JP2017519015A5 - - Google Patents
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- Publication number
- JP2017519015A5 JP2017519015A5 JP2016573776A JP2016573776A JP2017519015A5 JP 2017519015 A5 JP2017519015 A5 JP 2017519015A5 JP 2016573776 A JP2016573776 A JP 2016573776A JP 2016573776 A JP2016573776 A JP 2016573776A JP 2017519015 A5 JP2017519015 A5 JP 2017519015A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline compound
- compound according
- subject
- methyl
- pyrrolidin
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 27
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 9
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 239000013078 crystal Substances 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 208000006399 Premature Obstetric Labor Diseases 0.000 claims 4
- 206010036600 Premature labour Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000026440 premature labor Diseases 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- 230000004580 weight loss Effects 0.000 claims 4
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 3
- 230000032692 embryo implantation Effects 0.000 claims 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims 3
- 206010000117 Abnormal behaviour Diseases 0.000 claims 2
- 206010003805 Autism Diseases 0.000 claims 2
- 208000020706 Autistic disease Diseases 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000005171 Dysmenorrhea Diseases 0.000 claims 2
- 206010013935 Dysmenorrhoea Diseases 0.000 claims 2
- 201000009273 Endometriosis Diseases 0.000 claims 2
- 102100028139 Oxytocin receptor Human genes 0.000 claims 2
- 101710103206 Oxytocin receptor Proteins 0.000 claims 2
- 208000005107 Premature Birth Diseases 0.000 claims 2
- 206010036590 Premature baby Diseases 0.000 claims 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 2
- 201000001880 Sexual dysfunction Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000017525 heat dissipation Effects 0.000 claims 2
- 208000000509 infertility Diseases 0.000 claims 2
- 230000036512 infertility Effects 0.000 claims 2
- 231100000535 infertility Toxicity 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 206010036596 premature ejaculation Diseases 0.000 claims 2
- 230000010346 psychosocial stress Effects 0.000 claims 2
- 231100000872 sexual dysfunction Toxicity 0.000 claims 2
- 230000011273 social behavior Effects 0.000 claims 2
- 102000004279 Oxytocin receptors Human genes 0.000 claims 1
- 108090000876 Oxytocin receptors Proteins 0.000 claims 1
- OLUJSZLBWZWGJT-KOXKPCSVSA-N [(2s,4e)-2-(hydroxymethyl)-4-methoxyiminopyrrolidin-1-yl]-[4-(2-methylphenyl)phenyl]methanone Chemical compound C1C(=N/OC)/C[C@@H](CO)N1C(=O)C1=CC=C(C=2C(=CC=CC=2)C)C=C1 OLUJSZLBWZWGJT-KOXKPCSVSA-N 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- 238000010908 decantation Methods 0.000 claims 1
- -1 diethyl [(2'-methyl-1,1'-biphenyl -4 -Yl) carbonyl] pyrrolidin-3-one Chemical compound 0.000 claims 1
- 125000004177 diethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 210000001161 mammalian embryo Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 238000000527 sonication Methods 0.000 claims 1
- 238000009987 spinning Methods 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 238000002411 thermogravimetry Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462020076P | 2014-07-02 | 2014-07-02 | |
| US62/020,076 | 2014-07-02 | ||
| PCT/EP2015/062881 WO2016000920A1 (en) | 2014-07-02 | 2015-06-10 | Crystalline (3z,5s)-5-(hydroxymethyl)-1-[(2'-methyl-1,1'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one o-methyloxime useful in methods of treating conditions related to the ot-r activity |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020186785A Division JP2021038236A (ja) | 2014-07-02 | 2020-11-09 | Ot−r活性に関する疾患を治療するための方法に有用な結晶質の(3z,5s)−5−(ヒドロキシメチル)−1−[(2’−メチル−1,1’−ビフェニル−4−イル)カルボニル]ピロリジン−3−オン о−メチルオキシム |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017519015A JP2017519015A (ja) | 2017-07-13 |
| JP2017519015A5 true JP2017519015A5 (OSRAM) | 2018-07-05 |
Family
ID=53434312
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016573776A Pending JP2017519015A (ja) | 2014-07-02 | 2015-06-10 | Ot−r活性に関する疾患を治療するための方法に有用な結晶質の(3z,5s)−5−(ヒドロキシメチル)−1−[(2’−メチル−1,1’−ビフェニル−4−イル)カルボニル]ピロリジン−3−オン о−メチルオキシム |
| JP2020186785A Pending JP2021038236A (ja) | 2014-07-02 | 2020-11-09 | Ot−r活性に関する疾患を治療するための方法に有用な結晶質の(3z,5s)−5−(ヒドロキシメチル)−1−[(2’−メチル−1,1’−ビフェニル−4−イル)カルボニル]ピロリジン−3−オン о−メチルオキシム |
| JP2022184804A Pending JP2023018037A (ja) | 2014-07-02 | 2022-11-18 | Ot-r活性に関する疾患を治療するための方法に有用な結晶質の(3z,5s)-5-(ヒドロキシメチル)-1-[(2’-メチル-1,1’-ビフェニル-4-イル)カルボニル]ピロリジン-3-オン о-メチルオキシム |
| JP2024182585A Pending JP2025013885A (ja) | 2014-07-02 | 2024-10-18 | Ot-r活性に関する疾患を治療するための方法に有用な結晶質の(3z,5s)-5-(ヒドロキシメチル)-1-[(2’-メチル-1,1’-ビフェニル-4-イル)カルボニル]ピロリジン-3-オン о-メチルオキシム |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020186785A Pending JP2021038236A (ja) | 2014-07-02 | 2020-11-09 | Ot−r活性に関する疾患を治療するための方法に有用な結晶質の(3z,5s)−5−(ヒドロキシメチル)−1−[(2’−メチル−1,1’−ビフェニル−4−イル)カルボニル]ピロリジン−3−オン о−メチルオキシム |
| JP2022184804A Pending JP2023018037A (ja) | 2014-07-02 | 2022-11-18 | Ot-r活性に関する疾患を治療するための方法に有用な結晶質の(3z,5s)-5-(ヒドロキシメチル)-1-[(2’-メチル-1,1’-ビフェニル-4-イル)カルボニル]ピロリジン-3-オン о-メチルオキシム |
| JP2024182585A Pending JP2025013885A (ja) | 2014-07-02 | 2024-10-18 | Ot-r活性に関する疾患を治療するための方法に有用な結晶質の(3z,5s)-5-(ヒドロキシメチル)-1-[(2’-メチル-1,1’-ビフェニル-4-イル)カルボニル]ピロリジン-3-オン о-メチルオキシム |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9718772B2 (OSRAM) |
| EP (2) | EP3164384B1 (OSRAM) |
| JP (4) | JP2017519015A (OSRAM) |
| KR (1) | KR102470283B1 (OSRAM) |
| CN (3) | CN114105850A (OSRAM) |
| AU (1) | AU2015283133B2 (OSRAM) |
| CA (1) | CA2953722C (OSRAM) |
| EA (2) | EA031353B1 (OSRAM) |
| ES (1) | ES2774789T3 (OSRAM) |
| IL (1) | IL249652B (OSRAM) |
| MX (1) | MX371068B (OSRAM) |
| UA (1) | UA122210C2 (OSRAM) |
| WO (1) | WO2016000920A1 (OSRAM) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2845850A1 (en) | 2013-09-10 | 2015-03-11 | ObsEva S.A. | Pyrrolidine derivatives as oxytocin/vasopressin V1a receptors antagonists |
| EP2886107A1 (en) | 2013-12-17 | 2015-06-24 | ObsEva S.A. | Oral formulations of pyrrolydine derivatives |
