SG11201903327PA - Crystalline forms of eravacycline - Google Patents

Crystalline forms of eravacycline

Info

Publication number
SG11201903327PA
SG11201903327PA SG11201903327PA SG11201903327PA SG11201903327PA SG 11201903327P A SG11201903327P A SG 11201903327PA SG 11201903327P A SG11201903327P A SG 11201903327PA SG 11201903327P A SG11201903327P A SG 11201903327PA SG 11201903327P A SG11201903327P A SG 11201903327PA
Authority
SG
Singapore
Prior art keywords
international
crystalline forms
structural formula
bis
compound
Prior art date
Application number
SG11201903327PA
Inventor
Danny Lafrance
Philip Hogan
Yansheng Liu
Minsheng He
Chi-Li Chen
John Niu
Original Assignee
Tetraphase Pharmaceuticals 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 Tetraphase Pharmaceuticals Inc filed Critical Tetraphase Pharmaceuticals Inc
Publication of SG11201903327PA publication Critical patent/SG11201903327PA/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • A61K31/65—Tetracyclines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

WO 18/0757 67 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 April 2018 (26.04.2018) WIPO I PCT omit VIII °nolo III o IID 100 1111010 Imo oimIE (10) International Publication Number WO 2018/075767 Al (51) International Patent Classification: C07D 295/15 (2006.01) A61P 35/00 (2006.01) A61K 31/65 (2006.01) A61P 1/00 (2006.01) A61P 31/00 (2006.01) (21) International Application Number: PCT/US2017/057385 (22) International Filing Date: 19 October 2017 (19.10.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/410,230 19 October 2016 (19.10.2016) US (71) Applicant: TETRAPHASE PHARMACEUTICALS, INC. [US/US]; 480 Arsenal Street, Suite 110, Watertown, MA 02472 (US). (72) Inventors; and (71) Applicants: LAFRANCE, Danny [US/US]; 22A Welles- ley Ave., Natick, MA 01760 (US). HOGAN, Philip, C. [US/US]; 437 Washington St., Apt. 1, Brighton, MA 02135 (US). LIU, Yansheng [CN/US]; 8 Ginn Road, Winches- ter, MA 01890 (US). HE, Minsheng [US/US]; 34 Mar- land Street, Andover, MA 01810 (US). CHEN, Chi-Li [CN/US]; 11 Waban Street, Newton, MA 02458 (US). NIU, John [US/US]; 20 Reeves Road, Bedford, MA 01730 (US). (74) Agent: ABELLEIRA, Susan, M. et al.; Foley Hoag LLP, 155 Seapiort Boulevard, Boston, MA 02210-2600 (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). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) Published: — with international search report (Art. 2 I (3)) (54) Title: CRYSTALLINE FORMS OF ERAVACYCLINE S i'. ee_ H 3 C, N ,CH 3 OH sitions comprising crystalline forms of the bis-HCL salt of a compound repre- NH 2 sented by Structural Formula 1 described herein. The crystalline forms of the (57) : The invention relates to crystalline forms of the bis-HCI salt of a compound represented by Structural Formula 1, and pharmaceutical compo- bis-HCI salt of a compound of Structural Formula 1 and compositions com- OH 0 HO O 0 (1), prising the crystalline forms of the compound of Structural Formula 1 provid- ed herein, in particular, crystalline Form I, crystalline Form J, crystalline Form A, and crystalline Form B, or mixtures thereof, can be incorporated into phar- maceutical compositions, which can be used to treat various disorders. Also described herein are methods for preparing the crystalline forms (e.g., Forms I, J, B and A) of the bis-HCI salt of a compound represented by Structural Formula 1.
SG11201903327PA 2016-10-19 2017-10-19 Crystalline forms of eravacycline SG11201903327PA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662410230P 2016-10-19 2016-10-19
PCT/US2017/057385 WO2018075767A1 (en) 2016-10-19 2017-10-19 Crystalline forms of eravacycline

Publications (1)

Publication Number Publication Date
SG11201903327PA true SG11201903327PA (en) 2019-05-30

Family

ID=60263035

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201903327PA SG11201903327PA (en) 2016-10-19 2017-10-19 Crystalline forms of eravacycline

Country Status (15)

Country Link
US (3) US10961190B2 (en)
EP (1) EP3529236B1 (en)
JP (2) JP7492335B2 (en)
KR (2) KR102660864B1 (en)
CN (2) CN110582486B (en)
DK (1) DK3529236T3 (en)
ES (1) ES2978198T3 (en)
HR (1) HRP20240605T1 (en)
HU (1) HUE066360T2 (en)
MA (1) MA46567A (en)
PH (1) PH12019500822A1 (en)
PL (1) PL3529236T4 (en)
SG (1) SG11201903327PA (en)
SI (1) SI3529236T1 (en)
WO (1) WO2018075767A1 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2890673T3 (en) 2012-08-31 2019-03-18 Tetraphase Pharmaceuticals Inc tetracycline
EP3778567A1 (en) 2016-01-22 2021-02-17 Sandoz Ag Crystalline eravacycline bis-hydrochloride
KR102660864B1 (en) * 2016-10-19 2024-04-25 테트라페이즈 파마슈티컬스, 인코포레이티드 Crystalline form of eravacycline
WO2023233397A1 (en) * 2022-05-29 2023-12-07 B. G. Negev Technologies And Applications Ltd., At Ben-Gurion University Eravacycline for treating cancer
CN115006411A (en) * 2022-07-26 2022-09-06 中南大学湘雅医院 Application of eudragit compounds, medicine and preparation method thereof

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