PE20161437A1 - Formas solidas de 2-(ter-butilamino)-4-((1r,3r,4r)-3-hidroxi-4-metilciclohexilamino)pirimidin-5-carboxamida, composiciones de la misma y metodos para su uso - Google Patents

Formas solidas de 2-(ter-butilamino)-4-((1r,3r,4r)-3-hidroxi-4-metilciclohexilamino)pirimidin-5-carboxamida, composiciones de la misma y metodos para su uso

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Publication number
PE20161437A1
PE20161437A1 PE2016001300A PE2016001300A PE20161437A1 PE 20161437 A1 PE20161437 A1 PE 20161437A1 PE 2016001300 A PE2016001300 A PE 2016001300A PE 2016001300 A PE2016001300 A PE 2016001300A PE 20161437 A1 PE20161437 A1 PE 20161437A1
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PE
Peru
Prior art keywords
carboxamide
hydroxy
pyrimidin
butylamine
ter
Prior art date
Application number
PE2016001300A
Other languages
English (en)
Inventor
Lianfeng Huang
Daozhong Zou
Mark A Nagy
Robert Hilgraf
Ying Li
Nathan Andrew Boersen
Antonio Christian Ferretti
Mohit Atul Kothare
Marie Georges Beauchamps
Kelvin Hin-Yeong Yong
Jean Xu
Jale Muslehiddinoglu
Hon-Wah Man
Nanfei Zou
Original Assignee
Signal Pharm Llc
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53678405&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20161437(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Signal Pharm Llc filed Critical Signal Pharm Llc
Publication of PE20161437A1 publication Critical patent/PE20161437A1/es

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    • 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
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Diabetes (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
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  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicinal Preparation (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se refiere al compuesto cristalino 2-(ter-butilamino)-4-(1R,3R,4R)-3-hidroxi-4-metilciclohexilamino)-pirimidin-5-carboxamida de formula 1 caracterizado por poseer un patron de difraccion en polvo por rayos X que comprende picos con angulos de 2(teta) de: 10.55, 13.61 y 19.84, el cual es un inhibidor de cinasas JNK1 o JNK2 y es util en el tratamiento de fibrosis pulmonar intersticial, esclerosis sistematica, entre otros. Tambien se refiere a un metodo de tratamiento y a un metodo de preparacion de los compuestos intermediarios de formula iv y iii, donde: R1 y R2 son alquilo C1-C8 o cicloalquilo sustituido o no sustituido
PE2016001300A 2014-01-30 2015-01-29 Formas solidas de 2-(ter-butilamino)-4-((1r,3r,4r)-3-hidroxi-4-metilciclohexilamino)pirimidin-5-carboxamida, composiciones de la misma y metodos para su uso PE20161437A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461933636P 2014-01-30 2014-01-30
US201462025161P 2014-07-16 2014-07-16

Publications (1)

Publication Number Publication Date
PE20161437A1 true PE20161437A1 (es) 2017-01-07

Family

ID=53678405

Family Applications (1)

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PE2016001300A PE20161437A1 (es) 2014-01-30 2015-01-29 Formas solidas de 2-(ter-butilamino)-4-((1r,3r,4r)-3-hidroxi-4-metilciclohexilamino)pirimidin-5-carboxamida, composiciones de la misma y metodos para su uso

Country Status (31)

Country Link
US (6) US9365524B2 (es)
EP (2) EP3738954A1 (es)
JP (3) JP2017504632A (es)
KR (2) KR102505677B1 (es)
CN (3) CN106163523A (es)
AU (2) AU2015211036B2 (es)
BR (2) BR112016017776A8 (es)
CA (1) CA2938187C (es)
CL (1) CL2016001927A1 (es)
CR (1) CR20160346A (es)
CY (1) CY1123267T1 (es)
DK (1) DK3099302T3 (es)
EA (2) EA031671B1 (es)
ES (1) ES2811834T3 (es)
HR (1) HRP20201244T1 (es)
HU (1) HUE051266T2 (es)
IL (2) IL246931B (es)
LT (1) LT3099302T (es)
MX (3) MX2016009989A (es)
MY (1) MY180020A (es)
NZ (3) NZ715903A (es)
PE (1) PE20161437A1 (es)
PH (1) PH12016501472A1 (es)
PL (1) PL3099302T3 (es)
PT (1) PT3099302T (es)
RS (1) RS60715B1 (es)
SA (1) SA516371578B1 (es)
SG (1) SG11201606054SA (es)
SI (1) SI3099302T1 (es)
TW (1) TWI631108B (es)
WO (1) WO2015116755A2 (es)

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