SG187166A1 - 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
SG187166A1
SG187166A1 SG2013004965A SG2013004965A SG187166A1 SG 187166 A1 SG187166 A1 SG 187166A1 SG 2013004965 A SG2013004965 A SG 2013004965A SG 2013004965 A SG2013004965 A SG 2013004965A SG 187166 A1 SG187166 A1 SG 187166A1
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SG
Singapore
Prior art keywords
methyl
methylamino
substituted methylene
hal
monosubstituted
Prior art date
Application number
SG2013004965A
Other languages
English (en)
Inventor
Bayard R Huck
Constantin Neagu
Reinaldo C Jones
Lizbeth Celeste Deselm
Yufang Xiao
Srinivasa R Karra
Ruoxi Lan
Igor Mochalkin
Amanda E Sutton
Thomas E Richardson
Original Assignee
Merck Patent Gmbh
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
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of SG187166A1 publication Critical patent/SG187166A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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)
SG2013004965A 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k SG187166A1 (en)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
SG187166A1 true SG187166A1 (en) 2013-02-28

Family

ID=44532723

Family Applications (1)

Application Number Title Priority Date Filing Date
SG2013004965A SG187166A1 (en) 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k

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
ES2608474T3 (es) 2010-04-22 2017-04-11 Vertex Pharmaceuticals Incorporated Proceso de producción de compuestos indol cycloalkylcarboxamido
AU2011282684B2 (en) * 2010-07-29 2015-05-21 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
LT2643313T (lt) * 2010-11-24 2016-10-25 Merck Patent Gmbh Chinazolino karboksamido azetidinai
US9321760B2 (en) 2011-09-12 2016-04-26 Merck Patent Gmbh Aminopyrimidine derivatives for use as modulators of kinase activity
PT2755965T (pt) 2011-09-12 2017-11-02 Merck Patent Gmbh Novas imidazol aminas como moduladores da atividade quinase
EP2920154B1 (en) 2012-11-16 2017-10-11 Merck Patent GmbH Novel imidazol-piperidinyl derivatives as modulators of kinase activity
US9580443B2 (en) 2012-11-16 2017-02-28 Merck Patent Gmbh Heterocyclic derivatives as modulators of kinase activity
NZ706418A (en) * 2012-11-29 2019-09-27 Merck Patent Gmbh Azaquinazoline carboxamide derivatives
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
EP3125935B1 (en) 2014-04-03 2019-10-23 Merck Patent GmbH Combinations of cancer therapeutics
ES2885181T3 (es) 2014-04-15 2021-12-13 Vertex Pharma Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de la conductancia transmembrana de fibrosis quística
CN116322773A (zh) * 2020-04-21 2023-06-23 马萨诸塞大学 用于治疗年龄相关性黄斑变性的方法和组合物
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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GB9613021D0 (en) * 1996-06-21 1996-08-28 Pharmacia Spa Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors
AR016817A1 (es) * 1997-08-14 2001-08-01 Smithkline Beecham Plc Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento
KR100774855B1 (ko) * 2000-04-27 2007-11-08 아스텔라스세이야쿠 가부시키가이샤 축합 헤테로아릴 유도체
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
JPWO2004014861A1 (ja) * 2002-08-09 2005-12-02 杏林製薬株式会社 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
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Also Published As

Publication number Publication date
CA2806610C (en) 2018-08-28
MX2013001054A (es) 2013-02-21
EA201300186A1 (ru) 2013-12-30
IL224072A0 (en) 2013-03-05
HK1183302A1 (zh) 2013-12-20
US20130137677A1 (en) 2013-05-30
US8710044B2 (en) 2014-04-29
CA2806610A1 (en) 2012-02-02
EP2598492A1 (en) 2013-06-05
EP2598492B1 (en) 2015-10-28
NZ604379A (en) 2015-01-30
CL2013000263A1 (es) 2013-09-06
IL224072A (en) 2016-02-29
CN103003250A (zh) 2013-03-27
CN103003250B (zh) 2016-02-17
WO2012013282A8 (en) 2012-03-29
KR20130096714A (ko) 2013-08-30
JP2013532668A (ja) 2013-08-19
UA110113C2 (xx) 2015-11-25
WO2012013282A1 (en) 2012-02-02
EA023132B1 (ru) 2016-04-29
AR082414A1 (es) 2012-12-05
AU2011285247B2 (en) 2016-08-04
KR101852644B1 (ko) 2018-04-26
JP5894157B2 (ja) 2016-03-23
ES2557383T3 (es) 2016-01-25
BR112013002090A2 (pt) 2016-05-24
AU2011285247A1 (en) 2013-03-14

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