5-HT6 receptor modulators: A patent update. Part 2. Diversity in heterocyclic scaffolds

Expert Opinion on Therapeutic Patents

Volumn 22, Issue 10, 2012, Pages 1123-1168

  Ivachtchenko, Alexandre V ^a,b   Ivanenkov, Yan A ^a,b   Skorenko, Andrey V ^b  

^a CHEMDIV INC   (United States)

^b Chemical Diversity Research Institute   (Russian Federation)

Author keywords

5 HT6R; Alzheimer's disease; Antagonists; Depression; Huntington's disease; Ligands; Obesity; Schizophrenia; Serotonin receptors

Indexed keywords

ALPHA 1A ADRENERGIC RECEPTOR; ALPHA 1B ADRENERGIC RECEPTOR; ALPHA 1D ADRENERGIC RECEPTOR; ALPHA 2A ADRENERGIC RECEPTOR; ALPHA 2B ADRENERGIC RECEPTOR; ALPHA 2C ADRENERGIC RECEPTOR; AZETIDINE DERIVATIVE; CALCIUM CHANNEL L TYPE; CHOLINESTERASE; CYCLOALKANE DERIVATIVE; DOPAMINE 1 RECEPTOR; DOPAMINE 3 RECEPTOR; DOPAMINE RECEPTOR; G PROTEIN COUPLED RECEPTOR; HETEROCYCLIC COMPOUND; HISTAMINE H1 RECEPTOR; HISTAMINE H2 RECEPTOR; HISTAMINE RECEPTOR; INDOLE DERIVATIVE; LYSERGIDE; PIPERAZINE DERIVATIVE; PIPERIDONE DERIVATIVE; SEROTONIN 1B RECEPTOR; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN 2C RECEPTOR; SEROTONIN 6 ANTAGONIST; SEROTONIN 6 RECEPTOR; SEROTONIN 7 RECEPTOR; UNINDEXED DRUG; CENTRAL NERVOUS SYSTEM AGENTS; LIGAND; SEROTONIN ANTAGONIST; SEROTONIN RECEPTOR;

ALKYLATION; ALZHEIMER DISEASE; AMYOTROPHIC LATERAL SCLEROSIS; BINDING AFFINITY; BORDERLINE STATE; BRAIN ISCHEMIA; DEGENERATIVE DISEASE; DOWN SYNDROME; HIV ASSOCIATED DEMENTIA; HUMAN; HUNTINGTON CHOREA; IC 50; ISOMERISM; LIGAND BINDING; MILD COGNITIVE IMPAIRMENT; MULTIINFARCT DEMENTIA; OBESITY; PARKINSON DISEASE; PROTEIN FUNCTION; PROTEIN STRUCTURE; PSYCHOSIS; RACEMIC MIXTURE; RADIOASSAY; RECEPTOR AFFINITY; REVIEW; STRUCTURE ACTIVITY RELATION; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECT; METABOLISM; PATENT;

ANIMALS; CENTRAL NERVOUS SYSTEM AGENTS; DRUG DISCOVERY; HETEROCYCLIC COMPOUNDS; HUMANS; LIGANDS; MOLECULAR STRUCTURE; PATENTS AS TOPIC; RECEPTORS, SEROTONIN; SEROTONIN ANTAGONISTS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84866641745     PISSN: 13543776     EISSN: 17447674     Source Type: Journal    
DOI: 10.1517/13543776.2012.722205     Document Type: Review

References (41)

1. Ivashchenko AV, Ivanenkov YA, Tkachenko SE. 5-Hydroxytryptamine subtype 6 receptor modulators: a patent survey. Expert Opin Ther Pat 2010;20:1171-96.
2. Galenea Corporation, USA. Compounds and methods of use thereof. WO019738; 2011
3. Medivation Technologies, Inc, USA. Azepino[4, 5-b]indoles and methods of use. WO051503; 2010
4. Medivation Technologies, Inc, USA. New 2, 3, 4, 5-terahydro-1H-[4, 3-b]indole compounds and methods of use thereof. WO094668; 2009
5. Medivation Technologies, Inc, USA. New tetracyclic compounds. WO055828; 2009
6. D2e, LLC, USA. Fluoro-containing derivatives of hydrogenated pyrido[4, 3-b] indole derivatives with neuroprotective and cognition enhancing properties, process for preparing and use. WO038764; 2009
7. Medivation Technologies, Inc, USA. Cyrido[4, 3-b]indoles and methods of use. WO127177; 2010
8. Kamal MA, Qu X, Yu QS, et al. Tetrahydrofurobenzofuran cymserine, a potent butyrylcholinesterase inhibitor and experimental Alzheimer drug candidate, enzyme kinetic analysis. J Neural Transm 2008;115:889-98
9. Chen X, Fang L, Liu J, Zhan CG. Reaction pathway and free energy profile for butyrylcholinesterase-catalyzed hydrolysis of acetylcholine. J Phys Chem B 2011;115:1315-22
10. Hartmann J, Kiewert C, Duysen EG, et al. Excessive hippocampal acetylcholine levels in acetylcholinesterase-deficient mice are moderated by butyrylcholinesterase activity. J Neurochem 2007;100:1421-9
11. Medivation Technologies, Inc, USA. Pyrido[4, 3-b]indoles containing rigid moieties. WO051501; 2010
12. Medivation Technologies, Inc, USA. Pyrido[4, 3-b]indoles and methods of use. WO019417; 2011
13. Medivation Technologies, Inc, USA. New 2, 3, 4, 5-tetrahydro-1H-pyrido[4, 3-b] indoles and methods of use. WO014695; 2011
14. Medivation Technologies, Inc, USA. Pyrido[4, 3-b]indole and pyrido[3, 4-b] indole derivatives and methods of use. WO103433; 2011
15. Medivation Technologies, Inc, USA. Pyrido[4, 3-b]indole and pyrido[3, 4-b] indole derivatives and methods of use. WO103487; 2011
16. Medivation Technologies, Inc, USA. Fused tetracyclic pyrido[4, 3-b]indole and pyrido[3, 4-b]indole derivatives and methods of use. WO103485; 2011
17. OOO «Innomed», Russia. Hydrogenated pyrido[4, 3-b]indole, pharmaceutical composition and methods for the production and use thereof. WO014098; 2011
18. Alla Chem, LLC, USA. Ligands for alpha-adrenoreceptors and of dopamine, histamine, imidazoline and serotonin receptors and the use thereof. WO082268; 2009
19. Alla Chem, LLC, USA. Ligand with a broad spectrum of pharmacological activity, a pharmaceutical composition, a medicinal agent and a method of treatment. WO024717; 2010
20. Ivashchenko AV, Ivashchenko AA, Savchuk NF. Ligand with wide range of simultaneous receptor activity, pharmaceutical composition, method of preparing said composition and medicinal agent. RU2374245; 2009
21. Volk B, Gacsalyi I, Pallagi K, et al. Optimization of (arylpiperazinylbutyl) oxindoles exhibiting selective 5-HT7 receptor antagonist activity. J Med Chem 2011;54:6657-69
22. Egis Gyogyszergyar Nyilvanosan Mukoedo Reszvenytarsasag, HU. Optically active 3-[(phenylpiperazin-1-yl)alkyl]-3-alkyl-oxindole derivatives having CNS activity. WO089616; 2010.
23. Janssen Pharmaceutica NV, Belg. Serotonin receptor modulators. WO059393; 2010
24. Janssen Pharmaceutica NV, Belg. Ciperazin-1-yl trifluoromethyl- substituted-pyridine as fast dissociating dopamine 2 receptor antagonists. WO012758; 2010
25. Instytut Farmakologii Polskiej Akademii Nauk, Pol. New 4, 6-disubstituted 2-(4-methylpiperazin-l-yl)pyridine derivatives, a process for their preparation, pharmaceutical composition containing these compounds, their use, a method for modulating monoaminergic receptor activity and a monoaminergic receptor modulating agent. WO053388; 2010
26. Schering Corp, USA. Gamma-secretase modulators for the treatment of Alzheimer's disease. WO108766; 2009 23.
27. Schering Corporation, USA. Gamma secretase modulators. WO073777; 2009
28. Pfizer Inc, USA. Pyridinyl amides for treatment of CNS and metabolic disorders. US0197859; 2009
29. Janssen Pharmaceutica NV, Belg. Preparation of 2-aminopyrimidine compounds as serotonin receptor modulators. WO053825; 2010
30. Janssen Pharmaceutica NV, Belg. Substituted 6-(1-piperazinyl)pyridazines as 5-HT6 receptor antagonists. WO000456; 2010
31. Abbott Gmbh & Co. KG, Germany. Quinoline compounds suitable for treating that respond to modulation of the serononin serotonin 5-HT6 receptor. WO019286; 2009
32. Schering Corporation, USA. Gamma secretase modulators. WO073779; 2009
33. Boehringer Ingelheim International G.m.b.H, Germany. Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture. WO007300; 2009
34. Dainippon Sumitomo Pharma Co, Ltd, Japan. N-Acyl cyclic amine derivative or pharmaceutically acceptable salt thereof. WO111875; 2011
35. Abbott Laboratories, USA. Modulators of 5-HT receptors and methods of use thereof. WO124042; 2010
36. Abbott Laboratories, USA. Modulators of 5-HT receptors and methods of use thereof. WO135560; 2010
37. Abbott Laboratories, USA. Modulators of 5-HT receptors and methods of use thereof. US0130382; 2011
38. Ivachtchenko AV, Ivanenkov YA. 5-HT6 receptor antagonists: a patent update. Part 1. Sulfonyl derivatives. Expert Opin Ther Pat 2012;22:917-64.
39. Pullagurla MR, Westkaemper RB, Glennon RA. Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors. Bioorg Med Chem Lett 2004;14:4569-73
40. Lopez-Rodriguez ML, Benhamu B, de la Fuente T, et al. A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists. J Med Chem 2005;48:216-4219
41. Ivachtchenko AV, Ivanenkov YA. 5HT (6) receptor antagonists: a patent update. Part 1. Sulfonyl derivatives. Expert Opin. Ther Pat 2012;22:917-64