PE20171349A1 - Inhibidores de bace1 - Google Patents

Inhibidores de bace1

Info

Publication number
PE20171349A1
PE20171349A1 PE2017001451A PE2017001451A PE20171349A1 PE 20171349 A1 PE20171349 A1 PE 20171349A1 PE 2017001451 A PE2017001451 A PE 2017001451A PE 2017001451 A PE2017001451 A PE 2017001451A PE 20171349 A1 PE20171349 A1 PE 20171349A1
Authority
PE
Peru
Prior art keywords
alkyl
cycloalkyl
halogen
compound
refers
Prior art date
Application number
PE2017001451A
Other languages
English (en)
Inventor
Bjoern Bartels
Cosimo Dolente
Wolfgang Guba
Wolfgang Haap
Sander Ulrike Obst
Jens-Uwe Peters
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 PE20171349A1 publication Critical patent/PE20171349A1/es

Links

Classifications

    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D417/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Se refiere a un compuesto inhibidor de BACE1 de formula (I), donde A y B son heteroarilos, R1 y R2 son alquilo C1-C6 o halogeno-alquilo C1-C6 o R1 y R2 forman con el atomo de C un cicloalquilo C3-C6 opcionalmente sustituido; R3 es H, cicloalquilo C3-C6, entre otros; R4 es H o alquilo-C1-C6; R5 es alquilo C1-C6 o halogeno-alquilo C1-C6; R6 es halogeno; R7 es amino, ciano, entre otros. Es un compuesto seleccionado el (1R,3R)-3-[2-fluoro-5-[3-(5-metoxipirazin-2-il)isoxazol-5-il]fenil]-3,6,6-trimetil-1-metilimino-1-oxo-2H-1,4-tiazin-5-amina;acido 2,2,2 trifluoroacetico; entre otros. Tambien se refiere a una composicion. Dicho compuesto es util en el tratamiento de la enfermedad de Alzheimer
PE2017001451A 2015-03-20 2016-03-16 Inhibidores de bace1 PE20171349A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP15160101 2015-03-20

Publications (1)

Publication Number Publication Date
PE20171349A1 true PE20171349A1 (es) 2017-09-13

Family

ID=52780400

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017001451A PE20171349A1 (es) 2015-03-20 2016-03-16 Inhibidores de bace1

Country Status (18)

Country Link
US (4) US10047081B2 (es)
EP (1) EP3271355B1 (es)
JP (1) JP6674960B2 (es)
KR (1) KR20170129745A (es)
CN (1) CN107406440B (es)
AU (1) AU2016236402B2 (es)
BR (1) BR112017015474A2 (es)
CA (1) CA2979113A1 (es)
CL (1) CL2017002229A1 (es)
CO (1) CO2017007691A2 (es)
CR (1) CR20170426A (es)
IL (1) IL253322A0 (es)
MX (1) MX2017012188A (es)
PE (1) PE20171349A1 (es)
PH (1) PH12017501668A1 (es)
RU (1) RU2712272C2 (es)
SG (1) SG11201707050VA (es)
WO (1) WO2016150785A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20170426A (es) * 2015-03-20 2017-10-23 Hoffmann La Roche Inhibidores de bace 1
CN110467611B (zh) * 2018-05-11 2022-09-27 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
AR115495A1 (es) 2018-06-06 2021-01-27 Syngenta Crop Protection Ag Derivados heterocíclicos con sustituyentes que contienen azufre activos como plaguicidas

Family Cites Families (36)

