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MA33032B1 - Pyrimidines condensees - Google Patents

Pyrimidines condensees

Info

Publication number
MA33032B1
MA33032B1 MA34073A MA34073A MA33032B1 MA 33032 B1 MA33032 B1 MA 33032B1 MA 34073 A MA34073 A MA 34073A MA 34073 A MA34073 A MA 34073A MA 33032 B1 MA33032 B1 MA 33032B1
Authority
MA
Morocco
Prior art keywords
compounds
primidines
intensive
tautomer
stereoisomer
Prior art date
Application number
MA34073A
Other languages
Arabic (ar)
English (en)
Inventor
Matthias Vennemann
Thomas Bär
Thomas Maier
Swen HÖLDER
Gerrit Beneke
Florian Dehmel
Armin Zülch
Andreas Strub
Thomas Beckers
Stuart Ince
Hartmut Rehwinkel
Ningshu Liu
Ulf Bömer
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 MA33032B1 publication Critical patent/MA33032B1/fr

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

Abstract

La présente invention concerne des composés de formule (I) ou un N-oxyde, un sel, un tautomère ou un stéréo-isomère desdits composés, ou un sel dudit N-oxyde, tautomère ou stéréo-isomère desdits composés, où le cycle B et la pyrimidine avec laquelle il est condensé, R4, R5, R6, R7, m et n ont les significations telles que données dans la description et les revendications, qui sont des inhibiteurs efficaces de la voie Pi3K/Akt, des procédés pour leur production et leur utilisation en tant qu'agents pharmaceutiques.
MA34073A 2009-02-13 2010-02-02 Pyrimidines condensees MA33032B1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09075072 2009-02-13
EP09152914 2009-02-16
PCT/EP2010/000620 WO2010091808A1 (fr) 2009-02-13 2010-02-02 Pyrimidines condensées

Publications (1)

Publication Number Publication Date
MA33032B1 true MA33032B1 (fr) 2012-02-01

Family

ID=42115325

Family Applications (1)

Application Number Title Priority Date Filing Date
MA34073A MA33032B1 (fr) 2009-02-13 2010-02-02 Pyrimidines condensees

Country Status (28)

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

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PE20090944A1 (es) * 2007-08-14 2009-08-09 Bayer Schering Pharma Ag PIRIMIDINAS BICICLICAS FUSIONADAS COMO INHIBIDORES DE LA VIA Pi3K/AKT
CA2806655A1 (fr) 2010-07-28 2012-02-02 Bayer Intellectual Property Gmbh Imidazo[1,2-b]pyridazines substituees
CA2821777A1 (fr) * 2010-12-16 2012-06-21 Bayer Intellectual Property Gmbh Pyrimido [1,2-b]indazoles substitues et leur utilisation comme modulateurs de la voie pi3k/akt
SI2694510T1 (sl) * 2011-04-07 2016-02-29 Bayer Intellectual Property Gmbh Imidazopiridazini kot inhibitorji AKT kinaze
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
EP2948447B1 (fr) 2013-01-23 2016-09-21 Astrazeneca AB Composés chimiques
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
CN106831722B (zh) 2013-10-16 2019-08-30 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
CA3025594C (fr) * 2016-06-16 2024-06-18 Janssen Pharmaceutica Nv Derives bicycliques de pyridine, de pyrazine et de pyrimidine utilises en tant qu'inhibiteurs de pi3k beta
EP3548035A4 (fr) 2016-11-30 2020-07-22 Case Western Reserve University Combinaisons d'inhibiteurs de 15-pgdh avec des corcostéroïdes et/ou des inhibiteurs du tnf et leurs utilisations
CN110573154A (zh) 2017-02-06 2019-12-13 卡斯西部储备大学 调节短链脱氢酶活性的组合物和方法
KR102642378B1 (ko) 2017-03-24 2024-02-28 픽사이 인코포레이티드 유용한 약학적 적용을 갖는 융합된 트리아졸로-피리미딘 화합물
BR112019020309A2 (pt) 2017-03-29 2020-04-28 Janssen Pharmaceutica Nv derivados de quinoxalina e piridopirazina como inibidores de pi3k-beta
EA202191422A1 (ru) 2018-11-21 2021-10-21 Кейс Вестерн Ризерв Юниверсити Композиции и способы модулирования активности короткоцепочечной дегидрогеназы
WO2020159942A1 (fr) * 2019-01-29 2020-08-06 Tosk, Inc. Modulateurs de pyrazolopyrimidine de ras gtpase
US20220227772A1 (en) * 2019-05-07 2022-07-21 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
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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Also Published As

Publication number Publication date
MX2011008583A (es) 2011-12-12
CU20110159A7 (es) 2012-02-15
US20130317002A1 (en) 2013-11-28
AU2010213192A1 (en) 2011-08-04
CL2011001972A1 (es) 2012-03-23
JP2012517963A (ja) 2012-08-09
BRPI1008782A2 (pt) 2019-09-24
IL213953A0 (en) 2011-08-31
JP5777526B2 (ja) 2015-09-09
SV2011003997A (es) 2012-01-06
AR075253A1 (es) 2011-03-16
TN2011000404A1 (en) 2013-03-27
CN102317291A (zh) 2012-01-11
SG172898A1 (en) 2011-08-29
CA2752105A1 (fr) 2010-08-19
UY32432A (es) 2010-09-30
DOP2011000260A (es) 2011-10-15
WO2010091808A8 (fr) 2011-07-21
CA2752105C (fr) 2017-10-31
TW201036978A (en) 2010-10-16
WO2010091808A1 (fr) 2010-08-19
CR20110432A (es) 2011-10-24
EP2396330B1 (fr) 2016-04-06
US8957064B2 (en) 2015-02-17
ZA201106663B (en) 2013-03-27
EA201101186A1 (ru) 2012-04-30
KR20110114663A (ko) 2011-10-19
PE20120534A1 (es) 2012-05-10
EP2396330A1 (fr) 2011-12-21
ES2580779T3 (es) 2016-08-26
HK1165423A1 (en) 2012-10-05
ECSP11011258A (es) 2011-10-31
CN102317291B (zh) 2015-02-11
CO6410298A2 (es) 2012-03-30

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