PE20191811A1 - Derivados de pirimidina como moduladores del receptor de pge2 - Google Patents
Derivados de pirimidina como moduladores del receptor de pge2Info
- Publication number
- PE20191811A1 PE20191811A1 PE2019002395A PE2019002395A PE20191811A1 PE 20191811 A1 PE20191811 A1 PE 20191811A1 PE 2019002395 A PE2019002395 A PE 2019002395A PE 2019002395 A PE2019002395 A PE 2019002395A PE 20191811 A1 PE20191811 A1 PE 20191811A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- membered
- pyrimidine derivatives
- ring
- receptor modulators
- Prior art date
Links
- 108010088540 Prostaglandin E receptors Proteins 0.000 title abstract 3
- 102000008866 Prostaglandin E receptors Human genes 0.000 title abstract 3
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 101150109738 Ptger4 gene Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 238000002512 chemotherapy Methods 0.000 abstract 1
- 150000001907 coumarones Chemical class 0.000 abstract 1
- XEYBRNLFEZDVAW-ARSRFYASSA-N dinoprostone Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1C\C=C/CCCC(O)=O XEYBRNLFEZDVAW-ARSRFYASSA-N 0.000 abstract 1
- 229960002986 dinoprostone Drugs 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 230000028993 immune response Effects 0.000 abstract 1
- 210000000987 immune system Anatomy 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- XEYBRNLFEZDVAW-UHFFFAOYSA-N prostaglandin E2 Natural products CCCCCC(O)C=CC1C(O)CC(=O)C1CC=CCCCC(O)=O XEYBRNLFEZDVAW-UHFFFAOYSA-N 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
- 238000001959 radiotherapy Methods 0.000 abstract 1
- 230000007420 reactivation Effects 0.000 abstract 1
- 238000002626 targeted therapy Methods 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
-
- 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
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—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
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
- C07D239/26—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
-
- 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
- C07D401/14—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 three or more hetero 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
- C07D403/12—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
-
- 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
-
- 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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
- C07D417/14—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Electrochromic Elements, Electrophoresis, Or Variable Reflection Or Absorption Elements (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Referido a un compuesto de formula I, en donde el anillo (A) es un anillo de 5 a 6 miembros aromaticos o un anillo no aromatico de 5 a 7 miembros, esta fusionado al grupo fenilo, en donde de forma independiente contiene opcionalmente 1 o 2 heteroatomos entre N, O, o S; (R1)n es 1, 2,3 o 4 sustituyentes opcionales, donde dichos sustituyentes R1 son alquilo (C1-3), alquenilo (C2-3), entre otros; R3 es H, metilo o trifluorometilo; R4a y R4b son independientemente H, metilo, entre otros; R5a y R5b son H, metilo, entre otros; Ar1 es fenilo o heteroarilo de 5 o 6 miembros, entre otros. Estos derivados de pirimidina modulan la respuesta inmune que comprende una reactivacion del sistema inmune en el tumor, actuando sobre el receptor de prostaglandina E2 (PGE2), especialmente, los receptores EP2 y/o EP4; tambien se refiere a nuevos derivados de benzofurano y benzotiofeno; procesos para la preparacion de dichos compuestos, composiciones farmaceuticas que los comprende, y su uso en combinacion con uno o mas agentes de quimioterapia y/o radioterapia y/o terapia dirigida en el tratamiento del cancer, como endometriosis, cancer de pulmon, entre otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2017061989 | 2017-05-18 | ||
