WO2006133417A1 - Phenylamino isothiazole carboxamidines comme inhibiteurs de mek - Google Patents

Phenylamino isothiazole carboxamidines comme inhibiteurs de mek Download PDF

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WO2006133417A1
WO2006133417A1 PCT/US2006/022491 US2006022491W WO2006133417A1 WO 2006133417 A1 WO2006133417 A1 WO 2006133417A1 US 2006022491 W US2006022491 W US 2006022491W WO 2006133417 A1 WO2006133417 A1 WO 2006133417A1
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methyl
alkyl
compound
formula
specific embodiment
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PCT/US2006/022491
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Hassan El Abdellaoui
Robert Tam
Varaprasad Chamakura
Stanley Lang
Zhi Hong
Dinesh Barawkar
Andreas Maderna
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Valeant Pharmaceuticals International
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
    • C07D275/03—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Definitions

  • the invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted- 3-hydroxy-5-aryl- isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.
  • Oncogenes genes that contribute to the production of cancers ⁇ are generally mutated forms of certain normal cellular genes ("proto-oncogenes"). Oncogenes often encode abnormal versions of signal pathway components, such as receptor tyrosine kinases, serine-threonine kinases, or downstream signaling molecules.
  • the central downstream signaling molecules are the Ras proteins, which are anchored on the inner surfaces of cytoplasmic membranes, and which hydrolyze bound guanosine triphosphate (GTP) to guanosine diphosphate (GDP).
  • GTP guanosine triphosphate
  • GDP guanosine diphosphate
  • Ras alternates between an active "on” state with a bound GTP (hereafter “Ras.GTP”) and an inactive "off state with a bound GDP.
  • the active "on” state, Ras.GTP binds to and activates proteins that control the growth and differentiation of cells.
  • Ras.GTP leads to the activation of a cascade of serine/threonine kinases.
  • MAP kinase mitogen- «ctivated/?rotein kinase
  • Ras.GTP leads to the activation of a cascade of serine/threonine kinases.
  • One of several groups of kinases known to require a Ras.GTP for their own activation is the Raf family.
  • the Raf proteins activate "MEKl” and "MEK2,” abbreviations for /nitogen-activated £RK- activating kinases (where ERK is extracellular signal-regulated protein kinase, another designation for MAPK).
  • MEKl and MEK2 are dual-function serine/threonine and tyrosine protein kinases and are also known as MAP kinase kinases.
  • Ras.GTP activates Raf, which activates MEKl and MEK2, which activate MAP kinase (MAPK).
  • MAPK MAP kinase
  • Blockade of downstream Ras signaling as by use of a dominant negative Raf-1 protein, can completely inhibit mitogenesis, whether induced from cell surface receptors or from oncogenic Ras mutants.
  • Raf and Ras are key regulatory steps in the control of cell proliferation.
  • no substrates of MEK other than MAPK have been identified; however, recent reports indicate that MEK may also be activated by other upstream signal proteins such as MEK kinase or MEKKl and PKC.
  • Activated MAPK translocates and accumulates in the nucleus, where it can phosphorylate and activate transcription factors such as EIk-I and Sapla, leading to the enhanced expression of genes such as that for c-fos.
  • Raf and other kinases phosphorylate MEK on two neighboring serine residues, S and S in the case of MEK-I . These phosphorylations are required for activation of MEK as a kinase.
  • MEK phosphorylates MAP kinase on two residues separated by a single amino acid: a tyrosine, Y 185 , and a threonine, T 183 .
  • MEK appears to associate strongly with MAP kinase prior to phosphorylating it, suggesting that phosphorylation of MAP kinase by MEK may require a prior strong interaction between the two proteins.
  • MEK' s mechanism of action may differ sufficiently from the mechanisms of other protein kinases as to allow for selective inhibitors of MEK. Possibly, such inhibitors would operate through allosteric mechanisms rather than through the more usual mechanism involving blockage of an ATP binding site.
  • MEKl and MEK2 are, therefore, validated and accepted targets for anti-proliferative therapies, even when the oncogenic mutation does not affect MEK structure or expression. See, e.g., U.S. Patent Publications 2003/0149015 by Barrett et al. and 2004/0029898 by Boyle et al.
  • This invention provides a compound of formula I
  • dotted line represents an optional double bond, the five-membered ring is fused to Ar 1 , and R x is selected from substituents listed above for R 3 ;
  • R x where the five-membered ring is fused to Ar 1 , and R x is selected from substituents listed above for R 3 ;
  • Ar 2 is phenyl, pyridyl, pyrimidyl, pyridazinyl, or triazinyl, where ring carbon atoms are optionally substituted with substituents R 4 -R 6 , where R 4 is defined as for Ri-R 3 above;
  • R5 and R 6 are, independently, H, F, Cl, Br, CH 3 , or CF 3 ; and in which all alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, and heteroaryl groups in R 1 -R 9 are optionally substituted with one, two, or three groups selected from F, Cl, Br, I, OH, CN, Ci-C 4 alkyl, Ci-C 4 alkoxyl, and C 2 -C 4 alkenyl; which are selected independently from H, F, Cl, Br, CH 3 , or CF 3 ;
  • R v is selected from substituents listed above for R 3
  • R 1 is OH; 0-C)-C 6 alkyl; Ci-C 6 alkyl, said Ci-C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci -C 3 alkoxy, and phenyl; -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C7-C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -Cg bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyL piperidinyl, N- morpholyl, tetrahydrofuryl, and naphthyl groups are optionally substituted with one to three groups selected independently from hydroxy, halogen
  • R' is (CH 2 )[ I -G, where n is 1 or 2 and G is a five- or six-membered ring or a 9 - 14- membered fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and Cj-C 4 alkyl, wherein said Ci-C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds;
  • R' is -CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl.
  • this invention provides a compound of formula I where Ar 1 and Ar 2 are both 6-membered rings.
  • this invention provides a compound of formula I in which A is S, CH 2 , N 2 , CO, C(O)CH 2 , or NHC(O).
  • this invention provides a compound of formula I, in which A is O, C(O), or CH 2 C(O).
  • this invention provides a compound of formula I where R' is OH; 0-Ci-C 6 alkyl; Cj-Cg alkyl, said Ci-C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, C]-C 3 alkoxy, and phenyl, said phenyl group or groups optionally substituted with one to three groups selected independently from hydroxy, halogen, and methyl.
  • this invention provides a compound of formula I where R 1 is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -Cg bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl groups are optionally substituted with one to three groups selected independently from hydroxy, halogen, and methyl.
  • this invention provides a compound of formula I where R 1 is (CH 2 ) n -G, where n is 1 or 2 and G is a five- or six-membered ring or a 9 - 14- membered fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and Cj -C 4 alkyl, wherein said Cj-C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds.
  • this invention provides a compound of formula I where R 1 is CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl.
  • this invention provides a compound of formula II
  • A is -0-, -CH 2 -, -N 2 -, -CH 2 C(O)-, C(O)CH 2 , -S-, or -C(O)-;
  • Ri, R 2 , and R 3 are, independently, hydrogen; halogen; hydroxy; nitro; cyano; C]-C 4 alkyl, optionally substituted with one to three fluorine atoms; CH 3 O; 2-methoxy ethenyl; (CH 3 ) 2 N; CH 3 OC(O); CH 3 CH 2 OC(O); NR 7 Rs 1 -C(O)NR 7 R 8 ; Or-S(O) 2 NR 7 R 8 , where R 7 and R 8 are, independently, H, CH 3 , or CH 3 CH 2 ; or Ri and R 2 are attached to adjacent carbons and, together with the ring atoms to which they are attached, form an additional, fused, five- or six-membered ring, optionally containing one heteroatom, which ring may be aromatic or aliphatic;
  • R 4 -R 6 are, independently, H, F, Cl, Br, CH 3 , or CF 3 ;
  • R* is H, except when Ri and R 2 are both F; when Ri and R 2 are both F, R* is either H or Cl;
  • R' is OH; O-Ci-Cg alkyl; Ci-C 6 alkyl, said Cj-C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci-C 3 alkoxy, and phenyl; - CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -Cg bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -C 9 bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N- morpholyl
  • R' is (CH 2 ) n -G, where n is 1 or 2 and G is a five- or six-membered ring or a 9 - 14- membered fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and Cj-C 4 alkyl, wherein said Ci-C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds;
  • R' is -CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl.
  • this invention provides a compound of formula II in which A is O.
  • this invention provides a compound of formula II in which A is O and R' is -CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl.
  • this invention provides a compound of formula II in which A is O and R' is (CH 2 ) n -G, where n is 1 or 2 and G is a five- or six-membered ring or a 9 - 14- membered fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and Cj -C 4 alkyl, wherein said Ci-C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds.
  • this invention provides a compound of formula II in which A is O and R' is OH; 0-C]-C 6 alkyl; C 1 -C 6 alkyl, said C 1 -C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci-C 3 alkoxy, and phenyl; -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -Cg bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphth
  • this invention provides a compound of formula II in which A is-O-, Ri is 2-C(O)G, where G is selected from: -OJ, where J is isopropyl, cyclopropyl, cyclopentyl, dimethylamino, or methoxyethyl; and -NHJ' where J' is methyl, ethyl, isopropyl, cyclopropyl, dimethylaminomethyl, or 3-methyl- 2-yl-butanoic acid methyl ester and -N(CH 3 )?; or N-methyl piperazinyl; R 2 and R 3 are H; and R 4 is isopropyl or 1-hydroxy-isopropyl.
  • this invention provides a compound of formula II in which A is O; R 1 is -CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl; Ri is H; R 2 is 2-Cl, 2-Me, 2-CF 3 , 3-F, 3-
  • R 3 is hydrogen; halogen; hydroxy; nitro; cyano; Ci-C 4 alkyl, optionally substituted with one to three fluorine atoms;
  • this invention provides a compound of formula II in which A is O; R' is -CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl; Ri is 2-Me, 2-F, or 2-Cl; R 2 is 3-Me, 3- F, 3 -Cl, 5-Me, 5-F, 5-Cl or 3-CF 3 ; and R 3 is hydrogen; halogen; hydroxy; nitro; cyano; Cj-C 4 alkyl, optionally substituted with one to three fluorine atoms; CH 3 O; 2-methoxy ethenyl; (CH 3 ) 2 N; CH 3 OC(O); CH 3 CH 2 OC(O); NR 7 R 81 -C(O)NR 7 R 8 ; or -S(O) 2 NR 7 R 8 , where R
  • this invention provides a compound of formula II in which A is O; R' is -CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl; R t is 5-Cl; R 2 is -C(O)NR 7 R 8 , or- S(O) 2 NR 7 Rg, and R 3 is hydrogen; halogen; hydroxy; nitro; cyano; Cj -C 4 alkyl, optionally substituted with one to three fluorine atoms; CH 3 O; 2-methoxy ethenyl; (CH 3 ) 2 N; CH 3 OC(O); CH 3 CH 2 OC(O); NR 7 R 81 -C(O)NR 7 R 8 ; Or-S(O) 2 NR 7 R 8 , where R 7 and R 8 are, independently, H 5
  • this invention provides a compound of formula II in which A is O and R' is (CH 2 ) n -G; Ri is H; R 2 is 2-Cl 5 2-Me, 2-CF 3 , 3-F, 3-Me 5 3-N(CH 3 ) 2 ; 3- C(O)OEt 5 3- C(O)OMe, 4-Cl, or 4-OH; and R 3 is hydrogen; halogen; hydroxy; nitro; cyano; Ci -C 4 alkyl, optionally substituted with one to three fluorine atoms; CH 3 O; 2-methoxy ethenyl; (CH 3 ) 2 N; CH 3 OC(O); CH 3 CH 2 OC(O); NR 7 R 81 -C(O)NR 7 R 8 ; Or -S(O) 2 NR 7 R 8 , where R 7 and R 8 are, independently, H 5 CH 3 , or CH 3 CH 2 .
  • this invention provides a compound of formula II in which A is O and R 1 is (CH 2 ) R -G, where n is 1 or 2 and G is a five- or six-membered ring or a 9- to 14- membered fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and C 1 -C 4 alkyl, wherein said Ci -C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds; Ri is 2-Me, 2-F, or 2-Cl; R 2 is 3-Me, 3-F, 3-Cl, 5-Me, 5-F, 5-Cl or 3-CF 3 ; and R 3 is hydrogen; halogen; hydroxy; nitro; cyano; Ci-C 4 alkyl
  • this invention provides a compound of formula II in which A is O, R' is (CH 2 ) n -G; Ri is 5-Cl; R 2 is -C(O)NR 7 R 8 , or -S(O) 2 NR 7 R 8 ; and R 3 is hydrogen; halogen; hydroxy; nitro; cyano; C 1 -C 4 alkyl, optionally substituted with one to three fluorine atoms; CH 3 O; 2-methoxy ethenyl; (CH 3 ) 2 N; CH 3 OC(O); CH 3 CH 2 OC(O); NR 7 R 8 ,-
  • this invention provides a compound of formula II in which A is-O-, R' is OH; 0-C]-C 6 alkyl; or Ci-C 6 alkyl, said Cj-Cg alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Cj-C 3 alkoxy, and phenyl; R 1 is H; R 2 is 2-Cl, 2-Me, 2-CF 3 , 3-F, 3-Me, 3-N(CH 3 ) 2 ; 3- C(O)OEt, 3- C(O)OMe, 4-Cl, or 4-OH; and R 3 is hydrogen; halogen; hydroxy; nitro; cyano; Cj-C 4 alkyl, optionally substituted with one to three fluorine atoms; CH 3 O; 2-methoxy eth
  • this invention provides a compound of formula II in which A is-O-, R 1 is OH; 0-Ci-C 6 alkyl; or Ci-C 6 alkyl, said Ci-C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci-C 3 alkoxy, and phenyl; R t is 2-Me, 2-F, or 2-Cl; R 2 is 3-Me, 3-F, 3-Cl, 5-Me, 5-F, 5-Cl or 3-CF 3 ; and R 3 is hydrogen; halogen; hydroxy; nitro; cyano; C] -C 4 alkyl, optionally substituted with one to three fluorine atoms; CH 3 O; 2-methoxy ethenyl; (CH 3 ) 2 N; CH 3 OC(O); CH 3 CH 2 OC(O); NR 7 R 8 ,-C(O)NR 7 R 8 ; or -S(O) 2 NR 7 R 8 , where R 7
  • this invention provides a compound of formula II in which A is -0-, R 1 is OH; 0-Ci-C 6 alkyl; or Ci-Ce alkyl, said Ci-C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci-C 3 alkoxy, and phenyl; Ri is 5-Cl; R 2 is -C(O)NR 7 R 8 , or -S(O) 2 NR 7 R 8 ; and R 3 is hydrogen; halogen; hydroxy; nitro; cyano; Cj-C 4 alkyl, optionally substituted with one to three fluorine atoms; CH 3 O; 2-methoxy ethenyl; (CH 3 ) 2 N; CH 3 OC(O); CH 3 CH 2 OC(O); NR 7 R 8 ,- C(O)NR 7 R 8 ; or -S(O) 2 NR 7 R 8 , where R 7 and R 3 are, independently, H, CH 3
  • this invention provides a compound of formula II in which A is -0-, R' is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; Q-C 9 bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl groups are optionally substituted with one to three groups selected independently from hydroxy, halogen, and methyl; Rj is H; R 2 is 2-Cl, 2-Me, 2-CF 3 , 3-F, 3-Me, 3-N(CH 3 ) 2 ; 3- C(
  • this invention provides a compound of formula II in which A is -O- R 1 is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morphoIyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -C 9 bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl groups are optionally substituted with one to three groups selected independently from hydroxy, halogen, and methyl; Ri is 2- Me, 2-F, or 2-Cl; R 2 is 3-Me, 3-F, 3-Cl, 5-Me, 5-F, 5-Cl or
  • this invention provides a compound of formula II II in which A is -O- R' is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N ⁇ morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -C 9 bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl groups are optionally substituted with one to three groups selected independently from hydroxy, halogen, and methyl; Ri is 5- Cl; R 2 is -C(O)NR 7 Rg, or -S(O) 2 NR 7 R 8 ; and R 3 is
  • this invention provides a compound of formula III
  • this invention provides a compound of formula III in which A is -O-.
  • this invention provides a compound of formula III in which A is C(O), -CH 2 -, or C(O)CH 2 .
  • this invention provides a compound of formula III in which A is -0-, and R' is Cj-C 6 alkyl or C 3-6 cycloalkyl, all such Ci-C 6 alkyl and C 3- 6 cycloalkyl optionally substituted with one to three OH groups.
  • this invention provides a compound of formula III in which A is -O-; and R' is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-6 cycloalkyl, phenyl, pyridyl, piperazin-1-yl, piperidin-1-yl, N-morpholyl, tetrahydrofuryl, and naphthyl.
  • this invention provides a compound of formula III in which A is -0-; and R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl.
  • this invention provides a compound of formula III in which A is -O-; R 1 is Ci-C 6 alkyl or C 3-6 cycloalkyl, all such Ci-C 6 alkyl and C 3-6 cycloalkyl optionally substituted with one to three OH groups; and R 4 is H, CH 3 , or CF 3 .
  • this invention provides a compound of formula III in which A is -0-; R 1 is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-6 cycloalkyl, phenyl, pyridyl, piperazin-1-yl, piperidin-1-yl, N-morpholyl, tetrahydrofuryl, and naphthyl; and R 4 is H, CH 3 , or CF 3 .
  • this invention provides a compound of formula III in which A is -O-; R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl; and R 4 is H, CH 3 , or CF 3 .
  • this invention provides a compound of formula III in which A is -O-; R' is C]-C 6 alkyl or C 3-6 cycloalkyl, all such Ci-C 6 alkyl and C 3-6 cycloalkyl optionally substituted with one to three OH groups; and R 4 is F, Cl, or Br.
  • this invention provides a compound of formula III in which A is -0-; R' is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-6 cycloalkyl, phenyl, pyridyl, piperazin-1-yl, piperidin-1-yl, N-morpholyl, tetrahydrofuryl, and naphthyl; and R 4 is F 5 Cl, or Br.
  • this invention provides a compound of formula III in which A is -O-; R is 2-propyl, l-hydroxy-2 -propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl; and R 4 is F, Cl, or Br.
  • this invention provides a compound of formula III in which A is-O-; R' is C]-C 6 alkyl or C 3-6 cycloalkyl, all such Ci-C 6 alkyl and C 3-6 cycloalkyl optionally substituted with one to three OH groups; R 4 is H, CH 3 , or CF 3 ; and R 5 is F.
