JP2022500372A - 癌治療のためのブロモドメインBRD4阻害剤としてのtert−ブチル(S)−2−(4−(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)アセテート誘導体及び関連化合物 - Google Patents
癌治療のためのブロモドメインBRD4阻害剤としてのtert−ブチル(S)−2−(4−(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)アセテート誘導体及び関連化合物 Download PDFInfo
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- RTKIYFITIVXBLE-QEQCGCAPSA-N trichostatin A Chemical compound ONC(=O)/C=C/C(/C)=C/[C@@H](C)C(=O)C1=CC=C(N(C)C)C=C1 RTKIYFITIVXBLE-QEQCGCAPSA-N 0.000 description 1
- KVJXBPDAXMEYOA-CXANFOAXSA-N trilostane Chemical compound OC1=C(C#N)C[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@@]32O[C@@H]31 KVJXBPDAXMEYOA-CXANFOAXSA-N 0.000 description 1
- 229960001670 trilostane Drugs 0.000 description 1
- IEDVJHCEMCRBQM-UHFFFAOYSA-N trimethoprim Chemical compound COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 IEDVJHCEMCRBQM-UHFFFAOYSA-N 0.000 description 1
- 229960001082 trimethoprim Drugs 0.000 description 1
- NOYPYLRCIDNJJB-UHFFFAOYSA-N trimetrexate Chemical compound COC1=C(OC)C(OC)=CC(NCC=2C(=C3C(N)=NC(N)=NC3=CC=2)C)=C1 NOYPYLRCIDNJJB-UHFFFAOYSA-N 0.000 description 1
- 229960001099 trimetrexate Drugs 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 229960000875 trofosfamide Drugs 0.000 description 1
- UMKFEPPTGMDVMI-UHFFFAOYSA-N trofosfamide Chemical compound ClCCN(CCCl)P1(=O)OCCCN1CCCl UMKFEPPTGMDVMI-UHFFFAOYSA-N 0.000 description 1
- UIVFDCIXTSJXBB-ITGUQSILSA-N tropisetron Chemical compound C1=CC=C[C]2C(C(=O)O[C@H]3C[C@H]4CC[C@@H](C3)N4C)=CN=C21 UIVFDCIXTSJXBB-ITGUQSILSA-N 0.000 description 1
- 229960003688 tropisetron Drugs 0.000 description 1
- SZCZSKMCTGEJKI-UHFFFAOYSA-N tuberin Natural products COC1=CC=C(C=CNC=O)C=C1 SZCZSKMCTGEJKI-UHFFFAOYSA-N 0.000 description 1
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- 238000010798 ubiquitination Methods 0.000 description 1
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- MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 description 1
- 229960000604 valproic acid Drugs 0.000 description 1
- 229960000653 valrubicin Drugs 0.000 description 1
- ZOCKGBMQLCSHFP-KQRAQHLDSA-N valrubicin Chemical compound O([C@H]1C[C@](CC2=C(O)C=3C(=O)C4=CC=CC(OC)=C4C(=O)C=3C(O)=C21)(O)C(=O)COC(=O)CCCC)[C@H]1C[C@H](NC(=O)C(F)(F)F)[C@H](O)[C@H](C)O1 ZOCKGBMQLCSHFP-KQRAQHLDSA-N 0.000 description 1
- JQSHBVHOMNKWFT-DTORHVGOSA-N varenicline Chemical compound C12=CC3=NC=CN=C3C=C2[C@H]2C[C@@H]1CNC2 JQSHBVHOMNKWFT-DTORHVGOSA-N 0.000 description 1
- 229950000578 vatalanib Drugs 0.000 description 1
- YCOYDOIWSSHVCK-UHFFFAOYSA-N vatalanib Chemical compound C1=CC(Cl)=CC=C1NC(C1=CC=CC=C11)=NN=C1CC1=CC=NC=C1 YCOYDOIWSSHVCK-UHFFFAOYSA-N 0.000 description 1
- LLDWLPRYLVPDTG-UHFFFAOYSA-N vatalanib succinate Chemical compound OC(=O)CCC(O)=O.C1=CC(Cl)=CC=C1NC(C1=CC=CC=C11)=NN=C1CC1=CC=NC=C1 LLDWLPRYLVPDTG-UHFFFAOYSA-N 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 229960003862 vemurafenib Drugs 0.000 description 1
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical group CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 description 1
- CILBMBUYJCWATM-PYGJLNRPSA-N vinorelbine ditartrate Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.OC(=O)[C@H](O)[C@@H](O)C(O)=O.C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC CILBMBUYJCWATM-PYGJLNRPSA-N 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 230000029812 viral genome replication Effects 0.000 description 1
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- 239000003871 white petrolatum Substances 0.000 description 1
- 210000002268 wool Anatomy 0.000 description 1
- QDLHCMPXEPAAMD-QAIWCSMKSA-N wortmannin Chemical compound C1([C@]2(C)C3=C(C4=O)OC=C3C(=O)O[C@@H]2COC)=C4[C@@H]2CCC(=O)[C@@]2(C)C[C@H]1OC(C)=O QDLHCMPXEPAAMD-QAIWCSMKSA-N 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
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- 239000011701 zinc Substances 0.000 description 1
- XRASPMIURGNCCH-UHFFFAOYSA-N zoledronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CN1C=CN=C1 XRASPMIURGNCCH-UHFFFAOYSA-N 0.000 description 1
- 229940002005 zometa Drugs 0.000 description 1
- CGTADGCBEXYWNE-JUKNQOCSSA-N zotarolimus Chemical compound N1([C@H]2CC[C@@H](C[C@@H](C)[C@H]3OC(=O)[C@@H]4CCCCN4C(=O)C(=O)[C@@]4(O)[C@H](C)CC[C@H](O4)C[C@@H](/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C3)OC)C[C@H]2OC)C=NN=N1 CGTADGCBEXYWNE-JUKNQOCSSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/16—Peri-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Description
本出願は、2018年9月11日に出願された米国特許仮出願第62/729,679号の優先権及び利益を主張し、その内容が全体として本明細書に参照により組み込まれている。
の化合物又はその薬学的に許容される塩若しくはエナンチオマーであって、式中、
X1は、S又はC(R11)であり、
X2は、存在しないか又はC(R12)であり、
X3は、N又はOであり、
環Aは、フェニル又は6員のヘテロアリールであり、環Aは任意に、ハロ、ヒドロキシ、−C1〜3−アルキル、−O−C1〜3−アルキル、及び−NH2からなる群から選択される1つ以上の置換基で更に置換されており、
R1は、−O−C1〜C6−アルキル、又は−N(R8)(R9)であり、
R2は、メチルであり、
R3、R4、R11、及びR12はそれぞれ、H、メチル、及びメトキシからなる群から独立して選択され、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシからなる群から選択され、
R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択され、
R8及びR9は、H、C1〜C4−アルキル、及びフェニルからなる群から独立して選択され、式中、フェニルは、R10で任意に置換されており、
R10は、ヒドロキシであり、
Lは、C1〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンであり、
は、単結合又は二重結合であり、X1がC(R11)である場合、
は、X1とX2との間の二重結合であり、X3がNである場合、
は、X3と分子の残りの部分との間の二重結合である、
化合物又はその薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物又はその薬学的に許容される塩であって、式中、R1、R2、R3、R4、R5、環A、L、及び
は、式(I)で定義したとおりである、化合物又はその薬学的に許容される塩に関する。
I.定義
が示されるとき、二重結合と単結合の両方が、示される化合物の文脈内で提示される。
II.BRD4阻害剤化合物
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、
X1は、S又はC(R11)であり、
X2は、存在しないか又はC(R12)であり、
X3は、N又はOであり、
環Aは、フェニル又は6員のヘテロアリールであり、環Aは任意に、ハロ、ヒドロキシ、−C1〜3−アルキル、−O−C1〜3−アルキル、及び−NH2からなる群から選択される1つ以上の置換基で、一実施形態において更に置換されており、
R1は、−O−C1〜C6−アルキル、又は−N(R8)(R9)であり、
R2は、メチルであり、
R3、R4、R11、及びR12はそれぞれ、H、メチル、及びメトキシからなる群から独立して選択され、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシからなる群から選択され、
R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択され、
R8及びR9は、H、C1〜C4−アルキル、及びフェニルからなる群から独立して選択され、式中、フェニルは、R10で任意に置換されており、
R10は、ヒドロキシであり、
Lは、C1〜C4アルキレン、C2〜C4アルケニレン、及びC2−C4アルキニレンからなる群から選択され、
は、単結合又は二重結合であり、X1がC(R11)である場合、
は、X1とX2との間の二重結合であり、X3がNである場合、
は、X3と分子の残りの部分との間の二重結合である、
化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーに関する。
は、式(I)について上で定義したとおりであり、式中、LはC2〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンである、化合物、又はその塩である。
は、式(I)について上で定義したとおりであり、式中、R5は−N(R6)(R7)であり、R6及びR7は、H、メチル、−C(NH)−NH2、及びヒドロキシからなる群から独立して選択され、Lは、C3〜C4アルキレン、C3〜C4アルケニレン、又はC3〜C4アルキニレンである、化合物、又はその塩である。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、X1、X2、X3、環A、R1、R2、R3、R4、R5、L、及び
は、式(I)について上で定義したとおりである、化合物、又はその塩に関する。
からなる群から選択され、式中、R5、R13、及びLは、式(I)、(Ia)、又は(Ib)について上で定義したとおりであり、nは0、1、2、又は3である、化合物、又はその塩である。特定の一実施形態では、環Aは、L及びR5と合わせて、
であり、式中、R5、R13、及びLは、式(I)、(Ia)、又は(Ib)について上で定義したとおりであり、nは0、1、2、又は3である。
からなる群から選択され、
式中、L、R5、及びR13は、式(I)、(Ia)、又は(Ib)について上で定義したとおりであり、nは0、1、2、又は3である、化合物、又はその塩である。特定の一実施形態では、環Aは、L及びR5と合わせて、
であり、式中、L及びR5は、式(I)、(Ia)、又は(Ib)について上で定義したとおりである。
からなる群から選択され、式中、R5、R13、及びLは、式(I)、(Ia)、又は(Ib)について上で定義したとおりであり、nは0、1、2、3、又は4である。
からなる群から選択され、式中、R5、R13、及びLは、式(I)、(Ia)、又は(Ib)について上で定義したとおりである、化合物、又はその塩である。
であり、式中、L及びR5は、式(I)、(Ia)、又は(Ib)について上で定義したとおりである、化合物、又はその塩である。
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、X3、環A、R1、R2、R3、R4、R5、L、及び
は、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、X3、環A、R1、R2、R3、R4、R5、L、及び
は、式(I)について上で定義したとおりである、化合物、又はその塩である。
は二重結合である、化合物、又はその塩である。例えば、特定の一実施形態において、化合物は、式(III):
