AR112794A1 - Compuestos heteroaromáticos sustituidos con cicloolefinas y su uso en el tratamiento de enfermedades inducidas por mutaciones idh - Google Patents
Compuestos heteroaromáticos sustituidos con cicloolefinas y su uso en el tratamiento de enfermedades inducidas por mutaciones idhInfo
- Publication number
- AR112794A1 AR112794A1 ARP180102548A ARP180102548A AR112794A1 AR 112794 A1 AR112794 A1 AR 112794A1 AR P180102548 A ARP180102548 A AR P180102548A AR P180102548 A ARP180102548 A AR P180102548A AR 112794 A1 AR112794 A1 AR 112794A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- membered
- cycloalkyl
- halo
- optionally substituted
- Prior art date
Links
- 150000001925 cycloalkenes Chemical group 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 150000002390 heteroarenes Chemical group 0.000 title 1
- 230000035772 mutation Effects 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 125000005843 halogen group Chemical group 0.000 abstract 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 5
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 abstract 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 4
- 229910052805 deuterium Inorganic materials 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- -1 C1−6 Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
- C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
- C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
- C07D251/40—Nitrogen atoms
- C07D251/48—Two nitrogen atoms
-
- 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
- A61K31/53—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
- C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
- C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
- C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
- C07D251/18—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
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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
- C07D401/12—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 chain containing hetero atoms as chain links
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- C07D403/12—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 chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D405/02—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 containing two hetero rings
- C07D405/12—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 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- C07D417/12—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 chain containing hetero atoms as chain links
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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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
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- 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
- C07B2200/05—Isotopically modified compounds, e.g. labelled
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- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
La presente se refiere a un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, y/o solvatos, mezclas racémicas, enantiómeros, diastereómeros y tautómeros del mismo. Reivindicación 1: Un compuesto de fórmula (1), y/o una sal farmacéuticamente aceptable del mismo, y/o solvatos, mezclas racémicas, enantiómeros, diastereómeros y tautómeros del mismo, en donde A está elegido a partir de los compuestos del grupo de fórmulas (2), en donde, R⁷ está elegido a partir de H, halo, -CN, -OH, o -NH₂; R⁸ está elegido a partir de halo, -CN, -OH, o -NH₂; q es 1 ó 2; R¹ está elegido a partir de H, -OH, halo, C₁₋₆ alquilo, C₁₋₆ alcoxilo, -NH₂, -NH(C₁₋₄ alquilo), -N(C₁₋₄ alquilo)₂, oxo, o C₃₋₈ cicloalquilo; cada uno de R² está independientemente elegido a partir de H, deuterio, halo, -OH, -NH₂, -CN, -SH, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ haloalquilo, C₃₋₈ cicloalquilo, oxo, -OR⁵, -OCOR⁵, -NHR⁵, -N(R⁵)(C₁₋₄ alquilo), -COR⁵, -NHCOR⁵, o heterociclilo de 3 - 8 miembros; en el cual cada uno de dicho C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₃₋₈ cicloalquilo o heterociclilo de 3 - 8 miembros está opcionalmente sustituido con uno o más grupos elegidos a partir de deuterio, halo, -CN, -OH, -SH, -NH₂, -NH(C₁₋₄ alquilo), -N(C₁₋₄ alquilo)₂, o C₁₋₆ alcoxilo; o dos R², que se unen al mismo