AU2012243329B2 - 5-substituted iminothiazines and their mono-and dioxides as BACE inhibitors,compositions,and their use - Google Patents

5-substituted iminothiazines and their mono-and dioxides as BACE inhibitors,compositions,and their use Download PDF

Info

Publication number
AU2012243329B2
AU2012243329B2 AU2012243329A AU2012243329A AU2012243329B2 AU 2012243329 B2 AU2012243329 B2 AU 2012243329B2 AU 2012243329 A AU2012243329 A AU 2012243329A AU 2012243329 A AU2012243329 A AU 2012243329A AU 2012243329 B2 AU2012243329 B2 AU 2012243329B2
Authority
AU
Australia
Prior art keywords
disease
compound
mmol
pct
group
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.)
Ceased
Application number
AU2012243329A
Other languages
English (en)
Other versions
AU2012243329A1 (en
AU2012243329A8 (en
Inventor
Chad Edward BENNETT
Duane A. Burnett
Jared N. Cumming
Eric J. Gilbert
Xuanjia Peng
Jack D. Scott
Andrew W. Stamford
Wen-Lian Wu
Younong Yu
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.)
Merck Sharp & Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp & Dohme LLC
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 Merck Sharp and Dohme Ltd, Merck Sharp & Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Publication of AU2012243329A1 publication Critical patent/AU2012243329A1/en
Publication of AU2012243329A8 publication Critical patent/AU2012243329A8/en
Application granted granted Critical
Publication of AU2012243329B2 publication Critical patent/AU2012243329B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other 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
    • A61K31/54—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/10—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 carbon chain containing aromatic 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
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2012243329A 2011-04-13 2012-04-12 5-substituted iminothiazines and their mono-and dioxides as BACE inhibitors,compositions,and their use Ceased AU2012243329B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161475215P 2011-04-13 2011-04-13
US61/475,215 2011-04-13
US201161503254P 2011-06-30 2011-06-30
US61/503,254 2011-06-30
CN2012000435 2012-04-05
CNPCT/CN2012/000435 2012-04-05
PCT/CN2012/000497 WO2012139425A1 (en) 2011-04-13 2012-04-12 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use

Publications (3)

Publication Number Publication Date
AU2012243329A1 AU2012243329A1 (en) 2013-10-17
AU2012243329A8 AU2012243329A8 (en) 2013-11-21
AU2012243329B2 true AU2012243329B2 (en) 2015-09-17

Family

ID=50086365

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012243329A Ceased AU2012243329B2 (en) 2011-04-13 2012-04-12 5-substituted iminothiazines and their mono-and dioxides as BACE inhibitors,compositions,and their use

Country Status (10)

Country Link
US (1) US9499502B2 (enExample)
EP (1) EP2697210B1 (enExample)
JP (1) JP2014514302A (enExample)
CN (1) CN103596939A (enExample)
AU (1) AU2012243329B2 (enExample)
BR (1) BR112013026341A2 (enExample)
CA (1) CA2832473A1 (enExample)
MX (1) MX2013011947A (enExample)
RU (1) RU2013150349A (enExample)
WO (1) WO2012139425A1 (enExample)

