US 2006/0217412 A1Published application

Imidazo-fused oxazolo[4,5-b]pyridine and imidazo-fused thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same

OwnerWilliam Pitts, Makonen Belema +6inventors

InventorsWilliam Pitts, Makonen Belema, Patrice Gill, James Kempson, Yuping Qiu, Claude Quesnelle, Steven Spergel, Fred Zusi

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Abstract

The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.

Claims20

Dependent claims

A compound of formula (I),

enantiomers, diastereomers, salts, and solvates thereof wherein
X is selected from O or S;
R1 is selected from hydrogen, C1-3 alkyl, C2-3 alkenyl, and C2-3 alkynyl;
R2 is hydrogen, halo, cyano,
(b) alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkoxy, heterocyclooxy, aryloxy, heteroaryloxy, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1a, Z2a and Z3a;
or
(c) —OR10a, —SR10a, or —SO2R10a;
R3 and R4 are independently selected from
(a) hydrogen,
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b;
(c) —OR11, —NR12R13, —N(R12)C(O)R14, —N(R12)C(O)OR14, —N(R12)SO2R14, —N(R12)C(O)NR12aR13, or —N(R12)SO2NR12aR13 or —C(O)OR14, —C(O)R11, —C(O)NR12R13, —SO2R14, —SO2NR12R13;
(d) R3 and R4 together with the nitrogen atom to which they are attached combine to form a 3 to 8 membered heterocyclic ring optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b;
R6 is
(a) hydrogen, hydroxy, halo, or cyano,
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, heterocyclo, aryl, heteroaryl, (cycloalkyl)alkyl, (heterocyclo)alkyl, (aryl)alkyl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1d Z2d and Z3d;
or
(c) —OR7a, —SR7a, —NR8aR9a, —N(R8a)SO2R10, —N(R8a)SO2NR8bR9b, —N(R8a)SO2R10, —N(R8a)C(O)R7a, —N(R8a)N(R8a)C(O)R7a, —N(R8a)C(O)NR8bR9b, —N(R8a)C(O)OR7a, —SO2R10, —SO2NR8bR9b, —C(O)R7a, —C(O)OR7a, —OC(O)R7a, —C(O)NR8aR9a, or —OC(O)NR8aR9a;
R7a and R7b are independently
(a) hydrogen, or
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1c, Z2c and Z3c;
R8a, R8b, R9a and R9b are independently
(a) hydrogen,
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1d, Z2d and Z3d;
or
R10, R10a, at each occurance, are independently alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1d, Z2d and Z3d;
R11, R12, R12a and R13 are independently
(a) hydrogen, or
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1e, Z2e and Z3e;
R14 is alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1e, Z2e and Z3e;
Z1a-1e, Z2a-2e, and Z3a-3e are optional substituents at each occurrence independently selected from —W1—V1;
—W2—V2;
—W3—V3;
—W4—V4;
—W5—V5;
where W1-5 are independently
(1) a bond
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
or
where V1-5 are independently
(1) H
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
(3) —U1—O—Y5,
(4) —U1—S—Y5,
(5) —U1—C(O)t—H, —U1—(O)t—Y5 where t is 1 or 2,
(6) —U1—SO3—H, or —U1—S(O)tY5,
(7) —U1-halo,
(8) —U1-cyano,
(9) —U1-nitro,
(10) —U1—NY2Y3,
(11) —U1—N(Y4)—C(O)—Y1,
(12) —U1—N(Y4)—C(S)—Y1,
(13) —U1—N(Y4)—C(O)—NY2Y3,
(14) —U1—N(Y4)—C(S)—NY2Y3,
(15) —U1—N(Y4)—C(O)O—Y5,
(16) —U1—N(Y4)—S(O)2—Y1,
(17) —U1—N(Y4)—S(O)2—NY2Y3,
(18) —U1—C(O)—NY2Y3,
(19) —U1—OC(O)—NY2Y3
(20) —U1—S(O)2—N(Y4)—Y1,
(21) —U1—N(Y4)—C(═NV1a)—NY2Y3,
(22) —U1—N(Y4)—C(═NV1a)—Y1,
(23) —U1—C(═NV1a)—NY2Y3,
(24) oxo;
(25) —U1—Y5;
V1a is independently hydrogen, alkyl, —CN, —C(O)Y1, —S(O)2Y5, S(O)2NY2Y3;
Y1, Y2, Y3, Y4 and Y5
(1) are each independently hydrogen, alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl, any of which may be optionally independently substituted as valence allows with one or more Z4, Z5 and Z6;
or
(2) Y2 and Y3 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, or
(4) Y2 and Y3 together with the nitrogen atom to which they are attached may combine to form a group —N═CY6Y7 where Y6 and Y7 are each independently H or alkyl;
and
Z4, Z5, and Z6 are optional substituents at each occurrence independently selected from
(1) H
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
(3) —U1—O—Y5a,
(4) —U1—S—Y5a,
(5) —U1—C(O)t—H, —U1—C(O)t—Y5a where t is 1 or 2,
(6) —U1—SO3—H, or —U1—S(O)tY5a,
(7) —U1-halo,
(8) —U1-cyano,
(9) —U1-nitro,
(10) —U1—NY2aY3a,
(11) —U1—N(Y4a)—C(O)—Y1a,
(12) —U1—N(Y4a)—C(S)—Y1a,
(13) —U1—N(Y4a)—C(O)—NY2aY3a,
(14) —U1—N(Y4a)—C(S)—NY2aY3a,
(15) —U1—N(Y4a)—C(O)O—Y5a,
(16) —U1—N(Y4a)—S(O)2—Y1a,
(17) —U1—N(Y4a)—S(O)2—NY2aY3a,
(18) —U1—C(O)—NY2aY3a,
(19) —U1—C(O)—NY2aY3a
(20) —U1—S(O)2—N(Y4a)—Y1a,
(21) —U1—N(Y4a)—C(═NV1a)—NY2aY3a,
(22) —U1—N(Y4a)—C(═NV1a)—Y1a,
(23) —U1—C(═NV1a)—NY2aY3a,
(24) oxo;
(25) —U1—Y5a;
Y1a, Y2a, Y3a, Y4a and Y5a
(1) are each independently hydrogen, alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl;
U1 is independently
(1) a single bond,
(2) alkylene,
(3) alkenylene, or
(4) alkynylene.

