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 (enExample) | 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 (enExample) |
| EP (1) | EP2326638B9 (enExample) |
| JP (1) | JP5530438B2 (enExample) |
| KR (1) | KR101280786B1 (enExample) |
| CN (1) | CN102171206B (enExample) |
| AU (1) | AU2009278838B2 (enExample) |
| CA (1) | CA2731897C (enExample) |
| DK (1) | DK2326638T5 (enExample) |
| ES (1) | ES2421920T3 (enExample) |
| IL (1) | IL210703A (enExample) |
| MX (1) | MX2011001405A (enExample) |
| WO (1) | WO2010015972A1 (enExample) |
| ZA (1) | ZA201100374B (enExample) |
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 |
| BRPI0708264A2 (pt) | 2006-02-23 | 2011-05-24 | Pfizer Ltd | piperidinilpirrolidinas agonistas do receptor tipo 4 de melanocortina |
| 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 |
| ES2732077T3 (es) | 2011-12-29 | 2019-11-20 | Rhythm Pharmaceuticals Inc | Método para tratar trastornos asociados con el receptor de melanocortina-4 en portadores heterocigotos |
| MY173159A (en) * | 2013-04-11 | 2019-12-31 | Ctc Bio Inc | Tadalafil free base-containing film dosage form containing polyethylene glycol-based polymer and/or vinyl pyrrolidone-based polymer as dispersion stabilizer |
| 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 |
| EP3333165B1 (en) * | 2015-08-04 | 2019-09-18 | Astellas Pharma Inc. | Piperazine derivative |
| ES2985734T3 (es) | 2015-09-30 | 2024-11-07 | Rhythm Pharmaceuticals Inc | Método de tratamiento de trastornos asociados a la vía del receptor de la melanocortina-4 |
| AU2019249255A1 (en) | 2018-04-06 | 2020-11-05 | Alastair GARFIELD | Compositions for treating kidney disease |
| EP3870292A4 (en) | 2018-10-26 | 2022-11-09 | The Research Foundation for The State University of New York | COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE 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 |
| EP0703905A1 (en) * | 1993-06-18 | 1996-04-03 | 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 |
| NZ295353A (en) | 1994-10-27 | 1998-08-26 | Janssen Pharmaceutica Nv | Heterocyclyl-thiomethyl substituted dioxolane derivatives and medicaments compositions thereof |
| US5521186A (en) | 1994-10-27 | 1996-05-28 | Janssen Pharmaceutica N.V. | Apolipoprotein-β synthesis inhibitors |
| US6194413B1 (en) * | 1995-11-13 | 2001-02-27 | Smithkline Beecham Corporation | Hemoregulatory compounds |
| KR20000029984A (ko) * | 1996-08-14 | 2000-05-25 | 사라 엔 람베쓰 | 치환된피리미딘유도체및이의약학적용도 |
| WO1998007692A1 (en) * | 1996-08-17 | 1998-02-26 | 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 |
| WO2000035298A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Chewing gum containing medicament active agents |
| IL141769A0 (en) | 1998-09-11 | 2002-03-10 | Aventis Pharma Sa | Azetidine derivatives, preparation and medicines containing them |
| FR2789079B3 (fr) | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
| MXPA03005388A (es) | 2000-12-14 | 2003-09-25 | Amylin Pharmaceuticals Inc | Peptido yy y agonistas de peptido yy para el tratamiento de desordenes metabolicos. |
| EA200300944A1 (ru) | 2001-02-28 | 2004-04-29 | Мерк Энд Ко., Инк. | Ацилированные пиперидиновые производные в качестве агонистов рецептора-4 меланокортина |
| ES2272703T3 (es) | 2001-02-28 | 2007-05-01 | MERCK & CO., INC. | Derivados de piperidina acilados como agonistas de receptor de melanocortina-4. |
| IL153508A (en) | 2001-03-22 | 2008-07-08 | Solvay Pharm Bv | Derivatives of 4,5 - Dihydro-1H-pyrazole with antagonistic activity to the 1CB receptor |
| US20050015820A1 (en) | 2001-09-24 | 2005-01-20 | Michael Cowley | Assessment of neurons in the arcuate nucleus to screen for agents that modify feeding behavior |
| EP1482794A1 (en) | 2002-03-06 | 2004-12-08 | Merck & Co., Inc. | Method of treatment or prevention of obesity |
| ES2301833T3 (es) | 2002-07-29 | 2008-07-01 | Hoffmann La Roche | Derivados de benzodioxol. |
| ES2294330T3 (es) | 2002-08-02 | 2008-04-01 | MERCK & CO., INC. | Derivados de furo(2,3-b)piridina sustituidos. |
| 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 |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7141669B2 (en) | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod 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 |
| SI1802307T1 (sl) * | 2004-10-15 | 2008-08-31 | Glaxo Group Ltd | Derivati pirolidina kot ligandi histaminskih receptorjev |
| JP5009785B2 (ja) * | 2005-03-25 | 2012-08-22 | キッセイ薬品工業株式会社 | 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 |
| JP2009503050A (ja) | 2005-08-04 | 2009-01-29 | ファイザー・リミテッド | ピペリジノイル−ピロリジンおよびピペリジノイル−ピペリジン化合物 |
-
2009
- 2009-07-30 MX MX2011001405A patent/MX2011001405A/es active IP Right Grant
- 2009-07-30 WO PCT/IB2009/053317 patent/WO2010015972A1/en not_active Ceased
- 2009-07-30 ES ES09786755T patent/ES2421920T3/es active Active
- 2009-07-30 AU AU2009278838A patent/AU2009278838B2/en not_active Ceased
- 2009-07-30 KR KR1020117005275A patent/KR101280786B1/ko not_active Expired - Fee Related
- 2009-07-30 JP JP2011521666A patent/JP5530438B2/ja not_active Expired - Fee Related
- 2009-07-30 US US13/057,319 patent/US8592403B2/en not_active Expired - Fee Related
- 2009-07-30 CA CA2731897A patent/CA2731897C/en not_active Expired - Fee Related
- 2009-07-30 DK DK09786755.0T patent/DK2326638T5/da active
- 2009-07-30 EP EP09786755.0A patent/EP2326638B9/en not_active Not-in-force
- 2009-07-30 CN CN200980139321.7A patent/CN102171206B/zh 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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