JP2020504716A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020504716A5 JP2020504716A5 JP2019531160A JP2019531160A JP2020504716A5 JP 2020504716 A5 JP2020504716 A5 JP 2020504716A5 JP 2019531160 A JP2019531160 A JP 2019531160A JP 2019531160 A JP2019531160 A JP 2019531160A JP 2020504716 A5 JP2020504716 A5 JP 2020504716A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- tumor
- alkyl
- 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 description 112
- 206010028980 Neoplasm Diseases 0.000 claims description 101
- 150000001875 compounds Chemical class 0.000 claims description 96
- -1 cyano, carboxy Chemical group 0.000 claims description 73
- 125000000217 alkyl group Chemical group 0.000 claims description 70
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 47
- 125000003545 alkoxy group Chemical group 0.000 claims description 46
- 201000011510 cancer Diseases 0.000 claims description 44
- 125000005843 halogen group Chemical group 0.000 claims description 44
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 43
- 201000010536 head and neck cancer Diseases 0.000 claims description 42
- 125000001188 haloalkyl group Chemical group 0.000 claims description 40
- 125000000623 heterocyclic group Chemical group 0.000 claims description 36
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 33
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 32
- 210000004027 cell Anatomy 0.000 claims description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims description 24
- 239000001257 hydrogen Substances 0.000 claims description 24
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 21
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 20
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 18
- 206010039491 Sarcoma Diseases 0.000 claims description 18
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 18
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 18
- 206010025323 Lymphomas Diseases 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 16
- 125000001072 heteroaryl group Chemical group 0.000 claims description 16
- 210000002308 embryonic cell Anatomy 0.000 claims description 15
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 14
- 208000003445 Mouth Neoplasms Diseases 0.000 claims description 12
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 11
- 208000011580 syndromic disease Diseases 0.000 claims description 11
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 10
- 125000004432 carbon atom Chemical group C* 0.000 claims description 10
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims description 10
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims description 9
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 9
- 208000027866 inflammatory disease Diseases 0.000 claims description 9
- 208000016800 primary central nervous system lymphoma Diseases 0.000 claims description 9
- 125000001424 substituent group Chemical group 0.000 claims description 9
- 208000023275 Autoimmune disease Diseases 0.000 claims description 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 8
- 206010007953 Central nervous system lymphoma Diseases 0.000 claims description 8
- 208000011231 Crohn disease Diseases 0.000 claims description 8
- 230000001363 autoimmune Effects 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 208000018084 Bone neoplasm Diseases 0.000 claims description 7
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims description 7
- 125000002947 alkylene group Chemical group 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 7
- 210000003491 skin Anatomy 0.000 claims description 7
- 210000000115 thoracic cavity Anatomy 0.000 claims description 7
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 6
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 6
- 206010005949 Bone cancer Diseases 0.000 claims description 6
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 6
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 6
- 206010021042 Hypopharyngeal cancer Diseases 0.000 claims description 6
- 206010056305 Hypopharyngeal neoplasm Diseases 0.000 claims description 6
