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公开(公告)号：US10351624B2
公开(公告)日：2019-07-16
申请号：US15502088
申请日：2015-08-06
发明人： Tomoaki Komai , Takako Kimura , Daichi Baba , Yoshikuni Onodera , Kento Tanaka , Takashi Kagari , Anri Aki , Nobumi Nagaoka
摘要： It is intended to provide a therapeutic and/or prophylactic agent for transplant rejections, immunological diseases, allergic diseases, inflammatory diseases, thrombosis, cancers, etc., targeting human Orai1. The present invention provides, for example, a pharmaceutical composition comprising an antibody that specifically recognizes human Orai1 and has the activity of inhibiting human T cell activation.
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公开(公告)号：US20190175551A1
公开(公告)日：2019-06-13
申请号：US16136318
申请日：2018-09-20
发明人： Kiyoshi Arai , Tsuyoshi Homma , Tomoko Sawanobori , Shin Nakajima , Rie Hisatomi , Motonobu Yoshimura
摘要： Provided is a pharmaceutical composition for treating a renal disease. The pharmaceutical composition for treating a renal disease comprises a mineralocorticoid receptor antagonist.
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公开(公告)号：US10316026B2
公开(公告)日：2019-06-11
申请号：US15760411
申请日：2016-11-04
发明人： Kohei Kadota , Tsuyoshi Ueda
IPC分类号： C07D213/76 , C07D239/69 , C07D277/52 , C07D403/12
摘要： In a method for producing a de-dimethoxybenzylated compound by removing a dimethoxybenzyl group from a compound containing a dimethoxybenzyl group bonded to a nitrogen atom in the presence of an acid, the de-dimethoxybenzylated compound is obtained by removing the dimethoxybenzyl group without forming a poorly soluble product resulting from the removed dimethoxybenzyl group. The de-dimethoxybenzylation reaction is carried out in the presence of triphenylphosphine or diethylthiourea.
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公开(公告)号：US20190144559A1
公开(公告)日：2019-05-16
申请号：US16256715
申请日：2019-01-24
发明人： Toshinori Agatsuma , Shu Takahashi , Jun Hasegawa , Daisuke Okajima , Hirofumi Hamada , Miki Yamaguchi
IPC分类号： C07K16/30 , A61K47/68 , A61K31/4745
摘要： It is intended to provide an antitumor drug having an excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. There is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-TROP2 antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(═O)— wherein the anti-TROP2 antibody is connected to the terminal of L1, and the antitumor compound is connected to the carbonyl group of the —(CH2)n2-C(═O)— moiety with the nitrogen atom of the amino group at position 1 as a connecting position.
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公开(公告)号：US20190092741A1
公开(公告)日：2019-03-28
申请号：US16088696
申请日：2017-03-29
发明人： Keiji Saito , Katsuyoshi Nakajima , Toru Taniguchi , Osamu Iwamoto , Satoshi Shibuya , Yasuyuki Ogawa , Kazumasa Aoki , Nobuya Kurikawa , Shinji Tanaka , Momoko Ogitani , Eriko Kioi , Kaori Ito , Natsumi Nishihama , Tsuyoshi Mikkaichi , Wataru Saitoh
IPC分类号： C07D307/94 , C07D413/14 , C07D413/10 , C07D405/10 , C07D407/12
摘要： An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof.The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof. wherein the symbols in the formula are defined below: R1: e.g., a C1-C6 alkyl group; R2: a C1-C6 alkyl group; A: e.g., an oxygen atom; and R3: e.g., a C1-C6 alkyl group.
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公开(公告)号：US10227417B2
公开(公告)日：2019-03-12
申请号：US15821662
申请日：2017-11-22
发明人： Toshinori Agatsuma , Shu Takahashi , Jun Hasegawa , Daisuke Okajima , Hirofumi Hamada , Miki Yamaguchi
IPC分类号： A61K31/47 , A61K47/68 , C07K16/30 , A61K31/4745
摘要： It is intended to provide an antitumor drug having an excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. There is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-TROP2 antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(═O)— wherein the anti-TROP2 antibody is connected to the terminal of L1, and the antitumor compound is connected to the carbonyl group of the —(CH2)n2-C(═O)— moiety with the nitrogen atom of the amino group at position 1 as a connecting position.
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公开(公告)号：US10221195B2
公开(公告)日：2019-03-05
申请号：US15874768
申请日：2018-01-18
发明人： Shojiro Miyazaki , Yuko Yamamoto , Keisuke Suzuki , Masaharu Inui , Masanori Izumi , Kaori Soma , Anthony Pinkerton , Taeko Shinozaki
IPC分类号： C07D498/10 , C07D498/04 , A61K9/20 , A61K9/48 , A61K31/553
摘要： The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I): wherein R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R2 and R3 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R4 and R5 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R6 represents a hydrogen atom or the like, each R7 may be the same or different and may each represent an optionally substituted C1-6 alkoxy group or the like, X represents —CH═, —C(—R7)═, or —N═, and m represents 1 to 4, or a pharmacologically acceptable salt thereof.
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48.发明申请公开(公告)号：US20180350058A1
公开(公告)日：2018-12-06
申请号：US16102147
申请日：2018-08-13
申请人： Kensuke ITO , Yasuhiro SUZUKI
发明人： Kensuke ITO , Yasuhiro SUZUKI
CPC分类号： G06T7/001 , A61J3/005 , A61J3/10 , A61J2200/40 , A61J2200/72 , A61K9/2072 , A61K9/2095 , A61K9/2893 , G01N21/9508 , G06K9/00 , G06K9/00577 , G06K9/6277 , G06T2207/30121 , G06T2207/30204 , Y10T428/2991
摘要： A method of producing a tablet in which an uncoated tablet is coated by a coating agent, the method including: a coating process of coating uncoated tablets with a coating agent by spray coating the coating agent onto tablets that are churned and tumbled inside a container, and drying the tablets inside the container by supplying drying air into the container and exhausting air from the container, wherein spray coating conditions, including air supply temperature, air supply rate, and spray speed, are controlled according to the weight of the coating agent with which the uncoated tablets are coated, such that the humidity of air exhausted during spray coating is within a range of from 14% RH to 30% RH.
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公开(公告)号：US20180327399A1
公开(公告)日：2018-11-15
申请号：US15764264
申请日：2016-09-28
发明人： Manoj Kumar Khera , Tarun Mathur , Jitendra A. Sattigeri , Nobuhisa Masuda , Tsuyoshi Soneda , Yoshiko Kagoshima , Toshiyuki Konosu , Tetsuya Suzuki , Makoto Yamaoka , Ryo Itooka
IPC分类号： C07D417/14 , A61P31/04
CPC分类号： C07D417/14 , A61P31/04
摘要： Problem to be Solved There is a need for a new antibiotic having a novel mechanism of action which exhibit strong antibacterial activity not only against sensitive bacteria but also against resistant bacteria thereof, and at the same time possesses excellent solubility an a safety profile amenable to human use.Solution to the Problem As a result of intensive research, the present inventors have found that a compound represented by general formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof inhibits DNA gyrase GyrB subunit and/or topoisomerase IV ParE subunit possesses excellent solubility and a safety profile for use in humans for the treatment of bacterial infectious diseases.
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公开(公告)号：US10111858B2
公开(公告)日：2018-10-30
申请号：US15723097
申请日：2017-10-02
发明人： Kiyoshi Arai , Tsuyoshi Homma , Makoto Mizuno
IPC分类号： A61K31/40 , A61K9/20 , A61K31/4178 , A61K31/4422 , A61K31/549 , A61K45/00
摘要： A pharmaceutical for the prophylaxis or treatment of hypertension or a disease derived from hypertension. The pharmaceutical is characterized by comprising (i) a specific mineralocorticoid receptor antagonist and (ii) one or more components selected from the following components (A) to (C), for administration simultaneously or separately at a time interval: (A) an angiotensin II receptor antagonist, (B) a calcium antagonist, and (C) a diuretic.
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