- AMIDOPYRAZOLE DERIVATIVE
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A platelet coagulation inhibitor which inhibits neither COX-1 nor COX-2 is provided. The inhibitor is a compound represented by general formula (I): wherein Ar1 and Ar2 independently represent a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents, or a phenyl group optionally substituted with 1 to 3 substituents; R1 represents a lower acyl group, carboxyl group, a lower alkoxycarbonyl group, a lower alkoxy group, a lower alkyl group optionally substituted with 1 or 2 substituents, a carbamoyl group optionally substituted with 1 or 2 substituents, an oxamoyl group optionally substituted with 1 or 2 substituents, an amino group optionally substituted with 1 or 2 substituents, a 4- to 7-membered alicyclic heterocyclic group optionally substituted with 1 or 2 substituents, a phenyl group optionally substituted with 1 to 3 substituents, or a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents; and R2 represents hydrogen atom, a halogeno group, or the like.
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Page/Page column 24
(2010/11/23)
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- 5-HT1F agonists
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The present invention relates to substituted furo[3,2-b]pyridine compounds of formula I: or a pharmaceutical acid addition salt thereof; where; R is E—D is C═CH or CH—CH2; R1is hydrogen or C1-C4alkyl; R2is hydrogen, halo, hydroxy, —NR3R4, —SR3, —C(O)R3, —C(O)MR3R4, —NR3SO2R5, —NHC(Q)NR3R4, —NHC(O)OR3, or —NR3C(O)R5; R3, R4, and R5are independently hydrogen, C1-C4alkyl, C2-C6alkenyl, C2-C6alkynyl, or —(CH2)naryl; or R3and R4combine, together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, piperazine, 4-substituted piperazine, morpholine, or thiomorpholine ring; n is 0, 1, 2, 3, 4, 5, or 6; and Q is O or S. The present invention further relates to pharmaceutical. formulations containing compounds formula I and to the use of compounds of formula I for activating 5-HT1Freceptors, inhibiting neuronal protein extravasation, and treating and/or preventing migraine in a mammal.
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Page column 19
(2008/06/13)
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- TRIAZOLO-PYRIDINES AS ANTI-INFLAMMATORY COMPOUNDS
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The present invention relates to novel triazolo-pyridines of the formula (I) wherein X is >CH2, >NH, sulfur, >S=O, >S02 or oxygen; wherein said >CH2 and >NH may optionally be substituted with a suitable substituent; R1 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; R2 is selected from the group consisting of hydrogen, (Cl-C6)alkyl and other suitable 10 substituents; s is an integer from 0-4; R3 is R4, R5-(NR6)-, R5-S-, R5-(S=O)-, R5-(S02)-, R5-S02-NR6-, R5-(NR6)-S02-, R5-O-,R5-(C=O)-, R5-(NR6)-(C=O)-, R5-(C=O)-NR6-, R5-O-(C=O)-, R5-(C=O)-O-, R5-CR7=CR8- or R5-C=-C-; such that the molecular weight of R3 is less than 500 AMU, preferably less than 250 15 AMU; R4, R5 and R6 are each selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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- A general method for the preparation of 2,3,5-trisubstituted-furo[3,2-b]pyridines
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The preparation of 2,3,5-trisubstituted-furo[3,2-b]pyridines via a Pd(0)-catalyzed intramolecular cyclization of methyl 4-(6-chloro-2-iodopyridin-3-yloxy)-substituted-butenoates 9a-f is described. This approach was both efficient and general, and provided the highly functionalized heterocyclic ring system in high yield. Among the several examples provided is the preparation of 3-[2-(N,N-dimethylamino)ethyl]-5-(4-fluorobenzoyl)amino-2-methylfuro[3,2-b] pyridine 4, a selective 5-HT1F receptor agonist.
- Mathes, Brian M.,Filla, Sandra A.
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p. 725 - 728
(2007/10/03)
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- Heterocyclic compounds useful as pharmaceutical agents
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Compounds of formula (I) in which all variables are defined in the description and their salts inhibit the enzyme oxido squalene cyclase and are useful in treating hypercholesterolemia and also as anti-fungal agents. Processes for their preparation are also described together with their use in medicine.
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- Efficient asymmetric synthesis of ABT-594; a potent, orally effective analgesic
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A concise asymmetric synthesis of (R)-2-chloro-5-(2- azetidinylmethoxy)pyridine (ABT-594) is presented in which the key intermediate t-butoxycarbonyl protected (2R)-azetidinylalcohol is obtained in three steps from the dibenzyl ester of D-aspartic acid in 44% yield and >99% ee.
- Lynch, John K.,Holladay, Mark W.,Ryther, Keith B.,Bai, Hao,Hsiao, Chi-Nung,Morton, Howard E.,Dickman, Daniel A.,Arnold, William,King, Steven A.
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p. 2791 - 2794
(2007/10/03)
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