ME03800B - Heteroaril amidi kao inhibitori proteinske agregacije - Google Patents
Heteroaril amidi kao inhibitori proteinske agregacijeInfo
- Publication number
- ME03800B ME03800B MEP-2020-148A MEP2020148A ME03800B ME 03800 B ME03800 B ME 03800B ME P2020148 A MEP2020148 A ME P2020148A ME 03800 B ME03800 B ME 03800B
- Authority
- ME
- Montenegro
- Prior art keywords
- acceptable salt
- pharmaceutically acceptable
- nitrogen
- substituted
- attached form
- Prior art date
Links
- 230000004845 protein aggregation Effects 0.000 title claims 3
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 17
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 15
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 10
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 3
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims 2
- 201000002832 Lewy body dementia Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- -1 chloro, bromo, methyl Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005842 heteroatom Chemical group 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
- 239000000203 mixture Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 125000006413 ring segment Chemical group 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
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims 2
- NDOVLWQBFFJETK-UHFFFAOYSA-N 1,4-thiazinane 1,1-dioxide Chemical compound O=S1(=O)CCNCC1 NDOVLWQBFFJETK-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000009829 Lewy Body Disease Diseases 0.000 claims 1
- 208000001089 Multiple system atrophy Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- XYOVOXDWRFGKEX-UHFFFAOYSA-N azepine Chemical compound N1C=CC=CC=C1 XYOVOXDWRFGKEX-UHFFFAOYSA-N 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000002452 interceptive effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 230000006919 peptide aggregation Effects 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
- A61K31/41—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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles 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
- A61K31/495—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
- A61K31/535—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- A—HUMAN NECESSITIES
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (17)
1. Jedinjenje sa formulom (1): gde:R1 je H, halo, C1-4alkil, ili CF3;R2 je -CF3, ili C1-4alkil nesupstituisan ili supstituisan sa halo ili -CF3;A je 5- člani heteroaril prsten; Y je odsutno ili je C1-4alkilen; gde Y je odsutno:R3 i R4 zajedno sa azotom za koji su vezani formiraju monociklicni heterocikloalkil prsten, nesupstituisan iii supstituisan sa C1-4alkilom; igde Y je C1-4alkilen:R3 i R4 zajedno sa azotom za koji su vezani formiraju monociklicni heterocikloalkil prsten, nesupstituisan ili supstituisan sa C1-4alkilom; iliR3 i Y zajedno sa azotom za koji R3 je vezan formiraju monociklicni heterocikloalkil prsten, i R4 je H ili C1-4alkil;ili farmaceutski prihvatljiva so istog.
2. Jedinjenje u skladu sa patentnim zahtevom 1, ili farmaceutski prihvatljiva so istog, gde: R1 je H, fluoro, hloro, bromo, metil, etil, propil, izopropil, butil, izobutil, sek-butil, ili terc-butil; ili R1 je H ili fluoro.
3. Jedinjenje u sldadu sa patentnim zahtevom 1 ili 2, ili fannaceutski prihvatljiva so istog, gde: R2 je -CF3; iii R2 je metil, etil, propil, izopropil, butil, izobutil, sek-butil, ili terc-butil, svaki nesupstituisan ili supstituisan sa fluoro, hloro, bromo, ili -CF3; ili R2 je C1-4alkil po izboru supstituisan sa halo ili -CF3; ili R2 je C3-4alkil, nesupstituisan iii supstituisan sa fluoro ili -CF3; ili R2 je butil; ili R2 je propil supstituisan sa -CF3.
4. Jedinjenje u sldadu sa bilo kojim od patentnih zahteva 1 do 3, ili fannaceutski prihvatljiva so istog, gde: A je 5- člani heteroaril prsten sa dva ili tri atoma prstena koja su heteroatomi; ili A je 5- člani heteroaril prsten sa dva nesusedna atoma prstena koja su heteroatomi; ili A je tiazol, tiadiazol, oksazol, imidazol, ili triazol; ili A je tiazol iii tiadiazol; ili A je tiazol.
