JP2014511892A5 - - Google Patents
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- Publication number
- JP2014511892A5 JP2014511892A5 JP2014505612A JP2014505612A JP2014511892A5 JP 2014511892 A5 JP2014511892 A5 JP 2014511892A5 JP 2014505612 A JP2014505612 A JP 2014505612A JP 2014505612 A JP2014505612 A JP 2014505612A JP 2014511892 A5 JP2014511892 A5 JP 2014511892A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- salt
- pharmaceutically acceptable
- alkyl
- acceptable salt
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 22
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 229940125763 bromodomain inhibitor Drugs 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- SYWATAHTVWWKEE-CCLHPLFOSA-N 2-[4-[(2s,4r)-1-acetyl-4-[(5-cyanopyridin-2-yl)amino]-2-methyl-3,4-dihydro-2h-quinolin-6-yl]phenyl]-n-[2-(dimethylamino)ethyl]acetamide Chemical compound N([C@@H]1C[C@@H](N(C2=CC=C(C=C21)C=1C=CC(CC(=O)NCCN(C)C)=CC=1)C(C)=O)C)C1=CC=C(C#N)C=N1 SYWATAHTVWWKEE-CCLHPLFOSA-N 0.000 claims 1
- XZPYLOTVLUIJBU-QMHKHESXSA-N 6-[(2s,4r)-1-acetyl-4-[(5-cyanopyridin-2-yl)amino]-2-methyl-3,4-dihydro-2h-quinolin-6-yl]-n-(2-hydroxyethyl)pyridine-3-carboxamide Chemical compound N([C@@H]1C[C@@H](N(C2=CC=C(C=C21)C=1N=CC(=CC=1)C(=O)NCCO)C(C)=O)C)C1=CC=C(C#N)C=N1 XZPYLOTVLUIJBU-QMHKHESXSA-N 0.000 claims 1
- OSDXAECFLKDYBD-AVRWGWEMSA-N 6-[(2s,4r)-1-acetyl-4-[(5-cyanopyridin-2-yl)amino]-2-methyl-3,4-dihydro-2h-quinolin-6-yl]-n-[2-(dimethylamino)ethyl]pyridine-3-carboxamide Chemical compound N([C@@H]1C[C@@H](N(C2=CC=C(C=C21)C=1N=CC(=CC=1)C(=O)NCCN(C)C)C(C)=O)C)C1=CC=C(C#N)C=N1 OSDXAECFLKDYBD-AVRWGWEMSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- VAWXXAHAIYEJAS-UHFFFAOYSA-N C=Cc(nc1)ccc1N Chemical compound C=Cc(nc1)ccc1N VAWXXAHAIYEJAS-UHFFFAOYSA-N 0.000 description 1
- KVFIJIWMDBAGDP-UHFFFAOYSA-N CCc1cnccn1 Chemical compound CCc1cnccn1 KVFIJIWMDBAGDP-UHFFFAOYSA-N 0.000 description 1
- RILVNLMOTMFTMQ-UHFFFAOYSA-N CCc1ncccn1 Chemical compound CCc1ncccn1 RILVNLMOTMFTMQ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1106750.1A GB201106750D0 (en) | 2011-04-21 | 2011-04-21 | Novel compounds |
| GB1106750.1 | 2011-04-21 | ||
| PCT/EP2012/057113 WO2012143415A1 (en) | 2011-04-21 | 2012-04-19 | Tetrahydroquinoline derivatives useful as bromodomain inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014511892A JP2014511892A (ja) | 2014-05-19 |
| JP2014511892A5 true JP2014511892A5 (cg-RX-API-DMAC10.html) | 2015-04-30 |
| JP5905075B2 JP5905075B2 (ja) | 2016-04-20 |
Family
ID=44147342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014505612A Active JP5905075B2 (ja) | 2011-04-21 | 2012-04-19 | ブロモドメイン阻害剤として有用なテトラヒドロキノリン誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8993554B2 (cg-RX-API-DMAC10.html) |
| EP (2) | EP2699551B1 (cg-RX-API-DMAC10.html) |
| JP (1) | JP5905075B2 (cg-RX-API-DMAC10.html) |
| ES (1) | ES2615238T3 (cg-RX-API-DMAC10.html) |
| GB (1) | GB201106750D0 (cg-RX-API-DMAC10.html) |
| WO (1) | WO2012143415A1 (cg-RX-API-DMAC10.html) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201106743D0 (en) * | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201107325D0 (en) | 2011-05-04 | 2011-06-15 | Glaxosmithkline Llc | Novel compounds |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| CN105073744B (zh) | 2012-12-21 | 2019-11-08 | 齐尼思表观遗传学有限公司 | 作为溴结构域抑制剂的新型杂环化合物 |
| JP2016516701A (ja) | 2013-03-11 | 2016-06-09 | アッヴィ・インコーポレイテッド | 縮合四環系ブロモドメイン阻害剤 |
| JP2016512524A (ja) | 2013-03-11 | 2016-04-28 | アッヴィ・インコーポレイテッド | ブロモドメイン阻害剤 |
| HRP20182179T1 (hr) | 2013-03-14 | 2019-02-22 | Glaxosmithkline Intellectual Property (No. 2) Limited | 2,3-disupstituirani 1-acil-4-amino-1,2,3,4-tetrahidrokonolin derivati i njihova uporaba kao inhibitora bromodomena |
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| CA2915838C (en) | 2013-06-21 | 2023-04-18 | Zenith Epigenetics Corp. | Bicyclic bromodomain inhibitors |
| US9636328B2 (en) | 2013-06-21 | 2017-05-02 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
| US9290514B2 (en) | 2013-07-08 | 2016-03-22 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
| CN105593224B (zh) | 2013-07-31 | 2021-05-25 | 恒元生物医药科技(苏州)有限公司 | 作为溴结构域抑制剂的新型喹唑啉酮类化合物 |
