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
- -1 1,3-oxazol-2-yl Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- 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
- 239000011780 sodium chloride Substances 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
- 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
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000001820 oxy group Chemical group [*:1]O[*:2] 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
- 150000002829 nitrogen Chemical group 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
- 206010061536 Parkinson's disease Diseases 0.000 claims 2
- 125000004429 atoms Chemical group 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
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical group O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 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
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000000969 carrier Substances 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
- 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 | ||
| CN2010001334 | 2010-09-02 | ||
| CNPCT/CN2010/001334 | 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 (US07585860-20090908-C00112.png) | 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)
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2576541T3 (pl) | 2010-06-04 | 2016-10-31 | Pochodne aminopirymidyny jako modulatory lrrk2 | |
| JP5781611B2 (ja) * | 2010-09-02 | 2015-09-24 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｌｒｒｋ２キナーゼ阻害剤としての２−（ベンジルオキシ）ベンズアミド類 |
| LT3124483T (lt) | 2010-11-10 | 2019-09-25 | Genentech, Inc. | Pirazolo aminopirimidino dariniai, kaip lrrk2 moduliatoriai |
| JP5985611B2 (ja) * | 2011-05-03 | 2016-09-06 | シンタ ファーマシューティカルズ コーポレーション | 炎症および免疫関連用途のための化合物 |
| WO2012162254A1 (en) * | 2011-05-23 | 2012-11-29 | Elan Pharmaceuticals, Inc. | Inhibitors of lrrk2 kinase activity |
| HUE029728T2 (en) | 2011-09-30 | 2017-03-28 | Ipsen Pharma Sas | Macrocyclic LRRK2 kinase inhibitors |
| CN103958482B (zh) * | 2011-11-29 | 2017-06-09 | 健泰科生物技术公司 | 作为lrrk2调节剂的氨基嘧啶衍生物 |
| RU2651544C2 (ru) | 2011-11-29 | 2018-04-20 | Дженентек, Инк. | Производные аминопиримидина в качестве модуляторов богатой лейцином повторной киназы 2 (lrrk2) |
| JP6180426B2 (ja) | 2011-11-29 | 2017-08-16 | ジェネンテック， インコーポレイテッド | パーキンソン病の処置のためのキナーゼｌｒｒｋ２モジュレーターとしての２−（フェニル又はピリド−３−イル）アミノピリミジン誘導体 |
| AR089182A1 (es) | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| 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 |
| AP3902A (en) | 2012-06-29 | 2016-11-17 | Pfizer | Novel 4-(substituted-amino)-7H-pyrrolo[2,3-d]pyrimidines as LRRK2 inhibitors |
| BR112015025543B1 (pt) * | 2013-12-09 | 2020-11-03 | Unichem Laboratories Limited | processo para a preparação de (3r,4r)-(1-benzil-4- metilpiperidina-3-il)-metilamina e compostos intermediários |
| 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 |
| CA2937430A1 (en) | 2014-01-29 | 2015-08-06 | Glaxosmithkline Intellectual Property Development Limited | Compounds |
| CR20160348A (es) * | 2014-01-29 | 2017-04-28 | Glaxosmithline Intellectual Property Dev Ltd | Compuestos |
| EP3126332A4 (en) * | 2014-03-31 | 2017-09-06 | The Trustees of Columbia University in the City of New York | Histone acetyltransferase activators and uses thereof |
| 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 |
| DK3174858T3 (da) | 2014-07-31 | 2019-07-15 | Basf Se | Fremgangsmåde til fremstilling af pyrazoler |
| 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 |
