AR105820A1 - Análogos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5 - Google Patents
Análogos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5Info
- Publication number
- AR105820A1 AR105820A1 ARP160102600A ARP160102600A AR105820A1 AR 105820 A1 AR105820 A1 AR 105820A1 AR P160102600 A ARP160102600 A AR P160102600A AR P160102600 A ARP160102600 A AR P160102600A AR 105820 A1 AR105820 A1 AR 105820A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- cycloalkyl
- halo
- aromatic ring
- Prior art date
Links
- VZQXUWKZDSEQRR-UHFFFAOYSA-N Nucleosid Natural products C12=NC(SC)=NC(NCC=C(C)C)=C2N=CN1C1OC(CO)C(O)C1O VZQXUWKZDSEQRR-UHFFFAOYSA-N 0.000 title 1
- 102100034607 Protein arginine N-methyltransferase 5 Human genes 0.000 title 1
- 101710084427 Protein arginine N-methyltransferase 5 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 29
- 229910052739 hydrogen Inorganic materials 0.000 abstract 12
- 239000001257 hydrogen Substances 0.000 abstract 12
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 7
- 125000001424 substituent group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 229910052757 nitrogen Inorganic materials 0.000 abstract 6
- 150000002431 hydrogen Chemical group 0.000 abstract 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 125000002619 bicyclic group Chemical group 0.000 abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000001963 4 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/14—Pyrrolo-pyrimidine radicals
-
- 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
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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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- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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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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- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/23—Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562209941P | 2015-08-26 | 2015-08-26 | |
| EP15184011 | 2015-09-07 | ||
| US201662306233P | 2016-03-10 | 2016-03-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR105820A1 true AR105820A1 (es) | 2017-11-15 |
Family
ID=54065259
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160102600A AR105820A1 (es) | 2015-08-26 | 2016-08-25 | Análogos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5 |
Country Status (35)
Families Citing this family (75)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI870767B (zh) | 2015-08-26 | 2025-01-21 | 比利時商健生藥品公司 | 使用作為prmt5抑制劑之新穎經6-6雙環芳香環取代之核苷類似物 |
| MA43671A (fr) * | 2016-03-10 | 2018-11-28 | Janssen Pharmaceutica Nv | Analogues de nucléosides substitués destinés à être utilisés en tant qu'inhibiteurs de prmt5 |
| CA2969295A1 (en) * | 2016-06-06 | 2017-12-06 | Pfizer Inc. | Substituted carbonucleoside derivatives, and use thereof as a prmt5 inhibitor |
| ES2966316T3 (es) | 2016-09-14 | 2024-04-19 | Janssen Pharmaceutica Nv | Inhibidores bicíclicos fusionados de interacción de MENIN-MLL |
| BR112019004691A2 (pt) | 2016-09-14 | 2019-06-25 | Janssen Pharmaceutica Nv | inibidores bicíclicos em espiro da interação menina-mll |
| US12084462B2 (en) | 2016-09-14 | 2024-09-10 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| MX2019003843A (es) * | 2016-10-03 | 2019-06-24 | Janssen Pharmaceutica Nv | Análogos novedosos de carbanucleósidos sustituidos de sistema anular monocíclico y bicíclico para su uso como inhibidores de prmt5. |
| WO2018065365A1 (en) | 2016-10-03 | 2018-04-12 | Janssen Pharmaceutica Nv | Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors |
| KR102513564B1 (ko) | 2016-12-15 | 2023-03-22 | 얀센 파마슈티카 엔.브이. | 메닌-mll 상호작용의 아제판 억제제 |
