JP2013010790A5 - - Google Patents
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- Publication number
- JP2013010790A5 JP2013010790A5 JP2012223526A JP2012223526A JP2013010790A5 JP 2013010790 A5 JP2013010790 A5 JP 2013010790A5 JP 2012223526 A JP2012223526 A JP 2012223526A JP 2012223526 A JP2012223526 A JP 2012223526A JP 2013010790 A5 JP2013010790 A5 JP 2013010790A5
- Authority
- JP
- Japan
- Prior art keywords
- acid
- solvate
- pharmaceutically acceptable
- methylpropyl
- dimethyl
- 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
- 239000012453 solvate Substances 0.000 claims 10
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 9
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 9
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 6
- -1 2-indanyl Chemical group 0.000 claims 5
- 239000002253 acid Substances 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- LCTONWCANYUPML-UHFFFAOYSA-N Pyruvic acid Chemical compound CC(=O)C(O)=O LCTONWCANYUPML-UHFFFAOYSA-N 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- 229940077476 2,5-piperazinedione Drugs 0.000 claims 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 1
- 229940092714 benzenesulfonic acid Drugs 0.000 claims 1
- BEWUOCYETMDWGE-FKDQZALLSA-N benzenesulfonic acid;(3r,6r)-6-[(2s)-butan-2-yl]-3-(2,3-dihydro-1h-inden-2-yl)-1-[(1r)-1-(2,6-dimethylpyridin-3-yl)-2-morpholin-4-yl-2-oxoethyl]piperazine-2,5-dione Chemical compound OS(=O)(=O)C1=CC=CC=C1.O=C([C@H](N1[C@@H](C(N[C@@H](C1=O)C1CC2=CC=CC=C2C1)=O)[C@@H](C)CC)C=1C(=NC(C)=CC=1)C)N1CCOCC1 BEWUOCYETMDWGE-FKDQZALLSA-N 0.000 claims 1
- UJJWWBIBTKGJEO-FVBWLAGSSA-N benzenesulfonic acid;(3r,6r)-6-[(2s)-butan-2-yl]-3-(2,3-dihydro-1h-inden-2-yl)-1-[(1r)-1-(2,6-dimethylpyridin-3-yl)-2-morpholin-4-yl-2-oxoethyl]piperazine-2,5-dione;hydrate Chemical compound O.OS(=O)(=O)C1=CC=CC=C1.O=C([C@H](N1[C@@H](C(N[C@@H](C1=O)C1CC2=CC=CC=C2C1)=O)[C@@H](C)CC)C=1C(=NC(C)=CC=1)C)N1CCOCC1 UJJWWBIBTKGJEO-FVBWLAGSSA-N 0.000 claims 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 1
- 235000015165 citric acid Nutrition 0.000 claims 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
- 239000001530 fumaric acid Substances 0.000 claims 1
- 239000004310 lactic acid Substances 0.000 claims 1
- 235000014655 lactic acid Nutrition 0.000 claims 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 1
- 239000011976 maleic acid Substances 0.000 claims 1
- 229940098779 methanesulfonic acid Drugs 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 229940107700 pyruvic acid Drugs 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000011975 tartaric acid Substances 0.000 claims 1
- 235000002906 tartaric acid Nutrition 0.000 claims 1
- 0 C[C@](C(N([C@](*)C(*)=O)[C@]1*)=O)NC1=O Chemical compound C[C@](C(N([C@](*)C(*)=O)[C@]1*)=O)NC1=O 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0414093.5 | 2004-06-23 | ||
| GBGB0414093.5A GB0414093D0 (en) | 2004-06-23 | 2004-06-23 | Novel compounds |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007517197A Division JP5405019B2 (ja) | 2004-06-23 | 2005-06-21 | オキシトシン受容体アンタゴニストとしてのピペラジンジオン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013010790A JP2013010790A (ja) | 2013-01-17 |
| JP2013010790A5 true JP2013010790A5 (enExample) | 2014-03-27 |
| JP5503709B2 JP5503709B2 (ja) | 2014-05-28 |
Family
ID=32800053
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007517197A Expired - Fee Related JP5405019B2 (ja) | 2004-06-23 | 2005-06-21 | オキシトシン受容体アンタゴニストとしてのピペラジンジオン |
| JP2012223526A Expired - Fee Related JP5503709B2 (ja) | 2004-06-23 | 2012-10-05 | オキシトシン受容体アンタゴニストとしてのピペラジンジオン |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007517197A Expired - Fee Related JP5405019B2 (ja) | 2004-06-23 | 2005-06-21 | オキシトシン受容体アンタゴニストとしてのピペラジンジオン |
Country Status (30)
| Country | Link |
|---|---|
| US (9) | US7550462B2 (enExample) |
| EP (2) | EP1758886B1 (enExample) |
| JP (2) | JP5405019B2 (enExample) |
| KR (1) | KR101186447B1 (enExample) |
| CN (1) | CN1972924B (enExample) |
| AR (1) | AR049405A1 (enExample) |
| AU (1) | AU2005256470B2 (enExample) |
| BR (1) | BRPI0512376A (enExample) |
| CA (1) | CA2571527C (enExample) |
| CY (1) | CY1116183T1 (enExample) |
| DK (1) | DK1758886T3 (enExample) |
| ES (1) | ES2537801T3 (enExample) |
| GB (1) | GB0414093D0 (enExample) |
| HK (1) | HK1208669A1 (enExample) |
| HR (1) | HRP20150401T1 (enExample) |
| HU (1) | HUE025869T2 (enExample) |
| IL (2) | IL179905A0 (enExample) |
| MA (1) | MA28675B1 (enExample) |
| MX (1) | MXPA06014545A (enExample) |
| MY (1) | MY143578A (enExample) |
| NO (1) | NO338769B1 (enExample) |
| NZ (1) | NZ551733A (enExample) |
| PE (1) | PE20060477A1 (enExample) |
| PL (1) | PL1758886T3 (enExample) |
| PT (1) | PT1758886E (enExample) |
| RU (1) | RU2382038C2 (enExample) |
| SI (1) | SI1758886T1 (enExample) |
| TW (1) | TWI348466B (enExample) |
| WO (1) | WO2006000399A1 (enExample) |
| ZA (1) | ZA200610022B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0130677D0 (en) | 2001-12-21 | 2002-02-06 | Glaxo Group Ltd | Medicaments and novel compounds |
| ES2397327T3 (es) | 2002-06-17 | 2013-03-06 | Thrasos, Inc. | Compuestos asociados a un dominio único de TDF y análogos de los mismos |
| GB0314738D0 (en) | 2003-06-24 | 2003-07-30 | Glaxo Group Ltd | Novel compounds |
| AU2005265098B2 (en) | 2004-06-17 | 2012-02-23 | Thrasos Innovation, Inc. | TDF-related compounds and analogs thereof |
| GB0414100D0 (en) * | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0414093D0 (en) * | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| HUE026634T2 (en) | 2005-09-20 | 2016-07-28 | Thrasos Innovation Inc | TDF-related compounds and analogues thereof |
| US8716286B2 (en) | 2009-10-30 | 2014-05-06 | Glaxo Group Limited | Crystalline forms of (3R, 6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione |
| AU2017205254B2 (en) | 2016-01-04 | 2021-05-20 | Xoma (Us) Lcc | Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof |
| WO2017203012A1 (en) * | 2016-05-27 | 2017-11-30 | Glaxosmithkline Intellectual Property (No.2) Limited | Epelsiban for use in the treatment of adenomyosis |
| WO2018015497A2 (en) | 2016-07-21 | 2018-01-25 | ObsEva S.A. | Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage |
| RU2762019C1 (ru) * | 2018-05-29 | 2021-12-14 | Као Корпорейшн | Способ оценки функциональной способности листа вызывать ощущение комфорта и лист, вызывающий ощущение комфорта |
| EP4595974A3 (en) | 2018-10-22 | 2025-08-13 | William D. Carlson | Therapeutic combinations of tdfrps and additional agents and methods of use |
| CN114667141A (zh) | 2019-09-03 | 2022-06-24 | 奥布赛瓦股份公司 | 用于促进胚胎移植和预防流产的催产素拮抗剂给药方案 |
| WO2021160597A1 (en) | 2020-02-10 | 2021-08-19 | ObsEva S.A. | Biomarkers for oxytocin receptor antagonist therapy |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4596819A (en) | 1984-01-23 | 1986-06-24 | Warner-Lambert Company | Modified tripeptides |
| DE3830096A1 (de) | 1988-09-03 | 1990-03-15 | Hoechst Ag | Piperazindione mit psychotroper wirkung |
| US5464788A (en) | 1994-03-24 | 1995-11-07 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| US5817751A (en) | 1994-06-23 | 1998-10-06 | Affymax Technologies N.V. | Method for synthesis of diketopiperazine and diketomorpholine derivatives |
| GB2326639A (en) | 1997-06-18 | 1998-12-30 | Merck & Co Inc | Piperazine Oxytocin Receptor Antagonists |
| HUP0101810A3 (en) | 1998-01-27 | 2002-05-28 | Aventis Pharm Prod Inc | Substituted oxoazaheterocyclyl factor xa inhibitors and pharmaceutical compositions containing them |
| JP2002501944A (ja) | 1998-01-29 | 2002-01-22 | アヴェンティス ファーマシューティカルズ プロダクツ インコーポレイテッド | N−[(脂肪族又は芳香族)カルボニル]−2−アミノアセトアミド化合物及び環化化合物の製造方法 |
| EP1070084A4 (en) | 1998-03-16 | 2001-09-12 | Ontogen Corp | PIPERAZINE AS INHIBITORS OF FRUKTOSE-1,6-BISPHOSPHATASE (FBPASE) |
| GB0130677D0 (en) * | 2001-12-21 | 2002-02-06 | Glaxo Group Ltd | Medicaments and novel compounds |
| GB0314738D0 (en) * | 2003-06-24 | 2003-07-30 | Glaxo Group Ltd | Novel compounds |
| GB0314733D0 (en) * | 2003-06-24 | 2003-07-30 | Glaxo Group Ltd | Medicaments |
| GB0414092D0 (en) | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0414100D0 (en) | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0414093D0 (en) * | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| GB0428235D0 (en) | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
-
2004
- 2004-06-23 GB GBGB0414093.5A patent/GB0414093D0/en not_active Ceased
-
2005
- 2005-06-21 BR BRPI0512376-3A patent/BRPI0512376A/pt not_active Application Discontinuation
- 2005-06-21 KR KR1020067027107A patent/KR101186447B1/ko not_active Expired - Fee Related
- 2005-06-21 WO PCT/EP2005/006760 patent/WO2006000399A1/en not_active Ceased
- 2005-06-21 AU AU2005256470A patent/AU2005256470B2/en not_active Ceased
- 2005-06-21 RU RU2007102274/04A patent/RU2382038C2/ru not_active IP Right Cessation
- 2005-06-21 CA CA2571527A patent/CA2571527C/en not_active Expired - Fee Related
- 2005-06-21 HU HUE05755563A patent/HUE025869T2/en unknown
- 2005-06-21 ES ES05755563.3T patent/ES2537801T3/es not_active Expired - Lifetime
- 2005-06-21 CN CN2005800210140A patent/CN1972924B/zh not_active Expired - Fee Related
- 2005-06-21 PT PT57555633T patent/PT1758886E/pt unknown
- 2005-06-21 SI SI200531963T patent/SI1758886T1/sl unknown
- 2005-06-21 US US11/630,179 patent/US7550462B2/en not_active Expired - Fee Related
- 2005-06-21 NZ NZ551733A patent/NZ551733A/en not_active IP Right Cessation
- 2005-06-21 MX MXPA06014545A patent/MXPA06014545A/es active IP Right Grant
- 2005-06-21 EP EP05755563.3A patent/EP1758886B1/en not_active Expired - Lifetime
- 2005-06-21 JP JP2007517197A patent/JP5405019B2/ja not_active Expired - Fee Related
- 2005-06-21 EP EP15157368.0A patent/EP2918580A1/en not_active Withdrawn
- 2005-06-21 HR HRP20150401TT patent/HRP20150401T1/hr unknown
- 2005-06-21 PL PL05755563T patent/PL1758886T3/pl unknown
- 2005-06-21 MY MYPI20052837A patent/MY143578A/en unknown
- 2005-06-21 AR ARP050102539A patent/AR049405A1/es not_active Application Discontinuation
- 2005-06-21 DK DK05755563T patent/DK1758886T3/da active
- 2005-06-21 TW TW094120517A patent/TWI348466B/zh not_active IP Right Cessation
- 2005-06-22 PE PE2005000714A patent/PE20060477A1/es active IP Right Grant
-
2006
- 2006-11-30 ZA ZA200610022A patent/ZA200610022B/en unknown
- 2006-12-07 IL IL179905A patent/IL179905A0/en not_active IP Right Cessation
- 2006-12-21 MA MA29549A patent/MA28675B1/fr unknown
-
2007
- 2007-01-10 NO NO20070173A patent/NO338769B1/no not_active IP Right Cessation
- 2007-07-23 HK HK15109142.1A patent/HK1208669A1/en unknown
-
2009
- 2009-06-08 US US12/480,182 patent/US20090247541A1/en not_active Abandoned
-
2010
- 2010-08-04 US US12/850,386 patent/US7919492B2/en not_active Expired - Fee Related
-
2011
- 2011-02-25 US US13/035,366 patent/US8202864B2/en not_active Expired - Fee Related
-
2012
- 2012-04-19 US US13/451,196 patent/US20120202811A1/en not_active Abandoned
- 2012-10-05 JP JP2012223526A patent/JP5503709B2/ja not_active Expired - Fee Related
-
2013
- 2013-05-20 US US13/897,853 patent/US8742099B2/en not_active Expired - Fee Related
-
2014
- 2014-04-25 US US14/261,994 patent/US20140235639A1/en not_active Abandoned
-
2015
- 2015-02-16 US US14/623,098 patent/US20150157640A1/en not_active Abandoned
- 2015-03-02 IL IL237513A patent/IL237513A0/en unknown
- 2015-04-08 CY CY20151100339T patent/CY1116183T1/el unknown
- 2015-10-13 US US14/881,322 patent/US9408851B2/en not_active Expired - Fee Related
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