DK2824100T3 - 1,2,5-oxadiazoler som inhibitorer af indolamin-2,3-dioxygenase - Google Patents
1,2,5-oxadiazoler som inhibitorer af indolamin-2,3-dioxygenase Download PDFInfo
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- DK2824100T3 DK2824100T3 DK14175271.7T DK14175271T DK2824100T3 DK 2824100 T3 DK2824100 T3 DK 2824100T3 DK 14175271 T DK14175271 T DK 14175271T DK 2824100 T3 DK2824100 T3 DK 2824100T3
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
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- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/08—1,2,5-Oxadiazoles; Hydrogenated 1,2,5-oxadiazoles
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- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
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- 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
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Claims (12)
- 4-({3-[(aminosulfonyl)amino]propyl}amino)-/V-(3-chlor-4-fluorphenyl)-/\/'- hydroxy-l,2,5-oxadiazol-3-carboximidamid; /V-(3-chlor-4-fluorphenyl)-/V'-hydroxy-4-({3- [(methylsulfonyl)amino]propyl>amino)-l,2,5-oxadiazol-3-carboximidamid; 4-({2-[(aminosulfonyl)amino]ethyl>amino)-/V-[4-fluor-3- (trifluormethyl)phenyl]-/V'-hydroxy-l,2,5-oxadiazol-3-carboximidamid; /V-[4-fluor-3-(trifluormethyl)phenyl]-/V'-hydroxy-4-({2-[(methylsulfonyl)amino] ethyl>-amino)-l ,2,5-oxadiazol-3-carboximidamid; 4-({3-[(aminosulfonyl)amino]propyl>amino)-/V-[4-fluor-3- (trifluormethyl)phenyl]-/V'-hydroxy-l,2,5-oxadiazol-3-carboximidamid; /V-[4-fluor-3-(trifluormethyl)phenyl]-/V'-hydroxy-4-({3- [(methylsulfonyl)amino]propyl>-amino)-l,2,5-oxadiazol-3-carboximidamid; 4-({2-[(aminosulfonyl)amino]ethyl>amino)-yV'-hydroxy-/V-[3- (trifluormethyl)phenyl]-l,2,5-oxadiazol-3-carboximidamid; /V'-hydroxy-4-({2-[(methylsulfonyl)amino]ethyl}amino)-/V-[3- (trifluormethyl)phenyl]-l,2,5-oxadiazol-3-carboximidamid; 4-({3-[(aminosulfonyl)amino]propyl}amino)-/V'-hydroxy-/\/-[3- (trifluormethyl)phenyl]-l,2,5-oxadiazol-3-carboximidamid; A/'-hydroxy-4-({3-[(methylsulfonyl)amino]propyl>amino)-/V-[3- (trifluormethyl)phenyl]-l,2,5-oxadiazol-3-carboximidamid; A/-(4-fluor-3-methylphenyl)-/V'-hydroxy-4-({2- [(methylsulfonyl)amino]ethyl}amino)-l,2,5-oxadiazol-3-carboximidamid; 4-({2-[(aminosulfonyl)amino]ethyl}amino)-/V-(3-cyano-4-fluorphenyl)-A/'-hydroxy-l,2,5-oxadiazol-3-carboximidamid; og /V-(3-cyano-4-fluorphenyl)-/V'-hydroxy-4-({2- [(methylsulfonyl)amino]ethyl>amino)-l,2,5-oxadiazol-3-carboximidamid; eller et farmaceutisk acceptabelt salt deraf, i kombination med et anti-PD-1-antistof til anvendelse ifølge krav 1. 7. 4-({2-[(aminosulfonyl)amino]ethyl}amino)-/V-(3-brom-4-fluorphenyl)-/V'-hydroxy-l,2,5-oxadiazol-3-carboximidamid, eller et farmaceutisk acceptabelt salt deraf, i kombination med et anti-PD-l-antistof til anvendelse ifølge krav 1. 8. 4-({2-[(aminosulfonyl)amino]ethyl}amino)-/V-(3-brom-4-fluorphenyl)-/V'-hydroxy-l,2,5-oxadiazol-3-carboximidamid, i kombination med et anti-PD-l-antistof til anvendelse ifølge krav 1.
- 9. Forbindelsen eller salt til anvendelse ifølge krav 1, hvor forbindelsen er en fast form af 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-brom-4-fluorphenyl)-N'-hydroxy-l,2,5-oxadiazol-3-carboximidamid, som er: (a) krystallinsk; eller (b) indeholder mindre end 2% vand.
- 10. Forbindelsen eller salt til anvendelse ifølge krav 9, hvor den faste form har et smeltepunkt på 162 til 166°C, ±3°C.
