AR073757A1 - 4- morfolin-pirido(3,2-d) pirimidinas - Google Patents
4- morfolin-pirido(3,2-d) pirimidinasInfo
- Publication number
- AR073757A1 AR073757A1 ARP090103817A ARP090103817A AR073757A1 AR 073757 A1 AR073757 A1 AR 073757A1 AR P090103817 A ARP090103817 A AR P090103817A AR P090103817 A ARP090103817 A AR P090103817A AR 073757 A1 AR073757 A1 AR 073757A1
- Authority
- AR
- Argentina
- Prior art keywords
- denotes
- het
- so2a
- hal
- ort
- Prior art date
Links
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 125000005010 perfluoroalkyl group Chemical group 0.000 abstract 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- XXJGBENTLXFVFI-UHFFFAOYSA-N 1-amino-methylene Chemical compound N[CH2] XXJGBENTLXFVFI-UHFFFAOYSA-N 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 239000012828 PI3K inhibitor Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Composicion farmacéutica y proceso de produccion, inhibidores de la Pi3K para tratar enfermedades autoinmunes, trastornos inflamatorios, esclerosis multiple y otras enfermedades como cánceres. Reivindicacion 1: Un compuesto de formula (1) en donde R1 denota H, perfluoroalquilo, -NH2 -NA2, A, -NH-A, -NH-(CH2)p-A, -SO-A, SO2-A, -COORT, -(CH2)p-ORT, -(CH2)p-SRT, -COA, -CO-Het, -CO-N(H)2-m(A)m; -SO-N(H)2-m(A)m, SO2-N(H)2-m(A)m, -(CH2)p-N(H)2-m(A)m, -CO-NH-(CH2)p-N(H)2-m(A)m, -(CH2)p-NH-(CH2)p-N(H)2-m(A)m, Ar, Het; R2 denota H, Hal, CF3, A, Ar, Het, SA, OA, OH, -SOA, -SO2A, -OCO-A, -N(H)2-m(A)m, -NH-(CH2)p-N(H)2-m(A)m, -NA-(CH2)p-ORT, -NH-(CH2)p-OA, -(CH2)p-Het, -(CH2)p-N(H)2-m(A)m; R3 denota Hal, Ar, OA, SA, -SOA, -SO2A, -NH-SO2A, CF3, -CN, A, -NH-SO2Ar, o si al menos uno de R1 o R2 es diferente de H, R3 también denota Het; RT denota H, A, Ar, Het; Ar denota un anillo carbocíclico monocíclico o bicíclico, aromático que posee 6 a 14 átomos de carbono, que está no sustituido o monosustituido, disustituido o trisustituido por Hal, CF3, OCF3, NO2, CN, perfluoroalquilo, A, OA, NH2, COH, CONH2, -NHCOA, -NHSO2A, NHSO2-N(H)2-m(A)m, N(H)1-qAqCOA, N(H)1-qAqSO2-N(H)2-m(A)m, -N(H)1-qAqCON(H)2-m(A)m, -COOA, -SO2A, -SO2N(H)2-m(A)m, -SO2Het, -(CH2)p-N(H)2-m(A)m, -(CH2)p-ORT, o disustituido o trisustituido por OH y 1 o 2 de los sustituyentes descriptos anteriormente; Het denota un anillo heterocíclico aromático, monocíclico o bicíclico, saturado o insaturado, que posee 1, 2, 3 o 4 átomos de N, O y/o S, que está no sustituido o monosustituido, disustituido o trisustituido por alquilo C1-8, alcoxi C1-8, Hal, CF3, OCF3, NO2, CN, perfluoroalquilo, A, OA, OH, NH2, COH, CONH2, -NHCOA, -NHSO2A, -NHSO2-N(H)2-m(A)m N(H)1-qAqCOA, N(H)1-qAqSO2-N(H)2-m(A)m, -N(H)1-qAqCON(H)2-m(A)m, -COOA, -SO2A, -SO2N(H)2-m(A)m, -SO2Het, -(CH2)p-N(H)2-m(A)m, -(CH2)p-ORT; m denota 0, 1 o 2; p denota 0, 1, 2, 3 o 4; q denota 0 o 1; A es un alquilo C1-12 ramificado o lineal, en donde