HRP20220310T1 - Inhibitori glukozilceramid sintaze - Google Patents
Inhibitori glukozilceramid sintaze Download PDFInfo
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- HRP20220310T1 HRP20220310T1 HRP20220310TT HRP20220310T HRP20220310T1 HR P20220310 T1 HRP20220310 T1 HR P20220310T1 HR P20220310T T HRP20220310T T HR P20220310TT HR P20220310 T HRP20220310 T HR P20220310T HR P20220310 T1 HRP20220310 T1 HR P20220310T1
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- 239000003892 ceramide glucosyltransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 24
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 6
- 208000026372 Congenital cystic kidney disease Diseases 0.000 claims 5
- 208000015439 Lysosomal storage disease Diseases 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 201000002648 nephronophthisis Diseases 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 102000044956 Ceramide glucosyltransferases Human genes 0.000 claims 3
- 208000015872 Gaucher disease Diseases 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 108091000114 ceramide glucosyltransferase Proteins 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 230000002132 lysosomal effect Effects 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 2
- 208000010061 Autosomal Dominant Polycystic Kidney Diseases 0.000 claims 2
- 208000002814 Autosomal Recessive Polycystic Kidney Diseases 0.000 claims 2
- 208000017354 Autosomal recessive polycystic kidney disease Diseases 0.000 claims 2
- 102000004190 Enzymes Human genes 0.000 claims 2
- 108090000790 Enzymes Proteins 0.000 claims 2
- 208000024720 Fabry Disease Diseases 0.000 claims 2
- 102000004547 Glucosylceramidase Human genes 0.000 claims 2
- 108010017544 Glucosylceramidase Proteins 0.000 claims 2
- 208000007696 Multicystic Dysplastic Kidney Diseases 0.000 claims 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 2
- 208000026911 Tuberous sclerosis complex Diseases 0.000 claims 2
- 102000005840 alpha-Galactosidase Human genes 0.000 claims 2
- 108010030291 alpha-Galactosidase Proteins 0.000 claims 2
- 208000022185 autosomal dominant polycystic kidney disease Diseases 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 230000002981 neuropathic effect Effects 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
- 208000009999 tuberous sclerosis Diseases 0.000 claims 2
- 208000006542 von Hippel-Lindau disease Diseases 0.000 claims 2
- OJCLMSVFVVKWJX-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-3-yl n-[2-[3-(4-fluorophenyl)phenyl]propan-2-yl]carbamate Chemical compound C1N(CC2)CCC2C1OC(=O)NC(C)(C)C(C=1)=CC=CC=1C1=CC=C(F)C=C1 OJCLMSVFVVKWJX-UHFFFAOYSA-N 0.000 claims 1
- 208000006515 AB Variant Tay-Sachs Disease Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000036075 Autosomal dominant tubulointerstitial kidney disease Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 208000026292 Cystic Kidney disease Diseases 0.000 claims 1
- 201000008892 GM1 Gangliosidosis Diseases 0.000 claims 1
- 208000037310 Gaucher disease type 2 Diseases 0.000 claims 1
- 208000037311 Gaucher disease type 3 Diseases 0.000 claims 1
- 102000016871 Hexosaminidase A Human genes 0.000 claims 1
- 108010053317 Hexosaminidase A Proteins 0.000 claims 1
- 102000016870 Hexosaminidase B Human genes 0.000 claims 1
- 108010053345 Hexosaminidase B Proteins 0.000 claims 1
- 208000034946 Juvenile nephronophthisis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- YFHRCLAKZBDRHN-MRXNPFEDSA-N [(3s)-1-azabicyclo[2.2.2]octan-3-yl] n-[2-[2-(4-fluorophenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate Chemical compound O([C@H]1C2CCN(CC2)C1)C(=O)NC(C)(C)C(N=1)=CSC=1C1=CC=C(F)C=C1 YFHRCLAKZBDRHN-MRXNPFEDSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000007547 defect Effects 0.000 claims 1
- 238000000502 dialysis Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000000523 end stage renal failure Diseases 0.000 claims 1
- 150000002339 glycosphingolipids Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 201000001228 nephronophthisis 1 Diseases 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
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- 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
- A61K31/435—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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- 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
- A61K31/535—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
