KR102120505B1 - 통증 치료용 아자인다졸 또는 디아자인다졸 타입의 유도체 - Google Patents

통증 치료용 아자인다졸 또는 디아자인다졸 타입의 유도체 Download PDF

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KR102120505B1
KR102120505B1 KR1020157004735A KR20157004735A KR102120505B1 KR 102120505 B1 KR102120505 B1 KR 102120505B1 KR 1020157004735 A KR1020157004735 A KR 1020157004735A KR 20157004735 A KR20157004735 A KR 20157004735A KR 102120505 B1 KR102120505 B1 KR 102120505B1
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charom
arom
pain
mmol
reaction
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KR20150038295A (ko
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삐에르 쏘꼴로프
프레데리끄 까꾸
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피에르 파브르 메디카먼트
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020157004735A 2012-07-27 2013-07-29 통증 치료용 아자인다졸 또는 디아자인다졸 타입의 유도체 Expired - Fee Related KR102120505B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12305922.2A EP2689778A1 (en) 2012-07-27 2012-07-27 Derivatives of azaindoles or diazaindoles for treating pain
EP12305922.2 2012-07-27
PCT/EP2013/065907 WO2014016433A1 (en) 2012-07-27 2013-07-29 Derivatives of azaindazole or diazaindazole type for treating pain

Publications (2)

Publication Number Publication Date
KR20150038295A KR20150038295A (ko) 2015-04-08
KR102120505B1 true KR102120505B1 (ko) 2020-06-08

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KR1020157004735A Expired - Fee Related KR102120505B1 (ko) 2012-07-27 2013-07-29 통증 치료용 아자인다졸 또는 디아자인다졸 타입의 유도체

Country Status (28)

Country Link
US (1) US9381195B2 (enExample)
EP (2) EP2689778A1 (enExample)
JP (2) JP6456823B2 (enExample)
KR (1) KR102120505B1 (enExample)
CN (1) CN104684554B (enExample)
AU (1) AU2013294920B2 (enExample)
BR (1) BR112015001502B1 (enExample)
CA (1) CA2879595C (enExample)
CY (1) CY1118478T1 (enExample)
DK (1) DK2877177T3 (enExample)
ES (1) ES2612349T3 (enExample)
HR (1) HRP20170104T1 (enExample)
HU (1) HUE032919T2 (enExample)
IL (1) IL236917A (enExample)
LT (1) LT2877177T (enExample)
MA (1) MA37866B1 (enExample)
MX (1) MX363605B (enExample)
MY (1) MY183398A (enExample)
NZ (1) NZ705253A (enExample)
PL (1) PL2877177T3 (enExample)
PT (1) PT2877177T (enExample)
RS (1) RS55646B1 (enExample)
RU (1) RU2640046C2 (enExample)
SI (1) SI2877177T1 (enExample)
TN (1) TN2015000034A1 (enExample)
UA (1) UA116107C2 (enExample)
WO (1) WO2014016433A1 (enExample)
ZA (1) ZA201501209B (enExample)

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PT3106463T (pt) 2008-10-22 2018-05-18 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como inibidores de cinase trk
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
RU2735545C2 (ru) 2010-05-20 2020-11-03 Эррэй Биофарма Инк. Макроциклические соединения в качестве ингибиторов киназы trk
EP2689778A1 (en) * 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain
WO2015143652A1 (en) * 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
US9573948B2 (en) 2014-10-06 2017-02-21 Flatley Discovery Lab Triazolopyridine compounds and methods for the treatment of cystic fibrosis
EP3218380B1 (en) 2014-11-16 2021-03-17 Array Biopharma, Inc. Preparation of a crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
WO2016096709A1 (en) 2014-12-16 2016-06-23 Eudendron S.R.L. Heterocyclic derivatives modulating activity of certain protein kinases
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
IL304018A (en) 2016-04-04 2023-08-01 Loxo Oncology Inc Liquid formulations of (S)-N-(5-((R)-2-(5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-A]pyrimidin-3-yl)-3 -hydroxypyrrolidine-1-carboxamide
ES2952056T3 (es) 2016-05-18 2023-10-26 Loxo Oncology Inc Preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
WO2018049271A1 (en) * 2016-09-09 2018-03-15 Flx Bio, Inc. Chemokine receptor modulators and uses thereof
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018079759A1 (ja) * 2016-10-31 2018-05-03 塩野義製薬株式会社 ＴｒｋＡ阻害活性を有する縮合複素環および縮合炭素環誘導体
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
WO2019212256A1 (ko) * 2018-05-02 2019-11-07 제이더블유중외제약 주식회사 신규한 헤테로 사이클 유도체
KR102129114B1 (ko) * 2018-07-26 2020-07-02 주식회사 온코파마텍 TrkA 저해 활성을 갖는 화합물 및 이를 유효성분으로 함유하는 통증의 예방 또는 치료용 약학적 조성물
EP3725777A1 (en) * 2019-04-17 2020-10-21 Rottapharm Biotech S.r.l. Benzo- and pyrido-pyrazoles as protein kinase inhibitors
CN110105356B (zh) * 2019-05-31 2022-04-01 四川国康药业有限公司 一种氮杂吲哚类化合物及其制备方法和用途
CN121358733A (zh) * 2023-05-24 2026-01-16 长春金赛药业有限责任公司 Fgfr2/3选择性抑制剂、药物组合物及其应用

