JP2021503486A5 - - Google Patents
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- JP2021503486A5 JP2021503486A5 JP2020527899A JP2020527899A JP2021503486A5 JP 2021503486 A5 JP2021503486 A5 JP 2021503486A5 JP 2020527899 A JP2020527899 A JP 2020527899A JP 2020527899 A JP2020527899 A JP 2020527899A JP 2021503486 A5 JP2021503486 A5 JP 2021503486A5
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- JP
- Japan
- Prior art keywords
- subject
- pharmaceutical composition
- diabetes
- pancreatic
- tgfβ
- Prior art date
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- 238000000034 method Methods 0.000 claims description 44
- 150000001875 compounds Chemical class 0.000 claims description 26
- 102000004887 Transforming Growth Factor beta Human genes 0.000 claims description 22
- 108090001012 Transforming Growth Factor beta Proteins 0.000 claims description 22
- 239000003112 inhibitor Substances 0.000 claims description 21
- 230000019491 signal transduction Effects 0.000 claims description 16
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 claims description 14
- 108091000080 Phosphotransferase Proteins 0.000 claims description 12
- 102000020233 phosphotransferase Human genes 0.000 claims description 12
- 206010012601 diabetes mellitus Diseases 0.000 claims description 10
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 10
- 125000000217 alkyl group Chemical group 0.000 claims description 9
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- 150000002367 halogens Chemical class 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 108010059616 Activins Proteins 0.000 claims description 6
- 102100026818 Inhibin beta E chain Human genes 0.000 claims description 6
- 239000000488 activin Substances 0.000 claims description 6
- 210000004027 cell Anatomy 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 claims description 6
- 230000003914 insulin secretion Effects 0.000 claims description 5
- 102000007350 Bone Morphogenetic Proteins Human genes 0.000 claims description 4
- 108010007726 Bone Morphogenetic Proteins Proteins 0.000 claims description 4
- 102100028554 Dual specificity tyrosine-phosphorylation-regulated kinase 1A Human genes 0.000 claims description 4
- 101000838016 Homo sapiens Dual specificity tyrosine-phosphorylation-regulated kinase 1A Proteins 0.000 claims description 4
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 4
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 4
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims description 4
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 4
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims description 4
- 229940112869 bone morphogenetic protein Drugs 0.000 claims description 4
- 230000004663 cell proliferation Effects 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 238000002054 transplantation Methods 0.000 claims description 4
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 201000001119 neuropathy Diseases 0.000 claims description 3
- 230000007823 neuropathy Effects 0.000 claims description 3
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 3
- 230000026731 phosphorylation Effects 0.000 claims description 3
- 238000006366 phosphorylation reaction Methods 0.000 claims description 3
- 230000001105 regulatory effect Effects 0.000 claims description 3
- LBPKYPYHDKKRFS-UHFFFAOYSA-N 1,5-naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1h-pyrazol-4-yl]- Chemical compound CC1=CC=CC(C2=C(C=NN2)C=2N=C3C=CC=NC3=CC=2)=N1 LBPKYPYHDKKRFS-UHFFFAOYSA-N 0.000 claims description 2
- 102000018918 Activin Receptors Human genes 0.000 claims description 2
- 108010052946 Activin Receptors Proteins 0.000 claims description 2
- 102000001893 Bone Morphogenetic Protein Receptors Human genes 0.000 claims description 2
- 108010040422 Bone Morphogenetic Protein Receptors Proteins 0.000 claims description 2
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims description 2
- 206010068271 Cystic fibrosis related diabetes Diseases 0.000 claims description 2
- 230000005778 DNA damage Effects 0.000 claims description 2
- 231100000277 DNA damage Toxicity 0.000 claims description 2
- 201000010374 Down Syndrome Diseases 0.000 claims description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 2
- 208000018565 Hemochromatosis Diseases 0.000 claims description 2
- 206010022489 Insulin Resistance Diseases 0.000 claims description 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 2
- 108091005735 TGF-beta receptors Proteins 0.000 claims description 2
- 102000016715 Transforming Growth Factor beta Receptors Human genes 0.000 claims description 2
