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Article ; Online: Target Cell Activation of a Structurally Novel NOD-Like Receptor Pyrin Domain-Containing Protein 3 Inhibitor NT-0796 Enhances Potency.

Smolak, Pamela / Nguyen, MyTrang / Diamond, Christine / Wescott, Heather / Doedens, John R / Schooley, Kenneth / Snouwaert, John N / Bock, Mark G / Harrison, David / Watt, Alan P / Koller, Beverly H / Gabel, Christopher A

The Journal of pharmacology and experimental therapeutics

2024 Volume 388, Issue 3, Page(s) 798–812

Abstract: The NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome is a central regulator of innate immunity, essential for processing and release of interleukin- ... ...

Abstract	The NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome is a central regulator of innate immunity, essential for processing and release of interleukin-1
MeSH term(s)	Humans ; Animals ; Mice ; NLR Family, Pyrin Domain-Containing 3 Protein/metabolism ; NLR Proteins ; Pyrin Domain ; Inflammasomes/metabolism ; Caspase 1/metabolism ; Esters ; Carboxylic Ester Hydrolases/metabolism ; Interleukin-1beta/metabolism
Chemical Substances	NLR Family, Pyrin Domain-Containing 3 Protein ; NLR Proteins ; Inflammasomes ; Caspase 1 (EC 3.4.22.36) ; Esters ; Carboxylic Ester Hydrolases (EC 3.1.1.-) ; Interleukin-1beta
Language	English
Publishing date	2024-02-15
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	3106-9
ISSN	1521-0103 ; 0022-3565
ISSN (online)	1521-0103
ISSN	0022-3565
DOI	10.1124/jpet.123.001941
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Article ; Online: Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders.

Harrison, David / Billinton, Andy / Bock, Mark G / Doedens, John R / Gabel, Christopher A / Holloway, M Katharine / Porter, Roderick A / Reader, Valérie / Scanlon, Jane / Schooley, Kenneth / Watt, Alan P

Journal of medicinal chemistry

2023 Volume 66, Issue 21, Page(s) 14897–14911

Abstract: The NLRP3 inflammasome is a component of the innate immune system involved in the production of proinflammatory cytokines. Neurodegenerative disorders, including Alzheimer's disease, Parkinson's disease, multiple sclerosis, and amyotrophic lateral ... ...

Abstract	The NLRP3 inflammasome is a component of the innate immune system involved in the production of proinflammatory cytokines. Neurodegenerative disorders, including Alzheimer's disease, Parkinson's disease, multiple sclerosis, and amyotrophic lateral sclerosis, have been shown to have a component driven by NLRP3 inflammasome activation. Diseases such as these with large unmet medical needs have resulted in an interest in inhibiting the NLRP3 inflammasome as a potential pharmacological treatment, but to date, no marketed drugs specifically targeting NLRP3 have been approved. Furthermore, the requirement for CNS-penetrant molecules adds additional complexity to the search for NLRP3 inflammasome inhibitors suitable for clinical investigation of neuroinflammatory disorders. We designed a series of ester-substituted carbamate compounds as selective NLRP3 inflammasome inhibitors, leading to
MeSH term(s)	Humans ; Inflammasomes/metabolism ; NLR Family, Pyrin Domain-Containing 3 Protein/physiology ; Neuroinflammatory Diseases ; Brain/metabolism ; Esters
Chemical Substances	Inflammasomes ; NLR Family, Pyrin Domain-Containing 3 Protein ; Esters
Language	English
Publishing date	2023-10-24
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.3c01398
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Article: Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors.

Harrison, David / Bock, Mark G / Doedens, John R / Gabel, Christopher A / Holloway, M Katharine / Lewis, Arwel / Scanlon, Jane / Sharpe, Andrew / Simpson, Iain D / Smolak, Pamela / Wishart, Grant / Watt, Alan P

ACS medicinal chemistry letters

2022 Volume 13, Issue 8, Page(s) 1321–1328

Abstract: The NLRP3 inflammasome is a multiprotein complex that facilitates activation and release of the proinflammatory cytokines interleukin-1β (IL-1β) and IL-18 in response to infection or endogenous stimuli. It can be inappropriately activated by a range of ... ...

Abstract	The NLRP3 inflammasome is a multiprotein complex that facilitates activation and release of the proinflammatory cytokines interleukin-1β (IL-1β) and IL-18 in response to infection or endogenous stimuli. It can be inappropriately activated by a range of danger signals resulting in chronic, low-grade inflammation underlying a multitude of diseases, such as Alzheimer's disease, Parkinson's disease, osteoarthritis, and gout. The discovery of potent and specific NLRP3 inhibitors could reduce the burden of several common morbidities. In this study, we identified a weakly potent triazolopyrimidone hit (
Language	English
Publishing date	2022-08-01
Publishing country	United States
Document type	Journal Article
ISSN	1948-5875
ISSN	1948-5875
DOI	10.1021/acsmedchemlett.2c00242
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Article ; Online: Bradykinin B1 receptor antagonists as novel analgesics: a retrospective of selected medicinal chemistry developments.

Kuduk, Scott D / Bock, Mark G

Current topics in medicinal chemistry

2008 Volume 8, Issue 16, Page(s) 1420–1430

Abstract: Bradykinin B(1) receptor antagonists embody a potentially novel approach for the treatment of chronic pain and inflammation. The identification of non-peptide B(1) antagonists has been a notable advance in the kinin field that will allow evaluation of ... ...

Abstract	Bradykinin B(1) receptor antagonists embody a potentially novel approach for the treatment of chronic pain and inflammation. The identification of non-peptide B(1) antagonists has been a notable advance in the kinin field that will allow evaluation of their therapeutic potential in the clinical realm. The current review is a high level summary of our contributions to the area that culminated in the discovery of a clinical candidate.
MeSH term(s)	Analgesics/chemistry ; Analgesics/pharmacology ; Analgesics/therapeutic use ; Animals ; Bradykinin B1 Receptor Antagonists ; Chemistry, Pharmaceutical ; Humans ; Inflammation/drug therapy ; Pain/drug therapy ; Receptor, Bradykinin B1/metabolism ; Structure-Activity Relationship
Chemical Substances	Analgesics ; Bradykinin B1 Receptor Antagonists ; Receptor, Bradykinin B1
Language	English
Publishing date	2008-10-24
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	2064823-6
ISSN	1873-4294 ; 1568-0266
ISSN (online)	1873-4294
ISSN	1568-0266
DOI	10.2174/156802608786264263
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Article ; Online: The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders.

Troxler, Thomas / Feuerbach, Dominik / Zhang, Xuechun / Yang, Charles R / Lagu, Bharat / Perrone, Mark / Wang, Tie-Lin / Briner, Karin / Bock, Mark G / Auberson, Yves P

ChemMedChem

2019 Volume 14, Issue 13, Page(s) 1238–1247

Abstract: Histamine H3 receptor (H3R) inverse agonists that have been in clinical trials for the treatment of excessive sleep disorders, have been plagued with insomnia as a mechanism-based side effect. We focused on the identification of compounds that achieve ... ...

Abstract	Histamine H3 receptor (H3R) inverse agonists that have been in clinical trials for the treatment of excessive sleep disorders, have been plagued with insomnia as a mechanism-based side effect. We focused on the identification of compounds that achieve high receptor occupancy within a short time, followed by rapid disengagement from the receptor, a target profile that could provide therapeutic benefits without the undesired side effect of insomnia. This article describes the optimization work that led to the discovery of 1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate (18 b, LML134).
MeSH term(s)	Animals ; Drug Evaluation, Preclinical ; Drug Inverse Agonism ; Half-Life ; Histamine Agonists/chemistry ; Histamine Agonists/pharmacokinetics ; Histamine Agonists/therapeutic use ; Humans ; Male ; Microsomes, Liver/metabolism ; Piperazine/chemistry ; Piperazine/pharmacokinetics ; Piperazine/therapeutic use ; Piperazines/chemistry ; Piperazines/pharmacokinetics ; Piperazines/therapeutic use ; Rats ; Rats, Sprague-Dawley ; Receptors, Histamine H3/chemistry ; Receptors, Histamine H3/metabolism ; Sleep Wake Disorders/drug therapy ; Structure-Activity Relationship
Chemical Substances	Histamine Agonists ; Piperazines ; Receptors, Histamine H3 ; Piperazine (1RTM4PAL0V)
Language	English
Publishing date	2019-05-21
Publishing country	Germany
Document type	Journal Article
ZDB-ID	2218496-X
ISSN	1860-7187 ; 1860-7179
ISSN (online)	1860-7187
ISSN	1860-7179
DOI	10.1002/cmdc.201900176
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Article: Tetrabutylammonium salt induced denitration of nitropyridines: synthesis of fluoro-, hydroxy-, and methoxypyridines.

Kuduk, Scott D / DiPardo, Robert M / Bock, Mark G

Organic letters

2005 Volume 7, Issue 4, Page(s) 577–579

Abstract: An efficient method for the synthesis of fluoropyridines via the fluorodenitration reaction is reported. The reaction is mediated by tetrabutylammonium fluoride (TBAF) under mild conditions without undue regard to the presence of water. The ... ...

Abstract	An efficient method for the synthesis of fluoropyridines via the fluorodenitration reaction is reported. The reaction is mediated by tetrabutylammonium fluoride (TBAF) under mild conditions without undue regard to the presence of water. The fluorodenitration is general for 2- or 4-nitro-substituted pyridines, while 3-nitropyridines require attendant electron-withdrawing groups for the reaction to proceed efficiently. Nitropyridines also undergo hydroxy- and methoxydenitration under mild conditions in the presence of the corresponding tetrabutylammonium species. [reaction: see text]
MeSH term(s)	Models, Molecular ; Nitrates ; Nitro Compounds/chemistry ; Pyridines/chemical synthesis ; Quaternary Ammonium Compounds
Chemical Substances	Nitrates ; Nitro Compounds ; Pyridines ; Quaternary Ammonium Compounds ; tetrabutylammonium (CBU2X6BBJR)
Language	English
Publishing date	2005-02-17
Publishing country	United States
Document type	Journal Article
ISSN	1523-7060
ISSN	1523-7060
DOI	10.1021/ol047688v
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Article ; Online: From ergolines to indoles: improved inhibitors of the human H3 receptor for the treatment of narcolepsy.

Auberson, Yves P / Troxler, Thomas / Zhang, Xuechun / Yang, Charles R / Feuerbach, Dominik / Liu, Yu-Chih / Lagu, Bharat / Perrone, Mark / Lei, Lijun / Shen, Xiaoxia / Zhang, Dushan / Wang, Chunxiu / Wang, Tie-Lin / Briner, Karin / Bock, Mark G

ChemMedChem

2015 Volume 10, Issue 2, Page(s) 266–275

Abstract: Ergolines were recently identified as a novel class of H3 receptor (H3R) inverse agonists. Although their optimization led to drug candidates with encouraging properties for the treatment of narcolepsy, brain penetration remained low. To overcome this ... ...

Abstract	Ergolines were recently identified as a novel class of H3 receptor (H3R) inverse agonists. Although their optimization led to drug candidates with encouraging properties for the treatment of narcolepsy, brain penetration remained low. To overcome this issue, ergoline 1 ((6aR,9R,10aR)-4-(2-(dimethylamino)ethyl)-N-phenyl-9-(pyrrolidine-1-carbonyl)-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinoline-7(4H)-carboxamide)) was transformed into a series of indole derivatives with high H3R affinity. These new molecules were profiled by simultaneous determination of their brain receptor occupancy (RO) levels and pharmacodynamic (PD) effects in mice. These efforts culminated in the discovery of 15 m ((R)-1-isopropyl-5-(1-(2-(2-methylpyrrolidin-1-yl)ethyl)-1H-indol-4-yl)pyridin-2(1H)-one), which has an ideal profile showing a strong correlation of PD effects with RO, and no measurable safety liabilities. Its desirably short duration of action was confirmed by electroencephalography (EEG) measurements in rats.
MeSH term(s)	Animals ; Brain/metabolism ; CHO Cells ; Cricetinae ; Cricetulus ; Electroencephalography ; Ergolines/chemistry ; Ergolines/pharmacokinetics ; Ergolines/therapeutic use ; Half-Life ; Histamine Antagonists/chemistry ; Histamine Antagonists/pharmacokinetics ; Histamine Antagonists/therapeutic use ; Humans ; Indoles/chemistry ; Indoles/pharmacokinetics ; Indoles/therapeutic use ; Male ; Mice ; Narcolepsy/drug therapy ; Narcolepsy/metabolism ; Narcolepsy/pathology ; Protein Binding ; Pyridones/chemistry ; Pyridones/pharmacokinetics ; Pyridones/therapeutic use ; Rats ; Rats, Sprague-Dawley ; Receptors, Histamine H3/chemistry ; Receptors, Histamine H3/metabolism ; Structure-Activity Relationship
Chemical Substances	1-isopropyl-5-(1-(2-(2-methylpyrrolidin-1-yl)ethyl)-1H-indol-4-yl)pyridin-2(1H)-one ; Ergolines ; Histamine Antagonists ; Indoles ; Pyridones ; Receptors, Histamine H3
Language	English
Publishing date	2015-02
Publishing country	Germany
Document type	Journal Article
ZDB-ID	2218496-X
ISSN	1860-7187 ; 1860-7179
ISSN (online)	1860-7187
ISSN	1860-7179
DOI	10.1002/cmdc.201402418
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Article ; Online: Ergoline-derived inverse agonists of the human h3 receptor for the treatment of narcolepsy.

Auberson, Yves P / Troxler, Thomas / Zhang, Xuechun / Yang, Charles R / Fendt, Markus / Feuerbach, Dominik / Liu, Yu-Chih / Lagu, Bharat / Lerchner, Andreas / Perrone, Mark / Lei, Lijun / Zhang, Chao / Wang, Chunxiu / Wang, Tie-Lin / Bock, Mark G

ChemMedChem

2014 Volume 9, Issue 8, Page(s) 1683–1696

Abstract: Ergoline derivative (6aR,9R)-4-(2-(dimethylamino)ethyl)-N-phenyl-9-(pyrrolidine-1-carbonyl)-6,6a,8,9-tetrahydroindolo[4,3-fg]quinoline-7(4H)-carboxamide (1), a CXCR3 antagonist, also inhibits human histamine H3 receptors (H3R) and represents a ... ...

Abstract	Ergoline derivative (6aR,9R)-4-(2-(dimethylamino)ethyl)-N-phenyl-9-(pyrrolidine-1-carbonyl)-6,6a,8,9-tetrahydroindolo[4,3-fg]quinoline-7(4H)-carboxamide (1), a CXCR3 antagonist, also inhibits human histamine H3 receptors (H3R) and represents a structurally novel H3R inverse agonist chemotype. It displays favorable pharmacokinetic and in vitro safety profiles, and served as a lead compound in a program to explore ergoline derivatives as potential drug candidates for the treatment of narcolepsy. A key objective of this work was to enhance the safety and efficacy profiles of 1, while minimizing its duration of action to mitigate the episodes of insomnia documented with previously reported clinical candidates during the night following administration. Modifications to the ergoline core at positions 1, 6 and 8 were systematically investigated, and derivative 23 (1-((4aR,8R,9aR)-8-(hydroxymethyl)-1-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)-4,4a,7,8,9,9a-hexahydroindolo[1,14-fg]quinolin-6(1H)-yl)ethanone) was identified as a promising lead compound. Derivative 23 has a desirable pharmacokinetic profile and demonstrated efficacy by enhancing brain concentrations of tele-methylhistamine, a major histamine metabolite. This validates the potential of the ergoline scaffold to serve as a template for the development of H3R inverse agonists.
MeSH term(s)	Animals ; Caco-2 Cells ; Cell Line ; Dogs ; Drug Inverse Agonism ; Ergolines/chemistry ; Ergolines/pharmacokinetics ; Ergolines/therapeutic use ; Half-Life ; Histamine Agonists/chemistry ; Histamine Agonists/pharmacokinetics ; Histamine Agonists/therapeutic use ; Humans ; Madin Darby Canine Kidney Cells ; Male ; Mice ; Microsomes, Liver/metabolism ; Narcolepsy/drug therapy ; Protein Binding ; Rats ; Rats, Sprague-Dawley ; Receptors, Histamine H3/chemistry ; Receptors, Histamine H3/metabolism ; Structure-Activity Relationship
Chemical Substances	1-(8-(hydroxymethyl)-1-(2-(2-methylpyrrolidin-1-yl)ethyl)-4,4a,7,8,9,9a-hexahydroindolo(1,14-fg)quinolin-6(1H)-yl)ethanone ; Ergolines ; Histamine Agonists ; Receptors, Histamine H3
Language	English
Publishing date	2014-08
Publishing country	Germany
Document type	Journal Article
ZDB-ID	2218496-X
ISSN	1860-7187 ; 1860-7179
ISSN (online)	1860-7187
ISSN	1860-7179
DOI	10.1002/cmdc.201402055
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Article ; Online: Discovery of Potent, Selective, and State-Dependent Na

Ramdas, Vidya / Talwar, Rashmi / Kanoje, Vijay / Loriya, Rajesh M / Banerjee, Moloy / Patil, Pradeep / Joshi, Advait Arun / Datrange, Laxmikant / Das, Amit Kumar / Walke, Deepak Sahebrao / Kalhapure, Vaibhav / Khan, Talha / Gote, Ganesh / Dhayagude, Usha / Deshpande, Shreyas / Shaikh, Javed / Chaure, Ganesh / Pal, Ravindra R / Parkale, Santosh /

