JP2013530240A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013530240A5 JP2013530240A5 JP2013518740A JP2013518740A JP2013530240A5 JP 2013530240 A5 JP2013530240 A5 JP 2013530240A5 JP 2013518740 A JP2013518740 A JP 2013518740A JP 2013518740 A JP2013518740 A JP 2013518740A JP 2013530240 A5 JP2013530240 A5 JP 2013530240A5
- Authority
- JP
- Japan
- Prior art keywords
- cyclopropyl
- carbon atoms
- triazol
- optionally substituted
- pharmaceutically acceptable
- 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
Links
- 125000004432 carbon atom Chemical group C* 0.000 claims description 74
- 150000001875 compounds Chemical class 0.000 claims description 56
- -1 4-cyclopropyl-1H-imidazol-1-yl Chemical group 0.000 claims description 50
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 47
- 125000000217 alkyl group Chemical group 0.000 claims description 46
- 125000005843 halogen group Chemical group 0.000 claims description 43
- 150000003839 salts Chemical class 0.000 claims description 32
- 125000001424 substituent group Chemical group 0.000 claims description 24
- 125000003545 alkoxy group Chemical group 0.000 claims description 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 19
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 18
- 239000001257 hydrogen Substances 0.000 claims description 18
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 10
- 125000002883 imidazolyl group Chemical group 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000004043 oxo group Chemical group O=* 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 8
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 6
- IBBMAWULFFBRKK-UHFFFAOYSA-N picolinamide Chemical compound NC(=O)C1=CC=CC=N1 IBBMAWULFFBRKK-UHFFFAOYSA-N 0.000 claims description 5
- 230000001154 acute effect Effects 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 3
- BXWKCDYKCYLKLD-NSHDSACASA-N 4-(4-cyclopropylimidazol-1-yl)-n-[2-[4-[(2s)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]-1,3-thiazol-4-yl]pyridine-2-carboxamide Chemical compound FC(F)(F)[C@H](C)N1C=NN=C1C1=NC(NC(=O)C=2N=CC=C(C=2)N2C=C(N=C2)C2CC2)=CS1 BXWKCDYKCYLKLD-NSHDSACASA-N 0.000 claims description 2
- NHCMYVVORIJKBE-UHFFFAOYSA-N 4-(4-cyclopropylimidazol-1-yl)-n-[5-(4-cyclopropyl-1,2,4-triazol-3-yl)thiophen-3-yl]-5-methylpyridine-2-carboxamide Chemical compound CC1=CN=C(C(=O)NC=2C=C(SC=2)C=2N(C=NN=2)C2CC2)C=C1N(C=1)C=NC=1C1CC1 NHCMYVVORIJKBE-UHFFFAOYSA-N 0.000 claims description 2
- RQIGKHWWWTYKQA-UHFFFAOYSA-N 4-(6-cyclopropylpyridin-3-yl)-n-[2-(4-cyclopropyl-1,2,4-triazol-3-yl)-1,3-thiazol-4-yl]pyridine-2-carboxamide Chemical compound C=1C(C=2C=NC(=CC=2)C2CC2)=CC=NC=1C(=O)NC(N=1)=CSC=1C1=NN=CN1C1CC1 RQIGKHWWWTYKQA-UHFFFAOYSA-N 0.000 claims description 2
- VKWGKBVWKPPWRG-UHFFFAOYSA-N 4-(6-cyclopropylpyridin-3-yl)-n-[5-(4-cyclopropyl-1,2,4-triazol-3-yl)thiophen-3-yl]pyridine-2-carboxamide Chemical compound C=1C(C=2C=NC(=CC=2)C2CC2)=CC=NC=1C(=O)NC(C=1)=CSC=1C1=NN=CN1C1CC1 VKWGKBVWKPPWRG-UHFFFAOYSA-N 0.000 claims description 2
