JP2021119140A5 - - Google Patents
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- JP2021119140A5 JP2021119140A5 JP2021065309A JP2021065309A JP2021119140A5 JP 2021119140 A5 JP2021119140 A5 JP 2021119140A5 JP 2021065309 A JP2021065309 A JP 2021065309A JP 2021065309 A JP2021065309 A JP 2021065309A JP 2021119140 A5 JP2021119140 A5 JP 2021119140A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- butyl
- tetrahydro
- naphthylidine
- butanoic acid
- 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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- -1 pyrazolopyrimidinyl Chemical group 0.000 claims description 314
- 125000000217 alkyl group Chemical group 0.000 claims description 181
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 171
- 229910052805 deuterium Inorganic materials 0.000 claims description 171
- 229910052736 halogen Inorganic materials 0.000 claims description 152
- 150000002367 halogens Chemical class 0.000 claims description 140
- 150000001875 compounds Chemical class 0.000 claims description 133
- 150000003839 salts Chemical class 0.000 claims description 114
- 125000004043 oxo group Chemical group O=* 0.000 claims description 107
- 239000008194 pharmaceutical composition Substances 0.000 claims description 81
- 125000001072 heteroaryl group Chemical group 0.000 claims description 62
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 60
- 125000000623 heterocyclic group Chemical group 0.000 claims description 59
- 125000003118 aryl group Chemical group 0.000 claims description 50
- 125000003545 alkoxy group Chemical group 0.000 claims description 49
- 125000001188 haloalkyl group Chemical group 0.000 claims description 48
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 46
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 44
- 229910052739 hydrogen Inorganic materials 0.000 claims description 37
- 239000001257 hydrogen Substances 0.000 claims description 37
- 125000001153 fluoro group Chemical group F* 0.000 claims description 32
- 102000006495 integrins Human genes 0.000 claims description 31
- 108010044426 integrins Proteins 0.000 claims description 31
- 125000000304 alkynyl group Chemical group 0.000 claims description 30
- 201000010099 disease Diseases 0.000 claims description 26
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 26
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 24
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 22
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 20
- 229910052799 carbon Inorganic materials 0.000 claims description 19
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 18
- 230000003176 fibrotic effect Effects 0.000 claims description 18
- 150000002431 hydrogen Chemical class 0.000 claims description 16
- 125000004429 atom Chemical group 0.000 claims description 15
- 230000000694 effects Effects 0.000 claims description 15
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 13
- 125000004431 deuterium atom Chemical group 0.000 claims description 12
- 125000005843 halogen group Chemical group 0.000 claims description 12
- 230000002401 inhibitory effect Effects 0.000 claims description 10
- 125000004076 pyridyl group Chemical group 0.000 claims description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 10
- 230000005764 inhibitory process Effects 0.000 claims description 9
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 8
- 208000010157 sclerosing cholangitis Diseases 0.000 claims description 8
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims description 7
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims description 6
- 229910052731 fluorine Inorganic materials 0.000 claims description 6
- 239000011737 fluorine Substances 0.000 claims description 6
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 6
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 5
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 5
- 230000001105 regulatory effect Effects 0.000 claims description 5
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000005347 halocycloalkyl group Chemical group 0.000 claims description 4
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 4
- 125000004254 isoquinolin-1-yl group Chemical group [H]C1=C([H])C2=C([H])C([H])=C([H])C([H])=C2C(*)=N1 0.000 claims description 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 4
- 125000004262 quinoxalin-2-yl group Chemical group [H]C1=NC2=C([H])C([H])=C([H])C([H])=C2N=C1* 0.000 claims description 4
- 102000004887 Transforming Growth Factor beta Human genes 0.000 claims description 3
- 108090001012 Transforming Growth Factor beta Proteins 0.000 claims description 3
- 230000004913 activation Effects 0.000 claims description 3
- 230000033228 biological regulation Effects 0.000 claims description 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 3
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 3
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 claims description 2
- VFZYCYBBIMIWOZ-UHFFFAOYSA-N 2-ethoxy-2-hydroxy-2-methoxyacetamide Chemical compound OC(C(=O)N)(OCC)OC VFZYCYBBIMIWOZ-UHFFFAOYSA-N 0.000 claims description 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 2
- 206010010317 Congenital absence of bile ducts Diseases 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 2
- 125000003282 alkyl amino group Chemical group 0.000 claims description 2
- 125000004104 aryloxy group Chemical group 0.000 claims description 2
- 229940049706 benzodiazepine Drugs 0.000 claims description 2
- 201000005271 biliary atresia Diseases 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 2
- 230000002496 gastric effect Effects 0.000 claims description 2
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 2
- HBGXFJGNUSQCKP-UHFFFAOYSA-N n-methyl-1-phenoxymethanamine Chemical compound CNCOC1=CC=CC=C1 HBGXFJGNUSQCKP-UHFFFAOYSA-N 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 2
- 201000002793 renal fibrosis Diseases 0.000 claims description 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 350
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 254
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 218
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 36
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 28
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 15
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims 8
- HNEGJTWNOOWEMH-UHFFFAOYSA-N 1-fluoropropane Chemical group [CH2]CCF HNEGJTWNOOWEMH-UHFFFAOYSA-N 0.000 claims 7
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 5
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 4
- BQDJLAWUTBCDHK-UHFFFAOYSA-N 2-(trifluoromethyl)pyrimidine Chemical compound FC(F)(F)C1=NC=CC=N1 BQDJLAWUTBCDHK-UHFFFAOYSA-N 0.000 claims 3
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 3
- CPCHRGFQWZMVNX-UHFFFAOYSA-N 5-(trifluoromethyl)pyrimidine Chemical compound FC(F)(F)C1=CN=CN=C1 CPCHRGFQWZMVNX-UHFFFAOYSA-N 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- LVXOXXGCJHYEOS-UHFFFAOYSA-N 5-phenylpyrimidine Chemical compound C1=CC=CC=C1C1=CN=CN=C1 LVXOXXGCJHYEOS-UHFFFAOYSA-N 0.000 claims 2
- HJKGBRPNSJADMB-UHFFFAOYSA-N beta-Phenylpyridine Natural products C1=CC=CC=C1C1=CC=CN=C1 HJKGBRPNSJADMB-UHFFFAOYSA-N 0.000 claims 2
- 230000002685 pulmonary effect Effects 0.000 claims 2
- WWSQPSBEFSUKKH-UHFFFAOYSA-N 2-(trifluoromethyl)quinazoline Chemical compound C1=CC=CC2=NC(C(F)(F)F)=NC=C21 WWSQPSBEFSUKKH-UHFFFAOYSA-N 0.000 claims 1