101 more elements

A compound of formula (II),

enantiomers, diastereomers, salts, and solvates thereof wherein
R1 is selected from hydrogen, C1-3 alkyl, C2-3 alkenyl, and C2-3 alkynyl;
R2 is hydrogen, halo, cyano,
(b) alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkoxy, heterocyclooxy, aryloxy, heteroaryloxy, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1a, Z2a and Z3a;
or
(c) —OR10a, —SR10a, or —SO2R10a;
R5, at each occurrence, is independently selected from F, Cl, Br, and I;
R10a, at each occurance, are independently alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1d, Z2d and Z3d;
Z1a-1e, Z2a-2e, and Z3a-3e are optional substituents at each occurrence independently selected from —W1—V1;
—W2—V2;
—W3—V3;
—W4—V4;
—W5—V5;
where W1-5 are independently
(1) a bond
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
or
where V1-5 are independently
(1) H
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
(3) —U1—O—Y5,
(4) —U1—S—Y5,
(5) —U1—C(O)t—H, —U1—C(O)t—Y5 where t is 1 or 2,
(6) —U1—SO3—H, or —U1—S(O)tY5,
(7) —U1-halo,
(8) —U1-cyano,
(9) —U1-nitro,
(10) —U1—NY2Y3,
(11) —U1—N(Y4)—C(O)—Y1,
(12) —U1—N(Y4)—C(S)—Y1,
(13) —U1—N(Y4)—C(O)—NY2Y3,
(14) —U1—N(Y4)—C(S)—NY2Y3,
(15) —U1—N(Y4)—C(O)O—Y5,
(16) —U1—N(Y4)—S(O)2—Y1,
(17) —U1—N(Y4)—S(O)2—NY2Y3,
(18) —U1—C(O)—NY2Y3,
(19) —U1—OC(O)—NY2Y3
(20) —U1—S(O)2—N(Y4)—Y1,
(21) —U1—N(Y4)—C(═NV1a)—NY2Y3,
(22) —U1—N(Y4)—C(═NV1a)—Y1,
(23) —U1—C(═NV1a)—NY2Y3,
(24) oxo;
(25) —U1—Y5;
V1a is independently hydrogen, alkyl, —CN, —C(O)Y1, —S(O)2Y5, S(O)2NY2Y3;
Y1, Y2, Y3, Y4 and Y5
(1) are each independently hydrogen, alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl, any of which may be optionally independently substituted as valence allows with one or more Z4, Z5 and Z6;
or
(2) Y2 and Y3 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, or
(4) Y2 and Y3 together with the nitrogen atom to which they are attached may combine to form a group —N═CY6Y7 where Y6 and Y7 are each independently H or alkyl;
and
Z4, Z5, and Z6 are optional substituents at each occurrence independently selected from
(1) H
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
(3) —U1—OY5a,
(4) —U1—S—Y5a,
(5) —U1—C(O)t—H, —U1—C(O)t—Y5a where t is 1 or 2,
(6) —U1—SO3—H, or —U1—S(O)tY5a,
(7) —U1-halo,
(8) —U1-cyano,
(9) —U1-nitro,
(10) —U1—NY2aY3a,
(11) —U1—N(Y4a)—C(O)—Y1a,
(12) —U1—N(Y1a)—C(S)—Y1a,
(13) —U1—N(Y4a)—C(O)—NY2aY3a,
(14) —U1—N(Y4a)—C(S)—NY2aY3a,
(15) —U1—N(Y4a)—C(O)O—Y5a,
(16) —U1—N(Y4a)—S(O)2—Y1a,
(17) —U1—N(Y4a)—S(O)2—NY2aY3a,
(18) —U1—C(O)—NY2aY3a,
(19) U1—OC(O)—NY2aY3a
(20) —U1—S(O)2—N(Y4a)—Y1a,
(21) —U1—N(Y4a)—C(═NV1a)—NY2aY3a,
(22) —U1—N(Y4a)—C(═NV1a)—Y1a,
(23) —U1—C(═NV1a)—NY2aY3a,
(24) oxo;
(25) —U1—Y5a;
Y1a, Y2a, Y3a, Y4a and Y5a
(1) are each independently hydrogen, alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl;
U1 is independently
(1) a single bond,
(2) alkylene,
(3) alkenylene, or
(4) alkynylene.

80 more elements

Dependencies are inferred from the claim text.

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Abstract

A compound of formula (I),

enantiomers, diastereomers, salts, and solvates thereof wherein
X is selected from O or S;
R1 is selected from hydrogen, C1-3 alkyl, C2-3 alkenyl, and C2-3 alkynyl;
R2 is hydrogen, halo, cyano,
(b) alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkoxy, heterocyclooxy, aryloxy, heteroaryloxy, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1a, Z2a and Z3a;
or
(c) —OR10a, —SR10a, or —SO2R10a;
R3 and R4 are independently selected from
(a) hydrogen,
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b;
(c) —OR11, —NR12R13, —N(R12)C(O)R14, —N(R12)C(O)OR14, —N(R12)SO2R14, —N(R12)C(O)NR12aR13, or —N(R12)SO2NR12aR13 or —C(O)OR14, —C(O)R11, —C(O)NR12R13, —SO2R14, —SO2NR12R13;
(d) R3 and R4 together with the nitrogen atom to which they are attached combine to form a 3 to 8 membered heterocyclic ring optionally independently substituted as valence allows with one or more Z1b, Z2b and Z3b;
R6 is
(a) hydrogen, hydroxy, halo, or cyano,
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, heterocyclo, aryl, heteroaryl, (cycloalkyl)alkyl, (heterocyclo)alkyl, (aryl)alkyl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1d Z2d and Z3d;
or
(c) —OR7a, —SR7a, —NR8aR9a, —N(R8a)SO2R10, —N(R8a)SO2NR8bR9b, —N(R8a)SO2R10, —N(R8a)C(O)R7a, —N(R8a)N(R8a)C(O)R7a, —N(R8a)C(O)NR8bR9b, —N(R8a)C(O)OR7a, —SO2R10, —SO2NR8bR9b, —C(O)R7a, —C(O)OR7a, —OC(O)R7a, —C(O)NR8aR9a, or —OC(O)NR8aR9a;
R7a and R7b are independently
(a) hydrogen, or
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1c, Z2c and Z3c;
R8a, R8b, R9a and R9b are independently
(a) hydrogen,
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1d, Z2d and Z3d;
or
R10, R10a, at each occurance, are independently alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1d, Z2d and Z3d;
R11, R12, R12a and R13 are independently
(a) hydrogen, or
(b) alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1e, Z2e and Z3e;
R14 is alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl any of which may be optionally independently substituted as valence allows with one or more Z1e, Z2e and Z3e;
Z1a-1e, Z2a-2e, and Z3a-3e are optional substituents at each occurrence independently selected from —W1—V1;
—W2—V2;
—W3—V3;
—W4—V4;
—W5—V5;
where W1-5 are independently
(1) a bond
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
or
where V1-5 are independently
(1) H
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
(3) —U1—O—Y5,
(4) —U1—S—Y5,
(5) —U1—C(O)t—H, —U1—(O)t—Y5 where t is 1 or 2,
(6) —U1—SO3—H, or —U1—S(O)tY5,
(7) —U1-halo,
(8) —U1-cyano,
(9) —U1-nitro,
(10) —U1—NY2Y3,
(11) —U1—N(Y4)—C(O)—Y1,
(12) —U1—N(Y4)—C(S)—Y1,
(13) —U1—N(Y4)—C(O)—NY2Y3,
(14) —U1—N(Y4)—C(S)—NY2Y3,
(15) —U1—N(Y4)—C(O)O—Y5,
(16) —U1—N(Y4)—S(O)2—Y1,
(17) —U1—N(Y4)—S(O)2—NY2Y3,
(18) —U1—C(O)—NY2Y3,
(19) —U1—OC(O)—NY2Y3
(20) —U1—S(O)2—N(Y4)—Y1,
(21) —U1—N(Y4)—C(═NV1a)—NY2Y3,
(22) —U1—N(Y4)—C(═NV1a)—Y1,
(23) —U1—C(═NV1a)—NY2Y3,
(24) oxo;
(25) —U1—Y5;
V1a is independently hydrogen, alkyl, —CN, —C(O)Y1, —S(O)2Y5, S(O)2NY2Y3;
Y1, Y2, Y3, Y4 and Y5
(1) are each independently hydrogen, alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl, any of which may be optionally independently substituted as valence allows with one or more Z4, Z5 and Z6;
or
(2) Y2 and Y3 may together be alkylene or alkenylene, completing a 3- to 8-membered saturated or unsaturated ring together with the atoms to which they are attached, or
(4) Y2 and Y3 together with the nitrogen atom to which they are attached may combine to form a group —N═CY6Y7 where Y6 and Y7 are each independently H or alkyl;
and
Z4, Z5, and Z6 are optional substituents at each occurrence independently selected from
(1) H
(2) alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, or (heteroaryl)alkyl;
(3) —U1—O—Y5a,
(4) —U1—S—Y5a,
(5) —U1—C(O)t—H, —U1—C(O)t—Y5a where t is 1 or 2,
(6) —U1—SO3—H, or —U1—S(O)tY5a,
(7) —U1-halo,
(8) —U1-cyano,
(9) —U1-nitro,
(10) —U1—NY2aY3a,
(11) —U1—N(Y4a)—C(O)—Y1a,
(12) —U1—N(Y4a)—C(S)—Y1a,
(13) —U1—N(Y4a)—C(O)—NY2aY3a,
(14) —U1—N(Y4a)—C(S)—NY2aY3a,
(15) —U1—N(Y4a)—C(O)O—Y5a,
(16) —U1—N(Y4a)—S(O)2—Y1a,
(17) —U1—N(Y4a)—S(O)2—NY2aY3a,
(18) —U1—C(O)—NY2aY3a,
(19) —U1—C(O)—NY2aY3a
(20) —U1—S(O)2—N(Y4a)—Y1a,
(21) —U1—N(Y4a)—C(═NV1a)—NY2aY3a,
(22) —U1—N(Y4a)—C(═NV1a)—Y1a,
(23) —U1—C(═NV1a)—NY2aY3a,
(24) oxo;
(25) —U1—Y5a;
Y1a, Y2a, Y3a, Y4a and Y5a
(1) are each independently hydrogen, alkyl, (hydroxy)alkyl, (alkoxy)alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, cycloalkenyl, (cycloalkenyl)alkyl, aryl, (aryl)alkyl, heterocyclo, (heterocylco)alkyl, heteroaryl, or (heteroaryl)alkyl;
U1 is independently
(1) a single bond,
(2) alkylene,
(3) alkenylene, or
(4) alkynylene.

101 more elements