CA3210612C - Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide - Google Patents

Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide

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Publication number
CA3210612C
CA3210612C CA3210612A CA3210612A CA3210612C CA 3210612 C CA3210612 C CA 3210612C CA 3210612 A CA3210612 A CA 3210612A CA 3210612 A CA3210612 A CA 3210612A CA 3210612 C CA3210612 C CA 3210612C
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Canada
Prior art keywords
compound
salt
weight
ray powder
powder diffraction
Prior art date
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Application number
CA3210612A
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English (en)
French (fr)
Other versions
CA3210612A1 (en
Inventor
Nathan Andrew Boersen
Indrajit Ghosh
Lianfeng Huang
Daozhong Zou
Original Assignee
Signal Pharmaceuticals LLC
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Filing date
Publication date
Application filed by Signal Pharmaceuticals LLC filed Critical Signal Pharmaceuticals LLC
Priority to CA3210612A priority Critical patent/CA3210612C/en
Publication of CA3210612A1 publication Critical patent/CA3210612A1/en
Application granted granted Critical
Publication of CA3210612C publication Critical patent/CA3210612C/en
Active legal-status Critical Current
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Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CA3210612A 2014-12-16 2015-12-15 Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide Active CA3210612C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA3210612A CA3210612C (en) 2014-12-16 2015-12-15 Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201462092537P 2014-12-16 2014-12-16
US62/092,537 2014-12-16
US201562196044P 2015-07-23 2015-07-23
US62/196,044 2015-07-23
CA2970926A CA2970926C (en) 2014-12-16 2015-12-15 Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CA3210612A CA3210612C (en) 2014-12-16 2015-12-15 Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CA2970926A Division CA2970926C (en) 2014-12-16 2015-12-15 Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide

Publications (2)

Publication Number Publication Date
CA3210612A1 CA3210612A1 (en) 2016-06-23
CA3210612C true CA3210612C (en) 2026-04-21

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CA2970926A Active CA2970926C (en) 2014-12-16 2015-12-15 Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide

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Country Status (19)

Country Link
US (3) US9796685B2 (enExample)
EP (2) EP3233809B1 (enExample)
JP (2) JP6762940B2 (enExample)
KR (1) KR102606253B1 (enExample)
CN (2) CN107108524A (enExample)
AU (2) AU2015362728B2 (enExample)
BR (1) BR112017012795A2 (enExample)
CA (2) CA3210612C (enExample)
CL (1) CL2017001545A1 (enExample)
CO (1) CO2017006087A2 (enExample)
EA (1) EA033530B1 (enExample)
EC (1) ECSP17038150A (enExample)
ES (2) ES2972295T3 (enExample)
IL (1) IL252900B (enExample)
MX (2) MX382253B (enExample)
NZ (1) NZ732793A (enExample)
SA (1) SA517381749B1 (enExample)
SG (2) SG11201704827UA (enExample)
WO (1) WO2016100310A1 (enExample)

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WO2016100310A1 (en) 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide
EP3233808B1 (en) * 2014-12-16 2021-07-14 Signal Pharmaceuticals, LLC Medical uses comprising methods for measurement of inhibition of c-jun n-terminal kinase in skin
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WO2016100310A1 (en) * 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide
EP3233808B1 (en) 2014-12-16 2021-07-14 Signal Pharmaceuticals, LLC Medical uses comprising methods for measurement of inhibition of c-jun n-terminal kinase in skin

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Publication number Publication date
JP6762940B2 (ja) 2020-09-30
US20190031619A1 (en) 2019-01-31
BR112017012795A2 (pt) 2018-01-02
US9796685B2 (en) 2017-10-24
NZ771013A (en) 2024-05-31
IL252900A0 (en) 2017-08-31
CL2017001545A1 (es) 2018-02-09
US20160168105A1 (en) 2016-06-16
US10131639B2 (en) 2018-11-20
CA2970926C (en) 2023-10-24
AU2020203497A1 (en) 2020-06-18
US20180009765A1 (en) 2018-01-11
EP3233809A1 (en) 2017-10-25
ES2972295T3 (es) 2024-06-12
JP7022172B2 (ja) 2022-02-17
EP3712134A1 (en) 2020-09-23
NZ732793A (en) 2023-07-28
WO2016100310A1 (en) 2016-06-23
IL252900B (en) 2021-10-31
AU2015362728A1 (en) 2017-07-13
AU2015362728B2 (en) 2020-06-25
EA033530B1 (ru) 2019-10-31
EP3712134B1 (en) 2023-11-29
MX2017007883A (es) 2017-09-05
ECSP17038150A (es) 2017-07-31
US10590089B2 (en) 2020-03-17
CA3210612A1 (en) 2016-06-23
CN112451502B (zh) 2023-10-27
SG10202010389TA (en) 2020-11-27
KR102606253B1 (ko) 2023-11-27
CA2970926A1 (en) 2016-06-23
CN107108524A (zh) 2017-08-29
MX382253B (es) 2025-03-12
EP3233809B1 (en) 2021-04-21
KR20170097037A (ko) 2017-08-25
SA517381749B1 (ar) 2021-12-04
ES2877642T3 (es) 2021-11-17
EP3233809A4 (en) 2018-05-30
JP2020158510A (ja) 2020-10-01
CO2017006087A2 (es) 2017-10-20
EA201791327A1 (ru) 2018-03-30
JP2017537954A (ja) 2017-12-21
CN112451502A (zh) 2021-03-09
MX2021005207A (es) 2021-07-15
SG11201704827UA (en) 2017-07-28
AU2020203497B2 (en) 2022-03-03

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