WO2021188692A1 - Crystalline forms of a farnesoid x receptor agonist - Google Patents

Crystalline forms of a farnesoid x receptor agonist Download PDF

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Publication number
WO2021188692A1
WO2021188692A1 PCT/US2021/022790 US2021022790W WO2021188692A1 WO 2021188692 A1 WO2021188692 A1 WO 2021188692A1 US 2021022790 W US2021022790 W US 2021022790W WO 2021188692 A1 WO2021188692 A1 WO 2021188692A1
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WO
WIPO (PCT)
Prior art keywords
theta
crystalline form
disease
xrpd
crystalline
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2021/022790
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English (en)
French (fr)
Inventor
Nicholas D. Smith
Robert Mansfield
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Metacrine Inc
Original Assignee
Metacrine 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
Priority to EP21770893.2A priority Critical patent/EP4121010A4/en
Priority to MX2022011582A priority patent/MX2022011582A/es
Priority to AU2021236648A priority patent/AU2021236648A1/en
Priority to BR112022018596A priority patent/BR112022018596A2/pt
Priority to JP2022555915A priority patent/JP7664278B2/ja
Priority to CN202180036362.4A priority patent/CN115666521A/zh
Priority to KR1020227036019A priority patent/KR20220155356A/ko
Priority to US17/906,582 priority patent/US12545660B2/en
Priority to IL296532A priority patent/IL296532A/en
Priority to CA3171987A priority patent/CA3171987A1/en
Application filed by Metacrine Inc filed Critical Metacrine Inc
Publication of WO2021188692A1 publication Critical patent/WO2021188692A1/en
Priority to MX2025009319A priority patent/MX2025009319A/es
Anticipated expiration legal-status Critical
Priority to JP2025062686A priority patent/JP2025121901A/ja
Priority to US19/446,296 priority patent/US20260226028A1/en
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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

Definitions

  • thermo-gravimetric analysis TGA substantially similar to the one set forth in Figure i i;
  • the crystalline form of 4-((4-( 1 -(tert-butyl )- 1H-pyrazo1-4- yl)pyridin-2-yl)((4-(4-methoxy-3-methylphenyl)bicyclo[2.2.2]octan-1- yl)methyl)carbamoyl)cyclohexyl 3 -hydroxy azeti dine-trans - 1 -carboxyl ate described herein is administered to the mammal by intravenous administration, subcutaneous administration, oral administration, inhalation, nasal administration, dermal administration, or ophthalmic administration.
  • a method of treating or preventing a liver inflammation in a mammal comprising administering to the mammal a crystalline form of 4-((4- ( 1 -(tert-butyl)-1H-pyrazol-4-yl)pyridin-2-yl)((4-(4-methoxy-3- methylphenyl)bicyclo[2.2.2]octan-1-yl)methyl)carbamoyl)cyclohexyl 3 -hydroxy azeti dine-trans - 1-carboxylate, or a pharmaceutically acceptable salt or solvate thereof.
  • the gastrointestinal disease or condition is necrotizing enterocolitis, gastritis, ulcerative colitis, Crohn’s disease, inflammatory bowel disease, irritable bowel syndrome, gastroenteritis, radiation induced enteritis, pseudomembranous colitis, chemotherapy induced enteritis, gastro-esophageal reflux disease (GERD), peptic ulcer, non-ulcer dyspepsia (NUD), celiac disease, intestinal celiac disease, post-surgical inflammation, gastric carcinogenesis, graft versus host disease or any combination thereof.
  • a method of treating or preventing a disease or condition in a mammal that would benefit from treatment with a FXR agonist comprising administering to the mammal a crystalline form of 4-((4-( 1 -(tert-butyl )- 1H-pyrazo1-4-yl )pyri di n-
  • Figure 6 illustrates a differential scanning calorimetry (DSC) thermogram of Form 2 of crystalline 4-((4-( 1 -(tert-butyl)- 1H-pyrazol-4-yl)pyridin-2-yl)((4-(4-methoxy-3- methylphenyl)bicyclo[2.2.2]octan-1-yl)methyl)carbamoyl)cyclohexyl 3 -hydroxy azeti dine-trans - 1-carboxylate free base.
  • DSC differential scanning calorimetry
  • the activation of FXR also correlates to the secretion of pancreatic polypeptide-fold such as peptide YY (PYY or PYY3-36).
  • peptide YY is a gut hormone peptide that modulates neuronal activity within the hypothalamic and brainstem, regions of the brain involved in reward processing.
  • reduced level of PYY correlates to increased appetite and weight gain.
  • disclosed herein include methods for treating or preventing cholestasis, cirrhosis, primary biliary cirrhosis, non-alcoholic steatohepatitis
  • thermo-gravimetric analysis TGA substantially similar to the one set forth in Figure i i;
  • crystalline Compound 1, Form 4 is characterized as having at least two of the properties selected from (a) to (e). In some embodiments, crystalline Compound 1, Form 4, is characterized as having at least three of the properties selected from (a) to (e). In some embodiments, crystalline Compound 1, Form 4, is characterized as having at least four of the properties selected from (a) to (e). In some embodiments, crystalline Compound 1, Form 4, is characterized as having properties (a) to (e).

