JP2016506418A5 - - Google Patents
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- JP2016506418A5 JP2016506418A5 JP2015552757A JP2015552757A JP2016506418A5 JP 2016506418 A5 JP2016506418 A5 JP 2016506418A5 JP 2015552757 A JP2015552757 A JP 2015552757A JP 2015552757 A JP2015552757 A JP 2015552757A JP 2016506418 A5 JP2016506418 A5 JP 2016506418A5
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- 150000001875 compounds Chemical class 0.000 claims 21
- 238000000034 method Methods 0.000 claims 19
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 108091008606 PDGF receptors Proteins 0.000 claims 8
- 102000011653 Platelet-Derived Growth Factor Receptors Human genes 0.000 claims 8
- 102100030485 Platelet-derived growth factor receptor alpha Human genes 0.000 claims 7
- 101710148465 Platelet-derived growth factor receptor alpha Proteins 0.000 claims 7
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims 7
- 238000006467 substitution reaction Methods 0.000 claims 7
- QSZCGGBDNYTQHH-UHFFFAOYSA-N 2,3-dimethoxyphenol Chemical compound COC1=CC=CC(O)=C1OC QSZCGGBDNYTQHH-UHFFFAOYSA-N 0.000 claims 6
- 208000019693 Lung disease Diseases 0.000 claims 6
- 229910052794 bromium Inorganic materials 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 230000005764 inhibitory process Effects 0.000 claims 6
- 229910052740 iodine Inorganic materials 0.000 claims 6
- 108040008097 MAP kinase activity proteins Proteins 0.000 claims 5
- 102000019149 MAP kinase activity proteins Human genes 0.000 claims 5
- 108010051742 Platelet-Derived Growth Factor beta Receptor Proteins 0.000 claims 5
- 230000002159 abnormal effect Effects 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- LHGVFZTZFXWLCP-UHFFFAOYSA-N guaiacol Chemical compound COC1=CC=CC=C1O LHGVFZTZFXWLCP-UHFFFAOYSA-N 0.000 claims 4
- -1 guanidinyl groups Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 208000002815 pulmonary hypertension Diseases 0.000 claims 4
- 101000876610 Dictyostelium discoideum Extracellular signal-regulated kinase 2 Proteins 0.000 claims 3
- 101001052493 Homo sapiens Mitogen-activated protein kinase 1 Proteins 0.000 claims 3
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 claims 3
- 108091000080 Phosphotransferase Proteins 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- JHJNPOSPVGRIAN-SFHVURJKSA-N n-[3-[(1s)-1-[[6-(3,4-dimethoxyphenyl)pyrazin-2-yl]amino]ethyl]phenyl]-5-methylpyridine-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1C1=CN=CC(N[C@@H](C)C=2C=C(NC(=O)C=3C=C(C)C=NC=3)C=CC=2)=N1 JHJNPOSPVGRIAN-SFHVURJKSA-N 0.000 claims 3
- 102000020233 phosphotransferase Human genes 0.000 claims 3
- 230000035755 proliferation Effects 0.000 claims 3
- 210000001147 pulmonary artery Anatomy 0.000 claims 3
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 3
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 3
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 3
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- 239000000758 substrate Substances 0.000 claims 3
- ABDKAPXRBAPSQN-UHFFFAOYSA-N veratrole Chemical compound COC1=CC=CC=C1OC ABDKAPXRBAPSQN-UHFFFAOYSA-N 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 208000026151 Chronic thromboembolic pulmonary hypertension Diseases 0.000 claims 2
- 102000012085 Endoglin Human genes 0.000 claims 2
- 108010036395 Endoglin Proteins 0.000 claims 2
- 208000031953 Hereditary hemorrhagic telangiectasia Diseases 0.000 claims 2
- 206010020880 Hypertrophy Diseases 0.000 claims 2
- 101710164680 Platelet-derived growth factor receptor beta Proteins 0.000 claims 2
- 108010017324 STAT3 Transcription Factor Proteins 0.000 claims 2
- 102100024040 Signal transducer and activator of transcription 3 Human genes 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 125000001891 dimethoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 210000002889 endothelial cell Anatomy 0.000 claims 2
- 210000002950 fibroblast Anatomy 0.000 claims 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 2
- 230000003993 interaction Effects 0.000 claims 2
- 230000003902 lesion Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 210000000651 myofibroblast Anatomy 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000026731 phosphorylation Effects 0.000 claims 2
- 238000006366 phosphorylation reaction Methods 0.000 claims 2
- 230000002685 pulmonary effect Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 230000002792 vascular Effects 0.000 claims 2
- 230000002861 ventricular Effects 0.000 claims 2
- 102100025422 Bone morphogenetic protein receptor type-2 Human genes 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
- 208000002330 Congenital Heart Defects Diseases 0.000 claims 1
- 201000006306 Cor pulmonale Diseases 0.000 claims 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 1
- 206010052337 Diastolic dysfunction Diseases 0.000 claims 1
- 208000000059 Dyspnea Diseases 0.000 claims 1
- 206010013975 Dyspnoeas Diseases 0.000 claims 1
- 208000015872 Gaucher disease Diseases 0.000 claims 1
- 101000934635 Homo sapiens Bone morphogenetic protein receptor type-2 Proteins 0.000 claims 1
- 101000617830 Homo sapiens Sterol O-acyltransferase 1 Proteins 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010021133 Hypoventilation Diseases 0.000 claims 1
- 206010021143 Hypoxia Diseases 0.000 claims 1
- 208000020875 Idiopathic pulmonary arterial hypertension Diseases 0.000 claims 1
- 208000024934 IgG4-related mediastinitis Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 1
- 206010049459 Lymphangioleiomyomatosis Diseases 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- 208000003250 Mixed connective tissue disease Diseases 0.000 claims 1
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 208000009905 Neurofibromatoses Diseases 0.000 claims 1
- 206010061876 Obstruction Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 108091008611 Protein Kinase B Proteins 0.000 claims 1
- 208000021068 Pulmonary arterial hypertension associated with portal hypertension Diseases 0.000 claims 1
- 208000021085 Pulmonary hypertension with unclear multifactorial mechanism Diseases 0.000 claims 1
- 208000011191 Pulmonary vascular disease Diseases 0.000 claims 1
- 102100033810 RAC-alpha serine/threonine-protein kinase Human genes 0.000 claims 1
- 102100021993 Sterol O-acyltransferase 1 Human genes 0.000 claims 1
- 101000697584 Streptomyces lavendulae Streptothricin acetyltransferase Proteins 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010071436 Systolic dysfunction Diseases 0.000 claims 1
- 208000024799 Thyroid disease Diseases 0.000 claims 1
- 208000024248 Vascular System injury Diseases 0.000 claims 1
- 208000012339 Vascular injury Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 208000017304 adult pulmonary Langerhans cell histiocytosis Diseases 0.000 claims 1
- 230000004872 arterial blood pressure Effects 0.000 claims 1
- 230000037147 athletic performance Effects 0.000 claims 1
- 230000001746 atrial effect Effects 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000022831 chronic renal failure syndrome Diseases 0.000 claims 1
- 208000028831 congenital heart disease Diseases 0.000 claims 1
- 230000009547 development abnormality Effects 0.000 claims 1
- 238000000502 dialysis Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 208000007345 glycogen storage disease Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000007475 hemolytic anemia Diseases 0.000 claims 1
- 239000000833 heterodimer Substances 0.000 claims 1
- 239000000710 homodimer Substances 0.000 claims 1
- 150000003840 hydrochlorides Chemical class 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 230000007954 hypoxia Effects 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 229940001447 lactate Drugs 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 229940049920 malate Drugs 0.000 claims 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 201000004931 neurofibromatosis Diseases 0.000 claims 1
