TWI641592B - 激酶抑制劑 - Google Patents

激酶抑制劑 Download PDF

Info

Publication number
TWI641592B
TWI641592B TW103112073A TW103112073A TWI641592B TW I641592 B TWI641592 B TW I641592B TW 103112073 A TW103112073 A TW 103112073A TW 103112073 A TW103112073 A TW 103112073A TW I641592 B TWI641592 B TW I641592B
Authority
TW
Taiwan
Prior art keywords
methoxy
oxy
ethoxy
butyl
tertiary
Prior art date
Application number
TW103112073A
Other languages
English (en)
Chinese (zh)
Other versions
TW201529556A (zh
Inventor
湯瑪士 貝克
馬修 菲
葛瑞瑟 哈波托
維登 哈辛貝戈維克
皮恩杰 麥格哈尼
亞倫 里格拜
柯林 山姆布魯克
史蒂芬 索恩
Original Assignee
英商瑞斯比維特有限公司
英商托比維特藥品有限公司
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
Priority claimed from GB201305945A external-priority patent/GB201305945D0/en
Priority claimed from GBGB1322678.2A external-priority patent/GB201322678D0/en
Priority claimed from GB201402647A external-priority patent/GB201402647D0/en
Application filed by 英商瑞斯比維特有限公司, 英商托比維特藥品有限公司 filed Critical 英商瑞斯比維特有限公司
Publication of TW201529556A publication Critical patent/TW201529556A/zh
Application granted granted Critical
Publication of TWI641592B publication Critical patent/TWI641592B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • A61K31/55—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
    • 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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • 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
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/28—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
    • C07D211/86—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
TW103112073A 2013-04-02 2014-04-01 激酶抑制劑 TWI641592B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB201305945A GB201305945D0 (en) 2013-04-02 2013-04-02 New compounds
??1305945.6 2013-04-02
??1322678.2 2013-12-20
GBGB1322678.2A GB201322678D0 (en) 2013-12-20 2013-12-20 New compounds
??1402647.0 2014-02-14
GB201402647A GB201402647D0 (en) 2014-02-14 2014-02-14 New compounds

Publications (2)

Publication Number Publication Date
TW201529556A TW201529556A (zh) 2015-08-01
TWI641592B true TWI641592B (zh) 2018-11-21

Family

ID=50434228

Family Applications (1)

Application Number Title Priority Date Filing Date
TW103112073A TWI641592B (zh) 2013-04-02 2014-04-01 激酶抑制劑

Country Status (14)

