AR111941A1 - Derivados de pirimidina como moduladores del receptor de pge2 - Google Patents
Derivados de pirimidina como moduladores del receptor de pge2Info
- Publication number
- AR111941A1 AR111941A1 ARP180101315A ARP180101315A AR111941A1 AR 111941 A1 AR111941 A1 AR 111941A1 AR P180101315 A ARP180101315 A AR P180101315A AR P180101315 A ARP180101315 A AR P180101315A AR 111941 A1 AR111941 A1 AR 111941A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydroxy
- ring
- cycloalkyl
- alkoxy
- Prior art date
Links
Classifications
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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
- A61K31/495—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
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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
- A61K31/495—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
- 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
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
- 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
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Electrochromic Elements, Electrophoresis, Or Variable Reflection Or Absorption Elements (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1) para uso en el tratamiento de un cáncer, donde dicho cáncer se trata mediante la modulación de una respuesta inmune que comprende una reactivación del sistema inmune en el tumor; donde dicho compuesto se utiliza opcionalmente en combinación con uno o más agentes de quimioterapia y/o radioterapia y/o terapia dirigida; donde en compuestos de la fórmula (1) (R¹)ₙ representa uno, dos o tres sustituyentes opcionales en el anillo de fenilo, donde dichos sustituyentes se seleccionan independientemente de alquilo C₁₋₃, alcoxi C₁₋₃, -S-alquilo C₁₋₃, halógeno, fluoroalquilo C₁₋₃, fluoroalcoxi C₁₋₃, ciano, hidroxi, nitro, -CO-O-alquilo-C₁₋₃, -NRN⁷RN⁸ donde RN⁷ y RN⁸ representan independientemente hidrógeno o alquilo C₁₋₄, o RN⁷ y RN⁸ junto con el nitrógeno al que están unidos forman un anillo carbocíclico de 4 a 6 miembros; R³ representa hidrógeno, metilo o trifluorometilo; R⁴ᵃ y R⁴ᵇ representan independientemente hidrógeno, metilo, o R⁴ᵃ y R⁴ᵇ junto con el átomo de carbono al que están unidos representan un grupo cicloprop-1,1-diilo; R⁵ᵃ y R⁵ᵇ representan independientemente hidrógeno, metilo, o R⁵ᵃ y R⁵ᵇ junto con el átomo de carbono al que están unidos representan un grupo cicloprop-1,1-diilo; Ar¹ representa fenilo, o heteroarilo de 5 ó 6 miembros; dicho fenilo o heteroarilo de 5 ó 6 miembros es independientemente mono-, di- o tri-sustituido donde los sustituyentes se seleccionan independientemente de alquilo C₁₋₆; alcoxi C₁₋₄; fluoroalquilo C₁₋₃, donde dicho fluoroalquilo C₁₋₃ está opcionalmente sustituido con hidroxi; fluoroalcoxi C₁₋₃; halógeno; ciano; cicloalquilo C₃₋₆, donde dicho cicloalquilo C₃₋₆ está no sustituido o mono-sustituido con amino; cicloalquilo C₄₋₆ que contiene un átomo de oxígeno del anillo, donde dicho cicloalquilo C₄₋₆ que contiene un átomo de oxígeno del anillo no está sustituido o está mono-sustituido con hidroxi; cicloalquil C₃₋₆-oxi; hidroxi; -X¹-CO-RO¹, donde X¹ representa un enlace directo, alquileno C₁₋₃, alquileno-O-C₁₋₃-*, -NH-alquileno C₁₋₃-*, -S-CH₂-*, -CF₂-, -CH=CH-, -CHºCH-, -NH-CO-*, -CO-, o cicloalquileno C₃₋₅; donde los asteriscos indican el enlace que está unido al grupo -CO-RO¹; y RO¹ representa -OH; -O-alquilo C₁₋₄; -NH-SO₂-RS³ donde RS³ representa alquilo C₁₋₄, cicloalquilo C₃₋₆ donde el cicloalquilo C₃₋₆ opcionalmente contiene un átomo de oxígeno del anillo, cicloalquilo C₃₋₆-alquileno C₁₋₃ donde el cicloalquilo C₃₋₆ opcionalmente contiene un átomo de oxígeno del anillo, fluoroalquilo C₁₋₃, o -NH₂; -O-CH₂-CO-RO⁴, donde RO⁴ representa hidroxi, o alcoxi C₁₋₄, o N[alquilo C₁₋₄]₂; -O-CH₂-O-CO-RO⁵, donde RO⁵ representa alquilo C₁₋₄ o alcoxi C₁₋₄; -O-CH₂-CH₂-N[alquilo C₁₋₄]₂; o (5-metil-2-oxo-[1,3]dioxol-4-il)-metiloxi-; -CO-CH₂-OH; un compuesto de fórmula (2); 2-hidroxi-3,4-dioxo-ciclobut-1-enilo; hidroxi-alquilo C₁₋₄; dihidroxi-alquilo C₂₋₄; hidroxi-alcoxi C₂₋₄; alcoxi C₁₋₄-alcoxi C₂₋₄; -(CH₂)ʳ-CO-NRN³RN⁴ donde r representa el número entero 0 ó 1; y donde RN³ y RN⁴ representan independientemente hidrógeno, alquilo C₁₋₄, hidroxi-alquilo C₂₋₄, alquilo C₁₋₃-alquilo C₂₋₄, o hidroxi; -X²-NRN¹RN², donde X² representa -(CH₂)ₘ-, donde m representa el número entero 0 ó 1; o X² representa -O-CH₂-CH₂-*, donde el asterisco indica el enlace que está unido al grupo -NRN¹RN²; y donde RN¹ y RN² representan independientemente hidrógeno, alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₂₋₄, cicloalquilo C₃₋₆, o fluoroalquilo C₂₋₃; o RN¹ representa independientemente hidrógeno o alquilo C₁₋₄, y RN² representa independientemente -CO-H, -CO-alquilo C₁₋₃, -CO-alquileno C₁₋₃-OH, o -CO-O-alquilo C₁₋₃; o RN¹ y RN² junto con el nitrógeno al que están unidos forman un anillo saturado de 4, 5 ó 6 miembros que contiene opcionalmente un átomo de oxígeno del anillo o de azufre del anillo, donde dicho anillo no está sustituido, o está mono-sustituido con oxo en un átomo de carbono del anillo, o disustituido con oxo en un átomo de azufre del anillo; -NH-CO-NRN⁵RN⁶ donde RN⁵ y RN⁶ representan independientemente hidrógeno o alquilo C₁₋₃; -SO₂-RS¹ donde RS¹ representa, hidroxi, alquilo C₁₋₄, o NRN⁷RN⁸ donde RN⁷ y RN⁸ representan independientemente hidrógeno o alquilo C₁₋₃; -S-RS² donde RS² representa alquilo C₁₋₄, o cicloalquilo C₃₋₆ que contiene opcionalmente un átomo de oxígeno del anillo; (CH₂)q-HET¹, donde q representa el número entero 0, 1 ó 2; y donde HET¹ representa 5-oxo-4,5-dihidro-[1,2,4]oxadiazol-3-ilo, 3-oxo-2,3-dihidro-[1,2,4]oxadiazol-5-ilo, o 5-tioxo-4,5-dihidro-[1,2,4]oxadiazol-3-ilo; -(CH₂)ₚ-HET, donde p representa el número entero 0 ó 1; y donde HET representa un heteroarilo de 5 ó 6 miembros, donde dicho heteroarilo de 5 ó 6 miembros está no sustituido, o mono- o di-sustituido, donde los sustituyentes se seleccionan independientemente de alquilo C₁₋₄, alcoxi C₁₋₄, -COOH, hidroxi, hidroxi-alquilo C₁₋₃, cicloalquilo C₃₋₅ que contiene opcionalmente un átomo de oxígeno del anillo, o NRN⁹RN¹⁰ donde RN⁹ y RN¹⁰ representan independientemente hidrógeno, alquilo C₁₋₃ o hidroxi-alquilo C₂₋₄; o Ar¹ representa heteroarilo bicíclico de 8 a 10 miembros; donde dicho heteroarilo bicíclico de 8 a 10 miembros es independientemente no sustituido, mono-, o di-sustituido, donde los sustituyentes se seleccionan independientemente de alquilo C₁₋₄; alcoxi C₁₋₄; fluoroalquilo C₁₋₃; fluoroalcoxi C₁₋₃; halógeno; ciano; hidroxi, o -alquileno C₀₋₃-COORO² donde RO² representa hidrógeno o alquilo C₁₋₄; o Ar¹ representa un grupo de la estructura de fórmula (3) donde el anillo (B) representa un anillo no aromático de 5 ó 6 miembros fusionado al grupo fenilo, donde el anillo (B) comprende uno o dos heteroátomos seleccionados independientemente de nitrógeno y oxígeno; donde dicho anillo (B) es independientemente no sustituido, mono-, o di-sustituido, donde los sustituyentes se seleccionan independientemente de oxo, alquilo C₁₋₆ y -alquileno C₀₋₃-COORO³ donde RO³ representa hidrógeno o alquilo C₁₋₃; o una sal aceptable para uso farmacéutico del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2017062031 | 2017-05-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR111941A1 true AR111941A1 (es) | 2019-09-04 |
Family
ID=62186480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180101315A AR111941A1 (es) | 2017-05-18 | 2018-05-17 | Derivados de pirimidina como moduladores del receptor de pge2 |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US11712438B2 (es) |
| EP (1) | EP3625222B1 (es) |
| JP (1) | JP7159214B2 (es) |
| KR (1) | KR102632028B1 (es) |
| CN (1) | CN110612296A (es) |
| AR (1) | AR111941A1 (es) |
| AU (1) | AU2018269666B2 (es) |
| BR (1) | BR112019024109A2 (es) |
| CA (1) | CA3060597A1 (es) |
| CL (1) | CL2019003275A1 (es) |
| CO (1) | CO2019010578A2 (es) |
| CR (1) | CR20190559A (es) |
| CY (1) | CY1124608T1 (es) |
| DK (1) | DK3625222T3 (es) |
| EA (1) | EA201992676A1 (es) |
| ES (1) | ES2893452T3 (es) |
| HR (1) | HRP20211533T1 (es) |
| HU (1) | HUE056080T2 (es) |
| IL (1) | IL270623B2 (es) |
| LT (1) | LT3625222T (es) |
| MA (1) | MA49126B1 (es) |
| MX (1) | MX2019013718A (es) |
| PE (1) | PE20191814A1 (es) |
| PH (1) | PH12019502563A1 (es) |
| PL (1) | PL3625222T3 (es) |
| PT (1) | PT3625222T (es) |
| RS (1) | RS62440B1 (es) |
| SG (1) | SG11201908729UA (es) |
| SI (1) | SI3625222T1 (es) |
| TW (1) | TWI765041B (es) |
| UA (1) | UA125123C2 (es) |
| WO (1) | WO2018210994A1 (es) |
Families Citing this family (8)
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| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| TW201900180A (zh) | 2017-05-18 | 2019-01-01 | 瑞士商愛杜西亞製藥有限公司 | 嘧啶衍生物 |
| CA3063632A1 (en) | 2017-05-18 | 2018-11-22 | Idorsia Pharmaceuticals Ltd | Benzofurane and benzothiophene derivatives as pge2 receptor modulators |
| MA49128A (fr) | 2017-05-18 | 2021-03-17 | Idorsia Pharmaceuticals Ltd | Dérivés de pyrimidine utilisés en tant que modulateurs des récepteurs des pge2 |
| CA3086925A1 (en) | 2018-01-05 | 2019-07-11 | Ichan School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
| EP3768267A4 (en) | 2018-03-20 | 2022-04-20 | Icahn School of Medicine at Mount Sinai | KINA INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE |
| WO2020142486A1 (en) * | 2018-12-31 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| KR20230107228A (ko) | 2020-11-13 | 2023-07-14 | 오노 야꾸힝 고교 가부시키가이샤 | Ep4 길항약과 면역 체크포인트 저해 물질의 병용에 의한 암 치료 |
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