ECSP13012611A - Derivados de pirazol-aminopirimidina como moduladores de la lrrk2 - Google Patents

Derivados de pirazol-aminopirimidina como moduladores de la lrrk2

Info

Publication number
ECSP13012611A
ECSP13012611A ECSP13012611A ECSP13012611A EC SP13012611 A ECSP13012611 A EC SP13012611A EC SP13012611 A ECSP13012611 A EC SP13012611A EC SP13012611 A ECSP13012611 A EC SP13012611A
Authority
EC
Ecuador
Prior art keywords
lrrk2
aminopirimidine
pirazol
modulators
derivatives
Prior art date
Application number
Other languages
English (en)
Inventor
Mark Stuart Chambers
Zachary Kevin Sweeney
Anthony Estrada
Daniel Jon Burdick
Bryan K Chan
Huifen Chen
Charles Baker-Glenn
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 ECSP13012611A publication Critical patent/ECSP13012611A/es

Links

Classifications

    • 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
    • C07D403/14—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 three or more hetero 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
    • A61K31/495—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
    • 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
    • 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
    • C07D401/14—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 three or more hetero 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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

Landscapes

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

Abstract

Compuestos de la fórmula I:o sales farmacéuticamente aceptables de los mismos,en los que X, R1, R2, R3, R4 y R5 tienen los significados aquí definidos. Se describen también métodos para la obtención de los compuestos y de utilización de los compuestos para el tratamiento de enfermedades asociadas con el receptor de la LRRK2, por ejemplo la enfermedad de Parkinson.
ECSP13012611 2010-11-10 2013-05-08 Derivados de pirazol-aminopirimidina como moduladores de la lrrk2 ECSP13012611A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US41227310P 2010-11-10 2010-11-10
US201161546613P 2011-10-13 2011-10-13

Publications (1)

Publication Number Publication Date
ECSP13012611A true ECSP13012611A (es) 2013-07-31

Family

ID=44983512

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP13012611 ECSP13012611A (es) 2010-11-10 2013-05-08 Derivados de pirazol-aminopirimidina como moduladores de la lrrk2

Country Status (28)

