JP2020519625A5 - - Google Patents
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- JP2020519625A5 JP2020519625A5 JP2019562001A JP2019562001A JP2020519625A5 JP 2020519625 A5 JP2020519625 A5 JP 2020519625A5 JP 2019562001 A JP2019562001 A JP 2019562001A JP 2019562001 A JP2019562001 A JP 2019562001A JP 2020519625 A5 JP2020519625 A5 JP 2020519625A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- substituted
- groups
- compound according
- heteroaryl
- 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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- 150000001875 compounds Chemical class 0.000 claims 26
- 125000001072 heteroaryl group Chemical group 0.000 claims 26
- 125000001624 naphthyl group Chemical group 0.000 claims 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 24
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 125000003277 amino group Chemical group 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 14
- -1 (-O)- Chemical class 0.000 claims 12
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 12
- 125000006850 spacer group Chemical group 0.000 claims 12
- 238000000034 method Methods 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- WQZGKKKJIJFFOK-SVZMEOIVSA-N (+)-Galactose Chemical class OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-SVZMEOIVSA-N 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 230000002209 hydrophobic effect Effects 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 150000001413 amino acids Chemical class 0.000 claims 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims 6
- 229930195733 hydrocarbon Natural products 0.000 claims 6
- 150000002430 hydrocarbons Chemical class 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000003132 pyranosyl group Chemical group 0.000 claims 6
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 5
- 150000001720 carbohydrates Chemical class 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 239000004215 Carbon black (E152) Substances 0.000 claims 4
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 4
- 125000000623 heterocyclic group Chemical class 0.000 claims 4
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 206010016654 Fibrosis Diseases 0.000 claims 3
- 102000000802 Galectin 3 Human genes 0.000 claims 3
- 108010001517 Galectin 3 Proteins 0.000 claims 3
- 125000003843 furanosyl group Chemical group 0.000 claims 3
- 150000008195 galaktosides Chemical class 0.000 claims 3
- 239000001257 hydrogen Chemical class 0.000 claims 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 3
- 229910052698 phosphorus Inorganic materials 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 229910052711 selenium Inorganic materials 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims 2
- 239000001177 diphosphate Substances 0.000 claims 2
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 claims 2
- 235000011180 diphosphates Nutrition 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 150000004702 methyl esters Chemical class 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 230000001613 neoplastic effect Effects 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 150000003457 sulfones Chemical class 0.000 claims 2
- PMMURAAUARKVCB-DUVQVXGLSA-N 2-deoxy-D-galactopyranose Chemical class OC[C@H]1OC(O)C[C@@H](O)[C@H]1O PMMURAAUARKVCB-DUVQVXGLSA-N 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 108010001498 Galectin 1 Proteins 0.000 claims 1
- 102100021736 Galectin-1 Human genes 0.000 claims 1
- 102000044445 Galectin-8 Human genes 0.000 claims 1
- 102100031351 Galectin-9 Human genes 0.000 claims 1
- 101710121810 Galectin-9 Proteins 0.000 claims 1
- 102000007563 Galectins Human genes 0.000 claims 1
- 108010046569 Galectins Proteins 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 101000608769 Homo sapiens Galectin-8 Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- XXMPGRFKPAPNJH-UHFFFAOYSA-N N1N=NC=C1.FC1=CC=CC=C1 Chemical compound N1N=NC=C1.FC1=CC=CC=C1 XXMPGRFKPAPNJH-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 239000013256 coordination polymer Substances 0.000 claims 1
