916736-76-0Relevant articles and documents
The discovery of BMS-457, a potent and selective CCR1 antagonist
Gardner, Daniel S.,Santella III, Joseph B.,Duncia, John V.,Carter, Percy H.,Dhar, T.G.Murali,Wu, Hong,Guo, Weiwei,Cavallaro, Cullen,Van Kirk, Katy,Yarde, Melissa,Briceno, Stephanie W.,Robert Grafstrom,Liu, Richard,Patel, Sima R.,Tebben, Andrew J.,Camac, Dan,Khan, Javed,Watson, Andrew,Yang, Guchen,Rose, Anne,Foster, William R.,Cvijic, Mary Ellen,Davies, Paul,Hynes Jr., John
, p. 3833 - 3840 (2013/07/25)
A series of compounds which exhibited good human CCR1 binding and functional potency was modified resulting in the discovery of a novel series of high affinity, functionally potent antagonists of the CCR1 receptor. Issues of PXR activity, ion-channel pote
Bradykinin B1 receptor antagonists: An α-hydroxy amide with an improved metabolism profile
Kuduk, Scott D.,Chang, Ronald K.,DiPardo, Robert M.,Di Marco, Christina N.,Murphy, Kathy L.,Ransom, Richard W.,Reiss, Duane R.,Tang, Cuyue,Prueksaritanont, Thomayant,Pettibone, Douglas J.,Bock, Mark G.
scheme or table, p. 5107 - 5110 (2009/05/26)
A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.
l-HYDROXYCYCLOALKANECARBOXAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS
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, (2008/06/13)
α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; Rl, R2 and R3 are each independently selected from H, halogen and OH; or Rl and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or F; R6 is selected from -CO2-C1-4alkyl, -O-C1-4alkyl, -O- C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl l,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-l,2,4-oxadiazol-3-yl, 3-halomethyl- l,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-l,2,3-triazolyl, and 5-methyl-l ,2,3-triazolyl; R7 and R8 are each independently Cl or F; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
