Patent classifications
C07D279/28
Phenothiazine derivatives and uses thereof
The present invention provides phenothiazine compounds, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment of various diseases or conditions, for example ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA).
Phenothiazine derivatives and uses thereof
The present invention provides phenothiazine compounds, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment of various diseases or conditions, for example ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA).
NEW CLASS OF ANTIBIOTICS HAVING LOW MIC-VALUES TOWARDS DIFFERENT STRAINS OF BACTERIA
The present invention relates to a composition comprising a compound of formula (I) wherein X is selected from the group consisting of S, Se, P, PO, SO, NR.sup.1, CR.sup.1, CR.sup.1R.sup.1 or C.sub.0-2-alkyl; Z is selected from the group consisting of hydrogen, a halogen, SR.sup.4, OR.sup.4, COR.sup.4 where R.sup.4 is a C.sub.1-12-alkyl; each R.sup.2 is independently selected from the group consisting of C.sub.1-6-alkyl, halogen, C.sub.3-8-cycloalkyl, OH, NH.sub.2, NHR.sup.1, N(R.sup.1).sub.2, O—C.sub.1-6-alkyl, O—C.sub.3-8-cycloalkyl, NH—C.sub.1-6-alkyl, NH—C.sub.3-8-cycloalkyl, S—C.sub.1-6-alkyl, S—C.sub.3-8-cycloalkyl, aryl, heteroaryl, aryloxy, heteroaryloxy, arylamino, heteroarylamino, arylalkyl, heteroarylalkyl, arylalkyloxy and heteroarylalkyloxy; d is selected from 0, 1, 2, and 3; each R.sup.3 is independently selected from the group consisting of C.sub.1-6-alkyl, halogen, C.sub.3-8-cycloalkyl, OH, NH.sub.2, NHR.sup.1, N(R.sup.1).sub.2, O—C.sub.1-6-alkyl, O—C.sub.3-8-cycloalkyl, NH—C.sub.1-6-alkyl, NH—C.sub.3-8-cycloalkyl, S—C.sub.1-6-alkyl, S-C3-8-cycloalkyl, aryl, heteroaryl, aryloxy, heteroaryloxy, arylamino, heteroarylamino, arylalkyl, heteroarylalkyl, arylalkyloxy and heteroarylalkyloxy; e is selected from 0, 1, 2, 3, and 4; R.sup.1 is selected from the group consisting of C.sub.1-6-alkyl, C.sub.3-8-cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; R.sup.5 is N—(CHW)—N(Y.sup.1)(Y.sup.2)(Y.sup.3) or C═CH—(CHW)—N(Y.sup.1)(Y.sup.2)(Y.sup.3); each W is individually selected from the group consisting of linear or branched C.sub.1-6-alkyl or together with the nitrogen atom —N(Y.sup.1)(Y.sup.2)(Y.sup.3)— to which it is attached forms an optionally substituted nitrogen-containing heteroaryl or optionally substituted nitrogen-containing heterocyclyl together with Y.sup.1 where; Y.sup.1 is selected from the group consisting of C.sub.1-12-alkyl or together with the W and the nitrogen atom to which it is attached forms an optionally substituted nitrogen-containing heteroaryl or optionally substituted nitrogen-containing heterocyclyl; Y.sup.2 is selected from the group consisting of C.sub.1-12-alkyl; Y.sup.3 is selected from the group consisting of linear or branched C.sub.2-25-alkyl, linear or branched C.sub.2-25 alkenyl or linear or branched C.sub.2-25 alkynyl; where A is selected from any pharmaceutical relevant/acceptable anion/counterion; wherein if X is S and Z is a halogen then Y.sup.3 cannot be a C.sub.2-alkyl or a branched C.sub.3-alkyl; wherein if X is S and Z is hydrogen then Y.sup.3 cannot be C.sub.2-alkyl or linear or branched C.sub.5-alkyl. The invention also relates to anti-microbial composition fo
NEW CLASS OF ANTIBIOTICS HAVING LOW MIC-VALUES TOWARDS DIFFERENT STRAINS OF BACTERIA
The present invention relates to a composition comprising a compound of formula (I) wherein X is selected from the group consisting of S, Se, P, PO, SO, NR.sup.1, CR.sup.1, CR.sup.1R.sup.1 or C.sub.0-2-alkyl; Z is selected from the group consisting of hydrogen, a halogen, SR.sup.4, OR.sup.4, COR.sup.4 where R.sup.4 is a C.sub.1-12-alkyl; each R.sup.2 is independently selected from the group consisting of C.sub.1-6-alkyl, halogen, C.sub.3-8-cycloalkyl, OH, NH.sub.2, NHR.sup.1, N(R.sup.1).sub.2, O—C.sub.1-6-alkyl, O—C.sub.3-8-cycloalkyl, NH—C.sub.1-6-alkyl, NH—C.sub.3-8-cycloalkyl, S—C.sub.1-6-alkyl, S—C.sub.3-8-cycloalkyl, aryl, heteroaryl, aryloxy, heteroaryloxy, arylamino, heteroarylamino, arylalkyl, heteroarylalkyl, arylalkyloxy and heteroarylalkyloxy; d is selected from 0, 1, 2, and 3; each R.sup.3 is independently selected from the group consisting of C.sub.1-6-alkyl, halogen, C.sub.3-8-cycloalkyl, OH, NH.sub.2, NHR.sup.1, N(R.sup.1).sub.2, O—C.sub.1-6-alkyl, O—C.sub.3-8-cycloalkyl, NH—C.sub.1-6-alkyl, NH—C.sub.3-8-cycloalkyl, S—C.sub.1-6-alkyl, S-C3-8-cycloalkyl, aryl, heteroaryl, aryloxy, heteroaryloxy, arylamino, heteroarylamino, arylalkyl, heteroarylalkyl, arylalkyloxy