HRP20201054T1 - Modulatori receptora x jetre (lxr) - Google Patents
Modulatori receptora x jetre (lxr) Download PDFInfo
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- HRP20201054T1 HRP20201054T1 HRP20201054TT HRP20201054T HRP20201054T1 HR P20201054 T1 HRP20201054 T1 HR P20201054T1 HR P20201054T T HRP20201054T T HR P20201054TT HR P20201054 T HRP20201054 T HR P20201054T HR P20201054 T1 HRP20201054 T1 HR P20201054T1
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- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- image
- compound according
- alkyl
- Prior art date
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- 102000004311 liver X receptors Human genes 0.000 title 1
- 108090000865 liver X receptors Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- -1 -C(=O)NHCH2CF3 Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010008635 Cholestasis Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 108010023302 HDL Cholesterol Proteins 0.000 claims 1
- 206010019668 Hepatic fibrosis Diseases 0.000 claims 1
- 238000008214 LDL Cholesterol Methods 0.000 claims 1
- 108010028554 LDL Cholesterol Proteins 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 230000003143 atherosclerotic effect Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000007870 cholestasis Effects 0.000 claims 1
- 231100000359 cholestasis Toxicity 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002440 hepatic effect Effects 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000037819 metastatic cancer Diseases 0.000 claims 1
- 208000011575 metastatic malignant neoplasm Diseases 0.000 claims 1
- 208000021039 metastatic melanoma Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
-
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/06—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
- C07D233/08—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms
- C07D233/10—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring nitrogen atoms
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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Claims (14)
1. Spoj Formule (IA):
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time što:
L1 je veza ili C1-C6alkil;
R1 je -OR9, -C1-C6alkil, C2-C6alkenil, C1-C6haloalkil, ili -C(=O)N(R9)2;
R2 je C1-C6alkil;
R3 je vodik;
R4 je fenil supstituiran sa najmanje jednim R11;
svaki R11 je neovisno -NR10SO2R10, -SOR10, -SO2R10, -SO2N(R10)2, ili C1-C6alkil, pri čemu je navedeni C1-C6alkil izborno supstituiran sa 1 hidroksi;
pod uvjetom da je najmanje jedan R11 -NR10SO2R10, -SOR10, -SO2R10, ili -SO2N(R10)2,
svaki R10 je neovisno C1-C6 alkil; i
svaki R9 je neovisno vodik ili C1-C6haloalkil; i
n je 0.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što je -L1-R1 -C(=CH2)CH3, izopropil, -C(=O)NHCH2CF3, -CF3, ili -C(CH3)2OH.
3. Spoj prema bilo kojem od patentnih zahtjeva 1-2, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R2 izobutil ili sek-butil.
4. Spoj prema patentnom zahtjevu 1, naznačen time što je:
(a) Spoj Formule (IB):
[image]
pri čemu:
R11a je -NR10SO2R10, -SOR10, -SO2R10, ili -SO2N(R10)2; i
m je 0 ili 1;
ili njegova farmaceutski prihvatljiva sol; ili
(b) Spoj Formule (IC):
[image]
pri čemu je m 0 ili 1;
ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što:
(a)
L1 je veza ili C1-C6alkil;
R1 je -OR9, -C1-C6alkil, C2-C6alkenil, C1-C6haloalkil, ili -C(=O)N(R9)2;
R2 je C1-C6alkil;
R3 je vodik;
R4 je fenil supstituiran sa jednim R11, pri čemu je R11 -SO2R10 i R10 je C1-C6 alkil; ili
R4 je fenil supstituiran sa dva R11, pri čemu je jedan R11 -SO2R10 i jedan R11 je izborno supstituiran C1-C6alkil;
svaki R9 je neovisno vodik ili C1-C6haloalkil; i
n je 0; ili
(b)
-L1-R1 je -C(=CH2)CH3, izopropil, -C(=O)NHCH2CF3, -CF3, ili -C(CH3)2OH;
R2 je izobutil ili sek-butil;
R3 je vodik;
R4 je fenil supstituiran sa dva R11, pri čemu je jedan R11 -SO2CH3 i jedan R11 je -CH2OH; ili R4 je fenil supstituiran sa jednim R11,pri čemu je R11 -SO2R10 i R10 je CH3; i
n je 0.
6. Spoj prema patentnom zahtjevu 1, odabran od:
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema patentnom zahtjevu 1, odabran od:
[image]
[image]
i
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentnom zahtjevu 1, odabran od:
[image]
ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj:
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj:
[image]
ili njegova farmaceutski prihvatljiva sol.
11. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj:
[image]
ili njegova farmaceutski prihvatljiva sol.
12. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj:
[image]
ili njegova farmaceutski prihvatljiva sol.
13. Farmaceutski pripravak koja sadrži spoj u skladu sa bilo kojim od patentnih zahtjeva 1-12, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv nosač.
14. Spoj prema bilo kojem od patentnih zahtjeva 1-12, ili njegova farmaceutski prihvatljiva sol, za uporabu u liječenju bolesti, poremećaja ili stanja kod sisavaca koji bi imali koristi od LXR modulacije naznačen time što je bolest, poremećaj ili stanje kod sisavaca:
(a) povećana razina lipida, povećana razina kolesterola, nizak HDL-kolesterol, visok LDL- kolesterol, aterosklerotske bolesti, dijabetes, dijabetes melitus koji nije ovisan od inzulina, metabolički sindrom, dislipidemija, sepsa, upalne bolesti, infektivne bolesti, kožne bolesti, kolitis, pankreatitis, kolestaza jetre, fibroza jetre, psorijaza, oslabljena kognitivna funkcija/kognitivna funkcija koja se može poboljšati, HIV, akutna makularna degeneracija, i oblici makularne degeneracije povezane sa starošću (vlažni i suhi oblici); ili
(b) rak uključujući metastatski rak; ili
(c) maligni melanom uključujući metastatski melanom; ili
(d) Alzheimerova bolest; ili
(e) Parkinsonova bolest.
