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
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- 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 |
|---|---|---|---|---|
| JP2022511094A (ja) | 2018-12-06 | 2022-01-28 | ブリストル－マイヤーズ スクイブ カンパニー | ガレクチン－３の低分子阻害剤 |
| CN118373810A (zh) * | 2018-12-27 | 2024-07-23 | 糖模拟物有限公司 | 抑制c-糖苷的半乳凝素-3 |
| EP3947407B1 (en) * | 2019-03-26 | 2024-06-12 | Bristol-Myers Squibb Company | Small molecule inhibitors of galectin-3 |
| EP3953349A1 (en) | 2019-04-10 | 2022-02-16 | Bristol-Myers Squibb Company | Small molecule inhibitors of galectin-3 |
| EP4010348B1 (en) | 2019-08-09 | 2023-12-20 | Idorsia Pharmaceuticals Ltd | (2-acetamidyl)thio-beta-d-galactopyranoside derivatives |
| 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 |
| JP7604457B2 (ja) | 2019-08-15 | 2024-12-23 | イドルシア・ファーマシューティカルズ・リミテッド | ２－ヒドロキシシクロアルカン－１－カルバモイル誘導体 |
| CA3148365A1 (en) | 2019-08-29 | 2021-03-04 | Martin Bolli | Alpha-d-galactopyranoside derivatives |
| CA3161794A1 (en) * | 2019-12-24 | 2021-07-01 | John L. Magnani | Galectin-3 inhibiting c-glycoside ketones, ethers, and alcohols |
| KR20230006547A (ko) * | 2020-05-05 | 2023-01-10 | 브리스톨-마이어스 스큅 컴퍼니 | 갈렉틴-3의 소분자 억제제 |
| EP4149939A1 (en) | 2020-05-11 | 2023-03-22 | Bristol-Myers Squibb Company | Small molecule inhibitors of galectin-3 |
| EP4157833A1 (en) | 2020-05-28 | 2023-04-05 | Bristol-Myers Squibb Company | Galectin-3 inhibitors |
| ES3014851T3 (en) * | 2020-10-06 | 2025-04-25 | Idorsia Pharmaceuticals Ltd | Spiro derivatives of alpha-d-galactopyranosides |
| KR20230104190A (ko) | 2020-11-02 | 2023-07-07 | 이도르시아 파마슈티컬스 리미티드 | 갈렉틴-3 억제 2-히드록시시클로알칸-1-카르바모일 유도체 |
| KR20230145111A (ko) * | 2021-02-09 | 2023-10-17 | 이도르시아 파마슈티컬스 리미티드 | 히드록시헤테로시클로알칸-카르바모일 유도체 |
| PL4301748T3 (pl) * | 2021-03-03 | 2025-09-08 | Idorsia Pharmaceuticals Ltd | Triazolilo-metylo podstawione pochodne alfa-d-galaktopiranozydu |
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 |
| CA2668693A1 (en) | 2006-11-15 | 2008-05-22 | David E. Anderson | Therapeutic uses of tim-3 modulators |
| US8697862B2 (en) | 2008-05-16 | 2014-04-15 | Galecto Biotech Ab | Synthesis of galactoside inhibitors |
| CN102439021B (zh) | 2009-04-28 | 2015-09-02 | 格莱克特生物技术公司 | 半乳凝素的新型半乳糖苷抑制剂 |
| BR112012008063A2 (pt) | 2009-08-25 | 2016-11-22 | Bg Medicine Inc | galectina-3 e terapia de ressincronização cardíaca. |
| 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 |
| ES2869884T3 (es) | 2011-09-16 | 2021-10-26 | Galectin Therapeutics Inc | Composiciones de galacto-ramnogalacturonato para el tratamiento de la esteatohepatitis no alcohólica y la enfermedad de hígado graso no alcohólico |
| AU2012363033B2 (en) | 2011-12-28 | 2016-06-02 | Galectin Therapeutics, Inc. | Composition of novel carbohydrate drug for treatment of human diseases |
| EP2620443A1 (en) | 2012-01-25 | 2013-07-31 | Galecto Biotech AB | Novel galactoside inhibitors of galectins |
| US8828971B2 (en) | 2012-10-10 | 2014-09-09 | Galectin Therapeutics, Inc. | Galactose-pronged carbohydrate compounds for the treatment of diabetic nephropathy and associated disorders |
| JP2015535233A (ja) | 2012-10-31 | 2015-12-10 | ガレクト・バイオテック・エイビイ | ガレクチン−３のガラクトシド阻害剤及び肺線維症のためのその使用 |
| WO2014078655A1 (en) | 2012-11-15 | 2014-05-22 | Tufts University | Methods, compositions and kits for treating, modulating, or preventing ocular angiogenesis or fibrosis in a subject using a galectin protein inhibitor |
| JP2017512205A (ja) | 2014-03-10 | 2017-05-18 | ラ ホヤ ファーマシューティカル カンパニーＬａ Ｊｏｌｌａ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｃｏｍｐａｎｙ | 腎臓障害を治療するための組成物及び方法 |
| EP3129032A1 (en) | 2014-04-08 | 2017-02-15 | Galecto Biotech AB | Galactoside inhibitors for the treatment of alpha-synucleinopthies |
| EP3415522A1 (en) | 2014-07-09 | 2018-12-19 | Galecto Biotech AB | Novel hybrid galactoside inhibitor of galectins |
| JP6904906B2 (ja) | 2015-01-30 | 2021-07-21 | ガレクト・バイオテック・エイビイ | ガレクチンの新規なガラクトシド阻害剤 |
| WO2017019770A1 (en) | 2015-07-27 | 2017-02-02 | Wayne State University | Compositions and methods relating to galectin detection |
| ES2921500T3 (es) | 2015-11-09 | 2022-08-26 | Galecto Biotech Ab | 1,1'-sulfanodiil-di-beta-d-galactopiranósidos como inhibidores de galectinas |
| JP7086008B2 (ja) * | 2016-03-04 | 2022-06-17 | ガレクティン・サイエンシーズ・リミテッド・ライアビリティ・カンパニー | ガレクチンに関連する疾患を予防および処置するためのセレノガラクトシド化合物およびその使用 |
| US20200061095A1 (en) | 2017-05-12 | 2020-02-27 | Galectin Sciences, Llc | Compounds for the Treatment of Systemic Insulin Resistance Disorders and the Use Thereof |
-
2018
- 2018-05-11 CA CA3062648A patent/CA3062648A1/en active Pending
- 2018-05-11 JP JP2019562001A patent/JP7204676B2/ja active Active
- 2018-05-11 EP EP18797833.3A patent/EP3621973A4/en active Pending
- 2018-05-11 WO PCT/US2018/032349 patent/WO2018209255A1/en not_active Ceased
- 2018-05-11 MX MX2019013537A patent/MX392945B/es unknown
- 2018-05-11 US US16/611,609 patent/US11576924B2/en active Active
- 2018-05-11 KR KR1020197036413A patent/KR102626669B1/ko active Active
- 2018-05-11 AU AU2018265571A patent/AU2018265571B2/en active Active
- 2018-05-11 BR BR112019023722-4A patent/BR112019023722A2/pt not_active Application Discontinuation
- 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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