AR111807A1 - Derivados de benzofurano y benzotiofeno como moduladores del receptor pge2 - Google Patents
Derivados de benzofurano y benzotiofeno como moduladores del receptor pge2Info
- Publication number
- AR111807A1 AR111807A1 ARP180101312A ARP180101312A AR111807A1 AR 111807 A1 AR111807 A1 AR 111807A1 AR P180101312 A ARP180101312 A AR P180101312A AR P180101312 A ARP180101312 A AR P180101312A AR 111807 A1 AR111807 A1 AR 111807A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydroxy
- ring
- cycloalkyl
- alkoxy
- Prior art date
Links
- IANQTJSKSUMEQM-UHFFFAOYSA-N 1-benzofuran Chemical compound C1=CC=C2OC=CC2=C1 IANQTJSKSUMEQM-UHFFFAOYSA-N 0.000 title 2
- 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 title 1
- 229960002986 dinoprostone Drugs 0.000 title 1
- XEYBRNLFEZDVAW-UHFFFAOYSA-N prostaglandin E2 Natural products CCCCCC(O)C=CC1C(O)CC(=O)C1CC=CCCCC(O)=O XEYBRNLFEZDVAW-UHFFFAOYSA-N 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 16
- 229910052739 hydrogen Inorganic materials 0.000 abstract 12
- 239000001257 hydrogen Substances 0.000 abstract 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- -1 cycloprop-1,1-diyl group Chemical group 0.000 abstract 7
- 150000002431 hydrogen Chemical group 0.000 abstract 7
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 7
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 4
- 206010028980 Neoplasm Diseases 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 238000002512 chemotherapy Methods 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000002993 cycloalkylene group Chemical group 0.000 abstract 1
- 239000012634 fragment Substances 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
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 238000001959 radiotherapy Methods 0.000 abstract 1
- 230000007420 reactivation Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- 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
-
- 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
-
- 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
- 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
- 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)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1) para el uso en el tratamiento de cáncer, donde dicho cáncer es tratado mediante la modulación de una respuesta inmunitaria que comprende una reactivación del sistema inmunitario en el tumor; donde dicho compuesto opcionalmente se usa en combinación con uno o más agentes de quimioterapia y/o radioterapia y/o terapia dirigida; donde, en compuestos de la fórmula (1): el fragmento de fórmula (2) está sustituido con R², donde R² representa hidrógeno, C₁₋₄ alquilo, halógeno, o ciano; y está opcionalmente sustituido con (R¹)ₙ; donde (R¹)ₙ representa uno, dos o tres sustituyentes opcionales, donde dichos sustituyentes R¹ se seleccionan de manera independiente de C₁₋₃ alquilo, C₁₋₃ alcoxi, halógeno, C₁₋₃ fluoroalquilo, C₁₋₃ fluoroalcoxi, o ciano; X representa S u O; R³ representa hidrógeno, metilo o trifluorometilo; R⁴ᵃ y R⁴ᵇ representan de manera independiente 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 de manera independiente 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; donde dicho fenilo o heteroarilo de 5 ó 6 miembros está de manera independiente mono-, di- o trisustituido, donde los sustituyentes se seleccionan de manera independiente de C₁₋₆ alquilo; C₁₋₄ alcoxi; C₁₋₃ fluoroalquilo, donde dicho C₁₋₃ fluoroalquilo está opcionalmente sustituido con hidroxi; C₁₋₃ fluoroalcoxi; halógeno; ciano; C₃₋₆ cicloalquilo, donde dicho C₃₋₆ cicloalquilo está no sustituido o mono-sustituido con amino; C₄₋₆ cicloalquilo que contiene un átomo de oxígeno de anillo, donde dicho C₄₋₆ cicloalquilo que contiene un átomo de oxígeno de anillo está no sustituido o mono-sustituido con hidroxi; C₃₋₆ cicloalquilo-oxi; hidroxi; X¹-CO-RO¹, donde X¹ representa un enlace directo, C₁₋₃ alquileno, -O-C₁₋₃ alquileno-*, -NH-C₁₋₃ alquileno-*, -S-CH₂-*, -CF₂-, -CH=CH-, -CHºCH-, -NH-CO-*, -CO-, o C₃₋₅ cicloalquileno; donde los asteriscos indican el enlace que está unido al grupo -CO-RO¹; y RO¹ representa -OH; -O-C₁₋₄ alquilo; -NH-SO₂-RS³ donde RS³ representa C₁₋₄ alquilo, C₃₋₆ cicloalquilo donde el C₃₋₆ cicloalquilo opcionalmente contiene un átomo de oxígeno de anillo, C₃₋₆ cicloalquilo-C₁₋₃ alquileno donde el C₃₋₆ cicloalquilo opcionalmente contiene un átomo de oxígeno de anillo, C₁₋₃ fluoroalquilo, o -NH₂; -O-CH₂-CO-RO⁴, donde RO⁴ representa hidroxi, o C₁₋₄ alcoxi, o -N[C₁₋₄ alquilo]₂; -O-CH₂-O-CO-RO⁵, donde RO⁵ representa C₁₋₄ alquilo o C₁₋₄ alcoxi; -O-CH₂-CH₂-N[C₁₋₄ alquilo]₂; o -(5-metilo-2-oxo-[1,3]dioxol-4-ilo)-metilooxi-; -CO-CH₂-OH; un resto de fórmula (3); 2-hidroxi-3,4-dioxo-ciclobut-1-enilo; hidroxi-C₁₋₄ alquilo; dihidroxi-C₂₋₄ alquilo; hidroxi-C₂₋₄ alcoxi; C₁₋₄ alcoxi-C₂₋₄ alcoxi; -(CH₂)ʳ-CO-NRN³RN⁴ donde r representa el número entero 0 ó 1; y donde RN³ y RN⁴ representan de manera independiente hidrógeno, C₁₋₄ alquilo, hidroxi-C₂₋₄ alquilo, C₁₋₃ alcoxi-C₂₋₄ alquilo, 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 de manera independiente hidrógeno, C₁₋₄ alquilo, C₁₋₄ alcoxi-C₂₋₄ alquilo, C₃₋₆ cicloalquilo, o C₂₋₃ fluoroalquilo; o RN¹ representa de manera independiente hidrógeno o C₁₋₄ alquilo, y RN² representa de manera independiente -CO-H, -CO-C₁₋₃ alquilo, -CO-C₁₋₃ alquileno-OH, o -CO-O-C₁₋₃ alquilo; o RN¹ y RN² junto con el nitrógeno al que están unidos forman un anillo saturado de 4, 5 ó 6 miembros que opcionalmente contiene un átomo de oxígeno de anillo o átomo de azufre de anillo, donde dicho anillo está no sustituido, o mono-sustituido con oxo en un átomo de carbono de anillo, o disustituido con oxo en un átomo de azufre de anillo; -NH-CO-NRN⁵RN⁶ donde RN⁵ y RN⁶ representan de manera independiente hidrógeno o C₁₋₄ alquilo; -SO₂-RS¹ donde RS¹ representa hidroxi, C₁₋₄ alquilo, o -NRN⁷RN⁸ donde RN⁷ y RN⁸ representan de manera independiente hidrógeno o C₁₋₃ alquilo; -S-RS² donde RS² representa C₁₋₄ alquilo, o C₃₋₆ cicloalquilo que opcionalmente contiene un átomo de oxígeno de 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 de manera independiente de C₁₋₄ alquilo, C₁₋₄ alcoxi, -COOH, hidroxi, hidroxi-C₁₋₃ alquilo, C₃₋₅ cicloalquilo que opcionalmente contiene un átomo de oxígeno de anillo, o -NRN⁹RN¹⁰ donde RN⁹ y RN¹⁰ representan de manera independiente hidrógeno, C₁₋₃ alquilo, o hidroxi-C₂₋₄ alquilo; o Ar¹ representa heteroarilo bicíclico de 8 a 10 miembros; donde dicho heteroarilo bicíclico de 8 a 10 miembros es de manera independiente no sustituido, mono-, o di-sustituido, donde los sustituyentes se seleccionan de manera independiente de C₁₋₄ alquilo; C₁₋₄ alcoxi; C₁₋₃ fluoroalquilo; C₁₋₃ fluoroalcoxi; halógeno; ciano; hidroxi, o -C₀₋₃ alquileno-COORO² donde RO² representa hidrógeno o C₁₋₄ alquilo; o Ar¹ representa un grupo de la estructura de fórmula (4), donde el anillo (B) representa un anillo de 5 ó 6 miembros no aromático fusionado al grupo fenilo, donde el anillo (B) comprende uno o dos heteroátomos seleccionados de manera independiente de nitrógeno y oxígeno; donde dicho anillo (B) es de manera independiente no sustituido, mono-, o di-sustituido, donde los sustituyentes se seleccionan de manera independiente de oxo, C₁₋₆ alquilo y -C₀₋₃ alquileno-COORO³ donde RO³ representa hidrógeno o C₁₋₃ alquilo; o una de sus sales farmacéuticamente aceptables.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2017061987 | 2017-05-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR111807A1 true AR111807A1 (es) | 2019-08-21 |
Family
ID=62196583
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180101312A AR111807A1 (es) | 2017-05-18 | 2018-05-17 | Derivados de benzofurano y benzotiofeno como moduladores del receptor pge2 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11325899B2 (es) |
| EP (1) | EP3625227B1 (es) |
| JP (1) | JP7093791B2 (es) |
| KR (1) | KR102612649B1 (es) |
| CN (1) | CN110621671A (es) |
| AR (1) | AR111807A1 (es) |
| CA (1) | CA3063632A1 (es) |
| ES (1) | ES2929309T3 (es) |
| TW (1) | TW201900179A (es) |
| WO (1) | WO2018210987A1 (es) |
Families Citing this family (12)
| 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 |
| HUE069643T2 (hu) | 2017-03-27 | 2025-03-28 | Hydro Quebec | Elektrolitkeverékekben vagy elektródaadalékként való felhasználásra szánt sók |
| 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 |
| LT3625222T (lt) | 2017-05-18 | 2021-11-10 | Idorsia Pharmaceuticals Ltd | Fenilo dariniai, kaip pge2 receptoriaus moduliatoriai |
| PT3625228T (pt) | 2017-05-18 | 2021-09-16 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores dos recetores de 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 |
| US20220048987A1 (en) * | 2020-08-13 | 2022-02-17 | The Board Of Trustees Of The Leland Stanford Junior University | Method of treatment to prevent or reverse age-associated inflammation, cognitive decline, and neurodegeneration |
| JPWO2022102731A1 (es) | 2020-11-13 | 2022-05-19 | ||
| EP4359399A4 (en) | 2021-06-24 | 2025-04-23 | Reservoir Neuroscience, Inc. | EP2 antagonist compounds |
| CN114539193B (zh) * | 2022-01-20 | 2024-08-06 | 安徽普利药业有限公司 | 一种盐酸胺碘酮中间体的制备方法 |
| WO2024102968A1 (en) * | 2022-11-10 | 2024-05-16 | Tempest Therapeutics, Inc. | Uses of ep2/ep4 antagonist compounds for treating familial adenomatous polyposis (fap) |
| WO2025229177A1 (en) | 2024-05-02 | 2025-11-06 | Idorsia Pharmaceuticals Ltd | Crystalline forms of an n-substituted indole derivative |
Family Cites Families (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5948786A (en) | 1996-04-12 | 1999-09-07 | Sumitomo Pharmaceuticals Company, Limited | Piperidinylpyrimidine derivatives |
| JP2003528144A (ja) | 2000-03-24 | 2003-09-24 | ファーマジーン ラボラトリーズ リミテッド | 頭痛治療のためのプロスタノイドｅｐ４受容体アンタゴニストの使用およびそのアンタゴニストについてのアッセイ |
| HN2001000224A (es) | 2000-10-19 | 2002-06-13 | Pfizer | Compuestos de imidazol condensado con arilo o heteroarilo como agentes anti - inflamatorios y analgesicos. |
| GB0031295D0 (en) | 2000-12-21 | 2001-01-31 | Glaxo Group Ltd | Naphthalene derivatives |
| GB0031302D0 (en) | 2000-12-21 | 2001-01-31 | Glaxo Group Ltd | Napthalene derivatives |
