JP2013518129A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013518129A5 JP2013518129A5 JP2012551323A JP2012551323A JP2013518129A5 JP 2013518129 A5 JP2013518129 A5 JP 2013518129A5 JP 2012551323 A JP2012551323 A JP 2012551323A JP 2012551323 A JP2012551323 A JP 2012551323A JP 2013518129 A5 JP2013518129 A5 JP 2013518129A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- proteasome
- fluoroalkyl
- haloalkyl
- compound according
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 30
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 claims 18
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 claims 18
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 15
- 125000001188 haloalkyl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 14
- 239000012453 solvate Substances 0.000 claims 14
- 229940002612 prodrug Drugs 0.000 claims 13
- 239000000651 prodrug Substances 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 238000000034 method Methods 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 101100371648 Caenorhabditis elegans usp-14 gene Proteins 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- -1 4-methylpiperidin-1-yl Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- JUWDSDKJBMFLHE-UHFFFAOYSA-N 1-[1-(4-fluorophenyl)-2,5-dimethylpyrrol-3-yl]-2-pyrrolidin-1-ylethanone Chemical compound CC=1N(C=2C=CC(F)=CC=2)C(C)=CC=1C(=O)CN1CCCC1 JUWDSDKJBMFLHE-UHFFFAOYSA-N 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 241001529936 Murinae Species 0.000 claims 2
- 102000007056 Recombinant Fusion Proteins Human genes 0.000 claims 2
- 108010008281 Recombinant Fusion Proteins Proteins 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- ICCBZGUDUOMNOF-UHFFFAOYSA-N azidoamine Chemical compound NN=[N+]=[N-] ICCBZGUDUOMNOF-UHFFFAOYSA-N 0.000 claims 2
- 230000009504 deubiquitination Effects 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 239000000758 substrate Substances 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000005090 alkenylcarbonyl group Chemical group 0.000 claims 1
- 125000005193 alkenylcarbonyloxy group Chemical group 0.000 claims 1
- 125000003302 alkenyloxy group Chemical group 0.000 claims 1
- 125000005092 alkenyloxycarbonyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000005087 alkynylcarbonyl group Chemical group 0.000 claims 1
- 125000005198 alkynylcarbonyloxy group Chemical group 0.000 claims 1
- 125000005133 alkynyloxy group Chemical group 0.000 claims 1
- 125000005225 alkynyloxycarbonyl group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000001091 aminosulfinyl group Chemical group [H]N([H])S(*)=O 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 150000005347 biaryls Chemical group 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 125000004993 haloalkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004692 haloalkylcarbonyl group Chemical group 0.000 claims 1
