cas 846057-27-0, 1-(4-HydroxyMethyl-piperidin-1-yl)-ethanone

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PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to pyrazolopyrimidine derivatives having dual pharmacological activity towards both the α2δ subunit of the voltage-gated calcium channel and the sigma-1 (σ1) receptor, to processes of preparation of such compounds,
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Page/Page column 213; 215

(2021/12/08)

HETEROCYCLIC COMPOUND INTERMEDIATE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Disclosed by the invention is a heterocyclic compound, an intermediate, and a preparation method therefor and an application thereof. Provided by the invention are a heterocyclic compound as shown in formula I, and a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The heterocyclic compound hasa high P2X3 antagonistic activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.
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Paragraph 0522; 0525-0526

(2021/10/07)

N-ACYL-{4-[(4-ARYL-PHENYL)SULFONYLMETHYL]PIPERIDINE} COMPOUNDS AND THEIR THERAPEUTIC USE
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain N-acyl-{4-[(4-aryl- phenyl)sulfonylmethyl]piperidine} compounds of the following formula (collectively referred to
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Page/Page column 83; 84

(2020/10/28)

AZOLE-SUBSTITUTED PYRIDINE COMPOUND
The present invention provides a compound represented by formula [I'| shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme, wherein the structure represented by formula [III] shown below represents any of the structures represented by formula group [IV] shown below, wherein R1 represents a hydrogen atom, a fluorine atom, methyl, etc.; R2, R3, and R4 each independently represent a hydrogen atom, a fluorine atom, or methyl; W represents a single bond, C1-3alkanediyl, or the formula -O-CH2CH2-; and ring A represents (a) substituted C4-6cycloalkyl, (b) substituted 4- to 6-membered saturated nitrogen-containing heterocyclyl, (c) substituted phenyl, (d) substituted pyridyl, (e) substituted 2,3-dihydrobenzofuran, (f) 4- to 6-membered saturated oxygen-containing heterocyclyl, etc.
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Paragraph 0647; 0648

(2019/01/08)

Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent
A series of novel benzamide derivatives, altering the 4-fluorophenylalkyl moiety in cisapride, were synthesized as 5-HT4 receptor agonists, and SAR of these analogs was examined on in vitro and in vivo prokinetic activities. These compounds were synthesized for high 5-HT4 receptor binding affinities and low hERG affinities. Several types of analogs were obtained and screened for 5-HT4 binding, hERG blocking, agonism, and gastric emptying assessment. Among the analogues, compound 23g showed promising results compared with the other analogs with respect to gastric emptying rates in rats. Therefore, we suggest that it may be a clinical candidate for the development of a potent prokinetic agent to treat GI disorders.
Park, Jung Sang,Im, Weonbin,Choi, Sunghak,Park, Sook Jin,Jung, Jun Min,Baek, Ki Seon,Son, Han Pyo,Sharma, Satyasheel,Kim, In Su,Jung, Young Hoon
p. 75 - 88
(2016/01/09)

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors
ATAD2 is a bromodomain-containing protein whose overexpression is linked to poor outcomes in a number of different cancer types. To date, no potent and selective inhibitors of the bromodomain have been reported. This article describes the structure-based optimization of a series of naphthyridones from micromolar leads with no selectivity over the BET bromodomains to inhibitors with sub-100 nM ATAD2 potency and 100-fold BET selectivity.
Bamborough, Paul,Chung, Chun-Wa,Furze, Rebecca C.,Grandi, Paola,Michon, Anne-Marie,Sheppard, Robert J.,Barnett, Heather,Diallo, Hawa,Dixon, David P.,Douault, Clement,Jones, Emma J.,Karamshi, Bhumika,Mitchell, Darren J.,Prinjha, Rab K.,Rau, Christina,Watson, Robert J.,Werner, Thilo,Demont, Emmanuel H.
p. 6151 - 6178
(2015/08/24)

NOVEL BENZAMIDE DERIVATIVES AND PROCESS FOR THE PREPARTION THEREOF
The present invention provides a novel benzamide derivative represented by formula 1 and an isomer, a pharmaceutically acceptable salt or hydrate thereof, and a composition for activating a 5-HT4 receptor comprising the same, as an active ingredi
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Page/Page column 12-13

(2010/05/13)

A simple, general, and highly chemoselective acetylation of alcohols using ethyl acetate as the acetyl donor catalyzed by a tetranuclear zinc cluster
In the presence of a Zn-cluster catalyst, alcohols are efficiently converted to the corresponding acetate just by refluxing in EtOAc. The mild reaction conditions enabled the reactions of various functionalized alcohols to proceed in good to excellent yield. Moreover, even when a large excess of the acetyl donor is used, the hydroxyl groups are selectively acetylated in the presence of highly nucleophilic aliphatic amino groups, approaching chemoselectivity to that of enzymatic system. Georg Thieme Verlag Stuttgart.
Iwasaki, Takanori,Maegawa, Yusuke,Hayashi, Yukiko,Ohshima, Takashi,Mashima, Kazushi
experimental part
p. 1659 - 1663
(2009/12/04)

NOVEL BENZAMIDE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
The present invention provides a novel benzamide derivative represented by formula 1 and an isomer, a pharmaceutically acceptable salt or hydrate thereof, and a composition for activating a 5-HT4 receptor comprising the same, as an active ingre
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Page/Page column 30

(2008/12/07)

3, 4-SUBSTITUTED PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF HYPERTENSION
The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The substituted pyrrolidine compounds are of the formula (I), wherein R1, R2, R3, R4, R5 and T are defined as in the specification.
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Page/Page column 205

(2010/11/24)

Pyrrole derivatives and pharmaceutical compositions which contain them as hypnotics and anticonvulsants
Pyrrole derivatives of formula STR1 in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo-[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]-oxathiino-[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino-[2,3-c]pyrrole ring-system, Y+0, S or NH, Het=naphthyridinyl or quinolyl which are unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio, CN or CF 3 and R=(3 to 10 C) alkenyl or alkyl which is unsubstituted or substituted with alkyloxy, alkylthio, cycloalkyl, alkylcarbonyl, cycloalkylcarbonyl or cycloalkylcarbamoyl in which the cycloalkyl portions contain 3 to 6 C, NH 2, alkylamino, dialkylamino, alkylcarbonylamino, 1- or 2-piperazinyl, piperidyl, piperidino, morpholino, 1-azetidinyl, pyrrolidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, piperidylcarbonyl, (1-pyrrolidinyl)carbonyl, morpholinocarbonyl, aminoalkylcarbamoyl, alkylaminoalkylcarbamoyl, dialkylaminoalkylcarbamoyl, alkyloxyalkylcarbamoyl, phenyl, pyridyl, or 1-imidazolyl, or R=2- or 3-pyrrolidinyl, or 1-imidazolyl, or 2-, 3- or 4-piperidyl, the aforesaid piperazinyl, piperidino, piperidyl, pyrrolidinyl, and azetidinyl radicals being unsubstituted or substituted at any position by alkyl, OH, alkylcarbonyl, benzyl, or hydroxyalkyl, or can form (i) a lactam group with the nitrogen atom of the ring or (ii) a 2-spirodioxolane residue with a carbon of the ring, and the said alkyl radicals containing 1 to 10 C except where specifically stated, are useful as anxiolytics.
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(2008/06/13)