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| US201361873755P | 2013-09-04 | 2013-09-04 | |
| EP14842802.2A EP3041835B1 (en) | 2013-09-04 | 2014-09-04 | Liver x receptor (lxr) modulators |
| PCT/US2014/054043 WO2015035015A1 (en) | 2013-09-04 | 2014-09-04 | Liver x receptor (lxr) modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20201054T1 true HRP20201054T1 (hr) | 2021-01-08 |
Family
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| HRP20201054TT HRP20201054T1 (hr) | 2013-09-04 | 2020-07-03 | Modulatori receptora x jetre (lxr) |
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| US (7) | US10047055B2 (hr) |
| EP (2) | EP3041835B1 (hr) |
| JP (2) | JP6806961B2 (hr) |
| KR (1) | KR102281803B1 (hr) |
| CN (2) | CN105658636B (hr) |
| AU (1) | AU2014315280B2 (hr) |
| BR (1) | BR112016004904B1 (hr) |
| CA (1) | CA2923175C (hr) |
| CY (1) | CY1124057T1 (hr) |
| DK (1) | DK3041835T3 (hr) |
| ES (1) | ES2804304T3 (hr) |
| HR (1) | HRP20201054T1 (hr) |
| HU (1) | HUE051094T2 (hr) |
| IL (1) | IL244418B (hr) |
| LT (1) | LT3041835T (hr) |
| MX (1) | MX371343B (hr) |
| NZ (1) | NZ717688A (hr) |
| PL (1) | PL3041835T3 (hr) |
| PT (1) | PT3041835T (hr) |
| RS (1) | RS60479B1 (hr) |
| SG (1) | SG11201601640SA (hr) |
| SI (1) | SI3041835T1 (hr) |
| WO (1) | WO2015035015A1 (hr) |
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| LT3041835T (lt) | 2013-09-04 | 2020-07-27 | Ellora Therapeutics, Inc. | Kepenų x receptoriaus (lxr) moduliatoriai |
| SG11201601644RA (en) | 2013-09-04 | 2016-04-28 | Alexar Therapeutics Inc | Liver x receptor (lxr) modulators |
| CN110305141B (zh) * | 2019-07-18 | 2022-01-11 | 深圳市三启药物开发有限公司 | 一种螺(3,3’-异丙基吡咯烷氧化吲哚)类肝x受体调节剂及其制备方法和应用 |
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-
2014
- 2014-09-04 LT LTEP14842802.2T patent/LT3041835T/lt unknown
- 2014-09-04 CN CN201480057481.8A patent/CN105658636B/zh active Active
- 2014-09-04 NZ NZ717688A patent/NZ717688A/en not_active IP Right Cessation
- 2014-09-04 DK DK14842802.2T patent/DK3041835T3/da active
- 2014-09-04 US US14/916,275 patent/US10047055B2/en active Active
- 2014-09-04 SG SG11201601640SA patent/SG11201601640SA/en unknown
- 2014-09-04 KR KR1020167008708A patent/KR102281803B1/ko active IP Right Grant
- 2014-09-04 ES ES14842802T patent/ES2804304T3/es active Active
- 2014-09-04 SI SI201431603T patent/SI3041835T1/sl unknown
- 2014-09-04 MX MX2016002931A patent/MX371343B/es active IP Right Grant
- 2014-09-04 EP EP14842802.2A patent/EP3041835B1/en active Active
- 2014-09-04 AU AU2014315280A patent/AU2014315280B2/en not_active Ceased
- 2014-09-04 RS RS20200783A patent/RS60479B1/sr unknown
- 2014-09-04 BR BR112016004904-7A patent/BR112016004904B1/pt active IP Right Grant
- 2014-09-04 PT PT148428022T patent/PT3041835T/pt unknown
- 2014-09-04 PL PL14842802T patent/PL3041835T3/pl unknown
- 2014-09-04 CN CN201811528469.7A patent/CN110003108A/zh active Pending
- 2014-09-04 JP JP2016540374A patent/JP6806961B2/ja active Active
- 2014-09-04 HU HUE14842802A patent/HUE051094T2/hu unknown
- 2014-09-04 EP EP19194067.5A patent/EP3626712A3/en not_active Withdrawn
- 2014-09-04 WO PCT/US2014/054043 patent/WO2015035015A1/en active Application Filing
- 2014-09-04 CA CA2923175A patent/CA2923175C/en not_active Expired - Fee Related
-
2016
- 2016-03-03 IL IL24441816A patent/IL244418B/en active IP Right Grant
-
2018
- 2018-08-03 US US16/054,884 patent/US10246419B2/en active Active
-
2019
- 2019-02-06 US US16/269,444 patent/US11034657B2/en active Active
- 2019-04-11 JP JP2019075449A patent/JP6821737B2/ja active Active
-
2020
- 2020-07-03 HR HRP20201054TT patent/HRP20201054T1/hr unknown
- 2020-07-06 CY CY20201100620T patent/CY1124057T1/el unknown
-
2021
- 2021-05-07 US US17/315,035 patent/US20210269406A1/en not_active Abandoned
- 2021-12-15 US US17/552,287 patent/US20220106274A1/en not_active Abandoned
-
2022
- 2022-07-28 US US17/876,354 patent/US20220388963A1/en not_active Abandoned
-
2023
- 2023-03-09 US US18/181,451 patent/US20230212127A1/en not_active Abandoned
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