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
-
- 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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
WO2010072295A1 (en) | 2008-12-22 | 2010-07-01 | Merck Patent Gmbh | Novel polymorphic forms of 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof |
AU2012257802A1 (en) | 2011-05-17 | 2013-10-31 | F. Hoffmann-La Roche Ag | Inhibitors of Bruton's tyrosine kinase |
TW201311669A (zh) * | 2011-08-17 | 2013-03-16 | Hoffmann La Roche | 布魯頓氏酪胺酸激酶(bruton’s tyrosine kinase)之抑制劑 |
AR088643A1 (es) | 2011-11-03 | 2014-06-25 | Genentech Inc | Compuestos de 8-fluoroftalazin-1(2h)-ona |
KR101716011B1 (ko) | 2011-11-03 | 2017-03-13 | 에프. 호프만-라 로슈 아게 | Btk 활성의 억제제인 알킬화된 피페라진 화합물 |
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 |
IN2014DN09346A (es) * | 2012-06-13 | 2015-07-17 | Hoffmann La Roche | |
MX2015001081A (es) | 2012-07-24 | 2015-10-14 | Pharmacyclics Inc | Mutaciones asociadas a resistencia a inhibidores de la tirosina cinasa de bruton (btk). |
SG11201500499TA (en) | 2012-08-10 | 2015-03-30 | Boehringer Ingelheim Int | Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors |
KR20150054994A (ko) * | 2012-09-13 | 2015-05-20 | 에프. 호프만-라 로슈 아게 | 브루톤 티로신 키나아제의 억제제 |
ES2753163T3 (es) | 2012-09-25 | 2020-04-07 | Hoffmann La Roche | Derivados de hexahidropirrolo[3,4-c]pirrol y compuestos relacionados como inhibidores de la autotaxina (ATX) y como inhibidores de la producción de ácido lisofosfatídico (LPA) para tratar, por ejemplo, enfermedades renales |
JP6088063B2 (ja) * | 2012-11-16 | 2017-03-01 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | ブルトン型チロシンキナーゼの阻害剤 |
CN104968346B (zh) * | 2012-11-30 | 2017-06-27 | 弗·哈夫曼-拉罗切有限公司 | 酪氨酸蛋白激酶抑制剂 |
WO2014135474A1 (en) | 2013-03-05 | 2014-09-12 | F. Hoffmann-La Roche Ag | 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 |
PL2989106T3 (pl) | 2013-04-25 | 2017-08-31 | Beigene, Ltd. | Połączone związki heterocykliczne jako inhibitory kinazy białkowej |
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 |
EP3016943B1 (en) * | 2013-07-03 | 2019-08-21 | F. Hoffmann-La Roche AG | Heteroaryl pyridone and aza-pyridone amide compounds |
KR102100419B1 (ko) | 2013-09-13 | 2020-04-14 | 베이진 스위찰랜드 게엠베하 | 항-pd1 항체 및 이의 치료 및 진단 용도 |
WO2015082583A1 (en) | 2013-12-05 | 2015-06-11 | F. Hoffmann-La Roche Ag | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
US9802920B2 (en) | 2013-12-13 | 2017-10-31 | Hoffman-La Roche Inc. | Inhibitors of bruton's tyrosine kinase |
CA2942204A1 (en) | 2014-03-12 | 2015-09-17 | Novartis Ag | Combination comprising a btk inhibitor and an akt inhibitor |
JP6554481B2 (ja) | 2014-03-26 | 2019-07-31 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | オートタキシン(atx)及びリゾホスファチジン酸(lpa)産生の阻害剤としての縮合[1,4]ジアゼピン化合物 |
PL3122750T3 (pl) | 2014-03-26 | 2020-03-31 | F.Hoffmann-La Roche Ag | Związki bicykliczne jako inhibitory wytwarzania autotaksyny (ATX) i kwasu lizofosfatydowego (LPA) |
US9982265B2 (en) * | 2014-03-28 | 2018-05-29 | Board Of Regents, The University Of Texas System | Inhibition of Bruton's tyrosine kinase (Btk) in the lung to treat severe lung inflammation and lung injury |
CN106604742B (zh) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
WO2016209996A1 (en) | 2015-06-23 | 2016-12-29 | University Of Oregon | Phosphorus-containing heterocycles and a method for making and using |
MX2020004504A (es) | 2015-09-04 | 2021-11-10 | Hoffmann La Roche | Derivados de fenoximetilo. |
CN107614505B (zh) | 2015-09-24 | 2021-05-07 | 豪夫迈·罗氏有限公司 | 作为双重atx/ca抑制剂的新型二环化合物 |
CA2991615A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | Bicyclic compounds as atx inhibitors |
AU2016328436B2 (en) | 2015-09-24 | 2020-05-14 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
KR20180054830A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 억제제로서의 이환형 화합물 |
WO2018007885A1 (en) | 2016-07-05 | 2018-01-11 | Beigene, Ltd. | COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER |
CN116478166A (zh) | 2016-08-16 | 2023-07-25 | 百济神州(苏州)生物科技有限公司 | 一种化合物的晶型、其制备和用途 |
AU2017313085A1 (en) | 2016-08-19 | 2019-03-14 | Beigene Switzerland Gmbh | Use of a combination comprising a Btk inhibitor for treating cancers |
MX2019003134A (es) | 2016-09-19 | 2019-08-29 | Mei Pharma Inc | Terapia de combinacion. |
EP3573989A4 (en) | 2017-01-25 | 2020-11-18 | Beigene, Ltd. | CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) -PIPERIDINE-4-YL) -2- (4-PHENOXYPHENYL) -4,5,6,7-TETRAHYDROPYRAZOLO [1,5-A ] PYRIMIDINE-3-CARBOXAMIDE, MANUFACTURING AND USES THEREOF |
EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
AU2018233079B9 (en) | 2017-03-16 | 2021-07-22 | F. Hoffmann-La Roche Ag | Heterocyclic compounds useful as dual ATX/CA inhibitors |
EP3645569A4 (en) | 2017-06-26 | 2021-03-24 | BeiGene, Ltd. | IMMUNOTHERAPY FOR LIVER CELL CARCINOMA |
WO2019034009A1 (en) | 2017-08-12 | 2019-02-21 | Beigene, Ltd. | BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY |
TWI694995B (zh) * | 2017-11-06 | 2020-06-01 | 美商美國禮來大藥廠 | Btk抑制劑化合物 |
US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
CA3115526A1 (en) | 2018-10-15 | 2020-04-23 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
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 |
EP3953346A1 (en) | 2019-04-09 | 2022-02-16 | Nurix Therapeutics, Inc. | 3-substituted piperidine compounds for cbl-b inhibition, and use of a cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus |
EP3969447A1 (en) | 2019-05-17 | 2022-03-23 | Nurix Therapeutics, Inc. | Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof |
US20230024442A1 (en) * | 2019-11-08 | 2023-01-26 | Nurix Therapeutics, Inc. | Bifunctional compounds for grading btk via ubiquitin proteosome pathway |
CA3160368A1 (en) * | 2019-12-04 | 2021-06-10 | Henan Zhiwei Biomedicine Co., Ltd. | Substituted imidazolecarboxamide as bruton's tyrosine kinase inhibitors |
JP2023504147A (ja) | 2019-12-04 | 2023-02-01 | ニューリックス セラピューティクス,インコーポレイテッド | ユビキチンプロテオソーム経路を介したbtkの分解のための二官能性化合物 |
US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
Family Cites Families (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7312341B2 (en) | 2002-09-09 | 2007-12-25 | Cgi Pharmaceuticals, Inc. | 6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof |
PE20040801A1 (es) | 2002-12-12 | 2004-11-25 | Hoffmann La Roche | Derivados de pirazina y piridina 5-sustituidos como activadores de glucoquinasa |
US7405295B2 (en) | 2003-06-04 | 2008-07-29 | Cgi Pharmaceuticals, Inc. | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds |
TW200716551A (en) | 2005-03-10 | 2007-05-01 | Cgi Pharmaceuticals Inc | Certain substituted amides, method of making, and method of use thereof |
WO2006124731A2 (en) | 2005-05-12 | 2006-11-23 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
BRPI0614804A2 (pt) | 2005-08-09 | 2011-04-12 | Irm Llc | compostos e composições como inibidores de proteìna cinase |
EP1919906B1 (en) | 2005-08-29 | 2011-10-12 | Vertex Pharmaceuticals Incorporated | 3, 5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases |
AU2006285145A1 (en) | 2005-08-29 | 2007-03-08 | Vertex Pharmaceuticals Incorporated | 3,5-disubstituted pyrid-2-ones useful as inhibitors of Tec family of non-.receptor tyrosine kinases |
EP1919891B1 (en) | 2005-08-29 | 2012-03-07 | Vertex Pharmaceuticals Incorporated | 3,5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases |
CA2650611A1 (en) | 2006-05-15 | 2007-11-29 | Irm Llc | Compositions and methods for fgf receptor kinases inhibitors |
RU2009105818A (ru) | 2006-07-24 | 2010-08-27 | Ф.Хоффманн-Ля Рош Аг (Ch) | Пиразолы в качестве активаторов глюкокиназы |
PE20081370A1 (es) | 2006-09-11 | 2008-11-28 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas |
PE20080839A1 (es) | 2006-09-11 | 2008-08-23 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas |
US7838523B2 (en) | 2006-09-11 | 2010-11-23 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
WO2008033858A2 (en) | 2006-09-11 | 2008-03-20 | Cgi Pharmaceuticals, Inc. | Kinase inhibitors, and methods of using and identifying kinase inhibitors |
SG185330A1 (en) * | 2007-10-23 | 2012-11-29 | Hoffmann La Roche | Novel kinase inhibitors |
ES2462642T3 (es) | 2007-12-14 | 2014-05-26 | F. Hoffmann-La Roche Ag | Nuevos derivados de imidazo[1,2-a]piridina e imidazo[1,2-b]piridazina |
US7683064B2 (en) * | 2008-02-05 | 2010-03-23 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
EP2242749B1 (en) * | 2008-02-05 | 2013-04-10 | F. Hoffmann-La Roche AG | Novel pyridinones and pyridazinones |
US7741327B2 (en) | 2008-04-16 | 2010-06-22 | Hoffmann-La Roche Inc. | Pyrrolidinone glucokinase activators |
JP5536049B2 (ja) * | 2008-06-24 | 2014-07-02 | エフ.ホフマン−ラ ロシュ アーゲー | 新規な置換ピリジン−2−オン及びピリダジン−3−オン |
PT2300459E (pt) * | 2008-07-02 | 2013-07-04 | Hoffmann La Roche | Novas fenilpirazinonas utilizadas como inibidores de cinase |
US8299077B2 (en) * | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
WO2010122038A1 (en) * | 2009-04-24 | 2010-10-28 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
JP5842004B2 (ja) * | 2010-09-01 | 2016-01-13 | ジーアイリード コネチカット インコーポレーテッドGilead Connecticut,Inc. | ピリダジノン、その製造方法及びその使用方法 |
AU2012257802A1 (en) * | 2011-05-17 | 2013-10-31 | F. Hoffmann-La Roche Ag | Inhibitors of Bruton's tyrosine kinase |
-
2011
- 2011-08-08 AR ARP110102870A patent/AR082590A1/es unknown
- 2011-08-09 KR KR1020137006162A patent/KR101546167B1/ko not_active IP Right Cessation
- 2011-08-09 PE PE2013000232A patent/PE20131153A1/es not_active Application Discontinuation
- 2011-08-09 AU AU2011288489A patent/AU2011288489A1/en not_active Abandoned
- 2011-08-09 CA CA2807634A patent/CA2807634A1/en not_active Abandoned
- 2011-08-09 ES ES11746518.7T patent/ES2528371T3/es active Active
- 2011-08-09 CN CN201180048444.7A patent/CN103153984B/zh not_active Expired - Fee Related
- 2011-08-09 EP EP11746518.7A patent/EP2603500B1/en not_active Not-in-force
- 2011-08-09 MX MX2013001715A patent/MX2013001715A/es unknown
- 2011-08-09 JP JP2013523591A patent/JP5823518B2/ja not_active Expired - Fee Related
- 2011-08-09 WO PCT/EP2011/063657 patent/WO2012020008A1/en active Application Filing
- 2011-08-09 MA MA35658A patent/MA34465B1/fr unknown
- 2011-08-09 SG SG2013009246A patent/SG187747A1/en unknown
- 2011-08-09 EA EA201390207A patent/EA201390207A1/ru unknown
- 2011-08-09 BR BR112013003114A patent/BR112013003114A2/pt active Search and Examination
- 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 |
---|---|
WO2012020008A1 (en) | 2012-02-16 |
EP2603500B1 (en) | 2014-11-19 |
AU2011288489A1 (en) | 2013-02-07 |
PE20131153A1 (es) | 2013-10-05 |
CO6620025A2 (es) | 2013-02-15 |
CA2807634A1 (en) | 2012-02-16 |
ZA201300705B (en) | 2014-06-25 |
ES2528371T3 (es) | 2015-02-09 |
US8481540B2 (en) | 2013-07-09 |
ECSP13012437A (es) | 2013-03-28 |
CN103153984B (zh) | 2015-04-22 |
KR101546167B1 (ko) | 2015-08-20 |
US20130178461A1 (en) | 2013-07-11 |
MX2013001715A (es) | 2013-03-22 |
US20120040949A1 (en) | 2012-02-16 |
EA201390207A1 (ru) | 2013-08-30 |
BR112013003114A2 (pt) | 2016-06-28 |
SG187747A1 (en) | 2013-03-28 |
KR20130038420A (ko) | 2013-04-17 |
JP5823518B2 (ja) | 2015-11-25 |
MA34465B1 (fr) | 2013-08-01 |
CN103153984A (zh) | 2013-06-12 |
HK1186186A1 (en) | 2014-03-07 |
JP2013533300A (ja) | 2013-08-22 |
CL2013000391A1 (es) | 2013-09-23 |
EP2603500A1 (en) | 2013-06-19 |
US8940741B2 (en) | 2015-01-27 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR082590A1 (es) | Inhibidores de la tirosina-quinasa de bruton | |
AR086403A1 (es) | Inhibidores de la tirosina-quinasa de bruton | |
AR092536A1 (es) | Inhibidores de la tirosina-quinasa de bruton | |
AR087543A1 (es) | Inhibidores de la tirosina-quinasa de bruton | |
AR072545A1 (es) | Fenilpirazinonas como inhibidores de la btk, composicion farmaceutica que las contiene y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades autoinmunes e inflamatorias. | |
AR076066A1 (es) | Inhibidores de la tirosina-quinasa de bruton | |
AR070408A1 (es) | Piridinonas y piridazinonas | |
RU2348617C2 (ru) | Производные 2-пиридона в качестве ингибиторов эластазы нейтрофилов и их применение | |
AR052903A1 (es) | Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno. | |
PE20040164A1 (es) | Mimeticos de glucocorticoides, procedimientos para su preparacion y composiciones farmaceuticas | |
AR048789A1 (es) | Derivados de oxazol y sus composiciones como moduladores de receptor activado de proliferador de peroxisoma (ppar) | |
AR058362A1 (es) | Derivados de isoquinolina - aminopirazol su obtencion y su utilizacion como agentes farmaceuticos | |
AR074459A1 (es) | Pirrolopirazinil-ureas utiles para el tratamiento de enfermedades autoinmunes e inflamatorias. | |
AR072272A1 (es) | Piridin-2-onas y piridazin-3-onas sustituidas utiles para el tratamiento de enfermedades autoinmunes e inflamatorias causadas por una activacion aberrante de las celulas b, y composiciones farmaceuticas que las contienen. | |
AR046297A1 (es) | Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo | |
PE20061164A1 (es) | Piperazin-piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3 | |
AR066669A1 (es) | Derivados de imidazolona como inhibidores de bencimidazolona quimasa. composiciones farmaceuticas. | |
PE20142081A1 (es) | Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos | |
AR061419A1 (es) | Compuestos de piridil amida sustituidos como moduladores del receptor de histamida h3 | |
EA200801828A3 (ru) | Соединения 1,2,4,5- тетрагидро-3н-бензазепина, способ их получения и фармацевтические композиции, содержащие эти соединения | |
AR065583A1 (es) | Compuestos macrociclicos y composicion farmaceutica | |
AR057063A1 (es) | Moduladores de tienopirimidina y tienopiridina quinasa y composicion farmaceutica | |
AR072793A1 (es) | Compuestos de aril isoxazol con actividades antitumorales | |
AR093123A1 (es) | Inhibidores de la tirosina-quinasa de bruton | |
CO5650231A2 (es) | Derivados de 1-(alquilaminoalquil-pirrolidin-/piperidinil)-2,2-difenilacetamida como antagonistas del receptor muscarinico, su procedimiento de sintesis y composiciones farmaceuticas que los contienen |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |