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Volumn 12, Issue 4, 2009, Pages 519-532

GPR119 agonists: A promising new approach for the treatment of type 2 diabetes and related metabolic disorders

Author keywords

Agonist; Antidiabetic agent; GLP 1; GPCR; GPR119; Obesity; Type 2 diabetes

Indexed keywords

ANTIDIABETIC AGENT; APD 597; APD 668; AR 231453; CYCLIC AMP; DIPEPTIDYL PEPTIDASE IV INHIBITOR; EXENDIN 4; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR 119; G PROTEIN COUPLED RECEPTOR 119 AGONIST; GASTRIC INHIBITORY POLYPEPTIDE; GLIBENCLAMIDE; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; INSULIN; LYSOPHOSPHATIDYLCHOLINE; MBX 2982; N OLEOYLETHANOLAMINE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; PSN 119 1; PSN 119 1M; PSN 119 2; PSN 375963; PSN 632408; PSN 821; PYRIDINE DERIVATIVE; PYRIDONE DERIVATIVE; PYRIMIDINE DERIVATIVE; SITAGLIPTIN; UNCLASSIFIED DRUG; UNINDEXED DRUG;

EID: 67649979936     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (44)

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    • Arena Pharmaceuticals Inc: Arena Pharmaceuticals, Inc. announces initiation of phase 1 clinical trial of Arena type 2 diabetes drug candidate in collaboration with Ortho-McNeil, :February 07
    • Arena Pharmaceuticals Inc: Arena Pharmaceuticals, Inc. announces initiation of phase 1 clinical trial of Arena type 2 diabetes drug candidate in collaboration with Ortho-McNeil.Press Release (2006):February 07.
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    • Semple G: Discovery and pharmacological evaluation of agonists of the orphan receptor GDIR (GPR119). Second RSCSCI Symposium on GPCRs in Medicinal Chemistry, Gothenburg, Sweden (2008). · Preclinical data on Arena's first clinical candidate APD-668, which was discontinued to advance a more potent GPR119 agonist, were presented.
    • Semple G: Discovery and pharmacological evaluation of agonists of the orphan receptor GDIR (GPR119). Second RSCSCI Symposium on GPCRs in Medicinal Chemistry, Gothenburg, Sweden (2008). · Preclinical data on Arena's first clinical candidate APD-668, which was discontinued to advance a more potent GPR119 agonist, were presented.
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    • Arena Pharmaceuticals Inc: Arena Pharmaceuticals announces APD668 initial clinical study results suggest glucose-dependent insulinotropic receptors may improve glucose control in patients with type 2 diabetes. Press Release (2008):January 07.
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    • Arena Pharmaceuticals Inc: Arena Pharmaceuticals announces initiation of phase 1 clinical trial of type 2 diabetes drug candidate in partnership with Ortho-McNeil-Janssen Pharmaceuticals, :December 15
    • Arena Pharmaceuticals Inc: Arena Pharmaceuticals announces initiation of phase 1 clinical trial of type 2 diabetes drug candidate in partnership with Ortho-McNeil-Janssen Pharmaceuticals. Press Release (2008):December 15.
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    • Fyfe M, Mccormack J, Overton H, Procter M, Reynet C: PSN821: A novel oral GPR119 agonist for the treatment of type 2 diabetes producing substantial glucose lowering and weight loss in rats. American Diabetes Association Annual Scientific Sessions, San Francisco, CA, USA (2008) 68:Abs 297-OR. · Provided preclinical data on Prosidion's compound PSN-821, which is currently being evaluated in a phase I clinical trial.
    • Fyfe M, Mccormack J, Overton H, Procter M, Reynet C: PSN821: A novel oral GPR119 agonist for the treatment of type 2 diabetes producing substantial glucose lowering and weight loss in rats. American Diabetes Association Annual Scientific Sessions, San Francisco, CA, USA (2008) 68:Abs 297-OR. · Provided preclinical data on Prosidion's compound PSN-821, which is currently being evaluated in a phase I clinical trial.
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    • OSI Pharmaceuticals provides update on diabetes and obesity clinical programs
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    • (2009) Press Release
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    • Metabolex Inc: Metabolex announces positive results from phase 1a clinical trial of MBX-2982, November 03
    • Metabolex Inc: Metabolex announces positive results from phase 1a clinical trial of MBX-2982. Press Release (2008): November 03.
    • (2008) Press Release
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    • A novel dual DPP-IV inhibitor and GPR119 agonist that exhibits superior glucose lowering to sitagliptin in diabetic ZDF rats
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    • Swain S, Cock TA, Wong-Kai-In P: A novel dual DPP-IV inhibitor and GPR119 agonist that exhibits superior glucose lowering to sitagliptin in diabetic ZDF rats. American Diabetes Association Annual Scientific Sessions, New Orleans, LA, USA (2009) 69:Abs 453-P.
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    • Arena Pharmaceuticals Inc (Jones RM, Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Duvvuri K, Choi JSK, Xiong Y, Dave V): 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia. WO-2004065380 (2004).
    • Arena Pharmaceuticals Inc (Jones RM, Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Duvvuri K, Choi JSK, Xiong Y, Dave V): 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia. WO-2004065380 (2004).
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    • Jones RM): Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level.US-20060154866
    • Arena Pharmaceuticals Inc Chu Z-L, ·
    • Arena Pharmaceuticals Inc (Chu Z-L, Leonard JN, Al-Shamma HA, Jones RM): Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level.US-20060154866 (2006). · Provides evidence that GPR119 agonism and DPP-IV inhibition in combination lead to significant improvement in glycemic control.
    • Provides evidence that GPR119 agonism and DPP-IV inhibition in combination lead to significant improvement in glycemic control
    • Leonard, J.N.1    Al-Shamma, H.A.2
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    • OSI) Prosidion (Fyfe MCT, Widdowson P, Use of GPCR agonists to delay progression of diabetes. WO-2007138362 2007, · Explains the effects of a Prosidion's GPR119 agonist in delaying the progression of diabetes in animal models
    • (OSI) Prosidion (Fyfe MCT, Widdowson P): Use of GPCR agonists to delay progression of diabetes. WO-2007138362 (2007). · Explains the effects of a Prosidion's GPR119 agonist in delaying the progression of diabetes in animal models.
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    • OSI) Prosidion (Fyfe M, Gardner L, King-Underwood J, Procter M, Rasamison C, Schofield K, Thomas GH, Heterocyclic derivatives as GPCR receptor agonists. WO-2005061489 2005
    • (OSI) Prosidion (Fyfe M, Gardner L, King-Underwood J, Procter M, Rasamison C, Schofield K, Thomas GH): Heterocyclic derivatives as GPCR receptor agonists. WO-2005061489 (2005).
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    • Arena Pharmaceuticals Inc (Jones RM, Semple G, Xiong Y, Shin Y-J, Ren AS, Lehmann J, Fioravanti B, Bruce MA, Choi JSK): Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto. WO-2005121121 (2005).
    • Arena Pharmaceuticals Inc (Jones RM, Semple G, Xiong Y, Shin Y-J, Ren AS, Lehmann J, Fioravanti B, Bruce MA, Choi JSK): Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto. WO-2005121121 (2005).
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    • Arena Pharmaceuticals Inc (Jones RM, Semple G, Xiong Y, Shin Y-J, Ren AS, Calderon I, Choi JSK, Fioravanti B, Lehmann J, Bruce MA): Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto. WO-2005007647 (2005).
    • Arena Pharmaceuticals Inc (Jones RM, Semple G, Xiong Y, Shin Y-J, Ren AS, Calderon I, Choi JSK, Fioravanti B, Lehmann J, Bruce MA): Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto. WO-2005007647 (2005).
