JP2016501827A - Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 - Google Patents
Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 Download PDFInfo
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- JP2016501827A JP2016501827A JP2015516335A JP2015516335A JP2016501827A JP 2016501827 A JP2016501827 A JP 2016501827A JP 2015516335 A JP2015516335 A JP 2015516335A JP 2015516335 A JP2015516335 A JP 2015516335A JP 2016501827 A JP2016501827 A JP 2016501827A
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- 0 CC(CCCC(CCCC1)C2(*)*=C(N)O*C2(C)*)C1IC1CCCCCC1 Chemical compound CC(CCCC(CCCC1)C2(*)*=C(N)O*C2(C)*)C1IC1CCCCCC1 0.000 description 19
- YOZGHSJJOGIXCV-SAHWJRBASA-N CC(C)(C)OC(N(C(OC(C)(C)C)=O)C(O[C@H](CF)[C@@H]1OCC2)=N[C@]12c(cc(cc1)[N+]([O-])=O)c1F)=O Chemical compound CC(C)(C)OC(N(C(OC(C)(C)C)=O)C(O[C@H](CF)[C@@H]1OCC2)=N[C@]12c(cc(cc1)[N+]([O-])=O)c1F)=O YOZGHSJJOGIXCV-SAHWJRBASA-N 0.000 description 1
- BQQKYWSSFKXTPV-SAHWJRBASA-N CC(C)(C)OC(N(C(OC(C)(C)C)=O)C(O[C@H](CF)[C@@H]1OCC2)=N[C@]12c1cc(N)ccc1F)=O Chemical compound CC(C)(C)OC(N(C(OC(C)(C)C)=O)C(O[C@H](CF)[C@@H]1OCC2)=N[C@]12c1cc(N)ccc1F)=O BQQKYWSSFKXTPV-SAHWJRBASA-N 0.000 description 1
- DXKKYJSKQONWPR-XJKSGUPXSA-N CC(C)(C)OC(N[C@@]1([C@H](C=O)OCC1)c1ccccc1F)=O Chemical compound CC(C)(C)OC(N[C@@]1([C@H](C=O)OCC1)c1ccccc1F)=O DXKKYJSKQONWPR-XJKSGUPXSA-N 0.000 description 1
- NANSNYMQUFWYBG-XJKSGUPXSA-N CC(C)(C)OC(N[C@@]1([C@H](CO)OCC1)c(cccc1)c1F)=O Chemical compound CC(C)(C)OC(N[C@@]1([C@H](CO)OCC1)c(cccc1)c1F)=O NANSNYMQUFWYBG-XJKSGUPXSA-N 0.000 description 1
- GCMFPZDRDSJJGK-UHFFFAOYSA-N CC(C)C(C1CCCCC1)C1NCCCC1 Chemical compound CC(C)C(C1CCCCC1)C1NCCCC1 GCMFPZDRDSJJGK-UHFFFAOYSA-N 0.000 description 1
- MHGITPJBHNVRTI-UHFFFAOYSA-N CC(C)C(C1NCCCC1)c1ncccc1 Chemical compound CC(C)C(C1NCCCC1)c1ncccc1 MHGITPJBHNVRTI-UHFFFAOYSA-N 0.000 description 1
- GLIKSOKQYXUSLR-UHFFFAOYSA-N CC(C1NCCCC1)c1ccccc1 Chemical compound CC(C1NCCCC1)c1ccccc1 GLIKSOKQYXUSLR-UHFFFAOYSA-N 0.000 description 1
- DRUBJNFKXMYPCV-NWDGAFQWSA-N CC[C@@H]1OCC[C@]1(c1ccccc1F)N Chemical compound CC[C@@H]1OCC[C@]1(c1ccccc1F)N DRUBJNFKXMYPCV-NWDGAFQWSA-N 0.000 description 1
- WYEKIAQYIJOEDG-ATNBEAFSSA-N COc1cc(OC)c(CN(Cc(ccc(OC)c2)c2OC)C(O[C@H](CF)[C@@H]2OCC3)=N[C@]23c(cccc2)c2F)cc1 Chemical compound COc1cc(OC)c(CN(Cc(ccc(OC)c2)c2OC)C(O[C@H](CF)[C@@H]2OCC3)=N[C@]23c(cccc2)c2F)cc1 WYEKIAQYIJOEDG-ATNBEAFSSA-N 0.000 description 1
- RARUTAIKDFXRLL-ATNBEAFSSA-N COc1cc(OC)c(CN(Cc(ccc(OC)c2)c2OC)C(O[C@H](CI)[C@@H]2OCC3)=N[C@]23c(cccc2)c2F)cc1 Chemical compound COc1cc(OC)c(CN(Cc(ccc(OC)c2)c2OC)C(O[C@H](CI)[C@@H]2OCC3)=N[C@]23c(cccc2)c2F)cc1 RARUTAIKDFXRLL-ATNBEAFSSA-N 0.000 description 1
- BNUMCIMQZLYRPP-OKDKDVNESA-N C[C@@H]1[C@](c2cc([N+]([O-])=O)ccc2F)(C#C)N=C(N(C(OC(C)(C)C)=O)C(OC(C)(C)C)=O)O[C@@H]1COC Chemical compound C[C@@H]1[C@](c2cc([N+]([O-])=O)ccc2F)(C#C)N=C(N(C(OC(C)(C)C)=O)C(OC(C)(C)C)=O)O[C@@H]1COC BNUMCIMQZLYRPP-OKDKDVNESA-N 0.000 description 1
- GDDRTSCTPREXGN-XDFJSJKPSA-N C[N]([C@@]1([C@H]2OCC1)c1ccccc1F)(C(N(Cc(c(OC)c1)ccc1OC)Cc(ccc(OC)c1)c1OC)=O)C2=C Chemical compound C[N]([C@@]1([C@H]2OCC1)c1ccccc1F)(C(N(Cc(c(OC)c1)ccc1OC)Cc(ccc(OC)c1)c1OC)=O)C2=C GDDRTSCTPREXGN-XDFJSJKPSA-N 0.000 description 1
- HMTIZPWZVULFHR-MRXNPFEDSA-N NC(OCC1)=N[C@H]1C(Cc1cc(NC(c(nc2)ccc2C#N)=O)ccc1F)(F)F Chemical compound NC(OCC1)=N[C@H]1C(Cc1cc(NC(c(nc2)ccc2C#N)=O)ccc1F)(F)F HMTIZPWZVULFHR-MRXNPFEDSA-N 0.000 description 1
- AOUWJLVHTRHFFT-WDEREUQCSA-N N[C@@]1([C@H](CO)OCC1)c1ccccc1F Chemical compound N[C@@]1([C@H](CO)OCC1)c1ccccc1F AOUWJLVHTRHFFT-WDEREUQCSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- 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
- C07D498/10—Spiro-condensed systems
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2015516335A JP2016501827A (ja) | 2012-10-24 | 2013-10-23 | Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2012234461 | 2012-10-24 | ||
| JP2012234461 | 2012-10-24 | ||
| JP2013154451 | 2013-07-25 | ||
| JP2013154451 | 2013-07-25 | ||
| JP2015516335A JP2016501827A (ja) | 2012-10-24 | 2013-10-23 | Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| PCT/JP2013/079472 WO2014065434A1 (en) | 2012-10-24 | 2013-10-23 | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016501827A true JP2016501827A (ja) | 2016-01-21 |
| JP2016501827A5 JP2016501827A5 (enExample) | 2016-10-13 |
Family
ID=50544799
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015516335A Pending JP2016501827A (ja) | 2012-10-24 | 2013-10-23 | Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US9540359B2 (enExample) |
| EP (1) | EP2912035A4 (enExample) |
| JP (1) | JP2016501827A (enExample) |
| WO (1) | WO2014065434A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019507164A (ja) * | 2016-03-01 | 2019-03-14 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害剤 |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ589590A (en) | 2008-06-13 | 2012-05-25 | Shionogi & Co | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| WO2011071135A1 (ja) | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
| US9540359B2 (en) | 2012-10-24 | 2017-01-10 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
| TW201446758A (zh) | 2013-03-01 | 2014-12-16 | Amgen Inc | 作爲β-分泌酶抑制劑的全氟化5,6-二氫-4H-1,3-□-2-胺化合物及其用途 |
| 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 |
| MA44948A1 (fr) | 2013-04-11 | 2020-06-30 | Hoffmann La Roche | Inhibiteurs de bace 1 |
| PE20161225A1 (es) | 2014-02-19 | 2016-12-04 | H Lundbeck As | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer |
| TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有bace1抑制活性之二氫噻及二氫衍生物 |
| 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 |
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| 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 |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | H 朗德貝克公司 | 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療 |
| WO2017025559A1 (en) | 2015-08-12 | 2017-02-16 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors |
| WO2017061534A1 (en) | 2015-10-08 | 2017-04-13 | Shionogi & Co., Ltd. | Dihydrothiazine derivatives |
| WO2018112083A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| JP7159161B2 (ja) | 2016-12-15 | 2022-10-24 | 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シクロプロピル縮合チアジン誘導体および使用方法 |
| ES2910367T3 (es) | 2016-12-15 | 2022-05-12 | Amgen Inc | Derivados de tiazina y oxazina bicíclicos como inhibidores de beta-secretasa y métodos de uso |
| WO2018112081A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| AU2017376446B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| CN112313238B (zh) | 2018-04-27 | 2025-01-17 | 盐野义制药株式会社 | 具有选择性bace1抑制活性的四氢吡喃并噁嗪衍生物 |
| CN111592557A (zh) * | 2020-05-09 | 2020-08-28 | 河北合佳医药科技集团股份有限公司 | 一种7-氨基-3-乙烯基头孢烷酸的一步法环保制备方法 |
Citations (13)
| 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 |
| WO2011069934A1 (en) * | 2009-12-11 | 2011-06-16 | F. Hoffmann-La Roche Ag | 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors |
| WO2011071135A1 (ja) * | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
| WO2011070029A1 (en) * | 2009-12-10 | 2011-06-16 | F. Hoffmann-La Roche Ag | Amino oxazine derivatives |
| WO2012107371A1 (en) * | 2011-02-08 | 2012-08-16 | F. Hoffmann-La Roche Ag | 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 |
| WO2012139993A1 (en) * | 2011-04-11 | 2012-10-18 | F. Hoffmann-La Roche Ag | 1,3 oxazines as bace1 and/or bace2 inhibitors |
| WO2013110622A1 (en) * | 2012-01-26 | 2013-08-01 | F. Hoffmann-La Roche Ag | Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines |
| WO2013142613A1 (en) * | 2012-03-20 | 2013-09-26 | Elan Pharmaceuticals, Inc. | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
| JP2014513702A (ja) * | 2011-05-16 | 2014-06-05 | エフ.ホフマン−ラ ロシュ アーゲー | Bace1及び/又はbace2阻害剤としての1,3−オキサジン |
| JP2014516063A (ja) * | 2011-06-07 | 2014-07-07 | エフ.ホフマン−ラ ロシュ アーゲー | Bace1及び/又はbace2阻害剤としてのハロゲン−アルキル−1,3オキサジン |
| JP2014518895A (ja) * | 2011-06-07 | 2014-08-07 | エフ.ホフマン−ラ ロシュ アーゲー | [1,3]オキサジン |
| JP2014524463A (ja) * | 2011-08-25 | 2014-09-22 | ノバルティス アーゲー | 2−アミノ−4−(ピリジン−2−イル)−5,6−ジヒドロ−4h−1,3−オキサジン誘導体およびbace−1および/またはbace−2阻害剤としてのそれらの使用 |
| JP2014526534A (ja) * | 2011-09-21 | 2014-10-06 | エフ.ホフマン−ラ ロシュ アーゲー | BACE1阻害剤としてのN−(3−(2−アミノ−6,6−ジフルオロ−4,4a,5,6,7,7a−ヘキサヒドロ−シクロペンタ[e][1,3]オキサジン−4−イル)−フェニル)−アミド |
