IN2012DN03043A - - Google Patents

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Publication number: IN2012DN03043A
Authority: IN; India
Prior art keywords: present; bace1; oxazin; difluoro; alzheimer
Prior art date: 2009-12-11

Application number

Other languages

English (en)

Inventor

David Banner

Wolfgang Guba

Hans Hilpert

Harald Mauser

Alexander V Mayweg

Robert Narquizian

Emmanuel Pinard

Eoin Power

Mark Rogers-Evans

Thomas Woltering

Wolfgang Wostl

Original Assignee

Hoffmann La Roche

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.)

2009-12-11

Filing date

2010-12-06

Publication date

2015-07-31

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43585547&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IN2012DN03043(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2010-12-06 Application filed by Hoffmann La Roche, Siena Biotech Spa filed Critical Hoffmann La Roche

2015-07-31 Publication of IN2012DN03043A publication Critical patent/IN2012DN03043A/en

Links

208000024827 Alzheimer disease Diseases 0.000 abstract 1
102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
102100021277 Beta-secretase 2 Human genes 0.000 abstract 1
101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
101000894883 Homo sapiens Beta-secretase 2 Proteins 0.000 abstract 1
239000013543 active substance Substances 0.000 abstract 1
150000001875 compounds Chemical class 0.000 abstract 1
230000002401 inhibitory effect Effects 0.000 abstract 1
238000004519 manufacturing process Methods 0.000 abstract 1
239000008194 pharmaceutical composition Substances 0.000 abstract 1
238000011321 prophylaxis Methods 0.000 abstract 1
230000001225 therapeutic effect Effects 0.000 abstract 1
208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1

Classifications

- 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
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
- C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- 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
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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
- 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
- C07D413/12—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 chain containing hetero atoms as chain links

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Neurology (AREA)
Diabetes (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Orthopedic Medicine & Surgery (AREA)
Physical Education & Sports Medicine (AREA)
Immunology (AREA)
Hematology (AREA)
Rheumatology (AREA)
Pain & Pain Management (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Emergency Medicine (AREA)
Psychology (AREA)
Hospice & Palliative Care (AREA)
Psychiatry (AREA)
Vascular Medicine (AREA)
Urology & Nephrology (AREA)
Endocrinology (AREA)
Obesity (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

IN3043DEN2012 2009-12-11 2010-12-06 IN2012DN03043A (fr)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
EP09178983		2009-12-11
PCT/EP2010/068912 WO2011069934A1 (fr)	2009-12-11	2010-12-06	2-amino-5,5-difluoro-5,6-dihydro-4h-oxazines en tant qu'inhibiteurs de bace 1 et/ou bace 2

Publications (1)

Publication Number	Publication Date
IN2012DN03043A true IN2012DN03043A (fr)	2015-07-31

Family

ID=43585547

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IN3043DEN2012 IN2012DN03043A (fr)	2009-12-11	2010-12-06

Country Status (26)

Country	Link
US (1)	US8389513B2 (fr)
EP (1)	EP2509965A1 (fr)
JP (1)	JP5584778B2 (fr)
KR (1)	KR101506773B1 (fr)
CN (1)	CN102712609A (fr)
AR (1)	AR079327A1 (fr)
AU (1)	AU2010330031B2 (fr)
BR (1)	BR112012013175A2 (fr)
CA (1)	CA2776727C (fr)
CL (1)	CL2012001464A1 (fr)
CO (1)	CO6541656A2 (fr)
CR (1)	CR20120262A (fr)
EC (1)	ECSP12011961A (fr)
IL (1)	IL219107A (fr)
IN (1)	IN2012DN03043A (fr)
MA (1)	MA34779B1 (fr)
MX (1)	MX2012006493A (fr)
MY (1)	MY169962A (fr)
NZ (1)	NZ599008A (fr)
PE (1)	PE20121500A1 (fr)
PH (1)	PH12012500619A1 (fr)
RU (1)	RU2515221C2 (fr)
SG (1)	SG181610A1 (fr)
TW (1)	TWI487704B (fr)
UA (1)	UA103272C2 (fr)
WO (1)	WO2011069934A1 (fr)

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EP2689780A1 (fr)	2007-04-24	2014-01-29	Shionogi & Co., Ltd.	Intermédiaires de dérivés d'aminodihydrothiazine substitués avec un groupe cyclique
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UY32799A (es)	2009-07-24	2011-02-28	Novartis Ag	Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
EP2485591B1 (fr)	2009-10-08	2016-03-23	Merck Sharp & Dohme Corp.	Composés de type dioxyde d'imino-thiadiazine utilisés en tant qu'inhibiteurs de bace, compositions en contenant et leur utilisation
EP2485920B1 (fr)	2009-10-08	2016-04-27	Merck Sharp & Dohme Corp.	Composés hétérocycliques iminopentafluorosoufrés en tant qu'inhibiteurs de bace-1, compositions et leur utilisation
UA108363C2 (uk)	2009-10-08	2015-04-27		Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8557826B2 (en)	2009-10-08	2013-10-15	Merck Sharp & Dohme Corp.	Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
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TWI547482B (zh)	2011-01-25	2016-09-01	陶氏農業科學公司	增加可回收之3-氯-4,5,6-三氟-2-氰吡啶之量的改良方法
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
PH12013501805A1 (en)	2011-03-09	2013-11-18	Janssen Pharmaceutica Nv	3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
US9145426B2 (en)	2011-04-07	2015-09-29	Merck Sharp & Dohme Corp.	Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
EP2694489B1 (fr)	2011-04-07	2017-09-06	Merck Sharp & Dohme Corp.	Composés de dioxyde de thiadiazine condensés avec des dérivés oxacycliques en c5-c6 comme inhibiteurs de bace, compositions, et utilisation use
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RU2013150349A (ru)	2011-04-13	2015-05-20	Мерк Шарп И Доум Корп.	5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение
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KR20150023450A (ko) *	2012-06-26	2015-03-05	에프. 호프만-라 로슈 아게	Bace1 억제제로서의 다이플루오로-헥사하이드로-사이클로펜타옥사진일 및 다이플루오로-헥사하이드로-벤조옥사진일
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JP6389830B2 (ja) *	2013-03-01	2018-09-12	アムジエン・インコーポレーテツド	ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法
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2010
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- 2010-12-06 EP EP10785437A patent/EP2509965A1/fr not_active Withdrawn
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Publication number	Publication date
US8389513B2 (en)	2013-03-05
CA2776727A1 (fr)	2011-06-16
AU2010330031A1 (en)	2012-06-07
ECSP12011961A (es)	2012-07-31
SG181610A1 (en)	2012-07-30
RU2515221C2 (ru)	2014-05-10
JP2013513563A (ja)	2013-04-22
BR112012013175A2 (pt)	2019-09-24
PE20121500A1 (es)	2012-11-05
CR20120262A (es)	2012-07-27
NZ599008A (en)	2013-08-30
IL219107A0 (en)	2012-06-28
AR079327A1 (es)	2012-01-18
MA34779B1 (fr)	2014-01-02
KR101506773B1 (ko)	2015-03-27
CL2012001464A1 (es)	2014-03-07
JP5584778B2 (ja)	2014-09-03
CO6541656A2 (es)	2012-10-16
KR20120104598A (ko)	2012-09-21
PH12012500619A1 (en)	2012-10-22
EP2509965A1 (fr)	2012-10-17
MX2012006493A (es)	2012-07-03
CN102712609A (zh)	2012-10-03
CA2776727C (fr)	2016-05-31
UA103272C2 (uk)	2013-09-25
AU2010330031B2 (en)	2013-06-20
TW201124408A (en)	2011-07-16
IL219107A (en)	2015-10-29
TWI487704B (zh)	2015-06-11
US20110144097A1 (en)	2011-06-16
WO2011069934A1 (fr)	2011-06-16
MY169962A (en)	2019-06-19
RU2012126989A (ru)	2014-01-20

Publication	Publication Date	Title
IN2012DN03043A (fr)	2015-07-31
IN2012DN00766A (fr)	2015-06-26
PH12013502090A1 (en)	2018-03-21	1,3 oxazines as bace1 and/or bace2 inhibitors
MX2013007558A (es)	2013-08-21	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).
PH12013502156A1 (en)	2014-01-06	1,3-oxazines as bace1 and/or bace2 inhibitors
WO2012104263A3 (fr)	2012-09-27	1,4-oxazines en tant qu'inhibiteurs de bace1 et/ou bace2
MX2013008478A (es)	2013-08-12	1, 4 riazepinas/sulfonas como inhibidores de beta secretasa 1 (base1) y/o beta secretasa 2 (bace2).
MX2013014007A (es)	2014-03-12	[1,3] oxazinas.
PH12013502316A1 (en)	2015-09-04	Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors
MX2013008213A (es)	2013-08-09	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).
PH12013502262A1 (en)	2016-01-22	Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors
MX2013014194A (es)	2014-03-21	1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).
MX2014003408A (es)	2014-04-10	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).
PH12014501334A1 (en)	2014-09-15	Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
PH12014502541A1 (en)	2015-01-21	5-amino [1,4] thiazines as bace 1 inhibitors
PH12014502623A1 (en)	2015-01-21	Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors
MX2013002398A (es)	2013-04-03	Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes.
MX2016006906A (es)	2016-08-17	5-aril-1-imino-1-oxo-[1,2,4]tiadiazinas.