- HPXRVTGHNJAIIH-UHFFFAOYSA-N cyclohexanol Chemical compound OC1CCCCC1 HPXRVTGHNJAIIH-UHFFFAOYSA-N 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 229930182830 galactose Natural products 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 235000008935 nutritious Nutrition 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 239000013589 supplement Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 239000011782 vitamin Substances 0.000 claims 1
- 229940088594 vitamin Drugs 0.000 claims 1
- 229930003231 vitamin Natural products 0.000 claims 1
- 235000013343 vitamin Nutrition 0.000 claims 1
- 150000003722 vitamin derivatives Chemical class 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762505544P | 2017-05-12 | 2017-05-12 | |
| US62/505,544 | 2017-05-12 | ||
| PCT/US2018/032349 WO2018209255A1 (en) | 2017-05-12 | 2018-05-11 | Compounds for the prevention and treatment of diseases and the use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020519625A JP2020519625A (ja) | 2020-07-02 |
| JP2020519625A5 true JP2020519625A5 (https=) | 2021-07-26 |
| JP7204676B2 JP7204676B2 (ja) | 2023-01-16 |
Family
ID=64105444
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019562001A Active JP7204676B2 (ja) | 2017-05-12 | 2018-05-11 | 疾患の予防および治療用の化合物およびその使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11576924B2 (https=) |
| EP (1) | EP3621973A4 (https=) |
| JP (1) | JP7204676B2 (https=) |
| KR (1) | KR102626669B1 (https=) |
| CN (1) | CN110869378B (https=) |
| AU (1) | AU2018265571B2 (https=) |
| BR (1) | BR112019023722A2 (https=) |
| CA (1) | CA3062648A1 (https=) |
| IL (1) | IL270469B2 (https=) |
| MX (1) | MX392945B (https=) |
| WO (1) | WO2018209255A1 (https=) |
| ZA (1) | ZA201908165B (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20210100139A (ko) | 2018-12-06 | 2021-08-13 | 브리스톨-마이어스 스큅 컴퍼니 | 갈렉틴-3의 소분자 억제제 |
| CA3122321A1 (en) * | 2018-12-27 | 2020-07-02 | Glycomimetics, Inc. | Galectin-3 inhibiting c-glycosides |
| EP3947407B1 (en) | 2019-03-26 | 2024-06-12 | Bristol-Myers Squibb Company | Small molecule inhibitors of galectin-3 |
| US12269819B2 (en) | 2019-04-10 | 2025-04-08 | Bristol-Myers Squibb Company | Small molecule inhibitors of Galectin-3 |
| CN114206893A (zh) | 2019-08-09 | 2022-03-18 | 爱杜西亚药品有限公司 | (杂)芳基-甲基-硫代-β-D-吡喃半乳糖苷衍生物 |
| WO2021028323A1 (en) | 2019-08-09 | 2021-02-18 | Idorsia Pharmaceuticals Ltd | (2-acetamidyl)thio-beta-d-galactopyranoside derivatives |
| MA56883B1 (fr) | 2019-08-15 | 2025-04-30 | Idorsia Pharmaceuticals Ltd | Dérivés de 2-hydroxycycloalcane-1-carbamoyle |
| CN114585619B (zh) | 2019-08-29 | 2024-09-27 | 爱杜西亚药品有限公司 | α-D-吡喃半乳糖苷衍生物 |
| JP2023508363A (ja) * | 2019-12-24 | 2023-03-02 | グリコミメティクス， インコーポレイテッド | ガレクチン－３阻害性ｃ－グリコシドケトン、エーテル、およびアルコール |
| US12275720B2 (en) * | 2020-05-05 | 2025-04-15 | Bristol-Myers Squibb Company | Small molecule inhibitors of galectin-3 |
| US12286424B2 (en) | 2020-05-11 | 2025-04-29 | Bristol-Myers Squibb Company | Small molecule inhibitors of galectin-3 |
| KR20230018431A (ko) | 2020-05-28 | 2023-02-07 | 브리스톨-마이어스 스큅 컴퍼니 | 갈렉틴-3 억제제 |
| US12312362B2 (en) | 2020-10-06 | 2025-05-27 | Idorsia Pharmaceuticals Ltd | Spiro derivatives of Alpha-D-galactopyranosides |
| EP4237419A1 (en) | 2020-11-02 | 2023-09-06 | Idorsia Pharmaceuticals Ltd | Galectin-3 inhibiting 2-hydroxycycloalkane-1 -carbamoyl derivatives |
| CN116806219A (zh) * | 2021-02-09 | 2023-09-26 | 爱杜西亚药品有限公司 | 羟基杂环烷-氨甲酰基衍生物 |
| RS67032B1 (sr) * | 2021-03-03 | 2025-08-29 | Idorsia Pharmaceuticals Ltd | Alfa-d-galaktopiranozidni derivati supstituisani triazolil-metilom |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3812681A1 (de) * | 1988-04-16 | 1989-11-02 | Bayer Ag | Substituierte n-glycosylamide, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel |
| GB9626450D0 (en) * | 1996-12-20 | 1997-02-05 | Oxford Glycosciences Uk Ltd | Therapeutic compounds |
| SE0100172D0 (sv) | 2001-01-22 | 2001-01-22 | Ulf Nilsson | New inhibitors against galectins |
| US6680306B2 (en) | 2001-06-21 | 2004-01-20 | Glycogenesys, Inc. | Method for enhancing the effectiveness of cancer therapies |