Suravase, Sachin / Bhoskar, Smita / Gupta, Rajesh V / Kalia, Anil / Yeshodharan, Rajesh / Azhar, Mahammad / Daler, Jagadeesh / Mali, Vinod / Sharma, Geetika / Kishore, Amitesh / Vyawahare, Rupali / Agarwal, Gautam / Pareek, Himani / Budhe, Sagar / Nayak, Arun / Warude, Dnyaneshwar / Gupta, Praveen Kumar / Joshi, Parag / Joshi, Sneha / Darekar, Sagar / Pandey, Dilip / Wagh, Akshaya / Nigade, Prashant B / Mehta, Maneesh / Patil, Vinod / Modi, Dipak / Pawar, Shashikant / Verma, Mahip / Singh, Minakshi / Das, Sudipto / Gundu, Jayasagar / Nemmani, Kumar / Bock, Mark G / Sharma, Sharad / Bakhle, Dhananjay / Kamboj, Rajender Kumar / Palle, Venkata P

Journal of medicinal chemistry

2020 Volume 63, Issue 11, Page(s) 6107–6133

Abstract: Voltage-gated sodium channel ... ...

Abstract	Voltage-gated sodium channel Na
MeSH term(s)	Animals ; Chromans/chemistry ; Chromans/pharmacokinetics ; Chromans/therapeutic use ; Cytochrome P-450 CYP2C9/chemistry ; Cytochrome P-450 CYP2C9/metabolism ; Cytochrome P-450 CYP3A/chemistry ; Cytochrome P-450 CYP3A/metabolism ; Disease Models, Animal ; Drug Design ; Drug Evaluation, Preclinical ; Half-Life ; Male ; Mice ; Mice, Inbred BALB C ; NAV1.7 Voltage-Gated Sodium Channel/chemistry ; NAV1.7 Voltage-Gated Sodium Channel/metabolism ; Neuralgia/chemically induced ; Neuralgia/drug therapy ; Neuralgia/pathology ; Protein Isoforms/antagonists & inhibitors ; Protein Isoforms/metabolism ; Structure-Activity Relationship ; Sulfonamides/chemistry ; Sulfonamides/pharmacokinetics ; Sulfonamides/therapeutic use ; Voltage-Gated Sodium Channel Blockers/chemistry ; Voltage-Gated Sodium Channel Blockers/pharmacokinetics ; Voltage-Gated Sodium Channel Blockers/therapeutic use
Chemical Substances	Chromans ; NAV1.7 Voltage-Gated Sodium Channel ; Protein Isoforms ; Sulfonamides ; Voltage-Gated Sodium Channel Blockers ; Cytochrome P-450 CYP2C9 (EC 1.14.13.-) ; Cytochrome P-450 CYP3A (EC 1.14.14.1)
Language	English
Publishing date	2020-05-19
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.0c00361
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Article ; Online: Indazole derivatives as novel bradykinin B1 receptor antagonists.

Bodmer-Narkevitch, Vera / Anthony, Neville J / Cofre, Victoria / Jolly, Samson M / Murphy, Kathy L / Ransom, Richard W / Reiss, Duane R / Tang, Cuyue / Prueksaritanont, Thomayant / Pettibone, Douglas J / Bock, Mark G / Kuduk, Scott D

Bioorganic & medicinal chemistry letters

2010 Volume 20, Issue 23, Page(s) 7011–7014

Abstract: A new class of indazole-derived bradykinin B(1) antagonists and their structure-activity relationships (SAR) is reported. A number of compounds were found to have low-nanomolar affinity for the human B(1) receptor and possess acceptable P-gp and ... ...

Abstract	A new class of indazole-derived bradykinin B(1) antagonists and their structure-activity relationships (SAR) is reported. A number of compounds were found to have low-nanomolar affinity for the human B(1) receptor and possess acceptable P-gp and pharmacokinetics properties.
MeSH term(s)	ATP-Binding Cassette, Sub-Family B, Member 1 ; Bradykinin B1 Receptor Antagonists ; Humans ; Indazoles/pharmacokinetics ; Indazoles/pharmacology ; Protein Binding ; Structure-Activity Relationship
Chemical Substances	ATP-Binding Cassette, Sub-Family B, Member 1 ; Bradykinin B1 Receptor Antagonists ; Indazoles
Language	English
Publishing date	2010-12-01
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2010.09.121
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