C07D473/28

Crystalline form of GnRH receptor antagonist and preparation method therefor

Provided are a crystalline form of a GnRH receptor antagonist and a preparation method therefor. Specifically, provided are a crystalline form I of 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(6-methoxypyridazin-3-yl)-4,6-dicarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxy urea (a compound of formula I) and a preparation method, the use of same in a pharmaceutical composition and the use of the crystalline form I and the composition in the preparation of a drug for treating diseases associated with a GnRH receptor antagonist.

Heterocyclic amide compound

Provided is a heterocyclic amide compound that may have a PRS inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for PRS associated diseases and the like including cancer. A compound represented by the following formula (I): ##STR00001##
wherein a group represented by ##STR00002##
is a group represented by the following formula (II) or the following formula (III): ##STR00003##
and other symbols are as described in the DESCRIPTION, or a salt thereof.

Heterocyclic amide compound

Provided is a heterocyclic amide compound that may have a PRS inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for PRS associated diseases and the like including cancer. A compound represented by the following formula (I): ##STR00001##
wherein a group represented by ##STR00002##
is a group represented by the following formula (II) or the following formula (III): ##STR00003##
and other symbols are as described in the DESCRIPTION, or a salt thereof.

Substituted purine derivative

The present invention relates to a substituted purine derivative of formula (1) wherein R.sup.1 is alkoxy or the like, R.sup.2 is alkyl or the like, Ring Q.sup.1 is aryl or the like, W.sup.1 is alkylene or the like, Ring Q.sup.2 is aromatic carbocyclyl or the like, n is 1-4, R.sup.3 is hydrogen atom or the like, X.sup.1 is single bond or the like, W.sup.2 is alkylene or the like, and R.sup.4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease. ##STR00001##

Substituted purine derivative

The present invention relates to a substituted purine derivative of formula (1) wherein R.sup.1 is alkoxy or the like, R.sup.2 is alkyl or the like, Ring Q.sup.1 is aryl or the like, W.sup.1 is alkylene or the like, Ring Q.sup.2 is aromatic carbocyclyl or the like, n is 1-4, R.sup.3 is hydrogen atom or the like, X.sup.1 is single bond or the like, W.sup.2 is alkylene or the like, and R.sup.4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease. ##STR00001##

TYK2 inhibitors and uses thereof

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

TYK2 inhibitors and uses thereof

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

Nitrogen-Containing Heterocyclic Compound, Preparation Method, Intermediate, Pharmaceutical Composition and use
20200062758 · 2020-02-27 ·

Disclosed are a nitrogen-containing heterocyclic compound, preparation method, intermediate, pharmaceutical composition and use. The nitrogen-containing heterocyclic compound of the present invention has a novel structure, relatively high TLR7 agonist activity, high selectivity and good safety.

Nitrogen-Containing Heterocyclic Compound, Preparation Method, Intermediate, Pharmaceutical Composition and use
20200062758 · 2020-02-27 ·

Disclosed are a nitrogen-containing heterocyclic compound, preparation method, intermediate, pharmaceutical composition and use. The nitrogen-containing heterocyclic compound of the present invention has a novel structure, relatively high TLR7 agonist activity, high selectivity and good safety.

Azadecalin derivatives as inhibitors of human immunodeficiency virus replication

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, azadecaline derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: ##STR00001##
These compounds are useful for the treatment of HIV and AIDS.