EA202092422A1 - 1h-индазол-3-карбоксамидные соединения в качестве ингибиторов киназы гликогенсинтазы 3-бета - Google Patents
1h-индазол-3-карбоксамидные соединения в качестве ингибиторов киназы гликогенсинтазы 3-бетаInfo
- Publication number
- EA202092422A1 EA202092422A1 EA202092422A EA202092422A EA202092422A1 EA 202092422 A1 EA202092422 A1 EA 202092422A1 EA 202092422 A EA202092422 A EA 202092422A EA 202092422 A EA202092422 A EA 202092422A EA 202092422 A1 EA202092422 A1 EA 202092422A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- disorders
- inhibitors
- kinase
- beta
- carboxamide compounds
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000020233 phosphotransferase Human genes 0.000 title abstract 2
- DITBWPUMEUDVLU-UHFFFAOYSA-N 1h-indazole-3-carboxamide Chemical class C1=CC=C2C(C(=O)N)=NNC2=C1 DITBWPUMEUDVLU-UHFFFAOYSA-N 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 208000035475 disorder Diseases 0.000 abstract 3
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 abstract 2
- 150000008581 1H-indazole-3-carboxamides Chemical class 0.000 abstract 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 abstract 1
- 208000006029 Cardiomegaly Diseases 0.000 abstract 1
- 108010001483 Glycogen Synthase Proteins 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 102000004877 Insulin Human genes 0.000 abstract 1
- 108090001061 Insulin Proteins 0.000 abstract 1
- 208000019022 Mood disease Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 229940125396 insulin Drugs 0.000 abstract 1
- 230000003211 malignant effect Effects 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
- A61K31/41—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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non 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
- A61K31/435—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
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Настоящее изобретение относится к 1H-индазол-3-карбоксамидным соединениям, действующим в качестве ингибиторов киназы гликогенсинтазы 3-бета (GSK-3), и к их применению при лечении нарушений, связанных с GSK-3, таких как, например, (i) инсулинрезистентные нарушения; (ii) нейродегенеративные заболевания; (iii) расстройства настроения; (iv) шизофренические расстройства; (v) злокачественные нарушения; (vi) воспаление, (vii) остеопороз, (viii) гипертрофия сердца, (ix) эпилепсии и (x) невропатическая боль.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18171084 | 2018-05-07 | ||
| PCT/EP2019/061532 WO2019215075A1 (en) | 2018-05-07 | 2019-05-06 | 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA202092422A1 true EA202092422A1 (ru) | 2021-02-12 |
Family
ID=62134122
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202092422A EA202092422A1 (ru) | 2018-05-07 | 2019-05-06 | 1h-индазол-3-карбоксамидные соединения в качестве ингибиторов киназы гликогенсинтазы 3-бета |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US11472795B2 (ru) |
| EP (1) | EP3790873B1 (ru) |
| JP (1) | JP7411574B2 (ru) |
| KR (1) | KR20210005863A (ru) |
| CN (1) | CN112135821B (ru) |
| AU (1) | AU2019265606B2 (ru) |
| BR (1) | BR112020021922A2 (ru) |
| CA (1) | CA3094896A1 (ru) |
| DK (1) | DK3790873T3 (ru) |
| EA (1) | EA202092422A1 (ru) |
| ES (1) | ES2913975T3 (ru) |
| GE (1) | GEP20227437B (ru) |
| HR (1) | HRP20220664T1 (ru) |
| HU (1) | HUE058894T2 (ru) |
| IL (1) | IL278330B2 (ru) |
| LT (1) | LT3790873T (ru) |
| MA (1) | MA52557A (ru) |
| MD (1) | MD3790873T2 (ru) |
| MX (1) | MX2020011882A (ru) |
| PL (1) | PL3790873T3 (ru) |
| PT (1) | PT3790873T (ru) |
| RS (1) | RS63255B1 (ru) |
| SG (1) | SG11202009230WA (ru) |
| SI (1) | SI3790873T1 (ru) |
| UA (1) | UA128089C2 (ru) |
| WO (1) | WO2019215075A1 (ru) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102650856B1 (ko) * | 2019-12-16 | 2024-03-25 | 한국화학연구원 | 신규한 인다졸 유도체 및 이의 용도 |
| CN114230565B (zh) * | 2020-09-09 | 2023-10-27 | 成都奥睿药业有限公司 | 5-取代吲哚3-酰胺衍生物及其制备方法和用途 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR950704328A (ko) | 1992-11-05 | 1995-11-17 | 데이비드 로버츠 | 5-HT₄ 수용체 길항제로서의 피페리딘 유도체(Piperidine Derivatives as 5-HT₄ Receptor Antagonists) |
| GB0218625D0 (en) | 2002-08-10 | 2002-09-18 | Astex Technology Ltd | Pharmaceutical compounds |
| ITMI20030287A1 (it) | 2003-02-18 | 2004-08-19 | Acraf | Indazolammidi dotate di attivita' analgesica metodo, per |
| ITMI20030972A1 (it) | 2003-05-15 | 2004-11-16 | Acraf | Indazolo dotato di attivita' analgesica, metodo per prepararlo e composizione farmaceutica che lo comprende. |
| KR101061599B1 (ko) * | 2008-12-05 | 2011-09-02 | 한국과학기술연구원 | 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물 |
| TW201040191A (en) | 2009-03-27 | 2010-11-16 | Abbott Gmbh & Co Kg | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
| PE20141678A1 (es) * | 2011-09-14 | 2014-11-21 | Samumed Llc | Indazol-3-carboxamidas y su uso como inhibidores de la ruta de senalizacion de wnt/b-catenina |
| GEP20166489B (en) | 2012-02-21 | 2016-06-10 | Acraf | 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors |
| PL2817301T3 (pl) | 2012-02-21 | 2016-05-31 | Acraf | Zastosowanie związków 1H-indazolo-3-karboksyamidowych jako inhibitorów kinazy syntazy glikogenu 3-beta |
| KR20160135283A (ko) | 2014-03-20 | 2016-11-25 | 사뮤메드, 엘엘씨 | 5-치환된 인다졸-3-카르복스아미드 및 이의 제조 및 용도 |
| ES2945558T3 (es) * | 2018-02-23 | 2023-07-04 | Biosplice Therapeutics Inc | Indazol-3-carboxamidas sustituidas con 5-heteroarilo y preparación y uso de las mismas |
-
2019
- 2019-05-06 GE GEAP201915506A patent/GEP20227437B/en unknown
- 2019-05-06 EA EA202092422A patent/EA202092422A1/ru unknown
- 2019-05-06 DK DK19721295.4T patent/DK3790873T3/da active
- 2019-05-06 SI SI201930227T patent/SI3790873T1/sl unknown
- 2019-05-06 ES ES19721295T patent/ES2913975T3/es active Active
- 2019-05-06 AU AU2019265606A patent/AU2019265606B2/en active Active
- 2019-05-06 CA CA3094896A patent/CA3094896A1/en active Pending
- 2019-05-06 BR BR112020021922-3A patent/BR112020021922A2/pt unknown
- 2019-05-06 MA MA052557A patent/MA52557A/fr unknown
- 2019-05-06 MX MX2020011882A patent/MX2020011882A/es unknown
- 2019-05-06 KR KR1020207030163A patent/KR20210005863A/ko not_active Application Discontinuation
- 2019-05-06 CN CN201980029405.9A patent/CN112135821B/zh active Active
- 2019-05-06 MD MDE20210228T patent/MD3790873T2/ro unknown
- 2019-05-06 JP JP2020562568A patent/JP7411574B2/ja active Active
- 2019-05-06 RS RS20220482A patent/RS63255B1/sr unknown
- 2019-05-06 HU HUE19721295A patent/HUE058894T2/hu unknown
- 2019-05-06 PT PT197212954T patent/PT3790873T/pt unknown
- 2019-05-06 UA UAA202006085A patent/UA128089C2/uk unknown
- 2019-05-06 LT LTEPPCT/EP2019/061532T patent/LT3790873T/lt unknown
- 2019-05-06 IL IL278330A patent/IL278330B2/en unknown
- 2019-05-06 EP EP19721295.4A patent/EP3790873B1/en active Active
- 2019-05-06 PL PL19721295T patent/PL3790873T3/pl unknown
- 2019-05-06 WO PCT/EP2019/061532 patent/WO2019215075A1/en active Application Filing
- 2019-05-06 HR HRP20220664TT patent/HRP20220664T1/hr unknown
- 2019-05-06 US US17/051,352 patent/US11472795B2/en active Active
- 2019-05-06 SG SG11202009230WA patent/SG11202009230WA/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| LT3790873T (lt) | 2022-06-10 |
| IL278330B1 (en) | 2024-02-01 |
| WO2019215075A1 (en) | 2019-11-14 |
| PL3790873T3 (pl) | 2022-06-27 |
| CN112135821B (zh) | 2024-05-31 |
| HUE058894T2 (hu) | 2022-09-28 |
| CN112135821A (zh) | 2020-12-25 |
| IL278330A (ru) | 2020-12-31 |
| HRP20220664T1 (hr) | 2022-06-24 |
| KR20210005863A (ko) | 2021-01-15 |
| BR112020021922A2 (pt) | 2021-01-26 |
| AU2019265606B2 (en) | 2023-10-12 |
| JP2021523134A (ja) | 2021-09-02 |
| MD3790873T2 (ro) | 2022-07-31 |
| AU2019265606A1 (en) | 2020-10-15 |
| GEP20227437B (en) | 2022-11-10 |
| US20210053956A1 (en) | 2021-02-25 |
| DK3790873T3 (da) | 2022-05-23 |
| SG11202009230WA (en) | 2020-11-27 |
| RS63255B1 (sr) | 2022-06-30 |
| CA3094896A1 (en) | 2019-11-14 |
| EP3790873B1 (en) | 2022-04-27 |
| UA128089C2 (uk) | 2024-04-03 |
| US11472795B2 (en) | 2022-10-18 |
| SI3790873T1 (sl) | 2022-07-29 |
| ES2913975T3 (es) | 2022-06-07 |
| EP3790873A1 (en) | 2021-03-17 |
| PT3790873T (pt) | 2022-05-11 |
| MX2020011882A (es) | 2021-01-20 |
| JP7411574B2 (ja) | 2024-01-11 |
| MA52557A (fr) | 2021-03-17 |
| IL278330B2 (en) | 2024-06-01 |
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