- 11. Forbindelsen eller salt til anvendelse ifølge krav 9, hvor den faste form har: (a) mindst én XRPD top, udtrykt som 2-theta, valgt fra 18,4° ±0,2°, 18,9° ±0,2°, 21,8° ±0,2°, 23,9° ±0,2°, 29,2° ±0,2°, og 38,7° ±0,2°; eller (b) mindst to XRPD toppe, udtrykt som 2-theta, valgt fra 18,4° ±0,2°, 18,9° ±0,2°, 21,8° ±0,2°, 23,9° ±0,2°, 29,2° ±0,2°, og 38,7° ±0,2°; eller (c) mindst tre XRPD toppe, udtrykt som 2-theta, valgt fra 18,4° ±0,2°, 18,9° ±0,2°, 21,8° ±0,2°, 23,9° ±0,2°, 29,2° ±0,2°, og 38,7° ±0,2°.
- 12. Forbindelse med formel F28:eller et farmaceutisk acceptabelt salt deraf, i kombination med et anti-PD-1-antistof til anvendelse i behandling af cancer, hvor: R4 er F, Cl, Br, eller I; og n er 1 eller 2. 13. 4-({2-[(aminosulfonyl)amino]ethyl}amino)-/V-[(4-brom-2-furyl)methyl]-/V'-hydroxy-l,2,5-oxadiazol-3-carboximidamid, eller et farmaceutisk acceptabelt salt deraf, i kombination med et anti-PD-l-antistof til anvendelse ifølge krav 12. 14. 4-({2-[(aminosulfonyl)amino]ethyl}amino)-/V-[(4-chlor-2-furyl)methyl]-/V'-hydroxy-l,2,5-oxadiazol-3-carboximidamid, eller et farmaceutisk acceptabelt salt deraf, i kombination med et anti-PD-l-antistof til anvendelse ifølge krav 12.
- 15. Forbindelsen, salt, eller fast form til anvendelse ifølge et hvilket som helst af kravene 1 til 12, hvor canceren er valgt fra melanom, tyktarm cancer, bugspytkirtelcancer, brystcancer, prostatacancer, lungecancer, hjernecancer, æggestokcancer, livmoderhalscancer, testikelcancer, nyrecancer, cancer i hoved og hals, lymfom, og leukæmi.
- 16. Forbindelsen, salt, eller fast form til anvendelse ifølge et hvilket som helst af kravene 7 til 11, hvor canceren er melanom.
- 17. Forbindelsen, salt, eller fast form til anvendelse ifølge et hvilket som helst af kravene 7 til 13, hvor canceren er æggestokcancer.
- 18. Forbindelsen, salt, eller fast form til anvendelse ifølge et hvilket som helst af kravene 7 til 13, hvor canceren er brystcancer.
- 19. Forbindelsen, salt, eller fast form til anvendelse ifølge et hvilket som helst af kravene 7 til 11, hvor canceren er bugspytkirtelcancer.
- 20. Forbindelsen, salt, eller fast form til anvendelse ifølge et hvilket som helst af kravene 7 til 11, hvor canceren er prostatacancer.
- 21. Forbindelsen, salt, eller fast form til anvendelse ifølge et hvilket som helst af kravene 7 til 11, hvor canceren er lungecancer.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US7887608P | 2008-07-08 | 2008-07-08 | |
US15087309P | 2009-02-09 | 2009-02-09 | |
EP09790108.6A EP2315756B9 (en) | 2008-07-08 | 2009-07-07 | 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase |
Publications (1)
Publication Number | Publication Date |
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DK2824100T3 true DK2824100T3 (da) | 2018-04-16 |
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Application Number | Title | Priority Date | Filing Date |
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DK14175271.7T DK2824100T3 (da) | 2008-07-08 | 2009-07-07 | 1,2,5-oxadiazoler som inhibitorer af indolamin-2,3-dioxygenase |
DK09790108.6T DK2315756T5 (da) | 2008-07-08 | 2009-07-07 | 1,2,5-oxadiazoler som inhibitorer af indolamin-2,3-dioxygenase |
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DK09790108.6T DK2315756T5 (da) | 2008-07-08 | 2009-07-07 | 1,2,5-oxadiazoler som inhibitorer af indolamin-2,3-dioxygenase |
Country Status (37)
Country | Link |
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US (12) | US8088803B2 (da) |
EP (3) | EP3360873A1 (da) |
JP (2) | JP5465720B2 (da) |
KR (5) | KR102031538B1 (da) |
CN (2) | CN102164902B (da) |
AR (1) | AR072490A1 (da) |
AU (6) | AU2009268739B2 (da) |
BR (2) | BR122019015876B8 (da) |
CA (2) | CA3012229C (da) |
CL (2) | CL2009001554A1 (da) |
CO (1) | CO6341622A2 (da) |
CR (1) | CR11871A (da) |
CY (1) | CY1120617T1 (da) |
DK (2) | DK2824100T3 (da) |
EA (2) | EA022669B1 (da) |
EC (1) | ECSP11010798A (da) |
ES (2) | ES2524266T3 (da) |
HK (2) | HK1157692A1 (da) |
HR (2) | HRP20141094T1 (da) |
HU (1) | HUE036813T2 (da) |
IL (2) | IL210402A (da) |
LT (1) | LT2824100T (da) |
ME (1) | ME03065B (da) |
MX (1) | MX2011000235A (da) |
MY (3) | MY177058A (da) |
NO (1) | NO2824100T3 (da) |
NZ (1) | NZ590268A (da) |
PE (1) | PE20110308A1 (da) |
PH (1) | PH12014500947B1 (da) |
PL (2) | PL2824100T3 (da) |
PT (2) | PT2315756E (da) |
RS (2) | RS53688B9 (da) |
SG (2) | SG192485A1 (da) |
SI (2) | SI2824100T1 (da) |
SM (1) | SMT201400179B (da) |
TW (1) | TWI453204B (da) |
WO (1) | WO2010005958A2 (da) |
Families Citing this family (168)
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EP2559690B1 (en) * | 2005-05-10 | 2016-03-30 | Incyte Holdings Corporation | Modulators of indoleamine 2,3-dioxygenase and methods of using the same |
JP5294874B2 (ja) | 2005-12-20 | 2013-09-18 | インサイト・コーポレイション | インドールアミン2,3−ジオキシゲナーゼのモジュレーターとしてのn−ヒドロキシアミジノヘテロ環 |
WO2008036642A2 (en) * | 2006-09-19 | 2008-03-27 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
RS53688B9 (sr) | 2008-07-08 | 2020-01-31 | Incyte Holdings Corp | 1,2,5-oksadiazoli kao inhibitori indoleamin 2,3-dioksigenaze |
US8299295B2 (en) | 2009-10-15 | 2012-10-30 | Johnson Matthey Public Limited Company | Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs |
GB0919757D0 (en) * | 2009-11-12 | 2009-12-30 | Johnson Matthey Plc | Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs |
NO2694640T3 (da) | 2011-04-15 | 2018-03-17 | ||
ES2903205T3 (es) | 2011-11-09 | 2022-03-31 | Kyowa Kirin Co Ltd | Compuestos heterocíclicos que contienen nitrógeno |
GB201120860D0 (en) | 2011-12-05 | 2012-01-18 | Cambridge Entpr Ltd | Cancer immunotherapy |
CA2880896C (en) | 2012-06-26 | 2021-11-16 | Del Mar Pharmaceuticals | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof |
US10034939B2 (en) | 2012-10-26 | 2018-07-31 | The University Of Chicago | Synergistic combination of immunologic inhibitors for the treatment of cancer |
AU2014251038A1 (en) | 2013-04-08 | 2015-11-26 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
ME03792B (me) * | 2013-11-08 | 2021-04-20 | Incyte Holdings Corp | Postupak sinteze inhibitora indolamin 2,3-dioksigenaze |
CN106456753B (zh) | 2014-02-04 | 2021-05-11 | 因塞特公司 | 用于治疗癌症的pd-1拮抗剂和ido1抑制剂的组合 |
CR20160500A (es) | 2014-03-31 | 2016-12-14 | Genentech Inc | Anticuerpos anti-ox40 y métodos de uso |
BR112016022345A2 (pt) | 2014-03-31 | 2017-10-10 | Genentech Inc | terapia de combinação compreendendo agentes antiangiogênese e agonistas de ligação de ox40 |
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UA127372C2 (uk) | 2015-07-30 | 2023-08-02 | Макродженікс, Інк. | Моноспецифічне pd-1-сполучне моноклональне антитіло |
UA125747C2 (uk) | 2015-09-01 | 2022-06-01 | Фьост Вейв Байо, Інк. | Способи та композиції для лікування станів, пов'язаних із аномальною запальною відповіддю |
CN114748473A (zh) | 2015-11-04 | 2022-07-15 | 因赛特公司 | 用于吲哚胺2,3-双加氧酶抑制及其适应症的药物组合物和方法 |
JP2018020710A (ja) | 2016-08-05 | 2018-02-08 | 三井造船株式会社 | 船舶用舵及び船舶 |
EP3697423A4 (en) | 2018-01-05 | 2021-08-11 | Dicerna Pharmaceuticals, Inc. | REDUCED EXPRESSION OF BETA-CATENIN AND IDO TO POTENTIALIZE IMMUNOTHERAPY |
KR20220044527A (ko) | 2019-08-01 | 2022-04-08 | 인사이트 코포레이션 | Ido 억제제의 투여 요법 |
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