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 (https=) | 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) | US8937178B2 (https=) |
| EP (1) | EP2968323A4 (https=) |
| JP (1) | JP6545148B2 (https=) |
| KR (1) | KR101943490B1 (https=) |
| CN (1) | CN105307655B (https=) |
| AU (1) | AU2014243818B2 (https=) |
| BR (1) | BR112015023328A2 (https=) |
| CA (2) | CA2906008C (https=) |
| HK (1) | HK1220610A1 (https=) |
| MX (1) | MX365950B (https=) |
| NZ (1) | NZ712180A (https=) |
| WO (1) | WO2014160440A1 (https=) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3219705B1 (en) | 2005-12-28 | 2020-03-11 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of the amorphous form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| MX365950B (es) * | 2013-03-13 | 2019-06-19 | Flatley Discovery Lab Llc | Compuestos de piridazinona y metodos para el tratamiento de la fibrosis quistica. |
| EP3157917B1 (en) | 2014-06-19 | 2020-03-18 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| JP6506836B2 (ja) | 2014-08-14 | 2019-04-24 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｂ型肝炎ウイルス感染症の処置および予防のための新規ピリダゾンおよびトリアジノン |
| MA41051B1 (fr) | 2014-10-06 | 2020-11-30 | Vertex Pharma | Modulateurs du régulateur de conductance transmembranaire de la mucoviscidose |
| CN107250113B (zh) | 2014-10-07 | 2019-03-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调节蛋白的调节剂的共晶 |
| MX2017005663A (es) * | 2014-10-31 | 2018-03-01 | Abbvie Sarl | Tetrahidropiranos sustituidos y metodo de uso. |
| WO2016073545A1 (en) | 2014-11-06 | 2016-05-12 | Concert Pharmaceuticals, Inc. | Phenyloxadiazole benzoic acids |
| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| US10392378B2 (en) | 2014-12-23 | 2019-08-27 | Proteostasis Therapeutics, Inc. | Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| US10344023B2 (en) | 2014-12-23 | 2019-07-09 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| US10548878B2 (en) | 2015-07-24 | 2020-02-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods of increasing CFTR activity |
| MA43775A (fr) | 2016-04-07 | 2021-05-05 | Proteostasis Therapeutics Inc | Analogues du ivacaftor conentant des atomes de silicium |
| MA45397A (fr) | 2016-06-21 | 2019-04-24 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| WO2018064529A1 (en) * | 2016-09-29 | 2018-04-05 | The Uab Research Foundation | Methods and compositions for increasing mucus clearance |
| WO2018081378A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
| AU2017348186A1 (en) * | 2016-10-26 | 2019-05-16 | Proteostasis Therapeutics, Inc | Pyridazine derivatives, compositions and methods for modulating CFTR |
| 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 |
| MA49061A (fr) | 2017-04-28 | 2021-04-21 | Proteostasis Therapeutics Inc | Dérivés 4-sulfonylaminocarbonylquinoline pour augmenter l'activité cftr |
| DK3668513T3 (da) * | 2017-08-15 | 2022-01-10 | Agios Pharmaceuticals Inc | Pyruvatkinase-aktiveringsmidler til anvendelse til behandling af blodsygdomme |
| AU2018346602B2 (en) | 2017-10-06 | 2024-10-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods for increasing CFTR activity |
| EP3697354A4 (en) | 2017-10-20 | 2021-06-30 | The Regents of The University of Michigan | EYE DISEASE COMPOSITIONS AND METHODS |
| 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 |
| JP7640458B2 (ja) | 2018-10-05 | 2025-03-05 | アンナプルナ バイオ インコーポレイテッド | Ａｐｊ受容体活性に関連する状態を処置するための化合物および組成物 |
| AU2019374812B2 (en) | 2018-11-06 | 2025-03-06 | Edgewise Therapeutics, Inc. | Pyridazinone compounds and uses thereof |
| DK3877376T3 (da) | 2018-11-06 | 2023-10-02 | Edgewise Therapeutics Inc | Pyridazinonforbindelser og anvendelser deraf |
| CA3118908A1 (en) | 2018-11-06 | 2020-05-14 | 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 |
| WO2021113795A1 (en) * | 2019-12-05 | 2021-06-10 | Flatley Discovery Lab, Llc | Compounds and methods for the treatment of cystic fibrosis |
| AU2021311597A1 (en) * | 2020-07-21 | 2023-02-02 | The Regents Of The University Of Michigan | Compositions and methods for activating pyruvate kinase |
| TWI911262B (zh) * | 2020-08-14 | 2026-01-11 | 美商戴納立製藥公司 | 化合物、組合物及方法 |
| US20240100183A1 (en) * | 2020-12-11 | 2024-03-28 | University Of Iowa Research Foundation | Compositions comprising molecules for cystic fibrosis treatment |
| WO2023052783A1 (en) * | 2021-09-30 | 2023-04-06 | Sitryx Therapeutics Limited | Novel compounds |
| US20250145592A1 (en) * | 2022-02-16 | 2025-05-08 | Nico Therapeutics, Inc. | Compounds, compositions, and methods |
| EP4577525A1 (en) * | 2022-08-25 | 2025-07-02 | The Hospital For Sick Children | Pyridazinone compounds which modulate mutant proteins for treating respiratory diseases |
| KR20250105245A (ko) * | 2023-12-28 | 2025-07-08 | 아밀로이드솔루션 주식회사 | 신규 인덴온 유도체 및 이의 용도 |
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-
2014
- 2014-03-13 MX MX2015012866A patent/MX365950B/es active IP Right Grant
- 2014-03-13 CA CA2906008A patent/CA2906008C/en not_active Expired - Fee Related
- 2014-03-13 HK HK16108633.8A patent/HK1220610A1/zh unknown
- 2014-03-13 AU AU2014243818A patent/AU2014243818B2/en not_active Ceased
- 2014-03-13 CN CN201480021457.9A patent/CN105307655B/zh not_active Expired - Fee Related
- 2014-03-13 EP EP14773937.9A patent/EP2968323A4/en not_active Withdrawn
- 2014-03-13 BR BR112015023328A patent/BR112015023328A2/pt not_active Application Discontinuation
- 2014-03-13 WO PCT/US2014/026623 patent/WO2014160440A1/en not_active Ceased
- 2014-03-13 CA CA3044766A patent/CA3044766A1/en not_active Abandoned
- 2014-03-13 US US14/210,261 patent/US8937178B2/en active Active
- 2014-03-13 KR KR1020157027647A patent/KR101943490B1/ko not_active Expired - Fee Related
- 2014-03-13 US US14/210,273 patent/US9790215B2/en not_active Expired - Fee Related
- 2014-03-13 US US14/210,277 patent/US9783529B2/en not_active Expired - Fee Related
- 2014-03-13 JP JP2016502197A patent/JP6545148B2/ja not_active Expired - Fee Related
- 2014-03-13 NZ NZ712180A patent/NZ712180A/en not_active IP Right Cessation
-
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
-
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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