HRP20211923T1 - Pirimidin-2-ilamino-1h-pirazoli kao inhibitori lrrk2 za uporabu u liječenju neurodegenerativnih poremećaja - Google Patents
Pirimidin-2-ilamino-1h-pirazoli kao inhibitori lrrk2 za uporabu u liječenju neurodegenerativnih poremećaja Download PDFInfo
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- 208000015122 neurodegenerative disease Diseases 0.000 title claims 4
- 229940124786 LRRK2 inhibitor Drugs 0.000 title 1
- YZVIWEZBAJAZOB-UHFFFAOYSA-N N-pyrazol-1-ylpyrimidin-2-amine Chemical class N1=C(N=CC=C1)NN1N=CC=C1 YZVIWEZBAJAZOB-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 19
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 8
- -1 amino, amidino Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009900 Colitis ulcerative Diseases 0.000 claims 3
- 208000011231 Crohn disease Diseases 0.000 claims 3
- 206010012289 Dementia Diseases 0.000 claims 3
- 208000012661 Dyskinesia Diseases 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 3
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 3
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 3
- 206010024229 Leprosy Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- 208000018737 Parkinson disease Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 206010038389 Renal cancer Diseases 0.000 claims 3
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 201000005787 hematologic cancer Diseases 0.000 claims 3
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 201000010982 kidney cancer Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 230000004770 neurodegeneration Effects 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000005338 substituted cycloalkoxy group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 claims 1
- 102000009784 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Human genes 0.000 claims 1
- 108010020246 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Proteins 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-M Thiocyanate anion Chemical compound [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000001149 cognitive effect Effects 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 1
- 150000007857 hydrazones Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 208000028774 intestinal disease Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 150000002923 oximes Chemical class 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- BUUPQKDIAURBJP-UHFFFAOYSA-N sulfinic acid Chemical compound OS=O BUUPQKDIAURBJP-UHFFFAOYSA-N 0.000 claims 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 125000000464 thioxo group Chemical group S=* 0.000 claims 1
Classifications
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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Claims (20)
1. Spoj, naznačen time, da je predstavljen formulom Ia:
[image]
ili njegova farmaceutski prihvatljiva sol, deuterirani analog, stereoizomer, ili mješavina stereoizomera, gdje:
R1 je opcionalno supstituirani cikloalkil ili C1-6 alkil opcionalno supstituiran s halogenom;
R2 je halogen, cijano, opcionalno supstituirani C1-6 alkil, opcionalno supstituirani C1-6 alkenil, opcionalno supstituirani C1-6 alkinill, opcionalno supstituirani cikloalkil, opcionalno supstituirani C1-6 alkoksi, opcionalno supstituirani cikloalkoksi, opcionalno supstituirani C1-6 alkiltio, opcionalno supstituirani C1-6 alkilsulfonil, -C(O)R10, ili -C(O)N(R11)(R12);
R3 je opcionalno supstituirani C1-6 alkoksi, opcionalno supstituirani cikloalkil, opcionalno supstituirani cikloalkoksi, opcionalno supstituirani C1-6 alkiltio, opcionalno supstituirani C1-6 alkilsulfonil, ili -N(R11)(R12);
R4 je vodik ili halogen;
svaki od R6 i R7 je neovisno vodik ili C1-6 alkil opcionalno supstituiran s halogenom;
svaki od R8 i R9 je neovisno vodik, cijano, halogen, opcionalno supstituirani C1-6 alkil, opcionalno supstituirani C1-6 alkoksi, ili opcionalno supstituirani heteroaril;
svaki R10 je neovisno opcionalno supstituirani C1-6 alkil, ili opcionalno supstituirani C1-6 alkoksi; i
svaki od R11 i R12 je neovisno vodik, opcionalno supstituirani C1-6 alkil, ili opcionalno supstituirani cikloalkil;
pri čemu se opcionalni supstituent bira od sljedećih: alkil, alkenil, alkinil, alkoksi, alkiltio, acil, amido, amino, amidino, aril, aralkil, azido, karbamoil, karboksil, karboksil ester, cijano, cikloalkil, cikloalkilalkil, gvanadin, halogen, haloalkil, haloalkoksi, hidroksialkil, heteroalkil, heteroaril, heteroarilalkil, heterociklil, heterociklilalkil, hidrazin, hidrazon, imino, imido, hidroksi, okso, oksim, nitro, sulfonil, sulfinil, alkilsulfonil, alkilsulfinil, tiocijanat, sulfinska kiselina, sulfonska kiselina, sulfonamido, tiol, tiokso, N-oksid, ili -Si(Ry)3, dok je svaki Ry neovisno vodik, alkil, alkenil, alkinil, heteroalkil, cikloalkil, aril, heteroaril ili heterociklil.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da R6 i R7 su metil.
