PE20110777A1 - Nuevas lactamas como inhibidores de beta secretasa - Google Patents

Nuevas lactamas como inhibidores de beta secretasa

Info

Publication number
PE20110777A1
PE20110777A1 PE2011001066A PE2011001066A PE20110777A1 PE 20110777 A1 PE20110777 A1 PE 20110777A1 PE 2011001066 A PE2011001066 A PE 2011001066A PE 2011001066 A PE2011001066 A PE 2011001066A PE 20110777 A1 PE20110777 A1 PE 20110777A1
Authority
PE
Peru
Prior art keywords
cycloalkyl
alkyl
halogen
secretase inhibitors
compounds
Prior art date
Application number
PE2011001066A
Other languages
English (en)
Inventor
Michael Aaron Brodney
Ivan Viktorovich Efremov
Christopher John Helal
Brian Thomas O'neill
Original Assignee
Pfizer
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41481076&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20110777(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of PE20110777A1 publication Critical patent/PE20110777A1/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
    • C07D471/10—Spiro-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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE ESPIROPIPERIDINA DE FORMULA (I) DONDE B ES ALQUILO, ARILO, CICLOALQUILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDO CON R3, EN DONDE R3 ES HALOGENO, CN, OH, ENTRE OTROS; A ES ARILO, HETEROARILO, CICLOALQUILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDO CON R4, EN DONDE R4 ES ALQUILO, HALOGENO, CN, ENTRE OTROS; CUANDO ---- ES UN ENLACE SENCILLO R1a Y R1b SON CADA UNO H, ALQUILO, ALQUENILO, ENTRE OTROS; Y CUANDO ---- ES UN DOBLE ENLACE R1b ESTA AUSENTE Y R1a ES H, ALQUILO, (CH2)t-CICLOALQUILO, ENTRE OTROS, DONDE t ES DE 0 A 3; n ES DE 1 A 3; R2 ES ALQUILO, CICLOALQUILO O ALQUENILO OPCIONALMENTE SUSTITUIDO CON HALOGENO, OH O CN. SON COMPUESTOS PREFERIDOS: (5R,7S)-8-(4-HIDROXI-3-ISOPROPOXI-BENCIL)-7-METIL-1-FENIL-1,8-DIAZA-ESPIRO[4,5]DECAN-2-ONA; N-{4-[(5R,7S)-8-(4-HIDROXI-3-ISOPROPOXI-BENCIL)-7-METIL-2-OXO-1,8-DIAZA-ESPIRO[4,5]DEC-1-IL]-FENIL}-ACETAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA BETA-SECRETASA (BACE) SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, ISQUEMIA CEREBRAL, DEMENCIA
PE2011001066A 2008-11-23 2009-11-12 Nuevas lactamas como inhibidores de beta secretasa PE20110777A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11722508P 2008-11-23 2008-11-23

Publications (1)

Publication Number Publication Date
PE20110777A1 true PE20110777A1 (es) 2011-10-29

Family

ID=41481076

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011001066A PE20110777A1 (es) 2008-11-23 2009-11-12 Nuevas lactamas como inhibidores de beta secretasa

Country Status (28)

Country Link
US (1) US20110224231A1 (es)
EP (1) EP2370439A1 (es)
JP (2) JP4932065B2 (es)
KR (1) KR20110086769A (es)
CN (1) CN102317289A (es)
AP (1) AP2011005725A0 (es)
AU (1) AU2009318855A1 (es)
BR (1) BRPI0922799A2 (es)
CA (1) CA2743584A1 (es)
CL (1) CL2011001147A1 (es)
CO (1) CO6361924A2 (es)
CR (1) CR20110269A (es)
CU (1) CU20110113A7 (es)
DO (1) DOP2011000134A (es)
EA (1) EA201170722A1 (es)
EC (1) ECSP11011073A (es)
GE (1) GEP20135806B (es)
IL (1) IL212869A0 (es)
MA (1) MA32929B1 (es)
MX (1) MX2011005346A (es)
NI (1) NI201100096A (es)
NZ (1) NZ592823A (es)
PE (1) PE20110777A1 (es)
SV (1) SV2011003916A (es)
TN (1) TN2011000252A1 (es)
UA (1) UA99787C2 (es)
WO (1) WO2010058333A1 (es)
ZA (1) ZA201103738B (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR074466A1 (es) 2008-12-05 2011-01-19 Sanofi Aventis Piperidina espiro pirrolidinona y piperidinona sustituidas y su uso terapeutico en enfermedades mediadas por la modulacion de los receptores h3.
AR075854A1 (es) 2009-03-13 2011-05-04 Vitae Pharmaceuticals Inc Inhibidores de beta- secretasa
AU2010294214B2 (en) 2009-09-11 2015-05-07 Vivoryon Therapeutics N.V. Heterocylcic derivatives as inhibitors of glutaminyl cyclase
EP3372580B1 (de) * 2011-01-25 2020-07-22 Bayer CropScience Aktiengesellschaft Verfahren zur herstellung von 1-h-pyrrolidin-2,4-dion-derivaten
WO2012172449A1 (en) 2011-06-13 2012-12-20 Pfizer Inc. Lactams as beta secretase inhibitors
TWI557112B (zh) * 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β－分泌酶抑制劑
EP2900650A1 (en) 2012-09-28 2015-08-05 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US9926317B2 (en) 2014-07-14 2018-03-27 Merck Sharp Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2016008064A1 (en) * 2014-07-14 2016-01-21 Merck Sharp & Dohme Corp. Inhibitors of renal outer medullary potassium channel
WO2016100940A1 (en) 2014-12-19 2016-06-23 The Broad Institute, Inc. Dopamine d2 receptor ligands
EP3233799B1 (en) 2014-12-19 2021-05-19 The Broad Institute, Inc. Dopamine d2 receptor ligands
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
CN113045484B (zh) * 2019-12-27 2024-01-26 南京药石科技股份有限公司 一种2-氨基-2-(1-甲基-4-哌啶基)丙烷-1-醇的制备方法

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Also Published As

Publication number Publication date
JP4932065B2 (ja) 2012-05-16
CU20110113A7 (es) 2012-01-31
CL2011001147A1 (es) 2011-09-30
SV2011003916A (es) 2011-07-28
MA32929B1 (fr) 2012-01-02
BRPI0922799A2 (pt) 2019-09-24
ECSP11011073A (es) 2011-06-30
ZA201103738B (en) 2012-01-25
AU2009318855A1 (en) 2010-05-27
KR20110086769A (ko) 2011-07-29
UA99787C2 (en) 2012-09-25
WO2010058333A1 (en) 2010-05-27
GEP20135806B (en) 2013-04-10
EP2370439A1 (en) 2011-10-05
AP2011005725A0 (en) 2011-06-30
NI201100096A (es) 2011-10-31
CO6361924A2 (es) 2012-01-20
MX2011005346A (es) 2011-06-16
CN102317289A (zh) 2012-01-11
CR20110269A (es) 2011-07-04
EA201170722A1 (ru) 2011-10-31
IL212869A0 (en) 2011-07-31
JP2012509310A (ja) 2012-04-19
NZ592823A (en) 2012-12-21
DOP2011000134A (es) 2011-07-31
CA2743584A1 (en) 2010-05-27
JP2012107029A (ja) 2012-06-07
TN2011000252A1 (fr) 2012-12-17
US20110224231A1 (en) 2011-09-15

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