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

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/041,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/061,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hematology (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
EP09170126.8 2009-09-11
EP09170126 2009-09-11
EP09172068.0 2009-10-02
EP09172068 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 (h)
EP (1) EP2475658A1 (h)
JP (1) JP2013503838A (h)
CN (1) CN102482268B (h)
AR (1) AR078163A1 (h)
CA (1) CA2771374A1 (h)
IN (1) IN2012DN01233A (h)
SG (1) SG179034A1 (h)
TW (1) TW201114765A (h)
WO (1) WO2011029803A1 (h)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2597087B1 (en) 2005-10-25 2016-03-30 Shionogi&Co., Ltd. Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors
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
EP2360155A4 (en) * 2008-10-22 2012-06-20 Shionogi & Co 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
CN102834384A (zh) 2009-12-11 2012-12-19 盐野义制药株式会社 *嗪衍生物
US8927721B2 (en) 2010-10-29 2015-01-06 Shionogi & Co., Ltd. Naphthyridine derivative
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-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
CA2832473A1 (en) 2011-04-13 2012-10-18 Merck Sharp & Dohme Corp. 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions, and their use
EP2703399A4 (en) 2011-04-26 2014-10-15 Shionogi & Co OXAZINE DERIVATIVE AND BACE-1 HEMMER THEREOF
CN103649082A (zh) 2011-04-26 2014-03-19 盐野义制药株式会社 吡啶衍生物和含有该吡啶衍生物的bace1抑制剂
US8927535B2 (en) 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
WO2013028670A1 (en) 2011-08-22 2013-02-28 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
JP2015514073A (ja) 2012-03-20 2015-05-18 エラン ファーマシューティカルズ, リミテッド・ライアビリティ・カンパニー スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンbace阻害剤、ならびにその組成物および使用
WO2013148130A1 (en) 2012-03-29 2013-10-03 Oklahoma Medical Research Foundation Inhibition of memapsin 1 cleavage in the treatment of diabetes
CA2872179A1 (en) 2012-05-24 2013-11-28 F. Hoffmann-La Roche Ag 5-amino[1,4]thiazines as bace 1 inhibitors
EP2864300A1 (en) 2012-06-20 2015-04-29 F. Hoffmann-La Roche AG N-alkyltriazole compounds as lpar antagonists
US9556135B2 (en) 2012-10-12 2017-01-31 Amgen, Inc. Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
US9725469B2 (en) 2012-11-15 2017-08-08 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
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
EP3177618A1 (en) 2014-08-08 2017-06-14 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
AU2016236402B2 (en) 2015-03-20 2019-08-01 F. Hoffmann-La Roche Ag BACE1 inhibitors
US10246429B2 (en) 2015-08-06 2019-04-02 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
US10889579B2 (en) 2016-12-15 2021-01-12 Amgen Inc. Thiazine derivatives as β-secretase inhibitors and methods of use
MX386618B (es) 2016-12-15 2025-03-19 Amgen Inc Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso.
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
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
AU2017376445B2 (en) 2016-12-15 2021-09-30 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2597087B1 (en) * 2005-10-25 2016-03-30 Shionogi&Co., Ltd. Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors
AU2008245082B8 (en) * 2007-04-24 2012-09-13 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
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
WO2009103626A1 (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

Also Published As

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

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20160908