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
- 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
- A61K39/39541—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against normal tissues, cells
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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
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- 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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- 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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- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- 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)
- Microbiology (AREA)
- Mycology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Oncology (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 |
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 (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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| WO2016133838A1 (en) | 2015-02-20 | 2016-08-25 | Rigel Pharmaceuticals, Inc. | Gdf-8 inhibitors |
| BR112018003588A2 (pt) | 2015-08-26 | 2018-09-25 | Blueprint Medicines Corp | compostos e composições úteis para tratamento de distúrbios relacionados ao ntrk |
| SG11201803920TA (en) | 2015-11-19 | 2018-06-28 | Blueprint Medicines Corp | Compounds and compositions useful for treating disorders related to ntrk |
| ES3011058T3 (en) * | 2015-11-25 | 2025-04-07 | Convergene Llc | Bicyclic bet bromodomain inhibitors and uses thereof |
| MX387283B (es) | 2016-03-24 | 2025-03-18 | Cothera Biosciences Inc | Tratamiento del cancer con tg02. |
| 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 |
| 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 |
| 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 |
| BR112019014527A2 (pt) * | 2017-01-23 | 2020-02-27 | Revolution Medicines, Inc. | Compostos de piridina como inibidores de shp2 alostéricos |
| 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 |
| WO2019136320A1 (en) | 2018-01-05 | 2019-07-11 | Icahn School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
| ES3038913T3 (en) | 2018-03-20 | 2025-10-15 | Icahn School Med Mount Sinai | Beta-carboline derivatives as dyrk1a inhibitors for the treatment of e.g. diabetes |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
| US12102626B2 (en) | 2018-12-27 | 2024-10-01 | Nexys Therapeutics, Inc. | (Pyridin-2-yl)amine derivatives as TGF-BETA R1 (ALK5) inhibitors for the treatment of cancer |
| EP3904348A4 (en) * | 2018-12-28 | 2022-10-19 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Aminopyridine compound, preparation method therefor and use thereof |
| BR112021018864A2 (pt) | 2019-03-29 | 2021-11-30 | Sumitomo Chemical Co | Composto heterocíclico e composição de controle de praga artrópode nociva contendo o mesmo |
| WO2020223255A1 (en) | 2019-04-29 | 2020-11-05 | Solent Therapeutics, Llc | 3-amino-4h-benzo[e][1,2,4]thiadiazine 1,1-dioxide derivatives as inhibitors of mrgx2 |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| WO2021254464A1 (zh) * | 2020-06-19 | 2021-12-23 | 南京红云生物科技有限公司 | 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 |
| EP4223756A4 (en) | 2020-09-30 | 2025-05-21 | Sumitomo Chemical Company, Limited | HETEROCYCLIC COMPOUND AND COMPOSITION FOR CONTROLLING HARMFUL ARTHROPODS CONTAINING SAME |
| 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 |
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| 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 |
| MX2024007062A (es) * | 2021-12-10 | 2024-07-19 | Prothena Biosciences Ltd | Compuestos heterociclicos como inhibidores de dyrk1a. |
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| JPWO2024096093A1 (OSRAM) | 2022-11-04 | 2024-05-10 |
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| 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 |
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| WO2009032653A1 (en) * | 2007-08-31 | 2009-03-12 | Smith Kline Beecham Corporation | Inhibitors of akt activity |
| EA201201081A1 (ru) * | 2010-02-05 | 2013-03-29 | Мерк Патент Гмбх | Производные гетарил[1,8]нафтиридина |
| US9051318B2 (en) * | 2011-03-09 | 2015-06-09 | Merck Patent Gmbh | Pyrido [2, 3-B] pyrazine compounds and their therapeutical uses such as for inhibiting ATP consuming proteins and treating diseases associated therewith |
| KR101938368B1 (ko) * | 2011-07-13 | 2019-01-14 | 주식회사 티움바이오 | Alk5 및/또는 alk4 억제제로서의 2-피리딜-치환된 이미다졸 |
| KR20150072412A (ko) * | 2012-10-05 | 2015-06-29 | 리겔 파마슈티칼스, 인크. | Gdf-8 억제제 |
| WO2015157093A1 (en) * | 2014-04-08 | 2015-10-15 | Rigel Pharmaceuticals, Inc. | 2,3-disubstituted pyridine compounds as tgf-beta inhibitors and methods of use |
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2015
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- 2015-04-02 EP EP15716690.1A patent/EP3129367B1/en active Active
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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 |
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| US10233170B2 (en) | 2019-03-19 |
| JP2017515802A (ja) | 2017-06-15 |
| US20190284155A1 (en) | 2019-09-19 |
| TW201623279A (zh) | 2016-07-01 |
| US20170096409A1 (en) | 2017-04-06 |
| EP3129367B1 (en) | 2019-09-04 |
| WO2015157093A1 (en) | 2015-10-15 |
| EP3129367A1 (en) | 2017-02-15 |
| CN106536507B (zh) | 2020-04-07 |
| US10858335B2 (en) | 2020-12-08 |
| CN106536507A (zh) | 2017-03-22 |
| ES2759240T3 (es) | 2020-05-08 |
| UY36068A (es) | 2015-10-30 |
| JP2019196387A (ja) | 2019-11-14 |
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