PE20060608A1 - Analogos de 17-hidroxiwortmanina como inhibidores de pi3k - Google Patents
Analogos de 17-hidroxiwortmanina como inhibidores de pi3kInfo
- Publication number
- PE20060608A1 PE20060608A1 PE2005001208A PE2005001208A PE20060608A1 PE 20060608 A1 PE20060608 A1 PE 20060608A1 PE 2005001208 A PE2005001208 A PE 2005001208A PE 2005001208 A PE2005001208 A PE 2005001208A PE 20060608 A1 PE20060608 A1 PE 20060608A1
- Authority
- PE
- Peru
- Prior art keywords
- metoximethyl
- dodecahydroindene
- isocromen
- ilo
- dioxo
- Prior art date
Links
- 239000012828 PI3K inhibitor Substances 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 HYDROXY, CARBONYL Chemical class 0.000 abstract 2
- 208000006386 Bone Resorption Diseases 0.000 abstract 1
- 208000003174 Brain Neoplasms Diseases 0.000 abstract 1
- 230000024279 bone resorption Effects 0.000 abstract 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- HZVOZRGWRWCICA-UHFFFAOYSA-N methanediyl Chemical compound [CH2] HZVOZRGWRWCICA-UHFFFAOYSA-N 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- CFHIDWOYWUOIHU-UHFFFAOYSA-N oxomethyl Chemical compound O=[CH] CFHIDWOYWUOIHU-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
- C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
- C07J73/003—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by oxygen as hetero atom
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- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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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
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- 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
- A61P9/08—Vasodilators for multiple indications
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- 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
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/94—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Virology (AREA)
- AIDS & HIV (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE R1 ES NR4R5, SR6, OR7 DONDE R4 Y R5 SON H, OH, HETEROARILO, ENTRE OTROS; R6 ES ALQUILO, ARILO, HETEROARILO, ENTRE OTROS, R7 ES H, HETEROARILO, ARILO, ENTRE OTROS; R2 ES H, FORMILO, ACILO; R3 ES H, HIDROXI, CARBONILO, ENTRE OTROS; R8 ES OH, ACILOXI, ALCOXI. SON COMPUESTOS PREFERIDOS: ACETATO DE (1E,4S,4aR,5R,6aS,7S,9aR)-1-[(DIETILAMINO)METILEN]-7,11-DIHIDROXI-4-(METOXIMETIL)-4a,6a-DIMETIL-2,10-DIOXO-1,2,4,4a,5,6,6a,7,8,9,9a,10-DODECAHIDROINDENO[4,5-h]ISOCROMEN-5-ILO, ACETATO DE (1E,4S,4aR,5R,6aS,7S,9aR)-7,11-DIHIDROXI-4-(METOXIMETIL)-4a,6a-DIMETIL-2,10-DIOXO-1-(PIRROLIDIN-1-ILMETILEN)-1,2,4,4a,5,6,6a,7,8,9,9a,10-DODECAHIDROINDENO[4,5-h]ISOCROMEN-5-ILO, ACETATO DE (1E,4S,4aR,5R,6aS,7S,9aR)-1-(ANILINOMETILEN)-7,11-DIHIDROXI-4-(METOXIMETIL)-4a,6a-DIMETIL-2,10-DIOXO-1,2,4,4a,5,6,6a,7,8,9,9a,10-DODECAHIDROINDENO[4,5-h]ISOCROMEN-5-ILO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LA FOSFATIDILINOSITOL-3(OH)-QUINASA (PI3K) Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES TALES COMO CANCER CEREBRAL, RESORCION OSEA, ENTRE OTROS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61765404P | 2004-10-13 | 2004-10-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060608A1 true PE20060608A1 (es) | 2006-08-22 |
Family
ID=35502459
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005001208A PE20060608A1 (es) | 2004-10-13 | 2005-10-13 | Analogos de 17-hidroxiwortmanina como inhibidores de pi3k |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US7666901B2 (es) |
| EP (1) | EP1799699A1 (es) |
| JP (1) | JP2008515984A (es) |
| CN (1) | CN101039952A (es) |
| AR (1) | AR051388A1 (es) |
| AU (1) | AU2005295859A1 (es) |
| BR (1) | BRPI0516592A (es) |
| CA (1) | CA2582163A1 (es) |
| GT (1) | GT200500287A (es) |
| MX (1) | MX2007004489A (es) |
| PE (1) | PE20060608A1 (es) |
| TW (1) | TW200626610A (es) |
| WO (1) | WO2006044453A1 (es) |
Families Citing this family (107)
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| AU2005333515B2 (en) * | 2004-07-09 | 2012-05-10 | Arizona Board Of Regents, Acting On Behalf Of The University Of Arizona | Wortmannin analogs and methods of using same in combination with chemotherapeutic agents |
| ES2364495T3 (es) | 2005-02-03 | 2011-09-05 | The General Hospital Corporation | Método para tratar cáncer resistente a gefitinib. |
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| JP2009514870A (ja) | 2005-11-04 | 2009-04-09 | ワイス | ｍＴＯＲインヒビター、ハーセプチン、および／またはＨＫＩ−２７２の抗悪性腫瘍性組み合わせ |
| EP2043654A2 (en) * | 2006-06-12 | 2009-04-08 | Vertex Pharmaceuticals, Inc. | Thienopyrimidines useful as modulators of ion channels |
| CN101528231A (zh) | 2006-08-16 | 2009-09-09 | 埃克塞利希斯股份有限公司 | 在癌症的治疗中使用pi3k和mek调控剂 |
| TW200845960A (en) * | 2007-04-05 | 2008-12-01 | Wyeth Corp | Wortmannin-rapalog conjugate and uses thereof |
| US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
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| US20110135655A1 (en) * | 2009-01-13 | 2011-06-09 | PHILADELPHIA HEALTH AND EDUCATION CORPORATION d/b/a Drexel University College of Medicine; | Role of PI3K p110 delta Signaling in Retroviral Infection and Replication |
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| CN102821759A (zh) | 2010-03-30 | 2012-12-12 | 诺华有限公司 | 用于治疗具有慢性活性b细胞受体信号传导的b细胞淋巴瘤的pkc抑制剂 |
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| US5378725A (en) | 1993-07-19 | 1995-01-03 | The Arizona Board Of Regents | Inhibition of phosphatidylinositol 3-kinase with wortmannin and analogs thereof |
| US5468773A (en) | 1993-08-25 | 1995-11-21 | Eli Lilly And Company | Methods for inhibiting bone loss and cartilage degradation using wortmannin and its analogs |
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| BRPI0409681A (pt) * | 2003-04-23 | 2006-04-18 | Wyeth Corp | derivados de wortmanina solúveis em água |
| AU2005333515B2 (en) * | 2004-07-09 | 2012-05-10 | Arizona Board Of Regents, Acting On Behalf Of The University Of Arizona | Wortmannin analogs and methods of using same in combination with chemotherapeutic agents |
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- 2005-10-13 US US11/248,510 patent/US7666901B2/en not_active Expired - Fee Related
- 2005-10-13 TW TW094135618A patent/TW200626610A/zh unknown
- 2005-10-13 WO PCT/US2005/036664 patent/WO2006044453A1/en not_active Ceased
- 2005-10-13 AU AU2005295859A patent/AU2005295859A1/en not_active Abandoned
- 2005-10-13 GT GT200500287A patent/GT200500287A/es unknown
- 2005-10-13 MX MX2007004489A patent/MX2007004489A/es unknown
- 2005-10-13 EP EP05807576A patent/EP1799699A1/en not_active Withdrawn
- 2005-10-13 JP JP2007536835A patent/JP2008515984A/ja not_active Withdrawn
- 2005-10-13 BR BRPI0516592-0A patent/BRPI0516592A/pt not_active IP Right Cessation
- 2005-10-13 AR ARP050104294A patent/AR051388A1/es not_active Application Discontinuation
- 2005-10-13 CA CA002582163A patent/CA2582163A1/en not_active Abandoned
- 2005-10-13 CN CNA2005800349346A patent/CN101039952A/zh active Pending
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| GT200500287A (es) | 2006-04-17 |
| WO2006044453A1 (en) | 2006-04-27 |
| AU2005295859A1 (en) | 2006-04-27 |
| JP2008515984A (ja) | 2008-05-15 |
| CN101039952A (zh) | 2007-09-19 |
| EP1799699A1 (en) | 2007-06-27 |
| MX2007004489A (es) | 2007-09-21 |
| US7666901B2 (en) | 2010-02-23 |
| CA2582163A1 (en) | 2006-04-27 |
| US20060128793A1 (en) | 2006-06-15 |
| AR051388A1 (es) | 2007-01-10 |
| BRPI0516592A (pt) | 2008-09-23 |
| TW200626610A (en) | 2006-08-01 |
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