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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2007-11-6
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pubmed:abstractText |
We have continued to explore spirobenzazepines as vasopressin receptor antagonists to follow up on RWJ-339489 (2), which had advanced into preclinical development. Further structural modifications were pursued to find a suitable backup compound for human clinical studies. Thus, we identified carboxylic acid derivative 3 (RWJ-676070; JNJ-17158063) as a potent, balanced vasopressin V(1a)/V(2) receptor antagonist with favorable properties for clinical development. Compound 3 is currently undergoing human clinical investigation.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:ChenRobert HRH,
pubmed-author:DamianoBruce PBP,
pubmed-author:DemarestKeith TKT,
pubmed-author:GunnetJoseph WJW,
pubmed-author:LookRichardR,
pubmed-author:MaryanoffBruce EBE,
pubmed-author:McComseyDavid FDF,
pubmed-author:MinorLisa KLK,
pubmed-author:PatelMonaM,
pubmed-author:RybczynskiPhilip JPJ,
pubmed-author:VillaniFrank JFJ,
pubmed-author:WangYuanpingY,
pubmed-author:XiangMin AmyMA,
pubmed-author:ZhangHan-ChengHC,
pubmed-author:ZhongH MarlonHM
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6623-8
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pubmed:meshHeading |
pubmed-meshheading:17942308-Animals,
pubmed-meshheading:17942308-Antihypertensive Agents,
pubmed-meshheading:17942308-Benzazepines,
pubmed-meshheading:17942308-Drug Evaluation, Preclinical,
pubmed-meshheading:17942308-Female,
pubmed-meshheading:17942308-Humans,
pubmed-meshheading:17942308-Male,
pubmed-meshheading:17942308-Rats,
pubmed-meshheading:17942308-Rats, Long-Evans,
pubmed-meshheading:17942308-Receptors, Vasopressin,
pubmed-meshheading:17942308-Spiro Compounds,
pubmed-meshheading:17942308-Vasopressins
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pubmed:year |
2007
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pubmed:articleTitle |
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.
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pubmed:affiliation |
Research and Early Development, Johnson & Johnson Pharmaceutical Research & Development, 8 Clarke Drive, Cranbury, NJ 08512, USA.
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pubmed:publicationType |
Journal Article,
Comparative Study
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