JP2016513662A5 - - Google Patents
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- Publication number
- JP2016513662A5 JP2016513662A5 JP2016502197A JP2016502197A JP2016513662A5 JP 2016513662 A5 JP2016513662 A5 JP 2016513662A5 JP 2016502197 A JP2016502197 A JP 2016502197A JP 2016502197 A JP2016502197 A JP 2016502197A JP 2016513662 A5 JP2016513662 A5 JP 2016513662A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- aryl
- group
- alkynyl
- alkenyl
- 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.)
- Granted
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- 125000000623 heterocyclic group Chemical group 0.000 claims 107
- 125000001072 heteroaryl group Chemical group 0.000 claims 99
- 125000001931 aliphatic group Chemical group 0.000 claims 92
- 125000003118 aryl group Chemical group 0.000 claims 91
- 125000003342 alkenyl group Chemical group 0.000 claims 66
- 125000000304 alkynyl group Chemical group 0.000 claims 63
- 125000003107 substituted aryl group Chemical group 0.000 claims 57
- 229910052739 hydrogen Inorganic materials 0.000 claims 55
- 239000001257 hydrogen Substances 0.000 claims 55
- 150000002431 hydrogen Chemical group 0.000 claims 54
- 125000000217 alkyl group Chemical group 0.000 claims 51
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 46
- 229910052805 deuterium Inorganic materials 0.000 claims 46
- 229910052736 halogen Inorganic materials 0.000 claims 46
- 150000002367 halogens Chemical group 0.000 claims 46
- 125000000547 substituted alkyl group Chemical group 0.000 claims 46
- 125000004429 atom Chemical group 0.000 claims 43
- 125000002837 carbocyclic group Chemical group 0.000 claims 31
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 29
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 24
- 125000004404 heteroalkyl group Chemical group 0.000 claims 24
- 125000000753 cycloalkyl group Chemical group 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 7
- 150000002148 esters Chemical class 0.000 claims 7
- 239000000651 prodrug Substances 0.000 claims 7
- 229940002612 prodrug Drugs 0.000 claims 7
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 0.000 claims 4
- 230000007812 deficiency Effects 0.000 claims 4
- 201000010064 diabetes insipidus Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000004149 thio group Chemical group *S* 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 102000012605 Cystic Fibrosis Transmembrane Conductance Regulator Human genes 0.000 claims 2
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- -1 be a NR 100 Inorganic materials 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 229920000155 polyglutamine Polymers 0.000 claims 2
- 108010040003 polyglutamine Proteins 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- OOUGLTULBSNHNF-UHFFFAOYSA-N 3-[5-(2-fluorophenyl)-1,2,4-oxadiazol-3-yl]benzoic acid Chemical compound OC(=O)C1=CC=CC(C=2N=C(ON=2)C=2C(=CC=CC=2)F)=C1 OOUGLTULBSNHNF-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 102000014461 Ataxins Human genes 0.000 claims 1
- 108010078286 Ataxins Proteins 0.000 claims 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 1
- 206010008025 Cerebellar ataxia Diseases 0.000 claims 1
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010062264 Congenital hyperthyroidism Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013883 Dwarfism 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
- CEAZRRDELHUEMR-URQXQFDESA-N Gentamicin Chemical compound O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N CEAZRRDELHUEMR-URQXQFDESA-N 0.000 claims 1
- 229930182566 Gentamicin Natural products 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000031226 Hyperlipidaemia 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
- 208000015439 Lysosomal storage disease 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
- 201000005118 Nephrogenic diabetes insipidus Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain 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
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 229960003995 ataluren Drugs 0.000 claims 1
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 238000004587 chromatography analysis Methods 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002124 endocrine Effects 0.000 claims 1
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims 1
- 229960002518 gentamicin Drugs 0.000 claims 1
- 208000020346 hyperlipoproteinemia Diseases 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
- 229940005405 kalydeco Drugs 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000004570 mortar (masonry) Substances 0.000 claims 1
- 208000020460 mucolipidosis II alpha/beta Diseases 0.000 claims 1
- 206010028093 mucopolysaccharidosis Diseases 0.000 claims 1
- 201000000585 muscular atrophy Diseases 0.000 claims 1
- 208000000638 myeloperoxidase deficiency Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 201000009881 secretory diarrhea Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 0 C*1c2ccc(*(*)C(C*(*=C(c3cc(*)ccc3)c(cc3)c4cc3N=O)C4=O)=O)cc2OC1 Chemical compound C*1c2ccc(*(*)C(C*(*=C(c3cc(*)ccc3)c(cc3)c4cc3N=O)C4=O)=O)cc2OC1 0.000 description 5
- CGLUILODCRIQOR-ZUEIMRROSA-N CC1C(C)(CC2)O[C@H]2C1 Chemical compound CC1C(C)(CC2)O[C@H]2C1 CGLUILODCRIQOR-ZUEIMRROSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361778870P | 2013-03-13 | 2013-03-13 | |
| US61/778,870 | 2013-03-13 | ||
| PCT/US2014/026623 WO2014160440A1 (en) | 2013-03-13 | 2014-03-13 | Pyridazinone compounds and methods for the treatment of cystic fibrosis |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016513662A JP2016513662A (ja) | 2016-05-16 |
| JP2016513662A5 true JP2016513662A5 (enExample) | 2017-04-13 |
| JP6545148B2 JP6545148B2 (ja) | 2019-07-17 |
Family
ID=51529901
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016502197A Expired - Fee Related JP6545148B2 (ja) | 2013-03-13 | 2014-03-13 | ピリダジノン化合物及び嚢胞性線維症の治療のための方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (8) | US9783529B2 (enExample) |
| EP (1) | EP2968323A4 (enExample) |
| JP (1) | JP6545148B2 (enExample) |
| KR (1) | KR101943490B1 (enExample) |
| CN (1) | CN105307655B (enExample) |
| AU (1) | AU2014243818B2 (enExample) |
| BR (1) | BR112015023328A2 (enExample) |
| CA (2) | CA3044766A1 (enExample) |
| HK (1) | HK1220610A1 (enExample) |
| MX (1) | MX365950B (enExample) |
| NZ (1) | NZ712180A (enExample) |
| WO (1) | WO2014160440A1 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2635581C (en) | 2005-12-28 | 2017-02-28 | Vertex Pharmaceuticals Incorporated | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| WO2014160440A1 (en) * | 2013-03-13 | 2014-10-02 | Flatley Discovery Lab | Pyridazinone compounds and methods for the treatment of cystic fibrosis |
| WO2015196071A1 (en) | 2014-06-19 | 2015-12-23 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| KR101891933B1 (ko) | 2014-08-14 | 2018-08-24 | 에프. 호프만-라 로슈 아게 | B형 간염 바이러스 감염의 치료 또는 예방을 위한 신규한 피리다존 및 트라이아진온 |
| AU2015328174B2 (en) | 2014-10-06 | 2020-05-21 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| RU2749213C2 (ru) | 2014-10-07 | 2021-06-07 | Вертекс Фармасьютикалз Инкорпорейтед | Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе |
| BR112017009194A2 (pt) * | 2014-10-31 | 2017-12-26 | Abbvie Sarl | tetra-hidropiranos substituídos e método de uso |
| WO2016073545A1 (en) | 2014-11-06 | 2016-05-12 | Concert Pharmaceuticals, Inc. | Phenyloxadiazole benzoic acids |
| WO2016105477A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc | Derivatives of 5-phenyl- or 5-heteroarylthiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| CA2971835A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| EP3325474A1 (en) | 2015-07-24 | 2018-05-30 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| 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 |
| WO2018064529A1 (en) * | 2016-09-29 | 2018-04-05 | The Uab Research Foundation | Methods and compositions for increasing mucus clearance |
| CA3041675A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | N-phenyl-2-(3-phenyl-6-oxo-1,6-dihydropyridazin-1-yl)acetamide derivatives for treating cystic fibrosis |
| EP3532469A1 (en) | 2016-10-26 | 2019-09-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
| CA3041676A1 (en) * | 2016-10-26 | 2018-05-03 | Daniel Parks | Pyridazine derivatives, compositions and methods for modulating cftr |
| WO2018201126A1 (en) | 2017-04-28 | 2018-11-01 | Proteostasis Therapeutics, Inc. | 4-sulfonylaminocarbonylquinoline derivatives for increasing cftr activity |
| US11464775B2 (en) * | 2017-08-15 | 2022-10-11 | Agios Pharmaceuticals, Inc. | Pyruvate kinase modulators and use thereof |
| US20210369749A1 (en) | 2017-10-06 | 2021-12-02 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| US12233063B2 (en) | 2017-10-20 | 2025-02-25 | The Regents Of The University Of Michigan | Compositions and methods for treating eye disorders |
| WO2019136314A1 (en) | 2018-01-05 | 2019-07-11 | The Curators Of The University Of Missouri | Compounds and methods for treatment of cystic fibrosis |
| EP3828174A4 (en) * | 2018-07-19 | 2022-08-17 | Sumitomo Pharma Co., Ltd. | Pyridazinone derivative |
| CN108530476A (zh) * | 2018-07-24 | 2018-09-14 | 武汉轻工大学 | 一种克立硼罗中间体的制备方法 |
| LT3860998T (lt) | 2018-10-05 | 2024-06-25 | Annapurna Bio Inc. | Junginiai ir kompozicijos, skirti gydyti būkles, susijusias su apj receptoriaus aktyvumu |
| DK3877052T3 (da) | 2018-11-06 | 2023-09-25 | Edgewise Therapeutics Inc | Pyridazinonforbindelser og anvendelser deraf |
| AU2019374812B2 (en) | 2018-11-06 | 2025-03-06 | Edgewise Therapeutics, Inc. | Pyridazinone compounds and uses thereof |
| EP3877376B1 (en) | 2018-11-06 | 2023-08-23 | Edgewise Therapeutics, Inc. | Pyridazinone compounds and uses thereof |
| FR3103701B1 (fr) | 2019-11-28 | 2021-11-26 | Inst Nat Sante Rech Med | Composés de typen2-arylméthyl-4-haloalkyl-pyridazin-3-one et leur utilisation |
| JP2023505213A (ja) * | 2019-12-05 | 2023-02-08 | フラットリー ディスカバリー ラブ，エルエルシー | 嚢胞性線維症の治療のための化合物および方法 |
| AU2021311597A1 (en) * | 2020-07-21 | 2023-02-02 | The Regents Of The University Of Michigan | Compositions and methods for activating pyruvate kinase |
| MX2023001757A (es) * | 2020-08-14 | 2023-02-22 | Denali Therapeutics Inc | Compuestos, composiciones y metodos. |
| WO2023052783A1 (en) * | 2021-09-30 | 2023-04-06 | Sitryx Therapeutics Limited | Novel compounds |
| WO2023158708A1 (en) * | 2022-02-16 | 2023-08-24 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| CA3265895A1 (en) * | 2022-08-25 | 2024-02-29 | The Hospital For Sick Children | PYRIDAZINONE COMPOUNDS MODULATING MUTANT PROTEINS FOR THE TREATMENT OF RESPIRATORY DISEASES |
| WO2025143888A1 (ko) * | 2023-12-28 | 2025-07-03 | 아밀로이드솔루션 주식회사 | 신규 인덴온 유도체 및 이의 용도 |
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-
2014
- 2014-03-13 WO PCT/US2014/026623 patent/WO2014160440A1/en not_active Ceased
- 2014-03-13 US US14/210,277 patent/US9783529B2/en not_active Expired - Fee Related
- 2014-03-13 AU AU2014243818A patent/AU2014243818B2/en not_active Ceased
- 2014-03-13 MX MX2015012866A patent/MX365950B/es active IP Right Grant
- 2014-03-13 KR KR1020157027647A patent/KR101943490B1/ko not_active Expired - Fee Related
- 2014-03-13 CN CN201480021457.9A patent/CN105307655B/zh not_active Expired - Fee Related
- 2014-03-13 HK HK16108633.8A patent/HK1220610A1/zh unknown
- 2014-03-13 BR BR112015023328A patent/BR112015023328A2/pt not_active Application Discontinuation
- 2014-03-13 US US14/210,261 patent/US8937178B2/en active Active
- 2014-03-13 CA CA3044766A patent/CA3044766A1/en not_active Abandoned
- 2014-03-13 US US14/210,273 patent/US9790215B2/en not_active Expired - Fee Related
- 2014-03-13 JP JP2016502197A patent/JP6545148B2/ja not_active Expired - Fee Related
- 2014-03-13 CA CA2906008A patent/CA2906008C/en not_active Expired - Fee Related
- 2014-03-13 NZ NZ712180A patent/NZ712180A/en not_active IP Right Cessation
- 2014-03-13 EP EP14773937.9A patent/EP2968323A4/en not_active Withdrawn
-
2015
- 2015-01-19 US US14/599,998 patent/US9682969B2/en not_active Expired - Fee Related
-
2017
- 2017-06-06 US US15/615,466 patent/US10280160B2/en active Active
- 2017-10-06 US US15/726,813 patent/US10370366B2/en active Active
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2019
- 2019-04-30 US US16/398,680 patent/US10889576B2/en not_active Expired - Fee Related
- 2019-07-15 US US16/511,315 patent/US20200017486A1/en not_active Abandoned
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