BR112016022519A8 - cromeno e 1,1a,2,7b-tetra-hidrociclopropa[c]cromeno piridopirazinadionas como moduladores de gama-secretase - Google Patents

cromeno e 1,1a,2,7b-tetra-hidrociclopropa[c]cromeno piridopirazinadionas como moduladores de gama-secretase Download PDF

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Publication number
BR112016022519A8
BR112016022519A8 BR112016022519A BR112016022519A BR112016022519A8 BR 112016022519 A8 BR112016022519 A8 BR 112016022519A8 BR 112016022519 A BR112016022519 A BR 112016022519A BR 112016022519 A BR112016022519 A BR 112016022519A BR 112016022519 A8 BR112016022519 A8 BR 112016022519A8
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BR
Brazil
Prior art keywords
chromene
compounds
pyridopyrazinedione
tetrahydrocyclopropa
secretase modulators
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BR112016022519A
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English (en)
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BR112016022519A2 (pt
Inventor
Friederike Stepan Antonia
William; Am Ende Christopher
Antonia Rankic Danica
Scott Johnson Douglas
Wayne Kauffman Gregory
Michael Humphrey John
Youngjin Pettersson Martin
Robert Verhoest Patrick
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Pfizer
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Application filed by Pfizer filed Critical Pfizer
Publication of BR112016022519A2 publication Critical patent/BR112016022519A2/pt
Publication of BR112016022519A8 publication Critical patent/BR112016022519A8/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

Abstract

a presente invenção refere-se a compostos e sais farmaceuticamente aceitáveis dos compostos, em que os compostos têm a estrutura de fórmula (i) em que x, r1, r2a, r2b, r4a, r4b, r5a, r5b, r6, r7, y e z são como definidos no relatório descritivo. composições farmacêuticas correspondentes, métodos de tratamento, métodos de síntese e intermediários também são divulgados. estes compostos são moduladores da ¿-secretase, úteis para o tratamento de distúrbios neurodegenerativos e/ou neurológicos, tais como a doença de alzheimer e a síndrome de down.
BR112016022519A 2014-04-01 2015-03-18 cromeno e 1,1a,2,7b-tetra-hidrociclopropa[c]cromeno piridopirazinadionas como moduladores de gama-secretase BR112016022519A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461973436P 2014-04-01 2014-04-01
PCT/IB2015/051988 WO2015150957A1 (en) 2014-04-01 2015-03-18 Chromene and 1,1 a,2,7b-tetrahydrocyclopropa[c]chromene pyridopyrazinediones as gamma-secretase modulators

Publications (2)

Publication Number Publication Date
BR112016022519A2 BR112016022519A2 (pt) 2017-08-15
BR112016022519A8 true BR112016022519A8 (pt) 2018-03-06

Family

ID=52815058

Family Applications (1)

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BR112016022519A BR112016022519A8 (pt) 2014-04-01 2015-03-18 cromeno e 1,1a,2,7b-tetra-hidrociclopropa[c]cromeno piridopirazinadionas como moduladores de gama-secretase

Country Status (30)

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US (2) US20150274721A1 (pt)
EP (1) EP3126361B1 (pt)
JP (1) JP6643247B2 (pt)
KR (1) KR101886945B1 (pt)
CN (1) CN106211770B (pt)
AP (1) AP2016009465A0 (pt)
AR (1) AR099874A1 (pt)
AU (1) AU2015242330B2 (pt)
BR (1) BR112016022519A8 (pt)
CA (1) CA2944308A1 (pt)
CL (1) CL2016002422A1 (pt)
CR (1) CR20160454A (pt)
CU (1) CU20160140A7 (pt)
DK (1) DK3126361T3 (pt)
DO (1) DOP2016000266A (pt)
EA (1) EA031419B1 (pt)
EC (1) ECSP16078289A (pt)
ES (1) ES2759277T3 (pt)
HK (1) HK1231481A1 (pt)
IL (1) IL248154B (pt)
MD (1) MD20160102A2 (pt)
MX (1) MX369074B (pt)
NI (1) NI201600149A (pt)
PE (1) PE20161364A1 (pt)
PH (1) PH12016501864A1 (pt)
SG (1) SG11201607465UA (pt)
TW (1) TWI568733B (pt)
UY (1) UY36054A (pt)
WO (1) WO2015150957A1 (pt)
ZA (1) ZA201606252B (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
AU2016214102B2 (en) * 2015-02-03 2018-09-27 Pfizer Inc. Novel cyclopropabenzofuranyl pyridopyrazinediones
CN106580997B (zh) * 2016-12-09 2018-01-19 张田 一种治疗先兆流产的药物组合物
CA3047096A1 (en) 2016-12-16 2018-06-21 Pipeline Therapeutics, Inc. Methods of treating cochlear synaptopathy
CA3112326A1 (en) * 2018-09-12 2020-03-19 Novartis Ag Antiviral pyridopyrazinedione compounds
CN110907542A (zh) * 2018-09-17 2020-03-24 复旦大学 一种液质联用检测唾液中司来吉兰及其代谢物的方法
TW202100526A (zh) 2019-03-06 2021-01-01 日商第一三共股份有限公司 吡咯并吡唑衍生物
JP7417715B2 (ja) 2019-09-26 2024-01-18 ノバルティス アーゲー 抗ウイルスピラゾロピリジノン化合物

