JP2010503682A5 - - Google Patents
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- JP2010503682A5 JP2010503682A5 JP2009528319A JP2009528319A JP2010503682A5 JP 2010503682 A5 JP2010503682 A5 JP 2010503682A5 JP 2009528319 A JP2009528319 A JP 2009528319A JP 2009528319 A JP2009528319 A JP 2009528319A JP 2010503682 A5 JP2010503682 A5 JP 2010503682A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- methyl
- pharmaceutical composition
- compound according
- pyran
- 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.)
- Withdrawn
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- 150000001875 compounds Chemical class 0.000 claims 17
- 108091005502 Aspartic proteases Proteins 0.000 claims 13
- 102000035101 Aspartic proteases Human genes 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 9
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 7
- 239000005541 ACE inhibitor Substances 0.000 claims 5
- 229940118365 Endothelin receptor antagonist Drugs 0.000 claims 5
- 229940125364 angiotensin receptor blocker Drugs 0.000 claims 5
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 5
- -1 methyl compound Chemical class 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 230000009977 dual effect Effects 0.000 claims 4
- 229940044551 receptor antagonist Drugs 0.000 claims 4
- 239000002464 receptor antagonist Substances 0.000 claims 4
- 208000019553 vascular disease Diseases 0.000 claims 4
- 229940123338 Aldosterone synthase inhibitor Drugs 0.000 claims 3
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 3
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 claims 3
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 3
- 239000002160 alpha blocker Substances 0.000 claims 3
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 3
- 239000002876 beta blocker Substances 0.000 claims 3
- 229940097320 beta blocking agent Drugs 0.000 claims 3
- 239000000480 calcium channel blocker Substances 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 239000002934 diuretic Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000002792 enkephalinase inhibitor Substances 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- 230000002792 vascular Effects 0.000 claims 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 2
- KNTZCGBYFGEMFR-UHFFFAOYSA-N (propan-2-ylazaniumyl)formate Chemical compound CC(C)NC(O)=O KNTZCGBYFGEMFR-UHFFFAOYSA-N 0.000 claims 2
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 claims 2
- FZBZOIXHKQUVBU-KGLIPLIRSA-N 2-trimethylsilylethyl n-[(2s)-2-amino-3-[(3r)-oxan-3-yl]propyl]-n-methylcarbamate Chemical compound C[Si](C)(C)CCOC(=O)N(C)C[C@@H](N)C[C@H]1CCCOC1 FZBZOIXHKQUVBU-KGLIPLIRSA-N 0.000 claims 2
- 101710129690 Angiotensin-converting enzyme inhibitor Proteins 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- 101710086378 Bradykinin-potentiating and C-type natriuretic peptides Proteins 0.000 claims 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 2
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 2
- 208000006029 Cardiomegaly Diseases 0.000 claims 2
- 208000031229 Cardiomyopathies Diseases 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 229940097420 Diuretic Drugs 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 108010010369 HIV Protease Proteins 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 206010020571 Hyperaldosteronism Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 206010061216 Infarction Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 208000025966 Neurological disease Diseases 0.000 claims 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 2
- 206010062886 Procedural hypertension Diseases 0.000 claims 2
- 108090000783 Renin Proteins 0.000 claims 2
- 102100028255 Renin Human genes 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 238000002399 angioplasty Methods 0.000 claims 2
- 230000003042 antagnostic effect Effects 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 230000009787 cardiac fibrosis Effects 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 230000001882 diuretic effect Effects 0.000 claims 2
- 230000004410 intraocular pressure Effects 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- YNTOKMNHRPSGFU-UHFFFAOYSA-N n-Propyl carbamate Chemical compound CCCOC(N)=O YNTOKMNHRPSGFU-UHFFFAOYSA-N 0.000 claims 2
- 108010020708 plasmepsin Proteins 0.000 claims 2
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 150000003892 tartrate salts Chemical class 0.000 claims 2
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 1
- 102000008873 Angiotensin II receptor Human genes 0.000 claims 1
- 108050000824 Angiotensin II receptor Proteins 0.000 claims 1
- 102000015427 Angiotensins Human genes 0.000 claims 1
- 108010064733 Angiotensins Proteins 0.000 claims 1
- 102000002045 Endothelin Human genes 0.000 claims 1
- 108050009340 Endothelin Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 229940124308 alpha-adrenoreceptor antagonist Drugs 0.000 claims 1
- 125000006242 amine protecting group Chemical group 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940030606 diuretics Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000029142 excretion Effects 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000001452 natriuretic effect Effects 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- FBAOEVPHUAUGSW-MIEMQEKWSA-N CNC[C@H](CC1COCCC1)NC(N(CCC1)C[C@@H]1[C@H](c1cc(Cl)cc(F)c1)OCCNC(OC)=O)=O Chemical compound CNC[C@H](CC1COCCC1)NC(N(CCC1)C[C@@H]1[C@H](c1cc(Cl)cc(F)c1)OCCNC(OC)=O)=O FBAOEVPHUAUGSW-MIEMQEKWSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US84533106P | 2006-09-18 | 2006-09-18 | |
| PCT/US2007/020086 WO2008036216A1 (en) | 2006-09-18 | 2007-09-17 | Piperidine derivatives as renin inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010503682A JP2010503682A (ja) | 2010-02-04 |
| JP2010503682A5 true JP2010503682A5 (2) | 2010-11-11 |
Family
ID=38926325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009528319A Withdrawn JP2010503682A (ja) | 2006-09-18 | 2007-09-17 | レニン阻害剤としてのピペリジン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20090318501A1 (2) |
| EP (1) | EP2081927B1 (2) |
| JP (1) | JP2010503682A (2) |
| AT (1) | ATE520690T1 (2) |
| WO (1) | WO2008036216A1 (2) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0516132A (pt) | 2004-10-07 | 2007-12-04 | Vitae Pharmaceuticals Inc | compostos, composição destes, método de antagonização de uma ou mais proteases aspárticas e método para tratar ou melhorar um distúrbio mediado por protease aspártica |
| TWI411607B (zh) * | 2005-11-14 | 2013-10-11 | Vitae Pharmaceuticals Inc | 天門冬胺酸蛋白酶抑制劑 |
| CL2007002689A1 (es) * | 2006-09-18 | 2008-04-18 | Vitae Pharmaceuticals Inc | Compuestos derivados de piperidin-1-carboxamida, inhibidores de la renina; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como hipertension, insuficiencia cardiaca, fibrosis cardiaca, entre otras. |
| WO2009096996A1 (en) * | 2007-06-20 | 2009-08-06 | Smithkline Beecham Corporation | Renin inhibitors |
| EP2170815A2 (en) * | 2007-06-20 | 2010-04-07 | Vitae Pharmaceuticals, Inc. | Renin inhibitors |
| KR101403311B1 (ko) | 2008-05-05 | 2014-06-05 | 액테리온 파마슈티칼 리미티드 | 레닌 억제제로서의 3,4-치환된 피페리딘 유도체 |
| EP2307396A1 (en) * | 2008-06-20 | 2011-04-13 | Vitae Pharmaceuticals, Inc. | Renin inhibitors and method of use thereof |
| CA2729052A1 (en) * | 2008-06-26 | 2009-12-30 | Vitae Pharmaceuticals, Inc. | Salts of methyl 2-((r)-(3-chlorophenyl)((r)-1-((s)-2-(methylamino)-3((r)-tetrahydro-2h-pyran-3-yl)propylcarbamoyl)piperidin-3-yl)methoxy)ethylcarbamate |
| US20100010228A1 (en) * | 2008-06-26 | 2010-01-14 | Vitae Pharmaceuticals, Inc. | Process for the asymmetric reduction of 3-benzoylpiperidines |
| AR077692A1 (es) * | 2009-08-06 | 2011-09-14 | Vitae Pharmaceuticals Inc | Sales de 2-((r)-(3-clorofenil) ((r)-1-((s) -2-(metilamino)-3-((r)-tetrahidro-2h-piran-3-il) propilcarbamoil) piperidin -3-il) metoxi) etilcarbamato de metilo |
| US20120164120A1 (en) * | 2010-12-23 | 2012-06-28 | Food Industry Research And Development Institute | Novel monascuspurpurones, preparation process thereof, and uses of the monascuspurpurones |
| USRE50663E1 (en) | 2017-10-04 | 2025-11-18 | Bayer Aktiengesellschaft | Heterocycle derivatives as pesticides |
| US11414432B2 (en) | 2018-03-12 | 2022-08-16 | Bayer Aktiengesellschaft | Condensed bicyclic heterocyclic derivatives as pest control agents |
| WO2019201921A1 (de) | 2018-04-20 | 2019-10-24 | Bayer Aktiengesellschaft | Heterocyclen-derivate als schädlingsbekämpfungsmittel |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3017618A (en) * | 1960-04-25 | 1962-01-16 | Eastman Kodak Co | Device for removing and detecting foreign matter from a surface |
| US4908372A (en) * | 1988-10-13 | 1990-03-13 | Merrell Dow Pharmaceuticals Inc. | Antihistaminic piperidinyl benzimidazoles |
| DE4018070A1 (de) * | 1990-06-06 | 1991-12-12 | Bayer Ag | Morpholinoharnstoff-derivate |
| CA2097317C (en) * | 1990-12-14 | 2002-02-12 | Albert A. Carr | Antiallergic piperdinyl benzimidazoles |
| NZ249286A (en) * | 1992-02-13 | 1996-02-27 | Merrell Dow Pharma | Piperidine-4-ylmethyl thiophene and thiazole derivatives and pharmaceutical compositions |
| US5767144A (en) * | 1994-08-19 | 1998-06-16 | Abbott Laboratories | Endothelin antagonists |
| US6162927A (en) * | 1994-08-19 | 2000-12-19 | Abbott Laboratories | Endothelin antagonists |
| US6946481B1 (en) * | 1994-08-19 | 2005-09-20 | Abbott Laboratories | Endothelin antagonists |
| GB9826540D0 (en) * | 1998-12-02 | 1999-01-27 | Darwin Discovery Ltd | Process |
| US6900329B2 (en) * | 2001-03-21 | 2005-05-31 | Schering Corporation | MCH antagonists and their use in the treatment of obesity |
| AU2002359376B2 (en) * | 2001-11-08 | 2008-01-10 | Elan Pharmaceuticals, Inc. | N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives |
| US7557137B2 (en) * | 2002-08-05 | 2009-07-07 | Bristol-Myers Squibb Company | Gamma-lactams as beta-secretase inhibitors |
| US20070093492A1 (en) * | 2004-03-09 | 2007-04-26 | Weir-Torn Jiaang | Pyrrolidine derivatives |
| BRPI0516132A (pt) * | 2004-10-07 | 2007-12-04 | Vitae Pharmaceuticals Inc | compostos, composição destes, método de antagonização de uma ou mais proteases aspárticas e método para tratar ou melhorar um distúrbio mediado por protease aspártica |
| TWI411607B (zh) * | 2005-11-14 | 2013-10-11 | Vitae Pharmaceuticals Inc | 天門冬胺酸蛋白酶抑制劑 |
| US7872028B2 (en) * | 2006-04-05 | 2011-01-18 | Vitae Pharmaceuticals, Inc. | Diaminopropanol renin inhibitors |
| CL2007002689A1 (es) * | 2006-09-18 | 2008-04-18 | Vitae Pharmaceuticals Inc | Compuestos derivados de piperidin-1-carboxamida, inhibidores de la renina; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como hipertension, insuficiencia cardiaca, fibrosis cardiaca, entre otras. |
| EP2170815A2 (en) * | 2007-06-20 | 2010-04-07 | Vitae Pharmaceuticals, Inc. | Renin inhibitors |
| WO2009096996A1 (en) * | 2007-06-20 | 2009-08-06 | Smithkline Beecham Corporation | Renin inhibitors |
| US7773441B2 (en) * | 2008-06-18 | 2010-08-10 | Micron Technology, Inc. | Memory malfunction prediction system and method |
-
2007
- 2007-09-17 US US12/311,020 patent/US20090318501A1/en not_active Abandoned
- 2007-09-17 EP EP07838310A patent/EP2081927B1/en active Active
- 2007-09-17 WO PCT/US2007/020086 patent/WO2008036216A1/en not_active Ceased
- 2007-09-17 JP JP2009528319A patent/JP2010503682A/ja not_active Withdrawn
- 2007-09-17 AT AT07838310T patent/ATE520690T1/de not_active IP Right Cessation
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