JP2018536641A5 - - Google Patents
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- JP2018536641A5 JP2018536641A5 JP2018520090A JP2018520090A JP2018536641A5 JP 2018536641 A5 JP2018536641 A5 JP 2018536641A5 JP 2018520090 A JP2018520090 A JP 2018520090A JP 2018520090 A JP2018520090 A JP 2018520090A JP 2018536641 A5 JP2018536641 A5 JP 2018536641A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- optionally substituted
- formula
- iron
- membered
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 50
- XEEYBQQBJWHFJM-UHFFFAOYSA-N iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 36
- 229910052757 nitrogen Inorganic materials 0.000 claims 19
- 229910052742 iron Inorganic materials 0.000 claims 18
- 125000001424 substituent group Chemical group 0.000 claims 14
- 229910052799 carbon Inorganic materials 0.000 claims 12
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 6
- 125000005842 heteroatoms Chemical group 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 6
- 206010065973 Iron overload Diseases 0.000 claims 5
- 238000010521 absorption reaction Methods 0.000 claims 5
- 238000002648 combination therapy Methods 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- 206010001897 Alzheimer's disease Diseases 0.000 claims 3
- 206010053643 Neurodegenerative disease Diseases 0.000 claims 3
- 206010061536 Parkinson's disease Diseases 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- PMATZTZNYRCHOR-CGLBZJNRSA-N (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-ethyl-33-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17 Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 2
- 208000007502 Anemia Diseases 0.000 claims 2
- 206010010356 Congenital anomaly Diseases 0.000 claims 2
- ZIUSSTSXXLLKKK-HWUZOJPISA-N Curcumin Natural products C1=C(O)C(OC)=CC(\C=C\C(\O)=C/C(=O)/C=C/C=2C=C(OC)C(O)=CC=2)=C1 ZIUSSTSXXLLKKK-HWUZOJPISA-N 0.000 claims 2
- 206010022979 Iron excess Diseases 0.000 claims 2
- 102100017041 SLC40A1 Human genes 0.000 claims 2
- 108091006892 SLC40A1 Proteins 0.000 claims 2
- 208000002903 Thalassemia Diseases 0.000 claims 2
- 201000006288 alpha thalassemia Diseases 0.000 claims 2
- 244000052616 bacterial pathogens Species 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- YCKRFDGAMUMZLT-UHFFFAOYSA-N fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 201000003793 myelodysplastic syndrome Diseases 0.000 claims 2
- 239000003642 reactive oxygen metabolite Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- TZXKOCQBRNJULO-UHFFFAOYSA-N 1,2-Dimethyl-3-hydroxypyrid-4-one Chemical compound CC1=C(O)C(=O)C=CN1C TZXKOCQBRNJULO-UHFFFAOYSA-N 0.000 claims 1
- WTDRDQBEARUVNC-LURJTMIESA-N 3-hydroxy-L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 229960004308 ACETYLCYSTEINE Drugs 0.000 claims 1
- 229960004676 ANTITHROMBOTIC AGENTS Drugs 0.000 claims 1
- 229940064005 Antibiotic throat preparations Drugs 0.000 claims 1
- 229940083879 Antibiotics FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE Drugs 0.000 claims 1
- 229940042052 Antibiotics for systemic use Drugs 0.000 claims 1
- 229940042786 Antitubercular Antibiotics Drugs 0.000 claims 1
- 229940109262 Curcumin Drugs 0.000 claims 1
- 108010036949 Cyclosporine Proteins 0.000 claims 1
- 229960001489 Deferasirox Drugs 0.000 claims 1
- FMSOAWSKCWYLBB-VBGLAJCLSA-N Deferasirox Chemical compound C1=CC(C(=O)O)=CC=C1N(N\C(N\1)=C\2C(C=CC=C/2)=O)C/1=C\1C(=O)C=CC=C/1 FMSOAWSKCWYLBB-VBGLAJCLSA-N 0.000 claims 1
- 229960000958 Deferoxamine Drugs 0.000 claims 1
- 229940052760 Dopamine agonists Drugs 0.000 claims 1
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims 1
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 1
- 229940093922 Gynecological Antibiotics Drugs 0.000 claims 1
- 206010018872 Haemochromatosis Diseases 0.000 claims 1
- 206010053215 Haemoglobin E disease Diseases 0.000 claims 1
