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

    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/53—Heterocyclic 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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 (24)

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)
SG (1) SG195100A1 (es)
UY (1) UY34167A (es)
WO (1) WO2013004551A1 (es)

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TWI510480B (zh) 2011-05-10 2015-12-01 Gilead Sciences Inc 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
TW201837023A (zh) 2011-07-01 2018-10-16 美商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
JP5985658B2 (ja) * 2012-01-31 2016-09-06 ナンジン アルゲン ファルマ カンパニー リミテッドＮａｎｊｉｎｇ Ａｌｌｇｅｎ Ｐｈａｒｍａ Ｃｏ． Ｌｔｄ． ブルトンチロシンキナーゼ阻害薬としての環状分子
WO2015157644A1 (en) * 2014-04-10 2015-10-15 Lankenau Institute For Medical Research Methods and compositions for the treatment of ocular diseases and disorders
EP3148993B1 (en) 2014-05-28 2019-02-27 Bayer CropScience Aktiengesellschaft Process for preparing thiazole derivatives
US10214537B2 (en) 2014-10-22 2019-02-26 Bristol-Myers Squibb Company Bicyclic heteroaryl amine compounds
EP3209665B1 (en) * 2014-10-22 2019-08-14 Bristol-Myers Squibb Company Substituted pyrrolotriazine amine compounds as pi3k inhibitors
TW201632520A (zh) 2014-11-25 2016-09-16 拜耳製藥股份有限公司 經取代之吡啶並苯並二氮呯酮衍生物及其用途
AU2016249537B2 (en) 2015-04-16 2020-01-30 Merck Patent Gmbh 3-(1H-benzimidazol-2-yl)-1H-pyridin-2-one derivatives
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
KR102558066B1 (ko) * 2016-03-28 2023-07-25 인사이트 코포레이션 Tam 억제제로서 피롤로트리아진 화합물
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
KR20200088308A (ko) 2017-09-27 2020-07-22 인사이트 코포레이션 Tam 억제제로서 유용한 피롤로트리아진 유도체의 염
MA53010A (fr) 2018-06-29 2021-05-05 Incyte Corp Formulations d'un inhibiteur de axl/mer

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ES2328269T3 (es) * 1999-05-21 2009-11-11 Bristol-Myers Squibb Company Pirrolotriazinas como inhibires de quinasas.
AU2003254847B2 (en) 2002-08-08 2009-06-04 Kissei Pharmaceutical Co., Ltd. Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
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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
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ES2545907T3 (es) 2005-12-29 2015-09-16 Abbvie Inc. Inhibidores de proteína quinasa
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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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
AR087017A1 (es) 2014-02-05
CN103764657B (zh) 2016-05-25
MX2013014315A (es) 2014-01-31
AP2014007378A0 (en) 2014-01-31
CN103764657A (zh) 2014-04-30
CO6870031A2 (es) 2014-02-20
US9040691B2 (en) 2015-05-26
AU2012280508A1 (en) 2013-12-12
ECSP13013120A (es) 2014-02-28
EA023775B1 (ru) 2016-07-29
UY34167A (es) 2013-01-31
CU20130170A7 (es) 2014-04-24
SG195100A1 (en) 2013-12-30
ES2598027T3 (es) 2017-01-24
DOP2013000300A (es) 2014-02-28
GT201300313A (es) 2014-11-13
NZ619453A (en) 2016-01-29
EA201490103A1 (ru) 2014-06-30
IL229533A0 (en) 2014-01-30
JP5955953B2 (ja) 2016-07-20
AP3529A (en) 2016-01-11
WO2013004551A1 (en) 2013-01-10
US20140256718A1 (en) 2014-09-11
EP2726482B1 (en) 2016-07-20
EP2726482A1 (en) 2014-05-07
JP2014525902A (ja) 2014-10-02
CU24146B1 (es) 2016-02-29
MA35601B1 (fr) 2014-11-01
KR20140036269A (ko) 2014-03-25
CA2840518A1 (en) 2013-01-10
BR112014000049A2 (pt) 2017-02-07

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