Patent classifications
C07C325/02
Process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-B]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate and its purification for use as pharmaceutically active compound
The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) ##STR00001##
and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
PROCESS FOR PREPARING METHYL {4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL]PYRIMIDIN-5-YL}METHYLCARBAMATE AND ITS PURIFICATION FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND
The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3 -yl]pyrimidin-5 -yl methylcarbamate of the formula (I)
##STR00001##
and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3 -yl]pyrimidin-5 -yl methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
PROCESS FOR PREPARING METHYL {4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL]PYRIMIDIN-5-YL}METHYLCARBAMATE AND ITS PURIFICATION FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND
The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3 -yl]pyrimidin-5 -yl methylcarbamate of the formula (I)
##STR00001##
and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3 -yl]pyrimidin-5 -yl methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
NOVEL ANTI-FIBROTIC DRUGS
The present invention relates to new cinnamic add amides which may be used for treatment of fibrosis and neoplasia and to cinnamic acid amides for use in the treatment of fibrosis, neoplasia, arthrolithiasis, familiar mediterranean fever and pericarditis. Further, the invention relates to a pharmaceutical composition comprising said cinnamic acid amides and to a screening essay for identifying compounds suitable for the treatment of fibrosis.
NOVEL ANTI-FIBROTIC DRUGS
The present invention relates to new cinnamic add amides which may be used for treatment of fibrosis and neoplasia and to cinnamic acid amides for use in the treatment of fibrosis, neoplasia, arthrolithiasis, familiar mediterranean fever and pericarditis. Further, the invention relates to a pharmaceutical composition comprising said cinnamic acid amides and to a screening essay for identifying compounds suitable for the treatment of fibrosis.
METHOD OF QUENCHING SINGLET AND TRIPLET EXCITED STATES OF PHOTODEGRADABLE PIGMENTS, SUCH AS PORPHYRIN COMPOUNDS, PARTICULARLY PROTOPORPHYRIN IX, WITH CONJUGATED FUSED TRICYCLIC COMPOUNDS HAVING ELECTRON WITHDRAWING GROUPS, TO REDUCE GENERATION OF SINGLET OXYGEN
A method of quenching excited state energy from a photodegradable pigment that has been excited by absorption of light having a wavelength in the wavelength range of 290-800 nm, comprising reacting a pigment with a conjugated fused tricyclic compound having electron withdrawing groups of Formula (II) or a salt thereof:
##STR00001## wherein: A is selected from the group consisting of O, S, CO, CS,
##STR00002## B.sup.1, B.sup.2, D.sup.1 and D.sup.2 are each independently selected from the group consisting of F, Cl, Br, I, CF.sub.3, CC13, NR33+, NO2, CN, C(=0)R4, C(O)OR, SO2R5, aryl, and CCHR6; each m independently is 0, 1, 2, 3, or 4; a is 0 or 1; each R is independently selected from the group consisting of LI, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, and aryl; R.sup.2 is selected from the group consisting of H, alkyl, cycloalkyl, alkenyl, alkynyl, and aryl; each R.sup.3 is independently selected from the group consisting of H and C.sub.1-C.sub.6 alkyl; each R.sup.4 is independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, and aryl; each R.sup.5 is independently selected from the group consisting of H, O, OH, NH.sub.2, and Cl; and each R.sup.6 is-independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, and aryl.
METHOD OF QUENCHING SINGLET AND TRIPLET EXCITED STATES OF PHOTODEGRADABLE PIGMENTS, SUCH AS PORPHYRIN COMPOUNDS, PARTICULARLY PROTOPORPHYRIN IX, WITH CONJUGATED FUSED TRICYCLIC COMPOUNDS HAVING ELECTRON WITHDRAWING GROUPS, TO REDUCE GENERATION OF SINGLET OXYGEN
A method of quenching excited state energy from a photodegradable pigment that has been excited by absorption of light having a wavelength in the wavelength range of 290-800 nm, comprising reacting a pigment with a conjugated fused tricyclic compound having electron withdrawing groups of Formula (II) or a salt thereof:
##STR00001## wherein: A is selected from the group consisting of O, S, CO, CS,
##STR00002## B.sup.1, B.sup.2, D.sup.1 and D.sup.2 are each independently selected from the group consisting of F, Cl, Br, I, CF.sub.3, CC13, NR33+, NO2, CN, C(=0)R4, C(O)OR, SO2R5, aryl, and CCHR6; each m independently is 0, 1, 2, 3, or 4; a is 0 or 1; each R is independently selected from the group consisting of LI, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, and aryl; R.sup.2 is selected from the group consisting of H, alkyl, cycloalkyl, alkenyl, alkynyl, and aryl; each R.sup.3 is independently selected from the group consisting of H and C.sub.1-C.sub.6 alkyl; each R.sup.4 is independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, and aryl; each R.sup.5 is independently selected from the group consisting of H, O, OH, NH.sub.2, and Cl; and each R.sup.6 is-independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, and aryl.
Process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate and its purification for use as pharmaceutically active compound
The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) ##STR00001##
and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
Process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate and its purification for use as pharmaceutically active compound
The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) ##STR00001##
and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
Oxocarbon-, Pseudooxocarbon- and Radialene Compounds and Their Use
The present invention relates to oxocarbon-, pseudooxocarbon- and radialene compounds as well as to their use as doping agent for doping an organic semiconductive matrix material, as blocker material, as charge injection layer, as electrode material as well as organic semiconductor, as well as electronic components and organic semiconductive materials using them.