JPWO2019197630A5 - - Google Patents
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- JPWO2019197630A5 JPWO2019197630A5 JP2020555851A JP2020555851A JPWO2019197630A5 JP WO2019197630 A5 JPWO2019197630 A5 JP WO2019197630A5 JP 2020555851 A JP2020555851 A JP 2020555851A JP 2020555851 A JP2020555851 A JP 2020555851A JP WO2019197630 A5 JPWO2019197630 A5 JP WO2019197630A5
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- JP
- Japan
- Prior art keywords
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- pharmaceutically acceptable
- acceptable salt
- Prior art date
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- -1 Ibzilast Chemical compound 0.000 claims 28
- 239000000203 mixture Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000011780 sodium chloride Substances 0.000 claims 10
- AAOVKJBEBIDNHE-UHFFFAOYSA-N Diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 claims 8
- MLKXDPUZXIRXEP-MFOYZWKCSA-N Sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 claims 7
- 229960000894 Sulindac Drugs 0.000 claims 7
- 229960003529 diazepam Drugs 0.000 claims 7
- KZNIFHPLKGYRTM-UHFFFAOYSA-N Apigenin Chemical compound C1=CC(O)=CC=C1C1=CC(=O)C2=C(O)C=C(O)C=C2O1 KZNIFHPLKGYRTM-UHFFFAOYSA-N 0.000 claims 6
- XUSYGBPHQBWGAD-PJSUUKDQSA-N Carnosol Chemical compound CC([C@@H]1C2)(C)CCC[C@@]11C(=O)O[C@@H]2C2=C1C(O)=C(O)C(C(C)C)=C2 XUSYGBPHQBWGAD-PJSUUKDQSA-N 0.000 claims 6
- GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims 6
- IQPNAANSBPBGFQ-UHFFFAOYSA-N Luteolin Chemical compound C=1C(O)=CC(O)=C(C(C=2)=O)C=1OC=2C1=CC=C(O)C(O)=C1 IQPNAANSBPBGFQ-UHFFFAOYSA-N 0.000 claims 6
- LUKBXSAWLPMMSZ-OWOJBTEDSA-N Resveratrol Natural products C1=CC(O)=CC=C1\C=C\C1=CC(O)=CC(O)=C1 LUKBXSAWLPMMSZ-OWOJBTEDSA-N 0.000 claims 6
- QRYRORQUOLYVBU-VBKZILBWSA-N Salvin Chemical compound CC([C@@H]1CC2)(C)CCC[C@]1(C(O)=O)C1=C2C=C(C(C)C)C(O)=C1O QRYRORQUOLYVBU-VBKZILBWSA-N 0.000 claims 6
- XOAAWQZATWQOTB-UHFFFAOYSA-N Taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- DUGOZIWVEXMGBE-UHFFFAOYSA-N Adhd patch Chemical compound C=1C=CC=CC=1C(C(=O)OC)C1CCCCN1 DUGOZIWVEXMGBE-UHFFFAOYSA-N 0.000 claims 5
- 208000001914 Fragile X Syndrome Diseases 0.000 claims 5
- 108009000484 Fragile X Syndrome Proteins 0.000 claims 5
- 229960001344 Methylphenidate Drugs 0.000 claims 5
- DDBREPKUVSBGFI-UHFFFAOYSA-N Phenobarbital Chemical compound C=1C=CC=CC=1C1(CC)C(=O)NC(=O)NC1=O DDBREPKUVSBGFI-UHFFFAOYSA-N 0.000 claims 5
- 229960002695 Phenobarbital Drugs 0.000 claims 5
- VGKDLMBJGBXTGI-SJCJKPOMSA-N Sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 claims 5
- 229940079593 drugs Drugs 0.000 claims 5
- YQEZLKZALYSWHR-UHFFFAOYSA-N Calypsol Chemical compound C=1C=CC=C(Cl)C=1C1(NC)CCCCC1=O YQEZLKZALYSWHR-UHFFFAOYSA-N 0.000 claims 4
- 229960002073 Sertraline Drugs 0.000 claims 4
- HJMQDJPMQIHLPB-UHFFFAOYSA-N Zardaverine Chemical compound C1=C(OC(F)F)C(OC)=CC(C2=NNC(=O)C=C2)=C1 HJMQDJPMQIHLPB-UHFFFAOYSA-N 0.000 claims 4
- 229950001080 Zardaverine Drugs 0.000 claims 4
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims 4
- PHIQHXFUZVPYII-ZCFIWIBFSA-N (R)-carnitine Chemical compound C[N+](C)(C)C[C@H](O)CC([O-])=O PHIQHXFUZVPYII-ZCFIWIBFSA-N 0.000 claims 3
- GSNOZLZNQMLSKJ-UHFFFAOYSA-N 7-(Diethylamino)-5-methyl-s-triazolo(1,5-a)pyrimidine Chemical compound CCN(CC)C1=CC(C)=NC2=NC=NN12 GSNOZLZNQMLSKJ-UHFFFAOYSA-N 0.000 claims 3
