ECSP13012437A - Inhibidores de la tirosina-quinasa de bruton - Google Patents
Inhibidores de la tirosina-quinasa de brutonInfo
- Publication number
- ECSP13012437A ECSP13012437A ECSP13012437A ECSP13012437A EC SP13012437 A ECSP13012437 A EC SP13012437A EC SP13012437 A ECSP13012437 A EC SP13012437A EC SP13012437 A ECSP13012437 A EC SP13012437A
- Authority
- EC
- Ecuador
- Prior art keywords
- btk
- compounds
- useful
- tirosina
- quinasa
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000000694 effects Effects 0.000 abstract 2
- GQGMIWXIWCELQB-UHFFFAOYSA-N 6-[2-(hydroxymethyl)phenyl]-2-methylpyridazin-3-one Chemical class C1=CC(=O)N(C)N=C1C1=CC=CC=C1CO GQGMIWXIWCELQB-UHFFFAOYSA-N 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 230000001594 aberrant effect Effects 0.000 abstract 1
- 210000003719 b-lymphocyte Anatomy 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Esta solicitud se refiere a derivados de la 6-(2-hidroximetil-fenil)-2-metil-2H-piridazin-3-ona que se ajustan a la fórmula general I:en la que las variables X, R e Y4 tienen los significados aquí definidos, que inhiben la Btk. 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 I y por lo menos un vehículo, diluyente o excipiente.
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 |
---|---|
ECSP13012437A true ECSP13012437A (es) | 2013-03-28 |
Family
ID=45565273
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ECSP13012437 ECSP13012437A (es) | 2010-08-12 | 2013-02-08 | Inhibidores de la tirosina-quinasa de bruton |
Country Status (20)
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) |
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 (63)
Publication number | Priority date | Publication date | Assignee | Title |
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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 |
SI2361250T1 (sl) | 2008-12-22 | 2013-12-31 | Merck Patent Gmbh | Nove polimorfne oblike 6-(1-metil-1h-pirazol-4-il)-2-(3-(5-(2-morfolin-4-il-etoksi)-pirimidin- 2-il)-benzil)-2h-piridazin-3-on dihidrogenfosfata in postopki za proizvodnjo le-tega |
EP2709997B1 (en) | 2011-05-17 | 2016-06-29 | F.Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
BR112014003582A2 (pt) * | 2011-08-17 | 2017-03-14 | Hoffmann La Roche | inibidores da tirosina quinase de bruton |
BR112014010391A2 (pt) | 2011-11-03 | 2017-04-18 | Hoffmann La Roche | composto, composição farmacêutica, processo de produção de uma composição farmacêutica, método de tratamento, kit e uso de uma composição farmacêutica |
UA111756C2 (uk) | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
CA2853967A1 (en) * | 2011-11-03 | 2013-05-10 | F. Hoffmann-La Roche Ag | 8-fluorophthalazin-1 (2h) -one compounds as inhibitors of btk activity |
AR088642A1 (es) | 2011-11-03 | 2014-06-25 | Genentech Inc | Compuestos de piperazina alquilados |
WO2013186159A1 (en) * | 2012-06-13 | 2013-12-19 | F. Hoffmann-La Roche Ag | New diazaspirocycloalkane and azaspirocycloalkane |
US10954567B2 (en) | 2012-07-24 | 2021-03-23 | Pharmacyclics Llc | Mutations associated with resistance to inhibitors of Bruton's Tyrosine Kinase (BTK) |
MA37830B1 (fr) | 2012-08-10 | 2018-09-28 | Boehringer Ingelheim Int | Composés hétéroromatiques en tant qu'inhibiteurs de la tyrosine kinase de bruton (btk) |
EP2895473A1 (en) * | 2012-09-13 | 2015-07-22 | F. Hoffmann-La Roche AG | Inhibitors of bruton's tyrosine kinase |
PE20150758A1 (es) | 2012-09-25 | 2015-05-15 | Hoffmann La Roche | Nuevos derivados biciclicos |
CA2890671A1 (en) * | 2012-11-16 | 2014-05-22 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
RU2015122218A (ru) * | 2012-11-30 | 2017-01-10 | Ф. Хоффманн-Ля Рош Аг | Ингибиторы тирозинкиназы брутона |
US9663494B2 (en) | 2013-03-05 | 2017-05-30 | Hoffmann-La Roche Inc. | Inhibitors of bruton's tyrosine kinase |
AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
MX367918B (es) | 2013-04-25 | 2019-09-11 | Beigene Ltd | Compuestos heterociclicos fusionados como inhibidores de proteina quinasa. |
CN104177338B (zh) * | 2013-05-22 | 2018-04-03 | 南京勇山生物科技有限公司 | 一类布鲁顿激酶抑制剂 |
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KR102130600B1 (ko) | 2014-07-03 | 2020-07-08 | 베이진 엘티디 | Pd-l1 항체와 이를 이용한 치료 및 진단 |
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WO2016209996A1 (en) | 2015-06-23 | 2016-12-29 | University Of Oregon | Phosphorus-containing heterocycles and a method for making and using |
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EP4353747A3 (en) | 2016-08-19 | 2024-06-26 | BeiGene Switzerland GmbH | Combination of zanubrutinib with an anti-cd20 or an anti-pd-1 antibody for use in treating cancer |
US20190201409A1 (en) | 2016-09-19 | 2019-07-04 | Mei Pharma, Inc. | Combination therapy |
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CN109438377B (zh) * | 2018-12-13 | 2020-06-09 | 天津利安隆新材料股份有限公司 | 一种低温法制备含有醚键的长碳链三嗪类紫外线吸收剂的方法 |
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EP2229390B1 (en) | 2007-12-14 | 2014-04-09 | F. Hoffmann-La Roche AG | Novel imidazoý1,2-a¨pyridine and imidazoý1,2-b¨pyridazine derivatives |
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RU2505538C2 (ru) * | 2008-02-05 | 2014-01-27 | Ф.Хоффманн-Ля Рош Аг | Новые пиридиноны и пиридазиноны |
US7741327B2 (en) | 2008-04-16 | 2010-06-22 | Hoffmann-La Roche Inc. | Pyrrolidinone glucokinase activators |
RU2500680C2 (ru) * | 2008-06-24 | 2013-12-10 | Ф.Хоффманн-Ля Рош Аг | Новые замещенные пиридин-2-оны и пиридазин-3-оны |
EP2300459B1 (en) * | 2008-07-02 | 2013-05-29 | F. Hoffmann-La Roche AG | Novel phenylpyrazinones as kinase inhibitors |
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EP2709997B1 (en) * | 2011-05-17 | 2016-06-29 | F.Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
-
2011
- 2011-08-08 AR ARP110102870A patent/AR082590A1/es unknown
- 2011-08-09 SG SG2013009246A patent/SG187747A1/en unknown
- 2011-08-09 JP JP2013523591A patent/JP5823518B2/ja not_active Expired - Fee Related
- 2011-08-09 EP EP11746518.7A patent/EP2603500B1/en not_active Not-in-force
- 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 MX MX2013001715A patent/MX2013001715A/es unknown
- 2011-08-09 KR KR1020137006162A patent/KR101546167B1/ko not_active Expired - Fee Related
- 2011-08-09 ES ES11746518.7T patent/ES2528371T3/es active Active
- 2011-08-09 MA MA35658A patent/MA34465B1/fr unknown
- 2011-08-09 EA EA201390207A patent/EA201390207A1/ru unknown
- 2011-08-09 AU AU2011288489A patent/AU2011288489A1/en not_active Abandoned
- 2011-08-09 CN CN201180048444.7A patent/CN103153984B/zh not_active Expired - Fee Related
- 2011-08-09 WO PCT/EP2011/063657 patent/WO2012020008A1/en active Application Filing
- 2011-08-09 PE PE2013000232A patent/PE20131153A1/es not_active Application Discontinuation
- 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 CL CL2013000391A patent/CL2013000391A1/es unknown
- 2013-02-08 EC ECSP13012437 patent/ECSP13012437A/es unknown
- 2013-03-01 US US13/781,815 patent/US8940741B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
CA2807634A1 (en) | 2012-02-16 |
KR101546167B1 (ko) | 2015-08-20 |
AR082590A1 (es) | 2012-12-19 |
EA201390207A1 (ru) | 2013-08-30 |
WO2012020008A1 (en) | 2012-02-16 |
ES2528371T3 (es) | 2015-02-09 |
AU2011288489A1 (en) | 2013-02-07 |
JP5823518B2 (ja) | 2015-11-25 |
PE20131153A1 (es) | 2013-10-05 |
US8940741B2 (en) | 2015-01-27 |
US8481540B2 (en) | 2013-07-09 |
CL2013000391A1 (es) | 2013-09-23 |
CN103153984B (zh) | 2015-04-22 |
US20130178461A1 (en) | 2013-07-11 |
CO6620025A2 (es) | 2013-02-15 |
EP2603500A1 (en) | 2013-06-19 |
BR112013003114A2 (pt) | 2016-06-28 |
SG187747A1 (en) | 2013-03-28 |
JP2013533300A (ja) | 2013-08-22 |
ZA201300705B (en) | 2014-06-25 |
HK1186186A1 (en) | 2014-03-07 |
MA34465B1 (fr) | 2013-08-01 |
US20120040949A1 (en) | 2012-02-16 |
CN103153984A (zh) | 2013-06-12 |
MX2013001715A (es) | 2013-03-22 |
KR20130038420A (ko) | 2013-04-17 |
EP2603500B1 (en) | 2014-11-19 |
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