JP2007509158A5 - - Google Patents
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- JP2007509158A5 JP2007509158A5 JP2006536779A JP2006536779A JP2007509158A5 JP 2007509158 A5 JP2007509158 A5 JP 2007509158A5 JP 2006536779 A JP2006536779 A JP 2006536779A JP 2006536779 A JP2006536779 A JP 2006536779A JP 2007509158 A5 JP2007509158 A5 JP 2007509158A5
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- JP
- Japan
- Prior art keywords
- formula
- compound
- group
- alkyl
- compound according
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 31
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- -1 hydroxy, cyano, acetyl Chemical group 0.000 claims 5
- 239000002904 solvent Substances 0.000 claims 5
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 4
- 125000004663 dialkyl amino group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000004953 trihalomethyl group Chemical group 0.000 claims 4
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 2
- JOAYEJZDGOLEDZ-QGZVFWFLSA-N 6-(4-chlorophenyl)-3-[4-[(3r)-3-hydroxypyrrolidin-1-yl]-3-methoxyphenyl]thieno[3,2-d]pyrimidin-4-one Chemical compound COC1=CC(N2C(C=3SC(=CC=3N=C2)C=2C=CC(Cl)=CC=2)=O)=CC=C1N1CC[C@@H](O)C1 JOAYEJZDGOLEDZ-QGZVFWFLSA-N 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 239000003054 catalyst Substances 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 229910052763 palladium Inorganic materials 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000004951 trihalomethoxy group Chemical group 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- SYEXCHNVDLNLJK-UHFFFAOYSA-N 6-(4-chlorophenyl)-3-(3-methoxy-4-pyrrolidin-1-ylphenyl)thieno[3,2-d]pyrimidin-4-one Chemical compound COC1=CC(N2C(C=3SC(=CC=3N=C2)C=2C=CC(Cl)=CC=2)=O)=CC=C1N1CCCC1 SYEXCHNVDLNLJK-UHFFFAOYSA-N 0.000 claims 1
- JOAYEJZDGOLEDZ-KRWDZBQOSA-N 6-(4-chlorophenyl)-3-[4-[(3s)-3-hydroxypyrrolidin-1-yl]-3-methoxyphenyl]thieno[3,2-d]pyrimidin-4-one Chemical compound COC1=CC(N2C(C=3SC(=CC=3N=C2)C=2C=CC(Cl)=CC=2)=O)=CC=C1N1CC[C@H](O)C1 JOAYEJZDGOLEDZ-KRWDZBQOSA-N 0.000 claims 1
- JWZFGZYJZKNIMR-QGZVFWFLSA-N 6-(4-fluorophenyl)-3-[4-[(3r)-3-hydroxypyrrolidin-1-yl]-3-methoxyphenyl]thieno[3,2-d]pyrimidin-4-one Chemical compound COC1=CC(N2C(C=3SC(=CC=3N=C2)C=2C=CC(F)=CC=2)=O)=CC=C1N1CC[C@@H](O)C1 JWZFGZYJZKNIMR-QGZVFWFLSA-N 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 229940124802 CB1 antagonist Drugs 0.000 claims 1
- 229940122495 CCK A receptor agonist Drugs 0.000 claims 1
- 101000993364 Homo sapiens Ciliary neurotrophic factor Proteins 0.000 claims 1
- 101000978418 Homo sapiens Melanocortin receptor 4 Proteins 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 229940086609 Lipase inhibitor Drugs 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 102100023724 Melanocortin receptor 4 Human genes 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 1
- 238000006619 Stille reaction Methods 0.000 claims 1
- 238000006069 Suzuki reaction reaction Methods 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000000883 anti-obesity agent Substances 0.000 claims 1
- 229940125710 antiobesity agent Drugs 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 239000003153 chemical reaction reagent Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000007822 coupling agent Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 229940125425 inverse agonist Drugs 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 230000001561 neurotransmitter reuptake Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- JHHZLHWJQPUNKB-UHFFFAOYSA-N pyrrolidin-3-ol Chemical group OC1CCNC1 JHHZLHWJQPUNKB-UHFFFAOYSA-N 0.000 claims 1
- 229940044551 receptor antagonist Drugs 0.000 claims 1
- 239000002464 receptor antagonist Substances 0.000 claims 1
- 238000007363 ring formation reaction Methods 0.000 claims 1
- WRIKHQLVHPKCJU-UHFFFAOYSA-N sodium bis(trimethylsilyl)amide Chemical compound C[Si](C)(C)N([Na])[Si](C)(C)C WRIKHQLVHPKCJU-UHFFFAOYSA-N 0.000 claims 1
- KXCAEQNNTZANTK-UHFFFAOYSA-N stannane Chemical compound [SnH4] KXCAEQNNTZANTK-UHFFFAOYSA-N 0.000 claims 1
- 229910000080 stannane Inorganic materials 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- JLTRXTDYQLMHGR-UHFFFAOYSA-N trimethylaluminium Chemical compound C[Al](C)C JLTRXTDYQLMHGR-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US51380003P | 2003-10-23 | 2003-10-23 | |
| PCT/US2004/034846 WO2005042541A1 (en) | 2003-10-23 | 2004-10-21 | 3-(4-aminophenyl) thienopyrimid-4-one derivatives as mch r1 antagonists for the treatment of obesity, diabetes, depression and anxiety |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007509158A JP2007509158A (ja) | 2007-04-12 |
| JP2007509158A5 true JP2007509158A5 (enExample) | 2007-07-26 |
Family
ID=34549304
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006536779A Pending JP2007509158A (ja) | 2003-10-23 | 2004-10-21 | 肥満、糖尿病、うつ病及び不安を治療するためのｍｃｈｒ１アンタゴニストとしての３−（４−アミノフェニル）チエノピリミド−４−オン誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20070078125A1 (enExample) |
| EP (1) | EP1678184A1 (enExample) |
| JP (1) | JP2007509158A (enExample) |
| KR (1) | KR20060100412A (enExample) |
| CN (1) | CN1871242A (enExample) |
| AU (1) | AU2004285913A1 (enExample) |
| BR (1) | BRPI0415667A (enExample) |
| CA (1) | CA2543122A1 (enExample) |
| CO (1) | CO5690599A2 (enExample) |
| IL (1) | IL174693A0 (enExample) |
| MA (1) | MA28111A1 (enExample) |
| MX (1) | MXPA06003997A (enExample) |
| NO (1) | NO20061909L (enExample) |
| WO (1) | WO2005042541A1 (enExample) |
| ZA (1) | ZA200603181B (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080221107A1 (en) * | 2005-07-15 | 2008-09-11 | Astrazeneca Ab | Therapeutic Agents |
| AU2006298852A1 (en) | 2005-09-30 | 2007-04-12 | F. Hoffmann-La Roche Ag | Indane derivatives as MCH receptor antagonists |
| US8618115B2 (en) * | 2005-10-26 | 2013-12-31 | Bristol-Myers Squibb Company | Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them |
| US7745447B2 (en) | 2005-10-26 | 2010-06-29 | Bristol-Myers Squibb Company | Substituted thieno[3,2-D]pyrimidines as non-basic melanin concentrating hormone receptor-1 antagonists |
| JP5193878B2 (ja) | 2005-12-21 | 2013-05-08 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｍｃｈ−１が媒介する疾患における使用のための新規な置換ピラジノン誘導体 |
| US7553836B2 (en) | 2006-02-06 | 2009-06-30 | Bristol-Myers Squibb Company | Melanin concentrating hormone receptor-1 antagonists |
| TW200801022A (en) | 2006-02-15 | 2008-01-01 | Sanofi Aventis | Novel amino alcohol-substituted arylthienopyrimidinones, process for their preparation and their use as medicaments |
