- Synthesis method of 4,4-difluoropiperidine-1-formyl chloride
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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
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Paragraph 0012; 0013; 0016; 0017; 0019; 0020
(2019/11/12)
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- Aryl alkynyl hydrocarbon compound and preparation method and application thereof
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The invention relates to an aryl alkynyl hydrocarbon compound and a medicine compound containing the compound. The compound or the medicine compound can serve as an inhibitor of Retinoid-related orphan receptor gamma t (RORyt). The invention further relates to a method for preparing the compound and the medicine compound and application thereof to mammal treatment or prevention, especially RORyt mediated inflammation of humans or autoimmune diseases.
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- QUINOLINE OR ISOQUINOLINE SUBSTITUTED P2X7 ANTAGONISTS
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The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I)
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Page/Page column 16
(2009/12/05)
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- PYRAZOLE COMPOUNDS HAVING CANNABINOID RECEPTOR (CB1) ANTAGONIZING ACTIVITY
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The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: -N(R7)-, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: -N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
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Page/Page column 119
(2008/06/13)
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- Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl] piperidine series of histamine H3 receptor antagonists
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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.
- 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.
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p. 989 - 994
(2007/10/03)
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- Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains
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A series of benzoxathiin SERAMs with heteroatom-substituted amine side chains was prepared. Minor modifications in the side chain resulted in significant effects on biological activity, especially in uterine tissue.
- Blizzard, Timothy A.,DiNinno, Frank,Morgan II, Jerry D.,Wu, Jane Y.,Chen, Helen Y.,Kim, Seongkon,Chan, Wanda,Birzin, Elizabeth T.,Yang, Yi Tien,Pai, Lee-Yuh,Zhang, Zhoupeng,Hayes, Edward C.,DaSilva, Carolyn A.,Tang, Wei,Rohrer, Susan P.,Schaeffer, James M.,Hammond, Milton L.
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p. 3865 - 3868
(2007/10/03)
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- Quinolinecarboxamides as antiviral agents
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The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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