JP2005529954A5 - - Google Patents
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- Publication number
- JP2005529954A5 JP2005529954A5 JP2004513249A JP2004513249A JP2005529954A5 JP 2005529954 A5 JP2005529954 A5 JP 2005529954A5 JP 2004513249 A JP2004513249 A JP 2004513249A JP 2004513249 A JP2004513249 A JP 2004513249A JP 2005529954 A5 JP2005529954 A5 JP 2005529954A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- following formula
- formula
- hydrogen
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 10
- 229940100198 alkylating agent Drugs 0.000 claims 6
- 239000002168 alkylating agent Substances 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- JHGRUPGVUMAQQU-UHFFFAOYSA-N 2,3-dimethyl-6-nitroindazole Chemical compound C1=C([N+]([O-])=O)C=CC2=C(C)N(C)N=C21 JHGRUPGVUMAQQU-UHFFFAOYSA-N 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 125000001769 aryl amino group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 230000005494 condensation Effects 0.000 claims 2
- 238000009833 condensation Methods 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims 2
- KTPBKMYOIFHJMI-UHFFFAOYSA-N 5-amino-2-methylbenzenesulfonamide Chemical compound CC1=CC=C(N)C=C1S(N)(=O)=O KTPBKMYOIFHJMI-UHFFFAOYSA-N 0.000 claims 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- FUNWSYKLFDLUIZ-UHFFFAOYSA-N Cc1n[nH]c2cc([N+]([O-])=O)ccc12 Chemical compound Cc1n[nH]c2cc([N+]([O-])=O)ccc12 FUNWSYKLFDLUIZ-UHFFFAOYSA-N 0.000 description 2
- 0 CC1=C2C=CC(N(C)c3nc(*c4cc(S(N)(=O)=O)c(C)cc4)ncc3)=CC2NN1C Chemical compound CC1=C2C=CC(N(C)c3nc(*c4cc(S(N)(=O)=O)c(C)cc4)ncc3)=CC2NN1C 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38934902P | 2002-06-17 | 2002-06-17 | |
| PCT/US2003/019211 WO2003106416A2 (en) | 2002-06-17 | 2003-06-17 | Chemical process |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005529954A JP2005529954A (ja) | 2005-10-06 |
| JP2005529954A5 true JP2005529954A5 (enExample) | 2006-08-03 |
Family
ID=29736629
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004513249A Pending JP2005529954A (ja) | 2002-06-17 | 2003-06-17 | 化学プロセス |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20060252943A1 (enExample) |
| EP (1) | EP1515955A4 (enExample) |
| JP (1) | JP2005529954A (enExample) |
| CN (1) | CN1688553A (enExample) |
| AU (1) | AU2003276125B2 (enExample) |
| CA (1) | CA2489648A1 (enExample) |
| IL (1) | IL165286A0 (enExample) |
| MX (1) | MXPA04012860A (enExample) |
| PL (1) | PL374963A1 (enExample) |
| WO (1) | WO2003106416A2 (enExample) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| RS51752B (sr) | 2002-07-29 | 2011-12-31 | Rigel Pharmaceuticals | Metode tretiranja i prevencije autoimunih oboljenja jedinjenjima 2,4-pirimidindiamina |
| KR20050122220A (ko) | 2003-03-25 | 2005-12-28 | 다케다 샌디에고, 인코포레이티드 | 디펩티딜 펩티다제 억제제 |
| HRP20130602T1 (en) | 2003-07-30 | 2013-07-31 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| US7790736B2 (en) | 2003-08-13 | 2010-09-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US8003744B2 (en) | 2003-08-25 | 2011-08-23 | Kaneka Corporation | Curing composition with improved heat resistance |
| US7790734B2 (en) | 2003-09-08 | 2010-09-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| CN102079743B (zh) | 2004-03-15 | 2020-08-25 | 武田药品工业株式会社 | 二肽基肽酶抑制剂 |
| WO2006020564A1 (en) * | 2004-08-09 | 2006-02-23 | Smithkline Beecham Corporation | Pyrimidin derivatives for the treatment of multiple myeloma |
| US7872124B2 (en) | 2004-12-21 | 2011-01-18 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| DE602006010979D1 (de) | 2005-01-19 | 2010-01-21 | Rigel Pharmaceuticals Inc | Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| CA2608367C (en) | 2005-06-08 | 2014-08-19 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| EP1942898B2 (en) | 2005-09-14 | 2014-05-14 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors for treating diabetes |
| CN102675221A (zh) | 2005-09-16 | 2012-09-19 | 武田药品工业株式会社 | 用于制备嘧啶二酮衍生物的方法中的中间体 |
| SI1954281T1 (sl) | 2005-11-29 | 2011-06-30 | Glaxosmithkline Llc | Postopek zdravljenja raka |
| JP5180834B2 (ja) | 2005-11-29 | 2013-04-10 | スミスクライン ビーチャム コーポレーション | 治療方法 |
| ES2622493T3 (es) | 2006-02-24 | 2017-07-06 | Rigel Pharmaceuticals, Inc. | Composiciones y métodos para la inhibición de la ruta de JAK |
| 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 |
| US8093236B2 (en) | 2007-03-13 | 2012-01-10 | Takeda Pharmaceuticals Company Limited | Weekly administration of dipeptidyl peptidase inhibitors |
| DK2154967T5 (en) | 2007-04-16 | 2014-11-17 | Hutchison Medipharma Entpr Ltd | Pyriminderivater |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| KR20100132550A (ko) | 2008-04-16 | 2010-12-17 | 포톨라 파마슈티컬스, 인코포레이티드 | ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드 |
| AU2009244897B2 (en) | 2008-04-16 | 2014-11-13 | Alexion Pharmaceuticals, Inc. | 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors |
| WO2009131687A2 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| US20120232102A1 (en) | 2009-09-30 | 2012-09-13 | Chun-Fang Xu | Methods Of Administration And Treatment |
| US20120197019A1 (en) * | 2009-10-23 | 2012-08-02 | Dharmesh Surendra Bhanushali | Compositions and processes |
| WO2011058179A1 (en) | 2009-11-16 | 2011-05-19 | Ratiopharm Gmbh | 5- (4- (n- (2, 3 -dimethyl- 2h- indazol- 6 -yl) -n-methylamino) pyrimidin- 2 -ylamino) -2 -methylbenzenesulfonamide |
| WO2011069053A1 (en) | 2009-12-04 | 2011-06-09 | Teva Pharmaceutical Industries Ltd. | Process for the preparation of pazopanip hcl and crystalline forms of pazopanib hcl |
| CA2816219C (en) | 2010-11-01 | 2019-10-29 | Portola Pharmaceuticals, Inc. | Nicotinamides as syk modulators |
| EP2635557A2 (en) | 2010-11-01 | 2013-09-11 | Portola Pharmaceuticals, Inc. | Nicotinamides as jak kinase modulators |
| US20130317029A1 (en) | 2010-11-01 | 2013-11-28 | Portola Pharmaceuticals, Inc. | Oxypyrimidines as syk modulators |
| CA2819118A1 (en) * | 2010-11-29 | 2012-06-07 | Hetero Research Foundation | A process for the preparation of pazopanib using novel intermediate |
| CN102060848B (zh) * | 2010-12-09 | 2013-09-18 | 天津药物研究院 | 芳香胺取代的嘧啶衍生物的制备及用途 |
| SG10201601352UA (en) | 2011-11-23 | 2016-03-30 | Portola Pharm Inc | Pyrazine kinase inhibitors |
| CN103319410B (zh) * | 2012-03-22 | 2016-04-06 | 天津药物研究院 | 一种吲唑化合物的合成方法 |
| CN103373989B (zh) * | 2012-04-28 | 2016-04-13 | 上海医药工业研究院 | 盐酸帕唑帕尼的中间体的制备方法 |
| CN103373963B (zh) * | 2012-04-28 | 2015-07-08 | 上海医药工业研究院 | 盐酸帕唑帕尼的中间体及其制备方法 |
| EP2903970A4 (en) | 2012-10-08 | 2016-11-30 | Portola Pharm Inc | SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS |
| EP2935250B1 (en) | 2012-12-17 | 2018-03-28 | Sun Pharmaceutical Industries Limited | Process for the preparation of pazopanib or salts thereof |
| WO2014097152A1 (en) * | 2012-12-17 | 2014-06-26 | Ranbaxy Laboratories Limited | Process for the preparation of pazopanib or salts thereof |
| CN103232443B (zh) * | 2013-02-01 | 2014-12-10 | 天津药物研究院 | 一种吲唑衍生物的晶型及其制备和用途 |
| CN103450085B (zh) * | 2013-08-15 | 2015-11-18 | 凯莱英医药集团（天津）股份有限公司 | 一种盐酸帕唑帕尼关键中间体的制备方法 |
| WO2015068175A2 (en) * | 2013-11-05 | 2015-05-14 | Laurus Labs Private Limited | An improved process for the preparation of pazopanib or a pharmaceutically acceptable salt thereof |
| CN106565688B (zh) * | 2016-11-11 | 2018-08-31 | 重庆医科大学 | 帕唑帕尼二聚体及其制备方法和用途 |
| CN110028495B (zh) * | 2019-05-24 | 2019-12-03 | 济南爱思医药科技有限公司 | 帕唑帕尼盐酸盐的制备方法 |
| CN116554106A (zh) * | 2023-04-28 | 2023-08-08 | 扬州市普林斯医药科技有限公司 | 一种6-氯-2-甲基-2h-吲唑-5-胺的制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3755332A (en) * | 1971-07-01 | 1973-08-28 | Ciba Geigy Corp | Substituted 4 indazolaminoquinolines |
| GB9918035D0 (en) * | 1999-07-30 | 1999-09-29 | Novartis Ag | Organic compounds |
| ATE396978T1 (de) * | 1999-10-07 | 2008-06-15 | Amgen Inc | Triazin-kinase-hemmer |
| JP2003532635A (ja) * | 2000-02-17 | 2003-11-05 | アムジエン・インコーポレーテツド | キナーゼ阻害薬 |
| JP3711443B2 (ja) * | 2000-10-25 | 2005-11-02 | セイコーエプソン株式会社 | インクジェット式記録装置 |
| IL156306A0 (en) * | 2000-12-21 | 2004-01-04 | Glaxo Group Ltd | Pyrimidineamines as angiogenesis modulators |
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| GB0206215D0 (en) * | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
-
2003
- 2003-06-17 AU AU2003276125A patent/AU2003276125B2/en not_active Ceased
- 2003-06-17 EP EP03742050A patent/EP1515955A4/en not_active Withdrawn
- 2003-06-17 JP JP2004513249A patent/JP2005529954A/ja active Pending
- 2003-06-17 WO PCT/US2003/019211 patent/WO2003106416A2/en not_active Ceased
- 2003-06-17 PL PL03374963A patent/PL374963A1/xx not_active Application Discontinuation
- 2003-06-17 MX MXPA04012860A patent/MXPA04012860A/es unknown
- 2003-06-17 CN CNA038141698A patent/CN1688553A/zh active Pending
- 2003-06-17 CA CA002489648A patent/CA2489648A1/en not_active Abandoned
- 2003-06-17 US US10/518,349 patent/US20060252943A1/en not_active Abandoned
- 2003-06-17 IL IL16528603A patent/IL165286A0/xx unknown
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