  • this invention provides a compound of formula III in which A is-O-; R 1 is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-6 cycloalkyl, phenyl, pyridyl, pi ⁇ erazin-1-yl, piperidin-1-yl, N-morpholyl, tetrahydrofuryl, and naphthyl; R 4 is H, CH 3 , or CF 3 ; and R 5 is F.
  • this invention provides a compound of formula III in which A is-O-; R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl; R 4 is H, CH 3 , or CF 3 ; and R 5 is F.
  • this invention provides a compound of formula III in which A is-O-; R' is Ci-C 6 alkyl or C 3-6 cycloalkyl, all such Ci-C 6 alkyl and C 3-6 cycloalkyl optionally substituted with one to three OH groups; R 4 is F, Cl, or Br; and R 5 is F.
  • this invention provides a compound of formula III in which A is-O-; R' is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-6 cycloalkyl, phenyl, pyridyl, piperazin-1-yl, piperidin-1-yl, N-morpholyl, tetrahydrofuryl, and naphthyl; R 4 is F, Cl, or Br; and R 5 is F.
  • this invention provides a compound of formula III in which A is-O-; R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl; R 4 is F, Cl, or Br; and R 5 is F.
  • this invention provides a compound of formula III in which A is-O-, R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl, R 1 is H, and R 2 is selected from 2-Cl, 2-Me, 2-CF 3 , 3-F, 3-Me, 3-N(CH 3 ) 2 ; 3- C(O)OEt, 3- C(O)OMe, 4-Cl, and 4-OH.
  • this invention provides a compound of formula III in which A is-O-, R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl, R, is H, and R 2 is 2-Cl, 2-Me, 2-CF 3 , 3-F, 3-Me, 3-N(CH 3 ) 2 , 3- C(O)OEt, 3- C(O)OMe, 4-Cl, or 4-OH.
  • this invention provides a compound of formula III in which A is-O-, R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl, R, is 2-Me, 2-F, or 2-Cl; and R 2 is 3-Me, 3-F, 3-Cl, 5-Me, 5-F, 5-Cl or 3- CF 3 .
  • this invention provides a compound of formula III in which A is-O-, R 1 is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl, Ri is 5-Cl; and R 2 is -C(O)NR 7 R 8 , Or-S(O) 2 NR 7 R 8 .
  • this invention provides a compound of formula III in which A is-O-, R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl, R] is 2-Me, 2-F, or 2-Cl and R 2 is 4-F, 4-Cl, 4-1, 4-CF 3 .
  • this invention provides a compound of formula III in which A is-O-, R' is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl, Ri is 3-Me or 3-F and R 2 is 5-F, 5-Me or 5-CF 3 .
  • this invention provides a compound of formula III in which A is-O-, R 1 is 2-propyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 3-hydroxypropyl, or 2,3- dihydroxypropyl, R i;2 are 2-Cl and 5-Cl, Rj 1 S are 2-F and 5-F, and R 6 is H.
  • this invention provides a compound of formula III in which A is O; R' is -CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl; Ri is 2-Me, 2-F, or 2-Cl; and R 2 is 3-Me, 3-F, 3-Cl, 5-Me, 5-F, 5-Cl or 3-CF 3 .
  • this invention provides a compound of formula III in which A is O; R' is -CH(CH 2 OH)CH 2 D, where D is selected from imidazolyl, indolyl, carboxamido, phenyl, cyclohexyl, -CH 2 SCH 3 , and adamantin-1-yl; Ri is 5-Cl; and R 2 is -C(O)NR 7 R 8 , or - S(O) 2 NR 7 R 8 ,
  • this invention provides a compound of formula III in which A is O; R' is (CH 2 ) n -G, where n is 1 or 2 and G is a five- or six-membered ring or a 9 - 14- membered fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and Ci-C 4 alkyl, wherein said Ci-C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds; Ri is H; and R 2 is 2-Cl, 2- Me, 2-CF 3 , 3-F, 3-Me, 3-N(CH 3 ) 2 ; 3- C(O)OEt, 3- C(O)OMe, 4-Cl, or 4-OH.
  • this invention provides a compound of formula III in which A is O and R' is (CH 2 ) n -G, where n is 1 or 2 and G is a five- or six-membered ring or a 9 - 14- membered fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and Cj-C 4 alkyl, wherein said Ci-C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds; Ri is 2-Me, 2-F, or 2-Cl; and R 2 is 3-Me, 3-F, 3-Cl, 5-Me, 5-F, 5-Cl or 3-CF 3 .
  • this invention provides a compound of formula III in which A is O, R 1 is (CHo) n -G, where n is 1 or 2 and G is a five- or six-membered ring or a 9 - 14- membered fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and Ci-C 4 alkyl, wherein said Ci-C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds; Ri is 5-Cl; and R 2 is - C(O)NR 7 R 85 Or-S(O) 2 NR 7 R 8 , In another embodiment, this invention provides a compound of formula III in which A is-O-, R' is OH; 0-C 1 -C 6 alkyl; or
  • this invention provides a compound of formula III in which A is-O-, R' is OH; 0-Cj-C 6 alkyl; or Ci-C 6 alkyl, said Ci-C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci-C 3 alkoxy, and phenyl; Ri is 2-Me, 2-F, or 2-Cl; and R 2 is 3-Me, 3-F, 3-Cl, 5-Me, 5-F, 5-Cl or 3-CF 3 .
  • this invention provides a compound of formula III in which A is-O-, R 1 is OH; 0-Ci-C 6 alkyl; or Ci-C 6 alkyl, said Cj-C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci-C 3 alkoxy, and phenyl; Ri is 5-Cl; and R 2 is -C(O)NR 7 R 8 , or -S(O) 2 NR 7 R 8 .
  • this invention provides a compound of formula III in which A is-O-, R' is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -Cg bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl groups are optionally substituted with one to three groups selected independently from hydroxy, halogen, and methyl; Ri is H; and R 2 is 2-Cl, 2-Me, 2-CF 3 , 3-F, 3-Me, 3-N(CH 3 ) 2 ; 3-
  • this invention provides a compound of formula III in which A is-O-, R' is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -C 9 bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl groups are optionally substituted with one to three groups selected independently from hydroxy, halogen, and methyl; Rj is 2- Me, 2-F, or 2-Cl; and R 2 is 3-Me, 3-F, 3-Cl, 5-Me, 5-F, 5-Cl
  • this invention provides a compound of formula III in which A is-O-, R' is -CH 2 B or -CH 2 CH 2 B, where B is selected from C 3-7 cycloalkyl, C 7 -C 9 bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-morpholyl, tetrahydrofuryl, and naphthyl; C 3 -C 7 cycloalkyl; C 7 -C 9 bicycloalkyl, where all cycloalkyl, bicycloalkyl, pyridyl, piperazinyl, piperidinyl, N-moipholyl, tetrahydrofuryl, and naphthyl groups are optionally substituted with one to three groups selected independently from hydroxy, halogen, and methyl; Ri is 5- Cl; and R 2 is -C(O)NR 7 R 8 , Or-S(O) 2 NR 7 R 8
  • this invention provides a compound of formula IV
  • U, V, W, X, Y, and Z are, independently CH or N, provided that U, V, W, X, Y, and Z are not all CH;
  • A is -O-, -CH 2 -, -N 2 -, -NHC(O)-, -CH 2 C(O)-, -C(O)CH 2 -, -S-, or -C(O)-;
  • Ri and R 2 are, independently, hydrogen; halogen; hydroxy; cyano; CH 3 , optionally substituted with 1-3 fluorine atoms; CH 3 O; (CH 3 ) 2 N; CH 3 OC(O); 2-methoxy ethenyl; and CH 3 CH 2 OC(O); and
  • R' is OH; OCi-C 6 alkyl; Cj -C 6 alkyl, optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci-C 3 alkoxy, and phenyl; -
  • this invention provides a compound of formula IV, in which A is-O-, -CH 2 -, -NHC(O)-, -S-, or -C(O)-.
  • this invention provides a compound of formula V
  • U and X are, independently CH or N, provided that U and X are not both CH; Ri and R 2 are, independently, hydrogen; halogen; hydroxy; cyano; CH 3; optionally substituted with 1-3 fluorine atoms; CH 3 O; (CH 3 ) 2 N; CH 3 OC(O); 2-methoxy ethenyl; and CH 3 CH 2 OC(O); and R' is selected from Ci-Ce alkyl, optionally substituted with 1 - 3 hydroxyl groups; cyclopropyl; -CH 2 B; and -CH 2 CH 2 B, where B is selected from C 3-6 cycloalkyl, phenyl, pyridyl, piperzin-1-yl, piperidin-1-yl, N- morpholyl, tetrahydrofuryl, and naphthyl.
  • this invention provides a compound of formula VI
  • Y is -NH-, -S- or -O-, and Ri-R' are defined as for formula II.
  • this invention provides a compound of formula Via, where Y is -NH-, -S- or -0-,
  • this invention provides a compound of formula Via where Y is -S- or-O-, and R' is selected from 1-hydroxy-isopropyl, 2-hydroxy->2-propyl, 2-hydroxy- ethyl, and 2,3,-dihydroxy- «-propyl.
  • this invention provides a compound of formula VII
  • T - Z represent N, CH, or CRi, 2> or 4, provided that at most two of W, X, Y, and Z and at most 2 of T, U, and V are N;
  • Ri - R 4 are defined as for formula I; and where R' is OH; O-Cj-C ⁇ alkyl; Ci-C 6 alkyl, said Ci-C 6 alkyl groups optionally substituted with one to three groups selected independently from hydroxy, halogen, Ci-C 3 alkoxy, and phenyl; or R' is -(CH 2 ) n -B where n is 1 or 2 and B is defined as above.
  • this invention provides a compound of formula Vila,
  • this invention provides a compound of formula
  • R 3 and R 4 are both H and R' is Ci-C 6 alkyl or O-Ci-Ce alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula Vila, where R 2 - R 4 are H and R 1 is C]-Ce alkyl, optionally substituted with halogen, C 1 -C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula Vila, where R 2 - R 4 are H and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl, 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpi ⁇ erazin- 2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpho
  • this invention provides a compound of formula VIIA in which Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl; R 2 , R 3 , and R 4 are H, R 1 is - (CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, pyrimidyl, pyrrol
  • this invention contemplates the compound of formula VIIA in which Rj is 2-fluoro, -chloro, -bromo, -methyl, -trifluoromethyl, -methoxy, or -hydroxy; R 2 , R 3 , and R 4 are H; and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, mo ⁇ holyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula VIIA in which Ri is 3-fluoro, -chloro, -bromo, -methyl, -trifluoromethyl, -methoxy, or -hydroxy; R 2 , R 3 , and R 4 are H; and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula VIIA in which Ri is 4-fluoro, -chloro, -bromo, -methyl, -trifluoromethyl, -methoxy, or -hydroxy; R 2 , R 3 , and R 4 are H; and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, mo ⁇ holyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula VIIA in which R] is 5-fluoro, -chloro, -bromo, -methyl, -trifluoromethyl, -methoxy, or -hydroxy; R 2 , R 3 , and R 4 are H; and R is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, mo ⁇ holyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula VIIA-I, where Ri-R' are defined as for formula A.
  • this invention provides a compound of formula VIIA- 1 where Ri - R 4 are H and R' is isopropyl, 2-butyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula VII, in which at least one of T, U, V, W, X, Y, and Z is N.
  • this invention provides a compound of formula VII, in which at least one of W, X, Y, and Z is N.
  • this invention provides a compound of formula VII, in which at least one of T, U, and V is N.
  • this invention provides a compound of formula VII, in which two of W, X, Y, and Z are N.
  • this invention provides a compound of formula VII, in which one of T, U, and V and one of W, X, Y, and Z are N.
  • this invention provides a compound of formula VIIB
  • this invention provides a compound of formula VIIB-I
  • this invention provides a compound of formula VIIB-
  • Rj-R 4 are, independently, H, C 1 -C 3 alkyl, or halogen
  • R 1 is -(CH 2 ) n -B, where n is 1 or 2
  • B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula VIIB-I, where Ri-R 4 are H and R 1 is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy- 1 -propyl, or 3 ,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula VIIB-I where one of Ri and R 2 is H and the other is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 3 - R 4 are H, and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula
  • Ri and R 2 are H and the other is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl
  • R 3 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula VIIB-I, where Ri and R 2 are fused cyclohexyl or fused cyclopentyl, R 3 and R 4 are H, and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l -propyl, or 3,4-dihydroxy-2- butyl.
  • this invention provides a compound of formula VIIB-I, where Ri and R 2 are benzo, R 3 and R 4 are H, and R' is isopropyl, 2-(2-furyl)ethyl, 2- hydroxyethyl, 2,3-dihydroxy-l -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula VIIB-I, wherein Ri and R 2 are halogen, R 3 and R 4 are H, and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula VIIB-
  • Ri - R 3 are H
  • R 4 is 2-halo, 2-cyano, 2-hydroxy, or 2-methoxy
  • R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula VIIB-I, where Ri is halo, R 2 - R 4 are H and R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • the invention contemplates a compound of formula VIIB-I, where Ri is bromo, R 2 - R 4 are H and R 1 is isopropyl, 2-hydroxyethyl, 1- hydroxy-2-propyl, or 2,3 -dihydroxy-1 -propyl.
  • this invention provides a compound of formula VIIB-2
  • this invention provides a compound of formula VIIB- 2, where Ri-R 4 are, independently, H, Q-C 3 alkyl, or halogen, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula VIIB-2, wherein Ri and R 2 are halogen, R 3 and R 4 are H, and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3 -dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • the invention contemplates a compound of formula VIIB-2, where Rj is bromo, R 2 - R 4 are H and R' is 2-cyclopropyl ethyl, 2- hydroxyethyl, l-hydroxy-2-propyl, or 2,3-dihydroxy-l -propyl.
  • the invention contemplates a compound of formula VIIB-2, where Ri and R 2 are fused (2,3) pyrido, R 4 is 2-chloroethyl, and R' is 2- cyclopropyl ethyl, 2-hydroxyethyl, or 2-cyclopenylethyl.
  • the invention contemplates a compound of formula VIIB-2, where Ri and R 2 are fused (2,3) pyrrolo, fused (2,3) furyl, or fused (4,5) imidazolo, R 4 is H, and R' is 2-hydroxyethyl, or isopropyl.
  • the invention provides compounds according to any of formulas VIIB-3 to VIIB-37, wherein Ri-R 4 are all independently methyl, methoxy, ethyl, vinyl, ethynyl, halo, or H, and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl, cyclohexyl, or cyclohex
  • the invention provides compounds according to any of formulas VIIB-3 to VIIB-37, wherein Ri -R 4 are all independently halo, halomethyl, or H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is phenyl, pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • the invention provides compounds according to any of formulas VIIB-3 to VIIB-37, wherein Ri-R 4 are all independently halo, halomethyl, or H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is quinolyl, thiazolidinonyl, isothiazolidinonyl, or oxindolyl.
  • the invention contemplates compounds according to any of formulas VIIB-3 to VIIB-37, where Ri is bromo, R 2 -R 4 are H, and R' is isopropyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3-dihydroxy-l -propyl, or 3,4-dihydroxy-2- butyl.
  • the invention contemplates compounds according to any of formulas VIIB-3 to VIIB-37, where R 1 -R 4 are H and R' is isopropyl or 2,3-dihydroxy- 1 -propyl.
  • the invention contemplates compounds according to any of formulas VIIB-3 to VIIB-37, where Ri ispropyn-3-yl, R 2 -R 4 are H and R 1 is isopropyl or 2,3-dihydroxy-l-propyl.
  • the invention contemplates compounds according to any of formulas VIIB-3 to VIIB-37, where Ri is nitro or cyano, R 2 -R 4 are H and R' is 2-hydroxyethyl or 2-hydroxypropyl.
  • the invention contemplates compounds according to any of formulas VIIB-3 to VIIB-37, where R 2 is dimethylamino or dimethylaminomethyl, R 1 , R 3 , and R 4 are H and R 1 is isobutyl or 3-cyclopentyl-propyl.
  • the invention contemplates compounds according to any of formulas VIIB-3 to VIIB-37, where R 1 -R 3 are H, R 4 is chloro, and R' is isopropyl or 2,3-dihydroxy-l-propyl.
  • the invention contemplates compounds according to any of formulas VIIB-3 to VIIB-37, where R 2 is bromo, Ri, R 3 , and R 4 are H, and R 1 is isopropyl or 2,3-dihydroxy-l-propyl.
  • this invention provides a compound of formula VIII below,
  • this invention provides a compound of formula VIIIA below,
  • this invention provides a compound of formula
  • this invention provides a compound of formula VIIIA-I,
  • this invention provides a compound of formula VIIIA-I, where Ri and R 2 are as described above for formula VIII; R 3 and R 4 are both H; and R 1 is -(CH 2 ) n -B, where n is 1 or 2 and B is a five- or six-membered ring or a 9- to 14- member fused ring system, wherein each ring optionally contains 1- 3 heteroatoms selected independently from O, N, and S; wherein each ring is optionally substituted with 1-3 groups selected independently from the following: halogen, hydroxy, cyano, oxo, and Ci-C 4 alkyl, wherein said Ci-C 4 alkyl group is optionally substituted with one to three halogen atoms; and wherein each ring optionally contains one or more double bonds.
  • this invention provides a compound of formula
  • this invention provides a compound of formula VIIIA-I, where Ri and R 2 are as described above; R 3 and R 4 are both H and R' is Ci-C 6 alkyl or 0-Ci-C 6 alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula VIIIA-I, where Ri - R 4 are H and R 1 is Ci-C 6 alkyl or 0-Ci-C 6 alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are halogen; R 3 and R 4 are H; and R' is methyl, ethyl, isopropyl, or sec-butyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri is halogen; R 2 -R 4 are H; and R 1 is methyl, ethyl, isopropyl, or sec-butyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are halogen; R 3 and R 4 are H; and R' is l,2-chloropropan-3-yl or 1 -hydroxy-butan-3 -yl.
  • this invention provides a compound of formula VIIIA-I, in which Ri is bromo; R 2 -R 4 are H; and R' is isopropyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are halogen; R 3 and R 4 are H; and R 1 is l,2-dihydroxy-propan-3- yl, 2-hydroxyethyl, l,2-dihydroxybutan-4-yl, or 4-hydroxybutyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are halogen; R 3 and R 4 are Ci-C 6 alkyl; and R' is 1,2- dihydroxybutan-3-yl or 4-methoxybutyl.
  • this invention provides a compound of formula
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are H; R 3 is 2-hydroxy; R 4 is H; and R' is 3-hydroxypropyl.
  • this invention provides a compound of formula
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are 5-chloro and 6-chloro; R 3 is 2-hydroxy; R 4 is H; and R' is 3- hydroxypropyl.
  • this invention provides a compound of formula VIIIA-I, in which Rj and R 2 are, independently, H or halogen; R 3 is H, 2-OH, or 2-methyl; R 4 is H or methyl; and R' is l,2-chloropropan-3-yl.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are halogen; R 3 and R 4 are, independently H, OH, or methyl; and R' is l-hydroxy-butan-3-yl, l,2-dihydroxy-propan-3-yl, or 2-hydroxyethyl
  • this invention provides a compound of formula VIIIA-I, in which Ri is halo; R 2 -R 4 are, independently H, OH, or methyl; and R 1 is isopropyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are, independently, H or halogen; R 3 and R 4 are, independently, H, OH, or methyl; and R' is 4-hydroxybutyl or l,2-dihydroxybutan-4-yl
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are, independently, H or halogen; R 3 and R 4 are, independently, H, OH, or methyl; and R' is l,2-dihydroxybutan-3-yl.
  • this invention provides a compound of formula
  • Ri and R 2 are, independently, H, Ci-C 6 alkyl, Ci-C 6 alkenyl, Ci-C 6 cycloalkyl, or halogen; R 3 and R 4 are, independently, H, OH, or CpC 6 alkyl; and R' is 1,2- dihydroxybutan-3-yl.
  • this invention provides a compound of formula VIIIA-I, in which Rj and R 2 are, independently, H, CpCg alkyl, or halogen; R 3 and R 4 are, independently, H, OH or methyl; and R' is 4-methoxybutyl, 3-hydroxypropyl or 2- hydroxypropyl.
  • this invention provides a compound of formula VIIIA-I, where Ri and R 2 are fused cyclohexyl or fused cyclopentyl; R 3 and R 4 are, independently, H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2 -butyl.
  • this invention provides a compound of formula VIIIA-I, where Ri and R 2 are benzo; R 3 and R 4 are, independently, H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l -propyl, or 3,4-dihydroxy-2- butyl.
  • this invention contemplates a compound of formula VIIIA-I, where Ri and R 2 , at positions 4 and 5, are fused (4,5)-imidazolo; R 3 and R 4 are, independently, H, OH, or methyl; and R 1 is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula VIIIA-I, where Ri and R 2 , at positions 5 and 6, are fused (2,3)-furyl, (2,3)-pyridyl, or fused cyclopentyl; R 3 and R 4 are, independently, H, OH, or methyl; and R' is isopropyl, 2-(2- furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula VIIIA-I , where Ri and R 2 , at positions 5 and 6, are fused cyclopentyl; R 3 and R 4 are, independently, H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula VIIIA-I , where Ri and R 2 , at positions 6 and 7, are fused cyclopentyl, R 3 and R 4 are, independently, H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula VIIIA-I , where Ri and R 2 , at positions 5 and 6, are benzo; R 3 and R 4 are, independently, H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula VIIIA-I , where R] and R 2 , at positions 6 and 7, are benzo; R 3 and R 4 are, independently, H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula VIIIA-I, where Ri and R 2 , at positions 4 and 5, are benzo, said benzo group bearing fluoro at each ortho position; R 3 and R 4 are, independently, H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3 -dihydroxy-1 -propyl, or 3,4-dihydroxy-2- butyl.
  • this invention provides a compound of formula VIIIA-I, where R 2 - R 4 are H and R 1 is Ci-C 6 alkyl, optionally substituted with halogen, Q- C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula VIIIA-I, where Ri - R 4 are H and R 1 is Ci-C 4 alkyl, optionally substituted with one or two hydroxy groups.
  • this invention provides a compound of formula VIIIA-I, where Ri, R 2 , and R 4 are H; R 3 is methyl or OH; and R' is Ci-C 4 alkyl, optionally substituted with one or two hydroxy groups.
  • this invention provides a compound of formula VIIIA-I, where Ri and R 2 are H; R 3 is H, methyl, or OH; R 4 is H, OH, or Ci-C 4 alkyl, optionally substituted with halogen or hydroxy; and R 1 is C]-C 4 alkyl, optionally substituted with one or two hydroxy groups.
  • this invention provides a compound of formula VIIIA-I, where Ri and R 2 are H; R 3 is H, methyl, or OH; R 4 is methyl, optionally substituted with halogen or hydroxy; and R' is Cj-C 4 alkyl, optionally substituted with one or two hydroxy groups.
  • this invention provides a compound of formula
  • Ri and R 2 are H; R 3 is H, methyl, or OH; R 4 is C ⁇ -C ⁇ alkyl, optionally substituted with halogen or hydroxy; and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, oxazolidinonyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrrolidinonyl, thiazolinyl, thiazolidinyl, thiazolidinonyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula VIIIA-I, where Ri is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 2 - R 4 are H and R' is C 1 -Ce alkyl, optionally substituted with halogen, CpC 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula VIIIA-I, where Ri is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl, R 2 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with halogen, Cj-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula
  • V ⁇ iA-1 in which Ri and R 2 are both halogen, R 3 is 2-methyl, and R 4 is H, and R' is -(CH 2 ) n - B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula
  • R 1 and R 2 are both H, R 3 is 3 -methyl, R 4 is 2-chloro, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-(2-chloroethyl), and R f is - (CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri is 4-CF 3 , R 3 is 2-hydroxymethyl, R 2 and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, oxazolidinonyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrrolidinonyl, thiazolinyl, thiazolidinyl, thiazolidinonyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula VTIIA-I , in which Rj and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2- on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl- 2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl- 1 -pyrimidinyl.
  • this invention provides a compound of formula VIIIA-I, in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4- oxazolyl, 3-methyl-2-pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl; R 2 , R 3 , and R 4 are H, and R' is - (CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, foryl, tetrahydrofuryl, pyrimi
  • this invention contemplates the compound of formula VIIIA-I, in which Ri is 6-chloro, R 2 , R 3 , and R 4 are H, and R' is -(CHo) n -B 5 where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-I, in which Ri is 5-chloro, R 2 , R 3 , and R 4 are H, and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-I, in which Ri is 4-chloro, R 2 , R 3 , and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-I, in which Ri is 7-chloro, R 2 , R 3 , and R 4 are H, and R 1 is -(CH 2 ) O -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-I, in which Ri is 7-bromo, R 2 , R 3 , and R 4 are H, and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-I, in which Rj is 4-bromo, R 2 , R 3 , and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-I, in which Ri is 5-bromo, R 2 , R 3 , and R 4 are H, and R' is -(CH 2 ) U -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates a compound of formula VIIIA-I, in which Ri is 5-CF 3 , R 2 , R 3 , and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, oxazolidinonyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, thiazolidinonyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 , in positions 4 and 6, are both halogen, R 3 is 2-chloromethyl, and R 4 is H, and R' is -(CHa) n -B, where n is 1 or 2, and B is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2- piperidyl, 3-piperidyl, or 4-piperidyl.
  • this invention provides a compound of formula VIIIA-I, in which R] and R 2 , in positions 4 and 6, are both halogen, R 3 is 3-fiuoromethyl, and R 4 is H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is 2-pyrimidyl, 4-pyrimidyl, 2- morpholyl, or 3-morpholyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri and R 2 , in positions 4 and 6, are both halogen, R 3 is 3-fiuoromethyl, and R 4 is H, and R' is -(CH 2 ) n -B, where n is 2, and B is 4-bromo-2-pyrimidyl, 2-chloro-4- pyrimidyl, 2-morpholyl, or 3-morpholyl.
  • this invention provides a compound of formula VIIIA-I, in which Ri is 3-cyano, R 2 - R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2 ⁇ piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula VIIIA-I, in which R 1 is 3-hydroxy, 5-dimethylamino, 4-methoxy, 5-(2-methoxyethyl), or 6- methoxymethyl
  • R 2 - R 4 are H 5 and R 1 is -(CH 2 ) H -B, where n is 1 or 2, and B is 3-methyl-2- pyridyl, 3-methyl-2-piperazinyl, 3-meihylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3- methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention contemplates a compound of formula VIIIA-I, in which Ri is 4-ethoxy, 4-cyano, 4-CH 2 F, 7-acetoxy, 7-acetyl, 6- methyloxycarbonyl, 6-dimethylaminocarbonyl, 4-dimethylamino, 5-dimethylaminocarbonyl, 5-methyloxycarbonyl, 4-acetyl, 4-acetoxy, R 2 , R 3 , and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazo
  • this invention provides a compound of formula VIIIA-2
  • this invention provides a compound of formula A-2, where R 3 and R 4 are both H and R' is -(CH 2 ) n -B.
  • this invention provides a compound of formula VIIIA-2, where R 1 is Cj-Cg alkyl or 0-Ci-C 6 alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula VIIIA-2, where R 3 and R 4 are both H and R 1 is Ci-C 6 alkyl or 0-C 1 -C 6 alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula VIIIA-2, where R 2 - R 4 are H and R 1 is Cj-C 6 alkyl, optionally substituted with halogen, C 1 - C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula A-I, where R 1 , R 2 , and R 4 are H; R 3 is H, methyl or OH; and R' is Ci-C 4 alkyl, optionally substituted with one or two hydroxy groups.
  • this invention provides a compound of formula A-I, where Ri and R 2 are H; R 3 is H, methyl, or OH; R 4 is C]-C 4 alkyl, optionally substituted with halogen or hydroxy; and R' is Ci-C 4 alkyl, optionally substituted with one or two hydroxy groups.
  • this invention provides a compound of formula VIIIA-2, where Ri 1 in position 5, is dimethylamino, dimethylaminomethyl, or acetylamino, R 3 , in position 3, is methoxy or methoxymethyl, R 2 and R 4 are H, and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula VIIIA-2, where Ri , in position 4, is dimethylamino, dimethylaminomethyl, or acetylamino, R 2) in position 6, is bromomethyl, R 3 and R 4 are H, and R' is mono-hydroxy C 1 -C 4 alkyl.
  • this invention provides a compound of formula VIIIA-2, where R 1 is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl, R 2 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula VIIIA-2, in which Ri and R 2 are both halogen, R 3 is 2-methyl, and R 4 is H, and R' is -(CH 2 ) n - B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula VIIIA-2, in which Ri and R 2 , in positions 4 and 6, are both halogen, R 3 is 2-chloromethyl, and R 4 is H, and R' is -(CH 2 ) n -B, where n is 1, and B is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2- piperidyl, 3-piperidyl, or 4-piperidyl.
  • this invention provides a compound of formula VIIIA-2, in which Ri and R 2 , in positions 4 and 6, are both halogen, R 3 is 3-fluoromethyl, and R 4 is H, and R 1 is -(CHa) n -B, where n is 1, and B is 2-pyrimidyl, 4-pyrimidyl, 2-mo ⁇ holyl, or 3-morpholyl.
  • this invention contemplates a compound of formula VIIIA-2, where Ri - R 4 are H and R' is 2-(2-furyl)ethyl, 2-hydroxyethyl, or 2,3-dihydroxy-l- propyl.
  • this invention contemplates a compound of formula VIIIA-2 in which Ri and R 2 together, at positions 5 and 6, are benzo or fused cyclopentyl, R 3 and R 4 are H, and R' is isopropyl.
  • this invention contemplates a compound of formula VIIIA-2 in which Ri and R 2 together, at positions 6 and 7, are fused 2,3-pyrido or pyrrolo, R 3 and R 4 are H, and R' is isopropyl.
  • this invention contemplates a compound of formula VIIIA-2 in which Rj and R 2 together, at positions 4 and 5, are fused (2,3)-furyl, R 3 and R 4 are H, and R' is l,2-dihydroxy-propan-3-yl.
  • this invention contemplates a compound of formula VIIIA-2 in which Ri and R 2 together, at positions 6 and 7, are fused (2,3) thienyl, R 3 and R 4 are H, and R 1 is 2-hydroxyethyl.
  • this invention provides a compound of formula VIIIA-2 in which R] and R 2 are both H, R 3 is 4- methyl or 5-methyl, R 4 is 7-chloro, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula VIIIA-2 in which Ri is 4-CF 3 , R 3 is 6-hydroxymethyl, R 2 and R 4 are H, and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula VIIIA-2 in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is 3-methyl-2 -pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2- on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl- 2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-2 in which Rj is 5-chloro, 6-chloro, or 7-chloro, R 2 , R 3 , and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-2 in which Ri is 3-bromo, 4-bromo, or 5-bromo, R 2 , R 3 , and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula VIIIA-2 in which Ri is 6-chloro, R 2 is 7-chloro, R 3 and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula VIIIA-2 in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula VIIIA-2 in which Ri is 4-CF 3 , R 2 , R 3 , and R 4 are H, and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula VIIIA-2 in which Ri is 4-cyano, 4-hydroxy, 4-methoxy, 5-hydroxy, or 4-methoxymethyl, R 2 - R 4 are H, and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l- pyrimidinyl.
  • this invention contemplates a compound of formula VIIIA-2 in which Ri is 4-dimethylamino, 7-acetyl, 7-dimethylamino, 7- dimethylaminocarbonyl, or 7-methyloxycarbonyl, R 2 , R 3 , and R 4 are H, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazol-4-yl, isoxazol-3-yl, oxazol-2-yl, 2-oxazolin-2-yl, oxazolidin-4-yl, thiazol-2-yl, thien-2-yl, fur-2-yl, pyrrol-3-yl, pyrrolin-4-yl, pyrrolidin-3-yl, thiazolin-4-yl, thiazolidin-4-yl, imidazol-2-yl, 2-pyridyl, 4-pyridyl,
  • this invention contemplates a compound of formula VIIIA-2 in which Ri is 6-acetoxy, or 7-acetoxy, R 2 , R 3 , and R 4 are H, and R' is - (CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula VIIIA-2 in which Ri is 7-acetyl, or 7-acetoxy, R 2 , R 3 , and R 4 are H, and R' is - (CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula VIIIA-2 in which Ri is 3-CH 2 F, R 2 , R 3 , and R 4 are H, and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula VIIIB-I,
  • this invention provides a compound of formula VIIIB-I, where R 1 -R 4 are, independently, H, Ci-C 3 alkyl, OH, or halogen; and R' is -(CH 2 ),,- B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula VIIIB-I, where Rj-R 4 are, independently, H, C 1 -C 3 alkyl, OH, or halogen; and R 1 is C 1 -C 4 alkyl, optionally substituted with one or two hydroxy groups.
  • this invention provides a compound of formula
  • Rj-R 4 are H and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 1-hydroxy- 2-propyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula VIIIB-I, where Rj-R 4 are H and R' is l-hydroxy-2-propyl, 2,3-dihydroxy-l-propyl, or isopropyl.
  • this invention provides a compound of formula VIIIB-I, where Ri and R 2 are H; R 3 is 2-methyl or 2-hydroxy; R 4 is H or methyl; and R 1 is isopropyl.
  • this invention provides a compound of formula VIIIB-I, where Ri and R 2 are H; R 3 is 2-methyl or 2-hydroxy; R 4 is H or methyl; and R 1 is 2,3-dihydroxy-l-propyl or l-hydroxy-2- ⁇ ropyl.
  • this invention provides a compound of formula VIIIB-I, where Ri is C 1 -C 4 alkyl, Ci-C 4 alkenyl, C 1 -C 4 alkynyl, halomethyl, or halogen; R 2 -R 4 are H; and R 1 is 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula VIIIB-I, where Ri is C]-C 4 alkyl, Ci-C 4 alkenyl, Ci -C 4 alkynyl, halomethyl, or halogen; R 2 - is H; R 3 is 2-OH; R 4 is methyl or H; and R 1 is 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula VIIIB-I, where Ri-R 4 are H and R 1 is 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula VIIIB-I, where Ri-R 4 are H and R' is ethoxy, isopropoxy, or 0-CH(CH 3 )CH 2 CH 3 .
  • this invention provides a compound of formula VIIIB-I, where Ri -R 4 are H and R' is ethoxy.
  • this invention contemplates a compound of formula VIIIB-I, where Ri-R 4 are H and R' is 2-chloroethyl, 2-bromoethyl, or l,2-dichloro-3- propyl.
  • this invention provides a compound of formula VIIIB-I where one of Ri and R 2 is H and the other is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 3 - R 4 are H, and R' is C]-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula VIIIB-I, where one of Ri and R 2 is H and the other is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl, R 3 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula VIIIB-I, where Ri and R 2 are fused cyclohexyl or fused cyclopentyl, R 3 and R 4 are H, and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l- ⁇ ropyl, or 3,4-dihydroxy-2- butyl.
  • this invention provides a compound of formula VIIIB-I, where Ri and R 2 are benzo, R 3 and R 4 are H, and R' is isopropyl, 2-(2-furyl)ethyl, 2- hydroxyethyl, 2,3-dihydroxy-l -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula
  • R 1 and R 2 are halogen, R 3 and R 4 are H, and R' is isopropyl, 2-(2- furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula VIIIB-I, where R] - R 3 are H, R 4 is 2-halo, 2-cyano, 2-hydroxy, or 2-methoxy, and R' is - (CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula VIIIB-I, where Ri is halo, R 2 - R 4 are H and R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • the invention contemplates a compound of formula VIIIB-I, where Ri is bromo, R 2 - R 4 are H and R' is isopropyl, 2-hydroxyethyl, 1- hydroxy-2 -propyl, or 2,3-dihydroxy-l-propyl.
  • this invention provides a compound of formula VIIIB-2,
  • this invention provides a compound of formula VIIIB-2, where RpR 4 are, independently, H or halogen, and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2-methoxyethyl, l-hydroxy-2-propyl,l,2-dihydroxy-3-propyl, or 3,4- dihydroxy-2 -butyl.
  • this invention provides a compound of formula VIIIB-2, where one of Ri and R 2 is H and the other is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 3 - R 4 are H, and R 1 is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula VIIIB-2, where one of Ri and R 2 is H and the other is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl, R 3 - R 4 are H and R' is Ci-Ce alkyl, optionally substituted with halogen, C1-C3 alkoxy, or hydroxy.
  • the invention provides compounds according to any of formulas VIIIB-3 to VIIIB-20, wherein Rj -R 4 are all independently methyl, methoxy, ethyl, vinyl, ethynyl, halo, OH, or H, and R 1 is -(CH 2 ) n -B, where n is 1 or 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, fiiryl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl,
  • the invention provides compounds according to any of formulas VIIIB-I to VIIIB-20, wherein Ri-R 4 are all independently halo, halomethyl, OH, or H, and R' is -(CHa) n -B, where n is 1 or 2, and B is phenyl, pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • the invention contemplates compounds according to any of formulas VIIIB-I to VIIIB-20, where Ri is bromo; R 2 -R 4 are all H; and R' is isopropyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3-dihydroxy-l -propyl, or 3,4-dihydroxy- 2-butyl.
  • the invention contemplates compounds according to any of formulas VIIIB-I to VIIIB-20, where Ri -R 4 are, independently, H, OH, Ci-C 4 alkyl, Ci -C 4 alkenyl, Ci -C 4 alkynyl, halo, halomethyl, nitro, or cyano; and R' is isopropyl or 2,3- dihydroxy- 1 -propyl.
  • the invention contemplates compounds according to any of formulas VIIIB-I to VIIIB-20, where R 1 -R 4 are all H and R 1 is isopropyl or 2,3- dihydroxy- 1 -propyl.
  • the invention contemplates compounds according to any of formulas VIIIB-I to VIIIB-20, where Ri-R 4 are H; R 3 and R 4 are, independently, H, methyl, or OH; and R' is isopropyl or 2,3-dihydroxy-l-propyl.
  • the invention contemplates compounds according to any of formulas VIIIB-I to VIIIB-20, where Ri is acetyl, acetoxy, acetamido, methylcarbamoyl, methylsulfonyl, methyloxycarbonyl, ethyloxycarbonyl, or cyclopropylethynyl; R 2 -R 4 are all H; and R' is isopropyl or 2,3-dihydroxy-l-propyl.
  • the invention contemplates compounds according to any of formulas VIIIB-I to VIIIB-20, where Ri is acetyl, acetoxy, acetamido, methylcarbamoyl, methylsulfonyl, methyloxycarbonyl, ethyloxycarbonyl, or cyclopropylethynyl; R 2 is H; R 3 is 2-OH or 2-methyl; R 4 is H, OH, or methyl; and R' is isopropyl or 2,3-dihydroxy-l-propyl.
  • the invention contemplates compounds according to any of formulas VIIIB-I to VIIIB-20, where Ri -R 3 are all H; R 4 is chloro; and R' is isopropyl or 2,3-dihydroxy-l-propyl.
  • the invention contemplates compounds according to any of formulas VIIIB-I to VIIIB-20, where R 2 is bromo; R 1 , R 3 , and R 4 are all H; and R 1 is isopropyl or 2,3-dihydroxy-l-propyl.
  • this invention provides a compound of formula IX,
  • this invention provides a compound of formula A below, where all substituents are as defined for formula I above.
  • this invention provides a compound of formula IXB,
  • M, Q, T, U, and V represent N, CH, or CRi 12> or 3 , provided that at least one of M, Q, T, U, and V is N, and further provided that no two nitrogen atoms are adjacent, and where Ri - R 4 are as defined as above.
  • this invention provides a compound of formula IXA, where Ri - R 4 are defined as for formula IX, and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, isoxazolindinonyl, oxazolyl, oxazolinyl, oxazolidinyl, oxazolidinonyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, thiazolidinonyl, isothiazolinyl, isothiazolidinyl, isothiazolidinonyl, imidazolinyl, imidazolyl, pyridyl, tolyl, or phenyl, wherein all rings are optionally substituted as described above.
  • this invention provides a compound of formula IXA, where Rj and R 2 are as defined for formula DC; R 3 and R 4 are both H; and R 1 is -(CH 2 ) n - G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl , or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where Ri is 2-chloro, R 2 is 6-methyl, and R 3 - R' are as defined for formula IXA.
  • this invention provides a compound of formula IXA, where Ri - R 4 are defined as for formula I, and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is naphthyl, quinolyl, isoquinolyl, indanyl, or benzimidazolyl, wherein all rings are optionally substituted as described above in the definition of G for formula I.
  • this invention provides a compound of formula IXA, where Ri - R 4 are defined as for formula I, and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is cyclopentyl, cyclohexyl, tetrahydrofuryl, tetrahydrothienyl, piperidyl, piperazinyl, or morpholyl, wherein all rings are optionally substituted as with methyl or halo.
  • this invention provides a compound of formula IXA, where Ri - R 4 are defined as for formula I, and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, ⁇ iperazin-1- yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, 2- ⁇ yrrolidon-l-yl, or 2-pyrrolidon-6-yl.
  • this invention provides a compound of formula
  • Ri - R 3 are as defined for formula I, R 4 is H or methyl, and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl.
  • this invention provides a compound of formula IXA, where R] and R 2 , in positions 2 and 6, are alkyl or halo, R 3 is H, R 4 is H or methyl, and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4- morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, 1-methyl- piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl.
  • this invention provides a compound of formula IXA, where Rj - R 4 are defined as for formula II, and R' is C 1 -C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where Rj - R 3 are as defined for formula II, R 4 is H or methyl, and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where R 1 and R 2 , in positions 2 and 6, are alkyl or halo, R 3 is alkyl, haloalkyl, cycloalkyl, alkenyl, or alkynyl, R 4 is H or methyl, and R' is CpC 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where R 1 and R 2 , in positions 2 and 6, are alkyl or halo, R 3 is H, R 4 is H or methyl, and R' is C 1 -C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where Ri and R 2 are, independently, H, halo, or Ci-C 3 alkyl; R 3 and R 4 are both H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 2-halo or 2-methyl; R 2 is 6-methyl; R 3 and R 4 are, independently, H, Ci-C 3 alkyl, or halo; and R' is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-chloro; R 2 is 6-methyl; R 3 and R 4 are, independently, H, Q- C 3 alkyl, vinyl, cyclopropyl, or halo; and R' is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-methyl; R 2 and R 3 are H; R 4 is methyl; and R ! is isopropyl or mono- or di-hydroxy C]-C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Rj - R 4 are H; and R' is isopropyl or mono- or di-hydroxy Cj-C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-chloro; R 2 is 6-methyl; R 3 and R 4 are, independently, H, Cj-C 3 alkyl, CpC 3 alkoxy, Cj-C 3 alkenyl, Cj-C 3 alkenoxy, hydroxy, or halo; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6- dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2- on-4-yl, or 2-pyrrolidonyl , or R' is Q-Cg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Rj is 2-chloro; R 2 is 6-methyl; R 3 and R 4 are, independently, H, methyl, methoxy, vinyl, 2-methoxyethene, hydroxy, or chloro; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, 1- methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl , or R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • Ri is C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, or Ci-C 6 cycloalkyl
  • R 2 and R 3 are H
  • R 4 is H or methyl
  • R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where Ri is 2- methylpropenyl, 1-propynyl, or cyclopropyl; R 2 and R 3 are H; R 4 is H or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where Ri is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetamido; R 2 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where Ri is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl; R 2 - R 4 are H and R' is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, where Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl; R 2 - R 4 are H; and R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Rj is 2-methyl; R 2 and R 3 are both halogen; R 4 is H; R' is -(CH 2 ) H -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl, or R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri and R 2 are both chloro; R 3 is H; R 4 is methyl; R' is -(CHo) n -G, where n is 1, and G is piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, or tetrahydrofuryl, or R' is CpCg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 3-methyl; R 2 and R 3 are both H; R 4 is 2-chloroethyl; R' is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 2-hydroxymethyl; R 3 is 4-CF 3 ; R 2 and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri 3-methyl; R 2 is 5-chloro; R 3 and R 4 are both H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6 ⁇ dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which one or both of Ri and R 2 are CF 3 ; R 3 and R 4 are H; and R 1 is ⁇ (CH 2 ) n -G, where n is 1, and G is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2- pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula IXA, in which Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl; R 2 , R 3 , and R 4 are H; and R' is - (CH 2 ) n -G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, pyrimi
  • this invention contemplates the compound of formula IXA, in which R] is 3-chloro; R 2 , R 3 , and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 2-chloro; R 2 is 6-methyl; R 3 ; and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 4-chloro; R 2 , R 3 , and R 4 are H; and R 1 is -(CH 2 ) O -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri and R 2 are 2- and 6-chloro; R 2 , R 3 , and R 4 are H; and R' is ⁇ (CH 2 ) n - G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 2-bromo; R 2 ; R 3 ; and R 4 are H; and R 1 is -(CH 2 ) n -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula IXA, in which Ri is 3-bromo; R 2 ; R 3 ; and R 4 are H; and R 1 is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula IXA, in which Rj is 4-bromo; R 2 , R 3 , and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula IXA, in which Ri is 2-, 3-, or 4-bromo; R 2 , R 3 , and R 4 are H; and R 1 is -(CH 2 ) n -G, where n is 1, and G is R 1 is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 4-bromo; R 2 is 2-methyl; R 3 is 3-methyl; R 4 is H, methyl, or halo; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 2-bromo; R 2 is 6-methyl; R 3 is 3 -methyl; R 4 is H, methyl, or halo; and R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 3-bromo; R 2 is 6-methyl; R 3 is H; R 4 is H, methyl, or halo; and R' is Ci-C 4 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 2-chloro; R 2 is 4-chloro; R 3 and R 4 are H; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 2-methyl; R 2 is 6-methyl; R 3 and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which one or both of Ri and R 2 are CF 3 ; R 3 and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R' is Ci-Cg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which R] is 2-CF 3 ; R 2 ; R 3 ; and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri and R 2 , in positions 2 and 6, are, independently, methyl or halogen; R 3 is 2- chloromethyl, R 4 is H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-piperidyl, 3-piperidyl, or 4-piperidyl or R' is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Ri and R 2 , in positions 2 and 6, are, independently, methyl or halogen; R 3 is 3- fluoromethyl; and R 4 is H; R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 2-pyrimidyl, 4- pyrimidyl, 2-morpholyl, or 3-morpholyl or R' is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Rj and R 2 , in positions 2 and 6, are, independently, methyl or halogen; R 3 is 3- methyl; and R 4 is H; R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 2-pyridyl, 3-pyridyl, 4- pyridyl, 2-piperidyl, 3-piperidyl, or 4-pi ⁇ eridyl.
  • this invention provides a compound of formula IXA, in which Ri and R 2 , in positions 2 and 6, are, independently, methyl or halogen; R 3 is 3- fluoromethyl; and R 4 is H; R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-bromo-2-pyrimidyl, 2-chloro-4-pyrimidyl, 2-morpholyl, or 3-morpholyl.
  • this invention provides a compound of formula IXA, in which Ri is 3-cyano; R 2 is H or 6-methyl; R 3 and R 4 are H or methyl; and R' is - (CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl or R' is isopropyl or mono- or di-hydroxy Cj -C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Ri is 3-hydroxy; R 2 is H or 6-methyl; R 3 and R 4 are, independently, H or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3-methylpiperazin-2-on-l-yI, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1 -morpholyl, 3-methyl-2-furyL 3-methyl-2-tetrahydrofuryl, or 2-methyl-l- pyrimidinyl.
  • this invention provides a compound of formula IXA, in which Ri is 4-hydroxy; R 2 is H or 2-methyl; R 3 and R 4 are, independently, H or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l-mo ⁇ holyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l- pyrimidinyl or R 1 is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-, 3-, or 4- methoxy; R 2 is H or 2-methyl; R 3 and R 4 are, independently, H, hydroxy, or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3- methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2- piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl ⁇ 2-furyl, 3-methyl-2-tetrahydrofuryl, or 2- methyl-1-pyrimidinyl or R' is isopropyl or mono- or di-hydroxy CpC 4 alkyl.
  • this invention provides a compound of formula
  • Ri is 2-, 3-, or 4- methoxy
  • R 2 is H or 6-methyl
  • R 3 and R 4 are, independently, H or methyl
  • R 1 is -(CH 2 ) n -G, where n is 1 or 2
  • G is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2- ⁇ iperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl- 1- pyrimidinyl or R' is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-, 3-, or 4- ethoxymethyl; R 2 is H or 6-methyl; R 3 and R 4 are, independently, H, hydroxy, or methyl; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpi ⁇ erazin-2-on-l-yl, 3 -methyl- 1- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l -pyrimidinyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-, 3-, or 4- methoxymethyl; R 2 is H or 6-methyl; R 3 and R 4 are, independently, H, hydroxy, methoxy, halo, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 3-(2-methoxyethyl); R 2 is H, 2-methyl, or 6-methyl; R 3 and R 4 are, independently, H, hydroxy, methoxy, or methyl; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 4-(2-methoxyethyl); R 2 is H, 2-methyl, or 6-methyl; R 3 and R 4 are, independently, H or methyl; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2- pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l-piperidinyl, 3- methyl-2-piperidinonyl, 3-methyl-l-morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl or R' is CpC 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4- dimethylamino; R 2 is H or 6-methyl; R 3 and R 4 are, independently, H, methyl, or hydroxy; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4- dimethylamino; R 2 is H or 6-methyl; R 3 is 3-methyl; R 4 is methyl, halo, or H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4- dimethylaminocarbonyl; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4- methyloxycarbonyl; R 2 is H or 6-methyl; R 3 is H or methyl, R 4 is H; and R' is Q-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which R] is 2-, 3-, or 4- acetyl; R 2 is H or 6-methyl, R 3 is H, chloro, or methyl; R 4 is H or 5-methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4- acetoxy; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, methyl, or chloro; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4- morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, 1-methyl- piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R f is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which R) is 2-, 3-, or 4- dimethylamino; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, methyl, hydroxy, methoxy, or chloro; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R 1 is Ci-Cg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3- or 4-dimethylaminocarbonyl; R 2 is H or 6-methyl; R 3 is H or 3-methyl; R 4 is H, methyl, or chloro; and R is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4-methyloxycarbonyl; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, methyl, hydroxy, methoxy, or chloro; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3- or 4- chloroacetyl; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, methyl, hydroxy, methoxy, or chloro; and R' is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3- or 4-acetoxy; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, h ydroxy, methoxy, or chloro; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3- or 4- fluoromethyl; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H or 5-chloro; and R 1 is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 4-cyano; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, methyl, hydroxy, methoxy, halomethyl, or chloro; and R 1 is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or pheny
  • this invention provides a compound of formula
  • Ri is 2-, 3- or 4-ethoxy
  • R 2 is H or 6-methyl
  • R 3 is H or methyl
  • R 4 is H, methyl, hydroxy, methoxy, vinyl, halomethyl, or chloro
  • R' is -(CH 2 ) n -G, where n is 1 or 2
  • G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl
  • R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 2-, 3-, or 4-vinyl; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, methyl, or chloro; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4- morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, 1-methyl- piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 2-, 3-, or 4-chloromethoxy; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, methyl, hydroxy, methoxy, or chloro; and R 1 is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 4-methoxy; R 2 - R 4 are H; R' is -(CH 2 ) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-methyl; R 2 is 4-methylsulfonyl; R 3 and R 4 are, independently, H, hydroxy, halomethyl, or methyl; and R' is -(CHa) n -G, where n is 1, and G is 3-methyl-2- isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2-pyrrolyl, 3-methyl-2- pyridyl, or m-tolyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-, 3-, or 4-methoxy; R 2 is H or 6-methyl; R 3 is H or methyl; R 4 is H, methyl, or chloro; and R' is -(CH 2 ) H -G, where n is 1, and G is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula
  • Ri is 2-, 3-, or 4-bromo
  • R 2 is H or 6-methyl
  • R 3 is H or methyl
  • R 4 is H, methyl, or chloro
  • R 1 is -(CHa) n -G, where n is 1, and G is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula IXA, in which Ri is 2-chloro; R 2 is 3-, 4-, 5-, or 6-cyclopropyl, R 3 and R 4 are, independently, H, halo, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 3-cyclopropyl; R 2 - R 4 are H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 3-cyclopropyl; R 2 is 2-, 4-, 5-, or 6-chloro; R 3 and R 4 are H; and R 1 is Ci- C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 2-chloro; Ra is ⁇ r ⁇ r ⁇ -4-(2-methylcyclopropyl); R 3 and R 4 are H; R' is - (CHa) n -G, where n is 1, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula IXA, in which Ri is 4-cyclo ⁇ ropyl; R 2 is 2- or 3-chloro; R 3 and R 4 are, independently, H, halo, or Ci-C 3 alkyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • Ri is 4-isopropyl
  • R 2 is 2-chloro
  • R 3 is 2- or 3-chloro
  • R 4 is methyl, hydroxy, methoxy, or halo
  • R 1 is -(CH 2 ) n -G, where n is 1, and G is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l- pyrimidinyl or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri and R 2 are both halogen; R 3 is 3-methyl; R 4 is H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Rj and R 2 are both H; R 3 is 3-chloro; R 4 is methyl, hydroxy, methoxy, or halo; and R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • Ri and R 2 are both H;
  • R 3 is 2-(2-chloroethyl);
  • R 4 is methyl, hydroxy, methoxy, or halo;
  • R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or
  • R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • Ri is 2-hydroxymethyl
  • R 2 is 4-CF 3
  • R 3 and R 4 are H
  • R 1 is -(CH 2 ) U -G, where n is 2, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula IXA, in which Ri is 3-chloro; R 2 and R 3 are both H; R 4 is methyl; and R' is -(CH 2 ) ⁇ -G, where n is 2, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3- methyl-1-piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3- methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl, or R' is C 1 -Cg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which one or both of Ri and R 2 are CF 3 ; R 3 and R 4 are H; R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3- methyl-2-pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention contemplates the compound of formula IXA, in which Ri is 4-chloro; R 2 is 3-chloro; R 3 and R 4 are H; R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Rj is 2-, 3-, or 4- fluoro; R 2 , R 3 , and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula IXA, in which Ri is fluoro; R 2 is methyl; R 3 and R 4 are H; R' is -(CH 2 ) n -G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which R] is 6-chloro; R 2 , R 3 , and R 4 are H; R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula IXA, in which Ri is 2-bromo, 3-bromo, or 4-bromo; R 2 is methyl; R 3 ; and R 4 are H; R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, mo ⁇ holyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula IXA, in which Ri is 2-(2-chloroethyl); R 2 is 6-chloro; R 3 and R 4 are H; R 1 is -(CH 2 ) n - G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula IXA, in which Ri is 4-(3-chloropropyl); R 2 is 2-bromomethyl; R 3 and R 4 are H; R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-CF 3 ; R 2 , R 3 , and R 4 are H; R' is -(CH 2 ) n -G, where n is 1 or 2, and G is isothiazol-4-yl, isoxazol-4-yl, oxazol-2-yl, 2-oxazolin-4-yl, oxazolidin-5-yl, or thiazol-2-yl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Rj is 4-cyano; R 2 is 2-methyl; R 3 and R 4 are H or methyl; R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2- on-l-yl, 3 -methyl- 1 -piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1 -morpholyl, 3-methyl- 2-furyl, 3-methyl-2 -tetrahydrofuryl, or 2-methyl- 1 -pyrimidinyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-methyl; R 2 is 4- or 5-hydroxy; R 3 and R 4 are, independently, H, hydroxy, methoxy, halo, or methyl; R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 3-methyl-2- pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1 -piperidinyl, 3- methyl-2-pi ⁇ eridinonyl, 3-methyl-l -morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl- 1 -pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 2-hydroxymethyl; R 2 - R 4 are H; R' is -(CH 2 ) n -G, where n is 2, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyI, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl, or R' is Cj-Cg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula IXA, in which Ri is 2-methoxy; R 2 is H, halo, or methyl; R 3 and R 4 are, independently, H or methyl; R' is -(CH 2 ) H -G, where n is 2, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • Ri is 4-methoxy
  • R 2 - R 4 are H
  • R' is -(CH 2 ) n -G, where n is 2, and G is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyL 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention contemplates a compound of formula IXA, in which R] is 2-, 3-, or 4-dimethylamino; R 2 ; R 3 ; and R4 are H; R' is -(CHb) n - G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl, or R' is Ci-Ce alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4-acetyl; R 2 , R 3 , and R 4 are H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula IXA, hi which Ri is 2-, 3-, or 4-acetoxy; R 2 , R 3 , and R 4 are H; and R' is -(CHo) n -G, where n is 1 or 2, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula IXA, in which Ri is 4-methyloxycarbonyl; R 2 is H or methyl; R 3 and R4 are H; and R' is -(CH 2 )n-G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4- morpholyl, or 4-imidazolyl.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4-acetyl; R 2 , R 3 , and R4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4 ⁇ morpholyl, or 4- imidazolyl.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4-acetoxy; R 2 ; R 3 ; and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4- imidazolyl.
  • this invention contemplates a compound of formula IXA, in which Ri is 2-, 3-, or 4-CH 2 F; R 2 ; R 3 ; and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or A- imidazolyl.
  • this invention provides a compound of formula
  • Ri is 2-, 3-, or 4-cyano
  • R 2 - R 4 are H
  • R' is -(CHV) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula IXA 5 in which Ri is 2-, 3-, or 4-ethoxy; R 2 - R 4 are H; and R 1 is ⁇ (CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula IXA, in which Rj is 2-, 3-, or 4-trifluoromethoxy; R 2 - R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-, 3-, or 4-chloromethoxy; R 2 - R 4 are H; and R' is -(CH 2 ) H -G, where n is 1 or 2, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, f ⁇ ryl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrrolidinonyl, morpholyl, or imidazolyl.
  • this invention provides a compound of formula IXA, in which Ri is 2-, 3-, or 4-methoxy; R 2 - R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 5-oxazolidinyl, 4-thiazolyl, 3-thienyl, 2-furyl, 3-pyrrolyl, 2-pyrrolidinyl, N- pyrrolidinonyl, N-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula IXA, in which Ri is 3- or 4-methylsulfonyl R 2 is 2-(2-methyl cyclopropyl); R 3 and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 3-methyl-2-isothiazolyl, 3-methyl-2- isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2-pyrrolyl, 3-methyl-2- ⁇ yridyl, N-pyrrolidonyl, or m-tolyl.
  • this invention provides a compound of formula IXA, in which R] is 2-, 3-, or 4-methoxy; R 2 - R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is cyclopentyl, cyclo ⁇ enten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2- yi.
  • this invention provides a compound of formula IXA, in which Ri is 4-bromo or 4-bromomethyl; R 2 - R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula IXA, in which Ri is 2- or 3-chloro; R 2 is 4-(2-cyclopropylethyl); R 3 and R 4 are H; and R' is - (CH 2 ) n -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula
  • Ri is cyclopropyl or cyclopropylmethyl
  • R 2 - R 4 are H
  • R' is -(CH 2 ) n -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula IXA, in which Ri is £r ⁇ 7M-3-(2-methylcyclopropyl); R 2 is 6-chloro; R 3 and R 4 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4- morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula IXA, in which Ri is 3- or 4-cyclopropyl; R 2 is 5-chloro; R 3 is 2-(2-fluoroethyl); and R 4 is H, hydroxy, methoxy, or halo; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula IXA, in which Ri is 2- or 3-cyclopropyl; R 2 is 6-chloro; R 3 is 3-chloro; R 4 is methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- mo ⁇ holyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula IXA, in which Ri and R 2 are halogen or methyl; R 3 and R 4 are H; and R' is methyl, ethyl, isopropyl, or sec-butyl.
  • this invention provides a compound of formula IXA, in which Ri is halogen or methyl; R 2 -R 4 are H; and R 1 is methyl, ethyl, isopropyl, or sec-butyl.
  • this invention provides a compound of formula IXA, in which R] and R 2 are, independently, halogen or methyl; R 3 and R 4 are H; and R' is 1 ,2-chloropropan-3 -yl.
  • this invention provides a compound of formula IXA, in which Ri and R 2 are, independently, halogen or methyl; R 3 and R 4 are H; and R' is 1- hydroxy-butan-3 -yl.
  • this invention provides a compound of formula
  • this invention provides a compound of formula IXA, in which Ri and R 2 are, independently, halogen or methyl; R 3 and R 4 are H; and R' is 1 ,2-dihydroxy-propan-3 -yl.
  • this invention provides a compound of formula
  • this invention provides a compound of formula IXA, in which Ri and R 2 are, independently, halogen or methyl; R 3 and R 4 are H; and R' is 4- hydroxybutyl.
  • this invention provides a compound of formula IXA, in which Rj and R 2 are, independently, halogen or methyl; R 3 and R 4 are H; and R' is 1 ,2-dihydroxybutan-4-yl.
  • this invention provides a compound of formula IXA, in which Ri and R 2 are, independently, halogen or methyl; R 3 and R 4 are Ci-C 6 alkyl; and R 1 is l,2-dihydroxybutan-3-yl.
  • this invention provides a compound of formula
  • R] and R 2 are halogen or methyl; R 3 and R 4 are H; and R' is 4-methoxybutyl.
  • this invention provides a compound of formula IXA, in which Ri and R 2 are, independently, halogen or methyl; R 3 and R 4 are H; and R' is 3- hydroxypropyl.
  • this invention provides a compound of formula
  • Ri and R 2 together are fused cyclohexyl or fused cyclopentyl; R 3 and R 4 are H; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, 2,3-dihydroxy-l-pro ⁇ yl, or 3 ,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula IXA, where Rj and R 2 , at positions 3 and 4, are fused (4,5)-imidazolo; R 3 and R 4 are H; and R 1 is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, 2,3-dihydroxy-l- ⁇ ropyl, or 3 ,4-dihydroxy-2-Butyl.
  • this invention contemplates a compound of formula IXA, where Ri and R 2 , at positions 3 and 4, are fused (2,3)-furyl; R 3 and R 4 are H; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3 ,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula IXA, where Ri and R 2 , at positions 3 and 4, are fused (2,3)-pyrido; R 3 and R 4 are H; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, l-hydroxy-2 -propyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula IXA, where Ri and R 2 , at positions 3 and 4, are fused (3,4)pyrrolyl; R 3 and R 4 are H; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula IXA, where Ri and R 2 , at positions 2 and 3, are fused cyclopentyl; R 3 and R 4 are H; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3- dihydroxy- 1 -propyl, or 3 ,4-dihydroxy-2 -butyl.
  • this invention contemplates a compound of formula.IXA, where Ri and R 2 , at positions 3 and 4, are fused cyclopentyl; R 3 and R 4 are H; and R 1 is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula IXA, where Ri and R 2 , at positions 2 and 3, are benzo; R 3 and R 4 are H; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3-dihydroxy-l- propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula IXA, where Ri and R 2 , at positions 2 and 3, are benzo, substituted at one or both ortho positions; R 3 and R 4 are H; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2- hydroxyethyl, l-hydroxy-2-propyl, 2,3-dihydroxy-l -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula IXA, where Ri and R 2 , at positions 3 and 4, are benzo; R 3 and R 4 are H; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3-dihydroxy-l - propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of any of formulas IXB-I - IXB-6, in which R 1 , R 2 , and R 4 are, independently, H, Cj-C 4 alkyl, alkenyl, alkynyl, cycloalkyl, cyano, acetyl, acetoxy, acetamido, methylcarbamoyl, dimethylamino, or halo; R 3 is H, and R 1 is -(CH 2 ) n -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, optionally substituted as described above, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-I, where Ri is 3-methyl or 3-halo; R 2 and R 3 are H; R 4 is H, vinyl, cyano, halo, hydroxy, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-I, where Ri is 3-methyl or 3-halo; R 2 and R 3 are H; R 4 is H or methyl; and R' is Ci-Ce alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-2, where Ri is 2-methyl or 2-halo; R 2 and R 3 are, independently, H, halo, Q- C 6 alkyl, or Ci-C 6 alkenyl, said alkyl and alkenyl groups optionally substituted as described above; R 4 is H, vinyl, cyano, halo, hydroxy, or Ci-C 6 alkyl; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl- ⁇ iperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-2, where Ri is 4-methyl or 4-halo; R 2 and R 3 are H; R 4 is H, OH, halo, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups or R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-2, where Ri is 2-methyl; R 2 is 4-halo; R 3 is H; R 4 is H, OH 3 halo, or methyl; and R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-2, where Rj is 2-halo; R 2 is 4-methyl; R 3 is H; R 4 is H, OH, halo, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-2, where Rj is 2-methyl; R 2 is 4-chloro; R 3 is H; R 4 is H, OH, or methyl; and R 1 is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, l-hydroxy-2 -propyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound according to formula IXB-2, where R] is 2-chloro; R 2 is 4-methyl; R 3 is H; R 4 is H, OH, or methyl; and R' is isopropyl, (2-tetrahydrofuryl)methyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2 -butyl.
  • this invention provides a compound according to formula IXB-3, where Ri is 4-methyl or 4-halo; R 2 and R 3 are H; R 4 is H, vinyl, cyano, halo, hydroxy, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-3, where Ri is 4-methyl or 4-halo; R 2 is 6-methyl or 6-halo; R 3 is H; R 4 is H, hydroxy, or methyl; and R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-3, where Ri is 4-methyl or 4-halo; R 2 is 6-methyl or 6-halo; R 3 is H; R 4 is H or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1- ⁇ iperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl- 1- pyrimidinyl.
  • this invention provides a compound according to formula IXB-3, where Ri is 4-methyl or 4-halo; R 2 is 6-methyl or 6-halo; R 3 is H; R 4 is H or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-3, where Ri is 4-methyl or 4-halo; R 2 is H, 6-methyl, or 6-halo; R 3 is H, Ci - C 3 alkyl, dimethylamino methyl; chloromethyl, or bromomethyl; R 4 is H or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, 2- tetrahydrofuryl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-3, where Rj is 4-methyl; R 2 is 6-chloro; R 3 is H; R 4 is H, OH, or methyl; and R' is isopropyl, l-hydroxy-2 -propyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2-butyl, or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4- morpholyl, 2,6-dimethyl-4-morpholyl, 2-tetrahydrofuryl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-3, where Ri is 4-chloro; R 2 is 6-methyl; R 3 is H; R 4 is H, OH, or methyl; and R' is isopropyl, l-hydroxy-2 -propyl, 2-hydroxyethyl, 2,3-dihydroxy-l -propyl, or 3,4- dihydroxy-2-butyl, or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4- morpholyl, 2,6-dimethyl ⁇ 4-morpholyl, 2-tetrahydrofuryl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-4, where Ri is 5-methyl or 4-halo; R 2 is 6-methyl or 6-halo; R 3 is H; R 4 is H, hydroxy, halo, Ci-C 6 alkyl, or Cj-C 6 alkenyl; and R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N- pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, 2-tetrahydrofuryl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-4, where Rj is 5-methyl; R 2 is H, 6-methyl, or 6-chloro; R 3 is H; R 4 is H, OH, or methyl; and R' is CpC 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4- morpholyl, 2-tetrahydrofuryl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-4, where Ri and R 2 , at positions 5 and 6, are fused benzo or pyrido; R 3 is H; R 4 is H, OH, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R 1 is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4- morpholyl, 2,6-dimethyl-4-morpholyl, 2-tetrahydrofuryl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-4, where Ri is 5-chloro; R 2 is H, 6-methyl, or 6-chloro; R 3 is H; R 4 is H, OH, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4- morpholyl, 2-tetrahydrofuryl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-5, where Ri is 3-(Ci - C 4 alkyl), 3-(Ci - C 4 alkenyl), or 3-halo; R 2 and R 3 are H; R 4 is H, vinyl, cyano, halo, hydroxy, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N- pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, 2-tetrahydrofuryl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-5, where Ri is 3-methyl or 3-halo; R 2 is 5-methyl or 5-halo; R 3 is H; R 4 is H, OH, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R' is -(CHa) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6- dimethyl-4-morpholyl, 2-tetrahydrofuryl, or 4-imidazolyl or R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, l-hydroxy-2 -propyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound according to formula IXB-5, where R] is 3-methyl; R 2 is 5-chloro; R 3 is H; R 4 is H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound according to formula IXB-5, where Ri and R 2 , at positions 2 and 3, are fused benzo, pyrido, pyrrolo, or imidazolo, optionally substituted with halogen, methyl, halomethyl, or hydroxy; R 3 is H; R 4 is H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, l-hydroxy-2- propyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound according to formula IXB-5, where Ri is 3-methyl; R 2 is 5-chloro; R 3 is H; R 4 is H, OH, or methyl; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, l-hydroxy-2 -propyl, 2,3 -dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound according to formula IXB-5, where Ri is H, 2-methyl, 2-nitro, 2-methylcarbamoyl, or 2-halo; R 2 is 3- methyl or 3-chloro, and R 3 is H, 5-methyl, or 5-chloro; R 4 is H, OH, or methyl; and R 1 is C 1 - C 6 alkyl, optionally substituted with one or two or hydroxyl groups or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, 2- tetrahydrofuryl, or 4-imidazolyl or R 1 is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 1- hydroxy-2-propyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound according to formula IXB-5, where Ri is H, 2-acetyl, 2-acetamido, 2-dimethylamino, or 2-halomethyl; R 2 is 3-methyl or 3-chloro, and R 3 is H, 5-methyl, or 5-chloro; R 4 is H or methyl; and R' is C 1 -C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-5, where R] is 3-methyl; R 2 is H or 5-chloro; R 3 is H; R 4 is H ; and R' is isopropyl, l-hydroxy-2 -propyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2 -butyl.
  • this invention provides a compound according to formula IXB-5, where Ri is H, 2-bromomethyl, 2-ethynyl, 2-cyano; R 2 is 3-chloro; R 3 is H or 5-methyl; R 4 is H or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-5, where Ri is H or 2-chloro; R 2 is 3-chloro; R 3 is H or 5-chloro; R 4 is H or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-5, where Ri is H or 2-chloro; R 2 is 3-chloro; R 3 is H or 5-chloro; R 4 is H or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6- dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound according to formula IXB-6, where Ri is H, 4-acetyl, 4-acetamido, 4-dimethylamino, 4- Ci - C 4 alkyl, alkenyl, alkynyl, or cycloalkyl, or 4-halomethyl; R 2 is H, 5-methyl or 5-halo, and R 3 is H, 6- methyl, or 6-chloro; R 4 is H, hydroxy, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-6, where Ri is 4-methyl; R 2 is H or 5-chloro; R 3 is H or 6-chloro; R 4 is H or methyl; and R' is isopropyl, l-hydroxy-2-propyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3 ,4-dihydroxy-2-butyl.
  • this invention provides a compound according to formula IXB-6, where Ri is H, 4-bromomethyl, 4-ethynyl, 4-cyano; R 2 is H, 5-methyl, or 5-chloro; R 3 is H, 6-acetyl, 6-acetoxy, 6-acetamido, or 6-methylcarbamoyl; R 4 is H, vinyl, chloromethyl, hydroxy, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound according to formula IXB-6, where Ri and R 2 , at positions 4 and 5, are fused benzo; R 3 is H or 6- methyl; R 4 is H, halo, halomethyl, hydroxy, or methyl; and R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups or R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-rmidazolyl, or R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2-butyl.
  • this invention provides a compound according to formula IXB-6, where Ri and R 2 , at positions 4 and 5, are (2,3) fused imidazolo, pyrido, or pyrrolo; R 3 is H or 6-methyl; R 4 is H, halo, halomethyl, or methyl; and R 1 is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4- imidazolyl or R 1 is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula X
  • M, Q, T, U, V, W, X, Y, and Z represent N, CH, or CRi 12> 3j or4 , where Rj - R 4 are defined as for formula I.
  • this invention provides a compound of formula XA where M, Q, T, U, V, W, X, Y, and Z are all CH or CR 1> 2> 3) Or4 .
  • this invention provides a compound of formula XB,
  • this invention provides a compound of formula XA, where R' is -(CHi) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, oxazolidinonyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrrolidinonyl, thiazolinyl, thiazol ⁇ dinyl, thiazolidinonyl, isothiazolinyl, isothiazolidinyl, isothiazolidinonyl, imidazolinyl, imidazolyl, imidazolinonyl, pyridyl, pyrazyl, pyranyl, pyridazolyl, piperidinonyl, mo ⁇ holy
  • this invention provides a compound of formula XA, where R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6- dimethyl morpholyl), 2 -tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2- on-4-yl, or 2-pyrrolidonyl.
  • this invention provides a compound of formula XA, where R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, where Ri and R 2 are both ortho substituents.
  • this invention provides a compound of formula XA, where R 4 and R 5 occupy the 3- and 5- positions.
  • this invention provides a compound of formula XA, where R] and R 2 are as defined for formula I; R 4 and R 5 are both H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl , or R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, where R] and R 2 are defined as in formula XA; R 4 and R 5 are both H; and R' is Ci-C 6 alkyl or 0-Ci-C 6 alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula XA, where Ri and R 2 are H, halo, or Ci -C 3 alkyl; R 4 and R 5 are both H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 2-halo; R 2 is 6-methyl; R 4 and R 5 are, independently, H, C 1 -C3 alkyl, or halo; and R' is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula XA, in which R] is 2-chloro; R 2 is 6-methyl; R 4 and R 5 are, independently, H, Cp C 3 alkyl, or halo; and R' is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are H; R 4 and R 5 are, independently, methyl or halo; and R 1 is isopropyl or mono- or di-hydroxy C 1 -C 4 alkyl,
  • this invention provides a compound of formula XA, in which Ri and R 2 are H; R4 and R 5 are, independently, methyl or chloro; and R' is isopropyl or mono- or di-hydroxy Ci -C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are H; R 4 and R 5 are 3-chloro and 5-methyl; and R' is isopropyl or mono- or di-hydroxy Cj -C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri and R? are H; R 5 is 2-chloro or 3-chloro; R 4 is H; and R' is isopropyl or mono- or di-hydroxy C)-C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are H; R 5 is 2-methyl or 3-methyl; R 4 is H; and R 1 is isopropyl or mono- or di-hydroxy Cj-C 4 alkyl.
  • this invention provides a compound of formula XA, in which Rj is 2-chloro; R 2 is 6-methyl; R 4 and R 5 are, independently, H, CpC 3 alkyl, or halo; and R 1 is -(CHa) n -G, where n is 1 or 2; and G is 4- imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, 1- methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl , or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • Ri is C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, or Ci-C 6 cycloalkyl
  • R 2 - R5 are H
  • R' is C)-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, where R] is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino; R 2 - R 5 are H and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, where Ri is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl; R 2 - R5 are H and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, where Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl; R 2 - R 5 are H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri and R 2 are both halogen; R 5 is 2-methyl; and R 4 is H; R 1 is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydro furyl, or pyrimidyl, or R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri and R 2 are both H; R 5 is 2-chloro; R 4 is 3-methyl; R' is -(CH 2 ) n -G, where n is 1, and G is piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, or tetrahydrofuryl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri and R 2 are both H; R 5 is 3-methyl; R 4 is 6-(2-chloroethyl); R 1 is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 2-hydroxymethyl; R 5 is 4-CF 3 ; R 2 and R 4 are H; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R 1 is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of fo ⁇ nula XA, in which Ri and R 2 are both H; R 5 is 3-methyl; R 4 is 5-chloro; and R 1 is -(CEb) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which one or both of Rj and R 2 are CF 3 ; R 4 and R 5 are H; and R' is -(CH 2 ) n -G, where n is 1, and G is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2- pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula
  • Rj is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl;
  • R 2 ; R 4 ; and R 5 are H; and
  • R' is - (CH 2 ) n -G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, pyrimidinyl, pyrrolyl, pyrroliny
  • this invention contemplates the compound of formula XA, in which Ri is 3-chloro; R 2 ; R 4 and R 5 are H; R' is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which R] is 2-chloro; R 2 is 6-methyl; R 4 and R 5 are H; R' is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which R 1 is 4-chloro; R 2 ; R 4 and R 5 are H; R' is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Ri and R 2 are 2,6-di-chloro; R 2 ; R 4 and R 5 are H; and R 1 is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Rj is 2-bromo; R 2 ; R 4 and R 5 are H; and R' is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XA, in which Ri is 3-bromo; R 2 ; R 4 and Rs are H; and R' is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XA, in which Ri is 4-bromo; R 2 ; R 4 and R 5 are H; and R 1 is -(CH 2 ) n -G, where n is 1, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XA, in which Ri is 2-, 3-, or 4-bromo; R 2 ; R 4 and R 5 are H; and R' is -(CH 2 ) n -G, where n is 1, and G is R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Ri is 4-bromo; R 2 is 2-methyl; R 5 is 3-methyl; R 4 is H, 5-methyl, or 5- halo; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Rj is 2-bromo; R 2 is 6-methyl; R 5 is 3-methyl; R 4 is H, 5-methyl, or 5- halo; and R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Ri is 3-bromo; R 2 is 6-methyl; R 5 is 3-methyl; R 4 is H, 5-methyl, or 5- halo; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Ri is 2-,chloro; R 2 is 4-chloro; R 4 and R 5 are H; and R' is -(CH 2 ) H -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Ri is 2-methyl; R 2 is 6-methyl; R 4 and R 5 are H; and R' is -(CHo) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, ⁇ iperazin-2-on-4-yl, or 2- pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which one or both of R] and R 2 are CF 3 ; R 4 and R 5 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2- tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2- pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-CF 3 ; R 2 ; R 4 and R5 are H; and R'-is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri and R 2 , in positions 2 and 6, are methyl or halogen; R 5 is 2-chloromethyl, R 4 is H; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2- piperidyl, 3-piperidyl, or 4-piperidyl or R' is isopropyl or mono- or di-hydroxy C 1 -C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 , in positions 2 and 6, are methyl or halogen; R 5 is 3-fluoromethyl; and R 4 is H; R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 2-pyrimidyl, 4-pyrimidyl, 2- morpholyl, or 3-morpholyl or R 1 is isopropyl or mono- or di-hydroxy C 1 -C 4 alkyl.
  • this invention provides a compound of formula
  • Ri and R 2 in positions 2 and 6, are methyl or halogen; R 5 is 3 -methyl; and R 4 is H; R is -(CH 2 ) n -G, where n is 1 or 2; and G is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-piperidyl, 3-piperidyl, or 4-piperidyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 , in positions 2 and 6, are methyl or halogen; R 5 is 3-fluoromethyl; and R 4 is H; R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-bromo-2-pyrimidyl, 2-chloro-4- pyrimidyl, 2-morpholyl, or 3-morpholyl.
  • this invention provides a compound of formula XA, in which Ri is 3-cyano; R 2 is H or 6-methyl; R 4 and R 5 are H or methyl; and R is - (CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl or R is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri is 3-hydroxy; R 2 is H or 6-methyl; R 4 and R 5 are H or methyl; and R is - (CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XA, in which Ri is 4-hydroxy; R 2 is H or 2-methyl; R 4 and R 5 are H or methyl; and R' is - (CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl or R is isopropyl or mono- or di-hydroxy Ci-C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4- methoxy; R 2 is H or 2-methyl; R 4 and R 5 are H or methyl; and R' is -(CHj) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methyl ⁇ iperazm-2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyI, 3-methyl-2-tetrahydrofuryl, or 2-methyl- 1-pyrimidinyl or R 1 is isopropyl or mono- or di-hydroxy C t -C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4- methoxy; R 2 is H or 2-methyl; R 4 and R 5 are H or methyl; and R' is -(CHa) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyl, 3-methyl-2 ⁇ tetrahydrofuryl, or 2-methyl- 1-pyrimidinyl or R' is isopropyl or mono- or di-hydroxy C 1 -C 4 alkyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4- ethoxymethyl; R 2 is H or 2-methyl; R 4 and R 5 are H or methyl; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l -morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l- pyrimidinyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4- methoxymethyl; R 2 is H or 2-methyl; R 4 and R 5 are H, halo, or methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 3-(2-methoxyethyl); R 2 is H, 2-methyl, or 6-methyl; R 4 and R 5 are H or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3 -methylpiperazin-2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l-morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l- pyrimidinyl or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 4-(2-methoxyethyl); R 2 is H, 2-methyl, or 6-methyl; R 4 and R 5 are H or methyl; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is 3-methyl-2-pyridyl, 3-methyl-2- piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-me&yl-2-tetrahydrofuryl, or 2-methyl-l- pyrimidinyl or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4- dimethylamino; R 2 is H or 6-methyl; R 4 and R 5 are H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4- dimethylamino; R 2 is H or 6-methyl; R 5 is 3 -methyl; R 4 are 5-methyl, 5-halo, or H; and R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4- dimethylaminocarbonyl; R 2 is H or 6-methyl; R 5 is H or 3 -methyl; R 4 is H; and R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4- methyloxycarbonyl; R 2 is H or 6-methyl; R 5 is H or 3 -methyl, R 4 is H; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4- acetyl; R 2 is H or 6-methyl, R 5 is H, 3-chloro, or 3- methyl; R 4 is H or 5-methyl; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4- acetoxy; R 2 is H or 6-methyl; R 5 is H or 3-methyl; R 4 is H or 5-chloro; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4- dimethylamino; R 2 is H or 6-methyl; R5 is H or 3- methyl; R 4 is H or 5-chloro; and R' is -(CH 2 ) H -G, where n is 1 or 2; and G is 4-imidazolyl, A- morpholyl, 4-(2,6-dimethyl morpholyl), 2-tetrahydrofuryl, pi ⁇ erazin-1-yl, 1-methyl- piperazin-4-yl, piperazin-2-on-4-yl, or 2-pyrrolidonyl, or R 1 is Cj -CO alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3- or 4-dimethylaminocarbonyl; R 2 is H or 6-methyI; R 5 is H or 3-methyl; R 4 is H or 5-chloro; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4-methyloxycarbonyl; R 2 is H or 6-methyl; R 5 is H or 3- methyl; R 4 is H or 5-chloro; and R' is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3- or 4- chloroacetyl; R 2 is H or 6-methyl; R 5 is H or 3- methyl; R 4 is H or 5-chloro; and R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3- or 4-acetoxy; R 2 is H or 6-methyl; R5 is H or 3-methyl; R 4 is H or 5-chloro; and R f is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which R] is 2-, 3- or 4- fluoromethyl; R 2 is H or 6-methyl; R 5 is H or 3- methyl; R 4 is H or 5-chloro; and R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • Ri 4-cyano
  • R 2 is H or 6-methyl
  • R 5 is H or 3-methyl
  • R 4 is H or 5-chloro
  • R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R' is - (CH 2 ) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyL pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3- or 4-ethoxy; R 2 is H or 6-methyl; R 5 is H or 3-methyl; R 4 is H or 5- chloro; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6- dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2- on-4-yl, or 2-pyrrolidonyl, or R' is C 1 -C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4-vinyl; R 2 is H or 6-methyl; R 5 is H or 3-methyl; R 4 is H or 5- chloro; and R' is -(CH 2 ) n -G, where n is 1 or 2; and G is 4-imidazolyl, 4-morpholyl, 4-(2,6- dimethyl morpholyl), 2-tetrahydrofuryl, piperazin-1-yl, l-methyl-piperazin-4-yl, piperazin-2- on-4-yl, or 2-pyrrolidonyl, or R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4-chloromethoxy; R 2 is H or 6-methyl; R 5 is H or 3-methyl; R 4 is H or 5-chloro; and R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 4-methoxy; R 2 - R 5 are H; R' is -(CH 2 ) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XA, in which Ri is 2-methyl; R 2 is 4-methylsulfonyl; R 4 and R 5 are H or methyl; and R' is - (CH 2 ) n -G, where n is 1, and G is 3-methyl-2 -isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4- oxazolyl, 3-methyl-2-pyrrolyl, 3-methyl-2 -pyridyl, or m-tolyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4-methoxy; R 2 is H or 6-methyl; R 5 is H or 3-methyl; R 4 is H or 5-chloro; and R' is -(CH 2 ) n -G, where n is 1, and G is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4-bromo; R 2 is H or 6-methyl; R 5 is H or 3-methyl; R 4 is H or 5- chloro; and R 1 is -(CHa) n -G, where n is 1, and G is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula
  • Rj is 2-chloro
  • R 2 is 3-, A-, 5-, or 6-cyclopropyl
  • R 4 and R 5 are H, halo, or methyl
  • R 1 is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 3-cyclopropyl; R 2 - R 5 are H; and R 1 is CpC 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 3-cyclopropyl; R 2 is 2-, A-, 5-, or 6-chloro; R 4 and R 5 are H; and R' is Q- Ce alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 2-chloro; R 2 is /r ⁇ r ⁇ -4-(2-methylcyclo ⁇ ropyl); R4 and R5 are H; R' is - (CH 2 ) n -G, where n is 1, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XA, in which Rj is 4-cyclopropyl; R 2 is 2- or 3-chloro; R 4 and R 5 are H, halo, or C 1 -C 3 alkyl; and R' is Cj-Cg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 4-isopropyl; R 2 is 2-chloro; R 5 is 2- or 3-chloro; R 4 is 5- or 6-methyl; and R' is -(CH 2 ) n -G, where n is 1, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl or R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which R
  • this invention provides a compound of formula XA, in which Ri and R 2 are both H; R 5 is 3-chloro; R 4 is 5- methyl; and R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups or R 1 is C]-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • Ri and R 2 are both H;
  • R 5 is 2-(2-chloroethyl);
  • R 4 is 3-methyl;
  • R' is -(CH 2 ) ⁇ -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or
  • R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula
  • R t is 2-hydroxymethyl
  • R 2 is 4-CF 3
  • R 4 and R 5 are H
  • R 1 is -(CHa) n -G, where n is 2, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula
  • Rj and R 2 are both H; R 5 is 3-chloro; R 4 is 5-methyl; and R' is -(CHa) n -G, where n is 2, and G is 3-methyl-2 -pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l- yl, 3 -methyl- 1 -piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l -morpholyl, 3-methyl-2- furyl, 3-methyl-2 -tetrahydrofuryl, or 2-methyl-l -pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which one or both of Ri and R 2 are CF 3 ; R 4 and R5 are H; R 1 is -(CHa) n -G, where n is 1 or 2; and G is 3-methyl-2 -isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3- methyl-2 -pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula XA, in which Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyi, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl; R 2 ; R 5 ; and R 4 are H; R' is - (CH 2 ) ⁇ G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, mo ⁇ holyl, furyl, tetrahydrofuryl, pyrimidinyl,
  • this invention contemplates the compound of formula XA, in which Ri is 4-chloro; Rs is 3-chloro; R 2 and R 4 are H; R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R 1 is Ci-Ce alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Ri is 2-, 3-, or 4- fluoro; R 2 , R 4 and R 5 are H; and R 1 is -(CHs) n -G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XA, in which Ri is fluoro; R 2 is methyl; R 4 and R 5 are H; R' is -(CHa) n -G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl, or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups,
  • this invention contemplates the compound of formula XA, in which Rj is 6-chloro; R 2 , R 4 and R 5 are H; R' is -(CHs) n -G, where n is 1 or 2; and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XA, in which Rj is 2-bromo; R 2 is methyl; R5; and R 4 are H; R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydroforyl, or pyrimidinyl.
  • this invention contemplates the compound of formula XA, in which Ri is 3-bromo; R 2 ; R 4 and Rs are H; R' is -(CHa) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XA, in which Ri is 4-bromo; R 2 , R 4 and R 5 are H; R' is -(CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XA, in which Ri is 2-(2-chloroethyl); R 2 is 6-chloro; R 4 and R 5 are H; R' is -(CH 2 );]- G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates the compound of formula XA, in which Ri is 4-(3-chloropropyl); R 2 is 2-bromomethyl; R 4 and R 5 are H; R 1 is - (CH 2 ) n -G, where n is 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates a compound of formula XA, in which Ri is 2-CF 3 ; R 2 , R 4 and Rs are H; R' is -(CHa) n -G, where n is 1 or 2, and G is isothiazol-4-yl, isoxazol-4-yl, oxazol-2-yl, 2-oxazolin-4-yl, oxazolidin-5-yl, or thiazol-2-yl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which R] is 4-cyano; R 2 is 2-methyl; R 4 and R 5 are H or methyl; R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 3 ⁇ methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2- on-l-yl, 3 -methyl- 1 -piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l -morpholyl, 3-methyl- 2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl- 1 -pyrimidinyl.
  • this invention provides a compound of formula XA, in which Ri is 2-methyl; R 2 is 4- or 5-hydroxy; R 4 and R 5 are H or methyl; R' is -(CH 2 ) n - G, where n is 1 or 2, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin- 2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l-morpholyl, 3- methyl-2-ruryl, 3-methyl-2-tetrahydrofuryl, or 2-methyl- l ⁇ pyrimidinyl, or R' is Cj-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Rj is 2-hydroxymethyl; R 2 - R 5 are H; R' is -(CH 2 )D-G, where n is 2, and G is 3-methyl-2- ⁇ yridyl, 3-methyl-2-piperazinyl, 3-methylpi ⁇ erazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl- 1-pyrirm ' dinyl, or R' is CpCg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 2-methoxy; R 2 is H, halo, or methyl; R 4 and R 5 are H or methyl; R 1 is -(CH 2 ) n - G, where n is 2, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2- on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l-morpholyl, 3-methyl- 2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl- 1-pyrimidinyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention provides a compound of formula XA, in which Ri is 4-methoxy; R 2 - Rs are H; R' is -(CH 2 ) n -G, where n is 2, and G is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2- ⁇ iperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-fuiyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl- 1-pyrimidinyl.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4-dimethylamino; R 2 , R 4 , and R 5 are H; R' is -(CH 2 ) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl, or R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Rj is 2-, 3-, or 4-dimethylaminocarbonyl; R 2 is H or 6-methyl, ; R 4 and R5 are H, halo, or methyl; and R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl, or R 1 is Ci-C 6 alkyl, optionally substituted with one or two or
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4-methyloxycarbonyl; R 2 is H, 6-methyl, or 6-halo; ; R 4 and R 5 are H, halo, or methyl; and R' is -(CH 2 ) H -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl, or R' is C]-C 6 alkyl, optionally substituted with one or two or
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4-acetyl; R 2 , R 4 , and R 5 are H; and R' is Ci-Cg alkyl, optionally substituted with one or two or hydroxyl groups.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4-acetoxy; R 2 , R 4 , and R 5 are H; and R' is -(CH 2 ) n -G, where n is 2, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XA, in which Ri is 4-dimethylamino; R 2 is 2-methyl; R 4 and R 5 are H or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XA, in which Ri is 4-dimethylaminocarbonyl; R 2 is 2-methyl; ; R 4 and R5 are H or methyl; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6- dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention contemplates a compound of formula XA, in which Rj is 4-methyloxycarbonyl; R 2 is H or methyl; ; R 4 and R 5 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4- morpholyl, or 4-imidazolyl.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4-acetyl; R 2 , R 4 , and R 5 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4- imidazolyl.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4-acetoxy; R 2 ; R5; and R 4 are H; and R 1 is -(CEk) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4- imidazolyl.
  • this invention contemplates a compound of formula XA, in which Ri is 2-, 3-, or 4-CH 2 F; R 2 ; R 4; and R 5 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4- imidazolyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4-cyano; R 2 - R 5 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula
  • R is 2-, 3-, or 4-ethoxy
  • R 2 - R 4 are H
  • R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula
  • R] is 2-, 3-, or 4-trifluoromethoxy
  • R 2 - R 5 are H
  • R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl-4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4-chloromethoxy; R 2 - R5 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrrolidinonyl, morpholyl, or imidazolyl.
  • this invention provides a compound of formula XA, in which Ri is 2-, 3-, or 4-methoxy; R 2 - R 5 are H; and R 1 is -(CH 2 ) n -G, where n is 1 or 2, and G is 5-oxazolidinyl, 4-thiazolyl, 3-thienyl, 2-furyl, 3-pyrrolyl, 2-pyrrolidinyl, N- pyrrolidinonyl, N-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula
  • Ri is 3- or 4-methylsulfonyl
  • R 2 is 2-(2-methyl cyclopropyl);
  • R 4 and R 5 are H; and
  • R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 3-methyl-2-isothiazolyl, 3-methyl-2- isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2-pyrrolyl, 3-methyl-2-pyridyl, N-pyrrolidonyl, or m-tolyl.
  • this invention provides a compound of formula
  • Ri is 2-, 3-, or 4-methoxy
  • R 2 - R 5 are H
  • R' is -(CH 2 ) n -G, where n is 1 or 2, and G is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2- yi.
  • this invention provides a compound of formula XA, in which Ri is 4-bromo or 4-bromomethyl; R 2 - R 5 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula XA, in which Ri is 2- or 3-chloro; R 2 is 4-(2-cyclopropylethyl); R 4 and R 5 are H; and R' is - (CH 2 ) n -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XA, in which Ri is cyclopropyl or cyclopropylmethyl; R 2 - R 5 are H; and R 1 is -(CH 2 ) n -G, where n is 1 or 2, and G is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XA, in which Ri is £rar ⁇ -3-(2-methylcyclopropyl); R 2 is 6-chloro; R 4 and R5 are H; and R' is -(CH 2 ) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-mo ⁇ holyl, 2,6-dimethyl-4- morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula XA, in which R 1 is 3- or 4-cyclopropyl; R 2 is 5-chloro; R 5 is 2-(2-fluoroethyl); and R 4 is H; and R' is -(CHa) n -G, where n is 1 or 2, and G is N-pyrrolidinonyl, 4-morpholyl, 2,6-dimethyl- 4-morpholyl, or 4-imidazolyl.
  • this invention provides a compound of formula
  • Ri 2- or 3-cyclopropyl
  • R 2 is 6-chloro
  • R 5 is 3-chloro
  • R 4 is 5-methyl
  • R' is -(CH 2 ) n -G, where n is 1 or 2, and G is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- mo ⁇ holyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryI, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XA, in which
  • Ri and R 2 are halogen or methyl; R 4 and R 5 are H; and R' is methyl, ethyl, isopropyl, or sec- butyl
  • this invention provides a compound of formula XA, in which Rj is halogen or methyl; R 2 -Rs are H; and R' is methyl, ethyl, isopropyl, or sec- butyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are halogen or methyl; R 4 and Rs are H; and R f is 1,2-chloropropan- 3-yl.
  • this invention provides a compound of formula XA, in which Rj and R 2 are halogen or methyl; R 4 and R 5 are H; and R' is 1-hydroxy-butan- 3-yl.
  • this invention provides a compound of formula XA, in which Ri is bromo; R 2 -Rs are H; and R' is isopropyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are halogen or methyl; R 4 and R 5 are H; and R' is 1,2-dihydroxy- propan-3-yl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are halogen or methyl; R 4 and R 5 are H; and R' is 2-hydroxyethyl. In another more specific embodiment, this invention provides a compound of formula XA, in which Ri and R 2 are halogen or methyl; R 4 and R 5 are H; and R' is 4-hydroxybutyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are halogen or methyl; R 4 and R 5 are H; and R' is 1,2- dihydroxybutan-4-yl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are halogen or methyl; R 4 and R 5 are C]-C 6 alkyl; and R 1 is 1,2- dihydroxybutan-3 -yl .
  • this invention provides a compound of formula XA, in which Ri and R 2 are halogen or methyl; R 4 and R 5 are H; and R' is 4-methoxybutyl.
  • this invention provides a compound of formula XA, in which Ri and R 2 are halogen or methyl; R 4 and R 5 are H; and R' is 3-hydroxypropyl.
  • this invention provides a compound of formula XA, where Ri and R 2 are fused cyclohexyl or fused cyclopentyl; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l -propyl, or 3,4-dihydroxy-2- butyl.
  • this invention contemplates a compound of formula XA, where Ri and R 2 , at positions 3 and 4, are fused (4,5)-imidazolo; R 4 and R5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2-Butyl.
  • this invention contemplates a compound of formula XA, where Ri and R 2 , at positions 3 and 4, are fused (2,3)-furyl; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2-butyl.
  • this invention contemplates a compound of formula XA, where Ri and R 2 , at positions 3 and 4, are fused (2,3)-pyrido; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2-butyl. . ,,,,,
  • this invention contemplates a compound of formula XA, where Rj and R 2 , at positions 3 and 4, are fused (3,4)pyrrolyl; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2 -butyl.
  • this invention contemplates a compound of formula XA, where Rj and R 2 , at positions 2 and 3, are fused cyclopentyl; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2 -butyl.
  • this invention contemplates a compound of formula XA, where R] and R 2 , at positions 3 and 4, are fused cyclopentyl; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4- dihydroxy-2-butyl.
  • this invention contemplates a compound of formula XA, where Ri and R 2 , at positions 2 and 3, are benzo; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2- butyl.
  • this invention contemplates a compound of formula XA, where Ri and R 2 , at positions 2 and 3, are benzo, substituted at one or both ortho positions; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention contemplates a compound of formula XA, where R] and R 2 , at positions 3 and 4, are benzo; R 4 and R 5 are H; and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2- butyl.
  • this invention provides aza-substituted compounds of the types shown below, where substituents Ri - R 5 and R' are as defined above.
  • this invention provides a compound of formula XI below,
  • the dashed bond represents an optional double bond
  • symbols L, T, U, V, and W- Z represent N, CH, or CRi 1 2, o r 4 , provided that no two nitrogen atoms are adjacent
  • Ri - R 4 are, independently, hydrogen; halogen; hydroxy; nitro; cyano; Ci-C 6 alkyl ; 0-Cj-C 6 alkyl; C 2 -C 6 alkenyl; C 2 -C 6 alkynyl; C 1 -C 6 cycloalkyl; 2-methoxy ethenyl; CH 3 OC(O); CH 3 CH 2 OC(O); Cj-C 5 alkyl-C(O)-; Ci-C 5 alkyl-C(O)O-; -NR 6 R 7 , -CH 2 NR 6 R 7 , -NH-C(O)- R 6 , -C(O)NR 8 R 9 ; CH 3 S(O) 2 -, Or-S(O) 2
  • the invention provides a compound of formula XIA-I,
  • this invention provides a compound of formula XIA- 1, where Ri - R 4 are as described above for formula I, and where R' is Ci-C 6 alkyl, optionally substituted with one or two or hydroxyl groups, or R 1 is -(CH 2 ) n -G, where n is 1 or 2; and G is isothiazolyl, isoxazolyl, isoxazolidinyl, isoxazolidinonyl, oxazolyl, oxazolinyl, oxazolidinyl, oxazolidinonyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrrolidinonyl, thiazolinyl, thiazolidinyl, thiazolidinonyl, isothiazolinyl, isothiazolidinyl, isothiazolidinonyl, isothiazol
  • this invention provides a compound of formula XIA-I, where R 3 and R 4 are both H and R' is C)-C 6 alkyl or 0-Ci-C 6 alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula XIA-I, where R 2 - R 5 are H and R' is Cj-C 6 alkyl, optionally substituted with halogen, C 1 -C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIA-I, where R] is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 2 - R 4 are H and R' is C]-C 6 alkyl, optionally substituted with halogen, CpC 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIA-I, where Ri is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or ammosulfonyl, R 2 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula
  • XIA-I in which Ri and R 2 are both halogen, R 3 is 2-methyl, and R 4 is H, R 1 is -(CHs) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates a compound of formula XIA- 1 , where Ri - R 4 are H and R 1 is 2-(2-furyl)ethyl, 2-hydroxyethyl, or 2,3-dihydroxy- 1- propyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 together, at positions 3 and 4, are fused cyclopentyl, R 3 and R 4 are H, and R' is isopropyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 together, at positions 3 and 4, are benzo, R 3 and R 4 are H, and R 1 is isopropyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 together, at positions 3 and 4, are 2,3-pyrido, R 3 and R 4 are H, and R' is isopropyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 together, at positions 3 and 4, are 2,3-pyrrolo, R 3 and R 4 are H, and R' is isopropyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 together, at positions 4 and 5, are fused (2,3)-furyl, R 3 and R 4 are H, and R 1 is l,2-dihydroxy-propan-3-yl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 together, at positions 3 and 4, are fused (2,3) thienyl, R 3 and R 4 are H, and R' is 2-hydroxyethyl.
  • this invention provides a compound of formula XIA-I, in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula
  • XIA-I in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-(2-chloroethyl), R' is -(CH 2 ) n - B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 4-CF 3 , R 3 is 2-hydroxymethyl, R 2 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, R' is -(CH 2 ) n -B, where n is 1, and B is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3- methyl-1-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl- 1-morpholyl, 3-methyl-2-furyl, 3- methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl- 2-pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula
  • R] is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl; R 2 , R 3 , and R 4 are H, R' is - (CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, pyrimidinyl, pyrrolyl, pyrrolinyl,
  • this invention contemplates the compound of formula XIA-I, in which Ri is 2-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 3-chloro, R 2 , R 3 , and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 4-chloro, R 2 , R 3 , and R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 5-chloro, R 2 , R 3 , and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 3-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 4-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 5-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA- 1 , in which Ri is 2-chloro, R 2 is 4- chloro, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 3-chloro, R 2 is 4-chloro, R 3 and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention contemplates a compound of formula XIA- 1 , in which Ri is 3-CF 3 , R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1 , and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-cyano, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-hydroxy, R 2 - R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1- piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l-mo ⁇ holyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Rj is 4-hydroxy, R 2 - R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3 -methyl- 1- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-methoxy, R 2 - R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydro furyl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 4-methoxy, R 2 - R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-dimethylamino, R 25 R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-dimethylaminocarbonyl, R 2 , R 3 , and R 4 are H 5 R' is -(CH 2 ) n - B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-methyloxycarbonyl, R 2 , R 3 , and R 4 are H, R' is -(CHa) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Rj is 3-acetyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-acetoxy, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-dimethylamino, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-dimethylaminocarbonyl, R 2 , R 3 , and R 4 are H, R 1 is -(CH 2 ) n - B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-methyloxycarbonyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-acetyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-acetoxy, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-CH 2 F, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-cyano, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-ethoxy, R 2 - R 4 are H, R' is -(CH 2 ) H -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which R) is 4-ethoxy, R 2 - R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Rj is 3-chloromethoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 4-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) I i-B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 2-methyl, R 2 is 4-methylsulfonyl, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2-pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 4-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula XIA-I, in which R] is 4-bromo, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-cyclopropyl, R 2 is 4-chloro, R 3 and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-cyclopropyl, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which R t is 3-cyclopropyl, R 2 is 4-chloro, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is £r ⁇ «,y-3-(2-methylcyclopropyi), R 2 is 4-chloro, R 3 and R 4 are H, R' is - (CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Rj is 3-cyclopropyl, R 2 is 4-chloro, R 3 is 2-(2-fluoroethyl), and R 4 is H, R is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-cyclopropyl, R 2 is 4-chloro, R 3 is 2-chloro, R 4 is 2-fluoro, R' is - (CH 2 ) n -B, where n is 1, and B is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3-methyl-l-piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- mo ⁇ holyl, 3-methyl-2-furyl, 3-methyl-2-tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which R] and R 2 are both halogen, R 3 is 2-methyl, and R 4 is H, R 1 is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-(2-chloroethyl), R is -(CH 2 ),,- B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula
  • XIA-I in which Ri is 4-CF 3 , R 3 is 2-hydroxymethyl, R 2 and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula
  • XIA-I in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, R' is -(CH 2 ) n -B, where n is 2, and B is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3- methyl-1 -piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl- 1 -morpholyl, 3-methyl-2-furyl, 3- methyl-2 -tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula
  • XIA-I in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, R is -(CH 2 ) n -B, where n is 2, and B is 3-methyl-2-isothiazolyl, 3-methyl-2 -isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl- 2-pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula XIA-I, in which Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl; R 2 , R 3 , and R 4 are H, R' is - (CH 2 )[ I -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, pyrimidiny
  • this invention contemplates the compound of formula XIA-I, in which Ri is 2-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 3-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 4-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 5-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 3-bromo, R 2 , R 3 , and R 4 are H, R' is -(CHi) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 4-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) H -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, fiiryl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I 3 in which Ri is 5-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 2-chloro, R 2 is 4- chloro, R 3 and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates the compound of formula XIA-I, in which Ri is 3-chloro, R 2 is 4-chloro, R 3 and R 4 are H, R' is -(CHa) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-CF 3 , R 25 R 3 , and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-cyano, R 2 - R 4 are H, R' is -(CHa) n -B, where n is 2, and B is 3- methyl-2-pyridyl, 3-methyl-2- ⁇ iperazinyI, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which R 1 is 3-hydroxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 4-hydroxy, R 2 - R 4 are H, R is -(CH 2 ) n -B, where n is 2, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 4-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidinyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-dimethylamino, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-dimethylaminocarbonyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n - B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-methyloxycarbonyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-acetyl, R 2 , R 3 , and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-acetoxy, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-dimethylamino, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-dimethylaminocarbonyl, R 2 , R 3 , and R 4 are H, R is -(CEb) n - B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-methyloxycarbonyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-acetyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-I , in which Ri is 4-acetoxy, R 2 , R 3 , and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA- 1 , in which Ri is 3-CH 2 F, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-cyano, R 2 - R 4 are H, R' is -(CHo) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which R 1 is 3-ethoxy, R 2 - R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 4-ethoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I 5 in which Ri is 3-chloromethoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Rj is 4-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-I, in which Ri is 2-methyl, R 2 is 4-methylsulfonyl, R 3 and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2-pyrrolyl, 3-methyl-2 -pyridyl, or m-tolyl.
  • this invention provides a compound of formula
  • XIA-I in which Ri is 4-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula XIA-I, in which Ri is 4-bromo, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula XIA-I, in which Ri is 3-cyclopropyl, R 2 is 4-chloro, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-I, in which R 1 is 3-cyclopropyl, R 2 - R 4 are H, R !
  • n 2 -B
  • B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula
  • R 1 is 3-cyclopropyl
  • R 2 is 4-chloro
  • R 3 and R 4 are H
  • R' is -(CH 2 ) n -B, where n is 2
  • B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula
  • XIA-I in which Ri is trans-3 -(2-T ⁇ eth.ylcyclopropyl), R 2 is 4-chloro, R 3 and R 4 are H, R 1 is - (CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula
  • XIA-I in which Ri is 3-cyclopropyl, R 2 is 4-chloro, R 3 is 2-(2-fluoroethyl), and R 4 is H, R 1 is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula
  • XIA-I in which Ri is 3-cyclopropyl, R 2 is 4-chloro, R 3 is 2-chloro, R 4 is 2-fluoro, R' is - (CH 2 ) n -B, where n is 2, and B is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1 -piperidinyl, 3-methyl-2-piperidinonyl, 3-methyl-l- morpholyl, 3-methyl-2-furyl, 3-methyl-2 -tetrahydrofuryl, or 2-methyl-l -pyrimidinyl.
  • this invention provides a compound of formula
  • this invention provides a compound of formula XIA-I, in which Ri and R 2 are halogen, R 3 and R 4 are H, and R' is ethyl. In another more specific embodiment, this invention provides a compound of formula XIA-I, in which Rj and R 2 are halogen, R 3 and R 4 are H, and R 1 is l,2-chloropropan-3-yl.
  • this invention provides a compound of formula XIA-I, in which Ri and R 2 are halogen, R 3 and R 4 are H, and R' is l-hydroxy-butan-3-yl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-(methylcarbamoyl), R 2 is 5-fluoro, R 3 and R 4 are H, and R 1 is isopropyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-acetamido, R 2 is 5-fluoro, R 3 and R 4 are H, and R 1 is 1,2- dihydroxy-propan-3-yl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 are 4-fluoro and 5-fluoro, R 3 and R 4 are H, and R' is 2- hydroxyethyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 are 4-chloro and 5-chloro, R 3 and R 4 are H, and R' is 4- hydroxybutyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 are 4-fluoro and 5-fluoro, R 3 and R 4 are H, and R 1 is 4- hydroxybutyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 2-methoxymethyl, and R 2 is 3-chloro, R 3 and R 4 are H, and R' is l,2-dihydroxybutan-4-yl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 2-ethoxymethyl, and R 2 is 3-chloro, R 3 and R 4 are H, and R' is l,2-dihydroxybutan-3-yl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-methoxymethyl, R 2 is 4-chloro, R 3 and R 4 are H, and R 1 is 1 ,2-dihydroxybutan-4-yl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-nitro, R 2 is 4-methoxy, R 3 and R 4 are H, and R 1 is 1,2- dihydroxybutan-3-yl..
  • this invention contemplates a compound of formula XIA-I, in which Ri is 5-nitro, R 2 - R 4 are H, and R 1 is 4-hydroxybutyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-cyano, R 2 - R 4 are H, and R' is 4-hydroxybutyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 3-(2-methoxyethenyl), R 2 - R 4 are H, and R 1 is 4- hydroxybutyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri is 4-cyano, R 2 - R 4 are H, and R is 4-hydroxybutyl.
  • this invention contemplates a compound of formula XIA-I, in which Ri and R 2 are 3-chloromethyl and 4-chloromethyl, R 3 and R 4 are H, and R' is 3-hydroxypropyl.
  • this invention provides a compound of formula XIA-2, where Ri-R 1 are defined as for formula I.
  • this invention provides a compound of formula XIA- 2 where Ri - R 4 are H and R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-2 where Ri - R 4 are H and R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA-2 where Ri - R 4 are H and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-1 -propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula XIA-
  • Ri - R 4 are H and R' is isopropyl, 2-butyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-1 -propyl, or 3,4-duhydroxy-2-butyl.
  • this invention provides a compound of formula XIA-2, where Ri is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 2 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIA-2, where Ri is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl, R 2 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with halogen, C]-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIA- 2, where Ri is 4-acetyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIA-2, where Ri is 4-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is 3- methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2-pyrrolyl, 3- methyl-2-pyridyl, or m-tolyl.
  • this invention contemplates a compound of formula XIA-2, where R 1 is 5-bromo, R 2 and R 3 are H, R 4 is 2-fluoro, R' is -(CH 2 ) n -B, where n is 2, and B is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3- methyl-2-pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention contemplates a compound of formula XIA-2, where Ri is 5-cyano, R 2 is H, R 3 is 2-trifluoromethyl, R 4 is 2-fluoro, R 1 is - (CH 2 ) n -B, where n is 1, and B is 5-methyl-2-furyl, 5-methyl-2-pyrrolyl, or 3-pyrrolyl.
  • this invention contemplates a compound of formula XIA-2, where Ri is 4-fluoro, R 2 is 5-fluoro, R 3 is 3-acetamido, R 4 is 2-fluoro, R' is - (CH 2 ) n -B, where n is 1, and B is 5-methyl-2-furyl, 5-methyl-2-pyrrolyl, or 3- ⁇ yrrolyl.
  • this invention contemplates a compound of formula
  • Ri - R 4 are H and R 1 is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates a compound of formula XIA-2 where Ri - R 4 are H and R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention contemplates a compound of formula XIA-2 where Ri - R 4 are H and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3- dihydroxy-1 -propyl, or 3,4-duhydroxy-2-butyl.
  • this invention contemplates a compound of formula XIA-2, where Ri and R 2 together, at positions 3 and 4, are fused cyclopentyl, R 3 and R 4 are H, and R' is l-hydroxy-butan-3-yl.
  • this invention contemplates a compound of formula XIA-2 in which Ri and R 2 together, at positions 3 and 4, are fused cyclopentyl, R 3 and R 4 are H, and R' is isopropyl.
  • this invention contemplates a compound of formula XIA-2 in which R 1 and R 2 together, at positions 4 and 5, are fused (2,3)-furyl, R 3 and R 4 are H, and R' is l,2-dihydroxy-propan-3-yl.
  • this invention contemplates a compound of formula XIA-2 in which Ri and R 2 together, at positions 3 and 4, are fused (2,3) thienyl, R 3 and R 4 are H, and R' is 2-hydroxyethyl.
  • this invention contemplates a compound of formula XIA-2 in which Ri and R 2 together, at positions 3 and 4, are fused cyclopentyl, R 3 and R 4 are H, and R is 4-hydroxybutyl.
  • this invention provides a compound of formula
  • XIA-2 where Ri is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 2 - R 4 are H and R' is Ci-C 6 alkyl, optionally substituted with halogen, C]-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIA-2, where Rj is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl, R 2 - R 4 are H and R' is Cj-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention contemplates a compound of formula XIA-2, where Ri and R 2 together, at positions 3 and 4, are fused cyclopentyl, R 3 and R 4 are H, and R' is l-hydroxy-butan-3-yl.
  • this invention contemplates a compound of formula XIA-2 in which Ri and R 2 together, at positions 3 and 4, are fused cyclopentyl, R 3 and R 4 are H, and R is isopropyl.
  • this invention contemplates a compound of formula XIA-2 in which Ri and R 2 together, at positions 4 and 5, are fused (2,3)-furyl, R 3 and R 4 are H, and R is l,2-dihydroxy-propan-3-yl.
  • this invention contemplates a compound of formula XIA-2 in which Ri and R 2 together, at positions 3 and 4, are fused (2,3) thienyl, R 3 and R 4 are H, and R' is 2-hydroxyethyl.
  • this invention contemplates a compound of formula XIA-2 in which Rj and R 2 together, at positions 3 and 4, are fused cyclopentyl, R 3 and R 4 are H, and R' is 4-hydroxybutyl.
  • this invention contemplates a compound of formula XIA-2 in which Ri and R 2 together are fused furyl, R 3 and R 4 are H, and R' is 1,2- dihydroxybutan-4-yl.
  • this invention contemplates a compound of formula XIA-2 in which Ri and R 2 together are fused cyclopentyl, R 3 and R 4 are H, and R is 1 ,2-dihydroxybutan-4-yl.
  • this invention contemplates a compound of formula
  • XIA-2 in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-(2-chloroethyl), R' is -(CH 2 ) n - B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIA- 2 in which R] is 4-CF 3 , R 3 is 2-hydroxymethyl, R 2 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIA-2 in which Ri is 3-CH 2 F, R 2 is 5-cyano, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula B, where RpR' are defined as for formula A, where the dashed line represents an optional double bond, and where symbols L, T, U, V, and W- Z represent N, CH, or CRi, 2 , or 4, provided that at least one of L, T, U, V, and W- Z is N, and further provided that no two nitrogen atoms are adjacent. isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, l-hydroxy-2-propyl, 2,3-dihydroxy-l-propyl, or 3 ,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula XIB-I where one of Ri and R 2 is H and the other is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino; R 3 - R 4 are, independently, H, chloro, methyl, or hydroxy; and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIB-I, where one of Ri and R 2 is H and the other is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl; R 3 - R 4 are, independently, H, chloro, methyl, or hydroxy; and R' is Ci-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIB-I, where Ri and R 2 are fused cyclohexyl or fused cyclopentyl, R 3 and R 4 are, independently, H, chloro, methyl, or hydroxy; and R' is isopropyl, 2-(2-furyl)ethyl, 2- hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula XIB-I, where Ri and R 2 are fused benzo; R 3 and R 4 are, independently, H, chloro, methyl, or hydroxy; and R is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2-butyl.
  • this invention provides a compound of formula XIB-I, wherein Ri and R 2 are, independently, H or halogen, R 3 and R 4 are H, and R' is isopropyl, 2-(2-furyl)ethyl, 2-hydroxyethyl, 2,3-dihydroxy-l-propyl, or 3,4-dihydroxy-2- butyl.
  • this invention provides a compound of formula XIB- 1, where R] - R 3 are H, R 4 is 2-halo, 2-cyano, 2-hydroxy, or 2-methoxy, and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is 4-methyl-l-piperazinyl, 1-piperidinyl, piperidinonyl, 4-morpholyl, 2,6-dimethyl ⁇ 4-morpholyl, 2-furyl, 2-tetrahydrofuryl, 1-pyrrolidonyl, or pyrirnidinyl.
  • this invention provides a compound of formula XIB-
  • this invention provides a compound of formula XIB- 1, where Rj-R 4 are, independently, H, C 1 -C 6 alkyl, hydroxy, or halogen, and R 1 is -(CHa) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, 1- pyrrolidonyl, 2,6-dimethyl-4-morpholyl, 4-morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • this invention provides a compound of formula XIB-I, where Rj-R 4 are, independently, H, C 1 -C 6 alkyl, hydroxy, or halogen, and R' is Ci - C 4 alkyl, optionally substituted with one or two halogen atoms, hydroxy groups, or Ci-C 3 alkoxy groups.
  • this invention provides a compound of formula
  • Rj-R 4 are, independently, H, Ci-C 4 alkyl, hydroxy, or halogen, and R' is
  • this invention provides a compound of formula XIB-I, where Ri is halo, R 2 - R 4 are H and R' is -(CH 2 ) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidinyl.
  • the invention contemplates a compound of formula XIB-I, where R] is chloro or bromo; R 2 - R 4 are H; and R 1 is isopropyl, 2- hydroxyethyl, l-hydroxy-2-propyl, or 2,3 -dihydroxy-1 -propyl.
  • this invention provides a compound of formula XIB-2,
  • this invention provides a compound of formula XIB- 2, where Ri-R 4 are, independently, H or halogen, and R is isopropyl, 2-(2-furyl)ethyl, 2- hydroxyethyl, 2-methoxyethyl, l-hydroxy-2-propyl, l,2-dihydroxy-3 -propyl, or 3,4- dihydroxy-2 -butyl.
  • this invention provides a compound of formula XIB-2, where one of Ri and R 2 is H and the other is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 3 - R 4 are H, and R' is CpC 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula
  • Ri and R 2 are H and the other is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl
  • R 3 - R 4 are H and R 1 is Cj-C 6 alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIB-2, where Ri and R 2 are H, R 3 is methyl, methoxy, acetamido, or acetyl, R 4 is nitro, cyano, halo, halomethyl, dimethylamino, or methylaminocarbonyl, and R' is -(CHV) n -B, where n is 1 or 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates a compound of formula XIB-2, where Ri and R 2 are fused cyclohexyl or are both H, R 3 and R 4 are H, and R 1 is isopropyl or l-hydroxy-2-propyl.
  • this invention provides a compound of formula XII below, where the dashed bond represents an optional double bond, and where symbols T - Z represent N, CH, or CR 1 , 2> or 4 , that at most two of W, X, Y, and Z and at most 2 of T, U, and V are N;
  • Ri - R 4 are, independently, hydrogen; halogen; hydroxy; nitro; cyano; Ci-C 6 alkyl ; O- CpC 6 alkyl; C 2 -C 6 alkenyl; C 2 -C 6 alkynyl; Ci-C 6 cycloalkyl; 2-methoxy ethenyl; CH 3 OC(O); CH 3 CH 2 OC(O); Ci-C 5 alkyl-C(O)-; Ci-C 5 alkyl-C(O)O-; -NR 6 R 7 , -CH 2 NR 6 R 7 , -NH-C(O)- R 6 , -C(O)NR 8 Rg; CH 3 S(O) 2 -, Or-S(O) 2 NR 8 R 9 , where R 6 - R 9 are, independently, H or C 1 -C 4 alkyl; or any of the pairs Ri and R 2 , R 6 and R 7 , or Rs and Rg are attached to adjacent carbons and
  • this invention provides a compound of formula XIIA- 1,
  • this invention provides a compound of formula XIIA-
  • R 3 and R 4 are both H and R' is -(CH 2 ) n -B, where n is 1 or 2 and B is defined as above.
  • this invention provides a compound of formula XIIA-I where R 1 is Ci-C 6 alkyl or 0-Ci-C 6 alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula XIIA-I where R 3 and R 4 are both H and R' is Ci-C 6 alkyl or 0-Cj-C 6 alkyl, both optionally substituted as described above.
  • this invention provides a compound of formula
  • this invention provides a compound of formula XIIA-I, where R] is amino, methyl amino, dimethylamino, dimethylaminomethyl, or acetylamino, R 2 - R 4 are H and R 1 is Ci-C 6 alkyl, optionally substituted with halogen, C 1 -C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIIA-I, where Ri is nitro, cyano, methylcarbamoyl, dimethylcarbamoyl, or aminosulfonyl, R 2 - R 4 are H and R' is C 1 -Cg alkyl, optionally substituted with halogen, Ci-C 3 alkoxy, or hydroxy.
  • this invention provides a compound of formula XIIA-I in which Ri and R 2 are both halogen, R 3 is 2-methyl, and R 4 is H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, orpyrimidyl.
  • this invention provides a compound of formula XIIA-I in which R 1 and R 2 are both H 3 R 3 is 3-methyl, R 4 is 2-chloro, R' is -(CH 2 ) ⁇ -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula
  • XIIA-I in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-(2-chloroethyl), R 1 is -(CH 2 ) n - B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 4-CF 3 , R 3 is 2-hydroxymethyl, R 2 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIIA-I in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, R' is -(CHj) n -B, where nis 1, and B is 3-methyl-2 -pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3- methyl-1 -piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1 -morpholyl, 3-methyl-2-furyl, 3- methyl-2 -tetrahydrofuryl, or 2-methyl-l -pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl- 2-pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula
  • Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl; R 2 , R 3 , and R 4 are H, R 1 is - (CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, pyrimidyl, pyrrolyl, pyrrolinyl, pyrrolinyl, thi
  • this invention contemplates the compound of formula XIIA-I in which Ri is 2-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 3-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 4-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 5-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 3-bromo, R 2 , R 3 , and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which R] is 4-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 5-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 2-chloro, R 2 is 4- chloro, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 3-chloro, R 2 is 4-chloro, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 3-CF 3 , R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention provides a compound of formula XIIA-I in which R] is 3-cyano, R 2 - R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-hydroxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 4-hydroxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl- 1 -pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-mo ⁇ holyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 4-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-mo ⁇ holyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 3-dimethylamino, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 3-dimethylaminocarbonyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n - B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 3-methyloxycarbonyl, R 2 , R 3 , and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 3-acetyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 3-acetoxy, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 4-dimethylamino, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 4-dimethylaminocarbonyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n - B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 4-methyloxycarbonyl, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) U -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which R 1 is 4-acetyl, R 2 , R 3 , and R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 4-acetoxy, R 2 , R 3 , and R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention contemplates a compound of formula XIIA-I in which Ri is 3-CH 2 F, R 2 , R 3 , and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-cyano, R 2 - R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-ethoxy, R 2 - R 4 are H, R is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 4-ethoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-chloromethoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIIA-I in which Rj is 4-methoxy, R 2 - R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 2-methyl, R 2 is 4-methylsulfonyl, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is 3-methyl-2-isothiazolyl, 3-methyl-2 -isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl-2-pyrrolyl, 3-methyl-2 -pyridyl, or m-tolyl.
  • this invention provides a compound of formula
  • XIIA-I in which Ri is 4-methoxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula XIIA-I in which Ri is 4-bromo, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is cyclopentyl, cyclopenten-3-yl, cyclopentadien-4-yl; cyclohexyl, or cyclohexen-2-yl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-cyclopropyI, R 2 is 4-chloro, R 3 and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-cyclopropyl, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 1, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula
  • Rj is 3-cyclopropyl
  • R 2 is 4-chloro
  • R 3 and R 4 are H
  • R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula
  • XIIA-I in which Ri is ⁇ ra?w-3-(2-methylcyclo ⁇ ropyl), R 2 is 4-chloro, R 3 and R 4 are H, R' is - (CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula
  • XIIA-I in which Ri is 3-cyclopropyl, R 2 is 4-chloro, R 3 is 2-(2-fluoroethyl), and R 4 is H, R' is -(CH 2 ) n -B, where n is 1, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula
  • XIIA-I in which Ri is 3-cyclopropyl, R 2 is 4-chloro, R 3 is 2-chloro, R 4 is 2-fluoro, R 1 is - (CH 2 ) n -B, where n is 1, and B is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3- methylpiperazin-2-on-l-yl, 3 -methyl- 1 -piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1- morpholyl, 3-methyl-2-furyl, 3 -methyl-2 -tetrahydrofuryl, or 2-methyl-l -pyrimidyl.
  • this invention provides a compound of formula
  • XIIA-I in which Ri and R 2 are both halogen, R 3 is 2-methyl, and R 4 is H, R' is -(CEb) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-(2-chloroethyl), R 1 is -(CH 2 ) n - B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 4-CF 3 , R 3 is 2-hydroxymethyl, R 2 and R 4 are H, R' is -(CH 2 ) ⁇ -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, or phenyl.
  • this invention provides a compound of formula XIIA-I in which Ri and R 2 are both H, R 3 is 3-methyl, R 4 is 2-chloro, R' is -(CHa) n -B, where n is 2, and B is 3-methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3- methyl-1 -piperidinyl, 3-methyl-2- ⁇ iperidinonyl, 3 -methyl- 1 -morpholyl, 3-methyl-2-furyl, 3- methyl-2 -tetrahydrofuryl, or 2-methyl-l -pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is 3-methyl-2-isothiazolyl, 3-methyl-2-isoxazolyl, 3-methyl-4-oxazolyl, 3-methyl- 2-pyrrolyl, 3-methyl-2-pyridyl, or m-tolyl.
  • this invention provides a compound of formula XIIA-I in which Ri is isothiazolyl, isoxazolyl, oxazolyl, oxazolidyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl; R 2 , R 3 , and R 4 are H, R 1 is - (CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, pyrimidy
  • this invention contemplates the compound of formula XIIA-I in which Ri is 2-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 3-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 4-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 5-chloro, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 3-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 4-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 5-bromo, R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 2-chloro, R 2 is 4- chloro, R 3 and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention contemplates the compound of formula XIIA-I in which Ri is 3-chloro, R 2 is 4-chloro, R 3 and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is pyridyl, piperazinyl, piperazinonyl, piperidinyl, piperidinonyl, morpholyl, furyl, tetrahydrofuryl, or pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which one or both of Ri and R 2 are CF 3 , R 3 and R 4 are H, R 1 is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention contemplates a compound of formula XIIA-I in which R t is 3-CF 3 , R 2 , R 3 , and R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is isothiazolyl, isoxazolyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, thienyl, furyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, thiazolinyl, thiazolidinyl, isothiazolinyl, isothiazolidinyl, imidazolinyl, imidazolyl, pyridyl, phenyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-cyano, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1 -morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l -pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 3-hydroxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1 -morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l -pyrimidyl.
  • this invention provides a compound of formula XIIA-I in which Ri is 4-hydroxy, R 2 - R 4 are H, R' is -(CH 2 ) n -B, where n is 2, and B is 3- methyl-2-pyridyl, 3-methyl-2-piperazinyl, 3-methylpiperazin-2-on-l-yl, 3-methyl-l- piperidinyl, 3-methyl-2-piperidinonyl, 3 -methyl- 1-morpholyl, 3-methyl-2-furyl, 3-methyl-2- tetrahydrofuryl, or 2-methyl-l-pyrimidyl.

Abstract

L'invention concerne des composés de formule (I) qui inhibent la MEK et qui ont une activité comme agents anti-néoplasiques. Ces composés comprennent des 3-hydroxy-5- arylamino-isothiazole-4-carboxamidines N-substituées. Ils comprennent aussi les tautomères des isothiazol-3(2H)- ones.
PCT/US2006/022491 2005-06-07 2006-06-07 Phenylamino isothiazole carboxamidines comme inhibiteurs de mek WO2006133417A1 (fr)

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WO2011106298A1 (fr) 2010-02-25 2011-09-01 Dana-Farber Cancer Institute, Inc. Mutations de braf conférant une résistance aux inhibiteurs de braf
US8034953B2 (en) 2005-05-10 2011-10-11 Incyte Corporation Modulators of indoleamine 2,3-dioxygenase and methods of using the same
US8088803B2 (en) 2008-07-08 2012-01-03 Incyte Corporation 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
US8377976B2 (en) 2006-09-19 2013-02-19 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
US8450351B2 (en) 2005-12-20 2013-05-28 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
US8507541B2 (en) 2006-09-19 2013-08-13 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
WO2013169858A1 (fr) 2012-05-08 2013-11-14 The Broad Institute, Inc. Méthodes de diagnostic et de traitement chez des patients ayant ou présentant un risque de développer une résistance à une thérapie anticancéreuse
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WO2020188015A1 (fr) 2019-03-21 2020-09-24 Onxeo Molécule dbait associée à un inhibiteur de kinase pour le traitement du cancer
WO2021089791A1 (fr) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Méthodes pour le traitement de cancers qui ont acquis une résistance aux inhibiteurs de kinase
WO2021148581A1 (fr) 2020-01-22 2021-07-29 Onxeo Nouvelle molécule dbait et son utilisation
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