CO6290767A2 - Nuevos derivados de 5-fenil-1h-piridin-2-ona y 6-fenil-2h-piridazin-3-0na como moduladores de la actividad de la btk - Google Patents
Nuevos derivados de 5-fenil-1h-piridin-2-ona y 6-fenil-2h-piridazin-3-0na como moduladores de la actividad de la btkInfo
- Publication number
- CO6290767A2 CO6290767A2 CO10090865A CO10090865A CO6290767A2 CO 6290767 A2 CO6290767 A2 CO 6290767A2 CO 10090865 A CO10090865 A CO 10090865A CO 10090865 A CO10090865 A CO 10090865A CO 6290767 A2 CO6290767 A2 CO 6290767A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- hydroxy
- halogen
- lower alkyl
- amino
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto de las fórmulas I, II o III:en las que:R es H, -R1, R1-R2-R3, -R1-R3 o -R2-R3;R1 es arilo, heteroarilo, cicloalquilo o heterocicloalquilo y está opcionalmente sustituido por uno o más alquilo inferior, hidroxi, hidroxialquilo inferior, alcoxi inferior, halógeno, nitro, amino, amido, ciano, oxo o haloalquilo inferior;R2 es -C(=O), -C(=O)O, -C(=O)NR2´, -NHC(=O)O, -C(=NH)NR2', o S(=O)2; en los que R2´ es H o alquilo inferior;R3 es H o R4; en el que R4 es alquilo inferior, amino, arilo, arilalquilo, alquilarilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, cicloalquilo, alquil-cicloalquilo, cicloalquil-alquilo, heterocicloalquilo, alquil-heterocicloalquilo o heterocicloalquil-alquilo y está opcionalmente sustituido por uno o más alquilo inferior, hidroxi, alcoxi inferior, hidroxi-alquilo inferior, hidroxi-alcoxi inferior, (alquilo inferior)-sulfonilo, (alquilo inferior)-sulfonamido, carbamato, carboxi, éster, amido, acilo, halógeno, nitro, amino, ciano, oxo o haloalquilo inferior;X es CH o N;Y1 es H, alquilo inferior o haloalquilo inferior;cada Y2 es con independencia halógeno, oxima o alquilo inferior, dicho alquilo inferior está opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por hidroxi, alcoxi inferior, haloalcoxi inferior, haloalquilo inferior, carboxi, amino y halógeno;n es el número 0,1, 2 ó 3;Y3 es H, halógeno o alquilo inferior, dicho alquilo inferior está opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por hidroxi, alcoxi inferior, amino y halógeno;m es el número 0 ó 1;Y4 es Y4a, Y4b, Y4c o Y4d; en el que Y4a es H o halógeno; Y4b es alquilo inferior, opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por haloalquilo inferior, halógeno, hidroxi, amino, ciano y alcoxi inferior; Y4c es cicloalquilo inferior, opcionalmente sustituido con uno o más sustituyentes elegidos entre el grupo formado por alquilo inferior, haloalquilo inferior, halógeno, hidroxi, amino, ciano y alcoxi inferior; e Y4d es amino, opcionalmente sustituido por uno o más alquilo inferior, alcoxi-alquilo inferior o hidroxi-alquilo inferior;o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2620408P | 2008-02-05 | 2008-02-05 | |
| US12251008P | 2008-12-15 | 2008-12-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6290767A2 true CO6290767A2 (es) | 2011-06-20 |
Family
ID=40413736
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO10090865A CO6290767A2 (es) | 2008-02-05 | 2010-07-26 | Nuevos derivados de 5-fenil-1h-piridin-2-ona y 6-fenil-2h-piridazin-3-0na como moduladores de la actividad de la btk |
Country Status (30)
| Country | Link |
|---|---|
| EP (1) | EP2242749B1 (es) |
| JP (1) | JP5259739B2 (es) |
| KR (1) | KR101308803B1 (es) |
| CN (1) | CN101932573B (es) |
| AR (1) | AR070408A1 (es) |
| AU (1) | AU2009211514B2 (es) |
| BR (1) | BRPI0907915A2 (es) |
| CA (1) | CA2710462C (es) |
| CL (1) | CL2009000229A1 (es) |
| CO (1) | CO6290767A2 (es) |
| CR (1) | CR11598A (es) |
| CY (1) | CY1114114T1 (es) |
| DK (1) | DK2242749T3 (es) |
| EC (1) | ECSP10010384A (es) |
| ES (1) | ES2420846T3 (es) |
| HK (1) | HK1146826A1 (es) |
| HR (1) | HRP20130615T1 (es) |
| IL (1) | IL206357A (es) |
| MA (1) | MA32064B1 (es) |
| MX (1) | MX2010008197A (es) |
| MY (1) | MY158411A (es) |
| NZ (1) | NZ586916A (es) |
| PE (1) | PE20091484A1 (es) |
| PL (1) | PL2242749T3 (es) |
| PT (1) | PT2242749E (es) |
| RU (1) | RU2505538C2 (es) |
| SI (1) | SI2242749T1 (es) |
| TW (1) | TWI382024B (es) |
| WO (1) | WO2009098144A1 (es) |
| ZA (1) | ZA201005539B (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5536049B2 (ja) | 2008-06-24 | 2014-07-02 | エフ．ホフマン−ラ ロシュ アーゲー | 新規な置換ピリジン−２−オン及びピリダジン−３−オン |
| US8299077B2 (en) * | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| EP2421854B1 (en) * | 2009-04-24 | 2014-07-23 | F.Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| US8785440B2 (en) | 2009-09-04 | 2014-07-22 | Biogen Idec Ma, Inc. | Bruton's tyrosine kinase inhibitors |
| CN103038233B (zh) * | 2010-05-07 | 2017-06-20 | 吉利德康涅狄格有限公司 | 吡啶酮和氮杂吡啶酮化合物及使用方法 |
| EP2394998A1 (en) * | 2010-05-31 | 2011-12-14 | Almirall, S.A. | 3-(5-Amino-6-oxo-1,6-dihydropyridazin-3-yl)-biphenyl derivatives as PDE4 inhibitors |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
| EP2709997B1 (en) * | 2011-05-17 | 2016-06-29 | F.Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| MX349372B (es) * | 2011-08-17 | 2017-07-26 | Hoffmann La Roche | Inhibidores de la tirosina-cinasa de bruton. |
| UA111756C2 (uk) * | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| WO2013148603A1 (en) | 2012-03-27 | 2013-10-03 | Takeda Pharmaceutical Company Limited | Cinnoline derivatives as as btk inhibitors |
| BR112014024693A2 (pt) | 2012-04-05 | 2017-07-11 | Chdi Foundation Inc | composto de fórmula / ou um sal farmaceuticamente aceitável ou pró-fármaco do mesmo; composto; composição farmacêutica; método de tratamento de uma afecção ou distúrbio mediado por atividade de quinurenina 3-mono-oxigenase em um indivíduo que necessita de tal tratamento |
| CN104662018B (zh) | 2012-04-20 | 2017-10-24 | 阿迪维纳斯治疗有限公司 | 取代的杂双环化合物、组合物及其医疗应用 |
| AR091273A1 (es) * | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | Inhibidores de pirimidinil tirosina quinasa |
| KR20150054994A (ko) * | 2012-09-13 | 2015-05-20 | 에프. 호프만-라 로슈 아게 | 브루톤 티로신 키나아제의 억제제 |
| EP2920162B1 (en) * | 2012-11-16 | 2017-04-19 | F. Hoffmann-La Roche AG | Inhibitors of bruton's tyrosine kinase |
| EP2925323B1 (en) * | 2012-11-30 | 2017-05-17 | F. Hoffmann-La Roche AG | An inhibitor of bruton's tyrosine kinase |
| KR101763504B1 (ko) * | 2013-03-05 | 2017-07-31 | 에프. 호프만-라 로슈 아게 | 브루톤 티로신 키나아제의 억제제 |
| 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 |
| JO3377B1 (ar) | 2013-03-11 | 2019-03-13 | Takeda Pharmaceuticals Co | مشتقات بيريدينيل وبيريدينيل مندمج |
| ES2619125T3 (es) | 2013-04-25 | 2017-06-23 | Beigene, Ltd. | Compuestos heterocíclicos fusionados como inhibidores de proteína cinasa |
| 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 |
| CN110698481B (zh) * | 2013-07-03 | 2023-02-28 | 豪夫迈·罗氏有限公司 | 杂芳基吡啶酮和氮杂-吡啶酮酰胺化合物 |
| ES2927567T3 (es) | 2013-09-13 | 2022-11-08 | Beigene Switzerland Gmbh | Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico |
| 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 |
| TWI726608B (zh) | 2014-07-03 | 2021-05-01 | 英屬開曼群島商百濟神州有限公司 | 抗pd-l1抗體及其作為治療及診斷之用途 |
| 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 |
| WO2017123695A1 (en) * | 2016-01-13 | 2017-07-20 | Boehringer Ingelheim International Gmbh | Isoquinolones as btk inhibitors |
| WO2017173111A1 (en) | 2016-03-31 | 2017-10-05 | Takeda Pharmaceutical Company Limited | Isoquinolinyl triazolone complexes |
| EP3481393B1 (en) | 2016-07-05 | 2021-04-14 | Beigene, Ltd. | Combination of a pd-1 antagonist and a raf inhibitor for treating cancer |
| 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 |
| KR20230162137A (ko) | 2016-08-16 | 2023-11-28 | 베이진 스위찰랜드 게엠베하 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
| EP4353747A3 (en) | 2016-08-19 | 2024-06-26 | BeiGene Switzerland GmbH | Combination of zanubrutinib with an anti-cd20 or an anti-pd-1 antibody for use in treating cancer |
| WO2018053437A1 (en) | 2016-09-19 | 2018-03-22 | Mei Pharma, Inc. | Combination therapy |
| TWI774726B (zh) | 2017-01-25 | 2022-08-21 | 英屬開曼群島商百濟神州有限公司 | (S)-7-(1-(丁-2-炔醯基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氫吡唑并[1,5-a]嘧啶-3-甲醯胺的晶型、及其製備和用途 |
| CN106967073A (zh) * | 2017-04-24 | 2017-07-21 | 刘双伟 | 一种治疗类风湿性关节炎的药物 |
| CN106946891B (zh) * | 2017-05-08 | 2018-07-13 | 宿州市徽腾知识产权咨询有限公司 | 一种用于治疗类风湿性关节炎的药物 |
| EP3645569A4 (en) | 2017-06-26 | 2021-03-24 | BeiGene, Ltd. | IMMUNOTHERAPY FOR LIVER CELL CARCINOMA |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| 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 |
| MX2021004191A (es) | 2018-10-15 | 2021-05-27 | Nurix Therapeutics Inc | Compuestos bifuncionales para degradar la tirosina cinasa de bruton (btk) mediante la trayectoria de ubiquitina proteosoma. |
| CN114364798A (zh) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | 用于治疗癌症的Dbait分子与激酶抑制剂的组合 |
| IL287049B1 (en) | 2019-04-09 | 2024-09-01 | Nurix Therapeutics Inc | Trisubstituted pepidine compounds for CBL-B inhibition, and use of a CBL-B inhibitor in combination with a cancer vaccine and/or an oncolytic virus |
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| US20230024442A1 (en) * | 2019-11-08 | 2023-01-26 | Nurix Therapeutics, Inc. | Bifunctional compounds for grading btk via ubiquitin proteosome pathway |
| US20220401436A1 (en) | 2019-11-08 | 2022-12-22 | INSERM (Institute National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| IL293797A (en) | 2019-12-04 | 2022-08-01 | Nurix Therapeutics Inc | Bifunctional compounds for btk degradation via the ubiquitin proteosome pathway |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CA3214729A1 (en) | 2021-04-08 | 2022-10-13 | Marilena GALLOTTA | Combination therapies with cbl-b inhibitor compounds |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
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| JP3951395B2 (ja) * | 1996-12-13 | 2007-08-01 | 田辺製薬株式会社 | ピリジン誘導体、その製法及びその合成中間体 |
| AU771273B2 (en) * | 1999-03-12 | 2004-03-18 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compounds useful as anti-inflammatory agents |
| ES2232306B1 (es) * | 2003-11-10 | 2006-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
| RU2423351C2 (ru) * | 2004-12-16 | 2011-07-10 | Вертекс Фармасьютикалз Инкорпорейтед | Пирид-2-оны, применимые как ингибиторы протеинкиназ семейства тес для лечения воспалительных, пролиферативных и иммунологически-опосредованных заболеваний |
| AR055017A1 (es) * | 2004-12-24 | 2007-08-01 | Astrazeneca Ab | Derivados de amida, un proceso para su preparacion, composicion farmaceutica y uso del compuesto para la fabricacion de farmacos |
| AU2006223409B2 (en) * | 2005-03-10 | 2011-07-21 | Gilead Connecticut, Inc. | Certain substituted amides, method of making, and method of use thereof |
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| AU2006279992A1 (en) * | 2005-08-09 | 2007-02-22 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
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| BRPI0711628A2 (pt) | 2006-05-15 | 2011-12-06 | Irm Llc | composto, composição farmacêutica, uso e processo para preparação do composto |
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2009
- 2009-01-27 RU RU2010136665/04A patent/RU2505538C2/ru not_active IP Right Cessation
- 2009-01-27 MY MYPI2010003693A patent/MY158411A/en unknown
- 2009-01-27 MX MX2010008197A patent/MX2010008197A/es active IP Right Grant
- 2009-01-27 EP EP09709135.9A patent/EP2242749B1/en not_active Not-in-force
- 2009-01-27 PT PT97091359T patent/PT2242749E/pt unknown
- 2009-01-27 KR KR1020107016014A patent/KR101308803B1/ko not_active IP Right Cessation
- 2009-01-27 BR BRPI0907915-7A patent/BRPI0907915A2/pt not_active IP Right Cessation
- 2009-01-27 CN CN200980103857.3A patent/CN101932573B/zh not_active Expired - Fee Related
- 2009-01-27 DK DK09709135.9T patent/DK2242749T3/da active
- 2009-01-27 ES ES09709135T patent/ES2420846T3/es active Active
- 2009-01-27 AU AU2009211514A patent/AU2009211514B2/en not_active Expired - Fee Related
- 2009-01-27 SI SI200930630T patent/SI2242749T1/sl unknown
- 2009-01-27 CA CA2710462A patent/CA2710462C/en not_active Expired - Fee Related
- 2009-01-27 JP JP2010545433A patent/JP5259739B2/ja not_active Expired - Fee Related
- 2009-01-27 WO PCT/EP2009/050875 patent/WO2009098144A1/en active Application Filing
- 2009-01-27 PL PL09709135T patent/PL2242749T3/pl unknown
- 2009-01-27 NZ NZ586916A patent/NZ586916A/en not_active IP Right Cessation
- 2009-02-03 CL CL2009000229A patent/CL2009000229A1/es unknown
- 2009-02-03 TW TW098103399A patent/TWI382024B/zh not_active IP Right Cessation
- 2009-02-03 AR ARP090100345A patent/AR070408A1/es not_active Application Discontinuation
- 2009-02-04 PE PE2009000169A patent/PE20091484A1/es not_active Application Discontinuation
-
2010
- 2010-06-14 IL IL206357A patent/IL206357A/en not_active IP Right Cessation
- 2010-07-26 CO CO10090865A patent/CO6290767A2/es active IP Right Grant
- 2010-07-27 CR CR11598A patent/CR11598A/es not_active Application Discontinuation
- 2010-08-03 ZA ZA2010/05539A patent/ZA201005539B/en unknown
- 2010-08-05 EC EC2010010384A patent/ECSP10010384A/es unknown
- 2010-08-06 MA MA33066A patent/MA32064B1/fr unknown
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2011
- 2011-01-28 HK HK11100915.9A patent/HK1146826A1/xx not_active IP Right Cessation
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2013
- 2013-07-02 HR HRP20130615AT patent/HRP20130615T1/hr unknown
- 2013-07-08 CY CY20131100576T patent/CY1114114T1/el unknown
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