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 полиморф

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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
Application number
EA201891095A
Other languages
English (en)
Other versions
EA036990B1 (ru
Inventor
Патрик Наксос Пейдж
Маттиас Шварц
Кетрин Жоран-Лебрён
Анна Кваттропани
Винсент Помел
Original Assignee
Мерк Сероно С.А.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from US14/987,586 external-priority patent/US9447055B1/en
Application filed by Мерк Сероно С.А. filed Critical Мерк Сероно С.А.
Publication of EA201891095A1 publication Critical patent/EA201891095A1/ru
Publication of EA036990B1 publication Critical patent/EA036990B1/ru

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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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Emergency Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (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.
EA201891095A 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 EA036990B1 (ru)

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) EP4140988A1 (ru)
JP (5) JP7169573B2 (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) ES2915948T3 (ru)
HR (2) HRP20220673T1 (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) PT3400217T (ru)
RS (2) RS63286B1 (ru)
SG (4) SG11201804594YA (ru)
SI (2) SI3397622T1 (ru)
UA (2) UA125118C2 (ru)
WO (2) WO2017118641A1 (ru)
ZA (1) ZA201903769B (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201804594YA (en) * 2016-01-04 2018-06-28 Merck Serono Sa L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal 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
CN114728013A (zh) * 2019-09-23 2022-07-08 斯坦福大学托管董事会 延长妊娠以及月经或妊娠的并发症的治疗方法

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IL284912B (en) 2022-07-01
PL3400217T3 (pl) 2022-07-04
JP7169573B2 (ja) 2022-11-11
IL284912A (en) 2021-08-31
AU2017205254A1 (en) 2018-08-16
MA43549A (fr) 2021-05-26
LT3400217T (lt) 2022-06-27
PL3397622T3 (pl) 2022-07-04
ZA201903769B (en) 2023-03-29
PT3397622T (pt) 2022-06-15
JP2021178858A (ja) 2021-11-18
AU2021218003A1 (en) 2021-09-02
JP2019500351A (ja) 2019-01-10
EP4140988A1 (en) 2023-03-01
ES2916835T3 (es) 2022-07-06
WO2017118639A1 (en) 2017-07-13
JP7377588B2 (ja) 2023-11-10
CA3009573A1 (en) 2017-07-13
AU2017205670A1 (en) 2018-08-16
DK3397622T3 (en) 2022-06-07
LT3397622T (lt) 2022-06-27
SG11201804789QA (en) 2018-07-30
JP7432284B2 (ja) 2024-02-16
JP6933322B2 (ja) 2021-09-08
AU2021218009B2 (en) 2023-06-22
JP2024012376A (ja) 2024-01-30
HUE058871T2 (hu) 2022-09-28
IL260286B (en) 2022-02-01
DK3400217T3 (da) 2022-06-07
IL260286A (en) 2018-07-31
EA036990B1 (ru) 2021-01-25
JP2019501897A (ja) 2019-01-24
EP4144351A1 (en) 2023-03-08
CA3009576A1 (en) 2017-07-13
IL259742A (en) 2018-07-31
PT3400217T (pt) 2022-06-15
EP3397622A1 (en) 2018-11-07
RS63285B1 (sr) 2022-06-30
SG11201804594YA (en) 2018-06-28
MX2018008304A (es) 2019-01-24
ES2915948T3 (es) 2022-06-27
EP3400217A1 (en) 2018-11-14
EP3397622B1 (en) 2022-03-09
UA125118C2 (uk) 2022-01-12
AU2017205254B2 (en) 2021-05-20
IL259742B (en) 2021-08-31
WO2017118641A1 (en) 2017-07-13
MX2018008157A (es) 2018-09-03
UA125377C2 (uk) 2022-03-02
HRP20220674T1 (hr) 2022-07-22
AU2023233151A1 (en) 2023-10-12
IL289256A (en) 2022-02-01
MA43580A (fr) 2021-05-26
EP3400217B1 (en) 2022-03-09
SI3400217T1 (sl) 2022-07-29
MX2022000154A (es) 2022-02-21
SG10202009723PA (en) 2020-11-27
SI3397622T1 (sl) 2022-07-29
JP2023002668A (ja) 2023-01-10
KR20180099708A (ko) 2018-09-05
HRP20220673T1 (hr) 2022-07-08
CN108779087A (zh) 2018-11-09
KR20180100120A (ko) 2018-09-07
AU2017205670B2 (en) 2021-05-20
RS63286B1 (sr) 2022-06-30
AU2021218009A1 (en) 2021-09-09
HUE058872T2 (hu) 2022-09-28
SG10202009769WA (en) 2020-11-27

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