MX2012012560A - Piperazinotriazinas como inhibidores pi3k, para utilizar en el tratamiento de desordenes antiproliferativos. - Google Patents
Piperazinotriazinas como inhibidores pi3k, para utilizar en el tratamiento de desordenes antiproliferativos.Info
- Publication number
- MX2012012560A MX2012012560A MX2012012560A MX2012012560A MX2012012560A MX 2012012560 A MX2012012560 A MX 2012012560A MX 2012012560 A MX2012012560 A MX 2012012560A MX 2012012560 A MX2012012560 A MX 2012012560A MX 2012012560 A MX2012012560 A MX 2012012560A
- Authority
- MX
- Mexico
- Prior art keywords
- piperazinotriazines
- treatment
- pi3k inhibitors
- acryloylaminoethyl
- acryloyl
- Prior art date
Links
- FPUAVTTZMHSLMG-UHFFFAOYSA-N 4-piperazin-1-yltriazine Chemical class C1CNCCN1C1=CC=NN=N1 FPUAVTTZMHSLMG-UHFFFAOYSA-N 0.000 title 1
- 239000012828 PI3K inhibitor Substances 0.000 title 1
- 230000001028 anti-proliverative effect Effects 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- -1 methylaminoethyl Chemical group 0.000 abstract 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 abstract 2
- 125000003647 acryloyl group Chemical group O=C([*])C([H])=C([H])[H] 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000005977 Ethylene Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 abstract 1
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 abstract 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 125000005647 linker group Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
-
- 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
-
- 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
- A61P25/24—Antidepressants
-
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
-
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
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- 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
- C07D403/02—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 two hetero rings
- C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Psychology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
Abstract
La invención se refiere a compuestos de la fórmula (I) en donde R1 es metilo, n-hexilo, aminoetilo, metilaminoetilo, etilaminoetilo, dimetilaminoetilo, acriloilaminoetilo, metacriloilaminoetilo, metoxietilo, etoxietilo, C1-C4-alquil-sulfonilo, acriloilo o metacriloilo; o R1 es aminoetilo, acriloilo o acriloilaminoetilo que transporta un enlazador y una etiqueta y R2 y R3, independientemente entre si son, hidrógeno o C1-C4-alquilo, o R2 y R3 juntos forman un puente metileno o etileno; y tautómeros, solvatos y sales farmacéuticamente aceptables de los mismos. Estos compuestos son efectivos para evitar o tratar una enfermedad o desorden modulado por PI3 quinasas y/o mTOR, en particular tratamiento de un desorden hiperproliferativo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1007227.0A GB201007227D0 (en) | 2010-04-30 | 2010-04-30 | Piperazinotriazines |
| PCT/IB2011/051829 WO2011135520A1 (en) | 2010-04-30 | 2011-04-27 | Piperazinotriazines as pi3k inhibitors for use in the treatment antiproliferative disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012012560A true MX2012012560A (es) | 2012-12-17 |
Family
ID=42289874
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012012560A MX2012012560A (es) | 2010-04-30 | 2011-04-27 | Piperazinotriazinas como inhibidores pi3k, para utilizar en el tratamiento de desordenes antiproliferativos. |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20130040912A1 (es) |
| EP (1) | EP2563368A1 (es) |
| JP (1) | JP2013525419A (es) |
| KR (1) | KR20130118731A (es) |
| CN (1) | CN103002899A (es) |
| AU (1) | AU2011246952A1 (es) |
| BR (1) | BR112012027813A2 (es) |
| CA (1) | CA2797808A1 (es) |
| GB (1) | GB201007227D0 (es) |
| IL (1) | IL222692A0 (es) |
| MX (1) | MX2012012560A (es) |
| NZ (1) | NZ603859A (es) |
| RU (1) | RU2012151201A (es) |
| SG (1) | SG185067A1 (es) |
| WO (1) | WO2011135520A1 (es) |