Family Cites Families (201)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3235551A (en) | 1966-02-15 | Novel derivatives of | ||
| US3227713A (en) | 1966-01-04 | Azine derivatives | ||
| US2899426A (en) | 1959-08-11 | Synthesis of l | ||
| US3115494A (en) | 1961-10-13 | 1963-12-24 | Mcneilab Inc | 2-amino-5, 6-dihydro-4ii-1, 3-oxazines and a process for their preparation |
| BE637923A (enExample) | 1962-09-29 | |||
| US3636116A (en) | 1968-09-03 | 1972-01-18 | Dow Chemical Co | 1 2-substituted indene compounds |
| SU465792A3 (ru) | 1968-11-06 | 1975-03-30 | Хиноин Гиогисцер-Ес Вегиесцети Термекек Гиара Рт (Фирма) | Способ получени гетероциклических соединений |
| US3577428A (en) | 1969-04-14 | 1971-05-04 | Colgate Palmolive Co | 2-amino-4-aryloxyalkyl-4-alkyl-2-oxazolines |
| US3719674A (en) | 1971-02-08 | 1973-03-06 | Dow Chemical Co | 1,2-substituted indene compounds |
| DE2426653C3 (de) | 1974-06-01 | 1982-05-06 | Bayer Ag, 5090 Leverkusen | Derivate des 2-Amino-1,3-thiazins |
| DD140144A1 (de) | 1978-11-08 | 1980-02-13 | Horst Hartmann | Verfahren zur herstellung von p-aminophenylsubstituierten 2-amino-1,3-thiaziniumsalzen |
| US4311840A (en) | 1980-11-13 | 1982-01-19 | E. R. Squibb & Sons, Inc. | 2,3,6,7-Tetrahydro-2-thioxo-4H-oxazolo[3,2-a]-1,3,5 triazin-4-ones |
| JPS62120374A (ja) | 1985-11-20 | 1987-06-01 | Yoshitomi Pharmaceut Ind Ltd | 1,3−チアジンまたは1,3−オキサジン誘導体 |
| JPH0231792Y2 (enExample) | 1986-01-21 | 1990-08-28 | ||
| FI95572C (fi) | 1987-06-22 | 1996-02-26 | Eisai Co Ltd | Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi |
| CA1332151C (en) | 1988-01-28 | 1994-09-27 | Roman Amrein | Use of a benzamide to treat cognitive disorder |
| US5236942A (en) | 1990-04-19 | 1993-08-17 | Merrell Dow Pharmaceuticals Inc. | 5-aryl-4-alkyl-3H-1,2,4-triazole-3-thiones useful in the treatment of Altzheimer's dementia |
| US5328915A (en) | 1992-09-17 | 1994-07-12 | E. I. Du Pont De Nemours And Company | Arthropodicidal amidrazone ureas |
| JPH08503940A (ja) | 1992-11-27 | 1996-04-30 | ザ ウエルカム ファウンデーション リミテッド | 酵素阻害薬 |
| EP0723438A1 (en) | 1993-10-04 | 1996-07-31 | The Wellcome Foundation Limited | Substituted urea and isothiourea derivatives as no synthase inhibitors |
| GB9418912D0 (en) | 1994-09-20 | 1994-11-09 | Fisons Corp | Pharmaceutically active compounds |
| AU4149696A (en) | 1994-11-15 | 1996-06-06 | Merck & Co., Inc. | Substituted heterocycles as inhibitors of nitric oxide synthase |
| DE4442116A1 (de) | 1994-11-25 | 1996-05-30 | Cassella Ag | 2-Amino-1,3-thiazine als Hemmstoffe der Stickstoffmonoxid-Synthase |
| WO1996018607A1 (en) | 1994-12-12 | 1996-06-20 | Chugai Seiyaku Kabushiki Kaisha | Aniline derivative having the effect of inhibiting nitrogen monoxide synthase |
| JPH08333258A (ja) | 1994-12-14 | 1996-12-17 | Japan Tobacco Inc | チアジン又はチアゼピン誘導体及びそれら化合物を含有してなる一酸化窒素合成酵素阻害剤 |
| DE4444930A1 (de) | 1994-12-16 | 1996-06-27 | Cassella Ag | 2-Amino-1,3-thiazepine und deren Verwendung als Hemmstoffe der Stickstoffmonoxid-Synthase |
| BR9610766A (pt) | 1995-08-11 | 1999-07-13 | Pfizer | Triihdrato de metanossulfonato de (1s,2s)-1-(4-hidróxi-fenil)-2-(4-hidróxi-4-fenilpiperidin-1-il)-1-propanol |
| JPH0967355A (ja) | 1995-08-31 | 1997-03-11 | Tokyo Tanabe Co Ltd | チアジン誘導体、チアゾール誘導体及びそれらの製造方法 |
| ZA967840B (en) | 1995-09-18 | 1997-04-07 | Sankyo Co | New urea derivatives having a cat inhibitory activity their preparation and their therapeutic and prophylactic use |
| PL326353A1 (en) | 1995-10-17 | 1998-09-14 | Astra Pharma Prod | Pharmaceutically active quinozolinic compounds |
| IL126476A0 (en) | 1996-04-13 | 1999-08-17 | Astra Pharma Prod | Aminoisoquinolines and aminothienopyridine derivatives and their use as anti-inflammatory agents |
| US6096753A (en) | 1996-12-05 | 2000-08-01 | Amgen Inc. | Substituted pyrimidinone and pyridone compounds and methods of use |
| US5952374A (en) | 1997-09-29 | 1999-09-14 | Protein Technologies International, Inc. | Method for inhibiting the development of Alzheimer's disease and related dementias- and for preserving cognitive function |
