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1. (WO2019031615) HEMIASTERLIN DERIVATIVES AND ANTIBODY-DRUG CONJUGATES INCLUDING SAME
Latest bibliographic data on file with the International BureauSubmit observation

Pub. No.: WO/2019/031615 International Application No.: PCT/JP2018/030144
Publication Date: 14.02.2019 International Filing Date: 10.08.2018
IPC:
C07K 5/065 (2006.01) ,A61K 38/06 (2006.01) ,A61K 38/08 (2006.01) ,A61K 39/395 (2006.01) ,A61K 45/00 (2006.01) ,A61K 47/68 (2017.01) ,A61P 35/00 (2006.01) ,A61P 43/00 (2006.01) ,C07K 5/072 (2006.01) ,C07K 5/093 (2006.01) ,C07K 16/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
06
Dipeptides
065
the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
04
Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
06
Tripeptides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
04
Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
08
Peptides having 5 to 11 amino acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39
Medicinal preparations containing antigens or antibodies
395
Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
[IPC code unknown for A61K 47/68]
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
06
Dipeptides
072
the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
08
Tripeptides
093
the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
16
Immunoglobulins, e.g. monoclonal or polyclonal antibodies
18
against material from animals or humans
28
against receptors, cell surface antigens or cell surface determinants
Applicants:
大日本住友製薬株式会社 SUMITOMO DAINIPPON PHARMA CO., LTD. [JP/JP]; 大阪府大阪市中央区道修町2丁目6番8号 6-8, Dosho-machi 2-chome, Chuo-ku, Osaka-shi, Osaka 5418524, JP
Inventors:
坂 仁志 BAN Hitoshi; JP
西尾 幸博 NISHIO Yukihiro; JP
諏訪 篤志 SUWA Atsushi; JP
Agent:
長谷川 芳樹 HASEGAWA Yoshiki; JP
清水 義憲 SHIMIZU Yoshinori; JP
Priority Data:
2017-15598810.08.2017JP
Title (EN) HEMIASTERLIN DERIVATIVES AND ANTIBODY-DRUG CONJUGATES INCLUDING SAME
(FR) DÉRIVÉS D'HÉMIASTERLINE ET CONJUGUÉS ANTICORPS-MÉDICAMENT LES COMPRENANT
(JA) ヘミアスタリン誘導体及びこれらの抗体薬物複合体
Abstract:
(EN) Compounds represented by formula (1) or salts thereof. [In the formula, AA represents a specific amino acid residue or a C1–6 alkyl ester thereof, each AA being the same or different and the AAs being linked by an amide linkage when there are multiple AAs, and the N-terminal nitrogen atom of (AA)m forming an amide linkage with carbonyl (a), Q represents an unsubstituted phenyl group or a group represented by formula (Q-1), formula (Qa-2), formula (Qa-3), formula (Qa-4), formula (Qa-5), formula (Qa-6), or formula (Qa-7), R1a and R1b each independently represent a hydrogen atom or a C1–6 alkyl group, and m represents an integer from 1 to 10.]
(FR) L'invention concerne des composés représentés par la formule (1) ou des sels de ceux-ci. [Dans la formule, AA représente un résidu d'acide aminé spécifique ou un ester d'alkyle en C1–6 de celui-ci, chaque AA étant identique ou différent et les AA étant lié par une liaison amide lorsqu'il y a plusieurs AA, et l'atome d'azote N-terminal de (AA)m formant une liaison amide avec du carbonyle (a), Q représente un groupe phényle non substitué ou un groupe représenté par la formule (Q-1), la formule (Qa-2), la formule (Qa-3), la formule (Qa-4), la formule (Qa-5), la formule (Qa-6), ou la formule (Qa-7), R1a et R1b représentent chacun indépendamment un atome d'hydrogène ou un groupe alkyle en C1–6, et m représente un nombre entier de 1 à 10.]
(JA) 式(1): 【化1】 [式中、 AAは、特定のアミノ酸残基又はこれらのC1-6アルキルエステル体を表し、AAが複数ある場合、それぞれのAAは互いに同一であっても異なっていてもよく、また、AA同士はアミド結合を介して結合しており、 (AA)のN末端窒素原子はカルボニル(a)と共にアミド結合を形成しており、 Qは、無置換フェニル基又は式(Q-1)、式(Qa-2)、式(Qa-3)、式(Qa-4)、式(Qa-5)、式(Qa-6)又は式(Qa-7)で表される基を表し、 R1a及びR1bは、それぞれ独立して、水素原子又はC1-6アルキル基を表し、 mは1~10の整数を表す]で表される、化合物又はその塩。
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African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
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Publication Language: Japanese (JA)
Filing Language: Japanese (JA)