Country Link
US (1) US8815882B2 (es)
EP (3) EP3124483B1 (es)
JP (3) JP5986094B2 (es)
KR (1) KR101566091B1 (es)
CN (1) CN103313978B (es)
AR (1) AR083813A1 (es)
AU (1) AU2011328139A1 (es)
BR (1) BR112013011600B1 (es)
CA (2) CA2812669C (es)
CY (1) CY1120073T1 (es)
DK (2) DK3124483T3 (es)
EC (1) ECSP13012611A (es)
ES (2) ES2653967T3 (es)
HR (2) HRP20172006T1 (es)
HU (2) HUE046617T2 (es)
IL (1) IL225234A0 (es)
LT (2) LT2638031T (es)
MA (1) MA34644B1 (es)
MX (1) MX2013005199A (es)
NO (1) NO2638031T3 (es)
PH (1) PH12013500880A1 (es)
PL (2) PL3124483T3 (es)
PT (2) PT3124483T (es)
RS (2) RS56583B1 (es)
SG (1) SG189043A1 (es)
SI (2) SI3124483T1 (es)
TW (1) TW201302733A (es)
WO (1) WO2012062783A1 (es)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9884828B2 (en) 2011-05-23 2018-02-06 Imago Pharmaceuticals, Inc. Substituted cinnolines as inhibitors of LRRK2 kinase activity
AR089182A1 (es) 2011-11-29 2014-08-06 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
US20140228384A1 (en) * 2011-11-29 2014-08-14 Genentech, Inc. Assays and biomarkers for lrrk2
MX349556B (es) 2011-11-29 2017-08-03 Genentech Inc Derivados de aminopirimidina como moduladores de proteina cinasa 2 rica en unidades repetitivas de leucina (lrrk2).
CA2850594C (en) * 2011-11-29 2020-03-10 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as lrrk2 modulators
US8791130B2 (en) * 2011-11-29 2014-07-29 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 modulators
EP2785381B1 (en) * 2011-11-30 2016-05-18 F.Hoffmann-La Roche Ag Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (pet) imaging for lrrk2
EP2844658B1 (en) * 2012-05-03 2019-03-20 Genentech, Inc. Pyrazole aminopyrimidine derivatives as lrrk2 modulators for use in the treatment of parkinson's disease
CN104271569B (zh) * 2012-05-03 2016-08-24 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂的吡唑氨基嘧啶衍生物
CN105732639A (zh) 2012-06-29 2016-07-06 辉瑞大药厂 作为LRRK2抑制剂的4-(取代的氨基)-7H-吡咯并〔2,3-d〕嘧啶类
WO2014060381A1 (de) 2012-10-18 2014-04-24 Bayer Cropscience Ag Heterocyclische verbindungen als schädlingsbekämpfungsmittel
WO2017156493A1 (en) 2016-03-11 2017-09-14 Denali Therapeutics Inc. Compounds, compositions, and methods
WO2014134772A1 (en) * 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
JP6527520B2 (ja) 2013-12-17 2019-06-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ピルビン酸脱水素酵素キナーゼの阻害剤としてのｎ１−（３，３，３−トリフルオロ−２−ヒドロキソ−２−メチルプロピオニル）−ピペリジン誘導体
EP3083618B1 (en) 2013-12-17 2018-02-21 Pfizer Inc Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors
RU2016129380A (ru) 2013-12-20 2018-01-25 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Замещенные диаминопиримидильные соединения, их композиции и способы лечения с их участием
ES2717757T3 (es) 2014-01-29 2019-06-25 Glaxosmithkline Ip Dev Ltd Compuestos
US10087186B2 (en) * 2014-01-29 2018-10-02 Glaxosmithkline Intellectual Property Development Limited Compounds as LRRK2 kinase inhibitors
WO2015148868A1 (en) * 2014-03-28 2015-10-01 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
AU2015201630A1 (en) * 2014-03-31 2015-10-15 Commonwealth Scientific And Industrial Research Organisation Diamine compounds for phosphorescent diazaborole metal complexes and electroluminescent devices
US9656970B2 (en) 2014-05-08 2017-05-23 Tosoh F-Tech, Inc. 5-(trifluoromethyl)pyrimidine derivatives and method for producing same
WO2015176010A1 (en) 2014-05-15 2015-11-19 The United States Of America, As Represented By The Secretary, Departmentof Health & Human Services Treatment or prevention of an intestinal disease or disorder
JP6262079B2 (ja) * 2014-06-02 2018-01-17 東ソー・ファインケム株式会社 ４−（２，２，２−トリフルオロエトキシ）−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法
JP6431294B2 (ja) * 2014-06-16 2018-11-28 東ソー・ファインケム株式会社 ５−（トリフルオロメチル）ピリミジン誘導体及びその製造法
US10059689B2 (en) 2014-10-14 2018-08-28 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN108137586B (zh) 2015-09-14 2021-04-13 辉瑞大药厂 作为LRRK2抑制剂的新颖咪唑并[4,5-c]喹啉和咪唑并[4,5-c][1,5]萘啶衍生物
US11214565B2 (en) 2015-11-20 2022-01-04 Denali Therapeutics Inc. Compound, compositions, and methods
