AR069666A1 - Derivados de imidazo[1, 2 - a]piridina e imidazo[1, 2 -b]piridazina, una composicion farmaceutica que los contiene y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por las celulas b. - Google Patents
Derivados de imidazo[1, 2 - a]piridina e imidazo[1, 2 -b]piridazina, una composicion farmaceutica que los contiene y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por las celulas b.Info
- Publication number
- AR069666A1 AR069666A1 ARP080105399A ARP080105399A AR069666A1 AR 069666 A1 AR069666 A1 AR 069666A1 AR P080105399 A ARP080105399 A AR P080105399A AR P080105399 A ARP080105399 A AR P080105399A AR 069666 A1 AR069666 A1 AR 069666A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- heterocycloalkyl
- heteroaryl
- lower alkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
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- 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
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
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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]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Los derivados de imidazo[1,2-a]piridina e imidazo[1,2-b]piridazina inhiben la Btk y son utiles para el tratamiento de enfermedades autoinmunes e inflamatorias, provocadas por la activacion aberrante de las células B, p.ej. la artritis. Reivindicacion 1: Un compuesto de la formula (1) en la que Z es carbono o nitrogeno, R* es H, -R1, -R1-R2-R3, -R1-R3 o -R2-R3; en los que: R1 es arilo, heteroarilo, cicloalquilo o heterocicloalquilo, y está opcionalmente sustituido por alquilo inferior, hidroxi, alcoxi inferior, halogeno, nitro, amino, ciano o halo-alquilo inferior; R2 es -C(=O), -C(=O)O, -C(=O)NH, -S(=O)2, O, NR3 o alquilo inferior; R3 es H o R4; R4 es alquilo inferior, alcoxi inferior, arilo, arilalquilo, alquilarilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, cicloalquilo, alquil-cicloalquilo, cicloalquil-alquilo, heterocicloalquilo, alquil-heterocicloalquilo o heterocicloalquil-alquilo, y está opcionalmente sustituido por alquilo inferior, hidroxi, alcoxi inferior, halogeno, nitro, amino, ciano, alquilo inferior-sulfonilo, heterocicloalquilo o halo-alquilo inferior; R** es un grupo de la formula (2) o (3); Q es pirrolilo, cicloalquilo o cicloalquenilo; X es H, halogeno, alquilo inferior, hidroxi, hidroxi-alquilo inferior o alcoxi inferior; Y es H, -R5-R6, -R6 o -R5-R6-R7; R5 es -NHC(=O) , -NHC(=O)NR5', -(CH2)nC(=O)NR5', -NH o -(CH2)n-C(=O); en el que n es el numero 0, 1 o 2; y R5' es H, alquilo inferior, alcoxi inferior o hidroxi-alquilo inferior; R6 es alquilo inferior, alquenilo inferior, alquinilo inferior, arilo, arilalquilo, alquilarilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, cicloalquilo, alquil-cicloalquilo, cicloalquil-alquilo, heterocicloalquilo, alquil-heterocicloalquilo o heterocicloalquil-alquilo y está opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por alquilo inferior, hidroxi, halo-alquilo inferior, alcoxi inferior, halo-alcoxi inferior, halogeno, nitro, amino, amido, amido-alquilo inferior, ciano y trialquilsilanilo; y R7 es arilo, heteroarilo, cicloalquilo o heterocicloalquilo, opcionalmente sustituidos por uno o más sustituyentes elegidos entre el grupo formado por alquilo inferior, hidroxi, halo-alquilo inferior, alcoxi inferior, halo-alcoxi inferior, halogeno, nitro, amino, oxo, ciano y trialquilsilanilo, o está opcionalmente conectado a un anillo arilo, heteroarilo, cicloalquilo o heterocicloalquilo, de modo que los dos anillos formen un sistema de anillos fusionados bicíclico espirocíclico, opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por alquilo inferior, hidroxi, halo-alquilo inferior, alcoxi inferior, halo-alcoxi inferior, halogeno, nitro, amino, oxo, ciano y trialquilsilanilo; con la condicion de que si Z es carbono, R* es C(=O)CH3 y R** es un grupo I** en el que X es H, entonces Y no sea CF3 ni H; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US1376207P | 2007-12-14 | 2007-12-14 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR069666A1 true AR069666A1 (es) | 2010-02-10 |
Family
