JP2011506566A5 - - Google Patents
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- Publication number
- JP2011506566A5 JP2011506566A5 JP2010538738A JP2010538738A JP2011506566A5 JP 2011506566 A5 JP2011506566 A5 JP 2011506566A5 JP 2010538738 A JP2010538738 A JP 2010538738A JP 2010538738 A JP2010538738 A JP 2010538738A JP 2011506566 A5 JP2011506566 A5 JP 2011506566A5
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- JP
- Japan
- Prior art keywords
- alkyl
- group
- compound according
- compound
- formula
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 49
- 150000001875 compounds Chemical class 0.000 claims 46
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims 4
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 229960001340 histamine Drugs 0.000 claims 3
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 230000000172 allergic effect Effects 0.000 claims 2
- 229910021529 ammonia Inorganic materials 0.000 claims 2
- 125000003725 azepanyl group Chemical group 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000001012 protector Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 *c1nc(C#CI)nc(N)c1 Chemical compound *c1nc(C#CI)nc(N)c1 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07382006.0 | 2007-12-21 | ||
| EP07382006 | 2007-12-21 | ||
| US3153408P | 2008-02-26 | 2008-02-26 | |
| US61/031,534 | 2008-02-26 | ||
| PCT/EP2008/067950 WO2009080721A2 (en) | 2007-12-21 | 2008-12-18 | 4 -aminopyrimidine derivatives as histamine h4 receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011506566A JP2011506566A (ja) | 2011-03-03 |
| JP2011506566A5 true JP2011506566A5 (enExample) | 2012-02-02 |
| JP5498396B2 JP5498396B2 (ja) | 2014-05-21 |
Family
ID=39473347
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010538738A Active JP5498396B2 (ja) | 2007-12-21 | 2008-12-18 | ヒスタミンｈ４受容体アンタゴニストとしての４−アミノピリミジン誘導体 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8431580B2 (enExample) |
| EP (1) | EP2235012B1 (enExample) |
| JP (1) | JP5498396B2 (enExample) |
| KR (1) | KR101639819B1 (enExample) |
| CN (1) | CN101903385B (enExample) |
| AR (1) | AR069814A1 (enExample) |
| AU (1) | AU2008341678B2 (enExample) |
| BR (1) | BRPI0820779B8 (enExample) |
| CA (1) | CA2709650C (enExample) |
| CL (1) | CL2008003811A1 (enExample) |
| CY (1) | CY1114427T1 (enExample) |
| DK (1) | DK2235012T3 (enExample) |
| ES (1) | ES2430210T3 (enExample) |
| HR (1) | HRP20130918T1 (enExample) |
| IL (1) | IL206413A (enExample) |
| PE (1) | PE20091330A1 (enExample) |
| PL (1) | PL2235012T3 (enExample) |
| PT (1) | PT2235012E (enExample) |
| RU (1) | RU2489430C2 (enExample) |
| SI (1) | SI2235012T1 (enExample) |
| TW (1) | TWI429440B (enExample) |
| UA (1) | UA101963C2 (enExample) |
| WO (1) | WO2009080721A2 (enExample) |
| ZA (1) | ZA201005179B (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102007026341A1 (de) | 2007-06-06 | 2008-12-11 | Merck Patent Gmbh | Benzoxazolonderivate |
| DE102007032507A1 (de) | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102007061963A1 (de) | 2007-12-21 | 2009-06-25 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102008019907A1 (de) | 2008-04-21 | 2009-10-22 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102008028905A1 (de) | 2008-06-18 | 2009-12-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate |
| US8586599B2 (en) | 2008-12-22 | 2013-11-19 | Merck Patent Gmbh | Polymorphic forms of 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof |
| EP2201982A1 (en) | 2008-12-24 | 2010-06-30 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Histamine H4 receptor antagonists for the treatment of vestibular disorders |
| PL2493895T3 (pl) | 2009-10-29 | 2017-10-31 | Vectura Ltd | Zawierające azot (N) heteroarylowe pochodne jako inhibitory kinazy JAK3 |
| EP2516420B8 (en) | 2009-12-23 | 2018-10-17 | Medicis Pharmaceutical Corporation | Aminoalkylpyrimidine derivatives as histamine h4 receptor antagonists |
| EP3378476A1 (en) | 2012-06-08 | 2018-09-26 | Sensorion | H4 receptor inhibitors for treating tinnitus |
| ES2946551T3 (es) | 2017-10-17 | 2023-07-20 | Palau Pharma S L U | Síntesis de compuestos de 4-aminopirimidina |
| GB201817047D0 (en) | 2018-10-19 | 2018-12-05 | Heptares Therapeutics Ltd | H4 antagonist compounds |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2361869C2 (ru) * | 2002-02-05 | 2009-07-20 | ХАЙ ПОЙНТ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Новые арил- и гетероарилпиперазины |
| EP1505064A1 (en) * | 2003-08-05 | 2005-02-09 | Bayer HealthCare AG | 2-Aminopyrimidine derivatives |
| WO2005054239A1 (en) * | 2003-12-05 | 2005-06-16 | Bayer Healthcare Ag | 2-aminopyrimidine derivatives |
| CA2551944A1 (en) * | 2003-12-15 | 2005-06-30 | Almirall Prodesfarma Ag | 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists |
| EP1888565B1 (en) * | 2005-04-11 | 2011-03-23 | Almirall, S.A. | 2, 6-di (hetero) aryl -4-amido-pyrimidines as adenosine receptor antagonists |
| WO2007031529A1 (en) * | 2005-09-13 | 2007-03-22 | Palau Pharma, S.A. | 2-aminopyrimidine derivatives as modulators of the histamine h4 receptor activity |
| WO2007084914A2 (en) * | 2006-01-17 | 2007-07-26 | Neurocrine Biosciences, Inc. | Phenoxy-substituted pyrimidines as adenosine receptor antagonists |
-
2008
- 2008-12-18 RU RU2010130418/04A patent/RU2489430C2/ru active
- 2008-12-18 CA CA2709650A patent/CA2709650C/en active Active
- 2008-12-18 AU AU2008341678A patent/AU2008341678B2/en active Active
- 2008-12-18 HR HRP20130918AT patent/HRP20130918T1/hr unknown
- 2008-12-18 TW TW097149462A patent/TWI429440B/zh active
- 2008-12-18 KR KR1020107013477A patent/KR101639819B1/ko active Active
- 2008-12-18 DK DK08865603.8T patent/DK2235012T3/da active
- 2008-12-18 US US12/809,371 patent/US8431580B2/en active Active
- 2008-12-18 CN CN200880121970XA patent/CN101903385B/zh active Active
- 2008-12-18 EP EP08865603.8A patent/EP2235012B1/en active Active
- 2008-12-18 BR BRPI0820779A patent/BRPI0820779B8/pt active IP Right Grant
- 2008-12-18 PL PL08865603T patent/PL2235012T3/pl unknown
- 2008-12-18 AR ARP080105539A patent/AR069814A1/es unknown
- 2008-12-18 SI SI200831056T patent/SI2235012T1/sl unknown
- 2008-12-18 PT PT88656038T patent/PT2235012E/pt unknown
- 2008-12-18 ES ES08865603T patent/ES2430210T3/es active Active
- 2008-12-18 UA UAA201007805A patent/UA101963C2/ru unknown
- 2008-12-18 JP JP2010538738A patent/JP5498396B2/ja active Active
- 2008-12-18 CL CL2008003811A patent/CL2008003811A1/es unknown
- 2008-12-18 WO PCT/EP2008/067950 patent/WO2009080721A2/en not_active Ceased
- 2008-12-19 PE PE2008002160A patent/PE20091330A1/es active IP Right Grant
-
2010
- 2010-06-16 IL IL206413A patent/IL206413A/en active IP Right Grant
- 2010-07-20 ZA ZA2010/05179A patent/ZA201005179B/en unknown
-
2013
- 2013-09-10 CY CY20131100781T patent/CY1114427T1/el unknown