Back to results
US 2009/0214444 A1Published application
Poly aromatic sodium channel blockers
AssigneeParion Sciences, Inc.
InventorMichael Ross Johnson
Life of this patent
Estimating the term…
Abstract
Polyaromatic sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
Claims47
A compound represented by the formula (I):
- and racemates, enantiomers, diastereomers, tautomers, polymorphs, pseudopolymorphs and pharmaceutically acceptable salts, thereof, wherein:
- X is hydrogen, halogen, trifluoromethyl, lower alkyl, unsubstituted or substituted phenyl, lower alkyl-thio, phenyl-lower alkyl-thio, lower alkyl-sulfonyl, or phenyl-lower alkyl-sulfonyl;
- Y is hydrogen, hydroxyl, mercapto, lower alkoxy, lower alkyl-thio, halogen, lower alkyl, unsubstituted or substituted mononuclear aryl, or —N(R2)2;
- R1 is hydrogen or lower alkyl;
- each R2 is, independently, —R7, —(CH2)m—OR8, —(CH2)m—NR7R10, —(CH2)n(CHOR8)(CHOR8)n—CH2OR8, —(CH2CH2O)m—R8, —(CH2CH2O)m—CH2CH2NR7R10, —(CH2)n—C(═O)NR7R10, —(CH2)n-(Z)g-R7, —(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —(CH2)n—CO2R7, or
- R3 and R4 are each, independently, hydrogen, lower alkyl, hydroxyl-lower alkyl, phenyl, (phenyl)-lower alkyl, (halophenyl)-lower alkyl, ((lower-alkyl)phenyl)-lower-alkyl, ((lower-alkoxy)phenyl)-lower-alkyl, (naphthyl)-lower-alkyl, or (pyridyl)-lower-alkyl, or a group represented by formula A or formula B, with the proviso that at least one of R3 and R4 is a group represented by the formula A or formula B;
- —(C(RL)2)o-x-(C(RL)2)pA1 formula A
- —(C(RL)2)o-x-(C(RL)2)pA2 formula B
- A1 is a C7-C15-membered aromatic carbocycle substituted with at least one R5 and the remaining substituents are R6;
- A2 is a seven to fifteen-membered aromatic heterocycle substituted with at least one R5 and the remaining substituents are R6, wherein said aromatic heterocycle comprises 1-4 heteroatoms selected from the group consisting of O, N, and S;
- each RX is, independently, —R7, —(CH2), —OR8, —O—(CH2)m—R8, —(CH2)n—NR7R10), —O—(CH2)m—NR7R10, —(CH2)m(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m(CHOR8)(CHOR8)n—CH2OR8, —(CH2CH2O), —R8, —O—(CH2CH2O)m—R8, —(CH2CH2O)m—CH2CH2NR7R10, —O—(CH2CH2O)m—CH2CH2NR7R10, —(CH2)n—C(═O)NR7R10, —O—(CH2)m—C(═O)NR7R10, —(CH2)n-(Z)g-R7, —O—(CH2)m,(Z)g-R7, —(CH2)n—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —(CH2)n—CO2R7, —O—(CH2)m—CO2R7, —OSO3H, —O-glucuronide, —O-glucose,
- each o is, independently, an integer from 0 to 10;
- each p is, independently, an integer from 0 to 10;
- with the proviso that the sum of o and p in each contiguous chain is from 1 to 10;
- each x is, independently, O, NR10, C(═O), CHOH, C(═N—R10), CHNR7R10, or a single bond;
- each R5 is, independently, OH, —(CH2)m—OR8, —O—(CH2)m—OR8, —(CH2)n—NR7R10, —O—(CH2)m—NR7R10, —(CH2)n(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m(CHOR8)(CHOR8)n—CH2OR8, —(CH2CH2O)m—R8, —O—(CH2CH2O)m—R8, —(CH2CH2O)m—CH2CH2NR7R10, —O—(CH2CH2O)m—CH2CH2NR7R10, —(CH2)n—C(═O)NR7R10, —O—(CH2)m—C(═O)NR7R10, —(CH2)n-(Z)g-R7, —O—(CH2)m-(Z)g-R7, —(CH2)n—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)n—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —(CH2)n—CO2R7, —O—(CH2)m—CO2R7, —OSO3H, —O-glucuronide, —O-glucose,
- —(CH2)n—CO2R13, -Het-(CH2)m—CO2R13, —(CH2)n-(Z)g-CO2R13, -Het-(CH2)m-(Z)g-CO2R13, —(CH2)n—NR10—(CH2)m(CHOR8)n—CO2R13, -Het-(CH2)m—NR1O—(CH2)n—(CHOR8)n—CO2R13, —(CH2)n—(CHOR8)m—CO2R13, -Het-(CH2)m—(CHOR8)m—CO2R13, (CH2)m(CHOR8)m(Z)g-CO2R13, -Het-(CH2)n—(CHOR8)m-(Z)g-CO2R13, —(CH2)n-(Z)g-(CH2)m—CO2R13, —(CH2)n-(Z)g-(CH2)m—CO2R13, —(CH2)n-(Z)g(CHOR8)m-(Z)g-CO2R13, -Het-(CH2)n-(Z)g-(CHOR8)m-(Z)gCO2R13, —(CH2)n—CONH—C(═NR13)—NR13R13, -Het-(CH2)n—CO—NH—C(═NR13)—NR13R13, —(CH2)n-(Z)g-CONH—C(═NR13)—NR13R13, -Het-(CH2)n-(Z)g-CONH—C(═NR13)—NR13R13, —(CH2)n—NR10—(CH2)m(CHOR8)n—CONH—C(═NR13)—NR13R13, -Het-(CH2)n—NR10—(CH2)m(CHOR8)n—CONH—C(═NR13)—NR13R13, —(CH2), —(CHOR8)m—CONH—C(═NR13)—NR13R13, -Het-(CH2)n—(CHOR8)m—CONH—C(═NR13)—NR13R13, —(CH2)n—(CHOR8)m-(Z)g-CONH—C(═NR13)—NR13R13, -Het-(CH2)n—(CHOR8)m-(Z)g-CONH—C(═NR13)—NR13R13, —(CH2)n-(Z)g-(CH2)mCONH—C(═NR13)—NR13R13, -Het-(CH2)n-(Z)g-(CH2)mCONH—C(═NR13)—NR13R13, —(CH2)n-(Z)g-(CHOR8)m-(Z)g-CONH—C(═NR13)—NR13R13, Het-(CH2)n-(Z)g-(CHOR8)m-(Z)g-CONH—C(═NR13)—NR13R13, —(CH2)n—CONR7—CONR13