JP2017515857A5 - - Google Patents
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- JP2017515857A5 JP2017515857A5 JP2016567656A JP2016567656A JP2017515857A5 JP 2017515857 A5 JP2017515857 A5 JP 2017515857A5 JP 2016567656 A JP2016567656 A JP 2016567656A JP 2016567656 A JP2016567656 A JP 2016567656A JP 2017515857 A5 JP2017515857 A5 JP 2017515857A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- composition
- compound according
- alkyl
- ring
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 63
- 125000000217 alkyl group Chemical group 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 26
- 239000000203 mixture Substances 0.000 claims description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- 239000001257 hydrogen Substances 0.000 claims description 23
- 150000002367 halogens Chemical class 0.000 claims description 22
- 206010028980 Neoplasm Diseases 0.000 claims description 17
- 201000011510 cancer Diseases 0.000 claims description 17
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 12
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 12
- 125000005842 heteroatom Chemical group 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 12
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- 239000001301 oxygen Chemical group 0.000 claims description 12
- 229910052717 sulfur Chemical group 0.000 claims description 12
- 239000011593 sulfur Chemical group 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000000623 heterocyclic group Chemical group 0.000 claims description 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 8
- 125000004043 oxo group Chemical group O=* 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims description 7
- 125000002541 furyl group Chemical group 0.000 claims description 6
- 150000002431 hydrogen Chemical group 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 102000011727 Caspases Human genes 0.000 claims description 5
- 108010076667 Caspases Proteins 0.000 claims description 5
- 230000000694 effects Effects 0.000 claims description 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 4
- 101100507655 Canis lupus familiaris HSPA1 gene Proteins 0.000 claims description 4
- 125000001931 aliphatic group Chemical group 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 238000003556 assay Methods 0.000 claims description 3
- 238000003776 cleavage reaction Methods 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 230000007017 scission Effects 0.000 claims description 3
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 230000003213 activating effect Effects 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 230000006907 apoptotic process Effects 0.000 claims description 2
- 230000004663 cell proliferation Effects 0.000 claims description 2
- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000001939 inductive effect Effects 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 17
- 230000003834 intracellular effect Effects 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461992838P | 2014-05-13 | 2014-05-13 | |
| US61/992,838 | 2014-05-13 | ||
| PCT/US2015/030641 WO2015175707A1 (en) | 2014-05-13 | 2015-05-13 | Hsp70 modulators and methods for making and using the same |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017515857A JP2017515857A (ja) | 2017-06-15 |
| JP2017515857A5 true JP2017515857A5 (OSRAM) | 2018-06-21 |
| JP6607870B2 JP6607870B2 (ja) | 2019-11-20 |
Family
ID=53284541
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567656A Expired - Fee Related JP6607870B2 (ja) | 2014-05-13 | 2015-05-13 | Ｈｓｐ７０モジュレーターならびにその作製および使用方法 |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US9878987B2 (OSRAM) |
| EP (1) | EP3143013B1 (OSRAM) |
| JP (1) | JP6607870B2 (OSRAM) |
| KR (1) | KR102461419B1 (OSRAM) |
| CN (1) | CN107074806B (OSRAM) |
| AU (1) | AU2015259173B2 (OSRAM) |
| BR (1) | BR112016026470A8 (OSRAM) |
| CA (1) | CA2948621A1 (OSRAM) |
| EA (1) | EA201692155A1 (OSRAM) |
| ES (1) | ES2774975T3 (OSRAM) |
| IL (1) | IL248792B (OSRAM) |
| MX (1) | MX375924B (OSRAM) |
| PH (1) | PH12016502244A1 (OSRAM) |
| SG (1) | SG11201609336PA (OSRAM) |
| TW (1) | TWI699204B (OSRAM) |
| WO (1) | WO2015175707A1 (OSRAM) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2608670T3 (es) | 2009-08-17 | 2017-04-12 | Memorial Sloan-Kettering Cancer Center | Derivados de 2-(pirimidin-5-il)-tiopirimidina como moduladores de Hsp70 y Hsc70 para el tratamiento de trastornos proliferativos |
| EP3143013B1 (en) * | 2014-05-13 | 2019-12-18 | Memorial Sloan Kettering Cancer Center | Hsp70 modulators and methods for making and using the same |
| US20180280397A1 (en) | 2015-10-05 | 2018-10-04 | Memorial Sloan Kettering Cancer Center | Rational combination therapy for the treatment of cancer |
| KR102724968B1 (ko) * | 2018-03-21 | 2024-10-31 | 수조우 푸허 바이오파마 컴퍼니 리미티드 | Shp2 억제제 및 이의 용도 |
| AU2019327006B2 (en) | 2018-08-27 | 2024-02-15 | Sumitomo Pharma Co., Ltd. | Optically active azabicyclic derivative |
Family Cites Families (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB951432A (en) | 1959-03-17 | 1964-03-04 | Wellcome Found | Pyrimidine derivatives and the manufacture thereof |
| US3248393A (en) | 1960-06-23 | 1966-04-26 | Burroughs Wellcome Co | 1, 3-diazaphenothiazines and method |
| GB990857A (en) | 1961-10-13 | 1965-05-05 | Wellcome Found | 1,3-diazaphenothiazines |
| CH605828A5 (OSRAM) | 1974-12-24 | 1978-10-13 | Hoffmann La Roche | |
| US4039543A (en) | 1974-12-24 | 1977-08-02 | Hoffmann-La Roche Inc. | Benzylpyrimidines |
| US4096264A (en) | 1975-12-09 | 1978-06-20 | Merck & Co., Inc. | Certain substituted imidazo [1,2-a] pyridines |
| DE3311703A1 (de) | 1983-03-30 | 1984-10-04 | Bayer Ag, 5090 Leverkusen | Harnstoffderivate |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| EP0495421B1 (en) | 1991-01-15 | 1996-08-21 | Alcon Laboratories, Inc. | Use of carrageenans in topical ophthalmic compositions |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| HUT74464A (en) | 1993-10-12 | 1996-12-30 | Du Pont Merck Pharma | 1n-alkyl-n-arylpyrimidinamines and derivatives thereof, and pharmaceutical compositions containing them |
| DE4423098A1 (de) | 1994-07-01 | 1996-01-04 | Hoechst Ag | Verwendung von Pyrimidingruppen enthaltenden konjugierten Verbindungen als Elektrolumineszenzmaterialien |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| JPH09236070A (ja) | 1996-02-29 | 1997-09-09 | Denso Corp | スタータ |
| US5707930A (en) | 1996-09-16 | 1998-01-13 | Zeneca Limited | 4-cycloalkyl-5-substituted pyrimidine compounds useful as crop protection agents |
| PT1330452E (pt) | 2000-09-20 | 2009-01-22 | Ortho Mcneil Pharm Inc | Derivados de pirazina como moduladores de tirosina-cinases |
| WO2002053557A1 (en) | 2000-12-18 | 2002-07-11 | Actelion Pharmaceuticals Ltd | Novel sulfamides and their use as endothelin receptor antagonists |
| US6423720B1 (en) | 2001-02-01 | 2002-07-23 | Duquesne University Of The Holy Ghost | Pyrimidine compounds and methods for making and using the same |
| US7501429B2 (en) | 2001-04-11 | 2009-03-10 | Queen's University At Kingston | Pyrimidine compounds as anti-ictogenic and/or anti-epileptogenic agents |
| JP4399265B2 (ja) | 2001-12-21 | 2010-01-13 | ヴァーナリス（ケンブリッジ）リミテッド | ３，４−ジアリールピラゾール、および癌の治療におけるそれらの使用 |
| CN103169708B (zh) | 2002-07-29 | 2018-02-02 | 里格尔药品股份有限公司 | 用2,4‑嘧啶二胺化合物治疗或者预防自体免疫性疾病的方法 |
| CA2515841C (en) | 2003-02-13 | 2010-06-01 | Banyu Pharmaceutical Co., Ltd. | Novel 2-pyridine carboxamide derivatives |
| EP1675861B1 (en) | 2003-08-29 | 2015-12-23 | Vernalis (R&D) Ltd. | Pyrimidothiophene compounds |
| US20050070712A1 (en) | 2003-09-26 | 2005-03-31 | Christi Kosogof | Pyrimidine derivatives as ghrelin receptor modulators |
| HRP20120901T1 (hr) | 2004-03-05 | 2012-12-31 | F. Hoffmann - La Roche Ag | Diaminopirimidini kao p2x3 i p2x2/3 |
| US7482350B2 (en) | 2004-05-08 | 2009-01-27 | Neurogen Corporation | 4,5-disubstituted-2-aryl pyrimidines |
| CN101155799A (zh) | 2005-03-16 | 2008-04-02 | 塔格根公司 | 嘧啶化合物和使用方法 |
| WO2007025901A1 (en) * | 2005-09-01 | 2007-03-08 | F. Hoffmann-La Roche Ag | Diaminopyrimidines as p2x3 and p2x2/3 modulators |
| WO2007131034A1 (en) | 2006-05-03 | 2007-11-15 | The Regents Of The University Of Michigan | Pyrimidone derivatives which are modulators of heat shock protein (hsp) 70 |
| JP2008081492A (ja) | 2006-08-31 | 2008-04-10 | Banyu Pharmaceut Co Ltd | オーロラａ選択的阻害作用を有する新規アミノピリジン誘導体 |
| US20080124407A1 (en) | 2006-10-10 | 2008-05-29 | University Of Washington | Inhibiting cyp3a4 induction |
| BRPI0720264B1 (pt) | 2006-12-08 | 2022-03-03 | Novartis Ag | Compostos e composições como inibidores de proteína cinase |
| AU2008210266B2 (en) | 2007-01-31 | 2013-09-05 | Ym Biosciences Australia Pty Ltd | Thiopyrimidine-based compounds and uses thereof |
| WO2008153042A1 (ja) | 2007-06-11 | 2008-12-18 | Kyowa Hakko Kirin Co., Ltd. | 抗腫瘍剤 |
| WO2009023846A2 (en) | 2007-08-15 | 2009-02-19 | The Research Foundation Of State University Of New York | Methods for heat shock protein dependent cancer treatment |
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| PE20091236A1 (es) | 2007-11-22 | 2009-09-16 | Astrazeneca Ab | Derivados de pirimidina como immunomoduladores de tlr7 |
| US20130023497A1 (en) | 2009-06-08 | 2013-01-24 | Chunlin Tao | Triazine Derivatives and their Therapeutical Applications |
| ES2608670T3 (es) | 2009-08-17 | 2017-04-12 | Memorial Sloan-Kettering Cancer Center | Derivados de 2-(pirimidin-5-il)-tiopirimidina como moduladores de Hsp70 y Hsc70 para el tratamiento de trastornos proliferativos |
| CA2890748A1 (en) * | 2012-11-13 | 2014-05-22 | Memorial Sloan-Kettering Cancer Center | Indole compounds and their use as antimicrobials |
| EP3143013B1 (en) * | 2014-05-13 | 2019-12-18 | Memorial Sloan Kettering Cancer Center | Hsp70 modulators and methods for making and using the same |
| EP3310771B1 (en) * | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| AU2016324483B2 (en) * | 2015-09-18 | 2021-07-29 | Memorial Sloan Kettering Cancer Center | Methods and compositions of inhibiting DCN1-UBC12 interaction |
-
2015
- 2015-05-13 EP EP15727138.8A patent/EP3143013B1/en active Active
- 2015-05-13 ES ES15727138T patent/ES2774975T3/es active Active
- 2015-05-13 TW TW104115328A patent/TWI699204B/zh not_active IP Right Cessation
- 2015-05-13 WO PCT/US2015/030641 patent/WO2015175707A1/en not_active Ceased
- 2015-05-13 CN CN201580036973.3A patent/CN107074806B/zh not_active Expired - Fee Related
- 2015-05-13 SG SG11201609336PA patent/SG11201609336PA/en unknown
- 2015-05-13 BR BR112016026470A patent/BR112016026470A8/pt not_active Application Discontinuation
- 2015-05-13 MX MX2016014755A patent/MX375924B/es active IP Right Grant
- 2015-05-13 EA EA201692155A patent/EA201692155A1/ru unknown
- 2015-05-13 AU AU2015259173A patent/AU2015259173B2/en not_active Ceased
- 2015-05-13 US US15/310,142 patent/US9878987B2/en active Active
- 2015-05-13 CA CA2948621A patent/CA2948621A1/en active Pending
- 2015-05-13 JP JP2016567656A patent/JP6607870B2/ja not_active Expired - Fee Related
- 2015-05-13 KR KR1020167034791A patent/KR102461419B1/ko active Active
-
2016
- 2016-11-07 IL IL248792A patent/IL248792B/en active IP Right Grant
- 2016-11-11 PH PH12016502244A patent/PH12016502244A1/en unknown
-
2017
- 2017-12-14 US US15/842,755 patent/US10160729B2/en active Active
-
2018
- 2018-11-02 US US16/179,155 patent/US10647683B2/en active Active
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