PE20100138A1 - Derivados de morfolino pirimidina usados en enfermedades relacionadas en mtor quinasa y/o pi3k - Google Patents
Derivados de morfolino pirimidina usados en enfermedades relacionadas en mtor quinasa y/o pi3kInfo
- Publication number
- PE20100138A1 PE20100138A1 PE2008002157A PE2008002157A PE20100138A1 PE 20100138 A1 PE20100138 A1 PE 20100138A1 PE 2008002157 A PE2008002157 A PE 2008002157A PE 2008002157 A PE2008002157 A PE 2008002157A PE 20100138 A1 PE20100138 A1 PE 20100138A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- pi3k
- morpholin
- mtor kinase
- methylsulfonylmethyl
- Prior art date
Links
- ORXTYTVXABMVJS-UHFFFAOYSA-N morpholine;pyrimidine Chemical class C1COCCN1.C1=CN=CN=C1 ORXTYTVXABMVJS-UHFFFAOYSA-N 0.000 title abstract 2
- 102100023085 Serine/threonine-protein kinase mTOR Human genes 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 abstract 6
- -1 METHYLSULFONYLMETHYL Chemical class 0.000 abstract 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract 3
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000003112 inhibitor Substances 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000038030 PI3Ks Human genes 0.000 abstract 1
- 108091007960 PI3Ks 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
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003905 phosphatidylinositols Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
-
- 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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Hematology (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE MORFOLINO PIRIMIDINA DE FORMULA (I), DONDE Y1 E Y2 SON EXCLUSIVAMENTE N O CR8; X ES -CR4=CR5-, -CR4=CR5CR6R7-, -CR6R7CR5=CR4-, ENTRE OTROS; R4 Y R5 SON CADA UNO H, ALQUILO C1-C6, ENTRE OTROS; R6 Y R7 SON CADA UNO H, HALO, CN, ENTRE OTROS; R1 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R2 ES ALQUILO C1-C6, CARBOCICLILO, HETEROCICLILO, ENTRE OTROS; R3 ES HALO, CN, NO2. ENTRE OTROS; m ES DE 1-4. SON COMPUESTOS SELECCIONADOS: 3-ETIL-1-[4-[4-[(3S)-3-METILMORFOLIN-4-IL]-6-(METILSULFONILMETIL)PIRIMIDIN-2-IL]FENIL]TIOUREA; 3-CICLOPROPIL-1-[4-[4-[(3S)-3-METILMORFOLIN-4-IL]-6-(METILSULFONILMETIL)PIRIMIDIN-2-IL]FENIL]TIOUREA; 3-(4-FLUOROFENIL)-1-[4-[4-[(3S)-3-METILMORFOLIN-4-IL]-6-(METILSULFONILMETIL)PIRIMIDIN-2-IL]FENIL]TIOUREA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A SU PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE LA mTOR QUINASA E INHIBIDORES DE LA FOSFATIDILINOSITOL 3-QUINSAS (PI3K), UTLES EN EL TRATAMIENTO DEL CANCER, ENFERMEDADES INFLAMATORIAS, ENFERMEDADES CARDIOVASCULARES, ENTRE OTROS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94853907P | 2007-07-09 | 2007-07-09 | |
| PCT/GB2008/050548 WO2009007750A1 (en) | 2007-07-09 | 2008-07-08 | Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20100138A1 true PE20100138A1 (es) | 2010-03-20 |
Family
ID=39791229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008002157A PE20100138A1 (es) | 2007-07-09 | 2008-12-19 | Derivados de morfolino pirimidina usados en enfermedades relacionadas en mtor quinasa y/o pi3k |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8138183B2 (es) |
| EP (1) | EP2176238B1 (es) |
| JP (1) | JP5508260B2 (es) |
| KR (1) | KR20100042280A (es) |
| CN (1) | CN101809002B (es) |
| AR (1) | AR070079A1 (es) |
| AT (1) | ATE554075T1 (es) |
| AU (1) | AU2008273891B2 (es) |
| BR (1) | BRPI0814688A2 (es) |
| CA (1) | CA2692720A1 (es) |
| CL (1) | CL2008003940A1 (es) |
| CO (1) | CO6251364A2 (es) |
| CR (1) | CR11200A (es) |
| DO (1) | DOP2010000012A (es) |
| EA (1) | EA018708B1 (es) |
| EC (1) | ECSP109935A (es) |
| ES (1) | ES2385692T3 (es) |
| NI (1) | NI201000002A (es) |
| PE (1) | PE20100138A1 (es) |
| WO (1) | WO2009007750A1 (es) |
| ZA (1) | ZA200909224B (es) |
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| EP2448932B1 (fr) | 2009-07-02 | 2014-03-05 | Sanofi | Nouveaux derives de 6-morpholin-4-yl-pyrimidin-4-(3h)-one, leur preparation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb) |
| CN102548970B (zh) | 2009-07-02 | 2015-11-25 | 赛诺菲 | 新型(6-氧代-1,6-二氢嘧啶-2-基)酰胺衍生物、其制备方法以及其作为akt(pkb)磷酸化抑制剂的医药用途 |
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| CN103501813A (zh) | 2011-04-29 | 2014-01-08 | 西莱克塔生物科技公司 | 用于降低抗体应答的致耐受性合成纳米载体 |
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| US11407721B2 (en) | 2013-02-19 | 2022-08-09 | Amgen Inc. | CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer |
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| EA037683B1 (ru) | 2013-04-17 | 2021-04-29 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Фармацевтические составы, способы, твердые формы и способы применения, относящиеся к 1-этил-7-(2-метил-6-(1h-1,2,4-триазол-3-ил)пиридин-3-ил)-3,4-дигидропиразино[2,3-b] пиразин-2(1h)-ону |
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| EA201790534A1 (ru) | 2014-09-07 | 2017-07-31 | Селекта Байосайенсиз, Инк. | Способы и композиции для ослабления иммунных ответов против вирусного вектора для переноса, предназначенного для генной терапии |
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| WO2007063868A1 (ja) | 2005-11-29 | 2007-06-07 | Toray Industries, Inc. | アリールメチレンウレア誘導体及びその用途 |
| GB0525081D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0525080D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0525083D0 (en) * | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| BRPI0706395A2 (pt) | 2006-01-11 | 2011-03-22 | Astrazeneca Ab | composto, uso do mesmo, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente e para tratar doença, composição farmacêutica, e, processo para preparar um composto |
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| BRPI0621509A2 (pt) | 2006-03-15 | 2011-12-13 | Csir | modulação da atividade de fosforil transferase de glutamina sintetase |
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| CA2660758A1 (en) * | 2006-08-24 | 2008-02-27 | Astrazeneca Ab | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
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| WO2008125833A1 (en) | 2007-04-12 | 2008-10-23 | Piramed Limited | Pharmaceutical compounds |
| BRPI0814503A2 (pt) | 2007-07-09 | 2017-05-16 | Astrazeneca Ab | composto, uso de um composto, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente, e para tratar uma doença, e, composição farmacêutica |
-
2008
- 2008-07-08 WO PCT/GB2008/050548 patent/WO2009007750A1/en not_active Ceased
- 2008-07-08 CA CA 2692720 patent/CA2692720A1/en not_active Abandoned
- 2008-07-08 JP JP2010515602A patent/JP5508260B2/ja not_active Expired - Fee Related
- 2008-07-08 EP EP08776183A patent/EP2176238B1/en active Active
- 2008-07-08 US US12/668,056 patent/US8138183B2/en not_active Expired - Fee Related
- 2008-07-08 KR KR1020107002942A patent/KR20100042280A/ko not_active Ceased
- 2008-07-08 AT AT08776183T patent/ATE554075T1/de active
- 2008-07-08 AU AU2008273891A patent/AU2008273891B2/en not_active Ceased
- 2008-07-08 EA EA201000091A patent/EA018708B1/ru not_active IP Right Cessation
- 2008-07-08 BR BRPI0814688A patent/BRPI0814688A2/pt not_active IP Right Cessation
- 2008-07-08 ES ES08776183T patent/ES2385692T3/es active Active
- 2008-07-08 CN CN2008801062258A patent/CN101809002B/zh not_active Expired - Fee Related
- 2008-12-19 PE PE2008002157A patent/PE20100138A1/es not_active Application Discontinuation
- 2008-12-30 AR ARP080105784A patent/AR070079A1/es unknown
- 2008-12-30 CL CL2008003940A patent/CL2008003940A1/es unknown
-
2009
- 2009-12-23 ZA ZA2009/09224A patent/ZA200909224B/en unknown
-
2010
- 2010-01-08 NI NI201000002A patent/NI201000002A/es unknown
- 2010-01-08 DO DO2010000012A patent/DOP2010000012A/es unknown
- 2010-01-08 CR CR11200A patent/CR11200A/es not_active Application Discontinuation
- 2010-02-03 EC EC2010009935A patent/ECSP109935A/es unknown
- 2010-02-09 CO CO10014081A patent/CO6251364A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CN101809002B (zh) | 2013-03-27 |
| NI201000002A (es) | 2010-10-12 |
| ATE554075T1 (de) | 2012-05-15 |
| EA018708B1 (ru) | 2013-10-30 |
| AU2008273891A1 (en) | 2009-01-15 |
| ECSP109935A (es) | 2010-03-31 |
| CL2008003940A1 (es) | 2010-09-24 |
| AU2008273891B2 (en) | 2012-01-12 |
| JP5508260B2 (ja) | 2014-05-28 |
| AR070079A1 (es) | 2010-03-10 |
| BRPI0814688A2 (pt) | 2017-06-06 |
| CN101809002A (zh) | 2010-08-18 |
| KR20100042280A (ko) | 2010-04-23 |
| CA2692720A1 (en) | 2009-01-15 |
| JP2010533160A (ja) | 2010-10-21 |
| EP2176238B1 (en) | 2012-04-18 |
| EP2176238A1 (en) | 2010-04-21 |
| ZA200909224B (en) | 2011-05-25 |
| HK1142906A1 (en) | 2010-12-17 |
| US8138183B2 (en) | 2012-03-20 |
| CR11200A (es) | 2010-06-17 |
| DOP2010000012A (es) | 2010-01-31 |
| EA201000091A1 (ru) | 2010-06-30 |
| WO2009007750A1 (en) | 2009-01-15 |
| US20100249131A1 (en) | 2010-09-30 |
| CO6251364A2 (es) | 2011-02-21 |
| ES2385692T3 (es) | 2012-07-30 |
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