[go: up one dir, main page]

PE20151495A1 - Compuestos de pirrolopirimidina como inhibidores de quinasas - Google Patents

Compuestos de pirrolopirimidina como inhibidores de quinasas

Info

Publication number
PE20151495A1
PE20151495A1 PE2015000625A PE2015000625A PE20151495A1 PE 20151495 A1 PE20151495 A1 PE 20151495A1 PE 2015000625 A PE2015000625 A PE 2015000625A PE 2015000625 A PE2015000625 A PE 2015000625A PE 20151495 A1 PE20151495 A1 PE 20151495A1
Authority
PE
Peru
Prior art keywords
conditions
kinase inhibitors
pyrrolopyrimidine compounds
inhibitors
diseases
Prior art date
Application number
PE2015000625A
Other languages
English (en)
Inventor
Wei Chen
David J Loury
Longcheng Wang
Original Assignee
Pharmacyclics Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50728514&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20151495(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pharmacyclics Inc filed Critical Pharmacyclics Inc
Publication of PE20151495A1 publication Critical patent/PE20151495A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se refiere a compuestos derivados de pirrolopirimidina de formula (I) que son inhibidores de la tirosina quinasa de Bruton (Btk), donde los valores de los sustituyente R1, R6, R7, R8; R24, G, Y, Z y n son los que se definen en la solicitud. Ademas se describen metodos para utilizar los inhibidores Btk, solos o en combinacion con otros agentes terapeuticos, para el tratamiento de enfermedades o condiciones autoinmunes, enfermedades o condiciones heteroinmunes, cancer, incluido el linfoma, y enfermedades o condiciones inflamatorias
PE2015000625A 2012-11-15 2013-11-14 Compuestos de pirrolopirimidina como inhibidores de quinasas PE20151495A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261727031P 2012-11-15 2012-11-15

Publications (1)

Publication Number Publication Date
PE20151495A1 true PE20151495A1 (es) 2015-10-23

Family

ID=50728514

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015000625A PE20151495A1 (es) 2012-11-15 2013-11-14 Compuestos de pirrolopirimidina como inhibidores de quinasas

Country Status (24)

Country Link
US (3) US9096604B2 (es)
EP (1) EP2920180A4 (es)
JP (1) JP2015537033A (es)
KR (1) KR20150084923A (es)
CN (1) CN104854107A (es)
AR (1) AR093518A1 (es)
AU (1) AU2013344656A1 (es)
BR (1) BR112015011171A2 (es)
CA (1) CA2890934A1 (es)
CL (1) CL2015001268A1 (es)
CR (1) CR20150263A (es)
DO (1) DOP2015000108A (es)
EA (1) EA201590855A1 (es)
HK (1) HK1215253A1 (es)
IL (1) IL238728A0 (es)
MA (1) MA38183A1 (es)
MX (1) MX2015006168A (es)
NI (1) NI201500067A (es)
PE (1) PE20151495A1 (es)
PH (1) PH12015501067A1 (es)
SG (1) SG11201503842PA (es)
TN (1) TN2015000174A1 (es)
TW (1) TWI522359B (es)
WO (1) WO2014078578A1 (es)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120101114A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
CN105362277A (zh) 2008-07-16 2016-03-02 药品循环有限公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
MX342405B (es) 2010-06-03 2016-09-28 Pharmacyclics Inc El uso de inhibidores de la tirosina quinasa de bruton (btk).
WO2012158795A1 (en) 2011-05-17 2012-11-22 Principia Biopharma Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
PT2710005T (pt) 2011-05-17 2016-11-16 Principia Biopharma Inc Inibidores de tirosina-quinase
EA201490265A1 (ru) 2011-07-13 2014-12-30 Фармасайкликс, Инк. Ингибиторы тирозинкиназы брутона
ES2834093T3 (es) 2011-07-21 2021-06-16 Sumitomo Dainippon Pharma Oncology Inc Inhibidores de proteína quinasa heterocíclicos
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
MX387669B (es) 2012-06-04 2025-03-18 Pharmacyclics Llc Formas cristalinas de un inhibidor de tirosina quinasa de bruton.
BR112015001690A2 (pt) 2012-07-24 2017-11-07 Pharmacyclics Inc mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk)
PT2892900T (pt) 2012-09-10 2017-11-06 Principia Biopharma Inc Compostos de pirazolopirimidina como inibidores de cinase
BR112015011171A2 (pt) * 2012-11-15 2017-07-11 Pharmacyclics Inc compostos de pirrolopirimidina como inibidores da quinase
AU2014236820B2 (en) 2013-03-14 2018-08-02 Sumitomo Pharma Oncology, Inc. JAK2 and ALK2 inhibitors and methods for their use
US8957080B2 (en) 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
ES2709509T3 (es) 2013-08-12 2019-04-16 Pharmacyclics Llc Procedimientos para el tratamiento de cáncer amplificado por HER2
US9624224B2 (en) 2013-09-30 2017-04-18 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
US9951056B2 (en) 2013-09-30 2018-04-24 Beijing Innocare Pharma Tech Co., Ltd. Substituted nicotinamide inhibitors of BTK and their preparation and use in the treatment of cancer, inflammation and autoimmune disease
PT3107544T (pt) 2014-02-21 2021-01-05 Principia Biopharma Inc Sais e forma sólida de um inibidor de btk
US9885086B2 (en) 2014-03-20 2018-02-06 Pharmacyclics Llc Phospholipase C gamma 2 and resistance associated mutations
WO2016019233A1 (en) * 2014-08-01 2016-02-04 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
CA2955747A1 (en) 2014-08-07 2016-02-11 Pharmacyclics Llc Novel formulations of a bruton's tyrosine kinase inhibitor
CA2970723C (en) 2014-12-18 2023-09-05 Principia Biopharma Inc. Treatment of pemphigus
IL315294A (en) 2015-03-03 2024-10-01 Pharmacyclics Llc Pharmaceutical formulations of bruton's tyrosine kinase inhibitor
EP3313839A1 (en) 2015-06-24 2018-05-02 Principia Biopharma Inc. Tyrosine kinase inhibitors
US10550124B2 (en) * 2015-08-13 2020-02-04 San Diego State University Foundation Atropisomerism for increased kinase inhibitor selectivity
WO2017046604A1 (en) * 2015-09-16 2017-03-23 Redx Pharma Plc Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer
AU2016369584A1 (en) 2015-12-16 2018-07-19 Southern Research Institute Pyrrolopyrimidine compounds, use as inhibitors of the kinase LRRK2, and methods for preparation thereof
CN107513068A (zh) * 2016-06-16 2017-12-26 中国科学院上海药物研究所 一种具有fgfr抑制活性的新型化合物及其制备和应用
IL293621B2 (en) 2016-06-29 2023-09-01 Principia Biopharma Inc Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[4,3-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4 -Methyl-4-[4-(oxane-3-yl)piperazine-1-yl)penta-2-ananitrile
IL295972A (en) * 2016-09-16 2022-10-01 Vitae Pharmaceuticals Llc Inhibitors of the menin-mll interaction
US11590167B2 (en) 2016-12-03 2023-02-28 Juno Therapeutic, Inc. Methods and compositions for use of therapeutic T cells in combination with kinase inhibitors
CN106588937B (zh) * 2017-01-16 2018-09-21 东莞市真兴贝特医药技术有限公司 咪唑并吡嗪类化合物及其制备方法和应用
CN106946896B (zh) * 2017-03-30 2019-05-21 成都知普莱生物医药科技有限公司 呋喃并[2,3-d]嘧啶-4-胺衍生物
IT201700099690A1 (it) * 2017-09-06 2019-03-06 Abiogen Pharma Spa Composizione per l’integrazione di calcio
WO2019195753A1 (en) 2018-04-05 2019-10-10 Tolero Pharmaceuticals, Inc. Axl kinase inhibitors and use of the same
KR20200143454A (ko) 2018-04-13 2020-12-23 스미토모 다이니폰 파마 온콜로지, 인크. 골수증식성 신생물 및 암과 연관된 섬유증의 치료를 위한 pim 키나제 억제제
CN112512597A (zh) 2018-07-26 2021-03-16 大日本住友制药肿瘤公司 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂
CN114040760B (zh) * 2018-12-31 2025-05-09 拜欧米富士恩公司 Menin-mll相互作用的不可逆抑制剂
KR102904026B1 (ko) 2019-02-12 2025-12-26 스미토모 파마 아메리카, 인크. 헤테로시클릭 단백질 키나제 억제제를 포함하는 제제
TWI828861B (zh) * 2019-02-15 2024-01-11 日商大鵬藥品工業股份有限公司 7H-吡咯并[2,3-d]嘧啶-4-胺衍生物
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN111825674A (zh) * 2019-04-22 2020-10-27 上海仕谱生物科技有限公司 嘧啶并五元杂环类化合物及其作为突变型idh2抑制剂的用途
WO2020263822A1 (en) 2019-06-25 2020-12-30 San Diego State University Foundation Selective btk irreversible inhibitors
CA3154257A1 (en) 2019-10-14 2021-04-22 Principia Biopharma Inc. Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
EP4093397A1 (en) 2020-01-20 2022-11-30 Genzyme Corporation Therapeutic tyrosine kinase inhibitors for relapsing multiple sclerosis (rms)
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
AU2021209884A1 (en) 2020-01-22 2022-09-15 Principia Biopharma Inc. Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
WO2021185348A1 (zh) * 2020-03-20 2021-09-23 深圳市塔吉瑞生物医药有限公司 取代的丙烯酰胺衍生物及其组合物及用途
CN113527300B (zh) * 2020-06-04 2023-02-03 广州百霆医药科技有限公司 布鲁顿酪氨酸蛋白激酶抑制剂
WO2022109551A1 (en) * 2020-11-17 2022-05-27 Relay Therapeutics, Inc. Src inhibitors and uses thereof
WO2022121670A1 (zh) 2020-12-10 2022-06-16 苏州科睿思制药有限公司 Tolebrutinib的晶型及其制备方法和用途
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2023078413A1 (zh) * 2021-11-04 2023-05-11 微境生物医药科技(上海)有限公司 Fgfr2抑制剂、及其制备方法和医药用途
US12016941B2 (en) * 2022-03-03 2024-06-25 Profounda Health And Beauty Inc. Treatment composition for nasal and oral dryness, nosebleeds, and allergy symptoms
EP4611753A1 (en) 2022-10-31 2025-09-10 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms

Family Cites Families (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
JPH01167840A (ja) 1987-12-24 1989-07-03 Konica Corp 新規な写真用シアンカプラー
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
GB9226855D0 (en) 1992-12-23 1993-02-17 Erba Carlo Spa Vinylene-azaindole derivatives and process for their preparation
US6326469B1 (en) 1994-04-22 2001-12-04 Sugen, Inc. Megakaryocytic protein tyrosine kinases
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
IL131582A0 (en) 1997-03-19 2001-01-28 Basf Ag Pyrrolo [2,3d] pyrimidines and their use as tyrosine kinase inhibitors
KR20010042804A (ko) 1998-04-17 2001-05-25 파커 휴우즈 인스티튜트 비티케이 억제제와 그들의 동정 방법 및 용도
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
US20050287596A9 (en) 1998-06-26 2005-12-29 Braisted Andrew C Novel ligands and libraries of ligands
US6998233B2 (en) 1998-06-26 2006-02-14 Sunesis Pharmaceuticals, Inc. Methods for ligand discovery
US6335155B1 (en) 1998-06-26 2002-01-01 Sunesis Pharmaceuticals, Inc. Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules
US6306897B1 (en) 1999-03-19 2001-10-23 Parker Hughes Institute Calanolides for inhibiting BTK
BR0014073A (pt) 1999-09-17 2002-07-16 Abbott Gmbh & Co Kg Pirazolopirimidinas como agentes terapêuticos
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
MXPA02003364A (es) 1999-10-06 2002-08-23 Boehringer Ingelheim Pharma Compuestos heterociclicos utiles como inhibidores de las cinasas de tirosina.
AU4508601A (en) 1999-11-30 2001-06-18 Parker Hughes Institute Inhibitors of collagen-induced platelet aggregation
WO2001044258A1 (en) 1999-12-17 2001-06-21 Ariad Pharmaceuticals, Inc. Novel heterocycles
GB0005345D0 (en) 2000-03-06 2000-04-26 Mathilda & Terence Kennedy Ins Methods of treating sepsis septic shock and inflammation
HUP0303656A3 (en) 2000-10-23 2006-03-28 Bristol Myers Squibb Co Modulators of bruton's tyrosine kinase, their identification and use
EP1345592A2 (en) 2000-12-06 2003-09-24 Pharmacia Corporation Rapidly dispersing pharmaceutical composition comprising effervescent agents
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
US8306897B2 (en) 2001-05-04 2012-11-06 Stockshield, Inc. Method and system for insuring against investment loss
AU2002315389A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof
EP1418917A1 (en) 2001-08-10 2004-05-19 Novartis AG Use of c-src inhibitors alone or in combination with sti571 for the treatment of leukaemia
WO2003016338A1 (en) 2001-08-15 2003-02-27 Parker Hughes Institute Crystal structure of the btk kinase domain
CA2464094C (en) 2001-11-21 2013-07-02 Sunesis Pharmaceuticals, Inc. Methods for ligand discovery
US20050084905A1 (en) 2002-03-21 2005-04-21 Prescott John C. Identification of kinase inhibitors
GB2388594A (en) 2002-05-16 2003-11-19 Bayer Ag Imidazo-triazine PDE 4 inhibitors
CA2494942A1 (en) 2002-08-08 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted benzimidazole compounds
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
US7687506B2 (en) 2003-04-11 2010-03-30 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
US20050008640A1 (en) 2003-04-23 2005-01-13 Wendy Waegell Method of treating transplant rejection
EP1473039A1 (en) 2003-05-02 2004-11-03 Centre National De La Recherche Scientifique (Cnrs) Use of inhibitors and antisense oligonucleotides of BTK for the treatment of proliferative mastocytosis
WO2005014599A1 (en) 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
US8131475B2 (en) 2003-09-03 2012-03-06 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Methods for identifying, diagnosing, and predicting survival of lymphomas
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
BRPI0415395A (pt) 2003-10-15 2006-12-12 Osi Pharm Inc composto, métodos para inibir a atividade da proteìna quinase e para tratar um paciente que tenha uma condição que seja mediada pela atividade da proteìna quinase, e, composição
WO2005060956A1 (en) 2003-12-12 2005-07-07 University Of Maryland, Baltimore IMMUNOMODULATORY COMPOUNDS THAT TARGET AND INHIBIT THE pY+3 BINDING SITE OF TYROSENE KINASE p56 LCK SH2 DOMAIN
BRPI0418031A (pt) 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
EP1716151A1 (en) 2004-01-26 2006-11-02 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US20060025383A1 (en) 2004-02-03 2006-02-02 Neil Wishart Aminobenzoxazoles as therapeutic agents
AR053090A1 (es) 2004-07-20 2007-04-25 Osi Pharm Inc Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos
JP2008514635A (ja) 2004-09-27 2008-05-08 コーザン バイオサイエンシス インコーポレイテッド 特異的キナーゼ阻害剤
BRPI0516166A (pt) 2004-09-28 2008-08-26 Janssen Pharmaceutica Nv antagonista do ccr2 de dipiperidina substituìda
JP2008519843A (ja) 2004-11-10 2008-06-12 シージーアイ ファーマスーティカル インコーポレーテッド 特定のイミダゾ[1,2−a]ビラジン−8−イラミンズ、その生成方法及びそれに関する使用方法