3. Spoj prema patentnom zahtjevu 1, naznačen time, da najmanje jedan od R8 i R9 jest vodik, primjerice gdje oba dva R8 i R9 su vodik.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da ili (A) R1 je opcionalno supstituirani ciklopropil ili opcionalno supstituirani ciklobutil; ili (B) da R1 je cikloalkil neovisno supstituiran s jednim ili više halogena, hidroksi, cijano, ili heteroarila; ili (C) da R1 je ciklopropil, ciklobutil, hidroksiciklobut-3-il, cijanociklobut-3-il, triazol-2-il-ciklobut-3-il, triazol-1-il-ciklobut-3-il, ili fluorociklobut-3-il; ili (D) da R1 je CD3, etil, ili prop-2-il.
5. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, da R2 je halogen, cijano, C1-6 alkil opcionalno supstituiran s halogenom, primjerice time, da R2 je brom ili -CF3.
6. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, da R3 je opcionalno supstituirani cikloalkil, opcionalno supstituirani C1-6 alkoksi, ili -N(R11)(R12), primjerice time, da R3 je ciklopropil, metoksi, 1,1-difluoroet-2-ilamino, ciklopropilamino, -NH(CH3), ili -NH(CH2CH3).
7. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, da R4 je vodik.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da R1 je cikloalkil neovisno supstituiran s jednim ili više hidroksi, cijano ili heteroarila; R2 je halogen ili C1-6 fluoroalkil; R3 je -N(R11)(R12) ili C1-6 alkoksi; i R4 jest H.
9. Spoj prema patentnom zahtjevu 1, naznačen time, da se spoj bira od:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol, deuterirani analog, tautomer, stereoizomer, ili mješavina stereoizomera.
10. Spoj prema patentnom zahtjevu 9, naznačen time, da ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, deuterirani analog, ili tautomer.
11. Spoj prema patentnom zahtjevu 9, naznačen time, da ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, deuterirani analog, ili tautomer.
12. Spoj prema patentnom zahtjevu 9, naznačen time, da ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, deuterirani analog, ili tautomer.
13. Spoj prema patentnom zahtjevu 9, naznačen time, da ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, deuterirani analog, ili tautomer.
14. Spoj prema patentnom zahtjevu 9, naznačen time, da ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, deuterirani analog, ili tautomer.
15. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 9 do 14, ili njegovu farmaceutski prihvatljivu sol, deuterirani analog, tautomer, stereoizomer, ili mješavinu stereoizomera, te farmaceutski prihvatljiv nosač, razrjeđivač ili pomoćno sredstvo.
16. Farmaceutski pripravak prema patentnom zahtjevu 15, naznačen time, da je za uporabu u postupku liječenja bolesti ili stanja koje je barem djelomično posredovano s LRRK2, pri čemu postupak obuhvaća davanje učinkovite količine farmaceutskog pripravka prema patentnom zahtjevu 15, pojedincu kojemu je to potrebno, dok bolest ili stanje je neurodegenerativna bolest; Parkinsonova bolest ili demencija; poremećaj središnjeg živčanog sustava (CNS); Alzheimerova bolest ili L-Dopa inducirana diskinezija; rak; rak bubrega, rak dojke, rak prostate, rak krvi, papilarni rak, rak pluća, akutna mijeloična leukemija, ili multipli mijelom; upalna bolest; lepra, Crohnova bolest, upalna bolest crijeva, ulcerativni kolitis, amiotrofična lateralna skleroza, reumatoidni artritis ili ankilozantni spondilitis.
17. Farmaceutski pripravak prema patentnom zahtjevu 15, naznačen time, da je za uporabu u postupku povećanja kognitivne memorije, pri čemu postupak obuhvaća davanje učinkovite količine farmaceutskog pripravka prema patentnom zahtjevu 15, pojedincu kojemu je to potrebno.
18. Spoj prema patentnom zahtjevu 1, naznačen time, da je za uporabu u liječenju.
19. Spoj prema patentnom zahtjevu 1, naznačen time, da je za uporabu u liječenju neurodegenerativne bolesti, raka ili upalne bolesti; ili Alzheimerove bolesti, L-Dopa inducirane diskinezije, Parkinsonove bolesti, demencije, raka bubrega, raka dojke, raka prostate, raka krvi, papilarnog raka, raka pluća, akutne mijeloične leukemije, multiplog mijeloma, lepre, Crohnove bolesti, upalne bolesti crijeva, ulcerativnog kolitisa, amiotrofične lateralne skleroze, reumatoidnog artritisa ili ankilozantnog spondilitisa.
20. Uporaba spoja prema patentnom zahtjevu 1, naznačena time, da je za proizvodnju lijeka za liječenje neurodegenerativne bolesti, raka ili upalne bolesti; ili Alzheimerove bolesti, L-Dopa inducirane diskinezije, Parkinsonove bolesti, demencije, amiotrofične lateralne skleroze, raka bubrega, raka dojke, raka prostate, raka krvi, papilarnog raka, raka pluća, akutne mijeloične leukemije, multiplog mijeloma, lepre, Crohnove bolesti, upalne bolesti crijeva, ulcerativnog kolitisa, reumatoidnog artritisa ili ankilozantnog spondilitisa.
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