JP2013503838A - 糖尿病の処置のためのｂａｃｅ２阻害剤としての２−アミノジヒドロ［１，３］チアジン - Google Patents

糖尿病の処置のためのｂａｃｅ２阻害剤としての２−アミノジヒドロ［１，３］チアジン Download PDF

Info

Publication number
JP2013503838A
JP2013503838A JP2012527352A JP2012527352A JP2013503838A JP 2013503838 A JP2013503838 A JP 2013503838A JP 2012527352 A JP2012527352 A JP 2012527352A JP 2012527352 A JP2012527352 A JP 2012527352A JP 2013503838 A JP2013503838 A JP 2013503838A
Authority
JP
Japan
Prior art keywords
phenyl
alkyl
halogen
fluoro
ethyl
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
JP2012527352A
Other languages
English (en)
Japanese (ja)
Inventor
ボーチャンプ，ジェレミー
ベナルドー，アニエス
ヒルペルト，ハンス
ミグリオリーニ，クリスティアーノ
リブレ，ウィリアム
ワン，ハイヤン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of JP2013503838A publication Critical patent/JP2013503838A/ja
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2012527352A 2009-09-11 2010-09-07 糖尿病の処置のためのｂａｃｅ２阻害剤としての２−アミノジヒドロ［１，３］チアジン Pending JP2013503838A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09170126.8 2009-09-11
EP09170126 2009-09-11
EP09172068 2009-10-02
EP09172068.0 2009-10-02
PCT/EP2010/063071 WO2011029803A1 (en) 2009-09-11 2010-09-07 2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes

Publications (1)

Publication Number Publication Date
JP2013503838A true JP2013503838A (ja) 2013-02-04

Family

ID=43086098

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012527352A Pending JP2013503838A (ja) 2009-09-11 2010-09-07 糖尿病の処置のためのｂａｃｅ２阻害剤としての２−アミノジヒドロ［１，３］チアジン

Country Status (10)

Country Link
US (3) US20110065695A1 (https=)
EP (1) EP2475658A1 (https=)
JP (1) JP2013503838A (https=)
CN (1) CN102482268B (https=)
AR (1) AR078163A1 (https=)
CA (1) CA2771374A1 (https=)
IN (1) IN2012DN01233A (https=)
SG (1) SG179034A1 (https=)
TW (1) TW201114765A (https=)
WO (1) WO2011029803A1 (https=)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2416603C9 (ru) 2005-10-25 2012-06-20 Сионоги Энд Ко., Лтд. Производные аминодигидротиазина
EP2147914B1 (en) * 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
WO2009151098A1 (ja) * 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
CN102186841A (zh) * 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
TWI488852B (zh) 2009-12-11 2015-06-21 Shionogi & Co 衍生物
JP5766198B2 (ja) 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
JP5816630B2 (ja) 2010-10-29 2015-11-18 塩野義製薬株式会社 ナフチリジン誘導体
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
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
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
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
WO2012147762A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 ピリジン誘導体およびそれを含有するｂａｃｅ１阻害剤
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
BR112014023384A8 (pt) 2012-03-20 2018-01-16 R Artis Dean inibidores de bace espirocíclicos de di-hidro-tiazina e di-hidro-oxazina, e composições e usos dos mesmos.
WO2013148130A1 (en) 2012-03-29 2013-10-03 Oklahoma Medical Research Foundation Inhibition of memapsin 1 cleavage in the treatment of diabetes
PE20150021A1 (es) 2012-05-24 2015-01-28 Hoffmann La Roche 5-amino[1,4]tiazinas como inhibidores de bace1
UA109868C2 (ru) 2012-06-20 2015-10-12 Ф. Хоффманн-Ля Рош Аг Соединения n-алкилтриазола как антагонисты лизофосфатидной кислоты (lpar)
WO2014059185A1 (en) 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
CA2902212C (en) 2013-03-01 2020-10-13 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
AP2015008716A0 (en) 2013-03-08 2015-09-30 Amgen Inc Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
CR20170426A (es) 2015-03-20 2017-10-23 Hoffmann La Roche Inhibidores de bace 1
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
WO2018112084A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
JP7149272B2 (ja) 2016-12-15 2022-10-06 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チアジン誘導体および使用方法
JP7149271B2 (ja) 2016-12-15 2022-10-06 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１，４－チアジンジオキシドおよび１，２，４－チアジアジンジオキシド誘導体ならびに使用方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007049532A1 (ja) * 2005-10-25 2007-05-03 Shionogi & Co., Ltd. アミノジヒドロチアジン誘導体

