167710-67-0Relevant articles and documents
Preparation method of piperidine spiro derivative
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Paragraph 0032-0034, (2020/05/08)
The invention discloses a preparation method of a piperidine spiro derivative, and belongs to the field of synthesis of medical intermediates. The method comprises the following steps: 1, enabling N-benzyl substituted cyclic ketone 1 to react with bromo-c
MUSCARINIC RECEPTOR AGONISTS
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Page/Page column 45; 46, (2015/12/09)
This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2 R3 and R4 are as defined herein.
Structure activity relationships of new inhibitors of mammalian 2,3-oxidosqualene cyclase designed from isoquinoline derivatives
Binet, Jean,Thomas, Didier,Benmbarek, Abdellah,De Fornel, Daniel,Renaut, Patrice
, p. 316 - 329 (2007/10/03)
We have designed more potent inhibitors from the previously reported LF 05-0038, a 6-isoquinolinol based inhibitor of 2,3-oxidosqualene cyclase (IC 50: 1.1 μM). Replacement of the 3-OH group by various 3-substituted amino groups, and modification of the alkyl chain borne by the endocyclic nitrogen led to inhibitors with IC50 in the range of 0.15 to 1 μM. In a second step, opening of the bicyclic ring system afforded the corresponding aminoalkylpiperidines which were slightly more potent. Finally, introduction of suitable aromatic containing moieties on the piperidine nitrogen yielded very potent inhibitors such as 20x (IC50=18 nM) easy to synthesize and achiral. The recent availability of the crystal structure of squalene-hopene cyclase allowed us to construct a three-dimensional (3D) model of the related 2,3-oxidosqualene cyclase (OSC) which was tentatively used to describe the possible mode of binding of our compounds and which can be useful for designing new inhibitors.