- 125000005203 haloalkylcarbonyloxy group Chemical group 0.000 claims 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 125000005322 morpholin-1-yl group Chemical group 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- LFGREXWGYUGZLY-UHFFFAOYSA-N phosphoryl Chemical group [P]=O LFGREXWGYUGZLY-UHFFFAOYSA-N 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000017854 proteolysis Effects 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 125000004469 siloxy group Chemical group [SiH3]O* 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016060063A Division JP6371786B2 (ja) | 2010-01-28 | 2016-03-24 | プロテアソーム活性を向上させるための組成物および方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013518129A JP2013518129A (ja) | 2013-05-20 |
| JP2013518129A5 true JP2013518129A5 (enExample) | 2013-12-26 |
Family
ID=44320152
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012551323A Pending JP2013518129A (ja) | 2010-01-28 | 2011-01-28 | プロテアソーム活性を向上させるための組成物および方法 |
| JP2016060063A Expired - Fee Related JP6371786B2 (ja) | 2010-01-28 | 2016-03-24 | プロテアソーム活性を向上させるための組成物および方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016060063A Expired - Fee Related JP6371786B2 (ja) | 2010-01-28 | 2016-03-24 | プロテアソーム活性を向上させるための組成物および方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US20130045992A1 (enExample) |
| EP (1) | EP2528911B1 (enExample) |
| JP (2) | JP2013518129A (enExample) |
| KR (1) | KR20120117905A (enExample) |
| CN (1) | CN102844313B (enExample) |
| AU (1) | AU2011210765A1 (enExample) |
| BR (1) | BR112012018631A8 (enExample) |
| CA (1) | CA2787785C (enExample) |
| MX (1) | MX336731B (enExample) |
| RU (1) | RU2012136451A (enExample) |
| SG (1) | SG182662A1 (enExample) |
| WO (1) | WO2011094545A2 (enExample) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2012136451A (ru) | 2010-01-28 | 2014-03-10 | Президент Энд Феллоуз Оф Гарвард Колледж | Композиции и способы улучшения активности протеасомы |
| AU2011281015B2 (en) | 2010-07-23 | 2015-09-24 | President And Fellows Of Harvard College | Tricyclic proteasome activity enhancing compounds |
| JP6208122B2 (ja) | 2011-05-12 | 2017-10-04 | プロテオステイシス セラピューティクス，インコーポレイテッド | プロテオスタシス調節因子 |
| JP6103722B2 (ja) * | 2011-09-16 | 2017-03-29 | ヴィヴォルックス アーベー | プロテアソーム脱ユビキチン化阻害剤スクリーニング |
| CA2861464C (en) | 2012-01-25 | 2018-03-06 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating tricyclic 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 |
| US11306328B2 (en) * | 2013-07-26 | 2022-04-19 | President And Fellows Of Harvard College | Genome engineering |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| RS59007B1 (sr) | 2014-02-03 | 2019-08-30 | Vitae Pharmaceuticals Llc | Dihidropirolopiridinski inhibitori ror-gama |
| 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 |
| EA031967B1 (ru) | 2014-10-14 | 2019-03-29 | Вайтаи Фармасьютиклз, Инк. | ДИГИДРОПИРРОЛОПИРИДИНОВЫЕ ИНГИБИТОРЫ ROR-γ |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine 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 |
| KR20180086221A (ko) | 2015-11-20 | 2018-07-30 | 비타이 파마슈티컬즈, 인코포레이티드 | Ror-감마의 조절물질 |
| GB201521109D0 (en) * | 2015-11-30 | 2016-01-13 | Mission Therapeutics Ltd | Novel compounds |
| WO2017123826A1 (en) | 2016-01-14 | 2017-07-20 | 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 |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| 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 |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | 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 |
| CN106281935A (zh) * | 2016-08-08 | 2017-01-04 | 山东理工大学 | 一种促进中性蛋白酶活性的方法及其在啤酒澄清中的应用 |
