MX2010008700A - Moduladores de beta-amiloide. - Google Patents

Moduladores de beta-amiloide.

Info

Publication number
MX2010008700A
MX2010008700A MX2010008700A MX2010008700A MX2010008700A MX 2010008700 A MX2010008700 A MX 2010008700A MX 2010008700 A MX2010008700 A MX 2010008700A MX 2010008700 A MX2010008700 A MX 2010008700A MX 2010008700 A MX2010008700 A MX 2010008700A
Authority
MX
Mexico
Prior art keywords
modulators
amyloid beta
amyloid
formula
disease
Prior art date
Application number
MX2010008700A
Other languages
English (en)
Inventor
Synese Jolidon
Erwin Goetschi
Alexander Flohr
Thomas Luebbers
Helmut Jacobsen
Karlheinz Baumann
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 MX2010008700A publication Critical patent/MX2010008700A/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
    • C07D403/02—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
    • 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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La invención se refiere a compuestos de la fórmula I (ver fórmula (I)) en la que los sustituyentes tienen los significados definidos en la reivindicación 1. Se ha encontrado que los compuestos presentes de la fórmula I son moduladores de beta-amiloide y, por ello, pueden ser útiles para el tratamiento o la prevención de una enfermedad asociada con la deposición del ß-amiloide en cerebro, en particular la enfermedad de Alzheimer y otras enfermedades como son la angiopatía cerebral amiloide, la hemorragia cerebral hereditaria con amiloidosis de tipo Dutch (HCHWA-D), la demencia multiinfarto, la demencia pugilística y el síndrome de Down.
MX2010008700A 2008-02-22 2009-02-12 Moduladores de beta-amiloide. MX2010008700A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08151825 2008-02-22
PCT/EP2009/051613 WO2009103652A1 (en) 2008-02-22 2009-02-12 Modulators for amyloid beta

Publications (1)

Publication Number Publication Date
MX2010008700A true MX2010008700A (es) 2010-08-30

Family

ID=40481869

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2010008700A MX2010008700A (es) 2008-02-22 2009-02-12 Moduladores de beta-amiloide.

Country Status (18)

