MX2013007957A - 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). - Google Patents

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).

Info

Publication number
MX2013007957A
MX2013007957A MX2013007957A MX2013007957A MX2013007957A MX 2013007957 A MX2013007957 A MX 2013007957A MX 2013007957 A MX2013007957 A MX 2013007957A MX 2013007957 A MX2013007957 A MX 2013007957A MX 2013007957 A MX2013007957 A MX 2013007957A
Authority
MX
Mexico
Prior art keywords
bace1
oxazines
bace2 inhibitors
present
bace2
Prior art date
Application number
MX2013007957A
Other languages
English (en)
Inventor
Wolfgang Wostl
Robert Narquizian
Matteo Andreini
Emanuele Gabellieri
Massimiliano Travagli
Original Assignee
Siena Biotech Spa
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 Siena Biotech Spa filed Critical Siena Biotech Spa
Publication of MX2013007957A publication Critical patent/MX2013007957A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings

Abstract

La presente invención se refiere a 1,4-oxazinas de la fórmula (I): que tienen propiedades inhibidoras de BACE1 y/o BACE2, a su fabricación, a las composiciones farmacéuticas que las contienen y su uso como substancias terapéuticamente activas. Los compuestos activos de la presente invención son útiles en el tratamiento terapéutico y/o profiláctico por ejemplo de la enfermedad de Alzheimer y la diabetes del tipo 2.
MX2013007957A 2011-02-02 2012-01-31 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). MX2013007957A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11153095 2011-02-02
PCT/EP2012/051481 WO2012104263A2 (en) 2011-02-02 2012-01-31 1,4 oxazines as bace1 and/or bace2 inhibitors

Publications (1)

Publication Number Publication Date
MX2013007957A true MX2013007957A (es) 2013-08-01

Family

ID=45562303

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013007957A MX2013007957A (es) 2011-02-02 2012-01-31 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).

Country Status (11)

Country Link
US (1) US8399459B2 (es)
EP (1) EP2670738A2 (es)
JP (1) JP2014507427A (es)
KR (1) KR20140019340A (es)
CN (1) CN103339117B (es)
BR (1) BR112013014610A2 (es)
CA (1) CA2817841A1 (es)
HK (1) HK1187915A1 (es)
MX (1) MX2013007957A (es)
RU (1) RU2013137814A (es)
WO (1) WO2012104263A2 (es)

Families Citing this family (21)

* 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
WO2008133273A1 (ja) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
AU2008245082B8 (en) 2007-04-24 2012-09-13 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
NZ589590A (en) 2008-06-13 2012-05-25 Shionogi & Co Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
CA2783958A1 (en) 2009-12-11 2011-06-16 Shionogi & Co., Ltd. Oxazine derivative
US8927721B2 (en) 2010-10-29 2015-01-06 Shionogi & Co., Ltd. Naphthyridine derivative
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2703399A4 (en) 2011-04-26 2014-10-15 Shionogi & Co OXAZINE DERIVATIVE AND BACE-1 HEMMER THEREOF
JP2014524472A (ja) 2011-08-22 2014-09-22 メルク・シャープ・アンド・ドーム・コーポレーション Ｂａｃｅ阻害剤としての２−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用
BR112014008686A2 (pt) 2011-10-13 2017-04-25 Novartis Ag derivados de oxazina e uso dos mesmos no tratamento de doença
WO2013161929A1 (ja) * 2012-04-26 2013-10-31 塩野義製薬株式会社 ピリジニルモルホリノン誘導体およびそれらを含有する医薬組成物
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
CN104130204B (zh) * 2014-07-03 2016-04-27 浙江大学 一种制备n-磺酰基-1,4-噁嗪类衍生物的方法
PE20171349A1 (es) 2015-03-20 2017-09-13 Hoffmann La Roche Inhibidores de bace1

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006041404A1 (en) * 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-compounds and uses thereof
BRPI0617852A2 (pt) 2005-10-25 2011-08-09 Shionogi & Co compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos
BRPI0907563A2 (pt) 2008-02-18 2015-08-04 Hoffmann La Roche Derivados de 4,5-di-hidro-xazol-2-il amina
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
EP2580200B1 (en) * 2010-06-09 2016-09-14 Janssen Pharmaceutica, N.V. 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
US8785436B2 (en) * 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors

Also Published As

Publication number Publication date
KR20140019340A (ko) 2014-02-14
RU2013137814A (ru) 2015-03-10
WO2012104263A2 (en) 2012-08-09
JP2014507427A (ja) 2014-03-27
EP2670738A2 (en) 2013-12-11
CA2817841A1 (en) 2012-08-09
HK1187915A1 (en) 2014-04-17
WO2012104263A3 (en) 2012-09-27
CN103339117B (zh) 2015-05-27
CN103339117A (zh) 2013-10-02
US20120196863A1 (en) 2012-08-02
US8399459B2 (en) 2013-03-19
BR112013014610A2 (pt) 2016-09-20

Similar Documents

Publication Publication Date Title
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).
MX2013013692A (es) Halogenoalquil-1,3-oxazinas como inhibidores de beta secretasa 1 (bace1) y/o beta secretasa 2 (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).
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).
IN2012DN00766A (es)
MX2013014194A (es) 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).
PH12014501334A1 (en) Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
UA103272C2 (uk) 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
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
MX2013008056A (es) 1,4-oxazepinas como inhibidores de beta-secretasa 1 (bace1) y/o beta-secretasa 2 (bace2).
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.