公开(公告)号：US20240238209A1

公开(公告)日：2024-07-18

申请号：US18621501

申请日：2024-03-29

申请人： ESTETRA SRL

发明人： Séverine Francine Isabelle JASPART ,  Johannes Jan PLATTEEUW ,  Denny Johan Marijn VAN DEN HEUVEL

IPC分类号： A61K9/20 ,  A61K9/00 ,  A61K31/565 ,  A61P5/00 ,  A61P15/18 ,  A61K9/16

CPC分类号： A61K9/2095 ,  A61K9/0056 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2077 ,  A61K31/565 ,  A61P5/00 ,  A61P15/18 ,  A61K9/1623

摘要： The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of:



0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and
75-99.9 wt. % of one or more pharmaceutically acceptable ingredients;


the solid dosage unit comprising at least 100 μg of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 μm to 50 μm.


The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

公开(公告)号：US11964055B2

公开(公告)日：2024-04-23

申请号：US17504087

申请日：2021-10-18

申请人： ESTETRA SRL

发明人： Séverine Francine Isabelle Jaspart ,  Johannes Jan Platteeuw ,  Denny Johan Marijn Van Den Heuvel

IPC分类号： A61K9/20 ,  A61K9/00 ,  A61K9/16 ,  A61K31/565 ,  A61P5/00 ,  A61P15/18

CPC分类号： A61K9/2095 ,  A61K9/0056 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2077 ,  A61K31/565 ,  A61P5/00 ,  A61P15/18 ,  A61K9/1623

摘要： The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 μg of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 μm to 50 μm. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

公开(公告)号：US20230293442A1

公开(公告)日：2023-09-21

申请号：US18196617

申请日：2023-05-12

申请人： ESTETRA SRL

发明人： Séverine Francine Isabelle JASPART ,  Johannes Jan PLATTEEUW ,  Denny Johan Marijn VAN DEN HEUVEL

IPC分类号： A61K9/20 ,  A61K9/00 ,  A61K31/565 ,  A61P5/00 ,  A61P15/18

CPC分类号： A61K9/2095 ,  A61K9/0056 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2077 ,  A61K31/565 ,  A61P5/00 ,  A61P15/18 ,  A61K9/1623

摘要： The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt.% of estetrol particles containing at least 80 wt.% of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt.% of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 µg of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 µm to 50 µm. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

公开(公告)号：US20230248743A1

公开(公告)日：2023-08-10

申请号：US18107703

申请日：2023-02-09

申请人： ESTETRA SRL

发明人： Jean-Michel FOIDART ,  Maud JOST

IPC分类号： A61K31/585 ,  A61P15/18 ,  A61K31/565

CPC分类号： A61K31/585 ,  A61P15/18 ,  A61K31/565

摘要： Described are methods of providing contraception in a woman having a BMI≥30.0 kg/m2, comprising: selecting a woman determined to have a BMI≥30.0 kg/m2, and then orally administering to the selected woman a therapeutically effective amount of an estetrol component at a daily dose of from 14 mg to 16 mg, based on the estetrol moiety, and drospirenone at a daily dose of from 2.5 mg to 3.5 mg. Also described are methods of contraception that achieves a Pearl Index of

公开(公告)号：US11666585B2

公开(公告)日：2023-06-06

申请号：US17963712

申请日：2022-10-11

申请人： ESTETRA SRL

发明人： Melanie Taziaux ,  Glwadys Rausin ,  Maud Jost ,  Marie Mawet

IPC分类号： A61K31/565 ,  A61K31/585 ,  A61P15/12 ,  A61K9/00 ,  A61K31/55 ,  A61K31/57 ,  A61K31/573

CPC分类号： A61K31/585 ,  A61K9/0053 ,  A61K31/55 ,  A61K31/565 ,  A61K31/57 ,  A61K31/573 ,  A61P15/12

摘要： The present invention relates to a hormone replacement therapy, to the associated compounds and to the associated packaging units, for alleviating menopause-associated symptoms which is based on the administration to a female mammal of an estetrol component at specified daily doses, optionally in combination with a progestogenic component.
The therapy enjoys a statistically significant efficacy combined with a favourable profile for side effects compared to currently available methods for alleviating menopause-associated symptoms.

公开(公告)号：US20230041304A1

公开(公告)日：2023-02-09

申请号：US17937215

申请日：2022-09-30

申请人： ESTETRA SRL

发明人： Maud JOST ,  Glwadys RAUSIN

IPC分类号： A61K31/585 ,  A61K31/565 ,  A61P15/00 ,  A61K31/566

摘要： The present invention relates to a method for the management of dysmenorrhea involving administration of an estrogenic component which is preferably selected from the group consisting of estetrol and estetrol-like compounds. Estetrol-like compounds have been surprisingly found to be capable of mitigating dysmenorrhea, either when used alone or in combination with progestogenic components, and this to an extent surpassing the effect obtained with other compositions and with a favourable side-effect profile compared to currently available methods.

公开(公告)号：US20220211722A1

公开(公告)日：2022-07-07

申请号：US17701588

申请日：2022-03-22

申请人： ESTETRA SRL

发明人： Jean-Michel FOIDART

IPC分类号： A61K31/567 ,  A61K31/585 ,  A61K31/565 ,  A61P15/18

摘要： The present invention relates to a combined oral contraceptive with a reduced risk for side effects, including a reduced risk for QT interval prolongation, a reduced risk for testosterone decrease and a reduced risk for elevated C-reactive protein levels when compared to other combined oral contraceptives. The estetrol/drospirenone combined oral contraceptive described herein shows favorable pharmacokinetics for the progestogenic component. Use of a specific estrogenic component in the combined oral contraceptive entails multiple benefits over currently available combined oral contraceptives.

公开(公告)号：US20230031329A1

公开(公告)日：2023-02-02

申请号：US17893999

申请日：2022-08-23

申请人： ESTETRA SRL

发明人： Melanie Taziaux ,  Glwadys Rausin ,  Maud Jost ,  Marie Mawet

IPC分类号： A61K31/585 ,  A61P15/12 ,  A61K9/00 ,  A61K31/55 ,  A61K31/565 ,  A61K31/57 ,  A61K31/573

摘要： The present invention relates to a hormone replacement therapy, to the associated compounds and to the associated packaging units, for alleviating menopause-associated symptoms which is based on the administration to a female mammal of an estetrol component at specified daily doses, optionally in combination with a progestogenic component.
The therapy enjoys a statistically significant efficacy combined with a favourable profile for side effects compared to currently available methods for alleviating menopause-associated symptoms.

公开(公告)号：US20230025785A1

公开(公告)日：2023-01-26

申请号：US17900576

申请日：2022-08-31

申请人： ESTETRA SRL

发明人： Melanie Taziaux ,  Glwadys Rausin ,  Maud Jost ,  Marie Mawet

IPC分类号： A61K31/585 ,  A61K9/00 ,  A61K31/55 ,  A61P15/12 ,  A61K31/57 ,  A61K31/573 ,  A61K31/565

摘要： The present invention relates to a hormone replacement therapy, to the associated compounds and to the associated packaging units, for alleviating menopause-associated symptoms which is based on the administration to a female mammal of an estetrol component at a specific daily dose, optionally in combination with a progestogenic component. The therapy enjoys a statistically significant efficacy combined with a favourable profile for side effects compared to currently available methods for alleviating menopause-associated symptoms.

公开(公告)号：US11957694B2

公开(公告)日：2024-04-16

申请号：US16883052

申请日：2020-05-26

申请人： ESTETRA SRL

发明人： Séverine Francine Isabelle Jaspart ,  Johannes Jan Platteeuw ,  Denny Johan Marijn Van Den Heuvel

IPC分类号： A61K31/565 ,  A61K9/00 ,  A61K9/20

CPC分类号： A61K31/565 ,  A61K9/0056 ,  A61K9/006 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2072 ,  A61K9/2077 ,  A61K9/2095

摘要： An orodispersible solid pharmaceutical dosage unit of estetrol is disclosed. The solid dosage unit is easy to manufacture and suited for sublingual, buccal or sublabial administration. The orodispersible solid pharmaceutical dosage unit can include at least 100 μg of an estetrol component and pharmaceutically acceptable excipients. Methods of manufacturing the orodispersible solid pharmaceutical dosage unit are also disclosed.