Patent classifications
C07D493/08
SUBSTITUTED THIOPHENYL URACILS, SALTS THEREOF AND THE USE THEREOF AS HERBICIDAL AGENTS
The invention relates to substituted thiophenyl uracils of general formula (I)
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or the salts (I) thereof, wherein the groups in general formula (I) are as defined in the description, and to the use thereof as herbicides, in particular for controlling weeds and/or weed grasses in crops of cultivated plants and/or as plant growth regulators for influencing the growth of crops of cultivated plants.
GLS1 INHIBITORS FOR TREATING DISEASE
Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I:
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Methods of inhibition GLS1 activity in a human or animal subject are also provided.
GLS1 INHIBITORS FOR TREATING DISEASE
Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I:
##STR00001##
Methods of inhibition GLS1 activity in a human or animal subject are also provided.
NITROGEN CONTAINING HETEROCYCLES AS CDK12 INHIBITORS
- Koji Ono ,
- Masahiro Ito ,
- Toshio Tanaka ,
- Moriteru Asano ,
- Takaharu Hirayama ,
- Jun Fujimoto ,
- Nobuki Sakauchi ,
- Yasuhiro Hirata ,
- Akinori Toita ,
- Nao Morishita ,
- Hironori Kokubo ,
- Yasuhiro Imaeda ,
- Hironobu Maezaki ,
- Douglas Robert Cary ,
- Ryo Mizojiri ,
- Nobuo Cho ,
- Hiroshi Banno ,
- Hidekazu Tokuhara ,
- Yasuyoshi Arikawa
Provided is a compound that may have a superior CDK12 inhibitory action and is expected to be useful as a prophylactic or therapeutic drug for cancer and the like. A compound represented by the following formula (I):
##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
CROSS-LINKED NUCLEOSIDE AND NUCLEOTIDE USING SAME
A cross-linked nucleoside of the present invention is a compound represented by the formula (I) below. The cross-linked nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid, which has a risk of, for example, accumulation in a specific organ. The cross-linked nucleoside also has excellent industrial productivity.
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CROSS-LINKED NUCLEOSIDE AND NUCLEOTIDE USING SAME
A cross-linked nucleoside of the present invention is a compound represented by the formula (I) below. The cross-linked nucleoside of the present invention is usable as a substitute for a phosphorothioate-modified nucleic acid, which has a risk of, for example, accumulation in a specific organ. The cross-linked nucleoside also has excellent industrial productivity.
##STR00001##
COMPOUNDS
The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X-Y is —NHSO.sub.2— or —SO.sub.2NH—; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, Cl and alkyl; R.sub.4 is selected from H, Cl and F; R.sub.5 is selected from H, alkyl, alkynyl, alkenyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, Cl, F, SO.sub.2-alkyl, SO.sub.2NR.sub.13R.sub.14, optionally substituted heteroaryl and alkyl; R.sub.8 is selected from H, alkyl, haloalkyl and halo; R.sub.9 is H, C.sub.1-C.sub.3-alkyl, or halo; R.sub.10 and R.sub.11, together with the nitrogen to which they are attached, form an azepanyl group, wherein (a) said azepanyl group is substituted by one or more substituents, or (b) one or two carbons in said azepanyl group are replaced by a group selected from O, NH, S and CO, and said azepanyl group is optionally further substituted; or R.sub.10 and R.sub.11, together with the nitrogen to which they are attached, form an azetidinyl, pyrrolidinyl or piperidinyl group wherein (a) said azetidinyl, pyrrolidinyl or piperidinyl group is substituted by one or more substituents, or (b) one or two carbons in said azetidinyl, pyrrolidinyl or piperidinyl group are replaced by a group selected from NH, S and CO; or R.sub.10 and R.sub.11, together with the nitrogen to which they are attached, form an 8, 9 or 10-membered bicyclic heterocycloalkyl group, wherein one or two carbons in the bicyclic heterocycloalkyl ring are optionally replaced by a group selected from O, NH, S and CO, and said bicyclic heterocycloalkyl group is optionally substituted; or R.sub.10 and R.sub.11, together with the nitrogen to which they are attached, form a 6 to 12-membered bicyclic group containing a spirocyclic carbon atom, wherein one or two carbons in the bicyclic group are optionally replaced by a group selected from O, NH, S and CO, and said bicyclic group is optionally substituted, or said bicyclic group is optionally fused to a 5 or 6-membered aryl or heteroaryl group; R.sub.13 and R.sub.14 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.
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MACROLIDE COMPOUND AND ITS USE OF TREATMENT CHRONIC RESPIRATORY DISEASE
Macrolide compound and its use of treatment chronic respiratory disease are provided. Specifically, the macrolide compound is of formula (I) or pharmaceutically acceptable salts, stereoisomers and application thereof are effective in treating chronic respiratory disease.
MACROLIDE COMPOUND AND ITS USE OF TREATMENT CHRONIC RESPIRATORY DISEASE
Macrolide compound and its use of treatment chronic respiratory disease are provided. Specifically, the macrolide compound is of formula (I) or pharmaceutically acceptable salts, stereoisomers and application thereof are effective in treating chronic respiratory disease.
PPARg MODULATORS AND METHODS OF USE
Disclosed herein are novel compounds of Formula (1) and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the same, and methods of using the same.
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