WO2010058030A1 - Nouveaux composés - Google Patents

Nouveaux composés Download PDF

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Publication number
WO2010058030A1
WO2010058030A1 PCT/EP2009/065762 EP2009065762W WO2010058030A1 WO 2010058030 A1 WO2010058030 A1 WO 2010058030A1 EP 2009065762 W EP2009065762 W EP 2009065762W WO 2010058030 A1 WO2010058030 A1 WO 2010058030A1
Authority
WO
WIPO (PCT)
Prior art keywords
membered
compounds
group
independently
different
Prior art date
Application number
PCT/EP2009/065762
Other languages
English (en)
Inventor
Heinz Stadtmueller
Bodo Betzemeier
Ioannis Sapountzis
Original Assignee
Boehringer Ingelheim International Gmbh
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim International Gmbh filed Critical Boehringer Ingelheim International Gmbh
Priority to EP09756511.3A priority Critical patent/EP2367799B1/fr
Priority to ES09756511.3T priority patent/ES2690341T3/es
Priority to US13/130,069 priority patent/US20110288109A1/en
Publication of WO2010058030A1 publication Critical patent/WO2010058030A1/fr
Priority to US14/049,575 priority patent/US8785464B2/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention inclut des composés de Formule générale (1), où A, X, R1 et R2 sont tels que définis dans la revendication 1, lesdits composés étant adaptés au traitement de pathologies caractérisées par une prolifération cellulaire excessive ou anormale, et leur emploi dans l'élaboration d'un médicament présentant les propriétés susmentionnées.
PCT/EP2009/065762 2008-11-24 2009-11-24 Nouveaux composés WO2010058030A1 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP09756511.3A EP2367799B1 (fr) 2008-11-24 2009-11-24 Dérivés de 2-amino-5-trifluorométhyl-pyrimidine et leur utilisation comme inhibiteurs de ptk2-kinase
ES09756511.3T ES2690341T3 (es) 2008-11-24 2009-11-24 Derivados de 2-amino-5-trifluorometil-pirimidina y su uso como inhibidores de la quinasa PTK2
US13/130,069 US20110288109A1 (en) 2008-11-24 2009-11-24 New compounds
US14/049,575 US8785464B2 (en) 2008-11-24 2013-10-09 Pyrimidine derivatives that inhibit FAK/PTK2

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08169805 2008-11-24
EP08169805.2 2008-11-24

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/130,069 A-371-Of-International US20110288109A1 (en) 2008-11-24 2009-11-24 New compounds
US14/049,575 Continuation US8785464B2 (en) 2008-11-24 2013-10-09 Pyrimidine derivatives that inhibit FAK/PTK2

Publications (1)

Publication Number Publication Date
WO2010058030A1 true WO2010058030A1 (fr) 2010-05-27

Family

ID=40427570

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2009/065762 WO2010058030A1 (fr) 2008-11-24 2009-11-24 Nouveaux composés

Country Status (6)

Country Link
US (2) US20110288109A1 (fr)
EP (1) EP2367799B1 (fr)
AR (1) AR074209A1 (fr)
ES (1) ES2690341T3 (fr)
TW (1) TW201024281A (fr)
WO (1) WO2010058030A1 (fr)

Cited By (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011018518A1 (fr) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Préparation régiosélective de dérivés de 2-amino-5trifluorométhylpyrimidine
WO2011018517A1 (fr) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Préparation régiosélective de dérivés de 2-amino-5-trifluorométhylpyrimidine
WO2011151360A1 (fr) * 2010-06-04 2011-12-08 F. Hoffmann-La Roche Ag Dérivés d'aminopyrimidine au titre de modulateurs de lrrk2
WO2012041796A1 (fr) 2010-09-28 2012-04-05 Boehringer Ingelheim International Gmbh Stratification de patients cancéreux en fonction de leur sensibilité à une thérapie avec des inhibiteurs de ptk2
WO2012110774A1 (fr) 2011-02-17 2012-08-23 Cancer Therapeutics Crc Pty Limited Inhibiteurs sélectifs de fak
WO2012110773A1 (fr) 2011-02-17 2012-08-23 Cancer Therapeutics Crc Pty Limited Inhibiteurs de fak
WO2013079494A1 (fr) * 2011-11-29 2013-06-06 F. Hoffmann-La Roche Ag Dérivés 2-phénylaminopyrimidines en tant que modulateurs de kinase lrrk2 pour le traitement de la maladie de parkinson
US8466155B2 (en) 2009-10-02 2013-06-18 Boehringer Ingelheim International Gmbh Pyrimidines
WO2013113715A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés de pyrimidine fongicides
WO2013113791A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés de pyrimidine fongicides
WO2013113781A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés de pyrimidine fongicides i
WO2013113863A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés de pyrimidine fongicides
WO2013113716A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés de pyrimidine fongicides
WO2013113773A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés fongicides de pyrimidine
WO2013113782A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés de pyrimidine fongicides
WO2013113776A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés de pyrimidine fongicides
WO2013113719A1 (fr) 2012-02-03 2013-08-08 Basf Se Composés de pyrimidine fongicides ii
JP2013534227A (ja) * 2010-08-18 2013-09-02 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｆａｋ阻害剤としてのピリミジン誘導体
JP2014500295A (ja) * 2010-12-21 2014-01-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｉｇｆ１ｒ受容体阻害薬としてのオキシインドールピリミジン
KR20140097470A (ko) * 2011-11-30 2014-08-06 에프. 호프만-라 로슈 아게 Lrrk2에 대해 양전자 방사 단층촬영(pet) 이미징을 위한 불소-18 및 탄소-11 표지된 방사선 리간드
WO2015003658A1 (fr) * 2013-07-11 2015-01-15 Betta Pharmaceuticals Co., Ltd Modulateurs de la protéine tyrosine kinase et méthodes d'utilisation
JP2016003195A (ja) * 2014-06-16 2016-01-12 東ソ−・エフテック株式会社 ５−（トリフルオロメチル）ピリミジン誘導体及びその製造法
JP2016053012A (ja) * 2014-09-04 2016-04-14 東ソ−・エフテック株式会社 ４−フェニルチオ−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法
JP2016132620A (ja) * 2015-01-16 2016-07-25 東ソ−・エフテック株式会社 ４−アルコキシ−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法
GB2566622A (en) * 2014-05-08 2019-03-20 Tosoh F Tech Inc 5-(Trifluoromethyl)pyrimidine derivatives and method for producing same
CN111732548A (zh) * 2020-06-11 2020-10-02 浙江大学 N2-氨甲酰芳环-2-氨基嘧啶类衍生物及其医药用途
US20210355088A1 (en) * 2018-09-07 2021-11-18 H. Lee Moffitt Cancer Center And Research Institute, Inc. Brd4-jak2 inhibitors

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AR074209A1 (es) 2008-11-24 2010-12-29 Boehringer Ingelheim Int Derivados de pirimidina utiles para el tratamiento del cancer
TWI491605B (zh) 2008-11-24 2015-07-11 Boehringer Ingelheim Int 新穎化合物
US20220233298A1 (en) 2019-05-31 2022-07-28 W. L. Gore & Associates, Inc. A biocompatible membrane composite
BR112023019388A2 (pt) 2021-03-23 2023-11-07 Halia Therapeutics Inc Derivados de pirimidina úteis como inibidores de quinase lrrk2

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Cited By (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011018517A1 (fr) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Préparation régiosélective de dérivés de 2-amino-5-trifluorométhylpyrimidine
WO2011018518A1 (fr) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Préparation régiosélective de dérivés de 2-amino-5trifluorométhylpyrimidine
US8466155B2 (en) 2009-10-02 2013-06-18 Boehringer Ingelheim International Gmbh Pyrimidines
KR101531448B1 (ko) * 2010-06-04 2015-06-24 에프. 호프만-라 로슈 아게 Lrrk2 조절제로서의 아미노피리미딘 유도체
CN105837519A (zh) * 2010-06-04 2016-08-10 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂的氨基嘧啶衍生物
CN103038230A (zh) * 2010-06-04 2013-04-10 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂的氨基嘧啶衍生物
WO2011151360A1 (fr) * 2010-06-04 2011-12-08 F. Hoffmann-La Roche Ag Dérivés d'aminopyrimidine au titre de modulateurs de lrrk2
JP2013530954A (ja) * 2010-06-04 2013-08-01 エフ．ホフマン−ラ ロシュ アーゲー Ｌｒｒｋ２モジュレーターとしてのアミノピリミジン誘導体
EP3075730A1 (fr) * 2010-06-04 2016-10-05 F. Hoffmann-La Roche AG Dérivés d'aminopyrimidine comme modulateurs lrrk2
JP2013534227A (ja) * 2010-08-18 2013-09-02 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｆａｋ阻害剤としてのピリミジン誘導体
JP2017036268A (ja) * 2010-08-18 2017-02-16 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｆａｋ阻害剤としてのピリミジン誘導体
WO2012041796A1 (fr) 2010-09-28 2012-04-05 Boehringer Ingelheim International Gmbh Stratification de patients cancéreux en fonction de leur sensibilité à une thérapie avec des inhibiteurs de ptk2
JP2014500295A (ja) * 2010-12-21 2014-01-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｉｇｆ１ｒ受容体阻害薬としてのオキシインドールピリミジン
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US20140038993A1 (en) 2014-02-06
US20110288109A1 (en) 2011-11-24
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US8785464B2 (en) 2014-07-22

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