KR20070085702A - Ugt1a1에 의해 대사된 약물의 약력학을 개선시키기위한 아타자나비르의 용도 - Google Patents
Ugt1a1에 의해 대사된 약물의 약력학을 개선시키기위한 아타자나비르의 용도 Download PDFInfo
- Publication number
- KR20070085702A KR20070085702A KR1020077012547A KR20077012547A KR20070085702A KR 20070085702 A KR20070085702 A KR 20070085702A KR 1020077012547 A KR1020077012547 A KR 1020077012547A KR 20077012547 A KR20077012547 A KR 20077012547A KR 20070085702 A KR20070085702 A KR 20070085702A
- Authority
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- South Korea
- Prior art keywords
- alkyl
- compound
- atazanavir
- administered
- amount
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
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- AXRYRYVKAWYZBR-UHFFFAOYSA-N Atazanavir Natural products C=1C=C(C=2N=CC=CC=2)C=CC=1CN(NC(=O)C(NC(=O)OC)C(C)(C)C)CC(O)C(NC(=O)C(NC(=O)OC)C(C)(C)C)CC1=CC=CC=C1 AXRYRYVKAWYZBR-UHFFFAOYSA-N 0.000 title claims abstract description 114
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- 229940045145 uridine Drugs 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 210000003905 vulva Anatomy 0.000 description 1
- 229940009349 vytorin Drugs 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 239000002676 xenobiotic agent Substances 0.000 description 1
- 230000002034 xenobiotic effect Effects 0.000 description 1
- 230000031143 xenobiotic glucuronidation Effects 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
- 229940051223 zetia Drugs 0.000 description 1
Images
Classifications
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (2)
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| US63294504P | 2004-12-03 | 2004-12-03 | |
| US60/632,945 | 2004-12-03 |
Publications (1)
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| KR20070085702A true KR20070085702A (ko) | 2007-08-27 |
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| US (1) | US20070259894A1 (enExample) |
| EP (1) | EP1824957A4 (enExample) |
| JP (1) | JP2008521934A (enExample) |
| KR (1) | KR20070085702A (enExample) |
| CN (1) | CN101068916A (enExample) |
| AU (1) | AU2005311672B2 (enExample) |
| BR (1) | BRPI0518741A2 (enExample) |
| CA (1) | CA2588466A1 (enExample) |
| IL (1) | IL183383A0 (enExample) |
| MX (1) | MX2007006637A (enExample) |
| NO (1) | NO20073403L (enExample) |
| NZ (1) | NZ555215A (enExample) |
| RU (1) | RU2403066C2 (enExample) |
| WO (1) | WO2006060731A2 (enExample) |
| ZA (1) | ZA200703989B (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US7192948B2 (en) | 2004-05-28 | 2007-03-20 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7176196B2 (en) | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7491819B1 (en) | 2004-05-28 | 2009-02-17 | Bristol-Myers Squibb Company | N-[4-Fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide as an HIV integrase inhibitor |
| UA87884C2 (uk) | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| AU2005311714B2 (en) | 2004-12-03 | 2010-09-30 | Merck Sharp & Dohme Corp. | Pharmaceutical composition containing an anti-nucleating agent |
| WO2006060711A2 (en) | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition |
| ES2394952T3 (es) | 2007-06-12 | 2013-02-07 | Concert Pharmaceuticals Inc. | Derivados de axapéptido como inhibidores de la proteasa VIH |
| US20100273203A1 (en) * | 2009-04-23 | 2010-10-28 | Board Of Trustees Of The University Of Arkansas | Methods and compositions for detecting metabolites |
| US8410064B2 (en) * | 2009-08-24 | 2013-04-02 | The Board Of Trustees Of The University Of Arkansas | Classical cannabinoid metabolites and methods of use thereof |
| WO2011026112A1 (en) * | 2009-08-31 | 2011-03-03 | The Board Of Trustees Of The University Of Arkansas | Compositions comprising specific ugt inhibitors and methods of use thereof |
