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1. (WO2017094838) FLUORESCENT LIGAND FOR RETINOID X RECEPTOR, AND APPLICATION THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/094838 International Application No.: PCT/JP2016/085729
Publication Date: 08.06.2017 International Filing Date: 01.12.2016
IPC:
C07D 213/80 (2006.01) ,A61K 31/352 (2006.01) ,A61K 31/44 (2006.01) ,A61K 31/4433 (2006.01) ,A61K 31/4704 (2006.01) ,A61K 31/4709 (2006.01) ,A61P 3/00 (2006.01) ,A61P 3/10 (2006.01) ,A61P 7/00 (2006.01) ,A61P 25/16 (2006.01) ,A61P 25/28 (2006.01) ,A61P 35/00 (2006.01) ,A61P 43/00 (2006.01) ,C07D 215/54 (2006.01) ,C07D 311/16 (2006.01) ,C07D 401/12 (2006.01) ,C07D 405/12 (2006.01) ,G01N 33/15 (2006.01) ,G01N 33/50 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78
Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
79
Acids; Esters
80
in position 3
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
335
having oxygen as the only ring hetero atom, e.g. fungichromin
35
having six-membered rings with one oxygen as the only ring hetero atom
352
condensed with carbocyclic rings, e.g. cannabinols, methantheline
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4433
containing a six-membered ring with oxygen as a ring hetero atom
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
47
Quinolines; Isoquinolines
4704
2-Quinolinones, e.g. carbostyril
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
47
Quinolines; Isoquinolines
4709
Non-condensed quinolines containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
14
for treating abnormal movements, e.g. chorea, dyskinesia
16
Anti-Parkinson drugs
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
48
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
54
attached in position 3
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
311
Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02
ortho- or peri-condensed with carbocyclic rings or ring systems
04
Benzo [b] pyrans, not hydrogenated in the carbocyclic ring
06
with oxygen or sulfur atoms directly attached in position 2
08
not hydrogenated in the hetero ring
16
substituted in position 7
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
15
Medicinal preparations
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48
Biological material, e.g. blood, urine; Haemocytometers
50
Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
Applicants:
国立大学法人 岡山大学 NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY [JP/JP]; 岡山県岡山市北区津島中一丁目1番1号 1-1, Tsushima-Naka 1-chome, Kita-ku, Okayama-shi, Okayama 7008530, JP
Inventors:
加来田 博貴 KAKUTA, Hiroki; JP
山田 翔也 YAMADA, Shoya; JP
渡邉 将貴 WATANABE, Masaki; JP
Agent:
特許業務法人せとうち国際特許事務所 SETOUCHI INTERNATIONAL PATENT FIRM; 岡山県岡山市北区今4丁目9番1号 グロース第2ビル Growth-2 Building, 4-9-1, Ima, Kita-ku, Okayama-shi, Okayama 7000975, JP
Priority Data:
2015-23701703.12.2015JP
Title (EN) FLUORESCENT LIGAND FOR RETINOID X RECEPTOR, AND APPLICATION THEREOF
(FR) LIGAND FLUORESCENT DESTINÉ À UN RÉCEPTEUR RÉTINOÏDE X, ET SON APPLICATION
(JA) 蛍光性を有するレチノイドX受容体結合性分子及びその用途
Abstract:
(EN) By using a fluorescent ligand for a retinoid X receptor (RXR), said ligand being indicated by one of the following formulas (1)-(3), an evaluative test of ability to bind with RXR can be easily performed. (In the formulas, R1 is methyl, alkoxy, or styryl, R2 is hydroxy, alkoxy, or alkylamino, A is N or CH, B is NH or O, R3 is isopropyl or tertiary butyl, and R4 is isopropyl or isobutyl.)
(FR) La présente invention concerne l'utilisation d'un ligand fluorescent destiné à un récepteur rétinoïde X (RXR), ledit ligand étant indiqué par l'une des formules suivantes (1) à (3), permettant d'exécuter facilement un test d'évaluation de la capacité à se lier au RXR. (Dans les formules, R1 est un groupe méthyle, alcoxy, ou styryle, R2 est un groupe hydroxyle, alcoxy, ou alkylamino, A est N ou CH, B est NH ou O, R3 est un groupe isopropyle ou butyle tertiaire, et R4 est un groupe isopropyle ou isobutyle.)
(JA) 下記式(1)~(3)のいずれかで示され、蛍光性を有するレチノイドX受容体結合性分子を用いることで、RXRに対する結合性の評価試験が容易に行える。[式中、Rは、メチル、アルコキシ又はスチリルであり;Rは、ヒドロキシ、アルコキシ又はアルキルアミノであり;Aは、N又はCHであり;Bは、NH又はOであり;Rは、イソプロピル又はターシャリーブチルであり;Rは、イソプロピル又はイソブチルである。]
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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)
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)
Also published as:
CN108290841