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公开(公告)号:US20240360200A1
公开(公告)日:2024-10-31
申请号:US18663615
申请日:2024-05-14
CPC分类号: C07K14/81 , A61K38/55 , A61K38/57 , C07K14/811 , C07K14/8135 , A61K38/00 , C07K2319/30
摘要: SPINK2 mutant peptide conjugates are provided that inhibit KLK5. The KLK5 inhibitory peptide conjugates are Fc fusion peptides in which, in certain embodiments, the Fc region of the fusion peptides are the Fc region of human IgG1 or a fragment thereof. The KLK5 inhibitory peptide conjugates include an amino acid sequence of one of SEQ ID NOs: 34, 36, 38, 40, 42, 44, 46, 48, 96, 50, 52, 54, 56, 58, or 60. Pharmaceutical compositions that include the KLK5 inhibitory peptide conjugates useful for treating KLK5-related diseases are also provided.
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公开(公告)号:US12091395B2
公开(公告)日:2024-09-17
申请号:US18501481
申请日:2023-11-03
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 , A61K31/343 , A61K31/4155 , A61K31/4245 , C07D405/04 , C07D405/10 , C07D407/12 , C07D413/04 , C07D413/10 , C07D413/14
CPC分类号: C07D307/94 , A61K31/343 , A61K31/4155 , A61K31/4245 , C07D405/04 , C07D405/10 , C07D407/12 , C07D413/04 , C07D413/10 , C07D413/14
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.-
公开(公告)号:US20240294660A1
公开(公告)日:2024-09-05
申请号:US18660591
申请日:2024-05-10
CPC分类号: C07K16/2896 , A61K2039/505 , A61P35/00 , C07K16/2863 , C07K16/2887 , C07K16/32 , C07K2317/21 , C07K2317/565 , C07K2317/72 , C07K2317/732 , C07K2317/76
摘要: An anti-SIRPα antibody that can be used as a tumor agent and an anti-tumor agent comprising the antibody as an active ingredient. An antibody that binds specifically to human SIRPα to inhibit binding of human SIRPα to CD47.
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公开(公告)号:US20240293567A1
公开(公告)日:2024-09-05
申请号:US18642667
申请日:2024-04-22
发明人: Toshifumi TSUDA , Toshiki TABUCHI , Hideaki WATANABE , Hiroyuki KOBAYASHI , Masayuki ISHIZAKI , Kyoko HARA , Teiji WADA , Masami ARAI
CPC分类号: A61K47/6807 , A61K47/545 , A61K47/6855 , A61P35/00 , C07K16/32
摘要: Desired is development of novel CDN derivatives having STING agonist activity; and a therapeutic agents and/or therapeutic methods using the novel CDN derivatives for diseases associated with STING agonist activity. Further desired is development of a therapeutic agents and/or therapeutic methods capable of delivering the novel CDN derivatives specifically to targeted cells and organs for diseases associated with STING agonist activity. The present invention provides novel CDN derivatives having potent STING agonist activity, and antibody-CDN derivative conjugates including the novel CDN derivatives.
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公开(公告)号:US12060365B2
公开(公告)日:2024-08-13
申请号:US17535369
申请日:2021-11-24
发明人: Kenji Yoshikawa , Noriyasu Haginoya , Tomoaki Hamada , Ryutaro Kanada , Jun Watanabe , Yoshiko Kagoshima , Eri Tokumaru , Kenji Murata , Takayuki Baba , Mayumi Kitagawa , Akiko Kurimoto , Masashi Numata , Machiko Shiroishi , Taeko Shinozaki
IPC分类号: C07D495/04 , A61K45/06 , A61P35/02 , C07D403/12 , C07D403/14 , C07D519/00
CPC分类号: C07D495/04 , A61K45/06 , A61P35/02 , C07D403/12 , C07D403/14 , C07D519/00 , C07B2200/13
摘要: The present invention provides a compound or a pharmaceutically acceptable salt thereof having an inhibitory action on the interaction between menin and an MLL protein. The compound represented by the formula (1) or a pharmaceutically acceptable salt thereof.
wherein, in the formula (1), the dotted circle, R1, R2, R3, R4, R5, R6, R7, R8, Ring Q1, W, m and n are each as defined in the description.-
公开(公告)号:US20240190961A1
公开(公告)日:2024-06-13
申请号:US17769600
申请日:2020-10-23
发明人: Shinko HAYASHI , Saori ISHIDA , Kazuki SATOH , Masato HATA
CPC分类号: C07K16/2818 , A61K45/06 , A61P35/00 , C07K16/2827 , A61K2039/507 , C07K2317/24 , C07K2317/52 , C07K2317/565 , C07K2317/732 , C07K2317/76
摘要: Provided is a pharmaceutical composition for use in the treatment or prevention of cancer, etc. The present invention provides a pharmaceutical composition or a method for treating cancer, wherein an anti-GARP antibody and an immunomodulator are administered in combination.
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公开(公告)号:US11945882B2
公开(公告)日:2024-04-02
申请号:US16642245
申请日:2018-08-30
发明人: Tatsuya Yamaguchi , Takashi Kouko , Shigeru Noguchi , Yohei Yamane , Fumikatsu Kondo , Takahiro Aoki , Tadahiro Takeda , Kohei Sakanishi , Hitoshi Sato , Tsuyoshi Ueda , Shinji Matuura , Kei Kurahashi , Yutaka Kitagawa , Tatsuya Nakamura
CPC分类号: C07K5/10 , C07B2200/13
摘要: Crystals of the compound represented by formula (1), a method for the production thereof, and a method for producing an antibody-drug conjugate using the crystals.
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8.
公开(公告)号:US20240093227A1
公开(公告)日:2024-03-21
申请号:US18265756
申请日:2021-12-08
发明人: Masatora FUKUDA , Makoto KOIZUMI , Shinzo IWASHITA
CPC分类号: C12N15/85 , C12N9/78 , C12N15/11 , C12Y305/04 , A61K48/00 , C12N2310/315 , C12N2310/321 , C12N2800/107
摘要: Provided is an oligonucleotide which may induce an editing activity of ADRC in cell and has excellent stability in a living body. The oligonucleotide includes a first oligonucleotide identifying a target RNA and a second oligonucleotide linked to the 5′-side of the first oligonucleotide. The first oligonucleotide consists of a target-corresponding nucleotide residue, an oligonucleotide of 10 to 24 residues at the 3′-side, and an oligonucleotide of 3 to 6 residues at the 5′-side. The second oligonucleotide has no nucleotide residue corresponding to a nucleotide residue of the target RNA or has a nucleotide residue which does not form a complementary pair at the 3′-end thereof and the number of residue is 3 to 6. The residue at the 3′-side of the target-corresponding nucleotide residue is a 2′-deoxynucleotide residue, and the third nucleotide residue counted in the 3′-direction from the target-corresponding nucleotide in the oligonucleotide at the 3′-side of the target-corresponding nucleotide residue is a 2′-deoxy-2′-fluoronucleotide residue.
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公开(公告)号:US11932600B2
公开(公告)日:2024-03-19
申请号:US17287445
申请日:2019-10-22
IPC分类号: C07D213/71 , A61P3/14 , C07D239/38 , C07D401/12
CPC分类号: C07D213/71 , A61P3/14 , C07D239/38 , C07D401/12
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 following formula (I): wherein X1 represents a nitrogen atom or CR9, R1 represents a hydrogen atom, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a halogen atom, R3 represents a hydrogen atom or a halogen atom, R4 represents a hydrogen atom or a halogen atom, and R5 represents a C1-C3 alkylsulfonyl group, a substituted C1-C6 alkyl group, a substituted C1-C6 haloalkyl group, a substituted C1-C6 alkoxy group, or a substituted C1-C6 alkylamino group, or a pharmacologically acceptable salt thereof.
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10.
公开(公告)号:US20240026030A1
公开(公告)日:2024-01-25
申请号:US18367446
申请日:2023-09-12
发明人: Hiroyuki NAITO , Yusuke OGITANI , Takeshi MASUDA , Takashi NAKADA , Masao YOSHIDA , Shinji ASHIDA , Koji MORITA , Hideki MIYAZAKI , Yuji KASUYA , Ichiro HAYAKAWA , Yuki ABE
IPC分类号: C07K16/32 , C07D491/22 , A61K47/68 , A61K39/395 , C07K16/28 , A61K31/4745 , C07K16/30
CPC分类号: C07K16/32 , C07D491/22 , A61K47/6803 , A61K47/6855 , A61K47/6869 , A61K39/395 , C07K16/28 , A61K31/4745 , C07K16/30 , C07K16/3015 , C07K16/3023 , C07K16/303 , C07K16/3046 , C07K16/3069 , A61K47/6851 , A61K47/6857 , A61K47/6849 , A61K47/6859 , C07K2317/73 , C07K2317/24 , A61K2039/505
摘要: As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 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-HER2 antibody is connected to the terminal 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 the connecting position.
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