Country Link
US (5) US9481648B2 (OSRAM)
EP (2) EP2981535B8 (OSRAM)
JP (2) JP6464384B2 (OSRAM)
KR (3) KR102283883B1 (OSRAM)
CN (2) CN105408315B (OSRAM)
AU (2) AU2014246866B2 (OSRAM)
BR (2) BR112015024671A2 (OSRAM)
CA (1) CA2907663A1 (OSRAM)
DK (2) DK2981526T3 (OSRAM)
EA (2) EA030483B1 (OSRAM)
ES (2) ES2904277T3 (OSRAM)
MX (2) MX363950B (OSRAM)
TW (1) TWI641592B (OSRAM)
WO (2) WO2014162126A1 (OSRAM)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101945869B (zh) 2007-12-19 2014-06-18 癌症研究技术有限公司 吡啶并[2,3-b]吡嗪-8-取代化合物及其用途
US8815896B2 (en) 2010-02-01 2014-08-26 The Institute Of Cancer Research: Royal Cancer Hospital 1-(5-tert-butyl-2-phenyl-2H-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-B]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy
PE20142355A1 (es) 2011-10-03 2015-01-10 Respivert Ltd 1-pirazolil-3-(4-((2-anilinopirimidin-4-il)oxi)naftalen-1-il)ureas como inhibidores de proteinas cinasas activadas por mitogeno p38
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
WO2014033449A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
US20150225373A1 (en) 2012-08-29 2015-08-13 Respivert Limited Kinase inhibitors
WO2014033446A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
WO2014076484A1 (en) 2012-11-16 2014-05-22 Respivert Limited Kinase inhibitors
WO2014140582A1 (en) 2013-03-14 2014-09-18 Respivert Limited Kinase inhibitors
EA030483B1 (ru) 2013-04-02 2018-08-31 Респайверт Лимитед Производные мочевины, полезные в качестве ингибиторов киназы
WO2014162121A1 (en) 2013-04-02 2014-10-09 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
GB201320732D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Methods of chemical synthesis
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
EP3083604A1 (en) 2013-12-20 2016-10-26 Respivert Limited Urea derivatives useful as kinase inhibitors
PT3357919T (pt) 2014-02-14 2020-02-20 Respivert Ltd Compostos heterocíclicos aromáticos como compostos antiinflamatórios
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
WO2017108737A1 (en) 2015-12-23 2017-06-29 Chiesi Farmaceutici S.P.A. 1-(3-tert-butyl-phenyl)-3-(4-([1,2,4]triazolo[4,3-a]pyridin-6-yloxy)-1,2,3,4-tetrahydro- naphthalen-1-yl)-urea derivatives and their use as p38 mapk inhibitors
MA44607A (fr) 2016-04-06 2021-05-19 Oxular Acquisitions Ltd Inhibiteurs de kinase
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
CA3078232A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. Use of p38 inhibitors to reduce expression of dux4
CN110878055B (zh) * 2018-09-06 2021-02-05 中国科学院化学研究所 一种制备羰基杂环类化合物的方法
WO2020118194A1 (en) 2018-12-07 2020-06-11 University Of Maryland, Baltimore NON-ATP/CATALYTIC SITE p38 MITOGEN ACTIVATED PROTEIN KINASE INHIBITORS
CN117120422A (zh) * 2021-03-23 2023-11-24 Gen1E生命科学公司 取代的萘基P38α丝裂原活化的蛋白激酶抑制剂

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014870A1 (en) * 2002-08-08 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Fluorinated phenyl-naphthalenyl-urea compounds as inhibitors of cytokines involved in inflammatory processes

Family Cites Families (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4344960B2 (ja) 1997-05-23 2009-10-14 バイエル、コーポレイション アリール尿素によるｐ３８キナーゼ活性の阻害
CA2308428A1 (en) 1997-11-03 1999-05-14 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
EP1158985B1 (en) 1999-01-13 2011-12-28 Bayer HealthCare LLC OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
HUP0202248A3 (en) 1999-03-12 2006-06-28 Boehringer Ingelheim Pharma Compounds useful as anti-inflammatory agents
MXPA02000314A (es) 1999-07-09 2004-06-22 Boehringer Ingelheim Pharma Proceso novedoso para la sintesis de compuestos de urea substituidos con heteroarilo.
CA2389360C (en) 1999-11-16 2008-06-03 Steffen Breitfelder Urea derivatives as anti-inflammatory agents
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
US6492529B1 (en) 2000-01-18 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Bis pyrazole-1H-pyrazole intermediates and their synthesis
CA2490819A1 (en) 2001-04-13 2002-10-24 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as anti-inflammatory agents
WO2002083628A1 (en) 2001-04-13 2002-10-24 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-disubstituted benzo-fused compounds
JP2004530690A (ja) 2001-05-16 2004-10-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 抗炎症性薬剤として有用なジアリールウレア誘導体
EP1395561A1 (en) 2001-05-25 2004-03-10 Boehringer Ingelheim Pharmaceuticals Inc. Carbamate and oxamide compounds as inhibitors of cytokine production
AU2002316459A1 (en) 2001-07-11 2003-01-29 Boehringer Ingelheim Pharmaceuticals, Inc. Methods of treating cytokine mediated diseases
ES2425739T3 (es) 2002-02-11 2013-10-17 Bayer Healthcare Llc Sorafenib-tosilato para el tratamiento de enfermedades caracterizadas por angiogénesis anormal
US20040023961A1 (en) 2002-02-11 2004-02-05 Bayer Corporation Aryl ureas with raf kinase and angiogenisis inhibiting activity
EP1480973B1 (en) 2002-02-25 2008-02-13 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituted benzofused cycloalkyl urea compounds useful in treating cytokine mediated diseases
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
WO2004113352A1 (en) 2003-06-19 2004-12-29 Amedis Pharmaceuticals Ltd. Silylated heterocyclylurea derivatives as cytokine-inhibitors
JP2007518680A (ja) 2003-06-30 2007-07-12 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド ジ−アリール尿素化合物の製造方法
JP2007503393A (ja) 2003-08-22 2007-02-22 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド Ｃｏｐｄ及び肺高血圧の治療方法
EP1670787B1 (en) 2003-09-11 2012-05-30 iTherX Pharma, Inc. Cytokine inhibitors
WO2005044825A1 (en) 2003-10-21 2005-05-19 Amedis Pharmaceuticals Ltd. Silicon compounds and their use
RU2006122853A (ru) 2003-11-28 2008-01-10 Новартис АГ (CH) Производные диарилмочевины для лечения заболеваний, зависимых от протеинкиназы
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
GB0423554D0 (en) 2004-10-22 2004-11-24 Cancer Rec Tech Ltd Therapeutic compounds
TW200740820A (en) 2005-07-05 2007-11-01 Takeda Pharmaceuticals Co Fused heterocyclic derivatives and use thereof
DOP2006000234A (es) 2005-10-28 2007-05-31 Lilly Co Eli Inhibidores de cinasa
US7790756B2 (en) 2006-10-11 2010-09-07 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
GB0818033D0 (en) 2008-10-02 2008-11-05 Respivert Ltd Novel compound
KR20110070887A (ko) 2008-10-02 2011-06-24 레스피버트 리미티드 Ｐ38 엠에이피 키나제 억제제
KR20110094127A (ko) 2008-12-11 2011-08-19 레스피버트 리미티드 Ｐ38 ｍａｐ 키나제 억제제
GB0905955D0 (en) 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
EP3613729A1 (en) 2009-06-10 2020-02-26 Chugai Seiyaku Kabushiki Kaisha Tetracyclic compounds
GB0921730D0 (en) 2009-12-11 2010-01-27 Respivert Ltd Method of treatment
GB0921731D0 (en) 2009-12-11 2010-01-27 Respivert Ltd Theraputic uses
CN103864657A (zh) 2010-03-15 2014-06-18 宇部兴产株式会社 制备酰胺化合物的方法
GB201005589D0 (en) 2010-04-01 2010-05-19 Respivert Ltd Novel compounds
WO2011124930A1 (en) 2010-04-08 2011-10-13 Respivert Limited P38 map kinase inhibitors
JP5787976B2 (ja) 2010-04-08 2015-09-30 レスピバート・リミテツド Ｐ３８ｍａｐキナーゼ阻害剤としてのピラゾリルウレア
GB201009731D0 (en) * 2010-06-10 2010-07-21 Pulmagen Therapeutics Inflamma Kinase inhibitors
GB201010193D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Medicinal use
JP5973426B2 (ja) 2010-06-17 2016-08-23 レスピバート・リミテツド Ｐ３８ｍａｐｋ阻害剤を含む呼吸器用製剤
GB201010196D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Methods
KR20130141500A (ko) * 2010-09-29 2013-12-26 크리스탈지노믹스(주) 단백질 키나제 억제 활성을 갖는 신규한 아미노퀴나졸린 화합물
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
PE20142355A1 (es) * 2011-10-03 2015-01-10 Respivert Ltd 1-pirazolil-3-(4-((2-anilinopirimidin-4-il)oxi)naftalen-1-il)ureas como inhibidores de proteinas cinasas activadas por mitogeno p38
WO2013083604A1 (en) 2011-12-09 2013-06-13 Chiesi Farmaceutici S.P.A. Kinase inhibitors
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
WO2014033446A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
WO2014033449A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
US20150225373A1 (en) 2012-08-29 2015-08-13 Respivert Limited Kinase inhibitors
WO2014076484A1 (en) 2012-11-16 2014-05-22 Respivert Limited Kinase inhibitors
WO2014140582A1 (en) * 2013-03-14 2014-09-18 Respivert Limited Kinase inhibitors
WO2014162121A1 (en) 2013-04-02 2014-10-09 Topivert Pharma Limited Kinase inhibitors based upon n-alkyl pyrazoles
EA030483B1 (ru) * 2013-04-02 2018-08-31 Респайверт Лимитед Производные мочевины, полезные в качестве ингибиторов киназы
EP3083604A1 (en) 2013-12-20 2016-10-26 Respivert Limited Urea derivatives useful as kinase inhibitors
PT3357919T (pt) 2014-02-14 2020-02-20 Respivert Ltd Compostos heterocíclicos aromáticos como compostos antiinflamatórios
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
MA44607A (fr) * 2016-04-06 2021-05-19 Oxular Acquisitions Ltd Inhibiteurs de kinase

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014870A1 (en) * 2002-08-08 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Fluorinated phenyl-naphthalenyl-urea compounds as inhibitors of cytokines involved in inflammatory processes

Also Published As

Publication number Publication date
BR112015024671A2 (pt) 2017-07-18
MX363949B (es) 2019-04-08
AU2014246870B2 (en) 2018-05-24
MX2015013944A (es) 2015-12-11
US8927563B2 (en) 2015-01-06
MX2015013945A (es) 2015-12-11
US9790174B2 (en) 2017-10-17
CN105408315A (zh) 2016-03-16
EP2981535B1 (en) 2020-12-16
WO2014162122A1 (en) 2014-10-09
EA030483B1 (ru) 2018-08-31
CA2907663A1 (en) 2014-10-09
US20140296271A1 (en) 2014-10-02
AU2014246866B2 (en) 2018-05-10
JP2016519680A (ja) 2016-07-07
BR112015024678B1 (pt) 2023-02-23
DK2981535T3 (da) 2021-03-01
EP2981526B1 (en) 2021-11-03
KR102340654B1 (ko) 2021-12-16
US20160376232A1 (en) 2016-12-29
JP2016515606A (ja) 2016-05-30
AU2014246866A1 (en) 2015-10-01
TW201529556A (zh) 2015-08-01
CN105246884B (zh) 2018-05-22
CN105408315B (zh) 2018-09-14
JP6464384B2 (ja) 2019-02-06
ES2904277T3 (es) 2022-04-04
US20140296208A1 (en) 2014-10-02
KR20150138855A (ko) 2015-12-10
EA201591906A1 (ru) 2016-03-31
EP2981526A1 (en) 2016-02-10
US10435361B2 (en) 2019-10-08
AU2014246870C1 (en) 2018-09-13
US20150166483A1 (en) 2015-06-18
EP2981535A1 (en) 2016-02-10
EA201591907A1 (ru) 2016-02-29
BR112015024678A2 (pt) 2017-07-18
WO2014162126A1 (en) 2014-10-09
KR102283876B1 (ko) 2021-07-29
CN105246884A (zh) 2016-01-13
US20180044288A1 (en) 2018-02-15
EP2981535B8 (en) 2021-03-10
DK2981526T3 (da) 2022-02-07
EA027782B1 (ru) 2017-08-31
KR20210096313A (ko) 2021-08-04
US9481648B2 (en) 2016-11-01
ES2856902T3 (es) 2021-09-28
MX363950B (es) 2019-04-08
AU2014246870A1 (en) 2015-10-01
KR20150136536A (ko) 2015-12-07
JP6495238B2 (ja) 2019-04-03
KR102283883B1 (ko) 2021-07-29

Similar Documents

Publication Publication Date Title
TWI641592B (zh) 激酶抑制劑
TWI751099B (zh) 作為激酶抑制劑之吡唑基脲，包含其之製藥組成物及其用途
JP6514703B2 (ja) キナーゼインヒビターとして有用な尿素誘導体
EP2925742B1 (en) Kinase inhibitors
EP2890701B1 (en) Kinase inhibitors
US9771353B2 (en) Kinase inhibitors based upon N-alkyl pyrazoles
CN109071505B (zh) 激酶抑制剂
HK40051658B (zh) 作为激酶抑制剂的吡唑基-脲

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees