JP2007517006A5 - - Google Patents
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- Publication number
- JP2007517006A5 JP2007517006A5 JP2006546305A JP2006546305A JP2007517006A5 JP 2007517006 A5 JP2007517006 A5 JP 2007517006A5 JP 2006546305 A JP2006546305 A JP 2006546305A JP 2006546305 A JP2006546305 A JP 2006546305A JP 2007517006 A5 JP2007517006 A5 JP 2007517006A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- formula
- amino
- saturated
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 82
- 125000003545 alkoxy group Chemical group 0.000 claims 49
- 229920006395 saturated elastomer Polymers 0.000 claims 48
- 150000001875 compounds Chemical class 0.000 claims 28
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 24
- 125000003282 alkyl amino group Chemical group 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 239000001257 hydrogen Substances 0.000 claims 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 125000000524 functional group Chemical group 0.000 claims 14
- 125000001153 fluoro group Chemical group F* 0.000 claims 13
- 125000005843 halogen group Chemical group 0.000 claims 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 12
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 11
- -1 Amino, carbamoyl Chemical group 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 5
- 125000001786 isothiazolyl group Chemical group 0.000 claims 5
- 125000000842 isoxazolyl group Chemical group 0.000 claims 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 125000003363 1,3,5-triazinyl group Chemical group N1=C(N=CN=C1)* 0.000 claims 4
- 241001465754 Metazoa Species 0.000 claims 4
- 125000001246 bromo group Chemical group Br* 0.000 claims 4
- 125000001589 carboacyl group Chemical group 0.000 claims 4
- 125000001309 chloro group Chemical group Cl* 0.000 claims 4
- 125000002541 furyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 4
- 125000002971 oxazolyl group Chemical group 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000001425 triazolyl group Chemical group 0.000 claims 4
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 3
- 150000001412 amines Chemical class 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 108010090091 TIE-2 Receptor Proteins 0.000 claims 2
- 125000005236 alkanoylamino group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 125000002346 iodo group Chemical group I* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- UPQQXPKAYZYUKO-UHFFFAOYSA-N 2,2,2-trichloroacetamide Chemical compound OC(=N)C(Cl)(Cl)Cl UPQQXPKAYZYUKO-UHFFFAOYSA-N 0.000 claims 1
- 241001024304 Mino Species 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 150000001345 alkine derivatives Chemical class 0.000 claims 1
- 230000001772 anti-angiogenic effect Effects 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000000928 benzodioxinyl group Chemical group O1C(=COC2=C1C=CC=C2)* 0.000 claims 1
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000012948 isocyanate Substances 0.000 claims 1
- 150000002513 isocyanates Chemical class 0.000 claims 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- WTVXIBRMWGUIMI-UHFFFAOYSA-N trifluoro($l^{1}-oxidanylsulfonyl)methane Chemical group [O]S(=O)(=O)C(F)(F)F WTVXIBRMWGUIMI-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0330001A GB0330001D0 (en) | 2003-12-24 | 2003-12-24 | Compounds |
| GB0416850A GB0416850D0 (en) | 2004-07-29 | 2004-07-29 | Compounds |
| PCT/GB2004/005332 WO2005060969A1 (en) | 2003-12-24 | 2004-12-20 | Pyrimidines with tie2 (tek) activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007517006A JP2007517006A (ja) | 2007-06-28 |
| JP2007517006A5 true JP2007517006A5 (https=) | 2008-02-07 |
Family
ID=34712716
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006546305A Pending JP2007517006A (ja) | 2003-12-24 | 2004-12-20 | Tie2(tek)活性のあるピリミジン |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20080027076A1 (https=) |
| EP (1) | EP1737462B1 (https=) |
| JP (1) | JP2007517006A (https=) |
| AR (1) | AR046996A1 (https=) |
| AT (1) | ATE402705T1 (https=) |
| DE (1) | DE602004015509D1 (https=) |
| ES (1) | ES2309591T3 (https=) |
| TW (1) | TW200524607A (https=) |
| UY (1) | UY28700A1 (https=) |
| WO (1) | WO2005060969A1 (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AT410913B (de) * | 2001-08-14 | 2003-08-25 | Schelling Anlagenbau Gmbh | Auflagetisch für eine trennsäge mit einem maschinentisch |
| EP1737463B1 (en) * | 2003-12-24 | 2008-12-03 | AstraZeneca AB | Pyrimidines with tie2 (tek) activity |
| US7776869B2 (en) * | 2004-10-18 | 2010-08-17 | Amgen Inc. | Heteroaryl-substituted alkyne compounds and method of use |
| US20100048543A1 (en) * | 2005-02-01 | 2010-02-25 | Astrazeneca Ab | Pyrimidine compounds having ties (tek) inhibitory activity |
| WO2006082371A1 (en) * | 2005-02-01 | 2006-08-10 | Astrazeneca Ab | Pyrimidine compounds having tie2 (tek) inhibitory activity |
| GB0502418D0 (en) * | 2005-02-05 | 2005-03-16 | Astrazeneca Ab | Compounds |
| EP1893605A2 (en) * | 2005-03-31 | 2008-03-05 | AstraZeneca AB | Saminopyrimidine derivates with tie2 inhibiting activity |
| SI2495016T1 (sl) * | 2005-12-23 | 2020-04-30 | Ariad Pharmaceuticals, Inc. | Biciklične heteroarilne spojine |
| AU2015210454B2 (en) * | 2005-12-23 | 2016-10-27 | Takeda Pharmaceuticals U.S.A., Inc. | Bicyclic heteroaryl compounds |
| AU2013201243A1 (en) * | 2005-12-23 | 2013-03-28 | Ariad Pharmaceuticals, Inc. | Bicyclic heteroaryl compounds |
| CN101389338B (zh) * | 2005-12-23 | 2013-06-26 | 阿里亚德医药股份有限公司 | 双环杂芳基化合物 |
| AU2007249924B2 (en) | 2006-05-08 | 2013-07-04 | Ariad Pharmaceuticals, Inc. | Acetylenic heteroaryl compounds |
| BRPI0710331A2 (pt) | 2006-05-08 | 2012-03-20 | Ariad Pharmaceuticals, Inc | Compostos heteroarila monocíclicos para tratamento de câncer e composição |
| EP2022785A1 (en) | 2007-06-20 | 2009-02-11 | Bayer Schering Pharma Aktiengesellschaft | Alkynylpyrimidines as Tie2 kinase inhibitors |
| EP2070929A1 (en) * | 2007-12-11 | 2009-06-17 | Bayer Schering Pharma Aktiengesellschaft | Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
| EP2307456B1 (en) | 2008-06-27 | 2014-10-15 | Amgen Inc. | Ang-2 inhibition to treat multiple sclerosis |
| PE20110196A1 (es) | 2008-07-29 | 2011-04-03 | Boehringer Ingelheim Int | 5-alquinil-pirimidinas |
| EP2365809B8 (en) | 2008-11-12 | 2018-10-10 | Ariad Pharmaceuticals, Inc. | Pyrazinopyrazines and derivatives as kinase inhibitors |
| US8633183B2 (en) | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| US8618111B2 (en) * | 2010-01-26 | 2013-12-31 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| CA3022250A1 (en) | 2012-12-12 | 2014-06-12 | Ariad Pharmaceuticals, Inc. | Crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride |
| JP6665154B2 (ja) * | 2014-07-17 | 2020-03-13 | ノース・アンド・サウス・ブラザー・ファーマシー・インベストメント・カンパニー・リミテッド | 置換尿素誘導体及びその薬学的使用 |
| ES2921257T3 (es) * | 2016-06-20 | 2022-08-22 | Daegu Gyeongbuk Medical Innovation Found | Nuevo derivado de imidazopiridina, procedimiento para prepararlo y composición farmacéutica que contiene el mismo como ingrediente activo para prevenir o tratar el cáncer |
| ES2889749T3 (es) * | 2017-07-13 | 2022-01-13 | Sunshine Lake Pharma Co Ltd | Sal de derivado de urea sustituido y uso de la misma en medicina |
| US20210284647A1 (en) * | 2018-07-10 | 2021-09-16 | Voronoibio Inc. | N-(3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methylphenyl)-5-phenyl-4,5-dihydro-1h-pyrazole-1-carboxamide derivative, and pharmaceutical composition containing same as active ingredient for treating kinase-related diseases |
| US11746110B2 (en) | 2018-07-17 | 2023-09-05 | Shenzhen Targetrx, Inc. | Alkynyl (hetero) aromatic ring compounds used for inhibiting protein kinase activity |
| JP7505719B2 (ja) * | 2020-02-28 | 2024-06-25 | テグ-キョンプク メディカル イノベーション ファウンデーション | 3-((8-((1H-ピラゾール-4-イル)アミノ)イミダゾ[1,2-a]ピリジン-3-イル)エチニル)-N-フェニルベンズアミド誘導体、その調製法、それを活性成分として含有する癌の予防用又は治療用医薬組成物 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4064671B2 (ja) * | 2000-02-25 | 2008-03-19 | エフ.ホフマン−ラ ロシュ アーゲー | アデノシン受容体モジュレーター |
| DK1303495T3 (da) * | 2000-07-24 | 2010-09-20 | Krenitsky Pharmaceuticals Inc | Substituerede 5-alkylnylpyrimidiner med neurotrofisk aktivitet |
| US20030225273A1 (en) * | 2002-03-21 | 2003-12-04 | Michaelides Michael R. | Thiopyrimidine and isothiazolopyrimidine kinase inhibitors |
| US20030199525A1 (en) * | 2002-03-21 | 2003-10-23 | Hirst Gavin C. | Kinase inhibitors |
-
2004
- 2004-12-20 EP EP04806134A patent/EP1737462B1/en not_active Expired - Lifetime
- 2004-12-20 ES ES04806134T patent/ES2309591T3/es not_active Expired - Lifetime
- 2004-12-20 DE DE602004015509T patent/DE602004015509D1/de not_active Expired - Fee Related
- 2004-12-20 JP JP2006546305A patent/JP2007517006A/ja active Pending
- 2004-12-20 US US10/596,740 patent/US20080027076A1/en not_active Abandoned
- 2004-12-20 AT AT04806134T patent/ATE402705T1/de not_active IP Right Cessation
- 2004-12-20 WO PCT/GB2004/005332 patent/WO2005060969A1/en not_active Ceased
- 2004-12-23 UY UY28700A patent/UY28700A1/es not_active Application Discontinuation
- 2004-12-24 TW TW093140595A patent/TW200524607A/zh unknown
- 2004-12-27 AR ARP040104907A patent/AR046996A1/es unknown
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