R13, -Het-(CH2)n—CONR7—CONR13R13, —(CH2)n-(Z)g-CONR7—CONR13R13, —(CH2)n-(Z)g-CONR7—CONR13R13, —(CH2)n—NR10—(CH2)m(CHOR8)n—CONR7—CONR13R13, -Het-(CH2)n—NR10—(CH2)n—(CHOR8)m—CONR7—CONR13R13, —(CH2)n—(CHOR8)m—CONR7—CONR13R13, Het-(CH2)n—(CHOR8)m—CONR7—CONR13R13, —(CH2)n—(CHOR8)m-(Z)g-CONR7—CONR13R13, -Het-(CH2)n—(CHOR8)m-(Z)g-CNR7CONR13R13, —(CH2)n-(Z)g-(CH2)mCONR7—CONR13R13, -Het-(CH2)n-(Z)g-(CH2)mCONR7—CONR13R13, —(CH2)m-(Z)g(CHOR8)m-(Z)g-CONR7—CONR13R13,-Het-(CH2)n-(Z)g(CHOR8)m-(Z)g-CONR7—CONR13R13, —(CH2)n—CONR7SO2NR13R13, -Het-(CH2)m—CONR7SO2NR13R13, —(CH2)n-(Z)g-CONR7SO2NR13R13, -Het-(CH2)m-(Z)g-CONR7SO2NR13R13, —(CH2)n—NR10—(CH2)m(CHOR8)m—CONR7SO2NR13R13, -Het-(CH2)m—NR10—(CH2)m(CHOR8)n—CONR7SO2NR13R13, —(CH2)n—(CHOR8)m—CONR7SO2NR13R13, -Het-(CH2)m—(CHOR8)m—CONR7SO2NR13R13, —(CH2)n—(CHOR8)m-(Z)g-CONR7SO2NR13R13, -Het-(CH2)n—(CHOR8)m-(Z)g-CONR7SO2NR13R13, —(CH2)n-(Z)g-(CH2)mCONR7SO2NR13R13, -Het-(CH2)n-(Z)g-(CH2)mCONR7SO2NR13R13, —(CH2)n-(Z)g-(CHOR8)m-(Z)g-CONR7SO2NR13R13, -Het-(CH2)n-(Z)g-(CHOR8)m-(Z)g-CONR7SO2NR13R13, —(CH2)n—SO2NR13R13, -Het-(CH2)m—SO2NR13R13, —(CH2)n-(Z)g-SO2NR13R13, -Het-(CH2)m-(Z)g-SO2NR13R13, —(CH2)n—NR10—(CH2)m(CHOR8)n—SO2NR13R13, -Het-(CH2)m—NR10—(CH2)m(CHOR8)n—SO2NR13, —(CH2)n—(CHOR8)m—SO2NR13R13, -Het-(CH2)m—(CHOR8)m—SO2NR13R13, —(CH2)n—(CHOR8)m-(Z)g-SO2NR13R13, -Het-(CH2)n—(CHOR8)m-(Z)g-SO2NR13R13, —(CH2)n-(Z)g-(CH2)mSO2NR13R13, -Het-(CH2)n-(Z)g-(CH2)mSO2NR13R13, —(CH2)n-(Z)g-(CHOR8)m-(Z)g-SO2NR13R13, -Het-(CH2)n-(Z)g-(CHOR8)m-(Z)g-SO2NR13R13, —(CH2)n—CONR13, -Het-(CH2)n—CONR13R13, —(CH2)n-(Z)g-CONR13R13, -Het-(CH2)m-(Z)g-CONR13R13, —(CH2)m—NR10—(CH2)m(CHOR8)n—CONR13R13, -Het-(CH2)m—NR10—(CH2)m(CHOR8)n—CONR13R13, —(CH2)n—(CHOR8)m—CONR13R13, -Het-(CH2)m—(CHOR8)m—CONR13R13, —(CH2)n—(CHOR8)m-(Z)g-CONR13R13, -Het-(CH2)n—(CHOR8)m-(Z)g-CONR13R13, —(CH2)n-(Z)g-(CH2)mCONR13R13, -Het-(CH2)n-(Z)g-(CH2)mCONR13R13, —(CH2)n-(Z)g-(CHOR8)m-(Z)g-CONR13R13, -Het-(CH2)n-(Z)g-(CHOR8)m-(Z)g-CONR13R13, —(CH2)n—CONR7COR13, -Het-(CH2)m—CONR7COR13, —(CH2)n-(Z)g-CONR7COR13, -Het-(CH2)m-(Z)g-CONR7COR13, —(CH2)n—NR10—(CH2)m(CHOR8)n—CONR7COR13, -Het-(CH2)m—NR10—(CH2)m(CHOR8)m—CONR7COR13, —(CH2)n—(CHOR8)m—CONR7COR13, -Het-(CH2)m—(CHOR8)m—CONR7COR13, —(CH2)n—(CHOR8)m-(Z)g-CONR7COR13, -Het-(CH2)n—(CHOR8)n-(Z)g-CONR7COR13, —(CH2)n-(Z)g-(CH2)mCONR7COR13, —(CH2)n-(Z)g-(CH2)mCONR7COR13, -Het-(CH2)n-(Z)g-(CHOR8)m-(Z)g-CONR7COR13, —(CH2)n—CONR7CO2R13, —(CH2)n-(Z)g-CONR7CO2R13, -Het-(CH2)m-(Z)g-CONR7CO2R13, —(CH2)n—NR10—(CH2)m(CHOR8)n—CONR7CO2R13, -Het-(CH2)m—NR10—(CH2)m(CHOR8)n—CONR7CO2R13, —(CH2)n—(CHOR8)m—CONR7CO2R13, -Het(CH2)m—(CHOR8)m—CONR7CO2R13, —(CH2)n—(CHOR8)m-(Z)g-CONR7CO2R13, -Het-(CH2)n—(CHOR8)m-(Z)g-CONR7CO2R13, —(CH2)n-(Z)g-(CH2)mCONR7CO2R13, -Het-(CH2)n-(Z)g-(CH2)mCONR7CO2R13, —(CH2)n-(Z)g-(CHOR8)n-(Z)g-CONR7CO2R13, -Het-(CH2)n-(Z)g-(CHOR8)m-(Z)g-CONR7CO2R13, —(CH2)n—NH—C(═NR13)—NR13R13, -Het-(CH2)m—NH—C(═NR13)—NR13R13, —(CH2)n-(Z)g-NH—C(═NR13)—NR13R13, -Het-(CH2)m-(Z)g-NH—C(═NR13)—NR13R13, —(CH2)n—NR10—(CH2)m(CHOR8)n—NH—C(═NR13)—NR13R13, -Het-(CH2)m—NR10—(CH2)m(CHOR8)m—NH—C(═NR13)—NR13R13, —(CH2)n—(CHOR8)m—NH—C(═NR13)—NR13R13, -Het-(CH2)m—(CHOR8)m—NH—C(═NR13)—NR13R13, —(CH2)n—(CHOR8)m-(Z)g-NH—C(═NR13)—NR13R13, -Het-(CH2)n—(CHOR8)m-(Z)g-NH—C(═NR13)—NR13R13, —(CH2)n-(Z)g-(CH2)mNH—C(═NR13)—NR13R13, -Het-(CH2)n-(Z)g-(CH2)mNH—C(═NR13)—NR13R13, —(CH2)-(Z)g-(CHOR8)m-(Z)g-NH—C(═NR13)—NR13R13, -Het-(CH2)n-(Z)g-(CHOR8)m-(Z)g-NH—C(═NR13)—NR13R13, —(CH2)n—C(═NR13)—NR13R13, Het-(CH2)m—C(═NH)—NR13R13, —(CH2)n-(Z)g-C(═NH)—NR13R13, Het-(CH2)m-(Z)g-C(═NH)—NR13R13, —(CH2)n—NR10—(CH2)m(CHOR8)n—C(═NR13)—NR13R13, Het-(CH2)m—NR10—(CH2)m(CHOR8)n—C(═NR13)—NR13R13, —(CH2)n—(CHOR8)m—C(═NR13)—NR13R13, -Het-(CH2)m—(CHOR8)m—C(═NR13)—NR13R13, —(CH2), —(CHOR8)m-(Z)g-C(═NR13)—NR13R13, -Het-(CH2)n—(CHOR8)m-(Z)g-C(═NR13)—NR13R13, —(CH2)n-(Z)g-(CH2)m—C(═NHC(═NR13)—NR13R13, Het-(CH2)n-(Z)g-(CH2)m—C(═NR13)—NR13R13, —(CH2)n-(Z)g-(CHOR8)m-(Z)g-C(═NR13)—NR13R13, -Het-(CH2)n-(Z)g-(CHOR8)m-(Z)g-C(═NR13)—NR13R13, —(CH2)n—NR12R12, —O—(CH2)n—NR12R12, —O—(CH2)n—NR12R12, O—(CH2)m(Z)gR12, —(CH2)nNR11R11, —O—(CH2)m—NR11R11, —(CH2)n—N⊕—(R11)3, —O—(CH2)m—N⊕—(R11)3, —(CH2)n-(Z)g-(CH2)m—NR10R10, —O—(CH2)m-(Z)g-(CH2)m—NR10R10, —(CH2CH2O)m—CH2CH2NR12R12, —O—(CH2CH2O)m—CH2CH2NR12R12, —(CH2)n—(C═O)NR12R12, —O—(CH2)m—(C═O)NR12R12, —O—(CH2)m—(CHOR8)mCH2NR10-(Z)g-R10, —(CH2)n—(CHOR8)mCH2—NR10-(Z)g-R10, —(CH2)nNR10—O(CH2)m(CHOR8)nCH2NR10-(Z)g-R10, —O(CH2)m—NR10—(CH2)m—(CHOR8)nCH2NR10-(Z)g-R10, -(Het)-(CH2)m—OR8, -(Het)-(CH2)m—NR7R10, -(Het)-(CH2)m(CHOR8)(CHOR8)n—CH2OR8, -(Het)-(CH2CH2O)m—R8, -(Het)-(CH2CH2O)m—CH2CH2NR7R10, -(Het)-(CH2)m—C(═O)NR7R10, -(Het)-(CH2)m-(Z)g-R7, -(Het)-(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, -(Het)-(CH2)m—CO2R7, -(Het)-(CH2)n—NR12R12, -(Het)-(CH2)n—NR12R12, -(Het)-(CH2)m-(Z)gR12, -(Het)-(CH2)mNR11R11, -(Het)-(CH2)m—N⊕—(R11)3, -(Het)-(CH2)m-(Z)g-(CH2)n—NR10R10, -(Het)-(CH2CH2O)m—CH2CH2NR10, -(Het)-(CH2)m—(C═O)NR12R12, -(Het)-(CH2)m—(CHOR8)mCH2NR10-(Z)g-R10, -(Het)-(CH2)m—NR10—(CH2)m—(CHOR8)nCH2NR10-(Z)g-R10, —(CH2)n(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m(CHOR8)(CHOR8)n—CH2OR8—(CH2)—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8,
- —O—(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, Link (CH2)n-CAP, Link-(CH2)n(CHOR8)(CHOR8)n-CAP, Link-(CH2CH2O)m—CH2-CAP, Link-(CH2CH2O)m—CH2CH2-CAP, Link-(CH2)n-(Z)g-CAP, Link-(CH2)n(Z)g-(CH2)m-CAP, Link-(CH2)n—NR13—CH2(CHOR8)(CHOR8)n-CAP, Link-(CH2)n—(CHOR8)mCH2—NR13-(Z)g-CAP, Link-(CH2)nNR13—(CH2)m(CHOR8)mCH2NR13-(Z)g-CAP, -Link-(CH2)m-(Z)g-(CH2)m-CAP, Link-NH—C(═O)—NH—(CH2)m-CAP, Link-(CH2)m—C(═O)NR13—(CH2)m—C(═O)NR10R10, Link-(CH2)m—C(═O)NR13—(CH2)m-CAP, Link-(CH2)m—C(═O)NR11R11, Link-(CH2)m—C(═O)NR12R12, Link-(CH2)n-(Z)g-(CH2)m-(Z)g-CAP, Link-(Z)g-(CH2)m-Het-(CH2)m-CAP, Link-(CH2)nCR11R11-CAP, Link-(CH2)n(CHOR8)(CHOR8)n—CR11R11-CAP, Link-(CH2CH2O)m—CH2 CR11R11-CAP, Link-(CH2CH2O)m—CH2CH2—CR11R11-CAP, Link-(CH2)n-(Z)g-CR11R11-CAP, Link-(CH2)n(Z)g-(CH2)m—CR11R11-CAP, Link-(CH2)n—NR13—CH2(CHOR8)(CHOR8)n—CR11R11-CAP, Link-(CH2)n—(CHOR8)mCH2—NR13-(Z)g-CR11R11-CAP, Link-(CH2)nNR13—(CH2)m(CHOR8)nCH2NR13-(Z)g-CR11R11-CAP, Link-(CH2)m-(Z)g-(CH2)m—CR11R11-CAP, Link NH—C(═O)—NH—(CH2)m—CR11R11-CAP, Link-(CH2)m—C(═O)NR13—(CH2)m—CR11R11-CAP, Link-(CH2)n-(Z)g-(CH2)m-(Z)g-CR11R11-CAP, or Link-(Z)g-(CH2)m-Het-(CH2)m—CR11R11-CAP;
- each R6 is, independently, R5, —R7, —OR11, —N(R7)2, —(CH2)m—OR8, —O—(CH2)m—OR8, —(CH2)n—NR7R10, —O—(CH2)m—NR7R10, —(CH2)n(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m(CHOR8)(CHOR8)n—CH2OR8, —(CH2CH2O)m—R8, —O—(CH2CH2O)m—R8, —(CH2CH2O)m—CH2CH2NR7R10, —O—(CH2CH2O)m—CH2CH2NR7R10, —(CH2)n—C(═O)NR7R10, —O—(CH2)m—C(═O)NR7R10, —(CH2)n-(Z)g-R7, —O—(CH2)m-(Z)g-R7, —(CH2)n—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —O—(CH2)m—NR10—CH2(CHOR8)(CHOR8)n—CH2OR8, —(CH2)n—CO2R7, O—(CH2)m—CO2R7, —OSO3H, —O-glucuronide, —O-glucose,
- wherein when two R6 are —OR11 and are located adjacent to each other on the aromatic carbocycle or aromatic heterocycle, the two OR11 may form a methylenedioxy group;
- each R7 is, independently, hydrogen, lower alkyl, phenyl, substituted phenyl or —CH2(CHOR8)m—CH2OR8;
- each R8 is, independently, hydrogen, lower alkyl, —C(═O)—R11, glucuronide, 2-tetrahydropyranyl, or
- each R9 is, independently, —CO2R7, —CON(R7)2, —SO2CH3, —C(═O)R7, —CO2R13, —CON(R13)2, —SO2CH2R13, or —C(═O)R13;
- each R10 is, independently, —H, —SO2CH3, —CO2R7, —C(═O)NR7R9, —C(═O)R7, or —CH2—(CHOH)n—CH2OH;
- each Z is, independently, —(CHOH)—, —C(═O)—, —(CHNR7R10)—, —(C═NR10)—, —NR10—, —(CH2)n—, —(CHNR13R13)—, —(C═NR13)—, or —NR13_;
- each R11 is, independently, hydrogen, lower alkyl, phenyl lower alkyl or substituted phenyl lower alkyl;
- each R12 is, independently, —SO2CH3, —CO2R7, —C(═O)NR7R9, —C(═O)R7, —CH2(CHOH)n—CH2OH, —CO2R13, —C(═O)NR13R13, or —C(═O)R13;
- each R13 is, independently, R7, R10, —(CH2)m—NR7R10, —(CH2)m—NR7R7, —(CH2)m—NR11R11, —(CH2)m—(NR7R11R11)+, —(CH2)m—(CHOR8)m—(CH2)mNR11R11, —(CH2)m—(CHOR8)m—(CH2)mNR7R10, —(CH2)m—NR10R10, —(CH2)m—(CHOR8)m—(CH2)m—(NR11R11R11)+, —(CH2)m—(CHOR8)m—(CH2)mNR7R7,
- with the proviso that in the moiety —NR13R13, the two R13 along with the nitrogen to which they are attached may, optionally, form a ring selected from:
- each V is, independently, (CH2)m—NR7R10, —(CH2)m—NR7R7, —(CH2)m—(NR11R11R11)+, —(CH2)n—(CHOR8)m—(CH2)mNR7R10, —(CH2)n—NR1R10—(CH2)n—(CHOR8)m—(CH2)mNR7R7, —(CH2)n—(CHOR8)m—(CH2)m—(NR11R11R11)+ with the proviso that when V is attached directly to a nitrogen atom, then V can also be, independently, R7, R10, or (R11)2;
