The University of North Carolina at Chapel Hill

Icagen, Inc.

Ecstasy LLC

The United States of America, as Represented by the Secretary, Department of Health and Human Services

Other

Irm LLC

Meryx, Inc.

Qualcomm Incorporated

The University of Texas System

Astellas Pharma Gmbh

Xiaodong Wang

Weihe Zhang

Brian Edward Marron

Kerry Leigh Spear

Frank Kayser

Xiaoqi Chen

Mark J Suto

Xuelei Yan

Zhihua Ma

David John Kopecky

Zice Fu

Felix Gonzalez Lopez De Turiso

Michael D Bartberger

John Eksterowicz

Jason A Duquette

Julio Cesar Medina

Daqing Sun

Fawad Shaukat

Jeffrey Thomas Mihalic

Ming Yu

Jonathan Dante Low

Yosup Rew

Jiwen Liu

Hilary Plake Beck

Ana Zurisadai Gonzalez Buenrostro

Brian Stuart Lucas

Takeshi Suzuki

Li Liu

Anton Simeonov

Ajit Jadhav

Takahiro Ishii

Richard V Connors

Steven H Olson

Vijayalakshmi Rajasundaram Raveendran

Pingda Ren

Xiaolong Huang

Xiaohui Du

Xiaolin Li

Yun He

Valentina Molteni

Matthew R Kaller

Jef K De Brabander

Paul John Dransfield

Brian M Fox

Vatee Pattaropong

Lin Li

Stephen Frye

Alan Bradley Fulp

Dmitri Kireev

Jing Liu

Darrick Seconi

Jeffrey Deignan

Julie Anne Heath

Andrew Louis McIver

Yingcai Wang

Zhihong Li

Hua M Zhong

Jiasheng Fu

Yihong Li

Xin Huang

Benjamin Fisher

Jiang Zhu

Serge Beaudoin

Min Shen

Matthew Brian Boxer

Kyle Ryan Brimacombe

Jason Matthew Rohde

Mindy Irene Emily Davis

Rajan Pragani

Daniel B Horne

Alan C Cheng

Wen-Chen Yeh

Jon Christopher Loren

Juliet Nabakka

Mikkel V Debenedetto

Darin J Gustin

Zuosheng Liu

Su-Jen Lai

Xiaodong Liu

Kevin Yang

Gayathri Swaminath

Donatella Chianelli

Songchun Jiang

Matthew E Hall

Patrick G Harran

Michael J Schmitt

Yinhong Chen

Aarif Yusuf Khakoo

Taebo Sim

Daniel Jason Urban

Shuli You

Simon J Hedley

Christopher John Markworth

Christopher William West

Ranny Mathew Thomas

Philip M Roveto

Christopher Cow

Shulan Zhou

Malgorzata Wanska

Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

Aryl aminopyrimidines as dual MerTK and TYRO3 inhibitors and methods thereof

The invention relates to new crystal forms of compound (trans)-4-((2-cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl) cyclohexanol trihydrochloride, its hydrate, or solvate, as shown in Formula I. The invention also relates to methods for preparation of the described compound, crystal form, and related intermediate compounds, as well as pharmaceutical compositions containing the compounds. Further described is, the use of the compounds or crystal forms in the production of a medicament for the treatment of a disease, symptom, or condition, or the use in treatment of a disease, symptom or condition.

Polymorphs of a kinase inhibitor, pharmaceutical compositions containing such a compound, preparation methods, and applications

The present invention discloses a number of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

Amines for use as sigma receptor modulators

The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

Polycyclic amines as sigma receptor modulators

Polycyclics as sigma receptor modulators

The present disclosure is concerned with benzo annulene compounds that are capable of inhibiting a Mer tyrosine kinase and/or a Tyro3 tyrosine kinase and methods of treating a bacterial infection, a viral infection, and/or a disorder of uncontrolled cellular proliferation such as, for example, a cancer, using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Alkyl pyrrolopyrimidine analogs and methods of making and using same

A compound of Formula II or a pharmaceutically acceptable salt thereof, wherein CyN is a cyclic amine group bound via a nitrogen atom; X is C or N; Rand Rare each independently a halogen, CN, CF, CHF, CHF, a C-C10alkyl group, a C1-Calkoxy group, a di(C-Calkyl)amino; m and n are each independently 1, 2, or 3, and represents either a single bond or a double bond, wherein the racemic mixture of 3-(4-(4-chlorophenyl)thiazol-2-yl)-1-(2-ethyl-5-methoxyphenyl)-6-(2-methylprop-1-en-1-yl)-5-(piperazine-1-carbonyl)pyridin-2(1H)-one atropisomers is excluded.

Thiazole derivatives useful as mutant IDH1 inhibitors for treating cancer

Compounds of Formula I and Formula II and the pharmaceutically acceptable salts thereof are disclosed The variables A, B, Y, Z, X, X, Rand Rare disclosed herein. The compounds are useful for treating cancer disorders, especially those involving mutant IDH1 enzymes. Pharmaceutical compositions containing compounds of Formula I or Formula II and methods of treatment comprising administering compounds of Formula I and Formula II are also disclosed. 

Mutant IDH1 inhibitors useful for treating cancer

Polycyclic amines as opioid receptor modulators

This invention is in the area of improved therapeutic combinations for and methods of treating selected cancers using selected pyrimidine compounds having pan-TAM or Mer/Axl dual receptor tyrosine kinase inhibitory activity in combination with immune checkpoint inhibitors. In one aspect, an improved treatment for select cancers is disclosed using selected pyrimidine compounds described herein in combination with an immune checkpoint inhibitor, for example, a cytotoxic T-lymphocyte-associated protein 4 (CTLA4) inhibitor, a programmed cell death protein 1 (PD1) inhibitor, or a programmed death-ligand 1 (PDL-1) inhibitor, or combination thereof.

Pan-TAM inhibitors and Mer/Axl dual inhibitors

Compounds of Formula I: wherein: one of X and X' is N and the other of X and X&#x2032; is C, are described, along with compositions containing the same and methods of use thereof in the treatment of cancer.

Pyrrolopyrimidine compounds for the treatment of cancer

Uses of pyrrolopyrimidines with anti-Mer tyrosine kinase activity as anti-infective agents, immunostimulatory and immunomodulatory agents, anti-cancer agents (including against MerTK&#x2212;/&#x2212; tumors and ITD and TKD mutant forms of Acute Myeloid Leukemia (AML)), and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms.

Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity

Compounds of Formula I or II: are described, along with pharmaceutical compositions containing the same and methods of using such compounds for the treatment of cancer.

Pyrimidine compounds for the treatment of cancer

Compound of Formula I: are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.

Pyrazolopyrimidine compounds for the treatment of cancer

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Chapel Hill, NC, United States of America

Xiaodong Wang