[go: up one dir, main page]

SG10201407453TA - Kinase inhibitors - Google Patents

Kinase inhibitors

Info

Publication number
SG10201407453TA
SG10201407453TA SG10201407453TA SG10201407453TA SG10201407453TA SG 10201407453T A SG10201407453T A SG 10201407453TA SG 10201407453T A SG10201407453T A SG 10201407453TA SG 10201407453T A SG10201407453T A SG 10201407453TA SG 10201407453T A SG10201407453T A SG 10201407453TA
Authority
SG
Singapore
Prior art keywords
provides
protein kinase
present
kinase inhibitors
pyrropyrimidine
Prior art date
Application number
SG10201407453TA
Inventor
Jaekyoo Lee
Ho-Juhn Song
Jong Sung Koh
Hee Kyu Lee
Youngsam Kim
Hong Woo Kim
Sunhwa Chang
Sun-Hee Lim
Jang-Sik Choi
Jung-Ho Kim
Se-Won Kim
Original Assignee
Genosco
Oscotec 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
Application filed by Genosco, Oscotec Inc filed Critical Genosco
Publication of SG10201407453TA publication Critical patent/SG10201407453TA/en

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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P11/00—Drugs for disorders of the respiratory 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

Landscapes

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

Abstract

- 125 - KINASE INHIBITORS Abstract The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutical^ acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives. Figure: None
SG10201407453TA 2009-11-13 2010-11-12 Kinase inhibitors SG10201407453TA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26110009P 2009-11-13 2009-11-13

Publications (1)

Publication Number Publication Date
SG10201407453TA true SG10201407453TA (en) 2014-12-30

Family

ID=43992073

Family Applications (1)

Application Number Title Priority Date Filing Date
SG10201407453TA SG10201407453TA (en) 2009-11-13 2010-11-12 Kinase inhibitors

Country Status (16)

Country Link
US (1) US8629132B2 (en)
EP (1) EP2498607B1 (en)
JP (1) JP5740409B2 (en)
KR (1) KR101663637B1 (en)
CN (1) CN102811619B (en)
BR (1) BR112012011287B1 (en)
CA (1) CA2780892C (en)
CL (1) CL2012001221A1 (en)
EA (1) EA024729B1 (en)
IL (1) IL219726A (en)
MX (1) MX2012005332A (en)
MY (1) MY160820A (en)
NZ (1) NZ599041A (en)
SG (1) SG10201407453TA (en)
WO (1) WO2011060295A1 (en)
ZA (1) ZA201204246B (en)

