CN102603581B - 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 - Google Patents

作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 Download PDF

Info

Publication number
CN102603581B
CN102603581B CN201210012143.5A CN201210012143A CN102603581B CN 102603581 B CN102603581 B CN 102603581B CN 201210012143 A CN201210012143 A CN 201210012143A CN 102603581 B CN102603581 B CN 102603581B
Authority
CN
China
Prior art keywords
nhr
low
carbon
alkyl
fluorine
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201210012143.5A
Other languages
English (en)
Chinese (zh)
Other versions
CN102603581A (zh
Inventor
P·N·伊布拉赫姆
D·R·阿提斯
R·布莱姆
S·玛莫
M·那斯比
C·张
J·张
Y-L·朱
J·蔡
K-P·海那斯
G·博拉格
W·斯普瓦克
H·周
S·J·吉勒提
G·吴
H·朱
S·石
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Plexxikon Inc
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=37033831&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102603581(B) "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 CN102603581A publication Critical patent/CN102603581A/zh
Application granted granted Critical
Publication of CN102603581B publication Critical patent/CN102603581B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10—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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C37/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring
    • C07C37/62—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
    • C07C39/24—Halogenated derivatives
    • C07C39/26—Halogenated derivatives monocyclic monohydroxylic containing halogen bound to ring carbon atoms
    • C07C39/27—Halogenated derivatives monocyclic monohydroxylic containing halogen bound to ring carbon atoms all halogen atoms being bound to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/673—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
    • C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/56—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing hydroxy groups
    • C07C47/565—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing hydroxy groups all hydroxy groups bound to the ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/575—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
CN201210012143.5A 2005-06-22 2006-06-21 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 Active CN102603581B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US69296005P 2005-06-22 2005-06-22
US60/692,960 2005-06-22
US73152805P 2005-10-28 2005-10-28
US60/731,528 2005-10-28

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN2006800303262A Division CN101243084B (zh) 2005-06-22 2006-06-21 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物

Publications (2)

Publication Number Publication Date
CN102603581A CN102603581A (zh) 2012-07-25
CN102603581B true CN102603581B (zh) 2015-06-24

Family

ID=37033831

Family Applications (3)

Application Number Title Priority Date Filing Date
CN201110084299.XA Active CN102206216B (zh) 2005-06-22 2006-06-21 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
CN2006800303262A Active CN101243084B (zh) 2005-06-22 2006-06-21 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
CN201210012143.5A Active CN102603581B (zh) 2005-06-22 2006-06-21 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物

Family Applications Before (2)

Application Number Title Priority Date Filing Date
CN201110084299.XA Active CN102206216B (zh) 2005-06-22 2006-06-21 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
CN2006800303262A Active CN101243084B (zh) 2005-06-22 2006-06-21 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物

Country Status (35)

Country Link
US (10) US7863288B2 (US07863288-20110104-C00114.png)
EP (3) EP2395004B1 (US07863288-20110104-C00114.png)
JP (1) JP5007304B2 (US07863288-20110104-C00114.png)
KR (1) KR101125919B1 (US07863288-20110104-C00114.png)
CN (3) CN102206216B (US07863288-20110104-C00114.png)
AR (2) AR054624A1 (US07863288-20110104-C00114.png)
AT (1) ATE518860T1 (US07863288-20110104-C00114.png)
AU (1) AU2006261993B2 (US07863288-20110104-C00114.png)
BR (1) BRPI0611863B1 (US07863288-20110104-C00114.png)
CA (1) CA2613015C (US07863288-20110104-C00114.png)
CR (2) CR9677A (US07863288-20110104-C00114.png)
CY (2) CY1111996T1 (US07863288-20110104-C00114.png)
DE (1) DE122012000043I1 (US07863288-20110104-C00114.png)
DK (2) DK2395004T3 (US07863288-20110104-C00114.png)
EC (1) ECSP088121A (US07863288-20110104-C00114.png)
ES (2) ES2371397T3 (US07863288-20110104-C00114.png)
HK (2) HK1114610A1 (US07863288-20110104-C00114.png)
HU (2) HUE027370T2 (US07863288-20110104-C00114.png)
IL (1) IL188248A (US07863288-20110104-C00114.png)
LU (1) LU92035I2 (US07863288-20110104-C00114.png)
MA (1) MA29612B1 (US07863288-20110104-C00114.png)
MX (1) MX2007016463A (US07863288-20110104-C00114.png)
MY (2) MY153898A (US07863288-20110104-C00114.png)
NO (2) NO333913B1 (US07863288-20110104-C00114.png)
NZ (1) NZ565255A (US07863288-20110104-C00114.png)
PE (1) PE20070100A1 (US07863288-20110104-C00114.png)
PL (2) PL2395004T3 (US07863288-20110104-C00114.png)
PT (1) PT1893612E (US07863288-20110104-C00114.png)
RS (1) RS52010B (US07863288-20110104-C00114.png)
RU (3) RU2565071C2 (US07863288-20110104-C00114.png)
SI (2) SI1893612T1 (US07863288-20110104-C00114.png)
TW (3) TWI432193B (US07863288-20110104-C00114.png)
UA (1) UA95244C2 (US07863288-20110104-C00114.png)
WO (2) WO2007002325A1 (US07863288-20110104-C00114.png)
ZA (4) ZA200711152B (US07863288-20110104-C00114.png)

Families Citing this family (409)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2550361C (en) 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
US7507826B2 (en) 2004-03-30 2009-03-24 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
KR20070053205A (ko) 2004-09-17 2007-05-23 에자이 알앤드디 매니지먼트 가부시키가이샤 의약 조성물
US7846941B2 (en) 2005-05-17 2010-12-07 Plexxikon, Inc. Compounds modulating c-kit and c-fms activity and uses therefor
MY153898A (en) * 2005-06-22 2015-04-15 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
CA2615291A1 (en) 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
EP2251341A1 (en) 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
EP1925676A4 (en) 2005-08-02 2010-11-10 Eisai R&D Man Co Ltd TEST METHOD FOR THE EFFECT OF A VASCULARIZATION INHIBITOR
CA2620594C (en) * 2005-09-01 2012-08-21 Eisai R&D Management Co., Ltd. Pharmaceutical composition having improved disintegratability
RS54181B9 (sr) 2005-12-13 2020-01-31 Incyte Holdings Corp Heteroaril supstituisani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze
EP2559694A3 (en) 2006-01-17 2013-04-03 Vertex Pharmaceuticals, Inc. Azaindoles useful as inhibitors of Janus kinases
WO2007084667A2 (en) * 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
WO2007116866A1 (ja) 2006-04-03 2007-10-18 Astellas Pharma Inc. ヘテロ化合物
CN101443009A (zh) 2006-05-18 2009-05-27 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
WO2007135398A1 (en) * 2006-05-22 2007-11-29 Astrazeneca Ab Indole derivatives
US7964728B2 (en) 2006-07-06 2011-06-21 Solvay Pharmaceuticals B.V. Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition
ATE526327T1 (de) * 2006-07-06 2011-10-15 Abbott Healthcare Products Bv Azaindolderivate mit einer kombination eines teilweisen agonismus am nikotinischen acetylcholinrezeptor und einer inhibierung der dopaminwiederaufnahme
GB0617161D0 (en) * 2006-08-31 2006-10-11 Vernalis R&D Ltd Enzyme inhibitors
EP2530083B1 (en) 2006-09-22 2016-04-27 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
AU2007336811A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
EP2815750A1 (en) 2006-12-21 2014-12-24 Vertex Pharmaceuticals Incorporated 5-cyano-4-(pyrrolo [2,3b] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors
PE20121126A1 (es) * 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
US20120101114A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
SG10202107066WA (en) * 2007-03-28 2021-07-29 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
US8715665B2 (en) 2007-04-13 2014-05-06 The General Hospital Corporation Methods for treating cancer resistant to ErbB therapeutics
GB0710528D0 (en) * 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
MY154969A (en) 2007-06-13 2015-08-28 Incyte Corp Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
CN101808994B (zh) * 2007-07-17 2013-05-15 普莱希科公司 用于激酶调节的化合物和方法以及其适应症
MX2010001636A (es) * 2007-08-14 2010-03-15 Hoffmann La Roche Derivados de pirazolo[3,4-d]-pirimidina como agentes antiproliferativos.
EP2184988B1 (en) 2007-08-17 2014-12-17 University of Maryland, Baltimore Small molecule inhibitors of lck sh2 domain binding
CA2639416C (en) 2007-09-11 2019-12-31 F. Hoffmann-La Roche Ag Diagnostic test for susceptibility to b-raf kinase inhibitors
DE102007045919B4 (de) 2007-09-26 2018-07-05 Bayer Intellectual Property Gmbh Wirkstoffkombinationen mit insektiziden und akariziden Eigenschaften
DE102007045956A1 (de) 2007-09-26 2009-04-09 Bayer Cropscience Ag Wirkstoffkombination mit insektiziden und akariziden Eigenschaften
CA2703125C (en) 2007-10-25 2012-08-28 David J. Guerin Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer
JP5608097B2 (ja) 2008-01-08 2014-10-15 アレイ バイオファーマ、インコーポレイテッド キナーゼ阻害薬としてのピロロピリジン
US8426396B2 (en) * 2008-01-08 2013-04-23 Shriners Hospitals For Children Treatment for achondroplasia
CA2711741A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Pyrazolopyridines as kinase inhibitors
EA020885B1 (ru) * 2008-01-22 2015-02-27 Мерк Патент Гмбх Ингибиторы протеинкиназы и их применение
WO2009106445A1 (en) * 2008-02-25 2009-09-03 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
CN102015707A (zh) 2008-02-29 2011-04-13 阵列生物制药公司 Raf抑制剂化合物及其使用方法
WO2009111279A1 (en) 2008-02-29 2009-09-11 Array Biopharma Inc. Pyrazole [3, 4-b] pyridine raf inhibitors
CA2716949A1 (en) 2008-02-29 2009-09-11 Array Biopharma Inc. N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20110065577A1 (en) * 2008-05-21 2011-03-17 Basf Se Substituted pyridin-4-yl-methyl sulfonamides as fungicides
JP2011521924A (ja) * 2008-05-28 2011-07-28 ビーエーエスエフ ソシエタス・ヨーロピア 殺菌剤としての置換ピリジン−４−イル−メチルスルホンアミド
WO2009152083A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. 5h-pyrr0l0 [2,3-b] pyrazine derivatives 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
AR072008A1 (es) * 2008-06-13 2010-07-28 Merck & Co Inc Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38
US9447049B2 (en) 2010-03-01 2016-09-20 University Of Tennessee Research Foundation Compounds for treatment of cancer
JPWO2009157196A1 (ja) 2008-06-25 2011-12-08 武田薬品工業株式会社 アミド化合物
EP3311818A3 (en) 2008-07-16 2018-07-18 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
DE102008052943A1 (de) 2008-10-23 2010-04-29 Merck Patent Gmbh Azaindolderivate
EP2356116A1 (en) * 2008-11-20 2011-08-17 OSI Pharmaceuticals, Inc. Substituted pyrroloý2,3-b¨-pyridines and-pyrazines
AU2009324894B2 (en) * 2008-11-25 2015-04-09 University Of Rochester MLK inhibitors and methods of use
US8318446B2 (en) * 2008-12-05 2012-11-27 California Institute Of Technology DNA-damage-induced proteolysis
CN102307873B (zh) * 2009-02-10 2016-01-20 孟山都技术有限公司 用于控制线虫的组合物和方法
KR20110130463A (ko) * 2009-03-11 2011-12-05 플렉시콘, 인코퍼레이티드 Ｒａｆ 키나제의 억제를 위한 피롤로［２,３-ｂ］피리딘 유도체
AU2010224245B2 (en) 2009-03-11 2016-07-21 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of Raf kinases
WO2010111527A1 (en) * 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
MA33028B1 (fr) * 2009-04-03 2012-02-01 Plexxikon Inc Compositions et utilisations associees
TW201041888A (en) * 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
MY156727A (en) 2009-05-22 2016-03-15 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
MX2011012262A (es) 2009-05-22 2012-01-25 Incyte Corp 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il] octano-o heptano-nitrilo como inhibidores de cinasas janus (jak).
TWI476195B (zh) 2009-05-26 2015-03-11 Abbvie Bahamas Ltd 用於治療癌症及免疫及自體免疫疾病之細胞凋亡誘發劑
US9034875B2 (en) 2009-05-26 2015-05-19 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
US20220315555A1 (en) 2009-05-26 2022-10-06 Abbvie Inc. Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases
US8546399B2 (en) 2009-05-26 2013-10-01 Abbvie Inc. Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases
CN104922128B (zh) 2009-06-17 2019-12-20 沃泰克斯药物股份有限公司 流感病毒复制抑制剂
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US8329724B2 (en) * 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
MX2012002317A (es) 2009-08-24 2012-06-25 Ascepion Pharmaceuticals Inc Compuestos de urea que contienen heteroarilo 5,6-biciclicos como inhibidores de cinasa.
JP2013503190A (ja) 2009-08-28 2013-01-31 アレイ バイオファーマ、インコーポレイテッド Ｒａｆ阻害化合物およびその使用方法
CA2772316A1 (en) 2009-08-28 2011-03-03 Array Biopharma Inc. 1h-pyrazolo [3,4-b] pyridine compounds for inhibiting raf kinase
CA2772575A1 (en) 2009-08-28 2011-03-03 Genentech, Inc. Raf inhibitor compounds and methods of use thereof
US20120157453A1 (en) 2009-08-28 2012-06-21 Genentech, Inc. Raf inhibitor compounds and methods of use thereof
JP2013503187A (ja) 2009-08-28 2013-01-31 アレイ バイオファーマ、インコーポレイテッド Ｒａｆ阻害化合物およびその使用方法
SG178534A1 (en) * 2009-08-28 2012-03-29 Array Biopharma Inc Raf inhibitor compounds and methods of use thereof
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CA2778707A1 (en) 2009-10-23 2011-04-28 Mannkind Corporation Cancer immunotherapy and method of treatment
CN102695417A (zh) 2009-11-06 2012-09-26 普莱希科公司 用于激酶调节的化合物和方法及其适应症
WO2011060216A1 (en) 2009-11-12 2011-05-19 Concert Pharmaceuticals Inc. Substituted azaindoles
MY156210A (en) * 2009-11-18 2016-01-29 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
DE102009058280A1 (de) * 2009-12-14 2011-06-16 Merck Patent Gmbh Thiazolderivate
JP5815558B2 (ja) 2009-12-23 2015-11-17 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節のための化合物及び方法ならびにそれらの適応症
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
EP2521553A4 (en) 2010-01-06 2013-08-28 Errico Joseph P METHODS AND COMPOSITIONS FOR THE DEVELOPMENT OF TARGETED MEDICAMENTS
US8658170B2 (en) 2010-01-06 2014-02-25 Joseph P. Errico Combination therapy with MDM2 and EFGR inhibitors
EA201290774A1 (ru) 2010-02-11 2013-03-29 Вандербилт Юниверсити Пиразолопиридиновые, пиразолопиразиновые, пиразолопиримидиновые, пиразолотиофеновые и пиразолотиазоловые соединения как аллостерические потенциаторы mglur4, композиции и способы лечения неврологических дисфункций
US11084811B2 (en) 2010-03-01 2021-08-10 Oncternal Therapeutics, Inc. Compounds for treatment of cancer
KR102283091B1 (ko) 2010-03-10 2021-07-30 인사이트 홀딩스 코포레이션 Ｊａｋ１ 저해제로서의 피페리딘­４­일 아제티딘 유도체
JP2013529181A (ja) 2010-03-25 2013-07-18 ザ ジェイ． デヴィッド グラッドストーン インスティテューツ 神経障害を治療するための組成物および方法
CA2794808C (en) * 2010-04-16 2019-08-20 Ac Immune S.A. Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
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
CA2797281A1 (en) * 2010-05-06 2011-11-10 Merck Sharp & Dohme Corp. Aza-indole derivatives useful as modulators of faah
AR081039A1 (es) * 2010-05-14 2012-05-30 Osi Pharmaceuticals Llc Inhibidores biciclicos fusionados de quinasa
EP2569315A1 (en) 2010-05-14 2013-03-20 OSI Pharmaceuticals, LLC Fused bicyclic kinase inhibitors
EP3521291A1 (en) 2010-05-20 2019-08-07 Array Biopharma, Inc. Macrocyclic compounds as trk kinase inhibitors
TWI499421B (zh) 2010-05-21 2015-09-11 Incyte Corp Ｊａｋ抑制劑的局部製劑
EP2576566B1 (en) * 2010-05-28 2015-10-28 Merck Sharp & Dohme B.V. Thieno(2,3b)pyrazine compounds as b-raf inhibitors
NZ772688A (en) 2010-06-03 2022-09-30 Pharmacyclics Llc The use of inhibitors of bruton’s tyrosine kinase (btk)
US9593317B2 (en) 2010-06-09 2017-03-14 Bayer Cropscience Nv Methods and means to modify a plant genome at a nucleotide sequence commonly used in plant genome engineering
US8779150B2 (en) 2010-07-21 2014-07-15 Hoffmann-La Roche Inc. Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
CA2806670A1 (en) 2010-07-26 2012-02-09 Biomatrica, Inc. Compositions for stabilizing dna, rna and proteins in blood and other biological samples during shipping and storage at ambient temperatures
CA2806734A1 (en) 2010-07-26 2012-02-09 Biomatrica, Inc. Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
US8709419B2 (en) * 2010-08-17 2014-04-29 Hoffmann-La Roche, Inc. Combination therapy
US20120045433A1 (en) 2010-08-17 2012-02-23 Kapil Dhingra Combination therapy
WO2012037060A1 (en) 2010-09-13 2012-03-22 Concert Pharmaceuticals Inc. Substituted azaindoles
AU2011319842B2 (en) 2010-10-29 2014-05-29 Abbvie Inc. Solid dispersions containing an apoptosis-inducing agent
UA113500C2 (xx) 2010-10-29 2017-02-10 Одержані екструзією розплаву тверді дисперсії, що містять індукуючий апоптоз засіб
KR101236731B1 (ko) 2010-11-02 2013-02-25 한국과학기술원 아자인돌 화합물, 이를 포함하는 ｐｉ３ｋ 저해제용 약학 조성물 및 ｐｉ３ｋ와 연관된 질환 치료용 약학 조성물
CA2818545C (en) 2010-11-19 2019-04-16 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
BR112013012502A2 (pt) 2010-11-19 2019-03-06 Incyte Corporation pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak
ES2603129T3 (es) 2010-11-23 2017-02-23 Abbvie Ireland Unlimited Company Métodos de tratamiento utilizando inhibidores selectivos de Bcl-2
KR101923364B1 (ko) 2010-11-23 2018-11-30 애브비 인코포레이티드 아폽토시스­유도제의 염 및 결정형
WO2012075324A1 (en) 2010-12-02 2012-06-07 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Methods for treating a tumor using an antibody that specifically binds hmw-maa
US9295669B2 (en) * 2010-12-14 2016-03-29 Hoffman La-Roche Inc. Combination therapy for proliferative disorders
CA2822057A1 (en) 2010-12-16 2012-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
CA2824028A1 (en) 2011-01-06 2012-07-12 Beta Pharma Canada Inc. Novel ureas for the treatment and prevention of cancer
BR112013020041B1 (pt) * 2011-02-07 2021-11-23 Plexxikon, Inc Compostos e composições para a modulação de quinases e uso dos mesmos
EP2672963A4 (en) 2011-02-08 2015-06-24 Childrens Medical Center METHOD FOR THE TREATMENT OF MELANOMA
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
AR085279A1 (es) 2011-02-21 2013-09-18 Plexxikon Inc Formas solidas de {3-[5-(4-cloro-fenil)-1h-pirrolo[2,3-b]piridina-3-carbonil]-2,4-difluor-fenil}-amida del acido propano-1-sulfonico
WO2012123504A1 (en) * 2011-03-15 2012-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Compositions and methods for inhibiting tumor development caused by chemotherapy induced senescence
PT2694072T (pt) 2011-04-01 2018-02-26 Genentech Inc Combinação de composto inibidor de akt e abiraterona para utilização em tratamentos terapêuticos
WO2012138809A1 (en) * 2011-04-05 2012-10-11 Dawei Zhang Heterocyclic compounds as kinase inhibitors
KR101762999B1 (ko) 2011-04-18 2017-07-28 에자이 알앤드디 매니지먼트 가부시키가이샤 종양 치료제
AU2012253525B2 (en) * 2011-05-10 2016-09-22 Brunangelo Falini Hairy cell leukemia biomarkers and methods of using same
US20140088114A1 (en) 2011-05-16 2014-03-27 OSI Pharmaceuticals ,LLC Fused bicyclic kinase inhibitors
AU2012255275B2 (en) 2011-05-17 2016-01-28 Plexxikon Inc. Kinase modulation and indications therefor
JP2014515368A (ja) 2011-05-26 2014-06-30 第一三共株式会社 プロテインキナーゼ阻害剤としての複素環化合物
WO2012166899A2 (en) 2011-06-03 2012-12-06 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
EP2717694A4 (en) * 2011-06-10 2014-11-12 Glaxosmithkline Intellectual Property Ltd NEW COMPOUNDS
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
WO2013010136A2 (en) 2011-07-13 2013-01-17 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
KR102049817B1 (ko) 2011-08-01 2019-12-02 제넨테크, 인크. Pd-1 축 결합 길항제 및 mek 억제제를 사용하는 암 치료 방법
JP2014521725A (ja) 2011-08-10 2014-08-28 ノバルティス・ファルマ・アクチェンゲゼルシャフト ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
WO2013029043A1 (en) * 2011-08-25 2013-02-28 Reaction Biology Corp. Selective kinase inhibitors
CN107245056A (zh) 2011-08-26 2017-10-13 润新生物公司 化学实体、组合物及方法
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AU2012308238B2 (en) 2011-09-14 2017-05-25 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2570127A1 (en) 2011-09-16 2013-03-20 Sanofi Compositions and methods for treating cancer using PI3KB beta inhibitor and MAPK pathway inhibitor, including MEK and RAF inhibitors
RU2014114617A (ru) 2011-09-19 2015-10-27 Дженентек, Инк. Комбинированные виды лечения, содержащие антагонисты с-мет и антагонисты b-raf
EP2771011A4 (en) * 2011-10-24 2015-04-15 Glaxosmithkline Ip No 2 Ltd CHEMICAL COMPOUNDS
EP3569598A1 (en) 2011-11-17 2019-11-20 Dana Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
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
WO2013097224A1 (en) 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors
WO2013109142A1 (en) 2012-01-16 2013-07-25 Stichting Het Nederlands Kanker Instituut Combined pdk and mapk/erk pathway inhibition in neoplasia
CN102603734A (zh) * 2012-01-19 2012-07-25 盛世泰科生物医药技术(苏州)有限公司 一种蛋白激酶抑制剂及其应用
US9670180B2 (en) 2012-01-25 2017-06-06 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9216170B2 (en) 2012-03-19 2015-12-22 Hoffmann-La Roche Inc. Combination therapy for proliferative disorders
EP2830608B8 (en) * 2012-03-28 2020-01-15 UCB Biopharma SRL Phenyl-urea and phenyl-carbamate derivatives as inhibitors of protein aggregation
NZ702135A (en) * 2012-04-23 2016-09-30 Genentech Inc Intermediates and processes for preparing 5-bromo-4-chloro-3-nitro-1h-pyrrolo[2,3-b]pyridine
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
EP2858501A4 (en) * 2012-05-22 2015-12-09 Merck Sharp & Dohme TRK-A KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
US10077474B2 (en) * 2012-05-29 2018-09-18 Abbott Molecular, Inc. Method of designing primers, method of detecting single nucleotide polymorphisms (SNPs), method of distinguishing SNPs, and related primers, detectable oligonucleotides, and kits
RU2014149684A (ru) 2012-05-31 2016-07-20 Ф. Хоффманн-Ля Рош Аг Производные аминохиназолина и пиридопиримидина
US9150570B2 (en) * 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
KR20230170108A (ko) 2012-06-04 2023-12-18 파마싸이클릭스 엘엘씨 브루톤 타이로신 키나아제 저해제의 결정 형태
WO2014008270A1 (en) 2012-07-03 2014-01-09 Ratiopharm Gmbh Solid state form of vemurafenib choline salt
CA2879570A1 (en) 2012-07-24 2014-01-30 Pharmacyclics, Inc. Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
WO2014024077A1 (en) * 2012-08-07 2014-02-13 Aurigene Discovery Technologies Limited 5-(1H-PYRAZOL-4-YL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
SI2884979T1 (sl) 2012-08-17 2019-10-30 Hoffmann La Roche Kombinirana zdravljenja melanoma, ki vključujejo dajanje kobimetiniba in vemurafeniba
TWI601725B (zh) * 2012-08-27 2017-10-11 加拓科學公司 取代的氮雜吲哚化合物及其鹽、組合物和用途
CN103626765B (zh) * 2012-08-27 2016-08-10 广东东阳光药业有限公司 取代的氮杂吲哚化合物及其盐、组合物和用途
MX2015002887A (es) 2012-09-06 2015-07-06 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello.
WO2014047648A1 (en) 2012-09-24 2014-03-27 Neupharma, Inc. Certain chemical entities, compositions, and methods
CN105712992B (zh) * 2012-09-29 2018-10-26 上海科州药物研发有限公司 作为cMet抑制剂的化合物及其制备方法和用途
EP2912036A1 (en) 2012-10-04 2015-09-02 Pfizer Limited Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
CA2886138C (en) * 2012-10-08 2021-10-12 Oliver Planz Mek inhibitors in the treatment of virus diseases
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
EP2916838B1 (en) 2012-11-12 2019-03-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
KR20210037012A (ko) 2012-11-15 2021-04-05 인사이트 홀딩스 코포레이션 룩솔리티니브의 서방성 제형
AU2013344656A1 (en) 2012-11-15 2015-06-04 Pharmacyclics Llc Pyrrolopyrimidine compounds as kinase inhibitors
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
EP2934572A4 (en) 2012-12-20 2016-11-23 Biomatrica Inc FORMULATIONS AND METHODS FOR STABILIZING PCR REAGENTS
JPWO2014098176A1 (ja) 2012-12-21 2017-01-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体のアモルファス及びその製造方法
KR102212923B1 (ko) 2012-12-21 2021-02-04 플렉시콘 인코퍼레이티드 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
US9278950B2 (en) 2013-01-14 2016-03-08 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
AR094664A1 (es) 2013-01-15 2015-08-19 Incyte Corp Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
WO2014130856A2 (en) * 2013-02-21 2014-08-28 Wayne Rothbaum Treatment of skeletal-related disorders
MX2015010791A (es) 2013-02-22 2015-11-26 Hoffmann La Roche Metodos para tratar el cancer y prevenir la resistencia a farmacos.
JP6835472B2 (ja) * 2013-03-05 2021-02-24 ユニバーシティ オブ テネシー リサーチ ファウンデーション 癌の処置のための組成物
NZ711976A (en) 2013-03-06 2019-01-25 Incyte Holdings Corp Processes and intermediates for making a jak inhibitor
US20140275082A1 (en) 2013-03-14 2014-09-18 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
US9440971B2 (en) 2013-03-14 2016-09-13 Ratiopharm Gmbh Solid state forms of vemurafenib hydrochloride
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
EP2968350A1 (en) 2013-03-15 2016-01-20 Sanofi Anti-tumoral composition comprising a pi3kbeta inhibitor and a raf inhibitor, to overcome cancer cells resistance
MX2015012456A (es) 2013-03-15 2016-02-03 Plexxikon Inc Compuestos heterociclicos y usos de los mismos.
MX2015011899A (es) 2013-03-15 2016-05-05 Genentech Inc Metodos para el tratamiento de cáncer y prevención de resistencia a los fármacos para el cáncer.
US9206188B2 (en) 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
RU2658601C2 (ru) 2013-05-14 2018-06-21 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Биомаркер для прогнозирования и оценки чувствительности субъектов с раком эндометрия к соединениям ленватиниба
EP3004060B1 (en) 2013-05-30 2019-11-27 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
JP6604942B2 (ja) 2013-06-13 2019-11-13 バイオマトリカ，インク． 細胞安定化
WO2014206344A1 (en) 2013-06-28 2014-12-31 Beigene, Ltd. Fused tricyclic amide compounds as multiple kinase inhibitors
EP3019166B1 (en) * 2013-07-12 2019-05-08 Piramal Enterprises Limited A pharmaceutical combination for the treatment of melanoma
JP6800750B2 (ja) 2013-08-02 2020-12-16 ファーマサイクリックス エルエルシー 固形腫瘍の処置方法
SG10201801069QA (en) 2013-08-07 2018-03-28 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
ES2709509T3 (es) 2013-08-12 2019-04-16 Pharmacyclics Llc Procedimientos para el tratamiento de cáncer amplificado por HER2
US9556197B2 (en) 2013-08-23 2017-01-31 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
WO2015041533A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut Rock in combination with mapk-pathway
CA2925124A1 (en) 2013-09-30 2015-04-02 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
AU2014337122B2 (en) 2013-10-18 2019-01-03 Dana-Farber Cancer Institute, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
CN105849099B (zh) 2013-10-18 2020-01-17 达纳-法伯癌症研究所股份有限公司 周期蛋白依赖性激酶7(cdk7)的多环抑制剂
SI3068776T1 (sl) 2013-11-13 2019-09-30 Vertex Pharmaceuticals Incorporated Inhibitorji replikacije virusov influence
SI3068782T1 (sl) 2013-11-13 2018-10-30 Vertex Pharmaceuticals Incorporated Postopki za pripravo inhibitorjev v replikacije virusov gripe
WO2015073864A1 (en) * 2013-11-15 2015-05-21 The Wisar Institute Of Anatomy And Biology Ebna1 inhibitors and their method of use
WO2015075749A1 (en) * 2013-11-22 2015-05-28 Laurus Labs Private Limited Novel processes for the preparation of vemurafenib
CZ2013943A3 (cs) 2013-11-27 2015-06-03 Zentiva, K.S. Krystalické formy vemurafenibu
CN104710417B (zh) * 2013-12-11 2020-09-08 上海科州药物研发有限公司 氮杂吲哚类衍生物及其合成方法
BR112016014481B1 (pt) * 2013-12-20 2022-11-08 Biomed Valley Discoveries, Inc Uso de uma composição farmacêutica, método in vitro para efetuar a morte de células cancerosas, e kit
CN104739823A (zh) * 2013-12-28 2015-07-01 复旦大学附属华山医院 淫羊藿素在制备维罗非尼增敏剂中的用途
US9771369B2 (en) 2014-03-04 2017-09-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2015143400A1 (en) 2014-03-20 2015-09-24 Pharmacyclics, Inc. Phospholipase c gamma 2 and resistance associated mutations
WO2015156674A2 (en) 2014-04-10 2015-10-15 Stichting Het Nederlands Kanker Instituut Method for treating cancer
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
EP3139927A4 (en) * 2014-05-06 2017-12-13 The Regents of The University of California Wound healing using braf inhibitors
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
WO2015181628A1 (en) * 2014-05-27 2015-12-03 Eisai R&D Management Co., Ltd. Treatment of acute myeloid leukemia with an hck inhibitor
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
EP3154338B1 (en) 2014-06-10 2020-01-29 Biomatrica, INC. Stabilization of thrombocytes at ambient temperatures
US20170204187A1 (en) * 2014-06-13 2017-07-20 Genentech, Inc. Methods of treating and preventing cancer drug resistance
US20230190750A1 (en) 2014-06-13 2023-06-22 Genentech, Inc. Methods of treating and preventing cancer drug resistance
AR101106A1 (es) 2014-07-02 2016-11-23 Pharmacyclics Llc Inhibidores de tirosina quinasa de bruton
WO2016000615A1 (en) * 2014-07-02 2016-01-07 Sunshine Lake Pharma Co., Ltd. Heteroaryl compounds and pharmaceutical applications thereof
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
KR20170026630A (ko) 2014-07-15 2017-03-08 제넨테크, 인크. Pd-1 축 결합 길항제 및 mek 저해제를 사용하는 암의 치료용 조성물
WO2016019233A1 (en) 2014-08-01 2016-02-04 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
SG11201700849XA (en) 2014-08-07 2017-03-30 Pharmacyclics Llc Novel formulations of a bruton's tyrosine kinase inhibitor
MX2017001980A (es) 2014-08-28 2017-05-04 Eisai R&D Man Co Ltd Derivado de quinolina muy puro y metodo para su produccion.
WO2016044067A1 (en) 2014-09-15 2016-03-24 Plexxikon Inc. Heterocyclic compounds and uses thereof
KR101949624B1 (ko) 2014-09-26 2019-02-18 길리애드 사이언시즈, 인코포레이티드 Tank-결합 키나제 억제제 화합물로서 유용한 아미노트리아진 유도체
US20170248603A1 (en) 2014-10-06 2017-08-31 Dana-Farber Cancer Institute, Inc. Angiopoiten-2 biomarkers predictive of anti-immune checkpoint response
US10611765B2 (en) 2014-11-06 2020-04-07 Ohio State Innovation Foundation Pyrrolopyrimidine derivatives as Mps1/TTK kinase inhibitors
EP3223817A4 (en) * 2014-11-29 2018-05-30 Shilpa Medicare Limited Substantially pure vemurafenib and its salts
EP3236959A4 (en) 2014-12-23 2018-04-25 Dana Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2016105518A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
KR20170122734A (ko) 2015-02-25 2017-11-06 에자이 알앤드디 매니지먼트 가부시키가이샤 퀴놀린 유도체의 고미 억제 방법
PT3265084T (pt) 2015-03-03 2024-02-13 Pharmacyclics Llc Formulações farmacêuticas de inibidor de tirosina cinase de bruton
KR20240064733A (ko) 2015-03-04 2024-05-13 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
WO2016160617A2 (en) 2015-03-27 2016-10-06 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2016164641A1 (en) 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CZ2015250A3 (cs) 2015-04-14 2016-10-26 Zentiva, K.S. Amorfní formy vemurafenibu
JP6946194B2 (ja) 2015-05-06 2021-10-06 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼを調節する化合物の固体形態
JP6530826B2 (ja) 2015-05-06 2019-06-12 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼを修飾する１ｈ−ピロロ［２，３−ｂ］ピリジン誘導体の合成
JP6857617B2 (ja) 2015-05-13 2021-04-14 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
AU2016262572B2 (en) 2015-05-14 2020-04-30 The Wistar Institute Of Anatomy And Biology EBNA1 inhibitors and methods using same
US9776998B2 (en) 2015-05-22 2017-10-03 Plexxikon Inc. Synthesis of heterocyclic compounds
BR112017025045A2 (pt) 2015-05-22 2018-08-07 Plexxikon Inc plx-8394 ou plx-7904 para uso no tratamento de doenças relacionadas a braf-v600
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
RS59934B1 (sr) * 2015-06-09 2020-03-31 Abbvie Inc Modulatori nuklearnih receptora (ror) za lečenje inflamatornih i autoimunih oboljenja
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2016204193A1 (ja) 2015-06-16 2016-12-22 株式会社ＰＲＩＳＭ Ｐｈａｒｍａ 抗がん剤
RS61485B1 (sr) 2015-07-16 2021-03-31 Array Biopharma Inc Supstituisana pirazolo [1,5-a] piridinska jedinjenja kao inhibitori ret kinaze
CA2993018A1 (en) * 2015-07-20 2017-01-26 Genzyme Corporation Colony stimulating factor-1 receptor (csf-1r) inhibitors
WO2017019804A2 (en) 2015-07-28 2017-02-02 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US10729669B2 (en) * 2015-07-28 2020-08-04 University Of Iowa Research Foundation Compositions and methods for treating cancer
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2017053243A1 (en) 2015-09-21 2017-03-30 Plexxikon Inc. Heterocyclic compounds and uses thereof
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
US9890163B2 (en) 2015-10-15 2018-02-13 Princeton Drug Discovery Inc Inhibitors of protein kinases
KR20180102544A (ko) 2015-10-26 2018-09-17 더 리전츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코퍼레이트 Trk 억제제-내성 암에서의 점 돌연변이 및 이의 관련 방법
JP6952691B2 (ja) 2015-11-19 2021-10-20 ジェネンテック， インコーポレイテッド Ｂ−ｒａｆ阻害剤及び免疫チェックポイント阻害剤を使用してがんを治療する方法
JP6862468B2 (ja) 2015-12-07 2021-04-21 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節のための化合物及び方法ならびにそのための指示
KR102589056B1 (ko) 2015-12-08 2023-10-12 바이오매트리카 인코포레이티드 적혈구 침강 속도의 감소
EP3391643A4 (en) 2015-12-14 2019-07-31 Red.Com, Llc MODULAR DIGITAL CAMERA AND MOBILE PHONE
CA2951911A1 (en) 2015-12-17 2017-06-17 Gilead Sciences, Inc. Tank-binding kinase inhibitor compounds
CN109195957A (zh) * 2016-02-25 2019-01-11 塔克西斯医药股份有限公司 合成方法和中间体
CA3017972C (en) 2016-03-16 2023-03-28 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
AU2017246547B2 (en) 2016-04-04 2023-02-23 Loxo Oncology, Inc. Methods of treating pediatric cancers
RU2751767C2 (ru) 2016-04-04 2021-07-16 Локсо Онколоджи, Инк. Жидкие составы (s)-n-(5-((r)-2-(2,5-дифторфенил)пирролидин-1-ил)пиразоло[1,5-a]пиримидин-3-ил)-3-гидроксипирролидин-1-карбоксамида
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CA3018406A1 (en) 2016-04-15 2017-10-19 Genentech, Inc. Diagnostic and therapeutic methods for cancer
EP3800189B1 (en) 2016-05-18 2023-06-28 Loxo Oncology, Inc. Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
KR20230047210A (ko) * 2016-06-13 2023-04-06 케모센트릭스, 인크. 췌장 암을 치료하는 방법
AU2017281940A1 (en) 2016-06-24 2019-01-24 University Of Iowa Research Foundation Compositions and methods of treating melanoma
RS60451B1 (sr) 2016-07-01 2020-07-31 Fermion Oy Novi postupci za dobijanje vemurafeniba
SG11201900157RA (en) 2016-07-12 2019-02-27 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
WO2018050286A1 (en) * 2016-09-16 2018-03-22 Helmholtz Zentrum Muenchen - Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) Traf 6 inhibitors
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
EP3308773A1 (en) 2016-10-11 2018-04-18 Recordati Industria Chimica E Farmaceutica SPA Formulations of cysteamine and cysteamine derivatives
EP3528798A4 (en) 2016-10-19 2020-10-21 United States Government as Represented by The Department of Veterans Affairs COMPOSITIONS AND METHODS OF TREATMENT OF CANCER
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
AU2017363299B2 (en) 2016-11-23 2022-12-22 Chemocentryx, Inc. Method of treating focal segmental glomerulosclerosis
RU2763297C2 (ru) 2016-12-15 2021-12-28 Сосьете Де Продюи Нестле С.А. Композиции и способы регуляции уровня фосфора или ферментов у животного-компаньона
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
AU2017395023B2 (en) 2016-12-23 2022-04-07 Plexxikon Inc. Compounds and methods for CDK8 modulation and indications therefor
WO2018119448A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
AU2018209164B2 (en) * 2017-01-17 2021-11-04 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CA3049136C (en) 2017-01-18 2022-06-14 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
KR102665763B1 (ko) 2017-01-23 2024-05-10 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 이환 화합물
CA3051054A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
EP3579872A1 (en) 2017-02-10 2019-12-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
AU2018237047A1 (en) 2017-03-20 2019-10-17 Plexxikon Inc. Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1H- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain
US11555031B2 (en) 2017-03-20 2023-01-17 The Broad Institute, Inc. Compounds and methods for regulating insulin secretion
EP3600302A4 (en) * 2017-03-29 2020-12-30 United States Government as Represented by The Department of Veterans Affairs METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCER
CA3058183A1 (en) 2017-03-30 2018-10-04 Taxis Pharmaceuticals, Inc. Synthetic processes and synthetic intermediates
CN110545853A (zh) * 2017-04-28 2019-12-06 石英治疗有限公司 Raf降解偶联化合物
WO2018210661A1 (en) * 2017-05-15 2018-11-22 Basf Se Heteroaryl compounds as agrochemical fungicides
AU2018270295B2 (en) * 2017-05-19 2022-03-03 Nflection Therapeutics, Inc. Pyrrolopyridine-aniline compounds for treatment of dermal disorders
ES2913213T3 (es) 2017-05-19 2022-06-01 Nflection Therapeutics Inc Compuestos heteroaromáticos de anilina condensados para el tratamiento de trastornos dérmicos
US10428067B2 (en) 2017-06-07 2019-10-01 Plexxikon Inc. Compounds and methods for kinase modulation
WO2019006359A1 (en) 2017-06-30 2019-01-03 The Regents Of The University Of California COMPOSITIONS AND METHODS FOR MODULATION OF HAIR GROWTH
AU2018307910A1 (en) 2017-07-25 2020-01-23 Daiichi Sankyo Company, Limited Formulations of a compound modulating kinases
CN109384785B (zh) * 2017-08-10 2021-09-28 浙江海正药业股份有限公司 吡咯并吡啶酮类衍生物、其制备方法及其在医药上的用途
AU2018329925A1 (en) 2017-09-08 2020-03-05 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for cancer
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
TWI812649B (zh) 2017-10-10 2023-08-21 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
JP2020536919A (ja) 2017-10-11 2020-12-17 ケモセントリックス， インコーポレイテッド Ｃｃｒ２アンタゴニストによる巣状分節性糸球体硬化症の治療
AU2018347516A1 (en) 2017-10-12 2020-05-07 Revolution Medicines, Inc. Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors
JP2020536917A (ja) 2017-10-13 2020-12-17 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼを調節するための化合物の固体形態
IL274027B2 (en) 2017-10-26 2023-12-01 Xynomic Pharmaceuticals Inc B–RAF kinase inhibitor salt crystals
AU2018354423A1 (en) 2017-10-27 2020-05-14 Plexxikon Inc. Formulations of a compound modulating kinases
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
KR20200099530A (ko) 2017-12-15 2020-08-24 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 다환식 화합물
US11725185B2 (en) 2017-12-28 2023-08-15 University Of Houston System Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
JP7061195B2 (ja) 2018-01-18 2022-04-27 アレイ バイオファーマ インコーポレイテッド ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［３，４－ｄ］ピリミジン化合物
CA3087354C (en) 2018-01-18 2023-01-03 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
EP3746429B1 (en) 2018-01-30 2022-03-09 Incyte Corporation Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
MX2020007954A (es) 2018-01-31 2021-01-08 Heparegenix Gmbh Inhibidores de la proteina cinasa cinasa 4 activada por mitogeno (mkk4) para promover la regeneracion del higado o reducir o prevenir la muerte de los hepatocitos.
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
AU2019239952A1 (en) 2018-03-20 2020-10-08 Plexxikon Inc. Compounds and methods for IDO and TDO modulation, and indications therefor
EA202092343A1 (ru) 2018-03-30 2021-01-20 Инсайт Корпорейшн Лечение гнойного гидраденита с использованием ингибиторов jak
CA3095934A1 (en) * 2018-04-05 2019-10-10 Beth Israel Deaconess Medical Center, Inc. Aryl hydrocarbon receptor modulators and uses thereof
EP3560516A1 (en) * 2018-04-27 2019-10-30 Bergen Teknologioverforing AS Combination therapy including beta-sitosterol in combination with at least one of a braf inhibitor, a mek inhibitor or an erk inhibitor and methods and use thereof
TW201946919A (zh) 2018-05-17 2019-12-16 威斯塔研究所 Ebna1抑制劑晶形、其製備方法及其使用方法
GB201808321D0 (en) * 2018-05-21 2018-07-11 Univ College Dublin Nat Univ Ireland Dublin Compositions and uses thereof
RU2687107C1 (ru) * 2018-06-18 2019-05-07 федеральное государственное автономное образовательное учреждение высшего образования "Московский физико-технический институт (государственный университет)" Ингибитор braf киназы n-(3-(5-(4-хлорофенил)-1h-пиразоло[3,4-b]пиридин-3-карбонил)-2,4-дифторофенил) пропан-1-сульфонамид
US11731968B2 (en) 2018-06-21 2023-08-22 Heparegenix Gmbh Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
EP4266058A3 (en) * 2018-07-06 2024-02-21 The Regents of the University of Colorado, a body corporate Genetically encoded system for constructing and detecting biologically active agents
SG11202012732UA (en) 2018-07-16 2021-02-25 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
JP7317938B2 (ja) * 2018-07-19 2023-07-31 シェンチェン リンファン バイオテック カンパニー，リミティド アザインドール誘導体とＦＧＦＲ及びＣ－Ｍｅｔ阻害剤としてのその使用
CA3224945A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
EP3849986B1 (en) 2018-09-10 2022-06-08 Array Biopharma, Inc. Fused heterocyclic compounds as ret kinase inhibitors
US20210244716A1 (en) 2018-10-03 2021-08-12 Jyväskylän Yliopisto Vemurafenib and salts thereof for use in the treatment of enteroviral infections
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
JP2022504905A (ja) 2018-10-16 2022-01-13 ノバルティス アーゲー 標的化療法に対する応答を予測するためのバイオマーカーとしての単独の又は免疫マーカーと組み合わせた腫瘍突然変異負荷
US20220002294A1 (en) * 2018-11-16 2022-01-06 California Institute Of Technology Erk inhibitors and uses thereof
MA55141A (fr) 2018-11-20 2021-09-29 Nflection Therapeutics Inc Composés cyanoaryl-aniline pour le traitement d'affections de la peau
EP3891136B1 (en) * 2018-12-03 2023-07-19 Merck Patent GmbH 4-heteroarylcarbonyl-n-(phenyl or heteroaryl)piperidine-1-carboxamides as inhibitors of tankyrases
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体
JP2022515198A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物
SG11202108636SA (en) * 2019-02-11 2021-09-29 Merck Patent Gmbh Indazolyl-isoxazole derivatives for the treatment of diseases such as cancer
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
KR20220018475A (ko) 2019-04-09 2022-02-15 플렉시콘 인코퍼레이티드 Ep300 또는 cbp 조절 및 이의 표시를 위한 응축 아진
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US20220227760A1 (en) * 2019-05-29 2022-07-21 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
AU2020283597A1 (en) * 2019-05-31 2021-11-25 Fochon Biosciences, Ltd. Substituted pyrrolo (2, 3-b) pyridine and pyrazolo (3, 4-b) pyridine derivatives as protein kinase inhibitors
JP2022544074A (ja) 2019-07-29 2022-10-17 ヘパリジェニックス ゲーエムベーハー 肝臓再生を促進または肝細胞死を縮減もしくは防止するためのヘテロアリール置換ピラゾロ－ピリジンタンパク質キナーゼ阻害剤
AR119765A1 (es) 2019-08-14 2022-01-12 Incyte Corp Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2
WO2021067749A2 (en) * 2019-10-02 2021-04-08 The Board Of Trustees Of The Leland Stanford Junior University Methods and compositions for the treatment of osteoarthritis
WO2021072232A1 (en) 2019-10-11 2021-04-15 Incyte Corporation Bicyclic amines as cdk2 inhibitors
CN111004210A (zh) * 2019-10-23 2020-04-14 中山大学 化合物单晶及其制备方法
MX2022007678A (es) 2019-12-19 2022-09-19 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida del receptor de androgenos.
KR20220123023A (ko) 2019-12-27 2022-09-05 슈뢰딩거, 인크. 시클릭 화합물 및 이의 사용 방법
JP2023509760A (ja) 2020-01-08 2023-03-09 シンシス セラピューティクス，インコーポレイテッド Ａｌｋ５阻害剤複合体およびその使用
CN114981267A (zh) 2020-01-15 2022-08-30 海帕瑞吉尼克斯股份有限公司 用于治疗肝脏疾病的mkk4抑制剂3-苯甲酰基-1h-吡咯并[2,3-b]吡啶衍生物
WO2021152005A1 (en) 2020-01-28 2021-08-05 Universite De Strasbourg Antisense oligonucleotide targeting linc00518 for treating melanoma
EP4135700A4 (en) * 2020-04-15 2024-04-17 Pyramid Biosciences Inc METHOD FOR THE PRODUCTION OF TYROSINE RECEPTOR KINASE INHIBITORS
EP4139296A1 (en) 2020-04-23 2023-03-01 Opna Immuno Oncology, SA Compounds and methods for cd73 modulation and indications therefor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11529335B2 (en) 2020-07-31 2022-12-20 University Of Iowa Research Foundation Compositions and methods for treating cancer
JP2023542473A (ja) 2020-08-21 2023-10-10 プレキシコン インコーポレーテッド 併用薬抗がん治療
JP2023541047A (ja) 2020-09-10 2023-09-27 シュレーディンガー， インコーポレイテッド がんの治療のための複素環式ペリ縮環ｃｄｃ７キナーゼ阻害剤
WO2022063101A1 (zh) * 2020-09-23 2022-03-31 劲方医药科技(上海)有限公司 芳甲酰取代的三环化合物及其制法和用途
CN114478528A (zh) * 2020-10-28 2022-05-13 劲方医药科技(上海)有限公司 芳甲酰取代的三环化合物及其制法和用途
US20230406856A1 (en) * 2020-11-17 2023-12-21 Fochon Biosciences, Ltd. SUBSTITUTED PYRROLO [2, 3-b] PYRIDINE AND PYRAZOLO [3, 4-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
WO2022125524A1 (en) * 2020-12-07 2022-06-16 Lieber Institute, Inc. Compounds for inhibiting inositol hexakisphosphate kinase (ip6k) and methods of use thereof
US20240002377A1 (en) * 2020-12-07 2024-01-04 Medshine Discovery Inc. Pyrrolopyridine compound and application thereof
JP2024500919A (ja) 2020-12-23 2024-01-10 ジェンザイム・コーポレーション 重水素化コロニー刺激因子－１受容体（ｃｓｆ－１ｒ）阻害剤
JP2024505890A (ja) 2021-01-26 2024-02-08 シュレーディンガー， インコーポレイテッド がん、自己免疫及び炎症性障害の治療に有用な三環式化合物
CN112574200B (zh) * 2021-02-26 2021-06-11 安润医药科技（苏州）有限公司 Btk和/或btk的突变体c481s的小分子抑制剂
CN115073469B (zh) * 2021-03-15 2023-12-22 药雅科技(上海)有限公司 吡咯并嘧啶类化合物作为激酶抑制剂的制备及其应用
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
JP2024511373A (ja) 2021-03-18 2024-03-13 ノバルティス アーゲー がんのためのバイオマーカーおよびその使用
TW202304890A (zh) * 2021-04-14 2023-02-01 美商百歐克斯製藥公司 Klk5雙環雜芳香族抑制劑
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
WO2023059786A1 (en) * 2021-10-06 2023-04-13 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibitors of ulk1 and methods of use
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2023174300A1 (zh) * 2022-03-15 2023-09-21 劲方医药科技(上海)有限公司 Btk抑制剂的晶型及其酸式盐和其酸式盐的晶型
WO2023178240A2 (en) * 2022-03-16 2023-09-21 The Children's Medical Center Corporation Pyk2 inhibition modulates immune cell function
WO2024003350A1 (en) 2022-06-30 2024-01-04 Universite De Strasbourg Combination therapy for melanoma
CN115141197B (zh) * 2022-07-27 2024-03-26 安徽医科大学 一种3-芳杂环取代苯基衍生物及其制备方法与用途
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
WO2024054591A1 (en) 2022-09-07 2024-03-14 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3067237A (en) * 1959-04-14 1962-12-04 Sterling Drug Inc Lower-alkyl mono-or bis-(alkanesulfonamido) benzoate esters
US3124610A (en) * 1964-03-10 Preparation of intermediates
WO2003101959A1 (en) * 2002-05-31 2003-12-11 Glaxo Group Limited Pyrrole compounds for the treatment of prostaglandin mediated diseases
WO2004016610A1 (en) * 2002-08-14 2004-02-26 Astrazeneca Ab Substituted pyrrolopyridines

