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
Classifications
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- 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)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Cardiology (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 (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5746172B2 (ja) | 2009-08-20 | 2015-07-08 | カルス セラピューティクス リミテッド | ホスホイノシチド３−キナーゼ阻害剤としての三環式複素環化合物 |
| CA2786294A1 (en) * | 2010-02-22 | 2011-08-25 | F. Hoffmann-La Roche Ag | Pyrido[3,2-d]pyrimidine pi3k delta inhibitor compounds and methods of use |
| 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 |
| JP6329958B2 (ja) | 2012-11-07 | 2018-05-23 | カルス セラピューティクス リミテッド | 新規ヒストンデアセチラーゼインヒビターおよび治療におけるその使用 |
| CN105339001A (zh) | 2013-03-15 | 2016-02-17 | 基因泰克公司 | 治疗癌症和预防癌症耐药性的方法 |
| WO2014169167A1 (en) | 2013-04-12 | 2014-10-16 | Asana Biosciences, Llc | Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways |
| RS57816B1 (sr) | 2013-05-10 | 2018-12-31 | Karus Therapeutics Ltd | Inhibitori histon deacetilaze |
| GB201402431D0 (en) | 2014-02-12 | 2014-03-26 | Karus Therapeutics Ltd | Compounds |
| TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | ２-(嗎啉-４-基)-１,７-萘啶 |
| GB201419228D0 (en) | 2014-10-29 | 2014-12-10 | Karus Therapeutics Ltd | Compounds |
| GB201419264D0 (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 |
| GB201514754D0 (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 |
| GB201514751D0 (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 |
| SG11201911929XA (en) * | 2017-06-21 | 2020-01-30 | 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 |
| AU2021360636A1 (en) * | 2020-10-16 | 2023-06-15 | Shanghai De Novo Pharmatech Co., Ltd. | Triheterocyclic derivative, and pharmaceutical composition and application thereof |
| CN115916775A (zh) * | 2021-06-22 | 2023-04-04 | 成都苑东生物制药股份有限公司 | 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 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| DE2208534A1 (de) * | 1972-02-23 | 1973-08-30 | Thomae Gmbh Dr K | Neue pyrido eckige klammer auf 3,2-d eckige klammer zu pyrimidin |
| 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 CA CA2742550A patent/CA2742550A1/en not_active Abandoned
- 2009-09-30 EP EP09783585A patent/EP2344490A2/en not_active Withdrawn
- 2009-09-30 AU AU2009299894A patent/AU2009299894A1/en not_active Abandoned
- 2009-09-30 WO PCT/EP2009/062664 patent/WO2010037765A2/en active Application Filing
- 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 |
|---|---|
| US20110257170A1 (en) | 2011-10-20 |
| EP2344490A2 (en) | 2011-07-20 |
| CA2742550A1 (en) | 2010-04-08 |
| WO2010037765A3 (en) | 2010-07-15 |
| WO2010037765A2 (en) | 2010-04-08 |
| AU2009299894A1 (en) | 2010-04-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |