- AMINOPYRIMIDINE HETEROCYCLIC COMPOUND WITH ADENOSINE RECEPTOR ANTAGONISTIC ACTIVITY
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Disclosed hereinis an aminopyrimidine heterocyclic compound with adenosine receptor antagonistic activity, comprising a compound of the general formula (I), or a pharmaceutically acceptable salt thereof. The aminopyrimidine heterocyclic compound with adenosine receptor antagonistic activitydisclosed herein can be used as an effective adenosine receptor antagonist, and can be used for the treatment or prevention of disorders caused by abnormal level of adenosine.
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Paragraph 000101; 000102; 000103
(2017/06/23)
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- Novel benzamide-based histamine H3 receptor antagonists: The identification of two candidates for clinical development
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The preclinical characterization of novel phenyl(piperazin-1-yl)methanones that are histamine H3 receptor antagonists is described. The compounds described are high affinity histamine H3 antagonists. Optimization of the physical properties of these histamine H3 antagonists led to the discovery of several promising lead compounds, and extensive preclinical profiling aided in the identification of compounds with optimal duration of action for wake promoting activity. This led to the discovery of two development candidates for Phase I and Phase II clinical trials.
- Letavic, Michael A.,Aluisio, Leah,Apodaca, Richard,Bajpai, Manoj,Barbier, Ann J.,Bonneville, Anne,Bonaventure, Pascal,Carruthers, Nicholas I.,Dugovic, Christine,Fraser, Ian C.,Kramer, Michelle L.,Lord, Brian,Lovenberg, Timothy W.,Li, Lilian Y.,Ly, Kiev S.,McAllister, Heather,Mani, Neelakandha S.,Morton, Kirsten L.,Ndifor, Anthony,Nepomuceno, S. Diane,Pandit, Chennagiri R.,Sands, Steven B.,Shah, Chandra R.,Shelton, Jonathan E.,Snook, Sandra S.,Swanson, Devin M.,Xiao, Wei
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supporting information
p. 450 - 454
(2015/04/27)
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- Copper-promoted N-cyclopropylation of anilines and amines by cyclopropylboronic acid
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Reaction of anilines, primary and secondary aliphatic amines with cyclopropylboronic acid in dichloroethane in the presence of Cu(OAc)2 (1 equiv.), 2,2′-bipyridine (1 equiv.) and sodium carbonate or sodium bicarbonate (2 equiv.) under air atmos
- Benard, Sebastien,Neuville, Luc,Zhu, Jieping
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supporting information; experimental part
p. 3393 - 3395
(2010/07/06)
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- AURORA KINASE INHIBITORS
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Disclosed herein are Aurora kinase Inhibitors represented by Structural Formula (I): Values for the variables in Structural Formula (I) are defined herein.
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Page/Page column 68-69
(2009/10/22)
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- NOVEL COMPOUNDS
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There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
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Page/Page column 117; 129
(2008/12/06)
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- SUBSTITUTED BENZAMIDE MODULATORS OF THE HISTAMINE H3 RECEPTOR
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Certain substituted benzamide compounds are histamine H3receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
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Page/Page column 38-39
(2008/06/13)
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- CYCLOPROPYL AMINES AS MODULATORS OF THE HISTAMINE H3 RECEPTOR
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Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.
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Page/Page column 8
(2010/11/26)
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- PYRAZOLE DERIVATIVES
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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.
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Page/Page column 36
(2010/11/26)
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- NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES
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The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.
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Page/Page column 63
(2010/11/27)
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- NOVEL PROCESSES FOR THE PREPARATION OF PIPERAZINYL AND DIAZAPANYL BENZAMIDE DERIVATIVES
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The present invention is directed to novel processes for the preparation of substituted piperazinyl and diazepanyl benzamides, useful for the treatment of disorders and conditions mediated by the histamine receptor.
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Page/Page column 84
(2010/11/27)
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- FIVE-MEMBERED HETEROCYCLIC DERIVATIVE
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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.
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Page/Page column 47-48
(2010/11/08)
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- 1-Alkyl-4-acylpiperazines as a new class of imidazole-free histamine H 3 receptor antagonists
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With the aim of identifying structurally novel, centrally acting histamine H3 antagonists, arrays of monoacyldiamines were screened. This led to the discovery of a series of 1-alkyl-4-acylpiperazines which were potent antagonists at the human histamine H3 receptor. The most potent amides had antagonist potencies in the subnanomolar range.
- Zaragoza, Florencio,Stephensen, Henrik,Knudsen, Sanne M.,Pridal, Lone,Wulff, Birgitte S.,Rimvall, Karin
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p. 2833 - 2838
(2007/10/03)
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- A simple method for the formation of cyclopropylamines: The first synthesis of tricyclopropylamine
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A mild, one-step method to cyclopropylate amines is described. Treatment of a variety of secondary and primary amines with [(1-ethoxycyclopropyl)oxy]trimethylsilane and sodium cyanoborohydride in methanol gave mono- and dicyclopropylamines in good yield. Sterically hindered di- and tricyclopropylamines, including the previously unreported tricyclopropylamine, were prepared using this method. The pKas of some mono-, di- and tricyclopropylamines were measured showing a reduction of ~1-2 pKa unit per added cyclopropyl group.
- Gillaspy, Melissa L.,Lefker, Bruce A.,Hada, William A.,Hoover, Dennis J.
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p. 7399 - 7402
(2007/10/02)
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- Piperazine-1-carboxylic acid esters possessing antidepressant or analgesic activity
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Piperazine-1-carboxylic acid esters which are useful as antidepressants and as analgesics.
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