Country Link
US (2) US20090215759A1 (es)
EP (1) EP2257541B1 (es)
JP (1) JP5328816B2 (es)
KR (1) KR101247840B1 (es)
CN (1) CN101952275B (es)
AR (1) AR070437A1 (es)
AU (1) AU2009216851B2 (es)
BR (1) BRPI0907577A2 (es)
CA (1) CA2713716A1 (es)
CL (1) CL2009000380A1 (es)
ES (1) ES2428716T3 (es)
IL (1) IL206945A (es)
MX (1) MX2010008700A (es)
PE (1) PE20091472A1 (es)
RU (1) RU2010137300A (es)
TW (1) TW200938535A (es)
WO (1) WO2009103652A1 (es)
ZA (1) ZA201005399B (es)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA017252B1 (ru) 2007-08-28 2012-11-30 Айрм Ллк Производные 2-бифениламино-4-аминопиримидина в качестве ингибиторов киназ
WO2009032861A1 (en) * 2007-09-04 2009-03-12 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
CA2703824C (en) * 2008-01-11 2016-06-07 F. Hoffmann-La Roche Ag Modulators for amyloid beta
RU2010137300A (ru) 2008-02-22 2012-03-27 Ф. Хоффманн-Ля Рош Аг (Ch) Модуляторы бета-амилоида
UA101057C2 (en) * 2008-06-25 2013-02-25 Айерем Элелси Pyrimidine derivatives as kinase inhibitors
US8445505B2 (en) 2008-06-25 2013-05-21 Irm Llc Pyrimidine derivatives as kinase inhibitors
PE20100087A1 (es) 2008-06-25 2010-02-08 Irm Llc Compuestos y composiciones como inhibidores de cinasa
KR101324414B1 (ko) 2008-10-09 2013-11-01 에프. 호프만-라 로슈 아게 아밀로이드 베타의 조절자
EP2367826A4 (en) 2008-11-06 2012-07-04 Astrazeneca Ab MODULATORS OF THE PROTEIN -AMYLOID
KR101293421B1 (ko) * 2008-11-10 2013-08-05 에프. 호프만-라 로슈 아게 헤테로사이클릭 감마 분비효소 조절제
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
TW201030002A (en) 2009-01-16 2010-08-16 Bristol Myers Squibb Co Bicyclic compounds for the reduction of beta-amyloid production
ES2481715T3 (es) 2009-02-06 2014-07-31 Janssen Pharmaceuticals, Inc. Compuestos heterocíclicos bicíclicos sustituidos novedosos como moduladores de gamma-secretasa
TWI461425B (zh) 2009-02-19 2014-11-21 Janssen Pharmaceuticals Inc 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類
AU2010262036B2 (en) 2009-05-07 2014-10-30 Cellzome Limited Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators
KR20120050450A (ko) 2009-07-15 2012-05-18 얀센 파마슈티칼즈, 인코포레이티드 감마 세크레타제 조절제로서의 치환된 트리아졸 및 이미다졸 유도체
US8637525B2 (en) 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
TWI468402B (zh) * 2009-07-31 2015-01-11 必治妥美雅史谷比公司 降低β－類澱粉生成之化合物
EP2993169B1 (en) 2009-11-17 2017-12-20 Novartis AG Aryl-pyridine derivatives as aldosterone synthase inhibitors
ES2512840T3 (es) 2010-01-15 2014-10-24 Janssen Pharmaceuticals, Inc. Derivados de triazol bicíclicos sustituidos novedosos como moduladores de gamma-secretasa
US20110190269A1 (en) 2010-02-01 2011-08-04 Karlheinz Baumann Gamma secretase modulators
US8486967B2 (en) 2010-02-17 2013-07-16 Hoffmann-La Roche Inc. Heteroaryl substituted piperidines
US20110256064A1 (en) * 2010-04-16 2011-10-20 Ac Immune, S.A. Novel Compounds for the Treatment of Diseases Associated with Amyloid or Amyloid-like Proteins
EP2628734A4 (en) 2010-10-15 2014-04-23 Federalnoe G Bydzhetnoe Uchrezhdenie Nauki Inst Fiziol Aktivnikh Veschestv Rossiiskoi Akademii Nauk DERIVATIVES OF 5-AMINO - [1,2,4] THIADIAZOLE
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
MX336155B (es) * 2011-02-25 2016-01-07 Yuhan Corp Derivados de diaminopirimidina y procesos para su preparacion.
US8703763B2 (en) 2011-03-02 2014-04-22 Hoffmann-La Roche Inc. Bridged piperidine derivatives
US8987276B2 (en) 2011-03-24 2015-03-24 Janssen Pharmaceuticals, Inc. Substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators
ES2602794T3 (es) 2011-03-31 2017-02-22 Pfizer Inc Piridinonas bicíclicas novedosas
AU2012285931B2 (en) 2011-07-15 2017-01-12 Cellzome Limited Novel substituted indole derivatives as gamma secretase modulators
CN103781779B (zh) * 2011-09-05 2016-06-08 浙江海正药业股份有限公司 具有蛋白激酶抑制活性的4-取代-(3-取代-1h-吡唑-5-氨基)-嘧啶衍生物及其用途
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
ES2585009T3 (es) 2012-05-16 2016-10-03 Janssen Pharmaceuticals, Inc. Derivados de 3,4-dihidro-2H-pirido[1,2-a]pirazina-1,6-diona sustituidos útiles para el tratamiento de (inter alia) enfermedad de Alzheimer
WO2014007951A2 (en) 2012-06-13 2014-01-09 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
JP6275161B2 (ja) 2012-12-20 2018-02-07 ヤンセン ファーマシューティカ エヌ．ベー． γセクレターゼ調節剤としての新規な三環式３，４−ジヒドロ−２Ｈ−ピリド［１，２−ａ］ピラジン−１，６−ジオン誘導体
US10246454B2 (en) 2013-01-17 2019-04-02 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators
EP2958918B1 (en) 2013-02-21 2016-12-07 Boehringer Ingelheim International GmbH Dihydropteridinones ii
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
EP3004079B1 (en) * 2013-06-04 2018-01-17 Acturum Real Estate AB Pyrimidine compounds and their use as gamma secretase modulators
EP3004081B1 (en) 2013-06-04 2017-11-15 Acturum Real Estate AB Triazole compounds and their use as gamma secretase modulators
WO2014195322A1 (en) 2013-06-04 2014-12-11 Acturum Life Science AB Triazole compounds and their use as gamma secretase modulators
US10562897B2 (en) 2014-01-16 2020-02-18 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators
JP2015178576A (ja) * 2014-03-19 2015-10-08 富士フイルム株式会社 化合物、着色組成物、インクジェット記録用インク、インクジェット記録方法、インクジェットプリンタカートリッジ、及びインクジェット記録物
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
NZ773116A (en) 2015-02-20 2024-05-31 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
US10538516B2 (en) 2015-03-25 2020-01-21 National Center For Geriatrics And Gerontology Oxadiazole derivative and pharmaceutical containing same
JP6831372B2 (ja) * 2015-09-09 2021-02-17 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 架橋ピペリジン誘導体
CA2997537C (en) 2015-09-18 2024-02-13 Kaken Pharmaceutical Co., Ltd. Biaryl derivative and medicine containing same
AU2017250369A1 (en) * 2016-04-15 2018-10-11 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as EHMT1 and EHMT2 inhibitors
JP2019525947A (ja) 2016-06-01 2019-09-12 エムスリー・バイオテクノロジー・インコーポレイテッドＭ３ Ｂｉｏｔｅｃｈｎｏｌｏｇｙ， Ｉｎｃ． 化合物
CN109311878B (zh) 2016-06-27 2022-05-24 豪夫迈·罗氏有限公司 作为γ-分泌酶调节剂的三唑并吡啶类化合物
PL3555070T3 (pl) * 2016-12-19 2023-11-06 Epizyme, Inc. Związki heteroarylowe podstawione aminą jako inhibitory ehmt2 i sposoby ich zastosowania
AU2018254577B2 (en) 2017-04-21 2024-06-13 Epizyme, Inc. Combination therapies with EHMT2 inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3675861A4 (en) * 2017-09-01 2021-01-06 Kadmon Corporation, LLC ALPHA SUPERWINDING PROTEIN KINASE INHIBITORS ("COILED-COIL") ASSOCIATED WITH RHO
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
MX2020012034A (es) * 2018-05-11 2021-04-12 Glaxosmithkline Ip Dev Ltd Inhibidores de furina.
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP2023509260A (ja) 2019-08-14 2023-03-08 インサイト・コーポレイション Ｃｄｋ２阻害剤としてのイミダゾリルピリミジニルアミン化合物
US10702525B1 (en) 2019-09-04 2020-07-07 United Arab Emirates University Pyrimidine derivatives as anti-diabetic agents
CN114302876A (zh) * 2019-09-06 2022-04-08 英夫拉索姆有限公司 Nlrp3抑制剂
CN110590739A (zh) * 2019-09-20 2019-12-20 中国药科大学 一种艾乐替尼的制备方法
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AR120184A1 (es) 2019-10-11 2022-02-02 Incyte Corp Aminas bicíclicas como inhibidoras de la cdk2
BR112022007163A2 (pt) 2019-10-14 2022-08-23 Incyte Corp Heterociclos bicíclicos como inibidores de fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11407750B2 (en) 2019-12-04 2022-08-09 Incyte Corporation Derivatives of an FGFR inhibitor
JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
BR112022024068A2 (pt) 2021-05-17 2023-12-05 Voronoi Inc Compostos de derivado de heteroarila e usos dos mesmos
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
CN117447407B (zh) * 2023-12-19 2024-06-11 潍坊医学院 一种JAK2抑制剂Pacritinib及其中间体的制备方法

