摘要:
The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
摘要:
The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
摘要:
The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.
摘要:
This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要:
This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要:
Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-decahydronaphthalene esters and have the structure ##STR1## wherein Z is ##STR2## wherein R is alkali metal such as Na, or H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, a method for preparing the above-mevinic acid derivatives is also provided.
摘要:
Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.n,(x) phenyl-S(O).sub.n,(xi) substituted phenyl-S(O).sub.n in which one or more substituents are X and Y, and(xii) oxo,(c) alkyl-S(O).sub.n,(d) cycloalkyl-S(O).sub.n,(e) phenyl-S(O).sub.n,(f) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y,(g) halogen,(h) hydroxy,(i) alkoxy,(j) alkoxycarbonyl,(k) acyloxy,(l) phenyl, and(m) substituted phenyl in which one or more substituents are X and Y,(7) phenyl,(8) substituted phenyl in which one or more substituents are X or Y,(9) amino,(10) alkylamino,(11) dialkylamino,(12) phenylamino,(13) substituted phenylamino in which one or more substituents are X or Y,(14) alkyl(substituted phenyl)amino in which one or more substituents are X and Y,(15) phenylalkylamino,(16) di(phenylalkyl)amino,(17) substituted phenylalkylamino in which one or more substituents are X or Y,(18) a member selected from(a) piperidinyl,(b) pyrrolidinyl,(c) piperazinyl,(d) morpholinyl,(e) thiomorpholino,(f) histaminyl,(g) 3-aminomethyl pyridinyl, and(19) hydroxy substituted alkylamino;X and Y are independently hydrogen, halogen, trifluoromethyl, alkyl, nitro, alkoxy, or cyano;n is 0, 1, or 2;R.sup.4 is ##STR2## M+ is hydrogen, ammonium, or an alkali metal.