and heteroarylalkyloxy; e is selected from 0, 1, 2, 3, and 4; R.sup.1 is selected from the group consisting of C.sub.1-6-alkyl, C.sub.3-8-cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; R.sup.5 is N—(CHW)—N(Y.sup.1)(Y.sup.2)(Y.sup.3) or C═CH—(CHW)—N(Y.sup.1)(Y.sup.2)(Y.sup.3); each W is individually selected from the group consisting of linear or branched C.sub.1-6-alkyl or together with the nitrogen atom —N(Y.sup.1)(Y.sup.2)(Y.sup.3)— to which it is attached forms an optionally substituted nitrogen-containing heteroaryl or optionally substituted nitrogen-containing heterocyclyl together with Y.sup.1 where; Y.sup.1 is selected from the group consisting of C.sub.1-12-alkyl or together with the W and the nitrogen atom to which it is attached forms an optionally substituted nitrogen-containing heteroaryl or optionally substituted nitrogen-containing heterocyclyl; Y.sup.2 is selected from the group consisting of C.sub.1-12-alkyl; Y.sup.3 is selected from the group consisting of linear or branched C.sub.2-25-alkyl, linear or branched C.sub.2-25 alkenyl or linear or branched C.sub.2-25 alkynyl; where A is selected from any pharmaceutical relevant/acceptable anion/counterion; wherein if X is S and Z is a halogen then Y.sup.3 cannot be a C.sub.2-alkyl or a branched C.sub.3-alkyl; wherein if X is S and Z is hydrogen then Y.sup.3 cannot be C.sub.2-alkyl or linear or branched C.sub.5-alkyl. The invention also relates to anti-microbial composition fo
PHENOTHIAZINE DERIVATIVES AND USES THEREOF
The present invention provides phenothiazine compounds, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment of various diseases or conditions, for example ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA).
PHENOTHIAZINE DERIVATIVES AND USES THEREOF
The present invention provides phenothiazine compounds, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment of various diseases or conditions, for example ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA).
UBIQUITIN-SPECIFIC PEPTIDASE 24 INHIBITOR, MEDICINAL COMPOSITION INCLUDING THE SAME AND METHOD OF DELAYING OR REVERSING MULTIDRUG RESISTANCE IN CANCERS USING THE SAME
The present invention relates to a ubiquitin-specific peptidase 24 inhibitor, a medicinal composition including the same and a method of delaying or reversing multidrug resistance in cancers using the same. The USP24 inhibitor, which includes a shUSP24 RNA and/or a carbonyl substituted phenyl compound, can serve as a chemosensitizing agent for inhibiting the drug pump out, cancer sternness and genomic instability of cancer cells, thereby being applied to a medicinal composition and a method for delaying or reversing multidrug resistance in cancers.
Ubiquitin-specific peptidase 24 inhibitor, medicinal composition including the same and method of delaying or reversing multidrug resistance in cancers using the same
The present invention relates to a ubiquitin-specific peptidase 24 inhibitor, a medicinal composition including the same and a method of delaying or reversing multidrug resistance in cancers using the same. The USP24 inhibitor, which includes a shUSP24 RNA and/or a carbonyl substituted phenyl compound, can serve as a chemosensitizing agent for inhibiting the drug pump out, cancer sternness and genomic instability of cancer cells, thereby being applied to a medicinal composition and a method for delaying or reversing multidrug resistance in cancers.
Ubiquitin-specific peptidase 24 inhibitor, medicinal composition including the same and method of delaying or reversing multidrug resistance in cancers using the same
The present invention relates to a ubiquitin-specific peptidase 24 inhibitor, a medicinal composition including the same and a method of delaying or reversing multidrug resistance in cancers using the same. The USP24 inhibitor, which includes a shUSP24 RNA and/or a carbonyl substituted phenyl compound, can serve as a chemosensitizing agent for inhibiting the drug pump out, cancer sternness and genomic instability of cancer cells, thereby being applied to a medicinal composition and a method for delaying or reversing multidrug resistance in cancers.
Anti-infective heterocyclic compounds and uses thereof
The present invention relates to heterocyclic compounds of Formula I useful as anti-infective agents. The present invention further relates to a method of treating an infection by administering such compounds, and to pharmaceutical compositions comprising such compounds. ##STR00001##