JP6767875B2 - Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法 - Google Patents
Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法 Download PDFInfo
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- JP6767875B2 JP6767875B2 JP2016561626A JP2016561626A JP6767875B2 JP 6767875 B2 JP6767875 B2 JP 6767875B2 JP 2016561626 A JP2016561626 A JP 2016561626A JP 2016561626 A JP2016561626 A JP 2016561626A JP 6767875 B2 JP6767875 B2 JP 6767875B2
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- alkyl
- compound
- pyridine
- nmr
- indazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
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- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
- C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
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- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
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- Pharmacology & Pharmacy (AREA)
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- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Biomedical Technology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461976880P | 2014-04-08 | 2014-04-08 | |
| US61/976,880 | 2014-04-08 | ||
| US201462019577P | 2014-07-01 | 2014-07-01 | |
| US62/019,577 | 2014-07-01 | ||
| PCT/US2015/024146 WO2015157093A1 (en) | 2014-04-08 | 2015-04-02 | 2,3-disubstituted pyridine compounds as tgf-beta inhibitors and methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019134857A Division JP2019196387A (ja) | 2014-04-08 | 2019-07-22 | Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017515802A JP2017515802A (ja) | 2017-06-15 |
| JP2017515802A5 JP2017515802A5 (enExample) | 2018-05-24 |
| JP6767875B2 true JP6767875B2 (ja) | 2020-10-14 |
Family
ID=52875332
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016561626A Expired - Fee Related JP6767875B2 (ja) | 2014-04-08 | 2015-04-02 | Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法 |
| JP2019134857A Withdrawn JP2019196387A (ja) | 2014-04-08 | 2019-07-22 | Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019134857A Withdrawn JP2019196387A (ja) | 2014-04-08 | 2019-07-22 | Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US10233170B2 (enExample) |
| EP (1) | EP3129367B1 (enExample) |
| JP (2) | JP6767875B2 (enExample) |
| CN (1) | CN106536507B (enExample) |
| ES (1) | ES2759240T3 (enExample) |
| TW (1) | TW201623279A (enExample) |
| UY (1) | UY36068A (enExample) |
| WO (1) | WO2015157093A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019196387A (ja) * | 2014-04-08 | 2019-11-14 | ライジェル ファーマシューティカルズ, インコーポレイテッド | Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法 |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016133838A1 (en) | 2015-02-20 | 2016-08-25 | Rigel Pharmaceuticals, Inc. | Gdf-8 inhibitors |
| HK1255330A1 (zh) | 2015-08-26 | 2019-08-16 | 缆图药品公司 | 适用於治疗与ntrk相关的病症的化合物和组合物 |
| CA3005741A1 (en) * | 2015-11-19 | 2017-05-26 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to ntrk |
| ES2918589T3 (es) * | 2015-11-25 | 2022-07-19 | Convergene Llc | Inhibidores de bromodomios BET bicíclicos y usos de los mismos |
| JP7026299B2 (ja) * | 2016-03-24 | 2022-02-28 | コセラ バイオサイエンス, インコーポレイテッド | Tg02によるがん治療 |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Hdac抑制劑與pd-l1抑制劑之組合治療 |
| WO2018013430A2 (en) | 2016-07-12 | 2018-01-18 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus infection |
| CA3039220A1 (en) * | 2016-10-26 | 2018-05-03 | Icahn School Of Medicine At Mount Sinai | Method for increasing cell proliferation in pancreatic beta cells, treatment method, and composition |
| MX393780B (es) | 2017-01-17 | 2025-03-24 | Heparegenix Gmbh | Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos |
| RU2019126455A (ru) * | 2017-01-23 | 2021-02-24 | Революшн Медсинз, Инк. | Пиридиновые соединения в качестве аллостерических ингибиторов shp2 |
| CN108570038B (zh) * | 2017-03-08 | 2021-09-28 | 中国科学院上海药物研究所 | 二氢喹喔啉类溴结构域识别蛋白抑制剂及制备方法和用途 |
| CN107118210A (zh) * | 2017-04-28 | 2017-09-01 | 贵州大学 | 一种3‑碘‑6‑(三氟甲基)咪唑并[1,2‑a]吡啶的制备工艺 |
