JP2010520893A5 - - Google Patents
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- Publication number
- JP2010520893A5 JP2010520893A5 JP2009552982A JP2009552982A JP2010520893A5 JP 2010520893 A5 JP2010520893 A5 JP 2010520893A5 JP 2009552982 A JP2009552982 A JP 2009552982A JP 2009552982 A JP2009552982 A JP 2009552982A JP 2010520893 A5 JP2010520893 A5 JP 2010520893A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrocarbyl
- phenyl
- optionally substituted
- pyrrolidin
- group
- 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
- 150000001875 compounds Chemical class 0.000 claims 37
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 16
- 125000003373 pyrazinyl group Chemical group 0.000 claims 11
- 125000002098 pyridazinyl group Chemical group 0.000 claims 11
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 11
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 claims 11
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 11
- 125000000335 thiazolyl group Chemical group 0.000 claims 11
- 125000001544 thienyl group Chemical group 0.000 claims 11
- 125000004306 triazinyl group Chemical group 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 10
- 125000004076 pyridyl group Chemical group 0.000 claims 10
- ZYHQGITXIJDDKC-UHFFFAOYSA-N 2-[2-(2-aminophenyl)ethyl]aniline Chemical group NC1=CC=CC=C1CCC1=CC=CC=C1N ZYHQGITXIJDDKC-UHFFFAOYSA-N 0.000 claims 9
- -1 di-alkylamino Chemical group 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000000732 arylene group Chemical group 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- NSTWXSYXHFXOLU-AWEZNQCLSA-N 2,2,2-trifluoroethyl n-[(3s)-1-[4-[(2-aminophenyl)carbamoyl]phenyl]pyrrolidin-3-yl]carbamate Chemical compound NC1=CC=CC=C1NC(=O)C1=CC=C(N2C[C@H](CC2)NC(=O)OCC(F)(F)F)C=C1 NSTWXSYXHFXOLU-AWEZNQCLSA-N 0.000 claims 1
- UDSLGDKSJDZFLT-KRWDZBQOSA-N 2-(dimethylamino)ethyl n-[(3s)-1-[4-[(2-aminophenyl)carbamoyl]phenyl]pyrrolidin-3-yl]carbamate Chemical compound C1[C@@H](NC(=O)OCCN(C)C)CCN1C1=CC=C(C(=O)NC=2C(=CC=CC=2)N)C=C1 UDSLGDKSJDZFLT-KRWDZBQOSA-N 0.000 claims 1
- YQRHVEBSOBGLTF-AWEZNQCLSA-N C1CNC[C@@H]1CCNC(=O)OC2=CC=C(C=C2)C(=O)NC3=CC=CC=C3N Chemical compound C1CNC[C@@H]1CCNC(=O)OC2=CC=C(C=C2)C(=O)NC3=CC=CC=C3N YQRHVEBSOBGLTF-AWEZNQCLSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 102000003964 Histone deacetylase Human genes 0.000 claims 1
- 108090000353 Histone deacetylase Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- VBQSXSFITGZRRE-INIZCTEOSA-N [(3s)-1-[4-[(2-aminophenyl)carbamoyl]phenyl]pyrrolidin-3-yl] acetate Chemical compound C1[C@@H](OC(=O)C)CCN1C1=CC=C(C(=O)NC=2C(=CC=CC=2)N)C=C1 VBQSXSFITGZRRE-INIZCTEOSA-N 0.000 claims 1
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzene carboxamide Natural products NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- RUZLIIJDZBWWSA-INIZCTEOSA-N methyl 2-[[(1s)-1-(7-methyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)ethyl]amino]benzoate Chemical group COC(=O)C1=CC=CC=C1N[C@@H](C)C1=CC(C)=CN2C(=O)C=C(N3CCOCC3)N=C12 RUZLIIJDZBWWSA-INIZCTEOSA-N 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- JTWHPOCYOKKSDH-AWEZNQCLSA-N n-(2-aminophenyl)-4-[(3s)-3-hydroxypyrrolidin-1-yl]benzamide Chemical compound NC1=CC=CC=C1NC(=O)C1=CC=C(N2C[C@@H](O)CC2)C=C1 JTWHPOCYOKKSDH-AWEZNQCLSA-N 0.000 claims 1
- LBFHWFNYZXAOMS-KRWDZBQOSA-N n-[(3s)-1-[4-[(2-aminophenyl)carbamoyl]phenyl]pyrrolidin-3-yl]morpholine-4-carboxamide Chemical compound NC1=CC=CC=C1NC(=O)C1=CC=C(N2C[C@H](CC2)NC(=O)N2CCOCC2)C=C1 LBFHWFNYZXAOMS-KRWDZBQOSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90673307P | 2007-03-13 | 2007-03-13 | |
| US12/043,450 US8030344B2 (en) | 2007-03-13 | 2008-03-06 | Inhibitors of histone deacetylase |
| PCT/CA2008/000455 WO2008109994A1 (en) | 2007-03-13 | 2008-03-12 | Inhibitors of histone deacetylase |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014024898A Division JP5885311B2 (ja) | 2007-03-13 | 2014-02-12 | ヒストンデアセチラーゼの阻害剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010520893A JP2010520893A (ja) | 2010-06-17 |
| JP2010520893A5 true JP2010520893A5 (show.php) | 2011-05-06 |
Family
ID=39758948
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009552982A Pending JP2010520893A (ja) | 2007-03-13 | 2008-03-12 | ヒストンデアセチラーゼの阻害剤 |
