JPH04502458A - レニン阻害性ペプチド類の経皮および鼻腔内投与 - Google Patents
レニン阻害性ペプチド類の経皮および鼻腔内投与Info
- Publication number
- JPH04502458A JPH04502458A JP2501323A JP50132390A JPH04502458A JP H04502458 A JPH04502458 A JP H04502458A JP 2501323 A JP2501323 A JP 2501323A JP 50132390 A JP50132390 A JP 50132390A JP H04502458 A JPH04502458 A JP H04502458A
- Authority
- JP
- Japan
- Prior art keywords
- pro
- mehis
- lva
- peptide
- ile
- 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.)
- Pending
Links
- 108090000765 processed proteins & peptides Proteins 0.000 title claims description 25
- 108090000783 Renin Proteins 0.000 title claims description 12
- 102100028255 Renin Human genes 0.000 title claims description 11
- 230000002401 inhibitory effect Effects 0.000 title claims description 9
- 102000004196 processed proteins & peptides Human genes 0.000 title description 7
- 108010026906 renin inhibitory peptide Proteins 0.000 claims description 14
- 241000124008 Mammalia Species 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 10
- AIRMFERKNRDUKD-QLAANKDXSA-N (2s)-6-amino-2-[[(2s)-3-(4-hydroxyphenyl)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-3-(1h-imidazol-5-yl)-2-[[(2s)-2-[[1-[(2s)-3-(1h-imidazol-5-yl)-2-[[(2s)-pyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]propanoyl]am Chemical compound C([C@@H](C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CCCCN)C(O)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)C1N(CCC1)C(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NCCC1)C1=CC=CC=C1 AIRMFERKNRDUKD-QLAANKDXSA-N 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 206010020772 Hypertension Diseases 0.000 claims description 6
- 150000001204 N-oxides Chemical class 0.000 claims description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
- 230000037317 transdermal delivery Effects 0.000 claims description 5
- 210000003928 nasal cavity Anatomy 0.000 claims description 4
- 230000002265 prevention Effects 0.000 claims description 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- ILVXOBCQQYKLDS-UHFFFAOYSA-N pyridine N-oxide Chemical compound [O-][N+]1=CC=CC=C1 ILVXOBCQQYKLDS-UHFFFAOYSA-N 0.000 claims 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 18
- 150000001875 compounds Chemical class 0.000 description 9
- 241000700159 Rattus Species 0.000 description 5
- 102000004169 proteins and genes Human genes 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 230000036772 blood pressure Effects 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 210000000609 ganglia Anatomy 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 102000004881 Angiotensinogen Human genes 0.000 description 2
- 108090001067 Angiotensinogen Proteins 0.000 description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 101000579218 Homo sapiens Renin Proteins 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 229960001760 dimethyl sulfoxide Drugs 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 102000015427 Angiotensins Human genes 0.000 description 1
- 108010064733 Angiotensins Proteins 0.000 description 1
- -1 Boc Chemical class 0.000 description 1
- 241000723347 Cinnamomum Species 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 208000003098 Ganglion Cysts Diseases 0.000 description 1
- 208000001953 Hypotension Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 208000005400 Synovial Cyst Diseases 0.000 description 1
- 125000000539 amino acid group Chemical group 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 230000003276 anti-hypertensive effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 230000004531 blood pressure lowering effect Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 235000017803 cinnamon Nutrition 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000001087 glyceryl triacetate Substances 0.000 description 1
- 235000013773 glyceryl triacetate Nutrition 0.000 description 1
- 208000021822 hypotensive Diseases 0.000 description 1
- 230000001077 hypotensive effect Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 210000003127 knee Anatomy 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 230000002315 pressor effect Effects 0.000 description 1
- FOWDZVNRQHPXDO-UHFFFAOYSA-N propyl hydrogen carbonate Chemical compound CCCOC(O)=O FOWDZVNRQHPXDO-UHFFFAOYSA-N 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 239000002461 renin inhibitor Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000011269 tar Substances 0.000 description 1
- 238000013271 transdermal drug delivery Methods 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/55—Protease inhibitors
- A61K38/553—Renin inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Otolaryngology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28853188A | 1988-12-22 | 1988-12-22 | |
| US288,531 | 1988-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH04502458A true JPH04502458A (ja) | 1992-05-07 |
Family
ID=23107533
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2501323A Pending JPH04502458A (ja) | 1988-12-22 | 1989-12-01 | レニン阻害性ペプチド類の経皮および鼻腔内投与 |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP0449943A1 (de) |
| JP (1) | JPH04502458A (de) |
| AU (1) | AU4664089A (de) |
| CA (1) | CA2004571A1 (de) |
| WO (1) | WO1990006761A1 (de) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19819652A1 (de) * | 1998-05-02 | 1999-11-11 | Lohmann Therapie Syst Lts | Therapeutisches System zur topischen oder transmucosalen Applikation wenigstens eines Pflege- oder Wirkstoffs auf bzw. durch die Nasenschleimhaut sowie Verfahren zur Applikation des Systems |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK356085A (da) * | 1984-08-06 | 1986-02-07 | Upjohn Co | Reninhaemmende peptid eller et farmaceutisk acceptabelt syreadditionssalt deraf |
| US4906613A (en) * | 1985-11-05 | 1990-03-06 | Schering Corporation | Antiglaucoma compositions and methods |
| US4758584A (en) * | 1987-02-05 | 1988-07-19 | Ciba-Geigy Corporation | Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups |
-
1989
- 1989-12-01 WO PCT/US1989/005343 patent/WO1990006761A1/en not_active Ceased
- 1989-12-01 AU AU46640/89A patent/AU4664089A/en not_active Abandoned
- 1989-12-01 JP JP2501323A patent/JPH04502458A/ja active Pending
- 1989-12-01 EP EP90901256A patent/EP0449943A1/de not_active Withdrawn
- 1989-12-05 CA CA002004571A patent/CA2004571A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU4664089A (en) | 1990-07-10 |
| EP0449943A1 (de) | 1991-10-09 |
| CA2004571A1 (en) | 1990-06-22 |
| WO1990006761A1 (en) | 1990-06-28 |
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