CN111699193A

CN111699193A - 新型半乳糖苷类半乳凝素抑制剂

新型半乳糖苷类半乳凝素抑制剂 Download PDF

Info

Publication number: CN111699193A
Authority: CN; China
Prior art keywords: deoxy; galactopyranoside; thio; triazol; alpha
Prior art date: 2018-01-10
Legal status : Pending

Application number

CN201980007910.3A

Other languages

English (en)

Chinese (zh)

Inventor

F·塞特贝里

Current Assignee

Galecto Biotech AB

Original Assignee

Galecto Biotech AB

Priority date

2018-01-10

Filing date

2019-01-09

Publication date

2020-09-22

2019-01-09 Application filed by Galecto Biotech AB filed Critical Galecto Biotech AB

2020-09-22 Publication of CN111699193A publication Critical patent/CN111699193A/zh

Status Pending legal-status Critical Current

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102000007563 Galectins Human genes 0.000 title abstract description 43
108010046569 Galectins Proteins 0.000 title abstract description 43
239000003112 inhibitor Substances 0.000 title description 31
150000008195 galaktosides Chemical class 0.000 title description 2
150000001875 compounds Chemical class 0.000 claims abstract description 259
108010001498 Galectin 1 Proteins 0.000 claims abstract description 59
238000000034 method Methods 0.000 claims abstract description 32
WQZGKKKJIJFFOK-PHYPRBDBSA-N alpha-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 claims abstract description 16
241000124008 Mammalia Species 0.000 claims abstract description 15
125000001072 heteroaryl group Chemical group 0.000 claims abstract description 15
230000027455 binding Effects 0.000 claims abstract description 12
229960003082 galactose Drugs 0.000 claims abstract description 11
239000003446 ligand Substances 0.000 claims abstract description 10
125000004432 carbon atom Chemical group C* 0.000 claims abstract description 9
229910052799 carbon Inorganic materials 0.000 claims abstract description 5
GZCGUPFRVQAUEE-UHFFFAOYSA-N alpha-D-galactose Natural products OCC(O)C(O)C(O)C(O)C=O GZCGUPFRVQAUEE-UHFFFAOYSA-N 0.000 claims abstract description 4
WQZGKKKJIJFFOK-UHFFFAOYSA-N alpha-D-glucopyranose Natural products OCC1OC(O)C(O)C(O)C1O WQZGKKKJIJFFOK-UHFFFAOYSA-N 0.000 claims abstract description 4
150000003214 pyranose derivatives Chemical group 0.000 claims abstract description 4
102000000795 Galectin 1 Human genes 0.000 claims abstract 3
-1 d-galactopyranose compound Chemical class 0.000 claims description 204
229910052736 halogen Inorganic materials 0.000 claims description 59
150000002367 halogens Chemical class 0.000 claims description 59
206010028980 Neoplasm Diseases 0.000 claims description 38
229910052757 nitrogen Inorganic materials 0.000 claims description 34
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229910052794 bromium Inorganic materials 0.000 claims description 22
239000001257 hydrogen Substances 0.000 claims description 21
229910052739 hydrogen Inorganic materials 0.000 claims description 21
206010016654 Fibrosis Diseases 0.000 claims description 19
230000004761 fibrosis Effects 0.000 claims description 19
239000003814 drug Substances 0.000 claims description 18
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
238000011282 treatment Methods 0.000 claims description 18
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 17
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125000000623 heterocyclic group Chemical group 0.000 claims description 5
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