Scientist-turned-entrepreneur Bob Gadwood of Kalexsyn is the next speaker in the WMU Entrepreneurship Forum series
By Al Jones | ajones5@mlive.com
on October 31, 2012 at 5:25 PM, updated October 31, 2012 at 5:26 PM
KALAMAZOO, MI — Entrepreneurshipwas probably not the top thing on the minds of Kalamazoo-based scientists after Pfizer Inc. completed its buy-out of Pharmacia Corp. in 2003 and started to eliminate a lot of the research work done here.
But Bob Gadwood was among several Pharmacia/Pfizer scientists who enjoyed the work they did here, enjoyed living here and decided to take their skill sets and become entrepreneurs.
He became co-founder, president and chief scientific officer of Kalexsyn Inc., a contract research laboratory that specializes in solving chemistry problems for pharmaceutical and biotech companies.It is now considered one of the area’s emerging life-sciences companies.
On Friday, Nov. 9, Gadwood will explain his transition into entrepreneurship when he addresses the Haworth College of Business Entrepreneurship Forum at Western Michigan University.
As associate director of medicinal chemistry at Pharmacia, Gadwood supervised a staff of 19 chemists, and worked on multiple projects involving infectious diseases and central nervous system therapeutic areas. But in 2003, he and former Pharmacia executive David Zimmerman started Kalexsyn.
Among other things, it prepares new compounds for pharmaceutical companies and helps assess their safety and efficacy. Located at Western Michigan University’s Business Research and Technology Park, it is currently involved in research to find new medicines for use in therapeutic areas such as infectious diseases, cancer and diabetes.
Gadwood’s presentation is scheduled for 8 a.m. on Nov. 9, in Room 2159 of Schneider Hall, which is the home of the Haworth College of Business. The event is free and open to the public, but reservations are required by calling 269-387-6059. The event begins with a continental breakfast at 7:30 a.m.
Gadwood joined Upjohn in 1986 and remained with the company until the Pfizer acquisition in 2003. He has a bachelor’s degree from Marquette University (1974) and a doctorate from the University of Wisconsin (1978). He has 42 publications and 18 patents to his credit.
Kalexsyn has grown to have a staff of 37 employees and a customer base that includes small and large companies in the United States, Europe and Asia. Gadwood and his company were named Ernst and Young Entrepreneur of the Year in 2010 and Best Small Business of the Year in 2004 by the Michigan Small Business and Technology Development Center.
Discovery and Optimization of Chromenotriazolopyrimidines as Potent Inhibitors of the Mouse Double Minute 2-Tumor Protein 53 Protein-Protein Interaction
John G. Allen,*,† Matthew P. Bourbeau,† G. Erich Wohlhieter,† Michael D. Bartberger,† Klaus Michelsen,† Randall Hungate,† Robert C. Gadwood,‡ Rick D. Gaston,‡ Bruce Evans,‡ Larry W. Mann,‡, Michael E. Matison,‡ Stephen Schneider,§ Xin Huang,§ Dongyin Yu,§ Paul S. Andrews,§ Andreas Reichelt,† Alexander M. Long,§ Peter Yakowec,§ Evelyn Y. Yang,^ Tani Ann Lee, and Jonathan D. Oliner
†Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, ‡Kalexsyn Inc. 4502 Campus Drive, Kalamazoo, Michigan 49008, §Chemistry Research and Discovery, Amgen, Inc., One Kendall Square, Cambridge Massachusetts 02139, ^Protein Science, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, and ) Oncology Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320. z Current address: Pfizer Animal Health, 333 Portage Street, Kalamazoo, Michigan, 49007. 3 Current address: Prometheus Laboratories, Inc., San Diego, CA, 92121.
Abstract
Tumor protein 53 (p53) is a critical regulator of cell cycle and apoptosis that is frequently disabled in human tumors. In many tumor types, p53 is deleted or mutated, but in others p53 is inactivated by overexpression or amplification of its negative regulator mouse double minute 2 (MDM2). A highthroughput screening effort identified 6,7-bis(4-bromophenyl)-7,12-dihydro-6H-chromeno[4,3-d]- [1,2,4]triazolo[1,5-a]pyrimidine as a potent inhibitor of the MDM2-p53 protein-protein interaction. This screening hit was found to be chemically unstable and difficult to handle due to poor DMSO solubility. Co-crystallization with the target protein helped to direct further optimization and provided a tractable lead series of novelMDM2-p53 inhibitors. In cellular assays, these compounds were shown to upregulate p53 protein levels and p53 signaling and to cause p53-dependent inhibition of proliferation and apoptosis.’
TPGS-750-M: A Second-Generation Amphiphile for Metal-Catalyzed Cross-Couplings in Water at Room Temperature
Bruce H. Lipshutz,* Subir Ghorai, Alexander R. Abela, Ralph Moser, Takashi Nishikata, Christophe Duplais, and Arkady Krasovskiy
Department of Chemistry and Biochemistry, University of California, Santa Barbara, California 93106, United States
Ricky D. Gaston and Robert C. Gadwood*
Kalexsyn, Inc., 4502 Campus Drive, Kalamazoo, Michigan 49008, United States
ABSTRACT: An environmentally benign surfactant (TPGS-750-M), a diester composed of racemic R-tocopherol, MPEG- 750, and succinic acid, has been designed and readily prepared as an effective nanomicelle-forming species for general use in metal-catalyzed cross-coupling reactions in water. Several “name” reactions, including Heck, Suzuki-Miyaura, Sonogashira, and Negishi-like couplings, have been studied using this technology, as have aminations, C-H activations, and olefin metathesis reactions. Physical data in the form of DLS and cryo-TEM measurements suggest that particle size and shape are key elements in achieving high levels of conversion and, hence, good isolated yields of products. This new amphiphile will soon be commercially available.
Practical Synthesis of 3-Oxa-6-azabicyclo[3.1.1]heptane Hydrotosylate; a Novel Morpholine-Based Building Block
Synthesis 2012, 44, 2859
Abstract
Bridged bicyclic morpholines are important building blocks in medicinal chemistry research. The bicyclic morpholine 3-oxa-6-azabicylo[3.1.1]heptane (3a) is of particular interest as a morpholine isostere because it is achiral and shows similar lipophilicity to that of morpholine, based on the cLogP of a derived analogue. The first synthesis of morpholine 3a (tosylate salt) is described; the seven-step sequence begins with inexpensive starting materials and uses straightforward chemistry.
Supporting Information
for this article is available online at http://www.thieme-connect.com/ejournals/toc/synthesis.
Two Kalamazoo businessmen named Entrepreneurs of the Year by Ernst & Young
By Alex Nixon | Kalamazoo Gazette
KALAMAZOO — Kalexsyn Inc. co-founders David Zimmermann and Robert Gadwood have been named Entrepreneurs of the Year by Ernst & Young.
Zimmermann and Gadwood, who formed Kalexsyn in 2003 after Pfizer Inc. purchased Pharmacia Corp., received the award in the technology category for the Michigan and Northwest Ohio region, according to a press release from the company.
Zimmermann is Kalexsyn’s CEO and Gadwood is the company’s president and chief scientific officer.
The award, “which recognizes outstanding entrepreneurs who are building and leading dynamic, growing businesses,” according to the release, was presented at an event in Dearborn on June 10.
Secret Champions
Sunday, September 20, 2009
Text by Steffan Heuer (translated)
Small businesses in the USA? Do they exist? Sure. Thriving and developing – they are the backbone of the economy, even in the US – but the rules of the game are completely different than in Germany. For example: Kalamazoo, Michigan “The weather is to blame for our company”, says Bill Main and wipes the sweat off his forehead. It gets very hot in the green lowlands of Michigan during summer time. Hard to believe that there is so much snow in winter – so much so that horticulture companies have to let