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 PDFInfo
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- 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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- Prior art keywords
- crystalline form
- liver disorder
- fibrotic liver
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- effective amount
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- QBBRJRLJWXRSHQ-CKYFFXLPSA-N 2-(tert-butylamino)-4-[[(1r,3r,4r)-3-hydroxy-4-methylcyclohexyl]amino]pyrimidine-5-carboxamide Chemical compound C1[C@@H](O)[C@H](C)CC[C@H]1NC1=NC(NC(C)(C)C)=NC=C1C(N)=O QBBRJRLJWXRSHQ-CKYFFXLPSA-N 0.000 title 1
- 230000003176 fibrotic effect Effects 0.000 claims 4
- 208000019423 liver disease Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 206010063209 Chronic allograft nephropathy Diseases 0.000 claims 2
- 201000001200 Crouzon syndrome-acanthosis nigricans syndrome Diseases 0.000 claims 2
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 2
- 206010042953 Systemic sclerosis Diseases 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 229940125904 compound 1 Drugs 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
Classifications
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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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- 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)
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.
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 | |
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 |
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 |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20201244T1 true HRP20201244T1 (hr) | 2020-11-13 |
Family
ID=53678405
Family Applications (1)
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) | EP3738954A1 (hr) |
JP (3) | JP2017504632A (hr) |
KR (2) | KR102505677B1 (hr) |
CN (3) | CN106163523A (hr) |
AU (2) | AU2015211036B2 (hr) |
BR (2) | BR112016017776A8 (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) | PH12016501472A1 (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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MX351754B (es) | 2011-04-22 | 2017-10-27 | Signal Pharm Llc | Pirimidinas sustituidas de diaminocarboxamida y diaminocarbonitrilo, composiciones de las mismas y metodos de tratamiento con las mismas. |
NZ715903A (en) * | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
WO2016100308A1 (en) * | 2014-12-16 | 2016-06-23 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-jun n-terminal kinase in skin |
CA3210612A1 (en) * | 2014-12-16 | 2016-06-23 | Signal Pharmaceuticals, Llc | Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
WO2016123291A1 (en) | 2015-01-29 | 2016-08-04 | Signal Pharmaceuticals, Llc | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
EP3795553B1 (en) | 2015-07-24 | 2024-05-15 | Celgene Corporation | Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein |
CN111934089B (zh) | 2019-05-13 | 2021-10-26 | 华为技术有限公司 | 天线装置及移动终端 |
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