51627-76-0Relevant academic research and scientific papers
Synthesis and in vitro muscarinic activities of a series of 3-(pyrazol- 3-yl)-1-azabicyclo[2.2.2]octanes
Plate, Ralf,Plaum, Marc J. M.,Hulst, Rob G. A. V. D.,De Boer, Thijs
, p. 449 - 454 (2000)
A series of 3-(pyrazol-3-yl)-1-azabicyclo[2.2.2]octane derivatives C (Fig. 1) was synthesized and tested for muscarinic activity in receptor binding assays using [3H]-oxotremorine-M (OXO-M) and [3H]-pirenzepine (PZ) as ligands. Potential muscarinic agonistic or antagonistic properties of the compounds were determined using binding studies measuring their potencies to inhibit the binding of OXO-M and PZ. Preferential inhibition of OXO-M binding was used as an indicator for potential muscarinic agonistic properties; this potential was confirmed in functional studies on isolated organs. (C) 2000 Elsevier Science Ltd.
COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE
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Paragraph 00156, (2013/04/10)
The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
N-biarylamides
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, (2008/06/13)
The invention relates to N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improvement in cognition, concentration power, learning power and/or memory.
NICOTINIC ALPHA-7 RECEPTOR LIGANDS AND PREPARATION AND USES THEREOF
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Page/Page column 46-47, (2008/06/13)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
N-BIARYLAMIDES
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Page/Page column 18, (2008/06/13)
The invention relates to N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improvement in cognition, concentration power, learning power and/or memory.
INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USES THEREOF
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Page/Page column 109-110, (2010/02/14)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
5-HT3 receptor agonist, novel thiazole derivative and intermediate thereof
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, (2008/06/13)
A 5-HT3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): STR1 wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms; one of L1 or L2 represents a single bond and the other is non-existent or represents an alkylene or alkenylene group; R represents: STR2
Oxadiazoles useful in the treatment of senile dementia
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, (2008/06/13)
A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low lipophilicity; are potent muscarinic agonists, and have good CNS penetrability. The compounds are therefore useful in the treatment of neurological and mental illnesses.
Heterocyclic compounds
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, (2008/06/13)
Biphenylylquinuclidine derivatives of formula I, Q--Ar1 --Ar2, in which Q is of formula Ia or Ib, STR1 in which R1 and R2 are independently selected from hydrogen, alkyl, halogeno and hydroxy; or R1 and R2 when taken together define an oxo group; Xb is selected from --CH2 --, =CH-- and --CH(OH); Xa is selected from --CH2 --, =CH--, CO, --O--, and --S(O)n (wherein n=0, 1 or 2); Ar1 is a phenylene moiety; Ar2 is phenyl; and wherein one or both of Ar1 and Ar2 is optionally unsubstituted or substituted by one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-carbamoyl, N,N-di-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, alkanoyl and alkanoylamino; and their pharamaceutically acceptable salts are inhibitors of squalene synthase and hence useful in treating diseases and medical conditions in which a lowering of cholesterol is desirable. The use of these derivatives in medicine is disclosed tohether with novel compounds, processes for their preparation and pharmaceutical composition containing them.
AZABICYLO OXIME COMPOUNDS
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, (2008/06/13)
A compound of formula (I) or a pharmaceutically acceptable salt thereof: STR1 wherein R 1 represents STR2 in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1; R 2 is a group OR 4, where R 4 is C 1-4 alkyl, C. sub.2-4 alkenyl, C 2-4 alkynyl, a group OCOR 5 where R 5 is hydrogen or R 4, or a group NHR 6 or NR 7 R 8 where R 6, R 7 and R 8 are independently C 1-2 alkyl; and R 3 is chloro, fluoro, bromo, cyclopropyl, C 1-3 alkyl substituted by one, two or three halogen atoms, or R 3 is a group (CH. sub.2) n R 9 where R 9 is--CN,--OH,--OCH 3,--SH,--SCH 3,--C CH or--CH=CH 2 and n is O or 1, with the proviso that when n is 0, R 9 is not--OH or--SH.
