C07D473/28

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.

CRYSTALLINE FORM OF GNRH RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR
20190276455 · 2019-09-12 ·

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.

CRYSTALLINE FORM OF GNRH RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR
20190276455 · 2019-09-12 ·

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.

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.

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.

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##

Preparation and use of kinase inhibitor

Disclosed are a preparation method for a kinase inhibitor and a use thereof. The kinase inhibitor is a compound represented by formula (I) wherein the groups are defined as described in the description. The compound of formula (I) has a kinase inhibitory activity and therefore can be used for the preparation of medicines for treating kinase activity-related diseases. ##STR00001##

Preparation and use of kinase inhibitor

Disclosed are a preparation method for a kinase inhibitor and a use thereof. The kinase inhibitor is a compound represented by formula (I) wherein the groups are defined as described in the description. The compound of formula (I) has a kinase inhibitory activity and therefore can be used for the preparation of medicines for treating kinase activity-related diseases. ##STR00001##