PE20230162A1 - Derivados espirancos sustituidos de cadena lineal - Google Patents
Derivados espirancos sustituidos de cadena linealInfo
- Publication number
- PE20230162A1 PE20230162A1 PE2022001149A PE2022001149A PE20230162A1 PE 20230162 A1 PE20230162 A1 PE 20230162A1 PE 2022001149 A PE2022001149 A PE 2022001149A PE 2022001149 A PE2022001149 A PE 2022001149A PE 20230162 A1 PE20230162 A1 PE 20230162A1
- Authority
- PE
- Peru
- Prior art keywords
- spiranch
- isopropyl
- protein
- compounds
- linear chain
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 3
- 201000003793 Myelodysplastic syndrome Diseases 0.000 abstract 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 abstract 2
- 102000004169 proteins and genes Human genes 0.000 abstract 2
- 108090000623 proteins and genes Proteins 0.000 abstract 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 abstract 1
- 101710169972 Menin Proteins 0.000 abstract 1
- 102100030550 Menin Human genes 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000003993 interaction Effects 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 208000032839 leukemia Diseases 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
Classifications
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- 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
- C07D487/10—Spiro-condensed systems
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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
- A61K31/53—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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
-
- 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
-
- 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)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invencion se refiere a compuestos de Formula (I), los tautomeros o formas estereoisomericas de estos; en donde R1a representa -C(=O)-NRxaRxb, Het, entre otros; Het representa un anillo aromatico monociclico de 5 a 6 miembros, entre otros; R1b representa F o Cl; Y1 representa -CR5aR5b-, -O- o -NR5c-; R2 se selecciona de -O-alquilo C1-4 y -NR7aR7b; U es N o CH; n1, n2, n3 y n4 son 1 y 2; X1 es CH; X2 es N y R4 es isopropilo. Un compuesto seleccionado es (R)-(4-(6-(6-(2-(etil(isopropil)carbamoil)-4-fluorofenoxi)-1,2,4-triazin-5-il)-2,6-diazaespiro[3.4]octan-2-il)-5-metilhexil)carbamato de tert-butilo. Asimismo, refiere a una composicion farmaceutica que los comprende. Dichos compuestos son inhibidores de la interaccion proteina/proteina de la menina/MLL, siendo utiles para el tratamiento de cancer, que incluye leucemia, sindrome mielodisplasico (SMD) y neoplasias mieloproliferativas (NMP); y diabetes.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019126760 | 2019-12-19 | ||
| US202062961775P | 2020-01-16 | 2020-01-16 | |
| CN2020126595 | 2020-11-04 | ||
| PCT/CN2020/137266 WO2021121327A1 (en) | 2019-12-19 | 2020-12-17 | Substituted straight chain spiro derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20230162A1 true PE20230162A1 (es) | 2023-02-01 |
Family
ID=76476870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022001149A PE20230162A1 (es) | 2019-12-19 | 2020-12-17 | Derivados espirancos sustituidos de cadena lineal |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US12473295B2 (es) |
| EP (1) | EP4077312A4 (es) |
| JP (2) | JP7554829B2 (es) |
| KR (1) | KR20220118500A (es) |
| CN (4) | CN118255774A (es) |
| AU (1) | AU2020404305A1 (es) |
| CA (1) | CA3161045A1 (es) |
| CL (3) | CL2022001583A1 (es) |
| CO (1) | CO2022009085A2 (es) |
| CR (1) | CR20220346A (es) |
| DO (1) | DOP2022000125A (es) |
| EC (1) | ECSP22054700A (es) |
| IL (1) | IL293965A (es) |
| JO (1) | JOP20220154A1 (es) |
| MX (1) | MX2022007652A (es) |
| PE (1) | PE20230162A1 (es) |
| PH (1) | PH12022551502A1 (es) |
| TW (2) | TWI878414B (es) |
| UA (1) | UA129208C2 (es) |
| UY (1) | UY38988A (es) |
| WO (1) | WO2021121327A1 (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL312367A (en) | 2017-01-31 | 2024-06-01 | Arvinas Operations Inc | Cereblon ligands and bifunctional compounds comprising the same |
| CA3165168A1 (en) | 2019-12-19 | 2021-06-24 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| JOP20220154A1 (ar) | 2019-12-19 | 2023-01-30 | Janssen Pharmaceutica Nv | مشتقات سبيرو بسلسلة مستقيمة بها استبدال |
| CN117321049A (zh) | 2021-05-08 | 2023-12-29 | 詹森药业有限公司 | 取代的螺环衍生物 |
| JP2024518425A (ja) | 2021-05-08 | 2024-05-01 | ヤンセン ファーマシューティカ エヌ.ベー. | 置換スピロ誘導体 |
| WO2022237720A1 (en) | 2021-05-11 | 2022-11-17 | Janssen Pharmaceutica Nv | Combination therapies |
| CA3214861A1 (en) | 2021-05-11 | 2022-11-17 | Nikki DASKALAKIS | Combination therapies |
| CR20230605A (es) | 2021-06-01 | 2024-05-24 | Janssen Pharmaceutica Nv | Derivados de fenil-1h-pirrolo[2,3-c]piridina sustituidos |
| BR112023025436A2 (pt) | 2021-06-03 | 2024-02-27 | Janssen Pharmaceutica Nv | Piridazinas ou 1,2,4-triazinas substituídas por aminas espirocíclicas |
| PH12023553300A1 (en) * | 2021-06-17 | 2024-04-08 | Janssen Pharmaceutica Nv | (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cancer |
| CN116829559A (zh) * | 2021-12-03 | 2023-09-29 | 烨辉医药科技(上海)有限公司 | 羰基取代的二氮杂螺化合物及其用途 |
| JP2025530791A (ja) * | 2022-09-02 | 2025-09-17 | ハッチメッド リミティド | トリアジン化合物及びその使用 |
| EP4622635A1 (en) | 2022-11-24 | 2025-10-01 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
| WO2024218072A1 (en) | 2023-04-17 | 2024-10-24 | Janssen Pharmaceutica Nv | Combination of a menin-ll1 inhibitor, a dna intercalating agent and a pyrimidine analogue to treat a hematopoietic disorder. |
| WO2025082444A2 (en) | 2023-10-20 | 2025-04-24 | Janssen Pharmaceutica Nv | (r) -n-ethyl-5-fluoro-n-isopropyl-2- ( (5- (2- (6- ( (2-methoxyethyl) (methyl) amino) -2-methylhexan-3-yl) -2, 6-diazaspiro [3.4] octan-6-yl) -1, 2, 4-triazin-6-yl) oxy) benzamide, formulations and dosage regimens thereof, for use in treating cancer |
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| PH12022551502A1 (en) | 2023-04-24 |
| JOP20220154A1 (ar) | 2023-01-30 |
| CL2023001531A1 (es) | 2023-11-03 |
| UA129208C2 (uk) | 2025-02-05 |
| CA3161045A1 (en) | 2021-06-24 |
| AU2020404305A1 (en) | 2022-08-04 |
| US12473295B2 (en) | 2025-11-18 |
| KR20220118500A (ko) | 2022-08-25 |
| TW202525813A (zh) | 2025-07-01 |
| CN118255774A (zh) | 2024-06-28 |
| US20230142285A1 (en) | 2023-05-11 |
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| JP2023506530A (ja) | 2023-02-16 |
| CN114867721A (zh) | 2022-08-05 |
| CO2022009085A2 (es) | 2022-07-08 |
| WO2021121327A1 (en) | 2021-06-24 |
| CR20220346A (es) | 2022-10-26 |
| TW202138367A (zh) | 2021-10-16 |
| UY38988A (es) | 2021-06-30 |
| JP2024138279A (ja) | 2024-10-08 |
| ECSP22054700A (es) | 2022-11-30 |
| TWI878414B (zh) | 2025-04-01 |
| IL293965A (en) | 2022-08-01 |
| CN118255773A (zh) | 2024-06-28 |
| CL2022001583A1 (es) | 2023-02-03 |
| JP7554829B2 (ja) | 2024-09-20 |
| CN118344372A (zh) | 2024-07-16 |
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| EP4077312A4 (en) | 2024-01-17 |
| JP7781961B2 (ja) | 2025-12-08 |
| CL2023001530A1 (es) | 2023-11-03 |
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