* Cited by examiner, † Cited by third party
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AU2009216825A1 (en) 2008-02-18 2009-08-27 F. Hoffmann-La Roche Ag 4, 5-dihydro-oxazol-2-yl amine derivatives
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20110065695A1 (en) 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
UA103272C2 (uk) 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
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
US8815881B2 (en) 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
US20120053200A1 (en) 2010-09-01 2012-03-01 Harald Mauser Bace 2 inhibitors
US9242943B2 (en) 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US8399459B2 (en) 2011-02-02 2013-03-19 Hoffmann-La Roche Inc. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US8404680B2 (en) 2011-02-08 2013-03-26 Hoffmann-La Roche Inc. N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors
US8815841B2 (en) 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US9067924B2 (en) 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
US8748418B2 (en) 2011-03-18 2014-06-10 Hoffmann-La Roche Inc. 1,4-oxazepines as BACE1 and/or BACE2 inhibitors
US8877744B2 (en) 2011-04-04 2014-11-04 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
JP2014514302A (ja) * 2011-04-13 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション Ｂａｃｅ阻害薬としての５−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用
CN103596939A (zh) * 2011-04-13 2014-02-19 默沙东公司 作为bace抑制剂的5-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其应用
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US9079919B2 (en) 2011-05-27 2015-07-14 Hoffmann-La Roche Inc. Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors
BR112013031098A2 (pt) 2011-06-07 2016-12-06 Hoffmann La Roche halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou bace2
CN103608344B (zh) 2011-06-07 2016-11-23 霍夫曼-拉罗奇有限公司 [1,3]噁嗪类
US8927535B2 (en) 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
RU2014111055A (ru) 2011-08-22 2015-09-27 Мерк Шарп И Доум Корп. 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение
US20130073953A1 (en) 2011-09-21 2013-03-21 Timothy Onyenobi News headline screenshot viewing system
UA113538C2 (xx) 2012-01-26 2017-02-10 Фторметил-5,6-дигідро-4h-$1,3]оксазини
PE20150021A1 (es) * 2012-05-24 2015-01-28 Hoffmann La Roche 5-amino[1,4]tiazinas como inhibidores de bace1
CA2872181A1 (en) 2012-06-26 2014-01-03 F. Hoffmann-La Roche Ag Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors
EP2908825B1 (en) * 2012-10-17 2018-04-18 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
CN104968660A (zh) * 2013-01-22 2015-10-07 霍夫曼-拉罗奇有限公司 作为bace1抑制剂的氟-[1,3]噁嗪类化合物
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WO2014150331A1 (en) * 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
WO2014150344A1 (en) 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. C2-azaspiro iminothiazine dioxides as bace inhibitors
CR20170426A (es) * 2015-03-20 2017-10-23 Hoffmann La Roche Inhibidores de bace 1

Also Published As

Publication number Publication date
RU2017134884A3 (es) 2019-07-17
US20190337936A1 (en) 2019-11-07
BR112017015474A2 (pt) 2018-01-30
CA2979113A1 (en) 2016-09-29
SG11201707050VA (en) 2017-10-30
AU2016236402B2 (en) 2019-08-01
IL253322A0 (en) 2017-09-28
EP3271355A1 (en) 2018-01-24
US20180057485A1 (en) 2018-03-01
US11034687B2 (en) 2021-06-15
JP6674960B2 (ja) 2020-04-01
US20200308166A1 (en) 2020-10-01
CO2017007691A2 (es) 2017-10-20
WO2016150785A1 (en) 2016-09-29
RU2017134884A (ru) 2019-04-22
CR20170426A (es) 2017-10-23
JP2018507879A (ja) 2018-03-22
EP3271355B1 (en) 2020-07-29
KR20170129745A (ko) 2017-11-27
HK1244790A1 (zh) 2018-08-17
US10399969B2 (en) 2019-09-03
CN107406440A (zh) 2017-11-28
CN107406440B (zh) 2021-05-07
US10047081B2 (en) 2018-08-14
US10723729B2 (en) 2020-07-28
PH12017501668A1 (en) 2018-03-19
CL2017002229A1 (es) 2018-04-13
US20180319787A1 (en) 2018-11-08
AU2016236402A1 (en) 2017-07-27
RU2712272C2 (ru) 2020-01-28
MX2017012188A (es) 2017-12-15

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