JP2017526731A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017526731A5 JP2017526731A5 JP2017514515A JP2017514515A JP2017526731A5 JP 2017526731 A5 JP2017526731 A5 JP 2017526731A5 JP 2017514515 A JP2017514515 A JP 2017514515A JP 2017514515 A JP2017514515 A JP 2017514515A JP 2017526731 A5 JP2017526731 A5 JP 2017526731A5
- Authority
- JP
- Japan
- Prior art keywords
- butyl
- methyl
- cancer
- pharmaceutically acceptable
- 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
Links
- 150000003839 salts Chemical class 0.000 claims 39
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 36
- -1 —CF 3 Chemical group 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 14
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 14
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 13
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 13
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 12
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 12
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 12
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 9
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 9
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 9
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 9
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 7
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 6
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 6
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004850 cyclobutylmethyl group Chemical group C1(CCC1)C* 0.000 claims 6
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 6
- 125000004851 cyclopentylmethyl group Chemical group C1(CCCC1)C* 0.000 claims 6
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 6
- 125000006001 difluoroethyl group Chemical group 0.000 claims 6
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 6
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 4
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 3
- 208000006454 hepatitis Diseases 0.000 claims 3
- 231100000283 hepatitis Toxicity 0.000 claims 3
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 241000700605 Viruses Species 0.000 claims 2
- DLGYNVMUCSTYDQ-UHFFFAOYSA-N azane;pyridine Chemical compound N.C1=CC=NC=C1 DLGYNVMUCSTYDQ-UHFFFAOYSA-N 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 108091052242 Bromo- and Extra-Terminal domain (BET) family Proteins 0.000 claims 1
- WRNSJZMTERMQLP-RWWKDMOOSA-N C(C)(=O)N1C2CN(C(C1)C2)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C Chemical compound C(C)(=O)N1C2CN(C(C1)C2)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C WRNSJZMTERMQLP-RWWKDMOOSA-N 0.000 claims 1
- XGTBENVKMVXFJO-OYHNWAKOSA-N C(C)(=O)N1C[C@@H](N(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C)C Chemical compound C(C)(=O)N1C[C@@H](N(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C)C XGTBENVKMVXFJO-OYHNWAKOSA-N 0.000 claims 1
- OWRSQNNRKFOWNK-VBURHUQHSA-N C(C)(=O)N1C[C@H](N([C@H](C1)C)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C)C Chemical compound C(C)(=O)N1C[C@H](N([C@H](C1)C)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C)C OWRSQNNRKFOWNK-VBURHUQHSA-N 0.000 claims 1
- GHSNBXPTSMIQPL-OYHNWAKOSA-N C(C)(=O)N1[C@H](CN(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C)C Chemical compound C(C)(=O)N1[C@H](CN(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C)C GHSNBXPTSMIQPL-OYHNWAKOSA-N 0.000 claims 1
- CPKBVGXUMOILKV-JOCHJYFZSA-N C(CCC)(=O)N1CCN(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C Chemical compound C(CCC)(=O)N1CCN(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C CPKBVGXUMOILKV-JOCHJYFZSA-N 0.000 claims 1
- KFVXVHFSAAIXQI-JOCHJYFZSA-N C1(CC1)C(=O)N1CCN(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C Chemical compound C1(CC1)C(=O)N1CCN(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C KFVXVHFSAAIXQI-JOCHJYFZSA-N 0.000 claims 1
- HWZQFCPIMIHIHR-HSZRJFAPSA-N C1(CCC1)C(=O)N1CCN(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C Chemical compound C1(CCC1)C(=O)N1CCN(CC1)C1=NC2=CC=C(C3=C2N1[C@H](CO3)C1=NC=CC=C1)C=1C(=NOC=1C)C HWZQFCPIMIHIHR-HSZRJFAPSA-N 0.000 claims 1
- LSAGBYDJYRHTRW-JOCHJYFZSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)(C)NC(C)=O)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)(C)NC(C)=O)C LSAGBYDJYRHTRW-JOCHJYFZSA-N 0.000 claims 1
- URTLKQGQGJOMMK-XMMPIXPASA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(=O)C1CC1)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(=O)C1CC1)C)C URTLKQGQGJOMMK-XMMPIXPASA-N 0.000 claims 1
- SATUWZAHXGFNLD-RUZDIDTESA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(=O)C1CCC1)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(=O)C1CCC1)C)C SATUWZAHXGFNLD-RUZDIDTESA-N 0.000 claims 1
- WGVACKKKDBPNCF-HSZRJFAPSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(=O)N(C)C)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(=O)N(C)C)C)C WGVACKKKDBPNCF-HSZRJFAPSA-N 0.000 claims 1
- HHQXLCQBSIIXEP-XMMPIXPASA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(C(C)(C)C)=O)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(C(C)(C)C)=O)C)C HHQXLCQBSIIXEP-XMMPIXPASA-N 0.000 claims 1
- APUQYQHFLNFUIV-XMMPIXPASA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(C(C)C)=O)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(C(C)C)=O)C)C APUQYQHFLNFUIV-XMMPIXPASA-N 0.000 claims 1
- KQJJFAFXMLVFRW-HSZRJFAPSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(C)=O)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(C)=O)C)C KQJJFAFXMLVFRW-HSZRJFAPSA-N 0.000 claims 1
- KGXSUEGVKXWRQI-HSZRJFAPSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(CC)=O)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(CC)=O)C)C KGXSUEGVKXWRQI-HSZRJFAPSA-N 0.000 claims 1
- ADEWRUVSNLFKIT-XMMPIXPASA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(CCC)=O)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(C(CCC)=O)C)C ADEWRUVSNLFKIT-XMMPIXPASA-N 0.000 claims 1
- SAVAOMJTQJFGSR-JOCHJYFZSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(S(=O)(=O)C)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(S(=O)(=O)C)C)C SAVAOMJTQJFGSR-JOCHJYFZSA-N 0.000 claims 1
- SPOSSZBPBDNJNT-XMMPIXPASA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(S(=O)(=O)C1CC1)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)N(S(=O)(=O)C1CC1)C)C SPOSSZBPBDNJNT-XMMPIXPASA-N 0.000 claims 1
- DUPQOQJOCVRTBS-HSZRJFAPSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NC(=O)C1CC1)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NC(=O)C1CC1)C DUPQOQJOCVRTBS-HSZRJFAPSA-N 0.000 claims 1
- PUJWPYZXZNJVIG-XMMPIXPASA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NC(=O)C1CCC1)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NC(=O)C1CCC1)C PUJWPYZXZNJVIG-XMMPIXPASA-N 0.000 claims 1
- AOHRCIHLNZGGEC-HSZRJFAPSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NC(C(C)(C)C)=O)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NC(C(C)(C)C)=O)C AOHRCIHLNZGGEC-HSZRJFAPSA-N 0.000 claims 1
- OTNSFSFYTFKMEB-HSZRJFAPSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NC(CCC)=O)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NC(CCC)=O)C OTNSFSFYTFKMEB-HSZRJFAPSA-N 0.000 claims 1
- SJGWGZCUULTQIO-JOCHJYFZSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NS(=O)(=O)CC)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCC(CC1)NS(=O)(=O)CC)C SJGWGZCUULTQIO-JOCHJYFZSA-N 0.000 claims 1
- CYANTQDGHUIJGZ-JOCHJYFZSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCN(CC1)C(C(C)(C)C)=O)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCN(CC1)C(C(C)(C)C)=O)C CYANTQDGHUIJGZ-JOCHJYFZSA-N 0.000 claims 1
- OZALPVLVYBXRKE-JOCHJYFZSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCN(CC1)C(C(C)C)=O)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCN(CC1)C(C(C)C)=O)C OZALPVLVYBXRKE-JOCHJYFZSA-N 0.000 claims 1
- QQLIQKOWTUKCCX-OAQYLSRUSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCN(CC1)C(COC)=O)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1CCN(CC1)C(COC)=O)C QQLIQKOWTUKCCX-OAQYLSRUSA-N 0.000 claims 1
- QVFNWZZKUKTJTE-GAJHUEQPSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1C[C@@H](N(CC1)C(C(C)C)=O)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1C[C@@H](N(CC1)C(C(C)C)=O)C)C QVFNWZZKUKTJTE-GAJHUEQPSA-N 0.000 claims 1
- DGRMYTISESUMFZ-KSFYIVLOSA-N CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1C[C@@H](N(CC1)C(CC)=O)C)C Chemical compound CC1=NOC(=C1C1=CC=C2C=3N([C@H](COC=31)C1=NC=CC=C1)C(=N2)N1C[C@@H](N(CC1)C(CC)=O)C)C DGRMYTISESUMFZ-KSFYIVLOSA-N 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010007953 Central nervous system lymphoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 claims 1
- 241000701806 Human papillomavirus Species 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000005016 Intestinal Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010023825 Laryngeal cancer Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000009565 Pharyngeal Neoplasms Diseases 0.000 claims 1
- 206010034811 Pharyngeal cancer Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000000389 T-cell leukemia Diseases 0.000 claims 1
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 206010043515 Throat cancer Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 1
- 201000000053 blastoma Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000008184 embryoma Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000024519 eye neoplasm Diseases 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008106 ocular cancer Diseases 0.000 claims 1
- 208000027500 optic nerve neoplasm Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 208000010916 pituitary tumor Diseases 0.000 claims 1
- 208000016800 primary central nervous system lymphoma Diseases 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
- 206010062261 spinal cord neoplasm Diseases 0.000 claims 1
- 210000003802 sputum Anatomy 0.000 claims 1
- 208000024794 sputum Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 241000701161 unidentified adenovirus Species 0.000 claims 1
- 241001529453 unidentified herpesvirus Species 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 206010046885 vaginal cancer Diseases 0.000 claims 1
- 208000013139 vaginal neoplasm Diseases 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462050500P | 2014-09-15 | 2014-09-15 | |
| US62/050,500 | 2014-09-15 | ||
| PCT/US2015/049909 WO2016044130A1 (en) | 2014-09-15 | 2015-09-14 | Tricyclic heterocycles for use as bet protein inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017526731A JP2017526731A (ja) | 2017-09-14 |
| JP2017526731A5 true JP2017526731A5 (enExample) | 2018-10-25 |
| JP6599979B2 JP6599979B2 (ja) | 2019-10-30 |
Family
ID=54207768
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017514515A Active JP6599979B2 (ja) | 2014-09-15 | 2015-09-14 | Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US9527864B2 (enExample) |
| EP (1) | EP3194406B8 (enExample) |
| JP (1) | JP6599979B2 (enExample) |
| ES (1) | ES2855225T3 (enExample) |
| TW (1) | TWI712603B (enExample) |
| WO (1) | WO2016044130A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2903881C (en) | 2013-03-15 | 2021-05-18 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles 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 |
| WO2015164480A1 (en) | 2014-04-23 | 2015-10-29 | Incyte Corporation | 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| TW201722966A (zh) | 2015-10-29 | 2017-07-01 | 英塞特公司 | Bet蛋白質抑制劑之非晶固體形式 |
| SMT202300155T1 (it) | 2016-06-20 | 2023-07-20 | Incyte Corp | Forme solide cristalline di un inibitore di bet |
| TW202019408A (zh) * | 2018-06-28 | 2020-06-01 | 美商永恒生物科技公司 | 稠合三環雜環化合物及其治療用途 |
| CN112552314B (zh) * | 2018-08-24 | 2022-03-04 | 杭州阿诺生物医药科技有限公司 | Sting激动剂小分子抗肿瘤化合物及其应用 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (154)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS59170313A (ja) | 1983-03-14 | 1984-09-26 | Kurimoto Iron Works Ltd | スクリ−ンゲ−ト |
| JPS6085739U (ja) | 1983-11-18 | 1985-06-13 | クラリオン株式会社 | テ−プレコ−ダにおけるピンチロ−ラ装置 |
| JPH0314566A (ja) | 1989-06-09 | 1991-01-23 | Sankyo Co Ltd | ベンズイミダゾール誘導体 |
| US5244912A (en) | 1991-03-28 | 1993-09-14 | Eli Lilly And Company | 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz(cd)indoles and pharmaceutical use thereof |
| FR2710915B1 (fr) | 1993-10-04 | 1995-11-24 | Synthelabo | Dérivés de pipéridine, leur préparation et leur utilisation en thérapeutique. |
| FR2731708B1 (fr) * | 1995-03-13 | 1997-04-30 | Synthelabo | Derives de piperidine, leur procede de preparation et leur application en therapeutique |
| FR2747678B1 (fr) * | 1996-04-22 | 1998-05-22 | Synthelabo | Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique |
| CN1554341A (zh) | 2000-04-21 | 2004-12-15 | �������Ŷ���Լ��������˾ | 用于治疗纤维肌痛和慢性疲劳综合症的化合物 |
| KR100786927B1 (ko) | 2000-06-28 | 2007-12-17 | 스미스클라인비이참피이엘시이 | 습식 분쇄방법 |
| US6919334B2 (en) | 2002-09-12 | 2005-07-19 | Wyeth | Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine |
| NZ539952A (en) | 2002-11-22 | 2008-05-30 | Japan Tobacco Inc | Fused bicyclic nitrogen-containing heterocyclic compounds for treating diabetes, obesity and syndrome X |
| EP1462103A1 (en) | 2003-03-25 | 2004-09-29 | Faust Pharmaceuticals | NO donors, combination products and uses as modulators of neurotransmitter release |
| CA2554774A1 (en) | 2004-02-23 | 2005-09-01 | Dainippon Sumitomo Pharma Co., Ltd. | Novel heterocyclic compound |
| WO2005099688A2 (en) | 2004-04-07 | 2005-10-27 | Takeda Pharmaceutical Company Limited | Cyclic compounds |
| DE102005011058A1 (de) | 2005-03-10 | 2006-09-14 | Merck Patent Gmbh | Substituierte Tetrahydro-pyrrolo-chinolinderivate |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| MX2008001152A (es) | 2005-08-05 | 2008-04-02 | Astrazeneca Ab | Benzimidazoles triciclicos y su uso como moduladores del receptor de glutamato metabotropico. |
| US8975259B2 (en) | 2007-04-27 | 2015-03-10 | University Of Rochester | Compositions and methods for inhibiting G protein signaling |
| US9603848B2 (en) | 2007-06-08 | 2017-03-28 | Senomyx, Inc. | Modulation of chemosensory receptors and ligands associated therewith |
| US8633186B2 (en) | 2007-06-08 | 2014-01-21 | Senomyx Inc. | Modulation of chemosensory receptors and ligands associated therewith |
| US7928111B2 (en) | 2007-06-08 | 2011-04-19 | Senomyx, Inc. | Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors |
| WO2009020559A2 (en) | 2007-08-03 | 2009-02-12 | The J. David Gladstone Institutes | Agents that inhibit p-tefb interactions and methods of use thereof |
| US8476260B2 (en) | 2007-12-28 | 2013-07-02 | Mitsubishi Tanabe Pharma Corporation | Antitumor agent |
| DE102008052618A1 (de) | 2008-10-21 | 2010-04-22 | Henkel Ag & Co. Kgaa | Tricyclische Aldehyde und C,H-acide Verbindungen |
| WO2010111626A2 (en) | 2009-03-27 | 2010-09-30 | Takeda Pharmaceutical Company Limited | Poly (adp-ribose) polymerase (parp) inhibitors |
| TW201105681A (en) | 2009-06-10 | 2011-02-16 | Janssen Pharmaceutica Nv | Benzimidazole derivatives useful as TRPM8 channel modulators |
| TW201103941A (en) | 2009-06-10 | 2011-02-01 | Janssen Pharmaceutica Nv | Benzimidazole derivatives useful as TRPM8 channel modulators |
| WO2011024987A1 (ja) | 2009-08-31 | 2011-03-03 | 塩野義製薬株式会社 | 芳香族縮合へテロ環誘導体およびそれらを含有する医薬組成物 |
| GB0919431D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| MX2012005295A (es) | 2009-11-05 | 2012-06-19 | Glaxosmithkline Llc | Inhibidor de bromodominio de benzodiazepina. |
| ES2539964T3 (es) | 2009-11-05 | 2015-07-07 | Glaxosmithkline Llc | Procedimiento novedoso |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| US9102677B2 (en) | 2009-11-05 | 2015-08-11 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| WO2011133722A2 (en) | 2010-04-23 | 2011-10-27 | Kineta, Inc. | Anti-viral compounds |
| MX362384B (es) | 2010-05-14 | 2019-01-15 | Dana Farber Cancer Inst Inc | Composiciones y metodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos. |
| MX354217B (es) | 2010-05-14 | 2018-02-19 | 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 |
| CA2799373A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for modulating metabolism |
| US9085582B2 (en) | 2010-06-22 | 2015-07-21 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| KR20130116358A (ko) | 2011-02-09 | 2013-10-23 | 에프. 호프만-라 로슈 아게 | Pi3 키나아제 억제제로서 헤테로사이클릭 화합물 |
| CA2828212A1 (en) | 2011-02-23 | 2012-08-30 | Shiraz Mujtaba | Inhibitors of bromodomains as modulators of gene expression |
| GB201106743D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201106750D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201106799D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201107325D0 (en) | 2011-05-04 | 2011-06-15 | Glaxosmithkline Llc | Novel compounds |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| CA2840380A1 (en) | 2011-06-24 | 2012-12-27 | Dana-Farber Cancer Institute, Inc. | Selective inhibitors of histone deacetylase isoform 6 and methods thereof |
| JP2013010719A (ja) | 2011-06-30 | 2013-01-17 | Dainippon Sumitomo Pharma Co Ltd | ベンズイミダゾロンおよびオキシインドール誘導体ならびにそれらの医薬用途 |
| JP2014524409A (ja) | 2011-07-29 | 2014-09-22 | ザ・チルドレンズ・ホスピタル・オブ・フィラデルフィア | Ｈｉｖの治療のための組成物および方法 |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033270A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same |
| WO2013033269A1 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same |
| PH12014500130B1 (en) | 2011-08-31 | 2018-07-04 | Otsuka Pharma Co Ltd | Quinolone compound |
| DE102011082013A1 (de) | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| EP2757887B1 (en) | 2011-09-22 | 2017-04-26 | VIIV Healthcare UK Limited | Pyrrolopyridinone compounds and methods for treating hiv |
| WO2013044511A1 (zh) | 2011-09-30 | 2013-04-04 | 沈阳蓝桑医药生物技术研发有限公司 | 含有瑞利格内酯的药物组合物及其应用 |
| WO2013064900A1 (en) | 2011-11-01 | 2013-05-10 | Resverlogix Corp. | Oral immediate release formulations for substituted quinazolinones |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| WO2013148197A1 (en) | 2012-03-28 | 2013-10-03 | The J. David Gladstone Institutes | Compositions and methods for reactivating latent immunodeficiency virus |
| US20130281398A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| US20130281396A1 (en) * | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| US20130281397A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| CN104334526A (zh) | 2012-04-20 | 2015-02-04 | 艾伯维公司 | 异吲哚酮衍生物 |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| EP2864336B1 (en) | 2012-06-06 | 2016-11-23 | Constellation Pharmaceuticals, Inc. | Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof |
| RU2632915C2 (ru) | 2012-06-12 | 2017-10-11 | Эббви Инк. | Производные пиридинона и пиридазинона |
| IN2014DN11269A (enExample) | 2012-06-25 | 2015-10-09 | Oncoethix Sa | |
| WO2014015175A1 (en) | 2012-07-18 | 2014-01-23 | Massachusetts Institute Of Technology | Compositions and methods for modulating brd4 bioactivity |
| KR20150041787A (ko) | 2012-08-16 | 2015-04-17 | 바이엘 파마 악티엔게젤샤프트 | 2,3-벤조디아제핀 |
| ES2653990T3 (es) | 2012-08-16 | 2018-02-09 | Glaxosmithkline Llc | Benzodiazepinas para tratamiento del cáncer de pulmón de células pequeñas |
| JP6276277B2 (ja) | 2012-09-28 | 2018-02-07 | バイエル ファーマ アクチエンゲゼルシャフト | Ｂｅｔタンパク質阻害性の５−アリールトリアゾロアゼピン |
| EP2900221B1 (en) | 2012-09-28 | 2019-03-06 | Oncoethix GmbH | Pharmaceutical formulation containing thienotriazolodiazepine compounds |
| US9422290B2 (en) | 2012-11-13 | 2016-08-23 | Boehringer Ingelheim International Gmbh | Triazolopyridazine |
| ES2625945T3 (es) | 2012-11-14 | 2017-07-21 | Glaxosmithkline Llc | Tieno[3,2-c]piridin-4(5H)-onas como inhibidores de bet |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| CN105229002A (zh) | 2012-12-20 | 2016-01-06 | 拜耳医药股份有限公司 | 抑制bet蛋白的二氢吡啶并吡嗪酮 |
| CA2895426A1 (en) | 2012-12-20 | 2014-06-26 | Bayer Pharma Aktiengesellschaft | Bet-protein-inhibiting dihydroquinoxalinones |
| JP2016507496A (ja) | 2012-12-21 | 2016-03-10 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規複素環式化合物 |
| WO2014128655A1 (en) | 2013-02-25 | 2014-08-28 | Aurigene Discovery Technologies Limited | Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors |
| US9492460B2 (en) | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| WO2014134267A1 (en) | 2013-02-27 | 2014-09-04 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| WO2014164771A1 (en) | 2013-03-11 | 2014-10-09 | Abbvie Inc. | Bromodomain inhibitors |
| BR112015022674A2 (pt) | 2013-03-11 | 2017-07-18 | Abbvie Inc | inibidores de bromodomínio |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| US10035800B2 (en) | 2013-03-12 | 2018-07-31 | Abbvie Inc. | Substituted 1,4,10-triazadibenzo[cd,f]azulenes, substituted 1,4,5,10-tetraazadibenzo[cd,f]azulenes and substituted 1,4,5,7,10-pentaazadibenzo[cd,f]azulenes as bromodomain inhibitors |
| CA2905426A1 (en) | 2013-03-12 | 2014-10-09 | Abbvie Inc. | Pyrrole amide inhibitors |
| EP2970276A1 (en) | 2013-03-12 | 2016-01-20 | AbbVie Inc. | Dihydro-pyrrolopyridinone bromodomain inhibitors |
| ES2704048T3 (es) | 2013-03-14 | 2019-03-14 | Glaxosmithkline Ip No 2 Ltd | Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio |
| WO2014159392A1 (en) | 2013-03-14 | 2014-10-02 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| AU2014230816B9 (en) | 2013-03-14 | 2016-12-15 | Glaxosmithkline Intellectual Property (No.2) Limited | Furopyridines as bromodomain inhibitors |
| BR112015022417A2 (pt) | 2013-03-14 | 2017-07-18 | Convergene Llc | métodos e composições para inibição de proteínas contendo bromodomínio |
| BR112015021983B1 (pt) | 2013-03-15 | 2022-03-03 | Plexxikon, Inc | Compostos heterocíclicos, composições farmacêuticas que os compreendem e usos dos mesmos |
| CA2903881C (en) | 2013-03-15 | 2021-05-18 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| EP2968311A4 (en) | 2013-03-15 | 2016-07-20 | Epigenetix Inc | OXAZOLO [5,4-C] CHINOLIN-2-ON COMPOUNDS AS BROMODOMENA INHIBITORS |
| WO2014154762A1 (en) | 2013-03-27 | 2014-10-02 | Boehringer Ingelheim International Gmbh | Dihydroquinazolinone analogues as brd4 inhibitors |
| JP6370368B2 (ja) | 2013-03-27 | 2018-08-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｂｒｄ４阻害剤としてのインドリノン類似体 |
| TWI530499B (zh) | 2013-03-28 | 2016-04-21 | 吉李德科學股份有限公司 | 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類 |
| EP2996689A1 (en) | 2013-04-17 | 2016-03-23 | Albert-Ludwigs-Universität Freiburg | Compounds for use as bromodomain inhibitors |
| EA027139B1 (ru) | 2013-04-26 | 2017-06-30 | Бейджин, Лтд. | Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны |
| TWI527811B (zh) * | 2013-05-09 | 2016-04-01 | 吉李德科學股份有限公司 | 作爲溴結構域抑制劑的苯並咪唑衍生物 |
| WO2014191894A1 (en) | 2013-05-27 | 2014-12-04 | Novartis Ag | Imidazopyrrolidinone derivatives and their use in the treatment of disease |
| US8975417B2 (en) | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| PT3004112T (pt) | 2013-05-28 | 2017-12-11 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona e sua utilização no tratamento de doença |
| MX2015016421A (es) | 2013-05-28 | 2016-03-03 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades. |
| ITMI20130991A1 (it) | 2013-06-17 | 2014-12-18 | Industrie De Nora Spa | Sistema per la misurazione di correnti presenti sugli elettrodi in celle elettrolitiche interconnesse. |
| EP3010909A1 (de) | 2013-06-17 | 2016-04-27 | Bayer Pharma Aktiengesellschaft | Substituierte phenyl-2,3-benzodiazepine |
| CA2915622C (en) * | 2013-06-21 | 2020-08-18 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| MX365864B (es) | 2013-06-21 | 2019-06-18 | Zenith Epigenetics Ltd | Inhibidores de bromodominio biciclicos novedosos. |
| EP3013828A4 (en) | 2013-06-28 | 2016-11-23 | Abbvie Inc | BROMDOMÄNENINHIBITOREN |
| AR096758A1 (es) | 2013-06-28 | 2016-02-03 | Abbvie Inc | Inhibidores cristalinos de bromodominios |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| CN105555779B (zh) | 2013-07-16 | 2019-05-10 | 巴斯夫欧洲公司 | 除草的嗪类 |
| KR20160034379A (ko) | 2013-07-25 | 2016-03-29 | 다나-파버 캔서 인스티튜트 인크. | 전사 인자의 억제제 및 그의 용도 |
| KR101672096B1 (ko) | 2013-09-30 | 2016-11-02 | 주식회사 엘지화학 | 헤테로환 화합물 및 이를 포함하는 유기 발광 소자 |
| HRP20221389T1 (hr) | 2013-10-18 | 2023-01-06 | Celgene Quanticel Research, Inc. | Inhibitori bromodomena |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US20150148372A1 (en) | 2013-11-26 | 2015-05-28 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| AU2014363989A1 (en) | 2013-12-09 | 2016-06-16 | Abbvie Inc. | Dihydropyridinone and dihydropyridazinone derivatives useful as bromodomain inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| EP3083559B1 (en) | 2013-12-20 | 2021-03-10 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| UA117165C2 (uk) | 2014-01-09 | 2018-06-25 | Оріон Корпорейшн | Біциклічні гетероциклічні похідні як інгібітори бромодомену |
| AU2015222887B2 (en) | 2014-02-28 | 2019-06-27 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-b]indoles and related analogs as BET bromodomain inhibitors |
| WO2015164480A1 (en) | 2014-04-23 | 2015-10-29 | Incyte Corporation | 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS |
| CR20160545A (es) | 2014-04-23 | 2017-03-31 | Basf Se | Compuestos de diaminotriazina como herbicidas |
| ES2811088T3 (es) | 2014-04-23 | 2021-03-10 | Takeda Pharmaceuticals Co | Derivados de isoindolin-1-ona como actividad del modulador alostérico positivo del receptor M1 muscarínico colinérgico para el tratamiento de la enfermedad de Alzheimer |
| US20170095484A1 (en) | 2014-05-02 | 2017-04-06 | Oncoethix Gmbh | Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+non-small cell lung cancer using thienotriazolodiazepine compounds |
| KR20160145833A (ko) | 2014-05-02 | 2016-12-20 | 온코에틱스 게엠베하 | 티에노트리아졸로디아제핀 화합물을 사용한 급성 골수성 백혈병 및/또는 급성 림프아구성 백혈병의 치료 방법 |
| CN106852120A (zh) | 2014-05-08 | 2017-06-13 | 翁科埃斯克斯有限公司 | 利用噻吩并三唑并二氮杂*化合物治疗三阴性乳腺癌的方法 |
| WO2015169953A1 (en) | 2014-05-08 | 2015-11-12 | Oncoethix Gmbh | Method of treating glioma using thienotriazolodiazepine compounds |
| US10065951B2 (en) | 2014-05-30 | 2018-09-04 | Icahn School Of Medicine At Mount Sinai | Small molecule transcription modulators of bromodomains |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| CN105029258A (zh) | 2014-09-20 | 2015-11-11 | 林静 | 一种多味橄榄的制作方法 |
| MA40943A (fr) | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| WO2016123709A1 (en) | 2015-02-03 | 2016-08-11 | Trillium Therapeutics Inc. | Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins |
| WO2016186453A1 (en) | 2015-05-20 | 2016-11-24 | Kainos Medicine, Inc. | Quinoline derivatives as bromodomain inhibitors |
| KR20180011267A (ko) | 2015-05-29 | 2018-01-31 | 시오노기 앤드 컴파니, 리미티드 | Hiv 복제 저해 작용을 갖는 함질소 3환성 유도체 |
| TW201722966A (zh) | 2015-10-29 | 2017-07-01 | 英塞特公司 | Bet蛋白質抑制劑之非晶固體形式 |
| CN105254635A (zh) | 2015-10-30 | 2016-01-20 | 中国药科大学 | 一类咪唑并吡嗪类化合物及其药物组合物和用途 |
| US20170127985A1 (en) | 2015-11-11 | 2017-05-11 | Medtronic Minimed, Inc. | Sensor set |
| CN108602821B (zh) | 2015-12-14 | 2021-06-29 | 恒元生物医药科技(苏州)有限公司 | 1h-咪唑并[4,5-b]吡啶基bet溴结构域抑制剂 |
| WO2017127930A1 (en) | 2016-01-28 | 2017-08-03 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals |
| US20190040063A1 (en) | 2016-02-05 | 2019-02-07 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Tricyclic compound for bromodomain-containing protein inhibitor and preparation pharmaceutical composition, and application thereof |
| SMT202300155T1 (it) | 2016-06-20 | 2023-07-20 | Incyte Corp | Forme solide cristalline di un inibitore di bet |
| CN108069958A (zh) | 2016-11-10 | 2018-05-25 | 凯惠科技发展(上海)有限公司 | 一种含氮杂环类化合物、其制备方法、药物组合物及应用 |
-
2015
- 2015-09-14 US US14/852,958 patent/US9527864B2/en active Active
- 2015-09-14 ES ES15771373T patent/ES2855225T3/es active Active
- 2015-09-14 TW TW104130337A patent/TWI712603B/zh active
- 2015-09-14 WO PCT/US2015/049909 patent/WO2016044130A1/en not_active Ceased
- 2015-09-14 EP EP15771373.6A patent/EP3194406B8/en active Active
- 2015-09-14 JP JP2017514515A patent/JP6599979B2/ja active Active
-
2016
- 2016-11-18 US US15/356,002 patent/US9834565B2/en not_active Expired - Fee Related
-
2017
- 2017-11-02 US US15/802,142 patent/US10227359B2/en active Active
-
2019
- 2019-02-01 US US16/265,450 patent/US10618910B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017526731A5 (enExample) | ||
| US10301278B2 (en) | 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions therefor for inhibiting the activity of SHP2 | |
| US10934285B2 (en) | Compounds and compositions for inhibiting the activity of SHP2 | |
| KR102534028B1 (ko) | 트리아졸로피리미딘 화합물 및 그의 용도 | |
| JP2019524660A5 (enExample) | ||
| JP2013056930A5 (enExample) | ||
| CN101678014B (zh) | 杂环激酶调节剂 | |
| CN110573500A (zh) | N-(氮杂芳基)环内酰胺-1-甲酰胺衍生物及其制备方法和应用 | |
| JP2020128396A (ja) | Ｆｇｆｒ抑制剤としての二環式複素環 | |
| JP2013544847A5 (enExample) | ||
| JP2020504716A5 (enExample) | ||
| JP2017510642A5 (enExample) | ||
| CN111836805A (zh) | 吡啶衍生物及其用于治疗hiv感染的用途 | |
| HRP20150858T1 (hr) | Inhibitori bromodomena i njihove uporabe | |
| JP2017513879A5 (enExample) | ||
| JP2009513703A5 (enExample) | ||
| HRP20230466T1 (hr) | Kristalni čvrsti oblici bet inhibitora | |
| JP2016523973A5 (enExample) | ||
| JP2016518372A5 (enExample) | ||
| HRP20171248T1 (hr) | Amino-supstituirani imidazopiridazini | |
| WO2016203404A1 (en) | Compounds and compositions for inhibiting the activity of shp2 | |
| JP2014518544A5 (enExample) | ||
| JP2015537017A5 (enExample) | ||
| JP2016519147A5 (enExample) | ||
| RU2016101548A (ru) | Соединения амидов гетероарилпиридона и азапиридона |