EA201891095A1 - Альфа-сложные аминоэфиры производного гидроксипропилтиазолидин карбоксамида и его солевая форма, кристаллический полиморф - Google Patents
Альфа-сложные аминоэфиры производного гидроксипропилтиазолидин карбоксамида и его солевая форма, кристаллический полиморфInfo
- Publication number
- EA201891095A1 EA201891095A1 EA201891095A EA201891095A EA201891095A1 EA 201891095 A1 EA201891095 A1 EA 201891095A1 EA 201891095 A EA201891095 A EA 201891095A EA 201891095 A EA201891095 A EA 201891095A EA 201891095 A1 EA201891095 A1 EA 201891095A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- carboxamide
- complex
- hydroxypropyltiazolidine
- aminoesters
- alpha
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/095—Oxytocins; Vasopressins; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/06—Antiabortive agents; Labour repressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D277/06—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Pregnancy & Childbirth (AREA)
- Gynecology & Obstetrics (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Cephalosporin Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyrrole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Emergency Medicine (AREA)
Abstract
Изобретение обеспечивает α-сложные аминоэфиры производных гидроксипропилтиазолидин карбоксамида формулы (I), (2S)-3-([1,1'-бифенил]-4-илсульфонил)-N-[(1S)-3-гидрокси-1-фенилпропил]-1,3-тиазолидин-2-карбоксамид, а также их соли и кристаллические полиморфы. Соединение ингибирует рецептор простагландина F (PGF2alpha) и полезно для лечения нарушений, таких как преждевременные роды, на ранней гестационной стадии, или дисменореи.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662274674P | 2016-01-04 | 2016-01-04 | |
| US14/987,586 US9447055B1 (en) | 2016-01-04 | 2016-01-04 | α-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof |
| US201662395664P | 2016-09-16 | 2016-09-16 | |
| US201662407918P | 2016-10-13 | 2016-10-13 | |
| PCT/EP2017/050101 WO2017118641A1 (en) | 2016-01-04 | 2017-01-04 | L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201891095A1 true EA201891095A1 (ru) | 2019-01-31 |
| EA036990B1 EA036990B1 (ru) | 2021-01-25 |
Family
ID=57799697
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201891095A EA036990B1 (ru) | 2016-01-04 | 2017-01-04 | (3s)-3-({[(2s)-3-(бифенил-4-илсульфонил)-1,3-тиазолидин-2-ил]карбонил}амино)-3-(4-фторфенил)пропил l-валинат и его солевая форма, кристаллический полиморф |
Country Status (23)
| Country | Link |
|---|---|
| EP (4) | EP4144351A1 (ru) |
| JP (5) | JP6933322B2 (ru) |
| KR (2) | KR20180099708A (ru) |
| CN (1) | CN108779087A (ru) |
| AU (4) | AU2017205670B2 (ru) |
| CA (2) | CA3009573A1 (ru) |
| DK (2) | DK3400217T3 (ru) |
| EA (1) | EA036990B1 (ru) |
| ES (2) | ES2916835T3 (ru) |
| HR (2) | HRP20220674T1 (ru) |
| HU (2) | HUE058871T2 (ru) |
| IL (4) | IL284912B (ru) |
| LT (2) | LT3397622T (ru) |
| MA (2) | MA43580A (ru) |
| MX (3) | MX2018008304A (ru) |
| PL (2) | PL3400217T3 (ru) |
| PT (2) | PT3397622T (ru) |
| RS (2) | RS63286B1 (ru) |
| SG (4) | SG11201804789QA (ru) |
| SI (2) | SI3400217T1 (ru) |
| UA (2) | UA125377C2 (ru) |
| WO (2) | WO2017118641A1 (ru) |
| ZA (1) | ZA201903769B (ru) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL284912B (en) * | 2016-01-04 | 2022-07-01 | Merck Serono Sa | L-Valinate derivative of hydroxypropylthiazolidine carboxamide and salt form, crystalline polymorph thereof |
| RU2711615C1 (ru) * | 2019-09-12 | 2020-01-17 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт акушерства, гинекологии и репродуктологии имени Д.О. Отта" | Способ лечения эндометриоза на основании экспериментальной модели у крыс |
