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

    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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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UY31293A1 (es) * 2007-08-14 2009-03-31 Pirimidinas biciclicas fusionadas
ES2539257T3 (es) 2010-07-28 2015-06-29 Bayer Intellectual Property Gmbh Imidazo[1,2-b]piridazinas sustituidas
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
EA024890B1 (ru) * 2011-04-07 2016-10-31 Байер Интеллектчуал Проперти Гмбх Имидазопиридазины в качестве ингибиторов akt киназы
WO2013152717A1 (fr) 2012-04-10 2013-10-17 上海昀怡健康管理咨询有限公司 Composé de pyrimidine condensé, et procédé de préparation, intermédiaire, composition et utilisations dudit composé
RU2644769C2 (ru) 2013-01-23 2018-02-14 Астразенека Аб Химические соединения
JP6441910B2 (ja) 2013-09-30 2018-12-19 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、中間体、その調製方法、組成物及び使用
WO2015055071A1 (fr) 2013-10-16 2015-04-23 上海璎黎药业有限公司 Composé hétérocyclique condensé, son procédé de préparation, composition pharmaceutique et leurs utilisations
KR102472453B1 (ko) * 2016-06-16 2022-11-29 얀센 파마슈티카 엔.브이. Pi3k 베타 저해제로서의 이환식 피리딘, 피라진, 및 피리미딘 유도체
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
AU2018215678A1 (en) 2017-02-06 2019-08-22 Board Of Regents Of The University Of Texas System Compositions and methods of modulating short-chain dehydrogenase activity
KR102642378B1 (ko) 2017-03-24 2024-02-28 픽사이 인코포레이티드 유용한 약학적 적용을 갖는 융합된 트리아졸로-피리미딘 화합물
EP3601254B1 (fr) 2017-03-29 2022-05-25 Janssen Pharmaceutica NV Dérivés de pyridopyrazine et de quinoxaline en tant qu'inhibiteurs de pi3k-beta
IL321451A (en) 2018-11-21 2025-08-01 Univ Case Western Reserve Compositions and methods of modulating short-chain dehydrogenase activity
US11390626B2 (en) 2019-01-29 2022-07-19 Tosk, Inc. Pyrazolopyrimidine modulators of RAS GTPase
US12528796B2 (en) 2019-04-15 2026-01-20 Tosk, Inc. Modulators of 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
MX2022010258A (es) 2020-02-21 2023-01-24 Univ Case Western Reserve Composiciones y métodos para tratar la lesión renal.
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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UY31293A1 (es) 2007-08-14 2009-03-31 Pirimidinas biciclicas fusionadas

Also Published As

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

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