JP2004507527A5 - - Google Patents
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- Publication number
- JP2004507527A5 JP2004507527A5 JP2002523466A JP2002523466A JP2004507527A5 JP 2004507527 A5 JP2004507527 A5 JP 2004507527A5 JP 2002523466 A JP2002523466 A JP 2002523466A JP 2002523466 A JP2002523466 A JP 2002523466A JP 2004507527 A5 JP2004507527 A5 JP 2004507527A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- methyl
- alkyl
- compound
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 37
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000004423 acyloxy group Chemical group 0.000 claims 6
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 239000000651 prodrug Substances 0.000 claims 6
- 229940002612 prodrug Drugs 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 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 5
- -1 4-{[(4-amino-6,7-dimethoxy-quinazolin-2-yl) -methyl-amino] -methyl} -4-phenyl-piperidin-1-yl Chemical group 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 230000006806 disease prevention Effects 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 230000002194 synthesizing effect Effects 0.000 claims 2
- GHGQPLMWEBWRTF-GOSISDBHSA-N (3r)-1-[4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]methyl]-4-phenylpiperidin-1-yl]-3-hydroxybutan-1-one Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CC1(C=2C=CC=CC=2)CCN(C(=O)C[C@@H](C)O)CC1 GHGQPLMWEBWRTF-GOSISDBHSA-N 0.000 claims 1
- GHGQPLMWEBWRTF-SFHVURJKSA-N (3s)-1-[4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]methyl]-4-phenylpiperidin-1-yl]-3-hydroxybutan-1-one Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CC1(C=2C=CC=CC=2)CCN(C(=O)C[C@H](C)O)CC1 GHGQPLMWEBWRTF-SFHVURJKSA-N 0.000 claims 1
- ONHMOOVKCXOPTA-UHFFFAOYSA-N 1-[4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)methylamino]methyl]-4-phenylpiperidin-1-yl]-4,4,4-trifluorobutan-1-one Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1CNCC1(C=2C=CC=CC=2)CCN(C(=O)CCC(F)(F)F)CC1 ONHMOOVKCXOPTA-UHFFFAOYSA-N 0.000 claims 1
- ZIDXCCICXISHCE-UHFFFAOYSA-N 1-[4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)methylamino]methyl]-4-phenylpiperidin-1-yl]butan-1-one Chemical compound C1CN(C(=O)CCC)CCC1(C=1C=CC=CC=1)CNCC1=NC(N)=C(C=C(OC)C(OC)=C2)C2=N1 ZIDXCCICXISHCE-UHFFFAOYSA-N 0.000 claims 1
- PMQJAZZNTBMNEW-UHFFFAOYSA-N 2-[(1-cyclopropylsulfonyl-4-phenylpiperidin-4-yl)methyl]-6,7-dimethoxy-2-N-methyl-1H-quinazoline-2,4-diamine Chemical compound C1(CC1)S(=O)(=O)N1CCC(CC1)(C1=CC=CC=C1)CC1(NC2=CC(=C(C=C2C(=N1)N)OC)OC)NC PMQJAZZNTBMNEW-UHFFFAOYSA-N 0.000 claims 1
- DXPQTHAFYUTZRR-UHFFFAOYSA-N 2-methylquinazoline Chemical compound C1=CC=CC2=NC(C)=NC=C21 DXPQTHAFYUTZRR-UHFFFAOYSA-N 0.000 claims 1
- FJNLCHNQVJVCPY-UHFFFAOYSA-N 2-n-methoxy-2-n-methyl-4-n,6-n-dipropyl-1,3,5-triazine-2,4,6-triamine Chemical compound CCCNC1=NC(NCCC)=NC(N(C)OC)=N1 FJNLCHNQVJVCPY-UHFFFAOYSA-N 0.000 claims 1
- DQLPHKVITLOLRA-UHFFFAOYSA-N 4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]methyl]-4-phenyl-n-pyridin-3-ylpiperidine-1-carboxamide Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CC(CC1)(C=2C=CC=CC=2)CCN1C(=O)NC1=CC=CN=C1 DQLPHKVITLOLRA-UHFFFAOYSA-N 0.000 claims 1
- XLXDAWFMQFQZGK-UHFFFAOYSA-N 4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]methyl]-n,n-dimethyl-4-phenylpiperidine-1-sulfonamide Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CC1(C=2C=CC=CC=2)CCN(S(=O)(=O)N(C)C)CC1 XLXDAWFMQFQZGK-UHFFFAOYSA-N 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- MFNDNCQSZFQSOV-UHFFFAOYSA-N 6,7-dimethoxy-2-n-methyl-2-n-[(4-phenyl-1-propan-2-ylsulfonylpiperidin-4-yl)methyl]quinazoline-2,4-diamine Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CC1(C=2C=CC=CC=2)CCN(S(=O)(=O)C(C)C)CC1 MFNDNCQSZFQSOV-UHFFFAOYSA-N 0.000 claims 1
