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1. (WO2019045036) EXON 18 AND/OR EXON 21 MUTANT EGFR SELECTIVE INHIBITOR
Latest bibliographic data on file with the International BureauSubmit observation

Pub. No.: WO/2019/045036 International Application No.: PCT/JP2018/032314
Publication Date: 07.03.2019 International Filing Date: 31.08.2018
IPC:
A61K 31/519 (2006.01) ,A61P 35/00 (2006.01) ,C12N 9/99 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
9
Enzymes, e.g. ligases (6.); Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating, or purifying enzymes
99
Enzyme inactivation by chemical treatment
Applicants:
大鵬薬品工業株式会社 TAIHO PHARMACEUTICAL CO., LTD. [JP/JP]; 東京都千代田区神田錦町1-27 1-27, Kandanishiki-cho, Chiyoda-ku, Tokyo 1018444, JP
Inventors:
阿部 直美 ABE, Naomi; JP
羽迫 真一 HASAKO, Shinichi; JP
Agent:
特許業務法人三枝国際特許事務所 SAEGUSA & PARTNERS; 大阪府大阪市中央区道修町1-7-1 北浜TNKビル Kitahama TNK Building, 1-7-1, Doshomachi, Chuo-ku, Osaka-shi, Osaka 5410045, JP
Priority Data:
2017-16860601.09.2017JP
Title (EN) EXON 18 AND/OR EXON 21 MUTANT EGFR SELECTIVE INHIBITOR
(FR) INHIBITEUR SÉLECTIF DE L'EGFR MUTÉ SUR L'EXON 18 ET/OU SUR L'EXON 21
(JA) エクソン18及び/又はエクソン21変異型EGFR選択的阻害剤
Abstract:
(EN) An anti-tumor agent for treating patients with malignant tumors that express EGFR having at least one mutation selected from the group consisting of exon 18 G719X mutations, exon 18 E709X mutations, and exon 21 L861X mutations, the anti-tumor agent containing (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide or a salt thereof. [X represents a discretionary amino acid residue.]
(FR) L'invention concerne un agent antitumoral pour traiter des patients atteints de tumeurs malignes exprimant un EGFR présentant au moins une mutation appartenant au groupe constitué par les mutations G719X de l'exon 18, les mutations E709X de l'exon 18 et les mutations L861X de l'exon 21, l'agent antitumoral contenant du (S)-N-(4-amino-6-méthyl-5-(quinoline-3-yl)-8,9-dihydropyrimido[5,4-b]indolizine-8-yl)acrylamide ou un sel correspondant. [X représente un résidu d'acide aminé facultatif.]
(JA) (S)-N-(4-アミノ-6-メチル-5-(キノリン-3-イル)-8,9-ジヒドロピリミド[5,4-b]インドリジン-8-イル)アクリルアミド又はその塩を含有する、エクソン18のG719X変異、エクソン18のE709X変異及びエクソン21のL861X変異からなる群から選択される少なくとも1つの変異を有するEGFRを発現している悪性腫瘍患者を治療するための抗腫瘍剤。[Xは任意のアミノ酸残基を示す。]
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
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)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)