| EP4034129A4 (en) * | 2019-09-23 | 2023-11-01 | The Board of Trustees of the Leland Stanford Junior University | TREATMENT PROCEDURES FOR GESTATIONAL EXTENSION AND FOR MENSTRUAL OR GESTATIONAL COMPLICATIONS |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3835175A (en) | 1971-03-15 | 1974-09-10 | Research Corp | 9-fluorenylmethanol haloformates, carbonates and thiocarbonates |
| US3839396A (en) | 1971-07-15 | 1974-10-01 | Shionogi & Co | 9-lower alkyl-9-fluorenyl carbonates |
| US4108846A (en) | 1977-02-01 | 1978-08-22 | Hoffmann-La Roche Inc. | Solid phase synthesis with base N alpha-protecting group cleavage |
| SE430885B (sv) | 1980-03-24 | 1983-12-19 | Ferring Ab | Oxytocin-derivat |
| US4508657A (en) | 1982-01-19 | 1985-04-02 | Research Corporation | Peptide synthesis and amino acid blocking agents |
| US4581167A (en) | 1982-01-19 | 1986-04-08 | Research Corporation | Peptide synthesis and amino acid blocking agents |
| EP0112809B1 (en) | 1982-12-21 | 1986-05-28 | Ferring AB | Vasotocin derivatives |
| US4460501A (en) | 1983-08-30 | 1984-07-17 | Research Corporation | Process for the synthesis of peptides utilizing thioxanthylmethyloxycarbonyl dioxides |
| US5370135A (en) * | 1993-10-13 | 1994-12-06 | Biex, Inc. | Use of estriol measurement to monitor tocolytic therapy |
| DE4434488A1 (de) * | 1994-09-14 | 1996-03-21 | Schering Ag | Steroidester und -amide, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung |
| SE9604341D0 (sv) | 1996-11-26 | 1996-11-26 | Ferring Bv | Hepta-peptide oxytocin analogue |
| IN188411B (ru) * | 1997-03-27 | 2002-09-21 | Yuhan Corp | |
| AU2001261161A1 (en) * | 2000-05-30 | 2001-12-11 | Ortho-Mcneil Pharmaceutical, Inc. | Dihydropyridine compounds for inhibition of calcium-influx |
| GB0130677D0 (en) | 2001-12-21 | 2002-02-06 | Glaxo Group Ltd | Medicaments and novel compounds |
| ES2277640T3 (es) | 2002-02-27 | 2007-07-16 | Ferring Bv | Productos intermedios y metodos para preparar analogos de heptapeptido de oxitocina. |
| UA78021C2 (en) * | 2002-03-28 | 2007-02-15 | Applied Research Systems | Thiazolidine carboxamide derivatives as modulators of prostaglandine f receptors |
| GB0208785D0 (en) | 2002-04-17 | 2002-05-29 | Medical Res Council | Treatment methtods |
| US7521530B2 (en) | 2002-06-11 | 2009-04-21 | Universite De Montreal | Peptides and peptidomimetics useful for inhibiting the activity of prostaglandin F2α receptor |
| UA78058C2 (en) | 2002-07-05 | 2007-02-15 | Applied Research Systems | Pyrrolidine derivative as oxitocin antagonists |
| AU2003300901A1 (en) * | 2002-12-12 | 2004-06-30 | Idenix (Cayman) Limited | Process for the production of 2'-branched nucleosides |
| GB0314738D0 (en) | 2003-06-24 | 2003-07-30 | Glaxo Group Ltd | Novel compounds |
| GB0414093D0 (en) | 2004-06-23 | 2004-07-28 | Glaxo Group Ltd | Novel compounds |
| WO2011051814A1 (en) | 2009-10-30 | 2011-05-05 | Glaxo Group Limited | Novel 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 |
| 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 |
| WO2015192878A1 (en) | 2014-06-16 | 2015-12-23 | Glaxosmithkline Intellectual Property Development Limited | Retosiban for the treatment of pre-term labour |
| CN106795110A (zh) | 2014-07-02 | 2017-05-31 | 奥布赛瓦股份公司 | 治疗ot‑r活性相关的病症的方法中可用的晶体(3z，5s)‑5‑(羟甲基)‑1‑[(2’‑甲基‑1，1’‑联苯‑4‑基)羰基]吡咯烷‑3‑酮o‑甲基肟 |
| EP3037101B1 (en) | 2014-12-22 | 2019-03-06 | Ferring B.V. | Oxytocin receptor antagonist therapy in the luteal phase for implantation and pregnancy in women undergoing assisted reproductive technologies |
| IL284912B (en) | 2016-01-04 | 2022-07-01 | Merck Serono Sa | L-Valinate derivative of hydroxypropylthiazolidine carboxamide and salt form, crystalline polymorph thereof |
| US9447055B1 (en) * | 2016-01-04 | 2016-09-20 | Merck Serono S.A. | α-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof |
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2017
- 2017-01-04 IL IL284912A patent/IL284912B/en unknown
