CN102118969B - 组胺h4受体的二氨基吡啶、二氨基嘧啶和二氨基哒嗪调节剂 - Google Patents

组胺h4受体的二氨基吡啶、二氨基嘧啶和二氨基哒嗪调节剂 Download PDF

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CN102118969B
CN102118969B CN200980131846.6A CN200980131846A CN102118969B CN 102118969 B CN102118969 B CN 102118969B CN 200980131846 A CN200980131846 A CN 200980131846A CN 102118969 B CN102118969 B CN 102118969B
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amine
methylamino
pyrrolidin
pyrimidin
pyridin
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Chinese (zh)
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CN102118969A (zh
Inventor
蔡辉
F·沙维斯
P·J·邓福德
A·J·格林斯潘
S·P·梅杜纳
J·A·奎罗斯
B·M·萨瓦尔
K·L·泰斯
R·L·瑟蒙德
魏建梅
R·L·沃林
X·张
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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CN200980131846.6A 2008-06-12 2009-06-11 组胺h4受体的二氨基吡啶、二氨基嘧啶和二氨基哒嗪调节剂 Expired - Fee Related CN102118969B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US6103908P 2008-06-12 2008-06-12
US61/061039 2008-06-12
US11442508P 2008-11-13 2008-11-13
US11441608P 2008-11-13 2008-11-13
US61/114425 2008-11-13
US61/114416 2008-11-13
PCT/US2009/047033 WO2009152325A1 (en) 2008-06-12 2009-06-11 Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine h4 receptor

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CN102118969A CN102118969A (zh) 2011-07-06
CN102118969B true CN102118969B (zh) 2017-03-08

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CN200980131846.6A Expired - Fee Related CN102118969B (zh) 2008-06-12 2009-06-11 组胺h4受体的二氨基吡啶、二氨基嘧啶和二氨基哒嗪调节剂

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US (3) US8841287B2 (https=)
EP (1) EP2315521B1 (https=)
JP (1) JP5658662B2 (https=)
KR (1) KR101600278B1 (https=)
CN (1) CN102118969B (https=)
AU (1) AU2009257434B2 (https=)
BR (1) BRPI0915720A2 (https=)
CA (1) CA2727684C (https=)
CO (1) CO6321192A2 (https=)
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PE (1) PE20110061A1 (https=)
WO (1) WO2009152325A1 (https=)
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Publication number Priority date Publication date Assignee Title
WO2007117399A2 (en) 2006-03-31 2007-10-18 Janssen Pharmaceutica N.V. Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine h4 receptor
BRPI0915720A2 (pt) 2008-06-12 2015-08-04 Janssen Pharmaceutica Nv Moduladores de diaminopiridina, pirimidina, e piridazina do receptor de histamina h4
BRPI0915526A2 (pt) * 2008-06-12 2016-01-26 Janssen Pharmaceutica Nv uso de um antagonista da histamina h4 para o tratamento de aderências pós-operatórias
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
CN102438993A (zh) * 2009-05-19 2012-05-02 陶氏益农公司 用于控制真菌的化合物和方法
WO2011078143A1 (ja) * 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
RU2014150494A (ru) * 2012-05-30 2016-07-20 Ф. Хоффманн-Ля Рош Аг Пирролидиногетероциклы
PT2964229T (pt) 2013-03-06 2020-03-23 Janssen Pharmaceutica Nv Moduladores de piridina benzimidazol-2-ilo do recetor h4 de histamina
WO2014147586A1 (en) * 2013-03-22 2014-09-25 Novartis Ag 1-(2-(ethylamino)pyrimidin-4-yl)pyrrolidin-2-ones as inhibitors of mutant idh
EP3055301B1 (en) * 2013-10-07 2019-11-20 Kadmon Corporation, LLC (2-(5-isoindolin-2-yl)pyrimidin-4-yl)-amine derivatives as rho kinase inhibitors for treating autoimmune diseases
ES2741831T3 (es) 2014-07-31 2020-02-12 Basf Se Proceso para la preparación de pirazoles
KR102585412B1 (ko) 2015-05-11 2023-10-05 바스프 에스이 4-아미노-피리다진의 제조 방법
WO2018071687A1 (en) * 2016-10-13 2018-04-19 The Regents Of The University Of California Methods of treating pruritis
WO2018082964A1 (en) 2016-11-04 2018-05-11 Basf Se Process for the production of pyridazinyl-amides in a one-pot synthesis
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
MX2024000273A (es) * 2021-07-01 2024-01-31 Aerie Pharmaceuticals Inc Azetidinil pirimidinas y usos de las mismas.
CN116354937B (zh) * 2021-12-27 2025-07-11 江苏恩华药业股份有限公司 吡啶(嘧啶)胺类衍生物及其应用
CA3260763A1 (en) * 2022-06-29 2024-01-04 Alcon Inc. AZETIDINYL PYRIMIDINES AND THEIR USES AS JAK INHIBITORS

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005054239A1 (en) * 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
WO2007072163A2 (en) * 2005-12-20 2007-06-28 Pfizer Limited Pyrimidine derivatives

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE759371A (fr) 1969-11-24 1971-05-24 Bristol Myers Co Azaspirodecanediones heterocycliques et procedes pour leur preparation
GB8609630D0 (en) 1986-04-19 1986-05-21 Pfizer Ltd Anti-arrhythmia agents
HU206337B (en) 1988-12-29 1992-10-28 Mitsui Petrochemical Ind Process for producing pyrimidine derivatives and pharmaceutical compositions
HK1002235A1 (en) 1989-12-28 1998-08-07 Pharmacia & Upjohn Company Diaromatic substituted anti-aids compounds
US5449676A (en) * 1991-04-26 1995-09-12 Byk Gulden Lomberg Chemische Fabrik Gmbh Pyridazines
CA2346659A1 (en) * 1998-10-06 2000-04-13 Michiyo Gyoten Condensed pyridazine compounds, their production and use
CA2394727A1 (en) 1999-12-28 2001-07-05 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
EP1317450B1 (en) 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
SE0004245D0 (sv) 2000-11-20 2000-11-20 Pharmacia Ab Novel compounds and their use
WO2002072548A2 (en) 2001-03-09 2002-09-19 Ortho-Mcneil Pharmaceutical, Inc. Heterocyclic compounds and their use as histamine h4 ligands.
US6825198B2 (en) 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
MXPA04004178A (es) * 2001-11-01 2004-09-06 Janssen Pharmaceutica Nv Heteroarilaminas como inhibidores de glucogeno cintasa cinasa 3beta.
EP1485378B1 (en) 2002-03-13 2008-06-18 Janssen Pharmaceutica N.V. Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase
DE60326436D1 (en) 2002-03-13 2009-04-16 Janssen Pharmaceutica Nv Aminoderivate als histone-deacetylase-inhibitoren
KR20040093692A (ko) * 2002-03-13 2004-11-08 얀센 파마슈티카 엔.브이. 히스톤 디아세틸라제의 신규한 저해제로서의 피페라지닐-,피페리디닐- 및 모르폴리닐-유도체
WO2004052862A1 (ja) 2002-12-10 2004-06-24 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその医薬用途
EP1437348A1 (fr) 2003-01-13 2004-07-14 L'oreal Dérivés de de la 6-méthyl-pyrimidine-2,4-diamine, procédé de synthèse, compositions les comprenant et utilisations comme agents neutralisants basiques
EP1505064A1 (en) 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
JP2007522233A (ja) * 2004-02-11 2007-08-09 アムジエン・インコーポレーテツド バニロイド受容体リガンド及び治療におけるそれらの使用
AU2005303893A1 (en) 2004-11-11 2006-05-18 Argenta Discovery Ltd Pyrimidine compounds as histamine modulators
JP2008524131A (ja) 2004-12-16 2008-07-10 エフ．ホフマン−ラ ロシュ アーゲー 抗肥満薬としてのピペラジニルピリジン誘導体
US20090306038A1 (en) * 2005-09-13 2009-12-10 Carceller Gonzalez Elena 2-Aminopyrimidine derivatives as modulators of the histamine H4 receptor activity
EP1767537A1 (en) 2005-09-21 2007-03-28 Cellzome (UK) Ltd. Pyrimidine compounds for the treatment of inflammatory disorders
SI1981874T1 (sl) 2006-01-19 2009-10-31 Janssen Pharmaceutica Nv Aminofenilni derivati kot novi inhibitorji histon deacetilaze
EP1829879A1 (en) 2006-02-10 2007-09-05 Cellzome (UK) Ltd. Amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007090854A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Azetidine amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007090853A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Enantiomers of amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007117399A2 (en) 2006-03-31 2007-10-18 Janssen Pharmaceutica N.V. Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine h4 receptor
GB0610909D0 (en) * 2006-06-05 2006-07-12 Merck Sharp & Dohme Therapeutic treatment
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
EP1920654A1 (en) 2006-09-13 2008-05-14 Syngeta Participations AG Novel pyridopyrazine N-oxides
US7985745B2 (en) 2006-10-02 2011-07-26 Abbott Laboratories Method for pain treatment
WO2008074445A1 (en) 2006-12-18 2008-06-26 Ucb Pharma, S.A. Novel tricyclic and heterotricyclic derivatives, processes for preparing them, pharmaceutical compositions thereof
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
EP2144877A1 (en) 2007-04-04 2010-01-20 UCB Pharma, S.A. Novel pyridine derivatives, processes for preparing them, pharmaceutical compositions thereof
WO2009068512A1 (en) 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
AR072084A1 (es) 2008-06-12 2010-08-04 Sanofi Aventis Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim
BRPI0915720A2 (pt) 2008-06-12 2015-08-04 Janssen Pharmaceutica Nv Moduladores de diaminopiridina, pirimidina, e piridazina do receptor de histamina h4
SI2356123T1 (sl) 2008-11-13 2013-01-31 F. Hoffmann-La Roche Ag Piro-5,6-dihidro-4h-2,3,5,10b-tetraaza-benzo(e)azuleni
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005054239A1 (en) * 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
WO2007072163A2 (en) * 2005-12-20 2007-06-28 Pfizer Limited Pyrimidine derivatives

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