ES2797301T3 (es) 2016-03-29 2020-12-01 Merck Patent Gmbh Derivados de piperidinil-propanona
EP3448850B1 (en) 2016-04-28 2020-11-04 Merck Patent GmbH Piperidinyl derivatives
SI3472153T1 (sl) * 2016-06-16 2022-01-31 Denali Therapeutics Inc. Pirimidin-2-ilamino-1H-pirazoli kot zaviralci LRRK2 za uporabo pri zdravljenju nevrodegenerativnih motenj
CN106588884B (zh) * 2016-11-10 2019-04-09 浙江大学 2-多取代芳环-嘧啶类衍生物及制备和医药用途
CN106588885B (zh) * 2016-11-10 2019-03-19 浙江大学 2-取代芳环-嘧啶类衍生物及制备和应用
KR101923852B1 (ko) 2017-02-24 2018-11-29 재단법인 대구경북첨단의료산업진흥재단 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물
GB201705263D0 (en) * 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
WO2018217946A1 (en) * 2017-05-24 2018-11-29 Denali Therapeutics Inc. Compounds, compositions and methods
TWI769272B (zh) * 2017-06-30 2022-07-01 美商安進公司 奧美卡替莫卡必爾的合成
TW201920197A (zh) * 2017-07-14 2019-06-01 英商葛蘭素史克智慧財產發展有限公司 化合物
US10683297B2 (en) 2017-11-19 2020-06-16 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
PE20210157A1 (es) * 2017-11-21 2021-01-26 Denali Therapeutics Inc Polimorfos y formas solidas de un compuesto de pirimidinilamino-pirazol y metodos de produccion
US11834438B2 (en) * 2017-12-20 2023-12-05 Denali Therapeutics Inc. Process for the preparation of pyrimidinyl-4-aminopyrazole compounds
JP7364841B2 (ja) * 2018-02-14 2023-10-19 智彦 大和田 酸ハロゲン化物による化合物の製造方法
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
AR118641A1 (es) * 2019-04-11 2021-10-20 Denali Therapeutics Inc Compuestos, composiciones y métodos
AU2020274011B2 (en) 2019-05-10 2024-02-15 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
BR112021024194A2 (pt) * 2019-05-31 2022-01-11 Denali Therapeutics Inc Formulação de liberação modificada de um composto de pirimidinilamino-pirazol e métodos de tratamento
CN110627810B (zh) * 2019-06-05 2024-05-10 中国医学科学院药用植物研究所 一种三氟甲基吡唑衍生物的制备方法
CN119241444A (zh) 2019-06-17 2025-01-03 德西费拉制药有限责任公司 氨基嘧啶酰胺自噬抑制剂及其使用方法
EP3997081A1 (en) * 2019-07-11 2022-05-18 Escape Bio, Inc. Indazoles and azaindazoles as lrrk2 inhibitors
WO2021178485A1 (en) * 2020-03-06 2021-09-10 National Health Research Institutes Pyrimidine compounds and their pharmaceutical uses
KR102342803B1 (ko) 2020-03-23 2021-12-24 환인제약 주식회사 신규한 피리미딘 유도체 및 이를 포함하는 신경퇴행성 질환 및 암의 예방 또는 치료용 조성물
JP7671775B2 (ja) 2020-03-23 2025-05-02 ファニン ファーマシューティカル カンパニー リミテッド 新規なピリミジン誘導体及びこれを含む神経退行性疾患及び癌の予防又は治療用組成物
WO2022084210A1 (en) 2020-10-20 2022-04-28 F. Hoffmann-La Roche Ag Combination therapy of pd-1 axis binding antagonists and lrrk2 inhitibors
KR20230097093A (ko) 2020-10-29 2023-06-30 머크 샤프 앤드 돔 엘엘씨 Lrrk2 억제제로서의 n-연결된 이소퀴놀린 아미드, 제약 조성물 및 그의 용도
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Ａｌｋ﹘５抑制劑和彼之用途
WO2022197577A1 (en) * 2021-03-17 2022-09-22 Merck Sharp & Dohme Llc Heteroaroyl amides as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof
WO2022204299A1 (en) * 2021-03-23 2022-09-29 Halia Therapeutics, Inc. Pyrimidine derivatives useful as lrrk2 kinase inhibitors
US20240197729A1 (en) * 2021-03-26 2024-06-20 Sumitomo Pharma Oncology, Inc. ALK-5 Inhibitors and Uses Thereof
CN117355304A (zh) * 2021-03-26 2024-01-05 住友制药肿瘤公司 Alk-5抑制剂及其用途
WO2023076404A1 (en) 2021-10-27 2023-05-04 Aria Pharmaceuticals, Inc. Methods for treating systemic lupus erythematosus
WO2023174946A1 (en) 2022-03-15 2023-09-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Early and non-invasive method for assessing a subject's risk of having parkinson's disease
US20250313575A1 (en) * 2022-05-20 2025-10-09 Merck Sharp & Dohme Llc Macrocycles as lrrk2 inhibitors, pharmaceutical compositions, and uses 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
CN115819405A (zh) * 2022-12-20 2023-03-21 沪渝人工智能研究院 嘧啶氨基吡唑衍生物及其作为富亮氨酸重复激酶2抑制剂的应用
CN118546132A (zh) * 2023-02-27 2024-08-27 科辉智药(深圳)新药研究中心有限公司 亚砜酰亚胺化合物及其作为lrrk2蛋白激酶抑制剂的应用
CN119968373A (zh) * 2023-09-07 2025-05-09 上海翊石医药科技有限公司 一种芳杂环类化合物及其制备方法
WO2025235687A1 (en) * 2024-05-08 2025-11-13 Brenig Therapeutics, Inc. Lrrk2 inhibitors