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、環A、R1、R2、R3、R4、R5、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、環A、R1、R2、R3、R4、R5、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩である。
は二重結合である、化合物、又はその塩である。
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、R1、R2、R3、R4、R5、R13、L、及びnは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、R1、R2、R3、R4、R5、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、R1、R2、R3、R4、R5、R13、L、及びnは、式(I)について上で定義したとおりである、化合物、又はその塩である。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、R1、R2、R3、R4、R5、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩である。
は単結合である、化合物、又はその塩である。例えば、特定の一実施形態において、化合物は、式(V):
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、環A、R1、R2、R3、R4、R5、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、環A、R1、R2、R3、R4、R5、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩である。
は単結合である、化合物、又はその塩である。例えば、特定の一実施形態において、化合物は、式(VI):
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、R1、R2、R3、R4、R5、R13、L、及びnは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、R1、R2、R3、R4、R5、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、R1、R2、R3、R4、R5、R13、L、及びnは、式(I)について上で定義したとおりである、化合物、又はその塩である。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、R1、R2、R3、R4、R5、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩である。
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、R1、R2、R3、R4、R5、R11、R12、R13、L、及び
は、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、R1、R2、R3、R4、R5、R11、R12、L、及び
は、式(I)について上で定義したとおりである、化合物、又はその塩である。
は二重結合である、化合物、又はその塩である。例えば、特定の一実施形態において、化合物は、式(VIII):
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、R1、R2、R3、R4、R5、R11、R12、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、R1、R2、R3、R4、R5、R11、R12、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩である。
は二重結合である、化合物、又はその塩である。例えば、特定の一実施形態において、化合物は、式(IX):
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、R1、R2、R3、R4、R5、R11、R12、R13、L、及びnは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又は、その塩(例えば薬学的に許容される塩)若しくはエナンチオマーであって、
式中、R1、R2、R3、R4、R5、R11、R12、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩若しくはエナンチオマーである。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、R1、R2、R3、R4、R5、R11、R12、R13、L、及びnは、式(I)について上で定義したとおりである、化合物、又はその塩である。
の化合物、又はその塩(例えば薬学的に許容される塩)であって、
式中、R1、R2、R3、R4、R5、R11、R12、及びLは、式(I)について上で定義したとおりである、化合物、又はその塩である。
である。
からなる群から選択される、化合物、又はその塩である。
からなる群から選択される、化合物、又はその塩である。
からなる群から選択される、化合物、又はその塩である。
からなる群から選択される、化合物、又はその塩である。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、
R1は、−O−C1〜C6−アルキルであり、
R2は、メチルであり、
R3及びR4は、それぞれメチルであり、
Lは、C2〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンであり、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシルからなる群から選択され、式中、R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択され、
各R13基は独立して、H又はハロであり、
nは0、1、2、3、又は4である、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、
R1は、−O−C(CH3)3であり、
R2は、メチルであり、
R3及びR4は、それぞれメチルであり、
Lは、C2〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンであり、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシルからなる群から選択され、式中、R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択され、
nは0である、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、
R1は、−O−C1〜C6−アルキル、又は−N(R8)(R9)であり、式中、R8及びR9は、H、C1〜C4−アルキル、及びフェニルからなる群から独立して選択され、式中、フェニルは、R10で任意に置換されており、式中、R10はヒドロキシであり、
R2は、メチルであり、
R3及びR4はそれぞれ、H、メチル、及びメトキシはからなる群から独立して選択され、
Lは、C2〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンであり、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシルからなる群から選択され、式中、R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択される、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、
R1は、−O−C1〜C6−アルキルであり、
R2は、メチルであり、
R3及びR4は、それぞれメチルであり、
