Patent classifications
C07D221/10
RARE EARTH COMPLEX
A rare earth complex is represented by general formula (1).
M.sup.3+.Math.(HC).sub.n.Math.(L.sup.1).sub.m.sub.
Dyes and labeled molecules
Dimeric and trimeric nucleic acid dyes, and associated systems and methods are provided. Such a dye may form a hairpin-like structure that enables it to stain nucleic acids via a release-on-demand mechanism, for example. Such a dye may have low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, for example. A dye provided herein may be useful in a variety of applications, such as in DNA quantitation in real-time PCR, for example.
Dyes and labeled molecules
Dimeric and trimeric nucleic acid dyes, and associated systems and methods are provided. Such a dye may form a hairpin-like structure that enables it to stain nucleic acids via a release-on-demand mechanism, for example. Such a dye may have low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, for example. A dye provided herein may be useful in a variety of applications, such as in DNA quantitation in real-time PCR, for example.
Methods and kits using extended rhodamine dyes
Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure ##STR00001##
are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure ##STR00002## In addition, methods of making and using the dyes as fluorescent labels are disclosed.
Methods and kits using extended rhodamine dyes
Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure ##STR00001##
are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure ##STR00002## In addition, methods of making and using the dyes as fluorescent labels are disclosed.
SYNTHESIS OF THERAPEUTIC AND DIAGNOSTIC DRUGS CENTERED ON REGIOSELECTIVE AND STEREOSELECTIVE RING OPENING OF AZIRIDINIUM IONS
Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
MOLECULAR EDITING OF MULTIPLE C-H BONDS LEVERAGING RECOGNITION OF DISTANCE, GEOMETRY AND CHIRALITY
This disclosure provides functional templates that direct Pd to functionalize multiple CH bonds in polycyclic aza-arenes such as quinolines and related heterocycles at locations that are difficult to isolate and reach for substitution. Herein disclosed are two conceptually distinct directing templates (T) that enable site-selective C6 and C7-H activation of polycyclic aza-arenes. These catalytic pyridine-based templates recruit the aza-arene substrate through N-coordination, enabling the directing arm to deliver the catalyst and precisely activate remote and adjacent C6 or C7-H bond (FIG. 1d). In parallel, we discovered that the use of a simple and readily prepared template chaperone (TC) can turn over the directing template, allowing it to be used catalytically for the first time. Notably, chiral recognition is vital in the granular discrimination between competing C3 and C7-H bonds when the differentiation via distance and geometry is insufficient. Thus, precise recognition of a directing template's distance, geometry and chirality now enables the iterative CH editing of quinoline and related pharmacophores at any desired site and order. The methods disclosed herein can also be used for diverse and late-stage modification of heterocycle-based drug molecules and pharmacophores.
NOVEL HEPATOSELECTIVE POLYADENYLATING POLYMERASES INHIBITORS AND THEIR METHOD OF USE
Described herein are hepatoselective inhibitors of PAPD 5 and 7 having a disease-modifying action in the treatment of diseases associated with PAPD 5 and 7 that include disease such as hepatitis B and liver cancer. Compositions comprising same; and methods of making and using same are also described herein.
Compound or salt thereof
The present invention relates to a compound represented by the following General Formula (1) or a salt thereof. ##STR00001## In General Formula (1), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a linear or branched alkyl group which may have a substituent or the like. R.sup.1 and R.sup.2 may be bonded to each other to form a ring. R.sup.3 and R.sup.4 may be bonded to each other to form a ring. R.sup.1 and/or R.sup.2 may be bonded to a 6-membered ring to which NR.sup.1R.sup.2 is bonded to form a ring. R.sup.3 and/or R.sup.4 may be bonded to a 6-membered ring to which NR.sup.3R.sup.4 is bonded to form a ring. R.sup.5 represents .sup.11CH.sub.3, a linear or branched alkyl group which may have a substituent or the like. R.sup.6 represents F, .sup.18F or the like. X, Y and Z each independently represent a carbon atom, an oxygen atom or the like. n is 0 or 1.