- 206010062038 Lip neoplasm Diseases 0.000 claims description 6
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 6
- 206010029260 Neuroblastoma Diseases 0.000 claims description 6
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 6
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
- 230000002496 gastric effect Effects 0.000 claims description 6
- 208000006454 hepatitis Diseases 0.000 claims description 6
- 201000006866 hypopharynx cancer Diseases 0.000 claims description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 6
- 230000001394 metastastic effect Effects 0.000 claims description 6
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 6
- 201000008968 osteosarcoma Diseases 0.000 claims description 6
- 201000000849 skin cancer Diseases 0.000 claims description 6
- 206010055031 vascular neoplasm Diseases 0.000 claims description 6
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 5
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 5
- 206010009944 Colon cancer Diseases 0.000 claims description 5
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims description 5
- 206010061252 Intraocular melanoma Diseases 0.000 claims description 5
- 208000010505 Nose Neoplasms Diseases 0.000 claims description 5
- 206010033128 Ovarian cancer Diseases 0.000 claims description 5
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 5
- 201000005969 Uveal melanoma Diseases 0.000 claims description 5
- 230000002159 abnormal effect Effects 0.000 claims description 5
- 201000010881 cervical cancer Diseases 0.000 claims description 5
- 201000001981 dermatomyositis Diseases 0.000 claims description 5
- 201000011523 endocrine gland cancer Diseases 0.000 claims description 5
- 201000006721 lip cancer Diseases 0.000 claims description 5
- 208000026037 malignant tumor of neck Diseases 0.000 claims description 5
- 208000037830 nasal cancer Diseases 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 201000002575 ocular melanoma Diseases 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 230000002062 proliferating effect Effects 0.000 claims description 5
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 5
- 125000006432 1-methyl cyclopropyl group Chemical group [H]C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims description 4
- 125000002252 acyl group Chemical group 0.000 claims description 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 4
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 230000003211 malignant effect Effects 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 201000005962 mycosis fungoides Diseases 0.000 claims description 4
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 4
- 208000037968 sinus cancer Diseases 0.000 claims description 4
- 208000002008 AIDS-Related Lymphoma Diseases 0.000 claims description 3
- 208000006468 Adrenal Cortex Neoplasms Diseases 0.000 claims description 3
- 206010061424 Anal cancer Diseases 0.000 claims description 3
- 208000007860 Anus Neoplasms Diseases 0.000 claims description 3
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 3
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 claims description 3
- 206010008909 Chronic Hepatitis Diseases 0.000 claims description 3
- 208000015943 Coeliac disease Diseases 0.000 claims description 3
- 206010056979 Colitis microscopic Diseases 0.000 claims description 3
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 3
- 208000006926 Discoid Lupus Erythematosus Diseases 0.000 claims description 3
- 206010014733 Endometrial cancer Diseases 0.000 claims description 3
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 3
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 3
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims description 3
- 208000017604 Hodgkin disease Diseases 0.000 claims description 3
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims description 3
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 3
- 208000037396 Intraductal Noninfiltrating Carcinoma Diseases 0.000 claims description 3
- 208000009164 Islet Cell Adenoma Diseases 0.000 claims description 3
- 201000005099 Langerhans cell histiocytosis Diseases 0.000 claims description 3
- 206010023825 Laryngeal cancer Diseases 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010025312 Lymphoma AIDS related Diseases 0.000 claims description 3
- 208000004059 Male Breast Neoplasms Diseases 0.000 claims description 3
- 208000034578 Multiple myelomas Diseases 0.000 claims description 3
- 206010028372 Muscular weakness Diseases 0.000 claims description 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 3
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 208000000821 Parathyroid Neoplasms Diseases 0.000 claims description 3
- 208000002471 Penile Neoplasms Diseases 0.000 claims description 3
- 206010034299 Penile cancer Diseases 0.000 claims description 3
- 208000009565 Pharyngeal Neoplasms Diseases 0.000 claims description 3
- 206010034811 Pharyngeal cancer Diseases 0.000 claims description 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 201000008183 Pulmonary blastoma Diseases 0.000 claims description 3
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 3
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims description 3
- 206010061934 Salivary gland cancer Diseases 0.000 claims description 3
- 208000018020 Sickle cell-beta-thalassemia disease syndrome Diseases 0.000 claims description 3
- 201000009594 Systemic Scleroderma Diseases 0.000 claims description 3
- 206010042953 Systemic sclerosis Diseases 0.000 claims description 3
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 3
- 206010057644 Testis cancer Diseases 0.000 claims description 3
- 206010043391 Thalassaemia beta Diseases 0.000 claims description 3
- 206010043515 Throat cancer Diseases 0.000 claims description 3
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 3
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 3
- 208000006593 Urologic Neoplasms Diseases 0.000 claims description 3
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 3
- 208000008383 Wilms tumor Diseases 0.000 claims description 3
- 201000002454 adrenal cortex cancer Diseases 0.000 claims description 3
- 201000011165 anus cancer Diseases 0.000 claims description 3
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 3
- 210000003169 central nervous system Anatomy 0.000 claims description 3
- 230000001684 chronic effect Effects 0.000 claims description 3
- 208000004921 cutaneous lupus erythematosus Diseases 0.000 claims description 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 229910052805 deuterium Inorganic materials 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 3
- 208000028715 ductal breast carcinoma in situ Diseases 0.000 claims description 3
- 201000004101 esophageal cancer Diseases 0.000 claims description 3
- 208000024519 eye neoplasm Diseases 0.000 claims description 3
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 3
- 210000004392 genitalia Anatomy 0.000 claims description 3
- 208000024348 heart neoplasm Diseases 0.000 claims description 3
- 231100000283 hepatitis Toxicity 0.000 claims description 3
- 125000005842 heteroatom Chemical group 0.000 claims description 3
- 201000002313 intestinal cancer Diseases 0.000 claims description 3
- 210000003734 kidney Anatomy 0.000 claims description 3
- 210000001821 langerhans cell Anatomy 0.000 claims description 3
- 206010023841 laryngeal neoplasm Diseases 0.000 claims description 3
- 210000004185 liver Anatomy 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 206010025135 lupus erythematosus Diseases 0.000 claims description 3
- 208000004341 lymphocytic colitis Diseases 0.000 claims description 3
- 201000003175 male breast cancer Diseases 0.000 claims description 3
- 208000010907 male breast carcinoma Diseases 0.000 claims description 3
- 230000036244 malformation Effects 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 208000025854 malignant tumor of adrenal cortex Diseases 0.000 claims description 3
- 208000026045 malignant tumor of parathyroid gland Diseases 0.000 claims description 3
