John M. Wetzel, Ph.D.

John M. Wetzel, Ph.D. has served full time as Principal of Wetzel Chemistry Consulting, LLC since 2006. For clients engaged in drug development, he has managed synthetic route scouting, process optimization, analytical method development/qualification, structure elucidation, impurity qualification, salt screening, polymorph characterization, and API manufacturing under cGMP. He has managed the development and manufacturing of parenteral, dermal and oral clinical trial materials. He has authored Chemistry, Manufacturing and Controls (CMC) documents in support of >15 Investigational New Drug Application (IND), New Drug Application (NDA) and post-approval filings. These filings resulted in two drugs receiving U.S. marketing approval, and several more entering Phase 1 and Phase 2 clinical trials. He is currently Director of Chemistry, Manufacturing and Controls for BioMimetix JV, LLC and South Rampart Pharma, Inc.  His achievements on behalf of clients engaged in anticancer, immunomodulatory, antibacterial and antiviral drug discovery include prioritizing chemical series; elucidating binding modes, structure-activity relationships and off-target binding sites; designing lead optimization strategies; identifying new compounds with improved target selectivity; and helping to obtain patent claims. He provided trial and deposition testimony in the pharmaceutical Hatch-Waxman litigation case, Hospira v Sandoz, District of New Jersey.

Prior to becoming an independent consultant, Dr. Wetzel was Director, Chemistry Support Services at Lundbeck Research USA, where he led project teams for MCH1 antagonist discovery and Chemistry Technology Platform development. As Director, Department of Chemistry at Synaptic Pharmaceutical Corporation, he led a 40-member team in the discovery and clinical development of drug candidates targeting G-protein coupled receptors for indications that included pain, mood disorders, obesity, and urinary disorders.  Discoveries made under his supervision included the first subtype-selective alpha-1a adrenoceptor antagonist, SNAP 5089, and tool compounds selective for the alpha-1d adrenoceptor. He managed the CMC efforts for preclinical and clinical development of a novel anti-depressant, including chemical process development, GMP-compliant synthesis, GLP-compliant analysis and bioanalysis, and formulation, and authoring of the CMC sections of the IND.

He is an inventor on 21 issued US patents and co-author of 26 peer-reviewed publications.

Background: Dr. Wetzel’s consulting services are provided under confidentiality.  His contributions to some representative projects are described below in general terms. Central Findings: Project 1: The original, laboratory-scale synthetic process for a drug candidate was modified to improve safety and efficiency, and scaled up to produce >1 kg under cGMP. Multiple topical formulations were developed, manufactured under cGMP, and used in Phase 1 and 2 clinical trials. The API process and supporting analytical methods were further optimized in preparation for pending Phase 3 clinical trials. Project 2: A parenteral drug product was manufactured under cGMP and used in Phase 1 and 2 trials. The API process is currently undergoing optimization in preparation for a Phase 3 clinical trial.  Project 3: The structure of the API (MW > 1000, several chiral centers) was proven by 2D NMR.  A deuterium-labeled reference standard was synthesized and used in the development and validation of bioanalytical methods.  Three batches of a parenteral drug product were manufactured under cGMP.  An improved formulation for reconstitution of the lyophilized drug product was developed, and its in-use stability was demonstrated. A Phase 1 clinical trial was completed.  Project 4: A complex polymorph landscape was elucidated and stable form identified; the API process was optimized and 9 kg of cGMP API manufactured.  Project 5:  A sixteen-step convergent synthesis was optimized, analytical methods developed and qualified, and 10 kg of cGMP API manufactured. An IND was filed and Phase II trial completed.  Project 6:  Route scouting, process development and a salt/polymorph screen were conducted, resulting in >1kg of cGMP API and three US patent applications. An IND was filed and Phase I trial completed.  Project 7:  An API process was optimized, a polymorph screen conducted; analytical methods developed and qualified; and 10 kg of cGMP API manufactured. A novel oral formulation was developed and manufactured, resulting in good bioavailability for a poorly water soluble API and a patent application. Bioanalytical methods were developed, validated and used to support nonclinical and clinical studies. An IND was filed and Phase 1 clinical trial completed.  Project 8:  A synthetic route was developed on laboratory scale. Scale-up is in progress.  Project 9: A parental drug product was manufactured under cGMP. Project 10:  Several antibacterial and antiviral drug development programs were evaluated and ranked on behalf of a US government contractor.

