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1. (WO2017099237) AMINOAZOLE DERIVATIVE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/099237 International Application No.: PCT/JP2016/086784
Publication Date: 15.06.2017 International Filing Date: 09.12.2016
IPC:
C07D 263/48 (2006.01) ,A61K 31/421 (2006.01) ,A61K 31/422 (2006.01) ,A61K 31/4245 (2006.01) ,A61K 31/426 (2006.01) ,A61K 31/427 (2006.01) ,A61K 31/428 (2006.01) ,A61K 31/433 (2006.01) ,A61K 31/4439 (2006.01) ,A61K 31/454 (2006.01) ,A61K 31/4709 (2006.01) ,A61K 31/4725 (2006.01) ,A61K 31/497 (2006.01) ,A61K 31/498 (2006.01) ,A61K 31/501 (2006.01) ,A61K 31/5377 (2006.01) ,A61P 21/00 (2006.01) ,A61P 21/04 (2006.01) ,A61P 43/00 (2006.01) ,C07C 335/12 (2006.01) ,C07C 335/18 (2006.01) ,C07D 249/08 (2006.01) ,C07D 277/56 (2006.01) ,C07D 277/82 (2006.01) ,C07D 413/12 (2006.01) ,C07D 417/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
263
Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02
not condensed with other rings
30
having two or three double bonds between ring members or between ring members and non-ring members
34
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
Nitrogen atoms not forming part of a nitro radical
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42
Oxazoles
421
1,3-Oxazoles, e.g. pemoline, trimethadione
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42
Oxazoles
422
not condensed and 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4245
Oxadiazoles
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
426
1,3-Thiazoles
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
427
not condensed and 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
428
condensed with carbocyclic 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
433
Thiadiazoles
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
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
454
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965
Non-condensed pyrazines
497
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
498
Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50
Pyridazines; Hydrogenated pyridazines
501
not condensed and 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
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
21
Drugs for disorders of the muscular or neuromuscular system
04
for myasthenia gravis
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
335
Thioureas, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
04
Derivatives of thiourea
06
having nitrogen atoms of thiourea groups bound to acyclic carbon atoms
10
of an unsaturated carbon skeleton
12
the carbon skeleton containing six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
335
Thioureas, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
04
Derivatives of thiourea
16
having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
18
being further substituted by singly-bound oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
249
Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
08
1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
32
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
56
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
60
condensed with carbocyclic rings or ring systems
62
Benzothiazoles
68
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 in position 2
82
Nitrogen atoms
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
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
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
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
Applicants:
帝人ファーマ株式会社 TEIJIN PHARMA LIMITED [JP/JP]; 東京都千代田区霞が関三丁目2番1号 2-1, Kasumigaseki 3-chome, Chiyoda-ku, Tokyo 1000013, JP
Inventors:
細田 信之介 HOSODA, Shinnosuke; JP
鵜木 元 UNOKI, Gen; JP
渡邉 秀和 WATANABE, Hidekazu; JP
佐々木 浩介 SASAKI, Kosuke; JP
柴田 淳 SHIBATA, Jun; JP
横山 絵美 YOKOYAMA, Emi; JP
堀江 恭平 HORIE, Kyohei; JP
高木 健一郎 TAKAGI, Kenichiro; JP
Agent:
青木 篤 AOKI, Atsushi; JP
石田 敬 ISHIDA, Takashi; JP
福本 積 FUKUMOTO, Tsumoru; JP
古賀 哲次 KOGA, Tetsuji; JP
渡辺 陽一 WATANABE, Yoichi; JP
中村 和美 NAKAMURA, Kazumi; JP
Priority Data:
2015-24206511.12.2015JP
Title (EN) AMINOAZOLE DERIVATIVE
(FR) DÉRIVÉ D’AMINOAZOLE
(JA) アミノアゾール誘導体
Abstract:
(EN) A compound represented by formula (I) and having a property of modulating the activity of an androgen receptor, or a pharmaceutically acceptable salt of the compound. X represents S or O; Z represents (Ra)n-A-(CR13R14)0-1-(CR11R12)0-1-; A represents an aryl group or a heteroaryl group; R1 represents an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an alkoxyalkyl group, an aryl group, an arylalkyl group, a heterocyclic group or a heterocyclic alkyl group; R2 represents a hydrogen atom, a halogen atom, an alkyl group, a cycloalkyl group or a phenyl group; R3 represents a hydrogen atom, a halogen atom, an alkyl group, a cycloalkyl group, an alkoxyalkyl group, an alkenyl group, an alkynyl group, a cycloalkenyl group, an aryl group, an arylalkyl group, a heterocyclic group, a heterocyclic alkyl group, an acyl group, a cycloalkylcarbonyl group, a benzoyl group, a spiroalkyl group, an adamantyl group, a silyl group or R31R32NCO-; and R4 and R5 independently represent a hydrogen atom, a halogen atom, an alkyl group, a phenyl group or a cycloalkyl group.
(FR) La présente invention concerne un composé représenté par la formule (I) et ayant une propriété de modulation de l'activité d'un récepteur d'androgène, ou un sel pharmaceutiquement acceptable du composé. X représente S ou O ; Z représente (Ra)n-A-(CR13R14)0-1-(CR11R12)0-1- ; A représente un groupe aryle ou un groupe hétéroaryle ; R1 représente un groupe alkyle, un groupe cycloalkyle, un groupe alcényle, un groupe alcynyle, un groupe alcoxyalkyle, un groupe aryle, un groupe arylalkyle, un groupe hétérocyclique ou un groupe alkyl-hétérocyclique ; R2 représente un atome d'hydrogène, un atome d'halogène, un groupe alkyle, un groupe cycloalkyle ou un groupe phényle ; R3 représente un atome d'hydrogène, un atome d'halogène, un groupe alkyle, un groupe cycloalkyle, un groupe alcoxyalkyle, un groupe alcényle, un groupe alcynyle, un groupe cycloalcényle, un groupe aryle, un groupe arylalkyle, un groupe hétérocyclique, un groupe alkyl-hétérocyclique, un groupe acyle, un groupe cycloalkylcarbonyle, un groupe benzoyle, un groupe spiroalkyle, un groupe adamantyle, un groupe silyle ou R31R32NCO- ; et R4 et R5 représentent indépendamment un atome d'hydrogène, un atome d'halogène, un groupe alkyle, un groupe phényle ou un groupe cycloalkyle.
(JA) 下記式で表される、アンドロゲン受容体の活性調節作用を有する化合物またはその医薬上許容される塩。XはS、Oを、Zは(Ra)n-A-(CR13R14)0-1-(CR11R12)0-1-を、Aはアリール、ヘテロアリールを、R1はアルキル、シクロアルキル、アルケニル、アルキニル、アルコキシアルキル、アリール、アリールアルキル、複素環、複素環アルキルを、R2は、水素、ハロゲン、アルキル、シクロアルキル、フェニルを、R3は、水素、ハロゲン、アルキル、シクロアルキル、アルコキシアルキル、アルケニル、アルキニル、シクロアルケニル、アリール、アリールアルキル、複素環、複素環アルキル、アシル、シクロアルキルカルボニル、ベンゾイル、スピロアルキル、アダマンチル、シリル、R31R32NCO-を、R4、R5は水素、ハロゲン、アルキル、フェニル、シクロアルキルを表す。
front page image
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, 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 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:
MYPI 2018701082CA2997689AR107040AU2016366443JPWO2017099237IN201817009533
SG11201804359SIL259900CN108368068ID2018/09371EP3388425KR1020180088412
PH1/2018/500892MX2018007000BR112018011389US20190031628