AR057450A1 - DERIVATIVES OF N - [(1,2-DIFENIL-1H-IMIDAZOL-4- IL) METHYL] AMINA ITS PREPARATION AND ITS APPLICATION IN THERAPEUTICS - Google Patents
DERIVATIVES OF N - [(1,2-DIFENIL-1H-IMIDAZOL-4- IL) METHYL] AMINA ITS PREPARATION AND ITS APPLICATION IN THERAPEUTICSInfo
- Publication number
- AR057450A1 AR057450A1 ARP060102972A ARP060102972A AR057450A1 AR 057450 A1 AR057450 A1 AR 057450A1 AR P060102972 A ARP060102972 A AR P060102972A AR P060102972 A ARP060102972 A AR P060102972A AR 057450 A1 AR057450 A1 AR 057450A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- multiple times
- unsubstituted
- substituted once
- Prior art date
Links
- 239000003814 drug Substances 0.000 title 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 10
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- -1 methylenedioxy Chemical group 0.000 abstract 5
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000004429 atom Chemical group 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002883 imidazolyl group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical group C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- 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
- A61K31/41—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
- A61K31/4164—1,3-Diazoles
- A61K31/417—Imidazole-alkylamines, e.g. histamine, phentolamine
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Procedimiento de preparacion y aplicacion terapéutica. Reivindicacion 1: Compuesto de la formula (1) en la cual X representa un grupo -C(=O), -SO2-, -C(=O)-N(R6)-; R1 representa un alquilo C1-12 n sustituido o sustituido una o multiples veces con sustituyentes seleccionados independientemente entre un átomo de F, hidroxilo, alcoxi C1-4, fenoxi, un resto trifluorometoxi, difluorometoxi, difluorometiltio trifluorometiltio; un resto carbocíclico no aromático (C3-12) no sustituido o sustituido una o multiples veces con sustituyentes seleccionados independientemente entre alquilo C1-4, alcoxi C1-4, alquiltio C1-4, átomo de F, hidroxilo, trifluorometilo, trifluorometoxi, alquil C1-4-tio; un cicloalquil C3-7-metilo no sustituido o sustituido una o multiples veces en el carbociclo con sustituyentes seleccionados independientemente entre alquilo C1-4, alcoxi C1-4, F, hidroxilo, trifluorometilo, trifluorometoxi, un fenilo no sustituido o sustituido una o multiples veces con sustituyentes seleccionados independientemente entre un átomo de halogeno, hidroxilo, un grupo Alc, un grupo OAlc, metilendioxi, alquil C1-4-amino, dialquil C1-4-amino, ciano, nitro, un grupo S(O)nAlc, OS(O)nAlc, alquilC1-4-carbonilo; o entre un resto fenilo, fenoxi, pirrolilo, imidazolilo, piridilo o pirazolilo, en donde dicho sustituyente está no sustituido o sustituido una o multiples veces con un alquilo C1-4; un bencilo no sustituido o sustituido una o multiples veces en el fenilo con sustituyentes seleccionados independientemente entre un átomo de halogeno, un grupo Alc, un hidroxilo, un grupo OAlc, un metilendioxi, un grupo S(O)nAlc, OS(O)nAlc; y no sustituido o sustituido en alfa con uno o dos grupos iguales o diferentes, seleccionados entre un alquilo C1-4, un cicloalquilo C3-7; un fenetilo no sustituido o sustituido una o multiples veces en el fenilo con sustituyentes seleccionados independientemente entre un átomo de halogeno, alquilo C1-4, alcoxi C1-4, trifluorometilo; trifluorometoxi; un benzhidrilo, un benzhidrilmetilo; un 1,2,3,4-tetrahidronaftaleno no sustituido o sustituido una o multiples veces con un alquilo C1-4; un resto heterocíclico aromático seleccionado entre un pirrolilo, imidazolilo, furilo, tienilo, pirazolilo, oxazolilo, piridilo, indolilo, en donde dicho resto está no sustituido o sustituido una o multiples veces con sustituyentes seleccionados independientemente entre un átomo de halogeno o un alquilo C1-4, alcoxi C1-4, trifluorometilo, trifluorometoxi, ciano, nitro, alquil C1-4-tio; R2 representa un átomo de H o alquilo C1-3; R3 representa alquilo C1-5; R4 representa un fenilo sustituido una o multiples veces con sustituyentes seleccionados independientemente entre un átomo de halogeno, un grupo Alc, un grupo OAlc, un grupo S(O)nAlc o OS(O)nAlc; R5 representa un fenilo sustituido una o multiples veces con sustituyentes seleccionados independientemente entre un átomo de halogeno, un grupo Alc, OAlc, un grupo S(O)nAlc o OS(O)nAlc; R6 representa un átomo de H o alquilo C1-3; n representa 0 1 o 2; Alc representa un alquilo C1-4; no sustituido o sustituido una o multiples veces con un átomo de F; así como su hidrato o solvato.Procedure of preparation and therapeutic application. Claim 1: Compound of the formula (1) in which X represents a group -C (= O), -SO2-, -C (= O) -N (R6) -; R1 represents a C1-12 n alkyl substituted or substituted once or multiple times with substituents independently selected from an atom of F, hydroxyl, C1-4 alkoxy, phenoxy, a trifluoromethoxy moiety, difluoromethoxy, difluoromethylthio trifluoromethylthio; a non-aromatic (C3-12) carbocyclic moiety unsubstituted or substituted once or multiple times with substituents independently selected from C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, F atom, hydroxyl, trifluoromethyl, trifluoromethoxy, C1 alkyl -4-uncle; a C3-7-methylcycloalkyl unsubstituted or substituted once or multiple times in the carbocycle with substituents independently selected from C1-4 alkyl, C1-4 alkoxy, F, hydroxyl, trifluoromethyl, trifluoromethoxy, an unsubstituted or substituted one or multiple phenyl times with substituents independently selected from a halogen atom, hydroxyl, an Alc group, an OAlc group, methylenedioxy, C1-4-alkyl, C1-4 dialkyl, cyano, nitro, an S (O) nAlc, OS group (O) nAlc, C 1-4 alkylcarbonyl; or between a phenyl, phenoxy, pyrrolyl, imidazolyl, pyridyl or pyrazolyl moiety, wherein said substituent is unsubstituted or substituted once or multiple times with a C1-4 alkyl; a benzyl unsubstituted or substituted once or multiple times in the phenyl with substituents independently selected from a halogen atom, an Alc group, a hydroxyl, an OAlc group, a methylenedioxy, an S (O) nAlc, OS (O) nAlc group ; and unsubstituted or substituted in alpha with one or two same or different groups, selected from a C1-4 alkyl, a C3-7 cycloalkyl; a phenethyl unsubstituted or substituted once or multiple times in the phenyl with substituents independently selected from a halogen atom, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl; trifluoromethoxy; a benzhydryl, a benzhydrylmethyl; a 1,2,3,4-tetrahydronaphthalene unsubstituted or substituted once or multiple times with a C1-4 alkyl; an aromatic heterocyclic moiety selected from a pyrrolyl, imidazolyl, furyl, thienyl, pyrazolyl, oxazolyl, pyridyl, indolyl, wherein said moiety is unsubstituted or substituted once or multiple times with substituents independently selected from a halogen atom or a C1- alkyl 4, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy, cyano, nitro, C1-4 alkylthio; R2 represents an atom of H or C1-3 alkyl; R3 represents C1-5 alkyl; R4 represents a phenyl substituted once or multiple times with substituents independently selected from a halogen atom, an Alc group, an OAlc group, an S (O) nAlc or OS (O) nAlc group; R5 represents a phenyl substituted once or multiple times with substituents independently selected from a halogen atom, an Alc group, OAlc, an S (O) nAlc or OS (O) nAlc group; R6 represents an atom of H or C1-3 alkyl; n represents 0 1 or 2; Alc represents a C1-4 alkyl; not substituted or substituted once or multiple times with an atom of F; as well as its hydrate or solvate.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0507454 | 2005-07-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR057450A1 true AR057450A1 (en) | 2007-12-05 |
Family
ID=35966022
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060102972A AR057450A1 (en) | 2005-07-12 | 2006-07-11 | DERIVATIVES OF N - [(1,2-DIFENIL-1H-IMIDAZOL-4- IL) METHYL] AMINA ITS PREPARATION AND ITS APPLICATION IN THERAPEUTICS |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR057450A1 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9126944B2 (en) | 2013-02-28 | 2015-09-08 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| US9828345B2 (en) | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| US11091447B2 (en) | 2020-01-03 | 2021-08-17 | Berg Llc | UBE2K modulators and methods for their use |
-
2006
- 2006-07-11 AR ARP060102972A patent/AR057450A1/en not_active Application Discontinuation
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9126944B2 (en) | 2013-02-28 | 2015-09-08 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| US9458110B2 (en) | 2013-02-28 | 2016-10-04 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| US9828345B2 (en) | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| US11091447B2 (en) | 2020-01-03 | 2021-08-17 | Berg Llc | UBE2K modulators and methods for their use |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |