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HRP20150026T1 - 8-klor-3-pentil-3,7-dihidro-1h-purin-2,6-dion 2-amino-2-(hidroksimetil)-1,3-propandiol anhidrat za lijeäśenje bolesti - Google Patents

8-klor-3-pentil-3,7-dihidro-1h-purin-2,6-dion 2-amino-2-(hidroksimetil)-1,3-propandiol anhidrat za lijeäśenje bolesti Download PDF

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Publication number
HRP20150026T1
HRP20150026T1 HRP20150026AT HRP20150026T HRP20150026T1 HR P20150026 T1 HRP20150026 T1 HR P20150026T1 HR P20150026A T HRP20150026A T HR P20150026AT HR P20150026 T HRP20150026 T HR P20150026T HR P20150026 T1 HRP20150026 T1 HR P20150026T1
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HR
Croatia
Prior art keywords
compound
compound according
crystalline form
treatment
hydroxymethyl
Prior art date
Application number
HRP20150026AT
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English (en)
Inventor
Holly Esken
Beth Adams Norton
Original Assignee
Glaxosmithkline Llc
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Publication of HRP20150026T1 publication Critical patent/HRP20150026T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/133Amines having hydroxy groups, e.g. sphingosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (14)

1. Spoj, naznačen time što je kristalni 8-klor-3-pentil-3,7-dihidro-1H-purin-2,6-dion tris(hidroksimetil)aminometan anhidrat (Formula (IA): [image]
2. Spoj prema zahtjevu 1, gdje kristalni oblik spoja je naznačen time što XRPD uzorak sadržava sljedeće pikove: [image]
3. Spoj prema bilo kojem od zahtjeva 1 do 2, gdje kristalni oblik spoja je naznačen time što ima XRPD uzorak koji izgleda kao što je prikazano na Slici 2.
4. Spoj prema bilo kojem od zahtjeva 1 do 3 gdje kristalni oblik spoja je naznačen time što ima endotermno taljenje s temperaturom početka taljenja od 212 ± 2 °C u DSC termogramu.
5. Spoj prema bilo kojem od zahtjeva 1 do 4 gdje kristalni oblik spoja je naznačen time što ima sljedeće apsorpcijske pikove u ATR-IR spektru krutog produkta: 3370, 3041, 2946, 2858, 1680, 1656, 1528, 1266, 1243, 1078, 1068, 1049 ± 1 cm-1.
6. Spoj prema bilo kojem od zahtjeva 1 do 5 gdje kristalni oblik spoja je naznačen time što ima ATR infracrveni spektar koji izgleda kao što je prikazano na Slici 6.
7. Kombinacija, naznačena time što sadržava a) spoj kao što je definirano u bilo kojem od prethodnih zahtjeva 1 do 6 i b) jedno ili više terapijski aktivnih sredstava.
8. Spoj kao što je definirano u bilo kojem od zahtjeva 1 do 6, naznačen time što se koristi u terapiji.
9. Spoj prema zahtjevu 8, naznačen time što se upotrebljava za liječenje miješane dislipidemije, dijabetičke dislipidemije ili hiperlipoproteinemije.
10. Spoj prema zahtjevu 8, naznačen time što se upotrebljava za liječenje diabetes mellitus-a tipa II.
11. Spoj prema zahtjevu 8, naznačen time što se upotrebljava za liječenje dijabetičke dislipidemije, miješane dislipidemije, otkazivanja srca, hiperkolesterolemije, kardiovaskularne bolesti, ateroskleroze, arterioskleroze, hipertrigliceridemije, diabetes mellitus-a tipa II, dijabetesa tipa II, otpornosti na inzulin, hiperlipidemije, anoreksije nervose, pretilosti, bolesti koronarnih arterija, tromboze, angine, kroničnog otkazivanja bubrega, periferne vaskularne bolesti ili kapi.
12. Spoj prema zahtjevu 8, naznačen time što se upotrebljava za liječenje multiple skleroze.
13. Farmaceutski pripravak, naznačen time što sadržava: a) spoj kao što je definirano u bilo kojem od zahtjeva 1 do 6 i b) jedan ili više farmaceutski prihvatljivih nosača.
14. Postupak za dobivanje spoja kao što je definirano u bilo kojem od zahtjeva 1 do 6, naznačen time što spomenuti postupak sadržava korak miješanja spoja Formule (A) [image] s tris(hidroksimetil)aminometanom.
HRP20150026AT 2008-12-08 2009-12-07 8-klor-3-pentil-3,7-dihidro-1h-purin-2,6-dion 2-amino-2-(hidroksimetil)-1,3-propandiol anhidrat za lijeäśenje bolesti HRP20150026T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12059608P 2008-12-08 2008-12-08
PCT/US2009/066941 WO2010068581A1 (en) 2008-12-08 2009-12-07 Novel compounds
EP09832421.3A EP2370440B1 (en) 2008-12-08 2009-12-07 8-Chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione 2-amino-2-(hydroxymethyl)-1,3-propanediol anhydrate for the treatment of diseases

Publications (1)

Publication Number Publication Date
HRP20150026T1 true HRP20150026T1 (hr) 2015-02-13

Family

ID=42243044

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20150026AT HRP20150026T1 (hr) 2008-12-08 2009-12-07 8-klor-3-pentil-3,7-dihidro-1h-purin-2,6-dion 2-amino-2-(hidroksimetil)-1,3-propandiol anhidrat za lijeäśenje bolesti

Country Status (22)

Country Link
US (3) US9163024B2 (hr)
EP (1) EP2370440B1 (hr)
JP (1) JP5666464B2 (hr)
KR (1) KR101743783B1 (hr)
CN (1) CN102245606B (hr)
AU (1) AU2009324811B2 (hr)
BR (1) BRPI0922134A2 (hr)
CA (1) CA2746316C (hr)
CY (1) CY1116032T1 (hr)
DK (1) DK2370440T3 (hr)
EA (1) EA020037B1 (hr)
ES (1) ES2527354T3 (hr)
HR (1) HRP20150026T1 (hr)
IL (1) IL213032A (hr)
MX (1) MX2011006022A (hr)
PL (1) PL2370440T3 (hr)
PT (1) PT2370440E (hr)
RS (1) RS53777B1 (hr)
SI (1) SI2370440T1 (hr)
SM (1) SMT201500012B (hr)
WO (1) WO2010068581A1 (hr)
ZA (1) ZA201103397B (hr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1781657E (pt) 2004-02-14 2013-05-23 Glaxosmithkline Ip Dev Ltd Medicamentos com actividade no receptor hm74a
JP2009504592A (ja) 2005-08-10 2009-02-05 スミスクライン・ビーチャム・コーポレイション 選択的hm74aアゴニストとしてのキサンチン誘導体
CA2868033A1 (en) * 2012-03-22 2013-09-26 Transtech Pharma, Llc Tris(hydroxymethyl)aminomethane salts of a small-molecule glp1r agonist and pharmaceutical compositions and uses thereof
AU2024229006A1 (en) * 2023-02-27 2025-09-18 Shanton Pharma Pte. Ltd. Crystal form of 8-chloro-3-pentyl-3,7-dihydro-1h-purin-2,6-dione compound and preparation method therefor

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3657327A (en) * 1970-06-01 1972-04-18 Upjohn Co Prostaglandin salts of tris(hydroxymethyl)aminomethane
US4647585A (en) * 1984-11-08 1987-03-03 E. R. Squibb & Sons, Inc. Bicycloheptane substituted ethers
WO2001043692A2 (en) * 1999-12-15 2001-06-21 Smithkline Beecham Corporation SALTS OF Cis-4-CYANO-4-[3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL]CYCLOHEXANE-1-CARBOXYLIC ACID
US20030013905A1 (en) 2002-06-10 2003-01-16 Huang Guishu Kris Salts of cis-4-cyano-4[3(cyclopentyloxy)-4-methoxyphenyl]cyclohexane-1-carboxylic acid
PT1781657E (pt) 2004-02-14 2013-05-23 Glaxosmithkline Ip Dev Ltd Medicamentos com actividade no receptor hm74a
US20090209561A1 (en) 2004-10-22 2009-08-20 Richard Jonathan Daniel Hatley Xanthine Derivatives with HM74A Receptor Activity
GB0423568D0 (en) * 2004-10-22 2004-11-24 Smithkline Beecham Corp Novel compounds
GB0516464D0 (en) * 2005-08-10 2005-09-14 Smithkline Beecham Corp Novel compounds
JP2009504592A (ja) 2005-08-10 2009-02-05 スミスクライン・ビーチャム・コーポレイション 選択的hm74aアゴニストとしてのキサンチン誘導体

Also Published As

Publication number Publication date
CA2746316A1 (en) 2010-06-17
JP2012511028A (ja) 2012-05-17
KR20110097816A (ko) 2011-08-31
IL213032A0 (en) 2011-07-31
CA2746316C (en) 2017-01-03
US9163024B2 (en) 2015-10-20
EA201170783A1 (ru) 2011-12-30
US20110251218A1 (en) 2011-10-13
RS53777B1 (en) 2015-06-30
BRPI0922134A2 (pt) 2015-08-18
CN102245606A (zh) 2011-11-16
DK2370440T3 (en) 2014-12-08
SMT201500012B (it) 2015-05-03
AU2009324811B2 (en) 2013-01-24
PT2370440E (pt) 2015-01-14
EP2370440A4 (en) 2012-05-30
ZA201103397B (en) 2012-01-25
EP2370440B1 (en) 2014-11-12
CY1116032T1 (el) 2017-01-25
IL213032A (en) 2015-02-26
PL2370440T3 (pl) 2015-05-29
EA020037B1 (ru) 2014-08-29
WO2010068581A1 (en) 2010-06-17
JP5666464B2 (ja) 2015-02-12
EP2370440A1 (en) 2011-10-05
ES2527354T3 (es) 2015-01-22
US20170027945A1 (en) 2017-02-02
MX2011006022A (es) 2011-06-28
KR101743783B1 (ko) 2017-06-05
AU2009324811A1 (en) 2011-06-23
SI2370440T1 (sl) 2015-02-27
CN102245606B (zh) 2014-08-20
US20150366870A1 (en) 2015-12-24

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