| WO2015074081A1 (en) * | 2013-11-18 | 2015-05-21 | Bair Kenneth W | Benzopiperazine compositions as bet bromodomain inhibitors |
| HUE053645T2 (hu) | 2013-11-18 | 2021-07-28 | Forma Therapeutics Inc | Tetrahidrokinolin kompozíciók mint BET bromodomén inhibitorok |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| US9142676B2 (en) | 2013-12-30 | 2015-09-22 | Taiwan Semiconductor Manufacturing Company, Ltd. | Semiconductor liner of semiconductor device |
| PL3092227T3 (pl) * | 2014-01-09 | 2018-12-31 | Orion Corporation | Bicykliczne pochodne heterocykliczne jako inhibitory bromodomeny |
| EA034972B1 (ru) | 2014-04-23 | 2020-04-13 | Инсайт Корпорейшн | 1h-пирроло[2,3-c]пиридин-7(6h)-оны в качестве ингибиторов белков bet |
| ES2896400T3 (es) * | 2014-08-01 | 2022-02-24 | Nuevolution As | Compuestos activos frente a bromdominios |
| SMT201900019T1 (it) | 2014-09-12 | 2019-02-28 | Glaxosmithkline Ip No 2 Ltd | Derivati di tetraidrochinolina come inibitori di bromodominio |
| EP3194406B8 (en) | 2014-09-15 | 2021-03-31 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| EP3227281A4 (en) | 2014-12-01 | 2018-05-30 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| EP3227280B1 (en) | 2014-12-01 | 2019-04-24 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| US10292968B2 (en) | 2014-12-11 | 2019-05-21 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| HK1245247A1 (zh) | 2014-12-17 | 2018-08-24 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| WO2016203335A1 (en) | 2015-06-18 | 2016-12-22 | Pfizer Inc. | Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors |
| AR106520A1 (es) | 2015-10-29 | 2018-01-24 | Incyte Corp | Forma sólida amorfa de un inhibidor de proteína bet |
| PT3472157T (pt) | 2016-06-20 | 2023-05-30 | Incyte Corp | Formas sólidas cristalinas de um inibidor bet |
| ES2937307T3 (es) | 2016-07-26 | 2023-03-27 | Univ Southern California | Inhibición selectiva del bromodominio del BDF1 fúngico |
| WO2018111805A1 (en) * | 2016-12-13 | 2018-06-21 | St. Jude Children's Research Hospital | Tetrahydroquinoline-based bromodomain inhibitors |
| US11629152B2 (en) * | 2018-03-30 | 2023-04-18 | Kyowa Kirin Co., Ltd. | Compound with anticancer activity |
| KR102831570B1 (ko) | 2018-05-04 | 2025-07-10 | 레미디 플랜, 인크. | 암 줄기 세포를 표적화하는 암 치료 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| UY39276A (es) | 2020-06-19 | 2022-01-31 | Bayer Ag | Uso de compuestos de 1,3,4–oxadiazol–2–ilpirimidina para controlar microorganismos fitopatógenos, métodos de uso y composiciones. |
| WO2022129190A1 (en) | 2020-12-18 | 2022-06-23 | Bayer Aktiengesellschaft | (hetero)aryl substituted 1,2,4-oxadiazoles as fungicides |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| JP4641526B2 (ja) | 2003-11-03 | 2011-03-02 | グラクソ グループ リミテッド | 流体分配デバイス |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| EP2239264A4 (en) | 2007-12-28 | 2012-01-11 | Mitsubishi Tanabe Pharma Corp | ANTITUMORAL MEDIUM |
| WO2010018874A1 (en) * | 2008-08-12 | 2010-02-18 | Takeda Pharmaceutical Company Limited | Amide compound |
| WO2010074807A1 (en) * | 2008-10-30 | 2010-07-01 | Gilead Palo Alto, Inc. | 3, 4-dihydroquinolin-2 ( 1h ) -one derivatives as sodium channel modulators |
| WO2010111626A2 (en) * | 2009-03-27 | 2010-09-30 | Takeda Pharmaceutical Company Limited | Poly (adp-ribose) polymerase (parp) inhibitors |
| GB0919431D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| US9360482B2 (en) * | 2009-11-05 | 2016-06-07 | Glaxosmithkline Llc | Process for the identification of a compound which inhibits the binding of the second bromodomain of each of human BRD-2, BRD-3, and BRD-4 |
| GB0919432D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
-
2011
- 2011-04-21 GB GBGB1106750.1A patent/GB201106750D0/en not_active Ceased
-
2012
- 2012-04-19 WO PCT/EP2012/057113 patent/WO2012143415A1/en not_active Ceased
- 2012-04-19 ES ES12718620.3T patent/ES2615238T3/es active Active
- 2012-04-19 JP JP2014505612A patent/JP5905075B2/ja active Active
- 2012-04-19 US US14/111,625 patent/US8993554B2/en not_active Expired - Fee Related
- 2012-04-19 EP EP12718620.3A patent/EP2699551B1/en not_active Not-in-force
- 2012-04-19 EP EP16197070.2A patent/EP3168213B1/en not_active Not-in-force