AR070408A1 - Piridinonas y piridazinonas - Google Patents
Piridinonas y piridazinonasInfo
- Publication number
- AR070408A1 AR070408A1 ARP090100345A ARP090100345A AR070408A1 AR 070408 A1 AR070408 A1 AR 070408A1 AR P090100345 A ARP090100345 A AR P090100345A AR P090100345 A ARP090100345 A AR P090100345A AR 070408 A1 AR070408 A1 AR 070408A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- lower alkyl
- hydroxy
- halogen
- amino
- Prior art date
Links
Classifications
-
- 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
Abstract
Los compuestos aquí descritos son utiles para modular la actividad de la Btk y tratar enfermedades asociadas con una actividad excesiva de la Btk. Además, estos compuestos son utiles para tratar enfermedades inflamatorias y autoinmunes asociadas con la proliferacion aberrante de células B, por ejemplo la artritis reumatoide. Se describen también composiciones que contienen los compuestos de las formulas (1) - (3) y por lo menos un vehículo, diluyente o excipiente. Reivindicacion 1: Un compuesto de las formulas (1), (2) o (3) 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, hidroxi-alquilo inferior, alcoxi inferior, halogeno, nitro, amino, amido, ciano, oxo o halo-alquilo 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, halogeno, 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 halogeno, 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 halogeno; n es el numero 0, 1, 2 o 3; Y3 es H, halogeno 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 halogeno; m es el numero 0 o 1; Y4 es Y4a, Y4b, Y4c o Y4d; en el que Y4a es H o halogeno; Y4b es alquilo inferior, opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por haloalquilo inferior, halogeno, 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, halogeno, 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 |
|---|---|
| AR070408A1 true AR070408A1 (es) | 2010-04-07 |
Family
ID=40413736
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100345A AR070408A1 (es) | 2008-02-05 | 2009-02-03 | Piridinonas y piridazinonas |
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) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2728016C (en) | 2008-06-24 | 2017-02-28 | F. Hoffmann-La Roche Ag | Novel substituted pyridin-2-ones and pyridazin-3-ones |
| US8299077B2 (en) | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| ES2513915T3 (es) * | 2009-04-24 | 2014-10-27 | F. Hoffmann-La Roche Ag | Inhibidores de la tirosina quinasa de Bruton |
| NZ598985A (en) | 2009-09-04 | 2013-07-26 | Biogen Idec Inc | Bruton's tyrosine kinase inhibitors |
| CA2798634C (en) * | 2010-05-07 | 2019-04-16 | Gilead Connecticut, Inc. | Pyridone and aza-pyridone compounds and methods of use |
| 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 |
| CA2834077A1 (en) | 2011-05-17 | 2012-11-22 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| BR112014003582A2 (pt) * | 2011-08-17 | 2017-03-14 | Hoffmann La Roche | inibidores da tirosina quinase de bruton |
| UA111756C2 (uk) * | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| US9365566B2 (en) | 2012-03-27 | 2016-06-14 | Takeda Pharmaceutical Company Limited | Cinnoline derivatives |
| SG11201406311UA (en) | 2012-04-05 | 2014-11-27 | Chdi Foundation Inc | Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| JP6182593B2 (ja) | 2012-04-20 | 2017-08-16 | アドヴィーナス セラピューティクス リミテッド | 置換ヘテロ二環化合物、組成物及び医薬並びにそれらの用途 |
| AR091273A1 (es) * | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | Inhibidores de pirimidinil tirosina quinasa |
| JP2015531781A (ja) * | 2012-09-13 | 2015-11-05 | 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 |
| WO2014076104A1 (en) * | 2012-11-16 | 2014-05-22 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| 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 |
| RU2618529C2 (ru) * | 2013-03-05 | 2017-05-04 | Ф. Хоффманн-Ля Рош Аг | Ингибиторы тирозинкиназы брутона |
| CN105143215B (zh) * | 2013-03-05 | 2017-12-08 | 豪夫迈·罗氏有限公司 | 布鲁顿氏酪氨酸激酶抑制剂 |
| 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 |
| KR101815360B1 (ko) * | 2013-07-03 | 2018-01-04 | 에프. 호프만-라 로슈 아게 | 헤테로아릴 피리돈 및 아자-피리돈 아마이드 화합물 |
| JP6623353B2 (ja) | 2013-09-13 | 2019-12-25 | ベイジーン スウィッツァーランド ゲーエムベーハー | 抗ｐｄ−１抗体並びにその治療及び診断のための使用 |
| CA2929918C (en) * | 2013-12-05 | 2018-01-23 | F. Hoffmann-La Roche Ag | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
| JP6526189B2 (ja) | 2014-07-03 | 2019-06-05 | ベイジーン リミテッド | 抗ｐｄ−ｌ１抗体並びにその治療及び診断のための使用 |
| 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 |
| US10570118B2 (en) * | 2016-01-13 | 2020-02-25 | Boehringer Ingelheim International Gmbh | Isoquinolones as BTK inhibitors |
| AU2017240609B2 (en) | 2016-03-31 | 2021-07-15 | Takeda Pharmaceutical Company Limited | Isoquinolinyl triazolone complexes |