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 claims description 3
- 230000036473 myasthenia Effects 0.000 claims description 3
- 201000008026 nephroblastoma Diseases 0.000 claims description 3
- 201000008106 ocular cancer Diseases 0.000 claims description 3
- 210000003101 oviduct Anatomy 0.000 claims description 3
- 229910052760 oxygen Inorganic materials 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 208000007312 paraganglioma Diseases 0.000 claims description 3
- 208000005987 polymyositis Diseases 0.000 claims description 3
- 206010038038 rectal cancer Diseases 0.000 claims description 3
- 201000001275 rectum cancer Diseases 0.000 claims description 3
- 230000001953 sensory effect Effects 0.000 claims description 3
- 208000007056 sickle cell anemia Diseases 0.000 claims description 3
- 210000004500 stellate cell Anatomy 0.000 claims description 3
- 229910052717 sulfur Inorganic materials 0.000 claims description 3
- 201000003120 testicular cancer Diseases 0.000 claims description 3
- 201000002510 thyroid cancer Diseases 0.000 claims description 3
- 208000025444 tumor of salivary gland Diseases 0.000 claims description 3
- 206010046766 uterine cancer Diseases 0.000 claims description 3
- 206010046885 vaginal cancer Diseases 0.000 claims description 3
- 208000013139 vaginal neoplasm Diseases 0.000 claims description 3
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 2
- 208000005440 Basal Cell Neoplasms Diseases 0.000 claims description 2
- 206010061692 Benign muscle neoplasm Diseases 0.000 claims description 2
- 201000009030 Carcinoma Diseases 0.000 claims description 2
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims description 2
- 201000004458 Myoma Diseases 0.000 claims description 2
- 206010028767 Nasal sinus cancer Diseases 0.000 claims description 2
- 206010061332 Paraganglion neoplasm Diseases 0.000 claims description 2
- 208000033014 Plasma cell tumor Diseases 0.000 claims description 2
- 208000007452 Plasmacytoma Diseases 0.000 claims description 2
- 208000026149 Primary peritoneal carcinoma Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 229910005965 SO 2 Inorganic materials 0.000 claims description 2
- 208000015778 Undifferentiated pleomorphic sarcoma Diseases 0.000 claims description 2
- 208000009956 adenocarcinoma Diseases 0.000 claims description 2
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 claims description 2
- 125000003282 alkyl amino group Chemical group 0.000 claims description 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 2
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 201000000053 blastoma Diseases 0.000 claims description 2
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 2
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 2
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 201000008184 embryoma Diseases 0.000 claims description 2
- 201000009277 hairy cell leukemia Diseases 0.000 claims description 2
- 125000004994 halo alkoxy alkyl group Chemical group 0.000 claims description 2
- 125000004692 haloalkylcarbonyl group Chemical group 0.000 claims description 2
- 125000004405 heteroalkoxy group Chemical group 0.000 claims description 2
- 210000005036 nerve Anatomy 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 230000002611 ovarian Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 208000010626 plasma cell neoplasm Diseases 0.000 claims description 2
- 230000002207 retinal effect Effects 0.000 claims description 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 210000001519 tissue Anatomy 0.000 claims description 2
- 235000002566 Capsicum Nutrition 0.000 claims 1
- 240000008574 Capsicum frutescens Species 0.000 claims 1
- 206010015995 Eyelid ptosis Diseases 0.000 claims 1
- 208000002030 Merkel cell carcinoma Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 206010029266 Neuroendocrine carcinoma of the skin 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
- 208000035868 Vascular inflammations Diseases 0.000 claims 1
- 239000001390 capsicum minimum Substances 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000017763 cutaneous neuroendocrine carcinoma Diseases 0.000 claims 1