Family Cites Families (162)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2234705A (en) * 1940-04-12 1941-03-11 Eastman Kodak Co Cellulose organic derivative composition containing esters of monoalkoxy benzoic acids
US2413258A (en) * 1942-07-07 1946-12-24 United Gas Improvement Co Polystyrene-type resins plasticized with high boiling fatty acid alkyl esters
GB1141949A (en) 1966-02-23 1969-02-05 Sterling Drug Inc 7-azaindole derivatives
CH513136A (de) * 1966-10-21 1971-09-30 Minnesota Mining & Mfg Verfahren zur Herstellung N-substituierter, einen Perfluorkohlenstoffrest aufweisender Sulfonamide
IL46853A0 (en) * 1974-03-20 1975-05-22 Bayer Ag Novel alkoxycarbonylphenylureas,their preparation and their use as herbicides
DE2413258A1 (de) * 1974-03-20 1975-10-02 Bayer Ag Alkoxycarbonylphenylharnstoffe, verfahren zu ihrer herstellung und ihre verwendung als herbizide
GB1573212A (en) 1976-04-15 1980-08-20 Technicon Instr Immunoassay for gentamicin
US4301159A (en) * 1980-06-20 1981-11-17 Shionogi & Co., Ltd. N-(Diethylaminoethyl)-2-alkoxy-benzamide derivatives
AU547405B2 (en) * 1981-07-08 1985-10-17 Sanofi Amidobenzamides
US4664504A (en) 1983-01-20 1987-05-12 Tokyo Shibaura Denki Kabushiki Kaisha Image forming apparatus
US4568649A (en) * 1983-02-22 1986-02-04 Immunex Corporation Immediate ligand detection assay
US4626513A (en) * 1983-11-10 1986-12-02 Massachusetts General Hospital Method and apparatus for ligand detection
IL73486A (en) * 1983-11-14 1993-05-13 Dow Chemical Co N-aryl 1,2,4-triazolo (1,5-a) pyrimidine-2-sulfonamides, their preparation and compositions and methods of controlling undesired vegetation and suppressing the nitrification of ammonium nitrogen in soil
AU567140B2 (en) * 1984-01-06 1987-11-12 Shionogi & Co., Ltd. Sulphonamido-benzamide derivatives
DE3483099D1 (de) 1984-03-15 1990-10-04 Immunex Corp Test zur sofortigen feststellung von liganden, testsatz und seine herstellung.
IT1196133B (it) * 1984-06-06 1988-11-10 Ausonia Farma Srl Derivati furanici con attivita' antiulcera
US4714693A (en) 1986-04-03 1987-12-22 Uop Inc. Method of making a catalyst composition comprising uniform size metal components on carrier
US5688655A (en) * 1988-02-10 1997-11-18 Ict Pharmaceuticals, Inc. Method of screening for protein inhibitors and activators
US5700637A (en) * 1988-05-03 1997-12-23 Isis Innovation Limited Apparatus and method for analyzing polynucleotide sequences and method of generating oligonucleotide arrays
US6054270A (en) * 1988-05-03 2000-04-25 Oxford Gene Technology Limited Analying polynucleotide sequences
US5658775A (en) * 1988-05-17 1997-08-19 Sloan-Kettering Institute For Cancer Research Double copy retroviral vector
WO1990002806A1 (en) * 1988-09-01 1990-03-22 Whitehead Institute For Biomedical Research Recombinant retroviruses with amphotropic and ecotropic host ranges
US5703055A (en) * 1989-03-21 1997-12-30 Wisconsin Alumni Research Foundation Generation of antibodies through lipid mediated DNA delivery
US5143854A (en) * 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5800992A (en) * 1989-06-07 1998-09-01 Fodor; Stephen P.A. Method of detecting nucleic acids
US5527681A (en) * 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
US5744101A (en) * 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
US5360822A (en) * 1990-02-07 1994-11-01 Nippon Shinyaku Co. Ltd. Sulfonanilide derivatives and medicine
AU7906691A (en) * 1990-05-23 1991-12-10 United States of America, as represented by the Secretary, U.S. Department of Commerce, The Adeno-associated virus (aav)-based eucaryotic vectors
DE4022414A1 (de) 1990-07-13 1992-01-16 Bayer Ag Substituierte pyrrolo-pyridine
US5124335A (en) 1991-01-30 1992-06-23 Merck & Co., Inc. Substituted pyrollo-fused 6 membered heterocycles as angiotensin ii antagonists
WO1993002556A1 (en) * 1991-07-26 1993-02-18 University Of Rochester Cancer therapy utilizing malignant cells
US5632957A (en) * 1993-11-01 1997-05-27 Nanogen Molecular biological diagnostic systems including electrodes
FR2687402B1 (fr) * 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
JPH05236997A (ja) * 1992-02-28 1993-09-17 Hitachi Ltd ポリヌクレオチド捕捉用チップ
US5576319A (en) 1993-03-01 1996-11-19 Merck, Sharp & Dohme Ltd. Pyrrolo-pyridine derivatives
ATE184008T1 (de) * 1993-03-01 1999-09-15 Merck Sharp & Dohme Pyrrolopyridinderivate als dopaminrezeptor liganden
CN1118598A (zh) * 1993-03-01 1996-03-13 默克·夏普-道姆公司 吡咯并吡啶衍生物
US5549614A (en) * 1993-03-18 1996-08-27 Tunis; Scott W. Apparatus for folding flexible intraocular lenses
US5840485A (en) * 1993-05-27 1998-11-24 Selectide Corporation Topologically segregated, encoded solid phase libraries
DE69434998T2 (de) * 1993-05-27 2008-03-13 Aventis Pharmaceuticals Inc. Topologisch getrennte, kodierende Festphasen-Bibliotheken
US5631236A (en) * 1993-08-26 1997-05-20 Baylor College Of Medicine Gene therapy for solid tumors, using a DNA sequence encoding HSV-Tk or VZV-Tk
US5426039A (en) * 1993-09-08 1995-06-20 Bio-Rad Laboratories, Inc. Direct molecular cloning of primer extended DNA containing an alkane diol
JP3545461B2 (ja) 1993-09-10 2004-07-21 エーザイ株式会社 二環式ヘテロ環含有スルホンアミド誘導体
US6045996A (en) * 1993-10-26 2000-04-04 Affymetrix, Inc. Hybridization assays on oligonucleotide arrays
US5965452A (en) * 1996-07-09 1999-10-12 Nanogen, Inc. Multiplexed active biologic array
US6468742B2 (en) * 1993-11-01 2002-10-22 Nanogen, Inc. Methods for determination of single nucleic acid polymorphisms using bioelectronic microchip
US5486525A (en) * 1993-12-16 1996-01-23 Abbott Laboratories Platelet activating factor antagonists: imidazopyridine indoles
US5807522A (en) * 1994-06-17 1998-09-15 The Board Of Trustees Of The Leland Stanford Junior University Methods for fabricating microarrays of biological samples
US5763198A (en) * 1994-07-22 1998-06-09 Sugen, Inc. Screening assays for compounds
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
GB9416162D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
DE4430212A1 (de) * 1994-08-28 1996-02-29 Merck Patent Gmbh Ortho-substituierte Benzoesäure-Derivate
US5556752A (en) * 1994-10-24 1996-09-17 Affymetrix, Inc. Surface-bound, unimolecular, double-stranded DNA
US5830645A (en) * 1994-12-09 1998-11-03 The Regents Of The University Of California Comparative fluorescence hybridization to nucleic acid arrays
GB2298199A (en) * 1995-02-21 1996-08-28 Merck Sharp & Dohme Synthesis of azaindoles
GB9503400D0 (en) 1995-02-21 1995-04-12 Merck Sharp & Dohme Therpeutic agents
US5959098A (en) * 1996-04-17 1999-09-28 Affymetrix, Inc. Substrate preparation process
US6117681A (en) * 1995-03-29 2000-09-12 Bavarian Nordic Research Inst. A/S Pseudotyped retroviral particles
GB2299581A (en) 1995-04-07 1996-10-09 Merck Sharp & Dohme 3-(Tetrahydropyridin-1-yl-methyl)pyrrolo[2,3-b]pyridine derivatives as ligands for dopamine receptor subtypes
GB9507291D0 (en) 1995-04-07 1995-05-31 Merck Sharp & Dohme Therapeutic agents
US6110456A (en) * 1995-06-07 2000-08-29 Yale University Oral delivery or adeno-associated viral vectors
US5856174A (en) * 1995-06-29 1999-01-05 Affymetrix, Inc. Integrated nucleic acid diagnostic device
US5866411A (en) * 1995-09-08 1999-02-02 Pedersen; Finn Skou Retroviral vector, a replication system for said vector and avian or mammalian cells transfected with said vector
US5747276A (en) * 1995-09-15 1998-05-05 The Scripps Research Institute Screening methods for the identification of novel antibiotics
US5721118A (en) * 1995-10-31 1998-02-24 The Regents Of The University Of California, San Diego Mammalian artificial chromosomes and methods of using same
US6022963A (en) * 1995-12-15 2000-02-08 Affymetrix, Inc. Synthesis of oligonucleotide arrays using photocleavable protecting groups
US6013440A (en) * 1996-03-11 2000-01-11 Affymetrix, Inc. Nucleic acid affinity columns
US6025155A (en) * 1996-04-10 2000-02-15 Chromos Molecular Systems, Inc. Artificial chromosomes, uses thereof and methods for preparing artificial chromosomes
US5804585A (en) * 1996-04-15 1998-09-08 Texas Biotechnology Corporation Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin
DK0948495T3 (da) * 1996-11-19 2004-06-01 Amgen Inc Aryl- og heteroarylsubstitueret, kondenseret pyrrol som antiinflammatoriske midler
US6294330B1 (en) * 1997-01-31 2001-09-25 Odyssey Pharmaceuticals Inc. Protein fragment complementation assays for the detection of biological or drug interactions
WO1998039471A1 (en) * 1997-03-07 1998-09-11 Tropix, Inc. Protease inhibtor assay
US5977131A (en) 1997-04-09 1999-11-02 Pfizer Inc. Azaindole-ethylamine derivatives as nicotinic acetylcholine receptor binding agents
US6096718A (en) * 1997-06-05 2000-08-01 Gene Targeting Corp. Tissue specific adenovirus vectors for breast cancer treatment
