Amgen Inc.

Abbott Laboratories Corporation

F.i.s. Fabbrica Italiana Sintetici S.p.a.

Jason S Tedrow

Robert Ronald Milburn

Rodger F Henry

Jianzhang Mei

Steven Mennen

Sean M Mellican

John T Colyer

Cathie L Linton

Nahathai Charukamnoetkanok

Stephan D Parent

Gary T Wang

Anil Vasudevan

George S Sheppard

David M Barnes

Robert A Mantei

Megumi Kawai

Jieyi Wang

Lawrence Kolaczkowski

Jack Henkin

Douglas M Kalvin

Sheng Cui

Liang Huang

Simon J Hedley

Henry Morrison

Matthew Bio

William Sanders

Yuanqing Fang

Babak Riahi

Steve D Fidanze

Scott A Erickson

Eric A Bercot

Neil Fred Langille

Beatriz Dominguez

Nwe Y BaMaung

Philipp C Roosen

Austin G Smith

Alan H Cherney

Matthew G Beaver

Oliver Thiel

Amin Bornadel

Travis Houston

Serena Bisagni

Jacques Lepaih

Ahir Pushpanath

Iustina Slabu

Kenneth M Comess

Ki H Kim

Chang Hoon Park

David C Park

Johann Chan

Kyle D Baucom

Gabrielle St-pierre

Jonathan Vinh-Phu Truong

Alessandro Arena

Rahul P Sangodkar

Michael A Lovette

Ari Ericson

Melanie Bevill

Courtney Johnson

A method for reducing a substrate selected from 2-methyl-5-nitropyridine and methyl 4-(2-fluoro-3-nitrobenzyl)piperazine-1-carboxylate is provided catalysed by a nitroreductase and a disproportionation agent.

Method of reducing aromatic nitro compounds

Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound F that can be used to prepare them where the variable PG is as defined herein. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof.

Ring closing synthesis of macrocyclic MCL-1 inhibitor intermediates

Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound Z that can be used to prepare them. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof.

Synthesis of sulfonamide intermediates

Disclosed herein are salt and solvate forms of. (1S,3'R,6′R,7′S,8′E,11′S,12′R)-6-chloro-7′-methoxy-11′,12′-dimethyl-3,4-dihydro-2H,15′H-spiro[naphthalene-1,22′-[20]oxa[13]thia[1,14]diazatetracyclo[14.7.2.00]pentacosa[8,16,18,24]tetraen]-15′-one 13′,13′-dioxide (AMG 176): such as crystalline salt and solvate forms thereof. Also disclosed are methods of making the salt and solvate forms, and methods of treating diseases and disorders with the salt and solvate forms.

Salt forms and solvates of Mcl-1 antagonists

The present invention relates to processes for preparing protected glyceraldehydes, such as (hydroxy)methanesulfonates. In addition, the invention relates to thiadiazoles, particularly 3-diooxolanyl-thiadiazoles.

Method for the preparation of thiadiazoles

A crystalline N-(4-(4-aminothieno[2,3 -d]pyrimidin-5-yl)phenyl)-N'-(2-fluoro-5-(trifluoromethyl)phenyl)urea ethanolate characterized in the monoclinic crystal system and P2/n space group, when measured with radiation at 0.7107 &#x212b;, by lattice parameters a, b and c of 5.0318 &#x212b;&#xb1;0.006 &#x212b;, 23.684 &#x212b;&#xb1;0.002 &#x212b; and 18.877 &#x212b;&#xb1;0.002 &#x212b;, respectively, and &#x3b2; of 90.703&#xb1;0.003, ways to make it, compositions comprising it, and methods of treatment using it are disclosed.

Crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N'-(2-fluoro-5-(trifluoromethyl)phenyl)urea ethanolate

A crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N'-(2-fluoro-5-(trifluoromethyl)phenyl)urea benzenesulfonate characterized in the triclinic crystal system and P-1 space group, when measured with radiation at 0.7107 &#x212b;, by lattice parameters a, b and c of 7.800 &#x212b;&#xb1;0.001 &#x212b;, 13.406 &#x212b;&#xb1;0.002 &#x212b; and 13.554 &#x212b;&#xb1;0.002 &#x212b;, respectively and &#x3b1;, &#x3b2; and &#x3b3; of 67.155&#xb1;0.002, 79.724&#xb0;&#xb1;0.002&#xb0; and 84.067&#xb1;0.002, respectively, ways to make it, compositions comprising it, and methods of treatment using it are disclosed.

Crystalline N-(4-(4-ammoniumthieno[2,3-d]pyrimidin-5-yl)phenyl)-N'-(2-fluoro-5-(trifluoromethyl)phenyl)urea benzenesulfonate

Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

Sulfonamides having antiangiogenic and anticancer activity

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Evanston, IL, United States of America

Jason S Tedrow