[go: up one dir, main page]
More Web Proxy on the site http://driver.im/

AR086403A1 - Inhibidores de la tirosina-quinasa de bruton - Google Patents

Inhibidores de la tirosina-quinasa de bruton

Info

Publication number
AR086403A1
AR086403A1 ARP120101712A ARP120101712A AR086403A1 AR 086403 A1 AR086403 A1 AR 086403A1 AR P120101712 A ARP120101712 A AR P120101712A AR P120101712 A ARP120101712 A AR P120101712A AR 086403 A1 AR086403 A1 AR 086403A1
Authority
AR
Argentina
Prior art keywords
alkyl
amino
lower alkyl
halogen
heterocycloalkyl
Prior art date
Application number
ARP120101712A
Other languages
English (en)
Inventor
Roland J Billedeau
Rama K Kondru
Francisco Javier Lopez-Tapia
Yan Lou
Timothy D Owens
Yimin Qian
Sung So
Kshitij Chhabilbhai Sau-Thakkar
Jutta Wanner
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR086403A1 publication Critical patent/AR086403A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/02—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
    • C07D401/10—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 aromatic rings
    • 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
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/10—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 two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/10—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 two hetero rings linked by a carbon chain containing aromatic 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic 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
    • C07D417/02—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 two hetero rings
    • C07D417/10—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 two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)

Abstract

Los compuestos aquí descritos son útiles para modular la actividad de la Btk y tratar enfermedades asociadas con una actividad excesiva de la Btk. Los compuestos son útiles además 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 doble; A es un heteroarilo de 5 eslabones o es un heteroarilo bicíclico de 5 ó 6 eslabones, en el que el CONH2 está unido al heteroarilo de 5 eslabones, cada uno de ellos está opcionalmente sustituido por uno o más A’; A’ es -NHR o R4; R es H, -R1, -R1-R2-R3, -R1-R3 o -R2-R3; R1 es arilo, heteroarilo, cicloalquilo, heterocicloalquilo o heteroarilo fusionado con un heterocicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más R1’ o R1’’; cada R1’ es con independencia halógeno, nitro, ciano, alquilo inferior-sulfonamido, -S(O)2 u oxo; cada R1’’ es con independencia alquilo inferior, cicloalquilo, heterocicloalquilo, alcoxi inferior, amino o amido, cada uno de ellos está opcionalmente sustituido por uno o más R1’’’; cada R1’’’ es con independencia hidroxi, halógeno, amino, alquil-amino, dialquil-amino o heterocicloalquilo; R2 es -C(=O), -C(=O)O, -C(=O)NR2’, -NHC(=O)O, -C(R2’)2, -O, -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, 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 o espiroheterocicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, halógeno, (alquilo inferior)-amino, di(alquilo inferior)-amino, hidroxi, hidroxi-alquilo inferior, alcoxi inferior, halógeno, nitro, amino, amido, acilo, ciano, oxo, guanidino, hidroxil-amino, carboxi, carbamoilo, carbamato, haloalcoxi inferior o haloalquilo inferior; dos grupos alquilo inferior juntos pueden formar un anillo; Q es CH o N; X es CH, N o N(X’); X’ es alquilo inferior; Y0 es H, halógeno o alquilo inferior; Y1 es Y1a, Y1b, Y1c o Y1d; Y1a es H o halógeno; Y1b 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; Y1c 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; Y1d es amino opcionalmente sustituido por uno o más alquilo inferior, alcoxi alquilo inferior o hidroxi-alquilo inferior; Y2 es H, halógeno o alquilo inferior; Y3 es H, halógeno, alquilo inferior, haloalquilo inferior, alcoxi inferior o hidroxialquilo inferior; e Y4 es H, alquilo inferior o hidroxialquilo inferior; o una sal farmacéuticamente aceptable del mismo.
ARP120101712A 2011-05-17 2012-05-15 Inhibidores de la tirosina-quinasa de bruton AR086403A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161486809P 2011-05-17 2011-05-17
US201261635470P 2012-04-19 2012-04-19

Publications (1)

Publication Number Publication Date
AR086403A1 true AR086403A1 (es) 2013-12-11

Family

ID=46124327

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120101712A AR086403A1 (es) 2011-05-17 2012-05-15 Inhibidores de la tirosina-quinasa de bruton

Country Status (20)