RU2199532C2 (ru) 1997-06-27 2003-02-27 Фудзисава Фармасьютикал Ко., Лтд. Сульфонамидное соединение
US6235769B1 (en) * 1997-07-03 2001-05-22 Sugen, Inc. Methods of preventing and treating neurological disorders with compounds that modulate the function of the C-RET receptor protein tyrosine kinase
US6826296B2 (en) * 1997-07-25 2004-11-30 Affymetrix, Inc. Method and system for providing a probe array chip design database
US6161776A (en) * 1997-08-12 2000-12-19 Nibco Inc. Multi-layered, porous mat turf irrigation apparatus and method
IL134702A (en) * 1997-09-11 2004-03-28 Bioventures Inc High density arrays and methods of making the same
US6178384B1 (en) * 1997-09-29 2001-01-23 The Trustees Of Columbia University In The City Of New York Method and apparatus for selecting a molecule based on conformational free energy
US6465178B2 (en) * 1997-09-30 2002-10-15 Surmodics, Inc. Target molecule attachment to surfaces
US6048695A (en) * 1998-05-04 2000-04-11 Baylor College Of Medicine Chemically modified nucleic acids and methods for coupling nucleic acids to solid support
CA2319495A1 (en) * 1998-06-08 1999-12-16 Advanced Medicine, Inc. Multibinding inhibitors of microsomal triglyceride transferase protein
US6113913A (en) * 1998-06-26 2000-09-05 Genvec, Inc. Recombinant adenovirus
WO2000012074A2 (en) 1998-08-28 2000-03-09 Scios Inc. Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6350786B1 (en) 1998-09-22 2002-02-26 Hoffmann-La Roche Inc. Stable complexes of poorly soluble compounds in ionic polymers
US6277628B1 (en) * 1998-10-02 2001-08-21 Incyte Genomics, Inc. Linear microarrays
US6277489B1 (en) * 1998-12-04 2001-08-21 The Regents Of The University Of California Support for high performance affinity chromatography and other uses
US20010001449A1 (en) 1998-12-30 2001-05-24 Thomas R. Kiliany Low-pressure hydrocracking process
US7008945B1 (en) * 1999-03-17 2006-03-07 Astrazeneca Ab Amide derivatives
GB9906566D0 (en) 1999-03-23 1999-05-19 Zeneca Ltd Chemical compounds
US6221653B1 (en) * 1999-04-27 2001-04-24 Agilent Technologies, Inc. Method of performing array-based hybridization assays using thermal inkjet deposition of sample fluids
FR2793793B1 (fr) * 1999-05-19 2004-02-27 Adir Nouveaux derives dimeriques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
TWI234557B (en) * 1999-05-26 2005-06-21 Telik Inc Novel naphthalene ureas as glucose uptake enhancers
US6653151B2 (en) * 1999-07-30 2003-11-25 Large Scale Proteomics Corporation Dry deposition of materials for microarrays using matrix displacement
EP1106603A3 (en) * 1999-12-06 2003-11-19 Fuji Photo Film Co., Ltd. DNA chip and reactive solid carrier
AU784266B2 (en) * 1999-12-22 2006-03-02 Sugen, Inc. Indolinone derivatives for modulation of c-kit tyrosine kinase
DE60022906T2 (de) 1999-12-28 2006-07-06 Eisai Co., Ltd. Heterozyklische verbindungen mit sulfonamid-gruppen
JP2001278886A (ja) * 2000-03-28 2001-10-10 Dai Ichi Seiyaku Co Ltd ベンゾオキサジン誘導体及びこれを含有する医薬
GB0007934D0 (en) * 2000-03-31 2000-05-17 Darwin Discovery Ltd Chemical compounds
KR20030080013A (ko) 2001-02-21 2003-10-10 에자이 가부시키가이샤 인테그린 발현 억제를 통한 혈관 신생 억제제의 효과를검정하는 방법
JP4204326B2 (ja) 2001-04-11 2009-01-07 千寿製薬株式会社 視覚機能障害改善剤
AU2002258971A1 (en) 2001-04-24 2002-11-05 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-benzodioxan
GB0114417D0 (en) * 2001-06-13 2001-08-08 Boc Group Plc Lubricating systems for regenerative vacuum pumps
WO2002102783A1 (en) 2001-06-19 2002-12-27 Merck & Co., Inc. Tyrosine kinase inhibitors
US7291639B2 (en) 2001-06-20 2007-11-06 Wyeth Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
UA75425C2 (en) 2001-07-09 2006-04-17 Piperazine oxime derivatives with antagonistic activity to nk-1 receptor, use thereof, a pharmaceutical composition based thereon, a method for producing and a method for producing intermediary compounds
GB0117583D0 (en) 2001-07-19 2001-09-12 Astrazeneca Ab Novel compounds
US6858860B2 (en) * 2001-07-24 2005-02-22 Seiko Epson Corporation Apparatus and method for measuring natural period of liquid
GB0118479D0 (en) 2001-07-28 2001-09-19 Astrazeneca Ab Novel compounds
WO2003028724A1 (en) 2001-10-04 2003-04-10 Smithkline Beecham Corporation Chk1 kinase inhibitors
US20050014942A1 (en) 2001-10-30 2005-01-20 Yasufumi Maruyama Amide derivatives and drugs
US20030236277A1 (en) 2002-02-14 2003-12-25 Kadow John F. Indole, azaindole and related heterocyclic pyrrolidine derivatives
US6884889B2 (en) 2002-03-25 2005-04-26 Bristol-Myers Squibb Co. Processes for the preparation of antiviral 7-azaindole derivatives
DE60316542T2 (de) 2002-03-28 2008-07-03 Eisai R&D Management Co., Ltd. 7-azaindole als inhibitoren c-jun n-terminaler kinasen zur behandlung neurodegenerativer störungen
JP2005534619A (ja) 2002-03-28 2005-11-17 エーザイ株式会社 Ｃ−ｊｕｎｎ−末端キナーゼ阻害剤としてのアザインドール
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
TW200403243A (en) 2002-07-18 2004-03-01 Wyeth Corp 1-Heterocyclylalkyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US6878887B2 (en) * 2002-08-07 2005-04-12 Matsushita Electric Industrial Co., Ltd. Anti-malfunction mechanism for variable output device
BR122012021252B8 (pt) 2002-09-06 2021-05-25 Cerulean Pharma Inc polímeros à base de ciclodextrina para o fornecimento de agentes terapêuticos ligados a eles por covalência
WO2004024895A2 (en) 2002-09-16 2004-03-25 Plexxikon, Inc. Crystal structure of pim-1 kinase
WO2004054581A2 (en) * 2002-12-13 2004-07-01 Smithkline Beecham Corporation Cyclohexyl compounds as ccr5 antagonists
CN1744899A (zh) * 2002-12-13 2006-03-08 史密丝克莱恩比彻姆公司 作为ccr5拮抗剂的哌啶衍生物
US7696225B2 (en) * 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
SE0300119D0 (sv) 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
SE0300120D0 (sv) 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
US20050085463A1 (en) * 2003-01-23 2005-04-21 Weiner David M. Use of N-desmethylclozapine to treat human neuropsychiatric disease
TW200418830A (en) 2003-02-14 2004-10-01 Wyeth Corp Heterocyclyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands
WO2004078923A2 (en) 2003-02-28 2004-09-16 Plexxikon, Inc. Pyk2 crystal structure and uses
WO2005028624A2 (en) 2003-09-15 2005-03-31 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
DE10357510A1 (de) 2003-12-09 2005-07-07 Bayer Healthcare Ag Heteroarylsubstituierte Benzole
CA2550361C (en) * 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
DK2119771T3 (en) 2003-12-24 2018-12-10 Dupont Nutrition Biosci Aps PROTEINS
GB0330042D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them
GB0330043D0 (en) * 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them
GB0403635D0 (en) 2004-02-18 2004-03-24 Devgen Nv Pyridinocarboxamides with improved activity as kinase inhibitors
GB0405055D0 (en) 2004-03-05 2004-04-07 Eisai London Res Lab Ltd JNK inhibitors
US7507826B2 (en) 2004-03-30 2009-03-24 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
TW200616632A (en) * 2004-06-17 2006-06-01 Plexxikon Inc Compounds modulating c-kit activity and uses therefor
US7498342B2 (en) * 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
WO2006004984A1 (en) 2004-06-30 2006-01-12 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
WO2006015124A2 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
NZ553267A (en) 2004-07-27 2010-09-30 Sgx Pharmaceuticals Inc Pyrrolo-pyridine kinase modulators
US7626021B2 (en) * 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7709645B2 (en) * 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
GB0419192D0 (en) * 2004-08-27 2004-09-29 Merck Sharp & Dohme Therapeutic agents
EP1874769B1 (de) 2005-04-25 2011-09-14 Merck Patent GmbH Neuartige aza-heterozyklen als kinase-inhibitoren
US7846941B2 (en) * 2005-05-17 2010-12-07 Plexxikon, Inc. Compounds modulating c-kit and c-fms activity and uses therefor
KR20080016659A (ko) 2005-05-20 2008-02-21 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로서 유용한 피롤로피리딘
MY153898A (en) 2005-06-22 2015-04-15 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
GB0516156D0 (en) 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK inhibitors
JP2009530415A (ja) 2006-03-20 2009-08-27 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 医薬組成物
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
TW200908968A (en) * 2007-05-29 2009-03-01 Sgx Pharmaceuticals Inc Substituted pyrrolopyridines and pyrazolopyridines as kinase modulators
TW201041888A (en) * 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3124610A (en) * 1964-03-10 Preparation of intermediates
US3067237A (en) * 1959-04-14 1962-12-04 Sterling Drug Inc Lower-alkyl mono-or bis-(alkanesulfonamido) benzoate esters
WO2003101959A1 (en) * 2002-05-31 2003-12-11 Glaxo Group Limited Pyrrole compounds for the treatment of prostaglandin mediated diseases
WO2004016610A1 (en) * 2002-08-14 2004-02-26 Astrazeneca Ab Substituted pyrrolopyridines

