Patent classifications
C07D498/16
Macrocyclic indole derivatives
- Sarah Anna Liesa Johannes ,
- Philipp Buchgraber ,
- Ulrich Klar ,
- Clara Christ ,
- Kai Thede ,
- Joachim Kuhnke ,
- Manfred Moewes ,
- Knut Eis ,
- Amaury Ernesto Fernandez-Montalvan ,
- Nicolas Werbeck ,
- Ursula Mönning ,
- Philip Lienau ,
- Ulrike Sack ,
- Arne Scholz ,
- Michael H. Serrano-Wu ,
- Christopher Lemke ,
- David McKinney ,
- Mark Fitzgerald ,
- Christopher Nasveschuk ,
- Kiel Lazarski ,
- Steven James Ferrara ,
- Laura Furst ,
- Guo Wei ,
- Patrick Ryan McCarren
The present invention relates to macrocyclic indole derivatives of general formula (I) ##STR00001##
in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
Macrocyclic indole derivatives
- Sarah Anna Liesa Johannes ,
- Philipp Buchgraber ,
- Ulrich Klar ,
- Clara Christ ,
- Kai Thede ,
- Joachim Kuhnke ,
- Manfred Moewes ,
- Knut Eis ,
- Amaury Ernesto Fernandez-Montalvan ,
- Nicolas Werbeck ,
- Ursula Mönning ,
- Philip Lienau ,
- Ulrike Sack ,
- Arne Scholz ,
- Michael H. Serrano-Wu ,
- Christopher Lemke ,
- David McKinney ,
- Mark Fitzgerald ,
- Christopher Nasveschuk ,
- Kiel Lazarski ,
- Steven James Ferrara ,
- Laura Furst ,
- Guo Wei ,
- Patrick Ryan McCarren
The present invention relates to macrocyclic indole derivatives of general formula (I) ##STR00001##
in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
Near-infrared nerve-sparing fluorophores
The compounds provided herein are phenoxazines that can be used as far red to near-infrared nerve-sparing fluorescent compounds in medical procedures.
Near-infrared nerve-sparing fluorophores
The compounds provided herein are phenoxazines that can be used as far red to near-infrared nerve-sparing fluorescent compounds in medical procedures.
COVALENT RAS INHIBITORS AND USES THEREOF
The disclosure features compounds, or pharmaceutically acceptable salts thereof, alone and in combination with other therapeutic agents, pharmaceutical compositions, and protein conjugates thereof, capable of modulating biological processes including Ras, and their uses in the treatment of cancers.
COVALENT RAS INHIBITORS AND USES THEREOF
The disclosure features compounds, or pharmaceutically acceptable salts thereof, alone and in combination with other therapeutic agents, pharmaceutical compositions, and protein conjugates thereof, capable of modulating biological processes including Ras, and their uses in the treatment of cancers.
CYCLIC COMPOUNDS AND METHODS OF USING SAME
The present application relates to compounds of Formula (I), as defined herein, and pharmaceutically acceptable salts thereof. The present application also describes pharmaceutical composition comprising a compound of Formula (I), and pharmaceutically acceptable salts thereof, and methods of using the compounds and compositions for inhibiting kinase activity, and for treating cancer.
CYCLIC COMPOUNDS AND METHODS OF USING SAME
The present application relates to compounds of Formula (I), as defined herein, and pharmaceutically acceptable salts thereof. The present application also describes pharmaceutical composition comprising a compound of Formula (I), and pharmaceutically acceptable salts thereof, and methods of using the compounds and compositions for inhibiting kinase activity, and for treating cancer.
PRC1 INHIBITORS AND METHODS OF TREATMENT THEREWITH
Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.
PRC1 INHIBITORS AND METHODS OF TREATMENT THEREWITH
Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.