4-Alkyl- and 3,4-dialkyl-1,2,3,4,-tetrahydro-8-pyridono[5,6-g]quinolines: Potent, nonsteroidal androgen receptor agonists

Higuchi, Robert I.; Edwards, James P.; Caferro, Thomas R.; Ringgenberg, Josef D.; Kong, James W.; Hamann, Lawrence G.; Arienti, Kristen L.; Marschke, Keith B.; Davis, Robert L.; Farmer, Luc J.; Jones, Todd K.

doi:10.1016/s0960-894x(99)00186-9

Cited by 52 publications

(23 citation statements)

References 12 publications

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“…The acyclic 32 (generic structure III) and cyclic amidines (33)(34)(35)(36)(37)(38)(39) (generic structure IV) described in both patents of Bayer are a newly described pharmacophore for binding to the progesterone receptor. Although, acyclic compounds are described, the majority of the amidines are based on (multi)cyclic structures which have a high level of lipophilicity.…”

Section: Medicinal Chemistrymentioning

confidence: 99%

Non-Steroidal Steroid Receptor Modulators

Buijsman¹,

Hermkens²,

Rijn³

et al. 2005

CMC

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The last ten years much attention has been focused on the finding of non-steroidal ligands for steroidal nuclear receptors for reasons such as diminishing cross-reactivity to eliminate side effect profiles, changing physicochemical properties which might cause different tissue distribution profiles and altering binding modes which influence the binding of cofactors. Compounds with a selective functionality profile are referred to as selective nuclear receptor modulators (e.g., SARMs or SPRMs). In the following paragraphs non-steroidal ligands which have full or partial agonistic activity will be described for the following receptors: PR, GR, AR, LXR and FXR.

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Section: Medicinal Chemistrymentioning

confidence: 99%

Non-Steroidal Steroid Receptor Modulators

Buijsman¹,

Hermkens²,

Rijn³

et al. 2005

CMC

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“…Key features of the SAR and PK properties of the quinolone and coumarin series are summarized below [46][47][48][49][50]:…”

Section: A Linear Tricyclic and Tetracyclic Analogsmentioning

confidence: 99%

Selective Androgen Receptor Modulators in Drug Discovery: Medicinal Chemistry and Therapeutic Potential

Cadilla¹,

Turnbull²

2006

CTMC

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Modulation of the androgen receptor has the potential to be an effective treatment for hypogonadism, andropause, and associated conditions such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and sexual dysfunction. Side effects associated with classical anabolic steroid treatments have driven the quest for drugs that demonstrate improved therapeutic profiles. Novel, non-steroidal compounds that show tissue selective activity and improved pharmacokinetic properties have been developed. This review provides an overview of current advances in the development of selective androgen receptor modulators (SARMs).

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“…Ligand Pharm., Inc. was an early leader in the development of nonsteroidal AR ligands with their series of tricyclic quinolines [18][19][20]. Ligand Pharm.…”

Section: Tricyclic Quinoline Sarms (Ligand Pharm Inc) 321 Tricycmentioning

confidence: 99%

Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates

Mohler¹,

Nair²,

Hwang³

et al. 2005

Expert Opinion on Therapeutic Patents

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The androgen receptor (AR) is a nuclear hormone receptor that, upon binding to testosterone, dihydrotestosterone (DHT) and other endogenous androgens, supports the development, growth and maintenance of masculine features through activation of anabolic and androgenic metabolism. The AR has been demonstrated to be a productive therapeutic target. AR ligands in clinical practice include androgenic steroids, antiandrogenic steroids and antiandrogenic nonsteroidals. Of primary importance for this review are nonsteroidal selective AR modulators (SARMs) that have tissue-specific agonist and/or antagonist activities. The AR has a myriad of peripheral and central functions that can be modulated in a pleiotropic and tissue-specific fashion using the increasingly diverse collection of SARMs discussed herein. This suggests that SARMs will have a high level of clinical utility for a wide variety of health conditions. The patent literature focusing on SARMs is reviewed and reveals multiple chemical classes in various stages of preclinical and clinical development. Emphasis is placed on selected disease states for which SARMs show potential for therapeutic use in clinical practice.

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4-Alkyl- and 3,4-dialkyl-1,2,3,4,-tetrahydro-8-pyridono[5,6-g]quinolines: Potent, nonsteroidal androgen receptor agonists

Cited by 52 publications

References 12 publications

Non-Steroidal Steroid Receptor Modulators

Non-Steroidal Steroid Receptor Modulators

Selective Androgen Receptor Modulators in Drug Discovery: Medicinal Chemistry and Therapeutic Potential

Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates

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