| GB0103269D0 (en) | 2001-02-09 | 2001-03-28 | Glaxo Group Ltd | Napthalene derivatives |
| EP1495005A1 (en) | 2002-04-12 | 2005-01-12 | Pfizer Japan Inc. | Pyrazole compounds as anti-inflammatory and analgesic agents |
| EP1494667A1 (en) | 2002-04-12 | 2005-01-12 | Pfizer Japan Inc. | Imidazole compounds as anti-inflammatory and analgesic agents |
| JP2006506327A (ja) | 2002-05-23 | 2006-02-23 | セラテクノロジーズ インコーポレイティド | プロスタグランジンｅ２の受容体サブタイプｅｐ４のアンタゴニスト・ポリペプチド |
| CN100408570C (zh) | 2003-01-29 | 2008-08-06 | 阿斯特兰德英国有限公司 | Ep4受体拮抗剂 |
| TW200519116A (en) | 2003-08-26 | 2005-06-16 | Teijin Pharma Ltd | Pyrrolopyrimidine derivatives |
| AP2006003534A0 (en) | 2003-09-03 | 2006-04-30 | Pfizer | Phenyl or pyridyl amide compounds as prostaglandin E2 antagonists. |
| EP1678147B1 (en) | 2003-09-15 | 2012-08-08 | Lead Discovery Center GmbH | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| GB0324269D0 (en) | 2003-10-16 | 2003-11-19 | Pharmagene Lab Ltd | EP4 receptor antagonists |
| JP4054369B2 (ja) | 2004-05-04 | 2008-02-27 | ファイザー株式会社 | オルト置換アリールまたはヘテロアリールアミド化合物 |
| BRPI0510666A (pt) | 2004-05-04 | 2007-12-04 | Pfizer | compostos de amida de arila ou heteroarila de metila substituìda, composições farmacêuticas compreendendo os mesmos, uso e combinação |
| HN2005000795A (es) * | 2004-10-15 | 2010-08-19 | Aventis Pharma Inc | Pirimidinas como antagonistas del receptor de prostaglandina d2 |
| AU2006246930C1 (en) | 2005-05-19 | 2012-01-19 | Merck Canada Inc. | Quinoline derivatives as EP4 antagonists |
| WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| AR060403A1 (es) | 2006-04-12 | 2008-06-11 | Sanofi Aventis | Compuestos de amino- pirimidina 2,6- sustituidos -4- monosustituidos como antagonistas del receptor de prostaglandina d2 |
| JP5244091B2 (ja) | 2006-04-24 | 2013-07-24 | メルク カナダ インコーポレイテッド | Ｅｐ４受容体アンタゴニストとしてのインドールアミド誘導体 |
| EP2035376B1 (en) | 2006-06-12 | 2014-08-27 | Merck Canada Inc. | Indoline amide derivatives as ep4 receptor ligands |
| US20080280891A1 (en) | 2006-06-27 | 2008-11-13 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
| WO2008008059A1 (en) | 2006-07-12 | 2008-01-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents ans uses thereof |
| CA2657227A1 (en) | 2006-07-14 | 2008-01-17 | Novartis Ag | Pyrimidine derivatives as alk-5 inhibitors |
| EP2054401B1 (en) | 2006-08-11 | 2013-05-01 | Merck Canada Inc. | Thiophenecarboxamide derivatives as ep4 receptor ligands |
| WO2008039882A1 (en) | 2006-09-30 | 2008-04-03 | Sanofi-Aventis U.S. Llc | A combination of niacin and a prostaglandin d2 receptor antagonist |
| WO2008104055A1 (en) | 2007-02-26 | 2008-09-04 | Merck Frosst Canada Ltd. | Indole and indoline cyclopropyl amide derivatives as ep4 receptor antagonists |
| EP2141147A1 (en) | 2007-03-26 | 2010-01-06 | Astellas Pharma Inc. | Ornithine derivative |
| CA2681146A1 (en) | 2007-03-26 | 2008-10-02 | Merck Frosst Canada Ltd. | Naphthalene and quinoline sulfonylurea derivatives as ep4 receptor antagonists |
| EP2014657A1 (de) | 2007-06-21 | 2009-01-14 | Bayer Schering Pharma Aktiengesellschaft | Diaminopyrimidine als Modulatoren des EP2-Rezeptors |
| US20110028463A1 (en) | 2007-07-03 | 2011-02-03 | Astellas Pharma Inc. | Amide compounds |
| CN101889004B (zh) | 2007-10-12 | 2014-09-10 | 阿斯利康公司 | 蛋白激酶抑制剂 |
| CA2714743C (en) | 2008-02-19 | 2017-01-17 | Janssen Pharmaceutica N.V. | Aryl-hydroxyethylamino-pyrimidines and triazines as modulators of fatty acid amide hydrolase |
| SI2565191T1 (sl) | 2008-05-14 | 2014-12-31 | Astellas Pharma Inc. | Derivati 4-(indol-7-ilkarbonilaminometil)cikloheksan karboksilne kisline kot EP4 receptorski antagonisti, uporabni za zdravljenje kronične ledvične odpovedi ali diabetične nefropatije |
| US20130225528A1 (en) | 2008-05-21 | 2013-08-29 | Ariad Pharmaceuticals, Inc. | Phosphorus Derivatives as Kinase Inhibitors |
| US8404736B2 (en) | 2008-08-14 | 2013-03-26 | Beta Pharma Canada Inc. | Heterocyclic amide derivatives as EP4 receptor antagonists |
| CN102164942B (zh) | 2008-09-19 | 2017-02-15 | 生物科技研究有限公司 | 三萜系化合物及其使用的方法 |
| JP2012503605A (ja) | 2008-09-25 | 2012-02-09 | メルク カナダ インコーポレイテッド | Ｅｐ４受容体アンタゴニストとしてのベータ−カルボリンスルホニルウレア誘導体 |
| WO2011022348A1 (en) | 2009-08-18 | 2011-02-24 | Janssen Pharmaceutica Nv | Ethylene diamine modulators of fatty acid amide hydrolase |
| WO2011063181A1 (en) | 2009-11-23 | 2011-05-26 | Lexicon Pharmaceuticals, Inc. | Methods and assays for the treatment of irritable bowel syndrome |
| JP5607241B2 (ja) | 2010-05-21 | 2014-10-15 | ケミリア・エービー | 新規ピリミジン誘導体 |
| PT2619182T (pt) | 2010-09-21 | 2017-01-17 | Eisai R&D Man Co Ltd | Composição farmacêutica |
| KR101857310B1 (ko) | 2010-09-29 | 2018-05-11 | 가부시키가이샤 에누비 켄코우겡큐쇼 | 인간 프로스타글란딘 e2 수용체 ep4 에 대한 항체 |
| WO2012066065A1 (en) | 2010-11-17 | 2012-05-24 | Novartis Ag | Phenyl-heteroaryl amine compounds and their uses |
| BR112013012380A2 (pt) | 2010-11-17 | 2016-08-30 | Novartis Ag | compostos 3-(aminoaril)-piridina |
| WO2012076063A1 (en) | 2010-12-10 | 2012-06-14 | Rottapharm S.P.A. | Pyridine amide derivatives as ep4 receptor antagonists |
| WO2012103071A2 (en) | 2011-01-25 | 2012-08-02 | Eisai R&D Management Co., Ltd. | Compounds and compositions |
| EP2688883B1 (en) | 2011-03-24 | 2016-05-18 | Noviga Research AB | Pyrimidine derivatives |
| EP2702043A1 (en) | 2011-04-29 | 2014-03-05 | Exelixis, Inc. | Inhibitors of inducible form of 6-phosphofructose-2-kinase |
| US9518044B2 (en) | 2011-06-20 | 2016-12-13 | Emory University | Prostaglandin receptor EP2 antagonists, derivatives, compositions, and uses related thereto |
| US9181279B2 (en) | 2011-07-04 | 2015-11-10 | Rottapharm Biotech S.R.L. | Cyclic amine derivatives as EP4 receptor antagonists |
| EP2554662A1 (en) | 2011-08-05 | 2013-02-06 | M Maria Pia Cosma | Methods of treatment of retinal degeneration diseases |
| US20150004175A1 (en) | 2011-12-13 | 2015-01-01 | Yale University | Compositions and Methods for Reducing CTL Exhaustion |
| RS61664B1 (sr) * | 2012-04-24 | 2021-04-29 | Vertex Pharma | Inhibitori dna-pk |
| TWI572597B (zh) | 2012-06-29 | 2017-03-01 | 美國禮來大藥廠 | 二甲基－苯甲酸化合物 |
| JO3296B1 (ar) | 2012-06-29 | 2018-09-16 | Lilly Co Eli | مركبات فينوكسي إيثيل بيبريدين |
| EP2711364A1 (en) | 2012-09-21 | 2014-03-26 | Chemilia AB | 4-(Indolyl or benzimidazolyl)amino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer |
| MY182386A (en) | 2012-11-27 | 2021-01-22 | Thomas Helledays Stiftelse For Medicinsk Forskning | Pyrimidine-2,4-diamine derivatives for treatment of cancer |
| UA115576C2 (uk) | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| EP2765128A1 (en) | 2013-02-07 | 2014-08-13 | Almirall, S.A. | Substituted benzamides with activity towards EP4 receptors |
| TW201443004A (zh) | 2013-02-15 | 2014-11-16 | Lilly Co Eli | 苯氧基乙氧基化合物 |
| TWI636046B (zh) | 2013-05-17 | 2018-09-21 | 美國禮來大藥廠 | 苯氧基乙基二氫－１ｈ－異喹啉化合物 |
| SG11201510121RA (en) | 2013-06-12 | 2016-01-28 | Kaken Pharma Co Ltd | 4-alkynyl imidazole derivative and medicine comprising same as active ingredient |
| AU2014315457B2 (en) | 2013-09-04 | 2018-05-10 | Bristol-Myers Squibb Company | Compounds useful as immunomodulators |
| JP6521977B2 (ja) | 2013-09-06 | 2019-05-29 | オーリジーン ディスカバリー テクノロジーズ リミテッドＡｕｒｉｇｅｎｅ Ｄｉｓｃｏｖｅｒｙ Ｔｅｃｈｎｏｌｏｇｉｅｓ Ｌｉｍｉｔｅｄ | 免疫調節剤としての１，２，４−オキサジアゾール誘導体 |
| WO2015044900A1 (en) | 2013-09-27 | 2015-04-02 | Aurigene Discovery Technologies Limited | Therapeutic immunomodulating compounds |
| CN105636958B (zh) | 2013-10-17 | 2018-01-05 | 沃泰克斯药物股份有限公司 | Dna‑pk抑制剂 |
| SI3424920T1 (sl) | 2013-10-17 | 2020-08-31 | Vertex Pharmaceuticals Incorporated | Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk |
| DK3083562T3 (da) | 2013-12-17 | 2017-11-13 | Lilly Co Eli | Cykliske phenoxyethylaminderivater og deres aktivitet som EP4-receptormodulatorer |
| SI3083554T1 (sl) | 2013-12-17 | 2019-04-30 | Eli Lilly & Company | Spojine dimetilbenzojske kisline |
| TW201607943A (zh) | 2013-12-19 | 2016-03-01 | 拜耳製藥公司 | 作為ｅｐ４配體之新穎苯并咪唑衍生物 |
| TW201623277A (zh) | 2014-03-26 | 2016-07-01 | 安斯泰來製藥股份有限公司 | 醯胺化合物 |
| US10052332B2 (en) | 2014-04-29 | 2018-08-21 | Emory University | Prostaglandin receptor EP2 antagonists, derivatives, compositions, and uses related thereto |
| CN106572993B (zh) | 2014-05-23 | 2019-07-16 | 卫材R&D管理有限公司 | Ep4拮抗剂在制备治疗癌症的药物中的应用 |
| SG11201609981RA (en) | 2014-06-04 | 2016-12-29 | Thomas Helledays Stiftelse För Medicinsk Forskning | Mth1 inhibitors for treatment of inflammatory and autoimmune conditions |
| WO2016021742A1 (en) | 2014-08-07 | 2016-02-11 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds as ep4 receptor antagonists |
| TWI712595B (zh) | 2015-01-09 | 2020-12-11 | 日商小野藥品工業股份有限公司 | 三環性螺化合物 |
| CN108368127B (zh) | 2015-07-23 | 2020-12-11 | 武田药品工业株式会社 | 化合物及其作为ep4受体拮抗剂的用途 |
| US10316040B2 (en) | 2015-10-16 | 2019-06-11 | Eisai R&D Management Co., Ltd. | EP4 antagonists |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| EP4219462A1 (en) | 2016-07-13 | 2023-08-02 | Vertex Pharmaceuticals Incorporated | Methods, compositions and kits for increasing genome editing efficiency |
| PT3625228T (pt) | 2017-05-18 | 2021-09-16 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores dos recetores de pge2 |
| LT3625222T (lt) | 2017-05-18 | 2021-11-10 | Idorsia Pharmaceuticals Ltd | Fenilo dariniai, kaip pge2 receptoriaus moduliatoriai |
| LT3625224T (lt) | 2017-05-18 | 2021-10-25 | Idorsia Pharmaceuticals Ltd | N-pakeistieji indolo dariniai |
| 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 |
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2018
- 2018-05-17 CN CN201880031813.3A patent/CN110621671A/zh active Pending
- 2018-05-17 EP EP18725497.4A patent/EP3625227B1/en active Active
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| KR20200007048A (ko) | 2020-01-21 |
| TW201900179A (zh) | 2019-01-01 |
| EP3625227B1 (en) | 2022-09-14 |
| US11325899B2 (en) | 2022-05-10 |
| WO2018210987A1 (en) | 2018-11-22 |
| CA3063632A1 (en) | 2018-11-22 |
| KR102612649B1 (ko) | 2023-12-11 |
| US20210115031A1 (en) | 2021-04-22 |
| JP2020520357A (ja) | 2020-07-09 |
| EP3625227A1 (en) | 2020-03-25 |
| JP7093791B2 (ja) | 2022-06-30 |
| CN110621671A (zh) | 2019-12-27 |
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