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1. (WO2006016715) PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2006/016715 International Application No.: PCT/JP2005/015031
Publication Date: 16.02.2006 International Filing Date: 11.08.2005
IPC:
C07D 487/04 (2006.01) ,A61K 31/519 (2006.01) ,A61P 3/04 (2006.01) ,A61P 3/10 (2006.01) ,A61P 9/00 (2006.01) ,A61P 9/10 (2006.01) ,A61P 11/00 (2006.01) ,A61P 17/06 (2006.01) ,A61P 19/02 (2006.01) ,A61P 19/10 (2006.01) ,A61P 25/28 (2006.01) ,A61P 29/00 (2006.01) ,A61P 31/04 (2006.01) ,A61P 35/00 (2006.01) ,A61P 37/06 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed 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
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
519
ortho- or peri-condensed with 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
04
Anorexiants; Antiobesity agents
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
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
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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
17
Drugs for dermatological disorders
06
Antipsoriatics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
02
for joint disorders, e.g. arthritis, arthrosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
08
for bone diseases, e.g. rachitism, Paget's disease
10
for osteoporosis
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
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04
Antibacterial agents
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
37
Drugs for immunological or allergic disorders
02
Immunomodulators
06
Immunosuppressants, e.g. drugs for graft rejection
Applicants:
小杉 知巳 KOSUGI, Tomomi [JP/JP]; JP (UsOnly)
今井 穣 IMAI, Minoru [JP/JP]; JP (UsOnly)
牧野 弘明 MAKINO, Hiroaki [JP/JP]; JP (UsOnly)
高桑 美香 TAKAKUWA, Mika [JP/JP]; JP (UsOnly)
鵜木 元 UNOKI, Gen [JP/JP]; JP (UsOnly)
片岡 健一郎 KATAOKA, Kenichiro [JP/JP]; JP (UsOnly)
ミッシェル デイル ロバート MITCHELL, Dale, Robert [GB/GB]; GB (UsOnly)
シンプソン ドナルド ジェームズ SIMPSON, Donald, James [GB/GB]; GB (UsOnly)
ハリス クリフォード ジョン HARRIS, Clifford, John [GB/GB]; GB (UsOnly)
リー ジョエル LE, Joelle [GB/GB]; GB (UsOnly)
山越 優子 YAMAKOSHI, Yuko [JP/JP]; JP (UsOnly)
帝人ファーマ株式会社 TEIJIN PHARMA LIMITED [JP/JP]; 〒1000011 東京都千代田区内幸町二丁目1番1号 Tokyo 1-1, Uchisaiwaicho 2-chome, Chiyoda-ku, Tokyo 1000011, JP (AllExceptUS)
Inventors:
小杉 知巳 KOSUGI, Tomomi; JP
今井 穣 IMAI, Minoru; JP
牧野 弘明 MAKINO, Hiroaki; JP
高桑 美香 TAKAKUWA, Mika; JP
鵜木 元 UNOKI, Gen; JP
片岡 健一郎 KATAOKA, Kenichiro; JP
ミッシェル デイル ロバート MITCHELL, Dale, Robert; GB
シンプソン ドナルド ジェームズ SIMPSON, Donald, James; GB
ハリス クリフォード ジョン HARRIS, Clifford, John; GB
リー ジョエル LE, Joelle; GB
山越 優子 YAMAKOSHI, Yuko; JP
Agent:
三原 秀子 MIHARA, Hideko; 〒1000011 東京都千代田区内幸町二丁目1番1号 株式会社帝人知的財産センター内 Tokyo c/o Teijin Intellectual Property Center Limited 1-1, Uchisaiwaicho 2-chome Chiyoda-ku, Tokyo 1000011, JP
Priority Data:
2004-23603513.08.2004JP
Title (EN) PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE
(FR) DÉRIVÉ DE LA PYRAZOLO[1,5-a]PYRIMIDINE
(JA) ピラゾロ[1,5-a]ピリミジン誘導体
Abstract:
(EN) Pyrazolo[1,5-a]pyrimidine derivatives of the formula (I) and pharmaceutically acceptable salts thereof exhibit excellent MAPKAP-K2 inhibiting activity. Consequently, pharmaceutical products comprising these as active ingredients are expected to be effective in the prevention or treatment of MAPKAP-K2 mediated diseases, for example, inflammatory diseases, autoimmune diseases, osteoclastic disorder, cancer and/or tumor growth.
(FR) L'invention concerne des dérivés de la pyrazolo[1,5-a]pyrimidine de formule (I) et des sels pharmaceutiquement acceptables de celle-ci et présentant une excellente activité d'inhibition de la MAPKAP-K2. Par conséquent, les produits pharmaceutiques contenant ceux-ci comme ingrédients actifs sont supposés être efficaces dans la prévention ou le traitement des maladies médiées par MAPKAP-K2, par exemple, les maladies inflammatoires, les maladies auto-immunes, l’affection ostéoclastique, les cancers et/ou la croissance l tumorale.
(JA)  式(Ⅰ)で表わされるピラゾロ[1,5−a]ピリミジン誘導体とそれらの医薬上許容される塩は、優れたMAPKAP−K2阻害活性を示す。従って、有効成分としてこの化合物を含む医薬品は、例えば炎症性疾患、自己免疫性疾患、破壊性骨障害、癌および/または腫瘍成長などのMAPKAP−K2媒介性疾患の治療または予防に有用であることが期待される。
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)