AR074072A1 - Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme - Google Patents
Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiformeInfo
- Publication number
- AR074072A1 AR074072A1 ARP090104158A ARP090104158A AR074072A1 AR 074072 A1 AR074072 A1 AR 074072A1 AR P090104158 A ARP090104158 A AR P090104158A AR P090104158 A ARP090104158 A AR P090104158A AR 074072 A1 AR074072 A1 AR 074072A1
- Authority
- AR
- Argentina
- Prior art keywords
- imidazol
- piperidin
- prepare
- attached
- pharmaceutical composition
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
-
- 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
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
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- 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
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Reproductive Health (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuesto de imidazol-piperidin-(pirrol-pirimidin)-ona, inhibidor de cinasa p70 S6 y AKT, de la formula. Composicion farmacéutica que comprende. Uso para preparar un medicamento util para el tratar el glioblastoma multiforme. Reivindicacion 1: Un compuesto de imidazol-piperidin-pirrol pirimidin-6-ona caracterizado porque es de la formula: 1 donde: X es F, Cl, CF3, CN o H; Y es F, H o Cl; R1 y R2 son independientemente H, alquilo C1-4 o CH2CH2OH; o R1 y R2 junto con el átomo de nitrogeno al cual están unidos, forman un anillo pirrolidina opcionalmente sustituido con hidroximetilo en la posicion-2 o hidroxi en la posicion-3, o un anillo azetidina sustituido con hidroxi en la posicion-3; R3 es H o OH; R6 es H; o R6 y R2 junto con el átomo de nitrogeno al cual R2 está unido, forman un anillo piperidina; R7 y R8 son independientemente H o CH3 o R7 y R1 junto con el átomo de nitrogeno al cual R1 está unido, forman un anillo pirrolidina; W es CR4R5, NR10, C=O o C=CH-R9; R4 y R5 son independientemente H, CH3, o CH2CH3; R4 y R5 junto con el átomo de carbono al cual están unidos, forman un anillo ciclopentano; o uno de R4 o R5 es bencilo y el otro es H; R9 es 2-tiazolilo, 4-piridilo, 2-metil-4-tiazolilo, 2-imidazolilo, 5-tiazolilo, o 4-imidazolilo; y R10 es H o alquilo C1-3 o una sal del mismo farmacéuticamente aceptable.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11327308P | 2008-11-11 | 2008-11-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074072A1 true AR074072A1 (es) | 2010-12-22 |
Family
ID=41402451
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104158A AR074072A1 (es) | 2008-11-11 | 2009-10-28 | Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US8148387B2 (es) |
| EP (1) | EP2358710B1 (es) |
| JP (1) | JP5432275B2 (es) |
| KR (1) | KR101334460B1 (es) |
| CN (1) | CN102216302B (es) |
| AR (1) | AR074072A1 (es) |
| AU (1) | AU2009314324B2 (es) |
| BR (1) | BRPI0921916A2 (es) |
| CA (1) | CA2743019C (es) |
| CO (1) | CO6382114A2 (es) |
| CR (1) | CR20110240A (es) |
| CY (1) | CY1113409T1 (es) |
| DK (1) | DK2358710T3 (es) |
| DO (1) | DOP2011000129A (es) |
| EA (1) | EA018947B1 (es) |
| EC (1) | ECSP11011048A (es) |
| ES (1) | ES2391704T3 (es) |
| HK (1) | HK1158203A1 (es) |
| HN (1) | HN2011001247A (es) |
| HR (1) | HRP20120738T1 (es) |
| IL (1) | IL211940A (es) |
| JO (1) | JO2822B1 (es) |
| MA (1) | MA32776B1 (es) |
| MX (1) | MX2011005000A (es) |
| MY (1) | MY161461A (es) |
| NZ (1) | NZ592062A (es) |
| PA (1) | PA8846901A1 (es) |
| PE (1) | PE20110807A1 (es) |
| PL (1) | PL2358710T3 (es) |
| PT (1) | PT2358710E (es) |
| RS (1) | RS52520B (es) |
| SI (1) | SI2358710T1 (es) |
| TN (1) | TN2011000207A1 (es) |
| TW (1) | TWI422587B (es) |
| UA (1) | UA100190C2 (es) |
| WO (1) | WO2010056563A1 (es) |
| ZA (1) | ZA201102549B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2448927T1 (sl) | 2009-07-02 | 2014-06-30 | Sanofi | Novi (6-okso-1,6-dihidro-pirimidin-2-il)-amidni derivati, njihova priprava in njihova farmacevtska uporaba kot AKT fosforilacijski inhibitorji |
| CN102574852B (zh) * | 2009-10-23 | 2014-06-25 | 伊莱利利公司 | Akt抑制剂 |
| AP3597A (en) | 2011-04-07 | 2016-02-19 | Bayer Ip Gmbh | Imidazopyridazines as akt kinase inhibitors |
| JP5695800B2 (ja) * | 2011-07-09 | 2015-04-08 | 山東軒竹医薬科技有限公司 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の塩の結晶形ｉ、及びその製造方法並びにその応用 |
| SI2755965T1 (sl) * | 2011-09-12 | 2017-12-29 | Merck Patent Gmbh | Novi imidazolni amidi kot modulatorji kinazne aktivnosti |
| HUE034979T2 (en) | 2011-09-12 | 2018-05-02 | Merck Patent Gmbh | Aminopyrimidine derivatives for use as modulators of kinase activity |
| AU2013344552B2 (en) * | 2012-11-16 | 2018-03-15 | Xiaoling Chen | Novel heterocyclic derivatives as modulators of kinase activity |
| US9315517B2 (en) * | 2012-11-16 | 2016-04-19 | Merck Patent Gmbh | Imidazol-piperidinyl derivatives as modulators of kinase activity |
| ES2746756T3 (es) | 2013-03-11 | 2020-03-06 | Merck Patent Gmbh | Derivados de 6-[4-(1H-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de la actividad cinasa |
| WO2015123174A1 (en) * | 2014-02-11 | 2015-08-20 | Merck Patent Gmbh | Pyrimidine imidazole amines as modulators of kinase activity |
| TW201718574A (zh) | 2015-08-12 | 2017-06-01 | 美國禮來大藥廠 | Ｃｇｒｐ受體拮抗劑 |
| TWI679202B (zh) * | 2016-05-20 | 2019-12-11 | 日商大鵬藥品工業股份有限公司 | 新穎5H-吡咯并[2, 3-d]嘧啶-6(7H)-酮衍生物 |
| CN115397815B (zh) * | 2020-03-17 | 2024-06-14 | 江苏恒瑞医药股份有限公司 | 稠合二环类衍生物、其制备方法及其在医药上的应用 |
| CN113444110B (zh) * | 2020-03-25 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用 |
| TW202328138A (zh) | 2021-09-17 | 2023-07-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | 稠合二環類衍生物的可藥用鹽、晶型及其製備方法 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005249380C1 (en) | 2004-04-23 | 2012-09-20 | Exelixis, Inc. | Kinase modulators and methods of use |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| ATE543821T1 (de) | 2004-12-28 | 2012-02-15 | Exelixis Inc | Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungen |
| WO2006091450A1 (en) * | 2005-02-18 | 2006-08-31 | Lexicon Genetics Incorporated | 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds |
| EP1907383A1 (en) | 2005-06-30 | 2008-04-09 | Prosidion Limited | Gpcr agonists |
| EP2043655A2 (en) | 2006-04-25 | 2009-04-08 | Astex Therapeutics Limited | Purine and deazapurine derivatives as pharmaceutical compounds |
| JP2009536620A (ja) | 2006-04-25 | 2009-10-15 | アステックス、セラピューティックス、リミテッド | 医薬組み合わせ物 |
| WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
| AR064416A1 (es) * | 2006-12-21 | 2009-04-01 | Cancer Rec Tech Ltd | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. |
| UA99284C2 (ru) | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
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2009
- 2009-10-28 AR ARP090104158A patent/AR074072A1/es unknown
- 2009-10-29 PA PA20098846901A patent/PA8846901A1/es unknown
- 2009-10-29 JO JO2009400A patent/JO2822B1/en active
- 2009-10-29 TW TW098136731A patent/TWI422587B/zh not_active IP Right Cessation
- 2009-11-03 WO PCT/US2009/063020 patent/WO2010056563A1/en active Application Filing
- 2009-11-03 CA CA2743019A patent/CA2743019C/en not_active Expired - Fee Related
- 2009-11-03 KR KR1020117010569A patent/KR101334460B1/ko not_active IP Right Cessation
- 2009-11-03 EA EA201170680A patent/EA018947B1/ru not_active IP Right Cessation
- 2009-11-03 NZ NZ592062A patent/NZ592062A/xx not_active IP Right Cessation
- 2009-11-03 PT PT09744896T patent/PT2358710E/pt unknown
- 2009-11-03 RS RS20120443A patent/RS52520B/en unknown
- 2009-11-03 EP EP09744896A patent/EP2358710B1/en active Active
- 2009-11-03 CN CN2009801449532A patent/CN102216302B/zh active Active
- 2009-11-03 BR BRPI0921916A patent/BRPI0921916A2/pt not_active IP Right Cessation
- 2009-11-03 DK DK09744896.3T patent/DK2358710T3/da active
- 2009-11-03 PE PE2011001018A patent/PE20110807A1/es not_active Application Discontinuation
- 2009-11-03 ES ES09744896T patent/ES2391704T3/es active Active
- 2009-11-03 US US12/611,139 patent/US8148387B2/en active Active
- 2009-11-03 SI SI200930348T patent/SI2358710T1/sl unknown
- 2009-11-03 PL PL09744896T patent/PL2358710T3/pl unknown
- 2009-11-03 JP JP2011536383A patent/JP5432275B2/ja active Active
- 2009-11-03 MY MYPI2011002030A patent/MY161461A/en unknown
- 2009-11-03 AU AU2009314324A patent/AU2009314324B2/en not_active Ceased
- 2009-11-03 UA UAA201105367A patent/UA100190C2/ru unknown
- 2009-11-03 MX MX2011005000A patent/MX2011005000A/es active IP Right Grant
-
2011
- 2011-03-24 IL IL211940A patent/IL211940A/en not_active IP Right Cessation
- 2011-04-06 ZA ZA2011/02549A patent/ZA201102549B/en unknown
- 2011-04-25 TN TN2011000207A patent/TN2011000207A1/fr unknown
- 2011-05-03 HN HN2011001247A patent/HN2011001247A/es unknown
- 2011-05-06 CR CR20110240A patent/CR20110240A/es unknown
- 2011-05-09 MA MA33822A patent/MA32776B1/fr unknown
- 2011-05-09 DO DO2011000129A patent/DOP2011000129A/es unknown
- 2011-05-11 EC EC2011011048A patent/ECSP11011048A/es unknown
- 2011-05-12 CO CO11058555A patent/CO6382114A2/es active IP Right Grant
- 2011-11-24 HK HK11112734.3A patent/HK1158203A1/xx not_active IP Right Cessation
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2012
- 2012-09-17 HR HRP20120738AT patent/HRP20120738T1/hr unknown
- 2012-10-05 CY CY20121100928T patent/CY1113409T1/el unknown
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| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |