JP2004503538A5 - - Google Patents
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- Publication number
- JP2004503538A5 JP2004503538A5 JP2002510448A JP2002510448A JP2004503538A5 JP 2004503538 A5 JP2004503538 A5 JP 2004503538A5 JP 2002510448 A JP2002510448 A JP 2002510448A JP 2002510448 A JP2002510448 A JP 2002510448A JP 2004503538 A5 JP2004503538 A5 JP 2004503538A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- alkanoyl
- compound according
- conh
- 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
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- -1 amino, hydroxy, aminomethyl Chemical group 0.000 description 67
- 150000001875 compounds Chemical class 0.000 description 30
- 125000001589 carboacyl group Chemical group 0.000 description 24
- 229910052739 hydrogen Inorganic materials 0.000 description 21
- 239000001257 hydrogen Substances 0.000 description 21
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 20
- 125000005236 alkanoylamino group Chemical group 0.000 description 17
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 14
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 12
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 description 9
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 description 9
- 125000004093 cyano group Chemical group *C#N 0.000 description 9
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 description 8
- 125000000217 alkyl group Chemical group 0.000 description 8
- 150000002431 hydrogen Chemical class 0.000 description 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 8
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 description 7
- 125000002883 imidazolyl group Chemical group 0.000 description 7
- 125000003396 thiol group Chemical class [H]S* 0.000 description 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 6
- 125000004414 alkyl thio group Chemical group 0.000 description 6
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 6
- 125000005843 halogen group Chemical group 0.000 description 6
- 125000000335 thiazolyl group Chemical group 0.000 description 6
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 description 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 description 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 5
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 description 5
- 125000004076 pyridyl group Chemical group 0.000 description 5
- 125000005422 alkyl sulfonamido group Chemical group 0.000 description 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 4
- 125000002837 carbocyclic group Chemical group 0.000 description 4
- 125000000623 heterocyclic group Chemical group 0.000 description 4
- 125000001624 naphthyl group Chemical group 0.000 description 4
- 125000001544 thienyl group Chemical group 0.000 description 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 description 3
- 0 *C(**c1cc(C(*=CC2=CI2)N)ccc1*)I* Chemical compound *C(**c1cc(C(*=CC2=CI2)N)ccc1*)I* 0.000 description 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 3
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 description 3
- 125000004647 alkyl sulfenyl group Chemical group 0.000 description 3
- 125000000304 alkynyl group Chemical group 0.000 description 3
- 125000000753 cycloalkyl group Chemical group 0.000 description 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 3
- 125000002140 imidazol-4-yl group Chemical group [H]N1C([H])=NC([*])=C1[H] 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- 125000002971 oxazolyl group Chemical group 0.000 description 3
- 229910052760 oxygen Inorganic materials 0.000 description 3
- 125000003386 piperidinyl group Chemical group 0.000 description 3
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 description 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 2
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 description 2
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 2
- 125000004423 acyloxy group Chemical group 0.000 description 2
- 125000003368 amide group Chemical group 0.000 description 2
- 125000000539 amino acid group Chemical group 0.000 description 2
- 125000005605 benzo group Chemical group 0.000 description 2
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 2
- 125000001309 chloro group Chemical group Cl* 0.000 description 2
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 125000006125 ethylsulfonyl group Chemical group 0.000 description 2
- 125000002541 furyl group Chemical group 0.000 description 2
- 125000001188 haloalkyl group Chemical group 0.000 description 2
- 125000004531 indol-5-yl group Chemical group [H]N1C([H])=C([H])C2=C([H])C(*)=C([H])C([H])=C12 0.000 description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 description 2
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 description 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 description 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 description 2
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 2
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 description 2
- 125000004944 pyrazin-3-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 description 1
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 description 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 description 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 1
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 description 1
- 125000004861 4-isopropyl phenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 description 1
- 150000007650 D alpha amino acids Chemical class 0.000 description 1
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 125000005092 alkenyloxycarbonyl group Chemical group 0.000 description 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 description 1
- 125000004422 alkyl sulphonamide group Chemical group 0.000 description 1
- 125000004103 aminoalkyl group Chemical group 0.000 description 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 description 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 125000006263 dimethyl aminosulfonyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])S(*)(=O)=O 0.000 description 1
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- ZCRZCMUDOWDGOB-UHFFFAOYSA-N ethanesulfonimidic acid Chemical compound CCS(N)(=O)=O ZCRZCMUDOWDGOB-UHFFFAOYSA-N 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 125000006627 ethoxycarbonylamino group Chemical group 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 125000000350 glycoloyl group Chemical group O=C([*])C([H])([H])O[H] 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 description 1
- HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 description 1
- 125000006626 methoxycarbonylamino group Chemical group 0.000 description 1
- 125000006533 methyl amino methyl group Chemical group [H]N(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000006261 methyl amino sulfonyl group Chemical group [H]N(C([H])([H])[H])S(*)(=O)=O 0.000 description 1
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 description 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 description 1
- 125000003145 oxazol-4-yl group Chemical group O1C=NC(=C1)* 0.000 description 1
- 125000004304 oxazol-5-yl group Chemical group O1C=NC=C1* 0.000 description 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 description 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 125000002072 seryl group Chemical group 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 description 1
- 125000004496 thiazol-5-yl group Chemical group S1C=NC=C1* 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/GB2000/002291 WO2000077027A2 (en) | 1999-06-14 | 2000-06-13 | Serine protease inhibitors |
| PCT/GB2000/004764 WO2001044226A1 (en) | 1999-12-14 | 2000-12-13 | Serine protease inhibitors |
| PCT/GB2001/002566 WO2001096305A1 (en) | 2000-06-13 | 2001-06-12 | Serine protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004503538A JP2004503538A (ja) | 2004-02-05 |
| JP2004503538A5 true JP2004503538A5 (enExample) | 2009-03-12 |
Family
ID=26243532
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002510448A Pending JP2004503538A (ja) | 2000-06-13 | 2001-06-12 | セリンプロテアーゼインヒビター |
Country Status (4)
| Country | Link |
|---|---|
| JP (1) | JP2004503538A (enExample) |
| AU (2) | AU2001264077B2 (enExample) |
| DE (1) | DE60124397T2 (enExample) |
| WO (1) | WO2001096305A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0114185D0 (en) * | 2001-06-12 | 2001-08-01 | Protherics Molecular Design Lt | Compounds |
| US20050085531A1 (en) * | 2003-10-03 | 2005-04-21 | Hodge Carl N. | Thiophene-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof |
| WO2017078656A1 (en) * | 2015-11-05 | 2017-05-11 | Intel IP Corporation | Synchronization signals for license assisted access |
| BR112020001065A2 (pt) * | 2017-08-10 | 2020-07-14 | Panasonic Intellectual Property Corporation Of America | equipamento do usuário, estação base e método de comunicação sem fio |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20000005312A (ko) * | 1996-04-10 | 2000-01-25 | 오노 야꾸힝 고교 가부시키가이샤 | 트립타아제 억제제 및 신규 구아니디노 유도체 |
| DE69830410T2 (de) * | 1997-08-29 | 2006-01-26 | Tularik Ltd. | Meta-benzamidinderivate als serinprotease-inhibitoren |
| AU1176299A (en) * | 1997-11-26 | 1999-06-15 | Yoshitomi Pharmaceutical Industries, Ltd. | Tryptase inhibitors comprising heterocyclic amide compounds |
| AU3620099A (en) * | 1998-04-24 | 1999-11-16 | Proteus Molecular Design Limited | Aminomethyl-benzoic ester derivatives as tryptase inhibitors |
| WO2000076970A2 (en) * | 1999-06-14 | 2000-12-21 | Eli Lilly And Company | Serine protease inhibitors |
| EP1192132B1 (en) * | 1999-06-14 | 2005-09-07 | Eli Lilly And Company | Serine protease inhibitors |
| GB9929552D0 (en) * | 1999-12-14 | 2000-02-09 | Proteus Molecular Design | Compounds |
| GB0030303D0 (en) * | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
| GB0030304D0 (en) * | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
-
2001
- 2001-06-12 AU AU2001264077A patent/AU2001264077B2/en not_active Ceased
- 2001-06-12 JP JP2002510448A patent/JP2004503538A/ja active Pending
- 2001-06-12 WO PCT/GB2001/002566 patent/WO2001096305A1/en not_active Ceased
- 2001-06-12 DE DE60124397T patent/DE60124397T2/de not_active Expired - Lifetime
- 2001-06-12 AU AU6407701A patent/AU6407701A/xx active Pending
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