JP2007512283A5 - - Google Patents
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- Publication number
- JP2007512283A5 JP2007512283A5 JP2006540387A JP2006540387A JP2007512283A5 JP 2007512283 A5 JP2007512283 A5 JP 2007512283A5 JP 2006540387 A JP2006540387 A JP 2006540387A JP 2006540387 A JP2006540387 A JP 2006540387A JP 2007512283 A5 JP2007512283 A5 JP 2007512283A5
- Authority
- JP
- Japan
- Prior art keywords
- alkoxy
- alkyl
- optionally
- lower alkyl
- lower alkoxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 92
- 125000003545 alkoxy group Chemical group 0.000 claims description 76
- 150000001875 compounds Chemical class 0.000 claims description 27
- 150000003839 salts Chemical class 0.000 claims description 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 18
- -1 methylene, hydroxymethylene Chemical group 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
- 239000001257 hydrogen Substances 0.000 claims description 17
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 125000003342 alkenyl group Chemical group 0.000 claims description 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 5
- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims description 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000004414 alkyl thio group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 2
- 125000005110 aryl thio group Chemical group 0.000 claims description 2
- 125000004104 aryloxy group Chemical group 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 125000003107 substituted aryl group Chemical group 0.000 claims description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims 26
- 229910052736 halogen Inorganic materials 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 21
- 150000002367 halogens Chemical class 0.000 claims 20
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 208000011580 syndromic disease Diseases 0.000 claims 6
- 125000001589 carboacyl group Chemical group 0.000 claims 5
- 208000010877 cognitive disease Diseases 0.000 claims 5
- 208000019553 vascular disease Diseases 0.000 claims 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 125000003302 alkenyloxy group Chemical group 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 208000019901 Anxiety disease Diseases 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 3
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 3
- 208000006029 Cardiomegaly Diseases 0.000 claims 3
- 208000031229 Cardiomyopathies Diseases 0.000 claims 3
- 206010012289 Dementia Diseases 0.000 claims 3
- 206010052337 Diastolic dysfunction Diseases 0.000 claims 3
- 208000010412 Glaucoma Diseases 0.000 claims 3
- 206010019280 Heart failures Diseases 0.000 claims 3
- 206010020571 Hyperaldosteronism Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 206010061216 Infarction Diseases 0.000 claims 3
- 102100028255 Renin Human genes 0.000 claims 3
- 108090000783 Renin Proteins 0.000 claims 3
- 230000002159 abnormal effect Effects 0.000 claims 3
- 238000002399 angioplasty Methods 0.000 claims 3
- 230000036506 anxiety Effects 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 150000001721 carbon Chemical group 0.000 claims 3
- 230000009787 cardiac fibrosis Effects 0.000 claims 3
- 208000020832 chronic kidney disease Diseases 0.000 claims 3
- 208000019425 cirrhosis of liver Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 230000004406 elevated intraocular pressure Effects 0.000 claims 3
- 208000017169 kidney disease Diseases 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 201000001119 neuropathy Diseases 0.000 claims 3
- 230000007823 neuropathy Effects 0.000 claims 3
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims 3
- 230000035755 proliferation Effects 0.000 claims 3
- 208000037803 restenosis Diseases 0.000 claims 3
- 230000002792 vascular Effects 0.000 claims 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 208000002249 Diabetes Complications Diseases 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 150000002829 nitrogen Chemical class 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 230000029936 alkylation Effects 0.000 claims 1
- 238000005804 alkylation reaction Methods 0.000 claims 1
- 125000005530 alkylenedioxy group Chemical group 0.000 claims 1
- 239000000883 anti-obesity agent Substances 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 239000003524 antilipemic agent Substances 0.000 claims 1
- 229940125710 antiobesity agent Drugs 0.000 claims 1
- 125000005325 aryloxy aryl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000019771 cognition Effects 0.000 claims 1
- 125000004367 cycloalkylaryl group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000005326 heteroaryloxy alkyl group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000243 solution Substances 0.000 description 5
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 4
- SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 2
- MZRVEZGGRBJDDB-UHFFFAOYSA-N N-Butyllithium Chemical compound [Li]CCCC MZRVEZGGRBJDDB-UHFFFAOYSA-N 0.000 description 2
- 125000001475 halogen functional group Chemical group 0.000 description 2
- PAAZPARNPHGIKF-UHFFFAOYSA-N 1,2-dibromoethane Chemical compound BrCCBr PAAZPARNPHGIKF-UHFFFAOYSA-N 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 239000012267 brine Substances 0.000 description 1
- 235000019439 ethyl acetate Nutrition 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 238000003818 flash chromatography Methods 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US52537403P | 2003-11-26 | 2003-11-26 | |
| US60/525,374 | 2003-11-26 | ||
| PCT/EP2004/013412 WO2005051895A1 (en) | 2003-11-26 | 2004-11-25 | Organic compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007512283A JP2007512283A (ja) | 2007-05-17 |
| JP2007512283A5 true JP2007512283A5 (enExample) | 2007-12-13 |
| JP4884230B2 JP4884230B2 (ja) | 2012-02-29 |
Family
ID=34632978
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006540387A Expired - Fee Related JP4884230B2 (ja) | 2003-11-26 | 2004-11-25 | 有機化合物 |
Country Status (18)
| Country | Link |
|---|---|
| US (3) | US7582782B2 (enExample) |
| EP (2) | EP2266951A1 (enExample) |
| JP (1) | JP4884230B2 (enExample) |
| KR (1) | KR20060111530A (enExample) |
| CN (2) | CN1882528A (enExample) |
| AU (2) | AU2004293178B8 (enExample) |
| BR (1) | BRPI0417017A (enExample) |
| CA (1) | CA2600973C (enExample) |
| CO (1) | CO5700726A2 (enExample) |
| EC (1) | ECSP066561A (enExample) |
| IL (1) | IL175435A0 (enExample) |
| IS (1) | IS8513A (enExample) |
| MA (1) | MA28175A1 (enExample) |
| NO (1) | NO20062968L (enExample) |
| RU (1) | RU2413716C2 (enExample) |
| TN (1) | TNSN06156A1 (enExample) |
| WO (1) | WO2005051895A1 (enExample) |
| ZA (1) | ZA200602993B (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2266951A1 (en) * | 2003-11-26 | 2010-12-29 | Novartis AG | Organic compounds |
| GB0327839D0 (en) * | 2003-12-01 | 2003-12-31 | Novartis Ag | Organic compounds |
| BRPI0516128A (pt) * | 2004-10-08 | 2008-08-26 | Novartis Ag | uso de inibidores de renina para a prevenção ou tratamento de disfunção diastólica ou insuficiência cardìca diastólica |
| TW200631929A (en) * | 2004-12-10 | 2006-09-16 | Speedel Experimenta Ag | ω -phenyloctanamides |
| WO2006095020A1 (en) * | 2005-03-11 | 2006-09-14 | Speedel Experimenta Ag | Heterocyclic-substituted alkanamides useful as renin inhibitors |
| GB0505969D0 (en) * | 2005-03-23 | 2005-04-27 | Novartis Ag | Organic compounds |
| EP1937248B1 (en) * | 2005-09-17 | 2010-06-02 | Novartis Ag | Alcanoic acid amides substituted by saturated o-heterocycles |
| EP1764098A1 (en) * | 2005-09-17 | 2007-03-21 | Speedel Experimenta AG | Diaminoalcohols derivatives for the treatment of Alzheimer, malaria, HIV |
| GB0521083D0 (en) * | 2005-10-17 | 2005-11-23 | Novartis Ag | Organic compounds |
| US20080255084A1 (en) * | 2005-10-21 | 2008-10-16 | Randy Lee Webb | Combination of Organic Compounds |
| GB2431640A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| GB2431653A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| GB2431645A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| GB2431649A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| GB2431648A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| GB2431642A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| GB2431646A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| GB2431641A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| JP5306821B2 (ja) | 2005-12-30 | 2013-10-02 | ノバルティス アーゲー | レニン阻害剤としての３，５−置換ピペリジン化合物 |
| GB0611697D0 (en) * | 2006-06-13 | 2006-07-26 | Novartis Ag | Organic compounds |
| GB0611696D0 (en) * | 2006-06-13 | 2006-07-26 | Novartis Ag | Organic compounds |
| EP1872780A3 (en) * | 2006-06-14 | 2008-04-30 | Speedel Experimenta AG | Omega-Phenyloctanamides as therapeutic compounds |
| EP1867329A3 (en) * | 2006-06-14 | 2008-05-07 | Speedel Experimenta AG | 5-Amino-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamides as therapeutic compounds |