- DXPQTHAFYUTZRR-UHFFFAOYSA-N 2-methylquinazoline Chemical compound C1=CC=CC2=NC(C)=NC=C21 DXPQTHAFYUTZRR-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- MKLQPIYLZMLAER-UHFFFAOYSA-N 4-phenylpyrimidine Chemical compound C1=CC=CC=C1C1=CC=NC=N1 MKLQPIYLZMLAER-UHFFFAOYSA-N 0.000 claims 1
- JBRWPSRNDWASJF-UHFFFAOYSA-N 7-(trifluoromethyl)quinazoline Chemical compound C1=NC=NC2=CC(C(F)(F)F)=CC=C21 JBRWPSRNDWASJF-UHFFFAOYSA-N 0.000 claims 1
- QZMGIRFTPNSHNZ-UHFFFAOYSA-N 8-(trifluoromethyl)quinazoline Chemical compound N1=CN=C2C(C(F)(F)F)=CC=CC2=C1 QZMGIRFTPNSHNZ-UHFFFAOYSA-N 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000006005 fluoroethoxy group Chemical group 0.000 claims 1
- 230000002440 hepatic effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- UDJFFSGCRRMVFH-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine Chemical compound N1=CN=CC2=CC=CN=C21 UDJFFSGCRRMVFH-UHFFFAOYSA-N 0.000 claims 1
- BWESROVQGZSBRX-UHFFFAOYSA-N pyrido[3,2-d]pyrimidine Chemical compound C1=NC=NC2=CC=CN=C21 BWESROVQGZSBRX-UHFFFAOYSA-N 0.000 claims 1
- PAQYIEZTLSDLQO-UHFFFAOYSA-N pyrido[3,4-d]pyrimidine Chemical compound N1=CN=C2C=NC=CC2=C1 PAQYIEZTLSDLQO-UHFFFAOYSA-N 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 238000000034 method Methods 0.000 description 15
- 125000003342 alkenyl group Chemical group 0.000 description 9
- 150000001345 alkine derivatives Chemical class 0.000 description 7
- 206010016654 Fibrosis Diseases 0.000 description 3
- 230000004761 fibrosis Effects 0.000 description 3
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 2
- 208000029523 Interstitial Lung disease Diseases 0.000 description 2
- 230000001476 alcoholic effect Effects 0.000 description 2
- 230000009787 cardiac fibrosis Effects 0.000 description 2
- 208000033679 diabetic kidney disease Diseases 0.000 description 2
- 208000005069 pulmonary fibrosis Diseases 0.000 description 2
- 208000024985 Alport syndrome Diseases 0.000 description 1
- 206010004664 Biliary fibrosis Diseases 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 206010019668 Hepatic fibrosis Diseases 0.000 description 1
- 208000034189 Sclerosis Diseases 0.000 description 1
- 201000009594 Systemic Scleroderma Diseases 0.000 description 1
- 206010042953 Systemic sclerosis Diseases 0.000 description 1
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- 208000020832 chronic kidney disease Diseases 0.000 description 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 description 1
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 description 1
- 208000006454 hepatitis Diseases 0.000 description 1
- 231100000283 hepatitis Toxicity 0.000 description 1
- 208000003215 hereditary nephritis Diseases 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023074346A JP7624025B2 (ja) | 2018-03-07 | 2023-04-28 | アミノ酸化合物および使用方法 |
| JP2025006716A JP2025081308A (ja) | 2018-03-07 | 2025-01-17 | アミノ酸化合物および使用方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862639988P | 2018-03-07 | 2018-03-07 | |
| US62/639,988 | 2018-03-07 | ||
| US201862690933P | 2018-06-27 | 2018-06-27 | |
| US62/690,933 | 2018-06-27 | ||
| JP2020521559A JP6866535B2 (ja) | 2018-03-07 | 2019-03-07 | アミノ酸化合物および使用方法 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020521559A Division JP6866535B2 (ja) | 2018-03-07 | 2019-03-07 | アミノ酸化合物および使用方法 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023074346A Division JP7624025B2 (ja) | 2018-03-07 | 2023-04-28 | アミノ酸化合物および使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021119140A JP2021119140A (ja) | 2021-08-12 |
| JP2021119140A5 true JP2021119140A5 (enExample) | 2022-03-14 |
| JP7273882B2 JP7273882B2 (ja) | 2023-05-15 |
Family
ID=67844341
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020521559A Active JP6866535B2 (ja) | 2018-03-07 | 2019-03-07 | アミノ酸化合物および使用方法 |
| JP2021065309A Active JP7273882B2 (ja) | 2018-03-07 | 2021-04-07 | アミノ酸化合物および使用方法 |
