AR085276A1 - P2X7R ANTAGONISTS AND ITS USE - Google Patents
P2X7R ANTAGONISTS AND ITS USEInfo
- Publication number
- AR085276A1 AR085276A1 ARP120100542A ARP120100542A AR085276A1 AR 085276 A1 AR085276 A1 AR 085276A1 AR P120100542 A ARP120100542 A AR P120100542A AR P120100542 A ARP120100542 A AR P120100542A AR 085276 A1 AR085276 A1 AR 085276A1
- Authority
- AR
- Argentina
- Prior art keywords
- acetamide
- p2x7r
- azaindole
- indole
- halogen
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- -1 CN- Chemical group 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 229910052794 bromium Inorganic materials 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 229910052740 iodine Inorganic materials 0.000 abstract 2
- RROJHIZQOZNMSH-UHFFFAOYSA-N n-(1h-indol-3-yl)acetamide Chemical compound C1=CC=C2C(NC(=O)C)=CNC2=C1 RROJHIZQOZNMSH-UHFFFAOYSA-N 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000003449 preventive effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente se refiere a antagonistas de P2X7R que son compuestos de N-indol-3-il-acetamida y N-azaindol-3-il-acetamida, a composiciones farmacéuticas que los comprenden y a su uso para el tratamiento preventivo o terapéutico de enfermedades mediadas por la actividad de P2X7R.Reivindicación 1: Un compuesto de N-indol-3-il-acetamida y N-azaindol-3-il-acetamida representado por la fórmula general (1), en donde, R1 es un resto de fórmula (2) ó (3); R2 es un grupo mono- o bicicloalquilo; R3 está seleccionado del alquilo C1-5 lineal o ramificado que puede estar opcionalmente sustituido con -OH, -CH2-OH, alcoxi C1-5, CN-, CF3, halógeno (es decir, Cl, F, Br o I), piperidino, morfolino, pirrolidino, 5H-tetrazolilpropilo, metilcarbamoilo, dimetilcarbamoilo o etilcarbamoilo, en donde Ra es alquilo C1-5; R4, R5, R6, R7 están seleccionados en cada aparición, de modo independiente, de hidrógeno, halógeno (es decir, Cl, F, Br o I), metilo, metoxi, ciano o trifluorometilo, o, de ser necesario por valencia, puede estar ausente; a, b, c, d, x están seleccionados en cada aparición, de modo independiente, de carbono o nitrógeno; o una de sus sales o solvatos farmacéuticamente aceptables (en donde x debe tener un sustituyente de hidrógeno si es carbono).This refers to P2X7R antagonists that are compounds of N-indole-3-yl-acetamide and N-azaindole-3-yl-acetamide, pharmaceutical compositions that comprise them and their use for preventive or therapeutic treatment of mediated diseases by the activity of P2X7R. Claim 1: A compound of N-indole-3-yl-acetamide and N-azaindole-3-yl-acetamide represented by the general formula (1), wherein R1 is a moiety of formula ( 2 or 3); R2 is a mono- or bicycloalkyl group; R3 is selected from the linear or branched C1-5 alkyl which may be optionally substituted with -OH, -CH2-OH, C1-5 alkoxy, CN-, CF3, halogen (ie, Cl, F, Br or I), piperidine , morpholino, pyrrolidino, 5H-tetrazolylpropyl, methylcarbamoyl, dimethylcarbamoyl or ethylcarbamoyl, wherein Ra is C1-5 alkyl; R4, R5, R6, R7 are selected at each occurrence, independently, from hydrogen, halogen (ie, Cl, F, Br or I), methyl, methoxy, cyano or trifluoromethyl, or, if necessary by valence, may be absent; a, b, c, d, x are selected at each occurrence, independently, of carbon or nitrogen; or one of its pharmaceutically acceptable salts or solvates (where x must have a hydrogen substituent if it is carbon).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11154877 | 2011-02-17 | ||
| US201161444479P | 2011-02-18 | 2011-02-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR085276A1 true AR085276A1 (en) | 2013-09-18 |
Family
ID=45558013
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100542A AR085276A1 (en) | 2011-02-17 | 2012-02-17 | P2X7R ANTAGONISTS AND ITS USE |
Country Status (2)
| Country | Link |
|---|---|
| AR (1) | AR085276A1 (en) |
| WO (1) | WO2012110190A1 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103819479B (en) * | 2014-03-10 | 2017-01-04 | 东华大学 | A kind of containing pyrimidine group rigidity Conjugate macrocycle compound and its preparation method and application |
| WO2020150417A2 (en) * | 2019-01-17 | 2020-07-23 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| CN113233958B (en) * | 2021-01-18 | 2023-09-19 | 阜阳欣奕华材料科技有限公司 | Preparation method of 2- (trans-4-n-propylcyclohexyl) propane-1, 3-diol |
| IL310724A (en) | 2021-08-10 | 2024-04-01 | Ifm Due Inc | Compounds and compositions for treating conditions associated with sting activity |
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-
2012
- 2012-01-20 WO PCT/EP2012/000260 patent/WO2012110190A1/en not_active Ceased
- 2012-02-17 AR ARP120100542A patent/AR085276A1/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2012110190A1 (en) | 2012-08-23 |
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