WO2014093230A3 - Compositions et procédés de fabrication de composés pyrimidine et pyridine ayant une activité inhibitrice de btk - Google Patents

Compositions et procédés de fabrication de composés pyrimidine et pyridine ayant une activité inhibitrice de btk Download PDF

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Publication number
WO2014093230A3
WO2014093230A3 PCT/US2013/073895 US2013073895W WO2014093230A3 WO 2014093230 A3 WO2014093230 A3 WO 2014093230A3 US 2013073895 W US2013073895 W US 2013073895W WO 2014093230 A3 WO2014093230 A3 WO 2014093230A3
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pyrimidine
pyridine compounds
compositions
production
methods
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PCT/US2013/073895
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English (en)
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WO2014093230A2 (fr
Inventor
Lesley Liu-Bujalski
Theresa L. Johnson
Andreas Goutopoulos
Hui QIU
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Merck Patent Gmbh
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Publication of WO2014093230A2 publication Critical patent/WO2014093230A2/fr
Publication of WO2014093230A3 publication Critical patent/WO2014093230A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • 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
    • C07D213/60—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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/68—One oxygen atom attached in position 4
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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
    • C07D213/60—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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
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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
    • C07D213/60—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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D495/04—Ortho-condensed systems

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Abstract

La présente invention concerne de nouveaux composés pyrimidine et pyridine, qui sont fixés à une tête à éjection, et leur fabrication et utilisation pour le traitement de maladies hyperprolifératives comprenant, mais sans s'y limiter, le cancer, le lupus, des troubles allergiques, le syndrome de Sjögren et la polyarthrite rhumatoïde. L'invention concerne également des inhibiteurs de kinase comprenant, mais sans s'y limiter, des inhibiteurs de la tyrosine kinase de Bruton.
PCT/US2013/073895 2012-12-10 2013-12-09 Compositions et procédés de fabrication de composés pyrimidine et pyridine ayant une activité inhibitrice de btk WO2014093230A2 (fr)

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US201261735186P 2012-12-10 2012-12-10
US61/735,186 2012-12-10

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WO2014093230A2 WO2014093230A2 (fr) 2014-06-19
WO2014093230A3 true WO2014093230A3 (fr) 2014-08-28

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* Cited by examiner, † Cited by third party
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MX2017014163A (es) 2015-05-06 2018-08-15 Univ California Moduladores de k-ras.
CN108779095A (zh) * 2015-11-04 2018-11-09 默克专利有限公司 使用具有btk抑制活性的嘧啶和吡啶化合物治疗癌症的方法
NZ741294A (en) 2015-11-17 2023-07-28 Merck Patent Gmbh Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity
CN113444094B (zh) * 2016-07-20 2023-12-22 纳莹(上海)生物科技有限公司 一种荧光探针及其制备方法和用途
TW201900638A (zh) 2017-04-20 2019-01-01 加州大學董事會 Ｋ－ｒａｓ調節劑
AR113796A1 (es) * 2017-11-06 2020-06-10 Lilly Co Eli Compuestos inhibidores de tirosina cinasa de bruton (btk)
CN109824603B (zh) * 2017-11-23 2021-03-12 浙江省化工研究院有限公司 一种嘧啶胺类化合物、其制备方法及应用
CN108069911A (zh) * 2017-12-14 2018-05-25 中国药科大学 6－氨基－2－苯基嘧啶类化合物、制备方法和医药用途
US11325896B2 (en) 2017-12-20 2022-05-10 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
WO2019204442A1 (fr) * 2018-04-18 2019-10-24 Theras, Inc. Modulateurs de k-ras possédant une fraction cyanoacrylamide
CN112250666B (zh) * 2020-10-09 2022-01-14 广东东阳光药业有限公司 取代的嘧啶类化合物及其用途
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment

Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0658548A1 (fr) * 1993-12-17 1995-06-21 Tanabe Seiyaku Co., Ltd. Dérivés de la benzènesulfonamide et procédé de préparation
WO1996029301A1 (fr) * 1995-03-21 1996-09-26 Agrevo Uk Limited Composes fongicides
JPH0959160A (ja) * 1995-06-16 1997-03-04 Tanabe Seiyaku Co Ltd 医薬組成物
WO1997044325A1 (fr) * 1996-05-22 1997-11-27 Basf Aktiengesellschaft Derives d'acide de 2-(o-[pyrimidin-4-yl]methylenoxy)phenylacetique et leur utilisation pour lutter contre les champignons nuisibles et les parasites animaux
WO2005070934A1 (fr) * 2004-01-14 2005-08-04 Amgen Inc. Diazabicycloheptanes substitues et leur utilisation comme inhibiteurs de la proteine kinase
US20060217417A1 (en) * 2005-03-28 2006-09-28 Boehringer Ingelheim International Gmbh Pyridine derivatives useful as inhibitors of pkc-theta
WO2007084786A1 (fr) * 2006-01-20 2007-07-26 Novartis Ag Derives de pyrimidine utilises en tant qu’inhibiteurs de kinase pi-3
WO2010022725A1 (fr) * 2008-08-27 2010-03-04 Leo Pharma A/S Dérivés de pyridine comme récepteur de vegfr-2 et inhibiteurs de la protéine tyrosine kinase
JP2010209277A (ja) * 2009-03-12 2010-09-24 Konica Minolta Medical & Graphic Inc 有機圧電材料、超音波振動子および超音波探触子
WO2011060440A2 (fr) * 2009-11-16 2011-05-19 The Regents Of The University Of California Inhibiteurs de kinases
WO2011099764A2 (fr) * 2010-02-09 2011-08-18 Hanmi Holdings Co., Ltd. Nouveau dérivé de la pyrimidine pour l'inhibition de la croissance des cellules cancéreuses
US20120208815A1 (en) * 2007-03-01 2012-08-16 Matthew Burger Pim kinase inhibitors and methods of their use
WO2012158843A2 (fr) * 2011-05-17 2012-11-22 The Regents Of The University Of California Inhibiteurs de kinase
WO2012170976A2 (fr) * 2011-06-10 2012-12-13 Merck Patent Gmbh Compositions et procédés de production de composés pyrimidine et pyridine ayant une activité inhibitrice de btk

Patent Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0658548A1 (fr) * 1993-12-17 1995-06-21 Tanabe Seiyaku Co., Ltd. Dérivés de la benzènesulfonamide et procédé de préparation
WO1996029301A1 (fr) * 1995-03-21 1996-09-26 Agrevo Uk Limited Composes fongicides
JPH0959160A (ja) * 1995-06-16 1997-03-04 Tanabe Seiyaku Co Ltd 医薬組成物
WO1997044325A1 (fr) * 1996-05-22 1997-11-27 Basf Aktiengesellschaft Derives d'acide de 2-(o-[pyrimidin-4-yl]methylenoxy)phenylacetique et leur utilisation pour lutter contre les champignons nuisibles et les parasites animaux
WO2005070934A1 (fr) * 2004-01-14 2005-08-04 Amgen Inc. Diazabicycloheptanes substitues et leur utilisation comme inhibiteurs de la proteine kinase
US20060217417A1 (en) * 2005-03-28 2006-09-28 Boehringer Ingelheim International Gmbh Pyridine derivatives useful as inhibitors of pkc-theta
WO2007084786A1 (fr) * 2006-01-20 2007-07-26 Novartis Ag Derives de pyrimidine utilises en tant qu’inhibiteurs de kinase pi-3
US20120208815A1 (en) * 2007-03-01 2012-08-16 Matthew Burger Pim kinase inhibitors and methods of their use
WO2010022725A1 (fr) * 2008-08-27 2010-03-04 Leo Pharma A/S Dérivés de pyridine comme récepteur de vegfr-2 et inhibiteurs de la protéine tyrosine kinase
JP2010209277A (ja) * 2009-03-12 2010-09-24 Konica Minolta Medical & Graphic Inc 有機圧電材料、超音波振動子および超音波探触子
WO2011060440A2 (fr) * 2009-11-16 2011-05-19 The Regents Of The University Of California Inhibiteurs de kinases
WO2011099764A2 (fr) * 2010-02-09 2011-08-18 Hanmi Holdings Co., Ltd. Nouveau dérivé de la pyrimidine pour l'inhibition de la croissance des cellules cancéreuses
WO2012158843A2 (fr) * 2011-05-17 2012-11-22 The Regents Of The University Of California Inhibiteurs de kinase
WO2012170976A2 (fr) * 2011-06-10 2012-12-13 Merck Patent Gmbh Compositions et procédés de production de composés pyrimidine et pyridine ayant une activité inhibitrice de btk

Non-Patent Citations (12)

* Cited by examiner, † Cited by third party
Title
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; CORNELL, CLIVE LEONARD ET AL: "Preparation of 2-naphthyl-3-methoxyacrylates as agrochemical fungicides and pesticides", XP002725287, retrieved from STN Database accession no. 1996:716436 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; DENNY, WILLIAM A. ET AL: "Potential antitumor agents. 29. Quantitative structure-activity relationships for the antileukemic bisquaternary ammonium heterocycles", XP002725283, retrieved from STN Database accession no. 1979:66509 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; NISHIKUBO, YUICHI: "Organic piezoelectric materials, ultrasonic vibrators therewith, and ultrasound probes therewith", XP002720931, retrieved from STN Database accession no. 2010:1193753 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; PEGIADOU, S. ET AL: "The synthesis and characterization of new polymerizable pyrimidines: immobilization of the monomers onto hydrophilic graft copolymeric supports through radiation-induced copolymerization-grafting", XP002725282, retrieved from STN Database accession no. 1998:592481 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; RACK, MICHAEL ET AL: "Preparation of .alpha.-[2-(pyrimidinyloxymethyl)phenyl]acrylates as agrochemical fungicides and pesticides", XP002725285, retrieved from STN Database accession no. 1997:776155 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; SHULTZ, MICHAEL D. ET AL: "Optimization of the in vitro cardiac safety of hydroxamate-based Histone deacetylase inhibitors", XP002720930, retrieved from STN Database accession no. 2011:776102 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; YAMADA, KOICHIRO ET AL: "Preparation of (N-pyrimidinyl)benzenesulfonamide endothelin antagonists", XP002725288, retrieved from STN Database accession no. 1995:890091 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; YAMADA, KOICHIRO ET AL: "Preparation of pyrimidine derivatives as endothelin antagonists", XP002725286, retrieved from STN Database accession no. 1997:257401 *
DENNY, WILLIAM A. ET AL: "Potential antitumor agents. 29. Quantitative structure-activity relationships for the antileukemic bisquaternary ammonium heterocycles", JOURNAL OF MEDICINAL CHEMISTRY , 22(2), 134-50 CODEN: JMCMAR; ISSN: 0022-2623, 1979, DOI: 10.1021/JM00188A005 *
MI YOUNG CHA ET AL: "Synthesis and Biological Evaluation of Pyrimidine-Based Dual Inhibitors of Human Epidermal Growth Factor Receptor 1 (HER-1) and HER-2 Tyrosine Kinases", JOURNAL OF MEDICINAL CHEMISTRY, vol. 55, no. 6, 22 March 2012 (2012-03-22), pages 2846 - 2857, XP055104213, ISSN: 0022-2623, DOI: 10.1021/jm201758g *
PEGIADOU, S. ET AL: "The synthesis and characterization of new polymerizable pyrimidines: immobilization of the monomers onto hydrophilic graft copolymeric supports through radiation-induced copolymerization-grafting", JOURNAL OF APPLIED POLYMER SCIENCE , 70(2), 211-218 CODEN: JAPNAB; ISSN: 0021-8995, 1998, DOI: 10.1002/(SICI)1097-4628(19981010)70:2<211::AID-APP1>3.0.CO;2-X *
SHULTZ, MICHAEL D. ET AL: "Optimization of the in vitro cardiac safety of hydroxamate-based Histone deacetylase inhibitors", JOURNAL OF MEDICINAL CHEMISTRY , 54(13), 4752-4772 CODEN: JMCMAR; ISSN: 0022-2623, 2011, DOI: 10.1021/JM200388E *

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