5. Jedinjenje u sldadu sa bilo kojim od patentnog zahteva 1 do 4, ili fannaceutski prihvatljiva so istog, gde: Y je odsutno; ili Y je -CH2-, -CH2CH2-, -CH(CH3)-, -(CH2)3-, -C(CH3)2-, -(CH2)4-, -CH((CH2)2CH3)-, - CH(CH(CH3)2)-, -CH(CH2CH3)CH2-, -CH(CH3)CH(CH3)-, -CH(CH3)(CH2)2-, ili - CH2CH(CH3)CH2-; ili Y je -CH2-, -CH2CH2-, ili -CH(CH3)-; ili Y je -CH2CH2-.
6. Jedinjenje u skladu sa bilo kojim od patentnog zahteva 1 do 5, ili fannaceutski prihvatljiva so istog, gde: R3 i R4 su zajedno sa azotom za koji su vezani formiraju monocikli ni heterocikloalkil prsten, nesupstituisan ili supstituisan sa C1-4alkilom; ili R3 i R4 zajedno sa azotom za koji su vezani formiraju azetidin, pirolidipiperidin, azepin, piperazin, morfolin, tiomorfoliii 1,1-diokso-tiomorfolin, svaki nesupstituisan ili supstituisan sa C1-4alkilom; ili R3 i R4 zajedno sa azotom za koji su vezani formiraju piperazin, morfolin, ili pirolidin, svaki nesupstituisan ili supstituisan sa C1-4alkilom; ili R3 i R4 zajedno sa azotom za koji su vezani formiraju piperazin ili morfolin, svaki nesupstituisan ili supstituisan sa C1-4alkilom; ili R3 i R4 zajedno sa azotom za koji su vezani formiraju piperazin, nesupstituisan ili supstituisan sa C1-4alkilom; ili R3 i R4 zajedno sa azotom za koji su vezani formiraju piperazin ili 4-metil-piperazin.
7. Jedinjenje u skladu sa bilo kojim od patentnog zahteva 1 do 5, ili farmaceutski prihvatljiva so istog, gde: Y je C1-4alkilen, R3 i Y zajedno sa azotom za koji R3 je vezan formiraju monociklični heterocikloalkil prsten, i R4 je H ili C1-4alkil; ili Y je C1-4alkilen, R3 i Y zajedno sa azotom za koji R3 je vezan formiraju pirolidin ili piperidin.
8. Jedinjenje u skladu sa patentnim zahtevom 7, iii farmaceutski prihvatljiva so istog, gde: R4 je H ili metil.
9. Jedinjenje u skladu sa patentnim zahtevom 1, ili farmaceutski prihvatljiva so istog, gde: R1 je H, R2 je C1-4alkil, A je tiazol, Y je odsutno ili je etilen, i R3 i R4 zajedno sa azotom za koji su vezani formiraju N-metilpiperazin.
10. Jedinjenje u skladu sa bilo kojim od patentnog zahteva 1 do 9, ili farmaceutski prihvatljiva so istog, gde: R2 je u "R" stereohemijskoj konfiguraciji; ili R2 je u "S" stereohemijskoj konfiguraciji.
11. Jedinjenje u skladu sa patentnim zahtevom 1, odabrano od jedinjenja sa sledećim formulama, ili farmaceutski prihvatljiva so istog:
12. Jedinjenje u skladu sa patentnim zahtevom 1, odabrano od jedinjenja sa sledećim formulama, ili farmaceutski prihvatljiva so istog:
13. Farmaceutska kompozicija koja saddi (a) najmanje jedno jedinjenje ili farmaceutski prihvatljivu so istog u skladu sa bilo kojim od patentnih zahteva 1 do 12, i (b) farmaceutski prihvatljiv ekscipijens.
14. Fannaceutska kompozicija koja sadrži (a) najmanje jedno jedinjenje ili fannaceutski prihvatljivu so istog u skladu sa bilo kojim od patentnih zahteva 1 do 12, i (b) fannaceutski prihvatljiv ekscipijens gde R2 je u suštini u "R" ili u suštini u "S" stereohemijskoj konfiguraciji.
15. Jedinjenje iii fannaceutski prihvatljiva so u skladu sa bilo kojim od patentnih zahteva 1 do 12 ili fannaceutska kompozicija u skladu sa patentnim zahtevom 13 ili 14 za primenu u lečenju bolesti ili medicinskog stanja koje je u vezi sa proteinskom agregacijom.
16. Jedinjenje, fannaceutski prihvatljiva so, ili fannaceutska kompozicija za primenu u skladu sa patentnim zahtevom 15, gde je bolest ili medicinsko stanje Alchajmerova bolest, Parkinsonova bolest, fronto-temporalna demencija, demencija sa Levijevim telima (bolest Levijevih tela), Parkinsonova bolest sa demencijom, multipla sistemska atrofija, amiotrofi na lateralna skleroza, Huntington-ova bolest, kancer, melanom, ili inflamatoma bolest.
17. Metoda interferencije sa akumulacijom proteinskih ili peptidnih agregata u ćeliji, ili sprečavanja, usporavanja, preusmeravanja, ili inhibiranja proteinske ili peptidne agregacije u ćeliji, koja obuhvata stupanje u kontakt ćelije sa efikasnom količinom najmanje jednog jedinjenja ili fannaceutski prihvatljive soli u skladu sa bilo kojim od patentnih zahteva 1 do 12 ili farmaceutske kompozicije u sktadu sa patentnim zahtevom l3 ili 14, gde je stupanje u kontakt in vitro ili ex vivo
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461933246P | 2014-01-29 | 2014-01-29 | |
| US201462078895P | 2014-11-12 | 2014-11-12 | |
| EP18156929.4A EP3348556B1 (en) | 2014-01-29 | 2015-01-28 | Heteroaryl amides as inhibitors of protein aggregation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME03800B true ME03800B (me) | 2021-04-20 |
Family
ID=52484559
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2020-148A ME03800B (me) | 2014-01-29 | 2015-01-28 | Heteroaril amidi kao inhibitori proteinske agregacije |
Country Status (38)
| Country | Link |
|---|---|
| US (3) | US9738635B2 (me) |
| EP (2) | EP3099684B8 (me) |
| JP (2) | JP6619741B2 (me) |
| KR (1) | KR102383038B1 (me) |
| CN (2) | CN111039939B (me) |
| AP (1) | AP2016009347A0 (me) |
| AU (1) | AU2015211119B2 (me) |
| BR (2) | BR112016017344B1 (me) |
| CA (1) | CA2937967C (me) |
| CL (1) | CL2016001918A1 (me) |
| CR (1) | CR20160394A (me) |
| CY (2) | CY1120348T1 (me) |
| DK (2) | DK3099684T3 (me) |
| EA (1) | EA032374B1 (me) |
| EC (1) | ECSP16070327A (me) |
| ES (2) | ES2808978T3 (me) |
| HK (1) | HK1231470A1 (me) |
| HR (2) | HRP20180813T1 (me) |
| HU (2) | HUE040274T2 (me) |
| IL (1) | IL246987B (me) |
| LT (2) | LT3099684T (me) |
| ME (1) | ME03800B (me) |
| MX (1) | MX2016009896A (me) |
| MY (1) | MY187450A (me) |
| NZ (1) | NZ722487A (me) |
| PE (1) | PE20161393A1 (me) |
| PH (1) | PH12016501493B1 (me) |
| PL (2) | PL3348556T3 (me) |
| PT (2) | PT3099684T (me) |
| RS (2) | RS60547B1 (me) |
| SA (1) | SA516371579B1 (me) |
| SG (1) | SG11201606108RA (me) |
| SI (2) | SI3099684T1 (me) |
| SM (2) | SMT201800318T1 (me) |
| TR (1) | TR201809440T4 (me) |
| UA (1) | UA118209C2 (me) |
| WO (1) | WO2015116663A1 (me) |
| ZA (1) | ZA201605246B (me) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SMT201800318T1 (it) | 2014-01-29 | 2018-07-17 | Ucb Biopharma Sprl | Eteroarilammidi come inibitori dell'aggregazione proteica |
| WO2017020010A1 (en) | 2015-07-29 | 2017-02-02 | Neuropore Therapies, Inc. | Bis-heteroaryl derivatives as modulators of protein aggregation |
| CN106474121B (zh) * | 2016-11-25 | 2017-10-10 | 刘淑兰 | 一种治疗慢性盆腔炎的药物 |
| EP3824906A1 (en) | 2016-12-21 | 2021-05-26 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| US11091474B2 (en) * | 2017-01-26 | 2021-08-17 | UCB Biopharma SRL | Alkoxy bis-heteroaryl derivatives as modulators of protein aggregation |
| BR112019011932A2 (pt) | 2017-01-26 | 2019-10-29 | Ucb Biopharma Sprl | derivados de bis-heteroarila como moduladores da agregação de proteína |
| CA3045221A1 (en) * | 2017-01-26 | 2018-08-02 | Ucb Biopharma Sprl | Bicyclic bis-heteroaryl derivatives as modulators of protein aggregation |
| US11180518B2 (en) * | 2017-05-12 | 2021-11-23 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Phenyl-heterocycle-phenyl derivatives for use in the treatment or prevention of melanoma |
| JP2020529432A (ja) * | 2017-08-04 | 2020-10-08 | アキシャル バイオセラピューティクス, インク.Axial Biotherapeutics, Inc. | 微生物により誘発されるアミロイドの阻害剤 |
| US20200254068A1 (en) * | 2017-10-31 | 2020-08-13 | Loma Linda University | Methods for treating traumatic brain injury |
| WO2020041331A1 (en) | 2018-08-20 | 2020-02-27 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| EP4458824A4 (en) * | 2021-12-27 | 2025-12-24 | Shanghai Jingxin Biomedical Co Ltd | Fused bicyclic heteroarylamide compound useful as a protein aggregation inhibitor |
| GB202213796D0 (en) * | 2022-09-21 | 2022-11-02 | Wista Lab Ltd | Tau aggregation inhibitors |
| EP4611895A1 (en) * | 2022-11-02 | 2025-09-10 | AC Immune SA | Novel compounds for the diagnosis of tdp-43 proteinopathies |
| WO2024184179A1 (en) | 2023-03-06 | 2024-09-12 | UCB Biopharma SRL | Minzasolmin for use in the treatment of parkinson's disease |
| WO2024184180A1 (en) | 2023-03-06 | 2024-09-12 | UCB Biopharma SRL | Minzasolmin for use in the treatment of parkinson's disease |
| WO2025002040A1 (zh) * | 2023-06-25 | 2025-01-02 | 上海京新生物医药有限公司 | 双环杂芳基酰胺化合物的晶型及盐、制备方法和用途 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997023202A1 (en) * | 1995-12-22 | 1997-07-03 | STATE OF OREGON, acting by and through THE OREGON STATE BOARD OF HIGHER EDUCATION, acting for and on behalf of THE OREGON HEALTH SCIENCES UNIVERSITYA ND THE UNIVERSITY OF OREGON, EUGENE OREGON | Subtype-selective nmda receptor ligands and the use thereof |
| EA200500721A1 (ru) * | 2002-11-28 | 2005-12-29 | Шеринг Акциенгезельшафт | Пиримидины, ингибирующие chk, pdk и акт, их получение и применение в качестве лекарственных средств |
| CN101385722A (zh) * | 2003-02-27 | 2009-03-18 | 乔安妮·麦克劳林 | 预防、治疗和诊断蛋白聚集疾病的方法 |
| TW200528455A (en) * | 2003-12-19 | 2005-09-01 | Bristol Myers Squibb Co | Azabicyclic heterocycles as cannabinoid receptor modulators |
| AU2004309368A1 (en) * | 2003-12-19 | 2005-07-14 | Bristol-Myers Squibb Company | Azabicyclic heterocycles as cannabinoid receptor modulators |
| KR20070018824A (ko) * | 2003-12-19 | 2007-02-14 | 브리스톨-마이어스 스큅 컴퍼니 | 카나비노이드 수용체 조절제인 아자비사이클릭헤테로사이클 |
| PT1786785E (pt) * | 2004-08-26 | 2010-05-21 | Pfizer | Compostos amino-heteroarilo enantiomericamente puros como inibidores da proteína quinase |
| EA012607B1 (ru) * | 2004-09-20 | 2009-10-30 | 4Сц Аг | НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB |
| SE0403119D0 (sv) * | 2004-12-21 | 2004-12-21 | Astrazeneca Ab | Therapeutic agents |
| BRPI0615524A2 (pt) * | 2005-07-11 | 2010-04-06 | Devgen Nv | derivados da amida como inibidores da quinase |
| BRPI0614188A2 (pt) * | 2005-07-29 | 2011-03-15 | 4Sc Ag | compostos inibidores heterocìclicos de nf-kappab, uso dos mesmos e composição farmacêutica |
| KR20080104147A (ko) * | 2006-03-15 | 2008-12-01 | 4에스체 악티엔게젤샤프트 | 신규의 헤테로환 ＮＦ-κＢ 억제제 |
| EP2081892A4 (en) * | 2006-11-17 | 2014-03-05 | Donald F Weaver | COMPOUNDS AND METHOD FOR THE TREATMENT OF PROTEIN DISAPPEARANCE |
| US8450481B2 (en) * | 2007-06-14 | 2013-05-28 | The Regents Of The University Of California | Compounds for inhibiting protein aggregation, and methods for making and using them |
| WO2010068452A1 (en) * | 2008-11-25 | 2010-06-17 | Janssen Pharmaceutica Nv | Heteroaryl-substituted urea modulators of fatty acid amide hydrolase |
| GB0910003D0 (en) * | 2009-06-11 | 2009-07-22 | Univ Leuven Kath | Novel compounds for the treatment of neurodegenerative diseases |
| WO2011048525A1 (en) * | 2009-10-20 | 2011-04-28 | Pfizer Inc. | Novel heteroaryl imidazoles and heteroaryl triazoles as gamma-secretase modulators |
| KR20120112548A (ko) * | 2009-12-16 | 2012-10-11 | 뉴로포레 테라피스, 인코포레이티드 | 시누클레인 병을 치료하는데 적합한 화합물 |
| GB201021103D0 (en) | 2010-12-13 | 2011-01-26 | Univ Leuven Kath | New compounds for the treatment of neurodegenerative diseases |
| WO2013134371A1 (en) | 2012-03-06 | 2013-09-12 | Neuropore Therapies, Inc. | Methods and compounds to be used in the treatment of neurodegenerative diseases |
| MX2014011615A (es) | 2012-03-28 | 2015-01-19 | Neuropore Therapies Inc | Derivados de fenil-urea y fenil-carbamato como inhibidores de agregacion de proteina. |
| KR20150031481A (ko) | 2012-07-16 | 2015-03-24 | 뉴로포레 테라피스, 인코포레이티드 | 단백질 응집 저해제로서의 디- 및 트리-헤테로아릴 유도체 |
| SMT201800318T1 (it) | 2014-01-29 | 2018-07-17 | Ucb Biopharma Sprl | Eteroarilammidi come inibitori dell'aggregazione proteica |
| WO2017020010A1 (en) | 2015-07-29 | 2017-02-02 | Neuropore Therapies, Inc. | Bis-heteroaryl derivatives as modulators of protein aggregation |
| BR112019011932A2 (pt) | 2017-01-26 | 2019-10-29 | Ucb Biopharma Sprl | derivados de bis-heteroarila como moduladores da agregação de proteína |
| CA3045221A1 (en) | 2017-01-26 | 2018-08-02 | Ucb Biopharma Sprl | Bicyclic bis-heteroaryl derivatives as modulators of protein aggregation |
-
2015
- 2015-01-28 SM SM20180318T patent/SMT201800318T1/it unknown
- 2015-01-28 EP EP15705417.2A patent/EP3099684B8/en active Active
- 2015-01-28 PL PL18156929T patent/PL3348556T3/pl unknown
- 2015-01-28 BR BR112016017344-9A patent/BR112016017344B1/pt active IP Right Grant
- 2015-01-28 HR HRP20180813TT patent/HRP20180813T1/hr unknown
- 2015-01-28 EP EP18156929.4A patent/EP3348556B1/en active Active
- 2015-01-28 CR CR20160394A patent/CR20160394A/es unknown
- 2015-01-28 NZ NZ722487A patent/NZ722487A/en unknown
- 2015-01-28 PT PT15705417T patent/PT3099684T/pt unknown