| JP2023074346A Active JP7624025B2 (ja) | 2018-03-07 | 2023-04-28 | アミノ酸化合物および使用方法 |
| JP2025006716A Pending JP2025081308A (ja) | 2018-03-07 | 2025-01-17 | アミノ酸化合物および使用方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020521559A Active JP6866535B2 (ja) | 2018-03-07 | 2019-03-07 | アミノ酸化合物および使用方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023074346A Active JP7624025B2 (ja) | 2018-03-07 | 2023-04-28 | アミノ酸化合物および使用方法 |
| JP2025006716A Pending JP2025081308A (ja) | 2018-03-07 | 2025-01-17 | アミノ酸化合物および使用方法 |
Country Status (35)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN109996541A (zh) | 2016-09-07 | 2019-07-09 | 普利安特治疗公司 | N-酰基氨基酸化合物及其使用方法 |
| US10696672B2 (en) | 2016-12-23 | 2020-06-30 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| US11046685B2 (en) | 2017-02-28 | 2021-06-29 | Morphic Therapeutic, Inc. | Inhibitors of (α-v)(β-6) integrin |
| EP4159727B1 (en) | 2017-02-28 | 2026-04-08 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| CU24684B1 (es) * | 2018-03-07 | 2023-10-06 | Pliant Therapeutics Inc | Compuestos de aminoácidos como inhibidores de la integrina |
| TWI841573B (zh) | 2018-06-27 | 2024-05-11 | 美商普萊恩醫療公司 | 具有未分支連接子之胺基酸化合物及使用方法 |
| CN112654621B (zh) | 2018-06-27 | 2024-05-14 | 百时美施贵宝公司 | 可作为t细胞活化剂的经取代萘啶酮化合物 |
| WO2020047208A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| AU2019327475B2 (en) | 2018-08-29 | 2025-06-05 | Morphic Therapeutic, Inc. | INHIBITING αV β6 INTEGRIN |
| PT3844162T (pt) | 2018-08-29 | 2025-03-28 | Morphic Therapeutic Inc | Inibidores da integrina alfa v beta6 |
| TW202028179A (zh) | 2018-10-08 | 2020-08-01 | 美商普萊恩醫療公司 | 胺基酸化合物及使用方法 |
| WO2020092394A1 (en) | 2018-10-30 | 2020-05-07 | Gilead Sciences, Inc. | Imidazopyridine derivatives as alpha4beta7 integrin inhibitors |
| ES2987796T3 (es) | 2018-10-30 | 2024-11-18 | Gilead Sciences Inc | Derivados de N-benzoil-fenilalanina como inhibidores de la integrina alfa4beta7 para el tratamiento de enfermedades inflamatorias |
| DK3873884T3 (da) | 2018-10-30 | 2025-02-17 | Gilead Sciences Inc | 3-(quinolin-8-yl)-1,4-dihydropyrido[3,4-d]pyrimidin-2,4-dion-derivater som alpha4beta7-integrinhæmmere til behandling af inflammatoriske sygdomme |
| WO2020092401A1 (en) | 2018-10-30 | 2020-05-07 | Gilead Sciences, Inc. | COMPOUNDS FOR INHIBITION OF ALPHA 4β7 INTEGRIN |
| EP3952902A4 (en) * | 2019-04-08 | 2022-12-21 | Pliant Therapeutics, Inc. | DOSAGE FORMS AND THERAPY SCHEMES FOR AMINO ACID COMPOUNDS |
| AU2020329207B2 (en) | 2019-08-14 | 2024-02-29 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| EP4076454A1 (en) * | 2019-12-20 | 2022-10-26 | Novartis AG | Combination treatment of liver diseases using integrin inhibitors |
| KR20230049584A (ko) * | 2020-05-07 | 2023-04-13 | 플라이언트 테라퓨틱스, 인크. | 아미노산 화합물을 사용한 호흡기 질환의 치료 |
| TW202235417A (zh) * | 2020-11-19 | 2022-09-16 | 美商普萊恩醫療公司 | 整合素抑制劑及其用途 |
| US20230028658A1 (en) * | 2021-04-30 | 2023-01-26 | Pliant Therapeutics, Inc. | Expanded dosage regimens for integrin inhibitors |
| WO2023225119A1 (en) * | 2022-05-18 | 2023-11-23 | Pliant Therapeutics, Inc. | Stabilization of integrin inhibitors |
| EP4626878A1 (en) | 2022-12-02 | 2025-10-08 | Neumora Therapeutics, Inc. | Methods of treating neurological disorders |
| WO2024125634A1 (zh) * | 2022-12-16 | 2024-06-20 | 西藏海思科制药有限公司 | 一种四氢萘啶类化合物及其在医药上的应用 |
| WO2024155965A2 (en) * | 2023-01-21 | 2024-07-25 | Pliant Therapeutics, Inc. | Biomarkers for use in integrin inhibitor therapy |
| WO2024235299A1 (zh) * | 2023-05-17 | 2024-11-21 | 西藏海思科制药有限公司 | 一种羧基衍生物及其在医药上的应用 |
| WO2025024590A1 (en) * | 2023-07-24 | 2025-01-30 | The Johns Hopkins University | Compositions and methods to treat mucus-related diseases |
| WO2025067384A1 (zh) * | 2023-09-28 | 2025-04-03 | 成都微芯药业有限公司 | 一类氨基酸整联蛋白抑制剂、其制备方法及其应用 |
| US20250197393A1 (en) | 2023-12-14 | 2025-06-19 | Pliant Therapeutics, Inc. | Integrin inhibitor and uses thereof |