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- 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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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
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Claims (19)
1. Spoj za upotrebu u liječenju lizosomske bolesti nakupljanja kod subjekta kod kojeg je dijagnosticirana navedena bolest, koji se sastoji od davanja subjektu učinkovite količine spoja, te po izboru dodatno obuhvaća korak davanja subjektu terapeutski učinkovite količine lizosomalnog enzima, naznačen time što je spoj predstavljen sa sljedećom strukturnom formulom,
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu:
n je 1 ili 2;
m je 1;
p je 1;
t je 0 ili 1;
y je 1;
z je 0 ili 1;
E je O;
X1 je CR1;
X2 je O;
X3 je -NH;
X4 je izravna veza ili CR4R5;
X5 je izravna veza ili O;
R1 je H ili (C1-C6)alkil;
R4 i R5 su neovisno odabrani od (C1-C6)alkila, ili uzeti zajedno s ugljikom na koji su vezani tvore spiro (C3-C10)cikloalkilni prsten;
R6 je -H ili (C1-C6)alkil;
A1 je (C6-C12)aril ili (C2-C9)heteroaril, po izboru supstituiran s jednim ili više supstituenata odabranih iz skupine koju čine: halo; (C1-C6)alkil po izboru supstituiran s jednim do tri halo; (C1-C6)alkoksi; i -OH; i
A2 je (C6-C12)aril ili (C2-C9)heteroaril, supstituiran s jednim ili više supstituenata odabranih iz skupine koju čine: (C2-C9)heterocikloalkil; R8R9N-CO- pri čemu R8 i R9 su svaki neovisno odabrani iz skupine koju čine vodik i (C1-C6)alkil ili R8 i R9 mogu se uzeti zajedno s dušikom na koji su vezani tako da tvore (C2-C9)heterocikloalkilnu skupinu koja je izborno supstituirana s jednom do tri halo skupine; (C1-C6)alkilsulfonil izborno supstituiran s jednom ili dvije skupine odabrane od (C1-C6)alkoksi i (C3-C10)cikloalkil; (C1-C6)alkil supstituiran s jednim do četiri supstituenta odabrana iz skupine koju čine hidroksi, (C1-C6)alkoksi, (C1-C6)alkoksi(C1-C6)alkoksi, (C2-C9)heterocikloalkil, i (C2-C9)heteroaril; i (C1-C6)alkiloksi supstituiran s jednim do četiri supstituenta odabrana iz skupine koju čine cijano, (C1-C6)alkoksi, (C2-C9)heterocikloalkil, i (C2-C9)heteroaril.
2. Spoj za upotrebu prema patentnom zahtjevu 1, naznačen time što n je 1; t je 0; y je 1 i z je 1.
3. Spoj za upotrebu prema patentnom zahtjevu 1 ili zahtjevu 2, naznačen time što R6 je H.
4. Spoj za upotrebu prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time što R1 je vodik ili metil.
5. Spoj za upotrebu prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time što X4 je CR4R5 pri čemu R4 i R5 su svaki neovisno metil.
6. Spoj za upotrebu prema patentnom zahtjevu 1, naznačen time što je spoj predstavljen formulom
[image]
ili njegova farmaceutski prihvatljiva sol.
7. Spoj za upotrebu prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time što je lizosomska bolest nakupljanja posljedica defekta glikosfingolipidnog puta, na pr. pri čemu je lizosomska bolest nakupljanja odabrana iz skupine koju čine Gaucherova bolest, Fabryeva bolest, GM1-gangliozidoza, nedostatak GM2 aktivatora, Tay-Sachs i Sandhoff, posebno pri čemu je lizosomska bolest nakupljanja Fabryeva bolest, Gaucherova bolest tip 2 ili Gaucherova bolest tip 3.
8. Spoj za upotrebu prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time što je lizosomski enzim odabran iz skupine koju čine glukocerebrozidaza, alfa-galaktozidaza A, heksosaminidaza A, heksosaminidaza B i GM1-gangliozid-β-galaktozidaza, naročito pri čemu je lizosomski enzim alfa-galaktozidaza A ili glukocerebrozidaza.
9. Spoj za upotrebu u liječenju, ublažavanju ili prevenciji cističnih bolesti, npr. pri čemu je cistična bolest bubrega, po izboru odabrana iz niza koji čine stečena bubrežna cistična bolest (ARCD), cistična bolest povezana s dijalizom, autosomno dominantna policistična bolest bubrega (ADPKD), autosomno recesivna policistična bolest bubrega (ARPKD), kongenitalni multicistični bubreg (CMK), multicistični displastični bubreg, terminalna bubrežna bolest (ESRD), medularni spužvasti bubreg (MSK), kompleks nefronoftiza-medularna cistična bolest bubrega (NMCD), kompleks nefronoftiza-uremična medularna cistična bolest, juvenilna nefronoftiza, medularna cistična bolest, karcinom bubrežnih stanica (RCC), tuberozna skleroza (TS), i sindrom von Hippel-Lindau (VHLS), pri čemu navedeni spoj je (S)-kinuklidin-3-il (2-(2-(4-fluorofenil)tiazol-4-il)propan-2-il)karbamat, ili kinuklidin-3-il (2-(4'-fluoro-[1,1'-bifenil]-3-il)propan-2-il)karbamat, ili spoj formule I kako je definiran u bilo kojem od patentnih zahtjeva 1 do 6.
10. Spoj predstavljen sljedećom strukturnom formulom,
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time što:
n je 1 ili 2;
m je 1;
p je 1;
t je 0 ili 1;
y je 1;
z je 1;
E je O;
X1 je CR1;
X2 je O;
X3 je -NH;
X4 je CR4R5;
X5 je izravna veza ili O;
R1 je H ili (C1-C6)alkil;
R4 i R5 su neovisno odabrani od (C1-C6)alkil, ili uzeti zajedno s ugljikom na koji su vezani tvore spiro (C3-C10)cikloalkilni prsten;
R6 je -H ili (C1-C6)alkil;
A1 je (C6-C12)aril ili (C2-C9)heteroaril, po izboru supstituiran s jednim ili više supstituenata odabranih iz skupine koju čine: halo; (C1-C6)alkil po izboru supstituiran s jednim do tri halo; (C1-C6)alkoksi; i -OH; i
A2 je (C6-C12)aril ili (C2-C9)heteroaril, supstituiran s jednim ili više supstituenata odabranih iz skupine koju čine: (C2-C9)heterocikloalkil; R8R9N-CO- pri čemu R8 i R9 su svaki neovisno odabrani iz skupine koju čine vodik i (C1-C6)alkil ili R8 i R9 mogu se uzeti zajedno s dušikom na koji su vezani tako da tvore (C2-C9)heterocikloalkilnu skupinu koja je izborno supstituirana s jednom do tri halo skupine; (C1-C6)alkilsulfonil izborno supstituiran s jednom ili dvije skupine odabrane od (C1-C6)alkoksi i (C3-C10)cikloalkil; (C1-C6)alkil supstituiran s jednim do četiri supstituenta odabrana iz skupine koju čine hidroksi, (C1-C6)alkoksi, (C1-C6)alkoksi(C1-C6)alkoksi, (C2-C9)heterocikloalkil, i (C2-C9)heteroaril; i (C1-C6)alkiloksi supstituiran s jednim do četiri supstituenta odabrana iz skupine koju čine cijano, (C1-C6)alkoksi, (C2-C9)heterocikloalkil, i (C2-C9)heteroaril.
11. Spoj prema patentnom zahtjevu 10, naznačen time što n je 1; t je 0; y je 1 i z je 1.
12. Spoj prema patentnom zahtjevu 10 ili zahtjevu 11, naznačen time što R1 je vodik ili metil.
13. Spoj prema bilo kojem od patentnih zahtjeva 10 do 12, naznačen time što X4 je CR4R5 pri čemu su R4 i R5 svaki neovisno metil.
14. Spoj prema bilo kojem od patentnih zahtjeva 10 do 12, naznačen time što X4 je CR4R5 pri čemu su R4 i R5 uzeti zajedno s ugljikom na koji su vezani tako da tvore spiro ciklopropilni prsten.
15. Spoj predstavljen formulom
[image]
ili njegova farmaceutski prihvatljiva sol.
16. Farmaceutski pripravak naznačen time što sadrži spoj prema bilo kojem od patentnih zahtjeva 10 do 15 i najmanje jedan farmaceutski prihvatljiv nosač.
17. Spoj prema bilo kojem od patentnih zahtjeva 10 do 15, ili farmaceutski pripravak prema zahtjevu 16, za upotrebu u terapiji.
18. Spoj prema bilo kojem od patentnih zahtjeva 10 do 15, ili farmaceutski pripravak prema zahtjevu 16, za uporabu u liječenju bolesti ili poremećaja posredovanog glukozilceramid sintazom (GCS) ili bolesti ili poremećaja u kojem je implicirana GCS, pri čemu je bolest ili poremećaj rak, metabolički poremećaj, ili neuropatska bolest.
19. Spoj ili farmaceutski pripravak za upotrebu prema patentnom zahtjevu 18, naznačen time što je neuropatska bolest Alzheimerova bolest ili Parkinsonova bolest.
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US201261699714P | 2012-09-11 | 2012-09-11 | |
EP13765893.6A EP2895484B1 (en) | 2012-09-11 | 2013-09-10 | Glucosylceramide synthase inhibitors |
PCT/US2013/058896 WO2014043068A1 (en) | 2012-09-11 | 2013-09-10 | Glucosylceramide synthase inhibitors |
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