AR080940A1 - Compuestos heterociclicos utiles como inhibidores de quinasa - Google Patents

Compuestos heterociclicos utiles como inhibidores de quinasa

Info

Publication number
AR080940A1
AR080940A1 ARP110101385A ARP110101385A AR080940A1 AR 080940 A1 AR080940 A1 AR 080940A1 AR P110101385 A ARP110101385 A AR P110101385A AR P110101385 A ARP110101385 A AR P110101385A AR 080940 A1 AR080940 A1 AR 080940A1
Authority
AR
Argentina
Prior art keywords
fluorine
optionally substituted
lower alkyl
lower alkoxy
cycloalkyl
Prior art date
Application number
ARP110101385A
Other languages
English (en)
Inventor
Hing Zhang
Chao Zhang
Wayne Spevak
Todd Ewing
Prabha N Ibrahim
James Tsai
Jiazhong Zhang
Original Assignee
Plexxikon 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=44816304&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR080940(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Plexxikon Inc filed Critical Plexxikon Inc
Publication of AR080940A1 publication Critical patent/AR080940A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • 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

Landscapes

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

Abstract

Se describen los compuestos y sales, formulaciones, conjugados, derivados, formas y usos de los mismos. En ciertos aspectos y formas de realizacion, los compuestos descritos o sales, formulaciones, conjugados, derivados, formas del mismo son una o más proteínas quinasas activas tipo Fms, Kit, Flt3, TrkA, TrkB y TrkC. También se describen los métodos de uso de los mismos para tratar enfermedades y condiciones, incluyendo enfermedades y condiciones asociadas con la actividad de una o más de las quinasas Fms, Kit, Flt3, TrkA, TrkB y TrkC, incluyendo artritis reumatoide, osteoartritis, osteoporosis, osteolisis periprostética, esclerosis sistémica, desordenes desmielinizantes, esclerosis multiple, Síndrome de Charcot Marie Tooth, esclerosias lateral amiotropica, enfermedad de Alzheimer, enfermedad de Parkinson, isquemia global, colitis ulcerativa, enfermedad de Crohn, purpura trombocitopénica inmune, arterioesclerosis, lupus erimatoso sistémico, mielopreparacion para trasplante autologo, rechazo de trasplante, glomerulonefritis, nefritis intersticial, nefritis lupica, necrosis tubular, nefropatía diabética, hipertrofia renal, diabetes tipo I, dolor agudo, dolor inflamatorio, dolor neuropático, leucemia mieloide aguda, melanoma, mieloma multiple, cáncer de seno, cáncer de prostata, cáncer pancreático, cáncer de pulmon, cáncer de ovario, gliomas, glioblastoma, neurofibromatosis, metástasis osea, metástasis cerebral, tumores estromales gastrointestinales, y tumores de células gigantes. Reivindicacion 1: Un compuesto que tiene la estructura química de la Formula 1, o una sal, profármaco, solvato o tautomero o esteroisomero del mismo donde: X1 es-N=, -C(H)=, o -C(R1)=; Y1 es-N= y R3 es Hidrogeno; o Y1 