| PCT/EP2018/062844 WO2018210988A1 (en) | 2017-05-18 | 2018-05-17 | Pyrimidine derivatives as pge2 receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20191811A1 true PE20191811A1 (es) | 2019-12-26 |
Family
ID=62196584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019002395A PE20191811A1 (es) | 2017-05-18 | 2018-05-17 | Derivados de pirimidina como moduladores del receptor de pge2 |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US11839613B2 (es) |
| EP (1) | EP3625228B1 (es) |
| JP (1) | JP7159215B2 (es) |
| KR (1) | KR102626982B1 (es) |
| CN (1) | CN110612299A (es) |
| AR (1) | AR111808A1 (es) |
| AU (1) | AU2018268311B2 (es) |
| BR (1) | BR112019024105A2 (es) |
| CA (1) | CA3060394A1 (es) |
| CL (1) | CL2019003274A1 (es) |
| CO (1) | CO2019010505A2 (es) |
| CR (1) | CR20190560A (es) |
| CY (1) | CY1124799T1 (es) |
| DK (1) | DK3625228T3 (es) |
| EA (1) | EA201992677A1 (es) |
| ES (1) | ES2887041T3 (es) |
| HR (1) | HRP20211380T1 (es) |
| HU (1) | HUE056382T2 (es) |
| IL (1) | IL270620B2 (es) |
| LT (1) | LT3625228T (es) |
| MA (1) | MA49128A (es) |
| MX (1) | MX388257B (es) |
| PE (1) | PE20191811A1 (es) |
| PH (1) | PH12019502564A1 (es) |
| PL (1) | PL3625228T3 (es) |
| PT (1) | PT3625228T (es) |
| RS (1) | RS62398B1 (es) |
| SG (1) | SG11201908097YA (es) |
| SI (1) | SI3625228T1 (es) |
| TW (1) | TW201900178A (es) |
| UA (1) | UA125124C2 (es) |
| WO (1) | WO2018210988A1 (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| IL270623B2 (en) | 2017-05-18 | 2023-03-01 | Idorsia Pharmaceuticals Ltd | History of phenyl as pge2 receptor modulators |
| JP7253500B2 (ja) | 2017-05-18 | 2023-04-06 | イドーシア ファーマシューティカルズ リミテッド | ピリミジン誘導体 |
| AR111807A1 (es) | 2017-05-18 | 2019-08-21 | Idorsia Pharmaceuticals Ltd | Derivados de benzofurano y benzotiofeno como moduladores del receptor pge2 |
| WO2021060281A1 (ja) * | 2019-09-24 | 2021-04-01 | Ａｇｃ株式会社 | プロスタグランジンｅ２レセプターｅｐ２／ｅｐ４デュアルアンタゴニスト |
| JP7802769B2 (ja) * | 2020-08-18 | 2026-01-20 | サイビン アイアールエル リミテッド | 治療用フェネチルアミン組成物およびその使用方法 |
| US20230390303A1 (en) | 2020-11-13 | 2023-12-07 | Ono Pharmaceutical Co., Ltd. | Cancer treatment by combination of ep4 antagonist and immune checkpoint inhibitor |
| WO2022272062A1 (en) | 2021-06-24 | 2022-12-29 | Reservoir Neuroscience, Inc. | Ep2 antagonist compounds |
| CN113248354B (zh) * | 2021-07-07 | 2022-04-22 | 山东国邦药业有限公司 | 一种氟氯苯乙酮的合成方法 |
| US12492178B2 (en) | 2021-09-01 | 2025-12-09 | Empathbio, Inc. | Stable polymorph of R-MDMA HCl |
| US11912680B2 (en) | 2021-12-28 | 2024-02-27 | Empathbio, Inc. | Nitric oxide releasing prodrugs of MDA and MDMA |
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| CN116041245B (zh) * | 2022-12-30 | 2025-03-07 | 上海毕得医药科技股份有限公司 | 一种4-(二氟甲氧基)-1h-吲哚-2-羧酸的制备方法 |
| EP4648851A1 (en) | 2023-01-10 | 2025-11-19 | Astrazeneca AB | Substituted (hetero)anilines and their use |
| WO2025149498A1 (en) | 2024-01-09 | 2025-07-17 | Astrazeneca Ab | Benzylpiperidine derivatives as trp4 antagonists for the treatment of inflammatory diseases |
| WO2025229177A1 (en) | 2024-05-02 | 2025-11-06 | Idorsia Pharmaceuticals Ltd | Crystalline forms of an n-substituted indole derivative |
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