Citations (3)

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Publication number Priority date Publication date Assignee Title
WO1998041525A1 (en) 1997-03-19 1998-09-24 Basf Aktiengesellschaft Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors
WO2007023110A2 (en) 2005-08-25 2007-03-01 F. Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
KR101923751B1 (ko) * 2011-01-27 2018-11-29 피에르 파브르 메디카먼트 의약으로서의 아자인다졸 또는 디아자인다졸 유형의 유도체

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HUP0301183A3 (en) 2000-06-22 2006-02-28 Pfizer Process for the preparation of pyrazolopyrimidinones
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WO2008010964A1 (en) 2006-07-17 2008-01-24 Merck & Co., Inc. 1-hydroxy naphthyridine compounds as anti-hiv agents
ES2509820T3 (es) 2006-12-20 2014-10-20 Nerviano Medical Sciences S.R.L. Derivados de indazol como inhibidores de la cinasa para el tratamiento del cáncer
US20080194557A1 (en) * 2007-01-18 2008-08-14 Joseph Barbosa Methods and compositions for the treatment of pain, inflammation and cancer
WO2008112695A2 (en) * 2007-03-12 2008-09-18 Irm Llc Pyrazolo [3,4-d] pyrimidines and 1, 2, 5, 6-tetraaza- as- indacenes as protein kinase inhibitors for cancer treatment
EA018503B1 (ru) 2007-07-20 2013-08-30 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные производные индазола, активные как ингибиторы киназы
US8354399B2 (en) * 2008-12-18 2013-01-15 Nerviano Medical Sciences S.R.L. Substituted indazole derivatives active as kinase inhibitors
EP2689778A1 (en) * 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
WO1998041525A1 (en) 1997-03-19 1998-09-24 Basf Aktiengesellschaft Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors
WO2007023110A2 (en) 2005-08-25 2007-03-01 F. Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
KR101923751B1 (ko) * 2011-01-27 2018-11-29 피에르 파브르 메디카먼트 의약으로서의 아자인다졸 또는 디아자인다졸 유형의 유도체

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CN104684554A (zh) 2015-06-03
RS55646B1 (sr) 2017-06-30
US20150190394A1 (en) 2015-07-09
BR112015001502A2 (pt) 2017-07-04
CY1118478T1 (el) 2017-07-12
ZA201501209B (en) 2016-03-30
MX363605B (es) 2019-03-26
MY183398A (en) 2021-02-18
JP2015522650A (ja) 2015-08-06
CA2879595A1 (en) 2014-01-30
LT2877177T (lt) 2017-01-25
RU2015106434A (ru) 2016-09-20
IL236917A (en) 2016-11-30
TN2015000034A1 (en) 2016-06-29
JP2019031542A (ja) 2019-02-28
HUE032919T2 (hu) 2017-11-28
SI2877177T1 (sl) 2017-02-28
CN104684554B (zh) 2017-05-10
CA2879595C (en) 2020-07-28
NZ705253A (en) 2017-05-26
PT2877177T (pt) 2017-02-06
MA37866B1 (fr) 2016-12-30
AU2013294920B2 (en) 2017-08-24
UA116107C2 (uk) 2018-02-12
KR20150038295A (ko) 2015-04-08
HK1207302A1 (en) 2016-01-29
MA37866A1 (fr) 2016-05-31
EP2689778A1 (en) 2014-01-29
US9381195B2 (en) 2016-07-05
AU2013294920A1 (en) 2015-03-12
RU2640046C2 (ru) 2017-12-26
JP6456823B2 (ja) 2019-01-23
DK2877177T3 (en) 2017-02-06
BR112015001502B1 (pt) 2023-03-07
HRP20170104T1 (hr) 2017-03-24
EP2877177A1 (en) 2015-06-03
WO2014016433A1 (en) 2014-01-30
ES2612349T3 (es) 2017-05-16
MX2015001009A (es) 2015-06-04
JP6732855B2 (ja) 2020-07-29
PL2877177T3 (pl) 2017-04-28
EP2877177B1 (en) 2016-10-26

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