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2151435A4 (en) * 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
EP2147914B1 (en) * 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
AU2009216825A1 (en) * 2008-02-18 2009-08-27 F. Hoffmann-La Roche Ag 4, 5-dihydro-oxazol-2-yl amine derivatives
WO2010063718A1 (en) * 2008-12-02 2010-06-10 ETH Zürich Screening assay for metabolic disease therapeuticals

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007049532A1 (ja) * 2005-10-25 2007-05-03 Shionogi & Co., Ltd. アミノジヒドロチアジン誘導体

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
JPN6013045806; Ｊ．　Ｍｏｌ．　Ｂｉｏｌ． Ｖｏｌ．３５５, 2006, ｐ．２４９-２６１ *
JPN6013045807; Ｂｉｏｏｒｇ．　Ｍｅｄ．　Ｃｈｅｍ．　Ｌｅｔｔ． Ｖｏｌ．１８，　Ｉｓｓｕｅ　１１, 2008, ｐ．３２３６-３２４１ *
JPN6013045808; Ｂｉｏｏｒｇ．　Ｍｅｄ．　Ｃｈｅｍ．　Ｌｅｔｔ． Ｖｏｌ．１７．　Ｉｓｓｕｅ　１９, 2007, ｐ．５３５３-５３５６ *
JPN6013045810; Ｕｌｔｒａｓｔｒｕｃｔｕａｌ　Ｐａｔｈｏｌｏｇｙ Ｖｏｌ．３２, 2008, ｐ．２４６-２５１ *
JPN6013045811; Ｂｉｏｏｒｇ．　Ｍｅｄ．　Ｃｈｅｍ．　Ｌｅｔｔ． Ｖｏｌ．１９，　Ｉｓｓｕｅ　１, 200901, ｐ．２６４-２７４ *

Also Published As

Publication number Publication date
EP2475658A1 (en) 2012-07-18
US20110065695A1 (en) 2011-03-17
US20140221360A1 (en) 2014-08-07
AR078163A1 (es) 2011-10-19
CN102482268B (zh) 2014-11-26
TW201114765A (en) 2011-05-01
US20130096107A1 (en) 2013-04-18
CN102482268A (zh) 2012-05-30
CA2771374A1 (en) 2011-03-17
SG179034A1 (en) 2012-04-27
IN2012DN01233A (https=) 2015-05-15
WO2011029803A1 (en) 2011-03-17

Similar Documents

Publication Publication Date Title
JP2013503838A (ja) 糖尿病の処置のためのｂａｃｅ２阻害剤としての２−アミノジヒドロ［１，３］チアジン
JP5479575B2 (ja) Ｂａｃｅ２インヒビターとしての使用のためのジヒドロピリミジノン
KR101437750B1 (ko) 아미노 옥사진 유도체
RU2597308C2 (ru) N-[3-(5-амино-3,3а,7,7а-тетрагидро-1н-2,4-диокса-6-аза-инден-7-ил)-фенил]-амиды в качестве ингибиторов васе1 и(или) васе2
CN103429590B (zh) 作为bace1和/或bace2抑制剂的1，4硫氮杂*/砜
JP2013502393A (ja) ３−アミノ−５−フェニル−５，６−ジヒドロ−２ｈ−［１，４］オキサジン誘導体
CN103068806A (zh) 1,4,5,6-四氢-嘧啶-2-基胺化合物
KR20140048952A (ko) Bace1 및/또는 bace2 억제제로서의 사이클로프로필-융합-1,3-티아제핀
EP2611441A1 (en) Bace inhibitors for use in the treatment of diabetes
HK1190701B (en) 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
HK1181302A (en) Bace inhibitors for use in the treatment of diabetes
HK1193593A (en) Cyclopropyl-fused-1,3-thiazepines as bace 1 and/or bace 2 inhibitors

Legal Events

Date Code Title Description
A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130917

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20131216

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140722

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20141021

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150203

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20150305

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20150714