JP2015531747A5 - - Google Patents
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- Publication number
- JP2015531747A5 JP2015531747A5 JP2015517810A JP2015517810A JP2015531747A5 JP 2015531747 A5 JP2015531747 A5 JP 2015531747A5 JP 2015517810 A JP2015517810 A JP 2015517810A JP 2015517810 A JP2015517810 A JP 2015517810A JP 2015531747 A5 JP2015531747 A5 JP 2015531747A5
- Authority
- JP
- Japan
- Prior art keywords
- carbon atoms
- alkyl
- therapeutic agent
- optionally substituted
- thieno
- 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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- 125000004432 carbon atoms Chemical group C* 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 5
- 210000004027 cells Anatomy 0.000 claims 5
- 230000003211 malignant Effects 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- -1 diazepine compound Chemical class 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000004683 dihydrates Chemical class 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
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 206010012818 Diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 206010062113 Splenic marginal zone lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 125000002344 aminooxy group Chemical group [H]N([H])O[*] 0.000 claims 1
- 125000004429 atoms Chemical group 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 101710017890 large T Proteins 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
Claims (6)
- 式1:
- B細胞悪性癌がびまん性大細胞型B細胞リンパ腫である、請求項1に記載の治療剤。
- B細胞悪性癌が脾臓周辺帯リンパ腫である、請求項1に記載の治療剤。
- T細胞悪性癌が未分化大T細胞リンパ腫である、請求項1に記載の治療剤。
- 式1により表されるチエノトリアゾロジアゼピン化合物が、独立して、(i)(S)−2−[4−(4−クロロフェニル)−2,3,9−トリメチル−6H−チエノ[3,2−f][1,2,4]トリアゾロ−[4,3−a][1,4]ジアゼピン−6−イル]−N−(4−ヒドロキシフェニル)アセトアミドまたはその二水和物、(ii)メチル(S)−{4−(3’−シアノビフェニル−4−イル)−2,3,9−トリメチル−6H−チエノ[3,2−f][1,2,4]トリアゾロ[4,3−a][1,4]ジアゼピン−6−イル}アセタート、(iii)メチル(S)−{2,3,9−トリメチル−4−(4−フェニルアミノフェニル)−6H−チエノ[3,2−f][1,2,4]トリアゾロ[4,3−a][1,4]ジアゼピン−6−イル}アセタート、および(iv)メチル(S)−{2,3,9−トリメチル−4−[4−(3−フェニルプロピオニルアミノ)フェニル]−6H−チエノ[3,2−f−][1,2,4]トリアゾロ[4,3−a][1,4]ジアゼピン−6−イル}アセタートから選択される、請求項1から4のいずれか1項に記載の治療剤。
- 有効成分が(S)−2−[4−(4−クロロフェニル)−2,3,9−トリメチル−6H−チエノ[3,2−f][1,2,4]トリアゾロ−[4,3−a][1,4]ジアゼピン−6−イル]−N−(4−ヒドロキシフェニル)アセトアミドまたはその二水和物である、請求項1から4のいずれか1項に記載の治療剤。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261663885P | 2012-06-25 | 2012-06-25 | |
US61/663,885 | 2012-06-25 | ||
US201261670918P | 2012-07-12 | 2012-07-12 | |
US61/670,918 | 2012-07-12 | ||
PCT/EP2013/063313 WO2014001356A1 (en) | 2012-06-25 | 2013-06-25 | Method of treating lymphoma using thienotriazolodiazepine compounds |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2015531747A JP2015531747A (ja) | 2015-11-05 |
JP2015531747A5 true JP2015531747A5 (ja) | 2016-07-28 |
JP6265979B2 JP6265979B2 (ja) | 2018-01-24 |
Family
ID=48672651
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015517810A Expired - Fee Related JP6265979B2 (ja) | 2012-06-25 | 2013-06-25 | チエノトリアゾロジアゼピン化合物を使用するリンパ腫の治療方法 |
Country Status (12)
Country | Link |
---|---|
US (1) | US20140018353A1 (ja) |
EP (1) | EP2863923B1 (ja) |
JP (1) | JP6265979B2 (ja) |
KR (1) | KR20150045423A (ja) |
CN (1) | CN105050605A (ja) |
AU (1) | AU2013283378B2 (ja) |
BR (1) | BR112014032105A2 (ja) |
CA (1) | CA2877434A1 (ja) |
IN (1) | IN2014DN11269A (ja) |
MX (1) | MX2014015986A (ja) |
RU (1) | RU2659171C2 (ja) |
WO (1) | WO2014001356A1 (ja) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104736569A (zh) | 2012-01-12 | 2015-06-24 | 耶鲁大学 | 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法 |
UA119848C2 (uk) | 2013-03-15 | 2019-08-27 | Інсайт Холдинґс Корпорейшн | Трициклічні гетероцикли як інгібітори білків бет |
US9290514B2 (en) | 2013-07-08 | 2016-03-22 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
EP3027194A1 (en) * | 2013-08-01 | 2016-06-08 | Oncoethix GmbH | Pharmaceutical formulation containing thienotriazolodiazepine compounds |
WO2015018520A1 (en) * | 2013-08-06 | 2015-02-12 | Oncoethix Sa | A bet-brd inhibitor represents a novel agent for alk positive anaplastic large cell lymphoma |
WO2015018522A1 (en) * | 2013-08-06 | 2015-02-12 | Oncoethix Sa | Bet-bromodomain inhibitor shows synergism with several anti-cancer agents in pre-clinical models of diffuse large b-cell lymphoma (dlbcl) |
US20160158246A1 (en) * | 2013-08-06 | 2016-06-09 | Oncoethix Gmbh | Method of treating diffuse large b-cell lymphoma (dlbcl) using a bet-bromodomain inhibitor |
WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
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 |
KR20160079823A (ko) | 2013-11-27 | 2016-07-06 | 온코에틱스 게엠베하 | 티에노트리아졸로디아제핀 화합물을 함유하는 제약 제제를 사용하여 백혈병을 치료하는 방법 |
US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
EA039678B1 (ru) | 2014-04-23 | 2022-02-24 | Инсайт Корпорейшн | 1H-ПИРРОЛО[2,3-c]ПИРИДИН-7(6H)-ОНЫ И ПИРАЗОЛО[3,4-c]ПИРИДИН-7(6H)-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕЛКОВ BET |
JP2017514907A (ja) * | 2014-05-02 | 2017-06-08 | オンコエシックス ゲーエムベーハー | チエノトリアゾロジアゼピン化合物を用いる耐性非ホジキンリンパ腫、髄芽腫及び/又はalk+非小細胞肺癌の治療方法 |
WO2015168621A1 (en) | 2014-05-02 | 2015-11-05 | Oncoethix Sa | Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds |
WO2015169951A1 (en) | 2014-05-08 | 2015-11-12 | Oncoethix Gmbh | Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds |
KR20170016858A (ko) | 2014-06-13 | 2017-02-14 | 온코에틱스 게엠베하 | 티에노트리아졸로디아제핀 화합물을 사용하는 비소세포성 폐암 및/또는 소세포성 폐암의 치료 방법 |
KR20170037670A (ko) | 2014-08-19 | 2017-04-04 | 온코에틱스 게엠베하 | 티에노트리아졸로디아제핀 화합물을 사용한 림프종의 치료 방법 |
TWI712603B (zh) | 2014-09-15 | 2020-12-11 | 美商英塞特公司 | 作為bet蛋白抑制劑之三環雜環 |
KR101675984B1 (ko) * | 2015-02-23 | 2016-11-14 | 한양대학교 에리카산학협력단 | 티에노디아제핀 유도체 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 포함하는 약학적 조성물 |
CA2979070A1 (en) | 2015-03-18 | 2016-09-22 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
WO2016176335A1 (en) | 2015-04-27 | 2016-11-03 | Concert Pharmaceuticals, Inc. | Deuterated otx-015 |
US10772962B2 (en) | 2015-08-19 | 2020-09-15 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
PT3472157T (pt) | 2016-06-20 | 2023-05-30 | Incyte Corp | Formas sólidas cristalinas de um inibidor bet |
JP2021512153A (ja) | 2018-01-26 | 2021-05-13 | イエール ユニバーシティ | タンパク質分解のイミド系モジュレーターおよび使用方法 |
CN108070562A (zh) * | 2018-02-03 | 2018-05-25 | 金华市中心医院 | 一种“双打击”弥漫大b细胞淋巴瘤细胞系制备方法 |
CN112262134B (zh) | 2018-04-13 | 2024-05-24 | 阿尔维纳斯运营股份有限公司 | 小脑蛋白配体和包括其的双官能化合物 |
WO2021127443A1 (en) | 2019-12-19 | 2021-06-24 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1994006802A1 (en) | 1992-09-18 | 1994-03-31 | Yoshitomi Pharmaceutical Industries, Ltd. | Thienodiazepine compound and medicinal use thereof |
DE69717160T2 (de) * | 1996-09-13 | 2003-05-08 | Mitsubishi Pharma Corp | Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen |
EP2239264A4 (en) * | 2007-12-28 | 2012-01-11 | Mitsubishi Tanabe Pharma Corp | ANTITUMOR AGENT |
JP5715241B2 (ja) * | 2010-05-14 | 2015-05-07 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | 新生物、炎症性疾患、およびその他の障害を治療するための組成物および方法 |
CN104311562B (zh) * | 2010-05-14 | 2017-07-04 | 达那-法伯癌症研究所 | 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法 |
WO2013033420A1 (en) * | 2011-08-30 | 2013-03-07 | Whitehead Institute For Biomedical Research | Methods of downregulating translocated oncogene expression using bromodomain inhibitors |
-
2013
- 2013-06-25 KR KR20157000782A patent/KR20150045423A/ko active Search and Examination
- 2013-06-25 US US13/926,029 patent/US20140018353A1/en not_active Abandoned
- 2013-06-25 BR BR112014032105A patent/BR112014032105A2/pt not_active Application Discontinuation
- 2013-06-25 WO PCT/EP2013/063313 patent/WO2014001356A1/en active Application Filing
- 2013-06-25 CA CA2877434A patent/CA2877434A1/en not_active Abandoned
- 2013-06-25 EP EP13730912.6A patent/EP2863923B1/en not_active Not-in-force
- 2013-06-25 AU AU2013283378A patent/AU2013283378B2/en not_active Ceased
- 2013-06-25 MX MX2014015986A patent/MX2014015986A/es unknown
- 2013-06-25 RU RU2015101106A patent/RU2659171C2/ru not_active IP Right Cessation
- 2013-06-25 JP JP2015517810A patent/JP6265979B2/ja not_active Expired - Fee Related
- 2013-06-25 IN IN11269DEN2014 patent/IN2014DN11269A/en unknown
- 2013-06-25 CN CN201380045846.0A patent/CN105050605A/zh active Pending
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