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1. JP2017008052 - CONDENSED HETEROAROMATIC PYRROLIDINONE AS SYK INHIBITOR

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Japan
Application Number 2016133849
Application Date 06.07.2016
Publication Number 2017008052
Publication Date 12.01.2017
Grant Number 6196710
Grant Date 25.08.2017
Publication Kind B2
IPC
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 519/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
519Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
A61K 31/437
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 11/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
02Nasal agents, e.g. decongestants
CPC
A61K 31/437
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/527
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
527spiro-condensed
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Applicants TAKEDA CHEM IND LTD
武田薬品工業株式会社
Inventors ARIKAWA YASUYOSHI
有川　泰由
JONES BENJAMIN
ジョーンズ、ベンジャミン
BETTY LAM
ラム、ベティー
ZHE NIE
ニエ、ジャ
CHRISTOPHER SMITH
スミス、クリストファー
TAKAHASHI MASASHI
高橋　昌志
DONG QING
ドン、キン
VICTORIA FEHER
フェーフル、ヴィクトリア
Agents 高島　一
土井　京子
鎌田　光宜
田村　弥栄子
小池　順造
當麻　博文
Priority Data 61/289,969 23.12.2009 US
61/386,964 27.09.2010 US
Title
(EN) CONDENSED HETEROAROMATIC PYRROLIDINONE AS SYK INHIBITOR
(JA) ＳＹＫ阻害剤としての縮合複素芳香族ピロリジノン
Abstract
(EN)

PROBLEM TO BE SOLVED: To provide a manufacturing method of a compound useful as a spleen tyrosine kinase inhibitor.

SOLUTION: There is provided a manufacturing method of a compound of the formula 9-5 or a pharmaceutically acceptable salt thereof, including treating a corresponding N-t-butoxycarbonyl compound or a salt thereof with an acid to obtain the compound of the formula 9-5 or the salt thereof and converting the compound to the pharmaceutically acceptable salt if needed. 9-5, where R3 is independently selected from C2-6 alkyl, C3-8 cycloalkyl, C2-5 heterocyclyl, C1-9 heteroaryl which are optionally substituted by 1 to 5 substituent selected from halo, oxo, NO2, CN, (substituted)amino group or the like, R4 is independently selected from C3-8 cycloalkyl, C2-5 heterocyclyl, C6-14 aryl and C1-9 heteroaryl which are optionally substituted by same substituent.

SELECTED DRAWING: None

COPYRIGHT: (C)2017,JPO&INPIT


(JA)

【課題】脾臓チロシンキナーゼ阻害剤として有用な化合物の製造方法の提供。
【解決手段】式９−５の化合物又はその薬剤的に許容できる塩の製造方法であって、対応するＮ−ｔ−ブトキシカルボニル化合物又はその塩を酸で処理して、式９−５の化合物又はその塩を得、必要に応じて、該化合物を薬剤的に許容できる塩に変換することを含む方法。

式中、Ｒ３は、独立して、ハロ、オキソ、ＮＯ２、ＣＮ、（置換）アミノ基等から選択される１〜５つの置換基で随意に置換される、Ｃ２−６アルキル、Ｃ３−８シクロアルキル、Ｃ２−５ヘテロシクリル、Ｃ１−９ヘテロアリールから選択され；Ｒ４は、独立して、同様の置換基で随意に置換される、Ｃ３−８シクロアルキル、Ｃ２−５ヘテロシクリル、Ｃ６−１４アリール、及びＣ１−９ヘテロアリールから選択される。
【選択図】なし
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