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Agyin J.K.,University of Texas Health Science Center at San Antonio | Santhamma B.,Evestra Inc. | Roy S.S.,University of Texas Health Science Center at San Antonio
Bioorganic and Medicinal Chemistry Letters | Year: 2013

Multiple myeloma (MM) is an incurable neoplasm characterized by devastating and progressive bone destruction. Standard chemotherapeutic agents have not been effective at significantly prolonging the survival of MM patients and these agents are typically associated with often severe, dose-limiting side effects. There is great need for methods to target the delivery of novel, effective cytotoxic agents specifically to bone, where myeloma cells reside. We have synthesized and evaluated the effects of the bone-targeted proteasome inhibitors PS-341-BP-1, PS-341-BP-2 and MG-262-BP on cell proliferation using the mouse 5TGM1 and human RPMI 8226 cell lines in vitro. The compounds exhibit strong cytotoxicity on MM cell lines and reduce the number of viable cells in a dose dependent manner. © 2013 Elsevier Ltd. All rights reserved.


MAHWAH, N.J., March 1, 2017 /PRNewswire/ -- Glenmark Pharmaceuticals Inc., USA, and Evestra, Inc. have completed a strategic development, license and commercialization agreement to develop and market a generic version of Merck's & Co.'s NuvaRing® product – etonogestrel/ethinyl...


Ahmed G.,Evestra Inc. | Nickisch K.,Evestra Inc.
Steroids | Year: 2016

The synthesis of 17α-hydroxy steroids generally requires multiple synthetic manipulations. The synthesis of 17α-estradiol is no exception, as this process involves the protection and release of the 3-hydroxy functional group. The diastereoselective reduction of the 17-keto-steroid can be utilized to prepare 17α-hydroxy-steroids. Here, 17α-estradiol was synthesized from commercially available estrone under thermodynamic Meerwein-Ponndorf-Verley (MPV) conditions in a single step, followed by simple chromatographic separation over silica gel. The remaining mixture of unreacted estrone and estradiols was easily recycled through Oppenauer oxidation to estrone, with an overall yield of 68% 17α-estradiol. © 2016 Elsevier Inc. All rights reserved.


A range of 6-, 7-, and 11-substituted estradiols were synthesized by the selective aromatization of the A-ring of 19-nor steroids using phenylselenyl halides followed by oxidation with hydrogen peroxide. Established methods utilizing copper(II) halides failed or have given poor yields with these substrates. © 2013 Elsevier Ltd. All rights reserved.


Patent
Evestra Inc. | Date: 2014-07-11

Various prodrug compounds having the general structure: Active agent-(acid)-(linker)-SO_(2)NR_(1)R_(2 )are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.


Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.


Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2.


Trademark
Evestra Inc. | Date: 2011-02-15

Pharmaceutical products for female health care, namely, pharmaceutical products for the treatment of breast cancer; pharmaceutical products for female fertility control, namely, oral pharmaceutical contraception products; pharmaceutical products for female fertility control, namely, pharmaceutical products for stimulating fertility; pharmaceutical products for female contraception, namely, oral contraceptives; pharmaceutical products for female hormone replacement therapy; pharmaceutical products for treating edometriosis; pharmaceutical products for treating fibroids; and pharmaceutical products for female oncology.


Trademark
Evestra Inc. | Date: 2011-03-29

Pharmaceutical products for female health care, namely, pharmaceutical products for female fertility control, namely, oral pharmaceutical contraception products; pharmaceutical products for female fertility control, namely, pharmaceutical products for stimulating fertility; and pharmaceutical products for female contraception, namely, oral contraceptives.


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