University of Illinois

Janssen Pharmaceutica Nv

Scott E Denmark

Lieven Meerpoel

Tongfei Wu

Vineet Pande

Johannes Wilhelmus John F Thuring

Weimei Sun

Jonas Verhoeven

Guido Alfons F Verniest

Dirk Brehmer

Matthew B Wheeler

Marcello Rubessa

Malek Y S Ibrahim

Zhigang Wang

Weitao Pan

Ramzi F Sweis

Shyh-Ming Yang

Yang Wang

Brennan T Rose

Jeremy J Henle

Andrew F Zahrt

William T Darrow

Dianelys Gonzalez-Pena

Jun Young Choi

Andrea Ambrosi

Daniel Wehrli

Zhicai Wu

Luc Neuville

The present invention relates to novel spirobicyclic analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Spirobicyclic analogues

The present disclosure provides non-invasive methods for determining the gender of an embryo during in vitro embryo culture.

Non-invasive analysis of embryo metabolites

Catalyst design in asymmetric reaction development has traditionally been driven by empiricism, wherein experimentalists attempt to qualitatively recognize structural patterns to improve selectivity. Machine learning algorithms and chemoinformatics can potentially accelerate this process by recognizing otherwise inscrutable patterns in large datasets. Herein we report a computationally guided workflow for chiral catalyst selection using chemoinformatics at every stage of development. Robust molecular descriptors that are agnostic to the catalyst scaffold allow for selection of a universal training set on the basis of steric and electronic properties. This set can be used to train machine learning methods to make highly accurate predictive models over a broad range of selectivity space. Using support vector machines and deep feed-forward neural networks, we demonstrate accurate predictive modeling in the chiral phosphoric acid-catalyzed thiol addition to N-acylimines.

Extrapolative prediction of enantioselectivity enabled by computer-driven workflow, new molecular representations and machine learning

Disclosed herein is a method for extracting precious metals from supported catalysts. The precious metal in one embodiment is rhodium. The supported catalyst may be from equipment, such as a used catalytic converter. The method is carried out at low temperature, and does not require harsh conditions, such as the use of a strong acid. The method involves contacting the catalytic material with a polar molecule and a reactive gas.

Extraction of selected platinum-group metals from supported catalyst

The present invention relates to novel spirobicyclic analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament. 

Improved methods for generating a &#x2014;C&#x2014;C&#x2014; bond by cross-coupling of a transferable group with an acceptor group. The transferable group is a substituent of an organosilicon nucleophile and the acceptor group is provided as an organic electrophile. The reaction is catalyzed by a Group 10 transition metal complex (e.g., Ni, Pt or Pd), particularly by a palladium complex. Certain methods of this invention use improved organosilicon nucleophiles which are readily prepared, can give high product yields and exhibit high stereoselectivity. Methods of this invention employ activating ions such as halides, hydroxide, hydride and silyloxides. In specific embodiments, organosilicon nucleophilic reagents of this invention include siloxanes, particularly cyclic siloxanes. The combination of the cross-coupling reactions of this invention with ring-closing metathesis, hydrosilylation and intramolecular hydrosilylation reactions provide useful synthetic strategies that have wide application.

Cross-coupling reaction of organosilicon nucleophiles

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Champaign, IL, United States of America

Scott E Denmark