es -C(H)= y R3 es fluor o cloro; L1 es -C(H2)- o -C(O)-; Ci1 es Cicloalquilo opcionalmente sustituido con uno o más R4, el fenil opcionalmente sustituido con uno o más R5, o heteroaril de 5 o 6 miembros opcionalmente sustituido en un átomo de carbono disponible con uno o más R6 y opcionalmente sustituido en un átomo de nitrogeno disponible con R7; donde X1 es -C(R1)=, R2 es Hidrogeno; donde X1 es-N= o -C(H)=, R2 es seleccionado del grupo que consiste de hidrogeno, cicloalquilo, alquilo inferior opcionalmente sustituido con uno o más R8, -N(R9a)(R9b), y -O-R9; R1 es fluor, cloro, o alquilo inferior opcionalmente substitituido con uno o más fluor; cada R4 es independientemente seleccionado del grupo que consiste de fluor, -OH, alquilo inferior opcionalmente sustituido con uno o más fluor, y alcoxi inferior opcionalmente sustituido con uno o más fluor; cada R5 es independientemente seleccionado del grupo que consiste de fluor, cloro, -O-R10, -S-R11, -S(O2)-R12, y alquilo inferior opcionalmente sustituido con uno o más R13; cada R6 es independientemente seleccionado del grupo que consiste de fluor, cloro, bromo, cicloalquilo, alquilo inferior opcionalmente sustituido con uno o más fluor, y alcoxi inferior opcionalmente sustituido con uno o más fluor; o dos R6 unidos a átomos de carbono adyacentes del anillo heteroarilo forman un anillo cicloalquilo fusionado; R7 es Cicloalquilo, alcoxi inferior o alquilo inferior opcionalmente sustituido con uno o más fluor; R8 es fluor o alcoxi inferior opcionalmente sustituido con uno o más fluor; R9a es H y R9b es seleccionado del grupo que consiste de (i) H, alquilo inferior, alquilo inferior sustituido con uno o más fluor, alquilo inferior sustituido con alcoxi inferior o alquilo inferior sustituido con hidroxil y (ii) cicloalquilo, cicloalquiloalquilo, heterocícloalquilo, heterocicloalquiloalquilo, arilalquilo, heteroarilalquilo, cada uno de los cuales es opcionalmente sustituido con uno a tres miembros seleccionados de alquilo inferior, haloalquilo,alcoxi inferior o fluor; o R9a y R9b junto con nitrogeno al cual se adhieren forman un anillo de 5 a 6 miembros que tiene de 0 a 1 heteroátomos seleccionados de O, N o S, cada uno de los cuales es opcionalmente sustituido con uno a tres miembros seleccionados de alquilo inferior, haloalquilo, alcoxi inferior o fluor; R9 es alquilo inferior, alquilo inferior sustituido con uno o más fluor, o alquilo inferior sustituido con alcoxi inferior; cada R10, R11 y R12 son independientemente alquilo inferior opcionalmente sustituido con uno o más fluor; y cada R13 es independientemente seleccionado del grupo que consiste de fluor, -OH, y alcoxi inferior opcionalmente sustituido con uno o más fluor.
ARP110101385A 2010-04-21 2011-04-20 Compuestos heterociclicos utiles como inhibidores de quinasa AR080940A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US32662610P 2010-04-21 2010-04-21

