ES2632269T3 - Moduladores de quinolinailo enlazados a metileno de ROR-gamma-t - Google Patents
Moduladores de quinolinailo enlazados a metileno de ROR-gamma-t Download PDFInfo
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- ES2632269T3 ES2632269T3 ES13786564.8T ES13786564T ES2632269T3 ES 2632269 T3 ES2632269 T3 ES 2632269T3 ES 13786564 T ES13786564 T ES 13786564T ES 2632269 T3 ES2632269 T3 ES 2632269T3
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- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- 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
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- A—HUMAN NECESSITIES
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- 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
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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
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- 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]
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
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- 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
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Abstract
Un compuesto de Fórmula I en la que:**Fórmula** R1 es pirrolilo, pirazolilo, imidazolilo, triazolilo, tiazolilo, piridilo, piridilo N-óxido, pirazinilo, pirimidinilo, piridazilo, piperidinilo, quinazolinilo, cinolinilo, bcnzotiazolilo, indazolilo, tetrahidropiranilo, tetrahidrofuranilo, furanilo, fenilo, oxazolilo, isoxazolilo, tiofenilo, benzoxazolilo, bencimidazolilo, indolilo, tiadiazolilo, oxadiazolilo o quinolinilo; en el que dicho piridilo, piridilo N-óxido, pirazinilo, pirimidinilo, piridazilo, piperidinilo, quinazolinilo, cinolinilo, benzotiazolilo, indazolilo, imidazolilo, fenilo, tiofenilo, benzoxazolilo, bencimidazolilo, indolilo, quinolinilo, y pirazolilo están opcionalmente sustituidos con C(O)C(1-4)alquilo, C(O)NH2, C(O)NHC(1-2)alquilo, C(O)N(C(1-2)alquilo)2, NHC(O)C(1-4)alquilo, NHSO2C(1-4)alquilo, C(1-4)alquilo, CF3, CH2CF3, Cl, F, -CN, OC(1-4)alquilo, N(C(1-4)alquilo)2, (CH2)3OCH3, SC(1-4)alquilo, OH, CO2H, CO2C(1-4)alquilo, C(O)CF3, SO2CF3, OCF3, OCHF2, SO2CH3, SO2NH2, SO2NHC(1-2)alquilo, SO2N(C(1-2)alquilo)2, C(O)NHSO2CH3, o OCH2OCH3; y opcionalmente sustituidos con hasta dos sustituyentes adicionales seleccionados independientemente del grupo que consiste en Cl, C(1-2)alquilo, SCH3, OC(1-2)alquilo, CF3, -CN, y F; y en donde dichos triazolilo, oxazolilo, isoxazolilo, pirrolilo, y tiazolilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados independientemente del grupo que consiste en SO2CH3, SO2NH2, alquilo C(O)NH2, -CN, OC(1-2), (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, y C(1-2)alquilo; y dicho tiadiazolilo y oxadiazolilo están opcionalmente sustituidos con C(1-2)alquilo; y dichos piridilo, piridilo-N-óxido, pirimidinilo, piridazilo, y pirazinilo están opcionalmente sustituidos con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en C(O)NHC(1-2)alquilo, C(O)N(C(1-2)alquilo)2, NHC(O)C(1-4)alquilo, NHSO2C(1-4)alquilo, C(O)CF3, SO2CF3, SO2NHC(1-2)alquilo, SO2N(C(1-2)NHC alquilo)2, C(O)NHSO2CH3, SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-4)alquilo, (CH2)(2-3)OCH3, SC(1-4)alquilo, CF3, F, Cl, y C(1-4)alquilo; R2 es triazolilo, piridilo, piridilo-N-óxido, pirazolilo, pirimidinilo, oxazolilo, isoxazolilo, azetidina-3-ilo, N-acetilo-azetidina-3-ilo, N-metilosulfonilo-azetidina-3-ilo, N-Boc-azetidina-3-ilo, N-acetilo piperidinilo, 1-H-piperidinilo, N-Boc-piperidinilo, NC(1-3)alquilo-piperidinilo, tiazolilo, piridazilo, pirazinilo, 1-(3-metoxipropilo)-imidazolilo, tiadiazolilo, oxadiazolilo, o imidazolilo; en el que dicho imidazolilo está opcionalmente sustituido con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en C(1-2)alquilo, SCH3, OC(1-2)alquilo, CF3, -CN, F, y Cl; y dichos piridilo, piridilo-N-óxido, pirimidinilo, piridazilo, y pirazinilo, están opcionalmente sustituidos con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alquilo, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, o C(1-2)alquilo; y dichos triazolilo, tiazolilo, oxazolilo e isoxazolilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados independientemente del grupo que consiste en OC(1-2)alquilo SO2CH3, SO2NH2, C(O)NH2, -CN, (CH2)(2-3)OCH3, SCH, CF3, F, alquilo Cl, y C(1-2)alquilo; y dichos tiadiazolilo y oxadiazolilo están opcionalmente sustituidos con C(1-2)alquilo; y dicho pirazolilo está opcionalmente sustituido con hasta tres grupos CH3; R3 es H, OH, OCH3, o NH2; R4 es H o F; R5 es H, Cl, -CN, CF3, SC(1-4)alquilo, OC(1-4)alquilo, OH, C(1-4)alquilo, N(CH3)OCH3, NH(C(1-4)alquilo), N(C(1-4)alquilo)2, o 4-hidroxi-piperidinilo; R6 es fenilo, piridilo, benzotiofenilo, tiofenilo, pirimidinilo, piridazilo, o pirazinilo; donde dichos pirimidinilo, piridazilo, pirazinilo o están opcionalmente sustituidos con Cl, F, CH3, SCH, OC(1-4)alquilo, -CN, CONH2, SO2NH2, o SO2CH3; y en el que dicho fenilo o dicho piridilo está opcionalmente sustituido hasta dos veces con OCF3, SO2C(1-4)alquilo, CF3, CHF2, pirazolilo, triazolilo, imidazolilo, tetrazolilo, oxazolilo, tiazolilo, C(1-4)alquilo, C(3-4)cicloalquilo, OC(1-4)alquilo, N(CH3)2, SO2NH2, SO2NHCH3, SO2N(CH3)2, CONH2, CONHCH3, CON(CH3)2, Cl, F, -CN, CO2H, OH, CH2OH, 55 NHCO(1-2)alquilo, COC(1-2)alquilo, SCH3, CO2C(1-4)alquilo, NH2, NHC(1-2)alquilo, o OCH2CF3; en el que la selección de cada sustituyente opcional es independiente; y en donde dichos pirazolilo, triazolilo, imidazolilo, tetrazolilo, oxazolilo, y tiazolilo están opcionalmente sustituidos con CH3; R7 es H, Cl, -CN, C(1-4)alquilo, OC(1-4)alquiloCF3, OCF3, OCHF2, OCH2CH2OC(1-4)alquilo, CF3, SCH3, C(1-4)alquiloNA1A2, CH2OC(2-3)alquiloNA1A2, NA1A2, C(O)NA1A2, CH2NHC(2-3)alquiloNA1A2, CH2N(CH3)C(2-3)alquiloNA1A2, NHC(2-3)alquiloNA1A2, N(CH3)C(2-4)alquiloNA1A2, OC(2-4)alquiloNA1A2, OC(1-4)aIquilo, OCH2-(1-metilo)-imidazol-2-ilo, fenilo, tiofenilo, furilo, pirazolilo, imidazolilo, piridilo, piridazilo, pirazinilo o pirimidinilo; en el que dichos fenilo, tiofenilo, furilo, pirazolilo, imidazolilo, piridilo, piridazilo, pirazinilo, y pirimidinilo están opcionalmente sustituidos con hasta tres sustituyentes seleccionados independientemente entre el grupo que consiste en F, Cl, CH3, CF3, OCH3 y; A1 es H, o C(1-4)alquilo; A2 es H, alquilo C(1-4)alquilo, C(1-4)alquiloC(1-4)alquilo, C(1-4)alquiloH, C(O)C(1-4)alquilo, o OC(1-4)alquilo; o A1 y A2 pueden ser tomados juntos con su nitrógeno unido para formar un anillo seleccionado del grupo que consiste en:**Fórmula** Ra es H, OC(1-4)alquilo, CH2OH, NH(CH3), N(CH3)2, NH2, CH3, F, CF3, SO2CH3, o OH; Rb es H, CO2C(CH3), C(1-4)alquilo, C(O)C(1-4)alquilo, SO2C(1-4)alquilo, CH2CH2CF3, CH2CF3, CH2-ciclopropilo, fenilo, CH2-fenilo, o C(3-6)cicloalquilo; R8 es H, alquilo C(1-3)alquilo, OC(1-3), CF3, NH2, NHCH3, -CN, o F; R9 es H o F; y las sales farmacéuticamente aceptables de los mismos; siempre que (4-cloro-2-metoxi-3-(4-(trifluorometilo)bencilo)quinolina-6-ilo)bis(1,2,5-trimetilo-1H-imidazol-4-ilo)metanol, N-(2-((3-(4-(1 H-pirazol-1-ilo)bencilo)-6-((4-clorofenilo)(hidroxi)(1-metilo-1H-imidazol-5-ilo)metilo)-4-hidroxiquinolina-2-ilo)oxi)etilo)acetamida y (3-(4-(1H-pirazol-1-ilo)bencilo)-4-cloro-2-(4-metilopiperazina-1-ilo)quinolina-6-ilo)(1-metilo-1H-imidazol-5-ilo)(6-(trifluorometilo)piridina-3-ilo)metanol están excluidos de la reivindicación.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261714419P | 2012-10-16 | 2012-10-16 | |
US201261714419P | 2012-10-16 | ||
US201261725528P | 2012-11-13 | 2012-11-13 | |
US201261725528P | 2012-11-13 | ||
US201361782257P | 2013-03-14 | 2013-03-14 | |
US201361782257P | 2013-03-14 | ||
PCT/US2013/065013 WO2014062658A1 (en) | 2012-10-16 | 2013-10-15 | Methylene linked quinolinyl modulators of ror-gamma-t |
Publications (1)
Publication Number | Publication Date |
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ES2632269T3 true ES2632269T3 (es) | 2017-09-12 |
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Application Number | Title | Priority Date | Filing Date |
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ES13786564.8T Active ES2632269T3 (es) | 2012-10-16 | 2013-10-15 | Moduladores de quinolinailo enlazados a metileno de ROR-gamma-t |
Country Status (38)
Country | Link |
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US (1) | US9290476B2 (es) |
EP (1) | EP2909192B1 (es) |
JP (1) | JP6466335B2 (es) |
KR (1) | KR20150070347A (es) |
CN (1) | CN105209453B (es) |
AR (1) | AR093017A1 (es) |
AU (1) | AU2013331496B2 (es) |
BR (1) | BR112015008308A2 (es) |
CA (1) | CA2888210C (es) |
CL (1) | CL2015000945A1 (es) |
CR (1) | CR20150193A (es) |
CY (1) | CY1119234T1 (es) |
DK (1) | DK2909192T3 (es) |
EA (1) | EA026415B1 (es) |
EC (1) | ECSP15015022A (es) |
ES (1) | ES2632269T3 (es) |
GT (1) | GT201500093A (es) |
HK (1) | HK1213248A1 (es) |
HR (1) | HRP20171082T1 (es) |
HU (1) | HUE035335T2 (es) |
IL (1) | IL237866B (es) |
LT (1) | LT2909192T (es) |
ME (1) | ME02794B (es) |
MX (1) | MX358508B (es) |
MY (1) | MY189505A (es) |
NI (1) | NI201500053A (es) |
NZ (1) | NZ706775A (es) |
PE (1) | PE20150778A1 (es) |
PH (1) | PH12015500817A1 (es) |
PL (1) | PL2909192T3 (es) |
PT (1) | PT2909192T (es) |
RS (1) | RS56283B1 (es) |
SG (1) | SG11201502369XA (es) |
SI (1) | SI2909192T1 (es) |
TW (1) | TWI606045B (es) |
UY (1) | UY35084A (es) |
WO (1) | WO2014062658A1 (es) |
ZA (1) | ZA201503418B (es) |
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