CA2857155C - Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use - Google Patents

Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use Download PDF

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CA2857155C
CA2857155C CA2857155A CA2857155A CA2857155C CA 2857155 C CA2857155 C CA 2857155C CA 2857155 A CA2857155 A CA 2857155A CA 2857155 A CA2857155 A CA 2857155A CA 2857155 C CA2857155 C CA 2857155C
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compound
weight
pharmaceutical composition
solid
hydroxypropan
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French (fr)
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CA2857155A1 (en
Inventor
Terrence Joseph Connolly
Kevin Joseph Klopfer
William Wei-Hwa Leong
Anil Menon
Amanda Nicole Miklos
Matthew Michael Kreilein
Juan Antonio Gamboa
Jean Xu
Nathan BOERSEN
Ho-Wah Hui
Thomas Lee
Ying Li
Benjamin Cohen
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Signal Pharmaceuticals LLC
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Signal Pharmaceuticals LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (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)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CA2857155A 2011-12-02 2012-11-30 Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use Active CA2857155C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA3125862A CA3125862C (en) 2011-12-02 2012-11-30 PHARMACEUTICAL COMPOSITIONS OF 7-(6-(2-HYDROXYPROPAN-2-YL)PYRIDINE-3-YL)-1-((TRANS)-4-METHOXYCYCLOHEXYL)-3,4-DIHYDROPYRAZINO[2,3-B]PYRAZINE-2(1H)-ONE, RELATED SOLID FORM AND METHODS OF USE

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161566109P 2011-12-02 2011-12-02
US61/566,109 2011-12-02
US201261647288P 2012-05-15 2012-05-15
US61/647,288 2012-05-15
US201261653439P 2012-05-31 2012-05-31
US61/653,439 2012-05-31
US201261670419P 2012-07-11 2012-07-11
US61/670,419 2012-07-11
PCT/US2012/067172 WO2013082344A1 (en) 2011-12-02 2012-11-30 Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA3125862A Division CA3125862C (en) 2011-12-02 2012-11-30 PHARMACEUTICAL COMPOSITIONS OF 7-(6-(2-HYDROXYPROPAN-2-YL)PYRIDINE-3-YL)-1-((TRANS)-4-METHOXYCYCLOHEXYL)-3,4-DIHYDROPYRAZINO[2,3-B]PYRAZINE-2(1H)-ONE, RELATED SOLID FORM AND METHODS OF USE

Publications (2)

Publication Number Publication Date
CA2857155A1 CA2857155A1 (en) 2013-06-06
CA2857155C true CA2857155C (en) 2021-09-21

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Application Number Title Priority Date Filing Date
CA2857155A Active CA2857155C (en) 2011-12-02 2012-11-30 Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
CA3125862A Active CA3125862C (en) 2011-12-02 2012-11-30 PHARMACEUTICAL COMPOSITIONS OF 7-(6-(2-HYDROXYPROPAN-2-YL)PYRIDINE-3-YL)-1-((TRANS)-4-METHOXYCYCLOHEXYL)-3,4-DIHYDROPYRAZINO[2,3-B]PYRAZINE-2(1H)-ONE, RELATED SOLID FORM AND METHODS OF USE

Family Applications After (1)

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CA3125862A Active CA3125862C (en) 2011-12-02 2012-11-30 PHARMACEUTICAL COMPOSITIONS OF 7-(6-(2-HYDROXYPROPAN-2-YL)PYRIDINE-3-YL)-1-((TRANS)-4-METHOXYCYCLOHEXYL)-3,4-DIHYDROPYRAZINO[2,3-B]PYRAZINE-2(1H)-ONE, RELATED SOLID FORM AND METHODS OF USE

Country Status (23)

Country Link
US (1) US9403829B2 (cg-RX-API-DMAC7.html)
EP (1) EP2785325B1 (cg-RX-API-DMAC7.html)
JP (2) JP6076370B2 (cg-RX-API-DMAC7.html)
KR (1) KR102040997B1 (cg-RX-API-DMAC7.html)
CN (1) CN104093398B (cg-RX-API-DMAC7.html)
AU (1) AU2012304276B2 (cg-RX-API-DMAC7.html)
BR (1) BR112014013332B1 (cg-RX-API-DMAC7.html)
CA (2) CA2857155C (cg-RX-API-DMAC7.html)
CO (1) CO6990726A2 (cg-RX-API-DMAC7.html)
EA (1) EA026390B1 (cg-RX-API-DMAC7.html)
EC (1) ECSP14007473A (cg-RX-API-DMAC7.html)
ES (1) ES2694413T3 (cg-RX-API-DMAC7.html)
IL (1) IL232827B (cg-RX-API-DMAC7.html)
IN (1) IN2014CN04037A (cg-RX-API-DMAC7.html)
MX (1) MX363034B (cg-RX-API-DMAC7.html)
MY (1) MY169749A (cg-RX-API-DMAC7.html)
NI (1) NI201400052A (cg-RX-API-DMAC7.html)
PE (1) PE20141696A1 (cg-RX-API-DMAC7.html)
PH (2) PH12014501230A1 (cg-RX-API-DMAC7.html)
SG (2) SG11201402766UA (cg-RX-API-DMAC7.html)
UA (1) UA114496C2 (cg-RX-API-DMAC7.html)
WO (1) WO2013082344A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201403865B (cg-RX-API-DMAC7.html)

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ES2638179T3 (es) 2013-01-16 2017-10-19 Signal Pharmaceuticals, Llc Compuestos de pirrolopirimidina sustituidos, composiciones de los mismos, y métodos de tratamiento con los mismos
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KR20160002792A (ko) * 2013-04-17 2016-01-08 시그날 파마소티칼 엘엘씨 암 치료용 tor 키나제 억제제 및 n-(3-(5-플루오로-2-(4-(2-메톡시에톡시)페닐아미노)피리미딘-4-일아미노)페닐)아크릴아미드를 포함하는 병용 요법
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CN106715427A (zh) 2014-07-14 2017-05-24 西格诺药品有限公司 利用取代的吡咯并嘧啶化合物、其组合物治疗癌症的方法
KR102795129B1 (ko) * 2017-06-22 2025-04-15 셀진 코포레이션 B형 간염 바이러스 감염을 특징으로 하는 간세포 암종의 치료
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