San Diego, CA, United States

Seragon Pharmaceuticals

seragonpharm.com
San Diego, CA, United States
SEARCH FILTERS
Time filter
Source Type

Patent
Seragon Pharmaceuticals | Date: 2017-08-16

Described herein are compounds of formulae (I) and (VI) that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.


PubMed | Vanderbilt Ingram Cancer Center, Vanderbilt University, Seragon Pharmaceuticals and Genentech
Type: | Journal: eLife | Year: 2016

ER-targeted therapeutics provide valuable treatment options for patients with ER+ breast cancer, however, current relapse and mortality rates emphasize the need for improved therapeutic strategies. The recent discovery of prevalent ESR1 mutations in relapsed tumors underscores a sustained reliance of advanced tumors on ER signaling, and provides a strong rationale for continued targeting of ER. Here we describe GDC-0810, a novel, non-steroidal, orally bioavailable selective ER downregulator (SERD), which was identified by prospectively optimizing ER degradation, antagonism and pharmacokinetic properties. GDC-0810 induces a distinct ER conformation, relative to that induced by currently approved therapeutics, suggesting a unique mechanism of action. GDC-0810 has robust in vitro and in vivo activity against a variety of human breast cancer cell lines and patient derived xenografts, including a tamoxifen-resistant model and those that harbor ER mutations. GDC-0810 is currently being evaluated in Phase II clinical studies in women with ER+ breast cancer.


Rix P.J.,Seragon Pharmaceuticals | Vick A.,WIL Research | Attkins N.J.,Parexel International | Barker G.E.,Aires Pharmaceuticals | And 9 more authors.
Clinical Pharmacokinetics | Year: 2015

Introduction: The efficacy of nebulized sodium nitrite (AIR001) has been demonstrated in animal models of pulmonary arterial hypertension (PAH), but it was not known if inhaled nitrite would be well tolerated in human subjects at exposure levels associated with efficacy in these models.Methods: Inhaled nebulized sodium nitrite was assessed in three independent studies in a total of 82 healthy male and female subjects. Study objectives included determination of the maximum tolerated dose (MTD) and dose-limiting toxicity (DLT) under normal and mildly hypoxic conditions, and following co-administration with steady-state sildenafil, assessment of nitrite pharmacokinetics, and evaluation of the fraction exhaled nitric oxide (FENO) and concentrations of iron-nitrosyl hemoglobin (Hb(Fe)-NO) and S-nitrosothiols (R-SNO) as biomarkers of local and systemic NO exposure, respectively.Results: Nebulized sodium nitrite was well tolerated following 6 days of every 8 h administration up to 90 mg, producing significant increases in circulating Hb(Fe)-NO, R-SNO, and FENO. Pulmonary absorption of nitrite was rapid and complete, and plasma exposure dose was proportional through the MTD dosage level of 90 mg, without accumulation following repeated inhalation. At higher dosage levels, DLTs were orthostasis (observed at 120 mg) and hypotension with tachycardia (at 176 mg), but venous methemoglobin did not exceed 3.0 % at any time in any subject. Neither the tolerability nor pharmacokinetics of nitrite was impacted by conditions of mild hypoxia, or co-administration with sildenafil, supporting the safe use of inhaled nitrite in the clinical setting of PAH.Conclusion: On the basis of these results, nebulized sodium nitrite (AIR001) has been advanced into randomized trials in PAH patients. © 2014, The Author(s).


Patent
Seragon Pharmaceuticals | Date: 2013-03-14

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.


Patent
Seragon Pharmaceuticals | Date: 2012-12-14

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.


Patent
Seragon Pharmaceuticals | Date: 2012-12-14

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.


Patent
Seragon Pharmaceuticals | Date: 2013-12-20

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.


Patent
Seragon Pharmaceuticals | Date: 2014-05-28

A compound that has the structure of Formula (XII):X^(1) is CH, CR^(3) or N;X^(2) is N, CH, or CR^(3);Z is -OH or -OR^(10);R^(2) is C_(1)-C_(4)alkyl, C_(1)-C_(4)fluoroalkyl, C_(1)-C_(4)deuteroalkyl, C_(3)-C_(6)cycloalkyl, or -C_(1)-C_(4)alkylene-W;W is hydroxy, halogen, CN, C_(1)-C_(4)alkyl, C_(1)-C_(4)haloalkyl, C_(1)-C_(4)alkoxy, C_(1)-C_(4)haloalkoxy, and C_(3)-C_(6)cycloalkyl;each R^(3) is independently halogen, C_(1)-C_(4)alkyl, or C_(1)-C_(4)fluoroalkyl;each R^(4) is independently halogen, -CN, -OR^(9), -S(=O)_(2)R^(10), C_(1)-C_(4)alkyl, C_(1)-C_(4)fluoroalkyl, or C_(1)-C_(4)heteroalkyl;each R^(5) is independently halogen, -CN, -OR^(9), -S(=O)_(2)R^(10), C_(1)-C_(4)alkyl, C_(1)-C_(4)fluoroalkyl, or C_(1)-C_(4)heteroalkyl;R^(6) is H, C_(1)-C_(4)alkyl, or halogen;R^(7) is H, C_(1)-C_(4)alkyl, or halogen;R^(9) is H, C_(1)-C_(6)alkyl, C_(1)-C_(6)fluoroalkyl, or C_(3)-C_(6)cycloalkyl;R^(10) is C_(1)-C_(6)alkyl;m is 0, 1, or 2;n is 0, 1, 2, 3, or 4; andp is 0, 1, or 2;or a pharmaceutically acceptable or N-oxide thereof.


News Article | December 5, 2014
Site: www.xconomy.com

Amid String of Exits for VenBio, a Founding Partner Leaves, Too With three acquisitions of its portfolio companies, San Francisco biotech investment firm venBio has had a few good exits recently. Now one of its partners is exiting, too. Kurt Von Emster, one of four venBio founders, has decamped for Abingworth, a life science venture firm with a much longer history and global reach. Abingworth made the announcement early Friday, but as of this writing von Emster is still listed as a partner on the venBio website. In a statement, von Emster (pictured) lauded Abingworth’s 40 year track record and called its “multifaceted platform of investment opportunities” impressive. There was no mention of venBio. Von Emster did not immediately respond to a request for comment. Abingworth, headquartered in London, said von Emster will work in the firm’s Menlo Park, CA, office, and work on investments across all stages, from early private venture to public investments, where he has previous experience. Before he cofounded venBio, von Emster ran a hedge fund at MPM Capital that made public and private investments. VenBio has made at least two investments in public companies. Earlier this year it led a $52 million funding of Aurinia Pharmaceuticals, based in Victoria, BC, with von Emster joining the company’s board. (He is still listed as a board member.) In 2012, venBio led an attempt to recapitalize and turn around the fortunes of struggling Swiss immunotherapy firm Cytos Biotechnology. It did not go well. After a key trial failure in asthma earlier this year, Cytos decided to wind down operations and is looking to sell its underlying technology. (Abingworth was one of venBio’s coinvestors in the Cytos recapitalization.) However, Cytos has been the only obvious pothole in venBio’s young record. Formed in 2011 with a $180 million inaugural fund, venBio has had three big exits: The $200 million sale of Labrys Biologics to Teva Pharmaceutical, the $650 million sale of Aragon Pharmaceuticals to Johnson & Johnson, and the $725 billion sale of Seragon Pharmaceuticals to Roche’s Genentech division. (Seragon was formed around a breast-cancer drug that J&J didn’t take as part of the Aragon purchase.) All the deals had milestone payments attached that could push the final payouts much higher. The initial returns from Labrys and Aragon alone put the fund “in positive territory,” as venBio partner Corey Goodman told Xconomy in June. Goodman also said the activity has spurred venBio to seek a second fund of $250 million to $300 in size, with the same philosophy: “We won’t start companies assuming they’ll have IPOs. We’re assuming M&A.” Reached today, Goodman acknowledged von Emster’s departure but said venBio had no comment. The firm has also made a long-term bet on Solstice Biologics, a San Diego startup whose scientific cofounder Steve Dowdy has created a new way to deliver RNA-based drugs into cells that, if successful, could widen the use of treatments in the relatively new field. Solstice is the exclusive licensee of the intellectual property from Dowdy’s University of California, San Diego, lab.

Loading Seragon Pharmaceuticals collaborators
Loading Seragon Pharmaceuticals collaborators