JP2005510472A5 - - Google Patents
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- JP2005510472A5 JP2005510472A5 JP2003530670A JP2003530670A JP2005510472A5 JP 2005510472 A5 JP2005510472 A5 JP 2005510472A5 JP 2003530670 A JP2003530670 A JP 2003530670A JP 2003530670 A JP2003530670 A JP 2003530670A JP 2005510472 A5 JP2005510472 A5 JP 2005510472A5
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- JP
- Japan
- Prior art keywords
- group
- methyl
- aminomethyl
- atom
- tert
- 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.)
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- -1 cyclopropylmethoxy group Chemical group 0.000 description 26
- 125000003545 alkoxy group Chemical group 0.000 description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 description 1
- HLVFKOKELQSXIQ-UHFFFAOYSA-N 1-bromo-2-methylpropane Chemical compound CC(C)CBr HLVFKOKELQSXIQ-UHFFFAOYSA-N 0.000 description 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- 125000004414 alkyl thio group Chemical group 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 description 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 125000004429 atoms Chemical group 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- 125000004106 butoxy group Chemical group [*]OC([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
- 125000006309 butyl amino group Chemical group 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 125000004093 cyano group Chemical group *C#N 0.000 description 1
- 125000000000 cycloalkoxy group Chemical group 0.000 description 1
- 125000000753 cycloalkyl group Chemical group 0.000 description 1
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001352 cyclobutyloxy group Chemical group C1(CCC1)O* 0.000 description 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 description 1
- 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 description 1
- 125000001887 cyclopentyloxy group Chemical group C1(CCCC1)O* 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 125000000131 cyclopropyloxy group Chemical group C1(CC1)O* 0.000 description 1
- 125000004663 dialkyl amino group Chemical group 0.000 description 1
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000006264 diethylaminomethyl group Chemical group [H]C([H])([H])C([H])([H])N(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 description 1
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000006534 ethyl amino methyl group Chemical group [H]N(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 description 1
- 125000004705 ethylthio group Chemical group C(C)S* 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 125000005842 heteroatoms Chemical group 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 125000006316 iso-butyl amino group Chemical group [H]N(*)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000002510 isobutoxy group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])O* 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000005921 isopentoxy group Chemical group 0.000 description 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000006533 methyl amino methyl group Chemical group [H]N(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 description 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 description 1
- 125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 125000004433 nitrogen atoms Chemical group N* 0.000 description 1
- 125000004430 oxygen atoms Chemical group O* 0.000 description 1
- 125000004115 pentoxy group Chemical group [*]OC([H])([H])C([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 125000004894 pentylamino group Chemical group C(CCCC)N* 0.000 description 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
- 125000006308 propyl amino group Chemical group 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 125000004434 sulfur atoms Chemical group 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000006318 tert-butyl amino group Chemical group [H]N(*)C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 125000003774 valeryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
Description
Ｒ6で示されるベンゼン環が、１又は２以上の置換基を有している場合は、該環はさらにメチル基、エチル基、プロピル基、イソプロピル基、ブチル基、イソブチル基、ｓｅｃ−ブチル基、ｔｅｒｔ−ブチル基、ペンチル基、イソペンチル基、ネオペンチル基、１，１−ジメチルプロピル基などのＣ1〜Ｃ5のアルキル基；シクロプロピル基、シクロブチル基、シクロペンチル基、シクロヘキシル基などのＣ3〜Ｃ6のシクロアルキル基；シクロプロピロキシ基、シクロブチロキシ基、シクロペンチロキシ基、シクロヘキシロキシ基などのＣ3〜Ｃ6のシクロアルキロキシ基；水酸基；メトキシ基、エトキシ基、プロポキシ基、イソプロポキシ基、ブトキシ基、イソブトキシ基、ｔｅｒｔ−ブトキシ基、ペンチロキシ基、イソペンチロキシ基などのＣ1〜Ｃ5のアルコキシ基；シクロプロピルメトキシ基、シクロペンチルメトキシ基などのＣ4〜Ｃ7のシクロアルキルアルコキシ基；メチルチオ基、エチルチオ基、プロピルチオ基、ブチルチオ基、及びペンチルチオ基などのＣ1〜Ｃ5のアルキルチオ基；メタンスルホニル基、エタンスルホニル基、プロパンスルホニル基、ブタンスルホニル基、及びペンタンスルホニル基などのＣ1〜Ｃ5のアルキルスルホニル基；フッ素原子、塩素原子、臭素原子、及びヨウ素原子などのハロゲン原子；トリフルオロメチル基などのＣ1〜Ｃ5のハロゲン化アルキル基；トリフルオロメトキシ基、２，２，２−トリフルオロエトキシ基などのＣ1〜Ｃ5のハロゲン化アルコキシ基；水酸基；シアノ基；ニトロ基；ホルミル基；アセチル基、プロピオニル基、ブチリル基、及びバレリル基などのＣ2〜Ｃ6のアルキルカルボニル基；置換されていてもよいベンゼン環、置換されていてもよいナフタレン環、酸素原子、硫黄原子、及び窒素原子から成る群から選ばれる１〜4個のヘテロ原子を有し、かつ５〜１０個の環構成原子を有する、置換されていることもあるヘテロ環、置換されていてもよいフェノキシ基；置換されていてもよいフェニルアミノ基；アミノ基；メチルアミノ基、エチルアミノ基、プロピルアミノ基、イソプロピルアミノ基、ブチルアミノ基、イソブチルアミノ基、ｔｅｒｔ−ブチルアミノ基、ペンチルアミノ基、及びイソペンチルアミノ基などのＣ1〜Ｃ5のモノアルキルアミノ基；ジメチルアミノ基、エチルメチルアミノ基、ジエチルアミノ基、メチルプロピルアミノ基、及びジイソプロピルアミノ基などのＣ2〜Ｃ10のジアルキルアミノ基；メチルアミノメチル基、エチルアミノメチル基、プロピルアミノメチル基、イソブロピルアミノメチル基、ブチルアミノメチル基、イソブチルアミノメチル基、ｔｅｒｔ−ブチルアミノメチル基、ペンチルアミノメチル基、イソペンチルアミノメチル基などのＣ2〜Ｃ10のモノアルキルアミノメチル基；ジメチルアミノメチル基、ジエチルアミノメチル基、エチルメチルアミノメチル基、メチルプロピルアミノメチル基などのＣ3〜Ｃ11のジアルキルアミノメチル基；ピロリジニルメチル基；ピペリジニルメチル基；モルホリノメチル基；ピペラジニルメチル基；ピロリルメチル基；イミダゾリルメチル基；ピラゾリルメチル基；及びトリアゾリルメチル基から成る群から選ばれる1又は2以上の置換基を有していてもよい。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2001331674 | 2001-09-21 | ||
| JP2001331678 | 2001-09-21 | ||
| JP2001331675 | 2001-09-21 | ||
| JP2001331676 | 2001-09-21 | ||
| PCT/JP2002/009684 WO2003027080A1 (en) | 2001-09-21 | 2002-09-20 | 3-substituted-4-pyrimidone derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005510472A JP2005510472A (ja) | 2005-04-21 |
| JP2005510472A5 true JP2005510472A5 (ja) | 2006-02-09 |
| JP4368682B2 JP4368682B2 (ja) | 2009-11-18 |
Family
ID=27482650
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003530670A Expired - Lifetime JP4368682B2 (ja) | 2001-09-21 | 2002-09-20 | ３−置換−４−ピリミドン誘導体 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US7572793B2 (ja) |
| EP (1) | EP1427709B1 (ja) |
| JP (1) | JP4368682B2 (ja) |
| KR (1) | KR100754596B1 (ja) |
| CN (1) | CN1319950C (ja) |
| AR (2) | AR043700A1 (ja) |
| AT (1) | ATE312827T1 (ja) |
| AU (1) | AU2002337498B2 (ja) |
| BR (1) | BR0212893A (ja) |
| CA (1) | CA2460177C (ja) |
| CY (1) | CY1105554T1 (ja) |
| DE (1) | DE60208051T2 (ja) |
| DK (1) | DK1427709T3 (ja) |
| EA (1) | EA007224B1 (ja) |
| ES (1) | ES2256540T3 (ja) |
| HK (1) | HK1068608A1 (ja) |
| HU (1) | HUP0401898A3 (ja) |
| IL (2) | IL160701A0 (ja) |
| MX (1) | MXPA04002661A (ja) |
| NO (1) | NO326694B1 (ja) |
| NZ (1) | NZ531637A (ja) |
| PL (1) | PL368816A1 (ja) |
| TW (1) | TWI303171B (ja) |
| WO (1) | WO2003027080A1 (ja) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR023052A1 (es) | 1998-09-25 | 2002-09-04 | Mitsuharu Yoshimura Milton | Derivados de pirimidona |
| EA007576B1 (ru) | 2001-09-21 | 2006-12-29 | Мицубиси Фарма Корпорейшн | Производные 3-замещенных 4-пиримидонов |
| KR100956052B1 (ko) * | 2002-12-16 | 2010-05-06 | 미쓰비시 타나베 파마 코퍼레이션 | 3-치환-4-피리미돈 유도체 |
| US7550590B2 (en) | 2003-03-25 | 2009-06-23 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| TWI357408B (en) * | 2003-03-26 | 2012-02-01 | Mitsubishi Tanabe Pharma Corp | 3-substituted-4-pyrimidone derivatives |
| ZA200602051B (en) | 2003-08-13 | 2007-10-31 | Takeda Pharmaceutical | 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors |
| WO2005026148A1 (en) | 2003-09-08 | 2005-03-24 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| CN102127053A (zh) | 2004-03-15 | 2011-07-20 | 武田药品工业株式会社 | 二肽基肽酶抑制剂 |
| TW200621760A (en) * | 2004-09-09 | 2006-07-01 | Mitsubishi Pharma Corp | 2-morpholino-4-pyrimidone compound |
| BRPI0515851A (pt) | 2004-09-29 | 2008-08-12 | Mitsubishi Pharma Corp | composto de pirimidona |
| US7872124B2 (en) | 2004-12-21 | 2011-01-18 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| GB0510142D0 (en) * | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds A1 |
| GB0510141D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B3 |
| TW200740779A (en) * | 2005-07-22 | 2007-11-01 | Mitsubishi Pharma Corp | Intermediate compound for synthesizing pharmaceutical agent and production method thereof |
| DK1942898T4 (da) | 2005-09-14 | 2014-06-02 | Takeda Pharmaceutical | Dipeptidylpeptidase-inhibitorer til behandling af diabetes |
| KR101368988B1 (ko) | 2005-09-16 | 2014-02-28 | 다케다 야쿠힌 고교 가부시키가이샤 | 디펩티딜 펩티다제 억제제 |
| TW200813015A (en) * | 2006-03-15 | 2008-03-16 | Mitsubishi Pharma Corp | 2-(cyclic amino)-pyrimidone derivatives |
| EP2057141B1 (en) * | 2006-08-23 | 2011-10-26 | Pfizer Products Inc. | Pyrimidone compounds as gsk-3 inhibitors |