- JHCFQXNWYDLBOG-UHFFFAOYSA-N 8-cyclopropyl-3-[2-(3-fluorophenyl)ethyl]-7H-[1,3]oxazino[6,5-g][1,2,3]benzotriazine-4,9-dione Chemical compound FC1=CC=CC(CCN2C(C3=CC=4OCN(C(=O)C=4C=C3N=N2)C2CC2)=O)=C1 JHCFQXNWYDLBOG-UHFFFAOYSA-N 0.000 claims 3
- 229960001009 Acetylcarnitine Drugs 0.000 claims 3
- RDHQFKQIGNGIED-MRVPVSSYSA-N Acetylcarnitine Chemical compound CC(=O)O[C@H](CC([O-])=O)C[N+](C)(C)C RDHQFKQIGNGIED-MRVPVSSYSA-N 0.000 claims 3
- 229940117893 Apigenin Drugs 0.000 claims 3
- 229960002781 Bisoprolol Drugs 0.000 claims 3
- VHYCDWMUTMEGQY-UHFFFAOYSA-N Bisoprolol Chemical compound CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1 VHYCDWMUTMEGQY-UHFFFAOYSA-N 0.000 claims 3
- FFGPTBGBLSHEPO-UHFFFAOYSA-N Carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 claims 3
- BLMPQMFVWMYDKT-NZTKNTHTSA-N Carfilzomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)[C@]1(C)OC1)NC(=O)CN1CCOCC1)CC1=CC=CC=C1 BLMPQMFVWMYDKT-NZTKNTHTSA-N 0.000 claims 3
- DUGOZIWVEXMGBE-CHWSQXEVSA-N Dexmethylphenidate Chemical compound C([C@@H]1[C@H](C(=O)OC)C=2C=CC=CC=2)CCCN1 DUGOZIWVEXMGBE-CHWSQXEVSA-N 0.000 claims 3
- 229960003722 Doxycycline Drugs 0.000 claims 3
- XQTWDDCIUJNLTR-CVHRZJFOSA-N Doxycycline Chemical compound O.O=C1C2=C(O)C=CC=C2[C@H](C)[C@@H]2C1=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@@H]1[C@H]2O XQTWDDCIUJNLTR-CVHRZJFOSA-N 0.000 claims 3
- SPIUTQOUKAMGCX-UHFFFAOYSA-N Flavoxate Chemical compound C1=CC=C2C(=O)C(C)=C(C=3C=CC=CC=3)OC2=C1C(=O)OCCN1CCCCC1 SPIUTQOUKAMGCX-UHFFFAOYSA-N 0.000 claims 3
- 229960000855 Flavoxate Drugs 0.000 claims 3
- 229950006567 GANAXOLONE Drugs 0.000 claims 3
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapen Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 3
- ZXRVKCBLGJOCEE-UHFFFAOYSA-N Gaboxadol Chemical compound C1NCCC2=C1ONC2=O ZXRVKCBLGJOCEE-UHFFFAOYSA-N 0.000 claims 3
- 229950004346 Gaboxadol Drugs 0.000 claims 3
- PGTVWKLGGCQMBR-FLBATMFCSA-N Ganaxolone Chemical compound C([C@@H]1CC2)[C@](C)(O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 PGTVWKLGGCQMBR-FLBATMFCSA-N 0.000 claims 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 3
- KTUFNOKKBVMGRW-UHFFFAOYSA-N Imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 3
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 3
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 3
- IUBSYMUCCVWXPE-UHFFFAOYSA-N Metoprolol Chemical compound COCCC1=CC=C(OCC(O)CNC(C)C)C=C1 IUBSYMUCCVWXPE-UHFFFAOYSA-N 0.000 claims 3
- 229960002237 Metoprolol Drugs 0.000 claims 3
- 229960004023 Minocycline Drugs 0.000 claims 3
- DYKFCLLONBREIL-KVUCHLLUSA-N Minocycline Chemical compound C([C@H]1C2)C3=C(N(C)C)C=CC(O)=C3C(=O)C1=C(O)[C@@]1(O)[C@@H]2[C@H](N(C)C)C(O)=C(C(N)=O)C1=O DYKFCLLONBREIL-KVUCHLLUSA-N 0.000 claims 3
- XQYZDYMELSJDRZ-UHFFFAOYSA-N Papaverine Chemical compound C1=C(OC)C(OC)=CC=C1CC1=NC=CC2=CC(OC)=C(OC)C=C12 XQYZDYMELSJDRZ-UHFFFAOYSA-N 0.000 claims 3
- BYPFEZZEUUWMEJ-UHFFFAOYSA-N Pentoxifylline Chemical compound O=C1N(CCCCC(=O)C)C(=O)N(C)C2=C1N(C)C=N2 BYPFEZZEUUWMEJ-UHFFFAOYSA-N 0.000 claims 3
- ZULJGOSFKWFVRX-UHFFFAOYSA-N Pramiracetam Chemical compound CC(C)N(C(C)C)CCNC(=O)CN1CCCC1=O ZULJGOSFKWFVRX-UHFFFAOYSA-N 0.000 claims 3
- 229960003080 Taurine Drugs 0.000 claims 3
- 229960000363 Trapidil Drugs 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- 235000008714 apigenin Nutrition 0.000 claims 3
- 229960000623 carbamazepine Drugs 0.000 claims 3
- 229960002438 carfilzomib Drugs 0.000 claims 3
- 108010021331 carfilzomib Proteins 0.000 claims 3
- 235000004654 carnosol Nutrition 0.000 claims 3
- 229960001042 dexmethylphenidate Drugs 0.000 claims 3
- 229960002870 gabapentin Drugs 0.000 claims 3
- 229960002584 gefitinib Drugs 0.000 claims 3
- 229960002411 imatinib Drugs 0.000 claims 3
- 235000009498 luteolin Nutrition 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 229960001789 papaverine Drugs 0.000 claims 3
- 229960003389 pramiracetam Drugs 0.000 claims 3
- 229940016667 resveratrol Drugs 0.000 claims 3
- 235000021283 resveratrol Nutrition 0.000 claims 3
- WMBWREPUVVBILR-WIYYLYMNSA-N (-)-Epigallocatechin-3-o-gallate Chemical compound O([C@@H]1CC2=C(O)C=C(C=C2O[C@@H]1C=1C=C(O)C(O)=C(O)C=1)O)C(=O)C1=CC(O)=C(O)C(O)=C1 WMBWREPUVVBILR-WIYYLYMNSA-N 0.000 claims 2
- RBQOQRRFDPXAGN-UHFFFAOYSA-N 3-methyl-1-(5-oxohexyl)-7-propylpurine-2,6-dione Chemical compound CN1C(=O)N(CCCCC(C)=O)C(=O)C2=C1N=CN2CCC RBQOQRRFDPXAGN-UHFFFAOYSA-N 0.000 claims 2
- LFVPBERIVUNMGV-UHFFFAOYSA-N 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;hydrochloride Chemical compound Cl.C=1C=CC2=CN=CC=C2C=1S(=O)(=O)N1CCCNCC1 LFVPBERIVUNMGV-UHFFFAOYSA-N 0.000 claims 2
- 208000000044 Amnesia Diseases 0.000 claims 2
- 206010002855 Anxiety Diseases 0.000 claims 2
- 206010057666 Anxiety disease Diseases 0.000 claims 2
- IMOZEMNVLZVGJZ-QGZVFWFLSA-N Apremilast Chemical compound C1=C(OC)C(OCC)=CC([C@@H](CS(C)(=O)=O)N2C(C3=C(NC(C)=O)C=CC=C3C2=O)=O)=C1 IMOZEMNVLZVGJZ-QGZVFWFLSA-N 0.000 claims 2
- UPZWINBEAHDTLA-UHFFFAOYSA-N Basimglurant Chemical compound CC=1N(C=2C=CC(F)=CC=2)C(C)=NC=1C#CC1=CC=NC(Cl)=C1 UPZWINBEAHDTLA-UHFFFAOYSA-N 0.000 claims 2
- 229950000379 Basimglurant Drugs 0.000 claims 2
- ZVHNDZWQTBEVRY-UHFFFAOYSA-N CYT387 Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 ZVHNDZWQTBEVRY-UHFFFAOYSA-N 0.000 claims 2
- 229960004782 Chlordiazepoxide Drugs 0.000 claims 2
- ANTSCNMPPGJYLG-UHFFFAOYSA-N Chlordiazepoxide Chemical compound O=N=1CC(NC)=NC2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 ANTSCNMPPGJYLG-UHFFFAOYSA-N 0.000 claims 2
- ZJVFLBOZORBYFE-UHFFFAOYSA-N Ibudilast Chemical compound C1=CC=CC2=C(C(=O)C(C)C)C(C(C)C)=NN21 ZJVFLBOZORBYFE-UHFFFAOYSA-N 0.000 claims 2
- SGUAFYQXFOLMHL-UHFFFAOYSA-N Labetalol Chemical compound C=1C=C(O)C(C(N)=O)=CC=1C(O)CNC(C)CCC1=CC=CC=C1 SGUAFYQXFOLMHL-UHFFFAOYSA-N 0.000 claims 2
- PYZRQGJRPPTADH-UHFFFAOYSA-N Lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 claims 2
- HPHUVLMMVZITSG-ZCFIWIBFSA-N Levetiracetam Chemical compound CC[C@H](C(N)=O)N1CCCC1=O HPHUVLMMVZITSG-ZCFIWIBFSA-N 0.000 claims 2
- ZFPZEYHRWGMJCV-ZHALLVOQSA-N Mavoglurant Chemical compound C([C@]1(O)CCC[C@@H]2[C@H]1CCN2C(=O)OC)#CC1=CC=CC(C)=C1 ZFPZEYHRWGMJCV-ZHALLVOQSA-N 0.000 claims 2
- 229950007139 Mavoglurant Drugs 0.000 claims 2
- BUGYDGFZZOZRHP-UHFFFAOYSA-N Memantine Chemical compound C1C(C2)CC3(C)CC1(C)CC2(N)C3 BUGYDGFZZOZRHP-UHFFFAOYSA-N 0.000 claims 2
- MJVAVZPDRWSRRC-UHFFFAOYSA-N Menadione Chemical compound C1=CC=C2C(=O)C(C)=CC(=O)C2=C1 MJVAVZPDRWSRRC-UHFFFAOYSA-N 0.000 claims 2
- 229960003105 Metformin Drugs 0.000 claims 2
- 229950008814 Momelotinib Drugs 0.000 claims 2
- RDSACQWTXKSHJT-NSHDSACASA-N N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims 2
- 229940053207 Niacin Drugs 0.000 claims 2
- GMZVRMREEHBGGF-UHFFFAOYSA-N Piracetam Chemical compound NC(=O)CN1CCCC1=O GMZVRMREEHBGGF-UHFFFAOYSA-N 0.000 claims 2
