JP2016523973A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016523973A5 JP2016523973A5 JP2016525463A JP2016525463A JP2016523973A5 JP 2016523973 A5 JP2016523973 A5 JP 2016523973A5 JP 2016525463 A JP2016525463 A JP 2016525463A JP 2016525463 A JP2016525463 A JP 2016525463A JP 2016523973 A5 JP2016523973 A5 JP 2016523973A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- unsubstituted
- compound
- compound according
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 104
- 150000001875 compounds Chemical class 0.000 claims description 88
- 229910052739 hydrogen Inorganic materials 0.000 claims description 50
- 239000001257 hydrogen Substances 0.000 claims description 40
- 125000000623 heterocyclic group Chemical group 0.000 claims description 33
- 150000003839 salts Chemical class 0.000 claims description 30
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 29
- 229910052736 halogen Inorganic materials 0.000 claims description 27
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 26
- 201000010099 disease Diseases 0.000 claims description 26
- 150000002367 halogens Chemical class 0.000 claims description 26
- 102000001301 EGF receptor Human genes 0.000 claims description 25
- 108060006698 EGF receptor Proteins 0.000 claims description 25
- 206010028980 Neoplasm Diseases 0.000 claims description 18
- 125000005843 halogen group Chemical group 0.000 claims description 18
- 125000003342 alkenyl group Chemical group 0.000 claims description 15
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 15
- 150000002431 hydrogen Chemical class 0.000 claims description 13
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
- 108091008794 FGF receptors Proteins 0.000 claims description 9
- 102000044168 Fibroblast Growth Factor Receptor Human genes 0.000 claims description 9
- 201000011510 cancer Diseases 0.000 claims description 9
- 125000003107 substituted aryl group Chemical group 0.000 claims description 9
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 7
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims description 7
- 230000001404 mediated effect Effects 0.000 claims description 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 6
- 108091000080 Phosphotransferase Proteins 0.000 claims description 5
- 230000004913 activation Effects 0.000 claims description 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 5
- 102000020233 phosphotransferase Human genes 0.000 claims description 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 3
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims description 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 3
- 229960001433 erlotinib Drugs 0.000 claims description 3
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 3
- 229960002584 gefitinib Drugs 0.000 claims description 3
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims description 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 3
- 238000002626 targeted therapy Methods 0.000 claims description 3
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 2
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000008024 pharmaceutical diluent Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 238000000034 method Methods 0.000 description 41
- 230000035772 mutation Effects 0.000 description 20
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 13
- 201000005202 lung cancer Diseases 0.000 description 13
- 208000020816 lung neoplasm Diseases 0.000 description 13
- 206010006187 Breast cancer Diseases 0.000 description 9
- 208000026310 Breast neoplasm Diseases 0.000 description 9
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 9
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 9
- 208000008443 pancreatic carcinoma Diseases 0.000 description 9
- 208000008839 Kidney Neoplasms Diseases 0.000 description 8
- 206010038389 Renal cancer Diseases 0.000 description 8
