Patent classifications
C07D498/22
DIOXAZINE PIGMENT AND COLORANT
An object of the present invention is to provide a dioxazine pigment having excellent fluidity. More specifically, an object of the present invention is to provide a dioxazine pigment in which practically sufficient fluidity is attained in both (1) initial viscosity and (2) storage stability when the dioxazine pigment is used in a printing ink application. The object is attained by providing a dioxazine pigment having a contact angle with respect to water according to an infiltration rate method in a range of 30° to 75°, and a contact angle with respect to 1-bromonaphthalene according to an infiltration rate method in a range of 30° to 75°.
DIOXAZINE PIGMENT AND COLORANT
An object of the present invention is to provide a dioxazine pigment having excellent fluidity. More specifically, an object of the present invention is to provide a dioxazine pigment in which practically sufficient fluidity is attained in both (1) initial viscosity and (2) storage stability when the dioxazine pigment is used in a printing ink application. The object is attained by providing a dioxazine pigment having a contact angle with respect to water according to an infiltration rate method in a range of 30° to 75°, and a contact angle with respect to 1-bromonaphthalene according to an infiltration rate method in a range of 30° to 75°.
COMPOUND FOR INHIBITING AND INDUCING DEGRADATION OF EGFR KINASE
Provided is an EGFR kinase inhibitor according to general formula (I) and a pharmaceutical composition containing the inhibitor. The invention can be used to treat diseases related to EGFR kinase, such as cancer. Also provided is a preparation and use of the above inhibitor.
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COMPOUND FOR INHIBITING AND INDUCING DEGRADATION OF EGFR KINASE
Provided is an EGFR kinase inhibitor according to general formula (I) and a pharmaceutical composition containing the inhibitor. The invention can be used to treat diseases related to EGFR kinase, such as cancer. Also provided is a preparation and use of the above inhibitor.
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SUBSTITUTED MACROCYCLIC 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 ,
- Sven Wittrock ,
- David McKinney ,
- Michael H. Serrano-Wu ,
- Chris Lemke ,
- Mark Fitzgerald ,
- Christopher Nasveschuk ,
- Kiel Lazarski ,
- Steven James Ferrara ,
- Laura Furst ,
- Guo Wei ,
- Patrick Ryan McCarren ,
- Rebecca Ann Harvey
The present invention relates to substituted macrocyclic indole derivatives of general formula (I):
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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.
SUBSTITUTED MACROCYCLIC 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 ,
- Sven Wittrock ,
- David McKinney ,
- Michael H. Serrano-Wu ,
- Chris Lemke ,
- Mark Fitzgerald ,
- Christopher Nasveschuk ,
- Kiel Lazarski ,
- Steven James Ferrara ,
- Laura Furst ,
- Guo Wei ,
- Patrick Ryan McCarren ,
- Rebecca Ann Harvey
The present invention relates to substituted 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.
Synthesis of disorazoles and analogs thereof as potent anticancer agents
In one aspect, the present disclosure provides disorazole analogs of the formula: Formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. ##STR00001##
Polymorphic forms of bictegravir and its sodium salt
The present disclosure provides crystalline forms of bictegravir, amorphous bictegravir sodium, amorphous solid dispersion of bictegravir sodium with pharmaceutically acceptable carrier and processes for the preparation thereof.
Polymorphic forms of bictegravir and its sodium salt
The present disclosure provides crystalline forms of bictegravir, amorphous bictegravir sodium, amorphous solid dispersion of bictegravir sodium with pharmaceutically acceptable carrier and processes for the preparation thereof.
Pyrazolopyrimidine derivative and use thereof
A compound of formula (II), a tautomer thereof or a pharmaceutically acceptable salt thereof, and use thereof in the preparation of medicaments for treating solid tumor-related diseases. ##STR00001##