JP2019513741A5 - - Google Patents
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- JP2019513741A5 JP2019513741A5 JP2018552693A JP2018552693A JP2019513741A5 JP 2019513741 A5 JP2019513741 A5 JP 2019513741A5 JP 2018552693 A JP2018552693 A JP 2018552693A JP 2018552693 A JP2018552693 A JP 2018552693A JP 2019513741 A5 JP2019513741 A5 JP 2019513741A5
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- 150000001875 compounds Chemical class 0.000 claims 19
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 claims 8
- 102100023419 Cystic fibrosis transmembrane conductance regulator Human genes 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 229910052710 silicon Inorganic materials 0.000 claims 6
- 239000010703 silicon Substances 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 5
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 229910052805 deuterium Inorganic materials 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 201000003883 Cystic fibrosis Diseases 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 230000007812 deficiency Effects 0.000 claims 2
- 125000004431 deuterium atom Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- -1 methoxy, ethoxy, isopropoxy, tert-butoxy Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 2
- ICSWLKDKQBNKAY-UHFFFAOYSA-N 1,1,3,3,5,5-hexamethyl-1,3,5-trisilinane Chemical class C[Si]1(C)C[Si](C)(C)C[Si](C)(C)C1 ICSWLKDKQBNKAY-UHFFFAOYSA-N 0.000 claims 1
- XRPSUWYWZUQALB-UHFFFAOYSA-N 2-[7-ethoxy-4-(3-fluorophenyl)-1-oxophthalazin-2-yl]-n-methyl-n-(2-methyl-1,3-benzoxazol-6-yl)acetamide Chemical compound N=1N(CC(=O)N(C)C=2C=C3OC(C)=NC3=CC=2)C(=O)C2=CC(OCC)=CC=C2C=1C1=CC=CC(F)=C1 XRPSUWYWZUQALB-UHFFFAOYSA-N 0.000 claims 1
- 102100034452 Alternative prion protein Human genes 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003694 Atrophy Diseases 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 206010006473 Bronchopulmonary aspergillosis Diseases 0.000 claims 1
- 101150029409 CFTR gene Proteins 0.000 claims 1
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims 1
- 206010008635 Cholestasis Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000000668 Chronic Pancreatitis Diseases 0.000 claims 1
- 206010009137 Chronic sinusitis Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 206010062264 Congenital hyperthyroidism Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims 1
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 208000024720 Fabry Disease Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- 208000033981 Hereditary haemochromatosis Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims 1
- 206010051125 Hypofibrinogenaemia Diseases 0.000 claims 1
- 208000000038 Hypoparathyroidism Diseases 0.000 claims 1
- 102100024640 Low-density lipoprotein receptor Human genes 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 208000015439 Lysosomal storage disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008955 Mucolipidoses Diseases 0.000 claims 1
- 206010072928 Mucolipidosis type II Diseases 0.000 claims 1
- 208000002678 Mucopolysaccharidoses Diseases 0.000 claims 1
- 206010068871 Myotonic dystrophy Diseases 0.000 claims 1
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims 1
- 208000035467 Pancreatic insufficiency Diseases 0.000 claims 1
- 206010033649 Pancreatitis chronic Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 208000026378 Polyglandular endocrine disease Diseases 0.000 claims 1
- 108091000054 Prion Proteins 0.000 claims 1
- 201000005660 Protein C Deficiency Diseases 0.000 claims 1
- 208000004430 Pulmonary Aspergillosis Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims 1
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000037444 atrophy Effects 0.000 claims 1
- 230000002146 bilateral effect Effects 0.000 claims 1
- 201000009267 bronchiectasis Diseases 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 210000003591 cerebellar nuclei Anatomy 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims 1
- 230000015271 coagulation Effects 0.000 claims 1
- 238000005345 coagulation Methods 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 230000002950 deficient Effects 0.000 claims 1
- 201000010064 diabetes insipidus Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims 1
- 230000020764 fibrinolysis Effects 0.000 claims 1
- QVDYQHXNAQHIKH-TZIWHRDSSA-N galicaftor Chemical compound FC1(OC2=C(O1)C=CC(=C2)C1(CC1)C(=O)N[C@@H]1C[C@@H](OC2=CC(=CC=C12)OC(F)F)C1=CC=C(C(=O)O)C=C1)F QVDYQHXNAQHIKH-TZIWHRDSSA-N 0.000 claims 1
- 208000013746 hereditary thrombophilia due to congenital protein C deficiency Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 230000000155 isotopic effect Effects 0.000 claims 1
- PURKAOJPTOLRMP-UHFFFAOYSA-N ivacaftor Chemical compound C1=C(O)C(C(C)(C)C)=CC(C(C)(C)C)=C1NC(=O)C1=CNC2=CC=CC=C2C1=O PURKAOJPTOLRMP-UHFFFAOYSA-N 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000020460 mucolipidosis II alpha/beta Diseases 0.000 claims 1
- 206010028093 mucopolysaccharidosis Diseases 0.000 claims 1
- 208000000638 myeloperoxidase deficiency Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000001817 pituitary effect Effects 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 230000020978 protein processing Effects 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 210000000463 red nucleus Anatomy 0.000 claims 1
- 102200132013 rs121909041 Human genes 0.000 claims 1
- 102200132105 rs193922525 Human genes 0.000 claims 1
- 102200132017 rs267606723 Human genes 0.000 claims 1
- 102200132015 rs74503330 Human genes 0.000 claims 1
- 150000003377 silicon compounds Chemical class 0.000 claims 1
- 208000002320 spinal muscular atrophy Diseases 0.000 claims 1
- 201000003624 spinocerebellar ataxia type 1 Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 210000001177 vas deferen Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662319439P | 2016-04-07 | 2016-04-07 | |
| US62/319,439 | 2016-04-07 | ||
| PCT/US2017/026579 WO2017177124A1 (en) | 2016-04-07 | 2017-04-07 | Silicone atoms containing ivacaftor analogues |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019513741A JP2019513741A (ja) | 2019-05-30 |
| JP2019513741A5 true JP2019513741A5 (enExample) | 2020-05-14 |
| JP7061076B2 JP7061076B2 (ja) | 2022-04-27 |
Family
ID=58549338
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018552693A Active JP7061076B2 (ja) | 2016-04-07 | 2017-04-07 | アイバカフトール類似体を含有するケイ素原子 |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US10662207B2 (enExample) |
| EP (1) | EP3440057B1 (enExample) |
| JP (1) | JP7061076B2 (enExample) |
| KR (1) | KR102448404B1 (enExample) |
| CN (1) | CN109563047A (enExample) |
| AR (1) | AR108203A1 (enExample) |
| AU (1) | AU2017248253B2 (enExample) |
| BR (1) | BR112018070747B1 (enExample) |
| CA (1) | CA3019663C (enExample) |
| IL (1) | IL262030B (enExample) |
| MA (1) | MA43775A (enExample) |
| MX (1) | MX386698B (enExample) |
| NZ (1) | NZ746793A (enExample) |
| SA (1) | SA518400164B1 (enExample) |
| SG (1) | SG11201808682XA (enExample) |
| WO (1) | WO2017177124A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015328174B2 (en) | 2014-10-06 | 2020-05-21 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP3325474A1 (en) | 2015-07-24 | 2018-05-30 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| RU2752567C2 (ru) | 2015-10-06 | 2021-07-29 | Протеостазис Терапьютикс, Инк. | Соединения, композиции и способы для модуляции cftr |
| US10662207B2 (en) * | 2016-04-07 | 2020-05-26 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating CFTR |
| ES2954658T3 (es) | 2016-06-21 | 2023-11-23 | Proteostasis Therapeutics Inc | Compuestos, composiciones y procedimientos para aumentar la actividad de CFTR |
| JOP20190042B1 (ar) * | 2016-09-30 | 2021-08-17 | Vertex Pharma | مُعدِّل لمنظم موصلية التليف الكيسي عبر الغشاء، وتركيبات صيدلانية، وطرق للعلاج، وعملية لتصنيع المُعدِّل |
| JOP20190125B1 (ar) | 2016-12-09 | 2022-03-14 | Vertex Pharma | مُعدِّل لمنظم موصلية التليف الكيسي عبر الغشاء، وتركيبات صيدلانية، وطرق للعلاج، وعملية لتصنيع المُعدِّل |
| EP3634402A1 (en) | 2017-06-08 | 2020-04-15 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| US20200289482A1 (en) * | 2017-06-21 | 2020-09-17 | The Johns Hopkins University | Cystic fibrosis transmembrane conductance regulator modulators for treating autosomal dominant polycystic kidney disease |
| AU2018304168B2 (en) | 2017-07-17 | 2023-05-04 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| US11434201B2 (en) | 2017-08-02 | 2022-09-06 | Vertex Pharmaceuticals Incorporated | Processes for preparing pyrrolidine compounds |
| US20210369749A1 (en) * | 2017-10-06 | 2021-12-02 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| US10654829B2 (en) | 2017-10-19 | 2020-05-19 | Vertex Pharmaceuticals Incorporated | Crystalline forms and compositions of CFTR modulators |
| CA3085006A1 (en) | 2017-12-08 | 2019-06-13 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
| JOP20200178A1 (ar) | 2018-02-15 | 2022-10-30 | Vertex Pharma | حلقات ضخمة كمعدلات لمنظم توصيل التليف الكيسي عبر الغشاء، وتركيبات صيدلانية منها، واستخدامها في علاج التليف الكيسي، وعملية لتصنيعها |
| WO2019195739A1 (en) | 2018-04-05 | 2019-10-10 | Alexander Russell Abela | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP3774825A1 (en) | 2018-04-13 | 2021-02-17 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| WO2020006269A1 (en) | 2018-06-27 | 2020-01-02 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| CN109663129B (zh) * | 2019-02-27 | 2021-05-11 | 四川大学华西第二医院 | 扩张型心肌病治疗药物及其应用 |
| TWI848092B (zh) | 2019-04-03 | 2024-07-11 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白調節劑 |
| KR20220064366A (ko) | 2019-08-14 | 2022-05-18 | 버텍스 파마슈티칼스 인코포레이티드 | Cftr 조절제의 결정질 형태 |
| CA3150736A1 (en) | 2019-08-14 | 2021-02-18 | Vertex Pharmaceuticals Incorporated | Process of making cftr modulators |
| TWI867024B (zh) | 2019-08-14 | 2024-12-21 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白之調節劑 |
| IL303519A (en) | 2020-12-10 | 2023-08-01 | Vertex Pharma | Cystic fibrosis treatment methods |
| CN116425642B (zh) * | 2023-04-06 | 2025-06-10 | 浙江科聚生物医药有限公司 | 2-甲氧基-4-氟-5-胺基苯酚的制备方法 |
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-
2017
- 2017-04-07 US US16/091,401 patent/US10662207B2/en active Active
- 2017-04-07 BR BR112018070747-3A patent/BR112018070747B1/pt active IP Right Grant
- 2017-04-07 MX MX2018012331A patent/MX386698B/es unknown
- 2017-04-07 CN CN201780031083.2A patent/CN109563047A/zh active Pending
- 2017-04-07 AR ARP170100899A patent/AR108203A1/es active IP Right Grant
- 2017-04-07 KR KR1020187031895A patent/KR102448404B1/ko active Active
- 2017-04-07 JP JP2018552693A patent/JP7061076B2/ja active Active
- 2017-04-07 MA MA043775A patent/MA43775A/fr unknown
- 2017-04-07 EP EP17718318.3A patent/EP3440057B1/en active Active
- 2017-04-07 CA CA3019663A patent/CA3019663C/en active Active
- 2017-04-07 SG SG11201808682XA patent/SG11201808682XA/en unknown
- 2017-04-07 AU AU2017248253A patent/AU2017248253B2/en active Active
- 2017-04-07 WO PCT/US2017/026579 patent/WO2017177124A1/en not_active Ceased
- 2017-04-07 NZ NZ746793A patent/NZ746793A/en unknown
-
2018
- 2018-10-02 IL IL262030A patent/IL262030B/en unknown
- 2018-10-04 SA SA518400164A patent/SA518400164B1/ar unknown
-
2020
- 2020-04-14 US US16/848,345 patent/US11248010B2/en active Active
-
2023
- 2023-12-04 US US18/527,973 patent/US20240109922A1/en not_active Abandoned
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2024
- 2024-07-19 US US18/778,363 patent/US20240368198A1/en not_active Abandoned
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