MX2013014194A - 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2). - Google Patents

1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).

Info

Publication number
MX2013014194A
MX2013014194A MX2013014194A MX2013014194A MX2013014194A MX 2013014194 A MX2013014194 A MX 2013014194A MX 2013014194 A MX2013014194 A MX 2013014194A MX 2013014194 A MX2013014194 A MX 2013014194A MX 2013014194 A MX2013014194 A MX 2013014194A
Authority
MX
Mexico
Prior art keywords
bace
thiazepines
fused
cyclopropyl
inhibitors
Prior art date
Application number
MX2013014194A
Other languages
English (en)
Inventor
Thomas Woltering
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 MX2013014194A publication Critical patent/MX2013014194A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/14—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
    • A61P25/28—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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

La presente invención proporciona 1,3-tiazepinas fusionadas a ciclopropilo de la fórmula (I) (Ver Formula) que tienen actividad inhibidora de BACE1 y/o BACE2, su manufactura, composiciones farmacéuticas que las contienen y su uso como sustancias terapéuticamente activas. Los compuestos activos de la presente invención son útiles en el tratamiento terapéutico y/o profiláctico de, por ejemplo, enfermedad de Alzheimer y diabetes tipo 2.
MX2013014194A 2011-07-06 2012-07-03 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2). MX2013014194A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11172784 2011-07-06
PCT/EP2012/062867 WO2013004676A1 (en) 2011-07-06 2012-07-03 Cyclopropyl-fused-1,3-thiazepines as bace 1 and/or bace 2 inhibitors

Publications (1)

Publication Number Publication Date
MX2013014194A true MX2013014194A (es) 2014-03-21

Family

ID=46456591

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013014194A MX2013014194A (es) 2011-07-06 2012-07-03 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).

Country Status (11)

Country Link
US (1) US8927535B2 (es)
EP (1) EP2729464B8 (es)
JP (1) JP2014520777A (es)
KR (1) KR20140048952A (es)
CN (1) CN103649083A (es)
BR (1) BR112014000022A2 (es)
CA (1) CA2838331A1 (es)
ES (1) ES2539696T3 (es)
MX (1) MX2013014194A (es)
RU (1) RU2014101464A (es)
WO (1) WO2013004676A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9309263B2 (en) 2013-01-29 2016-04-12 Amgen Inc. Fused multi-cyclic sulfone compounds as inhibitors of beta-secretase and methods of use thereof
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CN105164121A (zh) * 2013-03-08 2015-12-16 美国安进公司 作为β分泌酶抑制剂的全氟化环丙基稠合的1,3-噁嗪-2-胺化合物以及其使用方法
WO2015017407A1 (en) 2013-07-30 2015-02-05 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta- secretase
MX2017001794A (es) 2014-08-08 2017-06-29 Amgen Inc Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.
PE20171349A1 (es) 2015-03-20 2017-09-13 Hoffmann La Roche Inhibidores de bace1
US10246429B2 (en) 2015-08-06 2019-04-02 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
AU2017378316B2 (en) 2016-12-15 2021-04-01 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
US11021493B2 (en) 2016-12-15 2021-06-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
MA54100A (fr) 2016-12-15 2021-10-20 Amgen Inc Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
JP7177773B2 (ja) 2016-12-15 2022-11-24 アムジエン・インコーポレーテツド β－セクレターゼ阻害剤としてのオキサジン誘導体および使用方法
MA54101A (fr) 2016-12-15 2021-10-27 Amgen Inc Dérivés de thiazine et d'oxazine bicycliques en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0617852A2 (pt) * 2005-10-25 2011-08-09 Shionogi & Co compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
UY32799A (es) * 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US20110065695A1 (en) 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
US20120245155A1 (en) * 2009-12-11 2012-09-27 Shionogi & Co., Ltd. Fused heterocyclic compound having amino group
US8673894B2 (en) * 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds

Also Published As

Publication number Publication date
US8927535B2 (en) 2015-01-06
EP2729464B8 (en) 2015-06-17
RU2014101464A (ru) 2015-08-20
EP2729464B1 (en) 2015-04-29
EP2729464A1 (en) 2014-05-14
JP2014520777A (ja) 2014-08-25
CA2838331A1 (en) 2013-01-10
CN103649083A (zh) 2014-03-19
BR112014000022A2 (pt) 2016-12-13
US20130012494A1 (en) 2013-01-10
ES2539696T3 (es) 2015-07-03
WO2013004676A1 (en) 2013-01-10
KR20140048952A (ko) 2014-04-24

Similar Documents

Publication Publication Date Title
MX2013013692A (es) Halogenoalquil-1,3-oxazinas como inhibidores de beta secretasa 1 (bace1) y/o beta secretasa 2 (bace2).
MX2013007558A (es) 1,4-oxazinas como inhibidores de los genes enzima de segmentacion de la proteina precursora del sitio 1 y/o 2 (bace1 y/o bace2).
MX2013007957A (es) 1,4-oxazinas como inhibidores de los genes de enzima de segmentacion de la proteina precursora amiloide del sitio beta 1 y/o (bace1 y/o bace2).
MX2013010795A (es) 1,3 oxazinas como inhibidores de beta-secretasa 1 (bace 1) y/o la beta-secretasa 2 (beta 2).
EA201391752A1 (ru) Спиро-[1,3]-оксазины и спиро-[1,4]-оксазепины в качестве ингибиторов bace1 и/или bace2
MX2013014007A (es) [1,3] oxazinas.
MX2013008478A (es) 1, 4 riazepinas/sulfonas como inhibidores de beta secretasa 1 (base1) y/o beta secretasa 2 (bace2).
MX2013014194A (es) 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).
EA201391670A1 (ru) 1,3-оксазины в качестве ингибиторов bace1 и/или bace2
MX2013008213A (es) N-[3-(5-amino-3,3a,7,7a-tetrahidro-1h-2,4-dioxa-6-aza-inden-7-il) -fenil]-amidas como inhibidores de beta-secretasa 1 (bace1) y/o beta-secretasa 2 (bace2).
MX2015008957A (es) Fluoro-[1,3]oxazinas como inhibidores de beta-secretasa 1 (bace1).
MX2012001985A (es) Derivados de 3-amino-5-fenil-5,6-dihidro-2h-[1,4]oxazina.
PH12014501334A1 (en) Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
MY169962A (en) 2-amino-5,5-difluoro-5,6-dihydro-oxazines as bace 1 and/or bace 2 inhibitors
MX2014003408A (es) N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][ 1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la beta-secretasa 1 (bace1).
PH12015502365A1 (en) Bace1 inhibitors
PH12014502623B1 (en) Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors
PH12014502541A1 (en) 5-amino [1,4] thiazines as bace 1 inhibitors
PH12017501668A1 (en) Bace1 inhibitors
MX2013002398A (es) Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes.
MX365292B (es) 5-aril-1-imino-1-oxo-[1,2,4]tiadiazinas.
MX2016016061A (es) 2,2,2-trifluoroetil-tiadiazinas.