- VPCXPQKTNBQUSD-UHFFFAOYSA-N 5-(4-cyclopropylimidazol-1-yl)-n-[2-(4-cyclopropyl-1,2,4-triazol-3-yl)-1,3-thiazol-4-yl]-2-methoxybenzamide Chemical compound COC1=CC=C(N2C=C(N=C2)C2CC2)C=C1C(=O)NC(N=1)=CSC=1C1=NN=CN1C1CC1 VPCXPQKTNBQUSD-UHFFFAOYSA-N 0.000 claims description 2
- VLQPKPCJTAVPON-UHFFFAOYSA-N 5-(4-cyclopropylimidazol-1-yl)-n-[5-(4-cyclopropyl-1,2,4-triazol-3-yl)thiophen-3-yl]-2-methoxybenzamide Chemical compound COC1=CC=C(N2C=C(N=C2)C2CC2)C=C1C(=O)NC(C=1)=CSC=1C1=NN=CN1C1CC1 VLQPKPCJTAVPON-UHFFFAOYSA-N 0.000 claims description 2
- XQLUBDAVNKCKQD-UHFFFAOYSA-N 5-(6-cyclopropylpyridin-3-yl)-n-[5-(4-cyclopropyl-1,2,4-triazol-3-yl)thiophen-3-yl]-2,4-dimethoxybenzamide Chemical compound COC1=CC(OC)=C(C=2C=NC(=CC=2)C2CC2)C=C1C(=O)NC(C=1)=CSC=1C1=NN=CN1C1CC1 XQLUBDAVNKCKQD-UHFFFAOYSA-N 0.000 claims description 2
- OXBWEFYXJCXFOR-UHFFFAOYSA-N 5-(6-cyclopropylpyridin-3-yl)-n-[5-(4-cyclopropyl-1,2,4-triazol-3-yl)thiophen-3-yl]-2-methoxybenzamide Chemical compound COC1=CC=C(C=2C=NC(=CC=2)C2CC2)C=C1C(=O)NC(C=1)=CSC=1C1=NN=CN1C1CC1 OXBWEFYXJCXFOR-UHFFFAOYSA-N 0.000 claims description 2
- 208000030090 Acute Disease Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 2
- 208000004852 Lung Injury Diseases 0.000 claims description 2
- 206010069363 Traumatic lung injury Diseases 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 2
- 230000003176 fibrotic effect Effects 0.000 claims description 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 2
- 208000017169 kidney disease Diseases 0.000 claims description 2
- 208000019423 liver disease Diseases 0.000 claims description 2
- 231100000515 lung injury Toxicity 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- LKFHDVNDOWOQLU-UHFFFAOYSA-N n-[2-(4-cyclopropyl-1,2,4-triazol-3-yl)-1,3-thiazol-4-yl]-4-pyridin-3-ylpyridine-2-carboxamide Chemical compound C=1C(C=2C=NC=CC=2)=CC=NC=1C(=O)NC(N=1)=CSC=1C1=NN=CN1C1CC1 LKFHDVNDOWOQLU-UHFFFAOYSA-N 0.000 claims description 2
- HDDBDWDCDKNSCS-UHFFFAOYSA-N n-[4-(4-cyclopropyl-1,2,4-triazol-3-yl)-1,3-thiazol-2-yl]-4-pyridin-3-ylpyridine-2-carboxamide Chemical compound C=1C(C=2C=NC=CC=2)=CC=NC=1C(=O)NC(SC=1)=NC=1C1=NN=CN1C1CC1 HDDBDWDCDKNSCS-UHFFFAOYSA-N 0.000 claims description 2
- SQTMEYNQSUNPLG-UHFFFAOYSA-N n-[5-(4-cyclopropyl-1,2,4-triazol-3-yl)thiophen-3-yl]-4-pyridin-3-ylpyridine-2-carboxamide Chemical compound C=1C(C=2C=NC=CC=2)=CC=NC=1C(=O)NC(C=1)=CSC=1C1=NN=CN1C1CC1 SQTMEYNQSUNPLG-UHFFFAOYSA-N 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 208000023504 respiratory system disease Diseases 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 3
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- SAFMUWNMQDZETL-UHFFFAOYSA-N 4-cyclopropyl-3-thiophen-2-yl-1,2,4-triazole Chemical compound C1CC1N1C(C=2SC=CC=2)=NN=C1 SAFMUWNMQDZETL-UHFFFAOYSA-N 0.000 claims 1
- 101001018196 Homo sapiens Mitogen-activated protein kinase kinase kinase 5 Proteins 0.000 claims 1
- 102100033127 Mitogen-activated protein kinase kinase kinase 5 Human genes 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 3
- BOQNUOWAVFCKKS-UHFFFAOYSA-N 4-(4-cyclopropylimidazol-1-yl)-n-[2-(4-cyclopropyl-1,2,4-triazol-3-yl)-1,3-thiazol-4-yl]-5-methylpyridine-2-carboxamide Chemical compound CC1=CN=C(C(=O)NC=2N=C(SC=2)C=2N(C=NN=2)C2CC2)C=C1N(C=1)C=NC=1C1CC1 BOQNUOWAVFCKKS-UHFFFAOYSA-N 0.000 description 1
