HRP20161690T1 - Modulatori jetrenog receptora x - Google Patents
Modulatori jetrenog receptora x Download PDFInfo
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- HRP20161690T1 HRP20161690T1 HRP20161690TT HRP20161690T HRP20161690T1 HR P20161690 T1 HRP20161690 T1 HR P20161690T1 HR P20161690T T HRP20161690T T HR P20161690TT HR P20161690 T HRP20161690 T HR P20161690T HR P20161690 T1 HRP20161690 T1 HR P20161690T1
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- alkyl
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- 102000004311 liver X receptors Human genes 0.000 title claims 2
- 108090000865 liver X receptors Proteins 0.000 title claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 59
- 125000001188 haloalkyl group Chemical group 0.000 claims 27
- 125000004093 cyano group Chemical group *C#N 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 18
- 229910003827 NRaRb Inorganic materials 0.000 claims 12
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000002950 monocyclic group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 5
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 150000001356 alkyl thiols Chemical class 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 201000005991 hyperphosphatemia Diseases 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 150000003573 thiols Chemical class 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- -1 tert7-butyl Chemical group 0.000 claims 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 208000000044 Amnesia Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 208000022461 Glomerular disease Diseases 0.000 claims 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010055171 Hypertensive nephropathy Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000010577 Niemann-Pick disease type C Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000028990 Skin injury Diseases 0.000 claims 1
- 206010040954 Skin wrinkling Diseases 0.000 claims 1
- 208000007930 Type C Niemann-Pick Disease Diseases 0.000 claims 1
- 206010048214 Xanthoma Diseases 0.000 claims 1
- 206010048215 Xanthomatosis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 201000001883 cholelithiasis Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 208000006132 lipodystrophy Diseases 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008024 pharmaceutical diluent Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 201000001474 proteinuria Diseases 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 230000009759 skin aging Effects 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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Claims (18)
1. Spoj. naznačen time što ga prikazuje sljedeća strukturna formula:
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
X je N ili CRC:
R1 je alkil ili-NRaRb;
R2 je H: halogen; -CN; -NRC(O)R; -C(O)OR: -C(O)NRaRb; monociklički heteroaromat. koji može biti supstituiran s jednom ili više skupina, koje se bira između alkila, -CN, -NRC(O)R, -C(O)OR, -C(O)NRaRb i halogena; monociklički nearomatski heterocikl. koji može biti supstituiran s jednom ili više skupina, koje se bira između alkila, halogena, -CN i =O; ili alkil, koji može biti supstituiran s jednom ili više skupina, koje se bira između halogena. hidroksi. alkoksi. -NRaRb, -NRC(O)R, -NRC(O)O(alkila), -NRC(O)N(R)2. -C(O)OR, tiola, alkiltiola. nitro, -CN. =O. -OC(O)H, -OC(O)(alkila), -OC(O)O(alkila). -OC(O)N(R)2 i -C(0)NRaRb;
R3 je alkil, halogenalkil, hidroksialkil, alkoksialkil. cikloalkil, monociklički nearomatski heterocikl. monociklički heteroaromat ili fenil, gdje fenil, monociklički nearomatski heterocikl i monociklička heteroaromatska skupina koju predstavlja R3 mogu biti supstituirani s jednom ili više skupina, koje se bira između alkila, halogena, halogenalkila, alkoksi, halogenalkoksi, nitro i -CN;
R4 i R5 su neovisno halogen, -CN, -OR, -SR, -N(R)2, -C(O)R, -C(O)0R, -OC(O)O(alkil). -C(O)O(halogenalkil), -OC(O)R. -C(O)N(R)2. -OC(O)N(R)2. -NRC(0)R, -NRC(O)O(alkil), -S(O)R, -SO2R. -SO2N(R):, -NRS(O)R, -NRSO2R, -NRC(O)N(R)2, -NRSO2N(R)2, halogenalkil, halogenalkoksi, cikloalkoksi, cikloalkil, monociklički nearomatski heterocikl. monociklički heteroaromat ili alkil, gdje alkil. monociklički nearomatski heterocikl i monociklička heteroaromatska skupina koju predstavlja R4 ili R5 mogu biti supstituirani s jednom ili više skupina, koje se bira između -CN, -OR, -SR, -N(R)2, =O, -C(O)R, -C(O)OR, -C(O)O(halogenalkila), -OC(O)R, -OC(O)O(alkila), -C(O)N(R)2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkil), -S(O)R, -SO2R. -SO2N(R)2. -NRS (O)R, -NRSO2R, -NRC(O)N(R)2 i –NRSO2N(R)2;
R6 je H. halogen. -CN, -OR, -SR, -N(R)2. -C(O)R, -C(O)OR, -OC(O)O(alkil), -C(O)O(halogenalkil). -OC(O)R, -C(O)N(R)2. -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R, -NRC(O)N(R)2. -NRSO2 N(R)2, halogenalkil, halogenalkoksi, cikloalkoksi, cikloalkil ili alkil, gdje je alkilna skupina koju predstavlja R6 izborno supstituirana s jednom ili više skupina, koje se bira između -CN, -OR, -SR, -N(R)2. =O, -C(O)R, -C(O)OR, -C(O)O(halogenalkila), -OC(O)R, -OC(O)O(alkila), -C(O)N(R)2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkila), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R. -NRC(O)N(R)2 i -NRSO2N(R)2: ili
R5 i R6. uzeti zajedno s atomima ugljika na koje su vezani, tvore monociklički nearomatski heterocikl, koji može biti supstituiran s jednom ili više skupina, koje se bira između alkila, halogena, hidroksialkila, alkoksialkila, halogenalkila i =O; i
svaki R je neovisno H ili alkil;
Ra i Rb su neovisno H, alkil, ili se Ra i Rb može uzeti zajedno s dušikom na kojeg su vezani kako bi tvorili monociklički nearomatski heterocikl; i
Rc je H, alkil ili halogen.
2. Spoj u skladu s patentnim zahtjevom 1. naznačen time što:
R3 je alkil, halogenalkil, hidroksialkil, alkoksialkil, cikloalkil, ili fenil, gdje je fenilna skupina koju predstavlja R3 izborno supstituirana s jednom ili više skupina, koje se bira između alkila, halogena. Halogenalkila, alkoksi, halogenalkoksi, nitro i -CN;
R4 i R5 su neovisno halogen. –CN, -OR, –SR, -N(R)2, -C(O)R, -C(O)OR, -OC(O)O(alkil), -C(O)O(halogenalkil), -OC(O)R, -C(O)N(R)2, -OC(O)N(R);. -NRC(O)R, -NRC(O)O(alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R, -NRC(0)N(R),. -NRSO2N(R)2, halogenalkil, halogenalkoksi, cikloalkoksi, cikloalkil ili alkil, gdje je alkil kojeg predstavlja R4 ili R5 izborno supstituiran s jednom ili više skupina, koje se bira između -CN, -OR, -SR, -N(R)2, =O, -C(O)R, -C(O)OR, -C(O)O(halogenalkila), -OC(O)R, -OC(O)O(alkila), -C(O)N(R)2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkil), -S(O)R -SO2R, -SO2N(R)2, -NRS (O)R, -NRSO2R, -NRC(O)N(R)2 i -NRSO2N(R)2;
R6 je H, halogen. -CN, -OR, -SR, -N(R)2, -C(o)R, -C(O)OR, -OC(O)O(alkil), -C(O)O(halogenalkil), -OC(O)R, -C(O)N(R)2, -OC(O)N(R)2. -NRC(O)R, -NRC(O)O (alkil), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R, -NRC(O)N(R)2, -NRSO2N(R)2, halogenalkil, halogenalkoksi, cikloalkoksi, cikloalkil ili alkil. gdje je alkilna skupina koju predstavlja R6 izborno supstituirana s jednom ili više skupina, koje se bira između -CN, -OR, -SR, -N(R)2, =O, -C(O)R, -C(O)OR, -C(O)O(halogenalkila), -OC(O)R, -OC(O)O(alkila), -C(O)N(R)2, -OC(O)N(R)2, -NRC(O)R, -NRC(O)O(alkila), -S(O)R, -SO2R, -SO2N(R)2, -NRS(O)R, -NRSO2R, -NRC(O)N(R)2 i -NRSO2N(R)2.
3. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što spoj prikazuje sljedeća strukturna formula:
[image]
ili njegova farmaceutski prihvatljiva sol.
4. Spoj u skladu s patentnim zahtjevom 1 ili 2. naznačen time što spoj prikazuje sljedeća strukturna formula:
[image]
ili njegova farmaceutski prihvatljiva sol.
5. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što:
R1 je metil ili-NH2;
R2 je H ili metil, gdje je metilna skupina koju predstavlja R2 izborno supstituirana s jednom ili više skupina, koje se bira između halogena, hidroksi, alkoksi, -NRaRb, -NRC(O)R, -NRC(O)O(alkila), -NRC(O)N(R)2, -C(O)OR, tiola. alkiltiola, nitro, -CN, =O, -OC(O)H, -OC(O)(alkila), -OC(O)O(alkila), -C(O)NRaRb i -OC(O)N(R)2;
R3 je metil. etil. propil, izopropil, tert7-butil, sec-butil, iso-butil. -CH2CF3, -CH(CH2F)2, -CH(CHF2)2, -CH(CF3)2- -CF(CH3)2, -CF3, ciklopropil, ciklobutil, ciklopentil, cikloheksil, -C(OH)(CH3)2, -CH(OH)(CH3) ili fenil, gdje je fenilna skupina koju predstavlja R3 izborno supstituirana s jednom ili više skupina, koje se bira između alkila, halogena, halogenalkila, alkoksi, halogenalkoksi, nitro i -CN; i
Rc. kada je prisutan, je H.
6. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što:
R1 je metil;
R2je-CH2OH:
R5 je izopropil; i
R4 i R3 su neovisno halogen, hidroksi, alkil, cikloalkil, cikloalkoksi, alkoksi, halogenalkoksi, halogenalkil, -N(R)2. -C(O)OH, -C(O)O(alkil), -C(O)O(halogenalkil), -C(O)(alkil), -C(O) N(R)2, -NRC(O)R, -SO2N(R)2, -OC(O)N(R)2, -CN, hidroksialkil ili dihidroksialkil.
7. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što su R4 i R5 neovisno metil, etil, hidroksi, CF3, izopropil, ciklopropil, -CH2OH, -CH(OH)(CH2)(OH), -C(OH)(CH3)2, -CH(OH)(CH3), -CH(OH)(CH2)(CH3), -CH(OH)(CH2)2(CH3), -C(O)NH2, -C(O)N(CH3)2, -C(O)OH, -C(O)NH(CH3), -C(O)CH3, -C (O)CH2CH3, -C(O)O(CH2)(CH3), -C(O)O(terc-butil), -C(O)O(C)(CH3)2(CF3), -NHC(O)CH3, -OCHF2, -OCF3, -OCH2CH3, -OCH(CH3)2 ili -OCH3.
8. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je R4 alkil, halogenalkil, cikloalkil, alkoksi, ili halogenalkoksi.
9. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je R4 metil, halogenirani metil, ciklopropil, -OCHF2 ili -OCH3.
10. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je R4 CF3.
11. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je R5 -C(OH)(CH3)2.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time što spoj prikazuje strukturna formula koja se bira između:
[image]
[image]
[image]
ili njihovih farmaceutski prihvatljivih soli.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time što spoj prikazuje sljedeća strukturna formula:
[image]
ili njegova farmaceutski prihvatljiva sol.
14. Farmaceutski pripravak, naznačen time što sadrži farmaceutsku podlogu ili razrjeđivač uz spoj u skladu s bilo kojim od patentnih zahtjeva 1-13.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-13. naznačen time što je namijenjen upotrebi u liječenju subjekta s bolešću ili poremećajem koji se može liječiti pozitivnim reguliranjem aktivnosti LXR.
16. Upotreba u skladu s patentnim zahtjevom 15. naznačena time što je bolest ili poremećaj hiperlipidemija, hiperkolesterolemija, hiperlipoproteinemija, hipertrigliceriđemija, lipodistrofija, masna jetra, nealkoholni steatohepatitis (NASH), nealkoholna bolest masne jetre (NAFLD), hiperglikemija. otpornost na inzulin, dijabetes melitus, dislipidemija, kardiovaskularna bolest, ateroskleroza, bolest žučnih kamenaca, obične akne, dermatitis. psorijaza. kontaktni dermatitis, atopični dermatitis, egzem, kožne ozljede, starenje kože, solarno starenje, boranje, dijabetes, Niemann-Pickova bolest tip C. Parkinsonova bolest, Alzheimerova bolest, upala, ksantom. pretilost, metabolički sindrom, sindrom X. inzult, periferna okluzivna bolest, gubitak pamćenja, dijabetične neuropatije, proteinurija, glomerulopatije. dijabetična nefropatija, hipertenzivna nefropatija, IGA nefropatija. lokalna segmentalna glomeruloskleroza. hiperfosfatemija, kardiovaskularne komplikacije hiperfosfatemije, rak ili multipla skleroza.
17. Spoj. namijenjen upotrebi u skladu s patentnim zahtjevom 16. naznačen time što je bolest ili poremećaj ateroskleroza. Alzheimerova bolest, kardiovaskularna bolest, kardiovaskularne komplikacije hiperfosfatemije ili dermatitis.
18. Spoj. naznačen time što ga prikazuje sljedeća strukturna formula:
[image]
ili njegova sol. gdje:
X je N ili CRc:
R10 je alkil ili -NRaRb:
R20 je H: halogen; -CN: -NRC(O)R; -C(O)OR; -C(O)NRaRb; monociklički heteroaromat, koji može biti supstituiran s jednom ili više skupina, koje se bira između alkila, -CN, -NRC(O)R, -C(O)OR, -C(O)NRaRb i halogena; monociklički nearomatski heterocikl. koji može biti supstituiran s jednom ili više skupina, koje se bira između alkila, halogena. -CN i =O: ili alkil, koji može biti supstituiran s jednom ili više skupina, koje se bira između halogena, hidroksi, alkoksi, -NRaRb, -NRC(O)R, -NRC(O)O(alkila), -NRC(O)N(R)2, -C(O)OR, tiola, alkiltiola, nitro, -CN, =O, -OC(O)H, -OC(O)(alkila), -OC(O)O(alkila), -OC(O)N(R)2, -C(O)NRaRb i -O(zaštitne skupine);
R30 je alkil, halogenalkil, hidroksialkil, alkoksialkil, cikloalkil ili fenil, gdje je fenilna skupina koju predstavlja R30 izborno supstituirana s jednom ili više skupina, koje se bira između alkila, halogenalkila, alkoksi, halogenalkoksi, nitro i -CN;
svaki R je neovisno H ili alkil;
Ra i Rb su neovisno H, alkil, ili se Ra i Rb može uzeti zajedno s dušikom na kojeg su vezani kako bi tvorili monociklički nearomatski heterocikl; i
Rc je H, alkil ili halogen.
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