JP4790871B2 - レニン阻害剤としての3,4−置換ピペリジン誘導体 - Google Patents
レニン阻害剤としての3,4−置換ピペリジン誘導体 Download PDFInfo
- Publication number
- JP4790871B2 JP4790871B2 JP2011507765A JP2011507765A JP4790871B2 JP 4790871 B2 JP4790871 B2 JP 4790871B2 JP 2011507765 A JP2011507765 A JP 2011507765A JP 2011507765 A JP2011507765 A JP 2011507765A JP 4790871 B2 JP4790871 B2 JP 4790871B2
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- Prior art keywords
- methyl
- amine
- added
- etoac
- solution
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- 0 Bc1c(C)c(*)cc(CN(C2CC2)C([C@@](C*CC2)[C@@]2(*)C(C(*)=C(*2C)N)=CC2=N)=O)c1* Chemical compound Bc1c(C)c(*)cc(CN(C2CC2)C([C@@](C*CC2)[C@@]2(*)C(C(*)=C(*2C)N)=CC2=N)=O)c1* 0.000 description 3
- RXVHRSQNFLHWSJ-UHFFFAOYSA-N CCC(NCCC[n]1c(cccc2)c2c(CN(C2CC2)C(C(CNCC2)C2C(C=CN2C)=CC2=O)=O)c1)=O Chemical compound CCC(NCCC[n]1c(cccc2)c2c(CN(C2CC2)C(C(CNCC2)C2C(C=CN2C)=CC2=O)=O)c1)=O RXVHRSQNFLHWSJ-UHFFFAOYSA-N 0.000 description 1
- AUOWJTDDNOBEPP-UHFFFAOYSA-N CN(C=CC(C(CCNC1)C1C(N(Cc1c[n](CCCOC)c2cccc(Cl)c12)C1CC1)=O)=C1)C1=O Chemical compound CN(C=CC(C(CCNC1)C1C(N(Cc1c[n](CCCOC)c2cccc(Cl)c12)C1CC1)=O)=C1)C1=O AUOWJTDDNOBEPP-UHFFFAOYSA-N 0.000 description 1
- IBKQTWGVJJTVKN-UHFFFAOYSA-N CN(C=CC(C(CCNC1)C1C(N(Cc1c[n](Cc(cc2)ccc2F)c2c1cccc2)C1CC1)=O)=C1)C1=O Chemical compound CN(C=CC(C(CCNC1)C1C(N(Cc1c[n](Cc(cc2)ccc2F)c2c1cccc2)C1CC1)=O)=C1)C1=O IBKQTWGVJJTVKN-UHFFFAOYSA-N 0.000 description 1
- NHUZFDRZCZFLLH-UHFFFAOYSA-N CN(C=CC(C(CCNC1)C1C(N(Cc1cc(C(F)(F)F)cc(CCCOC)c1)C1CC1)=O)=C1)C1=O Chemical compound CN(C=CC(C(CCNC1)C1C(N(Cc1cc(C(F)(F)F)cc(CCCOC)c1)C1CC1)=O)=C1)C1=O NHUZFDRZCZFLLH-UHFFFAOYSA-N 0.000 description 1
- IUBYUFBUDVQHOF-UHFFFAOYSA-N CN(C=CC(C(CCNC1)C1C(N(Cc1ccccc1Br)C1CC1)=O)=C1)C1=O Chemical compound CN(C=CC(C(CCNC1)C1C(N(Cc1ccccc1Br)C1CC1)=O)=C1)C1=O IUBYUFBUDVQHOF-UHFFFAOYSA-N 0.000 description 1
- LUCFTDJEKKRCSW-YNMFNDETSA-N CN(C=CC(C(CCNC1)[C@H]1C(N(Cc1c[n](CCCOC)c(cc2)c1cc2F)C1CC1)=O)=C1)C1=O Chemical compound CN(C=CC(C(CCNC1)[C@H]1C(N(Cc1c[n](CCCOC)c(cc2)c1cc2F)C1CC1)=O)=C1)C1=O LUCFTDJEKKRCSW-YNMFNDETSA-N 0.000 description 1
- FEFMYHRWHRBBAH-WCSIJFPASA-N CN(C=CC(C(CCNC1)[C@H]1C(N(Cc1c[n](CCCOC)c2cccc(F)c12)C1CC1)=O)=C1)C1=O Chemical compound CN(C=CC(C(CCNC1)[C@H]1C(N(Cc1c[n](CCCOC)c2cccc(F)c12)C1CC1)=O)=C1)C1=O FEFMYHRWHRBBAH-WCSIJFPASA-N 0.000 description 1
- UGAWEDRJDIKHFH-UHFFFAOYSA-N Cc1cccc(C[n]2c(cccc3)c3c(CN(C3CC3)C(C(CNCC3)C3C(C=CN3C)=CC3=O)=O)c2)c1 Chemical compound Cc1cccc(C[n]2c(cccc3)c3c(CN(C3CC3)C(C(CNCC3)C3C(C=CN3C)=CC3=O)=O)c2)c1 UGAWEDRJDIKHFH-UHFFFAOYSA-N 0.000 description 1
- SJIIDWBFRZACDQ-UHFFFAOYSA-N SCc1ccccn1 Chemical compound SCc1ccccn1 SJIIDWBFRZACDQ-UHFFFAOYSA-N 0.000 description 1
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- C07—ORGANIC CHEMISTRY
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- C07D401/00—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
- C07D401/14—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 three or more hetero rings
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- 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
