CN103003269B - 取代的杂环基苄基吡唑及其用途 - Google Patents

取代的杂环基苄基吡唑及其用途 Download PDF

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Publication number
CN103003269B
CN103003269B CN201180033637.5A CN201180033637A CN103003269B CN 103003269 B CN103003269 B CN 103003269B CN 201180033637 A CN201180033637 A CN 201180033637A CN 103003269 B CN103003269 B CN 103003269B
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formula
compounds
mmol
compound
methyl
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CN103003269A (zh
Inventor
M.赫特
H.贝克
S.格雷沙特-沙德
P.埃林豪斯
K.昂特舍姆
J.舒马歇尔
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Bayer Intellectual Property GmbH
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201180033637.5A 2010-05-08 2011-05-03 取代的杂环基苄基吡唑及其用途 Expired - Fee Related CN103003269B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10004855 2010-05-08
EP10004855.2 2010-05-08
PCT/EP2011/057021 WO2011141326A1 (de) 2010-05-08 2011-05-03 Substituierte heterocyclylbenzyl-pyrazole und ihre verwendung

Publications (2)

Publication Number Publication Date
CN103003269A CN103003269A (zh) 2013-03-27
CN103003269B true CN103003269B (zh) 2015-11-25

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Country Status (26)

Country Link
US (2) US20130172311A1 (enExample)
EP (1) EP2569312B1 (enExample)
JP (1) JP5727002B2 (enExample)
KR (1) KR20130108997A (enExample)
CN (1) CN103003269B (enExample)
AR (1) AR081368A1 (enExample)
AU (1) AU2011252223A1 (enExample)
BR (1) BR112012028651A2 (enExample)
CA (1) CA2798375A1 (enExample)
CO (1) CO6640218A2 (enExample)
CR (1) CR20120570A (enExample)
CU (1) CU20120157A7 (enExample)
DO (1) DOP2012000284A (enExample)
EA (1) EA201291167A1 (enExample)
EC (1) ECSP12012288A (enExample)
ES (1) ES2462522T3 (enExample)
IL (1) IL222851A0 (enExample)
MA (1) MA34939B1 (enExample)
MX (1) MX2012012960A (enExample)
PE (1) PE20130228A1 (enExample)
PH (1) PH12012502202A1 (enExample)
SG (1) SG185459A1 (enExample)
TN (1) TN2012000531A1 (enExample)
TW (1) TW201200510A (enExample)
UY (1) UY33369A (enExample)
WO (1) WO2011141326A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101688247A (zh) * 2007-05-01 2010-03-31 希尔氏宠物营养品公司 猫科动物骨关节炎的诊断方法和组合物
WO2008141731A2 (en) * 2007-05-18 2008-11-27 Bayer Healthcare Ag Inhibitors of hypoxia inducible factor (hif) useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
EA201291167A1 (ru) * 2010-05-08 2013-05-30 Байер Интеллектуэль Проперти Гмбх Замещенные гетероциклилбензилпиразолы и их применение
UA114915C2 (uk) 2012-07-02 2017-08-28 Монсанто Текнолоджи Ллс Спосіб одержання 3,5-дизаміщених 1,2,4-оксадіазолів (варіанти)
WO2014031928A2 (en) * 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
EP2888253A4 (en) 2012-08-24 2016-01-06 Univ Texas HETEROCYCLIC HIF ACTIVITY MODULATORS FOR THE TREATMENT OF DISEASES
DK2888255T3 (en) 2012-08-24 2018-10-29 Univ Texas HETOCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE
WO2015130790A2 (en) 2014-02-25 2015-09-03 Board Of Regents, University Of Texas System Salts of heterocyclic modulators of hif activity for treatment of disease
US10191597B2 (en) 2015-06-30 2019-01-29 Synaptics Incorporated Modulating a reference voltage to preform capacitive sensing
WO2018131657A1 (ja) * 2017-01-13 2018-07-19 日産化学工業株式会社 芳香族ジアミン化合物前駆体の製造方法
WO2021216530A1 (en) 2020-04-20 2021-10-28 Akebia Therapeutics, Inc. Treatment of viral infections, of organ injury, and of related conditions using a hif prolyl hydroxylase inhibitor or a hif-alpha stabilizer
CN115944626B (zh) * 2022-12-08 2024-04-19 桂林医学院附属医院 小分子化合物在制备抗缺氧或缺血再灌注损伤药物中的应用
AU2024371427A1 (en) * 2023-10-30 2026-06-04 Pretzel Therapeutics, Inc. Compositions and inhibitors of polrmt