uno o más, con preferencia 1 a 7 átomos de H, se pueden reemplazar por Hal, Ar, Het, OR6, -CN, -COO-alquilo o N(R6)2 y en donde uno o más, con preferencia, 1 a 7 grupos CH2 no adyacentes, con exclusion del átomo de C que está unido al resto de la molécula, se pueden reemplazar por O, NR6 o S y/o por grupos -CH=CH- o -CsC-, o denota cicloalquilo o cicloalquilalquileno, que posee 3-7 átomos de C de anillo; R6 es H, A, -(CH2)p-N(H)2-m(A)m, -(CH2)p-OA, CH2NH2; con la condicion de que se excluye el compuesto de formula (2); y sus derivados, solvatos, tautomeros, sales y estereoisomeros farmacéuticamente aceptables, con inclusion de sus mezclas en todas las relaciones.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08165839 | 2008-10-03 | ||
| US19540808P | 2008-10-07 | 2008-10-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR073757A1 true AR073757A1 (es) | 2010-12-01 |
Family
ID=40282282
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090103817A AR073757A1 (es) | 2008-10-03 | 2009-10-02 | 4- morfolin-pirido(3,2-d) pirimidinas |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20110257170A1 (es) |
| EP (1) | EP2344490A2 (es) |
| AR (1) | AR073757A1 (es) |
| AU (1) | AU2009299894A1 (es) |
| CA (1) | CA2742550A1 (es) |
| WO (1) | WO2010037765A2 (es) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2534326T3 (es) | 2009-08-20 | 2015-04-21 | Karus Therapeutics Limited | Compuestos tricíclicos heterocíclicos como inhibidores de la fosfoinositida 3-cinasa |
| CN102762565A (zh) * | 2010-02-22 | 2012-10-31 | 弗·哈夫曼-拉罗切有限公司 | 吡啶并[3,2-d]嘧啶PI3δ抑制剂化合物及使用方法 |
| US8968887B2 (en) * | 2010-04-28 | 2015-03-03 | Universal Display Corporation | Triphenylene-benzofuran/benzothiophene/benzoselenophene compounds with substituents joining to form fused rings |
| GB201007347D0 (en) | 2010-04-30 | 2010-06-16 | Karus Therapeutics Ltd | Compounds |
| GB201204125D0 (en) | 2012-03-08 | 2012-04-25 | Karus Therapeutics Ltd | Compounds |
| CN104797573A (zh) | 2012-11-07 | 2015-07-22 | 卡鲁斯治疗有限公司 | 新的组蛋白脱乙酰基酶抑制剂及其在治疗中的用途 |
| RU2015143437A (ru) | 2013-03-15 | 2017-04-27 | Дженентек, Инк. | Способы лечения рака и предотвращения устойчивости к лекарственным препаратам для лечения рака |
| MX2015014387A (es) * | 2013-04-12 | 2017-04-10 | Asana Biosciences Llc | Quinazolinas y azaquinazolinas como inhibidores duales de vias ras/raf/mek/erk y pi3k/akt/pten/mtor. |
| DK2994465T3 (en) | 2013-05-10 | 2018-10-08 | Karus Therapeutics Ltd | HISTONDEACETYLASE INHIBITORS UNKNOWN |
| GB201402431D0 (en) | 2014-02-12 | 2014-03-26 | Karus Therapeutics Ltd | Compounds |
| TWI656121B (zh) * | 2014-08-04 | 2019-04-11 | 德商拜耳製藥公司 | ２－（嗎啉－４－基）－１，７－萘啶 |
| GB201419264D0 (en) | 2014-10-29 | 2014-12-10 | Karus Therapeutics Ltd | Compounds |
| GB201419228D0 (en) | 2014-10-29 | 2014-12-10 | Karus Therapeutics Ltd | Compounds |
