AR110388A2 - INHIBIDORES DE LA QUINASA mTOR PARA INDICACIONES EN ONCOLOGÍA Y ENFERMEDADES ASOCIADAS CON LA VÍA DE mTOR / PI3K / AKT - Google Patents
INHIBIDORES DE LA QUINASA mTOR PARA INDICACIONES EN ONCOLOGÍA Y ENFERMEDADES ASOCIADAS CON LA VÍA DE mTOR / PI3K / AKTInfo
- Publication number
- AR110388A2 AR110388A2 ARP170103549A ARP170103549A AR110388A2 AR 110388 A2 AR110388 A2 AR 110388A2 AR P170103549 A ARP170103549 A AR P170103549A AR P170103549 A ARP170103549 A AR P170103549A AR 110388 A2 AR110388 A2 AR 110388A2
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- unsubstituted
- fused
- mtor
- Prior art date
Links
- 102000038030 PI3Ks Human genes 0.000 title 1
- 108091007960 PI3Ks Proteins 0.000 title 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 title 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000002950 monocyclic group Chemical group 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical group NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 abstract 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 abstract 2
- XYFCBTPGUUZFHI-UHFFFAOYSA-N Phosphine Chemical group P XYFCBTPGUUZFHI-UHFFFAOYSA-N 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000003367 polycyclic group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 abstract 1
- JOYRKODLDBILNP-UHFFFAOYSA-N Ethyl urethane Chemical group CCOC(N)=O JOYRKODLDBILNP-UHFFFAOYSA-N 0.000 abstract 1
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical group ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 abstract 1
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Chemical group CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-M Thiocyanate anion Chemical compound [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 abstract 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical group NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 150000001299 aldehydes Chemical group 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000005262 alkoxyamine group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 abstract 1
- 150000001409 amidines Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 150000001540 azides Chemical class 0.000 abstract 1
- 239000004202 carbamide Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- XLJMAIOERFSOGZ-UHFFFAOYSA-M cyanate Chemical compound [O-]C#N XLJMAIOERFSOGZ-UHFFFAOYSA-M 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Chemical group CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 abstract 1
- 150000002081 enamines Chemical group 0.000 abstract 1
- 150000002148 esters Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 abstract 1
- -1 hydrazide Chemical class 0.000 abstract 1
- 150000007857 hydrazones Chemical class 0.000 abstract 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 150000003949 imides Chemical group 0.000 abstract 1
- 150000002466 imines Chemical group 0.000 abstract 1
- 239000012948 isocyanate Substances 0.000 abstract 1
- 150000002513 isocyanates Chemical class 0.000 abstract 1
- 150000002540 isothiocyanates Chemical class 0.000 abstract 1
- 150000002576 ketones Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 150000002923 oximes Chemical group 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical group [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 abstract 1
- 229910000073 phosphorus hydride Inorganic materials 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229940124530 sulfonamide Drugs 0.000 abstract 1
- 150000003456 sulfonamides Chemical group 0.000 abstract 1
- 150000003457 sulfones Chemical group 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 abstract 1
- 150000003568 thioethers Chemical group 0.000 abstract 1
- 150000003573 thiols Chemical group 0.000 abstract 1
Classifications
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- C07—ORGANIC CHEMISTRY
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- 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
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- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- Emergency Medicine (AREA)
Abstract
Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), o su sal, clatrato, solvato, tautómero, estereoisómero o prodroga farmacéuticamente aceptable del mismo, en donde: R¹ es piridilo sustituido o no sustituido; R² es H, C₁₋₈ alquilo sustituido o no sustituido, C₃₋₁₀ cicloalquilo sustituido o no sustituido, heterociclilo de 3 a 10 miembros que contiene 1 a 4 heteroátomos del grupo que consiste en O, S y N sustituido o no sustituido, C₁₋₈ alquil-(heterociclilo de 3 a 10 miembros que contiene 1 a 4 heteroátomos del grupo que consiste en O, S y N) sustituido o no sustituido, C₁₋₈ alquil-C₆₋₁₄ aralquilo sustituido o no sustituido, o C₁₋₈ alquil-C₃₋₁₀ cicloalquilalquilo sustituido o no sustituido; R³ es H o C₁₋₈ alquilo sustituido o no sustituido; en donde sustituido significa sustituido con un sustituyente seleccionado del grupo que consiste en halógeno, alquilo, hidroxi, alcoxi, alcoxialquilo, amino, alquilamino, carboxi, nitro, ciano, tiol, tioeter, imina, imida, amidina, guanidina, enamina, aminocarbonilo, acilamino, fosfonato, fosfina, tiocarbonilo, sulfonilo, sulfona, sulfonamida, alquilsulfonilamino, cetona, aldehido, éster, urea, uretano, oxima, hidroxil amina, alcoxiamina, aralcoxiamina, N-óxido, hidrazina, hidrazida, hidrazona, azida, isocianato, isotiocianato, cianato, tiocianato, oxígeno, B(OH)₂, O(alquil)aminocarbonilo, cicloalquilo, que puede ser monocíclico o policíclico fusionado o no-fusionado, o un heterociclilo, que puede ser monocíclico o policíclico fusionado o no-fusionado, arilo o heteroarilo monocíclico o policíclico fusionado o no-fusionado, ariloxi, hidroxialquilo, aralquilo, aralquiloxi, hetorocicliloxi, heterociclilalquilo, y heterociclil alcoxi.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US10862708P | 2008-10-27 | 2008-10-27 |
Publications (1)
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AR110388A2 true AR110388A2 (es) | 2019-03-27 |
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Family Applications (2)
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ARP090104139A AR073995A1 (es) | 2008-10-27 | 2009-10-27 | Inhibidores de la quinasa mtor para indicaciones en oncologia y enfermedades asociadas con la via de mtor/pi3k/akt |
ARP170103549A AR110388A2 (es) | 2008-10-27 | 2017-12-18 | INHIBIDORES DE LA QUINASA mTOR PARA INDICACIONES EN ONCOLOGÍA Y ENFERMEDADES ASOCIADAS CON LA VÍA DE mTOR / PI3K / AKT |
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ARP090104139A AR073995A1 (es) | 2008-10-27 | 2009-10-27 | Inhibidores de la quinasa mtor para indicaciones en oncologia y enfermedades asociadas con la via de mtor/pi3k/akt |
Country Status (35)
Country | Link |
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US (10) | US8110578B2 (es) |
EP (5) | EP3660020B1 (es) |
JP (3) | JP5689420B2 (es) |
KR (2) | KR101815604B1 (es) |
CN (3) | CN102245611B (es) |
AR (2) | AR073995A1 (es) |
AU (1) | AU2009320137C1 (es) |
BR (1) | BRPI0920254A2 (es) |
CA (1) | CA2740975C (es) |
CO (1) | CO6501147A2 (es) |
CR (1) | CR20110223A (es) |
CY (2) | CY1117272T1 (es) |
DK (2) | DK2740732T3 (es) |
EC (1) | ECSP11011084A (es) |
ES (4) | ES2620774T3 (es) |
HK (3) | HK1154858A1 (es) |
HR (2) | HRP20160084T1 (es) |
HU (1) | HUE026834T2 (es) |
IL (1) | IL212440A (es) |
LT (1) | LT2740732T (es) |
MX (2) | MX2011004401A (es) |
MY (1) | MY159235A (es) |
NI (1) | NI201100080A (es) |
NZ (4) | NZ603831A (es) |
PE (3) | PE20110575A1 (es) |
PL (2) | PL2740732T3 (es) |
PT (1) | PT2740732T (es) |
RU (2) | RU2546658C2 (es) |
SG (3) | SG10201402273RA (es) |
SI (2) | SI2740733T1 (es) |
SM (1) | SMT201600089B (es) |
TW (3) | TWI605047B (es) |
UA (1) | UA108601C2 (es) |
WO (1) | WO2010062571A1 (es) |
ZA (1) | ZA201102813B (es) |
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