JPWO2020160010A5 - - Google Patents
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- JPWO2020160010A5 JPWO2020160010A5 JP2021543157A JP2021543157A JPWO2020160010A5 JP WO2020160010 A5 JPWO2020160010 A5 JP WO2020160010A5 JP 2021543157 A JP2021543157 A JP 2021543157A JP 2021543157 A JP2021543157 A JP 2021543157A JP WO2020160010 A5 JPWO2020160010 A5 JP WO2020160010A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- pharmaceutically acceptable
- acceptable salt
- alkyl
- compound
- 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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- 150000001875 compounds Chemical class 0.000 claims 41
- 150000003839 salts Chemical class 0.000 claims 39
- 229910052739 hydrogen Inorganic materials 0.000 claims 24
- 239000001257 hydrogen Substances 0.000 claims 24
- 150000002431 hydrogen Chemical class 0.000 claims 21
- 125000000547 substituted alkyl group Chemical group 0.000 claims 19
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical group 0.000 claims 13
- -1 3 -hydroxycyclobutyl Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000003107 substituted aryl group Chemical group 0.000 claims 9
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 6
- 239000000460 chlorine Substances 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 6
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 6
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 6
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 5
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 230000007812 deficiency Effects 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 4
- 201000010064 diabetes insipidus Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 102000008371 intracellularly ATP-gated chloride channel activity proteins Human genes 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 2
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 2
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 230000015271 coagulation Effects 0.000 claims 2
- 238000005345 coagulation Methods 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000003003 spiro group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102000014461 Ataxins Human genes 0.000 claims 1
- 108010078286 Ataxins Proteins 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 206010006473 Bronchopulmonary aspergillosis Diseases 0.000 claims 1
- 206010008025 Cerebellar ataxia Diseases 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
- 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
- 102100023419 Cystic fibrosis transmembrane conductance regulator Human genes 0.000 claims 1
- 208000027219 Deficiency disease 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
- 208000005139 Hereditary Angioedema Types I and II 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
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims 1
- 208000035467 Pancreatic insufficiency Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 208000024777 Prion disease Diseases 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
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 claims 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 208000004622 abetalipoproteinemia Diseases 0.000 claims 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000005002 aryl methyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000002146 bilateral effect Effects 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 201000009267 bronchiectasis Diseases 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 210000003591 cerebellar nuclei Anatomy 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims 1
- 230000020764 fibrinolysis Effects 0.000 claims 1
- 239000003527 fibrinolytic agent Substances 0.000 claims 1
- 230000003480 fibrinolytic effect Effects 0.000 claims 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims 1
- 208000012770 hereditary angioedema type 1 Diseases 0.000 claims 1
- 208000013746 hereditary thrombophilia due to congenital protein C deficiency Diseases 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 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
- XMSZANIMCDLNKA-UHFFFAOYSA-N methyl hypofluorite Chemical compound COF XMSZANIMCDLNKA-UHFFFAOYSA-N 0.000 claims 1
- 208000020460 mucolipidosis II alpha/beta Diseases 0.000 claims 1
- 230000000510 mucolytic effect Effects 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
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 230000002988 nephrogenic effect Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 108010040003 polyglutamine Proteins 0.000 claims 1
- 229920000155 polyglutamine Polymers 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 210000000463 red nucleus Anatomy 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 201000009881 secretory diarrhea Diseases 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 210000001177 vas deferen Anatomy 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962797743P | 2019-01-28 | 2019-01-28 | |
| US62/797,743 | 2019-01-28 | ||
| US201962931502P | 2019-11-06 | 2019-11-06 | |
| US62/931,502 | 2019-11-06 | ||
| PCT/US2020/015441 WO2020160010A1 (en) | 2019-01-28 | 2020-01-28 | Compounds and methods for the treatment of cystic fibrosis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022518778A JP2022518778A (ja) | 2022-03-16 |
| JPWO2020160010A5 true JPWO2020160010A5 (enExample) | 2023-02-01 |
Family
ID=71841934
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021543157A Pending JP2022518778A (ja) | 2019-01-28 | 2020-01-28 | 嚢胞性線維症の治療のための化合物および方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230055237A1 (enExample) |
| EP (1) | EP3917516A4 (enExample) |
| JP (1) | JP2022518778A (enExample) |
| CN (1) | CN113613649A (enExample) |
| WO (1) | WO2020160010A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR118050A1 (es) * | 2019-02-15 | 2021-09-15 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x |
| EP4192794A1 (en) * | 2020-08-06 | 2023-06-14 | Carlex Glass America, LLC | Method of attaching a connector to a glazing |
| EP4029500A1 (en) * | 2021-01-15 | 2022-07-20 | Universidad Autónoma de Madrid | Tetrahydro-spiroindoline-pyrrolopyrrole-triones inhibitors of the nrf2-beta-trcp interaction for use in the treatment of nrf2-related diseases |
| RU2763141C1 (ru) * | 2021-06-29 | 2021-12-27 | Федеральное государственное автономное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" (ПГНИУ) | Этил (3r*,3a'r*,8a'r*,8b's*)-1',2,3'-триоксо-2',5-дифенил-1-(4-хлорфенил)-1,2,2',3',3a',6',7',8',8a',8b'-декагидро-1'h-спиро[пиррол-3,4'-пирроло[3,4-a]пирролизин]-4-карбоксилат, обладающий противомикробной активностью |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101578235B1 (ko) * | 2007-12-10 | 2015-12-16 | 노파르티스 아게 | 유기 화합물 |
| WO2016201440A1 (en) * | 2015-06-12 | 2016-12-15 | The Regents Of The University Of California | Spiroindolinones and therapeutic uses thereof |
| US10072017B2 (en) * | 2015-12-30 | 2018-09-11 | Flatley Discovery Lab, Llc | Compounds and methods for the treatment of cystic fibrosis |
-
2020
- 2020-01-28 JP JP2021543157A patent/JP2022518778A/ja active Pending
- 2020-01-28 WO PCT/US2020/015441 patent/WO2020160010A1/en not_active Ceased
- 2020-01-28 CN CN202080018339.8A patent/CN113613649A/zh active Pending
- 2020-01-28 EP EP20747868.6A patent/EP3917516A4/en not_active Withdrawn
-
2021
- 2021-07-23 US US17/383,797 patent/US20230055237A1/en not_active Abandoned
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