| ATE495157T1 (de) | 2006-02-15 | 2011-01-15 | Sanofi Aventis | Neue aminoalkohol-substituierte aryldihydroisochinolinone, herstellungsverfahren und ihre verwendung als medikamente |
| JP5175228B2 (ja) | 2006-02-15 | 2013-04-03 | サノフイ | 新規なアザシクリル置換アリールジヒドロイソキノリノン、それらの製造方法及び薬剤としてそれらの使用 |
| JP2009526792A (ja) * | 2006-02-15 | 2009-07-23 | サノフィ−アベンティス | 新規なアザシクリル置換アリールチエノピリミジノン、それらの製造方法及び薬剤としてのそれらの使用 |
| CN101454328A (zh) * | 2006-06-08 | 2009-06-10 | 伊莱利利公司 | 新的mch受体拮抗剂 |
| JP2010501553A (ja) | 2006-08-18 | 2010-01-21 | アストラゼネカ アクチボラグ | Ｍｃｈｒ１アンタゴニストとしてのチエノピリミジン−４−オン誘導体およびチエノピリダジン−７−オン誘導体 |
| BRPI0806537A2 (pt) | 2007-01-10 | 2014-04-22 | Albany Molecular Res Inc | Indazóis substituídos por 5-piridinona |
| WO2008134480A1 (en) * | 2007-04-25 | 2008-11-06 | Bristol-Myers Squibb Company | Non-basic melanin concentrating hormone receptor-1 antagonists |
| ATE544759T1 (de) | 2007-07-21 | 2012-02-15 | Albany Molecular Res Inc | 5-pyridinon-substituierte indazole und pharmazeutische zusammensetzungen davon |
| PE20091928A1 (es) | 2008-05-29 | 2009-12-31 | Bristol Myers Squibb Co | Tienopirimidinas hidroxisustituidas como antagonistas de receptor-1 de hormona concentradora de melanina no basicos |
| US8278316B2 (en) | 2009-03-09 | 2012-10-02 | Bristol-Myers Squibb Company | Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists |
| HUP1100241A3 (en) | 2011-05-06 | 2013-12-30 | Richter Gedeon Nyrt | Oxetane substituted pyrimidones |
| KR20130013199A (ko) * | 2011-07-27 | 2013-02-06 | 한미약품 주식회사 | 신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물 |
| WO2013032535A1 (en) | 2011-08-26 | 2013-03-07 | O'neil Michael P | Tattoo removal system and method |
| AU2021206286A1 (en) * | 2020-01-10 | 2024-08-08 | Consynance Therapeutics, Inc. | Therapeutic combinations of drugs and methods of using them |
| HUP2200222A1 (hu) | 2022-06-17 | 2023-12-28 | Richter Gedeon Nyrt | MCHR1 antagonisták a Prader-Willi szindróma kezelésére |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0124627D0 (en) * | 2001-10-15 | 2001-12-05 | Smithkline Beecham Plc | Novel compounds |
-
2004
- 2004-10-21 CA CA002543122A patent/CA2543122A1/en not_active Abandoned
- 2004-10-21 BR BRPI0415667-6A patent/BRPI0415667A/pt not_active IP Right Cessation
- 2004-10-21 EP EP04795941A patent/EP1678184A1/en not_active Withdrawn
- 2004-10-21 JP JP2006536779A patent/JP2007509158A/ja active Pending
- 2004-10-21 MX MXPA06003997A patent/MXPA06003997A/es unknown
- 2004-10-21 AU AU2004285913A patent/AU2004285913A1/en not_active Abandoned
- 2004-10-21 KR KR1020067009417A patent/KR20060100412A/ko not_active Withdrawn
- 2004-10-21 CN CNA2004800313000A patent/CN1871242A/zh active Pending
- 2004-10-21 US US10/576,765 patent/US20070078125A1/en not_active Abandoned
- 2004-10-21 WO PCT/US2004/034846 patent/WO2005042541A1/en not_active Ceased
-
2006
- 2006-03-30 IL IL174693A patent/IL174693A0/en unknown
- 2006-04-20 ZA ZA200603181A patent/ZA200603181B/en unknown
- 2006-04-21 CO CO06038136A patent/CO5690599A2/es not_active Application Discontinuation
- 2006-04-25 MA MA28965A patent/MA28111A1/fr unknown
- 2006-04-28 NO NO20061909A patent/NO20061909L/no not_active Application Discontinuation
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