JP2018508525A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018508525A5 JP2018508525A5 JP2017546176A JP2017546176A JP2018508525A5 JP 2018508525 A5 JP2018508525 A5 JP 2018508525A5 JP 2017546176 A JP2017546176 A JP 2017546176A JP 2017546176 A JP2017546176 A JP 2017546176A JP 2018508525 A5 JP2018508525 A5 JP 2018508525A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- disorder
- methyl
- cancer
- pharmaceutical composition
- 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
- 208000010877 cognitive disease Diseases 0.000 claims description 9
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 150000001875 compounds Chemical class 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 206010008025 Cerebellar ataxia Diseases 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- 208000024827 Alzheimer disease Diseases 0.000 claims description 6
- 206010003591 Ataxia Diseases 0.000 claims description 6
- 208000020925 Bipolar disease Diseases 0.000 claims description 6
- FTALBRSUTCGOEG-UHFFFAOYSA-N Riluzole Chemical compound C1=C(OC(F)(F)F)C=C2SC(N)=NC2=C1 FTALBRSUTCGOEG-UHFFFAOYSA-N 0.000 claims description 6
- -1 diastereomers Chemical class 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 208000027061 mild cognitive impairment Diseases 0.000 claims description 6
- 229960004181 riluzole Drugs 0.000 claims description 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 5
- 230000002265 prevention Effects 0.000 claims description 5
- 208000019901 Anxiety disease Diseases 0.000 claims description 4
- 102000014461 Ataxins Human genes 0.000 claims description 4
- 108010078286 Ataxins Proteins 0.000 claims description 4
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims description 4
- 206010048327 Supranuclear palsy Diseases 0.000 claims description 4
- 239000002246 antineoplastic agent Substances 0.000 claims description 4
- 230000036506 anxiety Effects 0.000 claims description 4
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 206010001497 Agitation Diseases 0.000 claims description 3
- 208000000044 Amnesia Diseases 0.000 claims description 3
- 208000028698 Cognitive impairment Diseases 0.000 claims description 3
- 206010012218 Delirium Diseases 0.000 claims description 3
- 206010012289 Dementia Diseases 0.000 claims description 3
- 206010013142 Disinhibition Diseases 0.000 claims description 3
- 208000030814 Eating disease Diseases 0.000 claims description 3
- 208000019454 Feeding and Eating disease Diseases 0.000 claims description 3
- 208000001914 Fragile X syndrome Diseases 0.000 claims description 3
- 201000011240 Frontotemporal dementia Diseases 0.000 claims description 3
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims description 3
- 208000023105 Huntington disease Diseases 0.000 claims description 3
- 206010022998 Irritability Diseases 0.000 claims description 3
- 208000020358 Learning disease Diseases 0.000 claims description 3
- 208000026139 Memory disease Diseases 0.000 claims description 3
- 208000036626 Mental retardation Diseases 0.000 claims description 3
- 208000019022 Mood disease Diseases 0.000 claims description 3
- 206010028570 Myelopathy Diseases 0.000 claims description 3
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims description 3
- 208000018737 Parkinson disease Diseases 0.000 claims description 3
- 208000028017 Psychotic disease Diseases 0.000 claims description 3
- 208000006289 Rett Syndrome Diseases 0.000 claims description 3
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 3
- 208000009205 Tinnitus Diseases 0.000 claims description 3
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 3
- 208000016620 Tourette disease Diseases 0.000 claims description 3
- 238000013019 agitation Methods 0.000 claims description 3
- 208000029560 autism spectrum disease Diseases 0.000 claims description 3
- 230000001684 chronic effect Effects 0.000 claims description 3
- 235000014632 disordered eating Nutrition 0.000 claims description 3
- 206010013663 drug dependence Diseases 0.000 claims description 3
- 208000037870 generalized anxiety Diseases 0.000 claims description 3
- 208000037119 hereditary cerebellar ataxia Diseases 0.000 claims description 3
- 201000003723 learning disability Diseases 0.000 claims description 3
- 208000024714 major depressive disease Diseases 0.000 claims description 3
- 230000006984 memory degeneration Effects 0.000 claims description 3
- 208000023060 memory loss Diseases 0.000 claims description 3
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 3
- 208000019906 panic disease Diseases 0.000 claims description 3
- 208000022821 personality disease Diseases 0.000 claims description 3
- 208000028173 post-traumatic stress disease Diseases 0.000 claims description 3
- 238000001959 radiotherapy Methods 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- 239000003772 serotonin uptake inhibitor Substances 0.000 claims description 3
- 201000000849 skin cancer Diseases 0.000 claims description 3
- 239000012453 solvate Substances 0.000 claims description 3
- 208000020431 spinal cord injury Diseases 0.000 claims description 3
- 208000002320 spinal muscular atrophy Diseases 0.000 claims description 3
- 208000011117 substance-related disease Diseases 0.000 claims description 3
- 231100000886 tinnitus Toxicity 0.000 claims description 3
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000024412 Friedreich ataxia Diseases 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 201000002832 Lewy body dementia Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 208000001089 Multiple system atrophy Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 2
- 206010057644 Testis cancer Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 201000006517 essential tremor Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 230000001314 paroxysmal effect Effects 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- 201000003120 testicular cancer Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 206010000117 Abnormal behaviour Diseases 0.000 claims 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 2
- 206010039897 Sedation Diseases 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000002996 emotional effect Effects 0.000 claims 2
- 229930195712 glutamate Natural products 0.000 claims 2
- IPWFJLQDVFKJDU-UHFFFAOYSA-N pentanamide Chemical compound CCCCC(N)=O IPWFJLQDVFKJDU-UHFFFAOYSA-N 0.000 claims 2
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 2
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims 2
- UDYQHXHUPLIQEA-OAHLLOKOSA-N (2R)-2-amino-N-[2-[methyl-[2-oxo-2-[[6-(trifluoromethoxy)-1,3-benzothiazol-2-yl]amino]ethyl]amino]-2-oxoethyl]-3-phenylpropanamide Chemical compound N[C@@H](C(=O)NCC(=O)N(CC(NC=1SC2=C(N=1)C=CC(=C2)OC(F)(F)F)=O)C)CC1=CC=CC=C1 UDYQHXHUPLIQEA-OAHLLOKOSA-N 0.000 claims 1
