JP2020522544A5 - - Google Patents
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- JP2020522544A5 JP2020522544A5 JP2019567608A JP2019567608A JP2020522544A5 JP 2020522544 A5 JP2020522544 A5 JP 2020522544A5 JP 2019567608 A JP2019567608 A JP 2019567608A JP 2019567608 A JP2019567608 A JP 2019567608A JP 2020522544 A5 JP2020522544 A5 JP 2020522544A5
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- Prior art keywords
- patient
- pharmaceutical composition
- antigen
- antibody
- binding fragment
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 claims 23
- 102000004965 antibodies Human genes 0.000 claims 21
- 108090001123 antibodies Proteins 0.000 claims 21
- 239000000427 antigen Substances 0.000 claims 21
- 102000038129 antigens Human genes 0.000 claims 21
- 108091007172 antigens Proteins 0.000 claims 21
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 18
- 238000002560 therapeutic procedure Methods 0.000 claims 13
- 239000000556 agonist Substances 0.000 claims 10
- 108090001061 Insulin Proteins 0.000 claims 9
- 102000004877 Insulin Human genes 0.000 claims 9
- 208000009576 Hypercholesterolemia Diseases 0.000 claims 6
- 102100005352 PCSK9 Human genes 0.000 claims 6
- 101700000651 PCSK9 Proteins 0.000 claims 6
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 6
- 239000003112 inhibitor Substances 0.000 claims 6
- 230000002401 inhibitory effect Effects 0.000 claims 6
- 150000001413 amino acids Chemical group 0.000 claims 4
- 206010003210 Arteriosclerosis Diseases 0.000 claims 3
- 208000004981 Coronary Disease Diseases 0.000 claims 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 3
- 230000000271 cardiovascular Effects 0.000 claims 3
- 201000008739 coronary artery disease Diseases 0.000 claims 3
- 239000008103 glucose Substances 0.000 claims 3
- DTHNMHAUYICORS-KTKZVXAJSA-N 107444-51-9 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 2
- 206010012601 Diabetes mellitus Diseases 0.000 claims 2
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- 102100003818 GCG Human genes 0.000 claims 2
- 101710042131 GCG Proteins 0.000 claims 2
- 102000036849 Islet amyloid polypeptide Human genes 0.000 claims 2
- 108010041872 Islet amyloid polypeptide Proteins 0.000 claims 2
- 208000001072 Type 2 Diabetes Mellitus Diseases 0.000 claims 2
- 230000003178 anti-diabetic Effects 0.000 claims 2
- 239000003472 antidiabetic agent Substances 0.000 claims 2
- 230000001419 dependent Effects 0.000 claims 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 230000000051 modifying Effects 0.000 claims 2
- 239000000018 receptor agonist Substances 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- IDHVLSACPFUBDY-QCDLPZBNSA-N xenin Chemical compound C([C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(O)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CN=CN1 IDHVLSACPFUBDY-QCDLPZBNSA-N 0.000 claims 2
- 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
- ZOBPZXTWZATXDG-UHFFFAOYSA-N 1,3-thiazolidine-2,4-dione Chemical compound O=C1CSC(=O)N1 ZOBPZXTWZATXDG-UHFFFAOYSA-N 0.000 claims 1
- IGRCWJPBLWGNPX-UHFFFAOYSA-N 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-1,2-oxazole-4-carboxamide Chemical compound C=1C=C(Cl)C=CC=1N(C)C(=O)C1=C(C)ON=C1C1=CC=CC=C1Cl IGRCWJPBLWGNPX-UHFFFAOYSA-N 0.000 claims 1
- SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 claims 1
- OIRDTQYFTABQOQ-GAWUUDPSSA-N 9-β-D-XYLOFURANOSYL-ADENINE Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@H](O)[C@H]1O OIRDTQYFTABQOQ-GAWUUDPSSA-N 0.000 claims 1
- 206010000891 Acute myocardial infarction Diseases 0.000 claims 1
- OIRDTQYFTABQOQ-SXVXDFOESA-N Adenosine Natural products Nc1ncnc2c1ncn2[C@@H]3O[C@@H](CO)[C@H](O)[C@@H]3O OIRDTQYFTABQOQ-SXVXDFOESA-N 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- RCHHVVGSTHAVPF-ZPHPLDECSA-N Apidra Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3N=CNC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CNC=N1 RCHHVVGSTHAVPF-ZPHPLDECSA-N 0.000 claims 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 claims 1
- 102100008845 COPA Human genes 0.000 claims 1
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- 102100009019 FFAR1 Human genes 0.000 claims 1
- 102100009021 FFAR4 Human genes 0.000 claims 1
- 101700008340 FFAR4 Proteins 0.000 claims 1
- 102000018711 Facilitative Glucose Transport Proteins Human genes 0.000 claims 1
- 108091006011 G proteins Proteins 0.000 claims 1
- 102100016463 GPBAR1 Human genes 0.000 claims 1
- 101710045222 GPBAR1 Proteins 0.000 claims 1
- 102000025873 GPCR, family 2, glucagon receptor Human genes 0.000 claims 1
- 108010063919 GPCR, family 2, glucagon receptor Proteins 0.000 claims 1
- 102100018511 GPR142 Human genes 0.000 claims 1
- 101710030445 GPR142 Proteins 0.000 claims 1
- 102000030007 GTP-Binding Proteins Human genes 0.000 claims 1
- 108091000058 GTP-Binding Proteins Proteins 0.000 claims 1
- COCFEDIXXNGUNL-RFKWWTKHSA-N Glargine Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3NC=NC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(=O)NCC(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 COCFEDIXXNGUNL-RFKWWTKHSA-N 0.000 claims 1
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| PCT/IB2018/054182 WO2018225041A1 (fr) | 2017-06-09 | 2018-06-09 | Méthodes de traitement de l'hyperlipidémie chez des patients diabétiques par administration d'un inhibiteur de pcsk9 |
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| JP2023111915A Pending JP2023123842A (ja) | 2017-06-09 | 2023-07-07 | Ｐｃｓｋ９阻害剤の投与による糖尿病患者における高脂血症を治療する方法 |
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| PL3326648T3 (pl) | 2011-01-28 | 2021-10-11 | Sanofi Biotechnology | Kompozycje farmaceutyczne zawierające ludzkie przeciwciała przeciwko PCSK9 |
| AR087305A1 (es) | 2011-07-28 | 2014-03-12 | Regeneron Pharma | Formulaciones estabilizadas que contienen anticuerpos anti-pcsk9, metodo de preparacion y kit |
| EA201890519A1 (ru) | 2015-08-18 | 2018-07-31 | Ридженерон Фармасьютикалз, Инк. | Ингибирующие антитела против pcsk9 для лечения пациентов с гиперлипидемией, подвергающихся аферезу липопротеинов |
| CN113876956B (zh) * | 2020-07-01 | 2023-07-04 | 陈敏 | Pcsk9抑制剂在制备促进皮肤色素生成产品中的应用 |
| CN114525258A (zh) * | 2020-10-30 | 2022-05-24 | 未来智人再生医学研究院(广州)有限公司 | 一种表达pcsk9阻断物的多能干细胞或其衍生物及应用 |
| CN115992138A (zh) * | 2021-09-30 | 2023-04-21 | 北京安龙生物医药有限公司 | 用于治疗与pcsk9相关疾病的靶向寡核苷酸 |
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| JO3672B1 (ar) * | 2008-12-15 | 2020-08-27 | Regeneron Pharma | أجسام مضادة بشرية عالية التفاعل الكيماوي بالنسبة لإنزيم سبتيليسين كنفرتيز بروبروتين / كيكسين نوع 9 (pcsk9). |
| WO2015140079A1 (fr) * | 2014-03-17 | 2015-09-24 | Sanofi | Methodes pour traiter des sujets atteints d'hypercholestérolémie primaire qui n'est pas prise en charge de manière adéquate |
| JP6912374B2 (ja) * | 2014-07-16 | 2021-08-04 | サノフィ・バイオテクノロジー | 高コレステロール血症を有する高心血管リスク患者を処置するための方法 |
| KR20240017117A (ko) * | 2014-07-16 | 2024-02-06 | 사노피 바이오테크놀로지 | 이형접합성 가족성 고콜레스테롤혈증(heFH) 환자의 치료방법 |
| EA201890519A1 (ru) * | 2015-08-18 | 2018-07-31 | Ридженерон Фармасьютикалз, Инк. | Ингибирующие антитела против pcsk9 для лечения пациентов с гиперлипидемией, подвергающихся аферезу липопротеинов |
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2018
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- 2018-06-09 IL IL314423A patent/IL314423A/en unknown
- 2018-06-09 CA CA3066317A patent/CA3066317A1/fr active Pending
- 2018-06-09 EP EP18737034.1A patent/EP3634469A1/fr not_active Withdrawn
- 2018-06-09 JP JP2019567608A patent/JP2020522544A/ja active Pending
- 2018-06-09 CN CN201880037888.2A patent/CN110913889A/zh not_active Withdrawn
- 2018-06-09 IL IL271212A patent/IL271212B1/en unknown
- 2018-06-09 KR KR1020197038159A patent/KR20200026826A/ko not_active IP Right Cessation
- 2018-06-09 MX MX2019014831A patent/MX2019014831A/es unknown
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2023
- 2023-07-07 JP JP2023111915A patent/JP2023123842A/ja active Pending
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