HRP20201244T1 - Kristalni oblici 2-(tert-butilamino)-4-((1r,3r,4r)-3-hidroksi-4-metilcikloheksilamino)-pirimidin-5-karboksamida - Google Patents

Kristalni oblici 2-(tert-butilamino)-4-((1r,3r,4r)-3-hidroksi-4-metilcikloheksilamino)-pirimidin-5-karboksamida Download PDF

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Publication number
HRP20201244T1
HRP20201244T1 HRP20201244TT HRP20201244T HRP20201244T1 HR P20201244 T1 HRP20201244 T1 HR P20201244T1 HR P20201244T T HRP20201244T T HR P20201244TT HR P20201244 T HRP20201244 T HR P20201244T HR P20201244 T1 HRP20201244 T1 HR P20201244T1
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Croatia
Prior art keywords
crystalline form
liver disorder
fibrotic liver
subject
effective amount
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HRP20201244TT
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English (en)
Inventor
Antonio Christian Ferretti
Hon-Wah Man
Jale Muslehiddinoglu
Jean Xu
Kelvin Hin-Yeong Yong
Marie Georges Beauchamps
Mohit Atul Kothare
Nanfei Zou
Nathan Andrew Boersen
Ying Li
Robert Hilgraf
Mark A. Nagy
Daozhong Zou
Lianfeng Huang
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Signal Pharmaceuticals, Llc
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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=HRP20201244(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Signal Pharmaceuticals, Llc filed Critical Signal Pharmaceuticals, Llc
Publication of HRP20201244T1 publication Critical patent/HRP20201244T1/hr

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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
    • 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
    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Cosmetics (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Claims (4)

1. Kristalni oblik koji sadrži Spoj 1, ili njegov tautomer: [image] koji ima rendgenski uzorak difrakcije praška koji sadrži vrhove pri približno 10.55, 13.61 i 19.84 ° 2θ.
2. Kristalni oblik prema zahtjevu 1 za uporabu u postupku liječenja ili sprječavanja intersticijske plućne fibroze, sistemske skleroze, skleroderme, kronične alograft nefropatije, odbacivanja posrednog antitijela, lupusa, fibrotskog poremećaja jetre, dijabetesa, ili metaboličkog sindroma koji dovodi do fibrotskog poremećaja jetre, postupak sadrži davanje učinkovite količine kristalnog oblika subjektu kojem je to potrebno.
3. Kristalni oblik za uporabu prema zahtjevu 2 u postupku liječenja ili sprječavanja intersticijske plućne fibroze, sistemske skleroze, skleroderme, kronične alograft nefropatije, odbacivanja posrednog antitijela, ili lupusa, postupak sadrži davanje učinkovite količine kristalnog oblika subjektu kojem je to potrebno.
4. Kristalni oblik za uporabu prema zahtjevu 2 u postupku liječenja ili sprječavanja fibrotskog poremećaja jetre, dijabetesa ili metaboličkog sindroma koji vodi do fibrotskog poremećaja jetre, postupak sadrži davanje učinkovite količine kristala subjektu kojem je to potrebno.
HRP20201244TT 2014-01-30 2020-08-07 Kristalni oblici 2-(tert-butilamino)-4-((1r,3r,4r)-3-hidroksi-4-metilcikloheksilamino)-pirimidin-5-karboksamida HRP20201244T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201461933636P 2014-01-30 2014-01-30
US201462025161P 2014-07-16 2014-07-16
PCT/US2015/013412 WO2015116755A2 (en) 2014-01-30 2015-01-29 Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
EP15743503.3A EP3099302B1 (en) 2014-01-30 2015-01-29 Crystalline forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide

Publications (1)

Publication Number Publication Date
HRP20201244T1 true HRP20201244T1 (hr) 2020-11-13

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ID=53678405

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Application Number Title Priority Date Filing Date
HRP20201244TT HRP20201244T1 (hr) 2014-01-30 2020-08-07 Kristalni oblici 2-(tert-butilamino)-4-((1r,3r,4r)-3-hidroksi-4-metilcikloheksilamino)-pirimidin-5-karboksamida

Country Status (31)

Country Link
US (6) US9365524B2 (hr)
EP (2) EP3099302B1 (hr)
JP (3) JP2017504632A (hr)
KR (2) KR20220051440A (hr)
CN (3) CN106163523A (hr)
AU (2) AU2015211036B2 (hr)
BR (2) BR122020003206B1 (hr)
CA (1) CA2938187C (hr)
CL (1) CL2016001927A1 (hr)
CR (1) CR20160346A (hr)
CY (1) CY1123267T1 (hr)
DK (1) DK3099302T3 (hr)
EA (2) EA031671B1 (hr)
ES (1) ES2811834T3 (hr)
HR (1) HRP20201244T1 (hr)
HU (1) HUE051266T2 (hr)
IL (2) IL246931B (hr)
LT (1) LT3099302T (hr)
MX (3) MX2016009989A (hr)
MY (1) MY180020A (hr)
NZ (3) NZ715903A (hr)
PE (1) PE20161437A1 (hr)
PH (1) PH12016501472B1 (hr)
PL (1) PL3099302T3 (hr)
PT (1) PT3099302T (hr)
RS (1) RS60715B1 (hr)
SA (1) SA516371578B1 (hr)
SG (1) SG11201606054SA (hr)
SI (1) SI3099302T1 (hr)
TW (1) TWI631108B (hr)
WO (1) WO2015116755A2 (hr)

Families Citing this family (7)

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CN111499580A (zh) * 2011-04-22 2020-08-07 西格诺药品有限公司 取代的二氨基甲酰胺和二氨基甲腈嘧啶，其组合物，和用其治疗的方法
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EP3233809B1 (en) 2014-12-16 2021-04-21 Signal Pharmaceuticals, LLC Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide
WO2016100308A1 (en) * 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Methods for measurement of inhibition of c-jun n-terminal kinase in skin
EP3250557A4 (en) 2015-01-29 2018-06-20 Signal Pharmaceuticals, LLC Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
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