摘要:
Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5—, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要:
Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5 —, (f) —L4—N(R5)—C(W)—L7—L5 —, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要:
Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (a) (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, and —P(W)RR3RR3′; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5 —, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene (k) a covalent bond, (l) and (m) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要翻译:具有式的化合物或其药学上可接受的盐,其中R 1是(a)氢,(b)低级烷基,(c)烯基,(d)烷氧基,(e)硫代烷氧基,(f)卤素,(g)卤代烷基,(h) 芳基-L2-和(i)杂环-L2-; R 2选自(a)(b)-C(O)NH-CH(R 14)-C(O)OR 15,(d)-C(O)NH-CH(R 14)-C(O)NHSO 2 R 16 e)-C(O)NH-CH(R14) - 四唑基,(f)-C(O)NH-杂环基和(g)-C(O)NH-CH(R14)-C(O)NR17R18; R 3是取代或未取代的杂环或芳基,取代或未取代的环烷基或环烯基,和-P(W)RR 3 R R 3'; R4是氢,低级烷基,卤代烷基,卤素,芳基,芳基烷基,杂环或(杂环)烷基; (a)-L4-N(R5)-L5-,(b)-L4-O-L5-,(c)-L4-S(O)n-L5-(d) - L4-L6-C(W)-N(R5)-L5-,(e)-L4-L6-S(O)mN(R5)-L5 - ,(f)-L4-N(R5)-C W)-L7-L5-,(g)-L4-N(R5)-S(O)p-L7-L5-,(h)任选取代的亚烷基,(i)任选取代的亚烯基,(j)任选取代的亚炔基 (k)共价键,(1)和(m)是蛋白质异戊二烯基转移酶的抑制剂。 还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。
摘要:
Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (a) (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, and —P(W)RR3RR3′; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5—(d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5—, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene (k) a covalent bond, (l) and (m) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要翻译:具有式的化合物或其药学上可接受的盐,其中R 1是(a)氢,(b)低级烷基,(c)烯基,(d)烷氧基,(e)硫代烷氧基,(f)卤素,(g)卤代烷基,(h) 芳基-L2-和(i)杂环-L2-; R 2选自(a)(b)-C(O)NH-CH(R 14)-C(O)OR 15,(d)-C(O)NH-CH(R 14)-C(O)NHSO 2 R 16 e)-C(O)NH-CH(R14) - 四唑基,(f)-C(O)NH-杂环基和(g)-C(O)NH-CH(R14)-C(O)NR17R18; R 3是取代或未取代的杂环或芳基,取代或未取代的环烷基或环烯基,和-P(W)RR 3 R R 3'; R4是氢,低级烷基,卤代烷基,卤素,芳基,芳基烷基,杂环或(杂环)烷基; (a)-L4-N(R5)-L5-,(b)-L4-O-L5-,(c)-L4-S(O)n-L5-(d) - L4-L6-C(W)-N(R5)-L5-,(e)-L4-L6-S(O)mN(R5)-L5-,(f)-L4-N(R5)-C W)-L7-L5-,(g)-L4-N(R5)-S(O)p-L7-L5-,(h)任选取代的亚烷基,(i)任选取代的亚烯基,(j)任选取代的亚炔基 (k)共价键,(1)和(m)是蛋白质异戊二烯基转移酶的抑制剂。 还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。
摘要:
Compounds having formula (I) inhibit cellular proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
摘要:
Compounds having formula (I) inhibit cellular proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
摘要:
Triphenyl compounds of the formulae I, II, and VI: methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are compounds are interleukin-4 antagonists; and are useful for the treatment of asthma and allergies.
摘要:
Compounds having Formula I are useful for treating cancer. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of treating cancer in a mammal.
摘要:
In an alkanolamine gas treating process for removing acid gas from a feedstream in which hydrogen sulfide is present, reduced corrosion of steel parts or components is observed when solution concentrations of hydrogen sulfide and vanadium in the plus five valence state are maintained above certain minimum levels.
摘要:
Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.