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1. (WO2018181345) HETEROCYCLIC COMPOUND
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/181345 International Application No.: PCT/JP2018/012481
Publication Date: 04.10.2018 International Filing Date: 27.03.2018
IPC:
C07D 401/06 (2006.01) ,A61K 31/4725 (2006.01) ,A61K 31/5377 (2006.01) ,A61K 31/538 (2006.01) ,A61K 31/55 (2006.01) ,A61K 31/553 (2006.01) ,A61P 1/16 (2006.01) ,A61P 9/00 (2006.01) ,A61P 9/04 (2006.01) ,A61P 9/12 (2006.01) ,A61P 11/00 (2006.01) ,A61P 13/12 (2006.01) ,A61P 21/00 (2006.01) ,A61P 25/00 (2006.01) ,A61P 25/16 (2006.01) ,A61P 37/06 (2006.01) ,A61P 39/06 (2006.01) ,A61P 43/00 (2006.01) ,C07D 401/14 (2006.01) ,C07D 403/06 (2006.01) ,C07D 405/14 (2006.01) ,C07D 409/14 (2006.01) ,C07D 413/14 (2006.01) ,C07D 417/14 (2006.01) ,C07D 493/10 (2006.01)
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
06
linked by a carbon chain containing only aliphatic carbon atoms
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
472
Non-condensed isoquinolines, e.g. papaverine
4725
containing further heterocyclic rings
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
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
5377
not condensed and containing further heterocyclic rings, e.g. timolol
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
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
538
ortho- or peri-condensed with carbocyclic ring systems
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
553
having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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
16
for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
04
Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
12
Antihypertensives
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13
Drugs for disorders of the urinary system
12
of the kidneys
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21
Drugs for disorders of the muscular or neuromuscular system
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
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
37
Drugs for immunological or allergic disorders
02
Immunomodulators
06
Immunosuppressants, e.g. drugs for graft rejection
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
39
General protective or antinoxious agents
06
Free radical scavengers or antioxidants
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
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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
493
Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
Applicants: TAKEDA PHARMACEUTICAL COMPANY LIMITED[JP/JP]; 1-1, Doshomachi 4-chome, Chuo-ku, Osaka-shi, Osaka 5410045, JP
SCOHIA PHARMA, INC.[JP/JP]; 26-1, Muraoka-Higashi 2-chome, Fujisawa-shi, Kanagawa 2518555, JP
Inventors: KITAZAKI, Tomoyuki; JP
NISHIKAWA, Yoichi; JP
FUJIMOTO, Takuya; JP
KUBO, Osamu; JP
SASAKI, Minoru; JP
KINA, Asato; JP
MORIMOTO, Sachie; JP
KIKUCHI, Fumiaki; JP
TAKADA, Hiroyuki; JP
ISHICHI, Yuji; JP
TAKAKURA, Nobuyuki; JP
IKOMA, Minoru; JP
SATO, Kenjiro; JP
YAMASHITA, Toru; JP
YAMASAKI, Takeshi; JP
WATANABE, Koji; JP
MATSUMOTO, Shigemitsu; JP
FUKUSHI, Hideto; JP
NOGUCHI, Naoyoshi; JP
HARA, Ryoma; JP
KOBAYASHI, Toshitake; JP
MAEKAWA, Tsuyoshi; JP
Agent: TAKASHIMA, Hajime; JP
KAMADA, Mitsunori; JP
Priority Data:
2017-06395528.03.2017JP
Title (EN) HETEROCYCLIC COMPOUND
(FR) COMPOSÉ HÉTÉROCYCLIQUE
(JA) 複素環化合物
Abstract:
(EN) Provided is a compound which has an Nrf2-activating activity and is expected to be useful as a prophylactic or therapeutic agent for diseases associated with oxidative stress, particularly hepatitis (e.g., non-alcoholic steatohepatitis (NASH)), cardiovascular diseases (e.g., heart failure or pulmonary arterial hypertension), pulmonary diseases (e.g., chronic obstructive pulmonary disease (COPD)), kidney diseases (e.g., chronic kidney disease (CKD) or acute kidney injury (AKI)), central nervous system diseases (e.g., Parkinson's disease), mitochondrial diseases (e.g., Friedreich's ataxia, mitochondrial myopathy), autoimmune diseases (e.g., multiple sclerosis) and the like. The present invention relates to a compound represented by formula (I) [wherein each symbol is as defined in the description] or a salt thereof.
(FR) L'invention concerne un composé qui a une activité d'activation de Nrf2 et qui est supposé être utile en tant qu'agent prophylactique ou thérapeutique pour des maladies associées au stress oxydatif, en particulier l'hépatite (par exemple, la stéatohépatite non alcoolique (NASH)), des maladies cardiovasculaires (par exemple, une insuffisance cardiaque ou une hypertension artérielle pulmonaire), des maladies pulmonaires (par exemple, une maladie pulmonaire obstructive chronique (COPD)), des maladies rénales (par exemple, une maladie rénale chronique (CKD) ou une lésion rénale aiguë (AKI)), des maladies du système nerveux central (par exemple, la maladie de Parkinson), des maladies mitochondriales (par exemple l'ataxie de Friedreich, la myopathie mitochondriale), des maladies auto-immunes (par exemple, la sclérose en plaques) et analogues. La présente invention concerne un composé représenté par la formule (I) [dans laquelle chaque symbole est tel que défini dans la description] ou un sel de celui-ci.
(JA) Nrf2活性化作用を有し、酸化ストレスが関与する疾患、特に、肝炎(例えば、非アルコール性脂肪性肝炎(NASH))、心血管性疾患(例えば、心不全または肺動脈性高血圧症)、肺疾患(例えば、慢性閉塞性肺疾患(COPD))、腎疾患(例えば、慢性腎臓病(CKD)または急性腎障害(AKI))、中枢神経系疾患(例えば、パーキンソン病)、ミトコンドリア病(例えば、フリードライヒ運動失調症、ミトコンドリアミオパチー)、自己免疫疾患(例えば、多発性硬化症)などの予防または治療剤として有用であると期待される化合物を提供する。 本発明は、下記式(I):[式中、各記号は明細書記載の通りである。] で表される化合物またはその塩に関する。
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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)