C07D239/91

CRYSTALLINE FORMS OF QUINAZOLINONE COMPOUND AND PROCESS FOR PREPARING THE SAME

Provided are a crystal form D, a crystal form AJ, a crystal form AL, a crystal form AZ, a crystal form AF, a crystal form Z and a crystal form AE of a compound of formula (I), a process for preparing the same and the use thereof. The crystal forms have advantages in at least one aspect of solubility, melting point, stability, dissolution, hygroscopicity, adhesiveness, fluidity, biological effectiveness, processability, purification effect, preparation production, safety, etc., thus providing a new better choice for the preparation of pharmaceutical preparations containing the compound of formula (I), and having important significance for drug development.

CRYSTALLINE FORMS OF QUINAZOLINONE COMPOUND AND PROCESS FOR PREPARING THE SAME

Provided are a crystal form D, a crystal form AJ, a crystal form AL, a crystal form AZ, a crystal form AF, a crystal form Z and a crystal form AE of a compound of formula (I), a process for preparing the same and the use thereof. The crystal forms have advantages in at least one aspect of solubility, melting point, stability, dissolution, hygroscopicity, adhesiveness, fluidity, biological effectiveness, processability, purification effect, preparation production, safety, etc., thus providing a new better choice for the preparation of pharmaceutical preparations containing the compound of formula (I), and having important significance for drug development.

Tert-butyl (s)-(1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)propyl)carbamate precursor of a quinazolinone inhibitor of human phosphatidylinositol 3-kinase delta and a process for preparing thereof

Compounds that inhibit PI3K activity, including compounds that selectively inhibit PI3K activity, are disclosed. Methods of preparing such compounds are also disclosed, including the preparation and use of the compound tert-butyl (S)-(1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)propyl)carbamate of formula (110) as a precursor to synthesize an exemplary compound disclosed in this application, (S)-2-(1-((9H-purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K plays a role in leukocyte function, using the compounds also are disclosed. ##STR00001##

Tert-butyl (s)-(1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)propyl)carbamate precursor of a quinazolinone inhibitor of human phosphatidylinositol 3-kinase delta and a process for preparing thereof

Compounds that inhibit PI3K activity, including compounds that selectively inhibit PI3K activity, are disclosed. Methods of preparing such compounds are also disclosed, including the preparation and use of the compound tert-butyl (S)-(1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)propyl)carbamate of formula (110) as a precursor to synthesize an exemplary compound disclosed in this application, (S)-2-(1-((9H-purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K plays a role in leukocyte function, using the compounds also are disclosed. ##STR00001##

Quinolinone or quinazolinone comprising antibiofilm compositions, compounds and methods and uses relating thereto

An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): ##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2): ##STR00002##

Quinolinone or quinazolinone comprising antibiofilm compositions, compounds and methods and uses relating thereto

An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): ##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2): ##STR00002##

Anti-inflammatory agents
10882828 · 2021-01-05 · ·

Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.

Anti-inflammatory agents
10882828 · 2021-01-05 · ·

Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.

COMPOUNDS FOR THE TREATMENT OF BRAF-ASSOCIATED DISEASES AND DISORDERS

Provided herein are compounds of the Formula I:

##STR00001##

and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.

COMPOUNDS FOR THE TREATMENT OF BRAF-ASSOCIATED DISEASES AND DISORDERS

Provided herein are compounds of the Formula I:

##STR00001##

and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.