JP2011529959A5 - - Google Patents
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- Publication number
- JP2011529959A5 JP2011529959A5 JP2011521666A JP2011521666A JP2011529959A5 JP 2011529959 A5 JP2011529959 A5 JP 2011529959A5 JP 2011521666 A JP2011521666 A JP 2011521666A JP 2011521666 A JP2011521666 A JP 2011521666A JP 2011529959 A5 JP2011529959 A5 JP 2011529959A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- het
- oxo
- diazocan
- chlorophenyl
- 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 17
- -1 6-oxo-1,6-dihydropyridazin-3-yl Chemical group 0.000 claims 15
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 239000012453 solvate Substances 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 5
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical compound OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 claims 1
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 206010057671 Female sexual dysfunction Diseases 0.000 claims 1
- 206010057672 Male sexual dysfunction Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 102000008316 Type 4 Melanocortin Receptor Human genes 0.000 claims 1
- 108010021436 Type 4 Melanocortin Receptor Proteins 0.000 claims 1
- YRACHDVMKITFAZ-UHFFFAOYSA-N [1,2,4]triazolo[4,3-b]pyridazine Chemical compound C1=CC=NN2C=NN=C21 YRACHDVMKITFAZ-UHFFFAOYSA-N 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000008484 agonism Effects 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- YAXZJQLARJTMSP-GPTJOGTASA-N methyl 8-(4-chlorophenyl)-4-[(3s,4r)-4-(2-fluoro-4-methoxyphenyl)-1-(6-oxo-1h-pyridazin-3-yl)pyrrolidine-3-carbonyl]-1,4-diazocane-1-carboxylate Chemical compound COC(=O)N1CCN(C(=O)[C@H]2[C@@H](CN(C2)C2=NNC(=O)C=C2)C=2C(=CC(OC)=CC=2)F)CCCC1C1=CC=C(Cl)C=C1 YAXZJQLARJTMSP-GPTJOGTASA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8653008P | 2008-08-06 | 2008-08-06 | |
| US61/086,530 | 2008-08-06 | ||
| PCT/IB2009/053317 WO2010015972A1 (en) | 2008-08-06 | 2009-07-30 | Diazepine and diazocane compounds as mc4 agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011529959A JP2011529959A (ja) | 2011-12-15 |
| JP2011529959A5 true JP2011529959A5 (https=) | 2012-09-06 |
| JP5530438B2 JP5530438B2 (ja) | 2014-06-25 |
Family
ID=41226202
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011521666A Expired - Fee Related JP5530438B2 (ja) | 2008-08-06 | 2009-07-30 | Ｍｃ４作動薬としてのジアゼピンおよびジアゾカン化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8592403B2 (https=) |
| EP (1) | EP2326638B9 (https=) |
| JP (1) | JP5530438B2 (https=) |
| KR (1) | KR101280786B1 (https=) |
| CN (1) | CN102171206B (https=) |
| AU (1) | AU2009278838B2 (https=) |
| CA (1) | CA2731897C (https=) |
| DK (1) | DK2326638T5 (https=) |
| ES (1) | ES2421920T3 (https=) |
| IL (1) | IL210703A (https=) |
| MX (1) | MX2011001405A (https=) |
| WO (1) | WO2010015972A1 (https=) |
| ZA (1) | ZA201100374B (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2512778Y2 (ja) | 1990-06-19 | 1996-10-02 | 株式会社荏原製作所 | 全速待機運転ポンプ |
| WO2007096763A2 (en) | 2006-02-23 | 2007-08-30 | Pfizer Limited | Melanocortin type 4 receptor agonist piperidinoylpyrrolidines |
| CN102464623B (zh) * | 2010-11-19 | 2015-04-29 | 上海药明康德新药开发有限公司 | 1,4-二氮杂环辛烷-6-甲酸酯衍生物的制备方法 |
| LT3539551T (lt) | 2011-12-29 | 2022-01-10 | Rhythm Pharmaceuticals, Inc. | Su melanokortino-4 receptoriumi susijusių sutrikimų gydymo būdas heterozigotiniuose nešiotojuose |
| US11116769B2 (en) * | 2013-04-11 | 2021-09-14 | Ctc Bio, Inc. | Tadalafil free base-containing film dosage form containing polyethylene glycol-based polymer and/or vinyl pyrrolidone-based polymer as dispersion stabilizer |
| CN105209025B (zh) * | 2013-04-11 | 2019-06-18 | 西梯茜生命工学股份有限公司 | 包括聚乙二醇类聚合物和/或乙烯基吡咯烷酮类聚合物作为分散稳定剂的含他达拉非游离碱的膜剂形式 |
| EP3333165B1 (en) * | 2015-08-04 | 2019-09-18 | Astellas Pharma Inc. | Piperazine derivative |
| PL3356386T3 (pl) | 2015-09-30 | 2024-08-05 | Rhythm Pharmaceuticals, Inc. | Sposób leczenia zaburzeń związanych ze szlakiem receptora melanokortyny 4 |
| US20210169969A1 (en) | 2018-04-06 | 2021-06-10 | Leonardus H.T. Van Der Ploeg | Compositions for treating kidney disease |
| US20210393621A1 (en) | 2018-10-26 | 2021-12-23 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH507249A (de) * | 1968-05-31 | 1971-05-15 | Sandoz Ag | Verfahren zur Herstellung von 2-Brom-a-ergokryptin |
| GB8531071D0 (en) * | 1985-12-17 | 1986-01-29 | Boots Co Plc | Therapeutic compound |
| US5274143A (en) * | 1991-07-23 | 1993-12-28 | Hoffmann-La Roche Inc. | Process for the preparation of (R)-3-hexyl-5,6-dihydro-4-hydroxy-6-undecyl-2H-pyran-2-one and (R)-5,6-dihydro-6-undecyl-2H-pyran-2,4(3H)-dione |
| FR2692575B1 (fr) * | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| CA2098167C (en) * | 1992-06-24 | 2006-12-19 | Dorothea Isler | Foodstuffs and feedstuffs containing a lipase inhibitor |
| WO1995000497A1 (en) * | 1993-06-18 | 1995-01-05 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| TW381025B (en) * | 1993-08-05 | 2000-02-01 | Hoffmann La Roche | Pharmaceutical composition containing a glucosidase inhibitor and a lipase inhibitor |
| US5596106A (en) * | 1994-07-15 | 1997-01-21 | Eli Lilly And Company | Cannabinoid receptor antagonists |
| DE4435477A1 (de) * | 1994-10-04 | 1996-04-11 | Bayer Ag | Cycloalkano-indol- und -azaindol-derivate |
| US5521186A (en) * | 1994-10-27 | 1996-05-28 | Janssen Pharmaceutica N.V. | Apolipoprotein-β synthesis inhibitors |
| DE122007000005I2 (de) * | 1994-10-27 | 2008-04-24 | Janssen Pharmaceutica Nv | Apolipoprotein-b syntheseinhibitoren |
| US6194413B1 (en) * | 1995-11-13 | 2001-02-27 | Smithkline Beecham Corporation | Hemoregulatory compounds |
| CN1228087A (zh) * | 1996-08-14 | 1999-09-08 | 曾尼卡有限公司 | 取代的嘧啶衍生物和它们的药物用途 |
| US6946468B1 (en) * | 1996-08-17 | 2005-09-20 | Zeneca Limited | 3-mercaptopyrrolidines as farnesyl protein transferase inhibitors |
| US5929077A (en) * | 1996-11-08 | 1999-07-27 | Leftheris; Katerina | Thioproline-containing inhibitors of farnesyl protein transferase |
| WO2000035296A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Improved release of medicament active agents from a chewing gum coating |
| KR100652994B1 (ko) * | 1998-09-11 | 2006-11-30 | 아방티 파르마 소시에테 아노님 | 아제티딘 유도체, 이의 제조방법 및 이를 함유하는 약제 |
| FR2789079B3 (fr) * | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
| EP2123293A3 (en) | 2000-12-14 | 2010-09-08 | Amylin Pharmaceuticals, Inc. | Peptide YY and petide YY agonists for treatment of metabolic disorders |
| DE60215132T2 (de) | 2001-02-28 | 2007-08-23 | Merck & Co., Inc. | Acylierte piperidin-derivate als melanocortin-4-rezeptor-agonisten |
| CA2439152C (en) | 2001-02-28 | 2008-06-17 | Merck & Co., Inc. | Acylated piperidine derivatives as melanocortin-4 receptor agonists |
| PL363751A1 (en) | 2001-03-22 | 2004-11-29 | Solvay Pharmaceuticals B.V. | 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity |
| JP2005514008A (ja) | 2001-09-24 | 2005-05-19 | オレゴン ヘルス アンド サイエンス ユニバーシティー | 摂食行動を改変する薬剤をスクリーニングするための、弓状核におけるニューロンの評価方法 |
| EP1482794A1 (en) | 2002-03-06 | 2004-12-08 | Merck & Co., Inc. | Method of treatment or prevention of obesity |
| JP4202319B2 (ja) | 2002-07-29 | 2008-12-24 | エフ．ホフマン−ラ ロシュ アーゲー | 新規ベンゾジオキソール |
| EP1558252B1 (en) | 2002-08-02 | 2007-10-10 | Merck & Co., Inc. | Substituted furo [2,3-b]pyridine derivatives |
| US7129239B2 (en) | 2002-10-28 | 2006-10-31 | Pfizer Inc. | Purine compounds and uses thereof |
| MY134457A (en) | 2002-11-22 | 2007-12-31 | Merck & Co Inc | Substituted amides |
| US7329658B2 (en) | 2003-02-06 | 2008-02-12 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| US7141669B2 (en) | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod receptor ligands and uses thereof |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US20050192286A1 (en) * | 2003-10-22 | 2005-09-01 | Neurocrine Biosciences, Inc. | Ligands of melanocortin receptors and compositions and methods related thereto |
| US7151097B2 (en) * | 2003-11-07 | 2006-12-19 | Pfizer Inc. | Bicyclic pyrazolyl and imidazolyl compounds and uses thereof |
| US7649002B2 (en) | 2004-02-04 | 2010-01-19 | Pfizer Inc | (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists |
| JP2008516922A (ja) * | 2004-10-15 | 2008-05-22 | グラクソ グループ リミテッド | ヒスタミン受容体リガンドとしてのピロリジン誘導体 |
| WO2006104008A1 (ja) * | 2005-03-25 | 2006-10-05 | Kissei Pharmaceutical Co., Ltd. | ウレア誘導体、それを含有する医薬組成物およびそれらの医薬用途 |
| CA2617654A1 (en) | 2005-08-04 | 2007-02-08 | Pfizer Limited | Piperidinoyl-pyrrolidine and piperidinoyl-piperidine compounds |
-
2009
- 2009-07-30 KR KR1020117005275A patent/KR101280786B1/ko not_active Expired - Fee Related
- 2009-07-30 WO PCT/IB2009/053317 patent/WO2010015972A1/en not_active Ceased
- 2009-07-30 CA CA2731897A patent/CA2731897C/en not_active Expired - Fee Related
- 2009-07-30 CN CN200980139321.7A patent/CN102171206B/zh not_active Expired - Fee Related
- 2009-07-30 EP EP09786755.0A patent/EP2326638B9/en not_active Not-in-force
- 2009-07-30 ES ES09786755T patent/ES2421920T3/es active Active
- 2009-07-30 AU AU2009278838A patent/AU2009278838B2/en not_active Ceased
- 2009-07-30 JP JP2011521666A patent/JP5530438B2/ja not_active Expired - Fee Related
- 2009-07-30 MX MX2011001405A patent/MX2011001405A/es active IP Right Grant
- 2009-07-30 DK DK09786755.0T patent/DK2326638T5/da active
- 2009-07-30 US US13/057,319 patent/US8592403B2/en not_active Expired - Fee Related
-
2011
- 2011-01-14 ZA ZA2011/00374A patent/ZA201100374B/en unknown
- 2011-01-17 IL IL210703A patent/IL210703A/en not_active IP Right Cessation
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