JP2004536858A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2004536858A5 JP2004536858A5 JP2003513565A JP2003513565A JP2004536858A5 JP 2004536858 A5 JP2004536858 A5 JP 2004536858A5 JP 2003513565 A JP2003513565 A JP 2003513565A JP 2003513565 A JP2003513565 A JP 2003513565A JP 2004536858 A5 JP2004536858 A5 JP 2004536858A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- same
- halogen
- different
- phenyl
- 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- Withdrawn
Links
- -1 trifluoromethoxy, hydroxyl Chemical group 0.000 claims description 44
- 229910052736 halogen Inorganic materials 0.000 claims description 42
- 150000002367 halogens Chemical class 0.000 claims description 42
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 33
- 239000001257 hydrogen Substances 0.000 claims description 32
- 229910052739 hydrogen Inorganic materials 0.000 claims description 32
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 30
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 25
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 23
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 19
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 16
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 16
- 150000001875 compounds Chemical class 0.000 claims description 13
- 150000002431 hydrogen Chemical class 0.000 claims description 13
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 12
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 12
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 11
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 10
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 9
- 125000003118 aryl group Chemical group 0.000 claims description 9
- 125000000383 tetramethylene group Chemical group [H]C([H])([*:1])C([H])([H])C([H])([H])C([H])([H])[*:2] 0.000 claims description 9
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 7
- 239000012453 solvate Substances 0.000 claims description 7
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 6
- 125000003258 trimethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])[*:1] 0.000 claims description 6
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 125000003627 8 membered carbocyclic group Chemical group 0.000 claims description 4
- 125000000753 cycloalkyl group 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
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical group [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims description 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 3
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 125000000217 alkyl group Chemical group 0.000 claims description 3
- 229910052731 fluorine Inorganic materials 0.000 claims description 3
- 239000011737 fluorine Substances 0.000 claims description 3
- 125000001153 fluoro group Chemical group F* 0.000 claims description 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 4
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 3
- LSBDFXRDZJMBSC-UHFFFAOYSA-N 2-phenylacetamide Chemical compound NC(=O)CC1=CC=CC=C1 LSBDFXRDZJMBSC-UHFFFAOYSA-N 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 230000003796 beauty Effects 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 239000012442 inert solvent Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- KPSNUSOPDYSRSV-UHFFFAOYSA-N 2-[1-(benzenesulfonyl)-3-oxo-2,4-dihydroquinoxalin-2-yl]-n-phenylacetamide Chemical compound C=1C=CC=CC=1NC(=O)CC(C(NC1=CC=CC=C11)=O)N1S(=O)(=O)C1=CC=CC=C1 KPSNUSOPDYSRSV-UHFFFAOYSA-N 0.000 description 4
- 150000004677 hydrates Chemical class 0.000 description 3
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 2
- 239000005977 Ethylene Substances 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 description 1
- 125000003884 phenylalkyl group Chemical group 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10134721A DE10134721A1 (de) | 2001-07-17 | 2001-07-17 | Tetrahydrochinoxaline |
| PCT/EP2002/007416 WO2003007958A1 (de) | 2001-07-17 | 2002-07-04 | Tetrahydrochinoxaline als bradykininantagonisten |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004536858A JP2004536858A (ja) | 2004-12-09 |
| JP2004536858A5 true JP2004536858A5 (enExample) | 2006-01-05 |
Family
ID=7692082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003513565A Withdrawn JP2004536858A (ja) | 2001-07-17 | 2002-07-04 | テトラヒドロキノキサリン類 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20040235849A1 (enExample) |
| EP (1) | EP1411948A1 (enExample) |
| JP (1) | JP2004536858A (enExample) |
| CA (1) | CA2454007A1 (enExample) |
| DE (1) | DE10134721A1 (enExample) |
| WO (1) | WO2003007958A1 (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003228825A1 (en) * | 2002-05-03 | 2003-11-17 | Elan Pharmaceuticals, Inc. | Sulfonylquinoxalone acetamide derivatives and related compounds as bradykinin antagonists |
| EP1549622A1 (en) * | 2002-10-10 | 2005-07-06 | Elian Pharmaceuticals Inc. | Sulfonylbenzodiazepinone acetamides as bradykinin antagonists |
| US6908921B2 (en) | 2002-12-13 | 2005-06-21 | Merck & Co., Inc. | Quinoxalinone derivatives as bradykinin B1 antagonists |
| CA2522084A1 (en) | 2003-04-10 | 2004-10-28 | Amgen Inc. | Cyclic amine derivatives and their use in the treatment of inflammation-related disorders mediated by bradykinin |
| DE602004016992D1 (de) | 2003-05-02 | 2008-11-20 | Elan Pharm Inc | 4-bromo-5-(2-chloro-benzoylamino)-1h-pyrazol-3-carbonsäureamid-derivate und verwandte verbindungen als bradykinin b1 rezeptor antagonisten zur behandlung von entzündlichen erkrankungen |
| WO2005061467A2 (en) | 2003-06-20 | 2005-07-07 | Amgen Inc. | Piperazine derivatives as bradykinin antagonists |
| EP1878728A3 (en) * | 2003-06-20 | 2008-01-30 | Amgen Inc. | Derivatives of piperazine and higher homologues thereof for the treatment of inflammation-related disorders |
| US20070179155A1 (en) * | 2003-06-20 | 2007-08-02 | Brian Smith | N-phenyl-piperazine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases |
| CA2534887A1 (en) * | 2003-08-08 | 2005-02-24 | Janssen Pharmaceutica, N.V. | Process for the preparation of 2- (quinoxalin-5-ylsulfonylamino) -benzamide compounds |
| US7662811B2 (en) | 2004-07-15 | 2010-02-16 | Amgen Inc. | 1,2,3,4-tetrahydropyrazin-2-yl acetamides and methods of use |
| JPWO2006064780A1 (ja) * | 2004-12-14 | 2008-06-12 | 塩野義製薬株式会社 | 便秘治療剤 |
| AU2006321919A1 (en) * | 2005-12-07 | 2007-06-14 | Amgen Inc. | Bradykinin 1 receptor antagonists |
| MX358640B (es) | 2008-01-04 | 2018-08-29 | Intellikine Llc | Isoquinolin-1 (2h) -onas y tieno [2,3-d]pirimidin-4(3h) -onas substituidas, y metodos de uso de las mismas. |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| EP2316820A1 (en) | 2009-10-28 | 2011-05-04 | Dompe S.p.A. | 2-aryl-propionamide derivatives useful as bradykinin receptor antagonists and pharmaceutical compositions containing them |
| TWI546305B (zh) | 2011-01-10 | 2016-08-21 | 英菲尼提製藥股份有限公司 | 製備異喹啉酮之方法及異喹啉酮之固體形式 |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| EP2895204B1 (en) * | 2012-09-13 | 2020-10-21 | Provincial Health Services Authority | Compositions targeting bradykinin receptor b1 for medical imaging of cancer and other disorders |
| CN105102000B (zh) | 2012-11-01 | 2021-10-22 | 无限药品公司 | 使用pi3激酶亚型调节剂的癌症疗法 |
| EP2813502B1 (en) | 2013-06-14 | 2017-01-04 | Dompé farmaceutici s.p.a. | Bradykinin receptor antagonists and pharmaceutical compositions containing them |
| WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| EP3474856B1 (en) | 2016-06-24 | 2022-09-14 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| EP4294808A1 (en) | 2021-02-19 | 2023-12-27 | Sudo Biosciences Limited | Tyk2 inhibitors and uses thereof |
| JP2024508794A (ja) | 2021-02-19 | 2024-02-28 | スドー バイオサイエンシーズ リミテッド | Ｔｙｋ２阻害剤およびその使用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3247196A (en) * | 1962-06-21 | 1966-04-19 | Ciba Geigy Corp | Nuomega-derivatives of 7-(nu-amino-adipoylamino)-cephalosporanic acid |
| US3635971A (en) * | 1970-06-18 | 1972-01-18 | Abbott Lab | 3 (3 4-dihydro-3-oxo-2-quinoxalinyl) propionamides |
| DK0509398T3 (da) * | 1991-04-15 | 2002-01-14 | Aventis Pharma Gmbh | Quinoxaliner, fremgangsmåder til deres fremstilling samt deres anvendelse |
| DE19712960A1 (de) * | 1997-03-27 | 1998-10-01 | Hoechst Ag | Benzyloxy-substituierte, anellierte N-Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Bradykininrezeptorantagonisten |
| AU2003228825A1 (en) * | 2002-05-03 | 2003-11-17 | Elan Pharmaceuticals, Inc. | Sulfonylquinoxalone acetamide derivatives and related compounds as bradykinin antagonists |
-
2001
- 2001-07-17 DE DE10134721A patent/DE10134721A1/de not_active Withdrawn
-
2002
- 2002-07-04 WO PCT/EP2002/007416 patent/WO2003007958A1/de not_active Ceased
- 2002-07-04 CA CA002454007A patent/CA2454007A1/en not_active Abandoned
- 2002-07-04 US US10/483,464 patent/US20040235849A1/en not_active Abandoned
- 2002-07-04 EP EP02762319A patent/EP1411948A1/de not_active Withdrawn
- 2002-07-04 JP JP2003513565A patent/JP2004536858A/ja not_active Withdrawn