| JP2014024898A Expired - Fee Related JP5885311B2 (ja) | 2007-03-13 | 2014-02-12 | ヒストンデアセチラーゼの阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014024898A Expired - Fee Related JP5885311B2 (ja) | 2007-03-13 | 2014-02-12 | ヒストンデアセチラーゼの阻害剤 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8030344B2 (show.php) |
| EP (1) | EP2134680B1 (show.php) |
| JP (2) | JP2010520893A (show.php) |
| KR (2) | KR20150080025A (show.php) |
| CN (1) | CN101679239B (show.php) |
| CA (1) | CA2680467C (show.php) |
| ES (1) | ES2565243T3 (show.php) |
| TW (1) | TWI549676B (show.php) |
| WO (1) | WO2008109994A1 (show.php) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8030344B2 (en) * | 2007-03-13 | 2011-10-04 | Methylgene Inc. | Inhibitors of histone deacetylase |
| CN101918389A (zh) * | 2007-11-02 | 2010-12-15 | 梅特希尔基因公司 | 组蛋白脱乙酰酶抑制剂 |
| EP2330894B8 (en) | 2008-09-03 | 2017-04-19 | BioMarin Pharmaceutical Inc. | Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors |
| WO2010094678A1 (en) * | 2009-02-23 | 2010-08-26 | F. Hoffmann-La Roche Ag | Novel ortho-aminoamides for the treatment of cancer |
| WO2011053876A1 (en) | 2009-10-30 | 2011-05-05 | Massachusetts Institute Of Technology | The use of ci-994 and dinaline for the treatment of memory/cognition and anxiety disorders |
| US20130310379A1 (en) * | 2010-11-19 | 2013-11-21 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US10059723B2 (en) | 2011-02-28 | 2018-08-28 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| PT2680694T (pt) | 2011-02-28 | 2019-03-14 | Biomarin Pharm Inc | Inibidores de histona deacetilase |
| US8957066B2 (en) | 2011-02-28 | 2015-02-17 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| CN102775368B (zh) * | 2011-05-10 | 2016-08-17 | 上海驺虞医药科技有限公司 | 一类噻唑类化合物及其制备方法和用途 |
| EP2780013A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| US9206128B2 (en) | 2011-11-18 | 2015-12-08 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| JP5989805B2 (ja) | 2012-02-10 | 2016-09-07 | コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | メチル基変更酵素の調節物質、組成物及びその使用 |
| US9745305B2 (en) | 2013-03-15 | 2017-08-29 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| WO2014143666A1 (en) | 2013-03-15 | 2014-09-18 | Biomarin Pharmaceutical Inc. | Hdac inhibitors |
| US9969716B2 (en) | 2013-08-15 | 2018-05-15 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| US9274117B2 (en) * | 2013-12-21 | 2016-03-01 | Catholic University Industry Academic | Use of SIRT7 as novel cancer therapy target and method for treating cancer using the same |
| US9636298B2 (en) | 2014-01-17 | 2017-05-02 | Methylgene Inc. | Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs |
| GB201501870D0 (en) * | 2015-02-04 | 2015-03-18 | Cancer Rec Tech Ltd | Autotaxin inhibitors |
| KR20180022840A (ko) * | 2015-07-02 | 2018-03-06 | 바이오마린 파머수티컬 인크. | 히스톤 데아세틸라제 저해제 |
| WO2017040190A1 (en) | 2015-08-28 | 2017-03-09 | Constellation Pharmaceuticals, Inc. | Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide |
| US10457640B2 (en) | 2016-10-19 | 2019-10-29 | Constellation Pharmaceuticals, Inc. | Synthesis of inhibitors of EZH2 |
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-
2008
- 2008-03-06 US US12/043,450 patent/US8030344B2/en active Active
- 2008-03-12 ES ES08733559.2T patent/ES2565243T3/es active Active
- 2008-03-12 KR KR1020157016812A patent/KR20150080025A/ko not_active Ceased
- 2008-03-12 WO PCT/CA2008/000455 patent/WO2008109994A1/en not_active Ceased
- 2008-03-12 KR KR1020097021343A patent/KR101678611B1/ko active Active
- 2008-03-12 CA CA2680467A patent/CA2680467C/en not_active Expired - Fee Related
- 2008-03-12 CN CN200880015207.9A patent/CN101679239B/zh not_active Expired - Fee Related
- 2008-03-12 EP EP08733559.2A patent/EP2134680B1/en active Active
- 2008-03-12 JP JP2009552982A patent/JP2010520893A/ja active Pending
- 2008-03-12 TW TW097108730A patent/TWI549676B/zh active
-
2011
- 2011-05-11 US US13/105,151 patent/US8354445B2/en not_active Expired - Fee Related
-
2014
- 2014-02-12 JP JP2014024898A patent/JP5885311B2/ja not_active Expired - Fee Related
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