JP2013529611A5 - - Google Patents
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- Publication number
- JP2013529611A5 JP2013529611A5 JP2013515827A JP2013515827A JP2013529611A5 JP 2013529611 A5 JP2013529611 A5 JP 2013529611A5 JP 2013515827 A JP2013515827 A JP 2013515827A JP 2013515827 A JP2013515827 A JP 2013515827A JP 2013529611 A5 JP2013529611 A5 JP 2013529611A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- methyl
- triazolo
- chlorophenyl
- ethylacetamide
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 31
- 150000003839 salts Chemical class 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- -1 amino, hydroxyl Chemical group 0.000 claims 5
- 125000004452 carbocyclyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 229940125763 bromodomain inhibitor Drugs 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- PJPRMRNFJZOFLA-FQEVSTJZSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-(1h-pyrazol-4-yl)-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C2=CNN=C2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 PJPRMRNFJZOFLA-FQEVSTJZSA-N 0.000 claims 1
- WMKQEPQCESYBNS-FQEVSTJZSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-(1h-pyrazol-5-yl)-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2NN=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 WMKQEPQCESYBNS-FQEVSTJZSA-N 0.000 claims 1
- HFCOQWDWESZNEW-DEOSSOPVSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-(2-methylphenyl)-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C(=CC=CC=2)C)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 HFCOQWDWESZNEW-DEOSSOPVSA-N 0.000 claims 1
- QKKNSYUKNJSTRL-NDEPHWFRSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-[3-(pyrrolidin-1-ylmethyl)phenyl]-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=C(CN3CCCC3)C=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 QKKNSYUKNJSTRL-NDEPHWFRSA-N 0.000 claims 1
- PILKZSVRGDSFDN-LJAQVGFWSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=C(CN3CCN(C)CC3)C=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 PILKZSVRGDSFDN-LJAQVGFWSA-N 0.000 claims 1
- UCHHERPHYGYXQM-NDEPHWFRSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-[4-(pyrrolidin-1-ylmethyl)phenyl]-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=CC(CN3CCCC3)=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 UCHHERPHYGYXQM-NDEPHWFRSA-N 0.000 claims 1
- DODSTUSXECRXBY-LJAQVGFWSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=CC(CN3CCN(C)CC3)=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 DODSTUSXECRXBY-LJAQVGFWSA-N 0.000 claims 1
- LBNZQYJSQFKTMP-QHCPKHFHSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-phenyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=CC=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 LBNZQYJSQFKTMP-QHCPKHFHSA-N 0.000 claims 1
- MXNRKTOXHIEBKM-QFIPXVFZSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-pyridin-4-yl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=CN=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 MXNRKTOXHIEBKM-QFIPXVFZSA-N 0.000 claims 1
- SPAMVIHCDISFJZ-DEOSSOPVSA-N 2-[(4s)-6-(4-chlorophenyl)-8-(3-methoxyphenyl)-1-methyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=C(OC)C=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 SPAMVIHCDISFJZ-DEOSSOPVSA-N 0.000 claims 1
- DBNRUVQIPZTZFK-DEOSSOPVSA-N 2-[(4s)-6-(4-chlorophenyl)-8-(4-methoxyphenyl)-1-methyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=CC(OC)=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 DBNRUVQIPZTZFK-DEOSSOPVSA-N 0.000 claims 1