- IMLYDRHZHDRSMD-UHFFFAOYSA-N 5-(4-cyclopropylimidazol-1-yl)-n-[2-(4-cyclopropyl-1,2,4-triazol-3-yl)-1,3-thiazol-4-yl]-2-fluorobenzamide Chemical compound FC1=CC=C(N2C=C(N=C2)C2CC2)C=C1C(=O)NC(N=1)=CSC=1C1=NN=CN1C1CC1 IMLYDRHZHDRSMD-UHFFFAOYSA-N 0.000 description 1
- BKXLKDCLRVCQTO-UHFFFAOYSA-N 5-(4-cyclopropylimidazol-1-yl)-n-[5-(4-cyclopropyl-1,2,4-triazol-3-yl)thiophen-3-yl]-2-fluorobenzamide Chemical compound FC1=CC=C(N2C=C(N=C2)C2CC2)C=C1C(=O)NC(C=1)=CSC=1C1=NN=CN1C1CC1 BKXLKDCLRVCQTO-UHFFFAOYSA-N 0.000 description 1
- 229940127254 ASK1 inhibitor Drugs 0.000 description 1
- JQEROOCRTFCUNY-UHFFFAOYSA-N n-[4-(4-cyclopropyl-1,2,4-triazol-3-yl)-1,3-thiazol-2-yl]-4-(6-methoxypyridin-3-yl)pyridine-2-carboxamide Chemical compound C1=NC(OC)=CC=C1C1=CC=NC(C(=O)NC=2SC=C(N=2)C=2N(C=NN=2)C2CC2)=C1 JQEROOCRTFCUNY-UHFFFAOYSA-N 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36108010P | 2010-07-02 | 2010-07-02 | |
| US61/361,080 | 2010-07-02 | ||
| PCT/US2011/042694 WO2012003387A1 (en) | 2010-07-02 | 2011-06-30 | Apoptosis signal-regulating kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013530240A JP2013530240A (ja) | 2013-07-25 |
| JP2013530240A5 true JP2013530240A5 (enExample) | 2014-06-19 |
| JP5705314B2 JP5705314B2 (ja) | 2015-04-22 |
Family
ID=44318106
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013518740A Active JP5705314B2 (ja) | 2010-07-02 | 2011-06-30 | アポトーシスシグナル調節キナーゼ阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US8440665B2 (enExample) |
| EP (1) | EP2588475B1 (enExample) |
| JP (1) | JP5705314B2 (enExample) |
| KR (1) | KR101759759B1 (enExample) |
| CN (1) | CN102985418B (enExample) |
| AU (1) | AU2011272782B2 (enExample) |
| BR (1) | BR112012033715A2 (enExample) |
| CA (1) | CA2802743C (enExample) |
| EA (1) | EA023040B1 (enExample) |
| ES (1) | ES2543428T3 (enExample) |
| IL (2) | IL223556A (enExample) |
| MX (1) | MX2012015105A (enExample) |
| NZ (1) | NZ604831A (enExample) |
| PL (1) | PL2588475T3 (enExample) |
| PT (1) | PT2588475E (enExample) |
| SI (1) | SI2588475T1 (enExample) |
| WO (1) | WO2012003387A1 (enExample) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2331095B1 (en) | 2008-08-04 | 2014-10-15 | CHDI Foundation, Inc. | Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| TWI625121B (zh) | 2009-07-13 | 2018-06-01 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| PH12012501480A1 (en) | 2010-01-25 | 2012-10-22 | Chdi Foundation Inc | Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| SI2588475T1 (sl) * | 2010-07-02 | 2015-12-31 | Gilead Sciences, Inc. | Kinazni inhibitorji za regulacijo apoptoznega signala |
| EP2598660B1 (en) | 2010-07-26 | 2017-03-15 | Biomatrica, INC. | Compositions for stabilizing dna, rna and proteins in blood and other biological samples during shipping and storage at ambient temperatures |
| CA2806734A1 (en) | 2010-07-26 | 2012-02-09 | Biomatrica, Inc. | Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures |
| JP5927201B2 (ja) | 2010-12-16 | 2016-06-01 | カルチャン リミテッド | Ａｓｋ１阻害ピロロピリミジン誘導体 |
