[go: up one dir, main page]

PE20090248A1 - Moduladores de beta-amiloide - Google Patents

Moduladores de beta-amiloide

Info

Publication number
PE20090248A1
PE20090248A1 PE2008000822A PE2008000822A PE20090248A1 PE 20090248 A1 PE20090248 A1 PE 20090248A1 PE 2008000822 A PE2008000822 A PE 2008000822A PE 2008000822 A PE2008000822 A PE 2008000822A PE 20090248 A1 PE20090248 A1 PE 20090248A1
Authority
PE
Peru
Prior art keywords
methyl
phenyl
beta
metoxy
hetaryl
Prior art date
Application number
PE2008000822A
Other languages
English (en)
Inventor
Karlheinz Baumann
Alexander Flohr
Helmut Jacobsen
Synese Jolidon
Thomas Luebbers
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 PE20090248A1 publication Critical patent/PE20090248A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I, EN LA QUE HETARILO I ES a), b) O c); HETARILO II ES d), e) O f); R1 ES H, ALCOXI INFERIOR O CIANO; R2 Y R3 SON H, ALQUILO INFERIOR, -CH2-C(O)-PIPERIDIN-1-ILO, ENTRE OTROS; R4 ES H, -C(O)-FENILO OPCIONALMENTE SUSTUIDO POR HALOGENO, -CH2-CH2-FENILO, ENTRE OTROS; R5 ES H, HALOGENO O ALQUILO INFERIOR; n ES 0 O 1. SON SELECCIONADOS [5-(3-CLORO-BENCIL)-4-METIL-TIAZOL-2-IL]-[3-METOXI-4-(4-METIL-IMIDAZOL-1-IL)-FENIL]-AMINA, 2-METOXI-1-{2-[3-METOXI-4-(4-METIL-IMIDAZOL-1-IL)-FENILAMINO]-6,7-DIHIDRO-4H-TIAZOLO[5,4-c]PIRIDIN-5-IL}-ETANONA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCESO DE PREPARACION Y COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES BETA AMILOIDE, UTILES EN EL TRATAMIENTO DE ALZHEIMER, ANGIOPATIA CEREBRAL AMILOIDE, HCHWA-D, DEMENCIA MULTIINFARTO O PUGILISTICA O SINDROME DE DOWN
PE2008000822A 2007-05-11 2008-05-09 Moduladores de beta-amiloide PE20090248A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07108004 2007-05-11

Publications (1)

Publication Number Publication Date
PE20090248A1 true PE20090248A1 (es) 2009-03-27

Family

ID=39758855

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000822A PE20090248A1 (es) 2007-05-11 2008-05-09 Moduladores de beta-amiloide

Country Status (20)

Country Link
US (1) US7910740B2 (es)
EP (1) EP2155740B1 (es)
JP (1) JP5264890B2 (es)
KR (1) KR101138045B1 (es)
CN (1) CN101675045B (es)
AR (1) AR066509A1 (es)
AT (1) ATE496915T1 (es)
AU (1) AU2008250436B2 (es)
BR (1) BRPI0811993A2 (es)
CA (1) CA2686754C (es)
CL (1) CL2008001347A1 (es)
DE (1) DE602008004769D1 (es)
ES (1) ES2358863T3 (es)
IL (1) IL201566A (es)
MX (1) MX2009012163A (es)
PE (1) PE20090248A1 (es)
RU (1) RU2009140182A (es)
TW (1) TW200904420A (es)
WO (1) WO2008138753A1 (es)
ZA (1) ZA200907585B (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY149038A (en) * 2004-05-26 2013-07-15 Eisai R&D Man Co Ltd Cinnamide compound
ES2338904T3 (es) * 2004-10-26 2010-05-13 EISAI R&D MANAGEMENT CO., LTD. Forma amorfa de compuestos de cinamida.
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
US20090048448A1 (en) * 2005-11-18 2009-02-19 Ikuo Kushida Salts of cynnamide compound or solvates thereof
JP5221144B2 (ja) * 2005-11-24 2013-06-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 モルホリンタイプ・シンナミド化合物
TWI370130B (en) * 2005-11-24 2012-08-11 Eisai R&D Man Co Ltd Two cyclic cinnamide compound
TWI378091B (en) * 2006-03-09 2012-12-01 Eisai R&D Man Co Ltd Multi-cyclic cinnamide derivatives
US7737141B2 (en) * 2006-07-28 2010-06-15 Eisai R&D Management Co., Ltd. Prodrug of cinnamide compound
EP2097376A2 (en) 2006-12-22 2009-09-09 F. Hoffmann-Roche AG Spiro-piperidine derivatives
PE20081791A1 (es) * 2007-02-28 2009-02-07 Eisai Randd Man Co Ltd Dos derivados ciclicos de oxomorfolina
CA2687262A1 (en) * 2007-05-16 2008-11-20 Naoyuki Shimomura One-pot production process for cinnamide derivative
US7935815B2 (en) * 2007-08-31 2011-05-03 Eisai R&D Management Co., Ltd. Imidazoyl pyridine compounds and salts thereof
AR068121A1 (es) 2007-08-31 2009-11-04 Eisai R&D Man Co Ltd Compuestos multiciclicos para tratar enfermedades neurodegenerativas
KR101204213B1 (ko) * 2007-12-21 2012-11-26 에프. 호프만-라 로슈 아게 오렉신 수용체 길항제로서의 헤테로아릴 유도체
ES2375919T3 (es) * 2008-01-11 2012-03-07 F. Hoffmann-La Roche Ag Moduladores de beta-amiloide.
CA2712095A1 (en) * 2008-01-28 2009-08-06 Eisai R&D Management Co., Ltd. Crystalline cinnamide compounds or salts thereof
CN101952275B (zh) * 2008-02-22 2014-06-18 弗·哈夫曼-拉罗切有限公司 β-淀粉样蛋白的调节剂
MX2011003246A (es) * 2008-10-09 2011-04-21 Hoffmann La Roche Moduladores de beta amiloide.
KR20110082189A (ko) * 2008-11-06 2011-07-18 아스트라제네카 아베 아밀로이드 베타의 조절제
BRPI0921348A2 (pt) * 2008-11-10 2019-09-24 Hoffmann La Roche moduladores heterocíclicos da gama secretase
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
KR20110113197A (ko) 2009-02-06 2011-10-14 오르토-맥닐-얀센 파마슈티칼스 인코포레이티드 감마 세크레타제 조절제로서의 신규 치환된 비사이클릭 헤테로사이클릭 화합물
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
EP2427453B1 (en) * 2009-05-07 2013-07-17 Janssen Pharmaceuticals, Inc. Substituted indazole and aza-indazole derivatives as gamma secretase modulators
UY32622A (es) * 2009-05-12 2010-12-31 Astrazeneca Ab Nuevos compuestos para el tratamiento de patologías relacionadas con ab(beta)
CN102482227A (zh) 2009-07-15 2012-05-30 杨森制药公司 作为γ分泌酶调节剂的取代的三唑和咪唑衍生物
EP2523949B1 (en) 2010-01-15 2014-08-20 Janssen Pharmaceuticals Inc. Novel substituted triazole derivatives as gamma secretase modulators
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
ES2536442T3 (es) 2011-03-24 2015-05-25 Janssen Pharmaceuticals, Inc. Derivados novedosos de triazolil piperazina y triazolil piperidina como moduladores de la gamma secretasa
ES2602794T3 (es) 2011-03-31 2017-02-22 Pfizer Inc Piridinonas bicíclicas novedosas
JP6068464B2 (ja) 2011-07-15 2017-01-25 ヤンセン ファーマシューティカルズ,インコーポレーテッド γ−セクレターゼ調節剤としての新規な置換インドール誘導体
MX355164B (es) 2012-05-16 2018-04-06 Janssen Pharmaceuticals Inc Derivados de 3,4-dihidro-2h-pirido[1,2-a]pirazin-1,6-diona sustituidos utiles para el tratamiento de la enfermedad de alzheimer (inter alia).
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
KR102209418B1 (ko) 2012-12-20 2021-01-29 얀센 파마슈티카 엔.브이. 감마 세크레타제 조절 인자로서의 신규 삼환 3,4-디하이드로-2H-피리도[1,2-α]피라진-1,6-디온 유도체
CN104936958B (zh) 2013-01-17 2019-07-26 詹森药业有限公司 作为γ分泌酶调节剂的新颖的经取代的吡啶并-哌嗪酮衍生物
CN103664819A (zh) * 2013-12-16 2014-03-26 山东汇海医药化工有限公司 一种2-氨基-4-甲基噻唑-5-甲酸乙酯的制备方法
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
CN107406445B (zh) 2015-02-03 2019-12-24 辉瑞公司 新颖环丙苯并呋喃基吡啶并吡嗪二酮类
JP2019512491A (ja) * 2016-03-11 2019-05-16 エーシー・イミューン・エス・アー 診断及び療法のための二環式化合物
EP3523304B1 (en) * 2016-10-04 2021-01-27 H. Hoffnabb-La Roche Ag Bicyclic heteroaryl derivatives
CN110194764B (zh) * 2018-02-26 2022-08-16 云南大学 酰胺类化合物、其制备方法及用途
CR20210104A (es) 2018-09-03 2021-04-19 Hoffmann La Roche Derivados de heteroarilo bicíclicos
PT3894411T (pt) 2018-12-13 2024-08-08 Hoffmann La Roche Derivados da 7-fenoxi-n-(3-azabiciclo[3.2.1]octan-8-il)-6,7-dihidro-5h-pirrolo[1,2-b][1,2,4]triazol-2-amina e compostos relacionados enquanto moduladores da gama-secretase para o tratamento da doença de alzheimer
CN114222732B (zh) * 2019-10-28 2023-04-04 南京明德新药研发有限公司 一种尿酸促排剂及其合成方法和其在医药上的应用

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2256968T3 (es) * 1997-10-27 2006-07-16 Agouron Pharmaceuticals, Inc. Derivados de 4-aminotiazol, su preparacion y su uso como inhibidores de quinasas dependientes de ciclina.
ATE288904T1 (de) * 1998-06-18 2005-02-15 Bristol Myers Squibb Co Durch kohlenstoff substituierte aminothiazole als inhibitoren von zyclin-abhägigen kinasen
US20030176454A1 (en) * 2000-05-15 2003-09-18 Akira Yamada N-coating heterocyclic compounds
CA2525547C (en) * 2003-05-14 2012-07-03 Torreypines Therapeutics, Inc. Compounds and uses thereof in modulating amyloid beta
MY149038A (en) 2004-05-26 2013-07-15 Eisai R&D Man Co Ltd Cinnamide compound
US20080125432A1 (en) * 2004-12-01 2008-05-29 Devgen Nv 5-Carboxamido Substituted Thiazole Derivatives that Interact With Ion Channels, In Particular With Ion Channels From the Kv Family
US20060241038A1 (en) 2005-04-20 2006-10-26 Eisai Co., Ltd. Therapeutic agent for Abeta related disorders
US20090048448A1 (en) 2005-11-18 2009-02-19 Ikuo Kushida Salts of cynnamide compound or solvates thereof
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
US20070117839A1 (en) 2005-11-24 2007-05-24 Eisai R&D Management Co., Ltd. Two cyclic cinnamide compound
JP5221144B2 (ja) 2005-11-24 2013-06-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 モルホリンタイプ・シンナミド化合物
EP1992618B1 (en) 2006-03-09 2012-01-18 Eisai R&D Management Co., Ltd. Polycyclic cinnamide derivative
TWI378091B (en) 2006-03-09 2012-12-01 Eisai R&D Man Co Ltd Multi-cyclic cinnamide derivatives

Also Published As

Publication number Publication date
AU2008250436A1 (en) 2008-11-20
RU2009140182A (ru) 2011-06-20
AR066509A1 (es) 2009-08-26
TW200904420A (en) 2009-02-01
IL201566A0 (en) 2010-05-31
EP2155740A1 (en) 2010-02-24
KR20100008791A (ko) 2010-01-26
ZA200907585B (en) 2010-07-28
MX2009012163A (es) 2009-12-01
EP2155740B1 (en) 2011-01-26
AU2008250436B2 (en) 2013-03-28
CN101675045A (zh) 2010-03-17
JP2010526847A (ja) 2010-08-05
CA2686754A1 (en) 2008-11-20
WO2008138753A1 (en) 2008-11-20
ATE496915T1 (de) 2011-02-15
US20080280948A1 (en) 2008-11-13
DE602008004769D1 (en) 2011-03-10
US7910740B2 (en) 2011-03-22
KR101138045B1 (ko) 2012-04-24
BRPI0811993A2 (pt) 2014-11-18
CL2008001347A1 (es) 2009-05-29
JP5264890B2 (ja) 2013-08-14
CN101675045B (zh) 2012-11-28
IL201566A (en) 2013-08-29
ES2358863T3 (es) 2011-05-16
CA2686754C (en) 2014-10-28

Similar Documents

Publication Publication Date Title
PE20090248A1 (es) Moduladores de beta-amiloide
PE20091734A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PE20071094A1 (es) Derivados 1-ortoflurofenil sustituidos 1,2,5-tiadiazolidindionas como inhibidores de ptpasa
PE20091376A1 (es) Derivados de fenilamino como moduladores de beta-amiloide
PE20120505A1 (es) Derivados de 1-heterociclil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona como moduladores de pde9a
PE20091472A1 (es) Moduladores de beta-amiloide
PE20091173A1 (es) Derivados de heteroarilo como antagonistas de receptor de orexina
PE20110028A1 (es) Derivados de isoxazol y su uso como potenciadores de los receptores metabotropicos de glutamato
PE20091756A1 (es) Derivados de pirazolopirimidinona como moduladores de la pde9a
PE20110409A1 (es) Compuestos heterociclicos antiviricos
PE20091211A1 (es) Derivados de pirazolopirimidina como moduladores de pde9a
PE20121182A1 (es) Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina
PE20081377A1 (es) Compuestos de tiazol pirazolopirimidina
ECSP10010599A (es) Derivados de tienopiridonas como activadores de proteina quinasa activados por amp (ampk)
PE20080772A1 (es) Nuevos derivados de bipiridina sustituidos y su uso
PE20091080A1 (es) 2-[3-(2,2-difluoro-benzo[1,3]dioxol-5-ilamino)-5-(2,6-dimetil-piridin-4-il)-[1,2,4]triazol-1-il]-n-etil-acetamida y sus sales como moduladores de los receptores nicotinicos alfa 7
PE20070136A1 (es) COMPUESTOS DERIVADOS DE N-(PIRIDIN-2-IL)-SULFONAMIDA COMO INHIBIDORES DE LA ENZIMA 11-beta-HIDROXIESTEROIDE DESHIDROGENASA HUMANA TIPO 1
PE20130602A1 (es) Derivados de 6-cicloalquil-1,5-dihidro-pirazolo(3,4-d)pirimidin-4-onas y su uso como inhibidores de pde9a
ECSP088638A (es) Bencensulfonil-cromano, tiocromano, tetrahidronaftaleno e inhibidores de gamma secretasa relacionados
PE20080130A1 (es) Benzoimidazol-2-il pirimidinas y pirazinas como moduladores del receptor h4 de histamina
PE20081776A1 (es) Moduladores 2-aminopirimidina del receptor histamina h4
PE20140703A1 (es) Derivados de heteroarilo como moduladores de nachr alfa 7
DE602006006850D1 (de) Als modulatoren von dopamin-d3-rezeptoren geeignete azabicyclo-(3,1,0)-hexan-derivate
PE20110773A1 (es) Tetrahidropiran espiro pirrolidinona y piperidinona sustituidas, y su preparacion
PE20110777A1 (es) Nuevas lactamas como inhibidores de beta secretasa

Legal Events

Date Code Title Description
FC Refusal