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    • Arena Pharmaceuticals Inc (Jones RM, Lehmann J, Wong AS, Hurst D, Shin Y-J): Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto. US-20070167473 (2007).
    • Arena Pharmaceuticals Inc (Jones RM, Lehmann J, Wong AS, Hurst D, Shin Y-J): Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto. US-20070167473 (2007).
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    • Arena Pharmaceuticals Inc (Gharbaoui T, Fritch JR, Krishnan AM, Throop BW, Kato NS): Processes for preparing aromatic ethers.US-20060155129 (2006).
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    • Arena Pharmaceuticals Inc (Jones RM, Lehmann J): Modulators of metabolism and the treatment of disorders related thereto.WO-2007035355 (2007).
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    • Arena Pharmaceuticals Inc (Jones RM, Lehmann J, Siu-Ting Wong A): Modulators of metabolism and the treatment of disorders related thereto. WO-2008005569 (2008).
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    • Arena Pharmaceuticals Inc (Jones RM, Lehmann J): Modulators of metabolism and the treatment of disorders related thereto.WO-2008005576 (2008).
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    • Arena Pharmaceuticals Inc (Jones RM, Semple G, Xiong Y, Shin Y-J, Ren AS, Calderon I, Fioravanti B, Choi JSK, Sage CR): Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto.WO-2005007658 (2005).
    • Arena Pharmaceuticals Inc (Jones RM, Semple G, Xiong Y, Shin Y-J, Ren AS, Calderon I, Fioravanti B, Choi JSK, Sage CR): Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto.WO-2005007658 (2005).
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    • Arena Pharmaceuticals Inc (Gharbaoui T, Sengupta D, Lally EA, Kato NS, Carlos M, Rodriguez N): Processes for preparing pyrazolo[3,4-d] pyrimidine ethers. US-20060154940 (2006).
    • Arena Pharmaceuticals Inc (Gharbaoui T, Sengupta D, Lally EA, Kato NS, Carlos M, Rodriguez N): Processes for preparing pyrazolo[3,4-d] pyrimidine ethers. US-20060154940 (2006).
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    • OSI) Prosidion (Fyfe MCT, Gardner LS, Thomas GH, Williams GM, G-protein coupled receptor (GPR116) agonists and use thereof for treating obesity and diabetes. WO-2006067531 2006
    • (OSI) Prosidion (Fyfe MCT, Gardner LS, Thomas GH, Williams GM): G-protein coupled receptor (GPR116) agonists and use thereof for treating obesity and diabetes. WO-2006067531 (2006).
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    • OSI) Prosidion (Bradley SE, Dawson GJ, Fyfe MCT, Bertram LS, Gattrell W, Jeevaratnam RP, Keily J, Mistry NS, Procter MJ, Rasamison CM, Rushworth PJ et al, GPCR agonists. WO-2007003960 2007
    • (OSI) Prosidion (Bradley SE, Dawson GJ, Fyfe MCT, Bertram LS, Gattrell W, Jeevaratnam RP, Keily J, Mistry NS, Procter MJ, Rasamison CM, Rushworth PJ et al): GPCR agonists. WO-2007003960 (2007).
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    • OSI) Prosidion (Bertram LS, Fyfe MCT, Procter MJ, Williams GM, Heterocyclic GPCR agonists. WO-2007116229 2007
    • (OSI) Prosidion (Bertram LS, Fyfe MCT, Procter MJ, Williams GM): Heterocyclic GPCR agonists. WO-2007116229 (2007).
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    • OSI) Prosidion (Fyfe MCT, Keily J, Swain SA, Piperidine GPCR agonists. WO-2008081204 2008
    • (OSI) Prosidion (Fyfe MCT, Keily J, Swain SA): Piperidine GPCR agonists. WO-2008081204 (2008).