| MX2014002459A (es) | 2011-08-30 | 2014-04-10 | Chdi Foundation Inc | Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodos de uso de los mismos. |
| US9981918B2 (en) | 2011-08-30 | 2018-05-29 | Chdi Foundation, Inc. | Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| AU2015201188B2 (en) * | 2012-01-27 | 2016-12-15 | Gilead Sciences, Inc. | Apoptosis signal-regulating kinase inhibitor |
| UY34573A (es) | 2012-01-27 | 2013-06-28 | Gilead Sciences Inc | Inhibidor de la quinasa que regula la señal de la apoptosis |
| HK1217117A1 (zh) | 2012-12-20 | 2016-12-23 | 生物马特里卡公司 | 用於使pcr试剂稳定化的制剂和方法 |
| UY35212A (es) * | 2012-12-21 | 2014-06-30 | Gilead Sciences Inc | Inhibidores de la quinasa que regula la señal de la apoptosis |
| EP3007556B1 (en) | 2013-06-13 | 2020-05-20 | Biomatrica, INC. | Cell stabilization |
| MD4658B1 (ro) | 2013-12-20 | 2019-11-30 | Gilead Sciences Inc | Inhibitori ai kinazei inductoare de apoptoză |
| WO2015143653A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015143652A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015143654A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| US20150342943A1 (en) | 2014-06-03 | 2015-12-03 | Gilead Sciences, Inc. | Methods of treating liver disease |
| ES2786373T3 (es) | 2014-06-10 | 2020-10-09 | Biomatrica Inc | Estabilización de trombocitos a temperaturas ambiente |
| SG11201700341PA (en) | 2014-07-17 | 2017-02-27 | Chdi Foundation Inc | Methods and compositions for treating hiv-related disorders |
| TW201618781A (zh) | 2014-08-13 | 2016-06-01 | 吉李德科學股份有限公司 | 治療肺高血壓之方法 |
| AU2015320792B2 (en) | 2014-09-24 | 2018-08-30 | Gilead Sciences, Inc. | Methods of treating liver disease |
| MA41252A (fr) | 2014-12-23 | 2017-10-31 | Gilead Sciences Inc | Formes solides d'un inhibiteur d'ask 1 |
| JP6439050B2 (ja) | 2014-12-23 | 2018-12-19 | ギリアード サイエンシーズ， インコーポレイテッド | Ａｓｋ１阻害剤を調製するプロセス |
| WO2016161572A1 (en) | 2015-04-08 | 2016-10-13 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| WO2017100212A1 (en) | 2015-12-08 | 2017-06-15 | Biomatrica, Inc. | Reduction of erythrocyte sedimentation rate |
| CA3016081A1 (en) | 2016-03-04 | 2017-09-08 | Gilead Sciences, Inc. | Compositions and combinations of autotaxin inhibitors |
| FR3050112B1 (fr) | 2016-04-15 | 2020-09-04 | Soc Civ Immobiliere Gecinq | Utilisation de l'acide fenofibrique dans le traitement des maladies hepatiques |
| CN110036005B (zh) * | 2016-11-16 | 2022-09-27 | 广东东阳光药业有限公司 | 酰胺衍生物及其在药物中的应用 |
| WO2018157856A1 (zh) | 2017-03-03 | 2018-09-07 | 江苏豪森药业集团有限公司 | 酰胺类衍生物抑制剂及其制备方法和应用 |
| PL3621615T3 (pl) | 2017-05-12 | 2024-03-25 | Enanta Pharmaceuticals, Inc. | Inhibitory regulujące sygnał apoptozy kinazy 1 i sposoby ich stosowania |
| US10450301B2 (en) | 2017-05-25 | 2019-10-22 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| US10246439B2 (en) | 2017-05-25 | 2019-04-02 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| US10253018B2 (en) | 2017-05-25 | 2019-04-09 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| WO2019034096A1 (en) * | 2017-08-17 | 2019-02-21 | Sunshine Lake Pharma Co., Ltd. | FUSED BICYCLIC COMPOUNDS AND THEIR USES IN MEDICINE |
| US10597382B2 (en) | 2017-08-28 | 2020-03-24 | Enanta Pharmaceuticals, Inc. | Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| US10370352B2 (en) | 2017-09-07 | 2019-08-06 | Eli Lilly And Company | Cyclobutyl-imidazolidinone compounds |
| WO2019047094A1 (en) * | 2017-09-07 | 2019-03-14 | Eli Lilly And Company | CYCLOBUTYL-IMIDAZOLIDINONE COMPOUNDS |
| JP2020533335A (ja) * | 2017-09-08 | 2020-11-19 | フロンセラ ユー．エス． ファーマシューティカルズ エルエルシー | アポトーシスシグナル調節キナーゼ阻害剤およびその使用 |
| CN111518080A (zh) * | 2017-10-12 | 2020-08-11 | 深圳市塔吉瑞生物医药有限公司 | 一种1,2,4-三氮唑类化合物 |
| WO2019099703A1 (en) * | 2017-11-16 | 2019-05-23 | Sidecar Therapeutics, Inc. | Apoptosis signal-regulating kinase 1 (ask 1) inhibitor compounds |
| CN111655678B (zh) * | 2018-01-05 | 2023-08-22 | 广州市恒诺康医药科技有限公司 | 细胞凋亡信号调节激酶-1抑制剂及其应用 |
| CN110294742B (zh) * | 2018-03-21 | 2023-01-31 | 山东轩竹医药科技有限公司 | 并环类ask1抑制剂及其应用 |
| EP4537902A3 (en) * | 2018-04-12 | 2025-06-11 | Terns, Inc. | Tricyclic ask1 inhibitors |
| CN110407806B (zh) | 2018-04-28 | 2021-08-17 | 深圳微芯生物科技股份有限公司 | 甲酰胺类化合物、其制备方法及其应用 |
| US10683289B2 (en) | 2018-05-02 | 2020-06-16 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| JP7328254B2 (ja) | 2018-05-02 | 2023-08-16 | エナンタ ファーマシューティカルズ インコーポレイテッド | アポトーシスシグナル調節キナーゼ１阻害剤を含むテトラゾール及びその使用方法 |
| CA3109504A1 (en) * | 2018-08-14 | 2020-02-20 | Biogen Ma Inc. | Ask1 inhibiting agents |
| WO2020041417A1 (en) | 2018-08-22 | 2020-02-27 | Enanta Pharmaceuticals, Inc. | Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| WO2020106707A1 (en) | 2018-11-19 | 2020-05-28 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| WO2020198214A1 (en) | 2019-03-25 | 2020-10-01 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| CN111018831B (zh) * | 2019-11-21 | 2022-05-31 | 中国药科大学 | 细胞凋亡信号调节激酶抑制剂及其应用 |
| WO2021127643A1 (en) * | 2019-12-20 | 2021-06-24 | Tenaya Therapeutics, Inc. | Fluoroalkyl-oxadiazoles and uses thereof |
| WO2021252555A1 (en) * | 2020-06-09 | 2021-12-16 | Anima Biotech Inc. | Collagen 1 translation inhibitors and methods of use thereof |
| TW202220967A (zh) * | 2020-07-24 | 2022-06-01 | 美商伊尼製藥股份有限公司 | 噻吩hsd17b13抑制劑及其用途 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| CA1121825A (en) * | 1978-04-11 | 1982-04-13 | Franco Bolasco | 2-(2-thenoylthio)-propionylglycine: method for its preparation and pharmaceutical formulations containing said compound |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4902514A (en) | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| TW513418B (en) * | 1996-07-31 | 2002-12-11 | Otsuka Pharma Co Ltd | Thiazole derivatives, their production and use |
| WO1998034946A1 (en) | 1997-02-12 | 1998-08-13 | Massachusetts Institute Of Technology | Daxx, a novel fas-binding protein that activates jnk and apoptosis |
| US6881555B2 (en) | 1999-03-19 | 2005-04-19 | Aventis Pharmaceuticals Inc. | AKT nucleic acids, polypeptides, and uses thereof |
| AU782448B2 (en) | 1999-03-19 | 2005-07-28 | Aventis Pharmaceuticals Inc. | Akt nucleic acids, polypeptides, and uses thereof |
| US20070237770A1 (en) | 2001-11-30 | 2007-10-11 | Albert Lai | Novel compositions and methods in cancer |
