JP2016512208A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016512208A5 JP2016512208A5 JP2015562040A JP2015562040A JP2016512208A5 JP 2016512208 A5 JP2016512208 A5 JP 2016512208A5 JP 2015562040 A JP2015562040 A JP 2015562040A JP 2015562040 A JP2015562040 A JP 2015562040A JP 2016512208 A5 JP2016512208 A5 JP 2016512208A5
- Authority
- JP
- Japan
- Prior art keywords
- fibrosis
- disease
- induced
- ipf
- liver
- 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
- 206010016654 Fibrosis Diseases 0.000 description 37
- 230000004761 fibrosis Effects 0.000 description 33
- 208000019425 cirrhosis of liver Diseases 0.000 description 21
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 description 16
- 208000036971 interstitial lung disease 2 Diseases 0.000 description 16
- 239000003814 drug Substances 0.000 description 9
- 230000037390 scarring Effects 0.000 description 9
- 208000029523 Interstitial Lung disease Diseases 0.000 description 8
- 206010039710 Scleroderma Diseases 0.000 description 8
- 150000001875 compounds Chemical class 0.000 description 8
- 201000010099 disease Diseases 0.000 description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 8
- 229940079593 drug Drugs 0.000 description 8
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 description 8
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 description 8
- 208000005069 pulmonary fibrosis Diseases 0.000 description 7
- 238000000034 method Methods 0.000 description 5
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 description 4
- 206010001881 Alveolar proteinosis Diseases 0.000 description 4
- 206010003210 Arteriosclerosis Diseases 0.000 description 4
- 201000001320 Atherosclerosis Diseases 0.000 description 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 description 4
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 description 4
- 208000033222 Biliary cirrhosis primary Diseases 0.000 description 4
- 108010006654 Bleomycin Proteins 0.000 description 4
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 4
- 208000029147 Collagen-vascular disease Diseases 0.000 description 4
- 201000003883 Cystic fibrosis Diseases 0.000 description 4
- 208000001708 Dupuytren contracture Diseases 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- 206010018364 Glomerulonephritis Diseases 0.000 description 4
- 206010018691 Granuloma Diseases 0.000 description 4
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 description 4
- 208000018565 Hemochromatosis Diseases 0.000 description 4
- 206010020751 Hypersensitivity Diseases 0.000 description 4
- 206010020772 Hypertension Diseases 0.000 description 4
- 208000010159 IgA glomerulonephritis Diseases 0.000 description 4
- 206010021263 IgA nephropathy Diseases 0.000 description 4
- 208000026350 Inborn Genetic disease Diseases 0.000 description 4
- 206010072877 Intestinal fibrosis Diseases 0.000 description 4
- 208000002260 Keloid Diseases 0.000 description 4
- 206010023330 Keloid scar Diseases 0.000 description 4
- 201000005099 Langerhans cell histiocytosis Diseases 0.000 description 4
- 206010049459 Lymphangioleiomyomatosis Diseases 0.000 description 4
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 description 4
- 208000009905 Neurofibromatoses Diseases 0.000 description 4
- 208000004362 Penile Induration Diseases 0.000 description 4
- 208000020758 Peyronie disease Diseases 0.000 description 4
- 206010035664 Pneumonia Diseases 0.000 description 4
- 208000012654 Primary biliary cholangitis Diseases 0.000 description 4
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 description 4
- 201000010001 Silicosis Diseases 0.000 description 4
- 201000009594 Systemic Scleroderma Diseases 0.000 description 4
- 206010042953 Systemic sclerosis Diseases 0.000 description 4
- 208000026911 Tuberous sclerosis complex Diseases 0.000 description 4
- 241000700605 Viruses Species 0.000 description 4
- 238000009825 accumulation Methods 0.000 description 4
- 208000026935 allergic disease Diseases 0.000 description 4
- 208000011775 arteriosclerosis disease Diseases 0.000 description 4
- 239000010425 asbestos Substances 0.000 description 4
- 210000000013 bile duct Anatomy 0.000 description 4
- 229960001561 bleomycin Drugs 0.000 description 4
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 4
- 208000023819 chronic asthma Diseases 0.000 description 4
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 description 4
- 230000007882 cirrhosis Effects 0.000 description 4
- 230000006378 damage Effects 0.000 description 4
- 230000002500 effect on skin Effects 0.000 description 4
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 description 4
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 description 4
- 230000009610 hypersensitivity Effects 0.000 description 4
- 230000001969 hypertrophic effect Effects 0.000 description 4
- 230000000642 iatrogenic effect Effects 0.000 description 4
- 208000015181 infectious disease Diseases 0.000 description 4
- 210000001117 keloid Anatomy 0.000 description 4
- 230000002503 metabolic effect Effects 0.000 description 4
- 206010028537 myelofibrosis Diseases 0.000 description 4
- 201000004931 neurofibromatosis Diseases 0.000 description 4
- 230000002265 prevention Effects 0.000 description 4
- 201000002793 renal fibrosis Diseases 0.000 description 4
- 208000037803 restenosis Diseases 0.000 description 4
- 229910052895 riebeckite Inorganic materials 0.000 description 4
- 201000000306 sarcoidosis Diseases 0.000 description 4
- 208000020431 spinal cord injury Diseases 0.000 description 4
- 208000011580 syndromic disease Diseases 0.000 description 4
- 208000009999 tuberous sclerosis Diseases 0.000 description 4
- 208000037999 tubulointerstitial fibrosis Diseases 0.000 description 4
- 230000002792 vascular Effects 0.000 description 4
- 206010003827 Autoimmune hepatitis Diseases 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- 206010019668 Hepatic fibrosis Diseases 0.000 description 3
- 208000000185 Localized scleroderma Diseases 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 208000016361 genetic disease Diseases 0.000 description 3
- 230000006698 induction Effects 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 231100000331 toxic Toxicity 0.000 description 3
- 230000002588 toxic effect Effects 0.000 description 3
- LFTLOKWAGJYHHR-UHFFFAOYSA-N N-methylmorpholine N-oxide Chemical compound CN1(=O)CCOCC1 LFTLOKWAGJYHHR-UHFFFAOYSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 description 2
- 238000010790 dilution Methods 0.000 description 2
- 239000012895 dilution Substances 0.000 description 2
- 239000010410 layer Substances 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- MCUXGRJXNJGKPY-UHFFFAOYSA-N 1-[6-bromo-3-[[4-(4-fluorophenyl)-1,3-thiazol-2-yl]-methylamino]imidazo[1,2-a]pyridin-2-yl]-2-phenylethane-1,2-diol Chemical compound C=1C=CC=CC=1C(O)C(O)C=1N=C2C=CC(Br)=CN2C=1N(C)C(SC=1)=NC=1C1=CC=C(F)C=C1 MCUXGRJXNJGKPY-UHFFFAOYSA-N 0.000 description 1
- QKNYBSVHEMOAJP-UHFFFAOYSA-N 2-amino-2-(hydroxymethyl)propane-1,3-diol;hydron;chloride Chemical compound Cl.OCC(N)(CO)CO QKNYBSVHEMOAJP-UHFFFAOYSA-N 0.000 description 1
- UHNYTFYKANFKII-UHFFFAOYSA-N 6-bromo-3-[[4-(4-fluorophenyl)-1,3-thiazol-2-yl]-methylamino]imidazo[1,2-a]pyridine-2-carbaldehyde Chemical compound O=CC=1N=C2C=CC(Br)=CN2C=1N(C)C(SC=1)=NC=1C1=CC=C(F)C=C1 UHNYTFYKANFKII-UHFFFAOYSA-N 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- 102000010834 Extracellular Matrix Proteins Human genes 0.000 description 1
- 108010037362 Extracellular Matrix Proteins Proteins 0.000 description 1
- 102000016359 Fibronectins Human genes 0.000 description 1
- 108010067306 Fibronectins Proteins 0.000 description 1
- 208000028782 Hereditary disease Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 208000024556 Mendelian disease Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 230000005784 autoimmunity Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 229920001436 collagen Polymers 0.000 description 1
- 230000008602 contraction Effects 0.000 description 1
- 210000004087 cornea Anatomy 0.000 description 1
- 239000012043 crude product Substances 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 210000002744 extracellular matrix Anatomy 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 210000002216 heart Anatomy 0.000 description 1
- 208000006454 hepatitis Diseases 0.000 description 1
- 231100000283 hepatitis Toxicity 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 229910000489 osmium tetroxide Inorganic materials 0.000 description 1
- 239000012285 osmium tetroxide Substances 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361781174P | 2013-03-14 | 2013-03-14 | |
| US61/781,174 | 2013-03-14 | ||
| PCT/EP2014/054440 WO2014139882A1 (en) | 2013-03-14 | 2014-03-07 | Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018072964A Division JP6517976B2 (ja) | 2013-03-14 | 2018-04-05 | 炎症性障害の治療のための化合物及びその医薬組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016512208A JP2016512208A (ja) | 2016-04-25 |
| JP2016512208A5 true JP2016512208A5 (enExample) | 2017-04-06 |
| JP6339595B2 JP6339595B2 (ja) | 2018-06-06 |
Family
ID=50236198
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015562040A Active JP6339595B2 (ja) | 2013-03-14 | 2014-03-07 | 炎症性障害の治療のための化合物及びその医薬組成物 |
| JP2018072964A Active JP6517976B2 (ja) | 2013-03-14 | 2018-04-05 | 炎症性障害の治療のための化合物及びその医薬組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018072964A Active JP6517976B2 (ja) | 2013-03-14 | 2018-04-05 | 炎症性障害の治療のための化合物及びその医薬組成物 |
Country Status (29)
| Country | Link |
|---|---|
| US (7) | US8993590B2 (enExample) |
| EP (3) | EP3269716B1 (enExample) |
| JP (2) | JP6339595B2 (enExample) |
| KR (2) | KR20210034098A (enExample) |
| CN (1) | CN105143221B (enExample) |
| AR (1) | AR095280A1 (enExample) |
| AU (3) | AU2014231009B2 (enExample) |
| BR (1) | BR112015020998B1 (enExample) |
| CA (1) | CA2902103C (enExample) |
| CY (2) | CY1119352T1 (enExample) |
| DK (2) | DK3269716T3 (enExample) |
| ES (2) | ES2824723T3 (enExample) |
| HR (2) | HRP20171219T1 (enExample) |
| HU (2) | HUE051195T2 (enExample) |
| IL (2) | IL240531B (enExample) |
| LT (2) | LT2970255T (enExample) |
| MX (1) | MX358342B (enExample) |
| MY (1) | MY170260A (enExample) |
| NZ (1) | NZ711202A (enExample) |
| PH (1) | PH12015502055B1 (enExample) |
| PL (2) | PL2970255T3 (enExample) |
| PT (2) | PT2970255T (enExample) |
| RU (1) | RU2675818C2 (enExample) |
| SG (1) | SG11201507224RA (enExample) |
| SI (2) | SI2970255T1 (enExample) |
| TW (2) | TWI695002B (enExample) |
| UY (1) | UY35437A (enExample) |
| WO (1) | WO2014139882A1 (enExample) |
| ZA (1) | ZA201505909B (enExample) |
Families Citing this family (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012308570B2 (en) | 2011-09-14 | 2016-11-10 | Samumed, Llc | Indazole-3-carboxamides and their use as Wnt/b-catenin signaling pathway inhibitors |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| HUE051195T2 (hu) | 2013-03-14 | 2021-03-01 | Galapagos Nv | Új vegyületek és gyógyászati készítményeik gyulladásos rendellenességek kezelésére |
| US9796719B2 (en) | 2013-06-19 | 2017-10-24 | Galapagos Nv | Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
| CA2927541C (en) | 2013-10-15 | 2021-06-08 | Radux Devices, LLC | Securing a medical device to a valve instrument |
| MX386798B (es) | 2014-08-29 | 2025-03-19 | Chdi Foundation Inc | Sondas para la proyección de imagen de la proteína huntingtina. |
| WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
| WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| GB201501870D0 (en) | 2015-02-04 | 2015-03-18 | Cancer Rec Tech Ltd | Autotaxin inhibitors |
| GB201502020D0 (en) | 2015-02-06 | 2015-03-25 | Cancer Rec Tech Ltd | Autotaxin inhibitory compounds |
| CA2988306A1 (en) | 2015-06-05 | 2016-12-08 | Vertex Pharmaceuticals Incorporated | Triazoles for the treatment of demyelinating diseases |
| JP6871919B2 (ja) | 2015-06-16 | 2021-05-19 | ナノファギックス エルエルシー | 薬物送達及びイメージング化学コンジュゲート、製剤及びその使用方法 |
| US10195185B2 (en) | 2015-08-03 | 2019-02-05 | Samumed, Llc | 3-(1H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017024003A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10226448B2 (en) | 2015-08-03 | 2019-03-12 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-yl)-1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof |
| US10350199B2 (en) | 2015-08-03 | 2019-07-16 | Samumed, Llc | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| US10519169B2 (en) | 2015-08-03 | 2019-12-31 | Samumed, Llc | 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10285983B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof |
| WO2017023989A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017024004A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017023993A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10604512B2 (en) | 2015-08-03 | 2020-03-31 | Samumed, Llc | 3-(1H-indol-2-yl)-1H-indazoles and therapeutic uses thereof |
| US10383861B2 (en) | 2015-08-03 | 2019-08-20 | Sammumed, LLC | 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| US10206908B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| US10463651B2 (en) | 2015-08-03 | 2019-11-05 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof |
| WO2017023980A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| WO2017024015A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| CN108473491A (zh) * | 2015-11-06 | 2018-08-31 | 萨穆梅德有限公司 | 2-(1h-吲唑-3-基)-3h-咪唑并[4,5-c]吡啶以及其抗炎用途 |
| US11065251B2 (en) | 2016-05-06 | 2021-07-20 | Albert Einstein College Of Medicine | PAK1 inhibitors and uses thereof |
| DK3464285T3 (da) | 2016-06-01 | 2022-12-19 | Biosplice Therapeutics Inc | Fremgangsmåde til fremstilling af n-(5-(3-(7-(3-fluorphenyl)-3h-imidazo[4,5-c]pyridin-2-yl)-1h-indazol-5-yl)pyridin-3-yl)-3-methylbutanamid |
| EP3528808B1 (en) | 2016-10-21 | 2021-10-06 | BioSplice Therapeutics, Inc. | Methods of using indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors |
| WO2018080572A1 (en) | 2016-10-24 | 2018-05-03 | Precision Combustion, Inc. | Regenerative solid oxide stack |
| MA46696A (fr) | 2016-11-07 | 2019-09-11 | Samumed Llc | Formulations injectables à dose unique prêtes à l'emploi |
| WO2018106646A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Aminotriazoles for the treatment of demyelinating diseases |
| WO2018106643A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Heterocyclic azoles for the treatment of demyelinating diseases |
| WO2018106641A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Pyrazoles for the treatment of demyelinating diseases |
| GB201710851D0 (en) | 2017-07-06 | 2017-08-23 | Galápagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis |
| WO2019029620A1 (zh) * | 2017-08-09 | 2019-02-14 | 广州市恒诺康医药科技有限公司 | Atx抑制剂及其制备方法和应用 |
| MX2020001199A (es) * | 2017-08-09 | 2020-03-24 | Galapagos Nv | Compuestos y composiciones farmaceuticas de los mismos para usarse en el tratamiento de enfermedades fibroticas. |
| CN111343986A (zh) | 2017-11-15 | 2020-06-26 | 加拉帕戈斯股份有限公司 | 用于治疗纤维化疾病的化合物及其药物组合物 |
| EP3753943A4 (en) * | 2018-02-14 | 2021-06-23 | Suzhou Sinovent Pharmaceuticals Co., Ltd. | HETEROCYCLIC COMPOUND, ITS APPLICATION AND PHARMACEUTICAL COMPOSITION CONSISTING OF IT |
| AU2019272377B2 (en) * | 2018-05-24 | 2022-03-10 | Guangzhou Henovcom Bioscience Co., Ltd. | Heteroaromatic compounds, pharmaceutical compositions and uses thereof |
| JP2021526123A (ja) * | 2018-05-29 | 2021-09-30 | シーチュアン ハイスコ ファーマシューティカル シーオー．，エルティーディー． | オートタキシン阻害剤とその使用 |
| ES2952939T3 (es) | 2018-07-27 | 2023-11-07 | Mitsubishi Tanabe Pharma Corp | Derivados novedosos de piridina 3,5-disustituida y piridazina 3,5-disustituida y uso farmacéutico de los mismos |
| GB201812861D0 (en) | 2018-08-08 | 2018-09-19 | Galapagos Nv | Methods of administering therapy |
| US11104665B2 (en) | 2018-10-29 | 2021-08-31 | Boehringer Ingelheim International Gmbh | Pyridazines |
| KR20210108414A (ko) | 2018-12-25 | 2021-09-02 | 솔-겔 테크놀로지스 리미티드 | Egfr 억제제를 포함하는 조성물에 의한 피부 장애 치료 |
| GB201904375D0 (en) * | 2019-03-29 | 2019-05-15 | Galapagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
| CN113874354B (zh) * | 2019-06-04 | 2024-02-20 | 江苏恒瑞医药股份有限公司 | 吡啶酮类衍生物、其制备方法及其在医药上的应用 |
| WO2021034414A2 (en) * | 2019-07-03 | 2021-02-25 | Cornell University | Modulation of dendritic cell function by the phospholipid messenger lpa |
| US11465982B2 (en) | 2019-07-22 | 2022-10-11 | Boehringer Ingelheim International Gmbh | Pyridazines |
| DK4003978T3 (da) | 2019-07-22 | 2024-07-22 | Boehringer Ingelheim Int | N-methyl, n-(6-(methoxy)pyridazin-3-yl) aminderivater som autotaxin (atx) modulatorer til behandlingen af inflammatoriske luftvejs- eller fibrotiske sygdomme |
| US11485727B2 (en) | 2019-07-22 | 2022-11-01 | Boehringer Ingelheim International Gmbh | N-methyl, n-(6-(methoxy)pyridazin-3-yl) amine derivatives as autotaxin (ATX) modulators |
| EP3782997A1 (en) | 2019-08-19 | 2021-02-24 | Galapagos N.V. | Fused pyrimidine compounds and pharmaceutical compositions thereof for the treatment of fibrotic diseases |
| IL291114B2 (en) * | 2019-09-06 | 2025-09-01 | Wuhan Humanwell Innovative Drug Res And Development Center Limited Company | Pyrimidine compound and method for preparing same |
| CN112778334B (zh) * | 2019-11-07 | 2022-04-15 | 广州市恒诺康医药科技有限公司 | 芳杂环化合物、其药物组合物及其应用 |
| CN111004235A (zh) * | 2019-11-29 | 2020-04-14 | 沈阳药科大学 | 一种ATX抑制剂Ziritaxestat的合成方法 |
| CN113493453B (zh) * | 2020-04-07 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 稠合芳香环类衍生物、其制备方法及其在医药上的应用 |
| TW202202499A (zh) * | 2020-07-09 | 2022-01-16 | 大陸商蘇州愛科百發生物醫藥技術有限公司 | 一種atx抑制劑及其製備方法和應用 |
| CN114315825A (zh) * | 2020-09-30 | 2022-04-12 | 江西济民可信集团有限公司 | 吡啶并咪唑衍生物及其制备方法和应用 |
| AR123686A1 (es) | 2020-10-06 | 2023-01-04 | Ildong Pharmaceutical Co Ltd | Compuestos inhibidores de la autotaxina |
| CN116437917B (zh) * | 2020-11-04 | 2024-12-13 | 西藏海思科制药有限公司 | Atx抑制剂氘代衍生物及其应用 |
| CA3199039A1 (en) * | 2020-11-16 | 2022-05-19 | Qingan ZOU | Imidazothiazole compounds, pharmaceutical compositions, and uses thereof |
| PT4274572T (pt) | 2021-01-05 | 2026-03-11 | Zydus Lifesciences Ltd | Novos inibidores da autotaxina |
| KR20230153387A (ko) | 2021-02-02 | 2023-11-06 | 리미널 바이오사이언시스 리미티드 | Gpr84 길항제 및 이의 용도 |
| JP2024506858A (ja) | 2021-02-02 | 2024-02-15 | リミナル・バイオサイエンシーズ・リミテッド | Ｇｐｒ８４アンタゴニストおよびその使用 |
| CA3239101A1 (en) * | 2021-11-25 | 2023-06-01 | Gang Deng | Tricyclic derivative and preparation method therefor and application thereof |
| WO2023235871A2 (en) * | 2022-06-03 | 2023-12-07 | Seer, Inc. | Systems, compositions, and methods relating to neurodegenerative diseases |
| KR102587919B1 (ko) * | 2022-07-22 | 2023-10-11 | 주식회사 넥스트젠바이오사이언스 | 신규한 헤테로사이클릭 화합물 및 이를 포함하는 오토탁신 저해용 약학 조성물 |
| JP2025527250A (ja) | 2022-08-02 | 2025-08-20 | リミナル・バイオサイエンシーズ・リミテッド | ヘテロアリールカルボキサミド及び関連するｇｐｒ８４アンタゴニストならびにそれらの使用 |
| JP2025527248A (ja) | 2022-08-02 | 2025-08-20 | リミナル・バイオサイエンシーズ・リミテッド | 置換ピリドンｇｐｒ８４アンタゴニスト及びその使用 |
| JP2025527247A (ja) | 2022-08-02 | 2025-08-20 | リミナル・バイオサイエンシーズ・リミテッド | アリール－トリアゾリル及び関連するｇｐｒ８４アンタゴニストならびにそれらの使用 |
| GR1010570B (el) | 2022-12-22 | 2023-11-17 | Uni-Pharma Κλεων Τσετης Φαρμακευτικα Εργαστηρια Α.Β.Ε.Ε., | 4-(2-(4-((2,4-διοξοθειαζολιδιν-5-υλ)μεθυλ)φαινοξυ) παραγωγα με δραση αναστολης της αυτοταξινης |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1218382E (pt) * | 1999-10-08 | 2004-06-30 | Gruenenthal Gmbh | Derivados de imidazo-3-il-amina biciclica |
| EP1622912B1 (en) * | 2003-04-23 | 2009-05-27 | Schering Corporation | 2-alkynyl-and 2-alkenyl-pyrazolo- [4,3-e ] -1,2,4-triazolo- [1,5-c] -pyrimidine adenosine a2a receptor antagonists |
| US20080015193A1 (en) * | 2006-06-20 | 2008-01-17 | Mendoza Jose S | Certain azoles exhibiting ATP-utilizing enzyme inhibitory activity, compositions, and uses thereof |