- each R14 is, independently, H, R12, —(CH2)n—SO2CH3, —(CH2)n—CO2R13, —(CH2)n—C(═O)NR13R13, —(CH2)n—C(═O)R13, —(CH2)n—(CHOH)n—CH2OH, —NH—(CH2)n—SO2CH3, NH—(CH2)n—C(═O)R11, NH—C(═O)—NH—C(═O)R11, —C(═O)NR13R13, —OR11, —NH—(CH2)n—R10, —Br, —Cl, —F, —I, SO2NHR11, —NHR13, —NH—C(═O)—NR13R13, —(CH2)n—NHR13, or —NH—(CH2)n—C(═O)—R13;
- each g is, independently, an integer from 1 to 6;
- each m is, independently, an integer from 1 to 7;
- each n is, independently, an integer from 0 to 7;
- each -Het- is, independently, —N(R7)—, —N(R10)—, —S—, —SO—, —SO2—, —O—, —SO2NH—, —NHSO2—, —NR7CO—, —CONR7—, —N(R13)—, —SO2NR13—, —NR13CO—, or —CONR13—;
- each Link is, independently, —O—, —(CH2)n—, —O(CH2)m—, —NR13—C(═O)—NR13—, —NR13—C(═O)—(CH2)m—, —C(═O)NR13—(CH2)m−, —(CH2)n-(Z)g-(CH2)n—, —S—, —SO—, —SO2—, —SO2NR7—, —SO2N10—, or -Het-;
- each CAP is, independently, thiazolidinedione, oxazolidinedione, -heteroaryl-C(═O)NR13R13, heteroaryl-W, —CN, —O—C(═S)NR13R13, -(Z)gR13, —CR10((Z)gR13)((Z)gR13), —C(═O)OAr, —C(═O)NR13Ar, imidazoline, tetrazole, tetrazole amide, —SO2NHR13, —SO2NH—C(R13R13)-(Z)g-R13, a cyclic sugar or oligosaccharide, a cyclic amino sugar, oligosaccharide, —CR10(—(CH2)m—R9)(—(CH2)m—R9), —N(—(CH2)m—R9)(—(CH2)m—R9), —NR13(—(CH2)m—CO2R13),
- each Ar is, independently, phenyl, substituted phenyl, wherein the substituents of the substituted phenyl are 1-3 substituents independently selected from the group consisting of OH, OCH3, NR13R13, Cl, F, and CH3, or heteroaryl;
- and
- each W is, independently, thiazolidinedione, oxazolidinedione, heteroaryl-C(═O)NR13R13, —CN, —O—C(═S)NR13R13, -(Z)gR13, —CR10((Z)gR13)((Z)gR13), —C(═O)OAr, —C(═O)NR13Ar, imidazoline, tetrazole, tetrazole amide, —SO2NHR13, —SO2NH—C(R13R13)-(Z)g-R13, a cyclic sugar or oligosaccharide, a cyclic amino sugar, oligosaccharide,
- with the proviso that when any —CHOR8— or —CH2OR8 groups are located 1,2- or 1,3- with respect to each other, the R8 groups may, optionally, be taken together to form a cyclic mono- or di-substituted 1,3-dioxane or 1,3-dioxolane.
38 more elements
A compound represented by the formula:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.