| WO2007148775A1 (ja) * | 2006-06-23 | 2007-12-27 | Daiichi Sankyo Company, Limited | 鎖状アミン化合物 |
| MX2008016154A (es) * | 2006-06-23 | 2009-01-20 | Daiichi Sankyo Co Ltd | Compuesto de amina ciclica. |
| EP1958666A1 (en) * | 2007-02-13 | 2008-08-20 | Speedel Experimenta AG | Heterocyclic-substituted alkanamides as therapeutic compounds |
| EP2527338B1 (en) | 2007-06-25 | 2015-05-06 | Novartis AG | N5-(2-ethoxyethyl)-n3-(2-pyridinyl) -3,5-piperidinedicarboxamide derivatives for use as renin inhibitors |
| JP5223686B2 (ja) * | 2009-01-07 | 2013-06-26 | 株式会社リコー | 撮像装置および撮像方法 |
| EP2464623B1 (en) | 2009-08-11 | 2020-11-04 | Novartis AG | The ring opening of lactones and lactams |
| US8491927B2 (en) | 2009-12-02 | 2013-07-23 | Nimble Epitech, Llc | Pharmaceutical composition containing a hypomethylating agent and a histone deacetylase inhibitor |
| CN102161627A (zh) * | 2011-02-24 | 2011-08-24 | 中国药科大学 | ω-(N取代-氨基烷基)辛酰胺 |
| WO2012161173A1 (ja) * | 2011-05-23 | 2012-11-29 | 第一三共株式会社 | 置換アミド化合物 |
| WO2012165314A1 (ja) * | 2011-05-27 | 2012-12-06 | 第一三共株式会社 | アミド化合物 |
| WO2013045505A1 (en) | 2011-09-28 | 2013-04-04 | Novartis Ag | Biomarkers for raas combination therapy |
| EP2810644A1 (en) | 2013-06-06 | 2014-12-10 | Ferrer Internacional, S.A. | Oral formulation for the treatment of cardiovascular diseases |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL88619A0 (en) * | 1987-12-15 | 1989-07-31 | Pfizer | Non-peptidic renin inhibitors |
| IL96942A (en) * | 1990-01-31 | 1995-01-24 | Abbott Lab | A pharmaceutical mixture containing a history of amide prevents renin |
| JPH0532602A (ja) * | 1991-07-26 | 1993-02-09 | Terumo Corp | ナフチルメチルアミン誘導体及びこれを含有するレニン阻害剤 |
| JPH06199891A (ja) * | 1992-09-18 | 1994-07-19 | Japan Tobacco Inc | レニン阻害活性を有するアルコール誘導体及びその用途 |
| DE4300388C2 (de) * | 1993-01-09 | 1995-03-16 | Metallgesellschaft Ag | Verfahren zur kontinuierlichen Einstellung und Regelung des pH-Wertes einer sauren Flüssigkeit, bei dem die kontinuierliche Messung des pH-Wertes mit einer Glaselektrode erfolgt |
| MY119161A (en) * | 1994-04-18 | 2005-04-30 | Novartis Ag | Delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amides with enzyme especially renin inhibiting activities |
| US5606078A (en) | 1994-04-18 | 1997-02-25 | Ciba-Geigy Corporation | 3,5-Disubstituted tetrahydrofuran-2-ones |
| US8168616B1 (en) * | 2000-11-17 | 2012-05-01 | Novartis Ag | Combination comprising a renin inhibitor and an angiotensin receptor inhibitor for hypertension |
| AU2003238007A1 (en) * | 2002-06-11 | 2003-12-22 | Elan Pharmaceuticals, Inc. | Methods of treating alzheimer's disease using aryl alkanoic acid amides |
| EP2266951A1 (en) * | 2003-11-26 | 2010-12-29 | Novartis AG | Organic compounds |
-
2004
- 2004-11-25 EP EP10175765A patent/EP2266951A1/en not_active Withdrawn
- 2004-11-25 AU AU2004293178A patent/AU2004293178B8/en not_active Ceased
- 2004-11-25 EP EP04819222A patent/EP1689702B1/en not_active Expired - Lifetime
- 2004-11-25 US US10/579,427 patent/US7582782B2/en not_active Expired - Fee Related
- 2004-11-25 JP JP2006540387A patent/JP4884230B2/ja not_active Expired - Fee Related
- 2004-11-25 CN CNA2004800336784A patent/CN1882528A/zh active Pending
- 2004-11-25 RU RU2006122636/04A patent/RU2413716C2/ru not_active IP Right Cessation
- 2004-11-25 KR KR1020067010193A patent/KR20060111530A/ko not_active Ceased
- 2004-11-25 CN CN2011101379666A patent/CN102260188A/zh active Pending
- 2004-11-25 CA CA2600973A patent/CA2600973C/en not_active Expired - Fee Related
- 2004-11-25 BR BRPI0417017-2A patent/BRPI0417017A/pt not_active IP Right Cessation
- 2004-11-25 WO PCT/EP2004/013412 patent/WO2005051895A1/en not_active Ceased
-
2006
- 2006-04-11 ZA ZA200602993A patent/ZA200602993B/en unknown
- 2006-05-04 IL IL175435A patent/IL175435A0/en unknown
- 2006-05-11 EC EC2006006561A patent/ECSP066561A/es unknown
- 2006-05-24 MA MA29053A patent/MA28175A1/fr unknown
- 2006-05-25 TN TNP2006000156A patent/TNSN06156A1/en unknown
- 2006-06-15 CO CO06058533A patent/CO5700726A2/es not_active Application Discontinuation
- 2006-06-19 IS IS8513A patent/IS8513A/xx unknown
- 2006-06-26 NO NO20062968A patent/NO20062968L/no not_active Application Discontinuation
-
2009
- 2009-03-11 AU AU2009200957A patent/AU2009200957B2/en not_active Ceased
- 2009-06-12 US US12/483,582 patent/US7851642B2/en not_active Expired - Fee Related
- 2009-06-12 US US12/483,599 patent/US7919529B2/en not_active Expired - Fee Related
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