CN102015682B - 作为肾素抑制剂的3,4-取代的哌啶衍生物 - Google Patents

作为肾素抑制剂的3,4-取代的哌啶衍生物 Download PDF

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Publication number
CN102015682B
CN102015682B CN200980116219.5A CN200980116219A CN102015682B CN 102015682 B CN102015682 B CN 102015682B CN 200980116219 A CN200980116219 A CN 200980116219A CN 102015682 B CN102015682 B CN 102015682B
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methyl
equiv
amine
vacuo
etoac
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Expired - Fee Related
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CN200980116219.5A
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Chinese (zh)
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CN102015682A (zh
Inventor
A·C-Y·陈
D·迪布
P-A·富尼耶
E·L·格林
P·拉孔布
S·拉利贝特
D·麦唐纳
D·B·麦凯
D·J·麦凯
T·Y-H·吴
L-C·坎珀
J·P·斯科特
N·布勒迈尔
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Actelion Pharmaceuticals Ltd
Organon Pharma UK Ltd
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Actelion Pharmaceuticals Ltd
Merck Sharp and Dohme Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/42Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
    • 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
    • A61P9/10Drugs 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
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
CN200980116219.5A 2008-05-05 2009-05-04 作为肾素抑制剂的3,4-取代的哌啶衍生物 Expired - Fee Related CN102015682B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US12652908P 2008-05-05 2008-05-05
US61/126529 2008-05-05
US18830308P 2008-08-07 2008-08-07
US61/188303 2008-08-07
PCT/CA2009/000611 WO2009135299A1 (en) 2008-05-05 2009-05-04 3, 4 - substituted piperidine derivatives as renin inhibitors

Publications (2)

Publication Number Publication Date
CN102015682A CN102015682A (zh) 2011-04-13
CN102015682B true CN102015682B (zh) 2014-07-16

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CN200980116219.5A Expired - Fee Related CN102015682B (zh) 2008-05-05 2009-05-04 作为肾素抑制剂的3,4-取代的哌啶衍生物

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Country Link
US (1) US8889714B2 (enExample)
EP (1) EP2274295B1 (enExample)
JP (3) JP4790871B2 (enExample)
KR (2) KR20130029116A (enExample)
CN (1) CN102015682B (enExample)
AU (1) AU2009243875B2 (enExample)
BR (1) BRPI0912388A2 (enExample)
CA (1) CA2722734C (enExample)
CO (1) CO6311081A2 (enExample)
CR (1) CR11809A (enExample)
DO (1) DOP2010000329A (enExample)
EA (1) EA020853B1 (enExample)
ES (1) ES2548134T3 (enExample)
IL (1) IL208467A (enExample)
MA (1) MA32296B1 (enExample)
MX (1) MX2010012067A (enExample)
MY (1) MY152042A (enExample)
NI (1) NI201000188A (enExample)
NZ (1) NZ589019A (enExample)
PL (1) PL2274295T3 (enExample)
SG (1) SG192543A1 (enExample)
SV (1) SV2010003723A (enExample)
WO (1) WO2009135299A1 (enExample)

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CN102099036B (zh) 2008-06-03 2015-05-27 英特芒尼公司 用于治疗炎性疾患和纤维化疾患的化合物和方法
JP2012511514A (ja) * 2008-12-10 2012-05-24 メルク・カナダ・インコーポレイテツド レニン阻害剤としての3,4−置換ピペリジン誘導体
TWI562977B (en) * 2010-11-05 2016-12-21 Bayer Ip Gmbh Process for the preparation of substituted n-(benzyl)cyclopropanamines by imine hydrogenation
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AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
JP6525437B2 (ja) 2014-04-02 2019-06-05 インターミューン, インコーポレイテッド 抗線維性ピリジノン
CN107602381B (zh) * 2017-09-11 2021-03-16 陕西莱特光电材料股份有限公司 一种萘甲酸酯类衍生物及其制备方法
CN108033876A (zh) * 2017-12-20 2018-05-15 江汉大学 一种5-溴-2-氯苯甲醛的制备方法
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EP2274295B1 (en) 2015-08-05
JP5587246B2 (ja) 2014-09-10
EP2274295A4 (en) 2012-03-28
CN102015682A (zh) 2011-04-13
PL2274295T3 (pl) 2016-01-29
WO2009135299A1 (en) 2009-11-12
CA2722734A1 (en) 2009-11-12
JP4790871B2 (ja) 2011-10-12
JP2011519871A (ja) 2011-07-14
JP2011225580A (ja) 2011-11-10
IL208467A0 (en) 2010-12-30
EA201071269A1 (ru) 2011-06-30
BRPI0912388A2 (pt) 2017-09-26
KR101403311B1 (ko) 2014-06-05
US8889714B2 (en) 2014-11-18
IL208467A (en) 2014-07-31
EA020853B1 (ru) 2015-02-27
JP5653842B2 (ja) 2015-01-14
MA32296B1 (fr) 2011-05-02
CA2722734C (en) 2013-11-05
JP2011225579A (ja) 2011-11-10
AU2009243875A1 (en) 2009-11-12
EP2274295A1 (en) 2011-01-19
CO6311081A2 (es) 2011-08-22
SG192543A1 (en) 2013-08-30
MX2010012067A (es) 2010-12-06
KR20130029116A (ko) 2013-03-21
ES2548134T3 (es) 2015-10-14
DOP2010000329A (es) 2011-01-15
AU2009243875B2 (en) 2011-12-01
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US20110053940A1 (en) 2011-03-03
CR11809A (es) 2011-01-10
NI201000188A (es) 2012-02-02
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KR20100131007A (ko) 2010-12-14
SV2010003723A (es) 2011-01-24

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