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ECSP11011258A - Pirimidinas fusionadas - Google Patents

Pirimidinas fusionadas

Info

Publication number
ECSP11011258A
ECSP11011258A EC2011011258A ECSP11011258A ECSP11011258A EC SP11011258 A ECSP11011258 A EC SP11011258A EC 2011011258 A EC2011011258 A EC 2011011258A EC SP11011258 A ECSP11011258 A EC SP11011258A EC SP11011258 A ECSP11011258 A EC SP11011258A
Authority
EC
Ecuador
Prior art keywords
fusionated
pyrimidins
tautomer
stereoisomer
salt
Prior art date
Application number
EC2011011258A
Other languages
English (en)
Inventor
Stuart Ince
Hartmut Rehwinkel
Matthias Vennemann
Gerrit Beneke
Thomas Beckers
Thomas Maier
Ulf Bomer
Thomas Bar
Armin Zulch
Andreas Strub
Ningshu Liu
Swen Holder
Florian Dhmel
Original Assignee
Bayer Pharma AG
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 Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of ECSP11011258A publication Critical patent/ECSP11011258A/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/04Drugs for disorders of the respiratory system for throat disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuestos de la fórmula (I), o un N-óxido, una sal, un tautómero o un estereoisómero de dicho compuesto, o una sal de dicho N-óxido, tautómero o estereoisómero, en donde el anillo B y la pirimidina a la cual está fusionado, R4, R5, R6, R7, m y n tienen los valores indicados en la descripción y en las reivindicaciones, que son inhibidores eficaces de la vía Pi3K/Akt, procesos para su producción y su uso como fármacos.
EC2011011258A 2009-02-13 2011-08-11 Pirimidinas fusionadas ECSP11011258A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09075072 2009-02-13
EP09152914 2009-02-16

Publications (1)

Publication Number Publication Date
ECSP11011258A true ECSP11011258A (es) 2011-10-31

Family

ID=42115325

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2011011258A ECSP11011258A (es) 2009-02-13 2011-08-11 Pirimidinas fusionadas

Country Status (28)

Country Link
US (1) US8957064B2 (es)
EP (1) EP2396330B1 (es)
JP (1) JP5777526B2 (es)
KR (1) KR20110114663A (es)
CN (1) CN102317291B (es)
AR (1) AR075253A1 (es)
AU (1) AU2010213192A1 (es)
BR (1) BRPI1008782A2 (es)
CA (1) CA2752105C (es)
CL (1) CL2011001972A1 (es)
CO (1) CO6410298A2 (es)
CR (1) CR20110432A (es)
CU (1) CU20110159A7 (es)
DO (1) DOP2011000260A (es)
EA (1) EA201101186A1 (es)
EC (1) ECSP11011258A (es)
ES (1) ES2580779T3 (es)
IL (1) IL213953A0 (es)
MA (1) MA33032B1 (es)
MX (1) MX2011008583A (es)
PE (1) PE20120534A1 (es)
SG (1) SG172898A1 (es)
SV (1) SV2011003997A (es)
TN (1) TN2011000404A1 (es)
TW (1) TW201036978A (es)
UY (1) UY32432A (es)
WO (1) WO2010091808A1 (es)
ZA (1) ZA201106663B (es)

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JP5926727B2 (ja) 2010-07-28 2016-05-25 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH 置換イミダゾ[1,2−b]ピリダジン
ES2549443T3 (es) * 2010-12-16 2015-10-28 Bayer Intellectual Property Gmbh Pirimido[1,2-b]indazoles sustituidos y su uso como moduladores de la ruta de PI3K/AKT
US9206185B2 (en) * 2011-04-07 2015-12-08 Bayer Intellectual Property Gmbh Imidazopyridazines as Akt kinase inhibitors
CN103467482B (zh) 2012-04-10 2017-05-10 上海璎黎药业有限公司 稠合嘧啶类化合物,其制备方法,中间体,组合物和应用
US9156831B2 (en) 2013-01-23 2015-10-13 Astrazeneca Ab Chemical compounds
CN104513254B (zh) 2013-09-30 2019-07-26 上海璎黎药业有限公司 稠合嘧啶类化合物、中间体、其制备方法、组合物和应用
US9656996B2 (en) 2013-10-16 2017-05-23 Shanghai Yingli Pharmaceutical Co., Ltd. Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
EA037361B1 (ru) * 2016-06-16 2021-03-18 Янссен Фармацевтика Нв Производные бициклического пиридина, пиразина и пиримидина в качестве ингибиторов pi3k бета
JP7595413B2 (ja) 2016-11-30 2024-12-06 ケース ウエスタン リザーブ ユニバーシティ 15-pgdh阻害剤とコルチコステロイドおよび/またはtnf阻害剤との組み合わせならびにその使用
CA3052466A1 (en) 2017-02-06 2018-08-09 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase activity
EP3600328A4 (en) 2017-03-24 2021-01-06 3100 Central Expressway LLC MERGED TRIAZOLO-PYRIMIDINE COMPOUNDS WITH USEFUL PHARMACEUTICAL APPLICATION
AU2018246321B2 (en) 2017-03-29 2021-07-29 Janssen Pharmaceutica Nv Quinoxaline and pyridopyrazine derivatives as PI3K-beta inhibitors
CN113507931B (zh) 2018-11-21 2025-05-27 卡斯西部储备大学 调节短链脱氢酶活性的组合物和方法
US11390626B2 (en) 2019-01-29 2022-07-19 Tosk, Inc. Pyrazolopyrimidine modulators of RAS GTPase
WO2020227491A1 (en) * 2019-05-07 2020-11-12 The Trustees Of The University Of Pennsylvania Deuterated triazolopyrimidines
CN112921405B (zh) * 2019-12-05 2023-06-27 成都先导药物开发股份有限公司 一种合成On-DNA吡唑并[1,5-a]嘧啶化合物的方法
CN111333655B (zh) * 2020-04-13 2021-07-13 武汉工程大学 一种三唑并嘧啶类化合物及其制备方法和应用
US12180220B2 (en) 2020-10-14 2024-12-31 Tosk, Inc. Heteroaryl modulators of RAS GTPase
CN114874221A (zh) * 2022-05-12 2022-08-09 广州佳途科技股份有限公司 一种rip2激酶抑制剂中间体及其合成方法
CN118359616A (zh) * 2023-01-19 2024-07-19 中国科学院上海有机化学研究所 一种作为治疗神经系统疾病和肿瘤的多环化合物

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NZ583267A (en) 2007-08-14 2012-03-30 Bayer Schering Pharma Ag Fused bicyclic pyrimidines

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Publication number Publication date
US8957064B2 (en) 2015-02-17
ZA201106663B (en) 2013-03-27
CN102317291B (zh) 2015-02-11
JP2012517963A (ja) 2012-08-09
CA2752105A1 (en) 2010-08-19
KR20110114663A (ko) 2011-10-19
UY32432A (es) 2010-09-30
ES2580779T3 (es) 2016-08-26
EP2396330A1 (en) 2011-12-21
US20130317002A1 (en) 2013-11-28
CU20110159A7 (es) 2012-02-15
MA33032B1 (fr) 2012-02-01
WO2010091808A1 (en) 2010-08-19
AR075253A1 (es) 2011-03-16
CO6410298A2 (es) 2012-03-30
CA2752105C (en) 2017-10-31
MX2011008583A (es) 2011-12-12
DOP2011000260A (es) 2011-10-15
TW201036978A (en) 2010-10-16
WO2010091808A8 (en) 2011-07-21
BRPI1008782A2 (pt) 2019-09-24
CR20110432A (es) 2011-10-24
SG172898A1 (en) 2011-08-29
PE20120534A1 (es) 2012-05-10
CN102317291A (zh) 2012-01-11
TN2011000404A1 (en) 2013-03-27
HK1165423A1 (en) 2012-10-05
AU2010213192A1 (en) 2011-08-04
EP2396330B1 (en) 2016-04-06
IL213953A0 (en) 2011-08-31
EA201101186A1 (ru) 2012-04-30
JP5777526B2 (ja) 2015-09-09
CL2011001972A1 (es) 2012-03-23
SV2011003997A (es) 2012-01-06

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