135 results about "Azabicyclane" patented technology

The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I):wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

A method of stereoselectively making an aminocyclohexyl ether comprises, for example, reacting to form the aminocyclohexyl ether having the formula respectively, wherein independently at each occurrence, R1 and R2 are independently hydrogen, C1-C8alkyl, C3-C8alkoxyalkyl, C1-C8hydroxyalkyl, or C7-C12aralkyl; or R1 and R2 are independently C3-C8alkoxyalkyl, C1-C8hydroxyalkyl, and C7-C12aralkyl; or R1 and R2, when taken together with the nitrogen atom to which they are directly attached in formula (57) or (75), form a ring denoted by formula (I): wherein the ring of formula (I) is formed from the nitrogen as shown as well as three to nine additional ring atoms independently carbon, nitrogen, oxygen, or sulfur; where any two adjacent ring atoms may be joined together by single or double bonds, and where any one or more of the additional carbon ring atoms may be substituted with one or two substituents selected from the group consisting of hydrogen, hydroxy, C1-C3hydroxyalkyl, oxo, C2-C4acyl, C1-C3alkyl, C2-C4alkylcarboxy, C1-C3alkoxy, and C1-C20alkanoyloxy, or may be substituted to form a spiro five- or six-membered heterocyclic ring containing one or two oxygen and / or sulfur heteroatoms; or any two adjacent additional carbon ring atoms may be fused to a C3-C8carbocyclic ring, and any one or more of the additional nitrogen ring atoms may be substituted with substituents selected from the group consisting of hydrogen, C1-C6alkyl, C2-C4acyl, C2-C4hydroxyalkyl and C3-C8alkoxyalkyl; or R1 and R2, when taken together with the nitrogen atom to which they are directly attached in formula (I), may form a bicyclic ring system selected from the group consisting of 3-azabicyclo[3.2.2]nonan-3-yl, 2-azabicyclo[2.2.2]octan-2-yl, 3-azabicyclo[3.1.0]hexan-3-yl, and 3-azabicyclo[3.2.0]heptan-3-yl; and wherein R3, R4 and R5 are independently bromine, chlorine, fluorine, carboxy, hydrogen, hydroxy, hydroxymethyl, methanesulfonamido, nitro, cyano, sulfamyl, trifluoromethyl, C2-C7alkanoyloxy, C1-C6alkyl, C1-C6alkoxy, C2-C7alkoxycarbonyl, C1-C6thioalkyl, aryl or N(R6,R7) where R6 and R7 are independently hydrogen, acetyl, methanesulfonyl or C1-C6alkyl; or R3, R4 and R5 are independently hydrogen, hydroxy or C1-C6alkoxy; with the proviso that R3, R4 and R5 cannot all be hydrogen; and wherein O-J is a leaving group. Methods of making intermediates are also disclosed.

Compounds of formula I,wherein R1, R2, R3 and Ra Rh are as defined in the specification. The compounds are useful in the prophylaxis and in the treatment of arrhythmias, in particular a trial and ventricular arrhythmias.

Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

The present invention relates also to a process for the preparation of intermediate compounds useful in preparing the compounds of Formula (I) using the process of Scheme (II).