- AQHHHDLHHXJYJD-UHFFFAOYSA-N Proprasylyt Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 claims 2
- 206010037211 Psychomotor hyperactivity Diseases 0.000 claims 2
- 229960001285 Quercetin Drugs 0.000 claims 2
- REFJWTPEDVJJIY-UHFFFAOYSA-N Quercetin Chemical compound C=1C(O)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC=C(O)C(O)=C1 REFJWTPEDVJJIY-UHFFFAOYSA-N 0.000 claims 2
- 229950008933 Refametinib Drugs 0.000 claims 2
- 241001122767 Theaceae Species 0.000 claims 2
- JICJBGPOMZQUBB-UHFFFAOYSA-N Tianeptine Chemical compound O=S1(=O)N(C)C2=CC=CC=C2C(NCCCCCCC(O)=O)C2=CC=C(Cl)C=C21 JICJBGPOMZQUBB-UHFFFAOYSA-N 0.000 claims 2
- PMJIHLSCWIDGMD-UHFFFAOYSA-N Tideglusib Chemical compound O=C1SN(C=2C3=CC=CC=C3C=CC=2)C(=O)N1CC1=CC=CC=C1 PMJIHLSCWIDGMD-UHFFFAOYSA-N 0.000 claims 2
- 229950005284 Tideglusib Drugs 0.000 claims 2
- KJADKKWYZYXHBB-XBWDGYHZSA-N Topiramic acid Chemical compound C1O[C@@]2(COS(N)(=O)=O)OC(C)(C)O[C@H]2[C@@H]2OC(C)(C)O[C@@H]21 KJADKKWYZYXHBB-XBWDGYHZSA-N 0.000 claims 2
- PJDFLNIOAUIZSL-UHFFFAOYSA-N Vigabatrin Chemical compound C=CC(N)CCC(O)=O PJDFLNIOAUIZSL-UHFFFAOYSA-N 0.000 claims 2
- 229940041603 Vitamin K 3 Drugs 0.000 claims 2
- AFCGFAGUEYAMAO-UHFFFAOYSA-N acamprosate Chemical compound CC(=O)NCCCS(O)(=O)=O AFCGFAGUEYAMAO-UHFFFAOYSA-N 0.000 claims 2
- 229960004047 acamprosate Drugs 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 229960001164 apremilast Drugs 0.000 claims 2
- 230000006399 behavior Effects 0.000 claims 2
- 229960001948 caffeine Drugs 0.000 claims 2
- 229940003092 decanoic acid Drugs 0.000 claims 2
- 230000001066 destructive Effects 0.000 claims 2
- 229940030275 epigallocatechin gallate Drugs 0.000 claims 2
- 229960002491 ibudilast Drugs 0.000 claims 2
- 229960003299 ketamine Drugs 0.000 claims 2
- 229960001632 labetalol Drugs 0.000 claims 2
- 229960001848 lamotrigine Drugs 0.000 claims 2
- 229960004002 levetiracetam Drugs 0.000 claims 2
- WHXSMMKQMYFTQS-UHFFFAOYSA-N lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims 2
- 229910052744 lithium Inorganic materials 0.000 claims 2
- 229960001078 lithium Drugs 0.000 claims 2
- 150000004668 long chain fatty acids Chemical class 0.000 claims 2
- 150000004667 medium chain fatty acids Chemical class 0.000 claims 2
- 229960005201 menadione Drugs 0.000 claims 2
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 2
- DFPAKSUCGFBDDF-UHFFFAOYSA-N nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims 2
- 229960003512 nicotinic acid Drugs 0.000 claims 2
- 235000001968 nicotinic acid Nutrition 0.000 claims 2
- 239000011664 nicotinic acid Substances 0.000 claims 2
- 229960004526 piracetam Drugs 0.000 claims 2
- 229960002934 propentofylline Drugs 0.000 claims 2
- 229930002344 quercetin Natural products 0.000 claims 2
- 235000005875 quercetin Nutrition 0.000 claims 2
- 229960005138 tianeptine Drugs 0.000 claims 2
- 229960004394 topiramate Drugs 0.000 claims 2
- 229960005318 vigabatrin Drugs 0.000 claims 2
- 235000012711 vitamin K3 Nutrition 0.000 claims 2
- 239000011652 vitamin K3 Substances 0.000 claims 2
- AYXYPKUFHZROOJ-ZETCQYMHSA-N (3S)-3-(aminomethyl)-5-methylhexanoic acid Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims 1
- FJLGEFLZQAZZCD-JUFISIKESA-N (3S,5R)-fluvastatin Chemical compound C12=CC=CC=C2N(C(C)C)C(\C=C\[C@H](O)C[C@H](O)CC(O)=O)=C1C1=CC=C(F)C=C1 FJLGEFLZQAZZCD-JUFISIKESA-N 0.000 claims 1
- NWXMGUDVXFXRIG-WESIUVDSSA-N (4S,4aS,5aS,6S,12aR)-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carboxamide Chemical compound C1=CC=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]4(O)C(=O)C3=C(O)C2=C1O NWXMGUDVXFXRIG-WESIUVDSSA-N 0.000 claims 1
- WEAJZXNPAWBCOA-INIZCTEOSA-N Avanafil Chemical compound C1=C(Cl)C(OC)=CC=C1CNC1=NC(N2[C@@H](CCC2)CO)=NC=C1C(=O)NCC1=NC=CC=N1 WEAJZXNPAWBCOA-INIZCTEOSA-N 0.000 claims 1
- KPYSYYIEGFHWSV-UHFFFAOYSA-N Baclofen Chemical compound OC(=O)CC(CN)C1=CC=C(Cl)C=C1 KPYSYYIEGFHWSV-UHFFFAOYSA-N 0.000 claims 1
- 229950011318 Cannabidiol Drugs 0.000 claims 1
- QHMBSVQNZZTUGM-ZWKOTPCHSA-N Cannabidiol Chemical compound OC1=CC(CCCCC)=CC(O)=C1[C@H]1[C@H](C(C)=C)CCC(C)=C1 QHMBSVQNZZTUGM-ZWKOTPCHSA-N 0.000 claims 1
- QHMBSVQNZZTUGM-MSOLQXFVSA-N Cannabidiol Natural products OC1=CC(CCCCC)=CC(O)=C1[C@@H]1[C@@H](C(C)=C)CCC(C)=C1 QHMBSVQNZZTUGM-MSOLQXFVSA-N 0.000 claims 1
- ADEBPBSSDYVVLD-UHFFFAOYSA-N Donepezil Chemical compound O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 claims 1
- OMFNSKIUKYOYRG-MOSHPQCFSA-N Drotaverine Chemical compound C1=C(OCC)C(OCC)=CC=C1\C=C/1C2=CC(OCC)=C(OCC)C=C2CCN\1 OMFNSKIUKYOYRG-MOSHPQCFSA-N 0.000 claims 1
- DIWRORZWFLOCLC-UHFFFAOYSA-N Lorazepam Chemical compound C12=CC(Cl)=CC=C2NC(=O)C(O)N=C1C1=CC=CC=C1Cl DIWRORZWFLOCLC-UHFFFAOYSA-N 0.000 claims 1
- VGYFMXBACGZSIL-MCBHFWOFSA-N Pitavastatin Chemical compound OC(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1 VGYFMXBACGZSIL-MCBHFWOFSA-N 0.000 claims 1
- 108010013381 Porins Proteins 0.000 claims 1
- 229960002965 Pravastatin Drugs 0.000 claims 1
- TUZYXOIXSAXUGO-PZAWKZKUSA-N Pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N Tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 claims 1
- 229960002180 Tetracycline Drugs 0.000 claims 1
- OFVLGDICTFRJMM-WESIUVDSSA-N Tetracycline Chemical compound C1=CC=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O OFVLGDICTFRJMM-WESIUVDSSA-N 0.000 claims 1
- 239000004098 Tetracycline Substances 0.000 claims 1
- 229960000438 Udenafil Drugs 0.000 claims 1
- IYFNEFQTYQPVOC-UHFFFAOYSA-N Udenafil Chemical compound C1=C(C=2NC=3C(CCC)=NN(C)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)NCCC1CCCN1C IYFNEFQTYQPVOC-UHFFFAOYSA-N 0.000 claims 1
- 229960000307 avanafil Drugs 0.000 claims 1
- 229960004362 clorazepate Drugs 0.000 claims 1
- XDDJGVMJFWAHJX-UHFFFAOYSA-M clorazepic acid anion Chemical compound C12=CC(Cl)=CC=C2NC(=O)C(C(=O)[O-])N=C1C1=CC=CC=C1 XDDJGVMJFWAHJX-UHFFFAOYSA-M 0.000 claims 1
- QCHSEDTUUKDTIG-UHFFFAOYSA-M dipotassium;7-chloro-2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepine-3-carboxylic acid;hydroxide Chemical compound [OH-].[K+].[K+].C12=CC(Cl)=CC=C2NC(=O)C(C(=O)O)N=C1C1=CC=CC=C1 QCHSEDTUUKDTIG-UHFFFAOYSA-M 0.000 claims 1
- 229960003530 donepezil Drugs 0.000 claims 1
- 229940017744 drotaverin Drugs 0.000 claims 1
- 229960002065 drotaverine Drugs 0.000 claims 1
- 229960003765 fluvastatin Drugs 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 229960004391 lorazepam Drugs 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 229960002797 pitavastatin Drugs 0.000 claims 1
- 102000007739 porin activity proteins Human genes 0.000 claims 1
- 229960001233 pregabalin Drugs 0.000 claims 1
- 201000010874 syndrome Diseases 0.000 claims 1
- 229960000835 tadalafil Drugs 0.000 claims 1
- 235000019364 tetracycline Nutrition 0.000 claims 1
Claims (17)
当該キットは脆弱X症候群の治療における同時使用、個別使用、または連続使用のための下記(i)および(ii)を含み;
当該組成物は脆弱X症候群の治療における使用のための下記(i)および(ii)を含み;および
当該方法は下記(i)および(ii)を同時に、個別に、または連続して患者に投与することを含む脆弱X症候群を治療する方法であり;
(i)スリンダクまたはその薬学的に許容可能な塩の少なくとも1回投与量;および
(ii)化合物Aまたはその薬学的に許容可能な塩の少なくとも1回投与量、
化合物Aは、以下のリストから選択される:
ミノサイクリン、ドキシサイクリン、ロバスタチン、メトホルミン、没食子酸エピガロカテキン(EGCG-緑茶抽出物)、リチウム、チデグルシブ(tideglusib)、ラモトリジン、アカンプロセート、ガナキソロン、バスイムグルラント、マボグルラント(mavoglurant)、メチルフェニデート、L-カルニチン、L-アセチルカルニチン、ザルダベリン(zardaverine)、イブジラスト、メトプロロール、ペンブトロール、ファスジル、カルバマゼピン、ミドスタウリン、シルデナフィル、タダラフィル、ガバペンチン、スチリペントール、ドネペジル、テトラサイクリン、カンナビジオール、クルクミン、シンバスタチン、アトルバスタチン、プラバスタチン、フルバスタチン、ロスバスタチン、ピタバスタチン、アピゲニン、テルミサルタン、中鎖脂肪酸および長鎖脂肪酸、インジルビン、プレガバリン、バクロフェン、アルバクロフェン、メマンチン、エスクロルビノール、フェノバム、リルゾール、クリサボロール、S-ロリプラム、アプレミラスト、シロミラスト、ロフルミラスト、ジピリダモール、ドロタベリン、プロペントフィリン、カフェイン、パパベリン、トラピジル、フラボキサート、アンレキサノクス(amlexano X)、ペントキシフィリン、プロパノロール(propanolol)、ピンドロール、アセブタロール(acebutalol)、ビソプロロール、カルベジロール、ラベタロール、メチプラノロール、オクスプレナロール(oxprenalol)、ピンドロール、テルタトロール、チモロール、トピリマート(topirimate)、チアネプチン、ケルセチン、ジスルフィラム、イマチニブ、ゲフィチニブ、セルメチニブ、レファメチニブ(refametinib)、フシジン酸、セルトラリン、ロラゼパム、フェノバルビタール、バルデナフィル、ウデナフィル、アバナフィル、ルキソリチニブ、モメロチニブ(momelotinib)、ボルテゾミブ、カルフィルゾミブ、カルノソール、リルゾール、ルテオリン、カルノシン酸、レスベラトロール、メチルフェニデート、メナジオン、タウリン、ナイアシン、クロラゼプ酸、ジアゼパムおよび他の「アゼパム」類薬剤、クロルジアゼポキシド、スタウロスポリン、ガボキサドール(gaboxadol)、プロガビド、ツルラムパトル(tulrampator)、ケタミン(ketamine)、デカン酸、ピラセタム、プラミラセタム、デクスメチルフェニデート、オグレミラスト、レベチラセタム、またはビガバトリン。 Kit, composition, or method: where
The kit includes the following (i) and (ii) for concurrent, individual or continuous use in the treatment of Fragile X Syndrome;
The composition comprises the following (i) and (ii) for use in the treatment of Fragile X Syndrome; and
The method is a method for treating fragile X syndrome, which comprises administering the following (i) and (ii) to a patient simultaneously, individually or continuously;
(i) At least a single dose of sulindac or a pharmaceutically acceptable salt thereof ; and
(ii) At least a single dose of Compound A or a pharmaceutically acceptable salt thereof ,
Compound A is selected from the list below:
Minocycrine, Doxycycline, Robastatin, Metoformin, Epigallocatechin gallate (EGCG-green tea extract), Lithium, Tideglusib, Lamotrigine, Acamprosate, Ganaxolone, Basimglurant, mavoglurant, Methylphenidate, L-Carnitine, L-Acetylcarnitine, Zardaverine, Ibzilast, Metoprolol, Pembutrol, Fasdil, Carbamazepine, Midstaurine, Syldenafil, Tadarapyl, Gabapentine, Stilipentol, Donepegil, Tetracyclin, Cambastatin, Clumvastatin, Cambastatin Statins, losbatatin, pitavastatin, apigenin, thermisartan, medium-chain and long-chain fatty acids, indilbin, pregavalin, baclophen, arbaclophen, memantin, eschlorbinol, phenovam, rilzole, chrysabolol, S-loliplum, apremilast, syromyllast, loflumirast. , Drotavelin, Propentophylline, Caffeine, Papaverin, Trapidil, Flavoxate, Amlexano X, Pentoxyphyllin, Propanolol, Pindrol, Acebutalol, Bisoprolol, Carbegallocatechin, Labetalol, Mechipranolol, Oxprena Roll (oxprenalol), pindrol, tertatrol, timorol, topirimate, tianeptine, kercetin, diazepam, imatinib, gefitinib, selmethinib, refametinib, fushidic acid, sertraline, lorazepate, phenobarbital Luxolitinib, momelotinib, voltezomib, carfilzomib, carnosol, rilzole, luteolin, carnosic acid, resveratrol, methylphenidechin, menadione, taurine, niacin, clorazepate, diazepam, diazepam and other "azepam" drugs. Taurosporin, gaboxadol, progavid, tulrampator, ke Ketamine, decanoic acid, piracetam, pramiracetam, dexmethylphenidate, ogremirast, levetiracetam, or vigabatrin.
a)脆弱X症候群を有する患者の治療のための医薬品の製造のための、スリンダクまたはその薬学的に許容可能な塩、ここで、前記患者は化合物Aまたはその薬学的に許容可能な塩を投与されている; a) Sulindac or a pharmaceutically acceptable salt thereof for the manufacture of a drug for the treatment of a patient with Fragile X Syndrome, wherein said patient administers Compound A or a pharmaceutically acceptable salt thereof. Has been;
b)脆弱X症候群を有する患者の治療のための医薬品の製造のための、化合物Aまたはその薬学的に許容可能な塩、ここで、前記患者は、スリンダクまたはその薬学的に許容可能な塩を投与されている;または b) Compound A or a pharmaceutically acceptable salt thereof for the manufacture of a drug for the treatment of a patient with Vulnerable X Syndrome, wherein said patient receives sulindac or a pharmaceutically acceptable salt thereof. Have been administered; or
c)脆弱X症候群の治療のための医薬品の製造のための、スリンダクまたはその薬学的に許容可能な塩、および化合物Aまたはその薬学的に許容可能な塩; c) Sulindac or its pharmaceutically acceptable salt for the manufacture of pharmaceuticals for the treatment of Fragile X Syndrome, and Compound A or its pharmaceutically acceptable salt;
化合物Aは、以下のリストから選択される: Compound A is selected from the list below:
ミノサイクリン、ドキシサイクリン、ロバスタチン、メトホルミン、没食子酸エピガロカテキン(EGCG-緑茶抽出物)、リチウム、チデグルシブ(tideglusib)、ラモトリジン、アカンプロセート、ガナキソロン、バスイムグルラント、マボグルラント(mavoglurant)、メチルフェニデート、L-カルニチン、L-アセチルカルニチン、ザルダベリン(zardaverine)、イブジラスト、メトプロロール、ペンブトロール、ファスジル、カルバマゼピン、ミドスタウリン、シルデナフィル、タダラフィル、ガバペンチン、スチリペントール、ガナキソロン、ドネペジル、テトラサイクリン、カンナビジオール、クルクミン、シンバスタチン、アトルバスタチン、プラバスタチン、フルバスタチン、ロスバスタチン、ピタバスタチン、アピゲニン、テルミサルタン、中鎖脂肪酸および長鎖脂肪酸、インジルビン、プレガバリン、バクロフェン、アルバクロフェン、メマンチン、エスクロルビノール、フェノバム、リルゾール、クリサボロール、S-ロリプラム、アプレミラスト、シロミラスト、ロフルミラスト、ジピリダモール、ドロタベリン、プロペントフィリン、カフェイン、パパベリン、トラピジル、フラボキサート、アンレキサノクス(amlexano X)、ペントキシフィリン、プロパノロール(propanolol)、ピンドロール、アセブタロール(acebutalol)、ビソプロロール、カルベジロール、ラベタロール、メチプラノロール、オクスプレナロール(oxprenalol)、ピンドロール、テルタトロール、チモロール、トピラマート、チアネプチン、ケルセチン、ジスルフィラム、イマチニブ、ゲフィチニブ、セルメチニブ、レファメチニブ(refametinib)、フシジン酸、セルトラリン、ロラゼパム、フェノバルビタール、バルデナフィル、ウデナフィル、アバナフィル、ルキソリチニブ、モメロチニブ(momelotinib)、ボルテゾミブ、カルフィルゾミブ、カルノソール、リルゾール、ルテオリン、カルノシン酸、レスベラトロール、メチルフェニデート、メナジオン、タウリン、ナイアシン、クロラゼプ酸、ジアゼパムおよび他の「アゼパム」類薬剤、クロルジアゼポキシド、スタウロスポリン、ガボキサドール(gaboxadol)、プロガビド、ツルラムパトル(tulrampator)、ケタミン(ketamine)、デカン酸、ピラセタム、プラミラセタム、デクスメチルフェニデート、オグレミラスト、レベチラセタム、またはビガバトリン。 Minocycrine, Doxycycline, Robastatin, Metoformin, Epigallocatechin gallate (EGCG-green tea extract), Lithium, Tideglusib, Lamotrigine, Acamprosate, Ganaxolone, Basimglurant, mavoglurant, Methylphenidate, L-Carnitine, L-Acetylcarnitine, Zardaverine, Ibzilast, Metoprolol, Pembutrol, Faszil, Carbamazepine, Midstaurine, Syldenafil, Tadarapyl, Gabapentine, Stilipentol, Ganaxolone, Donepegil , Fluvastatin, losvasstatin, pitabastatin, apigenin, thermisartan, medium-chain and long-chain fatty acids, indylbin, pregabalin, bacrophen, arbaclophen, memantin, eschlorbinol, phenovam, lylsole, chrysabolol, S-loliplum, apremirast, siromirast , Dipallocatechin, drotaverin, propentophilin, caffeine, papaverin, trapidil, flavoxate, amplexanox, pentoxyphyllin, propanolol, pindrol, acebutalol, bisoprolol, carbegallocatechin, labetalol Oxprenalol, Pindrol, Teltatrol, Timorol, Topiramart, Tianeptine, Kersetin, Diazepam, Imatinib, Gefitinib, Sermethinib, Refametinib, Fushidic acid, Sertralin, Lorazepate, Phenobarbital, Phenobarbital , Momelotinib, voltezomib, carfilzomib, carnosol, rilzole, luteolin, carnosic acid, resveratrol, methylphenidate, menadione, taurine, niacin, chlorazepam, diazepam, diazepam and other "azepam" drugs, chlordiazepoxide Porin, gaboxadol, progavid, tulrampator, ketamin (k) etamine), decanoic acid, piracetam, pramiracetam, dexmethylphenidate, ogremirast, levetiracetam, or vigabatrin.
(i)スリンダクまたはその薬学的に許容可能な塩の少なくとも1回投与量;および (i) At least a single dose of sulindac or a pharmaceutically acceptable salt thereof; and
(ii)化合物Aまたはその薬学的に許容可能な塩の少なくとも1回投与量; (ii) At least a single dose of Compound A or a pharmaceutically acceptable salt thereof;
化合物Aは、以下のリストから選択される: Compound A is selected from the list below:
ミノサイクリン、ドキシサイクリン、メトホルミン、リチウム、チデグルシブ(tideglusib)、ラモトリジン、アカンプロセート、ガナキソロン、バスイムグルラント、マボグルラント(mavoglurant)、メチルフェニデート、L-カルニチン、L-アセチルカルニチン、ザルダベリン(zardaverine)、イブジラスト、メトプロロール、ペンブトロール、ファスジル、カルバマゼピン、ミドスタウリン、シルデナフィル、タダラフィル、ガバペンチン、スチリペントール、ドネペジル、テトラサイクリン、シンバスタチン、アトルバスタチン、プラバスタチン、フルバスタチン、ロスバスタチン、ピタバスタチン、アピゲニン、テルミサルタン、インジルビン、プレガバリン、バクロフェン、アルバクロフェン、メマンチン、エスクロルビノール、フェノバム、リルゾール、クリサボロール、S-ロリプラム、アプレミラスト、シロミラスト、ロフルミラスト、ジピリダモール、ドロタベリン、プロペントフィリン、パパベリン、トラピジル、フラボキサート、アンレキサノクス(amlexano X)、ペントキシフィリン、プロパノロール(propanolol)、ピンドロール、アセブタロール(acebutalol)、ビソプロロール、カルベジロール、ラベタロール、メチプラノロール、オクスプレナロール(oxprenalol)、ピンドロール、テルタトロール、チモロール、トピラマート、チアネプチン、ケルセチン、ジスルフィラム、イマチニブ、ゲフィチニブ、セルメチニブ、レファメチニブ(refametinib)、フシジン酸、セルトラリン、ロラゼパム、フェノバルビタール、バルデナフィル、ウデナフィル、アバナフィル、ルキソリチニブ、モメロチニブ(momelotinib)、カルフィルゾミブ、カルノソール、リルゾール、ルテオリン、カルノシン酸、レスベラトロール、メチルフェニデート、タウリン、クロラゼプ酸、ジアゼパムおよび他の「アゼパム」類薬剤、クロルジアゼポキシド、スタウロスポリン、ガボキサドール(gaboxadol)、プロガビド、ツルラムパトル(tulrampator)、ケタミン(ketamine)、デカン酸、ピラセタム、プラミラセタム、デクスメチルフェニデート、オグレミラスト、レベチラセタム、またはビガバトリン。Minocycline, Doxycycline, Methylphenidate, L-Carnitine, L-Acetylcarnitine, Zardaverine, Zardaverine , Metoprolol, Pembutrol, Fasdil, Carbamazepine, Midstaurine, Syldenafil, Tadalafil, Gabapentin, Stilpentol, Donepezil, Tetracycline, Simbatatin, Atlvastatin, Pravastatin, Fulvastatin, Losvastatin, Pitabastatin, Apigenin, Termisartane, , Eschlorbinol, Phenobarbital, Lilzole, Chrysabolol, S-Loliplum, Apremilast, Shiromirast, Loflumirast, Diazepam, Dorotaberin, Propentophylline, Papaverin, Trapidil, Flavoxate, Amplexanox (amlexano X), Pentoxyphyllin Pindrol, acebutalol, bisoprolol, carbegilol, labetarol, methiplanolol, oxprenalol, pindrol, tertatrol, timorol, topiramart, thianeptin, kelsetin, dizepam, imatinib, gefitinib, selmethinib Fushidic acid, sertraline, lorazepam, phenobarbital, valdenafil, udenafil, avanafil, luxolitinib, momerotinib, carfilzomib, carnosol, lysole, luteolin, carnosic acid, resveratrol, methylphenidate, taurine, etc. "Azepam" drugs, chlordiazepoxide, staulospolin, gaboxador (gaboxadol), progavid, tulrampator, ketamine, decanoic acid, pyrasetam, pramiracetam, dexmethylphenidate, ogremylast, levetylphenidate, levetyrasetam.
The kit, composition, method, or use according to any one of claims 1 to 15, which is administered by parenteral administration, transdermal administration, sublingual administration, rectal administration, or inhalation administration.
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WO2012170430A1 (en) | 2011-06-06 | 2012-12-13 | Cardero Therapeutics, Inc. | Methods and compositions for treatment of mitochondrial toxicity |
CN103622941A (en) | 2013-12-16 | 2014-03-12 | 新乡医学院 | Application of sulindac in preparation of medicine for treating autism |
EP3624770A1 (en) | 2017-05-15 | 2020-03-25 | BioChemics, Inc. | Transdermally-delivered combination drug therapy for pain |
WO2019197632A1 (en) | 2018-04-13 | 2019-10-17 | Healx Limited | Treatment of fragile x syndrome |
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2019
- 2019-04-12 JP JP2020555851A patent/JP2021524837A/en active Pending
- 2019-04-12 MX MX2020010697A patent/MX2020010697A/en unknown
- 2019-04-12 EP EP19721206.1A patent/EP3765087A1/en not_active Withdrawn
- 2019-04-12 BR BR112020020908-2A patent/BR112020020908A2/en not_active IP Right Cessation
- 2019-04-12 US US16/383,037 patent/US11590093B2/en active Active
- 2019-04-12 CN CN201980025306.3A patent/CN111989120A/en active Pending
- 2019-04-12 CA CA3096759A patent/CA3096759A1/en active Pending
- 2019-04-12 WO PCT/EP2019/059470 patent/WO2019197630A1/en unknown
- 2019-04-12 AU AU2019250612A patent/AU2019250612A1/en not_active Abandoned
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2020
- 2020-10-09 ZA ZA2020/06298A patent/ZA202006298B/en unknown
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2022
- 2022-08-04 US US17/881,242 patent/US20230028262A1/en not_active Abandoned
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