Families Citing this family (107)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105693720B (en) 2010-05-20 2019-01-18 阵列生物制药公司 Macrocyclic compound as TRK kinase inhibitor
HUE029196T2 (en) 2010-06-04 2017-02-28 Hoffmann La Roche Aminopyrimidine derivatives as lrrk2 modulators
BR112013011600B1 (en) 2010-11-10 2022-01-11 Genentech, Inc PYRAZOLE AMINOPYRIMIDINE DERIVATIVES, THEIR USE AND COMPOSITION INCLUDING THEM
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
WO2013054351A1 (en) * 2011-08-08 2013-04-18 Cadila Healthcare Limited Heterocyclic compounds
JP2014524456A (en) * 2011-08-25 2014-09-22 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Serine / threonine PAK1 inhibitor
WO2013092940A1 (en) * 2011-12-22 2013-06-27 F. Hoffmann-La Roche Ag 2, 4-diamine-pyrimidine derivative as serine/threonine kinase inhibitors
CN104203943B (en) * 2012-01-20 2017-12-29 盖诺斯克公司 Substituted pyrimidine compound and its purposes as SYK inhibitor
US9096579B2 (en) * 2012-04-20 2015-08-04 Boehringer Ingelheim International Gmbh Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments
CA2870339C (en) 2012-05-15 2020-06-02 Novartis Ag Compounds and compositions for inhibiting the activity of abl1, abl2 and bcr-abl1
BR112014027181A2 (en) 2012-05-15 2017-06-27 Novartis Ag benzamide derivatives for inhibition of abl1, abl2 and bcr-abl1 activity
ES2665539T3 (en) 2012-05-15 2018-04-26 Novartis Ag Benzamide derivatives to inhibit the activity of ABL1, ABL2 and BCR-ABL1
PL2861579T3 (en) 2012-05-15 2018-07-31 Novartis Ag Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1
ES2984771T3 (en) 2012-06-13 2024-10-31 Incyte Holdings Corp Substituted tricyclic compounds as FGFR inhibitors
KR20150027267A (en) 2012-06-29 2015-03-11 화이자 인코포레이티드 NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
JP6437452B2 (en) 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
ME03780B (en) 2013-01-15 2021-04-20 Incyte Holdings Corp THIAZOLE CARBOXAMIDE DERIVATIVES AND PYRIDINE CARBOXAMIDE DERIVATIVES USED AS PIM KINASE INHIBITORS
WO2014134772A1 (en) * 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
EA035095B1 (en) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Bicyclic heterocycles as fgfr inhibitors
CN103232394B (en) * 2013-05-14 2014-09-24 浙江医药高等专科学校 Pyrazole-containing compound, its preparation method and use
CN103382198B (en) * 2013-07-16 2014-11-19 浙江医药高等专科学校 Pyrazole amide compound, its preparation method and use
CN103382202B (en) * 2013-07-16 2014-11-26 浙江医药高等专科学校 Compound containing furan substitute and preparation method and use thereof
CN103387569B (en) * 2013-07-16 2014-09-24 浙江医药高等专科学校 A class of antitumor compound, its preparation method and use
CN103387568B (en) * 2013-07-16 2014-11-05 浙江医药高等专科学校 Compounds, preparation method thereof and applications thereof
CN103396400B (en) * 2013-07-16 2014-12-17 浙江医药高等专科学校 Pyrazole-containing amide compound, its preparation method and use
CN103420993B (en) * 2013-07-16 2014-12-17 浙江医药高等专科学校 Compound containing thiophene substitution, its preparation method and use
CN104341437A (en) * 2013-07-30 2015-02-11 山东亨利医药科技有限责任公司 SYK inhibitor containing bicyclo-radical
EA201690458A1 (en) 2013-08-23 2016-07-29 Инсайт Корпорейшн FURO- AND THYENOPYRIDINCARBOXAMIDES USED AS PIM-KINASE INHIBITORS
ES2890552T3 (en) * 2013-10-21 2022-01-20 Genosco Substituted Pyrimidine Compounds and Their Use as SYK Inhibitors
TW201601632A (en) * 2013-11-20 2016-01-16 杜邦股份有限公司 1-aryl-3-alkylpyrazole insecticide
US9695171B2 (en) 2013-12-17 2017-07-04 Pfizer Inc. 3,4-disubstituted-1 H-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazines as LRRK2 inhibitors
CN104974091B (en) * 2014-04-10 2018-01-02 沈阳药科大学 Diaryl pyrazole azole compound of 3 methyl 1,5 and its production and use
EP3166637B1 (en) 2014-07-10 2020-01-29 The J. David Gladstone Institutes Compositions and methods for treating dengue virus infection
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
KR101633722B1 (en) * 2014-10-08 2016-06-28 한국화학연구원 4-(1-pyrrole-3,4-dicarboxamide)pyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating cancer containing the same as an active ingredient
HRP20250213T1 (en) 2014-10-13 2025-04-25 Yuhan Corporation COMPOUNDS AND PREPARATIONS FOR MODULATING EGFR MUTANT KINASE ACTIVITY
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CN104788427B (en) * 2015-02-05 2017-05-31 上海泓博智源医药股份有限公司 3 (2 pyrimdinyl-amino) phenylacryloyl amine compounds and its application
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
MA41551A (en) 2015-02-20 2017-12-26 Incyte Corp BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EA038045B1 (en) 2015-02-20 2021-06-28 Инсайт Корпорейшн Bicyclic heterocycles as fgfr inhibitors
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
FI3307727T3 (en) * 2015-06-15 2024-01-08 Asana Biosciences Llc Heterocyclic inhibitors of erk1 and erk2 and their use in the treatment of cancer
EP3322706B1 (en) 2015-07-16 2020-11-11 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
AR105967A1 (en) 2015-09-09 2017-11-29 Incyte Corp SALTS OF A PIM QUINASA INHIBITOR
JP6873980B2 (en) 2015-09-14 2021-05-19 ファイザー・インク Novel imidazole [4,5-c] quinoline and imidazole [4,5-c] [1,5] naphthylidine derivatives as LRRK2 inhibitors
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
TWI757256B (en) 2015-11-02 2022-03-11 美商纜圖藥品公司 Inhibitors of ret
WO2017087905A1 (en) 2015-11-20 2017-05-26 Denali Therapeutics Inc. Compound, compositions, and methods
US11028080B2 (en) 2016-03-11 2021-06-08 Denali Therapeutics Inc. Substituted pyrimidines as LRKK2 inhibitors
TW201738228A (en) 2016-03-17 2017-11-01 藍圖醫藥公司 Inhibitors of RET