Family Cites Families (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995010506A1 (en) 1993-10-12 1995-04-20 The Du Pont Merck Pharmaceutical Company 1n-alkyl-n-arylpyrimidinamines and derivatives thereof
PL313973A1 (en) 1993-10-12 1996-08-05 Du Pont Merck Pharma 1 n-alkyl-n-arylopyrimidin amines and their derivatives
BRPI9909191B8 (pt) 1998-03-27 2021-07-06 Janssen Pharmaceutica Nv derivados de pirimidina inibidores do hiv, seu uso e composição farmacêutica que os compreende
US6458823B1 (en) 1998-06-08 2002-10-01 Wyeth Diaminopyrazoles
US6172222B1 (en) 1998-06-08 2001-01-09 American Home Products Corporation Diaminopyrazoles
SK287269B6 (sk) 1998-11-10 2010-05-07 Janssen Pharmaceutica N. V. Derivát pyrimidínu, jeho použitie, spôsob jeho prípravy a farmaceutická kompozícia, kombinácia a produkt s jeho obsahom
JP2003531103A (ja) 1999-08-12 2003-10-21 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 ｃ−ＪＵＮＮ−末端キナーゼ（ＪＮＫ）および他のタンパク質キナーゼの阻害剤
JP4919566B2 (ja) 1999-09-24 2012-04-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 抗ウイルス組成物
US6906067B2 (en) 1999-12-28 2005-06-14 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-α expression
JP5230050B2 (ja) 2000-05-08 2013-07-10 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｈｉｖ複製阻害剤
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
GB0021726D0 (en) 2000-09-05 2000-10-18 Astrazeneca Ab Chemical compounds
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
DK1318997T3 (da) 2000-09-15 2006-09-25 Vertex Pharma Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE407132T1 (de) 2000-12-05 2008-09-15 Vertex Pharma Inhibitoren von c-jun n-terminalen kinasen (jnk) und anderen proteinkinasen
US7122544B2 (en) 2000-12-06 2006-10-17 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
ATE430742T1 (de) 2000-12-21 2009-05-15 Smithkline Beecham Corp Pyrimidinamine als angiogenesemodulatoren
JP4316893B2 (ja) 2001-05-16 2009-08-19 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 Ｓｒｃおよび他のプロテインキナーゼのインヒビター
MEP13408A (en) 2001-05-29 2010-06-10 Bayer Schering Pharma Ag Cdk inhibiting pyrimidines, production thereof and their use as medicaments
GB0113041D0 (en) 2001-05-30 2001-07-18 Astrazeneca Ab Chemical compounds
HUP0402352A2 (hu) 2001-06-19 2005-02-28 Bristol-Myers Squibb Co. Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények
EP1408978A4 (en) 2001-06-21 2005-07-13 Ariad Pharma Inc NOVEL PHENYLAMINO-PYRIMIDINES AND THEIR USE
HUP0401711A3 (en) 2001-06-26 2009-07-28 Bristol Myers Squibb Co N-heterocyclic inhibitors of tnf-alpha and pharmaceutical compositions containing them
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
WO2003040141A1 (en) 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
EP1453516A2 (de) 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren
EP1438053B1 (de) 2001-10-17 2008-09-10 Boehringer Ingelheim Pharma GmbH & Co.KG Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
AU2002367172A1 (en) 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation 2,4-diamino-pyrimidine derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
GB0205688D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
US7288547B2 (en) 2002-03-11 2007-10-30 Schering Ag CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
EP1483260A1 (de) * 2002-03-11 2004-12-08 Schering Aktiengesellschaft Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel
AR039540A1 (es) 2002-05-13 2005-02-23 Tibotec Pharm Ltd Compuestos microbicidas con contenido de pirimidina o triazina
GB0211019D0 (en) 2002-05-14 2002-06-26 Syngenta Ltd Novel compounds
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
EA200500721A1 (ru) 2002-11-28 2005-12-29 Шеринг Акциенгезельшафт Пиримидины, ингибирующие chk, pdk и акт, их получение и применение в качестве лекарственных средств
DE602004022633D1 (de) 2003-01-30 2009-10-01 Boehringer Ingelheim Pharma 2,4-diaminopyrimidinderivate, die sich als inhibitoren von pkc-theta eignen
KR20060009917A (ko) 2003-05-21 2006-02-01 바이엘 크롭사이언스 아게 요오도피라졸릴 카복스아닐리드
JP2007523875A (ja) 2003-07-15 2007-08-23 ニューロジェン・コーポレーション バニロイド受容体リガンドとしての置換ピリミジン−４−イルアミン類縁体
AU2004261482A1 (en) 2003-07-30 2005-02-10 Cyclacel Limited Pyridinylamino-pyrimidine derivatives as protein kinase inhibitors
JP4886511B2 (ja) * 2003-07-30 2012-02-29 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物による自己免疫疾患の治療または予防方法
JP4741491B2 (ja) 2003-08-07 2011-08-03 ライジェル ファーマシューティカルズ， インコーポレイテッド 抗増殖剤としての２，４−ピリミジンジアミン化合物および使用
DE10349423A1 (de) 2003-10-16 2005-06-16 Schering Ag Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
GB0402653D0 (en) 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
BRPI0510963A (pt) 2004-05-14 2007-11-20 Pfizer Prod Inc derivados pirimidina para o tratamento do crescimento anormal de células
JP4812763B2 (ja) 2004-05-18 2011-11-09 ライジェル ファーマシューティカルズ， インコーポレイテッド シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
CA2571937A1 (en) 2004-07-08 2006-02-09 Boehringer Ingelheim Pharmaceuticals, Inc. Pyrimidine derivatives useful as inhibitors of pkc-theta
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
WO2006028833A1 (en) 2004-09-01 2006-03-16 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamine compounds
WO2006053109A1 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Heteroaryl compounds
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
US20090099160A1 (en) 2004-12-17 2009-04-16 David Andrews 4-(4-(Imidazol-4-Yl) Pyrimidin-2-Ylamino) Benzamides as CDK Inhibitors
AU2005322855B2 (en) 2004-12-30 2012-09-20 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
DE102005008310A1 (de) 2005-02-17 2006-08-24 Schering Ag Verwendung von CDKII Inhibitoren zur Fertilitätskontrolle
EP1705177A1 (en) 2005-03-23 2006-09-27 Schering Aktiengesellschaft N-aryl-sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents
CN101218229A (zh) * 2005-05-05 2008-07-09 阿斯利康(瑞典)有限公司 吡唑基-氨基取代的嘧啶及其在癌症治疗中的应用
AU2006254840B2 (en) 2005-06-08 2012-08-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
JP2008543855A (ja) 2005-06-13 2008-12-04 ライジェル ファーマシューティカルズ， インコーポレイテッド 変形性骨疾患を処置するための方法および組成物
EA015890B1 (ru) 2005-06-14 2011-12-30 Тайджен Байотекнолоджи Ко. Лтд. Производные пиримидина
US20070032514A1 (en) 2005-07-01 2007-02-08 Zahn Stephan K 2,4-diamino-pyrimidines as aurora inhibitors
WO2007023382A2 (en) 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
EP1931322B1 (en) 2005-09-07 2012-08-15 Merck Serono SA Ikk inhibitors for the treatment of endometriosis
WO2007035309A1 (en) * 2005-09-15 2007-03-29 Merck & Co., Inc. Tyrosine kinase inhibitors
DE102005048072A1 (de) 2005-09-24 2007-04-05 Bayer Cropscience Ag Thiazole als Fungizide
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
AR060890A1 (es) 2006-05-15 2008-07-23 Boehringer Ingelheim Int Compuestos derivados de pirimidina y composicion farmaceutica en base a ellos
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
US20070293525A1 (en) 2006-06-15 2007-12-20 Djung Jane F 2-anilino-4-aminoalkyleneaminopyrimidines
US20080131937A1 (en) 2006-06-22 2008-06-05 Applera Corporation Conversion of Target Specific Amplification to Universal Sequencing
WO2008016675A1 (en) 2006-08-01 2008-02-07 Praecis Pharmaceuticals Incorporated P38 kinase inhibitors
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
US20080194575A1 (en) 2006-10-04 2008-08-14 Naiara Beraza Treatment for non-alcoholic-steatohepatitis
ES2377717T3 (es) 2006-11-27 2012-03-30 Ares Trading S.A. Tratamiento del mieloma múltiple
ME00811B (me) 2006-12-08 2012-03-20 Novartis Ag JEDINJENJA l KOMPOZICIJE KAO INHIBITORI PROTEIN KINAZE
GB0625196D0 (en) 2006-12-18 2007-01-24 7Tm Pharma As Modulators of cannabinoid receptor
EP2099771A1 (en) 2006-12-19 2009-09-16 Genentech, Inc. Pyrimidine kinase inhibitors
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
EP2109605B1 (en) 2006-12-22 2013-02-20 Boehringer Ingelheim International GmbH 2- [(phenylamino) -pyrimidin-4ylamin0] -cyclopentane carboxamide derivatives and related compounds as inhibitors of kinases of the cell cycle for the treatment of cancer
AU2008215948A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of AD and related conditions
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
TW200846344A (en) 2007-04-25 2008-12-01 Astrazeneca Ab Chemical compounds
AU2008258508A1 (en) 2007-06-08 2008-12-11 Bayer Cropscience Ag Fungicide heterocyclyl-pyrimidinyl-amino derivatives
AU2008275918B2 (en) 2007-07-17 2014-01-30 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as PKC inhibitors
EP2610256B1 (en) 2007-09-28 2016-04-27 Cyclacel Limited Pyrimidine derivatives as protein kinase inhibitors
US8058279B2 (en) 2007-10-09 2011-11-15 Dow Agrosciences Llc Insecticidal pyrimidinyl aryl hyrdrazones
ES2569528T3 (es) 2007-11-16 2016-05-11 Incyte Holdings Corporation 4-pirazolil-N-arilpirimidin-2-aminas y 4-pirazolil-N-heteroarilpirimidin-2-aminas como inhibidores de quinasas Janus
WO2009071535A1 (en) 2007-12-03 2009-06-11 Boehringer Ingelheim International Gmbh Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation
CA2707989A1 (en) 2007-12-07 2009-06-11 Novartis Ag Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases
WO2009103032A1 (en) 2008-02-15 2009-08-20 Rigel Pharmaceuticals, Inc. Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
CL2009000600A1 (es) 2008-03-20 2010-05-07 Bayer Cropscience Ag Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas.
WO2009122180A1 (en) 2008-04-02 2009-10-08 Medical Research Council Pyrimidine derivatives capable of inhibiting one or more kinases
WO2009127642A2 (en) * 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
MX2010012703A (es) 2008-05-21 2010-12-21 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
PE20100087A1 (es) 2008-06-25 2010-02-08 Irm Llc Compuestos y composiciones como inhibidores de cinasa
EP2303824B1 (en) 2008-06-25 2015-03-25 Edison Pharmaceuticals, Inc. 2-heterocyclylaminoalkyl-(p-quinone) derivatives for treatment of oxidative stress diseases
US8445505B2 (en) 2008-06-25 2013-05-21 Irm Llc Pyrimidine derivatives as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
UA101676C2 (uk) 2008-07-31 2013-04-25 Дженентек, Инк. Піримідинові сполуки, композиції і способи застосування
BRPI0918472A2 (pt) 2008-09-01 2015-12-01 Astellas Pharma Inc composto 2,4-diaminopirimidina
EP2161259A1 (de) 2008-09-03 2010-03-10 Bayer CropScience AG 4-Halogenalkylsubstituierte Diaminopyrimidine als Fungizide
US20100144722A1 (en) 2008-09-03 2010-06-10 Dr. Reddy's Laboratories Ltd. Novel heterocyclic compounds as gata modulators
WO2010025863A2 (de) 2008-09-03 2010-03-11 Bayer Cropscience Ag 4-alkyl-substituierte diaminopyrimidine
WO2010025850A1 (de) 2008-09-03 2010-03-11 Bayer Cropscience Ag Heterozyklisch substituierte anilinopyrimidine als fungizide
KR20110051266A (ko) 2008-09-03 2011-05-17 바이엘 크롭사이언스 아게 살진균제로서의 헤테로사이클 치환된 아닐리노피리미딘
UY32158A (es) 2008-10-03 2010-04-30 Astrazeneca Ab Derivados heterociclicos y metodos de uso de los mismos
UY32240A (es) 2008-11-14 2010-06-30 Boeringer Ingelheim Kg Nuevas 2,4-diaminopirimidinas, sus sales farmacéuticamente aceptables, composiciones conteniéndolas y aplicaciones.
GB0821307D0 (en) 2008-11-21 2008-12-31 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
EP2379559B1 (en) 2009-01-06 2017-10-25 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
US20110071158A1 (en) 2009-03-18 2011-03-24 Boehringer Ingelheim International Gmbh New compounds
EP2415765A4 (en) * 2009-03-30 2012-08-15 Astellas Pharma Inc PYRIMIDINE COMPOUND
EP2419423A1 (en) 2009-04-14 2012-02-22 Cellzome Limited Fluoro substituted pyrimidine compounds as jak3 inhibitors
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法
TW201100441A (en) 2009-06-01 2011-01-01 Osi Pharm Inc Amino pyrimidine anticancer compounds
US20120142667A1 (en) 2009-06-10 2012-06-07 Nigel Ramsden Pyrimidine derivatives as zap-70 inhibitors
CA2764983A1 (en) * 2009-06-10 2010-12-16 Abbott Laboratories 2- ( lh-pyrazol-4 -ylamino ) -pyrimidine as kinase inhibitors
AR077033A1 (es) 2009-06-11 2011-07-27 Hoffmann La Roche Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas
US20120172384A1 (en) 2009-06-18 2012-07-05 Mihiro Sunose Heterocyclylaminopyrimidines as kinase inhibitors
EP2443095A1 (en) 2009-06-18 2012-04-25 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
IN2012DN02534A (es) 2009-09-16 2015-08-28 Avila Therapeutics Inc
US8778939B2 (en) 2009-09-29 2014-07-15 Glaxo Group Limited Compounds
JP5740409B2 (ja) 2009-11-13 2015-06-24 ジェノスコ キナーゼ阻害剤
SG181952A1 (en) 2009-12-29 2012-07-30 Emergent Product Dev Seattle Heterodimer binding proteins and uses thereof
US8470820B2 (en) 2010-01-22 2013-06-25 Hoffman-La Roche Inc. Nitrogen-containing heteroaryl derivatives
HUE029196T2 (en) * 2010-06-04 2017-02-28 Hoffmann La Roche Aminoprimidine derivatives as LRRK2 modulators
MX349556B (es) * 2011-11-29 2017-08-03 Genentech Inc Derivados de aminopirimidina como moduladores de proteina cinasa 2 rica en unidades repetitivas de leucina (lrrk2).
US8791130B2 (en) * 2011-11-29 2014-07-29 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 modulators
AR089182A1 (es) * 2011-11-29 2014-08-06 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
CA2850594C (en) * 2011-11-29 2020-03-10 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as lrrk2 modulators
EP2785381B1 (en) * 2011-11-30 2016-05-18 F.Hoffmann-La Roche Ag Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (pet) imaging for lrrk2

Also Published As

Publication number Publication date
MX2013005199A (es) 2013-06-28
JP6524284B2 (ja) 2019-06-05
EP3124483B1 (en) 2019-07-10
JP5986094B2 (ja) 2016-09-06
WO2012062783A1 (en) 2012-05-18
CA3017869C (en) 2021-07-27
EP2638031B9 (en) 2020-01-08
CA2812669C (en) 2018-11-06
RS56583B1 (sr) 2018-02-28
IL225234A0 (en) 2013-06-27
PT3124483T (pt) 2019-10-02
RS59106B1 (sr) 2019-09-30
JP2018109038A (ja) 2018-07-12
JP2013545741A (ja) 2013-12-26
CY1120073T1 (el) 2018-12-12
SI2638031T1 (en) 2018-02-28
CA2812669A1 (en) 2012-05-18
SI3124483T1 (sl) 2019-10-30
BR112013011600A8 (pt) 2021-09-08
JP2017008074A (ja) 2017-01-12
MA34644B1 (fr) 2013-11-02
HUE046617T2 (hu) 2020-03-30
EP3590933B1 (en) 2021-01-06
EP2638031A1 (en) 2013-09-18
PL3124483T3 (pl) 2020-03-31
JP6298115B2 (ja) 2018-03-20
DK3124483T3 (da) 2019-09-02
EP3124483A1 (en) 2017-02-01
TW201302733A (zh) 2013-01-16
EP3590933A1 (en) 2020-01-08
ES2746134T3 (es) 2020-03-04
CN103313978A (zh) 2013-09-18
CA3017869A1 (en) 2012-05-18
AU2011328139A1 (en) 2013-04-04
US20120157427A1 (en) 2012-06-21
CN103313978B (zh) 2015-04-15
BR112013011600A2 (pt) 2016-08-09
HK1187605A1 (en) 2014-04-11
AR083813A1 (es) 2013-03-27
LT2638031T (lt) 2017-12-11
ES2653967T3 (es) 2018-02-09
BR112013011600B1 (pt) 2022-01-11
HRP20172006T1 (hr) 2018-02-09
US8815882B2 (en) 2014-08-26
PT2638031T (pt) 2018-01-03
HUE037844T2 (hu) 2018-09-28
NO2638031T3 (es) 2018-03-10
EP2638031B1 (en) 2017-10-11
DK2638031T3 (en) 2017-12-11
KR101566091B1 (ko) 2015-11-04
PH12013500880A1 (en) 2013-07-01
LT3124483T (lt) 2019-09-25
KR20130093657A (ko) 2013-08-22
SG189043A1 (en) 2013-05-31
PL2638031T3 (pl) 2018-03-30
HRP20191781T1 (hr) 2019-12-27

