KR20220027871A - NF-kB 유도 키나아제의 소분자 억제제 - Google Patents
NF-kB 유도 키나아제의 소분자 억제제 Download PDFInfo
- Publication number
- KR20220027871A KR20220027871A KR1020217042635A KR20217042635A KR20220027871A KR 20220027871 A KR20220027871 A KR 20220027871A KR 1020217042635 A KR1020217042635 A KR 1020217042635A KR 20217042635 A KR20217042635 A KR 20217042635A KR 20220027871 A KR20220027871 A KR 20220027871A
- Authority
- KR
- South Korea
- Prior art keywords
- phenyl
- ethynyl
- pyrimidin
- hydroxy
- amino
- 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.)
- Pending
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- 0 CC(C)c1nc2c(*)nc(*)c([Rh])c2c(*)n1 Chemical compound CC(C)c1nc2c(*)nc(*)c([Rh])c2c(*)n1 0.000 description 64
- APKXTIJQLBCFKE-UHFFFAOYSA-N CC(C)c(cc1)cc2c1cnnc2N Chemical compound CC(C)c(cc1)cc2c1cnnc2N APKXTIJQLBCFKE-UHFFFAOYSA-N 0.000 description 2
- LGYFYVBTVMWCGJ-UHFFFAOYSA-N CC(C)c(cc12)cnc1ncnc2N Chemical compound CC(C)c(cc12)cnc1ncnc2N LGYFYVBTVMWCGJ-UHFFFAOYSA-N 0.000 description 2
- XFVDPTOYIQBMBX-UHFFFAOYSA-N C[n](cc12)nc1ncnc2N Chemical compound C[n](cc12)nc1ncnc2N XFVDPTOYIQBMBX-UHFFFAOYSA-N 0.000 description 2
- XYFVIZUWUPOWCH-UHFFFAOYSA-N CC(C)(C)C(CCC1(C)C)(C1=O)O Chemical compound CC(C)(C)C(CCC1(C)C)(C1=O)O XYFVIZUWUPOWCH-UHFFFAOYSA-N 0.000 description 1
- DABWGTJDDCXCBJ-SNVBAGLBSA-N CC(C)(C)[C@](CCN1C)(C(F)F)C1=O Chemical compound CC(C)(C)[C@](CCN1C)(C(F)F)C1=O DABWGTJDDCXCBJ-SNVBAGLBSA-N 0.000 description 1
- ILVCWGPHMHYZAZ-UHFFFAOYSA-N CC(C)(c1nnc(C)[o]1)O Chemical compound CC(C)(c1nnc(C)[o]1)O ILVCWGPHMHYZAZ-UHFFFAOYSA-N 0.000 description 1
- PVORTHBYWDTPOE-SECBINFHSA-N CC(C)[C@](C)(c1n[o]c(C)c1)O Chemical compound CC(C)[C@](C)(c1n[o]c(C)c1)O PVORTHBYWDTPOE-SECBINFHSA-N 0.000 description 1
- QNOAAQBRQAXVKM-UHFFFAOYSA-N CC(C)c1nc2ncnc(N)c2[s]1 Chemical compound CC(C)c1nc2ncnc(N)c2[s]1 QNOAAQBRQAXVKM-UHFFFAOYSA-N 0.000 description 1
- FILVIKOEJGORQS-UHFFFAOYSA-N CC(CC1)N(C)C1=O Chemical compound CC(CC1)N(C)C1=O FILVIKOEJGORQS-UHFFFAOYSA-N 0.000 description 1
- VQVREJAGUJGFCA-UHFFFAOYSA-N CC(CN(C)C1=O)C1O Chemical compound CC(CN(C)C1=O)C1O VQVREJAGUJGFCA-UHFFFAOYSA-N 0.000 description 1
- JOQNJBUUMSOBDS-UHFFFAOYSA-N CC(N1)=Nc(c(N)ncc2)c2C1=O Chemical compound CC(N1)=Nc(c(N)ncc2)c2C1=O JOQNJBUUMSOBDS-UHFFFAOYSA-N 0.000 description 1
- WPAPDOIRWDGLKY-UHFFFAOYSA-N CC1(c2ncc[n]2CC1)O Chemical compound CC1(c2ncc[n]2CC1)O WPAPDOIRWDGLKY-UHFFFAOYSA-N 0.000 description 1
- IHMZSFSUNLZWNX-JTQLQIEISA-N CCC(C)(C)[C@](C)(c1nnc(C)[o]1)O Chemical compound CCC(C)(C)[C@](C)(c1nnc(C)[o]1)O IHMZSFSUNLZWNX-JTQLQIEISA-N 0.000 description 1
- RERNMUGTYCXNIZ-UHFFFAOYSA-N CCC1=CN(C=C(C(C)C)NC2=O)C2=CC1 Chemical compound CCC1=CN(C=C(C(C)C)NC2=O)C2=CC1 RERNMUGTYCXNIZ-UHFFFAOYSA-N 0.000 description 1
- LCKBSQVRPUVPQD-SSDOTTSWSA-N CC[C@](C)(c1c[s]cn1)O Chemical compound CC[C@](C)(c1c[s]cn1)O LCKBSQVRPUVPQD-SSDOTTSWSA-N 0.000 description 1
Classifications
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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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
- 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
- C07D401/10—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 linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- C07D417/10—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 linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962855144P | 2019-05-31 | 2019-05-31 | |
| US62/855,144 | 2019-05-31 | ||
| US201962907833P | 2019-09-30 | 2019-09-30 | |
| US62/907,833 | 2019-09-30 | ||
| PCT/EP2020/065024 WO2020239999A1 (en) | 2019-05-31 | 2020-05-29 | SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20220027871A true KR20220027871A (ko) | 2022-03-08 |
Family
ID=71108552
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020217042635A Pending KR20220027871A (ko) | 2019-05-31 | 2020-05-29 | NF-kB 유도 키나아제의 소분자 억제제 |
Country Status (37)
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114222737B (zh) * | 2019-05-31 | 2024-07-26 | 詹森药业有限公司 | NF-κB诱导激酶的小分子抑制剂 |
| WO2020243423A1 (en) | 2019-05-31 | 2020-12-03 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| KR20220030222A (ko) | 2019-05-31 | 2022-03-10 | 이케나 온콜로지, 인코포레이티드 | Tead 억제제 및 이의 용도 |
| IL316886A (en) * | 2022-05-11 | 2025-01-01 | Janssen Pharmaceutica Nv | History of pyrrolidinones as NF kappa B kinase inhibitors |
| CA3257152A1 (en) * | 2022-05-11 | 2023-11-16 | Janssen Pharmaceutica Nv | Pyrrolidine derivatives useful as NF-κB induction kinase inhibitors |
| EP4637773A1 (en) | 2022-12-22 | 2025-10-29 | Boehringer Ingelheim International GmbH | Crystalline forms of a her2 inhibitor |
| WO2025020886A1 (zh) * | 2023-07-27 | 2025-01-30 | 浙江星浩澎博医药有限公司 | 氮杂喹唑啉环衍生物及其用途 |
| IL326016A (en) | 2023-07-28 | 2026-03-01 | Boehringer Ingelheim Int | Process for manufacturing a HER2 inhibitor |
| WO2025235874A1 (en) * | 2024-05-10 | 2025-11-13 | Schrödinger, Inc. | Heterocyclics as egfr inhibitors |
| JP2026022634A (ja) * | 2024-07-30 | 2026-02-12 | 日本たばこ産業株式会社 | ピラゾロピリミジン化合物及びその医薬用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| GB9930616D0 (en) | 1999-12-24 | 2000-02-16 | Mathilda & Terence Kennedy Ins | Activation and inhibition of the immune system |
| US7132428B2 (en) | 2003-07-03 | 2006-11-07 | Aventis Pharmaceuticals Inc. | Pyrazoloisoquinoline derivative as kinase inhibitors for the treatment of various disorders |
| JP2008509138A (ja) * | 2004-08-03 | 2008-03-27 | ワイス | 心臓血管疾患の治療に有用なインダゾール類 |
| WO2006053277A2 (en) | 2004-11-12 | 2006-05-18 | Chippac, Inc. | Wire bond interconnection |
| AU2009263037B2 (en) * | 2008-06-26 | 2011-10-06 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| WO2010042337A1 (en) | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
| MX2013010513A (es) * | 2011-03-16 | 2013-10-07 | Hoffmann La Roche | Compuestos de alcohol 6,5-heterociclil-propargilico y usos de los mismos. |
