ECSP13012858A - Derivados de piperidina puenteada - Google Patents

Derivados de piperidina puenteada

Info

Publication number
ECSP13012858A
ECSP13012858A ECSP13012858A ECSP13012858A EC SP13012858 A ECSP13012858 A EC SP13012858A EC SP13012858 A ECSP13012858 A EC SP13012858A EC SP13012858 A ECSP13012858 A EC SP13012858A
Authority
EC
Ecuador
Prior art keywords
lower alkyl
halogen
ring
alkyl substituted
substituted
Prior art date
Application number
Other languages
English (en)
Inventor
Andrew William Thomas
Thomas Luebbers
Luke Green
Karlheinz Baumann
Anja Limberg
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 ECSP13012858A publication Critical patent/ECSP13012858A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

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

Abstract

La presente invención se refiere a compuestos de la fórmula:en la que:hetarilo I es un grupo heteroarilo de cinco o seis eslabones, que contiene de 1 a 3 heteroátomos elegidos entre S y N; hetarilo II es un grupo heteroarilo de seis eslabones, que contiene de 1 a 3 heteroátomos elegidos entre S y N, o es un sistema cíclico de dos miembros que contiene de 1 a 4 heteroátomos elegidos entre S y N, de los que por lo menos un anillo es de naturaleza aromática; R1 es alquilo inferior, alcoxi inferior, alquilo inferior sustituido por halógeno o halógeno; R2 es alquilo inferior, alquilo inferior sustituido por halógeno, halógeno, alcoxi inferior, cicloalquilo sustituido por alquilo inferior o alquilo inferior sustituido por halógeno, o es alquilo inferior sustituido por hidroxi, o es furilo, o es O-bencilo, -(CH2)p-fenilo, opcionalmente sustituido por halógeno, alcoxi inferior, alquilo inferior sustituido por halógeno, alquilo inferior o por ciano;R3 es hidrógeno o alquilo inferior;Y es -(CH2)n-, -CH2OCH2-, -CH2O-, CH2S-, -CH2SCH2- y está unido a dos de los átomos de carbono del anillo, la unión se realiza con los átomos de carbono "a" y "b" del anillo o con los átomos de carbono "c" y "d" del anillo;p es el número 0 ó 1;m es el número 0, 1 ó 2; si m es 2, entonces R1 puede ser igual o diferente; n es el número 2 ó 3;"o" es el número 0, 1 ó 2, si "o" es 2, entonces R2 puede ser igual o diferente;o a sus sales de adición de ácido farmacéuticamente activas.Los compuestos presentes de la fórmula I son moduladores de beta-amiloide y por ello pueden ser útiles para el tratamiento o prevención de una enfermedad asociada con la deposición de ß-amiloide en el 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.
ECSP13012858 2011-03-02 2013-08-30 Derivados de piperidina puenteada ECSP13012858A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11156587 2011-03-02

Publications (1)

Publication Number Publication Date
ECSP13012858A true ECSP13012858A (es) 2013-10-31

Family

ID=45757448

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP13012858 ECSP13012858A (es) 2011-03-02 2013-08-30 Derivados de piperidina puenteada

Country Status (22)

Country Link
US (1) US8703763B2 (es)
EP (1) EP2681214B1 (es)
JP (1) JP5753591B2 (es)
KR (1) KR101550122B1 (es)
CN (1) CN103403003B (es)
BR (1) BR112013021924A2 (es)
CA (1) CA2824239A1 (es)
CL (1) CL2013002474A1 (es)
CO (1) CO6761320A2 (es)
CR (1) CR20130358A (es)
EA (1) EA025035B1 (es)
EC (1) ECSP13012858A (es)
IL (1) IL227251A (es)
MA (1) MA34964B1 (es)
MX (1) MX2013009031A (es)
MY (1) MY167264A (es)
PE (1) PE20140250A1 (es)
PH (1) PH12013501658A1 (es)
SG (1) SG193239A1 (es)
UA (1) UA110368C2 (es)
WO (1) WO2012116965A1 (es)
ZA (1) ZA201305322B (es)

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WO2008133300A1 (ja) * 2007-04-25 2008-11-06 Nissan Chemical Industries, Ltd. ポリイミド前駆体及びポリイミド並びに画像形成下層膜塗布液
US11090297B2 (en) 2013-06-21 2021-08-17 Prilenia Neurotherapeutics Ltd. Pridopidine for treating huntington's disease
EP3347363B1 (en) * 2015-09-09 2020-01-01 H. Hoffnabb-La Roche Ag N-(3-azabicyclo[3.2.1]octan-8-yl)-8-(4-phenyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[l,5-a]pyridin-2-amine derivatives as gamma-secretase modulators for treating alzheimer's disease
JP6659841B2 (ja) 2015-11-12 2020-03-04 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 脊髄性筋萎縮症を処置するための組成物
WO2017097728A1 (en) * 2015-12-10 2017-06-15 F. Hoffmann-La Roche Ag Bridged piperidine derivatives
IL294124B2 (en) 2015-12-10 2024-02-01 Ptc Therapeutics Inc Methods for treating huntington's disease
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
WO2018011164A1 (en) 2016-07-14 2018-01-18 F. Hoffmann-La Roche Ag Fused pyrimidine derivatives
EP4516356A3 (en) 2016-08-24 2025-05-14 Prilenia Neurotherapeutics Ltd. Use of pridopidine for treating functional decline
AR109829A1 (es) * 2016-09-29 2019-01-30 Hoffmann La Roche Derivados de piperidina puenteados
JP6956175B2 (ja) * 2016-10-04 2021-11-02 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 二環式ヘテロアリール誘導体
EP3535266B1 (en) * 2016-11-01 2021-12-29 F. Hoffmann-La Roche AG Bicyclic heteroaryl derivatives
AR110122A1 (es) 2016-11-08 2019-02-27 Hoffmann La Roche Fenoxitriazoles
WO2018111926A2 (en) 2016-12-16 2018-06-21 Inception 3, Inc. Methods of treating cochlear synaptopathy
US11407753B2 (en) 2017-06-05 2022-08-09 Ptc Therapeutics, Inc. Compounds for treating Huntington's disease
US11382918B2 (en) 2017-06-28 2022-07-12 Ptc Therapeutics, Inc. Methods for treating Huntington's Disease
WO2019005993A1 (en) 2017-06-28 2019-01-03 Ptc Therapeutics, Inc. METHODS OF TREATING HUNTINGTON'S DISEASE
US11339161B2 (en) * 2017-12-19 2022-05-24 Boehringer Ingelheim International Gmbh Triazolo pyridines as modulators of gamma-secretase
CN111417636B (zh) * 2018-01-22 2023-09-26 豪夫迈·罗氏有限公司 三唑并-氮杂䓬衍生物
MX2020009957A (es) 2018-03-27 2021-01-15 Ptc Therapeutics Inc Compuestos para el tratamiento de enfermedad de hungtinton.
EP3814345B8 (en) 2018-06-27 2024-10-30 PTC Therapeutics, Inc. Heteroaryl compounds for treating huntington's disease
EP3814360B8 (en) 2018-06-27 2024-11-06 PTC Therapeutics, Inc. Heteroaryl compounds for treating huntington's disease
PL3814357T3 (pl) 2018-06-27 2024-09-16 Ptc Therapeutics, Inc. Związki heterocykliczne i heteroarylowe do leczenia choroby huntingtona
US12084461B2 (en) * 2018-09-03 2024-09-10 Hoffmann-La Roche Inc. Bicyclic heteroaryl derivatives
BR112021009443A2 (pt) 2018-12-13 2021-08-17 F. Hoffmann-La Roche Ag derivados de 7-fenóxi-n-(3-azabiciclo[3.2.1]octan-8-il)-6,7-di-hidro-5h-pirrolo[1,2-b][1,2,4]triazol-2-amina e compostos relacionados como moduladores de gama-secretase para o tratamento da doença de alzheimer.
US12275709B2 (en) * 2018-12-27 2025-04-15 Hoffmann-La Roche Inc. Process for the preparation of exo-tert-butyl N-(3-azabicyclo[3.2.1]octan-8-yl)carbamate
WO2020231977A1 (en) 2019-05-13 2020-11-19 Ptc Therapeutics, Inc. Compounds for treating huntington's disease
CN113372364B (zh) * 2020-03-10 2024-05-31 明慧医药(上海)有限公司 一类jak激酶抑制剂及其制备和应用

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US6432985B2 (en) * 2000-04-25 2002-08-13 Hoffmann-La Roche Inc. Neuroprotective substituted piperidine compounds with activity as NMDA NR2B subtype selective antagonists
US7037902B2 (en) 2002-07-03 2006-05-02 Receptron, Inc. Affinity small molecules for the EPO receptor
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JP5328816B2 (ja) 2008-02-22 2013-10-30 エフ.ホフマン−ラ ロシュ アーゲー アミロイドβの調節薬
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US8486967B2 (en) 2010-02-17 2013-07-16 Hoffmann-La Roche Inc. Heteroaryl substituted piperidines

Also Published As

Publication number Publication date
US20120225884A1 (en) 2012-09-06
EP2681214A1 (en) 2014-01-08
KR101550122B1 (ko) 2015-09-03
CA2824239A1 (en) 2012-09-07
UA110368C2 (xx) 2015-12-25
CN103403003A (zh) 2013-11-20
CN103403003B (zh) 2016-09-14
BR112013021924A2 (pt) 2020-10-20
PH12013501658A1 (en) 2013-10-07
EP2681214B1 (en) 2017-03-22
CO6761320A2 (es) 2013-09-30
JP2014506903A (ja) 2014-03-20
WO2012116965A1 (en) 2012-09-07
MA34964B1 (fr) 2014-03-01
KR20130140142A (ko) 2013-12-23
EA025035B1 (ru) 2016-11-30
CR20130358A (es) 2013-10-03
NZ612525A (en) 2015-08-28
IL227251A (en) 2016-09-29
CL2013002474A1 (es) 2014-05-30
PE20140250A1 (es) 2014-03-12
SG193239A1 (en) 2013-10-30
MX2013009031A (es) 2013-09-02
MY167264A (en) 2018-08-14
JP5753591B2 (ja) 2015-07-22
EA201391209A1 (ru) 2013-12-30
IL227251A0 (en) 2013-09-30
US8703763B2 (en) 2014-04-22
ZA201305322B (en) 2014-04-30
AU2012222426A1 (en) 2013-07-11

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