| JP2021503486A (ja) | 2017-11-20 | 2021-02-12 | アイカーン スクール オブ メディシン アット マウント サイナイ | キナーゼ阻害剤化合物ならびに組成物および使用法 |
| CN111819193A (zh) | 2018-01-05 | 2020-10-23 | 西奈山伊坎医学院 | 增加胰腺β细胞增殖的方法、治疗方法以及组合物 |
| US11866427B2 (en) | 2018-03-20 | 2024-01-09 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
| EA202191619A1 (ru) | 2018-12-27 | 2021-09-28 | Нексис Терапьютикс, Инк. | Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразований |
| CN113166109B (zh) * | 2018-12-28 | 2024-01-02 | 四川科伦博泰生物医药股份有限公司 | 氨基吡啶类化合物及其制备方法和用途 |
| WO2020203763A1 (ja) | 2019-03-29 | 2020-10-08 | 住友化学株式会社 | 複素環化合物及びそれを含有する有害節足動物防除組成物 |
| PE20220425A1 (es) | 2019-04-29 | 2022-03-29 | Solent Therapeutics Llc | Derivado de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2 |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| CN115916759B (zh) * | 2020-06-19 | 2025-07-15 | 泰州红云制药有限公司 | 取代喹唑啉类化合物、其制备方法、药物组合及应用 |
| WO2021263129A1 (en) * | 2020-06-26 | 2021-12-30 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| JP7704770B2 (ja) | 2020-09-30 | 2025-07-08 | 住友化学株式会社 | 複素環化合物及びそれを含有する有害節足動物防除組成物 |
| CN112225736B (zh) * | 2020-11-12 | 2022-04-15 | 山东省科学院菏泽分院 | 一种6-溴咪唑并[1.2-a]吡啶-3-甲醛的制备方法 |
| WO2022246025A1 (en) * | 2021-05-20 | 2022-11-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors and degraders of pip4k protein |
| CN113416181B (zh) * | 2021-08-02 | 2022-05-03 | 四川大学 | 喹唑啉类衍生物及其用途 |
| CN114292259B (zh) * | 2021-11-30 | 2023-06-27 | 西安交通大学 | 4-氨基酸侧链取代的喹唑啉衍生物及其应用 |
| WO2023107714A2 (en) * | 2021-12-10 | 2023-06-15 | Prothena Biosciences Limited | Methods for treating neurological disorders |
| EP4596547A1 (en) | 2022-09-30 | 2025-08-06 | Sumitomo Chemical Company, Limited | Heterocyclic compound and harmful arthropod-controlling composition containing same |
| TW202423290A (zh) | 2022-11-04 | 2024-06-16 | 日商住友化學股份有限公司 | 雜環化合物及含有其之有害節肢動物防除組合物 |
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| US7320789B2 (en) * | 2001-09-26 | 2008-01-22 | Wyeth | Antibody inhibitors of GDF-8 and uses thereof |
| EP1720855A4 (en) * | 2004-03-02 | 2008-12-17 | Smithkline Beecham Corp | HEMMER OF ACT ACTIVITY |
| AU2005295734A1 (en) * | 2004-10-15 | 2006-04-27 | Biogen Idec Ma Inc. | Methods of treating vascular injuries |
| WO2008009078A2 (en) * | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| CA2694261A1 (en) | 2007-07-26 | 2009-01-29 | Novartis Ag | Organic compounds |
| WO2009032653A1 (en) * | 2007-08-31 | 2009-03-12 | Smith Kline Beecham Corporation | Inhibitors of akt activity |
| MX2012008550A (es) * | 2010-02-05 | 2012-09-07 | Merck Patent Gmbh | Derivados de hetaril-[1, 8]naftiridina. |
| MX2013010163A (es) * | 2011-03-09 | 2013-10-30 | Merck Patent Gmbh | Derivados de pirido[2,3-b] pirazina y sus usos terapeuticos. |
| RU2612958C2 (ru) * | 2011-07-13 | 2017-03-14 | Ск Кемикалз Ко., Лтд. | 2-пиридилзамещенные имидазолы в качестве ингибиторов alk5 и/или alk4 |
| MX2015004151A (es) * | 2012-10-05 | 2015-07-06 | Rigel Pharmaceuticals Inc | Inhibidores del factor de diferenciacion de crecimiento-8 (gdf-8). |
| US10233170B2 (en) * | 2014-04-08 | 2019-03-19 | Rigel Pharmaceuticals, Inc. | 2,3-disubstituted pyridine compounds as TGF-beta inhibitors and methods of use |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019196387A (ja) * | 2014-04-08 | 2019-11-14 | ライジェル ファーマシューティカルズ, インコーポレイテッド | Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法 |
Also Published As
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|---|---|
| JP2019196387A (ja) | 2019-11-14 |
| JP2017515802A (ja) | 2017-06-15 |
| UY36068A (es) | 2015-10-30 |
| US10858335B2 (en) | 2020-12-08 |
| US20170096409A1 (en) | 2017-04-06 |
| ES2759240T3 (es) | 2020-05-08 |
| CN106536507A (zh) | 2017-03-22 |
| EP3129367B1 (en) | 2019-09-04 |
| EP3129367A1 (en) | 2017-02-15 |
| US20190284155A1 (en) | 2019-09-19 |
| TW201623279A (zh) | 2016-07-01 |
| CN106536507B (zh) | 2020-04-07 |
| US10233170B2 (en) | 2019-03-19 |
| WO2015157093A1 (en) | 2015-10-15 |
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