DK2953948T3 - Fluorinerede integrinantagonister - Google Patents
Fluorinerede integrinantagonister Download PDFInfo
- Publication number
- DK2953948T3 DK2953948T3 DK14749249.0T DK14749249T DK2953948T3 DK 2953948 T3 DK2953948 T3 DK 2953948T3 DK 14749249 T DK14749249 T DK 14749249T DK 2953948 T3 DK2953948 T3 DK 2953948T3
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- DK
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- Prior art keywords
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- pharmaceutically acceptable
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines 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
- A61K31/495—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
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- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/40—Cyclodextrins; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Ophthalmology & Optometry (AREA)
- Diabetes (AREA)
- Inorganic Chemistry (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (12)
1. Forbindelse med formlen I:
eller et farmaceutisk acceptabelt salt eller solvat deraf, hvor: Z er
R og R’ hver uafhængigt er H eller F, eller R og R’, sammen med det carbonatom, hvortil de er bundet, danner en 3- eller 4-leddet carbocyklisk eller heterocyklisk ring; Q er
X er CH eller N; Y er CH eller N; Ri er methoxy substitueret med 0, 1, 2 eller 3 fluoratomer; og forudsat at forbindelsen med formlen (I) indeholder mindst ét fluoratom.
2. Forbindelse ifølge krav 1, hvor R og R’ hver er H.
3. Forbindelse ifølge krav 1, hvor X er N og Y er CH.
4. Forbindelse ifølge krav 1, hvor X og Y hver er CH.
5. Forbindelse ifølge krav 1, hvor X og Y hver er N.
6. Forbindelse ifølge krav 1, hvor Ri er OCHF2.
7. Forbindelse ifølge krav 1 med formlen II:
eller et farmaceutisk acceptabelt salt eller solvat deraf.
8. Forbindelse ifølge krav 1, udvalgt fra gruppen bestående af:
eller et farmaceutisk acceptabelt salt eller solvat deraf.
9. Forbindelse ifølge krav 8, hvor forbindelsen er
eller et farmaceutisk acceptabelt salt eller solvat deraf.
10. Farmaceutisk sammensætning, der omfatter en forbindelse ifølge et hvilket som helst af de foregående krav eller et farmaceutisk acceptabelt salt eller solvat deraf, og en farmaceutisk acceptabel bærer eller excipiens, hvor den farmaceutiske sammensætning eventuelt omfatter en yderligere aktiv bestanddel, der er udvalgt ffa gruppen bestående af a) en antagonist af integrin α5β1, b) et c y to to k s i s k/an t i p ro 1 i fc rat i v t middel, c) en hæmmer af epidermal-afledt, fibroblast-afledt eller blodpladeafledt vækstfaktor, d) en hæmmer af VEGF, e) en hæmmer af Flk-1/KDR, Fit-1, Tck/Tie-2, eller Tic-1 og f) en hæmmer af phosphoinositid-3-kinase og en blanding deraf.
11. Forbindelse ifølge et hvilket som helst af kravene 1 til 9 eller farmaceutisk acceptabelt salt eller solvat deraf, eventuelt i kombination med én eller flere terapier, eller sammensætning ifølge krav 10 til anvendelse i en fremgangsmåde til behandling eller forebyggelse af en sygdom eller tilstand medieret af et αν-integrin hos en person.
12. Forbindelse eller sammensætning til anvendelsen ifølge krav 11, hvor sygdommen eller tilstanden er udvalgt fra gruppen bestående af makuladegeneration, diabetisk retinopati (DR), makulaødem, diabetisk makulaødem (DME) og makulaødem efter retinalveneokklusion (RVO).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361762087P | 2013-02-07 | 2013-02-07 | |
| US201361900706P | 2013-11-06 | 2013-11-06 | |
| PCT/US2014/015372 WO2014124302A1 (en) | 2013-02-07 | 2014-02-07 | Fluorinated integrin antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2953948T3 true DK2953948T3 (da) | 2017-12-18 |
Family
ID=51300167
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK14749249.0T DK2953948T3 (da) | 2013-02-07 | 2014-02-07 | Fluorinerede integrinantagonister |
Country Status (24)
| Country | Link |
|---|---|
| US (6) | US9518053B2 (da) |
| EP (3) | EP2953948B1 (da) |
| JP (2) | JP6494528B2 (da) |
| KR (1) | KR102216091B1 (da) |
| CN (2) | CN108690022B (da) |
| AU (1) | AU2014214737B2 (da) |
| BR (2) | BR122019026750B1 (da) |
| CA (1) | CA2899321C (da) |
| CY (1) | CY1120213T1 (da) |
| DK (1) | DK2953948T3 (da) |
| ES (2) | ES2763556T3 (da) |
| HR (1) | HRP20171873T1 (da) |
| HU (1) | HUE035357T2 (da) |
| IL (2) | IL240181A (da) |
| LT (1) | LT2953948T (da) |
| ME (1) | ME02938B (da) |
| PL (1) | PL2953948T3 (da) |
| PT (1) | PT2953948T (da) |
| RS (1) | RS56711B1 (da) |
| RU (1) | RU2698195C2 (da) |
| SI (1) | SI2953948T1 (da) |
| SM (1) | SMT201700611T1 (da) |
| WO (1) | WO2014124302A1 (da) |
| ZA (1) | ZA201505575B (da) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2953948T (pt) * | 2013-02-07 | 2017-12-12 | Scifluor Life Sciences Inc | Antagonistas de integrina fluorada |
| US8901144B2 (en) | 2013-02-07 | 2014-12-02 | Scifluor Life Sciences, Llc | Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives |
| SI3050878T1 (sl) | 2013-09-24 | 2022-01-31 | Fujifilm Corporation | Nova dušik-vsebujoča spojina ali njena sol ali kovinski kompleks le-te |
| WO2015175954A1 (en) * | 2014-05-16 | 2015-11-19 | Scifluor Life Sciences, Inc. | Alpha v integrin antagonist compositions |
| US9790222B2 (en) * | 2015-02-19 | 2017-10-17 | Scifluor Life Sciences, Inc. | Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof |
| BR112017023432A2 (pt) | 2015-04-30 | 2018-07-24 | Scifluor Life Sciences Inc | Derivados de ácido propiônico tetra- hidronaftiridinila e usos do mesmo |
| US10118929B2 (en) | 2016-04-27 | 2018-11-06 | Scifluor Life Sciences, Inc. | Nonanoic and decanoic acid derivatives and uses thereof |
| US11192889B2 (en) * | 2016-07-05 | 2021-12-07 | The Rockefeller University | Tetrahydronaphthyridinepentanamide integrin antagonists |
| BR112019009245A2 (pt) * | 2016-11-08 | 2019-07-16 | Bristol-Myers Squibb Company | azol amidas e aminas como inibidores de alfav integrina |
| HRP20210228T1 (hr) * | 2016-11-08 | 2021-03-19 | Bristol-Myers Squibb Company | Amidi pirola kao inhibitori alfa v integrina |
| WO2018183795A1 (en) * | 2017-03-30 | 2018-10-04 | Scifluor Life Sciences, Inc. | Method of making tetrahydronaphthyridinyl nonanoic acid compounds |
| WO2021231581A1 (en) | 2020-05-12 | 2021-11-18 | Scifluor Life Sciences, Inc. | METHODS OF TREATING OR PREVENTING VIRAL INFECTION WITH FLUORINATED α V INTEGRIN ANTAGONISTS |
| WO2023230042A1 (en) * | 2022-05-23 | 2023-11-30 | Ocuterra Therapeutics, Inc. | Treating diabetic retinopathy using an integrin inhibitor |
| US20250367180A1 (en) * | 2022-06-27 | 2025-12-04 | Ocuterra Therapeutics, Inc. | Stable ophthalmic formulations of a fluorinated integrin antagonist |
| GB202301024D0 (en) * | 2023-01-24 | 2023-03-08 | Univ Bradford | Compounds |
| CN116239665B (zh) * | 2023-03-10 | 2024-08-23 | 山东大学 | Ncf4在制备调控炎症小体激活的制剂中的应用和作为炎症性疾病的治疗靶点中的应用 |
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| US8901144B2 (en) | 2013-02-07 | 2014-12-02 | Scifluor Life Sciences, Llc | Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives |
| US9790222B2 (en) | 2015-02-19 | 2017-10-17 | Scifluor Life Sciences, Inc. | Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof |
| BR112017023432A2 (pt) | 2015-04-30 | 2018-07-24 | Scifluor Life Sciences Inc | Derivados de ácido propiônico tetra- hidronaftiridinila e usos do mesmo |
| WO2018183795A1 (en) | 2017-03-30 | 2018-10-04 | Scifluor Life Sciences, Inc. | Method of making tetrahydronaphthyridinyl nonanoic acid compounds |
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