JP2013505969A5 - - Google Patents
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- Publication number
- JP2013505969A5 JP2013505969A5 JP2012531212A JP2012531212A JP2013505969A5 JP 2013505969 A5 JP2013505969 A5 JP 2013505969A5 JP 2012531212 A JP2012531212 A JP 2012531212A JP 2012531212 A JP2012531212 A JP 2012531212A JP 2013505969 A5 JP2013505969 A5 JP 2013505969A5
- Authority
- JP
- Japan
- Prior art keywords
- nitrogen
- methyl
- alkyl
- ring
- substituted
- 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
Links
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 14
- -1 1,3-oxazol-2-yl Chemical group 0.000 claims 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 12
- 125000005843 halogen group Chemical group 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000002947 alkylene group Chemical group 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000001153 fluoro group Chemical group F* 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 7
- 125000004498 isoxazol-4-yl group Chemical group O1N=CC(=C1)* 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- GHPHJDFIOQSUBE-UHFFFAOYSA-N 2-[(3,4-difluorophenyl)methoxy]-5-(1-hydroxyethyl)-n-pyridazin-4-ylbenzamide Chemical compound C=1C=NN=CC=1NC(=O)C1=CC(C(O)C)=CC=C1OCC1=CC=C(F)C(F)=C1 GHPHJDFIOQSUBE-UHFFFAOYSA-N 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 2
- XSAKVPQLGQBNEP-UHFFFAOYSA-N 5-chloro-2-[(2-cyanophenyl)methoxy]-n-phenylbenzamide Chemical compound C=1C=CC=CC=1NC(=O)C1=CC(Cl)=CC=C1OCC1=CC=CC=C1C#N XSAKVPQLGQBNEP-UHFFFAOYSA-N 0.000 claims 1
- AAACBXVBBDAYRQ-UHFFFAOYSA-N 5-chloro-2-phenylmethoxy-n-pyridin-3-ylbenzamide Chemical compound C=1C=CN=CC=1NC(=O)C1=CC(Cl)=CC=C1OCC1=CC=CC=C1 AAACBXVBBDAYRQ-UHFFFAOYSA-N 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24655009P | 2009-09-29 | 2009-09-29 | |
| US61/246,550 | 2009-09-29 | ||
| CNPCT/CN2010/001334 | 2010-09-02 | ||
| CN2010001334 | 2010-09-02 | ||
| PCT/CN2010/001501 WO2011038572A1 (en) | 2009-09-29 | 2010-09-27 | Novel compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013505969A JP2013505969A (ja) | 2013-02-21 |
| JP2013505969A5 true JP2013505969A5 (enExample) | 2013-11-14 |
| JP5752691B2 JP5752691B2 (ja) | 2015-07-22 |
Family
ID=43825509
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012531212A Expired - Fee Related JP5752691B2 (ja) | 2009-09-29 | 2010-09-27 | 新規化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8778939B2 (enExample) |
| EP (1) | EP2483254B1 (enExample) |
| JP (1) | JP5752691B2 (enExample) |
| KR (1) | KR20120081609A (enExample) |
| AU (1) | AU2010302842B2 (enExample) |
| BR (1) | BR112012006859A2 (enExample) |
| CA (1) | CA2775753A1 (enExample) |
| EA (1) | EA021437B1 (enExample) |
| ES (1) | ES2512727T3 (enExample) |
| IL (1) | IL218674A (enExample) |
| IN (1) | IN2012DN02763A (enExample) |
| MX (1) | MX2012003778A (enExample) |
| SG (1) | SG179120A1 (enExample) |
| WO (1) | WO2011038572A1 (enExample) |