CN109311857B (en) 2016-06-16 2021-11-12 戴纳立制药公司 Pyrimidin-2-ylamino-1H-pyrazoles as LRRK2 inhibitors for the treatment of neurodegenerative disorders
US10227329B2 (en) 2016-07-22 2019-03-12 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
WO2018022761A1 (en) 2016-07-27 2018-02-01 Blueprint Medicines Corporation Substituted cyclopentane-amides for treating disorders related to ret
TWI704148B (en) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
JOP20190077A1 (en) 2016-10-10 2019-04-09 Array Biopharma Inc Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
CN116283910A (en) * 2016-12-15 2023-06-23 阿瑞雅德制药公司 Benzimidazole compounds as C-KIT inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CN110267960B (en) 2017-01-18 2022-04-26 阿雷生物药品公司 Substituted pyrazolo [1,5-a ] pyrazine compounds as RET kinase inhibitors
BR112019015252A2 (en) * 2017-01-25 2020-04-14 Glaxosmithkline Ip Dev Ltd compounds
JOP20190213A1 (en) 2017-03-16 2019-09-16 Array Biopharma Inc Macrocyclic compounds as ros1 kinase inhibitors
AR111469A1 (en) * 2017-04-21 2019-07-17 Yuhan Corp COME OUT OF AN AMINOPIRIDINE DERIVATIVE COMPOUND, A CRYSTAL FORM OF THE SAME, AND A PROCESS TO PREPARE THE SAME
AR111960A1 (en) 2017-05-26 2019-09-04 Incyte Corp CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION
WO2018226739A1 (en) * 2017-06-06 2018-12-13 Signalrx Pharmaceuticals, Inc. Thienopyranones and furanopyranones as checkpoint inhibitors and modulatiors of anti-tumor immunity
DK3658552T3 (en) 2017-07-28 2023-11-20 Yuhan Corp PROCEDURE FOR THE PREPARATION OF N-(5-((4-(4-((DIMETHYLAMINO)METHYL)-3-PHENYL-1H-PYRAZOL-1-YL)PYRIMIDIN-2-YL)AMINO)-4-METHOXY-2- MORPHOLINOPHENYL)ACRYLAMIDE BY REACTION OF THE CORRESPONDING AMINE WITH A 3-HALOGEN-PROPIONYL CHLORIDE
HUE059501T2 (en) * 2017-07-28 2022-11-28 Yuhan Corp Intermediates suitable for the production of aminopyrimidine derivatives, a process for their production, and a process for the production of aminopyrimidine derivatives using them
PT3658547T (en) 2017-07-28 2023-10-20 Yuhan Corp Intermediates useful for the synthesis of a selective inhibitor against protein kinase and processes for preparing the same
TWI791053B (en) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 Crystalline forms of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile and pharmaceutical composition thereof
TWI812649B (en) 2017-10-10 2023-08-21 美商絡速藥業公司 Formulations of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
CN111971286B (en) 2018-01-18 2023-04-14 阿雷生物药品公司 Substituted pyrrolo[2,3-d]pyrimidine compounds as RET kinase inhibitors
TW201938169A (en) 2018-01-18 2019-10-01 美商亞雷生物製藥股份有限公司 Substituted pyrazolo[3,4-d]pyrimidine compounds as RET kinase inhibitors
JP7422084B2 (en) 2018-04-03 2024-01-25 ブループリント メディシンズ コーポレイション RET inhibitors for use in the treatment of cancers with RET alterations
RS66310B1 (en) 2018-05-04 2025-01-31 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
KR20190131981A (en) * 2018-05-18 2019-11-27 재단법인 대구경북첨단의료산업진흥재단 Pharmaceutical composition for use in preventing or treating Traumatic Brain Injury or stroke
WO2019227226A1 (en) 2018-06-01 2019-12-05 University Of Saskatchewan Phytochemical-antibiotic combination for the treatment of a bacterial infection
ES2922314T3 (en) 2018-09-10 2022-09-13 Array Biopharma Inc Fused Heterocyclic Compounds as RET Kinase Inhibitors
CN111285882B (en) * 2018-12-07 2022-12-02 四川科伦博泰生物医药股份有限公司 Fused ring compound, pharmaceutical composition containing same, and preparation method and application thereof
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2020222188A1 (en) 2019-05-01 2020-11-05 Clexio Biosciences Ltd. Methods of treating pruritus
CN112142731B (en) * 2019-06-28 2022-07-22 成都赜灵生物医药科技有限公司 2, 4-disubstituted pyrimidine derivative and preparation method and application thereof
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TWI759829B (en) 2019-08-23 2022-04-01 財團法人生物技術開發中心 Heterocyclic pyrazole derivatives as type iii receptor tyrosine kinase inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
PH12022550892A1 (en) 2019-10-14 2023-05-03 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP7738550B2 (en) * 2019-10-28 2025-09-12 アサナ バイオサイエンシズ，リミティド ライアビリティ カンパニー Improved methods, kits, compositions, and administration regimens for the use of heterocyclic inhibitors of ERK1 and ERK2
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
BR112022011834A2 (en) * 2019-12-16 2022-08-30 Korea Res Inst Chemical Tech PYRIMIDINE DERIVATIVE AND USE THEREOF
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3183728A1 (en) 2020-05-29 2021-12-02 Blueprint Medicines Corporation Solid forms of pralsetinib
CN116323595B (en) * 2020-09-23 2025-08-19 内尔维亚诺医疗科学公司 Pyrazolyl-pyrimidine derivatives as kinase inhibitors
US20240174679A1 (en) * 2021-03-17 2024-05-30 Merck Sharp & Dohme Llc Heteroaroyl amides as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof
JP2024513575A (en) 2021-04-12 2024-03-26 インサイト・コーポレイション Combination therapy including FGFR inhibitor and Nectin-4 targeting agent
CN115368364B (en) * 2021-05-19 2024-07-16 四川大学 7H-pyrrolo [2,3-d ] pyrimidine derivatives, preparation method and application thereof
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313610A (en) 2021-06-09 2023-04-01 美商英塞特公司 Tricyclic heterocycles as fgfr inhibitors
CN117813299A (en) * 2021-08-27 2024-04-02 上海翰森生物医药科技有限公司 Nitrogen-containing heterocyclic derivative inhibitors, preparation methods and applications thereof
WO2023076404A1 (en) 2021-10-27 2023-05-04 Aria Pharmaceuticals, Inc. Methods for treating systemic lupus erythematosus
KR102654662B1 (en) * 2022-06-13 2024-04-05 주식회사 이앤피 Development of a novel pharmaceutics (Plk3 inhibitor) and related materials thereof

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2278677A1 (en) * 1997-01-27 1998-07-30 Daiichi Pharmaceutical Co., Ltd. Pyrazole derivatives
US20030004174A9 (en) 2000-02-17 2003-01-02 Armistead David M. Kinase inhibitors
WO2004035604A2 (en) 2002-10-16 2004-04-29 Millennium Pharmaceuticals, Inc. Spleen tyrosine kinase catalytic domain:crystal structure and binding pockets thereof
GB0308466D0 (en) * 2003-04-11 2003-05-21 Novartis Ag Organic compounds
JP2006527230A (en) * 2003-06-13 2006-11-30 ノバルティス アクチエンゲゼルシャフト 2-Aminopyrimidine derivatives as RAF kinase inhibitors
JP2008525461A (en) * 2004-12-23 2008-07-17 バーテックス ファーマシューティカルズ インコーポレイテッド Selective inhibitor of ERK protein kinase and use thereof
EP1948659A1 (en) * 2005-10-13 2008-07-30 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
JP2009538352A (en) * 2006-05-26 2009-11-05 アストラゼネカ アクチボラグ 2-Carbocycloamino-4-imidazolylpyrimidines as agents for inhibiting cell proliferation
JP2009541318A (en) * 2006-06-22 2009-11-26 メルク エンド カムパニー インコーポレーテッド Tyrosine kinase inhibitor
WO2008068171A1 (en) * 2006-12-08 2008-06-12 F. Hoffmann-La Roche Ag Substituted pyrimidines and their use as jnk modulators
WO2009012647A1 (en) * 2007-07-20 2009-01-29 Shanghai Hengrui Pharmaceutical Co., Ltd. Preparation methods of quinazoline derivatives and their pharmaceutical uses
WO2009032703A1 (en) * 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
GB0719644D0 (en) * 2007-10-05 2007-11-14 Cancer Rec Tech Ltd Therapeutic compounds and their use