| CN107903208B (zh) * | 2016-12-26 | 2021-09-03 | 杭州市西溪医院 | 一类联芳吡啶类去泛素化酶抑制剂、其制备方法及应用 |
| WO2018237026A1 (en) | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| MA49685A (fr) | 2017-07-24 | 2021-04-14 | Vitae Pharmaceuticals Llc | INHIBITEURS DE ROR gamma |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| JP2021519337A (ja) | 2018-03-26 | 2021-08-10 | シー４ セラピューティクス， インコーポレイテッド | Ｉｋａｒｏｓの分解のためのセレブロン結合剤 |
| CN119751456A (zh) | 2018-04-16 | 2025-04-04 | C4医药公司 | 螺环化合物 |
| MA53014A (fr) * | 2018-06-27 | 2021-05-05 | Proteostasis Therapeutics Inc | Composés améliorant l'activité du protéasome |
| EP3814336A1 (en) * | 2018-06-27 | 2021-05-05 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| WO2020132561A1 (en) | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
| WO2021146386A1 (en) * | 2020-01-14 | 2021-07-22 | The Trustees Of Columbia University In The City Of New York | Compositions and methods for targeted protein stabilization by redirecting endogenous deubiquitinases |
| JP2022012379A (ja) * | 2020-07-01 | 2022-01-17 | 国立大学法人富山大学 | ユビキチン－プロテアソーム系の活性化剤、およびその利用 |
| WO2022250363A1 (ko) * | 2021-05-24 | 2022-12-01 | 재단법인대구경북과학기술원 | 아이유원 계열의 유비퀴틴 특이적 프로테아제 14 억제제를 유효성분으로 포함하는, 프로탁의 항암 효과 증진용 약학적 조성물 |
| WO2025219559A1 (en) * | 2024-04-18 | 2025-10-23 | Booster Therapeutics Gmbh | Pyrrolidine compounds as proteasome stimulators |
| CN119707772B (zh) * | 2024-12-23 | 2025-09-02 | 浙江大学 | 一种usp14共价抑制剂及其制备方法和应用 |
Family Cites Families (122)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2557341A1 (de) * | 1975-12-19 | 1977-06-30 | Hoechst Ag | Basisch substituierte indolderivate und verfahren zu ihrer herstellung |
| BR8008732A (pt) | 1979-06-28 | 1981-04-28 | Ciba Geigy Ag | Estabilizadores para compostos termoplasticos clorados |
| NL8701682A (nl) | 1986-07-30 | 1988-02-16 | Sandoz Ag | Werkwijze voor het therapeutisch toepassen van serotonine antagonisten, aktieve verbindingen en farmaceutische preparaten die deze verbindingen bevatten. |
| TW226019B (enExample) | 1992-03-23 | 1994-07-01 | Sankyo Co | |
| DE4325204C2 (de) | 1993-07-27 | 2002-11-28 | Matthias Lehr | Acylpyrrolalkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶ |
| US5852046A (en) | 1993-08-03 | 1998-12-22 | Hoechst Aktiengesellschaft | Benzo-fused heterocyclic compounds having a 5-membered ring processes for their preparation their use as medicaments their use as diagnostic agents and medicaments containing them |
| EP0639573A1 (de) | 1993-08-03 | 1995-02-22 | Hoechst Aktiengesellschaft | Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament |
| JPH07133274A (ja) | 1993-11-09 | 1995-05-23 | Sankyo Co Ltd | ピロール誘導体 |
| DE4338770A1 (de) | 1993-11-12 | 1995-05-18 | Matthias Dr Lehr | Indol-2-alkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶ |
| ATE229020T1 (de) | 1994-01-19 | 2002-12-15 | Sankyo Co | Pyrrolopyridazin-derivate |
| US6201129B1 (en) | 1995-02-01 | 2001-03-13 | Univ. College Cardiff Consultants | Tricyclic derivatives and their use as anti-cancer agents |
| EP0891339A1 (en) | 1996-04-03 | 1999-01-20 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5859035A (en) | 1996-04-03 | 1999-01-12 | Merck & Co., Inc. | Arylheteroaryl inhibitors of farnesyl-protein transferase |
| DE19622222A1 (de) | 1996-06-03 | 1997-12-04 | Hoechst Ag | Verwendung von Inhibitoren des zellulären Na·+·/H·+·-Exchangers (NHE) zur Herstellung eines Medikament zur Normalisierung der Serumlipide |
| US20040122096A1 (en) | 1996-06-03 | 2004-06-24 | Hoechst Aktiengesellschaft | Use of inhibitors of the cellular Na+/H+ exchanger (NHE) for preparing a medicament for normalizing serum lipids |
| KR100482268B1 (ko) | 1996-08-01 | 2005-04-14 | 메르클레 게엠베하 | 세포질 포스포리파제 ａ2의 저해제로서의 아실피롤디카르복실산 |
| US5998462A (en) | 1996-12-16 | 1999-12-07 | Allelix Biopharmaceuticals Inc. | 5-alkyl indole compounds |
| EA200000873A1 (ru) | 1998-02-25 | 2001-04-23 | Дженетикс Инститьют, Инк. | Ингибиторы фосфолипазы a |
| US6828344B1 (en) | 1998-02-25 | 2004-12-07 | Genetics Institute, Llc | Inhibitors of phospholipase enzymes |
| US6500853B1 (en) | 1998-02-28 | 2002-12-31 | Genetics Institute, Llc | Inhibitors of phospholipase enzymes |
| US6867209B1 (en) | 1998-05-22 | 2005-03-15 | Scios, Inc. | Indole-type derivatives as inhibitors of p38 kinase |
| US6589954B1 (en) | 1998-05-22 | 2003-07-08 | Scios, Inc. | Compounds and methods to treat cardiac failure and other disorders |
| AUPP433398A0 (en) | 1998-06-25 | 1998-07-16 | Australian National University, The | Compounds and processes |
| JP2000063354A (ja) | 1998-08-21 | 2000-02-29 | Sumitomo Pharmaceut Co Ltd | ピロール誘導体 |
| JP2001151771A (ja) | 1999-09-10 | 2001-06-05 | Kyowa Hakko Kogyo Co Ltd | 含窒素芳香族複素環誘導体 |
| WO2001044182A2 (en) | 1999-12-16 | 2001-06-21 | Eli Lilly And Company | New synthesis of spla2 inhibitors |
| CN1814596A (zh) | 2000-04-28 | 2006-08-09 | 阿卡蒂亚药品公司 | 毒蕈碱性激动剂 |
| ES2172415B2 (es) | 2000-07-28 | 2003-11-16 | Univ Madrid Complutense | Tratamiento del glaucoma y la hipertension ocular por medio de un analogo de la melatonina. |
| WO2002072549A1 (en) | 2001-03-12 | 2002-09-19 | Millennium Pharmaceuticals, Inc. | Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor |
| BR0214020A (pt) | 2001-11-09 | 2004-10-13 | Scios Inc | Método para tratar fibrose cìstica |
| US7528165B2 (en) | 2001-12-13 | 2009-05-05 | National Health Research Institutes | Indole compounds |
| US7632955B2 (en) | 2001-12-13 | 2009-12-15 | National Health Research Institutes | Indole compounds |
| CA2495943C (en) | 2002-08-29 | 2009-07-21 | Merck & Co., Inc. | Indoles having anti-diabetic activity |
| US7482354B2 (en) * | 2003-05-22 | 2009-01-27 | Nerviano Medical Sciences S.R.L. | Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors |
| JP4820169B2 (ja) | 2003-07-15 | 2011-11-24 | 大日本住友製薬株式会社 | 新規ヘテロアリール誘導体 |
| US7576206B2 (en) * | 2003-08-14 | 2009-08-18 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| US7767817B2 (en) | 2003-09-05 | 2010-08-03 | Binghe Wang | Water soluble boronic acid fluorescent reporter compounds and methods of use thereof |
| US20050203063A1 (en) * | 2003-09-12 | 2005-09-15 | Raymond Deshaies | Proteasome pathway inhibitors and related methods |
| TW200522944A (en) | 2003-12-23 | 2005-07-16 | Lilly Co Eli | CB1 modulator compounds |
| US7417063B2 (en) | 2004-04-13 | 2008-08-26 | Bristol-Myers Squibb Company | Bicyclic heterocycles useful as serine protease inhibitors |
| WO2005121175A2 (en) | 2004-06-08 | 2005-12-22 | Novartis Vaccines And Diagnostics Inc. | Env polypeptide complexes and methods of use |
| ES2246721B1 (es) | 2004-08-10 | 2007-03-16 | Laboratorios Del Dr. Esteve, S.A. | Compuestos indolicos sustituidos, su preparacion y su uso como medicamentos. |
| US20090264384A1 (en) | 2004-11-01 | 2009-10-22 | Nuada, Inc. | Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof |
| US20060135540A1 (en) | 2004-11-30 | 2006-06-22 | Jack Lin | PPAR active compounds |
| GB0500492D0 (en) | 2005-01-11 | 2005-02-16 | Cyclacel Ltd | Compound |
| WO2006075638A1 (ja) | 2005-01-14 | 2006-07-20 | Dainippon Sumitomo Pharma Co., Ltd. | 新規ヘテロアリール誘導体 |
| BRPI0607439A2 (pt) | 2005-02-16 | 2010-04-06 | Solvay Pharm Bv | compostos, composição farmacêutica, método de preparação de composições farmacêuticas, e, uso de um composto |
| WO2006125324A1 (en) | 2005-05-27 | 2006-11-30 | Queen's University At Kingston | Treatment of protein folding disorders |
| MX2008003202A (es) | 2005-09-16 | 2008-03-25 | Serenex Inc | Derivados de carbazol. |
| EP1783114A1 (en) | 2005-11-03 | 2007-05-09 | Novartis AG | N-(hetero)aryl indole derivatives as pesticides |
| JP2009526863A (ja) | 2006-02-15 | 2009-07-23 | アラーガン、インコーポレイテッド | スフィンゴシン−１−リン酸（ｓ１ｐ）受容体アンタゴニスト生物学的活性を有するアリールまたはヘテロアリール基を持つインドール−３−カルボン酸アミド、エステル、チオアミドおよびチオールエステル化合物 |
| WO2007112322A2 (en) | 2006-03-28 | 2007-10-04 | Allergan, Inc. | Indole compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity |
| US8877791B2 (en) | 2006-08-04 | 2014-11-04 | Beth Israel Deaconess Medical Center, Inc. | Inhibitors of pyruvate kinase and methods of treating disease |
| WO2008019357A2 (en) | 2006-08-07 | 2008-02-14 | Ironwood Pharmaceuticals, Inc. | Indole compounds |
| WO2008024978A2 (en) | 2006-08-24 | 2008-02-28 | Serenex, Inc. | Tetrahydroindolone and tetrahydroindazolone derivatives |
| EP1902733A1 (en) | 2006-09-19 | 2008-03-26 | Laboratorios Del Dr. Esteve, S.A. | Combination of a NMDA-receptor ligand and a compound with 5-HT6 receptor affinity |
| EP2089359A2 (en) | 2006-10-31 | 2009-08-19 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors |
| US8524917B2 (en) | 2007-01-11 | 2013-09-03 | Allergan, Inc. | 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity |
| EP2114876A4 (en) | 2007-02-05 | 2010-12-22 | Amira Pharmaceuticals Inc | INVERSE INDOLES AS INHIBITORS OF THE 5-LIPOXYGENASE ACTIVATION PROTEIN (FLAP) |
| JP2010518125A (ja) | 2007-02-12 | 2010-05-27 | インターミューン・インコーポレーテッド | Ｃ型肝炎ウイルス複製の新規な阻害剤 |
| DE602008002733D1 (de) | 2007-03-08 | 2010-11-04 | Irm Llc | Verbindungen und zusammensetzungen als modulatoren der gpr119-aktivität |
| CN101016294A (zh) | 2007-03-13 | 2007-08-15 | 中国人民武装警察部队医学院 | 具有多种生物活性的取代吲哚－3－基草酰胺衍生物 |
| US8293781B2 (en) | 2007-03-29 | 2012-10-23 | Daiichi Sankyo Company, Limited | Indole derivatives having cPLA2 inhibiting activity and applications and production methods of the same |
| US8091582B2 (en) | 2007-04-13 | 2012-01-10 | Cla-Val Co. | System and method for hydraulically managing fluid pressure downstream from a main valve between set points |
| WO2008133867A1 (en) | 2007-04-26 | 2008-11-06 | Merck & Co., Inc. | 2-substituted indole derivatives as calcium channel blockers |
| US8563594B2 (en) | 2007-05-08 | 2013-10-22 | Allergan, Inc. | S1P3 receptor inhibitors for treating pain |
| WO2008147536A1 (en) * | 2007-05-24 | 2008-12-04 | President And Fellows For Harvard College | Methods and compositions for enhancing proteasome activity |
| WO2008157740A2 (en) | 2007-06-20 | 2008-12-24 | Ironwood Pharmaceuticals, Inc. | Faah inhibitors |
| EP2018861A1 (en) | 2007-07-26 | 2009-01-28 | Laboratorios del Dr. Esteve S.A. | 5HT6-Ligands such as sulfonamide derivatives in drug-induced weight-gain |
| ATE495737T1 (de) | 2007-08-01 | 2011-02-15 | Esteve Labor Dr | Kombination von mindestens zwei 5-ht6-liganden |
| CA2705303A1 (en) | 2007-11-07 | 2009-05-14 | Foldrx Pharmaceuticals, Inc. | Modulation of protein trafficking |
| CA2932121A1 (en) | 2007-11-30 | 2009-06-11 | Newlink Genetics Corporation | Ido inhibitors |
| JP5301557B2 (ja) | 2007-12-04 | 2013-09-25 | エフ．ホフマン−ラ ロシュ アーゲー | イソオキサゾロ−ピリジン誘導体 |
| GB0723815D0 (en) | 2007-12-05 | 2008-01-16 | Glaxo Group Ltd | Compounds |
| AU2008345225A1 (en) * | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| JP2009179589A (ja) | 2008-01-30 | 2009-08-13 | Pharma Ip | 抗ウイルス剤 |
| EP2259679A4 (en) | 2008-01-31 | 2011-09-14 | Joslin Diabetes Ct | METHODS OF TREATING KALLIKREIN RELATED DISORDERS |
| WO2009108551A2 (en) | 2008-02-25 | 2009-09-03 | H. Lundbeck A/S | Heteroaryl amide analogues |
| RU2503676C2 (ru) | 2008-02-25 | 2014-01-10 | Ф.Хоффманн-Ля Рош Аг | Пирролопиразиновые ингибиторы киназы |
| US20110009453A1 (en) | 2008-03-17 | 2011-01-13 | Donello John E | s1p3 receptor inhibitors for treating inflammation |
| CN102036558A (zh) | 2008-03-20 | 2011-04-27 | 森林实验室控股有限公司 | 作为硬脂酰-CoA去饱和酶抑制剂的新颖哌啶衍生物 |
| AU2009228765B2 (en) * | 2008-03-24 | 2012-05-31 | Novartis Ag | Arylsulfonamide-based matrix metalloprotease inhibitors |
| US20110098483A1 (en) | 2008-03-27 | 2011-04-28 | University Of Southern California | Substituted Nitrogen Heterocycles and Synthesis and Uses Thereof |
| MX2010011408A (es) | 2008-04-16 | 2010-12-20 | Karobio Ab | Ligandos de receptor de estrogeno novedosos. |
| PL2283006T3 (pl) | 2008-04-24 | 2015-08-31 | F2G Ltd | Pirolowe środki przeciwgrzybicze |
| GB0808282D0 (en) | 2008-05-07 | 2008-06-11 | Medical Res Council | Compounds for use in stabilizing p53 mutants |
| WO2009158011A1 (en) | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| WO2009158371A1 (en) | 2008-06-26 | 2009-12-30 | Smithklike Beecham Corporation | Inhibitors of akt activity |
| EP2141163A1 (de) | 2008-07-02 | 2010-01-06 | Bayer Schering Pharma AG | Substituierte Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel |
| US20110237538A1 (en) | 2008-08-06 | 2011-09-29 | Summit Corporation Plc | Treatment of lysosomal storage disorders and other proteostatic diseases |
| US8426598B2 (en) | 2008-08-12 | 2013-04-23 | Merck, Sharp & Dohme, Corp. | N-heterocyclic M1 receptor positive allosteric modulators |
| US8143269B2 (en) | 2008-10-03 | 2012-03-27 | Calcimedica, Inc. | Inhibitors of store operated calcium release |
| TW201026695A (en) | 2008-12-12 | 2010-07-16 | Astrazeneca Ab | Piperidine compounds and uses thereof-596 |
| US8637507B2 (en) | 2009-03-18 | 2014-01-28 | Merck Sharp & Dohme Corp. | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
| WO2010129553A1 (en) | 2009-05-05 | 2010-11-11 | Allergan, Inc. | S1p3 receptor inhibitors for treating conditions of the eye |
| US8912220B2 (en) | 2009-08-10 | 2014-12-16 | Galenea Pharmaceuticals | Compounds and methods of use thereof |
| CN102216300B (zh) | 2009-09-30 | 2014-10-22 | 贝达药业股份有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| AU2010308306A1 (en) | 2009-10-19 | 2012-05-10 | Synta Pharmaceuticals Corp. | Combination cancer therapy with HSP90 inhibitory compounds |
| RU2012136451A (ru) | 2010-01-28 | 2014-03-10 | Президент Энд Феллоуз Оф Гарвард Колледж | Композиции и способы улучшения активности протеасомы |
| WO2011127333A2 (en) | 2010-04-09 | 2011-10-13 | University Of Louisville Research Foundation, Inc. | Compounds for treating disease, for administering, and for pharmaceutical compositions |
| EP2560640A1 (en) | 2010-04-19 | 2013-02-27 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a hsp90 inhibitory compounds and a egfr inhibitor |
| US20130156755A1 (en) | 2010-04-19 | 2013-06-20 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a hsp90 inhibitory compounds and a vegf inhibitor |
| WO2011149824A1 (en) | 2010-05-24 | 2011-12-01 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a hsp90 inhibitory compound and a topoisomerase ii inhibitor |
| AU2011281015B2 (en) * | 2010-07-23 | 2015-09-24 | President And Fellows Of Harvard College | Tricyclic proteasome activity enhancing compounds |
| WO2012037072A1 (en) | 2010-09-13 | 2012-03-22 | Synta Pharmaceuticals Corporation | Hsp90 inhibitors for treating non-small cell lung cancers in wild-type egfr and/or kras patients |
| US20140005145A1 (en) | 2010-12-08 | 2014-01-02 | Synta Pharmaceuticals Corp. | Combination breast cancer therapy with hsp90 inhibitory compounds |
| WO2012096919A1 (en) | 2011-01-11 | 2012-07-19 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with proteasome inhibitors |
| WO2012106343A2 (en) | 2011-02-01 | 2012-08-09 | The Board Of Trustees Of The University Of Illinois | Hdac inhibitors and therapeutic methods using the same |
| EP2678013A1 (en) | 2011-02-23 | 2014-01-01 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with radiotherapy |
| JP2014507443A (ja) | 2011-02-24 | 2014-03-27 | シンタ ファーマシューティカルズ コーポレーション | Ｈｓｐ９０阻害化合物での前立腺癌治療 |
| WO2012116247A1 (en) | 2011-02-25 | 2012-08-30 | Synta Pharmaceuticals Corp. | Hsp90 inhibitory compounds in treating jak/stat signaling-mediated cancers |
| JP6208122B2 (ja) | 2011-05-12 | 2017-10-04 | プロテオステイシス セラピューティクス，インコーポレイテッド | プロテオスタシス調節因子 |
| US20140228418A1 (en) | 2011-05-23 | 2014-08-14 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with mek inhibitors |
| US20140315943A1 (en) | 2011-05-24 | 2014-10-23 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with mtor/p13k inhibitors |
| US20140194388A1 (en) | 2011-05-26 | 2014-07-10 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with chk inhibitors |
| EP2714680B1 (en) | 2011-05-27 | 2015-11-25 | Amira Pharmaceuticals, Inc. | Heterocyclic autotaxin inhibitors and uses thereof |
| AU2012280931A1 (en) | 2011-07-07 | 2014-02-27 | Synta Pharmaceuticals Corp. | Treating cancer with HSP90 inhibitory compounds |
| ES2461997T3 (es) | 2011-07-22 | 2014-05-22 | Université Joseph Fourier | Derivados bis-indólicos nuevos, sus usos, en particular como antibacterianos |
| WO2013067162A1 (en) | 2011-11-02 | 2013-05-10 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of hsp90 inhibitors with topoisomerase i inhibitors |
| JP2014534228A (ja) | 2011-11-02 | 2014-12-18 | シンタ ファーマシューティカルズ コーポレーション | 白金含有剤とｈｓｐ９０阻害剤の組合せ療法 |
| CA2854188A1 (en) | 2011-11-14 | 2013-05-23 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitors with braf inhibitors |
| US9849135B2 (en) | 2013-01-25 | 2017-12-26 | President And Fellows Of Harvard College | USP14 inhibitors for treating or preventing viral infections |
-
2011
- 2011-01-28 RU RU2012136451/04A patent/RU2012136451A/ru not_active Application Discontinuation
- 2011-01-28 MX MX2012008626A patent/MX336731B/es unknown
- 2011-01-28 CN CN201180016116.9A patent/CN102844313B/zh not_active Expired - Fee Related
- 2011-01-28 SG SG2012054235A patent/SG182662A1/en unknown
- 2011-01-28 JP JP2012551323A patent/JP2013518129A/ja active Pending
- 2011-01-28 EP EP11737731.7A patent/EP2528911B1/en not_active Not-in-force
- 2011-01-28 AU AU2011210765A patent/AU2011210765A1/en not_active Abandoned
- 2011-01-28 US US13/575,812 patent/US20130045992A1/en not_active Abandoned
- 2011-01-28 BR BR112012018631A patent/BR112012018631A8/pt not_active Application Discontinuation
- 2011-01-28 KR KR1020127022300A patent/KR20120117905A/ko not_active Ceased
- 2011-01-28 CA CA2787785A patent/CA2787785C/en not_active Expired - Fee Related
- 2011-01-28 WO PCT/US2011/022929 patent/WO2011094545A2/en not_active Ceased
-
2015
- 2015-11-05 US US14/933,671 patent/US10351568B2/en not_active Expired - Fee Related
-
2016
- 2016-03-24 JP JP2016060063A patent/JP6371786B2/ja not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013518129A5 (enExample) | ||
| RU2012136451A (ru) | Композиции и способы улучшения активности протеасомы | |
| JP2011513305A5 (enExample) | ||
| CA2565813A1 (en) | Substituted methyl aryl or heteroaryl amide compounds | |
| JP2014506599A5 (enExample) | ||
| JP2013542996A5 (enExample) | ||
| JP2011512412A5 (enExample) | ||
| JP2012528166A5 (enExample) | ||
| RU2013108641A (ru) | Способ лечения офтальмологических заболеваний с использованием соединений ингибиторов киназы в пролекарственных формах | |
| JP2012501312A5 (enExample) | ||
| CA2652834A1 (en) | Substituted arylimidazolones and -triazolones and the use thereof | |
| JP2013533317A5 (enExample) | ||
| JP2012523457A5 (enExample) | ||
| RU2012129168A (ru) | Производные оксазина | |
| NO20072371L (no) | Kinuklidinderivater og deres anvendelse som muskarine M3-reseptorantagonister | |
| NZ592297A (en) | 2-Aryl-5-heteroaryl pyridine and pyrimidine derivatives as pharmaceutical active agents | |
| JP2018519323A5 (enExample) | ||
| JP2011502958A5 (enExample) | ||
| RU2007128322A (ru) | Циклические производные пиррола | |
| NZ593030A (en) | Pyridyloxyindoles inhibitors of vegf-r2 and use thereof for treatment of disease | |
| NO20091590L (no) | Heterocykliske amidforbindelser anvendbare som kinaseinhibitorer | |
| JP2013529210A5 (enExample) | ||
| CA2409741A1 (en) | Tnf-.alpha. production inhibitors | |
| JP2010515750A5 (enExample) | ||
| CA3120351A1 (en) | Aryl-aniline and heteroaryl-aniline compounds for treatment of skin cancers |