155137-18-1Relevant articles and documents
Synthesis method of 4,4-difluoropiperidine-1-formyl chloride
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Paragraph 0012; 0016; 0019, (2019/11/12)
The invention discloses a synthesis method of 4,4-difluoropiperidine-1-formyl chloride. The synthesis method comprises the following steps that first, a compound I, namely benzylpiperidin-4-one, and afluorine reagent are deoxidized and fluorated in a firs
Eliminative Deoxofluorination Using XtalFluor-E: A One-Step Synthesis of Monofluoroalkenes from Cyclohexanone Derivatives
Vandamme, Mathilde,Paquin, Jean-Fran?ois
supporting information, p. 3604 - 3607 (2017/07/15)
The eliminative deoxofluorination of cyclohexanone derivatives using XtalFluor-E is described. The corresponding monofluoroalkenes are obtained in up to 79% yield. Notably, this one-step procedure occurs at room temperature using readily accessible and cost-effective reagents.
ANTI-PULMONARY TUBERCULOSIS NITROIMIDAZOLE DERIVATIVE
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Paragraph 0260-0262, (2017/12/31)
Disclosed is a substituted nitroimidazole derivative, which is mainly used for treating related diseases caused by mycobacterial infections, such as Mycobacterium tuberculosis, especially being suitable for diseases caused by resistant Mycobacterium tuberculosis.
PYRAZOLE DERIVATIVES
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Page/Page column 33, (2010/11/26)
A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.
PYRAZOLE DERIVATIVE
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Page/Page column 41, (2010/11/27)
A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
1,5-DIHETEROCYCLE-1H-TRIAZOLE DERIVATIVE
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Page/Page column 26-27, (2010/11/27)
The present invention relates to a compound represented by Formula (I): wherein Ar1, Ar2, R1 and R2 each represent a substituent, a salt thereof, or a solvate of the compound or the salt, and to a medicine containing the same. According to the present invention, a potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
FIVE-MEMBERED HETEROCYCLIC DERIVATIVE
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Page/Page column 53, (2010/11/08)
The present invention relates to a compound represented by formula (I): a salt of the compound, or a solvate of the compound or the salt; a drug containing any of the compounds, the salts, and the solvates; a preventive and/or therapeutic agent for an ischemic disease containing any of the compounds, the salts, and the solvates; and a platelet coagulation inhibitor containing any of the compounds, the salts, and the solvates. The compound of the present invention is useful as a strong platelet coagulation inhibitor without inhibiting COX-1 or COX-2.
Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl] piperidine series of histamine H3 receptor antagonists
Berlin, Michael,Ting, Pauline C.,Vaccaro, Wayne D.,Aslanian, Robert,McCormick, Kevin D.,Lee, Joe F.,Albanese, Margaret M.,Mutahi, Mwangi W.,Piwinski, John J.,Shih, Neng-Yang,Duguma, Luli,Solomon, Daniel M.,Zhou, Wei,Sher, Rosy,Favreau, Leonard,Bryant, Matthew,Korfmacher, Walter A.,Nardo, Cymbelene,West Jr., Robert E.,Anthes, John C.,Williams, Shirley M.,Wu, Ren-Long,Susan She,Rivelli, Maria A.,Corboz, Michel R.,Hey, John A.
, p. 989 - 994 (2007/10/03)
A novel series of histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine template displaying low CYP2D6 and CYP3A4 inhibitory profiles has been identified. Structural features responsible for the reduction of P450 activity, a typical liability of 4-substituted imidazoles, have been established.
COMPOUNDS HAVING AFFINITY AT 5HT2C RECEPTOR AND USE THEREOF IN THERAPY
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Page/Page column 13, (2008/06/13)
Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: wherein R1 is hydrogen, hydroxy, fluoro, chloro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC
Synthesis and evaluation of (piperidinomethylene)bis(phosphonic acid) derivatives as anti-osteoporosis agents
Mimura,Hayashida,Nomiyama,Ikegami,Iida,Tamura,Hiyama,Ohishi
, p. 1971 - 1986 (2007/10/02)
Some (piperidinomethylene)bis(phosphonic acid) derivatives were prepared and their activity to inhibit a rise in serum calcium induced by parathyroid hormone in thyroparathyroidectomised rats was evaluated. Several (4- alkylidene-, 4,4-dialkyl-, or 4-alkyl-4- halopiperidinomethylene)bis(phosphonic acid) derivatives showed considerable inhibitory activity. But compounds having aromatic and polar substituents such as azido, hydroxy, amino and amido on the piperidine ring were generally inactive. In this study, two 4-alkylidene compounds (8a and 8b) and a 4,4- cyclic dialkyl compound (61) showed potent activity when administered either intravenously or perorally.