HRP20210095T1 - Novi derivati amino-imidazopiridina kao inhibitori janus kinaze i njihova farmaceutska upotreba - Google Patents
Novi derivati amino-imidazopiridina kao inhibitori janus kinaze i njihova farmaceutska upotreba Download PDFInfo
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- HRP20210095T1 HRP20210095T1 HRP20210095TT HRP20210095T HRP20210095T1 HR P20210095 T1 HRP20210095 T1 HR P20210095T1 HR P20210095T T HRP20210095T T HR P20210095TT HR P20210095 T HRP20210095 T HR P20210095T HR P20210095 T1 HRP20210095 T1 HR P20210095T1
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- Prior art keywords
- acetonitrile
- cyclohexyl
- imidazo
- pyridin
- hydroxyethyl
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Classifications
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- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
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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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- 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
- A61P37/08—Antiallergic 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (13)
1. Spoj prema općoj formuli (I)
[image]
gdje
A predstavlja C6-cikloalkil, pri čemu je navedeni C6-cikloalkil opcionalno supstituiran sa jednim ili više deuterija;
R1 predstavlja C1-alkil, pri čemu je navedeni C1-alkil opcionalno supstituiran sa jednim ili više deuterija;
R2 predstavlja C1-alkil, pri čemu je navedeni C1-alkil supstituiran sa supstituentom izabranim od R6; i pri čemu je navedeni C1-alkil opcionalno supstituiran sa jednim ili više deuterija;
R3 predstavlja C2-alkil, pri čemu je navedeni C2-alkil supstituiran sa supstituentom izabranim od R7 i pri čemu je navedeni C2-alkil opcionalno supstituiran sa jednim ili više deuterija;
R4 predstavlja vodik ili deuterij;
R5 predstavlja vodik ili deuterij;
R6 predstavlja cijano;
R7 predstavlja hidroksil;
ili njegove farmaceutski prihvatljive soli, hidrati ili solvati.
2. Spoj prema zahtjevu 1 pri čemu je formula (I) opća formula (Ia)
[image]
gdje su R1-R2, R4-R7 kako je definirano u zahtjevu 1 i gdje su Ra, Rb, Rc i Rd svaki nezavisno izabrani od vodika i deuterija.
3. Spoj prema zahtjevu 1 ili 2 pri čemu je formula (I) opća formula (Ib)
[image]
gdje R1-R2, R4-R7, Ra, Rb, Rc i Rd su kako je definirano u zahtjevu 1 ili 2.
4. Spoj prema bilo kojem od zahtjeva 1-3 izabran od
trans-2-[4-[2-[1-hidroksietil]-6-(metilamino)imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitrila, trans-2-[4-[2-[(1S)-1-hidroksietil]-6-(metilamino)imidazo[4,5-c]piridin-1-il]cikloheksil]-acetonitrila,
trans-2-[4-[2-[(1R)-1-hidroksietil]-6-(metilamino)imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitrila,
trans-2-[4-[2-[(1R)-1-hidroksietil]-6-(trideuteriometilamino)imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitrila,
trans-2-[4-[2-[1,2,2,2-tetradeuterio-1-hidroksietil]-6-(metilamino)imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitrila,
cis-2-[4-[2-[1-hidroksietil]-6-(metilamino)imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitrila i
cis-2-[4-[2-[(1R)-1-hidroksietil]-6-(metilamino)imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitrila,
ili njihovih farmaceutski prihvatljivih soli, hidrata ili solvata.
5. Spoj prema bilo kojem od zahtjeva 1-4, pri čemu je naveden spoj trans-2-[4-[2-[(1R)-1-hidroksietil]-6-(metilamino)imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitril, ili njegove farmaceutski prihvatljive soli.
6. Spoj prema bilo kojem od zahtjeva 1-5 za upotrebu kao lijek.
7. Spoj prema bilo kojem od zahtjeva 1-5 za upotrebu u preventivi i/ili liječenju bolesti imunološkog sustava kao što su autoimune bolesti, ili bolesti povezane s deregulacijom imunološkog sustava.
8. Spoj za upotrebu prema zahtjevu 7 u preventivi i/ili liječenju atopijskog dermatitisa.
9. Farmaceutski sastav koja sadrži spoj prema bilo kojem od zahtjeva 1-5 zajedno s farmaceutski prihvatljivim prijenosnikom ili pomoćnom tvari ili farmaceutski prihvatljivim nosačem(ima).
10. Farmaceutski sastav prema zahtjevu 9 zajedno s jednim ili više drugih terapeutski aktivnih spojeva.
11. Spoj prema bilo kojem od zahtjeva 1-5 za upotrebu u liječenju bolesti, gdje bolest reagira na inhibiciju aktivnosti JAK1 kinaze.
12. Spoj izabran od 2-[trans-4-[(5-amino-2-kloropiridin-4-il)amino]cikloheksil]acetonitrila ili njegovih soli.
13. Spoj izabran od
2-[trans-4-[6-kloro-2-(1-hidroksietil)-1H-imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitrila,
2-[trans-4-[6-kloro-2-[(1R)-1-hidroksietil]-1H-imidazo[4,5-c]piridin-1-il]cikloheksil]acetonitrila i
trans-2-[4-[6-kloro-2-(1,2,2,2-tetradeuterio-1-hidroksi-etil)imidazo[4,5-c]piridin-1-il]ciklohe-ksil]acetonitrila,
ili njihovih soli.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17151020 | 2017-01-11 | ||
| EP18702412.0A EP3568396B1 (en) | 2017-01-11 | 2018-01-10 | Novel amino-imidazopyridine derivatives as janus kinase inhibitors and pharmaceutical use thereof |
| PCT/EP2018/050548 WO2018130563A1 (en) | 2017-01-11 | 2018-01-10 | Novel amino-imidazopyridine derivatives as janus kinase inhibitors and pharmaceutical use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20210095T1 true HRP20210095T1 (hr) | 2021-03-05 |
Family
ID=57777557
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20210095TT HRP20210095T1 (hr) | 2017-01-11 | 2021-01-19 | Novi derivati amino-imidazopiridina kao inhibitori janus kinaze i njihova farmaceutska upotreba |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US10703751B2 (hr) |
| EP (1) | EP3568396B1 (hr) |
| JP (1) | JP7009504B2 (hr) |
| KR (1) | KR102548543B1 (hr) |
| CN (1) | CN110167938B (hr) |
| AU (1) | AU2018208516B2 (hr) |
| BR (1) | BR112019014191A2 (hr) |
| CA (1) | CA3045567A1 (hr) |
| CY (1) | CY1123864T1 (hr) |
| DK (1) | DK3568396T3 (hr) |
| ES (1) | ES2846741T3 (hr) |
| HR (1) | HRP20210095T1 (hr) |
| HU (1) | HUE052720T2 (hr) |
| IL (1) | IL267829B (hr) |
| LT (1) | LT3568396T (hr) |
| MX (1) | MX2019008331A (hr) |
| MY (1) | MY195576A (hr) |
| PL (1) | PL3568396T3 (hr) |
| PT (1) | PT3568396T (hr) |
| RS (1) | RS61317B1 (hr) |
| RU (1) | RU2019125177A (hr) |
| SI (1) | SI3568396T1 (hr) |
| TW (1) | TWI760419B (hr) |
| UA (1) | UA123972C2 (hr) |
| WO (1) | WO2018130563A1 (hr) |
| ZA (1) | ZA201904190B (hr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20220885T1 (hr) | 2016-12-16 | 2022-12-09 | Janssen Pharmaceutica Nv | Spojevi imidazo[4,5-d]pirolo[2,3-b]piridina kao inhibitori janus kinaze |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| TW202016110A (zh) | 2018-06-15 | 2020-05-01 | 比利時商健生藥品公司 | Ｊａｋ激酶家族之小分子抑制劑 |
| US20210269447A1 (en) * | 2018-07-06 | 2021-09-02 | Leo Pharma A/S | Novel amino-imidazopyrimidine derivatives as janus kinase inhibitors and pharmaceutical use thereof |
| WO2021040502A1 (ko) * | 2019-08-30 | 2021-03-04 | 주식회사 티에스디라이프사이언스 | 이미다조피리딘 유도체 및 이를 유효성분으로 함유하는 약학적 조성물 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2240488B1 (en) * | 2008-02-06 | 2016-11-02 | Bristol-Myers Squibb Company | Substituted imidazopyridazines useful as kinase inhibitors |
| AR079984A1 (es) * | 2010-01-12 | 2012-03-07 | Hoffmann La Roche | Compuestos heterociclicos triciclicos, composiciones y su uso en el tratamiento de enfermedades mediadas por la inhibicion de jak1 |
| US9115127B2 (en) * | 2010-08-05 | 2015-08-25 | Amgen Inc. | Benzimidazole and azabenzimidazole compounds that inhibit anaplastic lymphoma kinase |
| EP2518071A1 (en) | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Imidazopyridine derivatives as PI3K inhibitors |
| EP2527344A1 (en) * | 2011-05-25 | 2012-11-28 | Almirall, S.A. | Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases |
| WO2013007765A1 (en) * | 2011-07-13 | 2013-01-17 | F. Hoffmann-La Roche Ag | Fused tricyclic compounds for use as inhibitors of janus kinases |
| WO2013007768A1 (en) | 2011-07-13 | 2013-01-17 | F. Hoffmann-La Roche Ag | Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors |
| UY34616A (es) * | 2012-02-10 | 2013-09-30 | Galapagos Nv | Nuevo compuesto útil para el tratamiento de enfermedades degenerativas e inflamatorias. |
| TWI646099B (zh) | 2012-11-01 | 2019-01-01 | 英塞特控股公司 | 作爲ｊａｋ抑制劑之三環稠合噻吩衍生物 |
| CA2891655A1 (en) * | 2012-11-20 | 2014-05-30 | Genentech, Inc. | Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants |
| CN104098563A (zh) * | 2013-04-02 | 2014-10-15 | 山东亨利医药科技有限责任公司 | Jnk抑制剂化合物 |
| MA39987A (fr) * | 2014-04-30 | 2017-03-08 | Incyte Corp | Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées |
| RS62695B1 (sr) | 2016-10-03 | 2022-01-31 | Highlightll Pharmaceutical Hainan Co Ltd | Novi jak1 selektivni inhibitori i njihove upotrebe |
| JOP20190144A1 (ar) * | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
-
2018
- 2018-01-10 MX MX2019008331A patent/MX2019008331A/es unknown
- 2018-01-10 PT PT187024120T patent/PT3568396T/pt unknown
- 2018-01-10 EP EP18702412.0A patent/EP3568396B1/en active Active
- 2018-01-10 CA CA3045567A patent/CA3045567A1/en active Pending
- 2018-01-10 ES ES18702412T patent/ES2846741T3/es active Active
- 2018-01-10 UA UAA201908568A patent/UA123972C2/uk unknown
- 2018-01-10 RU RU2019125177A patent/RU2019125177A/ru unknown
- 2018-01-10 DK DK18702412.0T patent/DK3568396T3/da active
- 2018-01-10 AU AU2018208516A patent/AU2018208516B2/en active Active
- 2018-01-10 JP JP2019557681A patent/JP7009504B2/ja active Active
- 2018-01-10 PL PL18702412T patent/PL3568396T3/pl unknown
- 2018-01-10 KR KR1020197021697A patent/KR102548543B1/ko active Active
- 2018-01-10 MY MYPI2019003964A patent/MY195576A/en unknown
- 2018-01-10 RS RS20210044A patent/RS61317B1/sr unknown
- 2018-01-10 CN CN201880006261.0A patent/CN110167938B/zh active Active
- 2018-01-10 SI SI201830191T patent/SI3568396T1/sl unknown
- 2018-01-10 BR BR112019014191-0A patent/BR112019014191A2/pt active Search and Examination
- 2018-01-10 WO PCT/EP2018/050548 patent/WO2018130563A1/en active Application Filing
- 2018-01-10 US US16/477,249 patent/US10703751B2/en active Active
- 2018-01-10 HU HUE18702412A patent/HUE052720T2/hu unknown
- 2018-01-10 LT LTEP18702412.0T patent/LT3568396T/lt unknown
- 2018-01-11 TW TW107101035A patent/TWI760419B/zh active
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2019
- 2019-06-26 ZA ZA2019/04190A patent/ZA201904190B/en unknown
- 2019-07-03 IL IL267829A patent/IL267829B/en unknown
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2021
- 2021-01-19 HR HRP20210095TT patent/HRP20210095T1/hr unknown
- 2021-02-01 CY CY20211100085T patent/CY1123864T1/el unknown
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