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
PCT/US2021/022790 2020-03-18 2021-03-17 Crystalline forms of a farnesoid x receptor agonist Ceased WO2021188692A1 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
IL296532A IL296532A (en) 2020-03-18 2021-03-17 Crystal forms of farnesoid x receptor agonist
AU2021236648A AU2021236648A1 (en) 2020-03-18 2021-03-17 Crystalline forms of a farnesoid X receptor agonist
BR112022018596A BR112022018596A2 (pt) 2020-03-18 2021-03-17 Formas cristalinas de um agonista de receptor farnesoide x
JP2022555915A JP7664278B2 (ja) 2020-03-18 2021-03-17 ファルネソイドｘ受容体アゴニストの結晶質形態
CN202180036362.4A CN115666521A (zh) 2020-03-18 2021-03-17 法尼醇x受体激动剂的结晶形式
KR1020227036019A KR20220155356A (ko) 2020-03-18 2021-03-17 파르네소이드 x 수용체 효능제의 결정형
US17/906,582 US12545660B2 (en) 2020-03-18 2021-03-17 Crystalline forms of a farnesoid X receptor agonist
EP21770893.2A EP4121010A4 (en) 2020-03-18 2021-03-17 Crystalline forms of a farnesoid x receptor agonist
MX2022011582A MX2022011582A (es) 2020-03-18 2021-03-17 Formas cristalinas de un agonista del receptor farnesoide x.
CA3171987A CA3171987A1 (en) 2020-03-18 2021-03-17 Crystalline forms of a farnesoid x receptor agonist
MX2025009319A MX2025009319A (es) 2020-03-18 2022-09-15 Formas cristalinas de un agonista del receptor farnesoide x
JP2025062686A JP2025121901A (ja) 2020-03-18 2025-04-04 ファルネソイドｘ受容体アゴニストの結晶質形態
US19/446,296 US20260226028A1 (en) 2020-03-18 2026-01-12 Crystalline forms of a farnesoid x receptor agonist

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202062991213P 2020-03-18 2020-03-18
US62/991,213 2020-03-18

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US17/906,582 A-371-Of-International US12545660B2 (en) 2020-03-18 2021-03-17 Crystalline forms of a farnesoid X receptor agonist
US19/446,296 Continuation US20260226028A1 (en) 2020-03-18 2026-01-12 Crystalline forms of a farnesoid x receptor agonist

Publications (1)

Publication Number Publication Date
WO2021188692A1 true WO2021188692A1 (en) 2021-09-23

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PCT/US2021/022790 Ceased WO2021188692A1 (en) 2020-03-18 2021-03-17 Crystalline forms of a farnesoid x receptor agonist

Country Status (13)

Country Link
US (2) US12545660B2 (cg-RX-API-DMAC10.html)
EP (1) EP4121010A4 (cg-RX-API-DMAC10.html)
JP (2) JP7664278B2 (cg-RX-API-DMAC10.html)
KR (1) KR20220155356A (cg-RX-API-DMAC10.html)
CN (1) CN115666521A (cg-RX-API-DMAC10.html)
AR (1) AR121596A1 (cg-RX-API-DMAC10.html)
AU (1) AU2021236648A1 (cg-RX-API-DMAC10.html)
BR (1) BR112022018596A2 (cg-RX-API-DMAC10.html)
CA (1) CA3171987A1 (cg-RX-API-DMAC10.html)
IL (1) IL296532A (cg-RX-API-DMAC10.html)
MX (2) MX2022011582A (cg-RX-API-DMAC10.html)
TW (1) TW202144332A (cg-RX-API-DMAC10.html)
WO (1) WO2021188692A1 (cg-RX-API-DMAC10.html)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11773094B2 (en) 2018-09-18 2023-10-03 Organovo, Inc. Farnesoid X receptor agonists and uses thereof
US12491160B2 (en) 2020-03-18 2025-12-09 Eli Lilly And Company Formulations of a farnesoid X receptor agonist
US12545660B2 (en) 2020-03-18 2026-02-10 Eli Lilly And Company Crystalline forms of a farnesoid X receptor agonist

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