- 230000029087 digestion Effects 0.000 claims 1
- 230000035558 fertility Effects 0.000 claims 1
- 230000002538 fungal effect Effects 0.000 claims 1
- 208000034737 hemoglobinopathy Diseases 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000003004 ptosis Diseases 0.000 claims 1
- 208000015891 sexual disease Diseases 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 12
- 125000001153 fluoro group Chemical group F* 0.000 description 6
- 210000001161 mammalian embryo Anatomy 0.000 description 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 3
- 208000009329 Graft vs Host Disease Diseases 0.000 description 3
- 230000001413 cellular effect Effects 0.000 description 3
- 208000024908 graft versus host disease Diseases 0.000 description 3
- KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical group C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 description 2
- 208000003200 Adenoma Diseases 0.000 description 2
- 206010001233 Adenoma benign Diseases 0.000 description 2
- 206010004593 Bile duct cancer Diseases 0.000 description 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 description 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 description 2
- 206010005003 Bladder cancer Diseases 0.000 description 2
- 208000009458 Carcinoma in Situ Diseases 0.000 description 2
- 206010053717 Fibrous histiocytoma Diseases 0.000 description 2
- 208000007766 Kaposi sarcoma Diseases 0.000 description 2
- 206010028570 Myelopathy Diseases 0.000 description 2
- 208000007913 Pituitary Neoplasms Diseases 0.000 description 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 description 2
- 208000021386 Sjogren Syndrome Diseases 0.000 description 2
- 206010047115 Vasculitis Diseases 0.000 description 2
- 208000001119 benign fibrous histiocytoma Diseases 0.000 description 2
- 210000000013 bile duct Anatomy 0.000 description 2
- 210000000988 bone and bone Anatomy 0.000 description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 description 2
- 208000008609 collagenous colitis Diseases 0.000 description 2
- 208000029742 colonic neoplasm Diseases 0.000 description 2
- 201000008298 histiocytosis Diseases 0.000 description 2
- 201000004933 in situ carcinoma Diseases 0.000 description 2
- 239000007922 nasal spray Substances 0.000 description 2
- 229940097496 nasal spray Drugs 0.000 description 2
- 208000003154 papilloma Diseases 0.000 description 2
- 208000010916 pituitary tumor Diseases 0.000 description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 2
- 201000005112 urinary bladder cancer Diseases 0.000 description 2
- 208000037965 uterine sarcoma Diseases 0.000 description 2
- KJCVRFUGPWSIIH-UHFFFAOYSA-N 1-naphthol Chemical compound C1=CC=C2C(O)=CC=CC2=C1 KJCVRFUGPWSIIH-UHFFFAOYSA-N 0.000 description 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 206010004146 Basal cell carcinoma Diseases 0.000 description 1
- 206010028729 Nasal cavity cancer Diseases 0.000 description 1
- 208000033383 Neuroendocrine tumor of pancreas Diseases 0.000 description 1
- 206010067517 Pancreatic neuroendocrine tumour Diseases 0.000 description 1
- 201000000582 Retinoblastoma Diseases 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 210000000941 bile Anatomy 0.000 description 1
- 210000004252 chorionic villi Anatomy 0.000 description 1
- LMABXCRKZXCFTB-UHFFFAOYSA-N cinnolin-8-ylmethanamine Chemical compound NCc1cccc2ccnnc12 LMABXCRKZXCFTB-UHFFFAOYSA-N 0.000 description 1
- 125000000392 cycloalkenyl group Chemical group 0.000 description 1
- 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 description 1
- 210000000981 epithelium Anatomy 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 210000002768 hair cell Anatomy 0.000 description 1
- 125000005347 halocycloalkyl group Chemical group 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 1
- 125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 description 1
- 208000021284 ovarian germ cell tumor Diseases 0.000 description 1
- 239000001301 oxygen Chemical group 0.000 description 1
