PE20120081A1 - Derivados de 6-tert-butil-8-fluor-2-(2-hidroximetil-3-{1-metil-5-piridin-2-il-amino-6-oxo-1,6-dihidro-piridin-3-il}-fenil)-ftalazin-1-ona como inhibidores de la tirosina-quinasa de bruton - Google Patents
Derivados de 6-tert-butil-8-fluor-2-(2-hidroximetil-3-{1-metil-5-piridin-2-il-amino-6-oxo-1,6-dihidro-piridin-3-il}-fenil)-ftalazin-1-ona como inhibidores de la tirosina-quinasa de brutonInfo
- Publication number
- PE20120081A1 PE20120081A1 PE2011001551A PE2011001551A PE20120081A1 PE 20120081 A1 PE20120081 A1 PE 20120081A1 PE 2011001551 A PE2011001551 A PE 2011001551A PE 2011001551 A PE2011001551 A PE 2011001551A PE 20120081 A1 PE20120081 A1 PE 20120081A1
- Authority
- PE
- Peru
- Prior art keywords
- pyridin
- methyl
- halogen
- hydroximethyl
- ona
- Prior art date
Links
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 title abstract 2
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- -1 AMINO Chemical class 0.000 abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical group [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 2
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
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- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- C07D237/30—Phthalazines
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Abstract
SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (A) DONDE R ES H, -R1, -R1-R2-R3, ENTRE OTROS, EN DONDE R1 ES ARILO, HETEROARILO, CICLOALQUILO, ENTRE OTROS; R2 ES -C(=O), -NHC(=O)O, -S(=O)2, ENTRE OTROS; R3 ES H O R4, EN DONDE R4 ES ALQUILO INFERIOR, ALCOXI INFERIOR, AMINO, ENTRE OTROS; X Y X' SON CADA UNO CH O N; Y1 ES H, ALQUILO INFERIOR O HALOALQUILO INFERIOR; Y2' E Y2 SON CADA UNO HALOGENO, OXIMA O ALQUILO INFERIOR OPCIONALMENTE SUSTITUIDO CON HIDROXI, ALCOXI INFERIOR, HALOGENO, ENTRE OTROS; n ES DE 0 A 2; Z* ES UN COMPUESTO DE FORMULA (Ia), (IIa), ENTRE OTROS, EN DONDE Y3 ES H, HALOGENO O ALQUILO INFERIOR; m ES 0 A 1; Y5 ES HALOGENO, HIDROXI, ALQUILO INFERIOR, ENTRE OTROS; Y4 ES Y4a, Y4b, ENTRE OTROS, EN DONDE Y4a ES H O HALOGENO; Y4b ES ALQUILO INFERIOR OPCIONALMENTE SUSTITUIDO. SON COMPUESTOS PREFERIDOS: 2-(3-{5-[5-(1-AMINO-1-METIL-ETIL)-PIRIDIN-2-ILAMINO]-1-METIL-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL}-2-HIDROXIMETIL-FENIL)-6-TERT-BUTIL-8-FLUOR-2H-FTALAZIN-1-ONA; 6-TERT-BUTIL-2-(3-{5-[5-(1-ETILAMINO-1-METIL-ETIL)-PIRIDIN-2-ILAMINO]-1-METIL-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL}-2-HIDROXIMETIL-FENIL)-8-FLUOR-2H-FTALAZIN-1-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA TIROSINA QUINASA DE BRUTON (Btk) SIENDO UTILES EN EL TRATAMIENTO DE ARTRITIS REUMATOIDE, PSORIASIS, ASMA
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20902109P | 2009-03-02 | 2009-03-02 | |
| US30006410P | 2010-02-01 | 2010-02-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20120081A1 true PE20120081A1 (es) | 2012-02-06 |
Family
ID=42097405
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001551A PE20120081A1 (es) | 2009-03-02 | 2010-02-25 | Derivados de 6-tert-butil-8-fluor-2-(2-hidroximetil-3-{1-metil-5-piridin-2-il-amino-6-oxo-1,6-dihidro-piridin-3-il}-fenil)-ftalazin-1-ona como inhibidores de la tirosina-quinasa de bruton |
| PE2015001561A PE20151336A1 (es) | 2009-03-02 | 2010-02-25 | Inhibidores de la tirosina-quinasa de bruton |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015001561A PE20151336A1 (es) | 2009-03-02 | 2010-02-25 | Inhibidores de la tirosina-quinasa de bruton |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US8299077B2 (es) |
| EP (1) | EP2403846B1 (es) |
| JP (1) | JP5512707B2 (es) |
| KR (1) | KR101347978B1 (es) |
| CN (2) | CN102341383B (es) |
| AR (1) | AR076066A1 (es) |
| AU (1) | AU2010220435B2 (es) |
| BR (1) | BRPI1009112A2 (es) |
| CA (1) | CA2753341C (es) |
| CL (1) | CL2011002115A1 (es) |
| ES (1) | ES2607644T3 (es) |
| HK (1) | HK1216887A1 (es) |
| IL (1) | IL214351A0 (es) |
| MX (1) | MX339583B (es) |
| PE (2) | PE20120081A1 (es) |
| RU (1) | RU2542585C2 (es) |
| SG (1) | SG173816A1 (es) |
| TW (2) | TW201439080A (es) |
| WO (1) | WO2010100070A1 (es) |
| ZA (1) | ZA201301679B (es) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8258134B2 (en) * | 2008-04-16 | 2012-09-04 | Hoffmann-La Roche Inc. | Pyridazinone glucokinase activators |
| KR101523451B1 (ko) * | 2008-07-02 | 2015-05-27 | 에프. 호프만-라 로슈 아게 | 키나아제 억제제로서의 신규 페닐피라지논 |
| CN102159214A (zh) | 2008-07-16 | 2011-08-17 | 药品循环公司 | 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂 |
| MX2011009824A (es) | 2009-03-23 | 2012-01-25 | Glenmark Pharmaceuticals Sa | Derivados de pirimidina-diona fusionados como moduladores del trpa1. |
| MX387728B (es) | 2010-06-03 | 2025-03-18 | Pharmacyclics Llc | El uso de inhibidores de la tirosina quinasa de bruton (btk). |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
| EP2611798B1 (en) | 2010-09-01 | 2015-04-08 | Gilead Connecticut, Inc. | Pyridazinones, method of making, and method of use thereof |
| BR112013007506A2 (pt) * | 2010-09-01 | 2016-07-12 | Genentech Inc | piridinonas/pirazinonas - métodos de criação e de uso |
| CN103582637B (zh) | 2011-05-17 | 2015-08-12 | 弗·哈夫曼-拉罗切有限公司 | 酪氨酸激酶抑制剂 |
| US20130178483A1 (en) * | 2011-06-28 | 2013-07-11 | Pharmacyclics, Inc. | Methods and Compositions for Inhibition of Bone Resorption |
| JP2014520863A (ja) | 2011-07-13 | 2014-08-25 | ファーマサイクリックス,インク. | Bruton型チロシンキナーゼの阻害剤 |
| KR20140052032A (ko) * | 2011-08-17 | 2014-05-02 | 에프. 호프만-라 로슈 아게 | 브루톤 티로신 키나아제의 억제제 |
| CA3110966A1 (en) * | 2011-10-19 | 2013-04-25 | Pharmacyclics Llc | Use of inhibitors of bruton's tyrosine kinase (btk) |
| HK1205111A1 (en) * | 2011-11-03 | 2015-12-11 | 霍夫曼-拉罗奇有限公司 | 8-fluorophthalazin-1 (2h) - one compounds as inhibitors of btk activity |
| UA111756C2 (uk) * | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| BR112014010439A2 (pt) * | 2011-11-03 | 2017-04-18 | F Hoffmann - La Roche Ag | compostos, composição farmacêutica, processo de produção, método de tratamento de uma doença ou distúrbio, métodos, kit e uso de uma composição farmacêutica |
| BR112014013582A8 (pt) * | 2011-12-09 | 2017-06-13 | Hoffmann La Roche | inibidores de quinase de tirosina de bruton |
| CA2869954C (en) | 2012-04-20 | 2023-01-03 | Advinus Therapeutics Limited | Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof in medical conditions related to modulation of bruton's tyrosine kinase activity |
| WO2013157021A1 (en) | 2012-04-20 | 2013-10-24 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
| BR112015001690A2 (pt) | 2012-07-24 | 2017-11-07 | Pharmacyclics Inc | mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk) |
| US20140045813A1 (en) | 2012-08-10 | 2014-02-13 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds as btk inhibitors |
| KR20150054994A (ko) * | 2012-09-13 | 2015-05-20 | 에프. 호프만-라 로슈 아게 | 브루톤 티로신 키나아제의 억제제 |
| CN104812746B (zh) * | 2012-11-16 | 2017-03-08 | 弗·哈夫曼-拉罗切有限公司 | 布鲁顿氏酪氨酸激酶抑制剂 |
| JP6042995B2 (ja) * | 2012-11-30 | 2016-12-14 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | ブルトン型チロシンキナーゼの阻害薬 |
| JP6089124B2 (ja) * | 2013-03-05 | 2017-03-01 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | ブルトン型チロシンキナーゼの阻害薬 |
| JP2016510051A (ja) * | 2013-03-05 | 2016-04-04 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | ブルトン型チロシンキナーゼの阻害剤 |
| CN105492011A (zh) | 2013-04-08 | 2016-04-13 | 丹尼斯·M·布朗 | 不理想给药化学化合物的治疗增效 |
| CA2902686C (en) | 2013-04-25 | 2017-01-24 | Beigene, Ltd. | Fused heterocyclic compounds as protein kinase inhibitors |
| CN104177338B (zh) * | 2013-05-22 | 2018-04-03 | 南京勇山生物科技有限公司 | 一类布鲁顿激酶抑制剂 |
| CN104211703B (zh) * | 2013-05-30 | 2018-04-03 | 南京勇山生物科技有限公司 | 一类作为布鲁顿激酶抑制剂的稠杂环化合物 |
| EP3016943B1 (en) * | 2013-07-03 | 2019-08-21 | F. Hoffmann-La Roche AG | Heteroaryl pyridone and aza-pyridone amide compounds |
| JP6156953B2 (ja) * | 2013-07-26 | 2017-07-05 | カルナバイオサイエンス株式会社 | 新規トリアジン誘導体 |
| CN105764501A (zh) | 2013-07-26 | 2016-07-13 | 现代化制药公司 | 改善比生群治疗效益的组合物 |
| WO2015023703A1 (en) | 2013-08-12 | 2015-02-19 | Pharmacyclics, Inc. | Methods for the treatment of her2 amplified cancer |
| AU2013400609B9 (en) | 2013-09-13 | 2020-03-05 | Beone Medicines I Gmbh | Anti-PD1 antibodies and their use as therapeutics and diagnostics |
| US9512084B2 (en) * | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
| CN105793251B (zh) * | 2013-12-05 | 2018-10-12 | 豪夫迈·罗氏有限公司 | 具有亲电子官能性的杂芳基吡啶酮和氮杂-吡啶酮化合物 |
| MX374759B (es) * | 2013-12-13 | 2025-03-06 | Hoffmann La Roche | Inhibidores de tirosina cinasa de bruton. |
| JP2017509336A (ja) | 2014-03-20 | 2017-04-06 | ファーマサイクリックス エルエルシー | ホスホリパーゼcガンマ2及び耐性に関連した変異 |
| CN110156892B (zh) | 2014-07-03 | 2023-05-16 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| JP6507234B2 (ja) * | 2014-10-02 | 2019-04-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | ブルトンチロシンキナーゼ(btk)によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物 |
| CN104402828A (zh) * | 2014-11-05 | 2015-03-11 | 定陶县友帮化工有限公司 | 一种3-氨基-4-溴-6-氯哒嗪的合成方法 |
| TW201702218A (zh) | 2014-12-12 | 2017-01-16 | 美國杰克森實驗室 | 關於治療癌症、自體免疫疾病及神經退化性疾病之組合物及方法 |
| EP3042903B1 (en) | 2015-01-06 | 2019-08-14 | Impetis Biosciences Ltd. | Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof |
| SI3613745T1 (sl) | 2015-07-02 | 2021-12-31 | Acerta Pharma B.V. | Trdne oblike in formulacije (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin- 2-il)imidazo(1,5-a)pirazin-1-il)-n-(piridin-2-il)benzamida |
| RU2608128C1 (ru) * | 2015-11-12 | 2017-01-13 | федеральное государственное бюджетное образовательное учреждение высшего образования "Ростовский государственный медицинский университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО РостГМУ Минздрава России) | Способ лечения больных с х-сцепленной агаммаглобулинемией |
| US10570118B2 (en) * | 2016-01-13 | 2020-02-25 | Boehringer Ingelheim International Gmbh | Isoquinolones as BTK inhibitors |
| RU2749038C2 (ru) * | 2016-06-22 | 2021-06-03 | Шанхай Фокон Фармасьютикал Ко., Лтд. | Замещенные пирроло[2,3-d]пиридазин-4-оны и пиразоло[3,4-d]пиридазин-4-оны в качестве ингибиторов протеинкиназы |
| CN109475536B (zh) | 2016-07-05 | 2022-05-27 | 百济神州有限公司 | 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合 |
| CN110049976A (zh) | 2016-07-21 | 2019-07-23 | 比奥根Ma公司 | 布鲁顿氏酪氨酸激酶抑制剂的琥珀酸盐形式和组合物 |