| GB201700526D0 (en) * | 2017-01-12 | 2017-03-01 | Univ Of Hull | Therapeutic use |
| CA3049739A1 (en) | 2017-02-27 | 2018-08-30 | Janssen Pharmaceutica Nv | Use of biomarkers in identifying cancer patients that will be responsive to treatment with a prmt5 inhibitor |
| CA3072439A1 (en) | 2017-08-09 | 2019-02-14 | Prelude Therapeutics, Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (prmt5) |
| US11524962B2 (en) | 2017-10-26 | 2022-12-13 | Prelude Therapeutics, Incorporated | Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein arginine methyl transferase 5 (PRMT5) |
| KR20200096265A (ko) * | 2017-12-05 | 2020-08-11 | 앤젝스 파마수티컬, 인크. | Prmt5 억제제로서의 헤테로시클릭 화합물 |
| BR112020010815A2 (pt) * | 2017-12-08 | 2020-11-10 | Janssen Pharmaceutica Nv | análogos espirobicíclicos |
| US11459330B2 (en) | 2017-12-13 | 2022-10-04 | Lupin Limited | Substituted bicyclic heterocyclic compounds as PRMT5 inhibitors |
| US11396517B1 (en) | 2017-12-20 | 2022-07-26 | Janssen Pharmaceutica Nv | Exo-aza spiro inhibitors of menin-MLL interaction |
| US10711007B2 (en) | 2018-03-14 | 2020-07-14 | Prelude Therapeutics Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (PRMT5) |
| DK3765461T3 (da) * | 2018-03-14 | 2023-11-20 | Prelude Therapeutics Inc | Selektive protein argininmethyltransferase 5 (prmt5)-hæmmere |
| CA3108388A1 (en) * | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| EP3833668B1 (en) | 2018-08-07 | 2025-03-19 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| EP3833667B1 (en) | 2018-08-07 | 2024-03-13 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2020033285A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2020132603A2 (en) * | 2018-12-21 | 2020-06-25 | Memorial Sloan-Kettering Cancer Center | Salicyl-adenosinemonosulfamate analogs and uses thereof |
| CN109400545B (zh) * | 2018-12-24 | 2022-03-25 | 济南大学 | 一种精氨酸甲基转移酶5抑制剂及其应用 |
| CN109369507A (zh) * | 2018-12-26 | 2019-02-22 | 重庆市碚圣医药科技股份有限公司 | 一种n-(2,2-二乙氧基乙基)邻苯二甲酰亚胺的提纯方法 |
| JP2022521491A (ja) * | 2019-02-13 | 2022-04-08 | プレリュード・セラピューティクス・インコーポレイテッド | タンパク質アルギニンメチルトランスフェラーゼ５（ｐｒｍｔ５）の選択的阻害剤 |
| US20220160747A1 (en) * | 2019-03-20 | 2022-05-26 | Korea Research Institute Of Chemical Technology | Pharmaceutical composition comprising novel azolopyrimidine heterocyclic compound as active ingredient |
| JP7609798B2 (ja) * | 2019-03-25 | 2025-01-07 | カリフォルニア インスティチュート オブ テクノロジー | Ｐｒｍｔ５インヒビター及びその使用 |
| CN114072407A (zh) | 2019-04-02 | 2022-02-18 | 阿里戈斯治疗公司 | 靶向prmt5的化合物 |
| WO2020206289A1 (en) * | 2019-04-05 | 2020-10-08 | Prelude Therapeutics, Incorporated | Selective inhibitors of protein arginine methyltransferase 5 |
| JP2022526604A (ja) * | 2019-04-05 | 2022-05-25 | プレリュード・セラピューティクス・インコーポレイテッド | タンパク質アルギニンメチルトランスフェラーゼ５の選択的阻害剤 |
| JP2022534998A (ja) * | 2019-05-30 | 2022-08-04 | エンジェクス ファーマシューティカル インコーポレイテッド | Ｐｒｍｔ５阻害剤としての複素環式化合物 |
| TW202112375A (zh) | 2019-06-06 | 2021-04-01 | 比利時商健生藥品公司 | 使用ｐｒｍｔ５抑制劑治療癌症之方法 |
| PT3980417T (pt) * | 2019-06-10 | 2023-12-28 | Lupin Ltd | Inibidores de prmt5 |
| BR112021024457A2 (pt) * | 2019-06-12 | 2022-01-18 | Janssen Pharmaceutica Nv | Intermediários espirobicíclicos |
| CA3154566A1 (en) | 2019-09-18 | 2021-03-25 | Prelude Therapeutics Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (prmt5) |
| WO2021079196A2 (en) * | 2019-10-21 | 2021-04-29 | Accent Therapeutics, Inc | Mettl3 modulators |
| CA3156135A1 (en) * | 2019-10-22 | 2021-04-29 | Lupin Limited | PHARMACEUTICAL COMBINATION OF PRMT5 INHIBITORS |
| GB201915447D0 (en) * | 2019-10-24 | 2019-12-11 | Johnson Matthey Plc | Polymorphs of avapritinib and methods of preparing the polymorphs |
| CN115135651A (zh) * | 2019-12-03 | 2022-09-30 | 鲁皮恩有限公司 | 作为prmt5抑制剂的被取代的核苷类似物 |
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