| EP1661581A1 (en) | 2003-07-28 | 2006-05-31 | Osaka Industrial Promotion Organization | Remedy for cardiac failure comprising ask1 inhibitor as the active ingredient and method of screening the same |
| US7078064B2 (en) * | 2003-12-03 | 2006-07-18 | George Zabrecky | Compositions and methods useful for treating and preventing chronic liver disease, chronic HCV infection and non-alcoholic steatohepatitis |
| EP1794137A4 (en) | 2004-09-27 | 2009-12-02 | Kosan Biosciences Inc | SPECIFIC KINASE INHIBITORS |
| EP1677113A1 (en) | 2004-12-29 | 2006-07-05 | Max-Delbrück-Centrum für Molekulare Medizin (MDC) | Method for the identification of protein-protein interactions in disease related protein networks |
| JP2009524677A (ja) * | 2006-01-25 | 2009-07-02 | シンタ ファーマシューティカルズ コーポレーション | 炎症および免疫関連使用用のチアゾールおよびチアジアゾール化合物 |
| US20070276050A1 (en) | 2006-02-27 | 2007-11-29 | Gilead Sciences, Inc. | Methods for identifying ASK1 inhibitors useful for preventing and/or treating cardiovascular diseases |
| WO2008011560A2 (en) * | 2006-07-20 | 2008-01-24 | Mehmet Kahraman | Benzothiophene inhibitors of rho kinase |
| JPWO2008016131A1 (ja) * | 2006-08-04 | 2009-12-24 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| EP2104734A2 (en) | 2006-12-08 | 2009-09-30 | Asuragen, INC. | Mir-20 regulated genes and pathways as targets for therapeutic intervention |
| US8263595B2 (en) * | 2007-08-31 | 2012-09-11 | Merck Serono Sa | Triazolopyridine compounds and their use as ask inhibitors |
| JP5432982B2 (ja) | 2008-03-31 | 2014-03-05 | 武田薬品工業株式会社 | アポトーシスシグナル調節キナーゼ１阻害剤 |
| US8178555B2 (en) | 2008-06-24 | 2012-05-15 | Takeda Pharmaceutical Company Limited | Apoptosis signal-regulating kinase 1 inhibitors |
| WO2010045470A2 (en) | 2008-10-15 | 2010-04-22 | Dana-Farber Cancer Institute, Inc. | Compositions, kits, and methods for identification, assessment, prevention, and therapy of hepatic disorders |
| US20110294693A1 (en) | 2008-11-17 | 2011-12-01 | The George Washington University | Compositions and Methods for Identifying Autism Spectrum Disorders |
| EP2411516A1 (en) | 2009-03-27 | 2012-02-01 | Merck Sharp&Dohme Corp. | RNA INTERFERENCE MEDIATED INHIBITION OF APOPTOSIS SIGNAL-REGULATING KINASE 1 (ASK1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) |
| TWI625121B (zh) * | 2009-07-13 | 2018-06-01 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| WO2011041293A1 (en) | 2009-09-30 | 2011-04-07 | Takeda Pharmaceutical Company Limited | Pyrazolo [1, 5-a] pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors |
| US8802695B2 (en) | 2010-02-03 | 2014-08-12 | Takeda Pharmaceutical Company Limited | Apoptosis signal-regulating kinase 1 inhibitors |
| WO2011097594A2 (en) | 2010-02-08 | 2011-08-11 | Kinagen, Inc. | Therapeutic methods and compositions involving allosteric kinase inhibition |
| RU2018100142A (ru) | 2010-03-24 | 2019-02-20 | Амитек Терапетикс Солюшинс, Инк. | Гетероциклические соединения, эффективные для ингибирования киназы |
| SI2588475T1 (sl) * | 2010-07-02 | 2015-12-31 | Gilead Sciences, Inc. | Kinazni inhibitorji za regulacijo apoptoznega signala |
| CN103492590A (zh) | 2011-02-22 | 2014-01-01 | 卡里斯生命科学卢森堡控股有限责任公司 | 循环生物标志物 |
| JP2014526032A (ja) | 2011-06-07 | 2014-10-02 | カリス ライフ サイエンシズ ルクセンブルク ホールディングス エス．アー．エール．エル． | 癌に対する循環バイオマーカー |
