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)
  • 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)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Otolaryngology (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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CL2008002398A1 (es) * 2007-08-14 2009-07-31 Bayer Ip Gmbh Compuestos derivados de 6-(fenil piperidina) pirimidinas fusionadas con imidazol, triazol o pirozol, inhibidores de la via pi3k/akt; composicion farmaceutica; combinacion farmaceutica; y uso de los compuestos para el tratamiento de la neoplasia benigna y/o maligna y para el cancer.
CA2806655A1 (fr) 2010-07-28 2012-02-02 Bayer Intellectual Property Gmbh Imidazo[1,2-b]pyridazines substituees
CN103370321B (zh) * 2010-12-16 2015-07-29 拜耳知识产权有限责任公司 取代的嘧啶并[1,2-b]吲唑及其作为PI3K/AKT途径的调节剂的用途
DK2694510T3 (en) * 2011-04-07 2016-01-18 Bayer Ip Gmbh IMIDAZOPYRIDAZINER 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
MA38287B1 (fr) 2013-01-23 2018-08-31 Astrazeneca Ab Nouveaux dérivés aminopyrazine pour le traitement ou la prévention du cancer
WO2015043398A1 (fr) 2013-09-30 2015-04-02 上海璎黎药业有限公司 Composé de pyrimidine condensée, intermédiaire, procédé de préparation s'y rapportant et composition et application correspondantes
CA2926596C (fr) 2013-10-16 2020-07-14 Shanghai Yingli Pharmaceutical Co., Ltd Compose heterocyclique condense, son procede de preparation, composition pharmaceutique et leurs utilisations
HRP20210508T1 (hr) * 2016-06-16 2021-05-28 Janssen Pharmaceutica Nv Biciklički derivati piridina, pirazina i pirimidina kao inhibitori pi3k beta
WO2018102552A1 (fr) 2016-11-30 2018-06-07 Case Western Reserve University Combinaisons d'inhibiteurs de 15-pgdh avec des corcostéroïdes et/ou des inhibiteurs du tnf et leurs utilisations
US11718589B2 (en) 2017-02-06 2023-08-08 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase
US11066410B2 (en) 2017-03-24 2021-07-20 3100 Central Expressway Llc Fused triazolo-pyrimidine compounds having useful pharmaceutical application
EA201992296A1 (ru) 2017-03-29 2020-02-12 Янссен Фармацевтика Нв Производные хиноксалина и пиридопиразина в качестве ингибиторов pi3k-бета
KR102921276B1 (ko) 2018-11-21 2026-02-03 케이스 웨스턴 리저브 유니버시티 단쇄 데히드로게나아제 활성을 조절하는 조성물 및 방법
US11390626B2 (en) 2019-01-29 2022-07-19 Tosk, Inc. Pyrazolopyrimidine modulators of RAS GTPase
WO2020214537A1 (fr) 2019-04-15 2020-10-22 Tosk, Inc. Modulateurs 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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CL2008002398A1 (es) 2007-08-14 2009-07-31 Bayer Ip Gmbh Compuestos derivados de 6-(fenil piperidina) pirimidinas fusionadas con imidazol, triazol o pirozol, inhibidores de la via pi3k/akt; composicion farmaceutica; combinacion farmaceutica; y uso de los compuestos para el tratamiento de la neoplasia benigna y/o maligna y para el cancer.

Also Published As

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

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