WO2019222269A1 - Biaryl amides with modified sugar groups for treatment of diseases associated with heat shock protein pathway - Google Patents

Biaryl amides with modified sugar groups for treatment of diseases associated with heat shock protein pathway Download PDF

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Publication number
WO2019222269A1
WO2019222269A1 PCT/US2019/032292 US2019032292W WO2019222269A1 WO 2019222269 A1 WO2019222269 A1 WO 2019222269A1 US 2019032292 W US2019032292 W US 2019032292W WO 2019222269 A1 WO2019222269 A1 WO 2019222269A1
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Prior art keywords
alkyl
substituted
groups
alkanediyl
aralkyl
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PCT/US2019/032292
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English (en)
French (fr)
Inventor
Xin Jiang
Melean Visnick
Christopher F. BENDER
Gary Bolton
Bradley Caprathe
Chitase Lee
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Reata Pharmaceuticals Inc
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Reata Pharmaceuticals Inc
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Priority to AU2019271126A priority Critical patent/AU2019271126B2/en
Priority to IL278698A priority patent/IL278698B2/en
Priority to PE2020001859A priority patent/PE20211917A1/es
Priority to CN201980046311.2A priority patent/CN112513058B/zh
Priority to SG11202011311YA priority patent/SG11202011311YA/en
Priority to CA3100333A priority patent/CA3100333A1/en
Priority to MX2025007723A priority patent/MX2025007723A/es
Priority to JP2020564427A priority patent/JP7508375B2/ja
Priority to MX2020012366A priority patent/MX2020012366A/es
Priority to EA202092727A priority patent/EA202092727A1/ru
Priority to US17/055,331 priority patent/US11827664B2/en
Priority to CN202411057163.3A priority patent/CN119285591A/zh
Priority to EP19732770.3A priority patent/EP3794009A1/en
Application filed by Reata Pharmaceuticals Inc filed Critical Reata Pharmaceuticals Inc
Priority to UAA202007914A priority patent/UA130486C2/uk
Priority to KR1020207033977A priority patent/KR20210021457A/ko
Priority to IL309891A priority patent/IL309891B2/en
Priority to BR112020023277-7A priority patent/BR112020023277A2/pt
Publication of WO2019222269A1 publication Critical patent/WO2019222269A1/en
Priority to PH12020551941A priority patent/PH12020551941A1/en
Anticipated expiration legal-status Critical
Priority to CONC2020/0015380A priority patent/CO2020015380A2/es
Priority to US18/485,699 priority patent/US12595278B2/en
Priority to JP2024098452A priority patent/JP2024125338A/ja
Priority to AU2024267017A priority patent/AU2024267017A1/en
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/17—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/18—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C59/01—Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
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    • C07C69/67—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
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    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • C07D309/10—Oxygen atoms
    • C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
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    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
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    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
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    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/203—Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
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    • C07H9/02—Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing only oxygen as ring hetero atoms
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    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Definitions

  • the present invention relates generally to the fields of biology, chemistry, and medicine. More particularly, it concerns compounds, compositions and methods for the treatment and prevention of diseases and disorders, including neurological disorders, such as neurodegenerative diseases and nerve damaging disorders, for example, diabetic peripheral neuropathy.
  • neurological disorders such as neurodegenerative diseases and nerve damaging disorders, for example, diabetic peripheral neuropathy.
  • the heat shock protein 90 is associated with a wide variety of disorders which result from the misfolding of one or more proteins. These disorders include neurological diseases associated with damage, loss of function, or death of a neuron. These diseases may affect either peripheral neurons (peripheral neuropathy) or central neurons (central neuropathy) and result from systemic diseases or conditions such as diabetes, leprosy, vitamin deficiencies, medication, or diseases of the immune system or from conditions such as a viral infection or a traumatic injury. Damage to peripheral neurons due to diabetes is known as diabetic peripheral neuropathy and can result in nerve damage to any organ of the body. This condition can lead to a variety of different symptoms, but the hallmark symptom is chronic pain, numbness, and tingling, particularly in the distal extremities. In 2010, approximately 132 million people are believed to have diabetic peripheral neuropathy, which is the most common complication from diabetes and leading source of morbidity and mortality in diabetes.
  • the present disclosure provides biaryl Hsp90 inhibitors with modified ether groups with therapeutic properties, pharmaceutical compositions thereof, methods for their manufacture, and methods for their use.
