JP2004536858A5 - - Google Patents
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- 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- Withdrawn
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- -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 (cg-RX-API-DMAC7.html) | 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 (cg-RX-API-DMAC7.html) |
| EP (1) | EP1411948A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2004536858A (cg-RX-API-DMAC7.html) |
| CA (1) | CA2454007A1 (cg-RX-API-DMAC7.html) |
| DE (1) | DE10134721A1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2003007958A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2483573A1 (en) | 2002-05-03 | 2003-11-13 | Elan Pharmaceuticals, Inc. | Sulfonylquinoxalone acetamide derivatives and related compounds as bradykinin antagonists |
| JP2006505553A (ja) * | 2002-10-10 | 2006-02-16 | エラン ファーマシューティカルズ，インコーポレイテッド | ブラジキニン拮抗薬としてのスルホニルベンゾジアゼピノンアセトアミド |
| 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 |
| EP1633348B1 (en) | 2003-05-02 | 2008-10-08 | Elan Pharmaceuticals, Inc. | 4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE - 3 - CARBOXYLIC ACID AMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B sb 1 /sb RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES |
| EP1644347A1 (en) * | 2003-06-20 | 2006-04-12 | Arena Pharmaceuticals, Inc. | N-PHENYL-PIPERAZINE DERIVATIVES AND METHODS OF PROPHYLAXIS OR TREATMENT OF 5HT sb 2C /sb RECEPTOR ASSOCIATED DISEASES |
| MXPA05013469A (es) * | 2003-06-20 | 2006-03-09 | Amgen Inc | Derivados de piperazina y metodos de uso. |
| EP1878728A3 (en) * | 2003-06-20 | 2008-01-30 | Amgen Inc. | Derivatives of piperazine and higher homologues thereof for the treatment of inflammation-related disorders |
| MXPA06001482A (es) * | 2003-08-08 | 2006-09-04 | Johnson & Johnson | Procedimiento para la preparacion de compuestos de 2-(quinoxalin-5-ilsulfonilamino)-benzamida. |
| AU2005275036A1 (en) | 2004-07-15 | 2006-02-23 | Amgen Inc. | 1,2,3,4-tetrahydropyrazin-2-yl acetamides and their use as bradykinin antagonists for the treatment of inflammation related disorders |
| US20090069363A1 (en) * | 2004-12-14 | 2009-03-12 | Shionogi & Co. Ltd. A Legal Entity Of Japan | Therapeutic Agent for Constipation |
| WO2007067629A1 (en) * | 2005-12-07 | 2007-06-14 | Amgen Inc. | Bradykinin 1 receptor antagonists |
| MX2010007418A (es) | 2008-01-04 | 2010-11-12 | Intellikine Inc | Ciertas entidades quimicas, composiciones y metodos. |
| 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 |
| EP2663309B1 (en) | 2011-01-10 | 2017-03-15 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
| 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 |
| MX375194B (es) | 2012-11-01 | 2025-03-06 | Infinity Pharmaceuticals Inc | Tratamiento de cánceres utilizando moduladores de las isoformas de pi3 cinasa. |
| SI2813502T1 (sl) | 2013-06-14 | 2017-05-31 | Dompe Farmaceutici S.P.A. | Antagonisti receptorja za bradikinin in farmacevtski sestavki, ki jih vsebujejo |
| US20150320755A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| CN109640999A (zh) | 2016-06-24 | 2019-04-16 | 无限药品股份有限公司 | 组合疗法 |
| KR20230159419A (ko) | 2021-02-19 | 2023-11-21 | 수도 바이오사이언시즈 리미티드 | Tyk2 억제제 및 이의 용도 |
| MX2023009685A (es) | 2021-02-19 | 2023-10-30 | Sudo Biosciences Ltd | Inhibidores de tyk2 y sus usos. |
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 |
| DE59209965D1 (de) * | 1991-04-15 | 2002-10-17 | Aventis Pharma Gmbh | Chinoxaline, Verfahren zu ihrer Herstellung und ihre Verwendung |
| DE19712960A1 (de) * | 1997-03-27 | 1998-10-01 | Hoechst Ag | Benzyloxy-substituierte, anellierte N-Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Bradykininrezeptorantagonisten |
| CA2483573A1 (en) * | 2002-05-03 | 2003-11-13 | 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 EP EP02762319A patent/EP1411948A1/de not_active Withdrawn
- 2002-07-04 JP JP2003513565A patent/JP2004536858A/ja not_active Withdrawn
- 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 WO PCT/EP2002/007416 patent/WO2003007958A1/de not_active Ceased