Country Link
US (1) US8729078B2 (es)
EP (1) EP2709997B1 (es)
JP (1) JP5859640B2 (es)
KR (1) KR101585753B1 (es)
CN (1) CN103582637B (es)
AR (1) AR086403A1 (es)
AU (1) AU2012257802A1 (es)
BR (1) BR112013029620A2 (es)
CA (1) CA2834077A1 (es)
CO (1) CO6852067A2 (es)
EC (1) ECSP13013025A (es)
ES (1) ES2590491T3 (es)
HK (1) HK1194381A1 (es)
IL (1) IL229197A0 (es)
MA (1) MA35112B1 (es)
MX (1) MX345170B (es)
SG (1) SG194728A1 (es)
TW (1) TW201300374A (es)
WO (1) WO2012156334A1 (es)
ZA (1) ZA201308397B (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR082590A1 (es) * 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
UA111756C2 (uk) 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
US8729072B2 (en) 2011-11-03 2014-05-20 F. Hoffman-La Roche Ag Alkylated piperazine compounds
JP5976826B2 (ja) 2011-11-03 2016-08-24 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｂｔｋ活性阻害剤としての８−フルオロフタラジン−１（２ｈ）−オン化合物
ES2552514T3 (es) 2011-11-03 2015-11-30 Hoffmann-La Roche Ag Compuestos bicíclicos de piperazina
AU2013293087B2 (en) 2012-07-24 2017-08-31 Pharmacyclics Llc Mutations associated with resistance to inhibitors of Bruton's tyrosine kinase (BTK)
PE20150756A1 (es) 2012-08-10 2015-06-03 Boehringer Ingelheim Int Compuestos heteroaromaticos como inhibidores de btk
WO2014076104A1 (en) * 2012-11-16 2014-05-22 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
KR20150075115A (ko) * 2012-11-30 2015-07-02 에프. 호프만-라 로슈 아게 브루톤 티로신 키나제의 억제제
DK2989106T3 (en) 2013-04-25 2017-03-20 Beigene Ltd CONDENSED HETEROCYCLIC COMPOUNDS AS PROTEINKINASE INHIBITORS
CN104211703B (zh) * 2013-05-30 2018-04-03 南京勇山生物科技有限公司 一类作为布鲁顿激酶抑制剂的稠杂环化合物
CN105473573B (zh) 2013-06-25 2018-03-16 百时美施贵宝公司 用作激酶抑制剂的咔唑甲酰胺化合物
AR096721A1 (es) 2013-06-25 2016-01-27 Bristol Myers Squibb Co Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos
CA2912359A1 (en) 2013-07-03 2015-01-08 F. Hoffmann-La Roche Ag Heteroaryl pyridone and aza-pyridone amide compounds
PT3702373T (pt) 2013-09-13 2022-09-27 Beigene Switzerland Gmbh Anticorpos anti-pd1 e a sua utilização como agentes terapêuticos e de diagnóstico
CN105793251B (zh) 2013-12-05 2018-10-12 豪夫迈·罗氏有限公司 具有亲电子官能性的杂芳基吡啶酮和氮杂-吡啶酮化合物
US9624201B2 (en) 2013-12-13 2017-04-18 Hoffmann-La Roche Inc. Inhibitors of bruton's tyrosine kinase
JP2017507963A (ja) 2014-03-12 2017-03-23 ノバルティス アーゲー Ｂｔｋ阻害薬とａｋｔ阻害薬を含む組み合わせ
TWI687438B (zh) 2014-07-03 2020-03-11 英屬開曼群島商百濟神州生物科技有限公司 抗ｐｄ-ｌ１抗體及其作為治療及診斷之用途
WO2016050921A1 (en) * 2014-10-02 2016-04-07 F. Hoffmann-La Roche Ag Pyrazole carboxamide compounds for use in the treament of disorders mediated by bruton's tyrosine kinase (btk)
CN107108555B (zh) 2014-10-24 2020-12-01 百时美施贵宝公司 三环阻转异构体化合物
AU2015335703B2 (en) 2014-10-24 2020-05-21 Bristol-Myers Squibb Company Carbazole derivatives
MY188048A (en) 2014-10-24 2021-11-12 Bristol Myers Squibb Co Indole carboxamide compounds useful as kinase inhibitors
WO2017123695A1 (en) * 2016-01-13 2017-07-20 Boehringer Ingelheim International Gmbh Isoquinolones as btk inhibitors
JPWO2017169503A1 (ja) * 2016-04-01 2019-02-14 国立大学法人千葉大学 含窒素芳香族アミドの製造方法、ピロール・イミダゾールポリアミドの製造方法、及び化合物
AU2017293423B2 (en) 2016-07-05 2023-05-25 Beigene, Ltd. Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer
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
EP3500299B1 (en) 2016-08-19 2023-12-13 BeiGene Switzerland GmbH Combination of zanubrutinib with an anti-cd20 or an anti-pd-1 antibody for use in treating cancer
WO2018053437A1 (en) 2016-09-19 2018-03-22 Mei Pharma, Inc. Combination therapy
CN110461847B (zh) 2017-01-25 2022-06-07 百济神州有限公司 (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途
WO2018149284A1 (zh) * 2017-02-16 2018-08-23 四川科伦博泰生物医药股份有限公司 激酶抑制剂及其制备方法和用途
AU2018290532A1 (en) 2017-06-26 2019-11-21 Beigene, Ltd. Immunotherapy for hepatocellular carcinoma
US11377449B2 (en) 2017-08-12 2022-07-05 Beigene, Ltd. BTK inhibitors with improved dual selectivity
CN111801334B (zh) 2017-11-29 2023-06-09 百济神州瑞士有限责任公司 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2023198199A1 (zh) * 2022-04-15 2023-10-19 先声再明医药有限公司 膜缔合酪氨酸和苏氨酸激酶抑制剂
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050032869A1 (en) 2003-07-08 2005-02-10 Pharmacia Italia S.P.A. Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
MX2010008197A (es) * 2008-02-05 2010-08-23 Hoffmann La Roche Nuevas piridinonas y piridazinonas.
EP2307418B1 (en) * 2008-07-18 2014-03-12 F.Hoffmann-La Roche Ag Novel phenylimidazopyrazines
NZ593096A (en) * 2008-12-19 2012-11-30 Bristol Myers Squibb Co Carbazole carboxamide compounds useful as kinase inhibitors
US8299077B2 (en) 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton

Also Published As

Publication number Publication date
KR20140025519A (ko) 2014-03-04
KR101585753B1 (ko) 2016-01-14
MA35112B1 (fr) 2014-05-02
ECSP13013025A (es) 2014-01-31
JP5859640B2 (ja) 2016-02-10
CN103582637B (zh) 2015-08-12
HK1194381A1 (en) 2014-10-17
MX345170B (es) 2017-01-19
CO6852067A2 (es) 2014-01-30
ES2590491T3 (es) 2016-11-22
TW201300374A (zh) 2013-01-01
JP2014520079A (ja) 2014-08-21
US8729078B2 (en) 2014-05-20
WO2012156334A1 (en) 2012-11-22
EP2709997A1 (en) 2014-03-26
US20120295885A1 (en) 2012-11-22
ZA201308397B (en) 2014-07-30
CA2834077A1 (en) 2012-11-22
EP2709997B1 (en) 2016-06-29
AU2012257802A1 (en) 2013-10-31
BR112013029620A2 (pt) 2016-09-06
CN103582637A (zh) 2014-02-12
IL229197A0 (en) 2014-01-30
SG194728A1 (en) 2013-12-30
MX2013013267A (es) 2014-06-23

Similar Documents

Publication Publication Date Title
AR086403A1 (es) Inhibidores de la tirosina-quinasa de bruton
AR082590A1 (es) Inhibidores de la tirosina-quinasa de bruton
AR076066A1 (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.
AR092536A1 (es) Inhibidores de la tirosina-quinasa de bruton
AR070408A1 (es) Piridinonas y piridazinonas
AR087543A1 (es) Inhibidores de la tirosina-quinasa de bruton
AR092108A1 (es) Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn
AR110139A1 (es) COMPUESTOS MONO Y ESPIROCÍCLICOS QUE CONTIENEN CICLOBUTANO Y AZETIDINA COMO INHIBIDORES DE LA INTEGRINA aV
AR082945A1 (es) Derivados de imidazo[1,2-b]piridazina como inhibidores de la trk
AR058362A1 (es) Derivados de isoquinolina - aminopirazol su obtencion y su utilizacion como agentes farmaceuticos
AR052887A1 (es) Derivados de tiazol, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para tratar enfermedades mediadas por la inhibicion de la protein quinasa
AR076435A1 (es) Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos
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.
AR085150A1 (es) Agentes moduladores de s1p
CO6321170A2 (es) Heterociclos fusionados de ciclobutoxi amino y usos terapeuticos de los mismos
AR083199A1 (es) Compuestos de n-heteroarilo con unidad de puente ciclico
PE20142081A1 (es) Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos
ECSP066688A (es) Polimorfo cristalino de una sal de bisulfato de underivados de azepinoindol como agentes farmaceuticos antagonista del receptor de trombina
AR046297A1 (es) Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo
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.
AR087760A1 (es) Heterociclilaminas como inhibidores de pi3k
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
AR055431A1 (es) Derivados del acido 4-amino-tieno[3,2-c]piridina-7-carboxilico

Legal Events

Date Code Title Description
FA Abandonment or withdrawal