Abstract: The present application provides a VVN001-containing ophthalmic composition comprising an active material selected from a sodium salt represented by formula I and/or a free acid thereof, and ophthalmic excipients, to reduce the ocular inflammatory response by inhibiting a T cell-mediated inflammatory response through the active material. The concentration of the buffering agent in current invention is very low and the final buffer capacity of this ophthalmic composition is very close to the buffering capacity of the tear, which is tear-friendly and comfortable, and to increase the average residence time of the active material of the present application, as well as to increase the bioavailability of the active material represented by formula I according to the present application.

Abstract: The present invention relates to a prodrug containing a JAK inhibitor, a composition, and use thereof. In particular, the present invention relates to a compound represented by formula (II), a pharmaceutical composition containing the compound of the present invention, and use thereof as a JAK inhibitor prodrug in treating inflammatory diseases and tumor-related diseases.

Abstract: The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.

Abstract: An ophthalmic composition for treating non-infectious inflammatory diseases. The ophthalmic composition comprises an active substance and an ophthalmic excipient, wherein the active substance is a JAK inhibitor; and the ophthalmic excipient comprises a pH buffer, an osmotic pressure regulator, a solubilizer, and water for injection. The ophthalmic composition is used for topical eye drop administration, is compatible and stable with eyes, can improve the bioavailability of the active substance in the ophthalmic composition, can be used for treating non-infectious inflammatory diseases, is less invasive, has small side effects, involves a simple production process, and is amenable to large-scale production.

Abstract: The present invention provides a cyano-substituted cyclic hydrazine derivative, comprising: a compound represented by the following structural formula or a stereoisomer, a geometric isomer, a tautomer, a racemate, a hydrate, a solvate, a metabolite and a pharmaceutically acceptable salt or a prodrug thereof The compound is used for prevention, treatment or alleviation of autoimmune diseases or proliferative diseases in patients, and/or for inhibiting or modulating protein kinase activity.

Abstract: The present invention provides a cyano-substituted cyclic hydrazine derivative, comprising: a compound represented by the following structural formula or a stereoisomer, a geometric isomer, a tautomer, a racemate, a hydrate, a solvate, a metabolite and a pharmaceutically acceptable salt or a prodrug thereof. The compound is used for prevention, treatment or alleviation of autoimmune diseases or proliferative diseases in patients, and/or for inhibiting or modulating protein kinase activity.

Abstract: Provided are a crystal form of a compound of formula (I), a method for preparing the crystal form, a pharmaceutical composition containing the crystal form, and the use thereof in the preparation of a drug for treating diseases, disorders or symptoms, or a method thereof for treating diseases, disorders or symptoms.

Abstract: Provided herein is a method of treating, preventing, or ameliorating one or more symptoms of an inflammatory bowel disease with a lymphocyte function-associated antigen-1 antagonist.

Abstract: The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.

Abstract: The invention provides alkyne substituted quinazoline compounds, such as compounds of the formula (I), which are irreversible ErbB kinase inhibitors. The compounds are useful in the treatment of diseases and disorders where ErbB kinase activity is implicated such as a hyperproliferative disorder (e.g., cancer).

Abstract: The present invention provides a cyano-substituted cyclic hydrazine derivative, comprising: a compound represented by the following structural formula or a stereoisomer, a geometric isomer, a tautomer, a racemate, a hydrate, a solvate, a metabolite and a pharmaceutically acceptable salt or a prodrug thereof. The compound is used for prevention, treatment or alleviation of autoimmune diseases or proliferative diseases in patients, and/or for inhibiting or modulating protein kinase activity.

Abstract: A small molecule compound of a NO donor is a compound shown in the following structural formula I or a stereoisomer, a geometric isomer, a tautomer, a racemate, a deuterated isotopic derivative, a hydrate, a solvate, a metabolite, or a pharmaceutically acceptable salt or prodrug thereof; wherein a ring A is a substituted or unsubstituted heteroaromatic ring; X is selected from (CH2); R is a substituent of terminal —O—NO2; R1 is selected from hydrogen, a hydroxyl group, a halogen, an amino group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, or a substituted or unsubstituted heteroalkyl group; R2 and R3 are each independently selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted cycloalkyl group, or an amino protecting group.

Abstract: The present invention provides an anti-inflammatory compound, which is a compound having a structure (I) as shown below: The compound is a target that is important for autoimmune activation, and that has strong inhibitory effect on PDE4 and penetrates the skin easily, and is a new type anti-inflammatory compound that is easily degraded.

Abstract: The present invention provides a phosphorus-containing compound characterized by being a compound represented by the following structure: the compound is a novel immune cell migration inhibitor. The compound has good hydrophilicity and can be developed into eye drops. The compound has a strong inhibitory ability to immune cell migration and can relieve the symptoms of most dry-eye patients.

Abstract: The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.

Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

Abstract: The invention provides alkyne substituted quinazoline compounds, such as compounds of the formula (I), which are irreversible ErbB kinase inhibitors. The compounds are useful in the treatment of diseases and disorders where ErbB kinase activity is implicated such as a hyperproliferative disorder (e.g., cancer).

Abstract: The present invention provides an anti-inflammatory compound, which is a compound having a structure (I) as shown below: The compound is a target that is important for autoimmune activation, and that has strong inhibitory effect on PDE4 and penetrates the skin easily, and is a new type anti-inflammatory compound that is easily degraded.

Abstract: The invention provides lor compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds arc potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.

Abstract: The present invention provides a phosphorus-containing compound characterized by being a compound represented by the following structure: the compound is a novel immune cell migration inhibitor. The compound has good hydrophilicity and can be developed into eye drops. The compound has a strong inhibitory ability to immune cell migration and can relieve the symptoms of most dry-eye patients.