New pyrimidine derivatives together with a membrane penetrating agent, optionally with a detectable isotope and pharmaceutical composition for use in treatment or prevention of Gram-negative bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of Gram-negative biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. New pyrimidine derivatives together with a membrane penetrating agent; for use as radiotracer in diagnosing or prognosing Gram-negative bacterial infection in a host mammal.

The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.

The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.

The present invention provides a 6-dithio-substituted-2′-deoxyguanosine compound and a preparation method thereof and use thereof in anti-tumor drugs. According to the present invention, a series of brand-new thioredoxin-1 (Trx-1) inhibitors are designed and synthesized by using 2′-deoxyguanosine as a structure mother nucleus. The compound according to the present invention is a structure of formula I, and Trx-1 activity inhibition testing is performed on the type of compounds, showing apparent inhibitory activity. It is indicated from in vitro and vivo researches that these compounds show significant anti-tumor effects on multiple types of tumors, can be applied to drugs for tumors related to human body cell proliferation, and provide a new path for the research of anticancer drugs.

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The present invention provides a 6-dithio-substituted-2′-deoxyguanosine compound and a preparation method thereof and use thereof in anti-tumor drugs. According to the present invention, a series of brand-new thioredoxin-1 (Trx-1) inhibitors are designed and synthesized by using 2′-deoxyguanosine as a structure mother nucleus. The compound according to the present invention is a structure of formula I, and Trx-1 activity inhibition testing is performed on the type of compounds, showing apparent inhibitory activity. It is indicated from in vitro and vivo researches that these compounds show significant anti-tumor effects on multiple types of tumors, can be applied to drugs for tumors related to human body cell proliferation, and provide a new path for the research of anticancer drugs.

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Substituted indazoles linked to a substituted adenine with a polyethylene glycol moiety selectively bind to Hsp90. The compounds include detection moieties such as fluorophores and are useful in methods and kits for selective detection of Hsp90 in a sample. ##STR00001##

Substituted indazoles linked to a substituted adenine with a polyethylene glycol moiety selectively bind to Hsp90. The compounds include detection moieties such as fluorophores and are useful in methods and kits for selective detection of Hsp90 in a sample. ##STR00001##

Pyrimidine derivatives of formula (I):

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optionally with a detectable isotope, pharmaceutical composition and method of preparation thereof. Pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. Pyrimidine derivatives for use as radiotracer in diagnosing or prognosing bacterial infection in a host mammal.

The present invention provides compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.

The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example an addiction or compulsive disorder.