| ZA (1) | ZA201206898B (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2901613C (en) | 2013-03-13 | 2020-10-20 | The Regents Of The University Of Michigan | Dual mek/pi3k inhibitors and therapeutic methods using the same |
| US9951040B2 (en) | 2014-11-20 | 2018-04-24 | Council Of Scientific And Industrial Research | 1,3,5 -triazine based PI3K inhibitors as anticancer agents and a process for the preparation thereof |
| CN105130960B (zh) * | 2015-07-31 | 2018-07-06 | 沈阳药科大学 | 1,3,5-三嗪类衍生物及其应用 |
| EP3481822B1 (en) | 2016-07-06 | 2022-06-22 | The Regents of The University of Michigan | Multifunctional inhibitors of mek/pi3k and mtor/mek/pi3k biological pathways and therapeutic methods using the same |
| CN109810100B (zh) * | 2017-11-21 | 2022-03-11 | 中国药科大学 | 含有苯并呋喃的parp-1和pi3k双靶点抑制剂 |
| CN113200969B (zh) * | 2021-05-19 | 2022-11-25 | 中国药科大学 | 一种PI3Kα选择性抑制剂及其制备方法和应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100563514B1 (ko) * | 1997-07-24 | 2006-03-27 | 젠야쿠코교가부시키가이샤 | 헤테로고리 화합물 및 이를 유효성분으로 하는 항종양제 |
| CA2445395C (en) | 2001-04-27 | 2010-03-30 | Zenyaku Kogyo Kabushiki Kaisha | Heterocyclic compound and antitumor agent comprising the same as effective component |
| WO2004003782A1 (de) | 2002-07-01 | 2004-01-08 | Ognjen Amidzic | Verfahren zur erstellung von daten, die für die beurteilung kognitiver oder sensomotorischer leistungsfähigkeiten oder leistungen von testpersonen verwendbar sind |
| EP2316831B1 (en) * | 2002-11-21 | 2013-03-06 | Novartis AG | 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer |
| EP1864665B1 (en) * | 2005-03-11 | 2012-05-16 | Zenyaku Kogyo Kabushikikaisha | Immunosuppressive agent comprising a heterocyclic compound as active ingredient |
| WO2008032033A1 (en) * | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| US20110053907A1 (en) * | 2008-03-27 | 2011-03-03 | Auckland Uniservices Limited | Substituted pyrimidines and triazines and their use in cancer therapy |
| CN102089308A (zh) * | 2008-07-07 | 2011-06-08 | 艾科睿控股公司 | Pi3k亚型选择性抑制剂 |
| US8461158B2 (en) * | 2009-03-27 | 2013-06-11 | Pathway Therapeutics Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy |
-
2010
- 2010-04-30 GB GBGB1007227.0A patent/GB201007227D0/en not_active Ceased
-
2011
- 2011-04-27 BR BR112012027813A patent/BR112012027813A2/pt not_active IP Right Cessation
- 2011-04-27 KR KR1020127031105A patent/KR20130118731A/ko not_active Withdrawn
- 2011-04-27 SG SG2012079679A patent/SG185067A1/en unknown
- 2011-04-27 AU AU2011246952A patent/AU2011246952A1/en not_active Abandoned
- 2011-04-27 MX MX2012012560A patent/MX2012012560A/es not_active Application Discontinuation
- 2011-04-27 RU RU2012151201/04A patent/RU2012151201A/ru not_active Application Discontinuation
- 2011-04-27 CA CA2797808A patent/CA2797808A1/en not_active Abandoned
- 2011-04-27 CN CN2011800215135A patent/CN103002899A/zh active Pending
- 2011-04-27 NZ NZ603859A patent/NZ603859A/en not_active IP Right Cessation
- 2011-04-27 JP JP2013506793A patent/JP2013525419A/ja active Pending
- 2011-04-27 WO PCT/IB2011/051829 patent/WO2011135520A1/en not_active Ceased
- 2011-04-27 EP EP11723129A patent/EP2563368A1/en not_active Withdrawn
- 2011-04-27 US US13/643,357 patent/US20130040912A1/en not_active Abandoned
-
2012
- 2012-09-14 ZA ZA2012/06898A patent/ZA201206898B/en unknown
- 2012-10-25 IL IL222692A patent/IL222692A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011135520A1 (en) | 2011-11-03 |
| GB201007227D0 (en) | 2010-06-16 |
| AU2011246952A1 (en) | 2012-12-20 |
| US20130040912A1 (en) | 2013-02-14 |
| EP2563368A1 (en) | 2013-03-06 |
| WO2011135520A8 (en) | 2012-09-27 |
| ZA201206898B (en) | 2013-07-31 |
| SG185067A1 (en) | 2012-12-28 |
| BR112012027813A2 (pt) | 2018-05-15 |
| CN103002899A (zh) | 2013-03-27 |
| JP2013525419A (ja) | 2013-06-20 |
| CA2797808A1 (en) | 2011-11-03 |
| IL222692A0 (en) | 2012-12-31 |
| NZ603859A (en) | 2014-07-25 |
| RU2012151201A (ru) | 2014-06-10 |
| KR20130118731A (ko) | 2013-10-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |