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 |
|---|---|---|---|---|
| TWI719464B (zh) | 2013-03-15 | 2021-02-21 | 美商英塞特控股公司 | 作為bet蛋白抑制劑之三環雜環 |
| JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｂｅｔタンパク質阻害剤としての三環式複素環 |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| KR20240134245A (ko) | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| EP4234554A3 (en) | 2016-06-20 | 2023-12-27 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| EP3813827A4 (en) * | 2018-06-28 | 2022-04-13 | Jiangsu Hengrui Medicine Co., Ltd. | CONDENSED TRICYCLIC HETEROCYCLIC COMPOUNDS AND THERAPEUTIC USES THEREOF |
| WO2020038387A1 (zh) * | 2018-08-24 | 2020-02-27 | 杭州阿诺生物医药科技有限公司 | 高活性sting蛋白激动剂 |
| 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 |
| DE60115872T2 (de) | 2000-04-21 | 2006-07-13 | Pharmacia & Upjohn Co. Llc, Kalamazoo | Cabergolin zur behandlung von fibromyalgie und chronic-fatigue-syndrom |
| EP1294358B1 (en) | 2000-06-28 | 2004-08-18 | Smithkline Beecham Plc | Wet milling process |
| US6919334B2 (en) * | 2002-09-12 | 2005-07-19 | Wyeth | Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine |
| MXPA05005425A (es) | 2002-11-22 | 2005-11-23 | Japan Tobacco Inc | Heterociclos que contienen nitrogeno, biciclicos, fusionados. |
| EP1462103A1 (en) | 2003-03-25 | 2004-09-29 | Faust Pharmaceuticals | NO donors, combination products and uses as modulators of neurotransmitter release |
| WO2005080334A1 (ja) | 2004-02-23 | 2005-09-01 | Dainippon Sumitomo Pharma Co., Ltd. | 新規へテロ環化合物 |
| JP4790703B2 (ja) | 2004-04-07 | 2011-10-12 | 武田薬品工業株式会社 | 環式化合物 |
| 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 |
| US20080318999A1 (en) | 2005-08-05 | 2008-12-25 | Methvin Isaac | Tricyclic Benzimidazoles and Their Use as Metabotropic Glutamate Receptor Modulators |
| EP2147310A4 (en) | 2007-04-27 | 2010-09-08 | Univ Rochester | COMPOSITIONS AND METHODS OF 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 |
| CN101910182B (zh) | 2007-12-28 | 2013-07-17 | 田边三菱制药株式会社 | 抗癌剂 |
| 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 |
| EP3050885B1 (en) | 2009-11-05 | 2017-10-18 | GlaxoSmithKline LLC | Benzodiazepine bromodomain inhibitor |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| WO2011054851A1 (en) | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Novel process |
| ES2652304T3 (es) | 2009-11-05 | 2018-02-01 | Glaxosmithkline Llc | Compuesto de benzodiacepina novedoso |
| WO2011133722A2 (en) | 2010-04-23 | 2011-10-27 | Kineta, Inc. | Anti-viral compounds |
| HUE031073T2 (en) | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| WO2011143657A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Male contraceptive compositions and methods of use |
| CA2799403C (en) | 2010-05-14 | 2020-01-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| CN103119160B (zh) | 2010-05-14 | 2016-06-01 | 达那-法伯癌症研究所 | 用于调节代谢的组合物和方法 |
| WO2011161031A1 (en) | 2010-06-22 | 2011-12-29 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| US8653089B2 (en) | 2011-02-09 | 2014-02-18 | F. Hoffmann-La Roche Ag | Heterocyclic compounds and methods of use |
| AU2012220620A1 (en) | 2011-02-23 | 2013-10-03 | Icahn School Of Medicine At Mount Sinai | Inhibitors of bromodomains as modulators of gene expression |
| GB201106799D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201106743D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201106750D0 (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 |
| EP2721031B1 (en) | 2011-06-17 | 2016-01-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2723338A2 (en) | 2011-06-24 | 2014-04-30 | The Trustees of Stevens Institute of Technology | 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 |
| WO2013033269A1 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same |
| WO2013033270A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same |
| AU2012303954B2 (en) | 2011-08-31 | 2017-06-22 | Otsuka Pharmaceutical 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 |
| ES2632443T3 (es) | 2011-09-22 | 2017-09-13 | Viiv Healthcare Uk Limited | Compuestos de pirrolopiridinona y procedimientos de tratamiento del VIH |
| 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 |
| JP5992049B2 (ja) | 2011-11-01 | 2016-09-14 | レスバーロジックス コーポレイション | 置換されたキナゾリノンのための経口速放性製剤 |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| US20150133434A1 (en) | 2012-03-28 | 2015-05-14 | The J. David Gladstone Institutes | Compositions and Methods for Reactivating Latent Immunodeficiency Virus |
| US20130281397A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| 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 |
| HK1206744A1 (en) | 2012-04-20 | 2016-01-15 | Abbvie Inc. | Isoindolone derivatives |
| EP2864336B1 (en) | 2012-06-06 | 2016-11-23 | Constellation Pharmaceuticals, Inc. | Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| MX2014015156A (es) | 2012-06-12 | 2015-08-06 | Abbvie Inc | Derivados de piridinona y piridazinona. |
| EP2863923B1 (en) | 2012-06-25 | 2019-05-08 | Oncoethix GmbH | Thienotriazolodiazepine compounds for the treatment of lymphomas |
| US9610332B2 (en) | 2012-07-18 | 2017-04-04 | Massachusetts Institute Of Technology | Compositions and methods for modulating BRD4 bioactivity |
| PE20150729A1 (es) | 2012-08-16 | 2015-06-14 | Bayer Pharma AG | 2,3-benzodiazepines |
| ES2653990T3 (es) | 2012-08-16 | 2018-02-09 | Glaxosmithkline Llc | Benzodiazepinas para tratamiento del cáncer de pulmón de células pequeñas |
| MX2015003771A (es) | 2012-09-28 | 2016-03-04 | Oncoethix Gmbh | Formulacion farmaceutica que contiene compuestos de tienotriazolodiazepina. |
| WO2014048945A1 (de) | 2012-09-28 | 2014-04-03 | Bayer Pharma Aktiengesellschaft | Bet-proteininhibitorische 5-aryl-triazolo-azepine |
| US9422290B2 (en) | 2012-11-13 | 2016-08-23 | Boehringer Ingelheim International Gmbh | Triazolopyridazine |
| EP2920183B1 (en) | 2012-11-14 | 2017-03-08 | Glaxosmithkline LLC | Thieno[3,2-c]pyridin-4(5h)-ones as bet inhibitors |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| WO2014095775A1 (de) | 2012-12-20 | 2014-06-26 | Bayer Pharma Aktiengesellschaft | Bet-proteininhibitorische dihydrochinoxalinone |
| JP2016504990A (ja) | 2012-12-20 | 2016-02-18 | バイエル ファーマ アクチエンゲゼルシャフト | Ｂｅｔタンパク質抑制性ジヒドロピリドピラジノン |
| AU2013365926B9 (en) | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| 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 |
| CN105189488B (zh) | 2013-02-27 | 2018-07-24 | 百时美施贵宝公司 | 用作溴区结构域抑制剂的咔唑化合物 |
| CA2904048A1 (en) | 2013-03-11 | 2014-10-09 | Abbvie Inc. | Bromodomain inhibitors |
| CN105377851B (zh) | 2013-03-11 | 2018-07-20 | 密执安州立大学董事会 | Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法 |
| BR112015022674A2 (pt) | 2013-03-11 | 2017-07-18 | Abbvie Inc | inibidores de bromodomínio |
| JP6419735B2 (ja) | 2013-03-12 | 2018-11-07 | アッヴィ・インコーポレイテッド | 四環系ブロモドメイン阻害剤 |
| US9493411B2 (en) | 2013-03-12 | 2016-11-15 | Abbvie Inc. | Pyrrole-3-carboxamide bromodomain inhibitors |
| KR20150126696A (ko) | 2013-03-12 | 2015-11-12 | 애브비 인코포레이티드 | 디하이드로-피롤로피리디논 브로모도메인 억제제 |
| 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 |
| WO2014140077A1 (en) | 2013-03-14 | 2014-09-18 | Glaxosmithkline Intellectual Property (No.2) Limited | Furopyridines as bromodomain inhibitors |
| WO2014159392A1 (en) | 2013-03-14 | 2014-10-02 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| BR112015022417A2 (pt) | 2013-03-14 | 2017-07-18 | Convergene Llc | métodos e composições para inibição de proteínas contendo bromodomínio |
| RU2680100C9 (ru) | 2013-03-15 | 2019-04-18 | Плексксикон Инк. | Гетероциклические соединения и их применения |
| TWI719464B (zh) * | 2013-03-15 | 2021-02-21 | 美商英塞特控股公司 | 作為bet蛋白抑制劑之三環雜環 |
| US20160039842A1 (en) | 2013-03-15 | 2016-02-11 | Epigenetix, Inc. | Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors |
| US9199988B2 (en) | 2013-03-27 | 2015-12-01 | Boehringer Ingelheim International Gmbh | Dihydroquinazolinone analogues |
| 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 |
| US10435364B2 (en) | 2013-04-17 | 2019-10-08 | Albert Ludwigs Universität Freiburg | Compounds for use as bromodomain inhibitors |
| WO2014173241A1 (en) | 2013-04-26 | 2014-10-30 | Beigene, Ltd. | Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones |
| 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 |
| US8975417B2 (en) | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| MX2015016344A (es) | 2013-05-27 | 2016-03-01 | Novartis Ag | Derivados de imidazo-pirrolidinona y su uso en el tratamiento de enfermedades. |
| KR20160012195A (ko) | 2013-05-28 | 2016-02-02 | 노파르티스 아게 | Bet 억제제로서의 피라졸로-피롤리딘-4-온 유도체 및 질환의 치료에서의 그의 용도 |
| BR112015029353A2 (pt) | 2013-05-28 | 2017-07-25 | Novartis Ag | derivados de pirazolo-pirrolidin-4-ona e seu uso no tratamento de doenças |
| 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. |
| CA2915419A1 (en) | 2013-06-17 | 2014-12-24 | Bayer Pharma Aktiengesellschaft | Substituted phenyl-2,3-benzodiazepines |
| ES2661437T3 (es) * | 2013-06-21 | 2018-04-02 | Zenith Epigenetics Corp. | Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| AR096758A1 (es) | 2013-06-28 | 2016-02-03 | Abbvie Inc | Inhibidores cristalinos de bromodominios |
| SG11201510678TA (en) | 2013-06-28 | 2016-01-28 | Abbvie Inc | Bromodomain inhibitors |
| JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｂｅｔタンパク質阻害剤としての三環式複素環 |
| PL3022191T3 (pl) | 2013-07-16 | 2017-08-31 | Basf Se | Chwastobójcze azyny |
| 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 |
| PE20161065A1 (es) | 2013-10-18 | 2016-11-19 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| US20150148372A1 (en) | 2013-11-26 | 2015-05-28 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| JP2016539970A (ja) | 2013-12-09 | 2016-12-22 | アッヴィ・インコーポレイテッド | ブロモドメイン阻害薬として有用なジヒドロピリジノンおよびジヒドロピリダジノン誘導体 |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| WO2015095445A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| BR112016015311B1 (pt) | 2014-01-09 | 2023-01-24 | Orion Corporation | Compostos derivados heterocíclicos bicíclicos, composição farmacêutica que compreende os mesmos e uso dos ditos compostos para tratar uma doença associada com bromodomínio |
| WO2015131005A1 (en) | 2014-02-28 | 2015-09-03 | The Regents Of The University Of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
| AU2015250900B9 (en) | 2014-04-23 | 2019-03-21 | Basf Se | Diaminotriazine compounds as herbicides |
| KR20240134245A (ko) | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| PL3134386T3 (pl) | 2014-04-23 | 2020-11-16 | Takeda Pharmaceutical Company Limited | Pochodne izoindolin-1-onu jako dodatnia aktywność allosterycznego modulatora cholinergicznego receptora muskarynowego m1 do leczenia choroby alzheimera |
| WO2015168555A1 (en) | 2014-05-02 | 2015-11-05 | Oncoethix Sa | 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 |
| WO2015169953A1 (en) | 2014-05-08 | 2015-11-12 | Oncoethix Gmbh | Method of treating glioma using thienotriazolodiazepine compounds |
| BR112016026046A8 (pt) | 2014-05-08 | 2021-07-20 | Oncoethix Gmbh | uso de compostos de tienotriazolodiazepina |
| EP3148543B1 (en) | 2014-05-30 | 2020-04-08 | 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 |
| CA2974153A1 (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 |
| CA2987384A1 (en) | 2015-05-29 | 2016-12-08 | Shionogi & Co., Ltd. | Nitrogen-containing tricyclic derivative having hiv replication inhibitory activity |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| 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 |
| CA3007168A1 (en) | 2015-12-14 | 2017-06-22 | Zenith Epigenetics Ltd. | 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors |
| 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 |
| EP3412669A4 (en) | 2016-02-05 | 2019-09-04 | Chia Tai Tianqing Pharmaceutical Group Co.,Ltd | TRICYCLIC COMPOUND FOR PROTEIN INHIBITOR CONTAINING BROMODOMAINE AND PREPARATION, PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| EP4234554A3 (en) | 2016-06-20 | 2023-12-27 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| 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 JP JP2017514515A patent/JP6599979B2/ja active Active
- 2015-09-14 ES ES15771373T patent/ES2855225T3/es active 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 TW TW104130337A patent/TWI712603B/zh active
-
2016
- 2016-11-18 US US15/356,002 patent/US9834565B2/en active Active
-
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) | ||
| US10934285B2 (en) | Compounds and compositions for inhibiting the activity of SHP2 | |
| KR102534028B1 (ko) | 트리아졸로피리미딘 화합물 및 그의 용도 | |
| US9815813B2 (en) | 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions therefor for inhibiting the activity of SHP2 | |
| ES2853375T3 (es) | Sales novedosas y composiciones farmacéuticas de las mismas para el tratamiento de trastornos inflamatorios | |
| JP2013056930A5 (enExample) | ||
| JP2019524660A5 (enExample) | ||
| 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 | |
| JP2013544847A5 (enExample) | ||
| JP2017510642A5 (enExample) | ||
| CN111836805A (zh) | 吡啶衍生物及其用于治疗hiv感染的用途 | |
| JP2020504716A5 (enExample) | ||
| HRP20150858T1 (hr) | Inhibitori bromodomena i njihove uporabe | |
| JP2017513879A5 (enExample) | ||
| JP2009513703A5 (enExample) | ||
| CN107278201A (zh) | 用于治疗hiv的喹唑啉衍生物 | |
| JP2016523973A5 (enExample) | ||
| JP2016518372A5 (enExample) | ||
| HRP20171248T1 (hr) | Amino-supstituirani imidazopiridazini | |
| EP3310779A1 (en) | Compounds and compositions for inhibiting the activity of shp2 | |
| JP2014518544A5 (enExample) | ||
| JP2015537017A5 (enExample) | ||
| JP2016519147A5 (enExample) | ||
| RU2016101548A (ru) | Соединения амидов гетероарилпиридона и азапиридона | |
| CN107207498A (zh) | 用于治疗hiv的稠合嘧啶化合物 |