| TW202615060A (zh) * | 2024-06-21 | 2026-04-16 | 美商艾拉倫製藥公司 | 用於肝外遞送之整合素配體 |
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| US6361764B2 (en) | 1996-12-13 | 2002-03-26 | Societe L'oreal S.A. | Insoluble s-triazine derivatives and their use as UV filters |
| US6048861A (en) * | 1997-12-17 | 2000-04-11 | Merck & Co., Inc. | Integrin receptor antagonists |
| SK9192000A3 (en) | 1997-12-17 | 2001-03-12 | Merck & Co Inc | Integrin receptor antagonists |
| JP2004511434A (ja) * | 2000-06-15 | 2004-04-15 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| JP4272338B2 (ja) | 2000-09-22 | 2009-06-03 | バイエル アクチェンゲゼルシャフト | ピリジン誘導体 |
| ATE396174T1 (de) | 2001-06-01 | 2008-06-15 | Elan Pharm Inc | Hydroxyalkylaminderivate als beta-secretase- inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheiten |
| DE10233500A1 (de) | 2002-07-24 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-Z-[1-(4-(N-((4-Methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylen]-6-methoxycarbonyl-2-indolinon-Monoethansulfonat und dessen Verwendung als Arzneimittel |
| AU2003273310A1 (en) | 2002-09-10 | 2004-04-30 | Pharmacia And Upjohn | Substituted aminoethers for the treatment of alzheimer's disease |
| PE20060777A1 (es) | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
| EP1870400A1 (en) | 2006-06-08 | 2007-12-26 | Boehringer Ingelheim Pharma GmbH & Co. KG | Salts and crystalline salt forms of an 2-indolinone derivative |
| UA107560C2 (uk) | 2008-06-06 | 2015-01-26 | Фармацевтична лікарська форма для негайного вивільнення похідної індолінону | |
| PL2299987T3 (pl) | 2008-06-06 | 2018-08-31 | Boehringer Ingelheim International Gmbh | Farmaceutyczna postać dawkowania w formie kapsułki zawierająca formulację zwiesiny pochodnej indolinonu |
| IN2015DN00099A (enExample) * | 2012-07-18 | 2015-05-29 | Univ Saint Louis | |
| GB201305668D0 (en) | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| AU2014324426A1 (en) | 2013-09-30 | 2016-04-21 | The Regents Of The University Of California | Anti-alphavbeta1 integrin compounds and methods |
| AU2016228852A1 (en) | 2015-03-10 | 2017-10-19 | The Regents Of The University Of California | Anti-alphavbeta1 integrin inhibitors and methods of use |
| GB201604681D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| JP7170540B2 (ja) | 2016-04-14 | 2022-11-14 | マース インコーポレーテッド | コク味を調節するためにカルシウム感知受容体活性を調節する化合物及びそれを含むペットフード製品 |
| KR20190026001A (ko) * | 2016-07-05 | 2019-03-12 | 더 락커펠러 유니버시티 | 테트라하이드로나프티리딘펜탄아미드 인테그린 길항물질 |
| CN109996541A (zh) | 2016-09-07 | 2019-07-09 | 普利安特治疗公司 | N-酰基氨基酸化合物及其使用方法 |
| CN110062625A (zh) | 2016-12-12 | 2019-07-26 | 勃林格殷格翰国际有限公司 | 尼达尼布通过与奥达特罗共给予用于治疗间质性肺病的方法 |
| US10696672B2 (en) | 2016-12-23 | 2020-06-30 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| US11046685B2 (en) | 2017-02-28 | 2021-06-29 | Morphic Therapeutic, Inc. | Inhibitors of (α-v)(β-6) integrin |
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| CU24684B1 (es) * | 2018-03-07 | 2023-10-06 | Pliant Therapeutics Inc | Compuestos de aminoácidos como inhibidores de la integrina |
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| AU2019327475B2 (en) | 2018-08-29 | 2025-06-05 | Morphic Therapeutic, Inc. | INHIBITING αV β6 INTEGRIN |
| EP3843728B1 (en) | 2018-08-29 | 2025-04-30 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| WO2020047208A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| TW202028179A (zh) | 2018-10-08 | 2020-08-01 | 美商普萊恩醫療公司 | 胺基酸化合物及使用方法 |
| EP3952902A4 (en) | 2019-04-08 | 2022-12-21 | Pliant Therapeutics, Inc. | DOSAGE FORMS AND THERAPY SCHEMES FOR AMINO ACID COMPOUNDS |
| KR20230049584A (ko) | 2020-05-07 | 2023-04-13 | 플라이언트 테라퓨틱스, 인크. | 아미노산 화합물을 사용한 호흡기 질환의 치료 |
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