HRP20170403T1 - SUPSTITUIRANI BENZOAZEPINI KAO MODULATORI TOLL-u SLIČNIH RECEPTORA - Google Patents
SUPSTITUIRANI BENZOAZEPINI KAO MODULATORI TOLL-u SLIČNIH RECEPTORA Download PDFInfo
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- HRP20170403T1 HRP20170403T1 HRP20170403TT HRP20170403T HRP20170403T1 HR P20170403 T1 HRP20170403 T1 HR P20170403T1 HR P20170403T T HRP20170403T T HR P20170403TT HR P20170403 T HRP20170403 T HR P20170403T HR P20170403 T1 HRP20170403 T1 HR P20170403T1
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Classifications
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- 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
- C07D403/10—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 carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D223/16—Benzazepines; Hydrogenated benzazepines
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Immunology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Luminescent Compositions (AREA)
Claims (15)
1. Spoj s formulom I, ili njegova farmaceutski prihvatljiva sol:
[image]
,
naznačen time što
[image]
je dvostruka veza ili jednostruka veza;
R2 i R3 se neovisno bira između H i C1-C6 alkila, ili su R2 i R3 povezani kako bi tvorili zasićeni 3 do 7-eročlani karbocikl;
jedan od R7 i R8 je
[image]
ili
[image]
,
a drugi je vodik;
R4 je -NRcRd ili -OR10;
Rc i Rd su C1-C6 alkil, koji može biti supstituiran s jednim ili više -OH;
R10 je C1-C12 alkil, koji može biti supstituiran s jednim ili više -OH;
Z je C i
[image]
je dvostruka veza, ili Z je N, a
[image]
je jednostruka veza;
Ra i Rb se neovisno bira između H, C1-C12 alkila, C2-C10 alkenila, C2-C12 alkinila i Re, gdje C1-C12 alkil može biti supstituiran s jednim ili više -OR10, ili Re;
Re se bira između -NH2, -NH(C1-C12 alkil) i -N(C1-C12 alkil)2;
R1 je odsutan kada
[image]
je dvostruka veza, ili kada
[image]
je jednostruka veza, N1-R1 i jedan od Ra ili Rb su povezani kako bi tvorili zasićeni, djelomično nezasićeni ili nezasićeni 5-7-eročlani heterociklički prsten, a drugi od Ra ili Rb može biti vodik ili je po potrebi odsutan zbog nezasićenosti prstena; i
gdje vrijedi najmanje jedna od slijedećih točaka A-D:
A) R7 nije vodik;
B) R8 nije vodik i najmanje jedan od Ra i Rb nije vodik;
C) Z je N; ili
D) N1-R1 i jedan od Ra ili Rb su povezani kako bi tvorili zasićeni, djelomično nezasićeni ili nezasićeni 5-7-eročlani heterociklički prsten.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R7
[image]
ili
[image]
.
3. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što najmanje jedan od Ra i Rb nije vodik; ili je jedan od Ra i Rb C1-C12 alkil, a drugi od Ra i Rb je vodik; ili je jedan od Ra i Rb C1-C12 alkil, supstituiran s Re; ili su Ra i Rb oba C1-C12 alkil; ili je jedan od Ra i Rb Re, a drugi od Ra i Rb je vodik.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R8 nije vodik.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što su N1 i jedan od Ra ili Rb povezani kako bi tvorili zasićeni, djelomično nezasićeni ili nezasićeni 5-7-eročlani heterociklički prsten, a drugi od Ra ili Rb je vodik ili je po potrebi odsutan zbog nezasićenosti prstena.
6. Spoj u skladu s patentnim zahtjevom 5, naznačen time što su N1 i jedan od Ra ili Rb povezani kako bi tvorili zasićeni, djelomično nezasićeni ili nezasićeni 5-eročlani heterociklički prsten.
7. Spoj u skladu s patentnim zahtjevom 6, naznačen time što su N1 i jedan od Ra ili Rb povezani kako bi tvorili
[image]
ili
[image]
.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što najmanje jedan od R2 i R3 nije vodik; ili su R2 i R3 povezani kako bi tvorili zasićeni karbocikl.
9. Spoj u skladu s patentnim zahtjevom 8, naznačen time što su R2 i R3 povezani kako bi tvorili ciklopropil.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je Z N.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R4 -OR10, a R10 je alkil; ili je R4 -NRcRd, a Rc i Rd su oba alkil.
12. Spoj u skladu s patentnim zahtjevom 11, naznačen time što je R4 -O-etil ili -N(propil)2.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time što se bira između
[image]
[image]
ili njihovih farmaceutski prihvatljivih soli.
14. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-13 ili, njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljiv razrjeđivač ili podlogu.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-13 ili, njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju stanja koje se bira između raka, bolesti povezane s imunosnim kompleksom, autoimune bolesti, zarazne bolesti, upalnog poremećaja, imunodeficijencije, odbacivanja presatka, reakcije presatka prema domaćinu, alergije, kardiovaskularne bolesti, fibrotične bolesti, astme i sepse.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161432070P | 2011-01-12 | 2011-01-12 | |
| EP12733896.0A EP2663555B1 (en) | 2011-01-12 | 2012-01-12 | Substituted benzoazepines as toll-like receptor modulators |
| PCT/US2012/021116 WO2012097177A2 (en) | 2011-01-12 | 2012-01-12 | Substituted benzoazepines as toll-like receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20170403T1 true HRP20170403T1 (hr) | 2017-05-19 |
Family
ID=46507673
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170403TT HRP20170403T1 (hr) | 2011-01-12 | 2012-01-12 | SUPSTITUIRANI BENZOAZEPINI KAO MODULATORI TOLL-u SLIČNIH RECEPTORA |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20140088085A1 (hr) |
| EP (2) | EP3207930A1 (hr) |
| JP (2) | JP5985510B2 (hr) |
| CN (2) | CN106518851A (hr) |
| AU (1) | AU2012205490B2 (hr) |
| BR (1) | BR112013017947A2 (hr) |
| CA (1) | CA2824786A1 (hr) |
| DK (1) | DK2663555T3 (hr) |
| ES (1) | ES2620605T3 (hr) |
| HR (1) | HRP20170403T1 (hr) |
| HU (1) | HUE032638T2 (hr) |
| MX (1) | MX348935B (hr) |
| PL (1) | PL2663555T3 (hr) |
| PT (1) | PT2663555T (hr) |
| WO (1) | WO2012097177A2 (hr) |
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| MX2013008220A (es) | 2014-01-20 |
| BR112013017947A2 (pt) | 2018-12-18 |
| ES2620605T3 (es) | 2017-06-29 |
| CN103562201A (zh) | 2014-02-05 |
| PL2663555T4 (pl) | 2017-08-31 |
| PL2663555T3 (pl) | 2017-08-31 |
| EP2663555A4 (en) | 2014-07-16 |
| EP2663555B1 (en) | 2016-12-14 |
| JP2016199582A (ja) | 2016-12-01 |
| MX348935B (es) | 2017-07-03 |
| JP5985510B2 (ja) | 2016-09-06 |
| US20140088085A1 (en) | 2014-03-27 |
| DK2663555T3 (en) | 2017-03-27 |
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