AR092536A1 - Inhibidores de la tirosina-quinasa de bruton - Google Patents
Inhibidores de la tirosina-quinasa de brutonInfo
- Publication number
- AR092536A1 AR092536A1 ARP130103257A ARP130103257A AR092536A1 AR 092536 A1 AR092536 A1 AR 092536A1 AR P130103257 A ARP130103257 A AR P130103257A AR P130103257 A ARP130103257 A AR P130103257A AR 092536 A1 AR092536 A1 AR 092536A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- cycloalkyl
- optionally substituted
- halogen
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
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- 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
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Los compuestos son útiles además para tratar enfermedades inflamatorias y autoinmunes asociadas con la proliferación aberrante de las células B, por ejemplo la artritis reumatoide. Se describen también composiciones que contienen los compuestos de la fórmula (1) y por lo menos un vehículo, diluyente o excipiente. Reivindicación 1: Un compuesto de la fórmula (1), en la que: ⁻ ⁻ ⁻ ⁻ ⁻ es un enlace sencillo o un doble enlace; X es CH, CH₂ o N; R es H, -R¹, -R¹-R²-R³, -R¹-R³ o -R²-R³; R¹ es arilo, heteroarilo, heteroarilo bicíclico, cicloalquilo o heterocicloalquilo, cada uno de ellos 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(R²)₂, -O, -S, -C(=NH)NR² o -S(=O)₂; cada R² es con independencia H o alquilo inferior; R³ es H o R⁴; R⁴ es alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, (alquilo inferior)-amino, cicloalquil-amino, di(alquilo inferior)-amino, arilo, arilalquilo, alquilarilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, cicloalquilo, alquil-cicloalquilo, cicloalquil-alquilo, heterocicloalquilo, alquil-heterocicloalquilo, heterocicloalquilalquilo, cicloalquilo bicíclico, heterocicloalquilo bicíclico, espirocicloalquilo, espiroheterocicloalquilo o espiroheterocicloalquilo bicíclico, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, halógeno, (alquilo inferior)-amino, di(alquilo inferior)-amino, hidroxi, hidroxialquilo inferior, alcoxi inferior, alcanoílo inferior, halógeno, nitro, amino, amido, acilo, ciano, oxo, sulfonilo, alquilo inferior sulfonilo, guanidino, hidroxil-amino, carboxi, carbamoilo, carbamato, haloalcoxi inferior, heterocicloalquilo o haloalquilo inferior, en el que dos grupos alquilo inferior juntos pueden formar un anillo; Y⁴ es Y⁴ᵃ, Y⁴ᵇ, Y⁴ᶜ o Y⁴ᵈ; 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 por 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 hidroxialquilo inferior; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261700373P | 2012-09-13 | 2012-09-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR092536A1 true AR092536A1 (es) | 2015-04-22 |
Family
ID=49118551
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130103257A AR092536A1 (es) | 2012-09-13 | 2013-09-12 | Inhibidores de la tirosina-quinasa de bruton |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9499548B2 (es) |
| EP (1) | EP2895473A1 (es) |
| JP (1) | JP2015531781A (es) |
| KR (1) | KR20150054994A (es) |
| CN (1) | CN104619696A (es) |
| AR (1) | AR092536A1 (es) |
| BR (1) | BR112015005361A2 (es) |
| CA (1) | CA2881761A1 (es) |
| HK (1) | HK1210461A1 (es) |
| MX (1) | MX2015002901A (es) |
| RU (1) | RU2015111133A (es) |
| TW (1) | TW201416361A (es) |
| WO (1) | WO2014040965A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6348492B2 (ja) | 2012-08-10 | 2018-06-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤としてのヘテロ芳香族化合物 |
| CA2890671A1 (en) * | 2012-11-16 | 2014-05-22 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| 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 |
| 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 |
| 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 |
| US11479556B1 (en) | 2018-10-15 | 2022-10-25 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway |
| WO2020210508A1 (en) | 2019-04-09 | 2020-10-15 | 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 |
| CN114206855B (zh) | 2019-05-17 | 2024-11-26 | 紐力克斯治疗公司 | 用于Cbl-b抑制的氰基环丁基类化合物及其用途 |
| WO2021091575A1 (en) * | 2019-11-08 | 2021-05-14 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| EP4069237A1 (en) | 2019-12-04 | 2022-10-12 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| WO2022206924A1 (zh) * | 2021-04-02 | 2022-10-06 | 南京明德新药研发有限公司 | 含氮三并环双功能化合物及其制备方法和应用 |
| JP2024514836A (ja) | 2021-04-08 | 2024-04-03 | ニューリックス セラピューティクス，インコーポレイテッド | Ｃｂｌ－ｂ阻害化合物との組み合わせ療法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7683064B2 (en) * | 2008-02-05 | 2010-03-23 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| JP5259739B2 (ja) * | 2008-02-05 | 2013-08-07 | エフ．ホフマン−ラ ロシュ アーゲー | 新規ピリジノン及びピリダジノン |
| KR101299867B1 (ko) * | 2008-06-24 | 2013-08-23 | 에프. 호프만-라 로슈 아게 | 신규한 치환 피리딘-2-온 및 피리다진-3-온 |
| RU2507202C2 (ru) * | 2008-07-02 | 2014-02-20 | Ф.Хоффманн-Ля Рош Аг | Новые фенилпиразиноны в качестве ингибиторов киназы |
| US8299077B2 (en) * | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
-
2013
- 2013-09-10 EP EP13759240.8A patent/EP2895473A1/en not_active Withdrawn
- 2013-09-10 CA CA2881761A patent/CA2881761A1/en not_active Abandoned
- 2013-09-10 US US14/427,501 patent/US9499548B2/en not_active Expired - Fee Related
- 2013-09-10 RU RU2015111133A patent/RU2015111133A/ru not_active Application Discontinuation
- 2013-09-10 CN CN201380047474.5A patent/CN104619696A/zh active Pending
- 2013-09-10 WO PCT/EP2013/068659 patent/WO2014040965A1/en active Application Filing
- 2013-09-10 BR BR112015005361A patent/BR112015005361A2/pt not_active IP Right Cessation
- 2013-09-10 MX MX2015002901A patent/MX2015002901A/es unknown
- 2013-09-10 KR KR1020157009295A patent/KR20150054994A/ko not_active Application Discontinuation
- 2013-09-10 JP JP2015531530A patent/JP2015531781A/ja active Pending
- 2013-09-11 TW TW102132819A patent/TW201416361A/zh unknown
- 2013-09-12 AR ARP130103257A patent/AR092536A1/es unknown
-
2015
- 2015-11-11 HK HK15111138.3A patent/HK1210461A1/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2895473A1 (en) | 2015-07-22 |
| RU2015111133A (ru) | 2016-11-10 |
| TW201416361A (zh) | 2014-05-01 |
| CN104619696A (zh) | 2015-05-13 |
| CA2881761A1 (en) | 2014-03-20 |
| US20150210704A1 (en) | 2015-07-30 |
| WO2014040965A1 (en) | 2014-03-20 |
| US9499548B2 (en) | 2016-11-22 |
| JP2015531781A (ja) | 2015-11-05 |
| HK1210461A1 (en) | 2016-04-22 |
| BR112015005361A2 (pt) | 2017-07-04 |
| KR20150054994A (ko) | 2015-05-20 |
| MX2015002901A (es) | 2015-06-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |