PE20091384A1 - Compuestos tienopirimidina y pirazolopirimidina como inhibidores de quinasa mtor y quinasa p13 - Google Patents
Compuestos tienopirimidina y pirazolopirimidina como inhibidores de quinasa mtor y quinasa p13Info
- Publication number
- PE20091384A1 PE20091384A1 PE2008001780A PE2008001780A PE20091384A1 PE 20091384 A1 PE20091384 A1 PE 20091384A1 PE 2008001780 A PE2008001780 A PE 2008001780A PE 2008001780 A PE2008001780 A PE 2008001780A PE 20091384 A1 PE20091384 A1 PE 20091384A1
- Authority
- PE
- Peru
- Prior art keywords
- kinase
- halo
- oxa
- pyrimidin
- oct
- Prior art date
Links
- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical class C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 102100023085 Serine/threonine-protein kinase mTOR Human genes 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- NLOLSXYRJFEOTA-OWOJBTEDSA-N (e)-1,1,1,4,4,4-hexafluorobut-2-ene Chemical class FC(F)(F)\C=C\C(F)(F)F NLOLSXYRJFEOTA-OWOJBTEDSA-N 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 208000020084 Bone disease Diseases 0.000 abstract 1
- 102000038030 PI3Ks Human genes 0.000 abstract 1
- 108091007960 PI3Ks Proteins 0.000 abstract 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 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
- GTCAXTIRRLKXRU-UHFFFAOYSA-N carbamic acid methyl ester Natural products COC(N)=O GTCAXTIRRLKXRU-UHFFFAOYSA-N 0.000 abstract 1
- 239000004202 carbamide Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- 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
- 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
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- 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
- 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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
REFERIDA A COMPUESTOS DERIVADOS DE TIENOPIRIMIDINA Y PIRAZOLOPIRIMIDINA DE FORMULAS (Ia) Y (IIa), DONDE Het ES UN HETEROBICICLILO DE 5 A 10 MIEMBROS QUE CONTIENE POR LO MENOS UN ATOMO DE O Y N; Y OPCIONALMENTE HETEROATOMOS ADICIONALES DE O, S Y N; R20 ES OH, HALO, ALCOXI(C1-C2), ENTRE OTROS; R1 ES HALO, ALQUILO(C1-C6), ENTRE OTROS; R2 ES H, HALO, ACILO(C1-C8), ENTRE OTROS; R3 ES H, ALQUILO(C1-C6), ENTRE OTROS; R8 ES H, HALO, ALQUILO(C1-C6), ENTRE OTROS; Ar ES FENILO, NAFTILO, ENTRE OTROS; t ES DE 0 A 16; m ES DE 0 A 4; r ES 0 O 1. SON COMPUESTOS PREFERIDOS: 3-[4-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-1L)-1-FENIL-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL]FENOL, 1-METIL-3-{4-[4-(8-OXA-3-AZABICILO[3.2.1]OCT-3-IL)-1-(2,2,2-TRIFLUOROETIL)-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL]FENIL}UREA, {4-[4-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-IL)-1-(2,2,2-TRIFLUOROETIL)-1H-PIRAZOLO[2,3-d]PIRIMIDIN-6-IL]FENIL}CARBAMATO DE METILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASA mTOR Y DE QUINASA PI3K, SIENDO UTILES PARA EL TRATAMIENTO DE TRASTORNOS OSEOS, CANCER DE PROSTATA, ANGIOGENIA, ENTRE OTROS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98033207P | 2007-10-16 | 2007-10-16 | |
| US2759508P | 2008-02-11 | 2008-02-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091384A1 true PE20091384A1 (es) | 2009-09-09 |
Family
ID=40345078
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001780A PE20091384A1 (es) | 2007-10-16 | 2008-10-16 | Compuestos tienopirimidina y pirazolopirimidina como inhibidores de quinasa mtor y quinasa p13 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8129371B2 (es) |
| EP (1) | EP2212333A1 (es) |
| JP (1) | JP2011500702A (es) |
| KR (1) | KR20100083170A (es) |
| CN (1) | CN101883774A (es) |
| AP (1) | AP2010005234A0 (es) |
| AR (1) | AR068898A1 (es) |
| AU (1) | AU2008312631A1 (es) |
| BR (1) | BRPI0817681A2 (es) |
| CA (1) | CA2702838A1 (es) |
| CL (1) | CL2008003061A1 (es) |
| CO (1) | CO6321257A2 (es) |
| CR (1) | CR11373A (es) |
| DO (1) | DOP2010000118A (es) |
| EA (1) | EA201000484A1 (es) |
| EC (1) | ECSP10010112A (es) |
| IL (1) | IL205109A0 (es) |
| MA (1) | MA31884B1 (es) |
| MX (1) | MX2010004260A (es) |
| NI (1) | NI201000060A (es) |
| PA (1) | PA8799101A1 (es) |
| PE (1) | PE20091384A1 (es) |
| TN (1) | TN2010000171A1 (es) |
| TW (1) | TW200922593A (es) |
| WO (1) | WO2009052145A1 (es) |
| ZA (1) | ZA201003430B (es) |
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| CL2008003798A1 (es) | 2007-12-19 | 2009-10-09 | Amgen Inc | Compuestos derivados de heterobiciclos aromaticos sustituidos, inhibidores de pi3 quinasa; composicion farmaceutica; utiles en el tratamiento de cancer, melanomas, glioblastomas, entre otras enfermedades. |
| BRPI0911377A8 (pt) | 2008-04-11 | 2017-12-05 | Trubion Pharmaceuticals Inc | Imunoterápico de cd7 e combinação com quimioterápico bifuncional deste |
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| EP1277738B1 (en) | 2000-04-27 | 2011-03-30 | Astellas Pharma Inc. | Condensed heteroaryl derivatives |
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- 2008-10-15 MX MX2010004260A patent/MX2010004260A/es not_active Application Discontinuation
- 2008-10-15 AP AP2010005234A patent/AP2010005234A0/xx unknown
- 2008-10-15 AU AU2008312631A patent/AU2008312631A1/en not_active Abandoned
- 2008-10-15 CA CA2702838A patent/CA2702838A1/en not_active Abandoned
- 2008-10-15 WO PCT/US2008/079940 patent/WO2009052145A1/en not_active Ceased
- 2008-10-15 CN CN2008801190434A patent/CN101883774A/zh active Pending
- 2008-10-15 US US12/251,712 patent/US8129371B2/en not_active Expired - Fee Related
- 2008-10-15 BR BRPI0817681 patent/BRPI0817681A2/pt not_active Application Discontinuation
- 2008-10-15 KR KR1020107010683A patent/KR20100083170A/ko not_active Ceased
- 2008-10-15 EP EP08839537A patent/EP2212333A1/en not_active Withdrawn
- 2008-10-15 EA EA201000484A patent/EA201000484A1/ru unknown
- 2008-10-16 AR ARP080104520A patent/AR068898A1/es unknown
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- 2008-10-16 PE PE2008001780A patent/PE20091384A1/es not_active Application Discontinuation
- 2008-10-16 CL CL2008003061A patent/CL2008003061A1/es unknown
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- 2010-04-15 CR CR11373A patent/CR11373A/es not_active Application Discontinuation
- 2010-04-16 MA MA32778A patent/MA31884B1/fr unknown
- 2010-04-16 EC EC2010010112A patent/ECSP10010112A/es unknown
- 2010-04-16 TN TN2010000171A patent/TN2010000171A1/fr unknown
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- 2010-04-20 CO CO10046199A patent/CO6321257A2/es not_active Application Discontinuation
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Also Published As
| Publication number | Publication date |
|---|---|
| JP2011500702A (ja) | 2011-01-06 |
| AU2008312631A1 (en) | 2009-04-23 |
| CR11373A (es) | 2010-05-03 |
| AP2010005234A0 (en) | 2010-04-30 |
| MA31884B1 (fr) | 2010-12-01 |
| EP2212333A1 (en) | 2010-08-04 |
| KR20100083170A (ko) | 2010-07-21 |
| TW200922593A (en) | 2009-06-01 |
| PA8799101A1 (es) | 2009-05-15 |
| CN101883774A (zh) | 2010-11-10 |
| IL205109A0 (en) | 2010-11-30 |
| CO6321257A2 (es) | 2011-09-20 |
| EA201000484A1 (ru) | 2010-12-30 |
| DOP2010000118A (es) | 2010-06-30 |
| BRPI0817681A2 (pt) | 2015-04-14 |
| NI201000060A (es) | 2010-10-04 |
| ZA201003430B (en) | 2011-02-23 |
| MX2010004260A (es) | 2010-04-30 |
| US8129371B2 (en) | 2012-03-06 |
| WO2009052145A1 (en) | 2009-04-23 |
| AR068898A1 (es) | 2009-12-16 |
| CL2008003061A1 (es) | 2009-01-09 |
| US20090098086A1 (en) | 2009-04-16 |
| CA2702838A1 (en) | 2009-04-23 |
| ECSP10010112A (es) | 2010-08-31 |
| TN2010000171A1 (fr) | 2011-11-11 |
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