ES2661864T3 - Derivados de 2,3-dihidro-benzo[1,4]oxazina y compuestos relacionados como inhibidores de fosfoinositida-3 quinasa (PI3K) para el tratamiento de por ejemplo artritis reumatoide - Google Patents
Derivados de 2,3-dihidro-benzo[1,4]oxazina y compuestos relacionados como inhibidores de fosfoinositida-3 quinasa (PI3K) para el tratamiento de por ejemplo artritis reumatoide Download PDFInfo
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- ES2661864T3 ES2661864T3 ES12823036T ES12823036T ES2661864T3 ES 2661864 T3 ES2661864 T3 ES 2661864T3 ES 12823036 T ES12823036 T ES 12823036T ES 12823036 T ES12823036 T ES 12823036T ES 2661864 T3 ES2661864 T3 ES 2661864T3
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- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 title 2
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 2
- YRLORWPBJZEGBX-UHFFFAOYSA-N 3,4-dihydro-2h-1,4-benzoxazine Chemical class C1=CC=C2NCCOC2=C1 YRLORWPBJZEGBX-UHFFFAOYSA-N 0.000 title 1
- 102000038030 PI3Ks Human genes 0.000 title 1
- 108091007960 PI3Ks Proteins 0.000 title 1
- 206010039073 rheumatoid arthritis Diseases 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 17
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 6
- 229910052799 carbon Inorganic materials 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- -1 heterocyclyl-oxyl Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004529 1,2,3-triazinyl group Chemical group N1=NN=C(C=C1)* 0.000 abstract 1
- 125000004530 1,2,4-triazinyl group Chemical group N1=NC(=NC=C1)* 0.000 abstract 1
- 125000003363 1,3,5-triazinyl group Chemical group N1=C(N=CN=C1)* 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Un compuesto de la fórmula (I): **(Ver fórmula)** o una sal del mismo, en donde: Y se selecciona a partir de O o NH; V se selecciona a partir de CR5 o N; W se selecciona a partir de CH2, u O; U se selecciona a partir de N o CH; Q se selecciona a partir de N o CR6; en donde U y Q no son ambos N; R1 se selecciona a partir de fenilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, 1,2,3-triazinilo, 1,2,4-triazinilo, 1,3,5- triazinilo, o -X-R4 en donde X se selecciona a partir de C(O), S(O)2 o CH2, y R4 se selecciona a partir de alquilo de 1 a 8 átomos de carbono, halo-alquilo de 1 a 8 átomos de carbono, hidroxialquilo de 1 a 8 átomos de carbono, alcoxilo de 1 a 8 átomos de carbono-alquilo de 1 a 8 átomos de carbono, cianoalquilo de 1 a 8 átomos de carbono, N,N-di-alquilo de 1 a 4 átomos de carbono-amino-alquilo de 1 a 8 átomos de carbono, alquilo de 1 a 4 átomos de carbono-sulfonil-alquilo de 1 a 8 átomos de carbono, fenilo, heterociclilo, heterociclil-oxilo, heterociclil-alquilo de 1 a 8 átomos de carbono, cicloalquilo de 3 a 12 átomos de carbono, cicloalquiloxilo de 3 a 12 átomos de carbono, cicloalquilo de 3 a 12 átomos de carbono-alquilo de 1 a 8 átomos de carbono, heteroarilo, heteroaril-oxilo, heteroaril-alquilo de 1 a 8 átomos de carbono, hidroxilo, alcoxilo de 1 a 8 átomos de carbono, amino, N-alquilo de 1 a 8 átomos de carbono-amino, o N,N-di-alquilo de 1 a 8 átomos de carbono-amino, en donde el alquilo de 1 a 8 átomos de carbono en N-alquilo de 1 a 8 átomos de carbono-amino y en N,N-di-alquilo de 1 a 8 átomos de carbono-amino puede estar insustituido o sustituido por halógeno, hidroxilo, o alcoxilo de 1 a 4 átomos de carbono, en donde el cicloalquilo de 3 a 12 átomos de carbono en cicloalquilo de 3 a 12 átomos de carbono y en cicloalquilo de 3 a 12 átomos de carbono-alquilo de 1 a 8 átomos de carbono puede estar insustituido o sustituido por 1 a 5 sustituyentes seleccionados a partir de halógeno, hidroxilo, o alcoxilo de 1 a 4 átomos de carbono; ...
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161579231P | 2011-12-22 | 2011-12-22 | |
| PCT/IB2012/057554 WO2013093849A1 (en) | 2011-12-22 | 2012-12-20 | Dihydro-benzo-oxazine and dihydro-pyrido-oxazine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2661864T3 true ES2661864T3 (es) | 2018-04-04 |
Family
ID=47678928
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12823036T Active ES2661864T3 (es) | 2011-12-22 | 2012-12-20 | Derivados de 2,3-dihidro-benzo[1,4]oxazina y compuestos relacionados como inhibidores de fosfoinositida-3 quinasa (PI3K) para el tratamiento de por ejemplo artritis reumatoide |
Country Status (42)
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR089284A1 (es) | 2011-12-22 | 2014-08-13 | Galapagos Nv | Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios |
| PE20141598A1 (es) | 2011-12-22 | 2014-11-14 | Novartis Ag | Derivados de dihidro-benzo-oxazina y dihidro-pirido-oxazina |
| AU2012358803C1 (en) | 2011-12-22 | 2019-12-19 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| TW201422625A (zh) | 2012-11-26 | 2014-06-16 | Novartis Ag | 二氫－吡啶并－□衍生物之固體形式 |
| HUE036665T2 (hu) * | 2012-11-26 | 2018-07-30 | Novartis Ag | Dihidro-pirido-oxazin származék szilárd formái |
| CN105541698B (zh) * | 2015-12-23 | 2018-07-10 | 滨海康杰化学有限公司 | 一种5-溴-2-三氟甲基吡啶的制备方法 |
| GB2550437B (en) * | 2016-05-20 | 2021-06-23 | Bugworks Res Inc | Heterocyclic compounds useful as anti-bacterial agents and method for production |
| ES2971712T3 (es) * | 2017-12-22 | 2024-06-06 | Hibercell Inc | Derivados de cromenopiridina como inhibidores de la fosfatidilinositol fosfato cinasa |
| PE20211089A1 (es) | 2018-08-13 | 2021-06-14 | Hoffmann La Roche | Nuevos compuestos heterociclicos como inhibidores de la monoacilglicerol lipasa |
| MX2021006696A (es) | 2018-12-06 | 2021-07-07 | Daiichi Sankyo Co Ltd | Derivado de cicloalcano-1,3-diamina. |
| TW202112784A (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𠳭唏并嘧啶衍生物 |
| MX2022002311A (es) | 2019-09-12 | 2022-03-25 | Hoffmann La Roche | Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de monoacilglicerol lipasa (magl). |
| US12421252B2 (en) * | 2019-11-20 | 2025-09-23 | Hoffmann-La Roche Inc. | Spiro (isobenzofuranazetidine) compounds for the treatment of autoimmune disease |
| KR20220155593A (ko) * | 2020-03-19 | 2022-11-23 | 아르커스 바이오사이언시즈 인코포레이티드 | Hif-2알파의 억제제로서의 테트랄린 및 테트라히드로퀴놀린 화합물 |
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