Patent classifications
C07D237/32
RADIOHALIDE-LABELED TARGETED DIAGNOSTICS AND THERAPEUTICS
Disclosed are chemical entities of formula (I) wherein R.sub.1, R.sub.2 and n are defined herein, and methods of use thereof. These chemical entities are radiative emitters and are useful, e.g., as therapeutic agents for the treatment of, or as diagnostic (e.g., imaging) agents for cancers, e.g., cancers in which PARP1 is overexpressed.
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RADIOHALIDE-LABELED TARGETED DIAGNOSTICS AND THERAPEUTICS
Disclosed are chemical entities of formula (I) wherein R.sub.1, R.sub.2 and n are defined herein, and methods of use thereof. These chemical entities are radiative emitters and are useful, e.g., as therapeutic agents for the treatment of, or as diagnostic (e.g., imaging) agents for cancers, e.g., cancers in which PARP1 is overexpressed.
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PHTHALAZINONE COMPOUNDS AND USE THEREOF
Provided is a phthalazinone compound, or a racemate, steroisomer or pharmaceutically acceptable salt thereof; a pharmaceutical composition for the prevention or treatment of Sirt6-associated diseases, including as an active ingredient, a phthalazinone compound, or a racemate, steroisomer or pharmaceutically acceptable salt thereof; and a method for treating Sirt6-associated diseases including administering a phthalazinone compound, or a racemate, steroisomer or pharmaceutically acceptable salt thereof to a subject in need.
PHTHALAZINONE COMPOUNDS AND USE THEREOF
Provided is a phthalazinone compound, or a racemate, steroisomer or pharmaceutically acceptable salt thereof; a pharmaceutical composition for the prevention or treatment of Sirt6-associated diseases, including as an active ingredient, a phthalazinone compound, or a racemate, steroisomer or pharmaceutically acceptable salt thereof; and a method for treating Sirt6-associated diseases including administering a phthalazinone compound, or a racemate, steroisomer or pharmaceutically acceptable salt thereof to a subject in need.
Methhod for producing a crystalline form of 5-amino-2,3-dihydrophthalazine-1,4-dione
A new method for producing a crystalline form of 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) is provided. Advantageous uses for this crystalline form as a detecting agent or as an agent for forensic purposes are disclosed, as well a pharmaceutical composition containing said crystalline form.
Methhod for producing a crystalline form of 5-amino-2,3-dihydrophthalazine-1,4-dione
A new method for producing a crystalline form of 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) is provided. Advantageous uses for this crystalline form as a detecting agent or as an agent for forensic purposes are disclosed, as well a pharmaceutical composition containing said crystalline form.
PARP-1 and methods of use thereof
The invention is directed to roles for PARP-1 in disease.
Pyridinones and isoquinolinones as inhibitors of the bromodomain BRD9
The present invention encompasses compounds of general formula (I) wherein the groups R.sup.1 to R.sup.9, X.sub.1 and X.sub.2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament. ##STR00001##
Pyridinones and isoquinolinones as inhibitors of the bromodomain BRD9
The present invention encompasses compounds of general formula (I) wherein the groups R.sup.1 to R.sup.9, X.sub.1 and X.sub.2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament. ##STR00001##
TARGET PROTEIN DEGRADATION COMPOUNDS, THEIR ANTI-TUMOR USE, THEIR INTERMEDIATES AND USE OF INTERMEDIATES
The present disclosure relates to compounds of formula (I) and their anti-tumor uses, and their intermediates of formula (III), intermediates of formula (IV), and uses of the intermediates. The compound of formula (I) has a degrading effect on a specific target protein, which is mainly composed of three parts. The first part is a small molecule compound (SMBP, Small Molecules Binding Protein) that can bind to a protein, the second part LIN is a linker, and the three-part ULM is a ubiquitin ligand (ULM, Ubiquitin Ligase Binding Moiety), wherein SMBP is covalently bound to LIN, and LIN is covalently bound to ULM. A series of compounds designed and synthesized in the present disclosure have a wide range of pharmacological activities, including the functions of degrading specific proteins and/or inhibiting activities of specific proteins, and thus can be used in related tumor treatments.
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