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030022924A1 (en) * 2001-06-29 2003-01-30 Sivaram Pillarisetti Compositions and agents for modulating cellular proliferation and angiogenesis
CN1842332A (zh) * 2003-06-30 2006-10-04 Hif生物公司 化合物、组合物及方法
WO2006114313A1 (en) * 2005-04-26 2006-11-02 Glaxo Group Limited Pyrazole compounds as prostaglandin receptors ligands
WO2008141731A2 (en) * 2007-05-18 2008-11-27 Bayer Healthcare Ag Inhibitors of hypoxia inducible factor (hif) useful for treating hyper-proliferative disorders and diseases associated with angiogenesis

Family Cites Families (9)

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EP1613614A2 (en) 2003-04-03 2006-01-11 Merck & Co., Inc. Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5
JP4499721B2 (ja) 2003-06-30 2010-07-07 ヒフ バイオ，インク． 化合物、組成物および方法
WO2007065010A2 (en) 2005-12-02 2007-06-07 Hif Bio, Inc. Anti-angiogenesis compounds
CA2743424A1 (en) * 2008-11-14 2010-05-20 Michael Haerter Heteroaromatic compounds for use as hif inhibitors
DE102008057344A1 (de) * 2008-11-14 2010-05-20 Bayer Schering Pharma Aktiengesellschaft Aminoalkyl-substituierte Aryl-Verbindungen und ihre Verwendung
AU2009316019A1 (en) * 2008-11-14 2010-05-20 Bayer Intellectual Property Gmbh Heterocyclically substituted aryl compounds as HIF inhibitors
EP2202232A1 (en) 2008-12-26 2010-06-30 Laboratorios Almirall, S.A. 1,2,4-oxadiazole derivatives and their therapeutic use
ES2405054T3 (es) 2009-01-23 2013-05-30 Bristol-Myers Squibb Company Derivados de pirazol-1,2,4-oxadiazol como agonistas de esfingosina-1-fosfato
EA201291167A1 (ru) * 2010-05-08 2013-05-30 Байер Интеллектуэль Проперти Гмбх Замещенные гетероциклилбензилпиразолы и их применение

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030022924A1 (en) * 2001-06-29 2003-01-30 Sivaram Pillarisetti Compositions and agents for modulating cellular proliferation and angiogenesis
CN1842332A (zh) * 2003-06-30 2006-10-04 Hif生物公司 化合物、组合物及方法
WO2006114313A1 (en) * 2005-04-26 2006-11-02 Glaxo Group Limited Pyrazole compounds as prostaglandin receptors ligands
WO2008141731A2 (en) * 2007-05-18 2008-11-27 Bayer Healthcare Ag Inhibitors of hypoxia inducible factor (hif) useful for treating hyper-proliferative disorders and diseases associated with angiogenesis

Also Published As

Publication number Publication date
WO2011141326A1 (de) 2011-11-17
KR20130108997A (ko) 2013-10-07
TW201200510A (en) 2012-01-01
EP2569312B1 (de) 2014-03-26
UY33369A (es) 2011-12-01
US20120028950A1 (en) 2012-02-02
CR20120570A (es) 2013-04-22
EP2569312A1 (de) 2013-03-20
CN103003269A (zh) 2013-03-27
US8470811B2 (en) 2013-06-25
PE20130228A1 (es) 2013-03-15
US20130172311A1 (en) 2013-07-04
AU2011252223A1 (en) 2012-12-06
IL222851A0 (en) 2012-12-31
ECSP12012288A (es) 2012-12-28
CA2798375A1 (en) 2011-11-17
TN2012000531A1 (en) 2014-04-01
CU20120157A7 (es) 2013-03-27
JP5727002B2 (ja) 2015-06-03
EA201291167A1 (ru) 2013-05-30
JP2013526497A (ja) 2013-06-24
MA34939B1 (fr) 2014-03-01
MX2012012960A (es) 2012-12-17
DOP2012000284A (es) 2013-03-31
AR081368A1 (es) 2012-08-29
ES2462522T3 (es) 2014-05-23
BR112012028651A2 (pt) 2016-08-09
PH12012502202A1 (en) 2013-02-04
CO6640218A2 (es) 2013-03-22
SG185459A1 (en) 2012-12-28

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