HRP20171807T1 - Spojevi policikličkog karbamoilpiridona i njihova uporaba za liječenje hiv infekcija - Google Patents
Spojevi policikličkog karbamoilpiridona i njihova uporaba za liječenje hiv infekcija Download PDFInfo
- Publication number
- HRP20171807T1 HRP20171807T1 HRP20171807TT HRP20171807T HRP20171807T1 HR P20171807 T1 HRP20171807 T1 HR P20171807T1 HR P20171807T T HRP20171807T T HR P20171807TT HR P20171807 T HRP20171807 T HR P20171807T HR P20171807 T1 HRP20171807 T1 HR P20171807T1
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- Prior art keywords
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- compound according
- hydrogen
- alkyl
- following formula
- Prior art date
Links
- 208000031886 HIV Infections Diseases 0.000 title claims 4
- 150000001875 compounds Chemical class 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- -1 2,3-difluorophenyl Chemical group 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 3
- 208000037357 HIV infectious disease Diseases 0.000 claims 3
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 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
- A61K31/495—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D471/12—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 three hetero rings
- C07D471/18—Bridged systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
Claims (14)
1. Spoj koji ima slijedeću Formulu (I):
[image]
ili stereoizomer ili njegova farmaceutski prihvatljiva sol,
naznačen time da:
Y1 i Y2 su svaki, neovisno, vodik, C1-3alkil ili C1-3haloalkil;
R1 je fenil supstituiran s jednim do tri halogena;
X je -CHR2-;
W je veza ili -CHR3-;
Z je veza ili -CHR4-;
R2, R3, i R4 su svaki, neovisno, vodik ili C1-3alkil;
R5 je vodik, C1-3alkil ili C1-3haloalkil;
L je -C(Ra)2-, -C(Ra)2C(Ra)2- ili -C(Ra)2C(Ra)2C(Ra)2-; i
svaki Ra je, neovisno, vodik, halo, hidroksi ili C1-4alkil.
2. Spoj prema zahtjevu 1 koji ima slijedeću Formulu (I-A):
[image]
ili stereoizomer ili njegova farmaceutski prihvatljiva sol,
naznačen time da:
Y1 i Y2 su svaki, neovisno, vodik, C1-3alkil ili C1-3haloalkil;
R1 je fenil supstituiran s jednim do tri halogena;
X je -CHR2-;
W je veza ili -CHR3-;
Z je veza ili -CHR4-;
R2, R3, i R4 su svaki, neovisno, vodik ili C1-3alkil;
L je -C(Ra)2-, -C(Ra)2C(Ra)2- ili -C(Ra)2C(Ra)2C(Ra)2-; i
svaki Ra je, neovisno, vodik, halo, hidroksi ili C1-4alkil.
3. Spoj prema zahtjevu 1 naznačen time da ima slijedeću Formulu (II):
[image]
proizvoljno ima slijedeću Formulu (II-A):
[image]
4. Spoj prema zahtjevu 1 naznačen time da ima slijedeću Formulu (III):
[image]
proizvoljno ima slijedeću Formulu (III-A):
[image]
5. Spoj prema zahtjevu 1 naznačen time da ima slijedeću Formulu (IV):
[image]
proizvoljno ima slijedeću Formulu (IV-A):
[image]
6. Spoj prema bilo kojem od zahtjeva 1-5, naznačen time da je L -C(Ra)2-, ili -C(Ra)2C(Ra)2-, ili -C(Ra)2C(Ra)2C(Ra)2-.
7. Spoj prema bilo kojem od zahtjeva 1-6 naznačen time da svaki Ra je vodik.
8. Spoj prema bilo kojem od zahtjeva 1-7 naznačen time da R1 je supstituiran s
i) jednim halogenom, proizvoljno pri čemu R1 je 4-fluorofenil ili 2-fluorofenil; ili
ii) dva halogena, proizvoljno pri čemu R1 je 2,4-difluorofenil, 2,3-difluorofenil, 2,6-difluorofenil, 3-fluoro-4-klorofenil, 3,4-difluorofenil, 2-fluoro-3-klorofenil, 2-fluoro-4-klorofenil, ili 3,5-difluorofenil, proizvoljno pri čemu R1 je 2,4-difluorofenil; ili
iii) tri halogena, proizvoljno pri čemu R1 je 2,4,6-trifluorofenil li 2,3,4-trifluorofenil, proizvoljno pri čemu R1 je 2,4,6-trifluorofenil.
9. Spoj prema zahtjevu 1 naznačen time da R5 je i) vodik ili C1-3alkil, ili ii) vodik, ili iii) metil.
10. Spoj prema zahtjevu 1 naznačen time da se bira od:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
i
[image]
11. Farmaceutski pripravak naznačen time da sadrži spoj prema bilo kojem od zahtjeva 1-10, ili stereoizomer ili njegovu farmaceutski prihvatljivu sol, te farmaceutski prihvatljiv nosač, sredstvo za raspadanje ili pomoćno sredstvo.
12. Spoj prema bilo kojem od zahtjeva 1-10 ili farmaceutski pripravak prema zahtjevu 14 naznačen time da je za uporabu u postupku liječenja ili sprječavanja HIV infekcije kod ljudi koji imaju HIV infekciju ili imaju rizik od dobivanja infekcije, navedeni postupak obuhvaća davanje čovjeku terapeutski učinkovite količine spoja prema bilo kojem od zahtjeva 1-10 ili farmaceutsko pripravka prema zahtjevu 11.
13. Spoj kao što je opisano prema bilo kojem od zahtjeva 1-10, ili njegova farmaceutski prihvatljiva sol naznačen time da je za uporabu u medicinskoj terapiji.
14. Spoj kao što je opisano prema bilo kojem od zahtjeva 1-10, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za uporabu u profilaktičkom ili terapeutskom liječenju HIV infekcije.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361845807P | 2013-07-12 | 2013-07-12 | |
| EP14745053.0A EP3019499B1 (en) | 2013-07-12 | 2014-07-11 | Polycyclic-carbamoylpyridone compounds and their use for the treatment of hiv infections |
| PCT/US2014/046415 WO2015006733A1 (en) | 2013-07-12 | 2014-07-11 | Polycyclic-carbamoylpyridone compounds and their use for the treatment of hiv infections |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20171807T1 true HRP20171807T1 (hr) | 2018-01-26 |
Family
ID=51257630
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20171807TT HRP20171807T1 (hr) | 2013-07-12 | 2017-11-21 | Spojevi policikličkog karbamoilpiridona i njihova uporaba za liječenje hiv infekcija |
Country Status (18)
| Country | Link |
|---|---|
| US (5) | US9458159B2 (hr) |
| EP (2) | EP3019499B1 (hr) |
| JP (1) | JP6411492B2 (hr) |
| AU (3) | AU2014286995B2 (hr) |
| CA (1) | CA2918055C (hr) |
| CY (1) | CY1119545T1 (hr) |
| DK (1) | DK3019499T3 (hr) |
| ES (2) | ES2647216T3 (hr) |
| HK (2) | HK1246295A1 (hr) |
| HR (1) | HRP20171807T1 (hr) |
| HU (1) | HUE037343T2 (hr) |
| LT (1) | LT3019499T (hr) |
| NO (1) | NO2865735T3 (hr) |
| PL (1) | PL3019499T3 (hr) |
| PT (1) | PT3019499T (hr) |
| RS (1) | RS56539B1 (hr) |
| SI (2) | SI3252053T1 (hr) |
| WO (1) | WO2015006733A1 (hr) |
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| KR102527797B1 (ko) | 2012-12-21 | 2023-05-03 | 길리애드 사이언시즈, 인코포레이티드 | 폴리시클릭-카르바모일피리돈 화합물 및 그의 제약 용도 |
| CA2916993C (en) * | 2013-07-12 | 2019-01-15 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| NO2865735T3 (hr) | 2013-07-12 | 2018-07-21 | ||
| EP3196201B1 (en) | 2014-08-22 | 2021-04-28 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative having integrase-inhibiting activity |
| CN107108615B (zh) | 2015-03-04 | 2020-11-20 | 吉利德科学公司 | Toll样受体调节性4,6-二氨基-吡啶并[3,2-D]嘧啶化合物 |
| AU2016244035B2 (en) * | 2015-04-02 | 2018-11-01 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| US20210292327A1 (en) | 2015-08-26 | 2021-09-23 | Gilead Sciences, Inc. | Deuterated toll-like receptor modulators |
| MA42818A (fr) | 2015-09-15 | 2018-07-25 | Gilead Sciences Inc | Modulateurs de récepteurs de type toll pour le traitement du vih |
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