JP5781537B2 - ヒスタミンｈ４受容体アンタゴニストとしてのアミノアルキルピリミジン誘導体 - Google Patents
ヒスタミンｈ４受容体アンタゴニストとしてのアミノアルキルピリミジン誘導体 Download PDFInfo
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- JP5781537B2 JP5781537B2 JP2012545331A JP2012545331A JP5781537B2 JP 5781537 B2 JP5781537 B2 JP 5781537B2 JP 2012545331 A JP2012545331 A JP 2012545331A JP 2012545331 A JP2012545331 A JP 2012545331A JP 5781537 B2 JP5781537 B2 JP 5781537B2
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- 229940119240 Histamine H4 receptor antagonist Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims description 623
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- 125000000623 heterocyclic group Chemical group 0.000 claims description 122
- 125000003118 aryl group Chemical group 0.000 claims description 114
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- 229910052736 halogen Inorganic materials 0.000 claims description 91
- 229910052799 carbon Inorganic materials 0.000 claims description 86
- 150000002367 halogens Chemical class 0.000 claims description 82
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 82
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- 238000000034 method Methods 0.000 claims description 65
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- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 36
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- 125000005843 halogen group Chemical group 0.000 claims description 32
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- PLWRKPDLWQRXEK-UHFFFAOYSA-N 4-[3-(methylamino)azetidin-1-yl]-6-[(2-methylpropylamino)methyl]pyrimidin-2-amine Chemical compound C1C(NC)CN1C1=CC(CNCC(C)C)=NC(N)=N1 PLWRKPDLWQRXEK-UHFFFAOYSA-N 0.000 claims description 4
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- XSGFQLUNZSOVEQ-UHFFFAOYSA-N 4-[3-(methylamino)azetidin-1-yl]-6-[(2,2,2-trifluoroethylamino)methyl]pyrimidin-2-amine Chemical compound C1C(NC)CN1C1=CC(CNCC(F)(F)F)=NC(N)=N1 XSGFQLUNZSOVEQ-UHFFFAOYSA-N 0.000 claims description 3
- RWTXOMRUFONLJO-UHFFFAOYSA-N 4-[3-(methylamino)azetidin-1-yl]-6-[(propan-2-ylamino)methyl]pyrimidin-2-amine Chemical compound C1C(NC)CN1C1=CC(CNC(C)C)=NC(N)=N1 RWTXOMRUFONLJO-UHFFFAOYSA-N 0.000 claims description 3
- KNAYTBMVIPRJDN-UHFFFAOYSA-N 4-[[(2,2-diethylcyclopropyl)methylamino]methyl]-6-[3-(methylamino)azetidin-1-yl]pyrimidin-2-amine Chemical compound CCC1(CC)CC1CNCC1=CC(N2CC(C2)NC)=NC(N)=N1 KNAYTBMVIPRJDN-UHFFFAOYSA-N 0.000 claims description 3
- NEYYFVIUAGGKFC-VIFPVBQESA-N 4-[[[(2s)-butan-2-yl]amino]methyl]-6-[3-(methylamino)azetidin-1-yl]pyrimidin-2-amine Chemical compound NC1=NC(CN[C@@H](C)CC)=CC(N2CC(C2)NC)=N1 NEYYFVIUAGGKFC-VIFPVBQESA-N 0.000 claims description 3
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- YMBCJWGVCUEGHA-UHFFFAOYSA-M tetraethylammonium chloride Chemical compound [Cl-].CC[N+](CC)(CC)CC YMBCJWGVCUEGHA-UHFFFAOYSA-M 0.000 description 1
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Classifications
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Landscapes
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| US61/307,579 | 2010-02-24 | ||
| PCT/EP2010/070562 WO2011076878A1 (en) | 2009-12-23 | 2010-12-22 | Aminoalkylpyrimidine derivatives as histamine h4 receptor antagonists |
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| PH12021552978A1 (en) * | 2011-09-02 | 2022-08-22 | Incyte Holdings Corp | Heterocyclylamines as pi3k inhibitors |
| TWI797176B (zh) | 2017-10-17 | 2023-04-01 | 西班牙商帕羅製藥有限公司 | ４-胺基嘧啶化合物之合成 |
| GB201817047D0 (en) | 2018-10-19 | 2018-12-05 | Heptares Therapeutics Ltd | H4 antagonist compounds |
| JP2022165429A (ja) * | 2019-10-02 | 2022-11-01 | Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 | ヒスタミンｈ４受容体調節作用を有する新規トリアジン誘導体 |
| CN117018194A (zh) * | 2023-07-26 | 2023-11-10 | 同济大学 | 毒蕈碱型受体5型受体拮抗剂的用途 |
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| US6716978B2 (en) * | 1997-11-04 | 2004-04-06 | Pfizer Inc | Therapeutically active compounds based on indazole bioisostere replacement of catechol in PDE4 inhibitors |
| EP1562935B1 (de) * | 2002-10-28 | 2006-09-06 | Bayer HealthCare AG | Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren |
| US7494987B2 (en) * | 2002-11-25 | 2009-02-24 | Mochida Pharmaceutical Co., Ltd. | Agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient |
| 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 |
| KR20080004585A (ko) * | 2005-04-08 | 2008-01-09 | 바이엘 파마슈티칼스 코포레이션 | 피리미딘 유도체 및 암의 치료에서의 이의 용도 |
| KR20080043840A (ko) | 2005-09-13 | 2008-05-19 | 팔라우 파르마 에스에이 | 히스타민 ｈ4 수용체 활성의 조정자로서 2-아미노피리미딘유도체 |
| JP5191391B2 (ja) * | 2005-11-01 | 2013-05-08 | ターゲジェン インコーポレーティッド | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| WO2008031556A2 (en) | 2006-09-12 | 2008-03-20 | Ucb Pharma, S.A. | 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions |
| US7985745B2 (en) | 2006-10-02 | 2011-07-26 | Abbott Laboratories | Method for pain treatment |
| CL2008000467A1 (es) | 2007-02-14 | 2008-08-22 | Janssen Pharmaceutica Nv | Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma |
| AR069480A1 (es) * | 2007-11-30 | 2010-01-27 | Palau Pharma Sa | Derivados de 2-amino-pirimidina |
| PE20091524A1 (es) | 2007-12-19 | 2009-09-25 | Palau Pharma Sa | Derivados de 2-aminopirimidina |
| US8431580B2 (en) * | 2007-12-21 | 2013-04-30 | Palau Pharma, S.A. | 4-aminopyrimidine derivatives as histamine H4 receptor antagonists |
-
2010
- 2010-12-22 CN CN201080064585.3A patent/CN102803248B/zh active Active
- 2010-12-22 WO PCT/EP2010/070562 patent/WO2011076878A1/en not_active Ceased
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- 2010-12-22 EP EP10799037.6A patent/EP2516420B8/en active Active
- 2010-12-22 TW TW099145246A patent/TWI487697B/zh active
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- 2010-12-22 JP JP2012545331A patent/JP5781537B2/ja active Active
- 2010-12-22 US US13/518,729 patent/US8901146B2/en active Active
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Also Published As
| Publication number | Publication date |
|---|---|
| UA107818C2 (en) | 2015-02-25 |
| CN102803248B (zh) | 2015-09-16 |
| CA2785353C (en) | 2017-10-31 |
| IL220554A (en) | 2016-08-31 |
| PE20121505A1 (es) | 2012-11-05 |
| JP2013515698A (ja) | 2013-05-09 |
| EP2516420B1 (en) | 2018-08-22 |
| MX345142B (es) | 2017-01-18 |
| RU2573828C2 (ru) | 2016-01-27 |
| AU2010334804B2 (en) | 2015-04-02 |
| NZ601021A (en) | 2014-09-26 |
| KR20120124421A (ko) | 2012-11-13 |
| KR101740085B1 (ko) | 2017-05-25 |
| US8901146B2 (en) | 2014-12-02 |
| BR112012017126A2 (pt) | 2017-10-31 |
| EP2516420A1 (en) | 2012-10-31 |
| CA2785353A1 (en) | 2011-06-30 |
| TWI487697B (zh) | 2015-06-11 |
| AR079725A1 (es) | 2012-02-15 |
| MX2012007385A (es) | 2012-08-15 |
| TW201141840A (en) | 2011-12-01 |
| AU2010334804A1 (en) | 2012-07-19 |
| RU2012131223A (ru) | 2014-02-10 |
| EP2516420B8 (en) | 2018-10-17 |
| US20130018031A1 (en) | 2013-01-17 |
| WO2011076878A1 (en) | 2011-06-30 |
| CN102803248A (zh) | 2012-11-28 |
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