ID=40428199
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP080105399A AR069666A1 (es) | 2007-12-14 | 2008-12-12 | Derivados de imidazo[1, 2 - a]piridina e imidazo[1, 2 -b]piridazina, una composicion farmaceutica que los contiene y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por las celulas b. |
Country Status (10)
Country | Link |
---|---|
EP (1) | EP2229390B1 (es) |
JP (2) | JP5643105B2 (es) |
CN (1) | CN101952283B (es) |
AR (1) | AR069666A1 (es) |
CA (1) | CA2708361C (es) |
CL (1) | CL2008003698A1 (es) |
ES (1) | ES2462642T3 (es) |
PE (1) | PE20091085A1 (es) |
TW (1) | TW200930720A (es) |
WO (1) | WO2009077334A1 (es) |
Families Citing this family (50)
Publication number | Priority date | Publication date | Assignee | Title |
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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 |
NZ587039A (en) | 2008-02-13 | 2013-01-25 | Gilead Connecticut Inc | 6-aryl-imidazo[1, 2-a]pyrazine derivatives, method of making, and method of use thereof |
ATE517107T1 (de) | 2008-02-25 | 2011-08-15 | Hoffmann La Roche | Pyrrolopyrazinkinaseinhibitoren |
CN103408533B (zh) | 2008-06-24 | 2015-08-26 | 霍夫曼-拉罗奇有限公司 | 新型取代的吡啶-2-酮和哒嗪-3-酮 |
WO2010006947A1 (en) | 2008-07-15 | 2010-01-21 | F. Hoffmann-La Roche Ag | Novel phenyl-imidazopyridines and pyridazines |
EP2307418B1 (en) * | 2008-07-18 | 2014-03-12 | F.Hoffmann-La Roche Ag | Novel phenylimidazopyrazines |
EP3123864A1 (en) | 2008-12-08 | 2017-02-01 | Gilead Connecticut, Inc. | Imidazopyrazine syk inhibitors |
AU2009325133B2 (en) | 2008-12-08 | 2016-02-04 | Gilead Connecticut, Inc. | Imidazopyrazine Syk inhibitors |
US8450321B2 (en) | 2008-12-08 | 2013-05-28 | Gilead Connecticut, Inc. | 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor |
US8299077B2 (en) | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
WO2011051342A1 (en) | 2009-10-30 | 2011-05-05 | Janssen Pharmaceutica Nv | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
AU2011226689B2 (en) * | 2010-03-11 | 2016-09-01 | Kronos Bio, Inc. | Imidazopyridines Syk inhibitors |
AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
BR112013033375B1 (pt) | 2011-06-27 | 2022-05-10 | Janssen Pharmaceutica N.V | Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário |
KR20140058543A (ko) | 2011-07-08 | 2014-05-14 | 노파르티스 아게 | 신규 피롤로 피리미딘 유도체 |
JP6173327B2 (ja) * | 2011-11-01 | 2017-08-02 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | イミダゾピリダジン化合物 |
ES2552514T3 (es) * | 2011-11-03 | 2015-11-30 | Hoffmann-La Roche Ag | Compuestos bicíclicos de piperazina |
RU2627661C2 (ru) | 2012-01-10 | 2017-08-09 | Ф. Хоффманн-Ля Рош Аг | Соединения пиридазинамида и их применение в качестве ингибиторов тирозинкиназы селезенки (syk) |
US9365566B2 (en) | 2012-03-27 | 2016-06-14 | Takeda Pharmaceutical Company Limited | Cinnoline derivatives |
AU2013283426B2 (en) | 2012-06-26 | 2018-02-22 | Janssen Pharmaceutica Nv | Combinations comprising PDE 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and PDE 10 inhibitors for use in the treatment of neurological or metabolic disorders |
CN104411314B (zh) | 2012-07-09 | 2017-10-20 | 詹森药业有限公司 | 磷酸二酯酶10的抑制剂 |
JO3377B1 (ar) | 2013-03-11 | 2019-03-13 | Takeda Pharmaceuticals Co | مشتقات بيريدينيل وبيريدينيل مندمج |
EP2989106B1 (en) | 2013-04-25 | 2016-12-14 | Beigene, Ltd. | Fused heterocyclic compounds as protein kinase inhibitors |
KR101810798B1 (ko) | 2013-07-30 | 2017-12-19 | 질레드 코네티컷 인코포레이티드 | Syk 억제제의 다형체 |
UA115815C2 (uk) | 2013-07-30 | 2017-12-26 | Гіліад Коннектікут, Інк. | Склад на основі інгібіторів syk |
CN103360399B (zh) * | 2013-08-02 | 2016-03-02 | 北京大学 | 6-芳基取代-咪唑-[1,2-b]哒嗪类衍生物,其制备方法及用途 |
JP6623353B2 (ja) | 2013-09-13 | 2019-12-25 | ベイジーン スウィッツァーランド ゲーエムベーハー | 抗pd−1抗体並びにその治療及び診断のための使用 |
MX2016007311A (es) | 2013-12-04 | 2016-09-07 | Gilead Sciences Inc | Metodos para tratar canceres. |
US9290505B2 (en) | 2013-12-23 | 2016-03-22 | Gilead Sciences, Inc. | Substituted imidazo[1,2-a]pyrazines as Syk inhibitors |
TWI662037B (zh) | 2013-12-23 | 2019-06-11 | 美商基利科學股份有限公司 | 脾酪胺酸激酶抑制劑 |
WO2015157955A1 (en) * | 2014-04-17 | 2015-10-22 | Abbvie Inc. | Heterocyclic btk inhibit ors |
KR102130600B1 (ko) | 2014-07-03 | 2020-07-08 | 베이진 엘티디 | Pd-l1 항체와 이를 이용한 치료 및 진단 |
NZ726365A (en) | 2014-07-14 | 2018-06-29 | Gilead Sciences Inc | Combinations for treating cancers |
EP3124479A1 (en) * | 2015-07-29 | 2017-02-01 | Solvay SA | Method for the manufacture of fluorinated cyclic carbonates |
CN105418615B (zh) * | 2015-12-09 | 2018-02-02 | 北京工业大学 | 苯甲酰胺衍生物及制备和应用 |
EP3436447B1 (en) | 2016-03-31 | 2021-07-14 | Takeda Pharmaceutical Company Limited | Isoquinolinyl triazolone complexes |
CN109475536B (zh) | 2016-07-05 | 2022-05-27 | 百济神州有限公司 | 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合 |
IL293319A (en) | 2016-08-16 | 2022-07-01 | Beigene Ltd | Crystal structure of s)-7-(1-acryloylpiperidin-4-yl)-2-(4-)phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo(1,5-a)pyrimidine-3-carboxamide , preparation methods and its uses |
US11701357B2 (en) | 2016-08-19 | 2023-07-18 | Beigene Switzerland Gmbh | Treatment of B cell cancers using a combination comprising Btk inhibitors |
KR20190058550A (ko) | 2016-09-19 | 2019-05-29 | 메이 파마, 아이엔씨. | 병용 요법 |
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 |
BR112019021992A2 (pt) | 2017-04-21 | 2020-06-09 | Kyn Therapeutics | inibidores de ahr de indol e usos dos mesmos |
CN110799543A (zh) | 2017-06-26 | 2020-02-14 | 百济神州有限公司 | 肝细胞癌的免疫治疗 |
WO2019034009A1 (en) | 2017-08-12 | 2019-02-21 | Beigene, Ltd. | BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY |
AU2018321264A1 (en) | 2017-08-25 | 2020-02-27 | Kronos Bio, Inc. | Polymorphs of Syk inhibitors |
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 |
CA3130848A1 (en) | 2019-02-22 | 2020-08-27 | Kronos Bio, Inc. | Solid forms of condensed pyrazines as syk inhibitors |
AU2020394424A1 (en) | 2019-11-26 | 2022-06-16 | Ikena Oncology, Inc. | Polymorphic carbazole derivatives and uses thereof |
US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
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WO1998054093A1 (en) * | 1997-05-30 | 1998-12-03 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
US7067520B2 (en) * | 2000-11-17 | 2006-06-27 | Ishihara Sangyo Kaisha, Ltd. | Preventive or therapeutic medicines for diabetes containing fused-heterocyclic compounds or their salts |
EP1539756B1 (en) * | 2002-09-19 | 2007-11-14 | Schering Corporation | Imidazopyridines as cyclin dependent kinase inhibitors |
CA2587192A1 (en) * | 2004-11-10 | 2006-05-18 | Cgi Pharmaceuticals, Inc. | Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity |
TW200700064A (en) * | 2005-03-24 | 2007-01-01 | Glaxo Group Ltd | Novel compounds |
EP1931676B1 (en) | 2005-10-06 | 2011-11-16 | Schering Corporation | Pyrazolopyrimidines as protein 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 |
-
2008
- 2008-12-04 ES ES08861971.3T patent/ES2462642T3/es active Active
- 2008-12-04 CA CA2708361A patent/CA2708361C/en not_active Expired - Fee Related
- 2008-12-04 CN CN2008801206432A patent/CN101952283B/zh not_active Expired - Fee Related
- 2008-12-04 EP EP08861971.3A patent/EP2229390B1/en not_active Not-in-force
- 2008-12-04 JP JP2010537386A patent/JP5643105B2/ja not_active Expired - Fee Related
- 2008-12-04 WO PCT/EP2008/066758 patent/WO2009077334A1/en active Application Filing
- 2008-12-11 TW TW097148307A patent/TW200930720A/zh unknown
- 2008-12-11 PE PE2008002052A patent/PE20091085A1/es not_active Application Discontinuation
- 2008-12-12 AR ARP080105399A patent/AR069666A1/es unknown
- 2008-12-12 CL CL2008003698A patent/CL2008003698A1/es unknown
-
2014
- 2014-06-04 JP JP2014116005A patent/JP5871992B2/ja not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
JP5643105B2 (ja) | 2014-12-17 |
CA2708361C (en) | 2016-06-07 |
EP2229390B1 (en) | 2014-04-09 |
PE20091085A1 (es) | 2009-07-23 |
EP2229390A1 (en) | 2010-09-22 |
CA2708361A1 (en) | 2009-06-25 |
CN101952283B (zh) | 2013-04-17 |
ES2462642T3 (es) | 2014-05-26 |
JP2014196316A (ja) | 2014-10-16 |
TW200930720A (en) | 2009-07-16 |
CL2008003698A1 (es) | 2010-02-19 |
WO2009077334A1 (en) | 2009-06-25 |
JP2011506378A (ja) | 2011-03-03 |
JP5871992B2 (ja) | 2016-03-01 |
CN101952283A (zh) | 2011-01-19 |
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