PE20121159A1 - DERIVADOS DE PIRIDINA, PIRAZINA Y QUINOLINA COMO INHIBIDORES DE LA FOSFOINOSITIDA 3 CINASA Y LA mTOR - Google Patents
DERIVADOS DE PIRIDINA, PIRAZINA Y QUINOLINA COMO INHIBIDORES DE LA FOSFOINOSITIDA 3 CINASA Y LA mTORInfo
- Publication number
- PE20121159A1 PE20121159A1 PE2011001861A PE2011001861A PE20121159A1 PE 20121159 A1 PE20121159 A1 PE 20121159A1 PE 2011001861 A PE2011001861 A PE 2011001861A PE 2011001861 A PE2011001861 A PE 2011001861A PE 20121159 A1 PE20121159 A1 PE 20121159A1
- Authority
- PE
- Peru
- Prior art keywords
- amine
- mtor
- kinase
- pyridin
- methyl
- Prior art date
Links
- 108091007960 PI3Ks Proteins 0.000 title abstract 3
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 title abstract 3
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title abstract 3
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 title abstract 2
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 title abstract 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 title 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical class C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical group C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical group [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 abstract 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 abstract 1
- 229960002930 sirolimus Drugs 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring 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
- A61K31/52—Purines, e.g. adenine
-
- 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
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
REFERIDA A UN DERIVADO DE AMINA DE FORMULA (I), DONDE Ar1 ES UN ANILLO MONOCICLICO O BICICLICO DE 5 HASTA 10 MIEMBROS QUE PUEDE CONTENER DE 0 A 4 HETEROATOMOS SELECCIONADOS DE O, N Y S, EL CUAL PUEDE ESTAR SUSTITUIDO CON HALO, CN, NITRO, ENTRE OTROS; Q ES UN GRUPO (a); R2 ES METILO O ETILO; Z5 ES N O CRc; Z9 ES N, NR O CR; Z10 ES N, NR O CR; R ES H, OXO, HALOALQUILO C1-C4, ENTRE OTROS; Rc ES H, ALQUILO C1-C6, CF3, ENTRE OTROS; Z1, Z2, Z3 Y Z4 SON N, NR, CR, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(3-(4-AMINO-6-METIL-1,3,5-TRIZIN-2-IL)PIRIDIN-2-IL)-1H-INDOL-4-AMINA, 4-(2-(6-METOXIPIRIDIN-3-ILAMINO)PIRIDIN-3-IL)-6-METIL-1,3,5-TRIAZIN-2-AMINA, N-(3-(6-AMINO-2-METILPIRIMIDIN-4-IL)PIRIDIN-2-IL)-1H-INDAZOL-4-AMINA, ENTRE OTROS. DICHOS COMPUESTOS INHIBEN LA FOSFOINOSITIDA 3 CINASA (PIK3) Y/U OBJETIVO MAMIFERO DE RAPAMICINA (mTOR) Y SON UTILES EN EL TRATAMIENTO DEL CANCER
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17352009P | 2009-04-28 | 2009-04-28 | |
| US25853209P | 2009-11-05 | 2009-11-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121159A1 true PE20121159A1 (es) | 2012-09-19 |
Family
ID=42315845
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001861A PE20121159A1 (es) | 2009-04-28 | 2010-04-27 | DERIVADOS DE PIRIDINA, PIRAZINA Y QUINOLINA COMO INHIBIDORES DE LA FOSFOINOSITIDA 3 CINASA Y LA mTOR |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8362241B2 (es) |
| EP (1) | EP2424859B1 (es) |
| JP (1) | JP5697662B2 (es) |
| KR (1) | KR20120007540A (es) |
| CN (1) | CN102548984B (es) |
| AR (1) | AR076486A1 (es) |
| AU (1) | AU2010241723B2 (es) |
| BR (1) | BRPI1015262A2 (es) |
| CA (1) | CA2758986C (es) |
| CL (1) | CL2011002691A1 (es) |
| CO (1) | CO6440596A2 (es) |
| CR (1) | CR20110634A (es) |
| EA (1) | EA019700B1 (es) |
| IL (1) | IL215731A0 (es) |
| MA (1) | MA34207B1 (es) |
| MX (1) | MX2011011335A (es) |
| NZ (1) | NZ595572A (es) |
| PE (1) | PE20121159A1 (es) |
| SG (1) | SG175364A1 (es) |
| TW (1) | TW201103902A (es) |
| UY (1) | UY32582A (es) |
| WO (1) | WO2010126895A1 (es) |
| ZA (1) | ZA201108101B (es) |
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- 2010-04-27 EP EP10718364.2A patent/EP2424859B1/en active Active
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- 2010-04-27 JP JP2012508595A patent/JP5697662B2/ja active Active
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- 2010-04-27 WO PCT/US2010/032593 patent/WO2010126895A1/en not_active Ceased
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- 2010-04-27 SG SG2011078748A patent/SG175364A1/en unknown
- 2010-04-27 NZ NZ595572A patent/NZ595572A/xx not_active IP Right Cessation
- 2010-04-27 CN CN201080030184.6A patent/CN102548984B/zh not_active Expired - Fee Related
- 2010-04-27 PE PE2011001861A patent/PE20121159A1/es not_active Application Discontinuation
- 2010-04-27 AU AU2010241723A patent/AU2010241723B2/en active Active
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- 2010-04-27 EA EA201101583A patent/EA019700B1/ru not_active IP Right Cessation
- 2010-04-27 KR KR1020117028155A patent/KR20120007540A/ko not_active Withdrawn
- 2010-04-28 AR ARP100101435A patent/AR076486A1/es not_active Application Discontinuation
- 2010-04-28 TW TW099113553A patent/TW201103902A/zh unknown
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- 2011-11-04 ZA ZA2011/08101A patent/ZA201108101B/en unknown
- 2011-11-25 MA MA34389A patent/MA34207B1/fr unknown
- 2011-11-28 CR CR20110634A patent/CR20110634A/es unknown
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|---|---|
| IL215731A0 (en) | 2012-01-31 |
| JP2012525395A (ja) | 2012-10-22 |
| BRPI1015262A2 (pt) | 2016-05-03 |
| ZA201108101B (en) | 2012-07-25 |
| EP2424859A1 (en) | 2012-03-07 |
| CL2011002691A1 (es) | 2012-03-16 |
| HK1167862A1 (en) | 2012-12-14 |
| TW201103902A (en) | 2011-02-01 |
| US8772480B2 (en) | 2014-07-08 |
| CA2758986A1 (en) | 2010-11-04 |
| AU2010241723A1 (en) | 2011-11-17 |
| EA201101583A1 (ru) | 2012-05-30 |
| MX2011011335A (es) | 2011-11-18 |
| EA019700B1 (ru) | 2014-05-30 |
| CA2758986C (en) | 2014-05-27 |
| US20100273764A1 (en) | 2010-10-28 |
| KR20120007540A (ko) | 2012-01-20 |
| SG175364A1 (en) | 2011-11-28 |
| UY32582A (es) | 2010-11-30 |
| EP2424859B1 (en) | 2015-04-08 |
| JP5697662B2 (ja) | 2015-04-08 |
| CN102548984B (zh) | 2015-11-25 |
| NZ595572A (en) | 2013-07-26 |
| US20130079303A1 (en) | 2013-03-28 |
| US8362241B2 (en) | 2013-01-29 |
| MA34207B1 (fr) | 2013-05-02 |
| AU2010241723B2 (en) | 2012-12-13 |
| AR076486A1 (es) | 2011-06-15 |
| CR20110634A (es) | 2012-01-06 |
| WO2010126895A1 (en) | 2010-11-04 |
| CO6440596A2 (es) | 2012-05-15 |
| CN102548984A (zh) | 2012-07-04 |
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