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Preparation of S-(-)- and R-(+)-N-(quinuclidinyl-3)-amide

Optical active forms of the carboxylic acid amines of 3-aminoquinuclidine of formula (I), and the preparation thereof. These can be hydrolysed to the optical active forms of 3-aminoquinuclidine.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H112N | ChemSpider

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Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats

The purpose of our studies was to determine the effects of muscarinic receptor agonists on conditioned avoidance responding in the rat. Rats were trained to avoid or escape an electric shock delivered to the feet in a discrete trial procedure. The muscarinic receptor agonists pilocarpine and [2-ethyl-8-methyl-2,8-diazaspiro(4.5)decane-1,3-dione] hydrochloride (RS86) and the cholinesterase inhibitor physostigmine all decreased the percentage of avoidance responses at doses that produced less than approximately 30% response failures. Similar results were obtained with the antipsychotic drugs haloperidol, trifluoperazine, chlorpromazine, and clozapine. However, the benzodiazepine anxiolytic diazepam did not decrease avoidance responding up to doses that produced ataxia. On the other hand, oxotremorine and arecoline decreased avoidance responding only by producing response failures, whereas aceclidine produced intermediate changes. The muscarinic receptor antagonists scopolamine, trihexyphenidyl, and benztropine were without effect when administered alone but antagonized the decreases in avoidance responding produced by pilocarpine and RS86. Scopolamine had little effect on the decreases in avoidance responding produced by haloperidol. The newer muscarinic receptor partial agonists or agonist/antagonists [R-(Z)-(+)-alpha- (methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitrile] hydrochloride, talsaclidine, milameline, and xanomeline also produced dose-related decreases in avoidance responding. Our results demonstrate that muscarinic receptor agonists can decrease avoidance responding in a manner similar to dopamine- receptor antipsychotic drugs, suggesting that muscarinic receptor agonists may provide an alternative approach to the treatment of psychosis.

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Quinuclidine | C7H81N | ChemSpider

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5-HT3 RECEPTOR MODULATORS, METHODS OF MAKING, AND USE THEREOF

Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H100N | ChemSpider

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CRYSTALLINE FUMARATE SALTS OF 1-AZABICYCLO[2.2.2]OCT SUBSTITUTED FURO[2,3-C]PYRIDINYL CARBOXAMIDE AND COMPOSITIONS AND PREPARATIONS THEREOF

The invention provides fumarate salts of N-[1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, compositions, racemic mixtures, or pure enantiomers thereof, and preparation thereof. The fumarate salts are useful to treat diseases or conditions in which alpha7 nAChR is known to be involved. Formula (I).

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Quinuclidine – Wikipedia,
Quinuclidine | C7H113N | ChemSpider

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Visible-Light-Mediated Metal-Free Difunctionalization of Alkenes with CO2 and Silanes or C(sp3)?H Alkanes

Catalytic alkene difunctionalization via Si?H and C?H activations represents an ideal atom- and step-economic pathway for quick assembly of molecular complexity. We herein developed a visible-light-promoted metal-free difunctionalization of alkenes using abundant CO2 and readily available Si?H and C(sp3)?H bonds as feedstocks. Through the merger of photoredox and hydrogen-atom-transfer catalysis, a variety of value-added compounds, such as beta-silacarboxylic acids and acids bearing a gamma-heteroatom (e.g., N, O, S) could be directly accessed from simple alkenes in a redox-neutral fashion.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H63N | ChemSpider

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PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N-(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4′ are each independently H or alkyl; or R4 and R4′ together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like

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Quinuclidine – Wikipedia,
Quinuclidine | C7H108N | ChemSpider

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Improved preparation of (R) and (S)-3-aminoquinuclidine dihydrochloride

An improved procedure for the synthesis of either (R) or (S)-3-aminoquinuclidine was developed. Key intermediate imine 2 was made in a one pot process using lithium oxide as the base and molecular sieves.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H146N | ChemSpider

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IMMUNOMODULATING OXOPYRRAZOLOCINNOLINES AS CD 80 INHIBITORS

N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-4-(6,9-difluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-benzamide is a CD80 antagonist, useful in the treatment of dieases which benefit from immuno-inhibition.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H109N | ChemSpider

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Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists

Human alpha7 nicotinic acetylcholine receptor (nAChR) is a promising therapeutic target for the treatment of schizophrenia accompanied with cognitive impairment. Herein, we report the synthesis and agonistic activities of a series of indolizine derivatives targeting to alpha7 nAChR. The results show that all synthesized compounds have affinity to alpha7 nAChR and some give strong agonistic activity, particularly most active agonists show higher potency than control EVP-6124. The docking and structure-activity relationship studies provide insights to develop more potent novel alpha7 nAChR agonists.

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Quinuclidine | C7H159N | ChemSpider

The important role of Quinuclidin-4-ylmethanamine

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CEPHALOSPORIN HAVING CATECHOL GROUP

The present invention provides Cephem compounds which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria as follows: A compound of the formula: wherein, X is N, CH or C-Cl; T is S or the like; A and G are lower alkylene or the like; B is a single bond or the like; D is a single bond, -NR7-, -CO-, -CO-NR7-, -NR7-CO-, -NR7-CO-NR7-, or the like; E is optionally substituted lower alkylene; F is a single bond or optionally substituted phenylene; R3, R4, R5 and R6 each is independently hydrogen, halogene, nitrile, or the like; or an ester, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H22N | ChemSpider