Patent classifications
C07D207/40
Conjugates of cell binding molecules with cytotoxic agents
A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a Formula (I), wherein T, L, m, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.1, R.sup.12, and R.sup.13 are defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.
Hydantoin containing deoxyuridine triphosphatase inhibitors
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
Hydantoin containing deoxyuridine triphosphatase inhibitors
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##
Linker, Antibody-Drug Conjugate Including Same and Use Thereof
Provided are a linker represented by Formula I or I′, an antibody-drug conjugate containing the same, and use of thereof, a pharmaceutical composition comprising the antibody-drug conjugate, and use of the antibody-drug conjugate for treating and/or preventing a disease.
##STR00001##
Linker, Antibody-Drug Conjugate Including Same and Use Thereof
Provided are a linker represented by Formula I or I′, an antibody-drug conjugate containing the same, and use of thereof, a pharmaceutical composition comprising the antibody-drug conjugate, and use of the antibody-drug conjugate for treating and/or preventing a disease.
##STR00001##
Prodrugs of Fumarates and Their Use in Treating Various Diseases
The present invention provides compounds of formula (I),
##STR00001##
wherein: R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10 aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
Prodrugs of Fumarates and Their Use in Treating Various Diseases
The present invention provides compounds of formula (I),
##STR00001##
wherein: R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10 aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
Reduction-triggered antibacterial sideromycins
A compound is provided, comprising: an Fe(III)-binding or an Fe(III)-bound siderophore; one or more optional linker covalently bound to the siderophore; a drug; and an Fe(III) to Fe(II) reduction triggered linker bound to the drug and the linker or, if no linker is present, then bound to the drug and the siderophore. Compositions and methods including the compound are also provided.