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公开(公告)号：US11485696B2
公开(公告)日：2022-11-01
申请号：US16071709
申请日：2017-01-22
发明人： Jian Zhang , Dehui Jiang , Xiaojun Shen
IPC分类号： C07C45/51 , C07C45/42 , C07C249/16 , C07C49/713 , C07C49/753 , C07C251/84
摘要： This invention relates to a method for producing a high-purity cyclohexenone long-chain alcohol represented by formula I, and produces the compound of formula I by a metal-mediated Barbier reaction. The method of the present invention has advantages in its short scheme, high yield, and high-purity product, and is suitable for industrial scale up.
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公开(公告)号：US20220226291A1
公开(公告)日：2022-07-21
申请号：US17614074
申请日：2020-05-28
发明人： Hiroyuki Ueno , Sayaka Tsukioka
IPC分类号： A61K31/4245 , A61K39/395 , A61P35/00
摘要： This invention provides a method for enhancing antitumor effects of a ribonucleotide reductase (RNR) inhibitory compound. A pharmaceutical composition for treating and/or preventing a tumor used in combination with an immune checkpoint molecule regulator comprising a sulfonamide compound represented by Formula (I) or a salt thereof is also provided.
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13.发明申请公开(公告)号：US20220125793A1
公开(公告)日：2022-04-28
申请号：US17434573
申请日：2020-02-28
IPC分类号： A61K31/519 , A61K39/395 , A61P35/00
摘要： The problem to be solved by the present disclosure is to provide a novel combination therapy using (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof, the combination therapy exhibiting an excellent antitumor effect on cancer patients with resistance to immune checkpoint inhibitors. The present disclosure provides an antitumor agent comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient, the antitumor agent being administered in combination with an immune checkpoint inhibitor, except for pembrolizumab, to a cancer patient with resistance to immune checkpoint inhibitors.
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公开(公告)号：US20210387990A1
公开(公告)日：2021-12-16
申请号：US17292289
申请日：2019-11-08
发明人： Masashi KONDO
IPC分类号： C07D487/04
摘要： A method for producing a compound represented by formula (A-1) or a salt thereof, the method comprising reacting (S)-3-((3,5-dimethoxyphenyl)ethynyl)-1-(pyrrolidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine or a salt thereof with a compound represented by formula (I-1-A). Formula (I-1-A) and formula (A-1) are as described in the specification.
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公开(公告)号：US20210236613A1
公开(公告)日：2021-08-05
申请号：US17255672
申请日：2019-06-28
发明人： Yuki TANAKA
IPC分类号： A61K39/00 , A61K47/65 , A61K39/395 , A61P35/00
摘要： Provided is a novel cancer treatment method that exhibits a significantly excellent antitumor effect and causes less adverse reactions. The present invention provides an antitumor agent wherein a peptide having 4 linked epitopes and an immune checkpoint modulator are administered in combination. An antitumor effect in humans can be evaluated by providing a cell coexpressing an epitope peptide of a human tumor antigen derived from SART2 and human HLA-A24.
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公开(公告)号：US20210177850A1
公开(公告)日：2021-06-17
申请号：US17190068
申请日：2021-03-02
发明人： Kenichiro YOSHIDA
IPC分类号： A61K31/513 , A61K31/506 , A61K31/7072 , A61P13/12 , A61P35/00
摘要： A method for treating cancer in patients with creatinine clearance of 15 mL/min or more and less than 30 mL/min, including dividing a combination drug containing α,α,α-trifluorothymidine (FTD) and 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride in a molar ratio of 1:0.5, in a dose of 30 to 50 mg/m2/day as FTD-equivalent, into two to four times a day, and orally administering it to the patient.
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公开(公告)号：US11028069B2
公开(公告)日：2021-06-08
申请号：US16472000
申请日：2017-12-22
发明人： Morihiro Mitsuya
IPC分类号： C07D401/14 , A61K9/00 , A61P35/00
摘要： An object of the present invention is to provide a salt of the compound 1-(2,3-dichlorobenzoyl)-4-((5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl)methyl)piperidine-4-carboxylic acid, useful as an antitumor agent, and crystals thereof which are excellent in solubility, stability, and oral absorption and can be produced in large quantities. The present invention relates to a hydrochloride salt of 1-(2,3-dichlorobenzoyl)-4-((5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl)methyl)piperidine-4-carboxylic acid and crystals of the hydrochloride salt having characteristic peaks at particular diffraction angles in powder X-ray diffraction spectrum.
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公开(公告)号：US20210161908A1
公开(公告)日：2021-06-03
申请号：US17047436
申请日：2019-04-18
申请人： NATIONAL UNIVERSITY CORPORATION TOKYO UNIVERSITY OF AGRICULTURE AND TECHNOLOGY , TAIHO PHARMACEUTICAL CO., LTD.
发明人： Masaki INADA , Daisuke KAJIWARA
IPC分类号： A61K31/5377
摘要： This invention relates to a preventive and/or therapeutic agent for sarcopenia, comprising a prostaglandin D2 production inhibitor as an active ingredient.
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公开(公告)号：US11014930B2
公开(公告)日：2021-05-25
申请号：US16855226
申请日：2020-04-22
IPC分类号： C07D487/04 , C07D519/00 , A61P35/04 , A61K31/519 , A61K31/5377
摘要： The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.
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公开(公告)号：US20210030738A1
公开(公告)日：2021-02-04
申请号：US16645315
申请日：2018-09-06
发明人： Tomonori HARUMA
IPC分类号： A61K31/47 , A61K39/395 , A61P35/00
摘要： The present invention is intended to provide a novel antitumor agent that shows marked antitumor effects with reduced side effects. The present invention relates to an antitumor agent characterized by coadministration of an acyl thiourea compound represented by general formula (I) or a salt thereof, and an immune checkpoint molecule regulator.
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