CN101068550B - 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂 - Google Patents

含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂 Download PDF

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Publication number
CN101068550B
CN101068550B CN2005800412301A CN200580041230A CN101068550B CN 101068550 B CN101068550 B CN 101068550B CN 2005800412301 A CN2005800412301 A CN 2005800412301A CN 200580041230 A CN200580041230 A CN 200580041230A CN 101068550 B CN101068550 B CN 101068550B
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amount
preparation
compound
compd
poloxamer
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Expired - Fee Related
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Chinese (zh)
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CN101068550A (zh
Inventor
N·普尔卡沃斯
J·R·尼
M·T·克吕安斯
Y·吴
S·A·帕尔卡
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Merck Sharp and Dohme LLC
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Schering Corp
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    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CN2005800412301A 2004-12-03 2005-12-02 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂 Expired - Fee Related CN101068550B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US63294404P 2004-12-03 2004-12-03
US60/632,944 2004-12-03
PCT/US2005/043727 WO2006060711A2 (en) 2004-12-03 2005-12-02 Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition

Publications (2)

Publication Number Publication Date
CN101068550A CN101068550A (zh) 2007-11-07
CN101068550B true CN101068550B (zh) 2011-03-30

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CN2005800412301A Expired - Fee Related CN101068550B (zh) 2004-12-03 2005-12-02 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂

Country Status (16)

Country Link
US (1) US8852632B2 (cg-RX-API-DMAC7.html)
EP (2) EP2586444B1 (cg-RX-API-DMAC7.html)
JP (1) JP5228488B2 (cg-RX-API-DMAC7.html)
KR (1) KR101351059B1 (cg-RX-API-DMAC7.html)
CN (1) CN101068550B (cg-RX-API-DMAC7.html)
AU (1) AU2005311652B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0518781A2 (cg-RX-API-DMAC7.html)
CA (1) CA2588445C (cg-RX-API-DMAC7.html)
ES (1) ES2755273T3 (cg-RX-API-DMAC7.html)
IL (1) IL183615A (cg-RX-API-DMAC7.html)
MX (1) MX2007006635A (cg-RX-API-DMAC7.html)
NO (1) NO20073405L (cg-RX-API-DMAC7.html)
NZ (1) NZ555120A (cg-RX-API-DMAC7.html)
RU (1) RU2382648C2 (cg-RX-API-DMAC7.html)
WO (1) WO2006060711A2 (cg-RX-API-DMAC7.html)
ZA (1) ZA200703866B (cg-RX-API-DMAC7.html)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101068533B (zh) * 2004-12-03 2011-04-27 默沙东公司 含有抗成核剂的药物组合物
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
CA2588466A1 (en) * 2004-12-03 2006-06-08 Merck & Co., Inc. Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1
WO2009009531A2 (en) * 2007-07-09 2009-01-15 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives for the treatment of hiv infections
JP6122639B2 (ja) * 2009-10-26 2017-04-26 メルク・シャープ・エンド・ドーム・コーポレイション インテグラーゼ阻害剤を含有する固形医薬組成物
US8987272B2 (en) * 2010-04-01 2015-03-24 Critical Outcome Technologies Inc. Compounds and method for treatment of HIV
US9107922B2 (en) 2010-07-16 2015-08-18 Concert Pharmaceuticals, Inc. Pyrimidinecarboxamide derivatives
US9968607B2 (en) 2011-04-25 2018-05-15 Hetero Research Foundation Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof
ES2450944T3 (es) * 2011-06-01 2014-03-25 Ratiopharm Gmbh Composición y comprimido que comprenden raltegravir
EP2827845B1 (en) 2012-03-22 2018-12-26 Novo Nordisk A/S Compositions comprising a delivery agent and preparation thereof
WO2014030172A2 (en) * 2012-08-23 2014-02-27 Hetero Research Foundation Pharmaceutical formulations of rufinamide
US9763934B2 (en) * 2014-03-05 2017-09-19 Professional Compounding Centers Of America Synergistic effect of poloxamer-based composition and itraconazole on fungus and yeast
KR102293907B1 (ko) 2015-06-30 2021-08-26 한미약품 주식회사 이리노테칸 함유 경구용 고형제제 및 그 제조방법
CN108610338A (zh) * 2016-12-12 2018-10-02 天津国际生物医药联合研究院 一种嘧啶酮酰胺类化合物的制备方法
US20210290548A1 (en) * 2018-06-06 2021-09-23 Merck Sharp & Dohme Corp. Formulations of raltegravir