| MX371068B (es) | 2014-07-02 | 2020-01-15 | ObsEva SA | ((3z,5s)-5-(hidroximetil)-1-[(2'-metil-1,1'-bifenil-4-il)carbonil ]pirrolidin-3-ona o-metiloxima cristalina y métodos de uso de la misma. |
| JP6933322B2 (ja) | 2016-01-04 | 2021-09-08 | メルク セローノ エス.エー. | ヒドロキシプロピルチアゾリジンカルボキサミド誘導体のl−バリネート及びその塩形態、結晶多形 |
| CA3031252A1 (en) | 2016-07-21 | 2018-01-25 | ObsEva S.A. | Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage |
| KR20220075340A (ko) * | 2019-09-03 | 2022-06-08 | 옵스에파 에스에이 | 배아 착상을 촉진하고 유산을 예방하기 위한 옥시토신 길항제 투여 요법 |
| JP7083793B2 (ja) * | 2019-09-10 | 2022-06-13 | Jfeケミカル株式会社 | パラターフェニルテトラカルボン酸およびパラターフェニルテトラカルボン酸二無水物の製造方法 |
| AU2021218895A1 (en) | 2020-02-10 | 2022-09-15 | ObsEva S.A. | Biomarkers for oxytocin receptor antagonist therapy |
| EP4313061A4 (en) * | 2021-03-31 | 2025-03-05 | The Board of Trustees of the Leland Stanford Junior University | FORMULATIONS FOR PROLONGATION OF GESTATION AND FOR COMPLICATIONS OF MENSTRUATION OR GESTATION |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| YU120988A (en) | 1988-06-23 | 1990-06-30 | Lek Tovarna Farmacevtskih | Process for preparing new dispersion pills of cimetidine |
| YU183988A (en) | 1988-09-30 | 1990-08-31 | Lek Tovarna Farmacevtskih | Process for preparing dispersion pills of dihydroergotoxine |
| US5089043A (en) | 1989-11-09 | 1992-02-18 | Shionogi & Co., Ltd. | Heterocyclic oxy-phenoxyacetic acid derivatives and their use as herbicides |
| US5889001A (en) | 1993-07-29 | 1999-03-30 | American Cyanamid Company | Tricyclic diazepine vasopressin antagonists and oxytocin antagonists |
| JP3534903B2 (ja) | 1995-06-09 | 2004-06-07 | 鐘淵化学工業株式会社 | 1−[3−クロロ−(2s)−メチルプロピオニル]−ピロリジン−(2s)−カルボン酸の製造方法 |
| GB9603699D0 (en) | 1996-02-21 | 1996-04-17 | Boots Co Plc | Therapeutic composition |
| US6696484B2 (en) | 1997-10-31 | 2004-02-24 | University Of Chicago Office Of Technology And Intellectual Property | Method and compositions for regulation of 5-alpha reductase activity |
| US6329418B1 (en) | 1998-04-14 | 2001-12-11 | The Procter & Gamble Company | Substituted pyrrolidine hydroxamate metalloprotease inhibitors |
| JP4040878B2 (ja) | 1999-12-09 | 2008-01-30 | レキット ベンキーザー ヘルスケア (ユーケイ) リミテッド | 治療薬 |
| CA2401137A1 (en) | 2000-03-27 | 2001-10-11 | Applied Research Systems Ars Holding N.V. | Pharmaceutically active pyrrolidine derivatives as bax inhibitors |
| JP2003528854A (ja) | 2000-03-27 | 2003-09-30 | アプライド リサーチ システムズ エーアールエス ホールディング ナームロゼ フェンノートシャップ | 医薬として活性なピロリジン誘導体 |
| TW536751B (en) | 2000-07-14 | 2003-06-11 | Nitto Denko Corp | Cleaning sheet, conveying member using the same, and substrate processing equipment cleaning method using them |
| DE60226431D1 (de) | 2001-03-20 | 2008-06-19 | Serono Lab | Pyrrolidinesterderivate mit oxytocinmodulierender wirkung |
| KR200245627Y1 (ko) * | 2001-05-15 | 2001-10-15 | 김병두 | 전기 가열부재가 부착된 냄비 |
| AU2002319237B2 (en) | 2001-06-18 | 2008-01-03 | Merck Serono Sa | Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists |
| JP2003192582A (ja) | 2001-12-12 | 2003-07-09 | Merck Patent Gmbh | ナプロキセンナトリウムを含む速放性錠剤 |
| UA78058C2 (en) * | 2002-07-05 | 2007-02-15 | Applied Research Systems | Pyrrolidine derivative as oxitocin antagonists |