- 206010044688 Trisomy 21 Diseases 0.000 claims description 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 2
- 102000025151 activin receptor binding proteins Human genes 0.000 claims description 2
- 108091000818 activin receptor binding proteins Proteins 0.000 claims description 2
- 150000001412 amines Chemical class 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 2
- 208000003611 congenital autoimmune diabetes mellitus Diseases 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 229910052805 deuterium Inorganic materials 0.000 claims description 2
- 230000004069 differentiation Effects 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 150000002170 ethers Chemical class 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 239000000893 inhibin Substances 0.000 claims description 2
- ZPNFWUPYTFPOJU-LPYSRVMUSA-N iniprol Chemical compound C([C@H]1C(=O)NCC(=O)NCC(=O)N[C@H]2CSSC[C@H]3C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(N[C@H](C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N[C@@H](CC=4C=CC=CC=4)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC=4C=CC=CC=4)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC2=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H]2N(CCC2)C(=O)[C@@H](N)CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N2[C@@H](CCC2)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)N3)C(=O)NCC(=O)NCC(=O)N[C@@H](C)C(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H](C(=O)N1)C(C)C)[C@@H](C)O)[C@@H](C)CC)=O)[C@@H](C)CC)C1=CC=C(O)C=C1 ZPNFWUPYTFPOJU-LPYSRVMUSA-N 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 150000002825 nitriles Chemical class 0.000 claims description 2
- 230000035935 pregnancy Effects 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 238000002271 resection Methods 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- -1 -CF 3 Chemical class 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 description 2
- 0 C*C(NC1)=**=C1c1cc(C)c(*C(C)=O)cc1 Chemical compound C*C(NC1)=**=C1c1cc(C)c(*C(C)=O)cc1 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762588792P | 2017-11-20 | 2017-11-20 | |
| US62/588,792 | 2017-11-20 | ||
| PCT/US2018/062023 WO2019100062A1 (en) | 2017-11-20 | 2018-11-20 | Kinase inhibitor compounds and compositions and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021503486A JP2021503486A (ja) | 2021-02-12 |
| JP2021503486A5 true JP2021503486A5 (https=) | 2022-01-04 |
Family
ID=66539149
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020527899A Pending JP2021503486A (ja) | 2017-11-20 | 2018-11-20 | キナーゼ阻害剤化合物ならびに組成物および使用法 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11547712B2 (https=) |
| EP (1) | EP3717475B1 (https=) |
| JP (1) | JP2021503486A (https=) |
| CN (1) | CN111936490A (https=) |
| AU (1) | AU2018368790A1 (https=) |
| CA (1) | CA3084581A1 (https=) |
| WO (1) | WO2019100062A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019136320A1 (en) | 2018-01-05 | 2019-07-11 | Icahn School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
| CN112135613A (zh) | 2018-03-20 | 2020-12-25 | 西奈山伊坎医学院 | 激酶抑制剂化合物和组合物及使用方法 |
| US20250340575A1 (en) * | 2024-05-03 | 2025-11-06 | Biosplice Therapeutics, Inc. | 4-aminopyrrolo[2,1-f][1,2,4]triazines and preparation and uses thereof |
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| US11266647B2 (en) | 2016-10-26 | 2022-03-08 | Icahn School Of Medicine At Mount Sinai | Method for increasing cell proliferation in pancreatic beta cells, treatment method, and composition |
| EP3318563A1 (en) | 2016-11-07 | 2018-05-09 | Sanofi | Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders |
| CN110691782A (zh) | 2016-12-01 | 2020-01-14 | 艾普托斯生物科学公司 | 作为brd4和jak2双重抑制剂的稠合的嘧啶化合物及其使用方法 |
| WO2019136320A1 (en) | 2018-01-05 | 2019-07-11 | Icahn School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
| CN112135613A (zh) | 2018-03-20 | 2020-12-25 | 西奈山伊坎医学院 | 激酶抑制剂化合物和组合物及使用方法 |
| WO2020142485A1 (en) | 2018-12-31 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| JP2022515650A (ja) | 2018-12-31 | 2022-02-21 | アイカーン スクール オブ メディシン アット マウント サイナイ | キナーゼ阻害剤化合物及び組成物ならびに使用方法 |
-
2018
- 2018-11-20 WO PCT/US2018/062023 patent/WO2019100062A1/en not_active Ceased
- 2018-11-20 CA CA3084581A patent/CA3084581A1/en active Pending
- 2018-11-20 US US16/765,542 patent/US11547712B2/en active Active
- 2018-11-20 AU AU2018368790A patent/AU2018368790A1/en not_active Abandoned
- 2018-11-20 JP JP2020527899A patent/JP2021503486A/ja active Pending
- 2018-11-20 CN CN201880087073.5A patent/CN111936490A/zh active Pending
- 2018-11-20 EP EP18878625.5A patent/EP3717475B1/en active Active
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