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1.发明公开公开(公告)号：US20240293414A1
公开(公告)日：2024-09-05
申请号：US18634241
申请日：2024-04-12
IPC分类号： A61K31/519 , A61K38/09 , A61P15/00
CPC分类号： A61K31/519 , A61K38/09 , A61P15/00
摘要： The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated on the patient's level of anti-Müllerian hormone (AMH) or β17-estradiol (E2).
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2.发明公开公开(公告)号：US20240000785A1
公开(公告)日：2024-01-04
申请号：US18244773
申请日：2023-09-11
IPC分类号： A61K31/519 , A61P5/00 , A61K31/565 , A61K31/57
CPC分类号： A61K31/519 , A61K31/57 , A61K31/565 , A61P5/00
摘要： The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.
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公开(公告)号：US11759464B2
公开(公告)日：2023-09-19
申请号：US16619702
申请日：2018-06-05
申请人： ObsEva S.A.
IPC分类号： A61K31/519 , A61K31/565 , A61P5/00 , A61K31/57
CPC分类号： A61K31/519 , A61K31/565 , A61K31/57 , A61P5/00
摘要： The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.
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公开(公告)号：US20230286998A1
公开(公告)日：2023-09-14
申请号：US18004353
申请日：2021-07-05
发明人： Hideki TAKEUCHI , Kazumichi JO
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , C07B2200/13
摘要： An object of the present invention is to provide a compound which has high storage stability and is suitable for use as a drug substance. The present invention relates to a succinate salt of 1-{[(4aR,6R,8aR)-2-amino-3-cyano-8-methyl-4,4a,5,6,7,8,8a,9-octahydrothieno[3,2-g]quinolin-6-yl]carbonyl}-3-[2-(dimethylamino)ethyl]-1-propylurea, which is suitable as a drug substance having excellent storage stability and crystallinity and is useful for the treatment or prevention of Parkinson's disease, restless legs syndrome, hyperprolactinemia or the like.
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公开(公告)号：US11596644B2
公开(公告)日：2023-03-07
申请号：US17041577
申请日：2019-03-28
IPC分类号： A61K31/706 , A61K31/7056 , A61P3/08 , A61K31/702
摘要： Disclosed herein are methods, sodium-dependent glucose transporter (SGLT)1 compounds and compositions for the treatment of postprandial hypoglycemia, postprandial hypoglycemia that occurs as a consequence of gastric surgery.
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公开(公告)号：US20210046078A1
公开(公告)日：2021-02-18
申请号：US16843260
申请日：2020-04-08
发明人： Takuro Dan , Hideomi Takahashi , Yu Kuramochi
IPC分类号： A61K31/519 , A61P15/00 , A61P29/00
摘要： An object of the present invention is to provide pharmaceutical agents that reduce risk for decrease in bone mineral density due to their effect of reducing estrogen levels and exert excellent therapeutic effects on endometriosis. The present invention relates to pharmaceutical compositions for treating endometriosis comprising 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid or a pharmaceutically acceptable salt thereof, which are administered orally once a day at a daily dose of between 50 mg and 75 mg calculated as a free form.
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公开(公告)号：US20190002414A1
公开(公告)日：2019-01-03
申请号：US15781925
申请日：2016-12-06
IPC分类号： C07D241/04 , C07D211/32 , C07D401/06 , A61P1/08
CPC分类号： C07D241/04 , A61K31/451 , A61K31/495 , A61P1/08 , C07D211/32 , C07D211/62 , C07D401/06
摘要： A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, and thus is useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting.A compound represented by the formula (I): wherein W represents a fluorine atom and the like, ring A represents a cycloalkyl and the like, X1 represents CH or N, R represents methyl and the like, Y represents 0 to 2, U1, U2 and U3 each independently represents a single bond and the like, or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have an excellent NK1 receptor antagonist activity, and thus are also useful as an agent for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting.
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公开(公告)号：US20180312566A1
公开(公告)日：2018-11-01
申请号：US16034648
申请日：2018-07-13
IPC分类号： C07K14/735 , C12N15/09 , A61K38/16 , C07K16/18 , C07K14/705 , C07K19/00
CPC分类号： C07K14/70535 , A61K38/16 , C07K14/705 , C07K16/18 , C07K19/00 , C07K2319/30 , C12N15/09
摘要： Provided is an Fc fusion high affinity IgE receptor α-chain having excellent stability at low pH. An Fc fusion protein comprising: (i) a high affinity IgE receptor α-chain; and (ii) an Fc region of IgG1, wherein a linker fragment region between the (i) and the (ii) is the amino acid sequence shown in SEQ ID NO: 2.
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公开(公告)号：US20170320821A1
公开(公告)日：2017-11-09
申请号：US15659760
申请日：2017-07-26
发明人： Hitoshi Inoue , Kohsuke Ohno , Tetsuya Nakamura , Yusuke Ohsawa
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： [Problem] The present invention provides a novel compound having an S1P1 receptor antagonistic activity.[Solution] The present invention provides a compound represented by the general formula (I): (in the formula, Rl, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds of the present invention have an excellent S1P1 receptor antagonistic activity and therefore are useful as an agent for the treatment or prevention of antoimmune diseases and the like.
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公开(公告)号：US20160129031A1
公开(公告)日：2016-05-12
申请号：US14995489
申请日：2016-01-14
IPC分类号： A61K31/7056
CPC分类号： A61K31/7056 , C07H17/02
摘要： The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.
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