SG11201804594YA - L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof - Google Patents

L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof

Info

Publication number
SG11201804594YA
SG11201804594YA SG11201804594YA SG11201804594YA SG11201804594YA SG 11201804594Y A SG11201804594Y A SG 11201804594YA SG 11201804594Y A SG11201804594Y A SG 11201804594YA SG 11201804594Y A SG11201804594Y A SG 11201804594YA SG 11201804594Y A SG11201804594Y A SG 11201804594YA
Authority
SG
Singapore
Prior art keywords
international
genove
valinate
january
hydroxypropylthiazolidine
Prior art date
Application number
SG11201804594YA
Inventor
Page Patrick Naxos
Matthias Schwarz
Catherine Jorand-Lebrun
Anna Quattropani
Vincent Pomel
Original Assignee
Merck Serono Sa
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 Merck Serono Sa filed Critical Merck Serono Sa
Publication of SG11201804594YA publication Critical patent/SG11201804594YA/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/44221,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/095Oxytocins; Vasopressins; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06Antiabortive agents; Labour repressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04Heterocyclic 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
    • C07D277/06Heterocyclic 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)
  • 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)
  • Cephalosporin Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
  • Emergency Medicine (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -' Organization International Bureau res:0) (43) International Publication Date .... ....r .....) 13 July 2017 (13.07.2017) WI P0 I P CT (10) WO International 1111111111113111111111111111111111111111111111111111111111111111111111111111111111111111 2017/118641 Publication Number Al (51) International Patent Classification: SCHWARZ, Matthias; 43, Rue Philippe Plantamour, C07D 277/06 (2006.01) A61P 15/00 (2006.01) 1201 GenOve (CH). JORAND-LEBRUN, Catherine; A61K 31/426 (2006.01) A61P 15/06 (2006.01) Chef Lieu, 74270 Contamine-Sarzin (FR). QUATTRO- A61K 45/06 (2006.01) PANI, Anna; Rte de Cherie 2, 1207 GenOve (CH). POMEL, Vincent; 228, Chemin du Bois des Presses, (21) International Application Number: PCT/EP2017/050101 74570 Groisy (FR). (74) Agent: KATZAROV S.A.; 19 rue des Epinettes, 1227 (22) International Filing Date: GenOve (CH). 4 January 2017 (04.01.2017) (25) Filing Language: English (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (26) Publication Language: English AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (30) Priority Data: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 14/987,586 4 January 2016 (04.01.2016) US HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, ICH, KN, 62/274,674 4 January 2016 (04.01.2016) US KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, 62/395,664 16 September 2016 (16.09.2016) US MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 62/407,918 13 October 2016 (13.10.2016) US NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (71) Applicant: MERCK SERONO S.A. [CH/CH]; Centre In- RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, dustriel, 1267 Coinsins (CH). TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (72) Inventors: NAXOS PAGE, Patrick; Les Cyclades, Aven- ue de GenOve, 74160 Saint-Julien-en-Genevois (CH). [Continued on next page] (54) Title: L-VALINATE OF HYDROXYPROPYLTHIAZOLIDINE CARBOXAMIDE DERIVATIVE AND SALT FORM, CRYSTAL POLYMORPH THEREOF (57) : The invention the L- provides valinate ester of a hydroxypropylthiazolidine ( I) F derivative formula carboxamide of (I), (2S)- 3-([1,1'-biphenyl]-4-ylsulfony1)-N-[(1S)-3- hydroxy-1- phenylpropy1]-1,3-thiazolidine-2- 0 carboxamide, as well as salts and crystal cA , poly- ip...Nh, s sm morphs thereof. The compound inhibits the ‘\") 4 11 F receptor (PGF2alpha) and is a prostaglandin useful the treatment of such as Irl in disorders preterm labor at the early gestational stage or FIG. 1 dysmennorrhea. 4 -.:-.c.-,=.:.= Il .4t Il - P-- W - .4 Gni - veins)) -- 4\" - Atzwianat i t 4 Ott - $siR$tit4 . , 1 3 3 tan x initash, rn Il it--- , pel i'M lz ves4de-rckinf& p.m 11 C ei O WO 2017/118641 Al MMEDIMOMOIDEIRMEM3011111011001VOIRVOIS (84) Designated States (unless otherwise indicated, for every SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, kind of regional protection available): ARIPO (BW, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, GH, SZ, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, Published: RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, CZ, IT, RS, DE, — LT, SE, with international search report (Art. 21(3))
SG11201804594YA 2016-01-04 2017-01-04 L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof SG11201804594YA (en)

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 (1)

Publication Number Publication Date
SG11201804594YA true SG11201804594YA (en) 2018-06-28

Family

ID=57799697

Family Applications (4)

Application Number Title Priority Date Filing Date
SG11201804789QA SG11201804789QA (en) 2016-01-04 2017-01-04 Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
SG11201804594YA SG11201804594YA (en) 2016-01-04 2017-01-04 L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
SG10202009723PA SG10202009723PA (en) 2016-01-04 2017-01-04 Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
SG10202009769WA SG10202009769WA (en) 2016-01-04 2017-01-04 L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof

Family Applications Before (1)

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SG11201804789QA SG11201804789QA (en) 2016-01-04 2017-01-04 Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof

Family Applications After (2)

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SG10202009723PA SG10202009723PA (en) 2016-01-04 2017-01-04 Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
SG10202009769WA SG10202009769WA (en) 2016-01-04 2017-01-04 L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof

Country Status (23)

Country Link
EP (4) EP4140988A1 (en)
JP (5) JP6933322B2 (en)
KR (2) KR20180100120A (en)
CN (1) CN108779087A (en)
AU (4) AU2017205254B2 (en)
CA (2) CA3009576A1 (en)
DK (2) DK3397622T3 (en)
EA (1) EA036990B1 (en)
ES (2) ES2915948T3 (en)
HR (2) HRP20220673T1 (en)
HU (2) HUE058871T2 (en)
IL (4) IL284912B (en)
LT (2) LT3397622T (en)
MA (2) MA43580A (en)
MX (3) MX2018008157A (en)
PL (2) PL3397622T3 (en)
PT (2) PT3397622T (en)
RS (2) RS63286B1 (en)
SG (4) SG11201804789QA (en)
SI (2) SI3397622T1 (en)
UA (2) UA125377C2 (en)
WO (2) WO2017118641A1 (en)
ZA (1) ZA201903769B (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201804789QA (en) * 2016-01-04 2018-07-30 ObsEva SA Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
RU2711615C1 (en) * 2019-09-12 2020-01-17 Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт акушерства, гинекологии и репродуктологии имени Д.О. Отта" Method of endometriosis treatment based on an experimental model in rats
EP4034129A4 (en) * 2019-09-23 2023-11-01 The Board of Trustees of the Leland Stanford Junior University Methods of treatments to prolong gestation and complications of menstruation or gestation

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Publication number Publication date
RS63285B1 (en) 2022-06-30
HUE058871T2 (en) 2022-09-28
CA3009576A1 (en) 2017-07-13
AU2017205254A1 (en) 2018-08-16
IL259742A (en) 2018-07-31
PT3400217T (en) 2022-06-15
DK3397622T3 (en) 2022-06-07
SI3397622T1 (en) 2022-07-29
EA036990B1 (en) 2021-01-25
AU2017205670B2 (en) 2021-05-20
AU2023233151A1 (en) 2023-10-12
JP2023002668A (en) 2023-01-10
IL260286B (en) 2022-02-01
HRP20220674T1 (en) 2022-07-22
JP7432284B2 (en) 2024-02-16
MX2022000154A (en) 2022-02-21
JP7169573B2 (en) 2022-11-11
MA43549A (en) 2021-05-26
EP3400217A1 (en) 2018-11-14
EA201891095A1 (en) 2019-01-31
JP6933322B2 (en) 2021-09-08
ZA201903769B (en) 2023-03-29
JP2021178858A (en) 2021-11-18
MX2018008157A (en) 2018-09-03
JP2019501897A (en) 2019-01-24
PT3397622T (en) 2022-06-15
IL289256A (en) 2022-02-01
AU2017205670A1 (en) 2018-08-16
HUE058872T2 (en) 2022-09-28
AU2017205254B2 (en) 2021-05-20
EP4144351A1 (en) 2023-03-08
DK3400217T3 (en) 2022-06-07
WO2017118639A1 (en) 2017-07-13
KR20180100120A (en) 2018-09-07
PL3400217T3 (en) 2022-07-04
AU2021218009B2 (en) 2023-06-22
SI3400217T1 (en) 2022-07-29
AU2021218009A1 (en) 2021-09-09
JP2024012376A (en) 2024-01-30
PL3397622T3 (en) 2022-07-04
UA125377C2 (en) 2022-03-02
ES2916835T3 (en) 2022-07-06
KR20180099708A (en) 2018-09-05
JP2019500351A (en) 2019-01-10
MX2018008304A (en) 2019-01-24
EP3397622B1 (en) 2022-03-09
MA43580A (en) 2021-05-26
SG10202009769WA (en) 2020-11-27
JP7377588B2 (en) 2023-11-10
CA3009573A1 (en) 2017-07-13
EP4140988A1 (en) 2023-03-01
UA125118C2 (en) 2022-01-12
IL259742B (en) 2021-08-31
IL284912B (en) 2022-07-01
EP3397622A1 (en) 2018-11-07
AU2021218003A1 (en) 2021-09-02
RS63286B1 (en) 2022-06-30
IL284912A (en) 2021-08-31
SG10202009723PA (en) 2020-11-27
LT3397622T (en) 2022-06-27
HRP20220673T1 (en) 2022-07-08
EP3400217B1 (en) 2022-03-09
WO2017118641A1 (en) 2017-07-13
ES2915948T3 (en) 2022-06-27
SG11201804789QA (en) 2018-07-30
LT3400217T (en) 2022-06-27
IL260286A (en) 2018-07-31
CN108779087A (en) 2018-11-09

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