Dr. Wetzel’s Role: All laboratory and manufacturing activities described for Projects 1-10 were outsourced under his management or co-management. For most of these projects, and several others, he authored CMC sections, which were submitted in regulatory filings. he participated in several pre-IND meetings with FDA and addressed any CMC-related regulatory concerns, resulting in Study May Proceed letters from FDA.

Wetzel Chemistry Consulting, LLC
Albany, OH,
2005-present, Principal

How Clients Benefited in Drug Development:

• Novel active pharmaceutical ingredient (API) manufacturing processes were developed
• API and impurity structures were elucidated and impurities qualified
• API polymorphs were characterized
• Analytical and bioanalytical methods were developed and validated
• Novel oral, dermal and parenteral formulations were developed
• APIs and drug products were manufactured under cGMP, enabling clinical trials
• Chemistry, Manufacturing and Controls (CMC) documents were provided in support of >15 Investigational New Drug Application (IND), New Drug Application (NDA) and post-approval filings
• Two drugs received U.S. marketing approval
• New chemical entity, solid form, process and formulation patent applications were filed

How Clients Benefited in Drug Discovery:

• Several chemical series were prioritized according to their potential to yield drug-like leads for an anti-cancer target
• The binding mode, structure-activity relationships and likely sites of off-target binding were elucidated for two leading chemical series
• Predicted off-target binding was experimentally verified for several key cross-reactivity sites
• Testing strategies were designed and implemented for efficient prioritization of new compounds and minimization of off-target interactions
• New analogs with improved selectivity for the desired target were identified
• Patent applications were carefully written, Examiner concerns were addressed and patents were issued

How Clients Benefited in Litigation:

• Trial and deposition testimony was provided on behalf of defendant in the Hatch-Waxman Act litigation case, Hospira v Sandoz, District of New Jersey

BioMimetix JV, LLC, Greenwood Village, CO
2013 – present:
Director, Chemistry, Manufacturing & Controls

South Rampart Pharma, Inc., New Orleans, LA
2019 – present:
Director, Chemistry, Manufacturing & Controls

Ohio University, Athens, OH
2007 – 2009:
Visiting Assistant Professor, Department of Chemistry and Biochemistry

Lundbeck Research USA
Paramus, NJ.
2003-2005, Director, Chemistry Support Services

• Led project teams for MCH1 antagonist discovery and Chemistry Technology Platform development.
• Co-led the selection of an automated storage / retrieval strategy for the Lundbeck screening collection worldwide.

Synaptic Pharmaceutical Corporation
Paramus, NJ.
1990-2003, positions of increasing responsibility, culminating in Director, Department of Chemistry

• Managed 40 FTEs, including Medicinal, Computational, Analytical and Bioanalytical Chemists.
• Managed the outsourcing of Chemistry, Manufacturing and Controls (CMC) efforts for preclinical and clinical development of a novel anti-depressant, including chemical process development, GMP-compliant synthesis, GLP-compliant analysis and bioanalysis, and formulation. Contributed CMC section to IND filing and annual update.
• Designed and synthesized alpha-1a adrenoceptor antagonists for treatment of benign prostatic hyperplasia.
• Discovered the first subtype-selective alpha-1a antagonist, SNAP 5089
• Discovered highly selective alpha-1d adrenoceptor antagonists exemplified by SNAP 8493.
• Designed and implemented a novel strategy for the efficient characterization, purification and formatting of combinatorial libraries culminating in neat solid archive samples.
• Developed a novel LCMS-guided HPLC purification strategy for library purification.
• Conducted numerous HPLC separations, including enantioselective separations and high throughput library purifications, on milligram and gram scales.
• Procured and maintained NMR, LCMS, HPLC and other instruments.

Suntory Institute for Bioorganic Research
Osaka, Japan
1988-1990, Postdoctoral Fellow

• Explored the chemical relationship between the brown planthopper (Nilaparvata lugens) and its intracellular yeast-like symbiote through deuterium labeling and GCMS techniques.