  • the present disclosure provides compounds of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), aralkyl(c ⁇ i2), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 and R15 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R3 is -NR11R11' or -C(0)NRi2Ri2', wherein:
  • R 11 and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • R12 and R12' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 is carboxy or alkyl(c ⁇ 6), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein: R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • Rs, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl(c ⁇ 6 ) -heterocycloalkyl(c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X 2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl ( c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S;
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 is hydrogen, carboxy or alkyl(c ⁇ 6), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • Re and R9 are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i3 ⁇ 4, aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Rio is amino or alkylamino(c ⁇ 6), dialkylamino(c ⁇ i 2) , amido(c ⁇ i 2) , or a substituted version of any of these three groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X 2 is CRu or N, wherein: Ru is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • Ru and RI 4 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy(c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 is carboxy or alkyl(C3-8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i2) or substituted aralkyl(c ⁇ i2);
  • R 7 ' is hydrogen, carboxy, or alkyl(C3-8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i2) or substituted aralkyl(c ⁇ i2); or
  • R 7 and R ⁇ /' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • R 7 and R ⁇ /' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Rs, R9, and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Yi is substituted -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or substituted -C(0)-alkanediyl(c ⁇ 6)- ;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of any of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i 2) , aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X 2 is CRu or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6 ) , alkenediyl(c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R 2 are taken together and are alkanediyl(c ⁇ 6 ) , alkoxydiyl(c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 1 or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl(c ⁇ 8 ) , amido(c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , amido ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylthio ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NR I2 R I2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R I2 and R I2 ' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , heteroaryl ( c ⁇ i 2) , aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i2) or substituted aralkyl(c ⁇ i2); or
  • R 7 and R 7 ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Xi is CRM or N, wherein:
  • Ri4 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • Ri4 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S;
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 is carboxy or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • R 7 ' is hydrogen, carboxy, or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re is halo, alkoxy (C3-6) , acyloxy ( c ⁇ 6 ) , aralkoxy ( c ⁇ i 2) , or a substituted version of any of these groups;
  • R9 and Rio are each independently halo, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i 2) , aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein: R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), aralkyl(c ⁇ i2), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6 ) , alkoxydiyl(c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRi2Ri2', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl ( c ⁇ 6) ;
  • R12 and R12' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R7 and R7' are each independently hydrogen, carboxy or alkyl(c ⁇ 8 ) , alkenyl(c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • R7 and R7' are taken together and are -alkanediyl ( c ⁇ 7 ) -, -alkenediyl ( c ⁇ 7 ) -, or a substituted version of either of these groups;
  • Re, R9, and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRu or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • Ru and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or Ru and R 2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , amido ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , amido ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylthio ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R3 is -NR11R11' or -C(0)NR I2 R I2 ', wherein:
  • R11 and Ru' are each independently hydrogen, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R I2 and R I2 ' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 is carboxy or alkyl(c ⁇ 8 ) , alkenyl(c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , heteroaryl ( c ⁇ i 2) , aralkyl(c ⁇ i 3 ⁇ 4 , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl ( c ⁇ i 2) , or substituted aralkyl ( c ⁇ i 2) ;
  • R 7 ' is hydrogen, carboxy or alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl(c ⁇ i2 ) , aralkyl(c ⁇ i2 ) , heteroaralkyl(c ⁇ i2 ) , -alkanediyl ( c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl ( c ⁇ 7) -, -alkenediyl ( c ⁇ 7) -, or a substituted version of either of these groups;
  • Rs is halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR M or N, wherein:
  • Ri4 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • Ri4 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X 2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • Ri6 is alkyl ( c ⁇ i2 ) , cycloalkyl ( c ⁇ i2 ) , aryl ( c ⁇ i8 ) , heteroaryl(c ⁇ i8 ) , or a substituted version thereof;
  • Rn and Ris are each independently hydrogen, alkyl(c ⁇ 8 ) , or substituted alkyl ( c ⁇ 8 ) ;
  • R19 is carboxy or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i2), substituted alkyl(c ⁇ i2), aralkyl(c ⁇ i2), or substituted
  • R19' is hydrogen, carboxy or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i2), substituted alkyl(c ⁇ i2), aralkyl(c ⁇ i2), or substituted aralkyl(c ⁇ i2);
  • R20, R21, and R22 are each independently halo, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups, or a protected hydroxy group;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), aralkyl(c ⁇ i2), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 and R15 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 3 is -NRiiRn' or -C(0)NRi2Ri2', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R12 and R12' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R5, and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy(c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R7 is carboxy or alkyl ( c ⁇ 6 ) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl ( c ⁇ i2 ) or substituted aralkyl ( c ⁇ i2 ) ;