| UY35212A (es) * | 2012-12-21 | 2014-06-30 | Gilead Sciences Inc | Inhibidores de la quinasa que regula la señal de la apoptosis |
| MD4658B1 (ro) * | 2013-12-20 | 2019-11-30 | Gilead Sciences Inc | Inhibitori ai kinazei inductoare de apoptoză |
-
2011
- 2011-06-30 SI SI201130521T patent/SI2588475T1/sl unknown
- 2011-06-30 CN CN201180033172.3A patent/CN102985418B/zh active Active
- 2011-06-30 MX MX2012015105A patent/MX2012015105A/es active IP Right Grant
- 2011-06-30 PT PT117342204T patent/PT2588475E/pt unknown
- 2011-06-30 EA EA201291273A patent/EA023040B1/ru not_active IP Right Cessation
- 2011-06-30 NZ NZ604831A patent/NZ604831A/en not_active IP Right Cessation
- 2011-06-30 EP EP20110734220 patent/EP2588475B1/en active Active
- 2011-06-30 ES ES11734220.4T patent/ES2543428T3/es active Active
- 2011-06-30 WO PCT/US2011/042694 patent/WO2012003387A1/en not_active Ceased
- 2011-06-30 CA CA2802743A patent/CA2802743C/en active Active
- 2011-06-30 AU AU2011272782A patent/AU2011272782B2/en active Active
- 2011-06-30 PL PL11734220T patent/PL2588475T3/pl unknown
- 2011-06-30 KR KR1020137001239A patent/KR101759759B1/ko active Active
- 2011-06-30 US US13/174,459 patent/US8440665B2/en active Active
- 2011-06-30 JP JP2013518740A patent/JP5705314B2/ja active Active
- 2011-06-30 BR BR112012033715A patent/BR112012033715A2/pt not_active Application Discontinuation
-
2012
- 2012-12-11 IL IL223556A patent/IL223556A/en active IP Right Grant
-
2013
- 2013-03-14 US US13/828,984 patent/US8927582B2/en not_active Ceased
-
2016
- 2016-08-21 IL IL247405A patent/IL247405A0/en unknown
-
2017
- 2017-01-03 US US15/397,344 patent/USRE48150E1/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013530240A5 (enExample) | ||
| NZ604831A (en) | Apoptosis signal-regulating kinase inhibitors | |
| RU2461551C2 (ru) | Азолкарбоксамидное соединение или его фармацевтически приемлемая соль | |
| JP2010540462A5 (enExample) | ||
| JP2006500369A5 (enExample) | ||
| JP2010538076A5 (enExample) | ||
| JP2004534035A5 (enExample) | ||
| JP2013507350A5 (enExample) | ||
| JP2007531752A5 (enExample) | ||
| JP2010506825A5 (enExample) | ||
| JP2008500336A5 (enExample) | ||
| RU2021127810A (ru) | Замещенные гетероарилом пиридины и способы применения | |
| SI2509955T1 (en) | Pyrazole derivatives as calcium channel modulators activated by the release of calcium | |
| HRP20170112T1 (hr) | Supstituirani spojevi piridin-2-karboksamida kao kinazni inhibitori signalne regulacije apoptoze | |
| RU2013143028A (ru) | Тиазолилфенилбензолсульфонамидопроизводные в качестве ингибиторов киназ | |
| JP2009520825A5 (enExample) | ||
| JP2016513660A5 (enExample) | ||
| JP2009525285A5 (enExample) | ||
| JP2007519735A5 (enExample) | ||
| JP2010533158A5 (enExample) | ||
| JP2010513272A5 (enExample) | ||
| RU2009144113A (ru) | Ингибиторы фермента диацилглицерин о-ацилтрансферазы типа 1 | |
| RU2016133626A (ru) | 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера | |
| JP2021501179A5 (enExample) | ||
| RU2012116877A (ru) | Соединения 2-пиридона, применяемые в качестве ингибиторов нейтрофильной эластазы |