AR082590A1 - Inhibidores de la tirosina-quinasa de bruton - Google Patents
Inhibidores de la tirosina-quinasa de brutonInfo
- Publication number
- AR082590A1 AR082590A1 ARP110102870A ARP110102870A AR082590A1 AR 082590 A1 AR082590 A1 AR 082590A1 AR P110102870 A ARP110102870 A AR P110102870A AR P110102870 A ARP110102870 A AR P110102870A AR 082590 A1 AR082590 A1 AR 082590A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- heterocycloalkyl
- cycloalkyl
- halogen
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61P11/04—Drugs for disorders of the respiratory system for throat disorders
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- C07D405/14—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Abstract
Los compuestos aquí descritos son útiles para modular la actividad de la Btk y para tratar enfermedades asociadas, con una actividad excesiva de la Btk. Los compuestos son también útiles para tratar enfermedades inflamatorias y autoinmunes asociadas con una proliferación aberrante de las células B, por ejemplo la artritis reumatoide. Se describen también composiciones que contienen los compuestos de la fórmula (1) y por lo menos un vehículo, diluyente o excipiente.Reivindicación 1: Un compuesto de la fórmula (1), en la que - - - - - es un enlace sencillo o un doble enlace; X es CH, CH2 o N; R es H, -R1, -R1-R2-R3, -R1-R3 o -R2-R3; R1 es arilo, heteroarilo, heteroarilo bicíclico, cicloalquilo o heterocicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, hidroxi, hidroxialquilo inferior, alcoxi inferior, halógeno, nitro, amino, amido, ciano, oxo o haloalquilo inferior; R2 es -C(=O), -C(=O)O, -C(=O)NR2’, -NHC(=O)O, -C(R2’)2, -O, -S, -C(=NH)NR2’ o -S(=O)2; cada R2’ es con independencia H o alquilo inferior; R3 es H o R4; R4 es alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, (alquilo inferior)-amino, cicloalquilamino, di(alquilo inferior)-amino, arilo, arilalquilo, alquilarilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, cicloalquilo, alquil-cicloalquilo, cicloalquil-alquilo, heterocicloalquilo, alquil-heterocicloalquilo, heterocicloalquil-alquilo, cicloalquilo bicíclico, heterocicloalquilo bicíclico, espirocicloalquilo, espiroheterocicloalquilo, o espiroheterocicloalquilo bicíclico, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, halógeno, (alquilo inferior)-amino, di(alquilo inferior)-amino, hidroxi, hidroxialquilo inferior, alcoxi inferior, alcanoílo inferior, halógeno, nitro, amino, amido, acilo, ciano, oxo, sulfonilo, alquilsulfonilo inferior, guanidino, hidroxil-amino, carboxi, carbamoílo, carbamato, haloalcoxi inferior, heterocicloalquilo o haloalquilo inferior; dos grupos alquilo inferior juntos pueden formar un anillo; Y4 es Y4a, Y4b, Y4c o Y4d; Y4a es H o halógeno; Y4b es alquilo inferior, opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por haloalquilo inferior, halógeno, hidroxi, amino, ciano y alcoxi inferior; Y4c es cicloalquilo inferior, opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por alquilo inferior, haloalquilo inferior, halógeno, hidroxi, amino, ciano y alcoxi inferior; y Y4d es amino, opcionalmente sustituido por uno o más alquilo inferior, alcoxi alquilo inferior o hidroxialquilo inferior; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US37288710P | 2010-08-12 | 2010-08-12 | |
US201161497093P | 2011-06-15 | 2011-06-15 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR082590A1 true AR082590A1 (es) | 2012-12-19 |
Family
ID=45565273
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110102870A AR082590A1 (es) | 2010-08-12 | 2011-08-08 | Inhibidores de la tirosina-quinasa de bruton |
Country Status (21)
Country | Link |
---|---|
US (2) | US8481540B2 (es) |
EP (1) | EP2603500B1 (es) |
JP (1) | JP5823518B2 (es) |
KR (1) | KR101546167B1 (es) |
CN (1) | CN103153984B (es) |
AR (1) | AR082590A1 (es) |
AU (1) | AU2011288489A1 (es) |
BR (1) | BR112013003114A2 (es) |
CA (1) | CA2807634A1 (es) |
CL (1) | CL2013000391A1 (es) |
CO (1) | CO6620025A2 (es) |
EA (1) | EA201390207A1 (es) |
EC (1) | ECSP13012437A (es) |
ES (1) | ES2528371T3 (es) |
HK (1) | HK1186186A1 (es) |
MA (1) | MA34465B1 (es) |
MX (1) | MX2013001715A (es) |
PE (1) | PE20131153A1 (es) |
SG (1) | SG187747A1 (es) |
WO (1) | WO2012020008A1 (es) |
ZA (1) | ZA201300705B (es) |
Families Citing this family (60)
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DE102007026341A1 (de) | 2007-06-06 | 2008-12-11 | Merck Patent Gmbh | Benzoxazolonderivate |
DE102007032507A1 (de) | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
DE102007038957A1 (de) * | 2007-08-17 | 2009-02-19 | Merck Patent Gmbh | 6-Thioxo-pyridazinderivate |
DE102007061963A1 (de) * | 2007-12-21 | 2009-06-25 | Merck Patent Gmbh | Pyridazinonderivate |
DE102008019907A1 (de) * | 2008-04-21 | 2009-10-22 | Merck Patent Gmbh | Pyridazinonderivate |
DE102008028905A1 (de) * | 2008-06-18 | 2009-12-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate |
DE102008037790A1 (de) * | 2008-08-14 | 2010-02-18 | Merck Patent Gmbh | Bicyclische Triazolderivate |
KR101663335B1 (ko) | 2008-12-22 | 2016-10-06 | 메르크 파텐트 게엠베하 | 6-(1-메틸-1h-피라졸-4-일)-2-{3-[5-(2-모르폴린-4-일-에톡시)-피리미딘-2-일]-벤질}-2h-피리다진-3-온디히드로겐포스페이트의 신규한 다형체 및 이의 제조 방법 |
MX345170B (es) | 2011-05-17 | 2017-01-19 | Hoffmann La Roche | Inhibidores de la tirosina-cinasa de bruton. |
KR20140052032A (ko) * | 2011-08-17 | 2014-05-02 | 에프. 호프만-라 로슈 아게 | 브루톤 티로신 키나아제의 억제제 |
EA027561B1 (ru) | 2011-11-03 | 2017-08-31 | Ф.Хоффманн-Ля Рош Аг | Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона |
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UA111756C2 (uk) | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
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PL2861566T3 (pl) | 2012-06-13 | 2017-06-30 | F.Hoffmann-La Roche Ag | Nowy diazaspirocykloalkan i azaspirocykloalkan |
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HUE045797T2 (hu) | 2012-09-25 | 2020-01-28 | Hoffmann La Roche | Hexahidropirrolo[3,4-c]pirrol-származékok és rokonvegyületek mint autotaxin (ATX) inhibitorok, valamint a lizofoszfatidsav (LPA) termelés inhibitorai, például vesebetegségek kezelésére |
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-
2011
- 2011-08-08 AR ARP110102870A patent/AR082590A1/es unknown
- 2011-08-09 EP EP11746518.7A patent/EP2603500B1/en not_active Not-in-force
- 2011-08-09 PE PE2013000232A patent/PE20131153A1/es not_active Application Discontinuation
- 2011-08-09 JP JP2013523591A patent/JP5823518B2/ja not_active Expired - Fee Related
- 2011-08-09 BR BR112013003114A patent/BR112013003114A2/pt active Search and Examination
- 2011-08-09 CA CA2807634A patent/CA2807634A1/en not_active Abandoned
- 2011-08-09 SG SG2013009246A patent/SG187747A1/en unknown
- 2011-08-09 AU AU2011288489A patent/AU2011288489A1/en not_active Abandoned
- 2011-08-09 WO PCT/EP2011/063657 patent/WO2012020008A1/en active Application Filing
- 2011-08-09 CN CN201180048444.7A patent/CN103153984B/zh not_active Expired - Fee Related
- 2011-08-09 ES ES11746518.7T patent/ES2528371T3/es active Active
- 2011-08-09 MX MX2013001715A patent/MX2013001715A/es unknown
- 2011-08-09 MA MA35658A patent/MA34465B1/fr unknown
- 2011-08-09 EA EA201390207A patent/EA201390207A1/ru unknown
- 2011-08-09 KR KR1020137006162A patent/KR101546167B1/ko not_active IP Right Cessation
- 2011-08-11 US US13/207,481 patent/US8481540B2/en not_active Expired - Fee Related
-
2013
- 2013-01-25 ZA ZA2013/00705A patent/ZA201300705B/en unknown
- 2013-01-31 CO CO13018558A patent/CO6620025A2/es not_active Application Discontinuation
- 2013-02-08 EC ECSP13012437 patent/ECSP13012437A/es unknown
- 2013-02-08 CL CL2013000391A patent/CL2013000391A1/es unknown
- 2013-03-01 US US13/781,815 patent/US8940741B2/en not_active Expired - Fee Related
- 2013-12-10 HK HK13113723.2A patent/HK1186186A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
BR112013003114A2 (pt) | 2016-06-28 |
CO6620025A2 (es) | 2013-02-15 |
AU2011288489A1 (en) | 2013-02-07 |
CA2807634A1 (en) | 2012-02-16 |
MX2013001715A (es) | 2013-03-22 |
ECSP13012437A (es) | 2013-03-28 |
MA34465B1 (fr) | 2013-08-01 |
US20130178461A1 (en) | 2013-07-11 |
US8940741B2 (en) | 2015-01-27 |
US20120040949A1 (en) | 2012-02-16 |
JP2013533300A (ja) | 2013-08-22 |
KR20130038420A (ko) | 2013-04-17 |
SG187747A1 (en) | 2013-03-28 |
JP5823518B2 (ja) | 2015-11-25 |
CN103153984A (zh) | 2013-06-12 |
EA201390207A1 (ru) | 2013-08-30 |
HK1186186A1 (en) | 2014-03-07 |
PE20131153A1 (es) | 2013-10-05 |
ES2528371T3 (es) | 2015-02-09 |
US8481540B2 (en) | 2013-07-09 |
KR101546167B1 (ko) | 2015-08-20 |
EP2603500B1 (en) | 2014-11-19 |
WO2012020008A1 (en) | 2012-02-16 |
EP2603500A1 (en) | 2013-06-19 |
CL2013000391A1 (es) | 2013-09-23 |
ZA201300705B (en) | 2014-06-25 |
CN103153984B (zh) | 2015-04-22 |
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