- 208000021010 pancreatic neuroendocrine tumor Diseases 0.000 description 1
- 201000002628 peritoneum cancer Diseases 0.000 description 1
- 208000023974 pharynx neoplasm Diseases 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 206010062261 spinal cord neoplasm Diseases 0.000 description 1
- 208000037959 spinal tumor Diseases 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000011593 sulfur Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022096439A JP2022137047A (ja) | 2016-12-22 | 2022-06-15 | ヒストンメチルトランスフェラーゼ阻害剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662438121P | 2016-12-22 | 2016-12-22 | |
| US62/438,121 | 2016-12-22 | ||
| PCT/US2017/067855 WO2018119208A1 (en) | 2016-12-22 | 2017-12-21 | Histone methyltransferase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022096439A Division JP2022137047A (ja) | 2016-12-22 | 2022-06-15 | ヒストンメチルトランスフェラーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020504716A JP2020504716A (ja) | 2020-02-13 |
| JP2020504716A5 true JP2020504716A5 (enExample) | 2021-02-04 |
| JP7091336B2 JP7091336B2 (ja) | 2022-06-27 |
Family
ID=60972497
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019531160A Active JP7091336B2 (ja) | 2016-12-22 | 2017-12-21 | ヒストンメチルトランスフェラーゼ阻害剤 |
| JP2022096439A Pending JP2022137047A (ja) | 2016-12-22 | 2022-06-15 | ヒストンメチルトランスフェラーゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022096439A Pending JP2022137047A (ja) | 2016-12-22 | 2022-06-15 | ヒストンメチルトランスフェラーゼ阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US10829452B2 (enExample) |
| EP (2) | EP3558971B1 (enExample) |
| JP (2) | JP7091336B2 (enExample) |
| AR (1) | AR110443A1 (enExample) |
| ES (2) | ES2981507T3 (enExample) |
| TW (1) | TW201829386A (enExample) |
| WO (1) | WO2018119208A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3558971B1 (en) * | 2016-12-22 | 2022-02-23 | Global Blood Therapeutics, Inc. | Histone methyltransferase inhibitors |
| EP3612181A4 (en) | 2017-04-21 | 2021-01-06 | Epizyme, Inc. | Combination therapies with ehmt2 inhibitors |
| JP2021500327A (ja) * | 2017-10-18 | 2021-01-07 | エピザイム，インコーポレイティド | 免疫療法にｅｈｍｔ２阻害剤を使用する方法 |
| CA3081946A1 (en) * | 2017-10-18 | 2019-04-25 | Epizyme, Inc. | Methods of using ehmt2 inhibitors in preventing or treating blood disorders |
| WO2019173840A1 (en) | 2018-03-09 | 2019-09-12 | Schlumberger Technology Corporation | Integrated well construction system operations |
| CN111196817B (zh) * | 2018-11-19 | 2021-06-11 | 四川大学华西医院 | 作为brpf1抑制剂的三环化合物 |
| CN113195469B (zh) * | 2019-02-19 | 2024-05-24 | 四川科伦博泰生物医药股份有限公司 | 含氮并环化合物、其制备方法及用途 |
| CN111620818B (zh) * | 2019-02-28 | 2023-09-29 | 暨南大学 | 8,9-二甲氧基啡啶类化合物及其应用 |
| CN116710431A (zh) * | 2020-11-19 | 2023-09-05 | 泰洛治疗公司 | 小分子化合物和组合物 |
| PE20231312A1 (es) * | 2020-11-24 | 2023-08-24 | Amgen Inc | Derivados triciclicos de carboxamida como inhibidores de la prmt5 |
| AU2022212883A1 (en) | 2021-01-27 | 2023-08-17 | Vandria Sa | Urolithin derivatives and methods of use thereof |
| CN113004294B (zh) * | 2021-03-08 | 2023-01-17 | 温州大学新材料与产业技术研究院 | 一种四氢呋喃并1,4-二氢喹啉类化合物及其制备方法和应用 |
| CN114573569B (zh) * | 2022-03-30 | 2023-07-04 | 邦恩泰(山东)生物医药科技集团股份有限公司 | 一种异喹啉类化合物的制备方法 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4107288A (en) | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| CA2402549A1 (en) | 2000-03-15 | 2001-09-20 | Aventis Pharma Deutschland Gmbh | Substituted beta-carbolines |
| JP2006513212A (ja) | 2002-12-20 | 2006-04-20 | スリーエム イノベイティブ プロパティズ カンパニー | アリール／ヘタリール置換されたイミダゾキノリン |
| JP5128815B2 (ja) | 2003-08-27 | 2013-01-23 | スリーエム イノベイティブ プロパティズ カンパニー | アリールオキシ置換およびアリールアルキレンオキシ置換イミダゾキノリン |
| SG149828A1 (en) | 2003-10-03 | 2009-02-27 | 3M Innovative Properties Co | Alkoxy substituted imidazoquinolines |
| WO2006086449A2 (en) | 2005-02-09 | 2006-08-17 | Coley Pharmaceutical Group, Inc. | Alkyloxy substituted thiazoloquinolines and thiazolonaphthyridines |
| CA2974246C (en) * | 2006-09-01 | 2020-02-25 | Senhwa Biosciences, Inc. | Tricyclic heteroaryl compounds and their use as protein modulators |
| RU2487119C2 (ru) | 2007-02-22 | 2013-07-10 | Зингента Партисипейшнс Аг | Производные иминопиридина и их применение в качестве микробиоцидов |
| MX2010006457A (es) | 2007-12-19 | 2010-07-05 | Amgen Inc | Compuestos fusionados de piridina, pirimidina y triazina como inhibidores de ciclo celular. |
| SI2268618T1 (sl) | 2008-03-03 | 2015-09-30 | Novartis Ag | Spojine in sestavki kot modulatorji aktivnosti TLR |
| GB2465405A (en) | 2008-11-10 | 2010-05-19 | Univ Basel | Triazine, pyrimidine and pyridine analogues and their use in therapy |
| KR100968175B1 (ko) * | 2008-11-11 | 2010-07-07 | 제일약품주식회사 | 신규한 트리시클릭 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 약학적 조성물 |
| ES2586856T3 (es) | 2009-10-06 | 2016-10-19 | Millennium Pharmaceuticals, Inc. | Compuestos heterocíclicos útiles como inhibidores de PDK1 |
| US20130231360A1 (en) | 2010-04-22 | 2013-09-05 | The Brigham And Women S Hospital, Inc. | Beta-Carbolines as Inhibitors of Haspin and DYRK Kinases |
| JP2013533239A (ja) | 2010-06-25 | 2013-08-22 | ファキュルテ ユニヴェルシテール ノートル−ダム ド ラ ペ | 増殖性疾患の治療に有用なβカルボリン誘導体 |
| KR101606250B1 (ko) | 2011-03-23 | 2016-03-24 | 암젠 인크 | Cdk 4/6 및 flt3의 융합된 트리사이클릭 이중 저해제 |
| KR101827444B1 (ko) | 2012-02-01 | 2018-02-08 | 제일약품주식회사 | 트리사이클로 유도체 화합물의 신규한 결정형 산부가염 또는 이의 수화물 및 이의 제조방법 |
| US10662193B2 (en) | 2014-01-21 | 2020-05-26 | Ac Immune Sa | Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyloid-like proteins |
| US9284272B2 (en) * | 2014-03-28 | 2016-03-15 | Abbvie Inc. | Inhibitors of histone methyltransferase G9a |
| JP6527534B2 (ja) | 2014-06-16 | 2019-06-05 | ファンダシオン パラ ラ インベスティガシオン メディカ アプリカダＦｕｎｄａｃｉｏｎ Ｐａｒａ Ｌａ Ｉｎｖｅｓｔｉｇａｓｉｏｎ Ｍｅｄｉｃａ Ａｐｌｉｃａｄａ | ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物 |
| US10407423B2 (en) * | 2015-11-16 | 2019-09-10 | Fundación Para La Investigación Médica Aplicada | Compounds as inhibitors of DNA methyltransferases |
| EP3558971B1 (en) * | 2016-12-22 | 2022-02-23 | Global Blood Therapeutics, Inc. | Histone methyltransferase inhibitors |
-
2017
- 2017-12-21 EP EP17829543.2A patent/EP3558971B1/en active Active
- 2017-12-21 US US15/850,389 patent/US10829452B2/en active Active
- 2017-12-21 EP EP22153996.8A patent/EP4063358B1/en active Active
- 2017-12-21 WO PCT/US2017/067855 patent/WO2018119208A1/en not_active Ceased
- 2017-12-21 JP JP2019531160A patent/JP7091336B2/ja active Active
- 2017-12-21 TW TW106145167A patent/TW201829386A/zh unknown
- 2017-12-21 ES ES22153996T patent/ES2981507T3/es active Active
- 2017-12-21 ES ES17829543T patent/ES2910108T3/es active Active
- 2017-12-22 AR ARP170103662A patent/AR110443A1/es unknown
-
2020
- 2020-11-04 US US17/089,239 patent/US11713299B2/en active Active
-
2022
- 2022-06-15 JP JP2022096439A patent/JP2022137047A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020504716A5 (enExample) | ||
| US11571424B2 (en) | Polymorphs of ARRY-380, a selective HER2 inhibitor and pharmaceutical compositions containing them | |
| JP2020125349A5 (enExample) | ||
| CN103124729B (zh) | 作为Axl抑制剂的药物活性化合物 | |
| JP6654646B2 (ja) | Ｔａｍ ｒｔｋインヒビターとしてのキノリン誘導体 | |
| JP2016523973A5 (enExample) | ||
| RU2017118160A (ru) | Фармацевтическое соединение | |
| RU2015143717A (ru) | 2-Аминопиримидин-6-оны и аналоги, проявляющие противораковые и антипролиферативные действия | |
| JP2010241830A5 (enExample) | ||
| CN114430740A (zh) | Egfr抑制剂、组合物及其制备方法 | |
| WO2018214867A9 (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 | |
| TW200403210A (en) | Benzamide derivatives | |
| JP6969800B2 (ja) | 増殖性疾患の治療に使用される置換２，４−ジアミノ−キノリン誘導体 | |
| JP2017534569A (ja) | ＰＩ３Ｋ、ｍＴＯＲ阻害薬としての縮合キノリン化合物 | |
| JP2021525270A (ja) | Ａｘｌ／ｍｅｒ ｒｔｋおよびｃｓｆ１ｒの阻害剤としてのキノリン誘導体 | |
| CN117062819A (zh) | 多环化合物及其用途 | |
| WO2004087679A1 (en) | 2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases | |
| JP2019522681A5 (enExample) | ||
| JP6913955B2 (ja) | ＰＩ３Ｋ／ｍＴＯＲ阻害剤としての溶融キノリン化合物 | |
| JPWO2021076691A5 (enExample) | ||
| KR20230035070A (ko) | Atr 억제제 및 이의 용도 | |
| RU2021136789A (ru) | Триарильные соединения для лечения pd-l1 заболеваний | |
| WO2016050016A1 (zh) | 作为激酶抑制剂的取代杂环化合物及其制备方法和用途 | |
| TW201912636A (zh) | 泊馬度胺衍生物及其製備方法 | |
| JP2015534975A5 (enExample) |