Similar Documents

Publication Publication Date Title
ECSP13012611A (es) Derivados de pirazol-aminopirimidina como moduladores de la lrrk2
CO6620050A2 (es) Derivados de aminopirimidina como moduladores de la lrrk2
MX2014006026A (es) Derivados de aminopirimidina como moduladores de proteina cinasa 2 rica en unidades repetitivas de leucina (lrrk2).
MX2014006027A (es) Derivados de 2-fenilaminopirimidina como moduladores de proteina cinasa 2 rica en unidades repetitivas de leucina (lrrk2) para el tratamiento de la enfermedad de parkinson.
MX348606B (es) Derivados de aminopirimidina como moduladores de proteina cinasa 2 de repeticion rica en leucina (lrrk2).
BR112014027117A8 (pt) Derivados de pirazol aminopirimidina como moduladores de lrrk2, seus usos, e composição
MX348920B (es) Derivados de 2-(fenil o pirid-3-il)aminopirimidina como moduladores de proteina cinasa 2 de repeticion rica en leucina (lrrk2) para el tratamiento de la enfermedad de parkinson.
BR112014026952A2 (pt) derivados de aminopirimidina pirazol como moduladores lrrk2
GT201400301A (es) 7h-pirrolo [2,3-d] pirimidinas-4- ( aminho-substituidas) novedosas como inhibidores de lrrk2
ECSP10010582A (es) Derivados de aminodihidrotiazina como inhibidores de bace para el tratamiento de la enfermedad de alzheimer
MX388468B (es) Compuestos multicíclicos y métodos de uso de los mismos.
CO6491058A2 (es) Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurológicos
CY1117745T1 (el) Ετεροκυκλικες ενωσεις και χρηση αυτων ως ρυθμιστες υποδοχεα τυπου iii κινασων τυροσινης
ECSP14013215A (es) Compuestos novedosos
BR112012029647A2 (pt) novos derivados de pirimidinas
DOP2011000107A (es) Derivados de anilina-pirimidina sustituidos con sulfoximina como inhibidores de quinasas dependientes de ciclina (cdk), produccion y uso de los mismos como productos medicinales
CO6470820A2 (es) Espiro-epóxidos como productos intermedios
DOP2011000134A (es) Lactamas como inhibidores de beta secretasa
UY33655A (es) Co-cristales y sales de inhibidores de ccr30
UY32055A (es) Derivados sustituidos de la 5-Halo-N2-[sustituido](1-metil-1H-imidazol-4-il)pirimidin-2,-diamina y sus sales farmacéuticamente aceptables, procesos de preparación, composiciones y aplicaciones.
CO6321280A2 (es) Nueva clase espiro piperidinas para el tratamiento de enfermedades neurodegenerativas
MX376307B (es) Derivados de oxazetidina, proceso para su preparacion y uso de los mismos en medicina humana y en cosmetica.
UY31680A1 (es) "agonistas de los receptores muscarínicos, composiciones, métodos de tratamiento en que se emplean y sus procesos de preparación-176"
UY33584A (es) Nuevos compuestos benzamida de inhibidores lrrk2