| ZA (1) | ZA201201877B (enExample) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011260323A1 (en) | 2010-06-04 | 2012-11-15 | F. Hoffmann-La Roche Ag | Aminopyrimidine derivatives as LRRK2 modulators |
| ES2524892T3 (es) * | 2010-09-02 | 2014-12-15 | Glaxosmithkline Intellectual Property Development Limited | 2-(Benciloxi)benzamidas como inhibidores de LRRK2 quinasa |
| KR101566091B1 (ko) | 2010-11-10 | 2015-11-04 | 에프. 호프만-라 로슈 아게 | Lrrk2 조절제로서 피라졸 아미노피리미딘 유도체 |
| EP2704701B1 (en) * | 2011-05-03 | 2018-01-03 | PRCL Research Inc. | Compounds for inflammation and immune-related uses |
| WO2012162254A1 (en) | 2011-05-23 | 2012-11-29 | Elan Pharmaceuticals, Inc. | Inhibitors of lrrk2 kinase activity |
| PT2760453T (pt) | 2011-09-30 | 2016-08-02 | Ipsen Pharma Sas | Inibidores macrocíclicos da cinase lrrk2 |
| US8791130B2 (en) | 2011-11-29 | 2014-07-29 | Genentech, Inc. | Aminopyrimidine derivatives as LRRK2 modulators |
| AR089182A1 (es) | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| JP6185925B2 (ja) | 2011-11-29 | 2017-08-23 | ジェネンテック， インコーポレイテッド | Ｌｒｒｋ２モジュレーターとしてのアミノピリミジン誘導体 |
| US9145402B2 (en) * | 2011-11-29 | 2015-09-29 | Genentech, Inc. | Aminopyrimidine derivatives as LRRK2 modulators |
| WO2013079496A1 (en) | 2011-11-30 | 2013-06-06 | F. Hoffmann-La Roche Ag | Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (pet) imaging for lrrk2 |
| EA025186B1 (ru) | 2012-06-29 | 2016-11-30 | Пфайзер Инк. | НОВЫЕ 4-(ЗАМЕЩЕННЫЙ АМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LRRK2 |
| ES2865058T3 (es) * | 2013-12-09 | 2021-10-14 | Unichem Lab Ltd | Un proceso mejorado para la preparación de (3R,4R)-(1-bencil-4-metilpiperidin-3-il)-metilamina |
| EP3083618B1 (en) | 2013-12-17 | 2018-02-21 | Pfizer Inc | Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors |
| RU2016134751A (ru) | 2014-01-29 | 2018-03-02 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Соединения |
| SG11201605342UA (en) * | 2014-01-29 | 2016-08-30 | Glaxosmithkline Ip Dev Ltd | Compounds |
| JP2017511340A (ja) | 2014-03-31 | 2017-04-20 | ザ トラスティース オブ コロンビア ユニバーシティ イン ザ シティ オブ ニューヨーク | ヒストンアセチルトランスフェラーゼ活性剤及びその使用 |
| WO2015176010A1 (en) | 2014-05-15 | 2015-11-19 | The United States Of America, As Represented By The Secretary, Departmentof Health & Human Services | Treatment or prevention of an intestinal disease or disorder |
| JP6625610B2 (ja) | 2014-07-31 | 2019-12-25 | ビーエーエスエフ ソシエタス・ヨーロピアＢａｓｆ Ｓｅ | ピラゾールの調製方法 |
| CN105348182B (zh) * | 2014-08-24 | 2018-04-13 | 复旦大学 | 2‑烷氧基苯甲酰芳胺类化合物及其药物用途 |
| ES2717510T3 (es) | 2014-09-17 | 2019-06-21 | Oncodesign Sa | Inhibidores macrocíclicos de cinasa LRRK2 |
| CA2971413A1 (en) | 2014-12-16 | 2016-06-23 | Axovant Sciences Gmbh | Geminal substituted quinuclidine amide compounds as agonists of alpha-7 nicotinic acetylcholine receptors |
| UA124228C2 (uk) * | 2015-05-11 | 2021-08-11 | Басф Се | Спосіб одержання 4-амінопіридазинів |
| CN107592859A (zh) | 2015-05-11 | 2018-01-16 | 巴斯夫欧洲公司 | 制备4‑氨基哒嗪类的方法 |
| CN107847494A (zh) | 2015-06-10 | 2018-03-27 | 阿考温特科学股份有限公司 | 作为α7‑烟碱乙酰胆碱受体激动剂的氨基苯并异噁唑化合物 |
| US10428062B2 (en) | 2015-08-12 | 2019-10-01 | Axovant Sciences Gmbh | Geminal substituted aminobenzisoxazole compounds as agonists of α7-nicotinic acetylcholine receptors |
| RU2722149C1 (ru) | 2015-09-14 | 2020-05-27 | Пфайзер Инк. | Новые производные имидазо[4,5-c] хинолинов и имидазо[4,5-c][1,5] нафтиридинов в качестве ингибиторов LRRK2 |
| AU2017295745A1 (en) | 2016-07-12 | 2019-01-31 | Bayer Cropscience Aktiengesellschaft | Bicyclic compounds as pest control agents |
| WO2018082964A1 (en) | 2016-11-04 | 2018-05-11 | Basf Se | Process for the production of pyridazinyl-amides in a one-pot synthesis |
| EP3573956A4 (en) * | 2017-01-25 | 2020-08-12 | GlaxoSmithKline Intellectual Property Management Limited | COMPOUNDS |
| SG11201908234WA (en) | 2017-02-24 | 2019-10-30 | Daegu Gyeongbuk Medical Innovation Found | Pharmaceutical composition comprising compound capable of penetrating blood-brain barrier as effective ingredient for preventing or treating brain cancer |
| KR101990739B1 (ko) | 2018-07-24 | 2019-06-19 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| KR101990738B1 (ko) | 2018-07-24 | 2019-06-19 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| KR101992059B1 (ko) | 2018-08-23 | 2019-06-21 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| JP7345220B2 (ja) | 2019-08-30 | 2023-09-15 | ティーエスディー ライフ サイエンス カンパニー リミテッド | イミダゾピリジン誘導体及びこれを有効成分として含有する薬学的組成物 |
| WO2023076404A1 (en) | 2021-10-27 | 2023-05-04 | Aria Pharmaceuticals, Inc. | Methods for treating systemic lupus erythematosus |
| JP2025034990A (ja) * | 2023-08-31 | 2025-03-13 | 東京応化工業株式会社 | レジスト組成物、レジストパターン形成方法、化合物、及び酸拡散制御剤 |
| CN119432181B (zh) * | 2024-11-28 | 2025-07-15 | 佛山市德堡建材有限公司 | 一种环保型聚合物水泥防水涂料及其制备方法 |
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| US5449691A (en) | 1991-12-31 | 1995-09-12 | Sterling Winthrop Inc. | 3,4-disubstituted anilines-immunomodulating agents |
| SK27198A3 (en) | 1995-08-30 | 1998-09-09 | Bayer Ag | Acylaminosalicylic acid amides and their uses as pesticides |
| EP0986384B1 (en) | 1997-05-07 | 2012-02-22 | University Of Pittsburgh | Inhibitors of protein isoprenyl transferases |
| EP1014962A4 (en) | 1997-06-26 | 2007-06-27 | Lilly Co Eli | ANTITHROMBOTIC AGENTS |
| NZ507760A (en) | 1998-03-26 | 2002-10-25 | Japan Tobacco Inc | Amide derivatives and nociceptin antagonists |
| ATE260272T1 (de) | 2000-03-17 | 2004-03-15 | Bristol Myers Squibb Pharma Co | Beta-aminsäure-derivate zur verwendung als matrix-metalloproteasen- und tna-alpha-inhibitoren |
| GB0023983D0 (en) | 2000-09-29 | 2000-11-15 | Prolifix Ltd | Therapeutic compounds |
| DE10159453A1 (de) | 2001-12-04 | 2003-06-18 | Merck Patent Gmbh | Verwendung von 1-Phenyl-oxazolidin-2-on-Verbindungen als Protease |
| WO2003087044A2 (en) | 2002-04-09 | 2003-10-23 | 7Tm Pharma A/S | Novel carboxamide compounds for use in mch receptor related disorders |
| WO2003087045A1 (en) | 2002-04-09 | 2003-10-23 | 7Tm Pharma A/S | Novel methoxybenzamide compounds for use in mch receptor related disorders |
| WO2004099170A2 (en) | 2003-04-30 | 2004-11-18 | The Institutes For Pharmaceutical Discovery, Llc | Phenyl substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b |
| WO2004099127A1 (en) | 2003-05-07 | 2004-11-18 | Novo Nordisk A/S | Novel compounds as kinase inhibitors |
| WO2005000309A2 (en) | 2003-06-27 | 2005-01-06 | Ionix Pharmaceuticals Limited | Chemical compounds |
| US7550485B2 (en) | 2003-10-14 | 2009-06-23 | Wyeth | Substituted N-heterocycle derivatives and methods of their use |
| WO2005073210A1 (ja) * | 2004-01-28 | 2005-08-11 | Kissei Pharmaceutical Co., Ltd. | 新規なベンゾフラン誘導体、それを含有する医薬組成物およびそれらの用途 |
| TW200606133A (en) | 2004-06-30 | 2006-02-16 | Sankyo Co | Substituted benzene compounds |
| US7671077B2 (en) | 2004-07-19 | 2010-03-02 | Leu-Fen Hou Lin | Neuroprotective small organic molecules, compositions and uses related thereto |
| US20060276496A1 (en) | 2005-03-17 | 2006-12-07 | Boehringer Ingelheim Pharmaceuticals, Inc. | Anti-Cytokine Heterocyclic Compounds |
| CA2621406A1 (en) | 2005-09-07 | 2007-03-15 | Plexxikon, Inc. | Pparactive compounds |
| JP2007176799A (ja) | 2005-12-27 | 2007-07-12 | Sankyo Co Ltd | 置換ベンゼン化合物を含有する医薬 |
| AU2007223342A1 (en) | 2006-03-07 | 2007-09-13 | Bristol-Myers Squibb Company | Pyrrolotriazine aniline prodrug compounds useful as kinase inhibitors |
| EP2019824A2 (en) | 2006-04-28 | 2009-02-04 | Transtech Pharma, Inc. | Benzamide glucokinase activators |
| JP5069752B2 (ja) * | 2006-12-15 | 2012-11-07 | グラクソ グループ リミテッド | Ｅｐ４受容体アゴニストとしてのベンズアミド誘導体 |
| WO2009030270A1 (en) * | 2007-09-03 | 2009-03-12 | Novartis Ag | Dihydroindole derivatives useful in parkinson's disease |
| GB0722680D0 (en) | 2007-11-19 | 2007-12-27 | Topotarget As | Therapeutic compounds and their use |
| WO2010048559A2 (en) | 2008-10-24 | 2010-04-29 | Calcimedica Inc. | Phenylpyrazole inhibitors of store operated calcium release |
-
2010
- 2010-09-27 ES ES10819801.1T patent/ES2512727T3/es active Active
- 2010-09-27 IN IN2763DEN2012 patent/IN2012DN02763A/en unknown
- 2010-09-27 CA CA2775753A patent/CA2775753A1/en not_active Abandoned
- 2010-09-27 US US13/498,975 patent/US8778939B2/en not_active Expired - Fee Related
- 2010-09-27 KR KR1020127010852A patent/KR20120081609A/ko not_active Abandoned
- 2010-09-27 BR BR112012006859A patent/BR112012006859A2/pt not_active IP Right Cessation
- 2010-09-27 AU AU2010302842A patent/AU2010302842B2/en not_active Ceased
- 2010-09-27 JP JP2012531212A patent/JP5752691B2/ja not_active Expired - Fee Related
- 2010-09-27 WO PCT/CN2010/001501 patent/WO2011038572A1/en not_active Ceased
- 2010-09-27 EA EA201270480A patent/EA021437B1/ru not_active IP Right Cessation
- 2010-09-27 EP EP10819801.1A patent/EP2483254B1/en active Active
- 2010-09-27 SG SG2012017760A patent/SG179120A1/en unknown
- 2010-09-27 MX MX2012003778A patent/MX2012003778A/es active IP Right Grant
-
2012
- 2012-03-14 ZA ZA2012/01877A patent/ZA201201877B/en unknown
- 2012-03-15 IL IL218674A patent/IL218674A/en not_active IP Right Cessation
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