124results about "Ketal steroids" patented technology

Methods of using 7α,11β-dimethyl-17β-hydroxyestra-4,14-dien-3-one (III)and 17 esters thereof for various hormonal therapies, oral and parenteral dosage forms comprising these actives, and processes for their preparation.

Provided are methods of evaluating or treating a patient, e.g., a patient having a disorder described herein, comprising: a) optionally, acquiring a patient sample; b) acquiring an evaluation of and / or evaluating the sample for an alteration in the level S24(S)-hydroxycholesterol compared to a reference standard.

The invention provides a preparation method of ulipristal acetate (compound I), a key intermediate (compound of formula IV) for preparing the ulipristal acetate and the preparation of the key intermediate. The preparation method comprises the following steps: easy-to-get 3, 3-(ethylenedioxy group)-19-norpregn-5 (10), 9 (11)-diolefin-3, 17-diketone (compound II) and a cyanation reagent are additively reacted to obtain a compound III, then 17alpha-hydroxyl is protected to obtain the compound of formula IV, then the compound is reacted with a methyllithium or methyl Grignard reagent and hydrolyzed through acid to obtain the compound of formula V, the compound is reacted with ethylene glycol through the catalysis of p-toluene sulphonic acid and the like to obtain a compound VI, then the compound VI is epoxidized to obtain an epoxide VII which is then reacted with a Grignard reagent to obtain a compound VIII, a compound IX is obtained after hydrolysis under an acid condition, and finally the ulipristal acetate is obtained through acetylization, which is disclosed in the reaction formula, wherein R in the reaction formula is defined in the specification.

(3alpha,3beta)-disubstituted 17beta steroidal compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, are provided for the prevention and treatment of a variety of CNS-related conditions.

The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl. In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat meningiomas; to treat uterine leiomyomas; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce cervical ripening; to induce labor; and for contraception.

Compounds are provided according to Formula (I):and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3a, R3b, R4, R5a, R5b, R6a, and R6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.