Processing

Please wait...

Settings

Settings

Goto Application

1. WO2020111252 - DOCK1-INHIBITING COMPOUND AND USE THEREOF

Publication Number WO/2020/111252
Publication Date 04.06.2020
International Application No. PCT/JP2019/046862
International Filing Date 29.11.2019
IPC
A61K 31/40 2006.01
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/401 2006.01
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
401Proline; Derivatives thereof, e.g. captopril
A61K 31/4174 2006.01
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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
A61K 31/422 2006.01
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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42Oxazoles
422not condensed and containing further heterocyclic rings
A61K 31/437 2006.01
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 31/4439 2006.01
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
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
CPC
A61K 31/40
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/401
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
401Proline; Derivatives thereof, e.g. captopril
A61K 31/4174
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
A61K 31/422
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
42Oxazoles
422not condensed and containing further heterocyclic rings
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 31/4439
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
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Applicants
  • 国立大学法人九州大学 KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION [JP]/[JP]
Inventors
  • 福井 宣規 FUKUI, Yoshinori
  • 宇留野 武人 URUNO, Takehito
  • 金井 求 KANAI, Motomu
  • 生長 幸之助 OISAKI, Kounosuke
  • 堤 亮祐 TSUTSUMI, Ryosuke
Agents
  • 特許業務法人三枝国際特許事務所 SAEGUSA & PARTNERS
Priority Data
2018-22575330.11.2018JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) DOCK1-INHIBITING COMPOUND AND USE THEREOF
(FR) COMPOSÉ INHIBITEUR DE DOCK1 ET SON UTILISATION
(JA) DOCK1阻害化合物およびその用途
Abstract
(EN)
Provided is a compound that is usable as an active ingredient of an anticancer agent. Preferably, provided is a compound that has a DOCK1-inhibiting activity and exerts an anticancer effect based on the activity. A compound represented by formula (A) or a salt thereof: in formula (A), X represents a carbon atom or a nitrogen atom; Y represents an oxygen atom, a hydroxy group or a hydrocarbon group; R1 and R2 are different and represent a hydrogen atom or a group represented by formula (A-1): (in formula (A-1), R6 represents a pyrrolidino group or a phenyl group, and n2 represents 0 or 1) ; R3 represents -CO-R7 (wherein R7 represents an alkoxy group, an alkyl group or an alkylamino group), a 1,3-oxazole group, an alkylhydroxy group, a hydrogen atom or an oxygen atom; R4 represents a hydrogen atom, an oxygen atom or a hydrocarbon group in which a hydrogen atom may be substituted; R5 represents a halogen atom, a halogenated alkyl group or a halogenated alkylthio group; and n1 represents an integer of 0-5.) ; in formula (A), a solid line on the skeleton of the compound represents a single bond, a double line consisting of a solid line and a dotted line represents a single or double bond, and tow dotted lines represent a non-bond or a double bond.
(FR)
L'invention concerne un composé pouvant être utilisé en tant que principe actif d'un agent anticancéreux. De préférence, l'invention concerne un composé ayant une activité d'inhibition de DOCK1 et exerçant un effet anticancéreux sur la base de l'activité. Un composé représenté par la formule (A) ou un sel de celui-ci : dans la formule (A), X représente un atome de carbone ou un atome d'azote ; Y représente un atome d'oxygène, un groupe hydroxy ou un groupe hydrocarboné ; R1 et R2 sont différents et représentent un atome d'hydrogène ou un groupe représenté par la formule (A-1) : (dans la formule (A-1), R6 représente un groupe pyrrolidino ou un groupe phényle, et n2 représente 0 ou 1) ; R3 représente -CO-R7 (où R7 représente un groupe alcoxy, un groupe alkyle ou un groupe alkylamino), un groupe 1,3-oxazole, un groupe alkylhydroxy, un atome d'hydrogène ou un atome d'oxygène ; R4 représente un atome d'hydrogène, un atome d'oxygène ou un groupe hydrocarboné dans lequel un atome d'hydrogène peut être substitué ; R5 représente un atome d'halogène, un groupe alkyle halogéné ou un groupe alkylthio halogéné ; et n1 représente un entier de 0 à 5.) ; dans la formule (A), une ligne continue sur le squelette du composé représente une liaison simple, une double ligne constituée d'une ligne continue et d'une ligne en pointillé représente une liaison simple ou double, et deux lignes en pointillé représentent une double liaison ou une double liaison.
(JA)
抗がん剤の有効成分として用いることができる化合物の提供。好ましくは、DOCK1阻害作用を有し、当該作用に基づいて抗がん作用を発揮する化合物を提供する。 下式(A)で示される化合物またはその塩: 式(A)中、 Xは、炭素原子または窒素原子; Yは、酸素原子、ヒドロキシ基、または炭化水素基; R及びRは、異なって、水素原子又は下式(A-1)で示される基: (式(A-1)中、Rはピロリジノ基またはフェニル基、nは0または1を示す。); Rは、-CO-R(Rはアルコキシ基、アルキル基、またはアルキルアミノ基を意味する)、1,3-オキサゾール基、アルキルヒドロキシ基、水素原子、及び酸素原子;Rは、水素原子、酸素原子または水素原子が置換されていてもよい炭化水素基; Rは、ハロゲン原子、ハロゲン化アルキル基またはハロゲン化アルキルチオ基;nは0~5の整数を意味する。); 式(A)において化合物の骨格上の一本の実線は単結合、実線と点線とからなる二重線は単結合または二重結合、二本の点線は非結合または二重結合を意味する。
Latest bibliographic data on file with the International Bureau