公开(公告)号：WO2023046283A1

公开(公告)日：2023-03-30

申请号：PCT/EP2021/076120

申请日：2021-09-22

Applicant: FUNDACIÓ INSTITUT DE RECERCA BIOMÈDICA (IRB BARCELONA) ,  UNIVERSITAT DE BARCELONA ,  INSTITUCIÓ CATALANA DE RECERCA I ESTUDIS AVANÇATS ,  PROVINCIAL HEALTH SERVICES AUTHORITY

Inventor： SALVATELLA GIRALT, Xavier ,  RIERA ESCALÉ, Antoni ,  FRIGOLÉ VIVAS, Marta ,  SÁNCHEZ ZARZALEJO, Carolina ,  RUFFONI, Alessandro ,  VERDAGUER ESPAULELLA, Francesc Xavier ,  SADAR, Marianne Dorothy ,  BANUELOS, Carmen Adriana ,  MAWJI, Nasrin

IPC: A61K31/09 ,  A61K31/519 ,  A61P5/26 ,  A61P5/28 ,  A61P35/00

Abstract: The present invention relates to compounds of formula (I) and their use for modulating the transcriptional activity of the androgen receptor and its splice variants for treating various indications including prostate cancer

公开(公告)号：WO2022271951A1

公开(公告)日：2022-12-29

申请号：PCT/US2022/034726

申请日：2022-06-23

Applicant: UNIVERSITY OF IOWA RESEARCH FOUNDATION ,  SLUKA, Kathleen A. ,  LESNAK, Joseph ,  SALEM, Aliasger K. ,  NAKHLA, David

Inventor： SLUKA, Kathleen A. ,  LESNAK, Joseph ,  SALEM, Aliasger K. ,  NAKHLA, David

IPC: A61K9/16 ,  A61P29/00 ,  A61K31/167 ,  A61P5/26 ,  A61K31/277 ,  A61K31/40 ,  A61K31/404 ,  A61K31/541 ,  A61K9/0019 ,  A61K9/1635 ,  A61K9/1647

Abstract: A sustained release composition comprising one or more particles comprising a polymer and an amount of a select androgen receptor modulator (SARM), and methods of making and using the composition, are provided.

公开(公告)号：WO2022241404A1

公开(公告)日：2022-11-17

申请号：PCT/US2022/072213

申请日：2022-05-09

Applicant: TRUSTEES OF DARTMOUTH COLLEGE

Inventor： MICALIZIO, Glenn C. ,  BURRIS, Thomas

IPC: A61K47/28 ,  A61K31/56 ,  A61K31/58 ,  A61P5/26

Abstract: The present disclosure relates to polycyclic (e.g., fused tetracyclic) liver X receptor (LXR) modulators, synthetic methods for preparing such LXR modulators, and methods of using such LXR modulators to treat a disease or condition that would benefit from LXR modulation. Exemplary compounds have quaternary centers at C9 and C13 and a substituted sulfonamide moiety at C16.

公开(公告)号：WO2022104413A1

公开(公告)日：2022-05-27

申请号：PCT/AU2021/051361

申请日：2021-11-17

Applicant: DAY, Bryce Nicholas

Inventor： DAY, Bryce Nicholas

IPC: A61K31/4155 ,  A61K31/277 ,  A61K31/568 ,  A61P15/00 ,  A61P5/28 ,  A61P21/06 ,  A61P5/26 ,  A61K31/5685

Abstract: Provided herein are compositions, methods and kits for effectively preventing, treating, reducing, mitigating, or controlling female sexual interest and arousal disorder (FSIAD), wherein the method comprises administering to a subject in need thereof (i) a non-steroidal anti-androgen drug having minimal blood-brain-barrier penetration in a dosage that completely or partially blocks peripheral androgen receptors; and (ii) a supra-physiological dose of an anabolic androgenic steroid (AAS), a pro-drug, precursor or pro-hormone of an AAS, or a selective androgen receptor modulator (SARM).

公开(公告)号：WO2022017515A1

公开(公告)日：2022-01-27

申请号：PCT/CN2021/108229

申请日：2021-07-23

Applicant: 中国医学科学院医药生物技术研究所

Inventor： 胡来兴 ,  王天琦 ,  周金明 ,  刘永华 ,  吴萌 ,  李鑫

IPC: C07D231/12 ,  C07D233/61 ,  C07D261/08 ,  C07D277/28 ,  C07D401/04 ,  A61P5/26 ,  A61P35/00 ,  A61P13/08 ,  A61P15/00 ,  A61P17/08 ,  A61P17/10 ,  A61P17/00 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/42 ,  A61K31/426

Abstract: 本申请提供一种双芳香基胺类化合物及其制备方法和应用，该化合物具有式1的结构，R 1选自C1－12的烷基、C1－6的烷氧基、卤素、C1－3的卤代烷基、-CN、-NO2、-NH2、磺酰基或芳香基；R5为一个以上且R5和R2选自氢、C1－12的烷基、C1－6的烷氧基、卤素、C1－3的卤代烷基、-CN、-NO2、-NH2、磺酰基或芳香基；R3选自取代或未取代的五元杂环或六元杂环；Linker选自-SO2NR4-、-CONR4-、-NR4-，R4选自氢、C1－12的烷基；V、W、X、Y、Z独立地选自碳或者氮。本申请提供的双芳香基胺类化合物具有抑制雄激素受体的活性。

公开(公告)号：WO2020198712A1

公开(公告)日：2020-10-01

申请号：PCT/US2020/025545

申请日：2020-03-27

Applicant: ESSA PHARMA, INC. ,  THE UNIVERSITY OF BRITISH COLUMBIA ,  PROVINCIAL HEALTH SERVICES AUTHORITY

Inventor： VIRSIK, Peter ,  ZHOU, Han-Jie ,  SADAR, Marianne Dorothy ,  ANDERSEN, Raymond John ,  KUNZHONG, Jian ,  GOLEC, Daniel Andrew

IPC: A61K31/075 ,  C07C43/164 ,  A61P5/26 ,  A61P5/28

Abstract: The present disclosure generally relates to pharmaceutical compositions and combinations comprising an androgen receptor N-terminal domain inhibitor or an inhibitor and a second therapeutically active agent, such as an CDK4/6 inhibitor, a Pin1 inhibitor (inhibitor of peptidyl-prolyl cis/trans isomerases), or an antiandrogen. In particular, the present disclosure relates to pharmaceutical compositions and combintaions useful for treatment of various cancers, for example breast cancer and prostate cancer. Further, the present disclosure relates administering an androgen receptor N-terminal domain inhibitor in combination with radiation therapy for treatment of various cancers.

公开(公告)号：WO2020012315A1

公开(公告)日：2020-01-16

申请号：PCT/IB2019/055772

申请日：2019-07-07

Applicant: BUZZELET DEVELOPMENT AND TECHNOLOGIES LTD.

Inventor： RAZ, Noa ,  EYAL, Aharon ,  RAZ, Carmi

IPC: A61K31/352 ,  A61K31/015 ,  A61K47/38 ,  A61P31/04 ,  A61P5/26 ,  A61P13/02 ,  A61P13/08 ,  A61P15/08 ,  A61P15/10

Abstract: A terpene-enriched composition for treating conditions and/or symptoms associated therewith in a male subject is described, which composition comprises at least one cannabinoid in a specific amount, a primary terpene in a specific amount, at least 5% by weight of a non-cannabinoid, non-terpene, carrier, and optionally at least three secondary terpenes, wherein said non-cannabinoid, non-terpene carrier comprises cellulose and a weight/weight ratio of a total amount of terpenes to a total amount of cannabinoids in said composition is from about 0.1:1 to about 1:1 or wherein said non-cannabinoid, non-terpene carrier comprises less than 5% by weight cellulose and a weight/weight ratio of a total amount of terpenes to a total amount of cannabinoids in said compositions is from about 0.05:1 to about 1:1. Conditions and/or symptoms associated therewith are selected from the group consisting of androgen deficiency, male infertility, male urogenital or reproductive system infections and/or disorders.

公开(公告)号：WO2019088010A1

公开(公告)日：2019-05-09

申请号：PCT/JP2018/040065

申请日：2018-10-29

Applicant: 帝國製薬株式会社

Inventor： 川上　智 ,  堀川　靖

IPC: A61K31/568 ,  A61K9/70 ,  A61K47/02 ,  A61K47/10 ,  A61K47/14 ,  A61K47/24 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P5/26 ,  A61P5/50 ,  A61P9/10 ,  A61P15/10 ,  A61P15/12 ,  A61P19/10 ,  A61P21/00 ,  A61P25/24 ,  A61P25/28

Abstract: 本発明は、テストステロンの皮膚透過性に優れ、かつ製剤の物性に優れたテストステロン含有経皮投与製剤を提供する。具体的には、本発明は、膏体中に、テストステロン；ポリアクリル酸またはその塩；増粘剤；架橋剤；プロピレングリコールを含む可塑剤；および乳酸エステル、を含む経皮投与製剤を提供する。

公开(公告)号：WO2017187375A1

公开(公告)日：2017-11-02

申请号：PCT/IB2017/052430

申请日：2017-04-27

Applicant: SOCHIM INTERNATIONAL S.P.A.

Inventor： EIGENMANN, Carlo ,  DE LEO, Vincenzo

IPC: A61K31/047 ,  A61K31/519 ,  A61K31/593 ,  A61K33/24 ,  A61K36/61 ,  A61P5/26 ,  A61P43/00

Abstract: A composition for the treatment of polycystic ovary syndrome, as well as the endocrine-gynecological and metabolic disorders associated therewith are described. In particular, the composition of the invention comprises inositol and extract of banaba that have shown to be significantly effective as adjuvant in the treatment of this syndrome.

Abstract translation: 描述了用于治疗多囊卵巢综合征的组合物，以及与之相关的内分泌 - 妇科和代谢疾病。 具体而言，本发明的组合物包含肌醇和巴拿巴提取物，其已显示在治疗该综合征方面显着有效作为佐剂。

公开(公告)号：WO2016040234A1

公开(公告)日：2016-03-17

申请号：PCT/US2015/048801

申请日：2015-09-08

Applicant: ELI LILLY AND COMPANY

Inventor： BENSON, Charles Thomas

IPC: A61K31/4439 ,  A61P5/26 ,  A61P19/08 ,  A61P21/06 ,  A61P21/00

CPC classification number: A61K31/4439 ,  C07D209/94 ,  C07D401/06

Abstract: The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I: [Formula should be inserted here] or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明提供了一种治疗与雄激素剥夺疗法相关的症状的方法，包括向需要这种治疗的患者施用有效量的式I化合物：[式中应插入此处]或其药学上可接受的盐。