- UDYQHXHUPLIQEA-HNNXBMFYSA-N (2S)-2-amino-N-[2-[methyl-[2-oxo-2-[[6-(trifluoromethoxy)-1,3-benzothiazol-2-yl]amino]ethyl]amino]-2-oxoethyl]-3-phenylpropanamide Chemical compound N[C@H](C(=O)NCC(N(CC(NC=1SC2=C(N=1)C=CC(=C2)OC(F)(F)F)=O)C)=O)CC1=CC=CC=C1 UDYQHXHUPLIQEA-HNNXBMFYSA-N 0.000 claims 1
- YABJJWZLRMPFSI-UHFFFAOYSA-N 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-2-benzimidazolamine Chemical compound N=1C2=CC(OC=3C=C(N=CC=3)C=3NC(=CN=3)C(F)(F)F)=CC=C2N(C)C=1NC1=CC=C(C(F)(F)F)C=C1 YABJJWZLRMPFSI-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 1
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 claims 1
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 1
- RVAQIUULWULRNW-UHFFFAOYSA-N Ganetespib Chemical compound C1=C(O)C(C(C)C)=CC(C=2N(C(O)=NN=2)C=2C=C3C=CN(C)C3=CC=2)=C1O RVAQIUULWULRNW-UHFFFAOYSA-N 0.000 claims 1
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 1
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims 1
- 239000002139 L01XE22 - Masitinib Substances 0.000 claims 1
- 208000009829 Lewy Body Disease Diseases 0.000 claims 1
- 206010033799 Paralysis Diseases 0.000 claims 1
- ACWZRVQXLIRSDF-UHFFFAOYSA-N binimetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1F ACWZRVQXLIRSDF-UHFFFAOYSA-N 0.000 claims 1
- 229960003065 bosentan Drugs 0.000 claims 1
- SXTRWVVIEPWAKM-UHFFFAOYSA-N bosentan hydrate Chemical compound O.COC1=CC=CC=C1OC(C(=NC(=N1)C=2N=CC=CN=2)OCCO)=C1NS(=O)(=O)C1=CC=C(C(C)(C)C)C=C1 SXTRWVVIEPWAKM-UHFFFAOYSA-N 0.000 claims 1
- 229950003628 buparlisib Drugs 0.000 claims 1
- 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 1
- 229960002465 dabrafenib Drugs 0.000 claims 1
- BFSMGDJOXZAERB-UHFFFAOYSA-N dabrafenib Chemical compound S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 BFSMGDJOXZAERB-UHFFFAOYSA-N 0.000 claims 1
- 229960005167 everolimus Drugs 0.000 claims 1
- 229950009672 glembatumumab vedotin Drugs 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Substances C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 1
- 229960005386 ipilimumab Drugs 0.000 claims 1
- 229960004942 lenalidomide Drugs 0.000 claims 1
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims 1
- 229960003784 lenvatinib Drugs 0.000 claims 1
- WOSKHXYHFSIKNG-UHFFFAOYSA-N lenvatinib Chemical compound C=12C=C(C(N)=O)C(OC)=CC2=NC=CC=1OC(C=C1Cl)=CC=C1NC(=O)NC1CC1 WOSKHXYHFSIKNG-UHFFFAOYSA-N 0.000 claims 1
- 229960004655 masitinib Drugs 0.000 claims 1
- WJEOLQLKVOPQFV-UHFFFAOYSA-N masitinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3SC=C(N=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 WJEOLQLKVOPQFV-UHFFFAOYSA-N 0.000 claims 1
- SNHCRNMVYDHVDT-UHFFFAOYSA-N n-(4-methoxyphenyl)-n,2-dimethylquinazolin-4-amine Chemical compound C1=CC(OC)=CC=C1N(C)C1=NC(C)=NC2=CC=CC=C12 SNHCRNMVYDHVDT-UHFFFAOYSA-N 0.000 claims 1
- 210000004498 neuroglial cell Anatomy 0.000 claims 1
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims 1
- 229960001346 nilotinib Drugs 0.000 claims 1
- 238000010606 normalization Methods 0.000 claims 1
- 229960000435 oblimersen Drugs 0.000 claims 1
- MIMNFCVQODTQDP-NDLVEFNKSA-N oblimersen Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](COP(S)(=O)O[C@@H]2[C@H](O[C@H](C2)N2C3=NC=NC(N)=C3N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=NC=NC(N)=C3N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)CO)[C@@H](O)C1 MIMNFCVQODTQDP-NDLVEFNKSA-N 0.000 claims 1
- 230000003518 presynaptic effect Effects 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 229960003787 sorafenib Drugs 0.000 claims 1
- 229960004066 trametinib Drugs 0.000 claims 1
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical compound CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 claims 1
- 229950007217 tremelimumab Drugs 0.000 claims 1
- YBZSGIWIPOUSHY-UHFFFAOYSA-N troriluzole Chemical compound NCC(=O)NCC(N(CC(NC=1SC2=C(N=1)C=CC(=C2)OC(F)(F)F)=O)C)=O YBZSGIWIPOUSHY-UHFFFAOYSA-N 0.000 claims 1
- 229960003862 vemurafenib Drugs 0.000 claims 1
- 102100040678 Programmed cell death protein 1 Human genes 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 239000000203 mixture Substances 0.000 description 5
- 102100034458 Hepatitis A virus cellular receptor 2 Human genes 0.000 description 4
- 101001137987 Homo sapiens Lymphocyte activation gene 3 protein Proteins 0.000 description 4
- 102100029822 B- and T-lymphocyte attenuator Human genes 0.000 description 2
- 102100039498 Cytotoxic T-lymphocyte protein 4 Human genes 0.000 description 2
- 102100031351 Galectin-9 Human genes 0.000 description 2
- 101710083479 Hepatitis A virus cellular receptor 2 homolog Proteins 0.000 description 2
- 101001068133 Homo sapiens Hepatitis A virus cellular receptor 2 Proteins 0.000 description 2
- 102100034980 ICOS ligand Human genes 0.000 description 2
- 102000017578 LAG3 Human genes 0.000 description 2
- 102100020862 Lymphocyte activation gene 3 protein Human genes 0.000 description 2
- 102000012220 Member 14 Tumor Necrosis Factor Receptors Human genes 0.000 description 2
- 108010061593 Member 14 Tumor Necrosis Factor Receptors Proteins 0.000 description 2
- 101710089372 Programmed cell death protein 1 Proteins 0.000 description 2
- 102000004887 Transforming Growth Factor beta Human genes 0.000 description 2
- 108090001012 Transforming Growth Factor beta Proteins 0.000 description 2
- 210000003169 central nervous system Anatomy 0.000 description 2
- 238000009169 immunotherapy Methods 0.000 description 2
- 239000003446 ligand Substances 0.000 description 2
- 102000007471 Adenosine A2A receptor Human genes 0.000 description 1
- 108010085277 Adenosine A2A receptor Proteins 0.000 description 1
- 101150051188 Adora2a gene Proteins 0.000 description 1
- 101710144268 B- and T-lymphocyte attenuator Proteins 0.000 description 1
- 102100027207 CD27 antigen Human genes 0.000 description 1
- 108010021064 CTLA-4 Antigen Proteins 0.000 description 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 description 1
- 208000002339 Frontotemporal Lobar Degeneration Diseases 0.000 description 1
- 101710121810 Galectin-9 Proteins 0.000 description 1
- 101100229077 Gallus gallus GAL9 gene Proteins 0.000 description 1
- 101000864344 Homo sapiens B- and T-lymphocyte attenuator Proteins 0.000 description 1
- 101000914511 Homo sapiens CD27 antigen Proteins 0.000 description 1
- 101000889276 Homo sapiens Cytotoxic T-lymphocyte protein 4 Proteins 0.000 description 1
- 101001019455 Homo sapiens ICOS ligand Proteins 0.000 description 1
- 101710093458 ICOS ligand Proteins 0.000 description 1
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 description 1
- 108060003951 Immunoglobulin Proteins 0.000 description 1
- 102000015696 Interleukins Human genes 0.000 description 1
