- FIBROSIS INHIBITOR
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Medicament being useful as a fibrosis inhibitor for organs or tissues, which comprises a compound of the formula (I): wherein Ring Z is optionally substituted pyrrole ring, etc.; W2 is -CO-, -SO2-, optionally substituted C1-C4 alkylene, etc.; Ar2 is optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2):(1) W1 is optionally substituted C1-C4 alkylene, etc.; Ar1 is optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms:(2) W1 is optionally substituted C2-C5 alkylene, optionally substituted C2-C5 alkenylene, etc.; and Ar1 is aryl or monocyclic heteroaryl, which is substituted by carboxyl, alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof.
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- Pyrrole derivatives
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Pyrrole derivatives represented by the following formula: wherein Ring Z is an optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, an optionally substituted C1-C4 alkylene, etc.; Ar2 is an optionally substituted aryl, etc.; W2 and Ar1 mean the following (1) and (2): (1) W1 is an optionally substituted C1-C4 alkylene, etc.; Ar1 is an optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is an optionally substituted C2-C5 alkylene, an optionally substituted C2-C5 alkenylene, etc.; and Ar1 is an aryl or monocyclic heteroaryl, which are substituted by carboxyl, an alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof These compounds are useful as medicaments such as a fibrosis inhibitor for organs or tissues.
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- Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives
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A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1and R2each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8-positions of the quinoxaline nucleus, and R3, R4and R5each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain.
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- METHODS FOR USING (2-IMIDAZOLIN-2-YLAMINO) QUINOXALINE DERIVATIVES
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A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: STR1 and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R 1 and R 2 each is independently selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7-or 8-positions of the quinoxaline nucleus, and R 3, R 4 and R 5 each is located in one of the remaining 5-, 6-, 7-or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide treatment for ischemia.
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- Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives
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A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: STR1 , pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R5, R6 and R7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as constriction of one or more blood vessels and decongestion of one or more nasal passages.
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- METHODS FOR USING (2-IMIDAZOLIN-2-YLAMINO) QUINOXALINE DERIVATIVES
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A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: STR1 ,pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R 1 and R 4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R 2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R 3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7-or 8-positions of the quinoxaline nucleus; and R 5, R 6 and R 7 each is located in one of the remaining 5-, 6-, 7-or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, and reduction of at least one effect of an inflammatory disorder.
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- Method for using (2-imidazolin-2-ylamino) quinoxalines to reduce or maintain intraocular pressure
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Certain (2-imidazolin-2-ylamino) quinoxalines are disclosed. Such quinoxalines reduce or maintain intraocular pressure when administered directly to the eye of a mammal.
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- (2-imidazolin-2-ylamino) tetrahydroquinoxalines and methods for using same
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A compound selected from the group consisting of those having the formula: STR1 and pharmaceutically acceptable acid addition salts thereof, wherein R1 wherein R1 and R4 are independently selected from the group consisting of H and alkyl radicals containing 1 to 4 carbon atoms, R2 and R3 are independently selected from the group consisting of H, OXO, and alkyl radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R5, R6 and R7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the qunioxaline nucleus and is selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as alteration in the rate of fluid transport in the gastrointestinal tract, reduction in intraocular pressure, and increase in renal fluid flow.
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- Synthesis of the Food Mutagens MeIQx and 4,8-DiMeIQx by Copper(I) Promoted Quinoxaline Formation
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The regiocontrolled syntheses of the title compounds (1 and 2) is described.The key step is a new intramolecular alkyne amination and aromatization process (5 6; 8 9) effected by tetrakis(acetonitrile)copper(I) tetrafluoroborate.
- Knapp, Spencer,Ziv, Joseph,Rosen, Joseph D.
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p. 1293 - 1298
(2007/10/02)
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- 1,4,5,8-TETRA-AZAPHENANTHRENE COMPLEXES OF COPPER(I) AND SILVER(I)
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Cu(I) and Ag(I) complexes of 1,4,5,8-tetra-azaphenanthrene (TAP) and of two its methylated derivatives (3,6-dimethyl- and 2,3,6,7-tetramethyl-) have been made and characterized.Their 1HNMR spectra are discussed.The structure of the complex Ag(TAP)2(NO3), as determined by X-Ray crystallography, is that of strongly folded and twisted square planar arrangement of the chelating ligands around the silver atom; the four Ag-N bonds are not equal: they are shorter (2.36 Angstroem) in one pair of trans bonds than in the other (2.56 Angstroem). 3,6-Dimethyl-1,4,5,8-tetra-azaphenanthrene (3,6dmTAP), a new TAP derivative, has been synthesized starting from 2-hydroxy-3-methylquinoxaline which was nitrated, then treated with POCl3, the resulting 2-chloro-3-methyl-6-nitroquinoxaline reacted with hydrazine and the hydrazino group oxidized to give 3-methyl-6-nitroquinoxaline.This was aminated with hydroxylamine, reduced to the diamine and finally condensed with glyoxal to give 2,6-dimethyl- and 3,6-dimethyl-1,4,5,8-tetra-azaphenanthrene.
- Nasielski, J.,Nasielski-Hinkens, R.,Heilporn, S.,Rypens, C.,Declercq, J. P.
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p. 983 - 992
(2007/10/02)
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- SYNTHESIS OF 2-AMINO-3,8-DIMETHYLIMIDAZOQUINOXALINE (Me-IQx), A POTENT MUTAGEN ISOLATED FROM FRIED BEEF
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A potent mutagen, 2-amino-3,8-dimethylimidazoquinoxaline (Me-IQx), isolated from fried beef and its 3,7-dimethyl derivative were synthesized from 6-amino-3-methylquinoxaline and 6-amino-2-methylquinoxaline, respectively.These compounds showed strong mutagenic activity towards Salmonella typhimurium TA98 in the presence of S9 Mix.
- Kasai, Hiroshi,Shiomi, Tomoko,Sugimura, Takashi,Nishimura, Susumi
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p. 675 - 678
(2007/10/02)
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