BR112014027117A2 - derivados de pirazol aminopirimidina como moduladores de lrrk2 para uso no tratamento de doença de parkinson - Google Patents

derivados de pirazol aminopirimidina como moduladores de lrrk2 para uso no tratamento de doença de parkinson

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Publication number
BR112014027117A2
BR112014027117A2 BR112014027117A BR112014027117A BR112014027117A2 BR 112014027117 A2 BR112014027117 A2 BR 112014027117A2 BR 112014027117 A BR112014027117 A BR 112014027117A BR 112014027117 A BR112014027117 A BR 112014027117A BR 112014027117 A2 BR112014027117 A2 BR 112014027117A2
Authority
BR
Brazil
Prior art keywords
parkinson
disease
treatment
aminopyrimidine
pyrazole derivatives
Prior art date
Application number
BR112014027117A
Other languages
English (en)
Other versions
BR112014027117A8 (pt
BR112014027117B1 (pt
Inventor
Estrada Anthony
K Chan Bryan
baker glenn Charles
Dotson Jennafer
P Lyssikatos Joseph
Heffron Timothy
Kevin Sweeney Zachary
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112014027117A2 publication Critical patent/BR112014027117A2/pt
Publication of BR112014027117A8 publication Critical patent/BR112014027117A8/pt
Publication of BR112014027117B1 publication Critical patent/BR112014027117B1/pt

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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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Landscapes

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

Abstract

resumo patente de invenção: "derivados de pirazol aminopirimidina como moduladores de lrrk2 para uso no tratamento de doença de parkinson". compostos de fórmula i: i ou sais farmaceuticamente aceitáveis dos mesmos, em que x, r1, r2, r3 e a são como definido aqui. são também descritos, métodos de preparação dos compostos e uso dos compostos para o tratamento de doenças associadas com receptor de lrrk2, tal como doença de parkinson.
BR112014027117-8A 2012-05-03 2013-04-30 Derivados de pirazol aminopirimidina como moduladores de lrrk2, seus usos, e composição BR112014027117B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261642022P 2012-05-03 2012-05-03
US61/642,022 2012-05-03
PCT/EP2013/058942 WO2013164323A1 (en) 2012-05-03 2013-04-30 Pyrazole aminopyrimidine derivatives as lrrk2 modulators for use in the treatment of parkinson's disease

Publications (3)

Publication Number Publication Date
BR112014027117A2 true BR112014027117A2 (pt) 2017-06-27
BR112014027117A8 BR112014027117A8 (pt) 2017-07-11
BR112014027117B1 BR112014027117B1 (pt) 2022-09-06

Family

ID=48190523

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112014027117-8A BR112014027117B1 (pt) 2012-05-03 2013-04-30 Derivados de pirazol aminopirimidina como moduladores de lrrk2, seus usos, e composição

Country Status (11)

Country Link
US (1) US9212186B2 (pt)
EP (1) EP2844658B1 (pt)
JP (1) JP6211061B2 (pt)
KR (1) KR102091895B1 (pt)
CN (2) CN104271578B (pt)
BR (1) BR112014027117B1 (pt)
CA (1) CA2871375C (pt)
HK (1) HK1200819A1 (pt)
MX (1) MX358172B (pt)
RU (1) RU2637948C2 (pt)
WO (1) WO2013164323A1 (pt)