- 2017-01-04 RS RS20220548A patent/RS63286B1/sr unknown
- 2017-01-04 HR HRP20220674TT patent/HRP20220674T1/hr unknown
- 2017-01-04 PT PT177003910T patent/PT3397622T/pt unknown
- 2017-01-04 SI SI201731161T patent/SI3400217T1/sl unknown
- 2017-01-04 WO PCT/EP2017/050101 patent/WO2017118641A1/en active Application Filing
- 2017-01-04 UA UAA201806074A patent/UA125377C2/uk unknown
- 2017-01-04 HR HRP20220673TT patent/HRP20220673T1/hr unknown
- 2017-01-04 SG SG11201804789QA patent/SG11201804789QA/en unknown
- 2017-01-04 EP EP22153566.9A patent/EP4144351A1/en active Pending
- 2017-01-04 PL PL17700392T patent/PL3400217T3/pl unknown
- 2017-01-04 MA MA043580A patent/MA43580A/fr unknown
- 2017-01-04 LT LTEPPCT/EP2017/050099T patent/LT3397622T/lt unknown
- 2017-01-04 AU AU2017205670A patent/AU2017205670B2/en active Active
- 2017-01-04 EP EP17700391.0A patent/EP3397622B1/en active Active
- 2017-01-04 ES ES17700392T patent/ES2916835T3/es active Active
- 2017-01-04 CN CN201780015011.9A patent/CN108779087A/zh active Pending
- 2017-01-04 LT LTEPPCT/EP2017/050101T patent/LT3400217T/lt unknown
- 2017-01-04 UA UAA201806830A patent/UA125118C2/uk unknown
- 2017-01-04 RS RS20220547A patent/RS63285B1/sr unknown
- 2017-01-04 CA CA3009573A patent/CA3009573A1/en active Pending
- 2017-01-04 SG SG10202009769WA patent/SG10202009769WA/en unknown
- 2017-01-04 EP EP17700392.8A patent/EP3400217B1/en active Active
- 2017-01-04 SG SG11201804594YA patent/SG11201804594YA/en unknown
- 2017-01-04 MA MA043549A patent/MA43549A/fr unknown
- 2017-01-04 AU AU2017205254A patent/AU2017205254B2/en active Active
- 2017-01-04 WO PCT/EP2017/050099 patent/WO2017118639A1/en active Application Filing
- 2017-01-04 SG SG10202009723PA patent/SG10202009723PA/en unknown
- 2017-01-04 DK DK17700392.8T patent/DK3400217T3/da active
- 2017-01-04 EA EA201891095A patent/EA036990B1/ru unknown
- 2017-01-04 KR KR1020187018929A patent/KR20180099708A/ko not_active Application Discontinuation
- 2017-01-04 HU HUE17700392A patent/HUE058871T2/hu unknown
- 2017-01-04 HU HUE17700391A patent/HUE058872T2/hu unknown
- 2017-01-04 JP JP2018529634A patent/JP6933322B2/ja active Active
- 2017-01-04 CA CA3009576A patent/CA3009576A1/en active Pending
- 2017-01-04 JP JP2018529284A patent/JP7169573B2/ja active Active
- 2017-01-04 DK DK17700391.0T patent/DK3397622T3/da active
- 2017-01-04 EP EP22152238.6A patent/EP4140988A1/en active Pending
- 2017-01-04 PT PT177003928T patent/PT3400217T/pt unknown
- 2017-01-04 KR KR1020187018312A patent/KR20180100120A/ko not_active Application Discontinuation
- 2017-01-04 MX MX2018008304A patent/MX2018008304A/es unknown
- 2017-01-04 PL PL17700391T patent/PL3397622T3/pl unknown
- 2017-01-04 ES ES17700391T patent/ES2915948T3/es active Active
- 2017-01-04 SI SI201731162T patent/SI3397622T1/sl unknown
- 2017-01-04 MX MX2018008157A patent/MX2018008157A/es unknown
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2018
- 2018-05-31 IL IL259742A patent/IL259742B/en unknown
- 2018-06-26 IL IL260286A patent/IL260286B/en unknown
- 2018-06-29 MX MX2022000154A patent/MX2022000154A/es unknown
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2019
- 2019-05-24 ZA ZA2019/03769A patent/ZA201903769B/en unknown
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2021
- 2021-08-05 JP JP2021129297A patent/JP7432284B2/ja active Active
- 2021-08-16 AU AU2021218009A patent/AU2021218009B2/en active Active
- 2021-12-22 IL IL289256A patent/IL289256A/en unknown
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2022
- 2022-10-18 JP JP2022166814A patent/JP7377588B2/ja active Active
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2023
- 2023-09-21 AU AU2023233151A patent/AU2023233151A1/en active Pending
- 2023-10-25 JP JP2023183345A patent/JP2024012376A/ja active Pending
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