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1. (WO2018101329) NOVEL ESTER COMPOUND AND PIN1 INHIBITOR, INFLAMMATORY DISEASE THERAPEUTIC, AND COLON CANCER THERAPEUTIC IN WHICH SAID ESTER COMPOUND IS USED
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Pub. No.: WO/2018/101329 International Application No.: PCT/JP2017/042804
Publication Date: 07.06.2018 International Filing Date: 29.11.2017
IPC:
C07C 69/732 (2006.01) ,A61K 31/216 (2006.01) ,A61K 31/235 (2006.01) ,A61K 31/341 (2006.01) ,A61K 31/403 (2006.01) ,A61P 1/00 (2006.01) ,A61P 1/04 (2006.01) ,A61P 35/00 (2006.01) ,A61P 43/00 (2006.01) ,C07C 69/753 (2006.01) ,C07C 69/767 (2006.01) ,C07C 69/92 (2006.01) ,C07C 229/60 (2006.01) ,C07C 271/22 (2006.01) ,C07D 209/18 (2006.01) ,C07D 209/86 (2006.01) ,C07D 265/38 (2006.01) ,C07D 307/68 (2006.01) ,C12N 15/09 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
69
Esters of carboxylic acids; Esters of carbonic or haloformic acids
66
Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, -CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
73
of unsaturated acids
732
of unsaturated hydroxy carboxylic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
21
Esters, e.g. nitroglycerine, selenocyanates
215
of carboxylic acids
216
of acids having aromatic rings, e.g. benactizyne, clofibrate
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
21
Esters, e.g. nitroglycerine, selenocyanates
215
of carboxylic acids
235
having an aromatic ring attached to a carboxyl group
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
34
having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
341
not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403
condensed with carbocyclic rings, e.g. carbazole
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
04
for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
69
Esters of carboxylic acids; Esters of carbonic or haloformic acids
74
Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
753
of polycyclic acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
69
Esters of carboxylic acids; Esters of carbonic or haloformic acids
76
Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
767
esterified with unsaturated alcohols having the esterified hydroxy group bound to an acyclic carbon atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
69
Esters of carboxylic acids; Esters of carbonic or haloformic acids
76
Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
84
of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
92
with etherified hydroxyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
52
having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
54
with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
60
with amino and carboxyl groups bound in meta- or para- positions
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
271
Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06
Esters of carbamic acids
08
having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10
with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
22
to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
10
with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56
Ring systems containing three or more rings
80
[b, c]- or [b, d]-condensed
82
Carbazoles; Hydrogenated carbazoles
86
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
28
1,4-Oxazines; Hydrogenated 1,4-oxazines
34
condensed with carbocyclic rings
38
[b, e]-condensed with two six-membered rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
56
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
68
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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
15
Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09
Recombinant DNA-technology
Applicants: HIROSHIMA UNIVERSITY[JP/JP]; 3-2, Kagamiyama 1-chome, Higashihiroshima-shi, Hiroshima 7398511, JP
TOKYO UNIVERSITY OF OF PHARMACY & LIFE SCIENCES[JP/JP]; 1432-1, Horinouchi, Hachioji-shi, Tokyo 1920392, JP
THE UNIVERSITY OF TOKYO[JP/JP]; 3-1, Hongo 7-chome, Bunkyo-ku, Tokyo 1138654, JP
Inventors: ASANO Tomoichiro; JP
NAKATSU Yusuke; JP
ITO Hisanaka; JP
OKABE Takayoshi; JP
Agent: NAGASHIMA Takaaki; JP
NONAKA Nobuhiro; JP
WAKAYAMA Shunsuke; JP
Priority Data:
2016-23187529.11.2016JP
Title (EN) NOVEL ESTER COMPOUND AND PIN1 INHIBITOR, INFLAMMATORY DISEASE THERAPEUTIC, AND COLON CANCER THERAPEUTIC IN WHICH SAID ESTER COMPOUND IS USED
(FR) NOUVEAU COMPOSÉ ESTER ET INHIBITEUR DE PIN1, AGENT THÉRAPEUTIQUE POUR MALADIE INFLAMMATOIRE ET AGENT THÉRAPEUTIQUE POUR CANCER DU CÔLON DANS LESQUELS LEDIT COMPOSÉ ESTER EST UTILISÉ
(JA) 新規エステル体化合物並びにそれを用いたPin1阻害剤、炎症性疾患治療剤及び大腸癌治療剤
Abstract:
(EN) The purpose of the present invention is to develop a therapeutic agent for inflammatory diseases such as inflammatory bowel disease and NASH, said therapeutic agent having few adverse effects and high efficacy. The present invention provides compounds represented by formula (I) or salts thereof, and a Pin1 inhibitor, pharmaceutical composition, an agent for the treatment or prevention of inflammatory disease, and an agent for the treatment or prevention of colon cancer that contain these compounds or salts.
(FR) Le but de la présente invention est de développer un agent thérapeutique pour des maladies inflammatoires telles que la maladie intestinale inflammatoire et la NASH, ledit agent thérapeutique ayant peu d'effets secondaires et une efficacité élevée. La présente invention concerne des composés représentés par la formule (I) ou des sels de ceux-ci, et un inhibiteur de Pin1, une composition pharmaceutique, un agent pour le traitement ou la prévention d'une maladie inflammatoire, et un agent pour le traitement ou la prévention du cancer du côlon qui contiennent ces composés ou ces sels.
(JA) 本発明は、副作用が少なく有効性の高い、炎症性腸疾患やNASH等の炎症性疾患の治療剤を開発することを目的とする。 本発明は、式(I)で表される化合物又はその塩、並びにこれらの化合物を含有するPin1阻害剤、医薬組成物、炎症性疾患の治療剤又は予防剤、及び大腸癌の治療剤又は予防剤を提供する。
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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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)