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003035077A1 (en) * 2001-10-26 2003-05-01 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
WO2004058756A1 (en) * 2002-12-27 2004-07-15 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
UA56992C2 (uk) * 1995-05-08 2003-06-16 Фармація Енд Апджон Компані <font face="Symbol">a</font>-ПІРИМІДИНТІОАЛКІЛЗАМІЩЕНІ ТА <font face="Symbol">a</font>-ПІРИМІДИНОКСОАЛКІЛЗАМІЩЕНІ СПОЛУКИ
IE970588A1 (en) * 1997-08-01 2000-08-23 Elan Corp Plc Controlled release pharmaceutical compositions containing tiagabine
CN100400042C (zh) * 1999-12-03 2008-07-09 聚合化学股份公司 制备生物利用度改善的麦角生物碱持续释放药物组合物的方法及其组合物
PL366998A1 (en) * 2001-05-03 2005-02-07 F.Hoffmann-La Roche Ag Pharmaceutical dosage form of amorphous nelfinavir mesylate
WO2003017981A1 (en) * 2001-08-29 2003-03-06 Ranbaxy Laboratories Limited Controlled release formulation of clarithromycin or tinidazol
SE0102887D0 (sv) * 2001-08-29 2001-08-29 Astrazeneca Ab New formulation
CA2463975A1 (en) * 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
AU2003220186A1 (en) * 2002-04-10 2003-10-27 Merck And Co., Inc. Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant
DE602004031767D1 (de) 2003-12-31 2011-04-21 Bend Res Inc Stabilisierte pharmazeutische feste zusammensetzungen von arzneimitteln mit geringer löslichkeit, poloxameren und stabilisierenden polymeren
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
CA2588466A1 (en) 2004-12-03 2006-06-08 Merck & Co., Inc. Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1
CN101068533B (zh) * 2004-12-03 2011-04-27 默沙东公司 含有抗成核剂的药物组合物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003035077A1 (en) * 2001-10-26 2003-05-01 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
WO2004058756A1 (en) * 2002-12-27 2004-07-15 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors

Also Published As

Publication number Publication date
KR20070085695A (ko) 2007-08-27
JP2008521932A (ja) 2008-06-26
MX2007006635A (es) 2007-06-19
WO2006060711A2 (en) 2006-06-08
ES2755273T3 (es) 2020-04-22
IL183615A (en) 2013-01-31
EP1904067A2 (en) 2008-04-02
CN101068550A (zh) 2007-11-07
KR101351059B1 (ko) 2014-02-17
EP1904067B1 (en) 2013-11-20
JP5228488B2 (ja) 2013-07-03
CA2588445C (en) 2013-06-25
IL183615A0 (en) 2007-10-31
US20070292504A1 (en) 2007-12-20
WO2006060711A3 (en) 2006-09-08
CA2588445A1 (en) 2006-06-08
BRPI0518781A2 (pt) 2008-12-09
NZ555120A (en) 2009-11-27
EP2586444A1 (en) 2013-05-01
AU2005311652A1 (en) 2006-06-08
RU2007125122A (ru) 2009-01-10
ZA200703866B (en) 2008-03-26
EP2586444B1 (en) 2019-09-25
US8852632B2 (en) 2014-10-07
EP1904067B2 (en) 2017-10-11
AU2005311652B2 (en) 2010-12-02
RU2382648C2 (ru) 2010-02-27
NO20073405L (no) 2007-07-02

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Owner name: SCHERING CORP (US)

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Effective date: 20121031

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CP01 Change in the name or title of a patent holder

Address after: New jersey, USA

Patentee after: MERCK SHARP & DOHME Corp.

Address before: New jersey, USA

Patentee before: SCHERING Corp.

TR01 Transfer of patent right

Effective date of registration: 20121031

Address after: New jersey, USA

Patentee after: SCHERING Corp.

Address before: New jersey, USA

Patentee before: MERCK SHARP & DOHME Corp.

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20110330

Termination date: 20161202

CF01 Termination of patent right due to non-payment of annual fee