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
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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
- A61K31/435—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
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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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- C07D401/02—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
- 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
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- 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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- 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
- C07D417/14—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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- 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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- 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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- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Biomedical Technology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (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)
- 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 (OSRAM) | 2018-05-24 |
| JP6767875B2 true JP6767875B2 (ja) | 2020-10-14 |
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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 (OSRAM) |
| EP (1) | EP3129367B1 (OSRAM) |
| JP (2) | JP6767875B2 (OSRAM) |
| CN (1) | CN106536507B (OSRAM) |
| ES (1) | ES2759240T3 (OSRAM) |
| TW (1) | TW201623279A (OSRAM) |
| UY (1) | UY36068A (OSRAM) |
| WO (1) | WO2015157093A1 (OSRAM) |
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 |
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| JP6800158B2 (ja) * | 2015-02-20 | 2020-12-16 | 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 | Gdf−8阻害剤 |
| CN108137607B (zh) | 2015-08-26 | 2021-04-06 | 缆图药品公司 | 适用于治疗与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 |
| CN109641886B (zh) * | 2015-11-25 | 2022-11-18 | 康威基内有限公司 | 双环bet布罗莫结构域抑制剂及其用途 |
| SG11201808306PA (en) * | 2016-03-24 | 2018-10-30 | Tragara Pharmaceuticals Inc | Treatment of cancer with tg02 |
| 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 |
| 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 |
| WO2018013430A2 (en) | 2016-07-12 | 2018-01-18 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus infection |
| US11266647B2 (en) | 2016-10-26 | 2022-03-08 | Icahn School Of Medicine At Mount Sinai | Method for increasing cell proliferation in pancreatic beta cells, treatment method, and composition |
| WO2018134254A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| RU2019126455A (ru) * | 2017-01-23 | 2021-02-24 | Революшн Медсинз, Инк. | Пиридиновые соединения в качестве аллостерических ингибиторов shp2 |
| US11078188B2 (en) * | 2017-03-08 | 2021-08-03 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof |
| 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 |
| WO2019100062A1 (en) | 2017-11-20 | 2019-05-23 | Ichan School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| JP2021510153A (ja) | 2018-01-05 | 2021-04-15 | 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 | 膵臓ベータ細胞の増殖を増加させる方法、治療方法、および組成物 |
| WO2019183245A1 (en) | 2018-03-20 | 2019-09-26 | 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 |
| AU2019417418B2 (en) | 2018-12-27 | 2025-02-27 | Nexys Therapeutics, Inc. | (pyridin-2-yl)amine derivatives as ΤGFβR1 (Alk5) inhibitors for the treatment of cancer |
| 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 |
| PH12021500043A1 (en) | 2019-03-29 | 2022-06-06 | Sumitomo Chemical Co | Heterocyclic compound and harmful arthropod pest control composition containing same |
| TWI846868B (zh) | 2019-04-29 | 2024-07-01 | 美商索倫特醫療有限責任公司 | 作為mrgx2抑制劑之3-胺基-4h-苯并[e][1,2,4]噻二嗪1,1-二氧化物衍生物 |
| 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 |
| US20230234935A1 (en) * | 2020-06-26 | 2023-07-27 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| WO2022071434A1 (ja) | 2020-09-30 | 2022-04-07 | 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 |
| US20240277852A1 (en) * | 2021-05-20 | 2024-08-22 | 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 |
| KR20240133695A (ko) * | 2021-12-10 | 2024-09-04 | 프로테나 바이오사이언시즈 리미티드 | Dyrk1a 억제제로서의 헤테로시클릭 화합물 |
| WO2024071393A1 (ja) | 2022-09-30 | 2024-04-04 | 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 |
| EP4613750A1 (en) | 2022-11-04 | 2025-09-10 | Sumitomo Chemical Company, Limited | Heterocyclic compound and harmful arthropod control composition containing same |
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| US7320789B2 (en) * | 2001-09-26 | 2008-01-22 | Wyeth | Antibody inhibitors of GDF-8 and uses thereof |
| WO2005085227A1 (en) * | 2004-03-02 | 2005-09-15 | Smithkline Beecham Corporation | Inhibitors of akt activity |
| JP2008516962A (ja) * | 2004-10-15 | 2008-05-22 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | 血管傷害を治療する方法 |
| US9259426B2 (en) * | 2006-07-20 | 2016-02-16 | Gilead Sciences, Inc. | 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| WO2009013335A1 (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 |
| WO2011095196A1 (en) * | 2010-02-05 | 2011-08-11 | Merck Patent Gmbh | Hetaryl-[1,8]naphthyridine derivatives |
| KR20140022829A (ko) * | 2011-03-09 | 2014-02-25 | 메르크 파텐트 게엠베하 | 피리도 [2, 3 - b] 피라진 유도체 및 그 치료적 용도 |
| AU2012281281B2 (en) * | 2011-07-13 | 2017-06-01 | Tiumbio Co., Ltd | 2-pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors |
| MX2015004151A (es) * | 2012-10-05 | 2015-07-06 | Rigel Pharmaceuticals Inc | Inhibidores del factor de diferenciacion de crecimiento-8 (gdf-8). |
| EP3129367B1 (en) * | 2014-04-08 | 2019-09-04 | Rigel Pharmaceuticals, Inc. | 2,3-disubstituted pyridine compounds as tgf-beta inhibitors |
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- 2015-04-02 US US15/128,051 patent/US10233170B2/en active Active
- 2015-04-02 ES ES15716690T patent/ES2759240T3/es active Active
- 2015-04-02 CN CN201580030111.XA patent/CN106536507B/zh not_active Expired - Fee Related
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- 2015-04-08 UY UY0001036068A patent/UY36068A/es unknown
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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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|---|---|
| CN106536507A (zh) | 2017-03-22 |
| TW201623279A (zh) | 2016-07-01 |
| US20190284155A1 (en) | 2019-09-19 |
| WO2015157093A1 (en) | 2015-10-15 |
| JP2019196387A (ja) | 2019-11-14 |
| EP3129367A1 (en) | 2017-02-15 |
| JP2017515802A (ja) | 2017-06-15 |
| UY36068A (es) | 2015-10-30 |
| EP3129367B1 (en) | 2019-09-04 |
| US10233170B2 (en) | 2019-03-19 |
| US10858335B2 (en) | 2020-12-08 |
| CN106536507B (zh) | 2020-04-07 |
| ES2759240T3 (es) | 2020-05-08 |
| US20170096409A1 (en) | 2017-04-06 |
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