Also Published As

Publication number Publication date
CL2012001221A1 (en) 2013-06-07
CA2780892A1 (en) 2011-05-19
NZ599041A (en) 2014-05-30
AU2010319382A1 (en) 2012-04-19
US8629132B2 (en) 2014-01-14
KR20130006417A (en) 2013-01-16
ZA201204246B (en) 2013-09-25
WO2011060295A8 (en) 2011-10-27
EP2498607A1 (en) 2012-09-19
KR101663637B1 (en) 2016-10-07
CN102811619A (en) 2012-12-05
CN102811619B (en) 2015-04-22
MY160820A (en) 2017-03-31
JP5740409B2 (en) 2015-06-24
IL219726A0 (en) 2012-07-31
IL219726A (en) 2016-04-21
EP2498607B1 (en) 2016-02-17
CA2780892C (en) 2017-02-14
EA024729B1 (en) 2016-10-31
US20110281841A1 (en) 2011-11-17
WO2011060295A1 (en) 2011-05-19
MX2012005332A (en) 2012-10-15
JP2013510876A (en) 2013-03-28
EA201290324A1 (en) 2012-12-28
HK1179477A1 (en) 2013-10-04
BR112012011287B1 (en) 2022-02-08
BR112012011287A2 (en) 2020-09-01
EP2498607A4 (en) 2013-06-19

Similar Documents

Publication Publication Date Title
SG10201407453TA (en) Kinase inhibitors
MY173494A (en) Kinase inhibitors
PH12017500488A1 (en) Compounds and compositions for modulating egfr mutant kinase activities
CY1121433T1 (en) PRODUCTS OF BICYCLE HETEROCYCLES AS INHIBITORS IRAK4
MX347040B (en) Tyrosine kinase inhibitors.
MX2013012588A (en) Kinase inhibitors.
MX2013012776A (en) Amino-pyridine-containing spleen tyrosine kinase (syk) inhibitors.
PH12012502102A1 (en) Fused bicyclic kinase inhibitors
NZ630925A (en) Pyrazolopyrimidine compounds as kinase inhibitors
WO2014125408A3 (en) Substituted 1h-pyrrolopyridinone derivatives as kinase inhibitors
PH12015500719A1 (en) Gdf-8-inhibitors
MX352672B (en) Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer.
MY199894A (en) Prmt5 inhibitors and uses thereof
PH12014501695B1 (en) Pde9 inhibitors with imidazo triazinone backbone
MX346186B (en) Protein kinase inhibitors.
MX2009014013A (en) Pyrimidyl cyclopentanes as akt protein kinase inhibitors.
IN2012DN03085A (en)
MY165902A (en) Substituted pyridine derivatives as fabi inhibitors
WO2014106800A8 (en) Substituted 2-amino pyrimidine derivatives as kinase inhibitors
NZ610353A (en) Imidazole derivatives as pde10a enzyme inhibitors
MX2010007546A (en) Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor.
UA100545C2 (en) Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
MX347928B (en) Phenethylsulfone isoindoline derivatives as inhibitors of pde 4 and/or cytokines.
EA201001566A1 (en) NEW CLASS OF SPYROPIPERIDINES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
EA201071307A1 (en) CARBAMOIC DERIVATIVES OF BICYCLIC CARBONYLAMINOPYRAZOLE AS A MEDICINE