Also Published As

Publication number Publication date
CY2012021I2 (el) 2015-08-05
RU2008100933A (ru) 2009-07-27
ZA200711152B (en) 2012-06-27
TWI432193B (zh) 2014-04-01
US8143271B2 (en) 2012-03-27
BRPI0611863B1 (pt) 2021-11-23
EP3088400A1 (en) 2016-11-02
RU2565071C2 (ru) 2015-10-20
RS52010B (en) 2012-04-30
AU2006261993B2 (en) 2011-11-17
IL188248A (en) 2012-04-30
EP1893612A1 (en) 2008-03-05
US20120022098A1 (en) 2012-01-26
IL188248A0 (en) 2008-04-13
HUE027370T2 (en) 2016-10-28
CR20130216A (es) 2013-07-02
RU2012150759A (ru) 2014-06-10
PT1893612E (pt) 2011-11-21
NO2014006I2 (no) 2014-03-20
US20150290205A1 (en) 2015-10-15
PL1893612T3 (pl) 2012-01-31
ECSP088121A (es) 2008-02-20
AU2006261993A1 (en) 2007-01-04
HUS1200009I1 (hu) 2018-09-28
HK1114610A1 (en) 2008-11-07
CA2613015A1 (en) 2007-01-04
CN101243084B (zh) 2012-03-07
US8415469B2 (en) 2013-04-09
PL2395004T3 (pl) 2016-08-31
US20130261117A1 (en) 2013-10-03
EP2395004B1 (en) 2016-01-20
NO20076659L (no) 2008-03-18
AR078519A2 (es) 2011-11-16
JP5007304B2 (ja) 2012-08-22
MY147410A (en) 2012-11-30
US8470818B2 (en) 2013-06-25
CN102603581A (zh) 2012-07-25
TW201345906A (zh) 2013-11-16
US7863288B2 (en) 2011-01-04
MX2007016463A (es) 2008-03-04
CA2613015C (en) 2012-04-03
KR20080030619A (ko) 2008-04-04
US20180111929A1 (en) 2018-04-26
NZ565255A (en) 2010-04-30
US20100256365A1 (en) 2010-10-07
TWI522337B (zh) 2016-02-21
DK1893612T3 (da) 2011-11-21
ATE518860T1 (de) 2011-08-15
EP2395004A2 (en) 2011-12-14
NO2014006I1 (no) 2014-06-02
EP1893612B1 (en) 2011-08-03
TW200804370A (en) 2008-01-16
CN102206216A (zh) 2011-10-05
RU2418800C2 (ru) 2011-05-20
CR9677A (es) 2008-03-26
MY153898A (en) 2015-04-15
CY1111996T1 (el) 2015-08-05
CY2012021I1 (el) 2015-08-05
RU2629999C2 (ru) 2017-09-05
MA29612B1 (fr) 2008-07-01
LU92035I2 (fr) 2012-08-28
TW201514140A (zh) 2015-04-16
ZA201202024B (en) 2016-02-24
UA95244C2 (ru) 2011-07-25
US20160176865A1 (en) 2016-06-23
JP2008546797A (ja) 2008-12-25
AR054624A1 (es) 2007-07-04
EP2395004A3 (en) 2012-04-04
ES2565992T3 (es) 2016-04-08
US20110059963A1 (en) 2011-03-10
KR101125919B1 (ko) 2012-06-12
LU92035I9 (US07863288-20110104-C00114.png) 2019-01-04
US20130303534A1 (en) 2013-11-14
SI1893612T1 (sl) 2012-03-30
CN101243084A (zh) 2008-08-13
WO2007002325A1 (en) 2007-01-04
RU2011101140A (ru) 2012-07-20
DE122012000043I1 (de) 2012-09-13
NO333913B1 (no) 2013-10-21
ZA201202026B (en) 2012-11-28
TWI473808B (zh) 2015-02-21
US20120053177A1 (en) 2012-03-01
US20100249118A1 (en) 2010-09-30
DK2395004T3 (en) 2016-03-21
WO2007002433A1 (en) 2007-01-04
PE20070100A1 (es) 2007-03-10
SI2395004T1 (sl) 2016-05-31
CN102206216B (zh) 2014-11-12
HK1164866A1 (zh) 2012-09-28
ZA201202025B (en) 2022-03-30
ES2371397T3 (es) 2011-12-30
BRPI0611863A2 (pt) 2008-12-02

Similar Documents

Publication Publication Date Title
CN102603581B (zh) 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
US7820664B2 (en) Inhibitors of MEK
CN102093364B (zh) 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物
TWI826471B (zh) 化合物
CN101184734B (zh) 治疗细胞增殖紊乱的化合物和方法
KR101761963B1 (ko) 카테콜 ｏ－메틸 트랜스퍼라제의 억제제 및 정신병적 장애의 치료에서의 그의 용도
TW202108569A (zh) THR-β調節劑及其使用方法
CN104302358A (zh) 3-芳基-5-取代的异喹啉-1-酮化合物和它们的治疗用途
WO2015058589A1 (zh) 吡啶酮类衍生物、其制备方法及其在医药上的应用
CN101948425A (zh) 作为糖皮质激素配体的化合物、包含它们的药物组合物、试剂盒及其制备方法
JP2008545652A (ja) ｃ−ｋｉｔおよびｃ−ｆｍｓ活性を調節する化合物およびその用途
WO2021147879A1 (zh) Shp2抑制剂及其应用
CN108368116A (zh) Janus激酶抑制剂、其组合物及用途
CN1816536B (zh) 大麻素受体调节剂
CN110114343A (zh) 吡唑并嘧啶化合物及其使用方法
JP2021528454A (ja) 化合物
CN110066276A (zh) 芳香杂环化合物、其中间体、制备方法、药物组合物和应用
JP2007502298A (ja) 化合物
JP2010502648A (ja) Ｐｐａｒモジュレーターとして有用な１ｈ−インドール−２−カルボン酸誘導体
WO2019144765A1 (zh) 芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用
JP2015533778A (ja) がんの治療のための新規フェニル−ピリジン／ピラジンアミド
WO2009111260A1 (en) Phenylsulfonamide-substituted, pyrazolo[1, 5-a]pyrimidines, methods for preparation and uses thereof
CN107635961A (zh) 作为5‑氧代‑ete受体拮抗剂的吲哚类似物及其使用方法
TW202134213A (zh) 具有水解磷脂酸受體作動活性之化合物及其醫藥用途
CN1976705B (zh) 作为用于治疗炎性疾病和糖尿病的糖皮质激素配体的1,1,1-三氟-4-苯基-4-甲基-2-(1h-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇衍生物和相关化合物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant