JP2005530753A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2005530753A5 JP2005530753A5 JP2004501384A JP2004501384A JP2005530753A5 JP 2005530753 A5 JP2005530753 A5 JP 2005530753A5 JP 2004501384 A JP2004501384 A JP 2004501384A JP 2004501384 A JP2004501384 A JP 2004501384A JP 2005530753 A5 JP2005530753 A5 JP 2005530753A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- chloro
- eth
- ylcarbonyl
- oxo
- 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
- -1 amino, substituted amino Chemical group 0.000 claims 321
- 125000000623 heterocyclic group Chemical group 0.000 claims 161
- 125000001072 heteroaryl group Chemical group 0.000 claims 144
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 126
- 125000003118 aryl group Chemical group 0.000 claims 75
- 229910052739 hydrogen Inorganic materials 0.000 claims 68
- 239000001257 hydrogen Substances 0.000 claims 68
- 150000002431 hydrogen Chemical class 0.000 claims 65
- 125000003107 substituted aryl group Chemical group 0.000 claims 57
- 125000000753 cycloalkyl group Chemical group 0.000 claims 49
- 125000000217 alkyl group Chemical group 0.000 claims 46
- 125000000547 substituted alkyl group Chemical group 0.000 claims 46
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 45
- 125000002947 alkylene group Chemical group 0.000 claims 44
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 42
- 150000001875 compounds Chemical class 0.000 claims 41
- 125000003342 alkenyl group Chemical group 0.000 claims 33
- 229910052757 nitrogen Inorganic materials 0.000 claims 33
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 33
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 27
- 125000000304 alkynyl group Chemical group 0.000 claims 25
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 25
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 23
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 21
- 125000002252 acyl group Chemical group 0.000 claims 15
- 125000004423 acyloxy group Chemical group 0.000 claims 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 14
- 241000124008 Mammalia Species 0.000 claims 11
- 125000004104 aryloxy group Chemical group 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 10
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 10
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 101800004538 Bradykinin Proteins 0.000 claims 7
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 claims 7
- 102100035792 Kininogen-1 Human genes 0.000 claims 7
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 claims 7
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 6
- 208000024891 symptom Diseases 0.000 claims 6
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims 5
- 230000002411 adverse Effects 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 4
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 4
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 3
- 125000004574 piperidin-2-yl group Chemical group N1C(CCCC1)* 0.000 claims 3
- FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 2
- 208000004454 Hyperalgesia Diseases 0.000 claims 2
- 208000035154 Hyperesthesia Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- 208000001738 Nervous System Trauma Diseases 0.000 claims 2
- 206010030113 Oedema Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 208000005107 Premature Birth Diseases 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 230000002977 hyperthermial effect Effects 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000006357 methylene carbonyl group Chemical group [H]C([H])([*:1])C([*:2])=O 0.000 claims 2
- 206010027599 migraine Diseases 0.000 claims 2
- 208000028412 nervous system injury Diseases 0.000 claims 2
- 206010039083 rhinitis Diseases 0.000 claims 2
- 230000028327 secretion Effects 0.000 claims 2
- 230000035939 shock Effects 0.000 claims 2
- AUFIRGPROMANKW-UHFFFAOYSA-N 1-methyl-3,6-dihydro-2h-pyridine Chemical compound CN1CCC=CC1 AUFIRGPROMANKW-UHFFFAOYSA-N 0.000 claims 1
