AR075366A1 - Compuestos heterociclicos biciclicos sustituidos como modulares de la gamma secretasa - Google Patents

Compuestos heterociclicos biciclicos sustituidos como modulares de la gamma secretasa

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Publication number
AR075366A1
AR075366A1 ARP100100325A ARP100100325A AR075366A1 AR 075366 A1 AR075366 A1 AR 075366A1 AR P100100325 A ARP100100325 A AR P100100325A AR P100100325 A ARP100100325 A AR P100100325A AR 075366 A1 AR075366 A1 AR 075366A1
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AR
Argentina
Prior art keywords
alkyl
halo
substituents
optionally substituted
cycloalkyl
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Application number
ARP100100325A
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English (en)
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Ortho Mcneil Janssen Pharm
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Application filed by Ortho Mcneil Janssen Pharm filed Critical Ortho Mcneil Janssen Pharm
Publication of AR075366A1 publication Critical patent/AR075366A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • C07D403/10—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 carbon chain containing aromatic 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
    • 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
    • C07D413/10—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 carbon chain containing aromatic 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

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

Abstract

Los compuestos segun la presente resultan de utilidad como moduladores de la gamma secreta. También se refiere a los procedimientos para elaborar tales compuestos, a composiciones farmacéuticas que comprenden dichos compuestos a modo de ingrediente activo, así como al uso de dichos compuestos como medicamento. Reivindicacion 1: Un compuesto de la formula (1) o una forma estereoisomérica de éste, donde Het1 es un heterociclo aromático de 5 o 6 miembros que tiene la formula (2), (3), (4), (5) o (6); R0 es H o alquilo C1-4; R1 es H, alquilo C1-4 o alquil C1-4-oxialquilo C1-4; R2 es alquilo C1-4; X es O o S; G1 es CH o N; G2 es CH, N o C sustituido con alquilo C1-4; siempre que G1 y G2 no sean simultáneamente N; G3 es CH o N; R10a y R10b son, cada uno de manera independiente, hidrogeno o alquilo C1-4; A1 es CR3 o N; donde R3 es H, halo o alquil C1-4oxi; cada uno de A2, A3 y A4 es, de manera independiente, CH, CF o N; siempre que un máximo de dos de A1, A2, A3 y A4 sean N; Het2 es un heterociclo aromático bicíclico de 9 miembros que tiene la formula (7) o (8); Z1 es CH o N; Z2 es CR4a o N; Z3 es CH o N; siempre que como máximo uno de Z1, Z2 y Z3 sea N; Y1 es CH o N; Y2 es CR4b o N; Y3 es CH o N; siempre que como máximo uno de Y1, Y2 e Y3 sea N; R4a es H; halo; alquil C1-4oxi; ciano; cicloalquilo C3-7; alquil C1-4carbonilo; alquil C1-4oxicarbonilo o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en halo y amino; R4b es H; halo; alquil C1-4oxi; ciano; cicloalquilo C3-7 o alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en halo y amino; R5 es H; halo; ciano; alquil C1-4oxi; alquenilo C2-6 o alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en alquil C1-4oxi y halo; R6a es alquilo C2-6 sustituido con uno o más sustituyentes de halo; alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en piperidinilo, Ar, alquil C1-6oxi, tetrahidropiranilo, cicloalquil C3-7oxi y cicloalquilo C3-7; cicloalquilo C3-7; alquil C1-4carbonilo; tetrahidropiranilo; Ar; R8R9N-carbonilo o CH2-O-Ar; R6b es alquilo C2-6 sustituido con uno o más sustituyentes de halo; alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en piperidinilo, Ar, alquil C1-6oxi, tetrahidropiranilo, cicloalquil C3-7oxi y cicloalquilo C3-7; cicloalquilo C3-7; cicloalquilo C3-7 sustituido con uno o más sustituyentes de fenilo opcionalmente sustituido con uno o más sustituyentes de halo; piperidinilo; morfolinilo; pirrolidinilo; NR8R9 tetrahidropiranilo; O-Ar; alquil C1-6oxi; alquil C1-6tio; Ar; CH2-O-Ar; S-Ar; NCH3-Ar o NH-Ar; donde cada piperidinilo, morfolinilo y pirrolidinilo puede estar opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en alquilo C1-4, alquenilo C2-6, alquil C1-4carbonílo, halo, y alquil C1-4oxicarbonilo; donde cada Ar es, de manera independiente, fenilo opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en halo, alquil C1-4oxi, ciano, NR8R9, morfolinilo, alquilo C1-4 y alquilo C1-4 sustituido con uno o más sustituyentes de halo; piridinilo opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en halo, alquil C1-4oxi, ciano, alquilo C1-4 y alquilo C1-4 sustituido con uno o más sustituyentes de halo; oxazolilo opcionalmente sustituido con uno o más sustituyentes de alquilo C1-4; o tienilo opcionalmente sustituido con uno o más sustituyentes de halo; cada R8 es, de manera independiente, H o alquilo C1-4; cada R9 es, de manera independiente, H o alquilo C1-4; R7 es H, alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes, cada uno de los cuales se selecciona -de manera independiente- del grupo que consiste en halo, fenilo, y alquil C1-4oxi; o una sal de adicion farmacéuticamente aceptable o solvato de aquél.
ARP100100325A 2009-02-06 2010-02-05 Compuestos heterociclicos biciclicos sustituidos como modulares de la gamma secretasa AR075366A1 (es)

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EP (1) EP2393804B1 (es)
JP (1) JP5576403B2 (es)
KR (1) KR20110113197A (es)
CN (1) CN102325765B (es)
AP (1) AP2011005779A0 (es)
AR (1) AR075366A1 (es)
AU (1) AU2010211109B2 (es)
BR (1) BRPI1008473A2 (es)
CA (1) CA2748862A1 (es)
EA (1) EA019685B1 (es)
ES (1) ES2481715T3 (es)
IL (1) IL214425A (es)
MX (1) MX2011008335A (es)
NZ (1) NZ593951A (es)
SG (1) SG173510A1 (es)
TW (1) TWI496780B (es)
UA (1) UA106360C2 (es)
WO (1) WO2010089292A1 (es)
ZA (1) ZA201105788B (es)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009308675A1 (en) 2008-10-31 2010-05-06 Genentech, Inc. Pyrazolopyrimidine JAK inhibitor compounds and methods
EP2367826A4 (en) 2008-11-06 2012-07-04 Astrazeneca Ab MODULATORS OF THE PROTEIN -AMYLOID
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
MX2011008335A (es) 2009-02-06 2011-09-06 Ortho Mcneil Janssen Pharm Novedosos compuestos heterociclicos biciclicos sustituidos como moduladores de la 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
WO2010145883A1 (en) 2009-05-07 2010-12-23 Ortho-Mcneil-Janssen Pharmaceuticals, Inc Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
CA2778517A1 (en) 2009-07-15 2011-01-20 Janssen Pharmaceuticals, Inc. Substituted triazole and imidazole derivatives as gamma secretase modulators
KR20120123677A (ko) 2010-01-15 2012-11-09 얀센 파마슈티칼즈, 인코포레이티드 감마 세크레타제 조절제로서의 신규 치환된 비사이클릭 트리아졸 유도체
JP2013522267A (ja) * 2010-03-17 2013-06-13 エフ．ホフマン−ラ ロシュ アーゲー イミダゾピリジン化合物、組成物、および使用法
US8697708B2 (en) 2010-09-15 2014-04-15 F. Hoffmann-La Roche Ag Azabenzothiazole compounds, compositions and methods of use
EP2640722B1 (en) 2010-11-19 2015-11-04 F.Hoffmann-La Roche Ag Pyrazolopyridines and their use as tyk2 inhibitors
BR112013023984A2 (pt) 2011-03-24 2016-09-13 Cellzome Ltd derivados triazolil piperazina e triazolil piperidina substituidos como moduladores de gama secretase
EP2691393B1 (en) 2011-03-31 2016-09-14 Pfizer Inc Novel bicyclic pyridinones
TWI567079B (zh) 2011-07-15 2017-01-21 健生醫藥公司 作為伽瑪分泌酶調節劑之新穎的經取代的吲哚衍生物
ES2627347T3 (es) 2011-10-20 2017-07-27 Glaxosmithkline Llc Aza-heterociclos bicíclicos sustituidos y análogos como moduladores de sirtuina
BR112014009348A2 (pt) 2011-10-20 2017-04-18 Glaxosmithkline Llc aza-heterociclos substituídos bicíclicos e análogos como moduladores de sirtuina
RU2630677C2 (ru) 2011-12-21 2017-09-12 Оно Фармасьютикал Ко., Лтд. Соединения
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).
FR2993564B1 (fr) 2012-07-20 2014-08-22 Metabrain Res Derives d'imidazopyridine utiles dans le traitement du diabete
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
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
JP6283691B2 (ja) 2013-01-17 2018-02-21 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置換ピリド−ピペラジノン誘導体
EP2958919B1 (en) 2013-02-21 2019-05-22 Boehringer Ingelheim International GmbH Dihydropteridinones i
EP2958918B1 (en) 2013-02-21 2016-12-07 Boehringer Ingelheim International GmbH Dihydropteridinones ii
EP2818472A1 (en) * 2013-06-27 2014-12-31 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Imidazo[4,5-c]pyridine and pyrrolo[3,2-c]pyridine compounds as G-protein-coupled receptor kinase 5 (GRK5) 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
EP3134405B1 (en) 2014-04-25 2019-08-28 Pfizer Inc Heteroaromatic compounds and their use as dopamine d1 ligands
EP3137454A1 (en) 2014-04-28 2017-03-08 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
SG11201609830RA (en) 2014-05-23 2016-12-29 Hoffmann La Roche 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds which are jak inhibitors
ES2818806T3 (es) 2015-02-03 2021-04-14 Pfizer Novedosas ciclopropabenzofuranil piridopirazindionas
HUE054118T2 (hu) 2016-06-16 2021-08-30 Janssen Pharmaceutica Nv Biciklusos piridin-, pirazin- és pirimidin-származékok mint PI3K béta-inhibitorok
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
JP6683830B2 (ja) 2016-11-01 2020-04-22 日本農薬株式会社 オキシム基を有するキノリン化合物、ｎ‐オキサイド又はその塩類及び該化合物を含有する農園芸用殺虫剤並びにその使用方法
WO2018215389A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
CN108440509B (zh) * 2018-04-23 2021-03-02 山西大同大学 一种阿托伐他汀钙中间体制备的方法

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5767144A (en) 1994-08-19 1998-06-16 Abbott Laboratories Endothelin antagonists
WO1997003067A1 (en) 1995-07-13 1997-01-30 Knoll Aktiengesellschaft Piperazine derivatives as therapeutic agents
PT1192131E (pt) 1999-06-10 2004-11-30 Warner Lambert Co Metodo para inibicao da agergacao de proteinas amiloides e para visualizar depositos amiloides utilizando derivados de isoindolina
EP1284729A4 (en) 2000-04-13 2007-12-19 Mayo Foundation REDUCTION AGENTS OF A (BETA) 42
US20030176454A1 (en) 2000-05-15 2003-09-18 Akira Yamada N-coating heterocyclic compounds
DE10109867A1 (de) 2001-03-01 2002-09-05 Abbott Gmbh & Co Kg Verwendung von Triazolverbindungen zur Prophylaxe und Therapie neurodegenerativer Erkrankungen, Hirntrauma und zerebraler Ischämie
DE10238002A1 (de) 2002-08-20 2004-03-04 Merck Patent Gmbh Benzimidazolderivate
BRPI0407913A (pt) 2003-02-27 2006-03-01 Hoffmann La Roche antagonistas receptores de ccr-3
EP1628666B1 (en) 2003-05-14 2015-09-23 NeuroGenetic Pharmaceuticals, Inc. Compouds and uses thereof in modulating amyloid beta
CN1787822A (zh) * 2003-05-14 2006-06-14 托里派因斯疗法公司 化合物及其在调节淀粉样蛋白β中的用途
BRPI0413540A (pt) 2003-08-14 2006-10-10 Hoffmann La Roche moduladores gabanérgicos
US7884112B2 (en) 2004-03-08 2011-02-08 Stuart Edward Bradley Pyrrolopyridine-2-carboxylic acid hydrazides
US7667041B2 (en) 2004-05-26 2010-02-23 Eisai R&D Management Co., Ltd. Cinnamide compound
SA05260149B1 (ar) * 2004-05-26 2010-06-16 إيساي آر آند دي منجمنت كو.، ليمتد مركب سيناميد
WO2006046575A1 (ja) 2004-10-26 2006-05-04 Eisai R & D Management Co., Ltd. シンナミド化合物の非晶質体
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
US20070078136A1 (en) * 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
CA2623317A1 (en) 2005-09-22 2007-03-29 Sanofi-Aventis Amino-alkyl-amide derivatives as ccr3 receptor liquids
WO2007043786A1 (en) 2005-10-10 2007-04-19 Seiyang Yang Dynamic-based verification apparatus for verification from electronic system level to gate level, and verification method using the same
EP1937767B1 (en) 2005-10-11 2013-05-22 Chemtura Corporation Diaromatic amines
WO2007105053A2 (en) 2006-03-13 2007-09-20 Pfizer Products Inc. Tetralines antagonists of the h-3 receptor
GB0606774D0 (en) 2006-04-03 2006-05-10 Novartis Ag Organic compounds
US7893058B2 (en) 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
EP2099798A1 (en) 2006-12-01 2009-09-16 Galapagos N.V. Imidazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases
JP2010512390A (ja) 2006-12-12 2010-04-22 シェーリング コーポレイション 三環式系を含むアスパルチルプロテアーゼ阻害剤
JP2010513495A (ja) 2006-12-20 2010-04-30 シェーリング コーポレイション 新規なｊｎｋ阻害剤
US8183276B2 (en) 2007-02-08 2012-05-22 Christian Fischer Therapeutic agents
US8252803B2 (en) 2007-02-12 2012-08-28 Merck Sharp & Dohme Corp. Piperidine derivatives
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
WO2008137139A1 (en) 2007-05-07 2008-11-13 Schering Corporation Gamma secretase modulators
BRPI0811993A2 (pt) 2007-05-11 2014-11-18 Hoffmann La Roche " hetarilanilinas como moduladores para beta-amiloide ".
US8242150B2 (en) 2007-06-13 2012-08-14 Merck Sharp & Dohme Corp. Triazole derivatives for treating alzheimer'S disease and related conditions
JP2010532354A (ja) 2007-06-29 2010-10-07 シェーリング コーポレイション γセクレターゼモジュレーター
US7935815B2 (en) 2007-08-31 2011-05-03 Eisai R&D Management Co., Ltd. Imidazoyl pyridine compounds and salts thereof
MX2010002674A (es) 2007-09-06 2010-03-25 Schering Corp Moduladores de gamma secretasa.
GB0720444D0 (en) 2007-10-18 2007-11-28 Glaxo Group Ltd Novel compounds
AU2008333865A1 (en) 2007-12-06 2009-06-11 Schering Corporation Gamma secretase modulators
WO2009076352A1 (en) 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
EP2257541B1 (en) 2008-02-22 2013-08-14 F. Hoffmann-La Roche AG Modulators for amyloid beta
US20100137320A1 (en) 2008-02-29 2010-06-03 Schering Corporation Gamma secretase modulators
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
WO2010054078A1 (en) 2008-11-06 2010-05-14 Schering Corporation Gamma secretase modulators
BRPI0921348A2 (pt) 2008-11-10 2019-09-24 Hoffmann La Roche moduladores heterocíclicos da gama secretase
EP2367817A4 (en) 2008-12-03 2012-05-09 Via Pharmaceuticals Inc INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE ENZYME
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
MX2011008335A (es) 2009-02-06 2011-09-06 Ortho Mcneil Janssen Pharm Novedosos compuestos heterociclicos biciclicos sustituidos como moduladores de la 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
US8754100B2 (en) 2009-02-26 2014-06-17 Eisai R&D Management Co., Ltd. Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors
JP2012051806A (ja) 2009-02-26 2012-03-15 Eisai R & D Management Co Ltd イミダゾリルピラジン誘導体
JP2012051807A (ja) 2009-02-26 2012-03-15 Eisai R & D Management Co Ltd アリールイミダゾール化合物
CA2751534A1 (en) 2009-03-03 2010-09-10 Pfizer Inc. Novel phenyl imidazoles and phenyl triazoles as gamma-secretase modulators
US20110299830A1 (en) 2009-03-16 2011-12-08 Panasonic Corporation Application running device
WO2010126745A1 (en) 2009-04-27 2010-11-04 High Point Pharmaceuticals, Llc SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS β-SECRETASE INHIBITORS
WO2010145883A1 (en) 2009-05-07 2010-12-23 Ortho-Mcneil-Janssen Pharmaceuticals, Inc Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators
JP2010274429A (ja) 2009-05-26 2010-12-09 Ihi Corp アライメントステージ
CA2778517A1 (en) 2009-07-15 2011-01-20 Janssen Pharmaceuticals, Inc. Substituted triazole and imidazole derivatives as gamma secretase modulators
KR20120123677A (ko) 2010-01-15 2012-11-09 얀센 파마슈티칼즈, 인코포레이티드 감마 세크레타제 조절제로서의 신규 치환된 비사이클릭 트리아졸 유도체
BR112013023984A2 (pt) 2011-03-24 2016-09-13 Cellzome Ltd derivados triazolil piperazina e triazolil piperidina substituidos como moduladores de gama secretase
EP2691393B1 (en) 2011-03-31 2016-09-14 Pfizer Inc Novel bicyclic pyridinones
TWI567079B (zh) 2011-07-15 2017-01-21 健生醫藥公司 作為伽瑪分泌酶調節劑之新穎的經取代的吲哚衍生物

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