JP2004513940A5 - - Google Patents
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- Publication number
- JP2004513940A5 JP2004513940A5 JP2002542781A JP2002542781A JP2004513940A5 JP 2004513940 A5 JP2004513940 A5 JP 2004513940A5 JP 2002542781 A JP2002542781 A JP 2002542781A JP 2002542781 A JP2002542781 A JP 2002542781A JP 2004513940 A5 JP2004513940 A5 JP 2004513940A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- optionally substituted
- compound according
- propan
- dihydro
- 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
- 150000001875 compounds Chemical class 0.000 claims description 26
- -1 oxy, ethylenedioxy Chemical group 0.000 claims description 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 16
- UFUASNAHBMBJIX-UHFFFAOYSA-N propan-1-one Chemical compound CC[C]=O UFUASNAHBMBJIX-UHFFFAOYSA-N 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
- SHYWWIHHCWYFLV-UHFFFAOYSA-N 3-[4-(4,5-dihydro-1h-imidazol-2-ylamino)phenyl]-1-(2-fluoro-4-morpholin-4-ylphenyl)propan-1-one Chemical compound FC1=CC(N2CCOCC2)=CC=C1C(=O)CCC(C=C1)=CC=C1NC1=NCCN1 SHYWWIHHCWYFLV-UHFFFAOYSA-N 0.000 claims description 2
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims description 2
- 125000006260 ethylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 2
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 3
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 238000011282 treatment Methods 0.000 claims 3
- 108091006335 Prostaglandin I receptors Proteins 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- VKTPNGDSZNCARY-UHFFFAOYSA-N 1-(2,4-dichlorophenyl)-3-[4-(4,5-dihydro-1h-imidazol-2-ylamino)phenyl]propan-1-one Chemical compound ClC1=CC(Cl)=CC=C1C(=O)CCC(C=C1)=CC=C1NC1=NCCN1 VKTPNGDSZNCARY-UHFFFAOYSA-N 0.000 claims 1
- VWVSXLXCFBCNTF-UHFFFAOYSA-N 1-(2,4-difluorophenyl)-3-[4-(4,5-dihydro-1h-imidazol-2-ylamino)phenyl]propan-1-one Chemical compound FC1=CC(F)=CC=C1C(=O)CCC(C=C1)=CC=C1NC1=NCCN1 VWVSXLXCFBCNTF-UHFFFAOYSA-N 0.000 claims 1
- ARPJPZSQLOUFJO-UHFFFAOYSA-N 1-(4-chlorophenyl)-3-[4-(4,5-dihydro-1h-imidazol-2-ylamino)phenyl]propan-1-one Chemical compound C1=CC(Cl)=CC=C1C(=O)CCC(C=C1)=CC=C1NC1=NCCN1 ARPJPZSQLOUFJO-UHFFFAOYSA-N 0.000 claims 1
- HHQBWQDTBFUMAO-UHFFFAOYSA-N 3-[4-(4,5-dihydro-1h-imidazol-2-ylamino)phenyl]-1-(4-fluorophenyl)propan-1-one Chemical compound C1=CC(F)=CC=C1C(=O)CCC(C=C1)=CC=C1NC1=NCCN1 HHQBWQDTBFUMAO-UHFFFAOYSA-N 0.000 claims 1
- RSRNWPLIUTXGSK-UHFFFAOYSA-N 3-[4-(4,5-dihydro-1h-imidazol-2-ylamino)phenyl]-1-(4-morpholin-4-ylphenyl)propan-1-one Chemical compound C=1C=C(N2CCOCC2)C=CC=1C(=O)CCC(C=C1)=CC=C1NC1=NCCN1 RSRNWPLIUTXGSK-UHFFFAOYSA-N 0.000 claims 1
- DXEGFCISSXHHNK-UHFFFAOYSA-N 3-[4-(4,5-dihydro-1h-imidazol-2-ylamino)phenyl]-1-phenylpropan-1-one Chemical compound C=1C=CC=CC=1C(=O)CCC(C=C1)=CC=C1NC1=NCCN1 DXEGFCISSXHHNK-UHFFFAOYSA-N 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000001953 Hypotension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 208000026723 Urinary tract disease Diseases 0.000 claims 1
- 208000012931 Urologic disease Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000021822 hypotensive Diseases 0.000 claims 1
- 230000001077 hypotensive effect Effects 0.000 claims 1
- MTNDZQHUAFNZQY-UHFFFAOYSA-N imidazoline Chemical compound C1CN=CN1 MTNDZQHUAFNZQY-UHFFFAOYSA-N 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 208000014001 urinary system disease Diseases 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24888800P | 2000-11-14 | 2000-11-14 | |
| PCT/EP2001/012776 WO2002040453A1 (en) | 2000-11-14 | 2001-11-05 | Substituted 2-phenylaminoimidazoline phenyl ketone derivatives as ip antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004513940A JP2004513940A (ja) | 2004-05-13 |
| JP2004513940A5 true JP2004513940A5 (https=) | 2005-04-07 |
| JP4108474B2 JP4108474B2 (ja) | 2008-06-25 |
Family
ID=22941114
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002542781A Expired - Fee Related JP4108474B2 (ja) | 2000-11-14 | 2001-11-05 | Ｉｐアンタゴニストとしての置換２−フェニルアミノイミダゾリンフェニルケトン誘導体 |
Country Status (29)
| Country | Link |
|---|---|
| EP (1) | EP1339694B1 (https=) |
| JP (1) | JP4108474B2 (https=) |
| KR (1) | KR100562605B1 (https=) |
| CN (1) | CN1267423C (https=) |
| AR (1) | AR035502A1 (https=) |
| AT (1) | ATE305002T1 (https=) |
| AU (1) | AU2180802A (https=) |
| BG (1) | BG107814A (https=) |
| BR (1) | BR0115291A (https=) |
| CA (1) | CA2427900A1 (https=) |
| CZ (1) | CZ20031596A3 (https=) |
| DE (1) | DE60113563T2 (https=) |
| EC (1) | ECSP034602A (https=) |
| ES (1) | ES2248413T3 (https=) |
| HU (1) | HUP0303156A3 (https=) |
| IL (1) | IL155436A0 (https=) |
| MA (1) | MA26958A1 (https=) |
| MX (1) | MXPA03004073A (https=) |
| NO (1) | NO20032142D0 (https=) |
| NZ (1) | NZ525330A (https=) |
| PA (1) | PA8532201A1 (https=) |
| PE (1) | PE20020602A1 (https=) |
| PL (1) | PL362549A1 (https=) |
| RU (1) | RU2284995C2 (https=) |
| SK (1) | SK7222003A3 (https=) |
| UY (1) | UY27023A1 (https=) |
| WO (1) | WO2002040453A1 (https=) |
| YU (1) | YU37203A (https=) |
| ZA (1) | ZA200303413B (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1596858A1 (en) * | 2003-02-14 | 2005-11-23 | Medical Research Council | Ip receptor antagonists for the treatment of pathological uterine conditions |
| WO2004096213A1 (en) | 2003-05-01 | 2004-11-11 | F. Hoffmann-La Roche Ag | Imidazolin-2-ylaminophenyl amides as ip antagonists |
| JP2007521276A (ja) * | 2003-06-25 | 2007-08-02 | スミスクライン・ビーチャム・コーポレイション | Ｎｋ−２およびｎｋ−３として用いるための４−カルボキサミドキノリン誘導体 |
| MXPA06000269A (es) | 2003-07-09 | 2006-04-07 | Hoffmann La Roche | Tiofenilaminoimidazolinas. |
| CA2637292A1 (en) * | 2006-01-27 | 2007-08-16 | F. Hoffmann-La Roche Ag | Use of 2-imidazoles for the treatment of cns disorders |
| RU2009112496A (ru) | 2006-10-19 | 2010-11-27 | Ф. Хоффманн-Ля Рош Аг (Ch) | Аминометил-4-имидазолы |
| CA2668454A1 (en) | 2006-11-02 | 2008-05-08 | F. Hoffmann-La Roche Ag | Substituted 2-imidazoles |
| JP2010510184A (ja) | 2006-11-16 | 2010-04-02 | エフ．ホフマン−ラ ロシュ アーゲー | 置換４−イミダゾール類 |
| CA2672617A1 (en) | 2006-12-13 | 2008-06-19 | F. Hoffmann-La Roche Ag | Novel 2-imidazoles as ligands for trace amine associated receptors (taar) |
| US20080146523A1 (en) | 2006-12-18 | 2008-06-19 | Guido Galley | Imidazole derivatives |
| CN101600700B (zh) | 2007-02-02 | 2013-08-21 | 弗·哈夫曼-拉罗切有限公司 | 作为taar1配体用于cns病症的新的2-氨基噁唑啉 |
| KR101222412B1 (ko) | 2007-02-15 | 2013-01-15 | 에프. 호프만-라 로슈 아게 | Ｔａａｒ1 리간드로서의 2-아미노옥사졸린 |
| CN101687812A (zh) | 2007-07-02 | 2010-03-31 | 弗·哈夫曼-拉罗切有限公司 | 对痕量胺相关受体(taar)具有良好亲和性的2-咪唑啉化合物 |
| CA2691704A1 (en) | 2007-07-03 | 2009-01-08 | F. Hoffmann-La Roche Ag | 4-imidazolines and their use as antidepressants |
| CA2694362A1 (en) | 2007-07-27 | 2009-02-05 | F. Hoffmann-La Roche Ag | 2-azetidinemethaneamines and 2-pyrrolidinemethaneamines as taar-ligands |
| JP5341084B2 (ja) | 2007-08-03 | 2013-11-13 | エフ．ホフマン−ラ ロシュ アーゲー | Ｔａａｒ１リガンドとしてのピリジンカルボキシアミド及びベンズアミド誘導体 |
| US8242153B2 (en) | 2008-07-24 | 2012-08-14 | Hoffmann-La Roche Inc. | 4,5-dihydro-oxazol-2YL derivatives |
| US8354441B2 (en) | 2009-11-11 | 2013-01-15 | Hoffmann-La Roche Inc. | Oxazoline derivatives |
| WO2011080132A2 (en) | 2009-12-17 | 2011-07-07 | Katholieke Universiteit Leuven, K.U. Leuven R&D | Compounds, compositions and methods for controlling biofilms |
| US9452980B2 (en) | 2009-12-22 | 2016-09-27 | Hoffmann-La Roche Inc. | Substituted benzamides |
| WO2014143591A1 (en) | 2013-03-12 | 2014-09-18 | Allergan, Inc. | Inhibition of neovascularization by simultaneous inhibition of prostanoid ip and ep4 receptors |
| US9321745B2 (en) | 2013-03-12 | 2016-04-26 | Allergan, Inc. | Inhibition of neovascularization by inhibition of prostanoid IP receptors |
| US9827225B2 (en) * | 2016-01-25 | 2017-11-28 | Jenivision Inc. | Use of prostacyclin antagonists for treating ocular surface nociception |
| CN108713019B (zh) | 2016-03-17 | 2021-06-15 | 豪夫迈·罗氏有限公司 | 具有作为taar的激动剂的活性的5-乙基-4-甲基-吡唑-3-甲酰胺衍生物 |
| WO2022101435A1 (en) * | 2020-11-12 | 2022-05-19 | 3Z Ehf | Novel treatments of attention deficit/hyperactivity disorder |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4889868A (en) * | 1984-12-20 | 1989-12-26 | Rorer Pharmaceutical Corporation | Bis-imidazolinoamino derivatives as antiallergy compounds |
| GB9506188D0 (en) * | 1995-03-27 | 1995-05-17 | Fujisawa Pharmaceutical Co | Amidine derivatives |
| NZ331480A (en) * | 1997-09-04 | 2000-02-28 | F | 2-(Arylphenyl)amino-imidazoline derivatives and pharmaceutical compositions |
-
2001
- 2001-11-05 SK SK722-2003A patent/SK7222003A3/sk unknown
- 2001-11-05 AT AT01996531T patent/ATE305002T1/de not_active IP Right Cessation
- 2001-11-05 CN CNB018187471A patent/CN1267423C/zh not_active Expired - Fee Related
- 2001-11-05 YU YU37203A patent/YU37203A/sh unknown
- 2001-11-05 EP EP01996531A patent/EP1339694B1/en not_active Expired - Lifetime
- 2001-11-05 NZ NZ525330A patent/NZ525330A/en unknown
- 2001-11-05 WO PCT/EP2001/012776 patent/WO2002040453A1/en not_active Ceased
- 2001-11-05 BR BR0115291-2A patent/BR0115291A/pt not_active IP Right Cessation
- 2001-11-05 KR KR1020037006504A patent/KR100562605B1/ko not_active Expired - Fee Related
- 2001-11-05 CZ CZ20031596A patent/CZ20031596A3/cs unknown
- 2001-11-05 HU HU0303156A patent/HUP0303156A3/hu unknown
- 2001-11-05 AU AU2180802A patent/AU2180802A/xx not_active Withdrawn
- 2001-11-05 ES ES01996531T patent/ES2248413T3/es not_active Expired - Lifetime
- 2001-11-05 MX MXPA03004073A patent/MXPA03004073A/es active IP Right Grant
- 2001-11-05 IL IL15543601A patent/IL155436A0/xx unknown
- 2001-11-05 JP JP2002542781A patent/JP4108474B2/ja not_active Expired - Fee Related
- 2001-11-05 RU RU2003115426/04A patent/RU2284995C2/ru not_active IP Right Cessation
- 2001-11-05 PL PL01362549A patent/PL362549A1/xx unknown
- 2001-11-05 DE DE60113563T patent/DE60113563T2/de not_active Expired - Fee Related
- 2001-11-05 CA CA002427900A patent/CA2427900A1/en not_active Abandoned
- 2001-11-09 PE PE2001001118A patent/PE20020602A1/es not_active Application Discontinuation
- 2001-11-13 UY UY27023A patent/UY27023A1/es not_active Application Discontinuation
- 2001-11-13 PA PA20018532201A patent/PA8532201A1/es unknown
- 2001-11-13 AR ARP010105280A patent/AR035502A1/es not_active Application Discontinuation
-
2003
- 2003-05-02 ZA ZA200303413A patent/ZA200303413B/en unknown
- 2003-05-12 MA MA27154A patent/MA26958A1/fr unknown
- 2003-05-13 EC EC2003004602A patent/ECSP034602A/es unknown
- 2003-05-13 NO NO20032142A patent/NO20032142D0/no not_active Application Discontinuation
- 2003-05-14 BG BG107814A patent/BG107814A/bg unknown
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