JP2012520861A5 - - Google Patents
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- Publication number
- JP2012520861A5 JP2012520861A5 JP2012500308A JP2012500308A JP2012520861A5 JP 2012520861 A5 JP2012520861 A5 JP 2012520861A5 JP 2012500308 A JP2012500308 A JP 2012500308A JP 2012500308 A JP2012500308 A JP 2012500308A JP 2012520861 A5 JP2012520861 A5 JP 2012520861A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- heterocycloalkyl
- heteroaryl
- cycloalkyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 41
- 125000003118 aryl group Chemical group 0.000 claims 38
- 125000001072 heteroaryl group Chemical group 0.000 claims 34
- 125000001424 substituent group Chemical group 0.000 claims 33
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- -1 cyano, hydroxyl Chemical group 0.000 claims 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 239000011593 sulfur Substances 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical group [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 239000007822 coupling agent Substances 0.000 claims 2
- IKDUDTNKRLTJSI-UHFFFAOYSA-N hydrazine hydrate Chemical compound O.NN IKDUDTNKRLTJSI-UHFFFAOYSA-N 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- ANVUICNGPOHXRE-UHFFFAOYSA-N C1(=CC=CC=C1)P(C1=CC=CC=C1)[C-]1C=CC=C1.[CH-]1C=CC=C1.[Fe+2].Cl.Cl Chemical compound C1(=CC=CC=C1)P(C1=CC=CC=C1)[C-]1C=CC=C1.[CH-]1C=CC=C1.[Fe+2].Cl.Cl ANVUICNGPOHXRE-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 102000009784 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Human genes 0.000 claims 1
- 108010020246 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Proteins 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 238000003556 assay Methods 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 229910052763 palladium Inorganic materials 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0904746.5 | 2009-03-19 | ||
| GB0904746A GB0904746D0 (en) | 2009-03-19 | 2009-03-19 | Compounds |
| US16202409P | 2009-03-20 | 2009-03-20 | |
| US61/162,024 | 2009-03-20 | ||
| GB0912238A GB0912238D0 (en) | 2009-07-14 | 2009-07-14 | Compounds |
| GB0912238.3 | 2009-07-14 | ||
| GBGB1001418.1A GB201001418D0 (en) | 2010-01-28 | 2010-01-28 | Compounds |
| GB1001418.1 | 2010-01-28 | ||
| PCT/GB2010/000498 WO2010106333A1 (en) | 2009-03-19 | 2010-03-19 | Compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012520861A JP2012520861A (ja) | 2012-09-10 |
| JP2012520861A5 true JP2012520861A5 (enExample) | 2013-02-28 |
| JP5732036B2 JP5732036B2 (ja) | 2015-06-10 |
Family
ID=42226628
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012500308A Expired - Fee Related JP5732036B2 (ja) | 2009-03-19 | 2010-03-19 | 化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US20100317646A1 (enExample) |
| EP (1) | EP2408772B1 (enExample) |
| JP (1) | JP5732036B2 (enExample) |
| KR (1) | KR101700229B1 (enExample) |
| CN (1) | CN102428084B (enExample) |
| AU (1) | AU2010224693B2 (enExample) |
| CA (1) | CA2754605C (enExample) |
| CL (1) | CL2011002267A1 (enExample) |
| IL (1) | IL215147A0 (enExample) |
| MX (1) | MX2011009807A (enExample) |
| PE (1) | PE20120506A1 (enExample) |
| RU (1) | RU2011142182A (enExample) |
| WO (1) | WO2010106333A1 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602007013573D1 (de) * | 2006-08-16 | 2011-05-12 | Hoffmann La Roche | Nicht-nukleosidische reverse-transkriptase-hemmer |
| GB201008134D0 (en) * | 2010-05-14 | 2010-06-30 | Medical Res Council Technology | Compounds |
| GB201015949D0 (en) | 2010-09-22 | 2010-11-03 | Medical Res Council Technology | Compounds |
| EP2632260A4 (en) * | 2010-10-29 | 2015-06-17 | Merck Sharp & Dohme | LEUCINREICH REPEAT KINASE ENZYME ACTIVITY |
| US20130338106A1 (en) * | 2011-02-28 | 2013-12-19 | John A. McCauley | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| WO2012135631A1 (en) * | 2011-03-30 | 2012-10-04 | Arrien Pharmaeuticals Llc | Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors |
| TWI557121B (zh) * | 2011-04-21 | 2016-11-11 | 原真股份有限公司 | 新穎激酶抑制劑 |
| WO2012162254A1 (en) | 2011-05-23 | 2012-11-29 | Elan Pharmaceuticals, Inc. | Inhibitors of lrrk2 kinase activity |
| CN102558174B (zh) * | 2011-08-23 | 2014-03-19 | 天津市斯芬克司药物研发有限公司 | 一种全新吡唑并[4,3-c]吡啶化合物的发明及其合成方法 |
| PT2760453T (pt) * | 2011-09-30 | 2016-08-02 | Ipsen Pharma Sas | Inibidores macrocíclicos da cinase lrrk2 |
| GB201204985D0 (en) | 2012-03-21 | 2012-05-02 | Genentech Inc | Compounds |
| WO2013182612A1 (en) | 2012-06-07 | 2013-12-12 | Bayer Pharma Aktiengesellschaft | Glucose transport inhibitors |
| EA025186B1 (ru) | 2012-06-29 | 2016-11-30 | Пфайзер Инк. | НОВЫЕ 4-(ЗАМЕЩЕННЫЙ АМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LRRK2 |
| WO2014026330A1 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| WO2014060113A1 (en) | 2012-10-19 | 2014-04-24 | Origenis Gmbh | Novel kinase inhibitors |
| CN104812755B (zh) * | 2012-10-31 | 2017-08-08 | 拉夸里亚创药株式会社 | 作为ttx‑s阻断剂的吡唑并吡啶衍生物 |
| CA2889572C (en) * | 2012-11-08 | 2019-03-05 | Pfizer Inc. | Heteroaromatic compounds as dopamine d1 ligands |
| US9045477B2 (en) * | 2013-03-15 | 2015-06-02 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| US20160024071A1 (en) * | 2013-03-15 | 2016-01-28 | Elan Pharmaceuticals, Llc | Inhibitors of lrrk2 kinase activity |
| TW201533043A (zh) * | 2013-04-18 | 2015-09-01 | Lundbeck & Co As H | 作爲ｌｒｒｋ２抑制劑的芳基吡咯并吡啶衍生化合物 |
| AR096654A1 (es) | 2013-06-20 | 2016-01-27 | Ab Science | Derivados de benzimidazol como inhibidores selectivos de proteína quinasa |
| WO2015026683A1 (en) * | 2013-08-22 | 2015-02-26 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| 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 |
| WO2015162518A1 (en) | 2014-04-25 | 2015-10-29 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine d1 ligands |
| PE20161475A1 (es) * | 2014-05-14 | 2017-01-08 | Pfizer | Pirazolopiridinas y pirazolopirimidinas |
| US10954240B2 (en) | 2014-09-03 | 2021-03-23 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| 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 |
| WO2017215600A1 (en) | 2016-06-15 | 2017-12-21 | Suzhou Yabao Pharmaceutical R&D Co., Ltd. | Substituted tricyclic herteocyclic compounds and use thereof |
| 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 |
| EP3737680A1 (en) | 2018-01-08 | 2020-11-18 | F. Hoffmann-La Roche AG | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
| KR101990738B1 (ko) * | 2018-07-24 | 2019-06-19 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| CN114072405A (zh) | 2019-07-03 | 2022-02-18 | 豪夫迈·罗氏有限公司 | 杂环单酰基甘油脂肪酶(magl)抑制剂 |
| KR20220034104A (ko) | 2019-07-09 | 2022-03-17 | 에프. 호프만-라 로슈 아게 | 신규 헤테로고리 화합물 |
| EP4069212A4 (en) * | 2019-12-04 | 2024-03-06 | Arcus Biosciences, Inc. | INHIBITORS OF HIF-2ALPHA |
| UA130412C2 (uk) | 2020-06-22 | 2026-02-11 | Ф. Хоффманн-Ля Рош Аг | Похідні сульфону |
| PE20231372A1 (es) | 2020-09-03 | 2023-09-07 | Hoffmann La Roche | Compuestos heterociclicos |
| TWI846353B (zh) * | 2022-02-25 | 2024-06-21 | 大陸商蘇州亞寶藥物研發有限公司 | 取代的稠環化合物及其藥物組合物、製備方法和用途 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3835144A (en) * | 1972-06-16 | 1974-09-10 | Squibb & Sons Inc | Amino derivatives of (4,3-c pyrazolopyridine cabroxylic acids and esters |
| NZ207394A (en) | 1983-03-08 | 1987-03-06 | Commw Serum Lab Commission | Detecting or determining sequence of amino acids |
| US5478830A (en) * | 1992-05-29 | 1995-12-26 | The Du Pont Merck Pharmaceutical Company | Fused-ring heterocycles for the treatment of atherosclerosis |
| US5300478A (en) * | 1993-01-28 | 1994-04-05 | Zeneca Limited | Substituted fused pyrazolo compounds |
| CN1656079A (zh) * | 2002-05-31 | 2005-08-17 | 卫材株式会社 | 吡唑化合物和含有该化合物的药物组合物 |
| US7186716B2 (en) * | 2002-08-12 | 2007-03-06 | Sugen, Inc. | 3-Pyrrol-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors |
| US7348338B2 (en) * | 2003-07-17 | 2008-03-25 | Plexxikon, Inc. | PPAR active compounds |
| WO2005016875A2 (en) * | 2003-08-06 | 2005-02-24 | Sugen, Inc. | Geometrically restricted 3-cyclopentylidene-1,3-dihydroindol-2-ones as potent protein kinase inhibitors |
| WO2005121094A1 (en) * | 2004-06-09 | 2005-12-22 | Pfizer Limited | Piperazine and piperidine derivatives as anti-hiv-agents |
| EP1772454A4 (en) * | 2004-07-23 | 2009-02-25 | Mitsubishi Tanabe Pharma Corp | NITROGENIC CONDENSED BICYCLIC COMPOUND |
| PE20061119A1 (es) * | 2005-01-19 | 2006-11-27 | Aventis Pharma Sa | PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie |
| JP2009525046A (ja) * | 2006-01-31 | 2009-07-09 | エラン ファーマシューティカルズ，インコーポレイテッド | アルファ−シヌクレインキナーゼ |
| US20100273776A1 (en) * | 2006-03-29 | 2010-10-28 | FOLDRx PHARMACEUTICALS, INC | Inhibition of alpha-synuclein toxicity |
| PE20110854A1 (es) * | 2008-09-26 | 2011-12-23 | Boehringer Ingelheim Int | DERIVADOS DE 1-FENIL-1H-PIRAZOLO[3,4-c]PIRIDINA-4-CARBONILAMINA COMO ANTAGONISTAS DE LOS RECEPTORES CCR1 |
| GB201015949D0 (en) * | 2010-09-22 | 2010-11-03 | Medical Res Council Technology | Compounds |
-
2010
- 2010-03-19 EP EP10711443.1A patent/EP2408772B1/en not_active Not-in-force
- 2010-03-19 AU AU2010224693A patent/AU2010224693B2/en not_active Ceased
- 2010-03-19 KR KR1020117024068A patent/KR101700229B1/ko not_active Expired - Fee Related
- 2010-03-19 MX MX2011009807A patent/MX2011009807A/es not_active Application Discontinuation
- 2010-03-19 JP JP2012500308A patent/JP5732036B2/ja not_active Expired - Fee Related
- 2010-03-19 CA CA2754605A patent/CA2754605C/en not_active Expired - Fee Related
- 2010-03-19 US US12/727,754 patent/US20100317646A1/en not_active Abandoned
- 2010-03-19 PE PE2011001662A patent/PE20120506A1/es not_active Application Discontinuation
- 2010-03-19 WO PCT/GB2010/000498 patent/WO2010106333A1/en not_active Ceased
- 2010-03-19 CN CN201080021866.0A patent/CN102428084B/zh active Active
- 2010-03-19 RU RU2011142182/04A patent/RU2011142182A/ru unknown
-
2011
- 2011-09-13 CL CL2011002267A patent/CL2011002267A1/es unknown
- 2011-09-14 IL IL215147A patent/IL215147A0/en unknown
-
2017
- 2017-04-03 US US15/478,141 patent/US20170320870A1/en not_active Abandoned
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