SG11201909229SA - Crystalline forms of (s)-afoxolaner - Google Patents

Crystalline forms of (s)-afoxolaner

Info

Publication number
SG11201909229SA
SG11201909229SA SG11201909229SA SG11201909229SA SG 11201909229S A SG11201909229S A SG 11201909229SA SG 11201909229S A SG11201909229S A SG 11201909229SA SG 11201909229S A SG11201909229S A SG 11201909229SA
Authority
SG
Singapore
Prior art keywords
international
crystalline forms
pct
duluth
chemin
Prior art date
Application number
Inventor
De Vries Roelof Gorter
Bruno Baillon
Sylvaine Lafont
De Saint Michel Myriam Gay
Stephane Kozlovic
Original Assignee
Boehringer Ingelheim Animal Health Usa Inc
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
Application filed by Boehringer Ingelheim Animal Health Usa Inc filed Critical Boehringer Ingelheim Animal Health Usa Inc
Publication of SG11201909229SA publication Critical patent/SG11201909229SA/en

Links

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
    • A61K31/42Oxazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/04Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Liquid Crystal Substances (AREA)
  • Secondary Cells (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

WO 18/187 6 23 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 11 October 2018 (11.10.2018) WIPO I PCT omit IIl °nolo mono mil (10) International Publication Number WO 2018/187623 Al (51) International Patent Classification: CO7D 261/04 (2006.01) A61P 33/00 (2006.01) A61K 31/42 (2006.01) (21) International Application Number: PCT/US2018/026328 (22) International Filing Date: 05 April 2018 (05.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/482,175 05 April 2017 (05.04.2017) US (71) Applicant: MERIAL, INC. [US/US]; 3239 Satellite Blvd., Duluth, GA 30096 (US). (72) Inventors: GORTER DE VRIES, Roelof, Johannes; 50 Avenue Marcel Merieux, 69290 St. Genis Les 011ieres (FR). BAILLON, Bruno; 9 Chemin De Pierre Grosse, 05300 Le Poet (FR). LAFONT, Sylvaine; 9 Rue Des Romarines, Lieu Dit Les Saiettes, 04160 Chateau-amoux (FR). GAY DE SAINT MICHEL, Myriam; 1 Chemin Du Pra De L'intra, 04310 Peyruis (FR). KOZLOVIC, Stephane; 22 Rue Du Bosquet, 04200 Sisteron (FR). (74) Agent: JARECKI-BLACK, Judy; 3239 Satelite Blvd., Duluth, GA 30096 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, 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, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) (54) Title: CRYSTALLINE FORMS OF (S)-AFOXOLANER CI CF 3 CF 3 (Ia) (57) : The present invention provides crystalline forms of compound of formula (la) and processes of making the crystalline forms. Also provided are compositions comprising the crystalline forms and crystalline forms for treating or preventing parasitic in- fections in an animal.
SG11201909229S 2017-04-05 2018-04-05 Crystalline forms of (s)-afoxolaner SG11201909229SA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762482175P 2017-04-05 2017-04-05
PCT/US2018/026328 WO2018187623A1 (en) 2017-04-05 2018-04-05 Crystalline forms of (s)-afoxolaner

Publications (1)

Publication Number Publication Date
SG11201909229SA true SG11201909229SA (en) 2019-11-28

Family

ID=62092252

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201909229S SG11201909229SA (en) 2017-04-05 2018-04-05 Crystalline forms of (s)-afoxolaner

Country Status (23)

Country Link
US (2) US10662163B2 (en)
EP (1) EP3606911A1 (en)
JP (1) JP7222909B2 (en)
KR (1) KR102612648B1 (en)
CN (1) CN111032634A (en)
AR (1) AR111412A1 (en)
AU (1) AU2018250304B2 (en)
BR (1) BR112019021072A2 (en)
CA (1) CA3059114A1 (en)
CL (1) CL2019002840A1 (en)
CO (1) CO2019011980A2 (en)
EA (1) EA201992360A1 (en)
IL (1) IL269792B (en)
MD (1) MD20190080A2 (en)
MX (1) MX2019011931A (en)
MY (1) MY188420A (en)
PH (1) PH12019502277A1 (en)
SG (1) SG11201909229SA (en)
TW (1) TWI782976B (en)
UA (1) UA125727C2 (en)
UY (1) UY37665A (en)
WO (1) WO2018187623A1 (en)
ZA (1) ZA201906464B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2018250304B2 (en) * 2017-04-05 2022-03-03 Boehringer lngelheim Vetmedica GMBH Crystalline forms of (S)-afoxolaner
WO2021254445A1 (en) * 2020-06-19 2021-12-23 东莞市东阳光仿制药研发有限公司 Crystal form of gaba inhibitor and preparation method therefor

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI412322B (en) 2005-12-30 2013-10-21 Du Pont Isoxazolines for controlling invertebrate pests
TWI430995B (en) * 2007-06-26 2014-03-21 Du Pont Naphthalene isoxazoline invertebrate pest control agents
TWI649303B (en) * 2007-08-17 2019-02-01 杜邦股份有限公司 Compound and method for preparing 4-acetyl-n-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide
DK2576523T3 (en) * 2010-05-27 2016-04-18 Du Pont A crystalline form of 4- [5- [3-chloro-5- (trifluoromethyl) phenyl] -4,5-dihydro-5- (trifluoromethyl) -3-isoxazolyl] -N- [2-oxo-2 - [( 2,2,2-trifluoroethyl) amino] ethyl] - 1-naphthalenecarboxamide
BR122019001738B1 (en) * 2011-09-12 2019-11-05 Merial Inc parasiticidal compositions comprising an isoxazoline active agent and uses thereof
WO2014090918A1 (en) * 2012-12-13 2014-06-19 Novartis Ag Process for the enantiomeric enrichment of diaryloxazoline derivatives
JP2015028006A (en) * 2013-06-27 2015-02-12 日産化学工業株式会社 Crystalline polymorph of isoxazoline compound and method for producing the same
UY36570A (en) * 2015-02-26 2016-10-31 Merial Inc INJECTABLE FORMULATIONS OF PROLONGED ACTION THAT INCLUDE AN ISOXAZOLINE ACTIVE AGENT, METHODS AND USES OF THE SAME
SG10201912724SA (en) * 2015-04-08 2020-02-27 Boehringer Ingelheim Animal Health Usa Inc Extended release injectable formulations comprising an isoxazoline active agent, methods and uses thereof
RS62755B1 (en) 2016-04-06 2022-01-31 Boehringer Ingelheim Animal Health Usa Inc Process for the preparation of enantiomerically enriched isoxazoline compounds - crystalline toluene solvate of (s)-afoxolaner
AU2018250304B2 (en) * 2017-04-05 2022-03-03 Boehringer lngelheim Vetmedica GMBH Crystalline forms of (S)-afoxolaner

Also Published As

Publication number Publication date
UY37665A (en) 2018-10-31
UA125727C2 (en) 2022-05-25
US10662163B2 (en) 2020-05-26
AU2018250304A1 (en) 2019-10-31
MD20190080A2 (en) 2020-04-30
WO2018187623A1 (en) 2018-10-11
JP7222909B2 (en) 2023-02-15
CN111032634A (en) 2020-04-17
US11130739B2 (en) 2021-09-28
US20200270219A1 (en) 2020-08-27
WO2018187623A8 (en) 2019-10-24
MY188420A (en) 2021-12-08
IL269792B (en) 2022-04-01
MX2019011931A (en) 2020-01-13
TW201841895A (en) 2018-12-01
CL2019002840A1 (en) 2020-01-10
KR102612648B1 (en) 2023-12-11
AU2018250304B2 (en) 2022-03-03
EA201992360A1 (en) 2020-09-02
ZA201906464B (en) 2021-08-25
JP2020513010A (en) 2020-04-30
IL269792A (en) 2019-11-28
KR20190136055A (en) 2019-12-09
CA3059114A1 (en) 2018-10-11
TWI782976B (en) 2022-11-11
CO2019011980A2 (en) 2020-02-18
EP3606911A1 (en) 2020-02-12
BR112019021072A2 (en) 2020-05-12
PH12019502277A1 (en) 2020-09-14
AR111412A1 (en) 2019-07-10
US20180354917A1 (en) 2018-12-13

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