CO6761320A2 - Derivados de piperidina puenteada - Google Patents

Derivados de piperidina puenteada

Info

Publication number
CO6761320A2
CO6761320A2 CO13176486A CO13176486A CO6761320A2 CO 6761320 A2 CO6761320 A2 CO 6761320A2 CO 13176486 A CO13176486 A CO 13176486A CO 13176486 A CO13176486 A CO 13176486A CO 6761320 A2 CO6761320 A2 CO 6761320A2
Authority
CO
Colombia
Prior art keywords
lower alkyl
halogen
ring
substituted
amyloid
Prior art date
Application number
CO13176486A
Other languages
English (en)
Inventor
Kariheinz Baumann
Luke Green
Anja Limberg
Thomas Luebbers
Andrew Thomas
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 CO6761320A2 publication Critical patent/CO6761320A2/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)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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;Res alquilo inferior, alcoxi inferior, alquilo inferior sustituido por halógeno o halógeno;Res 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,–(CH)-fenilo, opcionalmente sustituido por halógeno, alcoxi inferior, alquilo inferior sustituido por halógeno, alquilo inferior o por ciano;Res hidrógeno o alquilo inferior;Y es –(CH)-, -CHOCH-, -CHO-, CHS-, -CHSCH- 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 Rpuede ser igual o diferente;n es el número 2 ó 3;“o” es el número 0, 1 ó 2, si “o” es 2, entonces Rpuede ser igual o diferente; o a sus sales de adición de ácido farmacéuticamente activas.Los compuestos presentes de la fórmula I son moduladores de betaamiloide 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.
CO13176486A 2011-03-02 2013-07-25 Derivados de piperidina puenteada CO6761320A2 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
CO6761320A2 true CO6761320A2 (es) 2013-09-30

Family

ID=45757448

Family Applications (1)

Application Number Title Priority Date Filing Date
CO13176486A CO6761320A2 (es) 2011-03-02 2013-07-25 Derivados de piperidina puenteada

Country Status (21)

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)
SG (1) SG193239A1 (es)
UA (1) UA110368C2 (es)
WO (1) WO2012116965A1 (es)
ZA (1) ZA201305322B (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5321839B2 (ja) * 2007-04-25 2013-10-23 日産化学工業株式会社 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
MX2018005890A (es) 2015-11-12 2018-08-15 Hoffmann La Roche Composiciones para tratar atrofia muscular espinal.
CN108137579B (zh) * 2015-12-10 2022-01-07 豪夫迈·罗氏有限公司 桥连哌啶衍生物
ES2879995T3 (es) 2015-12-10 2021-11-23 Ptc Therapeutics Inc Métodos para el tratamiento de la enfermedad de Huntington
EP3475279B1 (en) * 2016-06-27 2021-07-14 F. Hoffmann-La Roche AG Triazolopyridines as gamma-secretase modulators
EP3484884B1 (en) 2016-07-14 2021-01-27 Hoffmann-La Roche AG Fused pyrimidine derivatives
JP6912574B2 (ja) 2016-08-24 2021-08-04 プリレニア ニューロセラピューティクス リミテッド 機能低下を治療するためのプリドピジンの使用
AR109829A1 (es) * 2016-09-29 2019-01-30 Hoffmann La Roche Derivados de piperidina puenteados
CN109476670B (zh) * 2016-10-04 2022-06-28 豪夫迈·罗氏有限公司 二环杂芳基衍生物
JP7111704B2 (ja) * 2016-11-01 2022-08-02 エフ.ホフマン-ラ ロシュ アーゲー 二環式ヘテロアリール誘導体
WO2018087018A1 (en) 2016-11-08 2018-05-17 F. Hoffmann-La Roche Ag Phenoxytriazoles
JP6904612B2 (ja) 2016-12-16 2021-07-21 パイプライン セラピューティクス, インコーポレイテッド 蝸牛シナプス障害を処置する方法
EA201992878A1 (ru) 2017-06-05 2020-05-08 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Соединения для лечения болезни хантингтона
MX2019015580A (es) 2017-06-28 2020-07-28 Ptc Therapeutics Inc Metodos para tratar la enfermedad de huntington.
BR112019027717A2 (pt) 2017-06-28 2020-07-28 Ptc Therapeutics, Inc. métodos para tratar a doença de huntington
WO2019121596A1 (en) * 2017-12-19 2019-06-27 Boehringer Ingelheim International Gmbh Triazolo pyridines as modulators of gamma-secretase
EP3743428B1 (en) 2018-01-22 2022-01-19 F. Hoffmann-La Roche AG Triazolo-azepine derivatives
CN112135815A (zh) 2018-03-27 2020-12-25 Ptc医疗公司 用于治疗亨廷顿氏病的化合物
EP3814360A1 (en) 2018-06-27 2021-05-05 PTC Therapeutics, Inc. Heteroaryl compounds for treating huntington's disease
AU2019294478B2 (en) 2018-06-27 2023-03-23 Ptc Therapeutics, Inc. Heterocyclic and heteroaryl compounds for treating Huntington's disease
PT3846903T (pt) * 2018-09-03 2023-12-14 Hoffmann La Roche Derivados heteroarílicos bicíclicos
US20220056036A1 (en) * 2018-12-13 2022-02-24 Hoffmann-La Roche Inc. 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
CN113372364A (zh) * 2020-03-10 2021-09-10 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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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
US8703763B2 (en) 2014-04-22
UA110368C2 (en) 2015-12-25
SG193239A1 (en) 2013-10-30
JP5753591B2 (ja) 2015-07-22
US20120225884A1 (en) 2012-09-06
CN103403003A (zh) 2013-11-20
EP2681214A1 (en) 2014-01-08
AU2012222426A1 (en) 2013-07-11
MY167264A (en) 2018-08-14
PE20140250A1 (es) 2014-03-12
BR112013021924A2 (pt) 2020-10-20
KR101550122B1 (ko) 2015-09-03
CN103403003B (zh) 2016-09-14
ECSP13012858A (es) 2013-10-31
KR20130140142A (ko) 2013-12-23
CR20130358A (es) 2013-10-03
EA201391209A1 (ru) 2013-12-30
CL2013002474A1 (es) 2014-05-30
EP2681214B1 (en) 2017-03-22
IL227251A0 (en) 2013-09-30
MA34964B1 (fr) 2014-03-01
CA2824239A1 (en) 2012-09-07
MX2013009031A (es) 2013-09-02
NZ612525A (en) 2015-08-28
ZA201305322B (en) 2014-04-30
EA025035B1 (ru) 2016-11-30
WO2012116965A1 (en) 2012-09-07
JP2014506903A (ja) 2014-03-20

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