Lは、C2〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンであり、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシルからなる群から選択され、式中、R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択される、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、
R1は、−O−C(CH3)3であり、
R2は、メチルであり、
R3及びR4は、それぞれメチルであり、
Lは、C2〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンであり、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシルからなる群から選択され、式中、R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択される、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、
Lは、C2〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンであり、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシルからなる群から選択され、式中、R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択される、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、L及びR5は、
からなる群から選択される、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、L及びR5は、
からなる群から選択される、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
の化合物、又は、その薬学的に許容される塩若しくはエナンチオマーであって、式中、L及びR5は、
からなる群から選択される、化合物、又は、その薬学的に許容される塩若しくはエナンチオマーに関する。
III.製剤
IV.適応症及び治療方法
ブロモドメイン媒介性障害
同時投与
投与
V.製造物品
略語
LCMS法
SFC法
化合物A
tert−ブチル(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)アセテート
化合物B
tert−ブチル(S)−2−(4−(4−ヨードフェニル)−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)アセテート
ステップ1:tert−ブチル(S)−2−(4−(4−((ジフェニルメチレン)アミノ)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)アセテート
ステップ2:tert−ブチル(S)−2−(4−(4−アミノフェニル)−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)アセテート
ステップ3:tert−ブチル(S)−2−(4−(4−ヨードフェニル)−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)アセテート
実施例1a及び1b
tert−ブチル2−(4−(4−(3−アミノプロパ−1−イン−1−イル)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)アセテート(2つの単一の立体異性体)
実施例2
tert−ブチル(S)−2−(2,3,9−トリメチル−4−(4−(3−(メチルアミノ)プロパ−1−イン−1−イル)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)アセテート
実施例3
tert−ブチル(S)−2−(4−(4−(3−(ジメチルアミノ)プロパ−1−イン−1−イル)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)アセテート
実施例4
tert−ブチル(S)−2−(4−(4−(4−アミノブタ−1−イン−1−イル)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)アセテート
実施例5
tert−ブチル(S)−2−(4−(4−(3−グアニジノプロパ−1−イン−1−イル)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)アセテート
実施例6
tert−ブチル(S,E)−2−(4−(4−(3−アミノプロパ−1−エン−1−イル)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)アセテート
ステップ1:化合物6.2
ステップ2:tert−ブチル(S,E)−2−(4−(4−(3−アミノプロパ−1−エン−1−イル)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)アセテート
実施例7
tert−ブチル(S)−2−(4−(4−(3−ヒドロキシプロパ−1−イン−1−イル)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)アセテート
ステップ1:tert−ブチルジメチル(プロパ−2−イン−1−イルオキシ)シラン
ステップ2:tert−ブチル(S)−2−(4−(4−(3−((tert−ブチルジメチルシリル)オキシ)プロパ−1−イン−1−イル)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)アセテート
ステップ3:tert−ブチル(S)−2−(4−(4−(3−ヒドロキシプロパ−1−イン−1−イル)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)アセテート
実施例8
tert−ブチル(S)−2−(4−(4−(3−(ヒドロキシアミノ)プロパ−1−イン−1−イル)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)アセテート
ステップ1:tert−ブチル(S)−2−(2,3,9−トリメチル−4−(4−(3−((メチルスルホニル)オキシ)プロパ−1−イン−1−イル)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)アセテート
ステップ2:tert−ブチル(S)−2−(4−(4−(3−(ヒドロキシアミノ)プロパ−1−イン−1−イル)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)アセテート
実施例9
tert−ブチル(S)−2−(4−(4−(3−アミノプロピル)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)アセテート
実施例10
tert−ブチル(S)−2−(4−(4−(3−アセトアミドプロパ−1−イン−1−イル)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)アセテート
実施例11
tert−ブチル2−((6S)−4−(4−(3−アミノブタ−1−イン−1−イル)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)アセテート
実施例12
tert−ブチル(S)−2−(4−(4−(3−アミノ−3−メチルブタ−1−イン−1−イル)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)アセテート
実施例13
tert−ブチル(S)−2−(4−(4−(ブタ−1−イン−1−イル)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)アセテート
実施例14
tert−ブチル(S)−2−(2,3,9−トリメチル−4−(4−(プロパ−1−イン−1−イル)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)アセテート
実施例15
メチル4−(5−(3−アミノプロパ−1−イン−1−イル)−3−フルオロピリジン−2−イル)−10−メチル−7−((メチルスルホニル)メチル)−11−オキソ−3,4,10,11−テトラヒドロ−1H−1,4,10−トリアザジベンゾ[cd,f]アズレン−6−カルボキシレート(化合物15)
ステップ1:メチル2−(ブロモメチル)−5−ニトロ−ベンゾエート(化合物15.2)
ステップ2:メチル2−(メチルスルホニルメチル)−5−ニトロ−ベンゾエート(化合物15.3)
ステップ3:メチル5−アミノ−2−(メチルスルホニルメチル)ベンゾエート(化合物15.4)
ステップ4:メチル5−アミノ−4−ヨード−2−(メチルスルホニルメチル)ベンゾエート(化合物15.5)
ステップ5:(E)−2−(5−ブロモ−2−メトキシ−3−ニトロ−4−ピリジル)−N,N−ジメチル−エテンアミン(化合物15.7)
ステップ6:4−ブロモ−7−メトキシ−1H−ピロロ[2,3−c]ピリジン(化合物15.8)
ステップ7:4−ブロモ−7−メトキシ−1−(p−トリルスルホニル)ピロロ[2,3−c]ピリジン(化合物15.9)
ステップ8:4−ブロモ−1−(p−トリルスルホニル)−6H−ピロロ[2,3−c]ピリジン−7−オン(化合物15.10)
ステップ9:4−ブロモ−6−メチル−1−(p−トリルスルホニル)ピロロ[2,3−c]ピリジン−7−オン(化合物15.11)
ステップ10:6−メチル−1−(p−トリルスルホニル)−4−(4,4,5,5−テトラメチル−1,3,2−ジオキサボロラン−2−イル)ピロロ[2,3−c]ピリジン−7−オン(化合物15.12)
ステップ11:メチル5−アミノ−4−[6−メチル−7−オキソ−1−(p−トリルスルホニル)ピロロ[2,3−c]ピリジン−4−イル]−2−(メチルスルホニルメチル)ベンゾエート(化合物15.13)
ステップ12:メチル5−((5−クロロ−3−フルオロピリジン−2−イル)アミノ)−4−(6−メチル−7−オキソ−1−トシル−6,7−ジヒドロ−1H−ピロロ[2,3−c]ピリジン−4−イル)−2−((メチルスルホニル)メチル)ベンゾエート(化合物15.15)
ステップ13:メチル5−((5−クロロ−3−フルオロピリジン−2−イル)アミノ)−4−(6−メチル−7−オキソ−6,7−ジヒドロ−1H−ピロロ[2,3−c]ピリジン−4−イル)−2−((メチルスルホニル)メチル)ベンゾエート(化合物15.16)
ステップ14:メチル4−(5−クロロ−3−フルオロピリジン−2−イル)−10−メチル−7−((メチルスルホニル)メチル)−11−オキソ−3,4,10,11−テトラヒドロ−1H−1,4,10−トリアザジベンゾ[cd,f]アズレン−6−カルボキシレート(化合物15.17)
ステップ15:メチル4−(5−(3−((tert−ブトキシカルボニル)アミノ)プロパ−1−イン−1−イル)−3−フルオロピリジン−2−イル)−10−メチル−7−((メチルスルホニル)メチル)−11−オキソ−3,4,10,11−テトラヒドロ−1H−1,4,10−トリアザジベンゾ[cd,f]アズレン−6−カルボキシレート(化合物15.19)
ステップ16:メチル4−(5−(3−アミノプロパ−1−イン−1−イル)−3−フルオロピリジン−2−イル)−10−メチル−7−((メチルスルホニル)メチル)−11−オキソ−3,4,10,11−テトラヒドロ−1H−1,4,10−トリアザジベンゾ[cd,f]アズレン−6−カルボキシレート(化合物15)
実施例16
tert−ブチル(S)−2−(4−(4−(4−アミノブチル)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)アセテート
実施例17
tert−ブチル(S,E)−2−(4−(4−(4−アミノブタ−1−エン−1−イル)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)アセテート
ステップ1:化合物17.2
ステップ2:tert−ブチル(S,E)−2−(4−(4−(4−アミノブタ−1−エン−1−イル)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)アセテート
実施例20
tert−ブチル(S,E)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−エン−1−イル)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)アセテート
ステップ1:化合物20.2
ステップ2:化合物20.3
ステップ3:tert−ブチル(S,E)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−エン−1−イル)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)アセテート
実施例23
tert−ブチル(S)−2−(4−(4−(4−(ヒドロキシアミノ)ブチル)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)アセテート
実施例24
tert−ブチル(S)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−イン−1−イル)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)アセテート
ステップ1:化合物24.2
ステップ2:化合物24.3
ステップ3:tert−ブチル(S)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−イン−1−イル)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)アセテート
生物学的アッセイ
実施例A:BRD4 BD1及びBD2生化学的結合アッセイ
Claims (72)
- 式(I):
の化合物又はその薬学的に許容される塩若しくはエナンチオマーであって、
X1は、S又はC(R11)であり、
X2は、存在しないか又はC(R12)であり、
X3は、N又はOであり、
は、単結合又は二重結合であり、式中、
X1がC(R11)である場合、
は、X1とX2との間の二重結合であり、
X3がNである場合、
は、X3と分子の残りの部分との間の二重結合であり、
環Aは、フェニル又は6員のヘテロアリールであり、環Aは任意に、ハロ、ヒドロキシ、−C1〜3−アルキル、−O−C1〜3−アルキル、及び−NH2からなる群から選択される1つ以上の置換基で更に置換されており、
R1は、−O−C1〜C6−アルキル、又は−N(R8)(R9)であり、式中、
R8及びR9は、H、C1〜C4−アルキル、及びフェニルからなる群から独立して選択され、式中、フェニルは、R10で任意に置換されており、式中、R10はヒドロキシルであり、
R2は、メチルであり、
R3、R4、R11、及びR12はそれぞれ、H、メチル、及びメトキシからなる群から独立して選択され、
Lは、C1〜C4アルキレン、C2〜C4アルケニレン、又はC2〜C4アルキニレンであり、
R5は、−N(R6)(R7);−C(H)(CH3)−NH2;−C(CH3)2−NH2;メチル;及びヒドロキシルからなる群から選択され、式中、R6及びR7は、H、メチル、−C(NH)−NH2、ヒドロキシ、及び−C(O)CH3からなる群から独立して選択される、化合物、又はその薬学的に許容される塩若しくはエナンチオマー。 - R5が、−N(R6)(R7)であり、
R6及びR7が、H、メチル、−C(NH)−NH2、及びヒドロキシからなる群から独立して選択され、
Lが、C3〜C4アルキレン、C3〜C4アルケニレン、又はC3〜C4アルキニレンである、
請求項1に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。 - 環Aが、任意に置換されたフェニル、任意に置換されたピリジニル、及び任意に置換されたピリミジニルからなる群から選択される、請求項1〜3のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R1が、−O−C1〜C4−アルキルである、請求項1〜17のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R1が、−O−t−ブチルである、請求項18に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R1が、−O−CH3である、請求項18に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R1が、−N(R8)(R9)である、請求項1〜17のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R8及びR9が、それぞれHである、請求項21に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R8がHであり、R9がC1〜C4アルキルである、請求項21に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R8がHであり、R9がエチルである、請求項23に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R8がHであり、R9が、R10で置換されたフェニルである、請求項21に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R3及びR4が、それぞれメチルである、請求項1〜26のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R3及びR4が、それぞれHである、請求項12〜26のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R3がメトキシであり、R4がHである、請求項12〜26のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R5が、−N(R6)(R7)である、請求項1〜29のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R6及びR7が、それぞれHである、請求項30に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R6がHであり、R7がメチルである、請求項30に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R6及びR7が、それぞれメチルである、請求項30に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R6がHであり、R7が−C(NH)−NH2である、請求項30に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R6がHであり、R7がヒドロキシである、請求項30に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- Lが、C3〜C4アルキレンである、請求項1〜35のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- Lが、C3〜C4アルケニレンである、請求項1〜35のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- Lが、C3〜C4アルキニレンである、請求項1〜35のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- 請求項1〜45のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー、及び1種以上の薬学的に許容される賦形剤を含む、医薬組成物。
- 追加の生物活性剤を更に含む、請求項46に記載の医薬組成物。
- 疾患又は障害の治療を必要とするヒトにおける、疾患又は障害の治療方法であって、前記ヒトに、有効量の、請求項1〜45のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー、又は請求項46若しくは47に記載の組成物を投与することを含む、方法。
- 前記疾患又は前記障害がブロモドメイン媒介性疾患である、請求項48に記載の方法。
- 前記疾患が癌である、請求項48に記載の方法。
- 前記癌が、聴神経腫、急性白血病、急性リンパ性白血病、急性骨髄性白血病、急性T細胞白血病、基底細胞癌、胆管癌、膀胱癌、脳腫瘍、乳癌、気管支原性癌、子宮頚癌、軟骨肉腫、脊索腫、絨毛癌、慢性白血病、慢性リンパ性白血病、慢性骨髄性(顆粒球性)白血病、慢性骨髄性白血病、結腸癌、結腸直腸癌、頭蓋咽頭腫、嚢胞腺癌、びまん性大細胞型B細胞リンパ腫、異常増殖性変化、胎児性癌、子宮体癌、内皮肉腫、脳室上衣腫、上皮癌、赤白血病、食道癌、エストロゲン受容体陽性乳癌、本態性血小板血症、ユーイング腫瘍、線維肉腫、濾胞性リンパ腫、生殖細胞精巣癌、膠腫、グリア芽腫、膠肉腫、重鎖病、血管芽細胞腫、肝癌、肝細胞癌、ホルモン不感性前立腺癌、平滑筋肉腫、白血病、脂肪肉腫、肺癌、リンパ管内皮肉腫、リンパ管肉腫、リンパ芽球性白血病、リンパ腫(ホジキン及び非ホジキン)、膀胱、胸部、結腸、肺、卵巣、膵臓、前立腺、皮膚及び子宮の悪性腫瘍及び増殖過剰障害、T細胞又はB細胞由来のリンパ系悪性腫瘍、髄様癌、髄芽腫、黒色腫、髄膜腫、中皮腫、多発性骨髄腫、骨髄性白血病、骨髄腫、粘液肉腫、神経芽細胞腫、NUT正中線癌(NMC)、非小細胞肺癌、乏突起膠腫、口腔癌、骨原性肉腫、卵巣癌、膵癌、乳頭腺癌、乳頭状癌、松果体腫、真性多血症、前立腺癌、直腸癌、腎細胞癌、網膜芽細胞腫、横紋筋肉腫、肉腫、脂腺癌、セミノーマ、皮膚癌、小細胞肺癌、充実性腫瘍(癌及び肉腫)、小細胞肺癌、胃癌、扁平上皮細胞癌、滑膜腫、汗腺癌、甲状腺癌、ワルデンストレームマクログロブリン血症、精巣腫瘍、子宮癌、並びにウィルムス腫瘍からなる群から選択される、請求項50に記載の方法。
- 前記疾患が、アジソン病、急性痛風、強直性脊椎炎、喘息、アテローム性動脈硬化症、ベーチェット病、水疱性皮膚病、慢性閉塞性肺疾患(COPD)、クローン病、皮膚炎、湿疹、巨細胞動脈炎、糸球体腎炎、肝炎、下垂体炎、炎症性腸疾患、川崎病、狼瘡性腎炎、多発性硬化症、心筋炎、筋炎、腎炎、臓器移植拒絶反応、変形性関節症、膵炎、心膜炎、結節性多発性動脈炎、肺炎、原発性胆汁性肝硬変、乾癬、乾癬性関節炎、関節リウマチ、強膜炎、硬化性胆管炎、敗血症、全身性エリテマトーデス、高安動脈炎、毒素性ショック、甲状腺炎、I型糖尿病、潰瘍性大腸炎、ぶどう膜炎、白斑、血管炎、及びヴェゲナー肉芽腫症からなる群から選択される自己免疫疾患又は炎症性疾患である、請求項48に記載の方法。
- 前記疾患又は前記障害が、AIDS;慢性腎疾患、糖尿病性腎症、高血圧性腎症、HIV随伴腎症、糸球体腎炎、狼瘡性腎炎、IgA腎症、巣状分節性糸球体硬化症、膜糸球体腎炎、微小変化病、多発性嚢胞腎疾患、及び管状間質性腎炎;急性腎損傷又は疾患又は状態;肥満;脂質異常症;高コレステロール血症;アルツハイマー病;メタボリックシンドローム;肝脂肪症;2型糖尿病;インスリン抵抗性;並びに糖尿病性網膜症からなる群から選択される、請求項48に記載の方法。
- 細胞内でのブロモドメイン含有タンパク質の分解方法であって、前記方法が、前記細胞を、有効量の、請求項1〜45のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマーを含む組成物に暴露することを含み、前記化合物が、前記ブロモドメイン含有タンパク質の分解を引き起こす、方法。
- 前記ブロモドメイン含有タンパク質がブロモドメイン含有タンパク質4(BRD4)である、請求項54に記載の方法。
- Lが、C2〜C4アルキレンである、請求項1及び3〜35のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R5が、CH3、OH、NH2、NH(CH3)、N(CH3)2、NH(OH)、NH−C(NH)(NH2)、NH−C(O)(CH3)、CH(CH3)−NH2、及びC(CH3)2−NH2からなる群から選択される、請求項1〜35のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- R5が、NH2、NH(CH3)、N(CH3)2、NH(OH)、CH(CH3)−NH2、及びNH−C(NH)(NH2)からなる群から選択される、請求項1〜35のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- 前記化合物が
tert−ブチル2−(4−(4−(3−アミノプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(2,3,9−トリメチル−4−(4−(3−(メチルアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(3−(ジメチルアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(4−アミノブタ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(3−グアニジノプロパ−1−イン−1−イル)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)アセテート
tert−ブチル(E)−2−(4−(4−(3−アミノプロパ−1−エン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(3−ヒドロキシプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(3−(ヒドロキシアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(3−アミノプロピル)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)アセテート、
tert−ブチル2−(4−(4−(3−アセトアミドプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(3−アミノブタ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(3−アミノ−3−メチルブタ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(ブタ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(2,3,9−トリメチル−4−(4−(プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(4−アミノブチル)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)アセテート、
tert−ブチル(E)−2−(4−(4−(4−アミノブタ−1−エン−1−イル)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)アセテート、
tert−ブチル(E)−2−(4−(4−(4−アミノブタ−2−エン−1−イル)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)アセテート、
tert−ブチル(Z)−2−(4−(4−(4−アミノブタ−3−エン−1−イル)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)アセテート、
tert−ブチル(E)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−エン−1−イル)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)アセテート、
tert−ブチル(E)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−2−エン−1−イル)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)アセテート、
tert−ブチル(Z)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−3−エン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(4−(ヒドロキシアミノ)ブチル)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)アセテート、
tert−ブチル2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(4−(ヒドロキシアミノ)ブタ−2−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(4−(ヒドロキシアミノ)ブタ−3−イン−1−イル)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)アセテート、
tert−ブチル2−(4−(4−(4−アミノブタ−2−イン−1−イル)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」)アセテート、及び
tert−ブチル2−(4−(4−(4−アミノブタ−3−イン−1−イル)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)アセテート、
からなる群から選択される、請求項1に記載の化合物、
又はその薬学的に許容される塩若しくはエナンチオマー。 - 前記化合物が
tert−ブチル(S)−2−(4−(4−(3−アミノプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(3−アミノプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(2,3,9−トリメチル−4−(4−(3−(メチルアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(2,3,9−トリメチル−4−(4−(3−(メチルアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(3−(ジメチルアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(3−(ジメチルアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(4−アミノブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(4−アミノブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(3−グアニジノプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(3−グアニジノプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(S,E)−2−(4−(4−(3−アミノプロパ−1−エン−1−イル)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)アセテート、
tert−ブチル(R,E)−2−(4−(4−(3−アミノプロパ−1−エン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(3−ヒドロキシプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(3−ヒドロキシプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(3−(ヒドロキシアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(3−(ヒドロキシアミノ)プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(3−アミノプロピル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(3−アミノプロピル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(3−アセトアミドプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(3−アセトアミドプロパ−1−イン−1−イル)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)アセテート、
tert−ブチル2−((6S)−4−(4−(3−アミノブタ−1−イン−1−イル)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)アセテート、
tert−ブチル2−((6R)−4−(4−(3−アミノブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(3−アミノ−3−メチルブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(3−アミノ−3−メチルブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(ブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(ブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(2,3,9−トリメチル−4−(4−(プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(2,3,9−トリメチル−4−(4−(プロパ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(4−アミノブチル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(4−アミノブチル)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)アセテート、
tert−ブチル(S,E)−2−(4−(4−(4−アミノブタ−1−エン−1−イル)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)アセテート、
tert−ブチル(R,E)−2−(4−(4−(4−アミノブタ−1−エン−1−イル)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)アセテート、
tert−ブチル(S,E)−2−(4−(4−(4−アミノブタ−2−エン−1−イル)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)アセテート、
tert−ブチル(R,E)−2−(4−(4−(4−アミノブタ−2−エン−1−イル)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)アセテート、
tert−ブチル(S,Z)−2−(4−(4−(4−アミノブタ−3−エン−1−イル)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)アセテート、
tert−ブチル(R,Z)−2−(4−(4−(4−アミノブタ−3−エン−1−イル)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)アセテート、
tert−ブチル(S,E)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−エン−1−イル)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)アセテート、
tert−ブチル(R,E)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−エン−1−イル)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)アセテート、
tert−ブチル(S,E)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−2−エン−1−イル)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)アセテート
tert−ブチル(R,E)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−2−エン−1−イル)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)アセテート、
tert−ブチル(S,Z)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−3−エン−1−イル)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)アセテート、
tert−ブチル(R,Z)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−3−エン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(4−(ヒドロキシアミノ)ブチル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(4−(ヒドロキシアミノ)ブチル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−1−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−2−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−2−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−3−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(4−(ヒドロキシアミノ)ブタ−3−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(4−アミノブタ−2−イン−1−イル)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)アセテート、
tert−ブチル(R)−2−(4−(4−(4−アミノブタ−2−イン−1−イル)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)アセテート、
tert−ブチル(S)−2−(4−(4−(4−アミノブタ−3−イン−1−イル)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)アセテート、及び
tert−ブチル(R)−2−(4−(4−(4−アミノブタ−3−イン−1−イル)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)アセテート、
からなる群から選択される、請求項1に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。 - 医学療法に用いるための、請求項1〜45、若しくは56〜63のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー。
- ブロモドメイン媒介性障害の治療に用いるための、請求項1〜45、若しくは56〜63のいずれか一項に記載の化合物、請求項1〜45、若しくは56〜61のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマー、又は請求項46〜47のいずれか一項に記載の組成物。
- 前記ブロモドメイン媒介性障害が癌である、請求項65に記載の化合物又は組成物。
- ブロモドメイン媒介性障害の治療のための、請求項1〜45、若しくは56〜63のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマーの使用。
- ブロモドメイン媒介性障害の治療のための薬剤を調製するための、請求項1〜45、若しくは56〜63のいずれか一項に記載の化合物、又はその薬学的に許容される塩若しくはエナンチオマーの使用。
- 前記ブロモドメイン媒介性障害が癌である、請求項67又は68に記載の使用。
- 請求項1〜45、又は56〜63のいずれか一項に記載の化合物の調製方法。
- 前記化合物が、請求項68に記載の方法により得られる、請求項1〜45、又は56〜63のいずれか一項に記載の化合物。
- 上記に記載する通りの発明。
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