Patent classifications
A61K31/4162
Prodrugs of fused-bicyclic C5aR antagonists
The present disclosure provides, inter alia, Compounds of Formulae IA, IB, IC, IIA, IIB and IIC or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications. ##STR00001## ##STR00002##
COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISEASES
Compositions comprising satiety peptides (e.g., PYY, PYY(3-36), GLP-1, oxyntomodulin, and cholecystokinin) and DPP-IV inhibitors and methods of treating metabolic diseases with such compositions are provided.
COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISEASES
Compositions comprising satiety peptides (e.g., PYY, PYY(3-36), GLP-1, oxyntomodulin, and cholecystokinin) and DPP-IV inhibitors and methods of treating metabolic diseases with such compositions are provided.
Macrocyclic chlorine substituted indole derivatives
- Kai Thede ,
- Anne Mengel ,
- Clara Christ ,
- Joachim Kuhnke ,
- Sarah Anna Liesa Johannes ,
- Philipp Buchgraber ,
- Ulrich Klar ,
- Ulrike Rauh ,
- Stefan Kaulfuss ,
- Amaury Ernesto Fernandez-Montalvan ,
- Nicolas Werbeck ,
- Ursula Moenning ,
- Katrin Nowak-Reppel ,
- Chris Lemke ,
- Michael H. Serrano-Wu ,
- David McKinney ,
- Mark Fitzgerald ,
- Christopher Nasveschuk ,
- Kiel Lazarski ,
- Steven J. Ferrara ,
- Laura Furst ,
- Guo Wei ,
- Patrick R. McCarren ,
- Rebecca Ann Harvey ,
- Daniel Payne ,
- Thomas Pesnot ,
- Craig Wilson
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 chlorine substituted indole derivatives
- Kai Thede ,
- Anne Mengel ,
- Clara Christ ,
- Joachim Kuhnke ,
- Sarah Anna Liesa Johannes ,
- Philipp Buchgraber ,
- Ulrich Klar ,
- Ulrike Rauh ,
- Stefan Kaulfuss ,
- Amaury Ernesto Fernandez-Montalvan ,
- Nicolas Werbeck ,
- Ursula Moenning ,
- Katrin Nowak-Reppel ,
- Chris Lemke ,
- Michael H. Serrano-Wu ,
- David McKinney ,
- Mark Fitzgerald ,
- Christopher Nasveschuk ,
- Kiel Lazarski ,
- Steven J. Ferrara ,
- Laura Furst ,
- Guo Wei ,
- Patrick R. McCarren ,
- Rebecca Ann Harvey ,
- Daniel Payne ,
- Thomas Pesnot ,
- Craig Wilson
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 chlorine substituted indole derivatives
- Kai Thede ,
- Anne Mengel ,
- Clara Christ ,
- Joachim Kuhnke ,
- Sarah Anna Liesa Johannes ,
- Philipp Buchgraber ,
- Ulrich Klar ,
- Ulrike Rauh ,
- Stefan Kaulfuss ,
- Amaury Ernesto Fernandez-Montalvan ,
- Nicolas Werbeck ,
- Ursula Moenning ,
- Katrin Nowak-Reppel ,
- Chris Lemke ,
- Michael H. Serrano-Wu ,
- David McKinney ,
- Mark Fitzgerald ,
- Christopher Nasveschuk ,
- Kiel Lazarski ,
- Steven J. Ferrara ,
- Laura Furst ,
- Guo Wei ,
- Patrick R. McCarren ,
- Rebecca Ann Harvey ,
- Daniel Payne ,
- Thomas Pesnot ,
- Craig Wilson
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 AS INHIBITORS OF MCL-1
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.
Anti-cancer compounds targeting Ral GTPases and methods of using the same
Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.
Anti-cancer compounds targeting Ral GTPases and methods of using the same
Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.
Anti-cancer compounds targeting Ral GTPases and methods of using the same
Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.