Publications (1)

Publication Number Publication Date
AR080940A1 true AR080940A1 (es) 2012-05-16

Family

ID=44816304

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP110101385A AR080940A1 (es) 2010-04-21 2011-04-20 Compuestos heterociclicos utiles como inhibidores de quinasa
ARP190102503A AR115233A2 (es) 2010-04-21 2019-09-03 Pirrolo[2,3-d]pirimidinas

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP190102503A AR115233A2 (es) 2010-04-21 2019-09-03 Pirrolo[2,3-d]pirimidinas

Country Status (37)

Country Link
US (3) US8901118B2 (es)
EP (1) EP2560972B1 (es)
JP (2) JP5808793B2 (es)
KR (1) KR101799126B1 (es)
CN (1) CN102947305B (es)
AR (2) AR080940A1 (es)
AU (1) AU2011242778B2 (es)
BR (1) BR112012026927A2 (es)
CA (1) CA2796998C (es)
CL (1) CL2012002937A1 (es)
CO (1) CO6620045A2 (es)
CR (1) CR20120536A (es)
CY (1) CY1120554T1 (es)
DK (1) DK2560972T3 (es)
EA (1) EA028105B1 (es)
EC (1) ECSP12012245A (es)
ES (1) ES2641643T3 (es)
GE (1) GEP20156251B (es)
HR (1) HRP20171660T1 (es)
HU (1) HUE036461T2 (es)
IL (1) IL222498A (es)
LT (1) LT2560972T (es)
MA (1) MA34229B1 (es)
MX (1) MX336056B (es)
MY (1) MY160780A (es)
NZ (2) NZ703538A (es)
PE (1) PE20130240A1 (es)
PL (1) PL2560972T3 (es)
PT (1) PT2560972T (es)
RS (1) RS56588B1 (es)
SG (2) SG10201505606QA (es)
SI (1) SI2560972T1 (es)
TW (2) TWI619713B (es)
UA (1) UA109128C2 (es)
UY (1) UY33346A (es)
WO (1) WO2011133637A2 (es)
ZA (1) ZA201207898B (es)

Families Citing this family (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US20100190777A1 (en) 2007-07-17 2010-07-29 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
PL2350075T3 (pl) 2008-09-22 2014-07-31 Array Biopharma Inc Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk
BRPI0919873B8 (pt) 2008-10-22 2021-05-25 Array Biopharma Inc compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas
CN105237530A (zh) 2009-04-03 2016-01-13 豪夫迈罗氏公司 丙烷-1-磺酸{3-[5-(4-氯-苯基)-1H-吡咯并[2,3-b]吡啶-3-羰基]-2,4-二氟-苯基}-酰胺组合物及其用途
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011057022A1 (en) 2009-11-06 2011-05-12 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
RU2012125070A (ru) 2009-11-18 2013-12-27 Плексксикон, Инк. Соединения и способы модулирования киназы и показания к их применению
RU2012131373A (ru) 2009-12-23 2014-01-27 Плексксикон, Инк. Соединения и способы модулирования киназы, а также показания для такого модулирования
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
LT3205654T (lt) 2010-05-20 2019-05-27 Array Biopharma, Inc. Makrocikliniai junginiai kaip trk kinazės slopikliai
PT2672967T (pt) 2011-02-07 2018-12-07 Plexxikon Inc Compostos e métodos de modulação da quinase e suas indicações
CN103534257A (zh) 2011-04-05 2014-01-22 辉瑞有限公司 作为原肌球蛋白相关激酶抑制剂的吡咯并[2,3-d]嘧啶衍生物
WO2012158957A2 (en) 2011-05-17 2012-11-22 Plexxikon Inc. Kinase modulation and indications therefor
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
WO2014018888A1 (en) 2012-07-26 2014-01-30 Confluence Life Sciences Inc. 4-alkoxy/aralkoxy-5-substituted-pyrrolopyrimidine compounds as tak1 inhibitors in disease treatment
WO2014039714A2 (en) 2012-09-06 2014-03-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP2912036A1 (en) 2012-10-04 2015-09-02 Pfizer Limited Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
CA2885253A1 (en) 2012-10-04 2014-04-10 Pfizer Limited Pyrrolo[2,3-d]pyrimidine tropomyosin-related kinase inhibitors
EP2903986A1 (en) 2012-10-04 2015-08-12 Pfizer Limited Tropomyosin-related kinase inhibitors
WO2014100620A2 (en) 2012-12-21 2014-06-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
MX2015012456A (es) 2013-03-15 2016-02-03 Plexxikon Inc Compuestos heterociclicos y usos de los mismos.
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
US10407509B2 (en) 2013-07-30 2019-09-10 Blueprint Medicines Corporation NTRK2 fusions
CA2934010A1 (en) 2013-12-20 2015-06-25 Pfizer Limited N-acylpiperidine ether tropomyosin-related kinase inhibitors
SG11201605242YA (en) 2014-01-10 2016-07-28 Biogen Ma Inc Factor viii chimeric proteins and uses thereof
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP3131891A1 (en) 2014-04-15 2017-02-22 Pfizer Inc. Tropomyosin-related kinase inhibitors containing both a 1h-pyrazole and a pyrimidine moiety
EP3140298A1 (en) 2014-05-07 2017-03-15 Pfizer Inc. Tropomyosin-related kinase inhibitors
WO2016009296A1 (en) 2014-07-16 2016-01-21 Pfizer Inc. N-acylpiperidine ether tropomyosin-related kinase inhibitors
WO2016020784A1 (en) 2014-08-05 2016-02-11 Pfizer Inc. N-acylpyrrolidine ether tropomyosin-related kinase inhibitors
JP6832846B2 (ja) 2014-09-15 2021-02-24 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ヘテロ環化合物およびその用途
PL3699181T3 (pl) 2014-11-16 2023-05-22 Array Biopharma, Inc. Postać krystaliczna wodorosiarczanu (s)-n-(5-((r)-2-(2,5-difluorofenylo) - pirolidyn-1-ylo)-pirazolo[1,5-a]pirimidyn-3-ylo)-3-hydroksypirolidyno-1-karboksyamidu
US20180263945A1 (en) * 2014-12-19 2018-09-20 Research Institute At Nationwide Children's Hospital Pyruvate compounds for treatment of peripheral neuropathy
EP3247353A4 (en) 2015-01-23 2018-07-04 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
WO2016164641A1 (en) 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
RU2730506C2 (ru) 2015-05-06 2020-08-24 Плексксикон Инк. Твердые формы соединения, модулирующего киназы
CA2984899C (en) * 2015-05-06 2021-06-15 Plexxikon Inc. Synthesis of 1 h-pyrrolo[2,3-b]pyridin derivatives that modulate kinases
CN107771178B (zh) 2015-05-22 2021-04-06 普莱希科公司 杂环化合物的合成
EP3303631A1 (en) 2015-06-01 2018-04-11 Loxo Oncology Inc. Methods of diagnosing and treating cancer
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG10201912386RA (en) 2015-09-21 2020-02-27 Plexxikon Inc Heterocyclic compounds and uses thereof
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US9938273B2 (en) 2015-12-07 2018-04-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
JP6921846B6 (ja) 2016-03-16 2021-09-15 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節およびその適応症のための化合物および方法
EP3439663B1 (en) 2016-04-04 2024-07-17 Loxo Oncology, Inc. Methods of treating pediatric cancers
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
GEP20227339B (en) 2016-04-04 2022-01-25 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)- pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydro-xypyrrolidine-1-carboxamide
AU2017264839B2 (en) * 2016-05-11 2021-08-05 Beta Pharma, Inc. 2-Anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
CA3024603A1 (en) 2016-05-18 2017-11-23 Charles Todd Eary Process for the preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof
US11020398B2 (en) * 2016-08-24 2021-06-01 Arqule, Inc. Amino-pyrrolopyrimidinone compounds and methods of use thereof
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
US20180153922A1 (en) 2016-12-06 2018-06-07 New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery Inhibition of expansion and function of pathogenic age-associated b cells and use for the prevention and treatment of autoimmune disease
EP3558991A2 (en) 2016-12-23 2019-10-30 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
WO2018136661A1 (en) 2017-01-18 2018-07-26 Andrews Steven W SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
TWI674260B (zh) 2017-02-01 2019-10-11 德商菲尼克斯製藥股份有限公司 芳基烴受體(AhR)調節劑化合物
TWI752155B (zh) 2017-02-01 2022-01-11 德商菲尼克斯製藥股份有限公司 芳香烴受體(AhR)調節劑化合物
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
JP2020511467A (ja) 2017-03-20 2020-04-16 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ブロモドメインを阻害する４−（１−（１，１−ジ（ピリジン−２−イル）エチル）−６−（３，５−ジメチルイソオキサゾール−４−イル）−１Ｈ−ピロロ［３，２−ｂ］ピリジン−３−イル）安息香酸の結晶形
WO2018226846A1 (en) 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
KR102615829B1 (ko) 2017-07-25 2023-12-20 플렉시콘 인코퍼레이티드 키나제를 조정하는 화합물의 제제
TW202410896A (zh) 2017-10-10 2024-03-16 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
EP3694855A1 (en) 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
MA50456A (fr) 2017-10-26 2020-09-02 Array Biopharma Inc Formulations d'un inhibiteur de kinase trk macrocyclique
CA3080197C (en) 2017-10-27 2023-12-19 Plexxikon Inc. Formulations of a compound modulating kinases
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
TWI802635B (zh) 2018-01-18 2023-05-21 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡咯并[2,3-d]嘧啶化合物
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
WO2019157119A1 (en) * 2018-02-07 2019-08-15 University Of Cincinnati System and method for detecting small blood-tissue barrier disruption
CN112119072A (zh) 2018-03-20 2020-12-22 普莱希科公司 用于ido和tdo调节的化合物和方法，以及其适应症
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
TW202015723A (zh) 2018-05-18 2020-05-01 美商百歐維拉提夫治療公司 治療ａ型血友病的方法
KR102129114B1 (ko) * 2018-07-26 2020-07-02 주식회사 온코파마텍 TrkA 저해 활성을 갖는 화합물 및 이를 유효성분으로 함유하는 통증의 예방 또는 치료용 약학적 조성물
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제
CN110833557A (zh) * 2018-08-15 2020-02-25 广西梧州制药（集团）股份有限公司 吡唑并嘧啶衍生物在治疗肾小管肾炎的用途
CN110833552A (zh) * 2018-08-15 2020-02-25 广西梧州制药（集团）股份有限公司 吡唑并嘧啶衍生物在治疗狼疮肾炎的用途
US11969472B2 (en) 2018-08-22 2024-04-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
CN118530239A (zh) 2018-08-22 2024-08-23 上海睿跃生物科技有限公司 原肌球蛋白受体激酶(trk)降解化合物及使用方法
CA3111984A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CA3136224A1 (en) 2019-04-09 2020-10-15 Plexxikon Inc. Condensed azines for ep300 or cbp modulation and indications therefor
CN110643672A (zh) * 2019-10-15 2020-01-03 西安交通大学 高表达TrkB作为新型靶点在抑制胰腺癌转移方面的医药用途
JP2023522949A (ja) 2020-04-23 2023-06-01 オプナ バイオ ソシエテ アノニム Ｃｄ７３調節のための化合物及び方法並びにそれらの表示
TW202212341A (zh) 2020-08-18 2022-04-01 美商英塞特公司 製備ｊａｋ１抑制劑之方法及中間體
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
WO2022040512A1 (en) 2020-08-21 2022-02-24 Plexxikon Inc. Combinational drug anticancer therapies
WO2023288197A1 (en) 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
CN114920744B (zh) * 2021-11-16 2024-05-07 中国药科大学 一种非共价btk激酶抑制剂及其生物用途
AU2023238511A1 (en) * 2022-03-25 2024-09-26 Jumbo Drug Bank Co., Ltd. Crystal form of 1h-pyrrolo[2,3-c]pyridine compound and preparation method therefor

Family Cites Families (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6316474B1 (en) 1999-10-29 2001-11-13 Merck & Co., Inc. 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists
PT1294724E (pt) * 2000-06-26 2006-07-31 Pfizer Prod Inc Compostos pirrolo (2,3-d ) pirimidina como agentes imunosupressivos
GB0107368D0 (en) * 2001-03-23 2001-05-16 Novartis Ag Organic compounds
EP1392300A1 (en) 2001-05-11 2004-03-03 Vertex Pharmaceuticals Incorporated 2,5-disubstituted pyridine, pyrimidine, pyridazine and 1, 2, 4-triazine derivatives for use as p38 inhibitors
GEP20063909B (en) 2002-01-22 2006-08-25 Warner Lambert Co 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d] PYRIMIDIN-7-ONES
US20040171062A1 (en) 2002-02-28 2004-09-02 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
CA2503905A1 (en) 2002-09-16 2004-03-25 Plexxikon, Inc. Crystal structure of pim-1 kinase
GB0226370D0 (en) 2002-11-12 2002-12-18 Novartis Ag Organic compounds
US20050048573A1 (en) 2003-02-03 2005-03-03 Plexxikon, Inc. PDE5A crystal structure and uses
SE0300456D0 (sv) 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
WO2004078923A2 (en) 2003-02-28 2004-09-16 Plexxikon, Inc. Pyk2 crystal structure and uses
US20050079548A1 (en) 2003-07-07 2005-04-14 Plexxikon, Inc. Ligand development using PDE4B crystal structures
ATE412650T1 (de) 2003-07-11 2008-11-15 Warner Lambert Co Isethionat salz eines selektiven cdk4 inhibitors
NZ545326A (en) 2003-07-17 2009-12-24 Plexxikon Inc PPAR active compounds
US7348338B2 (en) 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
WO2005028624A2 (en) 2003-09-15 2005-03-31 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
EP1696920B8 (en) 2003-12-19 2015-05-06 Plexxikon Inc. Compounds and methods for development of ret modulators
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
US7517970B2 (en) 2003-12-19 2009-04-14 Plexxikon, Inc. Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same
CN1918158B (zh) * 2004-02-14 2011-03-02 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
WO2005082904A1 (ja) * 2004-02-26 2005-09-09 Kyowa Hakko Kogyo Co., Ltd. 好中球性炎症疾患の予防及び／または治療剤
WO2006078287A2 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. Pde4b inhibitors and uses therefor
WO2005116035A1 (en) 2004-05-27 2005-12-08 Pfizer Products Inc. Pyrrolopyrimidine derivatives useful in cancer treatment
JP2008503473A (ja) 2004-06-17 2008-02-07 プレキシコン，インコーポレーテッド Ｃ−ｋｉｔ活性を調節する化合物
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
EP1786813A2 (en) 2004-09-03 2007-05-23 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
WO2006060535A2 (en) 2004-11-30 2006-06-08 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
JP2008521829A (ja) 2004-11-30 2008-06-26 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
US20060160135A1 (en) 2004-12-08 2006-07-20 Weiru Wang SF-1 and LRH-1 modulator development
UA93679C2 (en) * 2005-05-17 2011-03-10 Плексикон, Инк. Compounds modulating c-kit and c-fms activity and uses therefor
NZ563444A (en) 2005-05-17 2011-04-29 Plexxikon Inc Pyrrolo(2,3-b)pyridine derivatives as protein kinase inhibitors
NZ565255A (en) 2005-06-22 2010-04-30 Plexxikon Inc Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors
JP2009509932A (ja) 2005-09-07 2009-03-12 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
AU2006287521A1 (en) 2005-09-07 2007-03-15 Plexxikon, Inc. PPARactive compounds
US20070072904A1 (en) 2005-09-07 2007-03-29 Jack Lin PPAR active compounds
WO2008063888A2 (en) * 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US8093246B2 (en) 2006-12-14 2012-01-10 Lexicon Pharmaceuticals, Inc. O-linked pyrimidin-4-amine-based compounds, compositions comprising them, and methods of their use to treat cancer
US7872018B2 (en) 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
MX2009009290A (es) 2007-03-08 2009-09-10 Plexxikon Inc Compuestos activos en ppar.
PE20090159A1 (es) 2007-03-08 2009-02-21 Plexxikon Inc COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
CA2686379A1 (en) 2007-05-04 2008-11-13 Irm Llc Phenylaminopyrimidine derivatives and compositions thereof as c-kit and pdgfr kinase inhibitors
US20100190777A1 (en) 2007-07-17 2010-07-29 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
JO3240B1 (ar) * 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
ES2383331T3 (es) * 2008-02-22 2012-06-20 Irm Llc Compuestos heterocíclicos y composiciones como inhibidores de las Cinasas C-KIT y PDGFR INHIBITORS
WO2009115084A2 (de) 2008-03-20 2009-09-24 Schebo Biotech Ag Neue pyrrolopyrimidin-derivate und deren verwendungen
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US8110576B2 (en) 2008-06-10 2012-02-07 Plexxikon Inc. Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications
CN102112478A (zh) 2008-06-10 2011-06-29 普莱希科公司 用于激酶调节的5h-吡咯[2，3-b]吡嗪衍生物和其适应症
BRPI0917459B1 (pt) 2008-08-20 2017-09-12 Zoetis Services Llc N-methyl-1- [trans-4- [methyl (7h-pyrrol [2,3-d] pyridol [2,3-d] pyrimidine compounds, use of these in therapy and crystalline a form of n-methyl- pyrimidin-4-yl) amino] cyclohexyl} methanosulphonamide
BRPI0919873B8 (pt) 2008-10-22 2021-05-25 Array Biopharma Inc compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas
TW201036973A (en) 2009-03-11 2010-10-16 Plexxikon Inc Compounds and uses thereof
US8129404B2 (en) 2009-03-11 2012-03-06 Plexxikon Inc. Compounds and uses thereof
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
CN105237530A (zh) 2009-04-03 2016-01-13 豪夫迈罗氏公司 丙烷-1-磺酸{3-[5-(4-氯-苯基)-1H-吡咯并[2,3-b]吡啶-3-羰基]-2,4-二氟-苯基}-酰胺组合物及其用途
WO2010129467A1 (en) 2009-05-04 2010-11-11 Plexxikon, Inc. Compounds and methods for inhibition of renin, and indications therefor
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
WO2011057022A1 (en) 2009-11-06 2011-05-12 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
RU2012125070A (ru) 2009-11-18 2013-12-27 Плексксикон, Инк. Соединения и способы модулирования киназы и показания к их применению
RU2012131373A (ru) 2009-12-23 2014-01-27 Плексксикон, Инк. Соединения и способы модулирования киназы, а также показания для такого модулирования
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
US8642606B2 (en) 2010-09-29 2014-02-04 Plexxikon Inc. ZAP-70 active compounds
PT2672967T (pt) 2011-02-07 2018-12-07 Plexxikon Inc Compostos e métodos de modulação da quinase e suas indicações
WO2012158957A2 (en) 2011-05-17 2012-11-22 Plexxikon Inc. Kinase modulation and indications therefor
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
WO2014039714A2 (en) 2012-09-06 2014-03-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2014100620A2 (en) 2012-12-21 2014-06-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
MX2015012456A (es) 2013-03-15 2016-02-03 Plexxikon Inc Compuestos heterociclicos y usos de los mismos.
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor

Also Published As

Publication number Publication date
ES2641643T3 (es) 2017-11-10
CA2796998C (en) 2019-03-05
SG10201505606QA (en) 2015-08-28
US20110263595A1 (en) 2011-10-27
HRP20171660T1 (hr) 2017-12-15
JP2016028073A (ja) 2016-02-25
ZA201207898B (en) 2016-09-28
US20170283423A1 (en) 2017-10-05
CN102947305A (zh) 2013-02-27
IL222498A (en) 2016-10-31
WO2011133637A3 (en) 2012-02-09
CO6620045A2 (es) 2013-02-15
PL2560972T3 (pl) 2018-01-31
WO2011133637A2 (en) 2011-10-27
PE20130240A1 (es) 2013-03-04
ECSP12012245A (es) 2012-11-30
LT2560972T (lt) 2017-10-25
NZ603087A (en) 2015-01-30
TW201544506A (zh) 2015-12-01
US20150183793A1 (en) 2015-07-02
GEP20156251B (en) 2015-02-25
SG184874A1 (en) 2012-11-29
CY1120554T1 (el) 2019-07-10
US8901118B2 (en) 2014-12-02
TWI510487B (zh) 2015-12-01
EP2560972B1 (en) 2017-09-20
MY160780A (en) 2017-03-15
MX2012012197A (es) 2012-12-17
EA028105B1 (ru) 2017-10-31
JP5808793B2 (ja) 2015-11-10
JP2013525363A (ja) 2013-06-20
EP2560972A2 (en) 2013-02-27
HUE036461T2 (hu) 2018-07-30
EP2560972A4 (en) 2013-11-20
CL2012002937A1 (es) 2013-01-25
CR20120536A (es) 2013-02-01
MA34229B1 (fr) 2013-05-02
NZ703538A (en) 2016-11-25
AR115233A2 (es) 2020-12-09
BR112012026927A2 (pt) 2017-10-10
PT2560972T (pt) 2017-10-09
US9682981B2 (en) 2017-06-20
TW201136929A (en) 2011-11-01
AU2011242778A1 (en) 2012-11-22
RS56588B1 (sr) 2018-02-28
KR20130066621A (ko) 2013-06-20
MX336056B (es) 2016-01-07
UY33346A (es) 2011-10-31
SI2560972T1 (sl) 2017-12-29
DK2560972T3 (da) 2017-11-27
EA201290973A1 (ru) 2013-04-30
CA2796998A1 (en) 2011-10-27
CN102947305B (zh) 2016-07-06
AU2011242778B2 (en) 2015-09-03
TWI619713B (zh) 2018-04-01
KR101799126B1 (ko) 2017-11-17
UA109128C2 (ru) 2015-07-27

Similar Documents

Publication Publication Date Title
AR080940A1 (es) Compuestos heterociclicos utiles como inhibidores de quinasa
AR078920A1 (es) Compuestos de pirrolopiridina como moduladores de quinasas. procesos de obtencion y composiciones farmaceuticas.
ES2684268T3 (es) Inhibidores de pirimidinil tirosina quinasa
PE20200447A1 (es) Compuestos de biheteroarilo y usos de los mismos
HRP20140437T1 (hr) Bicikliäśki spojevi i njihove uporabe kao dualnih c-src/jak inhibitora
AR094299A1 (es) Derivados de ftalazin-1(2h)-ona sustituidos
AR082886A1 (es) Compuestos y composiciones farmaceuticas que los contienen
ES2618003T3 (es) Compuestos tricíclicos sustituidos como inhibidores de FGFR
AR088449A1 (es) Benzilindazoles sustituidos
CO6321244A2 (es) Pirrolopiridinas como inhibidores de cinasa
PE20160523A1 (es) Derivados de arilo o heteroarilo como inhibidores de moleculas pequenas de fibrosis
AR090203A1 (es) Compuestos heterobiciclicos como inhibidores de pde10
AR082885A1 (es) Compuestos y composiciones para la inhibicion de nampt
RU2013143746A (ru) 1,4-оксазепины в качестве ингибиторов васе1 и(или) васе2
JP2022536773A (ja) 置換ピラゾロピラジン及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用
AR096119A1 (es) Derivados 2-fenil- o 2- hetaril-imidazol[1,2-a]piridina
CY1116769T1 (el) Υποκατεστhmενα παραγωγα βενζαμιδιου
AR084515A1 (es) Derivados heterociclicos nitrogenados, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades asociadas al sistema nervioso central tales como parkinson y alzheimer, entre otras
MX2021011971A (es) Proceso para preparar cicloserinas sustituidas.
AR097721A1 (es) Derivados de etinilo
BR112013000253A2 (pt) derivados de (3-metilpirrolidin-3-il) metil piridinil éter e seu uso como antagonistas do receptor nk-3
MX2013007411A (es) Derivados de pirrolidina como antagonistas del receptor de neuroquinina 3 (nk3).
US9969735B2 (en) Process for making tricyclic lactam compounds
AR074213A1 (es) Derivados de la espirociclobutilpiperidina
AR094898A1 (es) Compuestos de carboxamida y sus usos como nematicidas

Legal Events

Date Code Title Description
FC Refusal