- WNLVEKFOXYFXHP-UHFFFAOYSA-N C1(CC1)CC(=N)N1CCC(CC1)(C1=CC=CC=C1)CC1(NC2=CC(=C(C=C2C(=N1)N)OC)OC)NC Chemical compound C1(CC1)CC(=N)N1CCC(CC1)(C1=CC=CC=C1)CC1(NC2=CC(=C(C=C2C(=N1)N)OC)OC)NC WNLVEKFOXYFXHP-UHFFFAOYSA-N 0.000 claims 1
- 201000001880 Sexual dysfunction Diseases 0.000 claims 1
- 208000027520 Somatoform disease Diseases 0.000 claims 1
- 208000026723 Urinary tract disease Diseases 0.000 claims 1
- CLDHYZHTRGERAT-UHFFFAOYSA-N [4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]methyl]-4-phenylpiperidin-1-yl]-(oxolan-2-yl)methanone Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CC(CC1)(C=2C=CC=CC=2)CCN1C(=O)C1CCCO1 CLDHYZHTRGERAT-UHFFFAOYSA-N 0.000 claims 1
- KGWLKUXZQYJSDJ-UHFFFAOYSA-N [4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]methyl]-4-phenylpiperidin-1-yl]-cyclopropylmethanone Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CC(CC1)(C=2C=CC=CC=2)CCN1C(=O)C1CC1 KGWLKUXZQYJSDJ-UHFFFAOYSA-N 0.000 claims 1
- YPRSAAAUAFMTJD-UHFFFAOYSA-N [4-[[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]methyl]-4-phenylpiperidin-1-yl]-pyrrolidin-2-ylmethanone Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CC(CC1)(C=2C=CC=CC=2)CCN1C(=O)C1CCCN1 YPRSAAAUAFMTJD-UHFFFAOYSA-N 0.000 claims 1
- 239000000951 adrenergic alpha-1 receptor antagonist Substances 0.000 claims 1
- 239000000674 adrenergic antagonist Substances 0.000 claims 1
- 102000030619 alpha-1 Adrenergic Receptor Human genes 0.000 claims 1
- 108020004102 alpha-1 Adrenergic Receptor Proteins 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 208000027753 pain disease Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 231100000872 sexual dysfunction Toxicity 0.000 claims 1
- 208000014001 urinary system disease Diseases 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22950300P | 2000-08-31 | 2000-08-31 | |
| PCT/EP2001/009749 WO2002018348A2 (en) | 2000-08-31 | 2001-08-23 | Quinazoline derivatives as alpha-1 adrenergic antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004507527A JP2004507527A (ja) | 2004-03-11 |
| JP2004507527A5 true JP2004507527A5 (enExample) | 2005-04-07 |
| JP3971299B2 JP3971299B2 (ja) | 2007-09-05 |
Family
ID=22861517
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002523466A Expired - Fee Related JP3971299B2 (ja) | 2000-08-31 | 2001-08-23 | α−１アドレナリン作動性拮抗薬としてのキナゾリン誘導体 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US6559153B2 (enExample) |
| EP (1) | EP1315714B1 (enExample) |
| JP (1) | JP3971299B2 (enExample) |
| KR (1) | KR100602929B1 (enExample) |
| CN (1) | CN1308324C (enExample) |
| AR (1) | AR032475A1 (enExample) |
| AT (1) | ATE309240T1 (enExample) |
| AU (2) | AU9378801A (enExample) |
| BR (1) | BR0113585A (enExample) |
| CA (1) | CA2420177C (enExample) |
| DE (1) | DE60114852T2 (enExample) |
| ES (1) | ES2251512T3 (enExample) |
| GT (1) | GT200100181A (enExample) |
| MX (1) | MXPA03001777A (enExample) |
| PA (1) | PA8527901A1 (enExample) |
| PE (1) | PE20020407A1 (enExample) |
| UY (1) | UY26919A1 (enExample) |
| WO (1) | WO2002018348A2 (enExample) |
| ZA (1) | ZA200301082B (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE341552T1 (de) * | 2001-08-10 | 2006-10-15 | Neuro Therapeutics Ltd | Derivate morphinähnlicher opioidverbindungen |
| JP2005521728A (ja) * | 2002-04-03 | 2005-07-21 | オリオン コーポレーション | ＣＮＳ関連疾患のためのα２−アドレナリン受容体アンタゴニストの使用 |
| TW200403058A (en) * | 2002-04-19 | 2004-03-01 | Bristol Myers Squibb Co | Heterocyclo inhibitors of potassium channel function |
| ITMI20030151A1 (it) * | 2003-01-30 | 2004-07-31 | Recordati Ind Chimica E Farma Ceutica S P A | Uso di antagonisti selettivi del recettore mglu5 per il trattamento di disfunzioni neuromuscolari del tratto urinario inferiore. |
| ATE440825T1 (de) * | 2003-06-06 | 2009-09-15 | Vertex Pharma | Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern |
| DE602004020994D1 (de) * | 2003-07-24 | 2009-06-18 | Euro Celtique Sa | Piperidinverbindungen und pharmazeutische zusammensetzungen, die diese enthalten |
| WO2006021345A2 (en) * | 2004-08-27 | 2006-03-02 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with adrenergic alpha-1b receptor (adra1b) |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| US7413607B2 (en) * | 2005-03-31 | 2008-08-19 | 3M Innovative Properties Company | Templated semiconductor particles and methods of making |
| US7344583B2 (en) * | 2005-03-31 | 2008-03-18 | 3M Innovative Properties Company | Methods of making metal particles within cored dendrimers |
| BRPI0611537A2 (pt) * | 2005-05-04 | 2010-09-21 | Hoffmann La Roche | (3,4-diidro-quinazolin-2-il) -(2-arilóxi-etil)-aminas tendo uma atividade sobre o receptor de 5-ht |
| FI3719018T3 (fi) | 2006-04-25 | 2025-10-07 | Astex Therapeutics Ltd | Puriini- ja deatsapuriinijohdannaisia farmaseuttisina yhdisteinä |
| WO2008036700A2 (en) * | 2006-09-19 | 2008-03-27 | 3M Innovative Properties Company | Templated metal oxide particles and methods of making |
| MX2010003927A (es) | 2007-10-11 | 2010-04-30 | Astrazeneca Ab | Derivados de pirrolo [2,3-d] pirimidina como inhibidores de proteinas cinasas b. |
| TW200944526A (en) | 2008-04-22 | 2009-11-01 | Vitae Pharmaceuticals Inc | Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| KR101851820B1 (ko) | 2011-04-01 | 2018-06-04 | 아스트라제네카 아베 | 치료적 요법 |
| SG11201401471PA (en) | 2011-11-30 | 2014-08-28 | Astrazeneca Ab | Combination treatment of cancer |
| AU2013204533B2 (en) | 2012-04-17 | 2017-02-02 | Astrazeneca Ab | Crystalline forms |
| CN110662541B (zh) * | 2017-03-12 | 2023-02-10 | 王晓冬 | 多环胺作为阿片受体调节剂 |
| WO2019088095A1 (ja) * | 2017-11-02 | 2019-05-09 | 国立大学法人九州大学 | 鎮痛剤及びその使用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0853479A4 (en) | 1995-09-29 | 2001-04-11 | Merck & Co Inc | ALPHA 1B ADRENERGIC RECEPTOR ANTAGONISTS |
| GB9526546D0 (en) * | 1995-12-23 | 1996-02-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9700504D0 (en) | 1997-01-11 | 1997-02-26 | Pfizer Ltd | Pharmaceutical compounds |
| US6355641B1 (en) | 1999-03-17 | 2002-03-12 | Syntex (U.S.A.) Llc | Oxazolone derivatives and uses thereof |
-
2001
- 2001-08-23 CA CA002420177A patent/CA2420177C/en not_active Expired - Fee Related
- 2001-08-23 AU AU9378801A patent/AU9378801A/xx active Pending
- 2001-08-23 MX MXPA03001777A patent/MXPA03001777A/es active IP Right Grant
- 2001-08-23 JP JP2002523466A patent/JP3971299B2/ja not_active Expired - Fee Related
- 2001-08-23 EP EP01974210A patent/EP1315714B1/en not_active Expired - Lifetime
- 2001-08-23 ES ES01974210T patent/ES2251512T3/es not_active Expired - Lifetime
- 2001-08-23 KR KR1020037002933A patent/KR100602929B1/ko not_active Expired - Fee Related
- 2001-08-23 DE DE60114852T patent/DE60114852T2/de not_active Expired - Fee Related
- 2001-08-23 AT AT01974210T patent/ATE309240T1/de not_active IP Right Cessation
- 2001-08-23 CN CNB018165958A patent/CN1308324C/zh not_active Expired - Fee Related
- 2001-08-23 WO PCT/EP2001/009749 patent/WO2002018348A2/en not_active Ceased
- 2001-08-23 AU AU2001293788A patent/AU2001293788B2/en not_active Ceased
- 2001-08-23 BR BR0113585-6A patent/BR0113585A/pt not_active IP Right Cessation
- 2001-08-29 PE PE2001000870A patent/PE20020407A1/es not_active Application Discontinuation
- 2001-08-29 US US09/942,385 patent/US6559153B2/en not_active Expired - Fee Related
- 2001-08-30 PA PA20018527901A patent/PA8527901A1/es unknown
- 2001-08-30 GT GT200100181A patent/GT200100181A/es unknown
- 2001-08-30 AR ARP010104130A patent/AR032475A1/es unknown
- 2001-08-30 UY UY26919A patent/UY26919A1/es not_active Application Discontinuation
-
2003
- 2003-02-07 ZA ZA200301082A patent/ZA200301082B/en unknown
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