| PL3194405T4 (pl) | 2014-09-17 | 2019-07-31 | Oncodesign S.A. | Makrocykliczne inhibitory kinazy lrrk2 |
| US10183938B2 (en) | 2014-12-16 | 2019-01-22 | Axovant Sciences Gmbh | Geminal substituted quinuclidine amide compounds as agonists of α-7 nicotonic acetylcholine receptors |
| UA124228C2 (uk) * | 2015-05-11 | 2021-08-11 | Басф Се | Спосіб одержання 4-амінопіридазинів |
| EP3294725B1 (en) | 2015-05-11 | 2021-05-05 | Basf Se | Process for preparing 4-amino-pyridazines |
| MX2017016231A (es) | 2015-06-10 | 2018-11-29 | Axovant Sciences Gmbh | Compuestos de aminobencisoxazol como agonistas de receptores a7-nicotínicos de acetilcolina. |
| US10428062B2 (en) | 2015-08-12 | 2019-10-01 | Axovant Sciences Gmbh | Geminal substituted aminobenzisoxazole compounds as agonists of α7-nicotinic acetylcholine receptors |
| WO2017046675A1 (en) | 2015-09-14 | 2017-03-23 | Pfizer Inc. | Novel imidazo [4,5-c] quinoline and imidazo [4,5-c][1,5] naphthyridine derivatives as lrrk2 inhibitors |
| KR20190028763A (ko) | 2016-07-12 | 2019-03-19 | 바이엘 크롭사이언스 악티엔게젤샤프트 | 해충 방제제로서의 바이시클릭 화합물 |
| WO2018082964A1 (en) | 2016-11-04 | 2018-05-11 | Basf Se | Process for the production of pyridazinyl-amides in a one-pot synthesis |
| CA3050156A1 (en) | 2017-01-25 | 2018-08-02 | Glaxosmithkline Intellectual Property Development 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 |
| KR101990738B1 (ko) | 2018-07-24 | 2019-06-19 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| KR101990739B1 (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 |
| CA3148490C (en) | 2019-08-30 | 2024-04-30 | Jae Won Lee | Imidazopyridine derivative and pharmaceutical composition comprising same as active ingredient |
| WO2023076404A1 (en) | 2021-10-27 | 2023-05-04 | Aria Pharmaceuticals, Inc. | Methods for treating systemic lupus erythematosus |
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| AU7473398A (en) | 1997-05-07 | 1998-11-27 | University Of Pittsburgh | Inhibitors of protein isoprenyl transferases |
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| RU2202344C2 (ru) | 1998-03-26 | 2003-04-20 | Джапан Тобакко Инк. | Антагонисты ноцицептина, производные амида, аналгетик, способ инициирования антагонистического действия к ноцицептину, способ лечения боли, фармацевтические композиции |
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| GB0722680D0 (en) | 2007-11-19 | 2007-12-27 | Topotarget As | Therapeutic compounds and their use |
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-
2010
- 2010-09-27 CA CA2775753A patent/CA2775753A1/en not_active Abandoned
- 2010-09-27 KR KR1020127010852A patent/KR20120081609A/ko active IP Right Grant
- 2010-09-27 WO PCT/CN2010/001501 patent/WO2011038572A1/en active Application Filing
- 2010-09-27 SG SG2012017760A patent/SG179120A1/en unknown
- 2010-09-27 MX MX2012003778A patent/MX2012003778A/es active IP Right Grant
- 2010-09-27 IN IN2763DEN2012 patent/IN2012DN02763A/en unknown
- 2010-09-27 BR BR112012006859A patent/BR112012006859A2/pt not_active IP Right Cessation
- 2010-09-27 ES ES10819801.1T patent/ES2512727T3/es active Active
- 2010-09-27 JP JP2012531212A patent/JP5752691B2/ja not_active Expired - Fee Related
- 2010-09-27 US US13/498,975 patent/US8778939B2/en not_active Expired - Fee Related
- 2010-09-27 EP EP10819801.1A patent/EP2483254B1/en active Active
- 2010-09-27 EA EA201270480A patent/EA021437B1/ru not_active IP Right Cessation
- 2010-09-27 AU AU2010302842A patent/AU2010302842B2/en not_active Ceased
-
2012
- 2012-03-14 ZA ZA2012/01877A patent/ZA201201877B/en unknown
- 2012-03-15 IL IL218674A patent/IL218674A/en not_active IP Right Cessation
