CN103003250B - 作为激酶p70s6k抑制剂的二环氮杂环甲酰胺 - Google Patents

作为激酶p70s6k抑制剂的二环氮杂环甲酰胺 Download PDF

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Publication number
CN103003250B
CN103003250B CN201180037284.6A CN201180037284A CN103003250B CN 103003250 B CN103003250 B CN 103003250B CN 201180037284 A CN201180037284 A CN 201180037284A CN 103003250 B CN103003250 B CN 103003250B
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China
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methyl
ethyl
compound
group
carboxamide
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Expired - Fee Related
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CN201180037284.6A
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Chinese (zh)
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CN103003250A (zh
Inventor
B.R.胡克
C.尼古
R.C.琼斯
L.C.德塞尔姆
肖玉方
S.R.卡拉
兰若曦
I.莫查尔金
A.E.苏顿
T.E.理查森
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Merck Patent GmbH
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Merck Patent GmbH
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    • 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
    • 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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201180037284.6A 2010-07-29 2011-07-01 作为激酶p70s6k抑制剂的二环氮杂环甲酰胺 Expired - Fee Related CN103003250B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36896410P 2010-07-29 2010-07-29
US61/368964 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)

Publication Number Publication Date
CN103003250A CN103003250A (zh) 2013-03-27
CN103003250B true CN103003250B (zh) 2016-02-17

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CN201180037284.6A Expired - Fee Related CN103003250B (zh) 2010-07-29 2011-07-01 作为激酶p70s6k抑制剂的二环氮杂环甲酰胺

Country Status (18)

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

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US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
MX353408B (es) 2010-04-22 2018-01-11 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
US9586938B2 (en) 2010-07-29 2017-03-07 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
PT2643313T (pt) * 2010-11-24 2016-10-11 Merck Patent Gmbh Quinazolina carboxamida azetidinas
CN103930407B (zh) 2011-09-12 2019-02-26 默克专利有限公司 用作激酶活性调节剂的氨基嘧啶衍生物
MX346095B (es) 2011-09-12 2017-03-07 Merck Patent Gmbh Nuevas imidazol-aminas como moduladores de la actividad de cinasas.
CA2890288A1 (en) 2012-11-16 2014-05-22 Merck Patent Gmbh Novel heterocyclic derivatives as modulators of kinase activity
AR093511A1 (es) 2012-11-16 2015-06-10 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de cinasas
SG10201800741QA (en) * 2012-11-29 2018-03-28 Merck Patent Gmbh BENZO-[d][1,2,3]TRIAZINE COMPOUNDS AND USE AS p70S6K INHIBITORS
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
CA2944573C (en) 2014-04-03 2022-10-25 Merck Patent Gmbh Combinations of cancer therapeutics
RU2744460C2 (ru) 2014-04-15 2021-03-09 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости
WO2021216548A1 (en) * 2020-04-21 2021-10-28 University Of Massachusetts Methods and compositions for treatment of age-related macular degeneration
WO2022101459A1 (en) 2020-11-16 2022-05-19 Merck Patent Gmbh Kinase inhibitor combinations for cancer treatment
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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WO1999009024A1 (en) * 1997-08-14 1999-02-25 Smithkline Beecham Plc Phenyl urea and phenyl thiourea derivatives as hfgan72 antagonists
CN1426398A (zh) * 2000-04-27 2003-06-25 山之内制药株式会社 稠合杂芳基衍生物
WO2004014861A1 (ja) * 2002-08-09 2004-02-19 Kyorin Pharmaceutical Co., Ltd. 4-置換キノリン-8-カルボン酸アミド誘導体とその薬理上許容される付加塩
WO2005120509A1 (en) * 2004-06-04 2005-12-22 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof

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WO1999009024A1 (en) * 1997-08-14 1999-02-25 Smithkline Beecham Plc Phenyl urea and phenyl thiourea derivatives as hfgan72 antagonists
CN1426398A (zh) * 2000-04-27 2003-06-25 山之内制药株式会社 稠合杂芳基衍生物
WO2004014861A1 (ja) * 2002-08-09 2004-02-19 Kyorin Pharmaceutical Co., Ltd. 4-置換キノリン-8-カルボン酸アミド誘導体とその薬理上許容される付加塩
WO2005120509A1 (en) * 2004-06-04 2005-12-22 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof

Also Published As

Publication number Publication date
BR112013002090A2 (pt) 2016-05-24
US8710044B2 (en) 2014-04-29
JP5894157B2 (ja) 2016-03-23
UA110113C2 (xx) 2015-11-25
WO2012013282A1 (en) 2012-02-02
US20130137677A1 (en) 2013-05-30
AU2011285247B2 (en) 2016-08-04
SG187166A1 (en) 2013-02-28
IL224072A0 (en) 2013-03-05
JP2013532668A (ja) 2013-08-19
ES2557383T3 (es) 2016-01-25
HK1183302A1 (zh) 2013-12-20
IL224072A (en) 2016-02-29
CN103003250A (zh) 2013-03-27
CA2806610C (en) 2018-08-28
KR101852644B1 (ko) 2018-04-26
AU2011285247A1 (en) 2013-03-14
MX2013001054A (es) 2013-02-21
WO2012013282A8 (en) 2012-03-29
NZ604379A (en) 2015-01-30
EA201300186A1 (ru) 2013-12-30
CA2806610A1 (en) 2012-02-02
KR20130096714A (ko) 2013-08-30
EP2598492B1 (en) 2015-10-28
EA023132B1 (ru) 2016-04-29
AR082414A1 (es) 2012-12-05
CL2013000263A1 (es) 2013-09-06
EP2598492A1 (en) 2013-06-05

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