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41. 发明申请

US20210032313A1 KLK5 INHIBITORY PEPTIDE 有权
公开(公告)号：US20210032313A1
公开(公告)日：2021-02-04
申请号：US17064543
申请日：2020-10-06
申请人： DAIICHI SANKYO COMPANY, LIMITED
发明人： Daisuke Nishimiya , Hidenori Yano , Hidenori Takahashi , Shinji Yamaguchi , Shiho Ofuchi
IPC分类号： C07K14/81
摘要： Provided is a novel peptide. The peptide contains the amino acid sequence set forth in SEQ ID NO: 61 and inhibits a protease.

42. 发明授权

US10851092B2 Pyridine compound 有权
公开(公告)号：US10851092B2
公开(公告)日：2020-12-01
申请号：US16337896
申请日：2017-09-28
申请人： Daiichi Sankyo Company, Limited
发明人： Hiroaki Inagaki , Yoshihiro Shibata , Hidenori Namiki , Hideaki Kageji , Kiyoshi Nakayama , Yasuyuki Kaneta
IPC分类号： C07D413/14 , C07D401/14
摘要： The present invention relates to a compound having RET kinase inhibiting action or a pharmaceutically acceptable salt thereof, useful in the treatment of diseases such as cancer. In particular a compound represented by the following general formula (I) as defined herein: (I) or a pharmaceutically acceptable salt thereof.

43. 发明授权

US10808006B2 Sustained-release pharmaceutical composition for treatment and prevention of eye disease 有权
公开(公告)号：US10808006B2
公开(公告)日：2020-10-20
申请号：US16277861
申请日：2019-02-15
申请人： Daiichi Sankyo Company, Limited
发明人： Yuji Kasuya , Yasuhiro Nakagami , Emiko Hatano , Tatsuya Inoue , Kazuhiro Yoshida , Satoshi Komoriya , Yoko Murakami , Masaru Iwasaki , Atsunobu Sakamoto , Kayoko Masuda , Masako Minami , Mayumi Iizuka , Yasunori Ono , Takashi Ohnuki
IPC分类号： A61P27/02 , A61K31/58 , C07J71/00 , C07J63/00 , A61K9/00 , A61K9/16 , A61K9/20
摘要： The present invention relates to a terpenoid derivative that has the ability to activate the Keap1/Nrf2/ARE signaling pathway and is excellent in anti-inflammatory action and cytoprotective action, and a sustained-release pharmaceutical composition effective for the treatment and prevention of a posterior eye disease caused by oxidative stress, comprising the terpenoid derivative as an active ingredient. The present invention provides a local administration-type sustained-release pharmaceutical composition for the treatment or prevention of a posterior eye disease, comprising the terpenoid derivative of the present invention as an active ingredient, wherein the sustained-release pharmaceutical composition maintains a pharmacological action thereof for 1 week or longer by the sustained release of the terpenoid derivative under physiological conditions and has a base material administrable to the vitreous body and a form administrable to the vitreous body.

44. 发明授权

US10774087B2 Sulfonamide derivative having coumarin skeleton 有权
公开(公告)号：US10774087B2
公开(公告)日：2020-09-15
申请号：US16463792
申请日：2017-11-22
申请人： Daiichi Sankyo Company, Limited
发明人： Masahiro Ota , Hidekazu Inoue , Junya Kawai , Hitoshi Ohki , Tadashi Toki
IPC分类号： C07D491/052 , A61K31/496 , A61P35/00 , A61P43/00
摘要： Provided is a novel compound or a salt thereof inhibiting MTHFD2 and useful for treating a disease caused by overexpression of MTHFD2, a disease involved in overexpression of MTHFD2 and/or a disease associated with overexpression of MTHFD2.SolutionProvided is a sulfonamide derivative having a coumarin skeleton represented by the following formula (I) and having various substituents: wherein R1, R2, R3, R4, R5, R6 and R7 are the same as defined in the specification, and a salt thereof.

45. 发明申请

US20200261594A1 ANTIBODY-PYRROLOBENZODIAZEPINE DERIVATIVE CONJUGATE 审中-公开
公开(公告)号：US20200261594A1
公开(公告)日：2020-08-20
申请号：US16651501
申请日：2018-09-28
申请人： DAIICHI SANKYO COMPANY, LIMITED
发明人： Narihiro TODA , Yusuke OTA , Fuminao DOI , Masaki MEGURO , Ichiro HAYAKAWA , Shinji ASHIDA , Takeshi MASUDA , Takashi NAKADA , Mitsuhiro IWAMOTO , Naoya HARADA , Tomoko TERAUCHI , Daisuke OKAJIMA , Kensuke NAKAMURA , Hiroaki UCHIDA , Hirofumi HAMADA
IPC分类号： A61K47/68 , C07D487/04 , C07K16/30 , A61P35/00
摘要： The present invention provides a novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, and a novel CLDN6 and/or CLDN9 antibody.

46. 发明申请

US20200246369A1 ANTISENSE OLIGONUCLEOTIDE AND COMPOSITION FOR PREVENTION OR TREATMENT OF GLYCOGEN STORAGE DISEASE TYPE IA 审中-公开
公开(公告)号：US20200246369A1
公开(公告)日：2020-08-06
申请号：US16491435
申请日：2018-03-09
申请人： NATIONAL CENTER FOR CHILD HEALTH AND DEVELOPMENT , HIROSHIMA UNIVERSITY , DAIICHI SANKYO COMPANY, LIMITED
发明人： Go TAJIMA , Satoshi OKADA , Myyuki TSUMURA
IPC分类号： A61K31/7088 , C12N15/113 , A61P3/08
摘要： The present invention provides a novel antisense oligonucleotide and a composition for preventing or treating glycogen storage disease type Ia. The present invention provides an antisense oligonucleotide which hybridizes with a pre-mRNA sequence derived from a region including at least one of a base at position 42911000, a base at position 42911004, and a base at position 42911005 in a base sequence of human chromosome 17 of GRCh38/hg38 and has activity to inhibit aberrant splicing of pre-mRNA of c.648G>T variant G6PC.

47. 发明授权

US10729782B2 Antibody-drug conjugate produced by binding through linker having hydrophilic structure 有权
公开(公告)号：US10729782B2
公开(公告)日：2020-08-04
申请号：US15821697
申请日：2017-11-22
申请人： DAIICHI SANKYO COMPANY, LIMITED
发明人： Hiroyuki Naito , Takashi Nakada , Masao Yoshida , Shinji Ashida , Takeshi Masuda , Hideki Miyazaki , Yuji Kasuya , Yuki Abe , Yusuke Ogitani
IPC分类号： A61K47/68 , A61K31/47 , C07K16/30 , C07K16/28 , C07K16/00
摘要： As an antitumor drug 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 (I) is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- or -L1-L2-LP- wherein the antibody is connected to the terminal of L1, the antitumor compound is connected to the terminal of Lc or LP, and any one or two or more of linkers of L1, L2, and LP has a hydrophilic structure.

48. 发明申请

US20200172494A1 PYRIMIDINE DERIVATIVE 审中-公开
公开(公告)号：US20200172494A1
公开(公告)日：2020-06-04
申请号：US16473749
申请日：2017-12-26
申请人： Daiichi Sankyo Company, Limited
发明人： Yasuyuki Takeda , Yamato Suzuki , Toshiharu Noji , Hidenobu Murafuji , Satoshi Muneoka , Hidekazu Inoue , Bitoku Takahashi , Rie Inaba
IPC分类号： C07D239/34 , A61P11/12
摘要： Cystic fibrosis is developed through mutation of Cystic Fibrosis Transmembrane conductance Regulator (CFTR), which is one type of chloride channel. An object of the present invention is to provide compounds effective in the treatment of cystic fibrosis that open a chloride channel different from CFTR, which is the cause of the disease, and do not depend on CFTR.Compounds of the present invention are compounds or pharmaceutically acceptable salts thereof that open calcium dependent chloride channels (CaCCs) via G-protein coupled receptor 39 (GPR39) agonism to have strong chloride ion-secretory action, and are represented by the following general formula (I):General formula (I): wherein, X represents a carboxyl group or a tetrazolyl group; Q represents a C1-C3 alkylene group, an oxygen atom, a sulfur atom, etc.; G represents a phenyl group where the phenyl group may have 1 to 3 substituents independently selected from the group consisting of a halogen atom, a cyano group, a C1-C6 alkyl group, etc.; R1 represents a C1-C6 alkyl group, etc.; R2 represents a C1-C6 alkyl group that may have 1 to 3 substituents independently selected from the following group A, or a group selected from the following group B: Group A: a phenyl group and a pyridyl group, wherein the phenyl group and the pyridyl group may have 1 to 3 substituents independently selected from the following group D; Group B: —OH, —O-M, —SH, —S-M, —NH2, —NH-M, and —N-M2, wherein M is a C1-C6 alkyl group that may have 1 or 2 substituents independently selected from the following group C, or a C3-C6 cycloalkyl group that may have 1 or 2 substituents independently selected from the following group C; Group C: a halogen atom, a cyano group, a phenyl group, a pyridyl group, etc., wherein the phenyl group and the pyridyl group may have 1 to 3 substituents independently selected from the following group D; and Group D: a halogen atom, a cyano group, a C1-C6 alkyl group, etc.

49. 发明授权

US10654821B2 Griseofulvin compound 有权
公开(公告)号：US10654821B2
公开(公告)日：2020-05-19
申请号：US16561459
申请日：2019-09-05
申请人： Daiichi Sankyo Company, Limited
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 , C07D405/10 , C07D413/14 , C07D413/10 , 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.

50. 发明授权

US10603285B2 Solid preparation including colorant 有权
公开(公告)号：US10603285B2
公开(公告)日：2020-03-31
申请号：US15559700
申请日：2016-03-17
申请人： DAIICHI SANKYO COMPANY, LIMITED
发明人： Shinichiro Tajiri , Shinji Yoshinaga , Yurika Ozaki
IPC分类号： A61K47/02 , A61K9/28 , A61K31/195 , A61K47/22 , A61K47/12 , A61K47/36 , A61K47/10 , A61K47/38 , A61K47/26 , A61K47/20 , A61K47/14 , A61K9/20
摘要： An object of the present invention is to provide [(1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate as a stabilized pharmaceutical solid preparation, and also to provide a method for preparing the stabilized pharmaceutical solid preparation. The object can be attained by a pharmaceutical solid preparation comprising [(1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate which is compound represented by the following formula (I) in combination with (i) one or two or more components selected from the group consisting of D-mannitol, lactose, corn starch, and crystalline cellulose, (ii) carmellose calcium, and (iii) colorants.

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