RU2019125177A - Новые производные амино-имидазопиридина в качестве ингибиторов янус-киназы и их фармацевтическое применение - Google Patents
Новые производные амино-имидазопиридина в качестве ингибиторов янус-киназы и их фармацевтическое применение Download PDFInfo
- Publication number
- RU2019125177A RU2019125177A RU2019125177A RU2019125177A RU2019125177A RU 2019125177 A RU2019125177 A RU 2019125177A RU 2019125177 A RU2019125177 A RU 2019125177A RU 2019125177 A RU2019125177 A RU 2019125177A RU 2019125177 A RU2019125177 A RU 2019125177A
- Authority
- RU
- Russia
- Prior art keywords
- acetonitrile
- cyclohexyl
- imidazo
- pyridin
- hydroxyethyl
- Prior art date
Links
- KXQPVJRJUJJWQJ-UHFFFAOYSA-N 1h-imidazo[4,5-b]pyridin-2-amine Chemical class C1=CN=C2NC(N)=NC2=C1 KXQPVJRJUJJWQJ-UHFFFAOYSA-N 0.000 title 1
- 102000015617 Janus Kinases Human genes 0.000 title 1
- 108010024121 Janus Kinases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 7
- 229910052805 deuterium Inorganic materials 0.000 claims 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 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 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 210000000987 immune system Anatomy 0.000 claims 3
- ROANNSYULQYJLV-UHFFFAOYSA-N 2-[4-[2-(1-hydroxyethyl)-6-(methylamino)imidazo[4,5-c]pyridin-1-yl]cyclohexyl]acetonitrile Chemical compound CNC1=NC=C2N=C(C(C)O)N(C3CCC(CC#N)CC3)C2=C1 ROANNSYULQYJLV-UHFFFAOYSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- ROANNSYULQYJLV-PNESKVBLSA-N 2-[4-[2-[(1R)-1-hydroxyethyl]-6-(methylamino)imidazo[4,5-c]pyridin-1-yl]cyclohexyl]acetonitrile Chemical compound CNc1cc2n(C3CCC(CC#N)CC3)c(nc2cn1)[C@@H](C)O ROANNSYULQYJLV-PNESKVBLSA-N 0.000 claims 1
- BPYMPKDCQAPAQR-YWRZDDHQSA-N C1(=CC=2N(C(=NC=2C=N1)C(C)O)[C@H]1CC[C@@H](CC1)CC#N)Cl Chemical compound C1(=CC=2N(C(=NC=2C=N1)C(C)O)[C@H]1CC[C@@H](CC1)CC#N)Cl BPYMPKDCQAPAQR-YWRZDDHQSA-N 0.000 claims 1
- BPYMPKDCQAPAQR-LKNKNRNPSA-N ClC1=CC2=C(C=N1)N=C(N2[C@@H]1CC[C@H](CC1)CC#N)C(C([2H])([2H])[2H])(O)[2H] Chemical compound ClC1=CC2=C(C=N1)N=C(N2[C@@H]1CC[C@H](CC1)CC#N)C(C([2H])([2H])[2H])(O)[2H] BPYMPKDCQAPAQR-LKNKNRNPSA-N 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims 1
- ROANNSYULQYJLV-AVGNSLFASA-N N1(C2=C(N=C1[C@@H](O)C)C=NC(=C2)NC)[C@H]1CC[C@@H](CC1)CC#N Chemical compound N1(C2=C(N=C1[C@@H](O)C)C=NC(=C2)NC)[C@H]1CC[C@@H](CC1)CC#N ROANNSYULQYJLV-AVGNSLFASA-N 0.000 claims 1
- PQHPWXJREYZBAC-MGCOHNPYSA-N NC=1C(=CC(=NC=1)Cl)N[C@@H]1CC[C@H](CC1)CC#N Chemical compound NC=1C(=CC(=NC=1)Cl)N[C@@H]1CC[C@H](CC1)CC#N PQHPWXJREYZBAC-MGCOHNPYSA-N 0.000 claims 1
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims 1
- ROANNSYULQYJLV-PGOIJJQSSA-N [2H]C(C([2H])([2H])[2H])(O)C=1N(C2=C(C=NC(=C2)NC)N=1)[C@@H]1CC[C@H](CC1)CC#N Chemical compound [2H]C(C([2H])([2H])[2H])(O)C=1N(C2=C(C=NC(=C2)NC)N=1)[C@@H]1CC[C@H](CC1)CC#N ROANNSYULQYJLV-PGOIJJQSSA-N 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000008482 dysregulation Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
Classifications
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17151020 | 2017-01-11 | ||
| EP17151020.9 | 2017-01-11 | ||
| PCT/EP2018/050548 WO2018130563A1 (en) | 2017-01-11 | 2018-01-10 | Novel amino-imidazopyridine derivatives as janus kinase inhibitors and pharmaceutical use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2019125177A true RU2019125177A (ru) | 2021-02-15 |
| RU2019125177A3 RU2019125177A3 (cg-RX-API-DMAC7.html) | 2021-05-11 |
Family
ID=57777557
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2019125177A RU2019125177A (ru) | 2017-01-11 | 2018-01-10 | Новые производные амино-имидазопиридина в качестве ингибиторов янус-киназы и их фармацевтическое применение |
Country Status (26)
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| EP4086256A1 (en) | 2016-12-16 | 2022-11-09 | Janssen Pharmaceutica NV | Small molecule inhibitors of the jak family of kinases |
| 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 |
| CN112384514A (zh) * | 2018-07-06 | 2021-02-19 | 利奥制药有限公司 | 作为janus激酶抑制剂的新的氨基-咪唑并嘧啶衍生物及其药物用途 |
| CN114555595B (zh) * | 2019-08-30 | 2023-12-26 | Tsd生命科学有限公司 | 咪唑并吡啶衍生物及将其作为有效成分的药学组合物 |
| CA3213134A1 (en) | 2021-03-11 | 2022-09-15 | Janssen Pharmaceutica Nv | Lorpucitinib for use in the treatment of jak mediated disorders |
| CN119569971B (zh) * | 2025-02-07 | 2025-05-27 | 吉林大学 | 一种用于蛋白质磷酸化和棕榈酰化修饰同时筛选的Janus材料的制备方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101981033B (zh) * | 2008-02-06 | 2015-02-04 | 百时美施贵宝公司 | 用作激酶抑制剂的取代的咪唑并哒嗪化合物 |
| US8461328B2 (en) * | 2010-01-12 | 2013-06-11 | Genentech, Inc. | Tricyclic heterocyclic compounds, compositions and methods of use thereof |
| CN103168032A (zh) * | 2010-08-05 | 2013-06-19 | 安美基公司 | 抑制间变性淋巴瘤激酶的苯并咪唑和氮杂苯并咪唑化合物 |
| 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 |
| 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 |
| WO2013007765A1 (en) | 2011-07-13 | 2013-01-17 | F. Hoffmann-La Roche Ag | Fused tricyclic compounds for use as inhibitors of janus kinases |
| UY34616A (es) * | 2012-02-10 | 2013-09-30 | Galapagos Nv | Nuevo compuesto útil para el tratamiento de enfermedades degenerativas e inflamatorias. |
| UA117572C2 (uk) | 2012-11-01 | 2018-08-27 | Інсайт Холдинґс Корпорейшн | Трициклічні конденсовані похідні тіофену як інгібітори jak |
| EP3181564B1 (en) * | 2012-11-20 | 2019-09-18 | H. Hoffnabb-La Roche Ag | 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 |
| TW201625643A (zh) * | 2014-04-30 | 2016-07-16 | 英塞特公司 | 製備ｊａｋ１抑制劑之方法及其新形式 |
| PT3509591T (pt) | 2016-10-03 | 2021-12-27 | Highlightll Pharmaceutical Hainan Co Ltd | Novos inibidores seletivos da jak1 e usos dos mesmos |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
-
2018
- 2018-01-10 LT LTEP18702412.0T patent/LT3568396T/lt unknown
- 2018-01-10 HU HUE18702412A patent/HUE052720T2/hu unknown
- 2018-01-10 EP EP18702412.0A patent/EP3568396B1/en active Active
- 2018-01-10 MX MX2019008331A patent/MX389378B/es unknown
- 2018-01-10 CN CN201880006261.0A patent/CN110167938B/zh active Active
- 2018-01-10 ES ES18702412T patent/ES2846741T3/es active Active
- 2018-01-10 AU AU2018208516A patent/AU2018208516B2/en active Active
- 2018-01-10 US US16/477,249 patent/US10703751B2/en active Active
- 2018-01-10 WO PCT/EP2018/050548 patent/WO2018130563A1/en not_active Ceased
- 2018-01-10 NZ NZ754922A patent/NZ754922A/en unknown
- 2018-01-10 RS RS20210044A patent/RS61317B1/sr unknown
- 2018-01-10 KR KR1020197021697A patent/KR102548543B1/ko active Active
- 2018-01-10 PT PT187024120T patent/PT3568396T/pt unknown
- 2018-01-10 UA UAA201908568A patent/UA123972C2/uk unknown
- 2018-01-10 DK DK18702412.0T patent/DK3568396T3/da active
- 2018-01-10 PL PL18702412T patent/PL3568396T3/pl unknown
- 2018-01-10 JP JP2019557681A patent/JP7009504B2/ja active Active
- 2018-01-10 RU RU2019125177A patent/RU2019125177A/ru unknown
- 2018-01-10 HR HRP20210095TT patent/HRP20210095T1/hr unknown
- 2018-01-10 MY MYPI2019003964A patent/MY195576A/en unknown
- 2018-01-10 CA CA3045567A patent/CA3045567A1/en active Pending
- 2018-01-10 SI SI201830191T patent/SI3568396T1/sl 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
-
2021
- 2021-02-01 CY CY20211100085T patent/CY1123864T1/el unknown
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