  • Re, R9, and Rio are each independently hydrogen, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and R15 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R3 is -NR11R11' or -C(0)NRI 2 RI 2 ', wherein:
  • R11 and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 is hydrogen, carboxy or alkyl(c ⁇ 6), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • Re and R9 are each independently hydrogen, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i 2) , aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Rio is amino or alkylamino(c ⁇ 6), dialkylamino(c ⁇ i2), amido(c ⁇ i2), or a substituted version of any of these three groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), aralkyl(c ⁇ i2), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRi2Ri2', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • R12 and R12' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R7 is carboxy or alkyl(C3-8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i2) or substituted aralkyl(c ⁇ i2);
  • R7' is hydrogen, carboxy, or alkyl(C3-8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i2) or substituted aralkyl(c ⁇ i2); or
  • R7 and R7' are taken together and are -alkanediyl(c ⁇ 7)-, -alkenediyl(c ⁇ 7)-, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRu or N, wherein: Ru is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • Ru and RI 4 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i2) or substituted aralkyl(c ⁇ i2);
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Yi is substituted -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or substituted
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R 7 and R ⁇ /' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of any of these groups;
  • Re, R9, and Rio are each independently hydrogen, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i 2) , aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X 2 is CRu or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • Ru and RI 4 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 1 or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Xi is CRM or N, wherein:
  • Ri4 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • Ri4 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X 2 is CRu or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • Ru and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or R15 and R 2 are taken together and are alkanediyl(c ⁇ 6 ) , alkoxydiyl(c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl(c ⁇ 8 ) , amido(c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , aralkyl(c ⁇ i 3 ⁇ 4 , amido ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylthio ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NR I2 R I2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl ( c ⁇ 6 ) , substituted alkyl ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R I2 and R I2 ' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 is carboxy or alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i 2) , heteroaryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i 3 ⁇ 4 or substituted aralkyl(c ⁇ i 3 ⁇ 4 ;
  • R 7 ' is hydrogen, carboxy, or alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl ( c ⁇ i2 ) or substituted aralkyl ( c ⁇ i2 ) ; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl ( c ⁇ 7) -, -alkenediyl ( c ⁇ 7) -, or a substituted version of either of these groups;
  • Re is alkoxy (C3-6) , acyloxy ( c ⁇ 6 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • R9 and Rio are each independently hydroxy, or alkyl(c ⁇ 6 ) , alkoxy(c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy(c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl(c ⁇ 6 ) -heterocycloalkyl(c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl(c ⁇ 6 ) -heterocycloalkyl(c ⁇ 8 ) , or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R9, and Rio are each independently hydrogen, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i3 ⁇ 4, aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or Ri4 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; and
  • X 2 is CRis or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • Ru and RI 4 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein: Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R 12 and R 12 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy(c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R7 is carboxy or alkyl(c ⁇ 8 ) , alkenyl(c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl(c ⁇ i2 ) , aralkyl(c ⁇ i2 ) , heteroaralkyl(c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • R7' is hydrogen, carboxy or alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • R7 and R7' are taken together and are -alkanediyl ( c ⁇ 7 ) -, -alkenediyl ( c ⁇ 7 ) -, or a substituted version of either of these groups;
  • Rs is halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X 2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or R15 and R2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or a compound of the formula:
  • Ri6 is alkyl(c ⁇ i2), cycloalkyl(c ⁇ i2), aryl(c ⁇ i8), heteroaryl(c ⁇ i8), or a substituted version thereof;
  • Rn and Ris are each independently hydrogen, alkyl(c ⁇ 8), or substituted alkyl(c ⁇ 8);
  • Rig is alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), or a substituted version of any of these groups
  • R20, R21, and R22 are each independently hydroxy, alkoxy(c ⁇ i2), substituted alkoxy(c ⁇ i2), or a protected hydroxy group;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), aralkyl(c ⁇ i2), amido(c ⁇ 6), alkoxy ( c ⁇ 6 ) , alkylthio(c ⁇ 6 ) , alkylsulfonyl(c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6 ) , alkoxydiyl(c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRi2Ri2', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R12 and R12' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R7 is carboxy or alkyl ( c ⁇ 6 ) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl ( c ⁇ i2 ) or substituted aralkyl ( c ⁇ i2 ) ;
  • Re, R 9 , and Rio are each independently hydrogen, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRu or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • Ru and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R3 is -NR11R11' or -C(0)NRI 2 RI 2 ', wherein:
  • R 11 and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 is carboxy or alkyl (C3-8) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i 2) , heteroaryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i 3 ⁇ 4 or substituted aralkyl(c ⁇ i 3 ⁇ 4 ;
  • R 7 ' is hydrogen, carboxy, or alkyl(C3-8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i3 ⁇ 4, heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein: R13 is aralkyl ( c ⁇ i2 ) or substituted aralkyl ( c ⁇ i2 ) ; or
  • R 7 and R 7 ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy(c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy(c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl(c ⁇ 6 ) -heterocycloalkyl(c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl ( c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 or S;
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R9, and Rio are each independently hydrogen, hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i3 ⁇ 4, aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; and
  • X 2 is CRis or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • Ru and RI 4 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Yi is substituted -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or substituted
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy(c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 and R 7 ' are each independently hydrogen, carboxy or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl(c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl ( c ⁇ i2 ) or substituted aralkyl ( c ⁇ i2 ) ; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl ( c ⁇ 7) -, -alkenediyl ( c ⁇ 7) -, or a substituted version of any of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 1 or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i3 ⁇ 4 or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R 7 and R ⁇ /' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R 2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRi2Ri2', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • R12 and R12' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R7 is carboxy or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i2) or substituted aralkyl(c ⁇ i2);
  • R7' is hydrogen, carboxy, or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl(c ⁇ i2) or substituted aralkyl(c ⁇ i2); or
  • R7 and R7' are taken together and are -alkanediyl(c ⁇ 7)-, -alkenediyl(c ⁇ 7)-, or a substituted version of either of these groups;
  • Re is alkoxy (C3-6) , acyloxy ( c ⁇ 6 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • R9 and Rio are each independently hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRu or N, wherein: Ru is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • Ru and RI 4 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R ⁇ / ' are each independently hydrogen, carboxy or alkyl ( c ⁇ 8) , alkenyl ( c ⁇ 8) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is aralkyl ( c ⁇ i2 ) or substituted aralkyl ( c ⁇ i2 ) ;
  • R 7 and R 7 ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy(c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl(c ⁇ 6 ) -heterocycloalkyl(c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or a compound of the formula:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • Rs is hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i 2) , aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Xi is CRM or N, wherein:
  • Ri4 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • Ri4 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X 2 is CRu or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl(c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or a compound of the formula:
  • Ri6 is alkyl ( c ⁇ i2 ) , cycloalkyl ( c ⁇ i2 ) , aryl ( c ⁇ i8 ) , heteroaryl(c ⁇ i8 ) , or a substituted version thereof;
  • R17 and Ris are each independently hydrogen, alkyl(c ⁇ 8) , or substituted alkyl(c ⁇ 8) ;
  • R19 is alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , or a substituted version of any of these groups
  • R20, R21, and R22 are each independently hydroxy, alkoxy(c ⁇ i2 ) , substituted alkoxy(c ⁇ i2 ) , or a protected hydroxy group;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S;
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 is carboxy or alkyl(c ⁇ 6), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i 2) ;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i3 ⁇ 4, aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X 2 is CRu or N, wherein: R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino(c ⁇ 6 ) , -alkanediyl(c ⁇ 6 ) -heterocycloalkyl(c ⁇ 8 ) , or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R 2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a pharmaceutically acceptable salt of the formula.
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl ( c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl ( c ⁇ 6 ) , substituted alkyl ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl ( c ⁇ 6 ) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6 ) , substituted alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 is carboxy or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i 2) , heteroaryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl ( c ⁇ i 2) , or substituted aralkyl ( c ⁇ i 2) ; and Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl(c ⁇ i 3 ⁇ 4 , aralkoxy(c ⁇ i 3 ⁇ 4 , or a substituted version of any of these groups;
  • the compounds further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R3 is -NRiiRn' or -C(0)NRI 2 RI 2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6 ) , substituted alkyl(c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl ( c ⁇ 6 ) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 7 is carboxy or alkyl ( c ⁇ 6 ) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , heteroaryl ( c ⁇ i 2) , aralkyl(c ⁇ i 3 ⁇ 4 , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl(c ⁇ i 3 ⁇ 4 , or substituted aralkyl(c ⁇ i 3 ⁇ 4 ;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i 2) , aralkoxy ( c ⁇ i 2) , or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • R.7 is carboxy or alkyl(c ⁇ 6 ) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl(c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl(c ⁇ i2 ) , aralkyl(c ⁇ i2 ) , heteroaralkyl(c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , amido(c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , amido ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylthio(c ⁇ 6 ) , alkylsulfonyl(c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6 ) , alkoxydiyl(c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRi2Ri2', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R12 and R12' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R7 is hydrogen, carboxy or alkyl ( c ⁇ 6 ) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • Re and R9 are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Rio is amino or alkylamino(c ⁇ 6 ) , dialkylamino(c ⁇ i2 ) , amido(c ⁇ i2 ) , or a substituted version of any of these three groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl(c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRu or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; R15 and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl(c ⁇ 6 ) , or a substituted version of any of these groups; or
  • R15 and R 2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a pharmaceutically acceptable salt of the formula.
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R 3 is -NRiiRn' or -C(0)NR I2 R I2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl ( c ⁇ 6 ) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy(c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 is hydrogen, carboxy or alkyl ( c ⁇ 6 ) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , heteroaryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl(c ⁇ i 3 ⁇ 4 , or substituted aralkyl ( c ⁇ i 2) ;
  • Re and R9 are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i 2) , aralkoxy ( c ⁇ i 2) , or a substituted version of any of these groups;
  • Rio is amino or alkylamino(c ⁇ 6 ) , dialkylamino(c ⁇ i2 ) , amido(c ⁇ i2 ) , or a substituted version of any of these three groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R 3 is -NRnRii' or -C(0)NRi2Ri2', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl ( c ⁇ 6 ) , substituted alkyl ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R 12 and R 12 ' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 7 is hydrogen, carboxy or alkyl ( c ⁇ 6 ) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • Re and R 9 are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Rio is amino or alkylamino ( c ⁇ 6 ) , dialkylamino ( c ⁇ i2 ) , amido ( c ⁇ i2 ) , or a substituted version of any of these three groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl ( c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R3 is -NRiiRn' or -C(0)NRI 2 RI 2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6 ) , substituted alkyl(c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl ( c ⁇ 6 ) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 7 is hydrogen, carboxy or alkyl ( c ⁇ 6 ) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , heteroaryl ( c ⁇ i 2) , aralkyl(c ⁇ i 3 ⁇ 4 , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl ( c ⁇ i 2) , or substituted aralkyl(c ⁇ i 3 ⁇ 4 ;
  • Re and R9 are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i 2) , aralkoxy ( c ⁇ i 2) , or a substituted version of any of these groups;
  • Rio is amino or alkylamino(c ⁇ 6 ) , dialkylamino(c ⁇ i 2) , amido(c ⁇ i 2) , or a substituted version of any of these three groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 is carboxy or alkyl(C3-8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • R 7 ' is hydrogen, carboxy, or alkyl(C3-8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i3 ⁇ 4, heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i 2) , aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • Xi is CR M or N, wherein:
  • Ri4 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino(c ⁇ 6 ) , -alkanediyl(c ⁇ 6 ) -heterocycloalkyl(c ⁇ 8 ) , or a substituted version of any of these groups; or
  • Ri4 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X 2 is CRis or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino(c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • Ru and RM are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a pharmaceutically acceptable salt of the formula.
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R 3 is -NRiiRn' or -C(0)NR I2 R I2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R I2 and R I2 ' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy(c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 is carboxy or alkyl (C 3-8 ) , alkenyl(c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl(c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • R 7 ' is hydrogen, carboxy, or alkyl (C 3-8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl ( c ⁇ 7) -, -alkenediyl ( c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl ( c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R3 is -NR11R11' or -C(0)NRi2Ri2', wherein:
  • R11 and Rn' are each independently hydrogen, alkyl ( c ⁇ 6 ) , substituted alkyl ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R12 and R12' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R.7 is carboxy or alkyl (C3-8) , alkenyl(c ⁇ 8 ) , alkynyl(c ⁇ 8 ) , cycloalkyl(c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl(c ⁇ i2 ) , aralkyl(c ⁇ i2 ) , heteroaralkyl(c ⁇ i2 ) , -alkanediyl ( c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl(c ⁇ i2 ) , aralkyl(c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • R 7 ' is hydrogen, carboxy, or alkyl (C3-8) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ; or
  • R 7 and R ⁇ /' are taken together and are -alkanediyl ( c ⁇ 7) -, -alkenediyl ( c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • R 7 is carboxy or alkyl (C3-8) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • R 7 ' is hydrogen, carboxy, or alkyl (C3-8) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6) -ORi 3 , or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ; or R 7 and R 7 ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of any of these groups; and
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), aralkyl(c ⁇ i2), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R2 and R15 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups;
  • R3 is -NR11R11' or -C(0)NRi2Ri2', wherein:
  • R11 and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • R12 and R12' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl ( c ⁇ 8 ) , cycloalkyl(c ⁇ 8 ) , heterocycloalkyl(c ⁇ 8 ) , aryl(c£i2 ) , heteroaryl(c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl(c ⁇ i2 ) , -alkanediyl(c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl(c ⁇ i2 ) , aralkyl(c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ;
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of any of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a pharmaceutically acceptable salt of the formula.
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 or S
  • R 3 is -NRiiRn' or -C(0)NRI 2 RI 2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i 2) ;
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i3 ⁇ 4, aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y 1 is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 or S
  • R3 is -NR11R11' or -C(0)NRi2Ri2', wherein:
  • R11 and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • R12 and R12' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c£i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i2), substituted alkyl(c ⁇ i2), aralkyl(c ⁇ i2), or substituted aralkyl(c ⁇ i2);
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of any of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y 2 is CH 2 or S
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i3 ⁇ 4, heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • R 7 and R ⁇ /' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i3 ⁇ 4, aralkoxy(c ⁇ i3 ⁇ 4, or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Yi is substituted -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or substituted -C(0)-alkanediyl(c ⁇ 6)-;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , aralkyl(c ⁇ i3 ⁇ 4, amido(c ⁇ 6), alkoxy(c ⁇ 6), alkylthio(c ⁇ 6), alkylsulfonyl(c ⁇ 6), or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6 ) , alkoxydiyl(c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRi2Ri2', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R12 and R12' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 and R 7 ' are each independently hydrogen, carboxy or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c£i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl ( c ⁇ 7) -, -alkenediyl ( c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R9, and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRu or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • Ru and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or R15 and R 2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a pharmaceutically acceptable salt of the formula.
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Yi is substituted -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or substituted -C(0)-alkanediyl(c ⁇ 6)- ;
  • Y 2 is CH 2 , O, or S
  • R 3 is -NRnRii' or -C(0)NRI 2 RI 2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i3 ⁇ 4, heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R9, and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i 2) , aralkoxy(c ⁇ i 2) , or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Yi is substituted -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or substituted -C(0)-alkanediyl(c ⁇ 6)- ;
  • Y 2 is CH 2 , O, or S
  • R3 is -NR11R11' or -C(0)NRi2Ri2', wherein:
  • R11 and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • R12 and R12' are each independently hydrogen, alkyl(c ⁇ 6) , or substituted alkyl(c ⁇ 6);
  • R 7 and R 7 ' are each independently hydrogen, carboxy or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i2), substituted alkyl(c ⁇ i2), aralkyl(c ⁇ i2), or substituted aralkyl(c ⁇ i2); or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl(c ⁇ 6) , alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Yi is substituted -alkanediyl(c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or substituted -C(0)-alkanediyl ( c ⁇ 6 ) - ;
  • R 7 and R 7 ' are each independently hydrogen, carboxy or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl ( c ⁇ 8 ) , cycloalkyl(c ⁇ 8 ) , heterocycloalkyl(c ⁇ 8 ) , aryl(c£i2 ) , heteroaryl(c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl(c ⁇ i2 ) , -alkanediyl(c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl(c ⁇ i2 ) , aralkyl(c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re, R 9 , and Rio are each independently hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 1 or 2;
  • Y 1 is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl ( c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , amido ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , amido ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylthio ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl(c ⁇ 6 ) , alkoxydiyl(c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups;
  • R 3 is -NRnRii' or -C(0)NRi2Ri2', wherein:
  • Ru and Ru' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R12 and R12' are each independently hydrogen, alkyl ( c ⁇ 6) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 and R 7 ' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8) , alkenyl(c ⁇ 8) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c£i2 ) , heteroaryl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , heteroaralkyl ( c ⁇ i2 ) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl ( c ⁇ i2 ) , substituted alkyl ( c ⁇ i2 ) , aralkyl ( c ⁇ i2 ) , or substituted aralkyl ( c ⁇ i2 ) ; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl ( c ⁇ 7) -, -alkenediyl ( c ⁇ 7) -, or a substituted version of either of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups; or
  • R14 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • X2 is CRu or N, wherein:
  • Ru is hydrogen, halo, hydroxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylamino ( c ⁇ 6 ) , -alkanediyl ( c ⁇ 6 ) -heterocycloalkyl ( c ⁇ 8 ) , or a substituted version of any of these groups;
  • Ru and R14 are taken together and are alkanediyl ( c ⁇ 6 ) , alkenediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups; or
  • Ru and R 2 are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6) , or a substituted version of any of these groups; or a pharmaceutically acceptable salt of the formula.
  • the compounds are further defined as:
  • n 1 or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R3 is -NR11R11' or -C(0)NRI 2 RI 2 ', wherein:
  • R 11 and Rn' are each independently hydrogen, alkyl(c ⁇ 6) , substituted alkyl(c ⁇ 6) , acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R 5 , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6); and R7 and R7' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i3 ⁇ 4, heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i3 ⁇ 4, or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R7 and R7' are taken together and are -alkanediyl(c ⁇ 7)-, -alkenediyl(c ⁇ 7)-, or a substituted version of either of these groups;
  • the compounds are further defined as:
  • n 1 or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R3 is -NR11R11' or -C(0)NR I2 R I2 ', wherein:
  • R 11 and Rn' are each independently hydrogen, alkyl(c ⁇ 6 ) , substituted alkyl(c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • R I2 and R I2 ' are each independently hydrogen, alkyl ( c ⁇ 6 ) , or substituted alkyl ( c ⁇ 6 ) ;
  • R7 and R7' are each independently hydrogen, carboxy, or alkyl(c ⁇ 8 ) , alkenyl(c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , heteroaryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl(c ⁇ i 3 ⁇ 4 , or substituted aralkyl ( c ⁇ i 2) ; or
  • R7 and R7' are taken together and are -alkanediyl ( c ⁇ 7 ) -, -alkenediyl ( c ⁇ 7 ) -, or a substituted version of either of these groups;
  • the compounds further defined as:
  • n 1 or 2;
  • R7 and R7' are each independently hydrogen, carboxy, or alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i 2) , heteroaryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R7 and R7' are taken together and are -alkanediyl ( c ⁇ 7 ) -, -alkenediyl ( c ⁇ 7 ) -, or a substituted version of either of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • Ri is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl(c ⁇ 8 ) , amido(c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 is hydrogen, amino, halo, hydroxy, carboxy, or alkyl ( c ⁇ 6 ) , alkenyl ( c ⁇ 6 ) , alkynyl ( c ⁇ 6 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , amido ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , alkylthio ( c ⁇ 6 ) , alkylsulfonyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R 2 and Ru are taken together and are alkanediyl ( c ⁇ 6 ) , alkoxydiyl ( c ⁇ 6 ) , alkylaminodiyl ( c ⁇ 6 ) , or a substituted version of any of these groups;
  • R3 is -NR11R11' or -C(0)NRI 2 RI 2 ', wherein:
  • R11 and Ru' are each independently hydrogen, alkyl ( c ⁇ 6 ) , substituted alkyl ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl ( c ⁇ 6 ) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl ( c ⁇ 6) , substituted alkyl ( c ⁇ 6) , alkoxy ( c ⁇ 6 ) , substituted alkoxy ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , or substituted acyloxy ( c ⁇ 6 ) ;
  • R 7 is carboxy or alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , heteroaryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl(c ⁇ i 3 ⁇ 4 , or substituted aralkyl ( c ⁇ i 2) ;
  • R 7 ' is hydrogen, carboxy, or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i2), heteroaryl(c ⁇ i2), aralkyl(c ⁇ i2), heteroaralkyl(c ⁇ i2), -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i2), substituted alkyl(c ⁇ i2), aralkyl(c ⁇ i2), or substituted aralkyl(c ⁇ i2); or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re is alkoxy (C3-6) , acyloxy(c ⁇ 6 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • R9 and Rio are each independently halo or hydroxy, or alkyl(c ⁇ 6), alkoxy(c ⁇ 6), acyl(c ⁇ 6), acyloxy(c ⁇ 6), aralkyl(c ⁇ i2), aralkoxy(c ⁇ i2), or a substituted version of any of these groups;
  • Xi is CR 14 or N, wherein:
  • R14 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups; or
  • R14 and R15 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups;
  • X2 is CRis or N, wherein:
  • R15 is hydrogen, halo, hydroxy, or alkyl(c ⁇ 6), alkenyl(c ⁇ 6), alkynyl(c ⁇ 6), alkoxy(c ⁇ 6), alkylamino(c ⁇ 6), -alkanediyl(c ⁇ 6)-heterocycloalkyl(c ⁇ 8), or a substituted version of any of these groups;
  • R15 and R14 are taken together and are alkanediyl(c ⁇ 6), alkenediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6), or a substituted version of any of these groups; or
  • R15 and R2 are taken together and are alkanediyl(c ⁇ 6), alkoxydiyl(c ⁇ 6), alkylaminodiyl(c ⁇ 6) , or a substituted version of any of these groups; or a pharmaceutically acceptable salt of the formula.
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl(c ⁇ 6)-, -C(0)-alkanediyl(c ⁇ 6)-, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R3 is -NRiiRn' or -C(0)NRI 2 RI 2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), acyl(c ⁇ 6), or substituted acyl(c ⁇ 6);
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl(c ⁇ 6), or substituted alkyl(c ⁇ 6);
  • R 4 , R , and Re are each independently hydrogen, halo, alkyl(c ⁇ 6), substituted alkyl(c ⁇ 6), alkoxy(c ⁇ 6), substituted alkoxy(c ⁇ 6), acyloxy(c ⁇ 6), or substituted acyloxy(c ⁇ 6);
  • R 7 is carboxy or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i3 ⁇ 4, heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i 2) , heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i3 ⁇ 4;
  • R 7 ' is hydrogen, carboxy, or alkyl(c ⁇ 8), alkenyl(c ⁇ 8), alkynyl(c ⁇ 8), cycloalkyl(c ⁇ 8), heterocycloalkyl(c ⁇ 8), aryl(c ⁇ i 2) , heteroaryl(c ⁇ i 2) , aralkyl(c ⁇ i3 ⁇ 4, heteroaralkyl(c ⁇ i 2) , -alkanediyl(c ⁇ 6)-ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i3 ⁇ 4, substituted alkyl(c ⁇ i3 ⁇ 4, aralkyl(c ⁇ i 2) , or substituted aralkyl(c ⁇ i3 ⁇ 4; or
  • R 7 and R ⁇ / ' are taken together and are -alkanediyl(c ⁇ 7) -, -alkenediyl(c ⁇ 7) -, or a substituted version of either of these groups;
  • Re is alkoxy (C3-6) , acyloxy ( c ⁇ 6 ) , aralkoxy ( c ⁇ i 2) , or a substituted version of any of these groups; and R9 and Rio are each independently halo or hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl(c ⁇ i 3 ⁇ 4 , aralkoxy(c ⁇ i 3 ⁇ 4 , or a substituted version of any of these groups;
  • the compounds are further defined as:
  • n 0, 1, or 2;
  • Y i is -alkanediyl ( c ⁇ 6 ) -, -C(0)-alkanediyl(c ⁇ 6 ) -, or a substituted version of any of these groups;
  • Y 2 is CH 2 , O, or S
  • R3 is -NRiiRn' or -C(0)NRI 2 RI 2 ', wherein:
  • Rn and Rn' are each independently hydrogen, alkyl(c ⁇ 6 ) , substituted alkyl(c ⁇ 6 ) , acyl ( c ⁇ 6 ) , or substituted acyl ( c ⁇ 6 ) ;
  • RI 2 and RI 2 ' are each independently hydrogen, alkyl ( c ⁇ 6 ) , or substituted alkyl ( c ⁇ 6 ) ;
  • R 7 is carboxy or alkyl(c ⁇ 8 ) , alkenyl(c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl(c ⁇ i 3 ⁇ 4 , heteroaryl ( c ⁇ i 2) , aralkyl(c ⁇ i 3 ⁇ 4 , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl(c ⁇ i 3 ⁇ 4 , or substituted aralkyl(c ⁇ i 3 ⁇ 4 ;
  • R 7 ' is hydrogen, carboxy, or alkyl ( c ⁇ 8 ) , alkenyl ( c ⁇ 8 ) , alkynyl ( c ⁇ 8 ) , cycloalkyl ( c ⁇ 8 ) , heterocycloalkyl ( c ⁇ 8 ) , aryl ( c ⁇ i 2) , heteroaryl ( c ⁇ i 2) , aralkyl ( c ⁇ i 2) , heteroaralkyl ( c ⁇ i 2) , -alkanediyl ( c ⁇ 6 ) -ORi3, or a substituted version of any of these groups wherein:
  • R13 is alkyl(c ⁇ i 3 ⁇ 4 , substituted alkyl(c ⁇ i 3 ⁇ 4 , aralkyl ( c ⁇ i 2) , or substituted aralkyl ( c ⁇ i 2) ; or
  • R 7 and R ⁇ /' are taken together and are -alkanediyl ( c ⁇ 7) -, -alkenediyl ( c ⁇ 7) -, or a substituted version of either of these groups;
  • Re is alkoxy (C3-6) , acyloxy ( c ⁇ 6 ) , aralkoxy ( c ⁇ i 2) , or a substituted version of any of these groups; and R 9 and Rio are each independently halo or hydroxy, or alkyl ( c ⁇ 6 ) , alkoxy ( c ⁇ 6 ) , acyl ( c ⁇ 6 ) , acyloxy ( c ⁇ 6 ) , aralkyl ( c ⁇ i2 ) , aralkoxy ( c ⁇ i2 ) , or a substituted version of any of these groups;
  • the compounds are further defined as:

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CN201980046311.2A CN112513058B (zh) 2018-05-14 2019-05-14 治疗与热休克蛋白通路有关的疾病的具有修饰糖基团的联芳基酰胺类
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EA202092727A EA202092727A1 (ru) 2018-05-14 2019-05-14 Биариламиды с модифицированными сахарными группами для лечения заболеваний, связанных с путем белка теплового шока
US17/055,331 US11827664B2 (en) 2018-05-14 2019-05-14 Biaryl amides with modified sugar groups for treatment of diseases associated with heat shock protein pathway
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UAA202007914A UA130486C2 (uk) 2018-05-14 2019-05-14 Біариламіди з модифікованими цукровими групами для лікування захворювань, пов'язаних зі шляхом білка теплового шоку
KR1020207033977A KR20210021457A (ko) 2018-05-14 2019-05-14 열충격 단백질 경로와 연관된 질환의 치료를 위한 변형된 당기를 가진 바이아릴 아마이드
IL309891A IL309891B2 (en) 2018-05-14 2019-05-14 Biaryl amides with sugar groups that are suitable for the treatment of diseases related to the heat stress protein pathway
BR112020023277-7A BR112020023277A2 (pt) 2018-05-14 2019-05-14 biaril amidas com grupos açúcar modificados para tratamento de doenças associadas à trajetória da proteína de choque térmico
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US18/485,699 US12595278B2 (en) 2018-05-14 2023-10-12 Biaryl amides with modified sugar groups for treatment of diseases associated with heat shock protein pathway
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Cited By (9)

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US12024536B2 (en) 2012-02-09 2024-07-02 University Of Kansas C-terminal HSP90 inhibitors
US11643400B2 (en) 2018-05-14 2023-05-09 Gilead Sciences, Inc. MCL-1 inhibitors
US12162844B2 (en) 2018-05-14 2024-12-10 Gilead Sciences, Inc. MCL-1 inhibitors
US11667652B2 (en) 2019-11-12 2023-06-06 Gilead Sciences, Inc. MCL1 inhibitors
US12202842B2 (en) 2019-11-12 2025-01-21 Gilead Sciences, Inc. MCL1 inhibitors
US11760736B2 (en) 2019-11-26 2023-09-19 Gilead Sciences, Inc. Processes and intermediates for preparing MCL1 inhibitors
US12410146B2 (en) 2019-11-26 2025-09-09 Gilead Sciences, Inc. Processes and intermediates for preparing MCL1 inhibitors
US12202782B2 (en) 2020-11-19 2025-01-21 Gilead Sciences, Inc. Processes and intermediates for preparing MCL1 inhibitors
WO2023039293A1 (en) * 2021-09-13 2023-03-16 Rubedo Life Sciences, Inc. Coumarin derivatives of sugar analogs and uses thereof

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