JP2017529388A5 - - Google Patents
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- JP2017529388A5 JP2017529388A5 JP2017530419A JP2017530419A JP2017529388A5 JP 2017529388 A5 JP2017529388 A5 JP 2017529388A5 JP 2017530419 A JP2017530419 A JP 2017530419A JP 2017530419 A JP2017530419 A JP 2017530419A JP 2017529388 A5 JP2017529388 A5 JP 2017529388A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- gnrh antagonist
- inflammatory
- gnrh
- 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
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- 239000008194 pharmaceutical composition Substances 0.000 claims 41
- 239000002474 gonadorelin antagonist Substances 0.000 claims 30
- 229940121381 gonadotrophin releasing hormone (gnrh) antagonists Drugs 0.000 claims 30
- NMJREATYWWNIKX-UHFFFAOYSA-N GnRH Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CC(C)C)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 NMJREATYWWNIKX-UHFFFAOYSA-N 0.000 claims 10
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 claims 10
- 208000027866 inflammatory disease Diseases 0.000 claims 9
- 230000002093 peripheral effect Effects 0.000 claims 9
- 239000013543 active substance Substances 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- 230000002757 inflammatory effect Effects 0.000 claims 8
- 208000037976 chronic inflammation Diseases 0.000 claims 7
- 230000006020 chronic inflammation Effects 0.000 claims 7
- 206010061218 Inflammation Diseases 0.000 claims 6
- 239000003795 chemical substances by application Substances 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 6
- 230000004968 inflammatory condition Effects 0.000 claims 6
- 230000004054 inflammatory process Effects 0.000 claims 6
- -1 dovobette (R) Substances 0.000 claims 5
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical compound OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 claims 5
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 4
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 4
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 4
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 239000003163 gonadal steroid hormone Substances 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 230000001575 pathological effect Effects 0.000 claims 3
- 229920000642 polymer Polymers 0.000 claims 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 3
- 230000009885 systemic effect Effects 0.000 claims 3
- QLLWADSMMMNRDJ-AFRFTAIISA-N (2R)-N'-[5-[(Z)-2-(1H-benzimidazol-2-yl)-3-(2,5-difluorophenyl)-1-hydroxy-3-oxoprop-1-enyl]-2-fluorophenyl]sulfonyl-2-hydroxypropanimidamide Chemical compound C[C@@H](O)C(\N)=N\S(=O)(=O)c1cc(ccc1F)C(\O)=C(\C(=O)c1cc(F)ccc1F)c1nc2ccccc2[nH]1 QLLWADSMMMNRDJ-AFRFTAIISA-N 0.000 claims 2
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 2
- 206010042953 Systemic sclerosis Diseases 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 108010052004 acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide Proteins 0.000 claims 2
- 230000008499 blood brain barrier function Effects 0.000 claims 2
- 230000036772 blood pressure Effects 0.000 claims 2
- 210000001218 blood-brain barrier Anatomy 0.000 claims 2
- 125000000609 carbazolyl group Chemical class C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 2
- 229960003230 cetrorelix Drugs 0.000 claims 2
- 108700008462 cetrorelix Proteins 0.000 claims 2
- SBNPWPIBESPSIF-MHWMIDJBSA-N cetrorelix Chemical group C([C@@H](C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 SBNPWPIBESPSIF-MHWMIDJBSA-N 0.000 claims 2
- 229960002272 degarelix Drugs 0.000 claims 2
- MEUCPCLKGZSHTA-XYAYPHGZSA-N degarelix Chemical compound C([C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CC=1C=CC(NC(=O)[C@H]2NC(=O)NC(=O)C2)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(NC(N)=O)C=C1 MEUCPCLKGZSHTA-XYAYPHGZSA-N 0.000 claims 2
- 229940011871 estrogen Drugs 0.000 claims 2
- 239000000262 estrogen Substances 0.000 claims 2
- 229960003794 ganirelix Drugs 0.000 claims 2
- 108700032141 ganirelix Proteins 0.000 claims 2
- GJNXBNATEDXMAK-PFLSVRRQSA-N ganirelix Chemical compound C([C@@H](C(=O)N[C@H](CCCCN=C(NCC)NCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN=C(NCC)NCC)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 GJNXBNATEDXMAK-PFLSVRRQSA-N 0.000 claims 2
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 2
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 2
- 230000007774 longterm Effects 0.000 claims 2
- 238000012423 maintenance Methods 0.000 claims 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 claims 2
- 229930185107 quinolinone Natural products 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 229960003604 testosterone Drugs 0.000 claims 2
- NKCIVLISTXOILK-UHFFFAOYSA-N triazinane-4,5,6-trione Chemical compound OC1=NN=NC(O)=C1O NKCIVLISTXOILK-UHFFFAOYSA-N 0.000 claims 2
- 230000003442 weekly effect Effects 0.000 claims 2
- NOENHWMKHNSHGX-IZOOSHNJSA-N (2s)-1-[(2s)-2-[[(2s)-2-[[(2r)-2-[[(2r)-2-[[(2s)-2-[[(2r)-2-[[(2s)-2-[[(2r)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-(ca Chemical compound C([C@H](C(=O)N[C@H](CCCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 NOENHWMKHNSHGX-IZOOSHNJSA-N 0.000 claims 1
- YCIPQJTZJGUXND-UHFFFAOYSA-N Aglaia odorata Alkaloid Natural products C1=CC(OC)=CC=C1C1(C(C=2C(=O)N3CCCC3=NC=22)C=3C=CC=CC=3)C2(O)C2=C(OC)C=C(OC)C=C2O1 YCIPQJTZJGUXND-UHFFFAOYSA-N 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 108010023617 abarelix Proteins 0.000 claims 1
- 229960002184 abarelix Drugs 0.000 claims 1
- AIWRTTMUVOZGPW-HSPKUQOVSA-N abarelix Chemical compound C([C@@H](C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 AIWRTTMUVOZGPW-HSPKUQOVSA-N 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 229940035676 analgesics Drugs 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000000730 antalgic agent Substances 0.000 claims 1
- 108010070670 antarelix Proteins 0.000 claims 1
- 239000003435 antirheumatic agent Substances 0.000 claims 1
- 230000037182 bone density Effects 0.000 claims 1
- 230000007211 cardiovascular event Effects 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- BDYYDXJSHYEDGB-UHFFFAOYSA-N diloxanide furoate Chemical compound C1=CC(N(C(=O)C(Cl)Cl)C)=CC=C1OC(=O)C1=CC=CO1 BDYYDXJSHYEDGB-UHFFFAOYSA-N 0.000 claims 1
- 229960003497 diloxanide furoate Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 239000012530 fluid Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 239000003862 glucocorticoid Substances 0.000 claims 1
- 150000004676 glycans Chemical class 0.000 claims 1
- 238000002657 hormone replacement therapy Methods 0.000 claims 1
- MTNDZQHUAFNZQY-UHFFFAOYSA-N imidazoline Chemical compound C1CN=CN1 MTNDZQHUAFNZQY-UHFFFAOYSA-N 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 229920001282 polysaccharide Polymers 0.000 claims 1
- 239000005017 polysaccharide Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical compound OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 claims 1
- 150000003384 small molecules Chemical group 0.000 claims 1
- 201000005671 spondyloarthropathy Diseases 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 1
- 230000002195 synergetic effect Effects 0.000 claims 1
- 229950011372 teverelix Drugs 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462041873P | 2014-08-26 | 2014-08-26 | |
| US62/041,873 | 2014-08-26 | ||
| US201462082200P | 2014-11-20 | 2014-11-20 | |
| US62/082,200 | 2014-11-20 | ||
| US201562110731P | 2015-02-02 | 2015-02-02 | |
| US62/110,731 | 2015-02-02 | ||
| US201562181289P | 2015-06-18 | 2015-06-18 | |
| US62/181,289 | 2015-06-18 | ||
| PCT/EP2015/069369 WO2016030334A2 (en) | 2014-08-26 | 2015-08-24 | Methods, agents and compositions for treatment of inflammatory conditions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017529388A JP2017529388A (ja) | 2017-10-05 |
| JP2017529388A5 true JP2017529388A5 (enExample) | 2018-10-04 |
Family
ID=54012190
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017530419A Pending JP2017529388A (ja) | 2014-08-26 | 2015-08-24 | 炎症性病態の治療のための方法、薬剤および組成物 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10821152B2 (enExample) |
| EP (1) | EP3185881B1 (enExample) |
| JP (1) | JP2017529388A (enExample) |
| AU (1) | AU2015308987B2 (enExample) |
| WO (1) | WO2016030334A2 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3415517T (pt) | 2012-09-28 | 2022-05-13 | Takeda Pharmaceuticals Co | Forma cristalina de 1-(4-1-(2,6-difluorobenzil)-5- dimetilaminometil-3-(6-metoxipiridazin-3-il)-2,4-dioxo- 1,2,3,4-tetrahidrotieno(2,3-d)-pirimidin-6-il)fenil)-3- metoxiureia |
| WO2017221144A1 (en) * | 2016-06-20 | 2017-12-28 | Dr. Reddy's Laboratories Limited | Process for the preparation of elagolix sodium and its polymorph |
| EP3518932B1 (en) | 2016-09-30 | 2024-11-13 | Sumitomo Pharma Switzerland GmbH | Treatment of prostate cancer |
| US11564958B2 (en) * | 2017-12-21 | 2023-01-31 | Resolys Bio, Inc. | Compositions and methods of treatment of Ehlers-Danlos syndromes |
| CN109946467B (zh) * | 2017-12-21 | 2021-05-28 | 中国医学科学院北京协和医院 | 一种用于胸椎黄韧带骨化诊断的生物标记物 |
| US11400093B2 (en) | 2019-01-15 | 2022-08-02 | Lupin, Inc. | Deuterated elagolix-like compositions and methods |
| CN112578125B (zh) * | 2019-09-27 | 2022-10-25 | 成都中医药大学 | 检测粪钙卫蛋白含量的试剂在制备卵巢病变筛查试剂盒中的用途 |
| WO2021251565A1 (en) * | 2020-06-12 | 2021-12-16 | Hk Inno.N Corporation | Pharmaceutical composition comprising benzimidazole derivative compound |
| CN113750089B (zh) * | 2021-10-13 | 2023-09-19 | 南方医科大学南方医院 | 2-芳基-1,3二氢苯并咪唑衍生物在制备治疗慢性肝病的药物中的用途 |
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| TW201130854A (en) | 2009-12-22 | 2011-09-16 | Bayer Schering Pharma Ag | Pyridinone derivatives and pharmaceutical compositions thereof |
| MX338914B (es) | 2010-05-21 | 2016-05-06 | Xl Protein Gmbh | Polipeptidos biosinteticos de espira aleatoria de prolina/alanina y sus usos. |
| WO2012175514A1 (en) | 2011-06-21 | 2012-12-27 | Bayer Intellectual Property Gmbh | Pyridinone derivatives and pharmaceutical compositions thereof |
| KR101586791B1 (ko) | 2012-12-28 | 2016-01-19 | 주식회사 종근당 | ＧｎＲＨ 유도체의 서방성 지질 초기제제 및 이를 포함하는 약제학적 조성물 |
-
2015
- 2015-08-24 EP EP15756614.2A patent/EP3185881B1/en active Active
- 2015-08-24 US US15/506,210 patent/US10821152B2/en active Active
- 2015-08-24 AU AU2015308987A patent/AU2015308987B2/en active Active
- 2015-08-24 JP JP2017530419A patent/JP2017529388A/ja active Pending
- 2015-08-24 WO PCT/EP2015/069369 patent/WO2016030334A2/en not_active Ceased
-
2016
- 2016-08-12 US US15/235,487 patent/US20160346255A1/en not_active Abandoned
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