CN102844313B - 提高蛋白酶体活性的组合物和方法 - Google Patents
提高蛋白酶体活性的组合物和方法 Download PDFInfo
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- CN102844313B CN102844313B CN201180016116.9A CN201180016116A CN102844313B CN 102844313 B CN102844313 B CN 102844313B CN 201180016116 A CN201180016116 A CN 201180016116A CN 102844313 B CN102844313 B CN 102844313B
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- epoxide
- alkyl
- sulfinyl
- carbonyl
- sulfonyl
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- 0 CC(C)C1NC1C*1CCCC1 Chemical compound CC(C)C1NC1C*1CCCC1 0.000 description 4
- CZTVXRSMLZRUMJ-UHFFFAOYSA-N CC(C)c(ccc(F)c1)c1F Chemical compound CC(C)c(ccc(F)c1)c1F CZTVXRSMLZRUMJ-UHFFFAOYSA-N 0.000 description 1
- NIHOFUPGUVQJBQ-UHFFFAOYSA-N CCc(ccc(F)c1)c1Cl Chemical compound CCc(ccc(F)c1)c1Cl NIHOFUPGUVQJBQ-UHFFFAOYSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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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- A—HUMAN NECESSITIES
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- 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
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/333—Radicals substituted by oxygen or sulfur atoms
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/335—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
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- 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
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- 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
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- 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
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- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
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- C—CHEMISTRY; METALLURGY
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- 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
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- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
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- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
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- G01N2333/90—Enzymes; Proenzymes
- G01N2333/914—Hydrolases (3)
- G01N2333/948—Hydrolases (3) acting on peptide bonds (3.4)
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- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Ophthalmology & Optometry (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biochemistry (AREA)
- Analytical Chemistry (AREA)
- Biotechnology (AREA)
- Cell Biology (AREA)
- Microbiology (AREA)
- General Physics & Mathematics (AREA)
- Pathology (AREA)
- Food Science & Technology (AREA)
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33695910P | 2010-01-28 | 2010-01-28 | |
| US61/336,959 | 2010-01-28 | ||
| US37340410P | 2010-08-13 | 2010-08-13 | |
| US61/373,404 | 2010-08-13 | ||
| PCT/US2011/022929 WO2011094545A2 (en) | 2010-01-28 | 2011-01-28 | Compositions and methods for enhancing proteasome activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102844313A CN102844313A (zh) | 2012-12-26 |
| CN102844313B true CN102844313B (zh) | 2016-10-05 |
Family
ID=44320152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180016116.9A Expired - Fee Related CN102844313B (zh) | 2010-01-28 | 2011-01-28 | 提高蛋白酶体活性的组合物和方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US20130045992A1 (OSRAM) |
| EP (1) | EP2528911B1 (OSRAM) |
| JP (2) | JP2013518129A (OSRAM) |
| KR (1) | KR20120117905A (OSRAM) |
| CN (1) | CN102844313B (OSRAM) |
| AU (1) | AU2011210765A1 (OSRAM) |
| BR (1) | BR112012018631A8 (OSRAM) |
| CA (1) | CA2787785C (OSRAM) |
| MX (1) | MX336731B (OSRAM) |
| RU (1) | RU2012136451A (OSRAM) |
| SG (1) | SG182662A1 (OSRAM) |
| WO (1) | WO2011094545A2 (OSRAM) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG182662A1 (en) | 2010-01-28 | 2012-08-30 | Harvard College | Compositions and methods for enhancing proteasome activity |
| JP6042331B2 (ja) | 2010-07-23 | 2016-12-14 | プレジデント アンド フェローズ オブ ハーバード カレッジ | プロテアソーム活性を向上させる三環系化合物 |
| WO2012154967A1 (en) * | 2011-05-12 | 2012-11-15 | Proteostasis Therapeutics, Inc. | Proteostasis regulators |
| US9856511B2 (en) | 2011-09-16 | 2018-01-02 | Vivolux Ab | Protease deubiquitinating inhibitor screening |
| EP2806875B1 (en) * | 2012-01-25 | 2017-07-19 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating compounds |
| EP2938610A2 (en) | 2012-12-28 | 2015-11-04 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof |
| US9849135B2 (en) | 2013-01-25 | 2017-12-26 | President And Fellows Of Harvard College | USP14 inhibitors for treating or preventing viral infections |
| US10563225B2 (en) * | 2013-07-26 | 2020-02-18 | President And Fellows Of Harvard College | Genome engineering |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| EA031804B1 (ru) | 2014-02-03 | 2019-02-28 | Вайтаи Фармасьютиклз, Инк. | Дигидропирролопиридиновые ингибиторы ror-гамма |
| CN104844704B (zh) * | 2014-02-17 | 2018-02-23 | 华东师范大学 | Ub‑Nanoluc、Ub‑Ub‑GS‑Nanoluc报告基因系统及其构建和应用 |
| SI3207043T1 (sl) | 2014-10-14 | 2019-04-30 | Vitae Pharmaceuticals, Inc. | Dihidropirolopiridinovi inhibitorji za ROR-gama |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
| CN104478780B (zh) * | 2014-11-17 | 2017-04-19 | 华东师范大学 | 酰基吡咯类小分子有机化合物及其衍生物、用途及其制备方法 |
| WO2017024018A1 (en) | 2015-08-05 | 2017-02-09 | Vitae Pharmaceuticals, Inc. | Modulators of ror-gamma |
| CN108463458B (zh) | 2015-11-20 | 2022-02-01 | 生命医药有限责任公司 | ROR-γ的调节剂 |
| GB201521109D0 (en) * | 2015-11-30 | 2016-01-13 | Mission Therapeutics Ltd | Novel compounds |
| CA3010615C (en) | 2016-01-14 | 2024-02-20 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
| TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ROR-γ調節劑 |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| WO2017197055A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| CN106065389A (zh) * | 2016-08-08 | 2016-11-02 | 山东理工大学 | 一种促进木瓜蛋白酶活性的方法及其在啤酒澄清中的应用 |
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| JP2016147893A (ja) | 2016-08-18 |
| EP2528911A4 (en) | 2014-08-06 |
| JP2013518129A (ja) | 2013-05-20 |
| CA2787785A1 (en) | 2011-08-04 |
| US20130045992A1 (en) | 2013-02-21 |
| WO2011094545A3 (en) | 2012-01-05 |
| US10351568B2 (en) | 2019-07-16 |
| WO2011094545A2 (en) | 2011-08-04 |
| JP6371786B2 (ja) | 2018-08-08 |
| MX336731B (es) | 2016-01-28 |
| MX2012008626A (es) | 2012-08-15 |
| RU2012136451A (ru) | 2014-03-10 |
| EP2528911A2 (en) | 2012-12-05 |
| BR112012018631A8 (pt) | 2017-12-19 |
| BR112012018631A2 (pt) | 2016-04-05 |
| KR20120117905A (ko) | 2012-10-24 |
| CN102844313A (zh) | 2012-12-26 |
| CA2787785C (en) | 2018-03-06 |
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