SA517381749B1 - صيغ من 2-(تيرت-بيوتيل أمينو)-4-((1r،3r،4r)-3-هيدروكسي-4-ميثيل سيكلو هكسيل أمينو)-بيريميدين-5-كربوكساميد - Google Patents

صيغ من 2-(تيرت-بيوتيل أمينو)-4-((1r،3r،4r)-3-هيدروكسي-4-ميثيل سيكلو هكسيل أمينو)-بيريميدين-5-كربوكساميد

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Publication number
SA517381749B1
SA517381749B1 SA517381749A SA517381749A SA517381749B1 SA 517381749 B1 SA517381749 B1 SA 517381749B1 SA 517381749 A SA517381749 A SA 517381749A SA 517381749 A SA517381749 A SA 517381749A SA 517381749 B1 SA517381749 B1 SA 517381749B1
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Saudi Arabia
Prior art keywords
methylcyclohexylamino
butylamino
carboxamide
pyrimidine
tert
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SA517381749A
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English (en)
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جوش إندراجيت
زو داوزهونج
هوانج ليانفينج
آندرو بويرسن ناثان
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سيجنال فارماسيتوكالز، ال ال سي
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Publication of SA517381749B1 publication Critical patent/SA517381749B1/ar

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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
    • 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

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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)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

يتعلق الاختراع الحالي بتوفير تركيبات صيدلية وصور جرعة من 2-(تيرت-بيوتيل أمينو)-4-((1R،3R،4R)-3-هيدروكسي-4-ميثيل سيكلو هكسيل أمينو)-بيريميدين-5-كربوكساميد 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide ، أو أيزومر تجاسمي stereoisomer مقبول صيدليًا، مماثل كيميائيtautomer ، صورة صلبة، صورة متعددة الأشكالpolymorph ، ملح، هيدراتhydrate ، مركب مُشبِّكclathrate ، أو ذوّابة solvate من ذلك. يتم أيضًا توفير طرق لعلاج، التعامل مع، أو منع الاضطرابات المتنوعة ، مثل الأمراض diseases أو الاضطرابات القابلة للعلاج disorders treatable أو القابلة للوقاية preventable عن طريق تثبيط مسار pathway JNK في الثدييات باستخدام هذه التركيبات الصيدلية أو صور الجرعة. كما يتم بشكل إضافي توفير أملاح 2-(تيرت-بيوتيل أمينو)-4-((1R،3R،4R)-3-هيدروكسي-4-ميثيل سيكلو هكسيل أمينو)-بيريميدين-5-كربوكساميد 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide وطرق لتحضير هذه الأملاح.
SA517381749A 2014-12-16 2017-06-15 صيغ من 2-(تيرت-بيوتيل أمينو)-4-((1r،3r،4r)-3-هيدروكسي-4-ميثيل سيكلو هكسيل أمينو)-بيريميدين-5-كربوكساميد SA517381749B1 (ar)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462092537P 2014-12-16 2014-12-16
US201562196044P 2015-07-23 2015-07-23
PCT/US2015/065774 WO2016100310A1 (en) 2014-12-16 2015-12-15 Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide

Publications (1)

Publication Number Publication Date
SA517381749B1 true SA517381749B1 (ar) 2021-12-04

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SA517381749A SA517381749B1 (ar) 2014-12-16 2017-06-15 صيغ من 2-(تيرت-بيوتيل أمينو)-4-((1r،3r،4r)-3-هيدروكسي-4-ميثيل سيكلو هكسيل أمينو)-بيريميدين-5-كربوكساميد

Country Status (19)

Country Link
US (3) US9796685B2 (ar)
EP (2) EP3712134B1 (ar)
JP (2) JP6762940B2 (ar)
KR (1) KR102606253B1 (ar)
CN (2) CN112451502B (ar)
AU (2) AU2015362728B2 (ar)
BR (1) BR112017012795A2 (ar)
CA (2) CA3210612A1 (ar)
CL (1) CL2017001545A1 (ar)
CO (1) CO2017006087A2 (ar)
EA (1) EA033530B1 (ar)
EC (1) ECSP17038150A (ar)
ES (1) ES2877642T3 (ar)
IL (1) IL252900B (ar)
MX (2) MX2017007883A (ar)
NZ (1) NZ732793A (ar)
SA (1) SA517381749B1 (ar)
SG (2) SG11201704827UA (ar)
WO (1) WO2016100310A1 (ar)

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JP6903577B2 (ja) 2014-12-16 2021-07-14 シグナル ファーマシューティカルズ，エルエルシー 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法
EA033530B1 (ru) * 2014-12-16 2019-10-31 Signal Pharm Llc Композиции 2-(трет-бутиламино)-4-((1r,3r,4r)-3-гидрокси-4-метилциклогексиламино)пиримидин-5-карбоксамида

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