Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO2018124000) PYRIMIDINE DERIVATIVE
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/124000 International Application No.: PCT/JP2017/046504
Publication Date: 05.07.2018 International Filing Date: 26.12.2017
IPC:
C07D 239/28 (2006.01) ,A61K 31/505 (2006.01) ,A61K 31/506 (2006.01) ,A61P 11/00 (2006.01) ,C07D 239/34 (2006.01) ,C07D 239/38 (2006.01) ,C07D 239/42 (2006.01) ,C07D 239/47 (2006.01) ,C07D 239/48 (2006.01) ,C07D 239/52 (2006.01) ,C07D 239/56 (2006.01) ,C07D 239/58 (2006.01) ,C07D 401/06 (2006.01) ,C07D 401/12 (2006.01) ,C07D 403/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring 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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32
One oxygen, sulfur or nitrogen atom
34
One oxygen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32
One oxygen, sulfur or nitrogen atom
38
One sulfur atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32
One oxygen, sulfur or nitrogen atom
42
One nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
47
One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
48
Two nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
52
Two oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
56
One oxygen atom and one sulfur atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
58
Two sulfur atoms
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
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
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
04
directly linked by a ring-member-to-ring- member bond
Applicants:
第一三共株式会社 DAIICHI SANKYO COMPANY,LIMITED [JP/JP]; 東京都中央区日本橋本町三丁目5番1号 3-5-1,Nihonbashi Honcho,Chuo-ku, Tokyo 1038426, JP
Inventors:
武田 泰幸 TAKEDA, Yasuyuki; JP
鈴木 大和 SUZUKI, Yamato; JP
野地 寿治 NOJI, Toshiharu; JP
村藤 秀宣 MURAFUJI, Hidenobu; JP
宗岡 聡 MUNEOKA, Satoshi; JP
井上 英和 INOUE, Hidekazu; JP
高橋 美徳 TAKAHASHI, Bitoku; JP
稲葉 理恵 INABA, Rie; JP
Agent:
石橋 公樹 ISHIBASHI, Koki; JP
竹元 利泰 TAKEMOTO, Toshiyasu; JP
Priority Data:
2016-25385727.12.2016JP
Title (EN) PYRIMIDINE DERIVATIVE
(FR) DÉRIVÉ PYRIMIDINE
(JA) ピリミジン誘導体
Abstract:
(EN) The present invention addresses the problem of providing a compound that, when used in the treatment of cystic fibrosis, which is caused by a mutation of a cystic fibrosis transmembrane conductance regulator (CFTR), which is a kind of chloride channel, opens a chloride channel differing from the CFTR causative of the disease, and that is effective for the treatment of cystic fibrosis independently of the CFTR. The compound of the present invention is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof. The compound opens a calcium-activated chloride channel (CaCC) by means of G-protein-coupled receptor 39 (GPR39) agonistic activity and has intense chloride-ion-secreting activity.
(FR) La présente invention aborde le problème de la fourniture d'un composé qui, lorsqu'il est utilisé dans le traitement de la fibrose kystique, provoquée par une mutation d'un régulateur de conductance transmembranaire de fibrose kystique (CFTR), qui est un type de canal chlorure, ouvre un canal chlorure différent du CFTR responsable de la maladie, et qui est efficace pour le traitement de la fibrose kystique indépendamment du CFTR. La solution selon l'invention porte sur un composé représenté par la formule générale (I) ou un sel pharmaceutiquement acceptable de celui-ci. Le composé ouvre un canal chlorure activé par le calcium (CaCC) au moyen d'une activité agoniste du récepteur 39 couplé à la protéine G (GPR39) et a une activité de sécrétion d'ions de chlorure intense.
(JA) 本発明はクロライドチャネルの一種であるCystic Fibrosis Transmembrane conductance Regulator(CFTR)の変異によって発症する嚢胞性線維症において、病気の原因となるCFTRとは異なるクロライドチャネルを開口させ、CFTRに依存せずに嚢胞性線維症の治療に有効な化合物を提供することを課題とする。本発明の化合物は、G蛋白質共役型受容体39(GPR39)アゴニスト作用を介してカルシウム依存性クロライドチャネル(CaCC)を開口させ、強力なクロライドイオン分泌作用を有する下記一般式(I)で表される化合物またはその薬学上許容される塩である。
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, 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)