| PL236355B1 (pl) * | 2015-04-02 | 2021-01-11 | Celon Pharma Spolka Akcyjna | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3 |
| GB201514751D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds |
| GB201514758D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Formulation |
| GB201514760D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds and method of use |
| GB201514754D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds |
| GB201517264D0 (en) * | 2015-09-30 | 2015-11-11 | Ucb Biopharma Sprl And Katholieke Universiteit Leuven | Therapeutic agents |
| CN109311868B (zh) | 2015-12-22 | 2022-04-01 | 尚医治疗有限责任公司 | 用于治疗癌症和炎性疾病的化合物 |
| IL271230B2 (en) | 2017-06-21 | 2024-06-01 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| CN111205310B (zh) * | 2018-11-22 | 2023-12-19 | 上海迪诺医药科技有限公司 | 杂环稠合嘧啶衍生物、其药物组合物及应用 |
| JP7407461B2 (ja) | 2018-12-19 | 2024-01-04 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物 |
| JP7774621B2 (ja) * | 2020-10-16 | 2025-11-21 | シャンハイ ドーァ ノボ ファーマテック カンパニー，リミティド | 三複素環誘導体、その医薬組成物及び使用 |
| CN115916775B (zh) * | 2021-06-22 | 2025-02-07 | 成都硕德药业有限公司 | Atr抑制剂及其用途 |
| CN116283960A (zh) * | 2021-12-21 | 2023-06-23 | 上海安诺达生物科技有限公司 | 取代的稠杂环化合物及其制备方法与应用 |
| CN117088898A (zh) * | 2022-05-13 | 2023-11-21 | 中国药科大学 | 稠环嘧啶类化合物及其制备方法、药物组合物和应用 |
| WO2025003330A1 (en) | 2023-06-30 | 2025-01-02 | Forschungsverbund Berlin E.V. | Thiazolo tetrahydrochinoline compounds as class ii phosphoinositide 3-kinase inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2208534A1 (de) * | 1972-02-23 | 1973-08-30 | Thomae Gmbh Dr K | Neue pyrido eckige klammer auf 3,2-d eckige klammer zu pyrimidin |
| DE2117657B2 (de) * | 1971-04-10 | 1976-04-08 | Dr. Karl Thomae Gmbh, 7950 Biberach | Pyrido eckige klammer auf 3,2- d eckige klammer zu pyrimidine |
| JP3649395B2 (ja) * | 2000-04-27 | 2005-05-18 | 山之内製薬株式会社 | 縮合ヘテロアリール誘導体 |
| GB2431156A (en) * | 2005-10-11 | 2007-04-18 | Piramed Ltd | 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase |
| WO2008152387A1 (en) * | 2007-06-12 | 2008-12-18 | F.Hoffmann-La Roche Ag | Quinazoline derivatives as pi3 kinase inhibitors |
-
2009
- 2009-09-30 EP EP09783585A patent/EP2344490A2/en not_active Withdrawn
- 2009-09-30 CA CA2742550A patent/CA2742550A1/en not_active Abandoned
- 2009-09-30 WO PCT/EP2009/062664 patent/WO2010037765A2/en not_active Ceased
- 2009-09-30 AU AU2009299894A patent/AU2009299894A1/en not_active Abandoned
- 2009-09-30 US US13/122,799 patent/US20110257170A1/en not_active Abandoned
- 2009-10-02 AR ARP090103817A patent/AR073757A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2010037765A3 (en) | 2010-07-15 |
| EP2344490A2 (en) | 2011-07-20 |
| WO2010037765A2 (en) | 2010-04-08 |
| AU2009299894A1 (en) | 2010-04-08 |
| US20110257170A1 (en) | 2011-10-20 |
| CA2742550A1 (en) | 2010-04-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |