51052-79-0Relevant academic research and scientific papers
A Practical Synthesis of the Platelet Fibrinogen Antagonist, Elarofiban
Cohen, Judith H.,Roessler, Armin,Scott, Lorraine,Sorgi, Kirk L.,Villani Jr., Frank J.,Webster, Robin R. H.,Weh, Christian,Bos, Mary Ellen,Cesco-Cancian, Sergio,Harris, Bruce D.,Hortenstine, John T.,Justus, Michael,Maryanoff, Cynthia A.,Mills, John,Muller, Stefan
, p. 866 - 872 (2013/09/05)
Elarofiban is a novel, nonpeptide, orally active fibrinogen receptor antagonist useful for the treatment of platelet mediated thrombotic disorders (Costanzo, M. J.; Hoekstra, W. J.; Maryanoff, B. E. WO, 97/41102,1997). Herein we describe the process research that was carried out for the synthesis of elarofiban that eventually led to the development of a safe and cost-effective commercial scale process.
AMINE DERIVATIVES
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, (2008/06/13)
A compound of the formula: ???whereinX and X' are the same or different, and each represents a hydrogen atom, a fluorine atom, a chlorine atom or an amino optionally having substituents, and at least one of X and X' represents a fluorine atom, a chlorine atom or an amino optionally having substituents;R1 and R2 represent a hydrogen atom or C1-6 alkyl optionally having substituents, or R1 and R2, together with the adjacent nitrogen atom, form a nitrogen-containing heterocyclic ring optionally having substituents;Y and Q are the same or different, and each represents a bond or a spacer having a main chain of 1 to 6 atoms;... represents a single bond or a double bond;T1 and T2 are the same or different, and each represents C(R9) (R9 represents a hydrogen atom, a hydroxy or C1-6 alkyl) or N, when each of the adjacent ... is a single bond, and C when the adjacent ... is a double bond; andAr represents an aromatic group optionally having substituents, a C3-9 cycloalkyl group optionally having substituents, a 3 to 9-membered saturated heterocyclic group optionally having substituents, a hydrogen atom or a halogen atom; provided that 6-chloro-3-(R,S)-(N,N-dimethylamino)methyl-1-[3-(indol-3-yl)-2-[(R)-(4-phenylpiperazin-1-yl)carbonylamino]propanoyl]-1,2,3,4-tetrahydroquinoline; 6-chloro-3-(R,S)-(N,N-dimethylamino)methyl-1-[3-(indol-3-yl)-2-[(R)-4-(2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)piperidinocarbonylamino]propanoyl]-1,2,3,4-tetrahydroquinoline and 1-benzoyl-N-[(R)-2-[6-chloro-3-[(N,N-dimethylamino)methyl]-1,2,3,4-tetrahydroquinolin-1-yl]-1-[3-(indol-3-yl)propanoyl]-4-piperidinecarboxamide are excluded; a salt thereof or a prodrug thereof has an excellent somatostatin receptor binding inhibition action and is useful for preventing and/or treating diseases associated with somatostatin.
Tricycle substituted with azaheterocyclic carboxylic acids
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, (2008/06/13)
The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, R1, R2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
Partial GABAA Receptor Agonists. Synthesis and in Vitro Pharmacology of a Series of Nonannulated Analogs of 4,5,6,7-Tetrahydroisoxazolopyridin-3-ol
Froelund, Bente,Kristiansen, Uffe,Brehm, Lotte,Hansen, Annette B.,Krogsgaard-Larsen, Povl,Falch, Erik
, p. 3287 - 3296 (2007/10/02)
5-(4-Piperidyl)isoxazol-3-ol (4-PIOL, 10), a structural analog of 4-aminobutanoic acid (GABA, 1) and the GABAA agonist 4,5,6,7-tetrahydroisoxazolopyridin-3-ol (THIP, 5), is a low-efficiacy partial GABAA agonist.A number of com
