- Process for the manufacture of functional PFPE derivative
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A process for the manufacture of a functional (per)fluoropolyether derivative comprising at least one triazole group, such process comprising: (1) reacting a (per)fluoropolyether hydroxyl derivative having at least one hydroxyl group [derivative (PFPE-OH)] with an activating agent, to yield an activated (per)fluoropolyether hydroxyl derivative comprising at least one activated hydroxyl group [derivative (a-PFPE-OH)]; (2) reacting said activated (per)fluoropolyether hydroxyl derivative [derivative (a-PFPE-OH)] with at least one azide salt to yield a functional (per)fluoropolyether derivative comprising at least one azido group [derivative (PFPE-N3)]; and (3) reacting said functional (per)fluoropolyether derivative comprising at least one azido group [derivative (PFPE-N3)] with a hydrocarbon compound having a terminal alkyne group to yield a functional (per)fluoropolyether derivative comprising at least one triazole group [derivative (PFPE-azole)].
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- Substituted amino methyl factor Xa inhibitors
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The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- Heteroaryl-phenyl substituted factor Xa inhibitors
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The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.
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- Heteroaryl- phenyl heterobicyclic factor Xa inhibitors
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The present application describes heteroaryl-phenyl heterobicycles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- Benzimidazolinones, benzoxazolinones, benzopiperazinones, indanones, and derivatives thereof as inhibitors of factor Xa
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The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3may be N or C and J, Ja, and Jbcombine to form a substituted carbocycle or heterocycle.
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- 6-membered aromatics as factor Xa inhibitors
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The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors
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The present application describes m-amidino phenyl analogs of formula I: wherein D can be amidino and E can be phenyl, which are useful as inhibitors of factor Xa.
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- N-(AMIDINOPHENYL) CYCLOUREA ANALOGS AS FACTOR XA INHIBITORS
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The present application describes N-(amidinophenyl)cyclourea analogs of formula I: STR1 which are useful as inhibitors of factor Xa.
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- INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP
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The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
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- SYNTHESIS OF THE FIRST MONOSUBSTITUTED 1,2,4-TRIAZINE DI-N-OXIDE. 13C NMR OF 1,2,4-TRIAZINE N-OXIDES AND USE OF HYDROGEN/DEUTERIUM ISOTOPE SHIFTS FOR THE ASSIGNMENTS OF SOME DIHYDRO-1,2,4-TRIAZINE TAUTOMERS
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3-Amino-1,2,4-triazine 2,4-dioxide (4) was prepared by oxidation of 3-amino-1,2,4-triazine 2-oxide (3) with hydrogen peroxide in polyphosphoric acid, the first 1,2,4-triazine 2,4-dioxide ever reported.Some starting material gave ring contracted products as well as ring C-oxidation under a variety of reaction conditions employed in the attempted synthesis of the title compound (4). 13C nmr proved to be a method of choice for structural assignments of isomeric N-oxide.H/D isotope shifts unequivocally established the structures of compounds which could conceivably exist as several tautomers.
- Jovanovic, Misa V.
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p. 951 - 966
(2007/10/02)
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- CONFORMATIONAL STUDIES BY DINAMIC NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY. PART 27. KINETICS AND MECHANISM OF ANNULAR TAUTOMERISM IN ISOMERIC TRIAZOLES.
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The rates for the prototropic shift of the NH hydrogen in the two isomeric triazoles have been measured at low temperature by 1H n.m.r. (100 and 300 MHz), Only the less symmetric (cs) of the possible annular tautomers was found to be populated in the case of (1), whereas both (cs and c2v) were detected in (2).The relative proportions in the latter compound are dramatically dependent on temperature, concentration, and solvent.In either triazoles the kinetic process appears to be intramolecular and the mechanism corresponds to a 1,2 prototropic shift.The parameters of activation yielded similar ΔH(excit.) (5.8 and 6.5 kcal/mol) and quite negative ΔS(excit.)(-29 and -19 cal/mol.K) values,thus indicating a relatively low probability of attaining the ordered hree-membered) cyclic transition state.
- Lunazzi, Lodovico,Parisi, Francesco,Macciantelli, Dante
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p. 1025 - 1028
(2007/10/02)
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