CA2954999C - Fused quinoline compounds as pi3k, mtor inhibitors - Google Patents

Fused quinoline compounds as pi3k, mtor inhibitors Download PDF

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Publication number
CA2954999C
CA2954999C CA2954999A CA2954999A CA2954999C CA 2954999 C CA2954999 C CA 2954999C CA 2954999 A CA2954999 A CA 2954999A CA 2954999 A CA2954999 A CA 2954999A CA 2954999 C CA2954999 C CA 2954999C
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Prior art keywords
trifluoromethyl
phenyl
hexadeca
pentaazatetracyclo
c6alkyl
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CA2954999A
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English (en)
French (fr)
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CA2954999A1 (en
Inventor
Guoqing Paul Chen
Changren Yan
Michael Reale
Monica Chen
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Advenchen Pharmaceuticals Nanjing Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/22Heterocyclic 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 systems contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/14Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2954999A 2014-07-14 2015-07-11 Fused quinoline compounds as pi3k, mtor inhibitors Active CA2954999C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462024192P 2014-07-14 2014-07-14
US62/024,192 2014-07-14
PCT/US2015/040076 WO2016010869A2 (en) 2014-07-14 2015-07-11 FUSED QUINOLINE COMPUNDS AS PI3K, mTOR INHIBITORS

Publications (2)

Publication Number Publication Date
CA2954999A1 CA2954999A1 (en) 2016-01-21
CA2954999C true CA2954999C (en) 2020-01-07

Family

ID=55079153

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2954999A Active CA2954999C (en) 2014-07-14 2015-07-11 Fused quinoline compounds as pi3k, mtor inhibitors

Country Status (9)

Country Link
US (1) US10112945B2 (enExample)
EP (1) EP3169687B1 (enExample)
JP (1) JP6380777B2 (enExample)
KR (1) KR102426138B1 (enExample)
CN (1) CN105722840B (enExample)
AU (1) AU2015290007B2 (enExample)
CA (1) CA2954999C (enExample)
ES (1) ES2714100T3 (enExample)
WO (1) WO2016010869A2 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105311029A (zh) 2014-06-06 2016-02-10 正大天晴药业集团股份有限公司 抗肿瘤活性的喹啉衍生物
CN105311030B (zh) 2014-06-06 2020-03-24 正大天晴药业集团股份有限公司 用于抗肿瘤的螺取代化合物
WO2016091168A1 (zh) 2014-12-09 2016-06-16 正大天晴药业集团股份有限公司 抗非小细胞肺癌的喹啉衍生物
US9751859B2 (en) 2015-05-04 2017-09-05 Advenchen Pharmaceuticals, LLC Process for preparing an anti-cancer agent, 1-((4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine, its crystalline form and its salts
CN110078730B (zh) * 2015-07-11 2021-09-07 南京爱德程医药科技有限公司 作为pi3k/mtor抑制剂的喹啉取代的稠合喹啉化合物
CN107296811B (zh) 2016-04-15 2022-12-30 正大天晴药业集团股份有限公司 一种用于治疗胃癌的喹啉衍生物
CN107037153B (zh) * 2017-04-21 2019-05-14 常州佳德医药科技有限公司 高效液相色谱法检测al58805原料药或药物制剂中基因毒性杂质的方法
CN111936467B (zh) 2018-03-02 2022-02-18 正大天晴药业集团股份有限公司 作为c-Met激酶抑制剂的化合物的结晶及其制备方法和用途

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0211649D0 (en) * 2002-05-21 2002-07-03 Novartis Ag Organic compounds
GB0510390D0 (en) * 2005-05-20 2005-06-29 Novartis Ag Organic compounds
US9370508B2 (en) * 2007-02-20 2016-06-21 Novartis Ag Imidazoquinolines as dual lipid kinase and mTOR inhibitors
US8163923B2 (en) 2007-03-14 2012-04-24 Advenchen Laboratories, Llc Spiro substituted compounds as angiogenesis inhibitors
US8148532B2 (en) 2007-03-14 2012-04-03 Guoqing Paul Chen Spiro substituted compounds as angiogenesis inhibitors
WO2009155527A2 (en) * 2008-06-19 2009-12-23 Progenics Pharmaceuticals, Inc. Phosphatidylinositol 3 kinase inhibitors
IT1393351B1 (it) 2009-03-16 2012-04-20 Eos Ethical Oncology Science Spa In Forma Abbreviata Eos Spa Procedimento per la preparazione della 6-(7-((1-amminociclopropil)metossi)-6-metossichinolin-4-ilossi)-n-metil-1-naftammide e suoi intermedi di sintesi
CN103664892B (zh) 2010-08-01 2015-09-02 正大天晴药业集团股份有限公司 喹啉衍生物的结晶
US9181264B2 (en) * 2010-09-16 2015-11-10 Hutchison Medipharma Limited Fused heteroaryls and their uses
MA38274A1 (fr) 2013-01-18 2017-02-28 Advenchen Pharmaceuticals Llc Procédé pour l'élaboration d'un agent antitumoral, la 6-(7-((1-amino-cyclo-propyl)-méthoxy)-6- méthoxyquinolin-4-yloxy)-n-méthyl-1-naphthamide, et de sa forme cristalline
CN105311029A (zh) 2014-06-06 2016-02-10 正大天晴药业集团股份有限公司 抗肿瘤活性的喹啉衍生物
CN105311030B (zh) 2014-06-06 2020-03-24 正大天晴药业集团股份有限公司 用于抗肿瘤的螺取代化合物
US9751859B2 (en) 2015-05-04 2017-09-05 Advenchen Pharmaceuticals, LLC Process for preparing an anti-cancer agent, 1-((4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine, its crystalline form and its salts

Also Published As

Publication number Publication date
EP3169687A2 (en) 2017-05-24
KR20170035944A (ko) 2017-03-31
AU2015290007A1 (en) 2017-02-23
CA2954999A1 (en) 2016-01-21
AU2015290007B2 (en) 2019-11-21
US10112945B2 (en) 2018-10-30
US20170174687A1 (en) 2017-06-22
CN105722840A (zh) 2016-06-29
EP3169687B1 (en) 2019-01-02
WO2016010869A3 (en) 2016-04-07
EP3169687A4 (en) 2018-01-03
CN105722840B (zh) 2018-01-05
ES2714100T3 (es) 2019-05-27
JP2017534569A (ja) 2017-11-24
KR102426138B1 (ko) 2022-07-28
WO2016010869A2 (en) 2016-01-21
JP6380777B2 (ja) 2018-08-29

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