基本信息:
- 专利标题: タンキラーゼ阻害剤としての1,2,4−トリアゾール誘導体
- 申请号:JP2020571480 申请日:2019-06-19
- 公开(公告)号:JP2021533085A 公开(公告)日:2021-12-02
- 发明人: クラウス、ステファン , ナザレ、マルク , レフティオ、ラリ , ヴァーラー、ヨー , ヴェガート、アニタ , レーンダーズ、ルーベン ジェラーダス ジョージ
- 申请人: オスロ ユニヴェルジテットサイケフス ホーエフ , フォルシュングスフェアブント ベルリン エー ファウ , Forschungsverbund Berlin e.V. , ユニバーシティ オブ オウル
- 申请人地址: ノルウェー、エヌ−0424 オスロ、ニーダレン、ポストボクス 4950
- 专利权人: オスロ ユニヴェルジテットサイケフス ホーエフ,フォルシュングスフェアブント ベルリン エー ファウ,Forschungsverbund Berlin e.V.,ユニバーシティ オブ オウル
- 当前专利权人: オスロ ユニヴェルジテットサイケフス ホーエフ,フォルシュングスフェアブント ベルリン エー ファウ,Forschungsverbund Berlin e.V.,ユニバーシティ オブ オウル
- 当前专利权人地址: ノルウェー、エヌ−0424 オスロ、ニーダレン、ポストボクス 4950
- 代理人: 特許業務法人池内アンドパートナーズ
- 优先权: GB1810071.9 2018-06-19
- 国际申请: GB2019051728 JP 2019-06-19
- 国际公布: WO2019243822 JP 2019-12-26
- 主分类号: A61K31/506
- IPC分类号: A61K31/506 ; C07D471/04 ; C07D403/04 ; C07D417/14 ; C07D417/04 ; A61K31/4375 ; A61K31/4439 ; A61K31/427 ; A61K31/4709 ; A61P43/00 ; A61P35/00 ; A61P17/02 ; A61P31/22 ; A61P31/12 ; A61P17/00 ; A61P11/00 ; A61P13/12 ; A61P3/08 ; A61P3/00 ; C07D401/14
The present invention relates to compounds of formula (I), tautomers, stereoisomers, pharmaceutically acceptable salts and pro-drugs thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy wherein a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); Y represents: an aryl or heteroaryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); a 5- or 6-membered, saturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or a C3-6 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); and Z represents: an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); or an unsaturated, 5- to 10-membered mono- or bicyclic heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl). These compounds find particular use in the treatment and/or prevention of a disease or disorder responsive to inhibition of tankyrase 1 and/or 2, for example a disorder which is mediated by tankyrase 1 and/or 2 such as cancer.
信息查询:
EspacenetIPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K31/00 | 含有机有效成分的医药配制品 |
--------A61K31/33 | .杂环化合物 |
----------A61K31/335 | ..仅有氧作为环杂原子的,例如制霉色基素 |
------------A61K31/40 | ...有仅以1个氮作为环杂原子的五元环的,例如舒必利、琥珀酰亚胺、托尔米丁、甲氧吡丁苯 |
--------------A61K31/50 | ....哒嗪;氢化哒嗪 |
----------------A61K31/506 | .....未稠合的并且含有另外杂环的 |