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5750349A (en) 1993-01-25 1998-05-12 Takeda Chemical Industries Ltd. Antibodies to β-amyloids or their derivatives and use thereof
DE19709877A1 (de) 1997-03-11 1998-09-17 Bayer Ag 1,5-Dihydro-pyrazolo[3,4-d]-pyrimidinon-derivate
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
PT994728E (pt) 1997-04-09 2008-11-11 Intellect Neurosciences Inc Anticorpos recombinantes específicos contra terminações beta-amilóide, codificação por adn e métodos de utilização destes
GB9722520D0 (en) 1997-10-24 1997-12-24 Pfizer Ltd Compounds
US6905686B1 (en) 1997-12-02 2005-06-14 Neuralab Limited Active immunization for treatment of alzheimer's disease
TWI239847B (en) 1997-12-02 2005-09-21 Elan Pharm Inc N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease
EP1257584B2 (en) 2000-02-24 2013-03-06 Washington University St. Louis Humanized antibodies that sequester amyloid beta peptide
DE10045112A1 (de) 2000-09-11 2002-03-21 Merck Patent Gmbh Verwendung von Indolderivaten zur Behandlung von Erkrankungen des zentralen Nervensystems
AU3976402A (en) 2000-11-03 2002-06-03 Proteotech Inc Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from uncaria tomentosa and related plants
WO2003016466A2 (en) 2001-08-17 2003-02-27 Eli Lilly And Company ANTI-Aβ ANTIBODIES
US20030195205A1 (en) 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
AU2003221500B9 (en) * 2002-02-28 2008-11-20 Mitsubishi Pharma Corporation Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl -6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
DE10238723A1 (de) 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
DE10238724A1 (de) 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
KR20050071564A (ko) 2002-10-09 2005-07-07 리나트 뉴로사이언스 코퍼레이션 아밀로이드 베타 펩티드에 대한 항체를 사용하여알츠하이머병을 치료하는 방법 및 그의 조성물
US20040220186A1 (en) 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
EP1638935A1 (en) 2003-06-19 2006-03-29 Pfizer Products Inc. Nk1 antagonist
CA2538220A1 (en) 2003-09-09 2005-03-24 Takeda Pharmaceutical Company Limited Use of antibody
GB0327319D0 (en) 2003-11-24 2003-12-24 Pfizer Ltd Novel pharmaceuticals
EP1720847A1 (en) 2004-02-02 2006-11-15 Pfizer Products Incorporated Histamine-3 receptor modulators
US7456164B2 (en) 2004-05-07 2008-11-25 Pfizer, Inc 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands
EP1595881A1 (en) 2004-05-12 2005-11-16 Pfizer Limited Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
US7927594B2 (en) 2004-07-30 2011-04-19 Rinat Neuroscience Corp. Antibodies directed against amyloid-beta peptide
GB0423356D0 (en) 2004-10-21 2004-11-24 Merck Sharp & Dohme Therapeutic agents
US20090074775A1 (en) 2004-12-22 2009-03-19 David Michael Holtzman Use Of Anti-AB Antibody To Treat Traumatic Brain Injury
UY29504A1 (es) 2005-04-29 2006-10-31 Rinat Neuroscience Corp Anticuerpos dirigidos contra el péptido amiloide beta y métodos que utilizan los mismos.
PL1881985T3 (pl) 2005-05-12 2011-05-31 Pfizer Bezwodne krystaliczne postacie N-[1-(2-etoksyetylo)-5-(N-etylo-N-metyloamino)-7-(4-metylopirydyn-2-yloamino)-1H-pirazolo[4,3-d]pirymidyno-3-karbonylo]metano-sulfonoamidu
CA2608672A1 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridine [3,4-b] pyrazinones as pde-5 inhibitors
WO2006126083A1 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridine [3 , 4-b] pyrazinone compounds as pde-5 inhibitors
CA2603830A1 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Co Llc PYRIDINE [2,3-B] PYRAZINONES
CA2607499C (en) 2005-06-22 2010-11-30 Pfizer Products Inc. Histamine-3 receptor antagonists
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
WO2007052124A1 (en) 2005-11-04 2007-05-10 Pfizer Limited Tetrahydronaphthyridine derivative
WO2007063385A2 (en) 2005-12-01 2007-06-07 Pfizer Products Inc. Spirocyclic amine histamine-3 receptor antagonists
WO2007069053A1 (en) 2005-12-14 2007-06-21 Pfizer Products Inc. Benzimidazole antagonists of the h-3 receptor
WO2007088462A1 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Spirochromane antagonists of the h-3 receptor
WO2007088450A2 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Chromane antagonist of the h-3 receptor
WO2007099423A1 (en) 2006-03-02 2007-09-07 Pfizer Products Inc. 1-pyrrolidine indane derivatives as histamine-3 receptor antagonists
WO2007105053A2 (en) 2006-03-13 2007-09-20 Pfizer Products Inc. Tetralines antagonists of the h-3 receptor
AU2007242555B2 (en) 2006-04-21 2010-12-16 Pfizer Products Inc. Pyridine[3,4-b]pyrazinones
WO2007138431A2 (en) 2006-05-30 2007-12-06 Pfizer Products Inc. Azabicyclic ether histamine-3 antagonists
DK2124933T3 (da) 2007-01-22 2012-11-19 Pfizer Prod Inc Tosylatsalt af en terapeutisk forbindelse og farmaceutiske sammensætninger deraf
EP2355659A4 (en) * 2008-10-23 2012-10-10 Merck Sharp & Dohme M1 RECEPTOR MODULATORS CONCEALED HETEROCYCLIC POSITIVE ALLOSTERIC
WO2012131539A1 (en) * 2011-03-31 2012-10-04 Pfizer Inc. Novel bicyclic pyridinones
KR102096625B1 (ko) * 2012-05-16 2020-04-03 얀센 파마슈티칼즈, 인코포레이티드 (무엇보다도) 알츠하이머병의 치료에 유용한 치환 3,4-디하이드로-2h-피리도[1,2-a]피라진-1,6-디온 유도체
UA110688C2 (uk) * 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
CA2891755C (en) * 2013-01-17 2021-10-26 Janssen Pharmaceutica Nv Substituted pyrido-piperazinone derivatives as gamma secretase modulators
CA2925743C (en) * 2013-10-04 2018-03-06 Pfizer Inc. Novel bicyclic pyridinones as gamma-secretase modulators

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CR20160454A (es) 2016-12-06
AR099874A1 (es) 2016-08-24
AU2015242330A1 (en) 2016-09-22
MX369074B (es) 2019-10-28
EP3126361B1 (en) 2019-11-06
PH12016501864A1 (en) 2016-12-19
WO2015150957A1 (en) 2015-10-08
ECSP16078289A (es) 2017-02-24
UY36054A (es) 2015-10-30
KR101886945B1 (ko) 2018-08-08
MD20160102A2 (ro) 2017-04-30
CA2944308A1 (en) 2015-10-08
AP2016009465A0 (en) 2016-09-30
EA201600619A1 (ru) 2017-03-31
CU20160140A7 (es) 2017-02-02
PE20161364A1 (es) 2016-12-25
IL248154A0 (en) 2016-11-30
AU2015242330B2 (en) 2017-08-17
DOP2016000266A (es) 2016-11-15
CN106211770A (zh) 2016-12-07
TW201540716A (zh) 2015-11-01
IL248154B (en) 2020-09-30
US20170166566A1 (en) 2017-06-15
EP3126361A1 (en) 2017-02-08
ES2759277T3 (es) 2020-05-08
KR20160137635A (ko) 2016-11-30
ZA201606252B (en) 2018-05-30
DK3126361T3 (da) 2020-01-02
US20150274721A1 (en) 2015-10-01
CL2016002422A1 (es) 2017-02-03
SG11201607465UA (en) 2016-10-28
JP2017512803A (ja) 2017-05-25
JP6643247B2 (ja) 2020-02-12
TWI568733B (zh) 2017-02-01
NI201600149A (es) 2016-11-18
MX2016012904A (es) 2016-12-07
BR112016022519A2 (pt) 2017-08-15
EA031419B1 (ru) 2018-12-28
HK1231481A1 (zh) 2017-12-22
CN106211770B (zh) 2018-02-06

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