| ATE449067T1 (de) | 2003-02-27 | 2009-12-15 | Merck Serono Sa | Pyrrolidin-derivate als oxytocin antagonisten |
| ES2296137T3 (es) | 2004-02-26 | 2008-04-16 | Laboratoires Serono Sa | Metodo para preparar pirrolidin-oximas. |
| GB2411355B (en) | 2004-02-27 | 2006-02-22 | Niche Generics Ltd | Pharmaceutical composition |
| CA2605923C (en) | 2005-05-10 | 2012-07-24 | Ferring International Center Sa. | Use of antagonists of oxytocin and/or vasopressin |
| JP2008189732A (ja) | 2007-02-01 | 2008-08-21 | Fujifilm Corp | セルロースアシレート組成物、セルロースアシレートフィルム、光学補償シート、偏光板および液晶表示装置 |
| PT2572705T (pt) | 2007-10-01 | 2017-11-08 | Lesvi Laboratorios Sl | Comprimidos orodispersíveis |
| US9201077B2 (en) | 2009-07-27 | 2015-12-01 | Colorado State University Research Foundation | Direct enzyme immunoassay for measurement of serum progesterone levels |
| CA2892000A1 (en) | 2012-11-26 | 2014-05-30 | Piotr Pierzynski | Method and system for diagnosing uterine contraction levels using image analysis |
| EP2845850A1 (en) * | 2013-09-10 | 2015-03-11 | ObsEva S.A. | Pyrrolidine derivatives as oxytocin/vasopressin V1a receptors antagonists |
| EP2886107A1 (en) | 2013-12-17 | 2015-06-24 | ObsEva S.A. | Oral formulations of pyrrolydine derivatives |
| MX371068B (es) | 2014-07-02 | 2020-01-15 | ObsEva SA | ((3z,5s)-5-(hidroximetil)-1-[(2'-metil-1,1'-bifenil-4-il)carbonil ]pirrolidin-3-ona o-metiloxima cristalina y métodos de uso de la misma. |
| ES2716862T3 (es) | 2014-12-22 | 2019-06-17 | Ferring Bv | Terapia con antagonistas del receptor de oxitocina en la fase lútea para la implantación y embarazo en mujeres que se someten a tecnologías de reproducción asistida |
-
2015
- 2015-06-10 MX MX2016016751A patent/MX371068B/es active IP Right Grant
- 2015-06-10 CN CN202111228955.9A patent/CN114105850A/zh active Pending
- 2015-06-10 ES ES15730094T patent/ES2774789T3/es active Active
- 2015-06-10 EP EP15730094.8A patent/EP3164384B1/en active Active
- 2015-06-10 UA UAA201700678A patent/UA122210C2/uk unknown
- 2015-06-10 CA CA2953722A patent/CA2953722C/en active Active
- 2015-06-10 EA EA201790080A patent/EA031353B1/ru unknown
- 2015-06-10 EA EA201891873A patent/EA201891873A1/ru unknown
- 2015-06-10 CN CN201580047177.XA patent/CN106795110A/zh active Pending
- 2015-06-10 KR KR1020177001267A patent/KR102470283B1/ko active Active
- 2015-06-10 US US14/735,215 patent/US9718772B2/en active Active
- 2015-06-10 CN CN202111229040.XA patent/CN114105851A/zh active Pending
- 2015-06-10 EP EP19204954.2A patent/EP3753921A1/en active Pending
- 2015-06-10 JP JP2016573776A patent/JP2017519015A/ja active Pending
- 2015-06-10 WO PCT/EP2015/062881 patent/WO2016000920A1/en not_active Ceased
- 2015-06-10 AU AU2015283133A patent/AU2015283133B2/en active Active
-
2016
- 2016-12-19 IL IL249652A patent/IL249652B/en unknown
-
2017
- 2017-05-25 US US15/604,816 patent/US10752583B2/en active Active
-
2020
- 2020-11-09 JP JP2020186785A patent/JP2021038236A/ja active Pending
-
2022
- 2022-11-18 JP JP2022184804A patent/JP2023018037A/ja active Pending
-
2024
- 2024-10-18 JP JP2024182585A patent/JP2025013885A/ja active Pending
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