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PE20140570A1 - Pirrolotriazinas sustituidas con hidroximetilarilo y sus usos - Google Patents

Pirrolotriazinas sustituidas con hidroximetilarilo y sus usos

Info

Publication number
PE20140570A1
PE20140570A1 PE2013002774A PE2013002774A PE20140570A1 PE 20140570 A1 PE20140570 A1 PE 20140570A1 PE 2013002774 A PE2013002774 A PE 2013002774A PE 2013002774 A PE2013002774 A PE 2013002774A PE 20140570 A1 PE20140570 A1 PE 20140570A1
Authority
PE
Peru
Prior art keywords
triazin
methanol
amino
pyrrolotriazines
compounds
Prior art date
Application number
PE2013002774A
Other languages
English (en)
Inventor
Jurgen Klar
Verena Voehringer
Joachim Telser
Mario Lobelll
Frank Sussmeier
Volkhart Min-Jian Li
Michael Bottger
Stefan Golz
Dieter Lang
Karl-Heinz Schlemmer
Thomas Schlange
Andreas Schall
Wenlang Fu
Original Assignee
Bayer Ip Gmbh
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47436537&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20140570(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Ip Gmbh, Bayer Pharma AG filed Critical Bayer Ip Gmbh
Publication of PE20140570A1 publication Critical patent/PE20140570A1/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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRROLOTRIAZINAS DE FORMULA (I) DONDE A ES N O CR2, EN DONDE R2 ES H, F O Cl; R1 ES H, F, METILO, ETILO, ENTRE OTROS; Z ES ALQUILO(C1-C4), CICLOALQUILO(C3-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: [4-(4-AMINO-7-PROPILPIRROLO[2,1-f][1,2,4]TRIAZIN-5-IL)FENIL]METANOL; [4-(4-AMINO-7-PROPILPIRROLO[2,1-f][1,2,4]TRIAZIN-5-IL)-2,6-DIFLUOROFENIL]METANOL; {4-AMINO-5-[3,5-DIFLUORO-4-(HIDROXIMETIL)FENIL]PIRROLO[2,1-f][1,2,4]TRIAZIN-7-IL}-(CICLOPROPIL)METANOL; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DEL RECEPTOR DE ACTIVINA TIPO QUINASA-1 (ALK1) SIENDO UTILES EN EL TRATAMIENTO DE DEGENERACION MACULAR RELACIONADA CON LA EDAD (DME), NEOVASCULARIZACION COROIDEA (NVC), RETINOPATIA DIABETICA, EDEMA MACULAR DIABETICO (EMD)
PE2013002774A 2011-07-01 2012-06-26 Pirrolotriazinas sustituidas con hidroximetilarilo y sus usos PE20140570A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161503840P 2011-07-01 2011-07-01
EP12161547 2012-03-27

Publications (1)

Publication Number Publication Date
PE20140570A1 true PE20140570A1 (es) 2014-04-28

Family

ID=47436537

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013002774A PE20140570A1 (es) 2011-07-01 2012-06-26 Pirrolotriazinas sustituidas con hidroximetilarilo y sus usos

Country Status (25)

Country Link
US (1) US9040691B2 (es)
EP (1) EP2726482B1 (es)
JP (1) JP5955953B2 (es)
KR (1) KR20140036269A (es)
CN (1) CN103764657B (es)
AP (1) AP3529A (es)
AR (1) AR087017A1 (es)
AU (1) AU2012280508A1 (es)
BR (1) BR112014000049A2 (es)
CA (1) CA2840518A1 (es)
CO (1) CO6870031A2 (es)
CU (1) CU20130170A7 (es)
DO (1) DOP2013000300A (es)
EA (1) EA023775B1 (es)
EC (1) ECSP13013120A (es)
ES (1) ES2598027T3 (es)
GT (1) GT201300313A (es)
IL (1) IL229533A0 (es)
MA (1) MA35601B1 (es)
MX (1) MX2013014315A (es)
PE (1) PE20140570A1 (es)
PH (1) PH12013502695A1 (es)
SG (1) SG195100A1 (es)
UY (1) UY34167A (es)
WO (1) WO2013004551A1 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI577670B (zh) 2011-05-10 2017-04-11 基利科學股份有限公司 充當離子通道調節劑之稠合雜環化合物
NO3175985T3 (es) 2011-07-01 2018-04-28
TWI622583B (zh) 2011-07-01 2018-05-01 基利科學股份有限公司 作為離子通道調節劑之稠合雜環化合物
EP2809673B1 (en) * 2012-01-31 2016-11-02 Nanjing Allgen Pharma Co. Ltd. Spirocyclic molecules as bruton's tyrosine kinase inhibitors
CA2945149A1 (en) * 2014-04-10 2015-10-15 Lankenau Institute For Medical Research Methods and compositions for the treatment of ocular diseases and disorders
MX382659B (es) 2014-05-28 2025-03-11 Bayer Cropscience Ag Proceso para la preparación de derivados de tiazol.
US10214537B2 (en) 2014-10-22 2019-02-26 Bristol-Myers Squibb Company Bicyclic heteroaryl amine compounds
US10023576B2 (en) 2014-10-22 2018-07-17 Bristol-Myers Squibb Company Heteroaryl substituted pyrrolotriazine amine compounds as PI3K inhibitors
CA2968464A1 (en) 2014-11-25 2016-06-02 Bayer Pharma Aktiengesellschaft Substituted pyridobenzodiazepinone-derivatives and use thereof
EP3283475B1 (en) 2015-04-16 2019-10-16 Merck Patent GmbH 3-(1h-benzimidazol-2-yl)-1h-pyridin-2-one derivatives
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
TWI753892B (zh) 2016-03-28 2022-02-01 美商英塞特公司 作為tam抑制劑之吡咯并三嗪化合物
CN109111447A (zh) * 2017-06-23 2019-01-01 中国科学院上海药物研究所 7-位取代吡咯并三嗪类化合物或其药学上可用的盐,及其制备方法和用途
MA50655B1 (fr) 2017-09-27 2021-11-30 Incyte Corp Sels de dérivés de pyrrolotriazine utiles en tant qu'inhibiteurs de tam
MD3813800T2 (ro) 2018-06-29 2025-10-31 Incyte Corp Formulări de inhibitor al AXL/MER
CN115697343A (zh) 2020-03-06 2023-02-03 因赛特公司 包含axl/mer和pd-1/pd-l1抑制剂的组合疗法
CN120530116A (zh) 2022-11-04 2025-08-22 百时美施贵宝公司 Ret-ldd蛋白抑制剂

Family Cites Families (18)

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CA2373990C (en) * 1999-05-21 2007-05-08 Bristol-Myers Squibb Company Pyrrolotriazine inhibitors of kinases
CA2494179C (en) 2002-08-08 2012-04-24 Kissei Pharmaceutical Co., Ltd. Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
US7148226B2 (en) 2003-02-21 2006-12-12 Agouron Pharmaceuticals, Inc. Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
UY28931A1 (es) 2004-06-03 2005-12-30 Bayer Pharmaceuticals Corp Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis
DE102005042742A1 (de) * 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
JP5116687B2 (ja) * 2005-11-02 2013-01-09 バイエル・ファルマ・アクチェンゲゼルシャフト がんおよび他の過剰増殖性疾患の処置のためのピロロ[2,1−f][1,2,4]トリアジン−4−イルアミンIGF−1Rキナーゼ阻害剤
US7514435B2 (en) * 2005-11-18 2009-04-07 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
BRPI0619146A2 (pt) 2005-12-02 2011-09-13 Bayer Pharmaceuticals Corp derivados de 4-amino-pirroltriazina substituìda úteis no tratamento de disordens e doenças hiperproliferativas associadas com angiogênesis
PE20070855A1 (es) 2005-12-02 2007-10-14 Bayer Pharmaceuticals Corp Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas
CA2635231C (en) 2005-12-29 2014-07-15 Abbott Laboratories Protein kinase inhibitors
EP1873157A1 (en) * 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
CN101522682A (zh) * 2006-10-30 2009-09-02 诺瓦提斯公司 作为抗炎剂的杂环化合物
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US8124759B2 (en) 2007-05-09 2012-02-28 Abbott Laboratories Inhibitors of protein kinases
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JP5456681B2 (ja) * 2007-10-17 2014-04-02 ノバルティス アーゲー ALK阻害剤として有用なイミダゾ[1,2−a]ピリジン誘導体
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JP5656976B2 (ja) 2009-04-29 2015-01-21 ローカス ファーマシューティカルズ インコーポレイテッド ピロロトリアジン化合物

Also Published As

Publication number Publication date
AP2014007378A0 (en) 2014-01-31
CA2840518A1 (en) 2013-01-10
GT201300313A (es) 2014-11-13
EP2726482A1 (en) 2014-05-07
AP3529A (en) 2016-01-11
IL229533A0 (en) 2014-01-30
CU24146B1 (es) 2016-02-29
EA201490103A1 (ru) 2014-06-30
JP5955953B2 (ja) 2016-07-20
CN103764657B (zh) 2016-05-25
AU2012280508A1 (en) 2013-12-12
MA35601B1 (fr) 2014-11-01
UY34167A (es) 2013-01-31
NZ619453A (en) 2016-01-29
BR112014000049A2 (pt) 2017-02-07
US9040691B2 (en) 2015-05-26
EP2726482B1 (en) 2016-07-20
JP2014525902A (ja) 2014-10-02
SG195100A1 (en) 2013-12-30
WO2013004551A1 (en) 2013-01-10
US20140256718A1 (en) 2014-09-11
CU20130170A7 (es) 2014-04-24
PH12013502695A1 (en) 2019-06-14
MX2013014315A (es) 2014-01-31
EA023775B1 (ru) 2016-07-29
DOP2013000300A (es) 2014-02-28
AR087017A1 (es) 2014-02-05
ECSP13013120A (es) 2014-02-28
ES2598027T3 (es) 2017-01-24
CO6870031A2 (es) 2014-02-20
CN103764657A (zh) 2014-04-30
KR20140036269A (ko) 2014-03-25

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