átomo de carbono, junto con el átomo de carbono al que están unidos forman un cicloalquilo de 3 - 5 miembros el cual está opcionalmente sustituido con uno o más halo o deuterio; R³, R³, R⁴ y R⁴ están independientemente elegidos a partir de H, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₃₋₁₂ cicloalquilo, heterociclilo de 3 - 12 miembros, fenilo, heteroarilo de 5 - 12 miembros, -C(O)R⁵, -OR⁵, o -NHR⁵, en el cual cada uno de dichos C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₃₋₁₂ cicloalquilo, heterociclilo de 3 - 12 miembros, fenilo, o heteroarilo de 5 - 12 miembros está opcionalmente sustituido con uno o más R⁶; en donde R³, R³, R⁴ y R⁴ no son H simultáneamente; con la condición de que cuando uno de R³ y R⁴ es fenilo opcionalmente sustituido o heteroarilo opcionalmente sustituido de 5 - 6 miembros, el otro es -OR⁵ o -NHR⁵; o R³ y R³ están independientemente elegidos a partir de H, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₃₋₁₂ cicloalquilo, heterociclilo de 3 - 12 miembros, fenilo, heteroarilo de 5 - 12 miembros, -C(O)R⁵, -OR⁵, o -NHR⁵, en el cual cada uno de dichos C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₃₋₁₂ cicloalquilo, heterociclilo de 3 - 12 miembros, fenilo, o heteroarilo de 5 - 12 miembros está opcionalmente sustituido con uno o más R⁶; R⁴ y R⁴ junto con el átomo de N al cual están unidos forman un anillo heterocíclico de 3 - 8 miembros opcionalmente sustituido por uno o más R⁶; R⁵ está elegido a partir de C₁₋₆ alquilo o C₃₋₈ cicloalquilo, cada uno de los cuales está opcionalmente sustituido con uno o más grupos independientemente elegidos a partir de halo, -CN, -OH, -SH, -NH₂, o C₁₋₆ alcoxilo; cada uno de R⁶ está independientemente elegido a partir de deuterio, halo, -CN, -OH, -SH, -NH₂, C₁₋₆ alcoxilo, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₃₋₈ cicloalquilo, heterociclilo de 3 - 8 miembros, fenilo, o heteroarilo de 5 - 6 miembros, en el cual cada uno de dichos C₁₋₆ alcoxilo, C₁₋₆, alquilo, C₃₋₈ cicloalquilo, heterociclilo de 3 - 8 miembros, fenilo, o heteroarilo de 5 - 6 miembros está opcionalmente sustituido con uno o más grupos independientemente elegidos a partir de halo, -CN, -OH, -SH, -NH₂, C₁₋₆ alcoxilo, C₁₋₆ alquinilo, o C₁₋₆ alquilo; m es 0, 1, 2, 3, 4, 5 ó 6; n es 0, 1 ó 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710801364.3A CN109467538A (zh) | 2017-09-07 | 2017-09-07 | 环烯烃取代的杂芳环类化合物及其用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR112794A1 true AR112794A1 (es) | 2019-12-11 |
Family
ID=65634832
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180102548A AR112794A1 (es) | 2017-09-07 | 2018-09-07 | Compuestos heteroaromáticos sustituidos con cicloolefinas y su uso en el tratamiento de enfermedades inducidas por mutaciones idh |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US11414390B2 (es) |
| EP (1) | EP3679020A4 (es) |
| JP (2) | JP7273030B6 (es) |
| KR (1) | KR102566237B1 (es) |
| CN (6) | CN109467538A (es) |
| AR (1) | AR112794A1 (es) |
| AU (1) | AU2018329047B2 (es) |
| CA (1) | CA3073782A1 (es) |
| CL (1) | CL2020000553A1 (es) |
| EA (1) | EA202090653A1 (es) |
| IL (1) | IL272923B2 (es) |
| MX (1) | MX2020002505A (es) |
| PE (1) | PE20200727A1 (es) |
| PH (1) | PH12020500408A1 (es) |
| SG (1) | SG11202001642WA (es) |
| TW (1) | TWI816693B (es) |
| UA (1) | UA129118C2 (es) |
| WO (1) | WO2019047909A1 (es) |
| ZA (1) | ZA202001448B (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112020003494A2 (pt) | 2017-09-07 | 2020-08-25 | Augusta University Research Institute, Inc | composto, métodos para aumentar uma resposta imunossupressora, para tratar um distúrbio inflamatório, uma doença autoimune, doença do enxerto contra hospedeiro, infecção crônica e obesidade e para inibir ou reduzir a rejeição a um transplante, e, composição farmacêutica |
| CN109467538A (zh) * | 2017-09-07 | 2019-03-15 | 和记黄埔医药（上海）有限公司 | 环烯烃取代的杂芳环类化合物及其用途 |
| WO2022095756A1 (zh) * | 2020-11-09 | 2022-05-12 | 贝达药业股份有限公司 | 突变型idh1和idh2抑制剂及其应用 |
| CN118355008A (zh) * | 2022-01-11 | 2024-07-16 | 正大天晴药业集团股份有限公司 | 一种1,3,5-三嗪衍生物的制备方法 |
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| TWI259081B (en) * | 2001-10-26 | 2006-08-01 | Sugen Inc | Treatment of acute myeloid leukemia with indolinone compounds |
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