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

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C07D451/04—Heterocyclic 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
    • 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61P25/28—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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (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
WO2017042114A1 (en) 2015-09-09 2017-03-16 F. Hoffmann-La Roche Ag Bridged piperidine derivatives
AU2016353961B2 (en) 2015-11-12 2019-08-29 F. Hoffmann-La Roche Ag Compositions for treating spinal muscular atrophy
EP3386978B1 (en) * 2015-12-10 2021-01-27 H. Hoffnabb-La Roche Ag Bridged piperidine derivatives
CA3119019C (en) 2015-12-10 2024-06-11 Ptc Therapeutics, Inc. Compounds and 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
JP6980751B2 (ja) 2016-07-14 2021-12-15 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 縮合ピリミジン誘導体
IL311081A (en) 2016-08-24 2024-04-01 Prilenia Neurotherapeutics Ltd Use of pyridofidine to treat functional decline
AR109829A1 (es) * 2016-09-29 2019-01-30 Hoffmann La Roche Derivados de piperidina puenteados
EP3523304B1 (en) * 2016-10-04 2021-01-27 H. Hoffnabb-La Roche Ag Bicyclic heteroaryl derivatives
EP3535266B1 (en) * 2016-11-01 2021-12-29 F. Hoffmann-La Roche AG Bicyclic heteroaryl derivatives
US11319314B2 (en) 2016-11-08 2022-05-03 Hoffmann-La Roche Inc. Phenoxytriazoles
EP3554502A4 (en) 2016-12-16 2021-01-06 Pipeline Therapeutics, Inc. METHOD FOR TREATMENT OF COCHLEA SYNAPTOPATHY
EP4151627A1 (en) 2017-06-05 2023-03-22 PTC Therapeutics, Inc. Compounds for treating huntington's disease
CN111163838B (zh) 2017-06-28 2023-03-28 Ptc医疗公司 用于治疗亨廷顿氏病的方法
CN111182898B (zh) 2017-06-28 2024-04-16 Ptc医疗公司 用于治疗亨廷顿氏病的方法
EP3672971B1 (en) * 2017-12-19 2021-07-14 Boehringer Ingelheim International GmbH Triazolo pyridines as modulators of gamma-secretase
US11370802B2 (en) 2018-01-22 2022-06-28 Hoffmann-La Roche, Inc. Triazolo-azepine derivatives
BR112020019373A2 (pt) 2018-03-27 2020-12-29 Ptc Therapeutics, Inc. Compostos para o tratamento da doença de hutington
IL279688B2 (en) 2018-06-27 2025-01-01 Ptc Therapeutics Inc Heterocyclic and heteroaryl compounds for the treatment of Huntington's disease
WO2020005882A1 (en) 2018-06-27 2020-01-02 Ptc Therapeutics, Inc. Heteroaryl compounds for treating huntington's disease
KR20210038845A (ko) 2018-06-27 2021-04-08 피티씨 테라퓨틱스, 인크. 헌팅턴병 치료를 위한 헤테로아릴 화합물
MX2021002087A (es) * 2018-09-03 2021-04-28 Hoffmann La Roche Derivados de heteroarilo biciclicos.
AU2019395774B2 (en) * 2018-12-13 2024-12-12 F. Hoffmann-La Roche Ag 7-phenoxy-N-(3-azabicyclo[3.2.1]octan-8-yl)-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazol-2-amine derivatives and related compounds as gamma-secretase modulators for the treatment of Alzheimer's disease
AU2019412747B8 (en) * 2018-12-27 2025-04-24 F. Hoffmann-La Roche Ag Process for the preparation exo-tert-butyl N-(3-azabicyclo[3.2.1]octan-8-yl)carbamate
CA3139821A1 (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
HU227684B1 (en) 2003-08-29 2011-11-28 Sanofi Aventis Adamantane and azabicyclo-octane and nonane derivatives and their use as dpp-iv inhibitors
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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
IL227251A (en) 2016-09-29
SG193239A1 (en) 2013-10-30
ZA201305322B (en) 2014-04-30
EA201391209A1 (ru) 2013-12-30
CN103403003B (zh) 2016-09-14
MY167264A (en) 2018-08-14
JP2014506903A (ja) 2014-03-20
KR101550122B1 (ko) 2015-09-03
PE20140250A1 (es) 2014-03-12
IL227251A0 (en) 2013-09-30
US8703763B2 (en) 2014-04-22
CN103403003A (zh) 2013-11-20
NZ612525A (en) 2015-08-28
EA025035B1 (ru) 2016-11-30
JP5753591B2 (ja) 2015-07-22
CO6761320A2 (es) 2013-09-30
PH12013501658A1 (en) 2013-10-07
EP2681214A1 (en) 2014-01-08
CL2013002474A1 (es) 2014-05-30
BR112013021924A2 (pt) 2020-10-20
MX2013009031A (es) 2013-09-02
AU2012222426A1 (en) 2013-07-11
WO2012116965A1 (en) 2012-09-07
UA110368C2 (xx) 2015-12-25
EP2681214B1 (en) 2017-03-22
KR20130140142A (ko) 2013-12-23
CR20130358A (es) 2013-10-03
MA34964B1 (fr) 2014-03-01
CA2824239A1 (en) 2012-09-07
US20120225884A1 (en) 2012-09-06

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