| ES2898348T3 (es) | 2009-10-26 | 2022-03-07 | Merck Sharp & Dohme | Composiciones farmacéuticas sólidas que contienen un inhibidor de la integrasa |
| US8883218B2 (en) * | 2010-03-26 | 2014-11-11 | The Board Of Trustees Of The University Of Arkansas | Anti-cancer nanoparticle compositions and methods of use |
| US9095598B2 (en) | 2010-12-28 | 2015-08-04 | The Board Of Trustees Of The University Of Arkansas | Stilbenoid derivatives and their uses |
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| US5849911A (en) * | 1996-04-22 | 1998-12-15 | Novartis Finance Corporation | Antivirally active heterocyclic azahexane derivatives |
| US6087383A (en) * | 1998-01-20 | 2000-07-11 | Bristol-Myers Squibb Company | Bisulfate salt of HIV protease inhibitor |
| NZ525088A (en) * | 2000-10-12 | 2004-11-26 | Merck & Co Inc | Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors |
| SI1441735T1 (sl) * | 2001-10-26 | 2006-06-30 | Angeletti P Ist Richerche Bio | N-substituirani hidroksipirimidinon-karboksamidniinhibitorji HIV-integraze |
| AU2002334205B2 (en) * | 2001-10-26 | 2007-07-05 | Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa | Dihydroxypyrimidine carboxamide inhibitors of HIV integrase |
| WO2003055494A1 (en) * | 2001-12-21 | 2003-07-10 | Avmax, Inc. | Use of ugt inhibitors to increase bioavailability |
| AU2003292437A1 (en) * | 2002-12-27 | 2004-07-22 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | Tetrahydro-4h-pyrido(1,2-a)pyrimidines and related compounds useful as hiv integrase inhibitors |
| US20040192624A1 (en) * | 2003-03-24 | 2004-09-30 | Kempf Dale J. | Method for treating a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate |
| UA87884C2 (uk) * | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| AU2005311714B2 (en) * | 2004-12-03 | 2010-09-30 | Merck Sharp & Dohme Corp. | Pharmaceutical composition containing an anti-nucleating agent |
| WO2006060711A2 (en) * | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition |
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2005
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- 2005-12-02 WO PCT/US2005/043782 patent/WO2006060731A2/en not_active Ceased
- 2005-12-02 NZ NZ555215A patent/NZ555215A/en not_active IP Right Cessation
- 2005-12-02 CN CNA2005800413696A patent/CN101068916A/zh active Pending
- 2005-12-02 MX MX2007006637A patent/MX2007006637A/es unknown
- 2005-12-02 KR KR1020077012547A patent/KR20070085702A/ko not_active Withdrawn
- 2005-12-02 EP EP05852867A patent/EP1824957A4/en not_active Withdrawn
- 2005-12-02 CA CA002588466A patent/CA2588466A1/en not_active Abandoned
- 2005-12-02 US US11/792,189 patent/US20070259894A1/en not_active Abandoned
- 2005-12-02 JP JP2007544571A patent/JP2008521934A/ja not_active Withdrawn
- 2005-12-02 AU AU2005311672A patent/AU2005311672B2/en not_active Ceased
- 2005-12-02 RU RU2007125130/15A patent/RU2403066C2/ru not_active IP Right Cessation
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2007
- 2007-05-17 ZA ZA200703989A patent/ZA200703989B/xx unknown
- 2007-05-24 IL IL183383A patent/IL183383A0/en unknown
- 2007-07-02 NO NO20073403A patent/NO20073403L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200703989B (en) | 2008-09-25 |
| WO2006060731A2 (en) | 2006-06-08 |
| EP1824957A4 (en) | 2011-02-09 |
| EP1824957A2 (en) | 2007-08-29 |
| AU2005311672A1 (en) | 2006-06-08 |
| CN101068916A (zh) | 2007-11-07 |
| NZ555215A (en) | 2010-08-27 |
| NO20073403L (no) | 2007-08-31 |
| RU2007125130A (ru) | 2009-01-10 |
| US20070259894A1 (en) | 2007-11-08 |
| JP2008521934A (ja) | 2008-06-26 |
| MX2007006637A (es) | 2007-06-19 |
| IL183383A0 (en) | 2007-09-20 |
| CA2588466A1 (en) | 2006-06-08 |
| BRPI0518741A2 (pt) | 2008-12-02 |
| WO2006060731A3 (en) | 2006-09-28 |
| RU2403066C2 (ru) | 2010-11-10 |
| AU2005311672B2 (en) | 2010-07-22 |
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