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

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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 (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008137549A2 (en) * 2007-05-01 2008-11-13 Hill's Pet Nutrition, Inc. Methods and compositions for diagnosing osteoarthritis in a feline
KR20100016617A (ko) * 2007-05-18 2010-02-12 바이엘 쉐링 파마 악티엔게젤샤프트 과증식성 장애 및 혈관형성 관련 질환의 치료에 유용한 저산소증 유도성 인자 （ｈｉｆ）의 억제제
BR112012028651A2 (pt) * 2010-05-08 2016-08-09 Bayer Ip Gmbh heterociclilbenzilpirazóis substituídos e uso do mesmo
UA114915C2 (uk) 2012-07-02 2017-08-28 Монсанто Текнолоджи Ллс Спосіб одержання 3,5-дизаміщених 1,2,4-оксадіазолів (варіанти)
WO2014031936A2 (en) 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
WO2014031928A2 (en) * 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
US9115120B2 (en) 2012-08-24 2015-08-25 Board Of Regents, The University Of Texas Systems Heterocyclic modulators of HIF activity for treatment of disease
US9663504B2 (en) 2014-02-25 2017-05-30 Board Of Regents, The 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
JP7103232B2 (ja) * 2017-01-13 2022-07-20 日産化学株式会社 芳香族ジアミン化合物前駆体の製造方法
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
WO2025096662A1 (en) * 2023-10-30 2025-05-08 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)

* Cited by examiner, † Cited by third party
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US20060194807A1 (en) 2003-04-03 2006-08-31 Cosford Nicholas D P Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5
US7226941B2 (en) 2003-06-30 2007-06-05 Hif Bio, Inc. Compound for treating angiogenesis
WO2007065010A2 (en) 2005-12-02 2007-06-07 Hif Bio, Inc. Anti-angiogenesis compounds
CN102282142A (zh) * 2008-11-14 2011-12-14 拜耳先灵制药股份公司 取代的芳族化合物和它们的用途
EA022271B1 (ru) * 2008-11-14 2015-12-30 Байер Интеллектуэль Проперти Гмбх Гетероциклические замещенные соединения арила в качестве ингибиторов hif
DE102008057344A1 (de) * 2008-11-14 2010-05-20 Bayer Schering Pharma Aktiengesellschaft Aminoalkyl-substituierte Aryl-Verbindungen und ihre Verwendung
EP2202232A1 (en) 2008-12-26 2010-06-30 Laboratorios Almirall, S.A. 1,2,4-oxadiazole derivatives and their therapeutic use
JP2012515789A (ja) 2009-01-23 2012-07-12 ブリストル−マイヤーズ スクイブ カンパニー スフィンゴシン−１−リン酸アゴニストとしてのピラゾール−１，２，４−オキサジアゾール誘導体
BR112012028651A2 (pt) * 2010-05-08 2016-08-09 Bayer Ip Gmbh heterociclilbenzilpirazóis substituídos e uso do mesmo

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

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