RU2015104962A - Ди- и тригетероарильные производные в качестве ингибиторов агрегации белков - Google Patents
Ди- и тригетероарильные производные в качестве ингибиторов агрегации белков Download PDFInfo
- Publication number
- RU2015104962A RU2015104962A RU2015104962A RU2015104962A RU2015104962A RU 2015104962 A RU2015104962 A RU 2015104962A RU 2015104962 A RU2015104962 A RU 2015104962A RU 2015104962 A RU2015104962 A RU 2015104962A RU 2015104962 A RU2015104962 A RU 2015104962A
- Authority
- RU
- Russia
- Prior art keywords
- compound
- methylpiperazin
- indol
- carboxamide
- methyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 230000004845 protein aggregation Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 36
- -1 Salkoxy Chemical group 0.000 claims abstract 13
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims abstract 8
- 239000012634 fragment Substances 0.000 claims abstract 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 6
- 150000003839 salts Chemical class 0.000 claims abstract 6
- 125000002541 furyl group Chemical group 0.000 claims abstract 4
- 125000002883 imidazolyl group Chemical group 0.000 claims abstract 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims abstract 4
- 125000002971 oxazolyl group Chemical group 0.000 claims abstract 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims abstract 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims abstract 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims abstract 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims abstract 4
- 125000000335 thiazolyl group Chemical group 0.000 claims abstract 4
- 125000001544 thienyl group Chemical group 0.000 claims abstract 4
- 125000001425 triazolyl group Chemical group 0.000 claims abstract 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims abstract 2
- 229910052736 halogen Inorganic materials 0.000 claims abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims abstract 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims abstract 2
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- MVBFOPDCLIPGAT-UHFFFAOYSA-N 2-[1-butyl-5-(1h-indol-3-ylmethyl)imidazol-2-yl]-5-(4-methylpiperazin-1-yl)-1,3,4-thiadiazole Chemical compound CCCCN1C(CC=2C3=CC=CC=C3NC=2)=CN=C1C(S1)=NN=C1N1CCN(C)CC1 MVBFOPDCLIPGAT-UHFFFAOYSA-N 0.000 claims 1
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- LFNJITKDZFBJJI-UHFFFAOYSA-N 5-[1-butyl-5-(1h-indol-3-ylmethyl)imidazol-2-yl]-2-(4-methylpiperazin-1-yl)-1,3-thiazole Chemical compound CCCCN1C(CC=2C3=CC=CC=C3NC=2)=CN=C1C(S1)=CN=C1N1CCN(C)CC1 LFNJITKDZFBJJI-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003694 Atrophy Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 230000037444 atrophy Effects 0.000 claims 1
- 230000004900 autophagic degradation Effects 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261672239P | 2012-07-16 | 2012-07-16 | |
| US61/672,239 | 2012-07-16 | ||
| PCT/US2013/050719 WO2014014937A1 (en) | 2012-07-16 | 2013-07-16 | Di-and tri-heteroaryl derivatives as inhibitors of protein aggregation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2015104962A true RU2015104962A (ru) | 2016-09-10 |
Family
ID=49949212
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015104962A RU2015104962A (ru) | 2012-07-16 | 2013-07-16 | Ди- и тригетероарильные производные в качестве ингибиторов агрегации белков |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9284309B2 (https=) |
| EP (1) | EP2872143B1 (https=) |
| JP (1) | JP2015522617A (https=) |
| KR (1) | KR20150031481A (https=) |
| CN (1) | CN104703604A (https=) |
| AU (1) | AU2013290361A1 (https=) |
| BR (1) | BR112015001096A2 (https=) |
| CA (1) | CA2877983A1 (https=) |
| ES (1) | ES2661394T3 (https=) |
| HK (1) | HK1210598A1 (https=) |
| IL (1) | IL236712A0 (https=) |
| IN (1) | IN2015DN01171A (https=) |
| MX (1) | MX2015000618A (https=) |
| RU (1) | RU2015104962A (https=) |