- A61K31/4545—Non 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
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/02—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D417/14—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 containing three or more hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Reproductive Health (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Immunology (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Pregnancy & Childbirth (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12652908P | 2008-05-05 | 2008-05-05 | |
| US61/126,529 | 2008-05-05 | ||
| US18830308P | 2008-08-07 | 2008-08-07 | |
| US61/188,303 | 2008-08-07 | ||
| PCT/CA2009/000611 WO2009135299A1 (en) | 2008-05-05 | 2009-05-04 | 3, 4 - substituted piperidine derivatives as renin inhibitors |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011123054A Division JP5587246B2 (ja) | 2008-05-05 | 2011-06-01 | レニン阻害剤としての3,4−置換ピペリジン誘導体 |
| JP2011123057A Division JP5653842B2 (ja) | 2008-05-05 | 2011-06-01 | レニン阻害剤としての3,4−置換ピペリジン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011519871A JP2011519871A (ja) | 2011-07-14 |
| JP2011519871A5 JP2011519871A5 (enExample) | 2011-08-25 |
| JP4790871B2 true JP4790871B2 (ja) | 2011-10-12 |
Family
ID=41264366
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011507765A Expired - Fee Related JP4790871B2 (ja) | 2008-05-05 | 2009-05-04 | レニン阻害剤としての3,4−置換ピペリジン誘導体 |
| JP2011123057A Expired - Fee Related JP5653842B2 (ja) | 2008-05-05 | 2011-06-01 | レニン阻害剤としての3,4−置換ピペリジン誘導体 |
| JP2011123054A Expired - Fee Related JP5587246B2 (ja) | 2008-05-05 | 2011-06-01 | レニン阻害剤としての3,4−置換ピペリジン誘導体 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011123057A Expired - Fee Related JP5653842B2 (ja) | 2008-05-05 | 2011-06-01 | レニン阻害剤としての3,4−置換ピペリジン誘導体 |
| JP2011123054A Expired - Fee Related JP5587246B2 (ja) | 2008-05-05 | 2011-06-01 | レニン阻害剤としての3,4−置換ピペリジン誘導体 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US8889714B2 (enExample) |
| EP (1) | EP2274295B1 (enExample) |
| JP (3) | JP4790871B2 (enExample) |
| KR (2) | KR101403311B1 (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) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2296653B1 (en) | 2008-06-03 | 2016-01-27 | Intermune, Inc. | Compounds and methods for treating inflammatory and fibrotic disorders |
| AU2009326797B2 (en) * | 2008-12-10 | 2012-12-13 | Merck Canada Inc. | 3,4 - substituted piperidine derivatives as renin inhibitors |
| TWI562977B (en) * | 2010-11-05 | 2016-12-21 | Bayer Ip Gmbh | Process for the preparation of substituted n-(benzyl)cyclopropanamines by imine hydrogenation |
| 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 |
| RU2692485C2 (ru) | 2014-04-02 | 2019-06-25 | Интермьюн, Инк. | Противофиброзные пиридиноны |
| 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 |
| WO2020109039A1 (en) | 2018-11-28 | 2020-06-04 | Basf Se | Pesticidal compounds |
| EP4143167B1 (en) | 2020-04-28 | 2024-05-15 | Basf Se | Pesticidal compounds |
Family Cites Families (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5380758A (en) | 1991-03-29 | 1995-01-10 | Brigham And Women's Hospital | S-nitrosothiols as smooth muscle relaxants and therapeutic uses thereof |
| US5703073A (en) | 1995-04-19 | 1997-12-30 | Nitromed, Inc. | Compositions and methods to prevent toxicity induced by nonsteroidal antiinflammatory drugs |
| PL193686B1 (pl) | 1995-09-07 | 2007-03-30 | Hoffmann La Roche | Pochodne piperydyny, środki lecznicze zawierającepochodne piperydyny, sposoby wytwarzania tych pochodnych oraz zastosowanie pochodnych |
| US5994294A (en) | 1996-02-02 | 1999-11-30 | Nitromed, Inc. | Nitrosated and nitrosylated α-adrenergic receptor antagonist compounds, compositions and their uses |
| CA2270118A1 (en) | 1996-11-01 | 1998-05-14 | Nitromed Inc. | Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses |
| IT1295694B1 (it) | 1996-11-14 | 1999-05-27 | Nicox Sa | Nitrossi derivati per la preparazione di medicamenti ad attivita antitrombinica |
| IT1292426B1 (it) | 1997-06-27 | 1999-02-08 | Nicox Sa | Sali nitrati di ace-inibitori |
| KR100600550B1 (ko) | 2000-10-20 | 2006-07-13 | 에자이 가부시키가이샤 | 질소 함유 방향환 유도체 |
| KR100783863B1 (ko) | 2002-04-29 | 2007-12-10 | 액테리온 파마슈티칼 리미티드 | 7-아릴-3,9-디아자바이사이클로(3.3.1)논-6-엔 유도체 및고혈압, 심혈관 질환 또는 신장 질환의 치료에서 레닌저해물질로써 이들의 용도 |
| MXPA04012136A (es) | 2002-06-27 | 2005-04-19 | Actelion Pharmaceuticals Ltd | Nuevos derivados de tetrahidropiridina como inhibidores de renina. |
| US20040204455A1 (en) | 2003-04-10 | 2004-10-14 | Cody Wayne Livingston | Piperidine derivative rennin inhibitors |
| US20060217371A1 (en) | 2003-04-28 | 2006-09-28 | Olivier Bezencon | Diazabicyclononene and tetrahydropyriddine derivatives as renin inhibitors |
| MXPA05011478A (es) | 2003-04-29 | 2005-12-12 | Actelion Pharmaceuticals Ltd | Derivados de 1,2,3,6-tetrahidropiridina 3,4-disustituidos novedosos. |
| CA2521938A1 (en) | 2003-04-30 | 2004-11-11 | Actelion Pharmaceuticals Ltd | 9-azabicyclo[3.3.1]non-6-ene derivatives with a heteroatom at the 3-position as renin inhibitors |
| MXPA05011497A (es) | 2003-04-30 | 2005-12-15 | Actelion Pharmaceuticals Ltd | Derivados de tropano y su uso como inhibidores de la enzima de conversion de angiotensina (ace). |
| MXPA05011496A (es) | 2003-04-30 | 2005-12-15 | Actelion Pharmaceuticals Ltd | Derivados de azabiciclononeno. |
| EP1622564A2 (en) | 2003-05-02 | 2006-02-08 | Actelion Pharmaceuticals Ltd. | Diazabicyclononene derivatives |
| TW200513461A (en) | 2003-10-01 | 2005-04-16 | Speedel Experimenta Ag | Organische verbindungen |
| CN1863773A (zh) | 2003-10-09 | 2006-11-15 | 埃科特莱茵药品有限公司 | 四氢吡啶衍生物 |
| JP2007508262A (ja) | 2003-10-13 | 2007-04-05 | アクテリオン ファマシューティカルズ リミテッド | 新規ジアザビシクロノネン誘導体およびその使用 |
| CA2540817A1 (en) | 2003-10-23 | 2005-05-06 | Olivier Bezencon | Diazabicyclononene and tetrahydropyridine derivatives as renin inhibitors |
| US20070111989A1 (en) | 2003-12-05 | 2007-05-17 | Olivier Bezencon | Novel diazabicyclononene derivatives and use |
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