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
EP1863766B1 (en) 2005-03-10 2015-05-20 Gilead Connecticut, Inc. Certain substituted amides, method of making, and method of use thereof
BRPI0610278A2 (pt) 2005-05-13 2010-06-08 Irm Llc compostos e composições como inibidores de proteìna cinase
NZ565255A (en) 2005-06-22 2010-04-30 Plexxikon Inc Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors
US20070065449A1 (en) 2005-09-16 2007-03-22 Claire Verschraegen Method of treating cancer, especially soft tissue sarcoma utilizing gemcitabine in combination with docetaxel and anti-VEGF therapy (bevacizumab)
CA2629314A1 (en) 2005-11-12 2007-05-24 Boehringer Ingelheim International Gmbh Tec kinase inhibitors
KR20080098490A (ko) 2006-01-13 2008-11-10 파마시클릭스, 인코포레이티드 티로신 키나제 억제제 및 이의 용도
ES2420834T3 (es) 2006-01-30 2013-08-27 The Scripps Research Institute Métodos de detección de células tumorales circulantes y métodos de diagnóstico del cáncer en un sujeto mamífero
MX2008012928A (es) 2006-04-04 2009-03-06 Univ California Antagonistas de pi3-cinasa.
MX2008014450A (es) 2006-05-18 2009-03-09 Mannkind Corp Inhibidores de cinasa intracelular.
PL2529621T3 (pl) 2006-09-22 2017-06-30 Pharmacyclics Llc Inhibitory kinazy tyrozynowej brutona
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
NL2000640C2 (nl) 2007-03-05 2008-09-08 Stichting Wetsus Ct Of Excelle Werkwijze en systeem voor het zuiveren van een vloeistof.
US20120101114A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
EP2139487B1 (en) 2007-03-28 2015-11-11 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US20090010911A1 (en) 2007-04-06 2009-01-08 Iowa State University Research Foundation, Inc. Methods and compositions for affecting cyclophilin a regulation of kinases in modulating cellular activities
US7982036B2 (en) 2007-10-19 2011-07-19 Avila Therapeutics, Inc. 4,6-disubstitued pyrimidines useful as kinase inhibitors
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
CA2909988A1 (en) 2007-10-23 2009-04-30 F. Hoffmann-La Roche Ag Kinase inhibitors
US8426441B2 (en) 2007-12-14 2013-04-23 Roche Palo Alto Llc Inhibitors of bruton's tyrosine kinase
US20150152115A1 (en) 2007-12-27 2015-06-04 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
RU2536584C2 (ru) 2008-06-27 2014-12-27 Авила Терапьютикс, Инк. Гетероарильные соединения и их применение
CN105362277A (zh) 2008-07-16 2016-03-02 药品循环有限公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
NZ603495A (en) 2008-09-05 2014-05-30 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
US8426428B2 (en) * 2008-12-05 2013-04-23 Principia Biopharma, Inc. EGFR kinase knockdown via electrophilically enhanced inhibitors
JP5656976B2 (ja) 2009-04-29 2015-01-21 ローカス ファーマシューティカルズ インコーポレイテッド ピロロトリアジン化合物
MX339811B (es) 2009-09-16 2016-06-08 Celgene Avilomics Res Inc * Conjugados e inhibidores de cinasa de proteina.
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
WO2011152351A1 (ja) 2010-05-31 2011-12-08 小野薬品工業株式会社 プリノン誘導体
MX342405B (es) 2010-06-03 2016-09-28 Pharmacyclics Inc El uso de inhibidores de la tirosina quinasa de bruton (btk).
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
DK2975042T3 (en) 2010-06-23 2019-01-21 Hanmi Science Co Ltd Novel fused pyrimidine derivatives to inhibit tyrosine kinase activity
SG187796A1 (en) 2010-08-10 2013-03-28 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor
PT2710005T (pt) * 2011-05-17 2016-11-16 Principia Biopharma Inc Inibidores de tirosina-quinase
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
US8501724B1 (en) 2012-01-31 2013-08-06 Pharmacyclics, Inc. Purinone compounds as kinase inhibitors
MX387669B (es) 2012-06-04 2025-03-18 Pharmacyclics Llc Formas cristalinas de un inhibidor de tirosina quinasa de bruton.
DK2861599T3 (da) * 2012-06-18 2020-03-02 Principia Biopharma Inc Reversible kovalente pyrrolo- eller pyrazolopyrimidiner, der er nyttige til behandling af cancer og autoimmunsygdomme
BR112015001690A2 (pt) 2012-07-24 2017-11-07 Pharmacyclics Inc mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk)
BR112015011171A2 (pt) * 2012-11-15 2017-07-11 Pharmacyclics Inc compostos de pirrolopirimidina como inibidores da quinase
WO2014194254A1 (en) 2013-05-30 2014-12-04 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
EP3027192A4 (en) 2013-08-02 2017-03-22 Pharmacyclics, LLC Methods for the treatment of solid tumors
CN105848680A (zh) 2013-10-25 2016-08-10 药品循环有限责任公司 使用布鲁顿酪氨酸激酶抑制剂和免疫疗法的治疗
CN103923084B (zh) 2014-01-29 2016-08-17 苏州晶云药物科技有限公司 几种晶型及其制备方法
US20150238490A1 (en) 2014-02-21 2015-08-27 Pharmacyclics, Inc. Biomarkers for predicting response of dlbcl to treatment with ibrutinib
US9885086B2 (en) 2014-03-20 2018-02-06 Pharmacyclics Llc Phospholipase C gamma 2 and resistance associated mutations

Also Published As

Publication number Publication date
HK1215253A1 (zh) 2016-08-19
AR093518A1 (es) 2015-06-10
CR20150263A (es) 2015-08-24
DOP2015000108A (es) 2015-06-30
TW201425315A (zh) 2014-07-01
IL238728A0 (en) 2015-06-30
MA38183A1 (fr) 2017-03-31
CL2015001268A1 (es) 2015-07-10
US20160375026A1 (en) 2016-12-29
US20150239897A1 (en) 2015-08-27
BR112015011171A2 (pt) 2017-07-11
EP2920180A4 (en) 2016-04-13
PH12015501067A1 (en) 2015-08-10
EA201590855A1 (ru) 2015-11-30
KR20150084923A (ko) 2015-07-22
JP2015537033A (ja) 2015-12-24
NI201500067A (es) 2016-02-15
US9540385B2 (en) 2017-01-10
MX2015006168A (es) 2015-08-10
TWI522359B (zh) 2016-02-21
TN2015000174A1 (en) 2016-10-03
US9096604B2 (en) 2015-08-04
US20140142126A1 (en) 2014-05-22
SG11201503842PA (en) 2015-06-29
CN104854107A (zh) 2015-08-19
CA2890934A1 (en) 2014-05-22
EP2920180A1 (en) 2015-09-23
AU2013344656A1 (en) 2015-06-04
WO2014078578A1 (en) 2014-05-22

Similar Documents

Publication Publication Date Title
PE20151495A1 (es) Compuestos de pirrolopirimidina como inhibidores de quinasas
CY1123756T1 (el) Παραγωγα διπυραζολιου ως αναστολεις jak
CY1120866T1 (el) Παρεμποδιστες dna-pk
DOP2016000140A (es) Inhibidores de syk
PE20151064A1 (es) Nuevos derivados tienopirimidina, un proceso para su preparacion y composiciones farmaceuticas que los contienen
NI201500059A (es) Inhibidores de la tirosina-quinasa de bruton
MX2020010412A (es) Inhibidores de tirosina quinasa de bruton.
MX2017016344A (es) Compuestos de benzoxacepina oxazolidinona y metodos de uso.
CY1120204T1 (el) Αμορφη στερεα διασπορα για χρηση σε θεραπεια καρκινου του εγκεφαλο
EA201591753A1 (ru) 3-пиримидин-4-илоксазолидин-2-оны в качестве ингибиторов мутантного idh
CU20170162A7 (es) Derivados de fenil-tieno(2,3-d)pirimidina-hidroxiácido útiles en el tratamiento del cáncer y enfermedades autoinmunes, método de preparación de los mismos y composiciones farmacéuticas que los contienen
NI201500140A (es) Compuestos y composiciones terapéuticos
PH12015501576A1 (en) Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
ECSP15013883A (es) Benzamidas
UY35625A (es) Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos como inhibidores de quinasa
CR20160285A (es) Inhibidores de quinasa relacionada con la tropomiosina (trk)
DOP2015000176A (es) Compuestos de azetidiniloxifenilpirrolidina
EA201590656A1 (ru) Азаиндолины
UY35823A (es) Profármacos de antagonista de nmda
EA201501177A1 (ru) Фармацевтические композиции
CY1115039T1 (el) Συνθεση για επαλειψη στο δερμα και χρηση αυτης

Legal Events

Date Code Title Description
FD Application declared void or lapsed