JP2012502112A5 - - Google Patents
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- Publication number
- JP2012502112A5 JP2012502112A5 JP2011527012A JP2011527012A JP2012502112A5 JP 2012502112 A5 JP2012502112 A5 JP 2012502112A5 JP 2011527012 A JP2011527012 A JP 2011527012A JP 2011527012 A JP2011527012 A JP 2011527012A JP 2012502112 A5 JP2012502112 A5 JP 2012502112A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- membered
- cycloalkyl
- ring
- 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.)
- Granted
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- -1 C 1-6 -alkyl Chemical group 0.000 description 58
- 125000001188 haloalkyl group Chemical group 0.000 description 24
- 125000005843 halogen group Chemical group 0.000 description 24
- 125000005842 heteroatom Chemical group 0.000 description 20
- 125000004438 haloalkoxy group Chemical group 0.000 description 18
- 229910052760 oxygen Inorganic materials 0.000 description 17
- 125000002950 monocyclic group Chemical group 0.000 description 16
- 125000002619 bicyclic group Chemical group 0.000 description 15
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 description 12
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 12
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 description 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 12
- 125000001424 substituent group Chemical group 0.000 description 12
- 125000004122 cyclic group Chemical group 0.000 description 11
- 125000004432 carbon atom Chemical group C* 0.000 description 10
- 229910052757 nitrogen Inorganic materials 0.000 description 10
- 229920006395 saturated elastomer Polymers 0.000 description 10
- 229910052717 sulfur Inorganic materials 0.000 description 9
- QMYGFTJCQFEDST-UHFFFAOYSA-N 3-methoxybutyl acetate Chemical group COC(C)CCOC(C)=O QMYGFTJCQFEDST-UHFFFAOYSA-N 0.000 description 6
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 6
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 6
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 6
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 6
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 6
- 229910052739 hydrogen Inorganic materials 0.000 description 6
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 6
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 description 6
- 125000004043 oxo group Chemical group O=* 0.000 description 6
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 6
- 150000003839 salts Chemical group 0.000 description 6
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 6
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 6
- 101100240516 Caenorhabditis elegans nhr-10 gene Proteins 0.000 description 5
- 125000000217 alkyl group Chemical group 0.000 description 5
- 125000006546 (C4-C10) cycloalkyl group Chemical group 0.000 description 4
- 125000005309 thioalkoxy group Chemical group 0.000 description 4
- 125000003118 aryl group Chemical group 0.000 description 2
- 125000001072 heteroaryl group Chemical group 0.000 description 2
- 125000000304 alkynyl group Chemical group 0.000 description 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9608208P | 2008-09-11 | 2008-09-11 | |
| US61/096,082 | 2008-09-11 | ||
| PCT/US2009/056748 WO2010030954A1 (en) | 2008-09-11 | 2009-09-11 | Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012502112A JP2012502112A (ja) | 2012-01-26 |
| JP2012502112A5 true JP2012502112A5 (https=) | 2014-07-10 |
| JP5579720B2 JP5579720B2 (ja) | 2014-08-27 |
Family
ID=41319591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011527012A Expired - Fee Related JP5579720B2 (ja) | 2008-09-11 | 2009-09-11 | ベータ−セクレターゼ調節物質としてのスピロ四環式化合物および使用法 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8426447B2 (https=) |
| EP (1) | EP2328903B1 (https=) |
| JP (1) | JP5579720B2 (https=) |
| KR (1) | KR20110073511A (https=) |
| CN (1) | CN102209721A (https=) |
| AU (1) | AU2009291602B2 (https=) |
| BR (1) | BRPI0918449A2 (https=) |
| CA (1) | CA2736130C (https=) |
| CL (1) | CL2011000516A1 (https=) |
| CO (1) | CO6362014A2 (https=) |
| CR (1) | CR20110134A (https=) |
| EA (1) | EA201100461A1 (https=) |
| ES (1) | ES2459195T3 (https=) |
| IL (1) | IL211440A0 (https=) |
| MA (1) | MA32705B1 (https=) |
| MX (1) | MX2011002705A (https=) |
| MY (1) | MY148558A (https=) |
| PE (1) | PE20110805A1 (https=) |
| TW (1) | TWI385175B (https=) |
| WO (1) | WO2010030954A1 (https=) |
| ZA (1) | ZA201102674B (https=) |
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| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| CA2753730C (en) | 2009-03-13 | 2020-12-22 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| CN102812005B (zh) | 2010-02-24 | 2014-12-10 | 生命医药公司 | β-分泌酶抑制剂 |
| EP2547685A1 (en) * | 2010-03-15 | 2013-01-23 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta - secretase modulators |
| MX2012010657A (es) * | 2010-03-15 | 2013-02-07 | Amgen Inc | Compuestos de espiro amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso medico. |
| WO2011130741A1 (en) * | 2010-04-16 | 2011-10-20 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
| WO2012019056A1 (en) * | 2010-08-05 | 2012-02-09 | Amgen Inc. | Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use |
| EP2609081A1 (en) | 2010-08-23 | 2013-07-03 | Amgen Inc. | Sulfonylpiperazine derivatives that interact with glucokinase regulatory protein for the treatment of diabetes |
| JPWO2012070226A1 (ja) * | 2010-11-22 | 2014-05-19 | 出光興産株式会社 | 含酸素縮合環誘導体及びそれを含んでなる有機エレクトロルミネッセンス素子 |
| WO2012071458A1 (en) * | 2010-11-22 | 2012-05-31 | Array Biopharma Inc. | Heterocyclic inhibitors of beta - secretase for the treatment of neurodegenerative diseases |
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| US8415483B2 (en) | 2010-12-22 | 2013-04-09 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| EP2673279A1 (en) | 2011-02-07 | 2013-12-18 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use |
| EP2675810A1 (en) | 2011-02-15 | 2013-12-25 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of 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 |
| 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 |
| CN103608344B (zh) | 2011-06-07 | 2016-11-23 | 霍夫曼-拉罗奇有限公司 | [1,3]噁嗪类 |
| 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 |
| WO2013044092A1 (en) * | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| EP2780321B1 (en) | 2011-10-10 | 2015-12-30 | Astrazeneca AB | Mono-fluoro beta-secretase inhibitors |
| TWI557112B (zh) | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β－分泌酶抑制劑 |
| EP2650284A1 (en) * | 2012-04-10 | 2013-10-16 | Merz Pharma GmbH & Co. KGaA | Heterocyclic derivatives as metabotropic glutamate receptor modulators |
| JP2015518048A (ja) * | 2012-05-30 | 2015-06-25 | コメンティス， インコーポレイテッド | クロマン化合物 |
| US9000182B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | 2H-imidazol-4-amine compounds and their use as BACE inhibitors |
| US9000183B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US9000184B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US9000185B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cycloalkyl ether compounds and their use as BACE inhibitors |
| US10548882B2 (en) | 2012-06-21 | 2020-02-04 | Astrazeneca Ab | Camsylate salt |
| TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β－分泌酶抑制劑 |
| JP2015532282A (ja) | 2012-09-28 | 2015-11-09 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | β−セクレターゼの阻害剤 |
| WO2014078314A1 (en) * | 2012-11-15 | 2014-05-22 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| WO2016126726A1 (en) | 2015-02-02 | 2016-08-11 | Forma Therapeutics, Inc. | Bicyclic [4,6,0] hydroxamic acids as hdac6 inhibitors |
| SG11201708622UA (en) | 2015-02-02 | 2017-11-29 | Forma Therapeutics Inc | 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors |
| EP3472131B1 (en) | 2016-06-17 | 2020-02-19 | Forma Therapeutics, Inc. | 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors |
| DE102023106829A1 (de) | 2023-03-19 | 2024-09-19 | List Technology Ag | Verfahren und Vorrichtung zur Behandlung eines Ausgangsproduktes |
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| CL2008000791A1 (es) | 2007-03-23 | 2008-05-30 | Wyeth Corp | Compuestos derivados de 2-amino-5-(4-difluorometoxi-fenil)-5-fenil-imidazolidin-4-ona; composicion farmaceutica que comprende a dichos compuestos; y su uso en el tratamiento de una enfermedad asociada con la actividad bace excesiva, tales como enferm |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| TW200902503A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
| AU2009216825A1 (en) | 2008-02-18 | 2009-08-27 | F. Hoffmann-La Roche Ag | 4, 5-dihydro-oxazol-2-yl amine derivatives |
| US8450331B2 (en) | 2008-04-22 | 2013-05-28 | Merck Sharp & Dohme Corp. | Thiophenyl-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 |
| RU2513086C2 (ru) | 2008-07-24 | 2014-04-20 | Ф.Хоффманн-Ля Рош Аг | Производные 4,5-дигидро-оксазол-2-ила |
| EP2318416B1 (en) * | 2008-07-28 | 2013-09-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
-
2009
- 2009-09-11 CA CA2736130A patent/CA2736130C/en not_active Expired - Fee Related
- 2009-09-11 EP EP09737222.1A patent/EP2328903B1/en active Active
- 2009-09-11 PE PE2011000606A patent/PE20110805A1/es not_active Application Discontinuation
- 2009-09-11 TW TW098130795A patent/TWI385175B/zh not_active IP Right Cessation
- 2009-09-11 MY MYPI2011001092A patent/MY148558A/en unknown
- 2009-09-11 CN CN2009801456428A patent/CN102209721A/zh active Pending
- 2009-09-11 WO PCT/US2009/056748 patent/WO2010030954A1/en not_active Ceased
- 2009-09-11 EA EA201100461A patent/EA201100461A1/ru unknown
- 2009-09-11 US US12/558,426 patent/US8426447B2/en active Active
- 2009-09-11 ES ES09737222.1T patent/ES2459195T3/es active Active
- 2009-09-11 BR BRPI0918449A patent/BRPI0918449A2/pt not_active IP Right Cessation
- 2009-09-11 MX MX2011002705A patent/MX2011002705A/es active IP Right Grant
- 2009-09-11 JP JP2011527012A patent/JP5579720B2/ja not_active Expired - Fee Related
- 2009-09-11 KR KR1020117008316A patent/KR20110073511A/ko not_active Withdrawn
- 2009-09-11 AU AU2009291602A patent/AU2009291602B2/en not_active Ceased
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2011
- 2011-02-27 IL IL211440A patent/IL211440A0/en unknown
- 2011-03-10 CL CL2011000516A patent/CL2011000516A1/es unknown
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- 2011-03-25 CO CO11036742A patent/CO6362014A2/es not_active Application Discontinuation
- 2011-04-11 MA MA33762A patent/MA32705B1/fr unknown
- 2011-04-11 ZA ZA2011/02674A patent/ZA201102674B/en unknown
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