摘要:
The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.
摘要:
The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful for inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.
摘要:
The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.
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 (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 (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:
The invention provides compounds having the structure of formula I, and prodrugs, stereoisomers, racemates, salts, hydrates, solvates, acid salt hydrates and isomorphic crystalline forms thereof, wherein A, Y and the groups R1, R2, R3 and R4 are defined in the specification. These compounds can be administered in pharmaceutical formulations to modulate cannabinoid receptor activity for the prevention and treatment of a variety of diseases and conditions, including pain, inflammation and pruritis.
摘要:
This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
摘要:
An arbiter arbitrates between PCI agents within an ASIC. The ASIC interfaces with an external PCI bus. In operation, the arbiter receives request signals from the PCI agents, and in response thereto, generates a single external request signal. Once the grant is received by the ASIC, the arbiter will route it to a selected PCI agent. The selected agent then gains access to the PCI bus and all other agents are locked out until the transaction is completed. The arbiter is implemented in such a way that there is a minium delay between the generation of the request by any agent and the request sent out by the ASIC. This is performed by ORing all requests.