JP2018504436A5 - - Google Patents

Info

Publication number

JP2018504436A5

JP2018504436A5 JP2017541301A JP2017541301A JP2018504436A5 JP 2018504436 A5 JP2018504436 A5 JP 2018504436A5 JP 2017541301 A JP2017541301 A JP 2017541301A JP 2017541301 A JP2017541301 A JP 2017541301A JP 2018504436 A5 JP2018504436 A5 JP 2018504436A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

composition according

item

teriflunomide

tacrolimus

Prior art date

2016-02-05

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

• Espacenet
• Global Dossier
• Discuss

• 239000008194 pharmaceutical composition Substances 0.000 claims description 89
• 239000003795 chemical substances by application Substances 0.000 claims description 20
• RMMXLENWKUUMAY-UHFFFAOYSA-N telmisartan Chemical compound CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O RMMXLENWKUUMAY-UHFFFAOYSA-N 0.000 claims description 16
• QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims description 15
• 229960000681 leflunomide Drugs 0.000 claims description 15
• VHOGYURTWQBHIL-UHFFFAOYSA-N leflunomide Chemical compound O1N=CC(C(=O)NC=2C=CC(=CC=2)C(F)(F)F)=C1C VHOGYURTWQBHIL-UHFFFAOYSA-N 0.000 claims description 15
• 229960001967 tacrolimus Drugs 0.000 claims description 15
• QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 claims description 15
• 229960000331 teriflunomide Drugs 0.000 claims description 15
• UTNUDOFZCWSZMS-YFHOEESVSA-N teriflunomide Chemical compound C\C(O)=C(/C#N)C(=O)NC1=CC=C(C(F)(F)F)C=C1 UTNUDOFZCWSZMS-YFHOEESVSA-N 0.000 claims description 15
• 229960003073 pirfenidone Drugs 0.000 claims description 14
• ISWRGOKTTBVCFA-UHFFFAOYSA-N pirfenidone Chemical group C1=C(C)C=CC(=O)N1C1=CC=CC=C1 ISWRGOKTTBVCFA-UHFFFAOYSA-N 0.000 claims description 14
• 229960000830 captopril Drugs 0.000 claims description 13
• FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 claims description 13
• 229960001195 imidapril Drugs 0.000 claims description 9
• KLZWOWYOHUKJIG-BPUTZDHNSA-N imidapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1C(N(C)C[C@H]1C(O)=O)=O)CC1=CC=CC=C1 KLZWOWYOHUKJIG-BPUTZDHNSA-N 0.000 claims description 9
• 239000005537 C09CA07 - Telmisartan Substances 0.000 claims description 8
• 229960005187 telmisartan Drugs 0.000 claims description 8
• -1 tradolapril Chemical compound 0.000 claims description 7
• PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims description 6
• 108010036949 Cyclosporine Proteins 0.000 claims description 6
• 108010061435 Enalapril Proteins 0.000 claims description 6
• 239000005475 Fimasartan Substances 0.000 claims description 6
• 108010007859 Lisinopril Proteins 0.000 claims description 6
• 206010030113 Oedema Diseases 0.000 claims description 6
• 229960004669 basiliximab Drugs 0.000 claims description 6
• 229960001265 ciclosporin Drugs 0.000 claims description 6
• 229930182912 cyclosporin Natural products 0.000 claims description 6
• 229960000873 enalapril Drugs 0.000 claims description 6
• GBXSMTUPTTWBMN-XIRDDKMYSA-N enalapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 GBXSMTUPTTWBMN-XIRDDKMYSA-N 0.000 claims description 6
• 229960003489 fimasartan Drugs 0.000 claims description 6
• AMEROGPZOLAFBN-UHFFFAOYSA-N fimasartan Chemical compound CCCCC1=NC(C)=C(CC(=S)N(C)C)C(=O)N1CC1=CC=C(C=2C(=CC=CC=2)C=2NN=NN=2)C=C1 AMEROGPZOLAFBN-UHFFFAOYSA-N 0.000 claims description 6
• 229960002394 lisinopril Drugs 0.000 claims description 6
• RLAWWYSOJDYHDC-BZSNNMDCSA-N lisinopril Chemical compound C([C@H](N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(O)=O)C(O)=O)CC1=CC=CC=C1 RLAWWYSOJDYHDC-BZSNNMDCSA-N 0.000 claims description 6
• 239000002674 ointment Substances 0.000 claims description 6
• 229960002582 perindopril Drugs 0.000 claims description 6
• IPVQLZZIHOAWMC-QXKUPLGCSA-N perindopril Chemical compound C1CCC[C@H]2C[C@@H](C(O)=O)N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H]21 IPVQLZZIHOAWMC-QXKUPLGCSA-N 0.000 claims description 6
• 229960005330 pimecrolimus Drugs 0.000 claims description 6
• KASDHRXLYQOAKZ-ZPSXYTITSA-N pimecrolimus Chemical compound C/C([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H](C(C[C@H](O)[C@H]1C)=O)CC)=C\[C@@H]1CC[C@@H](Cl)[C@H](OC)C1 KASDHRXLYQOAKZ-ZPSXYTITSA-N 0.000 claims description 6
• 229960001455 quinapril Drugs 0.000 claims description 6
• JSDRRTOADPPCHY-HSQYWUDLSA-N quinapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2=CC=CC=C2C1)C(O)=O)CC1=CC=CC=C1 JSDRRTOADPPCHY-HSQYWUDLSA-N 0.000 claims description 6
• 229960002769 zofenopril Drugs 0.000 claims description 6
• IAIDUHCBNLFXEF-MNEFBYGVSA-N zofenopril Chemical compound C([C@@H](C)C(=O)N1[C@@H](C[C@@H](C1)SC=1C=CC=CC=1)C(O)=O)SC(=O)C1=CC=CC=C1 IAIDUHCBNLFXEF-MNEFBYGVSA-N 0.000 claims description 6
• XPCFTKFZXHTYIP-PMACEKPBSA-N Benazepril Chemical compound C([C@@H](C(=O)OCC)N[C@@H]1C(N(CC(O)=O)C2=CC=CC=C2CC1)=O)CC1=CC=CC=C1 XPCFTKFZXHTYIP-PMACEKPBSA-N 0.000 claims description 5
• 239000002947 C09CA04 - Irbesartan Substances 0.000 claims description 5
• 229930105110 Cyclosporin A Natural products 0.000 claims description 5
• 239000005480 Olmesartan Substances 0.000 claims description 5
• 229960004530 benazepril Drugs 0.000 claims description 5
• 229960002923 denileukin diftitox Drugs 0.000 claims description 5
• 108010017271 denileukin diftitox Proteins 0.000 claims description 5
• 229960002198 irbesartan Drugs 0.000 claims description 5
• YCPOHTHPUREGFM-UHFFFAOYSA-N irbesartan Chemical compound O=C1N(CC=2C=CC(=CC=2)C=2C(=CC=CC=2)C=2[N]N=NN=2)C(CCCC)=NC21CCCC2 YCPOHTHPUREGFM-UHFFFAOYSA-N 0.000 claims description 5
• VTRAEEWXHOVJFV-UHFFFAOYSA-N olmesartan Chemical compound CCCC1=NC(C(C)(C)O)=C(C(O)=O)N1CC1=CC=C(C=2C(=CC=CC=2)C=2NN=NN=2)C=C1 VTRAEEWXHOVJFV-UHFFFAOYSA-N 0.000 claims description 5
• 229960005117 olmesartan Drugs 0.000 claims description 5
• 229960003401 ramipril Drugs 0.000 claims description 5
• HDACQVRGBOVJII-JBDAPHQKSA-N ramipril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@@H]2CCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 HDACQVRGBOVJII-JBDAPHQKSA-N 0.000 claims description 5
• 239000000203 mixture Substances 0.000 claims description 4
• 241000195940 Bryophyta Species 0.000 claims description 3
• 208000027418 Wounds and injury Diseases 0.000 claims description 3
• 229960005025 cilazapril Drugs 0.000 claims description 3
• HHHKFGXWKKUNCY-FHWLQOOXSA-N cilazapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H]1C(N2[C@@H](CCCN2CCC1)C(O)=O)=O)CC1=CC=CC=C1 HHHKFGXWKKUNCY-FHWLQOOXSA-N 0.000 claims description 3
• 239000006071 cream Substances 0.000 claims description 3
• 230000006378 damage Effects 0.000 claims description 3
• 239000006260 foam Substances 0.000 claims description 3
• 208000014674 injury Diseases 0.000 claims description 3
• 239000004922 lacquer Substances 0.000 claims description 3
• 239000007788 liquid Substances 0.000 claims description 3
• 239000006210 lotion Substances 0.000 claims description 3
• 235000011929 mousse Nutrition 0.000 claims description 3
• 239000007921 spray Substances 0.000 claims description 3
• 239000000725 suspension Substances 0.000 claims description 3
• 239000004072 C09CA03 - Valsartan Substances 0.000 claims description 2
• 239000002053 C09CA06 - Candesartan Substances 0.000 claims description 2
• 206010025282 Lymphoedema Diseases 0.000 claims description 2
• 229960000932 candesartan Drugs 0.000 claims description 2
• SGZAIDDFHDDFJU-UHFFFAOYSA-N candesartan Chemical compound CCOC1=NC2=CC=CC(C(O)=O)=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SGZAIDDFHDDFJU-UHFFFAOYSA-N 0.000 claims description 2
• 229940079593 drug Drugs 0.000 claims description 2
• 239000003814 drug Substances 0.000 claims description 2
• 208000002502 lymphedema Diseases 0.000 claims description 2
• 230000002265 prevention Effects 0.000 claims description 2
• 238000011200 topical administration Methods 0.000 claims description 2
• 229960004699 valsartan Drugs 0.000 claims description 2
• SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 claims description 2
• 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
• 239000000499 gel Substances 0.000 claims 1
• 239000006072 paste Substances 0.000 claims 1
• 238000000034 method Methods 0.000 description 23
• UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical group C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 description 2
• 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 description 2
• 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 description 2
• 210000001365 lymphatic vessel Anatomy 0.000 description 2
• BIDNLKIUORFRQP-XYGFDPSESA-N (2s,4s)-4-cyclohexyl-1-[2-[[(1s)-2-methyl-1-propanoyloxypropoxy]-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylic acid Chemical compound C([P@@](=O)(O[C@H](OC(=O)CC)C(C)C)CC(=O)N1[C@@H](C[C@H](C1)C1CCCCC1)C(O)=O)CCCC1=CC=CC=C1 BIDNLKIUORFRQP-XYGFDPSESA-N 0.000 description 1
• 239000002083 C09CA01 - Losartan Substances 0.000 description 1
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• 229960002490 fosinopril Drugs 0.000 description 1
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• KJJZZJSZUJXYEA-UHFFFAOYSA-N losartan Chemical compound CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C=2[N]N=NN=2)C=C1 KJJZZJSZUJXYEA-UHFFFAOYSA-N 0.000 description 1
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