CN102015682A - 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 PDFInfo
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- CN102015682A CN102015682A CN2009801162195A CN200980116219A CN102015682A CN 102015682 A CN102015682 A CN 102015682A CN 2009801162195 A CN2009801162195 A CN 2009801162195A CN 200980116219 A CN200980116219 A CN 200980116219A CN 102015682 A CN102015682 A CN 102015682A
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- C07D401/04—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
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- C07D417/00—Heterocyclic 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
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- Organic Chemistry (AREA)
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- Veterinary Medicine (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Description
峰值(ppm) | 相对强度 |
120.1 | 100 |
31.2 | 76 |
17.1 | 73 |
43.5 | 71 |
41.6 | 71 |
29.4 | 68 |
58.5 | 67 |
71.4 | 66 |
28.7 | 64 |
42.5 | 64 |
138.3 | 60 |
143.6 | 58 |
途径 | ABC36h(mmHg*h) | MAP降低最大值(mmHg) | 期限(天) |
PO | 1143 | 57 | 2 |
TD | 514 | 30 | 1 |
途径 | AUC24h(μM*hr) | 在4h的PRA抑制(%) |
PO | 1.8 | n.a. |
TD | 2.9 | 98 |
Claims (41)
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US61/188303 | 2008-08-07 | ||
PCT/CA2009/000611 WO2009135299A1 (en) | 2008-05-05 | 2009-05-04 | 3, 4 - substituted piperidine derivatives as renin inhibitors |
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CN102015682A true CN102015682A (zh) | 2011-04-13 |
CN102015682B CN102015682B (zh) | 2014-07-16 |
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EP (1) | EP2274295B1 (zh) |
JP (3) | JP4790871B2 (zh) |
KR (2) | KR101403311B1 (zh) |
CN (1) | CN102015682B (zh) |
AU (1) | AU2009243875B2 (zh) |
BR (1) | BRPI0912388A2 (zh) |
CA (1) | CA2722734C (zh) |
CO (1) | CO6311081A2 (zh) |
CR (1) | CR11809A (zh) |
DO (1) | DOP2010000329A (zh) |
EA (1) | EA020853B1 (zh) |
ES (1) | ES2548134T3 (zh) |
IL (1) | IL208467A (zh) |
MA (1) | MA32296B1 (zh) |
MX (1) | MX2010012067A (zh) |
MY (1) | MY152042A (zh) |
NI (1) | NI201000188A (zh) |
NZ (1) | NZ589019A (zh) |
PL (1) | PL2274295T3 (zh) |
SG (1) | SG192543A1 (zh) |
SV (1) | SV2010003723A (zh) |
WO (1) | WO2009135299A1 (zh) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107602381A (zh) * | 2017-09-11 | 2018-01-19 | 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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CA3034994A1 (en) | 2008-06-03 | 2009-12-10 | Intermune, Inc. | Substituted aryl-2 pyridone compounds and use thereof for treating inflammatory and fibrotic disorders |
EP2376473A4 (en) * | 2008-12-10 | 2012-05-02 | Merck Canada Inc | 3,4-SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS |
TWI622573B (zh) * | 2010-11-05 | 2018-05-01 | 拜耳知識產權公司 | 藉由亞胺氫化製備經取代n-(苄基)環丙胺之方法 |
UA112897C2 (uk) * | 2012-05-09 | 2016-11-10 | Байєр Фарма Акцієнгезелльшафт | Біциклічно заміщені урацили та їх застосування для лікування і/або профілактики захворювань |
AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
KR102373700B1 (ko) | 2014-04-02 | 2022-03-11 | 인터뮨, 인크. | 항섬유성 피리디논 |
US20220002284A1 (en) | 2018-11-28 | 2022-01-06 | Basf Se | Pesticidal compounds |
WO2021219513A1 (en) | 2020-04-28 | 2021-11-04 | Basf Se | Pesticidal compounds |
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US5380758A (en) * | 1991-03-29 | 1995-01-10 | Brigham And Women's Hospital | S-nitrosothiols as smooth muscle relaxants and therapeutic uses thereof |
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US5994294A (en) * | 1996-02-02 | 1999-11-30 | Nitromed, Inc. | Nitrosated and nitrosylated α-adrenergic receptor antagonist compounds, compositions and their uses |
JP2001504457A (ja) | 1996-11-01 | 2001-04-03 | ニトロメド インコーポレーテッド | ニトロソ化およびニトロシル化ホスホジエステラーゼ阻害剤化合物、組成物及びその使用法 |
IT1295694B1 (it) * | 1996-11-14 | 1999-05-27 | Nicox Sa | Nitrossi derivati per la preparazione di medicamenti ad attivita antitrombinica |
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WO2007034445A2 (en) | 2005-09-26 | 2007-03-29 | Actelion Pharmaceuticals Ltd | Novel piperazine derivatives as renin inhibitors for cardiovascular events and renal insufficiency |
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BRPI0708567A2 (pt) | 2006-03-08 | 2011-05-31 | Actelion Pharmaceuticals Ltd | composto, composição farmacêutica que compreende e seu uso |
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JP2010535716A (ja) | 2007-08-07 | 2010-11-25 | メルク フロスト カナダ リミテツド | レニン阻害剤 |
AU2008331456A1 (en) * | 2007-12-04 | 2009-06-11 | Merck Frosst Canada Ltd | Renin inhibitors |
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EP2467385A4 (en) | 2009-08-18 | 2013-01-16 | Merck Canada Inc | INHIBITORS OF REINE |
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
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CN107602381A (zh) * | 2017-09-11 | 2018-01-19 | 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 |
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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