- 208000007475 Hemolytic Anemia Diseases 0.000 claims 1
- 206010020718 Hyperplasia Diseases 0.000 claims 1
- 229960003444 IMMUNOSUPPRESSANTS Drugs 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 102000006992 Interferon-alpha Human genes 0.000 claims 1
- 108010047761 Interferon-alpha Proteins 0.000 claims 1
- 206010022983 Iron metabolism disease Diseases 0.000 claims 1
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims 1
- 210000004185 Liver Anatomy 0.000 claims 1
- UBQYURCVBFRUQT-UHFFFAOYSA-N N-benzoyl-Ferrioxamine B Chemical compound CC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCN UBQYURCVBFRUQT-UHFFFAOYSA-N 0.000 claims 1
- 108009000578 Oxidative Stress Proteins 0.000 claims 1
- IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 claims 1
- 229960000329 Ribavirin Drugs 0.000 claims 1
- 208000007056 Sickle Cell Anemia Diseases 0.000 claims 1
- 206010043390 Thalassaemia alpha Diseases 0.000 claims 1
- NLVFBUXFDBBNBW-PBSUHMDJSA-N Tobramycin Chemical compound N[C@@H]1C[C@H](O)[C@@H](CN)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O2)O)[C@H](N)C[C@@H]1N NLVFBUXFDBBNBW-PBSUHMDJSA-N 0.000 claims 1
- 229960000707 Tobramycin Drugs 0.000 claims 1
- 229940024982 Topical Antifungal Antibiotics Drugs 0.000 claims 1
- 229960003165 Vancomycin Drugs 0.000 claims 1
- 108010059993 Vancomycin Proteins 0.000 claims 1
- 241000607265 Vibrio vulnificus Species 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000003110 anti-inflammatory Effects 0.000 claims 1
- 230000000111 anti-oxidant Effects 0.000 claims 1
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 239000003429 antifungal agent Substances 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 208000005980 beta-Thalassemia Diseases 0.000 claims 1
- 230000003115 biocidal Effects 0.000 claims 1
- 239000003124 biologic agent Substances 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000002738 chelating agent Substances 0.000 claims 1
- 238000004587 chromatography analysis Methods 0.000 claims 1
- 229960001265 ciclosporin Drugs 0.000 claims 1
- 229940000425 combination drugs Drugs 0.000 claims 1
- 235000012754 curcumin Nutrition 0.000 claims 1
- 239000004148 curcumin Substances 0.000 claims 1
- 229960003266 deferiprone Drugs 0.000 claims 1
- 208000006602 delta-Thalassemia Diseases 0.000 claims 1
- 201000009910 diseases by infectious agent Diseases 0.000 claims 1
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002124 endocrine Effects 0.000 claims 1
- 230000000925 erythroid Effects 0.000 claims 1
- 238000005755 formation reaction Methods 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 201000002433 hemoglobin H disease Diseases 0.000 claims 1
- 102000018511 hepcidin family Human genes 0.000 claims 1
- 108060003558 hepcidin family Proteins 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 230000001861 immunosuppresant Effects 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000000297 inotrophic Effects 0.000 claims 1
- 229940079866 intestinal antibiotics Drugs 0.000 claims 1
- 229960004502 levodopa Drugs 0.000 claims 1
- 201000004792 malaria Diseases 0.000 claims 1
- 230000001404 mediated Effects 0.000 claims 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229940005935 ophthalmologic Antibiotics Drugs 0.000 claims 1
- 230000036542 oxidative stress Effects 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000000069 prophylaxis Effects 0.000 claims 1
- 125000002098 pyridazinyl 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
- 239000000018 receptor agonist Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 241000894007 species Species 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 210000001519 tissues Anatomy 0.000 claims 1
- MYPYJXKWCTUITO-LYRMYLQWSA-O vancomycin(1+) Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C([O-])=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)[NH2+]C)[C@H]1C[C@](C)([NH3+])[C@H](O)[C@H](C)O1 MYPYJXKWCTUITO-LYRMYLQWSA-O 0.000 claims 1
- 230000000033 vasopressor Effects 0.000 claims 1
- 235000019195 vitamin supplement Nutrition 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15191179 | 2015-10-23 | ||
| EP15191179.9 | 2015-10-23 | ||
| EP15191176 | 2015-10-23 | ||
| EP15191176.5 | 2015-10-23 | ||
| PCT/EP2016/075305 WO2017068089A2 (en) | 2015-10-23 | 2016-10-21 | Novel ferroportin inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018536641A JP2018536641A (ja) | 2018-12-13 |
| JP2018536641A5 true JP2018536641A5 (US07846941-20101207-C00217.png) | 2019-04-25 |
| JP6810988B2 JP6810988B2 (ja) | 2021-01-13 |
Family
ID=57178421
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018520089A Active JP6710754B2 (ja) | 2015-10-23 | 2016-10-21 | 新規なフェロポーチン阻害剤 |
| JP2018520090A Active JP6810988B2 (ja) | 2015-10-23 | 2016-10-21 | 新規なフェロポーチン阻害剤 |
| JP2020091830A Active JP6967112B2 (ja) | 2015-10-23 | 2020-05-27 | 新規なフェロポーチン阻害剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018520089A Active JP6710754B2 (ja) | 2015-10-23 | 2016-10-21 | 新規なフェロポーチン阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020091830A Active JP6967112B2 (ja) | 2015-10-23 | 2020-05-27 | 新規なフェロポーチン阻害剤 |
Country Status (22)
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2968443T3 (pl) | 2013-03-15 | 2022-02-07 | Protagonist Therapeutics, Inc. | Analogi hepcydyny i ich zastosowania |
| TWI722031B (zh) | 2015-10-23 | 2021-03-21 | 瑞士商威佛（國際）股份有限公司 | 新穎的膜鐵運輸蛋白（ｆｅｒｒｏｐｏｒｔｉｎ）抑制劑 |
| JOP20180036A1 (ar) | 2017-04-18 | 2019-01-30 | Vifor Int Ag | أملاح لمثبطات فروبورتين جديدة |
| CN108314687A (zh) * | 2017-12-27 | 2018-07-24 | 重庆文理学院 | 1,2-二氢苯并[4,5]咪唑并[1,2-a]吡嗪-3（4H）-酮衍生物的合成 |
| EP3749345A4 (en) | 2018-02-08 | 2022-04-06 | Protagonist Therapeutics, Inc. | CONJUGATED HEPCIDIN MIMETICS |
| US20210252106A1 (en) * | 2018-04-30 | 2021-08-19 | The Children's Hospital Of Philadelphia | Methods of improving anemias by combining agents |
| EP3894416B1 (en) | 2018-12-13 | 2022-11-09 | Global Blood Therapeutics, Inc. | Ferroportin inhibitors and methods of use |
| TW202102478A (zh) | 2019-04-01 | 2021-01-16 | 瑞士商威佛（國際）股份有限公司 | 新穎的鐵螯合物 |
| US20220273634A1 (en) * | 2019-07-19 | 2022-09-01 | Vifor (International) Ag | Ferroportin-Inhibitors For The Use In The Treatment Of Transfusion-Dependent Beta-Thalassemia (TDT) |
| BR112022001063A2 (pt) * | 2019-07-19 | 2022-03-15 | Vifor Int Ag | Inibidores de ferroportina para o uso na prevenção e tratamento de lesões renais |
| EP3782702A1 (en) * | 2019-08-21 | 2021-02-24 | AC BioScience SA | Compounds and use thereof for the treatment of infectious diseases and cancer |
| EP4025592A4 (en) | 2019-09-03 | 2023-08-02 | Protagonist Therapeutics, Inc. | CONJUGATED HEPCIDIN MIMETICS |
| CA3154524A1 (en) | 2019-10-22 | 2021-04-21 | Vania Manolova | Methods and compositions for treating sickle cell disease with a ferroportin inhibitor (vit-2763) |
| AU2021243494A1 (en) | 2020-03-24 | 2022-08-25 | Vifor (International) Ag | Process for the production of ferroportin inhibitors |
| GB202012969D0 (en) * | 2020-08-19 | 2020-09-30 | Univ Of Oxford | Inhibitor compounds |
| EP4281072A1 (en) | 2021-01-20 | 2023-11-29 | Vifor (International) Ag | Ferroportin-inhibitors for the use in the treatment of myelodysplastic syndromes (mds) |
| WO2022173818A1 (en) * | 2021-02-09 | 2022-08-18 | University Of Virginia Patent Foundation | Use of biliverdin reductase b inhibitors to allow malaria eradication in patients with g6pd deficiency |
| TW202304896A (zh) | 2021-04-22 | 2023-02-01 | 瑞士商威佛（國際）股份有限公司 | 經修飾的膜鐵運輸蛋白(ferroportin)抑制劑 |
| AU2022353058A1 (en) | 2021-09-21 | 2024-03-21 | Vifor (International) Ag | N-substituted ferroportin inhibitors |
| WO2024083980A1 (en) | 2022-10-21 | 2024-04-25 | Vifor (International) Ag | Bicyclic ferroportin inhibitors |
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