| US8227603B2 (en) * | 2006-08-01 | 2012-07-24 | Cytokinetics, Inc. | Modulating skeletal muscle |
| WO2008138842A1 (en) * | 2007-05-10 | 2008-11-20 | Galapagos N.V. | Imidazopyrazines and triazolopyrazine for the treatment of joint degenerative and inflammatory diseases |
| DE102008059578A1 (de) | 2008-11-28 | 2010-06-10 | Merck Patent Gmbh | Benzo-Naphtyridin Verbindungen |
| EA201100879A1 (ru) * | 2008-12-01 | 2012-01-30 | Мерк Патент Гмбх | Производные пиридопиримидина в качестве ингибиторов аутотаксина |
| CA2757415C (en) | 2009-04-02 | 2018-02-06 | Merck Patent Gmbh | Autotaxin inhibitors |
| TW201120043A (en) * | 2009-11-05 | 2011-06-16 | Galapagos Nv | Fused pyrazine compounds as their salts, useful for the treatment of degenerative and inflammatory diseases |
| EP2338888A1 (en) * | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
| ES2646834T3 (es) * | 2010-08-20 | 2017-12-18 | Amira Pharmaceuticals, Inc. | Inhibidores de autotaxina y usos de los mismos |
| US20130052190A1 (en) * | 2011-02-22 | 2013-02-28 | Oxagen Limited | CRTH2 Antagonists for Treatment of Eosinophilic Diseases and Conditions |
| US9260416B2 (en) * | 2011-05-27 | 2016-02-16 | Amira Pharmaceuticals, Inc. | Heterocyclic autotaxin inhibitors and uses thereof |
| HUE051195T2 (hu) * | 2013-03-14 | 2021-03-01 | Galapagos Nv | Új vegyületek és gyógyászati készítményeik gyulladásos rendellenességek kezelésére |
-
2014
- 2014-03-07 HU HUE17177371A patent/HUE051195T2/hu unknown
- 2014-03-07 HR HRP20171219TT patent/HRP20171219T1/hr unknown
- 2014-03-07 BR BR112015020998-0A patent/BR112015020998B1/pt not_active IP Right Cessation
- 2014-03-07 SI SI201430403T patent/SI2970255T1/sl unknown
- 2014-03-07 KR KR1020217008013A patent/KR20210034098A/ko not_active Ceased
- 2014-03-07 PL PL14708291T patent/PL2970255T3/pl unknown
- 2014-03-07 CN CN201480014005.8A patent/CN105143221B/zh active Active
- 2014-03-07 EP EP17177371.6A patent/EP3269716B1/en active Active
- 2014-03-07 ES ES17177371T patent/ES2824723T3/es active Active
- 2014-03-07 SI SI201431673T patent/SI3269716T1/sl unknown
- 2014-03-07 RU RU2015143430A patent/RU2675818C2/ru active
- 2014-03-07 KR KR1020157029122A patent/KR102231637B1/ko not_active Expired - Fee Related
- 2014-03-07 ES ES14708291.1T patent/ES2638980T3/es active Active
- 2014-03-07 DK DK17177371.6T patent/DK3269716T3/da active
- 2014-03-07 JP JP2015562040A patent/JP6339595B2/ja active Active
- 2014-03-07 MX MX2015011077A patent/MX358342B/es active IP Right Grant
- 2014-03-07 DK DK14708291.1T patent/DK2970255T3/en active
- 2014-03-07 LT LTEP14708291.1T patent/LT2970255T/lt unknown
- 2014-03-07 PL PL17177371T patent/PL3269716T3/pl unknown
- 2014-03-07 MY MYPI2015703027A patent/MY170260A/en unknown
- 2014-03-07 PT PT147082911T patent/PT2970255T/pt unknown
- 2014-03-07 SG SG11201507224RA patent/SG11201507224RA/en unknown
- 2014-03-07 HU HUE14708291A patent/HUE035966T2/en unknown
- 2014-03-07 PT PT171773716T patent/PT3269716T/pt unknown
- 2014-03-07 LT LTEP17177371.6T patent/LT3269716T/lt unknown
- 2014-03-07 EP EP14708291.1A patent/EP2970255B9/en active Active
- 2014-03-07 CA CA2902103A patent/CA2902103C/en active Active
- 2014-03-07 NZ NZ711202A patent/NZ711202A/en not_active IP Right Cessation
- 2014-03-07 WO PCT/EP2014/054440 patent/WO2014139882A1/en not_active Ceased
- 2014-03-07 AU AU2014231009A patent/AU2014231009B2/en not_active Ceased
- 2014-03-07 EP EP20189787.3A patent/EP3760630A1/en not_active Withdrawn
- 2014-03-11 TW TW103108497A patent/TWI695002B/zh not_active IP Right Cessation
- 2014-03-11 TW TW108104845A patent/TWI749290B/zh not_active IP Right Cessation
- 2014-03-12 AR ARP140100893A patent/AR095280A1/es active IP Right Grant
- 2014-03-12 US US14/205,885 patent/US8993590B2/en active Active
- 2014-03-14 UY UY35437A patent/UY35437A/es not_active Application Discontinuation
- 2014-12-17 US US14/572,870 patent/US9249141B2/en active Active
-
2015
- 2015-08-12 IL IL240531A patent/IL240531B/en active IP Right Grant
- 2015-08-17 ZA ZA2015/05909A patent/ZA201505909B/en unknown
- 2015-09-11 PH PH12015502055A patent/PH12015502055B1/en unknown
- 2015-12-22 US US14/977,918 patent/US9670204B2/en not_active Expired - Fee Related
-
2017
- 2017-05-01 US US15/583,161 patent/US10125132B2/en active Active
- 2017-09-06 CY CY20171100940T patent/CY1119352T1/el unknown
- 2017-12-20 AU AU2017286828A patent/AU2017286828B2/en not_active Ceased
- 2017-12-27 IL IL256624A patent/IL256624B/en active IP Right Grant
-
2018
- 2018-04-05 JP JP2018072964A patent/JP6517976B2/ja active Active
- 2018-09-28 US US16/146,450 patent/US10526329B2/en active Active
-
2019
- 2019-06-27 AU AU2019204539A patent/AU2019204539B2/en not_active Ceased
- 2019-11-13 US US16/682,553 patent/US11072611B2/en active Active
-
2020
- 2020-10-09 CY CY20201100953T patent/CY1123521T1/el unknown
- 2020-10-13 HR HRP20201641TT patent/HRP20201641T1/hr unknown
-
2021
- 2021-06-18 US US17/351,765 patent/US20230022534A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR100698982B1 (ko) | Ｐｄｅ4 억제제로서 유용한 니코틴아미드 유도체 | |
| US8440672B2 (en) | Diphenyl substituted alkanes | |
| US8426413B2 (en) | Diaryl substituted alkanes | |
| EP2701512B1 (en) | Aldosterone synthase inhibitors | |
| JP2004518691A (ja) | Ｐｄｅ４アイソザイムの阻害剤として有効なチアゾリル−、オキサゾリル−、ピロリル−、イミダゾリル−酸アミド誘導体 | |
| KR20020071029A (ko) | Ｐｄｅ４ 이소자임 억제제로 유용한 피리미딘카르복스아미드 | |
| EP3793995B1 (en) | Matrix metalloproteinase (mmp) inhibitors and methods of use thereof | |
| JP2018516254A (ja) | バニン１酵素の阻害薬としての新規なヘテロ環化合物 | |
| TW201441185A (zh) | 用於治療肺纖維化、肝纖維化、皮膚纖維化及心臟纖維化之經取代之芳族化合物 | |
| KR20070014174A (ko) | 히스타민 ｈ3 수용체 리간드로서 유용한테트라하이드로나프티리딘 유도체 | |
| HRP20040151A2 (en) | Alkyne-aryl phosphodiesterase-4 inhibitors | |
| JP2002284766A (ja) | Ｐｄｅ４アイソザイムの阻害剤として活性なニコチンアミド酸類、アミド類およびそれらの模倣剤 | |
| CN105143221A (zh) | 用于治疗炎性障碍的化合物及其药物组合物 | |
| CN101243055A (zh) | 二氢嘧啶酮多聚体及其作为人中性粒细胞弹性蛋白酶抑制剂的用途 | |
| CN101495454A (zh) | 新型pde4抑制剂 | |
| JP2021035975A (ja) | 疾患を治療するための方法及び薬剤 | |
| JP4012935B2 (ja) | Ｐｄｅ４阻害剤として有用なニコチンアミド誘導体 | |
| US20100196476A1 (en) | Process for the preparation and pharmaceutical formulations for 4-quinolinones and quinolines and use thereof | |
| WO2022020381A1 (en) | Inhibitors of rho-associated coiled-coil kinase | |
| JP2006169138A (ja) | ピラゾロピリジンピラゾロン誘導体とその付加塩及びｐｄｅ阻害剤 | |
| PE20081664A1 (es) | Derivados de azabicicloalcano, su preparacion y su aplicacion en terapeutica | |
| TW200831463A (en) | Nitrate esters of aminoalcohols | |
| CN100366618C (zh) | 作为磷酸二酯酶4抑制剂的酞嗪衍生物 | |
| JP2006528658A (ja) | Ｐｄｅ４阻害薬として有用なニコチンアミド化合物 | |
| RU2820540C2 (ru) | Ингибиторы матриксной металлопротеиназы (mmp) и способы их применения |