公开(公告)号：WO2014145781A1

公开(公告)日：2014-09-18

申请号：PCT/US2014/030604

申请日：2014-03-17

Applicant: LIPOCINE INC.

Inventor： NACHAEGARI, Satish Kumar ,  GILIYAR, Chandrashekar ,  PATEL, Raj ,  NACHIAPPAN, Chidambaram ,  VENKATESHWARAN, Srinivansan ,  PATEL, Mahesh V.

IPC: A61K31/56 ,  A61K31/568 ,  A61P5/26

CPC classification number: A61K31/568 ,  A61K9/0053 ,  A61K9/2004 ,  A61K9/4841 ,  A61K31/575 ,  A61K47/12 ,  A61K47/14 ,  A61K47/44

Abstract: The present disclosure is drawn to oral pharmaceutical compositions and dosage forms containing select testosterone esters and related methods. In one embodiment of the present invention, an oral pharmaceutical composition for administration to subjects in need of testosterone is provided. The composition comprises a testosterone ester and a pharmaceutically acceptable carrier. The testosterone ester can have the structure wherein R is -C 13 H 25 O or -C 14 H 27 O. One or both of the esters can be present in the pharmaceutical composition. The composition is formulated such that upon single dose administration to a group of human subject, the composition provides a mean serum testosterone C avg t12-t24 that is within about 35% to about 70% of the mean serum testosterone C avg t0-t24.

Abstract translation: 本公开涉及含有选择性睾酮酯的口服药物组合物和剂型及相关方法。 在本发明的一个实施方案中，提供了用于给予需要睾酮的受试者的口服药物组合物。 组合物包含睾酮酯和药学上可接受的载体。 睾酮酯可以具有其中R为-C 13 H 25 O或-C 14 H 27 O的结构。 药物组合物中可以存在一种或两种酯。 组合物被配制成使得当向一组人受试者单剂量给药时，组合物提供平均血清睾酮Cavg t12-t24，其平均血清睾酮Cavg t0-t24的约35％至约70％。

公开(公告)号：WO2014093818A2

公开(公告)日：2014-06-19

申请号：PCT/US2013/075006

申请日：2013-12-13

Applicant: BIOJECT, INC.

Inventor： LOGOMASINI, Mark, A.

IPC: A61M5/30 ,  A61K31/568

CPC classification number: A61M5/30 ,  A61K9/0019 ,  A61K31/568

Abstract: Embodiments herein are directed to methods for increasing testosterone levels in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of testosterone by needle-free injection to an injection site. Some embodiments are further directed to a method of increasing testosterone levels in a subject in need thereof, by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of testosterone and a pharmaceutically acceptable carrier by needle-free injection. Some embodiments are directed to a method of minimizing fluctuations in testosterone levels in a subject diagnosed with hypogonadism, comprising serially administering to the subject a therapeutically effective amount of testosterone by needle-free injection to an injection site.

Abstract translation: 本文的实施方案涉及用于在有需要的受试者中增加睾酮水平的方法，包括通过无针注射向注射部位施用治疗有效量的睾酮。 一些实施方案进一步涉及通过向受试者施用包含治疗有效量的睾酮和药学上可接受的载体的药物组合物，通过无针注射来增加有此需要的个体中睾酮水平的方法。 一些实施方案涉及使被诊断患有性腺机能减退症的受试者的睾酮水平的波动最小化的方法，其包括通过无针注射向注射部位向受试者施用治疗有效量的睾酮。

公开(公告)号：WO2012079092A3

公开(公告)日：2012-12-06

申请号：PCT/US2011064495

申请日：2011-12-12

Applicant: LIPOCINE INC ,  CHICKMATH BASAWARAJ ,  GILIYAR CHANDRASHEKAR ,  NACHIAPPAN CHIDAMBARAM ,  PATEL MAHESH V ,  VENKATESHWARAN SRINIVANSAN

Inventor： CHICKMATH BASAWARAJ ,  GILIYAR CHANDRASHEKAR ,  NACHIAPPAN CHIDAMBARAM ,  PATEL MAHESH V ,  VENKATESHWARAN SRINIVANSAN

IPC: A61K47/48 ,  A61K9/14 ,  A61K9/16 ,  A61K31/138 ,  A61K31/568

CPC classification number: A61K9/2031 ,  A61K9/14 ,  A61K9/146 ,  A61K9/148 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/1694 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/282 ,  A61K9/2853 ,  A61K9/286 ,  A61K9/2866 ,  A61K9/4866 ,  A61K9/4875 ,  A61K31/568 ,  A61K47/10 ,  A61K47/36 ,  A61K47/38 ,  A61K47/40

Abstract: The present disclosure is drawn to pharmaceutical compositions and oral dosage forms containing testosterone undecanoate, as well as related methods of treatment. In one embodiment, the oral dosage form can include a therapeutically effective amount of testosterone undecanoate and a pharmaceutically acceptable carrier. The dosage form can be formulated such that, when measured using a USP Type II apparatus in 1000 mL of 8 wt% Triton X-100 in water at 37C and 100 rpm, the oral dosage form releases at least 20% more testosterone undecanoate after the first 120 minutes than an equivalent dose testosterone undecanoate containing oral dosage form without the pharmaceutically acceptable carrier.

Abstract translation: 本公开涉及含有睾酮十一烷酸酯的药物组合物和口服剂型以及相关的治疗方法。 在一个实施方案中，口服剂型可以包含治疗有效量的十一酸睾酮和药学上可接受的载体。 可以配制剂型，使得当使用USP II型仪器在1000mL的8wt％Triton X-100在37℃和100rpm的水中测量时，口服剂型释放至少20％的十一酸睾酮 比含有不含药学上可接受的载体的口服剂型的等当量睾酮十一烷酸酯首先120分钟。

公开(公告)号：WO2012156820A1

公开(公告)日：2012-11-22

申请号：PCT/IB2012001112

申请日：2012-05-15

Applicant: TRIMEL PHARMACEUTICALS CORP ,  KREPPNER WAYNE ,  FOGARTY SIOBHAN ,  OBEREGGER WERNER ,  MAES PAUL JOSE PIERRE MARIE

Inventor： KREPPNER WAYNE ,  FOGARTY SIOBHAN ,  OBEREGGER WERNER ,  MAES PAUL JOSE PIERRE MARIE

IPC: A61K9/00 ,  A61K9/06 ,  A61K31/568 ,  A61K47/34 ,  A61K47/44 ,  A61P5/26

CPC classification number: A61K47/34 ,  A61K9/0043 ,  A61K31/568 ,  A61K47/44

Abstract: The present invention relates to pernasal testosterone bio-adhesive gel formulations for intranasal administration and testosterone replacement treatment methods for using the pernasal testosterone bio-adhesive gel formulations for providing sustained intranasal delivery of testosterone to testosterone deficient males to treat, for example, male subjects diagnosed with hypogonadism.

Abstract translation: 本发明涉及用于鼻内给药的经鼻睾酮生物粘合剂凝胶制剂和用于使用经鼻睾酮生物粘合凝胶制剂的睾酮替代治疗方法，用于向睾酮缺乏的男性提供持续的鼻内递送睾酮以治疗例如被诊断的男性受试者 伴有性腺功能减退症。

公开(公告)号：WO2012083201A1

公开(公告)日：2012-06-21

申请号：PCT/US2011/065552

申请日：2011-12-16

Applicant: HARBOR BIOSCIENCES, INC. ,  WHITE, Steven, K. ,  JANSEN, Erin, E.

Inventor： WHITE, Steven, K. ,  JANSEN, Erin, E.

IPC: A61K31/568 ,  C07J1/00

CPC classification number: C07J1/00 ,  A61K31/568 ,  C07J1/0022

Abstract: The invention relates to solid state forms of androst-5-ene-3α,7β,16α,17β- tetrol, formulations containing or prepared from such solid state forms and use of these materials for modulating unwanted inflammation including acute and chronic non-productive inflammation. The formulations can be used to prevent, treat or slow the progression of conditions related to autoimmunity and metabolic disorders such as arthritis, multiple sclerosis, ulcerative colitis, Type 1 diabetes and Type 2 diabetes.

Abstract translation: 本发明涉及含有或由这种固态形式制备的雄甾-5-烯-3a，7β，16a，17β-四醇的固体形式，并且这些物质用于调节不希望的炎症，包括急性和慢性非生产性炎症 。 制剂可用于预防，治疗或减缓与自身免疫和代谢紊乱如关节炎，多发性硬化，溃疡性结肠炎，1型糖尿病和2型糖尿病有关的病症的进展。

公开(公告)号：WO2012075081A3

公开(公告)日：2012-06-07

申请号：PCT/US2011/062538

申请日：2011-11-30

Applicant: LIPOCINE INC. ,  GILIYAR, Chandrashekar ,  CHICKMATH, Basawaraj ,  NACHIAPPAN, Chidambaram ,  PATEL, Mahesh V. ,  VENKATESHWARAN, Srinivansan

Inventor： GILIYAR, Chandrashekar ,  CHICKMATH, Basawaraj ,  NACHIAPPAN, Chidambaram ,  PATEL, Mahesh V. ,  VENKATESHWARAN, Srinivansan

IPC: A61K31/568 ,  A61K9/48 ,  A61P3/10 ,  A61P9/00

Abstract: The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods of treatment. In one embodiment, the present invention provides for a pharmaceutical composition that includes a therapeutically effective amount of testosterone undecanoate and a solubilizer. The testosterone undecanoate is solubilized in the composition and is present in an amount such that it comprises about 14 wt% to about 35 wt% of the total composition.

公开(公告)号：WO2011051354A3

公开(公告)日：2012-03-01

申请号：PCT/EP2010066283

申请日：2010-10-27

Applicant: BESINS HEALTHCARE LU SARL ,  MASINI-ETEVE VALERIE ,  CANET DENIS

Inventor： MASINI-ETEVE VALERIE ,  CANET DENIS

IPC: A61K47/10 ,  A61K9/06 ,  A61K9/08 ,  A61K31/565 ,  A61K31/568 ,  A61K31/57 ,  A61K47/12 ,  A61K47/14

CPC classification number: A61K31/56 ,  A61K9/0014 ,  A61K9/06 ,  A61K31/565 ,  A61K31/566 ,  A61K31/568 ,  A61K31/57 ,  A61K31/573 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

Abstract: The present invention provides compositions and methods for providing sustained release of an active agent through the skin of a subject, wherein a pharmaceutical percutaneous composition comprises at least one fatty acid ester and a therapeutically effective amount of active agent.

Abstract translation: 本发明提供了用于通过受试者皮肤持续释放活性剂的组合物和方法，其中药物经皮组合物包含至少一种脂肪酸酯和治疗有效量的活性剂。

公开(公告)号：WO2011138460A1

公开(公告)日：2011-11-10

申请号：PCT/EP2011/057387

申请日：2011-05-09

Applicant: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) ,  RAFESTIN-OBLIN, Marie-Edith ,  ALAMI, Mouad ,  LOOSFELT, Hugues ,  HAMZE, Abdallah ,  KHAN, Ali Junaid ,  TIKAD, Abdellatif ,  LOMBES, Marc ,  BRION, Jean-Daniel

Inventor： RAFESTIN-OBLIN, Marie-Edith ,  ALAMI, Mouad ,  LOOSFELT, Hugues ,  HAMZE, Abdallah ,  KHAN, Ali Junaid ,  TIKAD, Abdellatif ,  LOMBES, Marc ,  BRION, Jean-Daniel

IPC: A61K31/56 ,  A61K31/567 ,  A61K31/568 ,  A61K31/5685 ,  A61K31/569 ,  A61K31/57 ,  A61K31/575 ,  C07J1/00 ,  C07J9/00 ,  C07J11/00 ,  C07J63/00 ,  A61P15/04 ,  A61P15/18 ,  A61P35/00

CPC classification number: C07J63/008 ,  A61K31/56 ,  A61K31/567 ,  A61K31/568 ,  A61K31/5685 ,  A61K31/569 ,  A61K31/57 ,  A61K31/575 ,  C07J1/0011 ,  C07J1/0022 ,  C07J1/0025 ,  C07J3/00 ,  C07J7/0005 ,  C07J7/002 ,  C07J7/007 ,  C07J9/00 ,  C07J11/00 ,  C07J21/006

Abstract: The present invention relates to a compound of formula (I): for its use as progesterone receptor antagonist, in particular for its use for the prevention and/or the treatment of cancer or uterine pathologies.

Abstract translation: 本发明涉及式（I）化合物：其用作孕激素受体拮抗剂，特别是其用于预防和/或治疗癌症或子宫病变的用途。

公开(公告)号：WO2011133475A2

公开(公告)日：2011-10-27

申请号：PCT/US2011032929

申请日：2011-04-18

Applicant: STANFORD RES INST INT ,  CHAO WAN-RU ,  COLLINS NATHAN ,  SAMBUCETTI LIDIA ,  DINH DOMINIC

Inventor： CHAO WAN-RU ,  COLLINS NATHAN ,  SAMBUCETTI LIDIA ,  DINH DOMINIC

IPC: A61K31/56 ,  A61K9/20 ,  A61K9/22 ,  A61K9/70 ,  A61K31/568 ,  A61P35/00

CPC classification number: A61K45/06 ,  A61K31/57

Abstract: The disclosure provides compositions and methods for treating multiple myeloma. In some embodiments, the compositions comprise (E)-3-hydroxy-21-[2'-(N,N-dimethylamino)ethoxy]-19-norpregna-1,3,5(10),17(20)-tetraene or a pharmaceutically acceptable salt or prodrug thereof and a pharmaceutical carrier.

Abstract translation: 本公开提供了治疗多发性骨髓瘤的组合物和方法。 在一些实施方案中，组合物包含（E）-3-羟基-21- [2' - （N，N-二甲基氨基）乙氧基] -19-去甲基-1,3,5（10），17（20） - 四烯 或其药学上可接受的盐或前药和药物载体。

公开(公告)号：WO2010075175A1

公开(公告)日：2010-07-01

申请号：PCT/US2009/068535

申请日：2009-12-17

Applicant: QUEST DIAGNOSTICS INVESTMENTS INCORPORATED ,  GOLDMAN, Mildred M. ,  CLARKE, Nigel J.

Inventor： GOLDMAN, Mildred M. ,  CLARKE, Nigel J.

IPC: A61K31/568 ,  C12Q1/68

CPC classification number: G01N33/743 ,  G01N30/724 ,  G01N33/6848 ,  G01N33/6851 ,  G01N2458/15 ,  H01J49/00 ,  H01J49/0027

Abstract: Methods are provided for detecting the amount of one or more HRT panel analytes (i.e., estrone (E1), estrone sulfate (E1s), 17α-estradiol (E2a), 17 β -estradiol (E2b), estradiol sulfate (E2s), estriol (E3), equilin (EQ), 17α-dihydroequilin (EQa), 17 β -dihydroequilin (EQb), Equilenin (EN), 17α-dihydroequilenin (ENa), 17 β -dihydroequilenin (ENb), and Δ8,9-dehydroestrone (dE1)) in a sample by mass spectrometry. The methods generally involve ionizing one or more HRT panel analytes in a sample and quantifying the generated ions to determine the amount of one or more HRT panel analytes in the sample. In methods where amounts of multiple HRT panel analytes are detected, the amounts of multiple analytes are detected in the same sample injection.

Abstract translation: 提供了用于检测一种或多种HRT面板分析物（即雌酮（E1），硫酸雌酮（E1）），17α-雌二醇（E2a），17β-雌二醇（E2b），硫酸雌二醇（E2s），雌三醇 E3），平衡（EQ），17α-二氢赖氨酸（EQa），17β-二氢等位基因（EQb），平衡蛋白（EN），17a-二氢马来西林（ENa），17β-二氢马来西林（ENb）和δ8,9-脱水雌酮 ））。 所述方法通常涉及将样品中的一种或多种HRT面板分析物离子化并量化产生的离子以确定样品中一种或多种HRT面板分析物的量。 在检测到多个HRT面板分析物的量的方法中，在相同的样品注入中检测到多种分析物的量。