Family Cites Families (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG47583A1 (en) * 1986-01-13 1998-04-17 American Cyanamid Co 4,5,6-Substituted-n- (substituted-phenyl) -2- pyrimidinamines
DE4208254A1 (de) 1992-03-14 1993-09-16 Hoechst Ag Substituierte pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel und fungizid
US5387595A (en) 1992-08-26 1995-02-07 Merck & Co., Inc. Alicyclic compounds as tachykinin receptor antagonists
US5686070A (en) * 1994-03-03 1997-11-11 Genentech, Inc. Methods for treating bacterial pneumonia
DE69620241T2 (de) 1995-12-14 2002-10-02 MERCK & CO., INC. (A NEW JERSEY CORP.) Gonadotropin releasing hormon- antagonisten
ES2237919T4 (es) 1998-06-18 2007-05-01 Bristol-Myers Squibb Company Inhibidores aminotiazol sustituidos con carbono de quinasas dependientes de ciclina.
WO2000025780A1 (en) * 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
US6596747B2 (en) 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
SE9803773D0 (sv) 1998-11-05 1998-11-05 Astra Pharma Prod Compounds
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
AU5852300A (en) 1999-07-15 2001-02-05 Sumitomo Pharmaceuticals Company, Limited Heteroaromatic ring compounds
GB9924862D0 (en) * 1999-10-20 1999-12-22 Celltech Therapeutics Ltd Chemical compounds
JP4794793B2 (ja) 1999-12-28 2011-10-19 ファーマコペイア， インコーポレイテッド Ｎ−ヘテロ環ＴＮＦ−α発現阻害剤
WO2001087845A2 (en) 2000-05-15 2001-11-22 Fujisawa Pharmaceutical Co., Ltd. N-containing heterocyclic compounds and their use as 5-ht antagonists
BR0116792A (pt) 2000-12-22 2004-02-17 Ortho Mcneil Pharm Inc Derivados de diamina de triazol substituìdos como inibidores de quinase
EP1399441B1 (en) 2001-06-28 2006-07-05 Smithkline Beecham Plc N-aroyl cyclic amine derivatives as orexin receptor antagonists
WO2003040141A1 (en) * 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
WO2003032994A2 (de) * 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
FR2833948B1 (fr) 2001-12-21 2004-02-06 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et leur utilisation en tant que medicament
AU2003244463A1 (en) 2002-02-05 2003-09-02 Yamanouchi Pharmaceutical Co., Ltd. 2,4,6-triamino-1,3,5-triazine derivative
WO2003095448A1 (en) * 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
MXPA05000200A (es) * 2002-07-02 2005-06-06 Schering Corp Nuevos antagonistas del receptor neuropeptido y y5.
US7163928B2 (en) 2003-02-03 2007-01-16 Cv Therapeutics, Inc. Partial and full agonists of A1 adenosine receptors
US7276502B2 (en) * 2003-03-25 2007-10-02 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
CN102584813B (zh) 2003-05-14 2016-07-06 Ngc药物公司 化合物及其在调节淀粉样蛋白β中的用途
WO2005003103A2 (en) 2003-06-30 2005-01-13 Astrazeneca Ab 2, 4, 6-tri-substituted 6-membered heterocycles and their use in the treatment of neurodegenerative diseases
DE602004032446D1 (de) * 2003-08-07 2011-06-09 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
JP2007508260A (ja) 2003-10-09 2007-04-05 アクテリオン　ファマシューティカルズ　リミテッド 新規なテトラヒドロピリジン誘導体
JP2007510647A (ja) 2003-10-30 2007-04-26 メルク　エンド　カムパニー　インコーポレーテッド カンナビノイド受容体調節剤としてのアラルキルアミン類
US20070167329A1 (en) 2003-12-24 2007-07-19 Bayer Cropscience Gmbh Plant growth regulation
US7649002B2 (en) 2004-02-04 2010-01-19 Pfizer Inc (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists
MY149038A (en) * 2004-05-26 2013-07-15 Eisai R&D Man Co Ltd Cinnamide compound
GT200500286A (es) * 2004-10-13 2006-06-13 Analogos de anilino-pirimidina
ATE387202T1 (de) 2004-10-15 2008-03-15 Glaxo Group Ltd Pyrrolidinderivate als histaminrezeptor-liganden
KR20070094754A (ko) 2004-12-01 2007-09-21 데브젠 엔브이 이온 채널, 특히 Ｋｖ 패밀리로부터의 이온 채널과상호작용하는 5-카복사미도 치환된 티아졸 유도체
WO2006113704A2 (en) 2005-04-18 2006-10-26 Neurogen Corporation Subtituted heteroaryl cb1 antagonists
US20060241038A1 (en) 2005-04-20 2006-10-26 Eisai Co., Ltd. Therapeutic agent for Abeta related disorders
EP1910369A1 (en) 2005-07-29 2008-04-16 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
KR101006362B1 (ko) 2005-10-06 2011-01-10 닛뽕소다 가부시키가이샤 고리형 아민 화합물 및 유해 생물 방제제
MY167260A (en) * 2005-11-01 2018-08-14 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007051333A1 (en) 2005-11-02 2007-05-10 Oncalis Ag Triazine beta-secretase inhibitors
WO2007054480A1 (en) 2005-11-08 2007-05-18 N.V. Organon 2-(benzimidazol-1-yl)-acetamide biaryl derivatives and their use as inhibitors of the trpv1 receptor
WO2007058304A1 (ja) 2005-11-18 2007-05-24 Eisai R & D Management Co., Ltd. シンナミド化合物の塩またはそれらの溶媒和物
JPWO2007058305A1 (ja) 2005-11-18 2009-05-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 シンナミド誘導体の製造方法
EP1953154A4 (en) 2005-11-24 2013-11-20 Eisai R&D Man Co Ltd CINNAMIDE COMPOUNDS OF MORPHOLINE TYPE
TWI370130B (en) 2005-11-24 2012-08-11 Eisai R&D Man Co Ltd Two cyclic cinnamide compound
US20070117839A1 (en) * 2005-11-24 2007-05-24 Eisai R&D Management Co., Ltd. Two cyclic cinnamide compound
US20090131407A1 (en) 2005-12-16 2009-05-21 Brian Safina Tetracyclic kinase inhibitors
WO2007076161A2 (en) 2005-12-27 2007-07-05 Myriad Genetics, Inc Compounds with therapeutic activity
EP2399922B1 (en) 2006-02-10 2019-06-26 Universal Display Corporation Metal complexes of cyclometallated imidazo(1,2-f) phenanthridine and diimidazo(1,2-A;1',2'-C)quinazoline ligands and isoelectronic and benzannulated analogs therof
MX2008011221A (es) 2006-03-09 2008-09-11 Eisai R&D Man Co Ltd Compuestos de cinamida policiclicos.
TWI378091B (en) * 2006-03-09 2012-12-01 Eisai R&D Man Co Ltd Multi-cyclic cinnamide derivatives
EP2060575A1 (de) 2006-04-19 2009-05-20 Boehringer Ingelheim International GmbH Dihydrothienopyrimidine zur Behandlung von entzündlichen Erkrankungen
EP2024342A2 (en) 2006-05-01 2009-02-18 Pfizer Products Incorporated Substituted 2-amino-fused heterocyclic compounds
ES2352320T3 (es) 2006-05-12 2011-02-17 Ab Science Nuevo procedimiento para la síntesis de compuestos de 2-aminoxazol.
WO2007135970A1 (ja) 2006-05-19 2007-11-29 Eisai R & D Management Co., Ltd. ヘテロ環系－シンナミド誘導体
WO2007135969A1 (ja) * 2006-05-19 2007-11-29 Eisai R & D Management Co., Ltd. ウレア系－シンナミド誘導体
JP2009184924A (ja) 2006-05-31 2009-08-20 Eisai R & D Management Co Ltd 生物学的試薬用化合物
US20080027001A1 (en) * 2006-07-07 2008-01-31 Andrew Wood Nogo receptor functional motifs, peptide mimetics, and mutated functional motifs related thereto, and methods of using the same
SA07280403B1 (ar) 2006-07-28 2010-12-01 إيساي أر أند دي منجمنت كو. ليمتد ملح رباعي لمركب سيناميد
US8133901B2 (en) 2006-12-01 2012-03-13 Actelion Pharmaceuticals Ltd. 3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors
EP2099771A1 (en) * 2006-12-19 2009-09-16 Genentech, Inc. Pyrimidine kinase inhibitors
JP2010518080A (ja) 2007-02-08 2010-05-27 メルク・シャープ・エンド・ドーム・コーポレイション 治療薬
US20100204230A1 (en) 2007-02-12 2010-08-12 Peter Blurton Piperazine derivatives for treatment of ad and related conditions
EP2120573A4 (en) 2007-02-12 2011-05-25 Merck Sharp & Dohme DERIVATIVES OF PIPERIDINE
DE102007010801A1 (de) * 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
EP3023422A1 (en) * 2007-03-12 2016-05-25 YM BioSciences Australia Pty Ltd Phenyl amino pyrimidine compounds and uses thereof
JP5264890B2 (ja) * 2007-05-11 2013-08-14 エフ．ホフマン−ラ ロシュ アーゲー アミロイドベータの調節剤としてのヘタリールアニリン
US8242150B2 (en) 2007-06-13 2012-08-14 Merck Sharp & Dohme Corp. Triazole derivatives for treating alzheimer'S disease and related conditions
WO2009032861A1 (en) * 2007-09-04 2009-03-12 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
MX2010002674A (es) 2007-09-06 2010-03-25 Schering Corp Moduladores de gamma secretasa.
WO2009046416A1 (en) * 2007-10-05 2009-04-09 Targegen Inc. Anilinopyrimidines as jak kinase inhibitors
US20110124649A1 (en) 2007-11-09 2011-05-26 The Johns Hopkins University Inhibitors of human methionine aminopeptidase 1 and methods of treating disorders
US20100298372A1 (en) 2007-12-11 2010-11-25 Schering Corporation Gamma secretase modulators
EP2234999A1 (en) * 2007-12-21 2010-10-06 F. Hoffmann-La Roche AG Heteroaryl derivatives as orexin receptor antagonists
CA2703824C (en) * 2008-01-11 2016-06-07 F. Hoffmann-La Roche Ag Modulators for amyloid beta
RU2010137300A (ru) 2008-02-22 2012-03-27 Ф. Хоффманн-Ля Рош Аг (Ch) Модуляторы бета-амилоида
BRPI0910021A2 (pt) 2008-06-20 2015-09-01 Genentech Inc "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinas em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase"
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
EP2367826A4 (en) * 2008-11-06 2012-07-04 Astrazeneca Ab MODULATORS OF THE PROTEIN -AMYLOID
CA2753696A1 (en) 2009-02-26 2010-09-02 Noritaka Kitazawa Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors

Also Published As

Publication number Publication date
BRPI0907577A2 (pt) 2015-07-21
ES2428716T3 (es) 2013-11-11
WO2009103652A1 (en) 2009-08-27
ZA201005399B (en) 2011-04-28
CA2713716A1 (en) 2009-08-27
US20090215759A1 (en) 2009-08-27
CL2009000380A1 (es) 2010-09-21
IL206945A0 (en) 2010-12-30
AR070437A1 (es) 2010-04-07
RU2010137300A (ru) 2012-03-27
AU2009216851A1 (en) 2009-08-27
EP2257541B1 (en) 2013-08-14
TW200938535A (en) 2009-09-16
JP5328816B2 (ja) 2013-10-30
IL206945A (en) 2015-04-30
CN101952275A (zh) 2011-01-19
EP2257541A1 (en) 2010-12-08
PE20091472A1 (es) 2009-09-24
AU2009216851B2 (en) 2013-11-07
US8962834B2 (en) 2015-02-24
US20130190302A1 (en) 2013-07-25
CN101952275B (zh) 2014-06-18
JP2011512380A (ja) 2011-04-21
KR101247840B1 (ko) 2013-03-26
KR20100118118A (ko) 2010-11-04

Similar Documents

Publication Publication Date Title
MX2010008700A (es) Moduladores de beta-amiloide.
MY167264A (en) Bridged piperidine derivatives
DOP2013000147A (es) Compuestos y su uso como inhibidores de bace
MX2009012163A (es) Hetarilanilinas como moduladores para beta-amiloide.
ECSP11011051A (es) Nuevos compuestos 578
EA201200355A1 (ru) Способы предотвращения и лечения ишемии головного мозга
ZA200907575B (en) C3b antobodies and methods for the prevention and treatment of complement associated disorders
TN2015000429A1 (en) 3-acetylamino-1-(phenyl-heteroaryl-aminocarbonyl or phenyl-heteroaryl-carbonylamino)benzene derivatives for the treatment of hyperproliferative disorders
NZ598694A (en) Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
MX2010002312A (es) Compuestos de triazolopiridina y su uso como inhibidores de cinasa reguladora de señal de apoptosis.
CR9347A (es) Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos
MX2009000657A (es) Composiciones y metodos para el tratamiento de mucositis.
TN2014000016A1 (en) 4 - piperidinyl compounds for use as tankyrase inhibitors
IN2014DN05772A (es)
WO2009067493A3 (en) 1,3,5 tri-subtituted benzenes for treatment of alzheimer's disease and other disorders
MY161818A (en) Styrenyl derivate compounds for treating ophthalmic diseases and disorders
WO2010033701A3 (en) Inhibitors of sphingosine kinase 1
BR112015007937A2 (pt) formas cristalinas de um inibidor de fator xia
MY183111A (en) 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9h-carbazole derivatives and their use as prostaglandin d2 receptor modulators
BR112017016378A2 (pt) composições da pró-droga de fumarato de monometila
AR081389A1 (es) Sal de tipo hemifumarato, composicion farmaceutica y proceso de obtencion de la misma.
MX2010008706A (es) Derivados de fenil-prenilo, de origen marino y sintetico. para el tratamiento de enfermedades o trastornos cognitivos, neurodegenerativos o neuronales.
DE602008002598D1 (en) Cyclohexylderivate
WO2009073138A3 (en) Treatment of metabolic syndrome with novel amides
CU20130083A7 (es) Compuestos y su uso como inhibidores de bace

Legal Events

Date Code Title Description
FG Grant or registration