C07D211/40

Method for synthesizing key intermediate of apixaban

The invention relates to a method for synthesizing an intermediate of Apixaban comprising reacting a compound of formula I with 5-chloro-valeryl chloride in the presence of inorganic base in an inert solvent to obtain a compound of formula II, with the reaction formula of (A), wherein R is selected from nitro group and the group (B). The method is mild in reaction condition, simple in operation, easy in purification, inexpensive in production cost, environmental-friendly, and suitable for industrial production. ##STR00001##

Inhibitors of atypical protein kinase C and their use in treating hedgehog pathway-dependent cancers

Methods and compositions are provided for modulating Hedgehog (Hh) pathway signaling in a cell. Aspects of the methods include methods for inhibiting Hh pathway-promoted cancer proliferation and/or metastasis that is promoted by Hh pathway signaling, methods for treating cancers promoted by Hh pathway signaling, and methods for screening candidate agents for the ability to treat a cancer promoted by Hh pathway signaling. In addition, reagents and kits thereof that find use in practicing the subject methods are provided.

Inhibitors of atypical protein kinase C and their use in treating hedgehog pathway-dependent cancers

Methods and compositions are provided for modulating Hedgehog (Hh) pathway signaling in a cell. Aspects of the methods include methods for inhibiting Hh pathway-promoted cancer proliferation and/or metastasis that is promoted by Hh pathway signaling, methods for treating cancers promoted by Hh pathway signaling, and methods for screening candidate agents for the ability to treat a cancer promoted by Hh pathway signaling. In addition, reagents and kits thereof that find use in practicing the subject methods are provided.

Solenopsin and derivatives, therapeutic compositions; and methods related thereto

This disclosure relates to solenopsin derivatives, pharmaceutical compositions, and therapeutic uses related thereto. In certain embodiments, the disclosure relates to compounds of the following formula: ##STR00001## or salts, esters or prodrugs thereof as described herein.

Solenopsin and derivatives, therapeutic compositions; and methods related thereto

This disclosure relates to solenopsin derivatives, pharmaceutical compositions, and therapeutic uses related thereto. In certain embodiments, the disclosure relates to compounds of the following formula: ##STR00001## or salts, esters or prodrugs thereof as described herein.

Targeted degradation of VAV1

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof) that degrades Proto-oncogene VAV 1 protein (VAV1). The chemical entities are useful, e.g., for treating a subject (e.g., a human subject) having an inflammatory or autoimmune disorder.

STAT3 inhibitor

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.

STAT3 inhibitor

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.

ANTI-INFLAMMATORY AND ANALGESIC COMPOUNDS AND USE THEREOF

It belongs to the field of medicinal chemistry, in particular discloses anti-inflammatory and analgesic compounds and use thereof, the compounds of the present invention are compounds, isomers or pharmaceutically acceptable salts as shown in formula (I) or formula (II); the compounds have significant curative effect on gouty arthritis in rats, and have excellent anti-inflammatory factor effect; therefore, the compounds have potential application prospects in anti-inflammatory and analgesic drugs, especially in anti-acute gouty arthritis drugs, anti-rheumatoid arthritis drugs, drugs to reduce inflammatory factors, drugs to treat inflammatory storm or coronavirus pneumonia.

ANTI-INFLAMMATORY AND ANALGESIC COMPOUNDS AND USE THEREOF

It belongs to the field of medicinal chemistry, in particular discloses anti-inflammatory and analgesic compounds and use thereof, the compounds of the present invention are compounds, isomers or pharmaceutically acceptable salts as shown in formula (I) or formula (II); the compounds have significant curative effect on gouty arthritis in rats, and have excellent anti-inflammatory factor effect; therefore, the compounds have potential application prospects in anti-inflammatory and analgesic drugs, especially in anti-acute gouty arthritis drugs, anti-rheumatoid arthritis drugs, drugs to reduce inflammatory factors, drugs to treat inflammatory storm or coronavirus pneumonia.