BR112014027117A8 - Derivados de pirazol aminopirimidina como moduladores de lrrk2, seus usos, e composição - Google Patents
Derivados de pirazol aminopirimidina como moduladores de lrrk2, seus usos, e composiçãoInfo
- Publication number
- BR112014027117A8 BR112014027117A8 BR112014027117A BR112014027117A BR112014027117A8 BR 112014027117 A8 BR112014027117 A8 BR 112014027117A8 BR 112014027117 A BR112014027117 A BR 112014027117A BR 112014027117 A BR112014027117 A BR 112014027117A BR 112014027117 A8 BR112014027117 A8 BR 112014027117A8
- Authority
- BR
- Brazil
- Prior art keywords
- composition
- aminopyrimidine derivatives
- lrrk2
- pyrazole
- compounds
- Prior art date
Links
Classifications
-
- 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
- A61K31/535—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
-
- 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
-
- 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
Abstract
DERIVADOS DE PIRAZOL AMINOPIRIMIDINA COMO MODULADORES DE LRRK2, SEUS USOS, E COMPOSIÇÃO. Compostos de fórmula 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.
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 BR112014027117A2 (pt) | 2017-06-27 |
BR112014027117A8 true 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) | CN106279202A (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) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6483707B2 (ja) | 2013-12-20 | 2019-03-13 | シグナル ファーマシューティカルズ,エルエルシー | 置換されたジアミノピリミジル化合物、それらの組成物、及びそれらによる治療方法 |
SG11201605342UA (en) | 2014-01-29 | 2016-08-30 | Glaxosmithkline Ip Dev Ltd | Compounds |
RU2016134751A (ru) | 2014-01-29 | 2018-03-02 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Соединения |
US9394281B2 (en) * | 2014-03-28 | 2016-07-19 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
EP3256475A4 (en) * | 2015-02-13 | 2019-02-13 | Dana-Farber Cancer Institute, Inc. | LRRK2 INHIBITORS AND METHOD FOR THE PRODUCTION AND USE THEREOF |
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 |
CN109071558B (zh) | 2016-06-15 | 2021-10-29 | 苏州亚宝药物研发有限公司 | 取代的三环杂环化合物及其用途 |
CA3025672A1 (en) | 2016-06-16 | 2017-12-21 | Denali Therapeutics Inc. | Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders |
UA126414C2 (uk) | 2017-11-21 | 2022-09-28 | Деналі Терапьютикс Інк. | Поліморфи та тверді форми піримідиніламінопіразолової сполуки та способи їх отримання |
JP7284172B2 (ja) | 2017-12-20 | 2023-05-30 | デナリ セラピューティクス インコーポレイテッド | ピリミジニル-4-アミノピラゾール化合物の調製方法 |
KR20230091871A (ko) | 2020-10-20 | 2023-06-23 | 에프. 호프만-라 로슈 아게 | Pd-1 축 결합 길항제 및 lrrk2 억제제의 병용 요법 |
CA3217230A1 (en) * | 2021-04-30 | 2022-11-03 | Denali Therapeutics Inc. | Methods for treating and monitoring parkinson's disease |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2340611C2 (ru) * | 2000-09-15 | 2008-12-10 | Вертекс Фармасьютикалз Инкорпорейтед | Производные пиразола, используемые в качестве ингибиторов протеинкиназы |
CA2422380C (en) * | 2000-09-15 | 2009-03-24 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
WO2005026129A1 (en) * | 2003-09-15 | 2005-03-24 | Gpc Biotech Ag | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
EP1934200A1 (en) * | 2005-09-15 | 2008-06-25 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
UA96618C2 (en) * | 2007-02-07 | 2011-11-25 | Пфайзер Инк. | 3-amino-pyrrolo[3,4-c] pyrazole- 5 (1h, 4h, 6h) carbaldehyde derivatives as pkc inhibitors |
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 |
PE20091236A1 (es) * | 2007-11-22 | 2009-09-16 | Astrazeneca Ab | Derivados de pirimidina como immunomoduladores de tlr7 |
JP2011513483A (ja) * | 2008-03-10 | 2011-04-28 | バーテックス ファーマシューティカルズ インコーポレイテッド | タンパク質キナーゼの阻害剤として有用なピリミジンおよびピリジン |
KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Egfr 억제제 및 질환 치료방법 |
SG182351A1 (en) * | 2010-01-13 | 2012-08-30 | Glaxosmithkline Llc | Compounds and methods |
JP6086326B2 (ja) * | 2010-05-24 | 2017-03-01 | ユニヴァーシティー オブ ロチェスター | 二環式ヘテロアリールキナーゼ阻害剤および使用方法 |
PT2576541T (pt) * | 2010-06-04 | 2016-07-08 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
KR101566091B1 (ko) * | 2010-11-10 | 2015-11-04 | 에프. 호프만-라 로슈 아게 | Lrrk2 조절제로서 피라졸 아미노피리미딘 유도체 |
WO2013079493A1 (en) * | 2011-11-29 | 2013-06-06 | F. Hoffmann-La Roche Ag | Aminopyrimidine derivatives as lrrk2 modulators |
CN103958498B (zh) * | 2011-11-29 | 2016-09-07 | 霍夫曼-拉罗奇有限公司 | 作为lrrk2调节剂的氨基嘧啶衍生物 |
PL2785711T3 (pl) * | 2011-11-29 | 2017-01-31 | F.Hoffmann-La Roche Ag | Pochodne 2-(fenylo lub piryd-3-ylo)aminopirymidyny jako modulatory kinazy lrrk2 do leczenia choroby parkinsona |
AR089182A1 (es) * | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
WO2013079496A1 (en) * | 2011-11-30 | 2013-06-06 | F. Hoffmann-La Roche Ag | Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (pet) imaging for lrrk2 |
KR102091894B1 (ko) * | 2012-05-03 | 2020-03-20 | 제넨테크, 인크. | Lrrk2 조절제로서의 피라졸 아미노피리미딘 유도체 |
MX2015015966A (es) * | 2013-05-30 | 2016-04-13 | Plexxikon Inc | Compuestos para la modulacion de cinasas e indicaciones para los mismos. |
-
2013
- 2013-04-30 CA CA2871375A patent/CA2871375C/en active Active
- 2013-04-30 WO PCT/EP2013/058942 patent/WO2013164323A1/en active Application Filing
- 2013-04-30 MX MX2014012804A patent/MX358172B/es active IP Right Grant
- 2013-04-30 CN CN201610674911.1A patent/CN106279202A/zh active Pending
- 2013-04-30 RU RU2014147382A patent/RU2637948C2/ru active
- 2013-04-30 BR BR112014027117-8A patent/BR112014027117B1/pt active IP Right Grant
- 2013-04-30 JP JP2015509411A patent/JP6211061B2/ja active Active
- 2013-04-30 EP EP13718860.3A patent/EP2844658B1/en active Active
- 2013-04-30 KR KR1020147033856A patent/KR102091895B1/ko active IP Right Grant
- 2013-04-30 CN CN201380023405.0A patent/CN104271578B/zh active Active
-
2014
- 2014-11-03 US US14/531,349 patent/US9212186B2/en active Active
-
2015
- 2015-02-05 HK HK15101248.1A patent/HK1200819A1/xx unknown
Also Published As
Publication number | Publication date |
---|---|
CA2871375A1 (en) | 2013-11-07 |
RU2637948C2 (ru) | 2017-12-08 |
EP2844658B1 (en) | 2019-03-20 |
BR112014027117B1 (pt) | 2022-09-06 |
CA2871375C (en) | 2020-10-27 |
RU2014147382A (ru) | 2016-06-27 |
WO2013164323A1 (en) | 2013-11-07 |
KR102091895B1 (ko) | 2020-04-14 |
EP2844658A1 (en) | 2015-03-11 |
US20150051201A1 (en) | 2015-02-19 |
HK1200819A1 (en) | 2015-08-14 |
JP2015519325A (ja) | 2015-07-09 |
JP6211061B2 (ja) | 2017-10-11 |
CN104271578A (zh) | 2015-01-07 |
BR112014027117A2 (pt) | 2017-06-27 |
KR20150016535A (ko) | 2015-02-12 |
CN106279202A (zh) | 2017-01-04 |
CN104271578B (zh) | 2016-09-14 |
US9212186B2 (en) | 2015-12-15 |
MX358172B (es) | 2018-08-08 |
MX2014012804A (es) | 2015-01-15 |
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Owner name: GENENTECH, INC. (US) |
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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] | ||
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B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 30/04/2013, OBSERVADAS AS CONDICOES LEGAIS |