| WO (1) | WO2014014937A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AP2016009347A0 (en) * | 2014-01-29 | 2016-07-31 | Neuropore Therapies Inc | Heteroarly amides as inhibitors of protein aggregation |
| EP3328379B1 (en) * | 2015-07-29 | 2021-07-28 | UCB Biopharma SRL | Bis-heteroaryl derivatives as modulators of protein aggregation |
| EA201991755A1 (ru) | 2017-01-26 | 2020-01-22 | Юсб Байофарма Спрл | Бициклические бисгетероарильные производные в качестве модуляторов агрегации белков |
| CN110198938B (zh) | 2017-01-26 | 2023-03-14 | Ucb生物制药私人有限公司 | 作为蛋白质聚集调节剂的双-杂芳基衍生物 |
| KR20190112031A (ko) * | 2017-01-26 | 2019-10-02 | 유씨비 바이오파마 에스피알엘 | 단백질 응집의 조절제로서의 알콕시 비스-헤테로아릴 유도체 |
| WO2018158160A1 (en) | 2017-02-28 | 2018-09-07 | Universitat Autonoma De Barcelona | (nitro-phenyl)-nitropyridine compounds for treating synucleinopathies |
| WO2019025424A1 (en) | 2017-08-04 | 2019-02-07 | Universitat Autonoma De Barcelona | COMPOUNDS FOR TREATING SYNUCLEINOPATHIES |
| WO2019161917A1 (en) | 2018-02-23 | 2019-08-29 | Universitat Autonoma De Barcelona | 4-substituted 1-ethenylsulfonyl-2-nitrobenzene compounds for treating synucleinopathies |
| CN113683598B (zh) * | 2020-05-18 | 2022-10-14 | 成都先导药物开发股份有限公司 | 一种免疫调节剂 |
| WO2025223458A1 (zh) * | 2024-04-23 | 2025-10-30 | 深圳众格生物科技有限公司 | 一种cyp11a1抑制剂、其制备方法及其应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4739632B2 (ja) | 2000-02-05 | 2011-08-03 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｅｒｋのインヒビターとして有用なピラゾール組成物 |
| EP1317453B1 (en) | 2000-09-15 | 2006-08-09 | Vertex Pharmaceuticals Incorporated | Isoxazoles and their use as inhibitors of erk |
| AU2003257094A1 (en) * | 2002-08-08 | 2004-02-25 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted benzimidazole compounds |
| LT2899191T (lt) | 2009-04-30 | 2017-10-25 | Glaxo Group Limited | Oksazolo pakeistieji indazolai kaip pi3-kinazės inhibitoriai |
| GB0910003D0 (en) * | 2009-06-11 | 2009-07-22 | Univ Leuven Kath | Novel compounds for the treatment of neurodegenerative diseases |
| KR20120112548A (ko) * | 2009-12-16 | 2012-10-11 | 뉴로포레 테라피스, 인코포레이티드 | 시누클레인 병을 치료하는데 적합한 화합물 |
| US9198891B2 (en) * | 2010-05-21 | 2015-12-01 | New York University | Method of treating cancer by inhibition of protein kinase-like endoplasmic reticulum protein kinase |
-
2013
- 2013-07-16 CN CN201380038158.1A patent/CN104703604A/zh active Pending
- 2013-07-16 HK HK15111382.6A patent/HK1210598A1/xx unknown
- 2013-07-16 MX MX2015000618A patent/MX2015000618A/es unknown
- 2013-07-16 WO PCT/US2013/050719 patent/WO2014014937A1/en not_active Ceased
- 2013-07-16 EP EP13820320.3A patent/EP2872143B1/en active Active
- 2013-07-16 US US14/415,120 patent/US9284309B2/en active Active
- 2013-07-16 BR BR112015001096A patent/BR112015001096A2/pt not_active Application Discontinuation
- 2013-07-16 KR KR20157004215A patent/KR20150031481A/ko not_active Withdrawn
- 2013-07-16 RU RU2015104962A patent/RU2015104962A/ru not_active Application Discontinuation
- 2013-07-16 CA CA2877983A patent/CA2877983A1/en not_active Abandoned
- 2013-07-16 ES ES13820320.3T patent/ES2661394T3/es active Active
- 2013-07-16 AU AU2013290361A patent/AU2013290361A1/en not_active Abandoned
- 2013-07-16 JP JP2015523185A patent/JP2015522617A/ja active Pending
-
2015
- 2015-01-14 IL IL236712A patent/IL236712A0/en unknown
- 2015-02-12 IN IN1171DEN2015 patent/IN2015DN01171A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20150183776A1 (en) | 2015-07-02 |
| CN104703604A (zh) | 2015-06-10 |
| ES2661394T3 (es) | 2018-03-28 |
| EP2872143B1 (en) | 2017-12-13 |
| MX2015000618A (es) | 2015-04-10 |
| CA2877983A1 (en) | 2014-01-23 |
| US9284309B2 (en) | 2016-03-15 |
| EP2872143A1 (en) | 2015-05-20 |
| AU2013290361A1 (en) | 2015-02-05 |
| BR112015001096A2 (pt) | 2017-06-27 |
| IN2015DN01171A (https=) | 2015-06-26 |
| JP2015522617A (ja) | 2015-08-06 |
| EP2872143A4 (en) | 2015-12-02 |
| IL236712A0 (en) | 2015-02-26 |
| WO2014014937A1 (en) | 2014-01-23 |
| KR20150031481A (ko) | 2015-03-24 |
| HK1210598A1 (en) | 2016-04-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20171017 |