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 1
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 208000008035 Back Pain Diseases 0.000 claims 1
- 101100513046 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) eth-1 gene Proteins 0.000 claims 1
- 206010036590 Premature baby Diseases 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004212 difluorophenyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
- 125000004283 imidazolin-2-yl group Chemical group [H]N1C(*)=NC([H])([H])C1([H])[H] 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 0 CC1(CC2=CC(C)(C)C=CC=C2*(C(**)C(*)NC)S(*)(=O)=O)*C1 Chemical compound CC1(CC2=CC(C)(C)C=CC=C2*(C(**)C(*)NC)S(*)(=O)=O)*C1 0.000 description 7
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37820602P | 2002-05-03 | 2002-05-03 | |
| PCT/US2003/013805 WO2003093245A1 (en) | 2002-05-03 | 2003-05-02 | Sulfonylquinoxalone acetamide derivatives and related compounds as bradykinin antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005530753A JP2005530753A (ja) | 2005-10-13 |
| JP2005530753A5 true JP2005530753A5 (enExample) | 2006-06-22 |
Family
ID=29401593
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004501384A Pending JP2005530753A (ja) | 2002-05-03 | 2003-05-02 | ブラジキニンアンタゴニストとしてのスルホニルキノキサロンアセトアミド誘導体および関連化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US7056937B2 (enExample) |
| EP (1) | EP1501807A1 (enExample) |
| JP (1) | JP2005530753A (enExample) |
| AU (1) | AU2003228825A1 (enExample) |
| CA (1) | CA2483573A1 (enExample) |
| WO (1) | WO2003093245A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10134721A1 (de) * | 2001-07-17 | 2003-02-06 | Bayer Ag | Tetrahydrochinoxaline |
| CA2483573A1 (en) * | 2002-05-03 | 2003-11-13 | Elan Pharmaceuticals, Inc. | Sulfonylquinoxalone acetamide derivatives and related compounds as bradykinin antagonists |
| CA2501801A1 (en) | 2002-10-10 | 2004-04-22 | Elan Pharmaceuticals, Inc. | Sulfonylbenzodiazepinone acetamides as bradykinin antagonists |
| US6908921B2 (en) * | 2002-12-13 | 2005-06-21 | Merck & Co., Inc. | Quinoxalinone derivatives as bradykinin B1 antagonists |
| US20050020591A1 (en) * | 2002-12-13 | 2005-01-27 | Dai-Shi Su | 2-Quinoxalinone derivatives as bradykinin antagonists and novel compounds |
| EP1572678A4 (en) * | 2002-12-19 | 2008-05-07 | Elan Pharm Inc | SUBSTITUTED N-PHENYL SULPHONAMIDES ALSBRADYKININ ANTAGONISTS |
| US7504423B2 (en) * | 2003-12-11 | 2009-03-17 | Mitsubishi Tanabe Pharma Corporation | α-amino acid derivatives and use thereof as medicines |
| CA2567343A1 (en) * | 2004-05-20 | 2005-12-01 | Elan Pharmaceuticals, Inc. | N-cyclic sulfonamido inhibitors of gamma secretase |
| US7351709B2 (en) * | 2004-06-09 | 2008-04-01 | Wyeth | Estrogen receptor ligands |
| 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 |
| US20070249690A1 (en) * | 2004-07-23 | 2007-10-25 | Darren Mansfield | N-[2-(4-Pyridinyl)Ethyl]Benzamide Derivatives as Fungicides |
| DE102005013967A1 (de) * | 2004-11-05 | 2006-10-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Bradykinin-B1-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel |
| US7563793B2 (en) * | 2004-12-20 | 2009-07-21 | Wyeth | Pyrrolo[1,2-a]quinoxalin-5-(4H)-yl)sulfonyls and carbonyls and their use as estrogenic agents |
| WO2007067629A1 (en) * | 2005-12-07 | 2007-06-14 | Amgen Inc. | Bradykinin 1 receptor antagonists |
| HU230518B1 (hu) * | 2005-12-20 | 2016-10-28 | Richter Gedeon Nyrt. | Bradykinin B1 receptor szelektív antagonista hatással rendelkező új fenatridin származékok, eljárás előállításukra, és az ezeket tartalmazó gyógyszerkészítmények |
| HUP0600808A3 (en) | 2006-10-27 | 2008-09-29 | Richter Gedeon Nyrt | New benzamide derivatives as bradykinin antagonists, process for their preparation and pharmaceutical compositions containing them |
| 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 |
| WO2012162291A1 (en) * | 2011-05-24 | 2012-11-29 | The Wistar Institute | Compositions and methods for modulating the activity of epstein-barr nuclear antigen 1 |
| LT2813502T (lt) | 2013-06-14 | 2017-03-10 | Dompé Farmaceutici S.P.A. | Bradikinino receptorių antagonistai ir juos turinčios farmacinės kompozicijos |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3654275A (en) * | 1969-10-15 | 1972-04-04 | Pfizer & Co C | Quinoxalinecarboxamide antiinflammatory agents |
| US3635971A (en) * | 1970-06-18 | 1972-01-18 | Abbott Lab | 3 (3 4-dihydro-3-oxo-2-quinoxalinyl) propionamides |
| US6369057B1 (en) * | 1991-04-15 | 2002-04-09 | Aventis Pharma Deutschland Gmbh | Quinoxalines, processes for their preparation and their use |
| AU680870B2 (en) * | 1993-04-28 | 1997-08-14 | Astellas Pharma Inc. | New heterocyclic compounds |
| DE4341663A1 (de) * | 1993-12-07 | 1995-06-08 | Basf Ag | Anellierte 2-Oxopiperazine, ihre Herstellung und Verwendung |
| FR2735128B1 (fr) * | 1995-06-07 | 1997-07-25 | Fournier Ind & Sante | Nouveaux composes de benzenesulfonamide, leur procede de preparation et utilisation en therapeutique. |
| DE19712960A1 (de) * | 1997-03-27 | 1998-10-01 | Hoechst Ag | Benzyloxy-substituierte, anellierte N-Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Bradykininrezeptorantagonisten |
| WO2000078747A1 (en) * | 1999-06-22 | 2000-12-28 | Takeda Chemical Industries, Ltd. | Acylhydrazine derivatives, process for preparing the same and use thereof |
| DE10134721A1 (de) * | 2001-07-17 | 2003-02-06 | Bayer Ag | Tetrahydrochinoxaline |
| CA2483573A1 (en) * | 2002-05-03 | 2003-11-13 | Elan Pharmaceuticals, Inc. | Sulfonylquinoxalone acetamide derivatives and related compounds as bradykinin antagonists |
-
2003
- 2003-05-02 CA CA002483573A patent/CA2483573A1/en not_active Abandoned
- 2003-05-02 WO PCT/US2003/013805 patent/WO2003093245A1/en not_active Ceased
- 2003-05-02 JP JP2004501384A patent/JP2005530753A/ja active Pending
- 2003-05-02 AU AU2003228825A patent/AU2003228825A1/en not_active Abandoned
- 2003-05-02 US US10/429,203 patent/US7056937B2/en not_active Expired - Fee Related
- 2003-05-02 US US10/429,917 patent/US7183281B2/en not_active Expired - Fee Related
- 2003-05-02 EP EP03726597A patent/EP1501807A1/en not_active Withdrawn
-
2006
- 2006-05-05 US US11/429,656 patent/US7635775B2/en not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2005530753A5 (enExample) | ||
| RU2462464C2 (ru) | Замещенные сульфамидные производные | |
| RU2401265C2 (ru) | Соединения и композиции в качестве ингибиторов протеинкиназы | |
| JP6346862B2 (ja) | オレキシンレセプターアンタゴニストとしての置換プロリン／ピペリジン | |
| DK2718266T3 (en) | PYRIDIN-2-AMIDES USED AS CB2 AGONISTS | |
| JP5210375B2 (ja) | ５−ｈｔ７受容体拮抗薬としての２−［４−（ピラゾール−４−イルアルキル）ピペラジン−１−イル］−３−フェニルピラジンおよびピリジンならびに３−［４−（ピラゾール−４−イルアルキル）ピペラジン−１−イル］−２−フェニルピリジン | |
| RU2386630C2 (ru) | Соединения и композиции в качестве ингибиторов протеинтирозинкиназы | |
| CN103391935B (zh) | 二氨基嘧啶衍生物及其制备方法 | |
| JPWO2021087025A5 (enExample) | ||
| RU2009147733A (ru) | Пиридилпиперидновые антагонисты рецептора орексинов | |
| CN1137886C (zh) | 新的2,3-二氧-1,2,3,4-四氢-喹喔啉基衍生物 | |
| JP2008525408A (ja) | 早産、月経困難症および子宮内膜症の処置用のオキトシン受容体アンタゴニストとしての１，６−置換（３ｒ，６ｒ）−３−（２，３−ジヒドロ−１ｈ−インデン−２−イル）−２，５−ピペラジンジオン誘導体 | |
| JP2018520201A5 (enExample) | ||
| JP2006500348A5 (enExample) | ||
| KR101800044B1 (ko) | 신규 아미드 유도체 및 그의 의약으로서의 용도 | |
| JP2011518836A5 (enExample) | ||
| RU2008135690A (ru) | Соединения и композиции в качестве ингибиторов протеинкиназы | |
| JP2006500369A5 (enExample) | ||
| JP2008500336A5 (enExample) | ||
| US20130184460A1 (en) | Glycine transporter inhibiting substances | |
| WO2015152367A1 (ja) | オキソ複素環誘導体 | |
| RU2009138219A (ru) | Новые бензамидные производные и способ их получения | |
| RU2015144485A (ru) | Геминально-замещенные цианоэтилпиразолопиридоны в качестве ингибиторов janus киназ | |
| KR20070007346A (ko) | ＴＡＦＩａ 억제제로서의 이미다졸 유도체 | |
| CN101048383A (zh) | 促性腺激素释放激素受体拮抗剂 |