CA2771374A1 - 2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes - Google Patents

2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes Download PDF

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Publication number
CA2771374A1
CA2771374A1 CA2771374A CA2771374A CA2771374A1 CA 2771374 A1 CA2771374 A1 CA 2771374A1 CA 2771374 A CA2771374 A CA 2771374A CA 2771374 A CA2771374 A CA 2771374A CA 2771374 A1 CA2771374 A1 CA 2771374A1
Authority
CA
Canada
Prior art keywords
phenyl
alkyl
halogen
fluoro
formula
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.)
Abandoned
Application number
CA2771374A
Other languages
English (en)
French (fr)
Inventor
Jeremy Beauchamp
Agnes Benardeau
Hans Hilpert
Cristiano Migliorini
William Riboulet
Haiyan Wang
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 CA2771374A1 publication Critical patent/CA2771374A1/en
Abandoned 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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2771374A 2009-09-11 2010-09-07 2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes Abandoned CA2771374A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09170126 2009-09-11
EP09170126.8 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
CA2771374A1 true CA2771374A1 (en) 2011-03-17

Family

ID=43086098

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2771374A Abandoned CA2771374A1 (en) 2009-09-11 2010-09-07 2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes

Country Status (10)

Country Link
US (3) US20110065695A1 (2)
EP (1) EP2475658A1 (2)
JP (1) JP2013503838A (2)
CN (1) CN102482268B (2)
AR (1) AR078163A1 (2)
CA (1) CA2771374A1 (2)
IN (1) IN2012DN01233A (2)
SG (1) SG179034A1 (2)
TW (1) TW201114765A (2)
WO (1) WO2011029803A1 (2)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2628074C (en) 2005-10-25 2014-01-14 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
US8653067B2 (en) * 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
JP5383484B2 (ja) * 2007-04-24 2014-01-08 塩野義製薬株式会社 環式基で置換されたアミノジヒドロチアジン誘導体
KR101324426B1 (ko) * 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
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
MX2012006491A (es) 2009-12-11 2012-07-03 Shionogi & Co Derivados de oxazina.
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
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
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
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
BR112013026341A2 (pt) 2011-04-13 2019-09-24 Merck Sharp & Dohe Corp composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia
US8883779B2 (en) 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
US20140235626A1 (en) 2011-04-26 2014-08-21 Shionogi & Co., Ltd. Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them
US8927535B2 (en) * 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
CN103874496A (zh) 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途
EP2827857A4 (en) 2012-03-20 2016-03-30 Elan Pharm Inc SPIROCYCLIC DIHYDRO-THIAZINE AND INHIBITORS OF BACE DIHYDRO-OXAZINE AND COMPOSITIONS AND USES THEREOF
WO2013148130A1 (en) 2012-03-29 2013-10-03 Oklahoma Medical Research Foundation Inhibition of memapsin 1 cleavage in the treatment of diabetes
UA113438C2 (xx) * 2012-05-24 2017-01-25 5-аміно$1,4]тіазини як інгібітори бета-секретази 1
JP2015520202A (ja) 2012-06-20 2015-07-16 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｌｐａｒ拮抗薬としてのｎ−アルキルトリアゾール化合物
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
WO2014134341A1 (en) 2013-03-01 2014-09-04 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
MX374512B (es) 2013-03-08 2025-03-06 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y métodos de uso.
CN106795147B (zh) 2014-08-08 2020-09-22 美国安进公司 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法
EP3271355B1 (en) 2015-03-20 2020-07-29 H. Hoffnabb-La Roche Ag Bace1 inhibitors
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
CA3047290A1 (en) 2016-12-15 2018-06-21 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
AU2017376441B2 (en) 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
MX394391B (es) 2016-12-15 2025-03-24 Amgen Inc Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso.

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2628074C (en) * 2005-10-25 2014-01-14 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
JP5383484B2 (ja) * 2007-04-24 2014-01-08 塩野義製薬株式会社 環式基で置換されたアミノジヒドロチアジン誘導体
US8653067B2 (en) * 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
EP2245019B1 (en) * 2008-02-18 2012-11-14 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

Also Published As

Publication number Publication date
SG179034A1 (en) 2012-04-27
IN2012DN01233A (2) 2015-05-15
CN102482268A (zh) 2012-05-30
JP2013503838A (ja) 2013-02-04
AR078163A1 (es) 2011-10-19
TW201114765A (en) 2011-05-01
US20110065695A1 (en) 2011-03-17
US20140221360A1 (en) 2014-08-07
WO2011029803A1 (en) 2011-03-17
US20130096107A1 (en) 2013-04-18
EP2475658A1 (en) 2012-07-18
CN102482268B (zh) 2014-11-26

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20160908