| SE9703693D0 (sv) | 1997-10-10 | 1997-10-10 | Astra Pharma Prod | Novel combination |
| TW460460B (en) | 1997-11-04 | 2001-10-21 | Chugai Pharmaceutical Co Ltd | Heterocyclic compounds having NOS inhibitory activities |
| US6294695B1 (en) | 1998-03-26 | 2001-09-25 | Mount Sinai School Of Medicine Of The City University Of New York | Aminobenzoic acid derivatives having anti-tumorigenic activity methods of making and using the same |
| AUPP285898A0 (en) | 1998-04-07 | 1998-04-30 | Fujisawa Pharmaceutical Co., Ltd. | Amido derivatives |
| SE9802333D0 (sv) | 1998-06-29 | 1998-06-29 | Astra Pharma Prod | Novel combination |
| US7375125B2 (en) | 1999-08-04 | 2008-05-20 | Ore Pharmaceuticals, Inc. | Melanocortin-4 receptor binding compounds and methods of use thereof |
| AU780787B2 (en) | 1999-09-17 | 2005-04-14 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| US20030060487A1 (en) | 2000-04-12 | 2003-03-27 | Bamdad R. Shoshana | Treatment of neurodegenerative disease |
| AU2001258771A1 (en) | 2000-05-19 | 2001-11-26 | Takeda Chemical Industries Ltd. | -secretase inhibitors |
| US6420566B2 (en) | 2000-06-09 | 2002-07-16 | Aventis Pharma S.A. | Pharmaceutical compositions containing a 4, 5-dihydro-1, 3-thiazol-2-ylamine derivative, novel derivatives and preparation thereof |
| US6713276B2 (en) | 2000-06-28 | 2004-03-30 | Scios, Inc. | Modulation of Aβ levels by β-secretase BACE2 |
| WO2002062766A2 (en) | 2001-02-07 | 2002-08-15 | Millennium Pharmaceuticals, Inc. | Melanocortin-4 receptor binding compounds and methods of use thereof |
| WO2002088101A2 (en) | 2001-04-27 | 2002-11-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
| US6562783B2 (en) | 2001-05-30 | 2003-05-13 | Neurologic, Inc. | Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors |
| CA2466284A1 (en) | 2001-11-08 | 2003-05-15 | Elan Pharmaceuticals, Inc. | N, n'-substituted-1,3-diamino-2-hydroxypropane derivatives |
| ATE319693T1 (de) | 2001-11-09 | 2006-03-15 | Aventis Pharma Sa | 2-amino-thiazolinderivate und ihre verwendung als hemmstoffe der induzierbaren no-synthase |
| BR0206363A (pt) | 2001-11-09 | 2003-12-23 | Aventis Pharma Sa | Utilização de deerivados de 2-amino-4-heteroariletiltiazolina como inibidores de no-sintase indutìvel |
| HUP0402033A2 (hu) | 2001-11-09 | 2005-02-28 | Aventis Pharma S.A. | 2-Amino-4-piridil-metil-tiazolin-származékok alkalmazása az indukálható NO-szintetáz inhibitoraként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények |
| US7271266B2 (en) | 2002-03-28 | 2007-09-18 | Merck & Co., Inc. | Substituted 2,3-diphenyl pyridines |
| AU2003257418A1 (en) | 2002-06-19 | 2004-01-06 | Solvay Pharmaceuticals Gmbh | Medicament for the treatment of diseases requiring inhibition or a reduction in the activity of ph value-regulating bicarbonate transporter proteins |
| WO2004009549A2 (en) | 2002-07-18 | 2004-01-29 | Actelion Pharmaceuticals Ltd | Piperidines useful for the treatment of central nervous system disorders |
| WO2004014843A1 (ja) | 2002-08-09 | 2004-02-19 | Takeda Chemical Industries, Ltd. | 置換アミノ化合物およびその用途 |
| TW200502221A (en) | 2002-10-03 | 2005-01-16 | Astrazeneca Ab | Novel lactams and uses thereof |
| JP2004149429A (ja) | 2002-10-29 | 2004-05-27 | Takeda Chem Ind Ltd | インドール化合物およびその用途 |
| JP2006096665A (ja) | 2002-10-29 | 2006-04-13 | Ono Pharmaceut Co Ltd | 脊柱管狭窄症治療剤 |
| US7109217B2 (en) | 2002-11-12 | 2006-09-19 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease |
| RU2252936C2 (ru) | 2002-12-05 | 2005-05-27 | Институт физиологически активных веществ РАН | S-замещенные n-1-[(гетеро)арил]алкил-n`-[(гетеро)арил]алкилизотиомочевины, способ их получения, фармацевтическая композиция, способ изучения глутаматэргической системы, способы лечения (варианты) |
| EP1631560A2 (en) | 2003-04-25 | 2006-03-08 | 3-Dimensional Pharmaceuticals, Inc. | C-fms kinase inhibitors |
| GB0324498D0 (en) | 2003-07-21 | 2003-11-26 | Aventis Pharma Inc | Heterocyclic compounds as P2X7 ion channel blockers |
| JP2007525482A (ja) | 2003-10-07 | 2007-09-06 | レノビス, インコーポレイテッド | イオンチャネルリガンドとしてのアミド化合物およびその使用 |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP2153832B1 (en) | 2003-12-15 | 2016-03-09 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors |
| BRPI0418081A (pt) | 2003-12-24 | 2007-04-17 | Halliburton Energy Serv Inc | métodos para estimar nìveis de contaminação em fluidos em um furo de sondagem, e para testagem de formação no furo descendente, aparelho para estimar nìveis de contaminação de fluidos de formação em um furo de sondagem, e, meio utilizável por computador |
| WO2005097767A1 (en) | 2004-03-30 | 2005-10-20 | Merck & Co., Inc. | 2-aminothiazole compounds useful as aspartyl protease inhibitors |
| US7459450B2 (en) | 2004-04-30 | 2008-12-02 | Schering Corporation | Neuropeptide receptor modulators |
| EP1758907B1 (en) | 2004-06-16 | 2009-02-18 | Wyeth | Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase |
| DE602005022320D1 (de) | 2004-08-23 | 2010-08-26 | Merck Sharp & Dohme | Kondensierte triazolderivate als dipeptidylpeptidase-iv-hemmer zur behandlung bzw. prävention von diabetes |
| EP1791818A1 (en) | 2004-09-14 | 2007-06-06 | The Genetics Company, Inc. | Hydrazone derivatives and their use as beta secretase inhibitors |
| CN101084199A (zh) | 2004-10-15 | 2007-12-05 | 阿斯利康(瑞典)有限公司 | 取代的氨基化合物及其用途 |
| EP1802588A4 (en) | 2004-10-15 | 2010-02-17 | Astrazeneca Ab | SUBSTITUTED AMINOPYRIMIDONE AND APPLICATIONS THEREOF |
| US20080287399A1 (en) | 2004-12-14 | 2008-11-20 | Astrazeneca Ab | Substituted Aminopyridines and Uses Thereof |
| TWI441819B (zh) | 2005-01-07 | 2014-06-21 | Synta Pharmaceuticals Corp | 用於炎症及免疫相關用途之化合物 |
| EP1836208A2 (en) | 2005-01-14 | 2007-09-26 | Wyeth Incoporated | AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE |
| WO2006088694A1 (en) | 2005-02-14 | 2006-08-24 | Wyeth | SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS |
| WO2006088705A1 (en) | 2005-02-14 | 2006-08-24 | Wyeth | Terphenyl guanidines as [beta symbol] -secretase inhibitors |
| RU2007131043A (ru) | 2005-02-14 | 2009-03-20 | Вайет (Us) | Азолилацилгуанидины, применяемые в качестве ингибиторов бета-секретазы |
| CN101142194B (zh) | 2005-03-14 | 2012-10-10 | 顶点制药有限责任公司 | 吲哚衍生物,组合物及用作β-分泌酶抑制剂的方法 |
| MX2007016182A (es) | 2005-06-14 | 2008-03-07 | Schering Corp | Inhibidores de aspartil proteasas. |
| EP1896032B1 (en) | 2005-06-14 | 2012-10-31 | Merck Sharp & Dohme Corp. | The preparation and use of compounds as protease inhibitors |
| EP1890703B1 (en) | 2005-06-14 | 2016-05-11 | Taigen Biotechnology | Pyrimidine compounds as chemokine receptors inhibitors |
| ATE482214T1 (de) | 2005-06-14 | 2010-10-15 | Schering Corp | Aspartylproteasehemmer |
| US7273882B2 (en) | 2005-06-21 | 2007-09-25 | Bristol-Myers Squibb Company | Aminoacetamide acyl guanidines as β-secretase inhibitors |
| JP2009500329A (ja) | 2005-06-30 | 2009-01-08 | ワイス | アミノ−5−(6員)ヘテロアリールイミダゾロン化合物およびβ−セレクターゼ調節のためのその使用 |
| TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| JP2009509957A (ja) | 2005-09-26 | 2009-03-12 | ワイス | β−セクレターゼ阻害剤としてのアミノ−5−[4−(ジフルオロメトキシ)フェニル]−5−フェニルイミダゾロン化合物 |
| US20090215801A9 (en) | 2005-11-15 | 2009-08-27 | Astrazeneca Ab, Sodertaije, Swedenastex Thereapeutics Ltd | Novel 2-Aminopyrimidinone Derivatives And Their Use |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| US20080318985A1 (en) | 2005-11-15 | 2008-12-25 | Astrazeneca Ab | Novel 2-Aminopyrimidinone Or 2-Aminopyridinone Derivatives and Their Use |
| WO2007058601A1 (en) | 2005-11-21 | 2007-05-24 | Astrazeneca Ab | Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia |
| TW200734311A (en) | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
| AR058381A1 (es) | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
| EP1966185A2 (en) | 2005-12-19 | 2008-09-10 | Wyeth a Corporation of the State of Delaware | 2-AMINO-5-PIPERIDINYLIMIDAZOLONE COMPOUNDS AND USE THEREOF FOR ß-SECRETASE MODULATION |
| UY30118A1 (es) | 2006-01-31 | 2007-06-29 | Tanabe Seiyaku Co | Compueto amina trisustituido |
| US7776882B2 (en) | 2006-02-06 | 2010-08-17 | Baxter Ellen W | 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
| US7868022B2 (en) | 2006-02-06 | 2011-01-11 | Janssen Pharmaceutica Nv | 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