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EP3736268A1 (en) 2013-12-20 2020-11-11 Signal Pharmaceuticals, LLC Process for the preparation of substituted diaminopyrimidyl compounds
AU2015210554A1 (en) 2014-01-29 2016-07-07 Glaxosmithkline Intellectual Property Development Limited Compounds
CR20160348A (es) 2014-01-29 2017-04-28 Glaxosmithline Intellectual Property Dev Ltd Compuestos
EP3327006B1 (en) * 2014-03-28 2020-05-20 Calitor Sciences, LLC Substituted heteroaryl compounds and methods of use
CN113563342A (zh) * 2015-02-13 2021-10-29 达纳－法伯癌症研究所公司 Lrrk2抑制剂及其制备和使用方法
WO2017087905A1 (en) * 2015-11-20 2017-05-26 Denali Therapeutics Inc. Compound, compositions, and methods
US11028080B2 (en) 2016-03-11 2021-06-08 Denali Therapeutics Inc. Substituted pyrimidines as LRKK2 inhibitors
TWI659955B (zh) * 2016-06-15 2019-05-21 大陸商蘇州亞寶藥物研發有限公司 取代的三環雜環化合物及其用途
CA3026844A1 (en) 2016-06-15 2017-12-21 Suzhou Yabao Pharmaceutical R&D Co., Ltd. Substituted tricyclic heterocyclic compounds and use thereof
PT3472153T (pt) 2016-06-16 2021-12-31 Denali Therapeutics Inc Pirimidin-2-ilamino-1h-pirazóis como inibidores de lrrk2 para uso no tratamento de distúrbios neurodegenerativos
MX2020005332A (es) 2017-11-21 2021-01-08 Denali Therapeutics Inc Polimorfos y formas solidas de un compuesto de pirimidinilamino-pirazol y metodos de produccion.
CA3086182A1 (en) 2017-12-20 2019-06-27 Denali Therapeutics Inc. Process for the preparation of pyrimidinyl-4-aminopyrazole compounds
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EP4329763A1 (en) * 2021-04-30 2024-03-06 Denali Therapeutics Inc. Methods for treating and monitoring parkinson's disease
US20240174647A1 (en) * 2022-09-30 2024-05-30 Neuron23, Inc. Kinase modulators and methods of use thereof
WO2024097394A1 (en) 2022-11-03 2024-05-10 Denali Therapeutics Inc. Solid and co-crystal forms of a pyrimidine triazole compound
WO2024112746A1 (en) 2022-11-22 2024-05-30 Denali Therapeutics Inc. Processes and intermediates for the preparation of a pyrimidine aminopyrazole compound

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RU2340611C2 (ru) * 2000-09-15 2008-12-10 Вертекс Фармасьютикалз Инкорпорейтед Производные пиразола, используемые в качестве ингибиторов протеинкиназы
WO2005026129A1 (en) * 2003-09-15 2005-03-24 Gpc Biotech Ag Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
WO2007035309A1 (en) * 2005-09-15 2007-03-29 Merck & Co., Inc. Tyrosine kinase inhibitors
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AP2009004958A0 (en) * 2007-02-07 2009-08-31 Pfizer 3-amino-pyrrolo [3,4-C] pyrazole - 5 (1H, 4H, 6H) carbaldehyde derivatives as PKC inhibitors
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Also Published As

Publication number Publication date
EP2844658B1 (en) 2019-03-20
JP2015519325A (ja) 2015-07-09
US20150051201A1 (en) 2015-02-19
WO2013164323A1 (en) 2013-11-07
RU2637948C2 (ru) 2017-12-08
BR112014027117A8 (pt) 2017-07-11
KR102091895B1 (ko) 2020-04-14
CN104271578A (zh) 2015-01-07
CA2871375C (en) 2020-10-27
RU2014147382A (ru) 2016-06-27
CA2871375A1 (en) 2013-11-07
HK1200819A1 (en) 2015-08-14
EP2844658A1 (en) 2015-03-11
US9212186B2 (en) 2015-12-15
JP6211061B2 (ja) 2017-10-11
CN104271578B (zh) 2016-09-14
MX358172B (es) 2018-08-08
CN106279202A (zh) 2017-01-04
BR112014027117B1 (pt) 2022-09-06
MX2014012804A (es) 2015-01-15
KR20150016535A (ko) 2015-02-12

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Legal Events

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B25A Requested transfer of rights approved

Owner name: GENENTECH, INC. (US)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

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