  • 85
    • 67649931903 scopus 로고    scopus 로고
    • OSI) Prosidion (Fyfe MCT, Jeevaratnam RP, Keily J, Swain SA, Piperidine GPCR agonists. WO-2008081207 2008
    • (OSI) Prosidion (Fyfe MCT, Jeevaratnam RP, Keily J, Swain SA): Piperidine GPCR agonists. WO-2008081207 (2008).
  • 86
    • 67649897710 scopus 로고    scopus 로고
    • OSI) Prosidion (Fyfe MCT, Jeevaratnam RP, Keily J, Swain SA, Piperidine GPCR agonists. WO-2008081208 2008
    • (OSI) Prosidion (Fyfe MCT, Jeevaratnam RP, Keily J, Swain SA): Piperidine GPCR agonists. WO-2008081208 (2008).
  • 87
    • 67649928867 scopus 로고    scopus 로고
    • OSI) Prosidion (Bertram LS, Fyfe MCT, Jeevaratnam RP, Keily J, Swain SA, Piperidine GPCR agonists. WO-2008081205 2008
    • (OSI) Prosidion (Bertram LS, Fyfe MCT, Jeevaratnam RP, Keily J, Swain SA): Piperidine GPCR agonists. WO-2008081205 (2008).
  • 88
    • 67649914818 scopus 로고    scopus 로고
    • OSI) Prosidion (Barba O, Bradley SE, Fyfe MCT, Hanrahan PE, Krulle TM, Procter MJ, Reynet Mccormack C, Schofield KL, Smyth D, Stewart AJW, Swain SA et al, Compounds for the treatment of metabolic disorders. WO-2009034388 2009
    • (OSI) Prosidion (Barba O, Bradley SE, Fyfe MCT, Hanrahan PE, Krulle TM, Procter MJ, Reynet Mccormack C, Schofield KL, Smyth D, Stewart AJW, Swain SA et al): Compounds for the treatment of metabolic disorders. WO-2009034388 (2009).
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    • 67649902376 scopus 로고    scopus 로고
    • Metabolex Inc (Chen X, Cheng P, Clemens LE, Johnson JD, Ma J, Murphy A, Nashashibi I, Rabbat CJ, Song J, Wilson ME, Zhu Y et al, Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders. WO-2008083238 2008
    • Metabolex Inc (Chen X, Cheng P, Clemens LE, Johnson JD, Ma J, Murphy A, Nashashibi I, Rabbat CJ, Song J, Wilson ME, Zhu Y et al): Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders. WO-2008083238 (2008).
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    • 67649913240 scopus 로고    scopus 로고
    • Metabolex Inc (Ma J, Rabbat CJ, Song J, Chen X, Nashashibi I, Zhao Z, Novack A, Shi DF, Cheng P, Zhu Y, Murphy A): N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders. WO-2009014910 (2009).
    • Metabolex Inc (Ma J, Rabbat CJ, Song J, Chen X, Nashashibi I, Zhao Z, Novack A, Shi DF, Cheng P, Zhu Y, Murphy A): N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders. WO-2009014910 (2009).
  • 91
    • 67649955255 scopus 로고    scopus 로고
    • Bristol-Myers Squibb Co (Fevig JM, Wacker DA): [6,6] and [6,7]-Bicyclic GPR119 G protein-coupled receptor agonists.WO-2008137435 (2008).
    • Bristol-Myers Squibb Co (Fevig JM, Wacker DA): [6,6] and [6,7]-Bicyclic GPR119 G protein-coupled receptor agonists.WO-2008137435 (2008).
  • 92
    • 67649900012 scopus 로고    scopus 로고
    • Bristol-Myers Squibb Co (Fevig JM, Wacker DA): [6,5]-Bicyclic GPR119 G protein-coupled receptor agonists. WO-2008137436 (2008).
    • Bristol-Myers Squibb Co (Fevig JM, Wacker DA): [6,5]-Bicyclic GPR119 G protein-coupled receptor agonists. WO-2008137436 (2008).
  • 93
    • 67649917945 scopus 로고    scopus 로고
    • Bristol-Myers Squibb Co (Wacker DA, Rossi KA, Wang Y): Pyridone GPR119 G protein-coupled receptor agonists. WO-2009012275 (2009).
    • Bristol-Myers Squibb Co (Wacker DA, Rossi KA, Wang Y): Pyridone GPR119 G protein-coupled receptor agonists. WO-2009012275 (2009).
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    • 67649917941 scopus 로고    scopus 로고
    • Bristol-Myers Squibb Co (Wacker DA, Rossi KA, Wang Y): Method for modulating GPR119 G protein-coupled receptor and selected compounds. WO-2009012277 (2009).
    • Bristol-Myers Squibb Co (Wacker DA, Rossi KA, Wang Y): Method for modulating GPR119 G protein-coupled receptor and selected compounds. WO-2009012277 (2009).
  • 95
    • 67649914817 scopus 로고    scopus 로고
    • Smithkline Beecham Corp (Katamreddy SR, Caldwell RD, Heyer D, Samano V, Thompson JB, Carpenter AJ, Conlee CR, Boros EE, Thompson BD): Chemical compounds. WO-2008008887 (2008).
    • Smithkline Beecham Corp (Katamreddy SR, Caldwell RD, Heyer D, Samano V, Thompson JB, Carpenter AJ, Conlee CR, Boros EE, Thompson BD): Chemical compounds. WO-2008008887 (2008).
  • 96
    • 67649913241 scopus 로고    scopus 로고
    • Smithkline Beecham Corp (Ammala C, Briscoe C): GPR119 agonists for the treatment of diabetes and related disorders.WO-2008008895 (2008).
    • Smithkline Beecham Corp (Ammala C, Briscoe C): GPR119 agonists for the treatment of diabetes and related disorders.WO-2008008895 (2008).
  • 97
    • 67649943602 scopus 로고    scopus 로고
    • Smithkline Beecham Corp (Fang J, Tang J, Carpenter AJ, Peckham G, Conlee CR, Du KS, Katamreddy SR): Chemical compounds and uses. WO-2008070692 (2008).
    • Smithkline Beecham Corp (Fang J, Tang J, Carpenter AJ, Peckham G, Conlee CR, Du KS, Katamreddy SR): Chemical compounds and uses. WO-2008070692 (2008).
  • 98
    • 67649928868 scopus 로고    scopus 로고
    • Biovitrum AB (Brandt P, Emond R, Johansson G, Johansson L, Koolmeister T, Nilsson BM, Sandvall T, Weber M, Pyridine compounds for treating GPR119 related disorders.WO-2008025798 2008
    • Biovitrum AB (Brandt P, Emond R, Johansson G, Johansson L, Koolmeister T, Nilsson BM, Sandvall T, Weber M): Pyridine compounds for treating GPR119 related disorders.WO-2008025798 (2008).
  • 99
    • 67649917947 scopus 로고    scopus 로고
    • Biovitrum AB (Brandt P, Johansson G, Johansson L, Koolmeister T, Nilsson BM, Sandvall T, Pyridazine compounds for treating GPR119 related disorders. WO-2008025799 2008
    • Biovitrum AB (Brandt P, Johansson G, Johansson L, Koolmeister T, Nilsson BM, Sandvall T): Pyridazine compounds for treating GPR119 related disorders. WO-2008025799 (2008).
  • 100
    • 67649893058 scopus 로고    scopus 로고
    • Biovitrum AB (Brandt P, Johansson G, Johansson L, Koolmeister T, Nilsson BM, Sandvall T, Weber M, Pyrimidine compounds for treating GPR119 related disorders. WO-2008025800 2008
    • Biovitrum AB (Brandt P, Johansson G, Johansson L, Koolmeister T, Nilsson BM, Sandvall T, Weber M): Pyrimidine compounds for treating GPR119 related disorders. WO-2008025800 (2008).
  • 101
    • 67649905543 scopus 로고    scopus 로고
    • Schering Corp (Boyle CD, Neelamkavil SF, Chackalamannil S, Neustadt BR, Hao J, Shah U, Harris J, Liu H, Stamford AW): Pyrimidinone derivatives and methods of use thereof.WO-2008130581 (2008).
    • Schering Corp (Boyle CD, Neelamkavil SF, Chackalamannil S, Neustadt BR, Hao J, Shah U, Harris J, Liu H, Stamford AW): Pyrimidinone derivatives and methods of use thereof.WO-2008130581 (2008).
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    • 67649925007 scopus 로고    scopus 로고
    • Schering Corp (Boyle CD, Chackalamannil S, Lankin CM, Shah UG, Neustadt BR, Liu H, Stamford AW): Pyrimidinone derivatives and methods of use thereof. WO-2008130584 (2008).
    • Schering Corp (Boyle CD, Chackalamannil S, Lankin CM, Shah UG, Neustadt BR, Liu H, Stamford AW): Pyrimidinone derivatives and methods of use thereof. WO-2008130584 (2008).
  • 103
    • 67649900013 scopus 로고    scopus 로고
    • Merck & Co Inc (Wood HB, Adams AD, Freeman S, Szewczyk JW, Santini C, Huang Y, Mosley RT): Acyl bipiperidinyl compounds, compositions containing such compounds and methods of treatment. WO-2008076243 (2008).
    • Merck & Co Inc (Wood HB, Adams AD, Freeman S, Szewczyk JW, Santini C, Huang Y, Mosley RT): Acyl bipiperidinyl compounds, compositions containing such compounds and methods of treatment. WO-2008076243 (2008).
  • 104
    • 67649902377 scopus 로고    scopus 로고
    • Merck & Co Inc (Wood HB, Adams AD, Freeman S, Szewczyk JW, Santini C, Huang Y): Bipiperidinyl compounds, compositions containing such compounds and methods of treatment.WO-2008085316 (2008).
    • Merck & Co Inc (Wood HB, Adams AD, Freeman S, Szewczyk JW, Santini C, Huang Y): Bipiperidinyl compounds, compositions containing such compounds and methods of treatment.WO-2008085316 (2008).
  • 105
    • 67649955256 scopus 로고    scopus 로고
    • IRM LLC (Alper P, Azimioara M, Cow C, Epple R, Jiang S, Lelais G, Michellys P-Y, Nguyen TN, Westscott-Baker L, Wu B, Compounds and compositions as modulators of GPR119 activity.WO-2008097428 2008
    • IRM LLC (Alper P, Azimioara M, Cow C, Epple R, Jiang S, Lelais G, Michellys P-Y, Nguyen TN, Westscott-Baker L, Wu B): Compounds and compositions as modulators of GPR119 activity.WO-2008097428 (2008).
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    • 67649913242 scopus 로고    scopus 로고
    • IRM LLC (Alper PB, Lelais G, Epple R, Mutnick D, Compounds and compositions as modulators of GPR119 activity. WO-2008109702 2008
    • IRM LLC (Alper PB, Lelais G, Epple R, Mutnick D): Compounds and compositions as modulators of GPR119 activity. WO-2008109702 (2008).
  • 107
    • 67649905542 scopus 로고    scopus 로고
    • IRM LLC (Alper P, Azimioara M, Cow C, Epple R, Jiang S, Lelais G, Michellys P-Y, Mutnick D, Nikulin V, Westcott-Baker L, Compounds and compositions as modulators of GPR119 activity.WO-2009038974 2009
    • IRM LLC (Alper P, Azimioara M, Cow C, Epple R, Jiang S, Lelais G, Michellys P-Y, Mutnick D, Nikulin V, Westcott-Baker L): Compounds and compositions as modulators of GPR119 activity.WO-2009038974 (2009).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.