| SE0401301D0 (sv) * | 2004-05-21 | 2004-05-21 | Forskarpatent I Syd Ab | Novel 3-triazolyl-galactoside inhibitors of galectins |
| SE0401300D0 (sv) | 2004-05-21 | 2004-05-21 | Forskarpatent I Syd Ab | Novel Galactoside Inhibitors of Galectins |
| GB0501008D0 (en) * | 2005-01-18 | 2005-02-23 | Amura Therapeutics Ltd | Method of producing conjugate vaccines |
| US9427449B2 (en) | 2005-08-26 | 2016-08-30 | Econugenics, Inc. | Binding of galectin-3 by low molecular weight pectin |
| EP2081961A2 (en) | 2006-11-15 | 2009-07-29 | The Brigham and Women's Hospital, Inc. | Therapeutic uses of tim-3 modulators |
| ES2543063T3 (es) | 2008-05-16 | 2015-08-14 | Galecto Biotech Ab | Nueva síntesis de inhibidores de galactósidos |
| ES2652488T3 (es) * | 2009-04-28 | 2018-02-02 | Galecto Biotech Ab | Nuevos inhibidores de galactósidos de galectinas |
| CN102576028A (zh) | 2009-08-25 | 2012-07-11 | 保函医药公司 | 半乳凝集素-3和心脏再同步疗法 |
| WO2011095772A2 (en) | 2010-02-04 | 2011-08-11 | Summit Corporation Plc | Novel iminosugar therapeutics |
| CA2794066C (en) | 2012-10-31 | 2017-02-28 | Neil Henderson | Galactoside inhibitor of galectins |
| US9243021B2 (en) | 2012-10-31 | 2016-01-26 | Galecto Biotech Ab | Galactoside inhibitor of galectins |
| MX360979B (es) | 2011-09-16 | 2018-11-22 | Galectin Therapeutics Inc | Composiciones de galacto-ramnogalacturonato para el tratamiento de la esteatohepatitis no alcohólica y de la enfermedad del higado graso no alcohólico. |
| MX363923B (es) | 2011-12-28 | 2019-04-08 | Galectin Therapeutics Inc | Composicion de farmaco de carbohidrato novedoso para el tratamiento de enfermedades humanas. |
| EP2620443A1 (en) | 2012-01-25 | 2013-07-31 | Galecto Biotech AB | Novel galactoside inhibitors of galectins |
| DK2906227T3 (en) | 2012-10-10 | 2018-12-10 | Galectin Therapeutics Inc | GALACTOSE-CONTAINING CARBOHYDRATE COMPOUNDS FOR THE TREATMENT OF DIABETIC Nephropathy |
| CN104755088A (zh) | 2012-10-31 | 2015-07-01 | 格莱克特生物技术公司 | 半乳凝集素-3的半乳糖苷抑制剂及其用于治疗肺纤维化的应用 |
| EP2919802A4 (en) | 2012-11-15 | 2016-09-14 | Univ Tufts | METHOD, COMPOSITIONS AND KITS FOR TREATING, MODULATING OR PREVENTING ANGIOGENESIS OR FIBROSIS IN A PATIENT USING A GALECTINE PROTEIN HEMMER |
| AR099707A1 (es) | 2014-03-10 | 2016-08-10 | La Jolla Pharma Co | Composiciones y métodos para tratar trastornos renales |
| WO2015155207A1 (en) | 2014-04-08 | 2015-10-15 | Galecto Biotech Ab | Galactoside inhibitors for the treatment of alpha-synucleinopthies |
| JP6735680B2 (ja) | 2014-07-09 | 2020-08-05 | ガレクト バイオテック エービー | ガレクチンの新規ハイブリッドガラクトシド阻害剤 |
| CA2970062C (en) | 2015-01-30 | 2023-02-28 | Galecto Biotech Ab | Alpha-d-galactoside inhibitors of galectins |
| WO2017019770A1 (en) | 2015-07-27 | 2017-02-02 | Wayne State University | Compositions and methods relating to galectin detection |
| CA3000924A1 (en) | 2015-11-09 | 2017-05-18 | Galecto Biotech Ab | Novel galactoside inhibitors of galectins |
| MX394409B (es) * | 2016-03-04 | 2025-03-24 | Galectin Sciences Llc | Compuestos de seleno-galactosida para la prevención y el tratamiento de las enfermedades asociadas con galectina y el uso de los mismos. |
| KR20200015528A (ko) | 2017-05-12 | 2020-02-12 | 갈랙틴 사이언시즈, 엘엘씨 | 전신 인슐린 내성 질환의 치료용 화합물 및 그의 용도 |
-
2018
- 2018-05-11 EP EP18797833.3A patent/EP3621973A4/en active Pending
- 2018-05-11 CA CA3062648A patent/CA3062648A1/en active Pending
- 2018-05-11 AU AU2018265571A patent/AU2018265571B2/en active Active
- 2018-05-11 US US16/611,609 patent/US11576924B2/en active Active
- 2018-05-11 WO PCT/US2018/032349 patent/WO2018209255A1/en not_active Ceased
- 2018-05-11 BR BR112019023722-4A patent/BR112019023722A2/pt not_active Application Discontinuation
- 2018-05-11 KR KR1020197036413A patent/KR102626669B1/ko active Active
- 2018-05-11 MX MX2019013537A patent/MX392945B/es unknown
- 2018-05-11 JP JP2019562001A patent/JP7204676B2/ja active Active
- 2018-05-11 CN CN201880045752.6A patent/CN110869378B/zh active Active
-
2019
- 2019-11-06 IL IL270469A patent/IL270469B2/en unknown
- 2019-12-09 ZA ZA2019/08165A patent/ZA201908165B/en unknown
-
2022
- 2022-06-08 US US17/835,363 patent/US20230132265A1/en active Pending
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