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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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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (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 (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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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
MX342288B (es) 2010-04-22 2016-09-23 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
WO2012016001A1 (en) * 2010-07-29 2012-02-02 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
CA2818706C (en) * 2010-11-24 2019-07-23 Merck Patent Gmbh Quinazoline carboxamide azetidines
ES2644536T3 (es) 2011-09-12 2017-11-29 Merck Patent Gmbh Imidazol-aminas novedosas como moduladores de la actividad cinasa
JP6082011B2 (ja) 2011-09-12 2017-02-15 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使用するためのアミノピリミジン誘導体
ES2807539T3 (es) 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
ES2620119T3 (es) 2012-11-16 2017-06-27 Merck Patent Gmbh Derivados heterocíclicos novedosos como moduladores de la actividad de quinasa
ES2821102T3 (es) * 2012-11-29 2021-04-23 Merck Patent Gmbh Derivados de azaquinazolincarboxamida
AR095202A1 (es) 2013-03-11 2015-09-30 Merck Patent Gmbh Heterociclos como moduladores de la actividad quinasa
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
KR102410696B1 (ko) 2014-04-03 2022-06-17 메르크 파텐트 게엠베하 암 치료법의 조합
KR102447581B1 (ko) 2014-04-15 2022-09-28 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막전도 조절자 매개 질환 치료용 약제학적 조성물
US20230220395A1 (en) * 2020-04-21 2023-07-13 University Of Massachusetts Methods and compositions for treatment of age-related macular degeneration
MX2023005520A (es) 2020-11-16 2023-05-23 Merck Patent Gmbh Combinaciones de inhibidores de cinasa para tratamiento de cancer.
WO2023039068A1 (en) * 2021-09-08 2023-03-16 Neubase Therapeutics, Inc. Compositions and methods for synthesis of peptide nucleic acid intermediates

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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

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

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