| CN101460480A (zh) | 2006-04-05 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途 |
| TW200808751A (en) | 2006-04-13 | 2008-02-16 | Astrazeneca Ab | New compounds |
| JP5089681B2 (ja) | 2006-04-20 | 2012-12-05 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | c−fmsキナーゼの阻害剤としての複素環式化合物 |
| EP2644600B1 (en) | 2006-06-12 | 2017-01-11 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors |
| BRPI0713187A2 (pt) | 2006-07-20 | 2012-10-16 | Mehmet Kahraman | método de inibir rho-quinase, método de tratamento de doença mediada por rho-quinase, composto e composição farmacêutica |
| TW200817406A (en) | 2006-08-17 | 2008-04-16 | Wyeth Corp | Imidazole amines as inhibitors of β-secretase |
| US8093254B2 (en) | 2006-12-12 | 2012-01-10 | Schering Corporation | Aspartyl protease inhibitors |
| CN101631779A (zh) | 2006-12-12 | 2010-01-20 | 先灵公司 | 含有三环系统的天冬氨酰蛋白酶抑制剂 |
| TW200831080A (en) | 2006-12-15 | 2008-08-01 | Irm Llc | Compounds and compositions as inhibitors of cannabinoid receptor 1 activity |
| RU2460725C2 (ru) | 2007-02-15 | 2012-09-10 | Ф. Хоффманн-Ля Рош Аг | Новые 2-аминооксазолины в качестве лигандов taar1 |
| 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 |
| JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
| GB0713686D0 (en) | 2007-07-13 | 2007-08-22 | Addex Pharmaceuticals Sa | New compounds 2 |
| JP4846769B2 (ja) | 2007-07-30 | 2011-12-28 | 田辺三菱製薬株式会社 | 医薬組成物 |
| US9986911B2 (en) | 2007-10-19 | 2018-06-05 | Smiths Medical Asd, Inc. | Wireless telecommunications system adaptable for patient monitoring |
| WO2009064418A1 (en) | 2007-11-14 | 2009-05-22 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
| PT2233474E (pt) | 2008-01-18 | 2015-10-26 | Eisai R&D Man Co Ltd | Derivado de aminodihidrotiazina condensado |
| EP2238111B1 (en) | 2008-01-28 | 2013-01-16 | Janssen Pharmaceutica NV | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of -secretase (bace) |
| NZ586830A (en) | 2008-01-29 | 2012-02-24 | Janssen Pharmaceutica Nv | 2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace) |
| KR20100116206A (ko) | 2008-02-01 | 2010-10-29 | 다케다 야쿠힌 고교 가부시키가이샤 | Hsp90 저해제로서의 옥심 유도체 |
| CN101952260B (zh) | 2008-02-18 | 2013-02-13 | 弗·哈夫曼-拉罗切有限公司 | 4,5-二氢-*唑-2-基胺衍生物 |
| CA2723222C (en) | 2008-04-22 | 2013-04-02 | Schering Corporation | 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 |
| NZ589590A (en) | 2008-06-13 | 2012-05-25 | Shionogi & Co | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| AU2009277485B2 (en) | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| WO2010013302A1 (ja) | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| WO2010019392A1 (en) | 2008-08-13 | 2010-02-18 | Merck Sharp & Dohme Corp. | Purine derivatives for treatment of alzheimer's disease |
| EP2312946A4 (en) | 2008-08-13 | 2012-10-24 | Merck Sharp & Dohme | PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF MORBUS ALZHEIMER |
| AU2009300836B2 (en) | 2008-09-30 | 2014-02-27 | Eisai R&D Management Co., Ltd. | Novel fused aminodihydrothiazine derivative |
| 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 |
| US20100125087A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
| US20100125081A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 574 |
| TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
| US20120015961A1 (en) | 2009-03-31 | 2012-01-19 | Shionogi & Co., Ltd. | Isothiourea derivatives or isourea derivatives having bace1 inhibitory activity |
| KR101123178B1 (ko) | 2009-04-09 | 2012-06-13 | (주)에스메디 | 2-아릴벤조싸이오펜 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물 |
| JP6186125B2 (ja) | 2009-05-07 | 2017-08-30 | ザ ボード オブ トラスティーズ オブ ザ リーランド スタンフォード ジュニア ユニバーシティ | 疼痛の研究、画像化および治療方法、ならびに疼痛の研究、画像化および治療のための組成物 |
| US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| 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 |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | 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 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| US8354441B2 (en) | 2009-11-11 | 2013-01-15 | Hoffmann-La Roche Inc. | Oxazoline derivatives |
