UY32432A - Compuestos de pirimidina fusionada como inhibidores de akt - Google Patents

Compuestos de pirimidina fusionada como inhibidores de akt

Info

Publication number
UY32432A
UY32432A UY0001032432A UY32432A UY32432A UY 32432 A UY32432 A UY 32432A UY 0001032432 A UY0001032432 A UY 0001032432A UY 32432 A UY32432 A UY 32432A UY 32432 A UY32432 A UY 32432A
Authority
UY
Uruguay
Prior art keywords
fusioned
pyrimidine compounds
akt inhibitors
tautomer
stereoisomer
Prior art date
Application number
UY0001032432A
Other languages
English (en)
Inventor
Dr Swen Holder
Hartmut Rehwinkel
Ince Stuart
Dr Matthias Vennemann
Beneke Gerrit
Dr Armin Zuelch
Dr Thomas Beckers
Dr Thomas Baer
Dr Thomas Maier
Dr Ulf Boemer
Dr Florian Dehmel
Dr Andreas Strub
Dr Ningshu Liu
Original Assignee
Bayer Schering 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 Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of UY32432A publication Critical patent/UY32432A/es

Links

Classifications

    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Neurology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (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 d 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
UY0001032432A 2009-02-13 2010-02-10 Compuestos de pirimidina fusionada como inhibidores de akt UY32432A (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
UY32432A true UY32432A (es) 2010-09-30

Family

ID=42115325

Family Applications (1)

Application Number Title Priority Date Filing Date
UY0001032432A UY32432A (es) 2009-02-13 2010-02-10 Compuestos de pirimidina fusionada como inhibidores de akt

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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WO2012080237A1 (en) * 2010-12-16 2012-06-21 Bayer Pharma Aktiengesellschaft Substituted pyrimido[1,2-b]indazoles and their use as modulators of the pi3k/akt pathway
HUE026323T2 (en) * 2011-04-07 2016-05-30 Bayer Ip Gmbh Imidazopyridazines as akt kinase inhibitors
US9499561B2 (en) 2012-04-10 2016-11-22 Shanghai Yingli Pharmaceutical Co., Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof
CA2897279C (en) 2013-01-23 2020-12-29 Astrazeneca Ab Aminopyrazine derivatives and pharmaceutical compositions thereof for use in the treatment of cancer
EP3053926B1 (en) 2013-09-30 2018-08-08 Shanghai Yingli Pharmaceutical Co. Ltd. Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof
CN104557872B (zh) 2013-10-16 2017-05-24 上海璎黎药业有限公司 稠合杂环化合物、其制备方法、药物组合物和用途
HRP20210508T1 (hr) * 2016-06-16 2021-05-28 Janssen Pharmaceutica Nv Biciklički derivati piridina, pirazina i pirimidina kao inhibitori pi3k beta
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JP2020514323A (ja) 2017-02-06 2020-05-21 ケース ウエスタン リザーブ ユニバーシティ 短鎖デヒドロゲナーゼ活性を調節する組成物と方法
AU2018237598B2 (en) 2017-03-24 2023-12-14 Piksci Inc. Fused triazolo-pyrimidine compounds having useful pharmaceutical application
WO2018178280A1 (en) 2017-03-29 2018-10-04 Janssen Pharmaceutica Nv Quinoxaline and pyridopyrazine derivatives as pi3k-beta inhibitors
KR102921276B1 (ko) 2018-11-21 2026-02-03 케이스 웨스턴 리저브 유니버시티 단쇄 데히드로게나아제 활성을 조절하는 조성물 및 방법
WO2020159942A1 (en) * 2019-01-29 2020-08-06 Tosk, Inc. Pyrazolopyrimidine modulators of ras gtpase
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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
GB2600384A (en) 2020-09-30 2022-05-04 Vaderis Therapeutics Ag Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia
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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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Publication number Publication date
CL2011001972A1 (es) 2012-03-23
TN2011000404A1 (en) 2013-03-27
US8957064B2 (en) 2015-02-17
ZA201106663B (en) 2013-03-27
CU20110159A7 (es) 2012-02-15
CR20110432A (es) 2011-10-24
ECSP11011258A (es) 2011-10-31
CN102317291B (zh) 2015-02-11
HK1165423A1 (en) 2012-10-05
DOP2011000260A (es) 2011-10-15
PE20120534A1 (es) 2012-05-10
MA33032B1 (fr) 2012-02-01
CN102317291A (zh) 2012-01-11
CA2752105A1 (en) 2010-08-19
WO2010091808A1 (en) 2010-08-19
JP5777526B2 (ja) 2015-09-09
MX2011008583A (es) 2011-12-12
SG172898A1 (en) 2011-08-29
EP2396330B1 (en) 2016-04-06
AR075253A1 (es) 2011-03-16
JP2012517963A (ja) 2012-08-09
WO2010091808A8 (en) 2011-07-21
US20130317002A1 (en) 2013-11-28
IL213953A0 (en) 2011-08-31
AU2010213192A1 (en) 2011-08-04
EP2396330A1 (en) 2011-12-21
SV2011003997A (es) 2012-01-06
CA2752105C (en) 2017-10-31
ES2580779T3 (es) 2016-08-26
BRPI1008782A2 (pt) 2019-09-24
TW201036978A (en) 2010-10-16
KR20110114663A (ko) 2011-10-19
CO6410298A2 (es) 2012-03-30
EA201101186A1 (ru) 2012-04-30

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