- JZVFVHUUEWVBPO-SANMLTNESA-N 2-[(4s)-6-(4-chlorophenyl)-8-[3-(ethylaminomethyl)phenyl]-1-methyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound CCNCC1=CC=CC(C=2C=C3C(N4C(C)=NN=C4[C@H](CC(=O)NCC)N=C3C=3C=CC(Cl)=CC=3)=CC=2)=C1 JZVFVHUUEWVBPO-SANMLTNESA-N 0.000 claims 1
- PHVGVVDKYSSPKA-SANMLTNESA-N 2-[(4s)-6-(4-chlorophenyl)-8-[4-(ethylaminomethyl)phenyl]-1-methyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound C1=CC(CNCC)=CC=C1C1=CC=C2N3C(C)=NN=C3[C@H](CC(=O)NCC)N=C(C=3C=CC(Cl)=CC=3)C2=C1 PHVGVVDKYSSPKA-SANMLTNESA-N 0.000 claims 1
- USCJQEZHNLJYPQ-SANMLTNESA-N 2-[(4s)-6-(4-chlorophenyl)-8-[4-[(dimethylamino)methyl]phenyl]-1-methyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=CC(CN(C)C)=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 USCJQEZHNLJYPQ-SANMLTNESA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 229940049706 benzodiazepine Drugs 0.000 claims 1
- 150000001557 benzodiazepines Chemical class 0.000 claims 1
- 125000003310 benzodiazepinyl group Chemical group N1N=C(C=CC2=C1C=CC=C2)* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 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
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1010514.6A GB201010514D0 (en) | 2010-06-22 | 2010-06-22 | Novel compounds |
| GB1010514.6 | 2010-06-22 | ||
| GB1106801.2 | 2011-04-21 | ||
| GBGB1106801.2A GB201106801D0 (en) | 2011-04-21 | 2011-04-21 | Novel compounds |
| PCT/EP2011/060179 WO2011161031A1 (en) | 2010-06-22 | 2011-06-20 | Benzotriazolodiazepine compounds inhibitors of bromodomains |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013529611A JP2013529611A (ja) | 2013-07-22 |
| JP2013529611A5 true JP2013529611A5 (enExample) | 2014-06-05 |
| JP5844358B2 JP5844358B2 (ja) | 2016-01-13 |
Family
ID=44310320
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013515827A Expired - Fee Related JP5844358B2 (ja) | 2010-06-22 | 2011-06-20 | ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9085582B2 (enExample) |
| EP (1) | EP2585465B1 (enExample) |
| JP (1) | JP5844358B2 (enExample) |
| ES (1) | ES2526671T3 (enExample) |
| WO (1) | WO2011161031A1 (enExample) |
Families Citing this family (81)
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| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| MX373121B (es) | 2010-05-14 | 2020-04-30 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| CA2799381A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Male contraceptive compositions and methods of use |
| US8981083B2 (en) | 2010-05-14 | 2015-03-17 | Dana Farber Cancer Institute, Inc. | Compositions and methods for treating neoplasia, inflammatory disease and other disorders |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2012151512A2 (en) | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9328117B2 (en) | 2011-06-17 | 2016-05-03 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
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| CN105209467B (zh) | 2013-05-27 | 2018-06-08 | 诺华股份有限公司 | 咪唑并吡咯烷酮衍生物及其在治疗疾病中的用途 |
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| ES2656471T3 (es) | 2013-05-28 | 2018-02-27 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de BET y su uso en el tratamiento de enfermedades |
| ES2650562T3 (es) | 2013-05-28 | 2018-01-19 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona y su uso en el tratamiento de enfermedades |
| WO2015006193A1 (en) | 2013-07-08 | 2015-01-15 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| BR112016001457A2 (pt) * | 2013-07-25 | 2017-08-29 | Dana Farber Cancer Inst Inc | Inibidores de fatores de transcrição e usos dos mesmos |
| KR20160072261A (ko) | 2013-11-08 | 2016-06-22 | 다나-파버 캔서 인스티튜트 인크. | 브로모도메인 및 엑스트라-말단 (bet) 단백질 저해제를 이용한 암 치료를 위한 조합 요법 |
| US9550796B2 (en) | 2013-11-21 | 2017-01-24 | Novartis Ag | Pyrrolopyrrolone derivatives and their use as BET inhibitors |
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| US9580430B2 (en) | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
| UA119870C2 (uk) | 2014-04-23 | 2019-08-27 | Інсайт Корпорейшн | 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET |
| CN106687463B (zh) | 2014-06-20 | 2019-04-09 | 星座制药公司 | 一种乙酰胺类化合物的晶型 |
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| US10918647B2 (en) | 2016-07-26 | 2021-02-16 | University Of Southern California | Selective bromodomain inhibition of fungal Bdf1 |
| US10975093B2 (en) | 2016-09-13 | 2021-04-13 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET protein degraders |
| CN110062759B (zh) | 2016-09-13 | 2022-05-24 | 密执安大学评议会 | 作为bet蛋白降解剂的稠合的1,4-氧氮杂䓬 |
| WO2018144789A1 (en) | 2017-02-03 | 2018-08-09 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as bet bromodomain inhibitors |
| WO2019055444A1 (en) | 2017-09-13 | 2019-03-21 | The Regents Of The University Of Michigan | DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS |
| CN107759607B (zh) * | 2017-11-29 | 2019-08-23 | 上海万巷制药有限公司 | 具有抗肿瘤活性的三氮唑并二氮卓化合物及其制备方法 |
| KR20210038921A (ko) | 2018-07-25 | 2021-04-08 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 브로모도메인 단백질 억제제로서의 설폭시민 화합물과 약학적 조성물 및 이의 의학적 용도 |
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| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| KR20230026461A (ko) | 2020-06-23 | 2023-02-24 | 제넨테크, 인크. | 거대고리 화합물 및 이의 사용 방법 |
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| DE3610848A1 (de) | 1986-04-01 | 1987-10-15 | Boehringer Ingelheim Kg | Neue 1,4-diazepine |
| MC1999A1 (fr) * | 1987-12-18 | 1990-01-26 | Hoffmann La Roche | Composes tricycliques |
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| US5593988A (en) | 1991-10-11 | 1997-01-14 | Yoshitomi Pharmaceutical Industries, Ltd. | Therapeutic agent for osteoporosis and diazepine compound |
| JPH06128257A (ja) | 1992-10-13 | 1994-05-10 | Yoshitomi Pharmaceut Ind Ltd | ピリドジアゼピン化合物 |
| JP2840454B2 (ja) | 1993-11-22 | 1998-12-24 | メルク エンド カンパニー インコーポレーテッド | ベンゾジアゼピン類 |
| AU694278B2 (en) | 1994-11-18 | 1998-07-16 | Japan Tobacco Inc. | Osteoporosis remedy and triazepine compound |
| CN1227555A (zh) | 1996-06-12 | 1999-09-01 | 日本烟草产业株式会社 | 细胞因子生成抑制剂、三氮䓬化合物及其中间体 |
| PT989131E (pt) | 1996-09-13 | 2003-03-31 | Mitsubishi Pharma Corp | Compostos de trienotriazolodiazepina e suas utilizacoes com fins medicinais |
| PL1699512T3 (pl) | 2003-11-03 | 2012-11-30 | Glaxo Group Ltd | Urządzenie do dozowania płynów |
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| GB0420970D0 (en) | 2004-09-21 | 2004-10-20 | Smithkline Beecham Corp | Novel triazoloquinoline compounds |
| EP1888594A2 (en) * | 2005-05-16 | 2008-02-20 | Wisys Technology Foundation, Inc. | Gabaergic agents to treat memory deficits |
| EP1887008B1 (en) | 2005-05-30 | 2021-04-21 | Mitsubishi Tanabe Pharma Corporation | Thienotriazolodiazepine compound and a medicinal use thereof |
| CL2007003244A1 (es) * | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| 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 |
| GB0919431D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
-
2011
- 2011-06-20 US US13/702,177 patent/US9085582B2/en not_active Expired - Fee Related
- 2011-06-20 EP EP11725769.1A patent/EP2585465B1/en not_active Not-in-force
- 2011-06-20 JP JP2013515827A patent/JP5844358B2/ja not_active Expired - Fee Related
- 2011-06-20 ES ES11725769.1T patent/ES2526671T3/es active Active
- 2011-06-20 WO PCT/EP2011/060179 patent/WO2011161031A1/en not_active Ceased
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