AR082600A1 - Polimorfos cristalinos de la sal de besilato de n-(3-(5-fluor-2-(4-(2-metoxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida, composiciones farmaceuticas que los contienen y uso de los mismos para tratar canceres, enfermedades autoinmunes y oseas, entre otras - Google Patents

Polimorfos cristalinos de la sal de besilato de n-(3-(5-fluor-2-(4-(2-metoxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida, composiciones farmaceuticas que los contienen y uso de los mismos para tratar canceres, enfermedades autoinmunes y oseas, entre otras

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Publication number
AR082600A1
AR082600A1 ARP110102882A ARP110102882A AR082600A1 AR 082600 A1 AR082600 A1 AR 082600A1 AR P110102882 A ARP110102882 A AR P110102882A AR P110102882 A ARP110102882 A AR P110102882A AR 082600 A1 AR082600 A1 AR 082600A1
Authority
AR
Argentina
Prior art keywords
crystalline
metoxyetoxi
oseas
polymorphes
pirimidin
Prior art date
Application number
ARP110102882A
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English (en)
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Avila Therapeutics Inc
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Publication date
Application filed by Avila Therapeutics Inc filed Critical Avila Therapeutics Inc
Publication of AR082600A1 publication Critical patent/AR082600A1/es

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    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

Reivindicación 1: Compuesto de fórmula (1).Reivindicación 2: El compuesto de acuerdo con la reivindicación 1, en donde dicho compuesto está en forma sólida. Reivindicación 3: El compuesto de acuerdo con la reivindicación 2, en donde dicho compuesto es cristalino. Reivindicación 4: El compuesto de acuerdo con la reivindicación 3, en donde dicho compuesto es un sólido cristalino sustancialmente libre del compuesto de fórmula (1) amorfo. Reivindicación 6: La forma sólida de acuerdo con la reivindicación 2, en donde dicha forma es la Forma P1. Reivindicación 8: La forma sólida de acuerdo con la reivindicación 7, que posee al menos dos picos en su PXRD seleccionado de aquellos a aproximadamente 6,21, aproximadamente 9,48, y aproximadamente 13,29 grados 2-q. Reivindicación 10: La forma sólida de acuerdo con la reivindicación 2, en donde dicha forma es la Forma P22. Reivindicación 12: La forma sólida de acuerdo con la reivindicación 11, que posee al menos dos picos en su PXRD seleccionado de aquellos a aproximadamente 7,29, aproximadamente 8,38, y aproximadamente 11,12 grados 2-q.
ARP110102882A 2010-08-10 2011-08-09 Polimorfos cristalinos de la sal de besilato de n-(3-(5-fluor-2-(4-(2-metoxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida, composiciones farmaceuticas que los contienen y uso de los mismos para tratar canceres, enfermedades autoinmunes y oseas, entre otras AR082600A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US37234910P 2010-08-10 2010-08-10

Publications (1)

Publication Number Publication Date
AR082600A1 true AR082600A1 (es) 2012-12-19

Family

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ARP110102882A AR082600A1 (es) 2010-08-10 2011-08-09 Polimorfos cristalinos de la sal de besilato de n-(3-(5-fluor-2-(4-(2-metoxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida, composiciones farmaceuticas que los contienen y uso de los mismos para tratar canceres, enfermedades autoinmunes y oseas, entre otras

Country Status (21)

Country Link
US (2) US8563568B2 (es)
EP (2) EP2603081B1 (es)
JP (1) JP6068340B2 (es)
KR (1) KR20130099040A (es)
CN (2) CN103096716B (es)
AR (1) AR082600A1 (es)
AU (1) AU2011289604C1 (es)
BR (1) BR112013003388A2 (es)
CA (1) CA2807051A1 (es)
DK (1) DK2603081T3 (es)
ES (1) ES2617763T3 (es)
IL (1) IL224271A (es)
MX (1) MX336875B (es)
MY (1) MY160734A (es)
NZ (1) NZ607845A (es)
PT (1) PT2603081T (es)
RU (1) RU2013109393A (es)
SG (1) SG187796A1 (es)
TW (1) TWI533872B (es)
WO (1) WO2012021444A1 (es)
ZA (1) ZA201301802B (es)

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US20140057929A1 (en) 2014-02-27
ZA201301802B (en) 2017-04-26
EP2603081A1 (en) 2013-06-19
RU2013109393A (ru) 2014-09-20
CA2807051A1 (en) 2012-02-16
US9604936B2 (en) 2017-03-28
IL224271A (en) 2017-07-31
SG187796A1 (en) 2013-03-28
JP6068340B2 (ja) 2017-01-25
TWI533872B (zh) 2016-05-21
WO2012021444A8 (en) 2012-05-31
PT2603081T (pt) 2017-01-13
CN103096716B (zh) 2016-03-02
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AU2011289604C1 (en) 2016-04-21
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EP2603081B1 (en) 2016-10-05
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AU2011289604A1 (en) 2013-03-21
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