- 208000005718 Stomach Neoplasms Diseases 0.000 description 8
- 206010017758 gastric cancer Diseases 0.000 description 8
- 201000010982 kidney cancer Diseases 0.000 description 8
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 8
- 201000002528 pancreatic cancer Diseases 0.000 description 8
- 201000011549 stomach cancer Diseases 0.000 description 8
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 8
- 206010025323 Lymphomas Diseases 0.000 description 7
- 206010009944 Colon cancer Diseases 0.000 description 6
- 208000032839 leukemia Diseases 0.000 description 6
- 206010005949 Bone cancer Diseases 0.000 description 5
- 208000018084 Bone neoplasm Diseases 0.000 description 5
- 208000003174 Brain Neoplasms Diseases 0.000 description 5
- 206010033128 Ovarian cancer Diseases 0.000 description 5
- 206010061535 Ovarian neoplasm Diseases 0.000 description 5
- 206010060862 Prostate cancer Diseases 0.000 description 5
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 5
- 208000000453 Skin Neoplasms Diseases 0.000 description 5
- 208000029742 colonic neoplasm Diseases 0.000 description 5
- 201000007270 liver cancer Diseases 0.000 description 5
- 208000014018 liver neoplasm Diseases 0.000 description 5
- 201000000849 skin cancer Diseases 0.000 description 5
- 208000030507 AIDS Diseases 0.000 description 4
- 201000004624 Dermatitis Diseases 0.000 description 4
- 208000032612 Glial tumor Diseases 0.000 description 4
- 206010018338 Glioma Diseases 0.000 description 4
- 206010035226 Plasma cell myeloma Diseases 0.000 description 4
- 206010063837 Reperfusion injury Diseases 0.000 description 4
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 description 4
- 206010003246 arthritis Diseases 0.000 description 4
- 208000005017 glioblastoma Diseases 0.000 description 4
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 4
- 201000000050 myeloid neoplasm Diseases 0.000 description 4
- 208000010125 myocardial infarction Diseases 0.000 description 4
- 201000000596 systemic lupus erythematosus Diseases 0.000 description 4
- 206010019280 Heart failures Diseases 0.000 description 3
- 206010035664 Pneumonia Diseases 0.000 description 3
- 208000006011 Stroke Diseases 0.000 description 3
- 230000000747 cardiac effect Effects 0.000 description 3
- -1 hydrogen Compound Chemical class 0.000 description 3
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 description 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 description 2
- 206010003210 Arteriosclerosis Diseases 0.000 description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 2
- 206010006895 Cachexia Diseases 0.000 description 2
- 206010007559 Cardiac failure congestive Diseases 0.000 description 2
- 208000024172 Cardiovascular disease Diseases 0.000 description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 description 2
- 208000011231 Crohn disease Diseases 0.000 description 2
- 208000007882 Gastritis Diseases 0.000 description 2
- 201000005569 Gout Diseases 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 2
- 208000003456 Juvenile Arthritis Diseases 0.000 description 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 2
- 208000012902 Nervous system disease Diseases 0.000 description 2
- 208000002193 Pain Diseases 0.000 description 2
- 208000033826 Promyelocytic Acute Leukemia Diseases 0.000 description 2
- 201000004681 Psoriasis Diseases 0.000 description 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 description 2
- 206010040047 Sepsis Diseases 0.000 description 2
- 230000003213 activating effect Effects 0.000 description 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 description 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 description 2
- 230000002917 arthritic effect Effects 0.000 description 2
- 208000006673 asthma Diseases 0.000 description 2
- 208000010668 atopic eczema Diseases 0.000 description 2
