JP2005504011A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2005504011A5 JP2005504011A5 JP2002589505A JP2002589505A JP2005504011A5 JP 2005504011 A5 JP2005504011 A5 JP 2005504011A5 JP 2002589505 A JP2002589505 A JP 2002589505A JP 2002589505 A JP2002589505 A JP 2002589505A JP 2005504011 A5 JP2005504011 A5 JP 2005504011A5
- Authority
- JP
- Japan
- Prior art keywords
- lower alkyl
- carbocyclic
- hydrogen
- aryl
- represent
- 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
- 229910052739 hydrogen Inorganic materials 0.000 claims description 32
- 239000001257 hydrogen Substances 0.000 claims description 32
- 150000001875 compounds Chemical class 0.000 claims description 25
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 8
- -1 pyrrolidinocarbonyl Chemical group 0.000 claims description 8
- 241000124008 Mammalia Species 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 150000002148 esters Chemical group 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims description 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 51
- 125000002837 carbocyclic group Chemical group 0.000 claims 20
- 150000002431 hydrogen Chemical group 0.000 claims 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000002252 acyl group Chemical group 0.000 claims 11
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000005841 biaryl group Chemical group 0.000 claims 5
- 125000004487 4-tetrahydropyranyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 3
- JQCSUVJDBHJKNG-UHFFFAOYSA-N 1-methoxy-ethyl Chemical group C[CH]OC JQCSUVJDBHJKNG-UHFFFAOYSA-N 0.000 claims 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 2
- 239000005977 Ethylene Substances 0.000 claims 2
- 125000004423 acyloxy group Chemical group 0.000 claims 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 150000002019 disulfides Chemical class 0.000 claims 2
- 125000004175 fluorobenzyl group Chemical group 0.000 claims 2
- 125000001207 fluorophenyl group Chemical group 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 125000006518 morpholino carbonyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])N(C(*)=O)C1([H])[H] 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 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 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000029422 Hypernatremia Diseases 0.000 claims 1
- 102000003729 Neprilysin Human genes 0.000 claims 1
- 108090000028 Neprilysin Proteins 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 1
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 1
- 125000001118 alkylidene group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 6
- 239000000203 mixture Substances 0.000 description 5
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 1
- UKAUYVFTDYCKQA-UHFFFAOYSA-N -2-Amino-4-hydroxybutanoic acid Natural products OC(=O)C(N)CCO UKAUYVFTDYCKQA-UHFFFAOYSA-N 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 241000416162 Astragalus gummifer Species 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 241000282693 Cercopithecidae Species 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
- UKAUYVFTDYCKQA-VKHMYHEASA-N L-homoserine Chemical compound OC(=O)[C@@H](N)CCO UKAUYVFTDYCKQA-VKHMYHEASA-N 0.000 description 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical class [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 1
- 239000004473 Threonine Substances 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- 239000002250 absorbent Substances 0.000 description 1
- 230000002745 absorbent Effects 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000008272 agar Substances 0.000 description 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 125000001769 aryl amino group Chemical group 0.000 description 1
- 125000005135 aryl sulfinyl group Chemical group 0.000 description 1
- BTMRYSYEOPOPBR-UHFFFAOYSA-N benzene;ethane Chemical compound CC.C1=CC=CC=C1 BTMRYSYEOPOPBR-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000012267 brine Substances 0.000 description 1
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- 239000000543 intermediate Substances 0.000 description 1
- 125000002346 iodo group Chemical group I* 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- VNWKTOKETHGBQD-UHFFFAOYSA-N methane Chemical compound C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000008137 solubility enhancer Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29108801P | 2001-05-15 | 2001-05-15 | |
| US33957501P | 2001-12-11 | 2001-12-11 | |
| PCT/EP2002/005293 WO2002092622A2 (en) | 2001-05-15 | 2002-05-14 | Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005504011A JP2005504011A (ja) | 2005-02-10 |
| JP2005504011A5 true JP2005504011A5 (enExample) | 2006-01-05 |
| JP4390458B2 JP4390458B2 (ja) | 2009-12-24 |
Family
ID=26966569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002589505A Expired - Fee Related JP4390458B2 (ja) | 2001-05-15 | 2002-05-14 | バソペプチダーゼ阻害剤としてｎ−末端２−チオアシル基を有するジペプチド誘導体 |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US6777443B2 (enExample) |
| EP (2) | EP1392720A2 (enExample) |
| JP (1) | JP4390458B2 (enExample) |
| KR (1) | KR100908152B1 (enExample) |
| CN (1) | CN1649893A (enExample) |
| AR (1) | AR035890A1 (enExample) |
| AU (1) | AU2002314067B2 (enExample) |
| BR (1) | BR0209652A (enExample) |
| CA (1) | CA2449292A1 (enExample) |
| CO (1) | CO5540347A2 (enExample) |
| CZ (1) | CZ20033077A3 (enExample) |
| HU (1) | HUP0304084A3 (enExample) |
| IL (1) | IL158772A0 (enExample) |
| MX (1) | MXPA03010403A (enExample) |
| MY (1) | MY127495A (enExample) |
| NO (1) | NO20035084L (enExample) |
| NZ (1) | NZ529438A (enExample) |
| PE (1) | PE20030042A1 (enExample) |
| PL (1) | PL366786A1 (enExample) |
| RU (1) | RU2298559C2 (enExample) |
| SK (1) | SK14032003A3 (enExample) |
| TW (1) | TWI295996B (enExample) |
| WO (1) | WO2002092622A2 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6777443B2 (en) * | 2001-05-15 | 2004-08-17 | Novartis Ag | Dipeptide derivatives |
| WO2003004456A1 (en) * | 2001-07-06 | 2003-01-16 | Teva Pharmaceutical Industries Ltd. | Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives |
| WO2003027091A1 (en) * | 2001-09-21 | 2003-04-03 | Novartis Ag | Pyrane derivatives as both ace- and nep- inhibitors |
| SI1467728T1 (sl) * | 2002-01-17 | 2008-02-29 | Novartis Ag | Farmacevtski sestavki vkljucujoci valsartan in NEP inhibitorje |
| US7468390B2 (en) | 2002-01-17 | 2008-12-23 | Novartis Ag | Methods of treatment and pharmaceutical composition |
| AU2003276960A1 (en) * | 2002-06-13 | 2003-12-31 | Novartis Ag | Calcium salts of indole derived statins |
| EP1750862B1 (en) | 2004-06-04 | 2011-01-05 | Teva Pharmaceutical Industries Ltd. | Pharmaceutical composition containing irbesartan |
| MX2007006279A (es) * | 2004-12-15 | 2007-06-14 | Solvay Pharm Gmbh | Composiciones farmaceuticas que comprenden inhibidores de nep, inhibidores del sistema de produccion de endotelina endogena, e inhibidores de hmg coa-reductasa. |
| JP2008533109A (ja) * | 2005-03-14 | 2008-08-21 | オリオン コーポレーション | 利尿を促進するための複合治療 |
| US7390789B2 (en) * | 2005-09-13 | 2008-06-24 | William H Simmons | Thio-containing inhibitors of aminopeptidase P, and compositions thereof |
| US7400236B2 (en) | 2005-10-21 | 2008-07-15 | Gm Global Technology Operations, Inc. | Vehicular lane monitoring system utilizing front and rear cameras |
| AR057882A1 (es) | 2005-11-09 | 2007-12-26 | Novartis Ag | Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra |
| US20120157387A1 (en) * | 2006-11-28 | 2012-06-21 | Apotex Technologies Inc. | Orally bioavailable d-gamma-glutamyl-d-tryptophan |
| TW200838501A (en) * | 2007-02-02 | 2008-10-01 | Theravance Inc | Dual-acting antihypertensive agents |
| TWI448284B (zh) * | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| TWI406850B (zh) | 2007-06-05 | 2013-09-01 | Theravance Inc | 雙效苯并咪唑抗高血壓劑 |
| WO2009035543A1 (en) | 2007-09-07 | 2009-03-19 | Theravance, Inc. | Dual-acting antihypertensive agents |
| ES2385773T3 (es) | 2007-12-11 | 2012-07-31 | Theravance, Inc. | Derivados de benzoimidazol, de doble acción, y su utilización como agentes antihipertensivos |
| US7989484B2 (en) | 2008-04-29 | 2011-08-02 | Theravance, Inc. | Dual-acting antihypertensive agents |
| US7863309B2 (en) | 2008-07-24 | 2011-01-04 | Theravance, Inc. | Dual-acting antihypertensive agents |
| JP5833000B2 (ja) | 2009-07-07 | 2015-12-16 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | 二重に作用するピラゾール抗高血圧症薬 |
| ES2441419T3 (es) | 2009-07-22 | 2014-02-04 | Theravance, Inc. | Agentes antihipertensivos de doble acción basados en oxazol |
| US8481549B2 (en) * | 2010-01-19 | 2013-07-09 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
| EA201391421A1 (ru) * | 2011-03-31 | 2014-02-28 | Апотекс Текнолоджиз Инк. | Пролекарства d-гамма-глутамил-d-триптофана и d-гамма-глутамил-l-триптофана |
| US9212206B1 (en) | 2014-11-24 | 2015-12-15 | William H Simmons | 4-Fluoro-Thio-containing inhibitors of APP2, compositions thereof and method of use |
| WO2018002673A1 (en) | 2016-07-01 | 2018-01-04 | N4 Pharma Uk Limited | Novel formulations of angiotensin ii receptor antagonists |
| UY38072A (es) | 2018-02-07 | 2019-10-01 | Novartis Ag | Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos |
| US11396497B2 (en) | 2018-05-04 | 2022-07-26 | New Mexico Tech University Research Park Corporation | Proteasome inhibitors |
| CN113956183B (zh) * | 2021-10-28 | 2023-06-20 | 成都市科隆化学品有限公司 | 一种Boc-Ser(Bzl)-OH及其制备方法 |
| WO2024230583A1 (zh) * | 2023-05-05 | 2024-11-14 | 上海济煜医药科技有限公司 | 一种短肽类化合物及其制备方法和医药应用 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3432307A1 (de) * | 1984-09-03 | 1986-04-10 | Boehringer Ingelheim KG, 6507 Ingelheim | Aminosaeurederivate, verfahren zu ihrer herstellung und pharmazeutische zusammensetzungen |
| AU6733190A (en) | 1989-11-27 | 1991-06-26 | Santen Pharmaceutical Co. Ltd. | Amino acid derivative |
| FR2679564A1 (fr) | 1991-07-23 | 1993-01-29 | Inst Nat Sante Rech Med | Nouveaux acylmercaptoalcanoldipeptides, leur preparation et les compositions qui les contiennent. |
| ATE159515T1 (de) | 1992-07-21 | 1997-11-15 | Ciba Geigy Ag | Oxamidsäure-derivate als hypocholesterämische mittel |
| US5432186A (en) * | 1993-11-16 | 1995-07-11 | Ciba-Geigy Corporation | Cyclic amino acid derivatives |
| US5508266A (en) | 1994-06-22 | 1996-04-16 | Ciba-Geigy Corporation | Gem-disubstituted amino acid derivatives |
| EP0820464A2 (en) | 1995-03-31 | 1998-01-28 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
| US6147114A (en) * | 1995-04-25 | 2000-11-14 | Fuji Yakuhin Kogyo Kabushiki Kaisha | Highly water-soluble metalloproteinase inhibitors |
| DE69627483T2 (de) | 1995-05-10 | 2004-04-01 | Darwin Discovery Ltd., Slough | Peptidartige stoffe, die metalloproteinasen und die tnf-freisetzung hemmen, und ihre therapeutische verwendung |
| WO1996040726A1 (en) * | 1995-06-07 | 1996-12-19 | Genta Incorporated | Novel carbamate-based cationic lipids |
| US6245809B1 (en) * | 1996-12-09 | 2001-06-12 | Cor Therapeutics Inc. | Integrin antagonists |
| US6492421B1 (en) * | 1997-07-31 | 2002-12-10 | Athena Neurosciences, Inc. | Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4 |
| DE19745151A1 (de) | 1997-10-14 | 1999-04-15 | Basf Ag | Neue Verbindungen zur Behandlung von Krankheiten, die mit der biologischen Wirkung von Endothelin assoziiert sind |
| FR2770844A1 (fr) | 1997-11-10 | 1999-05-14 | Inst Nat Sante Rech Med | Inhibiteurs de toxines clostridiales et compositions pharmaceutiques les contenant |
| CA2309792A1 (en) * | 1997-11-12 | 1999-05-20 | William C. Shakespeare | Novel signal transduction inhibitors, compositions containing them |
| BR9909805A (pt) | 1998-04-23 | 2000-12-26 | Novartis Ag | Certos inibidores de tiol de enzima de conversão de endotelina |
| WO1999055723A1 (en) | 1998-04-23 | 1999-11-04 | Novartis Ag | Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme |
| AU1719700A (en) | 1998-12-31 | 2000-07-24 | Aventis Pharmaceuticals Inc. | Selective inhibitors of mmp-12 |
| FR2788526B1 (fr) | 1999-01-20 | 2002-07-05 | Inst Nat Sante Rech Med | Composes tripeptidiques utiles a titre d'hinhibiteurs selectifs de l'aminopeptidase a et compositions pharmaceutiques correspondantes |
| CO5160290A1 (es) | 1999-03-29 | 2002-05-30 | Novartis Ag | Derivados de acido fenoxifeniloxamico sustituido . |
| US6503949B1 (en) * | 1999-05-17 | 2003-01-07 | Noro Nordisk A/S | Glucagon antagonists/inverse agonists |
| GB9917909D0 (en) * | 1999-07-31 | 1999-09-29 | Synphar Lab Inc | Cysteine protease inhibitors |
| DE60040397D1 (de) * | 1999-08-27 | 2008-11-13 | Cytovia Inc | Substituierte alpha-hydroxy-säuren als caspase-hemmer und ihre verwendung |
| US6803383B2 (en) * | 2000-03-27 | 2004-10-12 | The Scripps Research Institute | Inhibition of angiogenesis and tumor growth |
| AU2001287289A1 (en) | 2000-04-03 | 2001-10-15 | Bristol-Myers Squibb Company | Vasopeptidase inhibitors to treat isolated systolic hypertensions |
| IL152081A0 (en) | 2000-04-12 | 2003-05-29 | Novartis Ag | Novel medical use of aldosterone synthase inhibitors alone or in combination with at1-receptor antagonists |
| US20020013307A1 (en) | 2000-05-23 | 2002-01-31 | Pablo Lapuerta | Use of vasopeptidase inhibitors to treat or slow the progression of cognitive dysfunction and to treat and/or prevent dementia |
| US6777443B2 (en) * | 2001-05-15 | 2004-08-17 | Novartis Ag | Dipeptide derivatives |
-
2002
- 2002-05-09 US US10/142,693 patent/US6777443B2/en not_active Expired - Fee Related
- 2002-05-13 AR ARP020101736A patent/AR035890A1/es unknown
- 2002-05-14 SK SK1403-2003A patent/SK14032003A3/sk not_active Application Discontinuation
- 2002-05-14 NZ NZ529438A patent/NZ529438A/en unknown
- 2002-05-14 KR KR1020037014849A patent/KR100908152B1/ko not_active Expired - Fee Related
- 2002-05-14 AU AU2002314067A patent/AU2002314067B2/en not_active Ceased
- 2002-05-14 CZ CZ20033077A patent/CZ20033077A3/cs unknown
- 2002-05-14 MY MYPI20021740A patent/MY127495A/en unknown
- 2002-05-14 TW TW091110028A patent/TWI295996B/zh not_active IP Right Cessation
- 2002-05-14 HU HU0304084A patent/HUP0304084A3/hu unknown
- 2002-05-14 CN CNA028118499A patent/CN1649893A/zh active Pending
- 2002-05-14 RU RU2003134153/04A patent/RU2298559C2/ru not_active IP Right Cessation
- 2002-05-14 WO PCT/EP2002/005293 patent/WO2002092622A2/en not_active Ceased
- 2002-05-14 PL PL02366786A patent/PL366786A1/xx unknown
- 2002-05-14 JP JP2002589505A patent/JP4390458B2/ja not_active Expired - Fee Related
- 2002-05-14 EP EP02740600A patent/EP1392720A2/en not_active Withdrawn
- 2002-05-14 BR BR0209652-8A patent/BR0209652A/pt not_active IP Right Cessation
- 2002-05-14 MX MXPA03010403A patent/MXPA03010403A/es active IP Right Grant
- 2002-05-14 EP EP10164769A patent/EP2239268A1/en not_active Withdrawn
- 2002-05-14 CA CA002449292A patent/CA2449292A1/en not_active Abandoned
- 2002-05-14 IL IL15877202A patent/IL158772A0/xx unknown
- 2002-05-15 PE PE2002000407A patent/PE20030042A1/es not_active Application Discontinuation
-
2003
- 2003-11-14 NO NO20035084A patent/NO20035084L/no not_active Application Discontinuation
- 2003-12-02 CO CO03105928A patent/CO5540347A2/es not_active Application Discontinuation
-
2004
- 2004-07-02 US US10/884,150 patent/US6992105B2/en not_active Expired - Fee Related
-
2005
- 2005-10-21 US US11/255,827 patent/US20060058242A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2005504011A5 (enExample) | ||
| US5965692A (en) | Prodrugs of thrombin inhibitors | |
| EP0012845B1 (en) | Tetrahydroisoquinoline compounds, process for preparing same and pharmaceutical compositions containing them | |
| EP2125695B1 (en) | Nitric oxide donor compounds | |
| US5801274A (en) | N- mercaptoacyl(amino acid or peptide)! compounds and S-lipophilic aliphatic carbonyl derivatives thereof as antihypertensives | |
| RU2306309C2 (ru) | Производное 8-азапростагландина, фармацевтическая композиция, агент для профилактики заболеваний | |
| PT640617E (pt) | Compostos azepino-(2,1-a)-isoquinolina substituidos | |
| PT701568E (pt) | Novos derivados de peptidos | |
| JP2002528495A (ja) | ニトロソ化およびニトロシル化された非ステロイド抗炎症性化合物、組成物および使用方法 | |
| SK63194A3 (en) | Peptide derivatives | |
| JPS6121226B2 (enExample) | ||
| PT89346B (pt) | Processo para a preparacao de novas lactamas triciclicas contendo grupos sulfridilo e de composicoes farmaceuticas que as contem | |
| ES2901401T3 (es) | Compuesto de dihidropirimidina y método de preparación y uso del mismo | |
| IL127325A (en) | History of amino acids, process for their preparation, pharmaceutical preparations containing them and their uses in the preparation of drugs as thrombin inhibitors | |
| PT669936E (pt) | Derivados de lactama biciclica de mercaptoacetilamida uteis como inibidores de encefalinase e de ace | |
| ES2394622T3 (es) | Gamma-lactamas sustituidas como agente terapéutico | |
| JPH08508720A (ja) | ピロールーアミジン化合物およびその薬剤的に受容できる塩、その製造法ならびにこれを含む医薬組成物 | |
| US4310517A (en) | Tumor-resolving and histolytic medicaments and their use | |
| JPS6323897A (ja) | タフトシン類似体、その製法及び医薬組成物 | |
| PT1369419E (pt) | Composto de n-fenilarilsulfonamida, fármaco contendo o composto como ingrediente activo, produtos intermédios para a produção do composto e processos para a produção do composto | |
| PT747392E (pt) | Inibidores de accao dupla que contem 1,2-diazepina | |
| WO2006043655A1 (ja) | 吸入用医薬組成物 | |
| JPH05222005A (ja) | ３（ｓ）−アミノ−４−シクロヘキシル−２（ｒ）−ヒドロキシ酪酸若しくは４−シクロヘキシル−（２ｒ，３ｓ）−ジヒドロキシ酪酸又は関連類似体を含む環状レニン阻害剤 | |
| JPH08319284A (ja) | アシルグアニジンおよびアミジンプロドラッグ | |
| US4840936A (en) | Pharmaceutically useful derivatives of thiazolidine-4-carboxylic acid |