TW201200510A - Substituted heterocyclylbenzylpyrazoles and use thereof - Google Patents

Substituted heterocyclylbenzylpyrazoles and use thereof Download PDF

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Publication number
TW201200510A
TW201200510A TW100115869A TW100115869A TW201200510A TW 201200510 A TW201200510 A TW 201200510A TW 100115869 A TW100115869 A TW 100115869A TW 100115869 A TW100115869 A TW 100115869A TW 201200510 A TW201200510 A TW 201200510A
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Taiwan
Prior art keywords
compound
formula
mmol
solvate
group
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TW100115869A
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English (en)
Chinese (zh)
Inventor
Michael Haerter
Hartmut Beck
Susanne Greschat
Peter Ellinghaus
Kerstin Berhoerster
Joachim Schuhmacher
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Bayer Schering Pharma Ag
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Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of TW201200510A publication Critical patent/TW201200510A/zh

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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW100115869A 2010-05-08 2011-05-06 Substituted heterocyclylbenzylpyrazoles and use thereof TW201200510A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10004855 2010-05-08

Publications (1)

Publication Number Publication Date
TW201200510A true TW201200510A (en) 2012-01-01

Family

ID=44063276

Family Applications (1)

Application Number Title Priority Date Filing Date
TW100115869A TW201200510A (en) 2010-05-08 2011-05-06 Substituted heterocyclylbenzylpyrazoles and use thereof

Country Status (26)

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

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2155904A2 (en) * 2007-05-01 2010-02-24 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
CN103003269B (zh) * 2010-05-08 2015-11-25 拜耳知识产权有限责任公司 取代的杂环基苄基吡唑及其用途
DK2867230T3 (da) 2012-07-02 2020-04-14 Monsanto Technology Llc Fremgangsmåde til fremstilling af 3,5-disubstitueret 1,2,4-oxadiazoler
RU2698197C2 (ru) 2012-08-24 2019-08-23 Боард Оф Регентс, Зе Юниверсити Оф Тексас Систем Гетероциклические модуляторы активности hif для лечения заболеваний
US20140073634A1 (en) * 2012-08-24 2014-03-13 Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center Heterocyclic modulators of hif activity for treatment of disease
WO2014031933A2 (en) * 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
DK3110420T3 (da) 2014-02-25 2019-05-13 Board Of Regents Univ Of Texas System Salte af heterocykliske modulatorer af hif-aktivitet til behandling af sygdomme
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
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
WO2025096654A1 (en) * 2023-10-30 2025-05-08 Pretzel Therapeutics, Inc. Compositions and inhibitors of polrmt

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6610726B2 (en) * 2001-06-29 2003-08-26 North Shore-Long Island Jewish Research Institute Compositions and agents for modulating cellular proliferation and angiogenesis
WO2004089303A2 (en) 2003-04-03 2004-10-21 Merck & Co., Inc. Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5
AU2004275694B2 (en) 2003-06-30 2008-03-06 Bizbiotech Co., Ltd. Compounds, compositions and methods
CN1842332A (zh) * 2003-06-30 2006-10-04 Hif生物公司 化合物、组合物及方法
GB0508472D0 (en) * 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
WO2007065010A2 (en) 2005-12-02 2007-06-07 Hif Bio, Inc. Anti-angiogenesis compounds
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
DE102008057344A1 (de) * 2008-11-14 2010-05-20 Bayer Schering Pharma Aktiengesellschaft Aminoalkyl-substituierte Aryl-Verbindungen und ihre Verwendung
WO2010054764A1 (de) * 2008-11-14 2010-05-20 Bayer Schering Pharma Aktiengesellschaft Heteroaromatische verbindungen zur verwendung als hif-inhibitoren
HRP20150341T1 (hr) * 2008-11-14 2015-05-08 Bayer Intellectual Property Gmbh Heterocikliäśki supstituirani spojevi arila kao inhibitori hif
EP2202232A1 (en) 2008-12-26 2010-06-30 Laboratorios Almirall, S.A. 1,2,4-oxadiazole derivatives and their therapeutic use
US8389509B2 (en) 2009-01-23 2013-03-05 Bristol-Myers Squibb Company Substituted pyrazole compounds
CN103003269B (zh) * 2010-05-08 2015-11-25 拜耳知识产权有限责任公司 取代的杂环基苄基吡唑及其用途

Also Published As

Publication number Publication date
CO6640218A2 (es) 2013-03-22
MX2012012960A (es) 2012-12-17
US8470811B2 (en) 2013-06-25
PH12012502202A1 (en) 2013-02-04
EP2569312A1 (de) 2013-03-20
EA201291167A1 (ru) 2013-05-30
BR112012028651A2 (pt) 2016-08-09
DOP2012000284A (es) 2013-03-31
SG185459A1 (en) 2012-12-28
KR20130108997A (ko) 2013-10-07
IL222851A0 (en) 2012-12-31
JP2013526497A (ja) 2013-06-24
CU20120157A7 (es) 2013-03-27
EP2569312B1 (de) 2014-03-26
PE20130228A1 (es) 2013-03-15
US20120028950A1 (en) 2012-02-02
US20130172311A1 (en) 2013-07-04
CN103003269B (zh) 2015-11-25
TN2012000531A1 (en) 2014-04-01
UY33369A (es) 2011-12-01
JP5727002B2 (ja) 2015-06-03
ECSP12012288A (es) 2012-12-28
AR081368A1 (es) 2012-08-29
WO2011141326A1 (de) 2011-11-17
CN103003269A (zh) 2013-03-27
MA34939B1 (fr) 2014-03-01
AU2011252223A1 (en) 2012-12-06
ES2462522T3 (es) 2014-05-23
CR20120570A (es) 2013-04-22
CA2798375A1 (en) 2011-11-17

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