BR112017020131A2 - derivados de 7-(morfolin-4-il)pirazol[1,5-a]pirimidina que são úteis para o tratamento de doenças imunológicas ou inflamatórias ou câncer - Google Patents

derivados de 7-(morfolin-4-il)pirazol[1,5-a]pirimidina que são úteis para o tratamento de doenças imunológicas ou inflamatórias ou câncer

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Publication number
BR112017020131A2
BR112017020131A2 BR112017020131-3A BR112017020131A BR112017020131A2 BR 112017020131 A2 BR112017020131 A2 BR 112017020131A2 BR 112017020131 A BR112017020131 A BR 112017020131A BR 112017020131 A2 BR112017020131 A2 BR 112017020131A2
Authority
BR
Brazil
Prior art keywords
cancer
inflammatory diseases
morpholin
pyrazol
useful
Prior art date
Application number
BR112017020131-3A
Other languages
English (en)
Other versions
BR112017020131B1 (pt
Inventor
Dymek Barbara
Zagozda Marcin
Wieczorek Maciej
DUBIEL Krzysztof
Stanczak Aleksandra
Zdzalik Daria
Gunerka Pawel
Sekular Mariola
Dziachan Maciej
Original Assignee
Celon Pharma S.A.
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 Celon Pharma S.A. filed Critical Celon Pharma S.A.
Publication of BR112017020131A2 publication Critical patent/BR112017020131A2/pt
Publication of BR112017020131B1 publication Critical patent/BR112017020131B1/pt

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Classifications

    • 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
    • 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
    • A61K31/535Heterocyclic 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
    • 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]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

trata-se de um composto de fórmula geral (i) em que y representa -ch2- ou >c=0; r1 é selecionado a partir do grupo que consiste em a1, a2 e a3; r2 representa uma porção química de dioxotiomorfolino b1, porção química de piperazinila b2, porção química de azetidinila b3 ou porção química de piperidinila b4; r3 é selecionado a partir do grupo que consiste em h, halogênio e alquila c1 -c4; r4 é selecionado a partir do grupo que consiste em alquila c1 -c4, ciclolquila-c3-c4, alquila-c1 -c4 substituída por alcóxi-c1 -c4 e chf2 e seus sais farmaceuticamente aceitáveis. as composições farmacêuticas que compreendem os ditos compostos e seu uso no tratamento de doenças de sistema imunológico, doenças inflamatórias e câncer.
BR112017020131-3A 2015-04-02 2016-03-30 Composto, seu uso e composição farmacêutica BR112017020131B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PL411864A PL236355B1 (pl) 2015-04-02 2015-04-02 Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3
PL411864 2015-04-02
PCT/IB2016/051792 WO2016157091A1 (en) 2015-04-02 2016-03-30 7-(morpholin-4-yl)pyrazole[1,5-a]pyrimidine derivatives which are useful for the treatment of immune or inflammatory diseases or cancer

Publications (2)

Publication Number Publication Date
BR112017020131A2 true BR112017020131A2 (pt) 2018-05-29
BR112017020131B1 BR112017020131B1 (pt) 2023-02-28

Family

ID=55650626

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017020131-3A BR112017020131B1 (pt) 2015-04-02 2016-03-30 Composto, seu uso e composição farmacêutica

Country Status (18)

Country Link
US (1) US10138247B2 (pt)
EP (1) EP3277687B1 (pt)
JP (1) JP6665201B2 (pt)
KR (1) KR102559190B1 (pt)
CN (1) CN107743489B (pt)
AU (1) AU2016241568B2 (pt)
BR (1) BR112017020131B1 (pt)
CA (1) CA2978828A1 (pt)
DK (1) DK3277687T3 (pt)
EA (1) EA032826B1 (pt)
ES (1) ES2765642T3 (pt)
HR (1) HRP20192195T1 (pt)
HU (1) HUE047822T2 (pt)
MX (1) MX2017011423A (pt)
PL (2) PL236355B1 (pt)
PT (1) PT3277687T (pt)
SI (1) SI3277687T1 (pt)
WO (1) WO2016157091A1 (pt)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2021347913A1 (en) * 2020-09-28 2023-05-18 1ST Biotherapeutics, Inc. Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same
CN114957261B (zh) * 2022-05-17 2023-06-23 重庆文理学院 一种具有抗头颈癌作用的化合物及其制备方法和应用

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL191271B1 (pl) * 1996-02-07 2006-04-28 Neurocrine Biosciences Inc Pochodna pirazolopirymidyny i jej zastosowanie oraz kompozycja farmaceutyczna
WO2005062882A2 (en) 2003-12-23 2005-07-14 Activbiotics, Inc Rifamycin analogs and uses thereof
AU2006212457B2 (en) * 2005-02-11 2011-04-14 F. Hoffmann-La Roche Ag Pyrazolo-pyrimidine derivatives as mGLuR2 antagonists
MY146388A (en) * 2006-09-20 2012-08-15 Lilly Co Eli Thiazole pyrazolopyrimidines as crfi receptor antagonists
CN101835779B (zh) * 2007-10-26 2014-01-29 霍夫曼-拉罗奇有限公司 作为pi3激酶抑制剂的嘌呤衍生物
AU2009218515A1 (en) 2008-02-26 2009-09-03 Novartis Ag Heterocyclic compounds as inhibitors of CXCR2
KR20110042153A (ko) * 2008-05-30 2011-04-25 제넨테크, 인크. 퓨린 pi3k 억제 화합물 및 사용 방법
US20110257170A1 (en) * 2008-10-03 2011-10-20 Merck Serono Sa 4-morpholino-pyrido[3,2-d]pyrimidines
WO2010074284A1 (ja) * 2008-12-26 2010-07-01 味の素株式会社 ピラゾロピリミジン化合物
SG175195A1 (en) * 2009-04-16 2011-11-28 Ct Nac Investigaciones Oncologicas Cnio Imidazopyrazines for use as kinase inhibitors
EP2451811A1 (en) 2009-05-27 2012-05-16 F. Hoffmann-La Roche AG Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
CA2761445A1 (en) * 2009-05-27 2010-12-02 Genentech, Inc. Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
GB0912745D0 (en) 2009-07-22 2009-08-26 Wolfson Microelectronics Plc Improvements relating to DC-DC converters
CN102762565A (zh) 2010-02-22 2012-10-31 弗·哈夫曼-拉罗切有限公司 吡啶并[3,2-d]嘧啶PI3δ抑制剂化合物及使用方法
CA2789475C (en) 2010-03-04 2018-05-29 Merck Sharp & Dohme Corp. Inhibitors of catechol o-methyl transferase and their use in the treatment of psychotic disorders
US9096605B2 (en) * 2011-08-24 2015-08-04 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as PI3 kinase inhibitors

Also Published As

Publication number Publication date
EP3277687A1 (en) 2018-02-07
EA201792087A1 (ru) 2018-03-30
JP6665201B2 (ja) 2020-03-13
PL236355B1 (pl) 2021-01-11
US20180111939A1 (en) 2018-04-26
PL3277687T3 (pl) 2020-09-21
US10138247B2 (en) 2018-11-27
AU2016241568B2 (en) 2019-09-26
EP3277687B1 (en) 2019-10-30
JP2018510192A (ja) 2018-04-12
KR102559190B1 (ko) 2023-07-25
WO2016157091A1 (en) 2016-10-06
DK3277687T3 (da) 2019-12-16
CN107743489A (zh) 2018-02-27
PT3277687T (pt) 2020-01-10
HUE047822T2 (hu) 2020-05-28
BR112017020131B1 (pt) 2023-02-28
PL411864A1 (pl) 2016-10-10
EA032826B1 (ru) 2019-07-31
MX2017011423A (es) 2018-05-17
SI3277687T1 (sl) 2020-02-28
HRP20192195T1 (hr) 2020-03-06
AU2016241568A1 (en) 2017-10-19
KR20170132275A (ko) 2017-12-01
ES2765642T3 (es) 2020-06-10
CA2978828A1 (en) 2016-10-06
CN107743489B (zh) 2021-05-04

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