| JP2015507001A (ja) | 2012-02-17 | 2015-03-05 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 三環式化合物及びその使用方法 |
| US8859553B2 (en) * | 2012-07-30 | 2014-10-14 | Astar Biotech Llc | Protein kinase inhibitors |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| US20150057260A1 (en) * | 2013-08-22 | 2015-02-26 | Genentech, Inc. | Alkynyl alcohols and methods of use |
| US20160096850A9 (en) * | 2013-08-22 | 2016-04-07 | Genentech, Inc. | Alkynyl alcohols and methods of use |
| TWI704146B (zh) | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物 |
| TWI627173B (zh) | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物 |
| AU2015334917B2 (en) | 2014-10-23 | 2019-08-29 | Janssen Pharmaceutica Nv | New compounds as NIK inhibitors |
| BR112017008039B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V. | Derivados de pirazol como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende |
| JP6616412B2 (ja) | 2014-10-23 | 2019-12-04 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｎｉｋ阻害剤としての新規のピラゾロピリミジン誘導体 |
| MX371151B (es) | 2014-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK). |
| JP2018510140A (ja) | 2015-02-25 | 2018-04-12 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | アルキニルアルコール及び使用方法 |
| ES2775449T3 (es) | 2016-01-22 | 2020-07-27 | Janssen Pharmaceutica Nv | Nuevos derivados de cianoindolina sustituida como inhibidores de nik |
| EP3405464B1 (en) | 2016-01-22 | 2019-12-04 | Janssen Pharmaceutica NV | New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
| WO2018002217A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
| WO2018037058A1 (en) * | 2016-08-24 | 2018-03-01 | F. Hoffmann-La Roche Ag | 2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use |
| WO2018037059A1 (en) | 2016-08-24 | 2018-03-01 | F. Hoffmann-La Roche Ag | 2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use |
| CN110831940B (zh) | 2017-07-06 | 2023-06-20 | 詹森药业有限公司 | 作为nik抑制剂的新取代的氮杂吲哚啉衍生物 |
| CN109810110B (zh) * | 2017-11-22 | 2023-01-24 | 中国科学院上海药物研究所 | 一种具有2-氨基嘧啶结构的化合物，其制备方法和用途 |
| CN114222737B (zh) * | 2019-05-31 | 2024-07-26 | 詹森药业有限公司 | NF-κB诱导激酶的小分子抑制剂 |
| WO2020243423A1 (en) | 2019-05-31 | 2020-12-03 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| CR20240234A (es) | 2019-05-31 | 2024-07-09 | Sage Therapeutics Inc | ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629) |
| KR20220030222A (ko) | 2019-05-31 | 2022-03-10 | 이케나 온콜로지, 인코포레이티드 | Tead 억제제 및 이의 용도 |
| BR112021022099A2 (pt) | 2019-05-31 | 2021-12-28 | Chiesi Farm Spa | Derivados de amino quinazolina como inibidores de p2x3 |
| WO2021067217A1 (en) | 2019-09-30 | 2021-04-08 | Incyte Corporation | Pyrido[3,2-d]pyrimidine compounds as immunomodulators |
-
2020
- 2020-05-29 CN CN202080057418.XA patent/CN114222737B/zh active Active
- 2020-05-29 PT PT207336884T patent/PT3976597T/pt unknown
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