| TWI865873B (zh) | 2016-08-16 | 2024-12-11 | 瑞士商百濟神州瑞士有限責任公司 | (s)-7-(1-丙烯醯基六氫吡啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氫吡唑並[1,5-a]嘧啶-3-甲醯胺的晶型、其製備和用途 |
| TWI739887B (zh) | 2016-08-19 | 2021-09-21 | 英屬開曼群島商百濟神州有限公司 | 使用包含btk抑制劑的組合產品治療癌症 |
| US20190201409A1 (en) | 2016-09-19 | 2019-07-04 | Mei Pharma, Inc. | Combination therapy |
| AR110282A1 (es) | 2016-12-02 | 2019-03-13 | Hoffmann La Roche | Compuestos de amida bicíclica y uso de éstos en el tratamiento de enfermedades mediadas por rip1 |
| WO2018102785A2 (en) | 2016-12-03 | 2018-06-07 | Juno Therapeutics, Inc. | Methods and compositions for use of therapeutic t cells in combination with kinase inhibitors |
| EP3573989A4 (en) | 2017-01-25 | 2020-11-18 | Beigene, Ltd. | CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A ] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION AND ASSOCIATED USES |
| TW202515616A (zh) | 2017-06-26 | 2025-04-16 | 英屬開曼群島商百濟神州有限公司 | 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途 |
| EP3652178B1 (en) | 2017-07-14 | 2024-01-24 | F. Hoffmann-La Roche AG | Bicyclic ketone compounds and methods of use thereof |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| KR102613433B1 (ko) | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
| WO2019086494A1 (en) | 2017-10-31 | 2019-05-09 | F. Hoffmann-La Roche Ag | Bicyclic sulfones and sulfoxides and methods of use thereof |
| US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
| CN112020500A (zh) | 2017-12-22 | 2020-12-01 | 拉文纳制药公司 | 作为磷脂酰肌醇磷酸激酶抑制剂的氨基吡啶衍生物 |
| CN111961035B (zh) * | 2019-05-20 | 2022-11-01 | 南京科技职业学院 | 一类含有羟基异喹啉类结构的化合物、药物组合物以及其应用 |
| WO2020249001A1 (zh) | 2019-06-10 | 2020-12-17 | 百济神州瑞士有限责任公司 | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| AU2022269229B2 (en) * | 2021-05-05 | 2025-02-06 | F. Hoffmann-La Roche Ag | Process for preparing btk inhibitors |
| US20250145574A1 (en) * | 2022-02-10 | 2025-05-08 | Carna Biosciences, Inc. | Fluoroisoquinoline compound and production method thereof |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
| CN119080748A (zh) * | 2024-08-29 | 2024-12-06 | 中南大学 | 一种靶向brd7抑瘤蛋白的增稳剂及其在制备治疗实体肿瘤药物中的应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7312341B2 (en) | 2002-09-09 | 2007-12-25 | Cgi Pharmaceuticals, Inc. | 6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof |
| US7405295B2 (en) | 2003-06-04 | 2008-07-29 | Cgi Pharmaceuticals, Inc. | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds |
| MX2007007424A (es) * | 2004-12-24 | 2007-07-17 | Astrazeneca Ab | Derivados de amina. |
| AR063706A1 (es) | 2006-09-11 | 2009-02-11 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. |
| PE20081370A1 (es) * | 2006-09-11 | 2008-11-28 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas |
| JP5587193B2 (ja) * | 2007-10-23 | 2014-09-10 | エフ.ホフマン−ラ ロシュ アーゲー | 新規なキナーゼ阻害剤 |
| JP5643105B2 (ja) | 2007-12-14 | 2014-12-17 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 新規イミダゾ[1,2−a]ピリジン及びイミダゾ[1,2−b]ピリダジン誘導体 |
| AU2009211514B2 (en) | 2008-02-05 | 2014-02-20 | F. Hoffmann-La Roche Ag | Novel pyridinones and pyridazinones |
| US7683064B2 (en) | 2008-02-05 | 2010-03-23 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| WO2009156284A1 (en) | 2008-06-24 | 2009-12-30 | F. Hoffmann-La Roche Ag | Novel substituted pyridin-2-ones and pyridazin-3-ones |
| KR101523451B1 (ko) * | 2008-07-02 | 2015-05-27 | 에프. 호프만-라 로슈 아게 | 키나아제 억제제로서의 신규 페닐피라지논 |
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