HRP20201416T1 - Terapeutska sredstva na bazi sintetaze lantionin c-sličan 2 - Google Patents
Terapeutska sredstva na bazi sintetaze lantionin c-sličan 2 Download PDFInfo
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- HRP20201416T1 HRP20201416T1 HRP20201416TT HRP20201416T HRP20201416T1 HR P20201416 T1 HRP20201416 T1 HR P20201416T1 HR P20201416T T HRP20201416T T HR P20201416TT HR P20201416 T HRP20201416 T HR P20201416T HR P20201416 T1 HRP20201416 T1 HR P20201416T1
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- Prior art keywords
- diyl
- alkyl
- compound
- diamine
- disease
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- 102000008652 Lanthionine synthetase C-like Human genes 0.000 title 1
- 108050000440 Lanthionine synthetase C-like Proteins 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 15
- -1 piperazine-1,4-diyl Chemical group 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 4
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 208000035473 Communicable disease Diseases 0.000 claims 3
- 208000037976 chronic inflammation Diseases 0.000 claims 3
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 3
- 208000015181 infectious disease Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 150000004945 aromatic hydrocarbons Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 206010022000 influenza Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
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- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
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- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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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
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- 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
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- 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
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- C07C65/32—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing keto groups
- C07C65/40—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing keto groups containing singly bound oxygen-containing groups
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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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Claims (15)
1. Spoj, naznačen time, da je predstavljen sljedećom formulom:
[image]
ili njegova farmaceutski prihvatljiva sol ili njegov ester, u kojoj:
Q je piperazin-1,4-diil; 2,5-diazabiciklo[2.2.1]heptan-2,5-diil; 2,5-diazabiciklo[2.2.2]oktan-2,5-diil; 1,4-diazepan-1,4-diil; benzen-1,4-diamin-N1,N4-diil; etan-1,2-diamin-N1,N2-diil; N1,N2-dialkiletan-1,2-diamin-N1,N2-diil; propan-1,3-diamin-N1,N3-diil; N1,N3-dialkilpropan-1,3-diamin-N1,N3-diil; 1,4-diaminoantracen-9,10-dion-1,4-diil; C6-aren-1,4-diamin-N1,N4-diil gdje je aren supstituiran s jednim do četiri supstituenta na pozicijama 2, 3, 5 ili 6 i pritom su supstituenti neovisno odabrani iz skupine koju čine: -C(O)O(C1 do C6)alkil, OH, O(C1 do C6)alkil, (C1 do C6)alkil, CF3, F, Cl i Br; ili supstituirani piperazin-1,4-diil gdje je piperazin supstituiran s jednim do osam supstituenata na pozicijama 2, 3, 5 ili 6 i pritom su supstituenti neovisno odabrani iz skupine koju čine: (C1 do C6)alkil, aril, aril(C1 do C6)alkil, C(O)OH i C(O)O(C1 do C6)alkil;
svaki od A1 i A1' je neovisno N ili CR6;
svaki od A2 i A2' je neovisno N ili CR7;
A3 je NR8;
A3' je NR8, O ili S;
svaki od A4 i A4' je neovisno N ili CR9;
svaki od A5 i A5' je neovisno N ili CR10;
svaki od A6 i A6' je neovisno N ili CR11; i
ako su prisutni R1, R1', R2, R2', R3, R3', R4, R4', R6, R7, R8, R9, R10 i R11, u svakom pojavljivanju su neovisno odabrani iz skupine koju čine: vodik, alkil, halo, trifluorometil, dialkilamino gdje je svaki alkil isti ili različit, -NH2, alkilamino i arilalkil.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da jedan od A1 i A1' ili oba je/su N.
3. Spoj prema patentnom zahtjevu 2, naznačen time, da jedan od A2 i A2' ili oba je/su CH, A3 je NH, A4 je N, A5 je CH i A6 je CH.