- 2015-01-28 SI SI201530252T patent/SI3099684T1/en unknown
- 2015-01-28 CN CN201911278647.XA patent/CN111039939B/zh active Active
- 2015-01-28 MY MYPI2016001401A patent/MY187450A/en unknown
- 2015-01-28 AU AU2015211119A patent/AU2015211119B2/en active Active
- 2015-01-28 AP AP2016009347A patent/AP2016009347A0/en unknown
- 2015-01-28 ES ES18156929T patent/ES2808978T3/es active Active
- 2015-01-28 HU HUE15705417A patent/HUE040274T2/hu unknown
- 2015-01-28 RS RS20200827A patent/RS60547B1/sr unknown
- 2015-01-28 HK HK17105014.2A patent/HK1231470A1/zh unknown
- 2015-01-28 HU HUE18156929A patent/HUE050964T2/hu unknown
- 2015-01-28 BR BR122018001892-5A patent/BR122018001892B1/pt active IP Right Grant
- 2015-01-28 ES ES15705417.2T patent/ES2675301T3/es active Active
- 2015-01-28 SM SM20200376T patent/SMT202000376T1/it unknown
- 2015-01-28 UA UAA201609003A patent/UA118209C2/uk unknown
- 2015-01-28 DK DK15705417.2T patent/DK3099684T3/en active
- 2015-01-28 MX MX2016009896A patent/MX2016009896A/es active IP Right Grant
- 2015-01-28 EA EA201691529A patent/EA032374B1/ru unknown
- 2015-01-28 SI SI201531297T patent/SI3348556T1/sl unknown
- 2015-01-28 LT LTEP15705417.2T patent/LT3099684T/lt unknown
- 2015-01-28 RS RS20180644A patent/RS57533B1/sr unknown
- 2015-01-28 PE PE2016001285A patent/PE20161393A1/es unknown
- 2015-01-28 JP JP2016549488A patent/JP6619741B2/ja active Active
- 2015-01-28 DK DK18156929.4T patent/DK3348556T3/da active
- 2015-01-28 PL PL15705417T patent/PL3099684T3/pl unknown
- 2015-01-28 KR KR1020167023810A patent/KR102383038B1/ko active Active
- 2015-01-28 CA CA2937967A patent/CA2937967C/en active Active
- 2015-01-28 WO PCT/US2015/013263 patent/WO2015116663A1/en not_active Ceased
- 2015-01-28 LT LTEP18156929.4T patent/LT3348556T/lt unknown
- 2015-01-28 TR TR2018/09440T patent/TR201809440T4/tr unknown
- 2015-01-28 PT PT181569294T patent/PT3348556T/pt unknown
- 2015-01-28 ME MEP-2020-148A patent/ME03800B/me unknown
- 2015-01-28 SG SG11201606108RA patent/SG11201606108RA/en unknown
- 2015-01-28 CN CN201580017216.1A patent/CN106132960B/zh active Active
- 2015-12-29 US US14/983,243 patent/US9738635B2/en active Active
-
2016
- 2016-07-27 IL IL246987A patent/IL246987B/en unknown
- 2016-07-28 PH PH12016501493A patent/PH12016501493B1/en unknown
- 2016-07-28 CL CL2016001918A patent/CL2016001918A1/es unknown
- 2016-07-28 SA SA516371579A patent/SA516371579B1/ar unknown
- 2016-07-28 ZA ZA2016/05246A patent/ZA201605246B/en unknown
- 2016-08-29 EC ECIEPI201670327A patent/ECSP16070327A/es unknown
-
2017
- 2017-08-01 US US15/666,503 patent/US10358443B2/en active Active
-
2018
- 2018-06-15 CY CY20181100630T patent/CY1120348T1/el unknown
-
2019
- 2019-06-04 JP JP2019104159A patent/JP6783900B2/ja active Active
- 2019-06-11 US US16/438,348 patent/US11078196B2/en active Active
-
2020
- 2020-07-14 HR HRP20201107TT patent/HRP20201107T8/hr unknown
- 2020-07-24 CY CY20201100682T patent/CY1123374T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20201107T1 (hr) | Heteroaril amidi kao inhibitori proteinske agregacije | |
| RU2500680C2 (ru) | Новые замещенные пиридин-2-оны и пиридазин-3-оны | |
| JP2017505779A5 (me) | ||
| ZA202006378B (en) | N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, pharmaceutical composition thereof, and use thereof | |
| NZ627750A (en) | Carbamate compounds and of making and using same | |
| TN2014000436A1 (en) | Inhibitors of platelet aggregation | |
| DK2966079T1 (da) | Pyridopyrimidin eller pyrimidopyrimidinforbindelse, fremstillingsmetode, pharmaceutisk præparat og anvendelse heraf | |
| ME02892B (me) | Hemijska jedinjenja | |
| MX2021003739A (es) | Derivados de quinolino-pirrolidin-2-ona como inhibidores del gen mutado de ataxia telangiectasia (atm) y el uso de los mismos en el tratamiento de tumores sólidos. | |
| JP2015523383A5 (me) | ||
| UA109421C2 (uk) | Фармацевтична композиція, яка містить ліганди сигма-рецептора | |
| MX2010005824A (es) | Derivados de aminotiazol. | |
| PE20141167A1 (es) | Piridopirazinas sustituidas como inhibidores novedosos de ptk | |
| MY172534A (en) | Polymorphic forms of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-ylthio)acetic acid and uses thereof | |
| EA201101398A1 (ru) | Замещенные пиперидины в качестве антагонистов ccr3 | |
| AR091857A1 (es) | INHIBIDORES DE CISTATIONIN-g-LIASA (CSE) | |
| SE0400284D0 (sv) | Novel compounds | |
| BR112013031121A2 (pt) | composto de acordo com a fórmula i a v, ou um sal farmaceuticamente aceitável, solvato, polimorfo, ou pró-droga do mesmo; composto; polimorfo de sal cloridrato de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h-pirrol-3-il)tiazol-2-il)acetamida (fórmula i); ingrediente ativo constituído do mesmo; composição farmacêutica; polimorfo de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)1h-pirrol-3-il)tiazol-2-il)fenil)acetamida (fórmula i); ingrediente ativo constituído do mesmo; uso de um composto ou sal farmaceuticamente aceitável, solvato, polimorfo ou pró-droga do mesmo e uso de um polimorfo ou ingrediente ativo de sal cloridrato de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h-pirrol-3-il)tiazol-2il)tiazol-2-il)fenil)acetamida (fórmula i) e uso de um polimorfo ou ingrediente ativo de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h1pirrol-3-il)tiazol-2-il)fenil)acetamida(fórmula i) na fabricação de um medicamento | |
| SI3102573T1 (en) | SUBSTITUTED TIAZOL OR OXASOL AS ANTAGONISTS OF THE RECEPTOR P2X7 | |
| MX2014007878A (es) | Formulaciones de (+) - 2 - [1 - (3 - etoxi - 4 - metoxi - fenil) - 2 - metansulfonil - etil] - 4 - acetil aminoisoindolin - 1, 3 - diona. | |
| MX2010001020A (es) | Derivados de pirimidina utiles para el tratamiento de condiciones inflamatorias o alergicas. | |
| AR073117A1 (es) | Derivado de aminometil-fenil-piperidin-1-il-indolil-metanona, inhibidores de la triptasa de mastocitos, composiciones farmaceuticas que lo contienen, metodo de preparacion, compuestos intermediarios y uso del compuesto en el tratamiento de procesos inflamatorios. | |
| MX2018001925A (es) | Composiciones que comprenden compuestos triciclicos heterociclicos. | |
| BR112022001922A2 (pt) | Compostos de heteroarila de anel fundido como inibidores de ripk1 | |
| GEP20135959B (en) | Aryl piperazine and their usage as alpha2c antagonists |