- 208000015114 central nervous system disease Diseases 0.000 description 2
- 230000001684 chronic effect Effects 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 210000002919 epithelial cell Anatomy 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 208000027866 inflammatory disease Diseases 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 description 2
- 208000028867 ischemia Diseases 0.000 description 2
- 201000008482 osteoarthritis Diseases 0.000 description 2
- 230000036407 pain Effects 0.000 description 2
- 230000002685 pulmonary effect Effects 0.000 description 2
- 201000003651 pulmonary sarcoidosis Diseases 0.000 description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 description 2
- 201000005671 spondyloarthropathy Diseases 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- CSGQVNMSRKWUSH-IAGOWNOFSA-N (3r,4r)-4-amino-1-[[4-(3-methoxyanilino)pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol Chemical compound COC1=CC=CC(NC=2C3=C(CN4C[C@@H](O)[C@H](N)CC4)C=CN3N=CN=2)=C1 CSGQVNMSRKWUSH-IAGOWNOFSA-N 0.000 description 1
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 description 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 208000005440 Basal Cell Neoplasms Diseases 0.000 description 1
- 206010004146 Basal cell carcinoma Diseases 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 201000006474 Brain Ischemia Diseases 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- 208000031229 Cardiomyopathies Diseases 0.000 description 1
- 206010008120 Cerebral ischaemia Diseases 0.000 description 1
- 206010008342 Cervix carcinoma Diseases 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- 206010009900 Colitis ulcerative Diseases 0.000 description 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 description 1
- 208000031886 HIV Infections Diseases 0.000 description 1
- 208000037357 HIV infectious disease Diseases 0.000 description 1
- 208000016988 Hemorrhagic Stroke Diseases 0.000 description 1
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 description 1
- 208000023105 Huntington disease Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 239000002136 L01XE07 - Lapatinib Substances 0.000 description 1
- 206010062038 Lip neoplasm Diseases 0.000 description 1
- 208000004852 Lung Injury Diseases 0.000 description 1
- 208000019693 Lung disease Diseases 0.000 description 1
- 201000009906 Meningitis Diseases 0.000 description 1
- 206010027476 Metastases Diseases 0.000 description 1
- 208000000112 Myalgia Diseases 0.000 description 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 description 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 1
- 208000001388 Opportunistic Infections Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 1
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- 208000006265 Renal cell carcinoma Diseases 0.000 description 1
- 206010040070 Septic Shock Diseases 0.000 description 1
- 201000010001 Silicosis Diseases 0.000 description 1
- 208000007107 Stomach Ulcer Diseases 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 206010069363 Traumatic lung injury Diseases 0.000 description 1
- 208000025865 Ulcer Diseases 0.000 description 1
- 201000006704 Ulcerative Colitis Diseases 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 208000009956 adenocarcinoma Diseases 0.000 description 1
- 229960001686 afatinib Drugs 0.000 description 1
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 230000003321 amplification Effects 0.000 description 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 1
- 230000001640 apoptogenic effect Effects 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 208000019664 bone resorption disease Diseases 0.000 description 1
- 208000035269 cancer or benign tumor Diseases 0.000 description 1
- OMZCMEYTWSXEPZ-UHFFFAOYSA-N canertinib Chemical compound C1=C(Cl)C(F)=CC=C1NC1=NC=NC2=CC(OCCCN3CCOCC3)=C(NC(=O)C=C)C=C12 OMZCMEYTWSXEPZ-UHFFFAOYSA-N 0.000 description 1
- 150000001721 carbon Chemical group 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 201000010881 cervical cancer Diseases 0.000 description 1
- 229960005395 cetuximab Drugs 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 210000004351 coronary vessel Anatomy 0.000 description 1
- 230000037430 deletion Effects 0.000 description 1
- 238000012217 deletion Methods 0.000 description 1
- 208000010643 digestive system disease Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 201000004101 esophageal cancer Diseases 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 201000005917 gastric ulcer Diseases 0.000 description 1
- 208000018685 gastrointestinal system disease Diseases 0.000 description 1
- 208000024908 graft versus host disease Diseases 0.000 description 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 206010022000 influenza Diseases 0.000 description 1
- 230000037431 insertion Effects 0.000 description 1
- 238000003780 insertion Methods 0.000 description 1
- 208000020658 intracerebral hemorrhage Diseases 0.000 description 1
- 230000000302 ischemic 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
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 229960004891 lapatinib Drugs 0.000 description 1
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 201000006721 lip cancer Diseases 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 231100000515 lung injury Toxicity 0.000 description 1
- 201000004792 malaria Diseases 0.000 description 1
- 229950008001 matuzumab Drugs 0.000 description 1
- 230000009401 metastasis Effects 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 208000013465 muscle pain Diseases 0.000 description 1
- ZAJXXUDARPGGOC-UHFFFAOYSA-N n-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide Chemical compound C1CN(C)CCN1C(C)(C)C#CC1=CC2=NC=NC(NC=3C=C(Cl)C(F)=CC=3)=C2C=C1NC(=O)C=C ZAJXXUDARPGGOC-UHFFFAOYSA-N 0.000 description 1
- 230000009826 neoplastic cell growth Effects 0.000 description 1
- 201000008383 nephritis Diseases 0.000 description 1
- 229950008835 neratinib Drugs 0.000 description 1
- ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 description 1
- 208000004296 neuralgia Diseases 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 230000003959 neuroinflammation Effects 0.000 description 1
- 208000021722 neuropathic pain Diseases 0.000 description 1
- 238000003199 nucleic acid amplification method Methods 0.000 description 1
- 201000005443 oral cavity cancer Diseases 0.000 description 1
- 229960001972 panitumumab Drugs 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 230000036303 septic shock Effects 0.000 description 1
- 208000020352 skin basal cell carcinoma Diseases 0.000 description 1
- 201000010106 skin squamous cell carcinoma Diseases 0.000 description 1
- 201000002314 small intestine cancer Diseases 0.000 description 1
- 208000020431 spinal cord injury Diseases 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- HVXKQKFEHMGHSL-QKDCVEJESA-N tesevatinib Chemical compound N1=CN=C2C=C(OC[C@@H]3C[C@@H]4CN(C)C[C@@H]4C3)C(OC)=CC2=C1NC1=CC=C(Cl)C(Cl)=C1F HVXKQKFEHMGHSL-QKDCVEJESA-N 0.000 description 1
- 229950003046 tesevatinib Drugs 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 241001529453 unidentified herpesvirus Species 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361844304P | 2013-07-09 | 2013-07-09 | |
| US61/844,304 | 2013-07-09 | ||
| US201361901808P | 2013-11-08 | 2013-11-08 | |
| US61/901,808 | 2013-11-08 | ||
| PCT/US2014/046022 WO2015006492A1 (en) | 2013-07-09 | 2014-07-09 | Kinase inhibitors for the treatment of disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016523973A JP2016523973A (ja) | 2016-08-12 |
| JP2016523973A5 true JP2016523973A5 (enExample) | 2017-07-27 |
Family
ID=52280579
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016525463A Pending JP2016523973A (ja) | 2013-07-09 | 2014-07-09 | 疾患の処置のためのキナーゼ阻害物質 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US9783504B2 (enExample) |
| EP (1) | EP3019491A4 (enExample) |
| JP (1) | JP2016523973A (enExample) |
| AU (1) | AU2014287209B2 (enExample) |
| CA (1) | CA2917667A1 (enExample) |
| WO (1) | WO2015006492A1 (enExample) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| GB201204384D0 (en) | 2012-03-13 | 2012-04-25 | Univ Dundee | Anti-flammatory agents |
| US9611267B2 (en) | 2012-06-13 | 2017-04-04 | Incyte Holdings Corporation | Substituted tricyclic compounds as FGFR inhibitors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| EP3943087A1 (en) | 2013-03-15 | 2022-01-26 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| TWI649318B (zh) | 2013-04-19 | 2019-02-01 | 英塞特控股公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| WO2015006492A1 (en) * | 2013-07-09 | 2015-01-15 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
| LT3057943T (lt) | 2013-10-18 | 2018-11-12 | Eisai R&D Management Co., Ltd. | Pirimidino fgfr4 slopikliai |
| PE20160546A1 (es) | 2013-10-25 | 2016-05-26 | Novartis Ag | Compuestos derivados de piridilo biciclicos fusionados a anillo como inhibidores de fgfr4 |
| JP6522619B2 (ja) | 2013-12-13 | 2019-05-29 | ノバルティス アーゲー | 医薬剤形 |
| CN104860891B (zh) * | 2014-02-25 | 2017-06-30 | 上海海雁医药科技有限公司 | 芳氨基嘧啶类化合物及其应用以及由其制备的药物组合物和药用组合物 |
| MA38393B1 (fr) | 2014-03-13 | 2018-11-30 | Sanofi Sa | Composés hétéroaryle et utilisations associées |
| WO2016014542A1 (en) | 2014-07-21 | 2016-01-28 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| EP3172213B1 (en) | 2014-07-21 | 2021-09-22 | Dana-Farber Cancer Institute, Inc. | Macrocyclic kinase inhibitors and uses thereof |
| AU2015300782B2 (en) | 2014-08-08 | 2020-04-16 | Dana-Farber Cancer Institute, Inc. | Uses of salt-inducible kinase (SIK) inhibitors |
| JP6585167B2 (ja) | 2014-10-03 | 2019-10-02 | ノバルティス アーゲー | Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CN107530298B (zh) * | 2015-01-26 | 2021-06-04 | 耶鲁大学 | 利用酪氨酸激酶抑制剂的组合物和方法 |
| CN105985342B (zh) * | 2015-02-06 | 2018-07-24 | 华东理工大学 | 作为egfr抑制剂的嘧啶并嘧啶二酮衍生物及其应用 |
| CN105884695B (zh) * | 2015-02-13 | 2019-02-26 | 山东轩竹医药科技有限公司 | 杂环衍生物类酪氨酸激酶抑制剂 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| AU2016219822B2 (en) * | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9802917B2 (en) | 2015-03-25 | 2017-10-31 | Novartis Ag | Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide |
| WO2016168331A1 (en) | 2015-04-14 | 2016-10-20 | Eisai R&D Management Co., Ltd. | Crystalline fgfr4 inhibitor compound and uses thereof |
| CN104860890B (zh) * | 2015-04-29 | 2018-03-13 | 上海泓博智源医药股份有限公司 | T790m突变型egfr的抑制剂及其在制备抗肿瘤药物中的应用 |
| WO2017012647A1 (en) * | 2015-07-20 | 2017-01-26 | Galapagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
| AU2016296877B2 (en) * | 2015-07-20 | 2020-09-17 | Dana-Farber Cancer Institute, Inc. | Novel pyrimidines as EGFR inhibitors and methods of treating disorders |
| CN106892922B (zh) * | 2015-12-18 | 2019-04-19 | 华东理工大学 | 作为egfr抑制剂的5,8-二氢蝶啶-6,7-二酮衍生物及其应用 |
| JP7372740B2 (ja) | 2016-05-10 | 2023-11-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 細胞生存性及び／又は細胞増殖を低減するための薬物の組み合わせ |
| US10954242B2 (en) | 2016-07-05 | 2021-03-23 | The Broad Institute, Inc. | Bicyclic urea kinase inhibitors and uses thereof |
| US11241435B2 (en) | 2016-09-16 | 2022-02-08 | The General Hospital Corporation | Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis |
| US11285158B2 (en) | 2017-02-28 | 2022-03-29 | The General Hospital Corporation | Uses of pyrimidopyrimidinones as SIK inhibitors |
| AU2018229148B2 (en) * | 2017-03-03 | 2022-08-04 | Auckland Uniservices Limited | FGFR kinase inhibitors and pharmaceutical uses |
| CN108727382B (zh) * | 2017-04-19 | 2022-07-19 | 华东理工大学 | 作为btk抑制剂的杂环化合物及其应用 |
| DK3391907T3 (da) | 2017-04-20 | 2020-03-09 | Iomx Therapeutics Ag | Intracellulær kinase sik3, der er associeret med resistens over for antitumorimmunresponser, og anvendelser deraf |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN109384790B (zh) * | 2017-08-08 | 2022-05-10 | 药捷安康(南京)科技股份有限公司 | 成纤维细胞生长因子受体抑制剂及其用途 |
| WO2019075386A1 (en) | 2017-10-13 | 2019-04-18 | The Regents Of The University Of California | MODULATORS OF MTORC1 |
| ES2991427T3 (es) | 2018-05-04 | 2024-12-03 | Incyte Corp | Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas |
| TW201946630A (zh) | 2018-05-04 | 2019-12-16 | 美商英塞特公司 | Fgfr抑制劑之鹽 |
| JP2021530470A (ja) * | 2018-06-30 | 2021-11-11 | ナショナル インスティテュート オブ バイオロジカル サイエンシズ, ベイジンNational Institute Of Biological Sciences, Beijing | カテプシンｃ阻害剤 |
| US12415816B2 (en) | 2018-11-07 | 2025-09-16 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| WO2020097400A1 (en) * | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as janus kinase 2 inhibitors and uses thereof |
| US12522583B2 (en) | 2018-11-07 | 2026-01-13 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| RS65019B1 (sr) | 2019-05-10 | 2024-01-31 | Deciphera Pharmaceuticals Llc | Fenilaminopirimidin amidni inhibitori autofagije i postupci njihove primene |
| AU2020274011B2 (en) | 2019-05-10 | 2024-02-15 | Deciphera Pharmaceuticals, Llc | Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| CN119241444A (zh) | 2019-06-17 | 2025-01-03 | 德西费拉制药有限责任公司 | 氨基嘧啶酰胺自噬抑制剂及其使用方法 |
| CN110283130B (zh) * | 2019-07-05 | 2023-12-19 | 温州医科大学 | 一种1-(2,5-二甲氧基苯基)-3-取代脲类结肠癌抑制剂及其制备和应用 |
| CN110563657B (zh) * | 2019-07-05 | 2024-05-03 | 温州医科大学 | 一种1-(2,6-二氯苯基)-3-取代脲类结肠癌抑制剂及其制备和应用 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| GEAP202415945A (en) | 2019-10-14 | 2024-04-25 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AU2020414132B2 (en) * | 2019-12-23 | 2024-02-15 | Beijing Scitech-Mq Pharmaceuticals Limited | Cyano-substituted pyridine and cyano-substituted pyrimidine compound and preparation method therefor and application thereof |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| AU2021262482A1 (en) | 2020-04-28 | 2023-01-05 | Iomx Therapeutics Ag | Bicyclic kinase inhibitors and uses thereof |
| TW202204350A (zh) | 2020-05-06 | 2022-02-01 | 美商雅捷可斯治療公司 | 作為ｊａｋ２抑制劑之６－雜芳基氧基苯并咪唑及氮雜苯并咪唑 |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| US12043632B2 (en) | 2020-12-23 | 2024-07-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| EP4304586A4 (en) | 2021-03-10 | 2025-04-02 | Jnana Therapeutics Inc. | SMALL MOLECULE INHIBITORS OF MAMMALIAN SLC6A19 FUNCTION |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| AR126101A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4382520A4 (en) * | 2021-08-02 | 2025-07-16 | Abbisko Therapeutics Co Ltd | PYRIMIDINE-4,6-DIAMINE DERIVATIVE, ITS PREPARATION PROCESS AND ITS PHARMACEUTICAL USE |
| WO2023069959A1 (en) * | 2021-10-18 | 2023-04-27 | Dana-Farber Cancer Institute, Inc. | Covalent egfr inhibitors and methods of use thereof |
| WO2023086320A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of jak2 |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| CN115894381B (zh) * | 2022-11-11 | 2024-10-18 | 温州医科大学 | 一种2,4,5-三取代嘧啶类化合物及其制备方法和用途 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1801112A1 (en) | 1998-05-26 | 2007-06-27 | Warner-Lambert Company LLC | Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation |
| EE200000706A (et) * | 1998-05-26 | 2002-06-17 | Warner-Lambert Company | Bitsüklilised pürimidiinid ja bitsüklilised 3,4-dihüdropürimidiinid kui rakkude proliferatsiooni inhibiitorid |
| JP2003525897A (ja) * | 2000-03-06 | 2003-09-02 | アストラゼネカ アクチボラグ | 治 療 |
| US20030158188A1 (en) | 2002-02-20 | 2003-08-21 | Chih-Hung Lee | Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor |
| US7112676B2 (en) * | 2002-11-04 | 2006-09-26 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| US7504396B2 (en) * | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| BRPI0413005A (pt) * | 2003-07-29 | 2006-09-26 | Irm Llc | compostos e composições como inibidores da proteìna cinase |
| PT1733056E (pt) | 2004-03-31 | 2013-08-29 | Gen Hospital Corp | Método para determinar a responsividade do cancro a tratamentos visando o receptor do factor de crescimento epidérmico |
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| US20090023723A1 (en) * | 2005-09-21 | 2009-01-22 | Pharmacopeia Drug Discovery, Inc. | Purinone derivatives for treating neurodegenerative diseases |
| MEP3808A (xx) * | 2005-12-21 | 2010-02-10 | Novartis Ag | Derivati pirimidinil aril uree kao fgf inhibitori |
| MX2008014618A (es) * | 2006-05-15 | 2008-11-28 | Irm Llc | Composiciones y metodos para inhibidores de cinasas del receptor fgf. |
| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| AR079257A1 (es) * | 2009-12-07 | 2012-01-04 | Novartis Ag | Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas |
| US20120258940A1 (en) * | 2009-12-18 | 2012-10-11 | Giordano Caponigro | Method for treating haematological cancers |
| KR101301533B1 (ko) * | 2010-02-09 | 2013-09-04 | 한미사이언스 주식회사 | 암세포 성장 억제 효과를 갖는 신규 피리미딘 유도체 |
| CN102816162B (zh) * | 2011-06-10 | 2016-04-27 | 中国科学院广州生物医药与健康研究院 | 嘧啶并嘧啶酮类化合物及其药用组合物和应用 |
| WO2013088191A1 (en) * | 2011-12-12 | 2013-06-20 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3 |
| GB201204384D0 (en) * | 2012-03-13 | 2012-04-25 | Univ Dundee | Anti-flammatory agents |
| US9611267B2 (en) * | 2012-06-13 | 2017-04-04 | Incyte Holdings Corporation | Substituted tricyclic compounds as FGFR inhibitors |
| DK2872491T3 (da) * | 2012-07-11 | 2021-08-09 | Blueprint Medicines Corp | Inhibitorer af fibroblastvækstfaktorreceptoren |
| WO2015006492A1 (en) * | 2013-07-09 | 2015-01-15 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
-
2014
- 2014-07-09 WO PCT/US2014/046022 patent/WO2015006492A1/en not_active Ceased
- 2014-07-09 JP JP2016525463A patent/JP2016523973A/ja active Pending
- 2014-07-09 CA CA2917667A patent/CA2917667A1/en not_active Abandoned
- 2014-07-09 EP EP14822373.8A patent/EP3019491A4/en not_active Withdrawn
- 2014-07-09 US US14/903,650 patent/US9783504B2/en active Active
- 2014-07-09 AU AU2014287209A patent/AU2014287209B2/en not_active Ceased
-
2017
- 2017-09-06 US US15/696,309 patent/US10316002B2/en not_active Expired - Fee Related
-
2019
- 2019-05-06 US US16/403,793 patent/US10906878B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016523973A5 (enExample) | ||
| JP7738619B2 (ja) | Ｅｒｂｂ／ｂｔｋ阻害剤 | |
| AU2015222584B2 (en) | 2,4-disubstituted phenylene-1,5-diamine derivatives and applications thereof, and pharmaceutical compositions and pharmaceutically acceptable compositions prepared therefrom | |
| KR102166002B1 (ko) | 섬유 아세포 성장 인자 수용체 키나아제 억제제인 인다졸계 화합물 및 이의 제조와 응용 | |
| AU2015353210B2 (en) | 2-aminopyrimidine compound and pharmaceutical composition and use thereof | |
| JP2020528907A5 (enExample) | ||
| JP2019519476A5 (enExample) | ||
| JP2019514883A5 (enExample) | ||
| JP2019514903A5 (enExample) | ||
| JP5323289B1 (ja) | 新規ピペリジン化合物又はその塩 | |
| JP2020504716A5 (enExample) | ||
| JP2016509583A5 (enExample) | ||
| RU2015143717A (ru) | 2-Аминопиримидин-6-оны и аналоги, проявляющие противораковые и антипролиферативные действия | |
| JP2019514882A5 (enExample) | ||
| HUE033177T2 (en) | Pyrazine carboxamide compound | |
| JP2014503567A5 (enExample) | ||
| PT2727918T (pt) | Compostos e composições como inibidores de proteína quinase | |
| JP2010522765A5 (enExample) | ||
| JP2017537114A5 (enExample) | ||
| JPWO2010128659A1 (ja) | ジアミノへテロ環カルボキサミド化合物 | |
| CN110582483A (zh) | 含邻氨基杂芳环炔基的化合物及其制备方法和用途 | |
| WO2016006706A1 (ja) | テトラヒドロピラ二ルメチル基を有するピリドン誘導体 | |
| JP2014524476A5 (enExample) | ||
| JP2014530243A (ja) | Ａｒｒｙ−３８０の多形体、選択的ｈｅｒｂ２阻害剤、およびそれらを含有する薬学的組成物 | |
| JP2019510801A5 (enExample) |