| US8324383B2 (en) | 2006-09-13 | 2012-12-04 | Takeda Pharmaceutical Company Limited | Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| AR064660A1 (es) * | 2006-12-26 | 2009-04-15 | Mitsubishi Tanabe Pharma Corp | Derivados de pirimidinona 6-heterociclica 2-sustituida, medicamentos que los contienen y usos para prevenir y/o tratar enfermedades neurodegenerativas entre otras |
| US8093236B2 (en) | 2007-03-13 | 2012-01-10 | Takeda Pharmaceuticals Company Limited | Weekly administration of dipeptidyl peptidase inhibitors |
| EP2193129B1 (en) * | 2007-09-14 | 2012-10-24 | Mitsubishi Tanabe Pharma Corporation | 6-pyrimidinyl-pyrimid-2-one derivative |
| EP2078717A1 (en) | 2008-01-11 | 2009-07-15 | sanofi-aventis | 6-Pyrimidinyl-pyrimid-2-one derivative |
| EA201070366A1 (ru) * | 2007-09-14 | 2010-08-30 | Санофи-Авентис | 3-метил-2-((2s)-2-(4-(3-метил-1,2,4-оксадиазол-5-ил)фенил)морфолино)-6-(пиримидин-4-ил)пиримидин-4(3н)-он в качестве ингибитора тау-протеинкиназы |
| AR076014A1 (es) | 2009-04-02 | 2011-05-11 | Sanofi Aventis | Derivados de 3- (1,4) oxazepan -4-pirimidona |
| EP2464639A1 (en) | 2009-08-13 | 2012-06-20 | Mitsubishi Tanabe Pharma Corporation | Pyrimidone derivatives used as tau protein kinase 1 inhibitors |
| WO2011019090A1 (en) | 2009-08-13 | 2011-02-17 | Mitsubishi Tanabe Pharma Corporation | Pyrimidone derivatives used as tau protein kinase 1 inhibitors |
| EP2550361B1 (en) | 2010-03-25 | 2017-02-08 | The J. David Gladstone Institutes | Compositions and methods for treating neurological disorders |
| CA2831331C (en) | 2011-04-21 | 2019-10-15 | The Regents Of The University Of California | Functionalized magnetic nanoparticles and use in imaging amyloid deposits and neurofibrillary tangles |
| KR101631003B1 (ko) * | 2012-01-12 | 2016-06-15 | 에프. 호프만-라 로슈 아게 | 미량 아민 결합 수용체(taar)로서 헤테로환형 유도체 |
| JP6290212B2 (ja) | 2012-08-16 | 2018-03-07 | アイピエリアン，インコーポレイティド | タウオパチーの処置方法 |
| CN104870475B (zh) | 2012-10-25 | 2019-11-08 | 美国比奥维拉迪维股份有限公司 | 抗补体C1s抗体和其用途 |
| CA2889197A1 (en) | 2012-11-02 | 2014-05-08 | True North Therapeutics, Inc. | Anti-complement c1s antibodies and uses thereof |
| ES2800827T3 (es) | 2013-06-10 | 2021-01-04 | Ipierian Inc | Procedimientos de tratamiento de una tauopatía |
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-
2002
- 2002-09-20 AT AT02772870T patent/ATE312827T1/de active
- 2002-09-20 JP JP2003530670A patent/JP4368682B2/ja not_active Expired - Lifetime
- 2002-09-20 AR ARP020103546A patent/AR043700A1/es unknown
- 2002-09-20 PL PL02368816A patent/PL368816A1/xx not_active Application Discontinuation
- 2002-09-20 NZ NZ531637A patent/NZ531637A/en not_active IP Right Cessation
- 2002-09-20 IL IL16070102A patent/IL160701A0/xx unknown
- 2002-09-20 KR KR1020047004113A patent/KR100754596B1/ko not_active IP Right Cessation
- 2002-09-20 AU AU2002337498A patent/AU2002337498B2/en not_active Ceased
- 2002-09-20 CA CA2460177A patent/CA2460177C/en not_active Expired - Fee Related
- 2002-09-20 EA EA200400452A patent/EA007224B1/ru not_active IP Right Cessation
- 2002-09-20 HU HU0401898A patent/HUP0401898A3/hu unknown
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