4. Spoj prema patentnom zahtjevu 2, naznačen time, da jedan od A2 i A2' ili oba je/su CH, jedan od A3 i A3' ili oba je/su NH, jedan od A4 i A4' ili oba je/su N, jedan od A5 i A5' ili oba je/su CH, te jedan od A6 i A6' ili oba je/su CH.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time, da Q je piperazin-1,4-diil; 2,5-diazabiciklo[2.2.1]heptan-2,5-diil; 2,5-diazabiciklo[2.2.2]oktan-2,5-diil; 1,4-diazepan-1,4-diil; N1,N2-dialkiletan-1,2-diamin-N1,N2-diil; N1,N3-dialkilpropan-1,3-diamin-N1,N3-diil; 1,4-diaminoantracen-9,10-dion-1,4-diil; C6-aren-1,4-diamin-N1,N4-diil gdje je aren supstituiran s jednim do četiri supstituenta na pozicijama 2, 3, 5 ili 6 i pritom je svaki supstituent neovisno odabran iz skupine koju čine: -C(O)O(C1 do C6)alkil, OH, O(C1 do C6)alkil, (C1 do C6)alkil, CF3, F, Cl i Br; ili supstituirani piperazin-1,4-diil gdje je piperazin supstituiran s jednim do osam supstituenata na pozicijama 2, 3, 5 ili 6 i pritom je svaki supstituent neovisno odabran iz skupine koju čine: (C1 do C6)alkil, aril, aril(C1 do C6)alkil, C(O)OH i C(O)O(C1 do C6)alkil.
6. Spoj prema patentnom zahtjevu 1, naznačen time, da ako su prisutni R1, R1', R2, R2', R3, R3', R4, R4', R6, R7, R8, R9, R10 i R11, u svakom pojavljivanju su neovisno odabrani iz skupine koju čine: vodik, alkil, halo i trifluorometil.
7. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima sljedeću strukturu:
[image]
[image]
;
[image]
[image]
[image]
ili njegove soli.
8. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima sljedeću strukturu:
[image]
ili njegove soli.
9. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, da se upotrebljava u postupku liječenja zarazne bolesti, autoimune bolesti, dijabetesa ili kronične upalne bolesti.
10. Spoj za uporabu prema patentnom zahtjevu 9, naznačen time, da se upotrebljava u postupku liječenja zarazne bolesti, gdje zarazna bolest obuhvaća virusnu bolest, opcionalno gdje virusna bolest obuhvaća zarazu gripom.
11. Spoj za uporabu prema patentnom zahtjevu 9, naznačen time, da se upotrebljava u postupku liječenja autoimune bolesti, gdje autoimuna bolest obuhvaća autoimunu upalnu bolest, te pritom autoimuna upalna bolest obuhvaća upalnu bolest crijeva.
12. Spoj za uporabu prema patentnom zahtjevu 11, naznačen time, da se kod autoimune upalne bolesti radi o ulcerativnom kolitisu.
13. Spoj za uporabu prema patentnom zahtjevu 11, naznačen time, da se kod autoimune upalne bolesti radi o Crohnovoj bolesti.
14. Spoj za uporabu prema patentnom zahtjevu 9, naznačen time, da se upotrebljava u postupku liječenja dijabetesa, gdje se kod dijabetesa radi o dijabetesu tipa 1 ili dijabetesu tipa 2.
15. Spoj za uporabu prema patentnom zahtjevu 9, naznačen time, da se upotrebljava u postupku liječenja kronične upalne bolesti, gdje kronična upalna bolest obuhvaća metabolički sindrom.
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US201462068322P | 2014-10-24 | 2014-10-24 | |
US201562101164P | 2015-01-08 | 2015-01-08 | |
PCT/US2015/021417 WO2016064445A1 (en) | 2014-10-24 | 2015-03-19 | Lanthionine synthetase c-like 2-based therapeutics |
EP15714352.0A EP3209655B1 (en) | 2014-10-24 | 2015-03-19 | Lanthionine synthetase c-like 2-based therapeutics |
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EP (2) | EP3757099B1 (hr) |
JP (3) | JP6499306B2 (hr) |
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HR (1) | HRP20201416T1 (hr) |
HU (1) | HUE051299T2 (hr) |
IL (2) | IL252630B (hr) |
LT (1) | LT3209655T (hr) |
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PL (1) | PL3209655T3 (hr) |
PT (1) | PT3209655T (hr) |
RS (1) | RS61013B1 (hr) |
RU (3) | RU2688677C2 (hr) |
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WO2019050890A1 (en) | 2017-09-05 | 2019-03-14 | President And Fellows Of Harvard College | METHODS AND COMPOSITIONS FOR THE TREATMENT OF TUBERCULOSIS |
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EA202091325A1 (ru) | 2017-11-30 | 2020-08-28 | Лэндос Байофарма, Инк. | Способы лечения с помощью лигандов лантионин c-подобного белка 2 и подготовленных с их помощью клеток |
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