- 230000002085 persistent effect Effects 0.000 claims 1
- 235000021317 phosphate Nutrition 0.000 claims 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 210000003492 pulmonary vein Anatomy 0.000 claims 1
- 230000009467 reduction Effects 0.000 claims 1
- 230000029058 respiratory gaseous exchange Effects 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 201000004409 schistosomiasis Diseases 0.000 claims 1
- 208000013220 shortness of breath Diseases 0.000 claims 1
- 238000010911 splenectomy Methods 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 claims 1
- 230000004083 survival effect Effects 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 230000035488 systolic blood pressure Effects 0.000 claims 1
- 229940095064 tartrate Drugs 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 108700012359 toxins Proteins 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361751217P | 2013-01-10 | 2013-01-10 | |
| US61/751,217 | 2013-01-10 | ||
| US201361889887P | 2013-10-11 | 2013-10-11 | |
| US61/889,887 | 2013-10-11 | ||
| PCT/US2014/010778 WO2014110200A1 (en) | 2013-01-10 | 2014-01-09 | Non-selective kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018106185A Division JP6547042B2 (ja) | 2013-01-10 | 2018-06-01 | 非選択的キナーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016506418A JP2016506418A (ja) | 2016-03-03 |
| JP2016506418A5 true JP2016506418A5 (enExample) | 2016-04-14 |
| JP6387488B2 JP6387488B2 (ja) | 2018-09-12 |
Family
ID=51167358
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015552757A Active JP6387488B2 (ja) | 2013-01-10 | 2014-01-09 | 非選択的キナーゼ阻害剤 |
| JP2018106185A Active JP6547042B2 (ja) | 2013-01-10 | 2018-06-01 | 非選択的キナーゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018106185A Active JP6547042B2 (ja) | 2013-01-10 | 2018-06-01 | 非選択的キナーゼ阻害剤 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US9815815B2 (enExample) |
| EP (1) | EP3007689B1 (enExample) |
| JP (2) | JP6387488B2 (enExample) |
| CN (2) | CN109568319A (enExample) |
| AU (5) | AU2014205483B2 (enExample) |
| CA (1) | CA2897651C (enExample) |
| DK (1) | DK3007689T3 (enExample) |
| ES (1) | ES2675720T3 (enExample) |
| WO (1) | WO2014110200A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109568319A (zh) | 2013-01-10 | 2019-04-05 | 普尔莫凯恩股份有限公司 | 非选择性激酶抑制剂 |
| WO2014110198A2 (en) * | 2013-01-10 | 2014-07-17 | Zisman Lawrence S | Therapeutic indications of kinase inhibitors |
| KR20150131224A (ko) | 2013-03-14 | 2015-11-24 | 노파르티스 아게 | 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온 |
| JP6799201B2 (ja) * | 2013-07-31 | 2020-12-16 | アヴァリン ファーマ インク． | エアロゾルチロシンキナーゼ阻害剤の化合物、及びその使用 |
| WO2015054574A1 (en) | 2013-10-11 | 2015-04-16 | Zisman Lawrence S | Spray dry formulations |
| CN110087653A (zh) * | 2016-10-27 | 2019-08-02 | 普尔莫凯恩股份有限公司 | 用于治疗肺高血压的组合疗法 |
| CN110573878A (zh) * | 2017-03-16 | 2019-12-13 | 小利兰·斯坦福大学托管委员会 | 用于kras阳性癌症的诊断和治疗方法 |
| US20210038510A1 (en) * | 2018-02-08 | 2021-02-11 | Pulmokine, Inc. | Formulations of kinase inhibitors and prostanoids |
| CN109574296B (zh) * | 2018-11-27 | 2021-05-07 | 合肥工业大学 | 一种从含蟹肉蛋白废水中回收蛋白的方法 |
| US11464776B2 (en) | 2019-05-16 | 2022-10-11 | Aerovate Therapeutics, Inc. | Inhalable imatinib formulations, manufacture, and uses thereof |
| WO2020232238A1 (en) | 2019-05-16 | 2020-11-19 | Aerovate Therapeutics, Inc. | Inhalable formulations for kinase inhibition |
| CN117157282A (zh) * | 2021-05-07 | 2023-12-01 | Gb002股份有限公司 | N-{3-[(1s)-1-{[6-(3,4-二甲氧基苯基)吡嗪-2-基]氨基}乙基]苯基}-5-甲基吡啶-3-甲酰胺的结晶形式及相关产品和方法 |
| KR20240115979A (ko) | 2021-11-08 | 2024-07-26 | 프로젠토스 테라퓨틱스, 인크. | 혈소판-유래 성장 인자 수용체(pdgfr) 알파 억제제 및 이의 용도 |
| CA3260897A1 (en) | 2022-08-10 | 2024-02-15 | Gb002, Inc. | Polytherapy based on a tyrosine kinase inhibitor and a type 2 activin receptor antagonist for the treatment of pulmonary arterial hypertension (PAH) |
| CN119930631B (zh) * | 2025-04-07 | 2025-06-24 | 山东大学 | 一种靶向ddr1受体的化合物及其衍生的放射性示踪剂 |
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