JP2011509949A5 - - Google Patents
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- Publication number
- JP2011509949A5 JP2011509949A5 JP2010542509A JP2010542509A JP2011509949A5 JP 2011509949 A5 JP2011509949 A5 JP 2011509949A5 JP 2010542509 A JP2010542509 A JP 2010542509A JP 2010542509 A JP2010542509 A JP 2010542509A JP 2011509949 A5 JP2011509949 A5 JP 2011509949A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- halo
- alkyl
- subject
- tumor
- 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 description 37
- 206010028980 Neoplasm Diseases 0.000 claims description 20
- 125000001475 halogen functional group Chemical group 0.000 claims description 14
- 239000003814 drug Substances 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 230000002401 inhibitory effect Effects 0.000 claims description 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- -1 trifluoro Chemical group 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 4
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 4
- 230000005907 cancer growth Effects 0.000 claims description 4
- 230000004663 cell proliferation Effects 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 150000002431 hydrogen Chemical class 0.000 claims description 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 230000001613 neoplastic effect Effects 0.000 claims description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- 230000004614 tumor growth Effects 0.000 claims description 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- 230000001413 cellular effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 6
- 239000000543 intermediate Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2224708P | 2008-01-18 | 2008-01-18 | |
| US61/022,247 | 2008-01-18 | ||
| PCT/CZ2009/000004 WO2009089804A1 (en) | 2008-01-18 | 2009-01-15 | Novel cytostatic 7-deazapurine nucleosides |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013266910A Division JP2014058567A (ja) | 2008-01-18 | 2013-12-25 | 新規な細胞増殖抑制性7−デアザプリンヌクレオシド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011509949A JP2011509949A (ja) | 2011-03-31 |
| JP2011509949A5 true JP2011509949A5 (OSRAM) | 2013-02-21 |
| JP5485172B2 JP5485172B2 (ja) | 2014-05-07 |
Family
ID=40434932
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010542509A Active JP5485172B2 (ja) | 2008-01-18 | 2009-01-15 | 新規な細胞増殖抑制性7−デアザプリンヌクレオシド |
| JP2013266910A Withdrawn JP2014058567A (ja) | 2008-01-18 | 2013-12-25 | 新規な細胞増殖抑制性7−デアザプリンヌクレオシド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013266910A Withdrawn JP2014058567A (ja) | 2008-01-18 | 2013-12-25 | 新規な細胞増殖抑制性7−デアザプリンヌクレオシド |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8093226B2 (OSRAM) |
| EP (2) | EP2231689B1 (OSRAM) |
| JP (2) | JP5485172B2 (OSRAM) |
| CN (1) | CN101977923B (OSRAM) |
| AU (1) | AU2009204568B2 (OSRAM) |
| CA (1) | CA2711384C (OSRAM) |
| CY (2) | CY1118104T1 (OSRAM) |
| DK (2) | DK3133080T3 (OSRAM) |
| ES (2) | ES2693551T3 (OSRAM) |
| HR (2) | HRP20161344T1 (OSRAM) |
| HU (2) | HUE030767T2 (OSRAM) |
| LT (2) | LT2231689T (OSRAM) |
| NZ (1) | NZ586610A (OSRAM) |
| PL (2) | PL2231689T3 (OSRAM) |
| PT (2) | PT2231689T (OSRAM) |
| SI (2) | SI2231689T1 (OSRAM) |
| TR (1) | TR201815961T4 (OSRAM) |
| WO (1) | WO2009089804A1 (OSRAM) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3184526T3 (en) * | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| DK2740731T3 (en) | 2007-06-13 | 2016-04-11 | Incyte Holdings Corp | CRYSTALLINE SALTS OF JANUSKINASEINHIBITOREN (R) -3- (4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-CYCLOPENTYLPROPANNITRIL |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| JP5721275B2 (ja) * | 2009-04-22 | 2015-05-20 | インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエス シーアール, ブイ.ブイ.アイ. | 治療的使用のための新規7−デアザプリンヌクレオシド |
| MY156727A (en) | 2009-05-22 | 2016-03-15 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| AU2010249443B2 (en) * | 2009-05-22 | 2015-08-13 | Incyte Holdings Corporation | 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as JAK inhibitors |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| AU2011224484A1 (en) | 2010-03-10 | 2012-09-27 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
| MY161078A (en) | 2010-05-21 | 2017-04-14 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| EP2640392B1 (en) * | 2010-11-18 | 2015-01-07 | Kasina Laila Innova Pharmaceuticals Private Ltd. | Substituted 4-(selenophen-2(or 3)-ylamino)pyrimidine compounds and methods of use thereof |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| EP2640723A1 (en) | 2010-11-19 | 2013-09-25 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| KR20140040819A (ko) | 2011-06-20 | 2014-04-03 | 인사이트 코포레이션 | Jak 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체 |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| PH12020551186B1 (en) | 2012-11-15 | 2024-03-20 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| JP6397831B2 (ja) | 2013-03-06 | 2018-09-26 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害剤の製造方法及びその中間体 |
| KR20160045081A (ko) | 2013-08-07 | 2016-04-26 | 인사이트 코포레이션 | Jak1 억제제용 지속 방출 복용 형태 |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| EP3478701B1 (en) | 2016-06-29 | 2022-08-10 | Ustav organicke chemie a biochemie AV CR, v.v.i. | Substituted thienopyrrolopyrimidine ribonucleosides for therapeutic use |
| CZ307334B6 (cs) | 2016-08-02 | 2018-06-13 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | Substituované heteropentadieno-pyrrolopyrimidinové ribonukleosidy pro terapeutické použití |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| CN112105608B (zh) | 2018-01-30 | 2023-07-14 | 因赛特公司 | 制备(1-(3-氟-2-(三氟甲基)异烟碱基)哌啶-4-酮)的方法 |
| CZ308104B6 (cs) | 2018-03-12 | 2020-01-08 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v. v. i. | Pyridinopyrrolopyrimidinové ribonukleosidy pro terapeutické použití |
| SMT202400306T1 (it) | 2018-03-30 | 2024-09-16 | Incyte Corp | Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak. |
| JP2022527556A (ja) * | 2019-04-05 | 2022-06-02 | プレリュード・セラピューティクス・インコーポレイテッド | プロテインアルギニンメチルトランスフェラーゼ5の選択的阻害剤 |
| WO2020255979A1 (ja) * | 2019-06-18 | 2020-12-24 | 大鵬薬品工業株式会社 | ピロロピリミジン骨格を有する新規なカーボネート化合物又はその薬学的に許容可能な塩 |
| WO2021164848A1 (en) * | 2020-02-17 | 2021-08-26 | Katholieke Universiteit Leuven | Novel 6-substituted 7-deazapurines and corresponding nucleosides as medicaments |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN112190590A (zh) * | 2020-11-06 | 2021-01-08 | 牡丹江医学院 | 一种治疗动脉粥样硬化的硒核苷及其药物组合物 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS50125033A (OSRAM) * | 1974-03-19 | 1975-10-01 | ||
| IL108523A0 (en) * | 1993-02-03 | 1994-05-30 | Gensia Inc | Pharmaceutical compositions containing adenosine kinase inhibitors for preventing or treating conditions involving inflammatory responses and pain |
| JPH10158293A (ja) * | 1996-08-08 | 1998-06-16 | Rikagaku Kenkyusho | 3’−デオキシリボヌクレオチド誘導体 |
| JP3318579B2 (ja) * | 1997-07-07 | 2002-08-26 | 理化学研究所 | Dnaの塩基配列決定方法 |
| JP3489991B2 (ja) * | 1997-07-07 | 2004-01-26 | 理化学研究所 | 3’−デオキシリボヌクレオチド誘導体 |
| CZ9901996A3 (cs) * | 1999-06-04 | 2001-01-17 | Ústav organické chemie a biochemie AV ČR | Nové 6-fenylpurinové 9-ß-D-ribonukleosidy s antineoplastickým účinkem, jejich použití k přípravě farmaceutických preparátů a farmaceutické přípravky, které je obsahují |
| WO2003051899A1 (en) * | 2001-12-17 | 2003-06-26 | Ribapharm Inc. | Deazapurine nucleoside libraries and compounds |
| DE602004029904D1 (de) | 2003-08-27 | 2010-12-16 | Biota Scient Management | Neue tricyclische nukleoside oder nukleotide als therapeutische mittel |
| US20080280842A1 (en) * | 2004-10-21 | 2008-11-13 | Merck & Co., Inc. | Fluorinated Pyrrolo[2,3-D]Pyrimidine Nucleosides for the Treatment of Rna-Dependent Rna Viral Infection |
| CN101043893A (zh) * | 2004-10-21 | 2007-09-26 | 默克公司 | 治疗RNA-依赖性RNA病毒感染的氟化吡咯并[2,3-d]嘧啶核苷 |
| TW200720285A (en) * | 2005-04-25 | 2007-06-01 | Genelabs Tech Inc | Nucleoside compounds for treating viral infections |
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2009
- 2009-01-15 EP EP09702842.7A patent/EP2231689B1/en active Active
- 2009-01-15 HU HUE09702842A patent/HUE030767T2/en unknown
- 2009-01-15 TR TR2018/15961T patent/TR201815961T4/tr unknown
- 2009-01-15 DK DK16174985.8T patent/DK3133080T3/en active
- 2009-01-15 LT LTEP09702842.7T patent/LT2231689T/lt unknown
- 2009-01-15 LT LTEP16174985.8T patent/LT3133080T/lt unknown
- 2009-01-15 HU HUE16174985A patent/HUE041598T2/hu unknown
- 2009-01-15 US US12/354,432 patent/US8093226B2/en active Active
- 2009-01-15 PL PL09702842T patent/PL2231689T3/pl unknown
- 2009-01-15 NZ NZ586610A patent/NZ586610A/xx unknown
- 2009-01-15 PT PT97028427T patent/PT2231689T/pt unknown
- 2009-01-15 SI SI200931535A patent/SI2231689T1/sl unknown
- 2009-01-15 WO PCT/CZ2009/000004 patent/WO2009089804A1/en not_active Ceased
- 2009-01-15 PL PL16174985T patent/PL3133080T3/pl unknown
- 2009-01-15 ES ES16174985.8T patent/ES2693551T3/es active Active
- 2009-01-15 CN CN200980109880.3A patent/CN101977923B/zh active Active
- 2009-01-15 SI SI200931882T patent/SI3133080T1/sl unknown
- 2009-01-15 ES ES09702842.7T patent/ES2598503T3/es active Active
- 2009-01-15 EP EP16174985.8A patent/EP3133080B1/en active Active
- 2009-01-15 DK DK09702842.7T patent/DK2231689T3/en active
- 2009-01-15 HR HRP20161344TT patent/HRP20161344T1/hr unknown
- 2009-01-15 PT PT16174985T patent/PT3133080T/pt unknown
- 2009-01-15 AU AU2009204568A patent/AU2009204568B2/en active Active
- 2009-01-15 JP JP2010542509A patent/JP5485172B2/ja active Active
- 2009-01-15 CA CA2711384A patent/CA2711384C/en active Active
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2013
- 2013-12-25 JP JP2013266910A patent/JP2014058567A/ja not_active Withdrawn
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2016
- 2016-10-19 CY CY20161101041T patent/CY1118104T1/el unknown
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2018
- 2018-10-29 HR HRP20181774TT patent/HRP20181774T1/hr unknown
- 2018-10-30 CY CY20181101120T patent/CY1121364T1/el unknown