| WO2011058763A1 (ja) | 2009-11-13 | 2011-05-19 | 塩野義製薬株式会社 | アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体 |
| US8435994B2 (en) | 2009-11-16 | 2013-05-07 | Merck Sharp & Dohme Corp. | Substituted [1,2,4]triazolo[4,3-alpha]quinoxalines as adenosine A2a receptor antagonists |
| WO2011070781A1 (ja) | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | 置換アミノチアジン誘導体 |
| WO2011071057A1 (ja) | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物 |
| US20120245155A1 (en) | 2009-12-11 | 2012-09-27 | Shionogi & Co., Ltd. | Fused heterocyclic compound having amino group |
| EP2518059A4 (en) | 2009-12-24 | 2013-05-29 | Shionogi & Co | 4-AMINO-1,3-THIAZINE OR OXAZINE DERIVATIVE |
| BR112012015916A2 (pt) | 2009-12-31 | 2017-04-25 | Novartis Ag | derivados de pirazina e seu uso no tratamento de distúrbios neurológicos |
| 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 |
| CN102918036A (zh) | 2010-06-09 | 2013-02-06 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5-氨基-3,6-二氢-1H-吡嗪-2-酮衍生物 |
| WO2011154431A1 (en) | 2010-06-09 | 2011-12-15 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| EA201291413A1 (ru) | 2010-06-28 | 2013-05-30 | Янссен Фармацевтика Нв | Производные 3-амино-5,6-дигидро-1h-пиразин-2-она, применимые для лечения болезни альцгеймера и других форм деменции |
| MY150939A (en) | 2010-07-13 | 2014-03-14 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| US8815881B2 (en) | 2010-08-09 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds |
| CN103097389B (zh) | 2010-09-22 | 2015-10-14 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的4,7-二氢-吡唑并[1,5-a]吡嗪-6-基胺衍生物 |
| WO2012057248A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| BR112013015430A2 (pt) | 2010-12-22 | 2016-09-20 | Janssen Pharmaceutica Nv | derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace) |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| US20130281449A1 (en) | 2011-01-12 | 2013-10-24 | Novartis Ag | Oxazine Derivatives and their Use in the Treatment of Neurological Disorders |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| PL2663561T3 (pl) | 2011-01-13 | 2016-10-31 | Nowe pochodne heterocykliczne i ich zastosowanie w leczeniu zaburzeń neurologicznych | |
| CN103596569A (zh) | 2011-01-13 | 2014-02-19 | 诺瓦提斯公司 | 用于治疗代谢障碍的bace-2抑制剂 |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| US8399459B2 (en) | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| US20130040971A1 (en) | 2011-02-14 | 2013-02-14 | Boehringer Ingelheim International Gmbh | 6-cycloalkyl-pyrazolopyrimidinones for the treatment of cns disorders |
| US8809345B2 (en) | 2011-02-15 | 2014-08-19 | Boehringer Ingelheim International Gmbh | 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders |
| US8815841B2 (en) | 2011-02-18 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| SI2681219T1 (sl) | 2011-03-01 | 2016-02-29 | Janssen Pharmaceutica, N.V. | Derivati 6,7-dihidro-pirazolo(1,5-a)pirazin-4-ilamina uporabni kot inhibitorji beta-sekretaze (BACE) |
| US9067924B2 (en) | 2011-03-04 | 2015-06-30 | Hoffmann-La Roche Inc. | 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors |
| JP5853035B2 (ja) | 2011-03-09 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap | β−セクレターゼ(BACE)の阻害剤として有用な3,4−ジヒドロ−ピロロ[1,2−a]ピラジン−1−イルアミン誘導体 |
| US8748418B2 (en) | 2011-03-18 | 2014-06-10 | Hoffmann-La Roche Inc. | 1,4-oxazepines as BACE1 and/or BACE2 inhibitors |
| US8877744B2 (en) | 2011-04-04 | 2014-11-04 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| JPWO2012147763A1 (ja) | 2011-04-26 | 2014-07-28 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
| 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 |
| US8604024B2 (en) | 2011-05-24 | 2013-12-10 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| TW201302763A (zh) | 2011-05-24 | 2013-01-16 | 必治妥美雅史谷比公司 | 用於減少β-類澱粉產生之化合物 |
| US9079919B2 (en) | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
| JP2012250933A (ja) * | 2011-06-03 | 2012-12-20 | Shionogi & Co Ltd | オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物 |
| UA111749C2 (uk) | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| JP5989130B2 (ja) | 2011-12-06 | 2016-09-07 | ヤンセン ファーマシューティカ エヌ.ベー. | 5−(3−アミノフェニル)−5−アルキル−5,6−ジヒドロ−2h−[1,4]オキサジン−3−アミン誘導体 |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| WO2014001228A1 (en) | 2012-06-26 | 2014-01-03 | F. Hoffmann-La Roche Ag | Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors |
| WO2014010748A1 (en) | 2012-07-10 | 2014-01-16 | Shionogi & Co., Ltd. | Cyclopropane derivative having bace1 inhibiting activity |
| US9540359B2 (en) | 2012-10-24 | 2017-01-10 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
| JP2014101354A (ja) | 2012-10-24 | 2014-06-05 | Shionogi & Co Ltd | Bace1阻害作用を有するオキサジン誘導体 |
| JP2014101353A (ja) | 2012-10-26 | 2014-06-05 | Shionogi & Co Ltd | オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物 |
| US9475784B2 (en) | 2012-12-19 | 2016-10-25 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production |
| HK1210609A1 (en) | 2013-01-22 | 2016-04-29 | 霍夫曼-拉罗奇有限公司 | Fluoro-[1,3]oxazines as bace1 inhibitors |
| TW201446758A (zh) | 2013-03-01 | 2014-12-16 | Amgen Inc | 作爲β-分泌酶抑制劑的全氟化5,6-二氫-4H-1,3-□-2-胺化合物及其用途 |
| 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 |
| MA44948A1 (fr) | 2013-04-11 | 2020-06-30 | Hoffmann La Roche | Inhibiteurs de bace 1 |
-
2013
- 2013-10-23 US US14/434,013 patent/US9540359B2/en not_active Expired - Fee Related
- 2013-10-23 EP EP13848316.9A patent/EP2912035A4/en not_active Withdrawn
- 2013-10-23 JP JP2015516335A patent/JP2016501827A/ja active Pending
- 2013-10-23 WO PCT/JP2013/079472 patent/WO2014065434A1/en not_active Ceased
-
2016
- 2016-09-21 US US15/272,031 patent/US9758513B2/en not_active Expired - Fee Related
Patent Citations (13)
| 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 |
| WO2011070029A1 (en) * | 2009-12-10 | 2011-06-16 | F. Hoffmann-La Roche Ag | Amino oxazine derivatives |
| WO2011069934A1 (en) * | 2009-12-11 | 2011-06-16 | F. Hoffmann-La Roche Ag | 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors |
| WO2011071135A1 (ja) * | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
| WO2012107371A1 (en) * | 2011-02-08 | 2012-08-16 | F. Hoffmann-La Roche Ag | 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 |
| WO2012139993A1 (en) * | 2011-04-11 | 2012-10-18 | F. Hoffmann-La Roche Ag | 1,3 oxazines as bace1 and/or bace2 inhibitors |
| JP2014513702A (ja) * | 2011-05-16 | 2014-06-05 | エフ.ホフマン−ラ ロシュ アーゲー | Bace1及び/又はbace2阻害剤としての1,3−オキサジン |
| JP2014516063A (ja) * | 2011-06-07 | 2014-07-07 | エフ.ホフマン−ラ ロシュ アーゲー | Bace1及び/又はbace2阻害剤としてのハロゲン−アルキル−1,3オキサジン |
| JP2014518895A (ja) * | 2011-06-07 | 2014-08-07 | エフ.ホフマン−ラ ロシュ アーゲー | [1,3]オキサジン |
| JP2014524463A (ja) * | 2011-08-25 | 2014-09-22 | ノバルティス アーゲー | 2−アミノ−4−(ピリジン−2−イル)−5,6−ジヒドロ−4h−1,3−オキサジン誘導体およびbace−1および/またはbace−2阻害剤としてのそれらの使用 |
| JP2014526534A (ja) * | 2011-09-21 | 2014-10-06 | エフ.ホフマン−ラ ロシュ アーゲー | BACE1阻害剤としてのN−(3−(2−アミノ−6,6−ジフルオロ−4,4a,5,6,7,7a−ヘキサヒドロ−シクロペンタ[e][1,3]オキサジン−4−イル)−フェニル)−アミド |
| WO2013110622A1 (en) * | 2012-01-26 | 2013-08-01 | F. Hoffmann-La Roche Ag | Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines |
| WO2013142613A1 (en) * | 2012-03-20 | 2013-09-26 | Elan Pharmaceuticals, Inc. | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
Non-Patent Citations (2)
| Title |
|---|
| HANS HILPERT ET AL: "β-Secretase(BACE1) Inhibitors with High in Vivo Efficacy Suitable for Clinical Evaluation in Alzhei", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 10, JPN6017020921, 16 April 2013 (2013-04-16), pages 3980 - 3995, ISSN: 0003647800 * |
| WOLTERING,T.J. ET AL: "BACE1 inhibitors: A head group scan on a series of amides", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 23, no. 14, JPN6017020923, 18 May 2013 (2013-05-18), pages 4239 - 4243, ISSN: 0003647801 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019507164A (ja) * | 2016-03-01 | 2019-03-14 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| US9540359B2 (en) | 2017-01-10 |
| US9758513B2 (en) | 2017-09-12 |
| EP2912035A1 (en) | 2015-09-02 |
| US20150266865A1 (en) | 2015-09-24 |
| US20170008881A1 (en) | 2017-01-12 |
| WO2014065434A1 (en) | 2014-05-01 |
| EP2912035A4 (en) | 2016-06-15 |
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