| 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 |
| CA3031443A1 (en) | 2016-07-21 | 2018-01-25 | Biogen Ma Inc. | Succinate of pyrimidinyl derivatives and solid forms thereof as bruton's tyrosine kinase inhibitors |
| CN109563099B (zh) | 2016-08-16 | 2023-02-03 | 百济神州有限公司 | 一种化合物的晶型、其制备和用途 |
| AU2017313085A1 (en) | 2016-08-19 | 2019-03-14 | Beigene Switzerland Gmbh | Use of a combination comprising a Btk inhibitor for treating cancers |
| JP2019529419A (ja) | 2016-09-19 | 2019-10-17 | エムイーアイ ファーマ，インク． | 併用療法 |
| CN110461847B (zh) | 2017-01-25 | 2022-06-07 | 百济神州有限公司 | (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途 |
| 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 |
| CN108164536A (zh) * | 2017-05-08 | 2018-06-15 | 刘双伟 | 一种用于治疗类风湿性关节炎的新的化合物的合成方法 |
| CA3066518A1 (en) | 2017-06-26 | 2019-01-03 | Beigene, Ltd. | Immunotherapy for hepatocellular carcinoma |
| CN110997677A (zh) | 2017-08-12 | 2020-04-10 | 百济神州有限公司 | 具有改进的双重选择性的Btk抑制剂 |
| WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors |
| EP3867242A1 (en) | 2018-10-15 | 2021-08-25 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| AU2020272937A1 (en) | 2019-04-09 | 2021-10-21 | Nurix Therapeutics, Inc. | 3-substituted piperidine compounds for Cbl-b inhibition, and use of a Cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus |
| US11530229B2 (en) | 2019-05-17 | 2022-12-20 | Nurix Therapeutics, Inc. | Cyano cyclobutyl compounds for CBL-B inhibition and uses thereof |
| 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 |
| WO2021091575A1 (en) * | 2019-11-08 | 2021-05-14 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| MX2022006672A (es) | 2019-12-04 | 2022-08-08 | Nurix Therapeutics Inc | Compuestos bifuncionales para la degradacion de btk a traves de la via de proteosomas de ubiquitina. |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EE04799B1 (et) * | 1999-03-12 | 2007-04-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Ühendid, mis on kasulikud põletikuvastaste vahenditena, nende ühendite valmistamise meetodid ja neid sisaldavad farmatseutilised kompositsioonid |
| 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 |
| EP1831174B1 (en) * | 2004-12-24 | 2011-03-02 | AstraZeneca AB | Amide derivatives |
| BRPI0608252A2 (pt) * | 2005-03-10 | 2010-04-06 | Cgi Pharmaceuticals Inc | entidades quìmicas, composições farmacêuticas compreendendo as mesmas, métodos utilizando as referidas entidades quìmicas e uso das referidas entidades quìmicas |
| WO2006124731A2 (en) * | 2005-05-12 | 2006-11-23 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| CA2617359A1 (en) * | 2005-08-09 | 2007-02-22 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| JP2009507792A (ja) * | 2005-08-29 | 2009-02-26 | バーテックス ファーマシューティカルズ インコーポレイテッド | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| MX2008014618A (es) * | 2006-05-15 | 2008-11-28 | Irm Llc | Composiciones y metodos para inhibidores de cinasas del receptor fgf. |
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2009
- 2009-01-27 CN CN200980103857.3A patent/CN101932573B/zh not_active Expired - Fee Related
- 2009-01-27 BR BRPI0907915-7A patent/BRPI0907915A2/pt not_active IP Right Cessation
- 2009-01-27 NZ NZ586916A patent/NZ586916A/en not_active IP Right Cessation
- 2009-01-27 PL PL09709135T patent/PL2242749T3/pl unknown
- 2009-01-27 KR KR1020107016014A patent/KR101308803B1/ko not_active IP Right Cessation
- 2009-01-27 EP EP09709135.9A patent/EP2242749B1/en not_active Not-in-force
- 2009-01-27 CA CA2710462A patent/CA2710462C/en not_active Expired - Fee Related
- 2009-01-27 DK DK09709135.9T patent/DK2242749T3/da active
- 2009-01-27 SI SI200930630T patent/SI2242749T1/sl unknown
- 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 JP JP2010545433A patent/JP5259739B2/ja not_active Expired - Fee Related
- 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 PT PT97091359T patent/PT2242749E/pt unknown
- 2009-01-27 WO PCT/EP2009/050875 patent/WO2009098144A1/en active Application Filing
- 2009-01-27 MX MX2010008197A patent/MX2010008197A/es active IP Right Grant
- 2009-02-03 CL CL2009000229A patent/CL2009000229A1/es unknown
- 2009-02-03 AR ARP090100345A patent/AR070408A1/es not_active Application Discontinuation
- 2009-02-03 TW TW098103399A patent/TWI382024B/zh not_active IP Right Cessation
- 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
-
2011
- 2011-01-28 HK HK11100915.9A patent/HK1146826A1/xx not_active IP Right Cessation
-
2013
- 2013-07-02 HR HRP20130615AT patent/HRP20130615T1/hr unknown
- 2013-07-08 CY CY20131100576T patent/CY1114114T1/el unknown
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