Pfizer Corporation

University of Texas System

Curtana Pharmaceuticals, Inc.

Southwest Research Institute

Other

Pfizer Products Inc.

Stanton F McHardy

Bismarck Campos

Jotham Wadsworth Coe

Graham Beaton

Hua-Yu Leo Wang

Ambrosio Lopez, Jr

Michael Wade Tidwell

Donald M Maxwell

Richard Michael Corbett

Christopher J Bemben

John Adams Lowe, Iii

Spiros Liras

Stanley J Watowich

Cara B Gonzales

Hua-Yu Wang

Harshini Neelakantan

Fabio C Tucci

Douglas Philip Hanson

John Anthony Ragan

Derek Lawrence Tickner

Satheesh Babu Ravula

Brian C Vanderplas

Francisco Xavier Ruiz

Michael Girard Vetelino

Somshuvra Mukhopadhyay

Bryan William Davies

Steven D Heck

Hua-yu Wang

Ashley Cunningham

Crystal G Bashore

Andrey S Selyunin

Waldemar Gorski

Travis Menard

Andrew Fleischman

The present disclosure relates generally to derivatives of capsazepine and methods of use thereof. In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases.

Capsazepine analogs for the treatment of cancer and other proliferative diseases

Described herein are compounds and pharmaceutical compositions of phenyl-pyrimidinyl-urea derivatives, which inhibit the activity of Olig2. An example of a phenyl-pyrimidinyl-urea derivative has the following structure: Also described herein are methods using the Olig2 inhibitors for treating cancer and other diseases. The Olig2 inhibitors may be used to treat glioblastoma.

Inhibition of Olig2 activity

The present invention relates to quinoline derived small molecule inhibitors of nicotinamide N-methyltransferase (NNMT), the preparation thereof and uses thereof.

Quinoline derived small molecule inhibitors of nicotinamide N-methyltransferase (NNMT) and uses thereof

The present disclosure provides ammonium compounds, e.g., compounds according to Formula I as set forth herein, which are useful as antimicrobial agents. Methods for the treatment of bacterial infections and associated conditions, e.g., gastrointestinal conditions, are also described, as well as methods for altering the microbiome of subjects such as humans.

Antibiotic ammonium compounds and methods for the treatment of bacterial infections

Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Olig2 inhibitors may be used to treat glioblastoma.

Certain embodiments are directed hydrophilic redox substrates for leukocyte esterase (LE). In certain aspects a hydrophilic redox leukocyte esterase substrate or a small molecule enzyme substrate for use in methods and/or devices to electrochemically detect and/or measure LE activity in a sample.

Redox substrates for leukocyte esterase

The present invention relates to quinoline derived small molecule inhibitors of nicotinamide N-methyltransferase (NNMT), the preparation thereof and uses thereof. Formula (I). 

Methods for treating Shiga toxicosis, caused by infection with Shiga toxin bacteria, are provided. The methods include administering to a subject in need thereof an effective amount of one or more active agents selected from tamoxifen, 4-hydroxytamoxifen, endoxifen, toremifene, raloxifene, bazedoxifene, and pharmaceutically acceptable salts thereof. In some embodiments, the methods further include the administration of an antibiotic or a manganese compound to the subject. Pharmaceutical compositions for the treatment of Shiga toxicosis are also described.

Methods and compositions for the treatment of Shiga Toxicosis

Described herein are urea compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Olig2 inhibitors may be used to treat glioblastoma.

Inhibition of OLIG2 activity

The present disclosure relates generally to derivatives of capsazepine and methods of use thereof In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. In some aspects of the present disclosure, the disclosure provides capsazepine derivatives which may be useful in the treatment of cancer. Such cancers that the compounds may be used to treating include but are not limited to breast, cervical, oral, head, neck, or prostate cancer. In some aspects, the compounds may be useful in treating a tumor by direct injection of the compound into the tumor, particularly an oral tumor. In other aspects, the compounds are administered systemically. The compounds of the present disclosure may also be used to treat the pain associated with a tumor for which it is being administered.

The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.

Oximes for treatment of peripheral and central nervous system exposure to acetyl cholinesterase inhibitors

The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R-Rgroups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Bicyclic [3.1.0] heteroaryl amides as type 1 glycine transport inhibitors

Growing community of inventors

San Antonio, TX, United States of America

Stanton F McHardy