AU2011249912A1 - Pyridone and aza-pyridone compounds and methods of use - Google Patents

Pyridone and aza-pyridone compounds and methods of use Download PDF

Info

Publication number
AU2011249912A1
AU2011249912A1 AU2011249912A AU2011249912A AU2011249912A1 AU 2011249912 A1 AU2011249912 A1 AU 2011249912A1 AU 2011249912 A AU2011249912 A AU 2011249912A AU 2011249912 A AU2011249912 A AU 2011249912A AU 2011249912 A1 AU2011249912 A1 AU 2011249912A1
Authority
AU
Australia
Prior art keywords
methyl
oxo
hydroxymethyl
phenyl
dihydropyridin
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.)
Abandoned
Application number
AU2011249912A
Other languages
English (en)
Inventor
Antonio J. M. Barbosa
Peter A. Blomgren
Kevin S. Currie
Ravi Krishnamoorthy
Jeffrey E. Kropf
Seung H. Lee
Scott A. Mitchell
Daniel Ortwine
Aaron C. Schmitt
Xiaojing Wang
Jianjun Xu
Wendy Young
Honglu Zhang
Zhongdong Zhao
Pavel E. Zhichkin
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.)
Genentech Inc
Gilead Connecticut Inc
Original Assignee
Genentech Inc
Gilead Connecticut Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Genentech Inc, Gilead Connecticut Inc filed Critical Genentech Inc
Publication of AU2011249912A1 publication Critical patent/AU2011249912A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P5/00—Drugs for disorders of the endocrine 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
    • 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
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/62—Halogen-containing esters
    • C07C69/65—Halogen-containing esters of unsaturated acids
    • 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
    • C07D209/52—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 condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Otolaryngology (AREA)
AU2011249912A 2010-05-07 2011-05-06 Pyridone and aza-pyridone compounds and methods of use Abandoned AU2011249912A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US33235310P 2010-05-07 2010-05-07
US61/332,353 2010-05-07
US201161443952P 2011-02-17 2011-02-17
US61/443,952 2011-02-17
PCT/US2011/035596 WO2011140488A1 (en) 2010-05-07 2011-05-06 Pyridone and aza-pyridone compounds and methods of use

Publications (1)

Publication Number Publication Date
AU2011249912A1 true AU2011249912A1 (en) 2012-11-29

Family

ID=44475130

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2011249912A Abandoned AU2011249912A1 (en) 2010-05-07 2011-05-06 Pyridone and aza-pyridone compounds and methods of use

Country Status (19)

Country Link
US (4) US8618107B2 (https=)
EP (1) EP2566869B1 (https=)
JP (1) JP5832524B2 (https=)
KR (2) KR101862327B1 (https=)
CN (3) CN107253963B (https=)
AR (1) AR085683A1 (https=)
AU (1) AU2011249912A1 (https=)
BR (1) BR112012028530A2 (https=)
CA (2) CA2798634C (https=)
ES (1) ES2573716T3 (https=)
IL (3) IL222918B (https=)
MX (1) MX2012012975A (https=)
MY (1) MY160349A (https=)
NZ (1) NZ604004A (https=)
RU (2) RU2617405C2 (https=)
SG (1) SG185462A1 (https=)
TW (1) TWI503319B (https=)
WO (1) WO2011140488A1 (https=)
ZA (1) ZA201209205B (https=)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101862327B1 (ko) 2010-05-07 2018-05-29 질레드 코네티컷 인코포레이티드 피리돈 및 아자-피리돈 화합물 및 사용 방법
WO2012009194A1 (en) * 2010-07-12 2012-01-19 Merck Sharp & Dohme Corp. Tyrosine kinase inhibitors
BR112013007499A2 (pt) * 2010-09-01 2016-07-12 Genentech Inc piridazinonas - métodos de criação e usos
CA2809836C (en) * 2010-09-01 2019-01-15 Gilead Connecticut, Inc. Pyridinones/pyrazinones, method of making, and method of use thereof for the treatment of disorders mediated by bruton's tyrosine kinase
RU2628616C2 (ru) 2011-11-03 2017-08-21 Ф. Хоффманн-Ля Рош Аг Бициклические соединения пиперазина
UA111756C2 (uk) 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
MX2014005289A (es) * 2011-11-03 2014-05-30 Hoffmann La Roche Compuestos de piperazina alquilados.
WO2013067264A1 (en) 2011-11-03 2013-05-10 Genentech, Inc. 8-fluorophthalazin-1 (2h) - one compounds as inhibitors of btk activity
WO2013161848A1 (ja) * 2012-04-27 2013-10-31 カルナバイオサイエンス株式会社 新規１，２，４－トリアジン誘導体
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
WO2014083026A1 (en) 2012-11-30 2014-06-05 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
WO2014108820A1 (en) * 2013-01-08 2014-07-17 Aurigene Discovery Technologies Limited Substituted 2-pyrazinone derivatives as kinase inhibitors
US11039617B2 (en) 2013-01-30 2021-06-22 Agrofresh Inc. Large scale methods of uniformly coating packaging surfaces with a volatile antimicrobial to preserve food freshness
US10070649B2 (en) 2013-01-30 2018-09-11 Agrofresh Inc. Volatile applications against pathogens
WO2014125410A1 (en) * 2013-02-12 2014-08-21 Aurigene Discovery Technologies Limited N-substituted heterocyclic derivatives as kinase inhibitors
HRP20170217T1 (hr) 2013-04-25 2017-04-21 Beigene, Ltd. Fuzinirani heterociklički spojevi kao inhibitori protein kinaze
RU2016101548A (ru) 2013-07-03 2017-08-08 Ф. Хоффманн-Ля Рош Аг Соединения амидов гетероарилпиридона и азапиридона
EA034666B1 (ru) 2013-09-13 2020-03-04 Бейджин Свитзерланд Гмбх Антитело против pd-1 и его применение для лечения рака или вирусной инфекции и фрагмент антитела
WO2015082583A1 (en) 2013-12-05 2015-06-11 F. Hoffmann-La Roche Ag Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality
TWI726608B (zh) 2014-07-03 2021-05-01 英屬開曼群島商百濟神州有限公司 抗pd-l1抗體及其作為治療及診斷之用途
JP6507234B2 (ja) 2014-10-02 2019-04-24 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ブルトンチロシンキナーゼ（ｂｔｋ）によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物
EP3212645B1 (en) * 2014-10-27 2018-11-28 F.Hoffmann-La Roche Ag Process for making tricyclic lactam compounds
JP2018502889A (ja) 2015-01-20 2018-02-01 エックスオーシー ファーマシューティカルズ インコーポレイテッドＸｏｃ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ イソエルゴリン化合物およびその使用
JP6856532B2 (ja) 2015-01-20 2021-04-07 エックスオーシー ファーマシューティカルズ インコーポレイテッドＸｏｃ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ エルゴリン化合物およびその使用
AU2016278040B2 (en) 2015-06-16 2019-07-04 Nanophagix LLC Drug delivery and imaging chemical conjugate, formulations and methods of use thereof
US20200270265A1 (en) * 2016-02-19 2020-08-27 Novartis Ag Tetracyclic pyridone compounds as antivirals
EP4049660B1 (en) 2016-02-29 2025-02-19 F. Hoffmann-La Roche AG Dosage form compositions comprising an inhibitor of bruton's tyrosine kinase
WO2017155879A1 (en) 2016-03-07 2017-09-14 Agrofresh Inc. Synergistic methods of using benzoxaborole compounds and preservative gases as an antimicrobial for crops
EP3448861B1 (en) * 2016-04-28 2021-04-21 F. Hoffmann-La Roche AG A process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one
US10864203B2 (en) 2016-07-05 2020-12-15 Beigene, Ltd. Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer
CA3033827A1 (en) 2016-08-16 2018-02-22 Beigene, Ltd. Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl )-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide,preparation, and uses thereof
PT3500299T (pt) 2016-08-19 2024-02-21 Beigene Switzerland Gmbh Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro
CN109982687A (zh) 2016-09-19 2019-07-05 梅制药公司 联合疗法
SG10202009148XA (en) 2016-12-15 2020-10-29 Hoffmann La Roche Process for preparing btk inhibitors
EP3573989A4 (en) 2017-01-25 2020-11-18 Beigene, Ltd. CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A ] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION AND ASSOCIATED USES
KR102398659B1 (ko) * 2017-03-17 2022-05-16 주식회사 대웅제약 카이네이즈 저해제로서의 피롤로트리아진 유도체
EP3630758A1 (en) 2017-06-01 2020-04-08 Xoc Pharmaceuticals, Inc Ergoline derivatives for use in medicine
TW202515616A (zh) 2017-06-26 2025-04-16 英屬開曼群島商百濟神州有限公司 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
AU2018354972B2 (en) 2017-10-27 2021-07-08 Fresenius Kabi Oncology Ltd. An improved process for the preparation of ribociclib and its salts
AR113796A1 (es) * 2017-11-06 2020-06-10 Lilly Co Eli Compuestos inhibidores de tirosina cinasa de bruton (btk)
JP7091455B2 (ja) * 2017-11-24 2022-06-27 ノバルティス アーゲー ピリジノン誘導体及びそれらの選択的ａｌｋ－２阻害剤としての使用
CN111801334B (zh) 2017-11-29 2023-06-09 百济神州瑞士有限责任公司 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤
CN111741959B (zh) * 2018-02-19 2023-09-05 广州麓鹏制药有限公司 Btk的抑制剂及其突变体
JP7600123B2 (ja) 2018-10-15 2024-12-16 ニューリックス セラピューティクス，インコーポレイテッド ユビキチンプロテオソーム経路を介してｂｔｋを分解するための二官能性化合物
WO2020167518A1 (en) 2019-02-13 2020-08-20 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
EP3930717A1 (en) * 2019-02-25 2022-01-05 Guangzhou Lupeng Pharmaceutical Company Ltd. Inhibitor of btk and mutants thereof
EP3953346A1 (en) 2019-04-09 2022-02-16 Nurix Therapeutics, Inc. 3-substituted piperidine compounds for cbl-b inhibition, and use of a cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus
UY38696A (es) 2019-05-14 2020-11-30 Vertex Pharma Moduladores de alfa-1 antitripsina
EP3969447A1 (en) 2019-05-17 2022-03-23 Nurix Therapeutics, Inc. Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof
WO2020249001A1 (zh) 2019-06-10 2020-12-17 百济神州瑞士有限责任公司 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法
MX2021015675A (es) 2019-06-26 2022-02-03 Nurix Therapeutics Inc Compuestos de bencil-triazol sustituidos para la inhibicion de cbl-b y otros usos de los mismos.
US20220298111A1 (en) * 2019-08-09 2022-09-22 The Regents Of The University Of California Compositions and methods for treating metabolic disease
EP4034141A1 (en) 2019-09-24 2022-08-03 Nurix Therapeutics, Inc. Cbl inhibitors and compositions for expansion of immune cells
WO2021066958A1 (en) * 2019-10-05 2021-04-08 Newave Pharmaceutical Inc. Inhibitor of btk and mutants thereof
EP4045498B1 (en) * 2019-10-14 2025-12-03 The Regents of the University of California Broad spectrum anti-cancer compounds
CN112778311B (zh) * 2019-11-01 2024-06-04 上海翰森生物医药科技有限公司 含氮并环类衍生物抑制剂、其制备方法和应用
US20230024442A1 (en) * 2019-11-08 2023-01-26 Nurix Therapeutics, Inc. Bifunctional compounds for grading btk via ubiquitin proteosome pathway
US11820781B2 (en) 2019-12-04 2023-11-21 Nurix Therapeutics, Inc. Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway
CA3171012A1 (en) 2020-02-20 2021-08-26 Hutchison Medipharma Limited Heteroaryl heterocyclic compounds and uses thereof
WO2021183980A1 (en) 2020-03-13 2021-09-16 Fmc Corporation Substituted pyrimidines and triazines as herbicides
WO2021203014A1 (en) 2020-04-03 2021-10-07 Vertex Pharmaceuticals Incorporated Pyrano[4,3-b]l ndole derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd)
CN115715291B (zh) * 2020-06-18 2025-04-29 上海华汇拓医药科技有限公司 布鲁顿酪氨酸激酶抑制剂及其制备方法
CA3195525A1 (en) 2020-09-21 2022-03-24 Hutchison Medipharma Limited Heteroaryl heterocyclic compounds and uses thereof
WO2022133184A1 (en) * 2020-12-20 2022-06-23 Newave Pharmaceutical Inc. Btk degrader
CN117897388A (zh) * 2020-12-20 2024-04-16 广州麓鹏制药有限公司 Btk蛋白降解剂
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
US12016860B2 (en) 2021-04-08 2024-06-25 Nurix Therapeutics, Inc. Combination therapies with Cbl-b inhibitor compounds
AU2022379494A1 (en) 2021-10-26 2024-05-30 Nurix Therapeutics, Inc. Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading btk
FI4426434T3 (fi) 2021-11-02 2025-11-24 Flare Therapeutics Inc Pparg:n käänteisagonisteja ja niiden käyttöjä
CN114751910B (zh) * 2022-05-17 2023-02-24 重庆文理学院 一种可诱导细胞巨泡式死亡的化合物及其制备方法和应用
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
WO2025201531A1 (zh) * 2024-03-29 2025-10-02 深圳众格生物科技有限公司 三环类化合物及其用途

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
WO2003006151A1 (en) 2001-07-12 2003-01-23 Avecia Limited Microencapsulated catalyst, methods of preparation and methods of use thereof
RU2418788C2 (ru) * 2005-03-10 2011-05-20 Сги Фармасьютиклз, Инк. Некоторые замещенные амиды, способ их получения и способ их применения
HRP20110498T1 (hr) 2005-10-07 2011-08-31 Exelixis Azetidini kao inhibitori mek za liječenje proliferativnih bolesti
CN101437820A (zh) * 2006-03-07 2009-05-20 阿雷生物药品公司 杂二环吡唑化合物和使用方法
CN101472884A (zh) * 2006-06-20 2009-07-01 弗·哈夫曼-拉罗切有限公司 1,2,3,4-四氢化萘和茚满衍生物及其用途
AR063706A1 (es) * 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
WO2008058037A1 (en) * 2006-11-03 2008-05-15 Irm Llc Compounds and compositions as protein kinase inhibitors
CL2008002793A1 (es) * 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
WO2009053269A1 (en) * 2007-10-23 2009-04-30 F. Hoffmann-La Roche Ag Novel kinase inhibitors
CA2710462C (en) * 2008-02-05 2015-11-24 F. Hoffmann-La Roche Ag Pyridinones and pyridazinones
US8426424B2 (en) * 2008-05-06 2013-04-23 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
ES2552320T3 (es) * 2008-06-24 2015-11-27 F. Hoffmann-La Roche Ag Nuevas piridín-2-onas y piridazín-3-onas sustituidas
BRPI0913879A2 (pt) * 2008-07-02 2019-09-24 Hoffmann La Roche fenilpirazinonas como inibidores de quinase
KR101862327B1 (ko) 2010-05-07 2018-05-29 질레드 코네티컷 인코포레이티드 피리돈 및 아자-피리돈 화합물 및 사용 방법

Also Published As

Publication number Publication date
IL263780A (en) 2019-01-31
CN103038233A (zh) 2013-04-10
RU2017112518A (ru) 2019-01-25
SG185462A1 (en) 2012-12-28
KR101862327B1 (ko) 2018-05-29
CN110818724B (zh) 2020-11-13
HK1180326A1 (zh) 2013-10-18
CN107253963B (zh) 2020-04-14
CN103038233B (zh) 2017-06-20
CA2798634C (en) 2019-04-16
US20140057896A1 (en) 2014-02-27
MY160349A (en) 2017-02-28
TWI503319B (zh) 2015-10-11
US20180179229A1 (en) 2018-06-28
KR20180062465A (ko) 2018-06-08
RU2012152548A (ru) 2014-06-20
TW201206926A (en) 2012-02-16
IL222918B (en) 2019-11-28
IL269858A (en) 2019-11-28
CA3034600A1 (en) 2011-11-10
CA3034600C (en) 2020-11-10
WO2011140488A1 (en) 2011-11-10
RU2617405C2 (ru) 2017-04-25
ES2573716T3 (es) 2016-06-09
EP2566869A1 (en) 2013-03-13
MX2012012975A (es) 2013-02-26
KR101954044B1 (ko) 2019-03-04
US8618107B2 (en) 2013-12-31
HK1243417A1 (zh) 2018-07-13
ZA201209205B (en) 2013-08-28
CN110818724A (zh) 2020-02-21
NZ604004A (en) 2014-06-27
JP5832524B2 (ja) 2015-12-16
US20170073356A1 (en) 2017-03-16
CA2798634A1 (en) 2011-11-10
CN107253963A (zh) 2017-10-17
JP2013528595A (ja) 2013-07-11
US10344040B2 (en) 2019-07-09
US9505785B2 (en) 2016-11-29
US20120010191A1 (en) 2012-01-12
BR112012028530A2 (pt) 2017-12-19
RU2017112518A3 (https=) 2020-07-22
AR085683A1 (es) 2013-10-23
US10053469B2 (en) 2018-08-21
KR20140024203A (ko) 2014-02-28
EP2566869B1 (en) 2016-03-02

Similar Documents

Publication Publication Date Title
AU2020202707B2 (en) Heteroaryl pyridone and aza-pyridone compounds as inhibitors of Btk activity
US10344040B2 (en) Pyridone and aza-pyridone compounds and methods of use
HK1180326B (en) Pyridone and aza-pyridone compounds and methods of use
BR112014010459B1 (pt) Compostos e composição farmacêutica
BR122020017743B1 (pt) Processo para fabricação de uma composição farmacêutica e uso de uma composição farmacêutica

Legal Events

Date Code Title Description
MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application