HK1183302A1 - 作為激酶 抑制劑的二環氮雜環甲酰胺 - Google Patents

作為激酶 抑制劑的二環氮雜環甲酰胺

Info

Publication number
HK1183302A1
HK1183302A1 HK13110693.4A HK13110693A HK1183302A1 HK 1183302 A1 HK1183302 A1 HK 1183302A1 HK 13110693 A HK13110693 A HK 13110693A HK 1183302 A1 HK1183302 A1 HK 1183302A1
Authority
HK
Hong Kong
Prior art keywords
p70s6k
inhibitors
kinase
bicyclic
carboxamides
Prior art date
Application number
HK13110693.4A
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 HK1183302A1 publication Critical patent/HK1183302A1/zh

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
HK13110693.4A 2010-07-29 2013-09-17 作為激酶 抑制劑的二環氮雜環甲酰胺 HK1183302A1 (zh)

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
HK1183302A1 true HK1183302A1 (zh) 2013-12-20

Family

ID=44532723

Family Applications (1)

Application Number Title Priority Date Filing Date
HK13110693.4A HK1183302A1 (zh) 2010-07-29 2013-09-17 作為激酶 抑制劑的二環氮雜環甲酰胺

Country Status (19)

Country Link
US (1) US8710044B2 (zh)
EP (1) EP2598492B1 (zh)
JP (1) JP5894157B2 (zh)
KR (1) KR101852644B1 (zh)
CN (1) CN103003250B (zh)
AR (1) AR082414A1 (zh)
AU (1) AU2011285247B2 (zh)
BR (1) BR112013002090A2 (zh)
CA (1) CA2806610C (zh)
CL (1) CL2013000263A1 (zh)
EA (1) EA023132B1 (zh)
ES (1) ES2557383T3 (zh)
HK (1) HK1183302A1 (zh)
IL (1) IL224072A (zh)
MX (1) MX2013001054A (zh)
NZ (1) NZ604379A (zh)
SG (1) SG187166A1 (zh)
UA (1) UA110113C2 (zh)
WO (1) WO2012013282A1 (zh)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2013525371A (ja) 2010-04-22 2013-06-20 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 シクロアルキルカルボキサミド−インドール化合物の製造方法
EA028012B1 (ru) * 2010-07-29 2017-09-29 Мерк Патент Гмбх Циклический амин-азагетероциклический карбоксамид
MY186456A (en) * 2010-11-24 2021-07-22 Merck Patent Gmbh Quinazoline carboxamide azetidines
SG10201606301YA (en) 2011-09-12 2016-09-29 Merck Patent Gmbh Novel imidazole amines as modulators of kinase activity
DK2755958T3 (en) 2011-09-12 2017-09-25 Merck Patent Gmbh AMINOPYRIMIDINE DERIVATIVES USED AS MODULATORS OF KINASE ACTIVITY
WO2014078634A1 (en) 2012-11-16 2014-05-22 Merck Patent Gmbh Novel imidazol-piperidinyl derivatives as modulators of kinase activity
CA2890288A1 (en) 2012-11-16 2014-05-22 Merck Patent Gmbh Novel heterocyclic derivatives as modulators of kinase activity
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
RU2733401C2 (ru) 2014-04-03 2020-10-01 Мерк Патент Гмбх Комбинации противораковых лекарств
DK3424534T3 (da) 2014-04-15 2021-07-26 Vertex Pharma Farmaceutiske sammensætninger til behandling af sygdomme medieret af cystisk fibrosetransmembranledningsregulator
EP4138779A4 (en) * 2020-04-21 2024-05-22 University of Massachusetts METHODS AND COMPOSITIONS FOR THE 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

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN1186324C (zh) * 2000-04-27 2005-01-26 山之内制药株式会社 稠合杂芳基衍生物
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
JPWO2004014873A1 (ja) * 2002-08-09 2005-12-02 杏林製薬株式会社 ４−置換キナゾリン−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
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
EP1615906A1 (en) 2003-04-03 2006-01-18 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
WO2005033086A1 (en) 2003-09-30 2005-04-14 Irm Llc Compounds and compositions as protein kinase inhibitors
CA2541989C (en) 2003-10-24 2013-10-01 Exelixis, Inc. P70s6 kinase modulators and method of use
WO2005054237A1 (en) 2003-11-21 2005-06-16 Novartis Ag 1h-imidazoquinoline derivatives as protein kinase inhibitors
KR20060123463A (ko) 2003-12-09 2006-12-01 더 거번먼트 오브 더 유나이티드 스테이츠 오브 어메리카 애즈 레프리젠티드 바이 더 세크러터리 오브 더 디파트먼트 오브 헬쓰 앤드 휴먼 써비시즈 면역 반응을 억제하거나 증식성 장애를 치료하는 방법들
EP1750727A2 (en) 2004-04-23 2007-02-14 Exelixis, Inc. Kinase modulators and methods of use
JP2008501696A (ja) * 2004-06-04 2008-01-24 アンフォラ ディスカバリー コーポレーション Ａｔｐ利用酵素阻害活性を示すキノリンおよびイソキノリン系化合物、ならびにその組成物および使用
AU2005322085B2 (en) 2004-12-28 2012-07-19 Exelixis, Inc. [1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
WO2006136821A1 (en) 2005-06-22 2006-12-28 Astex Therapeutics Limited Pharmaceutical compounds
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
JP5642714B2 (ja) * 2009-02-11 2014-12-17 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 新規なアミノアザヘテロ環式カルボキサミド

Also Published As

Publication number Publication date
BR112013002090A2 (pt) 2016-05-24
CA2806610C (en) 2018-08-28
WO2012013282A1 (en) 2012-02-02
US20130137677A1 (en) 2013-05-30
AR082414A1 (es) 2012-12-05
CL2013000263A1 (es) 2013-09-06
JP5894157B2 (ja) 2016-03-23
US8710044B2 (en) 2014-04-29
CN103003250A (zh) 2013-03-27
JP2013532668A (ja) 2013-08-19
EP2598492A1 (en) 2013-06-05
MX2013001054A (es) 2013-02-21
WO2012013282A8 (en) 2012-03-29
CA2806610A1 (en) 2012-02-02
EA023132B1 (ru) 2016-04-29
KR101852644B1 (ko) 2018-04-26
IL224072A0 (en) 2013-03-05
ES2557383T3 (es) 2016-01-25
EA201300186A1 (ru) 2013-12-30
UA110113C2 (xx) 2015-11-25
SG187166A1 (en) 2013-02-28
EP2598492B1 (en) 2015-10-28
KR20130096714A (ko) 2013-08-30
AU2011285247B2 (en) 2016-08-04
AU2011285247A1 (en) 2013-03-14
IL224072A (en) 2016-02-29
CN103003250B (zh) 2016-02-17
NZ604379A (en) 2015-01-30

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Legal Events

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PC Patent ceased (i.e. patent has lapsed due to the failure to pay the renewal fee)

Effective date: 20200706