N4-hydroxycytidine and its derivatives, as well as related antiviral applications

Abstract

To provide specific N4-hydroxycytidine derivatives, pharmaceutical compositions, and related methods. [Solution] In certain embodiments, this disclosure relates to the treatment or prevention of viral infections such as Eastern equine encephalitis, Western equine encephalitis, and Venezuelan equine encephalitis (EEE, WEE, and VEE, respectively), Chikungunya fever (CHIK), Ebola, influenza, RSV, and Zika virus infection, by the compounds disclosed. In certain embodiments, this disclosure intends to provide derivatives of the compounds disclosed herein, such as compounds containing one or more of the same or different substituents.

Description

[Technical Field]

[0001] Confirmation of government support This invention was made possible with government support through grants HDTRA1-13-C-0072 and HDTRA1-15-C-0075 granted by the Department of Defense, and grant HHSN272201500008C granted by the National Institutes of Health. The government has certain rights to this invention.

[0002] This disclosure relates to N4-hydroxycytidine nucleosides and derivatives, as well as compositions and methods related thereto. In certain embodiments, this disclosure relates to the treatment or prevention of viral infections, specifically Eastern equine encephalitis, Western equine encephalitis, and Venezuelan equine encephalitis (EEE, WEE, and VEE, respectively), Chikungunya fever (CHIK), Ebola, influenza, RSV, and Zika virus infection. [Background technology]

[0003] The causative agents of Eastern equine encephalitis, Western equine encephalitis, and Venezuelan equine encephalitis (EEE, WEE, and VEE, respectively), as well as chikungunya fever (CHIK), are vector-borne viruses (Togaviridae, Alphavirus genus) that can be transmitted to humans through mosquito bites. Equine encephalitis viruses are CDC Class B pathogens, and CHIK virus is Class C. There are significant concerns regarding the use of virulent strains of the VEE virus, delivered via aerosols, as biological weapons against soldiers. Animal studies have demonstrated that VEE virus infection via aerosol exposure rapidly leads to massive brain infections, with high mortality and morbidity rates. See Roy et al., Pathogenesis of aerosolized Eastern equine encephalitis virus infection in guinea pigs. Virol J, 2009, 6:170.

[0004] Stuyver et al., report β-DN(4)-hydroxycytidine (NHC) was found to have anti-pestivirus and anti-hepasibiric activity. Antimicrob Agents Chemother, 2003, 47(1):244-54. Constantini et al. have reported an evaluation of the efficacy of 2'-C-MeC, 2'-F-2'-C-MeC, and NHC against Norwalk virus. See also Purohit et al., J Med Chem, 2012, 55(22):9988-9997, Ivanov et al., Collection of Czechoslovak Chem Commun, 2006, 71(7):1099-1106, and Fox et al., JACS, 1959, 81:178-87. Novel compounds and treatments are needed for viral infections. The compounds and methods disclosed herein address these needs. [Prior art documents] [Non-patent literature]

[0005] [Non-Patent Document 1] Roy et al.,Pathogenesis of aerosolized Eastern equine encephalitis virus infection in guinea pigs.Virol J,2009,6:170 [Non-Patent Document 2] Purohit et al.,J Med Chem,2012,55(22):9988-9997 [Non-Patent Document 3] Ivanov et al.,Collection of Czechoslovak Chem Commun,2006,71(7):1099-1106 [Non-Patent Document 4] Fox et al., JACS, 1959, 81:178-87 [Overview of the Initiative] [Means for solving the problem]

[0006] This disclosure relates to specific N4-hydroxycytidine and derivatives, combinations, pharmaceutical compositions, and related methods. In certain embodiments, this disclosure relates to compounds having formula I as defined herein. [ka] or relating to pharmaceutically acceptable salts, derivatives, or prodrugs thereof.

[0007] In certain embodiments, this disclosure intends to describe derivatives of the compounds disclosed herein, such as compounds containing one or more of the same or different substituents.

[0008] In certain embodiments, this disclosure envisions a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound disclosed herein. In certain embodiments, the pharmaceutical composition may be in the form of a tablet, capsule, pill, or aqueous buffer such as saline or phosphate buffer.

[0009] In certain embodiments, the disclosed pharmaceutical composition may comprise the compounds and propellants disclosed herein. In certain embodiments, the propellant is a vaporizing propellant such as compressed air, ethanol, nitrogen, carbon dioxide, nitrous oxide, hydrofluoroalkane (HFA), 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, or a combination thereof.

[0010] In certain embodiments, the Disclosure envisions pressurized or non-pressurized vessels containing compounds or pharmaceutical compositions as described herein. In certain embodiments, the vessel is a manual pump sprayer, inhaler, measuring inhaler, dry powder inhaler, atomizer, vibrating mesh atomizer, jet atomizer, or ultrasonic atomizer.

[0011] In certain embodiments, the present disclosure relates to a method for increasing bioavailability to treat or prevent a viral infection, comprising administering an effective amount of a compound or pharmaceutical composition disclosed herein to a subject in need thereof.

[0012] In certain embodiments, this disclosure relates to a method for treating or preventing a viral infection, comprising administering an effective amount of a compound or pharmaceutical composition disclosed herein to a subject in need thereof. In certain embodiments, the viral infection is Zika virus infection. In other embodiments, the viral infection is Eastern equine encephalitis, Western equine encephalitis, and Benevolent Equine Encephalitis. These include Zuehne encephalitis (EEE, WEE, and VEE, respectively), chikungunya fever (CHIK), Ebola, influenza, or RSV.

[0013] In certain embodiments, the compound or pharmaceutical composition is administered orally, intravenously, or through the lungs, i.e., intrapulmonaryly.

[0014] In certain embodiments, this disclosure relates to the use of compounds as described herein in the production of agents for treating or preventing viral infections such as eastern equine encephalitis, western equine encephalitis, and Venezuelan equine encephalitis (EEE, WEE, and VEE, respectively), chikungunya fever (CHIK), Ebola, influenza, RSV, or Zika virus infection.

[0015] In certain embodiments, this disclosure relates to a method for producing compounds disclosed herein by mixing the starting materials and reagents disclosed herein under conditions such that the compounds are formed.

[0016] Additional advantages are some described in the following description, some are evident from that description, or can be learned by the implementation of the embodiments described below. The advantages described below will be realized and achieved by the elements and combinations specifically indicated in the attached claims. It should be understood that both the summary of the invention above and the embodiments for carrying out the invention below are merely illustrative and descriptive, and not limiting. In embodiments of the present invention, for example, the following items are provided. (Item 1) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula I or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, X is CH2, CHCH3, C(CH3)2, CHF, CF2, or CD2. Y is either N or CR', Z is N or CR'', R' is hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, or carbonyl, and R' is optionally one or more of the same or different R's. 10 Replaced by, R'' is hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, hydroxyl, thiol, or carbonyl, and R' is optionally one or more of the same or different R 10 Replaced by, R 1 , R 2 , R 3 , and R 5is, independently of each other, H, an optionally substituted ester, an optionally substituted branched ester, an optionally substituted carbonate, an optionally substituted carbamate, an optionally substituted thioester, an optionally substituted branched thioester, an optionally substituted thiocarbonate, an optionally substituted S-thiocarbonate, an optionally substituted dithiocarbonate, an optionally substituted thiocarbamate, an optionally substituted oxymethoxycarbonyl, an optionally substituted oxymethoxythiocarbonyl, an optionally substituted oxymethylcarbonyl, an optionally substituted oxymethylthiocarbonyl, an L-amino acid ester, a D-amino acid ester, an N-substituted L-amino acid ester, an N,N-disubstituted L-amino acid ester, an N-substituted D-amino acid ester, an N,N-disubstituted D-amino acid ester, an optionally substituted sulfenyl, an optionally substituted imidate, an optionally substituted hydrazonate, an optionally substituted oxymyl, an optionally substituted imidinyl, an optionally substituted imidyl, an optionally substituted aminals, an optionally substituted hemiaminals, an optionally substituted acetals, an optionally substituted hemiacetals, an optionally substituted carbonimidate, an optionally substituted thiocarbonimidate, an optionally substituted carbonimidyl, an optionally substituted carbamimidate, an optionally substituted carbamimidyl, an optionally substituted thioacetal, an optionally substituted S-acyl-2-thioethyl, an optionally substituted bis-(acyloxybenzyl) ester, an optionally substituted (acyloxybenzyl) ester, and a BAB ester, R 1 R 2 R 3 and R 5 are optionally substituted with one or more identical or different R 10 and R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 2) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula II or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, X is CH2, CHCH3, C(CH3)2, CHF, CF2, or CD2. Y is either N or CR', Z is N or CR'', R' is deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, or carbonyl, and R' is optionally one or more of the same or different R's. 10 Replaced by, R'' is hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, hydroxyl, thiol, or carbonyl Yes, R' is one or more identical or different R's, at will. 10 Replaced by, R 1 , R 2 , R 3 , and R 5Each of these independently comprises H, an optionally substituted ester, an optionally substituted branched ester, an optionally substituted carbonate, an optionally substituted carbamate, an optionally substituted thioester, an optionally substituted branched thioester, an optionally substituted thiocarbonate, an optionally substituted S-thiocarbonate, an optionally substituted dithiocarbonate, an optionally substituted thiocarbamate, an optionally substituted oxymethoxycarbonyl, an optionally substituted oxymethoxythiocarbonyl, an optionally substituted oxymethylcarbonyl, an optionally substituted oxymethylthiocarbonyl, an optionally substituted L-amino acid ester, a D-amino acid ester, an N-substituted L-amino acid ester, an N,N-disubstituted L-amino acid ester, an N-substituted D-amino acid ester, an N,N-disubstituted D-amino acid ester, an optionally substituted L-amino acid ester, an optionally substituted L-amino acid ester, an N-substituted D-amino acid ester, an optionally substituted D-amino acid ester, an optionally substituted L-amino acid ester, an N-substituted L-amino acid ester, an N-substituted D-amino acid ester, an optional D-substituted L-amino acid ester, an optionally substituted L-substituted L-amino acid ester, an N-substituted D-amino acid ester, an optional D-substituted L Selected from selectively substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, However, R 1 , R 2 , R 3 , and R 5 However, provided that not all of them are H, R10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclocycleamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heteroacrylatethio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 3) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula III or a pharmaceutically or physiological salt thereof, [ka] During the ceremony, X is CH2, CHCH3, C(CH3)2, CHF, CF2, or CD2. Z is N or CR'', R'' is deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, hydroxyl, thiol, or carbonyl, and R' is optionally one or more of the same or different R 10 Replaced by, R 1 , R 2 , R 3 , and R 5Each of these independently comprises H, an optionally substituted ester, an optionally substituted branched ester, an optionally substituted carbonate, an optionally substituted carbamate, an optionally substituted thioester, an optionally substituted branched thioester, an optionally substituted thiocarbonate, an optionally substituted S-thiocarbonate, an optionally substituted dithiocarbonate, an optionally substituted thiocarbamate, an optionally substituted oxymethoxycarbonyl, an optionally substituted oxymethoxythiocarbonyl, an optionally substituted oxymethylcarbonyl, an optionally substituted oxymethylthiocarbonyl, an optionally substituted L-amino acid ester, a D-amino acid ester, an N-substituted L-amino acid ester, an N,N-disubstituted L-amino acid ester, an N-substituted D-amino acid ester, an N,N-disubstituted D-amino acid ester, an optionally substituted L-amino acid ester, an optionally substituted L-amino acid ester, an N-substituted D-amino acid ester, an optionally substituted D-amino acid ester, an optionally substituted L-amino acid ester, an N-substituted L-amino acid ester, an N-substituted D-amino acid ester, an optional D-substituted L-amino acid ester, an optionally substituted L-substituted L-amino acid ester, an N-substituted D-amino acid ester, an optional D-substituted L Selected from selectively substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, However, R 1 , R 2 , R 3 , and R 5 However, provided that not all of them are H, R10 Deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicamino, cycloalkamino, cycloalkenamino, aryl Kilthio, carbocyclilthio, heterocarbocyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 4) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula IV or a pharmaceutically or physiological salt thereof, [ka] During the ceremony, X is CHCH3, C(CH3)2, CHF, CF2, or CD2. R 1 , R 2 , R 3 , and R 5 These are, independently, H, optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, and L-amino acid esters. D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidi Selected from R, optionally substituted carbamidyl, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, 1 , R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, However, R 1 , R 2 , R 3 , and R 5 However, provided that not all of them are H, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 5) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula V or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 1 , R 2 , R 3 , and R 5 These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally Selectively substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally Selected from selectively substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 6) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula VI or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 1 , R 2 , and R 3 These are, independently of each other, the following: optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally Selected from selectively substituted imidates, optionally substituted hydrazonates, optionally substituted oxymyls, optionally substituted imidinyls, optionally substituted imidyls, optionally substituted aminals, optionally substituted hemiaminals, optionally substituted acetals, optionally substituted hemiacetals, optionally substituted carbonimidates, optionally substituted thiocarbonimidates, optionally substituted carbonimidyls, optionally substituted carbamidates, optionally substituted carbamidyls, optionally substituted thioacetals, optionally substituted S-acyl-2-thioethyls, optionally substituted bis-(acyloxybenzyl) esters, optionally substituted (acyloxybenzyl) esters, and BAB esters, R 1 , R 2 , and R 3is optionally substituted by one or more identical or different R 10 and R 10 is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclic, heterocarbocyclic, aryl, heteroaryl, heterocyclic, cycloalkyl, cycloalkenyl, alkoxy, carbocycloxy, heterocarbocycloxy, aryloxy, heteroaryloxy, heterocycloxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyclamino, heterocarbocyclamino, arylamino, heteroarylamino, heterocyclamino, cycloalkylamino, cycloalkenylamino, alkylthio, carbocyclicthio, heterocarbocyclicthio, arylthio, heteroarylthio, heterocyclicthio, cycloalkylthio, cycloalkenylthio, arenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R 10 is optionally substituted by one or more identical or different R 11 and R 11 is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclic, heterocarbocyclic, aryl, heteroaryl, heterocyclic, cycloalkyl, cycloalkenyl, alkoxy, carbocycloxy, heterocarbocycloxy, aryloxy, heteroaryloxy, heterocycloxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyclamino, heterocarbocyclamino, arylamino, heteroarylamino, heterocyclamino, cycloalkylamino, cycloalkenylamino, al kylthio, carbocyclicthio, heterocarbocyclicthio, arylthio, heteroarylthio, heterocyclicthio, cycloalkylthio, cycloalkenylthio, arenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 7) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formulas VIa-f or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 1 , R 2 , and R 3 These are, independently of each other, the following: optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acids Esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidide, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl Selected from -2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 、R 2 、and R 3 are optionally substituted with one or more of the same or different R 10 ; R 10 is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclic, heterocarbocyclic, aryl, heteroaryl, heterocyclic, cycloalkyl, cycloalkenyl, alkoxy, carbocycloxy, heterocarbocycloxy, aryloxy, heteroaryloxy, heterocycloxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyclicamino, heterocarbocyclicamino, arylamino, heteroarylamino, heterocyclicamino, cycloalkylamino, cycloalkenylamino, alkylthio, carbocyclicthio, heterocarbocyclicthio, arylthio, heteroarylthio, heterocyclicthio, cycloalkylthio, cycloalkenylthio, arenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R 10 is optionally substituted with one or more of the same or different R 11 ; R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 8) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula VII or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 1 , R 2 , and R 5 These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyls, optionally substituted oxymethoxythiocarbonyls, optionally substituted oxy methylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiamine Selected from R, optionally substituted acetals, optionally substituted hemiacetals, optionally substituted carbonimidates, optionally substituted thiocarbonimidates, optionally substituted carbonimidyls, optionally substituted carbamidates, optionally substituted carbamidyls, optionally substituted thioacetals, optionally substituted S-acyl-2-thioethyls, optionally substituted bis-(acyloxybenzyl) esters, optionally substituted (acyloxybenzyl) esters, and BAB esters, 1 , R 2 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 9) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula VIII or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 1 , R 3 , and R 5 These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from selectively substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1, R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 Deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, hetero These are reel amino acids, heterocycline amino acids, cycloalkamino acids, cycloalkeneamino acids, alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipids, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 10) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula IX or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 2 , R 3 , and R 5These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from selectively substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 10Deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, hetero Rylamino, heterocyclamino, cycloalkamino, cycloalkenamino, alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 11) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula X or a pharmaceutically or physiologically salted thereof, [ka] During the ceremony, R 1 and R 5 These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters Stellate, N,N-disubstituted L-amino acid ester, N-substituted D-amino acid ester, N,N-disubstituted D-amino acid ester, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally Selected from thioacetals substituted with, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) esters, optionally substituted (acyloxybenzyl) esters, and BAB esters, R1 and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 12) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XI or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 1 and R 3 These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethyl Carbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid ester, D-amino acid ester, N-substituted L-amino acid ester, N,N-disubstituted L-amino acid ester, N-substituted D-amino acid ester, N,N-disubstituted D-amino acid ester, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal Selected from optionally substituted acetals, optionally substituted hemiacetals, optionally substituted carbonimidates, optionally substituted thiocarbonimidates, optionally substituted carbonimidyls, optionally substituted carbamidates, optionally substituted carbamidyls, optionally substituted thioacetals, optionally substituted S-acyl-2-thioethyls, optionally substituted bis-(acyloxybenzyl) esters, optionally substituted (acyloxybenzyl) esters, and BAB esters, R 1 and R 3 This is an optional choice of one or more identical or different R 10 Replaced by, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 13) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XII or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 1 and R 2 These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from selectively substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 and R2 This is an optional choice of one or more identical or different R 10 Replaced by, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 Deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicamino, cycloalkamino, cycloalkenamino, aryl These are kylthio, carbocyclilthio, heterocarbocyclilthio, arylthio, heteroarylthio, heterocyclilthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 14) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XIII or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 2 and R 5These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from selectively substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 2 and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 10Deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclocycleamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykrillthio, heterocarbocykrillthio, arylthio, heteroaryl R is a chlorothio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 15) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XIV or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 2 and R 3 These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N - Disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidide, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted Selected from (acyloxybenzyl) esters and BAB esters, R 2 and R 3 This is an optional choice of one or more identical or different R 10 Replaced by, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 16) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XV or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 3 and R 5These are, independently of each other, the following: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from selectively substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 3 and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 17) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XVI or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 2 The following are: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 2 This is an optional choice of one or more identical or different R 10Replaced by, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 18) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XVII or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 3The following are: optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from substituted sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 3 This is an optional choice of one or more identical or different R 10 Replaced by, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 19) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XVIII or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 1 The following are examples: optionally substituted branched esters, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imide Selected from optionally substituted hydrazonates, optionally substituted oxymyls, optionally substituted imidinyls, optionally substituted imidyls, optionally substituted aminals, optionally substituted hemiaminals, optionally substituted acetals, optionally substituted hemiacetals, optionally substituted carbonimidates, optionally substituted thiocarbonimidates, optionally substituted carbonimidyls, optionally substituted carbamidates, optionally substituted carbamidyls, optionally substituted thioacetals, optionally substituted S-acyl-2-thioethyls, optionally substituted bis-(acyloxybenzyl) esters, optionally substituted (acyloxybenzyl) esters, and BAB esters, R 1 This is an optional choice of one or more identical or different R 10 Replaced by, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 20) A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula XIX or a pharmaceutically or physiologically salt thereof, [ka] During the ceremony, R 5 The following are: optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted Selected from substituted hydrazonates, optionally substituted oxymyls, optionally substituted imidinyls, optionally substituted imidyls, optionally substituted aminals, optionally substituted hemiaminals, optionally substituted acetals, optionally substituted hemiacetals, optionally substituted carbonimidates, optionally substituted thiocarbonimidates, optionally substituted carbonimidyls, optionally substituted carbamidates, optionally substituted carbamidyls, optionally substituted thioacetals, optionally substituted S-acyl-2-thioethyls, optionally substituted bis-(acyloxybenzyl) esters, optionally substituted (acyloxybenzyl) esters, and BAB esters, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. A pharmaceutical composition in which the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 21) R 1 , R 2 , R 3 , and R 5 However, each is independent of H, [ka] [ka] Selected from, Y 1 is either O or S, Y 3 is OH or BH3 - M + And, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9 These can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. The pharmaceutical composition according to item 1, wherein the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 22) R 1 However, hydrogen, [ka] The pharmaceutical composition described in item 21. (Item 23) R ’ The pharmaceutical composition described in item 1, wherein the active ingredient is methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, trijuteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl. (Item 24) R ” The pharmaceutical composition described in item 1, wherein the active ingredient is methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, trijuteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl. (Item 25) R ’ The pharmaceutical composition described in item 2, wherein the active ingredient is methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, trijuteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl. (Item 26) R ” The pharmaceutical composition described in item 2, wherein the active ingredient is methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, trijuteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl. (Item 27) The pharmaceutical composition described in item 3, wherein R'' is methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, triduteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl. (Item 28) R 1 , R 2 , R 3 , and R 5 However, each is independent of H, [ka] [ka] Selected from, However, R 1 , R 2 , R 3 , and R 5 However, provided that not all of them are H, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9 These can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclocycleamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heteroacrylatethio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. The pharmaceutical composition according to any one of items 2-5 or 8-17, wherein the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 29) R 1 , R 2 , and R 3 However, each is independent of the following: [ka] [ka] Selected from, R 6 is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, optionally substituted phenyl, optionally substituted aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicleamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid, R 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9 These can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclocycleamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heteroacrylatethio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. The pharmaceutical composition according to item 6 or 7, wherein the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 30) R 1 However, the following: [ka] [ka] Selected from, R 6 These are hydrogen, C1-C7n-alkyl, and C9-C 22 n-alkyl, optionally substituted C8n-alkyl, branched alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, -O(C1~C6n-alkyl), -O(C8~C 21 n-alkyl), optionally substituted -O(C7n-alkyl), -O(branched alkyl)carbocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, -NH(C1~C6n-alkyl), -NH(C8~C 21 n-alkyl), optionally substituted -NH(C7n-alkyl), -NH(branched alkyl)(alkyl)2amino, carbocylicamino, heterocarbocylicamino, arylamino, heteroarylamino, heterocyclicamino, cycloalkamino, cycloalkeneamino, alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid, R 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9 These can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11 These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. The pharmaceutical composition according to item 18, wherein the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 31) R 5 However, the following: [ka] [ka] Selected from, R 6 These are hydrogen, C2-C7n-alkyl, optionally substituted C8n-alkyl, C9-C 22 n-alkyl, alkenyl, alkynyl, carbocyrill, heterocarbocyrill, aryl, heteroaryl, heterocyclyl, C3-C9 cycloalkyl, C 11 ~C 22 Cycloalkyl, optionally substituted C 10 Cycloalkyl, cycloalkenyl, -O(C1~C6n-alkyl), -O(optionally substituted C7n-alkyl), -O(C8~C 21 n-alkyl), -O (branched alkyl), carbocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, -N(C2~C 21 n-alkyl)2, -N(optionally substituted C1 alkyl)2, -NH(optionally substituted C1 alkyl), -NH(C2~C6n-alkyl), -NH(optionally substituted C7n-alkyl), -NH(C8~C 15 n-alkyl), -NH (optionally substituted C 16 n-alkyl), -NH(C 17 n-alkyl), -NH (optionally substituted C 18 n-alkyl), -NH(C 19 ~C 21n-alkyl), -NH(branched alkyl), -N(branched alkyl)2, carbocyamino, heterocarbocyamino, optionally substituted arylamino, heteroarylamino, heterocyclamino, cycloalkamino, cycloalkenamino, alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipids, R 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9These can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. The pharmaceutical composition according to item 19, wherein the lipid is a C11-C22 higher alkyl, a C11-C22 higher alkoxy, polyethylene glycol, or an alkyl-substituted aryl, or a lipid as described herein. (Item 32) Pharmacologically acceptable excipients, and the following: [ka] A pharmaceutical composition comprising a compound selected from the above. (Item 33) Pharmacologically acceptable excipients, and the following: [ka] A pharmaceutical composition comprising a compound selected from the above. (Item 34) Pharmacologically acceptable excipients, and the following: [ka] A pharmaceutical composition comprising a compound selected from the above. (Item 35) Pharmacologically acceptable excipients, and the following: [ka] A pharmaceutical composition comprising a compound selected from the above. (Item 36) Pharmacologically acceptable excipients, and the following: [ka] A pharmaceutical composition comprising a compound selected from the above. (Item 37) Pharmacologically acceptable excipients, and the following: [ka] A pharmaceutical composition comprising a compound selected from the above. (Item 38) Pharmacologically acceptable excipients, and the following: [ka] A pharmaceutical composition comprising a compound selected from the above. (Item 39) Pharmacologically acceptable excipients, and the following: [ka] A pharmaceutical composition comprising a compound selected from the above. (Item 40) A pharmaceutically acceptable excipient and a compound having the following structure. [ka] A pharmaceutical composition comprising a pharmaceutically acceptable salt or physiological salt thereof. (Item 41) A pharmaceutically acceptable excipient and a compound having the following structure. [ka] A pharmaceutical composition comprising a pharmaceutically acceptable salt or physiological salt thereof. (Item 42) A pharmaceutically acceptable excipient and a compound having the following structure. [ka] A pharmaceutical composition comprising a pharmaceutically acceptable salt or physiological salt thereof. (Item 43) A pharmaceutical composition according to any one of items 1 to 42, further comprising a propellant. (Item 44) The pharmaceutical composition according to item 43, wherein the propellant is compressed air, ethanol, nitrogen, carbon dioxide, nitrous oxide, hydrofluoroalkane (HFA), 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, or a combination thereof. (Item 45) A pressurized container containing a pharmaceutical composition as described in any one of items 1 to 42. (Item 46) The containers described in item 45, which are manual pump sprayers, inhalers, measuring inhalers, dry powder inhalers, atomizers, vibrating mesh atomizers, jet atomizers, or ultrasonic atomizers. (Item 47) A method for treating or preventing a viral infection, comprising administering an effective amount of any one of items 1 to 42 to a subject in need thereof. (Item 48) The method according to item 47, wherein the viral infection is an alphavirus. (Item 49) The method according to item 48, wherein the virus is selected from Eastern equine encephalitis virus, Western equine encephalitis virus, Venezuelan equine encephalitis virus, Chikungunya virus, and Ross River virus. (Item 50) The method described in item 47, wherein the viral infection is a coronavirus. (Item 51) The method according to item 50, wherein the viral infection is human coronavirus, SARS coronavirus, and MERS coronavirus. (Item 52) The method described in item 47, wherein the viral infection is a filoviridae virus. (Item 53) The method according to item 52, wherein the viral infection is the Ebola virus. (Item 54) The method according to item 47, wherein the viral infection is an orthomyxoviridae virus. (Item 55) The method according to item 54, wherein the viral infection is influenza A virus and influenza B virus. (Item 56) The method described in item 47, wherein the viral infection is a paramyxoviridae virus. (Item 57) The method according to item 56, wherein the viral infection is RSV. (Item 58) A method for treating or preventing infection in patients with human coronavirus, SARS coronavirus, MERS coronavirus, Eastern equine encephalitis virus, Western equine encephalitis virus, Venezuelan equine encephalitis virus, Chikungunya virus, and Ross River infection, orthomyxoviridae viruses or paramyxoviridae viruses or RSV virus, or influenza A virus and influenza B virus, or filoviridae viruses or Ebola virus, comprising the following structure: [ka] A method comprising administering an effective amount of a compound having the same or a pharmaceutically acceptable salt or physiological salt thereof to a patient in need. (Item 59) A method for treating or preventing infection in patients with human coronavirus, SARS coronavirus, MERS coronavirus, Eastern equine encephalitis virus, Western equine encephalitis virus, Venezuelan equine encephalitis virus, Chikungunya virus, and Ross River infection, orthomyxoviridae viruses or paramyxoviridae viruses or RSV virus, or influenza A virus and influenza B virus, or filoviridae viruses or Ebola virus, comprising the following structure: [ka] A method comprising administering an effective amount of a compound having the same or a pharmaceutically acceptable salt or physiological salt thereof to a patient in need. (Item 60) A method for treating or preventing infection in patients with human coronavirus, SARS coronavirus, MERS coronavirus, Eastern equine encephalitis virus, Western equine encephalitis virus, Venezuelan equine encephalitis virus, Chikungunya virus, and Ross River infection, orthomyxoviridae viruses or paramyxoviridae viruses or RSV virus, or influenza A virus and influenza B virus, or filoviridae viruses or Ebola virus, comprising the following structure: [ka] A method comprising administering an effective amount of a compound having the same or a pharmaceutically acceptable salt or physiological salt thereof to a patient in need. [Brief explanation of the drawing]

[0017] The accompanying figures incorporated herein and constituting part thereof illustrate several embodiments described below.

[0018] [Figure 1]This is a scheme illustrating the preparation of β-DN-hydroxycytidine. The synthesis steps are: a) TBSCl, DMAP, DIPEA, DCM; b) (2,4,6-iPr)PhSO2Cl, DIPEA, DMAP, DCM; c) NH2OH-HCl, DIPEA, DCM; d) F source; and e) aqueous solution of NH2OH, AcOH, at 50°C. [Figure 2] Specific exemplary compounds are given as examples. [Figure 3] Specific exemplary compounds are given as examples. [Figure 4] The mean plasma concentrations and pharmacokinetic parameters derived from mice treated with exemplary compounds are shown. [Figure 5] This shows nucleoside accumulation in mouse organs in mice treated with exemplary compounds. [Figure 6] This shows triphot phosphate accumulation in mouse organs in mice treated with exemplary compounds. [Figure 7] This shows a reduction in paw pad swelling in CHIKV challenge mice treated with exemplary compounds. [Figure 8] This shows the reduction of CHIKV-RNA copies by PCR in CHIKV challenge mice treated with exemplary compounds. [Figure 9] This shows the survival of ZIKV challenge mice treated with exemplary compounds for 7 days. [Figure 10] This shows the survival of ZIKV challenge mice treated for 7 days with representative compounds, with varying post-infection treatment initiation times. [Figure 11] This shows the tissue concentration of N4-hydroxycytidine nucleoside derived from cynomolgus monkeys that were orally administered EIDD-1931 (100 mg / kg). [Figure 12] This shows the tissue concentration of N4-hydroxycytidine nucleoside derived from cynomolgus monkeys that received intravenous administration of EIDD-1931 (10 mg / kg). [Figure 13] The structure of the compound administered orally to cynomolgus monkeys is shown. [Figure 14]This shows the average plasma concentration of N4-hydroxycytidine nucleoside derived from cynomolgus monkeys administered orally with ester derivatives. [Figure 15] This shows the mean maximum concentration of N4-hydroxycytidine nucleoside in cynomolgus monkey plasma administered orally with ester derivatives. [Figure 16] This shows viral titers from nasal lavage and fever in influenza A / California / 07 / 2009(H1N1) infected ferrets orally treated with EIDD-2801 BID or vehicle. [Figure 17] This paper shows viral titers from nasal lavage, fever, and nasal turbinates in ferrets infected with influenza A / Wisconsin / 67 / 2005(H3N2) that were orally treated with EIDD-2801 BID or vehicle. [Figure 18] This study demonstrates the effect of EIDD-2801 treatment on the survival of mice infected with intranasal VEEV. [Figure 19] This study demonstrates the effect of EIDD-2801 hours of treatment initiation on the survival of mice infected with intranasal VEEV. [Figure 20] This study demonstrates the effect of EIDD-2801 prophylactic treatment on lung virus titers in SARS-infected mice. [Figure 21] This study demonstrates the effect of EIDD-2801 treatment time on pulmonary hemorrhage scores in SARS-infected mice. [Figure 22] This study demonstrates the effect of EIDD-2801 treatment time on lung virus titers in SARS-infected mice. [Figure 23] This study demonstrates the effect of EIDD-2801 treatment on pulmonary hemorrhage scores in MER-infected mice. [Modes for carrying out the invention]

[0019] Before describing this disclosure in more detail, it should be understood that this disclosure is not limited to the specific embodiments described and is therefore naturally subject to change. It should also be understood that the terms used herein are solely for the purpose of describing specific embodiments and are not intended to limit the scope of this disclosure to the extent that it is limited by the appended claims.

[0020] Unless otherwise defined, all technical and scientific terms used herein have the same meanings as those generally understood by those skilled in the art to which this disclosure pertains. Any methods and materials similar to or equivalent to those described herein may be used in the implementation or testing of this disclosure, but preferred methods and materials are described herein.

[0021] All publications and patents cited herein are incorporated herein by reference as if each individual publication or patent were specifically and individually indicated to be incorporated by reference, and are incorporated herein by reference to disclose and describe the manner and / or material by which the publications are cited. No publication is cited for its disclosure prior to the filing date, and this disclosure should not be construed as acknowledging that there is no right to date such publication prior to the filing date based on prior disclosure. Furthermore, the publication dates provided may differ from the actual publication dates which may need to be independently verified.

[0022] As will become apparent to those skilled in the art upon reading this disclosure, each of the individual embodiments described and illustrated herein has distinct components and features, which can be readily separated from or combined with any of several other embodiments without departing from the scope or spirit of this disclosure. Any enumerated method may be performed in the order of the enumerated events, or in any other logically possible order.

[0023] Embodiments of this disclosure will, unless otherwise indicated, utilize techniques within the scope of the art, such as medicine, organic chemistry, biochemistry, molecular biology, and pharmacology. Such techniques are adequately described in the literature.

[0024] In certain embodiments, agents, which may be in the form of a salt or prodrug, are administered by a method disclosed herein, which is specified by weight. This refers to the weight of the enumerated compounds. If the compound is in the form of a salt or prodrug, the weight is the molar equivalent of the corresponding salt or prodrug.

[0025] It should be noted that, as used herein and in the appended claims, the singular forms “a,” “an,” and “the” include plural references unless the context explicitly indicates otherwise.

[0026] "Subject" refers to any animal, preferably a human patient, livestock, or household pet.

[0027] As used herein, the terms “prevent” and “preventing” include prevention of recurrence, spread, or onset. This disclosure is not intended to be limited to complete prevention. In some embodiments, onset is delayed or the severity of the disease is reduced.

[0028] As used herein, the terms “to treat” and “to treat” are not limited to cases where the subject (e.g., a patient) is cured and the disease is eradicated. Rather, embodiments of the present disclosure may also intend to treat merely symptoms and / or slow the progression of the disease.

[0029] As used herein, the term “in combination with” means, when used to describe administration with additional treatment, that the drugs may be administered before, together with, or after, or in combination with, the additional treatment.

[0030] As used herein, “alkyl” refers to a straight-chain or branched-chain saturated hydrocarbon moiety, such as those containing 1 to 10 carbon atoms. “Higher alkyl” refers to a saturated hydrocarbon having 11 or more carbon atoms. 16 " refers to alkyl groups containing 6 to 16 carbon atoms. Similarly, "C6~C 22 "Alkyl" refers to alkyl groups containing 6 to 22 carbon atoms. Typical saturated linear alkyl groups include methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, n-septyl, n-octyl, and n-nonyl, while saturated branched alkyl groups include isopropyl, sec-butyl, isobutyl, tert-butyl, and isopentyl.

[0031] As used herein, the term "alkenyl" refers to an unsaturated, linear, or branched hydrocarbon moiety containing a double bond. Unless otherwise specified, C2-C 24 (For example, C2~C 22 , C2~C 20 , C2~C 18 , C2~C 16 , C2~C 14 , C2~C 12 , C2~C 10Alkenyl groups (C2-C8, C2-C6, or C2-C4) are intended. The alkenyl group may contain one or more unsaturated bonds.Examples include ethenyl, 1-propenyl, 2-propenyl, 1-methylethenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-methyl-1-propenyl, 2-methyl-1-propenyl, 1-methyl-2-propenyl, 2-methyl-2-propenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-methyl-1-butenyl, 2-methyl-1-butenyl, 3-methyl-1-butenyl, 1-methyl-2-butenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl, 1-methyl-3-butenyl, 2-methyl-3-butenyl 3-methyl-3-butenyl, 1,1-dimethyl-2-propenyl, 1,2-dimethyl-1-propenyl, 1,2-dimethyl-2-propenyl, 1-ethyl-1-propenyl, 1-ethyl-2-propenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl-1-pentenyl, 2-methyl-1-pentenyl, 3-methyl-1-pentenyl, 4-methyl-1-pentenyl, 1-methyl-2-pentenyl, 2-methyl-2-pentenyl, 3-methyl-2-pentenyl, 4-methyl-2-pentenyl, 1-methyl 3-methyl-3-pentenyl, 2-methyl-3-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1-methyl-4-pentenyl, 2-methyl-4-pentenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,1-dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 1,2-dimethyl-1-butenyl, 1,2-dimethyl-2-butenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl-1-butenyl, 1,3-dimethyl-2-butenyl, 1,3-dimethyl-3-butenyl, 2,2-dimethyl-3-butenyl Examples include nyl, 2,3-dimethyl-1-butenyl, 2,3-dimethyl-2-butenyl, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-1-butenyl, 3,3-dimethyl-2-butenyl, 1-ethyl-1-butenyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl, 2-ethyl-1-butenyl, 2-ethyl-2-butenyl, 2-ethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1-ethyl-1-methyl-2-propenyl, 1-ethyl-2-methyl-1-propenyl, and 1-ethyl-2-methyl-2-propenyl.The term "vinyl" refers to a group having the structure -CH=CH2, 1-propenyl refers to a group having the structure -CH=CH-CH3, and 2-propenyl refers to a group having the structure -CH2-CH=CH2. (Z. 1 Z 2 )C=C(Z 3 Z 4 Asymmetric structures such as ) are intended to include both E and Z isomers. This can be assumed in the structural formulas herein if asymmetric alkenes are present, or it can be explicitly indicated by the bond symbol C=C.

[0032] As used herein, the term "alkynyl" refers to a straight-chain or branched-chain hydrocarbon moiety containing a triple bond. Unless otherwise specified, C2-C 24 (For example, C2~C 24 , C2~C 20 , C2~C 18 , C2~C 16 , C2~C 14 , C2~C 12 , C2~C 10Alkynyl groups (C2-C8, C2-C6, or C2-C4) are intended. Alkynyl groups may contain more than one unsaturated bond. Examples include ethynyl, 1-propynyl, 2-propynyl (or propargyl), 1-butynyl, 2-butynyl, 3-butynyl, 1-methyl-2-propynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 3-methyl-1-butynyl, 1-methyl-2-butynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, 1,1-dimethyl-2-propynyl, 1-ethyl-2-propynyl, 1-hexynyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 5-hexynyl, 3-methyl-1-pentynyl, 4-methyl-1-pentynyl, 1- Examples of C2-C6 alkynyls include methyl-2-pentynyl, 4-methyl-2-pentynyl, 1-methyl-3-pentynyl, 2-methyl-3-pentynyl, 1-methyl-4-pentynyl, 2-methyl-4-pentynyl, 3-methyl-4-pentynyl, 1,1-dimethyl-2-butynyl, 1,1-dimethyl-3-butynyl, 1,2-dimethyl-3-butynyl, 2,2-dimethyl-3-butynyl, 3,3-dimethyl-1-butynyl, 1-ethyl-2-butynyl, 1-ethyl-3-butynyl, 2-ethyl-3-butynyl, and 1-ethyl-1-methyl-2-propynyl.

[0033] Non-aromatic monocyclic or polycyclic alkyl groups are referred to herein as "carbocyclic" or "carbocykyl" groups. Typical saturated carbocyclic groups include cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl, while unsaturated carbocyclic groups include cyclopentenyl and cyclohexenyl.

[0034] A "heterocarbocyclic" group is a carbon ring containing 1 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, which can be saturated or unsaturated (but not aromatic), monocyclic or polycyclic, and the nitrogen and sulfur heteroatoms can be optionally oxidized, and the nitrogen heteroatom can be optionally quaternized. Examples of heterocarbocyclic groups include morpholinyl, pyrrolidinonyl, pyrrolidinyl, piperidinyl, hydantoinyl, valerolactamyl, oxyranyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydropyridinyl, tetrahydroprimidinyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, tetrahydropyrimidinyl, tetrahydropyrimidinyl, tetrahydrothiophenyl, and tetrahydrothiopyranyl.

[0035] The term "aryl" preferably refers to a 6-12 membered aromatic homocyclic (i.e., hydrocarbon) monocyclic, bicyclic, or tricyclic ring-containing group, such as phenyl, naphthyl, and biphenyl. Phenyl is a preferred aryl group. The term "substituted aryl" preferably refers to an aryl group substituted with one or more groups selected from alkyl, substituted alkyl, alkenyl (optionally substituted), aryl (optionally substituted), heterocyclo (optionally substituted), halo, hydroxy, alkoxy (optionally substituted), aryloxy (optionally substituted), alkanoyl (optionally substituted), aroyl (optionally substituted), alkyl ester (optionally substituted), aryl ester (optionally substituted), cyano, nitro, amino, substituted amino, amide, lactam, urea, urethane, sulfonyl, etc., where one or more substituents optionally form a 3-7 membered ring with the atom to which they are bonded.

[0036] As used herein, “heteroaryl” or “heteroaromatic” refers to an aromatic heterocarbon ring containing at least one carbon atom, having 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulfur, and including both monocyclic and polycyclic ring systems. A polycyclic ring system may contain one or more nonaromatic rings, but is not required, as long as one of the rings is aromatic. Representative heteroaryls include furyl, benzofuranyl, thiophenyl, benzothiophenyl, pyrrolyl, indolyl, isoindolyl, azaindolyl, pyridyl, quinolinyl, isoquinolinyl, oxazolyl, isoxazolyl, benzoxazolyl, pyrazolyl, pyrazolyl, imidazolyl, benzimimidazolyl, thiazolyl, benzothiazolyl, isothiazolyl, pyridadinyl, pyrimidinyl, pyrazinyl, triazinyl, cinolinyl, phthalazinyl, and quinazolyl. The use of the term "heteroaryl" is intended to include N-alkylated derivatives such as 1-methylimidazole-5-yl substituents.

[0037] As used herein, “heterocyclic” refers to monocyclic and polycyclic systems having 1 to 4 heteroatoms selected from nitrogen, oxygen, and sulfur, and containing at least one carbon atom. Monocyclic and polycyclic systems may be aromatic rings, non-aromatic rings, or mixtures of aromatic and non-aromatic rings. Heterocyclic systems include heterocarbon rings, heteroaryl rings, and the like.

[0038] "Alkylthio" refers to an alkyl group, as defined above, having the indicated number of carbon atoms linked through a sulfur bridge. An example of alkylthio is methylthio (i.e., -S-CH3).

[0039] "Alkoxy" refers to an alkyl group having the indicated number of carbon atoms, as defined above, linked through an oxygen crosslink. Examples of alkoxys include, but are not limited to, methoxy, ethoxy, n-propoxy, i-propoxy, n-butoxy, s-butoxy, t-butoxy, n-pentoxy, and s-pentoxy. Preferred alkoxy groups are methoxy, ethoxy, n-propoxy, i-propoxy, n-butoxy, s-butoxy, and t-butoxy.

[0040] "Alkylamino" refers to an alkyl group, as defined above, having the indicated number of carbon atoms linked through an amino crosslink. An example of alkylamino is methylamino (i.e., -NH-CH3).

[0041] "Alkanoyl" refers to an alkyl group (i.e., -(C=O)alkyl) having the indicated number of carbon atoms linked through a carbonyl crosslink, as defined above.

[0042] "Alkylsulfonyl" refers to an alkyl (i.e., -S(=O)2 alkyl) having the indicated number of carbon atoms, as defined above, linked through a sulfonyl crosslink such as mesyl, while "arylsulfonyl" refers to an aryl (i.e., -S(=O)2 aryl) linked through a sulfonyl crosslink.

[0043] "Alkylsulfamoyl" refers to an alkyl (i.e., -NHS(=O)2alkyl) having the indicated number of carbon atoms bonded through a sulfamoyl bridge, as defined above, and "arylsulfamoyl" refers to an aryl (i.e., -NHS(=O)2aryl) bonded through a sulfamoyl bridge.

[0044] "Alkyl sulfinyl" refers to an alkyl (i.e., -S(=O) alkyl) having the indicated number of carbon atoms bonded through a sulfinyl crosslink, as defined above.

[0045] The terms "cycloalkyl" and "cycloalkenyl" refer to monocyclic, dicyclic, or tricyclic ring groups of 3 to 15 carbon atoms that are fully saturated and partially unsaturated, respectively. The term "cycloalkenyl" includes bicyclic and tricyclic ring systems that are not aromatic as a whole but contain aromatic moieties (e.g., fluorene, tetrahydronaptalene, dihydroindene, etc.). The rings of polycyclic cycloalkyl groups may be fused, crosslinked, and / or joined through one or more spirobonds. The terms "substituted cycloalkyl" and "substituted cycloalkenyl" refer, respectively, to cycloalkyl and cycloalkenyl groups substituted with one or more groups selected from, preferably, aryl, substituted aryl, heterocyclo, substituted heterocyclo, carbocyclo, substituted carbocyclo, halo, hydroxy, alkoxy (optionally substituted), aryloxy (optionally substituted), alkyl ester (optionally substituted), aryl ester (optionally substituted), alkanoyl (optionally substituted), ariol (optionally substituted), cyano, nitro, amino, substituted amino, amide, lactam, urea, urethane, sulfonyl, and the like.

[0046] The terms "halogen" and "halo" refer to fluorine, chlorine, bromine, and iodine.

[0047] The term "substituted" refers to a molecule in which at least one hydrogen atom is replaced by a substituent. When substituted, one or more of the groups are "substituents." Molecules can be multiple substituted. In the case of an oxo substituent ("=O"), two hydrogen atoms are substituted. Examples of substituents in this context include halogens, hydroxyls, alkyls, alkoxys, nitros, cyanos, oxos, carbocyclyls, carbocycloalkyls, heterocarbocyclyls, heterocarbocycloalkyls, aryls, arylalkyls, heteroaryls, heteroarylalkyls, -NRaRb, -NRaC(=O)Rb, -NRaC(=O)NRaNRb, -NRaC(=O)ORb, -NRaSO2Rb, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRb, -OC(=O)NRaRb, -ORa, -SRa, -SORa, -S(=O)2Ra, -OS(=O)2Ra, and -S(=O)2ORa. In this context, Ra and Rb may be the same or different, and independently may be hydrogen, halogen hydroxyl, alkyl, alkoxy, alkyl, amino, alkylamino, dialkylamino, carbocyrill, carbocyalkyl, heterocarbocyrill, heterocarbocyalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl.

[0048] As used herein, the term “optionally substituted” means that substitution at an additional group is optional, and therefore the specified atom may not be substituted. Thus, in the use of the term “optionally substituted,” this disclosure includes examples where the group is substituted and examples where it is not.

[0049] Examples of prodrugs that may be used to improve bioavailability include esters, optionally substituted esters, branched esters, optionally substituted branched esters, carbonates, optionally substituted carbonates, carbamates, optionally substituted carbamates, thioesters, optionally substituted thioesters, branched thioesters, optionally substituted branched thioesters, thiocarbonates, optionally substituted thiocarbonates, S-thiocarbonates, optionally substituted S-thiocarbonates, dithiocarbonates, optionally substituted Substituted dithiocarbonates, thiocarbamates, optionally substituted thiocarbonates, oxymethoxycarbonyl, optionally substituted oxymethoxycarbonyl, oxymethoxythiocarbonyl, optionally substituted oxymethoxythiocarbonyl, oxymethylcarbonyl, optionally substituted oxymethylcarbonyl, oxymethylthiocarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, sulfenyl, optionally substituted sulfenyl, imidate, optionally substituted imidate, hydrazonate, optionally substituted hydrazonate, oxymyl, optionally substituted oxymyl, imidinyl, optionally substituted imidinyl, imidyl, optionally substituted imidyl, aminal, optionally substituted aminal, hemiaminal, optionally substituted hemiaminal, acetal, optionally substituted acetal, hemiacetal, optionally substituted hemiacetal, carbonimidate, optionally substituted carbonimidate, thiocal Examples include bonimidate, optionally substituted thiocarbonimidate, carbonimidyl, optionally substituted carbonimidyl, carbamidate, optionally substituted carbamidate, carbamidyl, optionally substituted carbamidyl, thioacetal, optionally substituted thioacetal, S-acyl-2-thioethyl, optionally substituted S-acyl-2-thioethyl, bis-(acyloxybenzyl) ester, optionally substituted bis-(acyloxybenzyl) ester, (acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester.

[0050] compound In certain embodiments, this disclosure relates to compounds of formula I or their pharmaceutically or physiologically active salts. [ka] During the ceremony, X is CH2, CHCH3, C(CH3)2, CHF, CF2, or CD2. Y is either N or CR', Z is N or CR'', R' is hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, or carbonyl, and R' is optionally one or more of the same or different R's. 10 Replaced by, R'' is hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, hydroxyl, thiol, or carbonyl, and R' is optionally one or more of the same or different R 10 Replaced by, R 1 , R 2 , R 3 , and R 5 These are H, independently of each other. [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, Y 1 is either O or S, Y 3 is OH or BH3 - M + And, R6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0051] In certain embodiments, the lipids are fatty alcohols, fatty amines, or fatty thiols derived from essential and / or non-essential fatty acids.

[0052] In certain embodiments, the lipids are unsaturated, polyunsaturated, omegaunsaturated, or omega-polyunsaturated fatty alcohols, fatty amines, or fatty thiols derived from essential and / or non-essential fatty acids.

[0053] In certain embodiments, the lipids are fatty alcohols, fatty amines, or fatty thiols derived from essential and non-essential fatty acids having one or more carbon units substituted with oxygen, nitrogen, or sulfur.

[0054] In certain embodiments, the lipids are unsaturated, polyunsaturated, omegaunsaturated, or omega-polyunsaturated fatty alcohols, fatty amines, or fatty thiols derived from essential and / or non-essential fatty acids having one or more of their carbon units substituted with oxygen, nitrogen, or sulfur.

[0055] In certain embodiments, the lipids are optionally substituted fatty alcohols, fatty amines, or fatty thiols derived from essential and / or non-essential fatty acids.

[0056] In certain embodiments, the lipids are optionally substituted unsaturated, polyunsaturated, omegaunsaturated, or omega-polyunsaturated fatty alcohols, fatty amines, or fatty thiols derived from essential and / or non-essential fatty acids.

[0057] In certain embodiments, the lipid is a fatty alcohol, fatty amine, or fatty thiol derived from an essential and / or non-essential fatty acid having one or more of its carbon units optionally substituted with oxygen, nitrogen, or sulfur.

[0058] In certain embodiments, the lipid is an unsaturated, polyunsaturated, omegaunsaturated, or omega-polyunsaturated fatty alcohol, fatty amine, or fatty thiol derived from essential and / or non-essential fatty acids having one or more of their carbon units substituted with oxygen, nitrogen, or sulfur, which are optionally substituted.

[0059] In certain embodiments, the lipid is hexadecyloxypropyl.

[0060] In certain embodiments, the lipid is 2-aminohexadecyloxypropyl.

[0061] In certain embodiments, the lipid is 2-aminoalacidyl.

[0062] In certain embodiments, the lipid is 2-benzyloxyhexadecyloxypropyl.

[0063] In certain embodiments, the lipid is lauryl, myristyl, palmityl, stearyl, arachidyl, behenyl, or lignoceryl.

[0064] In certain embodiments, the lipid is a sphingolipid of the following formula: [ka] During the ceremony, Sphingolipid R 12 These are hydrogen, alkyl, and C(=O)R 16 , C(=O)OR 16 , or C(=O)NHR 16 And, Sphingolipid R 13 is hydrogen, fluoro, OR 16 ,OC(=O)R 16 , OC(=O)OR 16 , or OC(=O)NHR 16 And, Sphingolipid R 14 This is either a saturated or unsaturated alkyl chain of 6 to 22 carbon atoms optionally substituted with one or more halogens or hydroxyls, or the following formula: [ka] And, An expression where n is between 8 and 14 or between 8 and 14, o is between 9 and 15 or between 9 and 15, and the sum of m and n is between 8 and 14 or between 8 and 14, and the sum of m and o is between 9 and 15 or between 9 and 15, or [ka] And, An expression in which n is 4 to 10 or 4 to 10, o is 5 to 11 or 5 to 11, the sum of m and n is 4 to 10 or 4 to 10, and the sum of m and o is 5 to 11 or 5 to 11, or [ka] And, The expression has the structure that n is between 6 and 12, or n is between 6 and 12, and the sum of m and n is between 6 and 12, or n is between 6 and 12. Sphingolipid R 15 is OR 16 ,OC(=O)R 16 , OC(=O)OR 16 , or OC(=O)NHR 16 And, Sphingolipid R 16 R is hydrogen, cyano, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, or lipid. 16 This is an optional choice of one or more identical or different R 17 Replaced by, Sphingolipid R 17These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyryl, heterocarbocyryl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyrylamino, heterocarbocyrylamino, arylamino, heteroarylamino, heterocyclylamino, cycloalkamino, cycloalkenamino, alkylthio, carbocyrylthio, heterocarbocyrylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl.

[0065] In certain embodiments, sphingolipids R 12 These are H, methyl, ethyl, propyl, n-butyl, isopropyl, 2-butyl, 1-ethylpropyl, 1-propylbutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, benzyl, or phenyl.

[0066] In certain embodiments, the sphingolipid is a sphingolipid of the following formula: [ka] During the ceremony, Sphingolipid R 12 is hydrogen, hydroxyl, fluoro, OR 16 ,OC(=O)R 16 , OC(=O)OR 16 , or OC(=O)NHR 16 And, Sphingolipid R 13 is hydrogen, hydroxyl, fluoro, OR 16 ,OC(=O)R 16 , OC(=O)OR 16 , or OC(=O)NHR 16 And, Sphingolipid R 14 This is either a saturated or unsaturated alkyl chain of 6 to 22 carbon atoms, optionally substituted with one or more halogens, or the following formula: [ka] And, The structure of the expression is such that n is between 8 and 14 or between 8 and 14, and the sum or m and n are between 8 and 14 or between 8 and 14. Sphingolipid R 16 R is hydrogen, cyano, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, or lipid. 16 This is an optional choice of one or more identical or different R 17 Replaced by, Sphingolipid R 17These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyryl, heterocarbocyryl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyrylamino, heterocarbocyrylamino, arylamino, heteroarylamino, heterocyclylamino, cycloalkamino, cycloalkenamino, alkylthio, carbocyrylthio, heterocarbocyrylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, esteryl, formyl, carboxy, carbamoyl, amide, or acrylic.

[0067] In certain embodiments, sphingolipids R 16 These are H, methyl, ethyl, propyl, n-butyl, isopropyl, 2-butyl, 1-ethylpropyl, 1-propylbutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or benzyl.

[0068] Suitable sphingolipids include, but are not limited to, sphingosine, ceramide, or sphingomyelin, or optionally, 2-aminoalkyl groups substituted with one or more substituents.

[0069] Other suitable sphingolipids may be optionally substituted with one or more substituents: 2-aminooctadecane-3,5-diol, (2S,3S,5S)-2-aminooctadecane-3,5-diol, (2S,3R,5S)-2-aminooctadecane-3,5-diol, 2-(methylamino)octadecane-3,5-diol, (2S,3R,5S)-2-(methylamino)octadecane-3,5-diol, 2-(dimethylamino)octadecane-3,5-diol, (2R,3S,5S)-2-(dimethylamino)octadecane-3,5-diol All, 1-(pyrrolidine-2-yl)hexadecane-1,3-diol, (1S,3S)-1-((S)-pyrrolidine-2-yl)hexadecane-1,3-diol, 2-amino-11,11-difluorooctadecane-3,5-diol, (2S,3S,5S)-2-amino-11,11-difluorooctadecane-3,5-diol, 11,11-difluoro-2-(methylamino)octadecane-3,5-diol, (2S,3S,5S)-11,11-difluoro-2-(methylamino)octadecane-3,5-diol, N-((2S,3S (5S)-3,5-dihydroxyoctadecane-2-yl)acetamide, N-((2S,3S,5S)-3,5-dihydroxyoctadecane-2-yl)palmitamide, 1-(1-aminocyclopropyl)hexadecane-1,3-diol, (1S,3R)-1-(1-aminocyclopropyl)hexadecane-1,3-diol, (1S,3S)-1-(1-aminocyclopropyl)hexadecane-1,3-diol, 2-amino-2-methyloctadecane-3,5-diol, (3S,5S)-2-amino-2-methyloctadecane-3,5-diol (3S,5R)-2-amino-2-methyloctadecane-3,5-diol, (3S,5S)-2-methyl-2-(methylamino)octadecane-3,5-diol, 2-amino-5-hydroxy-2-methyloctadecane-3-one, (Z)-2-amino-5-hydroxy-2-methyloctadecane-3-one oxime, (2S,3R,5R)-2-amino-6,6-difluorooctadecane-3,5-diol, (2S,3S,5R)-2-amino-6,6-difluorooctadecane-3,5-diol, (2S,3S,5S)-2-amino-6,Examples include, but are not limited to, 6-difluorooctadecane-3,5-diol, (2S,3R,5S)-2-amino-6,6-difluorooctadecane-3,5-diol, and (2S,3S,5S)-2-amino-18,18,18-trifluorooctadecane-3,5-diol.

[0070] In an exemplary embodiment of formula I, R 1 is hydrogen, [ka] That is the case.

[0071] In an exemplary embodiment of formula I, R ’ These are methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, triduteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl.

[0072] In an exemplary embodiment of formula I, R ” These are methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, triduteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl.

[0073] In an exemplary embodiment of formula I, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0074] In an exemplary embodiment of formula I, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0075] In an exemplary embodiment of formula I, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0076] In an exemplary embodiment of formula I, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0077] In certain embodiments, this disclosure relates to a compound of formula II or a pharmaceutically or physiologically derived salt thereof. [ka] During the ceremony, X is CH2, CHCH3, C(CH3)2, CHF, CF2, or CD2. Y is either N or CR', Z is N or CR'', R' is deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, or carbonyl, and R' is optionally one or more of the same or different R's. 10 Replaced by, R'' is hydrogen, deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, hydroxyl, thiol, or carbonyl, and R' is optionally one or more of the same or different R 10 Replaced by, R 1 , R 2 , R 3 , and R 5 These are H, independently of each other. [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, However, R 1 , R 2 , R 3 , and R 5 However, provided that not all of them are H, R 6R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0078] In exemplary embodiments of Formula II, R' is methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, trijuteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl.

[0079] In exemplary embodiments of Formula II, R'' is methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, triduteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl.

[0080] In an exemplary embodiment of formula II, R 6These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0081] In an exemplary embodiment of formula II, R 7 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0082] In an exemplary embodiment of formula II, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0083] In an exemplary embodiment of formula II, R 9These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0084] In certain embodiments, this disclosure relates to a compound of formula III or a pharmaceutically or physiologically derived salt thereof. [ka] During the ceremony, X is CH2, CHCH3, C(CH3)2, CHF, CF2, or CD2. Z is N or CR'', R'' is deuterium, halogen, hydroxyl, amino, thiol, alkyl, alkenyl, alkynyl, aryl, heteroaryl, carbocykyl, heterocarbocykyl, cycloalkyl, heterocyclyl, hydroxyl, thiol, or carbonyl, and R' is optionally one or more of the same or different R 10 Replaced by, R 1 , R 2 , R 3 , and R 5 These are H, independently of each other. [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, However, R 1 , R 2 , R 3 , and R 5 However, provided that not all of them are H, R 6R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0085] In exemplary embodiments of Formula III, R'' is methyl, fluoro, hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, trijuteromethyl, thiomethyl, carboxylic acid, formyl, vinyl, or ethynyl.

[0086] In an exemplary embodiment of Equation III, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0087] In an exemplary embodiment of Equation III, R 7 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0088] In an exemplary embodiment of Equation III, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0089] In an exemplary embodiment of Equation III, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0090] In certain embodiments, this disclosure relates to compounds of formula IV or their pharmaceutically or physiologically derived salts. [ka] During the ceremony, X is CHCH3, C(CH3)2, CHF, CF2, or CD2. R 1 , R 2 , R 3 , and R 5 These are H, independently of each other. [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, However, R 1 , R 2 , R 3 , and R 5 However, provided that not all of them are H, R 6R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0091] In an exemplary embodiment of formula IV, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0092] In an exemplary embodiment of formula IV, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0093] In an exemplary embodiment of formula IV, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0094] In an exemplary embodiment of formula IV, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0095] In certain embodiments, this disclosure relates to compounds of formula V or their pharmaceutically or physiologically derived salts. [ka] During the ceremony, R 1 , R 2 , R 3 , and R 5 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R2 , R 3 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyklamino, heterocarbocyklamino, arylamino, heteroarylamino, heterocyclamino, cycloalkamino, cycloalkenamino, alkylthio, carbocyklthio, heterocarbocyklthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8, and R 9 They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0096] In an exemplary embodiment of formula V, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0097] In an exemplary embodiment of formula V, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0098] In an exemplary embodiment of formula V, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0099] In an exemplary embodiment of formula V, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0100] In certain embodiments, this disclosure relates to compounds of formula VI or their pharmaceutically or physiologically derived salts. [ka] During the ceremony, R 1 , R 2 , and R 3 These are, independently of each other, as follows: [ka] [ka] Optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted Selected from imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , and R 3This is an optional choice of one or more identical or different R 10 Replaced by, R 6 is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, optionally substituted phenyl, optionally substituted aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicleamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid, R 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0101] In an exemplary embodiment of formula VI, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0102] In an exemplary embodiment of formula VI, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0103] In an exemplary embodiment of formula VI, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0104] In an exemplary embodiment of formula VI, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0105] In certain embodiments, this disclosure relates to compounds of formulas VIa-f or their pharmaceutically or physiologically salted forms. [ka] During the ceremony, R 1 , R 2 , and R 3 These are, independently of each other, as follows: [ka] [ka] Optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted Selected from imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 2 , and R 3This is an optional choice of one or more identical or different R 10 Replaced by, R 6 is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, optionally substituted phenyl, optionally substituted aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicleamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid, R 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0106] In exemplary embodiments of equations VIa~f, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0107] In exemplary embodiments of equations VIa~f, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0108] In exemplary embodiments of equations VIa~f, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0109] In exemplary embodiments of equations VIa~f, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0110] In certain embodiments, this disclosure relates to compounds of formula VII or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 1 , R 2 , and R 5 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R2 , and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyklamino, heterocarbocyklamino, arylamino, heteroarylamino, heterocyclamino, cycloalkamino, cycloalkenamino, alkylthio, carbocyklthio, heterocarbocyklthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R8 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R9 They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0111] In an exemplary embodiment of formula VII, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0112] In an exemplary embodiment of formula VII, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0113] In an exemplary embodiment of formula VII, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0114] In an exemplary embodiment of formula VII, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0115] In certain embodiments, this disclosure relates to compounds of formula VIII or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 1 , R 3 , and R 5 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 , R 3, and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0116] In an exemplary embodiment of formula VIII, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0117] In an exemplary embodiment of formula VIII, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0118] In an exemplary embodiment of formula VIII, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0119] In an exemplary embodiment of formula VIII, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0120] In certain embodiments, this disclosure relates to compounds of formula IX or their pharmaceutically or physiologically derived salts. [ka] During the ceremony, R 2 , R 3 , and R 5 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 2 , R 3, and R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0121] In an exemplary embodiment of formula IX, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0122] In an exemplary embodiment of formula IX, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0123] In an exemplary embodiment of formula IX, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0124] In an exemplary embodiment of formula IX, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0125] In certain embodiments, this disclosure relates to compounds of formula X, [ka] During the ceremony, R1 and R 5 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 and R 5 This is an optional choice of one or more identical or different R10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0126] In an exemplary embodiment of formula X, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0127] In an exemplary embodiment of formula X, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0128] In an exemplary embodiment of formula X, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0129] In an exemplary embodiment of formula X, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0130] In certain embodiments, this disclosure relates to compounds of formula XI or their pharmaceutically or physiologically derived salts. [ka] During the ceremony, R 1 and R 3 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 and R 3This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0131] In an exemplary embodiment of formula XI, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0132] In an exemplary embodiment of formula XI, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0133] In an exemplary embodiment of formula XI, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0134] In an exemplary embodiment of formula XI, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0135] In certain embodiments, this disclosure relates to compounds of formula XII or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 1 and R 2 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 1 and R 2This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclic, heterocarbocyclic, aryl, heteroaryl, heterocyclic, cycloalkyl, cycloalkenyl, alkoxy, carbocycloxy, heterocarbocycloxy, aryloxy, heteroaryloxy, heterocycloxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyclicamino, heterocarbocyclicamino, arylamino, heteroarylamino, heterocyclicamino, cycloalkylamino, cycloalkenylamino, alkylthio, carbocyclicthio, heterocarbocyclicthio, arylthio, heteroarylthio, heterocyclicthio, cycloalkylthio, cycloalkenylthio, arenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R 8 is optionally substituted with one or more of the same or different R 10 and R 9 is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclic, heterocarbocyclic, aryl, heteroaryl, heterocyclic, cycloalkyl, cycloalkenyl, alkoxy, carbocycloxy, heterocarbocycloxy, aryloxy, heteroaryloxy, heterocycloxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyclicamino, heterocarbocyclicamino, arylamino, heteroarylamino, heterocyclicamino, cycloalkylamino, cycloalkenylamino, alkylthio, carbocyclicthio, heterocarbocyclicthio, arylthio, heteroarylthio, heterocyclicthio, cycloalkylthio, cycloalkenylthio, arenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R 9 is optionally substituted with one or more of the same or different R 10 and R 7 R 8 and 9can form a ring with the α-carbon to which they are attached and the amino group attached to the α-carbon, R 8 and R 9 can form a ring with the α-carbon to which they are attached, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclic, heterocarbocyclic, aryl, heteroaryl, heterocyclic, cycloalkyl, cycloalkenyl, alkoxy, carbocycloxy, heterocarbocycloxy, aryloxy, heteroaryloxy, heterocycloxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyclamino, heterocarbocyclamino, arylamino, heteroarylamino, heterocyclamino, cycloalkylamino, cycloalkenamino, alkylthio, carbocyclicthio, heterocarbocyclicthio, arylthio, heteroarylthio, heterocyclicthio, cycloalkylthio, cycloalkenylthio, arenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R 10 is optionally substituted with one or more of the same or different R 11 groups, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0136] In an exemplary embodiment of formula XII, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0137] In an exemplary embodiment of formula XII, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0138] In an exemplary embodiment of formula XII, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0139] In an exemplary embodiment of formula XII, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0140] In certain embodiments, this disclosure relates to compounds of formula XIII or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 2 and R 5 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 2 and R 5This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0141] In an exemplary embodiment of formula XIII, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0142] In an exemplary embodiment of formula XIII, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0143] In an exemplary embodiment of formula XIII, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0144] In an exemplary embodiment of formula XIII, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0145] In certain embodiments, this disclosure relates to compounds of formula XIV or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 2 and R 3 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 2 and R 3This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, heterocarbocyclyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocycloxy, heterocarbocycloxy, aryloxy, heteroaryloxy, heterocycloxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyclamino, heterocarbocyclamino, arylamino, heteroarylamino, heterocyclamino, cycloalkylamino, cycloalkenylamino, alkylthio, carbocyclylthio, heterocarbocyclylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, arenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R 8 is optionally substituted with one or more of the same or different R 10 and R 9 is deuterium, hydroxy, azido, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocyclyl, heterocarbocyclyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocycloxy, heterocarbocycloxy, aryloxy, heteroaryloxy, heterocycloxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocyclamino, heterocarbocyclamino, arylamino, heteroarylamino, heterocyclamino, cycloalkylamino, cycloalkenylamino, alkylthio, carbocyclylthio, heterocarbocyclylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, arenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, and R 9 is optionally substituted with one or more of the same or different R 10 and R 7 R 8 and 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0146] In an exemplary embodiment of formula XIV, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0147] In an exemplary embodiment of formula XIV, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0148] In an exemplary embodiment of formula XIV, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0149] In an exemplary embodiment of formula XIV, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0150] In certain embodiments, this disclosure relates to compounds of formula XV or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 3 and R 5 These are, independently of each other, as follows: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 3 and R 5This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0151] In an exemplary embodiment of formula XV, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0152] In an exemplary embodiment of formula XV, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0153] In an exemplary embodiment of formula XV, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0154] In an exemplary embodiment of formula XV, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0155] In certain embodiments, this disclosure relates to compounds of formula XVI or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 2 The following: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 2 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0156] In an exemplary embodiment of formula XVI, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0157] In an exemplary embodiment of formula XVI, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0158] In an exemplary embodiment of formula XVI, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0159] In an exemplary embodiment of formula XVI, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0160] In certain embodiments, this disclosure relates to compounds of formula XVII or their pharmaceutically or physiological salts. [ka] During the ceremony, R 3 The following: [ka] [ka] Optionally substituted esters, optionally substituted branched esters, optionally substituted carbonates, optionally substituted carbamates, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted Selected from sulfenyl, optionally substituted imidate, optionally substituted hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 3 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 R is hydrogen, alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid. 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 , R 8 , and R 9They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0161] In an exemplary embodiment of formula XVII, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0162] In an exemplary embodiment of formula XVII, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0163] In an exemplary embodiment of formula XVII, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0164] In an exemplary embodiment of formula I, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0165] In certain embodiments, this disclosure relates to compounds of formula XVIII or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 1 The following: [ka] [ka] Optionally substituted branched esters, optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imidate, optional Selected from selectively substituted hydrazonates, selectively substituted oxymyls, selectively substituted imidinyls, selectively substituted imidyls, selectively substituted aminals, selectively substituted hemiaminals, selectively substituted acetals, selectively substituted hemiacetals, selectively substituted carbonimidates, selectively substituted thiocarbonimidates, selectively substituted carbonimidyls, selectively substituted carbamidates, selectively substituted carbamidyls, selectively substituted thioacetals, selectively substituted S-acyl-2-thioethyls, selectively substituted bis-(acyloxybenzyl) esters, selectively substituted (acyloxybenzyl) esters, and BAB esters, R 1 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 These are hydrogen, C1-C7n-alkyl, and C9-C 22n-alkyl, optionally substituted C8n-alkyl, branched alkyl, alkenyl, alkynyl, carbocykyl, heterocarbocykyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, -O(C1~C6n-alkyl), -O(C8~C 21 n-alkyl), optionally substituted -O(C7n-alkyl), -O(branched alkyl)carbocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, -NH(C1~C6n-alkyl), -NH(C8~C 21 n-alkyl), optionally substituted -NH(C7n-alkyl), -NH(branched alkyl)(alkyl)2amino, carbocylicamino, heterocarbocylicamino, arylamino, heteroarylamino, heterocyclicamino, cycloalkamino, cycloalkeneamino, alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipid, R 6 This is an optional choice of one or more identical or different R 10 Replaced by, R 7 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R7 This is an optional choice of one or more identical or different R 10 Replaced by, R 8 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 8 This is an optional choice of one or more identical or different R 10 Replaced by, R 9 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 9 This is an optional choice of one or more identical or different R10 Replaced by, R 7 , R 8 , and R 9 They can form a ring with the α-carbon to which they are bonded, and with the amino group bonded to the α-carbon. R 8 and R 9 They can form rings with the α-carbon to which they bond, R 10 is deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl, R 10 This is an optional choice of one or more identical or different R 11 Replaced by, R 11These are deuterium, hydroxy, azide, thiol, amino, cyano, halogen, alkyl, alkenyl, alkynyl, carbocykrill, heterocarbocykrill, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, carbocyoxy, heterocarbocyoxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, alkylamino, (alkyl)2amino, carbocycleamino, heterocarbocycleamino, arylamino, heteroarylamino, heterocyclicumamino, cycloalkamino, cycloalkenamino, alkylthio, carbocykritolthio, heterocarbocykritolthio, arylthio, heteroarylthio, heterocyclicritolthio, cycloalkylthio, cycloalkenylthio, allenyl, sulfinyl, sulfamoyl, sulfonyl, lipid, nitro, or carbonyl. Lipids are C 11 ~C 22 High-grade alkyl, C 11 ~C 22 These are higher alkoxys, polyethylene glycols, or alkyl-substituted aryls, or lipids as described herein.

[0166] In an exemplary embodiment of formula XVIII, R 6 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0167] In an exemplary embodiment of formula XVIII, R 7These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0168] In an exemplary embodiment of formula XVIII, R 8 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0169] In an exemplary embodiment of formula XVIII, R 9 These are methyl, ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, pentyl, s-pentyl, t-pentyl, neopentyl, 3-pentyl, hexyl, t-hexyl, 4-septyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl 2,6-dimethylphenyl, isopropoxide, tert-butoxide, N-propylamino, N-isopropylamino, N-tert-butylamino, N,N-dimethylamino, N,N-diethylamino, or N,N-dipropylamino.

[0170] In certain embodiments, this disclosure relates to compounds of formula XIX or their pharmaceutically or physiologically active salts. [ka] During the ceremony, R 5 The following: [ka] [ka] Optionally substituted thioesters, optionally substituted branched thioesters, optionally substituted thiocarbonates, optionally substituted S-thiocarbonates, optionally substituted dithiocarbonates, optionally substituted thiocarbamates, optionally substituted oxymethoxycarbonyl, optionally substituted oxymethoxythiocarbonyl, optionally substituted oxymethylcarbonyl, optionally substituted oxymethylthiocarbonyl, L-amino acid esters, D-amino acid esters, N-substituted L-amino acid esters, N,N-disubstituted L-amino acid esters, N-substituted D-amino acid esters, N,N-disubstituted D-amino acid esters, optionally substituted sulfenyl, optionally substituted imidate, optionally substituted Selected from hydrazonate, optionally substituted oxymyl, optionally substituted imidinyl, optionally substituted imidyl, optionally substituted aminal, optionally substituted hemiaminal, optionally substituted acetal, optionally substituted hemiacetal, optionally substituted carbonimidate, optionally substituted thiocarbonimidate, optionally substituted carbonimidyl, optionally substituted carbamidate, optionally substituted carbamidyl, optionally substituted thioacetal, optionally substituted S-acyl-2-thioethyl, optionally substituted bis-(acyloxybenzyl) ester, optionally substituted (acyloxybenzyl) ester, and BAB ester, R 5 This is an optional choice of one or more identical or different R 10 Replaced by, R 6 These are hydrogen, C2-C7n-alkyl, optionally substituted C8n-alkyl, C9-C22 n-alkyl, alkenyl, alkynyl, carbocyrill, heterocarbocyrill, aryl, heteroaryl, heterocyclyl, C3-C9 cycloalkyl, C 11 ~C 22 Cycloalkyl, optionally substituted C 10 Cycloalkyl, cycloalkenyl, -O(C1~C6n-alkyl), -O(optionally substituted C7n-alkyl), -O(C8~C 21 n-alkyl), -O (branched alkyl), carbocyclooxy, heterocarbocyclooxy, aryloxy, heteroaryloxy, heterocyclooxy, cycloalkoxy, cycloalkenoxy, -N(C2~C 21 n-alkyl)2, -N(optionally substituted C1 alkyl)2, -NH(optionally substituted C1 alkyl), -NH(C2~C6n-alkyl), -NH(optionally substituted C7n-alkyl), -NH(C8~C 15 n-alkyl), -NH (optionally substituted C 16 n-alkyl), -NH(C 17 n-alkyl), -NH (optionally substituted C 18 n-alkyl), -NH(C 19 ~C 21 n-alkyl), -NH(branched alkyl), -N(branched alkyl)2, carbocyamino, heterocarbocyamino, optionally substituted arylamino, heteroarylamino, heterocyclamino, cycloalkamino, cycloalkenamino, alkylthio, carbocycrylthio, heterocarbocycrylthio, arylthio, heteroarylthio, heterocyclylthio, cycloalkylthio, cycloalkenylthio, allenyl, cyano, or lipids, R 6 This is an optional choice of one or more identical or different R 10 ...

Claims

[Claim 1] The invention described herein.

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