Abstract:
PROBLEM TO BE SOLVED: To provide a series of N-substituted diazabicyclic compound, a method for selectively controlling releasing of a synaptic transmission substance in mammals by using the compound, and a pharmaceutical composition including the compound.SOLUTION: The present invention provides a compound expressed by formula (I), a pharmaceutical composition of the compound, and use of the composition to control synaptic transmission in mammals (in a nicotinic acetylcholine receptor ligand). In formula (I), A is selected from a group consisting of CH2, CH2CH2, and the like; B is selected from a group consisting of CH2 and CH2CH2, however, when A is CH2CH2CH2, B is CH2; Y is selected from a group consisting of CH2 and CH2CH2; Z is selected from a group consisting of CH2 and CH2CH2, however, when Y is CH2CH2, Z is a covalent bond, and when Z is CH2CH2, Y is a covalent bond; and Rl is pyridine or the like.
Abstract:
Compounds of formula (I), pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals (nicotinic acetylcholine receptor ligands).
Abstract:
A series of 3-pyrrolidinyloxy-3'-pyridyl ether compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions including these compounds. Preferred compounds are 3-pyrrolidinylmethoxy-3'-(5'-and/or 6'-substituted) pyridyl ethers.
Abstract:
COMPOUNDS OF FORMULA I PHARMACEUTICAL COMPOSITIONS OF THESE COMPOUNDS, AND USE OF SAID COMPOSITIONS TO CONTROL SYNAPTIC TRANSMISSION IN MAMMALS.
Abstract:
The pyridazinon compounds are selective inhibitors of cyclooxygenase (COX), in particular of cyclooxygenase-2 (COX/2), COX-2 - inducible isoform which is related to the respective inflammation, as opposite to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important enzyme in many tissues, including the gastrointestinal tract and in the kidneys. The selectivity of the COX-2 compounds reduces to a minimum the unwanted side effects in the gastrointestinal tract and in the kidneys observed in the so-far knowm nonsteroid antiphlogistic medicaments.
Abstract:
The present invention describes pyridazinone compounds of formula (I) which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important "housekeeping" enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectively of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
Abstract:
Compounds of formula (I) Z-Ar 1 -Ar 2 wherein Z is a diazabicyclic amine, Ar 1 is a 5- or 6-membered aromatic ring, and Ar 2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4- (methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by .alpha.7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I ) and methods for using such compounds and compositions.
Abstract:
In the present invention, there are described pyridazinone compounds, which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1), which is an important "housekeeping" enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).