sadrži halo, C1-C6 alkil, C2-C6 alkenil, C1-C6 alkoksi, okso, hidroksi, amino, cijano i C1-C3 perfluoro alkil.
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PCT/US2013/063752 WO2014055996A2 (en) | 2012-10-05 | 2013-10-07 | Rho kinase inhibitors |
EP13843426.1A EP2903618B1 (en) | 2012-10-05 | 2013-10-07 | Rho kinase inhibitors |
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