The present invention relates to novel coumarin glyoxylates, a process for their preparation and their use as photoinitiators in photopolymerization compositions. The invention also concerns a process for the photopolymerization of compositions comprising said coumarin glyoxylates.

A method of increasing the self-renewal and/or expansion of hematopoietic stem and/or progenitor cells (HSPCs) is described. Inhibiting the activity and/or expression of cytochrome P450 1B1 (CYP1B1) and/or increasing the expression or activity of Musashi-2 (MSI2) increases the expansion of HSPCs. The HSPCs may be cultured in the presence of a CYP1B1 inhibitor and/or a MSI2 activator. Optionally, the cells may be expanded ex vivo and transplanted into a subject in need thereof.

A method of increasing the self-renewal and/or expansion of hematopoietic stem and/or progenitor cells (HSPCs) is described. Inhibiting the activity and/or expression of cytochrome P450 1B1 (CYP1B1) and/or increasing the expression or activity of Musashi-2 (MSI2) increases the expansion of HSPCs. The HSPCs may be cultured in the presence of a CYP1B1 inhibitor and/or a MSI2 activator. Optionally, the cells may be expanded ex vivo and transplanted into a subject in need thereof.

Disclosed are XBP-1/IRE-1 inhibitors having formula disclosed herein. Methods of making and using these inhibitors for the treatment of cancer, in particular B cell cancers, are also disclosed. Also disclosed is a genetic XBP-1-knockout cancer mouse model. In still further aspects, the disclosed subject matter relates to methods for treating oncological and inflammatory disorders in a patient. For example, disclosed herein are methods whereby an effective amount of a compound or composition disclosed herein is administered to a patient having an oncological disorder, for example B-cell chronic lymphocytic leukemia (CLL), and who is in need of treatment thereof. XBP-1 deficiency causes leukemic cells to acquire phenotypes that are disadvantageous for their survival, such as compromised BCR signaling capability and increased surface expression of S1P1.

Disclosed are XBP-1/IRE-1 inhibitors having formula disclosed herein. Methods of making and using these inhibitors for the treatment of cancer, in particular B cell cancers, are also disclosed. Also disclosed is a genetic XBP-1-knockout cancer mouse model. In still further aspects, the disclosed subject matter relates to methods for treating oncological and inflammatory disorders in a patient. For example, disclosed herein are methods whereby an effective amount of a compound or composition disclosed herein is administered to a patient having an oncological disorder, for example B-cell chronic lymphocytic leukemia (CLL), and who is in need of treatment thereof. XBP-1 deficiency causes leukemic cells to acquire phenotypes that are disadvantageous for their survival, such as compromised BCR signaling capability and increased surface expression of S1P1.

Disclosed herein are compounds having antiviral activity, and, in particular, an inhibitory activity on the replication of Respiratory Syncytial Virus (RSV). Druggable target sites, including Px, in the RSV N protein are disclosed, as well as compounds targeting Px. The compounds can be used to treat patients with RSV infection.

Disclosed herein are compounds having antiviral activity, and, in particular, an inhibitory activity on the replication of Respiratory Syncytial Virus (RSV). Druggable target sites, including Px, in the RSV N protein are disclosed, as well as compounds targeting Px. The compounds can be used to treat patients with RSV infection.

The present invention discloses the novel coumarin derivative of formula (1): ##STR00001##
its synthesis, pharmaceutical composition, preparation and use thereof. The pharmaceutical composition including: (1) the novel coumarin derivative of formula (1) as active pharmaceutical ingredient; and (2) one or more pharmaceutical excipients, required to yield final dosage forms suitable for therapeutic administration. The composition is safe and efficient therapeutic agent for viral diseases including the acquired immunodeficiency syndrome (AIDS).

The present invention discloses the novel coumarin derivative of formula (1): ##STR00001##
its synthesis, pharmaceutical composition, preparation and use thereof. The pharmaceutical composition including: (1) the novel coumarin derivative of formula (1) as active pharmaceutical ingredient; and (2) one or more pharmaceutical excipients, required to yield final dosage forms suitable for therapeutic administration. The composition is safe and efficient therapeutic agent for viral diseases including the acquired immunodeficiency syndrome (AIDS).

The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.