The Johns Hopkins University, Ph.D., Chemistry, 1988

• Dissertation: Part I: Silicon-promoted ring contractions in the synthesis of carbocyclic spiro compounds. Total synthesis of (-)-solavetivone. Part II: The trimethylsilyl cationic species as a bulky proton. Application to chemoselective dioxolanation.
• Advisor: Prof. Reuben Jih-Ru Hwu.

Ohio University, B.S., Chemistry, 1982

1. Use of Alpha1C Specific Compounds to Treat Benign Prostatic Hyperplasia. Gluchowski, C.; Forray, C.C.; Chiu, G.; Branchek, T.A.; Wetzel, J.M.; Hartig, P.R. (1995). U.S. Patent 5,403,847.
2. Use of Alpha-1C Specific Compounds to Treat Benign Prostatic Hyperplasia. Gluchowski, C.; Forray, C.C.; Chiu, G.; Branchek, T.A.; Wetzel, J.M.; Hartig, P.R. (1996). U.S. Patent 5,578,611.
3. Dihydropyridines and New Uses Thereof. Gluchowski, C.; Wetzel, J.M.; Chiu, G.; Marzabadi, M.R.; Wong, W.C.; Nagarathnam, D. (1998). U.S. Patent 5,767,131.
4. Use of Alpha1c Specific Compounds to Treat Benign Prostatic Hyperplasia. Gluchowski, C.; Forray, C.C.; Chiu, G.; Branchek, T.A.; Wetzel, J.M.; Hartig, P.R. (1998). U.S. Patent 5,780,485.
5. Alpha1C Specific Compounds to Treat Benign Prostatic Hyperplasia. Gluchowski, C.; Forray, C.C.; Chiu, G.; Branchek, T.A.; Wetzel; John M.; Hartig; Paul R. (1999) U.S. Patent 5,990,128.
6. Use of Alpha-1C Specific Compounds to Treat Benign Prostatic Hyperplasia. Gluchowski, C.; Forray, C.C.; Chiu, G.; Branchek, T.A.; Wetzel, J.M.; Hartig, P.R. (2000) U.S. Patent 6,015,819.
7. Dihydropyridines and New Uses Thereof. Gluchowski,C.; Wetzel, J.M.; Chiu, G.; Marzabadi, M.R.; Wong, W.C.; Nagarathnam, D. (2001) U.S. Patent 6,211,198.
8. Dihydropyridines and New Uses Thereof. Gluchowski, C.; Wetzel, J.M.; Chiu, G.; Marzabadi, M.R.; Wong, W.C.; Nagarathnam, D. (2001) U.S. Patent 6,310,076.
9. Use of Alpha1C Specific Compounds to Treat Benign Prostatic Hyperplasia. Gluchowski, C.; Forray, C.C.; Chiu; G.; Branchek, T.A.; Wetzel; J.M.; Hartig; P.R. (2003). U.S. Patent 6,602,888.
10. Dihydropyridines and New Uses Thereof. Gluchowski, C.; Wetzel; J.M.; Chiu; G.; Marzabadi, M.R.; Wong, W.C.; Nagarathnam, D. (2003). U.S. Patent 6,608,086.
11. Compounds Specific for the Human Alpha1d Adrenergic Receptor and Uses Thereof. Konkel, M.; Wetzel, J.M.; Noble, S.A.; Gluchowski, C.; Craig, D.A. (2004). U.S. Patent
6,706,716.
12. Selective Melanin Concentrating Hormone-1 (MCH1) Receptor Antagonists and Uses Thereof. Marzabadi, M.R.; Wetzel, J.; DeLeon, J.E.; Lagu, B; Gluchowski, C.; Noble, S.; Nagarathnam, D. (2004). U.S. Patent 6,720,324.
13. Substituted Anilinic Piperidines as MCH Selective Antagonists. Marzabadi, M.R.; Wetzel, J.; Deleon, J.E.; Jiang, Y.; Chen, C.-A.; Lu, K. (2004). U.S. Patent 6,727,264.
14. Substituted Anilinic Piperidines as MCH Selective Antagonists. Marzabadi, M.R.; Wetzel, J.; DeLeon, J.E.; Jiang, Y.; Chen, C.-A.; Lu, K. (2006). U.S. Patent 7,067,534.
15. Use of GALR3 Receptor Antagonists for the Treatment of Depression and/or Anxiety and Compounds Useful in Such Methods. Konkel, M.; Wetzel, J.M.; Talisman, J. (2006). U.S. Patent 7,081,470.
16. Substituted Alkyl Amido Piperidines. Marzabadi, M.R.; Wetzel, J.; Chen, C.-A.; Jiang, Y.; Lu, K. (2006). U.S. Patent 7,105,544.
17. 3-Imino-2-indolones for the Treatment of Depression and/or Anxiety. Konkel, M.; Wetzel, J.M.; Talisman, J. (2007). U.S. Patent 7,166,635.
18. Substituted Alkyl Amido Piperidines. Marzabadi,M.R.; Wetzel, J.; Chen, C.-A.; Jiang, Y.; Lu, K. (2007). U.S. Patent 7,199,135.
19. Spirocyclic Piperidines as MCH1 Antagonists and Uses Thereof. Marzabadi, M.R.; Jiang, Y.; Lu, K.; Chen, C.-A.; De Leon, J.E.; Wetzel, J.M.; Andersen, K. (2008). U.S. Patent 7,335,665.
20. Use of GALR3 Antagonist for Treatment of Depression and/or Anxiety and Compounds Useful in Such Methods. Blackburn, T.P.; Konkel, M.J.; Boteju, L.W.; Talisman, I.J.; Wetzel, J.M.; Packiarajan, M.; Chen, H.; Jimenez, H. (2008). U.S. Patent 7,465,750.
21. Secondary Amino Anilinic Piperidines as MCH1 Antagonists and Uses Thereof. Marzabadi, M.R.; Jiang, Y.; Lu, K.; Chen, C.-A.; De Leon, J.E.; Wetzel, J.M. (2009). U.S. Patent 7,473,698.

1. Mechanistic studies in the deoxygenation of pyridine N-oxide: new 1,2 elimination. Hwu, J.R.; Wetzel, J.M. (1985) Journal of Organic Chemistry 50(3), 400-2.
2. The trimethylsilyl cationic species as a bulky proton. Application to chemoselective dioxolanation. Hwu, J.R.; Wetzel, J.M. (1985) Journal of Organic Chemistry 50(20), 3946-8.
3. Calcium in liquid ammonia for the reduction of benzyl ethers. Mechanistic clues derived from chemoselectivity studies. Hwu, J.R.; Chua, V.; Schroeder, J.E.; Barrans, R.E., Jr.; Khoudary, K.P.; Wang, N.; Wetzel, J.M. (1986) Journal of Organic Chemisty 51(24), 4731-3.
4. General scope of 1,3-dioxolanation of alpha,beta-unsaturated aldehydes with 1,2-bis (trimethylsilyloxy) ethane and trimethylsilyl trifluoromethanesulfonate. Hwu, J.R.; Leu, L.C.; Robl, J.A.; Anderson, D.A.; Wetzel, J.M.. (1987) Journal of Organic Chemistry 52(2), 188-91.
5. Silicon-promoted ring contractions in the formation of carbocyclic spiro compounds. Total synthesis of (-)- solavetivone. Hwu, J.R.; Wetzel, J.M. (1992) Journal of Organic Chemistry 57 (3), 922-8.
6. Diversity in steroidogenesis of symbiotic microorganisms from planthoppers. Wetzel, J.M.; Ohnishi, M.; Fujita, T.; Nakanishi, K.; Naya, Y.; Noda, H.; Sugiura, M. (1992) Journal of Chemical Ecology 18(11), 2083-94.
7. Comparison of the electronic effect and the steric influence between the 1,1,2,2,2-pentamethyldisilanyl and the trimethylsilyl groups. Hwu, J.R.; Wetzel, J.M.; Lee, J.S.; Butcher, R.J. (1993) Journal of Organometallic Chemistry 453(1), 21-8.
8. The alpha1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha1c subtype. Forray, C.; Bard, J.A.; Wetzel, J.M.; Chiu, G.; Shapiro, E.; Tang, R.; Lepor, H.; Hartig, P.R.; Weinshank, R.L.; Branchek, T.A.; Gluchowski, C. (1994) Molecular Pharmacology 45(4), 703-8.
9. Discovery of alpha1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. Wetzel, J. M.; Miao, S.W.; Forray, C.; Borden, L.A.; Branchek, T.A.; Gluchowski, C. (1995) Journal of Medicinal Chemistry 38(10), 1579-81.
10. Fragmentation studies of ergosterol. The formation of the fragment ion at m/z 337. Kenney, P.T.M.; Wetzel, J.M. (1995) European Mass Spectrometry 1(4), 411-13.
11. Modeling and mutagenesis of the human alpha1a-adrenoceptor: orientation and function of transmembrane helix V sidechains. Wetzel, J.M.; Salon, J.A.; Tamm, J.A.; Forray, C.; Craig, D.; Nakanishi, H.; Cui, W.; Vaysse, P.J.-J.; Chiu, G.; Weinshank, R.L., Hartig, P.R., Branchek, T.A., Gluchowski, C. (1996)  receptors and Channels 4(3), 165-177.
12. Localization of mRNA and receptor binding sites for the alpha1a-adrenoceptor subtype in the rat, monkey and human urinary bladder and prostate. Walden, P.D.; Durkin, M.M.; Lepor, H.; Wetzel, J.M.; Gluchowski, C.; Gustafon, E.L. (1997) Journal of Urology (Baltimore) 157(3), 1032-1038.
13. Characterization of specific binding of [125I]L-762,459, a selective alpha1A-adrenoceptor radioligand to rat and human tissues. O’Malley, S.S.; Chen, T.B.; Francis, B.E.; Gibson, R.E.; Burns, H.D.; DiSalvo, J.; Bayne, M.L.; Wetzel, J.M.; Nagarathnam, D.; Marzabadi, M.; Gluchowski, C.; Chang, R.S.L. (1998) European Journal of Pharmacology 348(2/3), 287-295.
14. Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate. Wong, W.C.; Chiu, G.; Wetzel, J.M.; Marzabadi,M.R.; Nagarathnam, D.; Wang, D.; Fang, J.; Miao, S.W.; Hong, X.; Forray, C.; Vaysse, P.J.J.; Branchek, T.A.; Gluchowski, C.; Tang, R.; Lepor, H. (1998) Journal of Medicinal Chemistry 41(14), 2643-2650.
15. Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia. Nagarathnam, D.; Wetzel, J.M.; Miao, S.W.; Marzabadi, M.R.; Chiu, G.; Wong, W.C.; Hong, X.; Fang, J.; Forray, C.; Branchek, T.A.; Heydorn, W.E.; Chang, R.S.L.; Broten, T.; Schorn, T.W.; Gluchowski, C. (1998) Journal of Medicinal Chemistry 41(26), 5320-5333.
16. Design and synthesis of novel dihydropyridine alpha-1A antagonists. Marzabadi, M.R.; Hong, X.;  agarathnam, D.; Miao, S.; Chiu, G.; Wong, W.C.; Wetzel, J.M.; Fang, J.; Forray, C.; Chen, T.B.; O’Malley, S.S.; Chang, R.S.L.; Gluchowski, C. (1999) Bioorganic & Medicinal Chemistry Letters 9(19), 2843-2848.
17. Design and synthesis of novel alpha1a adrenoceptor-selective antagonists. 4. Structureactivity relationship in the dihydropyrimidine series. Wong, W.C.; Sun, W.; Lagu, B.; Tian, D.; Marzabadi, M.R.; Zhang, F.; Nagarathnam, D.; Miao, S.W.; Wetzel, J.M.; Peng, J.; Forray, C.; Chang, R.S.L.; Chen, T.B.; Ransom, R.; O’Malley, S.; Broten, T.P.; Kling, P.; Vyas, K.P.; Zhang, K.; Gluchowski, C. (1999) Journal of Medicinal Chemistry 42(23) 4804-4813.
18. Design and synthesis of novel alpha1a adrenoceptor-selective antagonists. 1. Structureactivity relationship in dihydropyrimidinones. Nagarathnam, D.; Miao, S. Wu; Lagu, B.; Chiu, G.; Fang, J.; Dhar, T.G. Murali; Zhang, J.; Tyagarajan, S.; Marzabadi, M.R.; Zhang, F.; Wong, W.C.; Sun, W.; Tian, D.; Wetzel, J.M.; Forray, C.; Chang, R.S.L.; Broten, T.P.; Ransom, R.W.; Schorn, T.W.; Chen, T.B.; O’Malley, S.; Kling, P.; Schneck, K.; Bendesky, R.; Harrell, C.M.; Vyas, K.P.; Gluchowski, C. (1999) Journal of Medicinal Chemistry 42(23), 4764-4777.
19. Design and synthesis of novel alpha1a adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety. Dhar, T.G.M.; Nagarathnam, D.; Marzabadi, M.R.; Lagu, B.; Wong, W.C.; Chiu, G.; Tyagarajan, S.; Miao, S.W.; Zhang, F.; Sun, W.; Tian, D.; Shen, Q.; Zhang, J.; Wetzel, J.M.; Forray, C.; Chang, R.S.L.; Broten, T.P.; Schorn, T.W.; Chen, T.B.; O’Malley, S.; Ransom, R.; Schneck, K.; Bendesky, R.; Harrell, C.M.; Vyas, K.P.; Zhang, K.; Gilbert, J.; Pettibone, D.J.; Patane, M.A.; Bock, M.G.; Freidinger, R.M.; Gluchowski, C. (1999) Journal of
Medicinal Chemistry 42 (23), 4778-4793.
20. De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability. Lagu,B.; Tian, D.; Jeon, Y.; Li, C.; Wetzel, J.M.; Nagarathnam, D.; Shen, Q.; Forray, C.; Chang, R.S.L.; Broten, T.P.; Ransom, R.W.; Chan, T.-B.; O’Malley, S.S.; Schorn, T.W.; Rodrigues, A.D.; Kassahun, K.; Pettibone, D.J.; Freidinger, R.; Gluchowski, C. (2000) Journal of Medicinal Chemistry 43(15), 2775-2778.
21. Determination of the relative and absolute stereochemistry of a potent and alpha1Aselective adrenoceptor antagonist. Lagu, B.; Wetzel, J. M.; Forray, C.; Patane, M.A.; Bock, M.G.
(2000) Bioorganic & Medicinal Chemistry Letters 10(24), 2705-2707.
22. Identification and characterization of two G protein-coupled receptors for neuropeptide FF. Bonini, J.A.; Jones, K.A.; Adham, N.; Forray, C.; Artymyshyn, R.; Durkin, M.M.; Smith, K.E.; Tamm, J.A.; Boteju, L.W.; Lakhlani, P.P.; Raddatz, R.; Yao, W.-J.; Ogozalek, K.L.; Boyle, N.; Kouranova, E.V.; Quan, Y.; Vaysse, P.J.; Wetzel, J.M.; Branchek, T.A.; Gerald, C.; Borowsky, B. (2000) Journal of Biological Chemistry 275(50), 39324-39331.
23. Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin- 1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists. Konkel, M.J.; Wetzel, J.M.; Cahir, M.; Craig, D.A.; Noble, S.A.; Gluchowski, C. (2005) Journal of Medicinal Chemistry 48(8), 3076-3079.
24. Synthesis and SAR Investigations for Novel Melanin-Concentrating Hormone 1 Receptor (MCH1) Antagonists Part 1. The Discovery of Arylacetamides as Viable Replacements for the Dihydropyrimidinone Moiety of an HTS Hit. Jiang, Y.; Chen, C.-A.; Lu, K.; Daniewska, I.; De Leon, J.; Kong, R.; Forray, C.; Li, B.; Hegde, L.G.; Wolinsky, T.D.; Craig, D.A.; Wetzel, J.M.; Andersen, K.; Marzabadi, M. (2007) Journal of Medicinal Chemistry 50(16), 3870-3882.
25. Synthesis and SAR Investigations for Novel Melanin-Concentrating Hormone 1 Receptor (MCH1) Antagonists Part 2: A Hybrid Strategy Combining Key Fragments of HTS Hits. Chen, C.-A.; Jiang, Y.; Lu, K.; Daniewska, I.; Mazza, C.G.; Negron, L.; Forray, C.; Parola, T.; Li, B.; Hegde, L.G.; Wolinsky, T.D.; Craig, D.A.; Kong, R.; Wetzel, J.M.; Andersen, K.; Marzabadi, M. (2007) Journal of Medicinal Chemistry 50(16), 3883-3890.