- 108010063738 Interleukins Proteins 0.000 description 1
- 102000002698 KIR Receptors Human genes 0.000 description 1
- 108010043610 KIR Receptors Proteins 0.000 description 1
- 208000027520 Somatoform disease Diseases 0.000 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- 230000019771 cognition Effects 0.000 description 1
- 230000000139 costimulatory effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000008451 emotion Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 description 1
- 102000018358 immunoglobulin Human genes 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 208000027753 pain disease Diseases 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 description 1
- 229960005486 vaccine Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562127684P | 2015-03-03 | 2015-03-03 | |
| US62/127,684 | 2015-03-03 | ||
| PCT/US2016/019787 WO2016140879A1 (en) | 2015-03-03 | 2016-02-26 | Riluzole prodrugs and their use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020080638A Division JP7012117B2 (ja) | 2015-03-03 | 2020-04-30 | リルゾールプロドラッグおよびそれらの使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018508525A JP2018508525A (ja) | 2018-03-29 |
| JP2018508525A5 true JP2018508525A5 (enExample) | 2019-01-31 |
| JP6700293B2 JP6700293B2 (ja) | 2020-05-27 |
Family
ID=56848452
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017546176A Active JP6700293B2 (ja) | 2015-03-03 | 2016-02-26 | リルゾールプロドラッグおよびそれらの使用 |
| JP2020080638A Active JP7012117B2 (ja) | 2015-03-03 | 2020-04-30 | リルゾールプロドラッグおよびそれらの使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020080638A Active JP7012117B2 (ja) | 2015-03-03 | 2020-04-30 | リルゾールプロドラッグおよびそれらの使用 |
Country Status (24)
| Country | Link |
|---|---|
| US (10) | US10639298B2 (enExample) |
| EP (2) | EP3265448B1 (enExample) |
| JP (2) | JP6700293B2 (enExample) |
| KR (2) | KR20230147746A (enExample) |
| CN (1) | CN107567438B (enExample) |
| AU (3) | AU2016226463B2 (enExample) |
| BR (1) | BR112017018832B1 (enExample) |
| CA (1) | CA2978158C (enExample) |
| CY (1) | CY1125112T1 (enExample) |
| DK (1) | DK3265448T3 (enExample) |
| EA (1) | EA034759B1 (enExample) |
| ES (1) | ES2905318T3 (enExample) |
| HR (1) | HRP20220208T1 (enExample) |
| HU (1) | HUE058204T2 (enExample) |
| IL (2) | IL253989B (enExample) |
| LT (1) | LT3265448T (enExample) |
| MX (1) | MX380828B (enExample) |
| PH (2) | PH12021550250A1 (enExample) |
| PL (1) | PL3265448T3 (enExample) |
| PT (1) | PT3265448T (enExample) |
| RS (1) | RS62915B1 (enExample) |
| SG (2) | SG11201706831RA (enExample) |
| SI (1) | SI3265448T1 (enExample) |
| WO (2) | WO2016140878A2 (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013138753A1 (en) | 2012-03-16 | 2013-09-19 | Fox Chase Chemical Diversity Center, Inc. | Prodrugs of riluzole and their method of use |
| HUE046869T2 (hu) * | 2014-11-21 | 2020-04-28 | Biohaven Therapeutics Ltd | Riluzol szublingvális formulációja |
| US11911369B2 (en) * | 2015-03-03 | 2024-02-27 | Biohaven Therapeutics Ltd. | Prodrugs of riluzole and their method of use |
| US12295942B2 (en) | 2015-03-03 | 2025-05-13 | Biohaven Therapeutics Ltd. | Riluzole prodrugs and their use |
| US10639298B2 (en) * | 2015-03-03 | 2020-05-05 | Biohaven Therapeutics Ltd. | Prodrugs of riluzole and their method of use |
| JP2017061430A (ja) * | 2015-09-25 | 2017-03-30 | 芳男 ▲浜▼田 | 新規なプロドラッグ |
| IL292302B2 (en) * | 2016-05-20 | 2023-10-01 | Biohaven Pharm Holding Co Ltd | Use of glutamate modulating factors in cancer immunotherapy |
| US12029731B2 (en) | 2016-08-10 | 2024-07-09 | Biohaven Therapeutics Ltd. | Acyl benzo[d]thiazol-2-amine and their methods of use |
| MY194462A (en) * | 2016-11-25 | 2022-11-30 | Genuv Inc | Composition for Promoting Differentiation of and Protecting Neural Stem Cells and Method for Inducing Neural Regeneration using same |
| CN110291089B (zh) | 2017-01-17 | 2022-05-27 | 海帕瑞吉尼克斯股份有限公司 | 用于促进肝再生或者减少或预防肝细胞死亡的蛋白激酶抑制剂 |
| US12201618B2 (en) * | 2017-01-18 | 2025-01-21 | Biohaven Therapeutics Ltd. | Use of riluzole prodrugs to treat Alzheimer's disease |
| US20180207138A1 (en) | 2017-01-23 | 2018-07-26 | Cadent Therapeutics, Inc. | Methods for the treatment of tremors by positive modulation of sk channels |
| US11014943B2 (en) * | 2017-02-28 | 2021-05-25 | Chia Tai Tianqing Pharmaceutical Group Go., Ltd. | Azetidine derivative |
| CN107021959A (zh) * | 2017-05-02 | 2017-08-08 | 青岛科技大学 | 一类新型吲哚衍生物及其体外抗肿瘤活性 |
| MD3706739T2 (ro) * | 2017-11-12 | 2025-02-28 | Biohaven Therapeutics Ltd | Utilizarea promedicamentelor de riluzol pentru tratarea ataxiei |
| US12161633B2 (en) * | 2018-07-22 | 2024-12-10 | Biohaven Therapeutics Ltd. | Use of riluzole prodrugs to treat alzheimer's disease |
| KR20210045423A (ko) * | 2018-08-16 | 2021-04-26 | 바이오하벤 테라퓨틱스 리미티드 | 질환 치료를 위한 릴루졸 경구 붕해 정제의 용도 |
| GB201818651D0 (en) * | 2018-11-15 | 2019-01-02 | Univ Sheffield | Compounds |
| WO2021072140A1 (en) * | 2019-10-10 | 2021-04-15 | Biohaven Therapeutics Ltd. | Prodrugs of myeloperoxidase inhibitors |
| CN114981298B (zh) | 2019-12-12 | 2024-08-20 | 听治疗有限责任公司 | 用于预防和治疗听力损失的组合物和方法 |
| BR112022025901A2 (pt) * | 2020-06-24 | 2023-01-10 | Biohaven Therapeutics Ltd | Composições e métodos para tratar transtorno obsessivo-compulsivo |
| US11672761B2 (en) | 2020-11-16 | 2023-06-13 | Orcosa Inc. | Rapidly infusing platform and compositions for therapeutic treatment in humans |
| EP4243796A4 (en) | 2020-11-16 | 2025-01-22 | Orcosa Inc. | IMPROVED USE OF CANNABINOIDS IN THE TREATMENT OF EPILEPSY |
| WO2022155564A1 (en) * | 2021-01-18 | 2022-07-21 | Biohaven Therapeutics Ltd. | Use of riluzole prodrugs to treat alzheimer's disease |
| EP4294392A4 (en) * | 2021-02-22 | 2025-06-25 | Yale University, Inc. | TARGETED BIFUNCTIONAL DEGRADING AGENTS AND METHODS OF USE THEREOF |
| KR102785404B1 (ko) | 2022-08-19 | 2025-03-21 | 부산대학교 산학협력단 | 리루졸 유도체 및 이를 유효성분으로 포함하는 대장 표적성 염증성 장질환 예방 또는 치료용 조성물 |
| CN114344297B (zh) * | 2022-03-01 | 2024-05-14 | 暨南大学 | 利鲁唑在治疗少精症中的应用 |
| CA3258423A1 (en) * | 2022-06-26 | 2024-01-04 | Biohaven Therapeutics Ltd. | METHODS OF TREATING A GLIOBLASTOMA WITH RILUZOLE PROMEDICINAL PRODUCTS |
| CN118085016B (zh) * | 2024-04-24 | 2024-07-30 | 天津卡普希科技有限公司 | 一种d-苯甘氨酰-甘氨酸的制备方法 |
| HUP2400349A1 (hu) * | 2024-07-05 | 2026-01-28 | Egis Gyógyszergyár Zrt. | Troriluzole-hidroklorid-sók |
| WO2026078657A1 (en) | 2024-10-10 | 2026-04-16 | Biohaven Therapeutics Ltd. | Prodrugs of riluzole |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999023083A1 (en) * | 1997-11-05 | 1999-05-14 | Mitsubishi Chemical Corporation | Novel alkylamino derivatives |
| FR2774592B1 (fr) * | 1998-02-06 | 2000-03-17 | Rhone Poulenc Rorer Sa | Application du 2-amino-6-trifluoromethoxybenzothiazole pour la prevention ou le traitement des dysfonctionnements du cervelet |
| WO2002100399A1 (en) * | 2001-06-12 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| WO2005037845A1 (en) * | 2003-10-17 | 2005-04-28 | Rigel Pharmaceuticals, Inc. | Benzothiazole and thiazole[5,5-b] pyridine compositions and their use as ubiquitin ligase inhibitors |
| AR050258A1 (es) * | 2004-07-21 | 2006-10-11 | Mitsui Chemicals Inc | Derivado de diamina, proceso de la preparacion de este, y fungicida que contiene el derivado de diamina como ingrediente activo |
| EP2201963B1 (en) | 2005-04-05 | 2016-01-27 | Yale University | Glutamate modulating agents in the treatment of mental disorders |
| FR2885129B1 (fr) * | 2005-04-29 | 2007-06-15 | Proskelia Sas | Nouveaux derives de l'ureee substituee parun thiazole ou benzothiazole, leur procede de preparation, leur application a titre de medicaments, les compositions pharmaceutiques les renfermant et utilisation. |
| WO2013138753A1 (en) * | 2012-03-16 | 2013-09-19 | Fox Chase Chemical Diversity Center, Inc. | Prodrugs of riluzole and their method of use |
| WO2013192610A2 (en) * | 2012-06-23 | 2013-12-27 | Fox Chase Chemical Diversity Center, Inc. | Pro-drugs of riluzole and their method of use for the treatment of amyotrophic lateral sclerosis |
| US11911369B2 (en) * | 2015-03-03 | 2024-02-27 | Biohaven Therapeutics Ltd. | Prodrugs of riluzole and their method of use |
| US10639298B2 (en) * | 2015-03-03 | 2020-05-05 | Biohaven Therapeutics Ltd. | Prodrugs of riluzole and their method of use |
| US12295942B2 (en) * | 2015-03-03 | 2025-05-13 | Biohaven Therapeutics Ltd. | Riluzole prodrugs and their use |
| JP7110094B2 (ja) | 2015-11-19 | 2022-08-01 | バイオヘイブン・ファーマシューティカル・ホールディング・カンパニー・リミテッド | 医薬化合物のアミンプロドラッグ |
| IL292302B2 (en) * | 2016-05-20 | 2023-10-01 | Biohaven Pharm Holding Co Ltd | Use of glutamate modulating factors in cancer immunotherapy |
| US12029731B2 (en) | 2016-08-10 | 2024-07-09 | Biohaven Therapeutics Ltd. | Acyl benzo[d]thiazol-2-amine and their methods of use |
| MD3706739T2 (ro) | 2017-11-12 | 2025-02-28 | Biohaven Therapeutics Ltd | Utilizarea promedicamentelor de riluzol pentru tratarea ataxiei |
-
2016
- 2016-02-26 US US15/549,152 patent/US10639298B2/en active Active
- 2016-02-26 EA EA201791951A patent/EA034759B1/ru unknown
- 2016-02-26 RS RS20220149A patent/RS62915B1/sr unknown
- 2016-02-26 DK DK16759303.7T patent/DK3265448T3/da active
- 2016-02-26 ES ES16759303T patent/ES2905318T3/es active Active
- 2016-02-26 WO PCT/US2016/019773 patent/WO2016140878A2/en not_active Ceased
- 2016-02-26 MX MX2017011196A patent/MX380828B/es unknown
- 2016-02-26 KR KR1020237034132A patent/KR20230147746A/ko not_active Ceased
- 2016-02-26 BR BR112017018832-5A patent/BR112017018832B1/pt active IP Right Grant
- 2016-02-26 EP EP16759303.7A patent/EP3265448B1/en active Active
- 2016-02-26 SG SG11201706831RA patent/SG11201706831RA/en unknown
- 2016-02-26 HU HUE16759303A patent/HUE058204T2/hu unknown
- 2016-02-26 HR HRP20220208TT patent/HRP20220208T1/hr unknown
- 2016-02-26 CA CA2978158A patent/CA2978158C/en active Active
- 2016-02-26 KR KR1020177027618A patent/KR102587894B1/ko active Active
- 2016-02-26 JP JP2017546176A patent/JP6700293B2/ja active Active
- 2016-02-26 PL PL16759303T patent/PL3265448T3/pl unknown
- 2016-02-26 SG SG10201908354V patent/SG10201908354VA/en unknown
- 2016-02-26 WO PCT/US2016/019787 patent/WO2016140879A1/en not_active Ceased
- 2016-02-26 LT LTEPPCT/US2016/019787T patent/LT3265448T/lt unknown
- 2016-02-26 AU AU2016226463A patent/AU2016226463B2/en active Active
- 2016-02-26 PT PT167593037T patent/PT3265448T/pt unknown
- 2016-02-26 EP EP21209037.7A patent/EP4011870A1/en active Pending
- 2016-02-26 SI SI201631457T patent/SI3265448T1/sl unknown
- 2016-02-26 PH PH1/2021/550250A patent/PH12021550250A1/en unknown
- 2016-02-26 CN CN201680025374.6A patent/CN107567438B/zh active Active
- 2016-02-26 US US15/549,154 patent/US10485791B2/en active Active
-
2017
- 2017-08-14 IL IL253989A patent/IL253989B/en active IP Right Grant
- 2017-08-31 PH PH12017501576A patent/PH12017501576B1/en unknown
-
2019
- 2019-06-24 US US16/449,948 patent/US10905681B2/en active Active
- 2019-11-20 US US16/689,150 patent/US11052070B2/en active Active
-
2020
- 2020-04-30 JP JP2020080638A patent/JP7012117B2/ja active Active
- 2020-09-15 AU AU2020233650A patent/AU2020233650B2/en active Active
- 2020-10-15 IL IL278080A patent/IL278080B/en unknown
-
2021
- 2021-02-01 US US17/164,654 patent/US12005046B2/en active Active
- 2021-07-05 US US17/367,484 patent/US12213965B2/en active Active
-
2022
- 2022-03-24 CY CY20221100236T patent/CY1125112T1/el unknown
- 2022-03-30 AU AU2022202163A patent/AU2022202163B2/en active Active
-
2023
- 2023-07-29 US US18/361,836 patent/US20240091205A1/en not_active Abandoned
- 2023-07-29 US US18/361,837 patent/US12005047B2/en active Active
- 2023-07-29 US US18/361,838 patent/US12472165B2/en active Active
-
2025
- 2025-10-16 US US19/359,922 patent/US20260041673A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI827646B (zh) | Ptpn11抑制劑 | |
| ES2902360T3 (es) | Inhibidores de PD-1/PD-L1 | |
| JP7373170B2 (ja) | ジヒドロオロト酸デヒドロゲナーゼ阻害のための方法及び組成物 | |
| KR102891799B1 (ko) | 암 및 감염 치료에 사용하기 위한 면역 체크포인트 조절 인자의 억제제 | |
| EP4395775A1 (en) | Cyclopenta[4,5]furo[3,2-c]pyridine derivatives as ras inhibitors for use in the treatment of hyperproliferative diseases or genetic disorders | |
| TWI786322B (zh) | 免疫療法與ｍｄｍ２抑制劑的組合及其用途 | |
| TW202016081A (zh) | 人類ｓｔｉｎｇ之小分子調節劑、結合物及治療應用 | |
| KR20200005662A (ko) | 암을 치료하기 위한 조합 요법 | |
| CA2959564A1 (en) | Anti-pd-l1 conjugates for treating tumors | |
| JP2025185043A (ja) | 癌を治療するための免疫調節剤と組み合わせた低酸素活性化型プロドラッグの投与 | |
| JP7028765B2 (ja) | ベンズアミドおよび活性化合物組成物および使用方法 | |
| CA2988126A1 (en) | Compositions comprising a cancer stemness inhibitor and an immunotherapeutic agent for use in treating cancer | |
| JP2020532539A (ja) | 抗癌剤としての環状ジヌクレオチド | |
| JP2020527173A5 (enExample) | ||
| KR20190003750A (ko) | 암을 치료하기 위한 1-테트라히드로피라닐카르보닐-2,3-디히드로-1h-인돌 화합물 | |
| TWI829329B (zh) | 組蛋白去乙醯化酶6和熱休克蛋白90之雙重抑制劑 | |
| Vaisitti et al. | Vls-101 is a novel therapeutic antibody-drug conjugate (ADC) targeting receptor tyrosine kinase-like orphan receptor 1 (ROR1) in Richter's syndrome (RS) | |
| JP2023105077A (ja) | 標的治療剤を含む併用療法 | |
| Gilad et al. | Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma | |
| JP7080234B2 (ja) | ベンズアミドおよび活性化合物組成物および使用方法 | |
| JP7636322B2 (ja) | 癌を処置するためのマドラシン誘導体化合物、組成物およびこれらの使用 | |
| EP3236961B1 (en) | Pharmaceutical composition for preventing or treating cancer | |
| EP3609878B1 (en) | Compounds, composition and uses thereof for treating cancer | |
| US20250250280A1 (en) | Nitrogen-containing derivatives of narasin, synthesis and uses thereof | |
| Gregor et al. | P-01.15 Prostanoid-insensitive chimeric antigen receptor modified T cells mediate therapeutic efficacy in solid cancer models |