Families Citing this family (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine 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
WO2012138734A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
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
JP6251249B2 (ja) * 2012-05-24 2017-12-20 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｂａｃｅ１阻害薬としての５−アミノ［１，４］チアジン類
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
US9447085B2 (en) 2012-12-14 2016-09-20 Merck Sharp & Dohme Corp. Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use
CN104870000A (zh) * 2012-12-20 2015-08-26 默沙东公司 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途
US9580396B2 (en) 2012-12-21 2017-02-28 Merck Sharp & Dohme Corp. C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
US9309263B2 (en) 2013-01-29 2016-04-12 Amgen Inc. Fused multi-cyclic sulfone compounds as inhibitors of beta-secretase and methods of use thereof
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
EP2964644B1 (en) 2013-03-08 2018-12-26 Amgen, Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
WO2014150340A1 (en) 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiadiazine compounds as bace inhibitors, compositions, and their use
US9422255B2 (en) 2013-03-15 2016-08-23 Merck Sharp & Dohme Corp. S-imino-S-oxo-iminothiazine compounds as BACE inhibitors, compositions, and their use
US9453034B2 (en) * 2013-03-15 2016-09-27 Merck Sharp & Dohme Corp. C2-azaspiro iminothiazine dioxides as BACE inhibitors, compositions, and their use
US9096615B2 (en) 2013-07-30 2015-08-04 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
EP3083575B1 (en) 2013-12-18 2021-11-03 Merck Sharp & Dohme Corp. C-6 spirocarbocyclic iminothiadiazine dioxides as bace inhibitors, compositions, and their use
US9745324B2 (en) 2013-12-18 2017-08-29 Merck Sharp & Dohme Corp. Iminothiadiazepane dioxide compounds as BACE inhibitors, compositions, and their use
EP2918171A1 (en) * 2014-03-14 2015-09-16 University of Vienna Novel plant growth regulators and their use in modulating organ number
JP6111002B1 (ja) 2014-04-10 2017-04-05 ファイザー・インク ２−アミノ−６−メチル−４，４ａ，５，６−テトラヒドロピラノ［３，４−ｄ］［１，３］チアジン−８ａ（８Ｈ）−イル−１，３−チアゾール−４−イルアミド
WO2015187437A1 (en) 2014-06-02 2015-12-10 Merck Sharp & Dohme Corp. C2-carbocyclic iminothiazine dioxides as bace inhibitors, compositions, and their use
CN106661053B (zh) 2014-07-25 2019-07-12 豪夫迈·罗氏有限公司 吡啶基-三氮杂二环类化合物
EP3191447B1 (en) 2014-09-12 2019-05-01 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
WO2016118404A1 (en) 2015-01-20 2016-07-28 Merck Sharp & Dohme Corp. Iminothiadiazine dioxides bearing an amine-linked substituent as bace inhibitors, compositions, and their use
CA2979113A1 (en) * 2015-03-20 2016-09-29 F. Hoffmann-La Roche Ag Bace1 inhibitors
JP6765681B2 (ja) * 2015-04-21 2020-10-07 オールジェネシス バイオセラピューティクス インコーポレイテッド Ｂａｃｅ１阻害剤としての化合物およびそれらの使用
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
WO2017051303A1 (en) 2015-09-24 2017-03-30 Pfizer Inc. Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors
JP2018531923A (ja) 2015-09-24 2018-11-01 ファイザー・インク Ｎ−［２−（２−アミノ−６，６−二置換−４，４ａ，５，６−テトラヒドロピラノ［３，４−ｄ］［１，３］チアジン−８ａ（８Ｈ）−イル）−１，３−チアゾール−４−イル］アミド
US20170107216A1 (en) 2015-10-19 2017-04-20 Incyte Corporation Heterocyclic compounds as immunomodulators
MD3377488T2 (ro) 2015-11-19 2023-02-28 Incyte Corp Compuși heterociclici ca imunomodulatori
WO2017095759A1 (en) 2015-12-04 2017-06-08 Merck Sharp & Dohme Corp. C5-c6-carbocyclic fused iminothiadiazine dioxides as bace inhibitors, compositions, and their use
ES2916874T3 (es) 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
CA3009474A1 (en) 2015-12-22 2017-06-29 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2906460T3 (es) 2016-05-06 2022-04-18 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3464279B1 (en) 2016-05-26 2021-11-24 Incyte Corporation Heterocyclic compounds as immunomodulators
SG11201811414TA (en) 2016-06-20 2019-01-30 Incyte Corp Heterocyclic compounds as immunomodulators
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
US20180057486A1 (en) 2016-08-29 2018-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
MX387729B (es) * 2016-12-15 2025-03-18 Amgen Inc Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso.
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.
AU2017376445B2 (en) 2016-12-15 2021-09-30 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
MX388697B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso.
AU2017376441B2 (en) 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
US10308644B2 (en) 2016-12-22 2019-06-04 Incyte Corporation Heterocyclic compounds as immunomodulators
EP4223369A1 (en) 2016-12-22 2023-08-09 Incyte Corporation Immunomodulator compounds and methods of use
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
AU2018346597B2 (en) 2017-10-06 2023-07-13 Forma Therapeutics, Inc. Inhibiting Ubiquitin Specific Peptidase 30
EP3728234B1 (en) * 2017-12-21 2025-05-14 F. Hoffmann-La Roche AG Radiolabeled compounds
CN112135825A (zh) 2018-03-13 2020-12-25 夏尔人类遗传性治疗公司 血浆激肽释放酶抑制剂及其用途
SMT202300065T1 (it) 2018-03-30 2023-05-12 Incyte Corp Composti eterociclici come immunomodulatori
BR112020021728A2 (pt) 2018-04-27 2021-01-26 Shionogi & Co., Ltd. derivados de tetra-hidropiranooxazina tendo atividade inibitória de bace1 seletiva
CN112752756B (zh) 2018-05-11 2024-06-25 因赛特公司 作为PD-L1免疫调节剂的四氢-咪唑并[4,5-c]吡啶衍生物
CN110467611B (zh) * 2018-05-11 2022-09-27 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
IL278291B2 (en) 2018-05-17 2023-10-01 Forma Therapeutics Inc Condensed bicyclic compounds are useful as ubiquitin-specific peptidase 30 inhibitors
CN108997328B (zh) * 2018-09-06 2021-06-08 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
CN109180671A (zh) * 2018-09-21 2019-01-11 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
CN109180672A (zh) * 2018-09-29 2019-01-11 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
EP4218934B1 (en) 2018-10-05 2025-06-18 Forma Therapeutics, Inc. Inhibiting ubiquitin-specific protease 30 (usp30)
CN109796447B (zh) * 2019-01-07 2020-03-13 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途
TW202115059A (zh) 2019-08-09 2021-04-16 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之鹽
EP4017850A1 (en) * 2019-08-21 2022-06-29 Kalvista Pharmaceuticals Limited Enzyme inhibitors
CN114728962B (zh) 2019-09-18 2025-09-19 武田药品工业有限公司 血浆激肽释放酶抑制剂及其用途
WO2021055589A1 (en) 2019-09-18 2021-03-25 Shire Human Genetic Therapies, Inc. Heteroaryl plasma kallikrein inhibitors
JP7559059B2 (ja) 2019-09-30 2024-10-01 インサイト・コーポレイション 免疫調節剤としてのピリド［３，２－ｄ］ピリミジン化合物
EP4058461A1 (en) 2019-11-11 2022-09-21 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
WO2022089598A1 (zh) * 2020-10-30 2022-05-05 杭州拉林智能科技有限公司 黄酮苷-有机胺类神经激动剂复盐化合物及其制备方法和应用
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
IL302590A (en) 2020-11-06 2023-07-01 Incyte Corp Process for preparing PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
CN113073098B (zh) * 2021-02-20 2024-08-20 北京理工大学 抑制BACE1基因表达的siRNA修饰物及其应用
CN113105318B (zh) * 2021-02-23 2022-05-20 中山大学 一种2,2-二氟环丁烷-1-羧酸的制备方法及应用
CA3256688A1 (en) 2022-04-28 2025-04-22 Daiichi Sankyo Company, Limited BENZOTRIAZOLE COMPOUND
CN119080651B (zh) * 2024-10-31 2025-02-07 汕头大学 一种可见光协同钴催化制备烯丙基砜类化合物的方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006017836A2 (en) * 2004-08-06 2006-02-16 Janssen Pharmaceutica, N.V. 2-amino-quinazoline derivatives useful as inhibitors of beta-secretase (bace)

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5534520A (en) 1990-04-10 1996-07-09 Fisher; Abraham Spiro compounds containing five-membered rings
WO2002058691A1 (en) * 2001-01-23 2002-08-01 Neurosearch A/S Use of non-competitive and selective glur5 antagonists as glutamate receptor modulating compounds
EP1608619A1 (en) * 2003-03-21 2005-12-28 Eli Lilly And Company Muscarinic agonists
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) * 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US20090221579A1 (en) * 2004-10-15 2009-09-03 Jeffrey Scott Albert Substituted Amino-Compounds and Uses Thereof
ES2537898T3 (es) * 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
TW200808751A (en) * 2006-04-13 2008-02-16 Astrazeneca Ab New compounds
CA2653650A1 (en) 2006-06-12 2007-12-21 Schering Corporation Heterocyclic aspartyl protease inhibitors
AU2008245082B8 (en) 2007-04-24 2012-09-13 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
CA2695543A1 (en) 2007-08-06 2009-02-12 Schering Corporation Gamma secretase modulators
AU2009239536C1 (en) 2008-04-22 2012-12-13 Merck Sharp & Dohme Corp. Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20110065695A1 (en) * 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 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
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
CN102686584A (zh) 2009-11-13 2012-09-19 盐野义制药株式会社 具有氨基连接基的氨基噻嗪或氨基噁嗪衍生物
US20120245154A1 (en) 2009-12-09 2012-09-27 Shionogi & Co., Ltd. Substituted aminothiazine derivative
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
UA103272C2 (uk) 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
WO2011077726A1 (ja) 2009-12-24 2011-06-30 塩野義製薬株式会社 ４－アミノ－１，３－チアジンまたはオキサジン誘導体
US20120277244A1 (en) 2009-12-31 2012-11-01 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
US8673894B2 (en) 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
US20110281894A1 (en) 2010-05-12 2011-11-17 Astrazeneca Ab Hemifumarate salt
EA201291366A1 (ru) 2010-06-09 2013-04-30 Янссен Фармацевтика Нв Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace)
AR081587A1 (es) 2010-06-09 2012-10-03 Janssen Pharmaceutica Nv DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE)
CN102666507B (zh) 2010-07-13 2014-09-17 诺华股份有限公司 噁嗪衍生物及其在治疗神经病症中的用途
US8815881B2 (en) 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006017836A2 (en) * 2004-08-06 2006-02-16 Janssen Pharmaceutica, N.V. 2-amino-quinazoline derivatives useful as inhibitors of beta-secretase (bace)

Also Published As

Publication number Publication date
WO2012139425A1 (en) 2012-10-18
RU2013150349A (ru) 2015-05-20
US20140128382A1 (en) 2014-05-08
BR112013026341A2 (pt) 2019-09-24
CA2832473A1 (en) 2012-10-18
EP2697210B1 (en) 2017-03-01
EP2697210A4 (en) 2014-09-17
US9499502B2 (en) 2016-11-22
AU2012243329A1 (en) 2013-10-17
CN103596939A (zh) 2014-02-19
AU2012243329A8 (en) 2013-11-21
JP2014514302A (ja) 2014-06-19
EP2697210A1 (en) 2014-02-19
MX2013011947A (es) 2014-01-16

Similar Documents

Publication Publication Date Title
EP2697210B1 (en) 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions, and their use
EP2694489B1 (en) C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2485590B1 (en) Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
EP2931284B1 (en) Bace inhibitors of iminothiadiazine dioxides
EP2694521B1 (en) Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
AU2012298983A1 (en) 2-spiro-substituted iminothiazines and their mono-and dioxides as BACE inhibitors, compositions and their use
EP3043802B1 (en) C5-spiro iminothiazine dioxides as bace inhibitors, compositions, and their use
AU2013363151A1 (en) C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors
EP2485591A1 (en) Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2968357A1 (en) S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
WO2014099788A9 (en) C5-spiro iminothiadiazine dioxides as bace inhibitors
EP2908824A1 (en) Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2014099768A1 (en) C6-azaspiro iminothiadiazine dioxides as bace inhibitors
WO2015094930A1 (en) C-6 spirocarbocyclic iminothiadiazine dioxides as bace inhibitors, compositions, and their use
EP2968353A1 (en) C2-azaspiro iminothiazine dioxides as bace inhibitors
EP3191447B1 (en) S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
KR20140022877A (ko) Bace 억제제로서의 5-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물, 및 그의 용도
TW201311680A (zh) 作為ｂａｃｅ抑制劑之５－經取代之亞胺噻□及其單一及二氧化物、組合物及其用途

Legal Events

Date Code Title Description
TH Corrigenda

Free format text: IN VOL 27 , NO 40 , PAGE(S) 5847 UNDER THE HEADING PCT APPLICATIONS THAT HAVE ENTERED THE NATIONAL PHASE - NAME INDEX UNDER THE NAME SCHERING CORPORATION, APPLICATION NO. 2012243329, UNDER INID (71) CORRECT THE APPLICANT NAME TO MERCK SHARP & DOHME CORP.

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired