AU2011285247B2 - Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70S6K - Google Patents

Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70S6K Download PDF

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Publication number
AU2011285247B2
AU2011285247B2 AU2011285247A AU2011285247A AU2011285247B2 AU 2011285247 B2 AU2011285247 B2 AU 2011285247B2 AU 2011285247 A AU2011285247 A AU 2011285247A AU 2011285247 A AU2011285247 A AU 2011285247A AU 2011285247 B2 AU2011285247 B2 AU 2011285247B2
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methyl
ethyl
substituted methylene
methylamino
monosubstituted
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AU2011285247A1 (en
Inventor
Lizbeth Celeste DESELM
Bayard R. Huck
Reinaldo C. Jones
Srinivasa R. Karra
Ruoxi Lan
Igor Mochalkin
Constantin Neagu
Thomas E. Richardson
Amanda E. Sutton
Yufang Xiao
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Merck Patent GmbH
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Merck Patent GmbH
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • 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
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/74—Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2011285247A 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70S6K Ceased AU2011285247B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36896410P 2010-07-29 2010-07-29
US61/368,964 2010-07-29
PCT/EP2011/003272 WO2012013282A1 (en) 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k

Publications (2)

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AU2011285247A1 AU2011285247A1 (en) 2013-03-14
AU2011285247B2 true AU2011285247B2 (en) 2016-08-04

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AU2011285247A Ceased AU2011285247B2 (en) 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70S6K

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US (1) US8710044B2 (enExample)
EP (1) EP2598492B1 (enExample)
JP (1) JP5894157B2 (enExample)
KR (1) KR101852644B1 (enExample)
CN (1) CN103003250B (enExample)
AR (1) AR082414A1 (enExample)
AU (1) AU2011285247B2 (enExample)
BR (1) BR112013002090A2 (enExample)
CA (1) CA2806610C (enExample)
CL (1) CL2013000263A1 (enExample)
EA (1) EA023132B1 (enExample)
ES (1) ES2557383T3 (enExample)
IL (1) IL224072A (enExample)
MX (1) MX2013001054A (enExample)
NZ (1) NZ604379A (enExample)
SG (1) SG187166A1 (enExample)
UA (1) UA110113C2 (enExample)
WO (1) WO2012013282A1 (enExample)

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CN105130948A (zh) 2010-04-22 2015-12-09 弗特克斯药品有限公司 制备环烷基甲酰胺基-吲哚化合物的方法
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WO2012069146A1 (en) * 2010-11-24 2012-05-31 Merck Patent Gmbh Quinazoline carboxamide azetidines
SI2755965T1 (sl) 2011-09-12 2017-12-29 Merck Patent Gmbh Novi imidazolni amidi kot modulatorji kinazne aktivnosti
SG2014009260A (en) 2011-09-12 2014-09-26 Merck Patent Gmbh Aminopyrimidine derivatives for use as modulators of kinase activity
ES2807539T3 (es) 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
JP6386467B2 (ja) 2012-11-16 2018-09-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ キナーゼ活性のモジュレーターとしての新規複素環式誘導体
WO2014085528A1 (en) * 2012-11-29 2014-06-05 Merck Patent Gmbh Azaquinazoline carboxamide derivatives
SG11201505999VA (en) 2013-03-11 2015-08-28 Merck Patent Gmbh 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity
CN103232401B (zh) * 2013-04-12 2015-11-04 浙江工业大学 一种4-芳硫基喹唑啉类化合物的合成方法
CN103254141B (zh) * 2013-04-26 2016-02-24 浙江工业大学 4-[4-(2-二丙氨基乙酰氨基)苯胺基]-6-取代喹唑啉类化合物及制备和应用
AU2015240094B2 (en) 2014-04-03 2020-07-30 Merck Patent Gmbh Combinations of cancer therapeutics
JP6543268B2 (ja) 2014-04-15 2019-07-10 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 嚢胞性線維症膜コンダクタンス調節因子が媒介する疾患を処置するための医薬組成物
WO2021216548A1 (en) * 2020-04-21 2021-10-28 University Of Massachusetts Methods and compositions for treatment of age-related macular degeneration
JP2023551408A (ja) 2020-11-16 2023-12-08 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング がん処置のためのキナーゼインヒビター組み合わせ
WO2023039068A1 (en) * 2021-09-08 2023-03-16 Neubase Therapeutics, Inc. Compositions and methods for synthesis of peptide nucleic acid intermediates
WO2026075985A1 (en) * 2024-10-01 2026-04-09 Neolaia Inc. Quinoline- and quinazoline-carboxamide derivatives as cd38 inhibitors

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Also Published As

Publication number Publication date
IL224072A0 (en) 2013-03-05
AR082414A1 (es) 2012-12-05
CL2013000263A1 (es) 2013-09-06
US8710044B2 (en) 2014-04-29
AU2011285247A1 (en) 2013-03-14
CN103003250B (zh) 2016-02-17
JP2013532668A (ja) 2013-08-19
EP2598492B1 (en) 2015-10-28
EA023132B1 (ru) 2016-04-29
WO2012013282A8 (en) 2012-03-29
WO2012013282A1 (en) 2012-02-02
CA2806610A1 (en) 2012-02-02
KR101852644B1 (ko) 2018-04-26
ES2557383T3 (es) 2016-01-25
CA2806610C (en) 2018-08-28
EP2598492A1 (en) 2013-06-05
KR20130096714A (ko) 2013-08-30
EA201300186A1 (ru) 2013-12-30
NZ604379A (en) 2015-01-30
US20130137677A1 (en) 2013-05-30
BR112013002090A2 (pt) 2016-05-24
JP5894157B2 (ja) 2016-03-23
MX2013001054A (es) 2013-02-21
CN103003250A (zh) 2013-03-27
SG187166A1 (en) 2013-02-28
UA110113C2 (xx) 2015-11-25
IL224072A (en) 2016-02-29
HK1183302A1 (zh) 2013-12-20

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